Commonly used endocrine drugs

Rosa, Mário Miguel; Dias, Teresa

doi:10.1016/b978-0-7020-4087-0.00054-1

Cited by 17 publications

(14 citation statements)

References 42 publications

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“…In support to these findings, Zhang and colleagues showed that AR deficiency drives microglia/macrophages toward an anti‐inflammatory after spinal cord injury in mice and treatment with the AR inhibitor Fidarestat induces c‐AMP response element binding protein (CREB) phosphorylation to increase Arg1 expression in cultured microglia (Figure ); (Q. Zhang et al, ). Importantly some AR inhibitors have gone through Phase‐3 clinical studies (Pandey, Srivastava, & Ramana, ) and Tolrestat has been approved to prevent diabetic complications (Rosa & Dias, ). Finally, regulation of sirtuins (SIRTs) may represent another strategy to promote protective microglial phenotype through metabolic remodeling.…”

Section: Metabolic Drugs and Molecular Pathways Which May Be Exploitementioning

confidence: 99%

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How to reprogram microglia toward beneficial functions

Fumagalli

Lombardi

Gressèns

et al. 2018

Glia

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Microglia, brain cells of nonneural origin, orchestrate the inflammatory response to diverse insults, including hypoxia/ischemia or maternal/fetal infection in the perinatal brain. Experimental studies have demonstrated the capacity of microglia to recognize pathogens or damaged cells activating a cytotoxic response that can exacerbate brain damage. However, microglia display an enormous plasticity in their responses to injury and may also promote resolution stages of inflammation and tissue regeneration. Despite the critical role of microglia in brain pathologies, the cellular mechanisms that govern the diverse phenotypes of microglia are just beginning to be defined. Here we review emerging strategies to drive microglia toward beneficial functions, selectively reporting the studies which provide insights into molecular mechanisms underlying the phenotypic switch. A variety of approaches have been proposed which rely on microglia treatment with pharmacological agents, cytokines, lipid messengers, or microRNAs, as well on nutritional approaches or therapies with immunomodulatory cells. Analysis of the molecular mechanisms relevant for microglia reprogramming toward pro-regenerative functions points to a central role of energy metabolism in shaping microglial functions. Manipulation of metabolic pathways may thus provide new therapeutic opportunities to prevent the deleterious effects of inflammatory microglia and to control excessive inflammation in brain disorders.

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Section: Metabolic Drugs and Molecular Pathways Which May Be Exploitementioning

confidence: 99%

“…Importantly some AR inhibitors have gone through Phase-3 clinical studies (Pandey, Srivastava, & Ramana, 2012) and Tolrestat has been approved to prevent diabetic complications (Rosa & Dias, 2014).…”

Section: Mir200b Reduces Inos Expression and No Production And Limitsmentioning

confidence: 99%

How to reprogram microglia toward beneficial functions

Fumagalli

Lombardi

Gressèns

et al. 2018

Glia

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“…The main downside of α-glucosidase inhibitors is abdominal discomfort due to its mechanism in preventing the degradation of polysaccharides into monosaccharides. The undigested polysaccaharides are digested by bacteria in the colon, thus inducing bloating and diarrhea [18].This study was aimed to isolate major terpenoid compounds from non-laccate Ganoderma. In vitro and in silico assays were conducted to understand the inhibition profile of this compound against DPP-4 and α-glucosidase enzyme.…”

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confidence: 99%

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confidence: 99%

An Integrated In Silico and In Vitro Assays of Dipeptidyl Peptidase-4 and α-Glucosidase Inhibition by Stellasterol from Ganoderma australe

et al. 2019

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Background: Ganoderma fungus is rich in terpenoids. These compounds are known for their anti-hyperglycemic activities. However, the study of terpenoids as the secondary metabolite from Ganoderma as a dipeptidyl peptidase-4 (DPP-4) inhibitor remains unexplored. In addition, we examined the α-glucosidase inhibition activity. Objective: This study aimed to isolate the major terpenoid from non-laccate Ganoderma and examined its inhibitor activity on DPP-4 and α-glucosidase enzymes, and its interaction. Methods: The compound was isolated using column chromatography from Ganoderma australe. The structure of the isolated compound was confirmed by 1H and 13C nuclear magnetic resonance spectroscopy, while the inhibitory activity was evaluated using an enzymatic assay. The interaction of the isolated compound with DPP-4 and α-glucosidase enzymes was investigated using an in silico study. Results: The isolated compound was identified as stellasterol; IC50 values for DPP-4 and α-glucosidase inhibitor were 427.39 µM and 314.54 µM, respectively. This study revealed that the inhibitory effect of stellasterol on DPP-4 enzyme is through hydrophobic interaction, while the α-glucosidase enzyme is due to the interaction with six amino acids of the enzyme. Conclusion: Stellasterol is the major component of the steroid from G. australe. Enzyme inhibitory assay and in silico study suggest that stellasterol may contribute antidiabetic activity with a mechanism closer to acarbose rather than to sitagliptin.

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“…Continuous endeavors with industrial support have encouraged the research and development of sulfa drugs to introduce different and wide range of applications. {Ballagi-Pordány, #4}Carbutamide, glibenclamide, gliquidone, glyclopyramide, and glimepiride are chemically classified as sulfonylurea and used as antidiabetic drugs [5][6][7][8]. Many other pharmacological activities of sulfonamides have been recently reported that include antiinflammatory, endothelin receptor, and 5-HT6 receptor antagonism [9,10].…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Antimicrobial, and Docking Investigations of Remarkably Modified Sulfathiazole Derivatives

et al. 2020

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S OME new sulfathiazole derivatives were synthesized. The sulfathiazole starting material was reacted with ethyl bromoacetate and gave unpredictably an ester product 2. The substitution occurred selectively at the tautomeric proton of the NH thiazolyl nitrogen rather than the aromatic NH 2 protons. The ester was further hydrazinolysed followed by condensation with several aldehydes to establish hydrazones (4a-h). Hantzesch thiazole synthesis was also applied to build antimicrobial agents containing multi-thiazole moieties. The structures of the synthesized compounds were confirmed by 1 H, 13 C, 2D 1 H NMR, MS, and microanalyses. The synthesized compounds were tested for their antimicrobial activity towards Gram-positive and Gram-negative bacteria, and fungi strains. Some of the investigated compounds showed prominent high potency. The docking study revealed the mode of action between the modified sulfathiazole ligands and the binding site of DHPS.

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Commonly used endocrine drugs

Cited by 17 publications

References 42 publications

How to reprogram microglia toward beneficial functions

How to reprogram microglia toward beneficial functions

An Integrated In Silico and In Vitro Assays of Dipeptidyl Peptidase-4 and α-Glucosidase Inhibition by Stellasterol from Ganoderma australe

Synthesis, Antimicrobial, and Docking Investigations of Remarkably Modified Sulfathiazole Derivatives

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