文冠果果壳中一个新生物碱

目的研究文冠果果壳的化学成分。方法通过硅胶柱色谱、制备型薄层色谱进行化合物的分离，利用多种波谱技术鉴定化合物结构。结果分离得到10个化合物，鉴定为：2-甲基-6-(2′，3′，4′-三羟基丁基)吡嗪(I)、cleomiscosin D(II)、柚皮素(III)、圣草素(IV)、山柰酚(V)、槲皮素(VI)、芦丁(VII)、5，7-二羟基色原酮(VIII)、酪醇(IX)、1-O-甲基-肌-肌醇(X)。结论化合物I为一新化合物；化合物II，IV，V和VII～X均为首次从该属植物中分离得到。     

中药附子成分研究——Ⅰ.去甲猪毛菜碱(salsolinol)的分离及其结构测定

中药附子是乌头属植物Aconitum carmichaeli Debx.的子根,具有温中散寒镇痛,回阳救逆强心作用,临床用于治疗休克和慢性心率失常等疾病。陈嬿和岩佐准三曾先后报道从川乌、附子中得到一些二萜类生物碱,但这些成分还不能完全解释附子的药效。1978年,小管卓夫报道从同属植物日本附子(A. japonicum Thumb.)中分得去甲乌药碱(hig-     

东风桔吖啶酮生物碱

自东风桔(Atalantia buxifolia)根分得11个化合物。经光谱分析和化学反应证明其中—新化合物结构为N-甲基-1,3-二羟基-2,5,6-三甲氧基吖啶酮-9,命名为东风桔碱。     

莫达非尼对1-甲基-4苯基-1,2,3,6-四氢吡啶所致的帕金森病的神经保护作用

目的　观察莫达非尼对 1 甲基 4苯基 1,2 ,3,6 四氢吡啶 (MPTP)诱导的帕金森病 (PD)模型的神经保护作用。方法给C5 7BL 6小鼠腹腔注射MPTP4d制备PD模型 ,与MPTP同时给予莫达非尼 (ip ,5 0or10 0mg·kg- 1 ·d- 1 ) 4天后 ,再连续给莫达非尼 10天。观测莫达非尼对小鼠的自发活动 ,震颤潜伏期、维持期和震颤评分及爬杆时间的影响 ,及对纹状体和黑质的酪氨酸羟化酶 (TH)阳性细胞和尼氏体的影响。测定纹状体中多巴胺 (DA) ,去甲肾上腺素 (NA)和 5 羟色胺 ( 5 HT)含量。结果　莫达非尼 ( 5 0和 10 0mg·kg- 1 )呈剂量依赖性显著减少了自发活动、震颤和爬杆的行为缺陷 (P <0 .0 5和P <0 .0 1,n =10 ) ,阻止了MPTP造成的TH和尼氏体数量的减少 (P <0 .0 5 ,n =10 ) ,及纹状体中DA ,NA和 5 HT含量的降低 (P <0 .0 5 ,n =10 )。结论在MPTP诱导的PD小鼠模型中 ,莫达非尼可改善MPTP引起的帕金森病行为缺陷 ,且对单胺能神经细胞的损伤有保护作用。     

豹皮菌中氨基酸类成分的研究

从豹皮菌Amanita panthorina新鲜子实体的乙醇提取物中分离得到了4个氨基酸类化合物(I～IV)。根据光谱分析及理化性质,鉴定Ⅰ的结构为3-amino-2-hydroxypentandioicacid,Ⅱ为2-amino-3-(1,2-dicarboxyethylthio)propanoicacid。其中I为一新化合物,Ⅱ是首次从该菌中提取得到的。药理实验证明Ⅰ及Ⅱ分别是谷氨酸NMDA受体兴奋剂及阻断剂。     

MPTP诱导小鼠肝脏帕金森病样病理变化研究

目的 研究1-甲基-4-苯基-1,2,3,6-四氢吡啶(1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine,MPTP)诱导的帕金森病(Parkinson's disease,PD)小鼠模型中肝脏生理功能变化和病理改变.方法 将雄性C57BL/6小鼠随机分为空白对照组和模型组,皮下注...     

