CN104306427A - 一种红景天提取物及其应用 - Google Patents
一种红景天提取物及其应用 Download PDFInfo
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- CN104306427A CN104306427A CN201410621313.9A CN201410621313A CN104306427A CN 104306427 A CN104306427 A CN 104306427A CN 201410621313 A CN201410621313 A CN 201410621313A CN 104306427 A CN104306427 A CN 104306427A
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- Prior art keywords
- radix rhodiolae
- extract
- rhodiolae extract
- rhodiola rosea
- medicine
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Abstract
本发明涉及一种红景天提取物,其中红景天多酚质量百分比含量为5%-70%,它是通过将红景天药材干燥、粉碎;与水或有机溶剂按质量体积比为1:3~50混合,利用煎煮或冷浸或超声提取中的一种或几种处理;滤去药渣,在旋转蒸发仪上以65℃蒸干,得到红景天提取物。本发明的具有α-糖苷酶抑制剂的活性,能够降低糖尿病人的餐后血糖,可以应用于制备具有降血糖功能的药品、食品、及保健品及治疗和预防糖尿病的药品、及保健品中。其优点主要表现在,能快速、有效的降低餐后血糖,与常用的α-葡萄糖苷酶抑制剂相比,毒副作用更小,有效地解决了药物联用易引发低血糖等问题。
Description
技术领域
本发明涉及天然植物提取,具体的设计一种传统草药红景天来源的α-葡萄糖苷酶抑制剂的提取及其应用。
背景技术
糖尿病是由内分泌紊乱引发的代谢类疾病,对人类健康危害极大,其代谢紊乱可导致肾脏、神经、眼睛、心脑血管等多种组织的慢性并发症,严重者可发生酮症酸中毒、昏迷等,且容易造成交叉感染。2011年6月在权威医学杂志《柳叶刀》上发表的一份研究结果显示,当前全世界约有3.47亿糖尿病患者。我国的情况也不容乐观,当前我国糖尿病患者人数已经达到了9240万,成为糖尿病第一大国,其中20岁以上的成人患病率达9.7%,而未诊断率也高达67%。由糖尿病导致的直接医疗开支占全国医疗总开支的13%,达到了1734亿人民币。更令人担忧的是,我国还有近1.48亿的糖尿病高危人群。因此,开发一种具有预防和治疗糖尿病作用的药物,是刻不容缓的事情。
当前市场上的口服类降血糖药物,主要有磺酰脲类、非磺酰脲类胰岛素促分泌剂、双胍类、噻唑烷二酮类、醛糖还原酶抑制剂、糖原异生抑制剂、α-糖苷酶抑制剂等。但是这些药物都普遍存在依赖性强、副作用较大等问题。其中口服降血糖药物阿卡波糖作为一种α-糖苷酶抑制剂,其原理主要是竞争抑制小肠上皮刷状缘葡萄糖淀粉酶、蔗糖酶及胰腺α-淀粉酶,阻止α-1,4糖苷键的水解,延缓淀粉和蔗糖的消耗吸收;造成肠道葡萄糖的吸收缓慢,降低餐后血糖的升高。阿卡波糖具有显著的降餐后血糖作用,还可以显著降低甘油三酯、胆固醇水平,而且可以控制糖化血红蛋白的水平,是首先被批准用于糖耐量受损(IGT)干预的药物,长期使用可极大降低由糖耐量受损转化为糖尿病的风险。由于具有以上优点,阿卡波糖一直在口服降血糖药物中占有较大的市场份额。然而,α-糖苷酶抑制剂其缺点是存在一定的毒副作用,可能会引起过敏性反应、消化、吸收障碍的慢性肠功能紊乱、由于肠胀气而可能恶化的情况、疝气,肠梗阻和肠溃疡等,同时值得注意的是阿卡波糖片在使用大剂量时会发生无症状的肝酶升高,对于肝功正常的停药后肝酶值会恢复正常,但肝功能不全的患者,就会加重病情造成损伤;因此有必要开发一类新的更安全的口服类的降糖药物。
