| Urticae Fissae Radix is the dry root of Urtica fissa E.Pritz.In Europe,America and other countries,OTC has been developed for the treatment of benign prostatic hyperplasia(BPH)with other Urtica plants.However,the research on the inbibitory BPH ingredients in Urticae Fissae Radix is not reported yet.In the present study,the material basis of Urticae Fissae Radix for BPH inhibition was investigated for the first time.1.Screening of the BPH inhibitory fractions in Urticae Fissae Radix.Firstly,the active fractions of Urticae Fissae Radix were screened with 5α-reductase as the target.The results showed that the extracts of dichloromethane and ethyl acetate had the siginificantly inhibitory activity of 5α-reductase,while the extracts of petroleum ether,n-butanol and water layer had the weak inhibition on reductase activity.Further experiments in vivo confirmed that dichloromethane and ethyl acetate fractions had the good anti-BPH effects.They could significantly decrease the wet weight of the prostate,the index of the prostate,the thickness of the epithelial cells of the prostate.So,dichloromethane and ethyl acetate fractions were regarded as the active fractions for the furher reasearch.2.Investigation on the chemical constituents of the active fractionsTh e chemical constituents in the fractions of dichloromethane and ethyl acetate were systematically investigated by silica gel column chromatography(CC),ODS CC,HPLC,and identified by NMR,MS methods.As results,33 compounds were obtained: dibutyl-O-phthalate(1),β-sitosterol(2),8’-acetyl oilvil(3),4-methoxyl-8’-acetyl oilvil(4),1-monolinolein(5),vanillic acid(6),epipinoresinol(7),5-hydroxy-3,4-dimethyl-5-pentanyl-2(5H)-furanone(8),E-7,9-diene-11-methenyl palmitic acid(9),stearic acid(10),glycerol(11),erythritol(12),evofolin B(13),ficusal(14),β-hydroxypropiovanillone(15),threo-2,3-bis(4-hydroxy-3-methoxy phenyl)-3-ethoxypropan-1-ol(16),p-hydroxybenzaldehyde(17),pinoresinol(18),α-viniferin(19),(9R,7E)-9-hydroxy-5,7-mengatigmadien-4-one-9-O-β-D-glucopyra noside(20),7-hydroxy-6-methoxycoumarin(21),indole-3-carboxaldehyde(22),phydroxy ethyl cinnamate(23),erythro-1,2-bis-(4-hydroxy-3-methoxyphenyl)-1,3-propanediol(24),urticol(25),urticol-7-O-β-glucopyranoside(26),benzyl alcohol-O-β-D-glucopyranoside(27),L-methionine(28),lobechine methyl(29),lobechine(30),4-methoxyaniline(31),thymine(32),6-aminopurine(33).Compound 3 was a new compound,compound 29 was a new natural product and compounds 1,5,7-9,11,13-16,19-24,27,28,31,33 were isolated from U.fissa for the first time.3.The active evaluation of the constituents in vivoFinally,the active components in vivo were studied by LC-Q-TOF-MS technique.After the blood was taken from the orbit,three components β-hydroxypropiovanillone,ficusal,α-viniferin were identified in the blood,using the purified compounds as the reference substances.The inhibitory effect of α-viniferin and β-hydroxypropiovanillone on 5α-reductase is stronger.The inhibitory effect of ficusal on the activity of 5α-reductase was weak.The results provide a scientific basis for the treatment of benign prostatic hyperplasia with Urticae Fissae Radix. |
