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Kim, Young Ho,Park, Eun Jung,Park, Mi Hyun,Badarch, Uranchimeg,Woldemichael, Girma Moges,Beutler, John Albert Pharmaceutical Society of Japan 2006 Biological & pharmaceutical bulletin Vol.29 No.10
<P>In a search for natural product inhibitors of hypoxia inducible factor-1 (HIF-1) function, crinamine (1), a crinane type alkaloid, showed potent dose dependent inhibition (IC<SUB>50</SUB>=2.7 μ<SMALL>M</SMALL>) of HIF-1α in a cell-based reporter gene assay. Crinamine (1) was isolated from the aerial parts of <I>Crinum asiaticum</I> var. <I>japonicum</I> together with lycorine (2), norgalanthamine (3) and epinorgalanthamine (4). The other components (2—4) showed no significant inhibition of HIF-1α induced transcriptional activity.</P>
Tai, Bui Huu,Nhut, Nguyen Duy,Nhiem, Nguyen Xuan,Quang, Tran Hong,Thanh Ngan, Nguyen Thi,Thuy Luyen, Bui Thi,Huong, Tran Thu,Wilson, Jennifer,Beutler, John A.,Ban, Ninh Khac,Cuong, Nguyen Manh,Kim, Yo Informa Healthcare 2011 PHARMACEUTICAL BIOLOGY Vol.49 No.10
<P><I>Context</I>: Acquired immune deficiency syndrome (AIDS) is a severe pandemic disease especially prevalent in poor and developing countries. Thus, developing specific, potent antiviral drugs that restrain infection by human immunodeficiency virus type 1 (HIV-1), a major cause of AIDS, remains an urgent priority.</P><P><I>Objective</I>: This study evaluated 32 extracts and 23 compounds from Vietnamese medicinal plants for their inhibitory effects against HIV-1 ribonuclease H (RNase H) and their role in reversing the cytopathic effects of HIV.</P><P><I>Materials and methods</I>: The plants were air-dried and extracted in different solvent systems to produce plant extracts. Natural compounds were obtained as previously published. Samples were screened for RNase H inhibition followed by a cytopathic assay. Data were analyzed using the Microsoft Excel.</P><P><I>Results and discussion</I>: At 50 μg/mL, 11 plant extracts and five compounds inhibited over 90% of RNase H enzymatic activity. Methanol extracts from <I>Phyllanthus reticulatus</I> and <I>Aglaia aphanamixis</I> leaves inhibited RNase H activity by 99 and 98%, respectively, whereas four extracts showed modest protection against the cytopathic effects of HIV.</P><P><I>Conclusion</I>: The screening results demonstrated that the butanol (BuOH) extract of <I>Celastrus orbiculata</I> leaves, methanol (MeOH) extracts of <I>Glycosmis stenocarpa</I> stems, <I>Eurya ciliata</I> leaves, and especially <I>P. reticulatus</I> leaves showed potential RNase H inhibition and protection against the viral cytopathic effects of HIV-1. Further chemical investigations should be carried out to find the active components of these extracts and compounds as potential anti-HIV drug candidates.</P>