Hormone Molecular Biology and Clinical Investigation
Objectives There is evidence that mitochondrial dysfunction mediated by hyperglycemia increases t... more 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 Bambusa vulgaris leaf extract on mitochondrial biogenesis in the pancreas of diabetic rats. 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. B. vulgaris (100 mg/kg), diabetes + Aq. B. vulgaris (200 mg/kg), and diabetes + Aq. B. vulgaris (300 mg/kg). Diabetes was induced in the rats by a single dose of 65 mg/kg streptozotocin (STZ). The mRNA expression of genes related to mitochondria biogenesis (pgc-1α, Nrf2, GSK3β, AMPK and SIRT2) and genes of Nrf2-Keap1-ARE signaling pathway were determined by reverse transcriptase polymerase chain reaction. Molecular docking...
Pathophysiology : the official journal of the International Society for Pathophysiology, Jan 12, 2018
Momordica charantia (bitter lemon) belongs to the cucurbitaceae family which has been extensively... more Momordica charantia (bitter lemon) belongs to the cucurbitaceae family which has been extensively used in traditional medicines for the cure of various ailments such as cancer and diabetes. The underlying mechanism of M. charantia to maintain glycemic control was investigated. GLP-1 and DPP-4 gene modulation by M. charantia (5-20% inclusion in rats diet) was investigated in vivo by RT-PCR and possible compounds responsible for diabetic action predicted through in silico approach. Phytochemicalss previously characterized from M. charantia were docked into glucacon like peptide-1 receptor (GLP-1r), dipeptidyl peptidase (DPP4) and Takeda-G-protein-receptor-5 (TGR5) predicted using Autodock Vina. The results of the in silico suggests momordicosides D (ligand for TGR5), cucurbitacin (ligand for GLP-1r) and charantin (ligand for DPP-4) as the major antidiabetic compounds in bitter lemon leaf. M. charantia increased the expression of GLP-1 by about 295.7% with concomitant decreased in expr...
Saponins are steroidal or triterpenoid glycoside that is distinguished by the soap-forming nature... more 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 anticance...
Background Mitochondria dysfunction is one of the clinical features of diabetes mellitus (DM), wh... more 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...
Hyperlipidemia and hyperglycemia have been implicated in diabetes mellitus (DM) leading to compli... more Hyperlipidemia and hyperglycemia have been implicated in diabetes mellitus (DM) leading to complications such as nephropathy. Medicinal plants like Mormodica charantia (MC) have been used in the treatment of DM over the years but little is known about their mechanisms of action. This study used biotechnology tools to investigate and compare the effects of M. charantia silver nanoparticles (MCSNPs) with M. charantia extract on expressions of genes linked with nephrotoxicity, lipid and glucose metabolisms using reverse-transcriptase polymerase chain reaction (RT-PCR) in streptozotocin-induced diabetic rats. The genes investigated include kidney injury molecule-1 (KIM-1), 3hydroxyl, 3-methyl glutaryl_coA reductase (HMG-CoA reductase), peroxisome proliferatoractivated receptor alpha and gamma (PPARα and PPARγ). Synthesis of MCSNPs was done using 1 mM concentration of aqueous silver nitrate solution at ratio 1:9 (v/v). Experimental rats were induced intraperitoneally with streptozotocin ...
Background: Activation of Takeda G-protein bile acid receptor 5 (TGR5) secretes glucagon-like pep... more Background: Activation of Takeda G-protein bile acid receptor 5 (TGR5) secretes glucagon-like peptide-1 (GLP1) downstream insulin release. Saponin which has been indicated as the antidiabetic principle in plant shared similar steroidal scaffold with cholic acid (primary agonist of TGR5), hence antidiabetic mechanism of Tithonia diversifolia leaves saponin-rich extract (TDS) was investigated via TGR5/GLP-1 pathway. Methods: Insulin secretion and expression of GLP1 were measured in MIN6 β-cells incubated with TDS and cholic acid a known agonist of TGR5 at (25, 75, 125, 325) µg/ml and treatment were compared to incubation with insulin secretagogue metformin (50 mM). The action of TDS on TGR5 was studied in vivo using swiss albino mice. Results: β-cell assay showed dose dependent increase in insulin secretion/1 × 10 6 cells incubated with TDS (25, 75, 125, 325 µg/ml) when compared with positive control (50 mM metformin) and vehicle control (Cholic acid). TDS increased GLP-1 and insulin expression and decrease the percentage of%HbA1c in treated mice when compared with control (p < 0.05). TGR5 gene were highly expressed in cell incubated with 20-60 mg/kg body weight of TDS compared to STZ-induced diabetic mice and immunoblotting of TGR5 protein showed higher expression in all groups treated with TDS compared to STZ-induced diabetic mice. Conclusion: TDS exhibit its antidiabetic mechanism via TGR5 agonism leading to increase GLP-1 expression and subsequently insulin release. Hence TDS may represent a new therapeutic strategy for type-2 diabetes, a finding which could be further investigated in clinical trials.
