Research progress on the puerarin derivatization through biocatalysis
10.16438/j.0513-4870.2020-0308
- VernacularTitle:生物催化介导的葛根素衍生化研究进展
- Author:
Xue-ning WANG
1
;
Jian-qiang KONG
1
Author Information
1. State Key Laboratory of Bioactive Substance and Function of Natural Medicines and NHC Key Laboratory of Biosynthesis of Natural Products, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
- Publication Type:Research Article
- Keywords:
puerarin;
biocatalysis;
structure modification;
bioavailability;
solubility
- From:
Acta Pharmaceutica Sinica
2020;55(7):1590-1603
- CountryChina
- Language:Chinese
-
Abstract:
Puerarin, also known as daidzein 8-C-glucoside, is a major isoflavone glycoside from Pueraria lobata. Puerarin has been shown to possess a variety of pharmacological activities. It has been widely used for the treatment of cardiovascular and cerebrovascular diseases. However, the further applications are limited due to its low water solubility and poor bioavailability. Structural modification is thus regarded as an efficient approach to improve the solubility and bioavailability of puerarin. Unlike chemical modifications, enzyme-assisted modifications, namely biocatalysis, is a promising alternative for the regioselective synthesis of puerarin derivatives due to its high selectivity. Up to date, acylation, glycosylation and hydroxylation of puerarin had been achieved through enzyme-based biocatalysis. Diverse active puerarin derivatives with improved solubility and bioavailability have been thus developed. Based on modification groups, this paper focused on the progress in the preparation of puerarin derivatives by biocatalysis, in which the whole-cells or pure enzymes were used as the biocatalysts. This article was expected to provide new ideas for the synthesis and development of puerarin drugs.
