Synthesis of water-soluble retinol derivatives by enzymatic method

摘要

Retinoids(vitamin A and derivatives) are of great commercial potentialin cosmetics and pharmaceuticals such as skin care products.However,the clinical effectiveness of these retionoids is limited by skin irritation,water insolubility,and except for retinylesters,extreme instability.In this paper,an enzymatic method for preparing water-soluble retionol derivatives catalyzed by immobilized lipase is described.The synthesis is based on a unique strategy of two-step enzymatic acylation.Among the different synthesized compounds,the most water-soluble are the disaccharide derivatives such as saccharose retinyl adipate (nonionic water-soluble retinol derivative) and the sodium salt of retinyl diacids such as retinyl succinate sodium salt (ionic water-soluble retinol derivative).