American Journal of Pharmacotherapy and Pharmaceutical Sciences
Objectives: Inflammation and pain among other comorbid conditions are prominent clinical complica... more Objectives: Inflammation and pain among other comorbid conditions are prominent clinical complications associated with sickle cell disease (SCD). Despite significant improvement in the understanding of SCD pathophysiology, adverse effects of current treatment options are of great concerns. Faradin® (TD) is a polyherbal mixture used in the management of SCD. This study evaluates the acute toxicity, antinociceptive, and anti-inflammatory actions of TD. Materials and Methods: Acute toxicity study of TD was conducted according to test guidelines-423 of the Organization for Economic, Cooperation, and Development. Anti-inflammatory effect was assessed with carrageenan-induced paw edema and xylene-induced ear edema while antinociceptive effect was assessed using tail immersion, acetic acid-induced writhing, and formalin-induced nociceptive methods. Results: Oral administration of TD showed no acute toxic behavior. TD showed non-dose-related inhibition of inflammation in carrageenan- and xy...
Background: Parkinson disease (PD) and Alzheimer’s disease (AD) are progressive neurodegenerative... more Background: Parkinson disease (PD) and Alzheimer’s disease (AD) are progressive neurodegenerative disorders characterized by loss of selective neurons in discreet part of the brain. The peptide angiotensin II (Ang II) plays significant role in hippocampal and striatal neurons degeneration through the generation of reactive oxygen species. Blockade of the angiotensin converting enzyme or ATI receptors provides protection in animal models of neurodegenerative diseases. In the present study, the neuroprotective effect of captopril was investigated in Drosophila melanogaster model using the UAS-GAL4 system to express the synuclein and Aβ42 peptide in the flies’ neurons. Methods: The disease causing human Aβ42 peptide or α-syn was expressed pan-neuronally (elav-GAL4) or dopamine neuron (DDC-GAL4) using the UAS-GAL4 system. Flies were either grown in food media with or without captopril (1, 5, or 10µM). This was followed by fecundity, larva motility, negative geotaxis assay (climbing) and...
Ethnopharmacological relevance: The leaf Q3 of Alchornea cordifolia (Euphorbiaceae) is used in tr... more Ethnopharmacological relevance: The leaf Q3 of Alchornea cordifolia (Euphorbiaceae) is used in traditional African medicine in the treatment of various neurological and psychiatric disorders including depression. Previous studies have shown its potent antidepressant-like effect in the forced swimming test (FST). To investigate the involvement of monoaminergic systems in the antidepressant-like effect elicited by hydroethanolic leaf extract of Alchornea cordifolia (HeAC) in the FST. Materials and methods: HeAC (25-400 mg/kg, p.o.) was administered 1 h before the FST. To investigate the contribution of monoaminergic systems to antidepressant-like effect, receptors antagonists were injected 15 min before oral administration of HeAC (200 mg/kg) to mice and 1 h thereafter, subjected to FST. Results: HeAC (200 and 400 mg/kg, p.o.) produced dose dependent and significant (P o0.001) antidepressant-like effect, in the FST, without accompanying changes in spontaneous locomotor activities in the open-field test. The anti-immobility effect of HeAC (200 mg/kg) in the FST was prevented by pretreatment of mice with SCH 23390 (0.05 mg/kg, s.c., a dopamine D 1 receptor antagonist), sulpiride (50 mg/kg, i.p., a dopamine D 2 receptor antagonist), prazosin (1 mg/kg, i.p., an α 1-adrenoceptor antagonist), yohimbine (1 mg/kg, i.p., an α 2-adrenoceptor antagonist), and GR 127993 (5-HT 1B receptor antagonist). Similarly, 3 days intraperitoneal injection of p-chlorophenylalanine (pCPA, 150 mg/kg, i.p., an inhibitor of serotonin synthesis) prevented the antidepressant-like effect elicited by HeAC. The combination of subeffective doses of imipramine (5 mg/kg, p.o.) or fluoxetine (5 mg/kg, p.o.), with HeAC (25 mg/kg, p.o., subeffective dose) produced a synergistic antidepressant-like effect in the FST. Conclusion: The hydroethanolic extract of Alchornea cordifolia possesses antidepressant-like effect mediated through interaction with dopamine (D 1 and D 2), noradrenergic (α 1 and α 2 adrenoceptors), and serotonergic (5HT 1B receptors) systems. Also, the potentiation of the anti-immobility effect of conventional antidepressants (fluoxetine and imipramine) by Alchornea cordifolia suggest potential therapeutic effect in depression.
