Comparative pharmacokinetic study of two boswellic acids in normal and arthritic rat plasma after oral administration of Boswellia serrata extract or Huo Luo Xiao Ling Dan by LC‐MS

Abstract

Huo Luo Xiao Ling Dan (HLXLD), a Chinese herbal formula composed of 11 different herbs, has been used traditionally for the treatment of arthritis and other chronic inflammatory diseases. However, the pharmacokinetic profile of its anti-inflammatory bioactive compounds has not been elucidated. Boswellic acids are the bioactive compounds with potent anti-inflammatory activity isolated from Boswellia serrate which is one of the 11 herbs of HLXLD. The objective of the study was to compare the pharmacokinetics of the two bioactive bowsellic acids: 11-keto-β-boswellic acid and 3-O-acetyl-11-keto-β-boswellic following oral administration of HLXLD or Boswellia serrata extract alone in normal and arthritic rats. An LC-MS method was developed and validated for the determination of 11-keto-β-boswellic acid and 3-O-acetyl-11-keto-β-boswellic in the comparative pharmacokinetic study. The results showed that there were significant differences in pharmacokinetic parameters between normal and arthritic groups. Interestingly, the absorptions of two boswellic acids were significantly higher in HLXLD than Boswellia serrata extract alone, indicating the synergistic effect of other herbal ingredients in HLXLD. This comparative pharmacokinetic study provided direct evidence supporting the notion that the efficacy of a complex mixture such as HLXLD is better than that of single components in treating human diseases.

Simultaneous determination of three flavonoids and one coumarin by LC–MS/MS: Application to a comparative pharmacokinetic study in normal and arthritic rats after oral administration of Daphne genkwa extract

“…Twelve rats were randomly divided into two groups ( n = 6 per group): a normal group administered D. genkwa extract and an arthritic model group administered D. genkwa extract. The arthritic group was injected by CFA as described previously (Wang et al, ). The arthritic and normal rats were injected with 100 μL of CFA and the same volume of saline once at the plantar surface of the left hind paw.…”

A liquid chromatography–tandem mass spectrometry method for the quantitation of actarit in rabbit plasma: application to pharmacokinetics and metabolic stability

“…Better recovery for ATR and IS (>85%) was obtained with MTBE. Since, the analyte and IS were weak acids, the addition of certain acids could make them unbounded from plasma proteins . Interestingly, addition of 2% acetic acid gave the best recovery for both ATR and IS when compared with those in the absence of acidifying agent.…”

Phytomedicine in Joint Disorders

“…The role of bioactive principles is revendicated by the boswellic acids [31,32], a family of pentacyclic triterpenes, among which the main contenders were, initially, 11-keto-β-boswellic acid and acetyl-11-keto-β-boswellic acid, considered to inhibit leukotriene synthesis by suppressing lipoxygenase-5 (LOX-5) [20,33]. Other mechanisms were also invoked such as suppression of NF-κB activation, reduction of the production of proinflammatory cytokines (TNF-α, IL-1, IL-2, IL-4, IL-6 and IFN-γ), and reduced cleavage of C3 into the active components C3a and C3b, hampering the activation of the classic path of the complement [34].…”