Tropical Journal of Drug Research is an international peer-reviewed journal with expedited processing times presenting the very latest research results related to novel and established drug molecules and the evaluation of new drug development. A key focus of the publication is translational medicine and the application of biological discoveries in the development of drugs for use in the clinical environment. Articles and experimental data from across the field of drug research address not only the issue of drug discovery, but also the statistical methods for evaluating results from experimental investigations and clinical trials. Publishing twelve times a year, Tropical Journal of Drug Research includes original research articles and modelling approaches as well as reviews, commentaries and short communications in the following areas: Medicinal chemistry and drug formulations Biochemistry and molecular biology Clinical and experimental pharmacology Drug interactions Pharmacodynamics Pharmacokinetics and systems pharmacology Toxicology, preclinical safety and early development Analytics applied to clinical trials Drug Formation Drug design Molecular targets of drugs Clinical Pharmacy/Pharmacy Practice
Time Course of Lead-Induced Dyslipidemia in Male Wistar Rats
Purpose: Previous studies have linked lead toxicity to dyslipidemia. However, this has not been well characterized in a time course study. This study investigates the effects of lead exposure on lipid metabolism with time, using a rat model. Method: Seventy-two (72) male Wistar rats were exposed to lead at concentrations of 0, 200, 300, and 400 ppm in their drinking water for 4, 8 and 12 weeks, after which blood, liver, kidney, brain, heart, spleen and lungs were removed from the animals and analyzed for lead and lipid dynamics. Results: Lead-induced inhibition of reverse cholesterol transport was both time-dependent as well as dose-dependent at 4 and 8 weeks. Plasma free fatty acids (FFAs) displayed a hormetic-like response at 4 weeks and increased dose-dependently at 12 weeks while erythrocyte FFAs increased in the 200 ppm dose at 4 weeks and in all the doses at 8 weeks. Increased hepatic, brain and renal cholesterogenesis were generally observed with highest increases occurring at 8 weeks in both organs. Hepatic, brain, renal, cardiac and pulmonary phospholipidosis were observed in all the lead doses and exposures. Cardiac cholesterol decreased while triglycerides increased at 4 weeks. Increases in hepatic and brain cholesterogenesis were neither dose nor time-dependent. Correlation studies showed both direct and inverse correlations between tissue lead and various lipid parameters. Conclusion: Lead exposure induced significant dyslipidemia and altered cholesterol metabolism over time, underscoring potential cardiovascular and metabolic risks.
Hydoxymethylglutaryl coenzyme A reductase.
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Phytochemical Screening, Gas Chromatography-Mass Spectrometry Analysis and Invitro antioxidant Activities of the Seed, Leaf and Essential oils of Petroselinum Crispum, Parsley (Mill.) Nym. Ex A.W. Hill, Apiaceae)
Purpose: This study investigated the phytochemistry and bioactive compounds in extracts of seed, leaf, and essential oils, as well as the in vitro antioxidant activity of Petroselinum crispum. Methods: Preliminary phytochemical evaluations used standard methods, and Gas Chromatography-Mass Spectrometry (GC-MS) analyzed the bioactive compounds. The antioxidant activity was assessed by the 1, 1-diphenyl-2-picrylhydrazyl (DPPH) reduction test. Results: The extracts contained major classes of phytochemicals, including flavonoids, alkaloids, terpenoids, and phenols; anthraquinones were absent in all extracts. Terpenoids were notably present in all extracts, with the highest in the seed essential oil (8.994 mg/g). GC–MS analysis identified 18 bioactive compounds in the aqueous seed extract and 26 in the ethanol seed extract, with Apiol making up 81.04% and 81.54%, respectively. For the leaf extract, 38 compounds in the aqueous form and 40 in the ethanol form were identified, with the highest percentages being 13.00% (MonoPalmitin) and 17.58% (Palmitic acid). The GC–MS analysis of the essential oils revealed 30 compounds in the seed oil and 52 in the leaf oil, with Apiol at 88.93% and Oleic acid at 17.67%, respectively. The aqueous seed extract of P. crispum showed the strongest antioxidant activity, with an IC50 of 6.7 μg/mL, while all other extracts exhibited antioxidant activity lower than the standard ascorbic acid (IC50=7.1 μg/mL). Conclusion: Overall the findings highlight numerous bioactive compounds in the seeds, leaves, and essential oil of P. crispum, with Apiol as the dominant compound in both the seed and essential oil. The presence of Apiol, along with other phenolics, volatile compounds, flavonoids, and terpenoids, contribute significantly to the plants’ antioxidant potential. This property may offer valuable applications in culinary, pharmaceutical and therapeutic fields.