The root decoction of Cnestis ferruginea (CF) Vahl DC (Connaraceae) is used in traditional Africa... more The root decoction of Cnestis ferruginea (CF) Vahl DC (Connaraceae) is used in traditional African medicine in the management of psychiatric disorders. This study presents the antidepressant and anxiolytic effects of amentoflavone (CF-2) isolated from the root extract of C. ferruginea. The antidepressant effect was studied using the forced swimming (FST) and tail suspension tests (TST) while the hole-board, elevated plus maze (EPM) and light/dark tests were used to evaluate the anxiolytic effect. Acute treatment with CF extract and amentoflavone significantly (p b 0.001) reduced the duration of immobility in FST and TST with peak effects observed at 100 and 50 mg/kg respectively in comparison to control treated. Antidepressant effects of CF and amentoflavone were significantly higher (p b 0.05) when compared to imipramine in FST but comparable to the fluoxetine treated group in TST. The pretreatment of mice with metergoline (4 mg/kg, i.p., a 5-HT2 receptor antagonist), prazosin (62.5 μg/ kg, i.p., an α1-adrenoceptor antagonist), and yohimbine (1 mg/kg, i.p., an α2-adrenoceptor antagonist), but not sulpiride (50 mg/kg, i.p., a dopamine D2 receptor antagonist), cyproheptadine (3 mg/kg, i.p., a 5-HT2 receptor antagonist), atropine (1 mg/kg, i.p., a muscarinic receptor antagonist) 15 mins before the administration of amentoflavone (50 mg/kg; p.o.) significantly prevented its antiimmobility effect in the FST. CF extract and CF-2 significantly (p b 0.05) attenuated anxiety by increasing the number of head-dips in the hole-board test, the time spent on the open arms in the EPM, and the exploration of the light chamber in the light/dark test. Pretreatment with flumazenil (3 mg/kg, i.p., ionotropic GABA receptor antagonist) 15 min before oral administration of amentoflavone (25 mg/kg) significantly reduced the time spent in the open arms in EPM. It is concluded from the results obtained that amentoflavone produces its antidepressant effect through interaction with 5-HT2 receptor and α1-, and α2-adrenoceptors while the anxiolytic effect involved the ionotropic GABA receptor.
Background: Olax subscorpioidea Oliv. (Olacaceae) is a medicinal plant commonly used in tradition... more Background: Olax subscorpioidea Oliv. (Olacaceae) is a medicinal plant commonly used in traditional medicine to relieve pain in inflammatory processes. Objective: In the present study, the in vivo anti-inflammatory and antinociceptive effects of aqueous leaf extract of Olax subscorpioidea (OLS) and its possible mechanisms of action were investigated. Methods: OLS (50, 100, 200, and 400 mg/kg, p.o.) was administered 1 h before injection of 0.6%v/v acetic v acid (10 ml/kg, i.p.), 1% / formalin (20 µl) or tail flick tests to evaluate antinociceptive effect while acute v anti-inflammatory effect was investigated using xylene-induced ear and carrageenan-induced paw edema models, chronic anti-inflammatory effect was investigated using the complete Freund's adjuvant (CFA) test in rats. Results: OLS (50-400 mg/kg) significantly (P<0.001) reduced acetic acid-induced writhes (68.28%, 50 mg/kg), duration of paw licking/biting by 73.10% (early phase) and 70.50% (late phase), 50 mg/kg) in...
Background:Neurodegenerative disorders (ND) are characterized by progressive loss of selectively ... more Background:Neurodegenerative disorders (ND) are characterized by progressive loss of selectively vulnerable populations of neurons, which contrasts with select static neuronal loss. Self-association of amyloid-beta(Aβ)orα-synucleinpeptidesintofibrilsand/orplaquelikeaggregatescauses neurotoxicity. Hence, identification of specific compounds that either inhibit the formation of Aβ or α-syn-fibrils makes an appealing therapeutic strategy in the development of drugs. In the present study, we investigated the protective effect of vildagliptin (VDG) (oral hypoglycemic agent) on genetic models of ND in Drosophila melanogaster. Methods: The disease causing human Aβ42 peptide or α-syn was expressed pan-neuronally (elav-GAL4) or dopamine neurons (DDC-GAL4) using the UAS-GAL4 system. Flies were either grown in food media with or without vildagliptin (1, 5, or 10μM). This was followed by fecundity, larva motility and negative geotaxis assay (climbing) as a measure of neurodegeneration. Results:...
ABSTRACTBackgroundThe rise in occurrence of hypertension, a non-communicable disease and a major ... more ABSTRACTBackgroundThe rise in occurrence of hypertension, a non-communicable disease and a major factor for chronic renal failure, cardiovascular disease, and stroke, which most times lead to sudden death is worrisome. Resistant hypertension is more common and may have no symptoms at all for months or years, but then can cause heart attack, stroke, and vision and kidney damage. Prevention and quick management of hypertension are therefore essential in reducing the risk of these debilitating ailments. Aqueous and ethanolic extracts of the leaves of Clerodendrum chinensis (AeC and EeC) are used by local communities of West Africa as medicine for rapid antihypertensive actions. We aim to discover the scientific basis for the use of the herb as medicine.MethodsThis work investigates the antihypertensive effects of AeC and EeC in L-Arginine Methyl Ester Hydrochloride (L-NAME)-induced hypertensive rats Acetylcholine, L-Arginine and Sodium Nitroprusside were used as standards. All results ...