取代2—羟甲基苯甲酰胺和1—亚氨基—1,3—二氢异苯并呋喃的合成

取代苯酞在三乙胺/三氯化铝存在下氨解生成取代2-羟甲基苯甲酰胺(3)和1-亚氨基-1,3-二氢异苯并呋喃(4),苯酞3-位以环状/非环状基团取代可能影响反应过程和产物的生成,当回流反应时只生成产物4,不生成产物3,且4的收率很低,1-苄亚氨基-3-,二取代-1,3-二氢异苯并呋喃在空气中能缓慢氧化为相应氢过氧化物,氢过氧化物结构用光谱法,化学分析法和单昌X-射线衍射确证,并推测了生成氢过氧化物的机理,化合物7米的1H-NMR表示6,34处有一单峰,归属为PhCHOOH氢质子,HMBC表明92\81处有吸收峰,归属为NCH(OOH)Ph碳质子,IR表明845cm^-1有吸收峰,归属为-O-O-吸收.     

四倍体板蓝根中的两个新生物碱

目的　研究四倍体菘蓝Isatis indigotica Fort.根的化学成分。方法　应用硅胶柱色谱对乙酸乙酯萃取部分中化学成分进行分离纯化,根据理化常数测定和光谱(IR, MS, ¹HNMR, ¹³CNMR, 2DNMR)分析技术鉴定结构。 结果　从乙酸乙酯萃取部位分离得到4种生物碱类化合物,分别鉴定为：色胺酮(I), 2,5-二羟基吲哚(II), 2,3-二氢-4-羟基-2-氧-吲哚-3-乙腈(III),吲哚-3-乙腈-6-O-β-D-葡糖苷(IV)。结论　II为首次从该种植物中分离得到,III,IV为新化合物。     

MPTP诱导野生型和A53T转基因型小鼠帕金森病模型纹状体中神经递质变化

目的 探究帕金森病(Parkinson's disease,PD)小鼠模型纹状体中多巴胺等神经递质的变化.方法 通过腹腔注射丙磺舒(probenecid)、皮下注射1-甲基-4-苯基-1,2,3,6-四氢吡啶(1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine,MPTP)制备PD野...     

巴戟天抗衰老活性成分研究(Ⅱ)

目的对巴戟天(Morinda officinalis How.)的活性部位进行化学成分研究。方法用色谱法分离,用波谱法对化合物结构进行鉴定。结果从巴戟天活性部位中分出7个化合物,分别为1-羟基-2-羟甲基蒽醌(1)、1-羟基-6-羟甲基蒽醌(2)、1-羟基-7-羟甲基蒽醌(3)、3-羟基-1,2-二甲氧基蒽醌(4)、2-羟基-3-甲基蒽醌(5)、2-甲氧甲酰基蒽醌(6)、1,2-二羟基-3-甲基蒽醌(7)。结论化合物6为首次从该属分离得到,化合物2、3为首次从该种分离得到,首次提供化合物2的核磁数据。     

纵条矶海葵对高血压大鼠的降压作用

采用监测大鼠颈动脉血压、心电图和呼吸、观察纵条矶海葵提取物对自发性高大鼠及不同因素所致正常大鼠血压变化的影响，以探讨其抗高血压作用。结果显示，纵条矶海葵对正常大鼠及高血压大鼠均有一定的降低血压效应，对心率无明显影响，其降压作用有量效关系，未见有快速耐受现象，不影响肾上腺素、苯肾小腺素、血管紧张素Ⅱ及垂体后叶素对大鼠血压的反应性。提示纵条矾海葵有抗血压作用，且降压时肯反射性增快心率、其降太效应与直接     

Structures of sea anemone toxins

Sea anemones produce a variety of toxic peptides and proteins, including many ion channel blockers and modulators, as well as potent cytolysins. This review describes the structures that have been determined to date for the major classes of peptide and protein toxins. In addition, established and emerging methods for structure determination are summarized and the prospects for modelling newly described toxins are evaluated. In common with most other classes of proteins, toxins display conformational flexibility which may play a role in receptor binding and function. The prospects for obtaining atomic resolution structures of toxins bound to their receptors are also discussed.     

