抗羟甲芬太尼单克隆抗体和抗羟甲芬太尼独特型抗体的特性研究

本文采用羟甲芬太尼免疫的BALB/c小鼠脾脏细胞与小鼠骨髓瘤细胞NS-1融合,获得分泌抗羟甲芬太尼抗体的单克隆杂交瘤细胞株。该株细胞分泌的抗羟甲芬太尼单克隆抗体与羟甲芬太尼结合的亲合力为3.65±0.59×10~7 l/mol。羟甲芬太尼类似物3-甲基芬太尼、β-羟基芬太尼和芬太尼与抗羟甲芬太尼单克隆抗体有部分交叉反应,而DAGO,纳洛酮和双氢依托啡与抗羟甲芬太尼单克隆抗体无交叉反应。应用纯化的抗羟甲芬太尼单克隆抗体免疫家免,获得高滴度的兔抗羟甲芬太尼独特型抗体。抗羟甲芬太尼独特型抗体与抗羟甲芬太尼单克隆抗体结合反应有剂量关系,并呈可饱和性。抗羟甲芬太尼独特型抗体能竞争抑制抗羟甲芬太尼单克隆抗体与原始抗原羟甲芬太尼的结合反应。受体结合分析表明抗羟甲芬太尼独特型抗体能与放射性配体[~3H]羟甲芬太尼和[~3H]DAGO竞争结合大鼠脑匀浆膜蛋白上的阿片受体。在离体生物检定实验中抗羟甲芬太尼独特型抗体还具有类似羟甲芬太尼样作用,能呈剂量依赖地抑制电场刺激引起的小鼠输精管的收缩。以上结果提示抗羟甲芬太尼独特型抗体能与羟甲芬太尼竞争结合抗羟甲芬太尼单克隆抗体上的同一结合位点,具有羟甲芬太尼的内影像结构,并能与μ阿片受体结合,呈阿片受体激动剂样作用。     

高效离子交换液相色谱法分离绿脓杆菌外膜蛋白

利用高效ＤＥＡＥ离子交换液相色谱法分离纯化了绿脓杆菌标准菌株ＰＡＯ１外膜蛋白。流动相为ｐＨ８．０Ｔｒｉｓ－ＨＣｌ缓冲液,色谱柱为ＴＳＫｇｅｌ－ＤＥＡＥ－５ＰＷ（０．７５ｃｍ×７．５ｃｍｉ．ｄ．）。通过纯化外膜蛋白,可以为研究绿脓杆菌外膜通透性与抗生素耐药性之间的关系及缩短研究周期提供有效的方法。     

曼氏血吸虫谷胱甘肽S—转移酶Sm26／2抗原肽研究

在计算机辅助下，应用Ｇｏｌｄｋｅｙ和ＰＣ－Ｇｅｎｅ程序，根据新报道的曼氏血吸虫谷胱甘肽Ｓ－转移酶Ｓｍ２６／２的氨基酸序列，进行亲水性、柔韧性、可接近性、电荷分布和二级结构分析，预测出６个抗原肽，并用固相法进行了合成。经Ｄｏｔ－ＥＬＩＳＡ法测定，其中的２个对抗日本血吸虫免疫球蛋白多克隆抗体（抗－Ｓｉ－ＩｇＧ－ＰｃＡｂ）显示出较好的抗原性，１个对抗血吸虫表膜单克隆抗体（Ａ６ＭｃＡｂ）显示出较好的抗原性     

O－（1－BENZOTRIAZOLYL）－SULFATE AS ALEAVING GROUP IN SUBSTITUTION OF NUCLEOSIDE

Ｏ－（１－ＢＥＮＺＯＴＲＩＡＺＯＬＹＬ）－ＳＵＬＦＡＴＥＡＳＡＬＥＡＶＩＮＧＧＲＯＵＰＩＮＳＵＢＳＴＩＴＵＴＩＯＮＯＦＮＵＣＬＥＯＳＩＤＥ￥ＹａｏＳｈｕＺＨＡＮＧ，ＬａｉＸｉｎＷＡＮＧａｎｄＬｉＨｅＺＨＡＮＧ（ＳｃｈｏｏｌｏｆＰｈａｒｍａｃｅｕｔｉｃ...     

