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Papers by Patrick Igbinaduwa

Acta Poloniae Pharmaceutica, May 1, 2007

... 1H-pyri-do-[2,3-d]1,3-oxazine-2,4-dione 2a and 1H-pyrido-[3,2-d]1,3-oxazine-2,4-dione 2b were... more ... 1H-pyri-do-[2,3-d]1,3-oxazine-2,4-dione 2a and 1H-pyrido-[3,2-d]1,3-oxazine-2,4-dione 2b were synthesized according to literature procedure (7, 8). Prop-2-ynyl-amine, triethylorthoformate and other reagents were obtained from ... CYRIL USIFOH* and PATRICK IGBINADUWA ...

Tropical Journal of Pharmaceutical Research, Sep 17, 2014

Purpose: To synthesize and characterize palmitoyl amino benzamides, and to evaluate them for poss... more Purpose: To synthesize and characterize palmitoyl amino benzamides, and to evaluate them for possible anti-inflammatory and anti-nociceptive activities. Methods: Palmitoyl amino benzamides were synthesized by the opening of isatoic anhydride ring with respective amino acids (glycine, β-alanine and γ-aminobutyric acid) and the condensation of the product with palmitoyl chloride. The final products were purified on column chromatography, eluting with dichloromethane/ethyl acetate. All the compounds were unequivocally characterized using the combination of infra red (IR), 1H and 13C (nuclear magnetic resonance (NMR), mass spectrometry (MS) and elemental analysis. In vivo anti-inflammatory and anti-nociceptive activities of the synthesized compounds at 20, 50 and 100mg/kg doses were carried out using carrageenan-induced paw oedema in rat and acetic acid-induced writhing in mice, respectively. Aspirin was used at a dose of 100mg/kg as the reference drug. Results: The compounds were obtained in high yield (70-90 %) and purity. The anti-inflammatory results showed a poor activity for the compounds except o-palmitoylamino N-carboxyethyl benzamide which produced significant inhibition (p < 0.05) at a dose of 50 mg/kg (43.8 % oedema inhibition) while the reference drug, aspirin, showed 51.3 % inhibition. The anti-nociceptive study, however, showed good inhibition (p < 0.05) of acetic acid-induced writhing, with o-palmitoylamino Ncarboxymethylbenzamide producing 86.2 % inhibition at 100 mg/kg dose compared with the reference drug (aspirin) which gave 74.3 % inhibition at 100 mg/kg. Conclusion: The findings of this study indicate that the synthesized compounds, though displaying poor anti-inflammatory activity, do possess promising anti-nociceptive activity.

Work has been done to determine the effect of Loranthus bengwensis supplemented diet on food inta... more Work has been done to determine the effect of Loranthus bengwensis supplemented diet on food intake, blood pressure and electrolyte levels in normal and hypertensive rats. Consequently, sixteen albino rats were divided into four groups of four each. The first group were fed on growers mash only (control), the second group on 92% growers mash and 8% NaCl (salt loaded group) the third on 8% NaCl, 8% mistletoe powder and 84% growers mash (salt loaded and mistletoe group) while the fourth on 8% mistletoe powder and 92% growers mash (normal and mistletoe group). The weight changes, daily food intake, faecal output, systolic and diastolic mean arterial and pulse pressures of the animals in various groups were recorded. The Na , K , Cl and + + HCO levels were determined. Results indicate that rats in the salt loaded group had significantly higher 3 systolic, diastolic and mean arterial pressures (P<0.05) but significantly lower pulse pressure (P<0.05) compared with control rats. Rats in the salt loaded and mistletoe group and normal and mistletoe group had lower systolic pressure and lower pulse pressure compared with control rats. Rats fed with salt loaded diet and salt loaded with mistletoe powder had higher Na and Cl levels compared with control but the K and HCO + + 3 concentrations did not differ significantly (P<0.05) from those of control rats. Rats in the three groups recorded higher food intake and faecal output but lower weight gain compared to control rats. The results showed that Loranthus bengwensis significantly reduced (P<0.05) diastolic, systolic and mean arterial pressures as well as Na and Cl concentration but significantly reduced weight gain in normal and hypertensive rat.

