The Schisandra Sphenanthera Chemical Constituents And Anti-inflammatory Activity

The dissertation is composed of four chapters. In the first chapter, the research advance of the chemical constitutes and bioactivities of the family Schisandraceae were summarized. In the second chapter, the isolation and identification of the chemical constitutes from the fruits of Schisandra sphenanthera Rehd. et Wils were described. Reports in the chapter 3 were about the anti-inflammatory activity of the compounds from S. sphenanthera. The last chapter was a summary report of the research work.(1)S. sphenanthera belongs to the genus Schisandra of the family schisandraceae. It is widely distributed in Sichuan, Hubei, Shanxi, Shanxi, Yunnan, Henan province. The fruits of S. sphenanthera are used as an antitussive, tonic and sedative agent under the name of Wuweizi in traditional Chinese medicine together with the fruits of Schisandra chinensis Baill. The genus Schisandra plants, belonging to the economically and medicinally important family Schisandraceae, has proved to be a rich source of dibenzocyclooctadiene lignans, as well as lanostane and cycloartane triterpenes, which have been found to possess many beneficial pharmacological effects. Intensive research on this plant led to the discovery of two drugs:schisantherin A and dimethylbiphenydicarboxylate, for the treatment of hepatitis.(2) In the preceding paper of this plant, we have reported the chemical constituents of the fruits of Schisandra sphenanthera, but no new compound was isolated. As a part of our research program to find new compounds with anti-inflammatory activities from S. sphenanthera Rehd. et Wils,19 compounds, including lignans, triterpenoids, steroids, and flavanols, were isolated and identified by the means of chromatographic methods and spectroscopic evidences. Among them, three compounds were showed to be new ones, including a new 3,4-seco-lanostane triterpenoid, schisanlactone G (1) and two new dibenzocyclooctadiene lignans, chloromethyl schisantherin B (2) and methylgomisin O (3). Compound 2 was identified as a cyclooctadiene moiety substituted with a chloromethyl, which was rarely found in natural products especially in terrestrial higher plants. The known compounds were elucidated as:epigomisin O (4),6-0-Benzoylgomisin (5), gomisin J (6), methylgomisin R (7), schisantherin A (8), schisantherin B (9), schisantherin C (10), schisantherin D (11), (+)-gomisin K3 (12), (+)-deoxyschisandrin (13), myristargenol A (14), sphenanlignan (15), catechin (16), schisanlactone D (17),β-sitosterol (18), and daucosterol (19). Compouds 1-5 and 14-17 were obtained from this plant for the first time.(3) The effects of extracts and compounds 3 and 8 from bioactive fraction on cytokine productions were investigated. Compounds 3 and 8 could downregulate tumor necrosis factor-a (TNF-a), and interleukin-6 (IL-6) production, and did not display any cellular toxicity against RAW264.7 cells. Therefore, compounds 3 and 8 may show positive anti-inflammatory activity.