Emmanuel Kofi Kumatia, Nguyen Huu Tung, Alex Asase
{"title":"红辣椒科辣椒皂苷、桃甾醇和三萜酯β-谷甾醇3-肉豆蔻酸酯的抗炎镇痛活性及其与TRPV1离子通道转运体的相互作用","authors":"Emmanuel Kofi Kumatia, Nguyen Huu Tung, Alex Asase","doi":"10.1155/bri/2621242","DOIUrl":null,"url":null,"abstract":"<p><p><i>Capparis erythrocarpos</i> 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 <i>C. erythrocarpos</i>, including their modulatory effects on TRPV1 ion channel activity. The isolated compounds were characterized as daucosterol (DC) and <i>β</i>-sitosterol 3-myristate (SM) using NMR and LC/GC-MS. DC significantly (<i>p</i> < 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.</p>","PeriodicalId":8826,"journal":{"name":"Biochemistry Research International","volume":"2025 ","pages":"2621242"},"PeriodicalIF":3.4000,"publicationDate":"2025-09-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12425617/pdf/","citationCount":"0","resultStr":"{\"title\":\"Anti-Inflammatory and Analgesic Activities of the Saponin, Daucosterol, and the Triterpenoid Ester, <i>β</i>-Sitosterol 3-Myristate, From <i>Capparis erythrocarpos</i> (Isert) Capparaceae, and Their Interaction With the TRPV1 Ion Channel Transporter.\",\"authors\":\"Emmanuel Kofi Kumatia, Nguyen Huu Tung, Alex Asase\",\"doi\":\"10.1155/bri/2621242\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p><i>Capparis erythrocarpos</i> 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 <i>C. erythrocarpos</i>, including their modulatory effects on TRPV1 ion channel activity. The isolated compounds were characterized as daucosterol (DC) and <i>β</i>-sitosterol 3-myristate (SM) using NMR and LC/GC-MS. DC significantly (<i>p</i> < 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.</p>\",\"PeriodicalId\":8826,\"journal\":{\"name\":\"Biochemistry Research International\",\"volume\":\"2025 \",\"pages\":\"2621242\"},\"PeriodicalIF\":3.4000,\"publicationDate\":\"2025-09-04\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12425617/pdf/\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Biochemistry Research International\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.1155/bri/2621242\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"2025/1/1 0:00:00\",\"PubModel\":\"eCollection\",\"JCR\":\"Q2\",\"JCRName\":\"BIOCHEMICAL RESEARCH METHODS\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Biochemistry Research International","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.1155/bri/2621242","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2025/1/1 0:00:00","PubModel":"eCollection","JCR":"Q2","JCRName":"BIOCHEMICAL RESEARCH METHODS","Score":null,"Total":0}
Anti-Inflammatory and Analgesic Activities of the Saponin, Daucosterol, and the Triterpenoid Ester, β-Sitosterol 3-Myristate, From Capparis erythrocarpos (Isert) Capparaceae, and Their Interaction With the TRPV1 Ion Channel Transporter.
Capparis erythrocarpos 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 C. erythrocarpos, including their modulatory effects on TRPV1 ion channel activity. The isolated compounds were characterized as daucosterol (DC) and β-sitosterol 3-myristate (SM) using NMR and LC/GC-MS. DC significantly (p < 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.