- Characterizing the Effect of Amylase Inhibitors on Maltodextrin Metabolism by Gut Bacteria Using Fluorescent Glycan Labeling. [Journal Article]ACS Chem Biol. 2023 Feb 02 [Online ahead of print]AC
- Diet-derived polysaccharides are an important carbon source for gut bacteria and shape the human gut microbiome. Acarbose, a compound used clinically to treat type 2 diabetes, is known to inhibit the growth of some bacteria on starches based on its activity as an inhibitor of α-glucosidases and α-amylases. In contrast to acarbose, montbretin A, a new drug candidate for the treatment of type 2 dia…
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- Synthesis of new diphenyl urea-clubbed imine analogs and its Implications in diabetic management through in vitro and in silico approaches. [Journal Article]
- Type II diabetes mellitus (T2DM) is a global health issue with high rate of prevalence. The inhibition of α-glucosidase enzyme has prime importance in the management of T2DM. This study was established to synthesize Schiff bases of 1,3-dipheny urea (3a-y) and to investigate their in vitro anti-diabetic capability via inhibiting α-glucosidase, a key player in the catabolism of carbohydrates. The s…
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- Achyranbidens A-C: three new compounds from Achyranthes bidentata Blume. [Journal Article]Nat Prod Res. 2023 Feb 01 [Online ahead of print]NP
- Phytochemical study on the roots of Achyranthes bidentata Blume led to the isolation of sixteen compounds including three new ones (1-3). Their chemical structures were determined as oleanolic acid 28-O-β-D-glucopyranoside-3-O-[β-D-glucopyranosyl-(1→3)-β-D-galactopyranoside) (1), methyl (8Z,11Z)-5,6,7-trihydroxytetradeca-8,11-dienoate (2), methyl (6E,11Z)-5,8,9-trihydroxytetradeca-6,11-dienoate (…
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- Alpha-glucosidase inhibitory activities of astilbin contained in Bauhinia strychnifolia Craib. stems: an investigation by in silico and in vitro studies. [Journal Article]
- CONCLUSIONS: In silico and in vitro studies reveal that astilbin inhibits AG and is superior to acarbose, validating its promise as an AG inhibitor. Overall, astilbin was the most bioactive component of BC for antidiabetic action.
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- Novel hybrids of thiazolidinedione-1,3,4-oxadiazole derivatives: synthesis, molecular docking, MD simulations, ADMET study, in vitro, and in vivo anti-diabetic assessment. [Journal Article]
- As compared to standard medicinal compounds, hybrid molecules that contain multiple biologically active functional groups have greater affinity and efficiency. Hence based on this concept, we predicted that a combination of thiazolidinediones and 1,3,4-oxadiazoles may enhance α-amylase and α-glucosidase inhibition activity. A series of novel 3-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)thiazolidine-2…
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- Two new cycloartane type triterpenes from Dysoxyllum binectariferum. [Journal Article]Nat Prod Res. 2023 Jan 29 [Online ahead of print]NP
- Dysoxyllum binectariferum is an important medicinal plant known for various biological activities like anti-inflammatory, CNS depressants, contraceptive, analgesic, immunomodulatory, antimalarial, antifeedant, leishmanicidal and antiviral. It is a rich source of rohitukine, a basic skeleton of flavopiridol. Phytochemical investigation of chloroform extracts of Dysoxyllum binectariferum leaves, le…
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- Design, synthesis, biological evaluation, and docking study of chromone-based phenylhydrazone and benzoylhydrazone derivatives as antidiabetic agents targeting α-glucosidase. [Journal Article]Bioorg Chem. 2023 Jan 20; 132:106384.BC
- To develop novel α-glucosidase inhibitors, a series of chromone-based phenylhydrazone and benzoylhydrazone derivatives were designed, synthesized, and evaluated their inhibitory effects on α-glucosidase. The target compounds were characterized using 1H NMR, 13C NMR, and high-resolution mass spectra. Some of the compounds showed a varying degree of α-glucosidase inhibitory activity with IC50 value…
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- Yunvjian Improves Glucose and Insulin Function in Diabetic Rats by Regulating Gastric Emptying Function. [Journal Article]
- CONCLUSIONS: Yunvjian can effectively control glucose and improve islet function, which may be closely related to its influence on gastric emptying function and related hormone secretion regulation.
