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Diabetes Mellitus/Anti-DM Pharmacological Management
Published in Mihai V. Putz, New Frontiers in Nanochemistry, 2020
Bogdan Bumbăcilă, Corina Duda-Seiman, Daniel Duda-Seiman, Mihai V. Putz
There are two naturally occurring incretin hormones that have a role in the maintenance of glycemic control: glucose-dependent insulinotropic polypeptide (GIP) and GLP-1, both of which have a short half-life because of their rapid inactivation by dipeptidyl peptidase-4 enzymes. In patients with type 2 diabetes, the incretin effect is reduced or, in some cases, absent. In particular, the insulinotropic action of GIP is lost in patients with type 2 diabetes. However, it has been shown that, after administration of pharmacological levels of GLP-1, the insulin secretory function can be restored in this population and thus GLP-1 has become an important target for research into new therapies for type 2 diabetes (Garber, 2011).
Toxicological and pharmacokinetic properties of sucralose-6-acetate and its parent sucralose: in vitro screening assays
Published in Journal of Toxicology and Environmental Health, Part B, 2023
Susan S. Schiffman, Elizabeth H. Scholl, Terrence S. Furey, H. Troy Nagle
Consumption of sucralose was noted to alter glucose and/or insulin concentrations in the plasma of some human subjects when delivered in liquids or capsules (Lertrit et al. 2018; Méndez-García et al. 2022; Pepino et al. 2013; Romo-Romo et al. 2018; Schiffman and Rother 2013; Suez et al. 2022) and when accompanied by carbohydrate (Dalenberg et al. 2020) or another non-caloric sweetener (Young et al. 2017). Maternal ingestion of sucralose during pregnancy impacted the progeny’s metabolism including downregulation of hepatic detoxification mechanisms and changes in bacterial metabolites (Olivier-Van Stichelen, Rother, and Hanover 2019). Additional studies reported that sucralose might affect incretin hormones including glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) as well as the sodium-dependent glucose co‑transporter‑1 (SGLT‑1) (Kreuch et al. 2018; Lertrit et al. 2018; Margolskee et al. 2007; Sun et al. 2017; Young et al. 2017). Further, sucralose was demonstrated to blunt thyroid function (Pałkowska-Goździk, Bigos, and Rosołowska-Huszcz 2018). Chronic sucralose ingestion at levels that have regulatory approval in the United States and Europe also modify the fecal metabolome (Bian et al. 2017), liver proteome (Liu et al. 2019), and induce the expression of two intestinal proteins involved in first-pass metabolism, specifically P-glycoprotein (P-gp) and cytochrome P450 (CYP3A4) (Abou-Donia et al. 2008).
A dipyrrole derivative from Aloe vera inhibits an anti-diabetic drug target Dipeptidyl Peptidase (DPP)-IV in vitro
Published in Preparative Biochemistry & Biotechnology, 2020
C. Prasannaraja, A. S. Kamalanathan, M. A. Vijayalakshmi, Krishnan Venkataraman
Understanding the mechanism of pancreatic rejuvenation has increased considerably upon discovery of incretins such as glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), which helps in maintaining glucose homeostasis (i.e., incretin effect) with increased β-cell mass and function.[5] GLP-1, is a glucose-dependent insulinotropic gut hormone, secreted by the intestinal L-cells that stimulate insulin secretion.[6] However, it is rapidly degraded by the ubiquitous proteolytic enzyme DPP-IV. Patients with type 2 diabetes have increased DPP-IV enzyme activity[7] and thus, inhibition of DPP-IV, the enzyme that makes GLP-1 biologically inactive, enhances the incretin effect and is considered as one of the targets for the treatment of T2DM.[8] Oral administration of synthetic DPP-IV inhibitors to type 2 diabetic patients effectively reduced glycated hemoglobin levels.[9] The synthetic DPP-IV inhibitors currently in use have very few side effects, however, the durability and long-term safety needs to be established.[10] Several food derived peptides and small molecules have been characterized for their anti-diabetic activity[11,12] and many of them have been identified and found to act as promising DPP-IV inhibitors, potentially contributing to glycemic control.[13–16]
Absorption, metabolism, and excretion of [14C]evogliptin tartrate in male rats and dogs
Published in Journal of Toxicology and Environmental Health, Part A, 2018
Dae Young Lee, Ju-Hyun Kim, Hyun Joo Shim, Hyeon-Uk Jeong, Hye Suk Lee
Evogliptin (Figure 1; trade name: Sugarnon®) selectively and potently reduces blood glucose levels by inhibiting dipeptidyl peptidase IV, a ubiquitous enzyme that rapidly degrades glucagon-like peptide 1 and glucose-dependent insulinotropic polypeptide (Cahn, Cernea, and Raz 2016; Chae et al. 2015; Cho et al. 2011; Deacon and Lebovitz 2016; Kim et al. 2017, 2012, 2016, 2011; Lee et al. 2017; Park et al. 2017; Tan and Hu 2016). Evogliptin is administered as a monotherapeutic, oral antihyperglycemic drug, or employed in combination with other antidiabetic agents to treat type II diabetes mellitus, a chronic metabolic disorder associated with insulin deficiency and insulin resistance (Hong et al. 2017; Rhee et al. 2016a, 2016b; Tan and Hu 2016; Yoon et al. 2017).