The Experts below are selected from a list of 1599 Experts worldwide ranked by ideXlab platform
Qi Qi - One of the best experts on this subject based on the ideXlab platform.
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Gambogic Acid promotes apoptosis and resistance to metastatic potential in mda mb 231 human breast carcinoma cells
Biochemistry and Cell Biology, 2012Co-Authors: Chenglin Li, Na Lu, Qi Qi, Fanni Li, Xiaotang WangAbstract:Gambogic Acid (GA) is considered a potent anti-tumor agent for its multiple effects on cancer cells in vitro and in vivo. Low concentrations of GA (0.3–1.2 µmol/L) can suppress invasion of human br...
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Gambogic Acid inhibits tumor cell adhesion by suppressing integrin β1 and membrane lipid rafts associated integrin signaling pathway
Biochemical Pharmacology, 2011Co-Authors: Chenglin Li, Na Lu, Qi Qi, Fanni Li, Yun Ling, Yan Chen, Zhiyu Li, Haiwei ZhangAbstract:Abstract Cell adhesion plays an important role in the steps of cancer metastasis. Regulation of cell–cell (intercellular) and cell–matrix adhesion is a promising strategy for cancer progression. Gambogic Acid is a xanthone derived from the resin of the Chinese plant Garciania hanburyi, with potent anti-metastasis activity on highly metastatic cells. The aim of this study was to investigate the function and mechanism of Gambogic Acid on tumor adhesion. We found that Gambogic Acid strongly inhibited the adhesion of human cancer cells to fibronectin. This inhibition was associated with the deformation of focal adhesion complex, which was mediated by suppressing the expression of integrin β1 and integrin signaling pathway. In vitro, cell lipid rafts clustering was inhibited following treatment of Gambogic Acid, which induced the suppression of integrin β1 and focal adhesion complex proteins colocalization within rafts. Moreover, Gambogic Acid significantly decreased cellular cholesterol content, whereas cholesterol replenishment lessened the inhibitory effect of Gambogic Acid on cell adhesion. Real-time PCR analysis showed that Gambogic Acid reduced mRNA levels of hydroxymethylglutaryl-CoA reductase and sterol regulatory element binding protein-2, while increased acetyl-CoA acetyltransferase-1/2. Taken together, these results demonstrate that Gambogic Acid inhibits cell adhesion via suppressing integrin β1 abundance and cholesterol content as well as the membrane lipid raft-associated integrin function, which provide new evidence for the anti-cancer activity of Gambogic Acid.
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Gambogic Acid reduced bcl 2 expression via p53 in human breast mcf 7 cancer cells
Journal of Cancer Research and Clinical Oncology, 2009Co-Authors: Hongyan Gu, Jie Zhao, Jia Wang, Rong Mu, Jingjing Rong, Qi QiAbstract:Purpose In this study, we investigated the correlation between p53 and bcl-2 in Gambogic Acid (GA)-induced apoptosis.
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inhibition of α4 integrin mediated adhesion was involved in the reduction of b16 f10 melanoma cells lung colonization in c57bl 6 mice treated with Gambogic Acid
European Journal of Pharmacology, 2008Co-Authors: Jie Zhao, Na Lu, Qi Qi, Hongyan Gu, Lei Qiang, Yong Yang, Wei Wang, Lingbo ZhangAbstract:Abstract Gambogic Acid, the major active ingredient of gamboge, has been shown to exhibit anti-cancer activity both in vivo and in vitro. However, its potential activity in tumor metastasis remains unclear. In the present study, we found that Gambogic Acid strongly inhibited the adhesion of highly metastatic mouse melanoma B16-F10 cells in vitro . Gambogic Acid also exhibited significant anti-metastasis activity on the development of in vivo artificial metastases (i.e. following tail vein i.v. injection of the B16-F10 melanoma tumor cells in C57BL/6 mice). Flow cytometric analysis and Western blot showed that Gambogic Acid inhibited the cell surface expression of α 4 integrin , while exhibited negligible effects on the expression of α 5 and β 1 integrin. Thus we concluded for the first time that Gambogic Acid could inhibit the adhesion and migration of B16-F10 cells in vitro and in vivo , in which down-regulation of α 4 integrin expression was involved.