高效离子交换液相色谱法分离绿脓杆菌外膜蛋白

 利用高效ＤＥＡＥ离子交换液相色谱法分离纯化了绿脓杆菌标准菌株ＰＡＯ１外膜蛋白。流动相为ｐＨ８．０Ｔｒｉｓ－ＨＣｌ缓冲液,色谱柱为ＴＳＫｇｅｌ－ＤＥＡＥ－５ＰＷ（０．７５ｃｍ×７．５ｃｍｉ．ｄ．）。通过纯化外膜蛋白,可以为研究绿脓杆菌外膜通透性与抗生素耐药性之间的关系及缩短研究周期提供有效的方法。     

HBVDNA与抗BHcIgM在临床检测中的价值

采用地高辛标记探针以分子杂交的方法对８５１例血清进行ＨＢＶＤＮＡ的检测,采用ＥＬＩＳＡ的方法对相同标本检测了抗－ＨＢｃＩｇＭ、ＨＢＶ二对半、抗－ＨＡＶＩｇＭ、抗－ＨＣＶ及抗－ＨＥＶ ＩｇＭ,发现ＨＢＶＤＮＡ阳性检出率与ＨＢｅＡｇ出现相关,且ＨＢｅＡｇ阴性的标本中仍有１０．２５％（４９／４７８）ＨＢ－ＶＤＮＡ阳性,说明仅以ＨＢｅＡｇ出现与否判定是否存在ＨＢＶ的复制是不可靠的。同时,还发现ＨＢＶＤＡＮ     

金表面自组装化学发光免疫传感器

用Ｎ－乙酰半胱氨酸金表面自组装技术及ＥＤＣ、ＮＨＳ偶联剂将兔ＩｇＧ固定于金表面制成免疫传感器探头，用碱性磷酸酯酶标记山羊抗兔ＩｇＧ加入待测的含有山羊抗兔ＩｇＧ的样品中，采用竞争头测定山羊抗兔ＩｇＧ含量，标记的碱性磷酸酯酶可催化底物ＡＭＰＰＤ产生化学发光，其发光强度与样品浓度成反比。测得山羊抗兔ＩｇＧ的最低检出限为０．８ｍｇ／Ｌ，线性测定范围为０．８－４０ｍｇ／Ｌ。     

石墨炉原子吸收光谱无标样分析法的研究Ⅲ．元素特征质量实验值的稳定性

在消除基体干扰的前提下，分别采用北二光Ｄ＿２／ＷＦＸ－ＩＥ－ＡＡＳ、日立Ｚ／１８０－８０－ＡＡＳ及Ｐ．Ｅ．Ｚ／３０３０－ＡＡＳ仪器，研究了不同测量日期中在同一台仪器上以最优化分析条件获得的海水基体中Ａｓ，Ｃｄ，Ｃｏ，Ｃｒ，Ｃｕ，Ｍｎ，Ｍｏ，Ｎｉ和Ｐｂ九个元素的ｍ＿（０Ｅ）值的稳定性；同时还考察了不同日期测得的玩具样品中Ａｓ元素的ｍ＿（０Ｅ）值的稳定性。研究结果表明对同一仪器元素的ｍ＿（０Ｅ）值不因实验者、样品基体和测量日期的不同而发生大的波动，具有一定的稳定性。     

INDOStudiesonElectronicStructuresof（C＿8H＿8）Ln（2，4－C＿4H＿11）（THF）（Ln＝Nd，Sm，Er）

ＩＮＤＯＳｔｕｄｉｅｓｏｎＥｌｅｃｔｒｏｎｉｃＳｔｒｕｃｔｕｒｅｓｏｆ（Ｃ＿８Ｈ＿８）Ｌｎ（２,４－Ｃ＿４Ｈ＿１１）（ＴＨＦ）（Ｌｎ＝Ｎｄ,Ｓｍ,Ｅｒ）ＷＡＮＧＺｈｉ－ｚｈｏｎｇ＊,ＦＥＮＧＪｉａｎ－ｎａｎ,ＺＨＡＮＧＳｏ－ｂｏａｎｄＬＩＵＪｕ－ｚｈ...     

反相高效液相色谱柱前衍生荧光法测定肠粘膜中的谷氨酰胺

以邻苯二甲醛及３－巯基丙酸为衍生试剂,５０ｍｍｏｌ／Ｌ磷酸缓冲液（ｐＨ７．０）－乙腈（９４∶６,Ｖ／Ｖ）为流动相,在ＬｉｃｈｒｏｓｏｒｂＲＰ１８（１５０ｍｍ×４．６ｍｍｉ．ｄ．,５μｍ）柱上,研究并建立了测定动物肠粘膜中谷氨酰胺（Ｇｌｎ）的柱前衍生荧光ＲＰ－ＨＰＬＣ法。样品与衍生剂按４∶１进行衍生反应,Ｅｘ＝２３０ｎｍ,Ｅｍ＝３８９ｎｍ;流速为２．０ｍＬ／ｍｉｎ。Ｇｌｎ的保留时间为３．１５８ｍｉｎ,检测限为２５μｍｏｌ／Ｌ（Ｓ／Ｎ＝３．５）,线性范围为５０～３２００μｍｏｌ／Ｌ,ｒ＝０．９９９６。     

A carbanion induced synthesis of highly congested pyrazole and imidazole containing heterocycles

An efficient approach to the synthesis of highly congested di, penta and hexacyclic pyrazoles as well as imidazole fragment containing novel heterocyclic molecule has been developed through a carbanion induced transformation of suitably functionalized 2H-pyran-2-ones, benzo[h]chromene and thiochromeno[4,3-b]pyrans. Due to the presence of fluorescence, we report their prime application metal sensor as off/on switching in ferric ions.     

