CN106138147A - 重瓣金光菊在制备黄嘌呤氧化酶抑制剂中的应用 - Google Patents
重瓣金光菊在制备黄嘌呤氧化酶抑制剂中的应用 Download PDFInfo
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Abstract
本发明涉及一种重瓣金光菊在制备黄嘌呤氧化酶抑制剂中的应用,属于中药领域。重瓣金光菊及其提取物作为活性组分在制备黄嘌呤氧化酶抑制剂中的用途,其中所述重瓣金光菊及其提取物包含所述重瓣金光菊原植物、及其溶剂提取物,其中所述溶剂提取物为水、乙醇、甲醇提取物。本发明的有益效果是:解决了高尿酸血症、痛风等相关疾病的血尿酸异常升高的问题,并间接的解决、缓解了高尿酸血症、痛风等疾病所导致的关节疼痛、肿胀变形及高血压、糖尿病、心血管疾病、肾脏疾病、代谢综合征等疾病的相关症状。
Description
技术领域
本发明涉及中药领域,特别涉及中药源黄嘌呤氧化酶抑制剂。
背景技术
体内尿酸水平持续偏高达过饱和会使尿酸钠晶体沉积在关节及周围组织中,造成一种嘌呤类代谢性疾病——痛风。高尿酸血症是痛风的重要标志,大约有5%~12%的高尿酸血症最终会发展成痛风,80%~90%的痛风患者伴随有高尿酸血症。此外,高尿酸血症还与高血压、糖尿病、心血管疾病、肾脏疾病、代谢综合征等疾病的发生密切相关。痛风的发病率地区间差异较大,尼日利亚其发病率只有0.03%,而台湾的土著居民中其发病率高达15.2%。流行病学调查显示,由于人们生活水平的提高,饮食的日益改善尤其是啤酒、动物内脏等高嘌呤性食物的摄入过多,导致痛风的发病率呈日渐上升的趋势。
传统的抗痛风药物主要包括促尿酸排泄药(如丙磺舒、苯溴马隆等)和尿酸生成抑制剂(如别嘌呤醇等)两大类,而尿酸生成抑制剂主要为黄嘌呤氧化酶抑制剂。黄嘌呤氧化酶(Xanthine Oxidase,简称XOD)是一种复合黄素蛋白酶,是人体内产生尿酸过程中的一种极其重要的酶,它能够催化体内的黄嘌呤和次黄嘌呤生成尿酸和过氧化物自由基,因此通过抑制其活性可达到防止或减少尿酸产生的作用。近年来,黄嘌呤氧化酶抑制剂作为一种极有效的抗痛风药物而受到国内外学者的广泛关注,由于传统的黄嘌呤氧化酶抑制剂别嘌呤醇的副作用如药物超敏反应综合征、史蒂文生氏-强生症候群等,从天然药物中发掘黄嘌呤氧化酶抑制剂将成为研究热点。现有的文献记载了对17种中药的黄嘌呤氧化酶抑制剂的筛选,以及花生四烯酸可以作为黄嘌呤氧化酶抑制剂(CN102133214),节杆菌可以生产黄嘌呤氧化酶抑制剂(CN101402922),中药组方提取物作为黄嘌呤氧化酶抑制剂(CN102205083),通过烘干、粉碎、超声提取、过滤、浓缩、干燥得到蔬菜提取物也可以用作黄嘌呤氧化酶抑制剂(CN102106516),以及以海参为原料制备黄嘌呤氧化酶抑制剂(CN102138938,CN102580063)。
我们在对长白山地区的近百种药用植物活性筛选过程中,发现了几种具有较强黄嘌呤氧化酶抑制活性的植物,其中就包括重瓣金光菊。
重瓣金光菊Rudbeckia laciniata var,属于菊科金光菊属植物。原产地北美洲,常用于布置花境或自然植于路边及林缘。多年生草本,高60~180厘米。茎分枝;上部叶片阔披针形,叶较宽,基生叶羽状5~7裂;茎生叶3~5裂,边缘具稀锯齿。头状花序具长柄,花径10~20厘米,黄色,重瓣,花期6—8月。目前,对重瓣金光菊的研究主要集中在其栽培、养护及绿化用途上,而对其生物活性及化学成分方面未见文献报道。
发明内容
本发明提供一种重瓣金光菊在制备黄嘌呤氧化酶抑制剂中的应用,以解决高尿酸血症、痛风等相关疾病的血尿酸异常升高的问题。
本发明采取的技术方案是:重瓣金光菊及其提取物作为活性组分在制备黄嘌呤氧化酶抑制剂中的用途,其中所述重瓣金光菊及其提取物包含所述重瓣金光菊原植物、及其溶剂提取物,其中所述溶剂提取物为水、乙醇、甲醇提取物。