In-vitro, Bioinformatics and Computational Biophysical Analyses of Antifungal Phytochemicals from Acalypha wilkesiana Variants Targeting Malassezia Lipase
Purpose: Seborrheic dermatitis (SD) is a common chronic inflammatory skin disorder, often associated with the activity of lipid-hydrolyzing enzymes secreted by Malassezia globosa. Conventional antifungals often show limited efficacy and adverse effects, while the mechanisms underlying traditional remedies like Acalypha wilkesiana remain underexplored. Methods: This study evaluated the antifungal potential of phytochemicals derived from the red and green variants of A. wikesiana, targeting M. globosa lipase (PDB ID: 3UUE). Crude ethanol extracts were analyzed via gas chromatography–mass spectrometry (GC-MS), and preliminary in-vitro antifungal activity was assessed against M. globosa. Identified compounds were subjected to molecular docking and molecular dynamics (MD) simulations to assess binding affinity and stability. ADMET profiling and density functional theory (DFT) calculations were employed to predict pharmacokinetics, toxicity, and electronic reactivity. Results: The red A. wikesiana extract demonstrated strong antifungal activity, producing a 60 mm inhibition zone, while the green variant was inactive. Molecular docking identified aspidospermidin-17-ol, 1-acetyl-19,21-epoxy-15,16-dimethoxy- (ASP) as the top-performing compound with a binding affinity of –6.8 kcal/mol, outperforming ketoconazole and the native ligand. MD simulations confirmed the structural stability of the ASP–lipase complex, exhibiting minimal RMSD fluctuations. ADMET predictions indicated low dermal and systemic toxicity, and DFT analysis confirmed favorable electronic properties. Conclusion: The findings highlight ASP from red A. wikesiana as a potent and safe inhibitor of M. globosa lipase, supporting its potential development as a novel, plant-based topical antifungal agent for the management of seborrheic dermatitis.
Histological Investigation of the Protective Effect of Lonchocarpus griffonianus (Baill.) Dunn (Fabaceae) Stem Bark Extract on Aluminium Chloride-induced Testicular Toxicity in Albino Mice
Purpose: Complications associated with male infertility, such as relationship issues and stress brought on by not being able to conceive, as well as the cost of fertility treatments, have led to a desire for safe, inexpensive, and easily accessible fertility-enhancing herbal remedies. Lonchocarpus griffonianus (Fabaceae) is utilized by the natives of Akwa Ibom State, Nigeria, to treat pharyngopulmonary disorders, stomachaches, infertility, amenorrhea, and inflammatory disorders. This study aims to validate the use of L. griffonianus in the management of infertility in ethnomedicine. Methods: L. griffonianus stem bark was collected, identified, dried, pulverised, and then extracted with absolute methanol. Aluminium chloride (4.3mg/kg) was given intraperitoneally to the animals to induce reproductive toxicity for 28 days. The extract was administered at graded doses of 100, 200, and 400 mg/kg orally, along with Aluminium chloride, for 28 days. On day 29, the animals were sacrificed under anaesthesia. The animal’s testes were harvested for histological analysis. Results: The demonstrated significant restorative effects on aluminium chloride–induced testicular toxicity in male mice. The standard control group exhibited normal testicular histoarchitecture with intact germ cells and spermatozoa. In contrast, the disease control group showed vacuolated connective tissue, atrophied spermatids, and scanty spermatozoa. Treatment with the extract (100–400 mg/kg) markedly improved spermatogenesis. Conclusion: L. griffonianus stem bark extract attenuated AlCl3-induced testicular toxicity, indicating its potential as a lead for developing herbal therapies against male infertility.