Nigerian Journal of Pharmaceutical Research, 2020

Background: Anthocleista djalonensis is a West African plant with several ethnomedicinal uses.Obj... more Background: Anthocleista djalonensis is a West African plant with several ethnomedicinal uses.Objectives: This study evaluated the effect of Anthocleista djalonensis methanol root bark extract on fertility parameters in male rats.Material and Methods: The rats were randomly allotted to four groups (n=5). Group A (control) received distilled water (10 ml/kg), groups B, C, D received oral doses of 100, 200 and 400 mg/kg/day of the extract respectively for 28 days. The mean body, testicular, and epididymal weights; sperm indices; and serum testosterone level were assessed.Results: There were no significant changes on the body weights of the treated rats but their testicular and epididymal weights increased significantly (P˂0.05) at the dose of 400 mg/kg in comparison with the control group. Sperm indices such as sperm count, motility, morphology and viability increased significantly (P˂0.05) at the doses of 200 and 400 mg/kg/day when compared to the control. There was also a significant (P˂0.05) increase in serum testosterone concentration at the dose of 400 mg/kg/day of the extract.Conclusion: The results suggest that the methanol root bark extract of A. djalonensis improves fertility parameters in male rats thereby justifying its use in ethnomedicine.Keywords: Sperm count, testosterone level, spermatogenesis, oxidative stress

Journal of Pharmacy & Bioresources, 2013

ABSTRACT The study assessed the phytochemical, acute toxicity, sub-acute toxicity and blood chemi... more ABSTRACT The study assessed the phytochemical, acute toxicity, sub-acute toxicity and blood chemistry of the aqueous leaf extract of Mucuna pruriens. Powdered leaf of Mucuna pruriens was extracted by maceration. 24 albino mice used for acute toxicity were administered between 1-8 g/kg body weight of the extract while the control group received distilled water. 12 Wistar albino rats were given oral single dose of 6 and 8g/kg of extract and water as control. For sub-acute toxicity, 20 Wistar albino rats were given 0.5, 2, 6 and 8g/kg body weight/day of the extract for 30 days. The biochemical parameters examined were Na+, K+, CO32-, Cl- , urea, aspartate aminotransferase, alanine aminotransferase, alkaline phosphatase enzymes, total and conjugated bilirubin. Phytochemical screening revealed the presence of carbohydrate, glycosides, saponins, anthraquinone, cardiac glycosides, and flavonoids in the plant. The extract at doses of 0.5, 2 and 8g/kg decreased creatinine and increased Na+ and Ca++ levels. No significant differences in other parameters were found. No signs of toxicity or behavioural changes were observed at all doses. Mucuna pruriens leaf extract is considered safe at these doses in the short term.

Nigerian Journal of Pharmaceutical and Applied Science Research, 2017

Nigerian Journal of Pharmaceutical and Applied Science Research, 2019

Journal of Pharmacy & Bioresources, 2012

ABSTRACT The work evaluated the behavioral and toxicological effects and its consequences on hema... more ABSTRACT The work evaluated the behavioral and toxicological effects and its consequences on hematological parameters and the phytochemical analysis of Jatropha tanjorensis leaf. Acute and sub-acute toxicity studies were done on Wistar albino mice and rats for 14 days and 28 days respectively. Hematological parameters of the rats were also determined. During acute toxicity, there were no adverse effect found in the general behavior and mortality at any dose level given (1000-8000mg/kg b.wt.). Sub-acute toxicity did not cause any changes in the body and organ weight except a statistical decrease in the spleen weight. Hematological investigation revealed an increase in the packed cell volume, red blood cells and hemoglobin. Phytochemical analysis revealed the presence of tannins, Flavonoid, Alkaloids, Anthraquinone, Saponin and Cardiac glycosides. This work thus justifies the ethnomedicinal use of the plant in the treatment of anaemia and its safety profile.

Journal of Pharmacy & Bioresources, 2013

ABSTRACT Spigelia anthelmia is used traditionally in Southern Nigeria for the treatment of infant... more ABSTRACT Spigelia anthelmia is used traditionally in Southern Nigeria for the treatment of infant convulsion and epilepsy. This study investigated the phytochemical constituents, proximate analysis and anticonvulsant effect of the methanolic extract of Spigelia anthelmia. Phytochemical evaluation and proximate analysis was carried out using standard procedure and the anticonvulsant screening was carried out using the maximum electroshock-induced seizure model on albino rat. Results show that the plant contains carbohydrates, reducing sugars, saponins, tannins, flavonoids, alkaloids, fats, proteins and fibre. Also, the plant exhibited a dose-dependent anti-seizure activity on the MESinduced seizure. At a dose of 150mg/kg, it exhibited 73.3% protection against electrically induced seizure in rat; suggesting that anti-seizure effect of S. anthelmia may be associated with the secretion and released of GABA since electroshock causes the inhibition of GABA release. This work will help in understanding and possibly explaining the ethnomedicinal use of the plant in the treatment of convulsion and epilepsy.