Aromatase, a cytochrome P450 enzyme complex present in breast tissues, plays a significant role i... more Aromatase, a cytochrome P450 enzyme complex present in breast tissues, plays a significant role in the biosynthesis of important endogenous estrogens. In hormone-dependent breast cancer, estrogen plays a significant role in the stimulation of breast cancer cell proliferation. Inhibition of aromatase has been put forward to be a therapeutic target for breast cancer. In silico predictions based on the crystal structure of aromatase was done. Active molecular docking studies using Autodock software revealed that borapetol is a novel inhibitor of aromatase with binding affinity of -9.4 kcal/mol compared to known aromatase inhibitor, anastrozole with binding affinity of -7.9 kcal/mol. The results showed that borapetol portrayed a better affinity to bind aromatase, by interacting at the catalytic site of enzyme. Hence, borapetol may be a potent lead compound for the treatment of breast cancer but further experimental and clinical confirmation is needed to prove it as valid drug.
British Journal of Medicine and Medical Research, 2016
Aims: Peroxisome proliferator-activated receptor gamma (PPARγ) agonists are beneficial in the man... more Aims: Peroxisome proliferator-activated receptor gamma (PPARγ) agonists are beneficial in the management of diabetes by increasing insulin sensitivity and inhibiting hepatic gluconeogenesis. The aim of the present study was to investigate PPAR-γ agonist property of rutin, a flavonoid found in many plant species compared to thiazolidenediones (TZDs) using in silico approach. Methodology: Molecular docking of rutin on human PPAR-γ protein was determined by Vina plugin in PYMOL 1.3 and compared with thiazolidinediones, a known agonist of PPARγ. Results: Rutin acts as a potential agonist with binding energy of-7.8 kcal/mol compared to thiazolidinediones with binding energy of-4.1 kcal/mol. The molecular interaction of rutin was at residues of GLU 319, ILE 369, LEU 368, MET 362, PHE 321, PHE 310, LEU 497, ALA 320, LYS 289, ILE 354. Conclusion: We conclude that rutin is a better PPARγ agonist than TZDs confirming the capability of rutin for binding at the active site of the PPARγ.
The quest for save herbal remedy for the managementof cardiovascular diseases prompted this inves... more The quest for save herbal remedy for the managementof cardiovascular diseases prompted this investigation and itis aimed at determining the effect ofSaponin fromSolanum anguivi fruits on serum lipid profile - a risk factor in thedevelopment coronary heart disease (CHD).Thirty six (36) rats(Rattusnovergicus) of average weight (125± 12g) were divided into six (6) groups of six animals each designated as A (n=6, 2.0ml distilled water), B (n=6, 20mg/kg saponin), C (n=6, 40mg/kg), D (n=6, 60mg/kg), E (n=6, 80mg/kg), and F (n=6, 100mg/kg). Saponin was administered orally once daily to groups B,C,D,E and F for (21) days.Serum lipid profile was determined usingdiagnostic kits. The result showed an initial significant increase (p<0.05) in weights of the treated animalswhen compared with thecontrol but by the third week, the increase was not significant. A significant reduction (P<0.05) in serum Triglycerides, total Cholesteroland Low-Density Lipoprotein(LDL) was observed while High-Den...
