Study on the pharmacokinetics and brain tissue distribution of eight anti-inflammatory active components in normal and neuroinflammatory rats orally administered with extract of Tinospora sinensis (Lour.) Merr. using the UPLC-MS/MS method

IF 2.5 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia Pub Date : 2025-05-08 DOI:10.1016/j.fitote.2025.106564

Liping Chen , Longhui Lu , Guoliang Xu , Zhihui Jiang , Qiujin Guo , Feijun Huang , Wenyan Yan , Hang Zhang , Yi Wu , Yongyan Xie , Liping Huang

{"title":"Study on the pharmacokinetics and brain tissue distribution of eight anti-inflammatory active components in normal and neuroinflammatory rats orally administered with extract of Tinospora sinensis (Lour.) Merr. using the UPLC-MS/MS method","authors":"Liping Chen , Longhui Lu , Guoliang Xu , Zhihui Jiang , Qiujin Guo , Feijun Huang , Wenyan Yan , Hang Zhang , Yi Wu , Yongyan Xie , Liping Huang","doi":"10.1016/j.fitote.2025.106564","DOIUrl":null,"url":null,"abstract":"<div><div><em>Tinospora sinensis (Lour.) Merr.</em> (<em>Tinospora sinensis</em>) is a traditional Chinese medicine commonly used by Tibetan people in China to prevent and treat diseases such as senile dementia, neuroinflammatory, and rheumatoid arthritis. However, the pharmacokinetic characteristics and tissue distribution of <em>Tinospora sinensis</em> active components in vivo, especially the distribution of brain regions, are unclear. Herein, a stable and accurate ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method was developed and validated to compare the pharmacokinetic patterns and differences in brain tissue distribution of eight anti-inflammatory active components in normal and neuroinflammatory rats after oral administration of extracts from <em>Tinospora sinensis</em>. ACE Excel 3 C18-AR (100 × 2.1 mm, 1.7 μm) column was used for gradient elution with 0.1 % formic acid water (A) and acetonitrile (B), rifampicin as an internal standard, electrospray ionization (ESI) positive and negative ion mode scanning, multiple reaction monitoring (MRM) determination, and DAS 2.0 software analysis. The UPLC-MS/MS method established through verification is accurate and reliable, and the methodology can meet the quantitative requirements. The pharmacokinetic results showed differences in the pharmacokinetic process and brain tissue distribution between normal rats and rats with neuroinflammation. All eight anti-inflammatory active components can be rapidly absorbed into the bloodstream (<em>Tmax</em> ≤ 2 h), but the plasma metabolism rate of rats with neuroinflammation is faster and the brain content is lower. Neuroinflammation has a significant impact on the in vivo process of oral administration of <em>Tinospora sinensis</em> in rats. The study provides experimental evidence for the quality control and clinical application of <em>Tinospora sinensis</em>.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"184 ","pages":"Article 106564"},"PeriodicalIF":2.5000,"publicationDate":"2025-05-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Fitoterapia","FirstCategoryId":"3","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0367326X25001893","RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}

引用次数: 0

Abstract

Tinospora sinensis (Lour.) Merr. (Tinospora sinensis) is a traditional Chinese medicine commonly used by Tibetan people in China to prevent and treat diseases such as senile dementia, neuroinflammatory, and rheumatoid arthritis. However, the pharmacokinetic characteristics and tissue distribution of Tinospora sinensis active components in vivo, especially the distribution of brain regions, are unclear. Herein, a stable and accurate ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method was developed and validated to compare the pharmacokinetic patterns and differences in brain tissue distribution of eight anti-inflammatory active components in normal and neuroinflammatory rats after oral administration of extracts from Tinospora sinensis. ACE Excel 3 C18-AR (100 × 2.1 mm, 1.7 μm) column was used for gradient elution with 0.1 % formic acid water (A) and acetonitrile (B), rifampicin as an internal standard, electrospray ionization (ESI) positive and negative ion mode scanning, multiple reaction monitoring (MRM) determination, and DAS 2.0 software analysis. The UPLC-MS/MS method established through verification is accurate and reliable, and the methodology can meet the quantitative requirements. The pharmacokinetic results showed differences in the pharmacokinetic process and brain tissue distribution between normal rats and rats with neuroinflammation. All eight anti-inflammatory active components can be rapidly absorbed into the bloodstream (Tmax ≤ 2 h), but the plasma metabolism rate of rats with neuroinflammation is faster and the brain content is lower. Neuroinflammation has a significant impact on the in vivo process of oral administration of Tinospora sinensis in rats. The study provides experimental evidence for the quality control and clinical application of Tinospora sinensis.

查看原文本刊更多论文

中药天螺提取物对正常大鼠和神经炎大鼠8种抗炎活性成分的药动学及脑组织分布研究稳定。采用UPLC-MS/MS法。

sinospora sinensis （Lour.）稳定。（Tinospora sinensis）是中国藏族人民常用的一种中药，用于预防和治疗老年性痴呆、神经炎症和类风湿性关节炎等疾病。然而，对中华Tinospora sinensis有效成分在体内的药代动力学特征和组织分布，特别是脑区的分布尚不清楚。本研究建立了一种稳定、准确的超高效液相色谱-串联质谱（UPLC-MS/MS）方法，比较正常大鼠和神经炎症大鼠口服Tinospora sinensis提取物后8种抗炎活性成分的药动学模式和脑组织分布差异。采用ACE Excel 3 C18-AR（100 × 2.1 mm, 1.7 μm）色谱柱，以0.1 %甲酸水(A)和乙腈(B)梯度洗脱，利福平为内标，电喷雾电离（ESI）正负离子模式扫描，多重反应监测（MRM）测定，DAS 2.0软件分析。通过验证建立的UPLC-MS/MS方法准确可靠，方法学满足定量要求。药代动力学结果显示正常大鼠与神经炎症大鼠在药代动力学过程和脑组织分布上存在差异。8种抗炎活性成分均能迅速被血流吸收（Tmax ≤ 2 h），但神经炎症大鼠血浆代谢速率较快，脑含量较低。神经炎症对大鼠口服中华Tinospora的体内过程有显著影响。本研究为中华Tinospora sinensis的质量控制和临床应用提供了实验依据。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

求助全文

约1分钟内获得全文求助全文

来源期刊

Fitoterapia 医学-药学

CiteScore

5.80

自引率

2.90%

发文量

198

审稿时长

1.5 months

期刊介绍： Fitoterapia is a Journal dedicated to medicinal plants and to bioactive natural products of plant origin. It publishes original contributions in seven major areas: 1. Characterization of active ingredients of medicinal plants 2. Development of standardization method for bioactive plant extracts and natural products 3. Identification of bioactivity in plant extracts 4. Identification of targets and mechanism of activity of plant extracts 5. Production and genomic characterization of medicinal plants biomass 6. Chemistry and biochemistry of bioactive natural products of plant origin 7. Critical reviews of the historical, clinical and legal status of medicinal plants, and accounts on topical issues.