Natural products from plants targeting key enzymes for the future development of antidiabetic agents

Mata, Rachel; Flores‐Bocanegra, Laura; Ovalle-Magallanes, Berenice; Figueroa, Mario

doi:10.1039/d3np00007a

Cited by 15 publications

(4 citation statements)

References 249 publications

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“…Likewise, α-amylase and α-glucosidase are the most important enzymes for the hydrolysis of carbohydrates. In this context, their inhibition can regulate blood sugar levels in diabetics following a high-carbohydrate diet [37]. As another example, tyrosinase is a key enzyme in the synthesis of melanin, which protects against harmful rays from the sun.…”

Section: Enzymes Inhibition Propertiesmentioning

confidence: 99%

Evaluating Phytochemical Profiles, Cytotoxicity, Antiviral Activity, Antioxidant Potential, and Enzyme Inhibition of Vepris boiviniana Extracts

Bakar,

Nilofar,

Mohamed

et al. 2023

Molecules

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In the present study, we performed comprehensive LC-MS chemical profiling and biological tests of Vepris boiviniana leaves and stem bark extracts of different polarities. In total, 60 bioactive compounds were tentatively identified in all extracts. The 80% ethanolic stem bark extract exhibited the highest activity in the ABTS assay, equal to 551.82 mg TE/g. The infusion extract of stem bark consistently demonstrated elevated antioxidant activity in all assays, with values ranging from 137.39 mg TE/g to 218.46 mg TE/g. Regarding the enzyme inhibitory assay, aqueous extracts from both bark and leaves exhibited substantial inhibition of AChE, with EC50 values of 2.41 mg GALAE/g and 2.25 mg GALAE/g, respectively. The 80% ethanolic leaf extract exhibited the lowest cytotoxicity in VERO cells (CC50: 613.27 µg/mL) and demonstrated selective cytotoxicity against cancer cells, particularly against H1HeLa cells, indicating potential therapeutic specificity. The 80% ethanolic bark extract exhibited elevated toxicity in VERO cells but had reduced anticancer selectivity. The n-hexane extracts, notably the leaves’ n-hexane extract, displayed the highest toxicity towards non-cancerous cells with selectivity towards H1HeLa and RKO cells. In viral load assessment, all extracts reduced HHV-1 load by 0.14–0.54 log and HRV-14 viral load by 0.13–0.72 log, indicating limited antiviral activity. In conclusion, our research underscores the diverse bioactive properties of Vepris boiviniana extracts, exhibiting potent antioxidant, enzyme inhibitory, and cytotoxicity potential against cancer cells.

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Section: Enzymes Inhibition Propertiesmentioning

confidence: 99%

Evaluating Phytochemical Profiles, Cytotoxicity, Antiviral Activity, Antioxidant Potential, and Enzyme Inhibition of Vepris boiviniana Extracts

Bakar,

Nilofar,

Mohamed

et al. 2023

Molecules

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“…These inhibitors may be categorized as orthosteric or allosteric based on their binding location, both of which result in the intended pharmacological outcome. Focusing on enzymes in drug development offers a notable benefit due to the simple nature of the needed assays, which consist of biochemical tests evaluating enzyme function [21][22][23][24][25]. In our In silico study, it shows that, the GPAT gene has an affinity value of -6.4, which is higher than -4.5, and an RMSD value of 0.000.…”

Section: Resultsmentioning

confidence: 98%

Determining the Role of Caffeic Acid on Lipogenic Regulators: An In-Silico Approach

Fathima A,

Renu,

Vishnu Priya

et al. 2024

TIJPH

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In this study we have used a computational method to investigate how caffeic acid affects important regulators in lipid metabolism, such as the DGAT, GPAT, and PAP genes. Studying how natural substances interact with important regulatory genes is key to understanding lipid metabolism, especially in the setting of metabolic diseases such as diabetes and obesity. We used molecular docking to find out how strongly caffeic acid binds to lipogenic regulators and how these regulators interact with each other. The findings indicate that caffeic acid can directly affect DGAT, GPAT, and PAP. We used predictive models to assess how caffeic acid-binding may influence enzyme activity, gene expression, and signalling pathways related to lipid metabolism. Our computer results give us important information about how caffeic acid might affect lipid metabolism (DGAT, GPAT, and PAP), but it is very important to stress that these interactions and their importance in the body need to be confirmed in experiments. In conclusion, because cellular and metabolic processes are so complicated, it is important to do both in vitro and in vivo studies to fully understand how caffeic acid affects lipid balance and how it might be used to treat metabolic diseases. This study establishes the foundation for the next research, highlighting the capacity of natural chemicals to impact crucial regulators of lipid metabolism.

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“…With the rapid development of medicinal and natural product chemistry, the diversity and complexity of organic molecules are increasing [ 1 , 2 , 3 , 4 , 5 , 6 ]. Therefore, developing efficient organic synthesis strategies to cope with this situation is very necessary.…”

Section: Introductionmentioning

confidence: 99%

Recent Advances in the Domino Annulation Reaction of Quinone Imines

Wang,

Fu,

et al. 2024

Molecules

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Quinone imines are important derivatives of quinones with a wide range of applications in organic synthesis and the pharmaceutical industry. The attack of nucleophilic reagents on quinone imines tends to lead to aromatization of the quinone skeleton, resulting in both the high reactivity and the unique reactivity of quinone imines. The extreme value of quinone imines in the construction of nitrogen- or oxygen-containing heterocycles has attracted widespread attention, and remarkable advances have been reported recently. This review provides an overview of the application of quinone imines in the synthesis of cyclic compounds via the domino annulation reaction.

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Natural products from plants targeting key enzymes for the future development of antidiabetic agents

Abstract: This review summarizes plant metabolites targeting crucial enzymes involved in glucose homeostasis useful for antidiabetic drug development.

Cited by 15 publications

References 249 publications

Evaluating Phytochemical Profiles, Cytotoxicity, Antiviral Activity, Antioxidant Potential, and Enzyme Inhibition of Vepris boiviniana Extracts

Evaluating Phytochemical Profiles, Cytotoxicity, Antiviral Activity, Antioxidant Potential, and Enzyme Inhibition of Vepris boiviniana Extracts

Determining the Role of Caffeic Acid on Lipogenic Regulators: An In-Silico Approach

Recent Advances in the Domino Annulation Reaction of Quinone Imines

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