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J Ethnopharmacol. 2017 Jan 20;196:39-46. doi: 10.1016/j.jep.2016.12.020. Epub 2016 Dec 15.

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

Author information

1
School of Pharmacy, Second Military Medical University, 325 Guohe Road, Yangpu District, Shanghai 200433, China. Electronic address: gaoshuangphu@163.com.
2
School of Pharmacy, Second Military Medical University, 325 Guohe Road, Yangpu District, Shanghai 200433, China. Electronic address: qunwang0523@163.com.
3
Institute of Interdisciplinary Complex Research, Shanghai University of Traditional Chinese Medicine, 1200 Cailun Road, Pudong New District, Shanghai 201203, China. Electronic address: tianxinhui@126.com.
4
School of Pharmacy, Second Military Medical University, 325 Guohe Road, Yangpu District, Shanghai 200433, China. Electronic address: faranli@hotmail.com.
5
School of Pharmacy, Second Military Medical University, 325 Guohe Road, Yangpu District, Shanghai 200433, China. Electronic address: shenyunheng@hotmail.com.
6
School of Pharmacy, Second Military Medical University, 325 Guohe Road, Yangpu District, Shanghai 200433, China. Electronic address: xkxu@smmu.edu.cn.
7
School of Pharmacy, Second Military Medical University, 325 Guohe Road, Yangpu District, Shanghai 200433, China. Electronic address: 496528260@qq.com.
8
School of Pharmacy, Second Military Medical University, 325 Guohe Road, Yangpu District, Shanghai 200433, China. Electronic address: zhenlinhu@hotmail.com.
9
School of Pharmacy, Second Military Medical University, 325 Guohe Road, Yangpu District, Shanghai 200433, China; Institute of Interdisciplinary Complex Research, Shanghai University of Traditional Chinese Medicine, 1200 Cailun Road, Pudong New District, Shanghai 201203, China. Electronic address: wdzhangy@hotmail.com.

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-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 collagen CONCLUSIONS: These results indicated potentials of TSL-IHL in prevention and therapy of rheumatoid arthritis.

KEYWORDS:

Anti-inflammatory; Inula helenium L.; Rheumatoid arthritis; Total sesquiterpene lactones

PMID:
27988396
DOI:
10.1016/j.jep.2016.12.020
[Indexed for MEDLINE]

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