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Gianni Sagratini - One of the best experts on this subject based on the ideXlab platform.
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Comparative Analysis of the Volatile Profiles from Wild, Cultivated, and Commercial Roots of Gentiana lutea L. by Headspace Solid Phase Microextraction (HS–SPME) Coupled to Gas Chromatography Mass Spectrometry (GC–MS)
Food Analytical Methods, 2016Co-Authors: Ahmed M. Mustafa, Giovanni Caprioli, Sauro Vittori, Filippo Maggi, Gianni SagratiniAbstract:The root of Gentiana lutea L. is famous for its bitter properties and often used in alcoholic bitter beverages, food products, and traditional medicine to stimulate the appetite and improve digestion. This study presents the first report of an accurate, simple, fast, and reliable headspace solid phase microextraction (HS–SPME) method coupled to gas chromatography–mass spectrometry (GC–MS) for the analysis of the volatile profile of G. lutea roots. The developed method proved to be reliable to perform comparative analysis of the volatiles constituents from different populations of cultivated, wild, and commercial roots of G. lutea . HS–SPME/GC–MS analysis of 22 samples led to identification of 154 compounds belonging to terpenoids, alcohols, aldehydes, ketones, esters, alkanes, fatty acid derivatives, benzene derivatives, and others. The results proved that the composition of the volatile fraction of cultivated G. lutea is mostly similar to that of the wild samples but quite different with respect to commercial roots, and this was confirmed by principal component analysis (PCA).
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evaluation of neuritogenic activity of cultivated wild and commercial roots of Gentiana lutea l
Journal of Functional Foods, 2015Co-Authors: Ahmed M. Mustafa, Gianni Sagratini, Giovanni Caprioli, Sauro Vittori, Filippo Maggi, Miris Dikmen, Elif Duygu Kaya, Yusuf OzturkAbstract:Several natural products have been proven to prevent neurodegenerative disorders by potentiating the action of nerve growth factor (NGF). Among them, secoiridoids have recently attracted interest for their potential use as neuritogenic compounds. A source of these compounds is the root of Gentiana lutea L. used in food products to improve digestion. The aim of this work was to evaluate the neuritogenic activity of methanolic extracts of cultivated, wild and commercial roots of G. lutea using rat pheochromocytoma (PC12) cells. Neuritogenic activity was assessed by xCELLigence real time cell analysis system (RTCA DP), neurite outgrowth image analysis and immunofluorescence staining. Extracts at 12.5 and 25 µg/ml with or without NGF showed a marked stimulation of neuritogenesis, without cytotoxic effects, and their neuritogenic action was synergistic to NGF activity. These results represent the first evidence of the neuritogenic effects of G. lutea and of its potential use as a functional food ingredient.
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comparative hplc esi ms and hplc dad study of different populations of cultivated wild and commercial Gentiana lutea l
Food Chemistry, 2015Co-Authors: Ahmed M. Mustafa, Giovanni Caprioli, Massimo Ricciutelli, Sauro Vittori, Filippo Maggi, R Marin, Gianni SagratiniAbstract:Abstract The root of Gentiana lutea L., famous for its bitter properties, is often used in alcoholic bitter beverages, food products and traditional medicine to stimulate the appetite and improve digestion. This study presents a new, fast, and accurate HPLC method using HPLC/ESI-MS and HPLC/DAD for simultaneous analysis of iridoids (loganic acid), secoiridoids (gentiopicroside, sweroside, swertiamarin, amarogentin) and xanthones (isogentisin) in different populations of G. lutea L., cultivated in the Monti Sibillini National Park, obtained wild there, or purchased commercially. Comparison of HPLC/ESI-MS and HPLC/DAD indicated that HPLC/ESI-MS is more sensitive, reliable and selective. Analysis of twenty samples showed that gentiopicroside is the most dominant compound (1.85–3.97%), followed by loganic acid (0.11–1.30%), isogentisin (0.03–0.48%), sweroside (0.05–0.35%), swertiamarin (0.08–0.30%), and amarogentin (0.01–0.07%). The results confirmed the high quality of the G. lutea cultivated in the Monti Sibillini National Park.
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Comparative HPLC/ESI-MS and HPLC/DAD study of different populations of cultivated, wild and commercial Gentiana lutea L.
