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Chinese Journal of Clinical Pharmacology and Therapeutics ›› 2019, Vol. 24 ›› Issue (8): 889-895.doi: 10.12092/j.issn.1009-2501.2019.08.007

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Tissue distribution and excretion study of GL-V9 in rats, a wogonin derivative with significant antitumor activity

XING Han, NING Chen, KONG Dexuan, CAI Hui, ZHOU Shiyu, REN Chang, KONG Ying, CHENG Yujie, CHEN Xijing   

  1. Clinical Pharmacokinetics Laboratory, China Pharmaceutical University, Nanjing 211198, Jiangsu, China
  • Received:2019-03-07 Revised:2019-06-03 Online:2019-08-26 Published:2019-08-30

Abstract:

AIM: To study the tissue distribution and excretion characteristics of GL-V9, an antitumor derivative of wogonin, in rats. METHODS: In tissue distribution study, blood and tissue samples of rats were collected after oral administration of GL-V9 (50 mg/kg), including stomach, small intestine, liver, and so on. Samples were processed with ethyl acetate and then analyzed by UPLC-MS/MS for quantification. In excretion study, rats were given GL-V9 by oral gavage at 50 mg/kg. Feces, urine and bile samples were gathered and determined using UPLC-MS/MS to investigate the excretion characteristics of GL-V9. RESULTS:The results indicated that the UPLC-MS/MS method for GL-V9 showed a good linearity over the linear range of 2-1 000 ng/mL. Tissue distribution results showed that the distribution trend of GL-V9 was from gastrointestinal tract to liver, lung and kidney tissues after oral administration, while the concentration levels of GL-V9 in brain, heart and blood were very low. The results of excretion experiments showed that the amount of GL-V9 in feces was the highest and the cumulative excretion percentage of feces was (75.41±41.77)%. CONCLUSION: GL-V9 can be widely distributed in various tissues of rats, especially in gastrointestinal tract, liver, lung and kidney tissues. Fecal excretion is the main excretion pathway of GL-V9 in rats.

Key words: GL-V9, antitumor, UPLC-MS/MS, tissue distribution, excretion

CLC Number: