WorldWideScience

Sample records for diosgenin

  1. Diosgenin hemihydrate

    Directory of Open Access Journals (Sweden)

    María-Guadalupe Hernández Linares

    2012-08-01

    Full Text Available Diosgenin [or (22R,25R-spirost-5-en-3β-ol] is the starting material of the Marker degradation, a cheap semi-synthesis of progesterone, which has been designated as an International Historic Chemical Landmark. Thus far, a single X-ray structure for diosgenin is known, namely its dimethyl sulfoxide solvate [Zhang et al. (2005. Acta Cryst. E61, o2324–o2325]. We have now determined the structure of the hemihydrate, C27H42O3·0.5H2O. The asymmetric unit contains two diosgenin molecules, with quite similar conformations, and one water molecule. Hydroxy groups in steroids and water molecules form O—H...O hydrogen-bonded R54(10 ring motifs. Fused edge-sharing R(10 rings form a backbone oriented along [100], which aggregates the diosgenin molecules in the crystal structure.

  2. HPTLC determination of diosgenin in fenugreek seeds

    Directory of Open Access Journals (Sweden)

    Król-Kogus Barbara

    2018-03-01

    Full Text Available A new HPTLC-densitometric method for diosgenin determination in fenugreek seeds was established after optimization of the conditions for efficient saponin extraction and acid hydrolysis. Several procedures were tested, the best of which was a three-step Soxhlet extraction, followed by hydrolysis of the obtained methanolic extract with 2 mol L-1 H2SO4. Best diosgenin separation from other hydrolysis products was obtained on HPTLC Si60F254 plates u sing a mixture of n-heptane/ethyl acetate (7:3, V/V and modified anisaldehyde as a spraying reagent. The method was preliminarily validated and the determined amounts of diosgenin in fenugreek seeds of Polish and African origin were found to be similar and ranged from 0.12-0.18 %.

  3. Cancer chemopreventive and therapeutic effects of diosgenin, a food saponin.

    Science.gov (United States)

    Raju, Jayadev; Mehta, Rekha

    2009-01-01

    Cancer chemoprevention is a strategy taken to retard, regress, or resist the multistep process of carcinogenesis, including the blockage of its vital morphogenetic milestones viz. normal-preneoplasia-neoplasia-metastasis. For several reasons, including safety, minimal (or no) toxicity and side-effects, and better availability, alternatives such as naturally occurring phytochemicals that are found in foods are becoming increasingly popular over synthetic drugs. Food saponins have been used in complimentary and traditional medicine against a variety of diseases including several cancers. Diosgenin, a naturally occurring steroid saponin found abundantly in legumes and yams, is a well-known precursor of various synthetic steroidal drugs that are extensively used in the pharmaceutical industry. Over the past decade, a series of preclinical and mechanistic studies have been conducted to understand the role of diosgenin as a chemopreventive/therapeutic agent against several cancers. This review highlights the biological activity of diosgenin that contributes to cancer chemoprevention and control. The anticancer mode of action of diosgenin has been demonstrated via modulation of multiple cell signaling events involving critical molecular candidates associated with growth, differentiation, apoptosis, and oncogenesis. Altogether, these preclinical and mechanistic findings strongly implicate the use of diosgenin as a novel, multitarget-based chemopreventive or therapeutic agent against several cancer types. Future research in this field will help to establish not only whether diosgenin is safe and efficacious as a chemopreventive agent against several human cancers, but also to develop and evaluate standards of evidence for health claims for diosgenin-containing foods as they become increasingly popular and enter the marketplace labeled as functional foods and nutraceuticals.

  4. Diosgenin induces apoptosis in IGF-1-stimulated human thyrocytes through two caspase-dependent pathways

    International Nuclear Information System (INIS)

    Mu, Shumin; Tian, Xingsong; Ruan, Yongwei; Liu, Yuantao; Bian, Dezhi; Ma, Chunyan; Yu, Chunxiao; Feng, Mei; Wang, Furong; Gao, Ling; Zhao, Jia-jun

    2012-01-01

    Highlights: ► Diosgenin induces apoptosis in IGF-1-treated thyrocytes through two caspase pathways. ► Diosgenin inhibits FLIP and activates caspase-8 in FAS related-pathway. ► Diosgenin increases ROS, regulates the ratio of Bax/Bcl-2 in mitochondrial pathway. -- Abstract: Insulin-like growth factor-1 (IGF-1) is a growth factor of the thyroid that has been shown in our previous study to possess proliferative and antiapoptotic effects in FRTL-5 cell lines through the upregulation of cyclin D and Fas-associated death domain-like interleukin-1-converting enzyme (FLICE)-inhibitory protein (FLIP). Diosgenin, a natural steroid sapogenin from plants, has been shown to induce apoptosis in many cell lines, with the exception of thyroid cells. In this report, we investigated the apoptotic effect and mechanism of diosgenin in IGF-1-stimulated primary human thyrocytes. Primary human thyrocytes were preincubated with or without IGF-1 for 24 h and subsequently exposed to varying concentrations of diosgenin for different times. We found that diosgenin induced apoptosis in human thyrocytes pretreated with IGF-1 in a dose-dependent manner through the activation of caspase cascades. Moreover, diosgenin inhibited FLIP and activated caspase-8 in the FAS-related apoptotic pathway. Diosgenin increased the production of ROS, regulated the balance of Bax and Bcl-2 and cleaved caspase-9 in the mitochondrial apoptotic pathway. These results indicate that diosgenin induces apoptosis in IGF-1-stimulated primary human thyrocytes through two caspase-dependent pathways.

  5. Diosgenin induces apoptosis in IGF-1-stimulated human thyrocytes through two caspase-dependent pathways

    Energy Technology Data Exchange (ETDEWEB)

    Mu, Shumin [Provincial Hospital Affiliated to Shandong University, Jinan 250021 (China); Hospital Affiliated to Shandong Traditional Chinese Medicine University, Jinan 250011 (China); Institute of Endocrinology, Shandong Academy of Clinical Medicine, Jinan 250021 (China); Tian, Xingsong; Ruan, Yongwei [Provincial Hospital Affiliated to Shandong University, Jinan 250021 (China); Liu, Yuantao [The Second Hospital of Shandong University, Jinan 250033 (China); Bian, Dezhi [Provincial Hospital Affiliated to Shandong University, Jinan 250021 (China); Jining Medical College, Jining 272013 (China); Ma, Chunyan [Provincial Hospital Affiliated to Shandong University, Jinan 250021 (China); Yu, Chunxiao [Provincial Hospital Affiliated to Shandong University, Jinan 250021 (China); Institute of Endocrinology, Shandong Academy of Clinical Medicine, Jinan 250021 (China); Feng, Mei [Provincial Hospital Affiliated to Shandong University, Jinan 250021 (China); Wang, Furong [Shandong University of Traditional Chinese Medicine, Jinan 250011 (China); Gao, Ling [Provincial Hospital Affiliated to Shandong University, Jinan 250021 (China); Institute of Endocrinology, Shandong Academy of Clinical Medicine, Jinan 250021 (China); Zhao, Jia-jun, E-mail: jjzhao@medmail.com.cn [Provincial Hospital Affiliated to Shandong University, Jinan 250021 (China); Institute of Endocrinology, Shandong Academy of Clinical Medicine, Jinan 250021 (China)

    2012-02-10

    Highlights: Black-Right-Pointing-Pointer Diosgenin induces apoptosis in IGF-1-treated thyrocytes through two caspase pathways. Black-Right-Pointing-Pointer Diosgenin inhibits FLIP and activates caspase-8 in FAS related-pathway. Black-Right-Pointing-Pointer Diosgenin increases ROS, regulates the ratio of Bax/Bcl-2 in mitochondrial pathway. -- Abstract: Insulin-like growth factor-1 (IGF-1) is a growth factor of the thyroid that has been shown in our previous study to possess proliferative and antiapoptotic effects in FRTL-5 cell lines through the upregulation of cyclin D and Fas-associated death domain-like interleukin-1-converting enzyme (FLICE)-inhibitory protein (FLIP). Diosgenin, a natural steroid sapogenin from plants, has been shown to induce apoptosis in many cell lines, with the exception of thyroid cells. In this report, we investigated the apoptotic effect and mechanism of diosgenin in IGF-1-stimulated primary human thyrocytes. Primary human thyrocytes were preincubated with or without IGF-1 for 24 h and subsequently exposed to varying concentrations of diosgenin for different times. We found that diosgenin induced apoptosis in human thyrocytes pretreated with IGF-1 in a dose-dependent manner through the activation of caspase cascades. Moreover, diosgenin inhibited FLIP and activated caspase-8 in the FAS-related apoptotic pathway. Diosgenin increased the production of ROS, regulated the balance of Bax and Bcl-2 and cleaved caspase-9 in the mitochondrial apoptotic pathway. These results indicate that diosgenin induces apoptosis in IGF-1-stimulated primary human thyrocytes through two caspase-dependent pathways.

  6. Preparation of tritium-labeled diosgenin, esmilagenin and tigogenin

    International Nuclear Information System (INIS)

    Rabinowitz, J.L.; Juarez-Oropeza, M.A.; Diaz Zagoya, J.C.

    1987-01-01

    The synthesis of 3 H -diosgenin, 3 H -esmilagenin and 3 H -tigogenin (three potential hypocholesterolemic agents) was accomplished by low pressure hydrogenation of commercial (Sigma D 1634) diosgenin with 3 H -gas. The mixture of 3 H materials obtained was separated by silica gel G-60 column chromatography by use of a benzene: ethyl acetate (8:2 v/v) solution. Purification of each sapogenin was by TLC chromatography. (author)

  7. Effect of β-cyclodextrin derivatives on the diosgenin absorption in Caco-2 cell monolayer and rats.

    Science.gov (United States)

    Okawara, Masaki; Tokudome, Yoshihiro; Todo, Hiroaki; Sugibayashi, Kenji; Hashimoto, Fumie

    2014-01-01

    Orally administrated diosgenin, a steroidal saponin found in the roots of Dioscorea villosa, improves reduced skin thickness in ovariectomized mice, and plays an important role in the treatment of hyperlipidemia. Diosgenin has been noticed as an active element in cosmeceutical and dietary supplements. We have already elucidated that the absolute oral bioavailability of diosgenin is very low; however, a high skin distribution of diosgenin was also observed. The aim of the present study was to examine and compare the effects of β-cyclodextrin (β-CD) and 3 kinds of its derivatives such as hydroxypropyl β-CD on the diosgenin permeability using a Caco-2 model and rat jejunal perfusion. These derivatives of β-CD greatly improved the low solubility of diosgenin. No significant increase was observed in the lactate dehydrogenase leakage from Caco-2 cell, while a slight decrease was found on the transepithelial electrical resistance by diosgenin and β-CD derivatives. However, β-CD derivatives, especially hydroxyethyl β-CD and hydroxypropyl β-CD, markedly enhanced diosgenin permeability across the Caco-2 monolayer and rat jejunum. The bioavailability of diosgenin in the presence of β-CD derivatives were about 4 to 11 fold higher than diosgenin suspension. The mechanisms of these enhancement effects may be due to improvements in solubility and tight junction opening.

  8. Comparative analysis of diosgenin in Dioscorea species and related medicinal plants by UPLC-DAD-MS.

    Science.gov (United States)

    Yi, Tao; Fan, Lan-Lan; Chen, Hong-Li; Zhu, Guo-Yuan; Suen, Hau-Man; Tang, Yi-Na; Zhu, Lin; Chu, Chu; Zhao, Zhong-Zhen; Chen, Hu-Biao

    2014-08-09

    Dioscorea is a genus of flowering plants, and some Dioscorea species are known and used as a source for the steroidal sapogenin diosgenin. To screen potential resource from Dioscorea species and related medicinal plants for diosgenin extraction, a rapid method to compare the contents of diosgenin in various plants is crucial. An ultra-performance liquid chromatography (UPLC) coupled with diode array detection (DAD) and electrospray ionization mass spectrometry (ESI-MS) method was developed for identification and determination of diosgenin in various plants. A comprehensive validation of the developed method was conducted. Twenty-four batches of plant samples from four Dioscorea species, one Smilax species and two Heterosmilax species were analyzed by using the developed method.The present method presented good sensitivity, precision and accuracy. Diosgenin was found in three Dioscorea species and one Heterosmilax species, namely D. zingiberensis, D. septemloba, D. collettii and H. yunnanensis. The method is suitable for the screening of diosgenin resources from plants. D. zingiberensis is an important resource for diosgenin harvesting.

  9. Diosgenin: Recent Highlights on Pharmacology and Analytical Methodology.

    Science.gov (United States)

    Jesus, Mafalda; Martins, Ana P J; Gallardo, Eugenia; Silvestre, Samuel

    2016-01-01

    Diosgenin, a steroidal sapogenin, occurs abundantly in plants such as Dioscorea alata , Smilax China, and Trigonella foenum graecum . This bioactive phytochemical not only is used as an important starting material for the preparation of several steroidal drugs in the pharmaceutical industry, but has revealed also high potential and interest in the treatment of various types of disorders such as cancer, hypercholesterolemia, inflammation, and several types of infections. Due to its pharmacological and industrial importance, several extraction and analytical procedures have been developed and applied over the years to isolate, detect, and quantify diosgenin, not only in its natural sources and pharmaceutical compositions, but also in animal matrices for pharmacodynamic, pharmacokinetic, and toxicological studies. Within these, HPLC technique coupled to different detectors is the most commonly analytical procedure described for this compound. However, other alternative methods were also published. Thus, the present review aims to provide collective information on the most recent pharmacological data on diosgenin and on the most relevant analytical techniques used to isolate, detect, and quantify this compound as well.

  10. Diosgenin: Recent Highlights on Pharmacology and Analytical Methodology

    Directory of Open Access Journals (Sweden)

    Mafalda Jesus

    2016-01-01

    Full Text Available Diosgenin, a steroidal sapogenin, occurs abundantly in plants such as Dioscorea alata, Smilax China, and Trigonella foenum graecum. This bioactive phytochemical not only is used as an important starting material for the preparation of several steroidal drugs in the pharmaceutical industry, but has revealed also high potential and interest in the treatment of various types of disorders such as cancer, hypercholesterolemia, inflammation, and several types of infections. Due to its pharmacological and industrial importance, several extraction and analytical procedures have been developed and applied over the years to isolate, detect, and quantify diosgenin, not only in its natural sources and pharmaceutical compositions, but also in animal matrices for pharmacodynamic, pharmacokinetic, and toxicological studies. Within these, HPLC technique coupled to different detectors is the most commonly analytical procedure described for this compound. However, other alternative methods were also published. Thus, the present review aims to provide collective information on the most recent pharmacological data on diosgenin and on the most relevant analytical techniques used to isolate, detect, and quantify this compound as well.

  11. Diosgenin Induces Apoptosis in HepG2 Cells through Generation of Reactive Oxygen Species and Mitochondrial Pathway

    Directory of Open Access Journals (Sweden)

    Dae Sung Kim

    2012-01-01

    Full Text Available Diosgenin, a naturally occurring steroid saponin found abundantly in legumes and yams, is a precursor of various synthetic steroidal drugs. Diosgenin is studied for the mechanism of its action in apoptotic pathway in human hepatocellular carcinoma cells. Based on DAPI staining, diosgenin-treated cells manifested nuclear shrinkage, condensation, and fragmentation. Treatment of HepG2 cells with 40 μM diosgenin resulted in activation of the caspase-3, -8, -9 and cleavage of poly-ADP-ribose polymerase (PARP and the release of cytochrome c. In the upstream, diosgenin increased the expression of Bax, decreased the expression of Bid and Bcl-2, and augmented the Bax/Bcl-2 ratio. Diosgenin-induced, dose-dependent induction of apoptosis was accompanied by sustained phosphorylation of JNK, p38 MAPK and apoptosis signal-regulating kinase (ASK-1, as well as generation of the ROS. NAC administration, a scavenger of ROS, reversed diosgene-induced cell death. These results suggest that diosgenin-induced apoptosis in HepG2 cells through Bcl-2 protein family-mediated mitochndria/caspase-3-dependent pathway. Also, diosgenin strongly generated ROS and this oxidative stress might induce apoptosis through activation of ASK1, which are critical upstream signals for JNK/p38 MAPK activation in HepG2 cancer cells.

  12. Diosgenin, a steroidal saponin, inhibits migration and invasion of human prostate cancer PC-3 cells by reducing matrix metalloproteinases expression.

    Directory of Open Access Journals (Sweden)

    Pin-Shern Chen

    Full Text Available BACKGROUND: Diosgenin, a steroidal saponin obtained from fenugreek (Trigonella foenum graecum, was found to exert anti-carcinogenic properties, such as inhibiting proliferation and inducing apoptosis in a variety of tumor cells. However, the effect of diosgenin on cancer metastasis remains unclear. The aim of the study is to examine the effect of diosgenin on migration and invasion in human prostate cancer PC-3 cells. METHODS AND PRINCIPAL FINDINGS: Diosgenin inhibited proliferation of PC-3 cells in a dose-dependent manner. When treated with non-toxic doses of diosgenin, cell migration and invasion were markedly suppressed by in vitro wound healing assay and Boyden chamber invasion assay, respectively. Furthermore, diosgenin reduced the activities of matrix metalloproteinase-2 (MMP-2 and MMP-9 by gelatin zymography assay. The mRNA level of MMP-2, -9, -7 and extracellular inducer of matrix metalloproteinase (EMMPRIN were also suppressed while tissue inhibitor of metalloproteinase-2 (TIMP-2 was increased by diosgenin. In addition, diosgenin abolished the expression of vascular endothelial growth factor (VEGF in PC-3 cells and tube formation of endothelial cells. Our immunoblotting assays indicated that diosgenin potently suppressed the phosphorylation of phosphatidylinositide-3 kinase (PI3K, Akt, extracellular signal regulating kinase (ERK and c-Jun N-terminal kinase (JNK. In addition, diosgenin significantly decreased the nuclear level of nuclear factor kappa B (NF-κB, suggesting that diosgenin inhibited NF-κB activity. CONCLUSION/SIGNIFICANCE: The results suggested that diosgenin inhibited migration and invasion of PC-3 cells by reducing MMPs expression. It also inhibited ERK, JNK and PI3K/Akt signaling pathways as well as NF-κB activity. These findings reveal new therapeutic potential for diosgenin in anti-metastatic therapy.

