From the traditional Chinese medicine plant Schisandra chinensis new scaffolds effective on HIV-1 reverse transcriptase resistant to non-nucleoside inhibitors

The Journal of Microbiology
Lijia XuEnzo Tramontano

Abstract

HIV-1 reverse transcriptase (RT) is still an extremely attractive pharmaceutical target for the identification of new inhibitors possibly active on drug resistant strains. Medicinal plants are a rich source of chemical diversity and can be used to identify novel scaffolds to be further developed by chemical modifications. We investigated the ability of the main lignans from Schisandra chinensis (Turcz.) Baill. fruits, commonly used in Traditional Chinese Medicine, to affect HIV-1 RT functions. We purified 6 lignans from Schisandra chinensis fruits and assayed their effects on HIV-1 RT and viral replication. Among the S. chinensis fruit lignans, Schisandrin B and Deoxyschizandrin selectively inhibited the HIV-1 RT-associated DNA polymerase activity. Structure activity relationship revealed the importance of cyclooctadiene ring substituents for efficacy. In addition, Schisandrin B was also able to impair HIV-1 RT drug resistant mutants and the early phases of viral replication. We identified Schisandrin B and Deoxyschizandrin as new scaffold for the further development of novel HIV-1 RT inhibitors.

References

Feb 27, 2003·Antimicrobial Agents and Chemotherapy·Cristina ParolinGiorgio Palù
Jun 9, 2004·The International Journal of Biochemistry & Cell Biology·Robert A Domaoal, Lisa M Demeter
Oct 21, 2005·Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences·Meijuan XuLei Yue
Aug 5, 2006·Medicinal Research Reviews·Donglei YuKuo-Hsiung Lee
Dec 28, 2006·Journal of Natural Products·Min ChenDao-Feng Chen
Jun 3, 2008·Journal of Ethnopharmacology·Alexander Panossian, Georg Wikman
Jul 11, 2009·Science·Jesse W-H Li, John C Vederas
Jul 25, 2009·Nucleic Acids Research·Hiroshi NishidaTetsuya Konishi
Sep 30, 2009·Journal of Medicinal Chemistry·Youcef Mehellou, Erik De Clercq
Jun 1, 2010·Archives of Pharmacal Research·Wei-Lie XiaoHan-Dong Sun
Sep 23, 2010·Current Medicinal Chemistry·E Tramontano, R Di Santo
Feb 18, 2011·Zhongguo Zhong yao za zhi = Zhongguo zhongyao zazhi = China journal of Chinese materia medica·Jinglei Xiao, Dacheng Jiang
May 2, 2013·Evidence-based Complementary and Alternative Medicine : ECAM·Si-Yuan PanKam-Ming Ko
Nov 23, 2013·Future Medicinal Chemistry·Angela CoronaStuart F J Le Grice
Oct 1, 2011·Journal of Traditional and Complementary Medicine·Min-Hsiung PanChi-Tang Ho
Aug 6, 2014·Antimicrobial Agents and Chemotherapy·Angela CoronaEnzo Tramontano

❮ Previous
Next ❯

Citations

Jun 18, 2016·BioMed Research International·Maria Barbara PisanoFrancesca Pintus
Oct 22, 2016·Phytomedicine : International Journal of Phytotherapy and Phytopharmacology·Francesca EspositoEnzo Tramontano
Dec 20, 2016·Chembiochem : a European Journal of Chemical Biology·Riccardo MartiniMaurizio Botta
Jan 19, 2018·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Chi-Lin LiTung-Hu Tsai
Oct 3, 2017·Annual Review of Pharmacology and Toxicology·Asmaa Boufridi, Ronald J Quinn
Jan 16, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Wei FengXin-Guo Wang
Jul 16, 2017·BMC Microbiology·Amalia Di PetrilloAldo Frau
Jul 11, 2018·International Journal of Molecular Sciences·Minyu ZhangHongjun Yang
Mar 11, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Jenny DesantisOriana Tabarrini
Mar 8, 2016·Chembiochem : a European Journal of Chemical Biology·Cristina TintoriMaurizio Botta
Jan 8, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Qinghua CuiLijun Rong
Sep 12, 2015·Chembiochem : a European Journal of Chemical Biology·Francesca EspositoEnzo Tramontano
Apr 10, 2021·Drug Design, Development and Therapy·Huihui TiShumei Wang
May 20, 2021·Archiv der Pharmazie·Angela CoronaEnzo Tramontano

❮ Previous
Next ❯

Related Concepts

Related Feeds

Antimicrobial Resistance

Antimicrobial resistance poses a significant threat to the continued successful use of antimicrobial agents for the treatment of bacterial infections.

Antimicrobial Resistance (ASM)

Antimicrobial resistance poses a significant threat to the continued successful use of antimicrobial agents for the treatment of bacterial infections.

© 2022 Meta ULC. All rights reserved