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Sample records for biological activity evaluation

  1. Physio-chemical evaluation and biological activity of Ajuga ...

    African Journals Online (AJOL)

    Physio-chemical evaluation and biological activity of Ajuga bracteosa wall and Viola odoroto Linn. Anwar Ali Shad, M. Zeeshan, Hina Fazal, Hamid Ullah Shah, Shabir Ahmed, Hasem Abeer, E. F. Abd_Allah, Riaz Ullah, Hamid Afridi, Akash tariq, Muhammad Adnan Asma ...

  2. Synthesis, characterization and evaluation of biological activities of ...

    African Journals Online (AJOL)

    Original Research Article. Synthesis, characterization and evaluation of biological activities of manganese-doped zinc oxide nanoparticles. Shakeel Ahmad Khan1*, Sammia Shahid1, Waqas Bashir1, Sadia Kanwal2 and. Ahsan Iqbal3. 1Department of Chemistry, University of Management and Technology, Lahore-54000, ...

  3. Evaluation of the biological activity of sunflower hull extracts

    Energy Technology Data Exchange (ETDEWEB)

    Taha, F. S.; Wagdy, S. M.; Hassanein, M. M. M.; Hamed, S. F.

    2012-11-01

    This work was planned with the aim of adding value to sunflower seed hulls, a waste product of the oil industry by preparing a sunflower hull phenolic extract rich in chlorogenic acid (CGA). In order to fulfill this goal, the optimization for the extraction of a phenolic extract from the hulls was investigated. The parameters studied were: type of solvent, solvent to water ratio and hull to solvent ratio. In addition, the solvent mixtures were also studied. The resulting phenolic extracts were evaluated for their biological activities. This included phenolic content determination, evaluation of the antioxidant and antimicrobial activities. Chlorogenic acid was determined in two chosen hull extracts using the UV spectrophotometric method and HPLC analysis. The anti carcinogenic activity of the two chosen extracts was tested on seven different cell line carcinomas. The results revealed that all the phenolic extracts of sunflower hull studied contain between 190-312.5 mg phenolics/ 100 g hulls. The highest phenolic extraction was achieved with 80% methanol (1:30, hull to solvent, w/v ratio) and methanol to ethanol to water (7:7:6 v/v/v) mixture with values of 312.5 and 306.5 mg phenolics/100 g hulls, respectively. The free radical scavenging activity and antioxidant activity of all the samples ranged from 33.6-72.6%. The highest antioxidant activity and free radical scavenging activity were achieved by the same extracts that possessed the highest phenolic content, namely methanol to ethanol to water extract and 80% methanol with values 71.8 and 72.6%, 68.2 and 70.9% respectively, compared to 77.9 and 76.9% respectively for TBHQ. All the phenolic extracts possessed antimicrobial activity but to different levels against different pathogenic bacteria. The two chosen extracts also possessed anti carcinogenic activity, which differed among varying cell line carcinomas. The HPLC analysis indicated that chlorogenic acid was the main phenolic acid in the extract. Thus it can

  4. Design, Synthesis, and Biological Evaluation of Isothiosemicarbazones with Antimycobacterial Activity

    Czech Academy of Sciences Publication Activity Database

    Novotná, E.; Waisser, K.; Kuneš, J.; Palát, K.; Skálová, L.; Szotáková, B.; Buchta, V.; Stolaříková, J.; Ulmann, V.; Pávová, Marcela; Weber, Jan; Komrsková, J.; Hašková, P.; Vokřál, I.; Wsól, V.

    2017-01-01

    Roč. 350, č. 8 (2017), č. článku e1700020. ISSN 0365-6233 Institutional support: RVO:61388963 Keywords : biological activity * cytotoxicity * isocitrate lyase * isothiosemicarbazone * tuberculosis Subject RIV: EE - Microbiology, Virology OBOR OECD: Microbiology Impact factor: 1.994, year: 2016

  5. Evaluation of Biological Activities of Chemically Synthesized Silver Nanoparticles

    Directory of Open Access Journals (Sweden)

    Ashraf A. Mostafa

    2015-01-01

    Full Text Available Silver nanoparticles were synthesized by the earlier reported methods. The synthesized nanoparticles were characterized using ultraviolet-visible spectrophotometry (UV/Vis, transmission electron microscopy (TEM, energy dispersive X-ray spectroscopy (EDX, and X-ray powder diffraction (XRD. The synthesized materials were also evaluated for their antibacterial activity against Gram positive and Gram negative bacterial strains. TEM micrograph showed the spherical morphology of AgNPs with size range of 40–60 nm. The synthesized nanoparticles showed a strong antimicrobial activity and their effect depends upon bacterial strain as AgNPs exhibited greater inhibition zone for Pseudomonas aeruginosa (19.1 mm followed by Staphylococcus aureus (14.8 mm and S. pyogenes (13.6 mm while the least activity was observed for Salmonella typhi (12.5 mm at concentration of 5 µg/disc. The minimum inhibitory concentration (MIC of AgNPs against S. aureus was 2.5 µg/disc and less than 2.5 µg/disc for P. aeruginosa. These results suggested that AgNPs can be used as an effective antiseptic agent for infectious control in medical field.

  6. Evaluation of Biological Activities of Chemically Synthesized Silver Nanoparticles

    International Nuclear Information System (INIS)

    Mostafa, A. A.; Solkamy, E.N.; Sayed, Sh. R. M.; Khan, M.; Shaik, M.R.; Al-Warthan, A.; Adil, S.F.

    2015-01-01

    Silver nanoparticles were synthesized by the earlier reported methods. The synthesized nanoparticles were characterized using ultraviolet-visible spectrophotometry (UV/Vis), transmission electron microscopy (TEM), energy dispersive X-ray spectroscopy (EDX), and X-ray powder diffraction (XRD). The synthesized materials were also evaluated for their antibacterial activity against Gram positive and Gram negative bacterial strains. TEM micrograph showed the spherical morphology of AgNPs with size range of 40-60 nm. The synthesized nanoparticles showed a strong antimicrobial activity and their effect depends upon bacterial strain as AgNPs exhibited greater inhibition zone for Pseudomonas aeruginosa (19.1 mm) followed by Staphylococcus aureus (14.8?mm) and S. pyogenes (13.6 mm) while the least activity was observed for Salmonella typhi (12.5 mm) at concentration of 5 μg/disc. The minimum inhibitory concentration (MIC) of AgNPs against S. aureus was 2.5 μg/disc and less than 2.5 μg/disc for P. aeruginosa. These results suggested that AgNPs can be used as an effective antiseptic agent for infectious control in medical field.

  7. Ultrasonic-Assisted Extraction and Evaluation of Biological Activities ...

    African Journals Online (AJOL)

    Flemingia philippinensis and to investigate the antioxidant and anti-tumor activities of the extracts of the materials from various locations in China. Methods: The total flavonoids in F. philippinensis were obtained by ultrasonic-assisted conventional solvent extraction method, and the extraction conditions were optimized by ...

  8. Biological activities of Rumex dentatus L: Evaluation of methanol ...

    African Journals Online (AJOL)

    PRECIOUS

    2009-12-15

    Dec 15, 2009 ... solani, respectively by methanol extracts of roots and leaves. Phytochemical analysis of hexane extracts showed presence of flavor-noids as major constituents, which might be responsible for antifungal activity. (Atindehou et al., 2002). Previously, fungitoxic surface flavonoids (Isoflavonoids) have been ...

  9. Evaluation of some biological activities of Abelia triflora R Br ...

    African Journals Online (AJOL)

    Purpose: To investigate the antioxidant, anti-inflammatory, antidiabetic, cardiovascular and cytotoxic activities of the leaf extract and major compounds isolated from Abelia triflora R. Br. (Caprifoliaceae) Methods: The chloroform soluble fraction of A. triflora leaves was subjected to several column chromatographic ...

  10. Co-evaluation of plant extracts as petrochemical substitutes and for biologically active compounds

    Energy Technology Data Exchange (ETDEWEB)

    McChesney, J.D.; Adams, R.P.

    Recent efforts to discover phytochemicals that could substitute for petroleum-derived fuels and industrial feedstocks have not given much attention to the potential of these same phytochemicals to provide sources of biologically active compounds. The suitability of extraction products made to assess specific plants as potential botanochemical sources has been evaluated for use in screening procedures for evidence of biologically active compounds. Screening procedures for antibacterial, antifungal and toxic properties are discussed. Screening results are presented for extracts of nearly 80 species of plants from the southeastern United States and southern Great Plains that had previously been evaluated as sources of botanochemicals.

  11. Synthesis and biological evaluation of arctigenin ester and ether derivatives as activators of AMPK.

    Science.gov (United States)

    Shen, Sida; Zhuang, Jingjing; Chen, Yijia; Lei, Min; Chen, Jing; Shen, Xu; Hu, Lihong

    2013-07-01

    A series of new arctigenin and 9-deoxy-arctigenin derivatives bearing different ester and ether side chains at the phenolic hydroxyl positions are designed, synthesized, and evaluated for activating AMPK potency in L6 myoblasts. Initial biological evaluation indicates that some alkyl ester and phenethyl ether arctigenin derivatives display potential activities in AMPK phosphorylation improvement. Further structure-activity relationship analysis shows that arctigenin ester derivatives 3a, 3h and 9-deoxy-arctigenin phenethyl ether derivatives 6a, 6c, 6d activate AMPK more potently than arctigenin. Moreover, the 2-(3,4-dimethoxyphenyl)ethyl ether moiety of 6c has been demonstrated as a potential functional group to improve the effect of AMPK phosphorylation. The structural optimization of arctigenin leads to the identification of 6c as a promising lead compound that exhibits excellent activity in AMPK activation. Copyright © 2013 The Authors. Published by Elsevier Ltd.. All rights reserved.

  12. [Evaluation of the concordance between biological markers and clinical activity in inflammatory bowel disease].

    Science.gov (United States)

    Miranda García, Pablo; Chaparro, María; Gisbert, Javier P

    2015-01-06

    Endoscopy is the gold standard to assess disease severity in inflammatory bowel disease, although it is an invasive procedure. Clinical activity and biological markers have been routinely used to determine disease activity in a non-invasive manner. The aim of this study was to determine concordance between common biological markers (C reactive protein, orosomucoid, erythrocyte sedimentation rate, fibrinogen, platelets, leukocytes, neutrophils and haemoglobin) and clinical activity in inflammatory bowel disease. Consecutive patients with inflammatory bowel disease were included. Clinical activity was evaluated according to the Harvey-Bradshaw index in Crohn's disease and to the partial Mayo score in ulcerative colitis. Serum concentrations of the different biomarkers were analysed. Concordance between clinical activity and elevation of the serological biomarkers was determined using the kappa statistic. In total, 350 patients were included (median age 46 years, Crohn's disease 59%). Eleven percent of patients had clinical activity. Crohn's disease patients had mild clinical activity in 44% of cases, moderate disease in 44% and only 12% of patients had severe clinical activity. In ulcerative colitis, patients had mild, moderate and severe clinical activity in 50, 42 and 8% of cases, respectively. None of the biomarkers included had an acceptable concordance with clinical activity (kappa statistic ≤ 0.30). Concordance between serological biomarkers and clinical activity in inflammatory bowel disease is remarkably low. Copyright © 2013 Elsevier España, S.L.U. All rights reserved.

  13. Evaluating the biological activity of oil-polluted soils using a complex index

    Science.gov (United States)

    Kabirov, R. R.; Kireeva, N. A.; Kabirov, T. R.; Dubovik, I. Ye.; Yakupova, A. B.; Safiullina, L. M.

    2012-02-01

    A complex index characterizing the biological activity of soils (BAS) is suggested. It is based on an estimate of the level of activity of catalase; the number of heterotrophic and hydrocarbon oxidizing microorganisms, microscopic fungi, algae, and cyanobacteria; and the degree of development of higher plants and insects in the studied soil. The data on using the BAS coefficient for evaluating the efficiency of rehabilitation measures for oil-polluted soils are given. Such measures included introducing the following biological preparations: Lenoil based on a natural consortium of microorganisms Bacillus brevis and Arthrobacter sp.; the Azolen biofertilizer with complex action based on Azotobacter vinelandii; the Belvitamil biopreparation, which is the active silt of pulp and paper production; and a ready-mixed industrial association of aerobic and anaerobic microorganisms that contains hydrocarbon oxidizing microorganisms of the Arthrobacter, Bacillus, Candida, Desulfovibrio, and Pseudomonas genera.

  14. Evaluation of Biologically Active Compounds from Calendula officinalis Flowers using Spectrophotometry

    Science.gov (United States)

    2012-01-01

    Background This study aimed to quantify the active biological compounds in C. officinalis flowers. Based on the active principles and biological properties of marigolds flowers reported in the literature, we sought to obtain and characterize the molecular composition of extracts prepared using different solvents. The antioxidant capacities of extracts were assessed by using spectrophotometry to measure both absorbance of the colorimetric free radical scavenger 2,2-diphenyl-1-picrylhydrazyl (DPPH) as well as the total antioxidant potential, using the ferric reducing power (FRAP) assay. Results Spectrophotometric assays in the ultraviolet-visible (UV-VIS) region enabled identification and characterization of the full range of phenolic and flavonoids acids, and high-performance liquid chromatography (HPLC) was used to identify and quantify phenolic compounds (depending on the method of extraction). Methanol ensured more efficient extraction of flavonoids than the other solvents tested. Antioxidant activity in methanolic extracts was correlated with the polyphenol content. Conclusions The UV-VIS spectra of assimilator pigments (e.g. chlorophylls), polyphenols and flavonoids extracted from the C. officinalis flowers consisted in quantitative evaluation of compounds which absorb to wavelengths broader than 360 nm. PMID:22540963

  15. Evaluation of flow injection analysis for determination of cholinesterase activities in biological material.

    Science.gov (United States)

    Cabal, Jiri; Bajgar, Jiri; Kassa, Jiri

    2010-09-06

    The method for automatic continual monitoring of acetylcholinesterase (AChE) activity in biological material is described. It is based on flexible system of plastic pipes mixing samples of biological material with reagents for enzyme determination; reaction product penetrates through the semipermeable membrane and it is spectrophotometrically determined (Ellman's method). It consists of sampling (either in vitro or in vivo), adding the substrate and flowing to dialyzer; reaction product (thiocholine) is dialyzed and mixed with 5,5'-dithio-bis-2-nitrobenzoic acid (DTNB) transported to flow spectrophotometer. Flowing of all materials is realised using peristaltic pump. The method was validated: time for optimal hydratation of the cellophane membrane; type of the membrane; type of dialyzer; conditions for optimal permeation of reaction components; optimization of substrate and DTNB concentrations (linear dependence); efficacy of peristaltic pump; calibration of analytes after permeation through the membrane; excluding of the blood permeation through the membrane. Some examples of the evaluation of the effects of AChE inhibitors are described. It was demonstrated very good uniformity of peaks representing the enzyme activity (good reproducibility); time dependence of AChE inhibition caused by VX in vitro in the rat blood allowing to determine the half life of inhibition and thus, bimolecular rate constants of inhibition; reactivation of inhibited AChE by some reactivators, and continual monitoring of the activity in the whole blood in vivo in intact and VX-intoxicated rats. The method is simple and not expensive, allowing automatic determination of AChE activity in discrete or continual samples in vitro or in vivo. It will be evaluated for further research of cholinesterase inhibitors. Copyright (c) 2010 Elsevier Ireland Ltd. All rights reserved.

  16. Evaluation of biological activity of Uncaria tomentosa (Willd.) DC. using the chicken embryo model.

    Science.gov (United States)

    Pilarski, Radosław; Bednarczyk, Marek; Gulewicz, Krzysztof

    2009-01-01

    The biological activity of Uncaria tomentosa (Willd.) DC. (cat's claw) was evaluated by application of the chicken embryo model. Among three groups of eggs (n = 360) with twelve-day old embryos, two were injected with different doses of cat's claw extracts (0.0492 and 0.492 mg/200 lambda). To the third control group 200 lambda of physiological salt was applied. All eggs were incubated in conventional forced-air apparatus until hatched. Hatchability, chicken weight and wholesomeness were analyzed. Selected parameters of blood including number of erythrocytes (RBC), number of leukocytes (WBC), mean red cell volume (MCV), hematocrit (HCT), hemoglobin concentration (HGB), mean amount of cell hemoglobin (MCH), mean cell hemoglobin concentration (MCHC) and embryo weight (MAS) were assayed and compared. Significant differences with ANOVA were observed for MCV (P = 0.002), MCHC (P = 0.00001) and MCH (P = 0.02). Applying the chicken embryo model brought new information about the biological activity of U. tomentosa showing an unfavourable effect on some morphological blood parameters.

  17. Synthesis, biological evaluation, QSAR analysis, and molecular docking of chalcone derivatives for antimalarial activity

    Directory of Open Access Journals (Sweden)

    Jufrizal Syahri

    2017-01-01

    Full Text Available Objective: To synthesize chalcone derivatives and investigate their antimalarial activity toward chloroquine-sensitive Plasmodium falciparum 3D7 (Pf3D7 strain; to develop quantitative structureactivity relationships (QSAR model to estimate IC50 values for biological activity of antimalarial and compared to experimental measurement; and to determine the binding interactions of the most active compounds with targeting P. falciparum dihydrofolate reductase-thymidylate synthase using molecular docking simulation. Methods: Seven chalcone derivatives have been synthesized from substituted acetophenone and substituted benzaldehyde in ethanol with the presence of bases catalysis at reflux condition. The QSAR analysis was conducted by using Gaussian 09 software to predict IC50 value for antimalarial activity. The in vitro test was evaluated against the chloroquine-sensitive Pf3D7 strain. Finally, the docking studies were performed with the CDOCKER protocol under the receptor-ligand interaction section in Discovery Studio® 3.1 (Accelrys, Inc., San Diego, USA. Results: Among the synthesized chalcone, a prenylated chalcone 5c and an allylated chalcones 10a showed the best IC 50 values of 1.08 and 1.73 μg/mL respectively against Pf3D7 strain (1.37 and 2.33 μg/mL based on QSAR analysis. Comparison between the prediction of IC50 value generated from the QSAR and the outcome from an in vitro assay showed a similar result as seen from the r2 value (r2 = 0.99. The most active compound 5c was employed in the docking simulation to determine the potential binding interactions with active sites of P. falciparum dihydrofolate reductase-thymidylate synthase (protein data bank ID: 1J3I. The docking simulation study showed 5c bind well with Ala16, Ser108, Ile164, Trp48, and Phe58 which are the crucial interactions that could possibly interrupt the sequential catalysis reactions in the thymidylate cycle and subsequently prevent deoxythymidine monophosphate production

  18. Development and evaluation of an active instructional framework for undergraduate biology education

    Science.gov (United States)

    Lysne, Steven John

    The practice of science education in American colleges and universities is changing and the role of faculty is changing as well. There is momentum in higher education to transform our instruction and do a better job at supporting more students' success in science and engineering programs. New teaching approaches are transforming undergraduate science instruction and new research demonstrates that these new approaches are more engaging for students, result in greater achievement, and create more positive attitudes toward science careers. Additionally, teaching scholars have described a paradigm shift toward placing the burden of content coverage on students which allows more time for in-class activities such as discussion and problem solving. Teaching faculty have been asked to redesign their courses and rebrand themselves as facilitators of student learning, rather than purveyors of information, to improve student engagement, achievement, and attitudes. This dissertation is a critical evaluation of both the assumption that active learning improves student achievement and knowledge retention and my own assumptions regarding science education research and my students' resiliency. This dissertation is a collection of research articles, published or in preparation, presenting the chronological development (Chapters 2 and 3) and evaluation (Chapters 4 and 5) of an active instructional model for undergraduate biology instruction. Chapters 1 and 6.provide a broad introduction and summary, respectively. Chapter 2 is an exploration of student engagement through interviews with a variety of students. From these interviews I identified several themes that students felt were important, and science instructors need to address, including the place where learning happens and strategies for better engaging students. Chapter 3 presents a review of the science education literature broadly and more focused review on the how students learn and how faculty teach. Consistent with what

  19. Synthesis and preliminary biological evaluation of new radioiodinated MMP inhibitors for imaging MMP activity in vivo

    International Nuclear Information System (INIS)

    Kopka, Klaus; Breyholz, Hans-Joerg; Wagner, Stefan; Law, Marilyn P.; Riemann, Burkhard; Schroeer, Sandra; Trub, Monika; Guilbert, Benedicte; Levkau, Bodo; Schober, Otmar; Schaefers, Michael

    2004-01-01

    Non-invasive measurement of matrix metalloproteinase (MMP) activity in vivo is a clinical challenge in many disease processes such as inflammation, tumor metastasis and atherosclerosis. Therefore, radioiodinated analogues of the non-peptidyl broad-spectrum MMP inhibitor (MMPI) CGS 27023A 1a were synthesized for non-invasive detection of MMP activity in vivo using single photon emission computed tomography (SPECT). The compounds Br-CGS 27023A 1b and HO-CGS 27023A 1d were synthesized from the amino acid D-valine and used as precursors for radioiodinated derivatives of CGS 27023A and their non-radioactive references I-CGS 27023A 1c and HO-I-CGS 27023A 1e. Radioiodination of the precursors with [ 123 I]NaI or [ 125 I]NaI produced the no-carrier-added MMP inhibitors [ 123 I]I-CGS 27023A 1f, [ 125 I]I-CGS 27023A 1g, HO-[ 123 I]I-CGS27023A 1h, and HO-[ 125 I]I-CGS 27023A 1i. In vitro studies showed that the non-radioactive analogues of the MMP inhibitors exhibited affinities against gelatinase A (MMP-2) and gelatinase B (MMP-9) in the nanomolar range, comparable to the parent compound CGS 27023A. In vivo biodistribution using HO-[ 125 I]I-CGS 27023A 1i in CL57 Bl6 mice showed rapid blood and plasma clearance and low retention in normal tissues. The preliminary biological evaluation warrant further studies of these radioiodinated MMP inhibitors as potential new radiotracers for imaging MMP activity in vivo

  20. Evaluation of some biological activities of the extracts of corn silk ...

    African Journals Online (AJOL)

    Ethanol and aqueous extracts obtained from the leaves and corn silk of maize were evaluated for antibacterial efficacy especially that there is a folklore claim that they have medicinal value. The aqueous corn silk extract was further used to investigate other biological properties such as acute and sub-acute toxicities; ...

  1. Biological activity evaluation of cloned and expressed caprine growth hormone from local Pakistani goat breed beetal

    International Nuclear Information System (INIS)

    Butt, H.I.; Shahzad, M.I.; Bashir, Q.

    2011-01-01

    Growth hormone cDNA of local goat breed-beetal was amplified by RT PCR and gene including leader sequence was cloned in pTZR57 cloning vector. The cGH-pTZR57 clone was confirmed by restriction digestion and sequence analyses before finally sub-cloning the gene in pND- a mammalian expression vector. The clones were again confirmed by restriction digestion and PCR analyses. Highly purified, supercoiled cGH-pND construct was used to transfect Vero cell lines for expression studies. The in vitro expression of cGH was checked by dot-ELISA technique. After confirming its in vitro cell line based expression, the construct was injected to 4 weeks old balb/c mice intramuscularly. Two animals were euthanized per week till four weeks to monitor the in vivo biological activity by evaluating the tibia epiphyseal width and body weight gain assays. Significant increase in tibia epiphyseal width and gain in body weight was observed from vaccinated animals. The study supports the concept that DNA based therapeutics are an efficient and cost effective method for gene delivery and in vivo transgene expressions. (author)

  2. Synthesis, biological evaluation, and structure-activity relationship of clonazepam, meclonazepam, and 1,4-benzodiazepine compounds with schistosomicidal activity.

    Science.gov (United States)

    Menezes, Carla M S; Rivera, Gildardo; Alves, Marina A; do Amaral, Daniel N; Thibaut, Jean Pierre B; Noël, François; Barreiro, Eliezer J; Lima, Lídia M

    2012-06-01

    The inherent morbidity and mortality caused by schistosomiasis is a serious public health problem in developing countries. Praziquantel is the only drug in therapeutic use, leading to a permanent risk of parasite resistance. In search for new schistosomicidal drugs, meclonazepam, the 3-methyl-derivative of clonazepam, is still considered an interesting lead-candidate because it has a proven schistosomicidal effect in humans but adverse effects on the central nervous system did not allow its clinical use. Herein, the synthesis, in vitro biological evaluation, and molecular modeling of clonazepam, meclonazepam, and analogues are reported to establish the first structure-activity relationship for schistosomicidal benzodiazepines. Our findings indicate that the amide moiety [N(1) H-C(2) (=O)] is the principal pharmacophoric unit of 1,4-benzodiazepine schistosomicidal compounds and that substitution on the amide nitrogen atom (N(1) position) is not tolerated. © 2012 John Wiley & Sons A/S.

  3. Biological Activities of Hydrazone Derivatives

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    S. Güniz Küçükgüzel

    2007-08-01

    Full Text Available There has been considerable interest in the development of novel compounds with anticonvulsant, antidepressant, analgesic, antiinflammatory, antiplatelet, antimalarial, antimicrobial, antimycobacterial, antitumoral, vasodilator, antiviral and antischistosomiasis activities. Hydrazones possessing an azometine -NHN=CH- proton constitute an important class of compounds for new drug development. Therefore, many researchers have synthesized these compounds as target structures and evaluated their biological activities. These observations have been guiding for the development of new hydrazones that possess varied biological activities.

  4. Evaluation of biological activities and chemical constituent of storage medicinal plant materials used as a traditional medicine in Nepal

    Directory of Open Access Journals (Sweden)

    Bishnu Prasad Pandey

    2017-12-01

    Full Text Available Aim: The main aims of the study were to evaluate the phytochemicals, antioxidant, antibacterial and chemical constituents of storage medicinal plant materials used as a traditional medicine in Nepal. Methods: Phytochemical screening, total phenolic content, total flavonoid content, antibacterial activities, anti-oxidant assay of the crude extract (water, methanol, n-hexane and acetone were carried out to identify the biological activities and phytonutrients present in the different extract. The chemical constituents present in the crude extract were analyzed using the high performance liquid chromatography (HPLC equipped with UV detector. Results: Evaluated medicinal plant materials were found to have diverse phytonutrients. Results revealed that methanol extract of Pakhanved and Jethimadhu have highest total flavonoids and polyphenol content. Among the selected medicinal plant materials Jethimadhu extract revealed the highest antioxidant activities. Furthermore, evaluated medicinal plants extract were found to exert a range of in vitro growth inhibition activity against both gram positive and gram negative species. The highest antibacterial activities were observed in the case of methanol extract, whereas, least activity was observed with the hexane extract. HPLC analysis of the acetone extract of Jethimadhu reveals the presence of diosmetin. Conclusions: Our result revealed that among the five evaluated medicinal plant materials, Jethimadhu extract revealed biological activities and exhibits a higher amount of polyphenol and flavonoid content. [J Complement Med Res 2017; 6(4.000: 369-377

  5. Evaluation of biological activities of nanocrystalline zirconia synthesis via combustion method

    International Nuclear Information System (INIS)

    Thakare, V.G.; Omanwar, S.K.; Bhatkar, V.B.; Wadegaokar, P.A.

    2016-01-01

    The objective of the following study was synthesis of nanocrystalline zirconia by modified solution combustion synthesis method and evaluation of its structural and biological properties. The sample was characterized by powder X-ray diffraction (XRD), Field Emission Scanning Electron Microscopy (FESEM) and evaluated for cytotoxicity study using 3T3 mouse fibroblast cells, the antibacterial property are investigated by spread plate method against E. coli bacterial pathogen and studied for degradation using phosphate buffered saline (PBS) solution. The XRD pattern shows that the monoclinic phase of nanocrystalline zirconia was obtained. The FESEM images showed that the prepared sample consists of particles in the range of 45 nm and homogenous particle size distribution. The sample of zirconia has excellent tissue biocompatibility and does not show any toxicity towards normal 3T3 mouse fibroblast cells. It also inhibited the bacterial growth. The sample shows stability at physiological condition and does not show degradation. (author)

  6. Expression of bovine interleukin 15 and evaluation of its biological activity in vitro

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    N. Vijay

    2015-03-01

    Full Text Available Background/Aim: Recent studies have shown that interleukin-15 (IL-15is a critical factor for the development and proliferation of CD8+ memory T cells. The aim of present study is to study the role bovine IL-15 (bIL-15in activation pathway of bovine CD8+ T cells if any, which will be useful in designing the adjuvant to increase the duration of immunity of the vaccine preparations. Materials and Methods: Coding region of bIL-15 (489 was amplified from cDNA of lipopolysaccharide-induced bovine peripheral blood mononuclear cells (PBMCs using gene specific primers and cloned into pcDNA3.1+. Mature length of bIL-15 was amplified using gene specific primers and cloned into pET32a for expression studies. Expressed fusion protein was purified using Ni-Nitrilotriacetic acid agarose affinity chromatography and analyzed by SDS-Polyacryamide gel electrophoresis (PAGE and western blotting. Biological activity of purified protein was analyzed by quantitative Polymerase Chain Reaction (qPCR for an increase in levels of Bcl2, STAT3 and STAT5a using cDNA synthesized from RNA of PBMCs induced with different concentrations of purified bIL-15. Role of IL-15 in inducing memory CD8+ T cells was analyzed by qPCR for increase in the level of Carnitine Palmitoyl Transferase 1a (CPT1a using cDNA synthesized from RNA of PBMCs induced with different concentrations of purified bIL-15. Results: Bovine IL-15 was amplified and analyzed by agarose gel electrophoresis, which showed a specific product of ~490bp, mature sequence was amplified using full-length as a template to get a product of ~350bp. The protein was expressed, purified and analyzed by SDS-PAGE and Western blotting, which showed a specific product of 32kDa. Biological activity of purified bIL-15 fusion protein showed an increase in levels of Bcl2, STAT3 and STAT5a with 5 fold, 9 fold, and 10 fold increases as analyzed by qPCR, respectively. Role of IL-15 in inducing memory T cells showed an increase in expression

  7. Design and biological evaluation of biphenyl-4-carboxylic acid hydrazide-hydrazone for antimicrobial activity.

    Science.gov (United States)

    Deep, Aakash; Jain, Sandeep; Sharma, Prabodh Chander; Verma, Prabhakar; Kumar, Mahesh; Dora, Chander Parkash

    2010-01-01

    Seven biphenyl-4-carboxylic acid hydrazide-hydrazones have been synthesized. These hydrazone derivatives were characterized by CHN analysis, IR, and 1H NMR spectral data. All the compounds were evaluated for their in vitro antimicrobial activity against two Gram negative strains (Escherichia coli and Pseudomonas aeruginosa) and two Gram positive strains (Bacillus subtilis and Staphylococcus aureus) and fungal strain Candida albicans and Aspergillus niger All newly synthesized compounds exhibited promising results.

  8. Parallel synthesis and biological evaluation of 837 analogues of procaspase-activating compound 1 (PAC-1).

    Science.gov (United States)

    Hsu, Danny C; Roth, Howard S; West, Diana C; Botham, Rachel C; Novotny, Chris J; Schmid, Steven C; Hergenrother, Paul J

    2012-01-09

    Procaspase-Activating Compound 1 (PAC-1) is an ortho-hydroxy N-acyl hydrazone that enhances the enzymatic activity of procaspase-3 in vitro and induces apoptosis in cancer cells. An analogue of PAC-1, called S-PAC-1, was evaluated in a veterinary clinical trial in pet dogs with lymphoma and found to have considerable potential as an anticancer agent. With the goal of identifying more potent compounds in this promising class of experimental therapeutics, a combinatorial library based on PAC-1 was created, and the compounds were evaluated for their ability to induce death of cancer cells in culture. For library construction, 31 hydrazides were condensed in parallel with 27 aldehydes to create 837 PAC-1 analogues, with an average purity of 91%. The compounds were evaluated for their ability to induce apoptosis in cancer cells, and through this work, six compounds were discovered to be substantially more potent than PAC-1 and S-PAC-1. These six hits were further evaluated for their ability to relieve zinc-mediated inhibition of procaspase-3 in vitro. In general, the newly identified hit compounds are two- to four-fold more potent than PAC-1 and S-PAC-1 in cell culture, and thus have promise as experimental therapeutics for treatment of the many cancers that have elevated expression levels of procaspase-3.

  9. Synthesis and Biological Evaluation of Novel 3-Alkylpyridine Marine Alkaloid Analogs with Promising Anticancer Activity

    Directory of Open Access Journals (Sweden)

    Alessandra Mirtes Marques Neves Gonçalves

    2014-07-01

    Full Text Available Cancer continues to be one of the most important health problems worldwide, and the identification of novel drugs and treatments to address this disease is urgent. During recent years, marine organisms have proven to be a promising source of new compounds with action against tumoral cell lines. Here, we describe the synthesis and anticancer activity of eight new 3-alkylpyridine alkaloid (3-APA analogs in four steps and with good yields. The key step for the synthesis of these compounds is a Williamson etherification under phase-transfer conditions. We investigated the influence of the length of the alkyl chain attached to position 3 of the pyridine ring on the cytotoxicity of these compounds. Biological assays demonstrated that compounds with an alkyl chain of ten carbon atoms (4c and 5c were the most active against two tumoral cell lines: RKO-AS-45-1 and HeLa. Micronucleus and TUNEL assays showed that both compounds are mutagenic and induce apoptosis. In addition, Compound 5c altered the cellular actin cytoskeleton in RKO-AS-45-1 cells. The results suggest that Compounds 4c and 5c may be novel prototype anticancer agents.

  10. Evaluation of Chemical Composition and Biological Activities of Citrus pseudolimon and Citrus grandis Peel Essential Oils

    International Nuclear Information System (INIS)

    Sajid, A.; Hanif, M.A.; Shahid, M.

    2016-01-01

    Essential oils and their volatile constituents are used extensively to prevent and treat human diseases. In the past decades, worldwide demand for citrus essential oils has greatly increased. Citrus essential oils containing 85-99 percent volatile and 1-15 percent non-volatile components. Essential oils from Citrus pseudolimon and Citrus grandis peels were extracted through steam distillation and characterized by GC-MS. C. pseudolimon has thirty six and C. grandis has thirty three total components; limonene 47.07 percent and 71.48 percent was the major component in both oils respectively. Antioxidant activity was checked by 2, 2-diphenyl-1-picrylhydrazyl radical assay and β-carotene/linoleic acid bleaching test. Both oils have modest activity. The antimicrobial potential was assessed against different bacterial and fungus strains. C. pseudolimon oil possessed strong activity against all tested strains while C. grandis has moderate activity. The antitumor activity was evaluated by potato disc assay, C. pseudolimon showed 81.25 inhibition. Hence the essential oils could have a great potential in pharmaceutical industry. (author)

  11. Synthesis, characterization and evaluation of biological activities of some 2,3-diaryl bicyclo methanones

    Directory of Open Access Journals (Sweden)

    Thirunarayanan Ganesamoorthy

    2016-06-01

    Full Text Available Sixteen (3,4-dichlorophenyl-3-(substituted phenylbicyclo[2.2.1]hept-5-ene-2-yl methanone derivatives have been synthesized by an aqueous phase fly-ash catalyzed [4+2] cycloaddition Diels-Alder reaction of cyclopentadiene and 3,4-dichloro phenyl chalcones. The yields of the methanones were greater than 60%. The synthesized methanones were characterized by their physical constants and spectral data. The antimicrobial and antioxidant activities of the synthesized methanones were evaluated using a variety of bacterial and fungal species and DPPH radical scavenging methods.

  12. Arylthioindole inhibitors of tubulin polymerization. 3. Biological evaluation, structure-activity relationships and molecular modeling studies.

    Science.gov (United States)

    La Regina, Giuseppe; Edler, Michael C; Brancale, Andrea; Kandil, Sahar; Coluccia, Antonio; Piscitelli, Francesco; Hamel, Ernest; De Martino, Gabriella; Matesanz, Ruth; Díaz, José Fernando; Scovassi, Anna Ivana; Prosperi, Ennio; Lavecchia, Antonio; Novellino, Ettore; Artico, Marino; Silvestri, Romano

    2007-06-14

    The new arylthioindole (ATI) derivatives 10, 14-18, and 21-24, which bear a halogen atom or a small size ether group at position 5 of the indole moiety, were compared with the reference compounds colchicine and combretastatin A-4 for biological activity. Derivatives 10, 11, 16, and 21-24 inhibited MCF-7 cell growth with IC50 values <50 nM. A halogen atom (14-17) at position 5 caused a significant reduction in the free energy of binding of compound to tubulin, with a concomitant reduction in cytotoxicity. In contrast, methyl (21) and methoxy (22) substituents at position 5 caused an increase in cytotoxicity. Compound 16, the most potent antitubulin agent, led to a large increase (56%) in HeLa cells in the G2/M phase at 24 h, and at 48 h, 26% of the cells were hyperploid. Molecular modeling studies showed that, despite the absence of the ester moiety present in the previously examined analogues, most of the compounds bind in the colchicine site in the same orientation as the previously studied ATIs. Binding to beta-tubulin involved formation of a hydrogen bond between the indole and Thr179 and positioning of the trimethoxy phenyl group in a hydrophobic pocket near Cys241.

  13. Development of parenteral formulations and evaluation of the biological activity of the trypanocide drug benznidazole.

    Science.gov (United States)

    Lamas, María C; Villaggi, Luciano; Nocito, Isabel; Bassani, Georgina; Leonardi, Darío; Pascutti, Fernanda; Serra, Esteban; Salomón, Claudio J

    2006-01-13

    Chagas disease, caused by Trypanosoma cruzi, is a major public health problem in Latin America. According to the World Health Organization, around 20 million people are infected and another 40 million are at risk of acquiring the disease. One of the drugs most frequently used for the treatment of Chagas disease is benznidazole (BZL). It is practically insoluble in water (0.4 mg/ml), which precludes the preparation of liquid dosage forms, in particular, parenteral formulations. Thus, the aim of this work was to investigate the solubilization of BZL at two pH values using various cosolvents such as ethyl alcohol, propylene glycol, polyethylene glycol 400, benzyl alcohol, diethylene glycol monoethyl ether (Transcutol) and surfactants such as polysorbates (Tween) 40 and 80, and sodium dioctyl sulfosuccinate (AOT). Solvent systems based on PEG 400, with the addition ethyl alcohol and/or potassium biphthalate buffer solution, increased the BZL solubility up to 10 mg/ml. These alcoholic vehicles showed no toxicity against parasite when assayed at 1%. Physical and chemical stability studies showed that the formulations were stable for at least 1.5 years. In agreement with the biological activity results, the selected formulations are suitable for further clinical studies. Moreover, increasing the aqueous solubility of BZL reduced the problems in vitro testing techniques and bioassays leading to more reliable results and/or reproducibility.

  14. Design, synthesis and biological evaluation of novel isoniazid derivatives with potent antitubercular activity.

    Science.gov (United States)

    Martins, Filomena; Santos, Susana; Ventura, Cristina; Elvas-Leitão, Ruben; Santos, Lídia; Vitorino, Susana; Reis, Marina; Miranda, Vanessa; Correia, Henrique F; Aires-de-Sousa, João; Kovalishyn, Vasyl; Latino, Diogo A R S; Ramos, Jorge; Viveiros, Miguel

    2014-06-23

    The disturbing emergence of multidrug-resistant strains of Mycobacterium tuberculosis (Mtb) has been driving the scientific community to urgently search for new and efficient antitubercular drugs. Despite the various drugs currently under evaluation, isoniazid is still the key and most effective component in all multi-therapeutic regimens recommended by the WHO. This paper describes the QSAR-oriented design, synthesis and in vitro antitubercular activity of several potent isoniazid derivatives (isonicotinoyl hydrazones and isonicotinoyl hydrazides) against H37Rv and two resistant Mtb strains. QSAR studies entailed RFs and ASNNs classification models, as well as MLR models. Strict validation procedures were used to guarantee the models' robustness and predictive ability. Lipophilicity was shown not to be relevant to explain the activity of these derivatives, whereas shorter N-N distances and lengthy substituents lead to more active compounds. Compounds 1, 2, 4, 5 and 6, showed measured activities against H37Rv higher than INH (i.e., MIC ≤ 0.28 μM), while compound 9 exhibited a six fold decrease in MIC against the katG (S315T) mutated strain, by comparison with INH (i.e., 6.9 vs. 43.8 μM). All compounds were ineffective against H37RvINH (ΔkatG), a strain with a full deletion of the katG gene, thus corroborating the importance of KatG in the activation of INH-based compounds. The most potent compounds were also shown not to be cytotoxic up to a concentration 500 times higher than MIC. Copyright © 2014 Elsevier Masson SAS. All rights reserved.

  15. Phytochemical profiles and biological activity evaluation of Zanthoxylum bungeanum Maxim seed against asthma in murine models.

    Science.gov (United States)

    Tang, Weizhuo; Xie, Qiangmin; Guan, Jian; Jin, Saihong; Zhao, Yuqing

    2014-03-28

    Zanthoxylum bungeanum Maxim seed (ZBMS) has been used in Traditional Chinese Medicine (TCM) as an ingredient of polyherbal formulations for the treatment of inflammation and asthma. The aim of this study was to analyze the major composition and to evaluate the anti-asthma activity of ZBMS. Some murine models including acetylcholine/histamine-induced asthma, ovalbumin-induced airway inflammation, ear edema and toe swelling measurement, citric acid-induced cough, and anti-stress abilities were investigated to fully study the anti-asthma activity of ZBMS.GC chromatography was also performed to analyze the major fatty acid composition of ZBMS. The results demonstrated that the major fatty acid composition of ZBMS includes oleic acid (20.15%), linoleic acid (26.54%), and α-linolenic acid (30.57%), which was the leading component of ZBMS, and that the total fatty acid content of ZBMS was 77.27%. The murine models demonstrated that ZBMS displays a protective effect on guinea pig sensitization, a dose-dependent inhibition of the increases in RL and decreases in Cdyn, which resulted in the relief of auricle edema and toe swelling in mice and anti-stress activity. Our results validate the traditional use of ZBMS for the treatment of asthma and other inflammatory joint disorders, and suggest that ZBMS has potential as a new therapeutic agent for asthma management. Copyright © 2014 Elsevier Ireland Ltd. All rights reserved.

  16. Flavonoids as Vasorelaxant Agents: Synthesis, Biological Evaluation and Quantitative Structure Activities Relationship (QSAR Studies

    Directory of Open Access Journals (Sweden)

    Yongzhou Hu

    2011-09-01

    Full Text Available A series of 2-(2-diethylamino-ethoxychalcone and 6-prenyl(or its isomers-flavanones 10a,b and 11a–g were synthesized and evaluated for their vasorelaxant activities against rat aorta rings pretreated with 1 μM phenylephrine (PE. Several compounds showed potent vasorelaxant activities. Compound 10a (EC50 = 7.6 μM, Emax = 93.1%, the most potent one, would be a promising structural template for development of novel and more efficient vasodilators. Further, 2D-QSAR analysis of compounds 10a,b and 11c-e as well as thirty previously synthesized flavonoids 1-3 and 12-38 using Enhanced Replacement Method-Multiple Linear Regression (ERM-MLR was further performed based on an optimal set of molecular descriptors (H5m, SIC2, DISPe, Mor03u and L3m, leading to a reliable model with good predictive ability (Rtrain2 = 0.839, Qloo2 = 0.733 and Rtest2 = 0.804. The results provide good insights into the structure- activity relationships of the target compounds.

  17. Evaluation of chemical composition and biological activity of the aerial parts of Artemisia fragrans

    Directory of Open Access Journals (Sweden)

    P. Akbari

    2017-11-01

    Full Text Available Background and objectives: The genus Artemisia, an important member of the Asteraceae family, is mostly distributed in Europe, North America, Asia and South Africa, and represented in Iranian flora by 34 species. In the Iranian traditional medicine these plants were used as anthelmintic and anti-inflammatory. The presence of sesquiterpene lactones and germacranolides were reported in A. fragrans. Our objective in this investigation was to identify the chemical constituents and antioxidant activity of A. fragrans. Methods: The essential oil (EO and different extracts (n-hexane, dichloromethane, and methanol of the aerial parts of A. fragrans were obtained by hydro-distillation and Soxhlet apparatus. The essential oil was analyzed by GC-MS and GC-FID. For further investigation, the MeOH extract (2 g was subjected to Sep-Pack fractionation using a step gradient of MeOH-water. Moreover, the free radical scavenging activity of the EO and extracts was evaluated by the 2, 2-diphenyl -1-picrylhydrazyl (DPPH method. Results: The GC-MS analysis, led to the identification of six main monoterpenes accounting for the 88.7% of the total components present. Among the extracts, camphor was the main component. The essential oil of A. fragrans displayed weak antioxidant activity whereas the antioxidant activity of the MeOH extract was high. The analysis of the 20% and 40% methanolic Sep-Pack fractions resulted in the isolation of two flavonoid glycosides and one dipeptide. Conclusion: The results of the present study introduced A. fragrans as a new source of flavonoid glycosides and suggested it as an appropriate candidate for further radical scavenging studies.

  18. Evaluation of some procedures relevant to the determination of trace elemental components in biological materials by destructive neutron activation analysis

    International Nuclear Information System (INIS)

    Berry, D.L.

    1979-01-01

    The development of a simplified procedure for the analysis of biological materials by destructive neutron activation analysis (DNAA) is described. The sample manipulations preceding gamma ray assay were investigated as five specific stages of processing: (1) pre-irradiation treatment; (2) sample irradiation; (3) removal of the organic matrix; (4) removal of interfering radioactivities; and (5) concentration and separation of analyte activities. Each stage was evaluated with respect to susceptibility to sample contamination, loss of trace elemental components, and compatibility with other operations in the overall DNAA procedures. A complete DNAA procedure was proposed and evaluated for the analysis of standard bovine liver and blood samples. The DNAA system was effective for the determination of As, Cu, Fe, Hg, Mo, Rb, Sb, Se, and Zn without yield determinations and with a minimum turn-around time of approximately 3 days

  19. Evaluation of some procedures relevant to the determination of trace elemental components in biological materials by destructive neutron activation analysis

    Energy Technology Data Exchange (ETDEWEB)

    Berry, D.L.

    1979-01-01

    The development of a simplified procedure for the analysis of biological materials by destructive neutron activation analysis (DNAA) is described. The sample manipulations preceding gamma ray assay were investigated as five specific stages of processing: (1) pre-irradiation treatment; (2) sample irradiation; (3) removal of the organic matrix; (4) removal of interfering radioactivities; and (5) concentration and separation of analyte activities. Each stage was evaluated with respect to susceptibility to sample contamination, loss of trace elemental components, and compatibility with other operations in the overall DNAA procedures. A complete DNAA procedure was proposed and evaluated for the analysis of standard bovine liver and blood samples. The DNAA system was effective for the determination of As, Cu, Fe, Hg, Mo, Rb, Sb, Se, and Zn without yield determinations and with a minimum turn-around time of approximately 3 days.

  20. Evaluation of Biological Activity and Computer-Aided Design of New Soft Glucocorticoids.

    Science.gov (United States)

    Dobričić, Vladimir; Jaćević, Vesna; Vučićević, Jelica; Nikolic, Katarina; Vladimirov, Sote; Čudina, Olivera

    2017-05-01

    Soft glucocorticoids are compounds that are biotransformed to inactive and non-toxic metabolites and have fewer side effects than traditional glucocorticoids. A new class of 17β-carboxamide steroids has been recently introduced by our group. In this study, local anti-inflammatory activity of these derivatives was evaluated by use of the croton oil-induced ear edema test. Glucocorticoids with the highest maximal edema inhibition (MEI) were pointed out, and the systemic side effects of those with the lowest EC 50 values were significantly lower in comparison to dexamethasone. A 3D-QSAR model was created and employed for the design of 27 compounds. By use of the sequential combination of ligand-based and structure-based virtual screening, three compounds were selected from the ChEMBL library and used as a starting point for the design of 15 derivatives. Molecular docking analysis of the designed derivatives with the highest predicted MEI and relative glucocorticoid receptor binding affinity (20, 22, 24-1, 25-1, 27, VS7, VS13, and VS14) confirmed the presence of interactions with the glucocorticoid receptor that are important for the activity. © 2017 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

  1. Phytochemical analysis and biological activity evaluation of essential oil of Scrophularia atropatana

    Directory of Open Access Journals (Sweden)

    H. Tabibi

    2017-11-01

    Full Text Available Background and objectives: Scrophularia atropatana (S. atropatana is endemic to western and central regions of Iran. It belongs to the genus of Scrophularia (family: Scrophulariaceae. These species have been found to possess antibacterial, antitumor and anti-inflammatory properties. Most of these effects were proven to be attributed to the non-volatile components, which were known as secondary metabolites. Iridoids, phenylpropanoids, phenolic acids and flavonoids have been identified as their main secondary metabolites. This investigation was performed to analyze the composition of the essential oil (EO of S. atropatana and evaluation of its anti-oxidant and total toxicity properties. Methods: About 150 g powder of the air dried parts of S. atropatana was submitted to hydro-distillation and also was successively extracted (with n-hexane, dichloromethane (DCM and methanol (MeOH, by using Clevenger and Soxhlet apparatus, respectively. In addition, Essential Oil (EO was analyzed by GC-MS and GC-FID. Furthermore, the anti-oxidant activity of the extracts, fractions and EO as well as general toxicity were investigated by DPPH and brine shrimp larva assay, respectively. Results: Totally, sixty eight volatile compounds were identified, which constituted 91.78% of the total oil composition. Among the compounds, major constituents were identified as non-terpenoides (59.59%. Moreover, among the extracts and EO, methanol extract demonstrated high free radical scavenging and general toxic activities with RC50 equal 0.143±0.13 mg/mL and LD50 0.271 mcg/mL respectively. Conclusion: Overall, the main constituents of S. atropatana were hydrocarbons. In comparison to other genesis of Scrophularia, antioxidant activity of the essential oil of S. atropatana was less noticeable.

  2. Biological activity evaluation of magnesium fluoride coated Mg-Zn-Zr alloy in vivo.

    Science.gov (United States)

    Jiang, Hongfeng; Wang, Jingbo; Chen, Minfang; Liu, Debao

    2017-06-01

    To explore the biodegradable characteristics and biological properties, which could promote new bone formation, of MgF 2 coated magnesium alloy (Mg-3wt%Zn-0.5wt%Zr) in rabbits. Magnesium alloy with MgF 2 coating was made and the MgF 2 /Mg-Zn-Zr was implanted in the femoral condyle of rabbits. Twelve healthy adult Japanese white rabbits in weight of 2.8-3.2kg were averagely divided into A(Mg-Zn-Zr) group and B(MgF 2 /MgZn-Zr) group. Indexes such as microstructural evolution, SEM scan, X-ray, Micro-CT and mechanical properties were observed and detected at 1th day, 2th, 4th, 8th, 12th, 24th week after implantation. Low-density regions occurred around the cancellous bone, and the regions gradually expanded during the 12weeks after implantation. The implant was gradually absorbed from 12 to 24weeks. The density of surrounding cancellous bone increased compared with the 12th week data. The degradation rate of B group was lower than that of A group (Pmagnesium ions. The biological properties of the coating itself presented good biocompatibility and bioactivity. Copyright © 2017 Elsevier B.V. All rights reserved.

  3. Comparison of real time RT-PCR and flow cytometry methods for evaluation of biological activity of recombinant human erythropoietin

    Directory of Open Access Journals (Sweden)

    Sepehrizadeh Z

    2008-05-01

    Full Text Available Background: Evaluation of bioactivity of recombinant erythropoietin is essential for pharmaceutical industry, quality control authorities and researchers. The purpose of this study was to compare real time RT-PCR and flow cytometry for the assay of biological activity of recombinant erythropoietin. Methods: Three concentrations of recombinant erythropoietin BRP (80, 40 and 20 IU/ml were injected subcutaneously to mice. After 4 days the blood was collected and used for reticulocyte counts by flow cytometry and also for the RNA extraction. Real time RT-PCR amplification was carried out for β-globin. Results and conclusion: There was a significant correlation between the total RNA amounts (R2= 0.9995, relative quantity of β-globin mRNA (R2= 0.984 and reticulocyte counts (R2= 0.9742 with rhEpo concentrations. Total RNA and quantitative RT-PCR showed significant dose dependent results as well the reticulocyte counts by flow cytometry for the biological activity assay of rhEpo and so these methods could be considered as alternatives for flow cytometry.

  4. Biological and structure-activity evaluation of chalcone derivatives against bacteria and fungi

    Energy Technology Data Exchange (ETDEWEB)

    Silva, Wender A.; Andrade, Carlos Kleber Z.; Napolitano, Hamilton B., E-mail: wender@unb.br, E-mail: ckleber@unb.br [Universidade de Brasilia (LaQMOS/UnB), DF (Brazil). Inst. de Quimica; Vencato, Ivo; Castro, Miriam R.C. de; Camargo, Ademir J. [Universidade Estadual de Goias (UEG), Anapolis, GO (Brazil). Ciencias Exatas e Tecnologicas; Lariucci, Carlito [Universidade Estadual de Goias (UEG), Goiania, GO (Brazil). Inst. de Fisica

    2013-01-15

    The present work describes the antibacterial and antifungal activities of several chalcones obtained by a straight Claisen-Schmidt aldol condensation determined by the minimal inhibitory concentration against different microorganisms (Gram-positive and Gram-negative bacteria and fungi). Solid state crystal structures of seven chalcones were determined by X-ray diffraction (XRD) analysis. Chemometric studies were carried out in order to identify a potential structure activity relationship. (author)

  5. Biological and structure-activity evaluation of chalcone derivatives against bacteria and fungi

    OpenAIRE

    Silva, Wender A.; Andrade, Carlos Kleber Z.; Napolitano, Hamilton B.; Vencato, Ivo; Lariucci, Carlito; Castro, Miriam. R. C. de; Camargo, Ademir J.

    2013-01-01

    The present work describes the antibacterial and antifungal activities of several chalcones obtained by a straight Claisen-Schmidt aldol condensation determined by the minimal inhibitory concentration against different microorganisms (Gram-positive and Gram-negative bacteria and fungi). Solid state crystal structures of seven chalcones were determined by X-ray diffraction (XRD) analysis. Chemometric studies were carried out in order to identify a potential structure-activity relationship. ...

  6. Evaluation of an ethnopharmacologically selected Bhutanese medicinal plants for their major classes of phytochemicals and biological activities.

    Science.gov (United States)

    Wangchuk, Phurpa; Keller, Paul A; Pyne, Stephen G; Taweechotipatr, Malai; Tonsomboon, Aunchalee; Rattanajak, Roonglawan; Kamchonwongpaisan, Sumalee

    2011-09-01

    As many as 229 medicinal plants have been currently used in the Bhutanese Traditional Medicine (BTM) as a chief ingredient of polyherbal formulations and these plants have been individually indicated for treating various types of infections including malaria, tumor, and microbial. We have focused our study only on seven species of these plants. We aim to evaluate the antiplasmodial, antimicrobial, anti-Trypanosoma brucei rhodesiense and cytotoxicity activities of the seven medicinal plants of Bhutan selected using an ethno-directed bio-rational approach. This study creates a scientific basis for their use in the BTM and gives foundation for further phytochemical and biological evaluations which can result in the discovery of new drug lead compounds. A three stage process was conducted which consisted of: (1) an assessment of a pharmacopoeia and a formulary book of the BTM for their mode of plant uses; (2) selecting 25 anti-infective medicinal plants based on the five established criteria, collecting them, and screening for their major classes of phytochemicals using appropriate test protocols; and (3) finally analyzing the crude extracts of the seven medicinal plants, using the standard test protocols, for their antiplasmodial, antimicrobial, anti-Trypanosoma brucei rhodesiense and cytotoxicity activities as directed by the ethnopharmacological uses of each plant. Out of 25 medicinal plants screened for their major classes of phytochemicals, the majority contained tannins, alkaloids and flavonoids. Out of the seven plant species investigated for their biological activities, all seven of them exhibited mild antimicrobial properties, five plants gave significant in vitro antiplasmodial activities, two plants gave moderate anti-Trypanosoma brucei rhodesiense activity, and one plant showed mild cytotoxicity. Meconopsis simplicifolia showed the highest antiplasmodial activity with IC(50) values of 0.40 μg/ml against TM4/8.2 strain (a wild type chloroquine and

  7. Evaluation of Zanthoxylum armatum Roxb for in vitro biological activities

    Directory of Open Access Journals (Sweden)

    Fiaz Alam

    2017-10-01

    Full Text Available Zanthoxylum armatum fruits are used traditionally as a spice in various food preparations. The aim of this study was analysis of antimicrobial, cytotoxic, phytotoxic, insecticidal, and anti-leishmanial activity. The crude extract showed 86 ± 10% antifungal activity (Agar tube dilution method against Trichophyton longifusis while n-hexane, chloroform, and aqueous-methanol fractions inhibited this pathogen by 90 ± 7, 85 ± 10 and 70 ± 9% respectively. The n-hexane and aqueous-methanol fraction also, respectively, showed 40 ± 10 and 87 ± 9% inhibition of Microsporum canis. Chloroform fraction also displayed antifungal activity against Aspergillus flavus (60 ± 10% and aqueous-methanol fraction against F. solani (40 ± 8%. The crude ethanolic extract and its chloroform and aqueous-methanol fraction exhibited significant toxicity (Brine shrimps lethality assay against brine shrimps having LC50 value of 6.66 ± 1.1, 21.4 ± 3.3 and 29.6 ± 3.9 μg/ml, respectively. The crude ethanolic extract and its n-hexane soluble portion exhibited good anti-leishmanial activity (well serial dilution method each having IC50 values of 50 ± 5 μg/ml. The crude extract and various fractions possessed excellent herbicidal activity (Lemna minor assay, and caused more than 90% inhibition of the plant growth at 1000 μg/mL. The ethanolic extract, n-hexane and chloroform soluble portions caused 90% mortality in insecticidal activity (direct contact method of Rhyzopertha dominica. The ethanolic extract and its n-hexane soluble portion, respectively, caused 80 and 90% mortality of Callosobruchus analis. The present study showed that the tested fruit extracts of Z. armatum exhibited strong antifungal, cytotoxic, phytotoxic, insecticidal, and anti-leishmanial effects.

  8. Synthesis and biological evaluation of curcumin derivatives containing NSAIDs for their anti-inflammatory activity.

    Science.gov (United States)

    Liu, Wenfeng; Li, Yonlian; Yue, Yuan; Zhang, Kun; Chen, Qian; Wang, Huaqian; Lu, Yujing; Huang, Mou-Tuan; Zheng, Xi; Du, Zhiyun

    2015-08-01

    Oral administration of nonsteroidal anti-inflammatory drugs (NSAIDs) was frequently associated with serious adverse effects. Inspired by curcumin-a naturally traditional Chinese medicine, a series of curcumin derivatives containing NSAIDs, used for transdermal application, were synthesized and screened for their anti-inflammatory activities in vitro and in vivo. Compared with curcumin and parent NSAID (salicylic acid and salsalate), topical application of A11 and B13 onto mouse ear edema, prior to TPA treatment markedly suppressed the expression of IL-1β, IL-6 and TNF-α, respectively. Mechanistically, A11 and B13 blocked the phosphorylation of IκBα and suppressed the activation of p65 and IκBα. It was found that A11 and B13 may be potent anti-inflammatory agents for the treatment of inflammatory diseases. Copyright © 2015 Elsevier Ltd. All rights reserved.

  9. Novel topoisomerase I inhibitors. Syntheses and biological evaluation of phosphorus substituted quinoline derivates with antiproliferative activity.

    Science.gov (United States)

    Alonso, Concepción; Fuertes, María; Martín-Encinas, Endika; Selas, Asier; Rubiales, Gloria; Tesauro, Cinzia; Knudssen, Birgitta K; Palacios, Francisco

    2018-02-22

    This work describes the synthesis of 1,2,3,4-tetrahydroquinolinylphosphine oxides, phosphanes and phosphine sulfides as well as that of quinolinylphosphine oxides and phosphine sulfides, which were synthesized in good to high overall yield. The synthetic route involves a multicomponent reaction of (2-phosphine-oxide)-, 2-phosphine- or (2-phosphine-sulfide)-aniline, aldehydes and olefins and allows the selective generation of two stereogenic centres in a short, efficient and reliable synthesis. The selective dehydrogenation of 1,2,3,4-tetrahydroquinolinylphosphine oxides and phosphine sulfides leads to the formation of corresponding phosphorus substituted quinolines. Some of the products which were prepared showed excellent activity as topoisomerase I (Top1) inhibitors. In addition, prolonged effect of the most potent compounds is maintained with the same intensity even after 3 min of the beginning of the enzymatic reaction. The cytotoxic effect on cell lines derived from human lung adenocarcinoma (A549), human ovarian carcinoma (SKOV03) and human embryonic kidney (HEK293) was also screened. 1,2,3,4-Tetrahydroquinolinylphosphine oxide 6g with an IC 50 value of 0.25 ± 0.03 μM showed excellent activity against the A549 cell line in vitro, while 1,2,3,4-tetrahydroquinolinylphosphane 9c with an IC 50 value of 0.08 ± 0.01 μM and 1,2,3,4-tetrahydroquinolinylphosphine sulfide derivative 10f with an IC 50 value of 0.03 ± 0.04 μM are more active against the A549 cell line. Moreover, selectivity towards cancer cell (A549) over non-malignant cells (MRC5) has been observed. According to their structure, they may be excellent antiproliferative candidates. Copyright © 2018 Elsevier Masson SAS. All rights reserved.

  10. Evaluation of the Biological Activity of Naturally Occurring 5,8-Dihydroxycoumarin

    OpenAIRE

    Slapšytė, Gražina; Dedonytė, Veronika; Lazutka, Juozas; Mierauskienė, Jūratė; Morkūnas, Vaidotas; Kazernavičiūtė, Rita; Pukalskas, Audrius; Venskutonis, Petras

    2013-01-01

    5,8-Dihydroxycoumarin (5,8-DHC) was isolated from aerial parts of sweet grass (Hierochloë odorata L.) and screened for antioxidant and genotoxic activities. A clear linear dependency of radical scavenging capacity in DPPH• and ABTS•+ assays was determined. 5,8-DHC was very efficient in retarding rapeseed oil oxidation (Oxipress test). TPC (total phenols content) and FRAP (the ability to reduce ferric ion to ferrous ion) assays revealed a somewhat lower antioxidant capacity of 5,8-DHC as compa...

  11. Synthesis and biological evaluation of indolyl-pyridinyl-propenones having either methuosis or microtubule disruption activity.

    Science.gov (United States)

    Trabbic, Christopher J; Overmeyer, Jean H; Alexander, Evan M; Crissman, Emily J; Kvale, Heather M; Smith, Marcie A; Erhardt, Paul W; Maltese, William A

    2015-03-12

    Methuosis is a form of nonapoptotic cell death characterized by an accumulation of macropinosome-derived vacuoles with eventual loss of membrane integrity. Small molecules inducing methuosis could offer significant advantages compared to more traditional anticancer drug therapies that typically rely on apoptosis. Herein we further define the effects of chemical substitutions at the 2- and 5-indolyl positions on our lead compound 3-(5-methoxy-2-methyl-1H-indol-3-yl)-1-(4-pyridinyl)-2-propene-1-one (MOMIPP). We have identified a number of compounds that induce methuosis at similar potencies, including an interesting analogue having a hydroxypropyl substituent at the 2-position. In addition, we have discovered that certain substitutions on the 2-indolyl position redirect the mode of cytotoxicity from methuosis to microtubule disruption. This switch in activity is associated with an increase in potency as large as 2 orders of magnitude. These compounds appear to represent a new class of potent microtubule-active anticancer agents.

  12. Seeing by Touch: Evaluation of a Soft Biologically-Inspired Artificial Fingertip in Real-Time Active Touch

    Directory of Open Access Journals (Sweden)

    Tareq Assaf

    2014-02-01

    Full Text Available Effective tactile sensing for artificial platforms remains an open issue in robotics. This study investigates the performance of a soft biologically-inspired artificial fingertip in active exploration tasks. The fingertip sensor replicates the mechanisms within human skin and offers a robust solution that can be used both for tactile sensing and gripping/manipulating objects. The softness of the optical sensor’s contact surface also allows safer interactions with objects. High-level tactile features such as edges are extrapolated from the sensor’s output and the information is used to generate a tactile image. The work presented in this paper aims to investigate and evaluate this artificial fingertip for 2D shape reconstruction. The sensor was mounted on a robot arm to allow autonomous exploration of different objects. The sensor and a number of human participants were then tested for their abilities to track the raised perimeters of different planar objects and compared. By observing the technique and accuracy of the human subjects, simple but effective parameters were determined in order to evaluate the artificial system’s performance. The results prove the capability of the sensor in such active exploration tasks, with a comparable performance to the human subjects despite it using tactile data alone whereas the human participants were also able to use proprioceptive cues.

  13. Biogenic silver nanoparticles based on trichoderma harzianum: synthesis, characterization, toxicity evaluation and biological activity

    Science.gov (United States)

    Guilger, Mariana; Pasquoto-Stigliani, Tatiane; Bilesky-Jose, Natália; Grillo, Renato; Abhilash, P. C.; Fraceto, Leonardo Fernandes; Lima, Renata De

    2017-03-01

    White mold is an agricultural disease caused by the fungus Sclerotinia sclerotiorum, which affects important crops. There are different ways of controlling this organism, but none provides inhibition of its resistance structures (sclerotia). Nanotechnology offers promising applications in agricultural area. Here, silver nanoparticles were biogenically synthesized using the fungus Trichoderma harzianum and characterized. Cytotoxicity and genotoxicity were evaluated, and the nanoparticles were initially tested against white mold sclerotia. Their effects on soybean were also investigated with no effects observed. The nanoparticles showed potential against S. sclerotiorum, inhibiting sclerotia germination and mycelial growth. Nanoparticle characterization data indicated spherical morphology, satisfactory polydispersity and size distribution. Cytotoxicity and genotoxicity assays showed that the nanoparticles caused both the effects, although, the most toxic concentrations were above those applied for white mold control. Given the potential of the nanoparticles against S. sclerotiorum, we conclude that this study presents a first step for a new alternative in white mold control.

  14. Biological evaluation of RVNRL

    International Nuclear Information System (INIS)

    Geertsma, R.E.; Orzechowski, T.J.H.; Jonker, M.; Dorpema, J.W.; Van Asten, J.A.A.M.

    1996-01-01

    Cytotoxicity testing (cell growth inhibition, LDH-assay) has shown that RVNRL materials are considerably less cytotoxic than sulphur-vulcanised materials. Also the effect of applying different leaching times during the production process was investigated and gave interesting results. Protein testing (BCA - comparable to a Lowry assay ) has shown that some, but not all proteins are destroyed during irradiation. For the total protein content of the materials as determined in this way, the effect of leaching proved to be very important. This was also checked by; SDS-PAGE assays: After irradiation a smear is observed with SDS-PAGE; when the irradiated material has been leached, most of the smear has disappeared. An important protein (14 kD) is still present and seems hardly to be affected. The materials have also been evaluated clinically, using well characterised patient sera (Western blotting) in order to determine whether the remaining proteins are allergenic

  15. New Human Monoamine Oxidase A Inhibitors with Potential Anti- Depressant Activity: Design, Synthesis, Biological Screening and Evaluation of Pharmacological Activity.

    Science.gov (United States)

    Evranos-Aksoz, Begum; Ucar, Gulberk; Tas, Sadik Taskin; Aksoz, Erkan; Yelekci, Kemal; Erikci, Acelya; Sara, Yildirim; Iskit, Alper Bektas

    2017-01-01

    Depression is a momentous disease that can greatly reduce the quality of life and cause death. In depression, neurotransmitter levels such as serotonine, dopamine and noradrenaline are impaired. Monoamine oxidases (MAO) are responsible for oxidative catalysis of these monoamine neurotransmitters. Because of this relation, MAO-A inhibitors show antidepressant activity by regulating neurotransmitter levels. This study was carried out to investigate the design, synthesis and activity of new antidepressant compounds in pyrazoline and hydrazone structure. Chalcones and hydrazides were heated under reflux to give new pyrazoline and hydrazone derivatives. Docking simulations were performed using AutoDock4.2. hMAO activities were determined by a fluorimetric method. To determine cell viability, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay was used. Behavioral activities of the three compounds were determined by using Forced Swim Test, Step-Through Passive Avoidance Test, Elevated Plus Maze and Open Field Arena Tests. According to in vitro tests, all of the synthesized compounds were found more potent than moclobemide and six of the synthesized compounds were found more selective than moclobemide. Three of the synthesized compounds were investigated for their behavioral activities comparing with moclobemide after 7 days of i.p. treatment at 30 mg/kg. One of the three compounds elicited significant antidepressant properties. All of the synthesized compounds were found potent hMAO-A inhibitors in in vitro screening tests. Only one of the in vivo tested three compounds, (3-(2-hydroxy-5-methylphenyl)-5- p-tolyl-4,5-dihydropyrazol-1-yl)(pyridin-4-yl) methanone indicated significant antidepressant activity. This article opens a window for further development of new pyrazoline and hydrazone derivatives as antidepressant agents. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

  16. Design, synthesis and biological activity evaluation of novel 4-subtituted 2-naphthamide derivatives as AcrB inhibitors.

