Inhibitory effects of Korean plants on HIV-1 activities.
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.
Min
B S
BS
College of Pharmacy, Chungnam National University, Taejon, 305-764, Korea.
Kim
Y H
YH
Tomiyama
M
M
Nakamura
N
N
Miyashiro
H
H
Otake
T
T
Hattori
M
M
D019380:Anti-HIV Agents / Q000494:pharmacology*; D016333:HIV Protease / Q000378:metabolism; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors; D015497:HIV-1 / Q000187:drug effects*; D029001:Herbal Medicine; D006801:Humans; D007723:Korea; D008517:Phytotherapy; D010936:Plant Extracts / Q000494:pharmacology*; D010946:Plants, Medicinal / Q000145:classification; D016914:Ribonuclease H / Q000037:antagonists & inhibitors / Q000378:metabolism
D019380:Anti-HIV Agents; D010936:Plant Extracts; D054303:HIV Reverse Transcriptase; D016914:Ribonuclease H; D016333:HIV Protease