从天然产物、中药中筛选更多、更便宜的a-葡萄糖苷酶抑制剂,近年来有不少报道,有多糖、黄酮、鞣质、皂甙、生物碱或提取物等各种类型。景天科(Crassulaceae)红景天属(Rhodiola)植物,全世界约有90种,主要分布于北半球高寒地带。多分布于喜马拉雅地区、亚洲西部至北部,经朝鲜、日本至北美洲,中国为红景天属植物的分布中心,约70余种。红景天属植物为多年生具根状茎草本,根状茎上有鳞片;花单性异株或杂性,排成伞房花序,通常4数,雄花有退化的雌蕊,雌花无退化的雄蕊,花瓣很小或完全消失。药理作用研究表明,红景天具有抗肿瘤、抗氧化、抗疲劳、抗辐射等功能,为航空、航天、军事医学、运动医学和卫生保健的重要药材。
发明内容
本发明的目的是为了提供一种红景天提取物及其制备方法,该红景天提取物可以作为α-糖苷酶抑制剂,在降血糖、治疗和预防糖尿病方面起到作用。
本发明的红景天提取物,其中红景天多酚质量百分比含量为5%-70%,具有α-糖苷酶抑制剂的活性。
所述的红景天提取物按照以下步骤制得:
a)将红景天药材干燥、粉碎;
b)将粉碎的红景天药材利用水或有机溶剂按药材(w):溶剂(v)=1:3~1:50混合,浸取;
c)滤去药渣,滤液干燥后,得到红景天提取物;或滤液通过过柱层析的方法,样品过柱后收集活性洗脱部位,浓缩干燥得到精制的红景天提取物。
进一步地,所述步骤b)所述的浸取为煎煮或冷浸或超声提取中的一种或几种组合。
进一步地,所述步骤c)的滤液在旋转蒸发仪上以65℃蒸干,得到红景天提取物。
进一步地,所述步骤b)中,使用的提取溶剂为水,处理方法为煎煮30~120min。
进一步地,所述步骤b)中,使用的提取溶剂为醇类。
进一步地,所述所述的醇类为甲醇、或乙醇。
进一步地,所述步骤c)中,使用的层析介质为大孔树脂、反相填料、聚酰胺树脂。
进一步地,所述步骤c)中,使用的层析洗脱溶剂为甲醇或乙醇的水溶液。
本发明的内容还包括所述的红景天提取物作为α-糖苷酶抑制剂的应用。
本发明的内容还包括所述的红景天提取物在制备具有降血糖功能的药品、食品、或保健品中的应用。
本发明的内容还包括所述的红景天提取物在制备治疗或预防糖尿病的药品、或保健品中的应用。
本发明的红景天提取物在制备药物中的应用中的任一技术方案,还包括药学上可接受的载体和/或赋形剂。其在药学上可接受的载体和/或赋形剂是一种或多种常用的填充剂、粘合剂、润湿剂、崩解剂、吸收促进剂、表面活性剂、吸附载体、润滑剂或矫味剂的载体。填充剂可选自淀粉、蔗糖、乳糖或微晶纤维素;粘合剂选自纤维素衍生物、藻酸盐、明胶或聚乙烯吡咯烷酮;崩解剂选自羧甲基淀粉钠、羟丙纤维素、交联羧甲基纤维素、琼脂、碳酸钙或碳酸氢钠;表面活性剂可以是十六烷醇或十二烷基硫酸钠;润滑剂选自滑石粉、硬脂酸钙、镁、微粉硅胶或聚乙二醇等。
本发明的红景天提取物在制备药物中的应用的制药剂型,包括片剂、胶囊剂、滴丸剂或颗粒剂。
