目的 研究狭基线纹香茶菜Isodon lophanthoides var. gerardianus的水溶性成分及其抗肿瘤活性。方法 采用大孔吸附树脂D-101、ODS、Sephdex LH-20等色谱技术和重结晶进行分离纯化,通过ESI-MS、¹H-NMR、¹³C-NMR等现代波谱技术进行结构鉴定;以HepG2为供试细胞株,采用MTT法对化合物进行体外抗肿瘤活性研究。结果 从狭基线纹香茶菜水提液中分离得到12个水溶性化合物,分别鉴定为新西兰牡荆苷Ⅱ(1)、新西兰牡荆苷Ⅲ(2)、异夏佛塔苷(3)、夏佛塔苷(4)、牡荆苷(5)、芹菜素-6, 8-二-C-α-L-吡喃阿拉伯糖苷(6)、芹菜素-7-O-葡萄糖醛酸苷(7)、芹菜素-6-C-β-L-吡喃阿拉伯糖-8-C-α-L-吡喃阿拉伯糖苷(8)、芹菜素-6-C-β-D-木糖-8-C-α-L-阿拉伯糖苷(9)、咖啡酸(10)、迷迭香酸(11)、芦丁(12)。结论 化合物1～9为首次从香茶菜属植物中分离得到;其中化合物1、6、11对HepG2细胞有较好的抑制作用。

Objective To investigate the water-soluble constituents of Isodon lophanthoides var. gerardianus. Methods Compouds were isolated and purified by D-101, Sephadex LH-20, and ODS column chromatographies. The chemical structures were elucidated on the basis of spectral data and physicochemical properties. Results Twelve compounds were isolated and identified as vitexin Ⅱ (1), vicenin Ⅲ (2), isoschaftoside (3), schaftoside (4), vitexin (5), 6, 8-di-C-α-L-arabinosylapigenin (6), apigenin-7-O-glucuronide (7), apigenin 6-C-β-L-arabin-osyl-8-C-α-L-arabinopyranoside (8), apigenin 6-C-β-D-xylopyranosyl-8-C-α-L-arabinopyranoside (9), caffeic acid (10), rosmarinic (11), and rutin (12). Conclusion Compounds 1—9 are separated from I. lophanthoides var. gerardianus for the first time, and constituents of the water-soluble parts of I. lophanthoides var. gerardianus are studied systematically for the first time. Compounds 1, 6, and 11 exert antiproliferative effects on HepG2 cells.

国家科技支撑计划项目(2012BAI29B00)