Study On Chemical Constituents And Screening Inhibiting PTP1B Of Active Components Of Dysoxylum Lukii Merr

Dysoxylum lukii Merr is a plant belonging to the species of genus Dysoxylum.The tetranortriterpenoids are considered to be the important constituents,some studies have demonstrated that its stem contains constituents which have anti sugar active.In this paper many constituents were isolated,purified and identificated,and main studies were about screening the chemical of inhibiting proteintyrosine phosphatase-1b of active.The paper selects Dysoxylum lukii Merr of medicinal plants as the research object,The compounds were isolated and purified by silica gel column chromatography,Sephadex LH-20 and semi-preparative HPLC.Base on HR-ESI-MS and NMR,their structures were identified.Thirty-four compounds were isolated and identification from Dysoxylum lukii Merr,which were thirty triterpenes,one sterides,one diterpene,one fatty acid and so on.It specifically includes 23S-21,23-epoxy-5α-cycloart-24-en-3β-ol(1),trans-phytol(2),2,3-seco-2-oxoolean-12-en-3-methylester-30-oic acid(3),2,3-secooxoolean-12-ene-2,3,28-trioic acid 3-methyl ester(4),3β-hydroxyolean-12-en-28-oic acid(5),3-hydroxy-3,4-seco-lup-3(24)-ene-3-methoxy group-30-acetyl(6),3-oxoolean-12-en-30-oic acid(7),aphanamgrandin J(8),2,3-seco-oxoolean-4,12-diene-23-aldehyde(9),12E-dien-19-oic acid(10),methyl manevalate(11),4,14-dimethyl-cholest-9(11)-en-3-ol(12),lup-20(29)-en-3β-ol(13),4-hydroxy-3,4-seco-lup-20(29)-ene-30-aldehyde-3 oic acid(14),2α-formyl-A(1)norlup-20(29)-en-28-oic acid(15),3,4-seco-lupa-4(23),20(29)-dien-3-ol(16),oleanolic aldehyde(17),3,4-seco-lup-4(23)-en-3-al(18),20-hydroxy-3,4-seco-lup-4(23)-en-3-aldehyde(19),lupeol acetate(20),dysoxyhainic H(21),lupa-1,20(29)-dien-28-al(22),3β,29-dihydroxy-olean-12-en-28-oic acid(23),hydrocarbon(24),3-hexadecenoic(25),canaric acid methyl ester(26),dysoxylukiine C(27),dysoxyhainic acid G(28),2,2’-oxybis(1,4-di-tert-butylbenzene)(29),morolic acid(30),3-oxo-olean-12-en-29-oic acid(31),30-hydroxylup-20(29)-en-3-one(32),4,20-dyhydroxy-3,4-seco-lup-3-acetyl(33),4-hydroxy-3,4-seco-20(29)-en-lup-30-aldehyde-3-methoxy ester(34).Based on the above experimental results,the inhibitory activity of the chemical components on PTP1 b was determined by enzymatic hydrolysis in vitro.Experimental results showed that eight chemical constituents indicated a certain enzyme inhibition activity,half of which inhibited IC50 value range 0.96-37.43 μM.The structure-activity relationship showed that lupane may be the key parent nucleus of these compounds to inhibit the activity of PTP1 b.The ring opening of the parent nucleus and with an electron donor group all were lead to the decrease of the inhibitory activity.Finally,the chemical constituents and pharmacological activities of the genus Melia were summarized.This review shows that the chemical composition of the genus Aralia is abundant,it possess a well excavation value.