Research progress on extraction, purification, biotransformation, pharmacological effects, toxicity, combined therapy...

Within the framework of traditional Chinese medicine, Bupleuri Radix (BR), distinguished by its bitter flavor and slightly cold properties, targets the liver and gallbladder meridians. It is traditionally used for liver soothing, depression alleviation, fever reduction, and the elevation of yang and qi. BR is a key component of traditional formulations such as Xiaochaihu Decoction and Xiaoyao Powder. Modern pharmacological investigations have identified saikosaponins as the principal active ingredients in BR, which exhibit a broad spectrum of therapeutic effects. However, current research on the pharmacology, toxicology, and development of new dosage forms for saikosaponins remains insufficient.

This review examined the detailed structure of saikosaponins and explored the current research progress in areas such as their extraction, purification, identification, biotransformation, pharmacological effects, toxicity, combination therapies, and new dosage form development. The review aims to provide a scientific foundation for future research and highlight knowledge gaps in these areas.

Data for this study were systematically gathered from various sources, including journal articles, books, and academic papers, using prominent databases such as Web of Science, ScienceDirect, Google Scholar, PubMed, SpringerLink, CNKI, VIP, and Wan Fang Data. Additional verification of species distribution and scientific names was performed using online resources like 'Flora of China,' 'Flora of the World,' and the 'Chinese Pharmacopoeia.' ChemDraw 20.0 software was employed to visualize the chemical composition.

The review summarized the most recent research on saikosaponins, focusing on extraction, purification, biotransformation, pharmacological effects, toxicity studies, combination therapies, and the development of new dosage forms. Over 130 saikosaponins have been isolated and characterized from BR in phytochemical studies. These saponins undergo glycosyl conversion through microbial or enzyme-catalyzed hydrolysis, thereby enhancing their pharmacological activity. Their effects include anti-inflammatory, antidepressant, antiepileptic, antitumor, and immune regulation properties. Despite these benefits, high doses of saikosaponins can induce toxicity, limiting their widespread clinical use.

This review visualized 132 saikosaponin structures for the first time, covering their extraction, purification, biotransformation, pharmacological effects, toxicity evaluation, combination therapies, and new dosage form development. Compared to existing literature, this review offers a more comprehensive perspective, emphasizing key biological activities, toxicity, and the development of new dosage forms while identifying challenges in this area. Additionally, this review explored the mechanisms underlying saikosaponins' effects and proposes optimizing dosage form design as a critical direction for future research.