Food Chemistry, 2014Co-Authors: Ahmed M. Mustafa, R Marı́n, Giovanni Caprioli, Massimo Ricciutelli, Sauro Vittori, Filippo Maggi, Gianni SagratiniAbstract:Abstract The root of Gentiana lutea L., famous for its bitter properties, is often used in alcoholic bitter beverages, food products and traditional medicine to stimulate the appetite and improve digestion. This study presents a new, fast, and accurate HPLC method using HPLC/ESI-MS and HPLC/DAD for simultaneous analysis of iridoids (loganic acid), secoiridoids (gentiopicroside, sweroside, swertiamarin, amarogentin) and xanthones (isogentisin) in different populations of G. lutea L., cultivated in the Monti Sibillini National Park, obtained wild there, or purchased commercially. Comparison of HPLC/ESI-MS and HPLC/DAD indicated that HPLC/ESI-MS is more sensitive, reliable and selective. Analysis of twenty samples showed that gentiopicroside is the most dominant compound (1.85–3.97%), followed by loganic acid (0.11–1.30%), isogentisin (0.03–0.48%), sweroside (0.05–0.35%), swertiamarin (0.08–0.30%), and amarogentin (0.01–0.07%). The results confirmed the high quality of the G. lutea cultivated in the Monti Sibillini National Park.
R Kesavan - One of the best experts on this subject based on the ideXlab platform.
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Gentiana lutea exerts anti atherosclerotic effects by preventing endothelial inflammation and smooth muscle cell migration
Nutrition Metabolism and Cardiovascular Diseases, 2016Co-Authors: R Kesavan, Uma Rani Potunuru, Shivam Chandel, Swapna Upadhyay, R Bendre, Raghu Ganugula, Hemant Giri, Giriraj Sahu, Uday P Kumar, Bhanuprakash G ReddyAbstract:Studies suggest that Gentiana lutea (GL), and its component isovitexin, may exhibit anti-atherosclerotic properties. In this study we sought to investigate the protective mechanism of GL aqueous root extract and isovitexin on endothelial inflammation, smooth muscle cell migation, and on the onset and progression of atherosclerosis in streptozotocin (STZ)-induced diabetic rats.Our results show that both GL extract and isovitexin, block leukocyte adhesion and generation of reactive oxygen species in human umbilical vein endothelial cells (HUVECs) and rat aortic smooth muscle cells (RASMCs), following TNF-alpha and platelet derived growth factor-BB (PDGF-BB) challenges respectively. Both the extract and isovitexin blocked TNF-α induced expression of ICAM-1 and VCAM-1 in HUVECs. PDGF-BB induced migration of RASMCs and phospholipase C-γ activation, were also abrogated by GL extract and isovitexin. Fura-2 based ratiometric measurements demonstrated that, both the extact, and isovitexin, inhibit PDGF-BB mediated intracellular calcium rise in RASMCs. Supplementation of regular diet with 2% GL root powder for STZ rats, reduced total cholesterol in blood. Oil Red O staining demonstrated decreased lipid accumulation in aortic wall of diabetic animals upon treatment with GL. Medial thickness and deposition of collagen in the aortic segment of diabetic rats were also reduced upon supplementation. Immunohistochemistry demonstrated reduced expression of vascular cell adhesion molecule-1 (VCAM-1), inducible nitric oxide synthase (iNOS), and vascular endothelial cadherin (VE-cadherin) in aortic segments of diabetic rats following GL treatment.Thus, our results support that GL root extract/powder and isovitexin exhibit anti-atherosclerotic activities.