  13. Diosgenin promotes oligodendrocyte progenitor cell differentiation through estrogen receptor-mediated ERK1/2 activation to accelerate remyelination.

    Science.gov (United States)

    Xiao, Lin; Guo, Dazhi; Hu, Chun; Shen, Weiran; Shan, Lei; Li, Cui; Liu, Xiuyun; Yang, Wenjing; Zhang, Weidong; He, Cheng

    2012-07-01

    Differentiation of oligodendrocyte progenitor cells (OPCs) into mature oligodendrocytes is a prerequisite for remyelination after demyelination, and impairment of this process is suggested to be a major reason for remyelination failure. Diosgenin, a plant-derived steroid, has been implicated for therapeutic use in many diseases, but little is known about its effect on the central nervous system. In this study, using a purified rat OPC culture model, we show that diosgenin significantly and specifically promotes OPC differentiation without affecting the viability, proliferation, or migration of OPC. Interestingly, the effect of diosgenin can be blocked by estrogen receptor (ER) antagonist ICI 182780 but not by glucocorticoid and progesterone receptor antagonist RU38486, nor by mineralocorticoid receptor antagonist spirolactone. Moreover, it is revealed that both ER-alpha and ER-beta are expressed in OPC, and diosgenin can activate the extracellular signal-regulated kinase 1/2 (ERK1/2) in OPC via ER. The pro-differentiation effect of diosgenin can also be obstructed by the ERK inhibitor PD98059. Furthermore, in the cuprizone-induced demyelination model, it is demonstrated that diosgenin administration significantly accelerates/enhances remyelination as detected by Luxol fast blue stain, MBP immunohistochemistry and real time RT-PCR. Diosgenin also increases the number of mature oligodendrocytes in the corpus callosum while it does not affect the number of OPCs. Taking together, our results suggest that diosgenin promotes the differentiation of OPC into mature oligodendrocyte through an ER-mediated ERK1/2 activation pathway to accelerate remyelination, which implicates a novel therapeutic usage of this steroidal natural product in demyelinating diseases such as multiple sclerosis (MS). Copyright © 2012 Wiley Periodicals, Inc.

  14. Development of a new certified reference material of diosgenin using mass balance approach and Coulometric titration method.

    Science.gov (United States)

    Gong, Ningbo; Zhang, Baoxi; Hu, Fan; Du, Hui; Du, Guanhua; Gao, Zhaolin; Lu, Yang

    2014-12-01

    Certified reference materials (CRMs) can be used as a valuable tool to validate the trueness of measurement methods and to establish metrological traceability of analytical results. Diosgenin has been selected as a candidate reference material. Characterization of the material relied on two different methods, mass balance method and Coulometric titration method (CT). The certified value of diosgenin CRM is 99.80% with an expanded uncertainty of 0.37% (k=2). The new CRM of diosgenin can be used to validate analytical methods, improve the accuracy of measurement data and control the quality of diosgenin in relevant pharmaceutical formulations. Copyright © 2014 Elsevier Inc. All rights reserved.

  15. Determination and correlation of the solubility for diosgenin in alcohol solvents

    International Nuclear Information System (INIS)

    Chen Feixiong; Zhao Mingrui; Liu Chuochuo; Peng Feifei; Ren Baozeng

    2012-01-01

    Highlights: ► The solubilities of diosgenin in different alcohols solvents have been obtained. ► The solubility decreases with the increase of the polarity of the alcohols solvents. ► The results show that the three models agree well with the experimental data. - Abstract: Using a laser monitoring technique, the solubility of diosgenin in ethanol, 1-propanol, 1-butanol, isobutyl alcohol, tert-butanol, 1-pentanol, and iso-octyl alcohol was measured over the temperature range from (290.15 to 330.15) K at atmospheric pressure. Its corresponding (solid + liquid) equilibrium data will provide essential support for industrial design and further theoretical studies. From the experimental results, the solubility of diosgenin in ethanol, 1-propanol, 1-butanol, isobutyl alcohol, tert-butanol, 1-pentanol, and iso-octyl alcohol was found to increase with increasing temperature and decrease with the increase of the polarity of the alcohols solvents. The Apelblat equation, the ideal model and the λh equation were used to correlate the solubility values. The results showed that the three models mentioned above agreed well with the experimental data.

  16. Enhancement of Diosgenin Production in Plantlet and Cell Cultures ...

    African Journals Online (AJOL)

    Enhancement of Diosgenin Production in Plantlet and Cell Cultures of Dioscorea zingiberensis by Palmarumycin C13 from the Endophytic fungus, Berkleasmium sp. Dzf12. Y Mou, K Zhou, D Xu, R Yu, J Li, C Yin, L Zhou ...

  17. Increased cyclooxygenase-2 and thromboxane synthase expression is implicated in diosgenin-induced megakaryocytic differentiation in human erythroleukemia cells.

    Science.gov (United States)

    Cailleteau, C; Liagre, B; Battu, S; Jayat-Vignoles, C; Beneytout, J L

    2008-09-01

    Differentiation induction as a therapeutic strategy has, so far, the greatest impact in hematopoietic malignancies, most notably leukemia. Diosgenin is a very interesting natural product because, depending on the specific dose used, its biological effect is very different in HEL (human erythroleukemia) cells. For example, at 10 microM, diosgenin induced megakaryocytic differentiation, in contrast to 40 microM diosgenin, which induced apoptosis in HEL cells previously demonstrated using sedimentation field-flow fractionation (SdFFF). The goal of this work focused on the correlation between cyclooxygenase-2 (COX-2) and thromboxane synthase (TxS) and megakaryocytic differentiation induced by diosgenin in HEL cells. Furthermore, the technique of SdFFF, having been validated in our models, was used in this new study as an analytical tool that provided us with more or less enriched differentiated cell fractions that could then be used for further analyses of enzyme protein expression and activity for the first time. In our study, we showed the implication of COX-2 and TxS in diosgenin-induced megakaryocytic differentiation in HEL cells. Furthermore, we showed that the analytical technique of SdFFF may be used as a tool to confirm our results as a function of the degree of cell differentiation.

  18. Anti-Proliferation and Anti-Invasion Effects of Diosgenin on Gastric Cancer BGC-823 Cells with HIF-1α shRNAs

    Directory of Open Access Journals (Sweden)

    Yuan-Neng Chou

    2012-05-01

    Full Text Available Drug resistance is a major factor for the limited efficacy of chemotherapy in gastric cancer treatment. Hypoxia-inducible factor-1α (HIF-1α, a central transcriptional factor in hypoxia, is suggested to participate in the resistance. Here, we identified a hypoxia-mimic (cobalt chloride sensitive gastric cell line BGC-823 to explore whether diosgenin, an aglycone of steroidal saponins, can inhibit cancer cell invasion and survival of solid tumor in a hypoxic mimic microenvironment. We have shown that diosgenin is a potent candidate for decreasing the ability of invasion and survival in cobalt chloride treated BGC-823 cells. In addition, when combined with HIF-1α specific short hairpin RNA (shRNA, diosgenin can inhibit BGC-823 cells more effectively. The anti-invasion role of diosgenin may be related to E-cadherin, integrinα5 and integrinβ6. These results suggest that diosgenin may be a useful compound in controlling gastric cancer cells in hypoxia condition, especially when combined with down-regulated HIF-1α.

  19. Attenuation of Streptozotocin-Induced Lipid Profile Anomalies in the Heart, Brain, and mRNA Expression of HMG-CoA Reductase by Diosgenin in Rats.

    Science.gov (United States)

    Hao, Shuang; Xu, Rihao; Li, Dan; Zhu, Zhicheng; Wang, Tiance; Liu, Kexiang

    2015-07-01

    Diabetes mellitus is associated with significant morbidity and mortality that contributes to pathogenesis of cardiovascular diseases. Diosgenin, a naturally occurring aglycone, is present abundantly in fenugreek. The steroidal saponin is being used as a traditional medicine for diabetes. The present study has investigated the effects of diosgenin on lipid profile in the heart and brain, mRNA expression, and hepatic HMG-CoA reductase (HMGR) activity of streptozotocin-induced diabetic rats. In our study, diosgenin was administered (40 mg/kg b.w.) orally for 45 days to control animals and experimentally induced diabetic rats. The effects of diosgenin on glucose, plasma insulin, cholesterol, triglycerides, free fatty acids, and phospholipids (PLs) in the heart and brain were studied. The levels of glucose, cholesterol, triglycerides, free fatty acids, PLs, and HMGR activity were increased significantly (P rats. Administration of diosgenin to diabetic rats significantly reduced blood glucose, cholesterol, triglycerides, free fatty acids, PLs levels, and also HMGR activity. In addition, the plasma insulin level was increased in diosgenin-treated diabetic rats. The above findings were correlated with histological observations of the heart and brain. The results showed that administration of diosgenin remarkably increased plasma insulin level with absolute reduction of blood glucose, lipid profile, and HMGR level when compared to diabetic control rats. The results have suggested that diosgenin prevents hypercholesterolemia and hepatosteatosis by modulation of enzymatic expression that is associated with cholesterol metabolism.

  20. Biotransformation of Dioscorea nipponica by Rat Intestinal Microflora and Cardioprotective Effects of Diosgenin

    Directory of Open Access Journals (Sweden)

    Jia-Fu Feng

    2017-01-01

    Full Text Available Studying the biotransformation of natural products by intestinal microflora is an important approach to understanding how and why some medicines—particularly natural medicines—work. In many cases, the active components are generated by metabolic activation. This is critical for drug research and development. As a means to explore the therapeutic mechanism of Dioscorea nipponica (DN, a medicinal plant used to treat myocardial ischemia (MI, metabolites generated by intestinal microflora from DN were identified, and the cardioprotective efficacy of these metabolites was evaluated. Our results demonstrate that diosgenin is the main metabolite produced by rat intestinal microflora from DN. Further, our results show that diosgenin protects the myocardium against ischemic insult through increasing enzymatic and nonenzymatic antioxidant levels in vivo and by decreasing oxidative stress damage. These mechanisms explain the clinical efficacy of DN as an anti-MI drug.

  1. Low pressure steam expansion pretreatment as a competitive approach to improve diosgenin yield and the production of fermentable sugar from Dioscorea zingiberensis C.H. Wright.

    Science.gov (United States)

    Wei, Mi; Tong, Yao; Wang, Hongbo; Wang, Lihua; Yu, Longjiang

    2016-04-01

    Development of efficient pretreatment methods which can disrupt the peripheral lignocellulose and even the parenchyma cells is of great importance for production of diosgenin from turmeric rhizomes. It was found that low pressure steam expansion pretreatment (LSEP) could improve the diosgenin yield by more than 40% compared with the case without pretreatment, while simultaneously increasing the production of fermentable sugar by 27.37%. Furthermore, little inhibitory compounds were produced in LSEP process which was extremely favorable for the subsequent biotransformation of fermentable sugar to other valuable products such as ethanol. Preliminary study showed that the ethanol yield when using the fermentable sugar as carbon source was comparable to that using glucose. The liquid residue of LSEP treated turmeric tuber after diosgenin production can be utilized as a quality fermentable carbon source. Therefore, LSEP has great potential in industrial application in diosgenin clean production and comprehensive utilization of turmeric tuber. Copyright © 2016 Elsevier Ltd. All rights reserved.

  2. Diosgenin reorganises hyperglycaemia and distorted tissue lipid profile in high-fat diet-streptozotocin-induced diabetic rats.

    Science.gov (United States)

    Naidu, Parim Brahma; Ponmurugan, Ponnusamy; Begum, Mustapha Sabana; Mohan, Karthick; Meriga, Balaji; RavindarNaik, Ramavat; Saravanan, Ganapathy

    2015-12-01

    Diabetes is often connected with significant morbidity, mortality and also has a pivotal role in the development of cardiovascular diseases. Diet intervention, particularly naturaceutical antioxidants have anti-diabetic potential and avert oxidative damage linked with diabetic pathogenesis. The present study investigated the effects of diosgenin, a saponin from fenugreek, on the changes in lipid profile in plasma, liver, heart and brain in high-fat diet-streptozotocin (HFD-STZ)-induced diabetic rats. Diosgenin was administered to HFD-STZ induced diabetic rats by orally at 60 mg kg(-1) body weight for 30 days to assess its effects on body weight gain, glucose, insulin, insulin resistance and cholesterol, triglycerides, free fatty acids and phospholipids in plasma, liver, heart and brain. The levels of body weight, glucose, insulin, insulin resistance, cholesterol, triglycerides, free fatty acids, phospholipids, VLDL-C and LDL-C were increased significantly (P rats. Administration of diosgenin to HFD-STZ diabetic rats caused a decrease in body weight gain, blood glucose, insulin, insulin resistance and also it modulated lipid profile in plasma and tissues. The traditional plant fenugreek and its constituents mediate its anti-diabetic potential through mitigating hyperglycaemic status, altering insulin resistance by alleviating metabolic dysregulation of lipid profile in both plasma and tissues. © 2014 Society of Chemical Industry.

  3. The role of diallyl thiosulfinate associated with nuciferine and diosgenin in the treatment of premature ejaculation: A pilot study

    Directory of Open Access Journals (Sweden)

    Tommaso Cai

    2018-03-01

    Full Text Available Objective: To assess the efficacy and safety of an association of diallyl thiosulfinate with nuciferine and diosgenin in the treatment of a group of patients suffering from premature ejaculation (PE, primary or secondary to erectile dysfunction (ED. Materials and methods: From July 2015 to October 2016, 143 patients (mean age 25.3; range 18-39 affected by PE completed the study and were finally analyzed in this phase I study. All patients, after clinical assessment and laboratory evaluation were asked to take an association of diallyl thiosulfinate with nuciferine and diosgenin as oral tablet, once a day, on alternate days, for three months. At the baseline and after three months of treatment, each patient was asked to complete the following questionnaires: International Index of Erectile Function (IIEF-5, Premature Ejaculation Diagnostic Tool (PEDT, Male Sexual Health Questionnaire (MSHQ. Results: A statistical significant improvement in terms of erectile function, comparing the IIEF-5 value at baseline and follow- up visit was found (respectively IIEF-5: 8.7 vs 14.01; p < 0.001. Moreover, at follow-up visit, 97/143 men (67.8% referred a subjective improvement of the erection quality and a better control of the ejaculation (PROs. The IELT improved too between the baseline evaluation and the follow-up visit (p < 0.001. Conclusion: In conclusion, our study, even if supported by preliminary results, showed how Diallyl Thiosulfinate, Nuciferine and Diosgenin is able to improve the control of ejaculation in patients suffering from PE, primary or secondary to ED without any significant adverse effects.

  4. Extração e isolamento de diosgenina de barbasco Extraction and isolation of diosgenin from yams

    Directory of Open Access Journals (Sweden)

    Marco Antonio Teixeira Zullo

    1987-01-01

    Full Text Available Dioscorea composita Hemsl. e D. floribunda Mart. & Gal., introduzidas no Brasil, mostraram teores de diosgenina de 3,15 ± 1,41% e 4,72 ± 0,24% na matéria seca dos tubérculos, com pureza mínima de 54,7 e 39,2% respectivamente. lamogenina também ocorre nos tubérculos de ambas as espécies. O teor de diosgenina em D. composita é crescente com a idade da planta, mostrando um máximo pronunciado em torno do terceiro ano de cultivo e estabilizando-se ao redor do sexto ano.Dioscorea composita Hemsl. and D. floribunda Mart. & Gal., introduced in Brazil, showed diosgenin contents of 3.15 ± 1.41% and 4.72 ± 0.24% on dried tubers, and minimum purities of 54.7% and 39.2%, respectively. Yamogenin co-occurs in the tubers of both species. The diosgenin content in D. composita increases according to the age of the plant, showing a pronounced maximum around the third year and stabilizing around the sixth year of cultivation. Methods for extraction, isolation and purification are also described.

  5. Production of diosgenin from Dioscorea zingiberensis with mixed culture in a new tray bioreactor

    Directory of Open Access Journals (Sweden)

    Yutong Cheng

    2016-01-01

    Full Text Available A new tray bioreactor was developed for the production of diosgenin from Dioscorea zingiberensis with Trichoderma reesei and Aspergillus fumigatus. The influence of initial moisture content, temperature, tray bed depth and mixing times was investigated. The best fermentation condition is initial moisture content of 75%, bioreactor temperature of 35°C, solid bed depth of 1.5 cm and three mixings carrying out on the first, third and fifth day. Under the optimized fermentation conditions, after 144 h incubation, maximum diogenin concentration of 68.2 μmol/g was detected.

