Article · Volume 19, Issue 3 · pp. 689–699

Obtaining Acid-sensitive Prosaikogenin F by Enzymatic Hydrolysis of Saikosaponin A

Yeting Zhu¹, Jiangsong Peng¹, Yaqin Zhao¹, Mengru Wu¹, Suping Chen¹, Jiali Shao¹, Xubo Wang², Guohua Xia¹, Yuping Shen¹

¹Department of Chinese Materia Medica and Pharmacy, School of Pharmacy, Jiangsu University, Jiangsu, China.
²Department of Chemical Engineering and Pharmaceutical Engineering, Changzhou Vocational Institute of Engineering, Jiangsu, China.

Abstract

Background: Prosaikogenin F (PSF) has stronger anti-cancer bioactivity than saikosaponin A (SSA), however, it was hardly isolated due to its trace amount in the raw material of Radix Bupleuri (RB). In addition, the active chemical constituent was unstable under acidic conditions owing to a 13,28-epoxy-ether moiety at the D ring of its aglycone.Objectives: This study was to develop an appropriate method for obtaining acid-sensitive PSF from SSA abundant in RB.Materials and Methods: Enzymatic hydrolysis was employed and snailase was selected due to its good hydrolysis performance under nearly neutral circumstances. Hydrolysis conditions were then optimized by one-factor-at-a-time experimentation before response surface methodology (RSM) by Box-Behnken Design (BBD).Results: The reaction system was constructed in Na2HPO4-NaH2PO4 buffer (pH 6.0) containing snailase/SSA (44:1) at 39°C, then the hydrolysis lasted for 12 h. Therefore, the highest conversion ratio of SSA was achieved at 100.0%.Conclusion: The newly proposed method is eco-friendly for obtaining acid-sensitive PSF, which lays a solid foundation for its development to be an anti-cancer new drug.

Keywords: Prosaikogenin F; saikosaponin A; one-factor-at-a-time experimentation; response surface methodology; enzymatic hydrolysis

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