The mode of action of primary bile salts on human platelets.

Cholate and its conjugated amide derivatives glycocholate and taurocholate solubilized human platelets differently as studied by the observations on: (1) the change in optical absorbance of platelet suspension, (2) marker leakiness and (3) component solubility. Cholate ruptures the membrane in an all-or-none process, while both conjugated derivatives shed off both proteins and lipids. The shed lipids formed vesicles and could be separated from the proteins. The conjugated salts gradually chop off the cell membrane into pieces causing the cells to become small spheres (1.5 microns in diameter) as revealed by scanning electron microscopy, which also revealed that morphological change of platelet in these bile salts depended on both concentration and incubation period. Platelets at the prelytic-stage concentration of these three salts deformed initially to spiculate disc and finally to a stretched-out flat form. Also, in the prelytic stage of these bile salts, platelets showed inhibited responses to thrombin which did not happen to platelets in deoxycholate (Shiao et al. (1989) Biochim. Biophys. Acta 980, 56-68.).