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- Synthesis and evaluation of ent-Conduramine C-1 derivatives as α-glucosidase inhibitors via CSI-mediated amination reaction. [Journal Article]Carbohydr Res. 2023 Jan 18; 524:108746.CR
- Concise synthesis of ent-conduramine C-1 and its derivatives has been achieved by using commercially available d-ribose. The key steps in the synthesis are regioselective and diastereoselective amination of polybenzyl ethers by chlorosulfonyl isocyanate (CSI), chelation-controlled carbonyl addition, and intramolecular olefin metathesis. All of the synthesized compounds were evaluated for inhibito…
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- Synthetic α-glucosidase inhibitors as promising anti-diabetic agents: Recent developments and future challenges. [Review]Eur J Med Chem. 2023 Jan 17; 249:115119.EJ
- Diabetes mellitus is one of the biggest challenges for the scientific community in the 21st century. It is a well-recognized multifactorial health problem contributes significantly to high mortality rates by causing serious health complications mainly related to cardiovascular diseases, kidney damage and neuropathy. The inhibition of α-glucosidase (enzyme that catalyses starch hydrolysis in the i…
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- In Vitro α-Amylase and α-Glucosidase Inhibitory Activity of Green Seaweed Halimeda tuna Extract from the Coast of Lhok Bubon, Aceh. [Journal Article]
- Seaweed belongs to marine biota and contains nutrients and secondary metabolites beneficial for health. This study aimed to determine the antidiabetic activity of extracts and fractions of green seaweed Halimeda tuna. The H. tuna sample was extracted with the maceration method using methanol and then partitioned using ethyl acetate and water to obtain ethyl acetate and water fractions. The methan…
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- Rhanteriol, a New Rhanterium suaveolens Desf. Lignan with Pharmacological Potential as an Inhibitor of Enzymes Involved in Neurodegeneration and Type 2 Diabetes. [Journal Article]
- Several specialized plant metabolites are reported to be enzyme inhibitors. In this investigation, the phytochemical composition and the biological activity of Rhanterium suaveolens Desf. were studied. One new lignan (rhanteriol 1) and seven known secondary metabolites were isolated from the aerial parts of R. suaveolens by using different chromatographic procedures. The biological properties of …
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- Antihyperglycemic Effects of Annona cherimola Miller and the Flavonoid Rutin in Combination with Oral Antidiabetic Drugs on Streptozocin-Induced Diabetic Mice. [Journal Article]
- Ethanolic extract obtained from Annona cherimola Miller (EEAc) and the flavonoid rutin (Rut) were evaluated in this study to determine their antihyperglycemic content, % HbA1c reduction, and antihyperlipidemic activities. Both treatments were evaluated separately and in combination with the oral antidiabetic drugs (OADs) acarbose (Aca), metformin (Met), glibenclamide (Gli), and canagliflozin (Can…
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- Synthesis, In Vitro α-Glucosidase Inhibitory Activity and Molecular Docking Study of New Benzotriazole-Based Bis-Schiff Base Derivatives. [Journal Article]
- This study was carried out to synthesize benzotriazole-based bis-Schiff base scaffolds (1-20) and assess them in vitro for α-glucosidase inhibitory potentials. All the synthetics analogs based on benzotriazole-based bis-Schiff base scaffolds were found to display an outstanding inhibition profile on screening against the α-glucosidase enzyme. The synthetic scaffolds showed a varied range of inhib…
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- Evaluation and molecular modelling of bis-Schiff base derivatives as potential leads for management of diabetes mellitus. [Journal Article]
- Developing a medication to cure and manage diabetes mellitus complications is of interest in medicinal chemistry. Toward this end, six bis-biphenyl-salicylaldehyde Schiff base derivatives have been evaluated for their α-glucosidase inhibition, antiglycation and anti-inflammation potentials. Four compounds (compounds 2-5) showed an excellent α-glucosidase inhibitory effect superior to that produce…
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- Acarbose May Function as a Competitive Exclusion Agent for the Producing Bacteria. [Journal Article]ACS Chem Biol. 2023 Jan 17 [Online ahead of print]AC
