Studies On Steroidal Immunosuppressive Activity Of C ₂₁

Apocynaceae is a major familiy of tropical flora, there are about250genera, more than2,000species. There are46genera, about176species,33varieties distributed in our country, while only33genera, about70species can be used as medicine. Epigynum Wight is one genus of Apocynaceae, about14species, mainly distributed in Malaysia and Myanmar. In our country only one specie, E.auritum Tsiang et P.T.Li, produced in southern Yunnan. The Dai ethnic group use boiled bark for food or medicine, it has some efficacy,such as clear heat, detoxification and relieve pain.In order to search for new compounds with pharmacological activities, we research Epigynum which were taken from Yunnan Xishuangbanna Nature Reserve as the object in the thesis, its chemical constituents were isolated, purified and structure identified, and the resulting compounds were screened preliminary activity for further research and provide theoretical basis for the development of new medicine.The thesis applied various Chromatographic method of filler such as MCI column, gel column, normal phase silica gel column and macroporous resin column, the chemical constituents of Epigynum can extracted and isolated.15compounds were identified from the extracts of Epigynum auritum,by uasing modern spectroscopic techniquessuch as IR. ESI-MS, NMR and UV. These compounds were made up of thirteen C-21steroids, one lignans and one|3-daucosterol. They were12p-Hydroxy-androst-4,6,8,14-tetraen-3,11,17-trione(l), Androst-4,6,8,14-tetraen-3,11,17-trione(2),(+)-l-Hydroxy-2-epipinore-sinol(3), A5-Pregnene-3p,17a,20S-triol(4), A5-pregnene-3p,17a,20S-triol3-O-p-D-digitalopyranoside(5), A5-pregnene-3p,17a,20-triol3-0-2-methyl-6-deoxy-P-D-talopyra-noside-20-O-D-olivopyranoside(6), P-daucosterol(7),20-O-Methyl-epigynumgenin A3-O-2-methyl-6-deoxy-P-D-talopyranoside(8), Epigynumgenin A3-O-2-methyl-6-deoxy-P-D-talopyranoside(9), Epigynumgenin A3-O-2-methyl-6-deoxy-P-D-talopyranoside-20-O-D-olivopyranoside(lO), A^-pregnene-Sp,15a,17a,20-triol3-0-2,4-di-O-methyl-D-Rhamno-pyranose(ll),17-0-Methyl-Epigynumgenin A3-0-2-methyl-6-deoxy-P-D-talopyranoside-20-O-D-olivopyranoside(12), Epigynumgenin C(13),3-0-Ethyl-Androsta-3p,12p-triol-4,14-diene-16-trione(14),3-O-Methyl-Androsta-3p,12p-triol-4,14-diene-16-trione(15). Compound4and5are isolated from this plant for the first time and compounds11-15are new compounds. Compounds14and15have new C21steroidal skeleton type. Compoun.113is a new type that its D ring is split.Meanwhile, in this thesis by lymphocyte transformation test in mice, these compounds which were isolated and indentified from Epigynum were researched of immunosuppressive activity. Study has found that most of the compounds has certain immunosuppressive activity, and compound2is the more efficient compound.