Medical principles and practice : international journal of the Kuwait University, Health Science Centre, Jan 17, 2017
This study sought to evaluate the protective effect of ethanolic leaf extract of Moringa Oleifera... more This study sought to evaluate the protective effect of ethanolic leaf extract of Moringa Oleifera (M. oleifera ) on testosterone-induced benign prostatic hyperplasia (BPH) in male Sprague-Dawley rats. BPH was induced in rats by administration of testosterone propionate (3 mg/kg, s.c., in olive oil) for 4 weeks. M. oleifera (50, 100 or 200 mg/kg), celecoxib (20 mg/kg) or M. oleifera (50 mg/kg) + celecoxib (20 mg/kg) were orally administered daily 15 min before testosterone. On day 29, blood was collected to measure the levels of serum testosterone and prostate specific antigen before the animals were sacrificed. The prostates were weighed, assayed and histologically examined. M. oleifera significantly reduced testosterone-induced increase in prostate weight (20.16%), prostatic index (65.85%), serum testosterone (72.86%) and prostate specific antigen (48.49%). Testosterone caused significant increase in malondialdehyde (73.00%) as well as reduction in glutathione (62.50%), superoxide ...
Diabetes and obesity have been reported to alter sex steroid hormone metabolism. In this study, a... more Diabetes and obesity have been reported to alter sex steroid hormone metabolism. In this study, an attempt was made to investigate the protective effect of atorvastatin (ATR) in combination with celecoxib (CEL) or pioglitazone (PIO) on testosterone-induced BPH in rats. Male Wistar rats (200-250 g) were randomly divided into nine groups (n = 8) and orally treated as follows for 28 consecutive days: group 1: vehicle control (10 mL/kg); group 2: vehicle testosterone (10 mL/kg); groups 3 - 5: ATR (0.5, 2.5, and 5 mg/kg, respectively); group 6: CEL (20 mg/kg); group 7: PIO (20 mg/kg); and groups 8-9: ATR 0.5 mg/kg, and 15 min later, animals were given CEL (20 mg/kg) or PIO (20 mg/kg), respectively. One hour post-treatment, animals in groups 2-9 were given testosterone propionate (3 mg/kg, s.c.). Twenty-four hours after last treatment on day 28, blood was collected for serum testosterone and prostate-specific antigen (PSA) analysis. Prostate was harvested for biochemical and histological assays. Subcutaneous injection of testosterone increased serum levels of testosterone and PSA which was ameliorated by pretreatments of rat with ATR, celecoxib, or pioglitazone. Similarly, testosterone-induced increase in MDA and reduction in the activity of GSH, superoxide dismutase (SOD), and catalase were attenuated by ATR. Conversely, celecoxib or pioglitazone treatment failed to affect the activity of antioxidant enzymes. The histology of the prostate showed significant improvement in prostatic cells of ATR, celecoxib, or pioglitazone treated. Findings from the study showed that atorvastatin attenuated testosterone-induced BPH. Moreover, synergistic effect was observed when atorvastatin was combined with celecoxib.
Benign prostatic hyperplasia (BPH) is a common health problem in ageing men. This study was carri... more Benign prostatic hyperplasia (BPH) is a common health problem in ageing men. This study was carried out to investigate the protective effect of telmisartan on testosterone-induced BPH in rats. Fifty-four male Wistar rats (200-250 g) were randomly divided into nine groups (n = 6) and orally treated for 28 consecutive days: group 1 - vehicle normal, olive oil (10 mL/kg); group 2 - BPH model control (10 mL/kg); groups 3-5 - telmisartan (5, 10 or 20 mg/kg, respectively); group 6 - pioglitazone (20 mg/kg); group 7 - celecoxib (20 mg/kg); group 8 - combination of telmisartan (5 mg/kg) and pioglitazone (20 mg/kg); group 9 - combination of telmisartan (5 mg/kg) and celecoxib (20 mg/kg). Animals in groups 2-9 were given testosterone propionate in olive oil (3 mg/kg) subcutaneously 15 min after pretreatments. On day 29, blood was collected for the estimation of serum testosterone and prostate-specific antigen (PSA). The prostates were excised, weighed and subjected to biochemical and histological studies. Testosterone injection induced significant increase in prostatic index, serum testosterone and PSA suggesting BPH as well as increased prostate oxidative stress which were ameliorated with the pretreatment of rats with telmisartan or co-administration of celecoxib and pioglitazone. Histological examination showed that testosterone disrupted the morphology of the prostate epithelial cells evidenced in the involution of the epithelial lining of the acini into the lumen indicating BPH which was reversed by telmisartan. Findings from this study showed that telmisartan alone or in combination with pioglitazone prevented the development of testosterone-induced prostatic hyperplasia.
