国际药学研究杂志
國際藥學研究雜誌
국제약학연구잡지
INTERNATIONAL JOURNAL OF PHARMACEUTICAL RESEARCH
2014年
4期
449-455
,共7页
李长伟%崔承彬%蔡兵%韩冰%李明明%范明
李長偉%崔承彬%蔡兵%韓冰%李明明%範明
리장위%최승빈%채병%한빙%리명명%범명
药物化学%多酚类%分离鉴定%南酸枣%抗肿瘤活性%抗缺氧活性%抗菌活性
藥物化學%多酚類%分離鑒定%南痠棘%抗腫瘤活性%抗缺氧活性%抗菌活性
약물화학%다분류%분리감정%남산조%항종류활성%항결양활성%항균활성
medicinal chemistry%polyphenol%isolation and identification%Choerospondias axillaries%anti-tumor activity%anti-hypoxia activity%anti-bacteria activity
目的:阐明南酸枣中没食子酸衍生物类化学成分及其体外抗肿瘤、抗缺氧、抗菌活性。方法利用各种色谱技术分离化学成分,根据理化性质和光谱数据鉴定结构,利用MTT法测评抗肿瘤与抗缺氧活性,用纸片法测定抗菌活性。结果从南酸枣树皮中分离鉴定了没食子酸(1)、没食子酸乙酯(2)、1-O-没食子酰基-β-D-吡喃葡萄糖(3)、1,6-二-O-没食子酰基-β-D-吡喃葡萄糖(4)、1,4-二-O-没食子酰基-β-D-吡喃葡萄糖(5)、1,4,6-三-O-没食子酰基-β-D-吡喃葡萄糖(6)、1,3,4,6-四-O-没食子酰基-β-D-吡喃葡萄糖(7)等7个没食子酸衍生物类化合物。化合物1、2、4~6对K562细胞呈较强抗肿瘤活性,IC50分别为2.9、14.6、39.1、40.2和41.2μg /ml;化合物3和7活性较弱,在100μg /ml浓度下对K562细胞的抑制率分别为20.8%和30.1%。在对ECV304和PC12细胞的缺氧损伤保护实验中,1~7在无明显细胞毒作用的浓度下呈较强的抗缺氧活性。化合物5~7还对受试金黄色葡萄球菌显示一定的抗菌活性。结论化合物2~7为首次从南酸枣属植物分离得到。化合物1~7作为南酸枣中抗肿瘤、抗缺氧活性成分系首次报道,其抗缺氧活性也属首次报道。
目的:闡明南痠棘中沒食子痠衍生物類化學成分及其體外抗腫瘤、抗缺氧、抗菌活性。方法利用各種色譜技術分離化學成分,根據理化性質和光譜數據鑒定結構,利用MTT法測評抗腫瘤與抗缺氧活性,用紙片法測定抗菌活性。結果從南痠棘樹皮中分離鑒定瞭沒食子痠(1)、沒食子痠乙酯(2)、1-O-沒食子酰基-β-D-吡喃葡萄糖(3)、1,6-二-O-沒食子酰基-β-D-吡喃葡萄糖(4)、1,4-二-O-沒食子酰基-β-D-吡喃葡萄糖(5)、1,4,6-三-O-沒食子酰基-β-D-吡喃葡萄糖(6)、1,3,4,6-四-O-沒食子酰基-β-D-吡喃葡萄糖(7)等7箇沒食子痠衍生物類化閤物。化閤物1、2、4~6對K562細胞呈較彊抗腫瘤活性,IC50分彆為2.9、14.6、39.1、40.2和41.2μg /ml;化閤物3和7活性較弱,在100μg /ml濃度下對K562細胞的抑製率分彆為20.8%和30.1%。在對ECV304和PC12細胞的缺氧損傷保護實驗中,1~7在無明顯細胞毒作用的濃度下呈較彊的抗缺氧活性。化閤物5~7還對受試金黃色葡萄毬菌顯示一定的抗菌活性。結論化閤物2~7為首次從南痠棘屬植物分離得到。化閤物1~7作為南痠棘中抗腫瘤、抗缺氧活性成分繫首次報道,其抗缺氧活性也屬首次報道。
목적:천명남산조중몰식자산연생물류화학성분급기체외항종류、항결양、항균활성。방법이용각충색보기술분리화학성분,근거이화성질화광보수거감정결구,이용MTT법측평항종류여항결양활성,용지편법측정항균활성。결과종남산조수피중분리감정료몰식자산(1)、몰식자산을지(2)、1-O-몰식자선기-β-D-필남포도당(3)、1,6-이-O-몰식자선기-β-D-필남포도당(4)、1,4-이-O-몰식자선기-β-D-필남포도당(5)、1,4,6-삼-O-몰식자선기-β-D-필남포도당(6)、1,3,4,6-사-O-몰식자선기-β-D-필남포도당(7)등7개몰식자산연생물류화합물。화합물1、2、4~6대K562세포정교강항종류활성,IC50분별위2.9、14.6、39.1、40.2화41.2μg /ml;화합물3화7활성교약,재100μg /ml농도하대K562세포적억제솔분별위20.8%화30.1%。재대ECV304화PC12세포적결양손상보호실험중,1~7재무명현세포독작용적농도하정교강적항결양활성。화합물5~7환대수시금황색포도구균현시일정적항균활성。결론화합물2~7위수차종남산조속식물분리득도。화합물1~7작위남산조중항종류、항결양활성성분계수차보도,기항결양활성야속수차보도。
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.