Reactive Oxygen Species (ROS) are generated via normal metabolic processes or as the products of ... more Reactive Oxygen Species (ROS) are generated via normal metabolic processes or as the products of exogenous insults. They are capable of damaging essential biomolecules and accelerating cancer, cardiovascular diseases and neurodegenerative diseases. In this study, the effect saponin from Solanum anguivi (SAS) fruits on Superoxide Dismutase (SOD), catalase (CAT) and Lipid Peroxidation (LPO) in the homogenates of the hearts and kidney was evaluated. Thirty six male Wister rats of average weight125±12 g were divided into six groups of six animals each. Five treated groups received a daily dose of saponin at 20, 40, 60, 80 and 100 mg/kg respectively, while distilled water was administered to the control group for 3 weeks. Solanum anguivi saponin significantly increased (p<0.05) both catalase and SOD activities in the heart, There was also corresponding increase in activities of both enzymes in the kidney but was not significant. MDA concentration was reduced significantly (p<0.05) ...
Objective: To evaluate the antioxidant and radical scavenging activities of saponins from Solanum... more Objective: To evaluate the antioxidant and radical scavenging activities of saponins from Solanum anguivi fruit (SAGU) and its possible effect on oxidative status of rat exposed to alloxan-induced diabetes. Methods: Antioxidant activity of SAGU was assayed by using 2,2'-azino-bis3-ethylbenzothiazoline-6-sulphonic acid (ABTS), reducing power, iron chelation and ability to inhibit lipid peroxidation in both liver and brain homogenates of rats. Also, the effect of SAGU on MDA level, an indicator of lipid peroxidation and activity of superoxide dismutase (SOD) and catalase (CAT) were determined in heart and kidney of rat exposed to alloxan (150mg/kg) for 21 days. Results: SAGU exhibited potent and concentration dependent free radical-scavenging activity (IC50/ABTS = 290.12 ± 1.34µg/ml). Reductive and iron chelation abilities also increase with increase in SAGU concentration. SAGU also inhibited peroxidation of hepatic and cerebral lipids subjected to iron oxidative assault. In addit...
The effects of saponin from the fruits of Solanum anguivi (SAS) on body weight, serum and liver s... more The effects of saponin from the fruits of Solanum anguivi (SAS) on body weight, serum and liver superoxide dismutase (SOD), catalase and malondialdehyde (MDA) of normal rats were investigated. Saponin from Solanum anguivi were administered by gavages to experimental rats at dosages of 20 mg/kg, 40 mg/kg, 60 mg/kg, 80 mg/kg and 100 mg/kg body weight, over a period of 21 days. A non significant increase (p<0.05) in weights of the treated animals was observed by the third week. Treatment had no significant effect (p<0.05) on serum activities of catalase, but caused statistically significant increase in SOD and decrease in MDA level at 80 and 100 mg/kg dosages in rats. A dose-dependent and statistically significant increase (p<0.05) in the hepatic activities of catalase and SOD as well as decrease in concentration of MDA was observed in rats administered 40-100 mg/kg dose of SAS . The result suggests that saponin from the fruit of S. anguivi has antioxidant and antiperoxidative...
The proximate analysis, mineral composition, amino acid composition and the anti- nutrient conten... more The proximate analysis, mineral composition, amino acid composition and the anti- nutrient content in leaf of Cnidoscolus aconitifolius was determined. The result showed that Cnidoscolus aconitifolius leaf has a high percentage of carbohydrate 35.70±2.00, protein 18.73±0.65, Ash 13.74±0.76, moisture con-tent 9.49±1.20, crude fibre 9.68±0.93. Amino acid concentrations present include Lys. 5.05±0.13, His 2.60±0.37, NH3 is nil, Arg 5.17±0.15, Asp 8.50±0.48, Thr 3.70±0.25, Ser 3.36±0.37, Glu 13.50±0.74, Pro 3.50±0.29, Gly 4.10±0.02, Ala 4.60±0.11, Cys 1.19±0.48, measured in g/100g. Glutamic acid have the highest concentration while cystine have the lowest concentra-tion. Anti –nutrient present are in low concentration, they include phytin phosphorus (2.67mg/100g), phytic acid (9.47mg/100g), oxalate (2.005mg/100g) and tannin(0.24mg/100g). The average values for Ca, Mg, Na, K, Fe, Zn and P were 400.80, 219.96, 725.44, 194.46, 0.57, 437.44, 0.13, 0.03mg/100g dry sample respectively. Sodium...