Gymnosporia heterophylla (Celastraceae) is an African medicinal plants used to treat painful and ... more Gymnosporia heterophylla (Celastraceae) is an African medicinal plants used to treat painful and inflammatory diseases with partial scientific validation. Solvent extractions followed by repeated chromatographic purification of the G. heterophylla aerial parts led to the isolation of one new β-dihydroagarofuran sesquiterpene alkaloid (1), and two triterpenes (2-3). In addition, eight known compounds including one β-dihydroagarofuran sesquiterpene alkaloid (4), and six triterpenes (5-10) were isolated. All structures were determined through extensive analysis of the NMR an MS data as well as by comparison with literature data. These compounds were evaluated for the anti-inflammatory activities against COX-1 and -2 inhibitory potentials. Most of the compound isolated showed non selective COX inhibitions except for 3-Acetoxy-1β-hydroxyLupe-20(29)-ene (5), Lup-20(29)-ene-1β,3β-diol (6) which showed COX-2 selective inhibition at 0.54 (1.85), and 0.45 (2.22) IC50, in mM (Selective Index),...
Nigerian journal of physiological sciences : official publication of the Physiological Society of Nigeria, 2015
The leaves of Clausena anisata (Willd.) Hook. f. ex Benth (Rutaceae) is used in Traditional Afric... more The leaves of Clausena anisata (Willd.) Hook. f. ex Benth (Rutaceae) is used in Traditional African medicine for the treatment of various ailments including arthritis. The present study sought to investigate the antinociceptive and anti-arthritic properties of hydroethanolic leaf extract of Clausena anisata (HeCA). HeCA (100, 200 or 400 mg/kg, p.o.) was administered 1 h before intraplantar injection of formalin 1%v/v in saline to evaluate antinociceptive effect. Moreover, its possible mechanism of antinociceptive action was investigated through pretreatment of mice with antagonists of receptors implicated in nociception. Anti¬inflammatory effect of the extract was investigated using the carrageenan-induced paw oedema and complete Freund's adjuvant (CFA)-induced arthritis models in rats. HeCA (400 mg/kg) treatment significantly reduced the duration of paw licking/biting during both in the early (42.12%) and late (75.79%) phases of formalin-induced nociception. However, the antino...
We have earlier reported the antinociceptive and anti-inflammatory effects of Alafia barteri Oliv... more We have earlier reported the antinociceptive and anti-inflammatory effects of Alafia barteri Oliver (Apocynaceae) in rodents but its mechanism of actionsare yet to be elucidated. This study sought toinvestigate the involvement of monoaminergic, nitric oxide-cyclic GMP-K+ channel and opioidergic pathways in its mechanism of actions. methanol root extract of Alafia barteri (ALA) (100-400 mg/kg, p.o.) was given 1 h before administration of chemical or thermal-induced nociception andhistamine/serotonin-induced inflammation. The mechanism of the antinociceptive effect was investigated through intraperitoneal injection of prazosin (62.5 pg/kg; alpha1-adrenoceptor antagonist), yohimbine (1 mg/kg; alpha2 adrenoceptor antagonist) N(G)-nitro-L-arginine (L-NNA) (20 mg/kg; nitric-oxide-synthase inhibitor), c y p r o h e p t a d i n e (10 mg/kg; 5-HT2R antagonist), glibenclamide (10 mg/kg; ATP-sensitive K+ -channel inhibitor), or naloxone (5 mg/kg; opioid-receptor antagonist) before the nocicept...
We have earlier reported antidepressant-like effect of Cnestis ferruginea and its bioflavonoid co... more We have earlier reported antidepressant-like effect of Cnestis ferruginea and its bioflavonoid constituent, amentoflavone in behavioural paradigms but its effects on neurochemical and neuroendocrine systems are yet to be elucidated. This study sought to investigate the effect of subchronic treatment of C. ferruginea (CF) on monoamines system, hypothalamo-pituitary adrenal axis and nitrosative/oxidative stresses. Male albino rats (150-200g) randomly divided into seven groups; Group I: vehicle treated (0.2%(v)/v Tween 80 in normal saline (10ml/kg; p.o.; unstressed), Group II: vehicle treated+restraint stress, Group III: imipramine (20mg/kg; p.o.), Group IV-VI: CF (12.5, 50, or 100mg/kg; p.o., respectively), Group VII: CF 6.25+imipramine 5mg/kg. One hour post-treatment, animals were subjected to 20min restraint stress and 6min, forced swim test (FST) for a period of 14 days. CF (12.5, 50 and 100mg/kg) produced significant reduction in immobility time and an increase in climbing behaviour. CF attenuated repeated restraint stress×FST-induced serum corticosterone [F(6,28)=5.45,P&lt;0.01]. Exposure of rats to FST+restraint stress paradigms produced significant (P&lt;0.05) increase in malondialdehyde and nitrite level, also reduced the glutathione level and superoxide dismutase activity which was reversed by subchronic treatment of rats with CF. Restraint stress×FST significantly decreased NA, DA and 5-HT concentrations, with increased DA and 5-HT turnover ratios in discrete brain regions which was ameliorated by CF or imipramine subchronic treatment. These results suggest that the antidepressant-like effect of C. ferruginea involved enhancement of monoamines and antioxidant as well as normalization of neuroendocrine systems.
