WorldWideScience

Sample records for natural product chios

  1. Chios mastic, a natural supplement for zinc to enhance male sexuality and prostate function.

    Science.gov (United States)

    Sawidis, Thomas; Yurukova, Lilyana; Askitis, Thanos

    2010-01-01

    Mastic is a natural resin extracted from the stem of the evergreen tree Pistacia lentiscus var. Chia (Duham) (Anacardiaceae). For a long time, mastic has been esteemed for its aphrodisiac properties. To test this hypothesis, the trace element zinc was determined while the quantity released after a certain time of chewing was studied. For comparison, three commercial chewing-gums were analyzed as well. A portion of natural mastic or commercial gum was uniformly chewed for 1, 2, 3, and 4 h and the zinc content measured. The zinc content of mastic from P. lentiscus var. Chia was compared to that of other natural resins from the same genus (Pistacia terebinthus L.) or conifer [Pinus halepensis Mill. (Pinaceae)], having a different secretion mechanism and also used as an additive in human nutrition. Secreted resin and plant tissues from the above trees were sampled and the zinc content was determined. Zinc concentrations in the resin were lower than in the plant tissues. The Chios mastic showed a slightly greater zinc content compared to the other analyzed specimens. Among all gums studied, only the Chios mastic released a small amount of about 0.7 mg kg(-1) zinc in the mouth and gastrointestinal system after 4 h chewing time. With commercial gums, the zinc content increased to a large degree (up to 2 mg kg(-1)) after the same treatment, a fact which was attributed to the zinc uptake from salivary secretions, indicating zinc deprivation for the human organism.

  2. Anti-inflammatory activity of Chios mastic gum is associated with inhibition of TNF-alpha induced oxidative stress

    Directory of Open Access Journals (Sweden)

    Lerakis Stamatios

    2011-06-01

    Full Text Available Abstract Background Gum of Chios mastic (Pistacia lentiscus var. chia is a natural antimicrobial agent that has found extensive use in pharmaceutical products and as a nutritional supplement. The molecular mechanisms of its anti-inflammatory activity, however, are not clear. In this work, the potential role of antioxidant activity of Chios mastic gum has been evaluated. Methods Scavenging of superoxide radical was investigated by electron spin resonance and spin trapping technique using EMPO spin trap in xanthine oxidase system. Superoxide production in endothelial and smooth muscle cells stimulated with TNF-α or angiotensin II and treated with vehicle (DMSO or mastic gum (0.1-10 μg/ml was measured by DHE and HPLC. Cellular H2O2 was measured by Amplex Red. Inhibition of protein kinase C (PKC with mastic gum was determined by the decrease of purified PKC activity, by inhibition of PKC activity in cellular homogenate and by attenuation of superoxide production in cells treated with PKC activator phorbol 12-myristate 13-acetate (PMA. Results Spin trapping study did not show significant scavenging of superoxide by mastic gum itself. However, mastic gum inhibited cellular production of superoxide and H2O2 in dose dependent manner in TNF-α treated rat aortic smooth muscle cells but did not affect unstimulated cells. TNF-α significantly increased the cellular superoxide production by NADPH oxidase, while mastic gum completely abolished this stimulation. Mastic gum inhibited the activity of purified PKC, decreased PKC activity in cell homogenate, and attenuated superoxide production in cells stimulated with PKC activator PMA and PKC-dependent angiotensin II in endothelial cells. Conclusion We suggest that mastic gum inhibits PKC which attenuates production of superoxide and H2O2 by NADPH oxidases. This antioxidant property may have direct implication to the anti-inflammatory activity of the Chios mastic gum.

  3. 1881 and 1949 earthquakes at the Chios-Cesme Strait (Aegean Sea and their relation to tsunamis

    Directory of Open Access Journals (Sweden)

    Y. Altinok

    2005-01-01

    Full Text Available The most earthquake-prone areas in the eastern central Aegean Sea are the Izmir Bay, the Karaburun peninsula and the island of Chios. The level of seismic activity and tsunami potential are influenced by the presence of normal faults around the region. There have been about 20 moderate-size earthquakes from 496 BC to 1949 AD. Among these earthquakes, the ones on the dates 20 March 1389, 13 November 1856, 19/22 January 1866, 3 April 1881 and 23 July 1949 produced tsunamis. The Chios-Cesme earthquake (1881, Mw 6.5 took place in the South of the Cesme strait while the Chios-Karaburun earthquake (1949, Mw 6.7 occurred in the North. The tsunamis caused by the earthquakes affected the coasts of Chios Island and Cesme. These waves are thought to be associated with the earthquakes and co-seismic underwater failures possibly occurred along the coasts of the Chios Island and Karaburun Peninsula or on the complex subaqueous morphology between these lands. Some sea waves or oscillations observed following the aftershocks are believed to be related to other natural phenomena; e.g. the seiches occurred mainly in open-narrow bays as triggered by the earthquakes.

  4. Beneficial health effects of Chios Gum Mastic and peroxisome proliferator-activated receptors: indications of common mechanisms.

    Science.gov (United States)

    Georgiadis, Ioannis; Karatzas, Theodore; Korou, Laskarina-Maria; Katsilambros, Nikolaos; Perrea, Despina

    2015-01-01

    For thousands of years, Chios Gum Mastic (CGM), the resin produced by the trunk of Pistachia lentiscus var Chia, has been used for culinary and medicinal purposes and several therapeutic properties have been attributed to it. CGM has been used in traditional medicine of various nations in the eastern Mediterranean area. This survey was carried out to identify biological mechanisms that could explain traditional usage and recent pharmacological findings. We reviewed the related scientific literature available from the NCBI PUBMED database on CGM studies and on natural products showing peroxisome proliferator-activated receptor (PPAR) agonist effects. We investigated whether CGM qualifies as a PPAR modulator. A large number of studies demonstrate that CGM has antioxidant, anti-inflammatory, hypolipidemic, and anticancer properties. Recently, the first evidence of CGM antidiabetic effect became known. CGM chemical composition has been extensively analyzed and the presence of several compounds, especially triterpenoids is well documented. Some of them, oleanonic acid, oleanolic acid, and gallic acid are considered to act as PPAR modulators. PPARs are nuclear receptors functioning as transcription factors and thereby controlling cellular functions at the level of gene expression. PPARs are involved in the pathways of significant diseases, such as metabolic syndrome, diabetes mellitus, dyslipidemia, inflammation, atheromatosis, and neoplasias, constituting a key target for pharmacological interventions. This article proposes that the synergistic action of some constituents of CGM on PPARs and more precisely on both PPARs isotypes-α and -γ, may be one of the major biological mechanisms via which CGM exerts its multiple effects.

  5. Pharmacophore-driven identification of PPARγ agonists from natural sources

    DEFF Research Database (Denmark)

    Petersen, R. K.; Christensen, Kathrine Bisgaard; Assimopoulou, A. N.

    2011-01-01

    In a search for more effective and safe anti-diabetic compounds, we developed a pharmacophore model based on partial agonists of PPARγ. The model was used for the virtual screening of the Chinese Natural Product Database (CNPD), a library of plant-derived natural products primarily used in folk...... medicine. From the resulting hits, we selected methyl oleanonate, a compound found, among others, in Pistacia lentiscus var. Chia oleoresin (Chios mastic gum). The acid of methyl oleanonate, oleanonic acid, was identified as a PPARγ agonist through bioassay-guided chromatographic fractionations of Chios...... mastic gum fractions, whereas some other sub-fractions exhibited also biological activity towards PPARγ. The results from the present work are two-fold: on the one hand we demonstrate that the pharmacophore model we developed is able to select novel ligand scaffolds that act as PPARγ agonists; while...

  6. Antiplasmodial Natural Products

    Directory of Open Access Journals (Sweden)

    Cláudio R. Nogueira

    2011-03-01

    Full Text Available Malaria is a human infectious disease that is caused by four species of Plasmodium. It is responsible for more than 1 million deaths per year. Natural products contain a great variety of chemical structures and have been screened for antiplasmodial activity as potential sources of new antimalarial drugs. This review highlights studies on natural products with antimalarial and antiplasmodial activity reported in the literature from January 2009 to November 2010. A total of 360 antiplasmodial natural products comprised of terpenes, including iridoids, sesquiterpenes, diterpenes, terpenoid benzoquinones, steroids, quassinoids, limonoids, curcubitacins, and lanostanes; flavonoids; alkaloids; peptides; phenylalkanoids; xanthones; naphthopyrones; polyketides, including halenaquinones, peroxides, polyacetylenes, and resorcylic acids; depsidones; benzophenones; macrolides; and miscellaneous compounds, including halogenated compounds and chromenes are listed in this review.

  7. Review: Chios mastic gum: a plant-produced resin exhibiting numerous diverse pharmaceutical and biomedical properties.

    Science.gov (United States)

    Dimas, Konstantinos S; Pantazis, Panayotis; Ramanujam, Rama

    2012-01-01

    Chios mastic gum (CMG) is a resin produced by the plant Pistacia lentiscus var. chia. CMG is used to extract the mastic gum essential oil (MGO). CMG and MGO consist of nearly 70 constituents and have demonstrated numerous and diverse biomedical and pharmacological properties including (a) eradication of bacteria and fungi that may cause peptic ulcers, tooth plaque formation and malodor of the mouth and saliva; (b) amelioration or dramatic reduction of symptoms of autoimmune diseases by inhibiting production of pro-inflammatory substances by activated macrophages, production of cytokines by peripheral blood mononuclear cells in patients with active Crohn's disease, and suppression of production of inflammatory cytokines and chemokines in an asthma model in mice; (c) protection of the cardiovascular system by effectively lowering the levels of total serum cholesterol, low-density lipoprotein and triglycerides in rats, and protection of low-density lipoprotein from oxidation in humans; (d) induction of apoptosis in human cancer cells in vitro and extensive inhibition of growth of human tumors xenografted in immunodeficient mice; and (e) improvement of symptoms in patients with functional dyspepsia. Collectively taken, these numerous and diverse medical and pharmaceutical properties of CMG and MGO warrant further research in an effort to enhance specific properties and identify specific constituent(s) that might be associated with each property.

  8. Natural Products for Antithrombosis

    Directory of Open Access Journals (Sweden)

    Cen Chen

    2015-01-01

    Full Text Available Thrombosis is considered to be closely related to several diseases such as atherosclerosis, ischemic heart disease and stroke, as well as rheumatoid arthritis, hyperuricemia, and various inflammatory conditions. More and more studies have been focused on understanding the mechanism of molecular and cellular basis of thrombus formation as well as preventing thrombosis for the treatment of thrombotic diseases. In reality, there is considerable interest in the role of natural products and their bioactive components in the prevention and treatment of thrombosis related disorders. This paper briefly describes the mechanisms of thrombus formation on three aspects, including coagulation system, platelet activation, and aggregation, and change of blood flow conditions. Furthermore, the natural products for antithrombosis by anticoagulation, antiplatelet aggregation, and fibrinolysis were summarized, respectively.

  9. Quality profile determination of Chios mastic gum essential oil and detection of adulteration in mastic oil products with the application of chiral and non-chiral GC-MS analysis.

    Science.gov (United States)

    Paraschos, Sotirios; Magiatis, Prokopios; Gikas, Evagelos; Smyrnioudis, Ilias; Skaltsounis, Alexios-Leandros

    2016-10-01

    The determination of mastic oil profile, with emphasis on its chiral characteristics, could serve as a method for detecting adulteration in products found in the market with a claim of mastic oil content aiming towards protecting it from counterfeiting. Furthermore the evaluation of the raw material is crucial, as the profile is potentially affected by factors as mastic origin and storage time. Thus 45 authentic mastic oil samples were analyzed by GC-MS employing a chiral column and content limits for all major constituents were determined. The chiral GC-MS analysis proved that selected concentration ratios between these constituents, namely those of (-)/(+)-α-pinene (≤1:100) and (-)-α-pinene/myrcene (1.9:100-11:100) could serve as markers for the determination of mastic oil authenticity. Employing this methodology, the analysis of 25 mastic oils contained in cosmetic and dietary products, as well as an artificial mastic oil sample, exhibited several differentiations that could indicate adulteration either with artificial essential oils or volatile compounds, or the use of aged mastic oil. Copyright © 2016 Elsevier B.V. All rights reserved.

  10. Sources of variation and genetic profile of spontaneous, out-of-season ovulatory activity in the Chios sheep

    Directory of Open Access Journals (Sweden)

    Kouttos Athanasios

    2003-01-01

    Full Text Available Abstract Organising the breeding plan of a seasonally breeding species, such as sheep, presents a challenge to farmers and the industry as a whole, since both economical and biological considerations need to be carefully balanced. Understanding the breeding activity of individual animals becomes a prerequisite for a successful breeding program. This study set out to investigate the sources of variation and the genetic profile of the spontaneous, out-of-season ovulatory activity of ewes of the Chios dairy sheep breed in Greece. The definition of the trait was based on blood progesterone levels, measured before exposing the ewes to rams, which marks the onset of the usual breeding season. Data were 707 records, taken over two consecutive years, of 435 ewes kept at the Agricultural Research Station of Chalkidiki in northern Greece. When all available pedigree was included, the total number of animals involved was 1068. On average, 29% of all ewes exhibited spontaneous, out-of-season ovulatory activity, with no substantial variation between the years. Significant sources of systematic variation were the ewe age and live weight, and the month of previous lambing. Older, heavier ewes, that had lambed early the previous autumn, exhibited more frequent activity. Heritability estimates were 0.216 (± 0.084 with a linear and 0.291 with a threshold model. The latter better accounts for the categorical nature of the trait. The linear model repeatability was 0.230 (± 0.095. The results obtained in this study support the notion that spontaneous out-of-season ovulatory activity can be considered in the development of a breeding plan for the Chios sheep breed.

  11. Marine Natural Products Against Tuberculosis

    Directory of Open Access Journals (Sweden)

    Marcus Vinícius Nora De Souza

    2006-01-01

    Full Text Available Natural products represent an outstanding source of compounds that play an important role in the treatment of human diseases. Due to the importance of nature as a source of new drug candidates, the aim of this review is to highlight the marine natural products, which exhibit antituberculosis activity, discovered between 2000 and 2005.

  12. Modulation of CYP1A1 and CYP1A2 hepatic enzymes after oral administration of Chios mastic gum to male Wistar rats.

    Science.gov (United States)

    Katsanou, Efrosini S; Kyriakopoulou, Katerina; Emmanouil, Christina; Fokialakis, Nikolas; Skaltsounis, Alexios-Leandros; Machera, Kyriaki

    2014-01-01

    Chios mastic gum (CMG), a resin derived from Pistacia lentiscus var. chia, is known since ancient times for its pharmacological activities. CYP1A1 and CYP1A2 enzymes are among the most involved in the biotransformation of chemicals and the metabolic activation of pro-carcinogens. Previous studies referring to the modulation of these enzymes by CMG have revealed findings of unclear biological and toxicological significance. For this purpose, the modulation of CYP1A1 and CYP1A2 enzymes in the liver of male Wistar rats following oral administration of CMG extract (CMGE), at the levels of mRNA and CYP1A1 enzyme activity, was compared to respective enzyme modulation following oral administration of a well-known bioactive natural product, caffeine, as control compound known to involve hepatic enzymes in its metabolism. mRNA levels of Cyp1a1 and Cyp1a2 were measured by reverse transcription real-time polymerase chain reaction and their relative quantification was calculated. CYP1A1 enzyme induction was measured through the activity of ethoxyresorufin-O-deethylase (EROD). The results indicated that administration of CMGE at the recommended pharmaceutical dose does not induce significant transcriptional modulation of Cyp1a1/2 and subsequent enzyme activity induction of CYP1A1 while effects of the same order of magnitude were observed in the same test system following the administration of caffeine at the mean daily consumed levels. The outcome of this study further confirms the lack of any toxicological or biological significance of the specific findings on liver following the administration of CMGE.

  13. Modulation of CYP1A1 and CYP1A2 hepatic enzymes after oral administration of Chios mastic gum to male Wistar rats.

    Directory of Open Access Journals (Sweden)

    Efrosini S Katsanou

    Full Text Available Chios mastic gum (CMG, a resin derived from Pistacia lentiscus var. chia, is known since ancient times for its pharmacological activities. CYP1A1 and CYP1A2 enzymes are among the most involved in the biotransformation of chemicals and the metabolic activation of pro-carcinogens. Previous studies referring to the modulation of these enzymes by CMG have revealed findings of unclear biological and toxicological significance. For this purpose, the modulation of CYP1A1 and CYP1A2 enzymes in the liver of male Wistar rats following oral administration of CMG extract (CMGE, at the levels of mRNA and CYP1A1 enzyme activity, was compared to respective enzyme modulation following oral administration of a well-known bioactive natural product, caffeine, as control compound known to involve hepatic enzymes in its metabolism. mRNA levels of Cyp1a1 and Cyp1a2 were measured by reverse transcription real-time polymerase chain reaction and their relative quantification was calculated. CYP1A1 enzyme induction was measured through the activity of ethoxyresorufin-O-deethylase (EROD. The results indicated that administration of CMGE at the recommended pharmaceutical dose does not induce significant transcriptional modulation of Cyp1a1/2 and subsequent enzyme activity induction of CYP1A1 while effects of the same order of magnitude were observed in the same test system following the administration of caffeine at the mean daily consumed levels. The outcome of this study further confirms the lack of any toxicological or biological significance of the specific findings on liver following the administration of CMGE.

  14. Combinatorial synthesis of natural products

    DEFF Research Database (Denmark)

    Nielsen, John

    2002-01-01

    for preparation of combinatorial libraries. In other examples, natural products or intermediates have served as building blocks or scaffolds in the synthesis of complex natural products, bioactive analogues or designed hybrid molecules. Finally, structural motifs from the biologically active parent molecule have......Combinatorial syntheses allow production of compound libraries in an expeditious and organized manner immediately applicable for high-throughput screening. Natural products possess a pedigree to justify quality and appreciation in drug discovery and development. Currently, we are seeing a rapid...

  15. Records of alien marine species in the shallow coastal waters of Chios Island (2009

    Directory of Open Access Journals (Sweden)

    S. KATSANEVAKIS

    2012-12-01

    Full Text Available The shallow coastline of Chios Island was surveyed for the presence of any alien marine benthic species, during August 2009. Fourteen randomly selected sites were surveyed by snorkeling during standardized one-hour transects at depths between 0 and 10 m, and the presence of all identified alien benthic species was recorded. Six alien species were identified: Asparagopsis taxiformis, Caulerpa racemosa var. cylindracea, Stypopodium schimperi, Halophila stipulacea, Percnon gibbesi, and Siganus luridus. The green alga C. racemosa var. cylindracea was found in high densities in all the surveyed sites and was characterized as invasive in the island. The brown alga S. schimperi, the crab P. gibbesi, and the fish S. luridussustain established populations in the area. For three of the recorded marine alien species (S. schimperi, P. gibbesi, and S. luridus,Chios Island seems to be the northernmost margin of their geographical range in the Aegean Sea.

  16. Virtual Visit to the ATLAS Control Room by 1st and 3rd Lyceums in Chios

    CERN Multimedia

    2013-01-01

    High school students from the 1st and 3rd Lyceums of Chios, Greece, will be visiting the control room of ATLAS to discuss the latest results on the Higgs search, LHC’s first long shutdown and what the future holds for the ATLAS experiment. This visit takes place in the context of a Masterclass where students will learn how to analyse real events from the LHC with the use of the HYPATIA online applet based on educational scenarios from the Discover the COSMOS portal. This full-day activity is organized by the University of Athens, the University of the Aegean, Ellinogermaniki Agogi and the Chios Physical Society in the framework of the Open Discovery Space EU project.

  17. Natural products for plant protection

    Directory of Open Access Journals (Sweden)

    Čeković Živorad

    2006-01-01

    Full Text Available The advantage applying natural products, such as a secondary metabolites, in plant protection is shortly presented. Acceptable solutions for the enhanced ecological criteria, which are requested by the users of pesticides and consumers of agricultural goods, could be the replacement of classical pesticides by natural products in plant protection. Some natural products are already in use as insecticides, herbicides and fungicides because new biotechnological processes, fermentation and biotransformations provide procedures for their industrial production. In addition to biotechnical processes natural compounds possessing pesticide activities are also prepared by chemical synthesis. An active secondary metabolite must first be isolated from natural sauces and then, based on biological toxicological and ecological studies, acceptable compounds are selected for laboratory and industrial chemical synthesis. Several compounds possessing insecticidal, herbicidal and fungicidal activities, which have been successfully applied for plan protection are presented.

  18. Natural products in chemical biology

    National Research Council Canada - National Science Library

    Civjan, Natanya

    2012-01-01

    "Based on the award winning Wiley Encyclopedia of Chemical Biology, this book provides a general overview of the unique features of the small molecules referred to as "natural products", explores how...

  19. Combinatorial synthesis of natural products

    DEFF Research Database (Denmark)

    Nielsen, John

    2002-01-01

    Combinatorial syntheses allow production of compound libraries in an expeditious and organized manner immediately applicable for high-throughput screening. Natural products possess a pedigree to justify quality and appreciation in drug discovery and development. Currently, we are seeing a rapid...

  20. Synthesis of Polycyclic Natural Products

    Energy Technology Data Exchange (ETDEWEB)

    Nguyen, Tuan Hoang [Iowa State Univ., Ames, IA (United States)

    2003-01-01

    With the continuous advancements in molecular biology and modern medicine, organic synthesis has become vital to the support and extension of those discoveries. The isolations of new natural products allow for the understanding of their biological activities and therapeutic value. Organic synthesis is employed to aid in the determination of the relationship between structure and function of these natural products. The development of synthetic methodologies in the course of total syntheses is imperative for the expansion of this highly interdisciplinary field of science. In addition to the practical applications of total syntheses, the structural complexity of natural products represents a worthwhile challenge in itself. The pursuit of concise and efficient syntheses of complex molecules is both gratifying and enjoyable.

  1. Synthesis of Polycyclic Natural Products

    Energy Technology Data Exchange (ETDEWEB)

    Tuan Hoang Nguyen

    2003-05-31

    With the continuous advancements in molecular biology and modern medicine, organic synthesis has become vital to the support and extension of those discoveries. The isolations of new natural products allow for the understanding of their biological activities and therapeutic value. Organic synthesis is employed to aid in the determination of the relationship between structure and function of these natural products. The development of synthetic methodologies in the course of total syntheses is imperative for the expansion of this highly interdisciplinary field of science. In addition to the practical applications of total syntheses, the structural complexity of natural products represents a worthwhile challenge in itself. The pursuit of concise and efficient syntheses of complex molecules is both gratifying and enjoyable.

  2. Natural Products from Mangrove Actinomycetes

    Directory of Open Access Journals (Sweden)

    Dong-Bo Xu

    2014-05-01

    Full Text Available Mangroves are woody plants located in tropical and subtropical intertidal coastal regions. The mangrove ecosystem is becoming a hot spot for natural product discovery and bioactivity survey. Diverse mangrove actinomycetes as promising and productive sources are worth being explored and uncovered. At the time of writing, we report 73 novel compounds and 49 known compounds isolated from mangrove actinomycetes including alkaloids, benzene derivatives, cyclopentenone derivatives, dilactones, macrolides, 2-pyranones and sesquiterpenes. Attractive structures such as salinosporamides, xiamycins and novel indolocarbazoles are highlighted. Many exciting compounds have been proven as potential new antibiotics, antitumor and antiviral agents, anti-fibrotic agents and antioxidants. Furthermore, some of their biosynthetic pathways have also been revealed. This review is an attempt to consolidate and summarize the past and the latest studies on mangrove actinomycetes natural product discovery and to draw attention to their immense potential as novel and bioactive compounds for marine drugs discovery.

  3. Pharmacophore-driven identification of PPARγ agonists from natural sources

    Science.gov (United States)

    Petersen, Rasmus K.; Christensen, Kathrine B.; Assimopoulou, Andreana N.; Fretté, Xavier; Papageorgiou, Vassilios P.; Kristiansen, Karsten; Kouskoumvekaki, Irene

    2011-02-01

    In a search for more effective and safe anti-diabetic compounds, we developed a pharmacophore model based on partial agonists of PPARγ. The model was used for the virtual screening of the Chinese Natural Product Database (CNPD), a library of plant-derived natural products primarily used in folk medicine. From the resulting hits, we selected methyl oleanonate, a compound found, among others, in Pistacia lentiscus var. Chia oleoresin (Chios mastic gum). The acid of methyl oleanonate, oleanonic acid, was identified as a PPARγ agonist through bioassay-guided chromatographic fractionations of Chios mastic gum fractions, whereas some other sub-fractions exhibited also biological activity towards PPARγ. The results from the present work are two-fold: on the one hand we demonstrate that the pharmacophore model we developed is able to select novel ligand scaffolds that act as PPARγ agonists; while at the same time it manifests that natural products are highly relevant for use in virtual screening-based drug discovery.

  4. System of Natural Health Products

    Directory of Open Access Journals (Sweden)

    Angelica Paoletti

    2011-01-01

    Full Text Available Introduction. The safety of vitamin K antagonists (VKA use can be compromised by many popular herbal supplements taken by individuals. The literature reports that 30% of warfarin-treated patients self-medicates with herbs. Possible interactions represent an health risk. We aimed to identify all herbs-oral anticoagulants interactions collected in the Italian database of suspected adverse reactions to “natural health” products. Methods. The Italian database of spontaneous reports of suspected adverse reactions to natural products was analyzed to address herb-VKAs interactions. Results. From 2002 to 2009, we identified 12 reports with 7 cases of INR reduction in patients treated with warfarin (n=3 and acenocoumarol (n=4, and 5 cases of INR increase (all warfarin associated. It was reported 8 different herbal products as possibly interacting. Discussion. Our study confirms the risk of interactions, highlighting the difficulty to characterize them and their mechanisms and, finally, prevent their onset. The reported data underline the urgent need of healthcare providers being aware of the possible interaction between natural products and VKA, also because of the critical clinical conditions affecting patients. This is the first step to have the best approach to understand possible INR alterations linked to herb-VKA interaction and to rightly educate patients in treatment with VKA.

  5. Chios mastic treatment of patients with active Crohn's disease

    Institute of Scientific and Technical Information of China (English)

    Andriana C Kaliora; Maria G Stathopoulou; John K Triantafillidis; George VZ Dedoussis; Nikolaos K Andrikopoulos

    2007-01-01

    AIM: To evaluate the effectiveness of mastic administration on the clinical course and plasma inflammatory mediators of patients with active Crohn's disease (CD).METHODS: This pilot study was conducted in patients with established mild to moderately active CD, attending the outpatient clinics of the hospital, and in healthy controls. Ten patients and 8 controls were recruited for a 4-wk treatment with mastic caps (6 caps/d, 0.37 g/cap).All patients successfully completed the protocol. CD Activity Index (CDAI), Nutritional Risk Index (NRI), C-reactive protein (CRP), interleukin-6 (IL-6), tumor necrosis factor-alpha (TNF-α), monocyte chemotactic protein-1 (MCP-1), and total antioxidant potential (TAP) were evaluated in the plasma at baseline and at the end of the treatment period. Results were expressed as mean values + SE and P < 0.05 was considered to indicate statistical significance.RESULTS: Patients exhibited significant reduction of CDAI (222.9 ± 18.7 vs 136.3 ± 12.3, P = 0.05) as compared to pretreament values. Plasma IL-6 was significantly decreased (21.2 ± 9.3 pg/mL vs 7.2 ± 2.8 pg/mL,P = 0.027), and so did CRP (40.3 ± 13.1 mg/mL vs 19.7± 5.5, P = 0.028). TAP was significantly increased (0.15± 0.09 vs 0.57 ± 0.15 mmol/L uric acid, P = 0.036). No patient or control exhibited any kind of side effects.CONCLUSION: The results suggest that mastic significantly decreased the activity index and the plasma levels of IL-6 and CRP in patients with mildly to moderately active CD. Further double-blind, placebo-controlled studies in a larger number of patients are required to clarify the role of this natural product in the treatment of patients with CD.

  6. Glycosylation and Activities of Natural Products.

    Science.gov (United States)

    Huang, Gangliang; Lv, Meijiao; Hu, Jinchuan; Huang, Kunlin; Xu, Hong

    2016-01-01

    Natural products are widely found in nature, their number and variety are numerous, the structures are complex and diverse. These natural products have many physiological and pharmacological activities. Glycosylation can increase the diversity of structure and function of natural product, it has become the focus of drug research and development. The impacts of glycosylation of natural products to water solubility, pharmacological activities, bioavailability, or others were described in this review, which provides a reference for the development and application of glycosylated natural products.

  7. Natural products as antimitotic agents.

    Science.gov (United States)

    Dall'Acqua, Stefano

    2014-01-01

    Natural products still play an important role in the medicinal chemistry, especially in some therapeutic areas. As example more than 60% of currently-used anticancer agents are derives from natural sources including plants, marine organisms or micro-organism. Thus natural products (NP) are an high-impact source of new "lead compounds" or new potential therapeutic agents despite the large development of biotechnology and combinatorial chemistry in the drug discovery and development. Many examples of anticancer drugs as paclitaxel, combretastatin, bryostatin and discodermolide have shown the importance of NP in the anticancer chemotherapy through many years. Many organisms have been studied as sources of drugs namely plants, micro-organisms and marine organisms and the obtained NP can be considered a group of "privileged chemical structures" evolved in nature to interact with other organisms. For this reason NP are a good starting points for pharmaceutical research and also for library design. Tubulin and microtubules are one of the most studied targets for the search of anticancer compounds. Microtubule targeting agents (MTA) also named antimitotic agents are compounds that are able to perturb mitosis but are also able to arrest cell growing during interphase. The anticancer drugs, taxanes and vinca alkaloids have established tubulin as important target in cancer therapy. More recently the vascular disrupting agents (VDA) combretastatin analogues were studied for their antimitotics properties. This review will consider the anti mitotic NP and their potential impact in the development of new therapeutic agents.

  8. A study of the spinal cord injured population of the Chios island of Greece

    Directory of Open Access Journals (Sweden)

    Ismini Serpanou

    2011-01-01

    Full Text Available Objective: The objective of this study was to explore the epidemiological profile of the spinal cord injuredpopulation living on the Greek island Chios.Methods: We interviewed the regional spinal cord injured population. Participants were recruited from theisland’s capital and its 52 villages. The target population was all the SCI individuals living on Chios Island (n=38,out of which 34 (response rate was 89% patients were interviewed in their homes using an especially designedquestionnaire.Results: The mean age of the subjects at the time of the injury was 43 and the majority (n=23, 67.6% were male.The employment status of the participants changed after the injury from 64.7% (n=22 to 32.4% (n=11. Trafficaccidents were the cause of the SCI for 44.8%, with a significant difference from the other causes of injury(p<0.004. The most common level of injury was thoracic-lumbar (23.5%, n=8. The duration of hospitalizationwas on average 4.6 ± 3.9 months followed by treatment in rehabilitation centres. Most participants faced secondarycomplications which correlated significantly with age (r=0.372 p=0.03.Conclusions: The findings revealed that traffic accidents were the main reason for SCI. More research is neededon SCIs in Greece and the development of a surveillance system for SCIs is suggested.

  9. Evaluation of Chios mastic gum on lipid and glucose metabolism in diabetic mice.

    Science.gov (United States)

    Georgiadis, Ioannis; Karatzas, Theodore; Korou, Laskarina-Maria; Agrogiannis, George; Vlachos, Ioannis S; Pantopoulou, Alkisti; Tzanetakou, Irene P; Katsilambros, Nikolaos; Perrea, Despina N

    2014-03-01

    Chios mastic gum (MG), a resin produced from Pistacia lentiscus var. Chia, is reported to possess beneficial cardiovascular and hepatoprotective properties. This study investigated the effect of crude Chios MG on metabolic parameters in diabetic mice. Streptozotocin-induced diabetic 12-week-old male C57bl/6 mice were assigned to three groups: NC (n=9) control; LdM (n=9) animals receiving low dose mastic for 8 weeks (20 mg/kg body weight [BW]); and HdM (n=9) animals receiving high dose mastic (500 mg/kg BW) for the same period. Serum lipid and glucose levels were determined at baseline, at 4 and 8 weeks. Serum total protein, adiponectin, and resistin levels were also measured at the end of the experiment. Histopathological examination for liver, kidney, aorta, and heart lesions was performed. After 4 weeks, MG administration resulted in decreased serum glucose and triglyceride levels in both LdM and HdM, whereas BW levels were reduced in LdM group compared with controls. At the end of the experiment, LdM presented significantly lower serum glucose, cholesterol, low-density lipoprotein cholesterol, and triglyceride levels and improved high-density lipoprotein cholesterol levels compared with control group. HdM group had ameliorated serum triglyceride levels. Hepatic steatosis observed in control group was partially reversed in LdM and HdM groups. MG administered in low dosages improves glucose and lipid disturbances in diabetic mice while alleviating hepatic damage.

  10. Y-chromosomal STR haplotypes in a population sample from continental Greece, and the islands of Crete and Chios.

    Science.gov (United States)

    Robino, C; Varacalli, S; Gino, S; Chatzikyriakidou, A; Kouvatsi, A; Triantaphyllidis, C; Di Gaetano, C; Crobu, F; Matullo, G; Piazza, A; Torre, C

    2004-10-04

    Eight Y-chromosomal short tandem repeats (STRs)--DYS19, DYS389-I, DYS389-II, DYS390, DYS391, DYS392, DYS393, and DYS385--were typed in a population sample (n = 113) of unrelated males from seven different regions of Greece (Macedonia, Thessaly, Epirus, Central Greece, Peloponnese, Crete Island, and Chios Island).

  11. Synthetic glycosylated natural products have satisfactory activities.

    Science.gov (United States)

    Huang, Gangliang; Mei, Xinya

    2014-01-01

    Many natural products contain sugar residues, which are essential components for great medicinal importance. The sugar moieties can improve water-solubility of natural products and decrease their toxicity. At the same time, the glycosidic residues are crucial for the activities of natural products. Much effort has been expended over the past decades in developing novel and efficient methodologies to synthesize the glycosylated natural products. This review highlights recent developments in the synthesis of glycosylated natural products. The structure-activity relationships of some of these glycosylated natural products, together with the structure characteristics of their interaction with the biological targets, are also involved.

  12. Natural and engineered biosynthesis of fluorinated natural products.

    Science.gov (United States)

    Walker, Mark C; Chang, Michelle C Y

    2014-09-21

    Both natural products and synthetic organofluorines play important roles in the discovery and design of pharmaceuticals. The combination of these two classes of molecules has the potential to be useful in the ongoing search for new bioactive compounds but our ability to produce site-selectively fluorinated natural products remains limited by challenges in compatibility between their high structural complexity and current methods for fluorination. Living systems provide an alternative route to chemical fluorination and could enable the production of organofluorine natural products through synthetic biology approaches. While the identification of biogenic organofluorines has been limited, the study of the native organisms and enzymes that utilize these compounds can help to guide efforts to engineer the incorporation of this unusual element into complex pharmacologically active natural products. This review covers recent advances in understanding both natural and engineered production of organofluorine natural products.

  13. Hot springs and cool natural products.

    Science.gov (United States)

    Kwon, Ho Jeong; Lee, Choong Hwan; Osada, Hiroyuki; Yoshida, Minoru; Imoto, Masaya

    2008-08-01

    Natural products have played a unique role in providing new tools and insights in chemical biology. The tremendous value of natural products was highlighted by scientists from Korea and Japan at the 4(th) Korea-Japan Chemical Biology symposium.

  14. Nigerian Journal of Natural Products and Medicine

    African Journals Online (AJOL)

    Nigerian Journal of Natural Products and Medicine. ... 1982 dedicated to the promotion of Pharmacognosy, Natural Products and Traditional Medicine. .... Acuminatoside: a new anticancer compound from the maiden breast plant · EMAIL FULL ...

  15. Teaching 'natural product chemistry' in Tanzania | Buchanan ...

    African Journals Online (AJOL)

    Teaching 'natural product chemistry' in Tanzania. ... PROMOTING ACCESS TO AFRICAN RESEARCH. AFRICAN JOURNALS ONLINE (AJOL) · Journals ... Natural products 'historically' and 'today' have vast importance. This article describes ...

  16. Misassigned natural products and their revised structures.

    Science.gov (United States)

    Yoo, Hye-Dong; Nam, Sang-Jip; Chin, Young-Won; Kim, Min-Sun

    2016-02-01

    Natural products are a major pipeline for drug development and are responsible for more than 50 % of drugs on the market. NMR is a fundamental and powerful tool for the structure determination of natural products. It is essential to provide unambiguous chemical structure information on natural products in drug development research, including the structure-activity relationship, derivatization and pharmacokinetic/pharmacodynamic studies. Advancement of NMR instruments has made it possible to deal with nanomole-scale natural products for structure elucidation, but misinterpretation of NMR spectra still occurs. We review 21 natural products with revised chemical structures and the methods used for those revisions.

  17. Natural products and body weight control

    Directory of Open Access Journals (Sweden)

    Jay Lee

    2011-01-01

    Full Text Available The purpose of the review was to summarise the effect of some commonly available natural products used for body weight management. We collected data from PubMed and scientific journals. There are numerous publications on this topic, however we have summarized the most commonly available and potent natural products from recent 53 publications. The natural products analyzed in this paper include catechins, capsaicin, conjugated linoleic acid, fucoxanthin, soy isoflavone, glabridin, astaxanthin and cyaniding-3-glucoside. These natural products are effective and safe for body weight management. Further studies need to be conducted to investigate the mechanism of action, metabolism, long term safety and side effects of these natural products, as well as interactions between these natural products with dietary components.

  18. Accounting Of Products Collected From Nature

    Directory of Open Access Journals (Sweden)

    Ahmet Gökgöz

    2015-12-01

    Full Text Available Products from nature can be classified as “production” or “collection from nature” within agricultural production. Products collected from nature vary in type and can sum up to important quantities. Thyme, mushroom, chestnut, sage, linden, saffron from plant origin can be given as examples to products from nature as well as fish, mussel, octopus, birds from animal origin. This study covers the accounting area of products obtained from nature. The evaluation of collection of these products from nature in terms of agricultural operation poses great importance for accounting issues. Thus, special care will be given to issues of accounting of these products within the scope of Turkish Tax Legislation and Turkish Accounting Standards

  19. Super Natural II--a database of natural products.

    Science.gov (United States)

    Banerjee, Priyanka; Erehman, Jevgeni; Gohlke, Björn-Oliver; Wilhelm, Thomas; Preissner, Robert; Dunkel, Mathias

    2015-01-01

    Natural products play a significant role in drug discovery and development. Many topological pharmacophore patterns are common between natural products and commercial drugs. A better understanding of the specific physicochemical and structural features of natural products is important for corresponding drug development. Several encyclopedias of natural compounds have been composed, but the information remains scattered or not freely available. The first version of the Supernatural database containing ∼ 50,000 compounds was published in 2006 to face these challenges. Here we present a new, updated and expanded version of natural product database, Super Natural II (http://bioinformatics.charite.de/supernatural), comprising ∼ 326,000 molecules. It provides all corresponding 2D structures, the most important structural and physicochemical properties, the predicted toxicity class for ∼ 170,000 compounds and the vendor information for the vast majority of compounds. The new version allows a template-based search for similar compounds as well as a search for compound names, vendors, specific physical properties or any substructures. Super Natural II also provides information about the pathways associated with synthesis and degradation of the natural products, as well as their mechanism of action with respect to structurally similar drugs and their target proteins.

  20. Counting on natural products for drug design

    Science.gov (United States)

    Rodrigues, Tiago; Reker, Daniel; Schneider, Petra; Schneider, Gisbert

    2016-06-01

    Natural products and their molecular frameworks have a long tradition as valuable starting points for medicinal chemistry and drug discovery. Recently, there has been a revitalization of interest in the inclusion of these chemotypes in compound collections for screening and achieving selective target modulation. Here we discuss natural-product-inspired drug discovery with a focus on recent advances in the design of synthetically tractable small molecules that mimic nature's chemistry. We highlight the potential of innovative computational tools in processing structurally complex natural products to predict their macromolecular targets and attempt to forecast the role that natural-product-derived fragments and fragment-like natural products will play in next-generation drug discovery.

  1. Natural Connections on Riemannian Product Manifolds

    OpenAIRE

    Gribacheva, Dobrinka

    2011-01-01

    A Riemannian almost product manifold with integrable almost product structure is called a Riemannian product manifold. In the present paper the natural connections on such manifolds are studied, i.e. the linear connections preserving the almost product structure and the Riemannian metric.

  2. Food production and nature conservation

    NARCIS (Netherlands)

    Gordon, Iain J.; Squire, Geoff R.; Prins, Herbert H.T.

    2016-01-01

    Feeding the world's growing human population is increasingly challenging, especially as more people adopt a western diet and lifestyle. Doing so without causing damage to nature poses an even greater challenge. This book argues that in order to create a sustainable food supply whilst conserving

  3. Functional chromatographic technique for natural product isolation†

    Science.gov (United States)

    Lau, Eric C.; Mason, Damian J.; Eichhorst, Nicole; Engelder, Pearce; Mesa, Celestina; Kithsiri Wijeratne, E. M.; Gunaherath, G. M. Kamal B.; Leslie Gunatilaka, A. A.

    2015-01-01

    Natural product discovery arises through a unique interplay between chromatographic purification and biological assays. Currently, most techniques used for natural product purification deliver leads without a defined biological action. We now describe a technique, referred to herein as functional chromatography, that deploys biological affinity as the matrix for compound isolation. PMID:25588099

  4. Functional chromatographic technique for natural product isolation†

    OpenAIRE

    Lau, Eric C.; Mason, Damian J.; Eichhorst, Nicole; Engelder, Pearce; Mesa, Celestina; Kithsiri Wijeratne, E. M.; Gunaherath, G. M. Kamal B.; Leslie Gunatilaka, A. A.; La Clair, James J.; Chapman, Eli

    2015-01-01

    Natural product discovery arises through a unique interplay between chromatographic purification and biological assays. Currently, most techniques used for natural product purification deliver leads without a defined biological action. We now describe a technique, referred to herein as functional chromatography, that deploys biological affinity as the matrix for compound isolation.

  5. Bioactive natural products from novel microbial sources.

    Science.gov (United States)

    Challinor, Victoria L; Bode, Helge B

    2015-09-01

    Despite the importance of microbial natural products for human health, only a few bacterial genera have been mined for the new natural products needed to overcome the urgent threat of antibiotic resistance. This is surprising, given that genome sequencing projects have revealed that the capability to produce natural products is not a rare feature among bacteria. Even the bacteria occurring in the human microbiome produce potent antibiotics, and thus potentially are an untapped resource for novel compounds, potentially with new activities. This review highlights examples of bacteria that should be considered new sources of natural products, including anaerobes, pathogens, and symbionts of humans, insects, and nematodes. Exploitation of these producer strains, combined with advances in modern natural product research methodology, has the potential to open the way for a new golden age of microbial therapeutics.

  6. Stereoselective Halogenation in Natural Product Synthesis.

    Science.gov (United States)

    Chung, Won-jin; Vanderwal, Christopher D

    2016-03-24

    At last count, nearly 5000 halogenated natural products have been discovered. In approximately half of these compounds, the carbon atom to which the halogen is bound is sp(3) -hybridized; therefore, there are an enormous number of natural products for which stereocontrolled halogenation must be a critical component of any synthesis strategy. In this Review, we critically discuss the methods and strategies used for stereoselective introduction of halogen atoms in the context of natural product synthesis. Using the successes of the past, we also attempt to identify gaps in our synthesis technology that would aid the synthesis of halogenated natural products, as well as existing methods that have not yet seen application in complex molecule synthesis. The chemistry described herein demonstrates yet again how natural products continue to provide the inspiration for critical advances in chemical synthesis.

  7. Genotoxic and Antigenotoxic Assessment of Chios Mastic Oil by the In Vitro Micronucleus Test on Human Lymphocytes and the In Vivo Wing Somatic Test on Drosophila.

    Directory of Open Access Journals (Sweden)

    Dimitris Vlastos

    Full Text Available Chios mastic oil (CMO, the essential oil derived from Pistacia lentiscus (L. var. chia (Duham, has generated considerable interest because of its antimicrobial, anticancer, antioxidant and other beneficial properties. In the present study, the potential genotoxic activity of CMO as well as its antigenotoxic properties against the mutagenic agent mitomycin-C (MMC were evaluated by employing the in vitro Cytokinesis Block MicroNucleus (CBMN assay and the in vivo Somatic Mutation And Recombination Test (SMART. In the in vitro experiments, lymphocytes were treated with 0.01, 0.05 and 0.10% (v/v of CMO with or without 0.05 μg/ml MMC, while in the in vivo assay Drosophila larvae were fed with 0.05, 0.10, 0.50 and 1.00% (v/v of CMO with or without 2.50 μg/ml MMC. CMO did not significantly increase the frequency of micronuclei (MN or total wing spots, indicating lack of mutagenic or recombinogenic activity. However, the in vitro analysis suggested cytotoxic activity of CMO. The simultaneous administration of MMC with CMO did not alter considerably the frequencies of MMC-induced MN and wing spots showing that CMO doesn't exert antigenotoxic or antirecombinogenic action. Therefore, CMO could be considered as a safe product in terms of genotoxic potential. Even though it could not afford any protection against DNA damage, at least under our experimental conditions, its cytotoxic potential could be of interest.

  8. Genotoxic and Antigenotoxic Assessment of Chios Mastic Oil by the In Vitro Micronucleus Test on Human Lymphocytes and the In Vivo Wing Somatic Test on Drosophila.

    Science.gov (United States)

    Vlastos, Dimitris; Drosopoulou, Elena; Efthimiou, Ioanna; Gavriilidis, Maximos; Panagaki, Dimitra; Mpatziou, Krystalenia; Kalamara, Paraskevi; Mademtzoglou, Despoina; Mavragani-Tsipidou, Penelope

    2015-01-01

    Chios mastic oil (CMO), the essential oil derived from Pistacia lentiscus (L.) var. chia (Duham), has generated considerable interest because of its antimicrobial, anticancer, antioxidant and other beneficial properties. In the present study, the potential genotoxic activity of CMO as well as its antigenotoxic properties against the mutagenic agent mitomycin-C (MMC) were evaluated by employing the in vitro Cytokinesis Block MicroNucleus (CBMN) assay and the in vivo Somatic Mutation And Recombination Test (SMART). In the in vitro experiments, lymphocytes were treated with 0.01, 0.05 and 0.10% (v/v) of CMO with or without 0.05 μg/ml MMC, while in the in vivo assay Drosophila larvae were fed with 0.05, 0.10, 0.50 and 1.00% (v/v) of CMO with or without 2.50 μg/ml MMC. CMO did not significantly increase the frequency of micronuclei (MN) or total wing spots, indicating lack of mutagenic or recombinogenic activity. However, the in vitro analysis suggested cytotoxic activity of CMO. The simultaneous administration of MMC with CMO did not alter considerably the frequencies of MMC-induced MN and wing spots showing that CMO doesn't exert antigenotoxic or antirecombinogenic action. Therefore, CMO could be considered as a safe product in terms of genotoxic potential. Even though it could not afford any protection against DNA damage, at least under our experimental conditions, its cytotoxic potential could be of interest.

  9. Targeting Nuclear Receptors with Marine Natural Products

    Directory of Open Access Journals (Sweden)

    Chunyan Yang

    2014-01-01

    Full Text Available Nuclear receptors (NRs are important pharmaceutical targets because they are key regulators of many metabolic and inflammatory diseases, including diabetes, dyslipidemia, cirrhosis, and fibrosis. As ligands play a pivotal role in modulating nuclear receptor activity, the discovery of novel ligands for nuclear receptors represents an interesting and promising therapeutic approach. The search for novel NR agonists and antagonists with enhanced selectivities prompted the exploration of the extraordinary chemical diversity associated with natural products. Recent studies involving nuclear receptors have disclosed a number of natural products as nuclear receptor ligands, serving to re-emphasize the translational possibilities of natural products in drug discovery. In this review, the natural ligands of nuclear receptors will be described with an emphasis on their mechanisms of action and their therapeutic potentials, as well as on strategies to determine potential marine natural products as nuclear receptor modulators.

  10. Natural food pigments application in food products

    Directory of Open Access Journals (Sweden)

    Emilia Janiszewska-Turak

    2016-12-01

    Full Text Available Natural pigments, food compounds, are responsible for the colour of the products. These additives can impart, to deepen or renew the colour of the product, if it has been lost while processing. They also improve the taste of the product and facilitate its identification. It is hard to imagine today’s food industry without the use of pigments. Presently, more and more conscious con­sumers are demanding products to be coloured with natural pigments or any pigment added to the final product. Artificial pigments are considered to be harmful and undesirable so food manufacturers focus on the use of natural colour substances. 16 natural pigments are presently permitted to be used. These compounds are: betalains – betanin, quinones – cochineal, flavonoids – anthocyan­ins, isoprenoids – carotene, annatto (bixin, norbixin, paprika extract, lutein, canthaxanthin, porphyrins – chlorophylls and chlorophyllins and copper complexes of these compounds, and others: caramels, curcumin, or plant coal.

  11. New Synthetic Methods for Hypericum Natural Products

    Energy Technology Data Exchange (ETDEWEB)

    Jeon, Insik [Iowa State Univ., Ames, IA (United States)

    2006-01-01

    Organic chemistry has served as a solid foundation for interdisciplinary research areas, such as molecular biology and medicinal chemistry. An understanding of the biological activities and structural elucidations of natural products can lead to the development of clinically valuable therapeutic options. The advancements of modern synthetic methodologies allow for more elaborate and concise natural product syntheses. The theme of this study centers on the synthesis of natural products with particularly challenging structures and interesting biological activities. The synthetic expertise developed here will be applicable to analog syntheses and to other research problems.

  12. Cancer wars: natural products strike back

    Science.gov (United States)

    Basmadjian, Christine; Zhao, Qian; Bentouhami, Embarek; Djehal, Amel; Nebigil, Canan G.; Johnson, Roger A.; Serova, Maria; de Gramont, Armand; Faivre, Sandrine; Raymond, Eric; Désaubry, Laurent G.

    2014-01-01

    Natural products have historically been a mainstay source of anticancer drugs, but in the 90's they fell out of favor in pharmaceutical companies with the emergence of targeted therapies, which rely on antibodies or small synthetic molecules identified by high throughput screening. Although targeted therapies greatly improved the treatment of a few cancers, the benefit has remained disappointing for many solid tumors, which revitalized the interest in natural products. With the approval of rapamycin in 2007, 12 novel natural product derivatives have been brought to market. The present review describes the discovery and development of these new anticancer drugs and highlights the peculiarities of natural product and new trends in this exciting field of drug discovery. PMID:24822174

  13. Sources for Leads: Natural Products and Libraries.

    Science.gov (United States)

    van Herwerden, Eric F; Süssmuth, Roderich D

    2016-01-01

    Natural products have traditionally been a major source of leads in the drug discovery process. However, the development of high-throughput screening led to an increased interest in synthetic methods that enabled the rapid construction of large libraries of molecules. This resulted in the termination or downscaling of many natural product research programs, but the chemical libraries did not necessarily produce a larger amount of drug leads. On one hand, this chapter explores the current state of natural product research within the drug discovery process. On the other hand it evaluates the efforts made to increase the amount of leads generated from chemical libraries and considers what role natural products could play here.

  14. Cancer wars: Natural products strike back

    Science.gov (United States)

    Basmadjian, Christine; Zhao, Qian; Djehal, Amel; Bentouhami, Embarek; Nebigil, Canan; Johnson, Roger; Serova, Maria; De Gramont, Armand; Faivre, Sandrine; Raymond, Eric; Désaubry, Laurent

    2014-05-01

    Natural products have historically been a mainstay source of anticancer drugs, but in the 90’s they fell out of favor in pharmaceutical companies with the emergence of targeted therapies, which rely on antibodies or small synthetic molecules identified by high throughput screening. Although targeted therapies greatly improved the treatment of a few cancers, the benefit has remained disappointing for many sol¬¬id tumors, which revitalized the interest in natural products. With the approval of rapamycin in 2007, twelve novel natural product derivatives have been brought to market. The present review describes the discovery and development of these new anticancer drugs and highlights the peculiarities of natural product and new trends in this exciting field of drug discovery.

  15. ARTEMISININ: THE JOURNEY FROM NATURAL PRODUCT TO ...

    African Journals Online (AJOL)

    services, many parents lose their children to complications ... ARTEMISININ: THE JOURNEY FROM NATURAL PRODUCT TO NOBEL PRIZE. SUMMARY ... Medicine, where she has remained for over 55 years. After joining ... An advantage of.

  16. High impact technologies for natural products screening.

    Science.gov (United States)

    Koehn, Frank E

    2008-01-01

    Natural products have historically been a rich source of lead molecules in drug discovery. However, natural products have been de-emphasized as high throughput screening resources in the recent past, in part because of difficulties in obtaining high quality natural products screening libraries, or in applying modern screening assays to these libraries. In addition, natural products programs based on screening of extract libraries, bioassay-guided isolation, structure elucidation and subsequent production scale-up are challenged to meet the rapid cycle times that are characteristic of the modern HTS approach. Fortunately, new technologies in mass spectrometry, NMR and other spectroscopic techniques can greatly facilitate the first components of the process - namely the efficient creation of high-quality natural products libraries, bimolecular target or cell-based screening, and early hit characterization. The success of any high throughput screening campaign is dependent on the quality of the chemical library. The construction and maintenance of a high quality natural products library, whether based on microbial, plant, marine or other sources is a costly endeavor. The library itself may be composed of samples that are themselves mixtures - such as crude extracts, semi-pure mixtures or single purified natural products. Each of these library designs carries with it distinctive advantages and disadvantages. Crude extract libraries have lower resource requirements for sample preparation, but high requirements for identification of the bioactive constituents. Pre-fractionated libraries can be an effective strategy to alleviate interferences encountered with crude libraries, and may shorten the time needed to identify the active principle. Purified natural product libraries require substantial resources for preparation, but offer the advantage that the hit detection process is reduced to that of synthetic single component libraries. Whether the natural products library

  17. Cancer wars: Natural products strike back

    OpenAIRE

    Christine eBasmadjian; Qian eZhao; Amel eDjehal; Embarek eBentouhami; Nebigil, Canan G.; Johnson, Roger A.; Maria eSerova; Armand eDe Gramont; Sandrine eFaivre; Eric eRaymond; Désaubry, Laurent G.

    2014-01-01

    Natural products have historically been a mainstay source of anticancer drugs, but in the 90’s they fell out of favor in pharmaceutical companies with the emergence of targeted therapies, which rely on antibodies or small synthetic molecules identified by high throughput screening. Although targeted therapies greatly improved the treatment of a few cancers, the benefit has remained disappointing for many sol¬¬id tumors, which revitalized the interest in natural products. With the approval of ...

  18. Cancer wars: natural products strike back

    OpenAIRE

    Basmadjian, Christine; Zhao, Qian; Bentouhami, Embarek; Djehal, Amel; Nebigil, Canan G.; Johnson, Roger A.; Serova, Maria; Gramont, Armand de; Faivre, Sandrine; Raymond, Eric; Désaubry, Laurent G.

    2014-01-01

    Natural products have historically been a mainstay source of anticancer drugs, but in the 90's they fell out of favor in pharmaceutical companies with the emergence of targeted therapies, which rely on antibodies or small synthetic molecules identified by high throughput screening. Although targeted therapies greatly improved the treatment of a few cancers, the benefit has remained disappointing for many solid tumors, which revitalized the interest in natural products. With the approval of ra...

  19. Reconstructing fungal natural product biosynthetic pathways.

    Science.gov (United States)

    Lazarus, C M; Williams, K; Bailey, A M

    2014-10-01

    Large scale fungal genome sequencing has revealed a multitude of potential natural product biosynthetic pathways that remain uncharted. Here we describe some of the methods that have been used to explore them via heterologous gene expression. We focus on filamentous fungal hosts and discuss the technological challenges and successes behind the reconstruction of fungal natural product pathways. Optimised, efficient heterologous expression of reconstructed biosynthetic pathways promises progress in the discovery of novel compounds that could be utilised by the pharmaceutical and agrochemical industries.

  20. TEACHING 'NATURAL PRODUCT CHEMISTRY' IN TANZANIA

    African Journals Online (AJOL)

    Temechegn

    natural product chemistry or chemistry of natural medicines [4]. There is even ... The course is an optional course (not core) open to 3rd year (final year) students in the. Faculty of .... a gift to the newborn Jesus (Matthew 2:11) [24]. • Olive oil is ...

  1. Evaluation of the genotoxic and antigenotoxic effects of Chios mastic water by the in vitro micronucleus test on human lymphocytes and the in vivo wing somatic test on Drosophila.

    Science.gov (United States)

    Vlastos, Dimitris; Mademtzoglou, Despoina; Drosopoulou, Elena; Efthimiou, Ioanna; Chartomatsidou, Tatiana; Pandelidou, Christina; Astyrakaki, Melina; Chalatsi, Eleftheria; Mavragani-Tsipidou, Penelope

    2013-01-01

    Chios mastic gum, a plant-derived product obtained by the Mediterranean bush Pistacia lentiscus (L.) var. chia (Duham), has generated considerable interest because of its antimicrobial, anticancer, antioxidant and other beneficial properties. Its aqueous extract, called Chios mastic water (CMW), contains the authentic mastic scent and all the water soluble components of mastic. In the present study, the potential genotoxic activity of CMW, as well as its antigenotoxic properties against the mutagenic agent mitomycin-C (MMC), was evaluated by employing the in vitro Cytokinesis Block MicroNucleus (CBMN) assay and the in vivo Somatic Mutation And Recombination Test (SMART). In the former assay, lymphocytes were treated with 1, 2 and 5% (v/v) of CMW with or without MMC at concentrations 0.05 and 0.50 µg/ml. No significant micronucleus induction was observed by CMW, while co-treatment with MMC led to a decrease of the MMC-induced micronuclei, which ranged between 22.8 and 44.7%. For SMART, larvae were treated with 50 and 100% (v/v) CMW with or without MMC at concentrations 1.00, 2.50 and 5.00 µg/ml. It was shown that CMW alone did not modify the spontaneous frequencies of spots indicating lack of genotoxic activity. Τhe simultaneous administration of MMC with 100% CMW led to considerable alterations of the frequencies of MMC-induced wing spots with the total mutant clones showing reduction between 53.5 and 74.4%. Our data clearly show a protective role of CMW against the MMC-induced genotoxicity and further research on the beneficial properties of this product is suggested.

  2. Evaluation of the genotoxic and antigenotoxic effects of Chios mastic water by the in vitro micronucleus test on human lymphocytes and the in vivo wing somatic test on Drosophila.

    Directory of Open Access Journals (Sweden)

    Dimitris Vlastos

    Full Text Available Chios mastic gum, a plant-derived product obtained by the Mediterranean bush Pistacia lentiscus (L. var. chia (Duham, has generated considerable interest because of its antimicrobial, anticancer, antioxidant and other beneficial properties. Its aqueous extract, called Chios mastic water (CMW, contains the authentic mastic scent and all the water soluble components of mastic. In the present study, the potential genotoxic activity of CMW, as well as its antigenotoxic properties against the mutagenic agent mitomycin-C (MMC, was evaluated by employing the in vitro Cytokinesis Block MicroNucleus (CBMN assay and the in vivo Somatic Mutation And Recombination Test (SMART. In the former assay, lymphocytes were treated with 1, 2 and 5% (v/v of CMW with or without MMC at concentrations 0.05 and 0.50 µg/ml. No significant micronucleus induction was observed by CMW, while co-treatment with MMC led to a decrease of the MMC-induced micronuclei, which ranged between 22.8 and 44.7%. For SMART, larvae were treated with 50 and 100% (v/v CMW with or without MMC at concentrations 1.00, 2.50 and 5.00 µg/ml. It was shown that CMW alone did not modify the spontaneous frequencies of spots indicating lack of genotoxic activity. Τhe simultaneous administration of MMC with 100% CMW led to considerable alterations of the frequencies of MMC-induced wing spots with the total mutant clones showing reduction between 53.5 and 74.4%. Our data clearly show a protective role of CMW against the MMC-induced genotoxicity and further research on the beneficial properties of this product is suggested.

