龙州山橙的生物碱类成分研究

对龙州山橙的生物碱类成分进行研究。采用硅胶柱色谱、反相柱色谱、高效制备液相等方法,对龙州山橙的总生物碱进行分离和纯化,并通过1H,13C-NMR,MS等波谱方法鉴定化合物的结构。该研究共分离得到7个生物碱类化合物,分别为scandine(1),tabersonine(2),melodinine N(3),melodinine P(4),melodinine T(5),19-epimeloscandonine(6),16-hydroxy-19 S-vindolinine(7)。化合物均1~7为首次从该植物中分离得到。采用MTT法对分离得到的化合物进行体外抗肿瘤活性评价,发现化合物1~7均表现出一定的体外细胞毒活性。     

景东山橙中生物碱类化学成分

目的:夹竹桃科(Apocynaceae)山橙属(Melodinus)植物在我国民间应用的历史悠久,其生物碱类化学成分具有抗肿瘤、抗菌、抗生育等生物活性。该文对夹竹桃科山橙属植物景东山橙(Melodinus khasianus)中生物碱类化学成分进行系统研究。方法:运用硅胶柱色谱、反相硅胶柱色谱及高效液相制备色谱对景东山橙中生物碱类化学成分进行分离和纯化,并通过其理化性质及波谱数据确证生物碱类化合物的结构。通过噻唑蓝(MTT)比色法,对分离得到的化合物进行前列腺癌细胞(PC-3),肺癌细胞(A549),胃癌细胞(HGC-27)和人白血病细胞(HL-60)的细胞增殖抑制筛选。结果:从景东山橙乙醇提取物的三氯甲烷部位分离得到12个化合物,分别鉴定为(+)epi-16α-hydro-14,15vincamine(1),16β,21β-epoxy-vincadine(2),melodinines G(3),melodinines P(4),melodinines N(5),16β-hydroxy-19S-vindolinine(6),16β-hydroxy-19R-vindolinine(7),15α-hydroxy-14,15-dihydrovindolinine(8),melodinines T(9),19-epimeloscandonine(10),门洛斯坎刀尼(11),攀援山橙碱(12)。结论:其中化合物1~10为首次从景东山橙中分离得到的生物碱。采用MTT比色法对化合物进行体外抗肿瘤活性筛选,发现化合物4,5对前列腺癌细胞(PC-3),肺癌细胞(A549),胃癌细胞(HGC-27)和人白血病细胞(HL-60)等肿瘤细胞具有一定的细胞增殖抑制作用。     

苦豆子种子生物碱类化学成分及细胞毒活性

目的:研究苦豆子种子的化学成分并对其抗肿瘤活性进行测试。方法:采用常规的硅胶柱层析(CC),葡聚糖(Sephadex LH-20)柱层析,和重结晶等实验手段对其进行了分离纯化,利用波谱技术(1H-NMR,13C-NMR)及与文献数据对照,对分离的化合物进行了结构鉴定;并采用MTT测定部分生物碱单体化合物体外对C6肿瘤细胞的细胞毒活性。结果:共分离出7个生物碱类化合物,分别鉴定为:苦参碱(1),氧化苦参碱(2),槐果碱(3),9α-羟基槐果碱(4),氧化槐果碱(5),9α-羟基槐胺碱(6),(-)-13,14-去氢槐定碱(7),1个非生物碱化合物3-吲哚甲醛(8)。结论:化合物8为首次从该属植物中分离得到。细胞毒活性测试结果表明,化合物1~3和5对鼠脑胶质瘤C6细胞显示了较强的生长抑制活性。     

从糖胶树树皮中分得2个新的生物碱

对印尼产糖胶树Alstonia scholaris R．Br．树皮中所含生物碱的研究鲜有报道。作者从该植物树皮中分离出1新的吲哚生物碱（1）、1新的糖生物碱（2）和5个已知生物碱（3～7）。并对这7个化合物进行了抗疟活性研究。     

