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CN100361599C - 抗氧化组合物 - Google Patents

抗氧化组合物 Download PDF

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Publication number
CN100361599C
CN100361599C CNB2003801021043A CN200380102104A CN100361599C CN 100361599 C CN100361599 C CN 100361599C CN B2003801021043 A CNB2003801021043 A CN B2003801021043A CN 200380102104 A CN200380102104 A CN 200380102104A CN 100361599 C CN100361599 C CN 100361599C
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vitamin
quercetin
tea
epicatechin
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CN1708234A (zh
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托马斯·克里斯琴·莱恩斯
小野光则
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FRS Co.
The new nutrition Co.
The new nutrition LLC
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Quercegen Holdings LLC
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Abstract

本发明涉及一种组合物，其包含槲皮素、维生素B1、维生素B2、维生素B3、维生素B6、维生素C、咖啡因、表没食子儿茶素没食子酸酯、表儿茶素、表儿茶素没食子酸酯、表没食子儿茶素及polypheron E。

Description

抗氧化组合物
相关申请的交叉参考
本申请要求于2002年11月22日提交的第10/302,544号美国专利申请的优先权，其又要求于2002年10月23日提交的第60/420,986号美国临时申请的优先权。
技术领域
本发明涉及抗氧化组合物。
背景技术
众所周知，某些天然抗氧化剂如植物类黄酮能抑制自由基所引起的急性或慢性疾病。并且，某些天然抗氧化剂在同与生物相关的氧化物如羟基、过氧化物、氧硫化物(oxysulfurs)、二氧化硫及二氧化氮反应时存在协同作用(synergy)。例如，研究已发现维生素C及酚类抗氧化剂的协同抗氧化活性。
发明内容
本发明基于一项出人意料的发现，槲皮素，一种抗氧化剂，及多种其它天然产物具有协同的有益健康的功效。
本发明公开一种组合物，其包含下列成分：维生素B1、维生素B2、维生素B3、维生素B6、维生素B12、维生素C、咖啡因、槲皮素、表没食子儿茶素没食子酸酯、表儿茶素、表儿茶素没食子酸酯、表没食子儿茶素及去咖啡因绿茶儿茶素混合物(polyphenon E)。该组合物还可包含其它成分，如维生素E、CoQ-10、大豆异黄酮、牛磺酸、甜菜果胶纤维或银杏提取物。该组合物还可进一步视需要添加甜味剂以提高甜度，前述甜味剂为例如山梨醇、麦芽糖醇、蔗糖、高果糖玉米糖浆等。该组合物还可包含氨基酸、矿物质、增味剂或着色剂。绿茶的叶子已知包含表没食子儿茶素没食子酸酯、表儿茶素、表儿茶素没食子酸酯、表没食子儿茶素及去咖啡因绿茶儿茶素混合物。因此前述五种成分适合由绿茶提取物提供。
