L-精氨酸-L-焦谷氨酸的应用及合成

L-精氨酸应用很广泛,但受到溶解性差及味感差的限制,其应用领域无法再拓宽。与L-焦谷氨酸配伍,制成L-精氨酸-L-焦谷氨酸复合盐,可应用在医疗、保健、化妆品等行业,并可使得单体的精氨酸和焦谷氨酸的应用功效增强。     

黔产天麻的化学成分

从黔产天麻（Ｇａｓｔｒｏｄｉａ ｅｌａｔａ Ｂｌ．）中分离得到１个新的含氮化合物,命名为天麻羟胺（ｇａｓｔｒｏｄａｍｉｎｅ,Ⅰ）,经波谱分析,确定其结构为双－（对羟苄基）羟胺。除β－谷甾醇和胡萝卜甙外,同时还分离鉴定了３个已知化合的：Ｌ－焦谷氨酸（Ⅱ）、柠檬酸单甲酯（Ⅲ）、柠檬酸双甲酯（Ⅳ）,其中化合物Ⅱ和Ⅳ为首次报道从天麻中得到的。     

相反相成药物治疗马骡结症的理论探讨

“对立统一规律是宇宙的根本规律。”动物体是完整统一的有机体,其各系统、各器官的机能活动是矛盾的,对立的,同时又是统一的。心脏的跳动,肺脏的呼吸,肌肉的伸缩,胃肠的蠕动等,都是由相互联系、相互制约的对立统一的活动完成的。在这些活动当中,神经系统起着主要的调节作用。中枢神经系统是支配全身活动的中枢,而内脏器官的活动是由相对自主的植     

云南一些植物特征成分与古夷平面的相关性

生理生态学的原则是随着纬度的升高,物种分布的海拔高度将随之降低。但是,云南一些植物特征成分的分布却与之相反,它们的分布与云南残留的古夷平面的分布相似,即随着纬度的升高,其分布的海拔高度也随之升高。二者的区别是云南古夷平面分布的趋势线的仰角大于那些特征成分分布的趋势线的仰角。可能的原因是：相对于剧烈的地质运动,物种的适应能力总是相对滞后的,并且物种的分布也受到其生长特性的制约;根据分布区形成的原则,这些成分的发生应早于夷平面的隆起。     

学案导学在高中生物教学中的应用

制作学案的过程,就是老师理解通透所传授的知识的前提下,阅读大量的相关的资料,根据学生的认知水平与知识的积累能力,为指导学生进行主动的知识建构而编制的学习方案,以便积极引导和帮助学生的自主学习的能力进行探究思索的方案。高中生物的教学研究问题,通过学案的方式向学生传授知识,是教师在教学理论与学习标准的指导下对高中生物的教学所提高的一个新层次。     

植物保护与农业可持续发展关系探究

随着社会的发展经济的进步我国在各个领域的发展上都得到了相应的提升,从农业的发展情况来看,由于我国在科学技术上进步故此在农业的发展上也取得了重大的成效,但是在农业发展的过程中也出现了一些严重的问题,就是对于化学药品的使用所造成的农产品的污染以及环境的污染。本文主要针对当前的一些植物保护的现状进行阐述,并对植物保护和农业的可持续发展间的关系进行了详细的分析探究,希望能够在此领域的学术发展起到一定的参考作用。     

自然和热凝固的人肝组织对KTP/YAG激光的光学特性的比较研究

本文采用双积分球测量系统和Inverse Add ing-Doub ling方法,研究了自然和热凝固的人肝组织对532nm的KTP激光和1 064 nm的Nd:YAG激光的光学特性。结果表明:热凝固的人肝组织对532 nm的KTP激光的吸收系数较自然的肝组织的吸收系数增大了23.5%(P<0.05),热凝固的肝组织对1 064 nm的Nd:YAG激光的吸收系数较自然的肝组织的吸收系数减小了34.3%(P<0.05)。热凝固的人肝组织对532 nm的KTP激光的散射系数较自然的肝组织的散射系数增大了4.50倍(P<0.05),热凝固的肝组织对1 064 nm的Nd:YAG激光的散射系数较自然的肝组织的散射系数增大了6.41倍(P<0.05)。热凝固的人肝组织对532 nm的KTP激光的各向异性因子较自然的肝组织的各向异性因子减小了5.47%,热凝固的肝组织对1 064 nm的Nd:YAG激光的各向异性因子较自然的肝组织的各向异性因子减小了1.95%。     

