CN101022818A - 生理活性的组合物 - Google Patents
生理活性的组合物 Download PDFInfo
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- CN101022818A CN101022818A CNA200580031615XA CN200580031615A CN101022818A CN 101022818 A CN101022818 A CN 101022818A CN A200580031615X A CNA200580031615X A CN A200580031615XA CN 200580031615 A CN200580031615 A CN 200580031615A CN 101022818 A CN101022818 A CN 101022818A
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Abstract
要求保护生理活性的组合物,其包含有效量的至少一种选自下述的化合物:4-O-甲基-davidigenin、4′-O-甲基-davidigenin、davidigenin、榄香素、异榄香脂素、7-甲氧基香豆素、去甲氧基茵陈色原酮特别是6-去甲氧基茵陈色原酮和/或6-去甲氧基-3′-甲氧基茵陈色原酮、hispiludin和9-羟基-10E,12Z,15Z-十八碳三烯酸以及它们的糖苷特别是4-O-甲基davidigenin和/或4′-O-甲基davidigenin的葡糖苷和/或鼠李葡糖苷、盐和衍生物。
Description
本发明涉及含有有效量的定义化合物的生理活性的组合物,还涉及其应用。
含有天然提取物或存在于其中的主要活性化合物的组合物正日益频繁地被消费者用于代谢疾病的自我药疗法。在该情况下,特别信任基于植物的提取物,其从例如自然疗法获知,或在外部培养循环中证实了其作用。
人群的典型疾病是心血管疾病以及代谢疾病,例如,特别是糖尿病及其前驱形式,以及由于营养不良或运动不足导致的病理学上改变的血液值,尤其应当提及升高的胆固醇或血脂值。
更具体地,在代谢疾病方面,在此期间市场上提供无需处方即可得到许多制剂,日益增加的兴趣是在糖尿病(更具体地,II型糖尿病)的预防和治疗。
从现有技术中已知许多文件,其包括使用天然提取物或植物成分来治疗糖尿病。
例如,国际专利申请WO 00/15174 A2描述了经定义的组合物的生物黄酮类化合物的应用,也是以植物提取物形式,用于降低哺乳动物的血糖水平。提及的典型的生物黄酮类化合物是橙皮苷、橙皮素、柑桔苷、柚皮素、地奥司明、芦丁和栎精。
欧洲专利申请EP 0 902 870 A1同样地公开了尤其是柚皮素和柑桔苷,其作为合适的降低血糖或血脂水平或预防糖尿病和高脂血症的黄烷酮。在该上下文中,还公开了黄烷酮可以源自植物提取物,例如柑橘属水果。
根据Herba Hungarica 1987,Tom.26,No.1的公开,黄酮类化合物例如存在于经选择的Bauhinia属的不同器官中,表现出对血糖水平的作用。在该上下文中,特别提及槲皮甙和山奈酚-3-半乳糖苷以及-鼠李葡糖苷;但是,也提及5,7-二甲氧基黄烷酮以及4-O-L-吡喃鼠李糖基-β-D-glycocyranoside。
最后,国际专利申请WO 03/020026 A1要求保护影响血糖水平、高血糖素样肽1(GLP1)的活性、胰岛素依赖性葡萄糖摄入的不同方法,还涉及治疗II型糖尿病的方法,其中通常需要摄入有效剂量的蒿属(Artemisia-Spezies)特别是龙蒿(Artemisia dracunculus)的适当极性的提取物。
对于糖尿病通常理解为复杂的代谢病症或疾病,其在大多数情况下的特征是升高的血糖水平,也伴有对碳水化合物、脂肪和蛋白代谢的严重影响。该疾病病征的原因是不能控制血糖水平,这是因为,例如,不充分的胰岛素水平(绝对的胰岛素缺乏)或不充分的胰岛素活性(相对的胰岛素缺乏)。升高的葡萄糖水平又导致继发的健康问题,它们使得额外的治疗步骤成为必需。伴随糖尿病的主要危险因素是动脉硬化、糖尿病性视网膜病、白内障、肾病、增加的感染机会、高血压、神经障碍以及痴呆。
总之,利用许多差异,可以区分两种重要的糖尿病类型。I型糖尿病通常影响儿童或少年,其原因是身体不能产生胰岛素(绝对的胰岛素缺乏)。远超过I型糖尿病而出现的II型糖尿病,是基于减少的胰岛素分泌,或更经常地基于胰岛素耐受性(相对的胰岛素缺乏)。常规采用的治疗方法指向,通过促进细胞的非选择性葡萄糖摄入,降低血糖水平。但是,该微弱控制的葡萄糖摄入也会影响脂细胞,其结果是又会导致体重问题。因此,在这些情况下,重要的是严格控制治疗方法和由此实现的变化。最普遍的常规治疗方法是施用胰岛素,其仍然非常昂贵,且对于患者而言,也仍然伴有不适和副作用,例如超剂量导致低血糖症的危险,变应性反应以及在注射位置形成局部的脂肪营养不良。
与常规治疗方法不同的是所谓的OTC-药疗法(非处方),例如上述天然产物,尤其是基于植物的那些。在传统的自然疗法中使用的众多植物科之一是,具有超过400个种的蒿科。Yazdanparast等在Biomedical Letters 59(1999),第137-141页报道了龙蒿,其醇基提取物能对大鼠发挥抗高血脂作用。但是,如在上述的PCT申请WO03/020026中已知描述的,还已经报道了其它蒿属,例如A.herba-alba或A.judaica与被扰乱的脂肪或糖平衡有关的有益效果。
