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1,2,6-tri-O-galloyl-beta-D-glucopyranose inhibits gp41-mediated HIV envelope fusion with target cell membrane / 南方医科大学学报
Journal of Southern Medical University ; (12): 1127-1131, 2008.
Artigo em Chinês | WPRIM | ID: wpr-270195
ABSTRACT
<p><b>OBJECTIVE</b>To observe the inhibitory effect of 1,2,6-Tri-O-galloyl-beta-D-glucopyranose (TGGP) from Balanophora japonica Makino on human immunodeficiency virus (HIV) entry into the host cells and explore the mechanisms.</p><p><b>METHODS</b>TGGP was purified from Balanophora japonica Makino by n-hexane and ethyl acetate extraction and column chromatography. The inhibitory activity of TGGP on HIV gp41 six-helix bundle formation was measured with ELISA, N-PAGE and SE-HPLC, and the inhibitory effect of TGGP on HIV envelope grlycoprotein-induced cell-cell fusion was detected using a non-infectious cell-based assay.</p><p><b>RESULTS</b>TGGP inhibited HIV gp41 six-helix bundle formation, with an IC50 of 1.37-/+0.19 microg/ml as determined by ELISA, and this activity was further confirmed by N-PAGE and SE-HPLC. TGGP at 25 microg/ml significantly inhibited syncytium formation between the effector (CHO-WT) and the target (MT-2) cells.</p><p><b>CONCLUSION</b>The HIV transmembrane subunit gp41 mediates the entry of HIV into the target cells. TGGP can inhibit HIV fusion and entry into the target cells by inhibiting the formation of gp41 six-helix bundles, suggesting the potential of TGGP as a microbicide to prevent sexual transmission of HIV.</p>
Assuntos
Texto completo: DisponíveL Índice: WPRIM (Pacífico Ocidental) Assunto principal: Farmacologia / Proteína gp41 do Envelope de HIV / Membrana Celular / HIV-1 / Fármacos Anti-HIV / Inibidores da Fusão de HIV / Taninos Hidrolisáveis / Fusão de Membrana / Metabolismo Limite: Humanos Idioma: Chinês Revista: Journal of Southern Medical University Ano de publicação: 2008 Tipo de documento: Artigo

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Texto completo: DisponíveL Índice: WPRIM (Pacífico Ocidental) Assunto principal: Farmacologia / Proteína gp41 do Envelope de HIV / Membrana Celular / HIV-1 / Fármacos Anti-HIV / Inibidores da Fusão de HIV / Taninos Hidrolisáveis / Fusão de Membrana / Metabolismo Limite: Humanos Idioma: Chinês Revista: Journal of Southern Medical University Ano de publicação: 2008 Tipo de documento: Artigo