    Science.gov (United States)

    Wang, Yinhu; Mowla, Rumana; Ji, Shengli; Guo, Liwei; De Barros Lopes, Miguel A; Jin, Chaobin; Song, Di; Ma, Shutao; Venter, Henrietta

    2018-01-01

    A novel series of 4-substituted 2-naphthamide derivatives were designed, synthesized and evaluated for their biological activity. In particular, the ability of the compounds to potentiate the action of antibiotics, to inhibit Nile Red efflux and to target AcrB specifically was investigated. The results indicated that most of the 4-substituted 2-naphthamide derivatives were able to synergize with the antibiotics tested, and inhibit Nile Red efflux by AcrB in the resistant phenotype. Subsequent exclusion of compounds with off target effects such as outer- or inner membrane permeabilization identified compounds 7c, 7g, 12c, 12i and 13g as efflux pump inhibitors (EPIs). Particularly, compounds 7c, 7g and 12i were found to be the most potent EPIs, which synergized with the two substrates tested at lower concentrations than that of parent A3, demonstrating an improvement in potency as compared to A3. Additionally, when the outer membrane of E. coli was permeabilized, compound 12c displayed a huge increase in efficacy and was able to synergize with erythromycin at a concentration that was 16 times lower than that of the parent A3. Hence we were able to design and synthesize compounds that displayed significant increase in efficacy as EPIs against AcrB. Copyright © 2017 Elsevier Masson SAS. All rights reserved.

  17. Brassinosteroids: synthesis and biological activities

    Czech Academy of Sciences Publication Activity Database

    Oklešťková, Jana; Rárová, Lucie; Kvasnica, Miroslav; Strnad, Miroslav

    2015-01-01

    Roč. 14, č. 6 (2015), s. 1053-1072 ISSN 1568-7767 R&D Projects: GA MŠk(CZ) LO1204 Institutional support: RVO:61389030 Keywords : Brassinosteroids * Chemical synthesis * Plant biological activity Subject RIV: EB - Genetics ; Molecular Biology Impact factor: 2.686, year: 2015

  18. Raman spectroscopy for the evaluation of the effects of different concentrations of Copper on the chemical composition and biological activity of basil essential oil

    Science.gov (United States)

    Nawaz, Haq; Hanif, Muhammad Asif; Ayub, Muhammad Adnan; Ishtiaq, Faiqa; Kanwal, Nazish; Rashid, Nosheen; Saleem, Muhammad; Ahmad, Mushtaq

    2017-10-01

    The present study is performed to evaluate the effect of different concentrations of Cu as fertilizer on the chemical composition of basil essential oil and its biological activity including antioxidant and antifungal activities by employing Raman spectroscopy. Moreover, the effect of Cu is also determined on the vegetative growth and essential oil yield. Both, antifungal and antioxidant activities were found to be maximum with essential oils obtained at 0.04 mg/l concentration of Cu fertilizer. The results of the GC-MS and Raman spectroscopy have revealed that the linalool and estragole are found to be as a major chemical compound in basil essential oil. The Raman spectral changes associated with these biological components lead to the conclusion that estragole seems to have dominating effect in the biological activities of the basil essential oil as compared to linalool although the latter is observed in greater concentration.

  19. First Evaluation of the Biologically Active Substances and Antioxidant Potential of Regrowth Velvet Antler by means of Multiple Biochemical Assays

    Directory of Open Access Journals (Sweden)

    Yujiao Tang

    2015-01-01

    Full Text Available We investigated the biologically active substances contained in RVA (regrowth velvet antler by comparing the composition of biologically active substances and antioxidant potential of different antler segments. RVA was subjected to extraction using DW (distilled water. RVA was divided into 3 segments: T-RVA (top RVA, M-RVA (middle RVA, and B-RVA (base RVA. The T-RVA section possessed the greatest amounts of uronic acid (36.251 mg/g, sulfated GAGs (sulfated glycosaminoglycans (555.76 mg/g, sialic acid (111.276 mg/g, uridine (0.957 mg/g, uracil (1.084 mg/g, and hypoxanthine (1.2631 mg/g. In addition, the T-RVA section possessed the strongest antioxidant capacity as determined by DPPH, H2O2 (hydrogen peroxide, hydroxyl, and ABTS (2,2′-azinobis-3-ethylbenzthiazoline-6-sulphonate radical scavenging activity as well as FRAP (ferric reducing antioxidant power and ORAC (oxygen radical absorbance capacity. The values of those were 53.44, 23.09, 34.12, 60.31, and 35.81 TE/μM at 1 mg/mL and 113.57 TE/μM at 20 μg/mL. These results indicate that the T-RVA section possesses the greatest amount of biologically active substances and highest antioxidant potential. This is the first report on the biologically active substances and antioxidant potential of RVA.

  20. Solid‐Phase Synthesis and Biological Evaluation of N‐Dipeptido L‐Homoserine Lactones as Quorum Sensing Activators

    DEFF Research Database (Denmark)

    Hansen, Mette Reimert; Le Quement, Sebastian Thordal; Jakobsen, Tim Holm

    2014-01-01

    ‐homoserine lactones. With the goal of identifying non‐native compounds capable of modulating bacterial QS, a virtual library of N‐dipeptido L‐homoserine lactones was screened in silico with two different crystal structures of LasR. The 30 most promising hits were synthesized on HMBA‐functionalized PEGA resin...... and released through an efficient acid‐mediated cyclative release mechanism. Subsequent screening for modulation of QS in Pseudomonas aeruginosa and E. coli identified six moderately strong activators. A follow‐up library designed from the preliminary derived structure–activity relationships was synthesized...... and evaluated for their ability to activate the QS system in this bacterium. This resulted in the identification of another six QS activators (two with low micromolar activity) thus illuminating structural features required for QS modulation....

  1. Synthesis and biological evaluation of 3,4-diaryloxazolones: A new class of orally active cyclooxygenase-2 inhibitors.

    Science.gov (United States)

    Puig, C; Crespo, M I; Godessart, N; Feixas, J; Ibarzo, J; Jiménez, J M; Soca, L; Cardelús, I; Heredia, A; Miralpeix, M; Puig, J; Beleta, J; Huerta, J M; López, M; Segarra, V; Ryder, H; Palacios, J M

    2000-01-27

    A series of 3,4-diaryloxazolones were prepared and evaluated for their ability to inhibit cyclooxygenase-2 (COX-2). Extensive structure-activity relationship work was carried out within this series, and a number of potent and selective COX-2 inhibitors were identified. The replacement of the methyl sulfone group on the 4-phenyl ring by a sulfonamide moiety resulted in compounds with superior in vivo antiinflammatory properties. In the sulfonamide series, the introduction of a methyl group at the 5-position of the oxazolone ring gave rise to very COX-2-selective compounds but with decreased in vivo activity. Selected 3,4-diaryloxazolones exhibited excellent activities in experimental models of arthritis and hyperalgesia. The in vivo activity of these compounds was confirmed with the evaluation of their antipyretic effectiveness and their ability to inhibit migration of proinflammatory cells. As expected from their COX-2 selectivity, most of the active compounds lacked gastrointestinal toxicity in vivo in rats after a 4-day treatment of 100 mg/kg/day. Within this novel series, sulfonamides 9-11 have been selected for further preclinical evaluation.

  2. Evaluation of antioxidant properties, total phenolic content, and biological activities of new tomato hybrids of industrial interest.

    Science.gov (United States)

    Tommonaro, Giuseppina; de Prisco, Rocco; Abbamondi, Gennaro Roberto; Marzocco, Stefania; Saturnino, Carmela; Poli, Annarita; Nicolaus, Barbara

    2012-05-01

    The objective of the present work was to establish the antioxidative ability linked to lipophilic, hydrophilic, and polyphenolic fractions of new tomato hybrids of industrial interest, grown in an outdoor field, named "Medugno", situated in the Agro-Nocerino Sarnese area (Province of Salerno, Campania Region, Italy). Antioxidant activities of lipophilic, hydrophilic, and polyphenolic extracts of tomato hybrids determined by the 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid), N,N-dimethyl-p-phenylenediamine dihydrochloride, and 2,2-diphenyl-1-picrylhydrazyl methods, respectively, showed the best results in hybrids obtained between the pure San Marzano and Black Tomato lines. Antioxidant activity tests, performed also on the San Marzano × Black Tomato hybrid (pulped tomatoes), indicated that the industrial transformation process of this new tomato hybrid did not cause a significant loss of antioxidant activity. The in vitro production of nitrite by lipopolysaccharide-stimulated macrophages J774A.1 performed on lipophilic extracts showed that only two hybrids (San Marzano × Black Tomato and Marmande × Black Tomato) inhibited, in a concentration-related manner, nitric oxide release. Results suggested that genotypic factors could determine the nutritional quality of tomato because of the content of biologically active compounds and their biosynthesis. Moreover, the new tomato hybrid achieved could have a potential for the agri-food industry because of its nutritional quality and because it lends itself in processes of industrial transformation.

  3. In Silico Screening, Structure-Activity Relationship, and Biologic Evaluation of Selective Pteridine Reductase Inhibitors Targeting Visceral Leishmaniasis▿ †

    Science.gov (United States)

    Kaur, Jaspreet; Kumar, Pranav; Tyagi, Sargam; Pathak, Richa; Batra, Sanjay; Singh, Prashant; Singh, Neeloo

    2011-01-01

    In this study we utilized the concept of rational drug design to identify novel compounds with optimal selectivity, efficacy and safety, which would bind to the target enzyme pteridine reductase 1 (PTR1) in Leishmania parasites. Twelve compounds afforded from Baylis-Hillman chemistry were docked by using the QUANTUM program into the active site of Leishmania donovani PTR1 homology model. The biological activity for these compounds was estimated in green fluorescent protein-transfected L. donovani promastigotes, and the most potential analogue was further investigated in intracellular amastigotes. Structure-activity relationship based on homology model drawn on our recombinant enzyme was substantiated by recombinant enzyme inhibition assay and growth of the cell culture. Flow cytometry results indicated that 7-(4-chlorobenzyl)-3-methyl-4-(4-trifluoromethyl-phenyl)-3,4,6,7,8,9-hexahydro-pyrimido[1,2-a]pyrimidin-2-one (compound 7) was 10 times more active on L. donovani amastigotes (50% inhibitory concentration [IC50] = 3 μM) than on promastigotes (IC50 = 29 μM). Compound 7 exhibited a Ki value of 0.72 μM in a recombinant enzyme inhibition assay. We discovered that novel pyrimido[1,2-a]pyrimidin-2-one systems generated from the allyl amines afforded from the Baylis-Hillman acetates could have potential as a valuable pharmacological tool against the neglected disease visceral leishmaniasis. PMID:21115787

  4. Risk Evaluation for Identification and Intervention in Dual Use Research of Concern (DURC) for International Biological R&D Activity

    Energy Technology Data Exchange (ETDEWEB)

    Jones, Katherine A. [Sandia National Lab. (SNL-NM), Albuquerque, NM (United States); DeMenno, Mercy [Sandia National Lab. (SNL-NM), Albuquerque, NM (United States); Hoffman, Matthew John [Sandia National Lab. (SNL-NM), Albuquerque, NM (United States); Caskey, Susan A. [Sandia National Lab. (SNL-NM), Albuquerque, NM (United States); Astuto-Gribble, Lisa M. [Sandia National Lab. (SNL-NM), Albuquerque, NM (United States); Gearhart, Jared Lee [Sandia National Lab. (SNL-NM), Albuquerque, NM (United States); Arguello, Bryan [Sandia National Lab. (SNL-NM), Albuquerque, NM (United States); Chavez, Lozanne M. [Sandia National Lab. (SNL-NM), Albuquerque, NM (United States); Pierson, Adam J. [Sandia National Lab. (SNL-NM), Albuquerque, NM (United States); Lopez, Elizabeth [Sandia National Lab. (SNL-NM), Albuquerque, NM (United States); Nozick, Linda Karen [Sandia National Lab. (SNL-NM), Albuquerque, NM (United States); Davis, Chad E. [Sandia National Lab. (SNL-NM), Albuquerque, NM (United States)

    2016-09-01

    This report summarizes the work performed as part of a Laboratory Directed Research and Development project focused on evaluating and mitigating risk associated with biological dual use research of concern. The academic and scientific community has identified the funding stage as the appropriate place to intervene and mitigate risk, so the framework developed here uses a portfolio-level approach and balances biosafety and biosecurity risks, anticipated project benefits, and available mitigations to identify the best available investment strategies subject to cost constraints. The modeling toolkit was designed for decision analysis for dual use research of concern, but is flexible enough to support a wide variety of portfolio-level funding decisions where risk/benefit tradeoffs are involved. Two mathematical optimization models with two solution methods are included to accommodate stakeholders with varying levels of certainty about priorities between metrics. An example case study is presented.

  5. Biological activities of substituted trichostatic acid derivatives

    Indian Academy of Sciences (India)

    New substituted trichostatic acid derivatives have been synthesized and evaluated for their biological activities towards the H661 non-small lung cancer cell line. These syntheses were achieved by alkylation of propiophenones to introduce the side chain with a terminal precursor of hydroxamic acid and aminobenzamide ...

  6. The green synthesis, characterization, and evaluation of the biological activities of silver nanoparticles synthesized from Leptadenia reticulata leaf extract

    Science.gov (United States)

    Kumara Swamy, M.; Sudipta, K. M.; Jayanta, K.; Balasubramanya, S.

    2015-01-01

    Biosynthesis of silver nanoparticles (Ag Nps) was carried out using methanol leaves extract of L. reticulata. Ag Nps were characterized based on the observations of UV-visible spectroscopy, transmission electron microscopy, and X-ray diffraction (XRD) analysis. These Ag Nps were tested for antimicrobial activity by agar well diffusion method against different pathogenic microorganisms and antioxidant activity was performed using DPPH assay. Further, the in vitro cytotoxic effects of Ag Nps were screened against HCT15 cancer cell line and viability of tumor cells was confirmed using MTT ((3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide, a yellow tetrazole)) assay. The nuclear condensation was studied using the propidium iodide-staining method. The color change from green to dark brown and the absorbance peak at about 420 nm indicated the formation of nanoparticles. XRD pattern showed characteristic peaks indexed to the crystalline planes (111), (200) and (220) of face-centered cubic silver. The nanoparticles were of spherical shape with varying sizes ranging from 50 to 70 nm. Biosynthesized Ag Nps showed potent antibacterial activity and effective radical scavenging activity. MTT assay revealed a dose-dependent decrease in cell viability. Microscopic observations showed distinct cellular morphological changes indicating unhealthy cells, whereas the control appeared normal. Increase in the number of propidium iodide positive cells were observed in maximum concentration. Methanolic leaf extract of L. reticulata acts as an excellent capping agent for the formation of silver nanoparticles and demonstrates immense biological activities. Hence, these Ag NPs can be used as antibacterial, antioxidant as well as cytotoxic agent in treating many medical complications.

  7. Biological activities of plant extracts from Ficus elastica and Selaginella vogelli: An antimalarial, antitrypanosomal and cytotoxity evaluation

    Directory of Open Access Journals (Sweden)

    Jean Emmanuel Mbosso Teinkela

    2018-01-01

    Full Text Available The cytotoxic, antiplasmodial, and antitrypanosomal activities of two medicinal plants traditionally used in Cameroon were evaluated. Wood of Ficus elastica Roxb. ex Hornem. aerial roots (Moraceae and Selaginella vogelii Spring (Selaginellaceae leaves were collected from two different sites in Cameroon. In vitro cell-growth inhibition activities were assessed on methanol extract of plant materials against Plasmodium falciparum strain 3D7 and Trypanosoma brucei brucei, as well as against HeLa human cervical carcinoma cells. Criteria for activity were an IC50 value < 10 μg/mL. The extract of S. vogelii did not significantly reduce the viability of P. falciparum at a concentration of 25 μg/mL but dramatically affected the trypanosome growth with an IC50 of 2.4 μg/mL. In contrast, at the same concentration, the extract of F. elastica exhibited plasmodiacidal activity (IC50 value of 9.5 μg/mL and trypanocidal (IC50 value of 0.9 μg/mL activity. Both extracts presented low cytotoxic effects on HeLa cancer cell line. These results indicate that the selected medicinal plants could be further investigated for identifying compounds that may be responsible for the observed activities and that may represent new leads in parasitical drug discovery.

  8. Evaluation of the insecticidal activity of the extracts from Piper grande Vahl (Piperaceae) using the biological model Drosophila melanogaster

    International Nuclear Information System (INIS)

    Granados N, Hillmer; Saez V, Jairo; Robles, Carolina; Vasquez, Luis F; Moreno, Maria E; Acevedo, Jose M; Pelaez, Carlos A; Callejas, Ricardo

    2002-01-01

    In this study, using the life cycle interruption test with the Drosophila melanogaster model, under (in-vitro conditions), the n-Hexane (roots and stems) and the EtOAc (roots and leaves) extracts were evaluated as insecticides and the results were promising. The larvae instars showed a significant activity reflected in the reduction of pupae population with respect to the control. The step from Pupae to adult did no show inhibition because in all cases the average of the relation pupae adult is found in values very near 1. The n-Hexane and the EtOAc extracts from roots were the most active with LC50 of 698.2 ppm and 1210.7 ppm. The n-Hexane (stems) and EtOAc (leaves) extracts showed a moderate activity with LC50 of 1654.1 ppm and 2376.0 ppm

  9. Imidazole: Having Versatile Biological Activities

    Directory of Open Access Journals (Sweden)

    Amita Verma

    2013-01-01

    Full Text Available Imidazoles have occupied a unique position in heterocyclic chemistry, and its derivatives have attracted considerable interests in recent years for their versatile properties in chemistry and pharmacology. Imidazole is nitrogen-containing heterocyclic ring which possesses biological and pharmaceutical importance. Thus, imidazole compounds have been an interesting source for researchers for more than a century. The imidazole ring is a constituent of several important natural products, including purine, histamine, histidine, and nucleic acid. Being a polar and ionisable aromatic compound, it improves pharmacokinetic characteristics of lead molecules and thus is used as a remedy to optimize solubility and bioavailability parameters of proposed poorly soluble lead molecules. There are several methods used for the synthesis of imidazole-containing compounds, and also their various structure reactions offer enormous scope in the field of medicinal chemistry. The imidazole derivatives possess extensive spectrum of biological activities such as antibacterial, anticancer, antitubercular, antifungal, analgesic, and anti-HIV activities. This paper aims to review the biological activities of imidazole during the past years.

  10. Phytochemical Profile and Evaluation of the Biological Activities of Essential Oils Derived from the Greek Aromatic Plant Species Ocimum basilicum, Mentha spicata, Pimpinella anisum and Fortunella margarita.

    Science.gov (United States)

    Fitsiou, Eleni; Mitropoulou, Gregoria; Spyridopoulou, Katerina; Tiptiri-Kourpeti, Angeliki; Vamvakias, Manolis; Bardouki, Haido; Panayiotidis, Mihalis Ι; Galanis, Alex; Kourkoutas, Yiannis; Chlichlia, Katerina; Pappa, Aglaia

    2016-08-16

    Natural products, known for their medicinal properties since antiquity, are continuously being studied for their biological properties. In the present study, we analyzed the composition of the volatile preparations of essential oils of the Greek plants Ocimum basilicum (sweet basil), Mentha spicata (spearmint), Pimpinella anisum (anise) and Fortunella margarita (kumquat). GC/MS analyses revealed that the major components in the essential oil fractions, were carvone (85.4%) in spearmint, methyl chavicol (74.9%) in sweet basil, trans-anethole (88.1%) in anise, and limonene (93.8%) in kumquat. We further explored their biological potential by studying their antimicrobial, antioxidant and antiproliferative activities. Only the essential oils from spearmint and sweet basil demonstrated cytotoxicity against common foodborne bacteria, while all preparations were active against the fungi Saccharomyces cerevisiae and Aspergillus niger. Antioxidant evaluation by DPPH and ABTS radical scavenging activity assays revealed a variable degree of antioxidant potency. Finally, their antiproliferative potential was tested against a panel of human cancer cell lines and evaluated by using the sulforhodamine B (SRB) assay. All essential oil preparations exhibited a variable degree of antiproliferative activity, depending on the cancer model used, with the most potent one being sweet basil against an in vitro model of human colon carcinoma.

  11. Phytochemical Profile and Evaluation of the Biological Activities of Essential Oils Derived from the Greek Aromatic Plant Species Ocimum basilicum, Mentha spicata, Pimpinella anisum and Fortunella margarita

    Directory of Open Access Journals (Sweden)

    Eleni Fitsiou

    2016-08-01

    Full Text Available Natural products, known for their medicinal properties since antiquity, are continuously being studied for their biological properties. In the present study, we analyzed the composition of the volatile preparations of essential oils of the Greek plants Ocimum basilicum (sweet basil, Mentha spicata (spearmint, Pimpinella anisum (anise and Fortunella margarita (kumquat. GC/MS analyses revealed that the major components in the essential oil fractions, were carvone (85.4% in spearmint, methyl chavicol (74.9% in sweet basil, trans-anethole (88.1% in anise, and limonene (93.8% in kumquat. We further explored their biological potential by studying their antimicrobial, antioxidant and antiproliferative activities. Only the essential oils from spearmint and sweet basil demonstrated cytotoxicity against common foodborne bacteria, while all preparations were active against the fungi Saccharomyces cerevisiae and Aspergillus niger. Antioxidant evaluation by DPPH and ABTS radical scavenging activity assays revealed a variable degree of antioxidant potency. Finally, their antiproliferative potential was tested against a panel of human cancer cell lines and evaluated by using the sulforhodamine B (SRB assay. All essential oil preparations exhibited a variable degree of antiproliferative activity, depending on the cancer model used, with the most potent one being sweet basil against an in vitro model of human colon carcinoma.

  12. Oxidative Stress Regulation on Endothelial Cells by Hydrophilic Astaxanthin Complex: Chemical, Biological, and Molecular Antioxidant Activity Evaluation

    Directory of Open Access Journals (Sweden)

    M. Zuluaga

    2017-01-01

    Full Text Available An imbalance in the reactive oxygen species (ROS homeostasis is involved in the pathogenesis of oxidative stress-related diseases. Astaxanthin, a xanthophyll carotenoid with high antioxidant capacities, has been shown to prevent the first stages of oxidative stress. Here, we evaluate the antioxidant capacities of astaxanthin included within hydroxypropyl-beta-cyclodextrin (CD-A to directly and indirectly reduce the induced ROS production. First, chemical methods were used to corroborate the preservation of astaxanthin antioxidant abilities after inclusion. Next, antioxidant scavenging properties of CD-A to inhibit the cellular and mitochondrial ROS by reducing the disturbance in the redox state of the cell and the infiltration of lipid peroxidation radicals were evaluated. Finally, the activation of endogenous antioxidant PTEN/AKT, Nrf2/HO-1, and NQOI gene and protein expression supported the protective effect of CD-A complex on human endothelial cells under stress conditions. Moreover, a nontoxic effect on HUVEC was registered after CD-A complex supplementation. The results reported here illustrate the need to continue exploring the interesting properties of this hydrophilic antioxidant complex to assist endogenous systems to counteract the ROS impact on the induction of cellular oxidative stress state.

  13. Novel 2-arylazoimidazole derivatives as inhibitors of Trypanosoma cruzi proliferation: Synthesis and evaluation of their biological activity.

    Science.gov (United States)

    Salerno, Alejandra; Celentano, Ana M; López, Julieta; Lara, Virginia; Gaozza, Carlos; Balcazar, Darío E; Carrillo, Carolina; Frank, Fernanda M; Blanco, María M

    2017-01-05

    In this work, the synthesis of a series of 2-arylazoimidazole derivatives 6-20 has been achieved through the reaction of imidazole with aryldiazonium salts, followed by ultrasound-assisted alkylation. This approach has important advantages including higher yield, shorter reaction times and milder reaction conditions. The structures of the compounds obtained were determined by MS, IR; and 1 H and 13 C NMR. The anti-Trypanosoma cruzi activity of the 15 compounds obtained was evaluated. Two compounds with piperidino substituents in the carboxamide moiety proved to be effective inhibitors of epimastigote proliferation, obtaining inhibition values comparable to those achieved with the reference drug Benznidazole. Besides, these compounds displayed low cytotoxicity on mammalian cells. In vivo, both compounds protected mice against a challenge with a lethal Trypanosoma cruzi strain. These results allow us to propose 2-arylazoimidazoles as lead compounds for the design of novel drugs to treat Chagas' disease. Copyright © 2016 Elsevier Masson SAS. All rights reserved.

  14. Synthesis and biological activity evaluation of hydrazone derivatives based on a Tröger's base skeleton

    Czech Academy of Sciences Publication Activity Database

    Kaplánek, R.; Havlík, M.; Dolenský, B.; Rak, J.; Džubák, P.; Konečný, P.; Hajdúch, M.; Králová, Jarmila; Král, V.

    2015-01-01

    Roč. 23, č. 7 (2015), s. 1651-1659 ISSN 0968-0896 R&D Projects: GA ČR(CZ) GAP303/11/1291 Grant - others:GA MŠk(CZ) EE2.3.30.0060; GA MŠk(CZ) LO1304 Program:EE; LD Institutional support: RVO:68378050 Keywords : Anticancer agents * Cancer treatment * Complexation studies * Hydrazone * Troger's base Subject RIV: EB - Genetics ; Molecular Biology Impact factor: 2.923, year: 2015

  15. Evaluation of Biological Activity of Cellulose Pulp by Means of the Static Respiration Index (At4)/ Ocena Aktywności Biologicznej Pulpy Celulozowej Testem Respiracyjnym At4

    Science.gov (United States)

    Myszograj, Sylwia; Kozłowska, Katarzyna; Krochmal, Agata

    2014-09-01

    In the countries of the European Union, work is presently being conducted on the standardisation of the limit values and test methods for the determination of the biological activity of waste. The aim of conducting the tests is to monitor the effectiveness of waste biodegradation during composting, the evaluate any decrease in the biological activity of the waste before its landfilling and control processes taking place at landfills. The evaluation of the waste's biological activity can be performed, among others, by testing respiration. One such method is AT4 (Static Respiration Index) determination. The results of respirometric tests depict the availability of substrates for microorganisms, that is, the biodegradability. The article describes the tests of the biological activity of the cellulose pulp, the impact of the degree of compost inoculation on the value of this parameter and the dependence on the content of organic mass and total organic carbon in the tested substrate. The measurements of the oxygen demand were made using the OxiTop® Control measuring system. W krajach UE prowadzone są obecnie prace nad ujednoliceniem wartości granicznych oraz metod testowych oznaczania aktywności biologicznej odpadów. Celem prowadzenia testów jest monitoring efektywności biologicznego rozkładu odpadów podczas kompostowania, ocena zmniejszenia aktywności biologicznej odpadów przed ich składowaniem, kontrola procesów zachodzących na składowiskach. Ocenę aktywności biologicznej odpadów można przeprowadzić m.in. poprzez badanie respiracji. Jedną z takich metod jest oznaczenie AT4 (Static Respiration Index). Wyniki badań respirometrycznych obrazują dostępność substratów dla mikroorganizmów, czyli podatność na biodegradację. W artykule opisano badania aktywności biologicznej pulpy celulozowej testem AT4, wpływ stopnia zaczepienia kompostem na wartość tego parametru oraz zależność od zawartości masy organicznej i OWO w badanym substracie

  16. Monitoring Biological Activity at Geothermal Power Plants

    Energy Technology Data Exchange (ETDEWEB)

    Peter Pryfogle

    2005-09-01

    The economic impact of microbial growth in geothermal power plants has been estimated to be as high as $500,000 annually for a 100 MWe plant. Many methods are available to monitor biological activity at these facilities; however, very few plants have any on-line monitoring program in place. Metal coupon, selective culturing (MPN), total organic carbon (TOC), adenosine triphosphate (ATP), respirometry, phospholipid fatty acid (PLFA), and denaturing gradient gel electrophoresis (DGGE) characterizations have been conducted using water samples collected from geothermal plants located in California and Utah. In addition, the on-line performance of a commercial electrochemical monitor, the BIoGEORGE?, has been evaluated during extended deployments at geothermal facilities. This report provides a review of these techniques, presents data on their application from laboratory and field studies, and discusses their value in characterizing and monitoring biological activities at geothermal power plants.

  17. Synthesis and biological evaluation of histamine Schiff bases as carbonic anhydrase I, II, IV, VII, and IX activators.

    Science.gov (United States)

    Akocak, Suleyman; Lolak, Nabih; Vullo, Daniela; Durgun, Mustafa; Supuran, Claudiu T

    2017-12-01

    A series of 20 histamine Schiff base was synthesised by reaction of histamine, a well known carbonic anhydrase (CA, E.C 4.2.2.1.) activator pharmacophore, with substituted aldehydes. The obtained histamine Schiff bases were assayed as activators of five selected human (h) CA isozymes, the cytosolic hCA I, hCA II, and hCA VII, the membrane-anchored hCA IV and transmembrane hCA IX. Some of these compounds showed efficient activity (in the nanomolar range) against the cytosolic isoform hCA VII, which is a key CA enzyme involved in brain metabolism. Moderate activity was observed against hCA I and hCA IV (in the nanomolar to low micromolar range). The structure-activity relationship for activation of these isoforms with the new histamine Schiff bases is discussed in detail based on the nature of the aliphatic, aromatic, or heterocyclic moiety present in the aldehyde fragment of the molecule, which may participate in diverse interactions with amino acid residues at the entrance of the active site, where activators bind, and which is the most variable part among the different CA isoforms.

  18. Biological activity of liposomal vanillin.

    Science.gov (United States)

    Castan, Leniher; Del Toro, Grisel; Fernández, Adolfo A; González, Manuel; Ortíz, Emilia; Lobo, Daliana

    2013-06-01

    This article presents a study of vanillin encapsulation inside multilamellar liposomes, with emphasis on the evaluation of antioxidant activity, the hemolytic effect, and the antisickling properties of these products. Egg phosphatidylcholine-cholesterol and egg phosphatidylcholine-cholesterol-1-O-decylglycerol liposomes were prepared by mechanical dispersion, all with vanillin included. Vesicles were characterized by determination of encapsulation efficiency and vanillin retention capacity. Antioxidant activity was determined by the 2,2-diphenyl-1-picrylhydrazyl (DPPH) method. The hemolytic effect of liposomes was also evaluated by spectrophotometry, as well as the antisickling activity by the Huck test using optical microscopy. Results showed that the lipid composition of liposomes did not significantly affect the encapsulation efficiency. Stable vesicles were obtained with a high retention percentage of vanillin. Liposomes exhibited a high capture of the DPPH radical compared to free vanillin and 1-O-decylglycerol (C10) in solution. Vesicles caused no significant hemolisys in normal erythrocytes, nor in those coming from patients with sickle cell anemia. Vanillin encapsulated in liposomes retained its antisickling activity, with a greater effect for C10-containing vesicles. Our results show that vanillin encapsulation in liposomes is a way to enhance the pharmacologic properties of this molecule using a suitable vehicle.

  19. Synthesis and biological evaluation of isomeric methoxy substitutions on anti-cancer indolyl-pyridinyl-propenones: Effects on potency and mode of activity.

    Science.gov (United States)

    Trabbic, Christopher J; George, Sage M; Alexander, Evan M; Du, Shengnan; Offenbacher, Jennifer M; Crissman, Emily J; Overmeyer, Jean H; Maltese, William A; Erhardt, Paul W

    2016-10-21

    Certain indolyl-pyridinyl-propenone analogues kill glioblastoma cells that have become resistant to conventional therapeutic drugs. Some of these analogues induce a novel form of non-apoptotic cell death called methuosis, while others primarily cause microtubule disruption. Ready access to 5-indole substitution has allowed characterization of this position to be important for both types of mechanisms when a simple methoxy group is present. We now report the syntheses and biological effects of isomeric methoxy substitutions on the indole ring. Additionally, analogues containing a trimethoxyphenyl group in place of the pyridinyl moiety were evaluated for anticancer activity. The results demonstrate that the location of the methoxy group can alter both the potency and the mechanism of cell death. Remarkably, changing the methoxy from the 5-position to the 6-position switched the biological activity from induction of methuosis to disruption of microtubules. The latter may represent a prototype for a new class of mitotic inhibitors with potential therapeutic utility. Copyright © 2016 Elsevier Masson SAS. All rights reserved.

  20. Isoflavones: estrogenic activity, biological effect and bioavailability.

    Science.gov (United States)

    Vitale, Daniela Cristina; Piazza, Cateno; Melilli, Barbara; Drago, Filippo; Salomone, Salvatore

    2013-03-01

    Isoflavones are phytoestrogens with potent estrogenic activity; genistein, daidzein and glycitein are the most active isoflavones found in soy beans. Phytoestrogens have similarity in structure with the human female hormone 17-β-estradiol, which can bind to both alpha and beta estrogen receptors, and mimic the action of estrogens on target organs, thereby exerting many health benefits when used in some hormone-dependent diseases. Numerous clinical studies claim benefits of genistein and daidzein in chemoprevention of breast and prostate cancer, cardiovascular disease and osteoporosis as well as in relieving postmenopausal symptoms. The ability of isoflavones to prevent cancer and other chronic diseases largely depends on pharmacokinetic properties of these compounds, in particular absorption and distribution to the target tissue. The chemical form in which isoflavones occur is important because it influences their bioavailability and, therefore, their biological activity. Glucose-conjugated isoflavones are highly polar, water-soluble compounds. They are hardly absorbed by the intestinal epithelium and have weaker biological activities than the corresponding aglycone. Different microbial families of colon can transform glycosylated isoflavones into aglycones. Clinical studies show important differences between the aglycone and conjugated forms of genistein and daidzein. The evaluation of isoflavone metabolism and bioavailability is crucial to understanding their biological effects. Lipid-based formulations such as drug incorporation into oils, emulsions and self-microemulsifying formulations have been introduced to increase bioavailability. Complexation with cyclodextrin also represent a valid method to improve the physicochemical characteristics of these substances in order to be absorbed and distributed to target tissues. We review and discuss pharmacokinetic issues that critically influence the biological activity of isoflavones.

  1. Exploring the biological activities of Echeveria leucotricha.

    Science.gov (United States)

    Martínez Ruiz, María G; Gómez-Velasco, Anaximandro; Juárez, Zaida N; Hernández, Luis R; Bach, Horacio

    2013-01-01

    Echeveria leucotricha J. A. Purpus (Crassulaceae) was evaluated for its potential antibacterial, antifungal, antiparasitic, cytotoxic and anti-inflammatory bioactivities. Aerial parts were extracted with hexane, methanol and chloroform, and fractionated accordingly. Biological activity was assessed in vitro against five Gram-positive and four Gram-negative bacteria, four human pathogenic fungi and the protozoan Leishmania donovani. Extracts and fractions showing bioactivities were further investigated for their cytotoxic activities on macrophages. Results show that several extracts and fractions exhibited significant antibacterial, antifungal, and antiparasitic activities, but no anti-inflammatory activity was recorded. Here, we report for the first time, and to the best of our knowledge, these bioactivities, which suggest that this plant can be used in the traditional Mexican medicine.

  2. Design, synthesis and biological evaluation of novel aryldiketo acids with enhanced antibacterial activity against multidrug resistant bacterial strains.

    Science.gov (United States)

    Cvijetić, Ilija N; Verbić, Tatjana Ž; Ernesto de Resende, Pedro; Stapleton, Paul; Gibbons, Simon; Juranić, Ivan O; Drakulić, Branko J; Zloh, Mire

    2018-01-01

    Antimicrobial resistance (AMR) is a major health problem worldwide, because of ability of bacteria, fungi and viruses to evade known therapeutic agents used in treatment of infections. Aryldiketo acids (ADK) have shown antimicrobial activity against several resistant strains including Gram-positive Staphylococcus aureus bacteria. Our previous studies revealed that ADK analogues having bulky alkyl group in ortho position on a phenyl ring have up to ten times better activity than norfloxacin against the same strains. Rational modifications of analogues by introduction of hydrophobic substituents on the aromatic ring has led to more than tenfold increase in antibacterial activity against multidrug resistant Gram positive strains. To elucidate a potential mechanism of action for this potentially novel class of antimicrobials, several bacterial enzymes were identified as putative targets according to literature data and pharmacophoric similarity searches for potent ADK analogues. Among the seven bacterial targets chosen, the strongest favorable binding interactions were observed between most active analogue and S. aureus dehydrosqualene synthase and DNA gyrase. Furthermore, the docking results in combination with literature data suggest that these novel molecules could also target several other bacterial enzymes, including prenyl-transferases and methionine aminopeptidase. These results and our statistically significant 3D QSAR model could be used to guide the further design of more potent derivatives as well as in virtual screening for novel antibacterial agents. Copyright © 2017 Elsevier Masson SAS. All rights reserved.

  3. Evaluation of the Biological Activity of Opuntia ficus indica as a Tissue- and Estrogen Receptor Subtype-Selective Modulator.

    Science.gov (United States)

    An, Byoung Ha; Jeong, Hyesoo; Zhou, Wenmei; Liu, Xiyuan; Kim, Soolin; Jang, Chang Young; Kim, Hyun-Sook; Sohn, Johann; Park, Hye-Jin; Sung, Na-Hye; Hong, Cheol Yi; Chang, Minsun

    2016-06-01

    Phytoestrogens are selective estrogen receptor modulators (SERMs) with potential for use in hormone replacement therapy (HRT) to relieve peri/postmenopausal symptoms. This study was aimed at elucidating the molecular mechanisms underlying the SERM properties of the extract of Korean-grown Opuntia ficus-indica (KOFI). The KOFI extract induced estrogen response element (ERE)-driven transcription in breast and endometrial cancer cell lines and the expression of endogenous estrogen-responsive genes in breast cancer cells. The flavonoid content of different KOFI preparations affected ERE-luciferase activities, implying that the flavonoid composition likely mediated the estrogenic activities in cells. Oral administration of KOFI decreased the weight gain and levels of both serum glucose and triglyceride in ovariectomized (OVX) rats. Finally, KOFI had an inhibitory effect on the 17β-estradiol-induced proliferation of the endometrial epithelium in OVX rats. Our data demonstrate that KOFI exhibited SERM activity with no uterotrophic side effects. Therefore, KOFI alone or in combination with other botanical supplements, vitamins, or minerals may be an effective and safe alternative active ingredient to HRTs, for the management of postmenopausal symptoms. Copyright © 2016 John Wiley & Sons, Ltd. Copyright © 2016 John Wiley & Sons, Ltd.

  4. Biological activities of leaves of ethnomedicinal plant, Borassus flabellifer Linn. (Palmyra palm: An antibacterial, antifungal and antioxidant evaluation

    Directory of Open Access Journals (Sweden)

    Prasad G. Jamkhande

    2016-06-01

    Full Text Available Plants contain a variety of phytochemicals that have the ability to exert effect on human body. Among them Borassus flabellifer Linn. is a medicinally important plant. In traditional medicine different parts of plants are being used for their medicinal properties. The methanol extract was obtained from powdered leaves and further fractions were prepared. Antimicrobial potential was investigated using eight pathogenic strains of bacteria and fungi by agar well diffusion method. Broth dilution method was employed to MIC and MMC of active samples and MIC index value was determined. ME was subjected to preliminary phytochemical analysis; and 1,1-diphenyl-2-picrylhydrazyl (DPPH and hydrogen peroxide (H2O2 radical scavenging activity. Phytochemical screening revealed the presence of several phytochemicals. The ME showed dose dependent radical scavenging activity as evidenced by IC50 values for DPPH (40.19 μg/ml and H2O2 (30.92 μg/ml radicals. The inhibition zones and MIC values for bacterial strains were in the range of 10–16 mm and 50–70 μg/ml, respectively. All the samples showed an inhibitory effect on fungal strains with inhibition zone (10–17 mm and MFC (50–70 μg/ml. Samples exhibited diverse patterns of antibacterial and antifungal effects. Among the tested samples, methanol extract and acetone fraction (AF had potent antibacterial and antifungal activities. These results lead to the conclusion that the plant has a broad spectrum antimicrobial and antioxidant activity and could be a potential option for treating various infectious diseases. The strong antioxidant property of methanol extract might be employed in the development of natural antioxidants for agro-food and pharmaceutical industries.

  5. Inorganic composition determination and evaluation of the biological activity of Peperomia pellucida in the Aspergillus flavus growth

    International Nuclear Information System (INIS)

    Sussa, Fabio Vitorio

    2011-01-01

    In recent decades, there has been a great advancement in research in developing drugs from plants. Nevertheless, little significant care exists in the literature about the stable concentration of elements, as well as the activity concentration of '2 38 U and 232 Th decay products in plants used for this purpose in Brazil. The presence of stable elements and radionuclides in plants constitutes the pathway for their migration to humans, via uptake of tea or remedies made with medicinal herbs. Peperomia pellucida, whose popular name is 'erva de jabuti', is a plant known by its medicinal usages, such as healing and analgesic properties plus antibacterial and antifungal activities against food fungi. In this study, the elemental composition of Peperomia pellucida and surrounding soil samples collected in the Botanical Garden in Rio de Janeiro was determined; the elemental concentration in the alcoholic extract and infusion processes of dry plants was also determined. The elemental concentration of As, Ba, Br, Ce, Co, Cr, Cs, Eu, Fe, Hf, K, La, Lu, Na, Nd, Rb, Sb, Sc, Sm, Ta, Tb, Th, U, Yb and Zn was determined in the leaves, aerial parts, including leaves, stems and roots of Peperomia pellucida, in their extracts obtained by maceration and infusions and in the surrounding soil by the Instrumental Neutron Activation Analysis (INAA). The analytical methodology used to determine the elements Cd, Hg and Pb was the Atomic Absorption Spectrometry (AAS); the activities of 226 Ra, 228 Ra and 210 Pb were carried out by gross alpha and beta counting, after radiochemical separation. The quality of the obtained results was assured by the analyses of the certified reference materials IAEA-336 Lichen, IAEA-Soil-7, IAEA-326 Radionuclides in soil, NIST 1515 Apple Leaves and NIST 1542 Peach Leaves. The relative standard deviations and the relative errors obtained in these analyses indicated good precision and accuracy of the results. The essential oil, ethanolic and hexane extracts of

  6. Synthesis and biological evaluation of indeno[1,5]naphthyridines as topoisomerase I (TopI) inhibitors with antiproliferative activity.

    Science.gov (United States)

    Alonso, Concepción; Fuertes, María; González, María; Rubiales, Gloria; Tesauro, Cinzia; Knudsen, Birgitta R; Palacios, Francisco

    2016-06-10

    In an effort to establish new candidates with improved anticancer activity, we report here the synthesis of various series of 7H-indeno[2,1-c][1,5]-naphthyridines and novel 7H-indeno[2,1-c][1,5]-naphthyridine-7-ones and 7H-indeno[2,1-c][1,5]-naphthyridine-7-ols. Most of the products which were synthesized were able to inhibit Topoisomerase I activity. Moreover, in vitro testing demonstrated that a subset of the products exhibited a cytotoxic effect on cell lines derived from human breast cancer (BT 20), human lung adenocarcinoma (A 549), or human ovarian carcinoma (SKOV3). Copyright © 2016 Elsevier Masson SAS. All rights reserved.

  7. Ethnobotanical and biological activities of Leptadenia pyrotechnica ...

    African Journals Online (AJOL)

    Conclusion: This review includes the substance of different ethnobotanical uses, phytochemistry and exclusive capability of this plant in the field of anti-microbial and human disease activities. Key words: Leptadenia pyrotechnica, Biological activities, Desert plant, Ethnobotanical, Phytochemical activity, phytochemistry.

  8. Structure-activity relationships in lipopolysaccharide neutralizers: design, synthesis, and biological evaluation of a 540-membered amphipathic bisamide library.

    Science.gov (United States)

    Burns, Mark R; Jenkins, Scott A; Wood, Stewart J; Miller, Kelly; David, Sunil A

    2006-01-01

    Lipopolysaccharides (LPS), also called "endotoxins", are outer-membrane constituents of Gram-negative bacteria. Lipopolysaccharides play a key role in the pathogenesis of "septic shock", a major cause of mortality in the critically ill patient. We had earlier shown that small molecules bind and neutralize LPS if they contain (i) two protonatable cationic groups separated by a distance of approximately 14 A to facilitate interactions with the phosphate moieties on the lipid Angstrom component of LPS and (ii) a long-chain aliphatic hydrocarbon to promote hydrophobic interactions. In an effort to identify optimal scaffolds possessing the above structural requirements, we now present an evaluation of a rationally designed combinatorial library in which the elements of the scaffold are systematically varied to maximize sampling of chemical space. Leads obtained via molecular analyses of the screening results were resynthesized and evaluated in greater detail with regard to the affinity of the interaction with LPS, as well as neutralization of endotoxicity in in vitro assays. The examination of a moderately sized 6 x 6 x 15 (540-membered) focused library allowed the assessment of the structural contributions to binding by the long-chain aliphatic tails, distance between charged amino groups, and potential aromatic CH-pi or OH-pi interactions. These findings are of value in further iterations of design and development of specific and potent endotoxin sequestrants.

  9. Evaluating vertical concentration profile of carbon source released from slow-releasing carbon source tablets and in situ biological nitrate denitrification activity

    Science.gov (United States)

    Yeum, Y.; HAN, K.; Yoon, J.; Lee, J. H.; Song, K.; Kang, J. H.; Park, C. W.; Kwon, S.; Kim, Y.

    2017-12-01

    Slow-releasing carbon source tablets were manufactured during the design of a small-scale in situ biological denitrification system to reduce high-strength nitrate (> 30 mg N/L) from a point source such as livestock complexes. Two types of slow-releasing tablets, precipitating tablet (PT, apparent density of 2.0 g/mL) and floating tablet (FT), were prepared to achieve a vertically even distribution of carbon source (CS) in a well and an aquifer. Hydroxypropyl methylcellulose (HPMC) was used to control the release rate, and microcrystalline cellulose pH 101 (MCC 101) was added as a binder. The #8 sand was used as a precipitation agent for the PTs, and the floating agents for the FTs were calcium carbonate and citric acid. FTs floated within 30 min. and remained in water because of the buoyance from carbon dioxide, which formed during the acid-base reaction between citric acid and calcium carbonate. The longevities of PTs with 300 mg of HPMC and FTs with 400 mg of HPMC were 25.4 days and 37.3 days, respectively. We assessed vertical CS profile in a continuous flowing physical aquifer model (release test, RT) and its efficiency on biological nitrate denitrification (denitrification test, DT). During the RT, PTs, FTs and a tracer (as 1 mg rhodamine B/L) were initially injected into a well of physical aquifer model (PAM). Concentrations of CS and the tracer were monitored along the streamline in the PAM to evaluate vertical profile of CS. During the DT, the same experiment was performed as RT, except continuous injection of solution containing 30 mg N/L into the PAM to evaluate biological denitrification activity. As a result of RT, temporal profiles of CS were similar at 3 different depths of monitoring wells. These results suggest that simultaneous addition of PT and FT be suitable for achieving a vertically even distribution of the CS in the injection well and an aquifer. In DT, similar profile of CS was detected in the injection well, and nitrate was biologically

  10. Phytochemical Characterization, Biological Activity Evaluation of Ethanolic Extract of Cinnamomum zeylanicum and Molecular Docking Analysis of Active Component Cinnamaldehyde against Selected Protein Targets.

    Science.gov (United States)

    Husain, Ishrat; Ahmad, Rumana; Chandra, Anu; Raza, Syed Tasleem; Shukla, Yogeshwer; Mahdi, Farzana

    2018-02-02

    India being a multicultural nation, every region of the country offers a distinct culinary flavor and taste. These flavours are attributed to spices and condiments which form the mainstay of Indian cuisine. Most of these spices and condiments are derived from various biodiversity hotspots in India and form the crux of India's multidiverse and multicultural cuisine. Apart from their varying aromas, flavors and tastes, these spices and condiments are known to possess several medicinal properties also. Most of these spices find considerable mention in Ayurveda, the indigenous system of medicine, as panaceas for several aliments. Cinnamomum zeylanicum (CZ), belonging to family Lauraceae and commonly known as cinnamon is one such spice known to have diverse medicinal properties since time immemorial. In the present study, apoptotic and anti-microbial activity of ethanolic extract of CZ was evaluated against human breast cancer cell line MDA-MB-231 and compared for its effect on normal kidney epithelial cell line Vero. Ethanolic extract of tree bark of CZ was used to determine the cytotoxic effect on MDA-MB-231 using Trypan blue dye exclusion method and cytometry. The tested dose of the extract was 10-100µg/mL. Antibacterial activity was determined using disc diffusion method against Staphylococcus aureus and Escherichia coli in the range 2-10mg/mL. Apoptotic activity was determined using DNA fragmentation assay. Molecular docking analysis of cinnamaldehyde, the major active component found in CZ bark, was carried out using AutoDock 4.0.1 to study its inhibitory action against selected protein targets. Ethanolic extract of CZ was found to have an IC 50 value of 25µg/mL against MDA cell line. On the other hand, CZ extract did not have any significant effect on Vero cells even at 100µg/mL (IC 50 >100µg/mL). The ethanolic extract of CZ bark showed significant antibacterial activity against S. aureus at 10mg/mL while no appreciable activity was detected against E. coli

  11. Factorial design of essential oil extraction from Fagraea fragrans Roxb. flowers and evaluation of its biological activities for perfumery and cosmetic applications.

    Science.gov (United States)

    Yingngam, B; Brantner, A H

    2015-06-01

    To optimize the extraction yields of essential oil from Fagraea fragrans Roxb. flowers in hydro-distillation using a central composite design (CCD) and to evaluate its biological activities for perfumery and cosmetic applications. Central composite design was applied to study the influences of operational parameters [water to flower weight (X(1)) and distillation time (X(2))] on the yields of essential oil (Y). Chemical compositions of the essential oil extracted from the optimized condition were identified by gas chromatography-mass spectrometry. Antioxidant activities of the essential oil were determined against ABTS(•+) and DPPH(•) radicals, and the cytotoxic effects were assessed on human embryonic kidney (HEK293) cells by the use of the MTT assay. Also, the aromatic properties of the essential oil were evaluated by five healthy trained volunteers. The best conditions to obtain the maximum essential oil yield were 7.5 mL g(-1) (X(1)) and 215 min (X(2)). The experimental yield of the essential oil (0.35 ± 0.02% v/w) was close to the value predicted by a mathematical model (0.35 ± 0.01% v/w). 3-Octadecyne, Z,Z,Z-7,10,13-hexadecatrienal, E-nerolidol, pentadecanal and linalool were the major constituents of the essential oil. The essential oil showed moderate antioxidant capacities with no toxic effects on HEK293 cells at 1-250 μg mL(-1). Also, the essential oil exhibited a very strong aroma and was classified to be top- to middle-notes. The results offer the effectively operational conditions in the extraction of essential oil from F. fragrans using hydro-distillation. The essential oil could be used as a natural fragrance, having antioxidant activity with slight cytotoxicity, for perfumery and cosmetic applications. © 2014 Society of Cosmetic Scientists and the Société Française de Cosmétologie.

  12. Colour Evaluation, Bioactive Compound Content, Phenolic Acid Profiles and in Vitro Biological Activity of Passerina del Frusinate White Wines: Influence of Pre-Fermentative Skin Contact Times

    Directory of Open Access Journals (Sweden)

    Katya Carbone

    2016-07-01

    Full Text Available Passerina del Frusinate is an autochthonous wine grape variety, which grows in the Lazio region that is currently being evaluated by local wine producers. In this study, colour properties (CIELab coordinates, bioactive compounds (total polyphenols and flavan-3-ols, HPLC-DAD phenolic acid profiles and in vitro biological activity of monovarietal Passerina del Frusinate white wines and the effect of different maceration times (0, 18 and 24 h were evaluated based on these parameters. Results highlighted statistically significant differences for almost all analysed parameters due to a strong influence of the pre-fermentative skin contact time. The flavan content of macerated wines was six times higher than that of the control, while total polyphenols were 1.5 times higher. According to their phytochemical content, macerated wines showed the highest antiradical capacity tested by means of DPPH• and ABTS+• assays. Besides, prolonged maceration resulted in a reduction of CIELab coordinates as well as of the content of phenolic substances and antiradical capacity. Among the phenolic acids analysed, the most abundant were vanillic acid and caffeic acid; the latter proved to be the most susceptible to degradation as a result of prolonged maceration. Passerina del Frusinate appears as a phenol-rich white wine with a strong antioxidant potential similar to that of red wines.

  13. Synthesis and Biological Activities of Some Benzimidazoles ...

    African Journals Online (AJOL)

    The chemical structures of these compounds were elucidated using NMR and elemental analysis. The biological activity of these compounds as fungicides was tested against three commercially known fungicides (C. albicans, patient isolate C. glabrata and C. krusei).The biological activity of two compounds was found to be ...

  14. Biological and biochemical evaluation of some prepared high ...

    African Journals Online (AJOL)

    Biological and biochemical evaluation of some prepared high antioxidant fruit beverages as functional foods. W A El-Malky ... The beverage which contain mango, red grape, carrot and tomato was the best prepared beverages according to the sensory evaluation, chemical composition and antioxidant activity. The high ...

  15. Synthesis and Biological Evaluation of Some Pyridine Derivatives as ...

    African Journals Online (AJOL)

    Synthesis and Biological Evaluation of Some Pyridine Derivatives as Antimicrobial Agents. ... Ethiopian Pharmaceutical Journal ... In this study, several pyridine derivatives were synthesized and evaluated for their in vitro antimicrobial activity against Gram-positive bacteria (Bacillus cereus and Staphylococcus aureus), ...

  16. Benzimidazoles: A biologically active compounds

    Directory of Open Access Journals (Sweden)

    Salahuddin

    2017-02-01

    Full Text Available Synthesis of commercially available benzimidazole involves condensation of o-phenylenediamine with formic acid. The most prominent benzimidazole compound in nature is N-riosyldimethylbenzimidazole, which serves as a axial ligand for cobalt in vitamin B12. The benzimidazole and its derivatives play a very important role as a therapeutic agent e.g. antiulcer and anthelmintic drugs. Apart from this the benzimidazole derivatives exhibit pharmacological activities such as antimicrobial, antiviral, anticancer, anti-inflammatory, analgesic, etc. The substituted benzimidazoles are summarized in this review to know about the chemistry as well as pharmacological activities.

  17. Synthesis, characterization and biological evaluation of tryptamine based benzamide derivatives.

    Science.gov (United States)

    Aftab, Kiran; Aslam, Kinza; Kousar, Shazia; Nadeem, Muhammad Jawad Ul Hasan

    2016-03-01

    Benzamides and tryptamine are biologically significant compounds, therefore, various benzamide analogous of tryptamine have been efficiently synthesized using tryptamine and different benzoyl chlorides, in order to find new biologically active compounds. The resulting products were then characterized by melting point determination, calculation of Rf values and LC-MS techniques. At last, structure activity relationship (SAR) of the synthesized compounds was evaluated against two microbial strains; Bacillus subtilis and Aspergillus niger. All the five prepared products have shown high yield, sharp characterization and significant resistance against the growth of tested microorganism, providing a new range of tryptamine based benzamide derivatives having significant antimicrobial activities.

  18. Evaluation of the biological activities of the IL-15 superagonist complex, ALT-803, following intravenous versus subcutaneous administration in murine models.

    Science.gov (United States)

    Liu, Bai; Jones, Monica; Kong, Lin; Noel, Terra; Jeng, Emily K; Shi, Sixiang; England, Christopher G; Alter, Sarah; Miller, Jeffrey S; Cai, Weibo; Rhode, Peter R; Wong, Hing C

    2018-02-13

    ALT-803 is a fusion protein complex consisting of an interleukin (IL)-15 superagonist and a dimeric IL-15 receptor alpha sushi domain IgG1 Fc fusion protein. When administered to mice, ALT-803 is capable of inducing natural killer (NK) and CD8 + T cell proliferation and activation, and effectively promoting potent anti-tumor responses. Currently, ALT-803 is in clinical trials for treatment of various solid tumors and hematological malignancies. In the initial phase of these clinical studies, intravenous (iv) injection was used according to the route used in pre-clinical efficacy studies. In order to evaluate the possible advantage of subcutaneous (sc) injection versus iv injection, this study compared the biological activity of the two treatment regimens of ALT-803 in pre-clinical in vivo models. The pharmacokinetics, immune stimulation, and anti-tumor efficacy of iv and sc injection routes of ALT-803 in C57BL/6 mice were compared. The half-life of ALT-803 was 7.5 h for iv versus 7.7 h for sc with the maximal detected serum concentration of ALT-803 to be 3926 ng/ml at 0.5 h time-point following iv injection versus 495 ng/ml at 16 h post sc injection. Biodistribution studies indicated that sc ALT-803, similarly to iv ALT-803 as previously reported, has a greater tissue distribution and longer residence time in lymphoid tissues compared to recombinant IL-15. Notably, ALT-803 when administered either iv or sc induced comparable proliferation and activation of CD8 + T and NK cells and resulted in similar reductions of tumor burden. A toxicity study of mice receiving multiple injections of ALT-803 for 4 weeks by iv or sc routes revealed equivalent immune-related changes. The gradual absorbance into the blood stream and lower maximal blood levels of ALT-803 in sc-injected mice, along with similar anti-tumor efficacy support the administration of ALT-803 by sc injection in patients with various malignancies and infectious diseases. Copyright © 2017 Elsevier

  19. Elsholtzia: phytochemistry and biological activities

    Directory of Open Access Journals (Sweden)

    Guo Zhiqin

    2012-12-01

    Full Text Available Abstract Plants of the genus Elsholtzia (Lamiaceae have a long history of medicinal use in folk. The phytochemical investigations revealed the presence of flavonoids, phenylpropanoids, terpenoids, and other compounds. Abundant volatile components are also identified. Pure compounds, volatile constituents and crude extracts from the genus exhibited a wide spectrum of in vitro and in vivo pharmacological activities. The aims of this review hopefully provide comprehensive information on the distribution, phytochemistry, volatile components, and pharmacological research of Elsholtzia for exploring the potential and advance researches.

  20. Triazoles: a valuable insight into recent developments and biological activities.

    Science.gov (United States)

    Sahu, Jagdish K; Ganguly, Swastika; Kaushik, Atul

    2013-09-01

    In recent years, heterocyclic compounds, analogs, and derivatives have attracted strong interest due to their useful biological and pharmacological properties. The small and simple triazole nucleus is present in compounds aimed at evaluating new entities that possess anti-microbial, anti-tumor, antitubercular, anti-convulsant, anti-depressant, antimalarial, and anti-inflammatory activities. Triazoles display a broad range of biological activities and are found in many potent, biologically active compounds, such as trazodone (antidepressant drug), rizatriptan (antimigrane drug), hexaconazole (antifungal drug) and alprazolam (hyptonic, sedative and tranquilizer drug). So far, modifications of the triazole ring have proven highly effective with improved potency and lesser toxicity. The present review highlights the recently synthesized triazoles possessing important biological activities. Copyright © 2013 China Pharmaceutical University. Published by Elsevier B.V. All rights reserved.

  1. Cytotoxic Activity of Origanum Vulgare L. on Hepatocellular Carcinoma cell Line HepG2 and Evaluation of its Biological Activity

    Directory of Open Access Journals (Sweden)

    Hazem S. Elshafie

    2017-08-01

    Full Text Available The potential of plant essential oils (EOs in anticancer treatment has recently received many research efforts to overcome the development of multidrug resistance and their negative side effects. The aims of the current research are to study (i the cytotoxic effect of the crude EO extracted from Origanum vulgare subsp hirtum and its main constituents (carvacrol, thymol, citral and limonene on hepatocarcinoma HepG2 and healthy human renal cells HEK293; (ii the antibacterial and phytotoxic activities of the above EO and its main constituents. Results showed that cell viability percentage of treated HepG2 by EO and its main constituents was significantly decreased when compared to untreated cells. The calculated inhibition concentration (IC50 values for HepG2 were lower than healthy renal cells, indicating the sort of selectivity of the studied substances. Citral is not potentially recommended as an anticancer therapeutic agent, since there are no significant differences between IC50 values against both tested cell lines. Results showed also that oregano EO and its main constituents have a significant antibacterial activity and a moderate phytotoxic effect. The current research verified that oregano EO and its main constituents could be potentially utilized as anticancer therapeutic agents.

  2. Marine Biology Activities. Ocean Related Curriculum Activities.

    Science.gov (United States)

    Pauls, John

    The ocean affects all of our lives. Therefore, awareness of and information about the interconnections between humans and oceans are prerequisites to making sound decisions for the future. Project ORCA (Ocean Related Curriculum Activities) has developed interdisciplinary curriculum materials designed to meet the needs of students and teachers…

  3. Genus Pouteria: chemistry and biological activity

    Directory of Open Access Journals (Sweden)

    Cíntia A. M. Silva

    Full Text Available The genus Pouteria belongs to the family Sapotaceae and can be widely found around the World. These plants have been used as building material, as food, because the eatable fruits, as well as remedies in folk medicine. Some biological activities have been reported to species of this genus such as antioxidant, anti-inflammatory, antibacterial and antifungal. However, the real potential of this genus as source of new drugs or phytomedicines remains unknown. Therefore, a review of the so far known chemical composition and biological activities of this genus is presented to stimulate new studies about the species already reported moreover that species have no reference about chemistry or biological activities could be found until now.

  4. Evaluation of Potential Biological Threats in Ukraine

    International Nuclear Information System (INIS)

    Pozdnyakova, L.; Slavina, N.; Pozdnyakov, S.

    2007-01-01

    Dilating of biological threats spectrum, EDI diffusion opportunities and routes, unpredictability of outbreaks connected with connatural, technogenic, terrorist factors determines constant monitoring and readiness for operative BPA indication and identification. Scientific analytical approach of existing and probable regional bio-threats evaluation is necessary for adequate readiness system creation and maintenance of medical counteraction tactics to probable biological threats. Basing on the international experience, we carry out analysis of a situation present in Ukraine and routes for the decisions. The basic directions are: - Evaluation of a reality for EDI penetration from abroad and presence of conditions for their further diffusion inside the country. - Revealing of presence and definition of connatural EDI foci biocenoses features and BPAs. - Appropriate level of biological safety and physical protection of bio-laboratories and pathogens collections maintenance. - Gene/molecular and phenotypical definition of EDI circulating strains. - Creation of the circulating EDI gene/ phenotypic characteristics regional data bank. - Ranging of EDI actual for area. - Introduction of GPT, mathematical modeling and forecasting for tactics development in case of technogenic accidents and connatural outbreaks. - Methodical basis and equipment improvement for BPA system indication for well-timed identification of natural, or modified agent. - Education and training The international cooperation in maintenance of biosafety and bioprotection within the framework of scientific programs, grants, exchange of experience, introduction of international standards and rules are among basic factors in the decision for creating system national biosafety for countries not included in EU and the NATO. (author)

  5. Expression and Purification of Soluble, Biologically Active ...

    African Journals Online (AJOL)

    Expression and Purification of Soluble, Biologically Active Recombinant Dipeptidyl Peptidase 4 (DPP4/CD26/ADAbp) Comprising the Extracellular Domain in the Yeast, Pichia ... Purpose: To investigate Pichia pastoris expression system for producing clinically usable, high-quality dipeptidyl peptidase 4 recombinant protein.

  6. Parameters of biological activity in colorectal cancer

    Czech Academy of Sciences Publication Activity Database

    Svobodová, Š.; Topolčan, O.; Holubec jr., L.; Levý, M.; Pecen, Ladislav; Svačina, Š.

    2011-01-01

    Roč. 31, č. 1 (2011), s. 373-378 ISSN 0250-7005 Institutional research plan: CEZ:AV0Z10300504 Keywords : colorectal cancer * biological activity * prognosis * tumor markers * angiogenetic factors * metalloproteinases * adhesion molecules Subject RIV: FD - Oncology ; Hematology Impact factor: 1.725, year: 2011

  7. Biological activity screening of seven Plectranthus species

    OpenAIRE

    Epole Ntungwe N; Joana Marçalo; Catarina Garcia; Catarina Reis; Catarina Teodósio; Carolina Oliveira; Cláudia Oliveira; Amílcar Roberto; Patrícia Rijo

    2017-01-01

    Natural products from Plectranthus spp. plants have an ethnopharmacological use, inspiring several scientific investigations. As such, this work aims to perform a biological activity screening in order to scientifically validate the use of these plants. Assays on in vitro acetylcholinesterase (AChE) inhibition, antioxidant effects, antimicrobial activity and Artemia salina lethality were performed on seven Plectranthus spp. extracts (P. swynnertonii, P. welwischii, P. woodii, P. cylindraceus,...

  8. Biological activity of SV40 DNA

    International Nuclear Information System (INIS)

    Abrahams, P.J.

    1978-01-01

    This thesis deals with a study on the biological activity of SV40 DNA. The transforming activity of SV40 DNA and DNA fragments is investigated in order to define as precisely as possible the area of the viral genome that is involved in the transformation. The infectivity of SV40 DNA is used to study the defective repair mechanisms of radiation damages of human xeroderma pigmentosum cells. (C.F.)

  9. SYNTHESIS OF BIOLOGICALLY-ACTIVE 2-BENZOYL PACLITAXEL ANALOGS

    DEFF Research Database (Denmark)

    GEORG, GI; ALI, SM; BOGE, TC

    1995-01-01

    The influence of aromatic substitution at the 2-benzoyl moiety of paclitaxel on biological activity was investigated, following the Topliss Operational Scheme. Twelve paclitaxel derivatives were synthesized and evaluated in a microtubule assembly assay and for cytotoxicity against B16 melanoma ce...

  10. Biological activities of species in the genus Tulbaghia : A review ...

    African Journals Online (AJOL)

    Species of the genus Tulbaghia has been widely used in traditional medicine to treat various ailments such rheumatism, fits, fever, earache, tuberculosis etc. It is believed that the species possess several therapeutic properties. This paper evaluates some of the biological activities of the genus Tulbaghia. It is evident from ...

  11. Synthesis, spectroscopic characterization and in vitro cytotoxicities of new organometallic palladium complexes with biologically active β-diketones; Biological evaluation probing of the interaction mechanism with DNA/Protein and molecular docking

    Science.gov (United States)

    Karami, Kazem; Rafiee, Mina; Lighvan, Zohreh Mehri; Zakariazadeh, Mostafa; Faal, Ali Yeganeh; Esmaeili, Seyed-Alireza; Momtazi-Borojeni, Amir Abbas

    2018-02-01

    [Pd{(C,N)sbnd C6H4CH (CH3)NH}(CUR)] (3) and [Pd2{(C,N)sbnd C6H4CH(CH3)NH2}2(μ-N3CS2)] (4) [cur = 1,7-bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dion] novel organometallic complexes with biologically active ligands have been prepared and characterized via elemental analysis, multinuclear spectroscopic techniques (1H, and 13C NMR and IR) and their biological activities, including antitumoral activity and DNA-protein interactions have been investigated. Fluorescence spectroscopy used to study the interaction of the complexes with BSA have shown the affinity of the complexes for these proteins with relatively high binding constant values and the changed secondary structure of BSA in the presence of the complexes. In the meantime, spectroscopy and competitive titration have been applied to investigate the interaction of complexes with Warfarin and Ibuprofen site markers for sites I and II, respectively, with BSA. The results have suggested that the locations of complexes 3 and 4 are sites II and I, respectively. UV-Vis spectroscopy, emission titration and helix melting methods have been used to study the interaction of these complexes with CT-DNA, indicating that complexes are bound to CT-DNA by intercalation binding mode. In addition, good cytotoxic activity against MCF-7 (human breast cancer) and JURKAT (human leukemia) cell line has been shown by both complexes whereas low cytotoxicity was exerted on normal peripheral blood mononuclear cells.

  12. 2-(Substituted phenyl-3,4-dihydroisoquinolin-2-iums as Novel Antifungal Lead Compounds: Biological Evaluation and Structure-Activity Relationships

    Directory of Open Access Journals (Sweden)

    Xin-Juan Yang

    2013-08-01

    Full Text Available The title compounds are a class of structurally simple analogues of quaternary benzo[c]phenanthridine alkaloids (QBAs. In order to develop novel QBA-like antifungal drugs, in this study, 24 of the title compounds with various substituents on the N-phenyl ring were evaluated for bioactivity against seven phytopathogenic fungi using the mycelial growth rate method and their SAR discussed. Almost all the compounds showed definite activities in vitro against each of the test fungi at 50 μg/mL and a broad antifungal spectrum. In most cases, the mono-halogenated compounds 2–12 exhibited excellent activities superior to the QBAs sanguinarine and chelerythrine. Compound 8 possessed the strongest activities on each of the fungi with EC50 values of 8.88–19.88 µg/mL and a significant concentration-dependent relationship. The SAR is as follows: the N-phenyl group is a high sensitive structural moiety for the activity and the characteristics and position of substituents intensively influence the activity. Generally, electron-withdrawing substituents remarkably enhance the activity while electron-donating substituents cause a decrease of the activity. In most cases, ortha- and para-halogenated isomers were more active than the corresponding m-halogenated isomers. Thus, the title compounds emerged as promising lead compounds for the development of novel biomimetic antifungal agrochemicals. Compounds 8 and 2 should have great potential as new broad spectrum antifungal agents for plant protection.

