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Hep G2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Hep G2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。
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 3shown the potent antitumor activity in vitro against Hep G2 and Hela tumor cell lines. Apoptotic cells were observed in Hep G2 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.
出处
《新乡医学院学报》
CAS
2016年第4期261-266,共6页
Journal of Xinxiang Medical University
基金
国家自然科学基金资助项目(编号:81072552)
河南省科技创新杰出青年基金资助项目(编号:104100510016)
关键词
蓝萼香茶菜
二萜
结构鉴定
抗肿瘤活性
凋亡
Isodon japonica var
glaucocalyx
diterpenoids
structural identification
antitumor activity
apoptosis
