CN1233386C - 老鹰茶水提取物在制备防治糖尿病药物中的应用 - Google Patents
老鹰茶水提取物在制备防治糖尿病药物中的应用 Download PDFInfo
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- CN1233386C CN1233386C CN 03158231 CN03158231A CN1233386C CN 1233386 C CN1233386 C CN 1233386C CN 03158231 CN03158231 CN 03158231 CN 03158231 A CN03158231 A CN 03158231A CN 1233386 C CN1233386 C CN 1233386C
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Abstract
本发明涉及老鹰茶水提取物在制药领域中的新用途。该老鹰茶水提取物能显著降低血糖值,能显著对抗由肾上腺素引起的血糖升高,适用于各型糖尿病,作用于多个环节,疗效确切。用于治疗或预防糖尿病采用口服给药,服用方便,毒副作用小,长期服药无危害。
Description
技术领域
本发明涉及老鹰茶水提取物的用途,确切地说是在制药领域中的用途。
背景技术
老鹰茶是我国江南农村的一种传统饮料,千百年来深受饮用者的喜爱和欢迎,原因在于原料丰富,加工简单,便于保管,饮用方便,而且是一种无毒、无污染的纯天然饮料。近年来,由于环境受到一定程度的污染,人们回归自然的意识不断增加,这种纯天然饮料越来越受到人们的青睐。为了认识和了解这一野生自然资源,更好的开发与利用,现将老鹰茶的研究与开发现状综述如下。
老鹰茶的植物学分类:属于樟科、木姜子属、毛豹皮樟,俗称“白茶”,也叫老鹰茶。学名Litsea coreana Leve.var.是一种常绿小乔木或乔木。常生长在海拔1000米左右的低山常绿阔叶林中,分布在四川、贵州、安徽、云南、重庆、湖南和江西等地。
当年生枝紫褐色或绿色,有卷曲柔毛,皮孔黄褐色或绿色,第二年枝秃净。芽卵形,鳞片外绿色或黄褐色绢毛。
叶革质、互生、椭圆形、狭椭圆形或倒卵状椭圆形,先端渐尖或突尖,基部楔形,长5-15cm,宽1.5-5.cm,背面灰白色,有卷曲柔毛,有时秃净,侧脉6-10条,叶柄长0.5-1.5cm,有毛。在自然环境下,年萌发新芽2轮,4-5月为春芽,8-9月为秋芽,以春芽产量为高。
花,腊黄色、花序无梗,数个簇生在叶腋,总苞外有短毛,每序有花4-8朵,花朵直径4-5mm。
果,近球状(有长椭圆形和倒椭圆形),直径约6mm,果梗粗壮,长0.5-0.8mm,有毛,果托扁平膨大,有宿存的花被裂片。花期8-9月,果期次年5-8月。
种子,由一层较薄的果皮包裹,种子坚硬,有蜡质。种子直径约6mm。
老鹰茶的化学成分:
老鹰茶中含有丰富的氨基酸,总含量为0.82%,8种人体必需氨基酸齐全,含量以亮氨酸最高,赖氨酸次之,蛋氨酸最低,这和绿茶相似,其中蛋氨酸含量还略高于绿茶。在非必需氨基酸中,以谷氨酸含量最高,其次是天冬氨酸和精氨酸,与绿茶相比无明显差异。从氨基酸总量上看,绿茶的氨基酸高于老鹰茶,其主要原因是绿茶中特有茶氨酸的含量高,茶氨酸在一定程度上反映绿茶与老鹰茶的口感差异,另一方面也说明绿茶原植物与老鹰茶植物有不同的氨基酸代谢类型。
老鹰茶富含多种矿物质元素,其中钾(K)、磷(P)、钙(Ca)、镁(Mg)、钠(Na)、锌(Zn)、铁(Fe)、硒(Se)都是人体必需的营养元素,尤其是锌(Zn)、铁(Fe)、硒(Se)元素含量高于绿茶,对造血、健脑有较好作用。更值得一提的是有害元素铅的含量明显低于绿茶。
老鹰茶含有的水溶性维生素主要是VC、VB1和VB2,其含量比绿茶稍低,可能与加工过程与代谢途径等因素有关。
老鹰茶中总黄酮(TF,total flavonoid)含量远高于绿茶,绿茶只有1.22%左右,而老鹰茶可高达3.45%,已经确定的有山柰酚(kaempferol),山柰酚-3-O-β-D-葡萄糖苷(kaempferol-3-O-β-D-glucopyranoside),槲皮素-3-O-β-D-葡萄糖苷(quercetin-3-O-β-D-glucopyranoside)。