Toward new camptothecins. Part 6: Synthesis of crucial ketones and their use in Friedländer reaction

In the context of the preparation of camptothecin and luotonin A analogs, the synthesis of some key keto-precursors and their use in Friedländer condensation are described. This paper also focuses on the stability of these keto intermediates and emphasizes the major differences between indolizinones and pyrroloquinazolinones series. Noteworthy is also the report of some original structures isolated as by-products of some experiments.     

Selective synthesis of 4,5-dihydroimidazo- and imidazo[1,5-a]quinoxalines via modified Pictet–Spengler reaction

An efficient tandem approach for the selective synthesis of 4,5-dihydroimidazo[1,5-a]quinoxalines 6a–g and imidazo[1,5-a]quinoxalines 7a–h by the reaction of 2-imidazolyl anilines 4a–c with aryl aldehydes 5a–k under mild reaction conditions is described. Introduction of electron releasing alkyl groups in substrates 4a–b was found to be instrumental for the success of the reaction.     

Understanding the Diels-Alder reactivity of 1,2-azaborine analogues

The Diels-Alder reactivity of 1,2-heteroborines (H₄C₄B(H)X, X?=?NH, PH, AsH; O, S, Se) has been computationally explored by means of Density Functional Theory (DFT) calculations. The influence of the HB?=?X fragment on the reactivity of the system has been quantitatively analyzed in detail by means of the so-called Activation Strain Model (ASM) of reactivity. It is found that the interaction between these species and the dienophile is significantly stronger than that computed for their all-carbon isoelectronic counterpart, benzene. In addition, the strain energy plays a key role in the observed reactivity trends. The role of the aromaticity strength of these heteroarenes on the reactivity is also assessed.     

Synthesis of N-substituted carbazolones from α-iodo enaminones via Pd(0)-catalyzed intramolecular coupling under microwave irradiation

A variety of N-aryl and N-alkyl carbazolones were conveniently achieved in good to high yields via Pd₂(dba)₃-mediated intramolecular coupling of N-substituted α-iodo enaminones under microwave irradiation. The Pd(0)-catalyzed cyclization was found to proceed favorably with the more electron-deficient phenyl ring during the reactions involving unsymmetrical N,N-diaryl α-iodo enaminones. This unique property enables the construction of carbazolone skeleton containing nitro substituted benzenoid ring.     

KMnO4-mediated oxidative CN bond cleavage of tertiary amines: Synthesis of amides and sulfonamides

KMnO₄-mediated oxidative CN bond cleavage of tertiary amines producing secondary amine was introduced, which was trapped by electrophiles (acyl chloride and sulfonyl chloride) to form amides and sulfonamides. The reaction could take place at mild condition, tolerating a wide range of function groups and affording products in moderate to excellent yields.     

Synthesis of substituted 2,4,5,6-tetrahydrocyclopenta[c]pyrazoles and 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles by intramolecular nitrilimine cycloaddition

Both substituted 2,4,5,6-tetrahydrocyclopenta[c]pyrazoles and 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles have been synthesized by the 3+2 intramolecular dipolar cycloaddition of nitrilimines to alkynes. This cyclization has been extended to more versatile 3-bromo derivatives by the use of alkynylbromides as dipolarophiles.     

Chemistry of heterocyclic compounds at the A. E. Favorsky Irkutsk Institute of Chemistry, Siberian Branch of the Russian Academy of Sciences, over 50 years (Review)

The review contains a concise historical account and information on the most significant researches undertaken by the staff at the A. E. Favorsky Irkutsk Institute of Chemistry, Siberian Branch of the Russian Academy of Sciences on the Chemistry of Heterocyclic Compounds. Dedicated to Academician of the Russian Academy of Sciences B. A. Trofimov on his 70th jubilee. Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 10, pp. 1443–1502, October, 2008.     

Catalyst free,visible-light promoted photoaddition reactions between C60 and N-trimethylsilylmethyl-substituted tertiary amines for synthesis of aminomethyl-1,2-dihydrofullerenes

An efficient and benign method for the preparation of aminomethyl-substituted fullerenes has been developed. The process, involving catalyst free, visible-light irradiation of 10% EtOH-toluene solutions containing fullerene C₆₀ and N-trimethylsilylmethyl-substituted amines by using a 20 W compact fluorescent lamp, leads to formation of aminomethyl-substituted fullerene adducts in a highly efficient manner. The photoaddition reaction takes place via a pathway initiated by visible light absorption by C₆₀, followed by SET from the amine to the triplet excited state of C₆₀. Ethanol-promoted desilylation of the resulting a minimum radical then generates the corresponding α-amino radical which couples with the C₆₀ radical anion to form the anion precursor of the fullerene adducts. The new approach using visible-light takes place under mild conditions and it does not require the use of photocatalysts. Thus, the method developed in this effort could broadens the range of functionalized fullerene derivatives that can be readily prepared.