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KMID : 0545120180280111876
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Journal of Microbiology and Biotechnology
2018 Volume.28 No. 11 p.1876 ~ p.1882
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Design, Synthesis and Evaluation of Pentacyclic Triterpenoids Similar to Glycyrrhetinic Acid Via Combination of Chemical and Microbial Modification as Glycogen Phosphorylases Inhibitor
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Zhu Yuyao
Zhang Jian
Huang Xiaode
Chen Bin
Qian Hua
Zhao Botao
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Abstract
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A series of pentacyclic triterpenoids similar to glycyrrhetinic acid were designed and synthesized via the combination of chemical modification and microbial catalysis. All products were screened for the glycogen phosphorylases inhibitory activities in vitro. Within this series of derivatives, compound 5 displayed good inhibitory activities with IC50 value of 27.7 μM, which is better than that of the other derivatives and glycyrrhetinic acid. Structure? activity relationship (SAR) analysis of these inhibitors was also discussed.
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KEYWORD
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Biocatalysis, glycyrrhetinic acid, oleanolic acid, Streptomyces griseus ATCC 13273, Aspergillus ochraceus CICC 40330
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