[1]任茜茜,周慧超,贺　爽,等.蓝萼香茶菜化学成分及抗肿瘤活性研究[J].新乡医学院学报,2016,33(4):261-266.[doi:10.7683/xxyxyxb.2016.04.004]
　REN Xi-xi,ZHOU Hui-chao,HE Shuang,et al.Chemical constituents and antitumor activity of Isodon japonica var.glaucocalyx[J].Journal of Xinxiang Medical University,2016,33(4):261-266.[doi:10.7683/xxyxyxb.2016.04.004]
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蓝萼香茶菜化学成分及抗肿瘤活性研究
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《新乡医学院学报》[ISSN:1004-7239/CN:41-1186/R]

卷:
33
期数:
2016年4
页码:
261-266
栏目:
基础研究
出版日期:
2016-04-06

文章信息/Info

Title:
Chemical constituents and antitumor activity of Isodon japonica var.glaucocalyx
作者:
任茜茜; 周慧超; 贺　爽; 白素平
（新乡医学院药学院，河南　新乡　453003）
Author(s):
REN Xi-xi; ZHOU Hui-chao; HE Shuang; BAI Su-ping
(School of Pharmacy,Xinxiang Medical University,Xinxiang 453003,Henan Province,China)
关键词:
蓝萼香茶菜; 二萜; 结构鉴定; 抗肿瘤活性; 凋亡
Keywords:
Isodon japonica var.glaucocalyx; diterpenoids; structural identification; antitumor activity; apoptosis
分类号:
R914
DOI:
10.7683/xxyxyxb.2016.04.004
文献标志码:
A
摘要:
目的　研究药用植物蓝萼香茶菜的化学成分，为进一步研究其抗肿瘤活性提供依据。方法　蓝萼香茶菜叶的70％丙酮提取物的乙酸乙酯萃取部分，应用反复硅胶柱层析、重结晶等方法分离纯化，并用波谱分析方法鉴定分离得到的化合物的结构；用四甲基偶氮唑盐法（MTT）检测评价了其中7个二萜化合物的体外抗肿瘤活性，并用荧光显微镜观察了化合物1对肿瘤细胞的形态学影响。结果　从蓝萼香茶菜叶中分离鉴定了12个已知化合物，其中7个化合物为对映-贝壳杉烷类二萜：蓝萼香茶菜甲素(1)、蓝萼香茶菜乙素(2)、蓝萼香茶菜丁素(3)、蓝萼香茶菜戊素(4)、毛叶醇(5)、对映-贝壳杉-3β,16β-二醇(6)和16R-甲基-3α,7α,14β-三羟基-对映-贝壳杉-15-酮(7)；2个化合物为三萜：2α-羟基乌苏酸 (8)和齐墩果酸 (9)；1个黄酮类化合物：胡麻素(10)；2个有机酸：正十四烷酸(11)和正十六烷酸(12)。MTT法检测结果发现，化合物1、2和3对人肝癌HepG2细胞和人宫颈癌Hela细胞显示较强的体外抗肿瘤活性；化合物1处理HepG2细胞后荧光倒置显微镜下观察到细胞凋亡现象。结论　河南辉县产药用植物蓝萼香茶菜富含有抗肿瘤活性的对映-贝壳杉烷类二萜，是一类具有前景的抗肿瘤先导化合物。化合物1通过诱导细胞凋亡抑制肿瘤细胞增殖。
Abstract:
Objective　To investigate the chemical constituents of medicinal plant Isodon japonica var.glaucocalyx which from Huixian of Henan province,and provide the support for further investigation of it′s antitumor activity.Methods　The chemical constituents were isolated and purified by means of repeated silica column chromatography and recrystallization from the ethyl acetate-portion of 70% acetone extract of the leaves of Isodon japonica var.glaucocalyx.Their structures were identified by spectral analysis and their antitumor activity was evaluated by 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2-H-tetrazolium bromide（MTT） assay.The effects of compound on morphological changes of tumor cells was observed under reverse fluorescence microscopy.Results　Twelve known compounds were identified from the leaves of Isodon japonica var.glaucocalyx.Seven of them were ent-kaurane diterpenoids,i.e.,glaueocalyxin A(1),glaucocalyxin B (2),glaucocalyxin D (3),glaucocalyxin E (4),gabdosinatol (5),ent-kaurane-3β,16β-diol(6),16R-methyl-3α,7α,14β-trihydroxy-ent-kaur-15-one (7).Two of them were triterpenoids,2α-hydroxyursoic acid (8) and oeanlic acid(9).One flavones,pedalitin(10).Two organic acid,i.e.,tetradecanoic acid (11) and hexadecanoic acid(12).The result of MTT assay indicated that compounds 1,2 and 3 shown the potent antitumor activity in vitro against HepG2 and Hela tumor cell lines.Apoptotic cells were observed in HepG2 cells treated with compound 1 under reverse fluorescence microscopy.Conclusion　The ent-kaurane diterpenoids with antitumor activity are the main active components of Isodon japonica vat.glaucocalyx collected from Huixian of Henan province.This kind of compounds is promising antitumor lead compound.Compound 1 can inhibit the growth of tumor cells by inducing cell apoptosis.

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更新日期/Last Update: 2016-04-05