Study On The Chemical Constituents Of Anoectochilus Roxburghii And Activity Of Derivatives Of Deoxypodophyllotoxin

The genus Anoectochilus, belonging to Orchidaceae, is a perennial herb, which comprise more than 40 species that are widespread in the tropical regions, from Asia to Oceania. There are 20 species and 2 varieties in China, from southwest to the south. Among them, Anoectochilus roxburghii and Anoectochilus formosanus are most valuable, which have been used in Chinese folk medicines, and at the same time, they are all ornamental plants. Several species of this genus are used as folk medicines for febrifugation, detoxification, dispelling wind, eliminating dampness and hypertension. The Anoectochilus roxburghii, a member of genus Anoectochilus, which is called "King Medicine", mainly distributes in Yunnan, Sichuan, Guizhou, Guangxi, Tibet, Zhejiang, Jiangxi, Guangdong, Hainan, Fujian and Taiwan etc. It is common knowledge that this genus has been identified to contain flavones and glycosides.This dissertation studies on chemical constituents of the EtoAc part of Anoectochilus roxburghii. 31 compounds have been isolated by silica gel column chromatography (CC), preparative thin layer chromatography (PTLC) and recrystallization etc.. The structures of 27 compounds have been elucidated by spectroscopic methods:UV,IR,MS,NMR, physical constants:melting point and optical rotation, as well as comparison with authentic samples or the data from literature. The were identified as flavones, glycosides and triterpenes etc., one of them is new compound, six compounds are isolated from this genus for the first time. Meanwhile, the antioxidative activities of some of them were tested.Podophyllotoxin is a natural lignan compound. Podophyllotoxin as well as its congeners and derivatives exhibits pronounced biological activity mainly as antiviral, antineoplastic and insecticidal etc.. Among them, antitumor activity is the most attractive, making it as a lead compound for anticancer drug design and development. In this part of thesis,7 novel spin labeled derivatives of deoxypodophyllotoxin compounds which have been synthesized, we evaluated for their cytotoxic, antioxidative activities in vitro and lipid-water partition coefficient. As a result,5 compounds show higher inhibition activity against A-549 cells compared with the clinical drug VP-16 and parent compound,3 compounds show excellent inhibition activity against HL-60 cells. All these derivatives have a good aqueous solubility and significantly antioxidative activity compared with VP-16 and parent compound.