Search

Objective: To explore the hypolipidemic activity and toxic side effect of lansiumamide B (LB) from chicken-heart shaped wampee (Clausena lansium) seeds in C57BL/6J mice fed on a high-fat-diet (HFD) model. Methods: The no observed adverse effect level (NOAEL) of LB in mice was assessed by oral acute toxicity test. HFD-fed mice were intragastrically administered with LB at 1/100, 1/50 and 1/25 NOAEL for 4 weeks. To evaluate the lipid-lowering activity of LB, body mass, serum lipids, insulin resistance, and oxidative stress indicators were measured. Results: The NOAEL of LB was 2 g/kg mb. LB significantly reduced body mass in HFD-fed mice. Compared with the HFD model group, body mass decreased by 15.51% and Lee’s index declined by 3.25% in the high-dose LB group; the concentration of high-density lipid-cholesterol (HDL-C) increased by 38.04%, and the activities of superoxide dismutase (SOD), glutathione peroxidase (GSH-Px) and catalase (CAT) in the serum increased by 41.86%, 41.95%, and 105.50%, respectively. Conclusion: LB within the NOAEL range has significant lipid-lowering activity in mice without obvious toxicity.

6-Gingerol is the major pungent component in ginger. It possesses a variety of health benefits including antitumor, anti-inflammatory and antioxidant, hypoglycemic, hypolipidemic and hypotensive activities as well as colitis prevention and treatment. However, the health effects of oral 6-gingerol are limited due to the low water solubility, poor gastrointestinal stability, rapid metabolism in the body, release at non-target sites, and pungent and bitter taste. In this article, the health effects of 6-gingerol including anticancer, anti-inflammatory and hypolipidemic activity, and preventing and treating cardiovascular and cerebrovascular diseases as well as gastrointestinal diseases are reviewed together with the underlying mechanisms. Based on a review of recent progress in the research on the gastrointestinal absorption of 6-gingerol, its distribution, metabolism and excretion in the systematic circulation and its metabolic processes in the upper and lower gastrointestinal tract, the current status of the design and development of oral delivery systems for 6-gingerol. The mechanism for the enhancing effect of delivery systems on the health benefits of 6-gingerol and the design principle of the strategies to enhance the health benefits of 6-gingerol are elucidated. Hopefully, this review will not only provide a theoretical guidance for the design of oral delivery systems for 6-gingerol and the research on the mechanism for the enhancing effect of oral delivery systems on the health benefits of 6-gingerol, but also provide scientific evidence for the design of 6-gingerol-based functional foods.

1-(4-(Pyrrolidin-1-yl-methyl)phenyl)-3-(4-((3-(trifluoromethyl) phenyl)amino)quinazolin-6-yl)urea (ZCJ14), a novel epidermal growth factor receptor (EGFR) inhibitor, with diarylurea moiety, displays anticancer effect. In the present study, an LCMS/MS method was established to determine the concentration of ZCJ14 in rat plasma. Furthermore, the method was applied to investigate the pharmacokinetic characteristics of ZCJ14. Chromatographic separation of ZCJ14 and internal standard (IS) [1-phenyl-3-(4-((3-(trifluoromethyl)phenyl)amino) quinazolin-6-yl)urea] was accomplished by gradient elution using the Kromasil C18 column. The selected reaction monitoring transitions were performed at m/z 507.24→436.18 and 424.13→330.96 for ZCJ14 and IS, resp. The established method was linear over the concentration range of 10–1000 ng mL−1. The intra- and inter-day precisions were < 11.0 % (except for LLOQ which was up to 14.3 %) and the respective accuracies were within the range of 87.5–99.0 %. The extraction recovery and matrix effect were within the range of 88.4–104.5 % and 87.3–109.9 %, resp. ZCJ14 was stable under all storage conditions. The validated method was successfully applied to the pharmacokinetic study of ZCJ14 in rats, and the pharmacokinetic parameters have been determined. The oral bioavailability of ZCJ14 was found to be 46.1 %. Overall, this accurate and reliable quantification method might be useful for other diarylurea moiety-containing drugs.