Biologically active polypeptides from the tropical sea anemone Radianthus macrodactylus.

Some biologically active polypeptides, three high and two low molecular weight cytolysins and four trypsin inhibitors were isolated from the sea anemone Radianthus macrodactylus and characterized. The purification steps involved acetone precipitation, gel filtration, ion-exchange, and affinity chromatography, and ion-exchange and reverse-phase HPLC. The relative molecular weight of high molecular weight Radianthus cytolysins named according to their N-terminal amino acids RTX-A (Ala), RTX-S (Ser) and RTX-G (Gly) was about 20,000. The isoelectric points were 9.8 for RTX-A and RTX-S, and 10.5 for RTX-G. The hemolytic activities of RTX-A, RTX-S and RTX-G were 3.5 x 10(4), 5.0 x10(4), and 1.0 x10(4)HU/mg, respectively, and were inhibited by sphingomyelin. The N-terminal amino acid sequence of RTX-A was determined as ALAGAIIAGAGLGLKILIEVLGEG-VKVKI-. Molecular weight of low molecular weight Radianthus cytolysins RmI, RmII, and of one trypsin inhibitor InI were 5100, 6100 and 7100, respectively. Isoelectric points for RmI and RmII were 9.2 and 9.3. Their hemolytic activity worked out 25 and 20 HU/mg, and was not inhibited by sphingomyelin. Toxicity of RmI and RmII was assessed by their histaminolytic activity. Amino acid composition of RmI and RmII was similar to that of tealiatoxin, histaminolytic cytolysin from the sea anemone Tealia felina.     

Comparison fo metridiolysin from the sea anemone with thiol-activated cytolysins from bacteria.

Metridiolysin, a cytotoxic protein from the sea anemone, Metridium senile, is activated by dithiothreitol and appears to be dependent for its activity on SH-groups. In this respect it resembles a class of SH-activated cytolytic bacterial proteins of which streptolysin O is the prototype. It shares also with SH-activated bacterial cytotoxins the capacity to produce ～ 33 nm rings demonstrable by electron microscopic examination of negatively stained preparations of membranes from metridiolysin-lysed erythrocytes. Ring formation appears to correlate with alterations in membrane structure revealed by freeze-fracture electron microscopy. Further comparison of metridiolysin with the SH-activated bacterial cytotoxins reveals that both are inhibitable by low concentrations of cholesterol and that both have biological effects that are broadly similar. They differ, however, in certain other respects including molecular weight and capacity to dissociate into subunits.     

Properties of a cytolytic toxin from the sea anemone, Stoichactis kenti

A cytolytic toxin (kentin) from the Indo-Pacific sea anemone, Stoichactis kenti, was purified to near homogeneity. The toxin is a basic polypeptide of molecular weight approximately 18,000. It broadly resembles cytotoxins from Stoichactis helianthus (helianthin), as well as similar toxins from a number of other anemones, namely Condylactis, Epiactis, Actinia, Pseudactinia, Tealia, Anthopleura, Radianthus and Gyrostoma. The amino acid composition of kentin shows considerable resemblance to that of helianthin, but there are also several significant differences. Neutralization tests indicate that kentin and helianthin are immunologically related but distinguishable. In contrast, no immunological relatedness was found between helianthin and cytolytic toxins from Condylactis gigantea and Epiactis prolifera.     

