Pharmacokinetics and oral bioavailability studies of three saikogenins in rats using a validated UFLC-MS/MS method

Radix Paeoniae Alba attenuates Radix Bupleuri-induced hepatotoxicity by modulating gut microbiota to alleviate the inhibition of saikosaponins on glutathione synthetase

“…As one of the main sites of drug metabolism, the intestine has important effects on drug absorption, metabolism, bioactivity, and toxicity [ 40 ]. It has been reported in the literature that saikosaponins are mainly transformed into the corresponding saikogenins by intestinal microflora with glycosidase activity [ 24 , 25 ]. Moreover, the quantitative analysis of saikosaponins and saikogenins in colon contents revealed that the main site of RPA-promoted conversion of saikosaponins to saikogenins occurs in the intestine ( Figs.…”

“…Therefore, it is speculated that intestinal microflora has a certain influence on RB-induced hepatotoxicity, suggesting that the difference in gut microbiota composition may be the potential reason for different people to have different tolerance to RB-induced hepatotoxicity. In addition, some scholars speculated that saikosaponins were converted into saikogenins by intestinal microflora before absorption and then exerted pharmacological effects [ [24] , [25] , [26] ]. Our previous studies showed that the combined use of RB and RPA could promote the conversion of saikosaponins to saikogenins in serum compared with RB alone [ 27 ].…”

Studies on the Changes of Pharmacokinetics Behaviors of Phytochemicals and the Influence on Endogenous Metabolites After the Combination of Radix Bupleuri and Radix Paeoniae Alba Based on Multi-Component Pharmacokinetics and Metabolomics

“…The saikogenin F, saikogenin G were deglycosylated metabolites of saikosaponin A and saikosaponin D transformed by intestinal bacteria in the gastrointestinal tract ( Shimizu et al, 1985 ). In addition, related studies speculated that saikosaponins, the main component of RB, was transformed into saikogenins by human intestinal flora, and then exerts pharmacological activity ( Liu et al, 2019 ). These research results indicated that compared to saikosaponin A and saikosaponin D, the pharmacological activity of saikogenin F and saikogenin G in the body may be more significant.…”

Saikosaponin D: review on the antitumour effects, toxicity and pharmacokinetics

“…Although the membrane permeability of SGs is improved compared with that of SSD, the bioavailability of SGs was found to be still low, and the efficacy of SSD might depend on the further transformation of secondary metabolites (Liu et al. 2019 ). The in vitro metabolism of SSD, as well as its two derivatives (PSG and SGG) in the gastrointestinal tract, was studied respectively in the liver microsomes of rats to explore their further metabolism after entering the circulatory system.…”