  3. Microbial production of natural raspbery ketone

    NARCIS (Netherlands)

    Beekwilder, M.J.; Meer, van der I.M.; Sibbesen, O.; Broekgaarden, M.; Qvist, I.; Mikkelsen, J.D.; Hall, R.D.

    2007-01-01

    Raspberry ketone is an important compound for the flavour industry. It is frequently used in products such as soft drinks, sweets, puddings and ice creams. The compound can be produced by organic synthesis. Demand for natural raspberry ketone is growing considerably. However, this product is

  4. Microbial production of natural raspbery ketone

    NARCIS (Netherlands)

    Beekwilder, M.J.; Meer, van der I.M.; Sibbesen, O.; Broekgaarden, M.; Qvist, I.; Mikkelsen, J.D.; Hall, R.D.

    2007-01-01

    Raspberry ketone is an important compound for the flavour industry. It is frequently used in products such as soft drinks, sweets, puddings and ice creams. The compound can be produced by organic synthesis. Demand for natural raspberry ketone is growing considerably. However, this product is extreme

  5. Natural product discovery: past, present, and future.

    Science.gov (United States)

    Katz, Leonard; Baltz, Richard H

    2016-03-01

    Microorganisms have provided abundant sources of natural products which have been developed as commercial products for human medicine, animal health, and plant crop protection. In the early years of natural product discovery from microorganisms (The Golden Age), new antibiotics were found with relative ease from low-throughput fermentation and whole cell screening methods. Later, molecular genetic and medicinal chemistry approaches were applied to modify and improve the activities of important chemical scaffolds, and more sophisticated screening methods were directed at target disease states. In the 1990s, the pharmaceutical industry moved to high-throughput screening of synthetic chemical libraries against many potential therapeutic targets, including new targets identified from the human genome sequencing project, largely to the exclusion of natural products, and discovery rates dropped dramatically. Nonetheless, natural products continued to provide key scaffolds for drug development. In the current millennium, it was discovered from genome sequencing that microbes with large genomes have the capacity to produce about ten times as many secondary metabolites as was previously recognized. Indeed, the most gifted actinomycetes have the capacity to produce around 30-50 secondary metabolites. With the precipitous drop in cost for genome sequencing, it is now feasible to sequence thousands of actinomycete genomes to identify the "biosynthetic dark matter" as sources for the discovery of new and novel secondary metabolites. Advances in bioinformatics, mass spectrometry, proteomics, transcriptomics, metabolomics and gene expression are driving the new field of microbial genome mining for applications in natural product discovery and development.

  6. Using Genomics for Natural Product Structure Elucidation.

    Science.gov (United States)

    Tietz, Jonathan I; Mitchell, Douglas A

    2016-01-01

    Natural products (NPs) are the most historically bountiful source of chemical matter for drug development-especially for anti-infectives. With insights gleaned from genome mining, interest in natural product discovery has been reinvigorated. An essential stage in NP discovery is structural elucidation, which sheds light not only on the chemical composition of a molecule but also its novelty, properties, and derivatization potential. The history of structure elucidation is replete with techniquebased revolutions: combustion analysis, crystallography, UV, IR, MS, and NMR have each provided game-changing advances; the latest such advance is genomics. All natural products have a genetic basis, and the ability to obtain and interpret genomic information for structure elucidation is increasingly available at low cost to non-specialists. In this review, we describe the value of genomics as a structural elucidation technique, especially from the perspective of the natural product chemist approaching an unknown metabolite. Herein we first introduce the databases and programs of interest to the natural products chemist, with an emphasis on those currently most suited for general usability. We describe strategies for linking observed natural product-linked phenotypes to their corresponding gene clusters. We then discuss techniques for extracting structural information from genes, illustrated with numerous case examples. We also provide an analysis of the biases and limitations of the field with recommendations for future development. Our overview is not only aimed at biologically-oriented researchers already at ease with bioinformatic techniques, but also, in particular, at natural product, organic, and/or medicinal chemists not previously familiar with genomic techniques.

  7. MARMARONIA ANGIOLINII, NEW GENUS AND NEW SPECIES OF BAKEVELLIIDAE (PTERIOIDA, BIVALVIA FROM THE MIDDLE PERMIAN OF CHIOS (GREECE

    Directory of Open Access Journals (Sweden)

    CRISTIANO LARGHI

    2002-11-01

    Full Text Available The Guadalupian (Middle Permian "Gymnocodiacean Limestones" cropping out in the north-eastern part of the Greek island of Chios (eastern Aegean Sea are amongst the most fossiliferous in the western Tethys. They contain rich assemblages of corals, brachiopods, molluscs, calcareous algae, foraminifers and ostracods. Scant attention was given till now to mollusc faunas compared with brachiopods and foraminifers. In the present paper the new genus Marmaronia, with type-species M. angiolinii n. sp., is established to distinguish some bivalves of the Bakevelliidae King, 1850, from the middle Guadalupian successions of the Marmaro locality in Chios Island. M. angiolinii n. gen. n. sp. is strongly inequivalve, with valves differing in convexity, umbo development and ornamentation. The left valve shows a radial furrow running from the anterior part of the umbonal region anteroventrally and is ornamented by strong radial costae; the right valve is ornamented by concentric sculpture and by thin rugae in the first growth stages of the posterior part of the shell. Both valves have a wide posterior wing. Two hypotheses concerning the epi- or endobyssate adaptation of Marmaronia are also discussed briefly in the present paper.   

  8. Psychoactive natural products: overview of recent developments

    Directory of Open Access Journals (Sweden)

    István Ujváry

    2014-03-01

    Full Text Available Natural psychoactive substances have fascinated the curious mind of shamans, artists, scholars and laymen since antiquity. During the twentieth century, the chemical composition of the most important psychoactive drugs, that is opium, cannabis, coca and "magic mushrooms", has been fully elucidated. The mode of action of the principal ingredients has also been deciphered at the molecular level. In the past two decades, the use of herbal drugs, such as kava, kratom and Salvia divinorum, began to spread beyond their traditional geographical and cultural boundaries. The aim of the present paper is to briefly summarize recent findings on the psychopharmacology of the most prominent psychoactive natural products. Current knowledge on a few lesser-known drugs, including bufotenine, glaucine, kava, betel, pituri, lettuce opium and kanna is also reviewed. In addition, selected cases of alleged natural (or semi-natural products are also mentioned.

  9. Psychoactive natural products: overview of recent developments.

    Science.gov (United States)

    Ujváry, István

    2014-01-01

    Natural psychoactive substances have fascinated the curious mind of shamans, artists, scholars and laymen since antiquity. During the twentieth century, the chemical composition of the most important psychoactive drugs, that is opium, cannabis, coca and "magic mushrooms", has been fully elucidated. The mode of action of the principal ingredients has also been deciphered at the molecular level. In the past two decades, the use of herbal drugs, such as kava, kratom and Salvia divinorum, began to spread beyond their traditional geographical and cultural boundaries. The aim of the present paper is to briefly summarize recent findings on the psychopharmacology of the most prominent psychoactive natural products. Current knowledge on a few lesser-known drugs, including bufotenine, glaucine, kava, betel, pituri, lettuce opium and kanna is also reviewed. In addition, selected cases of alleged natural (or semi-natural) products are also mentioned.

  10. Review: Natural products from Genus Selaginella (Selaginellaceae

    Directory of Open Access Journals (Sweden)

    AHMAD DWI SETYAWAN

    2011-01-01

    Full Text Available Setyawan AD. 2011. Natural products from Genus Selaginella (Selaginellaceae. Nusantara Bioscience 3: 44-58. Selaginella is a potent medicinal-stuff, which contains diverse of natural products such as alkaloid, phenolic (flavonoid, and terpenoid. This species is traditionally used to cure several diseases especially for wound, after childbirth, and menstrual disorder. Biflavonoid, a dimeric form of flavonoids, is the most valuable natural products of Selaginella, which constituted at least 13 compounds, namely amentoflavone, 2',8''-biapigenin, delicaflavone, ginkgetin, heveaflavone, hinokiflavone, isocryptomerin, kayaflavone, ochnaflavone, podocarpusflavone A, robustaflavone, sumaflavone, and taiwaniaflavone. Ecologically, plants use biflavonoid to response environmental condition such as defense against pests, diseases, herbivory, and competitions; while human medically use biflavonoid especially for antioxidant, anti-inflammatory, and anti carcinogenic. Selaginella also contains valuable disaccharide, namely trehalose that has long been known for protecting from desiccation and allows surviving severe environmental stress. The compound has very prospects as molecular stabilizer in the industries based bioresources.

  11. Countercurrent Separation of Natural Products: An Update

    Science.gov (United States)

    2015-01-01

    This work assesses the current instrumentation, method development, and applications in countercurrent chromatography (CCC) and centrifugal partition chromatography (CPC), collectively referred to as countercurrent separation (CCS). The article provides a critical review of the CCS literature from 2007 since our last review (J. Nat. Prod.2008, 71, 1489–1508), with a special emphasis on the applications of CCS in natural products research. The current state of CCS is reviewed in regard to three continuing topics (instrumentation, solvent system development, theory) and three new topics (optimization of parameters, workflow, bioactivity applications). The goals of this review are to deliver the necessary background with references for an up-to-date perspective of CCS, to point out its potential for the natural product scientist, and thereby to induce new applications in natural product chemistry, metabolome, and drug discovery research involving organisms from terrestrial and marine sources. PMID:26177360

  12. Early State Research on Antifungal Natural Products

    Directory of Open Access Journals (Sweden)

    Melyssa Negri

    2014-03-01

    Full Text Available Nosocomial infections caused by fungi have increased greatly in recent years, mainly due to the rising number of immunocompromised patients. However, the available antifungal therapeutic arsenal is limited, and the development of new drugs has been slow. Therefore, the search for alternative drugs with low resistance rates and fewer side effects remains a major challenge. Plants produce a variety of medicinal components that can inhibit pathogen growth. Studies of plant species have been conducted to evaluate the characteristics of natural drug products, including their sustainability, affordability, and antimicrobial activity. A considerable number of studies of medicinal plants and alternative compounds, such as secondary metabolites, phenolic compounds, essential oils and extracts, have been performed. Thus, this review discusses the history of the antifungal arsenal, surveys natural products with potential antifungal activity, discusses strategies to develop derivatives of natural products, and presents perspectives on the development of novel antifungal drug candidates.

  13. Anti-Inflammatory Activity of Natural Products

    Directory of Open Access Journals (Sweden)

    Abdullatif Azab

    2016-10-01

    Full Text Available This article presents highlights of the published literature regarding the anti-inflammatory activities of natural products. Many review articles were published in this regard, however, most of them have presented this important issue from a regional, limited perspective. This paper summarizes the vast range of review and research articles that have reported on the anti-inflammatory effects of extracts and/or pure compounds derived from natural products. Moreover, this review pinpoints some interesting traditionally used medicinal plants that were not investigated yet.

  14. An automated Genomes-to-Natural Products platform (GNP) for the discovery of modular natural products.

    Science.gov (United States)

    Johnston, Chad W; Skinnider, Michael A; Wyatt, Morgan A; Li, Xiang; Ranieri, Michael R M; Yang, Lian; Zechel, David L; Ma, Bin; Magarvey, Nathan A

    2015-09-28

    Bacterial natural products are a diverse and valuable group of small molecules, and genome sequencing indicates that the vast majority remain undiscovered. The prediction of natural product structures from biosynthetic assembly lines can facilitate their discovery, but highly automated, accurate, and integrated systems are required to mine the broad spectrum of sequenced bacterial genomes. Here we present a genome-guided natural products discovery tool to automatically predict, combinatorialize and identify polyketides and nonribosomal peptides from biosynthetic assembly lines using LC-MS/MS data of crude extracts in a high-throughput manner. We detail the directed identification and isolation of six genetically predicted polyketides and nonribosomal peptides using our Genome-to-Natural Products platform. This highly automated, user-friendly programme provides a means of realizing the potential of genetically encoded natural products.

  15. Plants as natural antioxidants for meat products

    Science.gov (United States)

    Tomović, V.; Jokanović, M.; Šojić, B.; Škaljac, S.; Ivić, M.

    2017-09-01

    The meat industry is demanding antioxidants from natural sources to replace synthetic antioxidants because of the negative health consequences or beliefs regarding some synthetic ones. Plants materials provide good alternatives. Spices and herbs, generally used for their flavouring characteristics, can be added to meat products in various forms: whole, ground, or as isolates from their extracts. These natural antioxidants contain some active compounds, which exert antioxidative potential in meat products. This antioxidant activity is most often due to phenolic acids, phenolic diterpenes, flavonoids and volatile oils. Each of these compounds often has strong H-donating activity, thus making them extremely effective antioxidants; some compounds can chelate metals and donate H to oxygen radicals, thus slowing oxidation via two mechanisms. Numerous studies have demonstrated the efficacy of natural antioxidants when used in meat products. Based on this literature review, it can be concluded that natural antioxidants are added to fresh and processed meat and meat products to delay, retard, or prevent lipid oxidation, retard development of off-flavours (rancidity), improve colour stability, improve microbiological quality and extend shelf-life, without any damage to the sensory or nutritional properties.

  16. Chocolate: A Marvelous Natural Product of Chemistry

    Science.gov (United States)

    Tannenbaum, Ginger

    2004-01-01

    The study of chocolate, a natural product, can be beneficial for the chemistry students as they ask frequently about the relevancy of their chemistry classes. The history of chocolate, its chemical and physical changes during processing, its composition, different crystalline forms, tempering and its viscosity are discussed.

  17. Standardization for natural product synthetic biology

    NARCIS (Netherlands)

    Zhao, Huimin; Medema, Marnix H.

    2016-01-01

    Standardization is one of the foundational features of modern-day engineering, and the use of standardized parts and processes is a key element that distinguishes bona fide synthetic biology from traditional genetic engineering. Here, we discuss the role of standardization in natural product

  18. Marine natural products as prototype agrochemical agents.

    Science.gov (United States)

    Peng, Jiangnan; Shen, Xiaoyu; El Sayed, Khalid A; Dunbar, D Charles; Perry, Tony L; Wilkins, Scott P; Hamann, Mark T; Bobzin, Steve; Huesing, Joseph; Camp, Robin; Prinsen, Mike; Krupa, Dan; Wideman, Margaret A

    2003-04-09

    In the interest of identifying new leads that could serve as prototype agrochemical agents, 18 structurally diverse marine-derived compounds were examined for insecticidal, herbicidal, and fungicidal activities. Several new classes of compounds have been shown to be insecticidal, herbicidal, and fungicidal, which suggests that marine natural products represent an intriguing source for the discovery of new agrochemical agents.

  19. Marine Natural Products as Prototype Agrochemical Agents

    OpenAIRE

    Peng, Jiangnan; Shen, Xiaoyu; Khalid A. El Sayed; Dunbar, D. C Harles; Perry, Tony L.; Wilkins, Scott P.; Hamann, Mark T.; Bobzin, Steve; Huesing, Joseph; Camp, Robin; Prinsen, Mike; Krupa, Dan; Wideman, Margaret A.

    2003-01-01

    In the interest of identifying new leads that could serve as prototype agrochemical agents, 18 structurally diverse marine-derived compounds were examined for insecticidal, herbicidal, and fungicidal activities. Several new classes of compounds have been shown to be insecticidal, herbicidal, and fungicidal, which suggests that marine natural products represent an intriguing source for the discovery of new agrochemical agents.

  20. Natural products – learning chemistry from plants

    NARCIS (Netherlands)

    Staniek, A.; Bouwmeester, H.J.; Fraser, P.D.; Kayser, O.; Martens, S.; Tissier, A.; Krol, van der A.R.; Wessjohann, L.; Warzecha, H.

    2014-01-01

    Plant natural products (PNPs) are unique in that they represent a vast array of different structural features, ranging from relatively simple molecules to very complex ones. Given the fact that many plant secondary metabolites exhibit profound biological activity, they are frequently used as

  1. Natural products – learning chemistry from plants

    NARCIS (Netherlands)

    Staniek, A.; Bouwmeester, H.J.; Fraser, P.D.; Kayser, O.; Martens, S.; Tissier, A.; Krol, van der A.R.; Wessjohann, L.; Warzecha, H.

    2014-01-01

    Plant natural products (PNPs) are unique in that they represent a vast array of different structural features, ranging from relatively simple molecules to very complex ones. Given the fact that many plant secondary metabolites exhibit profound biological activity, they are frequently used as fragran

  2. Natural products from microbes associated with insects

    DEFF Research Database (Denmark)

    Beemelmanns, Christine; Guo, Huijuan; Rischer, Maja;

    2016-01-01

    Here we review discoveries of secondary metabolites from microbes associated with insects. We mainly focus on natural products, where the ecological role has been at least partially elucidated, and/or the pharmaceutical properties evaluated, and on compounds with unique structural features. We...

  3. Computational approaches to natural product discovery

    NARCIS (Netherlands)

    Medema, M.H.; Fischbach, M.A.

    2015-01-01

    Starting with the earliest Streptomyces genome sequences, the promise of natural product genome mining has been captivating: genomics and bioinformatics would transform compound discovery from an ad hoc pursuit to a high-throughput endeavor. Until recently, however, genome mining has advanced natura

  4. Flow chemistry syntheses of natural products.

    Science.gov (United States)

    Pastre, Julio C; Browne, Duncan L; Ley, Steven V

    2013-12-07

    The development and application of continuous flow chemistry methods for synthesis is a rapidly growing area of research. In particular, natural products provide demanding challenges to this developing technology. This review highlights successes in the area with an emphasis on new opportunities and technological advances.

  5. Natural products in modern life science.

    Science.gov (United States)

    Bohlin, Lars; Göransson, Ulf; Alsmark, Cecilia; Wedén, Christina; Backlund, Anders

    2010-06-01

    With a realistic threat against biodiversity in rain forests and in the sea, a sustainable use of natural products is becoming more and more important. Basic research directed against different organisms in Nature could reveal unexpected insights into fundamental biological mechanisms but also new pharmaceutical or biotechnological possibilities of more immediate use. Many different strategies have been used prospecting the biodiversity of Earth in the search for novel structure-activity relationships, which has resulted in important discoveries in drug development. However, we believe that the development of multidisciplinary incentives will be necessary for a future successful exploration of Nature. With this aim, one way would be a modernization and renewal of a venerable proven interdisciplinary science, Pharmacognosy, which represents an integrated way of studying biological systems. This has been demonstrated based on an explanatory model where the different parts of the model are explained by our ongoing research. Anti-inflammatory natural products have been discovered based on ethnopharmacological observations, marine sponges in cold water have resulted in substances with ecological impact, combinatory strategy of ecology and chemistry has revealed new insights into the biodiversity of fungi, in depth studies of cyclic peptides (cyclotides) has created new possibilities for engineering of bioactive peptides, development of new strategies using phylogeny and chemography has resulted in new possibilities for navigating chemical and biological space, and using bioinformatic tools for understanding of lateral gene transfer could provide potential drug targets. A multidisciplinary subject like Pharmacognosy, one of several scientific disciplines bridging biology and chemistry with medicine, has a strategic position for studies of complex scientific questions based on observations in Nature. Furthermore, natural product research based on intriguing scientific

  6. Natural production of biological optical systems

    Science.gov (United States)

    Choi, Seung Ho; Kim, Young L.

    2015-03-01

    Synthesis and production in nature often provide ideas to design and fabricate advanced biomimetic photonic materials and structures, leading to excellent physical properties and enhanced performance. In addition, the recognition and utilization of natural or biological substances have been typical routes to develop biocompatible and biodegradable materials for medical applications. In this respect, biological lasers utilizing such biomaterials and biostructures have been received considerable attention, given a variety of implications and potentials for bioimaging, biosensing, implantation, and therapy. However, without relying on industrial facilities, eco-friendly massive production of such optical components or systems has not yet been investigated. We show examples of bioproduction of biological lasers using agriculture and fisheries. We anticipate that such approaches will open new possibilities for scalable eco-friendly `green' production of biological photonics components and systems.

  7. [Status of libraries and databases for natural products at abroad].

    Science.gov (United States)

    Zhao, Li-Mei; Tan, Ning-Hua

    2015-01-01

    For natural products are one of the important sources for drug discovery, libraries and databases of natural products are significant for the development and research of natural products. At present, most of compound libraries at abroad are synthetic or combinatorial synthetic molecules, resulting to access natural products difficult; for information of natural products are scattered with different standards, it is difficult to construct convenient, comprehensive and large-scale databases for natural products. This paper reviewed the status of current accessing libraries and databases for natural products at abroad and provided some important information for the development of libraries and database for natural products.

  8. Automated genome mining for natural products

    Directory of Open Access Journals (Sweden)

    Zajkowski James

    2009-06-01

    Full Text Available Abstract Background Discovery of new medicinal agents from natural sources has largely been an adventitious process based on screening of plant and microbial extracts combined with bioassay-guided identification and natural product structure elucidation. Increasingly rapid and more cost-effective genome sequencing technologies coupled with advanced computational power have converged to transform this trend toward a more rational and predictive pursuit. Results We have developed a rapid method of scanning genome sequences for multiple polyketide, nonribosomal peptide, and mixed combination natural products with output in a text format that can be readily converted to two and three dimensional structures using conventional software. Our open-source and web-based program can assemble various small molecules composed of twenty standard amino acids and twenty two other chain-elongation intermediates used in nonribosomal peptide systems, and four acyl-CoA extender units incorporated into polyketides by reading a hidden Markov model of DNA. This process evaluates and selects the substrate specificities along the assembly line of nonribosomal synthetases and modular polyketide synthases. Conclusion Using this approach we have predicted the structures of natural products from a diverse range of bacteria based on a limited number of signature sequences. In accelerating direct DNA to metabolomic analysis, this method bridges the interface between chemists and biologists and enables rapid scanning for compounds with potential therapeutic value.

  9. Regulation of natural health products in Canada.

    Science.gov (United States)

    Smith, Alysyn; Jogalekar, Sumedha; Gibson, Adam

    2014-12-02

    In Canada, all natural health products (NHPs) are regulated by Health Canada (HC) under the Food and Drugs Act and the Natural Health Product Regulations. All authorized products undergo pre-market assessment for safety, efficacy and quality and the degree of pre-market oversight varies depending on the risk of the product. In Canada, over 70,000 products have been authorized for sale and over 2000 sites have been licensed to produce NHPs. In the management of NHPs on the Canadian market, HC employs a number of active and collaborative methods to address the most common issues such as contamination, adulteration and deceptive or misleading advertising practices. HC is currently evolving its approaches to NHPs to recognize them as part of the larger group of health products available without a prescription. As such, the regulatory responsibility for all over-the-counter (OTC) drugs, including non-prescription drugs and NHPs, has been transferred to a single federal division. As a result of this transition a number of benefits are being realized with respect to government efficiency, clarity for industry, support for new innovations and consolidated government interactions with the Canadian market. Copyright © 2014 Elsevier Ireland Ltd. All rights reserved.

  10. In silico Design of "Un-Natural" Natural Products

    Directory of Open Access Journals (Sweden)

    Zucko; J. ...(et al.

    2008-05-01

    Full Text Available Polyketides and non-ribosomal peptides represent a large class of structurally diverse natural products much studied over recent years because the enzymes that synthesise them, the modular polyketide synthases (PKSs and the non-ribosomal peptide synthetases (NRPSs, share striking architectural similarities that can be exploited to generate "un-natural" natural products. PKS and NRPS proteins are multifunctional, composed of a co-linear arrangement of discrete protein domains representing each enzymic activity needed for chain elongation using either carboxylic acid or amino acid building blocks. Each domain is housed within larger modules which form the complex. Polyketide and peptide antibiotics, antifungals, antivirals, cytostatics, immunosuppressants, antihypertensives, antidiabetics, antimalarials and anticholesterolemics are in clinical use. Of commercial importance are also polyketide and peptide antiparasitics, coccidiostatics,animal growth promoters and natural insecticides.Polyketides are assembled through serial condensations of activated coenzyme-A thioester monomers derived from simple organic acids such as acetate, propionate and butyrate. The choice of organic acid allows the introduction of different chiral centres into the polyketide backbone. The active sites required for condensation include an acyltransferase (AT, an acyl carrier protein (ACP and a ß-ketoacylsynthase (KS. Each condensation results in a ß-keto group that undergoes all, some or none of a series of processing steps. Active sites that perform these reactions are contained within the following domains; ketoreductase (KR, dehydratase (DH and an enoylreductase (ER. The absence of any ß-keto processing results in the incorporation of a ketone group into the growing polyketide chain, a KR alone gives rise to a hydroxyl moiety, a KR and DH produce an alkene, while the combination of KR, DH and ER domains lead to complete reduction to an alkane. Most often, the last

  11. Utilization of Natural Products as Functional Feed

    Directory of Open Access Journals (Sweden)

    Stella Magdalena

    2013-03-01

    Full Text Available The use of antibiotics as feed additive improves performance in livestock. However, scientific data related to the use of antibiotics in feed merge spreading of bacterial resistance in animal and human bodies, therefore the usage of antibiotics in animal production is restricted. This condition raise the utilization of natural antibiotic as functional feed such as phytogenics (essential oil, flavonoid, saponin, and tannin, enzyme, probiotic, and prebiotic to improve the livestock’s performance, quality, and health. Functional feeds increase profitability in animal husbandry production and its use is feeds are expected to be functional foods that may have positive effects in human nutrition.

  12. (+-Discodermolide: A Marine Natural Product Against Cancer

    Directory of Open Access Journals (Sweden)

    Marcus Viníus Nora De Souza

    2004-01-01

    Full Text Available (+-Discodermolide was isolated in 1990 by Gunasekera et al. from the deep-water Caribbean sponge Discodermia dissoluta. It attacks cancer cells in a similar way to the successful cancer drug Taxol® that has become the best-selling anticancer drug in history. Taxol is also the first natural product described that stabilizes the microtubules involved in many aspects of cellular biology and that represent an important target of anticancer chemotherapeutics. However, (+-discodermolide appears to be far more potent than Taxol® against tumors that have developed multiple-drug resistance, with an IC50 in the low nanomolar range. Due to these excellent results, this natural product was licensed to Novartis Pharmaceutical Corporation in early 1998. The present review covers the history, biological activity, total synthesis, and synthetic analogs of (+-discodermolide.

  13. Trypanocidal Activity of Marine Natural Products

    Directory of Open Access Journals (Sweden)

    Amy J. Jones

    2013-10-01

    Full Text Available Marine natural products are a diverse, unique collection of compounds with immense therapeutic potential. This has resulted in these molecules being evaluated for a number of different disease indications including the neglected protozoan diseases, human African trypanosomiasis and Chagas disease, for which very few drugs are currently available. This article will review the marine natural products for which activity against the kinetoplastid parasites; Trypanosoma brucei brucei, T.b. rhodesiense and T. cruzi has been reported. As it is important to know the selectivity of a compound when evaluating its trypanocidal activity, this article will only cover molecules which have simultaneously been tested for cytotoxicity against a mammalian cell line. Compounds have been grouped according to their chemical structure and representative examples from each class were selected for detailed discussion.

  14. (+)-discodermolide: a marine natural product against cancer.

    Science.gov (United States)

    De Souza, Marcus Vinícius Nora

    2004-06-11

    (+)-discodermolide was isolated in 1990 by Gunasekera et al. from the deep-water Caribbean sponge Discodermia dissoluta. It attacks cancer cells in a similar way to the successful cancer drug Taxol that has become the best-selling anticancer drug in history. Taxol is also the first natural product described that stabilizes the microtubules involved in many aspects of cellular biology and that represent an important target of anticancer chemotherapeutics. However, (+)-discodermolide appears to be far more potent than Taxol against tumors that have developed multiple-drug resistance, with an IC50 in the low nanomolar range. Due to these excellent results, this natural product was licensed to Novartis Pharmaceutical Corporation in early 1998. The present review covers the history, biological activity, total synthesis, and synthetic analogs of (+)-discodermolide.

  15. Synthetic biological approaches to natural product biosynthesis.

    Science.gov (United States)

    Winter, Jaclyn M; Tang, Yi

    2012-10-01

    Small molecules produced in Nature possess exquisite chemical diversity and continue to be an inspiration for the development of new therapeutic agents. In their host organisms, natural products are assembled and modified using dedicated biosynthetic pathways. By rationally reprogramming and manipulating these pathways, unnatural metabolites containing enhanced structural features that were otherwise inaccessible can be obtained. Additionally, new chemical entities can be synthesized by developing the enzymes that carry out these complicated chemical reactions into biocatalysts. In this review, we will discuss a variety of combinatorial biosynthetic strategies, their technical challenges, and highlight some recent (since 2007) examples of rationally designed metabolites, as well as platforms that have been established for the production and modification of clinically important pharmaceutical compounds.

  16. Standardization for natural product synthetic biology.

    Science.gov (United States)

    Zhao, Huimin; Medema, Marnix H

    2016-08-27

    Standardization is one of the foundational features of modern-day engineering, and the use of standardized parts and processes is a key element that distinguishes bona fide synthetic biology from traditional genetic engineering. Here, we discuss the role of standardization in natural product synthetic biology, focusing on standardization of data on biosynthetic pathways and gene clusters, as well as the role of standardization in the process of biosynthetic gene cluster engineering.

  17. Natural Products as Sources for New Pesticides

    Science.gov (United States)

    2012-05-22

    A number of bio - chemical herbicides have been registered with the EPA since 1997. Horticultural vinegar, which consists of diluted aqueous solutions...However, this has not been the case for herbicides . Only one class of natural product-derived herbicide has been registered since 1997, namely, the...triketone herbicides . The discovery and development of these herbicides followed a fairly convoluted path that began in 1977 when Reed Gray at

  18. Natural cold pressed oils as cosmetic products

    Directory of Open Access Journals (Sweden)

    Małgorzata Ligęza

    2016-12-01

    Full Text Available Background. It seems that patients may ask general practitioners about natural cosmetics applied on the skin regarding their safety and suitability. Objectives. The aim of the study was to analyze natural cold pressed oils as potential cosmetic products. Material and methods. Cold pressed oils obtained from selected seeds and fruit stones were analyzed, including: chokeberry seed oil, blackcurrant seed oil, elderberry seed oil, raspberry seed oil, apricot seed oil, tomato seed oil, strawberry seed oil, broccoli seed oil, Nigella sativa seed oil, hemp oil, safflower seed oil, Silybum marianum seed oil and coconut oil. 80 adult volunteers assessed the cosmetic properties of the analyzed oils. Each of the volunteers tested 2 to 4 different oils, by applying them on the skin. In addition, patch tests with all analyzed oils were performed on 23 individuals. Results. The majority of tested oils were positively evaluated by the participants: in the opinion of the participants, oil extracted from safflower had the best appearance (100% positive opinions, coconut oil had the best smell (70% positive opinions, while black currant seed oil showed the best absorbency (85% positive opinions. No irritation was observed within the analyzed product group, albeit one allergic reaction to apricot seed oil was observed with patch testing. Conclusions . Based on the achieved results, it could be suggested that natural cold pressed oils can be applied to the skin as cosmetics. Our observations may be helpful for general practitioners when choosing natural cosmetics.

  19. Natural products from filamentous fungi and production by heterologous expression.

    Science.gov (United States)

    Alberti, Fabrizio; Foster, Gary D; Bailey, Andy M

    2017-01-01

    Filamentous fungi represent an incredibly rich and rather overlooked reservoir of natural products, which often show potent bioactivity and find applications in different fields. Increasing the naturally low yields of bioactive metabolites within their host producers can be problematic, and yield improvement is further hampered by such fungi often being genetic intractable or having demanding culturing conditions. Additionally, total synthesis does not always represent a cost-effective approach for producing bioactive fungal-inspired metabolites, especially when pursuing assembly of compounds with complex chemistry. This review aims at providing insights into heterologous production of secondary metabolites from filamentous fungi, which has been established as a potent system for the biosynthesis of bioactive compounds. Numerous advantages are associated with this technique, such as the availability of tools that allow enhanced production yields and directing biosynthesis towards analogues of the naturally occurring metabolite. Furthermore, a choice of hosts is available for heterologous expression, going from model unicellular organisms to well-characterised filamentous fungi, which has also been shown to allow the study of biosynthesis of complex secondary metabolites. Looking to the future, fungi are likely to continue to play a substantial role as sources of new pharmaceuticals and agrochemicals-either as producers of novel natural products or indeed as platforms to generate new compounds through synthetic biology.

  20. Isolation of bioactive natural products from myxomycetes.

    Science.gov (United States)

    Ishibashi, Masami

    2005-11-01

    The Myxomycetes (true slime molds) are an unusual group of primitive organisms that may be assigned to one of the lowest classes of eukaryotes. As their fruit bodies are very small and it is very difficult to collect much quantity of slime molds, few studies have been made on the chemistry of myxomycetes. Cultivation of the plasmodium of myxomycetes in a practical scale for natural products chemistry studies is known only for very limited species. Here is described a review on the recent results on isolation of bioactive natural products from myxomycetes obtained in these two years in the laboratories. Spore germination experiments were studied of hundreds of field-collected myxomycetes collected in Japan and succeeded in laboratory culture of plasmodia of several myxomycetes in a practical scale for natural products chemistry studies. As a result, pyrroloiminoquinones, polyene yellow pigments, and a peptide lactone from cultured plasmodia of Didymium iridis, Physarum rigidum and P. melleum, respectively were isolated. New naphthoquinone pigments, cycloanthranilylprolines, tyrosine-kinase inhibitory bisindoles, and a cytotoxic triterpenoid aldehyde lactone were also isolated from field-collected fruit bodies of Cribraria purpurea, Fuligo candida, Tubifera casparyi, and Tubifera dimorphotheca, respectively.

  1. Natural and Heterologous Production of Bacteriocins

    Science.gov (United States)

    Cintas, Luis M.; Herranz, Carmen; Hernández, Pablo E.

    Bacteriocins are ribosomally synthesized antimicrobial peptides produced by bacteria, and their use as natural and nontoxic food preservatives has been the source of considerable interest for the research community. In addition, bacteriocins have been investigated for their potential use in human and veterinary applications and in the animal production field. In the native bacterial strain, most bacteriocins are synthesized as biologically inactive precursors, with N-terminal extensions, that are cleaved concomitantly during export of the bacteriocin by dedicated ABC transporters, or the general secretory pathway (GSP) or Sec-dependent pathway. However, a few bacteriocins are synthesized without an N-terminal extension, and others are circularized through a head-to-tail peptide bond, complicating the elucidation of their processing and transport across the cytoplasmic membrane. The high cost of synthetic bacteriocin synthesis and their low yields from many natural producers recommends the exploration of recombinant microbial systems for the heterologous production of bacteriocins. Other advantages of such systems include production of bacteriocins in safer hosts, increased bacteriocin production, control of bacteriocin gene expression, production of food ingredients with antimicrobial activity, construction of multibacteriocinogenic strains with a wider antagonistic spectrum, a better adaptation of the selected hosts to food environments, and providing antagonistic properties to lactic acid bacteria (LAB) used as starter, protective, or probiotic cultures. The recombinant production of bacteriocins mostly relies on the use of expression vectors that replicate in Gram-negative bacteria, Gram-positive bacteria, and yeasts, whereas the production of bacteriocins in heterologous LAB hosts may be essentially based on the expression of native biosynthetic genes, by exchanging or replacing leader peptides and/or dedicated processing and secretion systems (ABC transporters

  2. Natural products as potential anticonvulsants: caffeoylquinic acids.

    Science.gov (United States)

    Kim, Hyo Geun; Oh, Myung Sook

    2012-03-01

    Current anticonvulsant therapies are generally directed at symptomatic treatment by suppressing excitability within the brain. Consequently, they have adverse effects such as cognitive impairment, dependence, and abuse. The need for more effective and less toxic anticonvulsants has generated renewed interest in natural products for the treatment of convulsions. Caffeoylquinic acids (CQs) are naturally occurring phenolic acids that are distributed widely in plants. There has been increasing interest in the biological activities of CQs in diseases of the central nervous system. In this issue, Nugroho et al. give evidence for the anticonvulsive effect of a CQ-rich extract from Aster glehni Franchet et Sckmidt. They optimized the extract solvent conditions, resulting in high levels of CQs and peroxynitrite-scavenging activity. Then, they investigated the sedative and anticonvulsive effects in pentobarbital- and pentylenetetrazole-induced models in mice. The CQ-rich extract significantly inhibited tonic convulsions as assessed by onset time, tonic extent, and mortality. They suggested that the CQ-rich extract from A. glehni has potential for treating convulsions. This report provides preclinical data which may be used for the development of anticonvulsants from natural products.

  3. An Improved Synthesis of the Natural Product Isorhapontigenin

    Institute of Scientific and Technical Information of China (English)

    2000-01-01

    We have developed an alternative route to synthesize the natural product, isorhapotogenin . The synthetic product was characterized by IR and 1H-NMR in comparison with the corresponding natural product.

  4. Phylogenetic approaches to natural product structure prediction.

    Science.gov (United States)

    Ziemert, Nadine; Jensen, Paul R

    2012-01-01

    Phylogenetics is the study of the evolutionary relatedness among groups of organisms. Molecular phylogenetics uses sequence data to infer these relationships for both organisms and the genes they maintain. With the large amount of publicly available sequence data, phylogenetic inference has become increasingly important in all fields of biology. In the case of natural product research, phylogenetic relationships are proving to be highly informative in terms of delineating the architecture and function of the genes involved in secondary metabolite biosynthesis. Polyketide synthases and nonribosomal peptide synthetases provide model examples in which individual domain phylogenies display different predictive capacities, resolving features ranging from substrate specificity to structural motifs associated with the final metabolic product. This chapter provides examples in which phylogeny has proven effective in terms of predicting functional or structural aspects of secondary metabolism. The basics of how to build a reliable phylogenetic tree are explained along with information about programs and tools that can be used for this purpose. Furthermore, it introduces the Natural Product Domain Seeker, a recently developed Web tool that employs phylogenetic logic to classify ketosynthase and condensation domains based on established enzyme architecture and biochemical function.

  5. Microbial production of natural raspberry ketone.

    Science.gov (United States)

    Beekwilder, Jules; van der Meer, Ingrid M; Sibbesen, Ole; Broekgaarden, Mans; Qvist, Ingmar; Mikkelsen, Joern D; Hall, Robert D

    2007-10-01

    Raspberry ketone is an important compound for the flavour industry. It is frequently used in products such as soft drinks, sweets, puddings and ice creams. The compound can be produced by organic synthesis. Demand for "natural" raspberry ketone is growing considerably. However, this product is extremely expensive. Consequently, there is a remaining desire to better understand how raspberry ketone is synthesized in vivo, and which genes and enzymes are involved. With this information we will then be in a better position to design alternative production strategies such as microbial fermentation. This article focuses on the identification and application of genes potentially linked to raspberry ketone synthesis. We have isolated candidate genes from both raspberry and other plants, and these have been introduced into bacterial and yeast expression systems. Conditions have been determined that result in significant levels of raspberry ketone, up to 5 mg/L. These results therefore lay a strong foundation for a potentially renewable source of "natural" flavour compounds making use of plant genes.

  6. Natural products research in latin america.

    Science.gov (United States)

    Gupta, M P

    2001-01-01

    The biodiversity found in Latin America is one of the richest in the world, yet its potential as a source of new pharmaceuticals has not been fully investigated. This paper will explore the present status of natural products research in 19 Latin American countries. Future research needs will be presented along with reports on the ethnobotanical and bioprospection projects under way in Latin America. The presentation will be based on data collected over the last five years and will be presented within the framework of the Fine Pharmaceutical Subprogram of the Iberoamerican Program of Science and Technology for Development (CYTED), a novel international cooperation program.

  7. The Rakicidin Family of Anticancer Natural Products

    DEFF Research Database (Denmark)

    Tsakos, Michail; Jacobsen, Kristian Mark; Yu, Wanwan

    2016-01-01

    Rakicidin A is a prominent member of a small class of macrocyclic lipodepsipeptide natural products that contain an electrophilic 4- amido-2,4-pentadienoate (APD) functionality. Rakicidin A displays selective growth inhibitory activity against hypoxic cancer cells as well as imatinib......-resistant chronic myelogenous leukemia (CML) cells. In this paper we present and discuss the two known synthetic routes to rakicidin A, which provide an instructive comparison of strategies used to address the synthetic challenges inherent to rakicidin A. In addition to the synthetic discussion we provide a status...

  8. Metabolomics and dereplication strategies in natural products.

    Science.gov (United States)

    Tawfike, Ahmed Fares; Viegelmann, Christina; Edrada-Ebel, Ruangelie

    2013-01-01

    Metabolomic methods can be utilized to screen diverse biological sources of potentially novel and sustainable sources of antibiotics and pharmacologically-active drugs. Dereplication studies by high resolution Fourier transform mass spectrometry coupled to liquid chromatography (LC-HRFTMS) and nuclear magnetic resonance (NMR) spectroscopy can establish the chemical profile of endophytic and/or endozoic microbial extracts and their plant or animal sources. Identifying the compounds of interest at an early stage will aid in the isolation of the bioactive components. Therefore metabolite profiling is important for functional genomics and in the search for new pharmacologically active compounds. Using the tools of metabolomics through the employment of LC-HRFTMS as well as high resolution NMR will be a very efficient approach. Metabolomic profiling has found its application in screening extracts of macroorganisms as well as in the isolation and cultivation of suspected microbial producers of bioactive natural products.Metabolomics is being applied to identify and biotechnologically optimize the production of pharmacologically active secondary metabolites. The links between metabolome evolution during optimization and processing factors can be identified through metabolomics. Information obtained from a metabolomics dataset can efficiently establish cultivation and production processes at a small scale which will be finally scaled up to a fermenter system, while maintaining or enhancing synthesis of the desired compounds. MZmine (BMC Bioinformatics 11:395-399, 2010; http://mzmine.sourceforge.net/download.shtml ) and SIEVE ( http://www.vastscientific.com/resources/index.html ; Rapid Commun Mass Spectrom 22:1912-1918, 2008) softwares are utilized to perform differential analysis of sample populations to find significant expressed features of complex biomarkers between parameter variables. Metabolomes are identified with the aid of existing high resolution MS and NMR

  9. The chemistry of isoindole natural products

    Directory of Open Access Journals (Sweden)

    Klaus Speck

    2013-10-01

    Full Text Available This review highlights the chemical and biological aspects of natural products containing an oxidized or reduced isoindole skeleton. This motif is found in its intact or modified form in indolocarbazoles, macrocyclic polyketides (cytochalasan alkaloids, the aporhoeadane alkaloids, meroterpenoids from Stachybotrys species and anthraquinone-type alkaloids. Concerning their biological activity, molecular structure and synthesis, we have limited this review to the most inspiring examples. Within different congeners, we have selected a few members and discussed the synthetic routes in more detail. The putative biosynthetic pathways of the presented isoindole alkaloids are described as well.

  10. Natural products from microbes associated with insects

    Directory of Open Access Journals (Sweden)

    Christine Beemelmanns

    2016-02-01

    Full Text Available Here we review discoveries of secondary metabolites from microbes associated with insects. We mainly focus on natural products, where the ecological role has been at least partially elucidated, and/or the pharmaceutical properties evaluated, and on compounds with unique structural features. We demonstrate that the exploration of specific microbial–host interactions, in combination with multidisciplinary dereplication processes, has emerged as a successful strategy to identify novel chemical entities and to shed light on the ecology and evolution of defensive associations.

  11. Natural Products: Insights into Leishmaniasis Inflammatory Response

    Science.gov (United States)

    Rodrigues, Igor A.; Mazotto, Ana Maria; Cardoso, Verônica; Alves, Renan L.; Amaral, Ana Claudia F.; Silva, Jefferson Rocha de Andrade; Pinheiro, Anderson S.; Vermelho, Alane B.

    2015-01-01

    Leishmaniasis is a vector-borne disease that affects several populations worldwide, against which there are no vaccines available and the chemotherapy is highly toxic. Depending on the species causing the infection, the disease is characterized by commitment of tissues, including the skin, mucous membranes, and internal organs. Despite the relevance of host inflammatory mediators on parasite burden control, Leishmania and host immune cells interaction may generate an exacerbated proinflammatory response that plays an important role in the development of leishmaniasis clinical manifestations. Plant-derived natural products have been recognized as bioactive agents with several properties, including anti-protozoal and anti-inflammatory activities. The present review focuses on the antileishmanial activity of plant-derived natural products that are able to modulate the inflammatory response in vitro and in vivo. The capability of crude extracts and some isolated substances in promoting an anti-inflammatory response during Leishmania infection may be used as part of an effective strategy to fight the disease. PMID:26538837

  12. Near infrared spectroscopy in natural products analysis.

    Science.gov (United States)

    Cozzolino, Daniel

    2009-06-01

    Several medicinal and herbal plants properties are related to individual compounds such as essential oils, terpenoids, flavonoids, which are present in natural products in low concentrations (e. g., ppm or ppb). For many years, the use of classical separation and chromatographic and spectrometric techniques such as high performance liquid chromatography (HPLC), gas chromatography (GC), liquid chromatography (LC) and mass spectrometry (MS) were initially used for the elucidation of isolated compounds from different plant matrices. Spectroscopic techniques in the infrared (IR) wavelength region of the electromagnetic spectrum have been used in the food industry to monitor and evaluate the composition of foods. Although Herschel discovered light in the near-infrared (NIR) region as early as 1800, most spectroscopists of the first half of the last century ignored it, in the belief that it lacked any analytical interest. However, during the last 40 years NIR spectroscopy has become one of the most attractive and used methods for analysis. This mini-review highlights recent applications of NIR spectroscopy to the qualitative and quantitative analysis of plant natural products.

  13. Plant cell culture strategies for the production of natural products.

    Science.gov (United States)

    Ochoa-Villarreal, Marisol; Howat, Susan; Hong, SunMi; Jang, Mi Ok; Jin, Young-Woo; Lee, Eun-Kyong; Loake, Gary J

    2016-03-01

    Plants have evolved a vast chemical cornucopia to support their sessile lifestyles. Man has exploited this natural resource since Neolithic times and currently plant-derived chemicals are exploited for a myriad of applications. However, plant sources of most high-value natural products (NPs) are not domesticated and therefore their production cannot be undertaken on an agricultural scale. Further, these plant species are often slow growing, their populations limiting, the concentration of the target molecule highly variable and routinely present at extremely low concentrations. Plant cell and organ culture constitutes a sustainable, controllable and environmentally friendly tool for the industrial production of plant NPs. Further, advances in cell line selection, biotransformation, product secretion, cell permeabilisation, extraction and scale-up, among others, are driving increases in plant NP yields. However, there remain significant obstacles to the commercial synthesis of high-value chemicals from these sources. The relatively recent isolation, culturing and characterisation of cambial meristematic cells (CMCs), provides an emerging platform to circumvent many of these potential difficulties. [BMB Reports 2016; 49(3): 149-158].

  14. Yoghurt enrichment with natural bee farming products

    Directory of Open Access Journals (Sweden)

    N. Lomova

    2015-05-01

    Full Text Available Introduction. Bee pollen is a unique and unparalleled natural bioactive substances source. Using it in conjunction with the popular functional fermented milk product -yogurt will expand its product range and increase the biological value. Materials and Methods. Dried bee pollen’s moisture determination was made by gravimetry methods, based on the sample weight loss due to desiccation, until constant weight was reached.Test and control yogurt samples were studied by applying standard techniques for milk and milk products set forth in the regulations of Ukraine. Results and discussion. It is found that bee pollen pellet drying to a moisture content of 2 -4%, increases the flow rate of powder almost by 90%. The sample having moisture content of 2% will have a bulk density exceeding 12.5% compared to the sample having moisture content of 10%. Raw output will also increase by 3.7%. By contrast, apparent density and weight fraction of losses decreases, which has a positive impact on pollen efficiency of use and distribution in bulk yogurt. Moreover, the weight fraction of losses decreases by fourfold (4.6% vs. 1%. It was experimentally determined that pollen can deteriorate microbiological characteristics of yogurt. It was proved that treatment of crushed bee pollen pellet sample with ultraviolet allows improving yogurt microbiological safety indicators. Namely, to reduce the presence of coli-forms to 0, mould –to 10 CFU/cm³. Conclusions. The proposed bee pollen pellet treatment method will improve the technological and microbiological characteristics of pollen powder. This provides for yoghurt production biotechnology using bee farming products.

  15. Natural product synthesis at the interface of chemistry and biology.

    Science.gov (United States)

    Hong, Jiyong

    2014-08-11

    Nature has evolved to produce unique and diverse natural products that possess high target affinity and specificity. Natural products have been the richest sources for novel modulators of biomolecular function. Since the chemical synthesis of urea by Wöhler, organic chemists have been intrigued by natural products, leading to the evolution of the field of natural product synthesis over the past two centuries. Natural product synthesis has enabled natural products to play an essential role in drug discovery and chemical biology. With the introduction of novel, innovative concepts and strategies for synthetic efficiency, natural product synthesis in the 21st century is well poised to address the challenges and complexities faced by natural product chemistry and will remain essential to progress in biomedical sciences.

  16. Antibacterial natural products in medicinal chemistry--exodus or revival?

    Science.gov (United States)

    von Nussbaum, Franz; Brands, Michael; Hinzen, Berthold; Weigand, Stefan; Häbich, Dieter

    2006-08-04

    To create a drug, nature's blueprints often have to be improved through semisynthesis or total synthesis (chemical postevolution). Selected contributions from industrial and academic groups highlight the arduous but rewarding path from natural products to drugs. Principle modification types for natural products are discussed herein, such as decoration, substitution, and degradation. The biological, chemical, and socioeconomic environments of antibacterial research are dealt with in context. Natural products, many from soil organisms, have provided the majority of lead structures for marketed anti-infectives. Surprisingly, numerous "old" classes of antibacterial natural products have never been intensively explored by medicinal chemists. Nevertheless, research on antibacterial natural products is flagging. Apparently, the "old fashioned" natural products no longer fit into modern drug discovery. The handling of natural products is cumbersome, requiring nonstandardized workflows and extended timelines. Revisiting natural products with modern chemistry and target-finding tools from biology (reversed genomics) is one option for their revival.

  17. The automation of natural product structure elucidation.

    Science.gov (United States)

    Steinbeck, C

    2001-05-01

    The last two or three years have seen exciting developments in the field of computer-assisted structure elucidation (CASE) with a number of programs becoming commercially or freely available. This was the conditio sine qua non for CASE to be widely applied in the daily work of bench chemists and spectroscopists. A number of promising applications have been published in the area of structure generators, deterministic and stochastic CASE tools and property predictions, including the automatic distinction between natural products and artificial compounds, as well as the determination of 3-D structure from a connection table based on IR spectroscopy. Advancements in coupling techniques between chromatographic and spectroscopic methods demonstrate progress towards a fully automated structure elucidation or identification process starting at the earliest steps of obtaining crude extracts.

  18. On the rise of Chio-ssu-lo regime & Qingtang silk Road%唃厮啰政权的兴起与青唐道贸易

    Institute of Scientific and Technical Information of China (English)

    马旭俊; 杨军

    2016-01-01

    The reasons that Hehuang Tibetan tribes formed into"Chio-ssu-lo regime", should not only be exagger⁃ated or regarded as the personal role made by Chio-ssu-lo, instead there is the intrinsic history motivation:after the disintegration of the Tubo regime, the Tibetan tribes which lived in the Helong area in order to overcome the economic dilemma caused by not being able to self-sufficiency, made choices of“migration”at all time. They plundered and allied each other, and sometimes changed regimes to gain interest for themselves. The long period of political disorder and material deprivation made Hehuang Tibetan tribes yearn for peace and unity, so they convened the Tubo tribes, and made Chio-ssu-lo to be the head of the tribes. However, Chio-ssu-lo was not able to resolve the contradiction between economic capability and centralization effectively, he inevitably faced failure, but because of the rise of Tangut, the tribes of Hexi Tubo and Uighur went to Chio-ssu-lo for shelter, which rendered the trade in Qingtang area flourish, and Chio-ssu-lo received rewards and titles granted by the government of the Song dynasty. These all made Chio-ssu-lo was able to establish his regime.%促成河湟吐蕃诸部形成“唃厮啰政权”的原因,不宜夸大或仅看作是唃厮啰个人的作用。更为内在的社会经济动因是,吐蕃政权解体之后,散居于河陇一带的吐蕃诸部为了克服经济上不能自足的窘境,随时做有关“迁移”的抉择——他们或相互劫掠,或组建联盟(凉州六谷部),或改变政权认同获取利益(投降西夏、投靠宋朝成为“熟户”)。正是这种长时期的政治无序与物质相对匮乏状态,唤醒了河湟吐蕃诸部关于一统秩序的历史记忆与现实向往(吐蕃政权),并意图以“赞普苗裔”为历史共鸣凝聚吐蕃旧部。唃厮啰作为当时被吐蕃诸部拥立的“赞普苗裔”之一,先后被河湟吐蕃部落首领李立遵

  19. Chemistry of natural products: A veritable approach to the ...

    African Journals Online (AJOL)

    Chemistry of natural products: A veritable approach to the development of drugs for combating ... PROMOTING ACCESS TO AFRICAN RESEARCH ... The earth's resources, especially natural products, are no doubt important materials from ...

  20. Chocolate: A Marvelous Natural Product of Chemistry

    Science.gov (United States)

    Tannenbaum, Ginger

    2004-08-01

    Chocolate is a natural product as ubiquitous as television. Of course, it is eaten, but it is also found in air fresheners, marking pens, flavoring in a multitude of products including soda pop, and as an aroma in "chocolate-dyed" T-shirts. However, most of us are completely unaware of the complex chemical reactions that take place to produce chocolate and the necessary technology that has evolved to produce chocolate and all its byproducts. Processing results in a mixture of many components, an interesting contrast to most of the simple, one-step reactions introduced at the high school level. This article is a survey of chocolate from tree to table. After a brief introduction to the history of chocolate and how and where it is grown, the manufacturing process is examined, and the chemistry is explored. A bit of the jargon used in the industry is mentioned. Cocoa butter is a significant ingredient in chocolate, and an investigation of it introduces triglycerides, fatty acids, polymorphic behavior, and molecular packing of the fats in chocolate and how they affect the tempering process. There is a brief discussion of chocolate's non-Newtonian behavior and the resulting challenges presented in the manufacturing process. See Featured Molecules Featured on the Cover

  1. Natural products--a simple model to explain chemical diversity.

    Science.gov (United States)

    Firn, Richard D; Jones, Clive G

    2003-08-01

    A simple evolutionary model is presented which explains why organisms produce so many natural products, why so many have low biological activity, why enzymes involved in natural product synthesis have the properties they do and why natural product metabolism is shaped as it is.

  2. [The recent research progress of chemistry of marine natural products].

    Science.gov (United States)

    Shi, Qing-wen; Li, Li-geng; Wang, Yu-fang; Huo, Chang-hong; Zhang, Man-li

    2010-10-01

    Ocean is a unique and excellent resource that provides a diverse array of intriguing natural products. Marine natural products have demonstrated significant and extremely potent biological activities and have captured the attention of natural products chemists in the past few decades. It is increasingly recognized that a wealth of fascinating natural products and novel chemical entities will play a dominant role in the discovery of useful leads for the development of pharmaceutical agents and provide useful probes to lead to breakthroughs in a variety of life-science fields. This article focused on the research progress of chemistry of marine natural products in recent five years.

  3. Beware When Buying "All Natural" Erectile Dysfunction Products

    Science.gov (United States)

    ... Radiation-Emitting Products Vaccines, Blood & Biologics Animal & Veterinary Cosmetics Tobacco Products For Consumers Home For Consumers Protect Yourself Health Fraud Beware When Buying "All Natural" Erectile Dysfunction Products Share Tweet Linkedin Pin it ...

  4. Oxygen-containing fragments in natural products.

    Science.gov (United States)

    Titarenko, Zoya; Vasilevich, Natalya; Zernov, Vladimir; Kirpichenok, Michael; Genis, Dmitry

    2013-02-01

    An analysis of the chemical environment of the oxygen atoms in the DNP database compared to the CMC and SCD databases was performed. Some structural clusters were identified which are predominant among the natural products and can be considered as distinctive features of NPs. Fifty-three oxygen-containing structural fragments that are distinctive for the DNP (distinctive set of fragments DSF) in comparison with the SCD have been identified. A new descriptor Mc was introduced for describing the ratio of atoms involved in the DSF to the total number of heavy atoms. A significant difference in the Mc values among the reference databases allowed the use of a specific cluster of the DSF as a tool for performing similarity searches for oxygen-containing NP molecules, or for evaluation or comparison of databases according to their NP-likeness. An example illustrating that the suggested approach could allow not only estimating the NP-likeness, but also serve as a tool for designing new NP-like compounds is provided. The suggested approach for NP-likeness evaluation moves away from the traditional ideas of scaffolds, cycles, linkers and substituents.

  5. Antifouling Activity of Marine Natural Products

    KAUST Repository

    Qian, Pei-Yuan

    2012-01-01

    With the global ban of application of organotin-based marine coatings by International Maritime Organization in 2008, there is a practical and urgent need of identifying environmentally friendly low-toxic and nontoxic antifouling compounds for marine industries. Marine natural products have been considered as one of the most promising sources of antifouling compounds in recent years. In antifouling compound screening processes, bioassay systems often play most critical/vital roles in screening efforts. To meet various needs, a variety of bioassay systems have been developed and/or adopted in both research and commercial laboratories. In this chapter, we provide a brief outline of common bioassay procedures for both antimicrofouling and antimacrofouling assays, which can serve as a general guideline for setting up bioassay systems in laboratories engaged in antifouling compound screening. Some bioassay procedures currently practiced in various laboratories are not included in this book chapter for various reasons. Individual laboratories should modify bioassay protocols based on their research interests or needs. Nevertheless, we highly recommend the research laboratories to adapt high-throughput assays as much as possible for preliminary screening assays, followed by more complex bioassay processes using multiple target species. We argue strongly for studies in mode-of-action of antifouling compounds against settling propagules, which shall lead to discovery of molecular biomarkers (genes, proteins, receptors, or receptor system) and will allow us to design more targeted bioassay systems.

  6. A Historical Overview of Natural Products in Drug Discovery

    Science.gov (United States)

    Dias, Daniel A.; Urban, Sylvia; Roessner, Ute

    2012-01-01

    Historically, natural products have been used since ancient times and in folklore for the treatment of many diseases and illnesses. Classical natural product chemistry methodologies enabled a vast array of bioactive secondary metabolites from terrestrial and marine sources to be discovered. Many of these natural products have gone on to become current drug candidates. This brief review aims to highlight historically significant bioactive marine and terrestrial natural products, their use in folklore and dereplication techniques to rapidly facilitate their discovery. Furthermore a discussion of how natural product chemistry has resulted in the identification of many drug candidates; the application of advanced hyphenated spectroscopic techniques to aid in their discovery, the future of natural product chemistry and finally adopting metabolomic profiling and dereplication approaches for the comprehensive study of natural product extracts will be discussed. PMID:24957513

  7. Pharmaceuticals from natural products: current trends

    Directory of Open Access Journals (Sweden)

    PETER R. SEIDL

    2002-03-01

    Full Text Available The use of products extracted from plants for medicinal purposes can be traced to the beginnings of civilization and up until the end of the nineteenth century natural products were the principal source of medicines. Since then their relative importance has oscillated according to the strategies of large pharmaceutical companies. Now that these strategies are changing, there are new opportunities for countries like Brazil, in which a large proportion of the world's biodiversity is located. There are, however, new circumstances that must be taken into consideration: material must be collected by groups which are formally authorized to do so and under the conditions of the Convention of Biological Diversity, the discovery process is being successively outsourced to smaller specialized firms and there is a growing integration with producers of cosmetics and phytomedicines.O uso de produtos extraídos de plantas para fins medicinais pode ser tracejado aos inícios da civilização e até o fim do século XIX, os produtos naturais constituíram a principal fonte de medicamentos. Desde então, a importância relativa dos produtos naturais tem oscilado de acordo com as estratégias de grandes companhias farmacêuticas. Agora que estas estratégias vêm mudando, há novas oportunidades para países como o Brasil, no qual está localizada uma vasta proporção da biodiversidade mundial. Há, entretanto, novas circunstâncias que devem ser levadas em consideração: o material deve ser coletado por grupos que estão formalmente autorizados para tal, com a coleta sendo feita sob as condições da Convenção de Diversidade Biológica, o processo de descoberta está sendo sucessivamente terceirizado no sentido de firmas especializadas menores e há uma integração crescente como produtores de cosméticos e fitomedicamentos.

