جستجوی مقالات مرتبط با کلیدواژه "linagliptin" در نشریات گروه "پزشکی"

The current study aimed to compare the renal effects of Empagliflozin with Linagliptin combined with Metformin in patients with type 2 diabetes mellitus (T2DM) and chronic kidney disease.

We conducted a randomized clinical trial on diabetic patients aged over 18 years with chronic renal failure and an EGFR between 20 to 60 ml/minutes/1.73 m2 corrected with the MDRD equation. Between January and December 2023, a total of 150 cases in Imam Hossein Hospital were randomized into two study arms of 75 cases receiving Empagliflozin (10 mg/day) and metformin or Linagliptin (5mg/day) and metformin for 6 months. The primary outcome was a change in chronic kidney disease (CKD) stage, while serum creatinine, fasting blood sugar (FBS), proteinuria, and blood pressure were evaluated at baseline, 3 and 6 months later.

The mean age of participants was 62.20 (± 4.45) years and 50% of them were females. Study indices including serum creatinine (P: 0.001), estimated glomerular filtration rate (eGFR) (P: 0.001), FBS (P: 0.001), HgA1c (P: 0.001), proteinuria (P: 0.001), and blood pressure (P: 0.001) reduced significantly over time in both groups. After adjustment for potential confounders, Empagliflozin reduced the level of serum creatinine independent of other factors.

Empagliflozin significantly reduces the level of serum creatinine compared to Linagliptin in patients with T2DM and chronic renal failure.

Previous studies have suggested that linagliptin may represent renoprotective effects besides its anti-hyperglycemic properties in patients with type 2 diabetes. However, there is a lack of decisive evidence to support this assumption. This study aimed to address the effect of linagliptin in type 2 diabetic patients with severely increased albuminuria.

In this randomized double-blind, placebo-controlled clinical trial, type 2 diabetic patients with severely increased albuminuria (albuminuria ≥ 300 mg/24 h) were enrolled. Patients were randomized to linagliptin (5 mg/d) and placebo based on a computer-generated list of random numbers. Biochemical (fasting blood sugar (FBS) (mg/dL), hemoglobin A1c (HbA1c) (%), proteinuria (mg/24h), blood urea nitrogen (BUN) (mg/dL), serum creatinine (mg/dL)) and clinical variables (weight (kg), systolic, and diastolic blood pressure (mmHg)) were measured at baseline and 3 and 6 months post intervention.

At baseline, no statistically significant difference was detected in demographic characteristics between the two groups (P > .05). A significant decrease was observed in proteinuria, FBS, weight, SBP, and DBP in the intervention group after 6 months (Ptime < .05), however; none of the clinical and biochemical variables showed a significant difference between groups after 6 months (Pgroup > .05).

Linagliptin may serve as a renoprotective therapeutic option in diabetic patients with severely increased albuminuria due to its role in proteinuria reduction. Results of this study can be used for future large-scale, long-term studies investigating the renoprotective effects of linagliptin in patients with diabetic nephropathy.

Alzheimer’s disease is one of the neurodegenerative disorders typified by the aggregate of amyloid-β (Aβ) and phosphorylated tau protein. Oxidative stress and neuroinflammation, because of Aβ peptides, are strongly involved in the pathophysiology of Alzheimer’s disease (AD). Linagliptin shows neuroprotective properties against AD pathological processes through alleviation of neural inflammation and AMPK activation.

We assessed the benefits of linagliptin pretreatment (at 10, 20, and 50 nM concentrations), against Aβ1-42 toxicity (20 μM) in SH-SY5Y cells. The concentrations of secreted cytokines, such as TNF-α, IL-6, and IL-1β, and signaling proteins, including pCREB, Wnt1, and PKCε, were quantified by ELISA.

We observed that Aβ led to cellular inflammation, which was assessed by measuring inflammatory cytokines (TNF-α, IL-1β, and IL-6). Moreover, Aβ1-42 treatment impaired pCREB, PKCε, and Wnt1 signaling in human SH-SY5Y neuroblastoma cells. Addition of Linagliptin significantly reduced IL-6 levels in the lysates of cells, treated with Aβ1-42. Furthermore, linagliptin prevented the downregulation of Wnt1 in Aβ1-42-treated cells exposed.