Public Health implications of the microbiological analysis of Zobo (Hibiscus sabdariffa) drink produced and hawked in Eket, South-South Nigeria
Purpose: Zobo drink is a local, cheaper soft drink made from Hibiscus sabdariffa calyx, which is an herbaceous medicinal plant grown in the tropics. The study was designed to assess the Public Health implications of the microbiological analysis of Zobo (Hibiscus sabdariffa) drink produced and hawked in Eket, South-South Nigeria. Methods: Hawked Zobo drinks packaged in plastic bottles were purchased from ten different hawkers at different locations. Nutrient Agar (NA), MacConkey Agar (MCA), Salmonella Shigella Agar (SSA) and Sabouraud Dextrose Agar (SDA) were used for analysis of bacteria and fungi. Different microscopic and biochemical tests were employed to further identify the bacterial and fungal isolates. Results: The bacteria isolated from the samples analyzed include Staphylococcus aureus, Salmonella spp, Pseudomonas spp., Escherichia coli, Streptococcus spp., Campylobacter spp., Lactobacillus spp., and Klebsiella spp., with the highest percentage of occurrence being S. aureus. The total bacterial count ranged from 2.6 to 6.6 x103 cfu/ml in Nutrient agar, 1.0 to 2.5 x 103 cfu/ml in MacConkey agar and 2.4 to 7.3 x 103 cfu/ml in Salmonella-shigella agar. The fungi isolated from the samples were yeast (Saccharomyces cerevisiae), Aspergillus sp, Fusarium sp, Penicillium sp and Rhizopus sp., with a total count ranging from 5.4 to 9.1 x 104 cfu/ml in Sabouraud dextrose agar. Conclusion: As Pubic Health implication, the likely sources of contamination of the zobo drinks analyzed are from the handlers, equipment and utensils used for processing, the water source and the method of dispensing into nylon or plastic bottles.
Phytochemical Constituents of Methanol Leaf Extract of Ficus capensis and the Assessment of Its Toxicity on Adult Wistar Rats
Purpose: This study aimed to evaluate the phytochemical constituents and conduct a detailed toxicological assessment of Ficus capensis methanolic leaf extract in Wistar rats. The primary objective was to document its previously undocumented toxicity profile and potential for genetic damage, given its recognized therapeutic and medicinal value. Methods: Ficus capensis leaf was methanol-extracted for phytochemical screening and proximate analysis. Toxicity assessment involved acute (up to 5000 mg/kg) and 28-day sub-chronic studies. In the sub-chronic phase, twenty Wistar rats per group received oral doses of 10, 100, or 1000 mg/kg body weight, with a control group receiving distilled water. Post-treatment, rats were sacrificed, and tissues were analyzed for biochemical parameters (ALT, AST, ALP, total protein, bilirubin), hematology, histopathology, and genotoxicity (Comet Assay). Results: Phytochemical analysis confirmed tannins, phenols, flavonoids, alkaloids, saponins, and cardiac glycosides. Proximate analysis showed 19.69% protein and 37.15% carbohydrates. Acute toxicity tests revealed no mortality or toxicity signs at up to 5000 mg/kg. The sub-chronic study demonstrated no significant changes in biochemical or hematological parameters across treated groups. Histopathological analysis showed no adverse effects on the liver or kidney. Crucially, the Comet assay indicated no genetic damage, with no significant differences in % Tail DNA or Tail moment. Conclusion: These findings strongly suggest that Ficus capensis leaf extract exhibits no toxicity or DNA damaging effects. This comprehensive toxicological assessment underscores its potential as a safe therapeutic alternative, with active compounds that may offer protective benefits against toxicity.
Acute Oral Toxicity of a Novel Pharmaceutical Excipient (Grewia gum) in Wistar Rats
Purpose: Grewia gum is reported to possess significant potential as a natural pharmaceuti cal excipient. However, there is currently a lack of information regarding its toxicity in animal models. Methods: The acute oral toxicity of Grewia gum (G. mollis) was evaluated in female Wistar rats using a fixed-dose procedure as outlined in Organisation for Economic Co-operation and Development Guideline No. 420. The animals were monitored for mortality, behavioural, biochemical, and haematological changes and their vital organs were preserved for histopathological analysis. Results:The results indicated no mortality, systemic toxicity, or behavioural changes in the rats administered Grewia gum, with the oral median lethal dose (LD50) exceeding 2000 mg/kg. Grewia gum did not affect food and water consumption in the animals. However, the concentrations of serum bicarbonate, total bilirubin and total protein increased significantly (p < 0.05) in the Grewia gum-treated animals. Furthermore, the administration of Grewia gum resulted in a significant reduction in mean corpuscular haemoglobin concentration (MCHC) values, which suggests subtle effect on haematopoietic tissue. Microscopic examinations of organ sections from both the control and Grewia gum-treated groups revealed no abnormalities. Conclusion:Thus, oral administration of Grewia gum resulted in mild effects on serum liver and haematological indices, indicating that the gum is safe at the present level of exposure in rats.
