Min B S, Kim Y H, Tomiyama M, Nakamura N, Miyashiro H, Otake T, Hattori M
College of Pharmacy, Chungnam National University, Taejon, 305-764, Korea.
Phytother Res. 2001 Sep;15(6):481-6. doi: 10.1002/ptr.751.
In the search for novel anti-human immunodeficiency virus type 1 (anti-HIV-1) agents from natural sources, 49 MeOH extracts of Korean plants were screened for their inhibitory effects against RNA-dependent DNA polymerase (RT) and ribonuclease H (RNase H) activities of HIV-1 reverse transcriptase and HIV-1 protease, and anti-HIV-1 activity. Regarding the HIV-1 reverse transcriptase, Agrimonia pilosa (whole plant), Cornus kousa (stem and leaf), Limonium tetragonum (root) and Mallotus japonicus (stem) showed significant inhibitory activity on RT activity with 50% inhibitory activity (IC(50)) of 8.9, 6.3, 7.5 and 11.9 microg/mL, respectively, whereas Agrimonia pilosa was also active against RNase H activity (IC(50) = 98.4 microg/mL). Four plants, namely Agrimonia pilosa (whole plant), Atractylodes japonica (root), Clematis heracleifolia (whole plant) and Syneilesis palmata (whole plant), were appreciably active (<35%) against recombinant HIV-1 protease at a concentration of 100 microg/mL. Crinum asiaticum var. japonicum (root) showed significant anti-HIV-1 activity (ED(50) = 12.5 microg/mL) with a favourable SI value of 16.
在从天然来源寻找新型抗人类免疫缺陷病毒1型（抗HIV-1）药物的过程中，对49种韩国植物的甲醇提取物进行了筛选，以检测它们对HIV-1逆转录酶的RNA依赖性DNA聚合酶（RT）和核糖核酸酶H（RNase H）活性、HIV-1蛋白酶以及抗HIV-1活性的抑制作用。对于HIV-1逆转录酶，龙牙草（全株）、四照花（茎和叶）、四翅滨藜（根）和野桐（茎）对RT活性表现出显著抑制活性，50%抑制活性（IC50）分别为8.9、6.3、7.5和11.9微克/毫升，而龙牙草对RNase H活性也有活性（IC50 = 98.4微克/毫升）。四种植物，即龙牙草（全株）、白术（根）、大叶铁线莲（全株）和合耳菊（全株），在浓度为100微克/毫升时对重组HIV-1蛋白酶有明显活性（<35%）。文殊兰（根）表现出显著的抗HIV-1活性（ED50 = 12.5微克/毫升），且具有良好的SI值16。
