贯叶连翘中苯丙素衍生物的抗疟原虫和细胞毒性活性研究

Antiplasmodial and cytotoxic activity of phloroglucinol derivatives from Hypericum erectum Thunb.

机构信息

Inam Neuroscience Research Center, Wonkwang University, Sanbon Medical Center, Kyunggi-Do, South Korea.

出版信息

Phytother Res. 2010 Jun;24(6):941-4. doi: 10.1002/ptr.3104.

PMID:20127665

Abstract

The chloroform extracts of whole plants of Hypericum erectum were investigated for antiplasmodial activity against chloroquine-sensitive strains of Plasmodium falciparum. Five phloroglucinol derivatives, otogirin (1), otogirone (2), erectquione A (3), erectquione B (4), and erectquione C (5) were isolated from the whole plants of H. erectum. Also, five compounds were evaluated for in vitro antiplasmodial activities as well as their cytotoxic potential on SK-OV-3 cancer cell line cells. Compounds 2, 4 showed notable growth inhibitory activity against chloroquine-sensitive strains of Plasmodium falciparum with IC(50) values from 5.6 and 7.2 microM. This compound showed no significant cytotoxicity (IC(50) > 150 microM) evaluated using SK-OV-3 cancer cell line cells.

摘要

研究了贯叶连翘全植物的氯仿提取物对氯喹敏感株疟原虫的抗疟原虫活性。从贯叶连翘全植物中分离得到了 5 种邻苯三酚衍生物：otogirin（1）、otogirone（2）、erectquione A（3）、erectquione B（4）和 erectquione C（5）。还评估了这 5 种化合物的体外抗疟原虫活性及其对 SK-OV-3 癌细胞系的细胞毒性。化合物 2、4 对氯喹敏感株疟原虫表现出显著的生长抑制活性，IC（50）值分别为 5.6 和 7.2 μM。该化合物对 SK-OV-3 癌细胞系细胞的细胞毒性无显著影响（IC（50）>150 μM）。