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inhibition of vascular smooth muscle cell proliferation by Gentiana lutea root extracts
PLOS ONE, 2013Co-Authors: R Kesavan, Gordana Joksic, Uma Rani Potunuru, Branislav Nastasijevic, T Avaneesh, Madhulika DixitAbstract:Gentiana lutea belonging to the Gentianaceae family of flowering plants are routinely used in traditional Serbian medicine for their beneficial gastro-intestinal and anti-inflammatory properties. The aim of the study was to determine whether aqueous root extracts of Gentiana lutea consisting of gentiopicroside, gentisin, bellidifolin-8-O-glucoside, demethylbellidifolin-8-O-glucoside, isovitexin, swertiamarin and amarogentin prevents proliferation of aortic smooth muscle cells in response to PDGF-BB. Cell proliferation and cell cycle analysis were performed based on alamar blue assay and propidium iodide labeling respectively. In primary cultures of rat aortic smooth muscle cells (RASMCs), PDGF-BB (20 ng/ml) induced a two-fold increase in cell proliferation which was significantly blocked by the root extract (1 mg/ml). The root extract also prevented the S-phase entry of synchronized cells in response to PDGF. Furthermore, PDGF-BB induced ERK1/2 activation and consequent increase in cellular nitric oxide (NO) levels were also blocked by the extract. These effects of extract were due to blockade of PDGF-BB induced expression of iNOS, cyclin D1 and proliferating cell nuclear antigen (PCNA). Docking analysis of the extract components on MEK1, the upstream ERK1/2 activating kinase using AutoDock4, indicated a likely binding of isovitexin to the inhibitor binding site of MEK1. Experiments performed with purified isovitexin demonstrated that it successfully blocks PDGF-induced ERK1/2 activation and proliferation of RASMCs in cell culture. Thus, Gentiana lutea can provide novel candidates for prevention and treatment of atherosclerosis.
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Inhibition of Vascular Smooth Muscle Cell Proliferation by Gentiana lutea Root Extracts
2012Co-Authors: R Kesavan, Uma Rani Potunuru, Avaneesh T, Madhulika DixitAbstract:Gentiana lutea belonging to the Gentianaceae family of flowering plants are routinely used in traditional Serbian medicine for their beneficial gastro-intestinal and anti-inflammatory properties. The aim of the study was to determine whether aqueous root extracts of Gentiana lutea consisting of gentiopicroside, gentisin, bellidifolin-8-O-glucoside, demethylbelli-difolin-8-O-glucoside, isovitexin, swertiamarin and amarogentin prevents proliferation of aortic smooth muscle cells in response to PDGF-BB. Cell proliferation and cell cycle analysis were performed based on alamar blue assay and propidium iodide labeling respectively. In primary cultures of rat aortic smooth muscle cells (RASMCs), PDGF-BB (20 ng/ml) induced a two-fold increase in cell proliferation which was significantly blocked by the root extract (1 mg/ml). The root extract also prevented the S-phase entry of synchronized cells in response to PDGF. Furthermore, PDGF-BB induced ERK1/2 activation and consequent increase in cellular nitric oxide (NO) levels were also blocked by the extract. These effects of extract were due to blockade of PDGF-BB induced expression of iNOS, cyclin D1 and proliferating cell nuclear antigen (PCNA). Docking analysis of the extract components on MEK1, the upstream ERK1/2 activating kinase using AutoDock4, indicated a likely binding of isovitexin to the inhibitor binding site of MEK1. Experiments performed with purified isovitexin demonstrated that it successfully blocks PDGF-induced ERK1/2 activation and proliferation of RASMCs in cell culture. Thus, Gentiana lute
Ahmed M. Mustafa - One of the best experts on this subject based on the ideXlab platform.
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Comparative Analysis of the Volatile Profiles from Wild, Cultivated, and Commercial Roots of Gentiana lutea L. by Headspace Solid Phase Microextraction (HS–SPME) Coupled to Gas Chromatography Mass Spectrometry (GC–MS)
Food Analytical Methods, 2016Co-Authors: Ahmed M. Mustafa, Giovanni Caprioli, Sauro Vittori, Filippo Maggi, Gianni SagratiniAbstract:The root of Gentiana lutea L. is famous for its bitter properties and often used in alcoholic bitter beverages, food products, and traditional medicine to stimulate the appetite and improve digestion. This study presents the first report of an accurate, simple, fast, and reliable headspace solid phase microextraction (HS–SPME) method coupled to gas chromatography–mass spectrometry (GC–MS) for the analysis of the volatile profile of G. lutea roots. The developed method proved to be reliable to perform comparative analysis of the volatiles constituents from different populations of cultivated, wild, and commercial roots of G. lutea . HS–SPME/GC–MS analysis of 22 samples led to identification of 154 compounds belonging to terpenoids, alcohols, aldehydes, ketones, esters, alkanes, fatty acid derivatives, benzene derivatives, and others. The results proved that the composition of the volatile fraction of cultivated G. lutea is mostly similar to that of the wild samples but quite different with respect to commercial roots, and this was confirmed by principal component analysis (PCA).