  6. Effect of diosgenin on metabolic dysfunction: Role of ERβ in the regulation of PPARγ

    Energy Technology Data Exchange (ETDEWEB)

    Wang, Xin, E-mail: xinwang@fmmu.edu.cn [Department of Toxicology, Shaanxi Key Lab of Free Radical Biology and Medicine, the Ministry of Education Key Lab of Hazard Assessment and Control in Special Operational Environment, School of Public Health, Fourth Military Medical University, Xi' an 710032 (China); Liu, Jun [Department of Orthopedics, Lanzhou General Hospital of PLA, South Binhe Road, No. 333, Lanzhou 730050 (China); Long, Zi; Sun, Quangui [The First Student Brigade, Fourth Military Medical University, Xi' an, Shaanxi, 710032 (China); Liu, Ying; Wang, Lele; Zhang, Xiaodi [Department of Toxicology, Shaanxi Key Lab of Free Radical Biology and Medicine, the Ministry of Education Key Lab of Hazard Assessment and Control in Special Operational Environment, School of Public Health, Fourth Military Medical University, Xi' an 710032 (China); Hai, Chunxu, E-mail: cx-hai@fmmu.edu.cn [Department of Toxicology, Shaanxi Key Lab of Free Radical Biology and Medicine, the Ministry of Education Key Lab of Hazard Assessment and Control in Special Operational Environment, School of Public Health, Fourth Military Medical University, Xi' an 710032 (China)

    2015-12-01

    The present study was designed to investigate the effect of diosgenin (DSG) on metabolic dysfunction and to elucidate the possible molecular mechanisms. High fat (HF) diet-fed mice and 3T3-L1 preadipocytes was used to evaluate the effect of DSG. We showed that DSG attenuated metabolic dysfunction in HF diet-fed mice, as evidenced by reduction of blood glucose level and improvement of glucose and insulin intolerance. DSG ameliorated oxidative stress, reduced body weight, fat pads, and systematic lipid profiles and attenuated lipid accumulation. DSG inhibited 3T3-L1 adipocyte differentiation and reduced adipocyte size through regulating key factors. DSG inhibited PPARγ and its target gene expression both in differentiated 3T3-L1 adipocytes and fat tissues in HF diet-fed mice. Overexpression of PPARγ suppressed DSG-inhibited adipocyte differentiation. DSG significantly increased nuclear expression of ERβ. Inhibition of ERβ significantly suppressed DSG-exerted suppression of adipocyte differentiation and PPARγ expression. In response to DSG stimulation, ERβ bound with RXRα and dissociated RXRα from PPARγ, leading to the reduction of transcriptional activity of PPARγ. These data provide new insight into the mechanisms underlying the inhibitory effect of DSG on adipocyte differentiation and demonstrate that ERβ-exerted regulation of PPARγ expression and activity is critical for DSG-inhibited adipocyte differentiation. - Highlights: • Diosgenin (DSG) attenuated metabolic dysfunction in high fat (HF) diet-fed mice. • DSG reduced oxidative stress and lipid accumulation in HF diet-fed mice. • DSG inhibited 3T3-L1 adipocyte differentiation and reduced adipocyte size. • DSG induced the binding of ERβ with RXRα. • DSG-induced activation of ERβ dissociated RXRα from PPARγ and reduced PPARγ activity.

  7. Effect of diosgenin on metabolic dysfunction: Role of ERβ in the regulation of PPARγ

    International Nuclear Information System (INIS)

    Wang, Xin; Liu, Jun; Long, Zi; Sun, Quangui; Liu, Ying; Wang, Lele; Zhang, Xiaodi; Hai, Chunxu

    2015-01-01

    The present study was designed to investigate the effect of diosgenin (DSG) on metabolic dysfunction and to elucidate the possible molecular mechanisms. High fat (HF) diet-fed mice and 3T3-L1 preadipocytes was used to evaluate the effect of DSG. We showed that DSG attenuated metabolic dysfunction in HF diet-fed mice, as evidenced by reduction of blood glucose level and improvement of glucose and insulin intolerance. DSG ameliorated oxidative stress, reduced body weight, fat pads, and systematic lipid profiles and attenuated lipid accumulation. DSG inhibited 3T3-L1 adipocyte differentiation and reduced adipocyte size through regulating key factors. DSG inhibited PPARγ and its target gene expression both in differentiated 3T3-L1 adipocytes and fat tissues in HF diet-fed mice. Overexpression of PPARγ suppressed DSG-inhibited adipocyte differentiation. DSG significantly increased nuclear expression of ERβ. Inhibition of ERβ significantly suppressed DSG-exerted suppression of adipocyte differentiation and PPARγ expression. In response to DSG stimulation, ERβ bound with RXRα and dissociated RXRα from PPARγ, leading to the reduction of transcriptional activity of PPARγ. These data provide new insight into the mechanisms underlying the inhibitory effect of DSG on adipocyte differentiation and demonstrate that ERβ-exerted regulation of PPARγ expression and activity is critical for DSG-inhibited adipocyte differentiation. - Highlights: • Diosgenin (DSG) attenuated metabolic dysfunction in high fat (HF) diet-fed mice. • DSG reduced oxidative stress and lipid accumulation in HF diet-fed mice. • DSG inhibited 3T3-L1 adipocyte differentiation and reduced adipocyte size. • DSG induced the binding of ERβ with RXRα. • DSG-induced activation of ERβ dissociated RXRα from PPARγ and reduced PPARγ activity.

  8. Self-assembled hyaluronic acid nanoparticles for controlled release of agrochemicals and diosgenin.

    Science.gov (United States)

    Quiñones, Javier Pérez; Brüggemann, Oliver; Covas, Carlos Peniche; Ossipov, Dmitri A

    2017-10-01

    Commercial sodium hyaluronate (HA) and synthetic hydrazide-modified HA were functionalized with diosgenin and two agrochemicals (brassinosteroids DI31 and S7) with degree of substitution ranging from 5.6 to 13.1%. The HA-steroid conjugates were studied with FTIR, 1 H NMR and differential scanning calorimetry. Dynamic light scattering revealed self-assembly of the HA-steroid conjugates into stable negatively charged nanoparticles of around 159nm-441nm in water, which after drying appeared as 140nm-370nm spherically shaped nanoparticles according to transmission electron microscopy. These nanoparticles exhibited almost constant release rates of steroids for the first 8h, demonstrating sustained steroids delivery for 72h in acidic medium. The nanoparticles formed from HA-steroid conjugates were not cytotoxic to human microvascular endothelial cells (HMVEC), while the HA- brassinosteroid nanoparticles showed in vitro agrochemical activity that was superior to the activity observed for the parent brassinosteroids DI31 and S7 at 10 -5 to 10 -7 mgmL -1 . Copyright © 2017 Elsevier Ltd. All rights reserved.

  9. Bivalent ligands incorporating curcumin and diosgenin as multifunctional compounds against Alzheimer's disease.

    Science.gov (United States)

    Chojnacki, Jeremy E; Liu, Kai; Saathoff, John M; Zhang, Shijun

    2015-11-15

    In an effort to combat the multifaceted nature of Alzheimer's disease (AD) progression, a series of multifunctional, bivalent compounds containing curcumin and diosgenin were designed, synthesized, and biologically characterized. Screening results in MC65 neuroblastoma cells established that compound 38 with a spacer length of 17 atoms exhibited the highest protective potency with an EC50 of 111.7 ± 9.0 nM. A reduction in protective activity was observed as spacer length was increased up to 28 atoms and there is a clear structural preference for attachment to the methylene carbon between the two carbonyl moieties of curcumin. Further study suggested that antioxidative ability and inhibitory effects on amyloid-β oligomer (AβO) formation may contribute to the neuroprotective outcomes. Additionally, compound 38 was found to bind directly to Aβ, similar to curcumin, but did not form complexes with the common biometals Cu, Fe, and Zn. Altogether, these results give strong evidence to support the bivalent design strategy in developing novel compounds with multifunctional ability for the treatment of AD. Copyright © 2015 Elsevier Ltd. All rights reserved.

  10. Diosgenin, 4-hydroxyisoleucine, and fiber from fenugreek: mechanisms of actions and potential effects on metabolic syndrome.

    Science.gov (United States)

    Fuller, Scott; Stephens, Jacqueline M

    2015-03-01

    Metabolic syndrome and its complications continue to rise in prevalence and show no signs of abating in the immediate future. Therefore, the search for effective treatments is a high priority in biomedical research. Products derived from botanicals have a time-honored history of use in the treatment of metabolic diseases including type 2 diabetes. Trigonella foenum-graecum, commonly known as fenugreek, is an annual herbaceous plant that has been a staple of traditional herbal medicine in many cultures. Although fenugreek has been studied in both clinical and basic research settings, questions remain about its efficacy and biologic mechanisms of action. Diosgenin, 4-hydroxyisoleucine, and the fiber component of the plant are the most intensively studied bioactive constituents present in fenugreek. These compounds have been demonstrated to exert beneficial effects on several physiologic markers including glucose tolerance, inflammation, insulin action, liver function, blood lipids, and cardiovascular health. Although insights into the molecular mechanisms underlying the favorable effects of fenugreek have been gained, we still do not have definitive evidence establishing its role as a therapeutic agent in metabolic disease. This review aims to summarize the currently available evidence on the physiologic effects of the 3 best-characterized bioactive compounds of fenugreek, with particular emphasis on biologic mechanisms of action relevant in the context of metabolic syndrome. © 2015 American Society for Nutrition.

  11. Removal of High -Concentration and Refractory Organic Matter from Diosgenin Manufacture Wastewater : a case study of a demonstration project in Hubei Province, P R China

    Science.gov (United States)

    Bao, J.; Wang, L.

    2009-12-01

    Wastewater from diosgenin manufacture is dark brown (3,500 ~4,000 times of the chroma) and acidic(pH=0.8~1.5)with high concentration of organic matter(COD=25,000~38,000 mg/L)and poor biodegradability(BOD5/COD= 0.25~0.30). It is highly toxic to biota due to the water-soluble saponin, tannins and pectin. Therefore removal of the organic matter is of great importance before the discharge of the wastewater into the environment. Here we presented a set of data from a demonstration project in Hubei province, P R China with an improved technics. This technics, focusing on the treatment of diosgenin wastewater, included hydrolytic acidification, internal electrolysis, neutralization, aerating-improved Up-flow Anaerobic Sludge Bed (UASB) and bio-contact oxidation treatment in sequence to remove the organic matter. After 60 days of starting-up, the water quality from hydrolytic acidification reactor was greatly improved. The effluent became clear, indicating the obvious removal of suspended solids in the water; the ratio of BOD/COD increased to 0.44, suggesting an significant increase of biodegradability; the content of volatile fatty acid (VFA) increased from 22.6 mmol/L to 86.8 mmol/L and the volume loading of COD reached 9.48 kg COD/(m3d). Basically at this stage the removal efficiency of COD was stabilized at 25%. Further treatment was conducted on the effluent from hydrolytic acidification reactor through the Improved UASB Reactor after the internal electrolysis and neutralization. The Improved UASB Reactor can start up at room temperature with an influent of 1,500 mg/L COD and inflow rate of 50(m3/d). Then, temperature was increased gradually to 38 oC (± 2 oC) to optimize the growth of the mesophilic anaerobes in the reactor. The content of VFA of the effluent was controlled below 8 mmol/L to guarantee the pH in the range of 6.8~7.2. After 150 days of debugging, the COD of the influent to UASB increased to 9,600 mg/L, hydraulic retaining time (HRT) was around 70 hrs

  12. Diosgenin a phytosterol substitute for cholesterol, prolongs the lifespan and mitigates glucose toxicity via DAF-16/FOXO and GST-4 in Caenorhabditis elegans.

    Science.gov (United States)

    Shanmugam, Govindan; Mohankumar, Amirthalingam; Kalaiselvi, Duraisamy; Nivitha, Sundararaj; Murugesh, Easwaran; Shanmughavel, Piramanayagam; Sundararaj, Palanisamy

    2017-11-01

    Caenorhabditis elegans is a sterol auxotroph requires minute amount of exogenous sterol for their growth and development. To culture the C. elegans, cholesterol was given as sterol molecule to maintain the optimum survival of worms. Diosgenin (DG), a plant derived steroidal saponin, structurally similar to cholesterol has been used as a precursor for the synthesis of steroidal hormones. In this study, worms were cultured with cholesterol (Cho + ) and cholesterol-free (Cho - ) medium with DG (5, 10 and 50μg/mL) at 20°C. It was observed that worms cultured in (Cho - ) exhibits late egg production, reduced lipid level and short lifespan, while addition of DG overcomes all defective facts. Combinations of both cholesterol and DG further extend the lifespan (20.8%), hinder lipid level and resistance to oxidative, thermal and high glucose stress. The intracellular ROS quantification was done by flouroscenic probe H2DCF-DA and confirmed that DG had significantly reduced ROS level (35.85%). Increased lifespan of worms were observed in the medium treated with DG which activates the nuclear translocation of DAF-16/FOXO transcription factor, followed by downstream antioxidant gene sod-3 as evidenced by GFP tagged strain. The expression of Phase II detoxification enzyme GST-4 significantly (pdaf-16, skn-1, and eat-2. These studies have proved that DG is a sterol source to worms and modulate the DAF-16, SOD-3 and GST-4 expression levels to extend the lifespan of worms. The present study has also highlighted the use of phytosterols as an alternative to cholesterol. Copyright © 2017 Elsevier Masson SAS. All rights reserved.

  13. N,O6-partially acetylated chitosan nanoparticles hydrophobically-modified for controlled release of steroids and vitamin E

    DEFF Research Database (Denmark)

    Quinones, Javier Perez; Gothelf, Kurt Vesterager; Kjems, Jørgen

    2013-01-01

    Diosgenin, two synthetic analogs of brassinosteroids, testosterone and dl-α-tocopherol were covalently linked to synthetic water-soluble N,O6-partially acetylated chitosan, for their controlled release. Drug linking was confirmed by FTIR spectroscopy and proton NMR. Conjugates were also character......Diosgenin, two synthetic analogs of brassinosteroids, testosterone and dl-α-tocopherol were covalently linked to synthetic water-soluble N,O6-partially acetylated chitosan, for their controlled release. Drug linking was confirmed by FTIR spectroscopy and proton NMR. Conjugates were also...

  14. In Silico and In Vitro Study of the Bromelain-Phytochemical Complex Inhibition of Phospholipase A2 (Pla2

    Directory of Open Access Journals (Sweden)

    Fatahiya Mohamed Tap

    2018-01-01

    Full Text Available Phospholipase A2 (Pla2 is an enzyme that induces inflammation, making Pla2 activity an effective approach to reduce inflammation. Therefore, investigating natural compounds for this Pla2 inhibitory activity has important therapeutic potential. The objective of this study was to investigate the potential in bromelain-phytochemical complex inhibitors via a combination of in silico and in vitro methods. Bromelain-amenthoflavone displays antagonistic effects on Pla2. Bromelian-asiaticoside and bromelain-diosgenin displayed synergistic effects at high concentrations of the combined compounds, with inhibition percentages of more than 70% and 90%, respectively, and antagonistic effects at low concentrations. The synergistic effect of the bromelain-asiaticoside and bromelain-diosgenin combinations represents a new application in treating inflammation. These findings not only provide significant quantitative data, but also provide an insight on valuable implications for the combined use of bromelain with asiaticoside and diosgenin in treating inflammation, and may help researchers develop more natural bioactive compounds in daily foods as anti-inflammatory agent.

  15. African Journal of Biotechnology - Vol 4, No 11 (2005)

    African Journals Online (AJOL)

    Variation in diosgenin level in seed kernels among different provenances of Balanites aegyptiaca Del (Zygophyllaceae) and its correlation with oil content ... Genetic relationships among Ethiopian mustard genotypes based on oil content and fatty acid composition · EMAIL FREE FULL TEXT EMAIL FREE FULL TEXT

  16. Microwave-assisted extraction and a new determination method for total steroid saponins from Dioscorea zingiberensis C.H. Wright.

    Science.gov (United States)

    Ren, Yao; Chen, Yu; Hu, Bohan; Wu, Hui; Lai, Furao; Li, Xiaofeng

    2015-12-01

    An efficient microwave-assisted extraction (MAE) technique was applied to isolate total steroid saponins from Dioscorea zingiberensis C.H. Wright (DZW). The optimal extracting conditions were established as 75% ethanol as solvent, ratio of solid/liquid 1:20 (g/ml), temperature 75 °C, irradiation power 600 W and three extraction cycles of 6 min each. Scanning electron microscopy (SEM) images of DZW processed by four different extractions provided visual evidence of the disruption effect on DZW. Diosgenin was quantified by HPLC and examined further by LC-ESI/MS after acid hydrolysis. Total steroid saponins were calculated using diosgenin from total steroid saponins. The MAE procedure was optimized, validated and compared with other conventional extraction processes. This report provides a convenient technology for the extraction and quantification of total saponins of DZW combining MAE with HPLC and LC-ESI/MS for the first time. Copyright © 2015 Elsevier Inc. All rights reserved.

  17. The day of the yam.

    Science.gov (United States)

    Rosser, A

    Yam, the staple food in several tropical countries, is a good source of the steroid used in the manufacture of the pill and other sex hormone preparations -- saponin diosgenin. In the early days of production of oral contraceptives (OCs), most yams were gathered from the wild in Mexico. The type richest in steroids takes 3 years to mature and its cultivation has become something of an art. Yams grow best in light, well-drained soil, and for this reason are grown in mounds which have been heavily manured. Propagation is by planting the tops or heads or by small portions of the tuber which is a swollen shoot. Other varieties are planted before the onset of the rains and the crop harvested about 8 months later. In 1970 the Mexican government nationalized the yam industry as a safeguard. This pushed up prices and the drug companies looked elsewhere for a cheap source. Although Mexico still remains the principal grower, India, South Africa, and the Far East supply the industry with plant origin steroids. As more than 90% of the hefty yam tubers consist of water, well over 100,000 tons have to be harvested every year to provide the 600-700 tons of the saponin diosgenin used by the drug companies. In China, where Western corticosteroids are regarded as too expensive for the barefoot doctors, several species of yam are used. Research has been going on to find another source of diosgenin and the most promising seems to be fenugreek, Trigonella foenumgraecum. "Foenum graecum" is Latin for Greek hay and was used by the early Greeks as a culinary and medicinal herb throughout the Mediterranean area. The richness of fenugreek was used to improve the roundness of women's breasts and to stimulate the flow of milk. Bath University has spent 10 years researching the development of a species of fenugreek which will yield large amounts of diosgenin. A certain amount of steroids come from animal sources. Such steroids are given when there is an adverse reaction from the

  18. Effects of Pseudomonas putida and Glomusintraradices Inoculations on Morphological and Biochemical Traitsin Trigonellafoenum-graecum L.