Exploring the efficacy of Calotropis procera methanol leaf extract with standard antimalarial drugs in the murine malaria model
Purpose: The emergence and proliferation of drug-resistant Plasmodium falciparum has critically compromised the efficacy of traditional antimalarial treatments significantly challenging global control efforts. There is a growing scientific focus on exploring plant-based therapies as complementary or alternative options for antimalarial treatment. This investigation sought to examine the antimalarial effect of Calotropis procera methanol leaf extract (MLCP) alone and in combination with standard antimalarial drugs in Plasmodium berghei-infected mice. Methods: Standard protocols were followed for oral acute toxicity evaluation and phytochemical tests of MLCP. Curative and prophylactic effects of MLCP individually and in combination with chloroquine (CQ), artesunate (ART), and pyrimethamine (PYR), were evaluated using recognized experimental techniques in Plasmodium berghei-infected mice. Results: MLCP at 200 and 400 mg/kg doses produced a marked decrease (p < 0.05) in parasitemia levels in both tests. In the curative study, the combination of MLCP + CQ (200/10 mg/kg) and MLCP + ART (200/5 mg/kg) considerably (p < 0.05) reduced parasitemia levels. The percentage of chemosuppression produced by MLCP + CQ (86.9 %) was better than CQ alone (47.2 %). However, the MLCP + ART combination and ART alone produced similar parasite suppressive effects with percentage chemosuppression of 73.6 % and 74.7 %, respectively. In the prophylactic test, the MLCP + PYR (200/1.2 mg/kg) combination produced a chemosuppression of 78.7 % compared to PYR alone which produced a chemosuppression of 78.0 %. Conclusion: The findings show that combining Calotropis procera leaves with standard antimalarial chloroquine enhanced antimalarial efficacy against Plasmodium berghei infection in mice.
Effects of Quercetin on Brain Architecture in Lipopolysaccharide-Induced Neuroinflammation in Mice
Purpose: Neuroinflammation is associated with oxidative stress, thereby leading to neuronal dysfunctions in the central nervous system. Quercetin is a well-known potent anti-oxidant capable of reducing the generation of free radicals. Preventing the generation of free radical may be a valuable therapeutic approach in the management of disorders such as Parkinson’s disease, multiples sclerosis and Alzheimer’s disease associated with neuroinflammation. This work was therefore designed to investigate the effect of quercetin on brain architecture in lipopolysaccharide (LPS) induced neuroinflammation in mice. Method: Fifteen (15) animals (mice) were randomly divided into a group of three consisting of five animals in each group. Neuroinflammation was induced by a single injection of 2 mg/kg Escherichia coli bacterial lipopolysaccharide (serotype 055:B5, Sigma, St Louis, MO, USA) dissolved in 0.9% sterile saline intra-peritonially (IP). Group A served as the control group and was administered distilled water for a period of three days while group B received only LPS meanwhile group C was induced and treated with quercetin (40 mg/kg p.o) for three days. After three days, all animals were sacrificed, and their brain tissues were carefully collected for analysis. Dendritic arborization and deoxyribonucleic acid (DNA) were quantified using silver stain and feulgen stain respectively Results: Silver stain revealed that quercetin in group C prevented axonal loss as compared to untreated group B. Meanwhile in the feulgen stain, the DNA was preserved by quercetin as compared to untreated group B. Conclusion: This study has clearly revealed that quercetin prevented neuronal dysfunction during neuroinflammation through mechanisms that may involve preventing axonal and DNA loss.
Sub-Chronic Toxicity: Biochemical, Hematological and Histopathological Effects of Picralima nitida (Apocynaeceae) Root Bark
Purpose: Picralima nitida, commonly called Akuamma, is a plant native to West Africa, and has been traditionally used for its medicinal properties. This study aimed to investigate the sub-chronic toxicity, with specific focus on biochemical, haematological and histopathological effects of the root bark of Picralima nitida. Methods: Adult male Wistar rats were randomly divided into four groups: Group 1 (control) received distilled water only, Groups 2 – 4 (treatment groups) were administered 50, 100, and 200 mg/kg of P. nitida root bark methanol extract, respectively orally once daily for 28 days. On the 29th day, rats were sacrificed, blood samples were collected for biochemical and haematological analyses, while vital organs (liver, kidney, and heart) were excised and used for histopathological analysis. Results: Results showed that the sub-chronic administration of P. nitida root bark did not cause significant changes in serum biochemical and haematological parameters in rats. However, the extract produced significant (P<0.05) increases in mid cells (MID), mean corpuscular volume (MCV) and mean corpuscular hemoglobin (MCH) when compared to the control. No significant increase (P>0.05) was observed in white blood cell (WBC) count, red blood cell (RBC) count, and hemoglobin (HGB) concentration. Histopathological examination revealed normal tissue architecture, although the presence of immunological cells, and vasodilatation may indicate toxicity. Conclusion: Findings from the study suggest that the root bark extract of P. nitida is nontoxic, and relatively safe on sub-chronic administration. However, further studies are needed with higher doses and longer duration of administration to fully understand the plant's toxicity.
