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swainsonine对胰岛素受体功能影响的研究

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生物化学杂志 1995年第1期11卷 55-60页

作者：戚维维陈惠黎上海医科大学生物化学教研室

以Ｓｗａｉｓｏｎｉｎｅ（Ｓｗ）作为高尔基体付糖链加工酶系中α－甘露糖苷酶Ⅱ的特异抑制剂，研究Ｎ－糖链结构和胰岛素受体（Ｉｎｓ－Ｒ）功能的关系．发现Ｓｗ不影响细胞生长和３Ｈ－亮氨酸参入ＳＭＭＣ７７２１细胞，但明显促进３... 详细信息

以Ｓｗａｉｓｏｎｉｎｅ（Ｓｗ）作为高尔基体付糖链加工酶系中α－甘露糖苷酶Ⅱ的特异抑制剂，研究Ｎ－糖链结构和胰岛素受体（Ｉｎｓ－Ｒ）功能的关系．发现Ｓｗ不影响细胞生长和３Ｈ－亮氨酸参入ＳＭＭＣ７７２１细胞，但明显促进３Ｈ－甘露糖参入细胞总糖蛋白和表面糖蛋白，并使后者的ＣｏｎＡ强结合组分显著增加，提示Ｓｗ使Ｉｎｓ－Ｒ的Ｎ－糖链变成杂合型及高甘露糖型。胰岛素结合试验后作Ｓｃａｔｃｈａｒｄ分析：发现Ｓｗ不改变Ｉｎｓ－Ｒ的结合容量和每个细胞表面的结合位点数，也不改变结合动力学。再用部分纯化的Ｉｎｓ－Ｒ研究自身磷酸化和对外源底物的酪氨酸蛋白激酶活力，也未发现Ｓｗ处理和对照细胞间的明显区别，表示Ｓｗ也不影响Ｉｓｎ－Ｒ的跨膜信息传递，结合已报道的衣霉素使细胞表面Ｉｎｓ－Ｒ减少的结果，提示Ｉｎｓ－Ｒ运送至细胞膜需要Ｎ－糖链存在。

关键词： swainsonine 胰岛素胰岛素受体细胞膜

The Mechanism of swainsonine Causing Early Pregnancy Abnormal Decidualization and Inducing Abortion by Changing Glycosylation Modification

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Advances in Reproductive Sciences 2018年第3期6卷 70-101页

作者： Yi Wang Xin Gao Ming Peng Yanfei You Fangyun Shi Yazhou Guo Baoyu Zhao Chenchen Wu Northwest A & F University Animal Medical College Yangling China

Locoweed is a poisonous plant that severely harms the development of grass-land and animal husbandry throughout the world. Oxytropis and Astragalus are the Latin names for the poisonous plants commonly known as locoweed. The main toxic substance in these plants is swainsonine. It is a strong inhibitor of lysosomal α-mannosidase I and Golgi body α-mannosidase II, resulting in the accumulation of oligosaccharides and glycoproteins in lysosomes, interfering with the molecular and cellular recognition of glycans, and causing tissue-cell vacuolar degeneration. Livestock shows a series of clinical and pathological symptoms, mainly for the decline of reproductive performance. The effects in dams are abortion, weak fetus, and fetal malformations. The key step in maintaining pregnancy in dams is early endometrial decidualization, because reproductive hormones, decidual cell apoptosis, endoplasmic reticulum (ER) stress, and other immune factors are negatively affected by swainsonine. This article addresses the modifications that occur through glycan processing and glycosylation resulting in the change of post-translational modification of the protein and the activity of the glycoprotein, and then direct and indirect mechanisms of ER stress, apoptosis, reproductive hormones, immune factors, and cell cycle and other pathways. Our aim is to find new methods of prevention and treatment of swainsonine poisoning in grassland animals.

