Inhibition of HIV-1 protease and RNase H of HIV-1 reverse transcriptase activities by long chain phenols from the Sarcotestas of Ginkgo biloba
Nine long chain phenols: four cardanols, two bilobols and three alkylsalicylic acids were isolated from the CH2Cl2 extracts of the sarcotestas of Ginkgo biloba for HIV-1 protease (PR) inhibitors. From these phenols, the bilobols (IC50, 2.6–5.8µM) and alkylsalicylic acids (IC50, 10.2–24.9µM) exhibited dose-dependent potent inhibitory activities on HIV-1 PR, while the cardanols did not. On the other hand, only the alkylsalicylic acids (IC50, 33.7–170.3µM) inhibited the activities of RNase H of HIV-1 reverse transcriptase (RT) while all of the compounds failed to affect the RNA dependent DNA polymerase (RDDP) of HIV-1 RT. Therefore, we regard bilobols as a new class and selective inhibitors of HIV-1 PR; in addition, alkylsalicylic acids are elucidated as new class inhibitors of HIV-1 PR and RNase H of HIV-1 RT.
Acknowledgements: This work was supported by the Korea Research Foundation Grant funded by the Korean Government (MOEHRD). (KRF-2005–050-E00007)
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