Studies On The Chemical Constituents Of Hedyotis Diffusa Willd. And Its Anti-tumour Activity In Vitro

Hedyotis diffusa Willd. is in function of clearing and detoxifying, diuretic swelling, blood pain.The modern pharmacology expresses that the herbal medie nce have obviously activities on tumor.Objective:Numerous studies on Hedyotis diffusa Willd. were mostly for its alcohol extracts. But the traditional decoction is the usual way in clinical me dicine. This research is to explore the chemical constituents and the pharmacol ogical activity of the water extracts.This study concentrates on researching the chemical constituents of the two parts of HDW3(which from the aqueous extracts of Hedyotis diffusa Willd. detached by HP-20 macroporous resin with50% ethanol- water) and HDW4( that was extracted from the residue by 95% ethanol).It obtains a series of polar parts and monomer compounds.The stu dy used on the A549,MCF-7,PLC and Hela cell to observe the anti-endometrial cancer activities.Methods: Looking for literatures on the chemical constituents, pharmacolo gical effects, clinical application of Hedyotis diffusa Willd. by widely searching CA, CNKI and Chinese Pharmacopoeia and other literatures in order to summ arized and generalize this literatures;The parts of HDW3 and HDW4 were separated by macroporous resin col umn chromatography, silica gel column chromatography, polyamide column chro matography, ODS column chromatography, Sephadex LH-20 gel column chroma tography, medium-pressure and high-performance liquid chromatography(HPLC)method. There were 20 monomeric compounds.Using thin layer chromatograph y(TLC) and high performance liquid chromatography(HPLC) method detected compounds’ purity. To identify the structure of these compounds by analysisin g their physical and chemical properties and these spectrums such as MS,1H-N MR,13C-NMR,1H-1H COSY,HSQC,HMBC.The study used on the A549,MCF-7,PLC and Hela cell to observe the anti-endometrial cancer activities of four monomeric compounds.Results: The parts of HDW3 and HDW4 were separated by various column chromatographies. At the same time we have isolated 20 kinds of compounds from the two parts and using the preparation of thin layer chromatograp hy, thepreparation of liquid chromatography to text the purity, and the followin g compounds were Hedyotis A, 2-hydroxy-3-methyl-1-methoxy anthraquinone, 2-hydroxy-3-methyl anthraquinone, quercetin,kaeperferol, stigmasterol, E-p-coumari c acid,p-hydroxybenzoic acid, trans-caffeic acid, ferulic acid, protocatechuic acid,3-methoxy 4-hydroxybenzoic acid, 4-hydroxy-6,7-hymethoxy-1-naphthoic acid,3,4-dihydroxybenzaldehyde, kaempfe-rol-3-O-β-D-sophorose, quercetin-3-O-[2-O-(6-O-E-sinapoyl)-β-D-glucopyranosyl]-β-glucopyranoside, quercetin-3-O-[2-O-(6-OE-feruloyl)-β-D-glucopyranosyl]-β-glucopyranoside, quercetin-3-O-[2-O-(6-O-E-fer uloyl)-β-D-glucopy-ranosyl]-β-galactopyranoside, kaeperferol-3-O-[2-O-(6-O-E-feru loyl)-β-D-glucop-yranosyl]-β-galactopyranoside, rutin。Conclusion:Exploring the chemical composition of water extract of Hedyot is diffusa Willd. by using all kinds of subjects and analytical methods.There ar e ganic compounds, flavonoids, anthraquinones, alkaloids and other compounds.The compound of 4-hydroxy-6,7-hymethoxy-1-naphthoic acid have no antitumor activity.The three phenolic compounds of kaempferol have significant antitumo r activity in vitro. It is for further study.