CN101810625A - 蒲公英甾醇的应用 - Google Patents
蒲公英甾醇的应用 Download PDFInfo
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Abstract
本发明涉及医药领域，公开了蒲公英甾醇的医药用途。蒲公英甾醇对于α-葡萄糖苷酶和α-淀粉酶有抑制作用，其抑制效果是阿卡波糖的5～60倍。因此可用于制备α-葡萄糖苷酶抑制剂、α-淀粉酶抑制剂和制备治疗糖尿病药物。蒲公英甾醇在植物中存在范围广，易得，性质比较稳定；既安全又经济，极具推广应用价值。
Description
技术领域
本发明涉及医药领域，具体为蒲公英甾醇在制药方面的应用，尤其是在制备α-葡萄糖苷酶抑制剂、α-淀粉酶抑制剂和制备治疗糖尿病药物方面的应用。
背景技术
糖尿病是一种以高血糖为特征，代谢紊乱，与胰岛素分泌密切相关的全身性疾病。全球糖尿病患者超过1.5亿，我国约有2000万，其中80％为非胰岛素依赖性糖尿病(2型)。糖尿病已成为心血管病、癌症之后的第三位“健康杀手”。
对于2型糖尿病人，餐后高血糖对机体的危害远远超过空腹高血糖，不仅极易诱发各种并发症，还会极大地增加糖尿病的死亡率。所以降低餐后血糖是预防糖尿病、减少并发症和降低死亡率的重要措施。目前α-葡萄糖苷酶抑制剂已被推荐为降低餐后血糖的一线药物。食物中主要成分是碳水化合物-淀粉，正常人进食后淀粉等被胰淀粉酶和糖苷酶水解成单糖被机体吸收。糖尿病患者因代谢障碍而导致血糖、胰岛素和脂蛋白的浓度发生异常改变。控制的方法是限制多糖在消化道内的分解和吸收。为此要降低α-葡萄糖苷酶和α-淀粉酶的活性，阻滞双糖水解成单糖，延缓糖的吸收，使血糖平稳。
Hussain Z以及Cho S.Y.等报道，蒲公英乙醇提取物有促进胰岛素分泌和降低糖尿病小鼠的血清葡萄糖浓度的效果。在我们筛选中药常见成分体外对α-葡萄糖苷酶和α-淀粉酶抑制活性时，发现了蒲公英甾醇有很强的抑制活性，IC50＜8μg/ml，是阿卡波糖活性的5～60倍，这为开发防治糖尿病及其并发症的新药展现了令人鼓舞的前景。
发明内容
本发明的目的在于将蒲公英甾醇应用于制备α-葡萄糖苷酶抑制剂。
本发明另一个目的在于将蒲公英甾醇应用于制备α-淀粉酶抑制剂。
本发明还将蒲公英甾醇应用于制备治疗糖尿病的药物。
蒲公英甾醇(taraxasterol)，其结构如式(I)所示，是蒲公英提取物中的一个组分，经过体外试验证实，蒲公英甾醇(taraxasterol)，对于α-葡萄糖苷酶和α-淀粉酶有抑制作用。以阿卡波糖为对照，其抑制效果是阿卡波糖的5～60倍。
式(I)
将蒲公英甾醇应用于制备治疗糖尿病的药物，可以单独使用，也可以与其他成分组合成复方，用于制备降低餐后血糖、防治糖尿病的各种制剂。
所述的药物还包括药学上可接受的载体，剂型包括片剂、颗粒剂、胶囊、软胶囊、滴丸、口服液、注射剂等。
所述的药物中，蒲公英甾醇的含量为5％～100％。
经体外实验证明蒲公英甾醇对α-葡萄糖苷酶和α-淀粉酶活性有很强的抑制作用，为开发成降低餐后血糖，防治糖尿病及其病发症提供科学依据。而且蒲公英甾醇在植物中存在范围广，如蒲公英和旋覆花等中药中含量较高，来源广泛，易得，性质比较稳定。既安全又经济，极具推广应用价值，有望开发成防治糖尿病及其并发症的新药。
具体实施方式
试剂：阿卡波糖对照品购自上海史瑞可生物有限公司；蒲公英甾醇对照品由上海药物研究所提供；蒲公英甾醇样品参照文献(上海药物研究所.中草药有效成分提取与分离，上海科技出版社，1983，382)方法提取制备所得。
α-葡萄糖苷酶(α-Glueosidase，Type I：From Bakers Yeast)、α-淀粉酶(α-Amylase，Type VI-B：From Porcine pancreas，PPA)、4-硝基苯酚-α-D-吡喃葡萄糖苷(4-Nitropheny-α-D-glucopyranoside，PNPG)和淀粉天青(Starch Azure：Potato starch covalently linked with RemazolBriliant Blue R)均购自Sigma；其余试剂均为分析纯。
