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Quantitative bioanalytical LC–MS/MS assay for S130 in rat plasma-application to a pharmacokinetic study

    Yanping Guan

    Institute of Clinical Pharmacology, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, PR China

    Guangdong Provincial Key Laboratory of New Drug Design & Evaluation, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, PR China

    Department of Pharmacy, Sun Yat-Sen Memorial Hospital, Sun Yat-Sen University, Guangzhou 510120, PR China

    ,
    Yuanyuan Fu

    Guangdong Provincial Key Laboratory of New Drug Design & Evaluation, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, PR China

    National & Local United Engineering Lab of Druggability & New Drugs Evaluation, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, PR China

    ,
    Yao Liu

    Institute of Clinical Pharmacology, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, PR China

    Guangdong Provincial Key Laboratory of New Drug Design & Evaluation, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, PR China

    ,
    Siyi Wang

    Institute of Clinical Pharmacology, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, PR China

    Guangdong Provincial Key Laboratory of New Drug Design & Evaluation, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, PR China

    ,
    Man Zhao

    Guangdong Provincial Key Laboratory of New Drug Design & Evaluation, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, PR China

    National & Local United Engineering Lab of Druggability & New Drugs Evaluation, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, PR China

    ,
    Zhongming Jin

    Institute of Clinical Pharmacology, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, PR China

    Guangdong Provincial Key Laboratory of New Drug Design & Evaluation, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, PR China

    ,
    Fulin Jiang

    Institute of Clinical Pharmacology, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, PR China

    Guangdong Provincial Key Laboratory of New Drug Design & Evaluation, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, PR China

    ,
    Liang Hong

    Guangdong Provincial Key Laboratory of New Drug Design & Evaluation, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, PR China

    National & Local United Engineering Lab of Druggability & New Drugs Evaluation, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, PR China

    ,
    Min Huang

    Institute of Clinical Pharmacology, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, PR China

    Guangdong Provincial Key Laboratory of New Drug Design & Evaluation, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, PR China

    ,
    Min Li

    Guangdong Provincial Key Laboratory of New Drug Design & Evaluation, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, PR China

    National & Local United Engineering Lab of Druggability & New Drugs Evaluation, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, PR China

    &
    Guoping Zhong

    *Author for correspondence: Tel.: 020 873 354 29113; Fax: 020 873 354 29113;

    E-mail Address: zhonggp@mail.sysu.edu.cn

    Institute of Clinical Pharmacology, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, PR China

    Guangdong Provincial Key Laboratory of New Drug Design & Evaluation, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, PR China

    Published Online:https://doi.org/10.4155/bio-2019-0101

    Aim: An innovative Atg4B inhibitor, S130, exhibited a negative influence on colorectal cancer cells in vitro and in vivo. To assist reliable toxicodynamic and pharmacokinetic evaluation, an LC–MS/MS assay of S130 in rat plasma must be necessary. Results: An LC–MS/MS assay for determination of S130 in rat plasma has been first developed and fully verified whose values met the admissible limits as per the US FDA guidelines. Chromatographic separation was achieved by using an isocratic elution after 3 min. MS was conducted under the ESI+ mode fitted with selected reaction monitoring. The calibration curve proved acceptable linearity over 0.50–800 ng/ml. Conclusion: The developed LC–MS/MS assay of S130 in rat plasma is easily applicable in pharmacokinetics study and the further toxicological evaluation.

    Papers of special note have been highlighted as: • of interest; •• of considerable interest

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