狗牙花生物碱成分分析

目的:对夹竹桃科狗牙花属植物中狗牙花的生物碱类化学成分进行分离并对分离得到的化合物进行结构鉴定。方法:将干燥狗牙花3.5 kg粉碎,加甲醇室温渗漉提取,收集渗滤液,将渗滤液减压浓缩得到浸膏。浸膏用2 mol·L~(-1)硫酸调节p H 2,加入乙酸乙酯萃取得到非碱性脂溶性成分浓缩物;萃取后的酸水液用氢氧化钠溶液调节p H 9~10,然后用三氯甲烷萃取,得到总生物碱10 g。通过硅胶柱色谱,小孔凝胶(MCI)柱色谱和LH-20羟丙基萄聚糖凝胶(Sephadex LH-20)柱色谱进行分离和重结晶技术纯化,应用TLC监测,分离得到纯度较高的单体化合物。利用现代波谱法结合理化分析对其化学结构进行进一步鉴定。结果:从狗牙花中共分离得到并鉴定了6个单吲哚生物碱,分别鉴定为ervaramine型:ervatamine(1),20-epiervatamine(3);vobasine型:tabernaemontanine(2),dregamine(4);aspidosperma型:(-)-mehranine(5),tetrahydroalstonine(6)。结论:化合物4,6为首次从该植物中分离得到。MTS法测定化合物的肿瘤细胞毒活性,化合物1~6对5种人体肿瘤细胞株(人早幼粒白血病细胞HL-60,人肝癌细胞SMMC-7721,人肺癌细胞A-549,人乳腺癌细胞MCF-7,人结肠癌细胞SW-480)未显示出细胞毒活性。     

无花果内生真菌FL10中吲哚二酮哌嗪类生物碱的研究

目的:研究无花果内生真菌FL10的次级代谢产物成分.方法:采用反复硅胶柱色谱法、Sephadex LH-20凝胶色谱法等进行分离纯化,从无花果内生真菌FL10的发酵液中分离得到6个吲哚二酮哌嗪类生物碱.结果:通过理化常数测定和光谱分析,6个吲哚二酮哌嗪类生物碱鉴定分别为verruculogen(1),cyclotryprostatins B(2),fumitremorgin C(3),cyclotryprostatin A(4),tryprostatin A(5),tryprostatin B(6).结论:这6个吲哚二酮哌嗪类生物碱是首次从无花果内生真菌中分离得到,目前研究表明,无花果内生真菌Aspergillus tamarii可以作为一种可产生吲哚二酮哌嗪类生物碱的新来源.     

马钱子属Strychos decussata(Pappe)Gilg的新吲哚生物碱,decussine的肌肉松弛活性

Strychnos decussata(pappe)Gilg是一种小树或灌木,主要分布于东南非和马达加斯加,属马钱科。曾发现其氯仿生物碱部分有强的肌肉松弛活性。以前从它的茎皮中分离出5种叔吲哚生物碱有致痉作用。最近Petitjean从这种植物的叶中分离出一种葡萄糖生物碱。本文所报道的decussine是一种新的叔吲哚生物碱,体内、体外试验表明有肌肉松弛活性。将1975年11月从肯尼亚卡拉瓦采集的植物茎皮(5公斤)粉碎,用1％醋酸于室温下搅拌提取二次,合并滤液,用5％盐酸酸化至pH2,加入Mayer试剂至不再出现沉     

