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抗癌药Swainsonine的实验与临床研究进展 被引量:5
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作者 陶厚权 《中国肿瘤临床》 CAS CSCD 北大核心 1996年第11期822-825,共4页
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
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抗癌药Swainsonine的基础与临床研究进展 被引量:6
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作者 陶厚权 《国外医药(合成药.生化药.制剂分册)》 1997年第1期34-36,共3页
关键词 抗肿瘤药 swainsonine 临床应用 研究
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Isolation and NMR Study on Swainsonine from Locoweed,Astragalus strictus 被引量:8
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作者 ZHAO Bao-yu LIU Zhong-yan +3 位作者 WANG Jian-jun SUN Li-sha WANG Zhan-xin WANG Yin-chao 《Agricultural Sciences in China》 CAS CSCD 2009年第1期115-120,共6页
Locoweed is a poisonous plant wildly distributed in most area of the world and can cause livestock poisoning or death with significant economic loss. The principal responsible for its toxicity is indolizidine alkaloid... Locoweed is a poisonous plant wildly distributed in most area of the world and can cause livestock poisoning or death with significant economic loss. The principal responsible for its toxicity is indolizidine alkaloid swainsonine, a new potential anticancer and antiviral drug. Astragalus strictus is mainly distributed in Tibet of China and is a serious hazard to the local livestock industry. To analyze its main toxic ingredients and supply more structural information and more accurate data, swainsonine has been isolated from this plant by D101 macroporous resin and the ^1H and ^13C chemical shifts of the compound has been assigned by 1D-NMR and 2D-NMR techniques. At the same time, complete assignments of swainsonine's ^13C spectral signals are reported. 展开更多
关键词 chemical shift assignment LOCOWEED NMR swainsonine
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Swainsonine对胰岛素受体功能影响的研究
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作者 戚维维 陈惠黎 《生物化学杂志》 CSCD 1995年第1期55-60,共6页
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... 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。 展开更多
关键词 swainsonine 胰岛素 胰岛素受体 细胞膜
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Preparation of Polyclonal Antibody Against Swainsonine and Its Effects in Treatment of Oxytropis glabrapoisoned Rabbits
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作者 Chen Genyuan Jia Qizhen +2 位作者 Pan Yiwei Jia Shanling Wang Shuai 《Animal Husbandry and Feed Science》 CAS 2014年第6期291-295,315,共6页
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. Eightee... 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. 展开更多
关键词 Oxytropis glabra DC swainsonine Polyclonal antibody TREATMENT RABBIT
