番石榴的化学成分及其抗肿瘤与抗真菌活性  

Chemical constituents of Psidium guajava and their antitumor and antifungal activities

作　　者：刘晓聪 林冬梅 刘敏[1] 张敏 李强[1] 王健[1] 徐露琳 高原 杨健[2] LIU Xiao-cong;LIN Dong-mei;LIU Min;ZHANG Min;LI Qiang;WANG Jian;XU Lu-lin;GAO Yuan;YANG Jian(Faculty of Materials and Chemical Engineerings Yibin University,Yibin 644000,China;State Key Laboratory Breeding Base of Dao-di Herbs,National Resource Center for Chinese Materia Medica,China Academy of Chinese Medical Sciences,Beijing 100700,China)

机构地区：[1]宜宾学院材料与化学工程学部,四川宜宾644000 [2]中国中医科学院中药资源中心道地药材国家重点实验室培育基地,北京100700

出　　处：《中国中药杂志》2021年第15期3877-3885,共9页China Journal of Chinese Materia Medica

基　　金：国家自然科学基金青年基金项目(21702181);国家重点研发计划项目(2020YFC1712700,2018YFC1706100);中央本级重大增减支项目(2060302);中央级公益性科研院所基本科研业务费专项(ZZXT201906)。

摘　　要：采用正相硅胶、Sephadex LH-20、制备液相色谱等分离方法,结合核磁共振谱(NMR)与质谱(MS)技术,从番石榴叶中分离鉴定出26个化合物,包括16个杂源萜(116),1个三萜(17),4个其他萜类衍生物(1821)以及5个芳香类化合物(2226),其中2126为首次从该属植物中分离得到。(R)-2-ethylhexyl 2H-1,2,3-triazole-4-carboxylate(24a)是最近从单叶藤橘属植物Paramignya trimera中分离得到的1种α-葡萄糖苷酶抑制剂,其结构被修正为24。对杂萜化合物116进行抗肿瘤与抗真菌活性测试,结果显示,番石榴杂萜psiguajadial D(4)、guapsidial A(5)、4,5-diepipsidial A(7)、guadial A(14)、guadial B(15)对5种人体肿瘤细胞株(HL-60、A-549、SMMC-7721、MCF-7、SW-480)均具有明显抑制作用,其中guapsidial A(5)活性最显著,半数抑制浓度为3.219.94μmol·L^(-1)。Twenty-six compounds, including sixteen meroterpenoids(1-16), a triterpenoid(17), four terpenoid derivatives(18-21), and five aromatic compounds(22-26), were isolated from the leaves of Psidium guajava. Their structures were identified by spectroscopic analyses including NMR and MS. Compounds 21-26 were obtained from plants of Psidium for the first time. Based on the structure,(R)-2-ethylhexyl 2H-1,2,3-triazole-4-carboxylate(24 a), an α-glucosidase inhibitor recently isolated from Paramignya trimera, should be revised as compound 24. Meroterpenoids 1-16 were evaluated for their antitumor and antifungal activities. Meroterpenoids psiguajadial D(4), guapsidial A(5), 4,5-diepipsidial A(7), guadial A(14), and guadial B(15) showed cytotoxicities against five human tumor cell lines(HL-60, A-549, SMMC-7721, MCF-7, and SW-480), among which 5 was the most effective with an IC50 of 3.21-9.94 μmol·L^(-1).

关 键 词：番石榴 化学成分 杂萜 抗肿瘤活性 抗真菌活性 

分 类 号：R284.1[医药卫生—中药学] R285[医药卫生—中医学]