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1.
J Ethnopharmacol ; 321: 117562, 2024 Mar 01.
Article En | MEDLINE | ID: mdl-38081399

ETHNOPHARMACOLOGICAL RELEVANCE: West African Albizia (Albizia zygia DC J. F. Macbr) leaves are a tropical plant that are frequently used in folkloric medicine to treat a number of illnesses, including type 2 diabetes (TY2D) and erectile dysfunction (ED), without having a complete scientific foundation. AIM OF THE STUDY: This investigation examined the effect of action of dietary augmentation of Albizia zygia leaves (AZL) on rat sexual functioning and important enzymes related to TY2D and ED. MATERIALS AND METHODS: Thirty matured adult Wistar rats of the weight 180-200 g were acclimatized in a lab environmental condition for two weeks prior to experiment given food and water to acclimate. Twenty-four of the rats got high fat diet (HFD) for periods of two weeks before receiving streptozotocin (STZ) intraperitoneally (i.p.), 35 mg/kg body weight single dose. Six rats got basal diets. Type 2 diabetes was identified in rats 72 h after STZ treatment. Rats were then used to evaluate the mounting number, mount delay, intromission number, and intromission latency. RESULTS: Following that, meals supplemented with AZL (5% or 10% inclusion) were given to diabetic-ED rats for 14 days. AZL was added. Therefore, in diabetic-ED rats, AZL supplementation could significantly (p0.05) lower blood glucose levels and the activities of alpha amylase, alpha glucosidase, phosphodiesterase-5, and arginase. In the case of diabetic-ED treated rats in consideration with diabetic-ED control group, nitric oxide levels were increased along with sexual function. CONCLUSION: Thus, experimental results of this study demonstrated rats that consumed AZL in their diets had less erectile dysfunction. In order to address ED caused by diabetes, AZL could be suggested as functional meals.


Albizzia , Aphrodisiacs , Diabetes Mellitus, Experimental , Diabetes Mellitus, Type 2 , Erectile Dysfunction , Male , Humans , Rats , Animals , Erectile Dysfunction/drug therapy , Erectile Dysfunction/etiology , Aphrodisiacs/pharmacology , Penile Erection , Diabetes Mellitus, Type 2/drug therapy , Diabetes Mellitus, Type 2/complications , Hypoglycemic Agents/pharmacology , Hypoglycemic Agents/therapeutic use , Rats, Wistar , Diabetes Mellitus, Experimental/complications , Diet
2.
J Complement Integr Med ; 21(1): 80-87, 2024 Mar 01.
Article En | MEDLINE | ID: mdl-37974314

OBJECTIVES: This research work studied the phenolic composition of Pentaclethra macrophylla (PM), the inclusion of dietary supplementation of PM leaves on sexual functions and its connection to inhibit enzymes (arginase and phosphodiesterase-5) and nitric oxide level, linked to type 2 diabetes-induced erectile dysfunction in rats. METHODS: Gallic acid, chlorogenic and ellagic acids, Kaempferol, and epicatechin etc. was spotted with High performance liquid chromatography-diode array detector from PM extract. Twenty-five (25) rats were used for the study. Five rats were placed with basal diet; diets not supplemented with PM leaves (normal rat group) while twenty rats were made diabetic by feeding them with high fat diet for two weeks, prior to single injection with 35 mg/kg of streptozotocin (STZ). After checking with glucometer, experimental animals with blood glucose level >250 mg/dL were accepted as diabetic. The diabetic rats were subsequently divided into four groups of five rats each (n=5). The diabetic rats were placed on basal diet, or diets supplemented with PM leaves (10 % or 5 % inclusion) or sildenafil citrate (SC). RESULTS: The result revealed that PM supplemented diets caused significant (p<0.05) reduction in blood glucose level, and augmented erectile function by inhibiting arginase and PDE5 activities as well as enhancing nitric oxide level. CONCLUSIONS: In conclusion, dietary inclusion of PM leaves could serve as a potent nutraceutical source in hyperglycemia induced erectile dysfunction management.


Diabetes Mellitus, Experimental , Diabetes Mellitus, Type 2 , Erectile Dysfunction , Male , Humans , Rats , Animals , Erectile Dysfunction/drug therapy , Erectile Dysfunction/etiology , Blood Glucose , Diabetes Mellitus, Experimental/complications , Nitric Oxide , Arginase , Piperazines/pharmacology , Nitric Oxide Synthase Type III
3.
Mol Cell Biochem ; 2023 Oct 04.
Article En | MEDLINE | ID: mdl-37792238

Plasma membrane anchored nucleotidases (E-ATPDases), as the E-NTPDase family, could hydrolyze and regulate the pericellular levels of nucleotides in lymphocytes. Each immune organ has a different microenvironment and display lymphocytes with different functions and phenotypes. Considering the different functions of each resident subpopulations of lymphocytes, the E-ATPDases activities in bone marrow (BML), thymus (TL) and mesenteric lymph node (MLL) lymphocytes of Wistar rats were characterized. The hydrolysis of extracellular nucleotides (eATP and eADP) showed linearity in time of reaction between 0 and 120 min, and concentration of lymphocytes expressed in proteins between 1 and 6 µg protein in the reaction medium. The optimal activity was attained at 37 °C in a pH value of 8.0. The necessity of the cofactors Ca2+ and Mg2+ for the enzymatic activity was confirmed through a curve of concentration of 0-1000 µM in the reaction medium, with both cofactors showing similar effects in the enzymatic activity. The Chevillard plot revealed that the hydrolysis of eATP and eADP occurred at the same active site of the enzyme. The analyses of E-ATPDases inhibitor and enzyme specificity showed possible involvement of E-NTPDase isoforms - 1 and - 2 in the isolated cells. Furthermore, different kinetic behavior of the nucleotide hydrolysis in each resident subpopulation lymphocyte was observed in this study, as MLL showed the higher Vmax with the lowest km values, while TL had the lowest Vmax and high km values. The kinetic values for E-NTPDase activity of each immune tissue lymphocytes can be an important therapeutic target for numeral immune-related diseases.

