CN116808097A - 一种具有降血糖活性的红大戟提取物及其应用 - Google Patents
一种具有降血糖活性的红大戟提取物及其应用 Download PDFInfo
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Abstract
本发明公开了一种具有降血糖活性的红大戟提取物及其应用,该红大戟提取物的制备方法按以下步骤实现:将红大戟的干燥根茎粉碎得到红大戟粉,采用75%的乙醇浸取2‑3次,每次提取5‑7d,得到提取液;(2)在提取液中加3‑4倍量的蒸馏水,静置2‑3天后抽滤,将滤液在50‑60℃下减压浓缩得到浸膏;(3)浸膏加水溶解后,先用石油醚萃取后,剩余部分用乙酸乙酯萃取,将萃取液浓缩后冷冻干燥得到红大戟提取物。本发明提供的红大戟提取物能显著降低STZ导致的糖尿病大鼠的血糖,提高糖尿病大鼠的葡萄糖耐量,改善糖尿病大鼠“三多一少”的症状,具有开发成新型降血糖产品的巨大潜力。
Description
技术领域
本发明属于天然药物技术领域,具体涉及一种具有降血糖活性的红大戟提取物及其应用。
背景技术
糖尿病是一种慢性代谢性疾病,由于其发病机制和因素的复杂性,目前世界上尚未有完全治愈的方法,已成为威胁人类健康的一大疾病。2015年报告显示我国糖尿病患病率和患者死亡率逐年快速增高,而预计到2040年,全球糖尿病患者总数将达到6.42亿。目前临床治疗糖尿病一方面通过二甲双胍、罗格列酮等药物治疗,另一方面通过注射胰岛素来维持血糖,然而西药带来的呕吐、头晕、胃肠道反应等副作用仍是不少患者和家庭的负担。寻找天然毒副作用较小的中药和天然降糖成分依然成为现在的急需解决的目标。
红大戟为茜草科 Rubiaceae红芽大戟属 Knoxia红大戟Knoxia roxburghii(Spreng.) M. A. Rau的干燥根,别名红芽大戟、云南大戟、紫大戟、广大戟。其野生资源主要分布于云南、广西、广东等地区,海拔1300-1500m地区,海拔1700m以上地区少有分布,目前只有野外偶见红大戟的零星分布,已处于濒临枯竭的状态,药用主要来源于人工种植。在中国药典中,记载的红大戟药理作用为泄水逐饮、消肿散结,已成为八宝玉枢丸、紫金散等治疗呕恶泄泻上市药的原料药。但关于红大戟的降血糖活性,国内外并没有相关资料文献等进行过详细的记载和报道。
发明内容
本发明的第一目的在于提供一种具有降血糖活性的红大戟提取物,进一步的目的在于提供该红大戟提取物的应用。
本发明的第一目的是这样实现的,一种具有降血糖活性的红大戟提取物,其制备方法按以下步骤实现:
将红大戟的干燥根茎粉碎得到红大戟粉,采用75%的乙醇浸取2-3次,每次提取5-7d,得到提取液;
(2)在提取液中加3-4倍量的蒸馏水,静置2-3天后抽滤,将滤液在50-60℃下减压浓缩得到浸膏;
(3)浸膏加水溶解后,先用石油醚萃取后,剩余部分用乙酸乙酯萃取,将萃取液浓缩后冷冻干燥得到红大戟提取物。
本发明进一步的目的是这样实现的,所述红大戟提取物的应用为在制备辅助降血糖的保健品中的应用。
本发明的有益效果为:本发明制备的红大戟提取物能显著降低STZ导致的糖尿病大鼠的血糖,提高糖尿病大鼠的葡萄糖耐量,改善糖尿病大鼠“三多一少”的症状,为糖尿病的预防和治疗提供了一种新的天然资源。
本发明方法制备的红大戟提取物,适于大批量生产。相比于传统的回流提取,浸渍提取能够避免高温对成分的破坏,浸渍时间长,成分浸出率较高。且先用石油醚对提取物进行脂肪类化合物的除杂,将有效成分聚集,易于后续分离。
