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14-Formyl-15-aryloxy/methoxymatrine and 14-Aryloxymethylidenyl-matrine Derivatives as Anti-HIV-1 Agents

[ Vol. 14 , Issue. 3 ]

Author(s):

Jiulin Huang, Si-Ying Xiang, Min Lv*, Liu-Meng Yang, Yuanyuan Zhang, Yong-Tang Zheng* and Hui Xu*   Pages 249 - 252 ( 4 )

Abstract:


Background: The human immunodeficiency virus (HIV)/acquired immunodeficiency syndrome (AIDS) has always been a global health threat and leading cause of deaths. However, due to the emergence of drug-resistant HIV, an inevitable consequence of increasing use of antiretroviral drugs posed a major threat to antiretroviral therapy success.

Objective: The discovery of anti-HIV-1 agents will be used for the effective treatment of HIV/AIDS.

Method: In continuation of our program aimed to discover anti-HIV-1 agents, twelve matrine derivatives, such as 14-formyl-15-aryloxy/methoxymatrines (3a-j) and 14-aryloxymethylidenylmatrines (3k,l), were semi-prepared from matrine, and evaluated against HIV-1 IIIB replication in acutely infected C8166 cells in vitro.

Results: Among them, compound 3j showed the most potent anti-HIV-1 activity with EC50 and therapeutic index (TI) values of 1.79 µg/mL, and 98.2, respectively.

Conclusion: It has been demonstrated that the positions of methyl on the phenyl ring and 14- formylmatrine-15-oxy on the naphthyl ring were very important for the activity. It will lay the foundation for further structural modification and application of matrines as HIV-1 inhibitors.

Keywords:

Matrine derivatives, AIDS, HIV-1, inhibitors, antiretroviral drugs, peptide drugs, matrines.

Affiliation:

Research Institute of Pesticidal Design & Synthesis, College of Chemistry and Pharmacy/Plant Protection, Northwest A&F University, Yangling 712100, Key Laboratory of Bioactive Peptides of Yunnan Province/Key Laboratory of Animal Models and Human Diseases Mechanisms of Chinese Academy of Sciences, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming, Yunnan 650223, Research Institute of Pesticidal Design & Synthesis, College of Chemistry and Pharmacy/Plant Protection, Northwest A&F University, Yangling 712100, Key Laboratory of Bioactive Peptides of Yunnan Province/Key Laboratory of Animal Models and Human Diseases Mechanisms of Chinese Academy of Sciences, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming, Yunnan 650223, Research Institute of Pesticidal Design & Synthesis, College of Chemistry and Pharmacy/Plant Protection, Northwest A&F University, Yangling 712100, Key Laboratory of Bioactive Peptides of Yunnan Province/Key Laboratory of Animal Models and Human Diseases Mechanisms of Chinese Academy of Sciences, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming, Yunnan 650223, Research Institute of Pesticidal Design & Synthesis, College of Chemistry and Pharmacy/Plant Protection, Northwest A&F University, Yangling 712100

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