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evaluation of neuritogenic activity of cultivated wild and commercial roots of Gentiana lutea l
Journal of Functional Foods, 2015Co-Authors: Ahmed M. Mustafa, Gianni Sagratini, Giovanni Caprioli, Sauro Vittori, Filippo Maggi, Miris Dikmen, Elif Duygu Kaya, Yusuf OzturkAbstract:Several natural products have been proven to prevent neurodegenerative disorders by potentiating the action of nerve growth factor (NGF). Among them, secoiridoids have recently attracted interest for their potential use as neuritogenic compounds. A source of these compounds is the root of Gentiana lutea L. used in food products to improve digestion. The aim of this work was to evaluate the neuritogenic activity of methanolic extracts of cultivated, wild and commercial roots of G. lutea using rat pheochromocytoma (PC12) cells. Neuritogenic activity was assessed by xCELLigence real time cell analysis system (RTCA DP), neurite outgrowth image analysis and immunofluorescence staining. Extracts at 12.5 and 25 µg/ml with or without NGF showed a marked stimulation of neuritogenesis, without cytotoxic effects, and their neuritogenic action was synergistic to NGF activity. These results represent the first evidence of the neuritogenic effects of G. lutea and of its potential use as a functional food ingredient.
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comparative hplc esi ms and hplc dad study of different populations of cultivated wild and commercial Gentiana lutea l
Food Chemistry, 2015Co-Authors: Ahmed M. Mustafa, Giovanni Caprioli, Massimo Ricciutelli, Sauro Vittori, Filippo Maggi, R Marin, Gianni SagratiniAbstract:Abstract The root of Gentiana lutea L., famous for its bitter properties, is often used in alcoholic bitter beverages, food products and traditional medicine to stimulate the appetite and improve digestion. This study presents a new, fast, and accurate HPLC method using HPLC/ESI-MS and HPLC/DAD for simultaneous analysis of iridoids (loganic acid), secoiridoids (gentiopicroside, sweroside, swertiamarin, amarogentin) and xanthones (isogentisin) in different populations of G. lutea L., cultivated in the Monti Sibillini National Park, obtained wild there, or purchased commercially. Comparison of HPLC/ESI-MS and HPLC/DAD indicated that HPLC/ESI-MS is more sensitive, reliable and selective. Analysis of twenty samples showed that gentiopicroside is the most dominant compound (1.85–3.97%), followed by loganic acid (0.11–1.30%), isogentisin (0.03–0.48%), sweroside (0.05–0.35%), swertiamarin (0.08–0.30%), and amarogentin (0.01–0.07%). The results confirmed the high quality of the G. lutea cultivated in the Monti Sibillini National Park.
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Comparative HPLC/ESI-MS and HPLC/DAD study of different populations of cultivated, wild and commercial Gentiana lutea L.
Food Chemistry, 2014Co-Authors: Ahmed M. Mustafa, R Marı́n, Giovanni Caprioli, Massimo Ricciutelli, Sauro Vittori, Filippo Maggi, Gianni SagratiniAbstract:Abstract The root of Gentiana lutea L., famous for its bitter properties, is often used in alcoholic bitter beverages, food products and traditional medicine to stimulate the appetite and improve digestion. This study presents a new, fast, and accurate HPLC method using HPLC/ESI-MS and HPLC/DAD for simultaneous analysis of iridoids (loganic acid), secoiridoids (gentiopicroside, sweroside, swertiamarin, amarogentin) and xanthones (isogentisin) in different populations of G. lutea L., cultivated in the Monti Sibillini National Park, obtained wild there, or purchased commercially. Comparison of HPLC/ESI-MS and HPLC/DAD indicated that HPLC/ESI-MS is more sensitive, reliable and selective. Analysis of twenty samples showed that gentiopicroside is the most dominant compound (1.85–3.97%), followed by loganic acid (0.11–1.30%), isogentisin (0.03–0.48%), sweroside (0.05–0.35%), swertiamarin (0.08–0.30%), and amarogentin (0.01–0.07%). The results confirmed the high quality of the G. lutea cultivated in the Monti Sibillini National Park.