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Inhibition of alpha(4) integrin mediated adhesion was involved in the reduction of B16-F10 melanoma cells lung colonization in C57BL/6 mice treated with Gambogic Acid.
European journal of pharmacology, 2008Co-Authors: Jie Zhao, Na Lu, Qi Qi, Hongyan Gu, Lei Qiang, Yong Yang, Wei Wang, Lingbo ZhangAbstract:Gambogic Acid, the major active ingredient of gamboge, has been shown to exhibit anti-cancer activity both in vivo and in vitro. However, its potential activity in tumor metastasis remains unclear. In the present study, we found that Gambogic Acid strongly inhibited the adhesion of highly metastatic mouse melanoma B16-F10 cells in vitro. Gambogic Acid also exhibited significant anti-metastasis activity on the development of in vivo artificial metastases (i.e. following tail vein i.v. injection of the B16-F10 melanoma tumor cells in C57BL/6 mice). Flow cytometric analysis and Western blot showed that Gambogic Acid inhibited the cell surface expression of alpha(4) integrin, while exhibited negligible effects on the expression of alpha(5) and beta(1) integrin. Thus we concluded for the first time that Gambogic Acid could inhibit the adhesion and migration of B16-F10 cells in vitro and in vivo, in which down-regulation of alpha(4) integrin expression was involved.
Hongyan Gu - One of the best experts on this subject based on the ideXlab platform.
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Gambogic Acid reduced bcl 2 expression via p53 in human breast mcf 7 cancer cells
Journal of Cancer Research and Clinical Oncology, 2009Co-Authors: Hongyan Gu, Jie Zhao, Jia Wang, Rong Mu, Jingjing Rong, Qi QiAbstract:Purpose In this study, we investigated the correlation between p53 and bcl-2 in Gambogic Acid (GA)-induced apoptosis.
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inhibition of α4 integrin mediated adhesion was involved in the reduction of b16 f10 melanoma cells lung colonization in c57bl 6 mice treated with Gambogic Acid
European Journal of Pharmacology, 2008Co-Authors: Jie Zhao, Na Lu, Qi Qi, Hongyan Gu, Lei Qiang, Yong Yang, Wei Wang, Lingbo ZhangAbstract:Abstract Gambogic Acid, the major active ingredient of gamboge, has been shown to exhibit anti-cancer activity both in vivo and in vitro. However, its potential activity in tumor metastasis remains unclear. In the present study, we found that Gambogic Acid strongly inhibited the adhesion of highly metastatic mouse melanoma B16-F10 cells in vitro . Gambogic Acid also exhibited significant anti-metastasis activity on the development of in vivo artificial metastases (i.e. following tail vein i.v. injection of the B16-F10 melanoma tumor cells in C57BL/6 mice). Flow cytometric analysis and Western blot showed that Gambogic Acid inhibited the cell surface expression of α 4 integrin , while exhibited negligible effects on the expression of α 5 and β 1 integrin. Thus we concluded for the first time that Gambogic Acid could inhibit the adhesion and migration of B16-F10 cells in vitro and in vivo , in which down-regulation of α 4 integrin expression was involved.
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Inhibition of alpha(4) integrin mediated adhesion was involved in the reduction of B16-F10 melanoma cells lung colonization in C57BL/6 mice treated with Gambogic Acid.
European journal of pharmacology, 2008Co-Authors: Jie Zhao, Na Lu, Qi Qi, Hongyan Gu, Lei Qiang, Yong Yang, Wei Wang, Lingbo ZhangAbstract:Gambogic Acid, the major active ingredient of gamboge, has been shown to exhibit anti-cancer activity both in vivo and in vitro. However, its potential activity in tumor metastasis remains unclear. In the present study, we found that Gambogic Acid strongly inhibited the adhesion of highly metastatic mouse melanoma B16-F10 cells in vitro. Gambogic Acid also exhibited significant anti-metastasis activity on the development of in vivo artificial metastases (i.e. following tail vein i.v. injection of the B16-F10 melanoma tumor cells in C57BL/6 mice). Flow cytometric analysis and Western blot showed that Gambogic Acid inhibited the cell surface expression of alpha(4) integrin, while exhibited negligible effects on the expression of alpha(5) and beta(1) integrin. Thus we concluded for the first time that Gambogic Acid could inhibit the adhesion and migration of B16-F10 cells in vitro and in vivo, in which down-regulation of alpha(4) integrin expression was involved.