海葵溶细胞素的生物信息学分析

利用生物信息学的软件与方法对已报道的17种海葵溶细胞素的氨基酸组成、理化性质、结构特征以及系统演化关系等进行预测和分析。结果表明不同海葵溶细胞素在氨基酸组成和理化性质上具有一定相似性,但其在结构上有一定差别。以MP法和NJ法对不同海葵溶细胞素构建的系统发生树基本一致,在亲缘关系较近的7种海葵溶细胞素中可以找到6个保守序列。     

Modification of arginine in sea anemone toxin RTX-III from Radianthus macrodactylus

Chemical modifications of the polypeptide neurotoxin RTX-III have allowed us to study the functional role of Arg residues. The effect of chemical modification has been estimated by measuring toxicity in mice. 2,4-Pentanedione did not react with Arg residues of RTX-III even after 100 hr incubation. Malonic aldehyde reacted readily with RTX-III, yielding an unusual derivative; a Schiff's base obtained by condensation of one of two aldehyde groups of malonic aldehyde with the guanidine group. The derivative was one-fourth as toxic as the native toxin. Modification of the guanidine side chain of Arg-13 with both 1,2-cyclohexanedione and phenylglyoxal decreased the toxicity of RTX-III by a factor of five. We conclude that Arg-13 is not fully responsible for toxicity. The toxin-receptor attachment might be multipoint, involving several structural elements of the protein molecule, with Arg-13, probably being one of them. The guanidine side chain of Arg-45 is buried in the sequence and apparently functionally nonessential.     

太平洋侧花海葵中的化学成分(Ⅲ)

目的　研究太平洋侧花海葵的活性成分。方法　采用稻瘟霉模型生物活性追踪方法 ,应用多种色谱技术进行分离 ,理化性质和波谱数据鉴定其结构。结果　分离并鉴定了 9个化合物 :正十六烷 ( ) ,正十三醇 ( ) ,棕榈酸 ( ) ,硬脂酸 ( ) ,棕榈酸甲酯 ( ) ,花生酸甲酯 ( ) ,1 - O-蜡酰甘油酯 ( )以及 2 S,3 R,Δ4 (E) ,Δ8(E) -十八碳鞘氨醇 -正十六碳酰胺和其同系物 2 S,3 R,Δ4 (E) ,Δ8(E) -十八碳鞘氨醇 -正十四碳酰胺的混合物 ( 和 ) ,其中 和 的混合物对稻瘟霉的最小菌丝变形浓度为 6 3 mg· L-1。结论　 9个化合物均为首次从该种海葵中获得 ,( 和 )具有诱导稻瘟霉菌丝变形活性     

太平洋侧花海葵中的化学成分(Ⅱ)

目的:研究太平洋侧花海葵的活性成分。方法:采用稻瘟霉模型生物活性追踪方法,应用多种色谱技术进行分离,理化性质和波谱数据鉴定其结构。结果:分离并鉴定了 5个化合物,5α,8α-过氧麦角甾-6,22-二烯-3β-醇(Ⅰ),对羟基苯甲醛(Ⅱ),N-甲基吡啶-2-羧酸盐(Ⅲ),脲基甲酸乙酯(Ⅳ),牛磺酸(Ⅴ),其中化合物和对稻瘟霉的最小菌丝变形浓度分别为0.46mmol·L~(-1)和1.9mmol·L~(-1)。结论:5个化合物均为首次从该种海葵中获得,化合物和具有诱导稻瘟霉菌丝变形活性。     

Amino acid sequence of two sea anemone toxins from Anthopleura fuscoviridis

The amino acid sequences of two toxins, AFT-I and AFT-II, from the sea anemone Anthopleura fuscoviridis were determined. AFT-I and -II consist of 47 and 48 amino acid residues, respectively, and are cross-linked with three disulfide bridges. The sequences have high homology to those of toxins I and II from Anemonia sulcata and anthopleurin-A and -B from Anthopleura xanthogrammica.