    Directory of Open Access Journals (Sweden)

    simin irankhah

    2017-02-01

    the best time and at a dilution of 0.5 McFarland was added to the seed.Pots were placed in a growth chamber (with a temperature of 25 ° C and 16 hours of light and 8 hours of darkness photoperiod.After ten days of planting, the water treatment was applied and continued until the end of the experiment. Results and Discussion:The results showed that the use of co -inoculation treatment ofP.putidaandG.intraradicesand application of G.intraradices aloneat non-stress conditions did not make a significant difference on the amount of plant biomass. In drought conditions, application of G.intraradice alone had significant difference (P≤0.05 compare with control (no inoculation microorganisms for biomass.In stress conditions, P.putida inoculation and also in combination with G.intraradicesincreased biomass in compare with control (no inoculation of micro-organisms, but this increasing was not statistically significant.VAMare important ecological symbiotic with roots are important component of the ecosystem and affect the absorption of minerals through the roots. The results of the present study showed that the amount of phosphorus in all of treatments was increased and the greatest increase was related to G.intraradicetreatment.The results also showed that drought stress increased the leaf soluble proteins in compared with non-stress condition. Increasing the concentration of soluble proteins under drought stress can be related to increased protein synthesis that maybe related to adaptation and reprogramming under new situation and itprotect the cells against stress. The results showed that the use of co -inoculation treatment ofP.putidaand G.intraradices, as well as each individual treatment, increased the amount of soluble proteins in leaves.In the case of the Diosgenin percentage, drought stress reduced the amount of Diosgenin percentage. Underdrought stress conditions, use of co -inoculation treatment ofP.putidaand G.intraradicesand application of G

  19. In-Silico Testing Of Nutraceutical Against The Murd Enzymes From Mycobacterium Tuberculosis

    Directory of Open Access Journals (Sweden)

    Mohammad Teimouri

    2015-08-01

    Full Text Available In spite of availability of moderately protective vaccine and antibiotics new antibacterial agents are urgently needed to decrease the global incidence of Mycobacterium tuberculosis infections. Mur family is an important target for the development of new drugs as they are involved in the biosynthesis of bacterial cell wall. MurC-MurF ligases catalyze a series of irreversible steps in the biosynthesis of peptidoglycan precursor i.e. MurD catalyzes the ligation of D-glutamate to the nucleotide precursor UMA. Here we developed a homology model of MurD from M. Tuberculosis and was validated by using rampage Errat and ProSA online servers. Different nutraceuticals were tested and reported for their activity. Among the 14 nutraceuticals Diosgenin Xanthohumol Capsaicin 1-acetoxychavicol acetate and 6-Gingerol have best docking score. The best of all was Diosgenin with the docking score -14.22988 Xanthohumol with -13.923555 Capsaicin with -12.880404 1-acetoxychavicol acetate with -12.573502 and 6-Gingerol -12.349156 which will play a guiding role in the experimental design and development of mycobacterium tuberculosis MurD

  20. Effects of synthetic glycosides on steroid balance in Macaca fascicularis

    International Nuclear Information System (INIS)

    Malinow, M.R.; Elliott, W.H.; McLaughlin, P.; Upson, B.

    1987-01-01

    The predominantly beta-anomer of diosgenin glucoside (DG) was synthesized and its effects on cholesterol homeostasis were tested in monkeys. Cynomolgus macaques (Macaca fascicularis) were fed, during two 3-week periods, a semipurified diet with 0.1% cholesterol and a similar ration containing 1% DG, respectively. A Chow diet was given for 5 weeks between the experimental periods. Cholesterol and bile acid balance were analyzed during the last week of each semipurified diet. Diosgenin glucoside reduced cholesterolemia from 292 mg/dl to 172 mg/dl, decreased intestinal absorption of exogenous cholesterol from 62.4% to 26.0%, and increased secretion of endogenous cholesterol from -0.8 to 93.5 mg/day. The fecal excretion of neutral steroids rose from 40.7 to 157.3 mg/day; that of bile acids changed, nonsignificantly, from 23.1 to 16.0 mg/day. The cholesterol balance was -44 mg/day in the control period, and 88 mg/day in the DG-fed animals. No toxic signs were observed. Thus, when long-term studies demonstrate that the glucoside is well tolerated, DG and other synthetic glycosides with similar activities may be of use in the management of hypercholesterolemia and atherosclerosis

  1. Valuable fenugreek (Trigonella foenum-graecum L.) mutants induced by gamma rays and alkylating agents

    Energy Technology Data Exchange (ETDEWEB)

    Floria, F [Biotechnology and Molecular Genetics Group, ' Stejarul' Research Centre for Biological Sciences, Piatra Neamt (Romania); Ichim, M C [Biotechnology and Molecular Genetics Group, ' Stejarul' Research Centre for Biological Sciences, Piatra Neamt (Romania)

    2006-12-15

    Seeds of fenugreek (Trigonella foenum-graecum L.) were treated with either gamma rays (25-15 kR) or ethyl methanesulphonate (EMS 0.1-0.5%, 2h) or ethylene imine (EI, 0.01- 0.1%, 2h). After repeated selection for better morphological performance from M{sub 2} to M{sub 4} generation, 11 mutant lines were identified with better yield potential and higher diosgenin content than their parent. (author)

  2. A New Class of Amphiphiles Bearing Rigid Hydrophobic Groups for Solubilization and Stabilization of Membrane Proteins

    DEFF Research Database (Denmark)

    Chae, Pil Seok; Rasmussen, Søren G F; Rana, Rohini R

    2012-01-01

    Non-traditional amphiphiles: Conferring aqueous solubility on membrane proteins generally requires the use of a detergent or other amphiphilic agent. A new class of amphiphiles was synthesized, based on steroidal lipophilic groups, and evaluated with several membrane proteins. The results show th...... that the new amphiphile, "glyco-diosgenin" (GDN; see figure), confers enhanced stability to a variety of membrane proteins in solution relative to popular conventional detergents, such as dodecylmaltoside (DDM)....

  3. A new source of elemol rich essential oil and existence of multicellular oil glands in leaves of the Dioscorea species.

    Science.gov (United States)

    Odimegwu, Joy I; Odukoya, Olukemi; Yadav, Ritesh K; Chanotiya, C S; Ogbonnia, Steve; Sangwan, Neelam S

    2013-01-01

    Dioscorea species is a very important food and drug plant. The tubers of the plant are extensively used in food and drug purposes owing to the presence of steroidal constituent's diosgenin in the tubers. In the present study, we report for the first time that the leaves of Dioscorea composita and Dioscorea floribunda grown under the field conditions exhibited the presence of multicellular oil glands on the epidermal layers of the plants using stereomicroscopy (SM) and scanning electron microscopy (SEM). Essential oil was also isolated from the otherwise not useful herbage of the plant, and gas chromatographic-mass spectroscopy analysis revealed confirmation of the essential oil constituents. Out of the 76 compounds detected in D. floribunda and 37 from D. composita essential oil, major terpenoids which are detected and reported for Dioscorea leaf essential oil are α -terpinene, nerolidol, citronellyl acetate, farnesol, elemol, α -farnesene, valerenyl acetate, and so forth. Elemol was detected as the major constituent of both the Dioscorea species occupying 41% and 22% of D. Floribunda and D. composita essential oils, respectively. In this paper, we report for the first time Dioscorea as a possible novel bioresource for the essential oil besides its well-known importance for yielding diosgenin.

  4. A New Source of Elemol Rich Essential Oil and Existence of Multicellular Oil Glands in Leaves of the Dioscorea Species

    Directory of Open Access Journals (Sweden)

    Joy I. Odimegwu

    2013-01-01

    Full Text Available Dioscorea species is a very important food and drug plant. The tubers of the plant are extensively used in food and drug purposes owing to the presence of steroidal constituent’s diosgenin in the tubers. In the present study, we report for the first time that the leaves of Dioscorea composita and Dioscorea floribunda grown under the field conditions exhibited the presence of multicellular oil glands on the epidermal layers of the plants using stereomicroscopy (SM and scanning electron microscopy (SEM. Essential oil was also isolated from the otherwise not useful herbage of the plant, and gas chromatographic-mass spectroscopy analysis revealed confirmation of the essential oil constituents. Out of the 76 compounds detected in D. floribunda and 37 from D. composita essential oil, major terpenoids which are detected and reported for Dioscorea leaf essential oil are α-terpinene, nerolidol, citronellyl acetate, farnesol, elemol, α-farnesene, valerenyl acetate, and so forth. Elemol was detected as the major constituent of both the Dioscorea species occupying 41% and 22% of D. Floribunda and D. composita essential oils, respectively. In this paper, we report for the first time Dioscorea as a possible novel bioresource for the essential oil besides its well-known importance for yielding diosgenin.

  5. Do diosgenin ameliorate urinary bladder toxic effect of ...

    African Journals Online (AJOL)

    SWEET

    2012-01-26

    Jan 26, 2012 ... experimental animal models? ... BSO doses using a Swiss albino mouse model. Toxicity modulation ... bladder inflammation induced by CP in rats and mice .... 0.1 ml NADPH (nicotinamide adenine dinucleotide phosphate.

  6. Enhancement of Diosgenin Production in Plantlet and Cell Cultures ...

    African Journals Online (AJOL)

    HSCCC),. Sephadex LH-20 chromatography and preparative .... phase of acetonitrile-water (90:10, v/v) at a flow rate of 1 mL/min at 30 ºC, and an LC ..... Spirobisnaphthalenes from fungi and their biological activities. Mini-Rev Med Chem 2010; 10: ...

  7. Comparative Physicochemical Evaluation of Kharekhasak (Tribulus terrestris Linn.) Before and After Mudabbar Process

    Science.gov (United States)

    Tauheed, Abdullah; Hamiduddin; Khanam, Salma; Ali, Mohd Akhtar; Zaigham, Mohammad

    2017-01-01

    Background and Objectives: Mudabbar/Tadbeere advia is referred to the processes performed on the drugs to detoxify, purify, and enhance therapeutic action and to reduce its doses before making the formulations in Unani medicine. It improves quality of drugs either by optimizing its desirable characteristics or minimizing the undesirable ones; it makes drug effective, safe, and specific. There is a need of comparative evaluation to understand its significance. Tadbeer of Kharekhasak (KK) khurd (Tribulus terrestris Linn. fruit) is described by Rabban Al-Tabari in Firdausul Hikmat, Akbar Arzani in Qarabadeene Qadri, etc., during the compounding of aphrodisiac formulations. Mudabbar Kharekhasak (MKK) used in Safoofe Kharekhasak mentioned in Al-Qarabadeene was evaluated in this work. Methods: Mudabbar/Tadbeer process was carried out by blending fresh KK. Juice with powdered dry KK and drying it under the sun. Juice used for process is thrice the weight of dry KK powder. The KK before and after the process was evaluated using physicochemical tests: powder characterization, extractive value, alcohol and water soluble matter, ash value, loss on drying (LOD) at 105°C, pH, high-performance thin layer chromatography (HPTLC) fingerprinting, and diosgenin content. Results: Powder characterizations were set in. Increase in successive and nonsuccessive extractive values in various solvents, water/alcohol-soluble content, total ash, acid-insoluble ash, water-soluble ash, and sulfated ash of MKK was noted in comparison with KK. Decrease in LOD at 105°C and pH of MKK powder was observed. HPTLC fingerprinting data were developed for the identification and evaluation. Quantification of diosgenin content increased to 432.1 g/g in MKK as compared to 144.5 g/g in KK, suggesting significant increase in saponin content. Conclusion: Data obtained clearly indicated changes in MKK validating the classical Mudabbar process, probably to enhance/modify the action of drug. Standards for crude

  8. Comparative Physicochemical Evaluation of Kharekhasak (Tribulus terrestris Linn.) Before and After Mudabbar Process.

    Science.gov (United States)

    Tauheed, Abdullah; Hamiduddin; Khanam, Salma; Ali, Mohd Akhtar; Zaigham, Mohammad

    2017-01-01

    Mudabbar/ Tadbeere advia is referred to the processes performed on the drugs to detoxify, purify, and enhance therapeutic action and to reduce its doses before making the formulations in Unani medicine. It improves quality of drugs either by optimizing its desirable characteristics or minimizing the undesirable ones; it makes drug effective, safe, and specific. There is a need of comparative evaluation to understand its significance. Tadbeer of Kharekhasak (KK) khurd ( Tribulus terrestris Linn. fruit) is described by Rabban Al-Tabari in Firdausul Hikmat, Akbar Arzani in Qarabadeene Qadri, etc., during the compounding of aphrodisiac formulations. Mudabbar Kharekhasak (MKK) used in Safoofe Kharekhasak mentioned in Al-Qarabadeene was evaluated in this work. Mudabbar/Tadbeer process was carried out by blending fresh KK. Juice with powdered dry KK and drying it under the sun. Juice used for process is thrice the weight of dry KK powder. The KK before and after the process was evaluated using physicochemical tests: powder characterization, extractive value, alcohol and water soluble matter, ash value, loss on drying (LOD) at 105°C, pH, high-performance thin layer chromatography (HPTLC) fingerprinting, and diosgenin content. Powder characterizations were set in. Increase in successive and nonsuccessive extractive values in various solvents, water/alcohol-soluble content, total ash, acid-insoluble ash, water-soluble ash, and sulfated ash of MKK was noted in comparison with KK. Decrease in LOD at 105°C and pH of MKK powder was observed. HPTLC fingerprinting data were developed for the identification and evaluation. Quantification of diosgenin content increased to 432.1 g/g in MKK as compared to 144.5 g/g in KK, suggesting significant increase in saponin content. Data obtained clearly indicated changes in MKK validating the classical Mudabbar process, probably to enhance/modify the action of drug. Standards for crude and MKK were established for future reference. Mudabbar

  9. Isolation and characterization of a furfural-degrading bacterium Bacillus cereus sp. strain DS1.

    Science.gov (United States)

    Zheng, Dan; Bao, Jianguo; Lu, Jueming; Gao, Chunlei

    2015-02-01

    Furfural was found to be the main organic pollutant in the wastewater coming from the Diosgenin factory. This substance is derived from acidic pentosan in Dioscorea zingiberensis and is also found in a variety of agricultural byproducts, including corncobs, oat, wheat bran, and sawdust. It is regarded as a toxicant and an inhibitor to the growth of microorganism in both sewage disposal and biological fermentation. A furfural-degrading strain (DS1) was isolated from activated sludge of wastewater treatment plant in a diosgenin factory by continuous enrichment culture. The strain was identified as Bacillus cereus based on morphological, physiological tests, as well as on 16S rDNA sequence and Biolog analyses. The capacity of this strain to grow on a mineral salt medium, utilizing furfural as the sole carbon and energy source to degrade furfural, was investigated in this study. Under the condition of pH 9.0, temperature 35 °C, with rotating speed of 150 rpm, and an inoculum of 6 %, the strain showed that the furfural degradation capacity reaches 35 % in 7 days, as measured by high-performance liquid chromatography. The addition of inorganic carbon sources could bring down the biodegradation efficiency of the furfural. The strain DS1 showed better furfural removal capacity, as compared to other inorganic carbon sources in the media. Furthermore, a furfural concentration of as high as 4,000 mg L(-1) was tolerated by the culture. The capacity to degrade furfural was demonstrated for the first time by using the genus B. cereus. This study suggests the possible application in biodegradation strategies.

  10. Weighted Gene Co-expression Network Analysis of the Dioscin Rich Medicinal Plant Dioscorea nipponica

    Directory of Open Access Journals (Sweden)

    Wei Sun

    2017-06-01

    Full Text Available Dioscorea contains critically important species which can be used as staple foods or sources of bioactive substances, including Dioscorea nipponica, which has been used to develop highly successful drugs to treat cardiovascular disease. Its major active ingredients are thought to be sterol compounds such as diosgenin, which has been called “medicinal gold” because of its valuable properties. However, reliance on naturally growing plants as a production system limits the potential use of D. nipponica, raising interest in engineering metabolic pathways to enhance the production of secondary metabolites. However, the biosynthetic pathway of diosgenin is still poorly understood, and D. nipponica is poorly characterized at a molecular level, hindering in-depth investigation. In the present work, the RNAs from five organs and seven methyl jasmonate treated D. nipponica rhizomes were sequenced using the Illumina high-throughput sequencing platform, yielding 52 gigabases of data, which were pooled and assembled into a reference transcriptome. Four hundred and eighty two genes were found to be highly expressed in the rhizomes, and these genes are mainly involved in stress response and transcriptional regulation. Based on their expression patterns, 36 genes were selected for further investigation as candidate genes involved in dioscin biosynthesis. Constructing co-expression networks based on significant changes in gene expression revealed 15 gene modules. Of these, four modules with properties correlating to dioscin regulation and biosynthesis, consisting of 4,665 genes in total, were selected for further functional investigation. These results improve our understanding of dioscin biosynthesis in this important medicinal plant and will help guide more intensive investigations.

  11. Effect of Dioscorea opposita Thunb. (yam) supplementation on physicochemical and sensory characteristics of yogurt.

    Science.gov (United States)

    Kim, S H; Lee, S Y; Palanivel, G; Kwak, H S

    2011-04-01

    A study was conducted to examine the physicochemical, microbial, and sensory properties of yogurt made by supplementing powdered yam Dioscorea opposita Thunb. (YPT) at different concentrations (0.2, 0.4, 0.6, and 0.8%, wt/vol) into milk, which was pasteurized and then fermented at 43°C for 6 h and stored for 16 d. The pH values of all samples decreased, whereas viscosity values and mean microbial counts increased during storage. The L* and a* color values (indicators of lightness and redness, respectively) of yogurt samples were not remarkably influenced by adding YPT, whereas the b* values (indicating yellowness) significantly increased with the addition of YPT at all concentrations at 0 d of storage, probably due to the original yellow color of yam powder. In functional component analyses, when the concentration of YPT increased, the amount of allantoin and diosgenin proportionally increased. The content of allantoin was 3.22 and diosgenin 4.69 μg/mL when 0.2% (wt/vol) YPT was supplemented and did not change quantitatively during the storage period (16 d). The sensory test revealed that the overall acceptability scores of YPT-supplemented yogurt samples (0.2 to 0.6%, wt/vol) were quite similar to those of the control throughout the storage period of 16 d. Based on the data obtained from the present study, it was concluded that the concentrations (0.2 to 0.6%, wt/vol) of YPT could be used to produce YPT-supplemented yogurt without significant adverse effects on physicochemical, microbial, and sensory properties, and enhance functional components from the supplementation. Copyright © 2011 American Dairy Science Association. Published by Elsevier Inc. All rights reserved.

