ABSTRACT
Bioactivity-directed fractionation of antitumor compounds from the stem barks of Choerospondias axillaries (Roxb.) Burtt et Hill (Anacardiaceae) afforded two new cytotoxic bridged-ring ketones, choerosponins A (1) and B (2), and their structures were elucidated by spectroscopic methods; their stereochemistry was determined by NOE difference experiments, CD spectra and the modified Mosher's method. Compound 1 has a rare dioxatricyclo skeleton. Flow cytometry and SRB methods were employed to evaluate the antitumor activity of the two compounds against tsFT210, HCT-15, HeLa, A2780 and MCF-7 cell lines, and both of them showed strong cytotoxicity. MTT and paper disc methods were also used to evaluate their anti-hypoxia and antibacterial activities, and both of them showed no apparent activities.
Subject(s)
Anacardiaceae/chemistry , Antineoplastic Agents, Phytogenic/chemistry , Antineoplastic Agents, Phytogenic/pharmacology , Ketones/chemistry , Ketones/pharmacology , Cell Hypoxia/drug effects , Cell Line, Tumor , Cell Proliferation/drug effects , Cell Survival/drug effects , Drug Screening Assays, Antitumor , Drugs, Chinese Herbal/chemistry , Drugs, Chinese Herbal/pharmacology , HeLa Cells , Humans , MCF-7 Cells , Molecular StructureABSTRACT
Objective To investigate gallic acid-derived chemical constituents of Choerospondias axillaries (Roxb.) Burtt. et Hill., and evaluate their in vitro anti-tumor, anti-hypoxia and anti-bacteria activities. Methods The aimed chemical constituents were isolated by various chromatographic means, and their structures were identified by physicochemical and spectroscopic data. MTT method was employed to evaluate anti-tumor and anti-hypoxia activities. Antibacterial activities were tested by paper disc method. Results Seven compounds 1-7 were isolated from the stem barks of Choerospondias axillaries (Roxb.) Burtt. et Hill. and identified as gallic acid (1)gallic acid ethyl ether (2)l-0-galloyl-β-A-glucose (3)1, 6-di-0-galloyl-β-D-glucose (4)1, 4-di-0- galloyl-β-D-glucose (5)1,4,6-tri-0-galloyl-β-β-glucose (6), and 1, 3, 4, 6-tetra-0-galloyl-β-D-glucose (7). Compounds 1, 2 and 4-6 significantly inhibited K562 cells with the IC50 values of 2.9, 14.6, 39.1, 40.2, 41.2 mg/ml, respectively, and 3 and 7 also showed a slight inhibition of the K562 cells with the inhibition rate of 20.8% and 30.1V at 100 !g/ml respectively. Compounds 1-7 showed protective effects on anoxia-induced injury in cultured ECY304 and PC12 cells at the concentrations showing no significant cytotoxicity, and 5-7 also showed an antibacterial effect on Staphylococcus aureus ATCC6538 to a certain extent. Conclusion Compounds 2-7 were isolated from the genus Choerospondias for the first time. It was the first time to report 1-7 as anti-tumor and anti-hypoxia constituents of Choerospondias axillaries, and the anti-hypoxia activity for 1-7 was also recorded for the first time in the present study.
ABSTRACT
Objective To investigate gallic acid-derived chemical constituents of Choerospondias axillaries (Roxb.) Burtt. et Hill., and evaluate their in vitro anti-tumor, anti-hypoxia and anti-bacteria activities. Methods The aimed chemical constituents were isolated by various chromatographic means, and their structures were identified by physicochemical and spectroscopic data. MTT method was employed to evaluate anti-tumor and anti-hypoxia activities. Antibacterial activities were tested by paper disc method. Results Seven compounds 1-7 were isolated from the stem barks of Choerospondias axillaries (Roxb.) Burtt. et Hill. and identified as gallic acid(1), gallic acid ethyl ether(2), 1-O-galloyl-β-D-glucose(3), 1,6-di-O-galloyl-β-D-glucose(4), 1,4-di-O-galloyl-β-D-glucose(5), 1,4,6-tri-O-galloyl-β-D-glucose(6), and 1,3,4,6-tetra-O-galloyl-β-D-glucose(7). Compounds 1, 2 and 4-6 significantly inhibited K562 cells with the IC50 values of 2.9, 14.6, 39.1, 40.2, 41.2 μg/ml, respectively, and 3 and 7 also showed a slight inhibition of the K562 cells with the inhibition rate of 20.8% and 30.1% at 100 μg/ml respectively. Compounds 1-7 showed protective effects on anoxia-induced injury in cultured ECV304 and PC12 cells at the concentrations showing no significant cytotoxicity, and 5-7 also showed an antibacterial effect on Staphylococcus aureus ATCC6538 to a certain extent. Conclusion Compounds 2-7 were isolated from the genus Choerospondias for the first time. It was the first time to report 1-7 as anti-tumor and anti-hypoxia constituents of Choerospondias axillaries, and the anti-hypoxia activity for 1-7 was also recorded for the first time in the present study.
ABSTRACT
Aim To study the molecular basis of protection on myocardial ischemic injuries of total flavones of choerospondias axiaris fructus(TFC). Methods The microarray analysis for the protein expression in myocardium provide a strong tool to explore the key protein candidates involved in the pathogenesis of ischemic injury.Surface enhanced laser desorption/ionization(SELDI) mass spectrometry with protein chip IMAC3,SAX2 and NP20 was used to compare the differentially expressed protein in TFC-treated and untreated ischemic myocardium in rats and the results were analysized with Proteinchip Software 3.0.2.Results Seven differentially expressed proteins were indentified in TFC treated myocardium.These differential effects correlated with the expression of five downregulated proteins and two upregulated proteins,and four of them were discovered on the IMAC3 chip and one of them was discovered on the SAX2 chip.Conclusions The myocardial protection of TFC may be mediated by the differential expression of these proteins which could be the key protein candidates for further investigation.
