蛇足石杉化学成分和药理作用研究进展

结合国内外文献综述蛇足石杉生物碱和三萜化学成分和药理作用,尤其重点归纳蛇足石杉石松生物碱的结构、类型。石杉碱甲为高选择性的乙酰胆碱酯酶抑制剂,优于国外已上市的老年痴呆症治疗药物,是首先从蛇足石杉中发现的lycodine生物碱类型,从蛇足石杉分离的该类型其他生物碱也具有较强的类似活性,具备进一步研究与开发的潜力。     

蛇足石杉生物碱成分的研究(Ⅵ)

蛇足石杉 H uperzia serratum( Thunb.) Trev.为石杉科石杉属植物 ,自从该植物中分得一个强效胆碱酯酶抑制剂福定碱即石杉碱甲 [1,2 ]以来 ,为进一步寻找生物活性成分 ,笔者又从中分得十几个生物碱成分[3～ 5] 。国内外文献报道及初步药理实验表明 ,具明显生理活性的化合物主要集中在类似 Selagine骨架的结构类型中 [6] 。笔者在继续寻找新的生理活性成分中 ,又分得 2个生物碱单体 (碱 和 ) ,经光谱鉴定分别为马尾杉碱 M和异福定碱 ,这两个化合物均为 Selagine型结构生物碱 ,并为首次从该植物中分得。初步药理实验表明 ,碱 也有较好的…     

中药石杉碱的苯并等排物的合成

石杉碱甲和乙是从中药蛇足石松(Lycopodium serratum Thunb)中分离得到的二个石松属生物碱,结构式为:这一生物碱具有抗胆碱酷酶作用,能增进实验性动物的记忆力。本文旨在改变其结构,以苯环代替其中的毗吮酮环,借以说明毗吮酮环是否为其     

藤石松的生物碱类成分研究

目的 研究藤石松Lycopodiastrum casuarinoides的生物碱类成分。方法 利用多种色谱方法对藤石松总生物碱部位进行分离纯化。通过多种波谱技术以及单晶X-射线衍射鉴定化合物的结构。结果 从藤石松全株植物中分离到11个化合物,分别鉴定为6-羟基-β-玉柏碱（1）、去-N-甲基-β-玉柏碱（2）、casuarine B(3)、石杉碱乙（4）、casuarinine B(5)、β-玉柏碱（6）、蛇足石杉碱（7）、N-demethylhuperzinine(8)、石杉碱丙（9）、8,15-dihydrohuperzinine(10)、casuarinine I(11)。结论 化合物1为新的石松碱类化合物。     

千层塔的生药学鉴定

<正> 千层塔之名早见于《植物名实图考》,《高等植物图鉴》称为蛇足石松。秦仁昌教授命名为蛇足石杉,其学名为Huperzia serrata(Thunb.)Trev.。《全国中草药汇编》仍用千层塔之名,并云千层塔为民间药。有散瘀消肿、解毒,止痛功能,用于瘀血肿痛,内伤吐血等。近年来从千层塔分离到石杉碱甲(Huperzine A),具有很强的抑制胆碱酯酶的活性,它对128例重症肌无力症的治疗有效率高达99.2％。另外石杉碱甲对老龄大鼠的学习、记忆保持的改善作用好。石杉碱甲是值得推广的胆碱酯酶的抑制药,它有可能用于临床治疗老年人的记忆减退和早、中期老年性痴呆。为了保证千层塔的化学、药理及临床研究的需要,我们对千层塔进行     

蛇足石杉生物碱成分的研究(Ⅳ)

从石杉科植物蛇足石杉中分离出二个生物碱,经光谱鉴定分别为６－β－羟基石杉碱甲和马尾杉碱Ｎ。这两个化合物均首次从该植物中得到。生物实验初步结果表明,６－β－羟基石杉碱甲为又一个强效胆碱酯酶抑制剂,其毒性低于石杉碱甲,而对电鳐ＡＣｈＥ的抑制作用比石杉碱甲强约４倍。     

石杉碱甲的药理作用与临床研究进展

千层塔是我国沿用了上千年的中草药,其有效成分石杉碱甲具有增强记忆,抗老年性痴呆的作用。本文综述了石杉碱甲药理特点与临床研究进展。     

产生物碱和石杉碱甲蛇足石杉内生真菌的初步研究

 目的 筛选产生物碱和石杉碱甲的内生真菌。方法 以分离自健康蛇足石杉植株组织中的14株内生真菌为材料,采用酸性染料比色法筛选产生物碱的菌株;在此基础上,对内生真菌发酵液进行HPLC测定,分析是否产生石杉碱甲;并利用形态学和rDNA ITS序列分析进行菌种的初步鉴定。结果 筛选出8株产生物碱的菌株,并从中筛选出一株产生石杉碱甲的内生真菌SY-02,初步鉴定内生真菌SY-02为1株炭角菌。结论 在分离自蛇足石杉的内生真菌中,能产生生物碱的真菌比例较高,内生真菌菌株SY-02能在发酵条件下产生石杉碱甲。以产生物碱的菌株为出发菌株,结合活性及结构检测,可以使产石杉碱甲内生真菌的筛选更具有方向性。     