4.
Andrologia ; 54(11): e14629, 2022 Dec.
Article En | MEDLINE | ID: mdl-36349558

Massularia acuminata stem is often used in folkloric medicine in the management of erectile dysfunction (ED), without full scientific basis for its action. Thus, the effects of aqueous extract of M. acuminata stem (MAS) on sexual activity, hormonal action, enzymatic activity and levels of molecules associated with erectile function were assessed. ED was induced by single intraperitoneal injection of 50 mg/kg body weight of streptozotocin in rats and treated with sildenafil citrate or MAS (50 or 100 mg/kg) orally for 2 weeks. The results revealed that there was significant (p < 0.05) reduction in mounting and intromission frequencies, testosterone, luteinizing hormone, and nitric oxide levels, as well as elevation in mounting and intromission latencies, phosphodiesterase 5, arginase, acetylcholinesterase, adenosine triphosphatidase, and adenosine deaminase activities, nitric oxide, thiobarbituric acid reactive species, and glycated haemoglobin levels were observed in ED rats in comparison with the control rats. Treatment with MAS or sildenafil citrate significantly (p < 0.05) modulated the sexual behaviour, biochemical parameters and histological architecture, with 100 mg/kg of MAS having the best erectogenic effects. Furthermore, phenolic characterization revealed that catechin and kaempferol as the main phenolic compounds present in MAS, that can act in synergistically or additively with other phytochemicals to confer erectogenic effect.


Erectile Dysfunction , Animals , Humans , Male , Rats , Acetylcholinesterase , Erectile Dysfunction/etiology , Erectile Dysfunction/chemically induced , Luteinizing Hormone/pharmacology , Nitric Oxide , Penile Erection , Plant Extracts/pharmacology , Rats, Wistar , Sildenafil Citrate/pharmacology , Streptozocin/toxicity
5.
Foods ; 11(15)2022 Jul 27.
Article En | MEDLINE | ID: mdl-35954004

This study investigated the flavonoid content, antioxidant activity, and toxicological properties of the acetone-water fraction of stem bark of Stryphnodendron rotundifolium Mart. (TFSR). The total flavonoid content and antioxidant activity were determined, as typified by DPPH● and ABTS●+ radical scavenging abilities, Fe3+ reducing antioxidant power (FRAP), relative antioxidant capacity (RAC), and the inhibition of thiobarbituric acid reactive species (TBARs) in Drosophila melanogaster tissue. Toxicity and locomotor functions were evaluated in adult D. melanogaster flies through aging and survival assays, startle-induced negative geotaxis, and centrophobic responses with video-assisted open field motion tracking. The flavonoid content of dry TFSR (DF) was 3.36 mg quercetin/g. Furthermore, the significant antioxidant activity of TFSR was revealed through scavenging 95.3% of the ABTS●+ radical and 82.4% of the DPPH● radical, as well reducing 74.7% of Fe3+ in the FRAP assay and 80% Mo6+ in the RAC assay. TFSR conferred 70.25% protection against lipid peroxidation in Drosophila tissue. Survival rates ranged from 84.65 to 103.98% in comparison to the non-supplemented control and no evident deterioration of locomotor functions and centrophobia responses was observed. These results revealed that TFSR has potent antioxidant activity and low toxicity in vivo, profiling TFSR as a promising natural product in the treatment/management of iron overload and associated conditions.

6.
J Pharm Pharmacol ; 73(11): 1547-1561, 2021 Oct 07.
Article En | MEDLINE | ID: mdl-34427673

OBJECTIVES: This study was aimed at assessing the anti-arthritic effects of hesperidin on the inflammatory markers in serum/plasma, ectoenzymes activity in platelet, reactive oxygen species (ROS), apoptosis and cell cycle in bone marrow cells of a rat model of arthritis. METHODS: Fifty-six adult female Wistar rats (245-274 g) were grouped into eight of seven rats each: control rats given normal saline or 40 mg/kg of hesperidin or 80 mg/kg of hesperidin, 0.2 mg/kg of dexamethasone, arthritic rats given normal saline, or 40 mg/kg of hesperidin or 80 mg/kg of hesperidin, and 0.2 mg/kg of dexamethasone. Myeloperoxidase and nitrate plus nitrite levels were evaluated in the plasma and serum, respectively. The ecto-nucleoside triphosphate diphosphohydrolases, ecto-5'-nucleotidase and ecto-adenosine deaminase activities were assessed in platelets. Subsequently, the cells of the bone marrow were obtained, and the assays for ROS, apoptosis and cell cycle were evaluated using flow cytometry. KEY FINDINGS: The results showed that hesperidin mitigated inflammation, modulated adenosine nucleotides and nucleoside hydrolysing enzymes and levels, minimized ROS intracellularly, attenuated apoptotic process and activated cell cycle arrest in arthritic rat. CONCLUSION: This study suggests that hesperidin could be a natural and promising anti-inflammatory compound for the management of arthritis.