The ability of the aqueous extract of flesh and seed of Solanum anguivi Lam fruit (African eggpla... more The ability of the aqueous extract of flesh and seed of Solanum anguivi Lam fruit (African eggplant) used in folk medicine to treat diabetes and hypertension to inhibit Fe 2+ and SNP induced lipid peroxidation in rats brain in vitro was determined. The total phenol, total flavonoid, vitamin C content, ferric reducing antioxidant property as well as Fe 2+ chelating ability were also determined. The results of this study revealed that aqueous extract of Solanum anguivi fruit (flesh and seed) cause a significant decrease (P<0.05) in the MDA production in rats brain when compared with control. The inhibitory effect of both flesh and seeds of Solanum anguivi on lipid peroxidation could be attributed to the phenol (flesh, 7.13 ± 0.73mg/g GAE, seed 8.20 ± 0.32 mg/g GAE), total flavonoid ( flesh 3.53 ± 0.49mg/g QE, seed 1.62 ± 0.61mg/g QE) and vitamin C content (flesh 12.85 ± 0.20mg/g, seed 14.92 ± 0.11 mg/g), as well as ferric reducing antioxidant property and Fe 2+ - chelating ability....
Solanum anguivi fruit saponin has antidiabetic property via interference with cellular energy met... more Solanum anguivi fruit saponin has antidiabetic property via interference with cellular energy metabolism and inhibition of reactive oxygen species (ROS) generation. In the current study, brain specific in vitro anti-oxidant role of S. anguivi saponin was investigated in the P2 synaptosomal fraction of rat brain. Using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide reduction assay, S. anguivi saponin concentration- dependently (10-200 µg/ml) reversed Fe(2+) and sodium nitroprusside- induced decrease in mitochondrial activity via inhibition of ROS production, ROS-induced oxidation of protein and non-protein thiol-containing molecules and lipid peroxidation as measured by thiobarbituric acid reactive substances levels. Conclusively, S. anguivi fruit saponin represents a class of natural compounds with the ability to reverse synaptosomal disruption, loss of mitochondrial integrity and function often associated with the progression of Huntington's disease, Alzheimer dis...
Indian journal of clinical biochemistry : IJCB, 2002
Dietary spice components ofCurcuma longa andAbroma augusta have been screened for their protectiv... more Dietary spice components ofCurcuma longa andAbroma augusta have been screened for their protective effect against reactive oxygen species induced lipid peroxidation. They have been found to be efficient antioxidant when administered in combination. The purpose of the study was to investigate the effect of oral administration (300mg/Kg) of the aqueous extract of turmeric whose active ingredient isCurcumin andAbromine powder as a hypoglycemic agent mixed with diet. The effect of this aqueous extract on blood glucose, lipid peroxidation (LPO) and the antioxidant defense system in rat tissues like liver, lung, kidney and brain was studied for 8 weeks in streptozotocin induced diabetic rats. The administration of an aqueous extract of turmeric and abromine powder resulted in a significant reduction in blood glucose and an increase in total haemoglobin. The aqueous extract also resulted in decreased free radical formation in the tissues studied.The decrease in thiobarbituric acid reactive...
Asian Pacific journal of tropical biomedicine, 2013
To evaluate the antioxidant and radical scavenging activities of Solanum anguivi fruit (SAG) and ... more To evaluate the antioxidant and radical scavenging activities of Solanum anguivi fruit (SAG) and its possible effect on mitochondrial permeability transition pore as well as mitochondrial membrane potential (ΔΨm) isolated from rat liver. Antioxidant activity of SAG was assayed by using 2,2-diphenyl-1-picrylhydrazyl (DPPH), reducing power, iron chelation and ability to inhibit lipid peroxidation in both liver and brain homogenate of rats. Also, the effect of SAG on mitochondrial membrane potential and mitochondrial swelling were determined. Identification and quantification of bioactive polyphenolics was done by HPLC-DAD. SAG exhibited potent and concentration dependent free radical-scavenging activity (IC50/DPPH=275.03±7.8 μg/mL). Reductive and iron chelation abilities also increase with increase in SAG concentration. SAG also inhibited peroxidation of cerebral and hepatic lipids subjected to iron oxidative assault. SAG protected against Ca(2+) (110 μmol/L)-induced mitochondrial swe...