Analgesic and Anti-inflammatory Activities of Leaf, Stem and Root Essential Oils of Borassus aethiopum (Arecaceae)
Purpose: Pain and inflammation have received man’s attention from time immemorial. Borassus aethiopum, a large fan shaped tree is found in Africa, with reported nutritional and biological activities. This study was designed to investigate the analgesic and anti-inflammatory activities of the leaf, stem and root essential oils of Borassus aethiopum. Methods: Plant sample was obtained from Gboko, Nigeria. Essential oils from leaf, stem and roots of this plant were extracted by hydro distillation using all-glass Clevenger apparatus. Acute toxicity test on essential oil samples of Borassus aethiopum was carried out using various dosages. Analgesic activity of these essential oils was investigated by measuring the number of acetic acid induced writhing in rats while oedema volume of rat’s paw was used to determine the anti-inflammatory activity of the essential oil samples. Results: Essential oil samples were safe at 25 ml/kg bodyweight. Analgesic activity of essential oil was best on leaf (71.4%) at 15 ml/kg; stem (94.64%) at 10 ml/kg; root (78.2%) at 10 ml/kg and root (77.6%) at 15 ml/kg bodyweight. During investigation of anti-inflammatory activity, all three essential oil samples: leaf, stem and roots showed better activity than the standard drug, indomethacin. However, leaf essential oil showed early phase inhibitory activity (0 minute) while late phase inhibitory effect (120 minutes) was seen in root essential oils of Borassus aethiopum. Conclusion: Results show that leaf, stem and root essential oils of Borassus aethiopum exhibited analgesic and anti-inflammatory activities and suggests their promise as drugs.
Activity of Vinpocetine in the Cerebellum of Nickel Chloride-Exposed Rats: An in-vivo and in-silico Study
Purpose: Nickel chloride (NiCl2), widely used in industry, poses neurotoxic risks, particularly to the cerebellum, which regulates motor and cognitive functions. Vinpocetine, an antioxidant and anti-inflammatory agent, may offer neuroprotection. This study investigated vinpocetine’s protective effects against NiCl2-induced cerebellar toxicity in Wistar rats. Methods: Forty-eight (42) Wistar rats were randomly distributed to six groups (n=8) and received the following treatments. Group A (control) - 1 ml distilled water; Group B - 5 mg/kg NiCl2; Groups C and D - 2.5 mg/kg and 5 mg/kg vinpocetine, respectively, alongside 5 mg/kg NiCl2; Groups E and F - 2.5 mg/kg and 5 mg/kg vinpocetine, respectively. Treatments were administered orally for 28 days, followed by neurobehavioral, oxidative stress, histological, and in-silico assessments. Results: NiCl2 significantly (p<0.05) reduced body, brain, and relative cerebellar weight. Behavioral deficits included impaired grip strength, coordination, and mobility. Oxidative stress markers showed reduced antioxidant enzymes activity and elevated lipid peroxidation. Histological examination revealed Purkinje cell degeneration and pyknotic nuclei in NiCl2-exposed rats. Vinpocetine treatment significantly improved motor function, antioxidant activity, and cerebellar structure while reducing oxidative damage. Conclusion: These findings suggest that vinpocetine protects against NiCl2-induced cerebellar toxicity in Wistar rats
Effects of 2’-hydroxychalcones against Oxidative Stress and Lipid Peroxidation Biomarkers in Paclitaxel-Induced Peripheral Neuropathy in Drosophila Melanogaster (Harwich Strain)
Purpose: Chemotherapy-induced peripheral neuropathy (CIPN), a common adverse effect of paclitaxel treatment, significantly impacts patients' quality of life. This study investigates the potential of 2’-hydroxychalcones, natural compounds with neuroprotective properties, to alleviate paclitaxel-induced peripheral neuropathy (PIPN). Methods: Leveraging the Drosophila melanogaster model, the research evaluates the compounds' effects on oxidative stress markers, Superoxide Dismutase (SOD), Reduced Glutathione (GSH) and lipid peroxidation biomarker Malondialdehyde (MDA). Flies were grouped into five groups (groups 1 to 5). Group 1 served as a positive control, group 2 the negative control exposed to Paclitaxel only, while groups 3 and 4 were served 100mg and 150mg/10ml feed 2’-hydroxychalcones, respectively, and group 5 was served Gabapentin, the standard drug. The flies were later on homogenized and the homogenates were used to assay for oxidative stress biomarkers (SOD, GSH) and lipid peroxidation (MDA) by spectrometry. Our results reveal that Paclitaxel exposure leads to significant impairments in ROS. The administration of 2’-hydroxychalcones (100mg and 150mg) mitigated this oxidative damage. Results: These results underscore the potential of chalcones as alternative therapeutic agents for CIPN, offering a foundation for further preclinical and clinical investigations. Conclusion: By bridging the gap between natural product pharmacology and neuropathy research, the study provides insights into novel strategies for managing CIPN.