Purpose: To synthesize and characterize palmitoyl amino benzamides, and to evaluate them for poss... more Purpose: To synthesize and characterize palmitoyl amino benzamides, and to evaluate them for possible anti-inflammatory and anti-nociceptive activities. Methods: Palmitoyl amino benzamides were synthesized by the opening of isatoic anhydride ring with respective amino acids (glycine, β-alanine and γ-aminobutyric acid) and the condensation of the product with palmitoyl chloride. The final products were purified on column chromatography, eluting with dichloromethane/ethyl acetate. All the compounds were unequivocally characterized using the combination of infra red (IR), 1H and 13C (nuclear magnetic resonance (NMR), mass spectrometry (MS) and elemental analysis. In vivo anti-inflammatory and anti-nociceptive activities of the synthesized compounds at 20, 50 and 100mg/kg doses were carried out using carrageenan-induced paw oedema in rat and acetic acid-induced writhing in mice, respectively. Aspirin was used at a dose of 100mg/kg as the reference drug. Results: The compounds were obtai...

Acta Poloniae Pharmaceutica - Drug Research

The synthesis of pyrazoles: 1-(3, 4, 5-trimethoxyphenyl)3-(2, 4-dimethoxy phenyl) dihydropyrazole... more The synthesis of pyrazoles: 1-(3, 4, 5-trimethoxyphenyl)3-(2, 4-dimethoxy phenyl) dihydropyrazole was executed by reaction of hydrazine hydrate with chalcones followed by concomitant dehydration and cyclization. The structure of the synthesized compounds were elucidated using infrared, nuclear magnetic 1 13 resonance ( H and C), and mass spectrometry. The chalcones and pyrazoles were screened for antibacterial activities using the agarwell diffusion method at a serial dilution of 106cfu/ml. The pyrazoles showed no significant bacteriocidal or bacteriostatic activity against the clinical isolates and typed culture of bacteria tested against. ABSTRACT

Acta poloniae pharmaceutica, 2007

2 Abstract: Work has been done to determine the effect of Loranthus bengwensis supplemented diet ... more 2 Abstract: Work has been done to determine the effect of Loranthus bengwensis supplemented diet on food intake, blood pressure and electrolyte levels in normal and hypertensive rats. Consequently, sixteen albino rats were divided into four groups of four each. The first group were fed on growers mash only (control), the second group on 92% growers mash and 8% NaCl (salt loaded group) the third on 8% NaCl, 8% mistletoe powder and 84% growers mash (salt loaded and mistletoe group) while the fourth on 8% mistletoe powder and 92% growers mash (normal and mistletoe group). The weight changes, daily food intake, faecal output, systolic and diastolic mean arterial and pulse pressures of the animals in various groups were recorded. The Na , K , Cl and ++ HCO levels were determined. Results indicate that rats in the salt loaded group had significantly higher 3 systolic, diastolic and mean arterial pressures (P<0.05) but significantly lower pulse pressure (P<0.05) compared with control...

Plasma total cholesterol, triglycerides, high density lipoprotein cholesterol, low density lipopr... more Plasma total cholesterol, triglycerides, high density lipoprotein cholesterol, low density lipoprotein cholesterol, Phospholipids and molonydialdehyde were determined in normotensives, hypertensives on anti – hypertensive drugs and hypertensives not on any anti hypertensive drugs aged between 30 – 60 years. Plasma samples were used. Result were statistically significant in all parameters studied at the level of (p < 0.001) in normotensives, hypertensives on drugs and hypertensives not on drugs except in phospholipids where there was no statistical difference. Relationship between blood pressure and lipid concentration were established. The product of lipid peroxidation, malonydialdehyde was statistically significant in hypertensives on anti-hypertensive drugs and hypertensives not on any anti-hypertensive drugs when compared to normotensive control at (p<0.001) indicating free radical generation as a result of oxidative stress. These finding indicates that there are high lipid...