- Acarbose is a well-known microbial specialized metabolite used clinically to treat type 2 diabetes. This natural pseudo-oligosaccharide (PsOS) shows potent inhibitory activity toward various glycosyl hydrolases, including α-glucosidases and α-amylases. While acarbose and other PsOSs are produced by many different bacteria, their ecological or biological role in microbial communities is still an o…
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- In vitro α-glucosidase inhibitory activity of isolated compounds and semisynthetic derivative from aerial parts of Erythrina senegalensis DC. [Journal Article]Nat Prod Res. 2023 Jan 17 [Online ahead of print]NP
- The current study was conducted to isolate the phytoconstituents from Erythrina senegalensis leaves and stem bark and evaluate their inhibitory activity against α-glucosidase, digestive enzyme related to diabetes mellitus. Phytochemical investigation of the leaves resulted in the isolation of three saponins (3-5), two triterpenoids (7 and 8) and two steroids (10a and 10b) as inseparable mixture, …
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- Novel ethyl p-methoxy cinnamate rich Kaempferia galanga (L.) essential oil and its pharmacological applications: special emphasis on anticholinesterase, anti-tyrosinase, α-amylase inhibitory, and genotoxic efficiencies. [Journal Article]
- CONCLUSIONS: Current research provides the basis for the fact that besides being a rich source of ethyl p-methoxycinnamate, EMCKG has the potential for future formulation and development of an inexpensive skin-care agent and for the preparation of anti-diabetic drugs.
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- Exogenous c-di-GMP inhibited the biofilm formation of Vibrio splendidus. [Journal Article]Microb Pathog. 2023 Feb; 175:105981.MP
- Vibrio splendidus, a gram-negative bacterium that is ubiquitously present in marine environments, has been increasingly deemed an important opportunistic pathogen of marine animals. In this study, the biofilm formation of V. splendidus was quantitatively determined and morphologically characterized. Three stages of biofilm formation, including adhesion, aggregation and maturation were observed in…
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- Anti-ageing effects of FDA-approved medicines: a focused review. [Review]J Basic Clin Physiol Pharmacol. 2023 Jan 13 [Online ahead of print]JB
- Ageing is the process generated by senescent cells, free radicals, inflammation and other relevant factors. Ageing contributes to age-related diseases that affect the quality of life. People are interested in anti-ageing intervention and many scientists attempt to search for anti-ageing medicines. This review focused on describing in vivo anti-ageing activity of US-FDA-approved drugs and found th…
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- New polychlorinated bibenzyls from Rhododendron minutiflorum. [Journal Article]
- Five new polychlorinated bibenzyls (1-5) along with 3 known compounds (6-8) were isolated from the stems and leaves of Rhododendron minutiflorum. The chemical structures of all the isolates were determined by spectroscopic methods, and compounds 1 and 2 were further verified by single-crystal X-ray diffraction analyses. Compounds 1-5 were halogenated compounds which bear three to five chlorine at…
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- Biosynthesis and Characterization of Silver Nanoparticles from the Extremophile Plant Aeonium haworthii and Their Antioxidant, Antimicrobial and Anti-Diabetic Capacities. [Journal Article]
- The present paper described the first green synthesis of silver nanoparticles (AgNPs) from the extremophile plant Aeonium haworthii. The characterization of the biosynthesized silver nanoparticles was carried out by using UV-Vis, FTIR and STM analysis. The antioxidant, antidiabetic and antimicrobial properties were also reported. The newly described AgNPs were spherical in shape and had a size of…
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- In Vitro Evaluation of α-amylase and α-glucosidase Inhibition of 2,3-Epoxyprocyanidin C1 and Other Constituents from Pterocarpus erinaceus Poir. [Journal Article]