天然提取物的普遍问题是标准化,这只能困难地进行,特别是因为栽培和收获条件、以及储存条件和加工的类型对原料以及从它们得到的提取物中的成分和它们各自的比例有显著影响。已知起源和尤其是有关的气候因素和土壤质量显著地影响植物成分的质量和数量。但是,储存温度、空气和湿度作用对已经收获的物质也起作用,例如以氧化性影响的形式。另外,还有加工类型和尤其是使用的溶剂的类型和质量,所以甚至在相同植物物种的情况下发现植物提取物组成的严重差异。
这发生在,尤其是,代表为龙蒿的上述蒿品种的情况下。所谓的“德国”或“法国”龙蒿的品种是最芳香的栽培类型,且含有高达3%精油,其香味主要是甲基胡椒酚(草蒿脑)和甲基丁香酚。另外,也存在对甲氧基肉桂酸、水芹烯、α-和β-蒎烯、莰烯、罗勒烯和柠檬烯。另一个品种是“俄罗斯”龙蒿,其含有明显较少的精油,完全不存在草蒿脑,其结果是,该品种不会形成法国龙蒿的那么令人愉悦的芬芳香味。替代的是包含黄酮类化合物:栎精和藤菊黄素,以草和涩味为特征。因此,习惯上没有将俄罗斯龙蒿描述为典型的烹调草药,而是归入龙蒿的原始野生型。但是,可以在相对寒冷的气候下,更容易地栽培俄罗斯龙蒿。从农业研究服务中心(“植物化学和人类植物学数据库”)(http://sun.arsgrin.gov:8080/npgspub/xsql/duke/plantdisp.xsql?taxon=123)中,可以获取蒿品种特别是龙蒿的潜在组分的综述。
在已经重复引用的国际专利申请WO 03/020026 A1中,列出了也可以存在于蒿提取物中的成分的典型代表。由此示范性列出了茵陈色原酮、四羟基甲氧基黄烷酮、伞形酮、野樱黄苷、三羟基甲氧基黄烷酮和三羟基黄烷酮。该文件也公开了新鲜的和冷冻的蒿提取物的各种色谱图,但是,其中在每种情况下给出的峰不允许作出关于可能存在的定义化合物的反向结论,尽管在实例中,将草蒿脑和甲基丁香酚作为龙蒿提取物的典型组分来提及。由于类似的陈述,即在完全生长的植物中,生物量比率从叶子转移到茎,因此,根据该文件研究的提取物主要在分离的茎和叶子上进行。在经加工的蒿叶子的基础上,制备了优选的提取物,仅仅进行了更详细地检查的提取物的相对评价。例如,提及例如,从冷冻的植物材料得到的龙蒿提取物表现出比新鲜的植物材料更高的活性。仅仅在与质谱的Wiley索引相对比的基础上,可以鉴别出主要峰,其显然地指向上述化合物为潜在成分。但是,在所述的弱极性的乙醇提取物中没有鉴别出其它组分,其尤其可能是对被扰乱的血糖水平的一同要求保护的有益作用的原因。
因此,本发明的一个目的是,提供生理活性的组合物,通过它们可以克服现有技术中存在的这些困难,其特别是由定义的化合物或化合物类别组成,且可以以有效剂量用于上述症候群和症状。该组合物应当含有尽可能容易获取的植物材料,且以于标准化的形式易于生产。另外,该组合物应当由现有技术已知化合物以外的组分组成,且在与它们的相互作用中也包括彼此作用,如果可能在各自选择的应用领域方面具有协同效应。
根据本发明,通过相应的组合物,已经实现了该目的,该组合物包含有效量的至少一种选自下述的化合物:4-O-甲基-davidigenin、4′-O-甲基-davidigenin、davidigenin、榄香素、异榄香脂素、7-甲氧基香豆素、去甲氧基茵陈色原酮特别是6-去甲氧基茵陈色原酮和/或6-去甲氧基-3′-甲氧基茵陈色原酮、高车前素(hispiludin)和9-羟基-10E,12Z,15Z-十八碳三烯酸以及它们的糖苷,更特别是,4-O-甲基davidigenin和/或4′-O-甲基davidigenin的葡糖苷和/或鼠李葡糖苷。另外,也可以包含它们各自的合适的盐和衍生物,以及使用HPLC分析可以检测到的蒿提取物中的所有化合物。
令人惊讶地,已经发现,在用作生产治疗代谢疾病的制剂的基础的植物提取物中,实际上可以检测出要求保护的化合物。与以前已知的公开不同,这些化合物优选地可以在蒿提取物中确认,且与预期的不同,各浓度以不能从以前已知的分析推导出的量存在。作为另一个优点,不仅通过包含纯物质的组合,还以简单的方式通过选择合适的植物提取物,特别容易获取要求保护的组合物,其中这些植物提取物本身的生产,不需要通过以前已知的植物材料的加工方法来进行。
在优选的实施方案中,要求保护的化合物的特征还在于,它另外包含至少一种选自下述的化合物:绿原酸、柚皮素、黄酮类化合物、黄烷酮类化合物、萜烯、萜类化合物和/或其衍生物,且其特别理解为糖苷和/或苷元。这些化合物作为单独的物质不是新的,但是根据本发明包含的组分的组合也展现出协同效应,优选地叠加效应。
根据本发明,优选的组合物包含纯形式和/或作为混合物的化合物,该混合物而且优选地作为天然提取物存在。基于它们的物理化学性能,鉴于它们的制备形式,根据本发明的组合物包含的化合物特别适合作为醇提取物,优选地醇/水提取物(与此相关的尤其是它们的醚级分)是合适的。
作为已知是极性液体的醇,更具体地甲醇、乙醇和异丙醇,特别适用于生产这样的提取物,在该情况下作为一个特别特征,其没有展现诱变活性或含有有害的毒素。
这样的提取物的生产不受任何限制,但是建议首先使植物原料接触诱导物组分,对此特别是多糖例如壳聚糖,但也可以是醋酸、水杨酸甲酯、茉莉酸甲酯,或者甚至是微生物是特别合适的。随后用提取液体(例如醇/水溶液)处理这样经分解的原料。醇含量应当是40-75%,优选地,已经证实50-60%的醇含量特别是乙醇含量是非常合适的。