The Internet Journal of Health, 2009

Plasma Ascorbic acid, total cholesterol, High density lipoprotein cholesterol levels and Total ch... more Plasma Ascorbic acid, total cholesterol, High density lipoprotein cholesterol levels and Total cholesterol/High density lipoprotein cholesterol ratio were determined in 52 newly diagnosed hypercholesterolaemic subjects and 48 normocholesterolaemic subjects. Hypercholesterolaemic subjects were defined as those with plasma total cholesterol ≥200mg/dl. The results showed that the mean plasma ascorbic acid levels were significantly lower in hypercholesterolaemic subjects when compared to normocholesterolaemics (P< 0.005) while total cholesterol , high density lipoprotein cholesterol and total cholesterol/high density lipoprotein cholesterol ratio were higher in hypercholesterolaemics than control (P<0.005). The low ascorbic acid levels observed in hypercholesterolaemics may be due to increased lipid peroxidation and hence low ascorbic acid levels may play a role in the aetiology of hypercholesterolaemia and therefore vitamin C supplements maybe useful in the management of Hypercholesterolaemia.

Nowadays, COX-2 inhibitors such as valdecoxib are removed from the market because of their cardio... more Nowadays, COX-2 inhibitors such as valdecoxib are removed from the market because of their cardiovascular toxicity and their potential to increase the risk of strokes. In response to this, medicinal chemists have attempted to synthesize new classes of COX-2 Inhibitors. Materials and Methods: In this study, three novel analogues of thiazolidin-4-ones derivatives 2a-c were synthesized. The ability of these compounds to inhibit ovine COX-1 and COX-2 (0.2-0.8 µM) was determined using a colorimetric method. The cytotoxic effect of the synthesized compounds (25-100 M) was also investigated by measuring their cytotoxicity against Caco-2 and MCF-7 cell lines using MTT assay. Cell apoptosis was determined by flow cytometry. Writhing test (7.5-75 mg/kg) was used to examine the antinociceptive effects in mice. The effect of the analogues against acute inflammation (7.5-75 mg/kg) was also studied using xylene-induced ear edema test in mice. Results: The synthesized compounds showed a weak capacity to inhibit the proliferation of Caco-2 and MCF-7 cell lines. The COX-2 inhibition potency and selectivity index for test compounds 2a-b were as follows; celecoxib > 2b > 2a. On the other hand, all three analogues exhibited strong antinociceptive activity against acetic acid-induced writhing. The anti-inflammatory and antinociceptive effects of the analogues were markedly more than positive control, celecoxib. Conclusion: This study demonstrates that the antinociceptive and anti-inflammatory activity profiles exhibited by the novel synthesized compounds are independent from their COX-2 inhibitory potencies. The found antinociceptive and anti-inflammatory effects can be caused by interaction with other target; independent from COX-2. Accordingly, the compounds 2a-c could serve as lead compounds to develop novel anti-inflammation and antinociceptive drugs.

Journal of Pharmacy & Bioresources

Long chain lipid amides isolated from animal tissues are known to have analgesic and anti-inflamm... more Long chain lipid amides isolated from animal tissues are known to have analgesic and anti-inflammatory properties. The synthesis of analogues of such lipid amides of biological origin was designed and carried out. The analgesic properties of some of the synthesized molecules were also carried out. Condensation reaction involving palmitoyl chloride and primary amino compounds was carried out to produce the desired compounds. Analgesic properties were investigated using acetic acid induced writhing and hot plate models. The synthetic procedure yielded the desired products in good quantity. There was a dose dependent analgesic activity of the products tested. These simple organic molecules, which show promising analgesic properties, could be developed into useful drugs that could be used as effective pain relievers.

The synthesis of pyrazoles: 1-(3, 4, 5-trimethoxyphenyl)-3-(2, 4-dimethoxy phenyl) dihydropyrazol... more The synthesis of pyrazoles: 1-(3, 4, 5-trimethoxyphenyl)-3-(2, 4-dimethoxy phenyl) dihydropyrazole was executed by reaction of hydrazine hydrate with chalcones followed by concomitant dehydration and cyclization. The structure of the synthesized compounds were elucidated using infrared, nuclear magnetic 1 13 resonance (H and C), and mass spectrometry. The chalcones and pyrazoles were screened for antibacterial activities using the agar-well diffusion method at a serial dilution of 106cfu/ml. The pyrazoles showed no significant bacteriocidal or bacteriostatic activity against the clinical isolates and typed culture of bacteria tested against. ABSTRACT Keywords:

Acta poloniae pharmaceutica

Acta Poloniae Pharmaceutica, May 1, 2007

... 1H-pyri-do-[2,3-d]1,3-oxazine-2,4-dione 2a and 1H-pyrido-[3,2-d]1,3-oxazine-2,4-dione 2b were... more ... 1H-pyri-do-[2,3-d]1,3-oxazine-2,4-dione 2a and 1H-pyrido-[3,2-d]1,3-oxazine-2,4-dione 2b were synthesized according to literature procedure (7, 8). Prop-2-ynyl-amine, triethylorthoformate and other reagents were obtained from ... CYRIL USIFOH* and PATRICK IGBINADUWA ...