关键词： swainsonine Glycosylation Modification Abortion Decidua Hormone Cell Apoptosis Endoplasmic Reticulum Stress

Preparation of Polyclonal Antibody Against swainsonine and Its Effects in Treatment of Oxytropis glabrapoisoned Rabbits

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Animal Husbandry and Feed Science 2014年第6期6卷 291-295,315页

作者： Chen Genyuan Jia Qizhen Pan Yiwei Jia Shanling Wang Shuai Key Laboratory of Tarim Animal Husbandry Science and Technology Xin Jiang Production & Construction Corps College of Life Science Tarim University College of Animal Science Tarim University

This study was conducted to optimize immunization program to gain the serum against swainsonine （SW） with high titer and to analyze the effects of polychinal antibody in treatment of loco disease of rabbits. Eighteen rabbits were randomly separated into control group, poisoning group and curing group, with six rabbits in each group. Rabbits in poisoning group and curing group were fed 10 g/（kg ~ d） powder of Oxytropis glabra DC every morning for 70 d till the rabbits in poisoning group began to die. From the 21＇t to 24＇h d of O. glabra administration, each of the rabbits in curing group was injected with 1 mL of polyclonal anti- body against SW every day. Blood samples were collected before O. glabra challenge, and then once every 7 d for the serological and immunological evaluation of serum. The resuhs showed that the serum alkaline phosphatase （AKP） activity and SW content in poisoning groups were significantly higher than those in control group on the 7th d （P 〈0.05 ） ; the serum aspartate transaminase （AST） and lactate dehydrogenase （LDH） activity in poisoning groups were significantly higher than those in control group on the 14th d （P 〈 0.05 ）, while the serum ct - mannosidase （AMA） and rate of E-rosette formation in poisoning groups were signifi- cantly lower than those in control group （ P 〈 0.05 ） ; the serum blood urea nitrogen （BUN）, creatinine （ CRE ） and glucose （ GLU ） concentration in poisoning groups were significantly higher than those in control group on the 21＇t d （P 〈 0.05 ）. By injecting serum against swainsonine, the serum AKP, LDH, AST, alanine transaminase （ALT） activity and contents of BUN, CRE, GLU, SW were reduced and serum AMA and rate of E-rosette formation were increased in curing group, by comparing with those in poisoning group. These results in this experiment indicated that polyclonal antibody against SW had good value of preventing from O. glabra DC.

关键词： Oxytropis glabra DC swainsonine Polyclonal antibody Treatment Rabbit

抗癌药swainsonine的实验与临床研究进展

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中国肿瘤临床 1996年第11期23卷 822-825页

作者：陶厚权上海第二医科大学瑞金医院外科上海市200025

swainsonine是首先从澳大利亚植物Swainsona canescens中分离出来的一个in-dolizidine碱,后来又从北美植物Astragalus和Oxytropis纯化获得。近年来研究表明。

关键词：抗癌药 swainsonine 临床研究实验研究

SmI2促进下手性硝酮与醛酮交叉耦联反应的方法学研究暨swainsonine立体异构体的不对称合成研究

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SmI2促进下手性硝酮与醛酮交叉耦联反应的方法学研究暨Swainsonin...

作者：徐守强厦门大学

学位级别：硕士

含(3S,4R)-3,4-二羟基吡咯烷结构的天然产物是为数众多具有生理活性的一类化合物,在医药和生化上有广阔的应用前景。关于这类化合物的不对称合成是当前有机合成界的一大热点,尤其是N-α位含羟烷基侧链的这类化合物的不对称合成,则是其... 详细信息

