Total sesquiterpene lactones prepared from Inula helenium L. has potentials in prevention and therapy of rheumatoid arthritis. (20th January 2017)

• Record Type: Journal Article
• Authors: Gao, Shuang; Wang, Qun; Tian, Xin-Hui; Li, Hui-Liang; Shen, Yun-Heng; Xu, Xi-Ke; Wu, Guo-Zhen; Hu, Zhen-Lin; Zhang, Wei-Dong
• Is Part Of: Journal of ethnopharmacology. Volume 196(2017)
• Page Start: 39
• Page End: 46
• Publication Date: 2017-01-20
• Subjects: Inula helenium L. -- Total sesquiterpene lactones -- Anti-inflammatory -- Rheumatoid arthritis; Ethnopharmacology -- Periodicals; Pharmacognosy -- Periodicals; Herbs -- Periodicals; Herbs -- Periodicals; Pharmacognosy -- Periodicals; Pharmacognosie -- Périodiques; Herbes -- Périodiques; 615.1
• DOI: 10.1016/j.jep.2016.12.020
• Languages: English
• ISSNs: 0378-8741

Abstract

Abstract: Backgrounds: Inula helenium L. is an herb with anti-inflammatory properties. Sesquiterpene lactones (SLs), mainly alantolactone (AL) and isoalantolactone (IAL), are considered as its active ingredients. However, the anti-inflammatory effects of SL-containing extracts of I. helenium have not been explored. Here we prepared total SLs from I. helenium (TSL-IHL), analyzed its chemical constituents, and performed cellular and animal studies to evaluate its anti-inflammatory activities. Materials and methods: The chemical profile of TSL-IHL was analyzed by HPLC-UV. Its in vitro effects on the activation of signaling pathways and expression of inflammatory genes were examined by western blotting and quantitative real-time PCR, respectively, and compared with those of AL and IAL. Its in vivo anti-inflammatory effects were evaluated in adjuvant- and collagen-induced arthritis rat models. Results: Chemical analysis showed that AL and IAL represent major constituents of TSL-IHL. TSL-IHL, as well as AL and IAL, could inhibit TNF- α -induced activation of NF- κ B and MAPK pathways in b. End3 cells, suppress the expressions of MMP-3, MCP-1, and IL-1 in TNF- α -stimulated synovial fibroblasts, and IL-1, IL-6, and iNOS in LPS-activated RAW 264.7 cells in a dose-dependent manner in the range of 0.6–2.4 μg/mL. Oral administration of TSL-IHL at 12.5−50 mg/kg could dose-dependently alleviate the arthritic severity and paw swelling in either developing or developed phases of arthritis of rats induced by adjuvant or collagen Conclusions: These results indicated potentials of TSL-IHL in prevention and therapy of rheumatoid arthritis. Graphical abstract: Total sesquiterpene lactones from Inula helenium L. (TSL-IHL) could effectively inhibit the activation of NF- κ B and MAPK pathways, suppress the inflammatory gene expressions in activated synovial fibroblasts and RAW 264.7 cells, and the oral treatment with TSL-IHL alleviated the paw swelling and arthritic severity in both AA and CIA rat arthritis models which indicated its therapeutic potential for rheumatoid arthritis.