本发明红大戟提取物效果稳定,成分相对温和,副作用小,具有开发成新型降血糖产品的潜力。
附图说明
图1为本发明红大戟提取物对大鼠血糖的影响图;
图2为本发明红大戟提取物对大鼠体重的影响图;
图3为本发明红大戟提取物对大鼠葡萄糖耐量的影响图;
图4为本发明红大戟提取物对糖尿病大鼠胰岛素分泌的影响图;
图5为本发明红大戟提取物对糖尿病大鼠糖化血红蛋白的影响图;
图6为本发明红大戟提取物对糖尿病大鼠胰岛的氧化应激影响图;
图7为红大戟乙酸乙酯萃取物对糖尿病大鼠血糖相关指标的影响图。A为血清胰岛素水平;B为干预期间大鼠空腹血糖变化图;C为灌胃33天后大鼠糖耐量情况;
图8为灌胃不同浓度的本发明红大戟提取物后小鼠的体重变化图。
具体实施方式
下面结合实施例对本发明作进一步的说明,但不以任何方式对本发明加以限制,基于本发明教导所作的任何变换或替换,均属于本发明的保护范围。
本发明提供了一种具有降血糖活性的红大戟提取物,其制备方法按以下步骤实现:
(1)将红大戟的干燥根茎粉碎得到红大戟粉,采用75%的乙醇浸取2-3次,每次提取5-7d,得到提取液;
(2)在提取液中加3-4倍量的蒸馏水,静置2-3天后抽滤,将滤液在50-60℃下减压浓缩得到浸膏;
(3)浸膏加水溶解后,先用石油醚萃取后,剩余部分用乙酸乙酯萃取,将萃取液浓缩后冷冻干燥得到红大戟提取物。
步骤(1)中,加入乙醇的重量为红大戟粉重量的8-10倍。
步骤(2)中,冷冻干燥的温度为-40℃。
本发明还提供了所述具有降血糖活性的红大戟提取物在在制备辅助降血糖的保健品中的应用。
所述红大戟提取物的应用还可以为在制备预防或治疗糖尿病药物中的应用。
实施例1
将人工种植红大戟干燥根茎粉碎成50kg粉末,用500L的75%乙醇密封条件下浸泡7天后,再将药渣用400L 75%乙醇浸泡提取5天,将两次滤液合并在55℃下减压浓缩至一定体积,后加3倍量蒸馏水静置48h,减压抽滤去除沉淀,得到提取液,将提取液在55℃条件下减压浓缩得到10.61kg浸膏。将浸膏加蒸馏水溶解,溶解后先用等体积石油醚进行萃取,后用等体积乙酸乙酯萃取得到乙酸乙酯萃取液,将萃取液减压浓缩、冷冻干燥得到红大戟提取物127.32g。
实施例2
将人工种植红大戟干燥根茎粉碎成6kg粉末,用60L的75%乙醇密封条件下浸泡3天后,再将药渣用48L的 75%乙醇浸泡提取3天,将两次滤液合并在50℃下减压浓缩至一定体积,后加3倍量蒸馏水静置48h,减压抽滤去除沉淀,得到提取液,将提取液在50℃条件下减压浓缩得到2.6kg浸膏。将浸膏加蒸馏水溶解,溶解后先用等体积石油醚进行萃取,后用等体积乙酸乙酯萃取得到乙酸乙酯萃取液,将萃取液减压浓缩、冷冻干燥得到红大戟提取物9g。
实施例3
将红大戟干燥根茎粉碎成47.5kg粉末,用475L的75%乙醇密封条件下浸泡7天后,再将药渣用380L 75%乙醇浸泡提取5天,将两次滤液合并在60℃下减压浓缩至一定体积,后加4倍量蒸馏水静置60h,减压抽滤去除沉淀,得到提取液,将提取液在60℃条件下减压浓缩得到10.61kg浸膏。将浸膏加蒸馏水溶解,溶解后先用等体积石油醚进行萃取,后用等体积乙酸乙酯萃取得到乙酸乙酯萃取液,将乙酸乙酯萃取液减压浓缩、冷冻干燥得到红大戟提取物127.3g。
实验例1 红大戟提取物降糖活性检测
检测实施例3制备的红大戟提取物对糖尿病大鼠血糖、体重、糖耐量的影响
1、实验动物:SD大鼠,湖南斯莱克景达实验动物有限公司,许可证号:SYXK(滇)K2022-0004。
