Enzymatic synthesis of puerarin 6''-o-acetate
CN115433747BActive Publication Date: 2026-06-26INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
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Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Patents(China)
- Current Assignee / Owner
- INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
- Filing Date
- 2021-06-02
- Publication Date
- 2026-06-26
AI Technical Summary
Technical Problem
Puerarin has poor solubility and low bioavailability, making it difficult to achieve effective concentrations in oil and water-soluble systems, thus affecting clinical efficacy.
Method used
Using maltose-O-acyltransferase (MAT) as a catalyst and diacerein or acetyl-CoA as an acyl donor, puerarin 6″-O-acetate was synthesized via an enzymatic reaction. Specific reaction conditions included a temperature of 20–80 °C and a pH of 3–9.
Benefits of technology
This improved the lipid solubility and bioavailability of puerarin, achieved efficient and simple acylation modification, and reduced synthesis costs.
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Abstract
The application provides two enzymatic synthesis methods of puerarin 6''-O-acetate, and particularly relates to a method for synthesizing puerarin 6''-O-acetate by using maltose-O-acyltransferase (MAT) as a biological catalyst to catalyze puerarin and diacetylsis or acetyl coenzyme A, and belongs to the field of biological catalysis. After condition optimization and directional evolution of MAT, the conversion efficiency of mutants MAT-E125V, MAT-E125M and MAT-E125R to puerarin is increased from 68.10% to 94.03% at most by using diacetylsis as an acyl donor. The conversion efficiency of mutants MAT-E125N, MAT-E125T and MAT-E125P to puerarin is increased from 29.62% to 68.53% at most by using acetyl coenzyme A as an acyl donor.
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