Hormone Molecular Biology and Clinical Investigation
Objectives There is evidence that mitochondrial dysfunction mediated by hyperglycemia increases t... more 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 Bambusa vulgaris leaf extract on mitochondrial biogenesis in the pancreas of diabetic rats. 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. B. vulgaris (100 mg/kg), diabetes + Aq. B. vulgaris (200 mg/kg), and diabetes + Aq. B. vulgaris (300 mg/kg). Diabetes was induced in the rats by a single dose of 65 mg/kg streptozotocin (STZ). The mRNA expression of genes related to mitochondria biogenesis (pgc-1α, Nrf2, GSK3β, AMPK and SIRT2) and genes of Nrf2-Keap1-ARE signaling pathway were determined by reverse transcriptase polymerase chain reaction. Molecular docking...
Pathophysiology : the official journal of the International Society for Pathophysiology, Jan 12, 2018
Momordica charantia (bitter lemon) belongs to the cucurbitaceae family which has been extensively... more Momordica charantia (bitter lemon) belongs to the cucurbitaceae family which has been extensively used in traditional medicines for the cure of various ailments such as cancer and diabetes. The underlying mechanism of M. charantia to maintain glycemic control was investigated. GLP-1 and DPP-4 gene modulation by M. charantia (5-20% inclusion in rats diet) was investigated in vivo by RT-PCR and possible compounds responsible for diabetic action predicted through in silico approach. Phytochemicalss previously characterized from M. charantia were docked into glucacon like peptide-1 receptor (GLP-1r), dipeptidyl peptidase (DPP4) and Takeda-G-protein-receptor-5 (TGR5) predicted using Autodock Vina. The results of the in silico suggests momordicosides D (ligand for TGR5), cucurbitacin (ligand for GLP-1r) and charantin (ligand for DPP-4) as the major antidiabetic compounds in bitter lemon leaf. M. charantia increased the expression of GLP-1 by about 295.7% with concomitant decreased in expr...
Saponins are steroidal or triterpenoid glycoside that is distinguished by the soap-forming nature... more 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 anticance...
Background Mitochondria dysfunction is one of the clinical features of diabetes mellitus (DM), wh... more 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...
Hyperlipidemia and hyperglycemia have been implicated in diabetes mellitus (DM) leading to compli... more Hyperlipidemia and hyperglycemia have been implicated in diabetes mellitus (DM) leading to complications such as nephropathy. Medicinal plants like Mormodica charantia (MC) have been used in the treatment of DM over the years but little is known about their mechanisms of action. This study used biotechnology tools to investigate and compare the effects of M. charantia silver nanoparticles (MCSNPs) with M. charantia extract on expressions of genes linked with nephrotoxicity, lipid and glucose metabolisms using reverse-transcriptase polymerase chain reaction (RT-PCR) in streptozotocin-induced diabetic rats. The genes investigated include kidney injury molecule-1 (KIM-1), 3hydroxyl, 3-methyl glutaryl_coA reductase (HMG-CoA reductase), peroxisome proliferatoractivated receptor alpha and gamma (PPARα and PPARγ). Synthesis of MCSNPs was done using 1 mM concentration of aqueous silver nitrate solution at ratio 1:9 (v/v). Experimental rats were induced intraperitoneally with streptozotocin ...
Background: Activation of Takeda G-protein bile acid receptor 5 (TGR5) secretes glucagon-like pep... more Background: Activation of Takeda G-protein bile acid receptor 5 (TGR5) secretes glucagon-like peptide-1 (GLP1) downstream insulin release. Saponin which has been indicated as the antidiabetic principle in plant shared similar steroidal scaffold with cholic acid (primary agonist of TGR5), hence antidiabetic mechanism of Tithonia diversifolia leaves saponin-rich extract (TDS) was investigated via TGR5/GLP-1 pathway. Methods: Insulin secretion and expression of GLP1 were measured in MIN6 β-cells incubated with TDS and cholic acid a known agonist of TGR5 at (25, 75, 125, 325) µg/ml and treatment were compared to incubation with insulin secretagogue metformin (50 mM). The action of TDS on TGR5 was studied in vivo using swiss albino mice. Results: β-cell assay showed dose dependent increase in insulin secretion/1 × 10 6 cells incubated with TDS (25, 75, 125, 325 µg/ml) when compared with positive control (50 mM metformin) and vehicle control (Cholic acid). TDS increased GLP-1 and insulin expression and decrease the percentage of%HbA1c in treated mice when compared with control (p &lt; 0.05). TGR5 gene were highly expressed in cell incubated with 20-60 mg/kg body weight of TDS compared to STZ-induced diabetic mice and immunoblotting of TGR5 protein showed higher expression in all groups treated with TDS compared to STZ-induced diabetic mice. Conclusion: TDS exhibit its antidiabetic mechanism via TGR5 agonism leading to increase GLP-1 expression and subsequently insulin release. Hence TDS may represent a new therapeutic strategy for type-2 diabetes, a finding which could be further investigated in clinical trials.
