Kinetics of α -amylase and α -glucosidase inhibitory potential of Zea mays Linnaeus (Poaceae), Stigma maydis aqueous extract: An in vitro assessment

Protein tyrosine phosphatase 1B (PTP1B) is an established therapeutic target for type 2 diabetes mellitus (T2DM) and obesity. The aim of this study was to investigate the inhibitory activity ofMagnolia officinalisextract (ME) on PTP1B and its anti-T2DM effects. Inhibition assays and inhibition kinetics of ME were performedin vitro. 3T3-L1 adipocytes and C2C12 myotubes were stimulated with ME to explore its bioavailability in cell level. Thein vivostudies were performed on db/db mice to probe its anti-T2DM effects. In the present study, ME inhibited PTP1B in a reversible competitive manner and displayed good selectivity against PTPsin vitro. Furthermore, ME enhanced tyrosine phosphorylation levels of cellular proteins, especially the insulin-induced tyrosine phosphorylations of insulin receptorβ-subunit (IRβ) and ERK1/2 in a dose-dependent manner in stimulated 3T3-L1 adipocytes and C2C12 myotubes. Meanwhile, ME enhanced insulin-stimulated GLUT4 translocation. More importantly, there was a significant decrease in fasting plasma glucose level of db/db diabetic mice treated orally with 0.5 g/kg ME for 4 weeks. These findings indicated that improvement of insulin sensitivity and hypoglycemic effects of ME may be attributed to the inhibition of PTP1B. Thereby, we pioneered the inhibitory potential of ME targeted on PTP1B as anti-T2DM drug discovery.

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In vitro assessment of CYP1A2 and 2C9 inhibition potential of Withania somnifera and Centella asiatica in human liver microsomes

Drug Metabolism and Personalized Therapy ◽

10.1515/dmdi-2014-0035 ◽

2015 ◽

Vol 30 (2) ◽

Cited By ~ 3

Author(s):

Jay Savai ◽

Alice Varghese ◽

Nancy Pandita ◽

Meena Chintamaneni

Keyword(s):

Medicinal Plants ◽

Human Liver ◽

Withania Somnifera ◽

Liver Microsomes ◽

Centella Asiatica ◽

Herbal Drugs ◽

In Vitro Assessment ◽

Inhibitory Potential ◽

Effective Use

AbstractSeveral herbal drugs and allopathic medicines when co-administered can lead to severe herb-drug interactions. Hence, this study was undertaken in order to assess theInhibitory potential of crude extracts of both the medicinal plants along with their principal phytoconstituents were investigated using selective probe substrate technique. ICThe results of the study revealed thatThus, these findings of the study might be helpful for safe and effective use of

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Antioxidant and Xanthine Oxidase Inhibitory Potential of Aqueous Extract of Ferula Asafoetida

Journal of Pharmaceutical Research International ◽

10.9734/jpri/2021/v33i57b34042 ◽

2021 ◽

pp. 166-173

Author(s):

G. G. Gopika ◽

R. Gayathri ◽

V. Vishnu Priya ◽

J. Selvaraj ◽

S. Kavitha

Keyword(s):

Antioxidant Activity ◽

Xanthine Oxidase ◽

Aqueous Extract ◽

Dependent Manner ◽

Phytochemical Screening ◽

Standard Drug ◽

Inhibitory Potential ◽

Ferula Asafoetida ◽

In Vitro Antioxidant Activity

Background: Ferula asafoetida is a dried latex that is exuded from rhizome or taproot species. Organosulfides are primarily responsible for flavour and odour of asafoetida.Ferula asafoetida is a natural medicine good for asthma and bronchitis. is also used to relieve stomach gas, digestive issues. It is usually added while cooking to hormonise the sweet, sour, salty, spicy taste of the food. Increased activity of xanthine oxidase is involved in the medical condition known as gout, which is characterized by hyperuricemia that leads to deposition of uric acid in the joints resulting in painful inflammation. Aim: To analyse the anti-oxidant and xanthine oxidase inhibitory potential of aqueous extract of Ferula asafoetida. Materials and Methods: Preparation of the aqueous seed extract of Ferula asafoetida done by hot percolation method. Phytochemical screening, in vitro antioxidant activity and xanthine oxidase inhibitory potential was done by standard procedures. The data were analyzed statistically by a one - way analysis of variance (ANOVA) followed by Duncan’s multiple range test was used to see the statistical significance among the groups. The results with the p<0.05 level were considered to be statistically significant. Results: The phytochemical screening revealed that the extract is rich in phytoconstituents. DPPH radical scavenging activity established the potent in vitro antioxidant activity (p<0.05) of Ferula asafoetida extract. The extract was also efficient in inhibiting the activity of xanthine oxidase enzyme (p<0.05) in a concentration dependent manner. Discussion: The extract has potent antioxidant and xanthine oxidase inhibitory potential, although the activities are less compared to the standard drug. Conclusion: The Ferula asafoetida extract can be used to treat gout and to combat various other disorders associated with xanthine oxidase activity.

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Membrane stabilization and kinetics of carbohydrate metabolizing enzymes ( α -amylase and α -glucosidase) inhibitory potentials of Eucalyptus obliqua L.Her. (Myrtaceae) Blakely ethanolic leaf extract: An in vitro assessment

South African Journal of Botany ◽

10.1016/j.sajb.2016.04.007 ◽

2016 ◽

Vol 105 ◽

pp. 264-269 ◽

Cited By ~ 14

Author(s):

S. Sabiu ◽

A.O.T. Ashafa

Keyword(s):

Leaf Extract ◽

Membrane Stabilization ◽

Metabolizing Enzymes ◽

In Vitro Assessment ◽

Kinetics Of ◽

Ethanolic Leaf Extract

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Effect of pH and inhibitors on beta-amyloid fibril assembly

Proceedings, annual meeting, Electron Microscopy Society of America ◽

10.1017/s0424820100166221 ◽

1996 ◽

Vol 54 ◽

pp. 752-753

Author(s):

Beverly E. Maleeff ◽

Timothy K. Hart ◽

Stephen J. Wood ◽

Ronald Wetzel

Keyword(s):

Amyloid Fibril ◽

Peptide Fragment ◽

Hydrophobic Peptides ◽

Amyloid Fibril Formation ◽

Effects Of Ph ◽

Severity Of The Disease ◽

Kinetics Of ◽

The Brain

Alzheimer's disease is characterized post-mortem in part by abnormal extracellular neuritic plaques found in brain tissue. There appears to be a correlation between the severity of Alzheimer's dementia in vivo and the number of plaques found in particular areas of the brain. These plaques are known to be the deposition sites of fibrils of the protein β-amyloid. It is thought that if the assembly of these plaques could be inhibited, the severity of the disease would be decreased. The peptide fragment Aβ, a precursor of the p-amyloid protein, has a 40 amino acid sequence, and has been shown to be toxic to neuronal cells in culture after an aging process of several days. This toxicity corresponds to the kinetics of in vitro amyloid fibril formation. In this study, we report the biochemical and ultrastructural effects of pH and the inhibitory agent hexadecyl-N-methylpiperidinium (HMP) bromide, one of a class of ionic micellar detergents known to be capable of solubilizing hydrophobic peptides, on the in vitro assembly of the peptide fragment Aβ.

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