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An antitumor promoter from Moringa oleifera Lam.
Authors:Amelia P. Guevara   Carolyn Vargas   Hiromu Sakurai   Yasuhiro Fujiwara   Keiji Hashimoto   Takashi Maoka   Mutzuo Kozuka   Yoshohiro Ito   Harukuni Tokuda  Hoyoku Nishino
Affiliation:a Institute of Chemistry, College of Science, University of the Philippines, Diliman, Quezon City, Philippines;b Kyoto Pharmaceutical University, Misasagi, Yamashina-ku, Kyoto 607, Japan;c Research Institute for Production Development, Kyoto 606, Japan;d Department of Biochemistry, Kyoto Prefectural University of Medicine, Kawaramachi-hirokoji, Kamigyo-ku, Kyoto 602, Japan
Abstract:In the course of studies on the isolation of bioactive compounds from Philippine plants, the seeds of Moringa oleifera Lam. were examined and from the ethanol extract were isolated the new O-ethyl-4-(α-Image-rhamnosyloxy)benzyl carbamate (1) together with seven known compounds, 4(α-Image-rhamnosyloxy)-benzyl isothiocyanate (2), niazimicin (3), niazirin (4), β-sitosterol (5), glycerol-1-(9-octadecanoate) (6), 3-O-(6′-O-oleoyl-β-Image-glucopyranosyl)-β-sitosterol (7), and β-sitosterol-3-O-β-Image-glucopyranoside (8). Four of the isolates (2, 3, 7, and 8), which were obtained in relatively good yields, were tested for their potential antitumor promoting activity using an in vitro assay which tested their inhibitory effects on Epstein–Barr virus-early antigen (EBV-EA) activation in Raji cells induced by the tumor promoter, 12-O-tetradecanoyl-phorbol-13-acetate (TPA). All the tested compounds showed inhibitory activity against EBV-EA activation, with compounds 2, 3 and 8 having shown very significant activities. Based on the in vitro results, niazimicin (3) was further subjected to in vivo test and found to have potent antitumor promoting activity in the two-stage carcinogenesis in mouse skin using 7,12-dimethylbenz(a)anthracene (DMBA) as initiator and TPA as tumor promoter. From these results, niazimicin (3) is proposed to be a potent chemo-preventive agent in chemical carcinogenesis.
Keywords:Antitumor promoter   Two-stage carcinogenesis   Epstein–  Barr virus-early antigen activation   O-ethyl-4-(α  -  http://www.sciencedirect.com/cache/MiamiImageURL/B6T2D-3W789ND-8-B/0?wchp=dGLzVzz-zSkWz"   alt="  Image"   title="  Image"   style="  vertical-align:bottom"   border="  0"   height=11 width="  12"  />-rhamnosyloxy)benzyl carbamate   Moringa oleifera Lam.
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