Molecular Insight and Mode of Inhibition of α‐Glucosidase and α‐Amylase by Pahangensin A from Alpinia pahangensis<scp>Ridl.</scp>

Loo, Kong Yong; Leong, Kok Hoong; Sivasothy, Yasodha; Ibrahim, Halijah; Awang, Khalijah

doi:10.1002/cbdv.201900032

Cited by 15 publications

(5 citation statements)

References 21 publications

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“…Carbohydrate metabolism requires α-glucosidase and α-amylase enzymes secreted in the small intestine to hydrolyse glycoside bonds from complex carbohydrate foods at different points to produce α-glucose as the product. Uncontrolled activities of these enzymes increase postprandial glucose that leads to an imbalance between glucose absorption in the bloodstream and insulin secretion for glucose uptake [21]. Inhibition of activities of α-glucosidase and α-amylase enzymes have been reported to reduce the risk of obesity, kidney failure and cardiovascular diseases during Type-2 diabetic (T2D) management [11].…”

Section: Introductionmentioning

confidence: 99%

The potential of chalcone-capped gold nanoparticles for the management of diabetes mellitus

Akinfenwa

Pearce

Omoruyi

et al. 2021

Surfaces and Interfaces

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Searching for new natural bioactive capping agents represent an urgent priority in the green synthesis of metal nanoparticles. Additionaly, the biosaftey of metal nanparticles is a major concern especially in medical applications. Recently, the use of pharmacollogicaly active natural products as capping agents has been deployed to avoid toxic effects during the nanoparticles preparation and to enhance their drugability compared with convential drugs. Helichrysum foetidum is a South African medicinal plant used in folk medicine for the treatment of different human pathologies, and it is known to contain a variety of bioactive compounds. Herein, the total extract and two pure chalcones, helichrysetin and helichrysin, isolated from the same plant were successfully used to synthesize quasi-monodispersed gold nanoparticles in the size range of 2-12 nm. The bio-evaluation of samples indicated that the AuNP/capping agent conjugates are biostable, and have different biological profiles from the total extract/pure compounds. The enzymatic inhibition assays showed significant inhibition by the total extract, helichrysetin and their gold nanoparticles. Interestingly, a similar activity was observed for glucose uptake in HEK293 treated cells. On the other hand, all the tested samples relatively demonstrated no cytotoxicity when tested against the HaCaT keratinocytes. In conclusion, the study demonstrated potential enhancement of glucose uptake in mammalian kidney cells, and inhibition of carbohydrate-hydrolysing enzymes by green synthesized gold nanoparticles of H. foetidum. It also provides a therapeutic appraisal of AuNPs/chalcones conjugate towards the development of antidiabetes drugs derived from H. foetidum and its gold nanoparticles.

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Section: Introductionmentioning

confidence: 99%

The potential of chalcone-capped gold nanoparticles for the management of diabetes mellitus

Akinfenwa

Pearce

Omoruyi

et al. 2021

Surfaces and Interfaces

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“…As illustrated in the Lineweaver–Burk plot analyses ( Figure 3 ), compounds 1 and 2 both displayed mixed-mode inhibition against BChE as indicated by their data lines, which either intersected in the first (for compound 1 ) or second (for compound 2 ) quadrants. This type of inhibitor is able to bind to the active site of the enzyme, as well as at different sites of the enzyme (allosteric site) due to the allosteric effect [ 40 , 41 ]. The inhibition constants, K i , were derived from the secondary plots for compounds 1 (0.67 µM) and 2 (0.05 µM), implying that compound 2 has a 13-fold higher affinity to BChE compared to compound 1 .…”

Section: Resultsmentioning

confidence: 99%

N-Methyl Costaricine and Costaricine, Two Potent Butyrylcholinesterase Inhibitors from Alseodaphne pendulifolia Gamb.

