Study On The Chemical Constituents And Biological Activities Of Sambora Chinensis

Trigonostemon lutescens is a species of the genus Trigonostemon from Euphorbiaceae.There are about 50 species of the genus T in the world,mainly distributed in the tropical and subtropical regions of Asia.Among them,there are about 10 species in China,and.lutescens is a unique plant in Guangxi.In China and Thailand,the genus T.is a folk medicine that has anti-inflammatory,antispasmodic,antidiarrheal and therapeutic effects on snake bites.Recent studies have found that there are many novel structural chemical components in this genus,including diterpenoids.alkaloids and other types of compounds,which have various biological pharmacological activities such as insecticidal,antitumor,antiviral and antibacterial activities.The genus T.is a kind of medicinal plant resource with high development value.According to the previous research of our group,we found that the main active ingredients were concentrated in the ethyl acetate extract.In order to further explore the pharmacodynamic basis of this plant,we selected the medium and large polarity of the ethyl acetate extract,the chemical composition study and the corresponding pharmacological activity studies were carried out at the site.In this experiment,many chromatographic techniques such as silica gel column chromatography,Sephadex LH-20 gel column chromatography,MCI column chromatography,rapid medium pressure preparative column chromatography,semi-preparative HPLC,etc.were used to isolate and purify the medium and large polar parts of the ethyl acetate extract.The structures of nineteen compounds,according to the spectral data(IR,UV,CD,ORD,MS,ID and 2D NMR),combined with their physical and chemical properties,then by comparison of literature datas,were identified as:Iutescin A(1),lutescin B(2),3'-methoxy-ellagic acid-4-rhamnoside(3),3,3',4-O-trimethyl ellagic acid(4),1-O-?-D-glucopyranosyl-4-allylbenzene(5),3,4-dihydroxyallylbenzene-4-O-?-D-glucopyranoside(6),lyciumide A(7),N-tranns-Feruloyltyramine(8),7,8-dihydroxy-4-hydrofuroquinoline(9),8-hydroxy-3-methoxy-5H-pyrido[2,1-c]pyrazin-5-one(10),3-Formylindole(11),umtatin(12),curdionolide A(13),(-)-loliolide(14),(+)-dehydrovomifoliol(15),1-(2-ethylphenyl)-1,2-ethanediol(16),syringaldehyde(17),clove acid(18),vanillic acid(19).Among them,compounds 1 and 2 are new compounds,which is the first time that ellagitannins have been reported in T.species.The compounds 1-3,7-13,16,18 are isolated from the genus T.for the first time.Compounds 14,15,19 were isolated from this plant for the first time.The structure of compound 7 was obtained by the mixed analysis of spectra.The chemical shifts of the 1H and 13C NMR of compound 8 and the corresponding integral ratios were combined with the HRESIMS,then by comparison of the literature data,the structure otf compound 7 was successfully identified.This mixed analytical method which based on ID NMR and MS has a certain guiding significance tor the analysis of the mixture which is difficult to purify in separation of phytochemistry.The anti-tumor activity of the isolated compounds was screened by CCK-8 method.The results showed that compounds 1,2,4,9 and 12 showed effective inhibition to HCT116 cells.MELA cells and HepG2 cells.Their function showed a dependence with concentration.Cmpounds 1 and 2 showed significant growth inhibition to LHCT116 cells with IC50 values of 16.58 ± 0.84 and 18.94±0.21 ?g/mL,respectively.Compounds 1,2,4 and 12 showed significant growth inhibition to HELA cells with IC50 values of 16.02±0.74,15.88 ± 0.27,13.60±0.81 and 15.48 ± 0.59 ?g/mL,respectively.Compounds 1 and 2 showed significant growth inhibition to HepG2 cells with IC50 values of 13.70±0.42 and 10.82±0.58 ?g/mL,respectively.