松潘乌头二萜生物碱的研究

甘肃省文县产的松潘乌头(Aconitum sungpanense Hand-Mazz),俗称缠绕乌头,民间用于治疗跌打损伤,风湿性关节痛等症。其化学成分尚未见报道。松潘乌头粗粉用0.5%的盐酸渗漉,通过阳离子树脂交换,经乙醚及二氯甲烷先后洗脱,乙醚部分用硅胶柱层析等     

Identification and Synthesis of Quinolizidines with Anti-Influenza A Virus Activity

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平贝母生物碱的分离和鉴定

自平贝母(Fritillaria ussuriensis Maxim)中分得四种生物碱。晶Ⅰ和晶Ⅱ是已知的生物碱,分别为西贝素和贝母辛。晶Ⅲ和晶Ⅳ是二个新的C-去甲-D-异甾体生物碱,分别命名为平贝碱甲和平贝碱乙。经制备衍生物和光谱分析推定平贝碱甲的结构为Ⅲ。平贝碱乙(熔点255～259℃,分子式C₂₇H₄₆O₆N)的结构尚在研究中。     

Stem bark alkaloids of Rauwolfia vomitoria

Forty-three indole alkaloids were isolated from 7 kg Rauwolfia vomitoria stem bark; 39 were identified and 2 partially characterised. At least 72 alkaloids classified into 19 types occur in the plant and the interrelationship of the alkaloids and their distribution throughout the plant has been discussed. The major alkaloids of the stems were heteroyohimbines (especially reserpiline) and N (a)-demethyldihydroindoles.     

Stem Bark Alkaloids of Rauwolfia vomitoria.

Forty-three indole alkaloids were isolated from 7 kg RAUWOLFIA VOMITORIA stem bark; 39 were identified and 2 partially characterised. At least 72 alkaloids classified into 19 types occur in the plant and the interrelationship of the alkaloids and their distribution throughout the plant has been discussed. The major alkaloids of the stems were heteroyohimbines (especially reserpiline) and N (a)-demethyldihydroindoles.     

Alkaloids from roots of Aconitum crassicaule

From the roots of ACONITUM CRASSICAULE, four diterpenoid alkaloids were isolated. Two of these were identified as chasmanine (5) and yunaconitine (4). The other two, Crassicauline A and Crassicauline B, are new alkaloids. The structure of crassicauline A, C (35)H (49)O (10)N, has been elucidated as structure (1) on the basis of chemical and spectral data, while the structure of crassicauline B, C (27)H (31)O (4)N, is still to be determined.     

Indole Alkaloids from Alstonia angustifolia

From the stem bark of ALSTONIA ANGUSTIFOLIA, eleven alkaloids were isolated. Seven of them are known ones: echitamine ( 1), N(b)-demethylechitamine ( 2), pseudoakuammigine ( 3), tubotaiwine ( 5), akuammicine ( 6), N(b)-beta-methylantirhine ( 12), and N(b)-methylakuammidine ( 13). The four others, pseudoakuammigine N-oxide ( 4), akuammicine N-oxide ( 7), N(b)-demethylalstogustine ( 8), and N(b)-demethylalstogustine N-oxide ( 11), are new alkaloids. Their structures were determined by means of spectroscopic analysis and chemical correlation with known alkaloids.     

New Polyindolenine Alkaloids from Calycodendron milnei

Four new alkaloids, representing the first members of new groups of polyindolinic alkaloids, have been isolated from the aerial parts of CALYCODENDRON MILNEI along with other alkaloids. The names vatine, its stereoisomer vatine A, vatamine, and vatamidine are proposed. They are polymers of six, seven, and eight N(b)-methyltryptamine units, respectively.     

Medicinal plants of surinam.

From ASPIDOSPERMA EXCELSUM, rootbark, which has previously been shown to exhibit antimicrobial activity, 6 antimicrobial active alkaloids were isolated and identified: 11-methoxytubotaiwine, ochrolifuanine A, tetrahydrosecamine, 16-demethoxycarbonyltetrahydrosecamine, 16-hydroxytetrahydrosecamine and 16-hydroxy, 16-demethoxycarbonyltetrahydrosecamine. The minimum inhibitory concentration was determined for some of the alkaloids, using BACILLUS SUBTILIS as test organism. Didemethoxycarbonyltetrahydrosecamine was also shown to exhibit antimicrobial activity. No activity against gram negative bacteria could be found for the alkaloids by means of biograms. The site of demethoxycarbonylation in demethoxycarbonyltetrahydrosecamine was established as C-16. The structures of the two new secamine type alkaloids, 16-hydroxytetrahydrosecamine and 16-hydroxy,16-demethoxycarbonyltetrahydrosecamine were determined by means of their spectral data. During the isolation of the antimicrobially active alkaloids some inactive alkaloids were also isolated: compactinervine, N (a)-acetylaspidospermidine, O-dimethylaspidospermine, aricine, yohimbine and O-acetylyohimbine.     