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The Mechanism of Swainsonine Causing Early Pregnancy Abnormal Decidualization and Inducing Abortion by Changing Glycosylation Modification
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作者 Yi Wang Xin Gao +5 位作者 Ming Peng Yanfei You Fangyun Shi Yazhou Guo Baoyu Zhao Chenchen Wu 《Advances in Reproductive Sciences》 2018年第3期70-101,共32页
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 locowe... 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. 展开更多
关键词 swainsonine GLYCOSYLATION Modification ABORTION DECIDUA Hormone Cell Apoptosis Endoplasmic Reticulum Stress
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Advance of swainsonine biosynthesis 被引量:4
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作者 Xiang-mei Tan Amanda Juan Chen +2 位作者 Bin WU Gui-Shan Zhang Gang Ding 《Chinese Chemical Letters》 SCIE CAS CSCD 2018年第3期417-422,共6页
Swainsonine (1) belongs to the family of indolizine alkaloid with strong neurologically toxic effects on herbivorous livestock. Recently, a great amount of evidence confirmed that this alkaloid displayed a wide rang... Swainsonine (1) belongs to the family of indolizine alkaloid with strong neurologically toxic effects on herbivorous livestock. Recently, a great amount of evidence confirmed that this alkaloid displayed a wide range of bioactivities especially anti-cancer biological effects. The potential targets of swainsonine (1) were now revealed to be the mannosidase and Golgi mannosidase 1I. Its low yield in plants or fungi, and no economically total synthesis route in practice as the key bottleneck restricted its further structure- activities relationships (SAR) investigation in drug discovery. This mini-review highlighted the biosynthetic advance of swainsonine (1) from 1973 to 2017 based on the results of isotope-labelled experiments and the recent research of its biosynthetic gene cluster, which could provide some thoughts for further biosynthetic investigation and efficiently biomimetic synthesis of swainsonine (1) in order to increase its output in practice. 展开更多
关键词 swainsonine Indolizine Biosynthesis Isotope-labeled Gene Cluster
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苦马豆素抗牛病毒性腹泻病毒的研究 被引量:21
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作者 郝宝成 武凡琳 +6 位作者 邢小勇 项海涛 温峰琴 王学红 权晓弟 胡永浩 梁剑平 《中国农业科学》 CAS CSCD 北大核心 2014年第1期170-181,共12页
