アスコルビン酸誘導体を用いた医薬品開発への可能性（特集『ビタミン誘導体による人工触媒系の開発および医療応用研究の最前線』 （第73回大会　シンポジウム））

田井 章博

doi:10.20632/vso.96.7_311

Ascorbic acid 2-glucoside (AA-2G) is a stable ascorbic acid (AsA) derivative approved as a quasi-drug principal ingredient in skin care and a food additive in Japan and is widely used in cosmetics and health foods. AA-2G is a provitamin C agent that exhibits vitamin C activity after its enzymatic hydrolysis to AsA by α-glucosidase. We have synthesized a series of lipophilic stable AsA derivatives (6-Acyl-AA-2G) having straight-acyl chains of varying carbon chain lengths from C₄ to C₁₈and branched-acyl chains of varying carbon chain lengths from C₆ to C₁₆ to improve the bioavailability of AA-2G and have indicated that 6-Acyl-AA-2G exerts usually known vitamin C functions efficiently in vitro and in vivo. Recently, we found that, unexpectedly, 6-Acyl-AA-2G having a straight-acyl chain per se had antiallergic activity based on its degranulation inhibitory action and that a 6-O-acyl AsA, an intermediate in the hydrolysis of 6-Acyl-AA-2G having a branched-acyl chain to AsA, showed a significant antitumor activity. More recently, we succeeded in creating AsA derivatives that exhibit a superior antiallergic effect. In this review, the author presents a possible drug development application for created AsA derivatives.

アスコルビン酸誘導体を用いた医薬品開発への可能性（特集『ビタミン誘導体による人工触媒系の開発および医療応用研究の最前線』（第73回大会　シンポジウム））

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アスコルビン酸誘導体を用いた医薬品開発への可能性（特集『ビタミン誘導体による人工触媒系の開発および医療応用研究の最前線』 （第73回大会 シンポジウム））