含(3S,4R)-3,4-二羟基吡咯烷结构的天然产物是为数众多具有生理活性的一类化合物,在医药和生化上有广阔的应用前景。关于这类化合物的不对称合成是当前有机合成界的一大热点,尤其是N-α位含羟烷基侧链的这类化合物的不对称合成,则是其中的研究重点。然而对于多羟基生物碱,如:(-)-swainsonine,一种简洁有效的逆合成分析是导向(3S,4R)-3,4-二羟基吡咯烷N-α位羟烷基化。对于N-α位羟烷基化方法,一种条件温和且高效的新方法是基于硝酮在SmI促进下与醛、酮发生类频那醇(pinacol-type)耦联反应的N-α位羟烷基化方法。该方法已有的研究集中于分子内的反应或是非手性分子间的反应,而对手性硝酮与醛、酮的反应及其在天然生物碱不对称合成中的应用则是一个有待于研究且具有挑战性的课题。因此本论文的目的之一是研究(3S,4R)-3,4-二羟基吡咯烷N-α位羟烷基化,即手性硝酮5在SmI促进下立体选择性地形成N-α位羟烷基化方法,并基于建立的N-α位羟烷基化方法,研究其在吲哚里西啶生物碱(-)-swainsonine的不对称合成中的应用。取得结果如下: 一、研究了手性硝酮5在SmI促进下与醛、酮发生类频那醇反应的化学产率和立体选择性及立体选择性产生的可能机理;研究了不同羰基化合物在不同的反应条件下的影响,以49-91%的产率得到N-α位羟烷基化产物。由于产物的N-OH键可以很方便的切除得到胺,从而建立了一条高效的(3S,4R)-3,4-二羟基吡咯烷N-α位羟烷基化方法。二、由建立的N-α位羟烷基化方法,经过4步反应以39%的总产率得到两个产物:(-)-8a-epi-swainsonine 2和(-)-8,8a-di-epi-swainsonine 3(其中:(-)-8a-epi-swainsonine 2产率为24%;(-).8,8a-di-epi-swainsonine 3产率为15%)。许多具有生理活性的生物碱都含有(3S,4R)-3,4-二羟基吡咯烷片段。天然产物1,4-dideoxy-1,4-imino-D-ribitol、(-)-swainsonine的几个可行的逆合成分析最终都导向(2R,3R)-2,3-二羟基-γ-丁内酰胺合成砌块。因而建立一条简洁高效的(2R,3R)-2,3-二羟基-γ-丁内酰胺的合成方法具有十分重要意义。因此本论文的另一目的是由简单易得的原料(2R,3R)-2,3-二羟基-γ-丁内酯出发,建立一条简单易行的(2R,3R)-2,3-二羟基-γ-丁内酰胺的合成路线,并利用该合成砌块[(2R,3R)-2,3-二羟基-γ-丁内酰胺]设计合成LRB(1,4-dideoxy-1,4-imino-L-ribitol),取得结果如下: 一、由双羟基丙酮叉保护的(2R,3R)-2,3-二羟基-γ-丁内酯出发,经过三步反应以50%的总产率得到了(2R,3R)-2,3-二羟基-γ-丁内酰胺38。与文献报道的路线相比,该路线所用原料易得,实验操作简单。二、由双羟基保护的(2R,3R)-2,3-二羟基-γ-丁内酰胺出发,经6步反应,以58%的总产率得到了立体单一的LRB盐酸盐。

关键词：硝酮二碘化钐 N-α位羟烷基化不对称合成吡咯烷 swainsonine γ-丁内酰胺 LRB

吲哚里西啶生物碱swainsonine及环肽内酯Thalassospiramides类分子中刚性环的合成研究

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吲哚里西啶生物碱Swainsonine及环肽内酯Thalassospiramides类分...

作者：王晓玲复旦大学

学位级别：硕士

天然产物的合成是天然产物化学与有机合成化学的交叉研究领域,是发展有机合成方法学与策略的驱动力,是发现新反应、新试剂、新方法、新理论的重要途径。天然产物的结构修饰、改造和构效关系研究是合理、安全、有效利用天然产物的直接途... 详细信息

天然产物的合成是天然产物化学与有机合成化学的交叉研究领域,是发展有机合成方法学与策略的驱动力,是发现新反应、新试剂、新方法、新理论的重要途径。天然产物的结构修饰、改造和构效关系研究是合理、安全、有效利用天然产物的直接途径,也是发现新药的重要源泉。多羟基吲哚（吡咯）里西啶类生物碱是一类重要的广泛存在于自然界的含氮杂环生物碱。由于该类生物碱绝大多数都具有广泛的生物活性和独特的化学结构,近年来,得到了众多有机合成化学家和药物学家的青睐。例如,从真菌Rhizoctonia leguminicola中分离得到的一类重要的具有抗癌活性和免疫增强活性的多羟基类吲哚里西啶生物碱swainsonine及其异构体在近30年来引起了广泛的研究。海洋天然产物的研究已成为近半个世纪天然产物化学研究的热点之一。由于海洋天然产物的活性更为广泛,结构更为复杂,且含量极低,仅靠分离的手段获取海洋天然产物已不能满足药理学等进一步的研究需要。因此,海洋天然产物的不对称合成已成为有机合成化学研究的最主要内容之一。本论文在天然产物类似物、关键中间体及分析方法上开展研究工作,主要取得如下结果：首先,本论文在小组建立的以谷氨酸制备合成砌块2-64的基础上,经6步反应制备了酮2-80,发展了以Li（t-BuO）3A1H为还原剂将其高选择性地还原为醇2-81的方法（dr=95：5）,再经过文献类似方法转化,完成了（-）-8a-epi-swainsonine的不对称合成。本文建立了一条基于廉价谷氨酸合成具有重要活性多羟基吲哚里西啶生物碱及其类似物的不对称合成新方法。其次,本论文建立了合成海洋天然产物Thalassospiramides A和B骨架环中三个关键片段的合成方法。环肽内酯Thalassospiramides A和B是Fenical等人2006年从海洋放线菌Thalassospir中分离得到的一种具有抗炎活性的次生代谢物,由于其结构复杂,特别该类分子中含有一个刚性很强的12员环肽内酯骨架结构,合成较为困难。本文具体实现了酪氨酸氨基的选择性单甲基化反应,高收率地制备得到了化合物3-16;建立了羟甲基氨基醇反式双键片段3-37的合成方法;研究了各片段之间连接的较佳缩合条件;探索了海洋天然产物Thalassospiramides A和B分子中刚性环3-41的成环条件。这些工作,为小组继续开展该类分子的不对称合成和活性评价等研究奠定了基础。