仪器：HWS26型电热恒温水浴锅；PHS-25酸度计；Anke TGL一16C离心机，上海申生科技；上海棱光S54PC紫外可见分光光度计
实施例1α-葡萄糖苷酶抑制剂活性测定
参照文献(中药材，2005，28(1)：38)的方法，以4-硝基苯酚-α-D-吡喃葡萄糖苷(PNPG)为底物。
反应体系为：2mL 0.1mol·L-1的磷酸盐缓冲液(pH 6.8)中加入待测样品葛根素溶液100μL(DMSO溶解，剂量见表1)，还原谷胱甘肽50μL(1mg·mL-1)，α-葡萄糖苷酶100μL(0.57U·mL-1)，摇匀后37℃温浴10分钟；然后加入37℃温浴好的底物PNPG 0.2mL(20mmol·L-1)37℃水浴反应15min后，加入0.1mol·L-1Na2CO3溶液10mL终止反应，在波长400nm处测定吸光度。阳性对照物为阿卡波糖，结果见表1。
α-葡萄糖苷酶抑制剂活性计算公式如下：
式中：
A空白：不加样品反应后的吸收值
A样品：加入样品反应后的吸收值
A背景：只加样品的吸收值
实施例2α-淀粉酶抑制剂活性测定
参照文献(Biosci.Biotechnol.Biochem.2000，64(5)：1041)方法，反应体系为：淀粉天青5mg用0.5mL的0.05mol·L-1pH 6.9Tris-HCl缓冲液(含CaCl20.01mol·L-1)配制成悬液，于90-95℃水浴加热5min，再于37℃水浴置5min后，加0.5mL待测样品蒲公英甾醇液(用DMSO溶解，剂量见表1)，加0.25mL的PPA(α-淀粉酶)溶液(2.3U·mL-1)，37℃水浴反应10min，加入1.25mL50％冰醋酸终止反应，混匀，4℃条件下6000r·min-1离心5min，595nm处测定吸光度。
阳性对照物为阿卡波糖(0.2mg·mL-1)，结果见表1。α-淀粉酶抑制剂活性计算公式如下：
式中：
Ac+：100％酶活性的吸收值(仅溶剂中加酶)
Ac-：0％酶活性的吸收值(仅溶剂未加酶)
As：待测样品的吸收值(待测样品加酶)
Ab：空白的吸收值(待测样品未加酶)
上述实施例1和2的酶抑制活性测定实验中，每个样品重复三次实验，取其平均值，以平均值计算酶活性抑制率，结果如表1。
表1蒲公英甾醇对α-葡萄糖苷酶和α-淀粉酶活性的抑制作用
实施例3
取蒲公英甾醇1kg，加入1kg淀粉，0.1kg微晶纤维素，硬脂酸镁0.01kg，滑石粉0.02kg，置混合机中混合均匀，分装胶囊。
实施例4
取琼脂55g溶于适量的蒸馏水中，加热使溶，加入200g甘油在搅拌下混匀，最后滴加尼泊金乙酯乙醇溶液100ml(50g·L-1)；另称取过80目筛的蒲公英甾醇粉10g，置研钵中，分次加入上述琼脂溶液，随加研磨，适当时间后，置搅拌机中高速搅拌至颗粒均匀细腻为止，加蒸馏水至10L，121℃灭菌20分钟，即得口服液。
实施例5
取蒲公英甾醇1kg，加入1kg淀粉、微晶纤维素0.2kg、羧甲基淀粉钠0.05kg，置混合机中混合均匀，用70％乙醇水溶液湿法制粒，70℃干燥，整粒，加硬脂酸镁0.01kg，滑石粉0.02kg，混匀，压片。
Claims (6)
1.蒲公英甾醇在制备α-葡萄糖苷酶抑制剂方面的应用。
2.蒲公英甾醇在制备α-淀粉酶抑制剂方面的应用。
3.蒲公英甾醇在制备治疗糖尿病药物方面的应用。
4.一种治疗糖尿病的药物，其特征在于，包括重量含量为5％～100％的蒲公英甾醇。
5.权利要求4所述治疗糖尿病的药物，其特征在于，还包括药学上可接受的载体。
6.权利要求4所述治疗糖尿病的药物，其特征在于，剂型为片剂、颗粒剂、胶囊、软胶囊、滴丸、口服液或注射剂。
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Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN103110100A (zh) * | 2013-02-05 | 2013-05-22 | 郭建鹏 | 一种朝医保健食品组合物及其制备方法和用途 |