  12. Dietary nutraceuticals as backbone for bone health.

    Science.gov (United States)

    Pandey, Manoj K; Gupta, Subash C; Karelia, Deepkamal; Gilhooley, Patrick J; Shakibaei, Mehdi; Aggarwal, Bharat B

    2018-03-27

    Bone loss or osteoporosis, is a slow-progressing disease that results from dysregulation of pro-inflammatory cytokines. The FDA has approved number of drugs for bone loss prevention, nonetheless all are expensive and have multiple side effects. The nutraceuticals identified from dietary agents such as butein, cardamonin, coronarin D curcumin, diosgenin, embelin, gambogic acid, genistein, plumbagin, quercetin, reseveratrol, zerumbone and more, can modulate cell signaling pathways and reverse/slow down osteoporosis. Most of these nutraceuticals are inexpensive; show no side effect while still possessing anti-inflammatory properties. This review provides various mechanisms of osteoporosis and how nutraceuticals can potentially prevent the bone loss. Published by Elsevier Inc.

  13. Final report of the amended safety assessment of Dioscorea Villosa (Wild Yam) root extract.

    Science.gov (United States)

    2004-01-01

    Dioscorea Villosa (Wild Yam) Root Extract is an extract of the rhizomes of the wild yam, D. villosa. A manufacturing process was described in which cut up and ground rhizomes are combined with an eluant (e.g., oleyl alcohol), the plant material precipitated with addition of a miscible solvent, washed, and redissolved in the original eluant. The extract contains glycoside and steroidal saponins (Food and Drug Administration (in a body and hand preparation), industry reported uses in body and hand creams, lotions, powders, and sprays at a concentration of 0.00001% (equivalent to 0.000002% plant solids), and in moisturizing creams, lotions, powders, and sprays at concentrations up to 15% (equivalent to 0.5% plant solids). Preparations fromD. villosaare used in herbal medicine for treatment of a variety of ailments and by the pharmaceutical industry in the preparation of steroids. Using Dioscorea Villosa (Wild Yam) Root Extract prepared via a specified process, it is possible to produce a stable extract with a narrow range of diosgenin content. The extract produced using this methodology was tested in acute and short-term toxicity tests, dermal irritation tests, a sensitization test, an ocular irritation test, a rat uterotropic assay, and genotoxicity tests. An acute oral toxicity test produced hypoactivity, piloerection, and dyspnea and a death in 1 of 10 rats at 2 g/kg using the specified extract, but no toxicity in rats given 0.5 g/kg. A dermal toxicity test using the specified extract demonstrated no acute toxicity in rats. Both a 7-day local tolerance test and a 28-day dermal toxicity test in rats produced no significant adverse effects at the maximum tested concentration of 10%. A single application of undiluted extract to the intact and abraded skin of rabbits produced sufficient irritation for the test material to be rated"irritant,"but a 10% dilution was not irritating. Undiluted extract was only mildly irritating to the conjuctiva of the rabbit eye

  14. Phytochemical Analysis and Free Radical Scavenging Activity of Medicinal Plants Gnidia glauca and Dioscorea bulbifera

    Science.gov (United States)

    Ghosh, Sougata; Derle, Abhishek; Ahire, Mehul; More, Piyush; Jagtap, Soham; Phadatare, Suvarna D.; Patil, Ajay B.; Jabgunde, Amit M.; Sharma, Geeta K.; Shinde, Vaishali S.; Pardesi, Karishma; Dhavale, Dilip D.; Chopade, Balu A.

    2013-01-01

    Gnidia glauca and Dioscorea bulbifera are traditional medicinal plants that can be considered as sources of natural antioxidants. Herein we report the phytochemical analysis and free radical scavenging activity of their sequential extracts. Phenolic and flavonoid content were determined. Scavenging activity was checked against pulse radiolysis generated ABTS•+ and OH radical, in addition to DPPH, superoxide and hydroxyl radicals by biochemical methods followed by principal component analysis. G. glauca leaf extracts were rich in phenolic and flavonoid content. Ethyl acetate extract of D. bulbifera bulbs and methanol extract of G. glauca stem exhibited excellent scavenging of pulse radiolysis generated ABTS•+ radical with a second order rate constant of 2.33×106 and 1.72×106, respectively. Similarly, methanol extract of G. glauca flower and ethyl acetate extract of D. bulbifera bulb with second order rate constants of 4.48×106 and 4.46×106 were found to be potent scavengers of pulse radiolysis generated OH radical. G. glauca leaf and stem showed excellent reducing activity and free radical scavenging activity. HPTLC fingerprinting, carried out in mobile phase, chloroform: toluene: ethanol (4: 4: 1, v/v) showed presence of florescent compound at 366 nm as well as UV active compound at 254 nm. GC-TOF-MS analysis revealed the predominance of diphenyl sulfone as major compound in G. glauca. Significant levels of n-hexadecanoic acid and octadecanoic acid were also present. Diosgenin (C27H42O3) and diosgenin (3á,25R) acetate were present as major phytoconstituents in the extracts of D. bulbifera. G. glauca and D. bulbifera contain significant amounts of phytochemicals with antioxidative properties that can be exploited as a potential source for herbal remedy for oxidative stress induced diseases. These results rationalize further investigation in the potential discovery of new natural bioactive principles from these two important medicinal plants. PMID:24367520

  15. Identification and functional analysis of cytochrome P450 complement in Streptomyces virginiae IBL14

    Science.gov (United States)

    2013-01-01

    Background As well known, both natural and synthetic steroidal compounds are powerful endocrine disrupting compounds (EDCs) which can cause reproductive toxicity and affect cellular development in mammals and thus are generally regarded as serious contributors to water pollution. Streptomyces virginiae IBL14 is an effective degradative strain for many steroidal compounds and can also catalyze the C25 hydroxylation of diosgenin, the first-ever biotransformation found on the F-ring of diosgenin. Results To completely elucidate the hydroxylation function of cytochrome P450 genes (CYPs) found during biotransformation of steroids by S. virginiae IBL14, the whole genome sequencing of this strain was carried out via 454 Sequencing Systems. The analytical results of BLASTP showed that the strain IBL14 contains 33 CYPs, 7 ferredoxins and 3 ferredoxin reductases in its 8.0 Mb linear chromosome. CYPs from S. virginiae IBL14 are phylogenetically closed to those of Streptomyces sp. Mg1 and Streptomyces sp. C. One new subfamily was found as per the fact that the CYP Svu001 in S. virginiae IBL14 shares 66% identity only to that (ZP_05001937, protein identifer) from Streptomyces sp. Mg1. Further analysis showed that among all of the 33 CYPs in S. virginiae IBL14, three CYPs are clustered with ferredoxins, one with ferredoxin and ferredoxin reductase and three CYPs with ATP/GTP binding proteins, four CYPs arranged with transcriptional regulatory genes and one CYP located on the upstream of an ATP-binding protein and transcriptional regulators as well as four CYPs associated with other functional genes involved in secondary metabolism and degradation. Conclusions These characteristics found in CYPs from S. virginiae IBL14 show that the EXXR motif in the K-helix is not absolutely conserved in CYP157 family and I-helix not absolutely essential for the CYP structure, too. Experimental results showed that both CYP Svh01 and CYP Svu022 are two hydroxylases, capable of bioconverting

  16. Biodegradation of furfural by Bacillus subtilis strain DS3.

    Science.gov (United States)

    Zheng, Dan; Bao, Jianguo; Lu, Jueming; Lv, Quanxi

    2015-07-01

    An aerobic bacterial strain DS3, capable of growing on furfural as sole carbon source, was isolated from actived sludge of wastewater treatment plant in a diosgenin factory after enrichment. Based on morphological physiological tests as well as 16SrDNA sequence and Biolog analyses it was identified as Bacillus subtilis. The study revealed that strain DS3 utilized furfural, as analyzed by high-performance liquid chromatography (HPLC). Under following conditions: pH 8.0, temperature 35 degrees C, 150 rpm and 10% inoculum, strain DS3 showed 31.2% furfural degradation. Furthermore, DS3 strain was found to tolerate furfural concentration as high as 6000 mg(-1). The ability of Bacillus subtilis strain DS3 to degrade furfural has been demonstrated for the first time in the present study.

  17. Break-through in seed fertility of autotetraploid Trigonella foenum graecum

    Energy Technology Data Exchange (ETDEWEB)

    Raghuvanshi, S S; Agrawal, Poonam; Singh, Jaya; Singh, Anil K [Plant Genetics Unit, Botany Department, Lucknow University, Lucknow (India)

    1990-01-01

    Full text: Fenugreek is an important legume crop in tropical and subtropical zones of India, used as green vegetable, cattle fodder, food flavourant and for pharmaceutical purposes. The seeds are a source of diosgenin, a steroid sapogenin used for synthesis of steroidal drugs like corticosteroide sex hormone and oral contraceptives. Seeds valuing 15-20 million rupees are exported annually. Polyploids are vegetatively superior but have poorer seed fertility. Cross breeding among locally collected germplasm and autopolyploidisation did not give satisfactory results. Mutation induction using gamma rays or EMS alone and in combination was undertaken to broaden the variability for increased grain yield. In M{sub 3}, mutants were selected with up to 143 pods per plant, compared to 80 in the diploid progenitors and up to 123 In advanced hybrids. 11 promising high yielding lines will be further evaluated. (author)

  18. (25R-6α-Hydroxy-5α-spirostan-3β-yl tosylate

    Directory of Open Access Journals (Sweden)

    María A. Fernández-Herrera

    2012-12-01

    Full Text Available The title steroid, C34H50O6S, is an intermediate on the synthetic route between diosgenin and brassinosteroids, which possess the A ring modified with the 2α,3α-diol functionality. The polycyclic spirostan system has the expected conformation, with six-membered rings adopting chair forms and the five-membered rings envelope forms (flap atoms are the methine C atom in the C/D-ring junction and the spiro C atom connecting rings E and F. The 3β-tosylate group is oriented in such a way that S=O bonds are engaged in intermolecular hydrogen bonds with O—H and C—H donors. Chains of molecules are formed along [100] via O—H...O hydrogen bonds, and secondary weak C—H...O interactions connect two neighbouring chains in the [001] direction.

  19. Break-through in seed fertility of autotetraploid Trigonella foenum graecum

    International Nuclear Information System (INIS)

    Raghuvanshi, S.S.; Agrawal, Poonam; Singh, Jaya; Singh, Anil K.

    1990-01-01

    Full text: Fenugreek is an important legume crop in tropical and subtropical zones of India, used as green vegetable, cattle fodder, food flavourant and for pharmaceutical purposes. The seeds are a source of diosgenin, a steroid sapogenin used for synthesis of steroidal drugs like corticosteroide sex hormone and oral contraceptives. Seeds valuing 15-20 million rupees are exported annually. Polyploids are vegetatively superior but have poorer seed fertility. Cross breeding among locally collected germplasm and autopolyploidisation did not give satisfactory results. Mutation induction using gamma rays or EMS alone and in combination was undertaken to broaden the variability for increased grain yield. In M 3 , mutants were selected with up to 143 pods per plant, compared to 80 in the diploid progenitors and up to 123 In advanced hybrids. 11 promising high yielding lines will be further evaluated. (author)

  20. Divergent Synthesis of Solanidine and 22-epi-Solanidine.

    Science.gov (United States)

    Hou, Ling-Li; Shi, Yong; Zhang, Zhi-Dan; Wu, Jing-Jing; Yang, Qing-Xiong; Tian, Wei-Sheng

    2017-07-21

    A divergent synthesis of solanidine and 22-epi-solanidine, two 25S natural steroidal alkaloids, from 25R-configured diosgenin acetate, is described. Initially, solanidine was synthesized through a series of transformations including a cascade ring-switching process of furostan-26-acid, an epimerization of C25 controlled by the conformation of six-membered lactone ring, an intramolecular Schmidt reaction, and an imine reduction/intramolecular aminolysis process. To address the epimerization issue during Schmidt reaction, an improved synthesis was developed, which also led to a synthesis of 22-epi-solanidine. In this synthesis, selective transformation of azido lactone to azido diol and amino diol was realized through a reduction relay tactic. The azido diol was transformed to solanidine via an intramolecular Schmidt reaction/N-alkylation/reduction process and to 22-epi-solanidine via an intramolecular double N-alkylation process.

  1. Targeting Inflammatory Pathways by Triterpenoids for Prevention and Treatment of Cancer

    Directory of Open Access Journals (Sweden)

    Bharat B. Aggarwal

    2010-10-01

    Full Text Available Traditional medicine and diet has served mankind through the ages for prevention and treatment of most chronic diseases. Mounting evidence suggests that chronic inflammation mediates most chronic diseases, including cancer. More than other transcription factors, nuclear factor-kappaB (NF-κB and STAT3 have emerged as major regulators of inflammation, cellular transformation, and tumor cell survival, proliferation, invasion, angiogenesis, and metastasis. Thus, agents that can inhibit NF-κB and STAT3 activation pathways have the potential to both prevent and treat cancer. In this review, we examine the potential of one group of compounds called triterpenes, derived from traditional medicine and diet for their ability to suppress inflammatory pathways linked to tumorigenesis. These triterpenes include avicins, betulinic acid, boswellic acid, celastrol, diosgenin, madecassic acid, maslinic acid, momordin, saikosaponins, platycodon, pristimerin, ursolic acid, and withanolide. This review thus supports the famous adage of Hippocrates, “Let food be thy medicine and medicine be thy food”.

  2. The mTOR signalling pathway in cancer and the potential mTOR inhibitory activities of natural phytochemicals.

    Science.gov (United States)

    Tan, Heng Kean; Moad, Ahmed Ismail Hassan; Tan, Mei Lan

    2014-01-01

    The mammalian target of rapamycin (mTOR) kinase plays an important role in regulating cell growth and cell cycle progression in response to cellular signals. It is a key regulator of cell proliferation and many upstream activators and downstream effectors of mTOR are known to be deregulated in various types of cancers. Since the mTOR signalling pathway is commonly activated in human cancers, many researchers are actively developing inhibitors that target key components in the pathway and some of these drugs are already on the market. Numerous preclinical investigations have also suggested that some herbs and natural phytochemicals, such as curcumin, resveratrol, timosaponin III, gallic acid, diosgenin, pomegranate, epigallocatechin gallate (EGCC), genistein and 3,3'-diindolylmethane inhibit the mTOR pathway either directly or indirectly. Some of these natural compounds are also in the clinical trial stage. In this review, the potential anti-cancer and chemopreventive activities and the current status of clinical trials of these phytochemicals are discussed.

  3. Ekstrak Biji Klabet Menurunkan Jumlah Sel Spermatozoa pada Kelinci

    Directory of Open Access Journals (Sweden)

    I Gusti Nyoman Sri Wiryawan

    2009-06-01

    Full Text Available Fenugreek seed (Trigonella foenum-graecum contains saponin diosgenin, wich has an antifertility effect on spermatozoa so it can be used as an oral contraceptive drug. This study was aimedto investigate the effect of fenugreek seed extract to spermatogenic process of rabbit, especially onviability spermatozoa. “Completely randomized control group post-test only design” was used inthis study. The animals were divided into four groups; one control group and three treatmentgroups with six replicates (P0 = control group; P1 = group were given 10 % fenugreek seed extract,1 cc/day; P2 = group were given 20 % fenugreek seed extract, 1 cc/day; P3 = group were given 30 %fenugreek seed extract, 1 cc/day. The extract was given orally once a day in 50 days. After treatment,testicles were sectioned and stained with Hematoxylin Eosin; for qualitative and quantitativemicroscopic analysis. The result of this study showed that the number of spermatozoa were decreasedsignificantly (p<0,05 after receiving 10% fenugreek seed extract 1 cc per day. In conclusion,fenugreek seed extract could reduce the number of spermatozoa.

  4. Top 10 botanical ingredients in 2010 anti-aging creams.

    Science.gov (United States)

    Cronin, Hyland; Draelos, Zoe Diana

    2010-09-01

    New developments in the realm of skin rejuvenation such as phytotherapy are at an astounding increasing pace in the cosmeceutical market. Yet, many of these products that are classified as cosmeceuticals are tested less vigorously and do not have to be approved by the Food and Drug Administration to establish efficacy and safety. Thus, as clinicians, we must ask the question, "Is there science-based evidence to validate the mechanism of these new treatments?" We assessed the top anti-aging creams currently on the market specifically evaluating their botanical ingredients. Some of the most common botanicals that are hot off the market are: Rosmarinus officinalis, Vitis vinifera (grape seed extract), Citronellol, Limonene, Oenothera biennis (evening primrose), Glycyrrhiza glabra (licorice extract), Aframomum angustifolium seed extract, Diosgenin (wild yam), N6 furfuryladenine (kinetin), and Ergothioneine. Through researching each of these botanical ingredients, we have concluded that randomized controlled trials are still needed in this area, but there is promise in some of these ingredients and science to validate them. © 2010 Wiley Periodicals, Inc.

