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Discovery of a semi-synthesized cyclolignan as a potent HIV-1 non-nucleoside reverse transcriptase inhibitor.
Guo, Jia-Mei; Ba, Ming-Yu; Yang, Ying; Yao, Chun-Suo; Yu, Miao; Shi, Jian-Gong; Guo, Ying.
Affiliation
  • Guo JM; a State Key Laboratory of Bioactive Substance and Function of Natural Medicines, and Beijing Key Laboratory of New Drug Mechanisms and Pharmacological Evaluation Study, Institute of Materia Medica , Chinese Academy of Medical Sciences and Peking Union Medical College , Beijing 100050 , China.
  • Ba MY; a State Key Laboratory of Bioactive Substance and Function of Natural Medicines, and Beijing Key Laboratory of New Drug Mechanisms and Pharmacological Evaluation Study, Institute of Materia Medica , Chinese Academy of Medical Sciences and Peking Union Medical College , Beijing 100050 , China.
  • Yang Y; a State Key Laboratory of Bioactive Substance and Function of Natural Medicines, and Beijing Key Laboratory of New Drug Mechanisms and Pharmacological Evaluation Study, Institute of Materia Medica , Chinese Academy of Medical Sciences and Peking Union Medical College , Beijing 100050 , China.
  • Yao CS; a State Key Laboratory of Bioactive Substance and Function of Natural Medicines, and Beijing Key Laboratory of New Drug Mechanisms and Pharmacological Evaluation Study, Institute of Materia Medica , Chinese Academy of Medical Sciences and Peking Union Medical College , Beijing 100050 , China.
  • Yu M; a State Key Laboratory of Bioactive Substance and Function of Natural Medicines, and Beijing Key Laboratory of New Drug Mechanisms and Pharmacological Evaluation Study, Institute of Materia Medica , Chinese Academy of Medical Sciences and Peking Union Medical College , Beijing 100050 , China.
  • Shi JG; a State Key Laboratory of Bioactive Substance and Function of Natural Medicines, and Beijing Key Laboratory of New Drug Mechanisms and Pharmacological Evaluation Study, Institute of Materia Medica , Chinese Academy of Medical Sciences and Peking Union Medical College , Beijing 100050 , China.
  • Guo Y; a State Key Laboratory of Bioactive Substance and Function of Natural Medicines, and Beijing Key Laboratory of New Drug Mechanisms and Pharmacological Evaluation Study, Institute of Materia Medica , Chinese Academy of Medical Sciences and Peking Union Medical College , Beijing 100050 , China.
J Asian Nat Prod Res ; 21(1): 76-85, 2019 Jan.
Article in En | MEDLINE | ID: mdl-29281889
ABSTRACT
Non-nucleoside reverse transcriptase inhibitors (NNRTIs) are essential components of highly active antiretroviral therapy (HAART) for human immunodeficiency virus type 1 (HIV-1) infection. In this study, we identified (+)-(7'S,8S,8'S)-3',4,4',5,5'-pentamethoxy-2,7'-cyclolignan (SG-1), a cyclolignan semi-synthesized from Machilus robusta and M. wangchiana extracts, as a potent NNRTI. SG-1 displayed anti-HIV-1 activity with an IC50 of 0.77 µmol/L by inhibiting reverse transcriptase (RT) RNA-dependent DNA polymerase activity through a direct binding. It had synergistic effects when combined with tenofovir/lamivudine or zidovudine/lamivudine. The pharmacodynamics properties of SG-1 render it a valuable lead for the development of novel NNRTIs.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Lignans / Reverse Transcriptase Inhibitors / Anti-HIV Agents / HIV Reverse Transcriptase Language: En Journal: J Asian Nat Prod Res Journal subject: BOTANICA / QUIMICA Year: 2019 Document type: Article Affiliation country: China
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Lignans / Reverse Transcriptase Inhibitors / Anti-HIV Agents / HIV Reverse Transcriptase Language: En Journal: J Asian Nat Prod Res Journal subject: BOTANICA / QUIMICA Year: 2019 Document type: Article Affiliation country: China