Synthesis of some novel orsellinates and lecanoric acid related depsides as <i>α</i>-glucosidase inhibitors

Krishna, Boddu Rama; Sistla, Ramakrishna; Sangaraju, Rajendra; Kuncha, Madhusudana; Mallavadhani, Uppuluri Venkata

doi:10.1080/10286020.2018.1490274

Cited by 9 publications

(3 citation statements)

References 19 publications

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“…All exhibited IC 50 values in the range of 10.7 to 17.6 µM, which was more potent than the positive control (acarbose) (IC 50 449 µM). Depsidone, a unique class of lichen metabolites possess a wide variety of biological activities [19][20][21][22][23]. Up to now, over 22 lichen extracts, (i.e., from Parmotrema grayana or P. hababianum), have been studied for α-glucosidase inhibition or in vivo antihyperglycemic activity [19,24].…”

Section: Resultsmentioning

confidence: 99%

α-Glucosidase Inhibitory Depsidones from the Lichen Parmotrema tsavoense

et al. 2020

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Chemical investigation of the lichen Parmotrema tsavoense led to the isolation of 5 new depsidones, parmosidones F – J (1 – 5). These compounds were structurally elucidated using spectroscopic methods including HRESIMS and 2D NMR data. Compounds 1, 3, and 4 were evaluated for their inhibition of α-glucosidase. All exhibited potent α-glucosidase inhibitory activity with IC50 values ranging from 10.7 to 17.6 µM, which was much lower than that of the positive control acarbose (IC50 449 µM).

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Section: Resultsmentioning

confidence: 99%

α-Glucosidase Inhibitory Depsidones from the Lichen Parmotrema tsavoense

et al. 2020

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“…Finally, in vitro studies revealed that lecanoric acid exhibited effective α-glucosidase inhibitory activity (85.9% of inhibition) with an IC 50 value of 350 µM [ 98 ] and moderate protein tyrosine phosphatase 1B (PTP1B) inhibitory activity (IC 50 31 μM) [ 99 ].…”

Section: Pharmacological Activity Of Lichen Depsides and Tridepsidesmentioning

confidence: 99%

Lichen Depsides and Tridepsides: Progress in Pharmacological Approaches

Hernández-Martín

González-Burgos

Divakar

et al. 2023

JoF

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Depsides and tridepsides are secondary metabolites found in lichens. In the last 10 years, there has been a growing interest in the pharmacological activity of these compounds. This review aims to discuss the research findings related to the biological effects and mechanisms of action of lichen depsides and tridepsides. The most studied compound is atranorin, followed by gyrophoric acid, diffractaic acid, and lecanoric acid. Antioxidant, cytotoxic, and antimicrobial activities are among the most investigated activities, mainly in in vitro studies, with occasional in silico and in vivo studies. Clinical trials have not been conducted using depsides and tridepsides. Therefore, future research should focus on conducting more in vivo work and clinical trials, as well as on evaluating the other activities. Moreover, despite the significant increase in research work on the pharmacology of depsides and tridepsides, there are many of these compounds which have yet to be investigated (e.g., hiascic acid, lassalic acid, ovoic acid, crustinic acid, and hypothamnolic acid).

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“…α-Glucosidase is an indispensable enzyme in the sugar metabolism pathway of organisms, and its main function is to hydrolyze glycosidic bonds into glucose ( Chaudhry et al, 2019 ; Dan et al, 2019 ; Gollapalli et al, 2019 ; Krishna et al, 2019 ; Mendieta-Moctezuma et al, 2019 ; Spasov et al, 2019 ; Ye et al, 2019 ). Thus inhibiting the α-glucosidase would obviously control the postprandial hyperglycemia.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Biological Evaluation of 5-Fluoro-2-Oxindole Derivatives as Potential α-Glucosidase Inhibitors

Lin

Liang

et al. 2022

Front. Chem.

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α-Glucosidase inhibitors are known to prevent the digestion of carbohydrates and reduce the impact of carbohydrates on blood glucose. To develop novel α-glucosidase inhibitors, a series of 5-fluoro-2-oxindole derivatives (3a ∼ 3v) were synthesized, and their α-glucosidase inhibitory activities were investigated. Biological assessment results showed that most synthesized compounds presented potential inhibition on α-glucosidase. Among them, compounds 3d, 3f, and 3i exhibited much better inhibitory activity with IC50 values of 49.89 ± 1.16 μM, 35.83 ± 0.98 μM, and 56.87 ± 0.42 μM, respectively, which were about 10 ∼ 15 folds higher than acarbose (IC50 = 569.43 ± 43.72 μM). A kinetic mechanism study revealed that compounds 3d, 3f, and 3i inhibited the α-glucosidase in a reversible and mixed manner. Molecular docking was carried out to simulate the affinity between the compound and α-glucosidase.

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Synthesis of some novel orsellinates and lecanoric acid related depsides as α-glucosidase inhibitors

Cited by 9 publications

References 19 publications

α-Glucosidase Inhibitory Depsidones from the Lichen Parmotrema tsavoense

α-Glucosidase Inhibitory Depsidones from the Lichen Parmotrema tsavoense

Lichen Depsides and Tridepsides: Progress in Pharmacological Approaches

Synthesis and Biological Evaluation of 5-Fluoro-2-Oxindole Derivatives as Potential α-Glucosidase Inhibitors

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