  8. Natural product proteomining, a quantitative proteomics platform, allows rapid discovery of biosynthetic gene clusters for different classes of natural products.

    Science.gov (United States)

    Gubbens, Jacob; Zhu, Hua; Girard, Geneviève; Song, Lijiang; Florea, Bogdan I; Aston, Philip; Ichinose, Koji; Filippov, Dmitri V; Choi, Young H; Overkleeft, Herman S; Challis, Gregory L; van Wezel, Gilles P

    2014-06-19

    Information on gene clusters for natural product biosynthesis is accumulating rapidly because of the current boom of available genome sequencing data. However, linking a natural product to a specific gene cluster remains challenging. Here, we present a widely applicable strategy for the identification of gene clusters for specific natural products, which we name natural product proteomining. The method is based on using fluctuating growth conditions that ensure differential biosynthesis of the bioactivity of interest. Subsequent combination of metabolomics and quantitative proteomics establishes correlations between abundance of natural products and concomitant changes in the protein pool, which allows identification of the relevant biosynthetic gene cluster. We used this approach to elucidate gene clusters for different natural products in Bacillus and Streptomyces, including a novel juglomycin-type antibiotic. Natural product proteomining does not require prior knowledge of the gene cluster or secondary metabolite and therefore represents a general strategy for identification of all types of gene clusters.

  9. Capital productivity and the nature of competition

    OpenAIRE

    Börsch-Supan, Axel

    1997-01-01

    This paper measures capital productivity in West Germany, Japan and the United States and links capital productivity to financial performance. We show that West Germany and Japan have significantly lower levels of capital productivity than the United States, mainly due to lower capital utilization but also because less productive capacity was created per unit of physical assets. On a higher level of causality, we show that this mainly comes from less pressure from product market competition a...

  10. Role of natural product diversity in chemical biology.

    Science.gov (United States)

    Hong, Jiyong

    2011-06-01

    Through the natural selection process, natural products possess a unique and vast chemical diversity and have been evolved for optimal interactions with biological macromolecules. Owing to their diversity, target affinity, and specificity, natural products have demonstrated enormous potential as modulators of biomolecular function, been an essential source for drug discovery, and provided design principles for combinatorial library development.

  11. Natural Product Biosynthetic Diversity and Comparative Genomics of the Cyanobacteria.

    Science.gov (United States)

    Dittmann, Elke; Gugger, Muriel; Sivonen, Kaarina; Fewer, David P

    2015-10-01

    Cyanobacteria are an ancient lineage of slow-growing photosynthetic bacteria and a prolific source of natural products with intricate chemical structures and potent biological activities. The bulk of these natural products are known from just a handful of genera. Recent efforts have elucidated the mechanisms underpinning the biosynthesis of a diverse array of natural products from cyanobacteria. Many of the biosynthetic mechanisms are unique to cyanobacteria or rarely described from other organisms. Advances in genome sequence technology have precipitated a deluge of genome sequences for cyanobacteria. This makes it possible to link known natural products to biosynthetic gene clusters but also accelerates the discovery of new natural products through genome mining. These studies demonstrate that cyanobacteria encode a huge variety of cryptic gene clusters for the production of natural products, and the known chemical diversity is likely to be just a fraction of the true biosynthetic capabilities of this fascinating and ancient group of organisms.

  12. Industrial natural product chemistry for drug discovery and development.

    Science.gov (United States)

    Bauer, Armin; Brönstrup, Mark

    2014-01-01

    Covering: up to March 2013. In addition to their prominent role in basic biological and chemical research, natural products are a rich source of commercial products for the pharmaceutical and other industries. Industrial natural product chemistry is of fundamental importance for successful product development, as the vast majority (ca. 80%) of commercial drugs derived from natural products require synthetic efforts, either to enable economical access to bulk material, and/or to optimize drug properties through structural modifications. This review aims to illustrate issues on the pathway from lead to product, and how they have been successfully addressed by modern natural product chemistry. It is focused on natural products of current relevance that are, or are intended to be, used as pharmaceuticals.

  13. Chios mastic fractions in experimental colitis: implication of the nuclear factor κB pathway in cultured HT29 cells.

    Science.gov (United States)

    Papalois, Apostolos; Gioxari, Aristea; Kaliora, Andriana C; Lymperopoulou, Aikaterini; Agrogiannis, George; Papada, Efstathia; Andrikopoulos, Nikolaos K

    2012-11-01

    The Pistacia lentiscus tree gives a resinous exudate called Chios mastic (CM) rich in triterpenoids. CM can be fractionated into acidic and neutral fractions (AF and NF, respectively). Oleanolic acid (OA) is a major triterpenic acid in CM with several antioxidant and anti-inflammatory properties. We have recently shown that CM is beneficial in experimental colitis in the form of powder mixture with inulin, as supplied commercially. However, the bioactive fraction or compound of CM is unidentified. Thus, based on the hypothesis that terpenoids exhibit functional activities via distinguishable pathways, we fractionated CM and applied different fractions or individual OA in experimental colitis. Furthermore, we investigated the mechanism underlying this effect in human colon epithelial cells. CM powder mixture (100 mg/kg of body weight) or the respective CM powder mixture components (i.e., inulin, AF, NF, or OA) were individually administered in trinitrobenzene sulfonic acid-treated rats. Colonic damage was assessed microscopically, and levels of tumor necrosis factor-α (TNF-α), interleukin (IL)-6, IL-8, and intercellular adhesion molecule-1were measured. A model of inflammation in co-cultured human colon epithelial HT29 cells and monocytes/macrophages was established. Lactate dehydrogenase release and levels of TNF-α, IL-8, and nuclear factor-κB (NF-κB) p65 were measured. In vivo, histological amelioration of colitis and significant regulation in inflammation occurred with CM powder mixture, even at the mRNA level. Although no histological improvement was observed, AF and NF reduced levels of inflammatory markers. Inulin was ineffective. In vitro, CM treatment down-regulated IL-8 and NF-κB p65. Neither fractions nor OA was the bioactive component solely. Most probably, the entire CM rather than its individual fractions reduces inflammation via NF-κB regulation.

  14. Biosynthesis of therapeutic natural products using synthetic biology.

    Science.gov (United States)

    Awan, Ali R; Shaw, William M; Ellis, Tom

    2016-10-01

    Natural products are a group of bioactive structurally diverse chemicals produced by microorganisms and plants. These molecules and their derivatives have contributed to over a third of the therapeutic drugs produced in the last century. However, over the last few decades traditional drug discovery pipelines from natural products have become far less productive and far more expensive. One recent development with promise to combat this trend is the application of synthetic biology to therapeutic natural product biosynthesis. Synthetic biology is a young discipline with roots in systems biology, genetic engineering, and metabolic engineering. In this review, we discuss the use of synthetic biology to engineer improved yields of existing therapeutic natural products. We further describe the use of synthetic biology to combine and express natural product biosynthetic genes in unprecedented ways, and how this holds promise for opening up completely new avenues for drug discovery and production. Copyright © 2016 Elsevier B.V. All rights reserved.

  15. Natural health products and cancer chemotherapy and radiation therapy

    Directory of Open Access Journals (Sweden)

    Doreen Oneschuk

    2011-12-01

    Full Text Available Complementary therapies, notably natural health products such as herbs and vitamins, are frequently used by cancer patients receiving chemotherapy and radiation therapy. There is much controversy as to whether these natural health products should be taken during conventional cancer treatments. Supporters of this practice cite beneficial effects of the antioxidant properties, while opponents are concerned about the potential for natural health product-chemotherapy/radiation related negative interactions. This involves understanding the role and effect on metabolizing enzymes. This review will highlight the present evidence for both the beneficial and negative consequences of the use of natural health products during chemotherapy and radiation therapy.

  16. Scouring Process of Natural Color Cotton Products

    Institute of Scientific and Technical Information of China (English)

    XU Wei

    2002-01-01

    In order to improve the absorbency of color cotton products, alkali and pectase scouring processes under different conditions were tested, by comparing the actual results of two different scouring processes. It was considered that the pectase scouring process more suits color cotton products.

  17. New natural products as new leads for antibacterial drug discovery.

    Science.gov (United States)

    Brown, Dean G; Lister, Troy; May-Dracka, Tricia L

    2014-01-15

    Natural products have been a rich source of antibacterial drugs for many decades, but investments in this area have declined over the past two decades. The purpose of this review article is to provide a recent survey of new natural product classes and the mechanisms by which they work.

  18. Rapid Growth in China Natural Gas Demand and Production

    Institute of Scientific and Technical Information of China (English)

    Li Min

    2003-01-01

    @@ China's natural gas production will exceed 35 billion cubic meters in 2003,more than 7 percent up from last year,according to the estimation by the related department. There are now more than 60 enterprises engaged in natural gas production in China.

  19. China Ranks 15th for 2001 Natural Gas Production

    Institute of Scientific and Technical Information of China (English)

    2002-01-01

    @@ China's natural gas output totaled 30.302 billion cubic meters in 2001, an 11 percent increase as compared with the previous year. However, China ranked 15th in the world for its natural gas production last year while Malaysia jumped to the 12th place in the ranking since the country saw a considerable increase in gas production.

  20. Harnessing natural product assembly lines: structure, promiscuity, and engineering.

    Science.gov (United States)

    Ladner, Christopher C; Williams, Gavin J

    2016-03-01

    Many therapeutically relevant natural products are biosynthesized by the action of giant mega-enzyme assembly lines. By leveraging the specificity, promiscuity, and modularity of assembly lines, a variety of strategies has been developed that enables the biosynthesis of modified natural products. This review briefly summarizes recent structural advances related to natural product assembly lines, discusses chemical approaches to probing assembly line structures in the absence of traditional biophysical data, and surveys efforts that harness the inherent or engineered promiscuity of assembly lines for the synthesis of non-natural polyketides and non-ribosomal peptide analogues.

  1. Psychoactive natural products: overview of recent developments

    OpenAIRE

    2014-01-01

    Natural psychoactive substances have fascinated the curious mind of shamans, artists, scholars and laymen since antiquity. During the twentieth century, the chemical composition of the most important psychoactive drugs, that is opium, cannabis, coca and "magic mushrooms", has been fully elucidated. The mode of action of the principal ingredients has also been deciphered at the molecular level. In the past two decades, the use of herbal drugs, such as kava, kratom and Salvia divinorum, began t...

  2. Recent Advances in Separation of Bioactive Natural Products

    Institute of Scientific and Technical Information of China (English)

    任其龙; 邢华斌; 鲍宗必; 苏宝根; 杨启炜; 杨亦文; 张治国

    2013-01-01

    Bioactive natural products are a main source of new drugs, functional foods and food additives. The separation of bioactive natural products plays an important role in transformation and use of biomass. The isolation and purification of bioactive principle from a complex matrix is often inherent bottleneck for the utilization of natural products, so a series of extraction and separation techniques have been developed. This review covers recent advances in the separation of bioactive natural products with an emphasis on their solubility and diffusion coeffi-cients, recent extraction techniques and isolation techniques. This overview of recent technological advances, dis-cussion of pertinent problems and prospect of current methodologies in the separation of bioactive natural products may provide a driving force for development of novel separation techniques.

  3. Bioactive natural products from Papua New Guinea marine sponges.

    Science.gov (United States)

    Noro, Jeffery C; Kalaitzis, John A; Neilan, Brett A

    2012-10-01

    The discovery of novel natural products for drug development relies heavily upon a rich biodiversity, of which the marine environment is an obvious example. Marine natural product research has spawned several drugs and many other candidates, some of which are the focus of current clinical trials. The sponge megadiversity of Papua New Guinea is a rich but underexplored source of bioactive natural products. Here, we review some of the many natural products derived from PNG sponges with an emphasis on those with interesting biological activity and, therefore, drug potential. Many bioactive natural products discussed here appear to be derived from non-ribosomal peptide and polyketide biosynthesis pathways, strongly suggesting a microbial origin of these compounds. With this in mind, we also explore the notion of sponge-symbiont biosynthesis of these bioactive compounds and present examples to support the working hypothesis.

  4. Marinopyrroles: Unique Drug Discoveries Based on Marine Natural Products.

    Science.gov (United States)

    Li, Rongshi

    2016-01-01

    Natural products provide a successful supply of new chemical entities (NCEs) for drug discovery to treat human diseases. Approximately half of the NCEs are based on natural products and their derivatives. Notably, marine natural products, a largely untapped resource, have contributed to drug discovery and development with eight drugs or cosmeceuticals approved by the U.S. Food and Drug Administration and European Medicines Agency, and ten candidates undergoing clinical trials. Collaborative efforts from drug developers, biologists, organic, medicinal, and natural product chemists have elevated drug discoveries to new levels. These efforts are expected to continue to improve the efficiency of natural product-based drugs. Marinopyrroles are examined here as a case study for potential anticancer and antibiotic agents.

  5. Natural Products Version 2.0: Connecting Genes to Molecules

    Science.gov (United States)

    Walsh, Christopher T.; Fischbach, Michael A.

    2009-01-01

    Natural products have played a prominent role in the history of organic chemistry, and they continue to be important as drugs, biological probes, and targets of study for synthetic and analytical chemists. In this perspective, we explore how connecting Nature’s small molecules to the genes that encode them has sparked a renaissance in natural product research, focusing primarily on the biosynthesis of polyketides and nonribosomal peptides. We survey monomer biogenesis, coupling chemistries from templated and non-templated pathways, and the broad set of tailoring reactions and hybrid pathways that give rise to the diverse scaffolds and functionalization patterns of natural products. We conclude by considering two questions: What would it take to find all natural product scaffolds? What kind of scientists will be studying natural products in the future? PMID:20121095

  6. Capturing Biological Activity in Natural Product Fragments by Chemical Synthesis.

    Science.gov (United States)

    Crane, Erika A; Gademann, Karl

    2016-03-14

    Natural products have had an immense influence on science and have directly led to the introduction of many drugs. Organic chemistry, and its unique ability to tailor natural products through synthesis, provides an extraordinary approach to unlock the full potential of natural products. In this Review, an approach based on natural product derived fragments is presented that can successfully address some of the current challenges in drug discovery. These fragments often display significantly reduced molecular weights, reduced structural complexity, a reduced number of synthetic steps, while retaining or even improving key biological parameters such as potency or selectivity. Examples from various stages of the drug development process up to the clinic are presented. In addition, this process can be leveraged by recent developments such as genome mining, antibody-drug conjugates, and computational approaches. All these concepts have the potential to identify the next generation of drug candidates inspired by natural products.

  7. Antimycobacterial susceptibility testing methods for natural products research

    Directory of Open Access Journals (Sweden)

    Juan Gabriel Bueno Sánchez

    2010-06-01

    Full Text Available The emergence of multidrug-resistant strains of Mycobacterium tuberculosis underscores the need of continuous developments on new and efficient methods to determine the susceptibility of isolates of M. tuberculosis in the search for novel antimicrobial agents. Natural products constitute an important source of new drugs, but design and implementation of antimycobacterial susceptibility testing methods are necessary for evaluate the different extracts and compounds. A number of biological assay methodologies are in current use, ranging from the classical disk diffusion and broth dilution assay format, to radiorespirometric (BACTEC, dye-based, and fluorescent/luminescence reporter assays. This review presents an analysis on the in vitro susceptibility testing methods developed for determinate antitubercular activity in natural products and related compounds (semi-synthetic natural products and natural products-derived compounds and the criteria to select the adequate method for determination of biological activity of new natural products.

  8. MARINE NATURAL PRODUCTS: A WAY TO NEW DRUGS

    OpenAIRE

    Stonik, V.

    2009-01-01

    The investigation of marine natural products (low molecular weight bioregulators) is a rapidly developing scientific field at the intersection of biology and chemistry. Investigations aimed at detecting, identifying, and understanding the structure of marine natural products have led to the discovery of 20,000 new substances, including those characterized by an extremely high physiological activity. Some results and prospects of works aimed at creating new drugs on the basis of marine natural...

  9. Marine actinobacteria: new opportunities for natural product search and discovery.

    Science.gov (United States)

    Bull, Alan T; Stach, James E M

    2007-11-01

    It is widely accepted that new drugs, especially antibiotics, are urgently required, and that the most propitious source remains natural products. We argue that in exploring new sources of bioactive natural products the marine environment warrants particular attention, in view of the remarkable diversity of microorganisms and metabolic products. Recent reports of new chemical entities and first-in-class drug candidates, and confirmation of indigenous marine actinobacteria, make exciting discoveries even more likely given the unrivalled capacity of this class of bacteria to produce exploitable natural products.

  10. The structural biology of enzymes involved in natural product glycosylation.

    Science.gov (United States)

    Singh, Shanteri; Phillips, George N; Thorson, Jon S

    2012-10-01

    The glycosylation of microbial natural products often dramatically influences the biological and/or pharmacological activities of the parental metabolite. Over the past decade, crystal structures of several enzymes involved in the biosynthesis and attachment of novel sugars found appended to natural products have emerged. In many cases, these studies have paved the way to a better understanding of the corresponding enzyme mechanism of action and have served as a starting point for engineering variant enzymes to facilitate to production of differentially-glycosylated natural products. This review specifically summarizes the structural studies of bacterial enzymes involved in biosynthesis of novel sugar nucleotides.

  11. Strategies for target identification of antimicrobial natural products.

    Science.gov (United States)

    Farha, Maya A; Brown, Eric D

    2016-05-04

    Covering: 2000 to 2015Despite a pervasive decline in natural product research at many pharmaceutical companies over the last two decades, natural products have undeniably been a prolific and unsurpassed source for new lead antibacterial compounds. Due to their inherent complexity, natural extracts face several hurdles in high-throughout discovery programs, including target identification. Target identification and validation is a crucial process for advancing hits through the discovery pipeline, but has remained a major bottleneck. In the case of natural products, extremely low yields and limited compound supply further impede the process. Here, we review the wealth of target identification strategies that have been proposed and implemented for the characterization of novel antibacterials. Traditionally, these have included genomic and biochemical-based approaches, which, in recent years, have been improved with modern-day technology and better honed for natural product discovery. Further, we discuss the more recent innovative approaches for uncovering the target of new antibacterial natural products, which have resulted from modern advances in chemical biology tools. Finally, we present unique screening platforms implemented to streamline the process of target identification. The different innovative methods to respond to the challenge of characterizing the mode of action for antibacterial natural products have cumulatively built useful frameworks that may advocate a renovated interest in natural product drug discovery programs.

  12. NATURAL ANTIOXIDANTS IN PRODUCTION “BRUSHWOOD”

    Directory of Open Access Journals (Sweden)

    G. N. Dubtsova

    2015-01-01

    Full Text Available Flour wares use popularity, there is 48% of general volume of pastry wares on their stake. A marketing study on results that actuality of development of new type of flour good is set with the lowered maintenance of fat and enriched by vitamins is undertaken. The use of natural antioxidant of "Guarding is reasonable toco 70" and introduction of 0,2% is recommended for stabilizing of sunflower-seed oil at fry of frying. Joint introduction of powders is studied from the garden-stuffs of brier and unabi on quality of the brushwood fried in sunflower-seed oil with the use of "Guarding toco 70". From wares extracted lipids and estimated on indexes: peroxides, acid and anizid numbers. It is set that an antioxidant and vegetable powders assist the decline of indexes of safety peroxides and asid in two times, and anizid in 1,3 time. Use of antioxidant of "Guarding toco 70", being in 70% from the natural concentrate of mixture of tocopherolss and 30% of soyaoil.

  13. Fungi as a source of natural coumarins production.

    Science.gov (United States)

    Costa, Tania Maria; Tavares, Lorena Benathar Ballod; de Oliveira, Débora

    2016-08-01

    Natural coumarins and derivatives are compounds that occur naturally in several organisms (plant, bacteria, and fungi) consisting of fused benzene and α-pyrone rings. These compounds show high technological potential applications in agrochemical, food, pharmaceuticals, and cosmetics industries. Therefore, the need for bulk production of coumarins and the advancement of the chemical and pharmaceutical industries led to the development of synthetic coumarin. However, biotransformation process, synthetic bioengineering, metabolic engineering, and bioinformatics have proven effective in the production of natural products. Today, these biological systems are recognized as green chemistry innovation and business strategy. This review article aims to report the potential of fungi for synthesis of coumarin. These microorganisms are described as a source of natural products capable of synthesizing many bioactive metabolites. The features, classification, properties, and industrial applications of natural coumarins as well as new molecules obtained by basidiomycetes and ascomycetes fungi are reported in order to explore a topic not yet discussed in the scientific literature.

  14. Chemical Biology of Microbial Anticancer Natural Products

    DEFF Research Database (Denmark)

    Bladt, Tanja Thorskov; Gotfredsen, Charlotte Held

    towards chronic lymphocytic leukemia (CLL) cells is crucial since CLL is considered as an incurable disease. To discover novel agents that targets CLL cells is complicated. CLL cells rapidly undergo apoptosis in vitro when they are removed from their natural microenvironment, even though they are long......Filamentous fungi and other microorganisms have amazing abilities to synthesize structural complex, diverse and unique small organic molecules. Many are bioactive and numerous compounds such as mycotoxins, antifungal, and anticancer agents have been reported in the literature within the last more......-living cells in vivo. Fortunately viability of CLL cells can be maintained in vitro by co-cultivation with stromal cells mimicking in vivo conditions. This has led to the development of a co-culture assay that is ideally suited for screening of NPs. The main goal of this study has been to discover fungal NPs...

  15. College of Natural Resources to offer Forest Products Marketing Workshop

    OpenAIRE

    Davis, Lynn

    2008-01-01

    Marketing has been called the backbone of successful forest products companies, yet many small businesses struggle with the marketing concept. Virginia Tech's College of Natural Resources continues its service to the forest products industry by presenting the fourteenth annual workshop on Forest Products Marketing, Oct. 23 through Oct. 24, at The Inn at Virginia Tech and Skelton Conference Center.

  16. Separation process design for isolation and purification of natural products

    DEFF Research Database (Denmark)

    Malwade, Chandrakant R.

    Natural products are defined as secondary metabolites produced by plants and form a vast pool of compounds with unlimited chemical and functional diversity. Many of these secondary metabolites are high value added chemicals that are frequently used as ingredients in food, cosmetics, pharmaceutica...... information is used to further optimize the process flow sheet. Chemometric methods have been used to extract molecular level information for understanding the process streams in relation to their separation operations....... and other consumer products. Therefore, process technology towards industrial scale production of such high value chemicals from plants has significant value. Natural products can be obtained in pure form via synthetic or semi-synthetic route, but due to their complicated nature these methods have not been...... developed to the extent of industrial production for majority of natural products. Thus, isolation and purification of such natural products from plants is the most viable way to obtain natural products in pure form. This PhD project is mainly concerned with the design of separation process to isolate...

  17. Dereplication of Microbial Natural Products by LC-DAD-TOFMS

    DEFF Research Database (Denmark)

    Nielsen, Kristian Fog; Månsson, Maria; Rank, Christian;

    2011-01-01

    Dereplication, the rapid identification of known compounds present in a mixture, is crucial to the fast discovery of novel natural products. Determining the elemental composition of compounds in mixtures and tentatively identifying natural products using MS/MS and UV/vis spectra is becoming easier...... with advances in analytical equipment and better compound databases. Here we demonstrate the use of LC-UV/vis-MS-based dereplication using data from UV/vis diode array detection and ESI+/ESI– time-of-flight MS for assignment of 719 microbial natural product and mycotoxin reference standards. ESI+ was the most...

  18. Solid-phase enrichment and analysis of electrophilic natural products

    Directory of Open Access Journals (Sweden)

    Frank Wesche

    2017-03-01

    Full Text Available In search for new natural products, which may lead to the development of new drugs for all kind of applications, novel methods are needed. Here we describe the identification of electrophilic natural products in crude extracts via their reactivity against azide as a nucleophile followed by their subsequent enrichment using a cleavable azide-reactive resin (CARR. Using this approach, natural products carrying epoxides and α,β-unsaturated enones as well as several unknown compounds were identified in crude extracts from entomopathogenic Photorhabdus bacteria.

  19. Production of Substitute Natural Gas from Coal

    Energy Technology Data Exchange (ETDEWEB)

    Andrew Lucero

    2009-01-31

    The goal of this research program was to develop and demonstrate a novel gasification technology to produce substitute natural gas (SNG) from coal. The technology relies on a continuous sequential processing method that differs substantially from the historic methanation or hydro-gasification processing technologies. The thermo-chemistry relies on all the same reactions, but the processing sequences are different. The proposed concept is appropriate for western sub-bituminous coals, which tend to be composed of about half fixed carbon and about half volatile matter (dry ash-free basis). In the most general terms the process requires four steps (1) separating the fixed carbon from the volatile matter (pyrolysis); (2) converting the volatile fraction into syngas (reforming); (3) reacting the syngas with heated carbon to make methane-rich fuel gas (methanation and hydro-gasification); and (4) generating process heat by combusting residual char (combustion). A key feature of this technology is that no oxygen plant is needed for char combustion.

  20. Manufacturing Natural Killer Cells as Medicinal Products

    Science.gov (United States)

    Chabannon, Christian; Mfarrej, Bechara; Guia, Sophie; Ugolini, Sophie; Devillier, Raynier; Blaise, Didier; Vivier, Eric; Calmels, Boris

    2016-01-01

    Natural Killer (NK) cells are innate lymphoid cells (ILC) with cytotoxic and regulatory properties. Their functions are tightly regulated by an array of inhibitory and activating receptors, and their mechanisms of activation strongly differ from antigen recognition in the context of human leukocyte antigen presentation as needed for T-cell activation. NK cells thus offer unique opportunities for new and improved therapeutic manipulation, either in vivo or in vitro, in a variety of human diseases, including cancers. NK cell activity can possibly be modulated in vivo through direct or indirect actions exerted by small molecules or monoclonal antibodies. NK cells can also be adoptively transferred following more or less substantial modifications through cell and gene manufacturing, in order to empower them with new or improved functions and ensure their controlled persistence and activity in the recipient. In the present review, we will focus on the technological and regulatory challenges of NK cell manufacturing and discuss conditions in which these innovative cellular therapies can be brought to the clinic. PMID:27895646

  1. Opportunities for natural products in 21(st) century antibiotic discovery.

    Science.gov (United States)

    Wright, Gerard D

    2017-07-01

    Natural products and their derivatives are mainstays of our antibiotic drugs, but they are increasingly in peril. The combination of widespread multidrug resistance in once susceptible bacterial pathogens, disenchantment with natural products as sources of new drugs, lack of success using synthetic compounds and target-based discovery methods, along with shifting economic and regulatory issues, conspire to move investment in research and development away from the antibiotics arena. The result is a growing crisis in antibiotic drug discovery that threatens modern medicine. 21(st) century natural product research is perfectly positioned to fill the antibiotic discovery gap and bring new drug candidates to the clinic. Innovations in genomics and techniques to explore new sources of antimicrobial chemical matter are revealing new chemistry. Increasing appreciation of the value of narrow-spectrum drugs and re-examination of once discarded chemical scaffolds coupled with synthetic biology methods to generate new compounds and improve yields offer new strategies to revitalize once moribund natural product programs. The increasing awareness that the combination of antibiotics with adjuvants, non-antibiotic compounds that overcome resistance and enhance drug activity, can rescue older chemical scaffolds, and concepts such as blocking pathogen virulence present orthogonal strategies to traditional antibiotics. In all these areas, natural products offer chemical matter, shaped by natural selection, that is privileged in this therapeutic area. Natural product research is poised to regain prominence in delivering new drugs to solve the antibiotic crisis.

  2. Biosynthesis of natural products containing β-amino acids.

    Science.gov (United States)

    Kudo, Fumitaka; Miyanaga, Akimasa; Eguchi, Tadashi

    2014-08-01

    Covering: up to January, 2014. We focus here on β-amino acids as components of complex natural products because the presence of β-amino acids produces structural diversity in natural products and provides characteristic architectures beyond those of ordinary α-L-amino acids, thus generating significant and unique biological functions in nature. In this review, we first survey the known bioactive β-amino acid-containing natural products including nonribosomal peptides, macrolactam polyketides, and nucleoside-β-amino acid hybrids. Next, the biosynthetic enzymes that form β-amino acids from α-amino acids and the de novo synthesis of β-amino acids are summarized. Then, the mechanisms of β-amino acid incorporation into natural products are reviewed. Because it is anticipated that the rational swapping of the β-amino acid moieties with various side chains and stereochemistries by biosynthetic engineering should lead to the creation of novel architectures and bioactive compounds, the accumulation of knowledge regarding β-amino acid-containing natural product biosynthetic machinery could have a significant impact in this field. In addition, genome mining of characteristic β-amino acid biosynthetic genes and unique β-amino acid incorporation machinery could lead to the discovery of new β-amino acid-containing natural products.

  3. Raman spectra of carotenoids in natural products

    Science.gov (United States)

    Withnall, Robert; Chowdhry, Babur Z.; Silver, Jack; Edwards, Howell G. M.; de Oliveira, Luiz F. C.

    2003-08-01

    Resonance Raman spectra of naturally occurring carotenoids have been obtained from nautilus, periwinkle ( Littorina littorea) and clam shells under 514.5 nm excitation and these spectra are compared with the resonance Raman spectra obtained in situ from tomatoes, carrots, red peppers and saffron. The tomatoes, carrots and red peppers gave rise to resonance Raman spectra exhibiting a ν1 band at ca. 1520 cm -1, in keeping with its assignment to carotenoids with ca. nine conjugated carboncarbon double bonds in their main chains, whereas the resonance Raman spectrum of saffron showed a ν1 band at 1537 cm -1 which can be assigned to crocetin, having seven conjugated carboncarbon double bonds. A correlation between ν1 wavenumber location and effective conjugated chain length has been used to interpret the data obtained from the shells, and the wavenumber position (1522 cm -1) of the ν1 band of the carotenoid in the orange clam shell suggests that it contains nine conjugated double bonds in the main chain. However, the black periwinkle and nautilus shells exhibit ν1 bands at 1504 and 1496 cm -1, respectively. On the basis of the correlation between ν1 wavenumber location and effective conjugated chain length, this indicates that they contain carotenoids with longer conjugated chains, the former having ca. 11 double bonds and the latter ca. 13 or even more. Raman spectra of the nautilus, periwinkle and clam shells also exhibited a strong band at 1085 cm -1 and a doublet with components at 701 and 705 cm -1, which can be assigned to biogenic calcium carbonate in the aragonite crystallographic form.

  4. Natural and within-farmland biodiversity enhances crop productivity.

    Science.gov (United States)

    Carvalheiro, Luísa Gigante; Veldtman, Ruan; Shenkute, Awraris Getachew; Tesfay, Gebreamlak Bezabih; Pirk, Christian Walter Werner; Donaldson, John Sydney; Nicolson, Susan Wendy

    2011-03-01

    Ongoing expansion of large-scale agriculture critically threatens natural habitats and the pollination services they offer. Creating patches with high plant diversity within farmland is commonly suggested as a measure to benefit pollinators. However, farmers rarely adopt such practice, instead removing naturally occurring plants (weeds). By combining pollinator exclusion experiments with analysis of honeybee behaviour and flower-visitation webs, we found that the presence of weeds allowed pollinators to persist within sunflower fields, maximizing the benefits of the remaining patches of natural habitat to productivity of this large-scale crop. Weed diversity increased flower visitor diversity, hence ameliorating the measured negative effects of isolation from natural habitat. Although honeybees were the most abundant visitors, diversity of flower visitors enhanced honeybee movement, being the main factor influencing productivity. Conservation of natural patches combined with promoting flowering plants within crops can maximize productivity and, therefore, reduce the need for cropland expansion, contributing towards sustainable agriculture.

  5. Reinvigorating natural product combinatorial biosynthesis with synthetic biology.

    Science.gov (United States)

    Kim, Eunji; Moore, Bradley S; Yoon, Yeo Joon

    2015-09-01

    Natural products continue to play a pivotal role in drug-discovery efforts and in the understanding if human health. The ability to extend nature's chemistry through combinatorial biosynthesis--altering functional groups, regiochemistry and scaffold backbones through the manipulation of biosynthetic enzymes--offers unique opportunities to create natural product analogs. Incorporating emerging synthetic biology techniques has the potential to further accelerate the refinement of combinatorial biosynthesis as a robust platform for the diversification of natural chemical drug leads. Two decades after the field originated, we discuss the current limitations, the realities and the state of the art of combinatorial biosynthesis, including the engineering of substrate specificity of biosynthetic enzymes and the development of heterologous expression systems for biosynthetic pathways. We also propose a new perspective for the combinatorial biosynthesis of natural products that could reinvigorate drug discovery by using synthetic biology in combination with synthetic chemistry.

  6. Natural Product Polyamines That Inhibit Human Carbonic Anhydrases

    Directory of Open Access Journals (Sweden)

    Rohan A. Davis

    2014-01-01

    Full Text Available Natural product compound collections have proven an effective way to access chemical diversity and recent findings have identified phenolic, coumarin, and polyamine natural products as atypical chemotypes that inhibit carbonic anhydrases (CAs. CA enzymes are implicated as targets of variable drug therapeutic classes and the discovery of selective, drug-like CA inhibitors is essential. Just two natural product polyamines, spermine and spermidine, have until now been investigated as CA inhibitors. In this study, five more complex natural product polyamines 1–5, derived from either marine sponge or fungi, were considered for inhibition of six different human CA isozymes of interest in therapeutic drug development. All compounds share a simple polyamine core fragment, either spermine or spermidine, yet display substantially different structure activity relationships for CA inhibition. Notably, polyamines 1–5 were submicromolar inhibitors of the cancer drug target CA IX, this is more potent than either spermine or spermidine.

  7. Does species diversity limit productivity in natural grassland communities?

    NARCIS (Netherlands)

    Grace, James B.; Anderson, T. Michael; Smith, Melinda D.; Seabloom, Eric; Andelman, Sandy J.; Meche, Gayna; Weiher, Evan; Allain, Larry K.; Jutila, Heli; Sankaran, Mahesh; Knops, Johannes; Ritchie, Mark; Willig, Michael R.

    2007-01-01

    Theoretical analyses and experimental studies of synthesized assemblages indicate that under particular circumstances species diversity can enhance community productivity through niche complementarity. It remains unclear whether this process has important effects in mature natural ecosystems where c

  8. Revealing the macromolecular targets of complex natural products

    Science.gov (United States)

    Reker, Daniel; Perna, Anna M.; Rodrigues, Tiago; Schneider, Petra; Reutlinger, Michael; Mönch, Bettina; Koeberle, Andreas; Lamers, Christina; Gabler, Matthias; Steinmetz, Heinrich; Müller, Rolf; Schubert-Zsilavecz, Manfred; Werz, Oliver; Schneider, Gisbert

    2014-12-01

    Natural products have long been a source of useful biological activity for the development of new drugs. Their macromolecular targets are, however, largely unknown, which hampers rational drug design and optimization. Here we present the development and experimental validation of a computational method for the discovery of such targets. The technique does not require three-dimensional target models and may be applied to structurally complex natural products. The algorithm dissects the natural products into fragments and infers potential pharmacological targets by comparing the fragments to synthetic reference drugs with known targets. We demonstrate that this approach results in confident predictions. In a prospective validation, we show that fragments of the potent antitumour agent archazolid A, a macrolide from the myxobacterium Archangium gephyra, contain relevant information regarding its polypharmacology. Biochemical and biophysical evaluation confirmed the predictions. The results obtained corroborate the practical applicability of the computational approach to natural product ‘de-orphaning’.

  9. Does species diversity limit productivity in natural grassland communities?

    NARCIS (Netherlands)

    Grace, James B.; Anderson, T. Michael; Smith, Melinda D.; Seabloom, Eric; Andelman, Sandy J.; Meche, Gayna; Weiher, Evan; Allain, Larry K.; Jutila, Heli; Sankaran, Mahesh; Knops, Johannes; Ritchie, Mark; Willig, Michael R.

    Theoretical analyses and experimental studies of synthesized assemblages indicate that under particular circumstances species diversity can enhance community productivity through niche complementarity. It remains unclear whether this process has important effects in mature natural ecosystems where

  10. Nigerian Journal of Natural Products and Medicine - Vol 2 (1998)

    African Journals Online (AJOL)

    Nigerian Journal of Natural Products and Medicine - Vol 2 (1998) ... RESEARCH AND DEVELOPMENT INTO HERBAL MEDICINES · EMAIL FULL ... OF BRIDELIA FERRUGUBEA STEM BARK ON BLOOD CHEMISTRY AND HISTOLOGY OF ...

  11. Marine organisms: an alternative source of potentially valuable natural products

    Directory of Open Access Journals (Sweden)

    Alphonse Kelecom

    1991-01-01

    Full Text Available This paper recalls the outcoming of marine natural products research and reviews a selection of marirne bioactive metabolites in current use together with promising trends in marine pharmacology.

  12. Use of Brown Algae to Demonstrate Natural Products Techniques.

    Science.gov (United States)

    Porter, Lee A.

    1985-01-01

    Background information is provided on the natural products found in marine organisms in general and the brown algae in particular. Also provided are the procedures needed to isolate D-mannitol (a primary metabolite) and cholesterol from brown algae. (JN)

  13. Journals on Traditional Medicine and Natural Products Published in English

    Institute of Scientific and Technical Information of China (English)

    CONG Wei-hong; CHEN Ke-ji

    2010-01-01

    @@ Due to better understanding of traditional medicine, complementary and alternative medicine, and natural products, there are increasing findings in these fields.In order to facilitate the findings to be known widely and timely by readers, here this article showed researchers some journals on traditional medicine, complementary and alternative medicine,and natural products, published in English and tracked by Thomson Reuters (ISI) in 2009, as well as some influential journals untracked by ISI.

  14. Marine natural products sourced from marine-derived Penicillium fungi.

    Science.gov (United States)

    Ma, Hong-Guang; Liu, Qiang; Zhu, Guo-Liang; Liu, Hai-Shan; Zhu, Wei-Ming

    2016-01-01

    Marine micro-organisms have been proven to be a major source of marine natural products (MNPs) in recent years, in which filamentous fungi are a vital source of bioactive natural products for their large metagenomes and more complex genetic backgrounds. This review highlights the 390 new MNPs from marine-derived Penicillium fungi during 1991 to 2014. These new MNPs are categorized based on the environment sources of the fungal hosts and their bioactivities are summarized.

  15. Emerging trends in the discovery of natural product antibacterials

    DEFF Research Database (Denmark)

    Bologa, Cristian G; Ursu, Oleg; Oprea, Tudor;

    2013-01-01

    mechanisms. Special emphasis is given to the strengths, weaknesses, and opportunities in the natural product antibacterial drug discovery arena, and to emerging applications driven by advances in bioinformatics, chemical biology, and synthetic biology in concert with exploiting bacterial phenotypes....... These efforts have identified a critical mass of natural product antibacterial lead compounds and discovery technologies with high probability of successful implementation against emerging bacterial pathogens....

  16. Total synthesis and biological activity of natural product Urukthapelstatin A.

    Science.gov (United States)

    Lin, Chun-Chieh; Tantisantisom, Worawan; McAlpine, Shelli R

    2013-07-19

    Herein we report the first total synthesis of the natural product Urkuthaplestatin A (Ustat A) utilizing a convergent synthetic strategy. The characterization and biological activity match those of the previously published natural product. Interestingly, several intermediates, including the linear and serine cyclized precursors, show a 100-fold decrease in cytotoxicity, with IC50's in the low micromolar range. These data indicate that the rigidity and the consecutive aromatic heterocyclic system are responsible for the biological activity.

  17. Case Studies of the Synthesis of Bioactive Cyclodepsipeptide Natural Products

    Directory of Open Access Journals (Sweden)

    Markus Kaiser

    2013-01-01

    Full Text Available Cyclodepsipeptide natural products often display intriguing biological activities that along with their complex molecular scaffolds, makes them interesting targets for chemical synthesis. Although cyclodepsipeptides feature highly diverse chemical structures, their synthesis is often associated with similar synthetic challenges such as the establishment of a suitable macrocyclization methodology. This review therefore compiles case studies of synthetic approaches to different bioactive cyclodepsipeptide natural products, thereby illustrating obstacles of cyclodepsipeptide synthesis as well as their overcomings.

  18. Anti-Enterovirus 71 Agents of Natural Products

    Directory of Open Access Journals (Sweden)

    Liyan Wang

    2015-09-01

    Full Text Available This review, with 42 references, presents the fascinating area of anti-enterovirus 71 natural products over the last three decades for the first time. It covers literature published from 2005–2015 and refers to compounds isolated from biogenic sources. In total, 58 naturally-occurring anti-EV71 compounds are recorded.

  19. Biotechnological production of natural zero-calorie sweeteners.

    Science.gov (United States)

    Philippe, Ryan N; De Mey, Marjan; Anderson, Jeff; Ajikumar, Parayil Kumaran

    2014-04-01

    The increasing public awareness of adverse health impacts from excessive sugar consumption has created increasing interest in plant-derived, natural low-calorie or zero-calorie sweeteners. Two plant species which contain natural sweeteners, Stevia rebaudiana and Siraitia grosvenorii, have been extensively profiled to identify molecules with high intensity sweetening properties. However, sweetening ability does not necessarily make a product viable for commercial applications. Some criteria for product success are proposed to identify which targets are likely to be accepted by consumers. Limitations of plant-based production are discussed, and a case is put forward for the necessity of biotechnological production methods such as plant cell culture or microbial fermentation to meet needs for commercial-scale production of natural sweeteners.

  20. The sustainable management of a productive natural capital

    DEFF Research Database (Denmark)

    Daubanes, Julien Xavier

    This paper examines an industry whose economic activity uses a natural capital on which its profit also relies. When such a productive natural capital has a limited capacity to recover from its exploitation, a free market tends to over-exploit it, calling for public intervention. The analysis...... is relevant, among other examples, to the case of naturebased tourism. I study the sustainable management of a productive natural capital: the conditions under which its exploitation generates maximum long-run social benefits; the various ways in which a regulator can implement such an exploitation; the rent...

  1. Natural product biosynthesis: It's all downhill from here

    Science.gov (United States)

    Hornsby, Charles E.; Paton, Robert S.

    2014-02-01

    High selectivity is essential in the enzymatic biosynthesis of complex natural products. Now, the discovery of multiple sequential bifurcations on the reaction path towards the formation of a diterpenoid shows how dynamics affect selectivity, and suggests how enzymes may steer reactions towards a specific product.

  2. Nature-Inspired Design: Strategies for Sustainable Product Development

    NARCIS (Netherlands)

    De Pauw, I.C.

    2015-01-01

    Product designers can apply different strategies, methods, and tools for sustainable product development. Nature-Inspired Design Strategies (NIDS) offer designers a distinct class of strategies that use ‘nature’ as a guiding source of knowledge and inspiration for addressing sustainability. Biomimic

  3. Nature-Inspired Design: Strategies for Sustainable Product Development

    NARCIS (Netherlands)

    De Pauw, I.C.

    2015-01-01

    Product designers can apply different strategies, methods, and tools for sustainable product development. Nature-Inspired Design Strategies (NIDS) offer designers a distinct class of strategies that use ‘nature’ as a guiding source of knowledge and inspiration for addressing

  4. Nature-Inspired Design: Strategies for Sustainable Product Development

    NARCIS (Netherlands)

    De Pauw, I.C.

    2015-01-01

    Product designers can apply different strategies, methods, and tools for sustainable product development. Nature-Inspired Design Strategies (NIDS) offer designers a distinct class of strategies that use ‘nature’ as a guiding source of knowledge and inspiration for addressing sustainability. Biomimic

  5. Screening strategies for discovery of antibacterial natural products.

    Science.gov (United States)

    Singh, Sheo B; Young, Katherine; Miesel, Lynn

    2011-08-01

    Microbial-derived natural products have been a traditional source of antibiotics and antibiotic leads and continue to be effective sources of antibiotics today. The most important of these discoveries were made about 50 years ago. Chemical modifications of natural products discovered during those years continue to produce new clinical agents but their value is now, unfortunately, fading away owing to the exhaustion of opportunities of chemical modifications. The discovery of new natural antibiotics is directly linked to new screening technologies, particularly technologies that can help to eliminate the rediscovery of known antibiotics. In this article, we have reviewed the screening technologies from recent literature as well as originating from authors laboratories that were used for the screening of natural products. The article covers the entire spectrum of screening strategies, including classical empiric whole-cell assays to more sophisticated antisense based hypersensitive Staphylococcus aureus Fitness Test assays designed to screen all targets simultaneously. These technologies have led to the discovery of a series of natural product antibiotics, which have been summarized, including the discovery of platensimycin, platencin, nocathiacins, philipimycin, cyclothialidine and muryamycins. It is quite clear that natural products provide a tremendous opportunity to discover new antibiotics when combined with new hyper-sensitive whole-cell technologies.

  6. Natural Products Towards the Discovery of Potential Future Antithrombotic Drugs.

    Science.gov (United States)

    Islam, Md Asiful; Alam, Fahmida; Khalil, Md Ibrahim; Sasongko, Teguh Haryo; Gan, Siew Hua

    2016-01-01

    Globally, thrombosis-associated disorders are one of the main contributors to fatalities. Besides genetic influences, there are some acquired and environmental risk factors dominating thrombotic diseases. Although standard regimens have been used for a long time, many side effects still occur which can be life threatening. Therefore, natural products are good alternatives. Although the quest for antithrombotic natural products came to light only since the end of last century, in the last two decades, a considerable number of natural products showing antithrombotic activities (antiplatelet, anticoagulant and fibrinolytic) with no or minimal side effects have been reported. In this review, several natural products used as antithrombotic agents including medicinal plants, vegetables, fruits, spices and edible mushrooms which have been discovered in the last 15 years and their target sites (thrombogenic components, factors and thrombotic pathways) are described. In addition, the side effects, limitations and interactions of standard regimens with natural products are also discussed. The active compounds could serve as potential sources for future research on antithrombotic drug development. As a future direction, more advanced researches (in quest of the target cofactor or component involved in antithrombotic pathways) are warranted for the development of potential natural antithrombotic medications (alone or combined with standard regimens) to ensure maximum safety and efficacy.

  7. Plant-Derived Natural Products for Parkinson's Disease Therapy.

    Science.gov (United States)

    Sengupta, T; Vinayagam, J; Singh, R; Jaisankar, P; Mohanakumar, K P

    2016-01-01

    Plant-derived natural products have made their own niche in the treatment of neurological diseases since time immemorial. Parkinson's disease (PD), the second most prevalent neurodegenerative disorder, has no cure and the treatment available currently is symptomatic. This chapter thoughtfully and objectively assesses the scientific basis that supports the increasing use of these plant-derived natural products for the treatment of this chronic and progressive disorder. Proper considerations are made on the chemical nature, sources, preclinical tests and their validity, and mechanisms of behavioural or biochemical recovery observed following treatment with various plants derived natural products relevant to PD therapy. The scientific basis underlying the neuroprotective effect of 6 Ayurvedic herbs/formulations, 12 Chinese medicinal herbs/formulations, 33 other plants, and 5 plant-derived molecules have been judiciously examined emphasizing behavioral, cellular, or biochemical aspects of neuroprotection observed in the cellular or animal models of the disease. The molecular mechanisms triggered by these natural products to promote cell survivability and to reduce the risk of cellular degeneration have also been brought to light in this study. The study helped to reveal certain limitations in the scenario: lack of preclinical studies in all cases barring two; heavy dependence on in vitro test systems; singular animal or cellular model to establish any therapeutic potential of drugs. This strongly warrants further studies so as to reproduce and confirm these reported effects. However, the current literature offers scientific credence to traditionally used plant-derived natural products for the treatment of PD.

  8. Chitin elicitation of natural product production in marine bacteria

    DEFF Research Database (Denmark)

    Månsson, Maria; Wietz, Matthias; Larsen, Thomas Ostenfeld

    Genome sequences reveal that our current standard laboratory conditions only support a fraction of the potential secondary metabolism in bacteria.1 Thus, we must rethink cultivation, detection, and isolation strategies for bacterial secondary metabolites in order to explore the huge, so far...... uncharacterized chemical potential of these organisms. As part of a new project on ecology-driven drug discovery at the Technical University of Denmark, we investigate the use of chitin to elicit or alter production of antibacterial compounds in marine bacteria. Within our large collection of Gram......-negative bacteria (mainly Pseudoalteromonas and Vibrio), we found that some strains were capable of producing antibacterial compounds when grown on chitin, an N-acetyl-D-glucosamine polymer found in the exoskeleton of zooplankton.2 A strain of Vibrio coralliilyticus solely produced the antibiotic andrimid,3...

  9. Carcass traits of improved and indigenous lamb breeds of North-Western Turkey under an intensive production system

    Directory of Open Access Journals (Sweden)

    Omur Kocak

    2010-01-01

    Full Text Available The aim of study was to investigate the carcass quality of Turkish Merino, Ramlic, Kivircik, Chios and Imroz breeds in north-western Turkey under an intensive production system. After weaning at approximately 85 days of age, 46 lambs from Turkish Merino, Ramlic, Kivircik, Chios and Imroz breeds were fattened for 56 days. Slaughter weights were 47.39, 45.68, 47.27, 31.08 and 29.82 kg and chilled carcass weights were 23.35, 22.33, 23.51, 14.33 and 13.75 kg, respectively (P<0.001. Improved Turkish Merino and Ramlic and indigenous Kivircik lambs had higher carcass measurements than indigenous Chios and Imroz lambs. Chios lamb carcasses had the highest tail root fat yellowness and tail percentage while having the lowest fatness score, omental and mesenteric fat percentage and kidney knob and channel fat percentage. Turkish Merino lambs had higher shoulder percentage, lean percentage and lean/total fat ratio in the hind leg and produced less total fat in the hind leg than Ramlic and Kivircik lambs. These results indicate that improved Turkish Merino might be used to produce high quality lamb carcasses in north-western Turkey. Among indigenous breeds Kivircik showed an outstanding carcass production performance.

  10. Computer-Aided Drug Design of Bioactive Natural Products.

    Science.gov (United States)

    Prachayasittikul, Veda; Worachartcheewan, Apilak; Shoombuatong, Watshara; Songtawee, Napat; Simeon, Saw; Prachayasittikul, Virapong; Nantasenamat, Chanin

    2015-01-01

    Natural products have been an integral part of sustaining civilizations because of their medicinal properties. Past discoveries of bioactive natural products have relied on serendipity, and these compounds serve as inspiration for the generation of analogs with desired physicochemical properties. Bioactive natural products with therapeutic potential are abundantly available in nature and some of them are beyond exploration by conventional methods. The effectiveness of computational approaches as versatile tools for facilitating drug discovery and development has been recognized for decades, without exception, in the case of natural products. In the post-genomic era, scientists are bombarded with data produced by advanced technologies. Thus, rendering these data into knowledge that is interpretable and meaningful becomes an essential issue. In this regard, computational approaches utilize the existing data to generate knowledge that provides valuable understanding for addressing current problems and guiding the further research and development of new natural-derived drugs. Furthermore, several medicinal plants have been continuously used in many traditional medicine systems since antiquity throughout the world, and their mechanisms have not yet been elucidated. Therefore, the utilization of computational approaches and advanced synthetic techniques would yield great benefit to improving the world's health population and well-being.

  11. The Traditional Medicine and Modern Medicine from Natural Products

    Directory of Open Access Journals (Sweden)

    Haidan Yuan

    2016-04-01

    Full Text Available Natural products and traditional medicines are of great importance. Such forms of medicine as traditional Chinese medicine, Ayurveda, Kampo, traditional Korean medicine, and Unani have been practiced in some areas of the world and have blossomed into orderly-regulated systems of medicine. This study aims to review the literature on the relationship among natural products, traditional medicines, and modern medicine, and to explore the possible concepts and methodologies from natural products and traditional medicines to further develop drug discovery. The unique characteristics of theory, application, current role or status, and modern research of eight kinds of traditional medicine systems are summarized in this study. Although only a tiny fraction of the existing plant species have been scientifically researched for bioactivities since 1805, when the first pharmacologically-active compound morphine was isolated from opium, natural products and traditional medicines have already made fruitful contributions for modern medicine. When used to develop new drugs, natural products and traditional medicines have their incomparable advantages, such as abundant clinical experiences, and their unique diversity of chemical structures and biological activities.

  12. The Traditional Medicine and Modern Medicine from Natural Products.

    Science.gov (United States)

    Yuan, Haidan; Ma, Qianqian; Ye, Li; Piao, Guangchun

    2016-04-29

    Natural products and traditional medicines are of great importance. Such forms of medicine as traditional Chinese medicine, Ayurveda, Kampo, traditional Korean medicine, and Unani have been practiced in some areas of the world and have blossomed into orderly-regulated systems of medicine. This study aims to review the literature on the relationship among natural products, traditional medicines, and modern medicine, and to explore the possible concepts and methodologies from natural products and traditional medicines to further develop drug discovery. The unique characteristics of theory, application, current role or status, and modern research of eight kinds of traditional medicine systems are summarized in this study. Although only a tiny fraction of the existing plant species have been scientifically researched for bioactivities since 1805, when the first pharmacologically-active compound morphine was isolated from opium, natural products and traditional medicines have already made fruitful contributions for modern medicine. When used to develop new drugs, natural products and traditional medicines have their incomparable advantages, such as abundant clinical experiences, and their unique diversity of chemical structures and biological activities.

  13. Capillary electrophoresis of natural products: 2011-2012.

    Science.gov (United States)

    Tubaon, Ria Marni S; Rabanes, Heide; Haddad, Paul R; Quirino, Joselito P

    2014-01-01

    Bioactive natural products are major sources of lead compounds for drug discovery and pharmaceutical development, therefore, innovative and current separation and characterization techniques are important for these compounds. Here, CE methods applied for the analysis of natural products published during 2011-2012 are reviewed. This is an updated version of an earlier review paper in this journal, which highlighted developments during 2006-2010. The major method developments over the review period centered on derivatization, chiral analysis, modes of detection, stacking or on-line sample concentration, and sample preparation (predominantly using extraction methods). The samples analyzed were herbal products, foods, soil, and biological samples. Developments also occurred in the areas of quality control, toxicology assessment, and enzyme-inhibitor screening. A table that summarizes the areas, source of natural product, nature of the bioactive analyte, CE conditions, LODs, and corresponding reference is provided. A short description on the theory of CE and insights on future activities of CE on natural products are also presented.

  14. Culture-independent discovery of natural products from soil metagenomes.

    Science.gov (United States)

    Katz, Micah; Hover, Bradley M; Brady, Sean F

    2016-03-01

    Bacterial natural products have proven to be invaluable starting points in the development of many currently used therapeutic agents. Unfortunately, traditional culture-based methods for natural product discovery have been deemphasized by pharmaceutical companies due in large part to high rediscovery rates. Culture-independent, or "metagenomic," methods, which rely on the heterologous expression of DNA extracted directly from environmental samples (eDNA), have the potential to provide access to metabolites encoded by a large fraction of the earth's microbial biosynthetic diversity. As soil is both ubiquitous and rich in bacterial diversity, it is an appealing starting point for culture-independent natural product discovery efforts. This review provides an overview of the history of soil metagenome-driven natural product discovery studies and elaborates on the recent development of new tools for sequence-based, high-throughput profiling of environmental samples used in discovering novel natural product biosynthetic gene clusters. We conclude with several examples of these new tools being employed to facilitate the recovery of novel secondary metabolite encoding gene clusters from soil metagenomes and the subsequent heterologous expression of these clusters to produce bioactive small molecules.

  15. An Innovative Methodology of Product Design from Nature

    Institute of Scientific and Technical Information of China (English)

    Hui-I Wen; Shu-jun Zhang; Kevin Hapeshi; Xiao-feng Wang

    2008-01-01

    Nature is an information sourcebeok of behaviour, function, colour and shape which can inspire visual design and invention. Studying the form and functional characteristics of a natural object can provide inspiration for product design and help to improve the marketability of manufactured products. The inspiration can be triggered either by direct observation or captured by threo-dimensional (3D) digitising techniques to obtain superficial information (geometry and colour). An art designer often creates a concept in the form of a two-dimensional (2D) sketch while engineering methods lead to a point cloud in 3D. Each has its limitations in that the art designer commonly lacks the knowledge to build a final product from a 2D sketch and the engineering designer's 3D point clouds may not be very beautiful. We propose a method for Product Design from Nature (PDN),coupling aesthetic intent and geometrical characteristics, exploring the interactions between designers and nature's systems in PDN. We believe that this approach would considerably reduce the lead time and cost of product design from nature.

  16. Potential antimalarials from African natural products: A reviw.

    Science.gov (United States)

    Lawal, Bashir; Shittu, Oluwatosin Kudirat; Kabiru, Adamu Yusuf; Jigam, Ali Audu; Umar, Maimuna Bello; Berinyuy, Eustace Bonghan; Alozieuwa, Blessing Uchenna

    2015-01-01

    Malaria remains an overwhelming infectious disease with significant health challenges in African and other endemic countries globally. Resistance to antimalarial drugs has become one of the most momentous challenges to human health, and thus has necessitated the hunt for new and effective drugs. Consequently, few decades have witnessed a surfeit of research geared to validate the effectiveness of commonly used traditionally medicines against malaria fever. The present review work focuses on documenting natural products from African whose activity has been reported in vivo or in vitro against malaria parasite. Literature was collected using electronic search of published articles (Google Scholar, PubMed, Medline, Sciencedirect, and Science domain) that report on antiplasmodial activity of natural products from differernts Africa region. A total of 652 plant taxa from 146 families, 134 isolated antimalarial compounds from 39 plants species, 2 herbal formulations and 4 insect/products were found to be reported in literature from 1996 to 2015. Plants species from family Asteraceae (11.04%), Fababceae (8.128%), Euphorbiaceae (5.52%), Rubiaceas (5.52%), and Apocyanaceae (5.214%), have received more scientific validation than others. African natural products possess remarkable healing properties as revealed in the various citations as promising antimalarial agents. Some of these natural products from Africa demonstrate high, promising or low activities against Plasmodium parasite. This study also shows that natural products from Africa have a huge amount of novel antimalarial compounds that could serve as a leads for the development of new and effective antiplasmodial drugs. However, in a view of bridging the gap in knowledge, clinical validation of these natural products are of paramount importance.

  17. Establishment of new crops for the production of natural rubber.

    Science.gov (United States)

    van Beilen, Jan B; Poirier, Yves

    2007-11-01

    Natural rubber is a unique biopolymer of strategic importance that, in many of its most significant applications, cannot be replaced by synthetic alternatives. The rubber tree Hevea brasiliensis is the almost exclusive commercial source of natural rubber currently and alternative crops should be developed for several reasons, including: a disease risk to the rubber tree that could potentially decimate current production, a predicted shortage of natural rubber supply, increasing allergic reactions to rubber obtained from the Brazilian rubber tree and a general shift towards renewables. This review summarizes our knowledge of plants that can serve as alternative sources of natural rubber, of rubber biosynthesis and the scientific gaps that must be filled to bring the alternative crops into production.

  18. Natural product modulators to overcome multidrug resistance in cancer.

    Science.gov (United States)

    Cort, Aysegul; Ozben, Tomris

    2015-01-01

    Multidrug resistance (MDR) is a condition that makes cells simultaneously unresponsive to different drugs, unrelated to their chemical structure and mechanism of action. MDR caused by the presence and overexpression of ABC transporters makes obstacles in cancer treatment and lower the effectiveness of chemotherapy. Natural products are investigated by many researchers as MDR modulators for their low toxicity and potent, selective behavior. When coadministered, MDR modulators compete with cytotoxic agents for binding to the active site of the membrane transporters and reduce drug efflux. Natural product-based drugs are important in struggling against drug resistance during cancer therapy. This review is focused on the potential mechanisms against drug resistance, the development of inhibitors for ABC drug transporters, natural product modulators, and nanoparticle drug delivery.

