Overview of Metformin as a Host Targeted Therapy in Tuberculosis

Priyadharshini, A; Ahalya, Sitaram; Alex, Maria; Mathew, Sunitha Elza

doi:10.5958/0974-360x.2019.00539.0

Cited by 3 publications

(1 citation statement)

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“…The results of the present study showed that PPC80 and PPC82 have inhibitory potential on the activity of pancreatic lipase, which may promote a reduction in intestinal fat absorption and potentially affect body weight [27]. Therefore, PPC80 and PPC82 derivatives are promising therapeutic agents for the treatment of obesity and lipid disorders, since orlistat (an anti-obesity drug) is associated with nephrotoxicity, hepatotoxicity, and gastrointestinal side effects [28].…”

Section: Discussionmentioning

confidence: 95%

Inhibitory Potential of Synthetic Amino Acid Derivatives against Digestive Enzymes as Promising Hypoglycemic and Anti-Obesity Agents

et al. 2023

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Over the last decades, the increased incidence of metabolic disorders, such as type two diabetes and obesity, has motivated researchers to investigate new enzyme inhibitors. In this study, the inhibitory effects of synthetic amino acid derivatives (PPC80, PPC82, PPC84, PPC89, and PPC101) on the activity of digestive enzymes were assessed using in vitro assays. The inhibitory effect was determined by the inhibition percentage and the 50% inhibitory concentration (IC50), and the mechanism of action was investigated using kinetic parameters and Lineweaver–Burk plots. PPC80, PPC82, and PPC84 inhibited pancreatic lipase (IC50 of 167–1023 µM) via competitive or mixed mechanisms. The activity of pancreatic α-amylase was suppressed by PPC80, PPC82, PPC84, PPC89, and PPC101 (IC50 of 162–519 µM), which acted as competitive or mixed inhibitors. Finally, PPC84, PPC89, and PPC101 also showed potent inhibitory effects on α-glucosidase (IC50 of 51–353 µM) as competitive inhibitors. The results suggest that these synthetic amino acid derivatives have inhibitory potential against digestive enzymes and may be used as therapeutic agents to control metabolic disorders.

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Section: Discussionmentioning

confidence: 95%

Inhibitory Potential of Synthetic Amino Acid Derivatives against Digestive Enzymes as Promising Hypoglycemic and Anti-Obesity Agents

et al. 2023

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A Review on Metformin: Clinical Significance and Side Effects

Mazumder

Ashini

2021

RJPT

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Metformin is a biguanide that has been used extensively worldwide for the treatment of type II diabetes mellitus. It improves glycaemic control by enhancing insulin sensitivity in liver and muscle. An advantage of metformin treatment is the tendency of weight reduction and the absence of significant hypoglycaemia; blood glucose levels are reduced only to normal as it does not stimulate insulin secretion. Metformin also has a beneficial effect on several cardiovascular risk factors including dyslipidemia, elevated plasminogen activator inhibitor 1 levels, other fibrinolytic abnormalities, hyperinsulinemia, and insulin resistance. Metformin enhances muscle and adipocyte insulin receptor number and/or affinity, increases insulin receptor tyrosine kinase activity, stimulates glucose transport and glycogen synthesis, and reduces both hepatic gluconeogenesis and glycogenolysis. The disadvantages are confined to the gastro-intestinal side effects and the potential risk of vitamin B 12 and folic acid deficiency during long-term use. These side effects can be minimized by slow titration and consumption with meals. The under lying mechanism for gastrointestinal intolerance are proposed to be stimulation of intestinal secretion of serotonin, alteration in incretin and metabolism of glucose, and malabsorption of bile salts. Lactic acidosis is rare contraindication associated with metformin. Most reported cases of lactic acidosis occur in patients with contraindications, particularly impaired renal function. Metformin has a good safety profile, efficacy and comparatively reduced cost. Its ability to improve insulin sensitivity and the cardiovascular risk profile of type II diabetic patients has enhanced its clinical use as first-line therapy.

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The effect of Metformin and its combinations with other hypoglycemic agents on CRP blood levels

Mansour,

Makhous

2023

RJPT

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Background: C-reactive protein (CRP) is linked to inflammation and elevated cardiovascular risk in metabolic disorders. Metformin has been shown to lower CRP concentrations. However, it is still unclear whether elevated CRP levels could be modulated by metformin. Objective: This study aims to evaluate the effects of metformin and its combinations on CRP levels in T2DM patients. Patients and Methods: a prospective comparative study was carried out at Tishreen University Hospital and some private diabetic clinics in Lattakia, Syria during the period between April 2020 and March 2022.The study included three groups of patients: group I (31 patients, 32.6%) received metformin at a dose of 1,000mg/d, group II (30 patients, 31.6%) received modified release gliclazide (60mg/d) and group III (34 patients, 35.8%) received metformin with sitagliptin (50/1000mg/d). CRP levels were measured at baseline and after 3 months of treatment. Results: a total of 95 patients, 55males (57.90%) and 40 females (42.1%) with a mean age of 50.72±6.6 years were included in the study. There were no significant differences between the three groups regarding age, sex, and BMI (p > 0.05). There was a significant decrease in FPG after treatment with metformin, gliclazide, and metformin with sitagliptin; 21.92%, 18.75%, and 24.39% respectively, p<0.0001. Metformin, gliclazide, and metformin with sitagliptin significantly reduced HbA1c by 18.7%, 17.36%, and 21.92% respectively. There was a significant change in CRP levels from baseline after receiving metformin (2.06±0.8 vs 3.46±0.9, p<0.001), and metformin with sitagliptin (1.84±0.6 vs 3.30±0.7, p:0<0001). However, the reduction in gliclazide group wasn’t significant (2.97±0.6 vs 3.14±1.1, p=0.09). Reduction in CRP levels wasn't influenced by age, sex or BMI, and was independent of glycemic control (p > 0.05). Conclusion: We demonstrated that metformin and its combination with sitagliptin have a favorable beneficial effect on inflammation marker CRP in patients with T2DM.

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Overview of Metformin as a Host Targeted Therapy in Tuberculosis

Cited by 3 publications

References 0 publications

Inhibitory Potential of Synthetic Amino Acid Derivatives against Digestive Enzymes as Promising Hypoglycemic and Anti-Obesity Agents

Inhibitory Potential of Synthetic Amino Acid Derivatives against Digestive Enzymes as Promising Hypoglycemic and Anti-Obesity Agents

A Review on Metformin: Clinical Significance and Side Effects

The effect of Metformin and its combinations with other hypoglycemic agents on CRP blood levels

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