中国延胡索的研究 Ⅱ.江苏元胡中的生物碱

从江苏野生的延胡索(Corydalis humasa Migo)的块茎中,分得五种生物碱,其中三种巳鉴定为普鲁托品(protopine)、左旋四氢黄连碱和毕扣扣灵(bicuculline);其他二种为未知成分,暂命名为苏元胡碱甲和乙。苏元胡碱甲的实验式为C₂₃H₂₃O₇N,熔点205℃;苏元胡碱乙的实验式为C₁₈H₁₉O₆N,熔点191—192℃。     

Biological activities of steroidal alkaloids isolated from Solanum leucocarpum

The alkaloids demissidine, dihydrosolacongestidine, solasodine and tomatidine were isolated and identified by spectroscopic methods and by comparison with literature data, from the aerial part of Solanum leucocarpum Dunal (Solanaceae) collected at the Regional Natural Park Ucumarí (Colombia). In order to examine topoisomerase I and II activities, the four isolated alkaloids were tested through a mechanism-based bioassay utilizing genetically engineered mutants of yeast Saccharomyces cerevisiae strains RS322N, R52Y and RS321. Dihydrosolacongestidine showed selective activity towards RS321 (249.8 μg/mL) strain rather than RS322N (1542.7 μg/mL), most probably indicating activity through inhibition of DNA topoisomerase II. In the same manner, tomatidine displayed activity through DNA topoisomerase II inhibition. Furthermore, solasodine showed DNA-damaging activity. In addition, the same isolated alkaloids were tested for antibacterial activity by using the agar well diffusion method. Solasodine and dihydrosolacongestidine showed MIC values of 62.5 and 125 μg/mL against Staphylococcus aureus, respectively. The isolation of these alkaloids and their biological activities are reported here for the first time for S. leucocarpum.     

New indole N-oxide alkaloids from Evodia fargesii

Three new indole N-oxide alkaloids, fargesine (5-hydroxy-12-methyl-10,11,12,13-tetrahydro-1 H-azepino[5,4,3-cd]indole N(12)-oxide, 1), plectocomine 12-methyl-5- O-beta-D-glucopyranoside N(12)-oxide (2), and bufotenine 5-O-beta-D-glucopyranoside N(12)-oxide (3), were isolated from the root and stem of Evodia fargesii Dode along with five known compounds. The structures of the new alkaloids were elucidated on the basis of spectroscopic analysis.     

Two new methyl chanofruticosinates from Kopsia flavida blume

Two new indole alkaloids with the methyl chanofruticosinate skeletal system viz., methyl 3-oxo-12-methoxy- N 1 -decarbomethoxy-14,15-didehydrochanofruticosinate ( 1 ) and methyl 3-oxo-11,12-methylenedioxy- N 1 -decarbomethoxy-14,15-didehydrochanofruticosinate ( 2 ), together with four known compounds, methyl 12-methoxy- N 1 -decarbomethoxychanofruticosinate, methyl 12-methoxychanofruticosinate, methyl 11,12-dimethoxychanofruticosinate and methyl 11,12-methylenedioxy- N 1 -decarbomethoxychanofruticosinate, were isolated in continuing studies on the leaves of Kopsia flavida Blume. The structures of the new indole alkaloids were assigned by NMR spectral data using various 2D-techniques.     

