Chemical Constituents Of Gentiana Crassicaulis And Anti-inflammatory Activities

"Qin-Jiao" has been widely used as one of the important herbs for fighting rheumatism since ancient times, which was recorded in"Shennong Bencao Jing" firstly. The efficacy of the herb is recorded for treatment of rheumatism, arthralgia, stroke, hemiplegia, pains, jaundice, and infantile malnutrition. The Chinese Pharmacopoeia provides that the roots of four plants, Gentiana macrophylla Pall., G. crassicaulis Duthie ex Burk., G. straminea Maxim, and G. dahurica Fisch, are used as the raw materials of "Qin-Jiao". The former three species are used to be called as "Qin-Jiao" or "Ma-Hua-Jiao" according to the properties of their roots, while the last one was called as "Xiao-Qin-Jiao"Wild production of "Qin-Jiao" was severely reduced. Some other Gentiana species have been introduced into cultivation, among which G.macrophylla and G. straminea are two commonly cultivated species in recent years in Northwest and Southwest areas. In addition, some Gentiana species are used as "Qin-Jiao" except for the four plants recorded in Chinese Pharmacopoeia. Therefore, the research of "Qin-Jiao" resources and sustainable utilization are urgent subject.The thesis investigate chemical constituents of the root from Gentiana crassicaulis Duthie ex Burk. and their anti-inflammatory activities, which led to the isolation of18compounds, including3new compound. Their structures were elucidated on the basis of extensive1D,2D spectroscopic analysis and MS techniques. The absolute configurstions of some new compounds were determined by acidic hydrolysis and GC method. Compounds1-3,5,9and10-11were evaluated for anti-inflammatory. All of them showed inhibitory effects on inflammatory mediators NO at a concentration of15μM, while5and9displayed the most potential inhibitory effects on TNF-α with IC50of0.06and0.05μM, respectively. It is noted that the terminal double bond between C-8and C-10should be a key to the inhibitory effect on TNF-α. Meanwhile, the result revealed that the number of monosaccharide units in their sugar chains could also affect their anti-inflammatory activities.In addition, the thesis review the herbal textual research, chemical constituents, biological activities and quality control of "Qin-Jiao"...