Chemotherapy-induced peripheral neuropathy (CIPN)
Superoxide Dismutase (SOD) Reduced Glutathione (GSH),
Unveiling the Antidiabetic and Anti-Inflammatory Potential of Piliostigma thonningii Ethanol Leaf Extract as a Dual PPAR-γ and COX-2 Modulator via In Vitro and Molecular Docking Insights
Purpose: Diabetes mellitus remains a global health challenge, prompting the search for safer, more effective therapies. Piliostigma thonningii, a medicinal plant used in traditional medicine, is known for its antidiabetic and anti-inflammatory properties. This study evaluates the ethanol leaf extract of P. thonningii for these activities Methods: Ethanol leaf extract was analyzed via GC-MS and subjected to in vitro assays. Identified phytochemicals were further assessed using molecular docking. Results: The extract demonstrated a dose-dependent inhibition of α-amylase and α-glucosidase activities, with IC₅₀ values of 68.50 ± 1.84 and 483.70 ± 2.69 µg/ml, respectively, suggesting its potential to regulate postprandial hyperglycemia. Additionally, the extract enhanced glucose uptake and adsorption, reinforcing its hypoglycemic activity. The anti-inflammatory assays revealed significant inhibition of protein denaturation (IC₅₀ = 61.50 ± 1.79 µg/ml), proteinase activity (IC₅₀ = 63.30 ± 1.80 µg/ml), membrane stabilization (IC₅₀ = 58.37 ± 1.77 µg/ml), and heat-induced hemolysis (IC₅₀ = 83.97 ± 1.92 µg/ml), indicating its potential as an anti-inflammatory agent. Molecular docking analyses further validated the pharmacological potential of P. thonningii, revealing strong binding affinities of its phytochemicals to peroxisome proliferator-activated receptor gamma (PPAR-γ) and cyclooxygenase-2 (COX-2). Notably, anthracene, 1,2,3,4-tetrahydro-9,10-dimethyl- exhibited the highest binding affinity for PPAR-γ (-7.24 kcal/mol), surpassing pioglitazone (-5.64 kcal/mol), while tetratriacontyl trifluoroacetate showed a strong interaction with COX-2 (-6.40 kcal/mol), comparable to celecoxib (-7.13 kcal/mol). Conclusion: P. thonningii exhibits dual antidiabetic and anti-inflammatory potential, supporting its traditional use. Further in vivo and clinical studies are warranted to confirm its therapeutic value.
In vivo analysis of Neuromodulatory and Biochemical Effects of Lacatomtom Drinks on Wistar Rat Brain
Purpose: This study investigated the neuromodulatory and biochemical effects of Lacatomtom, a mixture of a soft drink and candy, on Wistar rat brains. Methods: This research examined the activities of ATPases (Mg2+, Na+/K+, Ca2+/Mg2+), acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and levels of dopamine, serotonin, tumor necrosis factor-alpha (TNF-α), sodium ions (Na+), glutathione peroxidase (GPx), bicarbonate (HCO3-), and creatinine kinase (CK). Wistar rats were divided into four groups: control (water), Lacatomtom (LTT), Lacasera (LC) alone, and Tomtom candy dissolved in water (TTW). Results: Results revealed significant increases in AChE and BChE activities, particularly in the LTT group, suggesting potential cholinergic dysfunction. Elevated ATPase activity was observed in the LTT and LC groups, indicating altered energy metabolism. Furthermore, increased levels of nitrite and protein suggested oxidative stress. Conclusion: These findings indicate that LTT induces significant neurochemical alterations, potentially leading to neurotoxicity.