双苄基异喹啉类生物碱的生物活性及其国内资源

  本文综述了双苄基异喹啉类生物碱的生物活性及其国内资源的最近研究概况。分析了天然 存在的双苄基异喹啉类生物碱的结构类型和特点以及生物活性的主要方面，介绍了国内植物资源分布 和利用情况，重点反映了千金藤素、小檗胺、粉防己碱、防己诺林碱、左旋箭毒碱、轮环藤宁和箭毒 碱等生物碱的药理临床研究进展。     

UFLC法测定蛇足石杉不同部位的石杉碱甲含量

<正>石杉碱甲是20世纪80年代我国学者从蛇足石杉中分离得到的一种新型石松类生物碱,被广泛用于治疗阿尔茨海默症、重症肌无力,同时又能促智、提高青春期学生的学习记忆功能[1]。目前测定蛇足石杉不同部位提取物中生物碱含量的方法主要为反相高效液相色谱法(RP-HPLC)[2],尚无超高效液相     

Antiophidic solanidane steroidal alkaloids from Solanum campaniforme

Three new solanidane alkaloids bearing a 22,23-epoxy ring (1-3) and four known compounds were isolated from leaves of Solanum campaniforme. The structures were determined using spectroscopic techniques, including 1D and 2D NMR, and HRESIMS experiments. The antiophidic activity of the alkaloids was tested against Bothrops pauloensis venom. Compounds 1-3 completely inhibited myotoxicity without inhibiting phospholipase A2 activity of the venom, while hemorrhage and skin necrosis were significantly reduced in the presence of alkaloids 1 and 2.     

Diterpenoid alkaloids from the lateral root of Aconitum carmichaelii

Twenty-six new diterpenoid alkaloids, 1-26 (1-4: hetisan-type C(20)-diterpenoid alkaloids; 5-26: aconitane C(19)-diterpenoid alkaloids), and two known analogues, hypaconitine 27 and benzoylmesaconine 28, have been isolated from a water extract of the lateral root of Aconitum carmichaelii. Compounds 7 and 8 are rare examples of conformational isomers obtained from the same material. The conformation and conformational transformation of ring A in the C(19)-diterpenoid alkaloids are discussed on the basis of NMR data analysis in combination with single-crystal X-ray crystallography of 6 and 27 by anomalous scattering of Cu Kα radiation. In preliminary analgesic and toxicity assays, the isomer with ring A in the chair conformation (8 or 27) was found to be more active than that with ring A in the boat conformation (7 or 27a). In addition, 15, 16, and 19 showed neuroprotective activity.     

Triterpenoidal alkaloids from Buxus natalensis and their acetylcholinesterase inhibitory activity

Acetylcholinesterase (AChE) inhibition-directed phytochemical studies on the methanolic extract of Buxus natalensis, collected in South Africa, resulted in the isolation of 12 compounds: O(2)-natafuranamine (1), O(10)-natafuranamine (2), cyclonataminol (3), 31-demethylbuxaminol A (4), buxaminol A (5), buxafuranamide (6), buxalongifolamidine (7), buxamine A (8), cyclobuxophylline K (9), buxaminol C (10), methyl syringate (11), and p-coumaroylputrescine (12). Compounds 1-4 were new alkaloids, and compound 5 was isolated for the first time as a natural product. Their structures were elucidated with the aid of extensive NMR and mass spectroscopic studies. Compounds 1 and 2 are members of a rarely occurring class of Buxus alkaloids, having a tetrahydrofuran ring incorporated in their structures. Compounds 1-12 exhibited strong to moderate AChE inhibitory activity.     

New alkaloids from Pandanus amaryllifolius

Three new alkaloids, the two pyrrolidine type alkaloids (1 and 2) and 6E-pandanamine (3), together with five known alkaloids (4-8), were isolated from the leaves of Pandanus amaryllifolius collected in West Java, Indonesia. All the new alkaloids have two alpha-methyl alpha,beta-unsaturated gamma-lactone moieties, while compound 2 also has an additional seven-membered ring, which has not been encountered before in Pandanus alkaloids. Two different extraction methods, namely, a solvent partitioning extraction and acid-base treatment, were tested, giving secondary and tertiary amines, respectively. Spectroscopic and chemical studies showed that the tertiary amines isolated from the acid-base treatment were artifacts formed during the extraction process. This finding suggests that the use of conventional acid-base treatment in isolating Pandanus alkaloids should be reviewed since it can introduce artifacts.     

Triazole and dihydroimidazole alkaloids from the marine sediment-derived fungus Penicillium paneum SD-44

A novel triazole carboxylic acid, penipanoid A (1), two new quinazolinone alkaloids, penipanoids B (2) and C (3), and a very recently reported quinazolinone derivative (4) were isolated from the marine sediment-derived fungus Penicillium paneum SD-44. Their structures were elucidated by spectroscopic analysis, and the structure for 1 was confirmed by X-ray crystallographic analysis. Compound 1 represents the first example of a triazole derivative from marine sediment-derived fungi, and compound 2 is a rare quinazolinone derivative having a dihydroimidazole ring system. The cytotoxicity of compounds 1 and 4 and the antimicrobial activity of 1-4 were evaluated.     

