Anti-HIV Activities and Mechanism of 12-O-Tricosanoylphorbol-20-acetate, a Novel Phorbol Ester from Ostodes katharinae
Chen, Huan1,3; Zhang, Rong2; Luo, Rong-Hua1; Yang, Liu-Meng1; Wang, Rui-Rui1; Hao, Xiao-Jiang2; Zheng, Yong-Tang1,4
2017-09-01
Source PublicationMOLECULES
ISSN1420-3049
Volume22Issue:9Pages:1498
AbstractAPOBEC3G 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 mu M to 7.987 mu M. 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.
KeywordAntiviral Agent 12-o-tricosanoylphorbol-20-acetate Hiv Vif Apobec3g Phorbol Ester
Subject AreaChemistry, Organic
DOI10.3390/molecules22091498
Indexed BySCI
Language英语
WOS IDWOS:000411499400091
Citation statistics
Document Type期刊论文
Identifierhttp://ir.kib.ac.cn/handle/151853/54892
Collection植物化学与西部植物资源持续利用国家重点实验室
Affiliation1.Chinese Acad Sci, Kunming Inst Zool, Key Lab Anim Models & Human Dis Mech, Key Lab Bioact Peptides Yunnan Prov, Kunming 650223, Yunnan, Peoples R China
2.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Kunming 650201, Yunnan, Peoples R China
3.Univ Chinese Acad Sci, Kunming Coll Life Sci, Kunming 650204, Yunnan, Peoples R China
4.Soochow Univ, Coll Pharmaceut Sci, KIZ SU Joint Lab Anim Models & Drug Dev, Suzhou 215006, Jiangsu, Peoples R China
Recommended Citation
GB/T 7714
Chen, Huan,Zhang, Rong,Luo, Rong-Hua,et al. Anti-HIV Activities and Mechanism of 12-O-Tricosanoylphorbol-20-acetate, a Novel Phorbol Ester from Ostodes katharinae[J]. MOLECULES,2017,22(9):1498.
APA Chen, Huan.,Zhang, Rong.,Luo, Rong-Hua.,Yang, Liu-Meng.,Wang, Rui-Rui.,...&Zheng, Yong-Tang.(2017).Anti-HIV Activities and Mechanism of 12-O-Tricosanoylphorbol-20-acetate, a Novel Phorbol Ester from Ostodes katharinae.MOLECULES,22(9),1498.
MLA Chen, Huan,et al."Anti-HIV Activities and Mechanism of 12-O-Tricosanoylphorbol-20-acetate, a Novel Phorbol Ester from Ostodes katharinae".MOLECULES 22.9(2017):1498.
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