  13. Glycosides from Marine Sponges (Porifera, Demospongiae): Structures, Taxonomical Distribution, Biological Activities and Biological Roles

    Science.gov (United States)

    Kalinin, Vladimir I.; Ivanchina, Natalia V.; Krasokhin, Vladimir B.; Makarieva, Tatyana N.; Stonik, Valentin A.

    2012-01-01

    Literature data about glycosides from sponges (Porifera, Demospongiae) are reviewed. Structural diversity, biological activities, taxonomic distribution and biological functions of these natural products are discussed. PMID:23015769

  14. Biological Activities of the Essential Oil from Erigeron floribundus

    OpenAIRE

    Riccardo Petrelli; Giuseppe Orsomando; Leonardo Sorci; Filippo Maggi; Farahnaz Ranjbarian; Prosper C. Biapa Nya; Dezemona Petrelli; Luca A. Vitali; Giulio Lupidi; Luana Quassinti; Massimo Bramucci; Anders Hofer; Loredana Cappellacci

    2016-01-01

    Erigeron floribundus (Asteraceae) is an herbaceous plant widely used in Cameroonian traditional medicine to treat various diseases of microbial and non-microbial origin. In the present study, we evaluated the in vitro biological activities displayed by the essential oil obtained from the aerial parts of E. floribundus, namely the antioxidant, antimicrobial and antiproliferative activities. Moreover, we investigated the inhibitory effects of E. floribundus essential oil on nicotinate mononucle...

  15. Silychristin: Skeletal Alterations and Biological Activities

    Czech Academy of Sciences Publication Activity Database

    Biedermann, David; Buchta, M.; Holečková, Veronika; Sedlák, David; Valentová, Kateřina; Cvačka, Josef; Bednárová, Lucie; Křenková, Alena; Kuzma, Marek; Škuta, Ctibor; Peikerová, Žaneta; Bartůněk, Petr; Křen, Vladimír

    2016-01-01

    Roč. 79, č. 12 (2016), s. 3086-3092 ISSN 0163-3864 R&D Projects: GA ČR(CZ) GA15-03037S; GA MZd(CZ) NV16-27317A; GA MŠk LO1220; GA MŠk LM2015063; GA MŠk(CZ) LD15081 Institutional support: RVO:61388971 ; RVO:68378050 ; RVO:61388963 Keywords : Silychristin * skeletal alterations * biological activities Subject RIV: CC - Organic Chemistry Impact factor: 3.281, year: 2016

  16. Design, synthesis and biological evaluation of hybrid bioisoster derivatives of N-acylhydrazone and furoxan groups with potential and selective anti-Trypanosoma cruzi activity.

    Science.gov (United States)

    Massarico Serafim, Ricardo Augusto; Gonçalves, José Eduardo; de Souza, Felipe Pereira; de Melo Loureiro, Ana Paula; Storpirtis, Silvia; Krogh, Renata; Andricopulo, Adriano Defini; Dias, Luiz Carlos; Ferreira, Elizabeth Igne

    2014-07-23

    Hybrid bioisoster derivatives from N-acylhydrazones and furoxan groups were designed with the objective of obtaining at least a dual mechanism of action: cruzain inhibition and nitric oxide (NO) releasing activity. Fifteen designed compounds were synthesized varying the substitution in N-acylhydrazone and in furoxan group as well. They had its anti-Trypanosoma cruzi activity in amastigotes forms, NO releasing potential and inhibitory cruzain activity evaluated. The two most active compounds (6, 14) both in the parasite amastigotes and in the enzyme contain the nitro group in para position of the aromatic ring. The permeability screening in Caco-2 cell and cytotoxicity assay in human cells were performed for those most active compounds and both showed to be less cytotoxic than the reference drug, benznidazole. Compound 6 was the most promising, since besides activity it showed good permeability and selectivity index, higher than the reference drug. Thereby the compound 6 was considered as a possible candidate for additional studies. Copyright © 2014 Elsevier Masson SAS. All rights reserved.

  17. Synthesis, characterization and biological evaluation of ...

    Indian Academy of Sciences (India)

    5H-thiazolo[3,2-a]pyrimidine-2,6-dicarboxylic acid diethyl ester (3e) was verified by single crystal X-ray diffraction method. The antimicrobial activity was evaluated against four bacterial strains and one fungal species. Few of the derivatives ...

  18. Biology learning evaluation model in Senior High Schools

    Directory of Open Access Journals (Sweden)

    Sri Utari

    2017-06-01

    Full Text Available The study was to develop a Biology learning evaluation model in senior high schools that referred to the research and development model by Borg & Gall and the logic model. The evaluation model included the components of input, activities, output and outcomes. The developing procedures involved a preliminary study in the form of observation and theoretical review regarding the Biology learning evaluation in senior high schools. The product development was carried out by designing an evaluation model, designing an instrument, performing instrument experiment and performing implementation. The instrument experiment involved teachers and Students from Grade XII in senior high schools located in the City of Yogyakarta. For the data gathering technique and instrument, the researchers implemented observation sheet, questionnaire and test. The questionnaire was applied in order to attain information regarding teacher performance, learning performance, classroom atmosphere and scientific attitude; on the other hand, test was applied in order to attain information regarding Biology concept mastery. Then, for the analysis of instrument construct, the researchers performed confirmatory factor analysis by means of Lisrel 0.80 software and the results of this analysis showed that the evaluation instrument valid and reliable. The construct validity was between 0.43-0.79 while the reliability of measurement model was between 0.88-0.94. Last but not the least, the model feasibility test showed that the theoretical model had been supported by the empirical data.

  19. Synthesis, antibacterial activity, and biological evaluation of formyl hydroxyamino derivatives as novel potent peptide deformylase inhibitors against drug-resistant bacteria.

    Science.gov (United States)

    Yang, Shouning; Shi, Wei; Xing, Dong; Zhao, Zheng; Lv, Fengping; Yang, Liping; Yang, Yushe; Hu, Wenhao

    2014-10-30

    Peptide deformylase (PDF) has been identified as a promising target for novel antibacterial agents. In this study, a series of novel formyl hydroxyamino derivatives were designed and synthesized as PDF inhibitors and their antibacterial activities were evaluated. Among the potent PDF inhibitors (1o, 1q, 1o', 1q', and 1x), in vivo studies showed that compound 1q possesses mild toxicity, a good pharmacokinetic profile and protective effects. The good in vivo efficacy and low toxicity suggest that this class of compounds has potential for development and use in future antibacterial drugs. Copyright © 2014 Elsevier Masson SAS. All rights reserved.

  20. Biological Activities of Royal Jelly - Review

    Directory of Open Access Journals (Sweden)

    Crenguţa I. Pavel

    2011-10-01

    Full Text Available Royal jelly is a secretion product of the cephalic glands of nurse bees that has been used for centuries for itsextraordinary properties and health effects. This bibliographic study aims to review many of the scientific findingsand research that prove many of the remarkable various actions, effects and some uses of royal jelly. There are takeninto consideration numerous biological properties and effects of royal jelly: antioxidant, neurotrophic, hipoglicemiant, hipocholesterolemiant and hepatoprotective, hypotensive and blood pressure regulatory, antitumor, antibiotic, anti-inflammatory, immunomodulatory and anti-allergic, general tonic and antiaging. Royal jelly is one ofthe most studied bee products, but there still remains much to reveal about its biochemistry and biological activity infuture research for our health and life benefit.

  1. Synthesis, biological evaluation, and structure-activity relationships of potent noncovalent and nonpeptidic cruzain inhibitors as anti-Trypanosoma cruzi agents.

    Science.gov (United States)

    Ferreira, Rafaela S; Dessoy, Marco A; Pauli, Ivani; Souza, Mariana L; Krogh, Renata; Sales, Ana I L; Oliva, Glaucius; Dias, Luiz C; Andricopulo, Adriano D

    2014-03-27

    The development of cruzain inhibitors has been driven by the urgent need to develop novel and more effective drugs for the treatment of Chagas' disease. Herein, we report the lead optimization of a class of noncovalent cruzain inhibitors, starting from an inhibitor previously cocrystallized with the enzyme (K(i) = 0.8 μM). With the goal of achieving a better understanding of the structure-activity relationships, we have synthesized and evaluated a series of over 40 analogues, leading to the development of a very promising competitive inhibitor (8r, IC50 = 200 nM, K(i) = 82 nM). Investigation of the in vitro trypanocidal activity and preliminary cytotoxicity revealed the potential of the most potent cruzain inhibitors in guiding further medicinal chemistry efforts to develop drug candidates for Chagas' disease.

  2. Fluid dynamics in biological active nematics

    Science.gov (United States)

    Tan, Amanda; Hirst, Linda

    We use biological materials to form a self-mixing active system that consists of microtubules driven by kinesin clusters. Microtubules are rigid biopolymers that are a part of the cytoskeleton. Kinesin motors are molecular motors that walk along microtubules to transport cellular cargo. In this system, microtubules are bundled together, and as the kinesin clusters walk along the filaments, the microtubule bundles move relative to each other. As microtubules shear against each other, they extend, bend, buckle and fracture. When confined in a 2D water-oil interface, the system becomes an active nematic that self-mixes due to the buckling and fracturing. To quantify this self-mixing, we attached beads to the microtubules, and tracked their motion. We quantify the quality of mixing using the bead trajectories. This new active material has potential applications as a self-mixing solvent. CCBM NSF-CREST, UC Merced Health Science Research Institute.

  3. Biological activities of Curcuma longa L.

    Directory of Open Access Journals (Sweden)

    Araújo CAC

    2001-01-01

    Full Text Available There are several data in the literature indicating a great variety of pharmacological activities of Curcuma longa L. (Zingiberaceae, which exhibit anti-inflammatory, anti-human immunodeficiency virus, anti-bacteria, antioxidant effects and nematocidal activities. Curcumin is a major component in Curcuma longa L., being responsible for its biological actions. Other extracts of this plant has been showing potency too. In vitro, curcumin exhibits anti-parasitic, antispasmodic, anti-inflammatory and gastrointestinal effects; and also inhibits carcinogenesis and cancer growth. In vivo, there are experiments showing the anti-parasitic, anti-inflammatory potency of curcumin and extracts of C. longa L. by parenteral and oral application in animal models. In this present work we make an overview of the pharmacological activities of C. longa L., showing its importance.

  4. Synthesis, biological evaluation, docking study and ulcerogenicity profiling of some novel quinoline-2-carboxamides as dual COXs/LOX inhibitors endowed with anti-inflammatory activity.

    Science.gov (United States)

    Abdelrahman, Mostafa H; Youssif, Bahaa G M; Abdelgawad, Mohamed A; Abdelazeem, Ahmed H; Ibrahim, Hussein M; Moustafa, Abd El Ghany A; Treamblu, Laurent; Bukhari, Syed Nasir Abbas

    2017-02-15

    A series of novel quinoline-2-carboxamides 15-28 was synthesized and evaluated in vitro as dual COXs/LOX inhibitors. Compounds 19 and 27 exhibited the highest potency and selectivity for COX-2 inhibitory activity (IC 50  = 1.21 and 1.13 μM, respectively; selectivity index (COX-1/COX-2) = 6.52 and 7.61, respectively) in comparison to the reference drug celecoxib (COX-2 IC 50  = 0.88 μM; selectivity index (COX-1/COX-2) = 8.31). The anti-inflammatory activity of the newly synthesized compounds was further assessed in vivo using carrageenan induced paw edema assay. Interestingly, the in vitro results of COXs inhibitory assay were consistent with that of the in vivo assay where compounds 19 and 27 showed the highest anti-inflammatory activity with edema inhibition percentages of 59.38% and 65.03%, respectively compared to celecoxib (71.21%) after 5 h. Moreover, it was found that compounds 19 and 27 have a superior gastric safety profile comparable to indomethacin. The molecular docking study of compounds 19 and 27 into COX-2 active site suggested that these hits assumed binding pattern and interactions similar to that of bromocelecoxib (S-58) as a cocrystallized ligand explaining their remarkable COX-2 inhibitory activity and selectivity. Taken together, these results indicated that these derivatives are good leads for subsequent development into potential anti-inflammatory agents with least gastric damage. Copyright © 2016 Elsevier Masson SAS. All rights reserved.

  5. Design and optimization of N-acylhydrazone pyrimidine derivatives as E. coli PDHc E1 inhibitors: Structure-activity relationship analysis, biological evaluation and molecular docking study.

    Science.gov (United States)

    He, Haifeng; Xia, Hongying; Xia, Qin; Ren, Yanliang; He, Hongwu

    2017-10-15

    By targeting the thiamin diphosphate (ThDP) binding site of Escherichia coli (E. coli) pyruvate dehydrogenase multienzyme complex E1 (PDHc E1), a series of novel 'open-chain' classes of ThDP analogs A, B, and C with N-acylhydrazone moieties was designed and synthesized to explore their activities against E. coli PHDc E1 in vitro and their inhibitory activity against microbial diseases were further evaluated in vivo. As a result, A1-23 exhibited moderate to potent inhibitory activities against E. coli PDHc E1 (IC 50 =0.15-23.55μM). The potent inhibitors A13, A14, A15, C2, had strong inhibitory activities with IC 50 values of 0.60, 0.15, 0.39 and 0.34μM against E. coli PDHc E1 and with good enzyme-selective inhibition between microorganisms and mammals. Especially, the most powerful inhibitor A14 could 99.37% control Xanthimonas oryzae pv. Oryzae. Furthermore, the binding features of compound A14 within E. coli PDHc E1 were investigated to provide useful insights for the further construction of new inhibitor by molecular docking, site-directed mutagenesis, and enzymatic assays. The results indicated that A14 had most powerful inhibition against E. coli PDHc E1 due to the establishment of stronger interaction with Glu571, Met194, Glu522, Leu264 and Phe602 at active site of E.coli PDHc E1. It could be used as a lead compound for further optimization, and may have potential as a new microbicide. Copyright © 2017 Elsevier Ltd. All rights reserved.

  6. Polysulfides as biologically active ingredients of garlic.

    Science.gov (United States)

    Münchberg, Ute; Anwar, Awais; Mecklenburg, Susanne; Jacob, Claus

    2007-05-21

    Garlic has long been considered as a natural remedy against a range of human illnesses, including various bacterial, viral and fungal infections. This kind of antibiotic activity of garlic has mostly been associated with the thiosulfinate allicin. Even so, recent studies have pointed towards a significant biological activity of trisulfides and tetrasulfides found in various Allium species, including a wide range of antibiotic properties and the ability of polysulfides to cause the death of certain cancer cells. The chemistry underlying the biological activity of these polysulfides is currently emerging. It seems to include a combination of several distinct transformations, such as oxidation reactions, superoxide radical and peroxide generation, decomposition with release of highly electrophilic S(x) species, inhibition of metalloenzymes, disturbance of metal homeostasis and membrane integrity and interference with different cellular signalling pathways. Further research in this area is required to provide a better understanding of polysulfide reactions within a biochemical context. This knowledge may ultimately form the basis for the development of 'green' antibiotics, fungicides and possibly anticancer agents with dramatically reduced side effects in humans.

  7. Structural optimization and evaluation of butenolides as potent antifouling agents: modification of the side chain affects the biological activities of compounds

    KAUST Repository

    Li, Yongxin

    2012-09-01

    A recent global ban on the use of organotin compounds as antifouling agents has increased the need for safe and effective antifouling compounds. In this study, a series of new butenolide derivatives with various amine side chains was synthesized and evaluated for their anti-larval settlement activities in the barnacle, Balanus amphitrite. Side chain modification of butenolide resulted in butenolides 3c-3d, which possessed desirable physico-chemical properties and demonstrated highly effective non-toxic anti-larval settlement efficacy. A structure-activity relationship analysis revealed that varying the alkyl side chain had a notable effect on anti-larval settlement activity and that seven to eight carbon alkyl side chains with a tert-butyloxycarbonyl (Boc) substituent on an amine terminal were optimal in terms of bioactivity. Analysis of the physico-chemical profile of butenolide analogues indicated that lipophilicity is a very important physico-chemical parameter contributing to bioactivity. © 2012 Copyright Taylor and Francis Group, LLC.

  8. Phytochemical analysis and in vitro evaluation of the biological activity against herpes simplex virus type 1 (HSV-1) of Cedrus libani A. Rich.

    Science.gov (United States)

    Loizzo, Monica Rosa; Saab, Antoine; Tundis, Rosa; Statti, Giancarlo A; Lampronti, Ilaria; Menichini, Francesco; Gambari, Roberto; Cinatl, Jindrich; Doerr, Hans Wilhelm

    2008-01-01

    Cedrus libani are widely used as traditional medicine in Lebanon for treatment of different infection diseases. In the present study we reported the phytochemical composition analyzed by GC-MS of wood essential oil and cones and leaves ethanol extracts. The main components of wood essential oil were himachalol (22.50%), beta-himachalene (21.90%), and alpha-himachalene (10.50%). Leaves ethanol extract was characterized by a high content of germacrene d (29.40%). The same extract obtained from cones essentially contained alpha-pinene (51.0%) and beta-myrcene (13.0%). Moreover, we investigated extracts, essential oil, and identified compounds for their in vitro antiviral activities against herpes simplex virus type 1 (HSV-1). Cytotoxicity was evaluated by MTT assay in Vero cells. Cones and leaves ethanol extracts exhibited an interesting activity with IC50 of 0.50 and 0.66 mg/ml, respectively, at non-cytotoxic concentration. A comparable activity was found when essential oil was tested (IC50 of 0.44 mg/ml).

  9. Biological Activities of Polyphenols from Grapes

    Directory of Open Access Journals (Sweden)

    Hua-Bin Li

    2010-02-01

    Full Text Available The dietary consumption of grape and its products is associated with a lower incidence of degenerative diseases such as cardiovascular disease and certain types of cancers. Most recent interest has focused on the bioactive phenolic compounds in grape. Anthocyanins, flavanols, flavonols and resveratrol are the most important grape polyphenols because they possess many biological activities, such as antioxidant, cardioprotective, anticancer, anti-inflammation, antiaging and antimicrobial properties. This review summarizes current knowledge on the bioactivities of grape phenolics. The extraction, isolation and identification methods of polyphenols from grape as well as their bioavailability and potential toxicity also are included.

  10. Biological Activities of Polyphenols from Grapes

    Science.gov (United States)

    Xia, En-Qin; Deng, Gui-Fang; Guo, Ya-Jun; Li, Hua-Bin

    2010-01-01

    The dietary consumption of grape and its products is associated with a lower incidence of degenerative diseases such as cardiovascular disease and certain types of cancers. Most recent interest has focused on the bioactive phenolic compounds in grape. Anthocyanins, flavanols, flavonols and resveratrol are the most important grape polyphenols because they possess many biological activities, such as antioxidant, cardioprotective, anticancer, anti-inflammation, antiaging and antimicrobial properties. This review summarizes current knowledge on the bioactivities of grape phenolics. The extraction, isolation and identification methods of polyphenols from grape as well as their bioavailability and potential toxicity also are included. PMID:20386657

  11. Urine: Waste product or biologically active tissue?

    Science.gov (United States)

    2018-03-01

    Historically, urine has been viewed primarily as a waste product with little biological role in the overall health of an individual. Increasingly, data suggest that urine plays a role in human health beyond waste excretion. For example, urine might act as an irritant and contribute to symptoms through interaction with-and potential compromise of-the urothelium. To explore the concept that urine may be a vehicle for agents with potential or occult bioactivity and to discuss existing evidence and novel research questions that may yield insight into such a role, the National Institute of Diabetes and Digestive and Kidney Disease invited experts in the fields of comparative evolutionary physiology, basic science, nephrology, urology, pediatrics, metabolomics, and proteomics (among others) to a Urinology Think Tank meeting on February 9, 2015. This report reflects ideas that evolved from this meeting and current literature, including the concept of urine quality, the biological, chemical, and physical characteristics of urine, including the microbiota, cells, exosomes, pH, metabolites, proteins, and specific gravity (among others). Additionally, the manuscript presents speculative, and hopefully testable, ideas about the functional roles of urine constituents in health and disease. Moving forward, there are several questions that need further understanding and pursuit. There were suggestions to consider actively using various animal models and their biological specimens to elaborate on basic mechanistic information regarding human bladder dysfunction. Published 2018. This article is a U.S. Government work and is in the public domain in the USA.

  12. Reconstructing Causal Biological Networks through Active Learning.

    Directory of Open Access Journals (Sweden)

    Hyunghoon Cho

    Full Text Available Reverse-engineering of biological networks is a central problem in systems biology. The use of intervention data, such as gene knockouts or knockdowns, is typically used for teasing apart causal relationships among genes. Under time or resource constraints, one needs to carefully choose which intervention experiments to carry out. Previous approaches for selecting most informative interventions have largely been focused on discrete Bayesian networks. However, continuous Bayesian networks are of great practical interest, especially in the study of complex biological systems and their quantitative properties. In this work, we present an efficient, information-theoretic active learning algorithm for Gaussian Bayesian networks (GBNs, which serve as important models for gene regulatory networks. In addition to providing linear-algebraic insights unique to GBNs, leading to significant runtime improvements, we demonstrate the effectiveness of our method on data simulated with GBNs and the DREAM4 network inference challenge data sets. Our method generally leads to faster recovery of underlying network structure and faster convergence to final distribution of confidence scores over candidate graph structures using the full data, in comparison to random selection of intervention experiments.

  13. Biological activities of Croton palanostigma Klotzsch.

    Science.gov (United States)

    Mota, Eduardo Ferreira; Rosario, Diele Magno; Silva Veiga, Andreza Socorro; Barros Brasil, Davi Do Socorro; Silveira, Fernando Tobias; Dolabela, Maria Fâni

    2016-01-01

    Different species of Croton are used in traditional Amazonian medicine. Among the popular uses are treatment of bacterial diseases, poorly healing wounds and fevers. This study evaluated the antileishmanial, antiplasmodial and antimicrobial activities of the extracts and diterpenes of Croton palanostigma Klotzsch (Euphorbiaceae). Leaves and bark were extracted with dichloromethane and methanol. The bark dichloromethane extract (BDE) was chromatographed on a column, obtaining cordatin and aparisthman. The extracts and diterpenes were assayed thought agar disk diffusion method and their bactericidal or fungicidal effects were evaluated by minimum bactericidal or fungicidal concentration. The antiplasmodial activity was evaluated after 24 and 72 h of exposition. The antileishmanial activity was performed on promastigotes forms of Leishmania amazonensis. The bark methanol extract (BME) and cordatin were not active against any microbial strains tested; BDE and leaves methanol extract (LME) were positive for Pseudomonas aeruginosa and aparisthman was positive for Candida albicans. In the determination of the minimum bactericidal concentration, neither of them were active in the highest concentration tested. The extracts and diterpenes were inactive in Plasmodium falciparum, except the LME in 72 h. Any extract was shown to be active in promastigote forms of L. amazonensis. These results indicate that the BDE and LME did not inhibit the bacterial growth, then they probably had bacteriostatic effect. LME presented activity in P. falciparum.

  14. Biologically Active Secondary Metabolites from the Fungi.

    Science.gov (United States)

    Bills, Gerald F; Gloer, James B

    2016-11-01

    Many Fungi have a well-developed secondary metabolism. The diversity of fungal species and the diversification of biosynthetic gene clusters underscores a nearly limitless potential for metabolic variation and an untapped resource for drug discovery and synthetic biology. Much of the ecological success of the filamentous fungi in colonizing the planet is owed to their ability to deploy their secondary metabolites in concert with their penetrative and absorptive mode of life. Fungal secondary metabolites exhibit biological activities that have been developed into life-saving medicines and agrochemicals. Toxic metabolites, known as mycotoxins, contaminate human and livestock food and indoor environments. Secondary metabolites are determinants of fungal diseases of humans, animals, and plants. Secondary metabolites exhibit a staggering variation in chemical structures and biological activities, yet their biosynthetic pathways share a number of key characteristics. The genes encoding cooperative steps of a biosynthetic pathway tend to be located contiguously on the chromosome in coregulated gene clusters. Advances in genome sequencing, computational tools, and analytical chemistry are enabling the rapid connection of gene clusters with their metabolic products. At least three fungal drug precursors, penicillin K and V, mycophenolic acid, and pleuromutilin, have been produced by synthetic reconstruction and expression of respective gene clusters in heterologous hosts. This review summarizes general aspects of fungal secondary metabolism and recent developments in our understanding of how and why fungi make secondary metabolites, how these molecules are produced, and how their biosynthetic genes are distributed across the Fungi. The breadth of fungal secondary metabolite diversity is highlighted by recent information on the biosynthesis of important fungus-derived metabolites that have contributed to human health and agriculture and that have negatively impacted crops

  15. Biologically Active Metabolites Synthesized by Microalgae

    Directory of Open Access Journals (Sweden)

    Michele Greque de Morais

    2015-01-01

    Full Text Available Microalgae are microorganisms that have different morphological, physiological, and genetic traits that confer the ability to produce different biologically active metabolites. Microalgal biotechnology has become a subject of study for various fields, due to the varied bioproducts that can be obtained from these microorganisms. When microalgal cultivation processes are better understood, microalgae can become an environmentally friendly and economically viable source of compounds of interest, because production can be optimized in a controlled culture. The bioactive compounds derived from microalgae have anti-inflammatory, antimicrobial, and antioxidant activities, among others. Furthermore, these microorganisms have the ability to promote health and reduce the risk of the development of degenerative diseases. In this context, the aim of this review is to discuss bioactive metabolites produced by microalgae for possible applications in the life sciences.

  16. Biologically Active Metabolites Synthesized by Microalgae.

    Science.gov (United States)

    de Morais, Michele Greque; Vaz, Bruna da Silva; de Morais, Etiele Greque; Costa, Jorge Alberto Vieira

    2015-01-01

    Microalgae are microorganisms that have different morphological, physiological, and genetic traits that confer the ability to produce different biologically active metabolites. Microalgal biotechnology has become a subject of study for various fields, due to the varied bioproducts that can be obtained from these microorganisms. When microalgal cultivation processes are better understood, microalgae can become an environmentally friendly and economically viable source of compounds of interest, because production can be optimized in a controlled culture. The bioactive compounds derived from microalgae have anti-inflammatory, antimicrobial, and antioxidant activities, among others. Furthermore, these microorganisms have the ability to promote health and reduce the risk of the development of degenerative diseases. In this context, the aim of this review is to discuss bioactive metabolites produced by microalgae for possible applications in the life sciences.

  17. Biologically Active Metabolites Synthesized by Microalgae

    Science.gov (United States)

    Costa, Jorge Alberto Vieira

    2015-01-01

    Microalgae are microorganisms that have different morphological, physiological, and genetic traits that confer the ability to produce different biologically active metabolites. Microalgal biotechnology has become a subject of study for various fields, due to the varied bioproducts that can be obtained from these microorganisms. When microalgal cultivation processes are better understood, microalgae can become an environmentally friendly and economically viable source of compounds of interest, because production can be optimized in a controlled culture. The bioactive compounds derived from microalgae have anti-inflammatory, antimicrobial, and antioxidant activities, among others. Furthermore, these microorganisms have the ability to promote health and reduce the risk of the development of degenerative diseases. In this context, the aim of this review is to discuss bioactive metabolites produced by microalgae for possible applications in the life sciences. PMID:26339647

  18. Biological activity screening of seven Plectranthus species

    Directory of Open Access Journals (Sweden)

    Epole Ntungwe N

    2017-07-01

    Full Text Available Natural products from Plectranthus spp. plants have an ethnopharmacological use, inspiring several scientific investigations. As such, this work aims to perform a biological activity screening in order to scientifically validate the use of these plants. Assays on in vitro acetylcholinesterase (AChE inhibition, antioxidant effects, antimicrobial activity and Artemia salina lethality were performed on seven Plectranthus spp. extracts (P. swynnertonii, P. welwischii, P. woodii, P. cylindraceus, P. spicatus, P. ramosior and P. petiolaris. Acetonic extracts were obtained by sonication (10% w/v, where P. ramosior had the highest yield of dry extract (13.49% w/w. In the AChE inhibition assay, only P. cylindraceus extract decreased enzymatic activity (30.2 ± 3.78%. The antimicrobial activity was screened using the well diffusion method, against Gram positive and negative bacteria and yeast. P. ramosior extract showed not only an inhibition zone against S. aureus and C. albicans (15 and 11 mm, respectively, but also the highest scavenging activity (DPPH method, 36.4 ± 0.04%. On the lethality test in A. salina, P. swynnertonnii extract was the most toxic (LC50 = 0.036 mg/L. These preliminary results showed that P. cylindraceus, P. ramosior and P. swynnertonnii are potential bioactive extracts for further isolation and antimicrobial and cytotoxic studies.

  19. Evaluation of Teachers' Activities in the Use of Animated Instructional Resource Materials in Biology Teaching in Senior Secondary Schools in Bauchi State Nigeria

    Science.gov (United States)

    Kwasu, I. A.; Abubakar; Ema, E.

    2015-01-01

    This paper presents a profile on how teachers in senior secondary schools in Bauchi state Nigeria utilise animated instructional resource (AIR) in the teaching of biology. A structured questionnaire used to generate data on the availability, accessibility and application of the AIR for classroom instruction by teachers. The instrument for data…

  20. NBS activities in biological reference materials

    Energy Technology Data Exchange (ETDEWEB)

    Rasberry, S.D.

    1988-12-01

    NBS activities in biological reference materials during 1986-1988 are described with a preview of plans for future certifications of reference materials. During the period, work has been completed or partially completed on about 40 reference materials of importance to health, nutrition, and environmental quality. Some of the reference materials that have been completed during the period and are described include: creatinine (SRM 914a), bovine serum albumin (SRM 927a), cholesterol in human serum (SRM's 1951-1952), aspartate aminotransferase (RM 8430), cholesterol and fat-soluble vitamins in coconut oil (SRM 1563), wheat flour (SRM 1567a), rice flour (SRM 1568a), mixed diet (RM 8431a), dinitropyrene isomers and 1-nitropyrene (SRM 1596), and complex PAH's from coal tar (SRM 1597). Oyster tissue (SRM 1566a) is being analyzed and should be available in 1988.

  1. Biologically Active and Antimicrobial Peptides from Plants

    Directory of Open Access Journals (Sweden)

    Carlos E. Salas

    2015-01-01

    Full Text Available Bioactive peptides are part of an innate response elicited by most living forms. In plants, they are produced ubiquitously in roots, seeds, flowers, stems, and leaves, highlighting their physiological importance. While most of the bioactive peptides produced in plants possess microbicide properties, there is evidence that they are also involved in cellular signaling. Structurally, there is an overall similarity when comparing them with those derived from animal or insect sources. The biological action of bioactive peptides initiates with the binding to the target membrane followed in most cases by membrane permeabilization and rupture. Here we present an overview of what is currently known about bioactive peptides from plants, focusing on their antimicrobial activity and their role in the plant signaling network and offering perspectives on their potential application.

  2. ACTIVE AND PARTICIPATORY METHODS IN BIOLOGY: MODELING

    Directory of Open Access Journals (Sweden)

    Brînduşa-Antonela SBÎRCEA

    2011-01-01

    Full Text Available By using active and participatory methods it is hoped that pupils will not only come to a deeper understanding of the issues involved, but also that their motivation will be heightened. Pupil involvement in their learning is essential. Moreover, by using a variety of teaching techniques, we can help students make sense of the world in different ways, increasing the likelihood that they will develop a conceptual understanding. The teacher must be a good facilitator, monitoring and supporting group dynamics. Modeling is an instructional strategy in which the teacher demonstrates a new concept or approach to learning and pupils learn by observing. In the teaching of biology the didactic materials are fundamental tools in the teaching-learning process. Reading about scientific concepts or having a teacher explain them is not enough. Research has shown that modeling can be used across disciplines and in all grade and ability level classrooms. Using this type of instruction, teachers encourage learning.

  3. Novel Carbonyl Analogs of Tamoxifen: Design, Synthesis, and Biological Evaluation

    Directory of Open Access Journals (Sweden)

    Konstantinos M. Kasiotis

    2017-09-01

    Full Text Available Aim of this work was to provide tamoxifen analogs with enhanced estrogen receptor (ER binding affinity. Hence, several derivatives were prepared using an efficient triarylethylenes synthetic protocol. The novel compounds bioactivity was evaluated through the determination of their receptor binding affinity and their agonist/antagonist activity against breast cancer tissue using a MCF-7 cell-based assay. Phenyl esters 6a,b and 8a,b exhibited binding affinity to both ERα and ERβ higher than 4-hydroxytamoxifen while compounds 13 and 14 have shown cellular antiestrogenic activity similar to 4-hydroxytamoxifen and the known ER inhibitor ICI182,780. Theoretical calculations and molecular modeling were applied to investigate, support and explain the biological profile of the new compounds. The relevant data indicated an agreement between calculations and demonstrated biological activity allowing to extract useful structure-activity relationships. Results herein underline that modifications of tamoxifen structure still provide molecules with substantial activity, as portrayed in the inhibition of MCF-7 cells proliferation.

  4. Novel Carbonyl Analogues of Tamoxifen: Design, Synthesis, and Biological Evaluation

    Science.gov (United States)

    Kasiotis, Konstantinos M.; Lambrinidis, George; Fokialakis, Nikolas; Tzanetou, Evangelia N.; Mikros, Emmanuel; Haroutounian, Serkos A.

    2017-09-01

    Aim of this work was to provide tamoxifen analogues with enhanced estrogen receptor binding affinity. Hence, several derivatives were prepared using an efficient triarylethylenes synthetic protocol. The novel compounds bioactivity was evaluated through the determination of their receptor binding affinity and their agonist/antagonist activity against breast cancer tissue using a MCF-7 cell-based assay. Phenyl esters 6a,b and 8a,b exhibited binding affinity to both ERα and ERβ higher than 4-hydroxytamoxifen while compounds 13 and 14 have shown cellular antiestrogenic activity similar to 4-hydroxytamoxifen and the known estrogen receptor inhibitor ICI182,780. Theoretical calculations and molecular modelling were applied to investigate, support and explain the biological profile of the new compounds. The relevant data indicated an agreement between calculations and demonstrated biological activity allowing to extract useful structure-activity relationships. Results herein underline that modifications of tamoxifen structure still provide molecules with substantial activity, as portrayed in the inhibition of MCF-7 cells proliferation.

  5. Design, Synthesis, and Biological Evaluation of PKD Inhibitors

    Directory of Open Access Journals (Sweden)

    Marie-Céline Frantz

    2011-04-01

    Full Text Available Protein kinase D (PKD belongs to a family of serine/threonine kinases that play an important role in basic cellular processes and are implicated in the pathogenesis of several diseases. Progress in our understanding of the biological functions of PKD has been limited due to the lack of a PKD-specific inhibitor. The benzoxoloazepinolone CID755673 was recently reported as the first potent and kinase-selective inhibitor for this enzyme. For structure-activity analysis purposes, a series of analogs was prepared and their in vitro inhibitory potency evaluated.

  6. Isolation and biological evaluation of jatrophane diterpenoids from Euphorbia dendroides.

    Science.gov (United States)

    Aljancić, Ivana S; Pesić, Milica; Milosavljević, Slobodan M; Todorović, Nina M; Jadranin, Milka; Milosavljević, Goran; Povrenović, Dragan; Banković, Jasna; Tanić, Nikola; Marković, Ivanka D; Ruzdijić, Sabera; Vajs, Vlatka E; Tesević, Vele V

    2011-07-22

    From the Montenegrin spurge Euphorbia dendroides, seven new diterpenoids [jatrophanes (1-6) and a tigliane (7)] were isolated and their structures elucidated by spectroscopic techniques. The biological activity of the new compounds was studied against four human cancer cell lines. The most effective jatrophane-type compound (2) and its structurally closely related derivative (1) were evaluated for their interactions with paclitaxel and doxorubicin using a multi-drug-resistant cancer cell line. Both compounds exerted a strong reversal potential resulting from inhibition of P-glycoprotein transport.

  7. Center for Biologics Evaluation and Research (CBER)

    Data.gov (United States)

    Federal Laboratory Consortium — CBER is the Center within FDA that regulates biological products for human use under applicable federal laws, including the Public Health Service Act and the Federal...

  8. Synthesis, crystal structure and biological activity of novel diester cyclophanes

    Energy Technology Data Exchange (ETDEWEB)

    Zhang, Pengfei; Yang, Bingqin; Fang, Xianwen; Cheng, Zhao; Yang, Meipan, E-mail: yangbq@nwu.edu.cn [Department of Chemistry, Key Laboratory of Synthetic and Natural Functional Molecule Chemistry, Northwest University, Shaanxi (China)

    2012-10-15

    A series of novel diester cyclophanes was synthesized by esterification of 1,2-benzenedicarbonyl chloride with eight different diols under high dilution conditions. The structures of the compounds were verified by elemental analysis, {sup 1}H nuclear magnetic resonance (NMR), IR spectroscopy and high resolution mass spectrometry (HRMS). The crystal structures of two compounds were characterized by single crystal X-ray diffractometry (XRD). All the new cyclophanes were evaluated for biological activities and the results showed that some of these compounds have low antibacterial or antifungal activities (author)

  9. Biological activities and medicinal properties of Gokhru (Pedalium murex L.).

    Science.gov (United States)

    Rajashekar, V; Rao, E Upender; P, Srinivas

    2012-07-01

    Bada Gokhru (Pedalium murex L.) is perhaps the most useful traditional medicinal plant in India. Each part of the neem tree has some medicinal property and is thus commercially exploitable. During the last five decades, apart from the chemistry of the Pedalium murex compounds, considerable progress has been achieved regarding the biological activity and medicinal applications of this plant. It is now considered as a valuable source of unique natural products for development of medicines against various diseases and also for the development of industrial products. This review gives a bird's eye view mainly on the biological activities of some of this compounds isolated, pharmacological actions of the extracts, clinical studies and plausible medicinal applications of gokharu along with their safety evaluation.

  10. Synthesis and Biological Evaluation of Isomeric Methoxy Substitutions on Anti-Cancer Indolyl-Pyridinyl-Propenones: Effects on Potency and Mode of Activity

    OpenAIRE

    Trabbic, Christopher J.; George, Sage M.; Alexander, Evan M.; Du, Shengnan; Offenbacher, Jennifer M.; Crissman, Emily J.; Overmeyer, Jean H.; Maltese, William A.; Erhardt, Paul W.

    2016-01-01

    Certain indolyl-pyridinyl-propenone analogues kill glioblastoma cells that have become resistant to conventional therapeutic drugs. Some of these analogues induce a novel form of non-apoptotic cell death called methuosis, while others primarily cause microtubule disruption. Ready access to 5-indole substitution has allowed characterization of this position to be important for both types of mechanisms when a simple methoxy group is present. We now report the syntheses and biological effects of...

  11. Biological activity and photostability of biflorin micellar nanostructures.

    Science.gov (United States)

    Santana, Edson R B; Ferreira-Neto, João P; Yara, Ricardo; Sena, Kêsia X F R; Fontes, Adriana; Lima, Cláudia S A

    2015-05-13

    Capraria biflora L. is a shrub from the Scrophulariaceae family which produces in its roots a compound named biflorin, an o-naphthoquinone that shows activity against Gram-positive bacteria and fungi and also presents antitumor and antimetastatic activities. However, biflorin is hydrophobic and photosensitive. These properties make its application difficult. In this work we prepared biflorin micellar nanostructures looking for a more effective vehiculation and better preservation of the biological activity. Biflorin was obtained, purified and characterized by UV-Vis, infrared (IR) and 1H- and 13C-NMR. Micellar nanostructures of biflorin were then assembled with Tween 80®, Tween 20® and saline (0.9%) and characterized by UV-Vis spectroscopy and dynamic light scattering (DLS). The results showed that the micellar nanostructures were stable and presented an average size of 8.3 nm. Biflorin micellar nanostructures' photodegradation was evaluated in comparison with biflorin in ethanol. Results showed that the biflorin in micellar nanostructures was better protected from light than biflorin dissolved in ethanol, and also indicated that biflorin in micelles were efficient against Gram-positive bacteria and yeast species. In conclusion, the results showed that the micellar nanostructures could ensure the maintenance of the biological activity of biflorin, conferring photoprotection. Moreover, biflorin vehiculation in aqueous media was improved, favoring its applicability in biological systems.

  12. Biological Activity and Photostability of Biflorin Micellar Nanostructures

    Directory of Open Access Journals (Sweden)

    Edson R. B. Santana

    2015-05-01

    Full Text Available Capraria biflora L. is a shrub from the Scrophulariaceae family which produces in its roots a compound named biflorin, an o-naphthoquinone that shows activity against Gram-positive bacteria and fungi and also presents antitumor and antimetastatic activities. However, biflorin is hydrophobic and photosensitive. These properties make its application difficult. In this work we prepared biflorin micellar nanostructures looking for a more effective vehiculation and better preservation of the biological activity. Biflorin was obtained, purified and characterized by UV-Vis, infrared (IR and 1H- and 13C-NMR. Micellar nanostructures of biflorin were then assembled with Tween 80®, Tween 20® and saline (0.9% and characterized by UV-Vis spectroscopy and dynamic light scattering (DLS. The results showed that the micellar nanostructures were stable and presented an average size of 8.3 nm. Biflorin micellar nanostructures’ photodegradation was evaluated in comparison with biflorin in ethanol. Results showed that the biflorin in micellar nanostructures was better protected from light than biflorin dissolved in ethanol, and also indicated that biflorin in micelles were efficient against Gram-positive bacteria and yeast species. In conclusion, the results showed that the micellar nanostructures could ensure the maintenance of the biological activity of biflorin, conferring photoprotection. Moreover, biflorin vehiculation in aqueous media was improved, favoring its applicability in biological systems.

  13. BIOLOGICALLY ACTIVE SUBSTANCES OF SPIRIT PRODUCTION WASTE

    Directory of Open Access Journals (Sweden)

    A. S. Kayshev

    2014-01-01

    Full Text Available A content of biologically active compounds (BAC with signified pharmacological activity in distillers grains was proved. It is prospective for applications of these grains as a raw material resource of pharmaceuticals. A composition of BAC distillers grains received from wheat, corn, barley, millet at different spirit enterprises which use hydro fermentative grain processing. Considering polydispersity of distillers grains they were separated on solid and liquid phases preliminary. Physical and chemical characteristics of distillers grains' liquid base were identified. Elementary composition of distillers grains is signified by active accumulation of biogenic elements (phosphorus, potassium, magnesium, calcium, sodium, iron and low content of heavy metals. The solid phase of distillers grains accumulates carbon, hydrogen and nitrogen in high concentration. The liquid phase of distillers grains contains: proteins and amino acids (20-46%, reducing sugars (5,6%-17,5%, galacturonides (0,8-1,4%, ascorbic acid (6,2-11,4 mg%. The solid base of distillers grains contains: galacturonides (3,4-5,3%, fatty oil (8,4-11,1% with predomination of essential fatty acids, proteins and amino acids (2,1-2,5%, flavonoids (0,4-0,9%, tocopherols (3,4-7,7 mg%. A method of complex processing of distillers grains based on application of membrane filtering of liquid phase and liquid extraction by inorganic and organic solvents of solid phase, which allows almost full extraction of the sum of biologically active compounds (BAC from liquid phase (Biobardin BM and solid phase (Biobardin UL. Biobardin BM comprises the following elements: proteins and amino acids (41-69%, reducing sugars (3,5-15,6%, fatty oil (0,2-0,3%, flavonoids (0,2-0,7%, ascorbic acid (17-37 mg%. Biobardin UL includes: oligouronids (16,4-19,5%, proteins and amino acids (11-21%, fatty oil (3,2-4,9% which includes essential acids; flavonoids (0,6-1,5%, tocopherols (6,6-10,2 mg%, carotinoids (0,13-0,21 mg

  14. Expression of biologically active murine interleukin-18 in Lactococcus lactis.

    Science.gov (United States)

    Feizollahzadeh, Sadegh; Khanahmad, Hossein; Rahimmanesh, Ilnaz; Ganjalikhani-Hakemi, Mazdak; Andalib, Alireza; Sanei, Mohammad Hossein; Rezaei, Abbas

    2016-11-01

    The food-grade bacterium Lactococcus lactis is increasingly used for heterologous protein expression in therapeutic and industrial applications. The ability of L. lactis to secrete biologically active cytokines may be used for the generation of therapeutic cytokines. Interleukin (IL)-18 enhances the immune response, especially on mucosal surfaces, emphasizing its therapeutic potential. However, it is produced as an inactive precursor and has to be enzymatically cleaved for maturation. We genetically manipulated L. lactis to secrete murine IL-18. The mature murine IL-18 gene was inserted downstream of a nisin promoter in pNZ8149 plasmid and the construct was used to transform L. lactis NZ3900. The transformants were selected on Elliker agar and confirmed by restriction enzyme digestion and sequencing. The expression and secretion of IL-18 protein was verified by SDS-PAGE, western blotting and ELISA. The biological activity of recombinant IL-18 was determined by its ability to induce interferon (IFN)-γ production in L. lactis co-cultured with murine splenic T cells. The amounts of IL-18 in bacterial lysates and supernatants were 3-4 μg mL -1 and 0.6-0.7 ng mL -1 , respectively. The successfully generated L. lactis strain that expressed biologically active murine IL-18 can be used to evaluate the possible therapeutic effects of IL-18 on mucosal surfaces. © FEMS 2016. All rights reserved. For permissions, please e-mail: journals.permissions@oup.com.

  15. Ethnobotany, chemistry, and biological activities of the genus Tithonia (Asteraceae).

    Science.gov (United States)

    Chagas-Paula, Daniela A; Oliveira, Rejane B; Rocha, Bruno A; Da Costa, Fernando B

    2012-02-01

    The genus Tithonia is an important source of diverse natural products, particularly sesquiterpene lactones, diterpenes, and flavonoids. The collected information in this review attempts to summarize the recent developments in the ethnobotany, biological activities, and secondary metabolite chemistry of this genus. More than 100 structures of natural products from Tithonia are reported in this review. The species that has been most investigated in this genus is T. diversifolia, from which ca. 150 compounds were isolated. Biological studies are described to evaluate the anti-inflammatory, analgesic, antimalarial, antiviral, antidiabetic, antidiarrhoeal, antimicrobial, antispasmodic, vasorelaxant, cancer-chemopreventive, cytotoxic, toxicological, bioinsecticide, and repellent activities. A few of these studies have been carried out with isolated compounds from Tithonia species, but the majority has been conducted with different extracts. The relationship between the biological activity and the toxicity of compounds isolated from the plants of this genus as well as T. diversifolia extracts still remains unclear, and mechanisms of action remain to be determined. Copyright © 2012 Verlag Helvetica Chimica Acta AG, Zürich.

  16. Biologically active and biomimetic dual gelatin scaffolds for tissue engineering.

    Science.gov (United States)

    Sánchez, P; Pedraz, J L; Orive, G

    2017-05-01

    We have designed, developed and optimized Genipin cross-linked 3D gelatin scaffolds that were biologically active and biomimetic, show a dual activity both for growth factor and cell delivery. Type B gelatin powder was dissolved in DI water. 100mg of genipin was dissolved in 10ml of DI water. Three genipin concentrations were prepared: 0.1%, 0.2% and 0.3% (w/v). Solutions were mixed at 40°C and under stirring and then left crosslinking for 72h. Scaffolds were obtained by punching 8 mm-cylinders into ethanol 70% solution for 10min and then freeze-drying. Scaffolds were biologically, biomechanically and morphologically evaluated. Cell adhesion and morphology of D1-Mesenchymal stem cells (MSCs) and L-929 fibroblast was studied. Vascular endothelial grwoth factor (VEGF) and Sonic hedgehog (SHH) were used as model proteins. Swelling ratio increased and younǵs module decreased along with the concentration of genipin. All scaffolds were biocompatible according to the toxicity test. MSC and L-929 cell adhesion improved in 0.2% of genipin, obtaining better results with MSCs. VEGF and SHH were released from the gels. This preliminary study suggest that the biologically active and dual gelatin scaffolds may be used for tissue engineering approaches like bone regeneration. Copyright © 2017 Elsevier B.V. All rights reserved.

  17. Biological activity of Serratia marcescens cytotoxin

    Directory of Open Access Journals (Sweden)

    G.V. Carbonell

    2003-03-01

    Full Text Available Serratia marcescens cytotoxin was purified to homogeneity by ion-exchange chromatography on a DEAE Sepharose Fast Flow column, followed by gel filtration chromatography on a Sephadex G100 column. The molecular mass of the cytotoxin was estimated to be about 50 kDa. Some biological properties of the cytotoxin were analyzed and compared with well-characterized toxins, such as VT1, VT2 and CNF from Escherichia coli and hemolysin produced by S. marcescens. The sensitivity of the cell lines CHO, HeLa, HEp-2, Vero, BHK-21, MA 104 and J774 to the cytotoxin was determined by the cell viability assay using neutral red. CHO and HEp-2 were highly sensitive, with massive cellular death after 1 h of treatment, followed by BHK-21, HeLa, Vero and J774 cells, while MA 104 was insensitive to the toxin. Cytotoxin induced morphological changes such as cell rounding with cytoplasmic retraction and nuclear compactation which were evident 15 min after the addition of cytotoxin. The cytotoxic assays show that 15 min of treatment with the cytotoxin induced irreversible intoxication of the cells, determined by loss of cell viability. Concentrations of 2 CD50 (0.56 µg/ml of purified cytotoxin did not present any hemolytic activity, showing that the cytotoxin is distinct from S. marcescens hemolysin. Antisera prepared against S. marcescens cytotoxin did not neutralize the cytotoxic activity of VT1, VT2 or CNF toxin, indicating that these toxins do not share antigenic determinants with cytotoxin. Moreover, we did not detect gene sequences for any of these toxins in S. marcescens by PCR assay. These results suggest that S. marcescens cytotoxin is not related to any of these toxins from E. coli.

  18. Activation analysis of biological materials at the Activation Analysis Centre

    International Nuclear Information System (INIS)

    Kukula, F.; Obrusnik, I.; Simkova, M.; Kucera, J.; Krivanek, M.

    1976-01-01

    A review is presented of the work of the Activation Analysis Centre of the Nuclear Research Institute for different fields of the Czechoslovak economy, aimed primarily at analyzing biological materials with the purpose of determining the contents of the so-called vital trace elements and of elements which already have a toxic effect on the organism in trace concentrations. Another important field of research is the path of trace elements from the environment to the human organism. A destructive method for the simultaneous determination of 12 trace elements in 11 kinds of human tissue has been studied. (Z.M.)

  19. Evaluation of radiobiological effects in 3 distinct biological models

    International Nuclear Information System (INIS)

    Lemos, J.; Costa, P.; Cunha, L.; Metello, L.F.; Carvalho, A.P.; Vasconcelos, V.; Genesio, P.; Ponte, F.; Costa, P.S.; Crespo, P.

    2015-01-01

    Full text of publication follows. The present work aims at sharing the process of development of advanced biological models to study radiobiological effects. Recognizing several known limitations and difficulties of the current monolayer cellular models, as well as the increasing difficulties to use advanced biological models, our group has been developing advanced biological alternative models, namely three-dimensional cell cultures and a less explored animal model (the Zebra fish - Danio rerio - which allows the access to inter-generational data, while characterized by a great genetic homology towards the humans). These 3 models (monolayer cellular model, three-dimensional cell cultures and zebra fish) were externally irradiated with 100 mGy, 500 mGy or 1 Gy. The consequences of that irradiation were studied using cellular and molecular tests. Our previous experimental studies with 100 mGy external gamma irradiation of HepG2 monolayer cells showed a slight increase in the proliferation rate 24 h, 48 h and 72 h post irradiation. These results also pointed into the presence of certain bystander effects 72 h post irradiation, constituting the starting point for the need of a more accurate analysis realized with this work. At this stage, we continue focused on the acute biological effects. Obtained results, namely MTT and clonogenic assays for evaluating cellular metabolic activity and proliferation in the in vitro models, as well as proteomics for the evaluation of in vivo effects will be presented, discussed and explained. Several hypotheses will be presented and defended based on the facts previously demonstrated. This work aims at sharing the actual state and the results already available from this medium-term project, building the proof of the added value on applying these advanced models, while demonstrating the strongest and weakest points from all of them (so allowing the comparison between them and to base the subsequent choice for research groups starting

  20. Protease activated receptors (PARS) mediation in gyroxin biological activity

    International Nuclear Information System (INIS)

    Silva, Jose Alberto Alves da

    2009-01-01

    Gyroxin is a serine protease enzyme from the South American rattlesnake (Crotalus durissus terrificus) venom; it is only partially characterized and has multiple activities. Gyroxin induces blood coagulation, blood pressure decrease and a neurotoxic behavior named barrel rotation. The mechanisms involved in this neurotoxic activity are not known. Whereas gyroxin is a member of enzymes with high potential to become a new drug with clinical applications such as thrombin, batroxobin, ancrod, tripsyn and kalicrein, it is important to find out how gyroxin works. The analysis on agarose gel electrophoresis and circular dichroism confirmed the molecules' integrity and purity. The gyroxin intravenous administration in mice proved its neurotoxicity (barrel rotation). In vivo studies employing intravital microscopy proved that gyroxin induces vasodilation with the participation of protease activated receptors (PARs), nitric oxide and Na+K+ATPase. The leukocytes' adherence and rolling counting indicated that gyroxin has no pro inflammatory activity. Gyroxin induced platelet aggregation, which was blocked by inhibitors of PAR1 and PAR4 receptors (SCH 79797 and tcY-NH 2 , respectively). Finally, it was proved that the gyroxin temporarily alter the permeability of the blood brain barrier (BBB). Our study has shown that both the protease-activated receptors and nitric oxide are mediators involved in the biological activities of gyroxin. (author)

  1. Synthesis, characterization and biological evaluation of ...

    Indian Academy of Sciences (India)

    . Since the two heterocyclic moieties thiazole and pyrimidine constitute two active pharmacophores that are highly active against inflam- mation and pain, combining the two is expected to have a synergistic effect on their analgesic properties.

  2. Biological activity of lactoferrin-functionalized biomimetic hydroxyapatite nanocrystals.

    Science.gov (United States)

    Nocerino, Nunzia; Fulgione, Andrea; Iannaccone, Marco; Tomasetta, Laura; Ianniello, Flora; Martora, Francesca; Lelli, Marco; Roveri, Norberto; Capuano, Federico; Capparelli, Rosanna

    2014-01-01

    The emergence of bacterial strains resistant to antibiotics is a general public health problem. Progress in developing new molecules with antimicrobial properties has been made. In this study, we evaluated the biological activity of a hybrid nanocomposite composed of synthetic biomimetic hydroxyapatite surface-functionalized by lactoferrin (LF-HA). We evaluated the antimicrobial, anti-inflammatory, and antioxidant properties of LF-HA and found that the composite was active against both Gram-positive and Gram-negative bacteria, and that it modulated proinflammatory and anti-inflammatory responses and enhanced antioxidant properties as compared with LF alone. These results indicate the possibility of using LF-HA as an antimicrobial system and biomimetic hydroxyapatite as a candidate for innovative biomedical applications.

  3. New enamine derivatives of lapachol and biological activity.

    Science.gov (United States)

    Oliveira, Mailcar F; Lemos, Telma G; de Mattos, Marcos C; Segundo, Taciana A; Santiago, Gilvandete M P; Braz-Filho, Raimundo

    2002-06-01

    A convenient synthesis of the new enamine derivatives 2-(4-morpholinyl)-3-(3-methyl-2-butenyl)-1,4-naphthalenedione, 2-(1-piperidinyl)-3-(3-methyl-2-butenyl)-1,4-naphtalenedione and 2-(1-pyrrolidinyl)-3-(3-methyl-2-butenyl)-1,4-naphthalenedione was carried out from natural 2-hydroxy-3-(3-methyl-2-butenyl)-1,4-naphthalenedione (lapachol) and morpholine, piperidine and pyrrolidine. The structures of the products were established mainly by NMR analysis, including 2D experiments. Biological activities of these products were evaluated against Artemia salina, Aedes aegypti and cytotoxicity using A549 human breast cells.

  4. New enamine derivatives of lapachol and biological activity

    Directory of Open Access Journals (Sweden)

    OLIVEIRA MAILCAR F.

    2002-01-01

    Full Text Available A convenient synthesis of the new enamine derivatives 2-(4-morpholinyl-3-(3-methyl-2-butenyl-1,4-naphthalenedione, 2-(1-piperidinyl-3-(3-methyl-2-butenyl-1,4-naphtalenedione and 2-(1-pyrrolidinyl-3-(3-methyl-2-butenyl-1,4-naphthalenedione was carried out from natural 2-hydroxy-3-(3-methyl-2-butenyl-1,4-naphthalenedione (lapachol and morpholine, piperidine and pyrrolidine. The structures of the products were established mainly by NMR analysis, including 2D experiments. Biological activities of these products were evaluated against Artemia salina, Aedes aegypti and cytotoxicity using A549 human breast cells.

  5. Synthesizing a Berberine Derivative and Evaluating Antimicrobial Activity to Reinforce with Students the Potential Significance of Small Chemical Structure Changes for Biological Systems

    Science.gov (United States)

    Rodrigues, Catarina A. B.; Neto, Iris; Rijo, Patricia; Afonso, Carlos A. M.

    2018-01-01

    The convenient synthesis of dihydroberberine by the reduction of berberine is described as an experiment for an upper-division undergraduate organic chemistry laboratory course. Students obtained up to 74% yield of the desired pure product without the use of chromatographic techniques. The antimicrobial activities of both compounds against…

  6. SYNTHESIS AND BIOLOGICAL ACTIVITIES OF 3,6 ...

    African Journals Online (AJOL)

    SYNTHESIS AND BIOLOGICAL ACTIVITIES OF 3,6-DISUBSTITUTED-1,2,4-. TRIAZOLO-1,3 ... Thus, many chemists reported synthesis and antimicrobial activity of some 1,2,4-triazolothiadiazole derivatives in ..... N.H. Synthesis and biological activity of oxadiazole and triazolothiadiazole derivatives as tyrosinase inhibitors.

  7. Biological activity of lactoferrin-functionalized biomimetic hydroxyapatite nanocrystals

    Directory of Open Access Journals (Sweden)

    Nocerino N

    2014-03-01

    Full Text Available Nunzia Nocerino,1 Andrea Fulgione,1 Marco Iannaccone,1 Laura Tomasetta,1 Flora Ianniello,1 Francesca Martora,1 Marco Lelli,2 Norberto Roveri,2 Federico Capuano,3 Rosanna Capparelli1 1Department of Agriculture Special Biotechnology Center Federico II, CeBIOTEC Biotechnology, University of Naples Federico II, Naples, 2Department of Chemistry, G Ciamician, Alma Mater Studiorum, University of Bologna, Bologna, 3Department of Food Inspection IZS ME, Naples, Italy Abstract: The emergence of bacterial strains resistant to antibiotics is a general public health problem. Progress in developing new molecules with antimicrobial properties has been made. In this study, we evaluated the biological activity of a hybrid nanocomposite composed of synthetic biomimetic hydroxyapatite surface-functionalized by lactoferrin (LF-HA. We evaluated the antimicrobial, anti-inflammatory, and antioxidant properties of LF-HA and found that the composite was active against both Gram-positive and Gram-negative bacteria, and that it modulated proinflammatory and anti-inflammatory responses and enhanced antioxidant properties as compared with LF alone. These results indicate the possibility of using LF-HA as an antimicrobial system and biomimetic hydroxyapatite as a candidate for innovative biomedical applications. Keywords: lactoferrin, hydroxyapatite nanocrystals, biomimetism, biological activity, drug delivery

  8. Structure-based design, synthesis, and biological evaluation of novel pyrrolyl aryl sulfones: HIV-1 non-nucleoside reverse transcriptase inhibitors active at nanomolar concentrations.

    Science.gov (United States)

    Artico, M; Silvestri, R; Pagnozzi, E; Bruno, B; Novellino, E; Greco, G; Massa, S; Ettorre, A; Loi, A G; Scintu, F; La Colla, P

    2000-05-04

    Pyrrolyl aryl sulfones (PASs) have been recently reported as a new class of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT) inhibitors acting at the non-nucleoside binding site of this enzyme (Artico, M.; et al. J. Med. Chem. 1996, 39, 522-530). Compound 3, the most potent inhibitor within the series (EC(50) = 0.14 microM, IC(50) = 0.4 microM, and SI > 1429), was then selected as a lead compound for a synthetic project based on molecular modeling studies. Using the three-dimensional structure of RT cocrystallized with the alpha-APA derivative R95845, we derived a model of the RT/3 complex by taking into account previously developed structure-activity relationships. Inspection of this model and docking calculations on virtual compounds prompted the design of novel PAS derivatives and related analogues. Our computational approach proved to be effective in making qualitative predictions, that is in discriminating active versus inactive compounds. Among the compounds synthesized and tested, 20 was the most active one, with EC(50) = 0.045 microM, IC(50) = 0.05 microM, and SI = 5333. Compared with the lead 3, these values represent a 3- and 8-fold improvement in the cell-based and enzyme assays, respectively, together with the highest selectivity achieved so far in the PAS series.

  9. Office of Biological Informatics and Outreach geospatial technology activities

    Science.gov (United States)

    ,

    1998-01-01

    The U.S. Geological Survey (USGS) Office of Biological Informatics and Outreach (OBIO) in Reston, Virginia, and its Center for Biological Informatics (CBI) in Denver, Colorado, provide leadership in the development and use of geospatial technologies to advance the Nation's biological science activities.

  10. Biological activities of substituted trichostatic acid derivatives

    Indian Academy of Sciences (India)

    Administrator

    , although weaker zinc ligands than the hydroxamic acids, generally lead to bioactive molecules and pos- sess higher stability in biological environments. In this respect we prepared both hydroxamic acids and benzamide versions of the target ...

  11. Use of biological indicators to evaluate environmental stress

    International Nuclear Information System (INIS)

    Letourneau, C.; Castonguay, J.

    1987-09-01

    This report examines the usefulness of biological analyses for evaluating environmental stress. All forms of stress are addressed; particular attention, however, is paid to the use of biological analyses to evaluate the impact on the environment from radioactive releases of the nuclear industry. First, we will review different biological analyses which are grouped into two approaches: the holistic approach (biotic and diversity indices) and the reductionist approach ('biological indicators' per se). Secondly, we will compare the usefulness of plants and animals as indicators based on the established criteria. This report ends with a compilation of letters received from different organizations which outline the present usage in Canada of biological indicators for evaluating environmental stress

  12. Use of biological indicators for evaluating environmental stress

    International Nuclear Information System (INIS)

    Letourneau, C.; Castonguay, J.

    1988-09-01

    This report examines the usefulness of biological analyses for evaluating environmental stress. All forms of stress are addressed; particular attention, however, is paid to the use of biological analyses to evaluate the impact on the environment from radioactive releases of the nuclear industry. First, we will review different biological analyses which are grouped into two approaches: the holistic approach (biotic and diversity indices) and the reductionist approach ('biological indicators' per se). Secondly, we will compare the usefulness of plants and animals as indicators based on the established criteria. This report ends with a compilation of letters received from different organizations which outline the present use in Canada of biological indicators for evaluating environmental stress

  13. Evaluation of Biological and Enzymatic Activity of Soil in a Tropical Dry Forest: Desierto de la Tatacoa (Colombia) with Potential in Mars Terraforming and Other Similar Planets

    Science.gov (United States)

    Moreno Moreno, A. N.

    2009-12-01

    Desierto de la Tatacoa has been determined to be a tropical dry forest bioma, which is located at 3° 13" N 75° 13" W. It has a hot thermal floor with 440 msnm of altitude; it has a daily average of 28° C, and a maximum of 40° C, Its annual rainfall total can be upwards of 1250 mm. Its solar sheen has a daily average of 5.8 hours and its relative humidity is between 60% and 65%. Therefore, the life forms presents are very scant, and in certain places, almost void. It was realized a completely random sampling of soil from its surface down to 6 inches deep, of zones without vegetation and with soils highly loaded by oxides of iron in order to determine the number of microorganisms per gram and its subsequent identification. It was measured the soil basal respiration. Besides, it was determined enzymatic activity (catalase, dehydrogenase, phosphatase and urease). Starting with the obtained results, it is developes an alternative towards the study of soil genesis in Mars in particular, and recommendations for same process in other planets. Although the information found in the experiments already realized in Martian soil they demonstrate that doesnt exist any enzymatic activity, the knowledge of the same topic in the soil is proposed as an alternative to problems like carbonic fixing of the dense Martian atmosphere of CO2, the degradation of inorganic compounds amongst other in order to prepare the substratum for later colonization by some life form.

  14. Evaluation of the Redesign of an Undergraduate Cell Biology Course

    Science.gov (United States)

    McEwen, Laura April; Harris, dik; Schmid, Richard F.; Vogel, Jackie; Western, Tamara; Harrison, Paul

    2009-01-01

    This article offers a case study of the evaluation of a redesigned and redeveloped laboratory-based cell biology course. The course was a compulsory element of the biology program, but the laboratory had become outdated and was inadequately equipped. With the support of a faculty-based teaching improvement project, the teaching team redesigned the…

  15. Students' Evaluation of Classroom Interactions of Their Biology ...

    African Journals Online (AJOL)

    Nekky Umera

    Abstract. This correlational study investigated students' evaluation of their biology teachers' classroom interaction and their feelings towards biology lessons. Three research questions guided the study. Copies of a questionnaire containing 48 items were distributed to 1,216 senior secondary two students from nine ...

  16. ITS evaluations and activities.

    Science.gov (United States)

    2010-01-01

    Evaluations are critical in promoting innovative practices which may help to provide a safe and efficient transportation system. By conducting such evaluations, we develop quantifiable measures for those in policy development to appreciate and compre...

  17. Instrumental neutron activation analysis of biological samples

    International Nuclear Information System (INIS)

    Guinn, V.P.; Gavrilas, M.

    1990-01-01

    The elemental compositions of 18 biological reference materials have been processed, for 14 stepped combinations of irradiation/decay/counting times, by the INAA Advance Prediction Computer Program. The 18 materials studied include 11 plant materials, 5 animal materials, and 2 other biological materials. Of these 18 materials, 14 are NBS Standard Reference Materials and four are IAEA reference materials. Overall, the results show that a mean of 52% of the input elements can be determined to a relative standard deviation of ±10% or better by reactor flux (thermal plus epithermal) INAA

  18. Synthetic biology analysed tools for discussion and evaluation

    CERN Document Server

    2016-01-01

    Synthetic biology is a dynamic, young, ambitious, attractive, and heterogeneous scientific discipline. It is constantly developing and changing, which makes societal evaluation of this emerging new science a challenging task, prone to misunderstandings. Synthetic biology is difficult to capture, and confusion arises not only regarding which part of synthetic biology the discussion is about, but also with respect to the underlying concepts in use. This book offers a useful toolbox to approach this complex and fragmented field. It provides a biological access to the discussion using a 'layer' model that describes the connectivity of synthetic or semisynthetic organisms and cells to the realm of natural organisms derived by evolution. Instead of directly reviewing the field as a whole, firstly our book addresses the characteristic features of synthetic biology that are relevant to the societal discussion. Some of these features apply only to parts of synthetic biology, whereas others are relevant to synthetic bi...

  19. Pereskia aculeata Muller (Cactaceae Leaves: Chemical Composition and Biological Activities

    Directory of Open Access Journals (Sweden)

    Lucèia Fàtima Souza

    2016-09-01

    Full Text Available The aims of this work were to study the chemical composition of the essential oil from the leaves of Pereskia aculeata and to evaluate some biological activities of three leaf extracts. The phenolic content, antioxidant activity, and in vitro antimicrobial and antifungal activities were determined. The methanol extract showed antioxidant activity (EC50 7.09 mg/mL and high polyphenols content (15.04 ± 0.31 mg gallic acid equivalents (GAE/g. The petroleum ether extract exhibited potent antibacterial activity against Escherichia coli, whereas the chloroform extract showed inhibitory activity against Bacillus cereus and Staphylococcus aureus. The petroleum ether and methanol extracts were more effective in inhibiting the growth of Aspergillus versicolor. The possible cytotoxicity of extracts on neuroblastoma SH-SY5Y cancer cell line and the influence on adenylate cyclase (ADCY expression was also studied. P. aculeata chloroform extract showed antiproliferative activity with an IC50 value of 262.83 µg/mL. Treatments of SH-SY5Y neuroblastoma cells with 100 µg/mL of methanol extract significantly reduced ADCY1 expression.

  20. [Biological evaluation of Cuban plants VI].

    Science.gov (United States)

    Jiménez Misas, C A; Rojas Hernández, N M; López Abraham, A M

    1979-01-01

    The study of the antibacterial activity of plants growing in Cuba is pursued. Aqueous, alcoholic and ketonic extracts were prepared from five species, and it was found that the best inhibitions corresponded to the species Hamelia patens, Nephrolepis acuminata, Calocarpum sapota and Colocasia antiquorum.

  1. Dew formation and activity of biological crusts

    NARCIS (Netherlands)

    Veste, M.; Heusinkveld, B.G.; Berkowicz, S.M.; Breckle, S.W.; Littmann, T.; Jacobs, A.F.G.

