Cyr Louis, Langler Richard F, Crandall Ian, Lavigne Carole
Laboratoire de biologie cellulaire et de thérapie génique, Département de biologie, Moncton, Université de Moncton, Moncton, New Brunswick E1A 3E9, Canada.
Anticancer Res. 2007 May-Jun;27(3B):1437-48.
It has been well documented that some organosulfur compounds (OACs) show promise as anticancer agents.
The growth inhibitory effects of six novel different synthetic sulfonate esters was evaluated on cancerous (MCF-7) and non-cancerous (MCF-10A) human breast epithelial cells.
We found that the most active compounds against MCF-7 breast cancer cells had a common structure of p-methoxyphenyl p-toluenesulfonate with the methoxy substituent shifted from position 4 (22) to 2 (22o) or to 3 (22m). 3-Methoxyphenyl p-toluenesulfonate (22m) showed the lowest IC50 value (89.83 microM) on breast cancer cells but was also very active on non-cancerous MCF-10A cells (IC50 value of 53.96 microM). We found that compound 22 caused a greater degree of cell cycle arrest and induced apoptosis in cancerous MCF-7 cells compared with normal breast epithelial MCF-10A cells. However, compound 22m, was less selective by significantly arresting normal cells at G2/M-phase followed by a weak induction of apoptosis.
P-methoxyphenyl p-toluenesulfonate (22) appeared to be a more selective inhibitor of the growth of human breast cancer cells. Taken together, these results show that synthetic OSC compounds evaluated in this study can be effective antineoplastic agents and are worthy of further investigation.
有充分文献记载,一些有机硫化合物(OACs)有望成为抗癌剂。
评估了六种新型不同合成磺酸酯对人乳腺癌细胞(MCF - 7)和非癌细胞(MCF - 10A)的生长抑制作用。
我们发现,对MCF - 7乳腺癌细胞活性最强的化合物具有对甲氧基苯基对甲苯磺酸酯的共同结构,其中甲氧基取代基从4位(22)移至2位(22o)或3位(22m)。对甲苯磺酸3 - 甲氧基苯酯(22m)对乳腺癌细胞的IC50值最低(89.83 microM),但对非癌性MCF - 10A细胞也非常活跃(IC50值为53.96 microM)。我们发现,与正常乳腺上皮MCF - 10A细胞相比,化合物22在癌性MCF - 7细胞中引起更大程度的细胞周期停滞并诱导凋亡。然而,化合物22m的选择性较低,它能使正常细胞在G2/M期显著停滞,随后诱导较弱的凋亡。
对甲氧基苯基对甲苯磺酸酯(22)似乎是更具选择性的人乳腺癌细胞生长抑制剂。综上所述,这些结果表明本研究中评估的合成OSC化合物可能是有效的抗肿瘤剂,值得进一步研究。