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  1. Article ; Online: Momordica charantia nanoparticles potentiate insulin release and modulate antioxidant gene expression in pancreas of diabetic rats

    Olusola Olalekan Elekofehinti

    Egyptian Journal of Medical Human Genetics, Vol 23, Iss 1, Pp 1-

    2022  Volume 10

    Abstract: Abstract Background Green synthesis of nanoparticles with medicinal plants has inherent potential in the management of diabetes mellitus. This study synthesized Momordica charantia nanoparticles using silver nitrate to investigate the antidiabetic ... ...

    Abstract Abstract Background Green synthesis of nanoparticles with medicinal plants has inherent potential in the management of diabetes mellitus. This study synthesized Momordica charantia nanoparticles using silver nitrate to investigate the antidiabetic properties of this extract and the synthesized nanoparticles in vivo. Results The M. charantia nanoparticles used were synthesized biologically under ambient conditions from methanolic leaf extract of M. charantia using 1 mM concentration of aqueous silver nitrate and characterized using spectroscopic methods, FTIR and scanning electron microscopy. In vivo, the antidiabetic activity of M. charantia nanoparticle was assessed in streptozotocin-induced (65 mg/kg) rats. Rats were treated with M. charantia nanoparticle (50 mg/kg), aqueous leaf extract (100 mg/kg) metformin (100 mg/kg) and silver nitrate nanoparticle (10 mg/kg) for 21 days. Following treatment, rats were killed for biochemical analysis. Also, reverse transcript-polymerase chain reaction analyses of Takeda-G-protein-receptor-5, glucagon-like peptide-1, Insulin, superoxide dismutase, catalase and Nuclear factor-erythroid factor 2-related factor 2 (NRF2) - were carried out in the pancreas. A significant reduction in blood sugar levels was noted in rats treated with M. charantia nanoparticles. A reduction (p < 0.05) of pancreas alanine transaminase, aspartate aminotransferase and alkaline phosphatase was observed when compared with diabetic untreated rats. M. charantia nanoparticles significantly increase the antioxidant enzymes in diabetic rats when compared with diabetic untreated rats. The decrease in the level of triglyceride, cholesterol and low-density lipoprotein was observed when compared with diabetic control rats and also a significant increase in the expression of Takeda-G-protein-receptor-5, glucagon-like peptide-1, insulin, superoxide dismutase, catalase and NFE2-related factor 2 genes was observed when compared with diabetic untreated rats. Conclusions Momordica charantia nanoparticles exhibited ...
    Keywords Momordica charantia ; Antidiabetic ; Medicinal plants ; Silver nanoparticles ; Green synthesis ; Medicine (General) ; R5-920 ; Genetics ; QH426-470
    Subject code 500
    Language English
    Publishing date 2022-03-01T00:00:00Z
    Publisher SpringerOpen
    Document type Article ; Online
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  2. Article ; Online: Hepatoprotective Effect of Morin Hydrate in Type 2 Diabetic Wistar Rats Exposed to Diesel Exhaust Particles.

    Folorunso, Ibukun Mary / Lawal, Akeem Olalekan / Elekofehinti, Olusola Olalekan / Iwaloye, Opeyemi

    Applied biochemistry and biotechnology

    2023  Volume 195, Issue 10, Page(s) 5855–5880

    Abstract: Studies have shown that exposure to air pollutants such as diesel exhaust particles (DEP) exacerbate diabetes complications. Morin hydrate (MH), a plant bioflavonoid, provides hepatoprotection due to its diverse pharmacological properties. This study ... ...

