Production of Minor Ginsenoside CK from Major Ginsenosides by Biotransformation and Its Advances in Targeted Delivery to Tumor Tissues Using Nanoformulations

Abstract

For over 2000 years, ginseng (roots of Panax ginseng C.A. Meyer) has been used as a traditional herbal medicine. Ginsenosides are bioactive compounds present in ginseng responsible for the pharmacological effects and curing various acute diseases as well as chronic diseases including cardiovascular disease, cancer and diabetes. Structurally, ginsenosides consist of a hydrophobic aglycone moiety fused with one to four hydrophilic glycoside moieties. Based on the position of sugar units and their abundance, ginsenosides are classified into major and minor ginsenosides. Despite the great potential of ginsenosides, major ginsenosides are poorly absorbed in the blood circulation, resulting in poor bioavailability. Interestingly, owing to their small molecular weight, minor ginsenosides exhibit good permeability across cell membranes and bioavailability. However, extremely small quantities of minor ginsenosides extracted from ginseng plants cannot fulfill the requirement of scientific and clinical studies. Therefore, the production of minor ginsenosides in mass production is a topic of interest. In addition, their poor solubility and lack of targetability to tumor tissues limits their application in cancer therapy. In this review, various methods used for the transformation of major ginsenosides to minor ginsenoside compound K (CK) are summarized. For the production of CK, various transformation methods apply to major ginsenosides. The challenges present in these transformations and future research directions for producing bulk quantities of minor ginsenosides are discussed. Furthermore, attention is also paid to the utilization of nanoformulation technology to improve the bioavailability of minor ginsenoside CK.

Self-assembled nanodrug delivery systems for anti-cancer drugs from traditional Chinese medicine

“…Ginsenosides. Ginsenosides (GSs) are a group of ginseng-derived compounds 179 with bioactivities against diabetes, cancer, depression, cerebral ischemia, endothelial cell injury, and cardiovascular diseases among others. 180 Ginsenosides are used extensively in the development of anticancer drugs given that they have been shown to reduce multidrug resistance and improve the anti-tumor effect through synergy with other drugs.…”

β-Glucosidase and Its Application in Bioconversion of Ginsenosides in Panax ginseng

“…The identification and isolation of bacterial endophytes from P. ginseng and P. notoginseng have provided novel sources of both major and minor ginsenosides, with the latter based on β-glucosidase activity [ 9 ]. The major goals in practical application are mass production and nanoparticle preparation of minor ginsenosides with large pharmacological effects [ 96 , 97 ]. Novel forms of minor ginsenosides may have enormous promise as therapeutic agents [ 96 ].…”

“…Novel forms of minor ginsenosides may have enormous promise as therapeutic agents [ 96 ]. Functionalization or loading of minor ginsenosides onto biocompatible polymers and nanoformulations improved the solubilization and absorption of ginsenosides for clinical applications such as cancer therapy [ 97 ].…”

Ginsenoside CK inhibits androgenetic alopecia by regulating Wnt/β‐catenin and p53 signaling pathways in AGA mice

“…( P. ginseng ) is a traditional herb, the main ingredient of which is ginsenoside. Among many ginsenoside monomers, ginsenoside CK is a rare ginsenoside transformed from ginsenoside Rb1 (Jiang et al., 2021; Murugesan et al., 2022). Previous studies have shown that ginsenoside Rb1 can improve hair loss (Jeong et al., 2022; Shin et al., 2014; Zhang et al., 2019; Zheng et al., 2013).…”