Anti-Inflammatory Agents/pharmacology , Arthritis, Experimental , Cell Cycle Checkpoints/drug effects , Citrus/chemistry , Hesperidin/pharmacology , Hydrolases/metabolism , Inflammation , 5'-Nucleotidase/metabolism , Adenosine Deaminase/metabolism , Animals , Anti-Inflammatory Agents/therapeutic use , Apoptosis , Arthritis, Experimental/drug therapy , Arthritis, Experimental/metabolism , Arthritis, Experimental/pathology , Arthritis, Rheumatoid/drug therapy , Arthritis, Rheumatoid/metabolism , Arthritis, Rheumatoid/pathology , Female , Freund's Adjuvant , Hesperidin/therapeutic use , Inflammation/metabolism , Inflammation/prevention & control , Membrane Proteins/metabolism , Nucleoside-Triphosphatase/metabolism , Phytotherapy , Plant Extracts/pharmacology , Plant Extracts/therapeutic use , Pyrophosphatases , Rats, Wistar , Reactive Oxygen Species/metabolism
7.
J Complement Integr Med ; 18(4): 727-735, 2021 Apr 13.
Article En | MEDLINE | ID: mdl-33852232

OBJECTIVES: This study was designed to evaluate the ameliorative effect of almond (Terminalia catappa) leaf (ALE) and stem bark (ABE) extracts on the enzyme activities and oxidative stress markers in the brain and liver tissues of cyclosporine-A (CsA) stressed male albino rats. METHODS: Eighty-eight adult male rats weighing between 200 and 220 g were randomly distributed to into 11 groups (n=8) and different doses (100 and 200 mg/kg bwt.) of ALE and ABE were administered through oral gavages to the normal rats and 50 mg/kg/bwt/day CsA-stressed, while normal control rats was given a saline solution (p.o), and the treatment lasted for 14 days. Blood plasma, liver and brain tissues were prepared for biochemical analysis. RESULTS: Neuronal [acetylcholinesterase (AChE) and butrylcholinesterase (BChE) and arginase] enzyme activities and thiobarbituric acid reactive species (TBARS) level, plasma aspartate transferase (AST), alanine aminotransferase (ALT) and alkaline phosphatase (ALP) activities, liver non-protein thiol (NPSH) level were analyzed. The results revealed that, the administration of CsA induced a significant increase in neuronal AChE, BChE, arginase, TBARS level, but decreased nitric oxide (NO) level. CsA also increased ALT, AST, and ALP activities in the blood plasma of CsA stress rats compared to normal control, but were significantly reversed respectively (p<0.001) upon treatment with the ALE and ABE dose-dependently. CONCLUSIONS: The study revealed that ALE and ABE could prevent neuronal dysfunction and liver toxicity induced by CsA administration, however, higher dose (200 mg/kg) of the studied extracts appears to be more potent.


Chemical and Drug Induced Liver Injury , Prunus dulcis , Terminalia , Acetylcholinesterase/metabolism , Animals , Antioxidants/metabolism , Antioxidants/pharmacology , Brain , Chemical and Drug Induced Liver Injury/drug therapy , Cyclosporine/metabolism , Lipid Peroxidation , Liver/metabolism , Male , Oxidative Stress , Plant Extracts/metabolism , Plant Extracts/pharmacology , Plant Extracts/therapeutic use , Rats , Rats, Wistar
8.
Andrologia ; 53(7): e14074, 2021 Aug.
Article En | MEDLINE | ID: mdl-33930193

Berberine is an isoquinoline alkaloid, found in several plants. Diabetes induces erectile dysfunction (ED) via reduction in some hormones and enzymes implicated in sexual function. This study aimed to investigate the role of berberine on crucial biomolecules linked to penile function in diabetic rats. Sixty-three (63) adult male rats were used and distributed into nine groups (each = 7). Group I-IV normal rats administered with citrate buffer (pH 4.5), sildenafil citrate (SD, 5.0 mg/kg), 50 and 100 mg/kg of berberine, respectively, via oral gavage. Rats in groups V-IX were diabetic rat with ED treated with buffer, SD, 50 and 100 mg/kg of berberine, and acarbose (25 mg/kg ACA) respectively. The result revealed that histological architecture in penile tissues were altered in diabetic groups treated with berberine, sildenafil citrate and acarbose when compared to the diabetic control group. Treatment with berberine, increased testosterone, luteinizing hormone and follicle-stimulating hormone in diabetic rat with ED. Also, reduced prolactin level and acetylcholinesterase, angiotensin-1 converting enzyme, adenosine deaminase and arginase activities were observed in berberine treated diabetic rat with ED. Molecular docking analysis revealed that berberine had strong binding affinities for these enzymes. Thus, berberine could represent a potential therapeutic agent for diabetes-induced ED.