本发明的红景天提取物在制备药物中的应用各种制药剂型可以按照药学领域的常规生产方法制备所需要的制剂。例如,片剂可为普通片、薄膜片、肠溶片等,可以用上述组合物干粉,加入适量稀释剂选自淀粉、糊精、甘露醇、微晶纤维素,适量的粘合剂选自水、乙醇、纤维素、淀粉、明胶,适量的崩解剂选自羧甲基淀粉钠、低取代羟丙基纤维素、海藻酸钠,以及适当的润滑剂选自硬脂酸镁、滑石粉、聚乙二醇,加入甜味剂,选自D-木糖、木糖醇、麦芽糖醇、甜叶菊素、天冬甜母,按常规湿法制粒,干燥后整粒或者干法制粒后压片,如为包薄膜衣片,用成膜材料选自纤维素类、聚乙二醇类,按常规包衣,分装入密闭瓶或者铝塑板中。胶囊剂可为普通胶囊剂、肠溶胶囊剂等,可将药物组合物干粉加入适当辅料选自碳酸钙、甘露醇、氧化镁、微粉硅胶等,适当润滑剂选自滑石粉、硬脂酸镁、乙二醇酯、聚硅酮类,以及适当的粘合剂选自矿物油、食油,并加入适当甜味剂,选自D-木糖、木糖醇、麦芽糖醇、甜叶菊素、天冬甜母,混合成干粉或者制成颗粒,填充入胶囊,分装在密闭瓶或者铝塑板中。
本发明的上述α-糖苷酶抑制剂在制备药物中的应用可通过口服的方式施用于需要这种治疗的患者。
本发明的上述应用中,所述的糖尿病为Ⅰ型糖尿病或Ⅱ型糖尿病。
本发明所使用的红景天是景天科红景天属植物红景天(Rhodiola rosea L.)的根。红景天性味寒、甘、涩,入肺经。有清肺利咽止咳、疏肝和胃之功效,有补气清肺、益智养心、收涩止血、散瘀消肿的功效。主治气虚体弱、病后畏寒、气短乏力、肺热咳嗽、咯血、白带腹泻、跌打损伤等。我们在研究低毒、高效的降糖药物的过程中发现,单独使用红景天提取物能降低小鼠的餐后血糖。
本发明提出的红景天提取物具有良好的降糖效果,其优点主要表现在,全天然的植物提取物能更安全有效的降低餐后血糖,有效避免α-葡萄糖苷酶抑制剂的毒副作用,而且还有效地解决了药物联用易引发低血糖等问题。
为了更好地理解和实施,下面结合附图详细说明本发明。
附图说明
图1是红景天提取物正常小鼠的餐后血糖的抑制作用的实验结果图
具体实施方式
一、红景天提取物的制备
【实施例1】
精密称量已粉碎的红景天药材5克,用70%乙醇以(按药材(w):溶剂(v)=1:8)超声提取30分钟,过滤,同样操作合并两次滤液。在旋转蒸发仪上以65℃蒸干,得到1号红景天提取物1.2807克。
【实施例2】
精密称量已粉碎的红景天药材5克,用95%乙醇以(按药材(w):溶剂(v)=1:8)超声提取30min,过滤,同样操作合并两次滤液。在旋转蒸发仪上以65℃蒸干,得到2号红景天提取物0.8411克。
【实施例3】
精密称量已粉碎的红景天药材5克,用95%乙醇以(按药材(w):溶剂(v)=1:8)超声30min,过滤。滤渣用水以(1:8水)煮沸30min,用纱布过滤挤干,同样操作合并两次滤液。在旋转蒸发仪上以65℃蒸干,得到3号红景天提取物1.2858克。
【实施例4】
精密称量已粉碎的红景天药材5克,用水以(按药材(w):溶剂(v)=1:8)煮沸30min,用纱布过滤挤干,同样操作合并两次滤液。用纱布过滤挤干,同样操作合并两次滤液。在旋转蒸发仪上以65℃蒸干,得到4号红景天提取物0.6595克。
【实施例5】
精密称量已粉碎的红景天药材200g用水以(按药材(w):溶剂(v)=1:8)煮沸30min,用纱布过滤挤干,同样操作,合并两次滤液。滤液离心(5000r/min,10min),收集上清液。将滤液上样到大孔树脂层析柱进行分离,先用水洗脱(5个柱体积),收集溶液,在旋转蒸发仪上以65℃蒸干,得到5号红景天提取物25.1433g。再用乙醇洗脱(5个柱体积),收集溶液,在旋转蒸发仪上以65℃蒸干,得到6号红景天提取物18.7247g。
二、口服制剂的制备
【实施例6】红景天提取物口服剂-1的制备:
准确称取实施例1制得的红景天提取物粉末31.25mg(提取率25.6%),加入20ml 0.5%的CMC-Na水溶液,漩涡振荡器混匀,制成均匀的悬浊液。红景天提取物终浓度为0.4mg/ml。
【实施例7】红景天提取物提取物口服剂-2的制备:
准确称取实施例1制得的红景天提取物粉末625mg(提取率25.6%),加入20ml 0.5%的CMC-Na水溶液,漩涡振荡器混匀,制成均匀悬浊液。红景天提取物终浓度为8mg/ml。