浅谈果树病虫害综合防治技术研究

在我国的农业生产的过程中,对于果树的病虫害综合防治是农业生产效益的根本保障,我国是一个农业大国,尤其是在我国的北方,果树的栽培更是有着悠久的历史,在近些年中由于技术的进步果树的品种更新的速度也在不断的加快,但是随之而来的就是果树的病虫害的问题,它对于果树的影响非常的大,直接在经济上给果农带来严重的损失,为了能够让果农的经济效益得到保障,对于果树的病虫害防治就显得极为重要。本文主要是对东北地区的果树病虫害的现状进行简要的分析,并对果树病虫害的综合防治技术进行研究找出适当的对策,希望能有所裨益。     

浅析如何做好基层林业站的工作

在当前的形势下,我国的林业建设工作也是需要及时的调整发展方案,以此来适应新时代的发展的,要由传统的林业建设模式逐渐的向现代化的方向发展。从某种程度上来说,基层林业站的微观变化也会对林业建设的发展方向的宏观调整产生直接的影响,因此,要结合科学发展的建设理念,来指导林业站的工作,以此来促进林业的健康建设。文章主要阐述基层林业站的作用,主要是为更好的发挥基层林业站的效用服务的。     

Isolation of N-acetylglutamine, pyroglutamic acid and the butyl ester of pyroglutamic acid from human brain

N-acetyl-l -glutamine, pyroglutamic acid, and the butyl ester of pyroglutamic acid were isolated in pure form from an aqueous extract of human brain. These compounds were isolated by combination of paper and ion exchange chromatography. The isolated substance identified as N-acetyl-l -glutamine did not react with the ninhydrin reagent but yielded glutamic acid and ammonia upon acid hydrolysis. An acetyl hydrazide was identified by paper chromatography from hydrazinolysates of the isolated substance. The glutamic acid liberated by hydrolysis had the l -configuration. The results of elementary analysis of the isolated compound were in full accord with the analysis calculated for synthetic N-acetyl-l -glutamine. A large amount of pyroglutamic acid and a substance identical with the butyl ester of pyroglutamic acid were isolated in pure form. The results of our studies suggest that pyroglutamic and the butyl ester derivative were artifacts formed during the isolation and purification procedures.     

Screening for glucose‐triggered modifications of glutathione

Nonenzymatic protein glycation is caused by a Schiff's base reaction between the aldehyde groups of reducing sugars and the primary amines of proteins. These structures may undergo further Amadori rearrangement and free radical‐mediated oxidation to finally generate irreversible advanced glycation end products (AGEs). One of the factors known to modulate the glycation of proteins is glutathione, the most abundant nonprotein thiol tripeptide with the γ‐linkage, H‐Glu(Cys‐Gly‐OH)‐OH (GSH). Screening for products formed by GSH with D ‐glucose is an essential step in understanding the participation of GSH in glycation (the Maillard) reaction. Under the conditions used in these studies we observed N‐(1‐deoxy‐D ‐fructos‐1‐yl)‐pyroglutamic acid as the major glycation product formed in the mixtures of GSH and glucose in vitro. A RP HPLC/MS and tandem MS analyses of the GSH/glucose mixtures revealed that cleavage of the N‐terminal glutamic acid and the formation of pyroglutamic acid‐related Amadori product were accompanied by generation of Cys‐Gly‐derived Amadori and thiazolidine compounds. Copyright © 2009 European Peptide Society and John Wiley & Sons, Ltd.     

Stability and CTL activity of N-terminal glutamic acid containing peptides.