本发明还提供重瓣金光菊及其提取物的另一种应用,该应用为治疗高尿酸血症、痛风等相关疾病提供一种新的食品、食品添加剂、保健食品、药品。
所述的重瓣金光菊及其提取物用于制备治疗高尿酸血症、痛风相关疾病的食品、食品添加剂、保健食品、药品的应用,通过下述方法制备:
1.取重瓣金光菊,干燥,粉碎,附加药学可以接受的辅料,制成片剂、胶囊剂、散剂、丸剂等药学上可以接受的剂型。
2.取重瓣金光菊,以水、乙醇或甲醇等溶剂提取,浓缩至干,得到重瓣金光菊提取物,以该提取物为原料,附加药学可以接受的辅料,制成片剂、胶囊剂、散剂、丸剂、软胶囊等药学上可以接受的剂型。
3.取重瓣金光菊,以水、乙醇或甲醇等溶剂提取,浓缩至干,得到重瓣金光菊提取物,以该提取物为原料制成液体饮料、固体饮料、压片糖果等食品、保健食品可以接受的形式。
本发明的有益效果是:解决了高尿酸血症、痛风等相关疾病的血尿酸异常升高的问题,并间接的解决、缓解了高尿酸血症、痛风等疾病所导致的关节疼痛、肿胀变形及高血压、糖尿病、心血管疾病、肾脏疾病、代谢综合征等疾病的相关症状。
附图说明
图1是RLC对黄嘌呤氧化酶动力学考察Linewaver-Burk双倒数曲线图;
图2是RLT对黄嘌呤氧化酶动力学考察Linewaver-Burk双倒数曲线图;
图3是RLOL对黄嘌呤氧化酶动力学考察Linewaver-Burk双倒数曲线图。
具体实施方式
实施例1急性毒性试验
因限于给药浓度及给药体积,未能测出小鼠灌胃给药的LD50,重瓣金光菊生药粉碎后水悬液、水提取物、乙醇提取物、甲醇提取物的水溶液以90ml/kg剂量给小鼠灌胃给药,动物状态良好,未见急性毒性反应,小鼠一日内灌胃给药的最大剂量为≥90ml(四种提取物分别相当于生药量为125.5g/kg、140.5g/kg、160.0g/kg、165.0g/kg)。
实施例2:重瓣金光菊制备降尿酸产品的应用
1.重瓣金光菊降尿酸胶囊(Rudbeckia laciniata capsule,RLC):收取重瓣金光菊,阴干,粉碎,制成硬胶囊制剂。
2.重瓣金光菊降尿酸片(Rudbeckia laciniata tablet,RLT):收取重瓣金光菊,阴干,粉碎,以10倍量75%乙醇超声提取三次,每次30分钟,过滤,合并滤液,蒸干,粉碎,加淀粉适量,压片。
3.重瓣金光菊降尿酸口服液(Rudbeckia laciniata oral liquid,RLOL):取重瓣金光菊,10倍量水煎煮40分钟,过滤,滤液浓缩得流浸膏,加辅料,制成口服液。
实施例3:重瓣金光菊降尿酸产品活性研究
1材料
1.1药材与试剂
重瓣金光菊Rudbeckia laciniata采自长白山脉临江地区,黄嘌呤(xanthine,XA)、黄嘌呤氧化酶(xanthine oxidase,XOD),购自美国Sigma公司;别嘌醇,购自上海阿拉丁试剂公司;其他试剂均为国产分析纯。
1.2仪器
Thermo Multiskan GO型全波长酶标仪(赛默飞世尔科技);ABS 320-4N型分析天平(上海岛韩实业有限公司);KQ-250B型数控超声波清洗器(昆山市超声仪器有限公司);RE-52AA旋转蒸发器(上海亚荣生化仪器厂);DZF6020真空干燥器(上海一恒科学仪器有限公司)。
2方法
对文献[李英,陈君,李萍.金银花中酚酸类和黄酮类成分的黄嘌呤氧化酶抑制活性.中国药科大学学报,2011,42(5):407]中的黄嘌呤氧化酶抑制剂筛选方法进行了改良。
2.1溶液配制
磷酸盐缓冲液配制(0.2mol·L-1pH=7.5):A液(0.2mol·L-1磷酸二氢钾):取磷酸二氢钾(KH2PO4,MW136.09)1.361g,加双蒸水使溶解并定容至100ml。B液(0.2mol·L-1磷酸氢二钠):取磷酸氢二钠(Na2HPO4·2H2O,MW177.99)1.78g,加双蒸水溶解并定容至100ml。使用时分别取等量A液和B液混合即可得到pH为7.5的磷酸盐缓冲溶液,现用现配。
