Antidiabetic effect of kolaviron, a biflavonoid complex isolated from Garcinia kola seeds, in Wistar rats

Adaramoye, Oluwatosin A.

doi:10.4314/ahs.v12i4.16

Cited by 31 publications

(35 citation statements)

References 29 publications

(24 reference statements)

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“…Biflavonoids are flavonoid dimers that have been attached to each other by either C-C or C-O-C bonds representing a variety of chemical structures [2]. Several biological activities such as antioxidant [3,4], antiviral [5], hypolipidemic [6], antidiabetic [7], anti-tumoral [8], antituberculosis [9], antimalarial [10], antibacterial [11], antifungal [12], and anti-inflammatory [13] effects have been reported for biflavonoids.…”

Section: Introductionmentioning

confidence: 99%

Molecular docking and quantum mechanical studies on biflavonoid structures as BACE-1 inhibitors

et al. 2014

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Beta-site amyloid precursor protein cleaving enzyme (BACE-1) is a well-known therapeutic target for Alzheimer disease (AD) due to its characteristic role in the pathogenesis of AD. Numerous researches have been focused on the design and development of potent peptidic and nonpeptidic BACE-1 inhibitors. In the present contribution, a series of experimentally validated biflavonoid BACE-1 inhibitors (1-21) were subjected to our structure-based molecular modeling studies. Binding modes were elucidated through molecular docking in the active site of the enzyme. Relatively good correlations between the theoretical and experimental binding affinities could be achieved (R 2 = 0.61). Analysis of intermolecular binding energy components was performed via functional B3LYP in association with splitvalence basis set using polarization functions (Def2-SVP), and structure-binding relationships were further elucidated through ligand-residue binding energies. Since little studies have been performed on the modeling and structure activity/binding relationships of biflavonoid structures as BACE-1 inhibitors, the results of this study may be useful in further extending the scope of biflavonoid structures as potential anti-Alzheimer scaffolds.

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Section: Introductionmentioning

confidence: 99%

Molecular docking and quantum mechanical studies on biflavonoid structures as BACE-1 inhibitors

et al. 2014

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“…During diabetes, the activities of the aminotransferases are elevated. 44 The administration of ISTPPLG NPs produced a significant decrease in serum ALT activity, which was comparable to that of normal control.…”

Section: Effect Of Istpplg Nps On Lipid Profiles and Status Of Biochementioning

confidence: 66%

Novel PLGA-based nanoparticles for the oral delivery of insulin

Malathi¹,

Nandhakumar²,

Pandiyan³

et al. 2015

IJN

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Background Insulin is the drug therapy for patients with insulin-dependent diabetes mellitus. A number of attempts have been made in the past to overcome the problems associated with the oral delivery of insulin, but with little success. Orally administered insulin has encountered with many difficulties such as rapid degradation and poor intestinal absorption. The potential use of D-α-tocopherol poly(ethylene glycol) 1000 succinate (TPGS)-emulsified poly(ethylene glycol) (PEG)-capped poly(lactic- co -glycolic acid) (PLGA) nanoparticles (NPs) was investigated for sustained delivery of insulin (IS). Objective To investigate the efficacy of TPGS-emulsified PEG-capped PLGA NPs (TPPLG NPs) as a potential drug carrier for the oral delivery of insulin. Methods A series of biodegradable low-molecular-weight PLGA (80/20 [PLG4] and 70/30 [PLG6]) copolymers were synthesized by melt polycondensation. The commercial insulin-loaded TPGS-emulsified PEG-capped PLGA NPs (ISTPPLG NPs) were synthesized by water–oil–water emulsion solvent evaporation method. The physical and chemical properties of PLGA copolymers, particle size, zeta potential, and morphology of the NPs were examined. The in vivo studies of ISTPPLG NPs were carried out in diabetic rats by oral administration. Results The maximum encapsulation efficiency of ISTPPLG6 NPs was 78.6%±1.2%, and the mean diameter of the NPs was 180±20 nm. The serum glucose level was significantly (twofold) decreased on treatment with ISTPPLG NPs, and there was a threefold decrease with insulin-loaded PLGA (70/30) NPs when compared to that of free insulin-treated diabetic rats. The results show that the oral administration of ISTPPLG6 NPs is an effective method of reducing serum glucose level for a period of 24 hours. Histopathological studies reveal that ISTPPLG NPs could restore the damage caused by streptozotocin in the liver, kidneys, and pancreas, indicating its biocompatibility and regenerative effects. Conclusion ISTPPLG6 NPs can act as potential drug carriers for the oral delivery of insulin.

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“…Serum and cardiac protein, CK-MB and LDH levels were assayed by the methods described by Adaramoye [12].…”

Section: Protein Creatine Kinase Mb (Ck-mb) and Lactate Dehydrogenasmentioning

confidence: 99%

“…Extracts of the plant have been used in African herbal medicine for the treatment of laryngitis, heart burns, liver diseases, cough and hoarseness of voice [10]. Kolaviron (KV) is a bioflavonoid complex isolated from the seeds of G. kola and has been reported to possess anti-inflammatory, antidiabetic, antioxidant, antigenotoxic and hepatoprotective activities in model systems via multiple biochemical mechanisms [11,12]. Early studies by Adaramoye et al [13] and Adaramoye and Medeiros [14] showed the anti-atherogenic and vasorelaxant effects of KV in an animal model and isolated smooth muscle, respectively.…”

Section: Introductionmentioning

confidence: 99%

Kolaviron, a biflavonoid fraction from Garcinia kola, protects against isoproterenol-induced injury by mitigating cardiac dysfunction and oxidative stress in rats

Adaramoye

Lawal

2014

Journal of Basic and Clinical Physiology and Pharmacology

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Antidiabetic effect of kolaviron, a biflavonoid complex isolated from Garcinia kola seeds, in Wistar rats

Abstract: Background: Hypoglycaemic effect of kolaviron (KV), (biflavonoid from Garcinia kola) in streptozotocin (STZ)-diabetic rats has been established.

Cited by 31 publications

References 29 publications

Molecular docking and quantum mechanical studies on biflavonoid structures as BACE-1 inhibitors

Molecular docking and quantum mechanical studies on biflavonoid structures as BACE-1 inhibitors

Novel PLGA-based nanoparticles for the oral delivery of insulin

Kolaviron, a biflavonoid fraction from Garcinia kola, protects against isoproterenol-induced injury by mitigating cardiac dysfunction and oxidative stress in rats

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