中华大蟾蜍皮化学成分及其细胞毒活性  

Chemical constituents from the skins of Bufo bufo gargarizans and their cytotoxic activities

作　　者：孟令杰 孔庆宏 姜念 吕慧婧 黎成锦 郭朝霞 刘云 MENG Ling-jie;KONG Qing-hong;JIANG Nian;L Hui-jing;LI Cheng-jin;GUO Zhao-xia;LIU Yun(Guizhou Provincial College-based Key Laboratory for Tumor Prevention and Treatment with Distinctive Medicines,Zunyi Medical University,Zunyi 563000,China;College of Basic Medicine,Zunyi Medical University,Zunyi 563000,China;School of Forensic Medicine,Zunyi Medical University,Zunyi 563000,China)

机构地区：[1]遵义医科大学,贵州省普通高等学校特色药物肿瘤防治重点实验室,贵州遵义563000 [2]遵义医科大学基础医学院,贵州遵义563000 [3]遵义医科大学法医学院,贵州遵义563000

出　　处：《中成药》2023年第11期3622-3626,共5页Chinese Traditional Patent Medicine

基　　金：国家自然科学基金(82160693);贵州省科学技术基金(黔科合基础-ZK[2021]一般517号);贵州省科技计划项目(黔科合基础-ZK[2021]一般513号);贵州省科技支撑计划项目(黔科合支撑[2020]4Y154号);贵州省卫生健康委科学技术基金(gzwkj2023-566);遵义市科技计划项目(黔科平台人才[2020]003号,遵市科合HZ字[2021]277号);遵义医科大学博士科研启动项目(F-988);遵义医科大学创新训练项目(ZYDC202202165)。

摘　　要：目的研究中华大蟾蜍Bufo bufo gargarizans Cantor皮的化学成分及其细胞毒活性。方法中华大蟾蜍皮95%乙醇提取物采用硅胶、Sephadex LH-20、ODS、制备HPLC进行分离纯化,根据理化性质及波谱数据鉴定所得化合物的结构。采用SRB法评价其对结肠癌细胞HCT-116、HT-29的毒活性。结果从中分离得到5个化合物,分别鉴定为(2β,5β,14β,15β,16β)-2,15-二羟基-14,15-环氧-16-乙酰基-蟾蜍甾-20,22-二烯(1)、1β-羟基蟾毒灵(2)、19-oxobufalin(3)、(3α,5β,14β)-3,11,14-trihydroxy-12-oxo-bufa-9(11),20,22-trienolide(4)、(3β,5β,16α)-3,5,16-trihydroxy-bufa-14,20,22-trienolide(5)。化合物1~4对HCT-116细胞的IC_(50)值为0.08~2.67μmol/L,对HT-29细胞的IC_(50)值为0.24~9.80μmol/L。结论化合物1为新化合物。化合物1~4对HCT-116、HT-29细胞具有毒活性。AIM To study the chemical constituents from the skins of Bufo bufo gargarizans Cantor and their cytotoxic activities.METHODS The 95%ethanol extract from the skins of B.bufo gargarizans was isolated and purified by silica gel,Sephadex LH-20,ODS and preparative HPLC,then the structures of obtained compounds were identified by physicochemical properties and spectral data.Their cytotoxic activities against colon cancer cells HCT-116 and HT-29 were evaluated by SRB assay.RESULTS Five compounds were isolated and identified as(2β,5β,14β,15β,16β)-2,15-dihydroxy-14,15-epoxy-16-acetyloxy-bufa-20,22-dienolide(1),1β-hydroxylbufalin(2),19-oxobufalin(3),(3α,5β,14β)-3,11,14-trihydroxy-12-oxo-bufa-9(11),20,22-trienolide(4),(3β,5β,16α)-3,5,16-trihydroxy-bufa-14,20,22-trienolide(5).The IC_(50)values of compounds 1-4 on HCT-116 cell were 0.08-2.67μmol/L,and the IC_(50)values on HT-29 cell were 0.24-9.80μmol/L.CONCLUSION Compound 1 is a new compound.Compounds 1-4 exhibit cytotoxic activities on HCT-116 and HT-29 cells.

关 键 词：中华大蟾蜍 皮 化学成分 分离鉴定 细胞毒活性 

分 类 号：R284[医药卫生—中药学]