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inhibition of glioblastoma growth and angiogenesis by Gambogic Acid an in vitro and in vivo study
Biochemical Pharmacology, 2008Co-Authors: Lei Qiang, Na Lu, Qi Qi, Li Zhao, Hongyan Gu, Yong Yang, Lan Yang, Xiaotang WangAbstract:Abstract Gambogic Acid (GA) is the major active ingredient of gamboge, a brownish to orange resin exuded from Garcinia hanburryi tree in Southeast Asia. The present study aims to demonstrate that Gambogic Acid (GA) has potent anticancer activity for glioblastoma by in vitro and in vivo study. Rat brain microvascular endothelial cells (rBMEC) were used as an in vitro model of the blood–brain barrier (BBB). To reveal an involvement of the intrinsic mitochondrial pathway of apoptosis, the mitochondrial membrane potential and the western blot evaluation of Bax, Bcl-2, Caspase-3, caspase-9 and cytochrome c released from mitochondria were performed. Angiogenesis was detected by CD31 immunochemical study. The results showed that the uptake of GA by rBMEC was time-dependent, which indicated that it could pass BBB and represent a possible new target in glioma therapy. GA could cause apoptosis of rat C6 glioma cells in vitro in a concentration-dependent manner by triggering the intrinsic mitochondrial pathway of apoptosis. In vivo study also revealed that i.v. injection of GA once a day for two weeks could significantly reduce tumor volumes by antiangiogenesis and apoptotic induction of glioma cells. Collectively, the current data indicated that GA may be of potential use in treatment of glioblastoma by apoptotic induction and antiangiogenic effects.
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toxicological studies of Gambogic Acid and its potential targets in experimental animals
Basic & Clinical Pharmacology & Toxicology, 2006Co-Authors: Qi Qi, Li Zhao, Hongyan Gu, Zhaoqiu WuAbstract:Abstract: Acute and chronic toxicity of Gambogic Acid, a promising novel anticancer agent, was determined using albino mice and Beagle dogs as model animals. Histopathological examination and viscera parameter investigation were also carried out after autopsy. The LD50 of Gambogic Acid was found to be 45∼96 mg/kg and the 95% confidence limit was determined to be 43.18∼48.45 mg/kg. The results from the chronic toxicity studies demonstrated that the toxicity targets in the experimental animals were liver and kidney. The innocuous dose was established to be 4 mg/kg after administration to dogs for a total of 13 weeks at a frequency of one injection every other day. This dose (4 mg/kg) was approximately 9.6 (body weight) or 5.1 (body surface area) times the dosage (25 mg/60 kg, every other day) recommended for human trials. Our results provide the theoretical foundation for clinical applications of this promising natural anticancer agent and will likely bring about considerable economic and social benefits.
Na Lu - One of the best experts on this subject based on the ideXlab platform.
