Anti-HIV-1 activities of compounds isolated from the medicinal plant Rhus chinensis.
OBJECTIVE
Previously, we reported that the petroleum ether fraction, RC-1, and EtOAc fraction, RC-2, of the medicinal plant Rhus chinensis showed potent anti-HIV-1 activities. To address anti-HIV-1 constituents of RC-1 and RC-2, 17 compounds were isolated. Anti-HIV-1 activities and possible action mechanisms of these compounds were investigated.


METHODS
The syncytial formation induced by HIV-1 was determined under the inverted microscope, cellular toxicity and protection assay were assessed by MTT method, reduction of p24 antigen expression level and RT activity were measured by ELISA, and inhibition of recombinant HIV-1 PR was monitored by the fluorescent signal.


RESULTS
The compounds 1 and 13 inhibited HIV-1-induced syncytium formation potently with TI value of 42.31 and 19.07, respectively. Compounds 4, 5, 6, 9 and 10 were less potent with TI value of 8.94, 8.22, 4.14, 5.11 and 5.34, respectively. Compound 1, a benzofuranone-type compound, previously reported as a novel anti-HIV-1 agent, might target late-steps of HIV-1 life cycle. Compound 13 inhibited HIV-1 replication with EC(50) of 7.16mug/ml and might target at/before integration step.


CONCLUSIONS
These compounds might contribute to anti-HIV-1 activities extracts of the medicinal plant Rhus chinensis.
Wang
Rui-Rui
RR
Laboratory of Molecular Immunopharmacology, Key Laboratory of Animal Models and Human Disease Mechanisms, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming, Yunnan 650223, China.
Gu
Qiong
Q
Wang
Yun-Hua
YH
Zhang
Xue-Mei
XM
Yang
Liu-Meng
LM
Zhou
Jun
J
Chen
Ji-Jun
JJ
Zheng
Yong-Tang
YT
D019380:Anti-HIV Agents / Q000302:isolation & purification / Q000494:pharmacology*; D002460:Cell Line; D004797:Enzyme-Linked Immunosorbent Assay; D015726:Giant Cells / Q000187:drug effects / Q000502:physiology; D016655:HIV Core Protein p24 / Q000378:metabolism; D015658:HIV Infections / Q000188:drug therapy / Q000821:virology; D015497:HIV-1 / Q000187:drug effects*; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology; D018547:Plant Stems / Q000737:chemistry; D029045:Rhus / Q000737:chemistry*; D013778:Tetrazolium Salts; D013844:Thiazoles
D019380:Anti-HIV Agents; D016655:HIV Core Protein p24; D010936:Plant Extracts; D013778:Tetrazolium Salts; D013844:Thiazoles; C022616:thiazolyl blue