海南地不容生物碱抑制肿瘤细胞增殖及构效关系解析

目的研究海南地不容(Stephania hainanensis H. S. Lo et Y. Tsoong)生物碱对人肝癌细胞Hep G-2、乳腺癌细胞MCF-7、胃癌细胞SGC-7901增殖的影响,筛选出有效的抗肿瘤化合物以及其敏感细胞株;分析其生物碱的构效关系。方法采用MTT法检测不同浓度的海南地不容生物碱对人肝癌细胞Hep G-2、乳腺癌细胞MCF-7、胃癌细胞SGC-7901增殖的抑制率;通过查阅国内外相关文献,分析海南地不容生物碱抗肿瘤活性的基本构效关系。结果 MTT结果显示荷包牡丹碱、氧化克班宁、去甲荷包牡丹碱和克班宁对人肝癌Hep G-2、乳腺癌MCF-7和胃癌SGC-7901细胞的增值分别具有不同程度的剂量依赖性的抑制作用,各给药组分吸光度值与空白对照组比具有显著性差异(P <0. 01),与阳性对照比较无明显统计学差异(P> 0. 05);海南地不容生物碱结构中的1,2-亚甲二氧基、N-亚甲基等取代基以及其化学结构的平面性对其抗肿瘤活性有重要影响。结论海南地不容中具有明显抗肿瘤作用的生物碱为荷包牡丹碱、氧化克班宁、去甲荷包牡丹碱和克班宁,其敏感细胞株均为乳...     

Tripfordines A-C, sesquiterpene pyridine alkaloids from Tripterygium wilfordii, and structure anti-HIV activity relationships of Tripterygium alkaloids

Three new sesquiterpene pyridine alkaloids, tripfordines A-C (1-3), were isolated from an ethanolic extract of the roots of Tripterygium wilfordii, along with eight known pyridine alkaloids, and tested for in vitro cytotoxic and anti-HIV activity. The structures of the new compounds were established on the basis of spectroscopic data interpretation. Anti-HIV structure-activity relationships (SAR) for this compound type are proposed on the basis of the screening results from the newly isolated compounds and prior data of known sesquiterpene pyridine alkaloids. The position of a carboxyalkyl chain on the pyridine moiety was not critical since both 2'- and 4'-substituted compounds exhibited high anti-HIV activity (EC(50) 0.1 microg/mL). In contrast, a hydroxy group at C-8' (carboxypropyl side chain) or C-9' (carboxybutyl side chain) was found to affect anti-HIV activity.     

南海海绵Axinella sp.中两个含吡咯七元环内酰胺生物碱的分离鉴定

从中国南海采集的海绵Axinella sp.中分离得到两种化合物,经MS,NMR等光谱技术确定其结构分别为Hymenialdisine(1),Debromohymenialdisine(2)。这两种化合物系首次从中国海洋生物中分离得到,均为含吡咯七元环内酰胺的生物碱类化合物,都是MAPK途径抑制剂,有较高的生物活性。     

Daphnipaxianines A-D, alkaloids from Daphniphyllum paxianum

Four new Daphniphyllum alkaloids, daphnipaxianines A-D ( 1- 4), along with six known ones, have been isolated from the leaves and fruits of Daphniphyllum paxianum. Daphnipaxianines A and B ( 1, 2), a pair of epimers differing at C-10, are the first caliciphylline A type Daphniphyllum alkaloids with a Delta (9(15))-unsaturated cyclic ketone unit, and daphnipaxianine D ( 4) is the first yuzurine-type Daphniphyllum alkaloid containing a hexacyclic ring system. The structures of these alkaloids were characterized by spectroscopic methods, especially 2D NMR techniques. A single-crystal X-ray diffraction analysis was used to confirm the structure of 1.     

骨痛膜对兔膝关节骨性关节炎血清中SOD、NO、HA含量影响的实验研究

目的探讨骨痛膜对兔实验性膝关节骨性关节炎血清中超氧化物歧化酶(SOD)活性及透明质酸(HA)、一氧化氮(NO)含量的影响。方法将日本大耳白兔随机分成正常组、模型组、治疗组、对照组、基质组,除正常组外均行右股静脉结扎法造模。造模5周后各组采用相应的方法进行治疗,3周后将动物处死,取血清检测SOD活性、HA及NO的含量。结果模型组血清中SOD活性明显下降,对照组、治疗组SOD活性升高;模型组血清中HA含量明显升高,对照组、治疗组HA含量明显下降;模型组血清中NO含量明显升高,对照组、治疗组NO含量明显下降。结论骨痛膜能提高OA滑膜组织中SOD的活性,减少HA及NO的含量,抑制氧自由基对软骨细胞及基质的损害,改善关节软骨的血液循环,从而对关节软骨起到保护作用,从而防治膝关节骨性关节炎。