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Molecules 2017, 22(9), 1498; doi:10.3390/molecules22091498

Anti-HIV Activities and Mechanism of 12-O-Tricosanoylphorbol-20-acetate, a Novel Phorbol Ester from Ostodes katharinae

1
Key Laboratory of Bioactive Peptides of Yunnan Province/Key Laboratory of Animal Models and Human Disease Mechanisms of the Chinese Academy of Sciences, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming 650223, Yunnan, China
2
Kunming College of Life Science, University of Chinese Academy of Sciences, Kunming 650204, Yunnan, China
3
State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, Yunnan, China
4
KIZ-SU Joint Laboratory of Animal Models and Drug Development, College of Pharmaceutical Sciences, Soochow University, Suzhou 215006, Jiangsu, China
These authors contributed equally to this work.
*
Authors to whom correspondence should be addressed.
Received: 24 June 2017 / Revised: 1 September 2017 / Accepted: 6 September 2017 / Published: 8 September 2017
(This article belongs to the Section Natural Products)
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Abstract

APOBEC3G is a member of the human cytidine deaminase family that restricts Vif-deficient viruses by being packaged with progeny virions and inducing the G to A mutation during the synthesis of HIV-1 viral DNA when the progeny virus infects new cells. HIV-1 Vif protein resists the activity of A3G by mediating A3G degradation. Phorbol esters are plant-derived organic compounds belonging to the tigliane family of diterpenes and could activate the PKC pathway. In this study, we identified an inhibitor 12-O-tricosanoylphorbol-20-acetate (hop-8), a novel ester of phorbol which was isolated from Ostodes katharinae of the family Euphorbiaceae, that inhibited the replication of wild-type HIV-1 and HIV-2 strains and drug-resistant strains broadly both in C8166 cells and PBMCs with low cytotoxicity and the EC50 values ranged from 0.106 μM to 7.987 μM. One of the main mechanisms of hop-8 is to stimulate A3G expressing in HIV-1 producing cells and upregulate the A3G level in progeny virions, which results in reducing the infectivity of the progeny virus. This novel mechanism of hop-8 inhibition of HIV replication might represents a promising approach for developing new therapeutics for HIV infection. View Full-Text
Keywords: antiviral agent; 12-O-tricosanoylphorbol-20-acetate; HIV; Vif; APOBEC3G; phorbol ester antiviral agent; 12-O-tricosanoylphorbol-20-acetate; HIV; Vif; APOBEC3G; phorbol ester
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Chen, H.; Zhang, R.; Luo, R.-H.; Yang, L.-M.; Wang, R.-R.; Hao, X.-J.; Zheng, Y.-T. Anti-HIV Activities and Mechanism of 12-O-Tricosanoylphorbol-20-acetate, a Novel Phorbol Ester from Ostodes katharinae. Molecules 2017, 22, 1498.

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