本发明组合物可为干燥形式(如粉末或片剂)或含水形式(如饮料或糖浆)。其可为饮食补充剂或药物制剂，亦可为饮料或食品。其实例包括：茶(如茶饮料或袋装茶叶内容物)、软饮料、果汁(如水果提取物或果汁饮料)、牛奶、咖啡、饼干、禾谷类食品(cereals)、巧克力及消闲食品(snack bars)。本发明组合物在任何前述形式下皆可用于治疗关节炎、肿瘤、性功能障碍、慢性便秘、炎症性肠疾病；改善注意力或情绪；及降低胆固醇水平或血压。作为活性药物的本发明组合物以及该组合物在制备用于治疗上述疾病的药物中的应用也属于本发明的范围之内。
随着下文的叙述给出本发明一种或多种具体实施方式。其他本发明的特征、目的以及优点将通过说明书以及权利要求书加以说明。
具体实施方式
本发明组合物包含维生素B1、维生素B2、维生素B3、维生素B6、维生素B12、维生素C、咖啡因、槲皮素、表没食子儿茶素没食子酸酯、表儿茶素、表儿茶素没食子酸酯、表没食子儿茶素及去咖啡因绿茶儿茶素混合物。绿茶提取物适合用于提供表没食子儿茶素没食子酸酯、表儿茶素、表儿茶素没食子酸酯、表没食子儿茶素及去咖啡因绿茶儿茶素混合物。
该组合物成分的示例性含量为：0.1-50mg维生素B1、0.1-150mg维生素B2、0.1-2000mg维生素B3、0.1-200mg维生素B6、5-150μg维生素B12、50-2000mg维生素C、50-1500mg咖啡因、20-2000mg槲皮素、10-500mg表没食子儿茶素没食子酸酯、10-500mg表儿茶素、10-500mg表儿茶素没食子酸酯、10-500mg表没食子儿茶素及10-500mg的去咖啡因绿茶儿茶素混合物，其中前述成分可溶解或分散于1L水溶液中。这些成分的含量也可为与前述含量的相对比例相同。术语”槲皮素”指槲皮素苷元及槲皮素衍生物，例如：槲皮素-3-O-葡糖苷、槲皮素-5-O-葡糖苷、槲皮素-7-O-葡糖苷、槲皮素-9-O-葡糖苷、槲皮素-3-O-芸香糖苷、槲皮素-3-O-[α-鼠李糖基-(1→2)-α-鼠李糖基-(1→6)]-β-葡糖苷、槲皮素-3-O-半乳糖苷、槲皮素-7-O-半乳糖苷、槲皮素-3-O-鼠李糖苷及槲皮素-7-O-鼠李糖苷。在消化后，槲皮素衍生物转化为槲皮素苷元，一种被身体吸收的活性形式。前述槲皮素含量指槲皮素苷元或槲皮素衍生物中槲皮素部分的含量。例如：每日使用的组合物可为1L水溶液，该水溶液包含1000mg槲皮素、30mg维生素B1、85mg维生素B2、1g维生素B3、100mg维生素B6、120μg维生素B12、1200mg维生素C、1000 IU维生素E、1000mg咖啡因及包含120mg表没食子儿茶素没食子酸酯、140mg表儿茶素、360mg表儿茶素没食子酸酯、360mg表没食子儿茶素及120mg去咖啡因绿茶儿茶素混合物的绿茶提取物。
该组合物也可包含一种或多种其它活性成分，如维生素E、CoQ-10、大豆异黄酮、牛磺酸、甜菜果胶纤维及银杏提取物。这些成分的示例性含量为：3-1000 IU维生素E、10-400mg的CoQ-10、20-600mg大豆异黄酮、10-1000mg牛磺酸、1-15g甜菜果胶纤维及50-500mg银杏提取物(干重)。该组合物还可进一步视需要通过添加甜味剂来提高甜度，甜味剂例如为山梨醇、麦芽糖醇、氢化葡萄糖浆、氢化淀粉水解产物、高果糖玉米糖浆、蔗糖、甜菜糖、果胶及三氯半乳蔗糖。
前述组合物的一个实例为粉末形式，其可适用于制备饮料，如茶或果汁。该粉末组合物亦可用于制备糊、凝胶、胶囊或片剂。乳糖及玉米淀粉通常在胶囊中用作稀释物以及在片剂中用作载体。一般可加入润滑剂，如硬脂酸镁，以形成片剂。
本发明组合物可为饮食补充剂或药物制剂。作为饮食补充剂，该组合物可包含额外的营养物如矿物质或氨基酸。该组合物还可为饮料或食品，如茶、软饮料、果汁、牛奶、咖啡、饼干、禾谷类食品、巧克力及消闲食品。