American Journal of Pharmacotherapy and Pharmaceutical Sciences
Objectives: Inflammation and pain among other comorbid conditions are prominent clinical complica... more Objectives: Inflammation and pain among other comorbid conditions are prominent clinical complications associated with sickle cell disease (SCD). Despite significant improvement in the understanding of SCD pathophysiology, adverse effects of current treatment options are of great concerns. Faradin® (TD) is a polyherbal mixture used in the management of SCD. This study evaluates the acute toxicity, antinociceptive, and anti-inflammatory actions of TD. Materials and Methods: Acute toxicity study of TD was conducted according to test guidelines-423 of the Organization for Economic, Cooperation, and Development. Anti-inflammatory effect was assessed with carrageenan-induced paw edema and xylene-induced ear edema while antinociceptive effect was assessed using tail immersion, acetic acid-induced writhing, and formalin-induced nociceptive methods. Results: Oral administration of TD showed no acute toxic behavior. TD showed non-dose-related inhibition of inflammation in carrageenan- and xy...
Background: Parkinson disease (PD) and Alzheimer’s disease (AD) are progressive neurodegenerative... more Background: Parkinson disease (PD) and Alzheimer’s disease (AD) are progressive neurodegenerative disorders characterized by loss of selective neurons in discreet part of the brain. The peptide angiotensin II (Ang II) plays significant role in hippocampal and striatal neurons degeneration through the generation of reactive oxygen species. Blockade of the angiotensin converting enzyme or ATI receptors provides protection in animal models of neurodegenerative diseases. In the present study, the neuroprotective effect of captopril was investigated in Drosophila melanogaster model using the UAS-GAL4 system to express the synuclein and Aβ42 peptide in the flies’ neurons. Methods: The disease causing human Aβ42 peptide or α-syn was expressed pan-neuronally (elav-GAL4) or dopamine neuron (DDC-GAL4) using the UAS-GAL4 system. Flies were either grown in food media with or without captopril (1, 5, or 10µM). This was followed by fecundity, larva motility, negative geotaxis assay (climbing) and...
Ethnopharmacological relevance: The leaf Q3 of Alchornea cordifolia (Euphorbiaceae) is used in tr... more Ethnopharmacological relevance: The leaf Q3 of Alchornea cordifolia (Euphorbiaceae) is used in traditional African medicine in the treatment of various neurological and psychiatric disorders including depression. Previous studies have shown its potent antidepressant-like effect in the forced swimming test (FST). To investigate the involvement of monoaminergic systems in the antidepressant-like effect elicited by hydroethanolic leaf extract of Alchornea cordifolia (HeAC) in the FST. Materials and methods: HeAC (25-400 mg/kg, p.o.) was administered 1 h before the FST. To investigate the contribution of monoaminergic systems to antidepressant-like effect, receptors antagonists were injected 15 min before oral administration of HeAC (200 mg/kg) to mice and 1 h thereafter, subjected to FST. Results: HeAC (200 and 400 mg/kg, p.o.) produced dose dependent and significant (P o0.001) antidepressant-like effect, in the FST, without accompanying changes in spontaneous locomotor activities in the open-field test. The anti-immobility effect of HeAC (200 mg/kg) in the FST was prevented by pretreatment of mice with SCH 23390 (0.05 mg/kg, s.c., a dopamine D 1 receptor antagonist), sulpiride (50 mg/kg, i.p., a dopamine D 2 receptor antagonist), prazosin (1 mg/kg, i.p., an α 1-adrenoceptor antagonist), yohimbine (1 mg/kg, i.p., an α 2-adrenoceptor antagonist), and GR 127993 (5-HT 1B receptor antagonist). Similarly, 3 days intraperitoneal injection of p-chlorophenylalanine (pCPA, 150 mg/kg, i.p., an inhibitor of serotonin synthesis) prevented the antidepressant-like effect elicited by HeAC. The combination of subeffective doses of imipramine (5 mg/kg, p.o.) or fluoxetine (5 mg/kg, p.o.), with HeAC (25 mg/kg, p.o., subeffective dose) produced a synergistic antidepressant-like effect in the FST. Conclusion: The hydroethanolic extract of Alchornea cordifolia possesses antidepressant-like effect mediated through interaction with dopamine (D 1 and D 2), noradrenergic (α 1 and α 2 adrenoceptors), and serotonergic (5HT 1B receptors) systems. Also, the potentiation of the anti-immobility effect of conventional antidepressants (fluoxetine and imipramine) by Alchornea cordifolia suggest potential therapeutic effect in depression.