例外,根据所选择的原料,这也可以通过机械措施预处理,或者在提取过程中另外加工,更具体地,通过破坏细胞壁和膜结构,从而释放成分,并使其进入溶剂。更具体地,应当为此选择常规的研磨方法。但是,也可以将新鲜的或冷冻的而又解冻的原料在高温下干燥,以此方式降低甲基丁香酚的浓度,该甲基丁香酚是一种组分,一种公认的致癌物,其特别是存在于某些变胞藻科(Asteraceen)例如龙蒿植物中。
本发明包括,作为优选的更具体的组合物,其中它是蒿提取物。在此特别合适的提取物是下述植物的提取物:龙蒿,A.herba-alba,A.judaica,艾蒿(A.vulgaris),A.abysinica,A.absynthicum,A.afra,A.cannariensis,A.pallens,黄花蒿(A.annua),A.abrotanum,A.ludoviciana,茵陈蒿(A.capillaris)和猪毛蒿(A.scoparia)。
在存在于这些提取物中的组分的分析中,作为龙蒿的特别合适的亚种,已经特别地证实有用的那些是,尤其是,俄罗斯龙蒿或法国龙蒿,因为它们含有足够且稳定浓度的本发明必需的化合物。
与此相关地还需指明,根据本发明的组合物有利地特征在于,它含有有效量的各化合物或混合物或提取物,所述有效量是1至1000000ppm,即表征纯物质的最大值。但是,优选地,有效量是10至20000ppm,且特别优选地100至5000ppm。这些量反映了下述事实,尤其是,不同的化合物在不同的量表现出它们的部分地彼此不同的、但是补充的作用,如已经讨论的,其可以从大约同种疗法范围延伸至高达纯物质。
除了所述的组合物以外,本发明还包括其用于生产预防和/或治疗(前驱)糖尿病和与此有关的形式、并发病和/或继发病的制剂的应用,认为共11个应用领域是优选的。要求保护的应用主要包括用于生产制剂,所述制剂优选影响a)哺乳动物的血糖水平,b)胰岛素耐受性,c)肝葡萄糖释放,d)GLP-1(“高血糖素样肽1”)的活性,e)GLP-1和相关受体之间的结合能力,f)葡萄糖向糖原的转化,g)IRS-2(“胰岛素受体底物2”)多肽的表达,h)胰岛素控制的葡萄糖摄取和/或i)餐后葡萄糖水平。但是,可以用于下述目的的制剂也是合适的:j)治疗或预防II和/或I型糖尿病,k)治疗或预防前驱糖尿病,和/或1)定向影响体重,和/或m)增加身体的工作能力。
在影响下述内容的情况下,所述的影响代谢过程的可能性可以优选地用于降低:a)血糖水平,b)胰岛素耐受性,c)肝葡萄糖释放和/或i)餐后葡萄糖水平,和在下述情况下,引起它们的增加:d)GLP-1的活性,e)GLP-1和它的受体之间的结合行为,f)葡萄糖向糖原的转化,g)IRS-2多肽的表达,以及h)胰岛素控制的葡萄糖摄取。
在另一个实施方案中,本发明包括所述制剂作为食品补充剂、饮料、(食疗)食物和/或功能食物的非治疗性应用。但是、临床营养的范围内和/或作为运动食物的应用也是可能的,在每种情况下,非治疗性的应用领域是突出的。所要求保护的组合物生产的制剂因而特别适用于所谓的OTC产品,从而也适用于自我药疗法。
独立于它们各自的应用目的、与其相关的应用形式,本发明提供了一定量的所述制剂的应用,在所述的量中,组合物的有效的每日量是0.1至500mg/kg体重,认为1.5至150mg/kg体重的范围是优选的,且认为15mg/kg体重是特别优选的。
除了根据本发明的化合物和另外列出的化合物以外,所述制剂也可以另外包含至少一种活性化合物和/或一种活性提取物,其选自:匙羹藤(Gymnema sylvestre)、胡卢巴(“Fenugreek”)、苦瓜、α-硫辛酸(盐)、Corosol-Sure、乌索尼酸、D-松醇、羊角掌(Aloevera)、Chrompicolinat、Banaba、Yacou、苦瓜(Momordica charantia)、橄榄、Pherocarpus marsupium、Salacia reticulata、大蒜、山楂、磷脂且尤其是磷脂酰丝氨酸、ω-3脂肪酸和淀粉。在本发明的范围内,可以使用这样组成的制剂,特别用于预防和治疗(前驱)糖尿病。
但是,本发明还包括制剂的应用,所述制剂除了生理活性的组合物以外,包含至少一种选自下述的活性化合物:丙酮酸、L-肉毒碱、羟基柠檬酸、麻黄碱、咖啡因、缀合的亚麻酸、乙酰基水杨酸、α-硫辛酸和/或其盐和衍生物。已经证实,所述制剂特别适用于控制体重和特别是用于降低体重。
但是,在本发明的范围内也可能包括制剂的用途,所述制剂除了生理活性的组合物以外,包含至少一种选自下述的活性化合物:胍化合物特别是肌酸、肌酸一水合物、胍乙酸、Kreatinol、肌酸-柠檬酸化合物、丙酮酸肌酸、磷酸肌酸以及咖啡因、α-硫辛酸、葡糖胺、软骨素、经水解的胶原蛋白、甲磺酰甲烷、乳清蛋白、L-谷氨酰胺、磷脂特别是磷脂酰丝氨酸、磷脂酰胆碱以及胆碱、β-羟基-β-甲基丁酸酯、丙酮酸、L-肉毒碱、D-核糖、氨基酸、S-腺苷甲硫氨酸、牛磺酸、缀合的亚麻酸、甘油、肉桂和/或盐和衍生物。制剂的这些变体主要适用于升高非脂肪细胞中的细胞能。
另外,根据本发明,要求保护一种药剂,其包含单独使用的或与至少一种上述活性化合物和/或提取物相联合的根据本发明的组合物。