齐藤凹顶藻的化学成分研究

目的:研究齐藤凹顶藻Laurencia saitoi化学成分,并对单体化合物进行细胞毒活性筛选.方法:采用正相硅胶柱色谱、Sephadex LH-20凝胶色谱、重结晶等方法进行分离纯化;应用MS,1D和2D NMR等波谱学方法鉴定结构;通过MTY法对单体化合物进行细胞毒活性测试.结果:从齐藤凹顶藻中分离并鉴定了7个化合物,分别为aplysistatin(1),5-acetoxy-palisadin B(2),palisadin B(3),palisadin A(4),pacifigorgiol(S),豆甾4-烯-3α,6β-二醇(6),2,3,5,6-四溴-吲哚(7),其中化合物1～5为倍半萜类化合物,化合物6为甾醇类化合物,化合物7为四溴取代的吲哚类化合物.对化合物在人肿瘤细胞株Bel-7402,BGc-823模型上进行了细胞毒活性测定,IC_(50)均大于10μg·mL~(-1).结论:所有化合物均为首次从该种海藻中分离得到,但对人肿瘤细胞株Bel-7402,BGc-823均无明显活性.     

橙花瑞香茎中酚性成分研究

目的:研究橙花瑞香茎的酚性成分。方法:采用硅胶柱层析与凝胶柱色谱进行分离与纯化,并运用核磁共振和质谱等波谱方法鉴定化合物的结构。结果:从橙花瑞香茎的乙醇提取物中分离得到16个化学成分,包括10个木脂素类成分:(-)-罗汉松脂素(1)、7-羟基扁柏脂素(2)、4-O-去甲基橡胶素(3)、(-)-荜澄茄素(4)、3-甲氧基-3′,4′-(亚甲二氧基)-9,9′-环氧木脂素-4,7′-二醇(5)、(2S,3S)-3-(1,3-苯并二氧戊环-5-亚甲基)-1-(3,4-二甲氧苯基)-2-(羟甲氧基)-1,4-丁二醇(6)、异荜澄茄素(7)、2-(α-羟藜芦基)-3-藜芦基-1,4-丁二醇(8)、瑞香酮(9)、(S)-3-羟基-1,5-二苯基-1-戊酮(10);2个双黄酮类:毛瑞香素A(11)和狼毒素(12);4个香豆素:6-羟基-香豆素(13)、7-羟基-香豆素(14)、异莨菪亭(15)、6,8-二羟基-7-甲氧基-香豆素(16)。结论:所有化合物均为首次从该植物中分离得到。     

尖山橙枝叶化学成分研究

目的研究尖山橙Melodinus fusiformis枝叶非生物碱部位的化学成分。方法采用柱色谱进行分离,通过理化性质和光谱数据鉴定结构。结果从尖山橙枝叶甲醇提取物的醋酸乙酯部位分离得到28个化合物,分别鉴定为oleanderolide(1)、麦珠子酸(2)、3β-acetoxylup-20(29)-ene(3)、11,12-去氢乌索酸内酯(4)、齐墩果内酯(5)、24R-乙基-5α-胆甾烷-3β,6α-二醇(6)、(+)-松脂酚(7)、8α-羟基松脂酚(8)、番木鳖苷A(9)、紫云英苷(10)、α-tocopherol(11)、butyl isobutyl phthalate(12)、11-羟基柳叶水甘草碱(13)、(+)-voaphylline(14)、丁香树脂酚(15)、(+)-1-羟基丁香树脂酚(16)、(+)-fraxiresinol(17)、1-(4-hydroxy-3,5-dimethoxyphenyl)-hexahydro-1H-cyclopentafuran-4-o(l 18)、(±)-acyloxy enone(19)、2-羟基苯甲酸(20)、邻苯二甲酸二丁酯-N,N-二乙基-2-羟基苯甲酰胺(21)、6-羟基吲哚(22)、1,3-二油酸甘油酯(23)、邻苯二甲酸二丁酯(24)、双(2-乙基丁基)对苯二甲酸酯(25)、(6Z,8E,17E)-icosa-6,8,17-trien-lo-ol(26)、β-谷甾醇(27)、乌索酸(28)。结论尖山橙化学成分复杂多样,所分离的成分中有26个化合物(1～12、15～28)为首次从该植物中获得。     

