Highly Selective Bioconversion of Ginsenoside Rb1 to Compound K by the Mycelium of Cordyceps sinensis under Optimized Conditions

Abstract

Compound K (CK), a highly active and bioavailable derivative obtained from protopanaxadiol ginsenosides, displays a wide variety of pharmacological properties, especially antitumor activity. However, the inadequacy of natural sources limits its application in the pharmaceutical industry. In this study, we firstly discovered that Cordyceps sinensis was a potent biocatalyst for the biotransformation of ginsenoside Rb1 into CK. After a series of investigations on the biotransformation parameters, an optimal composition of the biotransformation culture was found to be lactose, soybean powder and MgSO4 without controlling the pH. Also, an optimum temperature of 30 °C for the biotransformation process was suggested in a range of 25 °C-50 °C. Then, a biotransformation pathway of Rb1 → Rd → F2 → CK was established using high performance liquid chromatography/quadrupole time-of-flight mass spectrometry (HPLC-Q-TOF-MS). Our results demonstrated that the molar bioconversion rate of Rb1 to CK was more than 82% and the purity of CK produced by C. sinensis under the optimized conditions was more than 91%. In conclusion, the combination of C. sinensis and the optimized conditions is applicable for the industrial preparation of CK for medicinal purposes.

Screening and characterization of a salt-tolerant aflatoxin B1-degrading strain isolated from Doubanjiang, a Chinese typical red pepper paste

“…The addition of beef extract, yeast extract, peptone and tryptone resulted in the degradation rate of AFB 1 to 74.85 ± 0.13%, 78.51 ± 0.96%, 73.9 ± 0.38%, and 80.56 ± 0.13%, respectively. Carbon is the key nutrient for microbial growth and energy metabolism, and nitrogen is an important component of proteins and nucleic acids (Wang et al, 2015). This result was in contrast to the findings of Mwakinyali et al (2019), who reported that adding carbon or nitrogen can increase the degradation rate of Myroides odoratimimus strain 3J2MO on AFB 1 .…”

Biotransformation of ginsenoside Rb1 with wild Cordyceps sinensis and Ascomycota sp. and its antihyperlipidemic effects on the diet‐induced cholesterol of zebrafish

“…As a biological hybrid of the larva and parasitic fungus, C. sinensis contains a complex enzymatic system and abundant ingredients with medicinal value (Chen et al, 2017; Hu et al, 2015; Zhong & Xiao, 2009). Several clinical trials regarding the transformation characteristics of C. sinensis have been published (Wang et al, 2015). However, Cordyceps militaris and Panax ginseng (cultivated ginseng, less than 5 years) had been confirmed as new resource food raw materials since 2009 and 2012 respectively, which can be directly used in food production.…”

Functional Regulation of Ginsenosides on Myeloid Immunosuppressive Cells in the Tumor Microenvironment

“…Fruitful proceedings have been accomplished through our research, including the establishment and optimization of biotransformation methods for the ample supply of some rare saponins, the discovery and elucidation on new saponin structures that provide potential anticancer agents, and others (Table1). [26][27][28] We also found that several rare or new ginsenosides enhance antitumor immune response in the tumor microenvironment, 25,26 and unpublished data, which will provide some novel medical products for clinical use of ginsenosides.…”