【实施例8】红景天提取物口服剂-3的制备:
准确称取按实施例1制得的红景天提取物粉末80mg,加入20ml 0.5%的CMC-Na水溶液,漩涡振荡器混匀,制成均匀悬浊液。红景天提取物终浓度为4mg/ml。
【实施例9】红景天提取物多酚含量的测定
9.1实验器材
9.2样品制备
●1号红景天提取物:按实施例1中所述方法提取红景天药材,得到1号红景天提取物
●2号红景天提取物:按实施例2中所述方法提取红景天药材,得到2号红景天提取物
●3号红景天提取物:按实施例3中所述方法提取红景天药材,得到3号红景天提取物
●4号红景天提取物:按实施例4中所述方法提取红景天药材,得到4号红景天提取物
●5号红景天提取物:按实施例5中所述方法提取红景天药材,得到5号红景天提取物
●6号红景天提取物:按实施例5中所述方法提取红景天药材,得到6号红景天提取物
9.3实验方法
称取没食子酸对照品1ml用水定容至10ml棕色容量瓶。量取0ml、0.1ml、0.2ml、0.4ml、0.6ml、0.8ml,分别置于10ml棕色容量瓶,各加入磷钼钨酸0.4ml,再分别加水5.2ml、4.9ml、4.8ml、4.6ml、4.4ml。各加入29%碳酸钠溶液4.4ml,摇匀,放置30min,以相应的试剂为空白在760nm处用紫外-可见分光光度计测定吸光度,以吸光度为纵坐标,浓度为横坐标,绘制标准曲线。量取样品0.2ml于10ml棕色容量瓶中按“各加入磷钼钨酸0.4ml”起制备并测定吸光度,从标准曲线中算出样品中没食子酸的量(mg)。
9.4结果
各种红景天提取物多酚含量测定数据表
【实施例10】红景天提取物抑制α-葡萄糖苷酶活性测定
10.1测定原理
底物p-NPG在α-葡萄糖苷酶催化作用下分解生成葡萄糖和对硝基苯酚,对硝基苯酚在微碱性条件下主动要以对硝基苯氧阴离子存在,颜色随着ph值的增加,由浅至深的黄色或棕黄色,对硝基苯酚转变为相应的阴离子后,分子内形成新的p-π共轭体系,分子能量降低,使特征吸收峰红移,在400nm-420nm范围内有较强的特征吸收,利用比色法可以测定样品中的对硝基苯酚含量,由此来测定α-葡萄糖苷酶的活力,α-GI对α-葡萄糖苷酶有抑制作用,从而抑制了α-葡萄糖苷分解p-NPG,使对硝基苯酚的量减少,利用比色法测定无抑制和抑制后样品颜色的变化,从而达到评价α-GI抑制α-葡萄糖苷酶活性的目的。
10.2试剂、供试品溶液配制
1)实验的试剂:
2)试剂配制
0.1mol/LNaH2PO4溶液:称取3.1218g NaH2PO4于小烧杯中,用蒸馏水溶解,转移至250ml容量瓶中,定容至250mL。
0.1mol/LNa2HPO4溶液,称取7.1595g Na2HPO4于小烧杯中,用蒸馏水溶解,转移至250ml容量瓶中,定容至250mL。
磷酸缓冲溶液的配制:0.1mol/LNaH2PO4溶液与0.1mol/LNa2HPO4溶液混合,调PH=6.81。(体积比大概=1:1)
P-NPG溶液:取P-NPG0.087g于小烧杯中,用磷酸缓冲溶液溶解,定容至10ml,成0.029mol/L溶液,临用前稀释至0.01mol/L。
0.1mol/L碳酸钠溶液:取无水碳酸钠1.0619g于小烧杯中用蒸馏水溶解,转移至100ml容量瓶中,定容至100ml。
葡萄糖苷酶:取0.0339g葡萄糖苷酶粉末,加磷酸缓冲液溶解,定容至5ml容量瓶中,分装于冻存管中,于-80℃摄氏度冷冻保存,临用前解冻。
3)样品配制
●阿卡波糖溶液:取0.0259g阿卡波糖粉末,于小烧杯中,加蒸馏水溶解,转移至25ml容量瓶中,定容至25ml。