樗鸡化学成分的研究

 目的：从樗鸡(Lycorma delicatula White)体中分离制备两种吲哚类生物碱,并鉴定其结构。方法：用溶剂和离子交换柱进行提取和纯化,用制备型高效液相色谱分离制备,用光谱法(¹H-NMR,¹³C-NMR,¹H-¹HCOSY,MS,DEPT)和化学方法对其进行结构鉴定。结果：分离得到两种生物碱,经鉴定其结构分别为 β-育亨宾和阿马里新。结论：两种生物碱在本种昆虫体中均为首次报道。     

不同因子对长春花愈伤组织中药用成分积累的影响

 目的 研究继代次数、继代龄(继代组织块的年龄)、生长素、金属离子等因子的改变对长春花愈伤组织生长及吲哚生物碱类药用成分积累的影响。方法 测定不同因子的影响下,长春花愈伤组织的鲜重,并对吲哚总碱进行提取、含量测定和比较。结果 随继代次数的增加,长春花愈伤组织中吲哚总碱含量有所下降;20 d继代龄最利于组织生长;2,4-二氯苯氧乙酸的存在对吲哚总碱的积累有一定的抑制作用,但却有利于愈伤组织生长,两种生长素组合比单一的生长素更利于组织生长,也较利于吲哚总碱积累;钙离子浓度为220 mg·L^-1,锌离子浓度为8.6哗·L^-1时,对提高吲哚总碱产量最有效。结论 继代次数、继代龄、生长素、金属离子对长春花愈伤组织生长及吲哚生物碱类药用成分的积累有较大影响。     

5-hydroxytryptamine-derived alkaloids from two marine sponges of the genus Hyrtios

Indonesian specimens of the marine sponges Hyrtios erectus and H. reticulatus were found to contain 5-hydroxytryptamine-derived alkaloids. Their structures were determined on the basis of their spectral properties. H. erectus contained hyrtiosulawesine (4), a new beta-carboline alkaloid, together with the already known alkaloids 5-hydroxyindole-3-carbaldehyde (1), hyrtiosin B (2), and 5-hydroxy-3-(2-hydroxyethyl)indole (3). H. reticulatus contained the novel derivative 1,6-dihydroxy-1,2,3,4-tetrahydro-beta-carboline (11) together with serotonin (5), 6-hydroxy-1-methyl-1,2,3,4-tetrahydro-beta-carboline (7), and 6-hydroxy-3,4-dihydro-1-oxo-beta-carboline (9).     

Indole alkaloids from Geissospermum reticulatum

Ten indole alkaloids were isolated from Geissospermum reticulatum, seven (1-7) from the leaves and three (8-10) from the bark. Seven were aspidospermatan-type alkaloids (1-3, 5-9), including four (5-8) with a 1-oxa-3-cyclopentene group in their molecule, which we named geissospermidine subtype. Compounds 1-3, 5-8, and 10 had not been reported previously as natural products, while 4 and 9 were the known alkaloids O-demethylaspidospermine and flavopereirine. Their structures were determined by spectroscopic techniques including 1D and 2D NMR experiments (COSY, NOESY, HSQC, HMBC). Additionally, X-ray crystallographic analyses of 1, 2, and 6 were performed. Antiparasitic activities of the ethanolic and alkaloidal extracts and of the pure alkaloids were tested against Trypanosoma cruzi and Leishmania infantum. In general, the extracts exhibited selective action and were more active against Leishmania than against Trypanosoma. Alkaloid 4 was also very active against L. infantum.     

Isolation of talathermophilins from the thermophilic fungus Talaromyces thermophilus YM3-4

Six indole alkaloids with various levels of prenylation were isolated from the thermophilic fungus Talaromyces thermophilus strain YM3-4. Their structures were identified by NMR and MS spectroscopic analyses. Compounds 1 and 2 are new analogues of the key versatile precursor notoamide E. Compound 3 is a novel analogue of preechinulin, and compound 4 was reported as a natural occurring cyclo(glycyltryptophyl) for the first time. The metabolite profile of this thermophilic organism displayed a biosynthetic pathway for talathermophilins.     