Aromatase, a cytochrome P450 enzyme complex present in breast tissues, plays a significant role i... more Aromatase, a cytochrome P450 enzyme complex present in breast tissues, plays a significant role in the biosynthesis of important endogenous estrogens. In hormone-dependent breast cancer, estrogen plays a significant role in the stimulation of breast cancer cell proliferation. Inhibition of aromatase has been put forward to be a therapeutic target for breast cancer. In silico predictions based on the crystal structure of aromatase was done. Active molecular docking studies using Autodock software revealed that borapetol is a novel inhibitor of aromatase with binding affinity of -9.4 kcal/mol compared to known aromatase inhibitor, anastrozole with binding affinity of -7.9 kcal/mol. The results showed that borapetol portrayed a better affinity to bind aromatase, by interacting at the catalytic site of enzyme. Hence, borapetol may be a potent lead compound for the treatment of breast cancer but further experimental and clinical confirmation is needed to prove it as valid drug.
British Journal of Medicine and Medical Research, 2016
Aims: Peroxisome proliferator-activated receptor gamma (PPARγ) agonists are beneficial in the man... more Aims: Peroxisome proliferator-activated receptor gamma (PPARγ) agonists are beneficial in the management of diabetes by increasing insulin sensitivity and inhibiting hepatic gluconeogenesis. The aim of the present study was to investigate PPAR-γ agonist property of rutin, a flavonoid found in many plant species compared to thiazolidenediones (TZDs) using in silico approach. Methodology: Molecular docking of rutin on human PPAR-γ protein was determined by Vina plugin in PYMOL 1.3 and compared with thiazolidinediones, a known agonist of PPARγ. Results: Rutin acts as a potential agonist with binding energy of-7.8 kcal/mol compared to thiazolidinediones with binding energy of-4.1 kcal/mol. The molecular interaction of rutin was at residues of GLU 319, ILE 369, LEU 368, MET 362, PHE 321, PHE 310, LEU 497, ALA 320, LYS 289, ILE 354. Conclusion: We conclude that rutin is a better PPARγ agonist than TZDs confirming the capability of rutin for binding at the active site of the PPARγ.
The quest for save herbal remedy for the managementof cardiovascular diseases prompted this inves... more The quest for save herbal remedy for the managementof cardiovascular diseases prompted this investigation and itis aimed at determining the effect ofSaponin fromSolanum anguivi fruits on serum lipid profile - a risk factor in thedevelopment coronary heart disease (CHD).Thirty six (36) rats(Rattusnovergicus) of average weight (125± 12g) were divided into six (6) groups of six animals each designated as A (n=6, 2.0ml distilled water), B (n=6, 20mg/kg saponin), C (n=6, 40mg/kg), D (n=6, 60mg/kg), E (n=6, 80mg/kg), and F (n=6, 100mg/kg). Saponin was administered orally once daily to groups B,C,D,E and F for (21) days.Serum lipid profile was determined usingdiagnostic kits. The result showed an initial significant increase (p<0.05) in weights of the treated animalswhen compared with thecontrol but by the third week, the increase was not significant. A significant reduction (P<0.05) in serum Triglycerides, total Cholesteroland Low-Density Lipoprotein(LDL) was observed while High-Den...