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Gambogic Acid suppresses cancer invasion and migration by inhibiting TGFβ1-induced epithelial-to-mesenchymal transition
Oncotarget, 2017Co-Authors: Kai Zhao, Shuai Zhang, Xiuming Song, Yuxin Zhou, Na LuAbstract:// Kai Zhao 1, * , Shuai Zhang 2, * , Xiuming Song 3 , Yuyuan Yao 1 , Yuxin Zhou 1 , Qidong You 1 , Qinglong Guo 1 , Na Lu 1 1 State Key Laboratory of Natural Medicines, College of Basic Medicine and Clinical Pharmacy, China Pharmaceutical University, Nanjing, People’s Republic of China 2 Department of Thoracic Surgery, Nanjing Medical University Affiliated Cancer Hospital, Jiangsu Key Laboratory of Molecular and Translational Cancer Research, Cancer Institute of Jiangsu Province, Nanjing, People’s Republic of China 3 Chia Tai Tianqing Pharmaceutical Group Co., Ltd, People’s Republic of China * These authors have contributed equally to this work Correspondence to: Na Lu, email: luna555@163.com Qinglong Guo, email: anticancer_drug@163.com Keywords: Gambogic Acid, invasion, A549 cells, EMT, NF-κB Received: April 13, 2016 Accepted: January 23, 2017 Published: February 17, 2017 ABSTRACT The epithelial-to-mesenchymal transition (EMT) contributes to the disruption of cell–cell junctions and imbues cancer cells with invasive and migratory properties. In this study, we investigated the effect of Gambogic Acid, a xanthone extracted from the resin of Garciania hanburyi, on transforming growth factor β1 (TGFβ1)-induced EMT. Gambogic Acid inhibited the invasion and migration of TGFβ1-induced A549 cells in vitro . Gambogic Acid also increased the mRNA and protein expression of E-cadherin, but repressed the mRNA and protein expression of N-cadherin, vimentin, and transcription factor TWIST1. Further examination of the mechanism revealed that the nuclear factor κB (NF-κB) pathway is involved in this regulation of EMT-related biomarkers. Gambogic Acid inhibited NF-κB p65 nuclear translocation and the phosphorylation of the inhibitor of NF-κB (IκBα) and IκBα kinase (IKKα). Gambogic Acid also suppressed the EMT induced by TGFβ1 and tumor necrosis factor α by inhibiting the NF-κB pathway. Our data also indicate that Gambogic Acid inhibited the primary lesion and lung metastasis of orthotopic model of A549 cells in vivo . We propose that Gambogic Acid might be developed as a candidate drug with therapeutic potential for the treatment of cancer invasion and migration.
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Gambogic Acid promotes apoptosis and resistance to metastatic potential in mda mb 231 human breast carcinoma cells
Biochemistry and Cell Biology, 2012Co-Authors: Chenglin Li, Na Lu, Qi Qi, Fanni Li, Xiaotang WangAbstract:Gambogic Acid (GA) is considered a potent anti-tumor agent for its multiple effects on cancer cells in vitro and in vivo. Low concentrations of GA (0.3–1.2 µmol/L) can suppress invasion of human br...
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Gambogic Acid inhibits tumor cell adhesion by suppressing integrin β1 and membrane lipid rafts associated integrin signaling pathway
Biochemical Pharmacology, 2011Co-Authors: Chenglin Li, Na Lu, Qi Qi, Fanni Li, Yun Ling, Yan Chen, Zhiyu Li, Haiwei ZhangAbstract:Abstract Cell adhesion plays an important role in the steps of cancer metastasis. Regulation of cell–cell (intercellular) and cell–matrix adhesion is a promising strategy for cancer progression. Gambogic Acid is a xanthone derived from the resin of the Chinese plant Garciania hanburyi, with potent anti-metastasis activity on highly metastatic cells. The aim of this study was to investigate the function and mechanism of Gambogic Acid on tumor adhesion. We found that Gambogic Acid strongly inhibited the adhesion of human cancer cells to fibronectin. This inhibition was associated with the deformation of focal adhesion complex, which was mediated by suppressing the expression of integrin β1 and integrin signaling pathway. In vitro, cell lipid rafts clustering was inhibited following treatment of Gambogic Acid, which induced the suppression of integrin β1 and focal adhesion complex proteins colocalization within rafts. Moreover, Gambogic Acid significantly decreased cellular cholesterol content, whereas cholesterol replenishment lessened the inhibitory effect of Gambogic Acid on cell adhesion. Real-time PCR analysis showed that Gambogic Acid reduced mRNA levels of hydroxymethylglutaryl-CoA reductase and sterol regulatory element binding protein-2, while increased acetyl-CoA acetyltransferase-1/2. Taken together, these results demonstrate that Gambogic Acid inhibits cell adhesion via suppressing integrin β1 abundance and cholesterol content as well as the membrane lipid raft-associated integrin function, which provide new evidence for the anti-cancer activity of Gambogic Acid.