    2008-01-01

    Biological soil crusts are prominent in many drylands and can be found in diverse parts of the globe including the Atacama desert, Chile, the Namib desert, Namibia, the Succulent-Karoo desert, South Africa, and the Negev desert, Israel. Because precipitation can be negligible in deserts ¿ the

  2. Biological activities of synthesized silver nanoparticles from ...

    Indian Academy of Sciences (India)

    Nanotechnology is interdisciplinary which includes physics, chemistry, biology, material science and medicine. Nanotechnology is a universal term for the creation, manip ... range of medical devices including bone cement, surgical instruments, surgical masks, etc. Synthesis of noble metal na- noparticles, in particular, silver ...

  3. Biological activities of radiation-degraded carrageenan

    Energy Technology Data Exchange (ETDEWEB)

    Relleve, Lorna; Dela Rosa, Alumanda; ABAD, Lucille; Aranilla, Charito; Aliganga, Anne Kathrina [Philippine Nuclear Research Institute, Quezon City (Philippines); Yoshii, Fumio; Kume, Tamikazu; Nagasawa, Naotsugu [Japan Atomic Energy Research Inst., Takasaki, Gunma (Japan). Takasaki Radiation Chemistry Research Establishment

    2001-03-01

    Carrageenans were irradiated in solid state to doses 50-1000 kGy in air at ambient temperature. Changes in their molecular weight and functional properties with respect to their FT-IR and UV spectra were evaluated. Irradiation of carrageenans resulted in a rapid decrease of molecular weight indicating main chain scission in their polymeric structures. Formations of some compounds were evident by new absorption peaks in their UV and FT-IR spectra and quantitative analyses of the FT-IR spectra which, in addition, support that there is a breakdown in the carrageenan structure. Irradiated carrageenans were investigated for their plant growth-promoting activity. Carrageenans were added to the nutrient solutions for rice seedlings under non-circulating hydroponics cultivation. Irradiated carrageenan induced weight gain in treated rice seedlings. Maximum weight gain was obtained with KC irradiated at 100 kGy while treatment with IC at 500 kGy. IC exhibited less growth promoting properties than KC. The growth of fungi on the roots disappeared with treatment of IC and KC irradiated at 500 kGy. Growth promotion of some leafy vegetables was also observed with application of degraded KC. The carrageenan molecule has been broken down to smaller molecule (s) or compound (s) that can be absorbed effectively as nourishment factors and anti-microbial agents by plants. (author)

  4. Biological activities of radiation-degraded carrageenan

    International Nuclear Information System (INIS)

    Relleve, Lorna; Dela Rosa, Alumanda; ABAD, Lucille; Aranilla, Charito; Aliganga, Anne Kathrina; Yoshii, Fumio; Kume, Tamikazu; Nagasawa, Naotsugu

    2001-01-01

    Carrageenans were irradiated in solid state to doses 50-1000 kGy in air at ambient temperature. Changes in their molecular weight and functional properties with respect to their FT-IR and UV spectra were evaluated. Irradiation of carrageenans resulted in a rapid decrease of molecular weight indicating main chain scission in their polymeric structures. Formations of some compounds were evident by new absorption peaks in their UV and FT-IR spectra and quantitative analyses of the FT-IR spectra which, in addition, support that there is a breakdown in the carrageenan structure. Irradiated carrageenans were investigated for their plant growth-promoting activity. Carrageenans were added to the nutrient solutions for rice seedlings under non-circulating hydroponics cultivation. Irradiated carrageenan induced weight gain in treated rice seedlings. Maximum weight gain was obtained with KC irradiated at 100 kGy while treatment with IC at 500 kGy. IC exhibited less growth promoting properties than KC. The growth of fungi on the roots disappeared with treatment of IC and KC irradiated at 500 kGy. Growth promotion of some leafy vegetables was also observed with application of degraded KC. The carrageenan molecule has been broken down to smaller molecule (s) or compound (s) that can be absorbed effectively as nourishment factors and anti-microbial agents by plants. (author)

  5. Synthesis and Biological Evaluation of Brain-Specific Anti-RNA Viral Agents

    Science.gov (United States)

    1989-06-30

    TITLE (Include Securrty Clasification ) Synthesis and Biological Evaluation of Brain Specific Anti-RNA Viral Agents 12. PERSONAL. AUTHOR(S) Marcus E...AD (FRONT COVER Contract No.: DAMD17-88-C-8011 Title: Synthesis and Biological Evaluation of Brain-Specific Anti-RNA Viral Agents Principal...matr s---. Further in vivo testing included tissue distribution studies and antiviral activity studies performed in a murine viral encephalitic model. 20

  6. Substituted Pyrazinecarboxamides: Synthesis and Biological Evaluation

    Directory of Open Access Journals (Sweden)

    Katarina Kralova

    2006-03-01

    Full Text Available Condensation of the corresponding chlorides of some substituted pyrazine-2-carboxylic acids (pyrazine-2-carboxylic acid, 6-chloropyrazine-2-carboxylic acid, 5-tert-butylpyrazine-2-carboxylic acid or 5-tert-butyl-6-chloropyrazine-2-carboxylic acid withvarious ring-substituted aminothiazoles or anilines yielded a series of amides. Thesyntheses, analytical and spectroscopic data of thirty newly prepared compounds arepresented. Structure-activity relationships between the chemical structures and the anti-mycobacterial, antifungal and photosynthesis-inhibiting activity of the evaluatedcompounds are discussed. 3,5-Bromo-4-hydroxyphenyl derivatives of substitutedpyrazinecarboxylic acid, 16-18, have shown the highest activity against Mycobacteriumtuberculosis H37Rv (54-72% inhibition. The highest antifungal effect againstTrichophyton mentagrophytes, the most susceptible fungal strain tested, was found for5-tert-butyl-6-chloro-N-(4-methyl-1,3-thiazol-2-ylpyrazine-2-carboxamide (8, MIC =31.25 μmol·mL-1. The most active inhibitors of oxygen evolution rate in spinachMolecules 2006, 11 243 chloroplasts were the compounds 5-tert-butyl-6-chloro-N-(5-bromo-2-hydroxyphenyl- pyrazine-2-carboxamide (27, IC50 = 41.9 μmol·L-1 and 5-tert-butyl-6-chloro-N-(1,3- thiazol-2-yl-pyrazine-2-carboxamide (4, IC50 = 49.5 μmol·L-1.

  7. Phytochemical Constituents and Biological Activities of Salvia suffruticosa

    Directory of Open Access Journals (Sweden)

    Arezoo Rustaie

    2018-03-01

    Full Text Available Background and objectives: Salvia suffruticosa is a perennial plant from Lamiaceae family. Many Salvia species have been employed as medicinal plants; despite the medicinal potentials of S. suffruticosa, there is limited studies regarding its phytochemical profile or biological properties. The aim of the present study was to investigate the chemical constituents of the essential oil and extract of the plant and evaluate its biological activities. Methods: Essential oil from the aerial parts of the plant was extracted by hydrodistillation and analyzed using gas chromatography/mass spectroscopy. Isolation of compounds from methanol and petroleum ether fractions was achieved by using column chromatography with different stationary phases. The structures of the isolated compounds were elucidated by NMR techniques. Cytotoxicity potentials were evaluated using MTT assay and acridine orange/ethidium bromide staining method. Antioxidant activity was assessed by DPPH method. Results: Hydrocarbon sesquiterpenes were identified as the predominant components of the oil, with β-caryophyllene (27.35%, bicyclogermacrene (22.15%, germacrene-D (9.49% and β-farnesene (9.08% as the major constituents. Phytochemical analysis of the extract resulted in isolation of lupeol (1, β-sitosterol (2, stigmasterol (3, caffeic acid (4 and 1-feruloyl-β-D-glucopyranose (5. Among the tested samples, lupeol demonstrated the most potent inhibitory activity toward breast cancer cell lines including MCF-7, T-47D and MDA-MB-231 with IC50 values equal to 33.38±2.6, 36.70±3.1 and 23.66±1.4 μg/mL, respectively; caffeic acid with IC50 value of 12.1±1.2 μg/mL showed the most potent radical scavenging activity. Conclusion: The results of this study suggested S. suffruticosa as a promising source of bioactive compounds useful in prevention and treatment of cancer.

  8. Biological Activities of Oleanolic Acid Derivatives from Calendula officinalis Seeds.

    Science.gov (United States)

    Zaki, Ahmed; Ashour, Ahmed; Mira, Amira; Kishikawa, Asuka; Nakagawa, Toshinori; Zhu, Qinchang; Shimizu, Kuniyoshi

    2016-05-01

    Phytochemical examination of butanol fraction of Calendula officinalis seeds led to the isolation of two compounds identified as 28-O-β-D-glucopyranosyl-oleanolic acid 3-O-β-D-glucopyranosyl (1→3)-β-D-glucopyranosiduronic acid (CS1) and oleanolic acid 3-O-β-D-glucopyranosyl (1→3)-β-D-glucopyranosiduronic acid (CS2). Biological evaluation was carried out for these two compounds such as melanin biosynthesis inhibitory, hyaluronic acid production activities, anti obesity using lipase inhibition and adipocyte differentiation as well as evaluation of the protective effect against hydrogen peroxide induced neurotoxicity in neuro-2A cells. The results showed that, compound CS2 has a melanin biosynthesis stimulatory activity; however, compound CS1 has a potent stimulatory effect for the production of hyaluronic acid on normal human dermal fibroblast from adult (NHDF-Ad). Both compounds did not show any inhibitory effect on both lipase and adipocyte differentiation. Compound CS2 could protect neuro-2A cells and increased cell viability against H2 O2 . These activities (melanin biosynthesis stimulatory and protective effect against H2 O2 of CS2 and hyaluronic acid productive activities of these triterpene derivatives) have been reported for the first time. Copyright © 2016 John Wiley & Sons, Ltd. Copyright © 2016 John Wiley & Sons, Ltd.

  9. Novel Triazole Hybrids of Betulin: Synthesis and Biological Activity Profile.

    Science.gov (United States)

    Bębenek, Ewa; Jastrzębska, Maria; Kadela-Tomanek, Monika; Chrobak, Elwira; Orzechowska, Beata; Zwolińska, Katarzyna; Latocha, Małgorzata; Mertas, Anna; Czuba, Zenon; Boryczka, Stanisław

    2017-11-01

    Betulin derivatives containing a 1,2,3-triazole ring possess a wide spectrum of biological activities, including antiviral, anticancer, and antibacterial activity. A series of novel triazoles were prepared by the 1,3-dipolar cycloaddition reaction between the alkyne derivatives of betulin and organic azides. The chemical structures of the obtained compounds were defined by ¹H and 13 C NMR, IR, and high-resolution mass spectrometry (HR-MS) analysis. The target triazoles were screened for their antiviral activity against DNA and RNA viruses. The cytotoxic activity of the obtained compounds 5a - k and 6a - h was determined using five human cancer cell lines (T47D, MCF-7, SNB-19, Colo-829, and C-32) by a WST-1 assay. The bistriazole 6b displayed a promising IC 50 value (0.05 μM) against the human ductal carcinoma T47D (500-fold higher potency than cisplatin). The microdilution method was applied for an evaluation of the antimicrobial activity of all of the compounds. The triazole 5e containing a 3'-deoxythymidine-5'-yl moiety exhibited antibacterial activity against two gram-negative bacteria vz. Klebsiella pneumoniae and Escherichia coli (minimal inhibitory concentration (MIC) range of 0.95-1.95 μM).

  10. Novel Triazole Hybrids of Betulin: Synthesis and Biological Activity Profile

    Directory of Open Access Journals (Sweden)

    Ewa Bębenek

    2017-11-01

    Full Text Available Betulin derivatives containing a 1,2,3-triazole ring possess a wide spectrum of biological activities, including antiviral, anticancer, and antibacterial activity. A series of novel triazoles were prepared by the 1,3-dipolar cycloaddition reaction between the alkyne derivatives of betulin and organic azides. The chemical structures of the obtained compounds were defined by 1H and 13C NMR, IR, and high-resolution mass spectrometry (HR-MS analysis. The target triazoles were screened for their antiviral activity against DNA and RNA viruses. The cytotoxic activity of the obtained compounds 5a–k and 6a–h was determined using five human cancer cell lines (T47D, MCF-7, SNB-19, Colo-829, and C-32 by a WST-1 assay. The bistriazole 6b displayed a promising IC50 value (0.05 μM against the human ductal carcinoma T47D (500-fold higher potency than cisplatin. The microdilution method was applied for an evaluation of the antimicrobial activity of all of the compounds. The triazole 5e containing a 3′-deoxythymidine-5′-yl moiety exhibited antibacterial activity against two gram-negative bacteria vz. Klebsiella pneumoniae and Escherichia coli (minimal inhibitory concentration (MIC range of 0.95–1.95 μM.

  11. Egg yolk proteins and peptides with biological activity

    Directory of Open Access Journals (Sweden)

    Aleksandra Zambrowicz

    2014-12-01

    Full Text Available Many proteins of food reveal biological activity. In the sequence of these proteins also numerous biologically active peptides are encrypted. These peptides are released during proteolysis naturally occurring in the gastrointestinal tract, food fermentation or during designed enzymatic hydrolysis in vitro. Biopeptides may exert multiple activities, affecting the cardiovascular, endocrine, nervous and immune systems. An especially rich source of bioactive proteins and biopeptides is egg. Bioactive peptides released from egg white proteins have been well described, whereas egg yolk proteins as precursors of biopeptides are less well characterized. This manuscript describes biologically active proteins and peptides originating from egg yolk and presents their potential therapeutic role.

  12. Galloylation of polyphenols alters their biological activity

    Czech Academy of Sciences Publication Activity Database

    Karas, D.; Ulrichová, J.; Valentová, Kateřina

    2017-01-01

    Roč. 105, JUL 2017 (2017), s. 223-240 ISSN 0278-6915 R&D Projects: GA MŠk(CZ) LD15082; GA MŠk(CZ) LD15084; GA MŠk(CZ) LO1304 Grant - others:GA ČR(CZ) GAP303/12/G163 Program:GA Institutional support: RVO:61388971 Keywords : Polyphenols * Gallic acid * Galloylation Subject RIV: CE - Biochemistry OBOR OECD: Biochemistry and molecular biology Impact factor: 3.778, year: 2016

  13. Phytochemical and biological evaluation of Salvia apiana.

    Science.gov (United States)

    Srivedavyasasri, Radhakrishnan; Hayes, Taylor; Ross, Samir A

    2017-09-01

    Salvia apiana (white sage, Lamiaceae family) plant is native to southern California and parts of Mexico. Some Native American tribes local to this region consider S. apiana to be sacred and burn the leaves as incense for purification ceremonies. The plant has been used to treat sore throats, coughs, chest colds, upper respiratory infections and poison oak rashes. The aqueous ethanolic extract of S. apiana showed moderate CB1 activity (58.3% displacement). Chromatographic purification of the ethanolic extract on silica gel column led to isolation of nine compounds: rosmadial (I), carnosol (II), 16-hydroxycarnosol (III), sageone (IV), cirsimaritin (V), salvigenin (VI), oleanolic acid (VII), 3β,28-dihydroxy-urs-12-ene (VIII), and ursolic acid (IX). The structures of the isolated compounds were determined by their 1D, 2D NMR and MS spectral data. All the fractions and isolated compounds were tested for cannabinoid and opioid receptor binding.

  14. Synthesis and biological evaluation of furanoallocolchicinoids.

    Science.gov (United States)

    Voitovich, Yuliya V; Shegravina, Ekaterina S; Sitnikov, Nikolay S; Faerman, Vladimir I; Fokin, Valery V; Schmalz, Hans-Gunther; Combes, Sebastien; Allegro, Diane; Barbier, Pascal; Beletskaya, Irina P; Svirshchevskaya, Elena V; Fedorov, Alexey Yu

    2015-01-22

    A series of conformationally flexible furan-derived allocolchicinoids was prepared from commercially available colchicine in good to excellent yields using a three-step reaction sequence. Cytotoxicity studies indicated the potent activity of two compounds against human epithelial and lymphoid cell lines (AsPC-1, HEK293, and Jurkat) as well as against Wnt-1 related murine epithelial cell line W1308. The results of in vitro experiments demonstrated that the major effect of these compounds was the induction of cell cycle arrest in the G2/M phase as a direct consequence of effective tubulin binding. In vivo testing of the most potent furanoallocolchicinoid 10c using C57BL/6 mice inoculated with Wnt-1 tumor cells indicated significant inhibition of the tumor growth.

  15. Biological activities of substituted trichostatic acid derivatives

    Indian Academy of Sciences (India)

    Administrator

    as 6-fluoro trichostatin A, with antiproliferative activities in the micromolar range and with histone deacetylase inhibitory activity. Keywords. Trichostatic acid; HDAC; inhibitor. 1. Introduction. Reversible chemical modifications of DNA and his- tones are important cellular events that promote activation or repression of DNA ...

  16. Fruit cuticular waxes as a source of biologically active triterpenoids.

    Science.gov (United States)

    Szakiel, Anna; Pączkowski, Cezary; Pensec, Flora; Bertsch, Christophe

    2012-06-01

    The health benefits associated with a diet rich in fruit and vegetables include reduction of the risk of chronic diseases such as cardiovascular disease, diabetes and cancer, that are becoming prevalent in the aging human population. Triterpenoids, polycyclic compounds derived from the linear hydrocarbon squalene, are widely distributed in edible and medicinal plants and are an integral part of the human diet. As an important group of phytochemicals that exert numerous biological effects and display various pharmacological activities, triterpenoids are being evaluated for use in new functional foods, drugs, cosmetics and healthcare products. Screening plant material in the search for triterpenoid-rich plant tissues has identified fruit peel and especially fruit cuticular waxes as promising and highly available sources. The chemical composition, abundance and biological activities of triterpenoids occurring in cuticular waxes of some economically important fruits, like apple, grape berry, olive, tomato and others, are described in this review. The need for environmentally valuable and potentially profitable technologies for the recovery, recycling and upgrading of residues from fruit processing is also discussed.

  17. Biological regeneration of para-nitrophenol loaded activated carbon

    International Nuclear Information System (INIS)

    Durrani, M.A.Q.; Martin, R.J.

    1997-01-01

    Biological regeneration is one of several methods that may be used to restore the adsorptive capacity of exhausted granular activated carbon (GAC). This study deals with in-situ biological regeneration on a pilot scale. The principal objective of this research was to ascertain whether biological regeneration of GAC could occur under conditions typical of water treatment. The important parameters which may have the greatest impact on bio regeneration of a given adsorbate were studied. The research investigated the extent of bio regeneration for para-nitrophenol (PNP) of concentration 50 mg/L. Bio regeneration in the total exhaustion system was evaluated in terms of regeneration efficiency and the substrate removal. A three mode procedure was followed for each bio regeneration run. The prepared carbon was initially exhausted with an adsorbate; it was then bio regenerated for para-nitrophenol (PNP) of concentration 50 mg/L. Bio regeneration in he total exhaustion system was evaluated in terms of regeneration efficiency and the substrate removal. A three mode procedure was followed for each bio regeneration run. The prepared carbon was initially exhausted with an adsorbate; it was then bio regenerated with a mixed culture of bacteria, and lastly the carbon was re-saturated. In the totally exhausted GAC system, the bio regeneration was enhanced by increasing the during of regeneration for a fixed initial biomass content of the bioreactor. The bio regeneration efficiency of the totally exhausted (with PNP) GAC the empty bed contact time (EBCT) and the initial concentration of the substrate had a profound effect on the bio regeneration efficiency. Bacterial counts in the effluents of regenerated GAC columns were significantly more than those of fresh carbon effluents. (author)

  18. BIOLOGICAL ACTIVITY OF APPLE JUICE ENRICHED BY HERBAL EXTRACTS

    Directory of Open Access Journals (Sweden)

    Eva Ivanišová

    2015-02-01

    Full Text Available Herbal phytochemicals have recently become an attractive subject for scientists in many different research areas. The aim of this study was to determine antioxidant activity, total polyphenol and flavonoid content of apple juice enriched by water herbal extracts. Secondary was to evaluate sensory characteristic of enriched apple juice. It was found that applications of water herbal extracts to apple juice increase antioxidant activities, and also total polyphenol and flavonoid content with compare to pure apple juice. The highest biological activities were detected in apple juice with addition of lemon balm (14.42 mg TEAC/L; 84.38 mg TEAC/L; 50.88 mg GAE/L; 36.26 μg QE/L, oregano (14.92 mg TEAC/L; 79.97 mg TEAC/L; 50.51 mg GAE/L; 31.02 μg QE/L and salvia (8.40 mg TEAC/L; 30.40 mg TEAC/L; 23.33 mg GAE/L; 27.67 μg QE/L water extract. Sensorial analysis of samples showed, that enriched juices had better properties for evaluators with compared to pure juice. The aim of this study was also to mention the potential use of medicinal herbs in food industry, because plant bioactive compounds can play an important role in preventing cardiovascular diseases, cancers and reduction inflammatory action.

  19. Ficus carica L. (Moraceae): Phytochemistry, Traditional Uses and Biological Activities

    Science.gov (United States)

    Mawa, Shukranul; Husain, Khairana; Jantan, Ibrahim

    2013-01-01

    This paper describes the botanical features of Ficus carica L. (Moraceae), its wide variety of chemical constituents, its use in traditional medicine as remedies for many health problems, and its biological activities. The plant has been used traditionally to treat various ailments such as gastric problems, inflammation, and cancer. Phytochemical studies on the leaves and fruits of the plant have shown that they are rich in phenolics, organic acids, and volatile compounds. However, there is little information on the phytochemicals present in the stem and root. Reports on the biological activities of the plant are mainly on its crude extracts which have been proven to possess many biological activities. Some of the most interesting therapeutic effects include anticancer, hepatoprotective, hypoglycemic, hypolipidemic, and antimicrobial activities. Thus, studies related to identification of the bioactive compounds and correlating them to their biological activities are very useful for further research to explore the potential of F. carica as a source of therapeutic agents. PMID:24159359

  20. SYNTHESIS, REACTIVITY AND BIOLOGICAL ACTIVITY OF QUINOXALIN-2-ONE DERIVATIVES

    OpenAIRE

    El Mokhtar Essassi; R. Bouhfid; Y. Kandri Rodi; S. Ferfra; H. Benzeid; Y. Ramli

    2010-01-01

    Quinoxalines have a great interest in various fields and particularly in chemistry, biology and pharmacology. It enabled the researchers to develop many methods for their preparations and to seek new fields of application. In this review, we’ll expose different methods of synthesis of the quinoxalin-2-one, its reactivity and finally we’ll discuss the various biological activities of its derivatives.

  1. Synthesis and biological activities of substituted N ...

    African Journals Online (AJOL)

    use

    2011-12-07

    Dec 7, 2011 ... The present study describes the synthesis, antioxidant and antibacterial activities of substituted N'- benzoylhydrazone derivatives, to ... addition, the dramatically rising prevalence of multidrug- resistant microbial infections has ...... extract of Chinese green tea (Camellia sinensis) on Listeria monocytogenes.

  2. Biological activities of Castela coccinea Griseb. extracts

    OpenAIRE

    Campagna, María Noel; Ratti, María Soledad; Sciara, Mariela; García Vescovi, Eleonora; Gattuso, Martha; Martínez, María Laura

    2011-01-01

    Infusions of leaf and bark of Castela coccinea Griseb. (Simaroubaceae) were traditionally used against dysentery. In this work, anti-bacterial and antioxidant activity were studied in C. coccinea extracts. The higest DPPH scavenging activity was detected in ethanolic leaf extracts with an IC50= 0.015 mg/ml. Bark ethanolic extracts showed inhibition of lipoperoxidation and free radical scavenging. However, a previous work evidenced that this extract is toxic at a concentration needed ...

  3. Chemistry and Biological Activities of Flavonoids: An Overview

    Science.gov (United States)

    Kumar, Shashank; Pandey, Abhay K.

    2013-01-01

    There has been increasing interest in the research on flavonoids from plant sources because of their versatile health benefits reported in various epidemiological studies. Since flavonoids are directly associated with human dietary ingredients and health, there is need to evaluate structure and function relationship. The bioavailability, metabolism, and biological activity of flavonoids depend upon the configuration, total number of hydroxyl groups, and substitution of functional groups about their nuclear structure. Fruits and vegetables are the main dietary sources of flavonoids for humans, along with tea and wine. Most recent researches have focused on the health aspects of flavonoids for humans. Many flavonoids are shown to have antioxidative activity, free radical scavenging capacity, coronary heart disease prevention, hepatoprotective, anti-inflammatory, and anticancer activities, while some flavonoids exhibit potential antiviral activities. In plant systems, flavonoids help in combating oxidative stress and act as growth regulators. For pharmaceutical purposes cost-effective bulk production of different types of flavonoids has been made possible with the help of microbial biotechnology. This review highlights the structural features of flavonoids, their beneficial roles in human health, and significance in plants as well as their microbial production. PMID:24470791

  4. Biological Activities of the Essential Oil from Erigeron floribundus.

    Science.gov (United States)

    Petrelli, Riccardo; Orsomando, Giuseppe; Sorci, Leonardo; Maggi, Filippo; Ranjbarian, Farahnaz; Biapa Nya, Prosper C; Petrelli, Dezemona; Vitali, Luca A; Lupidi, Giulio; Quassinti, Luana; Bramucci, Massimo; Hofer, Anders; Cappellacci, Loredana

    2016-08-13

    Erigeron floribundus (Asteraceae) is an herbaceous plant widely used in Cameroonian traditional medicine to treat various diseases of microbial and non-microbial origin. In the present study, we evaluated the in vitro biological activities displayed by the essential oil obtained from the aerial parts of E. floribundus, namely the antioxidant, antimicrobial and antiproliferative activities. Moreover, we investigated the inhibitory effects of E. floribundus essential oil on nicotinate mononucleotide adenylyltransferase (NadD), a promising new target for developing novel antibiotics, and Trypanosoma brucei, the protozoan parasite responsible for Human African trypanosomiasis. The essential oil composition was dominated by spathulenol (12.2%), caryophyllene oxide (12.4%) and limonene (8.8%). The E. floribundus oil showed a good activity against Staphylococcus aureus (inhibition zone diameter, IZD of 14 mm, minimum inhibitory concentration, MIC of 512 µg/mL). Interestingly, it inhibited the NadD enzyme from S. aureus (IC50 of 98 µg/mL), with no effects on mammalian orthologue enzymes. In addition, T. brucei proliferation was inhibited with IC50 values of 33.5 µg/mL with the essential oil and 5.6 µg/mL with the active component limonene. The essential oil exhibited strong cytotoxicity on HCT 116 colon carcinoma cells with an IC50 value of 14.89 µg/mL, and remarkable ferric reducing antioxidant power (tocopherol-equivalent antioxidant capacity, TEAC = 411.9 μmol·TE/g).

  5. Biological Activities of the Essential Oil from Erigeron floribundus

    Directory of Open Access Journals (Sweden)

    Riccardo Petrelli

    2016-08-01

    Full Text Available Erigeron floribundus (Asteraceae is an herbaceous plant widely used in Cameroonian traditional medicine to treat various diseases of microbial and non-microbial origin. In the present study, we evaluated the in vitro biological activities displayed by the essential oil obtained from the aerial parts of E. floribundus, namely the antioxidant, antimicrobial and antiproliferative activities. Moreover, we investigated the inhibitory effects of E. floribundus essential oil on nicotinate mononucleotide adenylyltransferase (NadD, a promising new target for developing novel antibiotics, and Trypanosoma brucei, the protozoan parasite responsible for Human African trypanosomiasis. The essential oil composition was dominated by spathulenol (12.2%, caryophyllene oxide (12.4% and limonene (8.8%. The E. floribundus oil showed a good activity against Staphylococcus aureus (inhibition zone diameter, IZD of 14 mm, minimum inhibitory concentration, MIC of 512 µg/mL. Interestingly, it inhibited the NadD enzyme from S. aureus (IC50 of 98 µg/mL, with no effects on mammalian orthologue enzymes. In addition, T. brucei proliferation was inhibited with IC50 values of 33.5 µg/mL with the essential oil and 5.6 µg/mL with the active component limonene. The essential oil exhibited strong cytotoxicity on HCT 116 colon carcinoma cells with an IC50 value of 14.89 µg/mL, and remarkable ferric reducing antioxidant power (tocopherol-equivalent antioxidant capacity, TEAC = 411.9 μmol·TE/g.

  6. Chemistry and Biological Activities of Flavonoids: An Overview

    Directory of Open Access Journals (Sweden)

    Shashank Kumar

    2013-01-01

    Full Text Available There has been increasing interest in the research on flavonoids from plant sources because of their versatile health benefits reported in various epidemiological studies. Since flavonoids are directly associated with human dietary ingredients and health, there is need to evaluate structure and function relationship. The bioavailability, metabolism, and biological activity of flavonoids depend upon the configuration, total number of hydroxyl groups, and substitution of functional groups about their nuclear structure. Fruits and vegetables are the main dietary sources of flavonoids for humans, along with tea and wine. Most recent researches have focused on the health aspects of flavonoids for humans. Many flavonoids are shown to have antioxidative activity, free radical scavenging capacity, coronary heart disease prevention, hepatoprotective, anti-inflammatory, and anticancer activities, while some flavonoids exhibit potential antiviral activities. In plant systems, flavonoids help in combating oxidative stress and act as growth regulators. For pharmaceutical purposes cost-effective bulk production of different types of flavonoids has been made possible with the help of microbial biotechnology. This review highlights the structural features of flavonoids, their beneficial roles in human health, and significance in plants as well as their microbial production.

  7. Synthetic Approaches and Biological Activities of 4-Hydroxycoumarin Derivatives

    Directory of Open Access Journals (Sweden)

    Oee-Sook Park

    2009-11-01

    Full Text Available The main purpose of this review is to summarize recent chemical syntheses and structural modifications of 4-hydroxycoumarin and its derivatives, of interest due to their characteristic conjugated molecular architecture and biological activities.

  8. Baltic cyanobacteria- A source of biologically active compounds

    Digital Repository Service at National Institute of Oceanography (India)

    Mazur-Marzec, H.; Błaszczyk, A.; Felczykowska, A.; Hohlfeld, N.; Kobos, J.; Toruńska-Sitarz, A.; PrabhaDevi; Montalva`o, S.; DeSouza, L.; Tammela, P.; Mikosik, A.; Bloch, S.; Nejman-Faleńczyk, B.; Węgrzyn, G.

    Cyanobacteria are effective producers of bioactive metabolites, including both acute toxins and potential pharmaceuticals. In the current work, the biological activity of 27 strains of Baltic cyanobacteria representing different taxonomic groups...

  9. Biologically active substances from Zanthoxylum capense(thumb.) Harv.

    CSIR Research Space (South Africa)

    Steyn, PS

    1998-08-01

    Full Text Available A chemical investigation into the composition of Zanthoxylum capense yielded several biologically active compounds, including pellitorine. A convenient HPLC method was developed to determine the presence of pellitorine in crude extracts from plants...

  10. Physical activity and biological maturation: a systematic review

    Directory of Open Access Journals (Sweden)

    Eliane Denise Araújo Bacil

    2015-03-01

    Full Text Available OBJECTIVE: To analyze the association between physical activity (PA and biological maturation in children and adolescents. DATA SOURCE: We performed a systematic review in April 2013 in the electronic databases of PubMed/MEDLINE, SportDiscus, Web of Science and LILACS without time restrictions. A total of 628 potentially relevant articles were identified and 10 met the inclusion criteria for this review: cross-sectional or longitudinal studies, published in Portuguese, English or Spanish, with schoolchildren aged 9-15 years old of both genders. DATA SYNTHESIS: Despite the heterogeneity of the studies, there was an inverse association between PA and biological maturation. PA decreases with increased biological and chronological age in both genders. Boys tend to be more physically active than girls; however, when controlling for biological age, the gender differences disappear. The association between PA and timing of maturation varies between the genders. Variation in the timing of biological maturation affects the tracking of PA in early adolescent girls. This review suggests that mediators (BMI, depression, low self-esteem, and concerns about body weight can explain the association between PA and biological maturation. CONCLUSIONS: There is an association between PA and biological maturation. PA decreases with increasing biological age with no differences between genders. As for the timing of biological maturation, this association varies between genders.

  11. Biological activity of Herissantia crispa (L. Brizicky

    Directory of Open Access Journals (Sweden)

    Igara Oliveira Lima

    Full Text Available The crude methanol extract (EMeOH of the aerial parts of Herissantia crispa (L. Brizicky, plant riches in flavonoids and without pharmacological studies, was tested to value its activity under the behaviour parameters and to determine the lethal dose (LD50 in mice; antimicrobial and antiulcerogenic activities. The EMeOH (5,000 mg/kg, v.o. or 2,000 mg/kg i.p. did not alter the behaviour parameters and there were not mice deaths. The extract inhibited the bacterial growth. The EMeOH (750 mg/kg showed anti-diarroeal activity. The EMeOH (250, 500 and 750 mg/kg decreased the gastric lesions induced by 0.3 M HCl/ethanol 60% in mice. In conclusion, the EMeOH presents anti-ulcerogenic activity;, however it is necessary to value the antiulcerogenic activity in more specific models and to study the action mechanism by which the vegetable sample protects the gastric mucosa.

  12. Controlled Release of Biologically Active Silver from Nanosilver Surfaces

    OpenAIRE

    Liu, Jingyu; Sonshine, David A.; Shervani, Saira; Hurt, Robert H.

    2010-01-01

    Major pathways in the antibacterial activity and eukaryotic toxicity of nano-silver involve the silver cation and its soluble complexes, which are well established thiol toxicants. Through these pathways, nano-silver behaves in analogy to a drug delivery system, in which the particle contains a concentrated inventory of an active species, the ion, which is transported to and released near biological target sites. Although the importance of silver ion in the biological response to nano-silver ...

  13. Activated Sludge. Student Manual. Biological Treatment Process Control.

    Science.gov (United States)

    Boe, Owen K.; Klopping, Paul H.

    This student manual contains the textual material for a seven-lesson unit on activated sludge. Topic areas addressed in the lessons include: (1) activated sludge concepts and components (including aeration tanks, aeration systems, clarifiers, and sludge pumping systems); (2) activated sludge variations and modes; (3) biological nature of activated…

  14. Raman Optical Activity of Biological Molecules

    Science.gov (United States)

    Blanch, Ewan W.; Barron, Laurence D.

    Now an incisive probe of biomolecular structure, Raman optical activity (ROA) measures a small difference in Raman scattering from chiral molecules in right- and left-circularly polarized light. As ROA spectra measure vibrational optical activity, they contain highly informative band structures sensitive to the secondary and tertiary structures of proteins, nucleic acids, viruses and carbohydrates as well as the absolute configurations of small molecules. In this review we present a survey of recent studies on biomolecular structure and dynamics using ROA and also a discussion of future applications of this powerful new technique in biomedical research.

  15. Synthesis and biological activity of radiolabeled phytosterols

    Energy Technology Data Exchange (ETDEWEB)

    De Palma, A.

    1984-01-01

    /sup 3/H and /sup 14/C-labeled phytosterols were synthesized for the purpose of elucidating insect sterol side-chain dealkylating mechanisms. Sitosterol, stigmasterol, and the 29-fluoro derivatives of these compounds, which are highly toxic, were labeled with /sup 3/H at C-29 in order to study the fate of the two-carbon dealkylation product in vivo and in vitro. The first rapid, reliable in vitro dealkylation bioassay was developed using doubly-labeled (29-/sup 3/H)-(24-/sup 14/C) fucosterol epoxides as the substrates, incubated with midgut preparations from Manduca sexta, the tobacco hornworm. Since C-28 and C-29 are lost in the dealkylation process, the extent of dealkylation is expressed as the change in the isotopic ratio when the system is partitioned between an organic solvent and water after incubation. As predicted, the /sup 3/H//sup 14/C ratio decreases in the organic layer as a function of time, due to loss of /sup 3/H into the aqueous phase as acetate or a biological equivalent. This ratio likewise increases in the aqueous phase for the same reason. The (29-/sup 3/H) phytosterols alone are reliable substrates for the first rapid in vivo bioassay of phytosterol dealkylation.

  16. Synthesis and biological activity of radiolabeled phytosterols

    International Nuclear Information System (INIS)

    De Palma, A.

    1984-01-01

    3 H and 14 C-labeled phytosterols were synthesized for the purpose of elucidating insect sterol side-chain dealkylating mechanisms. Sitosterol, stigmasterol, and the 29-fluoro derivatives of these compounds, which are highly toxic, were labeled with 3 H at C-29 in order to study the fate of the two-carbon dealkylation product in vivo and in vitro. The first rapid, reliable in vitro dealkylation bioassay was developed using doubly-labeled [29- 3 H]-[24- 14 C] fucosterol epoxides as the substrates, incubated with midgut preparations from Manduca sexta, the tobacco hornworm. Since C-28 and C-29 are lost in the dealkylation process, the extent of dealkylation is expressed as the change in the isotopic ratio when the system is partitioned between an organic solvent and water after incubation. As predicted, the 3 H/ 14 C ratio decreases in the organic layer as a function of time, due to loss of 3 H into the aqueous phase as acetate or a biological equivalent. This ratio likewise increases in the aqueous phase for the same reason. The [29- 3 H] phytosterols alone are reliable substrates for the first rapid in vivo bioassay of phytosterol dealkylation

  17. Biologically active compounds of semi-metals.

    Science.gov (United States)

    Rezanka, Tomás; Sigler, Karel

    2008-02-01

    Semi-metals (boron, silicon, arsenic and selenium) form organo-metal compounds, some of which are found in nature and affect the physiology of living organisms. They include, e.g., the boron-containing antibiotics aplasmomycin, borophycin, boromycin, and tartrolon or the silicon compounds present in "silicate" bacteria, relatives of the genus Bacillus, which release silicon from aluminosilicates through the secretion of organic acids. Arsenic is incorporated into arsenosugars and arsenobetaines by marine algae and invertebrates, and fungi and bacteria can produce volatile methylated arsenic compounds. Some prokaryotes can use arsenate as a terminal electron acceptor while others can utilize arsenite as an electron donor to generate energy. Selenium is incorporated into selenocysteine that is found in some proteins. Biomethylation of selenide produces methylselenide and dimethylselenide. Selenium analogues of amino acids, antitumor, antibacterial, antifungal, antiviral, anti-infective drugs are often used as analogues of important pharmacological sulfur compounds. Other metalloids, i.e. the rare and toxic tellurium and the radioactive short-lived astatine, have no biological significance.

  18. Biological evaluation of nanosilver incorporated cellulose pulp for hygiene products

    Energy Technology Data Exchange (ETDEWEB)

    Kavitha Sankar, P.C.; Ramakrishnan, Reshmi; Rosemary, M.J., E-mail: rosemarymj@lifecarehll.com

    2016-04-01

    Cellulose pulp has a visible market share in personal hygiene products such as sanitary napkins and baby diapers. However it offers good surface for growth of microorganisms. Huge amount of research is going on in developing hygiene products that do not initiate microbial growth. The objective of the present work is to produce antibacterial cellulose pulp by depositing silver nanopowder on the cellulose fiber. The silver nanoparticles used were of less than 100 nm in size and were characterised using transmission electron microscopy and X-ray powder diffraction studies. Antibacterial activity of the functionalized cellulose pulp was proved by JIS L 1902 method. The in-vitro cytotoxicity, in-vivo vaginal irritation and intracutaneous reactivity studies were done with silver nanopowder incorporated cellulose pulp for introducing a new value added product to the market. Cytotoxicity evaluation suggested that the silver nanoparticle incorporated cellulose pulp is non-cytotoxic. No irritation and skin sensitization were identified in animals tested with specific extracts prepared from the test material in the in-vivo experiments. The results indicated that the silver nanopowder incorporated cellulose pulp meets the requirements of the standard practices recommended for evaluating the biological reactivity and has good biocompatibility, hence can be classified as a safe hygiene product. - Highlights: • Different amounts of silver nanoparticles (0.2 g–0.4 g/napkin) were added to cellulose pulp. • The silver nanoparticle incorporated cellulose pulp was proved to be antibacterial by JIS L 1902 method. • The minimum concentration of silver required for antibacterial activity with no cytotoxicity has been found out. • In-vivo vaginal irritation and intracutaneous reactivity studies confirmed the biocompatibility of the material.

  19. Biological evaluation of nanosilver incorporated cellulose pulp for hygiene products

    International Nuclear Information System (INIS)

    Kavitha Sankar, P.C.; Ramakrishnan, Reshmi; Rosemary, M.J.

    2016-01-01

    Cellulose pulp has a visible market share in personal hygiene products such as sanitary napkins and baby diapers. However it offers good surface for growth of microorganisms. Huge amount of research is going on in developing hygiene products that do not initiate microbial growth. The objective of the present work is to produce antibacterial cellulose pulp by depositing silver nanopowder on the cellulose fiber. The silver nanoparticles used were of less than 100 nm in size and were characterised using transmission electron microscopy and X-ray powder diffraction studies. Antibacterial activity of the functionalized cellulose pulp was proved by JIS L 1902 method. The in-vitro cytotoxicity, in-vivo vaginal irritation and intracutaneous reactivity studies were done with silver nanopowder incorporated cellulose pulp for introducing a new value added product to the market. Cytotoxicity evaluation suggested that the silver nanoparticle incorporated cellulose pulp is non-cytotoxic. No irritation and skin sensitization were identified in animals tested with specific extracts prepared from the test material in the in-vivo experiments. The results indicated that the silver nanopowder incorporated cellulose pulp meets the requirements of the standard practices recommended for evaluating the biological reactivity and has good biocompatibility, hence can be classified as a safe hygiene product. - Highlights: • Different amounts of silver nanoparticles (0.2 g–0.4 g/napkin) were added to cellulose pulp. • The silver nanoparticle incorporated cellulose pulp was proved to be antibacterial by JIS L 1902 method. • The minimum concentration of silver required for antibacterial activity with no cytotoxicity has been found out. • In-vivo vaginal irritation and intracutaneous reactivity studies confirmed the biocompatibility of the material.

  20. Tests of biological activity of metabolites from Penicillium expansum (Link Thom various isolates

    Directory of Open Access Journals (Sweden)

    Halina Borecka

    2013-12-01

    Full Text Available Aqrobacterium tumefaciens and cucumber, mustard and linseeds were compared as test organisms for evaluation of the biological activity of patulin. It was found that the reaction of cucumber seeds and linseed to the patulin concentrations was more pronounced than that of mustard and Aqrobacterium tumefaciens. The activity of metabolites produced by Penicillium expansum was investigated with the use of cucumber seeds. As measure of activity served the percentage of radicule growth inhibition was compared with the growth in control seeds. The biological activity of the metabolites was specific for the isolates, those from apples being more active. Thirty two isolates from pears and 34 from apples were examined.

  1. Biological-based and physical-based optimization for biological evaluation of prostate patient's plans

    Science.gov (United States)

    Sukhikh, E.; Sheino, I.; Vertinsky, A.

    2017-09-01

    Modern modalities of radiation treatment therapy allow irradiation of the tumor to high dose values and irradiation of organs at risk (OARs) to low dose values at the same time. In this paper we study optimal radiation treatment plans made in Monaco system. The first aim of this study was to evaluate dosimetric features of Monaco treatment planning system using biological versus dose-based cost functions for the OARs and irradiation targets (namely tumors) when the full potential of built-in biological cost functions is utilized. The second aim was to develop criteria for the evaluation of radiation dosimetry plans for patients based on the macroscopic radiobiological criteria - TCP/NTCP. In the framework of the study four dosimetric plans were created utilizing the full extent of biological and physical cost functions using dose calculation-based treatment planning for IMRT Step-and-Shoot delivery of stereotactic body radiation therapy (SBRT) in prostate case (5 fractions per 7 Gy).

  2. Chemical constituents and biological activities of two Iranian Cystoseira species.

    Science.gov (United States)

    Yegdaneh, Afsaneh; Ghannadi, Alireza; Dayani, Ladan

    2016-07-01

    The marine environment represents approximately half of the global biodiversity and could provide unlimited biological resources for the production of therapeutic drugs. Marine seaweeds comprise few thousands of species representing a considerable part of the littoral biomass. Extracts of the Cystoseira indica and Cystoseira merica were subjected to phytochemical and cytotoxicity evaluation. The amount of total phenol was determined with Folin-Ciocalteu reagent. Cytotoxicity was characterized by IC50 of human cancer cell lines including MCF-7 (human breast adenocarcinoma), HeLa (cervical carcinoma), and HT-29 (human colon adenocarcinoma) using Sulforhodamin assay. Antioxidant activities were evaluated using 2,2-diphenylpicrylhydrazyl (DPPH) method. The analysis revealed that tannins, saponins, sterols and triterpenes were the most abundant constituents in these Cystoseira species while cyanogenic and cardiac glycosides were the least ones. C. indica had the higher content of total phenolics and also showed higher antioxidant activity. Cytotoxic results showed that both species inhibited cell growth effectively, especially against MCF-7 cell line. The present findings suggest potential pharmacological applications of selected seaweeds but require further investigation and identification of their bioactive principles.

  3. Copper Nanoparticles: Synthesis and Biological Activity

    Science.gov (United States)

    Satyvaldiev, A. S.; Zhasnakunov, Z. K.; Omurzak, E.; Doolotkeldieva, T. D.; Bobusheva, S. T.; Orozmatova, G. T.; Kelgenbaeva, Z.

    2018-01-01

    By means of XRD and FESEM analysis, it is established that copper nanoparticles with sizes less than 10 nm are formed during the chemical reduction, which form aggregates mainly with spherical shape. Presence of gelatin during the chemical reduction of copper induced formation of smaller size distribution nanoparticles than that of nanoparticles synthesized without gelatin and it can be related to formation of protective layer. Synthesized Cu nano-powders have sufficiently high activity against the Erwinia amylovora bacterium, and the bacterial growth inhibition depends on the Cu nanoparticles concentration. At a concentration of 5 mg / ml of Cu nanoparticles, the exciter growth inhibition zone reaches a maximum value within 72 hours and the lysis zone is 20 mm, and at a concentration of 1 mg / ml this value is 16 mm, which also indicates the significant antibacterial activity of this sample.

  4. Biological activities of synthesized silver nanoparticles from ...

    Indian Academy of Sciences (India)

    ical scavenging activity was measured by the salicylic acid method [16]. The synthesized AgNPs solution at different concentrations (10 to 80 μg ml. −1. ) was dissolved in 1 ml of distilled water. One millilitre of AgNPs mixed with 1 ml of. 9 mM salicylic acid, 1 ml of 9 mM ferrous sulphate and 1ml of 9 mM hydrogen peroxide.

  5. Heterologous expression of biologically active chicken granulocyte ...

    African Journals Online (AJOL)

    user

    2012-02-07

    Feb 7, 2012 ... CD4+ T cells to enhance the ability of secreting antibody and also enhance the function of CD8+ T cells. (Papatriantafyllou, 2011; Tovey and Lallemand, 2010). GM-CSF also is a key regulator of IL-1beta production. Furthermore, It was reported that GM-CSF play a key role in the activation of Th1 and Th17 ...

  6. Physical aspects of biological activity and cancer

    Science.gov (United States)

    Pokorný, Jiří

    2012-03-01

    Mitochondria are organelles at the boundary between chemical-genetic and physical processes in living cells. Mitochondria supply energy and provide conditions for physical mechanisms. Protons transferred across the inner mitochondrial membrane diffuse into cytosol and form a zone of a strong static electric field changing water into quasi-elastic medium that loses viscosity damping properties. Mitochondria and microtubules form a unique cooperating system in the cell. Microtubules are electrical polar structures that make possible non-linear transformation of random excitations into coherent oscillations and generation of coherent electrodynamic field. Mitochondria supply energy, may condition non-linear properties and low damping of oscillations. Electrodynamic activity might have essential significance for material transport, organization, intra- and inter-cellular interactions, and information transfer. Physical processes in cancer cell are disturbed due to suppression of oxidative metabolism in mitochodria (Warburg effect). Water ordering level in the cell is decreased, excitation of microtubule electric polar oscilations diminished, damping increased, and non-linear energy transformation shifted towards the linear region. Power and coherence of the generated electrodynamic field are reduced. Electromagnetic activity of healthy and cancer cells may display essential differences. Local invasion and metastastatic growth may strongly depend on disturbed electrodynamic activity. Nanotechnological measurements may disclose yet unknown properties and parameters of electrodynamic oscillations and other physical processes in healthy and cancer cells.

  7. An Evaluation of the Biological Availability of Chloramphenicol ...

    African Journals Online (AJOL)

    The biological availability of chloramphenicol from different commercial preparations was investigated. Methods used to evaluate the in vitro release were disintegration, de-aggregation and dissolution tests and particle size measurement. Considerable differences between the rate of release of the antibiotic from the ...

  8. Evaluating Biology Achievement Scores in an ICT Integrated PBL Environment

    Science.gov (United States)

    Osman, Kamisah; Kaur, Simranjeet Judge

    2014-01-01

    Students' achievement in Biology is often looked up as a benchmark to evaluate the mode of teaching and learning in higher education. Problem-based learning (PBL) is an approach that focuses on students' solving a problem through collaborative groups. There were eighty samples involved in this study. The samples were divided into three groups: ICT…

  9. Saponins from Swartzia langsdorffii: biological activities

    Directory of Open Access Journals (Sweden)

    Magalhães Aderbal Farias

    2003-01-01

    Full Text Available The presence of saponins and the molluscicidal activity of the roots, leaves, seeds and fruits of Swartzia langsdorffii Raddi (Leguminosae against Biomphalaria glabrata adults and eggs were investigated. The roots, seeds and fruits were macerated in 95% ethanol. These extracts exerted a significant molluscicidal activity against B. glabrata, up to a dilution of 100 mg/l. Four mixtures (A2, B2, C and D of triterpenoid oleanane type saponins were chromatographically isolated from the seed and fruit extracts. Two known saponins (1 and 2 were identified as beta-D-glucopyranosyl-[alpha-L-rhamnopyranosyl-(1->3- beta-D-glucuronopyranosyl-(1->3]-3beta-hydroxyolean-12-ene-28 -oate, and beta-D-glucopyranosyl-(1->3-beta-D-glucuronopyranosyl-(1 ->3]-3beta-hydroxyolean-12-ene-28-oate, respectively. These two saponins were present in all the mixtures, together with other triterpenoid oleane type saponins, which were shown to be less polar, by reversed-phase HPLC. The saponin identifications were based on spectral evidence, including ¹H-¹H two-dimensional correlation spectroscopy, nuclear Overhauser and exchange spectroscopy, heteronuclear multiple quantum coherence, and heteronuclear multiple-bond connectivity experiments. The toxicity of S. langsdorffii saponins to non-target organisms was prescreened by the brine shrimp lethality test.

  10. Biologically active extracts with kidney affections applications

    Science.gov (United States)

    Pascu (Neagu), Mihaela; Pascu, Daniela-Elena; Cozea, Andreea; Bunaciu, Andrei A.; Miron, Alexandra Raluca; Nechifor, Cristina Aurelia

    2015-12-01

    This paper is aimed to select plant materials rich in bioflavonoid compounds, made from herbs known for their application performances in the prevention and therapy of renal diseases, namely kidney stones and urinary infections (renal lithiasis, nephritis, urethritis, cystitis, etc.). This paper presents a comparative study of the medicinal plant extracts composition belonging to Ericaceae-Cranberry (fruit and leaves) - Vaccinium vitis-idaea L. and Bilberry (fruit) - Vaccinium myrtillus L. Concentrated extracts obtained from medicinal plants used in this work were analyzed from structural, morphological and compositional points of view using different techniques: chromatographic methods (HPLC), scanning electronic microscopy, infrared, and UV spectrophotometry, also by using kinetic model. Liquid chromatography was able to identify the specific compounds of the Ericaceae family, present in all three extracts, arbutosid, as well as specific components of each species, mostly from the class of polyphenols. The identification and quantitative determination of the active ingredients from these extracts can give information related to their therapeutic effects.

  11. Biologically active extracts with kidney affections applications

    International Nuclear Information System (INIS)

    Pascu, Mihaela; Pascu, Daniela-Elena; Cozea, Andreea; Bunaciu, Andrei A.; Miron, Alexandra Raluca; Nechifor, Cristina Aurelia

    2015-01-01

    Highlights: • The paper highlighted the compositional similarities and differences between the three extracts of bilberry and cranberry fruit derived from the same Ericaceae family. • A method of antioxidant activity, different cellulose membranes, a Whatman filter and Langmuir – kinetic model were used. • Arbutoside presence in all three extracts of bilberry and cranberry fruit explains their use in urinary infections – cystitis and colibacillosis. • Following these research studies, it was established that the fruits of bilberry and cranberry (fruit and leaves) significantly reduce the risk of urinary infections, and work effectively to protect against free radicals and inflammation. - Abstract: This paper is aimed to select plant materials rich in bioflavonoid compounds, made from herbs known for their application performances in the prevention and therapy of renal diseases, namely kidney stones and urinary infections (renal lithiasis, nephritis, urethritis, cystitis, etc.). This paper presents a comparative study of the medicinal plant extracts composition belonging to Ericaceae-Cranberry (fruit and leaves) – Vaccinium vitis-idaea L. and Bilberry (fruit) – Vaccinium myrtillus L. Concentrated extracts obtained from medicinal plants used in this work were analyzed from structural, morphological and compositional points of view using different techniques: chromatographic methods (HPLC), scanning electronic microscopy, infrared, and UV spectrophotometry, also by using kinetic model. Liquid chromatography was able to identify the specific compounds of the Ericaceae family, present in all three extracts, arbutosid, as well as specific components of each species, mostly from the class of polyphenols. The identification and quantitative determination of the active ingredients from these extracts can give information related to their therapeutic effects.

  12. Biologically active extracts with kidney affections applications

    Energy Technology Data Exchange (ETDEWEB)

    Pascu, Mihaela, E-mail: mihhaela_neagu@yahoo.com [SC HOFIGAL S.A., Analytical Research Department, 2 Intr. Serelor, Bucharest-4 042124 (Romania); Politehnica University of Bucharest, Faculty of Applied Chemistry and Material Science, 1-5 Polizu Street, 11061 Bucharest (Romania); Pascu, Daniela-Elena [Politehnica University of Bucharest, Faculty of Applied Chemistry and Material Science, 1-5 Polizu Street, 11061 Bucharest (Romania); Cozea, Andreea [SC HOFIGAL S.A., Analytical Research Department, 2 Intr. Serelor, Bucharest-4 042124 (Romania); Transilvania University of Brasov, Faculty of Food and Tourism, 148 Castle Street, 500036 Brasov (Romania); Bunaciu, Andrei A. [SCIENT – Research Center for Instrumental Analysis, S.C. CROMATEC-PLUS S.R.L., 18 Sos. Cotroceni, Bucharest 060114 (Romania); Miron, Alexandra Raluca; Nechifor, Cristina Aurelia [Politehnica University of Bucharest, Faculty of Applied Chemistry and Material Science, 1-5 Polizu Street, 11061 Bucharest (Romania)

    2015-12-15

    Highlights: • The paper highlighted the compositional similarities and differences between the three extracts of bilberry and cranberry fruit derived from the same Ericaceae family. • A method of antioxidant activity, different cellulose membranes, a Whatman filter and Langmuir – kinetic model were used. • Arbutoside presence in all three extracts of bilberry and cranberry fruit explains their use in urinary infections – cystitis and colibacillosis. • Following these research studies, it was established that the fruits of bilberry and cranberry (fruit and leaves) significantly reduce the risk of urinary infections, and work effectively to protect against free radicals and inflammation. - Abstract: This paper is aimed to select plant materials rich in bioflavonoid compounds, made from herbs known for their application performances in the prevention and therapy of renal diseases, namely kidney stones and urinary infections (renal lithiasis, nephritis, urethritis, cystitis, etc.). This paper presents a comparative study of the medicinal plant extracts composition belonging to Ericaceae-Cranberry (fruit and leaves) – Vaccinium vitis-idaea L. and Bilberry (fruit) – Vaccinium myrtillus L. Concentrated extracts obtained from medicinal plants used in this work were analyzed from structural, morphological and compositional points of view using different techniques: chromatographic methods (HPLC), scanning electronic microscopy, infrared, and UV spectrophotometry, also by using kinetic model. Liquid chromatography was able to identify the specific compounds of the Ericaceae family, present in all three extracts, arbutosid, as well as specific components of each species, mostly from the class of polyphenols. The identification and quantitative determination of the active ingredients from these extracts can give information related to their therapeutic effects.

  13. Synthesis, analysis and biological evaluation of new RGD mimetics

    Czech Academy of Sciences Publication Activity Database

    Balacheva, A. A.; Lambev, M. K.; Pashov, I.; Detcheva, R. L.; Sázelová, Petra; Momekov, G. Ts.; Kašička, Václav; Pajpanova, T. I.; Golovinsky, E. V.

    2017-01-01

    Roč. 49, SI E (2017), s. 7-10 ISSN 0324-1130. [Bulgarian Peptide Symposium /7./. Blagoevgrad, 10.06.2016-12.06.2016] Institutional support: RVO:61388963 Keywords : RGD * biologically active peptides * cytotoxicity Subject RIV: CB - Analytical Chemistry, Separation OBOR OECD: Analytical chemistry Impact factor: 0.238, year: 2016

  14. Zoanthid mucus as new source of useful biologically active proteins.

    Science.gov (United States)

    Guarnieri, Míriam Camargo; de Albuquerque Modesto, Jeanne Claíne; Pérez, Carlos Daniel; Ottaiano, Tatiana Fontes; Ferreira, Rodrigo da Silva; Batista, Fabrício Pereira; de Brito, Marlon Vilela; Campos, Ikaro Henrique Mendes Pinto; Oliva, Maria Luiza Vilela

    2018-03-01

    Palythoa caribaeorum is a very common colonial zoanthid in the coastal reefs of Brazil. It is known for its massive production of mucus, which is traditionally used in folk medicine by fishermen in northeastern Brazil. This study identified biologically active compounds in P. caribaerum mucus. Crude mucus was collected during low tides by the manual scraping of colonies; samples were maintained in an ice bath, homogenized, and centrifuged at 16,000 g for 1 h at 4 °C; the supernatant (mucus) was kept at -80 °C until use. The enzymatic (proteolytic and phospholipase A 2 ), inhibitory (metallo, cysteine and serine proteases), and hemagglutinating (human erythrocyte) activities were determined. The results showed high levels of cysteine and metallo proteases, intermediate levels of phosholipase A 2 , low levels of trypsin, and no elastase and chymotrypsin like activities. The mucus showed potent inhibitory activity on snake venom metalloproteases and cysteine proteinase papain. In addition, it showed agglutinating activity towards O + , B + , and A + erythrocyte types. The hemostatic results showed that the mucus prolongs the aPTT and PT, and strongly inhibited platelet aggregation induced by arachidonic acid, collagen, epinephrine, ADP, and thrombin. The antimicrobial activity was tested on 15 strains of bacteria and fungi through the radial diffusion assay in agar, and no activity was observed. Compounds in P. caribaeorum mucus were analyzed for the first time in this study, and our results show potential pharmacological activities in these compounds, which are relevant for use in physiopathological investigations. However, the demonstration of these activities indicates caution in the use of crude mucus in folk medicine. Furthermore, the present or absent activities identified in this mucus suggest that the studied P. caribaeorum colonies were in thermal stress conditions at the time of sample collection; these conditions may precede the bleaching

  15. [Oregano: properties, composition and biological activity].

    Science.gov (United States)

    Arcila-Lozano, Cynthia Cristina; Loarca-Piña, Guadalupe; Lecona-Uribe, Salvador; González de Mejía, Elvira

    2004-03-01

    The oregano spice includes various plant species. The most common are the genus Origanum, native of Europe, and the Lippia, native of Mexico. Among the species of Origanum. their most important components are the limonene, gamma-cariofilene, rho-cymenene, canfor, linalol, alpha-pinene, carvacrol and thymol. In the genus Lippia, the same compounds can be found. The oregano composition depends on the specie, climate, altitude, time of recollection and the stage of growth. Some of the properties of this plant's extracts are being currently studied due to the growing interest for substituting synthetic additives commonly found in foods. Oregano has a good antioxidant capacity and also presents antimicrobial activity against pathogenic microorganisms like Salmonella typhimurium, Escherichia coli, Staphylococcus aureus, Staphylococcus epidermidis, among others. These are all characteristics of interest for the food industry because they may enhance the safety and stability of foods. There are also some reports regarding the antimutagenic and anticarcinogenic effect of oregano; representing an alternative for the potential treatment and/or prevention of certain chronic ailments, like cancer.

  16. Azaglycomimetics: Natural Occurrence, Biological Activity, and Application

    Science.gov (United States)

    Asano, Naoki

    A large number of alkaloids mimicking the structures of monosaccharides or oligosaccharides have been isolated from plants and microorganisms. The sugar mimicking alkaloids with a nitrogen in the ring are called azasugars or iminosugars. Naturally occurring azasugars are classified into five structural classes: polyhydroxylated piperidines, pyrrolidines, indolizidines, pyrrolizidines, and nortropanes. They are easily soluble in water because of their polyhydroxylated structures and inhibit glycosidases because of a structural resemblance to the sugar moiety of the natural substrate. Glycosidases are involved in a wide range of anabolic and catabolic processes, such as digestion, lysosomal catabolism of glycoconjugates, biosynthesis of glycoproteins, and the endoplasmic reticulum (ER) quality control and ER-associated degradation of glycoproteins. Hence, modifying or blocking these processes in vivo by inhibitors is of great interest from a therapeutic point of view. Azasugars are an important class of glycosidase inhibitors and are arousing great interest for instance as antidiabetics, antiobesity drugs, antivirals, and therapeutic agents for some genetic disorders. This review describes the recent studies on isolation, characterization, glycosidase inhibitory activity, and therapeutic application of azaglycomimetics.

  17. Evaluating Biological Claims to Enhance Critical Thinking through Position Statements

    Directory of Open Access Journals (Sweden)

    Tracie M. Addy

    2013-11-01

    Full Text Available Critical thinking is an important skill for undergraduates to learn, yet rarely is it formally taught in the classroom. Here we explain how critical thinking can be fostered within an undergraduate biology course by encouraging students to evaluate biological claims related to current topics within the course. We found that with the completion of two writing assignments within a four-week period, students demonstrated a significantly greater ability to analyze the evidence within the claims. These results support the notion that even short-term learning experiences focused upon critical thinking can enhance students’ skills beyond discipline-specific knowledge.

  18. Comparative study of biological activity of glutathione, sodium ...

    African Journals Online (AJOL)

    Glutathione (GSH) and sodium tungstate (Na2WO4) are important pharmacological agents. They provide protection to cells against cytotoxic agents and thus reduce their cytotoxicity. It was of interest to study the biological activity of these two pharmacological active agents. Different strains of bacteria were used and the ...

  19. Assessing Student Behaviors and Motivation for Actively Learning Biology

    Science.gov (United States)

    Moore, Michael Edward

    2017-01-01

    Vision and Change states that one of the major changes in the way we design biology courses should be a switch in approach from teacher-centered learning to student-centered learning and identifies active learning as a recommended methods. Studies show performance benefits for students taking courses that use active learning. What is unknown is…

  20. Multifunctional biomaterial coatings: synthetic challenges and biological activity.

    Science.gov (United States)

    Pagel, Mareen; Beck-Sickinger, Annette G

    2017-01-01

    A controlled interaction of materials with their surrounding biological environment is of great interest in many fields. Multifunctional coatings aim to provide simultaneous modulation of several biological signals. They can consist of various combinations of bioactive, and bioinert components as well as of reporter molecules to improve cell-material contacts, prevent infections or to analyze biochemical events on the surface. However, specific immobilization and particular assembly of various active molecules are challenging. Herein, an overview of multifunctional coatings for biomaterials is given, focusing on synthetic strategies and the biological benefits by displaying several motifs.

  1. SYNTHESIS, REACTIVITY AND BIOLOGICAL ACTIVITY OF QUINOXALIN-2-ONE DERIVATIVES

    Directory of Open Access Journals (Sweden)

    El Mokhtar Essassi

    2010-04-01

    Full Text Available Quinoxalines have a great interest in various fields and particularly in chemistry, biology and pharmacology. It enabled the researchers to develop many methods for their preparations and to seek new fields of application. In this review, we’ll expose different methods of synthesis of the quinoxalin-2-one, its reactivity and finally we’ll discuss the various biological activities of its derivatives.

  2. Synthesis and characterization of some metal complexes derived from azo compound of 4,4‧-methylenedianiline and antipyrine: Evaluation of their biological activity on some land snail species

    Science.gov (United States)

    AbouEl-Enein, Saeyda A.; Emam, Sanaa M.; Polis, Magdy W.; Emara, Esam M.

    2015-11-01

    A novel series of metal complexes of the azo dye; bis-(1,5-dimethyl-4-[(E)-(3-methylphenyl)diazenyl]-2-phenyl-1,2-dihydro-3H-pyrazol-3-one) derived from 4,4‧-methylenedianiline and antipyrine was synthesized and characterized by different spectral, thermal and analytical methods. The tetradentate ligand reacts with the metal ions as a half unit. All complexes display an octahedral geometry, except Pd(II) complex (7) which has a square planar one. The thermal studies reveal that the complexes have higher thermal stability comparable with that of the free ligand. The activation thermodynamic parameters, such as activation energy (E*), enthalpy of activation (ΔH*), entropy of activation (ΔS*) and Gibbs free energy (ΔG*) have been calculated using DTG curves. The ESR spectra of the solid Cu(II) complexes showed an axial symmetry with 2B1g as a ground state and hyperfine structure. The biological activities of the ligand, as well as its metal complexes have been tested in vitro against two land snail species; Eobania vermiculata and Monacha obstructa. The results show that all the tested compounds have significant biological activities against the two tested land snail species with different sensitivity levels.

  3. Pomegranate Fruit as a Rich Source of Biologically Active Compounds

    Science.gov (United States)

    Sreekumar, Sreeja; Sithul, Hima; Muraleedharan, Parvathy; Azeez, Juberiya Mohammed; Sreeharshan, Sreeja

    2014-01-01

    Pomegranate is a widely used plant having medicinal properties. In this review, we have mainly focused on the already published data from our laboratory pertaining to the effect of methanol extract of pericarp of pomegranate (PME) and have compared it with other relevant literatures on Punica. Earlier, we had shown its antiproliferative effect using human breast (MCF-7, MDA MB-231), and endometrial (HEC-1A), cervical (SiHa, HeLa), and ovarian (SKOV3) cancer cell lines, and normal breast fibroblasts (MCF-10A) at concentration of 20–320 μg/mL. The expressions of selected estrogen responsive genes (PR, pS2, and C-Myc) were downregulated by PME. Unlike estradiol, PME did not increase the uterine weight and proliferation in bilaterally ovariectomized Swiss-Albino mice models and its cardioprotective effects were comparable to that of 17β-estradiol. We had further assessed the protective role of PME on skeletal system, using MC3T3-E1 cells. The results indicated that PME (80 μg/mL) significantly increased ALP (Alkaline Phosphatase) activity, supporting its suggested role in modulating osteoblastic cell differentiation. The antiosteoporotic potential of PME was also evaluated in ovariectomized (OVX) rodent model. The results from our studies and from various other studies support the fact that pomegranate fruit is indeed a source of biologically active compounds. PMID:24818149

  4. Phenolic Compounds Characterization and Biological Activities of Citrus aurantium Bloom

    Directory of Open Access Journals (Sweden)

    Armin Oskoueian

    2012-01-01

    Full Text Available Citrus plants are known to possess beneficial biological activities for human health. In addition, ethnopharmacological application of plants is a good tool to explore their bioactivities and active compounds. This research was carried out to evaluate the phenolic and flavonoid analysis, antioxidant properties, anti inflammatory and anti cancer activity of Citrus aurantium bloom. The total phenolics and flavonoids results revealed that methanolic extract contained high total phenolics and flavonoids compared to ethanolic and boiling water extracts. The obtained total phenolics value for methanolic Citrus aurantium bloom extract was 4.55 ± 0.05 mg gallic acid equivalent (GAE/g dry weight (DW, and for total flavonoids it was 3.83 ± 0.05 mg rutin equivalent/g DW. In addition, the RP-HPLC analyses of phenolics and flavonoids indicated the presence of gallic acid, pyrogallol, syringic acid, caffeic acid, rutin, quercetin and naringin as bioactive compounds. The antioxidant activity of Citrus aurantium bloom were examined by the 1,1-diphenyl-2-picryl-hydrazyl (DPPH assay and the ferric reducing/antioxidant potential (FRAP. The free radical scavenging and ferric reducing power activities were higher for the methanolic extract of Citrus aurantium bloom at a concentration of 300 μg/mL, with values of 55.3% and 51.7%, respectively, as compared to the corresponding boiling water and ethanolic extracts, but the activities were lower than those of antioxidant standards such as BHT and α-tocopherol. Furthermore, the anti-inflammatory result of methanolic extract showed appreciable reduction in nitric oxide production of stimulated RAW 264.7 cells at the presence of plant extract. Apart from that, the anticancer activity of the methanolic extract was investigated in vitro against human cancer cell lines (MCF-7; MDA-MB-231, human colon adenocarcinoma (HT-29 and Chang cell as a normal human hepatocyte. The obtained result demonstrated the moderate to

  5. Phenolic compounds characterization and biological activities of Citrus aurantium bloom.

    Science.gov (United States)

    Karimi, Ehsan; Oskoueian, Ehsan; Hendra, Rudi; Oskoueian, Armin; Jaafar, Hawa Z E

    2012-01-30

    Citrus plants are known to possess beneficial biological activities for human health. In addition, ethnopharmacological application of plants is a good tool to explore their bioactivities and active compounds. This research was carried out to evaluate the phenolic and flavonoid analysis, antioxidant properties, anti inflammatory and anti cancer activity of Citrus aurantium bloom. The total phenolics and flavonoids results revealed that methanolic extract contained high total phenolics and flavonoids compared to ethanolic and boiling water extracts. The obtained total phenolics value for methanolic Citrus aurantium bloom extract was 4.55 ± 0.05 mg gallic acid equivalent (GAE)/g dry weight (DW), and for total flavonoids it was 3.83 ± 0.05 mg rutin equivalent/g DW. In addition, the RP-HPLC analyses of phenolics and flavonoids indicated the presence of gallic acid, pyrogallol, syringic acid, caffeic acid, rutin, quercetin and naringin as bioactive compounds. The antioxidant activity of Citrus aurantium bloom were examined by the 1,1-diphenyl-2-picryl-hydrazyl (DPPH) assay and the ferric reducing/antioxidant potential (FRAP). The free radical scavenging and ferric reducing power activities were higher for the methanolic extract of Citrus aurantium bloom at a concentration of 300 μg/mL, with values of 55.3% and 51.7%, respectively, as compared to the corresponding boiling water and ethanolic extracts, but the activities were lower than those of antioxidant standards such as BHT and α-tocopherol. Furthermore, the anti-inflammatory result of methanolic extract showed appreciable reduction in nitric oxide production of stimulated RAW 264.7 cells at the presence of plant extract. Apart from that, the anticancer activity of the methanolic extract was investigated in vitro against human cancer cell lines (MCF-7; MDA-MB-231), human colon adenocarcinoma (HT-29) and Chang cell as a normal human hepatocyte. The obtained result demonstrated the moderate to appreciable

  6. Evaluation of Botanical Reference Materials for the Determination of Vanadium in Biological Samples

    DEFF Research Database (Denmark)

    Heydorn, Kaj; Damsgaard, Else

    1982-01-01

    Three botanical reference materials prepared by the National Bureau of Standards have been studied by neutron activation analysis to evaluate their suitability with respect to the determination of vanadium in biological samples. Various decomposition methods were applied in connection with chemical...

