【作者】 王珏；

【导师】 黄帅；

【作者基本信息】 西南交通大学 ， 生物工程（专业学位）， 2021， 硕士

【摘要】 全球乌头属植物共有400多种,其中有76种在我国被作为民族药治疗跌打损伤、风寒湿痹、类风湿性关节炎等疾病。白喉乌头为乌头属植物,分布于我国新疆、甘肃西北部,生长于海拔1400-2550米间的山地草坡或山谷沟边,因具有祛风除湿、消肿止痛的功效被哈萨克族作为民族药。国内外对白喉乌头中化学成分已有文献报道,目前已从白喉乌头中分离得到35个二萜生物碱,包括19个C₁₈-二萜生物碱、9个C₁₉-二萜生物碱和7个C₂₀-二萜生物碱。但白喉乌头中活性成分尚不明确,资源尚未得到合理开发,因此本论文选取白喉乌头为研究对象,研究其化学成分及生物活性。本论文通过酸提碱沉法制备白喉乌头根中总生物碱,结合正反相硅胶柱层析对总生物碱中单体化合物进行分离纯化,通过HR-ESI-MS,1D NMR和2D NMR鉴定化合物结构。从白喉乌头中分离共得到19个二萜生物碱和1个香豆素类化合物。其中3个新化合物命名为leucostosine A（1）,leucostosine B（2）和leucostosine C（3）,化合物1和3为新的高乌宁碱型C₁₈-二萜生物碱,化合物2为新的乌头碱型C₁₉-二萜生物碱。已知化合物包括2个冉乌宁碱型C₁₈-二萜生物碱leuconine（4）和leucostomine C（6）,2个高乌宁碱型C₁₈-二萜生物碱delphicrispuline（14）和N-deacetyllappaconitine（17）,7个乌头碱型C₁₉-二萜生物碱aconitine（5）、chasmaconitine（7）、14-acetyl-8-methyltalatisamine（10）、brochyponine A（11）、cammaconine（12）、mesaconitine（15）和pseudaconine（16）,3个牛扁碱型C₁₉-二萜生物碱delvestidine（13）、dehydroacosanine（18）和delphatine（19）,2个纳哌啉型C₂₀-二萜生物碱songoramine（8）和songorine（9）,1个香豆素类化合物bergapten（20）。化合物7、8、10、11、12、14、16和19为首次从该植物中分离得到。为寻找具有潜在生物活性的化合物,对分离得到的部分二萜生物碱进行体外抗乙酰胆碱酯酶活性、抗炎活性、抗肿瘤活性及对甜菜夜蛾的拒食活性研究。研究表明,所测二萜生物碱均表现较弱抗乙酰胆碱酯酶活性、抗炎活性、抗肿瘤活性。化合物2和13对甜菜夜蛾具有良好的拒食活性,其EC₅₀分别为1.54 mg/cm²和2.82 mg/cm²。更多还原

【Abstract】 Aconitum（Ranunculaceae）is a large genus comprising 400 species,and about 76Aconitum species in China are used as folk medicines,which are mainly used for the treatment of rheumatoid arthritis and various types of pains.Aconitum leucostomum Worosch grows at altitudes 1400–2550 m and distributes in the Gansu and Xinjiang provinces of China,which is belonging to the Aconitum genus.Aconitum leucostomum Worosch has been used as folk medicines in Kazak,which has the functions of dispelling wind and dehumidifying,reducing swelling and relieving pain.The isolation of thirty-five diterpenoid alkaloids from this plant had been reported,including nineteen C₁₈diterpenoid alkaloids,nine C₁₉diterpenoid alkaloids and seven C₂₀diterpenoid alkaloids.However,the active constituents in Aconitum leucostomum Worosch are not clear yet.Therefore,Aconitum leucostomum Worosch was selected as the study object,sthdied on chemical constituents of Aconitum leucostomum Worosch and their biological activities.The alkaloids in the root of Aconitum leucostomum Worosch were obtained by acid extraction and alkali precipitation.Compounds of alkaloid part were separated and purified by various separation methods.Their structures were elucidated on the basis of extensive spectroscopic analyses such as HR-ESI-MS,1D NMR and 2D NMR spectra.Nineteen diterpenoid alkaloids and one coumarin compound were isolated from Aconitum leucostomum Worosch.Three new compounds were named leucostosines A-C（1-3）,compounds 1 and 3 were new lappaconine-type C₁₈-diterpenoid alkaloid,and compound 2was a new aconitine-type C₁₉-diterpenoid alkaloid.The known compounds include two ranaconine-type C₁₈-diterpenoid alkaloid:leuconine（4）and leucostomine C（6）,two lappaconine-typeC₁₈-diterpenoidalkaloid:delphicrispuline（14）and N-deacetyllappaconitine（17）,seven aconitine-type C₁₉-diterpenoid alkaloid:aconitine（6）,chasmaconitine（8）,14-acetyl-8-methyltalatisamine（10）,brochyponine A（11）,cammaconine（12）,mesaconitine（15）,pseudaconine（16）,three lycoctonine-type C₁₉-diterpenoid alkaloid:delvestidine（13）,dehydroacosanine（18）,delphatine（19）,and two napelline-type C₂₀-diterpenoid alkaloid:songoramine（8）and songorine（9）,bergapten（20）.Compounds 7,8,10,11,12,14,16 and 19 were isolated from this plant for the first time.In order to search for potential bioactive compounds,some of the diterpenoid alkaloids were tested for their anti-acetylcholinesterase activity,anti-inflammatory activity,anti-tumor activity and antifeedant activity.All tasted diterpenoid alkaloids show weak activity,except compound 2 and compound 13 showed strong antifeedant activity against Spodoptera exigua Hübner(EC₅₀values of 1.54 mg/cm²and 2.82 mg/cm²).更多还原