Berberine , Diabetes Mellitus, Experimental , Erectile Dysfunction , Animals , Berberine/pharmacology , Diabetes Mellitus, Experimental/complications , Erectile Dysfunction/drug therapy , Erectile Dysfunction/etiology , Humans , Male , Molecular Docking Simulation , Penile Erection , Penis , Rats , Sildenafil Citrate/pharmacology
9.
J Complement Integr Med ; 18(3): 491-497, 2021 Jan 29.
Article En | MEDLINE | ID: mdl-33544523

OBJECTIVES: This study examined effect of berberine and piperine on neuroprotective potential of neostigmine in the management of neurological disorders. METHODS: Berberine and neostigmine were weighed (30 g), dissolved in distilled water (30 mL) separately, while, 30 mg piperine was dissolved in ethanol (0.45 mL), made up to 30 mL with distilled water. Antioxidant activities in 2, 2-diphenyl-1-picrylhydrazyl radical (DPPH), 2, 2-azinobis (3-ethylbenzothiazoline-6-sulfonate) radical (ABTS), Fe-chelation, ferric reducing properties (FRAP), nitric oxide (NO) and hydroxyl (OH) radical scavenging abilities and Fe2+, cisplatin and sodium nitroprusside (SNP) induced lipid peroxidation (LPO), and acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and monoamine oxidase (MAO) activities were assessed in vitro. RESULTS: The result revealed that tested compounds inhibited enzymes activities dose-dependently. However, berberine (IC50=0.17 mg/mL) had slight higher AChE inhibitory effect than piperine and neostigmine (p<0.05). Also, berberine had the highest BChE inhibitory effect (IC50=0.16 mg/mL) while piperine exhibited the highest MAO inhibitory effect (IC50=0.21 mg/mL). Berberine, piperine and neostigmine exhibited high antioxidant properties and inhibited Fe2+, cisplatin and SNP induced LPO. CONCLUSIONS: Both alkaloids demonstrated antiradical scavenging ability comparable to neostigmine action against Alzheimer's disease (AD). The modulatory and antioxidant berberine and piperine properties on these enzymes (AChE, BChE and MAO) could be possible underlying mechanisms in employing these compounds as a complementary therapy in neurodegenerative diseases (NDDs) management.


Alkaloids , Berberine , Acetylcholinesterase , Alkaloids/pharmacology , Antioxidants/pharmacology , Benzodioxoles , Butyrylcholinesterase , Cholinesterase Inhibitors/pharmacology , Neostigmine , Piperidines , Plant Extracts , Polyunsaturated Alkamides
10.
Metab Brain Dis ; 36(4): 627-638, 2021 04.
Article En | MEDLINE | ID: mdl-33394288

Microglia are immune cells that are resident in central nervous system. Activation of microglial cells are detrimental to the survival of neurons. Thus, prevention of microglia activation and/or protection against microglia activation could be potential therapeutic strategy towards the management of inflammation-mediated neurodegenerative diseases. Moringa oleifera is widely consumed as food and used in folklore medicine for treating several diseases. This study was convened to investigate the effect of aqueous extract of Moringa oleifera on cell viability, cholinergic and purinergic enzymes in BV-2 microglial cultured cell. Aqueous extract of Moringa oleifera was prepared, lyophilized and reconstituted in 0.5% dimethylsulphoxide (DMSO). Cells were treated with Moringa oleifera extracts (0.1-100 µg/mL) and assessed for cell viability and nitric oxide production. Furthermore, the effect of Moringa oleifera on enzymes of cholinergic (acetylcholinesterase) and purinergic (nucleoside triphosphate diphosphohydrolase; NTPDase, 5' nucleotidase and adenosine deaminase; ADA) systems in BV-2 microglial cells were determined. Incubation of BV-2 microglia cell with M. oleifera extract maintained cell viability, modulated cholinergic and purinergic enzymes activity. The phenolic compounds found in M. oleifera extracts, include chlorogenic acid, rutin; quercetin pentoside, kaempferol derivative and quercetin derivative. Thus, this study suggest that the potential therapeutic effect of the phenolic compounds found in M. oleifera may have been responsible for the maintenance of cell viability in BV-2 microglia cells and modulation of cholinergic as well as purinergic enzymes activity.


Microglia/drug effects , Microglia/enzymology , Moringa oleifera , Plant Extracts/pharmacology , 5'-Nucleotidase/metabolism , Acetylcholinesterase/metabolism , Adenosine Deaminase/metabolism , Animals , Cell Line , Cell Survival/drug effects , Cell Survival/physiology , Dose-Response Relationship, Drug , Mice , Plant Extracts/isolation & purification , Plant Leaves , Pyrophosphatases/metabolism
11.
J Food Biochem ; 45(3): e13435, 2021 03.
Article En | MEDLINE | ID: mdl-32794232

We investigated the effect of extracts from the leaf (ALE) and stem bark (ABE) of Almond tree on activities of some crucial enzymes [angiotensin-1 converting enzyme (ACE), arginase, acetylcholinesterase (AChE), phosphodiesterase-5 (PDE-5), adenosine deaminase (ADA), superoxide dismutase (SOD), catalase], and thiobarbituric acid reactive species (TBARS) associated with hypertension in normal adult male Wistar albino rats and Cyclosporine A (CsA)-stressed rats. The result revealed that CsA-stressed rats treated with captopril and extracts (ALE and ABE) had lowered ACE, arginase, AChE, PDE-5, ADA activities, and TBARS level, coupled with improved SOD and catalase activities compared with untreated CsA-stressed rats, which had reversed these biochemicals compared to normal rats. This suggests that the extracts could be explored to suppress hypertension and other cardiac injury known with CsA treatment; the potentials that could be linked with the constituent polyphenols. However, further studies including blood pressure should be determined to ascertain this claim. PRACTICAL APPLICATIONS: Drug-induced cardiotoxicity, hypertension, and organ damage are among the most common side effects of pharmaceutics. Therefore, it becomes imperative to find natural, effective, and alternative therapy with little or no side effect to combat drug toxicity. The use of Almond (leaf and stem bark) in folklore for the treatment/management of hypertension and other heart-related diseases without full scientific basis is on the increase. Hence, this study provides some biochemical evidences on the effect of Almond leaf and stem back extracts on crucial enzymes and oxidative stress markers involve in the incidence of hypertension in the course of Cyclosporine A administration. The findings of this study indicated that the studied plant materials could be promoted as nutraceutical agents to neutralize drug-induced cardiac injury and hypertension.