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inhibition of α4 integrin mediated adhesion was involved in the reduction of b16 f10 melanoma cells lung colonization in c57bl 6 mice treated with Gambogic Acid
European Journal of Pharmacology, 2008Co-Authors: Jie Zhao, Na Lu, Qi Qi, Hongyan Gu, Lei Qiang, Yong Yang, Wei Wang, Lingbo ZhangAbstract:Abstract Gambogic Acid, the major active ingredient of gamboge, has been shown to exhibit anti-cancer activity both in vivo and in vitro. However, its potential activity in tumor metastasis remains unclear. In the present study, we found that Gambogic Acid strongly inhibited the adhesion of highly metastatic mouse melanoma B16-F10 cells in vitro . Gambogic Acid also exhibited significant anti-metastasis activity on the development of in vivo artificial metastases (i.e. following tail vein i.v. injection of the B16-F10 melanoma tumor cells in C57BL/6 mice). Flow cytometric analysis and Western blot showed that Gambogic Acid inhibited the cell surface expression of α 4 integrin , while exhibited negligible effects on the expression of α 5 and β 1 integrin. Thus we concluded for the first time that Gambogic Acid could inhibit the adhesion and migration of B16-F10 cells in vitro and in vivo , in which down-regulation of α 4 integrin expression was involved.
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Inhibition of alpha(4) integrin mediated adhesion was involved in the reduction of B16-F10 melanoma cells lung colonization in C57BL/6 mice treated with Gambogic Acid.
European journal of pharmacology, 2008Co-Authors: Jie Zhao, Na Lu, Qi Qi, Hongyan Gu, Lei Qiang, Yong Yang, Wei Wang, Lingbo ZhangAbstract:Gambogic Acid, the major active ingredient of gamboge, has been shown to exhibit anti-cancer activity both in vivo and in vitro. However, its potential activity in tumor metastasis remains unclear. In the present study, we found that Gambogic Acid strongly inhibited the adhesion of highly metastatic mouse melanoma B16-F10 cells in vitro. Gambogic Acid also exhibited significant anti-metastasis activity on the development of in vivo artificial metastases (i.e. following tail vein i.v. injection of the B16-F10 melanoma tumor cells in C57BL/6 mice). Flow cytometric analysis and Western blot showed that Gambogic Acid inhibited the cell surface expression of alpha(4) integrin, while exhibited negligible effects on the expression of alpha(5) and beta(1) integrin. Thus we concluded for the first time that Gambogic Acid could inhibit the adhesion and migration of B16-F10 cells in vitro and in vivo, in which down-regulation of alpha(4) integrin expression was involved.
Jie Zhao - One of the best experts on this subject based on the ideXlab platform.
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Gambogic Acid reduced bcl 2 expression via p53 in human breast mcf 7 cancer cells
Journal of Cancer Research and Clinical Oncology, 2009Co-Authors: Hongyan Gu, Jie Zhao, Jia Wang, Rong Mu, Jingjing Rong, Qi QiAbstract:Purpose In this study, we investigated the correlation between p53 and bcl-2 in Gambogic Acid (GA)-induced apoptosis.
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inhibition of α4 integrin mediated adhesion was involved in the reduction of b16 f10 melanoma cells lung colonization in c57bl 6 mice treated with Gambogic Acid
European Journal of Pharmacology, 2008Co-Authors: Jie Zhao, Na Lu, Qi Qi, Hongyan Gu, Lei Qiang, Yong Yang, Wei Wang, Lingbo ZhangAbstract:Abstract Gambogic Acid, the major active ingredient of gamboge, has been shown to exhibit anti-cancer activity both in vivo and in vitro. However, its potential activity in tumor metastasis remains unclear. In the present study, we found that Gambogic Acid strongly inhibited the adhesion of highly metastatic mouse melanoma B16-F10 cells in vitro . Gambogic Acid also exhibited significant anti-metastasis activity on the development of in vivo artificial metastases (i.e. following tail vein i.v. injection of the B16-F10 melanoma tumor cells in C57BL/6 mice). Flow cytometric analysis and Western blot showed that Gambogic Acid inhibited the cell surface expression of α 4 integrin , while exhibited negligible effects on the expression of α 5 and β 1 integrin. Thus we concluded for the first time that Gambogic Acid could inhibit the adhesion and migration of B16-F10 cells in vitro and in vivo , in which down-regulation of α 4 integrin expression was involved.