老鹰茶经过常压水蒸气蒸馏提取老鹰茶的挥发性成分,得到浅黄色油状液体,香味浓郁,出油率0.1%左右。经气相色谱-质谱联用分析,鉴定出32种成分(其中萜类化合物及其衍生物20种),占挥发油组成的95%,主要成分是正癸醛(decanal)含量为71.53%;其次是10-烯-十一醛(10-undecenal),含量为5.02%;壬醛(n-nonaldehyde),含量3.58%;正十二酸乙烯酯(dodecanoic acid,ethenyl ester),含量2.63%。香味的主要成分为萜类,其中主要是分子量为204的萜类。
老鹰茶中还含有多糖、皂甙、多酚和天然色素等。
另外,尤其值得一提的是,与绿茶相比,老鹰茶的化学成分不含咖啡碱物质,无兴奋作用,不影响睡眠,这对需要控制咖啡碱摄入的人更是一种良好的选择。
老鹰茶(Litsea coreana Leve.var.)在我国江南广大农村饮用由来已久,深受广大劳动人民的喜爱,但仅仅作为一种饮料。近年来,四川、贵州等地进行了一些开发和利用,但也仅限于粗加工,还没有充分认识到它的药理功能,它所潜在的药理作用机制更无前人探讨。根据文献报道,长期饮用有防馊、防腐、消暑解渴、消食化积、解毒、消肿利尿,明目、健胃、益思的作用。
本发明的目的在于提供老鹰茶水提取物的新用途,即在制药中的新应用。
实际上,本发明提供了老鹰茶水提取物在制备治疗或预防糖尿病的药物中的应用。
随着人类寿命的延长,生活水平的不断提高,糖尿病(diabetes)的发病率在逐年上升,而且具有很高的致残率和致死率,严重威胁着人类的健康。据保守估计,全世界糖尿病的患者近四亿,而我国就有将近五千万。世界卫生组织已将防治这一类疾病列为全球人类健康的重要问题之一。
近年来,治疗糖尿病的药物发展很快。治疗糖尿病的药物有:
A、胰岛素,主要用于I型糖尿病、II糖尿病经饮食和其它药物未得到控制者、糖尿病并发症及机体处于应急状态下。但由于其是多肽类,必须注射给药,给患者带来许多不便,还有潜在的危险:(1)高胰岛素血症;(2)体重增加;(3)低血糖。
B、双胍类,主要用于经饮食和运动疗法未能控制的肥胖II型糖尿病患者或者与其它药物联合应用。其最常见的不良反应是胃肠道反应,最严重的不良反应是乳酸酸中毒和肾毒性。
C、磺酰脲类,中年以上发病的NIDDM紧饮食运动治疗未能满意控制者或与其他药物联用。其不良反应主要有:皮肤过敏反应、胃肠道反应和低血糖等。
D、α-葡萄糖苷酶抑制剂,主要用于餐后血糖不能满意控制者,但容易出现腹胀、腹痛和便秘等。
E、胰岛素增敏剂,临床应用于II糖尿病患者。不良反应虽少,但价格比较昂贵。
老鹰茶水提取物900mg/kg能显著降低正常小鼠的血糖值,(与对照组比较,p<0.05)。老鹰茶水提取物均能显著对抗由肾上腺素引起的小鼠血糖升高(与模型组比较,p<0.05),其中以100mg/kg的降糖作用最为显著(与模型组比较,p<0.01)。老鹰茶水提取物300mg/kg、900mg/kg能显著降低四氧嘧啶糖尿病小鼠的血糖值(与模型组比较,p<0.05)。
为了更好地理解本发明的实质,下面将用老鹰茶水提取物的药理实验及结果来说明其在制药领域中的新用途。
老鹰茶水提物的降血糖作用试验如下:
(一)材料
动物
昆明种小鼠,雌雄各半,体重18-22g,由本校实验动物中心提供。实验中未注明时均指实验前禁食2h。
药品与试剂
老鹰茶水提物,自制;
格列本脲(优降糖,glibenclamide):天津太平洋制药有限公司,批号020907。
苯乙双胍(苯乙福明,降糖灵,phenfarmin):南通制药总厂,批号011017。
四氧嘧啶(Alloxan):Sigma公司产品,临用前用生理盐水配制成1%溶液。
盐酸肾上腺素注射液:上海禾丰制药有限公司,批号021202-7。
葡萄糖(Glu)测定试剂盒:上海荣升生物技术有限公司产品。
(二)方法
老鹰茶水提物的制备
称取老鹰茶100g,加入蒸馏水2000毫升,超声30分钟,过滤分离,保留上清液,滤渣再加入蒸馏水2000毫升,重复以上步骤,合并2次上清液,减压浓缩后80℃水浴过夜烘干,50℃真空干燥,称重。
老鹰茶水提物对正常小鼠血糖的影响
正常小鼠50只随机分5组,灌胃给药(老鹰茶水提物100mg/kg、300mg/kg、900mg/kg,优降糖50mg/kg)或等体积生理盐水(20ml/kg),每天1次,连续5d,于末次给药后3h取血测血糖含量。
老鹰茶水提物对肾上腺素性高血糖小鼠血糖的影响
