title: Hypoglycemic activity of curcumin synthetic analogues in alloxan-induced diabetic rats.
abstract: The currently available therapies for type 2 diabetes have been unable to achieve normoglycemic status in the majority of patients. The reason may be attributed to the limitations of the drug itself or its side effects. In an effort to develop potent and safe oral antidiabetic agents, we evaluated the in vitro and in vivo hypoglycemic effects of 10 synthetic polyphenolic curcumin analogues on alloxan-induced male diabetic albino rats. In vitro studies showed 7-bis(3,4-dimethoxyphenyl)hepta-1,6-diene-3,5-dione (4) to be the most potential hypoglycemic agent followed by 1,5-bis(4-hydroxy-3-methoxyphenyl)penta-1,4-dien-3-one (10). Structure activity relationship (SAR) of the tested compounds was elucidated and the results were interpreted in terms of in vitro hypoglycemic activities. Furthermore, oral glucose tolerance test (OGTT) with compounds 4, 10 and reference hypoglycemic drug glipizide showed that compound 4 and glipizide had relatively similar effects on the reduction of blood glucose levels within 2 h. Thus, compound 4 might be regarded as a potential hypoglycemic agent being able to reduce glucose concentration both in vitro and in vivo.
authors: a Department of Physiology, Shri. B.M. Patil Medical College , BLDE University , Bijapur , Karnataka , India .
authors: Kusal K
authors: KK
authors: Das
authors: b Department of Medicinal Chemistry .|c Drugs and Advanced Sciences Research Center, School of Pharmacy , Ardabil University of Medical Sciences , Ardabil , Iran .
authors: Nima
authors: N
authors: Razzaghi-Asl
authors: d Department of Physiology , Al Ameen Medical College , Bijapur , Karnataka , India .
authors: Swati N
authors: SN
authors: Tikare
authors: e Dipartimento di Chimica e Tecnologie del Farmaco, Istituto Pasteur-Fondazione Cenci Bolognetti , Sapienza University of Rome , Rome , Italy , and.
authors: Roberto
authors: R
authors: Di Santo
authors: e Dipartimento di Chimica e Tecnologie del Farmaco, Istituto Pasteur-Fondazione Cenci Bolognetti , Sapienza University of Rome , Rome , Italy , and.
authors: Roberta
authors: R
authors: Costi
authors: e Dipartimento di Chimica e Tecnologie del Farmaco, Istituto Pasteur-Fondazione Cenci Bolognetti , Sapienza University of Rome , Rome , Italy , and.
authors: Antonella
authors: A
authors: Messore
authors: e Dipartimento di Chimica e Tecnologie del Farmaco, Istituto Pasteur-Fondazione Cenci Bolognetti , Sapienza University of Rome , Rome , Italy , and.
authors: Luca
authors: L
authors: Pescatori
authors: e Dipartimento di Chimica e Tecnologie del Farmaco, Istituto Pasteur-Fondazione Cenci Bolognetti , Sapienza University of Rome , Rome , Italy , and.
authors: Giuliana Cuzzucoli
authors: GC
authors: Crucitti
authors: d Department of Physiology , Al Ameen Medical College , Bijapur , Karnataka , India .
authors: Jameel G
authors: JG
authors: Jargar
authors: d Department of Physiology , Al Ameen Medical College , Bijapur , Karnataka , India .
authors: Salim A
authors: SA
authors: Dhundasi
authors: f Department of Physiology and Pharmacology "Vittorio Erspamer" , Sapienza University of Rome , Rome , Italy.
authors: Luciano
authors: L
authors: Saso
mesh_terms: D000284:Administration, Oral; D000496:Alloxan; D000818:Animals; D001786:Blood Glucose / Q000187:drug effects* / Q000378:metabolism; D003474:Curcumin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D003921:Diabetes Mellitus, Experimental / Q000139:chemically induced / Q000188:drug therapy*; D004305:Dose-Response Relationship, Drug; D005947:Glucose / Q000008:administration & dosage; D005951:Glucose Tolerance Test; D007004:Hypoglycemic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D008297:Male; D015394:Molecular Structure; D051381:Rats; D017208:Rats, Wistar; D013329:Structure-Activity Relationship
chemical_list: D001786:Blood Glucose; D007004:Hypoglycemic Agents; D000496:Alloxan; D003474:Curcumin; D005947:Glucose
keywords: Curcumin; OGTT; diabetic rats; hypoglycemic; in vitro; synthesis