Tropical Journal of Pharmaceutical Research, Sep 17, 2014

Purpose: To synthesize and characterize palmitoyl amino benzamides, and to evaluate them for poss... more Purpose: To synthesize and characterize palmitoyl amino benzamides, and to evaluate them for possible anti-inflammatory and anti-nociceptive activities. Methods: Palmitoyl amino benzamides were synthesized by the opening of isatoic anhydride ring with respective amino acids (glycine, β-alanine and γ-aminobutyric acid) and the condensation of the product with palmitoyl chloride. The final products were purified on column chromatography, eluting with dichloromethane/ethyl acetate. All the compounds were unequivocally characterized using the combination of infra red (IR), 1H and 13C (nuclear magnetic resonance (NMR), mass spectrometry (MS) and elemental analysis. In vivo anti-inflammatory and anti-nociceptive activities of the synthesized compounds at 20, 50 and 100mg/kg doses were carried out using carrageenan-induced paw oedema in rat and acetic acid-induced writhing in mice, respectively. Aspirin was used at a dose of 100mg/kg as the reference drug. Results: The compounds were obtained in high yield (70-90 %) and purity. The anti-inflammatory results showed a poor activity for the compounds except o-palmitoylamino N-carboxyethyl benzamide which produced significant inhibition (p < 0.05) at a dose of 50 mg/kg (43.8 % oedema inhibition) while the reference drug, aspirin, showed 51.3 % inhibition. The anti-nociceptive study, however, showed good inhibition (p < 0.05) of acetic acid-induced writhing, with o-palmitoylamino Ncarboxymethylbenzamide producing 86.2 % inhibition at 100 mg/kg dose compared with the reference drug (aspirin) which gave 74.3 % inhibition at 100 mg/kg. Conclusion: The findings of this study indicate that the synthesized compounds, though displaying poor anti-inflammatory activity, do possess promising anti-nociceptive activity.

Work has been done to determine the effect of Loranthus bengwensis supplemented diet on food inta... more Work has been done to determine the effect of Loranthus bengwensis supplemented diet on food intake, blood pressure and electrolyte levels in normal and hypertensive rats. Consequently, sixteen albino rats were divided into four groups of four each. The first group were fed on growers mash only (control), the second group on 92% growers mash and 8% NaCl (salt loaded group) the third on 8% NaCl, 8% mistletoe powder and 84% growers mash (salt loaded and mistletoe group) while the fourth on 8% mistletoe powder and 92% growers mash (normal and mistletoe group). The weight changes, daily food intake, faecal output, systolic and diastolic mean arterial and pulse pressures of the animals in various groups were recorded. The Na , K , Cl and + + HCO levels were determined. Results indicate that rats in the salt loaded group had significantly higher 3 systolic, diastolic and mean arterial pressures (P<0.05) but significantly lower pulse pressure (P<0.05) compared with control rats. Rats in the salt loaded and mistletoe group and normal and mistletoe group had lower systolic pressure and lower pulse pressure compared with control rats. Rats fed with salt loaded diet and salt loaded with mistletoe powder had higher Na and Cl levels compared with control but the K and HCO + + 3 concentrations did not differ significantly (P<0.05) from those of control rats. Rats in the three groups recorded higher food intake and faecal output but lower weight gain compared to control rats. The results showed that Loranthus bengwensis significantly reduced (P<0.05) diastolic, systolic and mean arterial pressures as well as Na and Cl concentration but significantly reduced weight gain in normal and hypertensive rat.

