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Total sesquiterpene lactones prepared from Inula helenium L. has potentials in prevention and therapy of rheumatoid arthritis

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
Journal of ethnopharmacology 2017 v.196 pp. 39-46
Inula helenium, Western blotting, active ingredients, adjuvants, anti-inflammatory activity, dose response, fibroblasts, genes, high performance liquid chromatography, inducible nitric oxide synthase, interleukin-1, interleukin-6, mitogen-activated protein kinase, oral administration, quantitative polymerase chain reaction, rats, rheumatoid arthritis, sesquiterpenoid lactones, signal transduction, therapeutics, traditional medicine, transcription factor NF-kappa B
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.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.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-κB 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 0.6–2.4μg/mL. Oral administration of TSL-IHL at 12.5−50mg/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 collagenThese results indicated potentials of TSL-IHL in prevention and therapy of rheumatoid arthritis.