Biologically active aspidofractinine alkaloids from Kopsia singapurensis

Ten new indole alkaloids of the aspidofractinine type, in addition to several recently reported indole alkaloids and 20 other known alkaloids, were obtained from the leaf and stem-bark extract of the Malayan Kopsia singapurensis, viz., kopsimalines A-E (1-5), kopsinicine (6), kopsofinone (7), and kopsiloscines H-J (8-10). The structures of these alkaloids were determined using NMR and MS analysis. Kopsimalines A (1), B (2), C (3), D (4), and E (5) and kopsiloscine J (10) were found to reverse multidrug-resistance in vincristine-resistant KB cells, with 1 showing the highest potency.     

Indole alkaloids from three species of the Ervatamia genus: E. officinalis, E. divaricata, and E. divaricata Gouyahua

Six new indole alkaloids, 14,15-didehydro-10,11-dimethoxy-16-epivincamine (1), 14,15-didehydro-10-hydroxy-11-methoxy-16-epivincamine (2), 14,15-didehydro-10,11-dimethoxyvincamine (3), 14,15-didehydro-10-hydroxy-11-methoxyvincamine (4), 19,20-didehydro-6alpha-hydroxyervatamine (5), and dehydroxyervataminol (6), along with 36 known indole alkaloids, were isolated from three species, E. officinalis, E. divaricata, and E. divaricata Gouyahua, of the Ervatamia genus. The structures of these alkaloids were characterized on the basis of spectroscopic methods and chemical correlation. The in vitro cytotoxic activities of all the alkaloids except 7, 18, 27, 38, 40, and 44 against the tumor cell lines P-388 murine leukemia and A-549 human lung carcinoma were evaluated. Only the dimeric indole alkaloids showed cytotoxic activities.     

Indole alkaloids and other constituents of Rauwolfia serpentina

From the dried roots of Rauwolfia serpentina were isolated five new indole alkaloids, N(b)-methylajmaline (1), N(b)-methylisoajmaline (2), 3-hydroxysarpagine (3), yohimbinic acid (4), isorauhimbinic acid (5), a new iridoid glucoside, 7-epiloganin (6), and a new sucrose derivative, 6'-O-(3,4,5-trimethoxybenzoyl)glomeratose A (7), together with 20 known compounds. The structures of the new compounds were determined by spectroscopic and chemical means. The inhibitory activities of the selected alkaloids on topoisomerase I and II and their cytotoxicity against the human promyelocytic leukemia (HL-60) cell lines were assessed.     

灯台树叶中鸭脚树叶碱型生物碱

目的：研究云南当地药材灯台树的化学成分．方法：运用硅胶柱色谱分离，光谱技术（核磁共振，红外，紫外和质谱）鉴定结构。结果：从灯台树叶中分离到4个鸭脚树叶碱类型的单萜吲哚生物碱：5β-methoxyaspidophylline（1），鸭脚树叶碱（2），鸭脚树叶醛（3），5-methoxystrictamine（4）．结论：1是一个新化合物.     

New alkaloids of the sarpagine group from Rauvolfia serpentina hairy root culture

Three new monoterpenoid indole alkaloids, 19(S),20(R)-dihydroperaksine (1), 19(S),20(R)-dihydroperaksine-17-al (2), and 10-hydroxy-19(S),20(R)-dihydroperaksine (3), along with 16 known alkaloids 4-19 were isolated from hairy root culture of Rauvolfia serpentina, and their structures were elucidated by 1D and 2D NMR analyses. Taking into account the stereochemistry of the new alkaloids and results of preliminary enzymatical studies, the putative biosynthetical relationships between the novel alkaloids are discussed.