Antioxidant and Anti-inflammatory Studies of Aqueous and Methanol Extracts of Pterocarpus erinaceus poir Leaves
Purpose: Increasing ethno-medicinal adoption of plant based management option for chronic diseases is well documented. Phytochemistry studies have shown presence of metabolites in plants with diverse pharmacological actions. This study evaluates antioxidant and anti-inflammatory potentials in Pterocarpus erinaceus leaf extracts. Method: The 2, 2-diphenyl-1-picryl-hydrazyl (DPPH) radical reduction and ferric-reducing antioxidant power (FRAP) were assayed for antioxidant evaluation. Human red blood cell membrane stabilization and the egg albumin (protein) denaturation inhibition were determined for the anti-inflammatory. Results: Significant concentrations of phenols, flavonoids, tannins, saponins, vitamins A, C and E were detected in the extract. The extract demonstrated a high total antioxidant capacity (TAC), DPPH radical was inhibited, IC50 0.70 μg/ ml (methanol) and 3.65 μg/ ml (aqueous), ferric pyridyltriazine (Fe3+-TPTZ) complex was also reduced to the ferrous ion (Fe2+) complex. Additionally, both extract inhibited protein denaturation and erythrocyte haemolysis. Aqueous extract however, produced more potency on protein, possessing a higher % protection with a lower IC50 of 0.24 μg/ ml, not significantly different from aspirin. Conclusion: Aqueous and methanol leaf extracts of P. erinaceus in this study demonstrated antioxidant and anti-inflammatory potentials. Vitamins and polyphenols in the extracts might have enhance the antioxidant and anti-inflammatory activities, therefore possible therapeutic effect of the plant could include antioxidant and anti-inflammation mechanisms.
Alleviation of clastogenic, hematotoxic, and nephrotoxic effects of Potassium dichromate by hydro-ethanol extract of Moringa oleifera in rats
Purpose: Chromium (VI) is a human carcinogen associated with tissue toxicity, affecting blood and kidneys. The adverse effects of current intervention regimens necessitate investigation into potential antidotes from medicinal flora such as Moringa oleifera Lam (M. oleifera), which exhibits notable pharmacological attributes. This study assesses the impact of the hydro-ethanol extract of M. oleifera (HEMO) on potassium dichromate [K2Cr2O7]-induced clastogenicity, hematotoxicity, and nephrotoxicity. Methods: Thirty male Wistar rats were divided equally into six groups. They were treated with 12 mg/kg K2Cr2O7, 3.5 mg/kg, and 7 mg/kg HEMO either alone or in combination. The K2Cr2O7 was given intraperitoneally once weekly, while HEMO was given orally daily for 5 weeks. Control rats had distilled water daily for 5 weeks by gavage.The levels of bone marrow micronucleated polychromatic erythrocytes (mPCEs), packed cell volume (PCV), white blood cells (WBC), neutrophils, lymphocytes, relative kidney weight (RKW), blood urea and creatinine were assessed following the 5-week treatment period and sacrifice. Renal malondialdehyde (MDA), superoxide dismutase (SOD), and glutathione-S-transferase (GST) were also determined. Additionally, renal histopathology and HPLC determination of polyphenols and flavonoids in HEMO were conducted. Results: The HEMO and K2Cr2O7 combination reduced mPCES, WBC, KWT, RWT, urea, creatinine, and renal MDA compared to the K2Cr2O7-treated group. However, HEMO augmented PCV, SOD, and GST in contrast to K2Cr2O7 and improved renal histology. The HEMO is rich in flavonoids including kaempferol, ferrulic acid, and amentoflavone that could protect against chromium(VI)-induced toxicities. Conclusion: The HEMO has the potential for use in the management and treatment of chromium(VI) toxicity.
Micronucleated polychromatic erythrocytes
Larvicidal potential of Khaya senegalensis seed oil against Dermestes maculatus Degeer
Purpose: Fishes are highly vulnerable to insect pest attacks during processing and storage resulting in physical, financial, and nutritional losses from these infestations. The prevailing tropical climate's humidity encourages the infestation of dermestids. Hence, post-harvest losses due to Dermestes maculatus infestation pose a significant challenge in the preservation of smoked-dried fish, necessitating alternative pest control strategies. The study focused on the examination of the insecticidal potential of Khaya senegalensis seed oil against the larvae of the hide beetle, Dermestes maculatus on smoked-dried African mud catfish, Clarias gariepinus. Methods: Oil was extracted from pulverized seeds of Khaya senegalensis using n-hexane by Soxhlet method. The Refractive index, Specific gravity, Acid, Iodine, Peroxide, and Saponification values of the oil were determined by Standard Methods. Parameters assessed were repellency and larval mortality at 24, 48, 72, and 96 hour exposure time. The doses of the seed oil administered were 0.003mLg-1, 0.009mLg-1, 0.027mLg-1, 0.081mLg-1, and 0.243mLg-1. Thirty late (5th) instar larvae of D. maculatus were exposed to each of the treated fish in triplicate including a control devoid of oil treatment. Results: The repellent activity of the oil was dose-dependent, with significant repellency observed at concentrations of 0.081 mLg⁻¹ and 0.243 mLg⁻¹. Mortality rates of D. maculatus larvae increased with oil concentration and exposure duration, with up to 85% mortality recorded at the highest dose after 96 hours (p<0.05). Conclusion: This findings suggest that K. senegalensis seed oil has strong potential as a sustainable, plant-based insecticide for protecting stored fish products. Further research should focus on isolating active compounds and assessing field applications.