【目的】疯草是中国西部影响草地生态和畜牧业健康发展的毒草之一。主要有豆科棘豆属和黄芪属有毒植物等,在冬季牧草严重缺乏的时节,牛羊等牲畜被迫采食后可引起中毒和生产性能下降,甚至死亡,每年给我国草地生态和畜牧业造成的直接经济... 【目的】疯草是中国西部影响草地生态和畜牧业健康发展的毒草之一。主要有豆科棘豆属和黄芪属有毒植物等,在冬季牧草严重缺乏的时节,牛羊等牲畜被迫采食后可引起中毒和生产性能下降,甚至死亡,每年给我国草地生态和畜牧业造成的直接经济损失达几十亿元,是危害最严重的毒草。目前,我国西部天然草地动物因疯草中毒死亡所造成的经济损失仍持续剧增。苦马豆素被认为是引起动物疯草中毒的主要毒性成分。由于疯草分布广泛,资源丰富,如何改善草地生态,合理开发利用疯草成为研究的课题和方向。近几十年来,随着对疯草研究的深入和扩展,人们发现苦马豆素不仅具有良好的抗肿瘤效果,还可作为免疫调节剂、抗HIV及扩散抑制剂、抗病毒和细胞保护剂等药物使用。目前,国内在对苦马豆素抗肿瘤、调节机体免疫方面研究较热,但是,对苦马豆素在抗病毒活性、作用机理方面的研究尚无相关报道。为了探讨茎直黄芪中生物碱苦马豆素(swainsonine,SW)抗牛病毒性腹泻病毒(bovine viral diarrhea virus,BVDV)的作用机制,明确其体外抗病毒作用效果,为抗BVDV的药物筛选提供参考依据。【方法】利用细胞培养技术,采用CPE观察法和MTT比色法相结合的方法测定不同浓度SW对牛肾原代细胞(madin-darby bovine kidney cells,MDBK)的毒性作用,确定药物的安全浓度和TD50,并分别采用先加药后感染病毒、先感染病毒后加药、药毒作用2 h后加入、感染病毒同时给药后再加药四种作用方式,检测不同浓度SW对BVDV入侵的阻断作用、复制的抑制作用、直接杀伤作用和综合作用,并计算不同作用方式下的治疗指数。【结果】结果显示:SW浓度小于0.256μg·mL-1范围内对MBDK细胞无毒性作用,在大于0.512μg·mL-1浓度下MBDK细胞表现出一定程度的病变,TD50为2.512μg·mL-1,按Reed-Muench氏法计算BVDV TCID50为10-4.7/0.1mL;在体外随苦马豆素质量浓度的增加,其抗BVDV作用具有很好的量效关系,且与作用方式有关,比较四种作用方式下的治疗指数1.05、2.47、2.08和3.21,说明SW对BVDV的综合作用(65.29%,P<0.01)和复制(65.05%,P<0.01)的抑制作用较好,亦有一定的直接杀伤作用,但对其入侵的阻断作用不佳。【结论】SW在体外有良好抗BVDV活性作用,并推测苦马豆素(SW)抗病毒的主要效应可能是SW能进入细胞内抑制BVDV的复制增殖以及直接灭活游离BVDV而发挥作用。 展开更多
关键词 茎直黄芪 苦马豆素(SW) 牛病毒性腹泻病毒(BVDV) 抗病毒 swainsonine (SW) bovine viral diarrhea virus (BVDV)
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离子抑制色谱法测定棘豆属植物提取物中的苦马豆素 被引量:15
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作者 郭治安 张小辉 +2 位作者 赵景婵 袁红安 梁小云 《色谱》 CAS CSCD 北大核心 2006年第6期656-656,共1页
关键词 离子抑制色谱法(ion suppression chromatography) 苦马豆素(swainsonine) 植物提取物(plant extract) 棘豆属植物(Oxytropis)
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气相色谱-甲基化-α-D-甘露糖苷内标法测定变异黄芪中的苦马豆素 被引量:14
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作者 赵兴华 崔忠华 +4 位作者 耿果霞 王建华 张志敏 宋毓民 刘志滨 《色谱》 CAS CSCD 北大核心 2007年第5期781-782,共2页
建立以甲基化-α-D-甘露糖苷为内标物,用气相色谱测定变异黄芪中苦马豆素的方法。植物样品经甲醇超声提取、氯仿去除杂质后,将碱性正丁醇萃取物用硅烷化试剂进行衍生化,通过AT.SE-54毛细管柱分离,氢火焰离子化检测器检测,测得变异黄芪... 建立以甲基化-α-D-甘露糖苷为内标物,用气相色谱测定变异黄芪中苦马豆素的方法。植物样品经甲醇超声提取、氯仿去除杂质后,将碱性正丁醇萃取物用硅烷化试剂进行衍生化,通过AT.SE-54毛细管柱分离,氢火焰离子化检测器检测,测得变异黄芪干草粉中苦马豆素含量为115.7mg/kg,加标回收率为82.6%~94.0%,相对标准偏差为2.8%。该方法能用于疯草样品中苦马豆素的含量检测。 展开更多
关键词 气相色谱(GC) 疯草(locoweed) 苦马豆素(swainsonine) 衍生化(derivatization)
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苦马豆素人工抗原免疫小鼠的安全性试验
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作者 陈根元 王帅 +3 位作者 张玲 吴书奇 胡建军 马春晖 《湖北农业科学》 北大核心 2013年第14期3370-3372,3377,共4页
通过分析苦马豆素(Swainsonine,SW)人工抗原SW-OVA对小鼠机体的影响,进行安全性评价。将36只昆明种小鼠随机分为对照组、试验Ⅰ组、试验Ⅱ组,每组12只。试验组依次进行首免和加强免疫,免疫前采血,分析血清生化指标谷草转氨酶(AST)、谷... 通过分析苦马豆素(Swainsonine,SW)人工抗原SW-OVA对小鼠机体的影响,进行安全性评价。将36只昆明种小鼠随机分为对照组、试验Ⅰ组、试验Ⅱ组,每组12只。试验组依次进行首免和加强免疫,免疫前采血,分析血清生化指标谷草转氨酶(AST)、谷丙转氨酶(ALT)、碱性磷酸酶(AKP)、乳酸脱氢酶(LDH)、α-甘露糖苷酶(AMA)、尿素氮(BUN)的变化,血常规指标红细胞数(RBC)、白细胞数(WBC)、淋巴细胞数(LYM)、血小板数(PLT)和血红蛋白含量(HGB)的变化,同时检测免疫组血清中有无SW,并观察小鼠脏器系数及其形态学变化。结果表明,免疫组小鼠与对照组小鼠血清生化指标、血常规指标和脏器系数差异不大,免疫小鼠血清中未检出SW,镜检未见免疫小鼠器官出现中毒现象。合成的人工抗原SW-OVA具有较好的安全性。 展开更多
关键词 苦马豆素(swainsonine SW) 人工抗原 免疫 小鼠
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