  5. Zn(II)-dipicolylamine-based metallo-lipids as novel non-viral gene vectors.

    Science.gov (United States)

    Su, Rong-Chuan; Liu, Qiang; Yi, Wen-Jing; Zhao, Zhi-Gang

    2017-08-01

    In this study, a series of Zn(II)-dipicolylamine (Zn-DPA) based cationic lipids bearing different hydrophobic tails (long chains, α-tocopherol, cholesterol or diosgenin) were synthesized. Structure-activity relationship (SAR) of these lipids was studied in detail by investigating the effects of several structural aspects including the type of hydrophobic tails, the chain length and saturation degree. In addition, several assays were used to study their interactions with plasmid DNA, and results reveal that these lipids could condense DNA into nanosized particles with appropriate size and zeta-potentials. MTT-based cell viability assays showed that lipoplexes 5 had low cytotoxicity. The in vitro gene transfection studies showed the hydrophobic tails clearly affected the TE, and hexadecanol-containing lipid 5b gives the best TE, which was 2.2 times higher than bPEI 25k in the presence of 10% serum. The results not only demonstrate that these lipids might be promising non-viral gene vectors, but also afford us clues for further optimization of lipidic gene delivery materials.

  6. Mechanism of membrane damage by El Tor hemolysin of Vibrio cholerae O1.

    Science.gov (United States)

    Ikigai, H; Akatsuka, A; Tsujiyama, H; Nakae, T; Shimamura, T

    1996-08-01

    El Tor hemolysin (ETH; molecular mass, 65 kDa) derived from Vibrio cholerae O1 spontaneously assembled oligomeric aggregates on the membranes of rabbit erythrocyte ghosts and liposomes. Membrane-associated oligomers were resolved by sodium dodecyl sulfate-polyacrylamide gel electrophoresis and immunoblotting into two to nine bands with apparent molecular masses of 170 to 350 kDa. ETH assembled oligomers on a liposomal membrane consisting of phosphatidylcholine and cholesterol, but not on a membrane of phosphatidylcholine alone. Cholesterol could be replaced with diosgenin or ergosterol but not with 5alpha-cholestane-3-one, suggesting that sterol is essential for the oligomerization. The treatment of carboxyfluorescein-encapsulated liposomes with ETH caused a rapid release of carboxyfluorescein into the medium. Because dextrin 20 (molecular mass, 900 Da) osmotically protected ETH-mediated hemolysis, this hemolysis is likely to be caused by pore formation on the membrane. The pore size(s) estimated from osmotic protection assays was in the range of 1.2 to 1.6 nm. The pore formed on a rabbit erythrocyte membrane was confirmed morphologically by electron microscopy. Thus, we provide evidence that ETH damages the target by the assembly of hemolysin oligomers and pore formation on the membrane.

  7. Nutrient digestibility and beef cattle performance fed by lerak (Sapindus rarak meal in concentrate ration

    Directory of Open Access Journals (Sweden)

    S. Suharti

    2009-10-01

    Full Text Available This research was aimed to study the use of Lerak fruit meal to improve performance and feed digestibility of beef cattle. The research consisted of two trials (in vitro and in vivo studies. The in vitro trial was screening of bioactive compounds (saponin, tanin, dan diosgenin in Lerak fruit (including seed and continued to evaluate the effectivity of these compounds against ruminal protozoa. The in vivo study was done using 12 Ongole Crossbreed cattle which received 1of 3 different treatments: 1 concentrate without Lerak as control, 2 concentrate containing 2.5% Lerak, and 3 concentrate containing 5% Lerak. Anti protozoal activity, daily gain, and nutrient digestibility of beef cattle were measured. Results showed that saponin concentration in Lerak extracted by methanol was higher than that in Lerak extracted by water and Lerak meal, 81.5%; 8.2% and 3.85% respectively. Lerak extracted by methanol have higher antiprotozoal activity in vitro than Lerak extracted by water. In vivo experiment showed that there were no significant differences (P>0.05 of nutrient intake and digestibility in all treatments, that means the ration had good palatability and quality. Average daily gain of PO fed 2.5% Lerak was 20% higher than that of control diet (0.9 kg/day.

  8. Cancer Cell Signaling Pathways Targeted by Spice-Derived Nutraceuticals

    Science.gov (United States)

    Sung, Bokyung; Prasad, Sahdeo; Yadav, Vivek R.; Aggarwal, Bharat B.

    2012-01-01

    Extensive research within the last half a century has revealed that cancer is caused by dysregulation of as many as 500 different gene products. Most natural products target multiple gene products and thus are ideally suited for prevention and treatment of various chronic diseases, including cancer. Dietary agents such as spices have been used extensively in the Eastern world for a variety of ailments for millennia, and five centuries ago they took a golden journey to the Western world. Various spice-derived nutraceuticals, including 1′-acetoxychavicol acetate, anethole, capsaicin, car-damonin, curcumin, dibenzoylmethane, diosgenin, eugenol, gambogic acid, gingerol, thymoquinone, ursolic acid, xanthohumol, and zerumbone derived from galangal, anise, red chili, black cardamom, turmeric, licorice, fenugreek, clove, kokum, ginger, black cumin, rosemary, hop, and pinecone ginger, respectively, are the focus of this review. The modulation of various transcription factors, growth factors, protein kinases, and inflammatory mediators by these spice-derived nutraceuticals are described. The anticancer potential through the modulation of various targets is also the subject of this review. Although they have always been used to improve taste and color and as a preservative, they are now also used for prevention and treatment of a wide variety of chronic inflammatory diseases, including cancer. PMID:22149093

  9. Purification, characterization, and substrate specificity of a glucoamylase with steroidal saponin-rhamnosidase activity from Curvularia lunata.

    Science.gov (United States)

    Feng, Bing; Hu, Wei; Ma, Bai-ping; Wang, Yong-ze; Huang, Hong-ze; Wang, Sheng-qi; Qian, Xiao-hong

    2007-10-01

    It has been previously reported that a glucoamylase from Curvularia lunata is able to hydrolyze the terminal 1,2-linked rhamnosyl residues of sugar chains at C-3 position of steroidal saponins. In this work, the enzyme was isolated and identified after isolation and purification by column chromatography including gel filtration and ion-exchange chromatography. Analysis of protein fragments by MALDI-TOF/TOF proteomics Analyzer indicated the enzyme to be 1,4-alpha-D-glucan glucohydrolase EC 3.2.1.3, GA and had considerable homology with the glucoamylase from Aspergillus oryzae. We first found that the glucoamylase was produced from C. lunata and was able to hydrolyze the terminal rhamnosyl of steroidal saponins. The enzyme had the general character of glucoamylase, which hydrolyze starch. It had a molecular mass of 66 kDa and was optimally active at 50 degrees C, pH 4, and specific activity of 12.34 U mg of total protein(-1) under the conditions, using diosgenin-3-O-alpha-L-rhamnopyranosyl(1-->4)-[alpha-L-rhamnopyranosyl (1-->2)]-beta-D-glucopyranoside (compound II) as the substrate. Furthermore, four kinds of commercial glucoamylases from Aspergillus niger were investigated in this work, and they had the similar activity in hydrolyzing terminal rhamnosyl residues of steroidal saponin.

  10. Edible provenances of Jatropha curcas from Quintana Roo state of Mexico and effect of roasting on antinutrient and toxic factors in seeds.

    Science.gov (United States)

    Makkar, H P; Becker, K; Schmook, B

    1998-01-01

    Seven seed samples of J. curcas, both in raw and roasted state, sold in some villages in Quintana Roo state, Mexico for human consumption were analyzed for physical characteristics, nutrients and antinutrients. The average seed weight varied from 0.53 to 0.74 g and kernel weight as proportion of raw seed weight was from 61 to 66%. The contents of crude protein, lipid and ash of kernels from raw seeds were 27-30%, 55-62% and 3.7-5.2% respectively. The levels of antinutrients in meal from the raw seeds were: trypsin inhibitor activity (14.6-28.7 mg trypsin inhibited/g), lectin (25.6-52.2 unit; one unit is the reverse of minimum amount of mg meal/ml assay which produced haemagglutination), saponins (1.9-2.3% as diosgenin equivalent) and phytate (8.4-10%). Phorbol esters in kernels from raw seeds were not detected in four samples and in other three samples it ranged from 0.01 to 0.02 mg/g as phorbol-12-myristate 13-acetate equivalent. Roasting of seeds inactivated almost 100% of trypsin inhibitor activity. Although lectin activity reduced on roasting, it was still present in high amounts. Saponins, phytate and phorbol esters were not affected by roasting.

  11. Effect of Detergents on Galactoside Binding by Melibiose Permeases.

    Science.gov (United States)

    Amin, Anowarul; Hariharan, Parameswaran; Chae, Pil Seok; Guan, Lan

    2015-09-29

    The effect of various detergents on the stability and function of the melibiose permeases of Escherichia coli (MelBEc) and Salmonella typhimurium (MelBSt) was studied. In n-dodecyl-β-d-maltoside (DDM) or n-undecyl-β-d-maltoside (UDM), WT MelBSt binds melibiose with an affinity similar to that in the membrane. However, with WT MelBEc or MelBSt mutants (Arg141 → Cys, Arg295 → Cys, or Arg363 → Cys), galactoside binding is not detected in these detergents, but binding to the phosphotransferase protein IIA(Glc) is maintained. In the amphiphiles lauryl maltose neopentyl glycol (MNG-3) or glyco-diosgenin (GDN), galactoside binding with all of the MelB proteins is observed, with slightly reduced affinities. MelBSt is more thermostable than MelBEc, and the thermostability of either MelB is largely increased in MNG-3 or GDN. Therefore, the functional defect with DDM or UDM likely results from the relative instability of the sensitive MelB proteins, and stability, as well as galactoside binding, is retained in MNG-3 or GDN. Furthermore, isothermal titration calorimetry of melibiose binding with MelBSt shows that the favorable entropic contribution to the binding free energy is decreased in MNG-3, indicating that the conformational dynamics of MelB is restricted in this detergent.

  12. Selected herbals and human exercise performance.

    Science.gov (United States)

    Bucci, L R

    2000-08-01

    Herbs have been used throughout history to enhance physical performance, but scientific scrutiny with controlled clinical trials has only recently been used to study such effects. The following herbs are currently used to enhance physical performance regardless of scientific evidence of effect: Chinese, Korean, and American ginsengs; Siberian ginseng, mahuang or Chinese ephedra; ashwagandha; rhodiola; yohimbe; CORDYCEPS: fungus, shilajit or mummio; smilax; wild oats; Muira puama; suma (ecdysterone); Tribulus terrestris; saw palmetto berries; beta-sitosterol and other related sterols; and wild yams (diosgenin). Controlled studies of Asian ginsengs found improvements in exercise performance when most of the following conditions were true: use of standardized root extracts, study duration (>8 wk, daily dose >1 g dried root or equivalent, large number of subjects, and older subjects. Improvements in muscular strength, maximal oxygen uptake, work capacity, fuel homeostasis, serum lactate, heart rate, visual and auditory reaction times, alertness, and psychomotor skills have also been repeatedly documented. Siberian ginseng has shown mixed results. Mahuang, ephedrine, and related alkaloids have not benefited physical performance except when combined with caffeine. Other herbs remain virtually untested. Future research on ergogenic effects of herbs should consider identity and amount of substance or presumed active ingredients administered, dose response, duration of test period, proper experimental controls, measurement of psychological and physiologic parameters (including antioxidant actions), and measurements of performance pertinent to intended uses.

  13. Rapid and sensitive determination of phytosterols in functional foods and medicinal herbs by using UHPLC-MS/MS with microwave-assisted derivatization combined with dual ultrasound-assisted dispersive liquid-liquid microextraction.

    Science.gov (United States)

    Sun, Jing; Zhao, Xian-En; Dang, Jun; Sun, Xiaoyan; Zheng, Longfang; You, Jinmao; Wang, Xiao

    2017-02-01

    In this work, a hyphenated technique of dual ultrasound-assisted dispersive liquid-liquid microextraction combined with microwave-assisted derivatization followed by ultra high performance liquid chromatography tandem mass spectrometry has been developed for the determination of phytosterols in functional foods and medicinal herbs. Multiple reaction monitoring mode was used for the tandem mass spectrometry detection. A mass spectrometry sensitive reagent, 4'-carboxy-substituted rosamine, has been used as the derivatization reagent for five phytosterols, and internal standard diosgenin was used for the first time. Parameters for the dual microextraction, microwave-assisted derivatization, and ultra high performance liquid chromatography tandem mass spectrometry were all optimized in detail. Satisfactory linearity, recovery, repeatability, accuracy and precision, absence of matrix effect, extremely low limits of detection (0.005-0.015 ng/mL) and limits of quantification (0.030-0.10 ng/mL) were achieved. The proposed method was compared with previously reported methods. It showed better sensitivity, selectivity, and accuracy. The matrix effect was also significantly reduced. The proposed method was successfully applied to the determination of five phytosterols in vegetable oil (sunflower oil, olive oil, corn oil, peanut oil), milk and orange juice (soymilk, peanut milk, orange juice), and medicinal herbs (Ginseng, Ganoderma lucidum, Cordyceps, Polygonum multiflorum) for the quality control of functional foods and medicinal herbs. © 2016 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

  14. Association of canalicular membrane enzymes with bile acid micelles and lipid aggregates in human and rat bile.

    Science.gov (United States)

    Accatino, L; Pizarro, M; Solís, N; Koenig, C S

    1995-01-18

    This study was undertaken to gain insights into the characteristics of the polymolecular association between canalicular membrane enzymes, bile acids, cholesterol and phospholipids in bile and into the celular mechanisms whereby the enzymes are secreted into bile. With this purpose, we studied the distribution of bile acids, cholesterol, phospholipids, proteins and representative canalicular membrane enzymes (alkaline phosphatase, 5'-nucleotidase and gamma-glutamyl transpeptidase), which can be considered specific marker constituents, in bile fractions enriched in phospholipid-cholesterol lamellar structures (multilamellar and unilamellar vesicles) and bile acid-mixed micelles. These fractions were isolated by ultracentrifugation from human hepatic bile, normal rat bile and bile of rats treated with diosgenin, a steroid that induces a marked increase in biliary cholesterol secretion, and were characterized by density, lipid composition and transmission electron microscopy. These studies demonstrate that alkaline phosphatase, 5'-nucleotidase and gamma-glutamyl transpeptidase are secreted into both human and rat bile where they are preferentially associated with bile acid-mixed micelles, suggesting a role for bile acids in both release of these enzymes and lipids from the canalicular membrane and solubilization in bile. In addition, heterogeneous association of these enzymes with nonmicellar, lamellar structures in human and rat bile is consistent with the hypothesis that processes independent of the detergent effects of bile acids might also result in the release of specific intrinsic membrane proteins into bile.

  15. The tuber extract and flour of Dioscorea alatanormalize the blood lipid profile of rabbits treated with high cholesterol diets

    Directory of Open Access Journals (Sweden)

    Nelis Imanningsih

    2014-08-01

    Full Text Available AbstrakLatar belakang: Umbi Dioscorea alata (DA memiliki potensi untuk mencegah kondisi hiperlipidemia karena mengandung senyawa bioaktif antosianin, serat pangan, dan diosgenin yang bermanfaat dalam menormalkan kadar lipida darah. Pada penelitian ini dipelajari pengaruh pemberian ekstrak air dan tepung umbi DA dalam menormalkan profil lipida darah kelinci yang diberi ransum tinggi kolesterol.Metode: Ekstrak dan tepung umbi DA diberikan kepada kelinci percobaan selama 60 hari dengan disain penelitian rancangan acak lengkap. Perlakuan ransum sebagai berikut: 1 Ransum basal sebagai kontrol negatif (K0, 2 Ransum basal + kolesterol 0.5% sebagai kontrol positif (K1, 3 Ransum basal+kolesterol 0.5% + ekstrak DA 1.8 g/100 g (KE1, 4 Ransum basal+kolesterol 0.5%+ekstrak DA 3.6 g/100 g (KE2, 5 Ransum basal mengandung 15% tepung DA + kolesterol 0.5% (KT1 dan 6 Ransum basal mengandung 30% tepung DA + kolesterol 0.5% (KT2. Kadar total kolesterol, LDL, HDL kolesterol dan trigliserida pada serum dianalisa pada awal, hari ke 28, hari ke 56 dan pada akhir penelitian. Hasil: Pemberian ransum tinggi kolesterol sebanyak 1% meningkatkan kadar kolesterol darah sebesar 16 kali dibandingkan kontrol. Pemberian 15% dan 30% tepung DA ransum tinggi kolesterol dapat mempertahakankan profil lipida darah kelinci ke arah normal, khususnya pada substitusi 30% tepung DA. Akan tetapi, ekstrak air tepung DA tidak dapat mempertahankan kadar lipida normal kelinci yang diberi ransum tinggi kolesterol. Kesimpulan:Tepung DA memiliki efek anti-hiperlipidemia. (Health Science Indones 2014;1:23-9Kata kunci:ekstrak, tepung, Dioscorea alata, hiperlipidemiaAbstractBackground: Dioscorea alata(DA tuber has potential to prevent the condition of hyperlipidemia due to the bioactive compound, such as anthocyanins, diosgenin, and dietary fiber that beneficial in normalizing blood lipid profiles. In this research, the effect of water extract and flour of DA tuber administration was examined on

  16. Saponinas esteroidales de la planta Agave brittoniana (Agavaceae con actividad contra el parásito Trichomona vaginalis

    Directory of Open Access Journals (Sweden)

    José Orestes Guerra

    2008-12-01

    the genital tract. To test in vitro the plant against Trichomona vaginalis, the dried and powdered leaves were extracted three times with ethanol-water (7 : 3 by maceration at room temperature. The solvent was removed under reduced pressure and the extract was suspended in distilled water, defatted with n-hexane, and extracted with water-saturated n-butanol. After solvent removal, a portion of the n-butanol extract was hydrolyzed. After extraction with ethyl acetate the hydrolysis products were compared with authentic sapogenins samples using thin layer chromatography (TLC. Most of the sapogenins (yuccagenin and diosgenin were isolated and their structures were confirmed. using nuclear magnetic resonance (NMR experiments. The n-butanol extract was subjected to a separation process through column chromatography to obtain five fractions. After multiple separation processes by reversed phase high performance liquid chromatography (HPLC, the most active one produced one refined fraction that contained two saponins with the same aglycone (diosgenin and one yuccagenin based saponin. Best results of the activity were obtained with the yuccagenin derived glycoside. Rev. Biol. Trop. 56 (4: 16451652. Epub 2008 December 12.

