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.
Background: This study aimed to examine the expression level and prognostic value of microRNA-29a (miR-29a) in human cholangiocarcinoma (CCA). Patients and Methods: The expression of miR-29a was measured in tissues collected from 125 CCA patients using quantitative real-time reverse transcription polymerase chain reaction (qRT-PCR). Survival analysis was carried out using the Kaplan-Meier method and log-rank test. The prognostic value of miR-29a was examined with Cox regression analysis. Results: The results of qRT-PCR demonstrated that miR-29a expression was significantly upregulated in CCA tissue samples compared with matched noncancerous samples. Overexpression of miR-29a was found to be correlated with lymph node metastasis, clinical stage, and differentiation of CCA. The Kaplan-Meier survival curves suggested that patients with high miR-29a levels had poor overall survival compared to those with low miR-29a expression. From the results of the Cox regression analysis, we considered increased miR-29a expression to be an independent prognostic factor for patients with CCA. Conclusion: Our study data demonstrated that upregulated miR-29a expression is associated with progression of CCA and might act as a prognostic biomarker in CCA patients.
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