●1号红景天提取物:按实施例1中所述方法提取红景天药材,得到1号红景天提取物
●2号红景天提取物:按实施例2中所述方法提取红景天药材,得到2号红景天提取物
●3号红景天提取物:按实施例3中所述方法提取红景天药材,得到3号红景天提取物
●4号红景天提取物:按实施例4中所述方法提取红景天药材,得到4号红景天提取物
●5号红景天提取物:按实施例5中所述方法提取红景天药材,取水部,得到5号红景天提取物
●6号红景天提取物:按实施例5中所述方法提取红景天药材,取乙醇部,得到6号红景天提取物
10.3、实验方法
按表中体积准确吸取样液加入96孔平板中,不同浓度的待测样液50ul,加入50ulα-葡萄糖苷酶溶液(C=100U/ml),随后37℃水浴30min后,再加入50ulp-NPG溶液(C=10mmol),再37℃水浴30min,加入100ul 1mol/l碳酸钠溶液,立即405nm测定吸光值。
α-葡萄糖苷酶抑制率(%)={1-(S1-S2)/(C1-C2)}*100
S1,S2,C1,C2分别为样品,样品空白,对照,对照空白在405nm下的吸收值。
*对照空白和样品空白:用磷酸缓冲液代替α-葡萄糖苷酶溶液,其他试剂不变。
*每个样品测定平行三个样。
10.4、实验结果
10.4.1、阿卡波糖
样品浓度(mg/ml) | 0.09 | 0.1 | 0.11 | 0.12 | 0.13 |
抑制率(%) | 26.27 | 0.5449 | 0.5195 | 0.4834 | 0.4472 |
10.4.2、1号红景天提取物
样品浓度(mg/ml) | 0.5 | 1 | 1.5 | 2 | 2.5 |
抑制率(%) | 0.3924 | 0.3286 | 0.3335 | 0.3247 | 0.3244 |
10.4.3、2号红景天提取物
样品浓度(mg/ml) | 0.84 | 1.35 | 1.85 | 2.35 | 2.86 |
抑制率(%) | 38.07 | 41.97 | 48.57 | 79.34 | 84.2 |
10.4.4、3号红景天提取物
样品浓度(mg/ml) | 0.26 | 0.39 | 0.51 | 0.64 | 0.77 |
抑制率(%) | 42.87 | 52.28 | 65.8 | 66.17 | 70.61 |
10.4.5、4号红景天提取物
样品浓度(mg/ml) | 0.079 | 0.097 | 0.11 | 0.12 | 0.13 |
抑制率(%) | 26.56 | 28.1 | 34.74 | 41.17 | 53.98 |
10.4.6、5号红景天提取物
样品浓度(mg/ml) | 0.50 | 0.75 | 1.00 | 1.25 | 1.50 |
抑制率(%) | 0.307 | 0.302 | 0.303 | 0.303 | 0.299 |
10.4.7、6号红景天提取物
样品浓度(mg/ml) | 7.0 | 8.0 | 9.0 | 10.0 | 11.0 |
抑制率(%) | 0.659 | 0.686 | 0.702 | 0.772 | 0.770 |
10.5、实验结论
根据α-葡萄糖苷酶抑制率(%)={1-(S1-S2)/(C1-C2)}*100的计算,可得出四种样品的IC50值,可看出先用纯净水提取的红景天提取物抑制α-葡萄糖苷酶活性能力比较好。
【实施例11】红景天提取物正常小鼠的餐后血糖的抑制作用
11.1实验器材:
罗氏血糖仪 罗氏诊断产品(上海)有限公司
血糖试纸 德国罗氏诊断有限公司
阿卡波糖片(拜唐苹) 拜耳医药保健有限公司·中国北京
11.2、样品制备:
11.2.1样液制备
●1号红景天提取物:按实施例1中所述方法提取红景天药材,得到1号红景天提取物