Nigerian Journal of Pharmaceutical Research, 2020

Background: Anthocleista djalonensis is a West African plant with several ethnomedicinal uses.Obj... more Background: Anthocleista djalonensis is a West African plant with several ethnomedicinal uses.Objectives: This study evaluated the effect of Anthocleista djalonensis methanol root bark extract on fertility parameters in male rats.Material and Methods: The rats were randomly allotted to four groups (n=5). Group A (control) received distilled water (10 ml/kg), groups B, C, D received oral doses of 100, 200 and 400 mg/kg/day of the extract respectively for 28 days. The mean body, testicular, and epididymal weights; sperm indices; and serum testosterone level were assessed.Results: There were no significant changes on the body weights of the treated rats but their testicular and epididymal weights increased significantly (P˂0.05) at the dose of 400 mg/kg in comparison with the control group. Sperm indices such as sperm count, motility, morphology and viability increased significantly (P˂0.05) at the doses of 200 and 400 mg/kg/day when compared to the control. There was also a significant (P˂0.05) increase in serum testosterone concentration at the dose of 400 mg/kg/day of the extract.Conclusion: The results suggest that the methanol root bark extract of A. djalonensis improves fertility parameters in male rats thereby justifying its use in ethnomedicine.Keywords: Sperm count, testosterone level, spermatogenesis, oxidative stress

Journal of Pharmacy & Bioresources, 2013

ABSTRACT The study assessed the phytochemical, acute toxicity, sub-acute toxicity and blood chemi... more ABSTRACT The study assessed the phytochemical, acute toxicity, sub-acute toxicity and blood chemistry of the aqueous leaf extract of Mucuna pruriens. Powdered leaf of Mucuna pruriens was extracted by maceration. 24 albino mice used for acute toxicity were administered between 1-8 g/kg body weight of the extract while the control group received distilled water. 12 Wistar albino rats were given oral single dose of 6 and 8g/kg of extract and water as control. For sub-acute toxicity, 20 Wistar albino rats were given 0.5, 2, 6 and 8g/kg body weight/day of the extract for 30 days. The biochemical parameters examined were Na+, K+, CO32-, Cl- , urea, aspartate aminotransferase, alanine aminotransferase, alkaline phosphatase enzymes, total and conjugated bilirubin. Phytochemical screening revealed the presence of carbohydrate, glycosides, saponins, anthraquinone, cardiac glycosides, and flavonoids in the plant. The extract at doses of 0.5, 2 and 8g/kg decreased creatinine and increased Na+ and Ca++ levels. No significant differences in other parameters were found. No signs of toxicity or behavioural changes were observed at all doses. Mucuna pruriens leaf extract is considered safe at these doses in the short term.

Nigerian Journal of Pharmaceutical and Applied Science Research, 2017

Nigerian Journal of Pharmaceutical and Applied Science Research, 2019

Journal of Pharmacy & Bioresources, 2012

ABSTRACT The work evaluated the behavioral and toxicological effects and its consequences on hema... more ABSTRACT The work evaluated the behavioral and toxicological effects and its consequences on hematological parameters and the phytochemical analysis of Jatropha tanjorensis leaf. Acute and sub-acute toxicity studies were done on Wistar albino mice and rats for 14 days and 28 days respectively. Hematological parameters of the rats were also determined. During acute toxicity, there were no adverse effect found in the general behavior and mortality at any dose level given (1000-8000mg/kg b.wt.). Sub-acute toxicity did not cause any changes in the body and organ weight except a statistical decrease in the spleen weight. Hematological investigation revealed an increase in the packed cell volume, red blood cells and hemoglobin. Phytochemical analysis revealed the presence of tannins, Flavonoid, Alkaloids, Anthraquinone, Saponin and Cardiac glycosides. This work thus justifies the ethnomedicinal use of the plant in the treatment of anaemia and its safety profile.

Journal of Pharmacy & Bioresources, 2013

ABSTRACT Spigelia anthelmia is used traditionally in Southern Nigeria for the treatment of infant... more ABSTRACT Spigelia anthelmia is used traditionally in Southern Nigeria for the treatment of infant convulsion and epilepsy. This study investigated the phytochemical constituents, proximate analysis and anticonvulsant effect of the methanolic extract of Spigelia anthelmia. Phytochemical evaluation and proximate analysis was carried out using standard procedure and the anticonvulsant screening was carried out using the maximum electroshock-induced seizure model on albino rat. Results show that the plant contains carbohydrates, reducing sugars, saponins, tannins, flavonoids, alkaloids, fats, proteins and fibre. Also, the plant exhibited a dose-dependent anti-seizure activity on the MESinduced seizure. At a dose of 150mg/kg, it exhibited 73.3% protection against electrically induced seizure in rat; suggesting that anti-seizure effect of S. anthelmia may be associated with the secretion and released of GABA since electroshock causes the inhibition of GABA release. This work will help in understanding and possibly explaining the ethnomedicinal use of the plant in the treatment of convulsion and epilepsy.