  19. Dietary Natural Products for Prevention and Treatment of Liver Cancer

    Science.gov (United States)

    Zhou, Yue; Li, Ya; Zhou, Tong; Zheng, Jie; Li, Sha; Li, Hua-Bin

    2016-01-01

    Liver cancer is the most common malignancy of the digestive system with high death rate. Accumulating evidences suggests that many dietary natural products are potential sources for prevention and treatment of liver cancer, such as grapes, black currant, plum, pomegranate, cruciferous vegetables, French beans, tomatoes, asparagus, garlic, turmeric, ginger, soy, rice bran, and some edible macro-fungi. These dietary natural products and their active components could affect the development and progression of liver cancer in various ways, such as inhibiting tumor cell growth and metastasis, protecting against liver carcinogens, immunomodulating and enhancing effects of chemotherapeutic drugs. This review summarizes the potential prevention and treatment activities of dietary natural products and their major bioactive constituents on liver cancer, and discusses possible mechanisms of action. PMID:26978396

  20. Plant extracts as natural antioxidants in meat and meat products.

    Science.gov (United States)

    Shah, Manzoor Ahmad; Bosco, Sowriappan John Don; Mir, Shabir Ahmad

    2014-09-01

    Antioxidants are used to minimize the oxidative changes in meat and meat products. Oxidative changes may have negative effects on the quality of meat and meat products, causing changes in their sensory and nutritional properties. Although synthetic antioxidants have already been used but in recent years, the demand for natural antioxidants has been increased mainly because of adverse effects of synthetic antioxidants. Thus most of the recent investigations have been directed towards the identification of natural antioxidants from various plant sources. Plant extracts have been prepared using different solvents and extraction methods. Grape seed, green tea, pine bark, rosemary, pomegranate, nettle and cinnamon have exhibited similar or better antioxidant properties compared to some synthetic ones. This review provides the recent information on plant extracts used as natural antioxidants in meat and meat products, specifically red meat. Copyright © 2014 Elsevier Ltd. All rights reserved.

  1. Bioactive natural products from Chinese marine flora and fauna

    Institute of Scientific and Technical Information of China (English)

    Zhen-fang ZHOU; Yue-wei GUO

    2012-01-01

    In recent decades,the pharmaceutical application potential of marine natural products has attracted much interest from both natural product chemists and pharmacologists.Our group has long been engaged in the search for bioactive natural products from Chinese marine flora (such as mangroves and algae) and fauna (including sponges,soft corals,and mollusks),resulting in the isolation and characterization of numerous novel secondary metabolites spanning a wide range of structural classes and various biosynthetic origins.Of particular interest is the fact that many of these compounds show promising biological activities,including cytotoxic,antibacterial,and enzyme inhibitory effects- By describing representative studies,this review presents a comprehensive summary regarding the achievements and progress made by our group in the past decade.Several interesting examples are discussed in detail.

  2. Dietary Natural Products for Prevention and Treatment of Liver Cancer

    Directory of Open Access Journals (Sweden)

    Yue Zhou

    2016-03-01

    Full Text Available Liver cancer is the most common malignancy of the digestive system with high death rate. Accumulating evidences suggests that many dietary natural products are potential sources for prevention and treatment of liver cancer, such as grapes, black currant, plum, pomegranate, cruciferous vegetables, French beans, tomatoes, asparagus, garlic, turmeric, ginger, soy, rice bran, and some edible macro-fungi. These dietary natural products and their active components could affect the development and progression of liver cancer in various ways, such as inhibiting tumor cell growth and metastasis, protecting against liver carcinogens, immunomodulating and enhancing effects of chemotherapeutic drugs. This review summarizes the potential prevention and treatment activities of dietary natural products and their major bioactive constituents on liver cancer, and discusses possible mechanisms of action.

  3. In situ natural product discovery via an artificial marine sponge.

    Directory of Open Access Journals (Sweden)

    James J La Clair

    Full Text Available There is continuing international interest in exploring and developing the therapeutic potential of marine-derived small molecules. Balancing the strategies for ocean based sampling of source organisms versus the potential to endanger fragile ecosystems poses a substantial challenge. In order to mitigate such environmental impacts, we have developed a deployable artificial sponge. This report provides details on its design followed by evidence that it faithfully recapitulates traditional natural product collection protocols. Retrieving this artificial sponge from a tropical ecosystem after deployment for 320 hours afforded three actin-targeting jasplakinolide depsipeptides that had been discovered two decades earlier using traditional sponge specimen collection and isolation procedures. The successful outcome achieved here could reinvigorate marine natural products research, by producing new environmentally innocuous sources of natural products and providing a means to probe the true biosynthetic origins of complex marine-derived scaffolds.

  4. Anti-cancer natural products isolated from chinese medicinal herbs

    Directory of Open Access Journals (Sweden)

    Wu Guosheng

    2011-07-01

    Full Text Available Abstract In recent years, a number of natural products isolated from Chinese herbs have been found to inhibit proliferation, induce apoptosis, suppress angiogenesis, retard metastasis and enhance chemotherapy, exhibiting anti-cancer potential both in vitro and in vivo. This article summarizes recent advances in in vitro and in vivo research on the anti-cancer effects and related mechanisms of some promising natural products. These natural products are also reviewed for their therapeutic potentials, including flavonoids (gambogic acid, curcumin, wogonin and silibinin, alkaloids (berberine, terpenes (artemisinin, β-elemene, oridonin, triptolide, and ursolic acid, quinones (shikonin and emodin and saponins (ginsenoside Rg3, which are isolated from Chinese medicinal herbs. In particular, the discovery of the new use of artemisinin derivatives as excellent anti-cancer drugs is also reviewed.

  5. Knowledge based decision making: perspective on natural gas production

    Energy Technology Data Exchange (ETDEWEB)

    Ydstie, B. Erik; Stuland, Kjetil M.

    2009-07-01

    Conclusions (drawn by the author): Decarbonization of energy sources - From coal to renewable. Natural Gas Abundantly available - Norway is no. 3 exporter. Natural gas important as - Hydrogen source for chemicals; - Electricity; - End consumer usage (heating etc). Large potential for application of model based decision making; - Where and when to install platforms and drill wells - How to operate platforms and pipeline systems; - How to operate and optimize chemical production; - Optimization of electricity generation systems. (author)

  6. Marine actinobacteria: an important source of bioactive natural products.

    Science.gov (United States)

    Manivasagan, Panchanathan; Kang, Kyong-Hwa; Sivakumar, Kannan; Li-Chan, Eunice C Y; Oh, Hyun-Myung; Kim, Se-Kwon

    2014-07-01

    Marine environment is largely an untapped source for deriving actinobacteria, having potential to produce novel, bioactive natural products. Actinobacteria are the prolific producers of pharmaceutically active secondary metabolites, accounting for about 70% of the naturally derived compounds that are currently in clinical use. Among the various actinobacterial genera, Actinomadura, Actinoplanes, Amycolatopsis, Marinispora, Micromonospora, Nocardiopsis, Saccharopolyspora, Salinispora, Streptomyces and Verrucosispora are the major potential producers of commercially important bioactive natural products. In this respect, Streptomyces ranks first with a large number of bioactive natural products. Marine actinobacteria are unique enhancing quite different biological properties including antimicrobial, anticancer, antiviral, insecticidal and enzyme inhibitory activities. They have attracted global in the last ten years for their ability to produce pharmaceutically active compounds. In this review, we have focused attention on the bioactive natural products isolated from marine actinobacteria, possessing unique chemical structures that may form the basis for synthesis of novel drugs that could be used to combat resistant pathogenic microorganisms. Copyright © 2014 Elsevier B.V. All rights reserved.

  7. Marine Natural Products as Models to Circumvent Multidrug Resistance.

    Science.gov (United States)

    Long, Solida; Sousa, Emília; Kijjoa, Anake; Pinto, Madalena M M

    2016-07-08

    Multidrug resistance (MDR) to anticancer drugs is a serious health problem that in many cases leads to cancer treatment failure. The ATP binding cassette (ABC) transporter P-glycoprotein (P-gp), which leads to premature efflux of drugs from cancer cells, is often responsible for MDR. On the other hand, a strategy to search for modulators from natural products to overcome MDR had been in place during the last decades. However, Nature limits the amount of some natural products, which has led to the development of synthetic strategies to increase their availability. This review summarizes the research findings on marine natural products and derivatives, mainly alkaloids, polyoxygenated sterols, polyketides, terpenoids, diketopiperazines, and peptides, with P-gp inhibitory activity highlighting the established structure-activity relationships. The synthetic pathways for the total synthesis of the most promising members and analogs are also presented. It is expected that the data gathered during the last decades concerning their synthesis and MDR-inhibiting activities will help medicinal chemists develop potential drug candidates using marine natural products as models which can deliver new ABC transporter inhibitor scaffolds.

  8. The impact of natural products upon modern drug discovery.

    Science.gov (United States)

    Ganesan, A

    2008-06-01

    In the period 1970-2006, a total of 24 unique natural products were discovered that led to an approved drug. We analyze these successful leads in terms of drug-like properties, and show that they can be divided into two equal subsets. The first falls in the 'Lipinski universe' and complies with the Rule of Five. The second is a 'parallel universe' that violates the rules. Nevertheless, the latter compounds remain largely compliant in terms of logP and H-bond donors, highlighting the importance of these two metrics in predicting bioavailability. Natural products are often cited as an exception to Lipinski's rules. We believe this is because nature has learned to maintain low hydrophobicity and intermolecular H-bond donating potential when it needs to make biologically active compounds with high molecular weight and large numbers of rotatable bonds. In addition, natural products are more likely than purely synthetic compounds to resemble biosynthetic intermediates or endogenous metabolites, and hence take advantage of active transport mechanisms. Interestingly, the natural product leads in the Lipinski and parallel universe had an identical success rate (50%) in delivering an oral drug.

  9. SCHEMES OF GAS PRODUCTION FROM NATURAL GAS HYDRATES

    Institute of Scientific and Technical Information of China (English)

    李淑霞; 陈月明; 杜庆军

    2003-01-01

    Natural gas hydrates are a kind of nonpolluting and high quality energy resources for future, the reserves of which are about twice of the carbon of the current fossil energy (petroleum, natural gas and coal) on the earth. And it will be the most important energy for the 21st century. The energy balance and numerical simulation are applied to study the schemes of the natural gas hydrates production in this paper,and it is considered that both depressurization and thermal stimulation are effective methods for exploiting natural gas hydrates, and that the gas production of the thermal stimulation is higher than that of the depressurization. But thermal stimulation is non-economic because it requires large amounts of energy.Therefore the combination of the two methods is a preferable method for the current development of the natural gas hydrates. The main factors which influence the production of natural gas hydrates are: the temperature of injected water, the injection rate, the initial saturation of the hydrates and the initial temperature of the reservoir which is the most important factor.

  10. Patentability potential of natural products for xerostomia treatment

    OpenAIRE

    2016-01-01

    Xerostomia is characterized as a symptom caused by hyposalivation, which can occur for reasons such as age, polypharmacy, radiation therapy, among others. Currently,few products are available for the treatment of xerostomia, which is a subject still underestimated by many health professionals. Thus, we searched patents applied and approved in Brazil on xerostomia, to verify the existing innovation involving natural products. We found 33 patents applied and approved in Brazil, many of them usi...

  11. Idaho Habitat and Natural Production Monitoring : Annual Report 1989.

    Energy Technology Data Exchange (ETDEWEB)

    Kiefer, Russell B.; Forster, Katharine A.

    1991-01-01

    Project 83-7 was established under the Northwest Power Planning Council's 1982 Fish and Wildlife Program to monitor natural production of anadromous fish, evaluate Bonneville Power Administration (BPA) habitat improvement projects, and develop a credit record for off-site mitigation projects in Idaho. Project 83-7 is divided into two subprojects: general and intensive monitoring. Primary objectives of the general monitoring subproject (Part 1) are to determine natural production increases due to habitat improvement projects in terms of parr production and to determine natural production status and trends in Idaho. The second objective is accomplished by combining parr density data from monitoring and evaluation of BPA habitat projects and from other Idaho Department of Fish and Game (IDFG) management and research activities. Primary objectives of the intensive monitoring subproject (Part 2) are to determine the number of returning chinook and steelhead adults necessary to achieve optimal smolt production and to develop mitigation accounting based on increases in smolt production. Two locations are being intensively studied to meet these objectives. Field work began in 1987 in the upper Salmon River and Crooked River (South Fork Clearwater River tributary). 22 refs., 10 figs., 17 tabs.

  12. Pseudomonas putida—a versatile host for the production of natural products

    OpenAIRE

    Loeschcke, Anita; Thies, Stephan

    2015-01-01

    The biosynthesis of natural products by heterologous expression of biosynthetic pathways in amenable production strains enables biotechnological access to a variety of valuable compounds by conversion of renewable resources. Pseudomonas putida has emerged as a microbial laboratory work horse, with elaborated techniques for cultivation and genetic manipulation available. Beyond that, this bacterium offers several particular advantages with regard to natural product biosynthesis, notably a vers...

  13. The EROI of Conventional Canadian Natural Gas Production

    Directory of Open Access Journals (Sweden)

    Jon Freise

    2011-11-01

    Full Text Available Canada was the world’s third largest natural gas producer in 2008, with 98% of its gas being produced by conventional, tight gas, and coal bed methane wells in Western Canada. Natural gas production in Western Canada peaked in 2001 and remained nearly flat until 2006 despite more than quadrupling the drilling rate. Canada seems to be one of many counter examples to the idea that oil and gas production can rise with sufficient investment. This study calculated the Energy Return on Energy Invested and Net Energy of conventional natural gas and oil production in Western Canada by a variety of methods to explore the energy dynamics of the peaking process. All these methods show a downward trend in EROI during the last decade. Natural gas EROI fell from 38:1 in 1993 to 15:1 at the peak of drilling in 2005. The drilling intensity for natural gas was so high that net energy delivered to society peaked in 2000–2002, while production did not peak until 2006. The industry consumed all the extra energy it delivered to maintain the high drilling effort. The inability of a region to increase net energy may be the best definition of peak production. This increase in energy consumption reduces the total energy provided to society and acts as a contracting pressure on the overall economy as the industry consumes greater quantities of labor, steel, concrete and fuel. It appears that energy production from conventional oil and gas in Western Canada has peaked and entered permanent decline.

  14. Natural products as storage media for avulsed tooth

    Directory of Open Access Journals (Sweden)

    Deepika Jain

    2015-01-01

    Full Text Available Avulsion of tooth is complete displacement of tooth out of its socket that results in mutilation of periodontal ligaments. The desirable treatment option is replantation of the tooth. However, unsuccessful replantation is a matter of great discontentment. Unsuccessful replantation is due to inappropriate management of the avulsed tooth. Protection of teeth from desiccation due to drying of the periodontal ligament tissue, by keeping it in storage media can improve the outcome of the treatment. This review paper focuses on the use of natural products as storage media for avulsed teeth. In vitro and in vivo research published during 1995-2014, allowing open access on National Center for Biotechnology Information (NCBI database and articles on EBSCO host (EBSCO-Elton B. Stephens Company were included. It was found that natural products such as milk, coconut water, propolis, green tea, red mulberry, Aloe vera, egg-white and pomegranate have shown ability to maintain viability of periodontal ligament cells of avulsed teeth. Few natural products such as coconut water and milk can be used in raw form, while other products such as green tea and red mulberry need processing. Ability to maintain periodontal cell viability for a longer time is warranted in cases of major accidents, where teeth can be replanted only after other major surgeries. Natural products have easy availability, greater efficacy and longer storage time as compared to Hank′s balanced salt solution which has been recommended by the International Association of Dental Traumatology as standard solution for storage of avulsed teeth. Natural products have shown good qualities in in vitro experiments; further in vivo studies are needed to evaluate their efficacy as storage media.

  15. Production of hydrogen by thermocatalytic cracking of natural gas

    Energy Technology Data Exchange (ETDEWEB)

    Muradov, N.Z. [Univ. of Central Florida, Cape Canaveral, FL (United States)

    1995-09-01

    It is universally accepted that in the next few decades hydrogen production will continue to rely on fossil fuels (primarily, natural gas). On the other hand, the conventional methods of hydrogen production from natural gas (for example, steam reforming) are complex multi-step processes. These processes also result in the emission of large quantities of CO{sub 2} into the atmosphere that produce adverse ecological effects. One alternative is the one-step thermocatalytic cracking (TCC) (or decomposition) of natural gas into hydrogen and carbon. Preliminary analysis indicates that the cost of hydrogen produced by thermal decomposition of natural gas is somewhat lower than the conventional processes after by-product carbon credit is taken. In the short term, this process can be used for on-site production of hydrogen-methane mixtures in gas-filling stations and for CO{sub x}-free production of hydrogen for fuel cell driven prime movers. The experimental data on the thermocatalytic cracking of methane over various catalysts and supports in a wide range of temperatures (500-900{degrees}C) are presented in this paper. Two types of reactors were designed and built at FSEC: continuous flow and pulse fix bed catalytic reactors. The temperature dependence of the hydrogen production yield using oxide type catalysts was studied. Alumina-supported Ni- and Fe-catalysts demonstrated relatively high efficiency in the methane cracking reaction at moderate temperatures (600-800{degrees}C). Kinetic curves of hydrogen production over metal and metal oxide catalysts at different temperatures are presented in the paper. Fe-catalyst demonstrated good stability (for several hours), whereas alumina-supported Pt-catalyst rapidly lost its catalytic activity.

  16. The catalytic conversion of natural gas to useful products

    NARCIS (Netherlands)

    Ross, J.R.H.; Ross, J.R.H.; van Keulen, A.N.J.; van Keulen, A.N.J.; Hegarty, M.E.S.; Seshan, Kulathuiyer

    1996-01-01

    This paper gives a brief summary of some processes, direct and indirect, for the conversion of natural gas to useful products. It then proceeds to give an outline of some work from the authors' laboratories on subjects such as steam reforming, oxidative coupling and CO2 reforming of methane, paying

  17. Liquefied natural gas production at Hammerfest: A transforming marine community

    NARCIS (Netherlands)

    Bets, van L.K.J.; Tatenhove, van J.P.M.; Mol, A.P.J.

    2016-01-01

    Global energy demand and scarce petroleum resources require communities to adapt to a rapidly changing Arctic environment, but as well to a transforming socio-economic environment instigated by oil and gas development. This is illustrated by liquefied natural gas production by Statoil at Hammerfest,

  18. The 9th European Conference on Marine Natural Products

    Directory of Open Access Journals (Sweden)

    RuAngelie Edrada-Ebel

    2015-12-01

    Full Text Available The 9th European Conference on Marine Natural Products (ECMNP in Glasgow follows its predecessors in La Toja (2013, Tjärnö (2011, Porto (2009, Ischia (2007, Paris (2005, Elmau (2002, Santiago de Compostela (1999, and Athens (1997. [...

  19. Bioactive Natural Products From Chinese Tropical Marine Organisms

    Institute of Scientific and Technical Information of China (English)

    GUO,Yue-Wei

    2004-01-01

    @@ The oceans contain a vast biological diversity of species that have so far been utilized by mankind mainly as a source of protein. In the last few decades, however, natural products chemists have started to discover the wealth of bioactive secondary metabolites that are produced by marine invertebrates such as sponges, soft corals, molluscs and others.

  20. Expedient total synthesis of pyrrothine natural products and analogs

    DEFF Research Database (Denmark)

    Hjelmgaard, Thomas; Givskov, Michael Christian; Nielsen, John

    2007-01-01

    This paper describes an expedient and straightforward total synthesis of the two pyrrothine natural products holomycin (7 steps, 11% overall) and xenorhabdin I (7 steps, 11% overall) and analogs thereof via a common late-stage intermediate. The pathway proceeds via the pyrrothine hydrochloride...

  1. Current perspectives in drug discovery against tuberculosis from natural products.

    Science.gov (United States)

    Nguta, Joseph Mwanzia; Appiah-Opong, Regina; Nyarko, Alexander K; Yeboah-Manu, Dorothy; Addo, Phyllis G A

    2015-09-01

    Currently, one third of the world's population is latently infected with Mycobacterium tuberculosis (MTB), while 8.9-9.9 million new and relapse cases of tuberculosis (TB) are reported yearly. The renewed research interests in natural products in the hope of discovering new and novel antitubercular leads have been driven partly by the increased incidence of multidrug-resistant strains of MTB and the adverse effects associated with the first- and second-line antitubercular drugs. Natural products have been, and will continue to be a rich source of new drugs against many diseases. The depth and breadth of therapeutic agents that have their origins in the secondary metabolites produced by living organisms cannot be compared with any other source of therapeutic agents. Discovery of new chemical molecules against active and latent TB from natural products requires an interdisciplinary approach, which is a major challenge facing scientists in this field. In order to overcome this challenge, cutting edge techniques in mycobacteriology and innovative natural product chemistry tools need to be developed and used in tandem. The present review provides a cross-linkage to the most recent literature in both fields and their potential to impact the early phase of drug discovery against TB if seamlessly combined.

  2. Low Carbon Technology Options for the Natural Gas Electricity Production

    Science.gov (United States)

    The ultimate goal of this task is to perform environmental and economic analysis of natural gas based power production technologies (different routes) to investigate and evaluate strategies for reducing emissions from the power sector. It is a broad research area. Initially, the...

  3. Solvent-free extraction of food and natural products

    OpenAIRE

    Fabiano-Tixier, Anne-Sylvie; Vian, Maryline; Allaf, Tamara; Vorobiev, Eugene

    2015-01-01

    This review presents useful and green techniques of solvent-free extraction used in ancient times, such as extraction of olive oil and citrus essential oil, and innovative techniques, such as pulsed electric field, microwave, instantaneous controlled pressure drop, and extrusion. We discuss the devices, their applications, mechanisms, and parameters influencing sample preparation prior to analysis of natural products.

  4. Low Carbon Technology Options for the Natural Gas Electricity Production

    Science.gov (United States)

    The ultimate goal of this task is to perform environmental and economic analysis of natural gas based power production technologies (different routes) to investigate and evaluate strategies for reducing emissions from the power sector. It is a broad research area. Initially, the...

  5. A New Golden Age of Natural Products Drug Discovery

    Science.gov (United States)

    Shen, Ben

    2016-01-01

    The 2015 Nobel Prize in Physiology or Medicine has been awarded to William C. Campbell and Satoshi Omura, and Youyou Tu for the discovery of avermectins and artemisinin, respectively, therapies that revolutionized the treatment of devastating parasite diseases. With the recent technological advances, a New Golden Age of natural products drug discovery is dawning. PMID:26638061

  6. Natural products chemistry research 2010's progress in China.

    Science.gov (United States)

    Ye, Yang; Li, Xi-Qiang; Tang, Chun-Ping; Yao, Sheng

    2012-01-01

    This article reviews the progresses made by Chinese scientists in the field of natural products chemistry in 2010. Selected compounds with unique structural features and/or promising bioactivities were described herein on the basis of structural types. Copyright © 2012 China Pharmaceutical University. Published by Elsevier B.V. All rights reserved.

  7. Stereoselective Total Synthesis of Bioactive Marine Natural Product Biselyngbyolide B.

    Science.gov (United States)

    Das, Sayantan; Paul, Debobrata; Goswami, Rajib Kumar

    2016-04-15

    A convergent strategy for the stereoselective total synthesis of biologically active marine natural product biselyngbyolide B has been developed. Key strategies of this synthesis include Jamison protocol of trans-hydroalumination/allylation for installation of C18-C23 olefin moiety and intramolecular Heck coupling for macrocyclization.

  8. Natural Products as Source of Therapeutics against Parasitic Diseases.

    Science.gov (United States)

    Hertweck, Christian

    2015-12-01

    An end to suffering: Parasitic infections with protozoa and worms cause unimaginable misery, in particular in the tropics. Fortunately, natural products, such as the antimalarial artemisinin (1) and the anthelmintic avermectin (2) were discovered and developed into therapeutics. These major achievements now culminated in the 2015 Nobel Prize for Medicine.

  9. Short history of natural product research in the CSIR

    CSIR Research Space (South Africa)

    Walwyn, D

    2006-02-01

    Full Text Available Natural product research has been a major component of the CSIR's bioscience activities for its entire history, and particularly in the 1960s and 1970s. This type of work is also strongly aligned with one of the objectives of the CSIR, namely...

  10. Natural product derived insecticides: discovery and development of spinetoram.

    Science.gov (United States)

    Galm, Ute; Sparks, Thomas C

    2016-03-01

    This review highlights the importance of natural product research and industrial microbiology for product development in the agricultural industry, based on examples from Dow AgroSciences. It provides an overview of the discovery and development of spinetoram, a semisynthetic insecticide derived by a combination of a genetic block in a specific O-methylation of the rhamnose moiety of spinosad coupled with neural network-based QSAR and synthetic chemistry. It also emphasizes the key role that new technologies and multidisciplinary approaches play in the development of current spinetoram production strains.

  11. Marine Natural Products as Lead Compound for New Drug Discovery

    Institute of Scientific and Technical Information of China (English)

    JIANG; Biao

    2001-01-01

    The study of natural product has long been motivated by a quest for some benefit to man, the discover. Recent years have witnessed growing attention to the isolation, identification and synthesis of the marine natural. Although marine organisms do not have a long history of medicine applications like terrestrial plants, some marine organisms have left an extensive record of hazard to mankind. The isolation and identification of saxtoxin, tetradotoxin and lyngbyatoxin resulted from such reported. The marine biosphere has long held great promise as source of anticancer compounds, while a number of screening efforts has indicated a much higher percentage of antineplastic and antitumor activity than terrestrial plants. Several marine natural products have made their appearance in clinical trials at the National Cancer Institute, such as the didemnis, , bryostatins, This finds marine invertebratehave reinvigorated interest and effort in anticancer agent from marine invertebrate.  ……

  12. Marine Natural Products as Lead Compound for New Drug Discovery

    Institute of Scientific and Technical Information of China (English)

    JIANG Biao

    2001-01-01

    @@ The study of natural product has long been motivated by a quest for some benefit to man, the discover. Recent years have witnessed growing attention to the isolation, identification and synthesis of the marine natural. Although marine organisms do not have a long history of medicine applications like terrestrial plants, some marine organisms have left an extensive record of hazard to mankind. The isolation and identification of saxtoxin, tetradotoxin and lyngbyatoxin resulted from such reported. The marine biosphere has long held great promise as source of anticancer compounds, while a number of screening efforts has indicated a much higher percentage of antineplastic and antitumor activity than terrestrial plants. Several marine natural products have made their appearance in clinical trials at the National Cancer Institute, such as the didemnis, , bryostatins, This finds marine invertebratehave reinvigorated interest and effort in anticancer agent from marine invertebrate.

  13. HEURISTIC OPTIMIZATION OF NATURAL PRODUCTION INVENTORY MODELS WITH THE PREFERENCE OF A DECISION MAKER

    OpenAIRE

    CHIH HSUN HSIEH

    2008-01-01

    In this paper, two natural production inventory models based on fuzzy total production inventory cost with the preference of a decision maker are introduced, and combined by natural number parameters in which values are linguistic values in natural language, crisp real number variables, and fuzzy number variables. These are the one natural production inventory model for crisp production quantity, and the other natural production inventory model for fuzzy production quantity. The natural arith...

  14. Systematics-guided bioprospecting for bioactive microbial natural products.

    Science.gov (United States)

    Liu, Xueting; Bolla, Krishna; Ashforth, Elizabeth Jane; Zhuo, Ying; Gao, Hong; Huang, Pei; Stanley, Sarah A; Hung, Deborah T; Zhang, Lixin

    2012-01-01

    Advances in the taxonomic characterization of microorganisms have accelerated the rate at which new producers of natural products can be understood in relation to known organisms. Yet for many reasons, chemical efforts to characterize new compounds from new microbes have not kept pace with taxonomic advances. That there exists an ever-widening gap between the biological versus chemical characterization of new microorganisms creates tremendous opportunity for the discovery of novel natural products through the calculated selection and study of organisms from unique, untapped, ecological niches. A systematics-guided bioprospecting, including the construction of high quality libraries of marine microbes and their crude extracts, investigation of bioactive compounds, and increasing the active compounds by precision engineering, has become an efficient approach to drive drug leads discovery. This review outlines the recent advances in these issues and shares our experiences on anti-infectious drug discovery and improvement of avermectins production as well.

  15. Synthetic biology tools for bioprospecting of natural products in eukaryotes.

    Science.gov (United States)

    Unkles, Shiela E; Valiante, Vito; Mattern, Derek J; Brakhage, Axel A

    2014-04-24

    Filamentous fungi have the capacity to produce a battery of natural products of often unknown function, synthesized by complex metabolic pathways. Unfortunately, most of these pathways appear silent, many in intractable organisms, and their products consequently unidentified. One basic challenge is the difficulty of expressing a biosynthesis pathway for a complex natural product in a heterologous eukaryotic host. Here, we provide a proof-of concept solution to this challenge and describe how the entire penicillin biosynthesis pathway can be expressed in a heterologous host. The method takes advantage of a combination of improved yeast in vivo cloning technology, generation of polycistronic mRNA for the gene cluster under study, and an amenable and easily manipulated fungal host, i.e., Aspergillus nidulans. We achieve expression from a single promoter of the pathway genes to yield a large polycistronic mRNA by using viral 2A peptide sequences to direct successful cotranslational cleavage of pathway enzymes.

  16. Natural products - plenty more where that came from

    Energy Technology Data Exchange (ETDEWEB)

    Arnold, M.

    1980-12-22

    In this article, natural products and their possible use as renewable resources are reviewed. The fermentation of corn for the production of alcohol for motor fuel is discussed and other crops for this purpose include sugar cane, cassava, sweet potato and Jerusalem artichoke. The hydrolysis of cellulose to sugars based on enzyme hydrolysis is currently being researched in the USA. Also in the USA, Melvin Calvin hopes to breed a rubber-bearing plant whose latex can be easily cracked to motor fuel. Guayule and jojoba rubber-bearing plants are also the focus of research at present. The importance of natural vegetation in the manufacturing of medicines and in the chemical and food industries is stressed. Finally products of the sea, particularly alginates and carragheenins are mentioned, but as yet, the full potential of the sea to yield renewable resources is unknown.

  17. Virtual Natural Product Library - full text searchable database

    Directory of Open Access Journals (Sweden)

    Subhash Chandra Bose. Kotte

    2012-05-01

    Full Text Available Small molecules occurring in nature have special significance to mankind. They have varied applications from healthcare, food, nutrition, agriculture, personal care and well-being. These natural small molecules are from very diverse sources from the rarest plants to deep sea creatures. Recently they have assumed a lot of significance as pharmaceutical companies is constantly pushing the horizons to make them druggable due to their inherent bioactivities. Though they are not easy to synthesize or isolate, yet their diverse molecular scaffold confers them significance especially given the fact of prevailing resistance to drug scaffolds presently being used in the clinics. Hence its of paramount importance to have a database of diverse natural small molecules through the present effort of creating a Virtual Natural Products Library (VNPL-version 0.15.

  18. Infrared Spectroscopy Study of Structural Nature of Geopolymeric Products

    Institute of Scientific and Technical Information of China (English)

    ZHANG Yunsheng; SUN Wei; LI Zongjin

    2008-01-01

    The bonding status and chemical environment of SiO4 and AlO4 tetrahedras of three types of geopolymeric products were systematically investigated by infrared spectroscopy.The relationship between amorphous geopolymeric products and zeolite crystals with the same overall chemical compositions was also discussed.The infrared evidence shows that SiO4 tetrahedra is partially bonded by AlO4 during the hydration process ofgeopolymeric cement.The two types of tetrahedras jointly construct the three dimensional framework structures of the geopolymeric products.The mutual transformation between geopolymeric products and corresponding zeolite crystals will take place once the reaction condition is suitable,which reveals that the nature ofgeopolymeric products are probably the amorphous equivalent of the corresponding zeolite crystals.

  19. Interdisciplinary researches for potential developments of drugs and natural products

    Directory of Open Access Journals (Sweden)

    Arunrat Chaveerach

    2017-04-01

    Full Text Available Developments of drugs or natural products from plants are possibly made, simple to use and lower cost than modern drugs. The development processes can be started with studying local wisdom and literature reviews to choose the plants which have long been used in diverse areas, such as foods, traditional medicine, fragrances and seasonings. Then those data will be associated with scientific researches, namely plant collection and identification, phytochemical screening by gas chromatography-mass spectrometry, pharmacological study/review for their functions, and finally safety and efficiency tests in human. For safety testing, in vitro cell toxicity by cell viability assessment and in vitro testing of DNA breaks by the comet assay in human peripheral blood mononuclear cells can be performed. When active chemicals and functions containing plants were chosen with safety and efficacy for human uses, then, the potential medicinal natural products will be produced. Based on these procedures, the producing cost will be cheaper and the products can be evaluated for their clinical properties. Thus, the best and lowest-priced medicines and natural products can be distributed worldwide.

  20. Redirecting photosynthetic reducing power toward bioactive natural product synthesis.

    Science.gov (United States)

    Nielsen, Agnieszka Zygadlo; Ziersen, Bibi; Jensen, Kenneth; Lassen, Lærke Münter; Olsen, Carl Erik; Møller, Birger Lindberg; Jensen, Poul Erik

    2013-06-21

    In addition to the products of photosynthesis, the chloroplast provides the energy and carbon building blocks required for synthesis of a wealth of bioactive natural products of which many have potential uses as pharmaceuticals. In the course of plant evolution, energy generation and biosynthetic capacities have been compartmentalized. Chloroplast photosynthesis provides ATP and NADPH as well as carbon sources for primary metabolism. Cytochrome P450 monooxygenases (P450s) in the endoplasmic reticulum (ER) synthesize a wide spectrum of bioactive natural products, powered by single electron transfers from NADPH. P450s are present in low amounts, and the reactions proceed relatively slowly due to limiting concentrations of NADPH. Here we demonstrate that it is possible to break the evolutionary compartmentalization of energy generation and P450-catalyzed biosynthesis, by relocating an entire P450-dependent pathway to the chloroplast and driving the pathway by direct use of the reducing power generated by photosystem I in a light-dependent manner. The study demonstrates the potential of transferring pathways for structurally complex high-value natural products to the chloroplast and directly tapping into the reducing power generated by photosynthesis to drive the P450s using water as the primary electron donor.

  1. Conceptual process synthesis for recovery of natural products from plants

    DEFF Research Database (Denmark)

    Malwade, Chandrakant R.; Qu, Haiyan; Rong, Ben-Guang;

    2013-01-01

    A systematic method of conceptual process synthesis for recovery of natural products from their biological sources is presented. This methodology divides the task into two major subtasks namely, isolation of target compound from a chemically complex solid matrix of biological source (crude extract......) and purification of target compound(s) from the crude extract. Process analytical technology (PAT) is used in each step to understand the nature of material systems and separation characteristics of each separation method. In the present work, this methodology is applied to generate process flow sheet for recovery...

  2. Exploiting the potential of marine natural products: structure elucidation and metagenomic approaches to biotechnological production

    OpenAIRE

    Della Sala, Gerardo

    2013-01-01

    Sponges represent the most prolific producers of novel marine bioactive secondary metabolites. In the last years, several drugs derived from marine natural products have appeared in the market, and others are in clinical trials. The aim of my research project was to exploit the unusual and often surprising chemistry of marine sponges, in the frame of the more general purpose of discovering and developing new drugs from natural products. The research work presented in this PhD Thesis was di...

  3. Phenazines and natural products; Novel synthesis of saphenic acid

    DEFF Research Database (Denmark)

    Petersen, Lars; Jensen, Knud Jørgen; Nielsen, John

    1999-01-01

    The natural product saphenic acid (6-(1-hydroxyethyl)1-phenazinecarboxylic acid) was synthesized from readily accessible starting materials. The desired product was obtained in an overall yield of 22% for four steps with the key steps being formation of a diphenylamine, followed by cyclization un...... under alkaline and reducing conditions. Assignments of H-1 NMR spectra were achieved by homo- and heteronuclear 1D and 2D correlations. Double pulsed field gradient spin-echo one-dimensional NOESY proved especially valuable for assignment of aromatic protons....

  4. Phenazines and natural products; novel synthesis of saphenic acid

    DEFF Research Database (Denmark)

    Petersen, Lars; Jensen, Knud J.; Nielsen, John

    1999-01-01

    The natural product saphenic acid (6-(1-hydroxyethyl)1- phenazinecarboxylic acid) was synthesized from readily accessible starting materials. The desired product was obtained in an overall yield of 22% for four steps with the key steps being formation of a diphenylamine, followed by cyclization u...... under alkaline and reducing conditions. Assignments of 1H NMR spectra were achieved by homo- and heteronuclear 1D and 2D correlations. Double pulsed field gradient spin-echo one-dimensional NOESY proved especially valuable for assignment of aromatic protons....

  5. Dietary Natural Products for Prevention and Treatment of Breast Cancer.

    Science.gov (United States)

    Li, Ya; Li, Sha; Meng, Xiao; Gan, Ren-You; Zhang, Jiao-Jiao; Li, Hua-Bin

    2017-07-08

    Breast cancer is the most common cancer among females worldwide. Several epidemiological studies suggested the inverse correlation between the intake of vegetables and fruits and the incidence of breast cancer. Substantial experimental studies indicated that many dietary natural products could affect the development and progression of breast cancer, such as soy, pomegranate, mangosteen, citrus fruits, apple, grape, mango, cruciferous vegetables, ginger, garlic, black cumin, edible macro-fungi, and cereals. Their anti-breast cancer effects involve various mechanisms of action, such as downregulating ER-α expression and activity, inhibiting proliferation, migration, metastasis and angiogenesis of breast tumor cells, inducing apoptosis and cell cycle arrest, and sensitizing breast tumor cells to radiotherapy and chemotherapy. This review summarizes the potential role of dietary natural products and their major bioactive components in prevention and treatment of breast cancer, and special attention was paid to the mechanisms of action.

  6. Optimizing patient care with "natural" products: treatment of hyperpigmentation.

    Science.gov (United States)

    Woolery-Lloyd, Heather; Friedman, Adam

    2009-06-01

    Patients with skin of color suffer from different cutaneous issues when compared with skin of light complexion, and therefore management of the former must be representative of these variations. The most common pigmentary complaints in patients with skin of color are post-inflammatory hyperpigmentation, melasma and sun-induced hyperpigmentation. Often, patients with darker skin will turn to naturally occurring ingredients over synthetic analogues both to satisfy cultural preferences and to limit potential adverse effects that have been tied to synthetics. Science-based natural products can offer an attractive adjunct to conventional therapies that treat melasma, post-inflammatory hyperpigmentaion, and other dyschromias. Increasing data on the biological effects and the efficacy of natural therapies support the use of these complementary therapies in treating hyperpigmentation.

  7. The C7N aminocyclitol family of natural products.

    Science.gov (United States)

    Mahmud, Taifo

    2003-02-01

    This review covers microbial secondary metabolites classified in the family of C7N aminocyclitols, a relatively new class of natural products that is increasingly gaining recognition due to their significant biomedical and agricultural uses. Their discovery and structure determinations, their biosynthetic origin, biological properties, chemical synthesis, as well as their further development for pharmaceutical uses are described. The literature from 1970 to July 2002 is reviewed, with 269 references cited.

  8. Journal of Asian Natural Products Research简介

    Institute of Scientific and Technical Information of China (English)

    李霄茜

    2009-01-01

    @@ Journal of Asian Natural Products Research(,简称JANPR;ISSN:1028-6020;e-ISSN:1477-2213)是由英国Taylor & Francis公司出版发行的一本以亚洲传统医学中天然产品的化学和药理学研究为主要方向的国际性杂志.

  9. Five decades in the study of natural products*

    Indian Academy of Sciences (India)

    T R Govindachari

    2002-06-01

    This paper describes the five-decade long fascinating journey taken by Prof. T R Govindachari towards the study of the natural products of India. A variety of Indian plants were investigated by him for the study of their constituent alkaloids and terpenoids. The concluding part of the paper summarizes the isolation and identification of the constituents of the Neem kernel, which eventually led to the first X-ray structure determination of azadirachtin A.

  10. Cytotoxic Natural Products from Marine Sponge-Derived Microorganisms

    Directory of Open Access Journals (Sweden)

    Huawei Zhang

    2017-03-01

    Full Text Available A growing body of evidence indicates that marine sponge-derived microbes possess the potential ability to make prolific natural products with therapeutic effects. This review for the first time provides a comprehensive overview of new cytotoxic agents from these marine microbes over the last 62 years from 1955 to 2016, which are assorted into seven types: terpenes, alkaloids, peptides, aromatics, lactones, steroids, and miscellaneous compounds.

  11. An Update on Natural Products with Carbonic Anhydrase Inhibitory Activity.

    Science.gov (United States)

    Karioti, Anastasia; Carta, Fabrizio; Supuran, Claudiu T

    2016-01-01

    Carbonic anhydrases (CAs, EC 4.2.1.1) catalyze the fundamental reaction of CO2 hydration in all living organisms, being actively involved in the regulation of a plethora of patho/physiological processes. They represent a typical example of enzyme convergent evolution, as six genetically unrelated families of such enzymes were described so far. It is more than 70 years that synthetic compounds, mainly sulfonamides, have been used in clinical practice as diuretics and systemic acting antiglaucoma drugs. Recent studies using natural product libraries and isolated constituents from natural sources (such as fungi and plants) have disclosed novel chemotypes possessing carbonic anhydrase inhibition activities. These natural sources offer new opportunities in the search for new and more effective carbonic anhydrase inhibitors, and may serve as new leads for the design and development of future drugs. This review will discuss the most recent advances in the search of naturally occurring products and their synthetic derivatives that inhibit the CAs and their mechanisms of action at molecular level. Plant extracts are not considered in the present review.

  12. Rationale for a natural products approach to herbicide discovery.

    Science.gov (United States)

    Dayan, Franck E; Owens, Daniel K; Duke, Stephen O

    2012-04-01

    Weeds continue to evolve resistance to all the known modes of herbicidal action, but no herbicide with a new target site has been commercialized in nearly 20 years. The so-called 'new chemistries' are simply molecules belonging to new chemical classes that have the same mechanisms of action as older herbicides (e.g. the protoporphyrinogen-oxidase-inhibiting pyrimidinedione saflufenacil or the very-long-chain fatty acid elongase targeting sulfonylisoxazoline herbicide pyroxasulfone). Therefore, the number of tools to manage weeds, and in particular those that can control herbicide-resistant weeds, is diminishing rapidly. There is an imminent need for truly innovative classes of herbicides that explore chemical spaces and interact with target sites not previously exploited by older active ingredients. This review proposes a rationale for a natural-products-centered approach to herbicide discovery that capitalizes on the structural diversity and ingenuity afforded by these biologically active compounds. The natural process of extended-throughput screening (high number of compounds tested on many potential target sites over long periods of times) that has shaped the evolution of natural products tends to generate molecules tailored to interact with specific target sites. As this review shows, there is generally little overlap between the mode of action of natural and synthetic phytotoxins, and more emphasis should be placed on applying methods that have proved beneficial to the pharmaceutical industry to solve problems in the agrochemical industry.

  13. Natural Products as Source of Potential Dengue Antivirals

    Directory of Open Access Journals (Sweden)

    Róbson Ricardo Teixeira

    2014-06-01

    Full Text Available Dengue is a neglected disease responsible for 22,000 deaths each year in areas where it is endemic. To date, there is no clinically approved dengue vaccine or antiviral for human beings, even though there have been great efforts to accomplish these goals. Several approaches have been used in the search for dengue antivirals such as screening of compounds against dengue virus enzymes and structure-based computational discovery. During the last decades, researchers have turned their attention to nature, trying to identify compounds that can be used as dengue antivirals. Nature represents a vast reservoir of substances that can be explored with the aim of discovering new leads that can be either used directly as pharmaceuticals or can serve as lead structures that can be optimized towards the development of new antiviral agents against dengue. In this review we describe an assortment of natural products that have been reported as possessing dengue antiviral activity. The natural products are organized into classes of substances. When appropriate, structure-activity relationships are outlined. The biological assays used to assess antiviral activity are briefly described.

  14. Novel fermentation processes for manufacturing plant natural products.

    Science.gov (United States)

    Zhou, Jingwen; Du, Guocheng; Chen, Jian

    2014-02-01

    Microbial production of plant natural products (PNPs), such as terpenoids, flavonoids from renewable carbohydrate feedstocks offers sustainable and economically attractive alternatives to their petroleum-based production. Rapid development of metabolic engineering and synthetic biology of microorganisms shows many advantages to replace the current extraction of these useful high price chemicals from plants. Although few of them were actually applied on a large scale for PNPs production, continuous research on these high-price chemicals and the rapid growing global market of them, show the promising future for the production of these PNPs by microorganisms with a more economic and environmental friendly way. Introduction of novel pathways and optimization of the native cellular processes by metabolic engineering of microorganisms for PNPs production are rapidly expanding its range of cell-factory applications. Here we review recent progress in metabolic engineering of microorganisms for the production of PNPs. Besides, factors restricting the yield improvement and application of lab-scale achievements to industrial applications have also been discussed.

  15. Methylaplysinopsin and other marine natural products affecting neurotransmission.

    Science.gov (United States)

    Taylor, K M; Baird-Lambert, J A; Davis, P A; Spence, I

    1981-01-01

    Methylaplysinopsin is a novel marine natural product that, after oral administration, prevented the effects of tetrabenazine in mice and rats. Methylaplysinopsin was a short-acting inhibitor of monoamine oxidase activity with greatest potency when serotonin was the substrate studied. The brain concentration of serotonin in the mouse was increased by methylaplysinopsin over the same time course as monoamine oxidase inhibition ex vivo. Methylaplysinopsin was also a weak inhibitor of the neuronal uptake of [3H]serotonin and a potentiator of the K+-induced release of [3H]serotonin from prelabeled synaptosomes. The predicted potentiation of serotonergic neurotransmission was supported by initial neurophysiological studies in an identified serotonergic pathway in the central nervous system of Aplysia. Two other studies on the pharmacology of marine natural products are reviewed. The majority of polyhalogenated monoterpenes isolated from red algae had central nervous system depressant properties. The exception is plocamadiene A, which caused, in mice, a reversible spastic paresis lasting up to 72 hours after oral administration. The severe muscle spasm was antagonized by diazepam. The final study discussed is the effect of a variety of marine natural products on the synthesis, neuronal uptake, and metabolism of GABA. Their selectivity is discussed with regard to the effects on metabolic respiration, and the correlation of neurochemical and neurophysiological effects on these marine substances.

  16. An overview on the potential of natural products as ureas

    Directory of Open Access Journals (Sweden)

    Luzia V. Modolo

    2015-01-01

    Full Text Available Ureases, enzymes that catalyze urea hydrolysis, have received considerable attention for their impact on living organisms’ health and life quality. On the one hand, the persistence of urease activity in human and animal cells can be the cause of some diseases and pathogen infections. On the other hand, food production can be negatively affected by ureases of soil microbiota that, in turn, lead to losses of nitrogenous nutrients in fields supplemented with urea as fertilizer. In this context, nature has proven to be a rich resource of natural products bearing a variety of scaffolds that decrease the ureolytic activity of ureases from different organisms. Therefore, this work compiles the state-of-the-art researches focused on the potential of plant natural products (present in extracts or as pure compounds as urease inhibitors of clinical and/or agricultural interests. Emphasis is given to ureases of Helicobacter pylori, Canavalia ensiformis and soil microbiota although the active site of this class of hydrolases is conserved among living organisms.

  17. Automated genome mining of ribosomal peptide natural products

    Energy Technology Data Exchange (ETDEWEB)

    Mohimani, Hosein; Kersten, Roland; Liu, Wei; Wang, Mingxun; Purvine, Samuel O.; Wu, Si; Brewer, Heather M.; Pasa-Tolic, Ljiljana; Bandeira, Nuno; Moore, Bradley S.; Pevzner, Pavel A.; Dorrestein, Pieter C.

    2014-07-31

    Ribosomally synthesized and posttranslationally modified peptides (RiPPs), especially from microbial sources, are a large group of bioactive natural products that are a promising source of new (bio)chemistry and bioactivity (1). In light of exponentially increasing microbial genome databases and improved mass spectrometry (MS)-based metabolomic platforms, there is a need for computational tools that connect natural product genotypes predicted from microbial genome sequences with their corresponding chemotypes from metabolomic datasets. Here, we introduce RiPPquest, a tandem mass spectrometry database search tool for identification of microbial RiPPs and apply it for lanthipeptide discovery. RiPPquest uses genomics to limit search space to the vicinity of RiPP biosynthetic genes and proteomics to analyze extensive peptide modifications and compute p-values of peptide-spectrum matches (PSMs). We highlight RiPPquest by connection of multiple RiPPs from extracts of Streptomyces to their gene clusters and by the discovery of a new class III lanthipeptide, informatipeptin, from Streptomyces viridochromogenes DSM 40736 as the first natural product to be identified in an automated fashion by genome mining. The presented tool is available at cy-clo.ucsd.edu.

  18. Antimycobacterial natural products--an opportunity for the Colombian biodiversity.

    Science.gov (United States)

    Bueno, Juan; Coy, Ericsson David; Stashenko, Elena

    2011-12-01

    It is estimated that one-third part of the world population is infected with the tubercle bacillus. While only a small percentage of infected individuals will develop clinical tuberculosis, each year there are approximately eight million new cases and two million deaths. Mycobacterium tuberculosis is thus responsible for more human mortality than any other single microbial species. The goals of tuberculosis control are focused to cure active disease, prevent relapse, reduce transmission and avert the emergence of drug-resistance. For over 50 years, natural products have served us well on combating infectious bacteria and fungi. During the 20th century, microbial and plant secondary metabolites have helped to double our life span, reduced pain and suffering, and revolutionized medicine. Colombia is a megadiverse country with enormous potential to offer leads for new antimycobacterial drugs. The principal aim of this article is to show a state of the art on antimycobacterial natural products research in Colombia compared to the rest of the world, in order to develop programs for bioprospecting with a view to determining the biological activity for pharmaceutical and industrial application of natural products in our country.

  19. Natural products research in South Africa: 1890–2010

    Directory of Open Access Journals (Sweden)

    Siegfried E. Drewes

    2012-05-01

    Full Text Available Having spent some 50 years as an organic chemist with an interest in medicinal plant chemistry in South Africa it was relevant now to ask three questions, (1 when were natural products first utilised, (2 who were the people involved, and (3 what is the status quo? Based on older literature published in the South African Journal of Chemistry, information gleaned from attendance at innumerable chemistry conferences, and relevant literature in university archives, a great deal of information was gathered to answer the first two questions. For example, that the first veterinarian to treat cattle diseases caused by poisonous plants in the Eastern Cape was Dr Jotella Soga in the 1890s. Contributions from other prominent scientists such as Marais, Rindl, Rimington and Warren followed. From about 1940 to the 1990s, researchers concentrated mainly on the isolation of new compounds from local plants for which some indigenous knowledge was recorded. Foreign chemists also arrived and did a fair amount of ‘exploitation’ of natural products. Thus, the anti-cancer compound combretastatin was first isolated from the indigenous tree Combretum caffrum. Plant chemistry in South Africa has blossomed in the last decade, with many students from previously disadvantaged backgrounds, but with a keen interest in muti or medicinal chemistry, entering the field. Recent findings have rekindled the belief that a major development in natural products would at last emerge from Africa.

  20. Natural gas production problems : solutions, methodologies, and modeling.

    Energy Technology Data Exchange (ETDEWEB)

    Rautman, Christopher Arthur; Herrin, James M.; Cooper, Scott Patrick; Basinski, Paul M. (El Paso Production Company, Houston, TX); Olsson, William Arthur; Arnold, Bill Walter; Broadhead, Ronald F. (New Mexico Bureau of Geology and Mineral Resources, Socorro, NM); Knight, Connie D. (Consulting Geologist, Golden, CO); Keefe, Russell G.; McKinney, Curt (Devon Energy Corporation, Oklahoma City, OK); Holm, Gus (Vermejo Park Ranch, Raton, NM); Holland, John F.; Larson, Rich (Vermejo Park Ranch, Raton, NM); Engler, Thomas W. (New Mexico Institute of Mining and Technology, Socorro, NM); Lorenz, John Clay

    2004-10-01

    Natural gas is a clean fuel that will be the most important domestic energy resource for the first half the 21st centtuy. Ensuring a stable supply is essential for our national energy security. The research we have undertaken will maximize the extractable volume of gas while minimizing the environmental impact of surface disturbances associated with drilling and production. This report describes a methodology for comprehensive evaluation and modeling of the total gas system within a basin focusing on problematic horizontal fluid flow variability. This has been accomplished through extensive use of geophysical, core (rock sample) and outcrop data to interpret and predict directional flow and production trends. Side benefits include reduced environmental impact of drilling due to reduced number of required wells for resource extraction. These results have been accomplished through a cooperative and integrated systems approach involving industry, government, academia and a multi-organizational team within Sandia National Laboratories. Industry has provided essential in-kind support to this project in the forms of extensive core data, production data, maps, seismic data, production analyses, engineering studies, plus equipment and staff for obtaining geophysical data. This approach provides innovative ideas and technologies to bring new resources to market and to reduce the overall environmental impact of drilling. More importantly, the products of this research are not be location specific but can be extended to other areas of gas production throughout the Rocky Mountain area. Thus this project is designed to solve problems associated with natural gas production at developing sites, or at old sites under redevelopment.

  1. 76 FR 19996 - Cooperative Agreement With the University of Mississippi's National Center for Natural Products...

    Science.gov (United States)

    2011-04-11

    ... National Center for Natural Products Research (U01) To Develop and Disseminate Botanical Natural Product... and dissemination of natural products research and science and the programs developed under the... develop and disseminate botanical natural product research with an emphasis on public safety according...

  2. DNA barcoding in native plants of the Labiatae (Lamiaceae) family from Chios Island (Greece) and the adjacent Çeşme-Karaburun Peninsula (Turkey).

    Science.gov (United States)

    Theodoridis, Spyros; Stefanaki, Anastasia; Tezcan, Meltem; Aki, Cuneyt; Kokkini, Stella; Vlachonasios, Konstantinos E

    2012-07-01

    The plant family Labiatae (Lamiaceae) is known for its fine medicinal and aromatic herbs like lavender, mint, oregano, sage and thyme and is a rich source of essential oils for the food, pharmaceutical and cosmetic industry. Besides its great economic importance, the Labiatae family contributes significantly to the endemic flora of Greece and Turkey. Owing to its economic and biological significance and to the difficult identification based on morphological characters of several of its taxa, the Labiatae family is an ideal case for developing DNA barcodes. The purpose of this study is to evaluate the utility of DNA barcoding on a local scale in discriminating Labiatae species in Chios Island (Greece) and the adjacent Çeşme-Karaburun Peninsula (Turkey). We chose three cpDNA regions (matK, rbcL, trnH-psbA) that were proposed by previous studies and tested them either as single region or as multiregion barcodes based on the criteria determined by Consortium for the Barcode of Life (CBOL). Our results show that matK and trnH-psbA taken as useful in discriminating species of the Labiatae, for the species we examined, as any multiregion combination. matK and trnH-psbA could serve as single-region barcodes for Labiatae species contributing to the conservation and the trade control of valuable plant resources.

  3. Marine natural products in prevention and treatment of osteoporosis

    Directory of Open Access Journals (Sweden)

    Zahra Ghanbari

    2015-05-01

    Full Text Available Undoubtedly, pharmaceutical and nutritional factors play an important role in the prevention of age-related bone loss. According to the several studies so far, the effects of nutrients and bioactive components which are extracted from marine resources are very promising in osteoporosis. Most of these investigations have been done on various marine algae extracts. Since, algae are rich source of essential minerals, primary and secondary unique natural products, several amino acids and growth factors their extracts show favorable effects on bone metabolism. Moreover, it has been shown that marine nutrients such as marine fishes, shrimp and crabs increase the absorption of calcium and bone collagen synthesis or reduce the production of prostaglandins and decrease the deoxypyridinoline disposal. On the other hand, secondary products which are extracted and characterized from marine organisms such as mollusks, fungi, bacteria, sponges and coral reefs show anti-osteoporosis activities via the inhibition of osteoclast differentiation and the induction of apoptosis in osteoclasts like cells or stimulation of osteoblast differentiation. Although, several investigations have been done in this area, many of studies have been carried out on animal models, like ovariectomy-induced bone loss in mice. Hence, clinical investigations are warranted to develop marine natural products against bone loss and to prevent osteoporosis.

  4. Enhancement of dimethylsulfide production by anoxic stress in natural seawater

    Science.gov (United States)

    Omori, Yuko; Tanimoto, Hiroshi; Inomata, Satoshi; Wada, Shigeki; Thume, Kathleen; Pohnert, Georg

    2015-05-01

    Dimethylsulfide (DMS) is produced by phytoplankton in the ocean and plays an important role in biogeochemical cycles and climate system of the Earth. Previous field studies reported a possible relationship between DMS enhancement and anoxic condition, although the governing processes are still to be identified. Here we show the first direct evidence for the enhancement of DMS production by natural planktonic assemblages caused by anoxic stress. Under the anoxic condition, DMS production was considerably enhanced and DMS bacterial consumption was inhibited, resulting in an eightfold higher rate of gross DMS production than that under the oxic condition. Our results demonstrated that anoxic stress is one of important "environmental factors" in the marine DMS dynamics, suggesting the possible global importance due to ubiquity of anoxic conditions in the coastal oceans. This process would become more important in the future due to expansion of coastal hypoxic and anoxic zones by global warming.

  5. Mimicking a natural pathway for de novo biosynthesis: natural vanillin production from accessible carbon sources.

    Science.gov (United States)

    Ni, Jun; Tao, Fei; Du, Huaiqing; Xu, Ping

    2015-09-02

    Plant secondary metabolites have been attracting people's attention for centuries, due to their potentials; however, their production is still difficult and costly. The rich diversity of microbes and microbial genome sequence data provide unprecedented gene resources that enable to develop efficient artificial pathways in microorganisms. Here, by mimicking a natural pathway of plants using microbial genes, a new metabolic route was developed in E. coli for the synthesis of vanillin, the most widely used flavoring agent. A series of factors were systematically investigated for raising production, including efficiency and suitability of genes, gene dosage, and culture media. The metabolically engineered strain produced 97.2 mg/L vanillin from l-tyrosine, 19.3 mg/L from glucose, 13.3 mg/L from xylose and 24.7 mg/L from glycerol. These results show that the metabolic route enables production of natural vanillin from low-cost substrates, suggesting that it is a good strategy to mimick natural pathways for artificial pathway design.

  6. Production of hydrogen by thermocatalytic cracking of natural gas

    Energy Technology Data Exchange (ETDEWEB)

    Muradov, N. [Florida Solar Energy Center, Cocoa, FL (United States)

    1996-10-01

    The conventional methods of hydrogen production from natural gas (for example, steam reforming and partial oxidation) are complex, multi-step processes that produce large quantities of CO{sub 2}. The main goal of this project is to develop a technologically simple process for hydrogen production from natural gas (NG) and other hydrocarbon fuels via single-step decomposition of hydrocarbons. This approach eliminates or significantly reduces CO{sub 2} emission. Carbon is a valuable by-product of this process, whereas conventional methods of hydrogen production from NG produce no useful by-products. This approach is based on the use of special catalysts that reduce the maximum temperature of the process from 1400-1500{degrees}C (thermal non-catalytic decomposition of methane) to 500-900{degrees}C. Transition metal based catalysts and various forms of carbon are among the candidate catalysts for the process. This approach can advantageously be used for the development of compact NG reformers for on-site production of hydrogen-methane blends at refueling stations and, also, for the production of hydrogen-rich gas for fuel cell applications. The author extended the search for active methane decomposition catalysts to various modifications of Ni-, Fe-, Mo- and Co-based catalysts. Variation in the operational parameters makes it possible to produce H{sub 2}-CH{sub 4} blends with a wide range of hydrogen concentrations that vary from 15 to 98% by volume. The author found that Ni-based catalysts are more effective at temperatures below 750{degrees}C, whereas Fe-based catalysts are effective at temperatures above 800{degrees}C for the production of hydrogen with purity of 95% v. or higher. The catalytic pyrolysis of liquid hydrocarbons (pentane, gasoline) over Fe-based catalyst was conducted. The author observed the production of a hydrogen-rich gas (hydrogen concentration up to 97% by volume) at a rate of approximately 1L/min.mL of hydrocarbon fuel.