Hypertension , Prunus dulcis , Terminalia , Animals , Cyclosporine , Hypertension/chemically induced , Hypertension/drug therapy , Male , Oxidative Stress , Plant Bark , Plant Extracts/pharmacology , Plant Extracts/therapeutic use , Plant Leaves , Rats , Rats, Wistar
12.
Immunopharmacol Immunotoxicol ; 42(5): 509-520, 2020 Oct.
Article En | MEDLINE | ID: mdl-32838587

BACKGROUND: This study sought to assess the effect of hesperidin on serum inflammatory cytokines and oxidative damage in liver of complete Freund's adjuvant (CFA)-induced arthritic rats. METHOD: Fifty-six adult female Wistar rats (220-250 g) were acclimatized for two weeks. Intraplantar injection of CFA was done for the induction of arthritis and confirmed on the 14th day prior to oral administration of 40 and 80 mg/kg of hesperidin or dexamethasone for 45 days. RESULT: The result showed that treatment with both doses of hesperidin and dexamethasone in the joint of arthritic rats significantly (p < .05) diminished paw swelling/edema and arthritis score as well as enhanced latency in thermal hyperalgesia test. In addition, hesperidin treatment in arthritis rats showed significant (p < .01) improvement in red blood cells and platelets counts as well as hemoglobin and hematocrit compared to the arthritis control rat group. Furthermore, hesperidin treatment significantly (p < .05) reduced serum interferon gamma (IFN-γ) and interleukin-4 (IL-4) levels in arthritic rat. In addition, treatment with hesperidin significantly (p < .05) decreased the liver of thiobarbituric acid reactive species and reactive oxygen species levels but raised the levels of total and non-protein thiols of rat induced with CFA. The reduced activities of liver δ-aminolevulinate dehydratase, catalase, glutathione-S transferase in arthritic rats were significantly (p < .05) increased with hesperidin treatment in arthritic rats. This study suggests that hesperidin demonstrated an anti-arthritic effect via modulation of serum IFN-γ and IL-4 levels as well as protection against oxidative damage. CONCLUSION: Hence, hesperidin could be a potential immune-modulatory, anti-inflammatory and anti-oxidant agent.


Anti-Inflammatory Agents/pharmacology , Antioxidants/pharmacology , Arthritis, Experimental/drug therapy , Hesperidin/pharmacology , Inflammation Mediators/blood , Interferon-gamma/blood , Interleukin-4/blood , Liver/drug effects , Oxidative Stress/drug effects , Animals , Arthritis, Experimental/chemically induced , Arthritis, Experimental/immunology , Arthritis, Experimental/metabolism , Catalase/metabolism , Female , Freund's Adjuvant , Glutathione Transferase/metabolism , Liver/metabolism , Rats, Wistar , Reactive Oxygen Species/metabolism , Thiobarbituric Acid Reactive Substances/metabolism
13.
Drug Chem Toxicol ; 43(1): 43-50, 2020 Jan.
Article En | MEDLINE | ID: mdl-31475590

This study investigated the effect of Thyme (Thymus vulgaris) leaf aqueous extract (TE) on purine and acetylcholine hydrolyzing enzyme activities and antioxidant status in the brain of 5-fluorouracil (5-FLU) administered rats. Sixty adult Wistar rats (210-225 g) were divided into Ten groups (n = 6). Group 1: received normal saline orally (NC), group 2, 3, 4 and 5 rats were respectively received 100, 200 and 400 mg/kg of TE and Vitamin C (25 mg/kg) orally; group 6 rats received normal saline orally and 150 mg/kg of 5-FLU via i.p., on the last day; rats in group 7, 8, 9 and 10 were orally pretreated with 100, 200 and 400 mg/kg of TE and Vit C (25 mg/kg) respectively, and administered with 150 mg/kg of 5-FLU i.p., on the last day. The purine [adenosine 5'-tri- and di-phosphatases (ATPase and ADPase), adenosine deaminase (ADA)] nucleotide and acetylcholine hydrolyzing [acetylcholinesterase (AChE) and butrylcholinesterase (BChE)] enzymes as well as arginase activities and antioxidant status were assessed. The result revealed that untreated 5-FLU rats had increased enzyme activities, which was reduced in the normal rats treated TE compared to NC. Interestingly, the TE-pretreated rats administered with 5-FLU had reduced enzyme activities compared with untreated 5-FLU rats. The antioxidant status was also normalized in the 5-FLU administered rats pretreated with TE Thus, the neuroprotective mechanisms of TE could be linked to attenuation of neuroactive enzymes and antioxidant status.