The root decoction of Cnestis ferruginea (CF) Vahl DC (Connaraceae) is used in traditional Africa... more The root decoction of Cnestis ferruginea (CF) Vahl DC (Connaraceae) is used in traditional African medicine in the management of psychiatric disorders. This study presents the antidepressant and anxiolytic effects of amentoflavone (CF-2) isolated from the root extract of C. ferruginea. The antidepressant effect was studied using the forced swimming (FST) and tail suspension tests (TST) while the hole-board, elevated plus maze (EPM) and light/dark tests were used to evaluate the anxiolytic effect. Acute treatment with CF extract and amentoflavone significantly (p b 0.001) reduced the duration of immobility in FST and TST with peak effects observed at 100 and 50 mg/kg respectively in comparison to control treated. Antidepressant effects of CF and amentoflavone were significantly higher (p b 0.05) when compared to imipramine in FST but comparable to the fluoxetine treated group in TST. The pretreatment of mice with metergoline (4 mg/kg, i.p., a 5-HT2 receptor antagonist), prazosin (62.5 μg/ kg, i.p., an α1-adrenoceptor antagonist), and yohimbine (1 mg/kg, i.p., an α2-adrenoceptor antagonist), but not sulpiride (50 mg/kg, i.p., a dopamine D2 receptor antagonist), cyproheptadine (3 mg/kg, i.p., a 5-HT2 receptor antagonist), atropine (1 mg/kg, i.p., a muscarinic receptor antagonist) 15 mins before the administration of amentoflavone (50 mg/kg; p.o.) significantly prevented its antiimmobility effect in the FST. CF extract and CF-2 significantly (p b 0.05) attenuated anxiety by increasing the number of head-dips in the hole-board test, the time spent on the open arms in the EPM, and the exploration of the light chamber in the light/dark test. Pretreatment with flumazenil (3 mg/kg, i.p., ionotropic GABA receptor antagonist) 15 min before oral administration of amentoflavone (25 mg/kg) significantly reduced the time spent in the open arms in EPM. It is concluded from the results obtained that amentoflavone produces its antidepressant effect through interaction with 5-HT2 receptor and α1-, and α2-adrenoceptors while the anxiolytic effect involved the ionotropic GABA receptor.
Background: Olax subscorpioidea Oliv. (Olacaceae) is a medicinal plant commonly used in tradition... more Background: Olax subscorpioidea Oliv. (Olacaceae) is a medicinal plant commonly used in traditional medicine to relieve pain in inflammatory processes. Objective: In the present study, the in vivo anti-inflammatory and antinociceptive effects of aqueous leaf extract of Olax subscorpioidea (OLS) and its possible mechanisms of action were investigated. Methods: OLS (50, 100, 200, and 400 mg/kg, p.o.) was administered 1 h before injection of 0.6%v/v acetic v acid (10 ml/kg, i.p.), 1% / formalin (20 µl) or tail flick tests to evaluate antinociceptive effect while acute v anti-inflammatory effect was investigated using xylene-induced ear and carrageenan-induced paw edema models, chronic anti-inflammatory effect was investigated using the complete Freund's adjuvant (CFA) test in rats. Results: OLS (50-400 mg/kg) significantly (P<0.001) reduced acetic acid-induced writhes (68.28%, 50 mg/kg), duration of paw licking/biting by 73.10% (early phase) and 70.50% (late phase), 50 mg/kg) in...
Background:Neurodegenerative disorders (ND) are characterized by progressive loss of selectively ... more Background:Neurodegenerative disorders (ND) are characterized by progressive loss of selectively vulnerable populations of neurons, which contrasts with select static neuronal loss. Self-association of amyloid-beta(Aβ)orα-synucleinpeptidesintofibrilsand/orplaquelikeaggregatescauses neurotoxicity. Hence, identification of specific compounds that either inhibit the formation of Aβ or α-syn-fibrils makes an appealing therapeutic strategy in the development of drugs. In the present study, we investigated the protective effect of vildagliptin (VDG) (oral hypoglycemic agent) on genetic models of ND in Drosophila melanogaster. Methods: The disease causing human Aβ42 peptide or α-syn was expressed pan-neuronally (elav-GAL4) or dopamine neurons (DDC-GAL4) using the UAS-GAL4 system. Flies were either grown in food media with or without vildagliptin (1, 5, or 10μM). This was followed by fecundity, larva motility and negative geotaxis assay (climbing) as a measure of neurodegeneration. Results:...
ABSTRACTBackgroundThe rise in occurrence of hypertension, a non-communicable disease and a major ... more ABSTRACTBackgroundThe rise in occurrence of hypertension, a non-communicable disease and a major factor for chronic renal failure, cardiovascular disease, and stroke, which most times lead to sudden death is worrisome. Resistant hypertension is more common and may have no symptoms at all for months or years, but then can cause heart attack, stroke, and vision and kidney damage. Prevention and quick management of hypertension are therefore essential in reducing the risk of these debilitating ailments. Aqueous and ethanolic extracts of the leaves of Clerodendrum chinensis (AeC and EeC) are used by local communities of West Africa as medicine for rapid antihypertensive actions. We aim to discover the scientific basis for the use of the herb as medicine.MethodsThis work investigates the antihypertensive effects of AeC and EeC in L-Arginine Methyl Ester Hydrochloride (L-NAME)-induced hypertensive rats Acetylcholine, L-Arginine and Sodium Nitroprusside were used as standards. All results ...
