Analysis of riociguat and desmethyl riociguat by UPLC-MS/MS and its interaction with quercetin

IF 4.4 2区 医学 Q1 PHARMACOLOGY & PHARMACY
Qingqing Li, Xiaohai Chen, Siping Zhang, Wanshu Li, Hangjuan Lin
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引用次数: 0

Abstract

Riociguat, an orally soluble guanylate cyclase (sGC)-promoting drug, is mainly used in the clinical treatment of pulmonary hypertension (PH). In this study, a novel ultra-performance liquid chromatography-tandem mass spectrometry method was developed to quantify the concentrations of riociguat and its metabolite (M1) in plasma. The precision, stability, accuracy, matrix effect, and recovery of the methodology were satisfactory. Quercetin, a well-recognized compound, functions as a novel anticancer agent with the potential to alleviate symptoms of PH. Therefore, the potential interaction between quercetin and riociguat was investigated in this study. The levels of riociguat and M1 in rat plasma were measured using the method developed in this study to evaluate the interactions between riociguat and quercetin in rats. The results revealed that quercetin significantly inhibited riociguat and M1 metabolism with increased systemic exposure.
通过 UPLC-MS/MS 分析里奥西瓜特和去甲基里奥西瓜特及其与槲皮素的相互作用
Riociguat 是一种口服可溶性鸟苷酸环化酶(sGC)促进药物,主要用于肺动脉高压(PH)的临床治疗。本研究建立了一种新型的超高效液相色谱-串联质谱法,用于定量检测血浆中里奥吉曲及其代谢物(M1)的浓度。该方法的精密度、稳定性、准确度、基质效应和回收率均令人满意。槲皮素是一种公认的化合物,它是一种新型抗癌剂,具有缓解 PH 症状的潜力。因此,本研究调查了槲皮素与里奥西瓜酯之间的潜在相互作用。采用本研究中开发的方法测定了大鼠血浆中瑞奥西瓜特和 M1 的水平,以评估瑞奥西瓜特和槲皮素在大鼠体内的相互作用。结果表明,随着全身暴露量的增加,槲皮素能明显抑制里奥西瓜特和 M1 的代谢。
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来源期刊
Frontiers in Pharmacology
Frontiers in Pharmacology PHARMACOLOGY & PHARMACY-
CiteScore
7.80
自引率
8.90%
发文量
5163
审稿时长
14 weeks
期刊介绍: Frontiers in Pharmacology is a leading journal in its field, publishing rigorously peer-reviewed research across disciplines, including basic and clinical pharmacology, medicinal chemistry, pharmacy and toxicology. Field Chief Editor Heike Wulff at UC Davis is supported by an outstanding Editorial Board of international researchers. This multidisciplinary open-access journal is at the forefront of disseminating and communicating scientific knowledge and impactful discoveries to researchers, academics, clinicians and the public worldwide.
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