A Study on the Inhibitory Potential of Dpp-Iv Enzyme by Lobeline through In silico and In vivo Approaches
Ghalia Sabbagh, Boushra Kurdi, Warid Khayata, Raghda Lahdo
International Research Journal of Pure and Applied Chemistry · pp. 79–91 · Published 13 Mar 2021
10.9734/irjpac/2021/v22i130376Abstract
Aims: To evaluate the inhibitory activity of Lobeline natural alkaloid against dipeptidyl peptidase IV (DPP IV) enzyme by in silico and in vivo experiments. Study Design: Evaluation of Antidiabetic Activity of Lobeline alkaloid. Place and Duration of Study: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Aleppo University, Aleppo, Syria, between March 2020 and December 2020. Methodology: in silico study was carried out using iGEM docking software to predict the binding affinity of lobeline with DPP IV enzyme in comparison with the reference synthetic compound Sitagliptin. Then in vivo experiment was performed on HFD/alloxan induced diabetic mice to evaluate the anti hyperglycemic effect of lobeline. After treatment duration of 21 days, FBG and the inhibitory effect on DPP IV enzyme activity were measured. Results: Lobeline bound efficiently to the active site of DPP IV enzyme and consumed less binding energy than Sitagliptin. This finding was confirmed by the in vivo study. Administration of lobe line at a dose of 25 mg/kg in HFD/alloxan induced diabetic mice produced a significant reduction in blood glucose level and in DPP IV activity compared to the diabetic control group (P value> .01). Conclusion: Lobe line could be a good candidate to be developed as a natural compound for treating diabetes mellitus.
References (23)
- 1 Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings 1PII of original article: S0169-409X(96)00423-1. The article was originally published in Advanced Drug Delivery Reviews 23 (1997) 3–25. 1 [DOI]
- 2 Molecular Properties That Influence the Oral Bioavailability of Drug Candidates [DOI]
- 3 Dipeptidyl-Peptidase IV from Bench to Bedside: An Update on Structural Properties, Functions, and Clinical Aspects of the Enzyme DPP IV [DOI]
- 4 GIP and GLP‐1, the two incretin hormones: Similarities and differences [DOI]
- 5 iGEMDOCK: a graphical environment of enhancing GEMDOCK using pharmacological interactions and post-screening analysis [DOI]
- 6 Natural medicines from plant source used for therapy of diabetes mellitus: An overview of its pharmacological aspects [DOI]
- 7 Computer-aided drug design and virtual screening of targeted combinatorial libraries of mixed-ligand transition metal complexes of 2-butanone thiosemicarbazone [DOI]
- 8 Vincristine and Vinblastine Anticancer Catharanthus Alkaloids: Pharmacological Applications and Strategies for Yield Improvement [DOI]
- 9 Possible Mechanisms of Morphine Analgesia [DOI]
- 10 Targeting Incretins in Type 2 Diabetes: Role of GLP-1 Receptor Agonists and DPP-4 Inhibitors [DOI]
- 11 Review of sitagliptin phosphate: a novel treatment for type 2 diabetes [DOI]
- 12 Method comparison of dipeptidyl peptidase IV activity assays and their application in biological samples containing reversible inhibitors [DOI]
- 13 Antihyperglycemic activity with DPP-IV inhibition of alkaloids from seed extract of Castanospermum australe: Investigation by experimental validation and molecular docking [DOI]
- 14 Dipeptidyl Peptidase- IV Inhibitory Activity of Berberis aristata
- 15 Glucagon-Like Peptide-1 Receptor Agonists for Diabetes Mellitus [DOI]
- 16 Experimental Models on Diabetes: A Comprehensive Review [DOI]
- 17 Primary Virtual and in vitro Bioassay Screening of Natural Inhibitors from Flavonoids against COX-2 [DOI]
- 18 Indole Alkaloids as New Leads for the Design and Development of Novel DPP-IV Inhibitors for the Treatment of Diabetes [DOI]
- 19 Molecular Docking Study of Certain Plant Alkaloid Derivatives as Inhibitors of Various Drug Targets of Alzheimer’s Disease [DOI]
- 20 AN IN SILICO STUDY OF NOVEL FLUOROQUINOLONES AS INHIBITORS OF DNA GYRASE OF STAPHYLOCOCCUS AUREUS
- 21 Insilico Design of a Ligand for Dpp IV in Type II Diabetes
- 22 Chemical constituents in leaves of Morus atropurpurea and their α-glucosidase activity
- 23 THE MODE OF ACTION OF CERTAIN DRUGS WHICH STIMULATE RESPIRATION [DOI]
Cited by 8
Léa Fleury, Barbara Deracinois, Camille Dugardin · International Journal of Molecular Sciences · 2022
Showing 1 of 8 known citations — external sources report more than can currently be individually listed.
Related research
- Novel Biomarkers for Early Detection and Metabolic Profiling in Diabetes and Prediabetes — shares topic coverage
- Association of Proteobacteria and Bacteriodetes with Obese Related Type-2 Diabetes Mellitus — shares topic coverage
- Echocardiographic Changes in Controlled Type 2 Diabetes Mellitus with Reference to Body Mass Index and Waist Hip Ratio — shares topic coverage
- Asymptomatic Cardiovascular Disorders in a Cohort of Clinically Stable Type 2 Diabetes Mellitus Patients in South Eastern Nigeria: A Cross Sectional Study — shares topic coverage
- Phytochemical and Antibacterial Investigation of Leaf Extracts of Vernonia amygdalina — shares topic coverage
Article metrics
Real usage data collected on this platform.
7
Page views
0
PDF downloads
5
Outbound clicks
8
Citations
Views over time
Views by country
Approximate, from request IP at view time — not citizenship or institution. Countries with fewer than 5 views are grouped as "Other".
Traffic sources
Referring site, by host.
Views and downloads exclude known bots/crawlers. Citations combines this platform's own DOI-resolved index with each external source's own reported total — see Cited by above for individually listed citing works. Last refreshed 0 seconds ago.