更新于：2024-12-09
Miglitol
米格列醇
更新于：2024-12-09
概要
基本信息
药物类型 小分子化药 |
别名 Diastabol、Miglibay、Miglitol (JP17/USAN/INN) + [12] |
作用机制 α-glucosidase抑制剂(酸性α-葡萄糖苷酶抑制剂) |
治疗领域 |
非在研适应症 |
原研机构 |
在研机构 |
最高研发阶段批准上市 |
首次获批日期 荷兰 (1996-07-23), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构
分子式C8H17NO5 |
InChIKeyIBAQFPQHRJAVAV-ULAWRXDQSA-N |
CAS号72432-03-2 |
关联
43
项与 米格列醇 相关的临床试验Miglitol combined with GC chemotherapy regimen to improve the efficacy of locally advanced and advanced bladder cancer
观察持证商为三和化学研究所株式会社的米格列醇片（规格：25 mg，商品名：SEIBULE®）在中国健康受试者中进行的单中心、开放、单序列、空腹、三周期、单次给药设计的药效动力学研究预试验
A single arm multicenter clinical study of miglitol in the treatment of muscle invasive bladder cancer
100 项与 米格列醇 相关的临床结果
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100 项与 米格列醇 相关的转化医学
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100 项与 米格列醇 相关的专利（医药）
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365
项与 米格列醇 相关的文献（医药）2024-12-31Journal of enzyme inhibition and medicinal chemistry
Development of iminosugar-based glycosidase inhibitors as drug candidates for SARS-CoV-2 virus via molecular modelling and in vitro studies
Article
作者: Djurkovic, Filip ; Ferjancic, Zorana ; Trmcic, Milena ; Vulovic, Bojan ; Pavlovic, Milos ; Djurdjevic Djelmas, Aleksandra ; Prodanovic, Radivoje ; Bihelovic, Filip ; Vignuzzi, Marco ; Matovic, Radomir ; Sladic, Dusan ; Kalicanin, Nevena ; Jankovic, Aleksandar ; Vallet, Thomas ; Zlatovic, Mario ; Saicic, Radomir N.
We developed new iminosugar-based glycosidase inhibitors against SARS-CoV-2. Known drugs (miglustat, migalastat, miglitol, and swainsonine) were chosen as lead compounds to develop three classes of glycosidase inhibitors (α-glucosidase, α-galactosidase, and mannosidase). Molecular modelling of the lead compounds, synthesis of the compounds with the highest docking scores, enzyme inhibition tests, and in vitro antiviral assays afforded rationally designed inhibitors. Two highly active α-glucosidase inhibitors were discovered, where one of them is the most potent iminosugar-based anti-SARS-CoV-2 agent to date (EC90 = 1.94 µM in A549-ACE2 cells against Omicron BA.1 strain). However, galactosidase inhibitors did not exhibit antiviral activity, whereas mannosidase inhibitors were both active and cytotoxic. As our iminosugar-based drug candidates act by a host-directed mechanism, they should be more resilient to drug resistance. Moreover, this strategy could be extended to identify potential drug candidates for other viral infections.
2024-12-31JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
New natural protein tyrosine phosphatase 1B inhibitors from
Gynostemma pentaphyllum
Article
作者: Wu, Di ; Qin, Lin ; Wang, Jianmei ; He, Yuqi ; Zhang, Qianru ; Du, Yimei ; Wu, Xingdong ; Tan, Daopeng ; Wang, Xianting ; Xie, Jian ; Deng, Yidan
Type 2 diabetes mellitus (T2DM) is a chronic metabolic disease mainly caused by insulin resistance, which can lead to a series of complications such as cardiovascular disease, retinopathy, and its typical clinical symptom is hyperglycaemia. Glucosidase inhibitors, including Acarbose, Miglitol, are commonly used in the clinical treatment of hypoglycaemia. In addition, Protein tyrosine phosphatase 1B (PTP1B) is also an important promising target for the treatment of T2DM. Gynostemma pentaphyllum is a well-known oriental traditional medicinal herbal plant, and has many beneficial effects on glucose and lipid metabolism. In the present study, three new and nine known dammarane triterpenoids isolated from G. pentaphyllum, and their structures were elucidated by spectroscopic methods including HR-ESI-MS,1H and 13C NMR and X-ray crystallography. All these compounds were evaluated for inhibitory activity against α-glucosidase, α-amylase and PTP1B. The results suggested that compounds 7∼10 were potential antidiabetic agents with significantly inhibition activity against PTP1B in a dose-dependent manner.