  7. Acute toxicity and chemical evaluation of coking wastewater under biological and advanced physicochemical treatment processes.

    Science.gov (United States)

    Dehua, Ma; Cong, Liu; Xiaobiao, Zhu; Rui, Liu; Lujun, Chen

    2016-09-01

    This study investigated the changes of toxic compounds in coking wastewater with biological treatment (anaerobic reactor, anoxic reactor and aerobic-membrane bioreactor, A1/A2/O-MBR) and advanced physicochemical treatment (Fenton oxidation and activated carbon adsorption) stages. As the biological treatment stages preceding, the inhibition effect of coking wastewater on the luminescence of Vibrio qinghaiensis sp. Nov. Q67 decreased. Toxic units (TU) of coking wastewater were removed by A1/A2/O-MBR treatment process, however approximately 30 % TU remained in the biologically treated effluent. There is a tendency that fewer and fewer residual organic compounds could exert equal acute toxicity during the biological treatment stages. Activated carbon adsorption further removed toxic pollutants of biologically treated effluent but the Fenton effluent increased acute toxicity. The composition of coking wastewater during the treatment was evaluated using the three-dimensional fluorescence spectra, gas chromatography-mass spectrometry (GC-MS). The organic compounds with high polarity were the main cause of acute toxicity in the coking wastewater. Aromatic protein-like matters in the coking wastewater with low biodegradability and high toxicity contributed mostly to the remaining acute toxicity of the biologically treated effluents. Chlorine generated from the oxidation process was responsible for the acute toxicity increase after Fenton oxidation. Therefore, the incorporation of appropriate advanced physicochemical treatment process, e.g., activated carbon adsorption, should be implemented following biological treatment processes to meet the stricter discharge standards and be safer to the environment.

  8. Evaluation of the Materials Developed For Biology Teaching

    Directory of Open Access Journals (Sweden)

    İ. Ümit YAPICI

    2013-12-01

    Full Text Available The aim of this study is to evaluate the course materials developed for biology teaching in Instructional Technologies and Material Design course by the pre-service biology teachers. The research group consist of 34 students who attending Instructional Technologies and Material Design course and studying at Department of Biology Education of Ziya Gökalp Education Faculty in Dicle University. The evaluation questionnaire which includes 17 items developed by İşman (2008 was used as data collection tool. Materials are organized as follows: Classical Educational Technologies 1 (black board, white board, magnetic board, swivel plate, etc.; Classical Educational Technologies 2 (graphics, modelsampling, posters, etc..; Modern Educational Technologies (video-TV, overhead projector, data projector, smart board, etc.. The findings of the means as follows: Classical Education Technology 1 X = 3.62; Classic Educational Technology 2 X = 3.64, respectively Modern Education Technology X = 3.81. As a result, pe-service biology teachers’ views about Modern Education Technology were more positive. Technology laboratories can be established for the students to prepare the materials. Also; the course time can be increased

  9. Biological activity of antitumoural MGBG: the structural variable.

    Science.gov (United States)

    Marques, M P M; Gil, F P S C; Calheiros, R; Battaglia, V; Brunati, A M; Agostinelli, E; Toninello, A

    2008-05-01

    The present study aims at determining the structure-activity relationships (SAR's) ruling the biological function of MGBG (methylglyoxal bis(guanylhydrazone)), a competitive inhibitor of S-adenosyl-L-methionine decarboxylase displaying anticancer activity, involved in the biosynthesis of the naturally occurring polyamines spermidine and spermine. In order to properly understand its biochemical activity, MGBG's structural preferences at physiological conditions were ascertained, by quantum mechanical (DFT) calculations.

  10. Mineralogical characteristics of the silica polymorphs in relation to their biological activities

    Energy Technology Data Exchange (ETDEWEB)

    Guthrie, G.D. Jr. [Los Alamos National Lab., NM (United States); Heaney, P.J. [Princeton Univ., NJ (United States). Dept. of Geological and Geophysical Sciences

    1993-10-01

    Numerous aspects of minerals (including the silica polymorphs) can effect their biological activities. These include periodic structures, compositional variations, dissolution characteristics, surface properties, and particle size/shape. In order to understand mineral-induced pathogenesis in a mechanistic way, the links between these properties and biochemical processes must be elucidated. This paper presents some of the basic properties of the silica polymorphs that may relate to pathogenicity and mineralogical strategies for designing biological assays to evaluate these properties.

  11. Evaluation Of Webquest In Biology:Teachers’ Perception

    Directory of Open Access Journals (Sweden)

    Kamisah OSMAN

    2014-01-01

    Full Text Available Teaching and learning based on web or web-based learning is a concept which integrates information and technology in education. Teachers and instructors have to assist their learners to learn to function in this information environment. However, teacher trainers and instructors have limited experience in the integration of ICT by using web in their teaching, mainly for Biology subject. The Indonesian Ministry of Education has started to implement ICT in the process of learning and teaching. Hence, it geared our attention to evaluate the suitability of WebQuest to be used in teacher training among Biology teachers in central Kalimantan. Results showed those teachers’ perceptions towards WebQuest on technical, content, as well as teaching and learning structure were on the high level. However, there was no significant difference on teachers’ perception towards WebQuest based on their experience. Further evaluation study should be done on students to gauge their perception towards the WebQuest.

  12. Secondary metabolites in grasses: characterization and biological activity

    Directory of Open Access Journals (Sweden)

    Aldo Tava

    2007-12-01

    Full Text Available In a series of studies dealing on the nutritional value of forage species, more attention was focussed on several compounds, named secondary metabolites, that are important in determining nutritional characteristics. Secondary metabolites are compounds detected in the green materials in low concentration compared to primary metabolites (proteins, sugars, lipids, fibers, but of fundamental importance for the plant physiology. The possess several biological activities and this contribute to their possible pharmacological use. In the present paper studies on secondary metabolites from herbaceous plants are reviewed. Indications of the chemical methods used for their analyses, their presence in the green material and their biological activity are also reported.

  13. Secondary metabolites in grasses: characterization and biological activity

    Directory of Open Access Journals (Sweden)

    Aldo Tava

    2011-02-01

    Full Text Available In a series of studies dealing on the nutritional value of forage species, more attention was focussed on several compounds, named secondary metabolites, that are important in determining nutritional characteristics. Secondary metabolites are compounds detected in the green materials in low concentration compared to primary metabolites (proteins, sugars, lipids, fibers, but of fundamental importance for the plant physiology. The possess several biological activities and this contribute to their possible pharmacological use. In the present paper studies on secondary metabolites from herbaceous plants are reviewed. Indications of the chemical methods used for their analyses, their presence in the green material and their biological activity are also reported.

  14. Biological Activity of Curcuminoids Isolated from Curcuma longa

    Directory of Open Access Journals (Sweden)

    Simay Çıkrıkçı

    2008-04-01

    Full Text Available Curcumin is the most important fraction of turmeric which is responsible for its biological activity. In this study, isolation and biological assessment of turmeric and curcumin have been discussed against standard bacterial and mycobacterial strains such as E.coli , S.aureus, E.feacalis, P.aeuroginosa, M.smegmatis, M.simiae, M.kansasii, M. terrae, M.szulgai and the fungi Candida albicans. The antioxidant activity of curcumin and turmeric were also determined by the CUPRAC method.

  15. Fabrication, Characterization, and Biological Activity of Avermectin Nano-delivery Systems with Different Particle Sizes

    Science.gov (United States)

    Wang, Anqi; Wang, Yan; Sun, Changjiao; Wang, Chunxin; Cui, Bo; Zhao, Xiang; Zeng, Zhanghua; Yao, Junwei; Yang, Dongsheng; Liu, Guoqiang; Cui, Haixin

    2018-01-01

    Nano-delivery systems for the active ingredients of pesticides can improve the utilization rates of pesticides and prolong their control effects. This is due to the nanocarrier envelope and controlled release function. However, particles containing active ingredients in controlled release pesticide formulations are generally large and have wide size distributions. There have been limited studies about the effect of particle size on the controlled release properties and biological activities of pesticide delivery systems. In the current study, avermectin (Av) nano-delivery systems were constructed with different particle sizes and their performances were evaluated. The Av release rate in the nano-delivery system could be effectively controlled by changing the particle size. The biological activity increased with decreasing particle size. These results suggest that Av nano-delivery systems can significantly improve the controllable release, photostability, and biological activity, which will improve efficiency and reduce pesticide residues.

  16. Synthesis and Biological Evaluation of 7-Deoxy-Epothilone Analogues

    Directory of Open Access Journals (Sweden)

    Laura M. Woods

    2017-03-01

    Full Text Available The synthesis of two deoxygenated analogues of potent epothilones is reported in an effort to analyze the relative importance of molecular conformation and ligand–target interactions to biological activity. 7-deoxy-epothilone D and 7-deoxy-(S-14-methoxy-epothilone D were prepared through total synthesis and shown to maintain the conformational preferences of their biologically active parent congeners through computer modeling and nuclear magnetic resonance (NMR studies. The significant decrease in observed potency for each compound suggests that a hydrogen bond between the C7-hydroxyl group and the tubulin binding site plays a critical role in the energetics of binding in the epothilone class of polyketides.

  17. Gemini ester quat surfactants and their biological activity.

    Science.gov (United States)

    Łuczyński, Jacek; Frąckowiak, Renata; Włoch, Aleksandra; Kleszczyńska, Halina; Witek, Stanisław

    2013-03-01

    Cationic gemini surfactants are an important class of surface-active compounds that exhibit much higher surface activity than their monomeric counterparts. This type of compound architecture lends itself to the compound being easily adsorbed at interfaces and interacting with the cellular membranes of microorganisms. Conventional cationic surfactants have high chemical stability but poor chemical and biological degradability. One of the main approaches to the design of readily biodegradable and environmentally friendly surfactants involves inserting a bond with limited stability into the surfactant molecule to give a cleavable surfactant. The best-known example of such a compound is the family of ester quats, which are cationic surfactants with a labile ester bond inserted into the molecule. As part of this study, a series of gemini ester quat surfactants were synthesized and assayed for their biological activity. Their hemolytic activity and changes in the fluidity and packing order of the lipid polar heads were used as the measures of their biological activity. A clear correlation between the hemolytic activity of the tested compounds and their alkyl chain length was established. It was found that the compounds with a long hydrocarbon chain showed higher activity. Moreover, the compounds with greater spacing between their alkyl chains were more active. This proves that they incorporate more easily into the lipid bilayer of the erythrocyte membrane and affect its properties to a greater extent. A better understanding of the process of cell lysis by surfactants and of their biological activity may assist in developing surfactants with enhanced selectivity and in widening their range of application.

  18. Continuous Vigilance - Evaluating Preparedness for a Biological Event

    Directory of Open Access Journals (Sweden)

    Bruria eAdini

    2014-04-01

    Full Text Available Objective: Effective response to biological events necessitates ongoing evaluation of preparedness. This study was a bilateral German-Israeli collaboration aimed at developing an evaluation tool for assessing preparedness of medical facilities for biological events.Methods: Measurable parameters were identified through a literature review for inclusion in the evaluation tool and disseminated to 228 content experts in 2 modified Delphi cycles. Focus groups were conducted to identify psychosocial needs of the medical teams. Table top and functional exercises were implemented to review applicability of the tool. Results: 117 experts from Germany and Israel participated in the modified Delphi. Out of 188 parameters that were identified, 183 achieved a consensus of >75% of the content experts. Following comments recommended in the Delphi cycles, and feedback from focus groups and hospital exercises, the final tool consisted of 172 parameters. Median level of importance of each parameter was calculated based on ranking recommended in the Delphi process. Computerized web-based software was developed to calculate scores of preparedness for biological events.Conclusions: Ongoing evaluation means, such as the tool developed in the study, can facilitate the need for a valid and reliable mechanism that may be widely adopted and implemented as quality assurance measures. The tool is based on measurable parameters and indicators that can effectively present strengths and weaknesses in managing a response to a public health threat, and accordingly, steps can be implemented to improve readiness. Adoption of such a tool is an important component of assuring public health and effective emergency management.Contact person regarding the evaluation tool: adinib@bgu.ac.ilLink to the computerized tool: http://www.be-prep.com/us

  19. Evaluation of nuclear reactor based activation analysis techniques

    International Nuclear Information System (INIS)

    Obrusnik, I.; Kucera, J.

    1977-09-01

    A survey is presented of the basic types of activation analysis applied in environmental control. Reactor neutron activation analysis is described (including the reactor as a neutron source, sample activation in the reactor, methodology of neutron activation analysis, sample transport into the reactor and sample packaging after irradiation, instrumental activation analysis with radiochemical separation, data measurement and evaluation, sampling and sample preparation). Sources of environmental contamination with trace elements, sampling and sample analysis by neutron activation are described. The analysis is described of soils, waters and biological materials. Methods are shown of evaluating neutron activation analysis results and of their interpretation for purposes of environmental control. (J.B.)

  20. Evaluation of a commercial biologically based IMRT treatment planning system

    International Nuclear Information System (INIS)

    Semenenko, Vladimir A.; Reitz, Bodo; Day, Ellen; Qi, X. Sharon; Miften, Moyed; Li, X. Allen

    2008-01-01

    A new inverse treatment planning system (TPS) for external beam radiation therapy with high energy photons is commercially available that utilizes both dose-volume-based cost functions and a selection of cost functions which are based on biological models. The purpose of this work is to evaluate quality of intensity-modulated radiation therapy (IMRT) plans resulting from the use of biological cost functions in comparison to plans designed using a traditional TPS employing dose-volume-based optimization. Treatment planning was performed independently at two institutions. For six cancer patients, including head and neck (one case from each institution), prostate, brain, liver, and rectal cases, segmental multileaf collimator IMRT plans were designed using biological cost functions and compared with clinically used dose-based plans for the same patients. Dose-volume histograms and dosimetric indices, such as minimum, maximum, and mean dose, were extracted and compared between the two types of treatment plans. Comparisons of the generalized equivalent uniform dose (EUD), a previously proposed plan quality index (fEUD), target conformity and heterogeneity indices, and the number of segments and monitor units were also performed. The most prominent feature of the biologically based plans was better sparing of organs at risk (OARs). When all plans from both institutions were combined, the biologically based plans resulted in smaller EUD values for 26 out of 33 OARs by an average of 5.6 Gy (range 0.24 to 15 Gy). Owing to more efficient beam segmentation and leaf sequencing tools implemented in the biologically based TPS compared to the dose-based TPS, an estimated treatment delivery time was shorter in most (five out of six) cases with some plans showing up to 50% reduction. The biologically based plans were generally characterized by a smaller conformity index, but greater heterogeneity index compared to the dose-based plans. Overall, compared to plans based on dose

  1. Purification of benzoyl-mercapto-acetyl-tri-glycine and ethyl cysteinate dimer complemented with biological evaluations

    International Nuclear Information System (INIS)

    Robles, A.; Ramos, B.; Herrera, J.

    1999-01-01

    Purification of benzoyl-mercaptoacetyl triglycine (MAG3) and ethyl cysteinate dimer (L,L-ECD) has been conducted through fractionated recrystallization of its impurities and isomers; biological behavior of the main isomers has been evaluated through biological distribution in mice. Chemical purity of synthesized MAG3 is 69,9%; after purification, 98, 12% is obtained from the compound with adequate biological distribution; fusion points range between 194 and 196 o C before and after purification; recrystallization yields is 12%. Radiochemical purity of testing lot is 98%. In biological evaluations conducted in mice, injection dose percentages for the purest one, after 5 minutes, is 31,20% in kidneys and 1,14% in the liver. Chemical purity of synthesized ECD is 80,29%; after purification, 98,76% is obtained from the isomer with adequate biological activity; fusion points range between 195 and 197 o C; yield percentage in recrystallization is 29%. radiochemical purity of testing lot is 97%; in biological evaluations conducted in mice, injection dose percentages for the purest one, after 5 minutes, is 1,37% in the brain, 25,70% in the liver and 13,40% in kidneys

  2. Recent Advances in Momordica charantia: Functional Components and Biological Activities.

    Science.gov (United States)

    Jia, Shuo; Shen, Mingyue; Zhang, Fan; Xie, Jianhua

    2017-11-28

    Momordica charantia L. ( M. charantia ), a member of the Cucurbitaceae family, is widely distributed in tropical and subtropical regions of the world. It has been used in folk medicine for the treatment of diabetes mellitus, and its fruit has been used as a vegetable for thousands of years. Phytochemicals including proteins, polysaccharides, flavonoids, triterpenes, saponins, ascorbic acid and steroids have been found in this plant. Various biological activities of M. charantia have been reported, such as antihyperglycemic, antibacterial, antiviral, antitumor, immunomodulation, antioxidant, antidiabetic, anthelmintic, antimutagenic, antiulcer, antilipolytic, antifertility, hepatoprotective, anticancer and anti-inflammatory activities. However, both in vitro and in vivo studies have also demonstrated that M. charantia may also exert toxic or adverse effects under different conditions. This review addresses the chemical constituents of M. charantia and discusses their pharmacological activities as well as their adverse effects, aimed at providing a comprehensive overview of the phytochemistry and biological activities of M. charantia .

  3. Recent Advances in Momordica charantia: Functional Components and Biological Activities

    Directory of Open Access Journals (Sweden)

    Shuo Jia

    2017-11-01

    Full Text Available Momordica charantia L. (M. charantia, a member of the Cucurbitaceae family, is widely distributed in tropical and subtropical regions of the world. It has been used in folk medicine for the treatment of diabetes mellitus, and its fruit has been used as a vegetable for thousands of years. Phytochemicals including proteins, polysaccharides, flavonoids, triterpenes, saponins, ascorbic acid and steroids have been found in this plant. Various biological activities of M. charantia have been reported, such as antihyperglycemic, antibacterial, antiviral, antitumor, immunomodulation, antioxidant, antidiabetic, anthelmintic, antimutagenic, antiulcer, antilipolytic, antifertility, hepatoprotective, anticancer and anti-inflammatory activities. However, both in vitro and in vivo studies have also demonstrated that M. charantia may also exert toxic or adverse effects under different conditions. This review addresses the chemical constituents of M. charantia and discusses their pharmacological activities as well as their adverse effects, aimed at providing a comprehensive overview of the phytochemistry and biological activities of M. charantia.

  4. Simple glycolipids of microbes: Chemistry, biological activity and metabolic engineering

    Directory of Open Access Journals (Sweden)

    Ahmad Mohammad Abdel-Mawgoud

    2018-03-01

    Full Text Available Glycosylated lipids (GLs are added-value lipid derivatives of great potential. Besides their interesting surface activities that qualify many of them to act as excellent ecological detergents, they have diverse biological activities with promising biomedical and cosmeceutical applications. Glycolipids, especially those of microbial origin, have interesting antimicrobial, anticancer, antiparasitic as well as immunomodulatory activities. Nonetheless, GLs are hardly accessing the market because of their high cost of production. We believe that experience of metabolic engineering (ME of microbial lipids for biofuel production can now be harnessed towards a successful synthesis of microbial GLs for biomedical and other applications. This review presents chemical groups of bacterial and fungal GLs, their biological activities, their general biosynthetic pathways and an insight on ME strategies for their production.

  5. Traditional uses, phytochemistry and biological activities of Cotula ...

    African Journals Online (AJOL)

    Cotula cinerea contains a wide range of phytochemical compounds such as saponins, essential oils, tannins, flavonoids, steroids, and terpenoids. This paper reviews information pertaining its traditional uses, phytochemistry and biological activities such as antibacterial, antifungal, antioxidant, herbicidal, anti-diarrheal and ...

  6. Polysaccharies of higher fungi: Biological role, structure and antioxidative activity

    NARCIS (Netherlands)

    Kozarski, M.S.; Klaus, A.; Niksic, M.; Griensven, van L.J.L.D.; Vrvic, M.M.; Jakovljevic, D.M.

    2014-01-01

    The fungal polysaccharides attract a lot of attention due to their multiple challenging bio-logical properties, such as: anti-tumor, anti-viral, anticomplementary, anticoagulant, hypo-lipidemic, immunomodulatory and immune-stimulatory activities, which all together make them suitable for application

  7. Occurrence, biological activity and synthesis of drimane sesquiterpenoids

    NARCIS (Netherlands)

    Jansen, B.J.M.; Groot, de Æ.

    2004-01-01

    In this review the names, structures and occurrence of all new drimanes and rearranged drimanes, which have been published between January 1990 and January 2003 have been collected. Subjects that have been treated are biosynthesis, analysis, biological activities, with special attention to cytotoxic

  8. The cell biology of T-dependent B cell activation

    DEFF Research Database (Denmark)

    Owens, T; Zeine, R

    1989-01-01

    The requirement that CD4+ helper T cells recognize antigen in association with class II Major Histocompatibility Complex (MHC) encoded molecules constrains T cells to activation through intercellular interaction. The cell biology of the interactions between CD4+ T cells and antigen-presenting cells...

  9. A Review on Chemical Constituents and Biological Activities of the ...

    African Journals Online (AJOL)

    The current review is aimed to deliver some updates on the ethnobotany, phytochemistry and biological activities of Beilschmiedia species in order to throw more light on their therapeutic potentials and future research priorities. Phytochemical studies on Beilschmiedia genus yielded essential oils, endiandric acid ...

  10. Solar Energy Education. Renewable energy activities for biology

    Energy Technology Data Exchange (ETDEWEB)

    1982-01-01

    An instructional aid for teachers is presented that will allow biology students the opportunity to learn about renewable energy sources. Some of the school activities include using leaves as collectors of solar energy, solar energy stored in wood, and a fuel value test for green and dry woods. A study of organic wastes as a source of fuel is included. (BCS)

  11. Traditional uses, phytochemistry and biological activities of Cotula ...

    African Journals Online (AJOL)

    Keywords: Asteraceae, Cotula cinerea, Traditional uses, Phytochemistry, Biological activities. This is an Open .... desert conditions with an average annual rainfall .... Desert area between. Cairo and. Ismailia. (Egypt). Not stated. [33]. The essential oil of C. cinerea has also been subjected to many studies. The essential oil.

  12. Volatile compounds and biological activities of aerial parts of ...

    African Journals Online (AJOL)

    Volatile compounds and biological activities of aerial parts of Pituranthos scoparius (Coss and ... mg/mL. Conclusion: These findings indicate that the essential oil of P.scoparius has a potential for use as a preservative and flavorant in ..... Values are expressed as mean ± standard deviation (n=3). Key: control (♢), BHT (□) ...

  13. Students' Learning Activities While Studying Biological Process Diagrams

    Science.gov (United States)

    Kragten, Marco; Admiraal, Wilfried; Rijlaarsdam, Gert

    2015-01-01

    Process diagrams describe how a system functions (e.g. photosynthesis) and are an important type of representation in Biology education. In the present study, we examined students' learning activities while studying process diagrams, related to their resulting comprehension of these diagrams. Each student completed three learning tasks. Verbal…

  14. Biological activity of phenolic compounds present in buckwheat plants

    Czech Academy of Sciences Publication Activity Database

    Kalinová, J.; Tříska, Jan; Vrchotová, Naděžda

    2005-01-01

    Roč. 16, č. 1 (2005), s. 123-129 ISSN 0971-4693 Institutional research plan: CEZ:AV0Z60870520 Keywords : biological activity, extract, Fagopyrum esculenthum Subject RIV: CB - Analytical Chemistry, Separation Impact factor: 0.686, year: 2005

  15. The Biological Activities of Moltkia aurea; an Endemic Species to ...

    African Journals Online (AJOL)

    Neslihan BALPINAR

    inclination that studies on medicinal plants, which are basis for the development of new biologically active molecules for pharmaceuticals, have rapidly increased. Recent studies associated with medicinal plants make possible to better understand their properties, safety and efficiency. In this study, Moltkia aurea Boiss.

  16. BIOLOGICALLY ENHANCED OXYGEN TRANSFER IN THE ACTIVATED SLUDGE PROCESS (JOURNAL)

    Science.gov (United States)

    Biologically enhanced oxgyen transfer has been a hypothesis to explain observed oxygen transfer rates in activated sludge systems that were well above that predicted from aerator clean-water testing. The enhanced oxygen transfer rates were based on tests using BOD bottle oxygen ...

  17. Biological activities of some Fluoroquinolones-metal complexes ...

    African Journals Online (AJOL)

    Background: Metal ions play a vital role in the design of more biologically active drugs. Aim: The paper reviewed the antimicrobial, toxicological and DNA cleavage studies of some synthesized metal complexes of fluoroquinolone antibiotics. Materials and Methods: Literature searches were done using scientific databases.

  18. Synthesis and biological evaluation of benzazepine oxazolidinone antibacterials.

    Science.gov (United States)

    Johnson, Paul D; Aristoff, Paul A; Zurenko, Gary E; Schaadt, Ronda D; Yagi, Betty H; Ford, Charles W; Hamel, Judith C; Stapert, Douglas; Moerman, Judy K

    2003-12-01

    Novel benzazepine oxazolidinone antibacterials were synthesized and evaluated against clinically relevant susceptible and resistant organisms. The effect of ring nitrogen position and N-substitution on antibacterial activity is examined.

  19. Biological activities of Peganum harmala leaves | Hayet | African ...

    African Journals Online (AJOL)

    The antioxidant activity was evaluated using ammonium thiocyanate method. Among tested extracts, methanol and chloroform extracts displayed a higher antibacterial activity against gram-positive than gram-negative bacteria. The methanol extract demonstrated the highest antioxidant activity and good antiviral activity ...

  20. Secondary Metabolites from Inula britannica L. and Their Biological Activities

    Directory of Open Access Journals (Sweden)

    Yoon-Ha Kim

    2010-03-01

    Full Text Available Inula britannica L., family Asteraceae, is used in traditional Chinese and Kampo Medicines for various diseases. Flowers or the aerial parts are a rich source of secondary metabolites. These consist mainly of terpenoids (sesquiterpene lactones and dimmers, diterpenes and triterpenoids and flavonoids. The isolated compounds have shown diverse biological activities: anticancer, antioxidant, anti-inflammatory, neuroprotective and hepatoprotective activities. This review provides information on isolated bioactive phytochemicals and pharmacological potentials of I. britannica.

  1. Secondary metabolites from Inula britannica L. and their biological activities.

    Science.gov (United States)

    Khan, Abdul Latif; Hussain, Javid; Hamayun, Muhammad; Gilani, Syed Abdullah; Ahmad, Shabir; Rehman, Gauhar; Kim, Yoon-Ha; Kang, Sang-Mo; Lee, In-Jung

    2010-03-10

    Inula britannica L., family Asteraceae, is used in traditional Chinese and Kampo Medicines for various diseases. Flowers or the aerial parts are a rich source of secondary metabolites. These consist mainly of terpenoids (sesquiterpene lactones and dimmers, diterpenes and triterpenoids) and flavonoids. The isolated compounds have shown diverse biological activities: anticancer, antioxidant, anti-inflammatory, neuroprotective and hepatoprotective activities. This review provides information on isolated bioactive phytochemicals and pharmacological potentials of I. britannica.

  2. Synthesis, structure and biological properties of active spirohydantoin derivatives

    Directory of Open Access Journals (Sweden)

    Lazić Anita M.

    2016-01-01

    Full Text Available Spirohidantoins represent an pharmacologically important class of heterocycles since many derivatives have been recognized that display interesting activities against a wide range of biological targets. First synthesis of cycloalkanespiro-5-hydantoins was performed by Bucherer and Lieb 1934 by the reaction of cycloalkanone, potassium cyanide and ammonium-carbonate at reflux in a mixture of ethanol and water. QSAR (Quantitative Structure-Activity Relationship studies showed that a wide range of biological activities of spirohydantoin derivatives strongly depend upon their structure. This paper describes different methods of synthesis of spirohydantoin derivatives, their physico-chemical properties and biological activity. It emphasizes the importance of cycloalkanespiro-5-hydantoins with anticonvulsant, antiproliferative, antipsychotic, antimicrobial and antiinflammatory properties as well as their importance in the treatment of diabetes. Numerous spirohydantoin compounds exhibit physiological activity such as serotonin and fibrinogen antagonist, inhibitors of the glycine binding site of the NMDA receptor also, antagonist of leukocyte cell adhesion, acting as allosteric inhibitors of the protein-protein interactions. Some spirohydantoin derivatives have been identified as antitumor agents. Their activity depends on the substituent presented at position N-3 of the hydantoin ring and increases in order alkene > ester > ether. Besides that, compounds that contain two electron withdrawing groups (e.g. fluorine or chlorine on the third and fourth position of the phenyl ring are better antitumor agents than compounds with a single electron withdrawing group. [Projekat Ministarstva nauke Republike Srbije, br. 172013

  3. Assessing Student Behaviors and Motivation for Actively Learning Biology

    Science.gov (United States)

    Moore, Michael Edward

    Vision and Change states that one of the major changes in the way we design biology courses should be a switch in approach from teacher-centered learning to student-centered learning and identifies active learning as a recommended methods. Studies show performance benefits for students taking courses that use active learning. What is unknown is why active learning is such an effective instructional tool and the limits of this instructional method’s ability to influence performance. This dissertation builds a case in three steps for why active learning is an effective instructional tool. In step one, I assessed the influence of different types of active learning (clickers, group activities, and whole class discussions) on student engagement behavior in one semester of two different introductory biology courses and found that active learning positively influenced student engagement behavior significantly more than lecture. For step two, I examined over four semesters whether student engagement behavior was a predictor of performance and found participation (engagement behavior) in the online (video watching) and in-class course activities (clicker participation) that I measure were significant predictors of performance. In the third, I assessed whether certain active learning satisfied the psychological needs that lead to students’ intrinsic motivation to participate in those activities when compared over two semesters and across two different institutions of higher learning. Findings from this last step show us that student’s perceptions of autonomy, competency, and relatedness in doing various types of active learning are significantly higher than lecture and consistent across two institutions of higher learning. Lastly, I tie everything together, discuss implications of the research, and address future directions for research on biology student motivation and behavior.

  4. Evaluating children's conservation biology learning at the zoo.

    Science.gov (United States)

    Jensen, Eric

    2014-08-01

    Millions of children visit zoos every year with parents or schools to encounter wildlife firsthand. Public conservation education is a requirement for membership in professional zoo associations. However, in recent years zoos have been criticized for failing to educate the public on conservation issues and related biological concepts, such as animal adaptation to habitats. I used matched pre- and postvisit mixed methods questionnaires to investigate the educational value of zoo visits for children aged 7-15 years. The questionnaires gathered qualitative data from these individuals, including zoo-related thoughts and an annotated drawing of a habitat. A content analysis of these qualitative data produced the quantitative data reported in this article. I evaluated the relative learning outcomes of educator-guided and unguided zoo visits at London Zoo, both in terms of learning about conservation biology (measured by annotated drawings) and changing attitudes toward wildlife conservation (measured using thought-listing data). Forty-one percent of educator-guided visits and 34% of unguided visits resulted in conservation biology-related learning. Negative changes in children's understanding of animals and their habitats were more prevalent in unguided zoo visits. Overall, my results show the potential educational value of visiting zoos for children. However, they also suggest that zoos' standard unguided interpretive materials are insufficient for achieving the best outcomes for visiting children. These results support a theoretical model of conservation biology learning that frames conservation educators as toolmakers who develop conceptual resources to enhance children's understanding of science. © 2014 Society for Conservation Biology.

  5. Heteroaryl Chalcones: Design, Synthesis, X-ray Crystal Structures and Biological Evaluation

    Directory of Open Access Journals (Sweden)

    Hoong-Kun Fun

    2013-10-01

    Full Text Available Chalcone derivatives have attracted increasing attention due to their numerous pharmacological activities. Changes in their structures have displayed high degree of diversity that has proven to result in a broad spectrum of biological activities. The present study highlights the synthesis of some halogen substituted chalcones 3(a–i containing the 5-chlorothiophene moiety, their X-ray crystal structures and the evaluation of possible biological activities such as antibacterial, antifungal and reducing power abilities. The results indicate the tested compounds show a varied range of inhibition values against all the tested microbial strains. Compound 3c with a p-fluoro substituent on the phenyl ring exhibits elevated antimicrobial activity, whereas the compounds 3e and 3f displayed the least antimicrobial activities. The compounds 3d, 3e, 3f and 3i showed good ferric and cupric reducing abilities, and the compounds 3b and 3c showed the weakest reducing power in the series.

  6. Teaching biological evolution - internal and external evaluation of learning outcomes

    Directory of Open Access Journals (Sweden)

    Clas Olander

    2012-06-01

    Full Text Available This paper reports from a study where teachers and researchers collaborate on designing and validatingtopic-oriented teaching-learning sequences. In an iterative process, data about learning andteaching biological evolution are generated through continuous cycles of design, teaching, evaluation,and redesign. The study involved 180 Swedish students aged 11 – 16, and the overall learning aim was that the students should be able to use the theory of evolution as a tool when explaining the development of life on earth. The aim of this paper is to validate the students’ learning outcome, estimated as appropriation of scientific ways of reasoning in written answers. The students’ answers of questions are analysed before and after interventions (internal evaluation, and compared with the answers from a national sample (external evaluation. The students in the experimental group did develop their reasoning, and they attained the aim, to a greater extent than a national sample.

  7. Controlled release of biologically active silver from nanosilver surfaces.

    Science.gov (United States)

    Liu, Jingyu; Sonshine, David A; Shervani, Saira; Hurt, Robert H

    2010-11-23

    Major pathways in the antibacterial activity and eukaryotic toxicity of nanosilver involve the silver cation and its soluble complexes, which are well established thiol toxicants. Through these pathways, nanosilver behaves in analogy to a drug delivery system, in which the particle contains a concentrated inventory of an active species, the ion, which is transported to and released near biological target sites. Although the importance of silver ion in the biological response to nanosilver is widely recognized, the drug delivery paradigm has not been well developed for this system, and there is significant potential to improve nanosilver technologies through controlled release formulations. This article applies elements of the drug delivery paradigm to nanosilver dissolution and presents a systematic study of chemical concepts for controlled release. After presenting thermodynamic calculations of silver species partitioning in biological media, the rates of oxidative silver dissolution are measured for nanoparticles and macroscopic foils and used to derive unified area-based release kinetics. A variety of competing chemical approaches are demonstrated for controlling the ion release rate over 4 orders of magnitude. Release can be systematically slowed by thiol and citrate ligand binding, formation of sulfidic coatings, or the scavenging of peroxy-intermediates. Release can be accelerated by preoxidation or particle size reduction, while polymer coatings with complexation sites alter the release profile by storing and releasing inventories of surface-bound silver. Finally, the ability to tune biological activity is demonstrated through a bacterial inhibition zone assay carried out on selected formulations of controlled release nanosilver.

  8. Biological activities of phenolic compounds present in virgin olive oil.

    Science.gov (United States)

    Cicerale, Sara; Lucas, Lisa; Keast, Russell

    2010-02-02

    The Mediterranean diet is associated with a lower incidence of atherosclerosis, cardiovascular disease, neurodegenerative diseases and certain types of cancer. The apparent health benefits have been partially ascribed to the dietary consumption of virgin olive oil by Mediterranean populations. Much research has focused on the biologically active phenolic compounds naturally present in virgin olive oils to aid in explaining reduced mortality and morbidity experienced by people consuming a traditional Mediterranean diet. Studies (human, animal, in vivo and in vitro) have demonstrated that olive oil phenolic compounds have positive effects on certain physiological parameters, such as plasma lipoproteins, oxidative damage, inflammatory markers, platelet and cellular function, antimicrobial activity and bone health. This paper summarizes current knowledge on the bioavailability and biological activities of olive oil phenolic compounds.

  9. Biological Activities of Phenolic Compounds Present in Virgin Olive Oil

    Directory of Open Access Journals (Sweden)

    Russell Keast

    2010-02-01

    Full Text Available The Mediterranean diet is associated with a lower incidence of atherosclerosis, cardiovascular disease, neurodegenerative diseases and certain types of cancer. The apparent health benefits have been partially ascribed to the dietary consumption of virgin olive oil by Mediterranean populations. Much research has focused on the biologically active phenolic compounds naturally present in virgin olive oils to aid in explaining reduced mortality and morbidity experienced by people consuming a traditional Mediterranean diet. Studies (human, animal, in vivo and in vitro have demonstrated that olive oil phenolic compounds have positive effects on certain physiological parameters, such as plasma lipoproteins, oxidative damage, inflammatory markers, platelet and cellular function, antimicrobial activity and bone health. This paper summarizes current knowledge on the bioavailability and biological activities of olive oil phenolic compounds.

  10. Should Soil Testing Services Measure Soil Biological Activity?

    Directory of Open Access Journals (Sweden)

    Alan J. Franzluebbers

    2016-02-01

    Full Text Available Health of agricultural soils depends largely on conservation management to promote soil organic matter accumulation. Total soil organic matter changes slowly, but active fractions are more dynamic. A key indicator of healthy soil is potential biological activity, which could be measured rapidly with soil testing services via the flush of CO during 1 to 3 d following rewetting of dried soil. The flush of CO is related to soil microbial biomass C and has repeatedly been shown strongly related to net N mineralization during standard aerobic incubations. New research is documenting the close association with plant N uptake in semicontrolled greenhouse conditions ( = 0.77, = 36. Field calibrations are underway to relate the flush of CO to the need for in-season N requirement in a variety of crops. An index of soil biological activity can and should be determined to help predict soil health and soil N availability.

  11. Structural Diversity and Biological Activities of Cyclic Depsipeptides from Fungi

    Directory of Open Access Journals (Sweden)

    Xiaohan Wang

    2018-01-01

    Full Text Available Cyclic depsipeptides (CDPs are cyclopeptides in which amide groups are replaced by corresponding lactone bonds due to the presence of a hydroxylated carboxylic acid in the peptide structure. These peptides sometimes display additional chemical modifications, including unusual amino acid residues in their structures. This review highlights the occurrence, structures and biological activities of the fungal CDPs reported until October 2017. About 352 fungal CDPs belonging to the groups of cyclic tri-, tetra-, penta-, hexa-, hepta-, octa-, nona-, deca-, and tridecadepsipeptides have been isolated from fungi. These metabolites are mainly reported from the genera Acremonium, Alternaria, Aspergillus, Beauveria, Fusarium, Isaria, Metarhizium, Penicillium, and Rosellina. They are known to exhibit various biological activities such as cytotoxic, phytotoxic, antimicrobial, antiviral, anthelmintic, insecticidal, antimalarial, antitumoral and enzyme-inhibitory activities. Some CDPs (i.e., PF1022A, enniatins and destruxins have been applied as pharmaceuticals and agrochemicals.

  12. Synthesis, biological activities, and quantitative structure-activity relationship (QSAR) study of novel camptothecin analogues.

    Science.gov (United States)

    Wu, Dan; Zhang, Shao-Yong; Liu, Ying-Qian; Wu, Xiao-Bing; Zhu, Gao-Xiang; Zhang, Yan; Wei, Wei; Liu, Huan-Xiang; Chen, An-Liang

    2015-05-13

    In continuation of our program aimed at the development of natural product-based pesticidal agents, three series of novel camptothecin derivatives were designed, synthesized, and evaluated for their biological activities against T. Cinnabarinus, B. brassicae, and B. xylophilus. All of the derivatives showed good-to-excellent activity against three insect species tested, with LC50 values ranging from 0.00761 to 0.35496 mmol/L. Remarkably, all of the compounds were more potent than CPT against T. Cinnabarinus, and compounds 4d and 4c displayed superior activity (LC50 0.00761 mmol/L and 0.00942 mmol/L, respectively) compared with CPT (LC50 0.19719 mmol/L) against T. Cinnabarinus. Based on the observed bioactivities, preliminary structure-activity relationship (SAR) correlations were also discussed. Furthermore, a three-dimensional quantitative structure-activity relationship (3D-QSAR) model using comparative molecular field analysis (CoMFA) was built. The model gave statistically significant results with the cross-validated q2 values of 0.580 and correlation coefficient r2 of 0.991 and  of 0.993. The QSAR analysis indicated that the size of the substituents play an important in the activity of 7-modified camptothecin derivatives. These findings will pave the way for further design, structural optimization, and development of camptothecin-derived compounds as pesticidal agents.

  13. Biological conversion of synthesis gas. Topical report: Economic evaluations

    Energy Technology Data Exchange (ETDEWEB)

    Clausen, E.C.; Gaddy, J.L.

    1993-09-01

    The purpose of the proposed research is to develop a technically and economically feasible process for biologically producing H{sub 2} from synthesis gas while, at the same time, removing harmful sulfur gas compounds. Six major tasks are being studied: culture development, where the best cultures are selected and conditions optimized for simultaneous hydrogen production and sulfur gas removal; mass transfer and kinetic studies in which equations necessary for process design are developed; bioreactor design studies, where the cultures chosen in Task 1 are utilized in continuous reaction vessels to demonstrate process feasibility and define operating conditions; evaluation of biological synthesis gas conversion under limiting conditions in preparation for industrial demonstration studies; process scale-up where laboratory data are scaled to larger-size units in preparation for process demonstration in a pilot-scale unit; and economic evaluation, where process simulations are used to project process economics and identify high cost areas during sensitivity analyses. The purpose of this report is to present economic evaluations for H{sub 2} production from synthesis gone by Rhodospirillum rubrum. Cases are presented with and without light requirements and in stirred tank and immobilized cell reactors. In addition, economic information is presented for isolate ERIH{sub 2} (from Engineering Resources, Inc.) in the two reactors with and without H{sub 2} recovery.

  14. Indonesian propolis: chemical composition, biological activity and botanical origin.

    Science.gov (United States)

    Trusheva, Boryana; Popova, Milena; Koendhori, Eko Budi; Tsvetkova, Iva; Naydenski, Christo; Bankova, Vassya

    2011-03-01

    From a biologically active extract of Indonesian propolis from East Java, 11 compounds were isolated and identified: four alk(en)ylresorcinols (obtained as an inseparable mixture) (1-4) were isolated for the first time from propolis, along with four prenylflavanones (6-9) and three cycloartane-type triterpenes (5, 10 and 11). The structures of the components were elucidated based on their spectral properties. All prenylflavanones demonstrated significant radical scavenging activity against diphenylpicrylhydrazyl radicals, and compound 6 showed significant antibacterial activity against Staphylococcus aureus. For the first time Macaranga tanarius L. and Mangifera indica L. are shown as plant sources of Indonesian propolis.

  15. QSAR Study of the Biologically Active Organosulfurs in Natural Products

    Directory of Open Access Journals (Sweden)

    Fakhr M. Abu-Awwad

    2010-01-01

    Full Text Available The biological activities of two sets of a total of 30 different polysulfides were investigated using QSAR. The semiempirical AM1 in Gaussian 2003 for windows was used to optimize the structures whereas a subsequent calculation of hundreds of various types of descriptors at the density functional (B3LYP/6-31G* using CODESSA package was employed. The known 15-lipoxygenase inhibitory activity data (IC50 of 19 polysulfides out of the whole data set were correlated in a multiple linear regression procedures with the computed descriptors. Statistically, the most significant overall correlations were five- and four- parameter equations with good statistical parameters; R2= 0.9981, R2CV = 0.9970 and R2=9967, R2CV = 0.9933 respectively. The models concluded that biological activity of polysulfides is mainly attributed to quantum-chemical, geometrical and topological descriptors with neither electrostatic contribution nor chief role of sulfur atoms. Also sulfur related descriptors were not the most significant contributors in the concluded models. The obtained models were efficiently employed to estimate the biological activities of the other 11 polysulfides available in natural products such as garlic and mushroom.

  16. Biological Activity Alterations of Human Amniotic Membrane Pre and Post Irradiation Tissue Banking.

    Science.gov (United States)

    Nemr, Waleed; Bashandy, A S; Araby, Eman; Khamiss, O

    Innate immunity of Human Amniotic Membrane (HAM) and its highly active secretome that rich with various types of growth factors and anti-inflammatory substances proposed it as a promising material for many medical studies and applications. This study evaluate the biological activity of cultivated HAM pre and post tissue banking process in which freeze-dried HAM was sterilized by 25 KGray (kGy) dose of γ radiation. The HAM's antimicrobial activity, viability, growth of isolated human amniotic epithelial cells (HAECs), hematopoietic stimulation of co-cultivated murine bone marrow cells (mammalian model), scaffold efficiency for fish brain building up (non-mammalian model) and self re-epithelialization after trypsin denuding treatment were examined as supposed biological activity features. Native HAM revealed viability indications and was active to kill all tested microorganisms; 6 bacterial species (3 Gram-positive and 3 Gram-negative) and Candida albicans as a pathogenic fungus. Also, HAM activity promoted colony formation of murine hematopoietic cells, Tilapia nilotica brain fragment building-up and self re-epithelialization after trypsin treatment. In contrary, radiation-based tissue banking of HAM caused HAM cellular death and consequently lacked almost all of examined biological activity features. Viable HAM was featured with biological activity than fixed HAM prepared by irradiation tissue banking.

  17. Medicinal Chemistry of Annonaceous Acetogenins: Design, Synthesis, and Biological Evaluation of Novel Analogues

    Directory of Open Access Journals (Sweden)

    Naoto Kojima

    2009-09-01

    Full Text Available Most Annonaceous acetogenins are characterized by between one and three THF ring(s with one or two flanking hydroxyl group(s in the center of a C32/34 fatty acid, and the terminal carboxylic acid is combined with a 2-propanol unit to form an α,β-unsaturated γ-lactone. While many studies have addressed the properties and synthesis of natural acetogenins due to their attractive biological activities and unique structural features, a number of analogues have also been described. This review covers the design, synthesis, and biological evaluation of acetogenin analogues.

  18. Characterization of biologically active substances from Calendula officinalis.

    Science.gov (United States)

    Lovecka, Petra; Lipov, Jan; Thumova, Kamila; Macurkova, Anna

    2018-02-26

    The aim of this work was to compare water and organic extracts, infusions and tinctures from flowers and leaves of Calendula officinalis in terms of their biological activity and composition. The purpose of work was investigation whether the leaves and stems are really the waste or they contain interesting substances which could be utilized. Antimicrobial, antifungal, antioxidant and anti-inflammatory activities were studied. Then the ability to inhibit collagenase was studied as well. Cytotoxicity was tested for all the samples on mammalian cell lines. To determine the composition of extracts, infusions and tinctures phytochemical analysis (the set of colour reactions for detection of groups of biologically active compounds) was carried out and shown that samples from flowers and leaves contain the same groups of biologically active substances (proteins and amino acids, reducing sugars, flavonoids, saponins, phenolics, terpenoids, steroids, glycosides). The antimicrobial activity of tested samples was proved, where the most sensitive bacterium was Micrococcus luteus and the most sensitive yeast was Geotrichum candidum. The study of anti - collagenase activity has shown that the enzymatic reaction of collagenase was affected by all tested samples and their effect was concentration dependent. Cytotoxicity of water and methanol extracts at cell lines HEK 293T and HepG2 was observed. Cells HepG2 were more sensitive than cells HEK 293T. Using cell line RAW 264.7 anti-inflammatory activity of all samples was observed. Tincture of leaves was the most effective. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

  19. Biological activity of selected plants with adaptogenic effect

    Directory of Open Access Journals (Sweden)

    Eva Ivanišová

    2016-05-01

    Full Text Available The aim of this study was to determine biological activity of plants with adaptogenic effect: Panax ginseng Mayer., Withania somnifera L., Eleuterococcus senticosus Rupr. et Maxim., Astragallus membranaceus Fisch. and Codonopsis pilosulae Franch. The antioxidant activity was detected by DPPH and phosphomolybdenum method, total polyphenol content with Folin – Ciocalteu reagent, flavonoids content by aluminium chloride method. The detection of antimicrobial activity was carried out by disc diffusion method against three species of Gram-negative bacteria: Escherichia coli CCM 3988, Salmonella enterica subsp. enterica CCM 3807, Yersinia enterocolitica CCM 5671 and two Gram-positive bacteria: Bacillus thuringiensis CCM 19, Stapylococcus aureus subsp. aureus CCM 2461. Results showed that plants with adaptogenic effect are rich for biologically active substances. The highest antioxidant activity by DPPH method was determined in the sample of Eleuterococcus senticosus (3.15 mg TEAC – Trolox equivalent antioxidant capacity per g of sample and by phosphomolybdenum method in the sample of Codonopsis pilosulae (188.79 mg TEAC per g of sample. In the sample of Panax ginseng was measured the highest content of total polyphenols (8.10 mg GAE – galic acid equivalent per g of sample and flavonoids (3.41 μg QE – quercetin equivalent per g of sample. All samples also showed strong antimicrobial activity with the best results in Panax ginseng and Withania somnifera in particular for species Yersinia enterocolitica CCM 5671 and Salmonella enterica subsp. enterica CCM 3807. The analyzed species of plant with high value of biological activity can be used more in the future, not only in food, but also in cosmetics and pharmaceutical industries.

  20. Marine Sponge Lectins: Actual Status on Properties and Biological Activities

    Directory of Open Access Journals (Sweden)

    Sandro Mascena Gomes Filho

    2014-12-01

    Full Text Available Marine sponges are primitive metazoans that produce a wide variety of molecules that protect them against predators. In studies that search for bioactive molecules, these marine invertebrates stand out as promising sources of new biologically-active molecules, many of which are still unknown or little studied; thus being an unexplored biotechnological resource of high added value. Among these molecules, lectins are proteins that reversibly bind to carbohydrates without modifying them. In this review, various structural features and biological activities of lectins derived from marine sponges so far described in the scientific literature are discussed. From the results found in the literature, it could be concluded that lectins derived from marine sponges are structurally diverse proteins with great potential for application in the production of biopharmaceuticals, especially as antibacterial and antitumor agents.

  1. MILK KEFIR: COMPOSITION, MICROBIAL CULTURES, BIOLOGICAL ACTIVITIES AND RELATED PRODUCTS

    Directory of Open Access Journals (Sweden)

    Maria Rosa Prado

    2015-10-01

    Full Text Available In recent years, there has been a strong focus on beneficial foods with probiotic microorganisms and functional organic substances. In this context, there is an increasing interest in the commercial use of kefir, since it can be marketed as a natural beverage that has health promoting bacteria. There are numerous commercially available kefir based-products. Kefir may act as a matrix in the effective delivery of probiotic microorganisms in different types of products. Also, the presence of kefir’s exopolysaccharides, known as kefiran, which has biological activity, certainly adds value to products. Kefiran can also be used separately in other food products and as a coating film for various food and pharmaceutical products. This article aims to update the information about kefir and its microbiological composition, biological activity of the kefir’s microflora and the importance of kefiran as a beneficial health substance.

  2. Milk kefir: composition, microbial cultures, biological activities, and related products.

    Science.gov (United States)

    Prado, Maria R; Blandón, Lina Marcela; Vandenberghe, Luciana P S; Rodrigues, Cristine; Castro, Guillermo R; Thomaz-Soccol, Vanete; Soccol, Carlos R

    2015-01-01

    In recent years, there has been a strong focus on beneficial foods with probiotic microorganisms and functional organic substances. In this context, there is an increasing interest in the commercial use of kefir, since it can be marketed as a natural beverage that has health promoting bacteria. There are numerous commercially available kefir based-products. Kefir may act as a matrix in the effective delivery of probiotic microorganisms in different types of products. Also, the presence of kefir's exopolysaccharides, known as kefiran, which has biological activity, certainly adds value to products. Kefiran can also be used separately in other food products and as a coating film for various food and pharmaceutical products. This article aims to update the information about kefir and its microbiological composition, biological activity of the kefir's microflora and the importance of kefiran as a beneficial health substance.

  3. Charged particle activation analysis of phosphorus in biological materials

    International Nuclear Information System (INIS)

    Masumoto, K.; Yagi, M.

    1983-01-01

    Charged particle activation analysis of phosphorus in biological materials using the 31 P(α,n) sup(34m)Cl reaction has been studied. Since sup(34m)Cl is also produced by the 32 S(α,pn) and the 35 Cl(α,α'n) reactions, the thick-target yield curves on phosphorus, sulfur and chlorine were determined in order to choose the optimum irradiation conditions. As a result, it was found that the activation analysis for phosphorus without interferences from sulfur and chlorine is possible by bombarding with less than 17 MeV alphas. The applicability of this method to biological samples was then examined by irradiating several standard reference materials. It was confirmed that phosphorus can readily be determined at the detection limit of 1μg free from interferences due to the matrix elements. (author)

  4. Biological activities of secondary metabolites of the order Zoanthids

    Directory of Open Access Journals (Sweden)

    Zahra Aminikhoei

    2015-11-01

    Full Text Available The phylum Cnidaria is a large, diverse and ecologically important group of marine invertebrates, which produce powerful toxins and venoms. The number of marine natural product from cnidarians isolated from class Anthozoa. Among the Anthozoa, the order of zoanthids are sessile, clonal and mostly brightly colored invertebrate which produce high biodiversity of cytolitic, neurotoxic and cardiotoxic compounds. Zoanthids containing palytoxins are reportedly among the most toxic marine organisms known. In addition, a high concentration of zoanthamine alkaloids extracted from this group.The zoanthamine alkaloids were isolated over 20 years ago, exhibit a broad range of biological activities.The best studied and most well-known biological activity of zoanthamine derivative significantly suppressed bone resorption and enhanced bone formation.

  5. Biological activities and medicinal properties of Cajanus cajan (L) Millsp.

    Science.gov (United States)

    Pal, Dilipkumar; Mishra, Pragya; Sachan, Neetu; Ghosh, Ashoke K

    2011-10-01

    Cajanus cajan (L) Millsp. (Sanskrit: Adhaki, Hindi: Arhar, English: Pigeon pea, Bengali: Tur) (family: Fabaceae) is the most important grain legume crop of rain-fed agriculture in semi-arid tropics. It is both a food crop and a cover/forage crop with high levels of proteins and important amino acids like methionine, lysine and tryptophan. During the last few decades extensive studies have been carried out regarding the chemistry of C. cajan and considerable progress has been achieved regarding its biological activities and medicinal applications. This review article gives an overview on the biological activities of the compounds isolated, pharmacological actions and clinical studies of C. cajan extracts apart from its general details.

  6. Biological activities and medicinal properties of Cajanus cajan (L Millsp.

    Directory of Open Access Journals (Sweden)

    Dilipkumar Pal

    2011-01-01

    Full Text Available Cajanus cajan (L Millsp. (Sanskrit: Adhaki, Hindi: Arhar, English: Pigeon pea, Bengali: Tur (family: Fabaceae is the most important grain legume crop of rain-fed agriculture in semi-arid tropics. It is both a food crop and a cover/forage crop with high levels of proteins and important amino acids like methionine, lysine and tryptophan. During the last few decades extensive studies have been carried out regarding the chemistry of C. cajan and considerable progress has been achieved regarding its biological activities and medicinal applications. This review article gives an overview on the biological activities of the compounds isolated, pharmacological actions and clinical studies of C. cajan extracts apart from its general details.

  7. Synthesis and Antiplatelet Activity of Antithrombotic Thiourea Compounds: Biological and Structure-Activity Relationship Studies

    Directory of Open Access Journals (Sweden)

    André Luiz Lourenço

    2015-04-01

    Full Text Available The incidence of hematological disorders has increased steadily in Western countries despite the advances in drug development. The high expression of the multi-resistance protein 4 in patients with transitory aspirin resistance, points to the importance of finding new molecules, including those that are not affected by these proteins. In this work, we describe the synthesis and biological evaluation of a series of N,N'-disubstituted thioureas derivatives using in vitro and in silico approaches. New designed compounds inhibit the arachidonic acid pathway in human platelets. The most active thioureas (compounds 3d, 3i, 3m and 3p displayed IC50 values ranging from 29 to 84 µM with direct influence over in vitro PGE2 and TXA2 formation. In silico evaluation of these compounds suggests that direct blockage of the tyrosyl-radical at the COX-1 active site is achieved by strong hydrophobic contacts as well as electrostatic interactions. A low toxicity profile of this series was observed through hemolytic, genotoxic and mutagenic assays. The most active thioureas were able to reduce both PGE2 and TXB2 production in human platelets, suggesting a direct inhibition of COX-1. These results reinforce their promising profile as lead antiplatelet agents for further in vivo experimental investigations.

  8. Propolis volatile compounds: chemical diversity and biological activity: a review

    OpenAIRE

    Bankova, Vassya; Popova, Milena; Trusheva, Boryana

    2014-01-01

    Propolis is a sticky material collected by bees from plants, and used in the hive as building material and defensive substance. It has been popular as a remedy in Europe since ancient times. Nowadays, propolis use in over-the-counter preparations, “bio”-cosmetics and functional foods, etc., increases. Volatile compounds are found in low concentrations in propolis, but their aroma and significant biological activity make them important for propolis characterisation. Propolis is a plant-derived...

  9. Secondary metabolites in grasses: characterization and biological activity

    OpenAIRE

    Aldo Tava

    2007-01-01

    In a series of studies dealing on the nutritional value of forage species, more attention was focussed on several compounds, named secondary metabolites, that are important in determining nutritional characteristics. Secondary metabolites are compounds detected in the green materials in low concentration compared to primary metabolites (proteins, sugars, lipids, fibers), but of fundamental importance for the plant physiology. The possess several biological activities and this contribute to th...

  10. Photoelectron spectra and biological activity of cinnamic acid derivatives revisited

    Science.gov (United States)

    Novak, Igor; Klasinc, Leo; McGlynn, Sean P.

    2018-01-01

    The electronic structures of several derivatives of cinnamic acid have been studied by UV photoelectron spectroscopy (UPS) and Green's function quantum chemical calculations. The spectra reveal the presence of dimers in the gas phase for p-coumaric and ferulic acids. The electronic structure analysis has been related to the biological properties of these compounds through the analysis of some structure-activity relationships (SAR).

  11. Polymer application for separation/filtration of biological active compounds

    Science.gov (United States)

    Tylkowski, B.; Tsibranska, I.

    2017-06-01

    Membrane technology is an important part of the engineer's toolbox. This is especially true for industries that process food and other products with their primary source from nature. This review is focused on ongoing development work using membrane technologies for concentration and separation of biologically active compounds, such as polyphenols and flavonoids. We provide the readers not only with the last results achieve in this field but also, we deliver detailed information about the membrane types and polymers used for their preparation.

  12. Biological Activities of Phenolic Compounds Present in Virgin Olive Oil

    OpenAIRE

    Cicerale, Sara; Lucas, Lisa; Keast, Russell

    2010-01-01

    The Mediterranean diet is associated with a lower incidence of atherosclerosis, cardiovascular disease, neurodegenerative diseases and certain types of cancer. The apparent health benefits have been partially ascribed to the dietary consumption of virgin olive oil by Mediterranean populations. Much research has focused on the biologically active phenolic compounds naturally present in virgin olive oils to aid in explaining reduced mortality and morbidity experienced by people consuming a trad...

  13. Recent Advances in Momordica charantia: Functional Components and Biological Activities

    OpenAIRE

    Jia, Shuo; Shen, Mingyue; Zhang, Fan; Xie, Jianhua

    2017-01-01

    Momordica charantia L. (M. charantia), a member of the Cucurbitaceae family, is widely distributed in tropical and subtropical regions of the world. It has been used in folk medicine for the treatment of diabetes mellitus, and its fruit has been used as a vegetable for thousands of years. Phytochemicals including proteins, polysaccharides, flavonoids, triterpenes, saponins, ascorbic acid and steroids have been found in this plant. Various biological activities of M. charantia have been report...

  14. Structural Diversity and Biological Activities of Cyclic Depsipeptides from Fungi

    OpenAIRE

    Xiaohan Wang; Xiao Gong; Peng Li; Daowan Lai; Ligang Zhou

    2018-01-01

    Cyclic depsipeptides (CDPs) are cyclopeptides in which amide groups are replaced by corresponding lactone bonds due to the presence of a hydroxylated carboxylic acid in the peptide structure. These peptides sometimes display additional chemical modifications, including unusual amino acid residues in their structures. This review highlights the occurrence, structures and biological activities of the fungal CDPs reported until October 2017. About 352 fungal CDPs belonging to the groups of cycli...

  15. Biological Activities and Phytochemicals of Swietenia macrophylla King

    Directory of Open Access Journals (Sweden)

    Habsah Abdul Kadir

    2013-08-01

    Full Text Available Swietenia macrophylla King (Meliaceae is an endangered and medicinally important plant indigenous to tropical and subtropical regions of the World. S. macrophylla has been widely used in folk medicine to treat various diseases. The review reveals that limonoids and its derivatives are the major constituents of S. macrophylla. There are several data in the literature indicating a great variety of pharmacological activities of S. macrophylla, which exhibits antimicrobial, anti-inflammatory, antioxidant effects, antimutagenic, anticancer, antitumor and antidiabetic activities. Various other activities like anti-nociceptive, hypolipidemic, antidiarrhoeal, anti-infective, antiviral, antimalarial, acaricidal, antifeedant and heavy metal phytoremediation activity have also been reported. In view of the immense medicinal importance of S. macrophylla, this review aimed at compiling all currently available information on its ethnomedicinal uses, phytochemistry and biological activities of S. macrophylla, showing its importance.

  16. Chemical composition and biological activities of the Agaricus mushrooms

    Directory of Open Access Journals (Sweden)

    L Munkhgerel

    2014-10-01

    Full Text Available Two species of Agaricus mushroom grown in Mongolia were analyzed for their element content. Biological activity and chemical components study of Agaricus, grown in the Mongolian flora has been investigated for the first time. The ethanol extracts of dried Agaricus sp. mushrooms were analyzed for antioxidant activity on 1,1-diphenyl-2- picrylhydrazyl (DPPH radicals and interferon-like activity. The ethanol extracts from Agaricus arvensis showed the most potent radical scavenging activity. The IC50 of A. silvaticus and A. arvensis were 216 and 17.75 g/ml respectively. Among the twenty three mushroom extracts, the extracts from A. silvatisus and A. arvensis have shown the interferon-like activity. DOI: http://dx.doi.org/10.5564/mjc.v14i0.197Mongolian Journal of Chemistry 14 (40, 2013, p41-45

  17. DESIGN, SYNTHESIS AND ANTICANCER ACTIVITY OF SOME NOVEL 1,2,4-TRIAZOLES CARRYING BIOLOGICALLY ACTIVE SULFONAMIDE MOIETIES.

    Science.gov (United States)

    Ghorab, Mostafa M; Alsaid, Mansour S; Al-Dosari, Mohammed

    2016-09-01

    Thirteen novel 1, 2, 4-triazoles incorporating a biologically active sulfonamide moieties 1-13 were designed and synthesized. The structures of the prepared compounds were elucidated on the basis of elemental analyses, IR, 'H-NMR, "C-NMR and mass spectral data. All the newly synthesized compounds were evaluated for their in vino anticancer activity against various cancer cell lines. The corresponding triazole carrying a biologically active free sulfonamide with unsubstituted phenyl ring 1 and triazole bearing sulfonamide with dimethylpyrimidine 11 were the most potent in this study which showed higher activity than the reference drug 2',7'-dichlorofluorescein (DCF). Cytotoxic screening of the tested compounds could offer an encouraging framework in the field that may lead to the discovery of potent anticancer activity.

  18. Radiosynthesis of [131I]IAZGP via nucleophilic substitution and its biological evaluation as a hypoxia marker - is specific activity a factor influencing hypoxia-mapping ability of a hypoxia marker?

    International Nuclear Information System (INIS)

    Suehiro, Makiko; Burgman, Paul; Carlin, Sean; Burke, Sean; Yang Guangbin; Ouerfelli, Ouathek; Oehler-Janne, Christoph; O'Donoghue, Joseph; Ling, Clifton; Humm, John

    2009-01-01

    Introduction: The hypoxia marker IAZGP, 1-(6-deoxy-6-iodo-β-D-galactopyranosyl)-2-nitroimidazole, has been labeled with 123 I/ 124 I/ 125 I/ 131 I via iodine-radioiodine exchange, which gives the radiotracer in a specific activity of 10-90 MBq/μmol. We synthesized the same radiotracer possessing several hundred to thousand times higher specific activity (high-SA IAZGP) via nucleophilic substitution and compared its biological behavior with that of conventionally produced IAZGP (low-SA IAZGP) to determine if specific activity is a factor influencing cell uptake kinetics, biodistribution and intratumor microregional localization of the radiotracer. Methods: High-SA [ 131 I]IAZGP was prepared by substitution of the tosyl functionality with [ 131 I]iodide. In vitro uptake of high- and low-SA [ 131 I]IAZGP by HCT8 and HT29 cells was assessed in normoxic and hypoxic conditions. Biodistribution and intratumor localization of high- and low-SA [ 131 I]IAZGP were determined by injection into HT29 tumor-bearing mice. Results: The nucleophilic substitution reaction proceeded efficiently in acetonitrile at 150 o C, giving the final product in an average yield of 42% and an average specific activity of 30 GBq/μmol. In vitro, high-SA [ 131 I]IAZGP was incorporated into the tumor cells with similar kinetics and oxygen dependence to low-SA [ 131 I]IAZGP. In HT29 tumor-bearing mice, biodistributions of high- and low-SA [ 131 I]IAZGP were equivalent. Ex vivo autoradiography revealed heterogeneous intratumor localization of high-SA [ 131 I]IAZGP corresponding closely to distributions of other exogenous and endogenous hypoxia markers. Comparable microregional distribution patterns were observed with low-SA [ 131 I]IAZGP. Conclusions: Radiolabeled IAZGP produced via nucleophilic substitution is validated as an exogenous hypoxia marker. Specific activity does not appear to influence the in vivo hypoxia-mapping ability of the radiotracer.

  19. Adsorption of Heavy Metals on Biologically Activated Brown Coal Sludge

    Directory of Open Access Journals (Sweden)

    Mária Praščáková

    2005-11-01

    Full Text Available Adsorption of cooper (II and zinc (II ions from aqueous solutions on a biologically activated brown coal sludge was investigated. Four families of adsorbents were prepared from the brown coal sludge bya microorganism’s activity. There were used microscopic fungi such as Aspergillus niger, Aspergillus clavatus, Penicillium glabrum and Trichoderma viride. Prepared sorbents were capable of removing Cu (II and Zn (II. The sorption isotherm has been constructed and the specific metal uptake and the maximum capacity of the adsorbent have been determined.

  20. Total synthesis and biological evaluation of fluorinated cryptophycins

    Directory of Open Access Journals (Sweden)

    Christine Weiß

    2012-11-01

    Full Text Available Cryptophycins are cytotoxic natural products that exhibit considerable activities even against multi-drug-resistant tumor cell lines. As fluorinated pharmaceuticals have become more and more important during the past decades, fluorine-functionalized cryptophycins were synthesized and evaluated in cell-based cytotoxicity assays. The unit A trifluoromethyl-modified cryptophycin proved to be highly active against KB-3-1 cells and exhibited an IC50 value in the low picomolar range. However, the replacement of the 3-chloro-4-methoxyphenyl-substituent in unit B by a pentafluorophenyl moiety resulted in a significant loss of activity.