●2号红景天提取物:按实施例2中所述方法提取红景天药材,得到2号红景天提取物
●3号红景天提取物:按实施例3中所述方法提取红景天药材,得到3号红景天提取物
●4号红景天提取物:按实施例4中所述方法提取红景天药材,得到4号红景天提取物
●5号红景天提取物:按实施例5中所述方法提取红景天药材,得到5号红景天提取物
●6号红景天提取物:按实施例5中所述方法提取红景天药材,得到6号红景天提取物
11.3实验方法
取48只18~22g的昆明小鼠(雄性,购于中山大学SPF实验动物中心)。随机分为A-H组,每组8只。实验前对各组小鼠禁食16h,自由给水,各组用淀粉(10g/kg)和药液混合溶液同时灌胃小鼠,以0.5ml/20g剂量对各组小鼠进行灌胃。各组给药情况如下:
A组:灌胃淀粉溶液,实际给药剂量淀粉为10g/kg;
B组:灌胃阿卡波糖片,实际给药剂量阿卡波糖为10mg/kg;
C组:灌胃1号红景天提取物,实际给药剂量1号红景天提取物1.28g/kg;
D组:灌胃2号红景天提取物,实际给药剂量2号红景天提取物0.84g/kg;
E组:灌胃3号红景天提取物,实际给药剂量3号红景天提取物1.285g/kg;
F组:灌胃4号红景天提取物,实际给药剂量4号红景天提取物0.66g/kg;
G组:灌胃5号红景天提取物,实际给药剂量5号红景天提取物0.66g/kg;
H组:灌胃6号红景天提取物,实际给药剂量6号红景天提取物0.66g/kg;
上述各组,分别在0min,60min,120min小鼠尾部取血,用血糖仪(罗氏,活力型)测定血糖值,其结果如下表所示:
注:*p<0.05;**p<0.01(与A组比较)
根据附图1,可以看出本发明的红景天提取物可以明显抑制正常小鼠餐后血糖的上升,且其抑制作用随给药浓度变化而变化。
Claims (12)
1.一种红景天提取物,其特征在于:其中红景天多酚质量百分比含量为5%-70%,具有α-糖苷酶抑制剂的活性。
2.根据权利要求1所述的红景天提取物,其特征在于:所述的提取物通过以下步骤制得:
a)将红景天药材干燥、粉碎;
b)将粉碎的红景天药材与水或有机溶剂按药材(w):溶剂(v)=1:3~1:50混合,浸取;
c)滤去药渣,滤液直接浓缩干燥得到红景天提取物;或滤液通过过柱层析的方法,样品过柱后收集活性洗脱部位,浓缩干燥得到精制的红景天提取物。
3.根据权利要求1所述的红景天提取物,其特征在于:步骤b)所述的浸取为煎煮或冷浸或超声提取或闪式提取中的一种或几种组合。
4.根据权利要求2所述的红景天提取物,其特征在于:步骤c)的滤液在旋转蒸发仪或其他减压浓缩设备上以65℃蒸干,得到红景天提取物。
5.根据权利要求2所述的红景天提取物,其特征在于:步骤b)中,使用的提取溶剂为水,处理方法为煎煮30~120min。
6.根据权利要求2所述的红景天提取物,其特征在于:步骤b)中,使用的提取溶剂为醇类。
7.根据权利要求6所述的红景天提取物,其特征在于:所述的醇类为甲醇、或乙醇。
8.根据权利要求2所述的红景天提取物,其特征在于:步骤c)中,使用的层析介质为大孔树脂、反相填料、聚酰胺树脂。
9.根据权利要求2所述的红景天提取物,其特征在于:步骤c)中,使用的层析洗脱溶剂为甲醇或乙醇的水溶液。
10.权利要求1至9任一所述的红景天提取物作为α-糖苷酶抑制剂的应用。
11.权利要求1至9任一所述的红景天提取物在制备具有降血糖功能的药品、食品、或保健品中的应用。
12.权利要求1至9任一所述的红景天提取物在制备治疗或预防糖尿病的药品、或保健品中的应用。
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