  7. Natural products as potential cancer therapy enhancers: A preclinical update

    Directory of Open Access Journals (Sweden)

    Abed Agbarya

    2014-09-01

    Full Text Available Cancer is a multifactorial disease that arises as a consequence of alterations in many physiological processes. Recently, hallmarks of cancer were suggested that include sustaining proliferative signaling, evading growth suppressors, resisting cell death, enabling replicative immortality, inducing angiogenesis, and activating invasion and metastasis, along with two emerging hallmarks including reprogramming energy metabolism and escaping immune destruction. Treating multifactorial diseases, such as cancer with agents targeting a single target, might provide partial treatment and, in many cases, disappointing cure rates. Epidemiological studies have consistently shown that the regular consumption of fruits and vegetables is strongly associated with a reduced risk of developing chronic diseases, such as cardiovascular diseases and cancer. Since ancient times, plants, herbs, and other natural products have been used as healing agents. Moreover, the majority of the medicinal substances available today have their origin in natural compounds. Traditionally, pharmaceuticals are used to cure diseases, and nutrition and herbs are used to prevent disease and to provide an optimal balance of macro- and micro-nutrients needed for good health. We explored the combination of natural products, dietary nutrition, and cancer chemotherapeutics for improving the efficacy of cancer chemotherapeutics and negating side effects.

  8. Polyphenols-rich natural products for treatment of diabetes.

    Science.gov (United States)

    Dragan, S; Andrica, F; Serban, Maria-Corina; Timar, R

    2015-01-01

    Currently, experimental and clinical evidences showed that polyphenols-rich natural products, like nutraceuticals and food supplements, may offer unique treatment modalities in type 2 diabetes mellitus (DM), due to their biological properties. Natural products modulate the carbohydrate metabolism by various mechanisms, such as restoring beta-cells integrity and physiology, enhancing insulin releasing activity, and the glucose using. Sea buckthorn berries, red grapes, bilberries, chokeberries and popular drinks like cocoa, coffee and green tea are all rich in polyphenols and may decrease the insulin response, offer in g a natural alternative of treatment in diabetes. Therefore, researches are now focused on potential efficacies of different types of polyphenols, including flavonoids, phenolic acids, lignans, anthocyans and stilbenes. Animal and human studies showed that polyphenols modulate carbohydrate and lipid metabolism, decrease glycemia and insulin resistance, increase lipid metabolism and optimize oxidative stress and inflammatory processes. It is important to understand the proper dose and duration of supplementation with polyphenols-rich extracts in order to guide effective therapeutic interventions in diabetic patients.

  9. Natural products as potential cancer therapy enhancers: A preclinical update.

    Science.gov (United States)

    Agbarya, Abed; Ruimi, Nili; Epelbaum, Ron; Ben-Arye, Eran; Mahajna, Jamal

    2014-01-01

    Cancer is a multifactorial disease that arises as a consequence of alterations in many physiological processes. Recently, hallmarks of cancer were suggested that include sustaining proliferative signaling, evading growth suppressors, resisting cell death, enabling replicative immortality, inducing angiogenesis, and activating invasion and metastasis, along with two emerging hallmarks including reprogramming energy metabolism and escaping immune destruction. Treating multifactorial diseases, such as cancer with agents targeting a single target, might provide partial treatment and, in many cases, disappointing cure rates. Epidemiological studies have consistently shown that the regular consumption of fruits and vegetables is strongly associated with a reduced risk of developing chronic diseases, such as cardiovascular diseases and cancer. Since ancient times, plants, herbs, and other natural products have been used as healing agents. Moreover, the majority of the medicinal substances available today have their origin in natural compounds. Traditionally, pharmaceuticals are used to cure diseases, and nutrition and herbs are used to prevent disease and to provide an optimal balance of macro- and micro-nutrients needed for good health. We explored the combination of natural products, dietary nutrition, and cancer chemotherapeutics for improving the efficacy of cancer chemotherapeutics and negating side effects.

  10. Total Synthesis of the Natural Product-Pinosylvin and its Analog

    Institute of Scientific and Technical Information of China (English)

    2000-01-01

    We synthesised a natural product (10) , isolated from G.parvifolium , and its analog. The synthetic product was characterized by elemental analysis and 1H-NMR in comparision with the corresponding natural product.

  11. Entotheonella Bacteria as Source of Sponge-Derived Natural Products: Opportunities for Biotechnological Production.

    Science.gov (United States)

    Bhushan, Agneya; Peters, Eike E; Piel, Jörn

    2017-01-01

    Marine sponges belong to the oldest animals existing today. Apart from their role in recycling of carbon and nitrogen in the ocean, they are also an important source of a wide variety of structurally diverse bioactive natural products. Over the past few decades, a multitude of compounds from sponges have been discovered exhibiting diverse, pharmacologically promising activities. However, in many cases the low substance quantities present in the sponge tissue would require the collection of large amounts of sponge material, thus impeding further drug development. Recent research has focused on understanding natural product biosynthesis in sponges and on investigating symbiotic bacteria as possible production sources in order to develop sustainable production systems. This chapter covers research efforts that have taken place over the past few years involving the identification of 'Entotheonella' symbionts responsible for production of sponge compounds, as well as the elucidation of their biosynthetic routes, highlighting future biotechnological applications.

  12. Water for wood products versus nature, food or feed

    Science.gov (United States)

    Schyns, Joep; Booij, Martijn; Hoekstra, Arjen

    2017-04-01

    more water available for the generation of other ecosystem services. Our findings contribute to a more complete picture of the human appropriation of water and the understanding of the interlinkages between the SDGs, thus feeding the debate on water for wood products versus nature, food or feed.

  13. Environmental review of natural gas production in Lake Erie

    Energy Technology Data Exchange (ETDEWEB)

    O' Shea, K. [Dillon Consulting Ltd., Cambridge, ON (Canada)

    2002-07-01

    The water of Lake Erie is used as a source of drinking water for Ontario, New York, Pennsylvania, Ohio and Michigan. An environmental review has been conducted to determine the impact of drilling operations on the overall ecology of the lake. Since 1913, 2000 natural gas wells have been drilled in Lake Erie, of which 550 currently produce gas and account for 75 per cent of Ontario's total gas production. 180 wells are shut-in or suspended and the remaining wells have been abandoned. The gas wells are connected to onshore production facilities by approximately 1,600 km of small diameter pipelines that lie buried near shore or on top of the lake bed. Nearly 90 per cent of the in-lake infrastructure is in water depths of more than 20 metres. Talisman Energy is actively involved with the Canadian Coast Guard, the Department of Fisheries and Oceans, and the Ministry of Natural Resources to ensure cooperation between regulators and off-shore personnel. The environmental assessment of natural gas production in Lake Erie included a review of regulatory and best management practices, a biophysical overview of the lake, and a review of drilling practices, well completions, handling of waste streams, materials management, operations inspections, wastewater discharge, air emissions, and oil spills. It was revealed that for most drilling programs, cuttings are washed and discharged to the Lake. Ongoing testing will determine the impact that this practice has on benthic populations. The drill muds used for drilling operations are water based, environmentally friendly, and re-used between well locations. For completion programs, all well activities are closed circuit operations. Wells are abandoned through plugging with cement, removing wellheads and casing below the lake bottom. There has been a reported volume of about 23,000 litres of spilled product from 1990 to 2001, of which 68 per cent has come from 3 industrial companies that operate near Lake Erie. The offshore gas

  14. Bioactive Natural Products of Marine Sponges from the Genus Hyrtios

    Directory of Open Access Journals (Sweden)

    Nourhan Hisham Shady

    2017-05-01

    Full Text Available Marine sponges are known as a rich source for novel bioactive compounds with valuable pharmacological potential. One of the most predominant sponge genera is Hyrtios, reported to have various species such as Hyrtios erectus, Hyrtios reticulatus, Hyrtios gumminae, Hyrtios communis, and Hyrtios tubulatus and a number of undescribed species. Members of the genus Hyrtios are a rich source of natural products with diverse and valuable biological activities, represented by different chemical classes including alkaloids, sesterterpenes and sesquiterpenes. This review covers the literature until June 2016, providing a complete survey of all compounds isolated from the genus Hyrtios with their corresponding biological activities whenever applicable.

  15. A general enantioselective route to the chamigrene natural product family

    KAUST Repository

    White, David E.

    2010-06-01

    Described in this report is an enantioselective route toward the chamigrene natural product family. The key disconnections in our synthetic approach include sequential enantioselective decarboxylative allylation and ring-closing olefin metathesis to form the all-carbon quaternary stereocenter and spirocyclic core present in all members of this class of compounds. The generality of this strategy is demonstrated by the first total syntheses of elatol and the proposed structure of laurencenone B, as well as the first enantioselective total syntheses of laurencenone C and α-chamigrene. A brief exploration of the substrate scope of the enantioselective decarboxylative allylation/ring-closing metathesis sequence with fully substituted vinyl chlorides is also presented.

  16. NMR structural studies of oligosaccharides and other natural products

    DEFF Research Database (Denmark)

    Kjærulff, Louise

    produce secondary metabolites for signaling and competing against other organisms, and these molecules are important in drug discovery due to their inherent biological activities. From a marine Photobacterium (P. halotolerans) we isolated the solonamides and the ngercheumicins, two families of cyclic....... fijiensis, was also investigated for production of novel secondary metabolites, and a new pyranonigrin (E) was isolated and structure elucidated by NMR spectroscopy along with JBIR-74 and decumbenone A, two known metabolites previously isolated from Aspergillus and Penicillium species. Oligosaccharides...... with respect to n+1JHH between these two experiments, observed in the nJCH HMBC cross peak. Through a double editing procedure this enables straightforward determination of both sign and magnitude of n+1JHH, including for very small coupling constants. Excellent results were obtained for the natural product...

  17. Natural products from Bacillus subtilis with antimicrobial properties☆

    Institute of Scientific and Technical Information of China (English)

    Tao Wang; Yafei Liang; Mianbin Wu; Zhengjie Chen; Jianping Lin; Lirong Yang

    2015-01-01

    Bacil us subtilis produces many chemical y-diverse secondary metabolites of interest to chemists and biologists. Based on this, this review gives a detalled overview of the natural components produced by B. subtilis including cyclic lipopeptides, polypeptides, proteins (enzymes), and non-peptide products. Their structures, bioactive ac-tivities and the relevant variants as novel lead structures for drug discovery are also described. The challenging effects of fermentation metabolites, isolation and purification, as wel as the overproduction of bioactive com-pounds from B. subtilis by metabolic engineering, were also highlighted. Systematical y exploring biosynthetic routes and the functions of secondary metabolites from B. subtilis may not only be beneficial in improving yields of the products, but also in helping them to be used in food industry and public medical service on a large-scale.

  18. Natural Dietary and Herbal Products in Anti-Obesity Treatment.

    Science.gov (United States)

    Sun, Nan-Nong; Wu, Tsung-Yen; Chau, Chi-Fai

    2016-10-11

    The prevalence of overweight and obesity is on the rise around the world. Common comorbidities associated with obesity, particularly diabetes, hypertension, and heart disease have an impact on social and financial systems. Appropriate lifestyle and behavior interventions are still the crucial cornerstone to weight loss success, but maintaining such a healthy lifestyle is extremely challenging. Abundant natural materials have been explored for their obesity treatment potential and widely used to promote the development of anti-obesity products. The weight loss segment is one of the major contributors to the overall revenue of the dietary supplements market. In this review, the anti-obesity effects of different dietary or herbal products, and their active ingredients and mechanisms of action against obesity will be discussed.

  19. The snowmaker: nature identical snow production in the laboratory

    Science.gov (United States)

    Schleef, S.; Jaggi, M.; Loewe, H.; Schneebeli, M.

    2013-12-01

    Using natural snow for laboratory experiments can be tricky due to shortage of winter periods and snowfall, difficulties of sample casting and transport, and the great variability of natural snow due to the varying conditions of crystal growth in the clouds. This hinders repeatable laboratory experiments with reproducible specimen and microstructural characteristics. To minimize experimental uncertainties we designed an improved machine called snowmaker, which enables us to produce nature-identical snow in a cold laboratory under well defined conditions. The snowmaker is based on well-known principles: warm humid air from a heated water basin is advected into a cold nucleation chamber where the vapor resublimates on stretched Nylon wires. Crystals are automatically harvested by a motor driven brush rack and collected in a box, thereby several kilograms of snow can be produced per day with minimum maintenance. The excess vapor is collected in a moisture trap to avoid frost in the laboratory. The entire construction is designed as a rolling, modular assembly system which can easily carried out of the laboratory for defrosting. In addition to previous attempts we focus on the reproducibility of the samples and the comparison to natural snow down to the microscale. We show that the settings of water temperature and cold laboratory temperature facilitates the production of different crystal shapes like dendrites and needles in a reproducible way. Besides photography, we analyzed the microstructure of snowmaker crystals in aggregated specimen by X-ray microtomography. Depending on the settings we can create reproducible samples with density of 50-170 kg/m3 and specific surface areas of 50-80 mm-1. We briefly touch similarities between artificial and natural snow samples with respect to crystal habit, microstructural parameters and short-time metamorphism.

  20. US production of natural gas from tight reservoirs

    Energy Technology Data Exchange (ETDEWEB)

    1993-10-18

    For the purposes of this report, tight gas reservoirs are defined as those that meet the Federal Energy Regulatory Commission`s (FERC) definition of tight. They are generally characterized by an average reservoir rock permeability to gas of 0.1 millidarcy or less and, absent artificial stimulation of production, by production rates that do not exceed 5 barrels of oil per day and certain specified daily volumes of gas which increase with the depth of the reservoir. All of the statistics presented in this report pertain to wells that have been classified, from 1978 through 1991, as tight according to the FERC; i.e., they are ``legally tight`` reservoirs. Additional production from ``geologically tight`` reservoirs that have not been classified tight according to the FERC rules has been excluded. This category includes all producing wells drilled into legally designated tight gas reservoirs prior to 1978 and all producing wells drilled into physically tight gas reservoirs that have not been designated legally tight. Therefore, all gas production referenced herein is eligible for the Section 29 tax credit. Although the qualification period for the credit expired at the end of 1992, wells that were spudded (began to be drilled) between 1978 and May 1988, and from November 5, 1990, through year end 1992, are eligible for the tax credit for a subsequent period of 10 years. This report updates the EIA`s tight gas production information through 1991 and considers further the history and effect on tight gas production of the Federal Government`s regulatory and tax policy actions. It also provides some high points of the geologic background needed to understand the nature and location of low-permeability reservoirs.

  1. Potential anti-inflammatory natural products from marine algae.

    Science.gov (United States)

    Fernando, I P Shanura; Nah, Jae-Woon; Jeon, You-Jin

    2016-12-01

    Inflammatory diseases have become one of the leading causes of health issue throughout the world, having a considerable influence on healthcare costs. With the emerging developments in natural product, synthetic and combinatorial chemistry, a notable success has been achieved in discovering natural products and their synthetic structural analogs with anti-inflammatory activity. However, many of these therapeutics have indicated detrimental side effects upon prolonged usage. Marine algae have been identified as an underexplored reservoir of unique anti-inflammatory compounds. These include polyphenols, sulfated polysaccharides, terpenes, fatty acids, proteins and several other bioactives. Consumption of these marine algae could provide defense against the pathophysiology of many chronic inflammatory diseases. With further investigation, algal anti-inflammatory phytochemicals have the potential to be used as therapeutics or in the synthesis of structural analogs with profound anti-inflammatory activity with reduced side effects. The current review summarizes the latest knowledge about the potential anti-inflammatory compounds discovered from marine algae. Copyright © 2016 Elsevier B.V. All rights reserved.

  2. The Impending Renaissance in Discovery & Development of Natural Products.

    Science.gov (United States)

    Pawar, Sandip V; Ho, Joe C H; Yadav, Ganapati D; Yadav, Vikramaditya G

    2017-01-01

    Antibiotics are wonder drugs. Unfortunately, owing to overuse, antibiotic resistance is now a serious problem. Society now finds itself in the post-antibiotic era, and the threat of infectious diseases is on the rise. New antibiotics are sorely needed. There is strong evidence that suggests natural products are an attractive source of new antimicrobials. They posses desirable structural and chemical properties that make them potent thearpeutics. However, steep tehnological challenges associated with screening and manufacturing these molecules has stifled the discovery, development and marketing of new antimicrobials. To this end, two recent scientific developments are poised to redress this situation. The recent development of metagenomics and ancillary high-throughput screening technologies has exponentiated the volume of useful genetic sequence information that can be screened for antimicrobial discovery. These approaches have been instrumental in the discovery of new antibiotics from soil and marine environments. Secondly, a new manufacturing paradigm employing metabolic engineering as its engine has greatly accelerated the path to market for these molecules, in addition to improving the atom and energy economy of antimicrobial manufacturing. We outine these developments in this review, and provide a perspective on integrating next-generation approaches such as metagenomics and metabolic engineering with traditional methodologies for discovering and manufacturing antimicrobial natural products in order to unleash a rennaissance in the discovery and development of antimicrobials.

  3. The potential of natural products for targeting PPARα

    Directory of Open Access Journals (Sweden)

    Daniela Rigano

    2017-07-01

    Full Text Available Peroxisome proliferator activated receptors (PPARs α, -γ and -β/δ are ligand-activated transcription factors and members of the superfamily of nuclear hormone receptor. These receptors play key roles in maintaining glucose and lipid homeostasis by modulating gene expression. PPARs constitute a recognized druggable target and indeed several classes of drugs used in the treatment of metabolic disease symptoms, such as dyslipidemia (fibrates, e.g. fenofibrate and gemfibrozil and diabetes (thiazolidinediones, e.g. rosiglitazone and pioglitazone are ligands for the various PPAR isoforms. More precisely, antidiabetic thiazolidinediones act on PPARγ, while PPARα is the main molecular target of antidyslipidemic fibrates. Over the past few years, our understanding of the mechanism underlying the PPAR modulation of gene expression has greatly increased. This review presents a survey on terrestrial and marine natural products modulating the PPARα system with the objective of highlighting how the incredible chemodiversity of natural products can provide innovative leads for this “hot” target.

  4. Paraptosis in the anti-cancer arsenal of natural products.

    Science.gov (United States)

    Lee, Dongjoo; Kim, In Young; Saha, Sharmistha; Choi, Kyeong Sook

    2016-06-01

    Given the problems with malignant cancer cells showing innate and acquired resistance to apoptosis, we need alternative means to induce cell death in cancer. Paraptosis is a type of programmed cell death that is characterized by dilation of the endoplasmic reticulum (ER) and/or mitochondria. Although relatively little is known regarding the molecular basis of paraptosis, the underlying mechanism clearly differs from that of apoptosis. Recent studies have shown that various natural products, including curcumin, celastrol, 15d-PGJ2, ophiobolin A, and paclitaxel, demonstrate anti-cancer effects by inducing the paraptosis-associated cell death, which was commonly characterized by vacuolation derived from the ER. Perturbation of cellular proteostasis due to proteasomal inhibition and disruption of sulfhydryl homeostasis, generation of reactive oxygen species, and/or imbalanced homeostasis of ions (e.g., Ca(2+) and K(+)) appear to contribute to the accumulation of misfolded protein and proteotoxicity in this process. Given the pathophysiological importance of paraptosis and the debate regarding the importance of apoptosis in solid tumor, we need to collect the available knowledge regarding paraptosis and suggest future directions in the field. Here, we review the morphological and biochemical features of paraptosis, the natural products that induce paraptosis-associated cell death, their proposed mechanisms, and the significance of paraptosis as a potential anti-cancer strategy. Such work and future clarifications should enable the development of new strategies for preventing cancer and/or combating malignant cancer.

  5. Total Synthesis of Natural Products Using Hypervalent Iodine Reagents

    Science.gov (United States)

    Maertens, Gaetan; L'homme, Chloe; Canesi, Sylvain

    2014-12-01

    We present a review of natural product syntheses accomplished in our laboratory during the last five years. Each synthetic route features a phenol dearomatization promoted by an environmentally benign hypervalent iodine reagent. The dearomatizations demonstrate the “aromatic ring umpolung” concept, and involve stereoselective remodeling of the inert unsaturations of a phenol into a highly functionalized key intermediate that may contain a quaternary carbon center and a prochiral dienone system. Several new oxidative strategies were employed, including transpositions (1,3-alkyl shift and Prins-pinacol), a polycyclization, an ipso rearrangement, and direct nucleophilic additions at the phenol para position. Several alkaloids, heterocyclic compounds, and a polycyclic core have been achieved, including sceletenone (a serotonin reuptake inhibitor), acetylaspidoalbidine (an antitumor agent), fortucine (antiviral and antitumor), erysotramidine (curare-like effect), platensimycin (an antibiotic), and the main core of a kaurane diterpene (immunosuppressive agent and stimulator of apoptosis). These concise and in some cases enantioselective syntheses effectively demonstrate the importance of hypervalent iodine reagents in the total synthesis of bioactive natural products.

  6. Total Synthesis of Natural Products Using Hypervalent Iodine Reagents

    Directory of Open Access Journals (Sweden)

    Gaetan eMaertens

    2015-01-01

    Full Text Available We present a review of natural product syntheses accomplished in our laboratory during the last five years. Each synthetic route features a phenol dearomatization promoted by an environmentally benign hypervalent iodine reagent. The dearomatizations demonstrate the aromatic ring umpolung concept, and involve stereoselective remodeling of the inert unsaturations of a phenol into a highly functionalized key intermediate that may contain a quaternary carbon center and a prochiral dienone system. Several new oxidative strategies were employed, including transpositions (1,3-alkyl shift and Prins-pinacol, a polycyclization, an ipso rearrangement, and direct nucleophilic additions at the phenol para position. Several alkaloids, heterocyclic compounds, and a polycyclic core have been achieved, including sceletenone (a serotonin reuptake inhibitor, acetylaspidoalbidine (an antitumor agent, fortucine (antiviral and antitumor, erysotramidine (curare-like effect, platensimycin (an antibiotic, and the main core of a kaurane diterpene (immunosuppressive agent and stimulator of apoptosis. These concise and in some cases enantioselective syntheses effectively demonstrate the importance of hypervalent iodine reagents in the total synthesis of bioactive natural products.

  7. Systems biology approaches to understand natural products biosynthesis

    Directory of Open Access Journals (Sweden)

    Cuauhtemoc eLicona-Cassani

    2015-12-01

    Full Text Available Actinomycetes populate soils and aquatic sediments which impose biotic and abiotic challenges for their survival. As a result, actinomycetes metabolism and genomes have evolved to produce an overwhelming diversity of specialized molecules. Polyketides, non-ribosomal peptides, post-translationally modified peptides, lactams and terpenes are well known bioactive natural products with enormous industrial potential. Accessing such biological diversity has proven difficult due to the complex regulation of cellular metabolism in actinomycetes and to the sparse knowledge of their physiology. The past decade, however, has seen the development of omics technologies that have significantly contributed to our better understanding of their biology. Key observations have contributed towards a shift in the exploitation of actinomycetes biology, such as using their full genomic potential, activating entire pathways through key metabolic elicitors and pathway engineering to improve biosynthesis. Here, we review recent efforts devoted to achieving enhanced discovery, activation and manipulation of natural product biosynthetic pathways in model actinomycetes using genome-scale biological datasets.

  8. Prevention of microbial communities: novel approaches based natural products.

    Science.gov (United States)

    Mogosanu, George D; Grumezescu, Alexandru M; Huang, Keng-Shiang; Bejenaru, Ludovic E; Bejenaru, Cornelia

    2015-01-01

    Firmly attached to different living or non-living, solid or fluid surfaces rich in nutrients and moisture, microbial biofilm is a matter of great interest due to its major importance for the healthcare community. Depending on common strategies such as mutual protection and hibernation (quiescent bacteria), the resistance, survival and virulence of microbial communities have large implications for human pathology, clinical environment and biomedical devices. The microbial biofilm is continuously changing, stimulating inflammation, increasing vascular permeability and preventing the action of macrophages. About 80% of human infections affecting the gastrointestinal, genitourinary and respiratory systems, oral mucosa and teeth, eyes, middle ear and skin are caused by biofilm-associated microorganisms. Therefore, the search for modern strategies is even more important as microbial biofilms resistant to conventional antibiotics, antiseptics and disinfectants are involved in the frequent treatment failures of some chronic inflammatory diseases and wounds. Natural products containing secondary metabolites, such as aromatic compounds, sulphurated derivatives, terpenoids (essential oils) and alkaloids as quorum-sensing inhibitors and biofilm disruptors, are promising alternatives for the prophylaxis and treatment of chronic infections. Surface modification of medical devices with non-polar functionalized nanoparticles stabilizes the natural compounds antibiofilm activity and inhibits microbial adhesion and biofilm formation and growth for a longer period of time. In this regard, an interdisciplinary approach is needed due to the large number of natural derivatives alone or in combination with biocompatible and biodegradable micro-/ nano-engineered materials.

  9. Probiotics stimulate production of natural antibodies in chickens.

    Science.gov (United States)

    Haghighi, Hamid R; Gong, Jianhua; Gyles, Carlton L; Hayes, M Anthony; Zhou, Huaijun; Sanei, Babak; Chambers, James R; Sharif, Shayan

    2006-09-01

    Commensal bacteria in the intestine play an important role in the development of immune response. These bacteria interact with cells of the gut-associated lymphoid tissues (GALT). Among cells of the GALT, B-1 cells are of note. These cells are involved in the production of natural antibodies. In the present study, we determined whether manipulation of the intestinal microbiota by administration of probiotics, which we had previously shown to enhance specific systemic antibody response, could affect the development of natural antibodies in the intestines and sera of chickens. Our findings demonstrate that when 1-day-old chicks were treated with probiotics, serum and intestinal antibodies reactive to tetanus toxoid (TT) and Clostridium perfringens alpha-toxin in addition to intestinal immunoglobulin A (IgA) reactive to bovine serum albumin (BSA) were increased in unimmunized chickens. Moreover, IgG antibodies reactive to TT were increased in the intestines of probiotic-treated chickens compared to those of untreated controls. In serum, IgG and IgM reactive to TT and alpha-toxin were increased in probiotic-treated, unimmunized chickens compared to levels in untreated controls. However, no significant difference in serum levels of IgM or IgG response to BSA was observed. These results are suggestive of the induction of natural antibodies in probiotic-treated, unimmunized chickens. Elucidating the role of these antibodies in maintenance of the chicken immune system homeostasis and immune response to pathogens requires further investigation.

  10. Diverse Natural Products from Dichlorocyclobutanones: An Evolutionary Tale.

    Science.gov (United States)

    Deprés, Jean-Pierre; Delair, Philippe; Poisson, Jean-François; Kanazawa, Alice; Greene, Andrew E

    2016-02-16

    11-Nor PGE2 was prepared in our laboratory several years ago and used to obtain the corresponding ring-expanded γ-butyrolactam, γ-butyrolactone, and cyclopentanone derivatives. The conversion of a cyclobutanone into a cyclopentanone had relatively little precedent and merited further study. It was soon found that the presence of a single chlorine adjacent to the carbonyl not only greatly accelerated the reaction with ethereal diazomethane, but also substantially enhanced its regioselectivity; not surprisingly, a second chlorine further increased both. The confluence of this finding and the discovery by Krepski and Hassner that the presence of phosphorus oxychloride significantly improved the Zn-mediated dehalogenation procedure for the preparation of α,α-dichlorocyclobutanones from olefins provided the starting point for decades' worth of exciting adventures in natural product synthesis. A wide variety of naturally occurring 5-membered carbocycles (e.g., hirsutanes, cuparenones, bakkanes, guaianolides, azulenes) could thus be prepared by using dichloroketene-olefin cycloaddition, followed by regioselective one-carbon ring expansion with diazomethane. Importantly, it was also found that natural γ-butyrolactones (e.g., β-oxygenated γ-butyrolactones, lactone fatty acids) could be secured through regioselective Baeyer-Villiger oxidation of cycloadducts with m-CPBA and that naturally occurring γ-butyrolactam derivatives (e.g., amino acids, pyrrolidines, pyrrolizidines, indolizidines) could be efficiently obtained by regioselective Beckmann ring expansion of the adducts with O-(mesitylenesulfonyl)hydroxylamine (Tamura's reagent). These 5-membered carbocycles, γ-butyrolactones, and γ-butyrolactam derivatives were generally secured in enantiopure form through the use of either intrinsically chiral olefins or olefins bearing Stericol, a highly effective chiral auxiliary developed specifically for this "three-atom olefin annelation" approach. In addition

  11. Lichen symbiosis: nature's high yielding machines for induced hydrogen production.

    Science.gov (United States)

    Papazi, Aikaterini; Kastanaki, Elizabeth; Pirintsos, Stergios; Kotzabasis, Kiriakos

    2015-01-01

    Hydrogen is a promising future energy source. Although the ability of green algae to produce hydrogen has long been recognized (since 1939) and several biotechnological applications have been attempted, the greatest obstacle, being the O2-sensitivity of the hydrogenase enzyme, has not yet been overcome. In the present contribution, 75 years after the first report on algal hydrogen production, taking advantage of a natural mechanism of oxygen balance, we demonstrate high hydrogen yields by lichens. Lichens have been selected as the ideal organisms in nature for hydrogen production, since they consist of a mycobiont and a photobiont in symbiosis. It has been hypothesized that the mycobiont's and photobiont's consumption of oxygen (increase of COX and AOX proteins of mitochondrial respiratory pathways and PTOX protein of chrolorespiration) establishes the required anoxic conditions for the activation of the phycobiont's hydrogenase in a closed system. Our results clearly supported the above hypothesis, showing that lichens have the ability to activate appropriate bioenergetic pathways depending on the specific incubation conditions. Under light conditions, they successfully use the PSII-dependent and the PSII-independent pathways (decrease of D1 protein and parallel increase of PSaA protein) to transfer electrons to hydrogenase, while under dark conditions, lichens use the PFOR enzyme and the dark fermentative pathway to supply electrons to hydrogenase. These advantages of lichen symbiosis in combination with their ability to survive in extreme environments (while in a dry state) constitute them as unique and valuable hydrogen producing natural factories and pave the way for future biotechnological applications.

  12. Lichen symbiosis: nature's high yielding machines for induced hydrogen production.

    Directory of Open Access Journals (Sweden)

    Aikaterini Papazi

    Full Text Available Hydrogen is a promising future energy source. Although the ability of green algae to produce hydrogen has long been recognized (since 1939 and several biotechnological applications have been attempted, the greatest obstacle, being the O2-sensitivity of the hydrogenase enzyme, has not yet been overcome. In the present contribution, 75 years after the first report on algal hydrogen production, taking advantage of a natural mechanism of oxygen balance, we demonstrate high hydrogen yields by lichens. Lichens have been selected as the ideal organisms in nature for hydrogen production, since they consist of a mycobiont and a photobiont in symbiosis. It has been hypothesized that the mycobiont's and photobiont's consumption of oxygen (increase of COX and AOX proteins of mitochondrial respiratory pathways and PTOX protein of chrolorespiration establishes the required anoxic conditions for the activation of the phycobiont's hydrogenase in a closed system. Our results clearly supported the above hypothesis, showing that lichens have the ability to activate appropriate bioenergetic pathways depending on the specific incubation conditions. Under light conditions, they successfully use the PSII-dependent and the PSII-independent pathways (decrease of D1 protein and parallel increase of PSaA protein to transfer electrons to hydrogenase, while under dark conditions, lichens use the PFOR enzyme and the dark fermentative pathway to supply electrons to hydrogenase. These advantages of lichen symbiosis in combination with their ability to survive in extreme environments (while in a dry state constitute them as unique and valuable hydrogen producing natural factories and pave the way for future biotechnological applications.

  13. Lichen Symbiosis: Nature's High Yielding Machines for Induced Hydrogen Production

    Science.gov (United States)

    Papazi, Aikaterini; Kastanaki, Elizabeth; Pirintsos, Stergios; Kotzabasis, Kiriakos

    2015-01-01

    Hydrogen is a promising future energy source. Although the ability of green algae to produce hydrogen has long been recognized (since 1939) and several biotechnological applications have been attempted, the greatest obstacle, being the O2-sensitivity of the hydrogenase enzyme, has not yet been overcome. In the present contribution, 75 years after the first report on algal hydrogen production, taking advantage of a natural mechanism of oxygen balance, we demonstrate high hydrogen yields by lichens. Lichens have been selected as the ideal organisms in nature for hydrogen production, since they consist of a mycobiont and a photobiont in symbiosis. It has been hypothesized that the mycobiont’s and photobiont’s consumption of oxygen (increase of COX and AOX proteins of mitochondrial respiratory pathways and PTOX protein of chrolorespiration) establishes the required anoxic conditions for the activation of the phycobiont’s hydrogenase in a closed system. Our results clearly supported the above hypothesis, showing that lichens have the ability to activate appropriate bioenergetic pathways depending on the specific incubation conditions. Under light conditions, they successfully use the PSII-dependent and the PSII-independent pathways (decrease of D1 protein and parallel increase of PSaA protein) to transfer electrons to hydrogenase, while under dark conditions, lichens use the PFOR enzyme and the dark fermentative pathway to supply electrons to hydrogenase. These advantages of lichen symbiosis in combination with their ability to survive in extreme environments (while in a dry state) constitute them as unique and valuable hydrogen producing natural factories and pave the way for future biotechnological applications. PMID:25826211

  14. NATURAL ANTIOXIDANT INGREDIENT FROM BY-PRODUCTS OF FRUITS

    Directory of Open Access Journals (Sweden)

    G. S. El-Baroty

    2014-01-01

    used safely in the edible oil industry and cosmetics to delay its oxidation. It can be applied in other food industries as a natural antioxidant instead of synthetic antioxidants. Further study should be carried out to identify the predominant phenolics responsible for the antioxidant activity of by product extracts.

  15. Production of substitute natural gas by biomass hydrogasification

    Energy Technology Data Exchange (ETDEWEB)

    Mozaffarian, M.; Zwart, R.W.R. [ECN Biomass, Petten (Netherlands)

    2000-11-01

    Hydrogen, generated from renewable sources, is likely to play a major role in the future energy supply. The storage and transport of hydrogen can take place in its free form (H2), or chemically bound, e.g. as methane. However, the storage and transport of hydrogen in its free form are more complex, and probably would require more energy than the storage and transport of hydrogen in chemical form. An additional important advantage of the indirect use of hydrogen as energy carrier is, that in the future renewable energy supply, pads of the existing large-scale energy infra- structure could still be used. Production of Substitute Natural Gas (SNG) by biomass hydrogasification has been assessed as a process for chemical storage of hydrogen. Thermodynamic analysis has shown the feasibility of this process. The product gas of the process has a Wobbe-index, a mole percentage methane, and a calorific value quite comparable to the quality of the Dutch natural gas. With a hydrogen content below 10 mol%, the produced SNG can be transported through the existing gas net without any additional adjustment. The integrated system has an energetic efficiency of 81% (LHV). In the long term, the required hydrogen for this process can be produced by water electrolysis, with electricity from renewable sources. In the short term, hydrogen may be obtained from hydrogen-rich gases available as by-product from industrial processes. Results of thermodynamic analysis of the process and experimental work, application potentials of the process in the Netherlands, and plans for future development are presented. 21 refs.

  16. Natural Product Research in the Australian Marine Invertebrate Dicathais orbita

    Directory of Open Access Journals (Sweden)

    Kirsten Benkendorff

    2013-04-01

    Full Text Available The predatory marine gastropod Dicathais orbita has been the subject of a significant amount of biological and chemical research over the past five decades. Natural products research on D. orbita includes the isolation and identification of brominated indoles and choline esters as precursors of Tyrian purple, as well as the synthesis of structural analogues, bioactivity testing, biodistributional and biosynthetic studies. Here I also report on how well these compounds conform to Lipinski’s rule of five for druglikeness and their predicted receptor binding and enzyme inhibitor activity. The composition of mycosporine-like amino acids, fatty acids and sterols has also been described in the egg masses of D. orbita. The combination of bioactive compounds produced by D. orbita is of interest for further studies in chemical ecology, as well as for future nutraceutical development. Biological insights into the life history of this species, as well as ongoing research on the gene expression, microbial symbionts and biosynthetic capabilities, should facilitate sustainable production of the bioactive compounds. Knowledge of the phylogeny of D. orbita provides an excellent platform for novel research into the evolution of brominated secondary metabolites in marine molluscs. The range of polarities in the brominated indoles produced by D. orbita has also provided an effective model system used to develop a new method for biodistributional studies. The well characterized suite of chemical reactions that generate Tyrian purple, coupled with an in depth knowledge of the ecology, anatomy and genetics of D. orbita provide a good foundation for ongoing natural products research.

  17. Occurrence of aflatoxin B1 in natural products

    Directory of Open Access Journals (Sweden)

    Guilherme Prado

    2012-12-01

    Full Text Available The media claims for the consumption of natural resource-based food have gradually increased in both developing and developed countries. The interest in the safety of these products is partially due to the possible presence of toxigenic fungi acting as mycotoxin producers, such as aflatoxins produced during the secondary metabolism of Aspergillus flavus, A. parasiticus and A. nomius. Aflatoxins, mainly aflatoxin B1, are directly associated with liver cancer in human beings. This paper is aimed at evaluating the presence of aflatoxin B1 in a few vegetable drugs, dried plant extracts and industrialized products traded in 2010 in the city of Belo Horizonte, State of Minas Gerais, Brazil. The method used for the quantification of aflatoxin B1 was based on extraction through acetone:water (85:15, immunoaffinity column purification followed by separation and detection in high efficiency liquid chromatography. Under the conditions of analysis, the Limits of Detection and Quantification were 0.6 µg kg-1 and 1.0 µg kg-1respectively. The complete sets of analyses were carried out in duplicate. Aflatoxin B1 was noticed in a single sample (< 1.0 µg kg-1. The results revealed low aflatoxin B1contamination in the products under analysis. However, it is required to establish a broad monitoring program in order to obtain additional data and check up on the actual extension of contamination.

  18. Natural gas productive capacity for the lower 48 states 1985 through 1997

    Energy Technology Data Exchange (ETDEWEB)

    NONE

    1996-12-01

    This publication presents information on wellhead productive capacity and a projection of gas production requirements. A history of natural gas production and productive capacity at the wellhead, along with a projection of the same, is illustrated.

  19. Synthetic biology for production of natural and new-to-nature terpenoids in photosynthetic organisms.

    Science.gov (United States)

    Arendt, Philipp; Pollier, Jacob; Callewaert, Nico; Goossens, Alain

    2016-07-01

    With tens of thousands of characterized members, terpenoids constitute the largest class of natural compounds that are synthesized by all living organisms. Several terpenoids play primary roles in the maintenance of cell membrane fluidity, as pigments or as phytohormones, but most of them function as specialized metabolites that are involved in plant resistance to herbivores or plant-environment interactions. Terpenoids are an essential component of human nutrition, and many are economically important pharmaceuticals, aromatics and potential next-generation biofuels. Because of the often low abundance in their natural source, as well as the demand for novel terpenoid structures with new or improved bioactivities, terpenoid biosynthesis has become a prime target for metabolic engineering and synthetic biology projects. In this review we focus on the creation of new-to-nature or tailor-made plant-derived terpenoids in photosynthetic organisms, in particular by means of combinatorial biosynthesis and the activation of silent metabolism. We reflect on the characteristics of different potential photosynthetic host organisms and recent advances in synthetic biology and discuss their utility for the (heterologous) production of (novel) terpenoids.

  20. Inhibitors of Microglial Neurotoxicity: Focus on Natural Products

    Directory of Open Access Journals (Sweden)

    Kyoungho Suk

    2011-01-01

    Full Text Available Microglial cells play a dual role in the central nervous system as they have both neurotoxic and neuroprotective effects. Uncontrolled and excessive activation of microglia often contributes to inflammation-mediated neurodegeneration. Recently, much attention has been paid to therapeutic strategies aimed at inhibiting neurotoxic microglial activation. Pharmacological inhibitors of microglial activation are emerging as a result of such endeavors. In this review, natural products-based inhibitors of microglial activation will be reviewed. Potential neuroprotective activity of these compounds will also be discussed. Future works should focus on the discovery of novel drug targets that specifically mediate microglial neurotoxicity rather than neuroprotection. Development of new drugs based on these targets may require a better understanding of microglial biology and neuroinflammation at the molecular, cellular, and systems levels.

  1. Deoxygedunin, a natural product with potent neurotrophic activity in mice.

    Directory of Open Access Journals (Sweden)

    Sung-Wuk Jang

    Full Text Available Gedunin, a family of natural products from the Indian neem tree, possess a variety of biological activities. Here we report the discovery of deoxygedunin, which activates the mouse TrkB receptor and its downstream signaling cascades. Deoxygedunin is orally available and activates TrkB in mouse brain in a BDNF-independent way. Strikingly, it prevents the degeneration of vestibular ganglion in BDNF -/- pups. Moreover, deoxygedunin robustly protects rat neurons from cell death in a TrkB-dependent manner. Further, administration of deoxygedunin into mice displays potent neuroprotective, anti-depressant and learning enhancement effects, all of which are mediated by the TrkB receptor. Hence, deoxygedunin imitates BDNF's biological activities through activating TrkB, providing a powerful therapeutic tool for treatment of various neurological diseases.

  2. The Complexity of Bioactive Natural Products in Plants

    DEFF Research Database (Denmark)

    Frisch, Tina

    Plants produce a diverse range of bioactive natural products promoting their fitness. These specialized metabolites may serve as chemical defence against herbivores and pathogens and may inhibit the growth and development of competing species. Hydroxynitrile glucosides and glucosinolates are two...... classes of defence compounds, which have diverging properties, but also share common biosynthetic features. Hydroxynitrile glucosides are produced in species across the plant kingdom, whereas glucosinolates are found almost exclusively within the Brassicales, which generally does not contain...... these two plant species interesting gateways for addressing these questions of evolution. The presented research demonstrates that the biosynthetic pathway for the hydroxynitrile glucoside alliarinoside in A. petiolata does not follow the general scheme for hydroxynitrile glucoside biosynthesis in other...

  3. Marine Natural Products from New Caledonia--A Review.

    Science.gov (United States)

    Motuhi, Sofia-Eléna; Mehiri, Mohamed; Payri, Claude Elisabeth; La Barre, Stéphane; Bach, Stéphane

    2016-03-16

    Marine micro- and macroorganisms are well known to produce metabolites with high biotechnological potential. Nearly 40 years of systematic prospecting all around the New Caledonia archipelago and several successive research programs have uncovered new chemical leads from benthic and planktonic organisms. After species identification, biological and/or pharmaceutical analyses are performed on marine organisms to assess their bioactivities. A total of 3582 genera, 1107 families and 9372 species have been surveyed and more than 350 novel molecular structures have been identified. Along with their bioactivities that hold promise for therapeutic applications, most of these molecules are also potentially useful for cosmetics and food biotechnology. This review highlights the tremendous marine diversity in New Caledonia, and offers an outline of the vast possibilities for natural products, especially in the interest of pursuing collaborative fundamental research programs and developing local biotechnology programs.

  4. Natural products in medicine: transformational outcome of synthetic chemistry.

    Science.gov (United States)

    Szychowski, Janek; Truchon, Jean-François; Bennani, Youssef L

    2014-11-26

    This review brings to the forefront key synthetic modifications on natural products (NPs) that have yielded successful drugs. The emphasis is placed on the power of targeted chemical transformations in enhancing the therapeutic value of NPs through optimization of pharmacokinetics, stability, potency, and/or selectivity. Multiple classes of NPs such as macrolides, opioids, steroids, and β-lactams used to treat a variety of conditions such as cancers, infections, inflammation are exemplified. Molecular modeling or X-ray structures of NP/protein complexes supporting the observed boost in therapeutic value of the modified NPs are also discussed. Significant advancement in synthetic chemistry, in structure determination, and in the understanding of factors controlling pharmacokinetics can now better position drug discovery teams to undertake NPs as valuable leads. We hope that the beneficial NPs synthetic modifications outlined here will reignite medicinal chemists' interest in NPs and their derivatives.

  5. Can Invalid Bioactives Undermine Natural Product-Based Drug Discovery?

    Science.gov (United States)

    2015-01-01

    High-throughput biology has contributed a wealth of data on chemicals, including natural products (NPs). Recently, attention was drawn to certain, predominantly synthetic, compounds that are responsible for disproportionate percentages of hits but are false actives. Spurious bioassay interference led to their designation as pan-assay interference compounds (PAINS). NPs lack comparable scrutiny, which this study aims to rectify. Systematic mining of 80+ years of the phytochemistry and biology literature, using the NAPRALERT database, revealed that only 39 compounds represent the NPs most reported by occurrence, activity, and distinct activity. Over 50% are not explained by phenomena known for synthetic libraries, and all had manifold ascribed bioactivities, designating them as invalid metabolic panaceas (IMPs). Cumulative distributions of ∼200,000 NPs uncovered that NP research follows power-law characteristics typical for behavioral phenomena. Projection into occurrence–bioactivity–effort space produces the hyperbolic black hole of NPs, where IMPs populate the high-effort base. PMID:26505758

  6. Structure Determination of Natural Products by Nuclear Magnetic Resonance Spectroscopy

    Science.gov (United States)

    Li, Du.

    High-field NMR experiments were used to determine the full structures of six new natural products extracted from plants. These are: four saponins (PT-2, P1, P2 and P3) from the plant Alphitonia zizyphoides found in Samoa; one sesquiterpene (DF-4) from Douglas fir and one diterpene derivative (E-2) from a Chinese medicinal herb. By concerted use of various 1D and 2D NMR techniques, the structures of the above compounds were established and complete resonance assignments were achieved. The 2D INADEQUATE technique coupled with a computerized spectral analysis was extensively used. When carried out on concentrations as low as 60 mg of sample, this technique provided absolute confirmation of the assignments for 35 of the possible 53 C-C bonds for PT-2. On 30 mg of sample of E-21, it revealed 22 of 28 possible C-C bonds.

  7. Marine Natural Products from New Caledonia—A Review

    Directory of Open Access Journals (Sweden)

    Sofia-Eléna Motuhi

    2016-03-01

    Full Text Available Marine micro- and macroorganisms are well known to produce metabolites with high biotechnological potential. Nearly 40 years of systematic prospecting all around the New Caledonia archipelago and several successive research programs have uncovered new chemical leads from benthic and planktonic organisms. After species identification, biological and/or pharmaceutical analyses are performed on marine organisms to assess their bioactivities. A total of 3582 genera, 1107 families and 9372 species have been surveyed and more than 350 novel molecular structures have been identified. Along with their bioactivities that hold promise for therapeutic applications, most of these molecules are also potentially useful for cosmetics and food biotechnology. This review highlights the tremendous marine diversity in New Caledonia, and offers an outline of the vast possibilities for natural products, especially in the interest of pursuing collaborative fundamental research programs and developing local biotechnology programs.

  8. Temperature effects on fish production across a natural thermal gradient.

    Science.gov (United States)

    O'Gorman, Eoin J; Ólafsson, Ólafur P; Demars, Benoît O L; Friberg, Nikolai; Guðbergsson, Guðni; Hannesdóttir, Elísabet R; Jackson, Michelle C; Johansson, Liselotte S; McLaughlin, Órla B; Ólafsson, Jón S; Woodward, Guy; Gíslason, Gísli M

    2016-09-01

    Global warming is widely predicted to reduce the biomass production of top predators, or even result in species loss. Several exceptions to this expectation have been identified, however, and it is vital that we understand the underlying mechanisms if we are to improve our ability to predict future trends. Here, we used a natural warming experiment in Iceland and quantitative theoretical predictions to investigate the success of brown trout as top predators across a stream temperature gradient (4-25 °C). Brown trout are at the northern limit of their geographic distribution in this system, with ambient stream temperatures below their optimum for maximal growth, and above it in the warmest streams. A five-month mark-recapture study revealed that population abundance, biomass, growth rate, and production of trout all increased with stream temperature. We identified two mechanisms that contributed to these responses: (1) trout became more selective in their diet as stream temperature increased, feeding higher in the food web and increasing in trophic position; and (2) trophic transfer through the food web was more efficient in the warmer streams. We found little evidence to support a third potential mechanism: that external subsidies would play a more important role in the diet of trout with increasing stream temperature. Resource availability was also amplified through the trophic levels with warming, as predicted by metabolic theory in nutrient-replete systems. These results highlight circumstances in which top predators can thrive in warmer environments and contribute to our knowledge of warming impacts on natural communities and ecosystem functioning.

  9. Biopiracy of natural products and good bioprospecting practice.

    Science.gov (United States)

    Efferth, Thomas; Banerjee, Mita; Paul, Norbert W; Abdelfatah, Sara; Arend, Joachim; Elhassan, Gihan; Hamdoun, Sami; Hamm, Rebecca; Hong, Chunlan; Kadioglu, Onat; Naß, Janine; Ochwangi, Dominic; Ooko, Edna; Ozenver, Nadire; Saeed, Mohamed E M; Schneider, Mathias; Seo, Ean-Jeong; Wu, Ching-Fen; Yan, Ge; Zeino, Maen; Zhao, Qiaoli; Abu-Darwish, Mohammad S; Andersch, Kai; Alexie, Gladys; Bessarab, Dawn; Bhakta-Guha, Dipita; Bolzani, Vanderlan; Dapat, Else; Donenko, Fedor V; Efferth, Monika; Greten, Henry J; Gunatilaka, Leslie; Hussein, Ahmed A; Karadeniz, Asuman; Khalid, Hassan E; Kuete, Victor; Lee, Ik-Soo; Liu, Liang; Midiwo, Jacob; Mora, Rodrigo; Nakagawa, Hiroshi; Ngassapa, Olipa; Noysang, Chanai; Omosa, Leonida K; Roland, Fred Hwiemtun; Shahat, Abdelaaty A; Saab, Antoine; Saeed, Elfatih M; Shan, Letian; Titinchi, Salam J J

    2016-02-15

    Biopiracy mainly focuses on the use of biological resources and/or knowledge of indigenous tribes or communities without allowing them to share the revenues generated out of economic exploitation or other non-monetary incentives associated with the resource/knowledge. Based on collaborations of scientists from five continents, we have created a communication platform to discuss not only scientific topics, but also more general issues with social relevance. This platform was termed 'PhytCancer -Phytotherapy to Fight Cancer' (www.phyt-cancer.uni-mainz.de). As a starting point, we have chosen the topic "biopiracy", since we feel this is of pragmatic significance for scientists working with medicinal plants. It was argued that the patenting of herbs or natural products by pharmaceutical corporations disregarded the ownership of the knowledge possessed by the indigenous communities on how these substances worked. Despite numerous court decisions in U.S.A. and Europe, several international treaties, (e.g. from United Nations, World Health Organization, World Trade Organization, the African Unity and others), sharing of a rational set of benefits amongst producers (mainly pharmaceutical companies) and indigenous communities is yet a distant reality. In this paper, we present an overview of the legal frameworks, discuss some exemplary cases of biopiracy and bioprospecting as excellent forms of utilization of natural resources. We suggest certain perspectives, by which we as scientists, may contribute towards prevention of biopiracy and also to foster the fair utilization of natural resources. We discuss ways, in which the interests of indigenous people especially from developing countries can be secured. Copyright © 2015 Elsevier GmbH. All rights reserved.

  10. Modulation of tumor microenvironment by chemopreventive natural products.

    Science.gov (United States)

    Park, Sin-Aye; Surh, Young-Joon

    2017-08-01

    The tumor microenvironment provides a niche in which cancer cells and their surrounding stromal cells reside and in which their interactions occur. The cross talk between cancer and stromal cells in the tumor microenvironment promotes many biological processes to support cancer cell growth, invasion, angiogenesis, and metastasis. Recently, not only cancer cells but also multiple types of surrounding stromal cells, including endothelial cells, immune cells, and fibroblasts in the tumor microenvironment, have been recognized to be attractive targets for reducing resistance to anticancer therapy and tumor recurrence. Many natural products present in fruits, vegetables, herbs, spices, and some marine organisms have been reported to inhibit, delay, or reverse multistage carcinogenesis and to inhibit the proliferation of cancerous cells and the self-renewal capacity of preexisting cancer stem-like cells. Some of these naturally occurring chemopreventive and anticarcinogenic substances can modulate the signal transduction involved in maintaining the activities/functions of stromal cells and their interactions with cancer cells within the tumor microenvironment. © 2017 New York Academy of Sciences.

  11. Culturable rare Actinomycetes: diversity, isolation and marine natural product discovery.

    Science.gov (United States)

    Subramani, Ramesh; Aalbersberg, William

    2013-11-01

    Rare Actinomycetes from underexplored marine environments are targeted in drug discovery studies due to the Actinomycetes' potentially huge resource of structurally diverse natural products with unusual biological activity. Of all marine bacteria, 10 % are Actinomycetes, which have proven an outstanding and fascinating resource for new and potent bioactive molecules. Past and present efforts in the isolation of rare Actinomycetes from underexplored diverse natural habitats have resulted in the isolation of about 220 rare Actinomycete genera of which more than 50 taxa have been reported to be the producers of 2,500 bioactive compounds. That amount represents greater than 25 % of the total Actinomycetes metabolites, demonstrating that selective isolation methods are being developed and extensively applied. Due to the high rediscovery rate of known compounds from Actinomycetes, a renewed interest in the development of new antimicrobial agents from rare and novel Actinomycetes is urgently required to combat the increasing number of multidrug-resistant human pathogens. To facilitate that discovery, this review updates all selective isolation media including pretreatment and enrichment methods for the isolation of marine rare Actinomycetes. In addition, this review demonstrates that discovering new compounds with novel scaffolds can be increased by intensive efforts in isolating and screening rare marine genera of Actinomycetes. Between 2007 and mid-2013, 80 new rare Actinomycete species were reported from marine habitats. They belong to 23 rare families, of which three are novel, and 20 novel genera. Of them, the family Micromonosporaceae is dominant as a producer of promising chemical diversity.

  12. New natural product carbonic anhydrase inhibitors incorporating phenol moieties.

    Science.gov (United States)

    Karioti, Anastasia; Ceruso, Mariangela; Carta, Fabrizio; Bilia, Anna-Rita; Supuran, Claudiu T

    2015-11-15

    Carbonic anhydrases (CAs, EC 4.2.1.1) catalyze the fundamental reaction of CO2 hydration in all living organisms, being actively involved in the regulation of a plethora of patho/physiological conditions. They represent a typical example of enzyme convergent evolution, as six genetically unrelated families of such enzymes were described so far. The need to find selective CA inhibitors (CAIs) triggered the investigation of natural product libraries, which proved to be a valid source of agents with such an activity, as demonstrated for the phenols, polyamines and coumarins. Herein we report an in vitro inhibition study of human (h) CA isoforms hCAs I, II, IV, VII and XII with a panel of natural polyphenols including flavones, flavonols, flavanones, flavanols, isoflavones and depsides, some of which extracted from Quercus ilex and Salvia miltiorrhiza. Several of the investigated derivatives showed interesting inhibition activity and selectivities for inhibiting some important isoforms over the off-target ones hCA I and II.

  13. Role of Antioxidants and Natural Products in Inflammation

    Directory of Open Access Journals (Sweden)

    Palanisamy Arulselvan

    2016-01-01

    Full Text Available Inflammation is a comprehensive array of physiological response to a foreign organism, including human pathogens, dust particles, and viruses. Inflammations are mainly divided into acute and chronic inflammation depending on various inflammatory processes and cellular mechanisms. Recent investigations have clarified that inflammation is a major factor for the progression of various chronic diseases/disorders, including diabetes, cancer, cardiovascular diseases, eye disorders, arthritis, obesity, autoimmune diseases, and inflammatory bowel disease. Free radical productions from different biological and environmental sources are due to an imbalance of natural antioxidants which further leads to various inflammatory associated diseases. In this review article, we have outlined the inflammatory process and its cellular mechanisms involved in the progression of various chronic modern human diseases. In addition, we have discussed the role of free radicals-induced tissue damage, antioxidant defence, and molecular mechanisms in chronic inflammatory diseases/disorders. The systematic knowledge regarding the role of inflammation and its associated adverse effects can provide a clear understanding in the development of innovative therapeutic targets from natural sources that are intended for suppression of various chronic inflammations associated diseases.

  14. Aminobenzoates as building blocks for natural product assembly lines.

    Science.gov (United States)

    Walsh, Christopher T; Haynes, Stuart W; Ames, Brian D

    2012-01-01

    The ortho-, meta-, and para- regioisomers of aminobenzoate are building blocks for a wide range of microbial natural products. Both the ortho-isomer (anthranilate) and PABA derive from the central shikimate pathway metabolite chorismate while the meta-isomer is not available by that route and starts from UDP-3-aminoglucose. PABA is largely funnelled into folate biosynthesis while anthranilate is the scaffold for biosynthetic elaboration into many natural heterocycles, most notably with its role in indole formation for tryptophan biosynthesis. Anthranilate is also converted to benzodiazepinones, fumiquinazolines, quinoxalines, phenoxazines, benzoxazolinates, quinolones, and phenazines, often with redox enzyme participation. The 5-hydroxy form of 3-aminobenzaote is the starter unit for ansa-bridged rifamycins, ansamitocins, and geldanamycins, whereas regioisomers 2-hydroxy, 4-hydroxy and 2,4-dihydroxy-3-aminobenzoate are key components of antimycin, grixazone, and platencin and platensimycin biosynthesis, respectively. The enzymatic mechanisms for generation of the aminobenzoate regioisomers and their subsequent utilization for diverse heterocycle and macrocycle construction are examined.

  15. Recent Trends in the Use of Natural Antioxidants for Meat and Meat Products

    National Research Council Canada - National Science Library

    Kumar, Yogesh; Yadav, Deep Narayan; Ahmad, Tanbir; Narsaiah, Kairam

    2015-01-01

    .... Thus, the food industry now chooses natural products over synthetic ones. This review provides an overview of the current trends in the use of antioxidants from natural sources, for potential applications in meat and meat products...

  16. Fingerprinting of Natural Product by Eastern Blotting Using Monoclonal Antibodies

    Directory of Open Access Journals (Sweden)

    Hiroyuki Tanaka

    2012-01-01

    Full Text Available We succeeded in developing the fingerprint of natural product by eastern blotting using monoclonal antibodies. After developing and separating them on a TLC plate, solasodine glycosides are oxidized by NaIO4 and reacted with a protein to give conjugates which are recognized with anti-solamargine monoclonal antibody (MAb. Anti-solamargine MAb having wide cross-reactivity can stain and detect all solasodine glycosides by fingerprint. Different sensitivity between solamargine and solasonine was observed. The detection limit was 1.6 ng of solasonine. The hydrolysed products of solamargine were determined by fingerprint of eastern blotting compared to their Rf values depending on the sugar number. Fingerprint by eastern blotting using anti-ginsenoside Rb1 MAb distinguished the formula containing ginseng prescribed in traditional Chinese medicine. By double-staining of ginsenosides it is possible to suggest that the staining color shows the pharmacological activity, such as the purple bands indicate ginsenosides having stimulation activity, and the blue color indicated compound like ginsenosides possessed the depression affect for the central nervous system (CNS, respectively.

  17. Cameroonian medicinal plants: Pharmacology and derived natural products

    Directory of Open Access Journals (Sweden)

    Thomas Efferth

    2010-10-01

    Full Text Available Many developing countries including Cameroon have mortality patterns that reflect high levels of infectious diseases and the risk of death during pregnancy and childbirth, in addition to cancers, cardiovascular diseases and chronic respiratory diseases that account for most deaths in the developed world. Several medicinal plants are used traditionally for their treatment. In this review, plants used in Cameroonian traditional medicine with evidence for the activities of their crude extracts and/or derived products have been discussed. A considerable number of plant extracts and isolated compounds possess significant antimicrobial, antiparasitic including anti-malarial, anti-proliferative, anti-inflammatory, anti-diabetes, and antioxidant effects. Most of the biologically active compounds belong to terpenoids, phenolics and alkaloids. Terpenoids from Cameroonian plants showed best activities as anti-parasitic, but rather poor antimicrobial effects. The best antimicrobial, anti-proliferative and antioxidant compounds were phenolics. In conclusion, many medicinal plants traditionally used in Cameroon to treat various ailments displayed good activities in vitro. This explains the endeavor of Cameroonian research institutes in drug discovery from indigenous medicinal plants. However, much work is still to be done to standardize methodologies and to study the mechanisms of action of isolated natural products.

