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Lijia Xu,Nicole Grandi,Claudia Del Vecchio,Daniela Mandas,Angela Corona,Dario Piano,Francesca Esposito,Cristina Parolin,Enzo Tramontano 한국미생물학회 2015 The journal of microbiology Vol.53 No.4
HIV-1 reverse transcriptase (RT) is still an extremely attractivepharmaceutical target for the identification of new inhibitorspossibly active on drug resistant strains. Medicinalplants are a rich source of chemical diversity and can be usedto identify novel scaffolds to be further developed by chemicalmodifications. We investigated the ability of the main lignansfrom Schisandra chinensis (Turcz.) Baill. fruits, commonlyused in Traditional Chinese Medicine, to affect HIV-1 RTfunctions. We purified 6 lignans from Schisandra chinensisfruits and assayed their effects on HIV-1 RT and viral replication. Among the S. chinensis fruit lignans, Schisandrin Band Deoxyschizandrin selectively inhibited the HIV-1 RTassociatedDNA polymerase activity. Structure activity relationshiprevealed the importance of cyclooctadiene ring substituentsfor efficacy. In addition, Schisandrin B was also ableto impair HIV-1 RT drug resistant mutants and the earlyphases of viral replication. We identified Schisandrin B andDeoxyschizandrin as new scaffold for the further developmentof novel HIV-1 RT inhibitors.