本发明组合物在任何前述形式下皆可用于治疗疾病或病症，如关节炎、肿瘤、性功能障碍、慢性便秘、炎症性肠疾病；并改善注意力或情绪；及降低胆固醇水平或血压。术语“肿瘤”指良性肿瘤及恶性肿瘤(白血病、结肠癌、肾癌、肝癌、乳腺癌或肺癌)。术语“治疗”、“改善”及“降低”指向患有一种或两种前述疾病或病症的患者，或具有一种或多种前述疾病之征状或倾向的患者给药有效量的本发明组合物，其目的在于治愈、减轻、缓解、矫正或改善一种或多种疾病或病症，或一种或多种疾病或病症的征状或倾向。术语“给药”涵盖以任何适宜的形式向患者口服或非胃肠道传递本发明组合物，该适宜的形式为例如食品、饮料、片剂、胶囊、混悬剂及溶液。术语“非胃肠道”指皮下、皮内、静脉内、肌内、关节内、动脉内、滑液内、胸骨内、鞘内、病灶内、或颅骨内注射，及不同的输注技术。术语“有效量”指能充分提供治疗疗效的组合物剂量，该疗效为例如降低胆固醇水平或血压。可进行体内及体外试验以确定最佳给药途径及给药剂量。
下列具体实施例应被认为仅为说明性，而绝不能被认为是用于限制本发明所公开的其他部分。任何熟悉本技术领域之人士可依本说明书公开的内容，不需进一步阐述即可最充分地利用本发明。此处引用的所有文献在此全文并入作为参考。
制剂1制备如下。室温下，向30mL纯水中加入维生素B1(8mg)、维生素B2(21.1mg)、维生素B3(248mg)、维生素B6(24.8mg)、维生素B12(20.4mg)、维生素C(74.4mg)、维生素E(37.2 IU)、咖啡因(99.2mg)、槲皮素苷元(248mg)、及包含表没食子儿茶素没食子酸酯(80mg)、表儿茶素(80mg)、表儿茶素没食子酸酯(80mg)、表没食子儿茶素(80mg)及去咖啡因绿茶儿茶素混合物(80mg)的绿茶提取物。所有成分可自Spectrum Laboratory Products，Inc.，Gardena，CA；sigma，St.Louis，MO；及Aldrich，Milwaukee，WI.获得。将前述混合物用食品混拌器剧烈搅拌，然后以纯水稀释至150mL。
在一实验中，雄性Spregue-dawley大鼠(150-180克，Charles RiverLab，boston，MA)被置于顶端有滤网的笼子并可自由进食食物和水，并养在在试验期间内控制温度和光周期的正压房间内。炎症性肠疾病(如Crohn’s病)、结肠炎(发炎导致的结肠生长)的动物模型通过在结肠内滴注溶于0.5ml体积比30％乙醇的25mg半抗原试剂2，4-二硝基苯磺酸(TCI，Japan)诱导。每一只大鼠先以metafane麻醉，然后以PE 50插管将DNBS/乙醇注入结肠内距离肛门8公分处。然后通过插管缓慢注入2ml空气以确保溶液留在结肠中，之后将大鼠维持直立位置30秒后放回鼠笼中。以相同的方法，为空白对照组大鼠注入0.5ml、30％乙醇。请参阅Hogaboam，等，Eur.J.Pharmacol.(1996)309：261-269。制剂1及包含甲基纤维素(MC)最终浓度为1％的槲皮素苷元溶液分别一天一次口服方式饲予大鼠，持续7天。每个每日剂量包含每公斤体重3.125mg至25mg的槲皮素苷元。每24小时监测大鼠的体重。在第七天，处死大鼠并取出结肠称重。在取出每一条结肠前，在打开腹腔时记录结肠与其它器官是否存在粘连，然后计算出每只动物的结肠-体重比，赋形剂对照组相对于空白对照组比率的净增加作为与治疗组比较的基准值。制剂1与槲皮素苷元两者在25mg/kg剂量下能抑制结肠成长，但在3.125mg/kg的剂量下无法抑制结肠成长。然而，在6.25mg/kg和12.5mg/kg的剂量下，制剂1对结肠生长的抑制远比槲皮素苷元有效。
在另一实验中，通过悬浮土壤制备10mg/ml的细菌混悬液，在不完全弗氏佐剂中加热杀死结核杆菌H37Ra。在雌性Lewis大鼠中将0.1ml前述混悬剂皮内注射至尾巴基部以诱发佐剂性关节炎(AA)。然后，自诱导之后那天开始，口服给予该大鼠制剂1或槲皮素苷元溶液(1％MC)，每天一次持续12天，每日剂量为25mg/kg槲皮素糖苷。在关键期间(从免疫后10日至25日)，每日用肉眼观察监测多发性关节炎的发展并为所有动物指定关节炎指数。多发性关节炎的强度依下列方案评分：(a)根据关节的红斑、肿胀及畸形给予每只脚爪等级为0-3的评分，即0表示没有红斑或肿胀；如果在至少一关节上可观察到肿胀则给予0.5；1表示轻微的肿胀及红斑；2表示脚踝及腕骨都有肿胀及红斑；3表示关节强直及骨头畸形。(b)身体其它部分的等级：0.5表示耳朵呈红色，另一个0.5表示耳朵有硬块；1表示鼻子结缔组织肿胀；及1表示尾巴打结或扭结。参考Schorlemmer等，Drugs Exptl.Clin.Res.(1991)17：471-483。与使用槲皮素苷元治疗的大鼠比较，以制剂1治疗的大鼠在18天时关节炎症状显示出更为显著的改善。
