Studies On The Bioactive Constituents Of Agastache Rugosa And Syringa Oblata

This thesis consists of four chapters.The first chapter summarized the progress of chemicalconstituents and biological activities of Agastache genus.The second chapter studied the chemical constituents and coagulation activity of A.rugosa.The third chapter investigated the application of ionic liquid in extraction active ingredients tilianin and acacetin in A.rugosa.The fourth chapter studied chemical constituents from the Syringa oblata Lindl.Chapter 1.Advances of chemical constituents and biological activities of Agastache genusThe progress of chemical constituents and biological activities of Agastache genus weresummarized.Chapter 2.Chemical constituents and coagulation activity of Agastache rugosaThrough various column chromatography separation to elucidate the chemical constituents of A. rugosa,and then investigated the biological activity of the major constituents.Ten known compounds were isolated from the aerial parts of A.rugosa.Compounds 1¹0 were identified as methyl hexadecanoate（1）,β-sitosterol（2）,acacetin（3）,ursolic acid（4）,apigenin（5）,protocatechuic acid（6）,euscaphic acid（7）,β-daucosterol（8）,tilianin（9）,soybean cerebroside-?（10）.Compounds 1,6,7 and 10 were isolated from the Agastache genus for the first time,and 4 were obtained from the plant for the first time.The extracts and main composition of A.rugosa were evaluated for coagulation effect by assay activated partial thromboplastin time（APTT）,prothrombin time（PT）,thrombin time（TT）and fibrinogen（FIB）in vitro.The results showed that Ar.TE,Ar.Pe had a significant coagulant activity,and Ar.Ea and Ar.Bu possessed a certain procoagulant activity,while its main components,ursolic acid,acacetin and tilianin possessed significant anticoagulant activity.Apigenin,protocatechuic acid and most of the compounds had a certain anticoagulant activity in vitro,only euscaphic acid had coagulant activity.Chapter 3.Application of ionic liquid in extraction active ingredients in Agastache rugosaIonic liquid 1-butyl-3-methylimidazolium bromide-methanol-based ultrasonic-assisted extraction （ILUAE）was used to extract tilianin and acacetin from the aerial parts of Agastache rugose（A.rugose）,and simultaneously determined by reversed phase high performance liquid chromatographic（RP-HPLC）method with ultraviolet detection（RP-HPLC-UV）.A Inert Sustain RP-C₁₈ column was used with the mobile phase consisting of methanol and 0.2%acetic acid as gradient elution at the detection wavelength of332 nm.The flow rate was 0.8 mL/min,and the column temperature was 30°C.Under the optimized conditions,tilianin and acacetin displayed good linearity in the ranges of 0.0595-4.76μg/mL and0.0585-4.68μg/mL,respectively,with the average recoveries being 96.93%and 97.88%,respectively.The extraction conditions were optimized by single factor variable method.Under the optimal conditions,the content of tilianin and acacetin were 5.19 mg/g and 0.91 mg/g in dry sample.Chapter 4.Chemical constituents and hypoglycemic activity of Syringa oblata LindlThe chemical constituents from the S.oblate were studied by column chromatography.15compounds were isolated and identified as quercetin（1）,kaempferol-3-O-α-L-rhamnosyl-（1→6）-β-D-glucoside（2）,4-Hydroxyphenethyl alcohol（3）,vanillic acid（4）,caffeic acid（5）,dictamnoside A（6）,Lilacoside（7）,quercetin-3-O-β-D-glucoside（8）,rutin（9）,palmitic acid（10）,lauric acid（11）,oleanolic acid（12）,ursolic acid（13）,naringenin（14）,β-daucosterol（15）.Compounds 6,10,11 and 14 were isolated from Syringa genus for the first time.Compounds 1,2,4,5,8 and 9 were isolated from the plant for the first time.Different extracts and main compounds of S.oblata were assayed forα-glucosidase inhibitiory activity in vitro.The results showed that the extract of 40%ethanol,ursolic acid and oleanolic acid exhibited higherα-glucosidase inhibitiory activity than the positive control of acarbose.The extracts and main composition of S.oblate were assayed for coagulation activity in vitro.The results showed that the extract of water,the extract of 20%ethanol,lauric acid,kaempferol-rutinose had a significant coagulant activity,and the extract of water,lauric acid,and kaempferol-rutinose were similar to positive group Yunnan Baiyao.