几种制剂中生物碱的离子交换分离测定法

制剂中生物碱的含量測定,各国药典經典方法均采用有机溶剂提取,分离杂貭后再测定含量。近几年来,采用离子交换法分离制剂中生物碱的方法已有不少报导。由于离子交換剂能够比較簡单的定量交換生物碱,并可以用一定溶剂洗脫,这样可以避免一般較复杂费时的提取手續,因而采用离子交换法分离生物碱具有一定的优点。Kamp等报告了用IMAC-22強酸树脂,从顛茄、番木鱉等数种生药及其制剂中分离生物碱,对于用交換柱操作方法、洗脫条件等都进行一定工作。Brochmann-Hanssen連續报导了快速分离测     

小叶锦鸡儿种子中的生物碱及其细胞毒活性

目的鉴定小叶锦鸡儿种子中的生物碱类成分,研究其抗癌活性。方法采用色谱和光谱法对小叶锦鸡儿种子中所含有的总生物碱进行分离并作结构鉴定;对小叶锦鸡儿种子的总生物碱及分离得到的5个生物碱单体分别进行细胞毒活性筛选。结果从总生物碱中共分离得到了5个原小檗碱型生物碱,分别为去氢白莲叶碱、黄连碱、表小檗碱、脱氢卡维丁以及刻叶紫堇明碱,它们对Saos-2,A375,Hela细胞株均表现出明显的细胞毒活性。结论5个生物碱单体均为首次从锦鸡儿属植物中分离得到,提示小叶锦鸡儿种子提取物具有抗肿瘤的药用价值。     

马钱子生物碱在大鼠体内的组织分布

目的　研究马钱子生物碱在大鼠体内的组织分布。方法　大鼠静脉注射马钱子总碱后 ,定时用高效液相色谱法测定各组织中士的宁 (strychnine ,S)、马钱子碱 (brucine,B)、士的宁氮氧化物 (strychnineN oxide ,SNO)和马钱子碱氮氧化物(brucineN oxide ,BNO)的含量。结果　S、B、SNO和BNO在脑和脊髓中均有较多的分布。结论　S、B、SNO和BNO均可穿透血脑屏障 ,到达脑和脊髓 ,从而对中枢产生作用     

Alkaloids from Rauwolfia cubana Stem Bark

Six indole alkaloids, tetrahydroalstonine, aricine, 16- EPI-affinine, ajmaline, amerovolfine, and amerovolficine have been isolated from the ethanolic extract of the stem bark of RAUWOLFIA CUBANA A. DC. Amerovolfine ( N(alpha)-demethylaccedine) and amerovolficine (16-demethoxy-carbonylpagicerine) are new alkaloids related to 16- EPI-affinine, and their structures have been determined by spectroscopic analysis.     

Study on the Alkaloids of Melodinus tenuicaudatus

Fourteen alkaloids were isolated from the stem bark of MELODINUS TENUICAUDATUS Tsiang et P. T. Li. Eleven of them were identified as known alkaloids, namely, scandine ( 2), Delta (14)-eburnamine ( 4), vindolinine N(b)-oxide ( 5), 11-methoxytabersonine ( 6), vindolinine ( 7), EPI-vindolinine N(b)-oxide ( 8), hazuntine ( 9), compactinervine ( 10), 11-hydroxytabersonine ( 11), Delta (14)-vincine ( 12), and normacusine B ( 14). Two alkaloids were new: 10-hydroxyscandine ( 1), and the dimer, tenuicausine ( 3); their structures were elucidated by spectroscopic and chemical methods. One alkaloid ( 13) occurring in trace amounts, could not be identified.     

双稠吡咯啶生物碱的研究 Ⅰ.森林千里光的生物碱

从浙江天目山采集的森林千里光(Senecio nemorensis)中分得二个双稠吡咯啶类型的生物碱,其中之一熔点为55—57℃,分子式为C₁₃H₂₁O₃N。另一熔点为42—43℃,分子式为C₁₈H₂₇O₅N。由其理化常数及酒石酸盐、苦味酸盐、水解产物等结果,与文献上记载的大叶千里光中所得的macrophylline及从瓶草千里光中所得的sarracine比较,证明前者与macrophylline相同,而后者与sarracine相同。     

露蕊乌头生物碱的研究(Ⅰ)

从藏药露蕊乌头(Aconitum gymnandrum Maxim)中分得四个生物碱,经化学和光谱鉴定,其中两个为已知生物碱atisine.Hcl(A)和talatisamine(B),另两个为新的二萜类生物碱,分别命名为露乌碱,(C)(gymnaconitine)和甲基露乌碱(D)(mgthyl gymnaconitine),这两种新的生物碱均联接有二甲基咖啡酸酯:在乌头生物碱中是首次发现。