Application of alkaloid compound namely 5-hydroxypyrrolidine-2-ketone in preparation of anticomplement drug
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A technology of hydroxypyrrolidine and alkaloids, which is used in drug combinations, antipyretics, anti-inflammatory agents, etc.
Active Publication Date: 2018-01-30
SHIHEZI UNIVERSITY
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[0004] So far, there has been no report about the alkaloid compou
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[0026] 取补体(人血清)0.2ml,加入AP稀释液(巴比妥缓冲液,pH 7.4,含5 m Mg 2+ ,8 mMEGTA)配制成1:5的溶液,并对倍稀释成1:10、1:20、1:40、1:80、1:160、1:320和1:640的溶液,取各浓度补体0.15ml、AP稀释液0.15ml及0.5%兔红细胞(RE)0.20 ml,混匀,37℃水浴30 min后置于低温高速离心机,在5000 rpm、4℃条件下离心10 min,分别取每管上清0.2 ml于96孔板,在405nm测定吸光度,实验同时设置全溶血组(0.20 ml 0.5%RE溶于0.3 ml三蒸水),以三蒸水溶血管的吸光度作为全溶血标准,计算溶血率,以补体稀释度为X轴,各稀释浓度补体造成的溶血百分率为Y轴作图,选择达到相似高溶血率的最低补体浓度作为确保体系能正常溶血所需的临界补体浓度,取确定的临界浓度的补体与供试品混匀,于37℃预水浴10min后,加入0.,2 ml 0.5%RE,将每管37℃水浴30 min后置于低温高速离心机,5000 rpm、4℃条件下离心10 min后,分别取每管上清0.2 ml于96孔板,405 nm下测定其吸光度,实验同时设置供试品对照组、补体组和全溶血组,将供试品吸光度值扣除相应供试品对照组吸光度值后计算溶血率,以供试品浓度作为X轴,溶血抑制率作为Y轴作图,计算50%抑制溶血所需供试品的浓度(AP 50 );体外抗补体旁路途径试验结果如表1所示。
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Abstract
The invention belongs to the field of preparation of traditional Chinese medicines, and relates to an application of an alkaloid compound namely 5-hydroxypyrrolidine-2-ketone in preparation of an anticomplement drug. According to the invention, the alkaloid compound namely 5-hydroxypyrrolidine-2-ketone is separated from the n-butanol extraction part of an ethanol extract of a dried whole Borraginaceae plant namely Anchusaitalica Retz.; meanwhile, in-vitro anticomplement activity evaluation experiment results verify that the alkaloid compound namely 5-hydroxypyrrolidine-2-ketone has strong inhibitory effects on the classical pathway and the alternative pathway of a complement system. The alkaloid compound namely 5-hydroxypyrrolidine-2-ketone has a CH50 value of 83 [mu]g/ml and an AP50 valueof 77 [mu]g/ml, and can be used as an active ingredient for preparation of the anticomplement drug.
Description
technical field [0001] 本发明属中药制药领域,涉及从维药牛舌草中分离得到的生物碱类化合物5-羟基吡咯烷-2-酮在制备抗补体药物中的用途。 Background technique [0002] 现有技术公开了补体系统的过度激活会引发系统性红斑狼疮、类风湿性关节炎、急性呼吸窘迫综合征等多种重大疾病。抗补体药物研究多年来一直是世界药学研究的热点和重点。然而目前对此类疾病尚缺乏较为理想的治疗药物,因此临床上急需高效、低毒、专一的新型补体抑制剂。从天然产物中研究开发补体抑制剂是近年来一个受到越来越多关注的重要研究领域,其具有成本低、毒性低等特点。国内外学者已从包括海洋生物等在内的多种天然产物中分离得到大量具有补体系统抑制作用的单体化合物,为抗补体药物的研究与开发提供了广阔的前景。 [0003] 维药牛舌草为紫草科植物意大利牛舌草( Anchusa italica Retz.)的干燥全草。味微甘酸。具有生湿生热,调节异常黑胆质,生湿补脑,祛寒补心,爽心悦志,润燥消炎,止咳平喘的功效。现有技术对维药牛舌草的药理研究仅集中在抗氧化和抗菌等方面,化学成分研究发现了一些三萜类、黄酮类、生物碱类和木质素类化合物。 [0004] 迄今为止尚未见有关生物碱类化合物5-羟基吡咯烷-2-酮具有补体抑制活性的报道。 Contents of the invention [0005] 本发明的目的是提供新的具有抗补体活性的物质,具体涉及从维药牛舌草中分离得到的生物碱类化合物5-羟基吡咯烷-2-酮。 [0006] 本发明的进一步目的是提供上述维药牛舌草中生物碱类化合物在制备抗补体药物中的用途。 [0007] 本发明所述的抗补体活性生物碱类化合物具有以下化学结构: [0008] [0009] 本发明所述的生物碱类化合物通过下述方法制备: [0010] 取干燥的意大利牛舌草全草,粉碎,用95%乙醇室温冷浸5次,合并提取液并浓缩至无醇味,浸膏加水稀释,依次以等体积石油醚(60-90℃)、乙酸乙酷、正丁醇萃取3次,合并正丁醇萃取液并浓缩至干,即得正丁醇萃取物;正丁醇萃取部位经硅胶柱色谱分离,依次以氯仿-甲醇(氯仿, 50:1, 30:1, 15:1, 9:1, 7:1, 5:1, 3:1, 2:1, 1:1...
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