The chemical constituents from the roots of <i>Gentiana crassicaulis</i> and their inhibitory effects on inflammatory mediators NO and TNF-<i>α</i>

doi:10.1007/s13659-012-0067-3

Natural Products and Bioprospecting

2012, Vol. 2

Issue (5) : 217-221 DOI: 10.1007/s13659-012-0067-3

Short Communication

The chemical constituents from the roots of Gentiana crassicaulis and their inhibitory effects on inflammatory mediators NO and TNF-α

Tao LV^a,b, Min XU^a, Dong WANG^a, Hong-Tao ZHU^a, Chong-Ren YANG^a,c, Tian-Tai ZHANG^d, Ying-Jun ZHANGa

a State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, China;
b Yunnan University of Traditional Chinese Medicine, Kunming 650500, China;
c Weihe Biotech Research and Development Center, Yuxi 653101, China;
d National Center for Pharmaceutical Screening, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China

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Abstract Chemical study on the roots of Gentiana crassicaulis Duthie ex Burk(Gentianaceae) afforded 15 compounds, including two new iridoid glycosides, qinjiaosides B(1) and C(2). Their structures were elucidated by spectroscopic methods and chemical evidence. The isolated iridoid glycosides 1, 4-6 and 8-11 were tested for their anti-inflammatory activity by the inhibitory effects on LPS-induced NO and TNF-α production in macrophage RAW264.7 cells. All of them showed inhibitory effects on inflammatory mediators NO at a concentration of 15 μM, while 5 and 9 displayed the most potential inhibitory effects on TNF-α with IC₅₀ of 0.06 and 0.05 μM, respectively. The structure-activity relationships(SARs) of these iridoid derivatives were discussed.

Keywords Gentiana crassicaulis Gentianaceae iridoid glycosides qinjiaosides

Fund:This work was supported by the Science&Technology Planning Project of Yunnan Province(2010CD106), the 973 Program of Ministry of Science&Technology of China(2011CB915503), the State Key Laboratory of Phytochemistry and Plant Resources in West China, Chinese Academy of Sciences(CAS)(P2010-ZZ03), the Fourteenth Candidates of the Young Academic Leaders of Yunnan Province(Min XU, 2011CI044) and the West Light program of CAS.

Issue Date: 11 February 2018

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Tao LV,Min XU,Dong WANG, et al. The chemical constituents from the roots of Gentiana crassicaulis and their inhibitory effects on inflammatory mediators NO and TNF-α[J]. Natural Products and Bioprospecting, 2012, 2(5): 217-221.

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http://npb.kib.ac.cn/EN/10.1007/s13659-012-0067-3 OR http://npb.kib.ac.cn/EN/Y2012/V2/I5/217

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