总之,使用要求保护的化合物和相关的特别应用案例,不仅能完全满足目的,而且尤其是,可以联合使用对代谢过程有有益作用的经定义的化合物,这些化合物不仅作为纯物质,也以提取物(更具体地,植物提取物)的形式展现出所希望的作用。通过彼此联合,但是也与其它类型的化合物联合,可以部分地超加和性地提高这些化合物的功效,更具体地,在非医学领域的自我药疗法方面,为终端用户带来显著的优点。
下面的实施例解释的本发明的所述优点。
实施例
实施例1:龙蒿提取物的生产
粉碎500g经干燥的俄罗斯龙蒿(Artemisia dracunculus)的地上植物部分(粒度<10mm),用8升80%乙醇(按体积计)在45℃提取16h。随后,过滤提取物,在旋转蒸发器上浓缩滤液至200ml,与50g微晶纤维素混合,并冷冻干燥。得到175g绿色粉末。
提取物的HPLC分析给出了下面的含量:
7-甲氧基香豆素 360ppm
Davidigenin 990ppm
6-去甲氧基茵陈色原酮 1450ppm
6-去甲氧基-3′-甲氧基茵陈色原酮 15ppm
榄香素 195ppm
异榄香脂素 420ppm
Hispiludin 65ppm
9-羟基-10E,12Z,15Z-十八碳三烯酸 25ppm
4′-O-甲基davidigenin 465ppm
4-O-甲基davidigenin 35ppm
4-O-甲基davidigenin-4′-葡糖苷 585ppm
4-O-甲基davidigenin-4′-鼠李葡糖苷 675ppm
实施例2:醇的龙蒿提取物对II型糖尿病的餐后血糖水平的紧急作用-动物模型
以下列出了动物研究的结果,其中在具有肥胖症且同时具有升高的空腹血糖(II型糖尿病)的动物中研究了龙蒿提取物对餐后血糖水平的急性作用。使用葡萄糖溶液,其含有根据实施例1得到粉末。
在每种情况下,研究时间是最长5小时,其中以不同剂量的提取物或安慰剂,用每只动物进行口服葡萄糖耐量试验。
研究了共30只具有升高的血糖水平的大鼠,或研究了ob/ob小鼠(对ob基因(依据英语obese=肥胖的)纯合的脂肪小鼠),每个治疗组研究10只动物。禁食14小时后,测量动物中的禁食血糖水平。它是平均138.8mg/dl(小鼠)或136.0mg/dl葡萄糖(大鼠),且组之间没有显著差异。随后,通过胃管给动物施用给定量的葡萄糖溶液(3.33ml溶液/kg体重大鼠,或10ml/kg体重小鼠),该溶液含有500mg/kg体重或1000mg/kg体重的提取物溶液,或作为仅有葡萄糖溶液(60%浓度(大鼠)或20%浓度(小鼠)+作为增溶剂的2%吐温80)组成的对照。施用葡萄糖溶液后,以15分钟的间隔采血,持续180分钟,以确定血糖浓度和胰岛素浓度。表1和2给出了餐后葡萄糖水平的值。
所有动物都耐受治疗,没有任何不耐变性的迹象。
表1:用500mg/kg体重或1000mg/kg体重在葡萄糖溶液中的提取物或对照葡萄糖溶液治疗的糖尿病小鼠的餐后血糖浓度(mg/dl)
时间[min] | 0 | 15 | 30 | 60 | 90 | 120 | 180 |
对照 | |||||||
平均值 | 142.2 | 433.2 | 686.0 | 357.1 | 340.4 | 335.0 | 313.5 |
SD(标准偏差) | 54.2 | 88.2 | 118.9 | 110.5 | 124.2 | 131.9 | 97.5 |
500mg/kg体重 | |||||||
平均值 | 143.7 | 353.9 | 534.2 | 319.7 | 274.0 | 260.5 | 259.9 |
SD | 60.4 | 85.7 | 100.2 | 71.8 | 77.9 | 61.5 | 50.7 |
1000mg/kg体重 | |||||||
平均值 | 130.5 | 313.4 | 476.9 | 300.9 | 265.6 | 251.3 | 236.1 |
SD | 44.6 | 88.1 | 100.9 | 76.8 | 63.8 | 75.4 | 76.6 |
表2:用500mg/kg体重或1000mg/kg体重在葡萄糖溶液中的提取物或对照葡萄糖溶液治疗的糖尿病大鼠的餐后血糖浓度(mg/dl)
时间[min] | 0 | 15 | 30 | 60 | 90 | 120 | 180 |
对照 | |||||||
平均值 | 133.2 | 323.7 | 430.2 | 452.6 | 367.5 | 286.3 | 235 |
SD | 28.3 | 43.8 | 62.3 | 75.9 | 79.3 | 81.7 | 65.5 |
500mg/kg体重 | |||||||
平均值 | 135.2 | 306.9 | 382.4 | 364.2 | 294.8 | 230.5 | 195.8 |
SD | 16.1 | 65.8 | 77.2 | 59.3 | 58.2 | 55.2 | 46.8 |
1000mg/kg体重 | |||||||
平均值 | 139.6 | 281.4 | 314.3 | 297.7 | 245.6 | 210.4 | 194.2 |
SD | 42.2 | 99.8 | 82.4 | 91.8 | 102.2 | 93.2 | 55.4 |
实施例3:龙蒿提取物对患有葡萄糖耐受不良或II型糖尿病的人的餐后血糖水平的紧急作用