底物配制:取黄嘌呤适量,精密称定,加磷酸盐缓冲溶液配成1.5mmol·L-1的黄嘌呤底物溶液。底物溶液需新鲜配制,现用现配。
酶液配制:精密称取黄嘌呤氧化酶1mg,加磷酸盐缓冲溶液配成0.05U·mL-1的黄嘌呤氧化酶溶液。
2.2重瓣金光菊降尿酸产品的样品溶液的配制
重瓣金光菊降尿酸产品见“实施例2”,取相应产品,胶囊取内容物、片剂研为细粉、口服液直接吸取,分别加磷酸盐缓冲溶液配成相应浓度的样品溶液。
2.3产品对黄嘌呤氧化酶活性的影响
按表1顺序分别将相应溶液加入96孔板中加入完毕后震荡2min,于37℃条件下反应10min,用酶标仪测定290nm处的吸光度值,每个样品均作3次重复,取平均值,同时测定相应浓度样品自身的吸光度以扣除干扰,并测无样品时酶与底物反应的吸光度作为空白对照,按照公式计算抑制率。
式中:A1为反应体系中加入样品后的吸光度值,A2为样品溶液自身的吸光度值,A0为空白对照的吸光度值。
本实验以别嘌醇为阳性对照,将高活性(抑制率大于60%)的样品稀释成6个浓度,进行梯度复筛。根据抑制剂的浓度及其平均抑制率,经非线性回归方法计算得各样品的IC50。
表1重瓣金光菊降尿酸产品对黄嘌呤氧化酶抑制作用反应体系(μL)
2.4产品对黄嘌呤氧化酶抑制类型的判断分别吸取不同浓度的产品溶液,再加入不同浓度的底物黄嘌呤(浓度分别为0.012、0.024、0.036、0.048、0.060mmol·L-1),在25℃条件下反应30min,测定反应速度,通过Linewaver-Burk双倒数作图法判断提取物的抑制作用类型。
3结果与分析
3.1产品对黄嘌呤氧化酶的抑制作用
各产品在2mg·mL-1浓度时对黄嘌呤氧化酶的抑制率均大于60%,继续稀释至6个浓度,进行梯度复筛,结果表明呈明显的量-效关系。根据抑制剂浓度及其平均抑制率,经SPSS计算得样品RLC、RLT、RLOL的IC50分别为:1.01mg·mL-1、0.13mg·mL-1、0.28mg·mL-1。别嘌呤醇的IC50为:3.8μM。
3.2各产品对黄嘌呤氧化酶的动力学特征
根据Linewaver-Burk双倒数作图法,得到图1-图3,从图1-图3可以得到重瓣金光菊各产品均为非竞争性抑制剂(三条线交叉于X轴),说明以上产品与黄嘌呤氧化酶活性中心以外的必须基团结合,这种结合不会影响酶与底物的结合,而底物与酶的结合,也不会影响与抑制剂的结合。但酶-底物-抑制剂复合物(ESI)不能进一步变成产物,此种抑制方式,只要抑制剂存在,ESI就不能解脱出来,即底物浓度增加不能降低抑制剂对酶的抑制程度。
实施例4:重瓣金光菊降尿酸食品的制备
1重瓣金光菊袋泡茶:收取新鲜重瓣金光菊,阴干,粉碎、过40目筛,24目筛筛选,紫外线灯杀菌,机械装袋,包装,喷印日期,塑封,入库。
2重瓣金光菊饮料:取重瓣金光菊,10倍量超声处理20分钟,过滤,滤液加苯甲酸、苯甲酸钠等防腐剂,加香味剂调味,灭菌,灌装,喷印日期,包装入库。
Claims (5)
1.重瓣金光菊在制备黄嘌呤氧化酶抑制剂中的应用。
2.重瓣金光菊提取物在制备黄嘌呤氧化酶抑制剂中的应用。
3.根据权利要求2所述的重瓣金光菊提取物在制备黄嘌呤氧化酶抑制剂中的应用,所述重瓣金光菊提取物为重瓣金光菊水提取物、重瓣金光菊乙醇提取物或重瓣金光菊甲醇提取物。
4.如权利要求1所述的重瓣金光菊在制备黄嘌呤氧化酶抑制剂中的应用,所述的制备黄嘌呤氧化酶抑制剂的产品包括食品、食品添加剂、保健食品、药品。
5.如权利要求2所述的重瓣金光菊提取物在制备黄嘌呤氧化酶抑制剂中的应用,所述的制备黄嘌呤氧化酶抑制剂的产品包括食品、食品添加剂、保健食品、药品。
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