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An Intestine/Liver Microphysiological System for Drug Pharmacokinetic and Toxicological Assessment
Published on: December 3, 2020
Preventive effects of soyasapogenol B derivatives on liver injury in a concanavalin A-induced hepatitis model
Kazue Sasaki1, Nobuto Minowa, Hiroyuki Kuzuhara
1Medicinal Chemistry Research Laboratory, Pharmaceutical Research Department, Meiji Seika Kaisha, Ltd., 760 Morooka-cho, Yokohama 222-8567, Japan.
Abstract:
To shed light on the structure-activity relationship, various soyasapogenol B derivatives were synthesized and evaluated for preventive effects on liver injury in the concanavalin A (Con A)-induced hepatitis model in mice. Con A injection into mice induces some pathophysiology of human liver disease such as autoimmune or viral hepatitis. Two hydroxyl groups on the A ring of soyasapogenol B are required for amelioration of liver damage. Modification of the C-22 hydroxyl moiety with an acyloxy or alkyloxy group, or removal of the hydroxyl group, resulted in a greatly enhanced percentage of alleviation. Among the series of soyasapogenol B derivatives examined, six compounds exhibited preventive effects on liver damage.
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