用于研究龙蒿提取物对患有葡萄糖耐受不良或II型糖尿病的人的餐后血糖水平的急性活性的单中心的、双盲随机安慰剂-控制的交叉研究。通过膳食耐量试验(MTT),确定制品的作用。
在研究中包括8位具有升高的禁食血糖水平、排它地接受食疗的男性或女性患者。在筛选试验(V0)中,测试可能的参与者的参与该研究的适合性,此外,该研究包含2个可走动的研究日出诊1(V1)+出诊2(V2),其由2-至3-周间歇期隔开,以及V2以后的最后研究。
已经建立参与者的适合性后,给参与者随机地指定治疗计划,并在双盲交叉方法的研究过程中,接受提取物以及安慰剂(微晶纤维素)的治疗。在各个研究日,在标准的早餐之前,在每种情况下的患者接受1000mg提取物或安慰剂的单独的经口给药,此后,通过在5小时内定期测定血糖值和随后分析血清胰岛素水平,确定治疗对餐后血糖水平的作用。随着出诊2(在该过程中进行最后研究)的完成,结束对参与者的研究。
感兴趣的人参与临床研究的前提是他/她对参与的书面同意,此后通知他/她关于临床研究的性质、重要性和后果口头和书面。研究人员有义务使研究符合国际调和大会(ICH)的赫尔辛基(Helsinki)宣言(爱丁堡修订版,2000年10月),即优良临床试验规范(GCP)的原则,和国家条例和指南。
发给参与者关于研究的所有方面以及数据保护的信息单。除了受试者的同意宣言外,通过负责的研究医生的签字,记录受试者的通知。
根据选择标准,在研究中包括5位男性和3位女性受试者,其年龄为35至70岁,BMI>29且<40kg/m2,禁食血糖水平≥125且≤220mg/dl,HbAlc值>6.1%,没有用片剂或胰岛素进行抗糖尿病治疗,以及同意的书面宣言条款。根据研究医生的估计,这些受试者没有表现出与初步试验的实验室值的任何临床上显著的差异(更具体地:血清肌酸酐和血清血红蛋白值,以及谷氨酸盐-草醋酸盐转氨酶(GOT)和谷氨酸盐-丙酮酸盐转氨酶(GPT)的活性,其指示着急性或慢性疾病/障碍)。
表3:标准早餐后,用1000mg提取物或安慰剂治疗的糖尿病受试者的餐后血糖浓度(mg/dl)
时间[min] | 0 | 30 | 60 | 90 | 120 | 180 | 300 |
安慰剂 | |||||||
平均值 | 142.4 | 202.7 | 234.4 | 243.7 | 223.5 | 185.7 | 152.6 |
SD | 2.59 | 5.95 | 7.08 | 9.53 | 7.32 | 4.89 | 3.30 |
1000mg | |||||||
平均值 | 141.3 | 185.7 | 218.4 | 207.6 | 184.8 | 159.3 | 133.7 |
SD | 3.34 | 14.59 | 10.55 | 6.18 | 3.31 | 4.78 | 3.45 |
表4:标准早餐后,用1000mg提取物或安慰剂治疗的糖尿病受试者的餐后血浆胰岛素浓度(μU/ml)
时间[min] | 0 | 30 | 60 | 90 | 120 | 180 | 300 |
安慰剂 | |||||||
平均值 | 14.1 | 79.9 | 149.8 | 173.8 | 178.7 | 148.3 | 56.9 |
SD | 4.2 | 18.4 | 26.7 | 20.2 | 23.7 | 14.5 | 6.3 |
1000mg | |||||||
平均值 | 13.2 | 72.1 | 134.4 | 156.7 | 145.5 | 118.6 | 42.9 |
SD | 2.9 | 20.3 | 18.9 | 26.8 | 19.6 | 11.4 | 7.3 |
Claims (23)
1.生理活性的组合物,其包含有效量的至少一种选自下述的化合物:4-O-甲基-davidigenin、4′-O-甲基-davidigenin、davidigenin、榄香素、异榄香脂素、7-甲氧基香豆素、去甲氧基茵陈色原酮特别是6-去甲氧基茵陈色原酮和/或6-去甲氧基-3′-甲氧基茵陈色原酮、hispiludin和9-羟基-10E,12Z,15Z-十八碳三烯酸以及它们的糖苷。
2.如权利要求所述1的生理活性的组合物,其特征在于,所述糖苷选自:4-O-甲基davidigenin和/或4′-O-甲基davidigenin的葡糖苷和/或鼠李葡糖苷,及其盐和衍生物,以及通过HPLC分析可检测到的蒿提取物中的化合物。
3.如权利要求1或2所述的组合物,其特征在于,它另外包含至少一种选自下述的化合物:绿原酸、柚皮素、黄酮类化合物、黄烷酮类化合物、萜烯、萜类化合物和/或其衍生物。
4.如权利要求3所述的组合物,其特征在于,它包含至少一种糖苷和/或苷元形式的化合物。
5.如权利要求1至4中任一项所述的组合物,其特征在于,它包含纯形式和/或作为混合物的化合物。
6.如权利要求6所述的组合物,其特征在于,它包含天然提取物形式的混合物。
7.如权利要求6所述的组合物,其特征在于,它包含醇和/或醇/水提取物。
8.如权利要求7所述的组合物,其特征在于,它包含醇/水提取物的醚级分。
9.如权利要求6至8中任一项所述的组合物,其特征在于,它是蒿提取物。
10.如权利要求9所述的组合物,其特征在于,蒿提取物是下述蒿的提取物:龙蒿(A.dracunculus)、A.herba-alba、A.judaica、艾蒿(A.vulgaris)、A.abysinica、A.absynthicum、A.afra、A.cannariensis、A.pallens、黄花蒿(A.annua)、A.abrotanum、A.ludoviciana、茵陈蒿(A.capillaris)和/或猪毛蒿(A.scoparia)。