Several cytotoxic T lymphocyte peptide-based vaccines against hepatitis B, human immunodeficiency virus and melanoma were recently studied in clinical trials. One interesting melanoma vaccine candidate alone or in combination with other tumor antigens, is the decapeptide ELA. This peptide is a Melan-A/MART-1 antigen immunodominant peptide analog, with an N-terminal glutamic acid. It has been reported that the amino group and gamma-carboxylic group of glutamic acids, as well as the amino group and gamma-carboxamide group of glutamines, condense easily to form pyroglutamic derivatives. To overcome this stability problem, several peptides of pharmaceutical interest have been developed with a pyroglutamic acid instead of N-terminal glutamine or glutamic acid, without loss of pharmacological properties. Unfortunately compared with ELA, the pyroglutamic acid derivative (PyrELA) and also the N-terminal acetyl-capped derivative (AcELA) failed to elicit cytotoxic T lymphocyte (CTL) activity. Despite the apparent minor modifications introduced in PyrELA and AcELA, these two derivatives probably have lower affinity than ELA for the specific class I major histocompatibility complex. Consequently, in order to conserve full activity of ELA, the formation of PyrELA must be avoided. Furthermore, this stability problem is worse in the case of clinical grade ELA, produced as an acetate salt, like most of the pharmaceutical grade peptides. We report here that the hydrochloride salt, shows higher stability than the acetate salt and may be suitable for use in man. Similar stability data were also obtained for MAGE-3, another N-terminal glutamic acid containing CTL peptide in clinical development, leading us to suggest that all N-terminal glutamic acid and probably glutamine-containing CTL peptide epitopes may be stabilized as hydrochloride salts.     

Stability and CTL-activity of P40/ELA Melanoma Vaccine Candidate

The decapeptide ELA (ELAGIGILTV), a Melan-A/MART-1 antigen immunodominant peptide analogue, is an interesting melanoma vaccine candidate alone or in combination with other tumour antigens. P40, the recombinant outer membrane protein A of Klebsiella pneumoniae (kpOmpA), was recently shown to target dendritic cells and to induce peptide-specific CTLs. Here we investigated the adjuvant role of P40 mixed or chemically conjugated to ELA. This compound is an N-terminal glutamic acid-containing peptide. However, it has been reported that the amino group and the gamma-carboxylic group of glutamic acids easily condense to form pyroglutamic derivatives. Usually, to overcome this stability problem, peptides of pharmaceutical interest were developed with a pyroglutamic acid instead of N-terminal glutamic acid, without loss of pharmacological properties. Unfortunately, the pyroglutamic acid derivative (PyrELA) as well as the N-terminal acetyl capped derivative (AcELA) failed to elicit CTL activity when mixed with P40 adjuvant protein. Despite the apparent minor modifications introduced by PyrELA and AcELA, these two derivatives have probably lower affinity than ELA for the class I Major Histocompatibility Complex. Furthermore, this stability problem is worse in the case of clinical grade ELA, produced as an acetate salt, like most of the pharmaceutical grade peptides. We report here that the hydrochloride shows a higher stability than the acetate and may be suitable for use in man.     

Pyroglutamyl N-termini of thermal polyamino acids

It has been established indirectly that the N-termini of the thermal polyamino acids are pyroglutamic acid. This was determined by trifluoroacetic acid hydrolysis of the lactam ring followed by Dansyl labelling. The polyamino acids contained Ala, Gly, Glu, Leu, Phe, and Pro. In the experiments described here, the presence of pyroglutamic acid at the N-terminus of a polyamino acid was determined directly by the use of pyrrolidone carboxylyl peptidase. The enzyme catalyzes the removal of pyroglutamyl residues at the N-terminus of polypeptide chains. The polyamino acids used in these studies contained glutamic acid, aspartic acid, alanine, glycine, isoleucine, proline and valine. Alkaline hydrolysis was also used to determine indirectly that the N-termini of these polyamino acids are pyroglutamic acid. Another interesting finding was that many of the amino acids in the polymerization mixture were found to occur penultimate to the N-terminal amino acid. This is interpreted to mean that the diffusible fraction contains many polyamino acids.     

