Studied On The Chemical Constituents And Bioactivities Of Cortex Phellodendron Chinenseis AND Coptis Chinensis Franch

Traditional Chinese medicine Cortex phellodendron Chinenseis is the dry bark of Phellodendron chinense Schneid,which is belonged to Rutaceal family.It has been widely used in heat-cleating and detoxicating,lowering the blood pressure,treating enteron ulcer,counteracting pathogen germ,et.al.In our previous researches,it was found that the alkaloid part of Coptis chinensis Franch has a good effect on lowering blood sugar.Protoberberine compounds are also the major components in Cortex phellodendron Chinenseis.The hypoglycemic effect has been evaluated for both the alkaloid part of Cortexphellodendron Chinenseis and Coptis chinensis Franch on normal mouse.Cortex phellodendron Chinenseis exhibited better activity than Coptis chinensis Franch.In recent ten years few researches on chemical constituents of Cortex phellodendron Chinenseis have been reported.So a further research on the chemical constituents and bioactivities of Cortex phellodendron Chinenseis is very important.40 compounds have been isolated from the 70%alcohol extraction of Cortex phellodendron Chinenseis.39 compounds of them were identified as:Bererine(1), Caffeic acid ethyl ester(2),lsovanillin(3),Ferulaic acid(4),(±)-5,5'-Dimethoxylariciresinol (5),Methyl orsellinate(6),γ-Fagirine(7),(±)-Lyoniresinol(8),β-Sitosterol (9),Stigmasterine(10),Jateorhizine hydrochloride(11),Palmatine(12),Columbamine (13),Phellodendrine(14),Campesterol(15),4-Hydroxybenzoic acid(16), 4-Hydroxyphenethanol(18),1-Methoxy-2-hydroxybenzoic acid(19),5-O-Fernloylquini acid(20),3-O-Fernloylquini acid(21),4-O-Fernloylquini acid(22),Methyl 3-O-fernloyl-quinate (23),Methyl 5-O-fernloyl-quinate(24),7R,8S-4,7,9,9'-Tetrohydroxy 3,3'- dimethoxy-8-O-4'-neoligan(25),7S,8R-4,7,9,9'-Tetrohydroxy-3,3'-dimethoxy-8-O-4'-neoligan(26),3',4-Di-O-methoxyl-cadrusin(27),Syringin(28),Caffeic acid(29), Triethylamine(30),Cinnamic acid(31),2,4-Dihydroxy-3,5-di-methylbenzoic acid(32), Fernloylbutyrate(33),Epiberberine(34),Berberine acetate(35),Beberastine(36), Synapylaldehyde(37),3,4,5-Trimethoxyphenyl-β-D-glucopyranoside(38),Ethyl orsellinate(39),3-O-Fernloyl-muco-quiniacid(40).Compounds 2-4,6,17-19,22,25,26, 27,29,31-33,35,37,39,40,41 were isolated for the first time from this genus.6 compounds were isolated from the alkaloid part of Coptis chinensis Franch.5 compounds were identified as:Bererine(1),Jaterorhizine(11),Palmatine(12),Coptisine (36),Tetrahydrocoptisine(16).Alkaloids constituents of Cortex phellodendron Chinenseis were compared with Coptis chinensis Franch by UV,HPLC and LC-MSⁿ,5 compounds from alkaloid part of Cortex phellodendron Chinenseis have been identified by LC-MSⁿ,which were Bererine (1),Jateorhizine(11),Palmatine(12),Berberrubine(42),Phellodendron A(43),6 compounds from alkaloid part of Coptis chinensis Franch have been identify by LC-MSⁿ, which were Bererine(1),Jaterorhizine(11),Palmatine(12),Coptisine(36),Epibererine (35) and Berberubine(42).Some of the isolated compounds have been made PTP1B enzyme activity screen.It was a pity that no one showed good activity.In addition,a series of Fernloylquinates have been isolated from Cortex phellodendron Chinenseis,which are formed by condensation of Quinic acid and Ferulic acid.While isolating,better separating effect could be obtained by using NH₄Cl in the mobil phase which inhibiting dissociation of carboxy group and phenolic hydroxyl group. Coupling was not clear in ¹H-NMR and signals in high field area were short in ¹³C-NMR, this might be coursed by conformation astable.¹H-NMR gave a much better crack in 70℃which confirmed our guess.Some regularity of Fernloylquinates in ¹H-NMR has been summarized.