    Abstract Studies have shown that exposure to air pollutants such as diesel exhaust particles (DEP) exacerbate diabetes complications. Morin hydrate (MH), a plant bioflavonoid, provides hepatoprotection due to its diverse pharmacological properties. This study examines the hepatoprotective effects of MH in Wistar rats with type 2 diabetes exposed to diesel exhaust (DE). Procured male Wistar rats (n = 60) were separated into 12 groups of five rat each. Type 2 diabetes was induced following oral therapy with fructose solution and one-time injection of 45 mg/kg of streptozotocin (STZ). The DEP extract was administered by nasal instillation, whereas MH was administered via oral gavage. Biochemical assays were used to determine the effect of MH on diabetic rats and DEP-exposed diabetic rats with respect to liver function indices (AST and ALT), liver antioxidants (SOD, CAT, Gpx, and GSH), lipid profile, and oxidative stress marker (conjugated diene and lipid peroxidation). The mRNA expression of PI3K/AKT/GLUT4 and AMPK/GLUT4 signaling pathways were quantified using RT-PCR. The results show that normal rats, diabetic rats, and diabetic rats exposed to DEP exhibited a substantial decrease in oxidative stress indicators, serum lipid profile, and levels of AST and ALP, as well as an increase in liver natural antioxidants following oral administration of MH. The gene expression study demonstrated that MH promotes the activation of the insulin signaling pathways which facilitates the uptake of glucose from the blood. This study suggests that MH offered hepatoprotection in type 2 diabetic rats and DEP exposed diabetic rats.
    MeSH term(s) Rats ; Animals ; Antioxidants/metabolism ; Rats, Wistar ; Vehicle Emissions/toxicity ; Diabetes Mellitus, Experimental/metabolism ; Diabetes Mellitus, Type 2/chemically induced ; Diabetes Mellitus, Type 2/drug therapy ; Phosphatidylinositol 3-Kinases/metabolism ; Oxidative Stress ; Flavonoids/pharmacology ; Flavonoids/therapeutic use ; Lipids/pharmacology
    Chemical Substances Antioxidants ; Vehicle Emissions ; Phosphatidylinositol 3-Kinases (EC 2.7.1.-) ; morin (8NFQ3F76WR) ; Flavonoids ; Lipids
    Language English
    Publishing date 2023-01-28
    Publishing country United States
    Document type Journal Article
    ZDB-ID 392344-7
    ISSN 1559-0291 ; 0273-2289
    ISSN (online) 1559-0291
    ISSN 0273-2289
    DOI 10.1007/s12010-023-04366-4
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  3. Article ; Online: Momordica charantia nanoparticles promote mitochondria biogenesis in the pancreas of diabetic-induced rats

    Olusola Olalekan Elekofehinti / Olusola Christianah Ayodele / Opeyemi Iwaloye

    Egyptian Journal of Medical Human Genetics, Vol 22, Iss 1, Pp 1-

    gene expression study

    2021  Volume 11

    Abstract: Abstract Background Mitochondria dysfunction is one of the clinical features of diabetes mellitus (DM), which is a hallmark of insulin resistance (IR). This study investigates the therapeutic effect of Momordica charantia nanoparticles on mitochondria ... ...

    Abstract Abstract Background Mitochondria dysfunction is one of the clinical features of diabetes mellitus (DM), which is a hallmark of insulin resistance (IR). This study investigates the therapeutic effect of Momordica charantia nanoparticles on mitochondria biogenesis in diabetic-induced rats. Forty-two adult wistar rats (average weight of 189 ± 10.32) were grouped as follows: STZ (65 mg/kg), control group, STZ + silver nitrate (10 mg/kg), STZ + M. charantia silver nanoparticles (50 mg/kg), STZ + metformin (100 mg/kg), and STZ + M. charantia aqueous extract (100 mg/kg). DM was induced intraperitoneal using freshly prepared solution of STZ (65 mg/kg), and rats with fasting blood sugar (FBS) above 250 mg/dl after 72 h of induction were considered diabetic. Treatment started after the third day of induction and lasted for 11 days. Effect of M. charantia nanoparticles on glucose level and pancreatic expression of genes involved in mitochondria biogenesis (PGC-1α, AMPK, GSK-3β, PPARϒ), inflammation (IL-1B, TNFα) and glucose sensitivity (PI3K, AKT, PTEN Insulin and Glut2) were quantified using reverse-transcriptase polymerase chain reaction (RT-PCR). Results The results showed that M. charantia nanoparticles promote mitochondria biogenesis, glucose sensitivity and reverse inflammation in the pancreas of diabetes rat model through upregulation of PGC-1α, AMPK, PPARϒ, AKT, Insulin and Glut2 mRNA expression and downregulation of GSK-3β, PI3K, IL-1B and TNFα mRNA expression in the pancreas of diabetic rats. Conclusion This study thus concludes that M. charantia nanoparticles may provide effective therapeutics against mitochondria dysfunction in the pancreas of diabetic model.
    Keywords Diabetes mellitus ; Mitochondria biogenesis ; Inflammation ; Glucose sensitivity ; Momordica charantia nanoparticles ; Medicine (General) ; R5-920 ; Genetics ; QH426-470
    Subject code 610
    Language English
    Publishing date 2021-11-01T00:00:00Z
    Publisher SpringerOpen
    Document type Article ; Online
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  4. Article ; Online: Bambusa vulgaris

    Elekofehinti, Olusola Olalekan / Aladenika, Yetunde Victoria / Iwaloye, Opeyemi / Okon, Enoabasi Ima-Abasi / Adanlawo, Isaac Gbadura

    Hormone molecular biology and clinical investigation

    2023  Volume 44, Issue 2, Page(s) 159–180

    Abstract: Objectives: There is evidence that mitochondrial dysfunction mediated by hyperglycemia increases the incidence of diabetes and age-related insulin resistance. Thus, maintaining mitochondrial integrity may provide alternative therapeutic approach in ... ...

