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Archive > Volume 11 Issue 1 > 2019,11(1):28-38. DOI:10.1016/j.chmed.2018.05.005 Prev Next

藥代動(dòng)力學(xué)和核磁共振代謝組學(xué)方法評(píng)價(jià)小檗堿和黃連對(duì)膿毒癥的治療效果

Original articles

Pharmacokinetic and NMR metabolomics approach to evaluate therapeutic effect of berberine and Coptidis Rhizoma for sepsis

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    摘要:
    目的：膿毒癥是由感染引起的系統(tǒng)性炎癥反應(yīng)，經(jīng)常會(huì)導(dǎo)致器官功能障礙。盡管其死亡率和發(fā)病率很高，但其病理生理學(xué)仍然知之甚少。黃連及其主要活性成分小檗堿（生物堿類化合物）已經(jīng)在臨床上用作抗菌和抗炎藥物。本研究的目的是為了研究小檗堿和黃連在大鼠體內(nèi)的吸收與分布，以及對(duì)膿毒癥的治療效果。 方法：對(duì)黃連及其主要活性成分小檗堿進(jìn)行藥代動(dòng)力學(xué)和代謝組學(xué)研究。 結(jié)果：盲腸結(jié)扎穿孔誘導(dǎo)的膿毒癥大鼠的能量代謝和氨基酸代謝明顯被擾亂，而黃連和小檗堿治療之后能讓代謝物的擾亂向正常大鼠回歸。 結(jié)論：小檗堿與黃連在膿毒癥的治療上，具有相當(dāng)甚至更好的藥效。

    Abstract:
    Objective: Sepsis, a systemic response to infection, often leads to end-organ dysfunction. Despite its high rates of mortality and morbidity, its pathophysiology is still poorly understood. Coptidis Rhizoma and its main active alkaloid compound, berberine, have been as anti-bacterial and anti-inflammatory drugs used in clinic. The objective of this study was to gain more insights towards understanding the sepsis associated with drug absorption and disposition and treatments of berberine and Coptidis Rhizoma dynamically. Methods: Pharmacokinetic and metabolomic studies of Coptidis Rhizoma and its main active component berberine have been performed. Results: Cecal ligation and puncture (CLP) induced sepsis showed marked changes of metabolites concerning energy metabolism and amino acids metabolisms, which could be reversed towards the normal state by Coptidis Rhizoma and berberine. Conclusion: Berberine exhibited an equivalent and even better therapeutic effect than Coptidis Rhizoma.

    關(guān)鍵詞:
    小檗堿;盲腸結(jié)扎穿孔;黃連;代謝組學(xué);膿毒癥

    Keywords:


    Project Supported:
    This work was funded by the Key Project of National Natural Science Foundation of China (No. 81430092), the Program for Changjiang Scholars and Innovative Research Team in University (IRT_15R63), and the Priority Academic Program Development of Jiangsu Higher Education Institutions (PAPD).

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