KMID : 0043320090320121727
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Archives of Pharmacal Research 2009 Volume.32 No. 12 p.1727 ~ p.1736
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Apoptosis of Human Burkitt¡¯s Lymphoma Cells Induced by 2-N,NDiethylaminocarbonyloxymethyl-1-diphenylmethyl-4-(3,4,5-trimethoxybenzoyl) piperazine Hydrochloride (PMS-1077)
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Wang Qin
Wang Wen-di Xu Xi-ming Chen Ying Jiang Peng Dong Chang-zhi
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Abstract
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Piperazine is one of the heterocycles which are associated with diverse pharmacological activities. 2-N,N-Diethylaminocarbonyloxymethyl-1-diphenylmethyl-4-(3,4,5-trimethoxybenzoyl) piperazine hydrochloride (PMS-1077) is a trisubstituted piperazine which contains a trimethoxybenzene ring and a benzhydrylpiperazine fragment, both of which can induce cell proliferation regression by different mechanisms. We have therefore examined the effects of PMS-1077 on Human Burkitt¡¯s lymphoma cells (Raji). The viability of Raji cells was determined by MTT assay and also assessed by trypan blue dye exclusion method. The results demonstrate that PMS-1077 can suppress the proliferation of Raji cells in a dose- and timedependent manner, while inhibit colony formation ability of Raji cells merely in a dose-dependent manner in vitro. Meanwhile, morphological changes were observed using fluorescence microscope. Flow cytometric analysis through PI stains showed that PMS-1077 blocked the growth of Raji cells in the G0/G1 period, and induced apoptosis of Raji cells after 48 h of incubation. Cell apoptosis induced by PMS-1077 was further confirmed by staining with Annexin-V FITC and PI. Preliminary study by molecular docking suggests that PMS-1077 may inhibit tubulin polymerization. More experiments are in progress in our laboratory to reveal the mode of action of PMS-1077 in the induction of apoptosis of Raji cells.
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KEYWORD
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2-N, N-Diethylaminocarbonyloxymethyl-1-diphenylmethyl-4-(3, 4, 5-trimethoxybenzoyl) piperazine hydrochloride (PMS-1077), Apoptosis, Human Burkitt¡¯s lymphoma (Raji), Antiproliferative activity, Tubulin
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