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Analysis of metabolites of rocuronium bromide in human bile and the study of transmembrane transport mechanism
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Ai-nan ZHOU1, Zi-tao GUO1, Jia-jun CHEN2, Yun-quan LUO2, Bo TAN2, Xing-xing DIAO1, Da-fang ZHONG1, *
Acta Pharmaceutica Sinica | 2022, 57(8) : 2461 - 2470
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Acta Pharmaceutica Sinica | 2022, 57(8): 2461-2470
• Original Articles •
Analysis of metabolites of rocuronium bromide in human bile and the study of transmembrane transport mechanism
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Ai-nan ZHOU1, Zi-tao GUO1, Jia-jun CHEN2, Yun-quan LUO2, Bo TAN2, Xing-xing DIAO1, Da-fang ZHONG1, *
Affiliations
  • 1. Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
  • 2. Shuguang Hospital Affiliated to Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China
Published: 2022-08-12 doi: 10.16438/j.0513-4870.2022-0583
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Rocuronium bromide is an acetylcholine N2 receptor antagonist, which can be used as an auxiliary drug for general anesthesia. It has been reported that rocuronium has two possible metabolic pathways: N-dealkylation and O-deacetylation, which are mainly taken up by liver and excreted by bile in the form of primary drugs. In this paper, the metabolites of rocuronium in human bile were detected by UHPLC-QE-orbitrap-MS, thirteen metabolites were detected, including eleven phase I metabolites and two phase II metabolites, eleven of which had not been previously reported. At the same time, HEK293 cells overexpressing transporter were used to explore the transmembrane transport mechanism of rocuronium, the results showed that rocuronium was the substrate of MATE1, OCT1, OATP1B1 and OATP1B3. The above research results enrich the metabolic pathway of rocuronium in vivo, and put forward the possible transport mechanism of liver uptake and bile excretion, which can better guide the accurate and safe clinical drug application. The collection of human bile samples in this study was approved by the ethics committee of Shuguang Hospital Affiliated to Shanghai University of Traditional Chinese Medicine (Approval Number: 2019-775-130-01).

metabolite  /  rocuronium bromide  /  human bile  /  UHPLC-QE-Orbitrap-MS  /  transporter
Ai-nan ZHOU, Zi-tao GUO, Jia-jun CHEN, Yun-quan LUO, Bo TAN, Xing-xing DIAO, Da-fang ZHONG. Analysis of metabolites of rocuronium bromide in human bile and the study of transmembrane transport mechanism[J]. Acta Pharmaceutica Sinica, 2022 , 57 (8) : 2461 -2470 . DOI: 10.16438/j.0513-4870.2022-0583
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Article Info
doi: 10.16438/j.0513-4870.2022-0583
  • Receive Date：2022-05-12
  • Online Date：2025-12-23
  • Published：2022-08-12
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  • Received：2022-05-12
  • Revised：2022-06-08
Affiliations
    1. Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
    2. Shuguang Hospital Affiliated to Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China
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表12种不同金属材料的力学参数
科
Family		 属数
Number of
genus		 种数
Number of
species		 占总种数比例
Percentage of
total species (%)		 属
Genus		 种数
Number of
species		 占总种数比例
Percentage of total
species (%)
鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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