Planta Med 2008; 74 - PA13
DOI: 10.1055/s-0028-1084012

Inhibition of HIV-1 protease and RNase H of HIV-1 reverse transcriptase activities by long chain phenols from the Sarcotestas of Ginkgo biloba

JS Lee 1, M Hattori 2, J Kim 1
  • 1College of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul National University, Seoul, Korea
  • 2Research Institute for Natural Medicine (Wakan-Yaku), University of Toyama, Japan

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)

References: 1. Lee, J.S. et al. (1998)J Nat. Prod. 61:867–871

2. Ma, C. et al. (1999) Chem. Pharm. Bull. 47:141–5.

3. Min, B.S. et al. (2002) Phytother. Res. 16:57–62.

4. Ahn, M.J. et al. (2004) Biol. Pharm. Bull. 27:544–7.