Reactive Oxygen Species (ROS) are generated via normal metabolic processes or as the products of ... more Reactive Oxygen Species (ROS) are generated via normal metabolic processes or as the products of exogenous insults. They are capable of damaging essential biomolecules and accelerating cancer, cardiovascular diseases and neurodegenerative diseases. In this study, the effect saponin from Solanum anguivi (SAS) fruits on Superoxide Dismutase (SOD), catalase (CAT) and Lipid Peroxidation (LPO) in the homogenates of the hearts and kidney was evaluated. Thirty six male Wister rats of average weight125±12 g were divided into six groups of six animals each. Five treated groups received a daily dose of saponin at 20, 40, 60, 80 and 100 mg/kg respectively, while distilled water was administered to the control group for 3 weeks. Solanum anguivi saponin significantly increased (p<0.05) both catalase and SOD activities in the heart, There was also corresponding increase in activities of both enzymes in the kidney but was not significant. MDA concentration was reduced significantly (p<0.05) ...
Objective: To evaluate the antioxidant and radical scavenging activities of saponins from Solanum... more Objective: To evaluate the antioxidant and radical scavenging activities of saponins from Solanum anguivi fruit (SAGU) and its possible effect on oxidative status of rat exposed to alloxan-induced diabetes. Methods: Antioxidant activity of SAGU was assayed by using 2,2'-azino-bis3-ethylbenzothiazoline-6-sulphonic acid (ABTS), reducing power, iron chelation and ability to inhibit lipid peroxidation in both liver and brain homogenates of rats. Also, the effect of SAGU on MDA level, an indicator of lipid peroxidation and activity of superoxide dismutase (SOD) and catalase (CAT) were determined in heart and kidney of rat exposed to alloxan (150mg/kg) for 21 days. Results: SAGU exhibited potent and concentration dependent free radical-scavenging activity (IC50/ABTS = 290.12 ± 1.34µg/ml). Reductive and iron chelation abilities also increase with increase in SAGU concentration. SAGU also inhibited peroxidation of hepatic and cerebral lipids subjected to iron oxidative assault. In addit...
The effects of saponin from the fruits of Solanum anguivi (SAS) on body weight, serum and liver s... more The effects of saponin from the fruits of Solanum anguivi (SAS) on body weight, serum and liver superoxide dismutase (SOD), catalase and malondialdehyde (MDA) of normal rats were investigated. Saponin from Solanum anguivi were administered by gavages to experimental rats at dosages of 20 mg/kg, 40 mg/kg, 60 mg/kg, 80 mg/kg and 100 mg/kg body weight, over a period of 21 days. A non significant increase (p<0.05) in weights of the treated animals was observed by the third week. Treatment had no significant effect (p<0.05) on serum activities of catalase, but caused statistically significant increase in SOD and decrease in MDA level at 80 and 100 mg/kg dosages in rats. A dose-dependent and statistically significant increase (p<0.05) in the hepatic activities of catalase and SOD as well as decrease in concentration of MDA was observed in rats administered 40-100 mg/kg dose of SAS . The result suggests that saponin from the fruit of S. anguivi has antioxidant and antiperoxidative...
The proximate analysis, mineral composition, amino acid composition and the anti- nutrient conten... more The proximate analysis, mineral composition, amino acid composition and the anti- nutrient content in leaf of Cnidoscolus aconitifolius was determined. The result showed that Cnidoscolus aconitifolius leaf has a high percentage of carbohydrate 35.70±2.00, protein 18.73±0.65, Ash 13.74±0.76, moisture con-tent 9.49±1.20, crude fibre 9.68±0.93. Amino acid concentrations present include Lys. 5.05±0.13, His 2.60±0.37, NH3 is nil, Arg 5.17±0.15, Asp 8.50±0.48, Thr 3.70±0.25, Ser 3.36±0.37, Glu 13.50±0.74, Pro 3.50±0.29, Gly 4.10±0.02, Ala 4.60±0.11, Cys 1.19±0.48, measured in g/100g. Glutamic acid have the highest concentration while cystine have the lowest concentra-tion. Anti –nutrient present are in low concentration, they include phytin phosphorus (2.67mg/100g), phytic acid (9.47mg/100g), oxalate (2.005mg/100g) and tannin(0.24mg/100g). The average values for Ca, Mg, Na, K, Fe, Zn and P were 400.80, 219.96, 725.44, 194.46, 0.57, 437.44, 0.13, 0.03mg/100g dry sample respectively. Sodium...
