2026-04-15T03:18:04Z https://meral.edu.mm/oai

oai:meral.edu.mm:recid/2142 2021-12-13T03:48:59Z 1582963390870:1582967633684 user-uy

Isopimarane diterpenoids from Kaempferia pulchra rhizomes collected in Myanmar and their Vpr inhibitory activity Nwet Nwet Win Ito, Takuya Matsui, Takashi Aimaiti, Simayijiang Kodama, Takeshi Hla Ngwe Okamoto, Yasuko Tanaka, Masami Asakawa, Yoshinori Abe, Ikuro Morita, Hiroyuki Viral protein R (Vpr), an accessory gene of HIV-1, plays important roles in viral pathogenesis. Screening of Myanmar medicinal plants that are popular as primary treatments for HIV/AIDS and for HIV-related problems revealed the potent anti-Vpr activity of the CHCl3-soluble extract of Kaempferia pulchra rhizomes, in comparison with that of the positive control, damnacanthal. Fractionation of the active CHCl3-soluble extract led to the identification of 30 isopimarane diterpenoids, including kaempulchraols A–W (1–23). All isolates were assayed for anti-Vpr activity against TREx-HeLa-Vpr cells, in which Vpr expression is tightly regulated by tetracycline. Kaempulchraols B (2), D (4), G (7), Q (17), T (20), U (21), and W (23) exhibited potent anti-Vpr activity, at concentrations ranging from 1.56 to 6.25 lM. The structure–activity relationships of the active kaempulchraols suggested that the presence of a hydroxy group at C-14 in an isopimara-8(9),15-diene skeleton and the presence of an acetoxy group at C-1 or C-7 in an isopimara-8(14),15-diene skeleton are the critical factors for the inhibitory effects against TREx-HeLa-Vpr cells. 2016 http://hdl.handle.net/20.500.12678/0000002142 https://meral.edu.mm/records/2142