Fluorouracil/toxicity , Neuroprotective Agents/pharmacology , Plant Extracts/pharmacology , Thymus Plant/chemistry , Acetylcholine/metabolism , Acetylcholinesterase/metabolism , Animals , Antimetabolites, Antineoplastic/toxicity , Antioxidants/metabolism , Ascorbic Acid/pharmacology , Brain/drug effects , Brain/enzymology , Butyrylcholinesterase/metabolism , Dose-Response Relationship, Drug , Female , Male , Neuroprotective Agents/administration & dosage , Neuroprotective Agents/isolation & purification , Plant Extracts/administration & dosage , Plant Leaves , Rats , Rats, Wistar
14.
Cell Biochem Funct ; 37(7): 474-485, 2019 Oct.
Article En | MEDLINE | ID: mdl-31365139

The effect of quercetin was assessed in rats induced with complete Freund adjuvant (CFA). Arthritis scores, paw oedema, latency, activities of myeloperoxidase (MPO), ectonucleoside triphosphate diphosphohydrolase (E-NTPDase), and ectoadenosine deaminase (E-ADA) in lymphocytes were determined. Furthermore, nucleotide and nucleoside levels as well as the secretion of pro- and anti-inflammatory cytokines were evaluated. Animals were treated with saline and quercetin in doses of 5, 25, and 50 mg/kg for 45 days. The result revealed that quercetin (50 mg/kg) reduced arthritis score and paw oedema, and increased the latency in the thermal hyperalgesia test. Histopathological analysis showed that all the doses of quercetin reduced infiltration of inflammatory cells. MPO activity was increased in the arthritis group; however, quercetin reduced this activity. E-NTPDase activity was increased in lymphocytes of arthritis rats, and treatment with quercetin reversed this increase. However, E-ADA activity was reduced in the arthritis group, and treatment with quercetin modulated the activity of this enzyme in arthritis rat groups. Serum adenosine levels were increased in arthritis, and the levels were lowered with quercetin treatment. Quercetin treatment in arthritis groups decreased the elevated levels of cytokines in the arthritis control group. Thus, quercetin demonstrated an anti-inflammatory effect, and this flavonoid may be a promising natural compound for the treatment of arthritis. SIGNIFICANCE OF THE STUDY: Quercetin may represent a potential therapeutic compound in the treatment of rheumatoid arthritis. Findings from this study indicate that quercetin suppresses swelling and attenuates the underlying inflammatory responses. This is the first report where quercetin was shown to modulate the immune response to arthritis via attenuation of the purinergic system (E-NTPDase and E-ADA activities) and the levels of IFN-gamma and IL-4. Thus, this work is relevant to basic research and may be translated into clinical practice.


AMP Deaminase/antagonists & inhibitors , Adenosine Triphosphatases/antagonists & inhibitors , Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Arthritis, Rheumatoid/drug therapy , Cytokines/antagonists & inhibitors , Enzyme Inhibitors/pharmacology , Quercetin/pharmacology , AMP Deaminase/metabolism , Adenosine Triphosphatases/metabolism , Animals , Arthritis, Rheumatoid/chemically induced , Arthritis, Rheumatoid/metabolism , Cytokines/metabolism , Edema/chemically induced , Edema/drug therapy , Edema/metabolism , Female , Freund's Adjuvant , Rats , Rats, Wistar
15.
Andrologia ; 51(6): e13281, 2019 Jul.
Article En | MEDLINE | ID: mdl-30983021

This study investigated effect of p-coumaric acid (PCA) on erectogenic enzyme activity and non-protein thiol level in the penile tissue of normal and doxorubicin (DOX)-induced oxidative stress male rat. Sixty-four (64) adult male rats weighing between 170 and 180 g were used for this work. After 14 days of acclimatisation, the rats were divided into eight groups (n = 8). Rats were orally pre-treated with PCA dose dependently (50 and 100 mg/kg body weight [b.w.t]) and vitamin E (100 mg/kg b.w.t) for 14 days before induction with a single dose of DOX (15 mg/kg b.w.t, via i.p.). The result revealed that arginase, acetylcholinesterase (AChE), angiotensin-I-converting enzyme (ACE), phosphodiesterase-5 (PDE-5), adenosine monophosphohydrolase (AMPdase) activities were significantly (p < 0.05) higher in the DOX-induced rats as against the control, which was significantly p < 0.05) higher when compared to normal rats treated with PCA. PCA also improved non-protein thiol level in the penile tissue of both normal and DOX-induced rats. Hence, this study revealed that PCA is capable of causing inhibitory effects on the activities of enzymes, associated with oxidative stress-induced erectile dysfunction (ED) and could also be used as an aphrodisiac agent in the management/treatment of ED.


