Xanthohumol, a novel anti-HIV-1 agent purified from Hops Humulus lupulus.
Xanthohumol, prenylchacone flavonoid, is a natural product with multi-biofunctions purified from Hops Humulus lupulus. Its anti-HIV-1 activity was tested in the present study. Results showed that xanthohumol inhibited HIV-1 induced cytopathic effects, the production of viral p24 antigen and reverse transcriptase in C8166 lymphocytes at non-cytotoxic concentration. The EC50 values were 0.82, 1.28 and 0.50 microg/ml, respectively. The therapeutic index (TI) was about 10.8. Xanthohumol also inhibited HIV-1 replication in PBMC with EC50 value of 20.74 microg/ml. The activity of recombinant HIV-1 reverse transcriptase and the HIV-1 entry were not inhibited by xanthohumol. The results from this study suggested that xanthohumol is effective against HIV-1 and might serve as an interesting lead compound. It may represent a novel chemotherapeutic agent for HIV-1 infection. However, the mechanism of its anti-HIV-1 effect needs to be further clarified.
Wang
Qian
Q
Laboratory of Molecular Immunopharmacology, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming 650223, China.
Ding
Zhi-Hui
ZH
Liu
Ji-Kai
JK
Zheng
Yong-Tang
YT
D019380:Anti-HIV Agents / Q000302:isolation & purification / Q000494:pharmacology*; D002460:Cell Line; D005419:Flavonoids; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors / Q000378:metabolism; D027582:Humulus / Q000737:chemistry*; D010936:Plant Extracts / Q000494:pharmacology; D011427:Propiophenones / Q000302:isolation & purification / Q000494:pharmacology*
D019380:Anti-HIV Agents; D005419:Flavonoids; D010936:Plant Extracts; D011427:Propiophenones; D054303:HIV Reverse Transcriptase; C104536:xanthohumol