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

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Isopimarane diterpenoids from Kaempferia pulchra rhizomes collected in Myanmar and their Vpr inhibitory activity

http://hdl.handle.net/20.500.12678/0000002142

Publication type
		Journal article
Upload type
		Publication
Title
	Title	Isopimarane diterpenoids from Kaempferia pulchra rhizomes collected in Myanmar and their Vpr inhibitory activity
	Language	en
Publication date		2016
Authors
		Nwet Nwet Win
		Ito, Takuya
		Matsui, Takashi
		Aimaiti, Simayijiang
		Kodama, Takeshi
		Hla Ngwe
		Okamoto, Yasuko
		Tanaka, Masami
		Asakawa, Yoshinori
		Abe, Ikuro
		Morita, Hiroyuki
Description
		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.
Keywords
		Kaempferia pulchra
Identifier		http://uyr.uy.edu.mm/handle/123456789/124
Journal articles
Conference papaers
Books/reports/chapters
Thesis/dissertations