11.如权利要求6至10中任一项所述的组合物,其特征在于,所述提取物源自龙蒿的亚种。
12.如权利要求11所述的组合物,其特征在于,所述亚种是俄罗斯或法国龙蒿。
13.如权利要求1至12中任一项所述的组合物,其特征在于,有效量是1至1000000ppm。
14.如权利要求1至13中任一项所述的组合物在生产制剂中的应用,所述制剂用于预防和/或治疗(前驱)糖尿病和相关形式、并发病和/或继发病。
15.如权利要求14所述的组合物,其特征在于,在(前驱)糖尿病和相关形式、并发病和继发病的预防和/或治疗中,它会影响:
a)哺乳动物的血糖水平,
b)胰岛素耐受性,
c)肝葡萄糖释放,
d)GLP-1(“高血糖素样肽1”)的活性,
e)GLP-1和相关受体之间的结合能力,
f)葡萄糖向糖原的转化,
g)IRS-2(“胰岛素受体底物2”)多肽的表达,
h)胰岛素控制的葡萄糖摄取,和/或
i)餐后葡萄糖水平,和
j)用于治疗和/或预防II和/或I型糖尿病,
k)用于治疗和/或预防前糖尿病,和/或
l)用于定向影响体重,和/或
m)增加身体的工作能力。
16.如权利要求15所述的应用,其特征在于,在a),b),c)和i)的情况下,影响是降低,且在d),e),f),g),h)的情况下,影响是增加。
17.如权利要求14至16中任一项所述的非治疗性应用,其特征在于,制剂用作食品补充剂,饮料,食品,食疗食品,功能食品、临床营养的范围内和/或作为运动食品。
18.如权利要求14至17中任一项所述的应用,其特征在于,所述制剂的使用量与权利要求1至14中任一项所述组合物的有效每日量相当,且为0.1至500mg/kg体重。
19.如权利要求14至18中任一项所述的应用,其特征在于,除了生理活性的组合物以外,所述制剂包含
a)至少一种活性化合物和/或一种活性提取物,其选自:匙羹藤(Gymnema sylvestre)、胡卢巴、苦瓜、α-硫辛酸(盐)、Corosol-Sure、乌索尼酸、D-松醇、羊角掌(Aloe vera)、Chrompicolinat、Banaba、Yacou、苦瓜(Momordica charantia)、橄榄、Pherocarpusmarsupium、Salaciareticulata、大蒜、山楂、磷脂、ω-3脂肪酸和/或淀粉,
b)至少一种活性化合物,其选自丙酮酸、L-肉毒碱、羟基柠檬酸、麻黄素、咖啡因、缀合的亚麻酸、乙酰基水杨酸、α-硫辛酸和/或其盐和衍生物,和/或
c)至少一种活性化合物,其选自胍化合物、咖啡因、α-硫辛酸、葡糖胺、软骨素、水解胶原蛋白、甲磺酰甲烷、乳清蛋白、L-谷氨酰胺、磷脂,以及胆碱、β-羟基-β-甲基丁酸酯、丙酮酸、L-肉毒碱、D-核糖、氨基酸、S-腺苷甲硫氨酸、牛磺酸、缀合的亚麻酸、甘油、肉桂和/或其盐和衍生物。
20.如权利要求19所述的应用,其特征在于,在a)的情况下,磷脂是磷脂酰丝氨酸,且在c)的情况下,胍化合物是肌酸、肌酸一水合物、胍乙酸、Kreatinol、肌酸-柠檬酸化合物、丙酮酸肌酸和/或磷酸肌酸且磷脂是磷脂酰丝氨酸和/或磷脂酰胆碱。
21.如权利要求19或20所述的应用,其特征在于,在a)的情况下,所述制剂用于预防和/或治疗(前驱)糖尿病,
在b)的情况下,所述制剂用于控制体重,尤其是用于减少体重,和
在c)的情况下,所述制剂用于增加非脂肪细胞的细胞能量。
22.药剂,其包含如权利要求1至13中任一项所述的组合物。
23.如权利要求22所述的药剂,另外包含至少一种权利要求19所述的活性化合物和/或活性提取物。
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DE102004036047.2 | 2004-07-24 | ||
DE102004036047A DE102004036047A1 (de) | 2004-07-24 | 2004-07-24 | Physiologisch aktive Zusammensetzung |
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EP (1) | EP1784201B1 (zh) |
JP (1) | JP2008507486A (zh) |
KR (1) | KR20070056067A (zh) |
CN (1) | CN101022818A (zh) |
AT (1) | ATE485049T1 (zh) |
AU (1) | AU2005266545A1 (zh) |
CA (1) | CA2574894A1 (zh) |
DE (2) | DE102004036047A1 (zh) |
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Cited By (4)
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CN102421424A (zh) * | 2009-03-16 | 2012-04-18 | 根梅迪卡治疗公司 | 用于治疗代谢性疾病的组合疗法 |
