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Related Concept Videos

Oral Hypoglycemic Agents: Sulfonylureas01:17

Oral Hypoglycemic Agents: Sulfonylureas

Sulfonylureas are oral hypoglycemic agents utilized in treating type 2 diabetes. They are characterized by their unique sulfonylurea chemical structure. The family of sulfonylureas is divided into generations. First-generation sulfonylureas, including tolbutamide (Orinase), chlorpropamide (Diabinese), and tolazamide (Tolinase), trigger insulin release from pancreatic β cells and enhance peripheral tissues' insulin sensitivity. The second-generation members, such as glipizide (Glucotrol),...
Oral Hypoglycemic Agents: Biguanides and Glitazones01:26

Oral Hypoglycemic Agents: Biguanides and Glitazones

Biguanides, particularly metformin (Glucophage), are insulin sensitizers that enhance glucose uptake, thereby reducing insulin resistance. Unlike sulfonylureas, metformin doesn't prompt insulin secretion, which helps to curb hypoglycemia risk. Metformin is beneficial in treating conditions like polycystic ovary syndrome due to its insulin-resistance reduction capability. The drug's primary action involves curtailing hepatic gluconeogenesis, a significant contributor to high blood glucose levels...
Oral Hypoglycemic Agents: Glinides01:06

Oral Hypoglycemic Agents: Glinides

Repaglinide (Prandin) and Nateglinide (Starlix), known as glinides, are oral insulin secretagogues that stimulate insulin release from pancreatic β cells by closing the ATP-sensitive potassium channels (KATP channel). Repaglinide controls insulin release from pancreatic β cells by managing potassium efflux. It shares two binding sites with sulfonylureas and also has a unique site, indicating overlapping mechanisms of action. With a rapid onset and a 4-7 hour duration, it effectively manages...
Oral Hypoglycemic Agents: α-Glucosidase Inhibitors01:19

Oral Hypoglycemic Agents: α-Glucosidase Inhibitors

α-glucosidase inhibitors, including acarbose (Precose), miglitol (Glyset), and voglibose (Voglib) (primarily available in Asia), are drugs that control blood sugar levels by delaying the digestion of starch and disaccharides. They achieve this by inhibiting α-glucosidase enzymes in the intestine, which slow the absorption of carbohydrates in the intestine, which in turn leads to a prolonged release of the glucoregulatory hormone GLP-1 from intestinal L-cells.
Acarbose and miglitol are typically...
Glucagon-like Receptor Agonists01:24

Glucagon-like Receptor Agonists

Incretins include glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), which stimulate insulin secretion post-meals. In type 2 diabetes, GIP's efficacy is reduced, making GLP-1 a viable drug target. GIP originates from preproGIP.
GLP-1, when administered in high doses intravenously, triggers insulin secretion, inhibits glucagon release, slows gastric emptying, reduces food intake, and restores normal insulin secretion. However, its rapid inactivation by the...
Dipeptidyl Peptidase 4 Inhibitors01:23

Dipeptidyl Peptidase 4 Inhibitors

Dipeptidyl peptidase 4 (DPP-4) is a serine protease widely distributed in the body. It's involved in the inactivation of GLP-1 and GIP hormones, which are crucial for insulin regulation. DPP-4 inhibitors, such as sitagliptin (Januvia), saxagliptin (Onglyza), linagliptin (Tradjenta), alogliptin (Nesina), and vildagliptin (Galvus), help increase the proportion of active GLP-1, enhancing insulin secretion. These inhibitors work by competitively binding to DPP-4. This binding causes a significant...

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Updated: Jul 27, 2026

Synthesis of Indoxyl-glycosides for Detection of Glycosidase Activities
09:10

Synthesis of Indoxyl-glycosides for Detection of Glycosidase Activities

Published on: May 27, 2015

Alkylglycidic acids: potential new hypoglycemic agents.

W Ho, G F Tutwiler, S C Cottrell

    Journal of Medicinal Chemistry
    |November 1, 1986
    PubMed
    Summary

    Novel alkylglycidic acid derivatives effectively inhibit fatty acid oxidation and lower blood sugar in rats. The lead compound, methyl 2-tetradecylglycidate, shows potent hypoglycemic effects by inhibiting carnitine palmitoyltransferase-A.

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    An In Ovo Model for Testing Insulin-mimetic Compounds
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    Synthesis of Indoxyl-glycosides for Detection of Glycosidase Activities
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    Published on: May 27, 2015

    Sustained Administration of β-cell Mitogens to Intact Mouse Islets Ex Vivo Using Biodegradable Poly(lactic-co-glycolic acid) Microspheres
    09:31

    Sustained Administration of β-cell Mitogens to Intact Mouse Islets Ex Vivo Using Biodegradable Poly(lactic-co-glycolic acid) Microspheres

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    An In Ovo Model for Testing Insulin-mimetic Compounds
    06:09

    An In Ovo Model for Testing Insulin-mimetic Compounds

    Published on: April 23, 2018

    Area of Science:

    • Biochemistry
    • Pharmacology
    • Organic Chemistry

    Background:

    • Long-chain fatty acid oxidation is crucial for energy metabolism.
    • Carnitine acyl transferase enzymes facilitate fatty acid transport into mitochondria for beta-oxidation.
    • Dysregulation of fatty acid metabolism is implicated in conditions like hyperglycemia.

    Purpose of the Study:

    • To synthesize and evaluate alkylglycidic acid analogues for inhibiting fatty acid oxidation.
    • To assess the hypoglycemic potential of these compounds in vivo.
    • To elucidate structure-activity relationships for potent inhibition.

    Main Methods:

    • Synthesis of alkylglycidic acid analogues.
    • In vitro inhibition assays of [1-14C]palmitic acid oxidation in rat hemidiaphragm.
    • Determination of carnitine acyl transferase inhibition.
    • In vivo glucose tolerance tests in rats.

    Main Results:

    • 2-alkyl (C12-C16) glycidates demonstrated potent inhibition of fatty acid oxidation.
    • Methyl 2-tetradecylglycidate emerged as a lead compound with significant hypoglycemic activity.
    • Activity was dependent on the alkyl chain length and the integrity of the oxirane ring.

    Conclusions:

    • Alkylglycidic acid derivatives, particularly methyl 2-tetradecylglycidate, are effective inhibitors of fatty acid oxidation.
    • These compounds act by irreversibly inhibiting mitochondrial carnitine palmitoyltransferase-A.
    • The findings suggest potential therapeutic applications for managing metabolic disorders related to fatty acid oxidation.