| CN104208070A (zh) * | 2014-08-27 | 2014-12-17 | 浙江大学 | 蒲公英甾醇在制备抗hbv的药物中的应用 |
| CN105920024A (zh) * | 2016-04-27 | 2016-09-07 | 荆燕 | 一种含有阿卡波糖治疗糖尿病合并高血压的复方制剂及其制备方法 |
| CN110038015A (zh) * | 2019-05-21 | 2019-07-23 | 枣庄学院 | 蒲公英甾醇在制备治疗尼古丁中毒的药物中的应用 |
| CN110804083A (zh) * | 2019-11-30 | 2020-02-18 | 江苏省中医药研究院 | 醋栗叶醇的制备方法及其作为降糖药物的用途 |
| CN117919256A (zh) * | 2024-03-25 | 2024-04-26 | 潍坊众邦制药有限公司 | 一种含有药用甾醇活性物质组合物在制备治疗肝炎的用途 |
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| CN1747726A (zh) * | 2003-01-29 | 2006-03-15 | 艾克斯塞敦—艾克斯塞摩有限公司 | 一种用于治疗hiv－1和hiv－2的治疗性组合物 |
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| CN1747726A (zh) * | 2003-01-29 | 2006-03-15 | 艾克斯塞敦—艾克斯塞摩有限公司 | 一种用于治疗hiv－1和hiv－2的治疗性组合物 |
Non-Patent Citations (2)
| Title |
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| 《Biological Pharmaceutical Bulletin》 19991231 TAKASAKI M et al. Anti-carcinogenic activity of Taraxacum plant II. 第606－610页 4－5 第22卷, 第6期 2 * |
| 《中国优秀硕士论文电子期刊网》 20080501 詹勤 《大花紫薇叶降血糖活性成分研究蒲公英甾醇乙酸酯》 第11页-23页 权利要求1-3 , 2 * |
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| CN103110100A (zh) * | 2013-02-05 | 2013-05-22 | 郭建鹏 | 一种朝医保健食品组合物及其制备方法和用途 |
| CN104208070A (zh) * | 2014-08-27 | 2014-12-17 | 浙江大学 | 蒲公英甾醇在制备抗hbv的药物中的应用 |
| CN104208070B (zh) * | 2014-08-27 | 2016-08-24 | 浙江大学 | 蒲公英甾醇在制备抗hbv的药物中的应用 |
| CN105920024A (zh) * | 2016-04-27 | 2016-09-07 | 荆燕 | 一种含有阿卡波糖治疗糖尿病合并高血压的复方制剂及其制备方法 |
| CN110038015A (zh) * | 2019-05-21 | 2019-07-23 | 枣庄学院 | 蒲公英甾醇在制备治疗尼古丁中毒的药物中的应用 |
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| CN117919256B (zh) * | 2024-03-25 | 2024-05-24 | 潍坊众邦制药有限公司 | 一种含有药用甾醇活性物质组合物在制备治疗肝炎的用途 |
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