Red Polo Spent Chemical Composition And Biological Activity

Incarvillea delavayi,a member of the genus lncarvillea(Bignoniaceae),is mainly distributed in Yunnan and Sichuan provinces.It is often treated as ornamental plant because of its beautiful flowers.Recently,the Incarvillea species have been found to be a rich source of actinidine-type monoterpenoid alkaloids,and possess significant antinociceptive activity.It was also reported that some monoterpen alkaloids and iridoids have been isolated from I.delavayi.In this dissertation,we investigate the chemical constituents of the whole plant of Incarvillea delavayi systematically,anti-inflammatory,analgesic and cytotoxic activitities.Thirty-seven compounds were isolated from the whole plant of Incarvillea delavayi by silica gel,Sephadex LH-20,ODS,HPLC,PTLC and Pre-HPLC chromatography,and thirty-three compounds were identified as follows by spectral analysis:Delavatine A(1),Delavatine B(2),△⁵-dehydroskytanthine N-oxide(3),Isoincarvilline(4), Incarvine D(5),Incarvillic acid(6),Incarvilleaol(7),delavayol(8),Incarvialdehyde(9), (+)-6-hydroxy-1-methyl-2,3-dihydro-1H-Indene-4-carboxaldehyde(10),Cleroindicin B(11), Cleroindicin F(12),Rengyol(13),2-(1,4-dihydroxyl cyclohexyl)ethyl caffeate(14), Isoacteoside(15),Osmanthuside B₆(16),Plantainoside C(17),Isomartynoside(18), Isocrenatoside(19),3"'-O-methylisocrenatoside(20),quercetin(21), quercetin-7-O-α-L-rhamnoside(22),ethyl caffeate(23),p-coumaric acid(24),Ferulic acid(25), 3-O-methyl-4-hydroxy benzoic acid(26),o-cresol(27),daucosterol(28),β-sitosterol(29),oleanolic acid(30),ursolic acid(31),(2S,3R)-2,6-dimethyl-1,8-octanediol(32),hexacosoic acid(33).Among them,compounds 1-4,6-10,14,20 were determined as new compounds,among which compound 9 possessed a new carbon skeleton,compounds 11-13,15-19,21-27,32 were isolated from the genus Incarvillea(Bignoniaceae)for the first time,compounds 5,28-31,33 were isolated from this plant for the first time.In analgesic activity test of crude extract,four extractive fractions from this plant,the results showed that the crude extract,high-dosed chloroform fraction and high-dose EtOAc fraction displayed significant analgesic activity in vivo with asprin as control.In anti-inflammatory test of crude extract,four extractive fractions from this plant,the results showed that crude extract,chloroform fraction and EtOAc fraction displayed anti-inflammatory activity in vivo with asprin as control.Some compounds were also evaluated for cytotoxicity by MTT assay.The results indicated that the new alkaloid,namely compound 1 showed potent inhibition against 5 human cancer cell lines,A549,LOVO,HL-60,6T-CEM and HepG-2.Compound 2,another new alkaloid,showed medium inhibitory effect against HL-60 and compound 12 only showed cytotoxic effect against special human cancer cells.Conclusion:37 compounds were obtained from Incarvillea delavayi,including 11new compounds,16 compounds were isolated from this genus for the first time,and 6 compounds from this plant for the first time.On the basis of bioassay,it was found that crude extract,high-dosed chloroform fraction and high-dose EtOAc fraction displayed analgesic activity,while crude extract, chloroform fraction and EtOAc fraction showed anti-inflammatory activity.Compound 1 demonstrated significant cytotoxic effect against human tumor cell lines tested.