Synthesis and In Vitro AMPK Activation of CycloalkylAlkarylbiguanides with Robust In Vivo Antihyperglycemic Action
المؤلفون المشاركون
Ortega-Cuellar, Daniel
Carvajal, Karla
Estrada-Soto, Samuel
Gutierrez-Lara, Erika
Martínez-Conde, Carlos
Rosales-Ortega, Edgar
Ramírez-Espinosa, Juan José
Rivera-Leyva, Julio C.
Centurión, David
Navarrete-Vázquez, Gabriel
المصدر
العدد
المجلد 2017، العدد 2017 (31 ديسمبر/كانون الأول 2017)، ص ص. 1-8، 8ص.
الناشر
Hindawi Publishing Corporation
تاريخ النشر
2017-11-15
دولة النشر
مصر
عدد الصفحات
8
التخصصات الرئيسية
الملخص EN
This work describes the design, synthesis in one step, and the in vitro, in vivo, and in silico antidiabetic evaluation of a series of ten alicyclic and aromatic (alkyl +aryl: alkaryl)biguanides, analogues of metformin and phenformin.
The design was conceived using isosteric replacement, chain-ring transformation, and lower and higher homologation strategies.
All compounds were obtained as crystals and their structure was confirmed on the basis of their spectral data (NMR and mass spectra), and their purity was ascertained by microanalysis.
Compounds were in vitro evaluated as activators of AMP-Activated Protein Kinase (AMPK).
The results indicated that compounds 4, 5, and 6 showed similar or even better effect compared to metformin.
Docking analysis was performed with regulatory subunit γ of AMPK, showing several interactions with nucleotide binding pocket.
The in vivo evaluation of compounds 4–6 at a single dose of 50 mg/kg was performed in a murine experimental model of diabetes.
The results showed an important and robust decrease of plasmatic glucose levels (−40%).
Compound 6 was selected for an oral glucose tolerance test, showing an antihyperglycemic effect similar to metformin.
The in vivo results indicated that compounds 4–6 may be effective in treating experimental T2DM.
نمط استشهاد جمعية علماء النفس الأمريكية (APA)
Gutierrez-Lara, Erika& Martínez-Conde, Carlos& Rosales-Ortega, Edgar& Ramírez-Espinosa, Juan José& Rivera-Leyva, Julio C.& Centurión, David…[et al.]. 2017. Synthesis and In Vitro AMPK Activation of CycloalkylAlkarylbiguanides with Robust In Vivo Antihyperglycemic Action. Journal of Chemistry،Vol. 2017, no. 2017, pp.1-8.
https://search.emarefa.net/detail/BIM-1171330
نمط استشهاد الجمعية الأمريكية للغات الحديثة (MLA)
Gutierrez-Lara, Erika…[et al.]. Synthesis and In Vitro AMPK Activation of CycloalkylAlkarylbiguanides with Robust In Vivo Antihyperglycemic Action. Journal of Chemistry No. 2017 (2017), pp.1-8.
https://search.emarefa.net/detail/BIM-1171330
نمط استشهاد الجمعية الطبية الأمريكية (AMA)
Gutierrez-Lara, Erika& Martínez-Conde, Carlos& Rosales-Ortega, Edgar& Ramírez-Espinosa, Juan José& Rivera-Leyva, Julio C.& Centurión, David…[et al.]. Synthesis and In Vitro AMPK Activation of CycloalkylAlkarylbiguanides with Robust In Vivo Antihyperglycemic Action. Journal of Chemistry. 2017. Vol. 2017, no. 2017, pp.1-8.
https://search.emarefa.net/detail/BIM-1171330
نوع البيانات
مقالات
لغة النص
الإنجليزية
الملاحظات
Includes bibliographical references
رقم السجل
BIM-1171330
قاعدة معامل التأثير والاستشهادات المرجعية العربي "ارسيف Arcif"
أضخم قاعدة بيانات عربية للاستشهادات المرجعية للمجلات العلمية المحكمة الصادرة في العالم العربي
تقوم هذه الخدمة بالتحقق من التشابه أو الانتحال في الأبحاث والمقالات العلمية والأطروحات الجامعية والكتب والأبحاث باللغة العربية، وتحديد درجة التشابه أو أصالة الأعمال البحثية وحماية ملكيتها الفكرية. تعرف اكثر