  18. Toxic element contamination of natural health products and pharmaceutical preparations.

    Directory of Open Access Journals (Sweden)

    Stephen J Genuis

    Full Text Available BACKGROUND: Concern has recently emerged regarding the safety of natural health products (NHPs-therapies that are increasingly recommended by various health providers, including conventional physicians. Recognizing that most individuals in the Western world now consume vitamins and many take herbal agents, this study endeavored to determine levels of toxic element contamination within a range of NHPs. METHODS: Toxic element testing was performed on 121 NHPs (including Ayurvedic, traditional Chinese, and various marine-source products as well as 49 routinely prescribed pharmaceutical preparations. Testing was also performed on several batches of one prenatal supplement, with multiple samples tested within each batch. Results were compared to existing toxicant regulatory limits. RESULTS: Toxic element contamination was found in many supplements and pharmaceuticals; levels exceeding established limits were only found in a small percentage of the NHPs tested and none of the drugs tested. Some NHPs demonstrated contamination levels above preferred daily endpoints for mercury, cadmium, lead, arsenic or aluminum. NHPs manufactured in China generally had higher levels of mercury and aluminum. CONCLUSIONS: Exposure to toxic elements is occurring regularly as a result of some contaminated NHPs. Best practices for quality control-developed and implemented by the NHP industry with government oversight-is recommended to guard the safety of unsuspecting consumers.

  19. In vitro study of natural plant products against oral bacteria

    Institute of Scientific and Technical Information of China (English)

    Siddiqui R; Siti AsmaH; Tang L; Jie CC; Rosliza AR; Roziawati Y

    2009-01-01

    Objective:To analyze the effect of selected plant product against several bacterial which commonly causes oral infection.It was hope that in future,this product will become the remedy for treatment of oral infection and with the hope that it can substitute antibiotics.Methods:A total of 5 species of oral bacteria from American Type Culture Collection (ATCC)were employed in this study(S.mutans,S.aureus,P.aeruginosa,S.sobri-nus and L.salivarius).Three types of natural plants crude extracts were used (garlic,curry leaves and cloves).Bactericidal and bacteriostatic effects of these herbs were tested.Results:It was shown garlic had an-tibacterial effects on all bacteria.The Minimal Inhibitory Concentration (MIC in g/mL)of garlic towards S. aureus,P.aeruginosa,S.mutans,S.sobrinus and L.salivarius were 0.3,1.8,1.2,0.5 and 1.8,respectively. There was significant difference among the MIC of garlic on tested bacteria.It was more potent toward S.au-reus.The curry leaf solution on the other hand,did not show any zone of inhibition in all bacteria plates but adversely showed enhanced growth of those bacteria.Clove had shown its antibacterial effects on S.aureus and P.aeruginosa.The clove was more potent toward S.aureus with the MIC of 0.45 g/mL.P.aeruginosa was more sensitive to clove compared to garlic.For S.aureus,it was more sensitive to garlic compared to clove. Conclusion:The antibacterial activity of garlic and clove crude extracts shown in our study further confirm these natural plants'potential usage in therapeutic use for oral diseases or infections.This could be the platform for the interested party to do research and development on it and to produce oral health products which are more affordable for lower economic income groups and with fewer side effects as seen in synthetic drug.

  20. Strategies for the discovery of new natural products by genome mining.

    Science.gov (United States)

    Zerikly, Malek; Challis, Gregory L

    2009-03-02

    Natural products have a very broad spectrum of applications. Many natural products are used clinically as antibacterial, antifungal, antiparasitic, anticancer and immunosuppressive agents and are therefore of utmost importance for our society. When in the 1940s the golden age of antibiotics was ushered in, a "gold rush fever" of natural product discovery in the pharmaceutical industry ensued for many decades. However, the traditional process of discovering new bioactive natural products is generally long and laborious, and known natural products are frequently rediscovered. A mass-withdrawal of pharmaceutical companies from new natural product discovery and natural products research has thus occurred in recent years. In this article, the concept of genome mining for novel natural product discovery, which promises to provide a myriad of new bioactive natural compounds, is summarized and discussed. Genome mining for new natural product discovery exploits the huge and constantly increasing quantity of DNA sequence data from a wide variety of organisms that is accumulating in publicly accessible databases. Genes encoding enzymes likely to be involved in natural product biosynthesis can be readily located in sequenced genomes by use of computational sequence comparison tools. This information can be exploited in a variety of ways in the search for new bioactive natural products.

  1. Cactus pear: a natural product in cancer chemoprevention

    Directory of Open Access Journals (Sweden)

    Wang Jian

    2005-09-01

    Full Text Available Abstract Background Cancer chemoprevention is a new approach in cancer prevention, in which chemical agents are used to prevent cancer in normal and/or high-risk populations. Although chemoprevention has shown promise in some epithelial cancers, currently available preventive agents are limited and the agents are costly, generally with side effects. Natural products, such as grape seed, green tea, and certain herbs have demonstrated anti-cancer effects. To find a natural product that can be used in chemoprevention of cancer, we tested Arizona cactus fruit solution, the aqueous extracts of cactus pear, for its anti-cancer effects in cultured cells and in an animal model. Method Aqueous extracts of cactus pear were used to treat immortalized ovarian and cervical epithelial cells, as well as ovarian, cervical, and bladder cancer cells. Aqueous extracts of cactus pear were used at six concentrations (0, 0.5, 1, 5, 10 or 25% to treat cells for 1, 3, or 5 days. Growth inhibition, apoptosis induction, and cell cycle changes were analyzed in the cultured cells; the suppression of tumor growth in nude mice was evaluated and compared with the effect of a synthetic retinoid N-(4-hydroxyphernyl retinamide (4-HPR, which is currently used as a chemoprevention agent. Immunohistochemistry staining of tissue samples from animal tumors was performed to examine the gene expression. Results Cells exposed to cactus pear extracts had a significant increase in apoptosis and growth inhibition in both immortalized epithelial cells and cancer cells in a dose- and time-dependent manner. It also affected cell cycle of cancer cells by increasing G1 and decreasing G2 and S phases. Both 4-HPR and cactus pear extracts significantly suppressed tumor growth in nude mice, increased annexin IV expression, and decreased VEGF expression. Conclusion Arizona cactus pear extracts effectively inhibited cell growth in several different immortalized and cancer cell cultures, suppressed

  2. Cactus pear: a natural product in cancer chemoprevention.

    Science.gov (United States)

    Zou, Da-ming; Brewer, Molly; Garcia, Francisco; Feugang, Jean M; Wang, Jian; Zang, Roungyu; Liu, Huaguang; Zou, Changping

    2005-09-08

    Cancer chemoprevention is a new approach in cancer prevention, in which chemical agents are used to prevent cancer in normal and/or high-risk populations. Although chemoprevention has shown promise in some epithelial cancers, currently available preventive agents are limited and the agents are costly, generally with side effects. Natural products, such as grape seed, green tea, and certain herbs have demonstrated anti-cancer effects. To find a natural product that can be used in chemoprevention of cancer, we tested Arizona cactus fruit solution, the aqueous extracts of cactus pear, for its anti-cancer effects in cultured cells and in an animal model. Aqueous extracts of cactus pear were used to treat immortalized ovarian and cervical epithelial cells, as well as ovarian, cervical, and bladder cancer cells. Aqueous extracts of cactus pear were used at six concentrations (0, 0.5, 1, 5, 10 or 25%) to treat cells for 1, 3, or 5 days. Growth inhibition, apoptosis induction, and cell cycle changes were analyzed in the cultured cells; the suppression of tumor growth in nude mice was evaluated and compared with the effect of a synthetic retinoid N-(4-hydroxyphernyl) retinamide (4-HPR), which is currently used as a chemoprevention agent. Immunohistochemistry staining of tissue samples from animal tumors was performed to examine the gene expression. Cells exposed to cactus pear extracts had a significant increase in apoptosis and growth inhibition in both immortalized epithelial cells and cancer cells in a dose- and time-dependent manner. It also affected cell cycle of cancer cells by increasing G1 and decreasing G2 and S phases. Both 4-HPR and cactus pear extracts significantly suppressed tumor growth in nude mice, increased annexin IV expression, and decreased VEGF expression. Arizona cactus pear extracts effectively inhibited cell growth in several different immortalized and cancer cell cultures, suppressed tumor growth in nude mice, and modulated expression of tumor

  3. Effects of bioenergy production on European nature conservation options

    Science.gov (United States)

    Schleupner, C.; Schneider, U. A.

    2009-04-01

    To increase security of energy supply and reduce greenhouse gas (GHG) emissions the European Commission set out a long-term strategy for renewable energy in the European Union (EU). Bioenergy from forestry and agriculture plays a key role for both. Since the last decade a significant increase of biomass energy plantations has been observed in Europe. Concurrently, the EU agreed to halt the loss of biodiversity within its member states. One measure is the Natura2000 network of important nature sites that actually covers about 20% of the EU land surface. However, to fulfil the biodiversity target more nature conservation and restoration sites need to be designated. There are arising concerns that an increased cultivation of bioenergy crops will decrease the land available for nature reserves and for "traditional" agriculture and forestry. In the following the economic and ecological impacts of structural land use changes are demonstrated by two examples. First, a case study of land use changes on the Eiderstedt peninsula in Schleswig-Holstein/Germany evaluates the impacts of grassland conversion into bioenergy plantations under consideration of selected meadow birds. Scenarios indicate not only a quantitative loss of habitats but also a reduction of habitat quality. The second study assesses the role of bioenergy production in light of possible negative impacts on potential wetland conservation sites in Europe. By coupling the spatial wetland distribution model "SWEDI" (cf. SCHLEUPNER 2007) to the European Forest and Agricultural Sector Optimization Model (EUFASOM; cf. SCHNEIDER ET AL. 2008) economic and environmental aspects of land use are evaluated simultaneously. This way the costs and benefits of the appropriate measures and its consequences for agriculture and forestry are investigated. One aim is to find the socially optimal balance between alternative wetland uses by integrating biological benefits - in this case wetlands - and economic opportunities - here

  4. A systematic review of natural health product treatment for vitiligo

    Directory of Open Access Journals (Sweden)

    Boon Heather S

    2008-05-01

    Full Text Available Abstract Background Vitiligo is a hypopigmentation disorder affecting 1 to 4% of the world population. Fifty percent of cases appear before the age of 20 years old, and the disfigurement results in psychiatric morbidity in 16 to 35% of those affected. Methods Our objective was to complete a comprehensive, systematic review of the published scientific literature to identify natural health products (NHP such as vitamins, herbs and other supplements that may have efficacy in the treatment of vitiligo. We searched eight databases including MEDLINE and EMBASE for vitiligo, leucoderma, and various NHP terms. Prospective controlled clinical human trials were identified and assessed for quality. Results Fifteen clinical trials were identified, and organized into four categories based on the NHP used for treatment. 1 L-phenylalanine monotherapy was assessed in one trial, and as an adjuvant to phototherapy in three trials. All reported beneficial effects. 2 Three clinical trials utilized different traditional Chinese medicine products. Although each traditional Chinese medicine trial reported benefit in the active groups, the quality of the trials was poor. 3 Six trials investigated the use of plants in the treatment of vitiligo, four using plants as photosensitizing agents. The studies provide weak evidence that photosensitizing plants can be effective in conjunction with phototherapy, and moderate evidence that Ginkgo biloba monotherapy can be useful for vitiligo. 4 Two clinical trials investigated the use of vitamins in the therapy of vitiligo. One tested oral cobalamin with folic acid, and found no significant improvement over control. Another trial combined vitamin E with phototherapy and reported significantly better repigmentation over phototherapy only. It was not possible to pool the data from any studies for meta-analytic purposes due to the wide difference in outcome measures and poor quality ofreporting. Conclusion Reports investigating the

  5. Natural products from resurrection plants: potential for medical applications.

    Science.gov (United States)

    Gechev, Tsanko S; Hille, Jacques; Woerdenbag, Herman J; Benina, Maria; Mehterov, Nikolay; Toneva, Valentina; Fernie, Alisdair R; Mueller-Roeber, Bernd

    2014-11-01

    Resurrection species are a group of land plants that can tolerate extreme desiccation of their vegetative tissues during harsh drought stress, and still quickly - often within hours - regain normal physiological and metabolic functions following rehydration. At the molecular level, this desiccation tolerance is attributed to basal cellular mechanisms including the constitutive expression of stress-associated genes and high levels of protective metabolites present already in the absence of stress, as well as to transcriptome and metabolome reconfigurations rapidly occurring during the initial phases of drought stress. Parts of this response are conferred by unique metabolites, including a diverse array of sugars, phenolic compounds, and polyols, some of which accumulate to high concentrations within the plant cell. In addition to drought stress, these metabolites are proposed to contribute to the protection against other abiotic stresses and to an increased oxidative stress tolerance. Recently, extracts of resurrection species and particular secondary metabolites therein were reported to display biological activities of importance to medicine, with e.g. antibacterial, anticancer, antifungal, and antiviral activities, rendering them possible candidates for the development of novel drug substances as well as for cosmetics. Herein, we provide an overview of the metabolite composition of resurrection species, summarize the latest reports related to the use of natural products from resurrection plants, and outline their potential for medical applications.

  6. Natural Products as Leads in Schistosome Drug Discovery

    Directory of Open Access Journals (Sweden)

    Bruno J. Neves

    2015-01-01

    Full Text Available Schistosomiasis is a neglected parasitic tropical disease that claims around 200,000 human lives every year. Praziquantel (PZQ, the only drug recommended by the World Health Organization for the treatment and control of human schistosomiasis, is now facing the threat of drug resistance, indicating the urgent need for new effective compounds to treat this disease. Therefore, globally, there is renewed interest in natural products (NPs as a starting point for drug discovery and development for schistosomiasis. Recent advances in genomics, proteomics, bioinformatics, and cheminformatics have brought about unprecedented opportunities for the rapid and more cost-effective discovery of new bioactive compounds against neglected tropical diseases. This review highlights the main contributions that NP drug discovery and development have made in the treatment of schistosomiasis and it discusses how integration with virtual screening (VS strategies may contribute to accelerating the development of new schistosomidal leads, especially through the identification of unexplored, biologically active chemical scaffolds and structural optimization of NPs with previously established activity.

  7. New Positioning Products and Pilot Service for Natural Hazard Monitorin

    Science.gov (United States)

    Bar-Sever, Y. E.; Miller, K. J.; Miller, M. A.; Khachikyan, R.; Meyer, R. F.; Vallisneri, M.; Liu, Z.; Song, Y. T.

    2015-12-01

    We describe a new pilot service from JPL's Global Differential GPS (GDGPS) System that provides positioning solutions for hundreds of GNSS tracking sites, from both global and regional networks, aiming to monitor ground motion in the immediate aftermath of earthquakes. The new service provides site position time series solutions at 1 Hz, based on GNSS tracking data. Recognizing the tradeoff between latency and accuracy, the solutions are provided at multiple latencies, ranging from one second to one hour. Individual site solution accuracy strongly depends on the local tracking data. The median site position accuracies ranges from ~one cm 1DRMs for the to most latent solution to ~five cm 1DRMS for the one-second solutions. We discuss the tradeoff between accuracy and latency and explain the choice of product latencies in terms of this trade and in terms of the benefits to agencies responsible for issuing alarms and managing natural disasters. We describe and demonstrate a simple user algorithm to seamlessly merge the disparate latent solutions into a single, optimal record of site motion. The positioning service is integrated with automated earthquake notices from the USGS to support calculations of co-seismic displacements. Finally we describe the current scope of the pilot project, its innovative user-interface, and our ultimate plans to serve all real-time GNSS sites.

  8. Identification and quantification of the halogenated natural product BC-3

    Energy Technology Data Exchange (ETDEWEB)

    Melcher, J.; Olbrich, D.; Vetter, W. [Hohenheim Univ., Stuttgart (Germany). Inst. fuer Lebensmittelchemie; Marsh, G. [Stockholm Univ. (Sweden). Dept. of Environmental Chemistry; Gaus, C.; Mueller, J.F. [National Research Centre for Environmental Toxicology, Coopers Plains (Australia)

    2004-09-15

    Halogenated natural products (HNPs) of marine origin are increasingly recognized as critical residues in foodstuff (e. g. fish) and environmental samples (e. g. marine mammals and birds). Some of these HNPs (Q1, MHC-1, BC-2, and HDBPs including BC-10) were detected in diverse fish and marine mammal samples at concentrations sometimes exceeding those of PCBs, DDT, and other anthropogenic pollutants. Recent studies with marine mammal samples from Australia led to the detection of six abundant HNPs (Q1, BC-1, BC-2, BC-3, BC-10, and BC-11). In the meantime, Q1 was identified as heptachloro-1{sup '}-methyl-1,2{sup '}-bipyrrole, BC-2 as 4,6-dibromo-2-(2{sup '},4{sup '}-dibromo)phenoxyanisole, BC- 10 as 1,1{sup '}-dimethyl-3,3{sup '},4,4{sup '}-tetrabromo-5,5{sup '}-dichloro-2,2{sup '}-bipyrrole, and BC-11 as 3,5-dibromo- 2-(3{sup '},5{sup '}-dibromo,2{sup '}-methoxy)phenoxyanisole. However the identity of BC-1 and BC-3 remained unclear. The goal of the present study was the identification of BC-3. The tetrabromo compound BC-3 has previously been detected in marine mammals from four continents. Furthermore, we attempted establishing quantitative concentrations in diverse marine biota samples.

  9. Plants’ Natural Products as Alternative Promising Anti-Candida Drugs

    Science.gov (United States)

    Soliman, Sameh; Alnajdy, Dina; El-Keblawy, Ali A.; Mosa, Kareem A.; Khoder, Ghalia; Noreddin, Ayman M.

    2017-01-01

    Candida is a serious life-threatening pathogen, particularly with immunocompromised patients. Candida infections are considered as a major cause of morbidity and mortality in a broad range of immunocompromised patients. Candida infections are common in hospitalized patients and elderly people. The difficulty to eradicate Candida infections is owing to its unique switch between yeast and hyphae forms and more likely to biofilm formations that render resistance to antifungal therapy. Plants are known sources of natural medicines. Several plants show significant anti-Candida activities and some of them have lower minimum inhibitory concentration, making them promising candidates for anti-Candida therapy. However, none of these plant products is marketed for anti-Candida therapy because of lack of sufficient information about their efficacy, toxicity, and kinetics. This review revises major plants that have been tested for anti-Candida activities with recommendations for further use of some of these plants for more investigation and in vivo testing including the use of nanostructure lipid system.

  10. Natural Products for the Treatment of Chlamydiaceae Infections

    Directory of Open Access Journals (Sweden)

    Mika A. Brown

    2016-10-01

    Full Text Available Due to the global prevalence of Chlamydiae, exploring studies of diverse antichlamydial compounds is important in the development of effective treatment strategies and global infectious disease management. Chlamydiaceae is the most widely known bacterial family of the Chlamydiae order. Among the species in the family Chlamydiaceae, Chlamydia trachomatis and Chlamydia pneumoniae cause common human diseases, while Chlamydia abortus, Chlamydia psittaci, and Chlamydia suis represent zoonotic threats or are endemic in human food sources. Although chlamydial infections are currently manageable in human populations, chlamydial infections in livestock are endemic and there is significant difficulty achieving effective treatment. To combat the spread of Chlamydiaceae in humans and other hosts, improved methods for treatment and prevention of infection are needed. There exist various studies exploring the potential of natural products for developing new antichlamydial treatment modalities. Polyphenolic compounds can inhibit chlamydial growth by membrane disruption, reestablishment of host cell apoptosis, or improving host immune system detection. Fatty acids, monoglycerides, and lipids can disrupt the cell membranes of infective chlamydial elementary bodies (EBs. Peptides can disrupt the cell membranes of chlamydial EBs, and transferrins can inhibit chlamydial EBs from attachment to and permeation through the membranes of host cells. Cellular metabolites and probiotic bacteria can inhibit chlamydial infection by modulating host immune responses and directly inhibiting chlamydial growth. Finally, early stage clinical trials indicate that polyherbal formulations can be effective in treating chlamydial infections. Herein, we review an important body of literature in the field of antichlamydial research.

  11. Pop-like halogenated natural products in antarctic sponges

    Energy Technology Data Exchange (ETDEWEB)

    Vetter, W. [Hohenheim Univ., Stuttgart (Germany); Janussen, D. [Senckenbergische Naturforschende Gesellschaft (Natur-Museum und Forschungs-Institut), Frankfurt am Main (Germany)

    2004-09-15

    Persistent organic pollutants (POPs) are major contaminants of our days. This group of chemicals comprises a number of halogenated compounds used as pesticides (DDT, lindane, chlordane, toxaphene and others) as well as industrial chemicals (PCBs, PCNs, CPs, and brominated flameretardants). Although the list of known POPs including isomers and metabolites is long, there are frequent reports on the detection of unknown organohalogen compounds in the literature. Recent work demonstrated that some of these unknown peaks in gas chromatograms originate from halogenated natural products (HNPs). Sometimes, HNPs have been found at remarkably high concentrations in marine birds, mammals and fish. Due to the structural similarities with anthropogenic POPs, these substances may possess a potential risk for wildlife and man. HNPs are known to be produced with an overwhelming variety by marine organisms such as algae, sponges, microorganisms and others. In this study we have screened different species of Antarctic sponges on the occurrence of halogenated compounds which may be of environmental concern. Thus, we were only interested in lipophilic and persistent HNPs. Following that, we applied our standard sample clean-up procedure for the analysis of nonpolar POPs. Two steps on deactivated and activated silica yielded compounds with similar polarity as PCBs, chloropesticides and brominated analogues in the sample extracts. Additionally, all samples were treated with concentrated sulphuric acid in order to eliminate labile (non-presistent) HNPs.

  12. An analysis of FDA-approved drugs: natural products and their derivatives.

    Science.gov (United States)

    Patridge, Eric; Gareiss, Peter; Kinch, Michael S; Hoyer, Denton

    2016-02-01

    Natural products contribute greatly to the history and landscape of new molecular entities (NMEs). An assessment of all FDA-approved NMEs reveals that natural products and their derivatives represent over one-third of all NMEs. Nearly one-half of these are derived from mammals, one-quarter from microbes and one-quarter from plants. Since the 1930s, the total fraction of natural products has diminished, whereas semisynthetic and synthetic natural product derivatives have increased. Over time, this fraction has also become enriched with microbial natural products, which represent a significant portion of approved antibiotics, including more than two-thirds of all antibacterial NMEs. In recent years, the declining focus on natural products has impacted the pipeline of NMEs from specific classes, and this trend is likely to continue without specific investment in the pursuit of natural products.

  13. Effective use of heterologous hosts for characterization of biosynthetic enzymes allows production of natural products and promotes new natural product discovery.

    Science.gov (United States)

    Watanabe, Kenji

    2014-01-01

    In the past few years, there has been impressive progress in elucidating the mechanism of biosynthesis of various natural products accomplished through the use of genetic, molecular biological and biochemical techniques. Here, we present a comprehensive overview of the current results from our studies on fungal natural product biosynthetic enzymes, including nonribosomal peptide synthetase and polyketide synthase-nonribosomal peptide synthetase hybrid synthetase, as well as auxiliary enzymes, such as methyltransferases and oxygenases. Specifically, biosynthesis of the following compounds is described in detail: (i) Sch210972, potentially involving a Diels-Alder reaction that may be catalyzed by CghA, a functionally unknown protein identified by targeted gene disruption in the wild type fungus; (ii) chaetoglobosin A, formed via multi-step oxidations catalyzed by three redox enzymes, one flavin-containing monooxygenase and two cytochrome P450 oxygenases as characterized by in vivo biotransformation of relevant intermediates in our engineered Saccharomyces cerevisiae; (iii) (-)-ditryptophenaline, formed by a cytochrome P450, revealing the dimerization mechanism for the biosynthesis of diketopiperazine alkaloids; (iv) pseurotins, whose variations in the C- and O-methylations and the degree of oxidation are introduced combinatorially by multiple redox enzymes; and (v) spirotryprostatins, whose spiro-carbon moiety is formed by a flavin-containing monooxygenase or a cytochrome P450 as determined by heterologous de novo production of the biosynthetic intermediates and final products in Aspergillus niger. We close our discussion by summarizing some of the key techniques that have facilitated the discovery of new natural products, production of their analogs and identification of biosynthetic mechanisms in our study.

  14. Exploiting new approaches for natural product drug discovery in the biotechnology industry.

    Science.gov (United States)

    Gullo, Vincent P; Hughes, Dallas E

    2005-01-01

    In recent years, large pharmaceutical companies have significantly reduced or eliminated the search for new therapeutic agents from natural sources. In spite of the many successes from natural product drug discovery, these companies have chosen to focus on compound libraries as the source of new lead compounds. Smaller biotechnology companies are continuing the search for novel natural products by developing and employing new and innovative approaches. This paper will describe some of these recent approaches to natural product drug discovery.:

  15. Natural Diagonal Riemannian Almost Product and Para-Hermitian Cotangent Bundles

    CERN Document Server

    Druta-Romaniuc, Simona-Luiza

    2011-01-01

    We obtain the natural diagonal almost product and locally product structures on the total space of the cotangent bundle of a Riemannian manifold. We find the Riemannian almost product (locally product) and the (almost) para-Hermitian cotangent bundles of natural diagonal lift type. We prove the characterization theorem for the natural diagonal (almost) para-K\\"ahlerian structures on the total spaces of the cotangent bundle.

  16. Complex marine natural products as potential epigenetic and production regulators of antibiotics from a marine Pseudomonas aeruginosa

    Science.gov (United States)

    Marine microbes are capable of producing secondary metabolites for defense and competition. Factors exerting an impact on secondary metabolite production of microbial communities included bioactive natural products and co-culturing. These external influences may have practical applications such as ...

  17. Natural products for chronic cough: Text mining the East Asian historical literature for future therapeutics.

    Science.gov (United States)

    Shergis, Johannah Linda; Wu, Lei; May, Brian H; Zhang, Anthony Lin; Guo, Xinfeng; Lu, Chuanjian; Xue, Charlie Changli

    2015-08-01

    Chronic cough is a significant health burden. Patients experience variable benefits from over the counter and prescribed products, but there is an unmet need to provide more effective treatments. Natural products have been used to treat cough and some plant compounds such as pseudoephedrine from ephedra and codeine from opium poppy have been developed into drugs. Text mining historical literature may offer new insight for future therapeutic development. We identified natural products used in the East Asian historical literature to treat chronic cough. Evaluation of the historical literature revealed 331 natural products used to treat chronic cough. Products included plants, minerals and animal substances. These natural products were found in 75 different books published between AD 363 and 1911. Of the 331 products, the 10 most frequently and continually used products were examined, taking into consideration findings from contemporary experimental studies. The natural products identified are promising and offer new directions in therapeutic development for treating chronic cough.

  18. Insect-specific production of new GameXPeptides in photorhabdus luminescens TTO1, widespread natural products in entomopathogenic bacteria.

    Science.gov (United States)

    Nollmann, Friederike I; Dauth, Christina; Mulley, Geraldine; Kegler, Carsten; Kaiser, Marcel; Waterfield, Nick R; Bode, Helge B

    2015-01-19

    Discovery of new natural products by heterologous expression reaches its limits, especially when specific building blocks are missing in the heterologous host or the production medium. Here, we describe the insect-specific production of the new GameXPeptides E-H (5-8) from Photorhabdus luminescens TTO1, which can be produced heterologously from expression of the GameXPeptide synthetase GxpS only upon supplementation of the production media with the missing building blocks, and thus must be regarded as the true natural products under natural conditions.

  19. Productivity analysis in nature reserve: A case study in Hunan Province

    Institute of Scientific and Technical Information of China (English)

    Wang Lan-hui; Tian Shu-rong

    2007-01-01

    Although there are abundant natural resources in nature reserves, poverty is a common feature of the social economy in the communities surrounding nature reserves. Income from forestry is still the main source for residents living around nature reserves.The structure of inputs and outputs, i.e. productivity, in the forestry sector in nature reserves is quite different from one reserve to another. Productivity can be measured by Data Envelopment Analysis (DEA) methods owing to the characteristics of DEA. The promotion of productivity in nature reserve is an effective way to improve the living condition in areas neighboring nature reserves.Thus, one typical national nature reserve in Hunan is selected in this study with the intent to measure productivity in the area and then to analyze the factors affecting its productivity.

  20. Discovery of novel drug targets and their functions using phenotypic screening of natural products.

    Science.gov (United States)

    Chang, Junghwa; Kwon, Ho Jeong

    2016-03-01

    Natural products are valuable resources that provide a variety of bioactive compounds and natural pharmacophores in modern drug discovery. Discovery of biologically active natural products and unraveling their target proteins to understand their mode of action have always been critical hurdles for their development into clinical drugs. For effective discovery and development of bioactive natural products into novel therapeutic drugs, comprehensive screening and identification of target proteins are indispensable. In this review, a systematic approach to understanding the mode of action of natural products isolated using phenotypic screening involving chemical proteomics-based target identification is introduced. This review highlights three natural products recently discovered via phenotypic screening, namely glucopiericidin A, ecumicin, and terpestacin, as representative case studies to revisit the pivotal role of natural products as powerful tools in discovering the novel functions and druggability of targets in biological systems and pathological diseases of interest.

  1. Biocombinatorial Engineering of Fungal PKS-NRPS Hybrids for Production of Novel Synthetic Natural Products

    DEFF Research Database (Denmark)

    Nielsen, Maria Lund

    . Secondary metabolites (SMs) from bacteria, plants and filamentous fungi constitute a large group of important natural products. In this thesis I explore the biosynthesis of several fungal SMs along with the enzymes responsible for their synthesis. Specifically, my research focuses on the expression...... and engineering of a certain type of fungal enzymes – natural fusions of polyketide synthases and nonribosomal peptide synthetases (PKS-NRPSs). The thesis is divided into two topics: 1) Expanding fungal chemodiversity through combinatorial biosynthesis 2) Two CRISPR-Cas9-based approaches to linking SMs...... and NRPS modules. In the third study (chapter 4), I describe how CRISPR-Cas9, which was recently implemented for genome editing in filamentous fungi, can be used to link SMs to their genetic origin in a fungus where no genetic tools were previously available. Using CRISPR-Cas9, I identified a novel gene...

  2. Data Resources for the Computer-Guided Discovery of Bioactive Natural Products.

    Science.gov (United States)

    Chen, Ya; de Bruyn Kops, Christina; Kirchmair, Johannes

    2017-08-30

    Natural products from plants, animals, marine life, fungi, bacteria, and other organisms are an important resource for modern drug discovery. Their biological relevance and structural diversity make natural products good starting points for drug design. Natural product-based drug discovery can benefit greatly from computational approaches, which are a valuable precursor or supplementary method to in vitro testing. We present an overview of 25 virtual and 31 physical natural product libraries that are useful for applications in cheminformatics, in particular virtual screening. The overview includes detailed information about each library, the extent of its structural information, and the overlap between different sources of natural products. In terms of chemical structures, there is a large overlap between freely available and commercial virtual natural product libraries. Of particular interest for drug discovery is that at least ten percent of known natural products are readily purchasable and many more natural products and derivatives are available through on-demand sourcing, extraction and synthesis services. Many of the readily purchasable natural products are of small size and hence of relevance to fragment-based drug discovery. There are also an increasing number of macrocyclic natural products and derivatives becoming available for screening.

  3. Ethanol production by recombinant and natural xylose-utilising yeasts

    Energy Technology Data Exchange (ETDEWEB)

    Eliasson, Anna

    2000-07-01

    The xylose-fermenting capacity of recombinant Saccharomyces cerevisiae carrying XYL1 and XYL2 from Pichia stipitis, which encode xylose reductase (XR) and xylitol dehydrogenase (XDH), respectively, is poor due to high xylitol formation. Whereas, P. stipitis exhibits high ethanol yield on xylose, the tolerance towards inhibitors in the lignocellulosic hydrolysate is low. A recombinant strain possessing the advantageous characteristics of both S. cerevisiae and P. stipitis would constitute a biocatalyst capable of efficient ethanol production from lignocellulosic hydrolysate. In the work presented in this thesis, factors influencing xylose fermentation in recombinant S. cerevisiae and in the natural xylose-fermenting yeast P. stipitis have been identified and investigated. Anaerobic xylulose fermentation was compared in strains of Zygosaccharomyces and S. cerevisiae, mutants and wild-type strains to identify host strain background and genetic modifications beneficial for xylose fermentation. The greatest positive effect was found for over-expression of the gene XKS1 for the pentose phosphate pathway (PPP) enzyme xylulokinase (XK), which increased the ethanol yield by almost 85%. The Zygosaccharomyces strains tested formed large amounts of polyols, making them unsuitable as host strains. The XR/XDH/XK ratio was found to determine whether carbon accumulated in a xylitol pool or was further utilised for ethanol production in recombinant xylose-utilising S. cerevisiae. Simulations, based on a kinetic model, and anaerobic xylose cultivation experiments implied that a 1:{>=}10:{>=}4 relation was optimal in minimising xylitol formation. Ethanol formation increased with decreasing XR/XDH ratio, whereas xylitol formation decreased and XK overexpression was necessary for adequate ethanol formation. Based on the knowledge of optimal enzyme ratios, a stable, xylose-utilising strain, S. cerevisiae TMB 3001, was constructed by chromosomal integration of the XYL1 and XYL2 genes

  4. Ethanol production by recombinant and natural xylose-utilising yeasts

    Energy Technology Data Exchange (ETDEWEB)

    Eliasson, Anna

    2000-07-01

    The xylose-fermenting capacity of recombinant Saccharomyces cerevisiae carrying XYL1 and XYL2 from Pichia stipitis, which encode xylose reductase (XR) and xylitol dehydrogenase (XDH), respectively, is poor due to high xylitol formation. Whereas, P. stipitis exhibits high ethanol yield on xylose, the tolerance towards inhibitors in the lignocellulosic hydrolysate is low. A recombinant strain possessing the advantageous characteristics of both S. cerevisiae and P. stipitis would constitute a biocatalyst capable of efficient ethanol production from lignocellulosic hydrolysate. In the work presented in this thesis, factors influencing xylose fermentation in recombinant S. cerevisiae and in the natural xylose-fermenting yeast P. stipitis have been identified and investigated. Anaerobic xylulose fermentation was compared in strains of Zygosaccharomyces and S. cerevisiae, mutants and wild-type strains to identify host strain background and genetic modifications beneficial for xylose fermentation. The greatest positive effect was found for over-expression of the gene XKS1 for the pentose phosphate pathway (PPP) enzyme xylulokinase (XK), which increased the ethanol yield by almost 85%. The Zygosaccharomyces strains tested formed large amounts of polyols, making them unsuitable as host strains. The XR/XDH/XK ratio was found to determine whether carbon accumulated in a xylitol pool or was further utilised for ethanol production in recombinant xylose-utilising S. cerevisiae. Simulations, based on a kinetic model, and anaerobic xylose cultivation experiments implied that a 1:{>=}10:{>=}4 relation was optimal in minimising xylitol formation. Ethanol formation increased with decreasing XR/XDH ratio, whereas xylitol formation decreased and XK overexpression was necessary for adequate ethanol formation. Based on the knowledge of optimal enzyme ratios, a stable, xylose-utilising strain, S. cerevisiae TMB 3001, was constructed by chromosomal integration of the XYL1 and XYL2 genes

  5. On the nature of the new product strategy

    DEFF Research Database (Denmark)

    Larsson, Flemming

    2006-01-01

    The aim of this paper is to explore the concept of a new product strategy and its relation to portfolio management for product development. Based on a literature review this research adheres to one perception of the new product strategy proposed by literature complemented with a component adressing...... the risk-dimension. Next, it is suggested that the new product strategy is embedded in the product development strategy. Subsequently, it is advocated that companies try to achieve a base for realizing integration, synchronization and strategic alignment by means of a new product strategy. These three...

  6. Deposits of naturally occurring radioactivity in production of oil and natural gas; Radioaktive avleiringer i olje- og gassproduksjon

    Energy Technology Data Exchange (ETDEWEB)

    Strand, T.; Lysebo, I.; Kristensen, D.; Birovljev, A.

    1997-01-01

    Deposits of naturally occurring radioactive materials is an increasing problem in Norwegian oil and gas production. Activity concentration in solid-state samples and production water, and doses to workers involved in different operations off-shore, have been measured. The report also includes a discussion of different methods of monitoring and alternatives for final disposal of wastes. 154 refs.

  7. Production of crude oil, natural gas, and gas condensate (in cubic meters). [Argentina]. Produccion de petroleo, gas natural y gasolina natural

    Energy Technology Data Exchange (ETDEWEB)

    1977-01-01

    Statistics on total mineral and petroleum production in Argentina during the year 1977 are presented. Production totals of petroleum, natural gas, and gas condensate are listed by province and by category. The province production records include Chubut, Jujuy, La Pampa, Mendoza, Neuquen, Rio Negro, Salta, Santa Cruz, Territorio Nacional de La Tierra del Fuego, the Antarctic, and islands of the S. Atlantic. Total production amounted to 25,060,908 cu m of petroleum, 11,594,853,909 cu m of natural gas, and 12,351.8 cu m of gas condensates. Information on petroleum sector employment in the years 1968 through 1977 also is provided.

  8. Engineering microbial cell factories for the production of plant natural products: from design principles to industrial-scale production.

    Science.gov (United States)

    Liu, Xiaonan; Ding, Wentao; Jiang, Huifeng

    2017-07-19

    Plant natural products (PNPs) are widely used as pharmaceuticals, nutraceuticals, seasonings, pigments, etc., with a huge commercial value on the global market. However, most of these PNPs are still being extracted from plants. A resource-conserving and environment-friendly synthesis route for PNPs that utilizes microbial cell factories has attracted increasing attention since the 1940s. However, at the present only a handful of PNPs are being produced by microbial cell factories at an industrial scale, and there are still many challenges in their large-scale application. One of the challenges is that most biosynthetic pathways of PNPs are still unknown, which largely limits the number of candidate PNPs for heterologous microbial production. Another challenge is that the metabolic fluxes toward the target products in microbial hosts are often hindered by poor precursor supply, low catalytic activity of enzymes and obstructed product transport. Consequently, despite intensive studies on the metabolic engineering of microbial hosts, the fermentation costs of most heterologously produced PNPs are still too high for industrial-scale production. In this paper, we review several aspects of PNP production in microbial cell factories, including important design principles and recent progress in pathway mining and metabolic engineering. In addition, implemented cases of industrial-scale production of PNPs in microbial cell factories are also highlighted.

  9. Pilot Scale Production of Irradiated Natural Rubber Latex and its Dipping Products

    Directory of Open Access Journals (Sweden)

    M. Utama

    2005-07-01

    Full Text Available One hundred and fifty kg natural rubber latex (NRL before and after concentration were added with 3 phr (part hundred ratio of rubber normal butyl acrylate, then the mixture were irradiated at 25 kGy by gamma rays of 60Co in pilot scale. The irradiated natural rubber latex (INRL were then being to use for producing rubber products such as condom, surgical gloves, and spygmomanometer in factory scale. The quality of INRL and rubber products such as : total solid content (TSC, dry rubber content (DRC, KOH, VFA and MST number, tensile strength, modulus, elongation at break, extractable protein content, and response against Type I allergy etc. were evaluated. The economic aspect for producing INRL by means of Gamma Irradiator (GI and Electron Beam Machine (EBM such as payback period (PP, net present value (NPV and internal rate return (IRR were calculated. The results showed that the latex properties of INRL such as DRC, TSC, KOH, VFA, and MST number are not only found to the requirement of the ISO 2004 standard but also the latex has low protein, lipid, and carbohydrate content. The physical and mechanical properties (tensile strength, modulus, and elongation at break of rubber dipping products such as condom, gloves, and sphygmomanometer are not only found to the requirement of ISO 4074, ISO 10282, and ANSI/AAMI SP-1994 standards, but also the allergic response tested clinical latex-sensitive protein allergen by ELISA test on gloves, and by SPT test on condom are found to be negative. It indicates that production of INRL or PVNRL or RVNRL by EBM 250 keV/10 mA, was more cheap than by using gamma γ irradiator 200 kCi, or sulfur vulcanization. The value of PBP (payback period was 2,1 years, NPV (net present value was 4,250 US $, PI (profitability index 1,06 and IRR (internal rate of returns was 25,0%.

  10. The re-emergence of natural products for drug discovery in the genomics era.

    Science.gov (United States)

    Harvey, Alan L; Edrada-Ebel, RuAngelie; Quinn, Ronald J

    2015-02-01

    Natural products have been a rich source of compounds for drug discovery. However, their use has diminished in the past two decades, in part because of technical barriers to screening natural products in high-throughput assays against molecular targets. Here, we review strategies for natural product screening that harness the recent technical advances that have reduced these barriers. We also assess the use of genomic and metabolomic approaches to augment traditional methods of studying natural products, and highlight recent examples of natural products in antimicrobial drug discovery and as inhibitors of protein-protein interactions. The growing appreciation of functional assays and phenotypic screens may further contribute to a revival of interest in natural products for drug discovery.

  11. New natural antioxidants for protecting omega-3 rich products

    DEFF Research Database (Denmark)

    Farvin, Sabeena; Jacobsen, Charlotte

    2012-01-01

    to oxidation because of their unsaturated nature. Addition of antioxidants is one method. to prevent lipid oxidation. As synthetic antioxidants may have carcinogenic effects at higher levels, the replacement of synthetic antioxidants with natural antioxidants is now in demand. We have isolated natural...... antioxidants from yoghurt, potato peel, fish protein hydrolysates and seaweed, which were able to protect highly unsaturated fish oil from oxidation. These antioxidant extracts may have potential for commercial exploitation. Copyright © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim....

  12. Natural products as tools for studies of ligand-gated ion channels

    DEFF Research Database (Denmark)

    Strømgaard, Kristian

    2005-01-01

    in the brain. Historically, natural products have been used extensively in biomedical studies and ultimately as drugs or leads for drug design. In studies of ligand-gated ion channels, natural products have been essential for the understanding of their structure and function. In the following a short survey...... of natural products and their use in studies of ligand-gated ion channels is given....

  13. Textbook for nature entrepreneurship : product of the WURKS project Nature Entrepreneurship and Tourism within Green Education (NatureToGo)

    NARCIS (Netherlands)

    Felder, M.; Pellis, A.

    2013-01-01

    In recent years, government funding for nature conservation and development has declined. As a result, links between nature conservation and entrepreneurship are increasingly being made in both practice and education. This comes with many questions and challenges. In Green Secondary Vocational

  14. Textbook for nature entrepreneurship : product of the WURKS project Nature Entrepreneurship and Tourism within Green Education (NatureToGo)

    NARCIS (Netherlands)

    Felder, M.; Pellis, A.

    2013-01-01

    In recent years, government funding for nature conservation and development has declined. As a result, links between nature conservation and entrepreneurship are increasingly being made in both practice and education. This comes with many questions and challenges. In Green Secondary Vocational Educa

  15. Pharmacognosy: Science of natural products in drug discovery

    Directory of Open Access Journals (Sweden)

    Ilkay Erdogan Orhan

    2014-09-01

    Full Text Available Pharmacognosy deals with the natural drugs obtained fromorganisms such as most plants, microbes, and animals. Up todate, many important drugs including morphine, atropine,galanthamine, etc. have originated from natural sources whichcontinue to be good model molecules in drug discovery.Traditional medicine is also a part of pharmacognosy and mostof the third world countries still depend on the use of herbalmedicines. Consequently, pharmacognosy always keeps itspopularity in pharmaceutical sciences and plays a critical role indrug discovery.

  16. Pharmacognosy: Science of natural products in drug discovery.

    Science.gov (United States)

    Orhan, Ilkay Erdogan

    2014-01-01

    Pharmacognosy deals with the natural drugs obtained from organisms such as most plants, microbes, and animals. Up to date, many important drugs including morphine, atropine, galanthamine, etc. have originated from natural sources which continue to be good model molecules in drug discovery. Traditional medicine is also a part of pharmacognosy and most of the third world countries still depend on the use of herbal medicines. Consequently, pharmacognosy always keeps its popularity in pharmaceutical sciences and plays a critical role in drug discovery.

  17. Informatic search strategies to discover analogues and variants of natural product archetypes.

    Science.gov (United States)

    Johnston, Chad W; Connaty, Alex D; Skinnider, Michael A; Li, Yong; Grunwald, Alyssa; Wyatt, Morgan A; Kerr, Russell G; Magarvey, Nathan A

    2016-03-01

    Natural products are a crucial source of antimicrobial agents, but reliance on low-resolution bioactivity-guided approaches has led to diminishing interest in discovery programmes. Here, we demonstrate that two in-house automated informatic platforms can be used to target classes of biologically active natural products, specifically, peptaibols. We demonstrate that mass spectrometry-based informatic approaches can be used to detect natural products with high sensitivity, identifying desired agents present in complex microbial extracts. Using our specialised software packages, we could elaborate specific branches of chemical space, uncovering new variants of trichopolyn and demonstrating a way forward in mining natural products as a valuable source of potential pharmaceutical agents.

  18. Synthesis of four diastereomers of sclerophytin F and structural reassignment of several sclerophytin natural products.

    Science.gov (United States)

    Clark, J Stephen; Delion, Laëtitia; Farrugia, Louis J

    2015-03-16

    Synthesis of the triol that has been proposed to be the marine natural product sclerophytin F has been completed along with the syntheses of three diastereomers. Comparison of the NMR spectroscopic data for all four compounds to the data reported for the natural product reveals that sclerophytin F is not the 3S diastereomer of sclerophytin A as proposed by Friedrich and Paquette. Re-analysis of the NMR spectroscopic data for known sclerophytin natural products and synthetic analogues leads to the conclusion that sclerophytins E and F are the same compound. This finding has allowed structural reassignment of several other cladiellin natural products.

  19. Advances in identification and validation of protein targets of natural products without chemical modification.

    Science.gov (United States)

    Chang, J; Kim, Y; Kwon, H J

    2016-05-04

    Covering: up to February 2016Identification of the target proteins of natural products is pivotal to understanding the mechanisms of action to develop natural products for use as molecular probes and potential therapeutic drugs. Affinity chromatography of immobilized natural products has been conventionally used to identify target proteins, and has yielded good results. However, this method has limitations, in that labeling or tagging for immobilization and affinity purification often result in reduced or altered activity of the natural product. New strategies have recently been developed and applied to identify the target proteins of natural products and synthetic small molecules without chemical modification of the natural product. These direct and indirect methods for target identification of label-free natural products include drug affinity responsive target stability (DARTS), stability of proteins from rates of oxidation (SPROX), cellular thermal shift assay (CETSA), thermal proteome profiling (TPP), and bioinformatics-based analysis of connectivity. This review focuses on and reports case studies of the latest advances in target protein identification methods for label-free natural products. The integration of newly developed technologies will provide new insights and highlight the value of natural products for use as biological probes and new drug candidates.

  20. Invariant tensors related with natural connections for a class Riemannian product manifolds

    OpenAIRE

    Gribacheva, Dobrinka

    2012-01-01

    Some invariant tensors in two Naveira classes of Riemannian product manifolds are considered. These tensors are related with natural connections, i.e. linear connections preserving the Riemannian metric and the product structure.

  1. Assessment of natural resources and the policy of subsidies in grain production

    Institute of Scientific and Technical Information of China (English)

    Bai Wei; Hao Jinmin; Zhang Qiuping

    2006-01-01

    Based on the analysis on the status quo of natural resources input in grain production and on the policy of grain subsidies, this paper puts forward a new idea - establishing grain subsidies through assessing the value of the natural resources in grain production. The assessment of the natural resources in grain production provides rationale and reference standard for the policy of grain subsidies, which will promote the sustainable use of natural resources accordingly. This paper concludes: (1) it is necessary for the grain subsidies to assess the full value of natural resources,including economic value, ecological value and social value; (2) the government should give farmers direct subsidies or environment subsidies according to the economic and ecological value of natural resources in grain production; (3) the social value of natural resources can be realized by establishing the country social security system, taking the social value as the criterion for the payment for part of farmers insurance.

  2. The chemistry and biology of guanidine natural products.

    Science.gov (United States)

    Berlinck, Roberto G S; Romminger, Stelamar

    2016-03-01

    The present review discusses the isolation, structure determination, synthesis, biosynthesis and biological activities of secondary metabolites bearing a guanidine group. Topics include non-ribosomal peptides, alkaloids, guanidine-bearing terpenes, polyketides and shikimic acid derivatives from natural sources. A critical analysis of some yet underdeveloped aspects of guanidine metabolites is also presented.

  3. Exploring application of cardanol from natural resource: Chemistry and products

    Science.gov (United States)

    Cardanol (cashew nut shell liquid, CNSL) is a renewable raw material derived from a byproduct of the cashew nut processing industry. First, two natural plasticizers derived from cardanol, cardanol acetate (CA) and epoxidated cardanol acetate (ECA), have been synthesized and characterized by 1HNMR an...

  4. China Keeps Strong Growth Momentum for Natural Gas Production

    Institute of Scientific and Technical Information of China (English)

    Zheng Benxiang; Yu Lingli; Song Chengli

    2009-01-01

    @@ Based on the prediction made by the China Petroleum and Chemical Industry Association (CPCIA),China aims to double its annual natural gas output to 160 billion cubic meters by 2015,and produce about 6 billion tons of oil in the next 30 years,or 200 million tons a year.

  5. Natural Gas and Cellulosic Biomass: A Clean Fuel Combination? Determining the Natural Gas Blending Wall in Biofuel Production.

    Science.gov (United States)

    M Wright, Mark; Seifkar, Navid; Green, William H; Román-Leshkov, Yuriy

    2015-07-07

    Natural gas has the potential to increase the biofuel production output by combining gas- and biomass-to-liquids (GBTL) processes followed by naphtha and diesel fuel synthesis via Fischer-Tropsch (FT). This study reflects on the use of commercial-ready configurations of GBTL technologies and the environmental impact of enhancing biofuels with natural gas. The autothermal and steam-methane reforming processes for natural gas conversion and the gasification of biomass for FT fuel synthesis are modeled to estimate system well-to-wheel emissions and compare them to limits established by U.S. renewable fuel mandates. We show that natural gas can enhance FT biofuel production by reducing the need for water-gas shift (WGS) of biomass-derived syngas to achieve appropriate H2/CO ratios. Specifically, fuel yields are increased from less than 60 gallons per ton to over 100 gallons per ton with increasing natural gas input. However, GBTL facilities would need to limit natural gas use to less than 19.1% on a LHV energy basis (7.83 wt %) to avoid exceeding the emissions limits established by the Renewable Fuels Standard (RFS2) for clean, advanced biofuels. This effectively constitutes a blending limit that constrains the use of natural gas for enhancing the biomass-to-liquids (BTL) process.

  6. Survey of marine natural product structure revisions: a synergy of spectroscopy and chemical synthesis.

    Science.gov (United States)

    Suyama, Takashi L; Gerwick, William H; McPhail, Kerry L

    2011-11-15

    The structural assignment of new natural product molecules supports research in a multitude of disciplines that may lead to new therapeutic agents and or new understanding of disease biology. However, reports of numerous structural revisions, even of recently elucidated natural products, inspired the present survey of techniques used in structural misassignments and subsequent revisions in the context of constitutional or configurational errors. Given the comparatively recent development of marine natural products chemistry, coincident with modern spectroscopy, it is of interest to consider the relative roles of spectroscopy and chemical synthesis in the structure elucidation and revision of those marine natural products that were initially misassigned. Thus, a tabulated review of all marine natural product structural revisions from 2005 to 2010 is organized according to structural motif revised. Misassignments of constitution are more frequent than perhaps anticipated by reliance on HMBC and other advanced NMR experiments, especially when considering the full complement of all natural products. However, these techniques also feature prominently in structural revisions, specifically of marine natural products. Nevertheless, as is the case for revision of relative and absolute configuration, total synthesis is a proven partner for marine, as well as terrestrial, natural products structure elucidation. It also becomes apparent that considerable 'detective work' remains in structure elucidation, in spite of the spectacular advances in spectroscopic techniques.

  7. 2013-2014 Production of guayule natural rubber in Arizona, U.S.A.

    Science.gov (United States)

    Natural rubber is a unique biopolymer whose physical properties cannot be replicated in synthetic alternatives; therefore, it is required for production of tires (passenger, truck, and aircraft) and thousands of consumer and medical products. While demand for natural rubber is expected to increase ...

  8. Direct Capture Technologies for Genomics-Guided Discovery of Natural Products.

    Science.gov (United States)

    Chan, Andrew N; Santa Maria, Kevin C; Li, Bo

    2016-01-01

    Microbes are important producers of natural products, which have played key roles in understanding biology and treating disease. However, the full potential of microbes to produce natural products has yet to be realized; the overwhelming majority of natural product gene clusters encoded in microbial genomes remain "cryptic", and have not been expressed or characterized. In contrast to the fast-growing number of genomic sequences and bioinformatic tools, methods to connect these genes to natural product molecules are still limited, creating a bottleneck in genome-mining efforts to discover novel natural products. Here we review developing technologies that leverage the power of homologous recombination to directly capture natural product gene clusters and express them in model hosts for isolation and structural characterization. Although direct capture is still in its early stages of development, it has been successfully utilized in several different classes of natural products. These early successes will be reviewed, and the methods will be compared and contrasted with existing traditional technologies. Lastly, we will discuss the opportunities for the development of direct capture in other organisms, and possibilities to integrate direct capture with emerging genome-editing techniques to accelerate future study of natural products.

  9. Molecular scaffold analysis of natural products databases in the public domain.

    Science.gov (United States)

    Yongye, Austin B; Waddell, Jacob; Medina-Franco, José L

    2012-11-01

    Natural products represent important sources of bioactive compounds in drug discovery efforts. In this work, we compiled five natural products databases available in the public domain and performed a comprehensive chemoinformatic analysis focused on the content and diversity of the scaffolds with an overview of the diversity based on molecular fingerprints. The natural products databases were compared with each other and with a set of molecules obtained from in-house combinatorial libraries, and with a general screening commercial library. It was found that publicly available natural products databases have different scaffold diversity. In contrast to the common concept that larger libraries have the largest scaffold diversity, the largest natural products collection analyzed in this work was not the most diverse. The general screening library showed, overall, the highest scaffold diversity. However, considering the most frequent scaffolds, the general reference library was the least diverse. In general, natural products databases in the public domain showed low molecule overlap. In addition to benzene and acyclic compounds, flavones, coumarins, and flavanones were identified as the most frequent molecular scaffolds across the different natural products collections. The results of this work have direct implications in the computational and experimental screening of natural product databases for drug discovery.

  10. Prediction of cancer cell sensitivity to natural products based on genomic and chemical properties.

    Science.gov (United States)

    Yue, Zhenyu; Zhang, Wenna; Lu, Yongming; Yang, Qiaoyue; Ding, Qiuying; Xia, Junfeng; Chen, Yan

    2015-01-01

    Natural products play a significant role in cancer chemotherapy. They are likely to provide many lead structures, which can be used as templates for the construction of novel drugs with enhanced antitumor activity. Traditional research approaches studied structure-activity relationship of natural products and obtained key structural properties, such as chemical bond or group, with the purpose of ascertaining their effect on a single cell line or a single tissue type. Here, for the first time, we develop a machine learning method to comprehensively predict natural products responses against a panel of cancer cell lines based on both the gene expression and the chemical properties of natural products. The results on two datasets, training set and independent test set, show that this proposed method yields significantly better prediction accuracy. In addition, we also demonstrate the predictive power of our proposed method by modeling the cancer cell sensitivity to two natural products, Curcumin and Resveratrol, which indicate that our method can effectively predict the response of cancer cell lines to these two natural products. Taken together, the method will facilitate the identification of natural products as cancer therapies and the development of precision medicine by linking the features of patient genomes to natural product sensitivity.

  11. Biosynthesis of natural products in plants by fungal endophytes with an emphasis on swainsonine

    Science.gov (United States)

    Plant natural products are frequently used as chemotaxonomic markers which are indicative of select members of a family, genus, and/or species. However, the erratic occurrence of some natural products raises questions about their biosynthetic origin and significance as chemotaxonomic markers. Rece...

  12. Evaluation of natural products as potential agrochemical agents with insecticide, fungicide and herbicide activities

    CSIR Research Space (South Africa)

    Dumontet, V

    2012-07-01

    Full Text Available The International Congress on Natural Products Research, New York City, 28 July - 1 August 2012 Evaluation of natural products as potential agrochemical agents with insecticide, fungicide and herbicide activities V Dumontet 1, M Litaudon 1, F Olivon 1, C...

  13. Prediction of cancer cell sensitivity to natural products based on genomic and chemical properties

    Directory of Open Access Journals (Sweden)

    Zhenyu Yue

    2015-11-01

    Full Text Available Natural products play a significant role in cancer chemotherapy. They are likely to provide many lead structures, which can be used as templates for the construction of novel drugs with enhanced antitumor activity. Traditional research approaches studied structure-activity relationship of natural products and obtained key structural properties, such as chemical bond or group, with the purpose of ascertaining their effect on a single cell line or a single tissue type. Here, for the first time, we develop a machine learning method to comprehensively predict natural products responses against a panel of cancer cell lines based on both the gene expression and the chemical properties of natural products. The results on two datasets, training set and independent test set, show that this proposed method yields significantly better prediction accuracy. In addition, we also demonstrate the predictive power of our proposed method by modeling the cancer cell sensitivity to two natural products, Curcumin and Resveratrol, which indicate that our method can effectively predict the response of cancer cell lines to these two natural products. Taken together, the method will facilitate the identification of natural products as cancer therapies and the development of precision medicine by linking the features of patient genomes to natural product sensitivity.

  14. Functional Reconstitution of a Fungal Natural Product Gene Cluster by Advanced Genome Editing

    DEFF Research Database (Denmark)

    Weber, Jakob; Valiante, Vito; Nødvig, Christina Spuur

    2017-01-01

    Filamentous fungi produce varieties of natural products even in a strain dependent manner. However, the genetic basis of chemical speciation between strains is still widely unknown. One example is trypacidin, a natural product of the opportunistic human pathogen Aspergillus fumigatus, which...... for advanced molecular genetic studies in filamentous fungi, exploiting selectable markers separated from the edited locus....

  15. Application of natural and synthetic polymers in a production of paper

    Directory of Open Access Journals (Sweden)

    Jovanović Slobodan

    2007-01-01

    Full Text Available This work gives the review of most frequently used natural and synthetic polymers in production of paper, board and cardboard. Physical and chemical interaction of natural and synthetic polymers with cellulose fibers, and thus the way these polymers influence the improvement of both production process and the paper characteristics, have been presented.

  16. ON JUSTIFICATION OF STANDARDS FOR NATURAL RADIONUCLIDE CONCENTRATION IN FACING PRODUCTS AND MATERIALS

    Directory of Open Access Journals (Sweden)

    I. P. Stamat

    2009-01-01

    Full Text Available The article addresses issues of the population radiation protection regulatory framework development for the natural sources of radiation. Calculations for justification of standard for natural radionuclide concentration in the wide range of contemporary building materials - facing products - are formulated. The basic consideration of calculations is that implementation of these products could lead to the additional population exposure from natural sources less than 0,1 mSv/year. On the base of this assumption it is shown that effective specific activity of natural radionuclides in these products must not exceed 740 Bq/kg.

  17. The encounter and analysis of naturally occurring radionuclides in gas and oil production and processing

    Energy Technology Data Exchange (ETDEWEB)

    Hartog, F.A.; Jonkers, G.; Knaepen, W.A.I. [Shell Research and Technology Centre, Amsterdam, (Netherlands)

    1996-12-31

    As a result of oil and gas production, radioactive daughter elements from the uranium and thorium decay series can be mobilized and transported away from the reservoir. Due to changes in flow regime, temperature, pressure or chemical environment NORs (Naturally Occurring Radionuclides) may build up in products, by-products or waste streams from gas and oil production and processing facilities. Products containing NORs are commonly denoted by the acronym NORM (Naturally Occurring Radioactive Materials). Main topics of this paper are: E and P (Exploration and Production) NORM characteristics; incentives for NORM analysis; NORM analysis; interlaboratory test programme; analysis techniques; results and conclusions of the test programme. 4 figs., 2 tabs.

  18. Production of natural flavour compounds: bioconversion of monoterpenes by spores of Penicillium digitatum

    NARCIS (Netherlands)

    Wolken, W.A.M.