正常小鼠60只随机分6组,灌胃给药(老鹰茶水提物100mg/kg、300mg/kg、900mg/kg,优降糖50mg/kg)或等体积生理盐水(正常对照、模型),每天1次,连续5d,于末次给药后1h,正常对照组ip生理盐水,其余5组均ip肾上腺素300ug/kg,于注射后30分钟取血测血糖含量。
老鹰茶水提物对四氧嘧啶糖尿病小鼠血糖的影响
正常小鼠60只,除10只正常对照组外,其余均尾静脉注射1%四氧嘧啶生理盐水100mg/kg造成糖尿病模型,72h后(禁食12h)取血预测血糖后分5组,灌胃给药(老鹰茶水提物100mg/kg、300mg/kg、900mg/kg,降糖灵100mg/kg)或等体积生理盐水,每天1次,连续5d,于末次给药前禁食16h,末次给药后1h取血测血糖含量。
(三)结果
老鹰茶水提物对正常小鼠血糖的影响
由表1可见,老鹰茶水提物均能降低正常小鼠的血糖值,其中以900mg/kg降糖作用最为显著(p<0.01)。
表1老鹰茶水提物对正常小鼠血糖的影响(
x±s,n=10)
组别 剂量(mg/kg) 血糖(mmol/l)
对照 - 7.20±0.60
老鹰茶水提物 100 6.92±1.60
300 6.48±1.53
900 5.78±1.32**
优降糖 50 6.08±0.87*
*与对照组比较,p<0.05**与对照组比较,p<0.01
老鹰茶水提物对肾上腺素性高血糖小鼠血糖的影响
老鹰茶水提物均能显著对抗由肾上腺素引起的小鼠血糖升高,其中以100mg/kg的降糖作用最为显著(p<0.01),结果见表2。
表2老鹰茶水提物对肾上腺素性高血糖小鼠血糖的影响(
x±s,n=10)
组别 剂量(mg/kg) 血糖(mmol/l)
对照 - 6.42±1.66
模型 - 10.43±2.51△
老鹰茶水提物 100 6.66±1.53**
300 7.77±1.42*
900 7.11±2.53*
优降糖 50 5.86±2.05**
△与对照组比较,p<0.01**与模型组比较,p<0.01
*与模型组比较,p<0.05
老鹰茶水提物对四氧嘧啶糖尿病小鼠血糖的影响
老鹰茶水提物均能降低四氧嘧啶糖尿病小鼠的血糖值,其中以300mg/kg、900mg/kg的降糖作用最为显著(p<0.05),结果见表3。
表3老鹰茶水提物对四氧嘧啶糖尿病小鼠血糖的影响(
x±s,n=10)
组别 剂量(mg/kg) 血糖(mmol/l)
对照 - 7.35±1.54
模型 - 26.71±3.96△
老鹰茶水提物 100 23.98±5.14
300 21.68±4.96*
900 21.52±1.82*
降糖灵 100 19.34±6.22*
△与对照组比较,p<0.01**与模型组比较,p<0.01
*与模型组比较,p<0.05
从上述试验结果可以得出本发明具有几方面的优点:
1、本发明对老鹰茶水提取物发掘了新的药用前景,开拓了一个新的应用领域。
2、本发明的老鹰茶水提取物采用口服给药,服用方便,毒副作用小,长期服药无危害。
3、本发明的老鹰茶水提取物适用于各型糖尿病,作用于多个环节,疗效确切。
4、本发明的老鹰茶水提取物的原料资源丰富,具有良好的社会和经济效益。
5、可以本发明为基础进行进一步的新药研究开发。
具体实施方式
下面结合实施例对本发明作进一步地描述。
实施例:
称取老鹰茶100g,加入蒸馏水2000毫升,超声30分钟,过滤分离,保留上清液,滤渣再加入蒸馏水2000毫升,重复以上步骤,合并2次上清液,减压浓缩后80℃水浴过夜烘干,50℃真空干燥,即得黄褐色颗粒状老鹰茶水提取物,具有芳香味,易潮解。
老鹰茶水取物推荐临床剂量:600-5400mg/日,口服,分三次服用。
Claims (1)
1、老鹰茶水提取物在制药中的应用,其特征在于:老鹰茶水提取物在制备防治糖尿病药物中的应用。
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CN104336775A (zh) * | 2013-07-26 | 2015-02-11 | 江西中烟工业有限责任公司 | 一种老鹰茶提取物及其制备方法以及该提取物在卷烟中的应用 |
CN103504374A (zh) * | 2013-09-23 | 2014-01-15 | 安徽凯利粮油食品有限公司 | 一种保健瓜蒌籽加工方法 |
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