Antioxidants/pharmacology , Erectile Dysfunction/drug therapy , Oxidative Stress/drug effects , Penis/drug effects , Propionates/pharmacology , Animals , Antioxidants/therapeutic use , Coumaric Acids , Disease Models, Animal , Doxorubicin/toxicity , Erectile Dysfunction/etiology , Erectile Dysfunction/physiopathology , Humans , Male , Oxidative Stress/physiology , Penile Erection/drug effects , Penile Erection/physiology , Penis/chemistry , Penis/enzymology , Propionates/therapeutic use , Rats , Sulfhydryl Compounds/analysis , Sulfhydryl Compounds/metabolism
16.
J Basic Clin Physiol Pharmacol ; 30(2): 185-193, 2018 Nov 13.
Article En | MEDLINE | ID: mdl-30422801

Background Eugenol is the foremost constituent of clove oil and widely distributed in many plants. It possesses many pharmaceutical applications, including antioxidant, anti-inflammatory, and anti-tumorigenic properties, among others. This study evaluates the influence of eugenol on oxidative stress biomarkers in the liver of carrageenan-induced arthritis (CIA) rats. Methods Sixty albino rats were randomly divided into 10 (n=6) groups. Group I is the control group that received saline solution orally. Groups II and VII rats received 2.5 mg/kg of eugenol orally (EUG-2.5). Rats in groups III/VIII and IV/IX received 5 and 10 mg/kg of eugenol orally (EUG-5 and EUG-10), respectively. Groups V and X received 0.2 mg/kg of dexamethasone (DEX-0.2) orally. Groups VI to X were injected with 1% carrageenan intra-articularly. Behavioral studies were conducted after 21 days of treatment. Thereafter, the animals were sacrificed, and the livers were isolated and used for biochemical analysis. Results Reduced body weight in arthritic rats was recorded compared to normal controls. Reduced tibiofemoral joint edema and increased spontaneous movement were observed in CIA rats with decreased superoxide dismutase, catalase, reduced glutathione (GSH), glutathione peroxidase, and GSH S-transferase activities compared with the normal control group. Increased endogenous enzyme activities and decreased elevated lipid peroxidation were also observed after eugenol treatment. Conclusion Eugenol ameliorates carrageenan-induced oxidative stress in the liver of arthritic rats.


Arthritis/drug therapy , Biomarkers/metabolism , Carrageenan/pharmacology , Eugenol/pharmacology , Liver/drug effects , Liver/metabolism , Oxidative Stress/drug effects , Animals , Antioxidants/metabolism , Arthritis/chemically induced , Arthritis/metabolism , Catalase/metabolism , Glutathione/metabolism , Glutathione Peroxidase/metabolism , Lipid Peroxidation/drug effects , Rats , Rats, Wistar , Superoxide Dismutase/metabolism
17.
Biomed Pharmacother ; 106: 1616-1623, 2018 Oct.
Article En | MEDLINE | ID: mdl-30119237

This study investigated the effect of eugenol on arginase, nucleotidase and adenosine deaminase activities in platelets of carrageenan-induced arthritic rat model to explain a possible anti-arthritic mechanism of eugenol. Fifty adult female rats (140-250 g) were divided into ten (10) groups (n = 5). Group I received oral administration of corn oil, group II received 2.50 mg/kg of eugenol, group III and IV rats received oral administration of 5.0 and 10.0 mg/kg of eugenol respectively, group V received 0.20 mg/kg of dexamethasone orally, group VI rats was injected with 1% carrageenan (arthritic rats) and received saline solution orally (arthritic control rat group), group VII, VIII and IX: arthritic rats received 2.50, 5.0 or 10 mg/kg of eugenol orally respectively, group X: arthritic rats was administered with 0.20 mg/kg of dexamethasone orally. The animals were treated for 21 days, thereafter, tibiofemoral histological examination, thiobabituric acid reactive substances level, arginase, nucleoside triphosphate diphosphohydrolase, 5´-nucleotidase and adenosine deaminase activities were assessed. Tibiofemoral histological examination result showed that infiltration of inflammatory cells was significantly decreased with an increase in eugenol dose. Activities of arginase, adenosine triphosphate and adenosine monophosphate hydrolyses were significantly decreased while adenosine diphosphate hydrolysis and adenosine deaminase activities were significantly increased in arthritic rat groups administered with different doses of eugenol. Therefore, eugenol might be a natural complement and alternative promising anti-arthritic agent. These possible anti-arthritic mechanisms may be partly through the modulation of arginase and adenosine nucleotides hydrolyzing enzyme activities as well as the antioxidative action of eugenol.


5'-Nucleotidase/antagonists & inhibitors , Adenosine Deaminase/metabolism , Anti-Inflammatory Agents/pharmacology , Arginase/antagonists & inhibitors , Arthritis, Experimental/prevention & control , Blood Platelets/drug effects , Carrageenan , Enzyme Inhibitors/pharmacology , Eugenol/pharmacology , Joints/drug effects , 5'-Nucleotidase/metabolism , Adenosine Diphosphate/blood , Adenosine Monophosphate/blood , Adenosine Triphosphate/blood , Animals , Antioxidants/pharmacology , Arginase/metabolism , Arthritis, Experimental/chemically induced , Arthritis, Experimental/enzymology , Arthritis, Experimental/pathology , Blood Platelets/enzymology , Dexamethasone/pharmacology , Female , GPI-Linked Proteins/antagonists & inhibitors , GPI-Linked Proteins/metabolism , Hydrolysis , Joints/metabolism , Joints/pathology , Oxidative Stress/drug effects , Rats, Wistar , Thiobarbituric Acid Reactive Substances/metabolism
18.
Toxicol Mech Methods ; 28(8): 573-586, 2018 Oct.
Article En | MEDLINE | ID: mdl-29781752

