Chemical Composition Of Embelia Ribes And Hypericum Uralum And Their Biological Activities

This thesis is composed of three chapters.Chapter one described the chemical constituents and related biological activities of Embelia ribes.Chapter two elaborated the chemical constituents and biological activity of Hypericum uralum.Chapter three reviewed the research progress about Embelia plants.Objective: To study the chemical constituents and biological activities of two medicinal plants,E.ribes and H.uralum.Methods: The compounds were separated and purified by various chromatographic techniques,and their structures were elucidated by physicochemical properties and spectroscopic data.In addition,the analgesic experiments and anti-malarial experiments were used to study the activities of related components.Results: Six compounds were isolated from 95% ethanol extract of aerial part of E.ribes,and these compounds were identified as ?-sitosterol(1),stigmasterol(2),daucosterol(3),catechin(4),rutin(5),and isoquercetin(6).In the acetic acid writhing test in mice,the analgesic rate of the total extract from the aerial part of E.ribes was 47.78% at the dose of 1000 mg/kg,and the analgesic rates of ethyl acetate fraction,n-butanol fraction and water fraction from the aerial part of E.ribe were 51.00%,51.00% and 48.28% respectively at the dose of 500 mg/kg,and the analgesic rates of mixture 1 and 2,compounds 3,4,5 and 6 were 40.00%,22.89%,55.26%,44.21% and 29.74% respectively at the dose of 100 mg/kg.In the hot water tail-flick test in mice,the increase rates of pain threshold of mixture 1 and 2,compounds 3,4 and 5 were 26.09%,31.71%,8.70% and 13.72% respectively at the dose of 100 mg/kg.Eight compounds were obtained from the 95% ethanol extract of the underground part of E.ribes,and the compounds were identified as ?-sitosterol(1'),stigmasterol(2'),daucosterol(3'),rutin(4'),(+)-lyoniresinol-3?-O-?-D-glucopyranoside(5'),catechin(6'),embelin(7'),and 2,5-dihydroxy-3-tridecyl-1,4-benzoquinone(8').The inhibitory activities of compounds 3',4',6' and 7' on ?-hematin formation showed that the activities of the four compounds were weak.The average inhibition rate of compound 7' in antimalarial experiments in vivo was 54.53% at the dose of 100 mg/kg/day.The inhibition rate of compound 7' in acetic acid writhing test in mice was 82.74 % at the dose of 50 mg/kg.The increase rate of pain threshold of compound 7' in the hot water tail-flick test in mice was 134.37% at the dose of 50 mg/kg.Nineteen compounds were obtained from the 95% ethanol extract of H.uralum,and they were identified as(-)-eriodictyol(1),quercetin(2),epicatechin(3),3,4,5-trihydroxy xanthone(4),1,7-dihydroxy xanthone(5),4-hydroxy-2,3-dimethoxy xanthone(6),toxyloxanthone B(7),1,3,6,7-tetrahydroxy xanthone(8),2,3-dimethoxy xanthone(9),1,5,6-trihydroxy-3-methoxy xanthone(10),hyperielliptone HD(11),3,3',4,4'-tetrahydroxybi-phenyl(12),shikimic acid(13),daucosterol(14),stigmasterol(15),?-sitosterol(16),betulinic acid(17),quercetin-3-O-(4''-methoxy)-?-L-rahmnopyranosyl(18),and proanthocyanidin A-2(19).The analgesic rates of compounds 5 and 18,isolated from H.uralum,were 22.56% and 50.89% respectively in acetic acid writhing test in mice at the dose of 50 mg/kg.Compounds 5 and 18 have no activities in the hot water tail-flick test in mice at the dose of 50 mg/kg.Conclusion: The components of aerial part of E.ribes have good analgesic activities.Compound 4,isolated from the aerial part of E.ribes,has the best activity in the acetic acid writhing test in mice.Mixtures 1 and 2,compounds 3 and 5,isolated from the aerial part of E.ribes,showed some analgesic activities in hot water tail-flick test in mice.Compounds 3',4',6' and 7',isolated from the underground part of E.ribes,showed weak inhibitory activities on ?-hemin formation inhibitory activity.Compound 7' showed good activity in the study of anti-malarial activity in vivo and strong activities in analgesic experiment.In acetic acid writhing test in mice,the analgesic rates of compound 18 isolated from H.uralum at the dose of 50 mg/kg showed similar activity to the positive drug at the dose of 200 mg/kg.