Medical principles and practice : international journal of the Kuwait University, Health Science Centre, Jan 17, 2017
This study sought to evaluate the protective effect of ethanolic leaf extract of Moringa Oleifera... more This study sought to evaluate the protective effect of ethanolic leaf extract of Moringa Oleifera (M. oleifera ) on testosterone-induced benign prostatic hyperplasia (BPH) in male Sprague-Dawley rats. BPH was induced in rats by administration of testosterone propionate (3 mg/kg, s.c., in olive oil) for 4 weeks. M. oleifera (50, 100 or 200 mg/kg), celecoxib (20 mg/kg) or M. oleifera (50 mg/kg) + celecoxib (20 mg/kg) were orally administered daily 15 min before testosterone. On day 29, blood was collected to measure the levels of serum testosterone and prostate specific antigen before the animals were sacrificed. The prostates were weighed, assayed and histologically examined. M. oleifera significantly reduced testosterone-induced increase in prostate weight (20.16%), prostatic index (65.85%), serum testosterone (72.86%) and prostate specific antigen (48.49%). Testosterone caused significant increase in malondialdehyde (73.00%) as well as reduction in glutathione (62.50%), superoxide ...
Diabetes and obesity have been reported to alter sex steroid hormone metabolism. In this study, a... more Diabetes and obesity have been reported to alter sex steroid hormone metabolism. In this study, an attempt was made to investigate the protective effect of atorvastatin (ATR) in combination with celecoxib (CEL) or pioglitazone (PIO) on testosterone-induced BPH in rats. Male Wistar rats (200-250 g) were randomly divided into nine groups (n = 8) and orally treated as follows for 28 consecutive days: group 1: vehicle control (10 mL/kg); group 2: vehicle testosterone (10 mL/kg); groups 3 - 5: ATR (0.5, 2.5, and 5 mg/kg, respectively); group 6: CEL (20 mg/kg); group 7: PIO (20 mg/kg); and groups 8-9: ATR 0.5 mg/kg, and 15 min later, animals were given CEL (20 mg/kg) or PIO (20 mg/kg), respectively. One hour post-treatment, animals in groups 2-9 were given testosterone propionate (3 mg/kg, s.c.). Twenty-four hours after last treatment on day 28, blood was collected for serum testosterone and prostate-specific antigen (PSA) analysis. Prostate was harvested for biochemical and histological assays. Subcutaneous injection of testosterone increased serum levels of testosterone and PSA which was ameliorated by pretreatments of rat with ATR, celecoxib, or pioglitazone. Similarly, testosterone-induced increase in MDA and reduction in the activity of GSH, superoxide dismutase (SOD), and catalase were attenuated by ATR. Conversely, celecoxib or pioglitazone treatment failed to affect the activity of antioxidant enzymes. The histology of the prostate showed significant improvement in prostatic cells of ATR, celecoxib, or pioglitazone treated. Findings from the study showed that atorvastatin attenuated testosterone-induced BPH. Moreover, synergistic effect was observed when atorvastatin was combined with celecoxib.
Benign prostatic hyperplasia (BPH) is a common health problem in ageing men. This study was carri... more Benign prostatic hyperplasia (BPH) is a common health problem in ageing men. This study was carried out to investigate the protective effect of telmisartan on testosterone-induced BPH in rats. Fifty-four male Wistar rats (200-250 g) were randomly divided into nine groups (n = 6) and orally treated for 28 consecutive days: group 1 - vehicle normal, olive oil (10 mL/kg); group 2 - BPH model control (10 mL/kg); groups 3-5 - telmisartan (5, 10 or 20 mg/kg, respectively); group 6 - pioglitazone (20 mg/kg); group 7 - celecoxib (20 mg/kg); group 8 - combination of telmisartan (5 mg/kg) and pioglitazone (20 mg/kg); group 9 - combination of telmisartan (5 mg/kg) and celecoxib (20 mg/kg). Animals in groups 2-9 were given testosterone propionate in olive oil (3 mg/kg) subcutaneously 15 min after pretreatments. On day 29, blood was collected for the estimation of serum testosterone and prostate-specific antigen (PSA). The prostates were excised, weighed and subjected to biochemical and histological studies. Testosterone injection induced significant increase in prostatic index, serum testosterone and PSA suggesting BPH as well as increased prostate oxidative stress which were ameliorated with the pretreatment of rats with telmisartan or co-administration of celecoxib and pioglitazone. Histological examination showed that testosterone disrupted the morphology of the prostate epithelial cells evidenced in the involution of the epithelial lining of the acini into the lumen indicating BPH which was reversed by telmisartan. Findings from this study showed that telmisartan alone or in combination with pioglitazone prevented the development of testosterone-induced prostatic hyperplasia.
