Context: Cepharanthine (CPA) has been reported to possess a wide range of pharmacological activities.Objective: This study investigates the pharmacokinetic characteristics after oral or intravenous administration of CPA by using a sensitive and rapid LC–MS/MS method.Materials and methods: A sensitive and rapid LC–MS/MS method was developed for the determination of CPA in Sprague–Dawley rat plasma. Twelve rats were equally randomized into two groups, including the intravenous group (1 mg/kg) and the oral group (10 mg/kg). Blood samples (250 μL) were collected at designated time points and determined using this method. The pharmacokinetic parameters were calculated.Results: The calibration curve was linear within the range of 0.1–200 ng/mL (r = 0.999) with the lower limit of quantification at 0.1 ng/mL. After 1 mg/kg intravenous injection, the concentration of CPA reached a maximum of 153.17 ± 16.18 ng/mL and the t1/2 was 6.76 ± 1.21 h. After oral administration of 10 mg/kg of CPA, CPA was not readily absorbed and reached Cmax 46.89 ± 5.25 ng/mL at approximately 2.67 h. The t1/2 was 11.02 ± 1.32 h. The absolute bioavailability of CPA by oral route was 5.65 ± 0.35%, and the bioavailability was poor.Discussion and conclusions: The results indicate that the bioavailability of CPA was poor in rats, and further research should be conducted to investigate the reason for its poor bioavailability and address this problem.
Acute stress induces tissue damage through excessive cellular apoptosis. In our study, the effects of sesamin on apoptosis and wound healing were investigated. The angiogenesis effect of sesamin was evaluated by the abilities of adherence, migration and tube formation in human umbilical vein endothelial cells (HUVECs). Our data demonstrated that treatment with sesamin dose-dependently promoted the proliferation, adherence, migration and enhanced their angiogenic ability in vitro. Moreover, the increased apoptosis in HUVECs, which stimulated by tert-butyl hydroperoxide (TBHP) was significantly attenuated by the sesamin treatment. Furthermore, we revealed that neogenesis of granulation tissue and deposition and remodeling of the collagen matrix were accelerated by the administration of sesamin in our in vivo study. These results confirm that sesamin accelerates wound healing at least partly through its antiapoptotic effects on endothelial cells at the injury site. Thus, sesamin represents a potential therapeutic medicine for vessel injury-related wounds.
Glioma is a common cancer in the central system. Exosomes play a key role in malignancies. This study mainly investigates the effect and mechanism of microRNA-1246 from self-derived exosomes on the apoptotic activities of astroglioma cells. Samples of malignant glioma were collected to measure microRNA-1246 expression. The glioma cells were cultured and their secreted exosomes were collected. Cells were randomized into NC group, miRNA-1246-mimic group and miRNA-1246-inhibitor group followed by analysis of invasion capability, expression of miR-1246 and CAMD1 gene, and AMD1 and apoptosis-related proteins expression by Western-blot as well as the relationship between miRNA-1246 and CAMD1. Under electron microscope, exosomes exhibited round shapes with a diameter of 50–290 nm and a positive expression of CD9 and CD63. miRNA-1246 was upregulated in exosomes from astroglioma patients. miRNA-1246 downregulated CADMI and apoptosis-related protein Bcl-2, but upregulated Caspase-3 and pro-apoptosis proteins in glioma cells. Moreover, miRNA-1246 facilitates astroglioma cells invasion while restraining apoptotic activities. CADM1 was confirmed to be a target of miRNA-1246. In conclusion, miR-1246 is highly expressed in exosomes that originated from astroglioma cells and suppressed the apoptosis of glioma cells via targeting CAMD1 genes.
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