具有抗肿瘤促进活性的糖甘油脂类似物：异头构型的影响。

Glycoglycerolipid analogues active as anti-tumor-promoters: the influence of the anomeric configuration.

作者信息

Colombo D, Compostella F, Ronchetti F, Scala A, Toma L, Tokuda H, Nishino H

机构信息

Dipartimento di Chimica e Biochimica Medica, Università di Milano, Via Saldini 50, 20133, Milan, Italy.

出版信息

Eur J Med Chem. 2000 Dec;35(12):1109-13. doi: 10.1016/s0223-5234(00)01193-4.

DOI:10.1016/s0223-5234(00)01193-4

PMID:11248409

Abstract

The in vitro anti-tumor promoting effect of monohexanoates of 2-O-alpha-D-gluco- and galactopyranosyl-sn-glycerol on the 12-O-tetradecanoylphorbol-13-acetate (TPA) induced Epstein-Barr virus early antigen (EBV-EA) activation was evaluated and compared to the potencies of the corresponding beta-anomers. The results show that the inversion of the anomeric configuration from beta to alpha does not seem to significantly influence the activity, which is present, as for the beta-anomers, even at 1x10 mol ratio without any cytotoxicity.

摘要

评估了2-O-α-D-葡萄糖吡喃糖基和半乳糖吡喃糖基-sn-甘油单己酸酯对12-O-十四烷酰佛波醇-13-乙酸酯（TPA）诱导的爱泼斯坦-巴尔病毒早期抗原（EBV-EA）激活的体外抗肿瘤促进作用，并与相应β-异头物的效力进行了比较。结果表明，异头构型从β型转变为α型似乎不会显著影响活性，对于β-异头物而言，即使在1×10⁻⁵摩尔比时也存在这种活性，且没有任何细胞毒性。