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来自白花菜科(伊塞尔)的皂苷、胡萝卜苷以及三萜酯β-谷甾醇3-肉豆蔻酸酯的抗炎和镇痛活性及其与TRPV1离子通道转运体的相互作用

Anti-Inflammatory and Analgesic Activities of the Saponin, Daucosterol, and the Triterpenoid Ester, -Sitosterol 3-Myristate, From (Isert) Capparaceae, and Their Interaction With the TRPV1 Ion Channel Transporter.

作者信息

Kumatia Emmanuel Kofi, Tung Nguyen Huu, Asase Alex

机构信息

Department of Phytochemistry, Centre for Plant Medicine Research, Mampong, Akuapem, Ghana.

Department of Medicinal Chemistry and Drug Quality Control, Faculty of Pharmacy, Phenikaa University, Hanoi, Vietnam.

出版信息

Biochem Res Int. 2025 Sep 4;2025:2621242. doi: 10.1155/bri/2621242. eCollection 2025.

Abstract

is a medicinal plant traditionally used as an antiarthritic, anti-inflammatory, and analgesic agent. However, no previous reports exist on the analgesic and acute anti-inflammatory activities of the individual chemical constituents from this plant. This study reports the isolation, characterization, and evaluation of analgesic and acute anti-inflammatory activities of chemical constituents from the root bark of , including their modulatory effects on TRPV1 ion channel activity. The isolated compounds were characterized as daucosterol (DC) and -sitosterol 3-myristate (SM) using NMR and LC/GC-MS. DC significantly ( < 0.05) inhibited both phases of carrageenan-induced edema in a reverse dose-dependent manner, demonstrating 58.38% anti-inflammatory activity at 2 mg/kg p.o., comparable to diclofenac sodium (DS) at 8 mg/kg p.o. (53.07%). SM inhibited only phase 2 of carrageenan-induced edema. Both compounds significantly inhibited cold-induced pain with superior analgesic activity compared to DS. Against inflammation-induced pain, DC showed the highest analgesic activity (47.37% at 2 mg/kg p.o.). Molecular docking studies revealed that DC and SM produced ΔG values of -10.60 and -9.80 kcal/mol, respectively, which are more negative than those of DS (-8.6 kcal/mol), suggesting that they might be superior TRPV1 ion channel inhibitors and that DS likely has additional mechanisms of action. These results demonstrate that DC and SM possess remarkable therapeutic properties, warranting further exploration for novel drug development.

摘要

是一种传统上用作抗关节炎、抗炎和镇痛剂的药用植物。然而,此前尚无关于该植物单个化学成分的镇痛和急性抗炎活性的报道。本研究报告了从[植物名称]根皮中分离、鉴定化学成分及其镇痛和急性抗炎活性的评估,包括它们对TRPV1离子通道活性的调节作用。使用NMR和LC/GC-MS将分离出的化合物鉴定为胡萝卜苷(DC)和β-谷甾醇3-肉豆蔻酸酯(SM)。DC以剂量依赖性方式显著(P<0.05)抑制角叉菜胶诱导的水肿的两个阶段,在口服2mg/kg时显示出58.38%的抗炎活性,与口服8mg/kg的双氯芬酸钠(DS)(53.07%)相当。SM仅抑制角叉菜胶诱导的水肿的第二阶段。与DS相比,这两种化合物均显著抑制冷诱导的疼痛,具有更高的镇痛活性。针对炎症诱导的疼痛,DC显示出最高的镇痛活性(口服2mg/kg时为47.37%)。分子对接研究表明,DC和SM产生的ΔG值分别为-10.60和-9.80kcal/mol,比DS的(-8.6kcal/mol)更负,表明它们可能是更好的TRPV1离子通道抑制剂,且DS可能具有其他作用机制。这些结果表明,DC和SM具有显著的治疗特性,值得进一步探索用于新药开发。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/51b1/12425617/8a9bd6a5b394/BRI2025-2621242.001.jpg

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