蓝萼香茶菜化学成分与生物活性研究

Chemical constituents and bioactivity of Isodon japonica var. glaucocalyx

目的研究蓝萼香茶菜叶的化学成分,为进一步研究其生物活性提供依据。方法利用硅胶柱层析对蓝萼香茶菜叶进行分离和纯化其化合物,用波谱分析方法鉴定其结构,并运用四甲基偶氮唑盐比色法对从该植物中分离得到的部分化合物进行了细胞毒活性筛选。结果从蓝萼香茶菜叶中分离鉴定了10个化合物,分别是蓝萼香茶菜庚素(1)、蓝萼香茶菜辛素(2)、蓝萼香茶菜壬素(3)、蓝萼香茶菜甲素(4)、蓝萼香茶菜乙素(5)、毛叶醇(6)、entkaurane-3β,16β-diol(7)、木犀草素-7-甲醚(8)、胡麻素(9)、水杨酸(10)。其中化合物1、4、5具有较强的细胞毒活性。结论化合物1、2、3、6、7、9、10首次从蓝萼香茶菜中分离得到,且化合物1、4、5对肿瘤细胞的增殖具有明显的抑制作用。

Objective To study the chemical constituents of Isodon japonica var. glaucocalyx and provide guidance for further investigation of its bioactivity. Methods Isodonjaponica var. glaucocalyx were separated and purified by silica gel column chromatography and their structures were determined by spectroscopic methods. The cytotoxic activity of some of the compounds which isolated from the Isodon japonica var. glaucocalyx was screened by methyl thiazolyl tetrazolium assay. Results Ten compounds were separated and purified from Isodon japonica var. glaucocalyx. All these compounds were identified as follows ： glaucocalyxin G（ 1 ） ,7α, 14β-dihydroxy-16-methoxy-methyl-ent-kaur-3,15-dione （ 2 ） , （16R） -methyl-3α ,7α, 14β-trihy- droxy-ent-kaur- 15-one （ 3 ）, glaucocalyxin A （ 4 ）, glaucocalyxin B （ 5 ）, rabdosinatol （ 6 ）, ent-kaurane-3 β,16β -diol （ 7 ）, 7-meth- ylluteolin （ 8 ）, pedalitin （9）, o-Hydroxy-benzoic acid （10）. Compounds 1,4 and 5 had strong cytotoxic activity. Conclusion Compounds 1,2,3,6,7,9 and 10 were separated from the genus of lsodon japonica vat. glaucocalyx for the first time. Compounds 1,4 and 5 have apparente depressant effect on tumor cell.