New alpha-lipoic acid ester(s) with antitumour and bio-surfactant activity - formulated as spontaneously dispersible concentrate with other surfactants, opt. contg. pharmaceutical or cosmetic active ingredients

摘要

Lipoic acid esters of formula (I) are new. Where, R1 = borneyl (endo-(1R or 1S)-1,7,7- trimethylbicyclo (2,2,1)heptan-2-yl); citronellyl; farnesyl; geranyl; menthyl ((1R,2S,5R or 1R,2S,5S)-2- isopropyl-5-methyl-cyclohexyl); myrtenyl; (iso)phytyl; thymyl or one of the gps. (II)=(VI); (dotted lines all single or all double; R2-R4=H or Me. Also new are spontaneously dispersible concentrates contg. (I). USE/ADVANTAGE - (I) have antitumour and biosurfactant activities, i.e. they can be used to prepare dispersible concentrates contg. pharmaceutical and cosmetic active ingredients. (I) are better co-surfactants for concentrate prepn. then known cpds. The concentrates when mixed with water form microemulsions of excellent phase stability and good permeation and spreading properties. They form micelles of radius 1.2-2.4 mm which penetrate the plasma membrane of tumour cells easily by a diffusion process independent of cellular metabolism.