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Inhibition of alpha(4) integrin mediated adhesion was involved in the reduction of B16-F10 melanoma cells lung colonization in C57BL/6 mice treated with Gambogic Acid.
European journal of pharmacology, 2008Co-Authors: Jie Zhao, Na Lu, Qi Qi, Hongyan Gu, Lei Qiang, Yong Yang, Wei Wang, Lingbo ZhangAbstract:Gambogic Acid, the major active ingredient of gamboge, has been shown to exhibit anti-cancer activity both in vivo and in vitro. However, its potential activity in tumor metastasis remains unclear. In the present study, we found that Gambogic Acid strongly inhibited the adhesion of highly metastatic mouse melanoma B16-F10 cells in vitro. Gambogic Acid also exhibited significant anti-metastasis activity on the development of in vivo artificial metastases (i.e. following tail vein i.v. injection of the B16-F10 melanoma tumor cells in C57BL/6 mice). Flow cytometric analysis and Western blot showed that Gambogic Acid inhibited the cell surface expression of alpha(4) integrin, while exhibited negligible effects on the expression of alpha(5) and beta(1) integrin. Thus we concluded for the first time that Gambogic Acid could inhibit the adhesion and migration of B16-F10 cells in vitro and in vivo, in which down-regulation of alpha(4) integrin expression was involved.
Hongxi Xu - One of the best experts on this subject based on the ideXlab platform.
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preparative separation of Gambogic Acid and its c 2 epimer using recycling high speed counter current chromatography
Journal of Chromatography A, 2006Co-Authors: Jingzheng Song, Chun Feng Qiao, Lina Wong, Hongxi XuAbstract:Abstract A recycling counter-current chromatographic system was first set up with a high-speed counter-current chromatography instrument coupled with a column switching valve. This system was first successfully applied to the preparative separation of epimers, Gambogic Acid and epiGambogic Acid from Garcinia hanburyi using n -hexane–methanol–water (5:4:1, v/v/v) as the two-phase solvent system. As a result, 28.2 mg Gambogic Acid and 18.4 mg epiGambogic Acid were separated from 50 mg of mixture. Their purities were both above 97% as determined by HPLC. The chemical structures were then identified by their 1 H NMR and 13 C NMR spectra.
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Short communication Preparative separation of Gambogic Acid and its C-2 epimer using recycling high-speed counter-current chromatography
2006Co-Authors: Jingzheng Song, Chun Feng Qiao, Lina Wong, Hongxi XuAbstract:A recycling counter-current chromatographic system was first set up with a high-speed counter-current chromatography instrument coupled with a column switching valve. This system was first successfully applied to the preparative separation of epimers, Gambogic Acid and epiGambogic Acid from Garcinia hanburyi using n-hexane–methanol–water (5:4:1, v/v/v) as the two-phase solvent system. As a result, 28.2 mg Gambogic Acid and 18.4 mg epiGambogic Acid were separated from 50 mg of mixture. Their purities were both above 97% as determined by HPLC. The chemical structures were then identified by their 1 H NMR and 13 C NMR spectra.
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stability and cytotoxicity of Gambogic Acid and its derivative gambogoic Acid
Biological & Pharmaceutical Bulletin, 2005Co-Authors: Susan Cheung, Chun Feng Qiao, Jingzheng Song, Hongxi XuAbstract:In this study, the stability of Gambogic Acid (GA), a polyprenylated xanthone with potent cytotoxicities against various cancer cell lines, was evaluated under several experimental conditions including addition of Acids, alkalis and organic solvents. GA was stable when dissolved in acetone, acetonitrile, and chloroform, even when Acids were added. However, a new derivative was produced after GA was stored in the methanol solution for a week at room temperature. The addition of alkalis could increase the rate of this chemical transformation. This derivative was determined to be gambogoic Acid (GOA) by the HPLC-MS comparison with the known compound. GOA was proposed to be the product of neuclophilic addition of methanol to the olefinic bond at C-10 of GA. Furthermore, when these two compounds were tested for their cytotoxicity, GOA showed significantly weaker inhibitory effects than GA. It was therefore deduced that the α,β-unsaturated carbonyl moiety at C-10 contributed to the cytotoxicity of Gambogic Acid.