White Butterfly (Clerodendrum volubile) leaf is commonly used in traditional medicine for the management of various diseases including diabetes without the full understanding of the scientific basis for its use. This study sought to evaluate the antihyperglycemic, antihyperlipidemic and antioxidant effect of C. volubile leaves in streptozotocin (STZ)-induced diabetic rats. Aqueous extract of C. volubile was prepared and its effect assessed on relevant enzymes associated with diabetes. Fifty male Wistar rats were randomly separated into 10 groups each containing five rats. The induction of diabetes in rats was by a single intraperitoneal injection of STZ (65 mg/kg body weight) while C. volubile extract was administered orally to diabetic and non-diabetic animals, at the doses of 50, 100 and 200 mg/kg body weight for 14 days. Metformin (100 mg/kg body weight) served as positive control. Clerodendrum volubile extract inhibited α-glucosidase (IC50 = 0.20 mg/ml) and α-amylase (IC50 = 0.58 mg/ml). Furthermore, administration of C. volubile extract significantly reduced the elevated plasma glucose level and body weight, improved kidney functions, attenuated oxidative stress by decreasing MDA levels, enhancing superoxide dismutase, catalase and glutathione peroxidase activities, reinstated the lipid profile to nearly normal level and restored pancreatic histological integrity in diabetic rats. The results reveal that C. volubile represents a source of phytochemicals that exerts their antidiabetic effects through the modulation of glycemic and atherogenic indices as well as mitigation of free-radical-mediated damage.


Antioxidants/metabolism , Blood Glucose/analysis , Clerodendrum/chemistry , Diabetes Mellitus, Experimental/drug therapy , Hypoglycemic Agents/therapeutic use , Lipids/blood , Plant Extracts/therapeutic use , Animals , Diabetes Mellitus, Experimental/blood , Hypoglycemic Agents/isolation & purification , Hypoglycemic Agents/toxicity , Male , Plant Extracts/isolation & purification , Plant Extracts/toxicity , Plant Leaves/chemistry , Rats, Wistar , Streptozocin , Toxicity Tests, Acute
19.
J Diet Suppl ; 15(6): 977-1009, 2018 Nov 02.
Article En | MEDLINE | ID: mdl-29281341

Functional foods describe the importance of foods in promoting health and preventing diseases aside their primary role of providing the body with the required amount of essential nutrients such as proteins, carbohydrates, vitamins, fats, and oils needed for its healthy survival. This review explains the interaction of functional food bioactive compounds including polyphenols (phenolic acids [hydroxybenzoic acids and hydroxycinnamic acids], flavonoids [flavonols, flavones, flavanols, flavanones, isoflavones, proanthocyanidins], stilbenes, and lignans), terpenoids, carotenoids, alkaloids, omega-3 and polyunsaturated fatty acids, among others with critical enzymes (α- amylase, α- glucosidase, angiotensin-I converting enzyme [ACE], acetylcholinesterase [AChE], and arginase) linked to some degenerative diseases (type-2 diabetes, cardiovascular diseases [hypertension], neurodegenerative diseases [Alzheimer's disease] and erectile dysfunction). Different functional food bioactive compounds may synergistically/additively confer an overwhelming protection against these degenerative diseases by modulating/altering the activities of these critical enzymes of physiological importance.


Chronic Disease/prevention & control , Chronic Disease/therapy , Dietary Supplements , Functional Food , Health Promotion , Alkaloids/administration & dosage , Cardiovascular Diseases/diet therapy , Cardiovascular Diseases/prevention & control , Carotenoids/administration & dosage , Diabetes Mellitus, Type 2/diet therapy , Diabetes Mellitus, Type 2/prevention & control , Erectile Dysfunction/diet therapy , Erectile Dysfunction/prevention & control , Flavonoids/administration & dosage , Humans , Lignans/administration & dosage , Male , Neurodegenerative Diseases/drug therapy , Neurodegenerative Diseases/prevention & control , Nutritional Requirements , Phenols/administration & dosage , Polyphenols/administration & dosage , Stilbenes/administration & dosage
20.
Food Funct ; 8(12): 4459-4468, 2017 Dec 13.
Article En | MEDLINE | ID: mdl-29090709

The present study seeks to investigate the effect of rutin, a flavonoid compound in rat models of acute inflammation induced by carrageenan (CAR). Twenty-four female Wistar rats weighing 222-247 g received saline or 2% λ-carrageenan in the pleural cavity and treatment with rutin (80 mg kg-1) or saline by oral gavage for 21 days prior to the intrapleural induction of CAR. After 4 h of induction, the rats were euthanized, the plasma was prepared from the blood for the analysis of haematological parameters and the pleural exudate was obtained for the analysis of the total cell count, cell viability, reactive oxygen species (ROS) production, apoptosis and cell cycle. The result revealed that rutin exhibited anti-inflammatory effects by modulating the ROS level, apoptosis and cell cycle. This study indicates that rutin may exert a protective effect against ROS-mediated oxidative damage associated with an anti-inflammatory activity in rat models of acute inflammation.


Anti-Inflammatory Agents/administration & dosage , Apoptosis/drug effects , Lung Diseases/drug therapy , Pleura/drug effects , Reactive Oxygen Species/metabolism , Rutin/administration & dosage , Animals , Carrageenan/adverse effects , Cell Cycle/drug effects , Female , Humans , Lung Diseases/immunology , Lung Diseases/metabolism , Lung Diseases/physiopathology , Pleura/cytology , Pleura/metabolism , Rats , Rats, Wistar
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