| Impatiens is an annual herb that has been used in Asian traditional medicine.The aerial parts of I.balsamina are traditionally used for the treatment of articular rheumatism,bruises and beriberi.Flowers are used to treat lumbago,neuralgia,burn and scald.Pharmacological active compounds derived from this plant include naphthoquinones,coumarins,phenolic acids,flavonoids,anthocyanidins,steroids and peptides.Recent studies have revealed that the extracts from its flowers exhibit anticancer,antimicrobial,antinociceptive,and antidermatitic activities.By means of many chromatographic methods,including the open column chromatography of silica gel,Sephadex LH-20,reversed phase ODS and semi-preparative HPLC,forty three compounds were isolated from the flowers of Impatiens balsamina(Linn).On the basis of physico-chemical data and spectral methods(1H-NMR,13C-NMR,HSQC,HMBC,CD and HR-ESI-MS),the structure of these compounds were identified as balsaminaces A-F(1-6),4-O-β-D-glucopyranosyl-2.6-dihydroxyphenylacetic acid(7),1,2-O-(4-dihydroxy-benzoyl)-2,4,6-trihydroxy phenylacetic acid(8),methyl 2-O-(4-hydroxybenzoyl)-2,4,6-trihydroxyphenylacetate(9),balsaminone D(10),balsaminone E(11),balsaminone B(12),2-methoxy-1,4-naphthoquinone(13),kaempferol(14),quercetin(15),apigenin(16),dihydromyricetin(17),myricetin(18),kaempferol-3-O-glucoside(19),quercetin-3-rhamnoside(20),myricetin-3-rhamnoside(21),kaempferol-3-O-rutinoside(22),rutin(23),kaempferol-3-O-α-rhamnoside-7,4-di-O-β-galactoside(24),tiliroside-7-O-β-D-glucoside(25),p-hydroxybenzoicacid(26),caffeic acid(27),p-hydroxycinnamic acid(28),ferulic acid(29),3-methoxy-4-hydroxyphenyl ethanol(30),gallic acid(31),6-O-(E)-p-hydroxy-cinnamoyl-β-D-glucose(32),6-O-(E)-p-hydroxy-cinnamoyl-α-D-glucose(33),autantiamide acetate(34)α-D-glucopyranosyl-(1→1’)-3’-amino-3’-deoxy-β-D-glucopyranoside(35),spinasterol(36).balsaminsides A-D(37-40),β-D-Glucopyranosiduronic acid,(3β)-17-carboxy-28-norolean-12-en-3-yl-O-β-D-glucopyranosyl-(1→2)-O-[β-D-xylop yranosyl-(1→4)](41),3-O-β-D-xylopyranosyl-(1→2)-β-D-glucopyranosyl-28-O-β-D-glucopyran-osyloleanolic acid(42),glycerol 9(E),11(Z),13(E)-octadecatrienoyl ester(43),of which 13 new compounds.The new structures 1-7 are depsides,10 and 11 are two new quinones,37-40 are novel triterpenoid saponins.Compounds 8,9,24,25,32-35,41-43 were obtained for the first time from the Impatiens balsamina.Analysis of the bioassay results showed the compounds had notable anti-hepatic fibrosis activity against murine Hepatic Stellate Cells(t-HSC/Cl-6)and anti-diabetics activity against α-glucosidase.Specifically,new compounds 5,10,11 showed significant inhibitory activity against t-HSC/Cl-6 cells with IC50 values of 42.12,30.54,40.67 μM respectively,while the IC50 values of positive control Silymarin was 202.34 μM.In addition,compounds 2,5,6 and 10 exhibited excellentα-glucosidase inhibitory activity.This article describes the first study investigating the activity of compounds isolated from the flowers of I.balsamina towards the treatment of hepatic fibrosis and diabetics.The antitumor mechanis of the compound 13 against 22RV-1 cells was detected by morphological analysis,flow cytometry,and Western blot.The results indicated that compound 13 induced apoptosis occurred via caspase 9 dependent pathway in a time-dependent manner.Pharmacokinetic characteristics of E5 was examined following oral and intravenous administration at a dose of 20 mg/kg to Sprague-Dawley rats.The pharmacokinetic study found that the absolute bioavailability was above 29.04%.Our results reveal that depsides,which are present in the flowers of I.balsamina,exhibit potential anti-hepatic fibrosis and anti-diabetic activities.We aslo investigate the antitumor mechanis of the compound 13 against 22RV-1 cells and also examined the pharmacokinetics of the compound in conjunction with assessing the in vivo activity. |
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