CN102762112A (zh) * | 2010-01-29 | 2012-10-31 | 雅培制药有限公司 | 包含hmb的塑料包装的营养液 |
CN103478632A (zh) * | 2013-09-17 | 2014-01-01 | 江西宇骏生物工程有限公司 | 一种果蔬保健片及其制备方法 |
US9241508B2 (en) | 2010-01-29 | 2016-01-26 | Abbott Laboratories | Nutritional emulsions comprising calcium HMB |
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BRPI0517429A (pt) * | 2004-12-16 | 2008-10-07 | Hills Pet Nutrition Inc | composição de ração, método para intensificar a palatabilidade de uma composição de ração e para reduzir o odor de excreta de animal, kit, e, meio para comunicar informação sobre ou instruções de uso das composições, dos métodos, ou dos kits |
PL1909601T3 (pl) * | 2005-08-02 | 2014-03-31 | Alzchem Ag | Ciekły preparat zawierający składnik na bazie kwasu guanidynooctowego |
JP2009527504A (ja) * | 2006-02-23 | 2009-07-30 | イオメディックス スリープ インターナショナル エスアールエル | 良質な睡眠の誘導および維持のための組成物および方法 |
US20070224301A1 (en) * | 2006-03-21 | 2007-09-27 | Ribnicky David M | Compounds from an extract of Artemisia and methods for treating disorders |
FR2914552B1 (fr) * | 2007-04-03 | 2012-08-03 | Darome | Procede d'extraction de coumarines |
EP2130443A1 (en) * | 2008-06-06 | 2009-12-09 | Finzelberg GmbH & Co. KG | Water-soluble extracts of Artemisia dracunculus (tarragon) for improvement of glucose metabolism |
JP2011528719A (ja) * | 2008-07-21 | 2011-11-24 | ユニジェン・インコーポレーテッド | スキンホワイトニング(色を薄くする)化合物系列 |
DE102009056927A1 (de) | 2009-12-03 | 2011-06-09 | Müller, R. Klaus, Prof. Dr. | Anregendes Kaltgetränk |
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WO2020209700A1 (ko) * | 2019-04-12 | 2020-10-15 | 이연제약 주식회사 | 용쑥 및 서양민들레를 포함하는 체중 또는 체지방 감소용 경구용 조성물 |
WO2021113473A1 (en) * | 2019-12-06 | 2021-06-10 | The Board Of Supervisors Of Louisiana State University And Agricultural And Mechanical College | Compositions and methods to modulate glucose homeostasis |
US20230129745A1 (en) * | 2020-02-06 | 2023-04-27 | Board Of Supervisors Of Louisiana State University And Agricultural And Mechanical College | Compounds, compositions, and methods to treat metabolic disease |
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EP0854712B1 (en) * | 1995-10-11 | 2003-05-07 | Avicena Group, Inc. | Use of creatine analogues for the treatment of disorders of glucose metabolism |