    Abstract Objectives: There is evidence that mitochondrial dysfunction mediated by hyperglycemia increases the incidence of diabetes and age-related insulin resistance. Thus, maintaining mitochondrial integrity may provide alternative therapeutic approach in diabetes treatment. This study aimed to evaluate the effect of
    Methods: 11 weeks old male rats (n=30) were purchased, and sorted into the following groups: control, diabetic control, diabetes + metformin (100 mg/kg), diabetes + Aq.
    Results: The results showed that
    Conclusions: This study thus suggests that
    MeSH term(s) Rats ; Male ; Animals ; Bambusa/genetics ; Bambusa/metabolism ; Kelch-Like ECH-Associated Protein 1/metabolism ; Diabetes Mellitus, Experimental/drug therapy ; Diabetes Mellitus, Experimental/genetics ; AMP-Activated Protein Kinases/genetics ; AMP-Activated Protein Kinases/metabolism ; AMP-Activated Protein Kinases/pharmacology ; Glycogen Synthase Kinase 3/metabolism ; Glycogen Synthase Kinase 3/pharmacology ; Glycogen Synthase Kinase 3/therapeutic use ; Molecular Docking Simulation ; NF-E2-Related Factor 2/metabolism ; NF-E2-Related Factor 2/pharmacology ; NF-E2-Related Factor 2/therapeutic use ; Mitochondria/metabolism ; DNA, Mitochondrial ; Plant Extracts/pharmacology ; Plant Extracts/therapeutic use ; RNA, Messenger/metabolism
    Chemical Substances Kelch-Like ECH-Associated Protein 1 ; AMP-Activated Protein Kinases (EC 2.7.11.31) ; Glycogen Synthase Kinase 3 (EC 2.7.11.26) ; NF-E2-Related Factor 2 ; DNA, Mitochondrial ; Plant Extracts ; RNA, Messenger
    Language English
    Publishing date 2023-01-03
    Publishing country Germany
    Document type Journal Article
    ZDB-ID 2536635-X
    ISSN 1868-1891 ; 1868-1883
    ISSN (online) 1868-1891
    ISSN 1868-1883
    DOI 10.1515/hmbci-2022-0053
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  5. Article: Exploring the antidiabetic potential of compounds isolated from

    Ukwenya, Victor Okoliko / Adelakun, Sunday Aderemi / Elekofehinti, Olusola Olalekan

    In silico pharmacology

    2021  Volume 9, Issue 1, Page(s) 25

    Abstract: Diabetes mellitus is becoming an important public health challenge worldwide and especially in developing nations. About 8.8 percent of the world adult population has been reported to have diabetes. Glutamine-fructose-6-phosphate amidotransferase 1 ( ... ...

    Abstract Diabetes mellitus is becoming an important public health challenge worldwide and especially in developing nations. About 8.8 percent of the world adult population has been reported to have diabetes. Glutamine-fructose-6-phosphate amidotransferase 1 (GFAT1) catalyses the first committed step in the pathway for biosynthesis of hexosamines in mammals, and its inhibition has been thought to prevent hyperglycaemia. Dipeptidyl peptidase-4 (DPP-4), on the other hand, degrades hormone glucagon-like peptide-1 (GLP-1), an enzyme that plays a major role in the enhancement of glucose-dependent insulin secretion, making these two proteins candidate targets for diabetes. To find potential inhibitors of DPP-4 and GFAT1 from Anacardium occidentale using a computational approach, glide XP (extra precision) docking, Induced Fit Docking (IFD), Binding free energy of the compounds were determined against prepared crystal structure of DPP-4 and GFAT1 using the Maestro molecular interface of Schrödinger suites. The Lipinski's rule of five (RO5) and ADME properties of the compounds were assessed. Predictive models for both protein targets were built using AutoQSAR. This study identified 8 hit compounds. Most of these compounds passed the RO5 and were within the recommended range for defined ADME parameters. In addition, the predicted pIC50 for the hit compounds were promising. The results obtained from the present study can be used to design an antidiabetic drug.
    Supplementary information: The online version contains supplementary material available at 10.1007/s40203-021-00084-z.
    Language English
    Publishing date 2021-04-03
    Publishing country Germany
    Document type Journal Article
    ZDB-ID 2702993-1
    ISSN 2193-9616
    ISSN 2193-9616
    DOI 10.1007/s40203-021-00084-z
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  6. Article ; Online: Virtual screening of natural compounds as selective inhibitors of polo-like kinase-1 at C-terminal polo box and N-terminal catalytic domain.