  1. Biological evaluation of certain substituted hydantoins and benzalhydantoins against microbes

    Science.gov (United States)

    Hidayat, Ika-Wiani; Thu, Yee Yee; Black, David St. C.; Read, Roger W.

    2016-02-01

    Twenty-three synthetic (thio)hydantoins and benzalhydantoins were evaluated for antimicrobial activity against Candida albicans, Malassezia furfur, Escherichia coli and Staphylococcus aureus, by the paper disc diffusion method. 3-n-butyl-4'-nitrobenzalhydantoin showed very high activity against E. coli and high selectivity with respect to the other microorganisms, while 3-n-butyl-2'-bromo-4',5'-dimethoxybenzal hydantoin demonstrated very high selectivity in its activity against M. furfur and S. aureus. These compounds show the most promise as drug lead compounds.

  2. On the mechanism of biological activation by tritium.

    Science.gov (United States)

    Rozhko, T V; Badun, G A; Razzhivina, I A; Guseynov, O A; Guseynova, V E; Kudryasheva, N S

    2016-06-01

    The mechanism of biological activation by beta-emitting radionuclide tritium was studied. Luminous marine bacteria were used as a bioassay to monitor the biological effect of tritium with luminescence intensity as the physiological parameter tested. Two different types of tritium sources were used: HTO molecules distributed regularly in the surrounding aqueous medium, and a solid source with tritium atoms fixed on its surface (tritium-labeled films, 0.11, 0.28, 0.91, and 2.36 MBq/cm(2)). When using the tritium-labeled films, tritium penetration into the cells was prevented. The both types of tritium sources revealed similar changes in the bacterial luminescence kinetics: a delay period followed by bioluminescence activation. No monotonic dependences of bioluminescence activation efficiency on specific radioactivities of the films were found. A 15-day exposure to tritiated water (100 MBq/L) did not reveal mutations in bacterial DNA. The results obtained give preference to a "non-genomic" mechanism of bioluminescence activation by tritium. An activation of the intracellular bioluminescence process develops without penetration of tritium atoms into the cells and can be caused by intensification of trans-membrane cellular processes stimulated by ionization and radiolysis of aqueous media. Copyright © 2016 Elsevier Ltd. All rights reserved.

  3. Distribution and biological activities of the flavonoid luteolin.

    Science.gov (United States)

    López-Lázaro, Miguel

    2009-01-01

    Epidemiological evidence suggests that flavonoids may play an important role in the decreased risk of chronic diseases associated with a diet rich in plant-derived foods. Flavonoids are also common constituents of plants used in traditional medicine to treat a wide range of diseases. The purpose of this article is to summarize the distribution and biological activities of one of the most common flavonoids: luteolin. This flavonoid and its glycosides are widely distributed in the plant kingdom; they are present in many plant families and have been identified in Bryophyta, Pteridophyta, Pinophyta and Magnoliophyta. Dietary sources of luteolin include, for instance, carrots, peppers, celery, olive oil, peppermint, thyme, rosemary and oregano. Preclinical studies have shown that this flavone possesses a variety of pharmacological activities, including antioxidant, anti-inflammatory, antimicrobial and anticancer activities. The ability of luteolin to inhibit angiogenesis, to induce apoptosis, to prevent carcinogenesis in animal models, to reduce tumor growth in vivo and to sensitize tumor cells to the cytotoxic effects of some anticancer drugs suggests that this flavonoid has cancer chemopreventive and chemotherapeutic potential. Modulation of ROS levels, inhibition of topoisomerases I and II, reduction of NF-kappaB and AP-1 activity, stabilization of p53, and inhibition of PI3K, STAT3, IGF1R and HER2 are possible mechanisms involved in the biological activities of luteolin.

  4. Radiation degradation of carbohydrates and their biological activities for plants

    International Nuclear Information System (INIS)

    Kume, T.; Nagasawa, N.; Matsuhashi, S.

    2000-01-01

    Radiation effects on carbohydrates such as chitosan, sodium alginate, carrageenan, cellulose, pectin have been investigated to improve the biological activities. These carbohydrates were easily degraded by irradiation and induced various kinds of biological activities such as anti-bacterial activity, promotion of plant growth, suppression of heavy metal stress, phytoalexins induction. Pectic fragments obtained from degraded pectin induced the phytoalexins such as glyceollins in soybean and pisatin in pea. The irradiated chitosan shows the higher elicitor activity for pisatin than that of pectin. For the plant growth promotion, alginate derived from brown marine algae, chitosan and ligno-cellulosic extracts show a strong activity. Kappa and iota carrageenan derived from red marine algae can promote growth of rice and the highest effect was obtained with kappa irradiated at 100 kGy. Some radiation degraded carbohydrates suppressed the damage of heavy metals on plants. The effects of irradiated carbohydrates on transportation of heavy metals have been investigated by PETIS (Positron Emitting Tracer Imaging System) and autoradiography using 48 V and 62 Zn. (author)

  5. Radiation degradation of carbohydrates and their biological activities for plants

    Energy Technology Data Exchange (ETDEWEB)

    Kume, T.; Nagasawa, N.; Matsuhashi, S. [Japan Atomic Energy Research Inst., Takasaki, Gunma (Japan). Takasaki Radiation Chemistry Research Establishment] [and others

    2000-03-01

    Radiation effects on carbohydrates such as chitosan, sodium alginate, carrageenan, cellulose, pectin have been investigated to improve the biological activities. These carbohydrates were easily degraded by irradiation and induced various kinds of biological activities such as anti-bacterial activity, promotion of plant growth, suppression of heavy metal stress, phytoalexins induction. Pectic fragments obtained from degraded pectin induced the phytoalexins such as glyceollins in soybean and pisatin in pea. The irradiated chitosan shows the higher elicitor activity for pisatin than that of pectin. For the plant growth promotion, alginate derived from brown marine algae, chitosan and ligno-cellulosic extracts show a strong activity. Kappa and iota carrageenan derived from red marine algae can promote growth of rice and the highest effect was obtained with kappa irradiated at 100 kGy. Some radiation degraded carbohydrates suppressed the damage of heavy metals on plants. The effects of irradiated carbohydrates on transportation of heavy metals have been investigated by PETIS (Positron Emitting Tracer Imaging System) and autoradiography using {sup 48}V and {sup 62}Zn. (author)

  6. Biological Activities of Phenolic Compounds of Extra Virgin Olive Oil

    Directory of Open Access Journals (Sweden)

    Maurizio Servili

    2013-12-01

    Full Text Available Over the last few decades, multiple biological properties, providing antioxidant, anti-inflammatory, chemopreventive and anti-cancer benefits, as well as the characteristic pungent and bitter taste, have been attributed to Extra Virgin Olive Oil (EVOO phenols. In particular, growing efforts have been devoted to the study of the antioxidants of EVOO, due to their importance from health, biological and sensory points of view. Hydrophilic and lipophilic phenols represent the main antioxidants of EVOO, and they include a large variety of compounds. Among them, the most concentrated phenols are lignans and secoiridoids, with the latter found exclusively in the Oleaceae family, of which the drupe is the only edible fruit. In recent years, therefore, we have tackled the study of the main properties of phenols, including the relationships between their biological activity and the related chemical structure. This review, in fact, focuses on the phenolic compounds of EVOO, and, in particular, on their biological properties, sensory aspects and antioxidant capacity, with a particular emphasis on the extension of the product shelf-life.

  7. Biological Activities of Phenolic Compounds of Extra Virgin Olive Oil.

    Science.gov (United States)

    Servili, Maurizio; Sordini, Beatrice; Esposto, Sonia; Urbani, Stefania; Veneziani, Gianluca; Di Maio, Ilona; Selvaggini, Roberto; Taticchi, Agnese

    2013-12-20

    Over the last few decades, multiple biological properties, providing antioxidant, anti-inflammatory, chemopreventive and anti-cancer benefits, as well as the characteristic pungent and bitter taste, have been attributed to Extra Virgin Olive Oil (EVOO) phenols. In particular, growing efforts have been devoted to the study of the antioxidants of EVOO, due to their importance from health, biological and sensory points of view. Hydrophilic and lipophilic phenols represent the main antioxidants of EVOO, and they include a large variety of compounds. Among them, the most concentrated phenols are lignans and secoiridoids, with the latter found exclusively in the Oleaceae family, of which the drupe is the only edible fruit. In recent years, therefore, we have tackled the study of the main properties of phenols, including the relationships between their biological activity and the related chemical structure. This review, in fact, focuses on the phenolic compounds of EVOO, and, in particular, on their biological properties, sensory aspects and antioxidant capacity, with a particular emphasis on the extension of the product shelf-life.

  8. PASS-predicted design, synthesis and biological evaluation of cyclic nitrones as nootropics.

    Science.gov (United States)

    Marwaha, Alka; Goel, R K; Mahajan, Mohinder P

    2007-09-15

    Out of 400 virtually designed imidazoline N-oxides, five cyclic nitrones were selected on the basis of PASS prediction as potent nootropics and were evaluated for their biological activities in albino mice. The selected N-alkyl and aryl-substituted nitrones were found to be excellent nootropics. A series of lead compounds acting as cognition enhancers have been provided, which can be further exploited in search of such New Chemical Entities (NCEs).

  9. Summary of diamino pyrazoles derived and study their biological activities

    International Nuclear Information System (INIS)

    Hagui, Marwa

    2016-01-01

    The work involves the synthesis of new heterocyclic structures diamino pyrazoles derivatives that are present in many natural products and products of pharmacological and therapeutic interests and study their biological activities. In order to develop a radiotracer interest and use in diagnostic nuclear medicine, we are interested to synthesis a pyrazole derivative with the precursor [Re(CO)5Br] and studying the antibacterial and antifungal activity of 3.5-diamino pyrazole and even thioamide complex rhenium. The objectives of our workout: 1/ Synthesis of molecules 3,5-diamino pyrazole and thioamide. 2/ Synthesis of 3,5-diamino pyrazole-rhenium complex. 3/ The in vitro study: Bacteriological Tests (Study of antibacterial and antifungal activity of 3,5-diamino pyrazole and thioamide). The first part of this work concerns the chemical synthesis of molecules such as: thioamide, Amp z1 Ampz2 and then we had synthesized the complex 3,5-diamino pyrazole-rhenium. Similarly we determined the physicochemical characteristics of the compounds synthesized by CLHP, CCM and RMN ( 1 H, 13 C). The second part is devoted to the study in vitro of biological activities of the synthesized molecules and complex 3,5 diaminopyrazole-rhenium with concentration 1 mg/mL and 2 mg/mL. The results allow us to say that the thioamide and Ampz2 have antibacterial activity against S. enterica and Ampz2 has low activity against S. aureus and P. aeruginossa. Other pyrazole derivatives have no significant antibacterial and antifungal activity. The results also show that the synthesized compounds of concentration 2 mg/mL in relation to the inhibition zones of amoxicillin and DMSO: 1/ Escherichia coli, there is antibacterial activity for thioamide, and the Amp z1-Re Ampz2 compound. 2/ Staphylococcus aureus, the complex Ampz 1-Re and the thioamide have significant antibacterial activity. 3/ Salmonella, we observe that the thioamide molecules, Ampz2 and Amp z1-Re have significant antibacterial activity

  10. The cell biology of T-dependent B cell activation

    DEFF Research Database (Denmark)

    Owens, T; Zeine, R

    1989-01-01

    The requirement that CD4+ helper T cells recognize antigen in association with class II Major Histocompatibility Complex (MHC) encoded molecules constrains T cells to activation through intercellular interaction. The cell biology of the interactions between CD4+ T cells and antigen-presenting cells...... includes multipoint intermolecular interactions that probably involve aggregation of both polymorphic and monomorphic T cell surface molecules. Such aggregations have been shown in vitro to markedly enhance and, in some cases, induce T cell activation. The production of T-derived lymphokines that have been...... implicated in B cell activation is dependent on the T cell receptor for antigen and its associated CD3 signalling complex. T-dependent help for B cell activation is therefore similarly MHC-restricted and involves T-B intercellular interaction. Recent reports that describe antigen-independent B cell...

  11. Biological activities of triazine derivatives. Combining DFT and QSAR results

    Directory of Open Access Journals (Sweden)

    Majdouline Larif

    2017-02-01

    Full Text Available In order to investigate the relationship between activities and structures, a 3D-QSAR study is applied to a set of 43 molecules based on triazines. This study was conducted using the principal component analysis (PCA method, the multiple linear regression method (MLR and the artificial neural network (ANN. The predicted values of activities are in good agreement with the experimental results. The artificial neural network (ANN techniques, considering the relevant descriptors obtained from the MLR, showed a correlation coefficient of 0.9 with an 8-3-1 ANN model which is a good result. As a result of quantitative structure–activity relationships, we found that the model proposed in this study is constituted of major descriptors used to describe these molecules. The obtained results suggested that the proposed combination of several calculated parameters could be useful to predict the biological activity of triazine derivatives.

  12. A comparison of the biological activities of four prostaglandins

    Science.gov (United States)

    Horton, E. W.; Main, I. H. M.

    1963-01-01

    The biological activities of prostaglandins E1, E2, E3 and F1α have been compared. Prostaglandins E1, E2, E3 were qualitatively similar; E1 and E2 were about equiactive, but E3 was less active on all preparations. Prostaglandin F1α was a less potent vasodilator than E1 on the cat gastrocnemius muscle blood flow and skin blood flow and a less potent depressor drug on rabbit blood pressure. On the rabbit isolated jejunum F1α was twice as active as E1 but on the guinea-pig isolated ileum E1 was about forty times more active than F1α. One qualitative difference between these prostaglandins was observed; on the rabbit fallopian tube in vivo prostaglandins of the E series decreased both the tone and the peristalsis of the tube whereas prostaglandin F1α increased tubal tone. ImagesFig. 2Fig. 3Fig. 5 PMID:14066143

  13. Biological activities of water-soluble fullerene derivatives

    Energy Technology Data Exchange (ETDEWEB)

    Nakamura, S; Mashino, T [Department of Pharmaceutical Sciences, Faculty of Pharmacy, Keio University, 1-5-30 Shiba-koen, Minato-ku, Tokyo 105-8512 (Japan)], E-mail: mashino-td@pha.keio.ac.jp

    2009-04-01

    Three types of water-soluble fullerene derivatives were synthesized and their biological activities were investigated. C{sub 60}-dimalonic acid, an anionic fullerene derivative, showed antioxidant activity such as quenching of superoxide and relief from growth inhibition of E. coli by paraquat. C{sub 60}-bis(7V,7V-dimethylpyrrolidinium iodide), a cationic fullerene derivative, has antibacterial activity and antiproliferative effect on cancer cell lines. The mechanism is suggested to be respiratory chain inhibition by reactive oxygen species produced by the cationic fullerene derivative. Proline-type fullerene derivatives showed strong inhibition activities on HIV-reverse transcriptase. The IC{sub 50} values were remarkably lower than nevirapine, a clinically used anti-HIV drug. Fullerene derivatives have a big potential for a new type of lead compound to be used as medicine.

  14. Synthesis, Biological Activity and Preliminary in Silico ADMET Screening of Polyamine Conjugates with Bicyclic Systems.

    Science.gov (United States)

    Szumilak, Marta; Galdyszynska, Malgorzata; Dominska, Kamila; Bak-Sypien, Irena I; Merecz-Sadowska, Anna; Stanczak, Andrzej; Karwowski, Boleslaw T; Piastowska-Ciesielska, Agnieszka W

    2017-05-12

    Polyamine conjugates with bicyclic terminal groups including quinazoline, naphthalene, quinoline, coumarine and indole have been obtained and their cytotoxic activity against PC-3, DU-145 and MCF-7 cell lines was evaluated in vitro. Their antiproliferative potential differed markedly and depended on both their chemical structure and the type of cancer cell line. Noncovalent DNA-binding properties of the most active compounds have been examined using ds-DNA thermal melting studies and topo I activity assay. The promising biological activity, DNA intercalative binding mode and favorable drug-like properties of bis(naphthalene-2-carboxamides) make them a good lead for further development of potential anticancer drugs.

  15. Waste rock revegetation: Evaluation of nutrient and biological amendments

    Energy Technology Data Exchange (ETDEWEB)

    Meikle, T.W.; Lu, S.; Barta, J.P.

    1999-07-01

    Lack of salvaged topsoil for the reclamation of historical waste rock piles is a common problem in the arid Great Basin region. Utilization of amended waste rock as a growth media could reduce further disturbance resulting from topsoil harvest, minimize hauling costs, and potentially allow for the use of a higher quality material for plant growth. Getchell Gold Corporation initiated a study in 1995 to determine the suitability of waste rock substrates to support plant growth following application of nutrient and biological amendments. Three nutrient amendments and a biological seed treatment were evaluation for use in establishing vegetative cover on three distinct waste rock substrates. Completely randomized blocks were placed on the three substrates. Treatments included organic fertilizers (Biosol and Gro-Power), a mineral fertilizer (16-20-0), and Azospirillum bacterial inoculant, plus controls. The seed mix consisted of Agropyron riparium, Agropyron spicatum, Elymus cinereus, Poa secunda, and Sitanion hystrix. Canopy and ground cover were monitored for three growing seasons. Conclusions from the study are: (1) two of the three substrates supported plant growth following amendment with organic fertilizers; (2) organic fertilizers increased cover substantially over the mineral fertilizer; and (3) Azospirillum had no effect on canopy cover.

  16. Use of the Immunegenetical Methods for Biological Risks Evaluation

    International Nuclear Information System (INIS)

    Pozdnyakova, L.; Stopchanskaya, A.; Parkhomenko, N.; Pilipenko, N.; Kostyuchenko, L.; Djurtubaeva, G.; Slavina, N.; Pozdnyakov, S.

    2007-01-01

    For the present biological risk evaluation and forecast, information on gene-phenotypic characteristics of circulating regional EDAs, their connatural sources and conditions for epidemic distribution is necessary. We lead a relative gene-phenotypic comparison of vaccine and wild F.tularensis strains isolated from carriers, vectors, environment and patients in the different natural foci. Phenotyping investigations were done on 'in vitro' model with use of the human peripheral blood immune competent cells (ICC) of non-vaccinated and vaccinated with LVS volunteers. Variations of virulence manifestations of F.tularensis strains, isolated from different sources (ticks, waters, patients) are revealed. Principal differences in interactions of ICC with strains of various virulence degree, presence of ICC structural-functional changes in cytokines secretion dynamics at the presence of the wild and vaccine strains are shown. Morphological proofs for toxic materials production by pathogen during reproductive development term, damaging membranes structure, nucleus and cytoplasm are received. Certain interrelations between isolates phenotypic characteristics, source of isolation and types of natural foci is revealed. VNTR-analysis has showed genotypical heterogeneity and specific peculiarities in VNTR locuses combination of F. tularensis strains from different sources. Biological sense of VNTR-locuses combinations variations and their influence upon virulence signs expression are discussed. The complex approach, including agent's gene-phenotypic characteristics, ecological and geographical features of the natural foci, level of the human recruitment into the epidemic process will promote development of measures for counteraction in case of agents and their modified variants deliberate use. (author)

  17. Upshot of the ripening time on biological activities, phenol content ...

    African Journals Online (AJOL)

    Anis

    2013-10-02

    Oct 2, 2013 ... Total phenol content and the antioxidant activities of three cultivars of Opuntia ficus-indica (L.) Mill. were evaluated. The results show that the ecotypes were significantly different according to their fatty acid composition, antioxidant and antibacterial activity, as well as their polyphenol profiles. Rossa fruit.

  18. Upshot of the ripening time on biological activities, phenol content ...

    African Journals Online (AJOL)

    Total phenol content and the antioxidant activities of three cultivars of Opuntia ficus-indica (L.) Mill. were evaluated. The results show that the ecotypes were significantly different according to their fatty acid composition, antioxidant and antibacterial activity, as well as their polyphenol profiles. Rossa fruit collected in August ...

  19. European activities in space radiation biology and exobiology

    International Nuclear Information System (INIS)

    Horneck, G.

    1996-01-01

    In view of the space station era, the European Space Agency has initiated a review and planning document for space life sciences. Radiation biology includes dosimetry of the radiation field and its modification by mass shielding, studies on the biological responses to radiation in space, on the potential impact of space flight environment on radiation effects, and assessing the radiation risks and establishing radiation protection guidelines. To reach a better understanding of the processes leading to the origin, evolution and distribution of life, exobiological activities include the exploration of the solar system, the collection and analysis of extraterrestrial samples and the utilization of space as a tool for testing the impact of space environment on organics and resistant life forms. (author)

  20. Chemical constituents and biological activities of the genus Linaria (Scrophulariaceae).

    Science.gov (United States)

    Cheriet, Thamere; Mancini, Ines; Seghiri, Ramdane; Benayache, Fadila; Benayache, Samir

    2015-01-01

    This is a review on 95 references dealing with the genus Linaria (Scrophularioideae-Antirrhineae tribe), a known genus of the Scrophulariaceae family, which comprises about 200 species mainly distributed in Europe, Asia and North Africa. The use of some Linaria species in folk medicine has attracted the attention for chemical and biological studies. This report is aimed to be a comprehensive overview on the isolated or identified known and often new metabolites from the 41 Linaria species so far cited. It is organised presenting first the phytochemical classes of alkaloids, polyphenols including flavonoids, the latter being quite diffused and mostly present as flavones, flavonols and their glycosides, and terpenoids including iridoids and steroids. Second, the results from biological investigation on plant extracts, pure natural products isolated from Linaria species and some synthetic derivatives are reported, with antitumour, anti-acetylcholinesterase, anti-inflammatory and analgesic, antioxidant and antibacterial activities.

  1. Evaluation of Pigeon Pea Lines for Biological Soil Decompaction

    Directory of Open Access Journals (Sweden)

    Rodolfo Godoy

    2009-01-01

    Full Text Available Soil decompaction is generally achieved through mechanical cultivation practices; however biological processes can significantly add to this process through root growth, development, and later senescence. This study was carried out in Piracicaba, SP, Brazil and had the purpose of selecting, among forty one pure pigeon pea lines, the most efficient genotypes that promote soil decompaction by roots penetrating compacted soil layers. Utilizing artificially compacted 30 mm high soil blocks, in a series of experiments, these lines were compared to the cultivar Fava Larga taken as a standard. Three lines were preliminarily selected out of the initial group, and afterwards, in more detailed screenings by monitoring soil resistance to penetration and also evaluating the behavior of Tanzania grass plants seeded after pigeon pea, two of them, g5-94 and g8-95, were selected as possessing the most fit root system to penetrate compacted soil layers.

  2. Comparative SPR study on the effect of nanomaterials on the biological activity of adsorbed proteins

    International Nuclear Information System (INIS)

    Mei, Q.; Chen, Y.; Hong, J.; Chen, H.; Ding, X.; Yin, Y.; Koh, K.; Lee, J.

    2012-01-01

    Bioactivity of proteins is evaluated to test the adverse effects of nanoparticles interjected into biological systems. Surface plasmon resonance (SPR) spectroscopy detects binding affinity that is normally related to biological activity. Utilizing SPR spectroscopy, a concise testing matrix is established by investigating the adsorption level of bovine serum albumin (BSA) and anti-BSA on the surface covered with 11-mercaptoundecanoic acid (MUA); magnetic nanoparticles (MNPs) and single-walled carbon nanotubes (SWCNTs), respectively. The immunoactivity of BSA on MNPs and SWCNT decreased by 18 % and 5 %, respectively, compared to that on the gold film modified with MUA. This indicates that MNPs cause a considerable loss of biological activity of adsorbed protein. This effect can be utilized for practical applications on detailed biophysical research and nanotoxicity studies. (author)

  3. Evaluation of conformal radiotherapy techniques through physics and biologic criteria

    International Nuclear Information System (INIS)

    Bloch, Jonatas Carrero

    2012-01-01

    In the fight against cancer, different irradiation techniques have been developed based on technological advances and aiming to optimize the elimination of tumor cells with the lowest damage to healthy tissues. The radiotherapy planning goal is to establish irradiation technical parameters in order to achieve the prescribed dose distribution over the treatment volumes. While dose prescription is based on radiosensitivity of the irradiated tissues, the physical calculations on treatment planning take into account dosimetric parameters related to the radiation beam and the physical characteristics of the irradiated tissues. To incorporate tissue's radiosensitivity into radiotherapy planning calculations can help particularize treatments and establish criteria to compare and elect radiation techniques, contributing to the tumor control and the success of the treatment. Accordingly, biological models of cellular response to radiation have to be well established. This work aimed to study the applicability of using biological models in radiotherapy planning calculations to aid evaluating radiotherapy techniques. Tumor control probability (TCP) was studied for two formulations of the linear-quadratic model, with and without repopulation, as a function of planning parameters, as dose per fraction, and of radiobiological parameters, as the α/β ratio. Besides, the usage of biological criteria to compare radiotherapy techniques was tested using a prostate planning simulated with Monte Carlo code PENELOPE. Afterwards, prostate planning for five patients from the Hospital das Clinicas da Faculdade de Medicina de Ribeirao Preto, USP, using three different techniques were compared using the tumor control probability. In that order, dose matrices from the XiO treatment planning system were converted to TCP distributions and TCP-volume histograms. The studies performed allow the conclusions that radiobiological parameters can significantly influence tumor control

  4. A systematic development and evaluation of an undergraduate course in zoo biology

    Science.gov (United States)

    Burchfield, Patrick Mullen

    The biology curricula offered by most institutions of higher education follow a classic pattern of basic taxonomy, phylogeny, physiology, genetics, molecular biology and biometry. This course regimen certainly provides a knowledge structure within the discipline, but is somewhat lacking in information that is directly applicable within the field of zoo biology. The zoo biology curriculum set forth in this dissertation was designed to offer students immersion into the rapidly evolving field of zoo biology. It also offers insight and perspectives into the zoo profession, encompassing 185 accredited zoological parks and aquariums, which employ numerous biologists. There is not a degree granting college or university in Texas that currently offers coursework in this specialization. In order to determine the merit and worth of a course in zoo biology, a field trial and a revised course were presented and subjected to a systematic evaluation. Four evaluative categories were utilized following Benton's (1992) design: (a) consistency between terminal performance objectives, activities and test instrument items, (b) effect on scientific knowledge, (c) activity usefulness as perceived by course participants and the instructor, (d) course worth. Student (N = 49) and component data were measured using a pre-post-test design, a questionnaire, and other informal instruments during the antecedent, transaction and outcome phases. Data from the pre-post-tests were analyzed using t-tests for correlated means. The analysis of activities and test items indicated that they were consistent with the terminal performance objectives. The pre-post-test results indicated that the course had a positive effect on knowledge gain within the field of study. A significant statistical difference was found between the test means at a probability of p ≤ 0.001. A post course attitudinal questionnaire elicited a rating of 4.65 on a Likert scale of 5.0 on perceived usefulness to the participants. A

  5. Investigating Biological Activity Spectrum for Novel Styrylquinazoline Analogues

    Directory of Open Access Journals (Sweden)

    Jaroslaw Polanski

    2009-10-01

    Full Text Available In this study, series of ring-substituted 2-styrylquinazolin-4(3H-one and 4-chloro-2-styrylquinazoline derivatives were prepared. The syntheses of the discussed compounds are presented. The compounds were analyzed by RP-HPLC to determine lipophilicity. They were tested for their inhibitory activity on photosynthetic electron transport (PET in spinach (Spinacia oleracea L. chloroplasts. Primary in vitro screening of the synthesized compounds was also performed against four mycobacterial strains and against eight fungal strains. Several compounds showed biological activity comparable with or higher than that of the standard isoniazid. It was found that the electronic properties of the R substituent, and not the total lipophilicity of the compound, were decisive for the photosynthesis-inhibiting activity of tested compounds.

  6. Biochemical studies on certain biologically active nitrogenous compounds

    International Nuclear Information System (INIS)

    Abdel kader, S.M.; El Sayed, M.M.; El Malt, E.A.; Shaker, E.S.; Abdel Aziz, H.G.

    2010-01-01

    Certain biologically active nitrogenous compounds such as alkaloids are widely distributed in many wild and medicinal plants such as peganum harmala L. (Phycophyllaceae). However, less literature cited on the natural compounds was extracted from the aerial parts of this plant; therefore this study was conducted on harmal leaves using several solvents. Data indicated that methanol extract was the inhibitoriest effect against some pathogenic bacteria, particularly Streptococcus pyogenus. Chromatographic separation illustrated that presence of four compounds; the most active one was the third compound (3). Elementary analysis (C, H, N) revealed that the primary chemical structure of the active antibacterial compound (C3) was: C17 H21 N3 O7 S with molecular weight 411. Spectroscopic analysis proved that coninical structure was = 1- thioformyl, 8?- D glucoperanoside- Bis- 2, 3 dihydroisopyridino pyrrol. This new compound is represented as a noval ?- carboline alkaloid compound

  7. Synthesis of Mono-PEGylated Growth Hormone Releasing Peptide-2 and Investigation of its Biological Activity.

    Science.gov (United States)

    Hu, Xiaoyu; Xu, Beihua; Zhou, Ziniu

    2015-10-01

    The purpose of this study was to investigate an efficient synthetic route to the mono-PEGylated growth hormone releasing peptide-2 (GHRP-2) and its biological activity in vivo. The commercially available key PEGylating reagent, mPEG-NHS ester, was successfully utilized to the synthesis of mono-PEGylated GHRP-2, during which the PEGylation profiles of GHRP-2 were monitored by high-performance liquid chromatography (HPLC). The product was purified by cation exchange chromatography, and its biological activity was conducted in rats. The desired mono-PEGylated GHRP-2 as the major product was readily obtained in anhydrous aprotic solvent, such as dimethyl formamide (DMF) and dimethylsulfoxide (DMSO), when the molar ratio of mPEG-NHS ester to GHRP-2 was fixed to be 0.8:1. The products were characterized by matrix-assisted laser desorption ionization time-of-flight (MALDI-TOF) mass spectrometry. The evaluation of the biological activity for the products showed that the mono-PEGylated GHRP-2 gave a more stable activity than GHRP-2, suggesting that PEGylation led to the increase in the half-life of GHRP-2 in plasma without greatly impairing the biological activity. PEGylation of the GHRP-2 is a good choice for the development of the GHRP-2 applications.

  8. Activating and inhibiting connections in biological network dynamics

    Directory of Open Access Journals (Sweden)

    Knight Rob

    2008-12-01

    Full Text Available Abstract Background Many studies of biochemical networks have analyzed network topology. Such work has suggested that specific types of network wiring may increase network robustness and therefore confer a selective advantage. However, knowledge of network topology does not allow one to predict network dynamical behavior – for example, whether deleting a protein from a signaling network would maintain the network's dynamical behavior, or induce oscillations or chaos. Results Here we report that the balance between activating and inhibiting connections is important in determining whether network dynamics reach steady state or oscillate. We use a simple dynamical model of a network of interacting genes or proteins. Using the model, we study random networks, networks selected for robust dynamics, and examples of biological network topologies. The fraction of activating connections influences whether the network dynamics reach steady state or oscillate. Conclusion The activating fraction may predispose a network to oscillate or reach steady state, and neutral evolution or selection of this parameter may affect the behavior of biological networks. This principle may unify the dynamics of a wide range of cellular networks. Reviewers Reviewed by Sergei Maslov, Eugene Koonin, and Yu (Brandon Xia (nominated by Mark Gerstein. For the full reviews, please go to the Reviewers' comments section.

  9. Synthesis and biological activities of turkesterone 11?-acyl derivatives

    Directory of Open Access Journals (Sweden)

    Laurence Dinan

    2003-02-01

    Full Text Available Turkesterone is a phytoecdysteroid possessing an 11alpha-hydroxyl group. It is an analogue of the insect steroid hormone 20-hydroxyecdysone. Previous ecdysteroid QSAR and molecular modelling studies predicted that the cavity of the ligand-binding domain of the ecdysteroid receptor would possess space in the vicinity of C-11/C-12 of the ecdysteroid. We report the regioselective synthesis of a series of turkesterone 11alpha-acyl derivatives in order to explore this possibility. The structures of the analogues have been unambiguously determined by spectroscopic means (NMR and low-resolution mass spectrometry. Purity was verified by HPLC. Biological activities have been determined in Drosophila melanogaster BII cell-based bioassay for ecdysteroid agonists and in an in vitro radioligand-displacement assay using bacterially expressed D. melanogaster EcR/USP receptor proteins. The 11alpha-acyl derivatives do retain a significant amount of biological activity relative to the parent ecdysteroid. Further, although activity initially drops with the extension of the acyl chain length (C2 to C4, it then increases (C6 to C10, before decreasing again (C14 and C20. The implications of these findings for the interaction of ecdysteroids with the ecdysteroid receptor and potential applications in the generation of affinity-labelled and fluorescently-tagged ecdysteroids are discussed.

  10. Immunoglobulin preparations for intravenous administration. A review of their biologic activities and comparison of various preparation methods

    DEFF Research Database (Denmark)

    Nielsen, H

    1994-01-01

    procedures are employed by different commercial suppliers of immunoglobulins, and from the literature it appears that various important biologic functions, e.g., opsonic activity, complement fixation, and Fc-receptor function, are subject to alterations during the preparation. The best preservation...... of such activity, when assessed in vitro, is obtained with polyethylene glycol precipitation or DEAE-Sephadex fractionation, whereas enzymatic or chemical treatment can potentially reduce the biologic activity. It is recommended that immunoglobulin preparations be evaluated in vitro for intact biologic function...

  11. Synthesis and Evaluation of in Vitro Biological Activity of 4-Substituted Arylpiperazine Derivatives of 1,7,8,9-Tetrachloro-10,10-dimethoxy-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione

    Directory of Open Access Journals (Sweden)

    David Collu

    2009-12-01

    Full Text Available A series of twenty arylpiperazine derivatives of 1,7,8,9-tetrachloro-10,10-dimethoxy-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione have been prepared. These derivatives were tested in vitro with the aim of identifying novel lead compounds active against emergent and re-emergent human and cattle infectious diseases (AIDS, hepatitis B and C, tuberculosis, bovine viral diarrhea. In particular, these compounds were evaluated in vitro against representatives of different virus classes, such as a HIV-1 (Retrovirus, a HBV (Hepadnavirus and the single-stranded RNA+ viruses Yellow fever virus (YFV and Bovine viral diarrhea virus (BVDV, both belonging to the Flaviridae. Compounds 2c, 2g and 3d showed a modest activity against CVB-2. The molecular structures of the starting imide 1 and one of propyl-piperazine derivatives, 3b, have been determined by an X-ray crystallography study.

  12. Nanodiamonds as Carriers for Address Delivery of Biologically Active Substances

    Directory of Open Access Journals (Sweden)

    Petunin AI

    2010-01-01

    Full Text Available Abstract Surface of detonation nanodiamonds was functionalized for the covalent attachment of immunoglobulin, and simultaneously bovine serum albumin and Rabbit Anti-Mouse Antibody. The nanodiamond-IgGI125 and RAM-nanodiamond-BSAI125 complexes are stable in blood serum and the immobilized proteins retain their biological activity. It was shown that the RAM-nanodiamond-BSAI125 complex is able to bind to the target antigen immobilized on the Sepharose 6B matrix through antibody–antigen interaction. The idea can be extended to use nanodiamonds as carriers for delivery of bioactive substances (i.e., drugs to various targets in vivo.

  13. Detection of biologically active diterpenoic acids by Raman Spectroscopy

    DEFF Research Database (Denmark)

    Talian, Ivan; Orinak, Andrej; Efremov, Evtim V.

    2010-01-01

    is not suitable for their unambiguous identification, especially not in solution. We attempted to increase the sensitivity by applying UV-resonance Raman spectroscopy and surface-enhanced Raman spectroscopy (SERS) techniques. The UV-Raman spectra of the three compounds in ethanol/water 50 : 50 showed only very......Three poorly detectable, biologically active diterpenoic acids, kaurenoic, abietic, and gibberellic acid, were studied by using different modes of Raman spectroscopy. Because of their structural similarities, in the absence of strongly polarizable groups, conventional Raman spectroscopy...

  14. Secondary metabolites and biological activity of Pentas species: A minireview

    Directory of Open Access Journals (Sweden)

    Heba-tollah M. Sweelam

    2018-03-01

    Full Text Available The genus Pentas belongs to the Rubiaceae family, which contains approximately 40 species. Several Pentas species were reported to be used as a folk treatment by African indigenous people in treating some diseases such as malaria, tapeworms, dysentery, gonorrhea, syphilis and snake poisoning. This article covers the period from 1962 to 2017 and presents an overview of the biological activity of different Pentas species and describes their phytochemical traits. As a conclusion, the main secondary metabolites from Pentas species are quinones, highly oxygenated chromene-based structures, and iridoids. Pentas species are widely used in folk medicine but they have to be more investigated for their medicinal properties.

  15. In vitro biological evaluation of 100 selected methanol extracts from the traditional medicinal plants of Asia.

    Science.gov (United States)

    Li, Chunmei; Wang, Myeong-Hyeon

    2014-04-01

    In Asia, various medicinal plants have been used as the primary sources in the health care regimen for thousands of years. In recent decades, various studies have investigated the biological activity and potential medicinal value of the medicinal plants. In this study, 100 methanol extracts from 98 plant species were evaluated for their biological activities. The research properties, including 1,1-diphenyl-2-pic-rylhydrazyl (DPPH) radical scavenging activity, α-glucosidase and α-tyrosinase inhibitory effects, anti-inflammatory activity, and anticancer activity were evaluated for the selected extracts. Fifteen of the extracts scavenged more than 90% of the DPPH radical. Among the extracts, approximately 20 extracts showed a strong inhibitory effect on α-glucosidase, while most had no effect on α-tyrosinase. In addition, 52% of the extracts showed low toxicity to normal cells, and parts of the extracts exhibited high anti-inflammatory and anticancer activities on the murine macrophage cell (RAW 264.7) and human colon cancer cell (HT-29) lines, respectively. Our findings may contribute to further nutrition and pharmacological studies. Detailed investigations of the outstanding samples are currently underway.

  16. Radio-active waste disposal and deep-sea biology

    International Nuclear Information System (INIS)

    Rice, A.L.

    1978-01-01

    The deep-sea has been widely thought of as a remote, sparsely populated, and biologically inactive environment, well suited to receive the noxious products of nuclear fission processes. Much of what is known of abyssal biology tends to support this view, but there are a few disquieting contra-indications. The realisation, in recent years, that many animal groups show a previously unsuspected high species diversity in the deep-sea emphasized the paucity of our knowledge of this environment. More dramatically, the discovery of a large, active, and highly mobile abysso-bentho-pelagic fauna changed the whole concept of abyssal life. Finally, while there is little evidence for the existence of vertical migration patterns linking the deep-sea bottom communities with those of the overlying water layers, there are similarly too few negative results for the possibility of such transport mechanisms to be dismissed. In summary, biological knowledge of the abyss is insufficient to answer the questions raised in connection with deep-sea dumping, but in the absence of adequate answers it might be dangerous to ignore the questions

  17. Discovery of diethyl 2,5-diaminothiophene-3,4-dicarboxylate derivatives as potent anticancer and antimicrobial agents and screening of anti-diabetic activity: synthesis and in vitro biological evaluation. Part 1.

    Science.gov (United States)

    Bozorov, Khurshed; Ma, Hai-Rong; Zhao, Jiang-Yu; Zhao, Hai-Qing; Chen, Hua; Bobakulov, Khayrulla; Xin, Xue-Lei; Elmuradov, Burkhon; Shakhidoyatov, Khusnutdin; Aisa, Haji A

    2014-09-12

    Series of diethyl 2,5-diaminothiophene-3,4-dicarboxylate (DDTD) derivatives: azomethines of DDTD (2a-l) have been synthesized and screened for their anticancer, antimicrobial and anti-diabetic activities. The novel synthesized compounds were characterized by (1)H, (13)C NMR, MS and FT-IR analyses. All compounds were evaluated for their antiproliferative activity against three types of cancer cell line such as T47D and MCF-7 (human breast cancer), Hela (human cervical cancer) and Ishikawa (human endometrial cancer) lines. The results showed that most compounds exhibited significant antiproliferative activity against breast cancer cells. The majority of azomethines DDTD influenced strongly against breast cancer cells T47D and MCF-7, among them compounds 2b (2.3 μM), 2c (12.1 μM), 2e (13.2 μM), 2i (14.9 μM), 2j (16.0 μM), 2k (7.1 μM), 2l (8.6 μM) manifest potent anticancer activity against cancer cell T47D than Doxorubicin (DOX, 15.5 μM). Compound 2j has shown potent activity on all three types of cancer cells concurrently and IC50 values were considerably low in comparison with positive control DOX. In addition, all compounds were tested for antimicrobial activity against Staphylococcus aureus ATCC 6538 (Gram positive bacteria), Escherichia coli ATCC 11229 (Gram negative bacteria) and Candida albicans ATCC 10231 (Fungi) strains and 2j which contains in the ring nitrofurfural fragment, showed the highest effect on the three species of microbial pathogens simultaneously. Some compounds induced enzymatic inhibition in a concentration-dependent manner on PTP-1B inhibitor. Copyright © 2014. Published by Elsevier Masson SAS.

  18. Hippeastrum reticulatum (Amaryllidaceae: Alkaloid Profiling, Biological Activities and Molecular Docking

    Directory of Open Access Journals (Sweden)

    Luciana R. Tallini

    2017-12-01

    Full Text Available The Amaryllidaceae family has proven to be a rich source of active compounds, which are characterized by unique skeleton arrangements and a broad spectrum of biological activities. The aim of this work was to perform the first detailed study of the alkaloid constituents of Hippeastrum reticulatum (Amaryllidaceae and to determine the anti-parasitological and cholinesterase (AChE and BuChE inhibitory activities of the epimers (6α-hydroxymaritidine and 6β-hydroxymaritidine. Twelve alkaloids were identified in H. reticulatum: eight known alkaloids by GC-MS and four unknown (6α-hydroxymaritidine, 6β-hydroxymaritidine, reticulinine and isoreticulinine by NMR. The epimer mixture (6α-hydroxymaritidine and 6β-hydroxymaritidine showed low activity against all protozoan parasites tested and weak AChE-inhibitory activity. Finally, a molecular docking analysis of AChE and BuChE proteins showed that isoreticulinine may be classified as a potential inhibitory molecule since it can be stabilized in the active site through hydrogen bonds, π-π stacking and hydrophobic interactions.

  19. Biological activities of the sulfated polysaccharide from the vascular plant Halodule wrightii

    Directory of Open Access Journals (Sweden)

    Juliana M. C. Silva

    2012-02-01

    Full Text Available A sulfated polysaccharide (SPSG was successfully isolated from seagrass Halodule wrightii Asch., Cymodoceaceae, and its antioxidant and anticoagulant activities were investigated. The data presented here showed that the SPSG is a 11 kDa sulfated heterogalactan with a sulfatation degree of 20.63% and it also contains glucose and xylose. SPSG antioxidant activities were evaluated using several in vitro assays and the anticoagulant activity was evaluated by aPTT and PT tests. These assays suggested that the SPSG possessed remarkable antioxidant properties in different in vitro assays and an outstanding anticoagulant activity 2.5-fold higher than that of heparin Clexane® in the aPTT test. This data represents the first reported on the sulfated polysaccharide biological activities from seagrass. These results indicate that SPSG can be considered in the future as a drug utilized in treating diseases from these systems.

  20. Effects of Integrated Fixed Film Activated Sludge on nitrogen removal in biological nutrient removal systems

    OpenAIRE

    Jensen, Keith R.

    1995-01-01

    The performance of Integrated Fixed Film Activated Sludge (IFAS) was evaluated for its effect on nitrification and denitrification in a bench scale biological nutrient removal (BNR) process configured as a Virginia Initiative Project (VIP) process. The IFAS systems consisted of a sponge - like biomass support system (Captor) operated in the aerobic zone of two independent treatment trains, and a fibrous biomass support system (Ringlace) operated in the aerobic zone of one indep...

  1. Facile Chemical Access to Biologically Active Norcantharidin Derivatives from Biomass

    Directory of Open Access Journals (Sweden)

    Konstantin I. Galkin

    2017-12-01

    Full Text Available Reductive amination of 2,5-diformylfuran (DFF was used to implement the transition from bio-derived 5-hydroxymethylfurfural (HMF to pharmaceuticals. The synthesized bis(aminomethylfurans were utilized as building blocks for the construction of new derivatives with structural cores of naturally occurring biologically active compounds. Using the one-pot procedure, which included the Diels–Alder reaction followed by hydrogenation of the double bond, bio-derived analogues of the anticancer drug norcantharidin were obtained. The cyclization process was diastereoselective, and resulted in the formation of tricyclic products with the endo configuration. Analysis of cytotoxycity for the resulting tricyclic amine-containing compounds showed an increase of anticancer activity as compared with the unsubstituted norcantharimide.

  2. Structural Diversity and Biological Activities of the Cyclodipeptides from Fungi

    Directory of Open Access Journals (Sweden)

    Xiaohan Wang

    2017-11-01

    Full Text Available Cyclodipeptides, called 2,5-diketopiperazines (2,5-DKPs, are obtained by the condensation of two amino acids. Fungi have been considered to be a rich source of novel and bioactive cyclodipeptides. This review highlights the occurrence, structures and biological activities of the fungal cyclodipeptides with the literature covered up to July 2017. A total of 635 fungal cyclodipeptides belonging to the groups of tryptophan-proline, tryptophan-tryptophan, tryptophan–Xaa, proline–Xaa, non-tryptophan–non-proline, and thio-analogs have been discussed and reviewed. They were mainly isolated from the genera of Aspergillus and Penicillium. More and more cyclodipeptides have been isolated from marine-derived and plant endophytic fungi. Some of them were screened to have cytotoxic, phytotoxic, antimicrobial, insecticidal, vasodilator, radical scavenging, antioxidant, brine shrimp lethal, antiviral, nematicidal, antituberculosis, and enzyme-inhibitory activities to show their potential applications in agriculture, medicinal, and food industry.

  3. Established and emerging biological activity markers of inflammatory bowel disease

    DEFF Research Database (Denmark)

    Nielsen, O H; Vainer, B; Madsen, S M

    2000-01-01

    Assessment of disease activity in inflammatory bowel disease (IBD), i.e., ulcerative colitis (UC) and Crohn's disease (CD), is done using clinical parameters and various biological disease markers. Ideally, a disease marker must: be able to identify individuals at risk of a given disorder......, be disease specific, mirror the disease activity and, finally, be easily applicable for routine clinical purposes. However, no such disease markers have yet been identified for IBD. In this article, classical disease markers including erythrocyte sedimentation rate, acute phase proteins (especially...... orosomucoid and CRP), leukocyte and platelet counts, albumin, neopterin, and beta2-microglobulin will be reviewed together with emerging disease markers such as antibodies of the ANCA/ASCA type, cytokines (e.g., IL-1, IL-2Ralpha, IL-6, IL-8, TNF-alpha, and TNF-alpha receptors) and with various adhesion...

  4. Enhanced biological activity of carotenoids stabilized by phenyl groups.

    Science.gov (United States)

    You, Ji Suk; Jeon, Sunhwa; Byun, Youn Jung; Koo, Sangho; Choi, Shin Sik

    2015-06-15

    Carotenoids are lipid soluble food ingredients with multifunction including antioxidant and anticancer activities. However, carotenoids are destructively oxidized upon reaction with radicals resulting in toxic effects on biological systems. Two synthetic carotenoids (BAS and BTS) containing the aromatic phenyl groups with a para-substituent (OMe and Me, respectively) at C-13 and C-13' position were prepared in order to overcome a structural instability of carotenoid. Both BAS and BTS exerted stronger radical scavenging activity than β-carotene in DPPH and ABTS assays. In particular, BTS significantly reduced in vivo ROS (reactive oxygen species) levels and improved body growth and reproduction of Caenorhabditiselegans. BTS has a great potential for the advanced and modified carotenoid material with stability leading to enhanced bioavailability. Copyright © 2015 Elsevier Ltd. All rights reserved.

  5. Synthesis and Biological Activity of Reversed Pyrimidine Nucleosides

    Directory of Open Access Journals (Sweden)

    Nataša Župančić

    2015-03-01

    Full Text Available An efficient approach to reversed nucleosides which enables their synthesis in gram quantities is described. N-1′-Pyrimidine reversed nucleosides were prepared by treating of the sodium salt of pyrimidine bases with protected 5-tosyl ribose. Additionally, N-1′,N-3′-disubstituted reversed nucleosides were isolated in the condensation reactions with the 5-halogen pyrimidines. Using the Sonogashira coupling of 5′-iodouracil reversed nucleoside with ethynyltrimethyl silane gave 5′-ethynyl derivative which was further transformed into 5′-acetyl reversed nucleoside. Biological activity of deprotected reversed nucleosides was validated on the panel of six human carcinoma cell lines (HeLa, MIAPaCa2, Hep2, NCI-H358, CaCo-2, and HT-29. 5′-Iodouracil derivative displayed moderate growth inhibition activity against human colon carcinoma (CaCo-2 cells.

  6. Established and emerging biological activity markers of inflammatory bowel disease

    DEFF Research Database (Denmark)

    Nielsen, O H; Vainer, B; Madsen, S M

    2000-01-01

    orosomucoid and CRP), leukocyte and platelet counts, albumin, neopterin, and beta2-microglobulin will be reviewed together with emerging disease markers such as antibodies of the ANCA/ASCA type, cytokines (e.g., IL-1, IL-2Ralpha, IL-6, IL-8, TNF-alpha, and TNF-alpha receptors) and with various adhesion......Assessment of disease activity in inflammatory bowel disease (IBD), i.e., ulcerative colitis (UC) and Crohn's disease (CD), is done using clinical parameters and various biological disease markers. Ideally, a disease marker must: be able to identify individuals at risk of a given disorder......, be disease specific, mirror the disease activity and, finally, be easily applicable for routine clinical purposes. However, no such disease markers have yet been identified for IBD. In this article, classical disease markers including erythrocyte sedimentation rate, acute phase proteins (especially...

  7. Template Synthesis of Tubular Nanostructures for Loading Biologically Active Molecules.

    Science.gov (United States)

    Karatas, Aysegul; Algan, Aslıhan Hilal

    2017-01-01

    The template synthesis is a low cost, simple and versatile nanofabrication method to produce cylindrical/tubular nanostructures with controllable dimensions such as length, diameter and aspect ratio. This method utilizes nanoporous membranes such as anodized aluminum oxide (AAO) or polycarbonate (PC) as templates which have nanosized specific, cylindrical and uniform inner pores to be coated with the desired material. Template synthesized nanotubular structures have been produced from variety of materials including ceramics, polymers and proteins for loading biologically active molecules. Available procedures of material deposition into the template nanopores consist of several techniques like wetting (melt or solution wetting), layer-by-layer (LbL) assembly and sol-gel chemistry. Template synthesis enables not only control of the geometry of the resulting nanostructures but also provides nanovehicles having separated inner and outer surfaces which can be variously functionalized. Tubular nanostructures fabricated by this method have numerous potential applications including delivery of biologically active molecules such as drugs, gene, enzymes and proteins. In this review we aimed to present up-to-date works on the template based synthesis which has greatly facilitated the fabrication of polymer and protein tubular nanostructures, principally. The strategies regarding the synthesis and designing of these promising tubular nanostructures together with recent approaches relevant of drug delivery was also presented. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

  8. Design, synthesis and biological evaluation of lapachol derivatives possessing indole scaffolds as topoisomerase I inhibitors.

    Science.gov (United States)

    Zhang, Chong; Qu, Yan; Niu, Bingxuan

    2016-11-15

    A series of novel lapachol derivatives possessing indole scaffolds was designed and synthesized. The in vitro anti-proliferative activity of these novel compounds was evaluated in Eca109 and Hela cell lines. Almost all the tested compounds showed manifested potent inhibitory activity against the two tested cancer cell lines. Topo I-mediated DNA relaxation activity indicated that these novel compounds have potent Topoisomerase I inhibition activity. The most potent compounds 4n and 4k demonstrated more cytotoxicity than camptothecin and was comparable to camptothecin in inhibitory activities on Topoisomerase I in our biological assay. In addition, the Hoechst 33342 staining method also showed that the complex can induce Hela cell apoptosis. Copyright © 2016 Elsevier Ltd. All rights reserved.

  9. The in vitro biological activity of Lepidium meyenii extracts.

    Science.gov (United States)

    Valentová, K; Buckiová, D; Kren, V; Peknicová, J; Ulrichová, J; Simánek, V

    2006-03-01

    The biological activity of methanolic and aqueous extracts from dehydrated hypocotyls of Lepidium meyenii (Brassicaceae, vernacular name "maca"), was studied on rat hepatocytes and human breast cancer MCF-7 cells. The extracts did not exhibit cytotoxicity in hepatocyte primary cultures up to 10 mg/ml as measured by the MTT viability test, and lactate dehydrogenase (LDH) and aspartate aminotransferase (AST) leakage. Moreover, after 72 h, extracts inhibited LDH and AST leakage from the hepatocytes. When hepatocytes were intoxicated by t-butyl hydroperoxide, neither extract prevented oxidative damage. Both extracts showed weak antioxidant activity in the DPPH radical scavenging test with IC(50) values of 3.46 +/- 0.16 and 0.71 +/- 0.10 mg/ml, for aqueous and methanolic extracts, respectively. Thus, the observed effect on spontaneous enzyme leakage is probably mediated through mechanisms other than antioxidant activity. Both methanolic and aqueous extracts have shown estrogenic activity comparable with that of silymarin in MCF-7 cell line. Maca estrogenicity was exhibited in the range from 100 to 200 mug of extract per ml. The findings in the present study show that maca does not display in vitro hepatotoxicity. In contrast, a slight cytoprotective effect, probably not mediated by antioxidant capacity, was noted. Maca extracts exhibited estrogenic activity comparably to the effect of silymarin in MCF-7 cells.

  10. Characterization of chickpea (Cicer arietinum L.) lectin for biological activity.

    Science.gov (United States)

    Gautam, Ajay Kumar; Gupta, Neha; Narvekar, Dakshita T; Bhadkariya, Rajni; Bhagyawant, Sameer S

    2018-05-01

    Lectins are proteins that are subject of intense investigations. Information on lectin from chickpea ( Cicer arietinum L.) with respect to its biological activities are very limited. In this study, we purified lectin from the seeds of chickpea employing DEAE-cellulose and SP-Sephadex ion exchange chromatography and identified its molecular subunit mass as 35 kDa. The free radical scavenging activity of lectin measured by the DPPH assay has IC 50 of 0.88 µg/mL. Lectin exerted antifungal activity against Candida krusei , Fusarium oxysporium oxysporium , Saccharomyces cerevisiae and Candida albicans , while antibacterial activity against E. coli , B. subtilis , S. marcescens and P. aeruginosa. The minimum inhibitory concentrations were 200, 240, 160 and 140 µg for C. krusei, F. oxysporium , S. cerevisiae and C. albicans respectively. Lectin was further examined for its antiproliferative potential against cancerous cell line. The cell viability assay indicated a high inhibition activity on Ishikawa, HepG2, MCF-7 and MDA-MB-231 with IC 50 value of 46.67, 44.20, 53.58 and 37.46 µg/mL respectively. These results can provide a background for future research into the benefits of chickpea lectin to pharmacological perspective.

  11. Six coordination compounds: mode of cytotoxic action and biological evaluation

    Directory of Open Access Journals (Sweden)

    ali aydin

    2016-09-01

    Full Text Available This study describes the biological and anticancer properties of followed coordination compounds. IR spectra, magnetic properties, thermal analyses and crystal structures of six cyanido-complexes derivatives with [MII(CN4]2- (MII= Ni and Pd and [Co(CN6]3- anions and N-bishydeten (N,N-bis(2-hydroxyethylethylenediamine as a capping ligand have been previously reported. Here, we investigated these complexes denoted as[Ni(N-bishydetenNi(CN4] (C1, [Zn2(N-bishydeten2Ni(CN4] (C2, [Ni(N-bishydetenPd(CN4] (C3, [Cd(N-bishydeten2][Pd(CN4] (C4, [Ni2(N-bishydeten2Co(CN6].3H2O (C5 and K[Cd(N-bishydetenCo(CN6].1.5H2O (C6, which were tested for their anti-proliferative activity against human cervical cancer (HeLa, human colon cancer (HT29, rat glioma (C6 and African green monkey kidney (Vero cell lines. The DNA/BSA binding affinities of these compounds were also elucidated by spectroscopic titrations, displacement experiments and electrophoresis measurements. Studies on cancerous cells revealed that C1, C2, C4 and C6 exhibited significant antitumor activity and inhibited tumor progression in testing cell lines and showed high solubility in the solvent. Absorbance and emission spectra data results revealed that the complexes interact with the DNA via groove binding mode of interaction. Overall, these compounds have been found to demonstrate effective anti-proliferative activity against the cancer cell lines, indicating that they are a potent candidate for preclinical or clinical study.

  12. Bone Scan in Detection of Biological Activity in Nonhypertrophic Fracture Nonunion

    OpenAIRE

    Gandhi, Sunny J.; Rabadiya, Bhavdeep

    2017-01-01

    Biological activity of the fracture site is very important factor in treatment planning of fracture nonunion. If no biological activity is detected, then an autologous bone graft can be supplemented or osteogenic supplementations, such as bone morphogenetic protein is given. If biological activity is present, then secure fixation is sufficient to achieve bony union. Biological activity of nonunions is usually assessed by conventional radiographs. The presence of callus formation is usually as...

  13. Preparation and characterization of new biologically active polyurethane foams.

    Science.gov (United States)

    Savelyev, Yuri; Veselov, Vitali; Markovskaya, Ludmila; Savelyeva, Olga; Akhranovich, Elena; Galatenko, Natalya; Robota, Ludmila; Travinskaya, Tamara

    2014-12-01

    Biologically active polyurethane foams are the fast-developed alternative to many applications of biomedical materials. Due to the polyurethane structure features and foam technology it is possible to incorporate into their structure the biologically active compounds of target purpose via structural-chemical modification of macromolecule. A series of new biologically active polyurethane foams (PUFs) was synthesized with polyethers (MM 2500-5000), polyesters MM (500-2200), 2,4(2,6) toluene diisocyanate, water as a foaming agent, catalysts, foam stabilizers and functional compounds. Different functional compounds: 1,4-di-N-oxy-2,3-bis-(oxymethyl)-quinoxaline (DOMQ), partial sodium salt of poly(acrylic acid) and 2,6-dimethyl-N,N-diethyl aminoacetatanilide hydrochloride were incorporated into the polymer structure/composition due to the chemical and/or physical bonding. Structural peculiarities of PUFs were studied by FTIR spectroscopy and X-ray scattering. Self-adhesion properties of PUFs were estimated by measuring of tensile strength at break of adhesive junction. The optical microscopy method was performed for the PUF morphology studies. Toxicological estimation of the PUFs was carried out in vitro and in vivo. The antibacterial action towards the Gram-positive and Gram-negative bacteria (Escherichia coli ATC 25922, E. coli ATC 2150, Klebsiella pneumoniae 6447, Staphylococcus aureus 180, Pseudomonas aeruginosa 8180, Proteus mirabilis F 403, P. mirabilis 6054, and Proteus vulgaris 8718) was studied by the disc method on the solid nutrient. Physic-chemical properties of the PUFs (density, tensile strength and elongation at break, water absorption and vapor permeability) showed that all studied PUFs are within the operational requirements for such materials and represent fine-cellular foams. Spectral studies confirmed the incorporation of DOMQ into the PUF's macrochain. PUFs are characterized by microheterogeneous structure. They are antibacterially active, non

  14. The importance of extremophile cyanobacteria in the production of biologically active compounds

    Directory of Open Access Journals (Sweden)

    Drobac-Čik Aleksandra V.

    2007-01-01

    Full Text Available Due to their ability to endure extreme conditions, terrestrial cyanobacteria belong to a group of organisms known as "extremophiles". Research so far has shown that these organisms posses a great capacity for producing biologically active compounds (BAC. The antibacterial and antifungal activities of methanol extracts of 21 cyanobacterial strains belonging to Anabaena and Nostoc genera, previously isolated from different soil types and water resources in Serbia, were evaluated. In general, larger number of cyanobacterial strains showed antifungal activity. In contrast to Nostoc, Anabaena strains showed greater diversity of antibacterial activity (mean value of percentages of sensitive targeted bacterial strains 3% and 25.9% respectively. Larger number of targeted fungi was sensitive to cultural liquid extract (CL, while crude cell extract (CE affected more bacterial strains. According to this investigation, the higher biological activity of terrestrial strains as representatives of extremophiles may present them as significant BAC producers. This kind of investigation creates very general view of cyanobacterial possibility to produce biologically active compounds but it points out the necessity of exploring terrestrial cyanobacterial extremophiles as potentially excellent sources of these substances and reveals the most prospective strains for further investigations.

  15. Phenolic compounds and biological activity of Capsicum annuum L ...

    African Journals Online (AJOL)

    The objective of this study was to evaluate antifungal and antioxidant activities of vegetable extracts (Capsicum annuum L. cv. Dora, cv. Strizanka, cv. Morava), grown in Serbia. Different experimental models have included the determination content of total phenolics, total flavonoids, antioxidant capacity and minimum ...

  16. Biological activities of four essential oils against Anopheles gambiae ...

    African Journals Online (AJOL)

    The control of malaria is still a challenge partly due to mosquito's resistance to current available insecticides. The aim of this work was to evaluate the ovicidal, larvicidal and repellent activities of Lantana camara, Hyptis suaveolens, Hyptis spicigera and Ocimum canum essential oils against Anopheles gambiae s.l. ...

  17. Phytochemical profile and some biological activities of three ...

    African Journals Online (AJOL)

    Purpose: To characterise the phytochemical profile of whole plants of Centaurea balsamita, C. depressa and C. lycopifolia with LC-ESI-MS/MS, and as well as their antioxidant, anticholinesterase and antimicrobial activities. Methods: Organic and aqueous extracts of the three Centaurea species were evaluated for DPPH ...

  18. Biological activities and phytochemical constituents of the gray ...

    African Journals Online (AJOL)

    In vitro assessment of the antibacteriophage, antibacterial and anticandidal activities as well as cytotoxicity were evaluated for both aqueous and ethanol extracts prepared from roots, cotyledons, leaves and stems of Avicennia marina. Aqueous extracts of both shoots and roots of the seedlings demonstrated ...

  19. Evaluation of relative biological efficiency of additives in sugarcane ensiling

    Directory of Open Access Journals (Sweden)

    Laura Maria Oliveira Borgatti

    2012-04-01

    Full Text Available The objective of this study was to evaluate the effects of adding alkalis on the fermentative pattern, aerobic stability and nutritive value of the sugarcane silage. A completely randomized design with 6 additives in two concentrations (1 or 2%, plus a control group, totalizing 13 treatments [(6×2+1] with four replications, was used. The additives were sodium hydroxide (NaOH, limestone (CaCO3, urea (CO(NH22, sodium bicarbonate (NaHCO3, quicklime (CaO and hydrated lime (Ca(OH2. The material was ensiled in 52 laboratory silos using plastic buckets with 12 L of capacity. Silos were opened 60 days after ensiling, when organic acids concentration, aerobic stability and chemical composition were determined. The Relative Biological Efficiency (RBE was calculated by the slope ratio method, using the data obtained from ratio between desirable and undesirable silage products, according to the equation: D/U ratio = [lactic/(ethanol + acetic + butyric]. All additives affected dry matter, crude protein, acid detergent fiber, neutral detergent fiber contents and buffering capacity. Except for urea and quicklime, all additives increased the in vitro dry matter digestibility. In general, these additives altered the fermentative pattern of sugarcane silage, inhibiting alcoholic fermentation and improving lactic acid production. The additive that showed the best RBE in relation to sodium hydroxide (100% was limestone (89.4%. The RBE values of urea, sodium bicarbonate and hydrated lime were 49.2%, 47.7% and 34.3%, respectively.

  20. Phytochemical prospection and biological activity of Duroia macrophylla (Rubiaceae

    Directory of Open Access Journals (Sweden)

    Daiane Martins

    2014-12-01

    Full Text Available Context: Duroia macrophylla (Rubiaceae is endemic from the Amazon Rainforest. Aims: To perform phytochemical profile of Duroia macrophylla extracts and to evaluate them as antioxidant, insecticidal and cytotoxic. Methods: Dichloromethane and methanol extracts of leaves and branches (collected three times were subjected to phytochemical screening by comparative thin layer chromatography and NMR analyses. The extracts were assayed to antioxidant (DPPH and Fe-phenanthroline, at 10 μg/mL, insecticidal on Sitophilus zeamais (by ingestion of stored grains and contact, both at 10 mg/mL and toxic activities on Artemia salina (1000 μg/mL. Results: There were found evidences of terpenes, phenolic substances (phenols and flavonoids and alkaloids, with differences between the vegetal part, collection period and solvent used. Antioxidant evaluations showed three of twelve were active and two were considered moderately active, with a relationship dependently of concentration. All methanol extracts showed the presence of phenolic substances (phenols and flavonoids but one showed only phenols. For insecticidal activity, there were three most active extracts, two of which showed only presence of terpenes and the other, besides terpenes, phenolic substances (phenols and flavonoids. For Artemia salina toxicity assay, the five most active were all from the 2nd and 3rd collections. Conclusions: The active extracts of D. macrophylla in each test were different. Three methanol extracts showed antioxidant activity; three extracts showed insecticidal activity and the presence of terpenic substances and five extracts presented cytotoxic activity, but it was not possible to correlate it with any specific secondary metabolite.

  1. Biological activity of soil contaminated with cobalt, tin, and molybdenum.

    Science.gov (United States)

    Zaborowska, Magdalena; Kucharski, Jan; Wyszkowska, Jadwiga

    2016-07-01

    In this age of intensive industrialization and urbanization, mankind's highest concern should be to analyze the effect of all metals accumulating in the environment, both those considered toxic and trace elements. With this aim in mind, a unique study was conducted to determine the potentially negative impact of Sn(2+), Co(2+), and Mo(5+) in optimal and increased doses on soil biological properties. These metals were applied in the form of aqueous solutions of Sn(2+) (SnCl2 (.)2H2O), Co(2+) (CoCl2 · 6H2O), and Mo(5+) (MoCl5), each in the doses of 0, 25, 50, 100, 200, 400, and 800 mg kg(-1) soil DM. The activity of dehydrogenases, urease, acid phosphatase, alkaline phosphatase, arylsulfatase, and catalase and the counts of twelve microorganism groups were determined on the 25th and 50th day of experiment duration. Moreover, to present the studied problem comprehensively, changes in the biochemical activity and yield of spring barley were shown using soil and plant resistance indices-RS. The study shows that Sn(2+), Co(2+), and Mo(5+) disturb the state of soil homeostasis. Co(2+) and Mo(5+) proved the greatest soil biological activity inhibitors. The residence of these metals in soil, particularly Co(2+), also generated a drastic decrease in the value of spring barley resistance. Only Sn(2+) did not disrupt its yielding. The studied enzymes can be arranged as follows for their sensitivity to Sn(2+), Co(2+), Mo(5+): Deh > Ure > Aryl > Pal > Pac > Cat. Dehydrogenases and urease may be reliable soil health indicators.

  2. Catalytically and biologically active silver nanoparticles synthesized using essential oil

    Science.gov (United States)

    Vilas, Vidya; Philip, Daizy; Mathew, Joseph

    2014-11-01

    There are numerous reports on phytosynthesis of silver nanoparticles and various phytochemicals are involved in the reduction and stabilization. Pure explicit phytosynthetic protocol for catalytically and biologically active silver nanoparticles is of importance as it is an environmentally benign green method. This paper reports the use of essential oil of Myristica fragrans enriched in terpenes and phenyl propenes in the reduction and stabilization. FTIR spectra of the essential oil and the synthesized biogenic silver nanoparticles are in accordance with the GC-MS spectral analysis reports. Nanosilver is initially characterized by an intense SPR band around 420 nm, followed by XRD and TEM analysis revealing the formation of 12-26 nm sized, highly pure, crystalline silver nanoparticles. Excellent catalytic and bioactive potential of the silver nanoparticles is due to the surface modification. The chemocatalytic potential of nanosilver is exhibited by the rapid reduction of the organic pollutant, para nitro phenol and by the degradation of the thiazine dye, methylene blue. Significant antibacterial activity of the silver colloid against Gram positive, Staphylococcus aureus (inhibition zone - 12 mm) and Gram negative, Escherichia coli (inhibition zone - 14 mm) is demonstrated by Agar-well diffusion method. Strong antioxidant activity of the biogenic silver nanoparticles is depicted through NO scavenging, hydrogen peroxide scavenging, reducing power, DPPH and total antioxidant activity assays.

  3. Soil degradation effect on biological activity in Mediterranean calcareous soils

    Science.gov (United States)

    Roca-Pérez, L.; Alcover-Sáez, S.; Mormeneo, S.; Boluda, R.

