Chemical Constituents From Derris Eriocarpa How And Structure Transformation Of The Active Ingerdient

By the modern theory and science technology,combing with the knowledge of the natural medicine chemistry,this research was aimed to study the chemistry composition of the natural medicine,and to understand the active ingredients,structural feature and physicochemical property.Especially directed by the bioactive,with the knowledge of the Medicinal Chemistry,Organic Chemistry,Biochemistry,Drug Design and other subjects,working for chemical synthesis,biosythesis and structual modification.Derris eriocarpa How,was commonly known in―Zhuang‖in Guangxi province of China.This plant was being used for relieving cough and reducing sputum,as well as in the treatment of nephritis,cystitis,urethritis,beriberi edema.This article contains three parts,including the extraction,separation and purification,and the structure transformation of the active ingredient.Part I.On the extraction prcess optimization of Derris eriocarpa How,first of all,was to establish the HPLC fingerprint to preliminary understand the compositon.And then,on the composition such as alkaloids,flavonoids,we used the method of response surface to optimizate the extraction process in order to get effective components in the maximum.Part II.Research was carried on the isolation,purification and sturcture identification,thin-layer chromatography（TLC）,column chrom-atography（CC）,and recrystallization were used to separate compounds,IR,UV,NMR,MS and X-ray single crystal diffractometer were needed for structural identification.Seven compounds was isolated as:3,5-dimethoxy-4’-O-prenyl-trans-stilbene,4,5-dimethoxy-8,8-dimethyl-3-(4-methoxyphenyl-2H,8H-benzo[1,2-b:5,4-b’]dip-yr an-2-one,3-Benzo[1,3]dioxol-5-yl-4,5-dimethoxy-8,8-dimethyl-8H-pyrano[3,2-g]chromen-2-one,3-（2,3-Dihydro-benzofuran-5-yl）-4,5-dimethoxy-8,8-dimethyl-8H-pyrano[3,2-g]chromen-2-one,3-（benzo[d][1,3]dioxol-5-yl）-5,7-dimethoxy-6-（3-methylbut-2-enyl）-4H-chromen-4-one,Derrubone,4-hydroxy-3-（4’-hydr-oxyphenyl）-5-methoxy-2’’,2’’-dimethyl-pyrano[5’’,6’’:6,7]coumarin。Part III.Trans-3,4,5,4’-tetramethoxystilbene,was isolated from the D.eriocarpa How,with the knowledge of Discovery Studio,by nitration,alkylate,halogenate,oxidation,reduction,to improve the stability,low bioavailability,and poor selectivity.22 novel compounds were gained.MTT method was used to evaluate the activity of the derivatives,3-(2-chloro-5-（trifluoromethyl）phenyl-2-（4-methoxyphenyl）acrylic acid（r）had the best antiproliferative,the IC₅₀ was7.49μM.3D QSAR could help guide the further structural optimization of compounds...