Hasnan

Sivasothy

Khaw

et al. 2023

IJMS

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Studies have been conducted over the last decade to identify secondary metabolites from plants, in particular those from the class of alkaloids, for the development of new anti-Alzheimer’s disease (AD) drugs. The genus Alseodaphne, comprising a wide range of alkaloids, is a promising source for the discovery of new cholinesterase inhibitors, the first-line treatment for AD. With regard to this, a phytochemical investigation of the dichloromethane extract of the bark of A. pendulifolia Gamb. was conducted. Repeated column chromatography and preparative thin-layer chromatography led to the isolation of a new bisbenzylisoquinoline alkaloid, N-methyl costaricine (1), together with costaricine (2), hernagine (3), N-methyl hernagine (4), corydine (5), and oxohernagine (6). Their structures were elucidated by the 1D- and 2D-NMR techniques and LCMS-IT-TOF analysis. Compounds 1 and 2 were more-potent BChE inhibitors than galantamine with IC50 values of 3.51 ± 0.80 µM and 2.90 ± 0.56 µM, respectively. The Lineweaver–Burk plots of compounds 1 and 2 indicated they were mixed-mode inhibitors. Compounds 1 and 2 have the potential to be employed as lead compounds for the development of new drugs or medicinal supplements to treat AD.

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“…Furthermore, compounds (-)-3-O-galloylepicatechin and (-)-3-O-galloylcatechin bind in the active site of isomaltase with a strong binding energy value of -9.5 and -10.0 Kcal/mol respectively compared to standard drug acarbose -8.4 Kcal/mol. [93] The lower the binding free energy of any protein-ligand complex, the higher is the stability. [94] Additionally, these compounds also have significant ADMET parameters (Table 8 and 9).…”

Section: Discussionmentioning

confidence: 99%

Phytochemical Analysis, Antidiabetic Potential and in-silico Evaluation of Some Medicinal Plants

Sapkota¹,

Khadayat²,

Adhikari³

et al. 2021

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Background:The increasing frequency of diabetes patients and the reported side effects of commercially available anti-hyperglycemic drugs have gathered the attention of researchers towards the search for new therapeutic approaches. Inhibition of activities of carbohydrate hydrolyzing enzymes is one of the approaches to reduce postprandial hyperglycemia by delaying digestion and absorption of carbohydrates. Objectives: The objective of the study was to investigate phytochemicals, antioxidants, digestive enzymes inhibitory effect, and molecular docking of potent extract. Materials and Methods: In this study, we carry out the substratebased α-glucosidase and α-amylase inhibitory activity of Asparagus racemosus, Bergenia ciliata, Calotropis gigantea, Mimosa pudica, Phyllanthus emblica, and Solanum nigrum along with the determination of total phenolic and flavonoids contents. Likewise, the antioxidant activity was evaluated by measuring the scavenging of DPPH radical. Additionally, antibacterial activity was also studied by Agar well diffusion method. Molecular docking of bioactive compounds from B. ciliata was performed via AutoDock vina. Results: B. ciliata, M. pudica, and P. emblica exhibit significant inhibitory activity against the α-glucosidase and α-amylase with IC 50 (µg/ml) of (2.24 ± 0.01, 46.19 ± 1.06), (35.73 ± 0.65, 99.93 ± 0.9) and (8.12 ± 0.29, no significant activity) respectively indicating a good source for isolating a potential drug candidate for diabetes. These plant extracts also showed significant antioxidant activity with the IC 50 ranges from 13.2 to 26.5 µg/mL along with the significant antibacterial activity towards Staphylococcus aureus and Klebsiella pneumonia. Conclusion: Bergenia extract appeared to be a potent α-glucosidase and α-amylase inhibitor. Further research should be carried out to characterize inhibitor compounds.

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Molecular Insight and Mode of Inhibition of α‐Glucosidase and α‐Amylase by Pahangensin A from Alpinia pahangensisRidl.

Cited by 15 publications

References 21 publications

The potential of chalcone-capped gold nanoparticles for the management of diabetes mellitus

The potential of chalcone-capped gold nanoparticles for the management of diabetes mellitus

N-Methyl Costaricine and Costaricine, Two Potent Butyrylcholinesterase Inhibitors from Alseodaphne pendulifolia Gamb.

Phytochemical Analysis, Antidiabetic Potential and in-silico Evaluation of Some Medicinal Plants

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