Purpose: To synthesize and characterize palmitoyl amino benzamides, and to evaluate them for poss... more Purpose: To synthesize and characterize palmitoyl amino benzamides, and to evaluate them for possible anti-inflammatory and anti-nociceptive activities. Methods: Palmitoyl amino benzamides were synthesized by the opening of isatoic anhydride ring with respective amino acids (glycine, β-alanine and γ-aminobutyric acid) and the condensation of the product with palmitoyl chloride. The final products were purified on column chromatography, eluting with dichloromethane/ethyl acetate. All the compounds were unequivocally characterized using the combination of infra red (IR), 1H and 13C (nuclear magnetic resonance (NMR), mass spectrometry (MS) and elemental analysis. In vivo anti-inflammatory and anti-nociceptive activities of the synthesized compounds at 20, 50 and 100mg/kg doses were carried out using carrageenan-induced paw oedema in rat and acetic acid-induced writhing in mice, respectively. Aspirin was used at a dose of 100mg/kg as the reference drug. Results: The compounds were obtai...

Acta Poloniae Pharmaceutica - Drug Research

The synthesis of pyrazoles: 1-(3, 4, 5-trimethoxyphenyl)3-(2, 4-dimethoxy phenyl) dihydropyrazole... more The synthesis of pyrazoles: 1-(3, 4, 5-trimethoxyphenyl)3-(2, 4-dimethoxy phenyl) dihydropyrazole was executed by reaction of hydrazine hydrate with chalcones followed by concomitant dehydration and cyclization. The structure of the synthesized compounds were elucidated using infrared, nuclear magnetic 1 13 resonance ( H and C), and mass spectrometry. The chalcones and pyrazoles were screened for antibacterial activities using the agarwell diffusion method at a serial dilution of 106cfu/ml. The pyrazoles showed no significant bacteriocidal or bacteriostatic activity against the clinical isolates and typed culture of bacteria tested against. ABSTRACT

Acta poloniae pharmaceutica, 2007

2 Abstract: Work has been done to determine the effect of Loranthus bengwensis supplemented diet ... more 2 Abstract: Work has been done to determine the effect of Loranthus bengwensis supplemented diet on food intake, blood pressure and electrolyte levels in normal and hypertensive rats. Consequently, sixteen albino rats were divided into four groups of four each. The first group were fed on growers mash only (control), the second group on 92% growers mash and 8% NaCl (salt loaded group) the third on 8% NaCl, 8% mistletoe powder and 84% growers mash (salt loaded and mistletoe group) while the fourth on 8% mistletoe powder and 92% growers mash (normal and mistletoe group). The weight changes, daily food intake, faecal output, systolic and diastolic mean arterial and pulse pressures of the animals in various groups were recorded. The Na , K , Cl and ++ HCO levels were determined. Results indicate that rats in the salt loaded group had significantly higher 3 systolic, diastolic and mean arterial pressures (P<0.05) but significantly lower pulse pressure (P<0.05) compared with control...

Plasma total cholesterol, triglycerides, high density lipoprotein cholesterol, low density lipopr... more Plasma total cholesterol, triglycerides, high density lipoprotein cholesterol, low density lipoprotein cholesterol, Phospholipids and molonydialdehyde were determined in normotensives, hypertensives on anti – hypertensive drugs and hypertensives not on any anti hypertensive drugs aged between 30 – 60 years. Plasma samples were used. Result were statistically significant in all parameters studied at the level of (p < 0.001) in normotensives, hypertensives on drugs and hypertensives not on drugs except in phospholipids where there was no statistical difference. Relationship between blood pressure and lipid concentration were established. The product of lipid peroxidation, malonydialdehyde was statistically significant in hypertensives on anti-hypertensive drugs and hypertensives not on any anti-hypertensive drugs when compared to normotensive control at (p<0.001) indicating free radical generation as a result of oxidative stress. These finding indicates that there are high lipid...