在另一实验中，雌性BD2F1(C57BL/6xDBA/2F1)大鼠自CharlesRiver Lab获得。大鼠可自由进食食物及水。在第0天，向7周龄雌性BD2F1大鼠腹膜内接种50,000 p388白血病细胞作为癌症动物模型。制剂1或槲皮素苷元溶液(1％MC)口服给药每日一次持续14天，每日剂量为12.5mg/kg槲皮素苷元。所有对照组大鼠而非治疗组大鼠在21天左右时死于腹水。通过比较治疗组与对照组的平均存活时间来确定抗癌活性。参考Yoshimatsu等，cancer Res.(1997)57：3208-3213。与以槲皮素苷元治疗的大鼠相较，以制剂1治疗的大鼠显示长得多的平均存活时间。
磷酸二酯酶-5(PDE-5)是一种参与性功能的酶。在进一步的实验中，以加以修改的众所周知的方法测定PDE-5的活性。参考Thompson等，Method Enzymol.(1974)38：205-212。纯化PDE-5的活性通过在1μM至100μM范围内不同浓度的制剂1、槲皮素苷元溶液及3-异丁基-1-甲基黄嘌呤(IBMX，一种常见的PDE-5抑制剂)溶液(1％MC)存在下与pH 7.5的混合物反应测量，该混合物包含8μM cGMP(64μCi/ml的[3H]-cGMP)、40mM MOPS、0.5mM EGTA、15mM醋酸镁、0.15mg/mlBSA。该反应在37℃下进行60分钟，然后加热至70℃维持2分钟以终止反应。之后，标记的酶促反应产物[3H]-GMP在0.1单位的核苷酸酶存在下降解成[3H]-鸟苷及磷酸。最后，未降解的[3H]-cGMP吸附于阴离子交换树脂，上清液中的[3H]-鸟苷在液体闪烁计数器中计数测定其放射性。结果显示制剂1抑制PDE-5活性的能力表现出剂量依赖性，其IC50值远低于槲皮素苷元和IBMX。
还进行了人体研究以评价本发明其它两种制剂，即制剂2和3。制剂2制备如下。室温下，向200mL纯水中加入维生素B1(30mg)、维生素B2(85mg)、维生素B3(1g)、维生素B6(100mg)、维生素B12(120μg)、维生素C(1200mg)、维生素E(1000 IU)、咖啡因(1000mg)、槲皮素苷元(1000mg)、及包含表没食子儿茶素没食子酸酯(120mg)、表儿茶素(140mg)、表儿茶素没食子酸酯(360mg)、表没食子儿茶素(360mg)及去咖啡因绿茶儿茶素混合物(120mg)的绿茶提取物。用食品混拌器剧烈搅拌前述混合物，然后以纯水稀释至1L。制剂3之制备如下。室温下，向200mL的纯水中加入维生素B1(3.75mg)、维生素B2(4.25mg)、维生素B3(50mg)、维生素B6(5mg)、维生素B12(15μg)、维生素C(150mg)、维生素E(7.5 IU)、咖啡因(200mg)、槲皮素苷元(50mg)、及包含表没食子儿茶素没食子酸酯(30mg)、表儿茶素(35mg)、表儿茶素没食子酸酯(90mg)、表没食子儿茶素(90mg)及去咖啡因绿茶儿茶素混合物(30mg)的绿茶提取物。将前述混合物用食品搅拌器剧烈搅拌。然后以纯水和橙汁将该混合物稀释至1L，使得最后溶液中包含10％重量百分比的橙汁。
在一研究试验中，以制剂2治疗患有高胆固醇和高血压的4位男性和4位女性受试者。每位受试者每日饮用1瓶制剂2(20fl.oz.，或591mL)持续10日。然后，该组中一半(1位男性受试者和3位女性受试者)继续每日饮用1瓶相同的制剂持续20日。组中另一半则停止此种治疗方案5天，然后开始每日饮用2瓶相同制剂持续20日。结果显示，所有受试者的集中力和情绪都得以改善。胆固醇水平和血压也下降至正常范围内。在受试者身上并没有观察到显著的体重减轻。两组中各有一位受试者在研究期间感到口渴。