2024-11-01Archives of physiology and biochemistry
Exploring plant-based alpha-glucosidase inhibitors: promising contenders for combatting type-2 diabetes
Review
作者: Mishra, Abha ; Kumari, Sonali ; Saini, Ravi ; Bhatnagar, Aditi
OBJECTIVE:
This systematic review aimed to provide comprehensive details on the α-G inhibitory potential of various bioactive compounds derived from natural sources.
METHODS:
A comprehensive literature search was conducted using various databases and search engines, including Science Direct, Google Scholar, SciFinder, Web of Science, and PubMed until May, 2023.
RESULTS AND CONCLUSIONS:
The enzyme alpha-glucosidase (α-G) is found in the brush border epithelium of the small intestine and consists of duplicated glycoside hydrolase (GH31) domain. It involves the conversion of disaccharides and oligosaccharides into monosaccharides by acting on alpha (1 → 4) and (1 → 6) linked glucose residue. Once absorbed, glucose enters the bloodstream and elevates postprandial glucose, which is associated with the development of type 2 Diabetes (T2D). Epidemic obesity, cardiovascular disease, and nephropathy are linked to T2D. Traditional medicinal plants with α-G inhibitory potential are commonly used to treat T2D due to the adverse effects of currently used α-G inhibitors miglitol, acarbose, and voglibose. Various bioactive compounds derived from natural sources, including lupenone, Wilforlide A, Baicalein, Betulinic acid, Ursolic acid, Oleanolic acid, Katononic acid, Carnosol, Hypericin, Astilbin, lupeol, betulonic acid, Fagomine, Lactucaxanthin, Erythritol, GP90-1B, Procyanidins, Galangin, and vomifoliol retain α-G inhibitory potential for regulating hyperglycaemia.
100 项与 米格列醇 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 糖尿病 | 日本 | 2005-10-11 | |
| 2型糖尿病 | 荷兰 | - | 1996-07-23 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 非胰岛素依赖型糖尿病2 | 临床3期 | 日本 | 2006-06-07 | |
| 1型糖尿病 | 临床3期 | 日本 | 2005-09-21 | |
| 肥胖 | 临床2期 | 美国 | - |
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临床结果
临床结果
适应症
分期
评价
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N/A | - | - | 艱膚鑰範範窪鑰壓觸願(憲醖觸鏇齋製鏇糧選夢) = 夢積壓構鹹齋鑰觸蓋壓 淵網醖鹽齋繭築觸憲選 (窪構願簾遞膚餘網鹹淵 ) 更多 | - | 2020-06-01 | ||
艱膚鑰範範窪鑰壓觸願(憲醖觸鏇齋製鏇糧選夢) = 壓簾糧觸憲繭廠選積繭 淵網醖鹽齋繭築觸憲選 (窪構願簾遞膚餘網鹹淵 ) 更多 | |||||||
N/A | 41 | 膚鑰觸鏇憲膚餘艱築蓋(繭構憲鹽顧醖簾壓艱夢) = 膚蓋襯構窪艱夢遞壓廠 醖醖糧觸膚顧鬱襯夢夢 (艱觸築鬱簾衊遞顧積餘, 0.11) 更多 | 积极 | 2013-09-24 | |||
Sitagliptin | 膚鑰觸鏇憲膚餘艱築蓋(繭構憲鹽顧醖簾壓艱夢) = 積襯繭構選蓋艱繭構壓 醖醖糧觸膚顧鬱襯夢夢 (艱觸築鬱簾衊遞顧積餘, 0.17) 更多 |
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