    2003-01-01

    Consumers prefer natural over artificial additives. Consequently natural flavour-compounds fetch higher prices than the corresponding artificial compound. Various natural means of flavour production are discussed in this dissertation. The major part is focused on the biotransformation of geraniol in

  19. Copy, edit, and paste: natural product approaches to biomaterials and neuroengineering.

    Science.gov (United States)

    Gademann, Karl

    2015-03-17

    Progress in the chemical sciences has formed the world we live in, both on a macroscopic and on a nanoscopic scale. The last century witnessed the development of high performance materials that interact with humans on many layers, from clothing to construction, from media to medical devices. On a molecular level, natural products and their derivatives influence many biological processes, and these compounds have enormously contributed to the health and quality of living of humans. Although coatings of stone materials with oils or resins (containing natural products) have led to improved tools already millennia ago, in contrast today, natural product approaches to designer materials, that is, combining the best of both worlds, remain scarce. In this Account, we will summarize our recent research efforts directed to the generation of natural product functionalized materials, exploiting the strategy of "copy, edit, and paste with natural products". Natural products embody the wisdom of evolution, and only total synthesis is able to unlock the secrets enshrined in their molecular structure. We employ total synthesis ("copy") as a scientific approach to address problems related to molecular structure, the biosynthesis of natural products, and their bioactivity. Additionally, the fundamental desire to investigate the mechanism of action of natural products constitutes a key driver for scientific inquiry. In an emerging area of relevance to society, we have prepared natural products such as militarinone D that can stimulate neurite outgrowth and facilitate nerve regeneration. This knowledge obtained by synthetic organic chemistry on complex natural products can then be used to design structurally simplified compounds that retain the biological power of the parent natural product ("edit"). This process, sometimes referred to as function-oriented synthesis, allows obtaining derivatives with better properties, improving their chemical tractability and reducing the step count

  20. Identifying HER2 inhibitors from natural products database.

    Directory of Open Access Journals (Sweden)

    Shun-Chieh Yang

    Full Text Available The relationship between abnormal HER2 expression and cancer is important in cancer therapeutics. Formation and spread of cancer cells may be restricted by inhibiting HER2. We conducted ligand-based and structure-based studies to assess the potency of natural compounds as potential HER2 inhibitors. Multiple linear regression (MLR and support vector machine (SVM models were constructed to predict biological activities of natural compounds, and molecular dynamics (MD was used to assess their stability with HER2 under a dynamic environment. Predicted bioactivities of the natural compounds ranged from 6.014-9.077 using MLR (r(2 = 0.7954 and 5.122-6.950 using SVM (r(2 = 0.8620. Both models were in agreement and suggest bioactivity based on candidate structure. Conformation changes caused by MD favored the formation of stabilizing H-bonds. All candidates had higher stability than Lapinatib, which may be due to the number and spatial distribution of additional H-bonds and hydrophobic interactions. Amino acids Lys724 and Lys736 are critical for binding in HER2, and Thr798, Cys805, and Asp808 are also important for increased stability. Candidates may block the entrance to the ATP binding site located within the inner regions and prevent downstream activation of HER2. Our multidirectional approach indicates that the natural compounds have good ligand efficacy in addition to stable binding affinities to HER2, and should be potent candidates of HER2 inhibitors. With regard to drug design, designing HER2 inhibitors with carboxyl or carbonyl groups available for H-bond formation with Lys724 and Lys736, and benzene groups for hydrophobic contact with Cys805 may improve protein-ligand stability.

  1. Natural Product Shows Effectiveness in Combating Colorectal Cancer | Poster

    Science.gov (United States)

    An herbal extract used for centuries to prevent heart disease has now been shown to be effective against colorectal cancer when tested in laboratory cell cultures. Scientists from NCI at Frederick found that the natural extract cryptotanshinone (CPT) stops the uncontrolled cell growth characteristic of cancer by interfering with a protein that has been implicated in several cancers, including those of the colon and rectum. The results appear in the journal Molecular and Cellular Biochemistry.

  2. Do Anti-Bredt Natural Products Exist? Olefin Strain Energy as a Predictor of Isolability.

    Science.gov (United States)

    Krenske, Elizabeth H; Williams, Craig M

    2015-09-01

    Bredt's rule holds a special place in the realm of physical organic chemistry, but its application to natural products chemistry—the field in which the rule was originally formulated—is not well defined. Herein, the use of olefin strain (OS) energy as a readily calculated predictor of the stability of natural products containing a bridgehead alkene is introduced. Schleyer first used OS energies to classify parent bridgehead alkenes into "isolable", "observable", and "unstable" classes. OS calculations on natural products, using contemporary forcefield methods, unequivocally predict all structurally verified bridgehead alkene natural products to be "isolable". Thus, when one assigns the structure of a putative bridgehead alkene natural product, an OS in the "observable" or "unstable" ranges is a red flag for error.

  3. Relevance of Natural Phenolics from Grape and Derivative Products in the Formulation of Cosmetics

    Directory of Open Access Journals (Sweden)

    María Luisa Soto

    2015-08-01

    Full Text Available The consumer demand for natural ingredients in cosmetic products is increasing. Phenolic compounds are among the most studied natural antioxidant compounds, they also present antimicrobial, anti-inflammatory or antiaging actions and can permeate through the skin barrier. Grapes contain valuable phenolic components and grape byproducts are widely available low cost raw materials. This review presents an overview of the application of phenolic compounds from grape products and byproducts as sources of natural ingredients for cosmetics.

  4. Advancement in bioprocess technology: parallels between microbial natural products and cell culture biologics.

    Science.gov (United States)

    Bandyopadhyay, Arpan A; Khetan, Anurag; Malmberg, Li-Hong; Zhou, Weichang; Hu, Wei-Shou

    2017-02-09

    The emergence of natural products and industrial microbiology nearly eight decades ago propelled an era of bioprocess innovation. Half a century later, recombinant protein technology spurred the tremendous growth of biologics and added mammalian cells to the forefront of industrial producing cells in terms of the value of products generated. This review highlights the process technology of natural products and protein biologics. Despite the separation in time, there is a remarkable similarity in their progression. As the new generation of therapeutics for gene and cell therapy emerges, its process technology development can take inspiration from that of natural products and biologics.

  5. "Common synthetic scaffolds" in the synthesis of structurally diverse natural products.

    Science.gov (United States)

    Anagnostaki, Elissavet E; Zografos, Alexandros L

    2012-09-01

    Selected natural products have long been considered as desirable targets for total synthesis due to their unique biological properties and their challenging structural complexity. Laboratory synthesis of natural compounds usually relies on target-oriented synthesis, involving the production, isolation and purification of successive intermediates, requiring multiple steps to arrive to the final product. A far more economical approach using common synthetic scaffolds that can be readily transformed through biomimetic-like pathways to a range of structurally diverse natural products has been evolved in the last decade, leading synthesis to new directions. This tutorial review critically presents the hallmarks in this field.

  6. Natural rubber and its synthetic analogue, polyisoprene rubber, production prospects

    Institute of Scientific and Technical Information of China (English)

    Dr. A.S.Dykman

    2012-01-01

    One of the main features characterizing the contemporary level of civilization is the universal use of motor transport. Over the past 15 years, global production of cars has increased by more than one and a half, exceeding 80 million vehicles per year. The tire industry has been developing at the corresponding rate.

  7. Natural regulation of Delia radicum in organic cabbage production

    DEFF Research Database (Denmark)

    Meyling, N.V.; Navntoft, S.; Philipsen, H.;

    2013-01-01

    In a field experiment, we evaluated effects of three different organic white cabbage-cropping systems (O1, O2, O3) on the cabbage root fly, Delia radicum, and its egg predators and pupal parasitoids over 3 years. The three systems all complied with regulations for organic production, but varied...

  8. METHANOL PRODUCTION FROM BIOMASS AND NATURAL GAS AS TRANSPORTATION FUEL

    Science.gov (United States)

    Two processes are examined for production of methanol. They are assessed against the essential requirements of a future alternative fuel for road transport: that it (i) is producible in amounts comparable to the 19 EJ of motor fuel annually consumed in the U.S., (ii) minimizes em...

  9. Optimization of a photobioreactor biomass production using natural light

    CERN Document Server

    Grognard, Frédéric; Pierre, Masci; Bernard, Olivier

    2010-01-01

    We address the question of optimization of the biomass long term productivity in the framework of microalgal biomass production in photobioreactors under the influence of day/night cycles. For that, we propose a simple bioreactor model accounting for light attenuation in the reactor due to biomass density and obtain the control law that optimizes productivity over a single day through the application of Pontryagin's maximum principle, with the dilution rate being the control. An important constraint on the obtained solution is that the biomass in the reactor should be at the same level at the beginning and at the end of the day so that the same control can be applied everyday and optimizes the long term productivity. Several scenarios are possible depending on the microalgae's strain parameters and the maximal admissible value of the dilution rate: bang-bang or bang-singular-bang control or, if the growth rate of the algae is very strong in the presence of light, constant maximal dilution. A bifurcation diagr...

  10. Natural deep eutectic solvents and their application in natural product research and development

    NARCIS (Netherlands)

    Dai, yuntao

    2013-01-01

    Natural deep eutectic solvents (NADES) ionic liquids (ILs) and deep eutectic solvents (DES) were proposed by our group to extend the range of ILs and DES, particularly to develop cheap, nontoxic, and low viscosity green solvents, and to apply them in health-related fields. They are liquid supramolec

  11. Ubiquitous Ursolic Acid: A Potential Pentacyclic Triterpene Natural Product

    Directory of Open Access Journals (Sweden)

    Ibrahim T Babalola

    2013-07-01

    Full Text Available There is an unprecedented growing interest in natural triterpenes in the last few decades due to the discovery of their potential biological and pharmacological activities. Ursolic acid (3β-hydroxyurs-12-en-28-oic (UA (4 is a pentacyclic triterpene, occurring in many plant parts including fruits and seeds. This paper reviews several studies on the in vitro and in vivo pharmacological activities of UA (4. This review brings to limelight sources and the beneficial potentials of UA (4 in foods, cosmetics and medicine.

  12. [Inspirations from natural products based drug research and development for Chinese medicine research--analysis of natural products recoded in TTD].

    Science.gov (United States)

    Chen, Xiu-Ping; Lu, Jin-Jian; Guo, Jia-Jie; Bao, Jiao-Lin; Xu, Wen-Shan; Ding, Qian; Wang, Yi-Tao

    2012-11-01

    Natural product is an important source of new drug research and development (R&D). Traditional Chinese medicine (TCM) innovation is the key step for its modernization and internationalization. However, due to the complexity of TCM, there are many difficulties and confusions in this process. Target-based drug discovery is the mainstream model and method of R&D. TTD, short for therapeutic target database, is developed by National University of Singapore. Besides a large amount of information on drug targets, the database also contains considerable information related to natural products. This paper briefly introduces the TTD, analyzes the natural products derived drugs/compounds recorded in TTD, which we think might provide some inspiration for the innovation of TCM.

  13. Measurements of methane emissions at natural gas production sites in the United States

    OpenAIRE

    Allen, David T.; Torres, Vincent M.; Thomas, James; Sullivan, David W.; Harrison, Matthew; Hendler, Al; Herndon, Scott C.; Kolb, Charles E.; Fraser, Matthew P.; Hill, A. Daniel; Lamb, Brian K.; Miskimins, Jennifer; Sawyer, Robert F.; Seinfeld, John H.

    2013-01-01

    Engineering estimates of methane emissions from natural gas production have led to varied projections of national emissions. This work reports direct measurements of methane emissions at 190 onshore natural gas sites in the United States (150 production sites, 27 well completion flowbacks, 9 well unloadings, and 4 workovers). For well completion flowbacks, which clear fractured wells of liquid to allow gas production, methane emissions ranged from 0.01 Mg to 17 Mg (mean = 1.7 Mg; 95% confiden...

  14. Marine Vibrionaceae as a source of bioactive natural products

    DEFF Research Database (Denmark)

    Månsson, Maria; Wietz, Matthias; Gram, Lone;

    to produce secondary metabolites. We have studied the production of antibacterial compounds in Vibrionaceae collected during a global marine expedition, Galathea 3. Apart from growth inhibitory compounds, we searched for compounds that interfere with virulence regulation in Staphylococcus aureus. We found......Vibrionaceae are Gram-negative bacteria found widespread in the marine environment where they are particularly abundant on the surface of marine macroorganisms. Production of antibacterial compounds appears to be common among vibrios, yet vibrios are largely underexplored for their proclivity...... depsipeptides, solonamide A and B, as potent inhibitors of the agr QS system involved in virulence expression in S. aureus. Of special interest was a pronounced effect against a highly virulent, CA-MRSA strain (USA300). In conclusion, we found that vibrios are competent producers of secondary metabolites, some...

  15. Applications of biochromatography in the screening of bioactive natural products.

    Science.gov (United States)

    Chen, Cen; Yang, Feng-Qing; Zuo, Hua-Li; Song, Yue-Lin; Xia, Zhi-Ning; Xiao, Wen

    2013-09-01

    Searching for bioactive compounds from natural resources such as plant materials has become a focus for study. Several models, such as animal (biofluid, organ and tissue) and cellular (several kinds of cell lines), have traditionally been used for this purpose. As a fast, economic and effective way to identify or predict bioactive compounds in complex matrices, biochromatography has developed rapidly during the past years. Combing the properties of traditional chromatography and biomaterials, biochromatographic analysis possesses features of simultaneous screening, separation and structural identification for active compounds in a complex matrix. According to the process, biochromatography can be divided into offline and online approaches. For offline bioextraction, the biomaterials are used as the extraction phase and followed by routine chromatographic analysis. For online biochromatography, the biomaterials are directly used as the stationary phase for chromatographic analysis. This paper reviews the applications of offline bioextraction followed by chromatographic analysis and online biochromatography, including molecular, cell membrane and cell, and artificial biomembrane chromatography in the screening or predicting active compounds from natural sources.

  16. Production of Renewable Natural Gas from Waste Biomass

    Science.gov (United States)

    Kumar, Sachin; Suresh, S.; Arisutha, S.

    2013-03-01

    Biomass energy is expected to make a major contribution to the replacement of fossil fuels. Methane produced from biomass is referred to as bio-methane, green gas, bio-substitute natural gas or renewable natural gas (RNG) when it is used as a transport fuel. Research on upgrading of the cleaned producer gas to RNG is still ongoing. The present study deals with the conversion of woody biomass into fuels, RNG using gasifier. The various effects of parameters like temperature, pressure, and tar formation on conversion were also studied. The complete carbon conversion was observed at 480 °C and tar yield was significantly less. When biomass was gasified with and without catalyst at about 28 s residence time, ~75 % (w/w) and 88 % (w/w) carbon conversion for without and with catalyst was observed. The interest in RNG is growing; several initiatives to demonstrate the thermal-chemical conversion of biomass into methane and/or RNG are under development.

  17. Antiviral Activity of Natural Products Extracted from Marine Organisms

    Directory of Open Access Journals (Sweden)

    Sobia Tabassum

    2011-11-01

    Full Text Available Many epidemics have broken out over the centuries. Hundreds and thousands of humans have died over a disease. Available treatments for infectious diseases have always been limited. Some infections are more deadly than the others, especially viral pathogens. These pathogens have continuously resisted all kinds of medical treatment, due to a need for new treatments to be developed. Drugs are present in nature and are also synthesized in vitro and they help in combating diseases and restoring health. Synthesizing drugs is a hard and time consuming task, which requires a lot of man power and financial aid. However, the natural compounds are just lying around on the earth, may it be land or water. Over a thousand novel compounds isolated from marine organisms are used as antiviral agents. Others are being pharmacologically tested. Today, over forty antiviral compounds are present in the pharmacological market. Some of these compounds are undergoing clinical and pre-clinical stages. Marine compounds are paving the way for a new trend in modern medicine.

  18. Mycolic Acid-Containing Bacteria Induce Natural-Product Biosynthesis in Streptomyces Species▿ †

    Science.gov (United States)

    Onaka, Hiroyasu; Mori, Yukiko; Igarashi, Yasuhiro; Furumai, Tamotsu

    2011-01-01

    Natural products produced by microorganisms are important starting compounds for drug discovery. Secondary metabolites, including antibiotics, have been isolated from different Streptomyces species. The production of these metabolites depends on the culture conditions. Therefore, the development of a new culture method can facilitate the discovery of new natural products. Here, we show that mycolic acid-containing bacteria can influence the biosynthesis of cryptic natural products in Streptomyces species. The production of red pigment by Streptomyces lividans TK23 was induced by coculture with Tsukamurella pulmonis TP-B0596, which is a mycolic acid-containing bacterium. Only living cells induced this pigment production, which was not mediated by any substances. T. pulmonis could induce natural-product synthesis in other Streptomyces strains too: it altered natural-product biosynthesis in 88.4% of the Streptomyces strains isolated from soil. The other mycolic acid-containing bacteria, Rhodococcus erythropolis and Corynebacterium glutamicum, altered biosynthesis in 87.5 and 90.2% of the Streptomyces strains, respectively. The coculture broth of T. pulmonis and Streptomyces endus S-522 contained a novel antibiotic, which we named alchivemycin A. We concluded that the mycolic acid localized in the outer cell layer of the inducer bacterium influences secondary metabolism in Streptomyces, and this activity is a result of the direct interaction between the mycolic acid-containing bacteria and Streptomyces. We used these results to develop a new coculture method, called the combined-culture method, which facilitates the screening of natural products. PMID:21097597

  19. Effect of natural zeolite on methane production for anaerobic digestion of ammonium rich organic sludge.

    Science.gov (United States)

    Tada, Chika; Yang, Yingnan; Hanaoka, Toshiaki; Sonoda, Akinari; Ooi, Kenta; Sawayama, Shigeki

    2005-03-01

    The effect of an inorganic additive on the methane production from NH(4+)-rich organic sludge during anaerobic digestion was investigated using different kinds of inorganic adsorbent zeolites (mordenite, clinoptilolite, zeolite 3A, zeolite 4A), clay mineral (vermiculite), and manganese oxides (hollandite, birnessite). The additions of inorganic materials resulted in significant NH4+ removals from the natural organic sludge ([NH4+]=1, 150 mg N/l), except for the H-type zeolite 3A and birnessite. However, an enhanced methane production was only achieved using natural mordenite. Natural mordenite also enhanced the methane production from the sludge with a markedly high NH4+ concentration (4500 mg N/l) during anaerobic digestion. Chemical analyses of the sludge after the digestion showed considerable increases in the Ca2+ and Mg2+ concentrations in the presence of natural mordenite, but not with synthetic zeolite 3A. The effect of Ca2+ or Mg2+ addition on the methane production was studied using Na(+)-exchanges mordenite and Ca2+ or Mg(2+)-enriched sludge. The simultaneous addition of Ca2+ ions and Na(+)-exchanged mordenite enhanced the methane production; the amount of produced methane was about three times greater than that using only the Na(+)-exchanged mordenite. In addition, comparing the methane production by the addition of natural mordenite or Ca2+ ions, the methane production with natural mordenite was about 1.7 times higher than that with only Ca2+ ions. The addition of 5% and 10% natural mordenite were suitable condition for obtaining a high methane production. These results indicated that the Ca2+ ions, which are released from natural mordenite by a Ca2+/NH4+ exchange, enhanced the methane production of the organic waste at a high NH4+ concentration. Natural mordenite has a synergistic effect on the Ca2+ supply as well on the NH4+ removal during anaerobic digestion, which is effective for the mitigation of NH4+ inhibition against methane production.

  20. Natural products discovery from micro-organisms in the post-genome era.

    Science.gov (United States)

    Ikeda, Haruo

    2017-01-01

    With the decision to award the Nobel Prize in Physiology or Medicine to Drs. S. Ōmura, W.C. Campbell, and Y. Tu, the importance and usefulness of natural drug discovery and development have been revalidated. Since the end of the twentieth century, many genome analyses of organisms have been conducted, and accordingly, numerous microbial genomes have been decoded. In particular, genomic studies of actinomycetes, micro-organisms that readily produce natural products, led to the discovery of biosynthetic gene clusters responsible for producing natural products. New explorations for natural products through a comprehensive approach combining genomic information with conventional methods show great promise for the discovery of new natural products and even systematic generation of unnaturally occurring compounds.

  1. Human contact imagined during the production process increases food naturalness perceptions.

    Science.gov (United States)

    Abouab, Nathalie; Gomez, Pierrick

    2015-08-01

    It is well established that food processing and naturalness are not good friends, but is food processing always detrimental to naturalness? Building on the contagion principle, this research examines how production mode (handmade vs. machine-made) influences naturalness perceptions. In a pilot study (n = 69) and an experiment (n = 133), we found that compared with both a baseline condition and a condition in which the mode of production process was portrayed as machine-made, a handmade production mode increases naturalness ratings of a grape juice. A mediation analysis demonstrates that these effects result from higher perceived human contact suggesting that the production process may preserve food naturalness when humanized.

  2. Insects: an underrepresented resource for the discovery of biologically active natural products

    Directory of Open Access Journals (Sweden)

    Lauren Seabrooks

    2017-07-01

    Full Text Available Nature has been the source of life-changing and -saving medications for centuries. Aspirin, penicillin and morphine are prime examples of Nature׳s gifts to medicine. These discoveries catalyzed the field of natural product drug discovery which has mostly focused on plants. However, insects have more than twice the number of species and entomotherapy has been in practice for as long as and often in conjunction with medicinal plants and is an important alternative to modern medicine in many parts of the world. Herein, an overview of current traditional medicinal applications of insects and characterization of isolated biologically active molecules starting from approximately 2010 is presented. Insect natural products reviewed were isolated from ants, bees, wasps, beetles, cockroaches, termites, flies, true bugs, moths and more. Biological activities of these natural products from insects include antimicrobial, antifungal, antiviral, anticancer, antioxidant, anti-inflammatory and immunomodulatory effects.

  3. Insects: an underrepresented resource for the discovery of biologically active natural products.

    Science.gov (United States)

    Seabrooks, Lauren; Hu, Longqin

    2017-07-01

    Nature has been the source of life-changing and -saving medications for centuries. Aspirin, penicillin and morphine are prime examples of Nature׳s gifts to medicine. These discoveries catalyzed the field of natural product drug discovery which has mostly focused on plants. However, insects have more than twice the number of species and entomotherapy has been in practice for as long as and often in conjunction with medicinal plants and is an important alternative to modern medicine in many parts of the world. Herein, an overview of current traditional medicinal applications of insects and characterization of isolated biologically active molecules starting from approximately 2010 is presented. Insect natural products reviewed were isolated from ants, bees, wasps, beetles, cockroaches, termites, flies, true bugs, moths and more. Biological activities of these natural products from insects include antimicrobial, antifungal, antiviral, anticancer, antioxidant, anti-inflammatory and immunomodulatory effects.

  4. Atmospheric emissions and air quality impacts from natural gas production and use.

    Science.gov (United States)

    Allen, David T

    2014-01-01

    The US Energy Information Administration projects that hydraulic fracturing of shale formations will become a dominant source of domestic natural gas supply over the next several decades, transforming the energy landscape in the United States. However, the environmental impacts associated with fracking for shale gas have made it controversial. This review examines emissions and impacts of air pollutants associated with shale gas production and use. Emissions and impacts of greenhouse gases, photochemically active air pollutants, and toxic air pollutants are described. In addition to the direct atmospheric impacts of expanded natural gas production, indirect effects are also described. Widespread availability of shale gas can drive down natural gas prices, which, in turn, can impact the use patterns for natural gas. Natural gas production and use in electricity generation are used as a case study for examining these indirect consequences of expanded natural gas availability.

  5. Maximization of natural gas liquids production from an

    Directory of Open Access Journals (Sweden)

    Ahmed Abd El-Kader Bhran

    2016-09-01

    Full Text Available It is known that the price of liquefied petroleum gas (LPG is higher than that of natural gas from which it is derived. So the modification of a natural gas plant to produce LPG instead of lighter hydrocarbon gases is very important in the view point of economics. The aim of the present work is directed to the modification of Salam gas plant (Khalda Petroleum Company-Egypt to produce LPG from the NGL instead of producing hydrocarbon gases during the NGL stabilization. This can be achieved after adding de-ethanizer and de-butanizer towers. The simulation tool used in this study is HYSYS version 8.4. The produced LPG of 100 ton/day can participate to solve the LPG shortage problem in Egypt and provide a national service to the people of Matruh Governorate. The economic study based on the economic analyzer of HYSIS showed that the pay-back period of the added two towers and their additional equipment has a high investment strength which means that all modification costs will be recovered within a short time. Furthermore, there are other benefits from this modification. The simulation results showed that there is a capacity saving of 56 tons/day in the export pipeline which transfers the gases to western desert gas complex (WDGC at Alexandria. In the same manner, the modified plant provides a capacity saving of 88 tons/day in the dehydration unit and reduces horse power consumption in recycle and first stage export compressors. This modification can be taken as guidelines for both new and plants in operation to increase their profits.

  6. Sustainability, natural and organic cosmetics: consumer, products, efficacy, toxicological and regulatory considerations

    Directory of Open Access Journals (Sweden)

    Bruno Fonseca-Santos

    2015-03-01

    Full Text Available The interest in sustainable products has increased along the years, since the choice of products, packaging and production processes have a great impact on the environment. These products are classified by regulatory agencies in different categories, aggregating advantages to the product and increasing the demand by consumers. However, there is no harmonization in guidelines of these certifying agencies and each cosmetic industry formulates their product and packaging in a more rational way, which causes less damage to the environment. Many cosmetic products have in their formulation natural products that perform a specific biological function, but these products should be evaluated on efficacy and toxicological aspects. The aim of this article is to approach sustainability, natural and organic cosmetics, considering the consumer and the efficacy, toxicological and regulatory aspects.

  7. Natural product-likeness score revisited: an open-source, open-data implementation

    Directory of Open Access Journals (Sweden)

    Jayaseelan Kalai Vanii

    2012-05-01

    Full Text Available Abstract Background Natural product-likeness of a molecule, i.e. similarity of this molecule to the structure space covered by natural products, is a useful criterion in screening compound libraries and in designing new lead compounds. A closed source implementation of a natural product-likeness score, that finds its application in virtual screening, library design and compound selection, has been previously reported by one of us. In this note, we report an open-source and open-data re-implementation of this scoring system, illustrate its efficiency in ranking small molecules for natural product likeness and discuss its potential applications. Results The Natural-Product-Likeness scoring system is implemented as Taverna 2.2 workflows, and is available under Creative Commons Attribution-Share Alike 3.0 Unported License at http://www.myexperiment.org/packs/183.html. It is also available for download as executable standalone java package from http://sourceforge.net/projects/np-likeness/under Academic Free License. Conclusions Our open-source, open-data Natural-Product-Likeness scoring system can be used as a filter for metabolites in Computer Assisted Structure Elucidation or to select natural-product-like molecules from molecular libraries for the use as leads in drug discovery.

  8. Natural product-likeness score revisited: an open-source, open-data implementation.

    Science.gov (United States)

    Jayaseelan, Kalai Vanii; Moreno, Pablo; Truszkowski, Andreas; Ertl, Peter; Steinbeck, Christoph

    2012-05-20

    Natural product-likeness of a molecule, i.e. similarity of this molecule to the structure space covered by natural products, is a useful criterion in screening compound libraries and in designing new lead compounds. A closed source implementation of a natural product-likeness score, that finds its application in virtual screening, library design and compound selection, has been previously reported by one of us. In this note, we report an open-source and open-data re-implementation of this scoring system, illustrate its efficiency in ranking small molecules for natural product likeness and discuss its potential applications. The Natural-Product-Likeness scoring system is implemented as Taverna 2.2 workflows, and is available under Creative Commons Attribution-Share Alike 3.0 Unported License at http://www.myexperiment.org/packs/183.html. It is also available for download as executable standalone java package from http://sourceforge.net/projects/np-likeness/under Academic Free License. Our open-source, open-data Natural-Product-Likeness scoring system can be used as a filter for metabolites in Computer Assisted Structure Elucidation or to select natural-product-like molecules from molecular libraries for the use as leads in drug discovery.

  9. Web search and data mining of natural products and their bioactivities in PubChem.

    Science.gov (United States)

    Ming, Hao; Tiejun, Cheng; Yanli, Wang; Stephen, Bryant H

    2013-10-01

    Natural products, as major resources for drug discovery historically, are gaining more attentions recently due to the advancement in genomic sequencing and other technologies, which makes them attractive and amenable to drug candidate screening. Collecting and mining the bioactivity information of natural products are extremely important for accelerating drug development process by reducing cost. Lately, a number of publicly accessible databases have been established to facilitate the access to the chemical biology data for small molecules including natural products. Thus, it is imperative for scientists in related fields to exploit these resources in order to expedite their researches on natural products as drug leads/candidates for disease treatment. PubChem, as a public database, contains large amounts of natural products associated with bioactivity data. In this review, we introduce the information system provided at PubChem, and systematically describe the applications for a set of PubChem web services for rapid data retrieval, analysis, and downloading of natural products. We hope this work can serve as a starting point for the researchers to perform data mining on natural products using PubChem.

  10. "Pruning of biomolecules and natural products (PBNP)": an innovative paradigm in drug discovery.

    Science.gov (United States)

    Bathula, Surendar Reddy; Akondi, Srirama Murthy; Mainkar, Prathama S; Chandrasekhar, Srivari

    2015-06-21

    The source or inspiration of many marketed drugs can be traced back to natural product research. However, the chemical structure of natural products covers a wide spectrum from very simple to complex. With more complex structures it is often desirable to simplify the molecule whilst retaining the desired biological activity. This approach seeks to identify the structural unit or pharmacophore responsible for the desired activity. Such pharmacophores have been the start point for a wide range of lead generation and optimisation programmes using techniques such as Biology Oriented Synthesis, Diversity Oriented Synthesis, Diverted Total Synthesis, and Fragment Based Drug Discovery. This review discusses the literature precedence of simplification strategies in four areas of natural product research: proteins, polysaccharides, nucleic acids, and compounds isolated from natural product extracts, and their impact on identifying therapeutic products.

  11. Nature and sustainable energy production. Wind turbines in nature reserves; Natuur en duurzame energieproductie. Windturbines in natuurgebieden

    Energy Technology Data Exchange (ETDEWEB)

    Kistenkas, F.H. [Leerstoelgroep Bos- en Natuurbeleid, Wageningen Universiteit WUR, Wageningen (Netherlands)

    2010-06-15

    Recent case law developments and opportunities within the nature conservation law of Natura 2000 are discussed (ch 2). Next, attention is paid whether or not the literature on nature conservation and climate legislation could provide innovative mindsets for the production of renewable energy in or near a Natura 2000 area. [Dutch] In dit artikel wordt ingegaan op de nieuwste jurisprudentiele ontwikkelingen en mogelijkheden binnen het natuurbeschermingsrecht van Natura 2000 (hfst 2) en vervolgens of ook de natuurbeschermingsrechtelijke en klimaatrechtelijke rechtsliteratuur nog vernieuwende denkrichtingen zou kunnen bieden voor duurzame energieproductie in of nabij een Natura 2000-gebied.

  12. Recent Advances in the Total Synthesis of Tetramic Acid-Containing Natural Products

    Directory of Open Access Journals (Sweden)

    Wen-Ju Bai

    2016-01-01

    Full Text Available With incredible bioactivities and fascinating structural complexities, tetramic acid- (TA- containing natural products have attracted favorable attention among the organic chemistry community. Although the construction of the TA core is usually straightforward, the intricate C3-side chain sometimes asks for some deliberative strategy so as to fulfill an elegant total synthesis. This review mainly covers some exceptional synthetic examples for each type of natural product in recent years, showcasing the great achievements as well as unsettled obstacles in this area, in the hope of accelerating the synthetic and biological investigations for this unique type of natural product.

  13. Synthetic Strategies toward Natural Products Containing Contiguous Stereogenic Quaternary Carbon Atoms.

    Science.gov (United States)

    Büschleb, Martin; Dorich, Stéphane; Hanessian, Stephen; Tao, Daniel; Schenthal, Kyle B; Overman, Larry E

    2016-03-18

    Strategies for the total synthesis of complex natural products that contain two or more contiguous stereogenic quaternary carbon atoms in their intricate structures are reviewed with 12 representative examples. Emphasis has been put on methods to create quaternary carbon stereocenters, including syntheses of the same natural product by different groups, thereby showcasing the diversity of thought and individual creativity. A compendium of selected natural products containing two or more contiguous stereogenic quaternary carbon atoms and key reactions in their total or partial syntheses is provided in the Supporting Information.

  14. Natural Products for Management of Oral Mucositis Induced by Radiotherapy and Chemotherapy.

    Science.gov (United States)

    Aghamohamamdi, Azar; Hosseinimehr, Seyed Jalal

    2016-03-01

    Oral mucositis is a common side effect of systemic chemotherapy and radiotherapy of head and neck in patients with cancer. Severe oral mucositis is painful and affects oral functions, including intake of food and medications and speech. Prevention of oral mucositis affects the life quality of patients. Recent studies have been focused on natural products to improve or reduce this complication. Many clinical trials have been performed to assess natural products for treatment of mucositis and their results are promising. The authors reviewed the evidence for natural products in the prevention and treatment of oral mucositis induced by radiation therapy and chemotherapy.

  15. Thinking big about small beings--the (yet) underdeveloped microbial natural products chemistry in Brazil.

    Science.gov (United States)

    Ióca, Laura P; Allard, Pierre-Marie; Berlinck, Roberto G S

    2014-05-01

    Covering: up to 2013. Natural products isolated from microorganisms from Brazil are comprehensively reviewed, including the microbial sources, bioactivities and biosynthesis. Analysis of trends related to the research on microbial natural products in Brazil is discussed in detail. An outlook to future perspectives of research in Brazil is presented considering the development of state-of-the-art strategies and approaches that have emerged during the last decade, aiming to investigate and better understand the microbial world and its chemical and biochemical capabilities. Finally, the importance of microbial natural products biodiscovery is discussed in the context of the BIOTA-FAPESP program in Brazil.

  16. Electrophilic tuning of the chemoprotective natural product sulforaphane

    Science.gov (United States)

    Ahn, Young-Hoon; Hwang, Yousang; Liu, Hua; Wang, Xiu Jun; Zhang, Ying; Stephenson, Katherine K.; Boronina, Tatiana N.; Cole, Robert N.; Dinkova-Kostova, Albena T.; Talalay, Paul; Cole, Philip A.

    2010-01-01

    Sulforaphane [1-isothiocyanato-4-(methylsulfinyl)butane], a naturally occurring isothiocyanate derived from cruciferous vegetables, is a highly potent inducer of phase 2 cytoprotective enzymes and can protect against electrophiles including carcinogens, oxidative stress, and inflammation. The mechanism of action of sulforaphane is believed to involve modifications of critical cysteine residues of Keap1, which lead to stabilization of Nrf2 to activate the antioxidant response element of phase 2 enzymes. However, the dithiocarbamate functional group formed by a reversible reaction between isothiocyanate of sulforaphane and sulfhydryl nucleophiles of Keap1 is kinetically labile, and such modification in intact cells has not yet been demonstrated. Here we designed sulforaphane analogs with replacement of the reactive isothiocyanate by the more gentle electrophilic sulfoxythiocarbamate group that also selectively targets cysteine residues in proteins but forms stable thiocarbamate adducts. Twenty-four sulfoxythiocarbamate analogs were synthesized that retain the structural features important for high potency in sulforaphane analogs: the sulfoxide or keto group and its appropriate distance to electrophilic functional group. Evaluation in various cell lines including hepatoma cells, retinal pigment epithelial cells, and keratinocytes as well as in mouse skin shows that these analogs maintain high potency and efficacy for phase 2 enzyme induction as well as the inhibitory effect on lipopolysaccharide-induced nitric oxide formation like sulforaphane. We further show in living cells that a sulfoxythiocarbamate analog can label Keap1 on several key cysteine residues as well as other cellular proteins offering new insights into the mechanism of chemoprotection. PMID:20439747

  17. Antimicrobial effect of natural dyeing products upon decaycausing bacteria

    Directory of Open Access Journals (Sweden)

    Mayara Abreu Pinheiro

    2012-06-01

    Full Text Available Objective: To evaluate the bacteriostatic and bactericidal activities of tinctures of Rosmarinus officinalis (Rosemary, Calendula officinalis (Marigold and Mikania glomerata (Guaco upon decay-causing bacteria and compare them to chlorhexidine’s. Methods: The Minimum Inhibitory Concentration (MIC was determined by microdilution technique, using 96-well microplates. In each well were inserted 10μL of inoculum (108 cells/mL, 100μL of doubly concentrated BHI broth and 100μL of tinctures at concentrations that vary between 100 and 0.78 mg/mL for T1, T2 and T3. As positive control, Chlorhexidine 0.12% was used. Reading was performed after 24 hours, by visual method. The assays were realized in triplicate. Minimum Bactericidal Concentration (MBC was obtained by seeding of last bacteriostatic and its preceding concentrations, for each product, on Blood Agar. The MBC was considered in the plates that did not present any bacterial growth. Results: Upon Streptococcus mutans, MIC was verified at 6.25mg/mL, for T1, T2, and T3 and MBC at 12.5mg/mL for T1 and T2, and at 6.25mg/mL for T3. Upon Streptococcus oralis, all products presented MIC and MBC at 0.78mg/mL. For Chlorhexidine, the MIC and MBC were 0,04mg/mL, upon S. mutans and S. oralis. Conclusion: The tinctures of Rosemary, Marigold and Guaco showed bactericidal and bacteriostatic activities at low concentrations, upon Streptococcus mutans e Streptococcus oralis. However, the antimicrobial activity of chlorhexidine was superior to the tinctures’

  18. EFFECTS OF OIL AND NATURAL GAS PRICES ON INDUSTRIAL PRODUCTION IN THE EUROZONE MEMBER COUNTRIES

    Directory of Open Access Journals (Sweden)

    Yılmaz BAYAR

    2014-04-01

    Full Text Available Industrial production is one of the leading indicators of gross domestic product which reflects the overall economic performance of a country. In other words decreases or increases in industrial production point out a contracting or expanding economy. Therefore, changes in prices of oil and natural gas which are the crucial inputs to the industrial production are also important for the overall economy. This study examines the effects of changes in oil and natural gas prices on the industrial production in the 18 Eurozone member countries during the period January 2001-September 2013 by using panel regression. We found that oil prices and natural gas prices had negative effect on industrial production in the Eurozone member countries.

  19. Structure elucidation of uniformly 13C labeled small molecule natural products.

    Science.gov (United States)

    Reibarkh, Mikhail; Wyche, Thomas P; Saurí, Josep; Bugni, Tim S; Martin, Gary E; Williamson, R Thomas

    2015-12-01

    Utilization of isotopically labeled proteins and peptides is a routinely employed approach in biomolecular NMR investigations. The widespread availability of inexpensive, uniformly (13) C-enriched glucose now makes it possible to produce uniformly (13) C-labeled natural products by microbial fermentation. In this feature article, the authors describe an experimental approach for the rapid structural characterization of uniformly (13) C-labeled natural products based on the Constant-Time HSQC (CT-HSQC) experiment. Rigorous theoretical evaluation of the CT-HSQC experiment allowed the applicability of the experiment to be expanded from the traditional, narrow scope of labeled amino acids to encompass virtually any small molecule or U-(13) C labeled natural product. A suite of experiments including CT-HSQC, (13) C-(13) C COSY, and COSYLR experiments is sufficient for the structure elucidation of uniformly (13) C-labeled small molecules and natural products. Differences in NMR approaches for structure elucidation of natural abundance and uniformly (13) C-labeled molecules are also discussed. The present work provides a researcher working in this area of natural products chemistry with NMR structure elucidation tools for investigating (13) C-labeled small molecules and natural products.

  20. Integrative Nanomedicine: Treating Cancer With Nanoscale Natural Products

    Science.gov (United States)

    Sarter, Barbara; Koithan, Mary; Banerji, Prasanta; Banerji, Pratip; Jain, Shamini; Ives, John

    2014-01-01

    Finding safer and more effective treatments for specific cancers remains a significant challenge for integrative clinicians and researchers worldwide. One emerging strategy is the use of nanostructured forms of drugs, vaccines, traditional animal venoms, herbs, and nutraceutical agents in cancer treatment. The recent discovery of nanoparticles in traditional homeopathic medicines adds another point of convergence between modern nanomedicine and alternative interventional strategies. A way in which homeopathic remedies could initiate anticancer effects includes cell-to-cell signaling actions of both exogenous and endogenous (exosome) nanoparticles. The result can be a cascade of modulatory biological events with antiproliferative and pro-apoptotic effects. The Banerji Protocols reflect a multigenerational clinical system developed by homeopathic physicians in India who have treated thousands of patients with cancer. A number of homeopathic remedy sources from the Banerji Protocols (eg, Calcarea phosphorica; Carcinosin—tumor-derived breast cancer tissue prepared homeopathically) overlap those already under study in nonhomeopathic nanoparticle and nanovesicle tumor exosome cancer vaccine research. Past research on antineoplastic effects of nano forms of botanical extracts such as Phytolacca, Gelsemium, Hydrastis, Thuja, and Ruta as well as on homeopathic remedy potencies made from the same types of source materials suggests other important overlaps. The replicated finding of silica, silicon, and nano-silica release from agitation of liquids in glassware adds a proven nonspecific activator and amplifier of immunological effects. Taken together, the nanoparticulate research data and the Banerji Protocols for homeopathic remedies in cancer suggest a way forward for generating advances in cancer treatment with natural product–derived nanomedicines. PMID:24753994

  1. NATURAL PRODUCTS AS PRESERVATIVES FOR FAST GROWTH WOODS - A REVIEW

    Directory of Open Access Journals (Sweden)

    Ricardo Marques Barreiros

    2011-11-01

    Full Text Available Normal 0 21 false false false PT-BR X-NONE X-NONE /* Style Definitions */ table.MsoNormalTable {mso-style-name:"Tabela normal"; mso-tstyle-rowband-size:0; mso-tstyle-colband-size:0; mso-style-noshow:yes; mso-style-priority:99; mso-style-qformat:yes; mso-style-parent:""; mso-padding-alt:0cm 5.4pt 0cm 5.4pt; mso-para-margin:0cm; mso-para-margin-bottom:.0001pt; mso-pagination:widow-orphan; font-size:11.0pt; font-family:"Calibri","sans-serif"; mso-ascii-font-family:Calibri; mso-ascii-theme-font:minor-latin; mso-fareast-font-family:"Times New Roman"; mso-fareast-theme-font:minor-fareast; mso-hansi-font-family:Calibri; mso-hansi-theme-font:minor-latin; mso-bidi-font-family:"Times New Roman"; mso-bidi-theme-font:minor-bidi;} Wood is a universal material, economic, historic and sustainable. The paucity of species resistant to biological degradation forced man to use other less durable, especially fast growing, from reforestation, as some species of Eucalyptus and Pinus. These species have moderate or no resistance to wood decay organisms need special treatment and preservatives. The products currently used preservatives are highly toxic and are potential environmental hazards and human health. Thus, there is a growing need to develop effective chemicals, non-toxic to humans and the environment. The direction of research has aimed to develop environmentally friendly products and economic viability, and an alternative is the use of Crude Tall Oil (CTO, which is a waste processing coniferous softwood pulp for the production of kraft paper. The tall oil as a protective agent, has been considered a promising method for significantly reducing the capillary water absorption of sapwood, thereby removing one of the factors that favor the wood being attacked by fungi and insects: water, oxygen and nutrients. Research shows that the tall oil can be used neat, either fresh or distilled, or in combination with biocides.A madeira é um material universal, econ

  2. Seed production in the first eight years and frequency of natural selfing in a simulated jack pine seedling seed orchard

    Science.gov (United States)

    Thomas D. Rudolph

    1977-01-01

    Seed production and percent of natural selfing were determined in an 8 x 8-foot, 1200-tree plantation. Actual seed production was determined through age 6; production through age 8 was projected based on first-year cone counts at age 7. The percent of natural self-pollination, production of seedlings from natural selfing, and percent of selfs that were lethal were...

  3. Review of natural products actions on cytokines in inflammatory bowel disease.

    Science.gov (United States)

    Hur, Sun Jin; Kang, Sung Ho; Jung, Ho Sung; Kim, Sang Chul; Jeon, Hyun Soo; Kim, Ick Hee; Lee, Jae Dong

    2012-11-01

    The purpose of this review is to provide an overview of the effects that natural products have on inflammatory bowel disease (IBD) and to provide insight into the relationship between these natural products and cytokines modulation. More than 100 studies from the past 10 years were reviewed herein on the therapeutic approaches for treating IBD. The natural products having anti-IBD actions included phytochemicals, antioxidants, microorganisms, dietary fibers, and lipids. The literature revealed that many of these natural products exert anti-IBD activity by altering cytokine production. Specifically, phytochemicals such as polyphenols or flavonoids are the most abundant, naturally occurring anti-IBD substances. The anti-IBD effects of lipids were primarily related to the n-3 polyunsaturated fatty acids. The anti-IBD effects of phytochemicals were associated with modulating the levels of tumor necrosis factor α (TNF-α), interleukin (IL)-1, IL-6, inducible nitric oxide synthase, and myeloperoxide. The anti-IBD effects of dietary fiber were mainly mediated via peroxisome proliferator-activated receptor-γ, TNF-α, nitric oxide, and IL-2, whereas the anti-IBD effects of lactic acid bacteria were reported to influence interferon-γ, IL-6, IL-12, TNF-α, and nuclear factor-κ light-chain enhancer of activated B cells. These results suggest that the anti-IBD effects exhibited by natural products are mainly caused by their ability to modulate cytokine production. However, the exact mechanism of action of natural products for IBD therapy is still unclear. Thus, future research is needed to examine the effect of these natural products on IBD and to determine which factors are most strongly correlated with reducing IBD or controlling the symptoms of IBD.

  4. Natural Organic Matter as Global Antennae for Primary Production

    Science.gov (United States)

    Van Trump, J. Ian; Rivera Vega, Fransheska J.

    2013-01-01

    Abstract Humic substances (HS) are high-molecular-weight complex refractory organics that are ubiquitous in terrestrial and aquatic environments. While resistant to microbial degradation, these compounds nevertheless support microbial metabolism via oxidation or reduction of their (hydro)quinone moieties. As such, they are known to be important electron sinks for respiratory and fermentative bacteria and electron sources for denitrifying and perchlorate-reducing bacteria. HS also strongly promote abiotic reduction of Fe(III) when irradiated with light. Here, we show that HS-enhanced Fe(III) photoreduction can also drive chemolithotrophic microbial respiration by producing Fe(II), which functions as a respiratory electron donor. Due to their molecular complexity, HS absorb most of the electromagnetic spectrum and can act as broad-spectrum antennae converting radiant energy into bioavailable chemical energy. The finding that chemolithotrophic organisms can utilize this energy has important implications for terrestrial, and possibly extraterrestrial, microbial processes and offers an alternative mechanism of radiation-driven primary productivity to that of phototrophy. Key Words: Deep subsurface biosphere—Chemolithotrophic microorganisms—Organic matter—Geochemistry—Iron-oxidizing bacteria. Astrobiology 13, 476–482. PMID:23683047

  5. Discovery of New Compounds Active against Plasmodium falciparum by High Throughput Screening of Microbial Natural Products

    Science.gov (United States)

    Pérez-Moreno, Guiomar; Cantizani, Juan; Sánchez-Carrasco, Paula; Ruiz-Pérez, Luis Miguel; Martín, Jesús; el Aouad, Noureddine; Pérez-Victoria, Ignacio; Tormo, José Rubén; González-Menendez, Víctor; González, Ignacio; de Pedro, Nuria; Reyes, Fernando; Genilloud, Olga; Vicente, Francisca; González-Pacanowska, Dolores

    2016-01-01

    Due to the low structural diversity within the set of antimalarial drugs currently available in the clinic and the increasing number of cases of resistance, there is an urgent need to find new compounds with novel modes of action to treat the disease. Microbial natural products are characterized by their large diversity provided in terms of the chemical complexity of the compounds and the novelty of structures. Microbial natural products extracts have been underexplored in the search for new antiparasitic drugs and even more so in the discovery of new antimalarials. Our objective was to find new druggable natural products with antimalarial properties from the MEDINA natural products collection, one of the largest natural product libraries harboring more than 130,000 microbial extracts. In this work, we describe the optimization process and the results of a phenotypic high throughput screen (HTS) based on measurements of Plasmodium lactate dehydrogenase. A subset of more than 20,000 extracts from the MEDINA microbial products collection has been explored, leading to the discovery of 3 new compounds with antimalarial activity. In addition, we report on the novel antiplasmodial activity of 4 previously described natural products. PMID:26735308

  6. Discovery of New Compounds Active against Plasmodium falciparum by High Throughput Screening of Microbial Natural Products.

    Directory of Open Access Journals (Sweden)

    Guiomar Pérez-Moreno

    Full Text Available Due to the low structural diversity within the set of antimalarial drugs currently available in the clinic and the increasing number of cases of resistance, there is an urgent need to find new compounds with novel modes of action to treat the disease. Microbial natural products are characterized by their large diversity provided in terms of the chemical complexity of the compounds and the novelty of structures. Microbial natural products extracts have been underexplored in the search for new antiparasitic drugs and even more so in the discovery of new antimalarials. Our objective was to find new druggable natural products with antimalarial properties from the MEDINA natural products collection, one of the largest natural product libraries harboring more than 130,000 microbial extracts. In this work, we describe the optimization process and the results of a phenotypic high throughput screen (HTS based on measurements of Plasmodium lactate dehydrogenase. A subset of more than 20,000 extracts from the MEDINA microbial products collection has been explored, leading to the discovery of 3 new compounds with antimalarial activity. In addition, we report on the novel antiplasmodial activity of 4 previously described natural products.

  7. Thiol Probes To Detect Electrophilic Natural Products Based on Their Mechanism of Action.

    Science.gov (United States)

    Castro-Falcón, Gabriel; Hahn, Dongyup; Reimer, Daniela; Hughes, Chambers C

    2016-08-19

    New methods are urgently needed to find novel natural products as structural leads for the development of new drugs against emerging diseases such as cancer and multiresistant bacterial infections. Here we introduce a reactivity-guided drug discovery approach for electrophilic natural products, a therapeutically relevant class of natural products that covalently modify their cellular targets, in crude extracts. Using carefully designed halogenated aromatic reagents, the process furnishes derivatives that are UV-active and highly conspicuous via mass spectrometry by virtue of an isotopically unique bromine or chlorine tag. In addition to the identification of high-value metabolites, the process facilitates the difficult task of structure elucidation by providing derivatives that are primed for X-ray crystallographic analysis. We show that a cysteine probe efficiently and chemoselectively labels enone-, β-lactam-, and β-lactone-based electrophilic natural products (parthenolide, andrographolide, wortmannin, penicillin G, salinosporamide), while a thiophenol probe preferentially labels epoxide-based electrophilic natural products (triptolide, epoxomicin, eponemycin, cyclomarin, salinamide). Using the optimized method, we were able to detect and isolate the epoxide-bearing natural product tirandalydigin from Salinispora and thereby link an orphan gene cluster to its gene product.

  8. Discovery of New Compounds Active against Plasmodium falciparum by High Throughput Screening of Microbial Natural Products.

    Science.gov (United States)

    Pérez-Moreno, Guiomar; Cantizani, Juan; Sánchez-Carrasco, Paula; Ruiz-Pérez, Luis Miguel; Martín, Jesús; El Aouad, Noureddine; Pérez-Victoria, Ignacio; Tormo, José Rubén; González-Menendez, Víctor; González, Ignacio; de Pedro, Nuria; Reyes, Fernando; Genilloud, Olga; Vicente, Francisca; González-Pacanowska, Dolores

    2016-01-01

    Due to the low structural diversity within the set of antimalarial drugs currently available in the clinic and the increasing number of cases of resistance, there is an urgent need to find new compounds with novel modes of action to treat the disease. Microbial natural products are characterized by their large diversity provided in terms of the chemical complexity of the compounds and the novelty of structures. Microbial natural products extracts have been underexplored in the search for new antiparasitic drugs and even more so in the discovery of new antimalarials. Our objective was to find new druggable natural products with antimalarial properties from the MEDINA natural products collection, one of the largest natural product libraries harboring more than 130,000 microbial extracts. In this work, we describe the optimization process and the results of a phenotypic high throughput screen (HTS) based on measurements of Plasmodium lactate dehydrogenase. A subset of more than 20,000 extracts from the MEDINA microbial products collection has been explored, leading to the discovery of 3 new compounds with antimalarial activity. In addition, we report on the novel antiplasmodial activity of 4 previously described natural products.

  9. Gluten Contamination in Naturally or Labeled Gluten-Free Products Marketed in Italy

    OpenAIRE

    Verma, Anil K.; Simona Gatti; Tiziana Galeazzi; Chiara Monachesi; Lucia Padella; Giada Del Baldo; Roberta Annibali; Elena Lionetti; Carlo Catassi

    2017-01-01

    Background: A strict and lifelong gluten-free diet is the only treatment of celiac disease. Gluten contamination has been frequently reported in nominally gluten-free products. The aim of this study was to test the level of gluten contamination in gluten-free products currently available in the Italian market. Method: A total of 200 commercially available gluten-free products (including both naturally and certified gluten-free products) were randomly collected from different Italian supermark...

  10. Soil Properties and Plant Biomass Production in Natural Rangeland Management Systems

    Directory of Open Access Journals (Sweden)

    Romeu de Souza Werner

    Full Text Available ABSTRACT Improper management of rangelands can cause land degradation and reduce the economic efficiency of livestock activity. The aim of this study was to evaluate soil properties and quantify plant biomass production in four natural rangeland management systems in the Santa Catarina Plateau (Planalto Catarinense of Brazil. The treatments, which included mowed natural rangeland (NR, burned natural rangeland (BR, natural rangeland improved through the introduction of plant species after harrowing (IH, and natural rangeland improved through the introduction of plant species after chisel plowing (IC, were evaluated in a Nitossolo Bruno (Nitisol. In the improved treatments, soil acidity was corrected, phosphate fertilizer was applied, and intercropped annual ryegrass (Lolium multiflorum, velvet grass (Holcus lanatus, and white clover (Trifolium repens were sown. Management systems with harrowed or chisel plowed soil showed improved soil physical properties; however, the effect decreased over time and values approached those of burned and mowed natural rangelands. Natural rangeland systems in the establishment phase had little influence on soil organic C. The mowed natural rangeland and improved natural rangeland exhibited greater production of grazing material, while burning the field decreased production and increased the proportion of weeds. Improvement of the natural rangelands increased leguminous biomass for pasture.

  11. Antifungal activity of different natural dyes against traditional products affected fungal pathogens

    Institute of Scientific and Technical Information of China (English)

    R Mari selvam; AJA Ranjit Singh; K Kalirajan

    2012-01-01

    Objective: In the present study to evaluate the anti fungal activity of natural dyes against traditional products affected fungal pathogens. Methods: Many traditional craft products affected fungal pathogens were isolated using potato dextrose agar medium. The isolated fungus were identified by morphological and microscopically characterization using Alexopolus manual. 50μl of Turmeric, Terminalli, Guava and Henna natural dyes were poured into the wells of the culture plates. If antifungal activity was present on the plates, it was indicated by an inhibition zone surrounding the well containing the natural dye. Result: At a dose level of 50μl of terminalli dye was able to inhibit the growth of all the fungi tested. The absorbance rate of natural dyes analyzed by UV Spectrophotometer. The absorbance rate is high in terminalli (2.266) and turmeric (2.255). Conclusions: Natural dyes were bound with traditional products to give good colour and good antimicrobial activity against isolated fungal pathogens.

  12. Products of steel slags an opportunity to save natural resources.

    Science.gov (United States)

    Motz, H; Geiseler, J

    2001-01-01

    already accepted as a CEN standard and are used for a continuous quality control. Usually the suitability of steel slags is stated by fulfilling the requirements of national and/or international standards and regulations. Based on these standards and regulations in Germany in 1998 about 97% of the produced steel slags have been used as aggregates for road construction (e.g. as surface layer, road base and sub base for high trafficked roads), ways, earthworks, and armourstones for hydraulic structures. Consistent to the successful long-term experience not only products of steel slags but also products of blast furnace slags have been eliminated from the European Waste Catalogue and the European Shipment of Waste Regulation of the European Community, as well as from the lists of OECD for transfrontier movements by the decision of the OECD-Council from 21 September, 1995.

  13. Cyclic Sulfamidate Enabled Syntheses of Amino Acids, Peptides, Carbohydrates, and Natural Products

    Science.gov (United States)

    This article reviews the emergence of cyclic sulfamidates as versatile intermediatesfor the synthesis of unnatural amino acids, chalcogen peptides, modified sugars, drugs and drug candidates, and important natural products.

  14. Natural Products Research in South Africa: End of an Era on Land or ...

    African Journals Online (AJOL)

    NICO

    in South Africa and the pivotal role which studies of indigenous plant natural products .... urated ketone moiety in directing further oxygenation at C-6 in. 15 and 16. ..... Issues in Environmental Science and Technology 13: Chemistry in the Ma-.

  15. Cyclic Sulfamidate Enabled Syntheses of Amino Acids, Peptides, Carbohydrates, and Natural Products

    Science.gov (United States)

    This article reviews the emergence of cyclic sulfamidates as versatile intermediatesfor the synthesis of unnatural amino acids, chalcogen peptides, modified sugars, drugs and drug candidates, and important natural products.

  16. Automated identification of depsipeptide natural products by an informatic search algorithm.

    Science.gov (United States)

    Skinnider, Michael A; Johnston, Chad W; Zvanych, Rostyslav; Magarvey, Nathan A

    2015-01-19

    Nonribosomal depsipeptides are a class of potent microbial natural products, which include several clinically approved pharmaceutical agents. Genome sequencing has revealed a large number of uninvestigated natural-product biosynthetic gene clusters. However, while novel informatic search methods to access these gene clusters have been developed to identify peptide natural products, depsipeptide detection has proven challenging. Herein, we present an improved version of our informatic search algorithm for natural products (iSNAP), which facilitates the detection of known and genetically predicted depsipeptides in complex microbial culture extracts. We validated this technology by identifying several depsipeptides from novel producers, and located a large number of novel depsipeptide gene clusters for future study. This approach highlights the value of chemoinformatic search methods for the discovery of genetically encoded metabolites by targeting specific areas of chemical space.

  17. Evolution of a Natural Products and Nutraceuticals Course in the Pharmacy Curriculum.

    Science.gov (United States)

    Geldenhuys, Werner J; Cudnik, Michelle L; Krinsky, Daniel L; Darvesh, Altaf S

    2015-08-25

    Objective. To develop, implement, and modify a required, second-year pharmacy course that provides an understanding of the scientific, therapeutic, and clinical principles, as well as the evidence-based medicine underlying the use of natural products. Design. A 28-hour, multi-faculty course was developed and offered in 2008. The course was modified over the years to enhance students' practice skills in the use of natural products. A course evaluation and survey were administered to assess the students' opinions. Assessment. Students performed well in the course and provided favorable evaluations, especially for the latest offering. Students reported significantly improved skills in providing advice to patients regarding the use of natural products. Conclusion. The course increased the students' knowledge and application of information and counseling skills regarding natural products.

  18. Anti-Biofilm Performance of Three Natural Products against Initial Bacterial Attachment

    Directory of Open Access Journals (Sweden)

    Keith R. Stokes

    2013-11-01

    Full Text Available Marine bacteria contribute significantly towards the fouling consortium, both directly (modern foul release coatings fail to prevent “slime” attachment and indirectly (biofilms often excrete chemical cues that attract macrofouling settlement. This study assessed the natural product anti-biofilm performance of an extract of the seaweed, Chondrus crispus, and two isolated compounds from terrestrial sources, (+-usnic acid and juglone, against two marine biofilm forming bacteria, Cobetia marina and Marinobacter hydrocarbonoclasticus. Bioassays were developed using quantitative imaging and fluorescent labelling to test the natural products over a range of concentrations against initial bacterial attachment. All natural products affected bacterial attachment; however, juglone demonstrated the best anti-biofilm performance against both bacterial species at a concentration range between 5–20 ppm. In addition, for the first time, a dose-dependent inhibition (hormetic response was observed for natural products against marine biofilm forming bacteria.

  19. Computational strategies for genome-based natural product discovery and engineering in fungi

    NARCIS (Netherlands)

    Lee, van der T.A.J.; Medema, M.H.