The current findings reveal that linagliptin alleviates Aβ1-42-induced inflammation in SH-SY5Y cells, probably through the suppression of IL-6 release, and some of its benefits are mediated through the activation of the Wnt1 signaling pathway.

A simple, rapid, and ultra sensitive dispersive solid phase extraction based on nano graphene oxide was developed for simultaneous measurement of trace amounts of metformin (MET) and linagliptin (LIN) in plasma samples by HPLC-UV-Vis. Affecting factors on the extraction of these drugs, including adsorbent weight, extraction time, organic solvent type, desorption situations, and composition of solvent were examined and optimized. In optimum conditions, the LOD (limit of detection) and LOQ (limit of quantification) of the suggested technique were 2.0 ngmL-1 and 6.1 (ngmL-1) for LIN and 3.0 ngmL-1 and 9.2 ngmL-1 for MET, respectively. Suitable linear behavior in the considered ranges of concentration (10-2000 ngmL-1) and good correlation coefficient of 0.9901 and 0.9903 (r2) for LIN and MET were obtained, respectively. The RSD (relative standard deviations) according to three replicate measurements at 2, 20, 200 ngmL-1 levels of these drugs was less than 8.0%. In the last step, applicability of the suggested technique was examined by analyzing the drugs in plasma samples and reasonable results were achieved.

In temporal lobe epilepsy (TLE), recurrent seizures accompany with cognitive deficit. In some patients, the current medications cannot provide satisfactory control of seizures, therefore new drugs that act through different mechanisms are required. In the present study, the useful effect of dipeptidyl peptidase-4 inhibitor was evaluated in experimental model of temporal lobe epilepsy in male rats.
In this study, the effects of administration of dipeptidyl peptidase-4 inhibitor, linagliptin, on seizures score according to Racine’s scores and learning and memory impairment induced by intrahippocampal injection of kainic acid (4 g) using Y-maze and passive avoidance test were studied in rats. Linagliptin thirty minutes before kainic acid injection was administrated intracerebroventricularly.
In this study, the kainic acid-induced recurrent seizures, reduced alternation level in Y-maze test (p The obtained data indicate that linagliptin in kainate rats mitigates seizure severity and develops short-term memory.

Druggability of a target protein depends on the interacting micro-environment between the target protein and drugs. Therefore, a precise knowledge of the interacting micro-environment between the target protein and drugs is requisite for drug discovery process. To understand such micro-environment, we performed in silico interaction analysis between a human target protein, Dipeptidyl Peptidase-IV (DPP-4), and three anti-diabetic drugs (saxagliptin, linagliptin and vildagliptin).
During the theoretical and bioinformatics analysis of micro-environmental properties, we performed drug-likeness study, protein active site predictions, docking analysis and residual interactions with the protein-drug interface. Micro-environmental landscape properties were evaluated through various parameters such as binding energy, intermolecular energy, electrostatic energy, van der Waals’bond痫⢖ energy (EVHD) and ligand efficiency (LE) using different in silico methods. For this study, we have used several servers and software, such as Molsoft prediction server, CASTp server, AutoDock software and LIGPLOT server.
Through micro-environmental study, highest log P value was observed for linagliptin (1.07). Lowest binding energy was also observed for linagliptin with DPP-4 in the binding plot. We also identified the number of H-bonds and residues involved in the hydrophobic interactions between the DPP-4 and the anti-diabetic drugs. During interaction, two H-bonds and nine residues, two H-bonds and eleven residues as well as four H-bonds and nine residues were found between the saxagliptin, linagliptin as well as vildagliptin cases and DPP-4, respectively.
Our in silico data obtained for drug-target interactions and micro-environmental signature demonstrates linagliptin as the most stable interacting drug among the tested anti-diabetic medicines.