Formation of specific amino acid sequences during carbodiimide-mediated condensation of amino acids in aqueous solution

Carbodiimide-mediated peptide synthesis in aqueous solution at room temperature has been studied with respect to self-ordering of amino acids. Inasmuch as glutamic acid is readily converted into pyroglutamic acid, the peptides formed by copolymerization of glutamic acid with other amino acids are preferentially pyroglutamyl-peptides. Competition experiments were carried out to determine the influence of the amino acid side chains on the reactivity of amino acids and peptides during the dehydration condensation. The results show that the self-ordering process is controlled by both the activated carboxyl component (amino acid or growing peptide) and the incoming amino acid. A condensation of pyroglutamic acid, alanine and another amino acid component Xxx (Xxx = Gly, Val, Leu or Gly-Tyr) preferentially yielded the dipeptide pyroGlu-Ala, but the formation of the tripeptide pyroGlu-Ala-Ala became strongly reduced because of competing reactions. A simple explanation for the observed selectivities is not at hand. Polypeptides were so far only obtained when they were allowed to precipitate in the reaction system. Evidence for the non-random copolymerization of larger peptides is presented as well.     

Preparation and reactivity of aminoacyl pyroglutamates. Facile synthesis of 10-membered-ring cyclic dipeptides derived from 1,4-diaminobutyric and glutamic acids.

A number of protected proline-containing dipeptides Boc-Xaa-Pro-OBu(t) were converted via epimerization-free oxidation with RuO4 to dipeptides with an internal pyroglutamic acid residue, Boc-Xaa-Glp-OBu(t). The latter were subjected to oxidative Hoffman-type rearrangement induced by PhI[OC(O)CF3]2 to give N-(aminoacyl)-pyroglutamates. The behavior of these derivatives under basic conditions was studied, and for two such a derivatives an aminoacyl incorporation reaction was observed, producing otherwise poorly accessible 10-membered-ring dilactams derived from 1,4-diaminobutyric and glutamic acids in practicable yields.     

Isolation and properties of ovine [1-pyroglutamic acid]-β-lipoprotein

A new form of ovine β-lipotropin has been isolated by partition chromatography on agarose gel. All the evidence is consistent with the conclusion that its structure is identical to that of ovine β-lipotropin with the exception that the glutamic acid residue in position 1 was replaced by a pyroglutamic acid residue. Its lipolytic activity in isolated rabbit fat cells was about one-half that of β-lipotropin.     

On the Manner of Cyclization of <Emphasis Type="Italic">N</Emphasis>-Acylated Aspartic and Glutamic Acid Derivatives

Abstract  

When synthesizing arylpiperazine library modified with N-acylated amino acid derivatives (e.g., cyclized aspartic acid, cyclized glutamic acid, proline) we wished to rapidly determine the way of cyclization of N-acylated glutamic acid derivatives. During concomitant cleavage and cyclization two alternative routes were possible—either formation of six-member imide (glutarimide) or five-member lactam. Application of MS/MS and ¹H NMR method allowed us to establish that cyclization of N-acylated glutamic acid derivatives preceded to lactams—N-acylated pyroglutamic acid derivatives.     

Formation of specific amino acid sequences during carbodiimide-mediated condensation of amino acids in aqueous solution,and computer-simulated sequence generation

Carbodiimide-mediated peptide synthesis in aqueous solution has been studied with respect to self-ordering of amino acids. The copolymerisation of amino acids in the presence of glutamic acid or pyroglutamic acid leads to short pyroglutamyl peptides. Without pyroglutamic acid the formation of higher polymers is favoured.The interactions of the amino acids and the peptides, however, are very complex. Therefore, the experimental results are rather difficult to explain. Some of the experimental results, however, can be explained with the aid of computer simulation programs. Regarding only the tripeptide fraction the copolymerisation of pyroGlu, Ala and Leu, as well as the simulated copolymerisation lead to pyroGlu-Ala-Leu as the main reaction product. The amino acid composition of the insoluble peptides formed during the copolymerisation of Ser, Gly, Ala, Val, Phe, Leu and Ile corresponds in part to the computer-simulated copolymerisation data.