关键词：不对称合成天然产物生物碱 swainsonine Thalassospiramides

Extraction and GC Study on swainsonine from Locoweed, Astragalus strictus in Tibet

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Extraction and GC Study on Swainsonine from Locoweed, Astrag...

抗癌药swainsonine的基础与临床研究进展

第十五届中国科协年会第21分会场：中药与天然药物现代研究学术研讨会

作者： HAO Baocheng YANG Xianpeng WANG Xuehong LIU Jianzhi WANG Baohai LIU Yu GUO Wenzhu GUO Zhiting SHANG Ruofeng HU Yonghao LIANG Jianping Institute of Husbandry and Pharmaceutical Sciences of CAAS

Locoweed is a poisonous plant, which wildly distributed in most area of the world, it can cause livestock poisoning or death with significant economic loss. The Astragalus strictus belongs to a species of locoweed .It is mainly distributed in Tibet of China and is a serious hazard to the local livestock industry. The objective of this study is extracting and purifying condition of swainsonine from Astragalus strictus with the microwave-assisted extraction method. An optimum extracting technology of SW from Astragalus strictus was investigated through the orthogonal experiment under the microwave assistance conditions, then the content of swainsonine was analyzed with gas chromatography(GC)method. The optimized extraction conditions were as follow: at room temperature, the time of using the petroleum ether ultrasonic to make the swainsonine degreased with ultrasonic was 1h, and then use the method of extraction with microwave-assisted, solid-liquid ratio (M: V) 1:10, microwave frequencies 280W , extraction time 20 s. Under the above conditions, the extraction percentage of the swainsonine was 0.009264%.Extracting swainsonine with microwave-assisted extraction method has characteristics of rapid, efficient, convenient and low energy consumption. It is benefit for producing swainsonine from Astragalus strictus.

关键词： extraction Astragalus strictus swainsonine microwave gas chromatography (GC)

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国外医药（合成药．生化药．制剂分册） 1997年第1期18卷 34-36页

作者：陶厚权上海第二医科大学瑞金医院外科

Effect of SW of Oxytropis glabra DC. on α-mannosidase gene relative expression of mice liver

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畜牧与饲料科学 2015年第Z1期 104-109页

作者： WANG Yu ZHANG Jianjun LIU Zhanjiang HAN Min Ministry of Agriculture Key Laboratory of Clinical Diagnosis and Treatment Technology in Animal Disease College of Veterinary Medicine Inner Mongolia Agricultural University

[Background]Oxytropis glabra *** whole plant toxin is one of locoweed and it widely distributes in the western region of Inner *** livestocks cause chronic poisoning after *** primary toxicant that Oxytropis glabra *** livestock poisoning is swainsonine(SW).The study investigates toxicated mechanism of Oxytropis glabra by detecting liver α-mannosidase gene relative expression in different time of mice drenched different doses of SW.[Methods]The animal tissue total RNA kit method for the extraction of total RNA of liver;the microplate method for the determination of RNA purity;the gel electrophoresis for the determination of RNA integrity and the real-time quantitative PCR for the detection of a-mannosidase gene transcription.[Results]Each experimental group and the control group of α-mannosidase gene were expressed,but the transcript expression levels of different groups are *** with the control group,low dose SW can promote liver a-mannosidase gene expression,and the promoting results are more obvious with the test *** and middle dose SW can also improve the α-mannosidase gene relative expression at the initial stage,but it can severely inhibit α-mannosidase gene expression over a long period of time and the inhibiting results are more obvious with the test conducting.[Conclusion]Low dose SW can promote liver α-mannosidase gene ***,high and middle dose SW can inhibit *** Oxytropis glabra *** toxic effect.

关键词： Oxytropis glabra DC swainsonine gene expression