2、实验试剂:链脲佐菌素STZ(sigma,)柠檬酸钠缓冲液(0.1M,PH=4.5,批号:20220810,solarbio),血糖仪(三诺血糖仪),大鼠胰岛素ELISA试剂盒、大鼠糖化血红蛋白ELISA试剂盒(上海酶联生物科技公司)、SOD、MDA、TP均购自南京建成
3、实验方法:
造模和分组:大鼠(200-220g)普通饲料适应性喂养7天后,空腹12h腹腔注射40mg/kg STZ,5天后测量大鼠随机血糖,采用尾尖取血便携式血糖仪进行血糖监测,血糖值大于11.1mmol/l的视为造模成功,反则按照30mg/kg剂量对未成模的大鼠进行STZ补射,补射STZ的大鼠三天后测量血糖,将两次注射成模的大鼠按照血糖值随机分为红大戟提取物高剂量组、红大戟提取物低剂量组、模型组和正常组。每组老鼠数量不低于10只。
给药:每天下午固定时间给药,给药组给药剂量为2.4mg/kg(高剂量)、0.8mg/kg(低剂量),模型组和正常组灌胃同体积蒸馏水,干预时长为5周。每周记录大鼠血糖和体重,给药最后一天记录大鼠葡萄糖耐量,待给药结束后将所有大鼠进行解剖,保留腹腔动脉血液,将肝脏、胰腺和肾脏等器官放入液氮中速冻并放进-80℃冰箱保存,后进行相关指标测定。
4、实验结果
实验数据采用单因素方差分析(ANOVA)检验确定差异是否显著,*P<0.05表明有显著差异,**P<0.01表明有极显著差异。
(1)如图1所示,在干预期间,给药组血糖从第三周开始呈现下降的趋势,第5周时,红大戟提取物高剂量组空腹血糖值与模型组血糖相比具有显著性差异(P<0.05),而模型组在给予蒸馏水的情况下,始终保持高血糖的水平,由此可知,红大戟能一定程度上降低糖尿病大鼠的血糖。
(2)糖尿病最明显的症状便是“三多一少”,糖尿病大鼠的体重会随着时间的增长逐渐减小,由图2可以得知,模型组的大鼠其体重在干预期间幅度变化较小,其余给药组大鼠体重都在逐渐增大,但比正常组相比增大幅度小,可以看出给药组大鼠在抵抗由于糖尿病所造成的体重减少,说明本发明红大戟提取物在一定程度上能够改善糖尿病大鼠体重减少的情况。
(3)葡萄糖耐量能够反映大鼠葡萄糖耐受情况和短时间内调节血糖的能力,由图3可以看出,在大鼠灌胃给予葡萄糖后,模型组由于胰岛的破坏,调节血糖的能力下降,在给予葡萄糖后半小时血糖达到最大值,后随着时间的增长逐渐下降,红大戟提取物给药组血糖值遵循同样的规律进行变化,但红大戟提取物高剂量组血糖最大值始终小于模型组,正常组由于胰岛未受到破坏,能够正常调节血糖,所以血糖波动较小,始终接近于正常水平。由此可以看出红大戟提取物能够在一定程度上改善糖尿病大鼠调节血糖的能力。
实验例2
1、氧化损伤、血浆胰岛素指数和糖化血红蛋白指标的测定
由于胰岛是分泌胰岛素和调节血糖的重要器官,本实验对实验例1中的实验大鼠进行解剖,取胰岛和血浆进行氧化损伤、血浆胰岛素指数和糖化血红蛋白指标的测定。
结果:图4是空腹状态下大鼠血清胰岛素情况,由于STZ的影响,糖尿病大鼠胰岛受到破坏,分泌胰岛素能力下降,由图4可以明显看出,给药组血清胰岛素水平显著高于模型组(P<0.05),且接近正常组正常胰岛素水平。糖化血红蛋白水平反应了干预期间大鼠平均血糖水平,红大戟提取物高、低剂量组都能降低糖尿病大鼠糖化血红蛋白含量,高剂量组减少蛋白糖化效果更为明显。
SOD(超氧化物歧化酶)含量越高代表清除自由基抗氧化能力越强,MDA(丙二醛)为自由基氧化终产物,具有细胞毒性,含量越高细胞损伤越严重,由图6可以看出红大戟提取物高剂量组相对于模型组能够减少MDA的释放,增强SOD活力,一定程度上保护胰腺的氧化损伤,且高剂量保护效果要高于低剂量组。