  17. Monitoring of some Wild Plant Species Grown on Natural Radioactive Soils, Wadi EI -Gemal Area, Southeastern Desert, Egypt

    International Nuclear Information System (INIS)

    Morsy, A.M.A.; Afifi, S.Y.

    2008-01-01

    Fore long time ago, human kind has relied on natural products of plants as a primary source for medicine. Herbs, flora, molt and even leeches were employed to bring up relief to the sick and infirmly. As a part of ongoing investigations for the effect of natural radionuclide radiations on biochemical constituents of plants, .two native species (Salvadora persica and Balanites aegyptiaca). grown on virgin radionuclide soils along with Wadi EI-Gemal area, Southeastern Desert, Egypt were collected. This study dealt with amounts of radionuclide taken by plants and their effects on their biochemical constituents, beneficiation uses on remedy of contaminated and even polluted soils and sick treatments as well as exploration of radioactive materials. These plant samples were subjected to certain analysis techniques for the amounts of uranium that were followed by determining carbohydrates, lipids and proteins. The results indicated that both plants uptake uranium but with different amounts. Uranium has a passive effect on the total soluble suger (T.S.S.) of Balanties aegyptiaca plant, while no clear trend appears on T.S.S. of Snlvndora persica root samples. No clear trend appeared for effect of uranium on both fatty acids and amino acids of the investigated plants. Meanwhile uranium has a passive effect on saponin in both plant species, alkaloid in S. persica root and flavonoids in B. aegyptiaca fruits, while showed a positive effect on alkaloids in B. aegyptiaca and no clear trend appeared for flavonoids in S. persica. As for diosgenin uranium has passive effect on its amount in B. aegyptiaca

  18. Fenugreek, A Potent Hypoglycaemic Herb Can Cause Central Hypothyroidism Via Leptin - A Threat To Diabetes Phytotherapy.

    Science.gov (United States)

    Majumdar, Jayjeet; Chakraborty, Pratip; Mitra, Analava; Sarkar, Nirmal Kumar; Sarkar, Supriti

    2017-07-01

    Fenugreek ( Trigonella foenum graecum) , a medicinal herb with potent antihyperglycaemic and hypoglycaemic effects, is used to treat diabetes. This study is aimed to explore the interaction of fenugreek seed extract (FSE) and HPT (hypothalamic-pituitary-thyroid) axis in context of leptin secretion which have important role in normal and type-1 diabetic subjects. FSE (confirmed to contain trigonelline, diosgenin, 4 hydroxyisoleucine) was gavaged (0.25 gm/kg body weight/day) to normal and alloxan-induced type-1 diabetic rats for 4 weeks. Expression of hypothalamic prepro-TRH (Thyrotropin releasing hormone) mRNA, serum levels of TRH, TSH (Thyroid stimulating hormone), fT 3 , fT 4 , insulin, leptin, glucose; thyroperoxidase activity and growth of thyroid gland, food intake, adiposity index were also studied FSE significantly down regulated prepro-TRH mRNA expression; decreased serum TRH, TSH, fT 3 , fT 4 levels, and regressed thyroid gland in FSE-fed normal and diabetic rats than those observed in normal diet-fed control and diabetic rats. FSE decreased (psecretion, increased food intake and body weight in all FSE-fed rats. FSE improved insulin secretion, decreased glucose level but impaired HPT axis in diabetic rats, indicating insulin-independent central hypothyroidism. Results suggested that the dominant signal to hypothalamus suppressing HPT axis is the fall in leptin level which i resulted from decreased adiposity index following FSE feeding. Fenugreek simultaneously having hypoglycaemic and hypothyroidal actions raises questions whether it can be safely used to treat diabetes and/or hyperthyroidism as was suggested by many workers. © Georg Thieme Verlag KG Stuttgart · New York.

  19. Extraction Optimization of Water-Extracted Mycelial Polysaccharide from Endophytic Fungus Fusarium oxysporum Dzf17 by Response Surface Methodology

    Directory of Open Access Journals (Sweden)

    Ligang Zhou

    2012-05-01

    Full Text Available Water-extracted mycelial polysaccharide (WPS from the endophytic fungus Fusarium oxysporum Dzf17 isolated from Dioscorea zingiberensis was found to be an efficient elicitor to enhance diosgenin accumulation in D. zingigerensis cultures, and also demonstrated antioxidant activity. In this study, response surface methodology (RSM was employed to optimize the extraction process of WPS from F. oxysporum Dzf17 using Box-Behnken design (BBD. The ranges of the factors investigated were 1–3 h for extraction time (X1, 80–100 °C for extraction temperature (X2, and 20–40 (v/w for ratio of water volume (mL to raw material weight (g (X3. The experimental data obtained were fitted to a second-order polynomial equation using multiple regression analysis. Statistical analysis showed that the polynomial regression model was in good agreement with the experimental results with the determination coefficient (R2 of 0.9978. By solving the regression equation and analyzing the response surface contour plots, the extraction parameters were optimized as 1.7 h for extraction time, 95 °C for extraction temperature, 39 (v/w for ratio of water volume (mL to raw material weight (g, and with 2 extractions. The maximum value (10.862% of WPS yield was obtained when the WPS extraction process was conducted under the optimal conditions.

  20. Structural requirements of cholesterol for binding to Vibrio cholerae hemolysin.

    Science.gov (United States)

    Ikigai, Hajime; Otsuru, Hiroshi; Yamamoto, Koichiro; Shimamura, Tadakatsu

    2006-01-01

    Cholesterol is necessary for the conversion of Vibrio cholerae hemolysin (VCH) monomers into oligomers in liposome membranes. Using different sterols, we determined the stereochemical structures of the VCH-binding active groups present in cholesterol. The VCH monomers are bound to cholesterol, diosgenin, campesterol, and ergosterol, which have a hydroxyl group at position C-3 (3betaOH) in the A ring and a C-C double bond between positions C-5 and C-6 (C-C Delta(5)) in the B ring. They are not bound to epicholesterol and dihydrocholesterol, which form a covalent link with a 3alphaOH group and a C-C single bond between positions C-5 and C-6, respectively. This result suggests that the 3betaOH group and the C-CDelta(5) bond in cholesterol are required for VCH monomer binding. We further examined VCH oligomer binding to cholesterol. However, this oligomer did not bind to cholesterol, suggesting that the disappearance of the cholesterol-binding potential of the VCH oligomer might be a result of the conformational change caused by the conversion of the monomer into the oligomer. VCH oligomer formation was observed in liposomes containing sterols with the 3betaOH group and the C-C Delta(5) bond, and it correlated with the binding affinity of the monomer to each sterol. Therefore, it seems likely that monomer binding to membrane sterol leads to the assembly of the monomer. However, since oligomer formation was induced by liposomes containing either epicholesterol or dihydrocholesterol, the 3betaOH group and the C-C Delta(5) bond were not essential for conversion into the oligomer.

  1. Chemical characteristics of saponins from Paris fargesii var. brevipetala and cytotoxic activity of its main ingredient, paris saponin H.

    Science.gov (United States)

    Wen, Feiyan; Yin, Hongxiang; Chen, Chu; Liu, Xianbo; Xue, Dan; Chen, Tiezhu; He, Jun; Zhang, Hao

    2012-06-01

    More attention was paid to the anti-tumor activity of Rhizoma Paridis (RP) recently, of which the wild resource was decreased significantly. This study was aimed to elucidate the chemical characteristics of Paris fargesii var. brevipetala (PFB) that may be administrated as alternate resource of legal RP. A HPLC-ELSD method was established to characterize the steroid saponins in rhizomes of PFB and two legal Paris species [Paris polyphylla var. chinensis (PPC) and P. polyphylla var. yunnanensis (PPY)] in Chinese Pharmacopoeia (CP). Ten saponins (paris saponins I, II, V, VI, VII, H, gracillin and other three paris saponins) were involved as standards. The results indicated that PFB contained pennogenyl saponins as the main components with small amounts of diosgenin saponins. The total contents of the detected saponins in PFB ranged from 9.12mg/g to 85.33mg/g. Nine of the twelve PFB samples own a total content of paris saponins I, II, VI, and VII more than 6.0mg/g (meeting the standard of CP 2010 edition). Principal Component Analysis (PCA) and Partial Least Squares-Discriminate Analysis (PLS-DA) both confirmed the fact that saponin profiles of PFB, PPC and PPY were different from each other. In addition, paris saponin H (Ps H), the predominant saponin of PFB (>50%), was tested in vitro to evaluate its cytotoxic activities on HepG2, A549, RPE and L929 cells with a positive control of Cisplatin. Ps H showed a remarkable cytotoxic activity on A549 cells with an IC(50) value of 1.53±0.08μg/mL. Copyright © 2012 Elsevier B.V. All rights reserved.

  2. Phytochemical Analysis and Antimicrobial Activities of Methanolic Extracts of Leaf, Stem and Root from Different Varieties of Labisa pumila Benth

    Directory of Open Access Journals (Sweden)

    Ehsan Karimi

    2011-05-01

    Full Text Available A local herb, Kacip Fatimah, is famous amongst Malay women for its uses in parturition; however, its phytochemical contents have not been fully documented. Therefore, a study was performed to evaluate the phenolics, flavonoids, and total saponin contents, and antibacterial and antifungal properties of the leaf, stem and root of three varieties of Labisia pumila Benth. Total saponins were found to be higher in the leaves of all three varieties, compared to the roots and stems. Leaves of var. pumila exhibited significantly higher total saponin content than var. alata and lanceolata, with values of 56.4, 43.6 and 42.3 mg diosgenin equivalent/g dry weight, respectively. HPLC analyses of phenolics and flavonoids in all three varieties revealed the presence of gallic acid, caffeic acid, rutin, and myricetin in all plant parts. Higher levels of flavonoids (rutin, quercitin, kaempferol were observed in var. pumila compared with alata and lanceolata, whereas higher accumulation of phenolics (gallic acid, pyrogallol was recorded in var. alata, followed by pumila and lanceolata. Antibacterial activities of leaf, stem and root extracts of all varieties determined against both Gram positive (Micrococcus luteus, Bacillus subtilis B145, Bacillus cereus B43, Staphylococcus aureus S1431 and Gram negative (Enterobacter aerogenes, Klebsiella pneumonia K36, Escherichia coli E256, Pseudomonas aeruginosa PI96 pathogens showed that crude methanolic extracts are active against these bacteria at low concentrations, albeit with lower antibacterial activity compared to kanamycin used as the control. Antifungal activity of methanolic extracts of all plant parts against Fusarium sp., Candida sp. and Mucor using the agar diffusion disc exhibited moderate to appreciable antifungal activities compared to streptomycin used as positive control.

  3. Phyto chemical Protection against Diethylnitrosoamine Induced Hepato carcinogenesis by Trigonella foenum graecum in Female Rats

    Energy Technology Data Exchange (ETDEWEB)

    Abdelgawad, M R; Mustafa, M M.M.; Kottb, M K.I. [Egyptian Atomic Energy Authority, Nuclear Research Center, Biological Applications Department, Cairo (Egypt)

    2012-05-15

    Trigonella foenum graecum (fenugreek) is traditionally used to treat. Recent studies suggest that fenugreek and its active constituents may possess anti carcinogenic potential. The preventive efficacy of dietary fenugreek seed 2% and 4% (w/w feed) on diethylnitrosamine-induced rat liver carcinogenesis were evaluated. Rats were sacrificed when rats became very weak with unstable shelf live were chosen as an end point. Egypt is an Islamic country alcoholic prohibition so the possible use of ethanol extraction may be accepted with high restriction towards its applications in human, that it may affect the active constituents of fenugreek seeds. Whereby, fenugreek seeds contain >8% oil, many valuable phenolic compounds, protein and amino acids, etc ... with different concentrations according to the extraction method. So, the present study was carried out to evaluate the effect of fenugreek powder on adult female rats fed experimental diets containing 2% or 4% (w/w) fenugreek seed powder (FSP) for 2 weeks and have phenobarbital in a dose of 200 mg/L ad lib. before and after a single injection with diethylnitrosamine (200 mg/kg body weight). Rats were sacrificed 20 weeks after intra-peritoneal (i.p) diethylnitrosamine injection and their livers, spleens, kidneys and lungs were excised washed well with cold saline, weighted and processed through paraffin wax preparation, staining and pathological changes were examined. It was found that, by comparison with control, continuous feeding of FSP 2% and 4% suppressed hepatocarcinogensity up to 20% and 50%, respectively. In addition, on the basis of these findings, the invaluable and precious fenugreek constituents are diosgenin [(25 R)-5-spirosten-3h-ol] and [5,7-dihydroxy-2-(4-hydroxyphenyl)-6-(3,4,5-trihydroxy-6(hydroxymethyl) tetra- hydro-2H-pyran-2-yl)chroman-4-one] besides, others. Finally, fenugreek seeds seem to have potential role as a novel cancer preventive agent and that needs further investigations

  4. Cyclopamine and jervine induce COX-2 overexpression in human erythroleukemia cells but only cyclopamine has a pro-apoptotic effect

    International Nuclear Information System (INIS)

    Ghezali, Lamia; Leger, David Yannick; Limami, Youness; Cook-Moreau, Jeanne; Beneytout, Jean-Louis; Liagre, Bertrand

    2013-01-01

    Erythroleukemia is generally associated with a very poor response and survival to current available therapeutic agents. Cyclooxygenase-2 (COX-2) has been described to play a crucial role in the proliferation and differentiation of leukemia cells, this enzyme seems to play an important role in chemoresistance in different cancer types. Previously, we demonstrated that diosgenin, a plant steroid, induced apoptosis in HEL cells with concomitant COX-2 overexpression. In this study, we investigated the antiproliferative and apoptotic effects of cyclopamine and jervine, two steroidal alkaloids with similar structures, on HEL and TF1a human erythroleukemia cell lines and, for the first time, their effect on COX-2 expression. Cyclopamine, but not jervine, inhibited cell proliferation and induced apoptosis in these cells. Both compounds induced COX-2 overexpression which was responsible for apoptosis resistance. In jervine-treated cells, COX-2 overexpression was NF-κB dependent. Inhibition of NF-κB reduced COX-2 overexpression and induced apoptosis. In addition, cyclopamine induced apoptosis and COX-2 overexpression via PKC activation. Inhibition of the PKC pathway reduced both apoptosis and COX-2 overexpression in both cell lines. Furthermore, we demonstrated that the p38/COX-2 pathway was involved in resistance to cyclopamine-induced apoptosis since p38 inhibition reduced COX-2 overexpression and increased apoptosis in both cell lines. - Highlights: ► Cyclopamine alone but not jervine induces apoptosis in human erythroleukemia cells. ► Cyclopamine and jervine induce COX-2 overexpression. ► COX-2 overexpression is implicated in resistance to cyclopamine-induced apoptosis. ► Apoptotic potential of jervine is restrained by NF-κB pathway activation. ► PKC is involved in cyclopamine-induced apoptosis and COX-2 overexpression

  5. Cyclopamine and jervine induce COX-2 overexpression in human erythroleukemia cells but only cyclopamine has a pro-apoptotic effect

    Energy Technology Data Exchange (ETDEWEB)

    Ghezali, Lamia; Leger, David Yannick; Limami, Youness [Université de Limoges, FR 3503 GEIST, EA 1069 “Laboratoire de Chimie des Substances Naturelles”, GDR CNRS 3049, Faculté de Pharmacie, Laboratoire de Biochimie et Biologie Moléculaire, 2 rue du Docteur Marcland, 87025 Limoges Cedex (France); Cook-Moreau, Jeanne [Université de Limoges, FR 3503 GEIST, UMR CNRS 7276 “Contrôle de la réponse immune B et lymphoproliférations”, Faculté de Médecine, 2 rue du Docteur Marcland, 87025 Limoges Cedex (France); Beneytout, Jean-Louis [Université de Limoges, FR 3503 GEIST, EA 1069 “Laboratoire de Chimie des Substances Naturelles”, GDR CNRS 3049, Faculté de Pharmacie, Laboratoire de Biochimie et Biologie Moléculaire, 2 rue du Docteur Marcland, 87025 Limoges Cedex (France); Liagre, Bertrand, E-mail: bertrand.liagre@unilim.fr [Université de Limoges, FR 3503 GEIST, EA 1069 “Laboratoire de Chimie des Substances Naturelles”, GDR CNRS 3049, Faculté de Pharmacie, Laboratoire de Biochimie et Biologie Moléculaire, 2 rue du Docteur Marcland, 87025 Limoges Cedex (France)

    2013-04-15

    Erythroleukemia is generally associated with a very poor response and survival to current available therapeutic agents. Cyclooxygenase-2 (COX-2) has been described to play a crucial role in the proliferation and differentiation of leukemia cells, this enzyme seems to play an important role in chemoresistance in different cancer types. Previously, we demonstrated that diosgenin, a plant steroid, induced apoptosis in HEL cells with concomitant COX-2 overexpression. In this study, we investigated the antiproliferative and apoptotic effects of cyclopamine and jervine, two steroidal alkaloids with similar structures, on HEL and TF1a human erythroleukemia cell lines and, for the first time, their effect on COX-2 expression. Cyclopamine, but not jervine, inhibited cell proliferation and induced apoptosis in these cells. Both compounds induced COX-2 overexpression which was responsible for apoptosis resistance. In jervine-treated cells, COX-2 overexpression was NF-κB dependent. Inhibition of NF-κB reduced COX-2 overexpression and induced apoptosis. In addition, cyclopamine induced apoptosis and COX-2 overexpression via PKC activation. Inhibition of the PKC pathway reduced both apoptosis and COX-2 overexpression in both cell lines. Furthermore, we demonstrated that the p38/COX-2 pathway was involved in resistance to cyclopamine-induced apoptosis since p38 inhibition reduced COX-2 overexpression and increased apoptosis in both cell lines. - Highlights: ► Cyclopamine alone but not jervine induces apoptosis in human erythroleukemia cells. ► Cyclopamine and jervine induce COX-2 overexpression. ► COX-2 overexpression is implicated in resistance to cyclopamine-induced apoptosis. ► Apoptotic potential of jervine is restrained by NF-κB pathway activation. ► PKC is involved in cyclopamine-induced apoptosis and COX-2 overexpression.

