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Separation and Cytotoxicity of Enzymatic Transformed Prosaikogenins from Bupleurum falcatum.

Hyejin Ko^1,2, Kyoung Jin Lee¹, Kwangho Song^1,3

¹College of Pharmacy, Natural Products Research Institute, Seoul National University, Seoul, Republic of Korea.

|June 10, 2025

Summary

This summary is machine-generated.

Enzymatic modification of saikosaponins improved their properties for drug development. Prosaikogenin G showed potent anticancer activity with low toxicity, highlighting its therapeutic potential.

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Area of Science:

Natural Product Chemistry
Biotechnology
Pharmacology

Background:

Saikosaponins from *Bupleurum falcatum* have limited use due to poor bioavailability and separation challenges.
Efficient methods are needed to enhance saikosaponin applications in pharmaceuticals.

Purpose of the Study:

To develop an efficient enzymatic and chromatographic strategy for saikosaponin derivative separation.
To evaluate the anticancer potential of isolated saikosaponin derivatives.

Main Methods:

Enzymatic deglycosylation of saikosaponins using cellulase and *α*-L-rhamnosidase.
Separation of lipophilic prosaikogenins via countercurrent chromatography (CCC) and preparative HPLC.
Anticancer activity screening against various cancer cell lines (MDA-MB-468, HepG2, HCT116) and normal cells.

Main Results:

Lipophilic prosaikogenins were produced through enzymatic transformation.
Four prosaikogenins (F, G, E1, E3) were successfully isolated using CCC and HPLC.
Prosaikogenin G exhibited significant anticancer activity and low toxicity in normal cells.

Conclusions:

The combined enzymatic and CCC approach provides an efficient method for saikosaponin derivative separation.
Prosaikogenin G is a promising candidate for anticancer drug development.
This strategy facilitates the pharmaceutical development of saikosaponin-based therapeutics.