State Key Laboratory for Quality Ensurance and Sustainable Use of Dao-di Herbs, Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing 100193, China.
School of Pharmacy, Jiangxi University of Chinese Medicine, Nanchang 330004, China.
Int J Mol Sci. 2024 Jun 5;25(11):6228. doi: 10.3390/ijms25116228.
Berberine (BBR) is used to treat cancer, inflammatory conditions, and so on. But the side effects of BBR causing constipation should not be ignored. In clinical application, the combination of Lour. (AVL) and BBR can relieve it. However, the effective ingredients and molecular mechanism of AVL in relieving constipation are not clear. A small intestine propulsion experiment was conducted in constipated mice to screen active ingredients of AVL. We further confirmed the molecular mechanism of action of the active ingredient on BBR-induced constipation. Quercetin (QR) was found to be the effective ingredient of AVL in terms of relieving constipation. QR can efficiently regulate the microbiota in mice suffering from constipation. Moreover, QR significantly raised the levels of substance P and motilin while lowering those of 5-hydroxytryptamine and vasoactive intestinal peptide; furthermore, it also increased the protein expression levels of calmodulin, myosin light-chain kinase, and myosin light chain. The use of QR in combination with BBR has an adverse effect-reducing efficacy. The study provides new ideas and possibilities for the treatment of constipation induced by BBR.
小檗碱(BBR)被用于治疗癌症、炎症等疾病。但 BBR 引起便秘的副作用不容忽视。在临床应用中,黄连(AVL)与 BBR 的联合使用可以缓解便秘。然而,AVL 缓解便秘的有效成分及分子机制尚不清楚。本研究通过建立便秘小鼠的小肠推进实验,筛选 AVL 的活性成分。进一步证实了该活性成分对 BBR 诱导的便秘的作用机制。研究发现槲皮素(QR)是 AVL 缓解便秘的有效成分。QR 可有效调节便秘小鼠的肠道菌群。此外,QR 可显著提高 P 物质和胃动素水平,降低 5-羟色胺和血管活性肠肽水平,同时增加钙调蛋白、肌球蛋白轻链激酶和肌球蛋白轻链的蛋白表达水平。QR 与 BBR 联合使用具有减效作用。本研究为 BBR 诱导的便秘治疗提供了新的思路和可能性。
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