Gordana Joksic - One of the best experts on this subject based on the ideXlab platform.
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toxicity assessment of Gentiana lutea l root extract and its monoterpene compounds
Indian Journal of Experimental Biology (IJEB), 2020Co-Authors: Ana Valenta Sobot, Jasmina Savic, Jelena Filipovic Trickovic, Dunja Drakulic, Gordana JoksicAbstract:Root of Gentiana lutea commercially available as gentian root, a natural antidote for different types of poisons, possess antioxidative, immunomodulatory, cytoprotective and anti-inflammatory, and adverse, genotoxic and mutagenic effects. It has monoterpenes loganic acid, swertiamarin, gentiopicroside and sweroside as most abundant constituents. In this study, we assessed the toxicity of monoterpenes’ reactive molecular fragments using in silico prediction by VEGA-QSAR platform. Further, we compared the data obtained with in vitro geno- and cyto- toxicity testing of the above monoterpenes and the G. lutea root extract (GE), on human primary unstimulated and mitogen-stimulated peripheral blood mononuclear cells (PBMCs). Viability was assessed by TB and XTT tests after 48 h treatmen. DNA damage was evaluated by alkaline comet assay on unstimulated cells, whereas cytokinesis-block micronucleus assay was employed on mitogen-stimulated PBMCs. Stability of compounds throughout treatment was monitored by UPLC. The observed in vitro results had highest compliance with in silico IRFMN/ISSCAN-CGX prediction model. Compounds showed high stability during experiment while treatment with single compounds reduced number of viable cells and increased DNA damage. GE treatment had toxic impact on unstimulated PBMCs but no significant genotoxic influence on mitogen-stimulated PBMCs. In summary, the mild GE effect suggests that the complexity of crude GE extract chemical composition may attenuate the toxicity of the tested monoterpenes loganic acid, swertiamarin, gentiopicroside and sweroside.
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Effects of Gentiana lutea root on vascular diseases.
Current Vascular Pharmacology, 2020Co-Authors: Gordana Joksic, Djordje Radak, Emina Sudar-milovanovic, Milan Obradovic, Jelena Radovanović, Esma R. IsenovicAbstract:Background Gentiana lutea (GL), commonly known as yellow gentian, bitter root, and bitterwort, belongs to family Gentianaceae. GL belongs to genus Gentiana, which is a rich natural source of iridoids, secoiridoids, xantones, flavonoids, triterpenoids, and carbohydrates. Medicinal plants from Gentiana species have anti-oxidant, anti-inflammatory, anti-mitogenic, anti-proliferative, and lipid-lowering effects, as well as a cardioprotective, hypotensive, vasodilator and anti-platelet activities. Objective We reviewed the recent literature related to the effects of Gentiana species, and their active components on vascular diseases. Methods Data used for this review were obtained by searching the electronic database [PUBMED/MEDLINE 1973 - February 2020]. The primary data search terms of interest were: Gentiana lutea, Gentienacea family, phytochemistry, vascular diseases, treatment of vascular diseases, anti-oxidant, anti-inflammatory, anti-atherogenic. Conclusion Gentiana species and their constituents affect many different factors related to vascular disease development and progression. Therefore, Gentiana-based therapeutics represent potentially useful drugs for the management of vascular diseases.
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Potential of Gentiana lutea for the Treatment of Obesity-associated Diseases.
Current Pharmaceutical Design, 2019Co-Authors: Gordana Joksic, Jelena G. Filipović Tričković, Ivana JoksicAbstract:BACKGROUND: Obesity, diabetes, and associated diseases are increasing all over the world, and pose a great burden on public health. According to the latest reports, 440 million people are suffering from diabetes. Diabetes is caused by impaired ability to produce or respond to the hormone insulin consequently resulting in hyperglycemia. METHODS: Data used for this review was obtained by using PUBMED/MEDLINE (1987-2018). The main data search terms were: Gentiana lutea, Gentiana lutea extract, Gentiana lutea constituents, obesity, diabetes mellitus, diabetic complications. RESULTS: In the present review, we describe the potential of root powder of yellow gentian (Gentiana lutea) for the prevention of obesity and diabetes including complications related to this disease. CONCLUSION: Reasonably effective, low-cost alternatives could fulfill an important role for a large part of the human population and could be of great value for the food market. Even a modest reduction of morbidity and mortality with respect to this disease translates into millions of lives saved.