在另一研究试验中，两位男性受试者和两位女性受试者持续1个月每日饮用2瓶制剂2(每瓶20fl.oz.)。结果显示，所有受试者的情绪和性欲皆得以改善。所有受试者的体重都经历10-25磅(体重的2-6％)范围内的减轻。在治疗方案结束后，大部分受试者具有情绪波动。
在另一研究测试中，以制剂3治疗患有严重便秘的一位男性和三位女性受试者。每位受试者持续1周每日饮用1-3瓶制剂3(每瓶20fl.oz.)。所有受试者的便秘都得以缓解。
在另一研究测试中，一位患有克罗恩氏病(Crohn’s disease)并有胃痛和腹泻症状的男性受试者使用制剂3治疗。该患者每日饮用2瓶制剂3(每瓶20fl.oz.)，持续一周。两种症状都显著减轻并且效果在治疗方案结束后仍维持至少1周。
其他具体实施方案
所有本说明书所公开之特征皆可以任何形式加以联合。本说明书中所公开的特征可以具有相同、相等或相似目的的特征所取代。因此，除非明确说明，所有本说明书中公开的特征仅为一系列相等或相似特征中的一个实例。
根据本说明书所公开的内容，任何一位熟习本技术领域的人士可轻易确认本发明的本质特征，且在不脱离其精神与范围下，可对本发明做出不同的改变与修饰使其符合不同的用途与情况。因此，其它具体实施方案也包含在下述权利要求书中。

Claims (16)

1.一种组合物，其包含维生素B1、维生素B2、维生素B3、维生素B6、维生素B12、维生素C、咖啡因、槲皮素、表没食子儿茶素没食子酸酯、表儿茶素、表儿茶素没食子酸酯、表没食子儿茶素以及去咖啡因绿茶儿茶素混合物，其中各成分的重量比为0.1-50维生素B1，0.1-150维生素B2，0.1-2000维生素B3，0.1-200维生素B6，0.005-0.15维生素B12，50-2000维生素C，50-1500咖啡因，20-2000槲皮素，10-500表没食子儿茶素没食子酸酯，10-500表儿茶素，10-500表儿茶素没食子酸酯，10-500表没食子儿茶素，10-500去咖啡因绿茶几茶素混合物。
2.如权利要求1所述的组合物，其进一步包含维生素E。
3.如权利要求1所述的组合物，其进一步包含CoQ-10、大豆异黄酮、牛磺酸、甜菜果胶纤维或银杏提取物。
4.如权利要求2所述的组合物，其进一步包含CoQ-10、大豆异黄酮、牛磺酸、甜菜果胶纤维或银杏提取物。
5.如权利要求1所述的组合物，其中所述组合物为干燥形式。
6.如权利要求2所述的组合物，其中所述组合物为干燥形式。
7.如权利要求3所述的组合物，其中所述组合物为干燥形式。
8.如权利要求4所述的组合物，其中所述组合物为干燥形式。
9.如权利要求1所述的组合物，其中所述组合物为茶、软饮料、果汁、牛奶、咖啡、饼干、禾谷类食品、巧克力或消闲食品。
10.如权利要求2所述的组合物，其中所述组合物为茶、软饮料、果汁、牛奶、咖啡、饼干、禾谷类食品、巧克力或消闲食品。
11.如权利要求3所述的组合物，其中所述组合物为茶、软饮料、果汁、牛奶、咖啡、饼干、禾谷类食品、巧克力或消闲食品。
12.如权利要求4所述的组合物，其中所述组合物为茶、软饮料、果汁、牛奶、咖啡、饼干、禾谷类食品、巧克力或消闲食品。
13.如权利要求1所述的组合物在制备用于治疗克罗恩氏病、关节炎、白血病、性功能障碍、或慢性便秘；改善注意力或情绪；或降低胆固醇水平或血压的药物中的应用。
14.如权利要求13所述的应用，其中所述组合物进一步包含维生素E。
15.如权利要求13所述的应用，其中所述组合物进一步包含CoQ-10、大豆异黄酮、牛磺酸、甜菜果胶纤维或银杏提取物。
16.如权利要求14所述的应用，其中所述组合物进一步包含CoQ-10、大豆异黄酮、牛磺酸、甜菜果胶纤维或银杏提取物。
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