CN113230243A - 二甲基甘氨酸在制备降低体重的药物中的应用 - Google Patents
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- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
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Abstract
本发明涉及二甲基甘氨酸在制备降低体重的药物中的应用。本发明通过动物实验研究，发现二甲基甘氨酸能够有效降低肥胖模型小鼠体重和血糖水平，改善肥胖模型小鼠糖耐量受损，且由于二甲基甘氨酸本身具有口服利用率高、使用剂量小、安全可靠的优点，因此将二甲基甘氨酸用于制备降低体重的药物或减肥的保健品具有很好的应用潜力。
Description
技术领域
本发明涉及医药技术领域，具体涉及二甲基甘氨酸在制备降低体重的药物中的应用。
背景技术
二甲基甘氨酸(Dimethylglycine，DMG)，分子式为(CH3)2NCH2COOH，外观为白色结晶，天然存在于谷物、豆类及动物肝脏中，是动植物代谢途径的天然物质。在动物体内，胆碱代谢产物甜菜碱在甜菜碱同型半胱氨酸转甲基酶的作用下转移一个甲基产生DMG。DMG在体内作为甲基供体发挥作用，其提供甲基给甲硫氨酸生成同型半胱氨酸，参与机体甲基循环。DMG在体内经由肝脏的脱甲基氧化酶代谢给四氢叶酸酯贡献两个甲基分别生成肌氨酸和甘氨酸，这些产物在细胞内发挥着重要的作用。
DMG目前被用作饲料添加剂，在动物的健康上显示出重要的生理生化功能。在肉鸡日粮中添加1000-1500mg/kg的DMG-Na能显著提高肉鸡胸肌的总抗氧化能力，并且随着添加剂量的提高，其能从一定程度上提高肉鸡的抗氧化能力。而在人体中，DMG作为一种营养代谢增强剂可增强运动员的运动机能，运动员口服DMG可增强运动机能和耐力，提高氧气利用率以及促进高强度运动后的肌肉恢复。DMG也被研究发现可用于治疗忧郁症、自闭症等神经系统和精神疾病。
然而，DMG的临床使用和开发利用，至今没有取得突破性进展。单独使用以二甲基甘氨酸为代表成分的药物是否具有明显的降低体重作用目前未见相关文献报道。
发明内容
本发明的目的是针对现有技术中的不足，提供二甲基甘氨酸的新用途。
本发明采取的具体技术方案为：
二甲基甘氨酸的用途，用于制备降低体重的药物或减肥的保健品。
作为本发明的一种具体实施方式，所述二甲基甘氨酸为唯一的活性成分。
作为本发明的另一种具体实施方式，所述药物或保健品包含常规载体。
可选地，所述常规载体选自乳化剂、填充剂、粘合剂、润湿剂、崩解剂、吸收促进剂、调味剂、着色剂和助溶剂。
作为本发明的另一种具体实施方式，所述药物或保健品为口服剂型。
可选地，所述口服剂型为片剂、胶囊剂、颗粒剂、丸剂或合剂。
作为本发明的另一种具体实施方式，所述二甲基甘氨酸用于制备针对肥胖并伴有高血糖个体的降低体重的药物或减肥的保健品。
可选地，所述肥胖并伴有高血糖是由于高脂饮食引起的。
本发明优点在于：
本发明经动物实验研究，发现二甲基甘氨酸能够有效降低肥胖模型小鼠体重和血糖水平，改善其糖耐量，进一步有预防糖尿病发生的作用。由于二甲基甘氨酸本身具有以下优点：(1)DMG作为一种小的水溶性亲脂分子能有效的通过细胞膜被肠壁细胞吸收而进入机体，使得口服DMG在机体中利用率得到提高；(2)DMG是人体内天然存在的小分子化合物，能有效的被机体内的酶系统代谢，且作为一种非常安全的食品类营养添加物被应用于畜牧业，因此其十分安全可靠；(3)DMG降血糖的治疗剂量远小于毒性剂量，且效果明显。因此，将二甲基甘氨酸用于制备降低体重、降血糖的药物或减肥保健品具有极大的应用潜力。
具体实施方式
下面对本发明提供的具体实施方式作详细说明。
实施例1二甲基甘氨酸对C57小鼠的降低体重作用
实验方法：选用8周龄雌性C57小鼠(上海斯莱克)，体重15.0g左右，20只，进行15周高脂饮食(戴茨生物)诱导发生肥胖和血糖升高，于造模前后测量小鼠体重，并使用血糖仪和血糖试纸测量尾静脉血糖。二甲基甘氨酸(DMG，上海生工)溶于生理盐水中，于小鼠造模成功后灌胃。
实验步骤：
(1)配制药品：称取DMG 250mg，溶于50ml 0.9％NaCl(生理盐水)溶液配成5mg/ml待用，称取戊巴比妥钠300mg，溶于30ml 0.9％NaCl(生理盐水)溶液配成10mg/ml待用。
(2)分组并造模：将20只雌性C57小鼠随机分成4组并标记，A(高脂饮食组)5只，B(高脂饮食+DMG组)5只，C(普通饮食组)5只，D(普通饮食+DMG组)5只。给予A、B两组为期15周的高脂饮食。
(3)给药：造模成功后，B、D两组小鼠均按照165mg/kg每3天灌胃给药共计15天；A、C两组小鼠给予相同剂量生理盐水作为对照。给药期间，各组老鼠维持原饮食不变。
(4)体重测量：给药前后，测量所有小鼠的体重并记录。
(5)血糖测定：给药前后，测量所有小鼠的随机血糖，并按1g/kg腹腔内注射葡萄糖进行糖耐量测验。
实验结果：各组小鼠给药前后的体重、血糖以及糖耐量测试结果见表1。数据表明，DMG可以显著降低高脂饮食组小鼠的体重和血糖水平，改善糖耐量，因此证明DMG有降低体重和降血糖的作用。
表1各组小鼠给药前后的体重、血糖和糖耐量
注：p#为高脂饮食+DMG组与高脂饮食组比较，p·为高脂饮食组与普通饮食组比较，pS为普通饮食+DMG组与普通饮食组比较
以上所述仅是本发明的优选实施方式，应当指出，对于本技术领域的普通技术人员，在不脱离本发明方法的前提下，还可以做出若干改进和补充，这些改进和补充也应视为本发明的保护范围。
Claims (6)
1.二甲基甘氨酸的用途，其特征在于，用于制备降低体重的药物或减肥的保健品。
2.根据权利要求1所述的用途，其特征在于，所述二甲基甘氨酸为唯一的活性成分。
3.根据权利要求1所述的用途，其特征在于，所述药物或保健品包含常规载体。
4.根据权利要求3所述的用途，其特征在于，所述常规载体选自乳化剂、填充剂、粘合剂、润湿剂、崩解剂、吸收促进剂、调味剂、着色剂和助溶剂。
5.根据权利要求1所述的用途，其特征在于，所述药物或保健品为口服剂型。
6.根据权利要求5所述的用途，其特征在于，所述口服剂型为片剂、胶囊剂、颗粒剂、丸剂或合剂。
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| CN110381944A (zh) * | 2016-12-22 | 2019-10-25 | 斯堪的比奥疗法有限公司 | 用于治疗脂肪肝相关病症的物质 |
| US20200296994A1 (en) * | 2017-10-25 | 2020-09-24 | Guangzhou Insighter Biotechnology Co., Ltd. | The compound salt of n,n-dimethylglycine and an organic acid and composition and use thereof |
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