The ability of the aqueous extract of flesh and seed of Solanum anguivi Lam fruit (African eggpla... more The ability of the aqueous extract of flesh and seed of Solanum anguivi Lam fruit (African eggplant) used in folk medicine to treat diabetes and hypertension to inhibit Fe 2+ and SNP induced lipid peroxidation in rats brain in vitro was determined. The total phenol, total flavonoid, vitamin C content, ferric reducing antioxidant property as well as Fe 2+ chelating ability were also determined. The results of this study revealed that aqueous extract of Solanum anguivi fruit (flesh and seed) cause a significant decrease (P<0.05) in the MDA production in rats brain when compared with control. The inhibitory effect of both flesh and seeds of Solanum anguivi on lipid peroxidation could be attributed to the phenol (flesh, 7.13 ± 0.73mg/g GAE, seed 8.20 ± 0.32 mg/g GAE), total flavonoid ( flesh 3.53 ± 0.49mg/g QE, seed 1.62 ± 0.61mg/g QE) and vitamin C content (flesh 12.85 ± 0.20mg/g, seed 14.92 ± 0.11 mg/g), as well as ferric reducing antioxidant property and Fe 2+ - chelating ability....
Solanum anguivi fruit saponin has antidiabetic property via interference with cellular energy met... more Solanum anguivi fruit saponin has antidiabetic property via interference with cellular energy metabolism and inhibition of reactive oxygen species (ROS) generation. In the current study, brain specific in vitro anti-oxidant role of S. anguivi saponin was investigated in the P2 synaptosomal fraction of rat brain. Using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide reduction assay, S. anguivi saponin concentration- dependently (10-200 µg/ml) reversed Fe(2+) and sodium nitroprusside- induced decrease in mitochondrial activity via inhibition of ROS production, ROS-induced oxidation of protein and non-protein thiol-containing molecules and lipid peroxidation as measured by thiobarbituric acid reactive substances levels. Conclusively, S. anguivi fruit saponin represents a class of natural compounds with the ability to reverse synaptosomal disruption, loss of mitochondrial integrity and function often associated with the progression of Huntington's disease, Alzheimer dis...
Indian journal of clinical biochemistry : IJCB, 2002
Dietary spice components ofCurcuma longa andAbroma augusta have been screened for their protectiv... more Dietary spice components ofCurcuma longa andAbroma augusta have been screened for their protective effect against reactive oxygen species induced lipid peroxidation. They have been found to be efficient antioxidant when administered in combination. The purpose of the study was to investigate the effect of oral administration (300mg/Kg) of the aqueous extract of turmeric whose active ingredient isCurcumin andAbromine powder as a hypoglycemic agent mixed with diet. The effect of this aqueous extract on blood glucose, lipid peroxidation (LPO) and the antioxidant defense system in rat tissues like liver, lung, kidney and brain was studied for 8 weeks in streptozotocin induced diabetic rats. The administration of an aqueous extract of turmeric and abromine powder resulted in a significant reduction in blood glucose and an increase in total haemoglobin. The aqueous extract also resulted in decreased free radical formation in the tissues studied.The decrease in thiobarbituric acid reactive...
Asian Pacific journal of tropical biomedicine, 2013
To evaluate the antioxidant and radical scavenging activities of Solanum anguivi fruit (SAG) and ... more To evaluate the antioxidant and radical scavenging activities of Solanum anguivi fruit (SAG) and its possible effect on mitochondrial permeability transition pore as well as mitochondrial membrane potential (ΔΨm) isolated from rat liver. Antioxidant activity of SAG was assayed by using 2,2-diphenyl-1-picrylhydrazyl (DPPH), reducing power, iron chelation and ability to inhibit lipid peroxidation in both liver and brain homogenate of rats. Also, the effect of SAG on mitochondrial membrane potential and mitochondrial swelling were determined. Identification and quantification of bioactive polyphenolics was done by HPLC-DAD. SAG exhibited potent and concentration dependent free radical-scavenging activity (IC50/DPPH=275.03±7.8 μg/mL). Reductive and iron chelation abilities also increase with increase in SAG concentration. SAG also inhibited peroxidation of cerebral and hepatic lipids subjected to iron oxidative assault. SAG protected against Ca(2+) (110 μmol/L)-induced mitochondrial swe...
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