US5891855A (en) * | 1996-02-12 | 1999-04-06 | The Scripps Research Institute | Inhibitors of leaderless protein export |
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AU2003234146A1 (en) * | 2002-04-22 | 2003-11-03 | Experimental And Applied Sciences, Inc. | Food supplements containing 4-hydroxyisoleucine and creatine |
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2004
- 2004-07-24 DE DE102004036047A patent/DE102004036047A1/de not_active Withdrawn
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2005
- 2005-07-21 US US11/658,342 patent/US20090142425A1/en not_active Abandoned
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- 2005-07-21 CN CNA200580031615XA patent/CN101022818A/zh active Pending
- 2005-07-21 KR KR1020077004084A patent/KR20070056067A/ko not_active Application Discontinuation
- 2005-07-21 CA CA002574894A patent/CA2574894A1/en not_active Abandoned
- 2005-07-21 WO PCT/EP2005/007964 patent/WO2006010560A2/de active Application Filing
- 2005-07-21 DE DE502005010427T patent/DE502005010427D1/de active Active
- 2005-07-21 AT AT05776027T patent/ATE485049T1/de active
- 2005-07-21 EP EP05776027A patent/EP1784201B1/de not_active Not-in-force
- 2005-07-21 JP JP2007521905A patent/JP2008507486A/ja active Pending
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Cited By (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN102421424A (zh) * | 2009-03-16 | 2012-04-18 | 根梅迪卡治疗公司 | 用于治疗代谢性疾病的组合疗法 |
CN102762112A (zh) * | 2010-01-29 | 2012-10-31 | 雅培制药有限公司 | 包含hmb的塑料包装的营养液 |
US9241508B2 (en) | 2010-01-29 | 2016-01-26 | Abbott Laboratories | Nutritional emulsions comprising calcium HMB |
CN103478632A (zh) * | 2013-09-17 | 2014-01-01 | 江西宇骏生物工程有限公司 | 一种果蔬保健片及其制备方法 |
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WO2006010560A8 (de) | 2006-03-30 |
DE502005010427D1 (de) | 2010-12-02 |
CA2574894A1 (en) | 2006-02-02 |
NZ553170A (en) | 2011-03-31 |
EP1784201B1 (de) | 2010-10-20 |
ATE485049T1 (de) | 2010-11-15 |
JP2008507486A (ja) | 2008-03-13 |
WO2006010560A3 (de) | 2006-06-01 |
EP1784201A2 (de) | 2007-05-16 |
AU2005266545A1 (en) | 2006-02-02 |
DE102004036047A1 (de) | 2006-02-23 |
WO2006010560A2 (de) | 2006-02-02 |
US20090142425A1 (en) | 2009-06-04 |
KR20070056067A (ko) | 2007-05-31 |
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