The Internet Journal of Health, 2009

Plasma Ascorbic acid, total cholesterol, High density lipoprotein cholesterol levels and Total ch... more Plasma Ascorbic acid, total cholesterol, High density lipoprotein cholesterol levels and Total cholesterol/High density lipoprotein cholesterol ratio were determined in 52 newly diagnosed hypercholesterolaemic subjects and 48 normocholesterolaemic subjects. Hypercholesterolaemic subjects were defined as those with plasma total cholesterol ≥200mg/dl. The results showed that the mean plasma ascorbic acid levels were significantly lower in hypercholesterolaemic subjects when compared to normocholesterolaemics (P< 0.005) while total cholesterol , high density lipoprotein cholesterol and total cholesterol/high density lipoprotein cholesterol ratio were higher in hypercholesterolaemics than control (P<0.005). The low ascorbic acid levels observed in hypercholesterolaemics may be due to increased lipid peroxidation and hence low ascorbic acid levels may play a role in the aetiology of hypercholesterolaemia and therefore vitamin C supplements maybe useful in the management of Hypercholesterolaemia.

Nowadays, COX-2 inhibitors such as valdecoxib are removed from the market because of their cardio... more Nowadays, COX-2 inhibitors such as valdecoxib are removed from the market because of their cardiovascular toxicity and their potential to increase the risk of strokes. In response to this, medicinal chemists have attempted to synthesize new classes of COX-2 Inhibitors. Materials and Methods: In this study, three novel analogues of thiazolidin-4-ones derivatives 2a-c were synthesized. The ability of these compounds to inhibit ovine COX-1 and COX-2 (0.2-0.8 µM) was determined using a colorimetric method. The cytotoxic effect of the synthesized compounds (25-100 M) was also investigated by measuring their cytotoxicity against Caco-2 and MCF-7 cell lines using MTT assay. Cell apoptosis was determined by flow cytometry. Writhing test (7.5-75 mg/kg) was used to examine the antinociceptive effects in mice. The effect of the analogues against acute inflammation (7.5-75 mg/kg) was also studied using xylene-induced ear edema test in mice. Results: The synthesized compounds showed a weak capacity to inhibit the proliferation of Caco-2 and MCF-7 cell lines. The COX-2 inhibition potency and selectivity index for test compounds 2a-b were as follows; celecoxib > 2b > 2a. On the other hand, all three analogues exhibited strong antinociceptive activity against acetic acid-induced writhing. The anti-inflammatory and antinociceptive effects of the analogues were markedly more than positive control, celecoxib. Conclusion: This study demonstrates that the antinociceptive and anti-inflammatory activity profiles exhibited by the novel synthesized compounds are independent from their COX-2 inhibitory potencies. The found antinociceptive and anti-inflammatory effects can be caused by interaction with other target; independent from COX-2. Accordingly, the compounds 2a-c could serve as lead compounds to develop novel anti-inflammation and antinociceptive drugs.

Journal of Pharmacy & Bioresources

Long chain lipid amides isolated from animal tissues are known to have analgesic and anti-inflamm... more Long chain lipid amides isolated from animal tissues are known to have analgesic and anti-inflammatory properties. The synthesis of analogues of such lipid amides of biological origin was designed and carried out. The analgesic properties of some of the synthesized molecules were also carried out. Condensation reaction involving palmitoyl chloride and primary amino compounds was carried out to produce the desired compounds. Analgesic properties were investigated using acetic acid induced writhing and hot plate models. The synthetic procedure yielded the desired products in good quantity. There was a dose dependent analgesic activity of the products tested. These simple organic molecules, which show promising analgesic properties, could be developed into useful drugs that could be used as effective pain relievers.

The synthesis of pyrazoles: 1-(3, 4, 5-trimethoxyphenyl)-3-(2, 4-dimethoxy phenyl) dihydropyrazol... more The synthesis of pyrazoles: 1-(3, 4, 5-trimethoxyphenyl)-3-(2, 4-dimethoxy phenyl) dihydropyrazole was executed by reaction of hydrazine hydrate with chalcones followed by concomitant dehydration and cyclization. The structure of the synthesized compounds were elucidated using infrared, nuclear magnetic 1 13 resonance (H and C), and mass spectrometry. The chalcones and pyrazoles were screened for antibacterial activities using the agar-well diffusion method at a serial dilution of 106cfu/ml. The pyrazoles showed no significant bacteriocidal or bacteriostatic activity against the clinical isolates and typed culture of bacteria tested against. ABSTRACT Keywords:

Acta poloniae pharmaceutica