  6. Mitochondrial dysfunction in H9c2 cells during ischemia and amelioration with Tribulus terrestris L.

    Science.gov (United States)

    Reshma, P L; Sainu, Neethu S; Mathew, Anil K; Raghu, K G

    2016-05-01

    The present study investigates the protective effect of partially characterized Tribulus terrestris L. fruit methanol extract against mitochondrial dysfunction in cell based (H9c2) myocardial ischemia model. To induce ischemia, the cells were maintained in an ischemic buffer (composition in mM -137 NaCl, 12 KCl, 0.5 MgCl2, 0.9 CaCl2, 20 HEPES, 20 2-deoxy-d-glucose, pH-6.2) at 37°C with 0.1% O2, 5% CO2, and 95% N2 in a hypoxia incubator for 1h. Cells were pretreated with various concentrations of T. terrestris L. fruit methanol extract (10 and 25μg/ml) and Cyclosporin A (1μM) for 24h prior to the induction of ischemia. Different parameters like lactate dehydrogenase release, total antioxidant capacity, glutathione content and antioxidant enzymes were investigated. Studies were conducted on mitochondria by analyzing alterations in mitochondrial membrane potential, integrity, and dynamics (fission and fusion proteins - Mfn1, Mfn2, OPA1, Drp1 and Fis1). Various biochemical processes in mitochondria like activity of electron transport chain (ETC) complexes, oxygen consumption and ATP production was measured. Ischemia for 1h caused a significant (p≤0.05) increase in LDH leakage, decrease in antioxidant activity and caused mitochondrial dysfunction. T. terrestris L. fruit methanol extract pretreatment was found effective in safeguarding mitochondria via its antioxidant potential, mediated through various bioactives. HPLC of T. terrestris L. fruit methanol extract revealed the presence of ferulic acid, phloridzin and diosgenin. T. terrestris L. fruit ameliorate ischemic insult in H9c2 cells by safeguarding mitochondrial function. This validates the use of T. terrestris L. against heart disorders. Copyright © 2016 Elsevier Inc. All rights reserved.

  7. Synthesis of silver nanoparticles using Dioscorea bulbifera tuber extract and evaluation of its synergistic potential in combination with antimicrobial agents.

    Science.gov (United States)

    Ghosh, Sougata; Patil, Sumersing; Ahire, Mehul; Kitture, Rohini; Kale, Sangeeta; Pardesi, Karishma; Cameotra, Swaranjit S; Bellare, Jayesh; Dhavale, Dilip D; Jabgunde, Amit; Chopade, Balu A

    2012-01-01

    Development of an environmentally benign process for the synthesis of silver nanomaterials is an important aspect of current nanotechnology research. Among the 600 species of the genus Dioscorea, Dioscorea bulbifera has profound therapeutic applications due to its unique phytochemistry. In this paper, we report on the rapid synthesis of silver nanoparticles by reduction of aqueous Ag(+) ions using D. bulbifera tuber extract. Phytochemical analysis revealed that D. bulbifera tuber extract is rich in flavonoid, phenolics, reducing sugars, starch, diosgenin, ascorbic acid, and citric acid. The biosynthesis process was quite fast, and silver nanoparticles were formed within 5 hours. Ultraviolet-visible absorption spectroscopy, transmission electron microscopy, high-resolution transmission electron microscopy, energy dispersive spectroscopy, and x-ray diffraction confirmed reduction of the Ag(+) ions. Varied morphology of the bioreduced silver nanoparticles included spheres, triangles, and hexagons. Optimization studies revealed that the maximum rate of synthesis could be achieved with 0.7 mM AgNO(3) solution at 50°C in 5 hours. The resulting silver nanoparticles were found to possess potent antibacterial activity against both Gram-negative and Gram-positive bacteria. Beta-lactam (piperacillin) and macrolide (eryth-romycin) antibiotics showed a 3.6-fold and 3-fold increase, respectively, in combination with silver nanoparticles selectively against multidrug-resistant Acinetobacter baumannii. Notable synergy was seen between silver nanoparticles and chloramphenicol or vancomycin against Pseudomonas aeruginosa, and was supported by a 4.9-fold and 4.2-fold increase in zone diameter, respectively. Similarly, we found a maximum 11.8-fold increase in zone diameter of streptomycin when combined with silver nanoparticles against E. coli, providing strong evidence for the synergistic action of a combination of antibiotics and silver nanoparticles. This is the first report on

  8. The function of androgen/androgen receptor and insulin growth factor‑1/insulin growth factor‑1 receptor on the effects of Tribulus terrestris extracts in rats undergoing high intensity exercise.

    Science.gov (United States)

    Wu, Yin; Yang, Hongfang; Wang, Xiaohui

    2017-09-01

    Our previous study demonstrated that treatment with Tribulus terrestris (TT) extracts (120 mg/kg) promoted the muscle weight gain and performance of rats undergoing high intensity exercise. The present study was designed to explore the mechanisms underlying the effect of treatment with TT extracts and the involvement of androgens, the androgen receptor (AR), insulin growth factor‑1 (IGF‑1) and the IGF‑1 receptor (IGF‑1R). A total of 32 Sprague‑Dawley rats were randomly divided into groups as follows: Control; TT, treated with TT extracts, E, high intensity exercise; E+TT, high intensity exercise plus TT treatment. The rats of the E and E+TT groups underwent high intensity exercise with a progressively increasing load for 5 weeks, and TT extracts were intragastrically administered in the TT and E+TT rats 30 min prior to training. TT extract composition was analyzed using ultra‑high performance liquid chromatography‑quadrupole‑time of flight mass spectrometry. Testosterone and IGF‑1 plasma levels and AR, IGF‑1R and myosin heavy chain (MHC) protein levels in muscles were determined by ELISA and western blotting, respectively. The saponins tigogenin and diosgenin comprised ~71.35% of the total peak area. Compared with the E group, TT extracts increased the testosterone and IGF‑1 plasma levels, and AR, IGF‑1R and MHC protein levels in the gastrocnemius of rats undergoing high intensity exercise, accompanied with increased body weight and gastrocnemius weight. In conclusion, the effect of TT extracts on the performance of high intensity exercise rats may be attributed to increased levels of circulating testosterone and IGF‑1 and increased AR and IGF‑1R protein expression levels in the gastrocnemius, resulting in increased muscle weight and increased MHC in the gastrocnemius. The present study provided preliminary evidence supporting the use of TT extracts as a dietary supplement for the promotion of skeletal muscle mass increase and the

  9. Effect and mechanism of dioscin from Dioscorea spongiosa on uric acid excretion in animal model of hyperuricemia.

    Science.gov (United States)

    Zhang, Yi; Jin, Lijun; Liu, Jinchang; Wang, Wei; Yu, Haiyang; Li, Jian; Chen, Qian; Wang, Tao

    2018-03-25

    Dioscin, a spirostane glycoside, the rhizoma of Dioscorea septemloba (Diocoreacea) is used for diuresis, rheumatism, and joints pain. Given the poor solubility and stability of Dioscin, we proposed a hypothesis that Dioscin's metabolite(s) are the active substance(s) in vivo to contribute to the reducing effects on serum uric acid levels. The aim of this study is to identify the active metabolite(s) of Dioscin in vivo and to explore the mechanism of its antihyperuricemic activity. After oral administration of Dioscin in potassium oxonate (PO) induced hyperuricemia rats and adenine-PO induced hyperuricemia mice models, serum uric acid and creatinine levels, clearance of uric acid and creatinine, fractional excretion of uric acid, and renal pathological lesions were determined were used to evaluate the antihyperuricemic effects. Renal glucose transporter-9 (GLUT-9) and organic anion transporter-1 (OAT-1) expressions were analyzed by western blotting method. Renal uric acid excretion was evaluated using stably urate transporter-1 (URAT-1) transfected human epithelial kidney cell line. Intestinal uric acid excretion was evaluated by measuring the transcellular transport of uric acid in HCT116 cells. In hyperuricemia rats, both 25 and 50mg/kg of oral Dioscin decreased serum uric acid levels over 4h. In the hyperuricemia mice, two weeks treatment of Dioscin significantly decreased serum uric acid and creatinine levels, increased clearance of uric acid and creatinine, increased fractional excretion of uric acid, and reduced renal pathological lesions caused by hyperuricemia. In addition, renal GLUT -9 was significantly down-regulated and OAT-1 was up-regulated in Dioscin treated hyperuricemia mice. Dioscin's metabolite Tigogenin significantly inhibited uric acid re-absorption via URAT1 from 10 to 100μM. Diosgenin and Tigogenin increased uric acid excretion via ATP binding cassette subfamily G member 2 (ABCG2). Decreasing effect of Dioscin on serum uric acid level and

  10. Anti-staphylococcal properties of Eichhornia crassipes, Pistacia vera, and Ziziphus amole leaf extracts: Isolates from cattle and rabbits.

    Science.gov (United States)

    Gutiérrez-Morales, Andrea; Velázquez-Ordoñez, Valente; Khusro, Ameer; Salem, Abdelfattah Z M; Estrada-Zúñiga, María Elena; Salem, Mohamed Z M; Valladares-Carranza, Benjamin; Burrola-Aguilar, Cristina

    2017-12-01

    The desideratum aim of the present context was to assess the biopotency of methanolic extracts of Eichhornia crassipes (E. crassipes), Pistacia vera (P. vera), and Ziziphus amole (Z. amole) leaves against various staphylococcal strains, and to quantify the phenolics as well as saponin content in them. The antibacterial activity of various concentrations (62.5-1000 μg/mL) of plant extracts was tested against control clinical strains (Staphylococcus aureus ATCC 25923, S. aureus ATCC 29213, and S. aureus ATCC 43300), methicillin-resistant S. aureus (MRSA1 and MRSA2), oxacillin sensitive S. aureus (SOSA1 and SOSA2), and coagulase-negative Staphylococcus epidermidis (CoNS1, CoNS2, and CoNS3) using disc diffusion assay. Leaf extracts of the three plants exhibited pronounced growth inhibitory characteristics against staphylococci in a dose dependent manner. E. crassipes extract depicted the highest relative percentage inhibition values against control clinical strains (68.6 ± 0.5%), while P. vera (68.6 ± 0.3%) and Z. amole (74.79 ± 0.3%) extracts showed pronounced relative inhibition values against staphylococcal strains isolated from cattle. Total phenols and saponin content of leaf extracts were investigated by standard in vitro methods. The methanolic extracts of these plants were found to comprise substantial content of phenolics and saponin at varying levels. The highest value of phenolics was estimated in P. vera extract (60.0 ± 1.3 mg gallic acid/g extract), followed by Z. amole (33.6 ± 1.4 mg gallic acid/g extract), and E. crassipes (23.0 ± 1.3 mg gallic acid/g extract). Saponin content for P. vera, Z. amole, and E. crassipes extracts were estimated as 41.0 ± 1.3, 35.8 ± 1.3, and 25.0 ± 1.2 mg diosgenin/g extract, respectively. The outcome of this study suggested the exploitation of methanolic extract of P. vera, Z. amole, and E. crassipes leaves for their possible application in ethnomedicine, particularly as drugs preparation

  11. Efecto sobre la viabilidad celular de una nueva serie de espirosteroides sintéticos en células PC12 Effect of a new series of synthetic spiroteroids on the PC12 cell line viability

    Directory of Open Access Journals (Sweden)

    Laura García-Pupo

    2013-03-01

    Full Text Available Introducción: la diosgenina y sus derivados se han descrito como potentes inhibidores de la proliferación en varias líneas tumorales. Sin embargo otras moléculas relacionadas estructuralmente con dichos derivados, se han reportado como candidatos terapéuticos y otras de ellas se incluyen en alimentos de consumo humano. Objetivo: el presente trabajo evalúa el efecto sobre la viabilidad celular de una nueva serie de espiroesteroides sintéticos derivados de la diosgenina, en células tipo neurales PC12. Métodos: la viabilidad de los cultivos de PC12 se determinó mediante el ensayo de MTT y se calcularon descriptores moleculares teóricos como la lipofilicidad (logP virtual y la superficie de área polar (SAP, con el objetivo de establecer relaciones estructura-actividad. Resultados: nuestros resultados demuestran que solo el acido taurodesoxicólico disminuye de manera significativa la viabilidad celular. Más aun, dicha molécula presenta valores menores y mayores de logP virtual y SAP, respectivamente, respecto al resto de los esteroides de la serie. Conclusiones: los resultados anteriores avalan el estudio del acido taurodesoxicólico como potencial inhibidor de la proliferación celular y al resto de las moléculas de la serie como candidatos neuroprotectores a evaluar en esta misma línea celular y dosis de tratamiento.Introduction: diosgenin and its derivatives have been described as potent anti-proliferative compounds in several tumor cell lines. However, other structurally-related compounds are reported to exert neuroprotective activity and are also included in food for human consumption. Objective: to evaluate the effect of a novel series of diogesin-derived synthetic spirosteroids on cellular viability of neuron-like PC12 cell line. Methods: cellular viability was determined by the MTT assay along with some theorical molecular descriptors, such as lipophilicity and polar surface area, in order to establish the structure

  12. Synthesis of silver nanoparticles using Dioscorea bulbifera tuber extract and evaluation of its synergistic potential in combination with antimicrobial agents

    Directory of Open Access Journals (Sweden)

    Ghosh S

    2012-02-01

    Full Text Available Sougata Ghosh1, Sumersing Patil1, Mehul Ahire1, Rohini Kitture2, Sangeeta Kale3, Karishma Pardesi4, Swaranjit S Cameotra5, Jayesh Bellare6, Dilip D Dhavale7, Amit Jabgunde7, Balu A Chopade11Institute of Bioinformatics and Biotechnology, University of Pune, Pune, 2Department of Electronic Science, Fergusson College, Pune, 3Department of Applied Physics, Defense Institute of Advanced Technology, Girinagar, Pune, 4Department of Microbiology, University of Pune, Pune, 5Institute of Microbial Technology, Chandigarh, 6Department of Chemical Engineering, Indian Institute of Technology, Mumbai, 7Garware Research Centre, Department of Chemistry, University of Pune, Pune, IndiaBackground: Development of an environmentally benign process for the synthesis of silver nanomaterials is an important aspect of current nanotechnology research. Among the 600 species of the genus Dioscorea, Dioscorea bulbifera has profound therapeutic applications due to its unique phytochemistry. In this paper, we report on the rapid synthesis of silver nanoparticles by reduction of aqueous Ag+ ions using D. bulbifera tuber extract.Methods and results: Phytochemical analysis revealed that D. bulbifera tuber extract is rich in flavonoid, phenolics, reducing sugars, starch, diosgenin, ascorbic acid, and citric acid. The biosynthesis process was quite fast, and silver nanoparticles were formed within 5 hours. Ultraviolet-visible absorption spectroscopy, transmission electron microscopy, high-resolution transmission electron microscopy, energy dispersive spectroscopy, and x-ray diffraction confirmed reduction of the Ag+ ions. Varied morphology of the bioreduced silver nanoparticles included spheres, triangles, and hexagons. Optimization studies revealed that the maximum rate of synthesis could be achieved with 0.7 mM AgNO3 solution at 50°C in 5 hours. The resulting silver nanoparticles were found to possess potent antibacterial activity against both Gram-negative and Gram

  13. Optimization of Callus Induction and Regeneration in Two Fenugreek Landraces as a Medicinal Plant during in vitro Condition

    Directory of Open Access Journals (Sweden)

    Hasan Hasani Jifroudi

    2017-10-01

    Full Text Available Introduction: Fenugreek (Trigonella foenum- graecum is a medicinal plant extensively distributed in most regions of the world. Fenugreek is an annual plant from the family of papilionaceae, leguminosae. Fenugreek leaves and seeds have been used extensively to prepare extracts and powders for medicinal uses. Its root, leaf and seed contain a number of important medicinal compounds such as polysaccharide, galactomannan, different saponins such as diosgenin, yamogenin, mucilage, volatile oil and alkaloids such as choline and trigonelline. Plant tissue culture is fundamental to most aspects of biotechnology of plants. Establishment of an efficient callus induction and direct regeneration protocol is an essential prerequisite in harnessing the advantage of cell and tissue culture for genetic improvement. For the successful application of the tissue culture technique in plant breeding, callus induction and plant regeneration potential of each plant must be determined. The present study was performed in order to determine the optimum concentration of plant growth regulators (IBA + TDZ for producing of in vitro plantlet using cotyledon and hypocotyl as an explant for two different Iranian genotypes (Ardestani and Neyshabouri. Materials and Methods: In this investigation, Ardestani and Neyshabouri genotypes were used for callus induction and direct shoot regeneration. The medium used in this investigation was MS (Murashige and Skoog basal medium. Then seeds were germinated on MS medium. For callus induction and direct shoot regeneration, cotyledon and hypocotyl explants were excised from 8-day-old sterile seedlings and cultured on MS medium containing various concentrations of IBA and TDZ. In this experiment, two combinations (TDZ + IBA were used. In the first composition, IBA had four levels (0, 0.1, 0.3, 0.5 mg l-1 and TDZ had five levels (0, 0.2, 0.4, 0.6, 0.8 mg l-1 and in the second composition, IBA had four levels (0, 0.05, 0.1, 0.15 mg l-1 and TDZ