Abstract
Paeoniflorin-6′-O-benzene sulfonate (code: CP-25) is a novel ester derivative of paeoniflorin (Pae). Compared to Pae, CP-25 has higher lipid solubility, bioavailability and better bioactivity. However, the tissue distribution and excretion of CP-25 still remain unknown. The LC–MS method was applied to investigate the tissue distribution and excretion of CP-25 in rats. As such, 50 mg/kg of CP-25 and Pae were administered to rats in multiple doses via an oral route. CP-25 and Pae were distributed widely and rapidly in all the tested tissues. Compared with Pae, the concentrations of CP-25 were almost increased evidently in most tissues. The highest CP-25 level was found in the liver (1476.33 ± 535.20 ng/g, male; 1970.38 ± 177.21 ng/g, female) at 3 h, and a high concentration of CP-25 was detected in male and female intestine, synovium, muscle, lung, and brain. Following a single oral dose of 50 mg/kg of CP-25 in rats, the total excretion of CP-25 was merely 21.8% (18.40, 3.19 and 0.22% for feces, bile and urine, respectively) in males; and was approximately 21.3% (14.04, 7.16 and 0.14% for feces, bile and urine, respectively) in females. The results indicated that the CP-25 concentration was higher in major tissues than Pae; CP-25 was primarily excreted through the feces; and there were gender-related differences in the tissue distribution and excretion.
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Acknowledgements
The authors thank the Anhui Collaborative Innovation Center of Anti-inflammatory and Immune Medicine for providing the experimental conditions. This work was financially supported by the National Natural Science Foundation of China (No. 81330081, No. 81302845), the Training Program of Academic and Technical Leaders in Universities of Anhui Province (No. 34), and the Scientific Research Foundation of the Institute for Translational Medicine of Anhui Province (No.2017zhyx33).
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Zhao, M., Zhou, P., Yu, J. et al. The tissue distribution and excretion study of paeoniflorin-6′-O-benzene sulfonate (CP-25) in rats. Inflammopharmacol 27, 969–974 (2019). https://doi.org/10.1007/s10787-018-0463-3
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DOI: https://doi.org/10.1007/s10787-018-0463-3