实验例3
以实施例3制备的红大戟提取物灌胃SD雄性大鼠(北京维通利华实验动物技术有限公司许可证号:SYXK(滇)K2022-0004),每组12只,高中低剂量组剂量分别为1.61mg/kg、3.22 mg/kg和4.83mg/kg,灌胃给药33天后对大鼠进行糖耐量测定,34天时检测最后一次空腹血糖,35天时将大鼠解剖,取血清冷冻保存后续测定,胰岛素含量等其他指标
结果:如图7所示,实施例3制备的红大戟提取物能够增加血液中胰岛素含量,三个剂量组大鼠对糖的耐受程度均高于模型组,给药最后一天给药组血糖值和模型组相比具有显著性差异(p<0.05)。
综上可知,本发明红大戟提取物能够降低糖尿病大鼠的血糖,改善胰岛的氧化损伤,根据现有数据推测其可能通过保护胰岛,促进胰岛素的释放等方式改善糖尿病大鼠的高血糖症状,具有开发降糖药物或保健品的潜力。
实验例4急性毒性实验
取40只健康小鼠,雌雄各半,体重18-22g,试验前禁食不禁水16小时,随机分为10组,每组4只,标记。
取干燥红大戟粉末进行75%乙醇回流提取3次,物料表比为1:10 1:8 1:6,将得到的提取液减压浓缩冷冻干燥得到醇提物粉末(条件同实例1相同)。将得到的醇提取物加蒸馏水溶液,配制为16号小鼠灌胃针刚好能通过的浓溶液,最大浓溶液浓度为2.23g/ml(1016g生药/kg),然后以0.85的剂量比距,以蒸馏水稀释,配制其余以下九个浓度:1.9、1.61、1.37、1.16、0.99、0.84、0.71、0.61g/ml。
分别将上述10个浓度的红大戟提取物给10组小鼠一日之内灌胃小鼠给药1次,,灌胃体积为0.4ml/10g,给药后立即观察动物的毒性反应,包括外观体征、行为活动、精神状态、食欲、大小便及颜色、被毛、肤色、呼吸,以及鼻、眼、口腔、生殖器等有无异常分泌物。后将小鼠连续观察4天,记录其体重变化和生命状态。
结果:灌胃最大剂量当天无因药物致死的小鼠,最高浓度小鼠,出现精神萎靡,身体蜷缩,呼吸喘息的状态,但经2h后,小鼠状态逐渐恢复正常。如图8所示,小鼠在灌胃后的4天内,正常生长,各组之间老鼠体重变化无显著性差异。以上结果说明在最大给药浓度下,本发明红大戟醇提物对小鼠达不到致死量。
Claims (5)
1.一种具有降血糖活性的红大戟提取物,其特征在于,其制备方法按以下步骤实现:
(1)将红大戟的干燥根茎粉碎得到红大戟粉,采用75%的乙醇浸取2-3次,每次提取5-7d,得到提取液;
(2)在提取液中加3-4倍量的蒸馏水,静置2-3天后抽滤,将滤液在50-60℃下减压浓缩得到浸膏;
(3)浸膏加水溶解后,先用石油醚萃取后,剩余部分用乙酸乙酯萃取,将萃取液浓缩后冷冻干燥得到红大戟提取物。
2.根据权利要求1所述具有降血糖活性的红大戟提取物,其特征在于,步骤(1)中,加入乙醇的重量为红大戟粉重量的8-10倍。
3.根据权利要求1所述具有降血糖活性的红大戟提取物,其特征在于,步骤(2)中,冷冻干燥的温度为-40℃。
4.权利要求1-3任意一项所述具有降血糖活性的红大戟提取物在制备辅助降血糖的保健品中的应用,其特征在于,所述保健品是通过在红大戟提取物中加入保健品中可接受的辅料制成。
5.权利要求1-3任意一项所述具有降血糖活性的红大戟提取物在制备预防或治疗糖尿病药物中的应用。
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