    Olawale, Femi / Iwaloye, Opeyemi / Elekofehinti, Olusola Olalekan

    Journal of biomolecular structure & dynamics

    2021  Volume 40, Issue 24, Page(s) 13606–13624

    Abstract: The over-expression of Polo-like kinase-1 (PLK1) is associated with cancer prognosis due to its pivotal role in cell proliferation. The N-terminal catalytic domain (NCD) and C-terminal polo box domain (PBD) of PLK1 are critical for the activity of the ... ...

    Abstract The over-expression of Polo-like kinase-1 (PLK1) is associated with cancer prognosis due to its pivotal role in cell proliferation. The N-terminal catalytic domain (NCD) and C-terminal polo box domain (PBD) of PLK1 are critical for the activity of the protein. Drugs that inhibit PLK1 by targeting these domains are on clinical trials, but so far, none has been approved by FDA. Thus, this study targets the two domains of PLK1 to identify compounds with inhibitory potential. Four validated e-pharmacophore models from NCD (PDB ID: 2OU7 and 4J52) and PBD (PDB ID: 5NEI and 5NN2) were used to screen over 26,000 natural compounds from NPASS database. Hits were identified after the well-fitted compounds were subjected to molecular docking study and ADME prediction. The pIC50 and electronic behaviour of the identified hits selectively targeting NCD and PBD of PLK1 were predicted via an externally validated QSAR model and quantum mechanics. The results showed that CAA180504, CAA197326, CAA74619, CAA328856 modulating PLK1 at NCD, and CBB130581, CBB230713, CBB206123, CBB12656 and CBB267117 modulating PLK1 at PBD had better molecular docking scores, pharmacokinetics and drug-like properties than NCD (volasertib) and PBD (purpurogallin) reference inhibitors. The compounds all had satisfactory inhibitory (pIC50) values which range from 6.187 to 7.157. The electronic behaviours of understudied compounds using HOMO/LUMO and global descriptive parameters revealed the atomic portion of the compounds prone to donating and accepting electrons. In conclusion, the hit compounds identified from the library of natural compounds are worthy of further experimental validation.Communicated by Ramaswamy H. Sarma.
    MeSH term(s) Humans ; Molecular Docking Simulation ; Catalytic Domain ; Noncommunicable Diseases ; Cell Cycle Proteins ; Protein Domains ; Cell Proliferation ; Protein Kinase Inhibitors/pharmacology ; Protein Kinase Inhibitors/metabolism
    Chemical Substances Cell Cycle Proteins ; Protein Kinase Inhibitors
    Language English
    Publishing date 2021-10-20
    Publishing country England
    Document type Journal Article
    ZDB-ID 49157-3
    ISSN 1538-0254 ; 0739-1102
    ISSN (online) 1538-0254
    ISSN 0739-1102
    DOI 10.1080/07391102.2021.1991476
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  7. Article: Momordica charantia

    Elekofehinti, Olusola Olalekan / Oyedokun, Victor Oluwatoyin / Iwaloye, Opeyemi / Lawal, Akeem Olalekan / Ejelonu, Oluwamodupe Cecilia

    Journal of diabetes and metabolic disorders

    2021  Volume 20, Issue 1, Page(s) 245–260

    Abstract: Objectives: Diabetes nephropathy (DN) is one of the complications of diabetes mellitus (DM) marked by gradual progressive loss of renal function. SOCS/JAK/STAT and PI3K/Akt/PTEN signalling pathways are among the chain of interactions implicated in the ... ...

    Abstract Objectives: Diabetes nephropathy (DN) is one of the complications of diabetes mellitus (DM) marked by gradual progressive loss of renal function. SOCS/JAK/STAT and PI3K/Akt/PTEN signalling pathways are among the chain of interactions implicated in the onset, progression and pathology of DN.
    Methods: The
    Results: Oral administration of
    Conclusion: Observation drawn from this study suggests that
    Language English
    Publishing date 2021-02-05
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2680289-2
    ISSN 2251-6581
    ISSN 2251-6581
    DOI 10.1007/s40200-021-00739-w
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  8. Article: Saponins: Anti-diabetic principles from medicinal plants - A review.

