Chemical Compositions Of Fallopia Multiflora Var. Cillinerve And Their Bioactivities

Fallopia multiflora var.cillinerve is a medicinally valuable perennial herb belongs to Fallopia Adans of Polygonaceae.It has a cool and bitter taste with clearing away heat,detoxification,removing rheumatism,cooling blood and strong waist.The roots are hypertrophic and ovate,its color of fresh cross-section similar to cinnabar.Therefore,it is known as“Zhu Sha Qi”,one of the Taibai“Qiyao”.The dried roots have been used traditionally in China for the treatment of quinsy,enteritis,gastritis diarrhoea,nephritis dropsy and allantois infection.However,there are very few studies on the chemical compositions of Fallopia multiflora var.cillinerve,and the reported compounds are only focus on terpenes,saponins,terpenoids,polyphenols,and polysaccharides.In order to further dig out the active ingredients in this plant,and make its medicinal purposes more useful,this paper studied the chemical constituents and biological activities of the roots of Fallopia multiflora var.cillinerve from Qinling Mountain systematically.The dried roots of 1.75 kg Fallopia multiflora var.cillinerve were extracted with 95%industrial alcohol,and the crude extracts obtained after concentration several times,then suspended in water and extracted with petroleum ether,ethyl acetate and n-butanol to afford the extracts.The three different polarities extracts were further separated and purified by silica gel column chromatography,Sephadex LH-20 and recrystallization.Finally,14 pure compounds were isolated and identified as:?-sitosterol?1?,Daucosterol?2?,Gallic acid?3?,Succinic acid?4?,Annulatin 3'-O-?-D-xyloside?5?,Erythritol?6?,?-D-glucose?7?,Inotodisaccharide?8?,Kaempferitrin?9?,Monobutyl 2-?4-hydroxybenzyl?tartrate?10?,Pyrrolezanthine-6-monobutyl-ether?11?,Methyl 2-?4-hydroxybenzyl?tartrate?12?,Piscidic acid?13?,n-butyl-?-D-fructopyranoside?14?by ESI-HR-MS,IR,UV,NMR,X-ray single crystal diffraction and other technologies.Compounds 11 and 12 were two new compounds,and 3¹4 were isolated from this plant for the first time.Four bacteria and seven plant pathogenic fungi used to test the antibacterial activity of the 14 compounds.The results showed that the flavonoids 5,9 and the new alkaloid 11 all showed a broad-spectrum antibacterial activity,Annulatin3'-O-?-D-xyloside exhibited antibacterial activity against Streptococcus lactis and Pyrrolezanthine-6-monobutyl-ether exhibited antifungal activity against Sclerotinia sclerotiorum with MIC value of 31.3?g·mL^-1.The antioxidation activity of compounds 3,5,9,10¹3 was tested by scavenging the DPPH radical.The results showed that the polyphenolic compounds 3 exhibited a stronger antioxidant activity than the positive control V_C with an IC₅₀0 value of 4.28?g·mL^-1.Flavonoids 5 and 9 also showed good antioxidant activity.However,due to different structures,antioxidation activity of 5 and 9 was different slightly.The?-glucosidase inhibition assay of the new alkaloid 11 was showed that the it did not show better?-glucosidase inhibitory activity.So whether there is an active ingredient which has a better?-glucosidase inhibitory activity to be further explored.