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首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Steroids from Commiphora mukul display antiproliferative effect against human prostate cancer PC3 cells via induction of apoptosis
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Steroids from Commiphora mukul display antiproliferative effect against human prostate cancer PC3 cells via induction of apoptosis

机译:来自Commiphora mukul的类固醇通过诱导细胞凋亡显示出对人前列腺癌PC3细胞的抗增殖作用

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摘要

Two new stigmastane-type steroids, stigmasta-5,22E-diene-3β,11α- diol (1) and stigmasta-5,22E-diene-3β,7α,11α-triol (2), together with eight known compounds, were isolated from the resinous exudates of Commiphora mukul. Their structures were established by extensive analysis of their HR-MS, 1D- and 2D-NMR (COSY, HMQC, HMBC and NOESY) spectra. The isolates were evaluated for their antiproliferative activities against four human cancer cell lines. Compound 2 demonstrated inhibitory effects with IC 50 values of 5.21, 9.04, 10.94 and 16.56 μM, respectively, against K562, MCF-7, PC3 and DU145 human cancer cell lines. Further study showed that 2 was able to enforce the PC3 cell cycle arrest in the G2/M phase, and induce the apoptosis of PC3 cells by activation of Bax, caspases 3 and 9, and by inhibition of Bcl-2. It was also found that 1 inhibited proliferation of PC3 cells via G0/G1 phase arrest of the cell cycle.
机译:两种新的柱头甾烷类固醇stigmasta-5,22E-diene-3β,11α-二醇(1)和stigmasta-5,22E-diene-3β,7α,11α-三醇(2)以及八种已知化合物分离自Commiphora mukul的树脂状分泌物。通过对其HR-MS,1D和2D-NMR(COSY,HMQC,HMBC和NOESY)光谱进行广泛分析,确定了它们的结构。评价分离物对四种人类癌细胞系的抗增殖活性。化合物2表现出对K562,MCF-7,PC3和DU145人癌细胞系的抑制作用,IC 50值分别为5.21、9.04、10.94和16.56μM。进一步的研究表明2能够通过激活Bax,胱天蛋白酶3和9以及抑制Bcl-2来将PC3细胞周期阻滞在G2 / M期,并诱导PC3细胞凋亡。还发现1通过细胞周期的G0 / G1期阻滞抑制PC3细胞的增殖。

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