    Elekofehinti, Olusola Olalekan

    Pathophysiology : the official journal of the International Society for Pathophysiology

    2015  Volume 22, Issue 2, Page(s) 95–103

    Abstract: Diabetes mellitus (DM) represents a global health problem. It is the most common of the endocrine disorders and is characterized by chronic hyperglycemia due to relative or absolute lack of insulin secretion or insulin actions. According to the World ... ...

    Abstract Diabetes mellitus (DM) represents a global health problem. It is the most common of the endocrine disorders and is characterized by chronic hyperglycemia due to relative or absolute lack of insulin secretion or insulin actions. According to the World Health Organization projections, the diabetes population is likely to increase to 300 million or more by the year 2025. Current synthetic agents and insulin used effectively for the treatment of diabetes are scarce especially in rural areas, expensive and have prominent adverse effects. Complementary and alternative approaches to diabetes management such as isolation of phytochemicals with anti-hyperglycemic activities from medicinal plants is therefore imperative. Saponins are phytochemical with structural diversity and biological activities. This paper reviews saponins and various plants from which they were isolated as well as properties that make them ideal for antidiabetic remedy.
    Language English
    Publishing date 2015-02-16
    Publishing country Netherlands
    Document type Journal Article ; Review
    ZDB-ID 1212740-1
    ISSN 0928-4680
    ISSN 0928-4680
    DOI 10.1016/j.pathophys.2015.02.001
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  9. Article: Identification of lead compounds from large natural product library targeting 3C-like protease of SARS-CoV-2 using E-pharmacophore modelling, QSAR and molecular dynamics simulation.

    Elekofehinti, Olusola Olalekan / Iwaloye, Opeyemi / Molehin, Olorunfemi R / Famusiwa, Courage D

    In silico pharmacology

    2021  Volume 9, Issue 1, Page(s) 49

    Abstract: COVID-19 is a novel disease caused by SARS-CoV-2 and has made a catastrophic impact on the global economy. As it is, there is no officially FDA approved drug to alleviate the negative impact of SARS-CoV-2 on human health. Numerous drug targets for ... ...

    Abstract COVID-19 is a novel disease caused by SARS-CoV-2 and has made a catastrophic impact on the global economy. As it is, there is no officially FDA approved drug to alleviate the negative impact of SARS-CoV-2 on human health. Numerous drug targets for neutralizing coronavirus infection have been identified, among them is 3-chymotrypsin-like-protease (3CL
    Language English
    Publishing date 2021-08-07
    Publishing country Germany
    Document type Journal Article
    ZDB-ID 2702993-1
    ISSN 2193-9616
    ISSN 2193-9616
    DOI 10.1007/s40203-021-00109-7
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  10. Article ; Online: Saponins in Cancer Treatment: Current Progress and Future Prospects.

    Elekofehinti, Olusola Olalekan / Iwaloye, Opeyemi / Olawale, Femi / Ariyo, Esther Opeyemi

    Pathophysiology : the official journal of the International Society for Pathophysiology

    2021  Volume 28, Issue 2, Page(s) 250–272

    Abstract: Saponins are steroidal or triterpenoid glycoside that is distinguished by the soap-forming nature. Different saponins have been characterized and purified and are gaining attention in cancer chemotherapy. Saponins possess high structural diversity, which ...

    Abstract Saponins are steroidal or triterpenoid glycoside that is distinguished by the soap-forming nature. Different saponins have been characterized and purified and are gaining attention in cancer chemotherapy. Saponins possess high structural diversity, which is linked to the anticancer activities. Several studies have reported the role of saponins in cancer and the mechanism of actions, including cell-cycle arrest, antioxidant activity, cellular invasion inhibition, induction of apoptosis and autophagy. Despite the extensive research and significant anticancer effects of saponins, there are currently no known FDA-approved saponin-based anticancer drugs. This can be attributed to a number of limitations, including toxicities and drug-likeness properties. Recent studies have explored options such as combination therapy and drug delivery systems to ensure increased efficacy and decreased toxicity in saponin. This review discusses the current knowledge on different saponins, their anticancer activity and mechanisms of action, as well as promising research within the last two decades and recommendations for future studies.
    Language English
    Publishing date 2021-06-05
    Publishing country Switzerland
    Document type Journal Article ; Review
    ZDB-ID 1212740-1
    ISSN 1873-149X ; 0928-4680
    ISSN (online) 1873-149X
    ISSN 0928-4680
    DOI 10.3390/pathophysiology28020017
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