2. Academic Validation
  3. Application of tandem biotransformation for biosynthesis of new pentacyclic triterpenoid derivatives with neuroprotective effect

Application of tandem biotransformation for biosynthesis of new pentacyclic triterpenoid derivatives with neuroprotective effect

  • Bioorg Med Chem Lett. 2020 Feb 15;30(4):126947. doi: 10.1016/j.bmcl.2019.126947.
Shao-Hua Xu 1,  Hai-Lan Chen 1,  Yong Fan 2,  Wei Xu 3,  Jian Zhang 4
Affiliations

Affiliations

  • 1 College of Pharmacy, Fujian University of Traditional Chinese Medicine, Fuzhou, Fujian 350122, China.
  • 2 Novo Nordisk Foundation Center for Basic Metabolic Research, Section of Metabolic Genetics, Faculty of Health and Medical Sciences, University of Copenhagen, Panum, Maersk Tower, Blegdamsvej 3B, Copenhagen N 2200, Denmark.
  • 3 College of Pharmacy, Fujian University of Traditional Chinese Medicine, Fuzhou, Fujian 350122, China. Electronic address: 2000017@fjtcm.edu.cn.
  • 4 State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, Jiangsu 210009, China. Electronic address: 1020071849@cpu.edu.cn.
PMID: 31924497 DOI: 10.1016/j.bmcl.2019.126947
Abstract

Tandem whole-cell biotransformation was applied successfully to deliver novel pentacyclic triterpenoid derivatives for the first time. In this process, the starting substrate oleanolic acid (1) was biotransformed into a hydroxylated metabolite 1a by Rhizopus chinensis CICC 40335 and then was further glycosylated to 1b by Bacillus subtilis ATCC 6633. Moreover, metabolite 1a was furtherly oxidized by Streptomyces griseus ATCC 13273 and generated two new derivatives as 1c and 1d. To validate the feasibility, tandem biotransformation of 18β-glycyrrhetinic acid (2) by R. chinensis and B. subtilis was also conducted and offered a glycosylated derivative (2c). Finally, the neuroprotective effects of the derivatives were assessed on neural injury PC12 cell model induced by cobalt chloride.

Keywords

Neuroprotective; Pentacyclic triterpenoid; Structural modification; Tandem biotransformation.

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