- Diabetes mellitus is a metabolic disorder which is one of the leading causes of mortality and morbidities in elderly humans. Chronic diabetes can lead to kidney failure, blindness, limb amputation, heart attack and stroke. Physical activity, healthy diets and medications can reduce the incidence of diabetes, so the search for more efficient antidiabetic therapies, most especially from natural pro…
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- Bioactive Properties of Instant Chicory Melanoidins and Their Relevance as Health Promoting Food Ingredients. [Journal Article]
- Instant chicory is a caffeine-free brew worldwide consumed as a coffee substitute. Like coffee grounds processing, chicory roots suffer a roasting process, which may lead to the formation of high-molecular weight nitrogen-brown compounds, the melanoidins. It is hypothesized that similarly to coffee, chicory melanoidins have health promoting potential. In this work, the chemical composition and bi…
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- Dual Regulation of Sulfonated Lignin to Prevent and Treat Type 2 Diabetes Mellitus. [Journal Article]Biomacromolecules. 2023 Jan 06 [Online ahead of print]B
- With the rapid increase of diabetes cases in the world, there is an increasing demand for slowing down and managing diabetes and its effects. It is considered that a viable prophylactic treatment for type 2 diabetes mellitus (T2DM) is to reduce carbohydrate digestibility by controlling the activities of α-amylase and α-glucosidase to control postprandial hyperglycemia and promote the growth of in…
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- Taxotrophises A and B, two new polyphenols from the stems of Taxotrophis ilicifolius. [Journal Article]Nat Prod Res. 2023 Jan 06 [Online ahead of print]NP
- From the EtOAc extract of the wood of the stems of Taxotrophis ilicifolius (Moraceae), two new secondary metabolites, named taxotrophises A (1) and B (2), were isolated, together with five known compounds (3-7). Their chemical structures have been elucidated by extensive NMR spectroscopic analysis. All isolated compounds have been evaluated for α-glucosidase inhibitory activity. In the present wo…
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- Comparing and contrasting different herbal products intended for the management of obesity approved in the Palestinian markets. [Journal Article]
- CONCLUSIONS: It can be concluded that the seven products showed varied anti-lipase, anti-amylase, and antioxidant effects. However, products F and G showed superiority in all categories.
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- Hesperetin-Cu(II) complex as potential α-amylase and α-glucosidase inhibitor: Inhibition mechanism and molecular docking. [Journal Article]Spectrochim Acta A Mol Biomol Spectrosc. 2022 Dec 31; 290:122301.SA
- Inhibition of α-amylase and α-glucosidase activity is an effective way for controlling postprandial blood glucose-related diabetes. The study found that hesperetin-Cu(II) complex (Hsp-Cu(II)) exhibited a stronger inhibitory ability on α-amylase and α-glucosidase compared to hesperetin (Hsp), with smaller IC50 values of Hsp-Cu(II) (60.3 ± 0.9 µM for α-amylase; 1.25 ± 0.03 µM for α-glucosidase) tha…
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- Fermented seeds of Pentaclethra macrophylla mitigate against memory deficit and restored altered enzymatic activity in the brain of streptozotocin-diabetic rats. [Journal Article]Metab Brain Dis. 2022 Dec 31 [Online ahead of print]MB
- Memory deficit has been reported as one of the complications of diabetes. Fermented seeds of Pentaclethra Macrophylla (P. macrophylla) have been used in folklore for the management of metabolic diseases. The research aims to evaluate the impact of diets with the inclusion of the fermented seed of P. macrophylla on memory deficit in diabetic rats and its underlying mechanisms. Before the induction…
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- Mechanistic Insight of Synthesized 1,4-Dihydropyridines as an Antidiabetic Sword against Reactive Oxygen Species. [Journal Article]J Med Chem. 2023 Jan 12; 66(1):991-1010.JM
- The pharmacologically privileged DHP derivatives were synthesized using the pragmatic multicomponent Hantzsch synthesis to screen the antidiabetic activity. Initially, the candidates were screened using an in vivo blood glucose test, where compound 8b showed the most prominent antidiabetic effect (% potency = 218%) compared to glimepiride. Then, a propositioned structure-activity relationship stu…
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