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inhibition of vascular smooth muscle cell proliferation by Gentiana lutea root extracts
PLOS ONE, 2013Co-Authors: R Kesavan, Gordana Joksic, Uma Rani Potunuru, Branislav Nastasijevic, T Avaneesh, Madhulika DixitAbstract:Gentiana lutea belonging to the Gentianaceae family of flowering plants are routinely used in traditional Serbian medicine for their beneficial gastro-intestinal and anti-inflammatory properties. The aim of the study was to determine whether aqueous root extracts of Gentiana lutea consisting of gentiopicroside, gentisin, bellidifolin-8-O-glucoside, demethylbellidifolin-8-O-glucoside, isovitexin, swertiamarin and amarogentin prevents proliferation of aortic smooth muscle cells in response to PDGF-BB. Cell proliferation and cell cycle analysis were performed based on alamar blue assay and propidium iodide labeling respectively. In primary cultures of rat aortic smooth muscle cells (RASMCs), PDGF-BB (20 ng/ml) induced a two-fold increase in cell proliferation which was significantly blocked by the root extract (1 mg/ml). The root extract also prevented the S-phase entry of synchronized cells in response to PDGF. Furthermore, PDGF-BB induced ERK1/2 activation and consequent increase in cellular nitric oxide (NO) levels were also blocked by the extract. These effects of extract were due to blockade of PDGF-BB induced expression of iNOS, cyclin D1 and proliferating cell nuclear antigen (PCNA). Docking analysis of the extract components on MEK1, the upstream ERK1/2 activating kinase using AutoDock4, indicated a likely binding of isovitexin to the inhibitor binding site of MEK1. Experiments performed with purified isovitexin demonstrated that it successfully blocks PDGF-induced ERK1/2 activation and proliferation of RASMCs in cell culture. Thus, Gentiana lutea can provide novel candidates for prevention and treatment of atherosclerosis.
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inhibition of aldose reductase by Gentiana lutea extracts
Experimental Diabetes Research, 2012Co-Authors: Chandrasekhar Akileshwari, Gordana Joksic, Branislav Nastasijevic, Puppala Muthenna, Mark J Petrash, G B ReddyAbstract:Accumulation of intracellular sorbitol due to increased aldose reductase (ALR2) activity has been implicated in the development of various secondary complications of diabetes. Thus, ALR2 inhibition could be an effective strategy in the prevention or delay of certain diabetic complications. Gentiana lutea grows naturally in the central and southern areas of Europe. Its roots are commonly consumed as a beverage in some European countries and are also known to have medicinal properties. The water, ethanol, methanol, and ether extracts of the roots of G. lutea were subjected to in vitro bioassay to evaluate their inhibitory activity on the ALR2. While the ether and methanol extracts showed greater inhibitory activities against both rat lens and human ALR2, the water and ethanol extracts showed moderate inhibitory activities. Moreover, the ether and methanol extracts of G. lutea roots significantly and dose-dependently inhibited sorbitol accumulation in human erythrocytes under high glucose conditions. Molecular docking studies with the constituents commonly present in the roots of G. lutea indicate that a secoiridoid glycoside, amarogentin, may be a potential inhibitor of ALR2. This is the first paper that shows G. lutea extracts exhibit inhibitory activity towards ALR2 and these results suggest that Gentiana or its constituents might be useful to prevent or treat diabetic complications.
Hermann Stuppner - One of the best experts on this subject based on the ideXlab platform.
