1. Academic Validation
  2. Pharmacokinetic study on bruceoside A revealed the potential role of quassinoid glycosides for the anticancer properties of Fructus Bruceae

Pharmacokinetic study on bruceoside A revealed the potential role of quassinoid glycosides for the anticancer properties of Fructus Bruceae

  • J Pharm Biomed Anal. 2019 Jun 5;170:264-272. doi: 10.1016/j.jpba.2019.03.052.
Yuan Xu 1 Mingming Xu 1 Lin Zhang 1 Zhenhua Zhu 1 Sheng Guo 1 Shulan Su 1 Jianming Guo 1 Chun-Tao Che 2 Zhi-Xiu Lin 3 Ming Zhao 4 Jin-Ao Duan 5
Affiliations

Affiliations

  • 1 Jiangsu Collaborative Innovation Center of Chinese Medicinal Resources Industrialization, National and Local Collaborative Engineering Center of Chinese Medicinal Resources Industrialization and Formulae Innovative Medicine, Nanjing University of Chinese Medicine, Nanjing, 210023, China.
  • 2 Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, Chicago, IL, 60612, United States.
  • 3 School of Chinese Medicine, Faculty of Medicine, The Chinese University of Hong Kong, Shatin, N.T., Hong Kong SAR, China.
  • 4 Jiangsu Collaborative Innovation Center of Chinese Medicinal Resources Industrialization, National and Local Collaborative Engineering Center of Chinese Medicinal Resources Industrialization and Formulae Innovative Medicine, Nanjing University of Chinese Medicine, Nanjing, 210023, China. Electronic address: mingzhao@njucm.edu.cn.
  • 5 Jiangsu Collaborative Innovation Center of Chinese Medicinal Resources Industrialization, National and Local Collaborative Engineering Center of Chinese Medicinal Resources Industrialization and Formulae Innovative Medicine, Nanjing University of Chinese Medicine, Nanjing, 210023, China. Electronic address: dja@njucm.edu.cn.
Abstract

Bruceoside A, an abundant quassinoid glycoside in Fructus Bruceae, was chosen for the pharmacokinetic study. It is the first case report on the pharmacokinetic study of quassinoid glycosides so far. A sensitive, accurate, and repeatable UHPLC-MS/MS method was developed for the determination of bruceoside A and its major metabolite. The results showed bruceoside A could be transformed into the potent Anticancer component brusatol in vivo, rather than its direct deglycosylated metabolite bruceosin. And the intestinal bacteria were proposed to take a potential role during such transformation. Based on the present study, it could be concluded that the quassinoid glycosides possessing weak activities in vitro could do contribution to the Anticancer properties of Fructus Bruceae in vivo via transforming into more active metabolites.

Keywords

Bruceoside A; Brusatol; Intestinal bacteria metabolism; Pharmacokinetic study; Quassinoid glycoside.

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