    2009-04-01

    Soil degradation processes include erosion, organic matter decline, compaction, salinization, landslides, contamination, sealing and biodiversity decline. In the Mediterranean region the climatological and lithological conditions, together with relief on the landscape and anthropological activity are responsible for increasing desertification process. It is therefore considered to be extreme importance to be able to measure soil degradation quantitatively. We studied soil characteristics, microbiological and biochemical parameters in different calcareous soil sequences from Valencia Community (Easter Spain), in an attempt to assess the suitability of the parameters measured to reflect the state of soil degradation and the possibility of using the parameters to assess microbiological decline and soil quality. For this purpose, forest, scrubland and agricultural soil in three soil sequences were sampled in different areas. Several sensors of the soil biochemistry and microbiology related with total organic carbon, microbial biomass carbon, soil respiration, microorganism number and enzyme activities were determined. The results show that, except microorganism number, these parameters are good indicators of a soil biological activity and soil quality. The best enzymatic activities to use like indicators were phosphatases, esterases, amino-peptidases. Thus, the enzymes test can be used as indicators of soil degradation when this degradation is related with organic matter losses. There was a statistically significant difference in cumulative O2 uptake and extracellular enzymes among the soils with different degree of degradation. We would like to thank Spanish government-MICINN for funding and support (MICINN, project CGL2006-09776).

  4. Evaluation of biological attributes of soil type latossol under agroecological production

    Directory of Open Access Journals (Sweden)

    Marisol Rivero Herrada

    2016-10-01

    Full Text Available Biological soil attributes have shown to be good indicators of soil changes as a result of the management function. The aim of this study was to evaluate the effect of using cover crops, as well as planting and tillage systems on the biological attributes of a yellowish red latosol soil. Soil samples were taken at 0 to 0.10 m depth, seven days before the bean harvest. Microbial biomass carbon and nitrogen, basal soil respiration, metabolic ratio and total enzyme activity were evaluated in this study. The best agroecological management was achieved under the association of the ground cover with millet and in direct seeding because they showed higher soil microbial biomass carbon and nitrogen content and lower metabolic quotient, being pork bean the best plant coverage. All biological soil attributes were sensitive to the tillage system, which showed the best results of the total enzyme activity and of the soil metabolic quotient which resulted to be the most efficient.

  5. Synthesis and biological evaluation of chalcone derivatives (mini review).

    Science.gov (United States)

    Bukhari, Syed Nasir Abbas; Jasamai, Malina; Jantan, Ibrahim

    2012-11-01

    Chalcones are the principal precursors for the biosynthesis of flavonoids and isoflavonoids. A three carbon α, β-unsaturated carbonyl system constitutes chalcones. Chalcones are the condensation products of aromatic aldehyde with acetophenones in attendance of catalyst. They go through an assortment of chemical reactions and are found advantageous in synthesis of pyrazoline, isoxazole and a variety of heterocyclic compounds. In synthesizing a range of therapeutic compounds, chalcones impart key role. They have showed worth mentioning therapeutic efficacy for the treatment of various diseases. Chalcone based derivatives have gained heed since they own simple structures, and diverse pharmacological actions. A lot of methods and schemes have been reported for the synthesis of these compounds. Amongst all, Aldol condensation and Claisen-Schmidt condensation still grasp high up position. Other distinguished techniques include Suzuki reaction, Witting reaction, Friedel-Crafts acylation with cinnamoyl chloride, Photo-Fries rearrangement of phenyl cinnamates etc. These inventive techniques utilize various catalysts and reagents including SOCl(2) natural phosphate, lithium nitrate, amino grafted zeolites, zinc oxide, water, Na(2)CO(3), PEG400, silicasulfuric acid, ZrCl(4) and ionic liquid etc. The development of better techniques for the synthesis of α, β- unsaturated carbonyl compounds is still in high demand. In brief, we have explained the methods and catalysts used in the synthesis of chalcones along with their biological activities in a review form to provide information for the development of new-fangled processes targeting better yield, less reaction time and least side effects with utmost pharmacological properties.

  6. Biological activity of interferon betas in patients with multiple sclerosis is affected by treatment regimen and neutralising antibodies.

    Science.gov (United States)

    Bertolotto, A; Sala, A; Malucchi, S; Marnetto, F; Caldano, M; Di Sapio, A; Capobianco, M; Gilli, F

    2004-09-01

    MxA gene expression is one of the most appropriate markers of biological activity of exogenous interferon (IFN) beta. We quantified MxA mRNA for five consecutive days in 62 patients treated with IFN beta (16, Avonex; 10, Betaferon; 24, Rebif 22; 12, Rebif 44), by quantitative-competitive polymerase chain reaction. Every three months, IFN beta induced neutralising antibodies (NAbs) were evaluated in sera using a cytopathic effect assay. Two categories of patients were identified: one group (49/62) had a sharp post-injection increase in MxA expression (defined as "IFN beta biological responder"), whereas the other group (13/62) had no MxA induction after IFN beta administrations (defined as "IFN beta biological non-responder"). In 11/13 biological non-responders, the persistent presence of NAbs correlated with abolished biological activity, independently of treatment regimen. The two remaining IFN beta biological non-responders were NAb-. Among the 49 IFN beta biological responders, biological activity was comparable between the four preparations on day 2 and 3 (+12 and +36 hours post-injection), but it was greater in Betaferon and both Rebif preparations on day 1, 4, and 5. In biological responders treated three times a week, only 82% (59/72) of injections were considered effective, compared with 100% (13/13) of Avonex injections. Our results suggest that an optimal IFN beta regimen is not yet available: Avonex, given once a week, shows lower cumulative biological activity. On the other hand, both Betaferon and Rebif, given three times a week, show 18% biologically ineffective injections and higher risk of developing NAbs, which abolish biological activity.

  7. BIOLOGICALLY ACTIVE SUBSTANCES OF THE LAURUS NOBILIS LEAVES

    Directory of Open Access Journals (Sweden)

    N. M. Nasukhova

    2017-01-01

    Full Text Available Laurus nobilis L. is an evergreen dioecious, rarely monecious plant up to 12-15 m high. The plant’s name is devoted to an Ancient Greek God of Sun Apollo and is a symbol of peace and victory. It was used in making up wreaths for emperors, generals, and poets. Its natural area includes Mediterranean countries with high level of annual precipitation. It is actively cultivated as a decorative plant in Europe, Russia, USA and other countries. It is cultivated in Turkey, Algeria, Morocco, Portugal, Spain, Italy, France, Russia, and Mexico. The aim of the study is the review of available literature about isolation, identification, quantitative determination of biologically active compounds of the Laurus nobilis leaves in the established species and their pharmacological activity. Materialsand methods. The study was carried out using searching (PubMed, CiteSeer, arXiv, library databases (eLibrary, Cyberleninka, and ResearchGate free social network. Results and discussion. We have established that Laurus nobilis leaves have components of essential oil, phenolic compounds, and sesquiterpenic lactones as the principal active substances. Qualitative composition and quantitative content of these compound groups in these raw materials varies depending on the ecological and geographical, edaphic, climatic factors, phase of the plant growth, cultivation technology, drying method etc. The results of the pharmacological studies of the extracts, summary fractions, and individual compounds of Laurus nobilis leaves characterize this type of raw materials as a perspective source for a more profound study. Conclusion. As the available open review data showed, the essential oil components, phenolic compounds (phenolic acids, flavonoids, etc, sesquiterpenic lactones of Laurus nobilis exhibit a diverse spectrum of pharmacological activity. Antimicrobial (widely, anti-virus, anti-inflammatory, anti-diabetic, and cytoxic (anticancer activities, established in extracts

  8. Laser Polarimeter for Measurement of Optical Activity of Biological Objects

    Science.gov (United States)

    Protasov, E. A.; Protasov, D. E.; Ryzhkova, A. V.

    In this paper has been described the polarimetric device for measurement of optical activity of biological tissues, where the source of radiation is an infrared laser with a wave λ=0.808 micron. The polarizers used are polarizing prisms of Glan - Taylor. To obtain required angular resolution (0.180/cm) has been developed a device that converts the angle of rotation of the analyzer into electrical signal, which is fed to the appropriate scan digital oscilloscope. The passage of the polarized light through the fingers of the hand was established and the angles of rotation of the polarization vector of the transmitted radiation were measured, the values of which may be determined by the content of hemoglobin in the blood.

  9. Relationships between the stereochemistry and biological activity of fungal phytotoxins.

    Science.gov (United States)

    Evidente, Antonio; Andolfi, Anna; Cimmino, Alessio

    2011-10-01

    Toxins produced by phytopathogenic fungi assume great importance because of their involvement in several plant diseases. Although such pathogens are known to have seriously damaged crops, forest, and environmental resources, they represent a very important tool to develop new environmentally friendly herbicides and fungicides. This review deals with the relationships between the biological activity of some phytotoxins produced by pathogenic fungi for major forest plants and for damaging weeds and their stereochemistry. In particular, the methods used to determine their relative and/or absolute configuration will be illustrated. These include the application of Mosher's and Murata's methods, X-ray diffractometric analysis, circular dichroism, and the use of computational methods to determine the theoretical optical rotatory power as well as the CD spectrum. The importance of determining the absolute configuration to achieve the total synthesis of some phytotoxins, interesting for their potential practical application, is also discussed. © 2011 Wiley-Liss, Inc.

  10. Radiation degradation of polysaccharides and induced biological activity

    Energy Technology Data Exchange (ETDEWEB)

    Nagasawa, Naotsugu; Yoshii, Fumio; Makuuchi Keizo; Kume Tamikazu [Japan Atomic Energy Research Inst., Takasaki, Gunma (Japan). Takasaki Radiation Chemistry Research Establishment; Mitomo, Hiroshi [Gunma Univ., Kiryu (Japan). Faculty of Engineering

    1999-09-01

    Relationship between irradiation effect of polysaccharides and induced biological activity for plants has been investigated. Sodium alginate was irradiated by gamma-rays from a Co-60 source in liquid state (aqueous solution) and in solid state (powder form). Measurement of molecular weight and analysis of UV spectra of irradiated sodium alginate have been carried out. The molecular weight was decreased by irradiation in both conditions. New absorbance peak derived from double bond or/and carbonyl group was appeared at close to 267 nm by irradiation in UV spectra. It was found that alginate having molecular weight about 10,000 is most suitable to used as growth promoter in plants. To obtain the molecular weight of 10,000 by irradiation, the necessary doses are 100 kGy in liquid state and 500 kGy in solid state, respectively. (author)

  11. Production and biological activities of yellow pigments from Monascus fungi.

    Science.gov (United States)

    Chen, Gong; Wu, Zhenqiang

    2016-08-01

    Monascus yellow pigments (MYPs), are azaphilone compounds and one of the three main components of total Monascus pigments (MPs). Thirty-five hydrophilic or hydrophobic MYPs have been identified, with the majority being hydrophobic. Apart from screening special Monascus strains, some advanced approaches, such as extractive and high-cell-density fermentations, have been applied for developing or producing new MYPs, especially extracellular hydrophilic MYPs. The outstanding performance of MYPs in terms of resistance to photodegradation, as well as tolerance for temperature and pH, give natural MYPs reasonable prospects, compared with the orange and red MPs, for practical use in the present and future. Meanwhile, MYPs have shown promising potential for applications in the food and pharmaceutical industries based on their described bioactivities. This review briefly summarizes the reports to date on chemical structures, biological activities, biosynthetic pathways, production technologies, and physicochemical performances of MYPs. The existing problems for MYPs are discussed and research prospects proposed.

  12. Neutron activation analysis on determination of arsenic in biological matrixes

    International Nuclear Information System (INIS)

    Menezes, Maria Angela de B.C.; Silva, Maria Aparecida

    2013-01-01

    Aiming at giving support to the Worker's Health Awareness Program of the Municipal Department of Health of Belo Horizonte, an assessment related arsenic was carried out in two galvanising factories by means of hair and toenail samples analysis as biomonitors. The arsenic was determined in all matrixes from the factories where gold electrodeposition process was applied. This is because arsenic salts are usually added to gold bath to improve the metal covering. The high concentration results surprised the health surveillance professionals, and alerted for the need of assessing the influence of a long-term exposure. Studies concerning galvanising process have usually been developed broaching many aspects, but so far few works has pointed out the detection and measurement of other elements like arsenic. The k 0 -Instrumental Neutron Activation method was applied confirming to be a suitable technique on determination of arsenic in biological matrixes. (author)

  13. Structure and Biological Activity of Pathogen-like Synthetic Nanomedicines

    Science.gov (United States)

    Lőrincz, Orsolya; Tőke, Enikő R.; Somogyi, Eszter; Horkay, Ferenc; Chandran, Preethi; Douglas, Jack F.; Szebeni, János; Lisziewicz, Julianna

    2011-01-01

    Here we characterize the structure, stability and intracellular mode-of-action of DermaVir nanomedicine that is under clinical development for the treatment of HIV/AIDS. This nanomedicine is comprised of pathogen-like pDNA/PEIm nanoparticles (NPs) having the structure and function resembling spherical viruses that naturally evolved to deliver nucleic acids to the cells. Atomic force microscopy demonstrated spherical 100–200nm NPs with a smooth polymer surface protecting the pDNA in the core. Optical-absorption determined both the NP structural stability and biological activity relevant to their ability to escape from the endosome and release the pDNA at the nucleus. Salt, pH and temperature influence the nanomedicine shelf-life and intracellular stability. This approach facilitates the development of diverse polyplex nanomedicines where the delivered pDNA-expressed antigens induce immune responses to kill infected cells. PMID:21839051

  14. [The release of biologically active compounds from peat peloids].

    Science.gov (United States)

    Babaskin, D V

    2011-01-01

    This work had the objective to study kinetics of the release of flavonoides from peat peloid compositions containing extracts of medicinal herbs in model systems.The key parameters of the process are defined. The rate of liberation of flavonoides is shown to depend on their initial concentration in the compositions being used. The influence of the flavonoide composition of the tested extracts and dimethylsulfoxide on the release of biologically active compounds contained in the starting material in the model environment is estimated. The possibility of the layer-by-layer deposition of the compositions and peat peloids in order to increase the efficacy of flavonoide release from the starting composition and to ensure more rational utilization of the extracts of medicinal plants is demonstrated.

  15. Certification of biological candidates reference materials by neutron activation analysis

    Science.gov (United States)

    Kabanov, Denis V.; Nesterova, Yulia V.; Merkulov, Viktor G.

    2018-03-01

    The paper gives the results of interlaboratory certification of new biological candidate reference materials by neutron activation analysis recommended by the Institute of Nuclear Chemistry and Technology (Warsaw, Poland). The correctness and accuracy of the applied method was statistically estimated for the determination of trace elements in candidate reference materials. The procedure of irradiation in the reactor thermal fuel assembly without formation of fast neutrons was carried out. It excluded formation of interfering isotopes leading to false results. The concentration of more than 20 elements (e.g., Ba, Br, Ca, Co, Ce, Cr, Cs, Eu, Fe, Hf, La, Lu, Rb, Sb, Sc, Ta, Th, Tb, Yb, U, Zn) in candidate references of tobacco leaves and bottom sediment compared to certified reference materials were determined. It was shown that the average error of the applied method did not exceed 10%.

  16. Biological Activities of Libidibia (Caesalpinia) ferrea var. parvifolia (Mart. ex Tul.) L. P. Queiroz Pod Preparations

    OpenAIRE

    Freitas, A. C. C.; Ximenes, N. C. A.; Aguiar, J. S.; Nascimento, S. C.; Lins, T. U. L.; Magalhães, L. R.; Coelho, L. C. B. B.; Carneiro-da-Cunha, M. G.; Gonçalves-Silva, T.; Correia, M. T. S.

    2012-01-01

    Libidibia ferrea has been used in folk medicine throughout Brazil, and this study evaluated the biological activities of crude extract (CE) as well as a partially purified fraction (F80) obtained from its pods. Results from the MTT assay revealed that only F80 inhibited NCI-H292 cell growth; however, neither CE nor F80 reduced HEp-2 cell growth or sarcoma 180 tumor weight with the in vivo assay. Acute oral toxicity of the extract and fraction was evaluated following the steps of Guideline 423...

  17. Biological activities of undescribed North American lichen species.

    Science.gov (United States)

    Yeash, Erik A; Letwin, Lyndon; Malek, Lada; Suntres, Zacharias; Knudsen, Kerry; Christopher, Lew P

    2017-11-01

    Lichens provide a large array of compounds with the potential for pharmaceutical development. In the present study, extracts from three previously undescribed North American lichen species were examined for antioxidant, antibacterial and anticancer activities. The results from this study demonstrated the following: (i) Acarospora socialis ethanol extract exhibited significant DPPH antioxidant scavenging activities, which were concentration dependent; (ii) acetone and ethyl acetate extracts of Xanthoparmelia mexicana inhibited Gram-positive bacteria but had no effect on Gram-negative bacteria; X. mexicana acetone extract yielded a minimum inhibitory concentration (MIC) of 20.9 µg mL -1 against Staphylococcus aureus, and 41.9 µg mL -1 against Enterococcus faecalis; (iii) acetone extract of Lobothallia alphoplaca inhibited growth of cultured breast cancer MCF-7 cells with an effective concentration (EC 50 ) of 87 µg mL -1 ; the MCF-7 cell cycle appears arrested in the G2 phase, whereas the DNA synthesis cell cycle (S) may be inhibited. New lichen species that possess strong biological activities have been identified. These lichens comprise secondary metabolites that possess antioxidant, antibacterial and anticancer properties. © 2017 Society of Chemical Industry. © 2017 Society of Chemical Industry.

  18. Synthesis, characterization and biological evaluation of some newer carbazole derivatives

    Directory of Open Access Journals (Sweden)

    Sharma Divyanshu

    2014-01-01

    Full Text Available A series of novel 5-((9H-carbazol-9-ylmethyl-N-((substituted phenyl(piperazin-1-ylmethyl-1,3,4-oxadiazol-2-amine (4a-4o derivatives was synthesized by starting with carbazole which on reaction with ethyl choloroacetate yielded ethyl 2-(9H-carbazole-9-ylacetate (1, compound (1 on reaction with semicarbazide followed by cyclisation with sulphuric acid gave 5-((9H-carbazole-9-yl-1,3,4-oxadiazol-2-amine (3 which through Mannich reaction with piperazine and a variety of aromatic aldehydes in the presence of acetic acid yielded the titled compounds (4a-4o. The structures of compounds were characterized by UV, FT-IR, 1H-NMR, MS spectral studies and elemental analysis. All the derivatives were evaluated for their antibacterial, antifungal and anticancer activities. Among the tested compounds 4a, 4d, 4e and 4n exhibited significant antibacterial and antifungal activity while the compounds 4a, 4d, 4k and 4n were found to be active on Human Breast Cancer Cell Line i.e. MCF7.

  19. Phytochemical Analysis and Biological Activities of Cola nitida Bark

    Directory of Open Access Journals (Sweden)

    Durand Dah-Nouvlessounon

    2015-01-01

    Full Text Available Kola nut is chewed in many West African cultures and is used ceremonially. The aim of this study is to investigate some biological effects of Cola nitida’s bark after phytochemical screening. The bark was collected, dried, and then powdered for the phytochemical screening and extractions. Ethanol and ethyl acetate extracts of C. nitida were used in this study. The antibacterial activity was tested on ten reference strains and 28 meat isolated Staphylococcus strains by disc diffusion method. The antifungal activity of three fungal strains was determined on the Potato-Dextrose Agar medium mixed with the appropriate extract. The antioxidant activity was determined by DPPH and ABTS methods. Our data revealed the presence of various potent phytochemicals. For the reference and meat isolated strains, the inhibitory diameter zone was from 17.5±0.7 mm (C. albicans to 9.5±0.7 mm (P. vulgaris. The MIC ranged from 0.312 mg/mL to 5.000 mg/mL and the MBC from 0.625 mg/mL to >20 mg/mL. The highest antifungal activity was observed with F. verticillioides and the lowest one with P. citrinum. The two extracts have an excellent reducing free radical activity. The killing effect of A. salina larvae was perceptible at 1.04 mg/mL. The purified extracts of Cola nitida’s bark can be used to hold meat products and also like phytomedicine.

  20. Biological activities of Suaeda heterophylla and Bergenia stracheyi

    Directory of Open Access Journals (Sweden)

    Iftikhar Ali

    2014-09-01

    Full Text Available Objective: To evaluate the antioxidant, phytotoxic, antimicrobial, insecticidal, cytotoxic, antiglycative, and xanthine oxidase activities of different extracts of Suaeda heterophylla (S. heterophylla and Bergenia stracheyi (B. stracheyi. Methods: The extracts of S. heterophylla and B. stracheyi were evaluated for antioxidant, phytotoxic, antimicrobial, insecticidal, cytotoxic, antiglycative, and xanthine oxidase activities using standard experimental methods. Results: The overall antioxidant potential of ethyl acetate extract of S. heterophylla was the strongest, followed by chloroform extract, methanolic extract and n-hexane extract. It is interesting to note that ethyl acetate fraction showed 94.98% inhibition at concentration of 60 µg/mL while standard ascorbic acid showed 98.49% inhibition at same concentration. The crude methanol extracts of S. heterophylla and B. stracheyi showed significant phytotoxic activity at the highest dose. Moreover, methanol extract of B. stracheyi possessed strong activity in xanthine oxidase enzyme inhibition. Conclusions: Antioxidant, phytotoxic, and xanthine oxidase activities of different fractions of S. heterophylla and B. stracheyi clearly demonstrate that these fractions possess great potential for the food, cosmetic and pharmaceutical industries.

  1. Preliminary Phytochemical and Biological activities on Russelia juncea Zucc

    Directory of Open Access Journals (Sweden)

    Maryam Bibi

    2017-12-01

    Full Text Available To probe the ethnomedicinal claims of Russelia juncea Zucc. (Plantaginaceae as prescribed traditionally in the folklore history of medicines. Methods: The dichloromethane and methanol extracts of aerial parts and roots were examined for antimicrobial, antioxidant, antiglycation, insecticidal, leishmanicidal, cytotoxic and phytotoxic activities. Different phytochemical tests were also performed to confirm the presence of various groups of secondary metabolites such as alkaloids, glycosides, saponins, tannins, flavonoids and terpenoids. Results: Phytochemical screening of this plant confirmed the presence of alkaloids, saponins, tannins, flavonoids and terpenoids. Antibacterial activity was only shown by RJRD with 80% inhibition at the concentration of 150µg/ml against Shigella flexneri. Among the tested samples, RJAM and RJRM displayed significant radical scavenging activity up to 93% and 89% with IC50 values of 184.75 ± 4.05µM and 263.01 ± 9.36µM. The significant antiglycation potential was exhibited by RJAD, RJAM and RJRM with 55.35%, 62.25% and 59.22% inhibition and IC50 values of 0.84 ± 0.08mg/ml, 1.37 ± 0.15mg/ml and 1.52 ± 0.10mg/ml respectively. Moderate leishmanicidal activity was exposed by RJAD and RJRM with IC50 values of 73.04 ± 1.05µg/ml and 77.66 ± 0.23µg/ml while RJAM was found to be more potent and exposed significant leishmanicidal activity having IC50 of 48 ± 0.39µg/ml. However, prominent cytotoxic activity was displayed by RJRM with 66.08% inhibition and IC50 of 31.20 ± 3µg/ml. Non-significant antifungal, insecticidal and phytotoxic activities were demonstrated by all the tested samples. Conclusion: All the above contributions give serious attentiveness to scientists to isolate and purify the biologically active phytoconstituents by using advanced scientific methodologies that serve as lead compounds in the synthesis of new therapeutic agents of desired interest in the world of drug discovery.

  2. Role of Muramyl Dipeptide in Lipopolysaccharide-Mediated Biological Activity and Osteoclast Activity

    Directory of Open Access Journals (Sweden)

    Hideki Kitaura

    2018-01-01

    Full Text Available Lipopolysaccharide (LPS is an endotoxin and bacterial cell wall component that is capable of inducing inflammation and immunological activity. Muramyl dipeptide (MDP, the minimal essential structural unit responsible for the immunological activity of peptidoglycans, is another inflammation-inducing molecule that is ubiquitously expressed by bacteria. Several studies have shown that inflammation-related biological activities were synergistically induced by interactions between LPS and MDP. MDP synergistically enhances production of proinflammatory cytokines that are induced by LPS exposure. Injection of MDP induces lethal shock in mice challenged with LPS. LPS also induces osteoclast formation and pathological bone resorption; MDP enhances LPS induction of both processes. Furthermore, MDP enhances the LPS-induced receptor activator of NF-κB ligand (RANKL expression and toll-like receptor 4 (TLR4 expression both in vivo and in vitro. Additionally, MDP enhances LPS-induced mitogen-activated protein kinase (MAPK signaling in stromal cells. Taken together, these findings suggest that MDP plays an important role in LPS-induced biological activities. This review discusses the role of MDP in LPS-mediated biological activities, primarily in relation to osteoclastogenesis.

  3. Biological activity of a genetically modified BMP-2 variant with inhibitory activity

    Directory of Open Access Journals (Sweden)

    Kübler Alexander C

    2009-02-01

    Full Text Available Abstract Background Alterations of the binding epitopes of bone morphogenetic protein-2 (BMP-2 lead to a modified interaction with the ectodomains of BMP receptors. In the present study the biological effect of a BMP-2 double mutant with antagonistic activity was evaluated in vivo. Methods Equine-derived collagenous carriers were loaded with recombinant human BMP-2 (rhBMP-2 in a well-known dose to provide an osteoinductive stimulus. The study was performed in a split animal design: carriers only coupled with rhBMP-2 (control were implanted into prepared cavities of lower limb muscle of rats, specimens coupled with rhBMP-2 as well as BMP-2 double mutant were placed into the opposite limb in the same way. After 28 days the carriers were explanted, measured radiographically and characterized histologically. Results As expected, the BMP-2 loaded implants showed a typical heterotopic bone formation. The specimens coupled with both proteins showed a significant decreased bone formation in a dose dependent manner. Conclusion The antagonistic effect of a specific BMP-2 double mutant could be demonstrated in vivo. The dose dependent influence on heterotopic bone formation by preventing rhBMP-2 induced osteoinduction suggests a competitive receptor antagonism.

  4. Biological ensemble modeling to evaluate potential futures of living marine resources

    DEFF Research Database (Denmark)

    Gårdmark, Anna; Lindegren, Martin; Neuenfeldt, Stefan

    2013-01-01

    in all models, intense fishing prevented recovery, and climate change further decreased the cod population. Our study demonstrates how the biological ensemble modeling approach makes it possible to evaluate the relative importance of different sources of uncertainty in future species responses, as well......Natural resource management requires approaches to understand and handle sources of uncertainty in future responses of complex systems to human activities. Here we present one such approach, the “biological ensemble modeling approach,” using the Eastern Baltic cod (Gadus morhua callarias......) as an example. The core of the approach is to expose an ensemble of models with different ecological assumptions to climate forcing, using multiple realizations of each climate scenario. We simulated the long-term response of cod to future fishing and climate change in seven ecological models ranging from...

  5. Societal Risk Evaluation Scheme (SRES: Scenario-Based Multi-Criteria Evaluation of Synthetic Biology Applications.

    Directory of Open Access Journals (Sweden)

    Christopher L Cummings

    Full Text Available Synthetic biology (SB applies engineering principles to biology for the construction of novel biological systems designed for useful purposes. From an oversight perspective, SB products come with significant uncertainty. Yet there is a need to anticipate and prepare for SB applications before deployment. This study develops a Societal Risk Evaluation Scheme (SRES in order to advance methods for anticipatory governance of emerging technologies such as SB. The SRES is based upon societal risk factors that were identified as important through a policy Delphi study. These factors range from those associated with traditional risk assessment, such as health and environmental consequences, to broader features of risk such as those associated with reversibility, manageability, anticipated levels of public concern, and uncertainty. A multi-disciplinary panel with diverse perspectives and affiliations assessed four case studies of SB using the SRES. Rankings of the SRES components are compared within and across the case studies. From these comparisons, we found levels of controllability and familiarity associated with the cases to be important for overall SRES rankings. From a theoretical standpoint, this study illustrates the applicability of the psychometric paradigm to evaluating SB cases. In addition, our paper describes how the SRES can be incorporated into anticipatory governance models as a screening tool to prioritize research, information collection, and dialogue in the face of the limited capacity of governance systems. To our knowledge, this is the first study to elicit data on specific cases of SB with the goal of developing theory and tools for risk governance.

  6. Biological activities and phenolic contents of Argania spinosa L ...

    African Journals Online (AJOL)

    Cytotoxic activity was evaluated by methyl-thiazolyldiphenyl-tetrazolium bromide (MTT) assay. Results: The results revealed abundant polyphenols and flavonoids (221.39 ± 5.70 μg GAEq/1 g and 66.86 ± 3.36 μg CAEq/1 g, respectively) in the leaf extract. UPLC-DAD-ESI-QTOF-MS profiling showed the presence of ...

  7. Solid-phase synthesis and biological evaluation of Joro spider toxin-4 from Nephila clavata

    DEFF Research Database (Denmark)

    Barslund, Anne Fuglsang; Poulsen, Mette Homann; Bach, Tinna Brøbech

    2011-01-01

    to be exploited in biological studies. Here, we have used solid-phase synthetic methodology for the efficient synthesis of Joro spider toxin-4 (JSTX-4) (1) from Nephila clavata, providing sufficient amounts of the toxin for biological evaluation at iGlu receptor subtypes using electrophysiology. Biological...

  8. Phytochemical and biological evaluation of Buddleja polystachya growing in Saudi Arabia.

    Science.gov (United States)

    Al Ati, Hanan Yehya; Fawzy, Ghada Ahmed; El Gamal, Ali Ali; Khalil, Ashraf Taha; El Din El Tahir, Kamal; Abdel-Kader, Maged Saad; Gilani, Anwarul-Hassan

    2015-07-01

    Several Buddleja species were the target of phytochemical and biological studies; however, nothing was reported concerning the chemistry of Buddleja polystachya Fresen. growing in Saudi Arabia. Sixteen constituents were isolated from the aerial parts of B. polystachya using various chromatographic techniques and were identified by the help of different spectral techniques including 1D, 2D NMR and mass spectrometry. Moreover, the different fractions were evaluated for their anti-inflammatory and hypoglycemic activities. The isobenzofuranone derivative (4-hydroxy-7-methylisobenzofuranone) (4), has been isolated for the first time from this natural source, B. polystachya, along with fifteen known compounds namely; phenolic fatty acid ester, 1'(4-hydroxyphenyl) ethanol ester of docosanoic (1), uvaol (2), sakuranetin (3), kumatakenin (5), cirsimaritin (6), 5-hydroxy-3,7,4'-trimethoxyflavone (7), oleanolic acid (8), herbacetin 3,7,8-trimethyl ether (9), ursolic acid (10), verbascoside (11), linarin (12), luteolin 7-O-β-D-glucoside (13), luteolin 7-(6"-caffeoyl)-O-β-D-glucopyranoside (14), luteolin (15), and 6-O-α-L-(4''-O-trans-cinnamoyl) rhamnopyranosylcatalpol (16). Regarding the biological activities investigated, the ethyl acetate fraction showed the most significant anti-inflammatory activity, followed by the n-butanol and the aqueous fractions. As for the petroleum ether and dichloromethane fractions, their anti-inflammatory effects were moderate. The highest hypoglycemic activity was possessed by the ethyl acetate fraction, followed by the dichloromethane fraction and the n-butanol fraction showed the weakest activity.

  9. Synthesis of New Indole Derivatives Structurally Related to Donepezil and Their Biological Evaluation as Acetylcholinesterase Inhibitors

    Directory of Open Access Journals (Sweden)

    Samar I. Faggal

    2012-04-01

    Full Text Available New series of indole derivatives analogous to donepezil, a well known anti-Alzheimer and acetylcholinesterase inhibitor drug, was synthesized. A full chemical characterization of the new compounds is provided. Biological evaluation of the new compounds as acetylcholinesterase inhibitors was performed. Most of the compounds were found to have potent acetylcholinesterase inhibitor activity compared to donepezil as standard. The compound 1-(2-(4-(2-fluorobenzyl piperazin-1-ylacetylindoline-2,3-dione (IIId was found to be the most potent.

  10. Preparation and biological evaluation of novel acylhydrazide derivatives of 2,3-dichloronaphthoquinone

    Directory of Open Access Journals (Sweden)

    Jomana Elaridi

    2017-04-01

    Full Text Available Naphthoquinones have been reported to possess a variety of pharmacological properties including antibacterial, antifungal, antiviral, anti-inflammatory, anti-artherosclerotic and anticancer effects. We have successfully synthesized a series of novel naphthoquinone acylhydrazides. The straightforward synthesis of these molecules involves a coupling reaction between 2,3-dichloro-1,4-naphthoquinone and several alkyl and aromatic hydrazides and the hydrazides of the pyrimidine nucleobases, uracil and thymine. The product hydrazides were isolated in good yields and completely characterized by spectroscopic analysis. Biological evaluation against human colon cancer HCT116 cells and human breast cancer MCF-7 cells indicated that the novel hydrazides possessed significant anticancer activity.

  11. Students' Evaluation of Classroom Interactions of Their Biology ...

    African Journals Online (AJOL)

    ' classroom interaction and their feelings towards biology lessons. Three research questions guided the study. Copies of a questionnaire containing 48 items were distributed to 1,216 senior secondary two students from nine randomly selected ...

  12. [Composition and content of biologically active substances in rose hips].

    Science.gov (United States)

    Dubtsova, G N; Negmatulloeva, R N; Bessonov, V V; Baĭkov, V G; Sheviakova, L V; Makhova, N N; Perederiaev, O I; Bogachuk, M N; Baĭgarin, E K

    2012-01-01

    The paper studies the chemical composition of the powders obtained from the pulp with the skins and seeds of fruits of wild rose hips. Research results have shown that the main fraction of the powder is dietary fiber, powder of seeds of insoluble fiber in 1,6 and 2,3 higher than in the powder of the fruit with a thin skin and pulp, respectively. The greatest amount of carbohydrates and protein found in powders and pulp of the fruit with a thin skin, and lipids predominate in the powder from the seeds. Found that the lipid powder rosehip richest in oleic, linoleic and linolenic acids, the share of oleic acid has 6,4-19,2%, linoleic and linolenic 19,7-45,8 and 23,3-33,9% of the amount of fatty acids. Lipids powders of hips and seeds of rose have higher levels of essential linoleic acid and powder from the pulp with the skins - linolenic acid. In the study established the presence of sterols 7 fractions, the predominant of which is the beta-sitosterol. In the powder from the pulp with the skins found the greatest amount of ascorbic acid, carotenoids, and the powder of seeds - vitamin E. Carotenoids in powders are beta-carotene and lycopene. The high content of ascorbic acid, vitamin E and carotenoids in powder from wild rose hips makes them a good source of antioxidants. Therefore, we studied the possibility of using vegetable powders obtained from hips of wild rose, to enrich biologically active substances such as vitamins C, E and carotenoids, food supply, particularly of health care use. Rosehip powder from the pulp with the skins had the highest antioxidant activity, antioxidant activity of hips powders was 74% of the activity of powder from the pulp with the skins, the lowest antioxidant activity was observed in the powder from the wild rose seeds. That's way, based on the analysis of the chemical composition of rose hip powder found high levels they ascorbic acid, carotenoids, flavonoids,found their high antioxidant activity. It allows to recommend powders

  13. Phytochemical components and biological activities of Silene arenarioides Desf.

    Science.gov (United States)

    Golea, Lynda; Benkhaled, Mohammed; Lavaud, Catherine; Long, Christophe; Haba, Hamada

    2017-12-01

    In this study, six known compounds 1-6 were isolated from the aerial parts of Silene arenarioides Desf. using different chromatographic methods. The structures of these compounds were identified as maltol glycoside (1), soyacerebroside I (2), chrysin (3), apigenin (4), quercetin (5) and stigmasterol glucoside (6). The compounds (1) and (2) are reported for the first time from this genus. The isolated compounds were determined using NMR techniques ( 1 H NMR, 13 C NMR, COSY, HSQC and HMBC) and mass spectroscopy (ESI-MS). The antibacterial and antioxidant activities of extracts and of compound (1) have been evaluated. The antioxidant activity was performed by DPPH radical scavenging method, which showed that methanol extract possesses a good antioxidant activity with value of IC 50  = 8.064 ± 0.005 μg/mL.

  14. Aging evaluation of active components by using performance evaluation

    International Nuclear Information System (INIS)

    Jung, S. K.; Jin, T. E.; Kim, J. S.; Jung, I. S.; Kim, T. R.

    2003-01-01

    Risk analysis and performance evaluation methodology were applied to the aging evaluation of active components in the periodic safety review of Wolsung unit 1. We conclude that evaluation of performance is more effective to discriminate the aging degradation of active component than the evaluation of aging mechanism. It is essential to analyze the common cause failures of low performance components to evaluate the properness of present maintenance system. Past 10 years failure history is used for establishing the performance criteria. Past 2 years failure history is used for the evaluating the recent performance condition. We analyze the failure mode of the components to improve the maintenance system. Performance evaluation methodology is useful for the quantitative evaluation of aging degradation of active components. Analysis on the repeated failures can be useful for the feedback to maintenance plan and interval

  15. A Conceptual Framework for Organizing Active Learning Experiences in Biology Instruction

    Science.gov (United States)

    Gardner, Joel; Belland, Brian R.

    2012-01-01

    Introductory biology courses form a cornerstone of undergraduate instruction. However, the predominantly used lecture approach fails to produce higher-order biology learning. Research shows that active learning strategies can increase student learning, yet few biology instructors use all identified active learning strategies. In this paper, we…

  16. Modeling large scale cohesive sediment transport affected by small scale biological activity

    NARCIS (Netherlands)

    Borsje, Bastiaan Wijnand; de Vries, Mindert; Hulscher, Suzanne J.M.H.; de Boer, Gerben J.

    2008-01-01

    Biological activity on the bottom of the seabed is known to have significant influence on the dynamics of cohesive sediment on a small spatial and temporal scale. In this study, we aim to understand the large-scale effects of small-scale biological activity. Hereto, effects of biology are

  17. A novel conformation of gel grown biologically active cadmium nicotinate

    Science.gov (United States)

    Nair, Lekshmi P.; Bijini, B. R.; Divya, R.; Nair, Prabitha B.; Eapen, S. M.; Dileep Kumar, B. S.; Nishanth Kumar, S.; Nair, C. M. K.; Deepa, M.; Rajendra Babu, K.

    2017-11-01

    The elimination of toxic heavy metals by the formation of stable co-ordination compounds with biologically active ligands is applicable in drug designing. A new crystalline complex of cadmium with nicotinic acid is grown at ambient temperature using the single gel diffusion method in which the crystal structure is different from those already reported. Single crystal x-ray diffraction reveals the identity of crystal structure belonging to monoclinic system, P21/c space group with cell dimensions a = 17.220 (2) Å, b = 10.2480 (2) Å, c = 7.229(9) Å, β = 91.829(4)°. Powder x-ray diffraction analysis confirmed the crystallinity of the sample. The unidentate mode of co-ordination between the metal atom and the carboxylate group is supported by the Fourier Transform Infra Red spectral data. Thermal analysis ensures the thermal stability of the complex. Kinetic and thermodynamic parameters are also calculated. The stoichiometry of the complex is confirmed by the elemental analysis. The UV-visible spectral analysis shows the wide transparency window of the complex in the visible region. The band gap of the complex is found to be 3.92 eV. The complex shows excellent antibacterial and antifungal activity.

  18. Soil biological activity as affected by tillage intensity

    Science.gov (United States)

    Gajda, A. M.; Przewłoka, B.

    2012-02-01

    The effect of tillage intensity on changes of microbiological activity and content of particulate organic matter in soil under winter wheat duirng 3 years was studied. Microbial response related to the tillage-induced changes in soil determined on the content of biomass C and N, the rate of CO2 evolution, B/F ratio, the activity of dehydrogenases, acid and alkaline phosphatases, soil C/N ratio and microbial biomass C/N ratio confirmed the high sensitivity of soil microbial populations to the tillage system applied. After three year studies, the direct sowing system enhanced the increase of labile fraction of organic matter content in soil. There were no significant changes in the labile fraction quantity observed in soil under conventional tillage. Similar response related to the tillage intensity was observed in particulate organic matter quantities expressed as a percentage of total organic matter in soil. A high correlation coefficients calculated between contents of soil microbial biomass C and N, particulate organic matter and potentially mineralizable N, and the obtained yields of winter wheat grown on experimental fields indicated on a high importance of biological quality of status of soil for agricultural crop production.

  19. A Review on the Medicinal Plant Dalbergia odorifera Species: Phytochemistry and Biological Activity

    Directory of Open Access Journals (Sweden)

    Son Ninh The

    2017-01-01

    Full Text Available The crucial medicinal plant Dalbergia odorifera T. Chen species belongs to genus Dalbergia, with interesting secondary metabolites, consisting of main classes of flavonoid, phenol, and sesquiterpene derivatives, as well as several arylbenzofurans, quinones, and fatty acids. Biological studies were carried out on extracts, fractions, and compounds from this species involved in cytotoxic assays; antibacterial, antioxidative, anti-inflammatory, antithrombotic, antiplatelet, antiosteosarcoma, antiosteoporosis, antiangiogenesis, and prostaglandin biosynthetic enzyme inhibition activities; vasorelaxant activities; alpha-glucosidase inhibitory activities; and many other effects. In terms of the valuable resources for natural new drugs development, D. odorifera species are widely used as medicinal drugs in many countries for treatment of cardiovascular diseases, cancer, diabetes, blood disorders, ischemia, swelling, necrosis, or rheumatic pain. Although natural products from this plant have been increasingly playing an important role in drug discovery programs, there is no supportive evidence to provide a general insight into phytochemical studies on D. odorifera species and biological activities of extracts, fractions, and isolated compounds. To a certain extent, this review deals with an overview of almost naturally occurring compounds from this species, along with extensive coverage of their biological evaluations.

  20. Biological regeneration of phenol-loaded activated carbon (up flow system)

    International Nuclear Information System (INIS)

    Durrani, M.A.Q.J.; Mirajuddin; Martin, R.J.

    1995-01-01

    This paper represents the report on the biological regeneration of totally activated carbon following the experimental studies carried out at the University of Birmingham, U.K. Biological regeneration is one of several methods that may be used to restore the adsorptive capacity of exhausted granular activated carbon. This study deals with in situ biological regeneration on a pilot scale. The principal objective of this research was to ascertain whether biological regeneration of GAC could occur under conditions typical of water treatment. The important parameters which may have the greatest impact on bio regeneration for a given adsorbate were studied. The research investigated the extent of bio regeneration for phenol of concentration 50 mg/l. Bio regeneration in the total exhaustion system was evaluated in terms of regeneration efficiency and the substrate removal. A three mode procedure was followed for each bio regeneration run. The prepared carbon was initialing exhausted with an adsorbate; it was then bio regenerated with a mixed culture of bacteria, and lastly the carbon was saturated. In the totally exhausted GAC system, the bio regeneration was enhanced by increasing the duration of regeneration for a fixed initial biomass content of the bioreactor. The regenerated phenol loaded GAC bed had nearly gained its original adsorption after the 5-day period of regeneration. Bacterial counts in the effluents of regenerated GAC columns were significantly more than those of fresh carbon effluents. (author)

  1. Discovery and optimization of ATX inhibitors via modeling, synthesis and biological evaluation.

    Science.gov (United States)

    Balupuri, Anand; Lee, Myeong Hwi; Chae, Sangeun; Jung, Eunmi; Yoon, Woosub; Kim, Yunki; Son, So Jung; Ryu, Jeonghee; Kang, Dae-Hyuck; Yang, Young-Jae; You, Ji-Na; Kwon, Hyunjin; Jeong, Jong-Woo; Koo, Tae-Sung; Lee, Dae-Yon; Kang, Nam Sook

    2018-02-17

    Autotaxin (ATX) is a potential target for the treatment of various cancers. A new series of ATX inhibitors was rationally designed and synthesized based on our previous study. Biological evaluation and structure-activity relationship (SAR) of this series are discussed. Among fourteen synthesized derivatives, six compounds (2, 3, 4, 12, 13 and 14) exhibited enhanced ATX inhibitory activities with IC 50 values in the low nanomolar range. Molecular interactions of all the synthesized compounds within the active site of ATX were studied through molecular docking studies. Herein, we describe our lead optimization efforts that resulted in the identification of a potent ATX inhibitor (compound 4 with IC 50  = 1.23 nM, FS-3 and 2.18 nM, bis-pNPP). Furthermore, pharmacokinetic properties of this most promising compound are profiled. Copyright © 2018 Elsevier Masson SAS. All rights reserved.

  2. Asymmetric chemoenzymatic synthesis of miconazole and econazole enantiomers. The importance of chirality in their biological evaluation.

    Science.gov (United States)

    Mangas-Sánchez, Juan; Busto, Eduardo; Gotor-Fernández, Vicente; Malpartida, Francisco; Gotor, Vicente

    2011-04-01

    A simple and novel chemoenzymatic route has been applied for the first time in the synthesis of miconazole and econazole single enantiomers. Lipases and oxidoreductases have been tested in stereoselective processes; the best results were attained with oxidoreductases for the introduction of chirality in an adequate intermediate. The behaviors of a series of ketones and racemic alcohols in bioreductions and acetylation procedures, respectively, have been investigated; the best results were found with alcohol dehydrogenases A and T, which allowed the production of (R)-2-chloro-1-(2,4-dichlorophenyl)ethanol in enantiopure form under very mild reaction conditions. Final chemical modifications have been performed in order to isolate the target fungicides miconazole and econazole both as racemates and as single enantiomers. Biological evaluation of the racemates and single enantiomers has shown remarkable differences against the growth of several microorganisms; while (R)-miconazole seemed to account for most of the biological activity of racemic miconazole on all the strains tested, both enantiomers of econazole showed considerable biological activities. In this manner, (R)-econazole showed higher values against Candida krusei , while higher values were observed for (S)-econazole against Cryptococcus neoformans, Penicillium chrysogenum, and Aspergillus niger.

  3. Synthesis and biological evaluation of dihydropyrano-[2,3-c]pyrazoles as a new class of PPARγ partial agonists

    DEFF Research Database (Denmark)

    Qvortrup, Katrine; Jensen, Jakob Feldthusen; Sørensen, Mikael S.

    2017-01-01

    Peroxisome proliferator-activated receptor γ (PPARγ) is a well-known target for thiazolidinedione antidiabetic drugs. In this paper, we present the synthesis and biological evaluation of a series of dihydropyrano[2,3-c]pyrazole derivatives as a novel family of PPARγ partial agonists. Two analogue...

  4. Actinobacteria from arid and desert habitats: diversity and biological activity

    Directory of Open Access Journals (Sweden)

    Joachim eWink

    2016-01-01

    Full Text Available Abstract The lack of new antibiotics in the pharmaceutical pipeline guides more and more researchers to leave the classical isolation procedures and to look in special niches and ecosystems. Bioprospecting of extremophilic Actinobacteria through mining untapped strains and avoiding resiolation of known biomolecules is among the most promising strategies for this purpose. With this approach, members of acidtolerant, alkalitolerant, psychrotolerant, thermotolerant, halotolerant and xerotolerant Actinobacteria have been obtained from respective habitats. Among these, little survey exists on the diversity of Actinobacteria in arid areas, which are often adapted to relatively high temperatures, salt concentrations, and radiation. Therefore, arid and desert habitats are special ecosystems which can be recruited for the isolation of uncommon Actinobacteria with new metabolic capability.At the time of this writing, members of Streptomyces, Micromonospora, Saccharothrix, Streptosporangium, Cellulomonas, Amycolatopsis, Geodermatophilus, Lechevalieria, Nocardia and Actinomadura are reported from arid habitats. However, metagenomic data present dominant members of the communities in desiccating condition of areas with limited water availability that are not yet isolated. Furthermore, significant diverse types of polyketide synthase (PKS and nonribosomal peptide synthetase (NRPS genes are detected in xerophilic and xerotolerant Actinobacteria and some bioactive compounds are reported from them. Rather than pharmaceutically active metabolites, molecules with protection activity against drying such as Ectoin and Hydroxyectoin with potential application in industry and agriculture have also been identified from xerophilic Actinobacteria. In addition, numerous biologically active small molecules are expected to be discovered from arid adapted Actinobacteria in the future. In the current survey, the diversity and biotechnological potential of Actinobacteria

  5. Actinobacteria from Arid and Desert Habitats: Diversity and Biological Activity.

    Science.gov (United States)

    Mohammadipanah, Fatemeh; Wink, Joachim

    2015-01-01

    The lack of new antibiotics in the pharmaceutical pipeline guides more and more researchers to leave the classical isolation procedures and to look in special niches and ecosystems. Bioprospecting of extremophilic Actinobacteria through mining untapped strains and avoiding resiolation of known biomolecules is among the most promising strategies for this purpose. With this approach, members of acidtolerant, alkalitolerant, psychrotolerant, thermotolerant, halotolerant and xerotolerant Actinobacteria have been obtained from respective habitats. Among these, little survey exists on the diversity of Actinobacteria in arid areas, which are often adapted to relatively high temperatures, salt concentrations, and radiation. Therefore, arid and desert habitats are special ecosystems which can be recruited for the isolation of uncommon Actinobacteria with new metabolic capability. At the time of this writing, members of Streptomyces, Micromonospora, Saccharothrix, Streptosporangium, Cellulomonas, Amycolatopsis, Geodermatophilus, Lechevalieria, Nocardia, and Actinomadura are reported from arid habitats. However, metagenomic data present dominant members of the communities in desiccating condition of areas with limited water availability that are not yet isolated. Furthermore, significant diverse types of polyketide synthase (PKS) and non-ribosomal peptide synthetase (NRPS) genes are detected in xerophilic and xerotolerant Actinobacteria and some bioactive compounds are reported from them. Rather than pharmaceutically active metabolites, molecules with protection activity against drying such as Ectoin and Hydroxyectoin with potential application in industry and agriculture have also been identified from xerophilic Actinobacteria. In addition, numerous biologically active small molecules are expected to be discovered from arid adapted Actinobacteria in the future. In the current survey, the diversity and biotechnological potential of Actinobacteria obtained from arid ecosystems

  6. Isolation, Biological Activities and Synthesis of Indoloquinoline Alkaloids: Cryptolepine, Isocryptolepine and Neocryptolepine

    Digital Repository Service at National Institute of Oceanography (India)

    Parvatkar, P.T.; Parameswaran, P.S.; Tilve, S.G.

    of biological properties. This review describes the isolation, brief biological activities and various synthetic methodologies developed during recent years for the preparation of this important class of alkaloids, with special emphasis on preparation...

  7. Biological evaluation of silver nanoparticles incorporated into chitosan-based membranes

    NARCIS (Netherlands)

    Shao, J.; Yu, N.; Kolwijck, E.; Wang, B.; Tan, K.W.; Jansen, J.A.; Walboomers, X.F.; Yang, F.

    2017-01-01

    AIM: To evaluate the antibacterial potential and biological performance of silver nanoparticles in chitosan-based membranes. MATERIALS & METHODS: Electrospun chitosan/poly(ethylene oxide) membranes with different amounts of silver nanoparticles were evaluated for antibacterial properties and

  8. Synthesis, Biological Evaluation and Molecular Docking of New Benzenesulfonylhydrazone as Potential anti-Trypanosoma cruzi Agents.

    Science.gov (United States)

    Elizondo-Jimenez, Silvia; Moreno-Herrera, Antonio; Reyes-Olivares, Rogelio; Dorantes-Gonzalez, Edith; Nogueda-Torres, Benjamín; Oliveira, Eduardo A Gamosa de; Romeiro, Nelilma C; Lima, Lidia M; Palos, Isidro; Rivera, Gildardo

    2017-01-01

    Chagas disease is a public health problem caused by Trypanosoma cruzi. Cruzain is a pharmacological target for designing a new drug against this parasite. Hydrazone and Nacylhydrazone derivatives have been traditionally associated as potential Cruzain inhibitors. Additionally, benzenesulfonyl derivatives show trypanocidal activity. Therefore, in this study, the combination of both structures has been taken into account for drug design. Seven benzenesulfonylhydrazone (BS-H) and seven N-propionyl benzenesulfonylhydrazone (BS-NAH) derivatives were synthetized and elucidated by infrared spectroscopy, nuclear magnetic resonance, and elemental analysis. All compounds were evaluated biologically in vitro against two strains of Trypanosoma cruzi (NINOA and INC-5), which are endemic in Mexico, and compared with the reference drugs nifurtimox and benznidazole. In order to gain insight into the putative molecular origin of the trypanocidal properties of these derivatives, docking studies were carried out with Cruzain. Compounds 4 and 6 (BS-H) and 10, 12-14 (BS-NAH) showed the best biological activity against NINOA and INC-5 strains, respectively. Compound 13 was the most potent trypanocidal compound showing a LC50 of 0.06 µM against INC-5 strain. However, compound 4 showed the best activity against both strains (LC50 activity. Benzenesulfonyl and N-propionyl benzenesulfonyl hydrazone derivatives are good options for developing new trypanocidal agents. Particularly, compound 4 could be considered a lead compound. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

  9. [Biologically active substances of black currant of new varieties].

    Science.gov (United States)

    Miasishcheva, N V; Artemova, E N

    2013-01-01

    The assortment of black currant actively replenishes and is constantly updated as a result of successful work of domestic and foreign selectors. New grades of black currant are characterized by the raised content of biologically active substances, including vitamin C, P-active agents, pectin and are of special interest for studying. Fresh berries of seven grades (Azhurnaya, Arapka, Iskushenie, Kreolka, Ladushka, Orel serenade, Ocharovanie) of black currant which were selected by the All-Russian research institute of selection of fruit crops and are perspective for cultivation in the Central Chernozem Region of Russia were chosen as objects for research. The nutritional value of fresh berries was found to vary. Average content of soluble solids was 14.1%, while those below the average were observed in Kreolka (12.1%). The maximum amount of sugars characterized Ladushka grade (11.05%), minimum--Kreolka (9.00%). It has been found that most varieties have fairly high acidity. It is worth noting grade Ladushka, which had the highest sugar-acid index (4.39), with the lowest acidity (2.51%). The highest content of ascorbic acid was found in varieties Orel Serenade--183.7 mg/100 g, the smallest--Ocharovanie--110 mg/100 g, grade Azhurnaya, Kreolka, Ladushka exceeded this indicator average value (144.9 mg/100 g). In terms of the amount of P-active substances stood grades having values above the average (722.2 mg/100 g): Azhurnaya (789.8 mg/100 g), Kreolka (864.5 mg/100 g), Oryol serenade (765.6 mg/100 g). The average content of pectin in the studied berries of black currant was 7.92%, with a minimum of 6.30% was observed in grades Azhurnaya, maximum 9.90%--the kind Oryol serenade. High values of this index were characterized by grade Ladushka, Ocharovanie. Azhurnaya varieties, Creole, Orel serenade had high levels of ascorbic acid and P-active substances. Sort Ladushka marked as a dessert due to the largest sugar-acid ratio. Ladushka, Orel Serenade, Ocharovanie have the

  10. 76 FR 71045 - Center for Biologics Evaluation and Research Report of Scientific and Medical Literature and...

    Science.gov (United States)

    2011-11-16

    ...] Center for Biologics Evaluation and Research Report of Scientific and Medical Literature and Information... ``Center for Biologics Evaluation and Research Report of Scientific and Medical Literature and Information... period for the notice on its report of scientific and medical literature and information concerning the...

  11. 75 FR 6401 - Medical Devices Regulated by the Center for Biologics Evaluation and Research; Availability of...

    Science.gov (United States)

    2010-02-09

    ... Biologics Evaluation and Research (HFM-17), Food and Drug Administration, suite 200N, 1401 Rockville Pike... DEPARTMENT OF HEALTH AND HUMAN SERVICES Food and Drug Administration [Docket No. FDA-2009-M-0513] Medical Devices Regulated by the Center for Biologics Evaluation and Research; Availability of Summaries...

  12. Synthesis and Biological Evaluation of Glycosidase Inhibitors: gem-Difluoromethylenated Nojirimycin Analogues

    DEFF Research Database (Denmark)

    Bols, Mikael; Wang, Ruo-Wen; Qiu, Xiao-Long

    2006-01-01

    In our ongoing program aimed at the design, synthesis, and biological evaluation of novel gem-difluoromethylenated glycosidase inhibitors, gem-4,4-difluoromethylenated iminosugars (5-9) were synthesized. The biological evaluation of these synthetic iminosugars showed that the gem...

  13. A Survey of Biology Teachers Use of Activity-Oriented, Laboratory Practical Exercises to Promote Functional Biology Education

    Directory of Open Access Journals (Sweden)

    Abigail Mgboyibo Osuafor

    2016-08-01

    Full Text Available A major goal of science education is fostering students’ intellectual competencies such as independent learning, problem-solving, decision-making and critical thinking. This goal can only be achieved when students are actively involved in the teaching-learning process through activity-based, practical-oriented instructional methods involving the use of laboratories. This study therefore, investigated the extent to which the biology teachers employ activity-oriented, laboratory/practical instructional methods in order to improve the learning outcome of their students. The descriptive survey involved 73 Biology teachers randomly selected from all the six education zones of Anambra state, Nigeria. Four research questions were posed and four hypotheses were formulated to guide the conduct of the study. A 32-item structured questionnaire which has reliability co-efficient of 0.82 was used to collect data. Data were analyzed using mean, standard deviation and t-tests. Results show that Biology teachers adopt practical-oriented strategies in teaching biology, conduct practical activities to a high extent, and perceive practical exercises as essential to effective teaching and learning of the subject. Provision of adequate number of laboratory materials, employment of adequate number of biology teachers, making provision for well designed laboratory activities in the curriculum and training of teachers on how to effectively combine theory with practical are some of the strategies that will encourage biology teachers to conduct practical lessons. There was no significant difference between male and female biology teachers in their responses to the different aspects investigated. Based on these findings, some recommendations were made that include that curriculum designers should incorporate guides for practical activities that go with each topic in the curriculum so as to encourage the teachers to teach theory with practical as a unified whole to

  14. Compositional studies and Biological activities of Perovskia abrotanoides Kar. oils

    OpenAIRE

    Ashraf, Sadaf Naz; Zubair, Muhammad; Rizwan, Komal; Tareen, Rasool Bakhsh; Rasool, Nasir; Zia-Ul-Haq, Muhammad; Ercisli, Sezai

    2014-01-01

    Background Current study has been designed to evaluate the chemical composition of essential and fixed oils from stem and leaves of Perovskia abrotanoides and antioxidant and antimicrobial activities of these oils. Results GC-MS analysis of essential oil identified 19 compounds with (E)-9-dodecenal being the major component in stem and hexadecanoic acid in leaves. In contrast, GC-MS analysis of fixed oil showed 40 constituents with α-amyrin the major component in stem and α-copaene in leaves....

  15. Essential Oils from Neotropical Piper Species and Their Biological Activities

    Science.gov (United States)

    da Trindade, Rafaela; Alves, Nayara Sabrina; Figueiredo, Pablo Luís; Maia, José Guilherme S.; Setzer, William N.

    2017-01-01

    The Piper genus is the most representative of the Piperaceae reaching around 2000 species distributed in the pantropical region. In the Neotropics, its species are represented by herbs, shrubs, and lianas, which are used in traditional medicine to prepare teas and infusions. Its essential oils (EOs) present high yield and are chemically constituted by complex mixtures or the predominance of main volatile constituents. The chemical composition of Piper EOs displays interspecific or intraspecific variations, according to the site of collection or seasonality. The main volatile compounds identified in Piper EOs are monoterpenes hydrocarbons, oxygenated monoterpenoids, sesquiterpene hydrocarbons, oxygenated sesquiterpenoids and large amounts of phenylpropanoids. In this review, we are reporting the biological potential of Piper EOs from the Neotropical region. There are many reports of Piper EOs as antimicrobial agents (fungi and bacteria), antiprotozoal (Leishmania spp., Plasmodium spp., and Trypanosoma spp.), acetylcholinesterase inhibitor, antinociceptive, anti-inflammatory and cytotoxic activity against different tumor cells lines (breast, leukemia, melanoma, gastric, among others). These studies can contribute to the rational and economic exploration of Piper species, once they have been identified as potent natural and alternative sources to treat human diseases. PMID:29240662

  16. Isoflavone profile and biological activity of soy bread.

    Science.gov (United States)

    Zhang, Yu Chu; Albrecht, Daniel; Bomser, Joshua; Schwartz, Steven J; Vodovotz, Yael

    2003-12-17

    The present study examines the ability of isoflavone extracts from whole soy bread and two soy bread fractions, crumb and crust, to modulate the proliferation of human prostate cancer PC-3 cells. Total isoflavone content in the two fractions of soy bread were similar (3.17 micromol/g dry basis). However, their conjugate patterns were altered. Both fractions of soy bread contained a similar level of isoflavone aglycones ( approximately 24%). Low concentrations of soy bread extracts increased PC-3 cell proliferation as much as 47% compared to untreated control. This proliferative effect in cell growth was reduced at higher extract concentration. Soy bread crust extract (10 mg/mL) reduced PC-3 cell proliferation by 15% compared to untreated control. Interestingly, wheat bread extracts increased cell proliferation at all concentrations tested. Although extracts from both breads possessed biological activity, only soy bread crust extract reduced PC-3 cell proliferation. This observation may be related to the presence of soy in this bread.

  17. Nonoxidized, biologically active parathyroid hormone determines mortality in hemodialysis patients

    DEFF Research Database (Denmark)

    Tepel, Martin; Armbruster, Franz Paul; Grön, Hans Jürgen

    2013-01-01

    Background: It was shown that nonoxidized PTH (n-oxPTH) is bioactive, whereas the oxidation of PTH results in a loss of biological activity. Methods: In this study we analyzed the association of n-oxPTH on mortality in hemodialysis patients using a recently developed assay system. Results......: Hemodialysis patients (224 men, 116 women) had a median age of 66 years. One hundred seventy patients (50%) died during the follow-up period of 5 years. Median n-oxPTH levels were higher in survivors (7.2 ng/L) compared with deceased patients (5.0 ng/L; P = .002). Survival analysis showed an increased survival...... in the highest n-oxPTH tertile compared with the lowest n-oxPTH tertile (χ(2), 14.3; P = .0008). Median survival was 1702 days in the highest n-oxPTH tertile, whereas it was only 453 days in the lowest n-oxPTH tertile. Multivariable-adjusted Cox regression showed that higher age increased odds for death, whereas...

  18. Synthesis of Combretastatin A-4 Analogs and their Biological Activities.

    Science.gov (United States)

    Siebert, Agnieszka; Gensicka, Monika; Cholewinski, Grzegorz; Dzierzbicka, Krystyna

    2016-01-01

    Combretastatin A-4 (CA-4) is a natural product, which consists of two phenyl rings, linked by an ethylene bridge. CA-4, inhibitor of polymerization of tubulin to microtubules, possesses a strong antitumor and anti-vascular properties both in vitro and in vivo. Previous studies showed that disodium phosphate salt of CA-4, a water-soluble prodrug is well tolerated at therapeutically useful doses. However, it should be noted that the cis-configuration of the double bond and the 3,4,5-trimethoxy group on ring A is necessary for the biological activity of CA-4. Structure of CA-4 renders the compound readily susceptible to isomerization, which reduces the potency and bioavailability. To circumvent this problem, a lot of scientists in the world synthesized a series of cis-restricted CA-4 analogs, where the double bond has been replaced by introduction of non-heterocyclic groups or heterocyclic groups like β -lactam and oxadiazole. This paper reviews the most important approaches in analogs of combretastatin synthesis and presents structure-reactivity relationships for these compounds. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

  19. Biological Activities of Three Essential Oils of the Lamiaceae Family

    Directory of Open Access Journals (Sweden)

    Gema Nieto

    2017-08-01

    Full Text Available Herbs and spices have been used since ancient times to improve the sensory characteristics of food, to act as preservatives and for their nutritional and healthy properties. Herbs and spices are generally recognized as safe (GRAS and are excellent substitutes for chemical additives. Essential oils are mixtures of volatile compounds obtained, mainly by steam distillation, from medicinal and aromatic plants. They are an alternative to synthetic additives for the food industry, and they have gained attention as potential sources for natural food preservatives due to the growing interest in the development of safe, effective, natural food preservation. Lamiaceae is one of the most important families in the production of essential oils with antioxidants and antimicrobial properties. Aromatic plants are rich in essential oils and are mainly found in the Mediterranean region, where the production of such oils is a profitable source of ecological and economic development. The use of essential oils with antimicrobial and antioxidant properties to increase the shelf life of food is a promising technology, and the essential oils of the Lamiaceae family, such as rosemary, thyme, and sage, have been extensively studied with respect to their use as food preservatives. Regarding the new applications of essential oils, this review gives an overview of the current knowledge and recent trends in the use of these oils from aromatic plants as antimicrobials and antioxidants in foods, as well as their biological activities, future potential, and challenges.

  20. Biological Activities of Three Essential Oils of the Lamiaceae Family.

    Science.gov (United States)

    Nieto, Gema

    2017-08-23

    Herbs and spices have been used since ancient times to improve the sensory characteristics of food, to act as preservatives and for their nutritional and healthy properties. Herbs and spices are generally recognized as safe (GRAS) and are excellent substitutes for chemical additives. Essential oils are mixtures of volatile compounds obtained, mainly by steam distillation, from medicinal and aromatic plants. They are an alternative to synthetic additives for the food industry, and they have gained attention as potential sources for natural food preservatives due to the growing interest in the development of safe, effective, natural food preservation. Lamiaceae is one of the most important families in the production of essential oils with antioxidants and antimicrobial properties. Aromatic plants are rich in essential oils and are mainly found in the Mediterranean region, where the production of such oils is a profitable source of ecological and economic development. The use of essential oils with antimicrobial and antioxidant properties to increase the shelf life of food is a promising technology, and the essential oils of the Lamiaceae family, such as rosemary, thyme, and sage, have been extensively studied with respect to their use as food preservatives. Regarding the new applications of essential oils, this review gives an overview of the current knowledge and recent trends in the use of these oils from aromatic plants as antimicrobials and antioxidants in foods, as well as their biological activities, future potential, and challenges.

  1. Polyphenols from Bee Pollen: Structure, Absorption, Metabolism and Biological Activity

    Directory of Open Access Journals (Sweden)

    Anna Rzepecka-Stojko

    2015-12-01

    Full Text Available Bee pollen constitutes a natural source of antioxidants such as phenolic acids and flavonoids, which are responsible for its biological activity. Research has indicated the correlation between dietary polyphenols and cardioprotective, hepatoprotective, anti-inflammatory, antibacterial, anticancerogenic, immunostimulating, antianaemic effects, as well as their beneficial influence on osseous tissue. The beneficial effects of bee pollen on health result from the presence of phenolic acids and flavonoids which possess anti-inflammatory properties, phytosterol and linolenic acid which play an anticancerogenic role, and polysaccharides which stimulate immunological activity. Polyphenols are absorbed in the alimentary tract, metabolised by CYP450 enzymes, and excreted with urine and faeces. Flavonoids and phenolic acids are characterised by high antioxidative potential, which is closely related to their chemical structure. The high antioxidant potential of phenolic acids is due to the presence and location of hydroxyl groups, a carboxyl group in the immediate vicinity of ortho-diphenolic substituents, and the ethylene group between the phenyl ring and the carboxyl group. As regards flavonoids, essential structural elements are hydroxyl groups at the C5 and C7 positions in the A ring, and at the C3′ and C4′ positions in the B ring, and a hydroxyl group at the C3 position in the C ring. Furthermore, both, the double bond between C2 and C3, and a ketone group at the C4 position in the C ring enhance the antioxidative potential of these compounds. Polyphenols have an ideal chemical structure for scavenging free radicals and for creating chelates with metal ions, which makes them effective antioxidants in vivo.

  2. Sustainable production of biologically active molecules of marine based origin.

    Science.gov (United States)

    Murray, Patrick M; Moane, Siobhan; Collins, Catherine; Beletskaya, Tanya; Thomas, Olivier P; Duarte, Alysson W F; Nobre, Fernando S; Owoyemi, Ifeloju O; Pagnocca, Fernando C; Sette, L D; McHugh, Edward; Causse, Eric; Pérez-López, Paula; Feijoo, Gumersindo; Moreira, Ma T; Rubiolo, Juan; Leirós, Marta; Botana, Luis M; Pinteus, Susete; Alves, Celso; Horta, André; Pedrosa, Rui; Jeffryes, Clayton; Agathos, Spiros N; Allewaert, Celine; Verween, Annick; Vyverman, Wim; Laptev, Ivan; Sineoky, Sergei; Bisio, Angela; Manconi, Renata; Ledda, Fabio; Marchi, Mario; Pronzato, Roberto; Walsh, Daniel J

    2013-09-25

    The marine environment offers both economic and scientific potential which are relatively untapped from a biotechnological point of view. These environments whilst harsh are ironically fragile and dependent on a harmonious life form balance. Exploitation of natural resources by exhaustive wild harvesting has obvious negative environmental consequences. From a European industry perspective marine organisms are a largely underutilised resource. This is not due to lack of interest but due to a lack of choice the industry faces for cost competitive, sustainable and environmentally conscientious product alternatives. Knowledge of the biotechnological potential of marine organisms together with the development of sustainable systems for their cultivation, processing and utilisation are essential. In 2010, the European Commission recognised this need and funded a collaborative RTD/SME project under the Framework 7-Knowledge Based Bio-Economy (KBBE) Theme 2 Programme 'Sustainable culture of marine microorganisms, algae and/or invertebrates for high value added products'. The scope of that project entitled 'Sustainable Production of Biologically Active Molecules of Marine Based Origin' (BAMMBO) is outlined. Although the Union is a global leader in many technologies, it faces increasing competition from traditional rivals and emerging economies alike and must therefore improve its innovation performance. For this reason innovation is placed at the heart of a European Horizon 2020 Strategy wherein the challenge is to connect economic performance to eco performance. This article provides a synopsis of the research activities of the BAMMBO project as they fit within the wider scope of sustainable environmentally conscientious marine resource exploitation for high-value biomolecules. Copyright © 2013 Elsevier B.V. All rights reserved.