Gymnosporia heterophylla (Celastraceae) is an African medicinal plants used to treat painful and ... more Gymnosporia heterophylla (Celastraceae) is an African medicinal plants used to treat painful and inflammatory diseases with partial scientific validation. Solvent extractions followed by repeated chromatographic purification of the G. heterophylla aerial parts led to the isolation of one new β-dihydroagarofuran sesquiterpene alkaloid (1), and two triterpenes (2-3). In addition, eight known compounds including one β-dihydroagarofuran sesquiterpene alkaloid (4), and six triterpenes (5-10) were isolated. All structures were determined through extensive analysis of the NMR an MS data as well as by comparison with literature data. These compounds were evaluated for the anti-inflammatory activities against COX-1 and -2 inhibitory potentials. Most of the compound isolated showed non selective COX inhibitions except for 3-Acetoxy-1β-hydroxyLupe-20(29)-ene (5), Lup-20(29)-ene-1β,3β-diol (6) which showed COX-2 selective inhibition at 0.54 (1.85), and 0.45 (2.22) IC50, in mM (Selective Index),...
Nigerian journal of physiological sciences : official publication of the Physiological Society of Nigeria, 2015
The leaves of Clausena anisata (Willd.) Hook. f. ex Benth (Rutaceae) is used in Traditional Afric... more The leaves of Clausena anisata (Willd.) Hook. f. ex Benth (Rutaceae) is used in Traditional African medicine for the treatment of various ailments including arthritis. The present study sought to investigate the antinociceptive and anti-arthritic properties of hydroethanolic leaf extract of Clausena anisata (HeCA). HeCA (100, 200 or 400 mg/kg, p.o.) was administered 1 h before intraplantar injection of formalin 1%v/v in saline to evaluate antinociceptive effect. Moreover, its possible mechanism of antinociceptive action was investigated through pretreatment of mice with antagonists of receptors implicated in nociception. Anti¬inflammatory effect of the extract was investigated using the carrageenan-induced paw oedema and complete Freund's adjuvant (CFA)-induced arthritis models in rats. HeCA (400 mg/kg) treatment significantly reduced the duration of paw licking/biting during both in the early (42.12%) and late (75.79%) phases of formalin-induced nociception. However, the antino...
We have earlier reported the antinociceptive and anti-inflammatory effects of Alafia barteri Oliv... more We have earlier reported the antinociceptive and anti-inflammatory effects of Alafia barteri Oliver (Apocynaceae) in rodents but its mechanism of actionsare yet to be elucidated. This study sought toinvestigate the involvement of monoaminergic, nitric oxide-cyclic GMP-K+ channel and opioidergic pathways in its mechanism of actions. methanol root extract of Alafia barteri (ALA) (100-400 mg/kg, p.o.) was given 1 h before administration of chemical or thermal-induced nociception andhistamine/serotonin-induced inflammation. The mechanism of the antinociceptive effect was investigated through intraperitoneal injection of prazosin (62.5 pg/kg; alpha1-adrenoceptor antagonist), yohimbine (1 mg/kg; alpha2 adrenoceptor antagonist) N(G)-nitro-L-arginine (L-NNA) (20 mg/kg; nitric-oxide-synthase inhibitor), c y p r o h e p t a d i n e (10 mg/kg; 5-HT2R antagonist), glibenclamide (10 mg/kg; ATP-sensitive K+ -channel inhibitor), or naloxone (5 mg/kg; opioid-receptor antagonist) before the nocicept...
We have earlier reported antidepressant-like effect of Cnestis ferruginea and its bioflavonoid co... more We have earlier reported antidepressant-like effect of Cnestis ferruginea and its bioflavonoid constituent, amentoflavone in behavioural paradigms but its effects on neurochemical and neuroendocrine systems are yet to be elucidated. This study sought to investigate the effect of subchronic treatment of C. ferruginea (CF) on monoamines system, hypothalamo-pituitary adrenal axis and nitrosative/oxidative stresses. Male albino rats (150-200g) randomly divided into seven groups; Group I: vehicle treated (0.2%(v)/v Tween 80 in normal saline (10ml/kg; p.o.; unstressed), Group II: vehicle treated+restraint stress, Group III: imipramine (20mg/kg; p.o.), Group IV-VI: CF (12.5, 50, or 100mg/kg; p.o., respectively), Group VII: CF 6.25+imipramine 5mg/kg. One hour post-treatment, animals were subjected to 20min restraint stress and 6min, forced swim test (FST) for a period of 14 days. CF (12.5, 50 and 100mg/kg) produced significant reduction in immobility time and an increase in climbing behaviour. CF attenuated repeated restraint stress×FST-induced serum corticosterone [F(6,28)=5.45,P&lt;0.01]. Exposure of rats to FST+restraint stress paradigms produced significant (P&lt;0.05) increase in malondialdehyde and nitrite level, also reduced the glutathione level and superoxide dismutase activity which was reversed by subchronic treatment of rats with CF. Restraint stress×FST significantly decreased NA, DA and 5-HT concentrations, with increased DA and 5-HT turnover ratios in discrete brain regions which was ameliorated by CF or imipramine subchronic treatment. These results suggest that the antidepressant-like effect of C. ferruginea involved enhancement of monoamines and antioxidant as well as normalization of neuroendocrine systems.
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