Teruko Imai

TL;DR: The expression pattern of CES in Caco-2 cell monolayer, a useful in vitro model for rapid screening of human intestinal drug absorption, is completely different from that in human small intestine but very similar to human liver that expresses a much higher level of hCE-1 and lower level ofhCE-2.

TL;DR: Interestingly, propranolol derivatives, good substrates for hCE-2, were easily hydrolyzed by substitution of the methyl group on the 2-position of the acyl moiety, but were barely Hydrolyzed when the methyl Group was substituted on the 3-position, suggesting that hCE -2 does not easily form acylated intermediates because of conformational interference in its active site.

TL;DR: In conclusion, the esterase expression and hydrolyzing pattern of dog plasma were found to be closest to that of human plasma, and should be considered when selecting model animals for preclinical studies.

TL;DR: Findings indicate that human small intestine and liver show extensive hydrolase activity attributed to CES, which is different from that in species commonly used as experimental animals.

TL;DR: In this paper, the effects of the molecular weights of chitosan hydrolysates on the release and absorption rates of indomethacin from gel beads were examined.