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nonprenylated xanthones from Gentiana lutea frasera caroliniensis and centaurium erythraea as novel inhibitors of vascular smooth muscle cell proliferation
Molecules, 2015Co-Authors: Birgit Waltenberger, Rongxia Liu, Atanas G Atanasov, Stefan Schwaiger, Elke H Heiss, Verena M Dirsch, Hermann StuppnerAbstract:Aberrant proliferation of vascular smooth muscle cells (VSMC) plays a major role in restenosis, the pathological renarrowing of the blood vessel lumen after surgical treatment of stenosis. Since available anti-proliferative pharmaceuticals produce unfavorable side effects, there is high demand for the identification of novel VSMC proliferation inhibitors. A natural product screening approach using a resazurin conversion assay enabled the identification of gentisin (1) from Gentiana lutea as a novel inhibitor of VSMC proliferation with an IC50 value of 7.84 µM. Aiming to identify further anti-proliferative compounds, 13 additional nonprenylated xanthones, isolated from different plant species, were also tested. While some compounds showed no or moderate activity at 30 µM, 1-hydroxy-2,3,4,5-tetramethoxyxanthone (4), swerchirin (6), and methylswertianin (7) showed IC50 values between 10.2 and 12.5 µM. The anti-proliferative effect of 1, 4, 6, and 7 was confirmed by the quantification of DNA synthesis (BrdU incorporation) in VSMC. Cell death quantification (determined by LDH release in the culture medium) revealed that the compounds are not cytotoxic in the investigated concentration range. In conclusion, nonprenylated xanthones are identified as novel, non-toxic VSMC proliferation inhibitors, which might contribute to the development of new therapeutic applications to combat restenosis.
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analysis of iridoids secoiridoids and xanthones in centaurium erythraea frasera caroliniensis and Gentiana lutea using lc ms and rp hplc
Journal of Pharmaceutical and Biomedical Analysis, 2011Co-Authors: Anita Aberham, Edward M Croom, Valerio Pieri, Ernst P Ellmerer, Hermann StuppnerAbstract:Abstract This study presents a new and validated HPLC method for the simultaneous determination of bioactive compounds in Centaurium erythraea , Frasera caroliniensis and Gentiana lutea . The iridoid loganic acid, four secoiridoids and 29 xanthones were separated on a RP-18 column, using aqueous o-phosphoric acid (0.085%, v/v) and acetonitrile as mobile phase. Phytochemical investigation of C. erythraea herb and F. caroliniensis roots resulted into isolation of 25 xanthones and three secoiridoids the structure of which was elucidated by spectroscopic means (NMR, MS and UV). 1,3,8-Trihydroxy-5,6-dimethoxyxanthone, isolated from C. erythraea , turned out to be a novel xanthone. The stability of the analytes was tested by subjecting samples to light, moisture and different temperatures. After six months of storage, decomposition of gentiopicroside and sweroside was observed. The swertiamarin content was nearly unchanged when stored at room temperature or in the refrigerator, but high temperature conditions reduced the content to 85%. In contrast, xanthones were stable under long-term, refrigerated and accelerated conditions. The established chromatographic method has been successfully applied for the quantification of the bioactive compounds in the three plants. The presence and distribution of polyoxygenated xanthones within the three members of the Gentianaceae family and their significance as analytical markers are discussed.
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determination of gentisin isogentisin and amarogentin in Gentiana lutea l by capillary electrophoresis
Journal of Separation Science, 2008Co-Authors: Hermann Stuppner, Ivana Citova, Markus Ganzera, Petr SolichAbstract:A novel, fast, and simple capillary electrophoresis method has been developed for the analysis of gentisin, isogentisin, and amarogentin in roots of Gentiana lutea (yellow gentian), an herb traditionally used as gastric stimulant. Gentisin and isogentisin are xanthones showing potent inhibition of monoamine oxidase type A and B, amarogentin represents one of the bitter principles of Gentiana, responsible for its gastric-roborant effects. Optimal CE-separation conditions comprise a 100 mM sodium tetraborate buffer of pH 9.3, containing 10 mM β-cyclodextrin as additive; optimum temperature and applied voltage were found to be 30°C and 25 kV, respectively. Direct diode array detection at 260 nm (gentisin, isogentisin) and 242 nm (amarogentin) was performed, and the required analysis time was only 11 min. The developed method was validated for linearity, sensitivity, precision, and accuracy, and utilized to assay several commercially available G. lutea samples. Quantitative data obtained with the developed CE method are compared with HPLC results, and the advantages of each approach are discussed.