Simultaneous determination of eight bioactive components in Marsdenia tenacissima extract in rat plasma by LC–MS/MS and its application in a pharmacokinetic study

Abstract

As a traditional Chinese medicine, Marsdenia tenacissima (Roxb.) Wight et Arn. plays an indispensable role in clinical practice owing to its specific efficacy in treating malignant tumors, leukocythemia, cystitis and asthma. This study aimed to establish a novel and scientific LC-MS/MS approach to simultaneously determine tenacissoside B, H, G and I, caffeic acid, cryptochlorogenic acid, chlorogenic acid and neochlorogenic acid from M. tenacissima extract within the rat plasma samples. Digoxin was used as the internal reference. All determinations were carried out using the Eclipse Plus C 18 column, and water (containing 0.1% formic acid) was used as the mobile phase A, while acetonitrile was the mobile phase B for gradient elution. The UPLC methods were validated, including calibration curves, accuracy, precision, stability and recovery of the total eight analytes, in accordance with the requirements for biopharmaceutical analysis. Moreover, the proposed approach was also used in comprehensive pharmacokinetic research on those eight analytes in rats following M. tenacissima extract gavage. According to the pharmacokinetic parameters, tenacissoside B, I, H and G are the long-acting and primary bioactive constituents in M. tenacissima extract, with long mean residence times and high concentrations. Our findings shed light on the absorption mechanism and provide significant information for the clinical application of M. tenacissima.

Cryptochlorogenic acid and its metabolites ameliorate myocardial hypertrophy through a HIF1α-related pathway

“…20,21 Besides, caffeic acid widely exists in many traditional Chinese medicines, and caffeic acid reached a peak concentration generally at 0.16–0.6 h after the gavage of relevant traditional Chinese medicines. 22,23 According to our data, caffeic acid reached a peak concentration, which was significantly delayed to at 2 h, and this could be attributed to two major factors. On the one hand, caffeic acid was produced by the hydrolysis of 4-CQA in the intestine and then absorbed into the blood stream for a certain time.…”

Determination of Tenacissoside G, Tenacissoside H, and Tenacissoside I in Rat Plasma by UPLC-MS/MS and Their Pharmacokinetics

“…The oral bioavailability of the drug was low (2.6%), the elimination was faster, and the first-pass effect was obvious. Li established a LC-MS/MS method for simultaneous determination of garcinia extract in rat plasma samples of tenacissoside B, tenacissoside H, tenacissoside I, caffeic acid, cryptochlorogenic acid, chlorogenic acid, and neochlorogenic acid [ 16 ]. Digoxin was used as an internal standard reference.…”

“…Tese compounds contain a variety of aglycones with diferent structures [8,9], of which there are 6 main confguration aglycones. In vivo pharmacokinetics of tenacissoside H and tenacissoside I have been reported in literature [14][15][16], but bioavailability has not been reported.…”