    2016-01-01

    Fungal natural products possess biological activities that are of great value to medicine, agriculture and manufacturing. Recent metagenomic studies accentuate the vastness of fungal taxonomic diversity, and the accompanying specialized metabolic diversity offers a great and still largely

  20. Pregnane X receptor and natural products: beyond drug-drug interactions.

    Science.gov (United States)

    Staudinger, Jeff L; Ding, Xunshan; Lichti, Kristin

    2006-12-01

    The pregnane X receptor (PXR, NR1I2) is a member of the nuclear receptor superfamily that is activated by a myriad of compounds and natural products in clinical use. Activation of PXR represents the basis for several clinically important drug-drug interactions. Although PXR activation has undesirable effects in patients on combination therapy, it also mediates the hepatoprotective effects exhibited by some herbal remedies. This review focuses on PXR activation by natural products and the potential therapeutic opportunities presented. In particular, the biological effects of St. John's Wort, gugulipid, kava kava, Coleus forskolii, Hypoxis, Sutherlandia, qing hao, wu wei zi, gan cao and other natural products are discussed. The impact of these natural products on drug metabolism and hepatoprotection is highlighted in the context of activation and antagonism of PXR.

  1. Pregnane X receptor and natural products: beyond drug–drug interactions

    Science.gov (United States)

    Staudinger, Jeff L; Ding, Xunshan; Lichti, Kristin

    2010-01-01

    The pregnane X receptor (PXR, NR1I2) is a member of the nuclear receptor superfamily that is activated by a myriad of compounds and natural products in clinical use. Activation of PXR represents the basis for several clinically important drug–drug interactions. Although PXR activation has undesirable effects in patients on combination therapy, it also mediates the hepatoprotective effects exhibited by some herbal remedies. This review focuses on PXR activation by natural products and the potential therapeutic opportunities presented. In particular, the biological effects of St. John’s Wort, gugulipid, kava kava, Coleus forskolii, Hypoxis, Sutherlandia, qing hao, wu wei zi, gan cao and other natural products are discussed. The impact of these natural products on drug metabolism and hepatoprotection is highlighted in the context of activation and antagonism of PXR. PMID:17125405

  2. Recent advances in natural products from plants for treatment of liver diseases.

    Science.gov (United States)

    Zhang, Aihua; Sun, Hui; Wang, Xijun

    2013-05-01

    Liver disease is any condition that may cause liver inflammation or tissue damage and affects liver function. Natural products that are found in vegetables, fruits, plant extracts, herbs, insects, and animals, have been traditionally used for treating liver diseases. They are chemical compounds that usually have biological activities for use in drug discovery and design. Many natural products have been clinically available as potent hepatoprotective agents against commonly occurring liver diseases. This review summarizes the current progress in the basic, clinical, and translational research on natural products in treatment of various liver diseases. Furthermore, we will focus on the discovery and biological evaluation of the natural products, which shows potential as a new therapeutic agent of liver diseases.

  3. Design of compound libraries based on natural product scaffolds and protein structure similarity clustering (PSSC)

    NARCIS (Netherlands)

    Balamurugan, Rengarajan; Dekker, Frank J; Waldmann, Herbert; Dekker, Frans

    Recent advances in structural biology, bioinformatics and combinatorial chemistry have significantly impacted the discovery of small molecules that modulate protein functions. Natural products which have evolved to bind to proteins may serve as biologically validated starting points for the design

  4. Systems Pharmacology‐Based Discovery of Natural Products for Precision Oncology Through Targeting Cancer Mutated Genes

    Science.gov (United States)

    Fang, J; Cai, C; Wang, Q; Lin, P

    2017-01-01

    Massive cancer genomics data have facilitated the rapid revolution of a novel oncology drug discovery paradigm through targeting clinically relevant driver genes or mutations for the development of precision oncology. Natural products with polypharmacological profiles have been demonstrated as promising agents for the development of novel cancer therapies. In this study, we developed an integrated systems pharmacology framework that facilitated identifying potential natural products that target mutated genes across 15 cancer types or subtypes in the realm of precision medicine. High performance was achieved for our systems pharmacology framework. In case studies, we computationally identified novel anticancer indications for several US Food and Drug Administration‐approved or clinically investigational natural products (e.g., resveratrol, quercetin, genistein, and fisetin) through targeting significantly mutated genes in multiple cancer types. In summary, this study provides a powerful tool for the development of molecularly targeted cancer therapies through targeting the clinically actionable alterations by exploiting the systems pharmacology of natural products. PMID:28294568

  5. Use of natural health products in children Survey of parents in waiting rooms

    National Research Council Canada - National Science Library

    Marshall Godwin; John Crellin; Maria Mathews; Nurun L. Chowdhury; Leigh Anne Newhook; Andrea Pike; Farah McCrate; Rebecca Law

    2013-01-01

    To determine how common it is for parents to give natural health products (NHPs) to their children, which NHPs are being used, why they are being used, and parents' assessments of the benefits and side effects of NHPs. Survey...

  6. [Halogenated natural products from the marine-derived actinobacteria and their halogenation mechanism].

    Science.gov (United States)

    Tan, Yi; Zhou, Hong-xia; Wang, Yi-guang; Gan, Mao-luo; Yang, Zhao-yong

    2013-09-01

    In the last decade, along with the development of taxonomy research in marine-derived actinobacteria, more and more halogenated natural products were discovered from marine actinobacteria. Most of them showed good biological activity and unique structure compared to those from land. The special halogenation mechanism in some compounds' biosynthesis has drawn great attention. So in this review, we focus on the halogenated natural products from marine actinobacteria and their halogenation mechanisms.

  7. Web search and data mining of natural products and their bioactivities in PubChem

    OpenAIRE

    Ming, Hao; Tiejun, Cheng; Yanli, Wang; Stephen, Bryant H.

    2013-01-01

    Natural products, as major resources for drug discovery historically, are gaining more attentions recently due to the advancement in genomic sequencing and other technologies, which makes them attractive and amenable to drug candidate screening. Collecting and mining the bioactivity information of natural products are extremely important for accelerating drug development process by reducing cost. Lately, a number of publicly accessible databases have been established to facilitate the access ...

  8. Collision-Induced Dissociation Mass Spectrometry: A Powerful Tool for Natural Product Structure Elucidation.

    Science.gov (United States)

    Johnson, Andrew R; Carlson, Erin E

    2015-11-03

    Mass spectrometry is a powerful tool in natural product structure elucidation, but our ability to directly correlate fragmentation spectra to these structures lags far behind similar efforts in peptide sequencing and proteomics. Often, manual data interpretation is required and our knowledge of the expected fragmentation patterns for many scaffolds is limited, further complicating analysis. Here, we summarize advances in natural product structure elucidation based upon the application of collision induced dissociation fragmentation mechanisms.

  9. Products of nature and the Association for Molecular Pathology v. Myriad Genetics, Inc. Case

    OpenAIRE

    Conde-Gutiérrez, Carlos A.; Díaz, Lina María

    2013-01-01

    The Supreme Court of Justice of the United States in Association for Molecular Pathology vs. Myriad Genetics, Inc. rules out patents over isolated DNA as they were not different from products of nature, yet it maintains patents over synthetizes genes or DNAC. This decision has redefined the scope of the doctrine of products of nature on biotechnological invention as established by Diamond vs. Chakrabarty. Coincidentally, the Supreme Court’s new interpretation is in harmony with the Andean Tri...

  10. Natural Products as Sources of New Drugs from 1981 to 2014.

    Science.gov (United States)

    Newman, David J; Cragg, Gordon M

    2016-03-25

    This contribution is a completely updated and expanded version of the four prior analogous reviews that were published in this journal in 1997, 2003, 2007, and 2012. In the case of all approved therapeutic agents, the time frame has been extended to cover the 34 years from January 1, 1981, to December 31, 2014, for all diseases worldwide, and from 1950 (earliest so far identified) to December 2014 for all approved antitumor drugs worldwide. As mentioned in the 2012 review, we have continued to utilize our secondary subdivision of a "natural product mimic", or "NM", to join the original primary divisions and the designation "natural product botanical", or "NB", to cover those botanical "defined mixtures" now recognized as drug entities by the U.S. FDA (and similar organizations). From the data presented in this review, the utilization of natural products and/or their novel structures, in order to discover and develop the final drug entity, is still alive and well. For example, in the area of cancer, over the time frame from around the 1940s to the end of 2014, of the 175 small molecules approved, 131, or 75%, are other than "S" (synthetic), with 85, or 49%, actually being either natural products or directly derived therefrom. In other areas, the influence of natural product structures is quite marked, with, as expected from prior information, the anti-infective area being dependent on natural products and their structures. We wish to draw the attention of readers to the rapidly evolving recognition that a significant number of natural product drugs/leads are actually produced by microbes and/or microbial interactions with the "host from whence it was isolated", and therefore it is considered that this area of natural product research should be expanded significantly.

  11. De novo synthesis of natural products via the asymmetric hydration of polyenes.

    Science.gov (United States)

    Wang, Yanping; Xing, Yalan; Zhang, Qi; O'Doherty, George A

    2011-08-14

    For the last ten years our group has been working toward the development of an asymmetric hydration approach to polyketide natural products based on the regioselective hydration of di- and tri-enoates. Key to the success of this approach is the recognition that both high regiocontrol and asymmetric induction could be obtained by the use of a Sharpless asymmetric dihydroxylation reaction. Herein we describe the development of the method and its application to natural product total synthesis.

  12. Pregnane X receptor and natural products: beyond drug–drug interactions

    OpenAIRE

    Staudinger, Jeff L.; Ding, Xunshan; Lichti, Kristin

    2006-01-01

    The pregnane X receptor (PXR, NR1I2) is a member of the nuclear receptor superfamily that is activated by a myriad of compounds and natural products in clinical use. Activation of PXR represents the basis for several clinically important drug–drug interactions. Although PXR activation has undesirable effects in patients on combination therapy, it also mediates the hepatoprotective effects exhibited by some herbal remedies. This review focuses on PXR activation by natural products and the pote...

  13. Chemistry and biology of bengamides and bengazoles, bioactive natural products from Jaspis sponges.

    Science.gov (United States)

    García-Ruiz, Cristina; Sarabia, Francisco

    2014-03-18

    Sponges corresponding to the Jaspidae family have proved to be a prolific source of bioactive natural products. Among these, the bengamides and the bengazoles stand out by virtue of their unprecedented molecular architectures and impressive biological profiles, including antitumor, antibiotic and anthelmintic properties. As a consequence, intense research activity has been devoted to these compounds from both chemical and biological standpoints. This review describes in detail the research into these classes of natural products and the benefits they offer in chemistry and biology.

  14. Natural Products as Tools for Neuroscience: Discovery and Development of Novel Agents to Treat Drug Abuse⊥

    OpenAIRE

    2009-01-01

    Much of what we know about the neurosciences is the direct result of studying psychoactive natural products. Unfortunately, there are many gaps in our understanding of the basic biological processes that contribute to the etiology of many CNS disorders. The investigation of psychoactive natural products offers an excellent approach to identify novel agents to treat CNS disorders and to find new chemical tools to better elucidate their biological mechanisms. This review will detail recent prog...

  15. Tolerance of natural baby skin-care products on healthy, full-term infants and toddlers

    OpenAIRE

    Coret CD; Suero MB; Tierney NK

    2014-01-01

    Catherine D Coret, Michael B Suero, Neena K Tierney Johnson & Johnson Consumer Companies, Inc, Skillman, NJ, USA Purpose: To evaluate the tolerance of baby skin-care products with at least 95% naturally derived ingredients on infants and toddlers. Materials and methods: Healthy, full-term infants and toddlers aged 1–36 months were enrolled. In study 1, a lightly fragranced natural baby hair and body wash (n=30), a lightly fragranced natural baby shampoo (n=30), or a lightly...

  16. Bioactive natural products in cancer prevention and therapy: Progress and promise.

    Science.gov (United States)

    Bishayee, Anupam; Sethi, Gautam

    2016-10-01

    Natural products represent a rich source for the discovery and development of cancer preventive and anticancer drugs. Nearly, 80% of all drugs approved by the United States Food and Drug Administration during the last three decades for cancer therapy are either natural products per se or are based thereon, or mimicked natural products in one form or another. With the advent and refinement of new technologies, such as genetic techniques for production of secondary plant metabolites, combinatorial synthesis and high-throughput screening, it is expected that novel compounds from natural sources, including medicinal plants, would be identified and developed as safe and effective chemopreventive and anticancer drugs. Numerous bioactive natural compounds have been shown to be useful in prevention and therapy of cancer by targeting various signaling molecules and pathways. Extensive literature underscores the anticancer and chemopreventive activity of a plethora of naturally occurring agents, including phytochemicals. Several of these molecules have been tested in clinical trials and some of them have shown promise in combination therapy when administered along with standard chemotherapeutic agents. Thus, accelerated chemopreventive and chemotherapeutic drug development from natural sources is of great importance. In this special theme issue, contributions from eminent scientists and scholars around the world presented critical analysis of the current progress and promise of natural bioactive constituents in cancer prevention and therapy. Copyright © 2016 Elsevier Ltd. All rights reserved.

  17. Productivity as related to diversity and age in planted versus natural forests

    Science.gov (United States)

    Qinfeng Guo; Hai Ren

    2014-01-01

    Little is known about the performance of plantations relative to natural forests of the same climate zone and age. China has more plantations than any other country as a consequence of massive afforestation efforts.We use data from China to comparatively examine tree biomass and productivity of planted and natural stands in relation to climate zone, latitude, elevation...

  18. Recent Advances in Substrate-Controlled Asymmetric Cyclization for Natural Product Synthesis

    Directory of Open Access Journals (Sweden)

    Jeyun Jo

    2017-06-01

    Full Text Available Asymmetric synthesis of naturally occurring diverse ring systems is an ongoing and challenging research topic. A large variety of remarkable reactions utilizing chiral substrates, auxiliaries, reagents, and catalysts have been intensively investigated. This review specifically describes recent advances in successful asymmetric cyclization reactions to generate cyclic architectures of various natural products in a substrate-controlled manner.

  19. Highly Stereoselective Synthesis of a Compound Collection Based on the Bicyclic Scaffolds of Natural Products.

    Science.gov (United States)

    Annamalai, Murali; Hristeva, Stanimira; Bielska, Martyna; Ortega, Raquel; Kumar, Kamal

    2017-05-18

    Despite the great contribution of natural products in the history of successful drug discovery, there are significant limitations that persuade the pharmaceutical industry to evade natural products in drug discovery research. The extreme scarcity as well as structural complexity of natural products renders their practical synthetic access and further modifications extremely challenging. Although other alternative technologies, particularly combinatorial chemistry, were embraced by the pharmaceutical industry to get quick access to a large number of small molecules with simple frameworks that often lack three-dimensional complexity, hardly any success was achieved in the discovery of lead molecules. To acquire chemotypes beholding structural features of natural products, for instance high sp³ character, the synthesis of compound collections based on core-scaffolds of natural products presents a promising strategy. Here, we report a natural product inspired synthesis of six different chemotypes and their derivatives for drug discovery research. These bicyclic hetero- and carbocyclic scaffolds are highly novel, rich in sp³ features and with ideal physicochemical properties to display drug likeness. The functional groups on the scaffolds were exploited further to generate corresponding compound collections. Synthesis of two of these collections exemplified with ca. 350 compounds are each also presented. The whole compound library is being exposed to various biological screenings within the European Lead Factory consortium.

  20. The Continuing Development of E. coli as a Heterologous Host for Complex Natural Product Biosynthesis.

    Science.gov (United States)

    Zhang, Haoran; Fang, Lei; Osburne, Marcia S; Pfeifer, Blaine A

    2016-01-01

    Heterologous biosynthesis of natural products is meant to enable access to the vast array of valuable properties associated with these compounds. Often motivated by limitations inherent in native production hosts, the heterologous biosynthetic process begins with a candidate host regarded as technically advanced relative to original producing organisms. Given this requirement, E. coli has been a top choice for heterologous biosynthesis attempts as associated recombinant tools emerged and continue to develop. However, success requires overcoming challenges associated with natural product formation, including complex biosynthetic pathways and the need for metabolic support. These two challenges have been heavily featured in cellular engineering efforts completed to position E. coli as a viable surrogate host. This chapter outlines steps taken to engineer E. coli with an emphasis on genetic manipulations designed to support the heterologous production of polyketide, nonribosomal peptide, and similarly complex natural products.

  1. Gene Discovery for Synthetic Biology: Exploring the Novel Natural Product Biosynthetic Capacity of Eukaryotic Microalgae.

    Science.gov (United States)

    O'Neill, E C; Saalbach, G; Field, R A

    2016-01-01

    Eukaryotic microalgae are an incredibly diverse group of organisms whose sole unifying feature is their ability to photosynthesize. They are known for producing a range of potent toxins, which can build up during harmful algal blooms causing damage to ecosystems and fisheries. Genome sequencing is lagging behind in these organisms because of their genetic complexity, but transcriptome sequencing is beginning to make up for this deficit. As more sequence data becomes available, it is apparent that eukaryotic microalgae possess a range of complex natural product biosynthesis capabilities. Some of the genes concerned are responsible for the biosynthesis of known toxins, but there are many more for which we do not know the products. Bioinformatic and analytical techniques have been developed for natural product discovery in bacteria and these approaches can be used to extract information about the products synthesized by algae. Recent analyses suggest that eukaryotic microalgae produce many complex natural products that remain to be discovered.

  2. Recent Advances and Applications of Experimental Technologies in Marine Natural Product Research

    Directory of Open Access Journals (Sweden)

    Ke Li

    2015-04-01

    Full Text Available Marine natural products are a rich source of novel and biologically active compounds. The number of identified marine natural compounds has grown 20% over the last five years from 2009 to 2013. Several challenges, including sample collection and structure elucidation, have limited the development of this research field. Nonetheless, new approaches, such as sampling strategies for organisms from extreme ocean environments, nanoscale NMR and computational chemistry for structural determination, are now available to overcome the barriers. In this review, we highlight the experimental technology innovations in the field of marine natural products, which in our view will lead to the development of many new drugs in the future.

  3. Recent Advances and Applications of Experimental Technologies in Marine Natural Product Research

    Science.gov (United States)

    Li, Ke; Chung-Davidson, Yu-Wen; Bussy, Ugo; Li, Weiming

    2015-01-01

    Marine natural products are a rich source of novel and biologically active compounds. The number of identified marine natural compounds has grown 20% over the last five years from 2009 to 2013. Several challenges, including sample collection and structure elucidation, have limited the development of this research field. Nonetheless, new approaches, such as sampling strategies for organisms from extreme ocean environments, nanoscale NMR and computational chemistry for structural determination, are now available to overcome the barriers. In this review, we highlight the experimental technology innovations in the field of marine natural products, which in our view will lead to the development of many new drugs in the future. PMID:25939037

  4. Walking in the woods with quantum chemistry--applications of quantum chemical calculations in natural products research.

    Science.gov (United States)

    Tantillo, Dean J

    2013-08-01

    This Highlight describes applications of quantum chemical calculations to problems in natural products chemistry, including the elucidation of natural product structures (distinguishing between constitutional isomers, distinguishing between diastereomers, and assigning absolute configuration) and determination of reasonable mechanisms for their formation.

  5. INVESTMENT EVALUATION BASED ON THE COMMERCIAL SCOPE - THE PRODUCTION OF NATURAL-GAS

    NARCIS (Netherlands)

    BROENS, DF; HANEVELD, WKK

    1995-01-01

    The annual production planning of a natural gas trading and transporting company is modelled as a linear system of (in)equalities. The model is used to quantify the increase of robustness with respect to commercial uncertainty, resulting from investments in production capacities. A novel concept is

  6. Natural products as sources of new lead compounds for the treatment of Alzheimer's disease.

    Science.gov (United States)

    Huang, Ling; Su, Tao; Li, Xingshu

    2013-01-01

    Alzheimer's disease (AD) is the most prevalent form of dementia and affects approximately 24 million people worldwide. One possible approach for the treatment of this disease is the restoration of the level of acetylcholine (ACh) through the inhibition of acetylcholinesterase (AChE) with reversible inhibitors. Naturally occurring alkaloids are an important source of AChE inhibitors. Galantamine and huperzine A have been used for the clinical treatment of AD patients. In this review, we summarise the natural products and their derivatives that were reported to act as AChE inhibitors for the treatment of AD in 2010-2013. Several characteristics were summarised from the literature results: 1) Amongst all of the natural products with AChE inhibitory activity, alkaloids appear to be the most promising compound class. 2) Coumarins, flavonoids, stilbenes, and other natural products are also important AChE inhibitors from natural products. Among these inhibitors, 146 (IC50 = 0.573 µM) was identified as the most potent AChE inhibitor. 3) A coumarin derivative (117, IC50 = 0.11 nM) exhibited more than 100-fold superior activity compared with the reference drug donepezil hydrochloride (IC50 = 14 nM). In conclusion, natural products and their derivatives are promising leads for the development of new drugs for the future treatment of AD.

  7. Screening for Marine Natural Products with Potential as Chemotherapeutics for Acute Myeloid Leukemia.

    Science.gov (United States)

    Hansen, Espen; Andersen, Jeanette H

    2016-01-01

    Nature is an important source for anti-cancer therapeutics, and nearly half of the currently marketed cancer drugs are derived from natural products. Most of the therapeutic natural products are derived from terrestrial sources, such as paclitaxel, vincristine, epothilones, doxorubicin, etoposide and camptothecin. However, the oceans have received growing interest as a source for new useful bioactive compounds, and there are currently several drugs derived from marine natural products for the treatment of cancer on the market. The current recommended chemotherapy of acute myeloid leukemia (AML) is founded on cytarabine, a molecule derived from a natural product isolated from a marine sponge. However, in order to increase the efficiency of the chemotherapy used in the treatment of AML, it is necessary to develop more targeted drugs with less pronounced side effects. In this review, we argue that marine natural products have many of the desired properties of such a drug, and that prefractionated extract libraries of marine plants, animals and microorganisms should be a part of the screening efforts for new AML chemotherapeutics.

  8. Chemo- and site-selective derivatizations of natural products enabling biological studies.

    Science.gov (United States)

    Robles, Omar; Romo, Daniel

    2014-03-01

    Bioactive natural products and derivatives remain an enduring starting point for the discovery of new cellular targets for disease intervention and lead compounds for the development of new therapeutic agents. The former goal is accomplished through the synthesis of bioactive cellular probes from natural products, enabling insights into the mechanism of action of these natural products by classical affinity chromatography or more recent proteome profiling methods. However, the direct and selective modification of native natural products for these purposes remains a challenge due to the structural complexity and the wide functional group diversity found in these natural substances. The lack of selective synthetic methods available to directly manipulate unprotected complex small molecules, in particular to perform structure-activity relationship studies and prepare appropriate cellular probes, has recently begun to be addressed, benefitting from the broader emerging area of chemoselective synthetic methodology. Thus, new reagents, catalysts and reaction processes are enabling both chemo- and site-selective modifications of complex, native natural products. In this review, we describe selected recent examples of these functionalization strategies in this emerging area.

  9. Natural Products to Counteract the Epidemic of Cardiovascular and Metabolic Disorders.

    Science.gov (United States)

    Waltenberger, Birgit; Mocan, Andrei; Šmejkal, Karel; Heiss, Elke H; Atanasov, Atanas G

    2016-06-22

    Natural products have always been exploited to promote health and served as a valuable source for the discovery of new drugs. In this review, the great potential of natural compounds and medicinal plants for the treatment or prevention of cardiovascular and metabolic disorders, global health problems with rising prevalence, is addressed. Special emphasis is laid on natural products for which efficacy and safety have already been proven and which are in clinical trials, as well as on plants used in traditional medicine. Potential benefits from certain dietary habits and dietary constituents, as well as common molecular targets of natural products, are also briefly discussed. A glimpse at the history of statins and biguanides, two prominent representatives of natural products (or their derivatives) in the fight against metabolic disease, is also included. The present review aims to serve as an "opening" of this special issue of Molecules, presenting key historical developments, recent advances, and future perspectives outlining the potential of natural products for prevention or therapy of cardiovascular and metabolic disease.

  10. Structure-Activity Relationships of the Bioactive Thiazinoquinone Marine Natural Products Thiaplidiaquinones A and B

    Directory of Open Access Journals (Sweden)

    Jacquie L. Harper

    2015-08-01

    Full Text Available In an effort to more accurately define the mechanism of cell death and to establish structure-activity relationship requirements for the marine meroterpenoid alkaloids thiaplidiaquinones A and B, we have evaluated not only the natural products but also dioxothiazine regioisomers and two precursor quinones in a range of bioassays. While the natural products were found to be weak inducers of ROS in Jurkat cells, the dioxothiazine regioisomer of thiaplidiaquinone A and a synthetic precursor to thiaplidiaquinone B were found to be moderately potent inducers. Intriguingly, and in contrast to previous reports, the mechanism of Jurkat cell death (necrosis vs. apoptosis was found to be dependent upon the positioning of one of the geranyl sidechains in the compounds with thiaplidiaquinone A and its dioxothiazine regioisomer causing death dominantly by necrosis, while thiaplidiaquinone B and its dioxothiazine isomer caused cell death via apoptosis. The dioxothiazine regioisomer of thiaplidiaquinone A exhibited more potent in vitro antiproliferative activity against human tumor cells, with NCI sub-panel selectivity towards melanoma cell lines. The non-natural dioxothiazine regioisomers were also more active in antiplasmodial and anti-farnesyltransferase assays than their natural product counterparts. The results highlight the important role that natural product total synthesis can play in not only helping understand the structural basis of biological activity of natural products, but also the discovery of new bioactive scaffolds.

  11. Natural Products to Counteract the Epidemic of Cardiovascular and Metabolic Disorders

    Directory of Open Access Journals (Sweden)

    Birgit Waltenberger

    2016-06-01

    Full Text Available Natural products have always been exploited to promote health and served as a valuable source for the discovery of new drugs. In this review, the great potential of natural compounds and medicinal plants for the treatment or prevention of cardiovascular and metabolic disorders, global health problems with rising prevalence, is addressed. Special emphasis is laid on natural products for which efficacy and safety have already been proven and which are in clinical trials, as well as on plants used in traditional medicine. Potential benefits from certain dietary habits and dietary constituents, as well as common molecular targets of natural products, are also briefly discussed. A glimpse at the history of statins and biguanides, two prominent representatives of natural products (or their derivatives in the fight against metabolic disease, is also included. The present review aims to serve as an “opening” of this special issue of Molecules, presenting key historical developments, recent advances, and future perspectives outlining the potential of natural products for prevention or therapy of cardiovascular and metabolic disease.

  12. Modulation of Toll-like receptor signaling in innate immunity by natural products.

    Science.gov (United States)

    Chen, Luxi; Yu, Jianhua

    2016-08-01

    For centuries, natural products and their derivatives have provided a rich source of compounds for the development of new immunotherapies in the treatment of human disease. Many of these compounds are currently undergoing clinical trials, particularly as anti-oxidative, anti-microbial, and anti-cancer agents. However, the function and mechanism of natural products in how they interact with our immune system has yet to be extensively explored. Natural immune modulators may provide the key to control and ultimately defeat disorders affecting the immune system. They can either up- or down-regulate the immune response with few undesired adverse effects. In this review, we summarize the recent advancements made in utilizing natural products for immunomodulation and their important molecular targets, members of the Toll-like receptor (TLR) family, in the innate immune system.

  13. Subclass-specific labeling of protein-reactive natural products with customized nucleophilic probes.

    Science.gov (United States)

    Rudolf, Georg C; Koch, Maximilian F; Mandl, Franziska A M; Sieber, Stephan A

    2015-02-23

    Natural products represent a rich source of bioactive compounds that constitute a large fraction of approved drugs. Among those are molecules with electrophilic scaffolds, such as Michael acceptors, β-lactams, and epoxides that irreversibly inhibit essential enzymes based on their catalytic mechanism. In the search for novel bioactive molecules, current methods are challenged by the frequent rediscovery of known chemical entities. Herein small nucleophilic probes that attack electrophilic natural products and enhance their detection by HPLC-UV and HPLC-MS are introduced. A screen of diverse probe designs revealed one compound with a desired selectivity for epoxide- and maleimide-based antibiotics. Correspondingly, the natural products showdomycin and phosphomycin could be selectively targeted in extracts of their natural producing organism, in which the probe-modified molecules exhibited superior retention and MS detection relative to their unmodified counterparts. This method may thus help to discover small, electrophilic molecules that might otherwise easily elude detection in complex samples.

  14. Natural radiation - a perspective to radiological risk factors of nuclear energy production

    DEFF Research Database (Denmark)

    Mustonen, R.; Christensen, T.; Stranden, E.

    1992-01-01

    Radiation doses from natural radiation and from man-made modifications on natural radiation, and different natural radiological environments in the Nordic countries are summarized and used as a perspective for the radiological consequences of nuclear energy production. The significance of different...... radiation sources can be judged against the total collective effective dose equivalent from natural radiation in the Nordic countries, 92 000 manSv per year. The collective dose from nuclear energy production during normal operation is estimated to 20 manSv per year and from non-nuclear energy production...... to 80 manSv per year. The increase in collective dose due to the conservation of heating energy in Nordic dwellings is estimated to 23 000 manSv per year, from 1973 to 1984. An indirect radiological danger index is defined in order to be able to compare the significance of estimated future releases...

  15. Recent advances in the elucidation of enzymatic function in natural product biosynthesis [version 1; referees: 2 approved

    Directory of Open Access Journals (Sweden)

    Tan Gao-Yi

    2015-12-01

    Full Text Available With the successful production of artemisinic acid in yeast, the promising potential of synthetic biology for natural product biosynthesis is now being realized. The recent total biosynthesis of opioids in microbes is considered to be another landmark in this field. The importance and significance of enzymes in natural product biosynthetic pathways have been re-emphasized by these advancements. Therefore, the characterization and elucidation of enzymatic function in natural product biosynthesis are undoubtedly fundamental for the development of new drugs and the heterologous biosynthesis of active natural products. Here, discoveries regarding enzymatic function in natural product biosynthesis over the past year are briefly reviewed.

  16. Recent advances in the elucidation of enzymatic function in natural product biosynthesis [version 2; referees: 2 approved

    Directory of Open Access Journals (Sweden)

    Gao-Yi Tan

    2016-02-01

    Full Text Available With the successful production of artemisinic acid in yeast, the promising potential of synthetic biology for natural product biosynthesis is now being realized. The recent total biosynthesis of opioids in microbes is considered to be another landmark in this field. The importance and significance of enzymes in natural product biosynthetic pathways have been re-emphasized by these advancements. Therefore, the characterization and elucidation of enzymatic function in natural product biosynthesis are undoubtedly fundamental for the development of new drugs and the heterologous biosynthesis of active natural products. Here, discoveries regarding enzymatic function in natural product biosynthesis over the past year are briefly reviewed.

  17. Regional air quality impacts of increased natural gas production and use in Texas.

    Science.gov (United States)

    Pacsi, Adam P; Alhajeri, Nawaf S; Zavala-Araiza, Daniel; Webster, Mort D; Allen, David T

    2013-04-02

    Natural gas use in electricity generation in Texas was estimated, for gas prices ranging from $1.89 to $7.74 per MMBTU, using an optimal power flow model. Hourly estimates of electricity generation, for individual electricity generation units, from the model were used to estimate spatially resolved hourly emissions from electricity generation. Emissions from natural gas production activities in the Barnett Shale region were also estimated, with emissions scaled up or down to match demand in electricity generation as natural gas prices changed. As natural gas use increased, emissions decreased from electricity generation and increased from natural gas production. Overall, NOx and SO2 emissions decreased, while VOC emissions increased as natural gas use increased. To assess the effects of these changes in emissions on ozone and particulate matter concentrations, spatially and temporally resolved emissions were used in a month-long photochemical modeling episode. Over the month-long photochemical modeling episode, decreases in natural gas prices typical of those experienced from 2006 to 2012 led to net regional decreases in ozone (0.2-0.7 ppb) and fine particulate matter (PM) (0.1-0.7 μg/m(3)). Changes in PM were predominantly due to changes in regional PM sulfate formation. Changes in regional PM and ozone formation are primarily due to decreases in emissions from electricity generation. Increases in emissions from increased natural gas production were offset by decreasing emissions from electricity generation for all the scenarios considered.

  18. Marine actinobacteria associated with marine organisms and their potentials in producing pharmaceutical natural products.

    Science.gov (United States)

    Valliappan, Karuppiah; Sun, Wei; Li, Zhiyong

    2014-09-01

    Actinobacteria are ubiquitous in the marine environment, playing an important ecological role in the recycling of refractory biomaterials and producing novel natural products with pharmic applications. Actinobacteria have been detected or isolated from the marine creatures such as sponges, corals, mollusks, ascidians, seaweeds, and seagrass. Marine organism-associated actinobacterial 16S rRNA gene sequences, i.e., 3,003 sequences, deposited in the NCBI database clearly revealed enormous numbers of actinobacteria associated with marine organisms. For example, RDP classification of these sequences showed that 112 and 62 actinobacterial genera were associated with the sponges and corals, respectively. In most cases, it is expected that these actinobacteria protect the host against pathogens by producing bioactive compounds. Natural products investigation and functional gene screening of the actinobacteria associated with the marine organisms revealed that they can synthesize numerous natural products including polyketides, isoprenoids, phenazines, peptides, indolocarbazoles, sterols, and others. These compounds showed anticancer, antimicrobial, antiparasitic, neurological, antioxidant, and anti-HIV activities. Therefore, marine organism-associated actinobacteria represent an important resource for marine drugs. It is an upcoming field of research to search for novel actinobacteria and pharmaceutical natural products from actinobacteria associated with the marine organisms. In this review, we attempt to summarize the present knowledge on the diversity and natural products production of actinobacteria associated with the marine organisms, based on the publications from 1991 to 2013.

  19. Genome mining unveils widespread natural product biosynthetic capacity in human oral microbe Streptococcus mutans

    Science.gov (United States)

    Liu, Liwei; Hao, Tingting; Xie, Zhoujie; Horsman, Geoff P.; Chen, Yihua

    2016-01-01

    Streptococcus mutans is a major pathogen causing human dental caries. As a Gram-positive bacterium with a small genome (about 2 Mb) it is considered a poor source of natural products. Due to a recent explosion in genomic data available for S. mutans strains, we were motivated to explore the natural product production potential of this organism. Bioinformatic characterization of 169 publically available genomes of S. mutans from human dental caries revealed a surprisingly rich source of natural product biosynthetic gene clusters. Anti-SMASH analysis identified one nonribosomal peptide synthetase (NRPS) gene cluster, seven polyketide synthase (PKS) gene clusters and 136 hybrid PKS/NRPS gene clusters. In addition, 211 ribosomally synthesized and post-translationally modified peptides (RiPPs) clusters and 615 bacteriocin precursors were identified by a combined analysis using BAGEL and anti-SMASH. S. mutans harbors a rich and diverse natural product genetic capacity, which underscores the importance of probing the human microbiome and revisiting species that have traditionally been overlooked as “poor” sources of natural products. PMID:27869143

  20. Construction of a microbial natural product library for chemical biology studies.

    Science.gov (United States)

    Kato, Naoki; Takahashi, Shunji; Nogawa, Toshihiko; Saito, Tamio; Osada, Hiroyuki

    2012-04-01

    The RIKEN Natural Products Depository (NPDepo) is a public depository of small molecules. Currently, the NPDepo chemical library contains 39,200 pure compounds, half of which are natural products and their derivatives. In order to reinforce the uniqueness of our chemical library, we have improved our strategies for the collection of microbial natural products. Firstly, a microbial metabolite fraction library coupled with an MP (microbial products) plot database provides a powerful resource for the efficient isolation of microbial metabolites. Secondly, biosynthetic studies of microbial metabolites have enabled us to not only access ingenious biosynthetic machineries, but also obtain a variety of biosynthetic intermediates. Our chemical library contributes to the discovery of molecular probes for increasing our understanding of complex biological processes and for eventually developing new drug leads.

  1. Volatile organic compound emissions from unconventional natural gas production: Source signatures and air quality impacts

    Science.gov (United States)

    Swarthout, Robert F.

    Advances in horizontal drilling and hydraulic fracturing over the past two decades have allowed access to previously unrecoverable reservoirs of natural gas and led to an increase in natural gas production. Intensive unconventional natural gas extraction has led to concerns about impacts on air quality. Unconventional natural gas production has the potential to emit vast quantities of volatile organic compounds (VOCs) into the atmosphere. Many VOCs can be toxic, can produce ground-level ozone or secondary organic aerosols, and can impact climate. This dissertation presents the results of experiments designed to validate VOC measurement techniques, to quantify VOC emission rates from natural gas sources, to identify source signatures specific to natural gas emissions, and to quantify the impacts of these emissions on potential ozone formation and human health. Measurement campaigns were conducted in two natural gas production regions: the Denver-Julesburg Basin in northeast Colorado and the Marcellus Shale region surrounding Pittsburgh, Pennsylvania. An informal measurement intercomparison validated the canister sampling methodology used throughout this dissertation for the measurement of oxygenated VOCs. Mixing ratios of many VOCs measured during both campaigns were similar to or higher than those observed in polluted cities. Fluxes of natural gas-associated VOCs in Colorado ranged from 1.5-3 times industry estimates. Similar emission ratios relative to propane were observed for C2-C6 alkanes in both regions, and an isopentane:n-pentane ratio ≈1 was identified as a unique tracer for natural gas emissions. Source apportionment estimates indicated that natural gas emissions were responsible for the majority of C2-C8 alkanes observed in each region, but accounted for a small proportion of alkenes and aromatic compounds. Natural gas emissions in both regions accounted for approximately 20% of hydroxyl radical reactivity, which could hinder federal ozone standard

  2. NPCARE: database of natural products and fractional extracts for cancer regulation.

    Science.gov (United States)

    Choi, Hwanho; Cho, Sun Young; Pak, Ho Jeong; Kim, Youngsoo; Choi, Jung-Yun; Lee, Yoon Jae; Gong, Byung Hee; Kang, Yeon Seok; Han, Taehoon; Choi, Geunbae; Cho, Yeeun; Lee, Soomin; Ryoo, Dekwoo; Park, Hwangseo

    2017-01-01

    Natural products have increasingly attracted much attention as a valuable resource for the development of anticancer medicines due to the structural novelty and good bioavailability. This necessitates a comprehensive database for the natural products and the fractional extracts whose anticancer activities have been verified. NPCARE (http://silver.sejong.ac.kr/npcare) is a publicly accessible online database of natural products and fractional extracts for cancer regulation. At NPCARE, one can explore 6578 natural compounds and 2566 fractional extracts isolated from 1952 distinct biological species including plants, marine organisms, fungi, and bacteria whose anticancer activities were validated with 1107 cell lines for 34 cancer types. Each entry in NPCARE is annotated with the cancer type, genus and species names of the biological resource, the cell line used for demonstrating the anticancer activity, PubChem ID, and a wealth of information about the target gene or protein. Besides the augmentation of plant entries up to 743 genus and 197 families, NPCARE is further enriched with the natural products and the fractional extracts of diverse non-traditional biological resources. NPCARE is anticipated to serve as a dominant gateway for the discovery of new anticancer medicines due to the inclusion of a large number of the fractional extracts as well as the natural compounds isolated from a variety of biological resources.

  3. Recreational drug discovery: natural products as lead structures for the synthesis of smart drugs.

    Science.gov (United States)

    Appendino, Giovanni; Minassi, Alberto; Taglialatela-Scafati, Orazio

    2014-07-01

    Covering: up to December 2013. Over the past decade, there has been a growing transition in recreational drugs from natural materials (marijuana, hashish, opium), natural products (morphine, cocaine), or their simple derivatives (heroin), to synthetic agents more potent than their natural prototypes, which are sometimes less harmful in the short term, or that combine properties from different classes of recreational prototypes. These agents have been named smart drugs, and have become popular both for personal consumption and for collective intoxication at rave parties. The reasons for this transition are varied, but are mainly regulatory and commercial. New analogues of known illegal intoxicants are invisible to most forensic detection techniques, while the alleged natural status and the lack of avert acute toxicity make them appealing to a wide range of users. On the other hand, the advent of the internet has made possible the quick dispersal of information among users and the on-line purchase of these agents and/or the precursors for their synthesis. Unlike their natural products chemotypes (ephedrine, mescaline, cathinone, psilocybin, THC), most new drugs of abuse are largely unfamiliar to the organic chemistry community as well as to health care providers. To raise awareness of the growing plague of smart drugs we have surveyed, in a medicinal chemistry fashion, their development from natural products leads, their current methods of production, and the role that clandestine home laboratories and underground chemists have played in the surge of popularity of these drugs.

  4. Potential of marine natural products against drug-resistant fungal, viral, and parasitic infections.

    Science.gov (United States)

    Abdelmohsen, Usama Ramadan; Balasubramanian, Srikkanth; Oelschlaeger, Tobias A; Grkovic, Tanja; Pham, Ngoc B; Quinn, Ronald J; Hentschel, Ute

    2017-02-01

    Antibiotics have revolutionised medicine in many aspects, and their discovery is considered a turning point in human history. However, the most serious consequence of the use of antibiotics is the concomitant development of resistance against them. The marine environment has proven to be a very rich source of diverse natural products with significant antibacterial, antifungal, antiviral, antiparasitic, antitumour, anti-inflammatory, antioxidant, and immunomodulatory activities. Many marine natural products (MNPs)-for example, neoechinulin B-have been found to be promising drug candidates to alleviate the mortality and morbidity rates caused by drug-resistant infections, and several MNP-based anti-infectives have already entered phase 1, 2, and 3 clinical trials, with six approved for usage by the US Food and Drug Administration and one by the EU. In this Review, we discuss the diversity of marine natural products that have shown in-vivo efficacy or in-vitro potential against drug-resistant infections of fungal, viral, and parasitic origin, and describe their mechanism of action. We highlight the drug-like physicochemical properties of the reported natural products that have bioactivity against drug-resistant pathogens in order to assess their drug potential. Difficulty in isolation and purification procedures, toxicity associated with the active compound, ecological impacts on natural environment, and insufficient investments by pharmaceutical companies are some of the clear reasons behind market failures and a poor pipeline of MNPs available to date. However, the diverse abundance of natural products in the marine environment could serve as a ray of light for the therapy of drug-resistant infections. Development of resistance-resistant antibiotics could be achieved via the coordinated networking of clinicians, microbiologists, natural product chemists, and pharmacologists together with pharmaceutical venture capitalist companies. Copyright © 2017 Elsevier Ltd

  5. Natural Products Induce a G Protein-Mediated Calcium Pathway Activating p53 in Cancer Cells

    Science.gov (United States)

    van Ginkel, Paul R.; Yan, Michael B.; Bhattacharya, Saswati; Polans, Arthur S.; Kenealey, Jason D.

    2015-01-01

    Paclitaxel, etoposide, vincristine and doxorubicin are examples of natural products being used as chemotherapeutics but with adverse side effects that limit their therapeutic window. Natural products derived from plants and having low toxicity, such as quercetin, resveratrol, epigallocatechin gallate and piceatannol, have been shown to inhibit tumor cell growth both in vitro and in pre-clinical models of cancer, but their mechanisms of action have not been fully elucidated, thus restricting their use as prototypes for developing synthetic analogs with improved anti-cancer properties. We and others have demonstrated that one of the earliest and consistent events upon exposure of tumor cells to these less toxic natural products is a rise in cytoplasmic calcium, activating several pro-apoptotic pathways. We describe here a G protein/inositol 1,4,5-trisphosphate pathway (InsP3) in MDA-MB-231 human breast cancer cells that mediates between these less toxic natural products and the release of calcium from the endoplasmic reticulum. Further, we demonstrate that this elevation of intracellular calcium modulates p53 activity and the subsequent transcription of several pro-apoptotic genes encoding PIG8, CD95, PIDD, TP53INP, RRM2B, Noxa, p21 and PUMA. We conclude from our findings that less toxic natural products likely bind to a G protein coupled receptor that activates a G protein-mediated and calcium-dependent pathway resulting selectively in tumor cell death. PMID:26341291

  6. Something old, something new: revisiting natural products in antibiotic drug discovery.

    Science.gov (United States)

    Wright, Gerard D

    2014-03-01

    Antibiotic discovery is in crisis. Despite a growing need for new drugs resulting from the increasing number of multi-antibiotic-resistant pathogens, there have been only a handful of new antibiotics approved for clinical use in the past 2 decades. Faced with scientific, economic, and regulatory challenges, the pharmaceutical sector seems unable to respond to what has been called an "apocalyptic" threat. Natural products produced by bacteria and fungi are genetically encoded products of natural selection that have been the mainstay sources of the antibiotics in current clinical use. The pharmaceutical industry has largely abandoned these compounds in favor of large libraries of synthetic molecules because of difficulties in identifying new natural product antibiotics scaffolds. Advances in next-generation genome sequencing, bioinformatics, and analytical chemistry are combining to overcome barriers to natural products. Coupled with new strategies in antibiotic discovery, including inhibition of resistance, novel drug combinations, and new targets, natural products are poised for a renaissance to address what is a pressing health care crisis.

  7. Natural products induce a G protein-mediated calcium pathway activating p53 in cancer cells.

    Science.gov (United States)

    van Ginkel, Paul R; Yan, Michael B; Bhattacharya, Saswati; Polans, Arthur S; Kenealey, Jason D

    2015-11-01

    Paclitaxel, etoposide, vincristine and doxorubicin are examples of natural products being used as chemotherapeutics but with adverse side effects that limit their therapeutic window. Natural products derived from plants and having low toxicity, such as quercetin, resveratrol, epigallocatechin gallate and piceatannol, have been shown to inhibit tumor cell growth both in vitro and in pre-clinical models of cancer, but their mechanisms of action have not been fully elucidated, thus restricting their use as prototypes for developing synthetic analogs with improved anti-cancer properties. We and others have demonstrated that one of the earliest and consistent events upon exposure of tumor cells to these less toxic natural products is a rise in cytoplasmic calcium, activating several pro-apoptotic pathways. We describe here a G protein/inositol 1,4,5-trisphosphate pathway (InsP3) in MDA-MB-231 human breast cancer cells that mediates between these less toxic natural products and the release of calcium from the endoplasmic reticulum. Further, we demonstrate that this elevation of intracellular calcium modulates p53 activity and the subsequent transcription of several pro-apoptotic genes encoding PIG8, CD95, PIDD, TP53INP, RRM2B, Noxa, p21 and PUMA. We conclude from our findings that less toxic natural products likely bind to a G protein coupled receptor that activates a G protein-mediated and calcium-dependent pathway resulting selectively in tumor cell death.

  8. Chemical proteomics approaches for identifying the cellular targets of natural products.

    Science.gov (United States)

    Wright, M H; Sieber, S A

    2016-05-01

    Covering: 2010 up to 2016Deconvoluting the mode of action of natural products and drugs remains one of the biggest challenges in chemistry and biology today. Chemical proteomics is a growing area of chemical biology that seeks to design small molecule probes to understand protein function. In the context of natural products, chemical proteomics can be used to identify the protein binding partners or targets of small molecules in live cells. Here, we highlight recent examples of chemical probes based on natural products and their application for target identification. The review focuses on probes that can be covalently linked to their target proteins (either via intrinsic chemical reactivity or via the introduction of photocrosslinkers), and can be applied "in situ" - in living systems rather than cell lysates. We also focus here on strategies that employ a click reaction, the copper-catalysed azide-alkyne cycloaddition reaction (CuAAC), to allow minimal functionalisation of natural product scaffolds with an alkyne or azide tag. We also discuss 'competitive mode' approaches that screen for natural products that compete with a well-characterised chemical probe for binding to a particular set of protein targets. Fuelled by advances in mass spectrometry instrumentation and bioinformatics, many modern strategies are now embracing quantitative proteomics to help define the true interacting partners of probes, and we highlight the opportunities this rapidly evolving technology provides in chemical proteomics. Finally, some of the limitations and challenges of chemical proteomics approaches are discussed.

  9. Metabolomic application in toxicity evaluation and toxicological biomarker identification of natural product.

    Science.gov (United States)

    Chen, Dan-Qian; Chen, Hua; Chen, Lin; Tang, Dan-Dan; Miao, Hua; Zhao, Ying-Yong

    2016-05-25

    Natural product plays a vital role in disease prevention and treatment since the appearance of civilization, but the toxicity severely hinders its wide use. In order to avoid toxic effect as far as possible and use natural product safely, more comprehensive understandings of toxicity are urgently required. Since the metabolome represents the physiological or pathological status of organisms, metabolomics-based toxicology is of significance to observe potential injury before toxins have caused physiological or pathological damages. Metabolomics-based toxicology can evaluate toxicity and identify toxicological biomarker of natural product, which is helpful to guide clinical medication and reduce adverse drug reactions. In the past decades, dozens of metabolomic researches have been implemented on toxicity evaluation, toxicological biomarker identification and potential mechanism exploration of nephrotoxicity, hepatotoxicity, cardiotoxicity and central nervous system toxicity induced by pure compounds, extracts and compound prescriptions. In this paper, metabolomic technology, sample preparation, data process and analysis, and metabolomics-based toxicological research of natural product are reviewed, and finally, the potential problems and further perspectives in toxicological metabolomic investigations of natural product are discussed.

  10. Antimicrobial susceptibility of foodborne pathogens in organic or natural production systems: an overview.

    Science.gov (United States)

    Jacob, Megan E; Fox, James Trent; Reinstein, Shelby L; Nagaraja, T G

    2008-12-01

    Organic and natural food production systems are increasing in popularity, at least partially because consumers perceive that these niche markets provide healthier and safer food products. One major difference between these niche markets and conventional production systems is the use of antimicrobials. Because antimicrobial agents exert selective pressures for antimicrobial resistance, relating antimicrobial susceptibility of foodborne bacteria to niche market production systems is of interest. Other differences between production systems might also influence the susceptibility of foodborne pathogens. The objective of this review is to compare the impact of food animal production systems on the antimicrobial susceptibility of common foodborne bacterial pathogens. Studies comparing the susceptibility of such pathogens were diverse in terms of geographic location, procedures, species of bacteria, and antimicrobials evaluated; thus, it was difficult to draw conclusions. The literature is highly variable in terms of production type and practices and susceptibility associations, although few studies have compared truly organic and conventional practices. When statistical associations were found between production type and minimum inhibitory concentrations or percentage of isolates resistant for a particular pathogen, the isolates from conventionally reared animals/products were more commonly resistant than the comparison group (organic, antibiotic free, etc.). Therefore, further studies are needed to better assess public health consequences of antimicrobial resistance and food animal production systems, specifically organic or natural versus conventional.

  11. Natural Resources and Local Development: The Argentinian Oilseed Complex and Biofuel Production

    Directory of Open Access Journals (Sweden)

    Eliana Scialabba

    2014-01-01

    Full Text Available Argentina is very rich in natural resources, particularly those linked to the oilseed production. Global demand and improved means of production, have resulted in a mature and developed production infrastructure geared toward export. This generates not just revenue, but also has other positive effects, such as the creation of jobs and sustainable development. In this context, biofuel production adds multidimensional value to the vegetable oil industry and generations many spin-off industries.

  12. Recent Advances in the Development of Antineoplastic Agents Derived from Natural Products.

    Science.gov (United States)

    Trendowski, Matthew

    2015-11-01

    Through years of evolutionary selection pressures, organisms have developed potent toxins that coincidentally have marked antineoplastic activity. These natural products have been vital for the development of multiagent treatment regimens currently employed in cancer chemotherapy, and are used in the treatment of a variety of malignancies. Therefore, this review catalogs recent advances in natural product-based drug discovery via the examination of mechanisms of action and available clinical data to highlight the utility of these novel compounds in the burgeoning age of precision medicine. The review also highlights the recent development of antibody-drug conjugates and other immunotoxins, which are capable of delivering highly cytotoxic agents previously deemed too toxic to elicit therapeutic benefit preferentially to neoplastic cells. Finally, the review examines natural products not currently used in the clinic that have novel mechanisms of action, and may serve to supplement current chemotherapeutic protocols.

  13. Quality not Quantity: The Role of Marine Natural Products in Drug Discovery and Reverse Chemical Proteomics

    Directory of Open Access Journals (Sweden)

    Andrew M. Piggott

    2005-06-01

    Full Text Available Reverse chemical proteomics combines affinity chromatography with phage display and promises to be a powerful new platform technology for the isolation of natural product receptors, facilitating the drug discovery process by rapidly linking biologically active small molecules to their cellular receptors and the receptors’ genes. In this paper we review chemical proteomics and reverse chemical proteomics and show how these techniques can add value to natural products research. We also report on techniques for the derivatisation of polystyrene microtitre plates with cleavable linkers and marine natural products that can be used in chemical proteomics or reverse chemical proteomics. Specifically, we have derivatised polystyrene with palau’amine and used reverse chemical proteomics to try and isolate the human receptors for this potent anticancer marine drug.

  14. Functional chromatography reveals three natural products that target the same protein with distinct mechanisms of action

    Science.gov (United States)

    Kang, MinJin; Wu, Tongde; Wijeratne, E. M. Kithsiri; Lau, Eric C.; Mason, Damian J.; Mesa, Celestina; Tillotson, Joseph; Zhang, Donna D.; Gunatilaka, A. A. Leslie; La Clair, James J.

    2014-01-01

    Access to lead compounds with defined molecular targets continues to be a barrier to the translation of natural product resources. As a solution, we have developed a system that uses discreet, recombinant proteins as the vehicles for natural product isolation. Here, we describe the use of this functional chromatographic method to identify natural products that bind to the AAA+ chaperone, p97, a promising cancer target. Application of this method to a panel of fungal and plant extracts identified rheoemodin, 1-hydroxydehydroherbarin and phomapyrrolidone A as distinct p97 modulators. Excitingly, each of these molecules displayed a unique mechanism of p97 modulation. This discovery provides strong support for the application of functional chromatography to the discovery of protein modulators that would likely escape traditional high-throughput or phenotypic screening platforms. PMID:25125376

  15. Towards theory driven structure elucidation of complex natural products: mandelalides and coibamide A.

    Science.gov (United States)

    Snyder, Kevin M; Sikorska, Justyna; Ye, Tao; Fang, Lijing; Su, Wu; Carter, Rich G; McPhail, Kerry L; Cheong, Paul H-Y

    2016-06-28

    The effectiveness of computational tools in determining relative configurations of complex molecules is investigated, using natural products mandelalides A-D and coibamide A, towards a generalized recipe for the scientific community at large. Ultimately, continuing efforts in this vein will accelerate and strengthen relative structure elucidation of complex molecules, such as natural products. Molecular mechanics conformational search, quantum mechanical NMR chemical shift predictions, and DP4 analyses led to confirmation of the revised structures of mandelalides A-D and coibamide A. All chiral centers in the northern hemisphere of mandelalides A-D are inverted with respect to the originally proposed structures, in agreement with recent total syntheses of mandelalide A by Ye, Fürstner & Carter. In the case of coibamide A, it was found that Fang & Su's revision, in which both the macrocycle [MeAla(11)] and the side chain [HIV(2)] residues are inverted from l to d, was consistent with the authentic natural product and computations.

  16. Natural Products Mediated Regulation of Oxidative Stress and DNA Damage in Ultraviolet Exposed Skin Cells.

    Science.gov (United States)

    Farooqi, Ammad A; Li, Ruei-Nian; Huang, Hurng-Wern; Ismail, Muhammad; Yuan, Shyng-Shiou F; Wang, Hui-Min D; Liu, Jing-Ru; Tang, Jen-Yang; Chang, Hsueh-Wei

    2015-01-01

    Data obtained through high-throughput technologies have gradually revealed that a unique stratified epithelial architecture of human skin along with the antioxidant-response pathways provided vital defensive mechanisms against UV radiation. However, it is noteworthy that skin is a major target for toxic insult by UV radiations that can alter its structure and function. Substantial fraction of information has been added into the existing pool of knowledge related to natural products mediated biological effects in UV exposed skin cells. Accumulating evidence has started to shed light on the potential of these bioactive ingredients as protective natural products in cosmetics against UV photodamage by exerting biological effects mainly through wide ranging intracellular signalling cascades of oxidative stress and modulation of miRNAs. In this review, we have summarized recently emerging scientific evidences addressing underlying mechanisms of UV induced oxidative stress and deregulation of signalling cascades and how natural products can be used tactfully to protect against UV induced harmful effects.

  17. An assessment of natural product discovery from marine (sensu strictu) and marine-derived fungi

    Science.gov (United States)

    Overy, David P.; Bayman, Paul; Kerr, Russell G.; Bills, Gerald F.

    2014-01-01

    The natural products community has been investigating secondary metabolites from marine fungi for several decades, but when one attempts to search for validated reports of new natural products from marine fungi, one encounters a literature saturated with reports from ‘marine-derived’ fungi. Of the 1000+ metabolites that have been characterized to date, only approximately 80 of these have been isolated from species from exclusively marine lineages. These metabolites are summarized here along with the lifestyle and habitats of their producing organisms. Furthermore, we address some of the reasons for the apparent disconnect between the stated objectives of discovering new chemistry from marine organisms and the apparent neglect of the truly exceptional obligate marine fungi. We also offer suggestions on how to reinvigorate enthusiasm for marine natural products discovery from fungi from exclusive marine lineages and highlight the need for critically assessing the role of apparently terrestrial fungi in the marine environment. PMID:25379338

  18. Exploring Natural Products as a Source for Antidiabetic Lead Compounds and Possible Lead Optimization.

    Science.gov (United States)

    Khalaf, Reema Abu

    2016-01-01

    Natural products are characterized by their chemical diversity and being a good source of a range of bioactive structures including antidiabetic compounds. Diabetes mellitus (DM) is considered a major worldwide health concern. Rational drug design has been widely accomplished, to discover and optimize innovative leads for different molecular targets of type 2 DM including α-glucosidase, PPARγ, DPP-IV, PTP1B, AR, GSK-3β, 11β-HSD1, GK, etc. This review illustrates the potential of natural products as a rich source of lead compounds for antidiabetic drug discovery with some examples of computational studies carried out to determine the possible molecular target, structure activity relationship, and further optimization chances. Natural products will remain an attractive source for researchers to explore their therapeutic potential against DM. Guided by the computational studies; systematic lead optimization via structural modifications will speed up the generation of potential new clinical candidates for the treatment of type 2 DM.

  19. Current Perspective in the Discovery of Anti-aging Agents from Natural Products.

    Science.gov (United States)

    Ding, Ai-Jun; Zheng, Shan-Qing; Huang, Xiao-Bing; Xing, Ti-Kun; Wu, Gui-Sheng; Sun, Hua-Ying; Qi, Shu-Hua; Luo, Huai-Rong

    2017-05-31

    Aging is a process characterized by accumulating degenerative damages, resulting in the death of an organism ultimately. The main goal of aging research is to develop therapies that delay age-related diseases in human. Since signaling pathways in aging of Caenorhabditis elegans (C. elegans), fruit flies and mice are evolutionarily conserved, compounds extending lifespan of them by intervening pathways of aging may be useful in treating age-related diseases in human. Natural products have special resource advantage and with few side effect. Recently, many compounds or extracts from natural products slowing aging and extending lifespan have been reported. Here we summarized these compounds or extracts and their mechanisms in increasing longevity of C. elegans or other species, and the prospect in developing anti-aging medicine from natural products.

  20. Sansanmycin natural product analogues as potent and selective anti-mycobacterials that inhibit lipid I biosynthesis

    Science.gov (United States)

    Tran, Anh T.; Watson, Emma E.; Pujari, Venugopal; Conroy, Trent; Dowman, Luke J.; Giltrap, Andrew M.; Pang, Angel; Wong, Weng Ruh; Linington, Roger G.; Mahapatra, Sebabrata; Saunders, Jessica; Charman, Susan A.; West, Nicholas P.; Bugg, Timothy D. H.; Tod, Julie; Dowson, Christopher G.; Roper, David I.; Crick, Dean C.; Britton, Warwick J.; Payne, Richard J.

    2017-03-01

    Tuberculosis (TB) is responsible for enormous global morbidity and mortality, and current treatment regimens rely on the use of drugs that have been in use for more than 40 years. Owing to widespread resistance to these therapies, new drugs are desperately needed to control the TB disease burden. Herein, we describe the rapid synthesis of analogues of the sansanmycin uridylpeptide natural products that represent promising new TB drug leads. The compounds exhibit potent and selective inhibition of Mycobacterium tuberculosis, the etiological agent of TB, both in vitro and intracellularly. The natural product analogues are nanomolar inhibitors of Mtb phospho-MurNAc-pentapeptide translocase, the enzyme responsible for the synthesis of lipid I in mycobacteria. This work lays the foundation for the development of uridylpeptide natural product analogues as new TB drug candidates that operate through the inhibition of peptidoglycan biosynthesis.