  3. Evaluation of various substrates and supplements for biological ...

    African Journals Online (AJOL)

    An experiment was conducted to determine the effects of different substrates namely wheat straw (Triticum aestivum), maize stover (Zea mays L), thatch grass (Hyparrhenia filipendula) and oil/protein rich supplements (maize bran, cottonseed hull [Gossypium hirsutum]) on biological efficiency of two oyster mushroom ...

  4. Biological Evaluation of the Protein Quality Sponge Guord ( Luffa ...

    African Journals Online (AJOL)

    Clinical performance of the test animals was determined. The faecal and urinal Nitrogen content were recorded. The True Protein Digestibility (TD); Biological value (BV); Net Protein Utilization (NPU); Net Protein Retention (NPR); and Protein Efficiency Ratio (PER) were determined for the various diets used. Results: There ...

  5. Structural Systems Biology Evaluation of Metabolic Thermotolerance in Escherichia coli

    DEFF Research Database (Denmark)

    Chang, Roger L.; Andrews, Kathleen; Kim, Donghyuk

    2013-01-01

    Improve the System A "systems biology" approach may clarify, for example, how particular proteins determine sensitivity of bacteria to extremes of temperature. Chang et al. (p. 1220) integrated information on protein structure with a model of metabolism, thus associating the protein structure of ...

  6. Identification and evaluation of Trichogramma parasitoids for biological pest control

    NARCIS (Netherlands)

    Silva, e I.M.M.S.

    1999-01-01

    Egg parasitoids of the genus Trichogramma are used as biological control agents against lepidopterous pests. From the 180 species described world-wide, only 5 have large scale application. The development of better methods to select other

  7. Simple synthesis and biological evaluation of flocoumafen and its ...

    Indian Academy of Sciences (India)

    Full Papers Volume 122 Issue 6 November 2010 pp 833-838 ... Abstract. Simple synthesis and biological properties of flocoumafen 1 and its structural isomers are described. The key synthetic strategies involve Knoevenagel condensation, Grignard reaction, intramolecular ring cyclization and coupling reaction.

  8. Simple synthesis and biological evaluation of flocoumafen and its ...

    Indian Academy of Sciences (India)

    Administrator

    Abstract. Simple synthesis and biological properties of flocoumafen 1 and its structural isomers are described. The key synthetic strategies involve Knoevenagel condensation, Grignard reaction, intramolecu- lar ring cyclization and coupling reaction. Flocoumafen 1 was easily separated into cis and trans forms using flash ...

  9. Synthesis of N-(6-Arylbenzo[d]thiazole-2-acetamide Derivatives and Their Biological Activities: An Experimental and Computational Approach

    Directory of Open Access Journals (Sweden)

    Yasmeen Gull

    2016-02-01

    Full Text Available A new series of N-(6-arylbenzo[d]thiazol-2-ylacetamides were synthesized by C-C coupling methodology in the presence of Pd(0 using various aryl boronic pinacol ester/acids. The newly synthesized compounds were evaluated for various biological activities like antioxidant, haemolytic, antibacterial and urease inhibition. In bioassays these compounds were found to have moderate to good activities. Among the tested biological activities screened these compounds displayed the most significant activity for urease inhibition. In urease inhibition, all compounds were found more active than the standard used. The compound N-(6-(p-tolylbenzo[d]thiazol-2-ylacetamide was found to be the most active. To understand this urease inhibition, molecular docking studies were performed. The in silico studies showed that these acetamide derivatives bind to the non-metallic active site of the urease enzyme. Structure-activity studies revealed that H-bonding of compounds with the enzyme is important for its inhibition.

  10. Evaluation of reversible contraceptive activities of Annona ...

    African Journals Online (AJOL)

    Evaluation of reversible contraceptive activities of Annona squamosa (Linn.) ... Plant Products Research Journal ... Therefore the present study was undertaken to evaluate the contraceptive activities of methanol extract of the stem bark of Annoa squamosa L. (Annonaceae) with their respective reversibility in male rats.

  11. Active spectral imaging nondestructive evaluation (SINDE) camera

    Energy Technology Data Exchange (ETDEWEB)

    Simova, E.; Rochefort, P.A., E-mail: eli.simova@cnl.ca [Canadian Nuclear Laboratories, Chalk River, Ontario (Canada)

    2016-06-15

    A proof-of-concept video camera for active spectral imaging nondestructive evaluation has been demonstrated. An active multispectral imaging technique has been implemented in the visible and near infrared by using light emitting diodes with wavelengths spanning from 400 to 970 nm. This shows how the camera can be used in nondestructive evaluation to inspect surfaces and spectrally identify materials and corrosion. (author)

  12. Design and synthesis of a new steroid-macrocyclic derivative with biological activity.

    Science.gov (United States)

    López-Ramos, Maria; Figueroa-Valverde, Lauro; Herrera-Meza, Socorro; Rosas-Nexticapa, Marcela; Díaz-Cedillo, Francisco; García-Cervera, Elodia; Pool-Gómez, Eduardo; Cahuich-Carrillo, Regina

    2017-04-01

    The aims of this study were to evaluate the positive inotropic effect of a new macrocyclic derivative (compound 11 ) and characterize the molecular mechanism involved in its biological activity. The first step was achieved by synthesis of a macrocyclic derivative involving a series of reactions for the preparation of several steroid derivatives such as (a) steroid-pyrimidinone ( 3 and 4 ), (b) steroid-amino ( 5 ), (c) steroid-imino ( 6 ), (d) ester-steroid ( 7 and 8 ), and (e) amido-steroid ( 9 and 10 ). Finally, 11 was prepared by removing the tert -butyldimethylsilane fragment of 10 . The biological activity of compounds on perfusion pressure and vascular resistance was evaluated on isolated rat heart using the Langendorff model. The inotropic activity of 11 was evaluated in presence of prazosin, metoprolol, indomethacin, nifedipine, and flutamide to characterize its molecular mechanism. Theoretical experiments were carried out with a Docking model, to assess potential interactions of androgen receptor with 11 . The results showed that only this macrocyclic derivative exerts changes on perfusion pressure and vascular resistance translated as the positive inotropic effect, and this effect was blocked with flutamide; these data indicate that the positive inotropic activity induced by this macrocyclic derivative was via androgen receptor activation. The theoretical results indicated that the interaction of the macrocyclic derivative with the androgen receptor involves several amino acid residues such as Leu 704 , Asn 705 , Met 780 , Cys 784 , Met 749 , Leu 762 , Phe 764 , Ser 778 , and Met 787 . In conclusion, all these data suggest that the positive inotropic activity of the macrocyclic derivative may depend on its chemical structure.

  13. Biological activities of Agave by-products and their possible applications in food and pharmaceuticals.

    Science.gov (United States)

    López-Romero, Julio Cesar; Ayala-Zavala, Jesús Fernando; González-Aguilar, Gustavo Adolfo; Peña-Ramos, Etna Aida; González-Ríos, Humberto

    2017-10-11

    Agave leaves are considered a by-product of alcoholic beverage production (tequila, mezcal and bacanora) because they are discarded during the production process, despite accounting for approximately 50% of the total plant weight. These by-products constitute a potential source of Agave extracts rich in bioactive compounds, such as saponins, phenolic compounds and terpenes, and possess different biological effects, as demonstrated by in vitro and in vivo tests (e.g. antimicrobial, antifungal, antioxidant, anti-inflammatory, antihypertensive, immunomodulatory, antiparasitic and anticancer activity). Despite their positive results in biological assays, Agave extracts have not been widely evaluated in food systems and pharmaceutical areas, and these fields represent a potential route to improve the usage of Agave plants as food additives and agents for treating medical diseases. © 2017 Society of Chemical Industry. © 2017 Society of Chemical Industry.

  14. Review-An overview of Pistacia integerrima a medicinal plant species: Ethnobotany, biological activities and phytochemistry.

    Science.gov (United States)

    Bibi, Yamin; Zia, Muhammad; Qayyum, Abdul

    2015-05-01

    Pistacia integerrima with a common name crab's claw is an ethnobotanically important tree native to Asia. Traditionally plant parts particularly its galls have been utilized for treatment of cough, asthma, dysentery, liver disorders and for snake bite. Plant mainly contains alkaloids, flavonoids, tannins, saponins and sterols in different parts including leaf, stem, bark, galls and fruit. A number of terpenoids, sterols and phenolic compounds have been isolated from Pistacia integerrima extracts. Plant has many biological activities including anti-microbial, antioxidant, analgesic, cytotoxicity and phytotoxicity due to its chemical constituents. This review covers its traditional ethnomedicinal uses along with progresses in biological and phytochemical evaluation of this medicinally important plant species and aims to serve as foundation for further exploration and utilization.

  15. Alternative preparation of propolis extracts: comparison of their composition and biological activities.

    Science.gov (United States)

    Kubiliene, Loreta; Laugaliene, Virginija; Pavilonis, Alvydas; Maruska, Audrius; Majiene, Daiva; Barcauskaite, Karolina; Kubilius, Raimondas; Kasparaviciene, Giedre; Savickas, Arunas

    2015-05-27

    Propolis is the bee product noted for multiple biological effects, and therefore it is widely used for the prevention and treatment of a variety of diseases. The active substances of propolis are easily soluble in ethanol. However ethanolic extracts cannot be used in treatment of certain diseases encountered in ophthalmology, pediatrics, etc. Unfortunately, the main biologically active substances of propolis are scarcely soluble in water, oil and other solvents usually used in pharmaceutical industry. The aim of this study was to investigate chemical composition, radical scavenging and antimicrobial activity of propolis extracts differently made in nonethanolic solvents. Total content of phenolic compounds in extracts was determined using Folin-Ciocalteu method. Chemical composition and radical scavenging activity of extracts were determined using HPLC system with free radical reaction detector. Antimicrobial activity of examined preparations was evaluated using the agar-well diffusion assay. Total amount of phenolic compounds in extracts made in polyethylene glycol 400 (PEG) and water mixture or in PEG, olive oil and water mixture at 70 °C was comparable to that of ethanolic extract. Predominantly identified compounds were phenolic acids, which contribute ca. 40 % of total radical scavenging activity. Investigated nonethanolic extracts inhibited the growth and reproduction of all tested microrganisms. Antimicrobial activity of some extracts was equal or exceeded the antimicrobial effect of ethanolic extract. Extracts made in pure water or oil only at room temperature, contained more than 5 - 10-fold lower amount of phenolic compounds, and demonstrated no antimicrobial activity. Nonethanolic solvent complex and the effect of higher temperature allows more effective extraction of active compounds from propolis. Concentration of total phenolic compounds in these extracts does not differ significantly from the concentration found in ethanolic extract. Propolis

  16. Small group gender ratios impact biology class performance and peer evaluations.

    Science.gov (United States)

    Sullivan, Lauren L; Ballen, Cissy J; Cotner, Sehoya

    2018-01-01

    Women are underrepresented in science, technology, engineering, and mathematics (STEM) disciplines. Evidence suggests the microclimate of the classroom is an important factor influencing female course grades and interest, which encourages retention of women in STEM fields. Here, we test whether the gender composition of small (8-9 person) learning groups impacts course performance, sense of social belonging, and intragroup peer evaluations of intellectual contributions. Across two undergraduate active learning courses in introductory biology, we manipulated the classroom microclimate by varying the gender ratios of learning groups, ranging from 0% female to 100% female. We found that as the percent of women in groups increased, so did overall course performance for all students, regardless of gender. Additionally, women assigned higher peer- evaluations in groups with more women than groups with less women. Our work demonstrates an added benefit of the retention of women in STEM: increased performance for all, and positive peer perceptions for women.

  17. Biological Activity of Bacillus thuringiensis (Bacillales: Bacillaceae) in Anastrepha fraterculus (Diptera: Tephritidae).

    Science.gov (United States)

    Martins, Liliane Nachtigall; Lara, Ana Paula de Souza Stori de; Ferreira, Márcio Soares; Nunes, Adrise Medeiros; Bernardi, Daniel; Leite, Fábio Pereira Leivas; Garcia, Flávio Roberto Mello

    2018-01-18

    Anastrepha fraterculus (Wiedemann) (Diptera: Tephritidae) is considered to be one of the major pest insects in fruit orchards worldwide. Bacillus thuringiensis Berliner (Bacillales: Bacillaceae) strains are widely used as biological control agents and show high biological activity against different insect species. The objective of this study was to evaluate the biological activity of different strains of B. thuringiensis against A. fraterculus larvae and adults. Bioassays were performed using suspensions of bacterial spores/crystals of B. thuringiensis var. israelensis (Bti), kurstaki (Btk), and oswaldocruzi (Bto) strains at three concentrations [2 × 107, 2 × 108, and 2 × 109 colony-forming units per ml (CFU ml-1)]. At a concentration of 2 × 109 CFU ml-1, a significant larval effect (mortality 60%) was observed when compared with the control treatment. Larvae that ingested spore/crystal suspensions of Bti, Btk, or Bto bacterial strains exhibited significant larval and pupal deformations, leading to a significant decrease (~50%) in the completion of the insects' biological cycle (egg to adult). The B. thuringiensis strains (Bti, Btk, or Bto) at a concentration of 2 × 109 CFU ml-1 in combination with one food attractant (BioAnastrepha 3% or CeraTrap 1.5%) in formulations of toxic baits provided high mortality (mortality > 85%) of A. fraterculus adults 7 d after treatment. However, the Btk strain in combination with CeraTrap 1.5% caused mortality of 40%. On the basis of these results, the native bacterial strains Bti, Btk, and Bto were considered to be promising candidates as biological control agents against A. fraterculus. © The Author(s) 2018. Published by Oxford University Press on behalf of Entomological Society of America. All rights reserved. For permissions, please e-mail: journals.permissions@oup.com.

  18. Selenylation Modification of Degraded Polysaccharide from Enteromorpha prolifera and Its Biological Activities

    Science.gov (United States)

    Lv, Haitao; Duan, Ke; Shan, Hu

    2018-04-01

    Polysaccharide extracted from Enteromorpha prolifera possessed excellent biological activities, but its molecular weight was greatly high which influenced the activity. Organic Se had higher biological activities and was safer than inorganic Se species. In the present study, Enteromorpha polysaccharide was degraded to low molecular weight by free-radical degradation method of H2O2 and ascorbic acid. By single factor and orthogonal experiments, the optimal degradation conditions were reaction time of 2 h, reaction temperature of 50°C, H2O2/ascorbic acid (n/n=1:1) concentration of 15 mmol L-1, and solid-liquid ratio of 1:50 (g mL-1). Then, the degraded polysaccharide was chemically modified to obtain its selenide derivatives by nitric acid-sodium selenite method. The selenium content was 1137.29 μg g-1, while the content of sulfate radical had no change. IR spectra indicated that the selenite ester group was formed. Degraded polysaccharide selenide was characterized and evaluated for antioxidant, antifungal and antibacterial activities. The results showed that degraded polysaccharide selenide had strong capacity of scavenging DPPH and ·OH free radical. It had significant antibacterial properties for Escherichia coli, Bacillus subtilis and Salmonella spp., and it also had significant antifungal properties for Apple anthrax. The result ascertained degradation and selenylation modification did not change the main structure of polysaccharides. It was possible that free-radical degradation was an effective way for enhancing antioxidant activity to decrease molecular weight of polysaccharides.

  19. Chemical and biological evaluation of rejects from the wood industry

    Directory of Open Access Journals (Sweden)

    Daniel Granato

    2005-06-01

    Full Text Available This study aimed chemical characterization and microbiological evaluation of extracts obtained from the waste of woods marketed in Paraná State: Peroba-Rosa (Aspidosperma sp., Roxinho (Peltogyne sp., Jatobá(Hymenaea sp., Curupixá (Micropholis sp., Itaúba (Mezilaurus sp., Cedrilho (Erisma sp. and Imbúia (Licaria sp., whose botanical identifications were based on anatomical studies. The extracts were prepared with different solvents, analyzed by TLC and UV/VIS techniques, and tested against: Proteus mirabilis ATCC15290, Staphylococcus aureus ATCC25923, Escherichia coli ATCC25922, Enterobacter aerogenes ATCC13048, Micrococcus luteus ATCC9341, Klebsiella pneumoniae ATCC13883, Pseudomonas aeroginosa ATCC27853, Staphylococcus aureus, Streptococcus mutans and Bacillus cereus isolated from the clinic. The ethanol extract from Peroba-rosa containing alkaloids showed activity against P. mirabilis. Itaúba, Jatobá and Imbúia methanol extracts containing phenolics, and the Roxinho ethyl acetate extract containing terpenoids and phenolics were active against K. pneumoniae, M. luteus, E. coli, S. aureus and P. mirabilis. P. aeroginosa, S. mutans and E. aerogenes were resistant to the extracts.Este estudo visa a caracterização química e a avaliação da atividade antimicrobiana de extratos obtidos a partir de rejeitos resultantes do beneficiamento de madeiras nobres comercializadas no Paraná: Peroba-Rosa (Aspidosperma sp., Roxinho (Peltogyne sp., Jatobá (Hymenaea sp., Curupixá (Micropholis sp., Itaúba (Mezilaurus sp., Cedrilho (Erisma sp. e Imbúia-do-Norte (Licaria sp., cujas identificações botânicas basearam-se em estudos anatômicos. Os extratos foram preparados com diversos solventes, analisados por CCD e espectrometria UV/VIS, testando-se contra: Proteus mirabilis ATCC15290, Escherichia coli ATCC25922, Enterobacter aerogenes ATCC13048, Staphylococcus aureus ATCC25923, Micrococcus luteus ATCC9341, Klebsiella pneumoniae ATCC13883

  20. Biological activity of Bt proteins expressed in different structures of transgenic corn against Spodoptera frugiperda

    OpenAIRE

    Bernardi, Daniel; Bernardi, Oderlei; Horikoshi, Renato Jun; Salmeron, Eloisa; Okuma, Daniela Miyuki; Omoto, Celso

    2016-01-01

    ABSTRACT: Spodoptera frugiperda (J. E. Smith) is the main target pest of Bt corn technologies, such as YieldGard VT PRO(tm) (Cry1A.105/Cry2Ab2) and PowerCore(tm) (Cry1A.105/Cry2Ab2/Cry1F). In this study, it was evaluated the biological activity of Bt proteins expressed in different plant structures of YieldGard VT PRO(tm) and PowerCore(tm) corn against S. frugiperda . Complete mortality of S. frugiperda neonates was observed on leaf-disc of both Bt corn technologies. However, the mortality ...

  1. Proteome profile and biological activity of caprine, bovine and human milk fat globules.

    Science.gov (United States)

    Spertino, Stefano; Cipriani, Valentina; De Angelis, Chiara; Giuffrida, Maria Gabriella; Marsano, Francesco; Cavaletto, Maria

    2012-04-01

    Upon combining bidimensional electrophoresis with monodimensional separation, a more comprehensive analysis of the milk fat globule membrane has been obtained. The proteomic profile of caprine milk fat globules revealed the presence of butyrophilin, lactadherin and perilipin as the major proteins, they were also associated to bovine and human milk fat globule membranes. Xanthine dehydrogenase/oxidase has been detected only in monodimensional gels. Biological activity of milk fat globules has been evaluated in Caco2-cells, as a representative model of the intestinal barrier. The increase of cell viability was indicative of a potential nutraceutical role for the whole milk fat globule, suggesting a possible employment in milk formula preparation.

  2. Vouacapane diterpenoids isolated from Pterodon and their biological activities

    Directory of Open Access Journals (Sweden)

    Leandra A.R. Oliveira

    Full Text Available Abstract The Pterodon genus comprises two native species in Brazil, known as “sucupira-branca” or “faveira”. Their fruits have long been used in Brazilian natural medicine, mainly for the treatment of infections and inflammations. The pharmacological properties of these fruits have often been linked with vouacapane diterpenoids. This review evaluated the scientific research in the period from 1973 to February 2017, aiming to answer how difficult it still is to develop a scientifically supported product based on Pterodon vouacapanes. Therefore, this paper reviews purification, identification, and quantification methods applied to vouacapane diterpenoids from Pterodon, as well as the performance of these phytochemicals in pharmacological tests described in the literature. Data analysis results support conventional notions that suggest vouacapane diterpenoids from Pterodon have anti-inflammatory properties. However, the studies carried out so far still represent partial assessment of the vouacapane activities and further studies need to be completed. Pterodon diterpenoids have also been associated with larvicidal, leishmanicidal, cardiovascular, and antitumor activities, which reinforces the genus' potential as a source of phytomedicines. Some remaining gaps about the reviewed activities were mentioned, while trends and perspectives for future research were proposed.

  3. Physicochemical properties and biological activities of Thai plant mucilages for artificial saliva preparation.

    Science.gov (United States)

    Manosroi, Aranya; Pattamapun, Kassara; Khositsuntiwong, Narinthorn; Kietthanakorn, Bang-on; Issarangporn, Witchapong; Chankhampan, Charinya; Manosroi, Worapaka; Manosroi, Jiradej

    2015-01-01

    Plant mucilages can be found in various parts of several Thai plants, which can be used as thickening, moisturizing, and lubricating agents in artificial saliva formulations. The objective of this study was to evaluate the physicochemical properties, biological activity, and cytotoxicity of Thai plant mucilages. The mucilages from Thai plants were extracted by various processes (temperature and pH variation, microwave oven, steam, and Tris-HCl buffer extraction). The viscosity and the rheology were evaluated using viscometer. Antioxidative activities including DPPH radical scavenging and metal chelating activities were investigated. The mucilages were determined for cytotoxicity on normal human gingival fibroblasts and anti-adherent activity of Streptococcus mutans. Mucilages from Ocimum citriodorum Vis. (Lamiaceae), Artocarpus heterophyllus Lam. (Moraceae), Abelmoschus esculentus (Linn.) Moench. (Malvaceae), and Basella alba Linn. (Basellaceae) exhibited pseudoplastic non-Newtonian rheology. The highest DPPH radical-scavenging and metal-chelating activities were observed in the mucilages from B. alba (microwave, 3 min) and A. esculentus (microwave, 1 min) with the SC50 and MC50 values (50% of scavenging activity and 50% of metal chelating activity, respectively) of 0.71 ± 0.32 and 1.11 ± 0.52 mg/ml, respectively. Most mucilages exhibited no cytotoxicity to normal human gingival fibroblasts. The mucilage from A. esculentus (microwave, 5 min) gave the shortest wetting time of 2.75 ± 0.51 min. The highest S. mutans adhesion inhibition was observed in A. esculentus (pH 11) of 5.39 ± 9.70%. This study has indicated the suitable physicochemical and biological properties and the potential application of mucilages from Thai plants for artificial saliva preparation.

  4. Chemical and biological evaluation of propolis of Alagoas

    OpenAIRE

    Gisele Rocha Aguiar

    2015-01-01

    The red propolis originally from the state of Alagoas has a chemical composition rich in isoflavones and has been used as traditional popular medicine presented as an antioxidant and antiviral properties. Its relevance to this study is mainly due to the same present several biological properties, among them: antimicrobial, anti-cancer, cytotoxic and anti-tumor. In this work it was performed the study of the fixed compounds present in hexane fraction of propolis, which presented three ester...

  5. Phytochemical Characterization and Biological Evaluation of the Aqueous and Supercritical Fluid Extracts from Salvia sclareoides Brot

    Directory of Open Access Journals (Sweden)

    Batista Daniela

    2017-04-01

    Full Text Available Plants belonging to the genus Salvia (Lamiaceae are known to have a wide range of biological properties. In this work, extracts obtained from the aerial parts of Salvia sclareoides Brot. were evaluated to investigate their chemical composition, toxicity, bioactivity, and stability under in vitro gastrointestinal conditions. The composition of the supercritical fluid extract was determined by GC and GC-MS, while the identification of the infusion constituents was performed by HPLC-DAD and LC-MS. The in vitro cytotoxicity of both extracts (0-2 mg/mL was evaluated in Caco-2 cell lines by the MTT assay. The anti-inflammatory and anticholinesterase activities were determined through the inhibition of cyclooxygenase-1 and acetylcholinesterase enzymes, while β-carotene/linoleic acid bleaching test and the DPPH assays were used to evaluate the antioxidant activity. The infusion inhibited cyclooxygenase-1 (IC50 = 271.0 μg/mL, and acetylcholinesterase (IC50 = 487.7 μg/ mL enzymes, also demonstrated significant antioxidant properties, as evaluated by the DPPH (IC50 = 10.4 μg/mL and β-carotene/linoleic acid (IC50 = 30.0 μg/mL assays. No remarkable alterations in the composition or in the bioactivities of the infusion were observed after in vitro digestion, which supports the potential of S. sclareoides as a source of bioactive ingredients with neuroprotective, anti-inflammatory and antioxidant properties.

  6. Production of biologically active recombinant human factor H in Physcomitrella.

    Science.gov (United States)

    Büttner-Mainik, Annette; Parsons, Juliana; Jérôme, Hanna; Hartmann, Andrea; Lamer, Stephanie; Schaaf, Andreas; Schlosser, Andreas; Zipfel, Peter F; Reski, Ralf; Decker, Eva L

    2011-04-01

    The human complement regulatory serum protein factor H (FH) is a promising future biopharmaceutical. Defects in the gene encoding FH are associated with human diseases like severe kidney and retinal disorders in the form of atypical haemolytic uremic syndrome (aHUS), membranoproliferative glomerulonephritis II (MPGN II) or age-related macular degeneration (AMD). There is a current need to apply intact full-length FH for the therapy of patients with congenital or acquired defects of this protein. Application of purified or recombinant FH (rFH) to these patients is an important and promising approach for the treatment of these diseases. However, neither protein purified from plasma of healthy individuals nor recombinant protein is currently available on the market. Here, we report the first stable expression of the full-length human FH cDNA and the subsequent production of this glycoprotein in a plant system. The moss Physcomitrella patens perfectly suits the requirements for the production of complex biopharmaceuticals as this eukaryotic system not only offers an outstanding genetical accessibility, but moreover, proteins can be produced safely in scalable photobioreactors without the need for animal-derived medium compounds. Transgenic moss lines were created, which express the human FH cDNA and target the recombinant protein to the culture supernatant via a moss-derived secretion signal. Correct processing of the signal peptide and integrity of the moss-produced rFH were verified via peptide mapping by mass spectrometry. Ultimately, we show that the rFH displays complement regulatory activity comparable to FH purified from plasma. © 2010 The Authors. Plant Biotechnology Journal © 2010 Society for Experimental Biology, Association of Applied Biologists and Blackwell Publishing Ltd.

  7. Quinoxaline 1, 4-di-N-oxides: Biological activities and mechanisms of actions

    Directory of Open Access Journals (Sweden)

    Guyue eCheng

    2016-03-01

    Full Text Available Quinoxaline 1, 4-di-N-oxides (QdNOs have manifold biological properties, including antimicrobial, antitumoral, antitrypanosomal and antiinflammatory/antioxidant activities. These diverse activities endow them broad applications and prospects in human and veterinary medicines. As QdNOs arouse widespread interest, the evaluation of their medicinal chemistry is still in progress. In the meantime, adverse effects have been reported in some of the QdNO derivatives. For example, genotoxicity and bacterial resistance have been found in QdNO antibacterial growth promoters, conferring urgent need for discovery of new QdNO drugs. However, the modes of actions of QdNOs are not fully understood, hindering the development and innovation of these promising compounds. Here, QdNOs are categorized based on the activities and usages, among which the antimicrobial activities are consist of antibacterial, antimycobacterial and anticandida activities, and the antiprotozoal activities include antitrypanosomal, antimalarial, antitrichomonas and antiamoebic activities. The structure-activity relationship and the mode of actions of each type of activity of QdNOs are summarized, and the toxicity and the underlying mechanisms are also discussed, providing insight for the future research and development of these fascinating compounds.

  8. Biological activities and DNA interactions of Amanita ovoidea.

    Science.gov (United States)

    Doğan, Hasan Hüseyin; Arslan, Emine

    2015-01-01

    Amanita ovoidea (Bull.) Link (Amanitaceae) is a well-known species due to its pleasant aroma and flavor since ancient times in the worldwide. This species is also known in Turkey and people consume it extensively. To evaluate medicinal importance of A. ovoidea for human health, to explain the effect of mushroom extracts on bacterial DNA, and to find preventive role on bacterial disease. Chloroform, acetone, and methanol extracts of A. ovoidea were tested for the antimicrobial activities against four Gram-positive bacteria, five Gram-negative bacteria, and yeast using a micro-dilution method. In addition, DNA binding, DNA cleavage activity, and restriction enzyme digestion of the methanol extract of A. ovoidea were examined at different concentrations (40.000-78.125 µg/mL). The highest minimum inhibitory concentration (MIC) value observed against the test micro-organisms was with the chloroform extract (MIC 19.5 µg/mL concentration) against Candida albicans. Other highest antimicrobial effects observed against the test micro-organisms were with the methanol extracts against Bacillus subtilis, Staphylococcus aureus, Listeria monocytogenes, Streptococcus pyogenes, Candida albicans, Klebsiella pneumoniae, Proteus vulgaris, and Salmonella enteritidis (MICs, 78 µg/mL concentrations). All concentrations reduced the mobility of plasmid DNA. BamHI and HindIII targeted specially to supercoils and cut them. Amanita ovoidea extract prevented cutting with HindIII by binding especially to the AA region in open circular DNA. Present results demonstrated that A. ovoidea has excellent antimicrobial and antifungal activities by its DNA interaction activity on pBR322.

  9. Synthesis and biological evaluation of coumarin derivatives containing imidazole skeleton as potential antibacterial agents.

    Science.gov (United States)

    Hu, Yang; Shen, Yufeng; Wu, Xiaohu; Tu, Xiao; Wang, Gao-Xue

    2018-01-01

    Emergence of multidrug-resistant bacteria causes an urgent need for new generation of antibiotics, which may have a different mechanism of inhibition or killing action from the existing. Here, we report on the design, synthesis, and biological evaluation of thirty-nine coumarin derivatives in order to solve the antibacterial resistance by targeting at the inhibition of biosynthesis pathway of fatty acids. Their antibacterial activities against Escherichia coli, Staphylococcus aureus, Streptococcus agalactiae, and Flavobacterium cloumnare are tested and action mechanism against the key enzyme in bacterial fatty acid synthesis pathway are studied. The results show that compounds 13 and 18 have potent and broad spectrum antimicrobial activity. In addition, 9, 14 and 19 show eminent antimicrobial efficacy toward S. aureus, S. agalactiae, and F. cloumnare. Mechanistically, coumarin derivatives display the antibacterial activity via the control of FabI and FabK function. The structure-activity relationship analysis indicate that the length of linker and imidazole substitute group could significantly influence the antimicrobial activity, as well as the inhibitory activity against FabI and FabK. The structural optimization analysis of coumarin suggest that derivatives 9, 13, 14, 18 and 19 could be a viable way of preventing and controlling bacteria and considered as promising lead compounds for the development of commercial drugs. Copyright © 2017 Elsevier Masson SAS. All rights reserved.

  10. Viability analysis in biological evaluations: Concepts of population viability analysis, biological population, and ecological scale

    Science.gov (United States)

    Gregory D. Hayward; John R. Squires

    1994-01-01

    Environmental protection strategies often rely on environmental impact assessments. As part of the assessment process biologists are routinely asked to evaluate the effects of management actions on plants and animals. This evaluation often requires that biologists make judgments about the viability of affected populations. However, population viability...

  11. Biological activity of Bt proteins expressed in different structures of transgenic corn against Spodoptera frugiperda

    Directory of Open Access Journals (Sweden)

    Daniel Bernardi

    2016-06-01

    Full Text Available ABSTRACT: Spodoptera frugiperda (J. E. Smith is the main target pest of Bt corn technologies, such as YieldGard VT PRO(tm (Cry1A.105/Cry2Ab2 and PowerCore(tm (Cry1A.105/Cry2Ab2/Cry1F. In this study, it was evaluated the biological activity of Bt proteins expressed in different plant structures of YieldGard VT PRO(tm and PowerCore(tm corn against S. frugiperda . Complete mortality of S. frugiperda neonates was observed on leaf-disc of both Bt corn technologies. However, the mortality in silks and grains was lower than 50 and 6%, respectively. In addition, more than 49% of the surviving larvae in silks and grains completed the biological cycle. However, all life table parameters were negatively affected in insects that developed in silks and grains of both Bt corn events. In summary, the low biological activity of Bt proteins expressed on silks and grains of YieldGard VT PRO(tm and PowerCore(tm corn can contribute to the resistance evolution in S. frugiperda populations.

  12. Characterization of biological macromolecules by electrophoresis and neutron activation

    International Nuclear Information System (INIS)

    Stone, S.F.; Hancock, D.; Zeisler, R.

    1987-01-01

    A procedure combining polyacrylamide gel electrophoresis (PAGE) with INAA and autoradiography was developed to study biological macromolecules and their associated trace elements. Results from the application of this method to several metalloproteins are presented. (author)

  13. Biological Treatment of tannery wastewater using activated sludge process

    International Nuclear Information System (INIS)

    Haydar, S.; Aziz, J.A.

    2007-01-01

    A study was conducted to evaluate the feasibility of Activated Sludge Process (ASP) for the treatment of tannery wastewater and to develop a simple design criteria under local conditions. A bench scale model comprising of an aeration tank and final clarifier was used for this purpose. The model was operated continuously for 267 days. Settled tannery wastewater was used as influent to the aeration tank. Five days Biochemical Oxygen Demand (BOD5) and Chemical Oxygen Demand (COD) of the influent and effluent were measured to find process efficiency at various mixed liquor volatile suspended solids (MLVSS) and hydraulic detention time. The results of the study demonstrated that an efficiency of above 90% and 80% for BOD5 and COD, respectively could be obtained if the ASP is operated at an MLVSS concentration of 3500 mg/L keeping an aeration time of 12 hours. (author)

  14. Accepting the Invitation to Open Innovation in Malaria Drug Discovery: Synthesis, Biological Evaluation, and Investigation on the Structure-Activity Relationships of Benzo[b]thiophene-2-carboxamides as Antimalarial Agents.

    Science.gov (United States)

    Pieroni, Marco; Azzali, Elisa; Basilico, Nicoletta; Parapini, Silvia; Zolkiewski, Michal; Beato, Claudia; Annunziato, Giannamaria; Bruno, Agostino; Vacondio, Federica; Costantino, Gabriele

    2017-03-09

    Malaria eradication is a global health priority, but current therapies are not always suitable for providing a radical cure. Artemisinin has paved the way for the current malaria treatment, the so-called Artemisinin-based Combination Therapy (ACT). However, with the detection of resistance to ACT, innovative compounds active against multiple parasite species and at multiple life stages are needed. GlaxoSmithKline has recently disclosed the results of a phenotypic screening of an internal library, publishing a collection of 400 antimalarial chemotypes, termed the "Malaria Box". After analysis of the data set, we have carried out a medicinal chemistry campaign in order to define the structure-activity relationships for one of the released compounds, which embodies a benzothiophene-2-carboxamide core. Thirty-five compounds were prepared, and a description of the structural features responsible for the in vitro activity against different strains of P. falciparum, the toxicity, and the metabolic stability is herein reported.

  15. Biology

    Indian Academy of Sciences (India)

    I am particularly happy that the Academy is bringing out this document by Professor M S. Valiathan on Ayurvedic Biology. It is an effort to place before the scientific community, especially that of India, the unique scientific opportunities that arise out of viewing Ayurveda from the perspective of contemporary science, its tools ...

  16. An Efficient Synthesis of 3,4-Dihydro-3-substituted-2H-naphtho[2,1-e][1,3]oxazine Derivatives Catalyzed by Zirconyl(IV) Chloride and Evaluation of its Biological Activities

    Energy Technology Data Exchange (ETDEWEB)

    Kategaonkar, Amol H.; Sonar, Swapnil S.; Pokalwar, Rajkumar U.; Shingate, Bapurao B.; Shingare, Murlidhar S. [Babasaheb Ambedkar Marathwada University, Maharashtra (India); Kategaonkar, Atul H. [Maharashtra Institute of Pharmacy, Maharashtra (India)

    2010-06-15

    An efficient and novel one-pot synthesis of new 3,4-dihydro-3-substituted-2H-naphtho[2,1-e][1,3]oxazine derivatives from 1-naphthol, various anilines and formalin at room temperature grinding is presented. The six-membered N,O-heterocyclic skeleton was constructed via zirconyl(IV) chloride promoted Mannich type reaction. In vitro antimicrobial activities of synthesized compounds have been investigated against Gram-positive Bacillus subtilis, Gram negative Escherichia coli and two fungi Candida albicans and Aspergillus niger in comparison with standard drugs. The results of preliminary bioassay indicate that some of title compounds possess significant antibacterial and antifungal activity.

  17. Chronological changes in baseline disease activity of patients with rheumatoid arthritis who received biologic DMARDs between 2003 and 2012.

    Science.gov (United States)

    Sato, Eri; Tanaka, Eiichi; Ochiai, Moeko; Shimizu, Yoko; Kobayashi, Akiko; Shidara, Kumi; Hoshi, Daisuke; Sugimoto, Naoki; Inoue, Eisuke; Seto, Yohei; Nakajima, Ayako; Taniguchi, Atsuo; Momohara, Shigeki; Yamanaka, Hisashi

    2015-05-01

    The use of biologic disease-modifying anti-rheumatic drugs (DMARDs) for rheumatoid arthritis (RA) has been increasing since 2003. In this study, we evaluated changes in the characteristics of patients receiving biologic DMARDs daily, in Japan. The characteristics of all RA patients who received any biologic DMARD at the Institute of Rheumatology, Tokyo Women's Medical University, within 1 year after its approval in Japan, were retrospectively evaluated. The periods of patient enrollment for each biologic agent were: infliximab (IFX), 2003-2004; etanercept (ETN), 2005-2006; tocilizumab (TCZ), 2008-2009; adalimumab (ADA), 2008-2009; abatacept (ABT), 2010-2011; and golimumab (GLM), 2011-2012. We retrospectively collected individual patient characteristics, concomitant medication usage, and disease activity assessed by disease activity score 28 (DAS28) at the time of administration, from the medical records. The retention rate for each agent at 6 months after treatment initiation was also assessed. The numbers of patients who received each biologic DMARD at our institute within 1 year after its approval were: IFX, 49; ETN, 50; TCZ, 62; ADA, 52; ABT, 40; and GLM, 77. From 2003 to 2012, the proportion of patients with prior use of any biologic DMARD increased, as did concomitant use and dose of methotrexate (MTX); however, corticosteroid use and doses decreased. DAS28, at the time of treatment initiation, gradually decreased. At the time of IFX administration, 75% and 25% of patients had high and moderate disease activity respectively, compared to 25% and 58% respectively, of patients who received GLM. No significant difference was observed in the retention rate of biologic DMARDs at 6 months (range, 75.0% to 89.6%). Baseline disease activity of RA patients who received biologic DMARDs between 2003 and 2012 has changed from high to moderate in daily practice in Japan.

  18. Removal of novel antiandrogens identified in biological effluents of domestic wastewater by activated carbon.

    Science.gov (United States)

    Ma, Dehua; Chen, Lujun; Liu, Rui

    2017-10-01

    Environmental antiandrogenic (AA) contaminants in effluents from wastewater treatment plants have the potential for negative impacts on wildlife and human health. The aim of our study was to identify chemical contaminants with likely AA activity in the biological effluents and evaluate the removal of these antiandrogens (AAs) during advanced treatment comprising adsorption onto granular activated carbon (GAC). In this study, profiling of AA contaminants in biological effluents and tertiary effluents was conducted using effect-directed analysis (EDA) including high performance liquid chromatography (HPLC) fractionation, a recombinant yeast screen containing androgen receptor (YAS), in combination with mass spectrometry analyses. Analysis of a wastewater secondary effluent from a membrane bioreactor revealed complex profiles of AA activity comprising 14 HPLC fractions and simpler profiles of GAC effluents with only 2 to 4 moderately polar HPLC fractions depending on GAC treatment conditions. Gas chromatography-mass spectrometry and ultra-high performance liquid chromatography-nanospray mass spectrometry analyses of AA fractions in the secondary effluent resulted in detection of over 10 chemical contaminants, which showed inhibition of YAS activity and were potential AAs. The putative AAs included biocides, food additives, flame retardants, pharmaceuticals and industrial contaminants. To our knowledge, it is the first time that the AA properties of N-ethyl-2-isopropyl-5-methylcyclohexanecarboxamide (WS3), cetirizine, and oxcarbazepine are reported. The EDA used in this study was proven to be a powerful tool to identify novel chemical structures with AA activity in the complex aquatic environment. The adsorption process to GAC of all the identified antiandrogens, except WS3 and triclosan, fit well with the pseudo-second order kinetics models. Adsorption to GAC could further remove most of the AAs identified in the biological effluents with high efficiencies. Copyright

  19. Phyto chemical and biological studies of certain plants with potential radioprotective activity

    International Nuclear Information System (INIS)

    Sherif, N.H.M.I

    2008-01-01

    One of the promising directions of radiation protection development is the search for natural radioprotective agents.The present work includes: I- Screening of certain edible and medicinal plants growing in Egypt for their radioprotective activities. II- Detailed phyto chemical and biolo-activity studies of the dried leaves of brassaia actinophylla endl. comprising: A-Phyto chemical screening and proximate analysis. B-Investigation of lipoidal matter. C- Isolation, characterization and structure elucidation of phenolic constituents. D- Isolation, characterization and structure elucidation of saponin constituents. E- Evaluation of radioprotective and antitumor activities. I- Evaluation of potential radioprotective activities of certain herbs: In vivo biological screening designed to investigate the radioprotective role of 70% ethanol extract of 11 different herbals was carried out by measuring the lipid peroxide content, as well as the activities of two antioxidant enzymes; viz glutathione, and superoxide dismutase in blood and liver tissues 1 and 7 days after radiation exposure. II : Phyto chemical and biolo-activity studies of the dried leaves of brassaia actinophylla Endl A : preliminary phyto chemical screening, determination and TLC examination of successive extractives. B : Investigation of lipoidal matter. GLC of unsaponifiable matter (USM)

  20. New hydrazones of ferulic acid: synthesis, characterization and biological activity.

    Science.gov (United States)

    Wolszleger, Maria; Stan, Cătălina Daniela; Apotrosoaei, Maria; Vasincu, Ioana; Pânzariu, Andreea; Profire, Lenuţa

    2014-01-01

    The ferulic acid (4-hydroxy-3-methoxy-cinnamic acid) is a phenolic compound with important antioxidant effects and which nowadays is being extensively studied for his potential indications in inflammatory and neurodegenerative diseases, hypertension, atherosclerosis, etc. The synthesis of new ferulic acid compounds with potential antioxidant activity. The synthesis of the designed compounds was performed in several steps: (i) the obtaining of ferulic acid chloride by reacting of ferulic acid with thionyl chloride; (ii) the reaction between the ferulic acid chloride and hydrazine hydrate 98% to obtain the ferulic acid hydrazide; (iii) the condensation of ferrulic acid hydrazide with various benzaldehydes (2-hydroxy/3-hydroxy/4-hydroxy/2-nitro/3-nitro/4-nitro/2-methoxi/ 4-chloro/4-fluoro/4-bromo-benzaldehyde) resulting the correspond- ing hydrazones. The structure of the synthesized compounds was confirmed by FT-IR spectroscopy and the evaluation of antioxidant potential was achieved by determining the total antioxidant capacity and reducing power. In this study new hydrazones of ferulic acid have been synthesized, physic-chemical and spectral characterized. The evaluation of antioxidant potential using in vitro methods showed the favorable influence of the structural modulation on the antioxidant effects of ferulic acid.

  1. Phytochemistry and biological activity of Spanish Citrus fruits.

    Science.gov (United States)

    Gironés-Vilaplana, Amadeo; Moreno, Diego A; García-Viguera, Cristina

    2014-04-01

    The evaluation of the potential inhibitory activity on α-glucosidase and pancreatic lipase by Citrus spp. fruits of Spanish origin (lemon, orange, grapefruit, lime, and mandarin) together with the evaluation of their phytochemical content and antioxidant capacity (DPPH˙, ORACFL, ABTS(+), FRAP and O2˙(-)) aiming for new applications of the fruits in nutrition and health was carried out. As far as we are aware, the presence of 3-O-caffeoylferuoylquinic acid and two hydrated feruloylquinic acids in orange and the presence of 3,5-diferuoylquinic acid in grapefruit have been reported for the first time. Although grapefruit showed higher contents of phytochemicals such as flavanones and vitamin C, lemon and lime showed higher potential for inhibitory effects on lipase, and lime also showed the best results for in vitro α-glucosidase inhibition. On the other hand, higher antioxidant capacity was reported for grapefruit, lemon and lime, which correlated well with their phytochemical composition. Based on the results, it could be concluded that Citrus fruits are of great value for nutrition and treatment of diet-related diseases such as obesity and diabetes, and consequently, a new field of interest in the food industry regarding new bioactive ingredients would be considered.

  2. Synthesis and biological evaluation of dihydropyrano-[2,3-c]pyrazoles as a new class of PPARγ partial agonists.

    Directory of Open Access Journals (Sweden)

    Katrine Qvortrup

    Full Text Available Peroxisome proliferator-activated receptor γ (PPARγ is a well-known target for thiazolidinedione antidiabetic drugs. In this paper, we present the synthesis and biological evaluation of a series of dihydropyrano[2,3-c]pyrazole derivatives as a novel family of PPARγ partial agonists. Two analogues were found to display high affinity for PPARγ with potencies in the micro molar range. Both of these hits were selective against PPARγ, since no activity was measured when tested against PPARα, PPARδ and RXRα. In addition, a novel modelling approach based on multiple individual flexible alignments was developed for the identification of ligand binding interactions in PPARγ. In combination with cell-based transactivation experiments, the flexible alignment model provides an excellent analytical tool to evaluate and visualize the effect of ligand chemical structure with respect to receptor binding mode and biological activity.

  3. Production of Some Biologically Active Secondary Metabolites From Marine-derived Fungus Varicosporina ramulosa

    Directory of Open Access Journals (Sweden)

    Atalla, M. M.

    2008-01-01

    Full Text Available In a screening of fungal isolates associated with marine algae collected from Abou-keer, Alexanderia during the four seasons of 2004, to obtain new biologically active compounds. Varicosporina ramulosa isolate was identified and selected as a producer of 13 compounds. Out of 13 pure compounds produced, compounds 3 and 10 were considered as antibacterial and antifungal compounds, respectively as they were active against gram positive, gram negative bacteria and a fungus. Optimization of conditions (fermentation media, incubation period, temperature, initial pH, aeration levels which activate compounds 3 and 10 production were studied. Also the spectral properties (UV, MS, GC/MS, IR and 1H-NMR of the purified compounds were determined. Compound 3 suggested to be dibutyl phthalate and compound 10 may be ergosterol or one of its isomers. Biological evaluation of the two compounds towards 6 different types of tumor cell lines showed weak effect of compound 3 at different concentrations on the viable cell count of the different tumor cell lines. While compound 10 showed different activities against the viable cell count of the 6 different tumor cell lines. It kills 50% of the viable infected liver and lung cells at concentrations equal to 99.7 µg/mL, 74.9µg/mL, respectively. Compound 10 can be recommended as new anticancer compounds.

  4. Comparison of growth methods and biological activities of brazilian marine Streptomyces

    Directory of Open Access Journals (Sweden)

    A. C. Granato

    2013-03-01

    Full Text Available The present work describes the study of the growth and the cytotoxic and antitumor activities of the extracts of the marine microorganisms Streptomyces acrymicini and Streptomyces cebimarensis, the latter a new strain. Both microorganisms were collected from coastal marine sediments of the north coast of São Paulo state. Growth was performed in a shaker and in a bioreactor using Gym medium and the broths of both microorganisms were extracted with ethyl acetate and n-butanol. Three extracts, two organic and one aqueous, from each microorganism were obtained and tested for cytotoxic and antitumor activity using the SF-295 (Central Nervous System, HCT-8 (Colon cell lines, and the MTT (3-(4,5-dimethylthiazol-2-yl-2,5-diphenyltetrazolium bromide method. The growth methods were compared and show that, although the shaker presented reasonable results, the bioreactor represents the best choice for growth of these microorganisms. The biological activity of the different extracts was evaluated and it was demonstrated that the growth methodology may influence the secondary metabolite production and the biological activity.

  5. Sifting abstracts from Medline and evaluating their relevance to molecular biology.

    Science.gov (United States)

    Grabar, Natalia; Jaulent, Marie-Christine; Chambaz, Antoine; Lefebvre, Céline; Néri, Christian

    2006-01-01

    The most important knowledge in the area of biology currently consists of raw text documents. Bibliographic databases of biomedical articles can be searched, but an efficient procedure should evaluate the relevance of documents to biology. In genetics, this challenge is even trickier, because of the lack of consistency in genes' naming tradition. We aim to define a good approach for collecting relevant abstracts for biology and for studied species and genes. Our approach relies on defining best queries, detecting and filtering best sources.

  6. Inorganic composition determination and evaluation of the biological activity of Peperomia pellucida in the Aspergillus flavus growth; Estudo da composicao inorganica e avaliacao da atividade biologica de Peperomia pellucida no crescimento de Aspergillus flavus

    Energy Technology Data Exchange (ETDEWEB)

    Sussa, Fabio Vitorio

    2011-07-01

    In recent decades, there has been a great advancement in research in developing drugs from plants. Nevertheless, little significant care exists in the literature about the stable concentration of elements, as well as the activity concentration of '2{sup 38}U and {sup 232}Th decay products in plants used for this purpose in Brazil. The presence of stable elements and radionuclides in plants constitutes the pathway for their migration to humans, via uptake of tea or remedies made with medicinal herbs. Peperomia pellucida, whose popular name is 'erva de jabuti', is a plant known by its medicinal usages, such as healing and analgesic properties plus antibacterial and antifungal activities against food fungi. In this study, the elemental composition of Peperomia pellucida and surrounding soil samples collected in the Botanical Garden in Rio de Janeiro was determined; the elemental concentration in the alcoholic extract and infusion processes of dry plants was also determined. The elemental concentration of As, Ba, Br, Ce, Co, Cr, Cs, Eu, Fe, Hf, K, La, Lu, Na, Nd, Rb, Sb, Sc, Sm, Ta, Tb, Th, U, Yb and Zn was determined in the leaves, aerial parts, including leaves, stems and roots of Peperomia pellucida, in their extracts obtained by maceration and infusions and in the surrounding soil by the Instrumental Neutron Activation Analysis (INAA). The analytical methodology used to determine the elements Cd, Hg and Pb was the Atomic Absorption Spectrometry (AAS); the activities of {sup 226}Ra, {sup 228}Ra and {sup 210}Pb were carried out by gross alpha and beta counting, after radiochemical separation. The quality of the obtained results was assured by the analyses of the certified reference materials IAEA-336 Lichen, IAEA-Soil-7, IAEA-326 Radionuclides in soil, NIST 1515 Apple Leaves and NIST 1542 Peach Leaves. The relative standard deviations and the relative errors obtained in these analyses indicated good precision and accuracy of the results. The essential

  7. Investigation of human exposure to triclocarban after showering, and preliminary evaluation of its biological effects

    Science.gov (United States)

    Schebb, Nils Helge; Inceoglu, Bora; Ahn, Ki Chang; Morisseau, Christophe; Gee, Shirley; Hammock, Bruce D.

    2012-01-01

    The antibacterial soap additive triclocarban (TCC) is widely used in personal care products. TCC has a high environmental persistence. We developed and validated a sensitive online solid phase extraction-LC-MS/MS method to rapidly analyze TCC and its major metabolites in urine and other biological samples to assess human exposure. We measured human urine concentrations 0–72 h after showering with a commercial bar soap containing 0.6% TCC. The major route of renal elimination was excretion as N-glucuronides. The absorption was estimated at 0.6% of the 70±15 mg TCC in the soap used. The TCC N-glucuronide urine concentration varied widely among the subjects and continuous daily use of the soap led to steady state levels of excretion. In order to assess potential biological effects arising from this exposure we screened TCC for the inhibition of human enzymes in vitro. We demonstrate that TCC is a potent inhibitor of the enzyme soluble epoxide hydrolase (sEH), whereas TCC′s major metabolites lack strong inhibitory activity. Topical administration of TCC at similar levels to rats in a preliminary in vivo study however failed to alter plasma biomarkers of sEH activity. Overall the analytical strategy described here revealed that use of TCC soap causes exposure levels that warrant further evaluation. PMID:21381656

  8. The synthesis, characterization and biological evaluation of a new nitric oxide donor agent

    Directory of Open Access Journals (Sweden)

    Profire Lenuta

    2014-01-01

    Full Text Available The synthesis of a new xanthine nitric oxide donor (TSP-81 has been discussed. The designed compound includes two structural moieties - theophylline (1,3-dimethylxanthine and acetaminophen (4-hydroxyacetanilide linked by the nitric oxide donor alkyl chain as a spacer. The compound has been characterized by microanalysis (CHN, 1H-NMR, 13C-NMR, FT-IR, UV-vis, TG and DTG. The thermal behaviour showed that TSP-81 melts with decomposition, in four steps, the most important ones being the 2nd one (the registered weight loss being 17.6 % and the 3rd one (with a registered weight loss of 30.4 %. The toxicity degree, the anti-inflammatory effect and the ability of releasing nitric oxide of the TSP-81 have also been evaluated. The biological assays established that TSP-81 exhibits enhanced biological properties such as lower toxicity and higher anti-inflammatory effect in reference with theophylline and acetaminophen, the drugs used as parents molecules. The TSP-81 is approximately 2 times more active than theophylline and 4 times more active than acetaminophen in reducing cotton pellet-granuloma formation. Furthermore, the release of nitric oxide (NO appears to have an important contribution to enhancing the anti-inflammatory effect.

  9. Synthesis and Biological Evaluation of Some Novel Dithiocarbamate Derivatives

    Directory of Open Access Journals (Sweden)

    Begüm Nurpelin Sağlık

    2014-01-01

    Full Text Available 18 novel dithiocarbamate derivatives were synthesized in order to investigate their inhibitory potency on acetylcholinesterase enzyme and antimicrobial activity. Structures of the synthesized compounds were elucidated by spectral data and elemental analyses. The synthesized compounds showed low enzyme inhibitory activity. However, they displayed good antimicrobial activity profile. Antibacterial activity of compounds 4a, 4e, and 4p (MIC = 25 μg/mL was equal to that of chloramphenicol against Klebsiella pneumoniae (ATCC 700603 and Escherichia coli (ATCC 35218. Most of the compounds exhibited notable antifungal activity against Candida albicans (ATCC 10231, Candida glabrata (ATCC 90030, Candida krusei (ATCC 6258, and Candida parapsilosis (ATCC 7330. Moreover, compound 4a, which carries piperidin-1-yl substituent and dimethylthiocarbamoyl side chain as variable group, showed twofold better anticandidal effect against all Candida species than reference drug ketoconazole.

  10. Systems Biology Graphical Notation: Activity Flow language Level 1 Version 1.2.

    Science.gov (United States)

    Mi, Huaiyu; Schreiber, Falk; Moodie, Stuart; Czauderna, Tobias; Demir, Emek; Haw, Robin; Luna, Augustin; Le Novère, Nicolas; Sorokin, Anatoly; Villéger, Alice

    2015-09-04

    The Systems Biological Graphical Notation (SBGN) is an international community effort for standardized graphical representations of biological pathways and networks. The goal of SBGN is to provide unambiguous pathway and network maps for readers with different scientific backgrounds as well as to support efficient and accurate exchange of biological knowledge between different research communities, industry, and other players in systems biology. Three SBGN languages, Process Description (PD), Entity Relationship (ER) and Activity Flow (AF), allow for the representation of different aspects of biological and biochemical systems at different levels of detail. The SBGN Activity Flow language represents the influences of activities among various entities within a network. Unlike SBGN PD and ER that focus on the entities and their relationships with others, SBGN AF puts the emphasis on the functions (or activities) performed by the entities, and their effects to the functions of the same or other entities. The nodes (elements) describe the biological activities of the entities, such as protein kinase activity, binding activity or receptor activity, which can be easily mapped to Gene Ontology molecular function terms. The edges (connections) provide descriptions of relationships (or influences) between the activities, e.g., positive influence and negative influence. Among all three languages of SBGN, AF is the closest to signaling pathways in biological literature and textbooks, but its well-defined semantics offer a superior precision in expressing biological knowledge.

  11. Polysaccharides from Traditional Chinese Medicines: Extraction, Purification, Modification, and Biological Activity.

    Science.gov (United States)

    Chen, Yun; Yao, Fangke; Ming, Ke; Wang, Deyun; Hu, Yuanliang; Liu, Jiaguo

    2016-12-13

    Traditional Chinese Medicine (TCM) has been used to treat diseases in China for thousands of years. TCM compositions are complex, using as their various sources plants, animals, fungi, and minerals. Polysaccharides are one of the active and important ingredients of TCMs. Polysaccharides from TCMs exhibit a wide range of biological activities in terms of immunity- modifying, antiviral, anti-inflammatory, anti-oxidative, and anti-tumor properties. With their widespread biological activities, polysaccharides consistently attract scientist's interests, and the studies often concentrate on the extraction, purification, and biological activity of TCM polysaccharides. Currently, numerous studies have shown that the modification of polysaccharides can heighten or change the biological activities, which is a new angle of polysaccharide research. This review highlights the current knowledge of TCM polysaccharides, including their extraction, purification, modification, and biological activity, which will hopefully provide profound insights facilitating further research and development.

  12. Development of methods for evaluating active faults

    International Nuclear Information System (INIS)

    2013-01-01

    The report for long-term evaluation of active faults was published by the Headquarters for Earthquake Research Promotion on Nov. 2010. After occurrence of the 2011 Tohoku-oki earthquake, the safety review guide with regard to geology and ground of site was revised by the Nuclear Safety Commission on Mar. 2012 with scientific knowledges of the earthquake. The Nuclear Regulation Authority established on Sep. 2012 is newly planning the New Safety Design Standard related to Earthquakes and Tsunamis of Light Water Nuclear Power Reactor Facilities. With respect to those guides and standards, our investigations for developing the methods of evaluating active faults are as follows; (1) For better evaluation on activities of offshore fault, we proposed a work flow to date marine terrace (indicator for offshore fault activity) during the last 400,000 years. We also developed the analysis of fault-related fold for evaluating of blind fault. (2) To clarify the activities of active faults without superstratum, we carried out the color analysis of fault gouge and divided the activities into thousand of years and tens of thousands. (3) To reduce uncertainties of fault activities and frequency of earthquakes, we compiled the survey data and possible errors. (4) For improving seismic hazard analysis, we compiled the fault activities of the Yunotake and Itozawa faults, induced by the 2011 Tohoku-oki earthquake. (author)

  13. Evaluation and Verification of a Biological Shield in a SHARS Unit

    Energy Technology Data Exchange (ETDEWEB)

    Dhlomo, S.V.; Swart, H.S. [Compliance Management Department, Nuclear Liabilities Management, South African Nuclear Energy Corporation, P.O. Box 582, Pretoria 0001 (South Africa)

    2008-07-01

    The International Atomic Energy Agency (IAEA) Waste Technology Section with additional support from the U.S. National Nuclear Security Agency (NNSA) through the IAEA Nuclear Security Fund has funded the design, fabrication, evaluation, and testing of a portable hot cell intended to address the problem of disused SHARS in obsolete irradiation devices such as teletherapy heads and dry irradiators. This unit, designed and manufactured by the South African Nuclear Energy Corporation (Necsa), can be assembled, disassembled and packed inside two ISO containers and transported to the desired destination with relative ease. The unit was also licensed by the South African Regulator, the Department of Health (DoH), Directorate Radiation Control. This facility is used for the recovery and conditioning of orphaned/ abandoned or spent high activity radioactive sources from teletherapy units, gamma irradiators, and brachytherapy units. The hot cell was designed for a 3,7 E+13 Bq (1000 Ci) activity although it was demonstrated that it can handle activities of more than 7,4 E+13 Bq (2000 Ci) with ease. The biological shield of the SHARS facility consists of river sand sandwiched between metal plates, and a viewing window filled with a 50% zinc bromide solution. The shielding effectiveness of the river sand is evaluated experimentally by determining its density. The experimentally measured dose rates are compared to the dose rates estimated by computational codes. (authors)

  14. Evaluation and Verification of a Biological Shield in a SHARS Unit

    International Nuclear Information System (INIS)

    Dhlomo, S.V.; Swart, H.S.

    2008-01-01

    The International Atomic Energy Agency (IAEA) Waste Technology Section with additional support from the U.S. National Nuclear Security Agency (NNSA) through the IAEA Nuclear Security Fund has funded the design, fabrication, evaluation, and testing of a portable hot cell intended to address the problem of disused SHARS in obsolete irradiation devices such as teletherapy heads and dry irradiators. This unit, designed and manufactured by the South African Nuclear Energy Corporation (Necsa), can be assembled, disassembled and packed inside two ISO containers and transported to the desired destination with relative ease. The unit was also licensed by the South African Regulator, the Department of Health (DoH), Directorate Radiation Control. This facility is used for the recovery and conditioning of orphaned/ abandoned or spent high activity radioactive sources from teletherapy units, gamma irradiators, and brachytherapy units. The hot cell was designed for a 3,7 E+13 Bq (1000 Ci) activity although it was demonstrated that it can handle activities of more than 7,4 E+13 Bq (2000 Ci) with ease. The biological shield of the SHARS facility consists of river sand sandwiched between metal plates, and a viewing window filled with a 50% zinc bromide solution. The shielding effectiveness of the river sand is evaluated experimentally by determining its density. The experimentally measured dose rates are compared to the dose rates estimated by computational codes. (authors)

  15. Inhibition of survivin influences the biological activities of canine histiocytic sarcoma cell lines.

    Directory of Open Access Journals (Sweden)

    Hiroki Yamazaki

    Full Text Available Canine histiocytic sarcoma (CHS is an aggressive malignant neoplasm that originates from histiocytic lineage cells, including dendritic cells and macrophages, and is characterized by progressive local infiltration and a very high metastatic potential. Survivin is as an apoptotic inhibitory factor that has major functions in cell proliferation, including inhibition of apoptosis and regulation of cell division, and is expressed in most types of human and canine malignant neoplasms, including melanoma and osteosarcoma. To investigate whether survivin was expressed at high levels in CHS and whether its expression was correlated with the aggressive biological behavior of CHS, we assessed relation between survivin expression and CHS progression, as well as the effects of survivin inhibition on the biological activities of CHS cells. We comparatively analyzed the expression of 6 selected anti-apoptotic genes, including survivin, in specimens from 30 dogs with histiocytic sarcoma and performed annexin V staining to evaluate apoptosis, methylthiazole tetrazolium assays to assess cell viability and chemosensitivity, and latex bead assays to measure changes in phagocytic activities in 4 CHS cell lines and normal canine fibroblasts transfected with survivin siRNA. Survivin gene expression levels in 30 specimens were significantly higher than those of the other 6 genes. After transfection with survivin siRNA, apoptosis, cell growth inhibition, enhanced chemosensitivity, and weakened phagocytic activities were observed in all CHS cell lines. In contrast, normal canine fibroblasts were not significantly affected by survivin knockdown. These results suggested that survivin expression may mediate the aggressive biological activities of CHS and that survivin may be an effective therapeutic target for the treatment of CHS.

  16. Citrus limon from Tunisia: Phytochemical and Physicochemical Properties and Biological Activities

    Directory of Open Access Journals (Sweden)

    Mohamed Makni

    2018-01-01

    Full Text Available Natural plant extracts contain a variety of phenolic compounds which are assigned various biological activities. Our work aims to make a quantitative and qualitative characterization of the Zest (ZL and the Flesh (FL of lemon (Citrus limon, to valorize the pharmacological uses of lemon, by evaluating in vitro activities (DPPH, free radical scavenging and reducing power. The antibacterial, antifungal, and antiproliferative activities were sought in the ability of Citrus limon extracts to protect DNA and protein. We found that the ZL contains high amounts of phenolics responsible for the important antioxidant properties of the extract. However, the FL is richer in flavonoids than the ZL. The FL extract was also found to be more effective than the ZL in protecting plasmid DNA against the strand breakage induced by hydroxyl radicals. We also concluded that the FL extract exhibited potent antibacterial activity unlike ZL. Analysis by LC/MS-MS identified 6 compounds (Caffeoyl N-Tryptophan, Hydroxycinnamoyl-Oglucoside acid, Vicenin 2, Eriocitrin, Kaempferol-3-O- rutinoside, and Quercetin-3-rutinoside. These preliminary results showed that Citrus limon has antibacterial and antioxidant activity in vitro. It would be interesting to conduct further studies to evaluate the in vivo potential in an animal model.

  17. Citrus limon from Tunisia: Phytochemical and Physicochemical Properties and Biological Activities.

    Science.gov (United States)

    Makni, Mohamed; Jemai, Raoua; Kriaa, Walid; Chtourou, Yassine; Fetoui, Hamadi

    2018-01-01

    Natural plant extracts contain a variety of phenolic compounds which are assigned various biological activities. Our work aims to make a quantitative and qualitative characterization of the Zest (ZL) and the Flesh (FL) of lemon (Citrus limon) , to valorize the pharmacological uses of lemon, by evaluating in vitro activities (DPPH, free radical scavenging and reducing power). The antibacterial, antifungal, and antiproliferative activities were sought in the ability of Citrus limon extracts to protect DNA and protein. We found that the ZL contains high amounts of phenolics responsible for the important antioxidant properties of the extract. However, the FL is richer in flavonoids than the ZL. The FL extract was also found to be more effective than the ZL in protecting plasmid DNA against the strand breakage induced by hydroxyl radicals. We also concluded that the FL extract exhibited potent antibacterial activity unlike ZL. Analysis by LC/MS-MS identified 6 compounds (Caffeoyl N-Tryptophan, Hydroxycinnamoyl-Oglucoside acid, Vicenin 2, Eriocitrin, Kaempferol-3-O- rutinoside, and Quercetin-3-rutinoside). These preliminary results showed that Citrus limon has antibacterial and antioxidant activity in vitro . It would be interesting to conduct further studies to evaluate the in vivo potential in an animal model.

  18. Activities in biological radiation research at the AGF

    International Nuclear Information System (INIS)

    1984-01-01

    The AGF is working on a wide spectrum of biological radiation research, with the different scientific disciplines contributing different methodologies to long-term research projects. The following fields are studied: 1. Molecular and cellular modes of action of radiation. 2. Detection and characterisation of biological radiation damage, especially in humans. 3. Medical applications of radiation effects. 4. Concepts and methods of radiation protection. The studies will lead to suggestions for radiation protection and improved radiotherapy. They may also contribute to the development of environmental protection strategies. (orig./MG) [de

  19. Synthesis and Biological Activity of Substituted Urea and Thiourea Derivatives Containing 1,2,4-Triazole Moieties

    Science.gov (United States)

    2013-03-19

    Biological Activity of Substituted Urea and Thiourea Derivatives Containing 1,2,4- Triazole Moieties Bedia Kocyigit-Kaymakcioglu 1,*, Ahmet Ozgur Celen...of novel thiourea and urea derivatives containing 1,2,4- triazole moieties were synthesized and evaluated for their antifungal and larvicidal activity... Triazole derivatives 3a–e and 4a–e were synthesized by reacting thiocarbohydrazide with thiourea and urea compounds 1a–e and 2a–e, respectively

  20. Amidine Sulfonamides and Benzene Sulfonamides: Synthesis and Their Biological Evaluation

    OpenAIRE

    Muhammad Abdul Qadir; Mahmood Ahmed; Hina Aslam; Sadia Waseem; Muhammad Imtiaz Shafiq

    2015-01-01

    New amidine and benzene sulfonamide derivatives were developed and structures of the new products were confirmed by elemental and spectral analysis (FT-IR, ESI-MS, 1HNMR, and 13CNMR). In vitro, developed compounds were screened for their antibacterial and antifungal activities against medically important bacterial strains, namely, S. aureus, B. subtilis, and E. coli, and fungi, namely, A. flavus, A. parasiticus, and A. sp. The antibacterial and antifungal activities have been determined by me...