GC-MS Fingerprint of Mitracarpus hirtus and Commiphora africana: Medicinal plants Used in the Treatment of Skin and Wound Infections in Bauchi Town
Purpose: Mitracarpus hirtus and Commiphora africana are two medicinal plants traditionally utilized in Bauchi town, Nigeria, for the treatment of skin and wound infections. However, the bioactive chemicals responsible for these effects have not been fully identified. On this basis, the current work employed GC-MS analysis in conjunction with computational prediction studies to investigate the presence of compounds in the aqueous extracts of these plants leaves, aiming to identify those with wound healing properties. Methods: The Plants leaves were air-dried, pulverized into powdered form and extracted with aqueous. The extracts obtained were subjected to GC-MS analysis where the compounds identified were search both in the literature and in-silico for their wound healing characteristic. In-silico prediction for compounds' physiochemical properties, adsorption, distribution, metabolism, excretion, toxicity as well as drug-likeness properties and bioactive characteristics, including wound healing, anti-inflammatory, antioxidant, antibacterial, growth stimulation, and so on, were predicted using an online software such as activity spectra for biologically active substances (PASS) etc. Results: The study’s findings revealed various capacities of phytochemicals in Mitracarpus hirtus and Commiphora africana extracts for wound healing. Compounds in the extracts of C. africana were detected at retention times ranging from 2.6 to 16. 5 minutes. Pyranone has the largest percentage yield at 2.06%, whereas 4-acetoxy-3-methoxystyrene has a lower yield of 0.12%. In M. hirtus extracts, components were detected after a retention duration of 5-22 minutes, with Phenol, 2,5-bis(1,1-dimethylethyl)-, having a higher presence at 2.74%. Among the compounds identified and predicted to be responsible for the wound healing properties of the plants extracts were resorcinol, undecanoic acid, and tetradecanoic acid. Quantitative Estimate of Drug-likeness (QED) for the compounds indicates that the values fall within a desirable range, with 2,5-bis(1,1-Dimethylethyl)phenol exhibiting the most favorable QED at a value of 0.68. Conclusion: Mitracarpus hirtus and Commiphora africana showed to possess compounds with good qualities for wound healing hence confirms their used in treating skin and wounds.
Extracts of Telfeiria occidentalis as an Alternative Treatment for Trypanosoma brucei Infection in Mice
Purpose: Historically, plants have been used to cure parasite illnesses, such as infections caused by Trypanosoma brucei. Using in vivo techniques, this study evaluated the antitrypanosomal properties of methanolic extracts of Telfairia occidentalis (Family Cucurbitaceae). Method: Mice were infected with 0.1 ml of blood containing roughly 1 × 10³ trypanosomes for the in vivo study. Blood samples were drawn, smeared, stained with 10% Giemsa dye, and seen under a microscope over the course of seven days. Extracts were added, incubated for 10 to 15 minutes, and then observed at concentrations of 0.1, 0.01, and 0.001 mg/ml. Before, during, and after a seven-day oral treatment, haematological parameters were tracked. With no discernible negative effects (P > 0.05). Results: The methanolic extract of Telfairia occidentalis (TOM) shows remarkable efficiency in maintaining and re-establishing normal physiological functioning in the infected mice. Fifteen bioactive components were found in the methanolic extract of Telfairia occidentalis leaves using gas chromatography-mass spectrometry (GC-MS) analysis. Among the other bioactive compounds discovered, oleic acid accounted for the largest percentage at 42.26 per cent, followed by propanoic acid (12.98 per cent) and docosanoic acid (1.18 per cent). Because of its efficacy and few side effects. Conclusion: The study emphasises Telfairia occidentalis methanolic extract as a possible treatment for trypanosomiasis. These results provide credence to its possible use in the treatment of this parasite illness. To guarantee safety and therapeutic success, it is crucial to optimise extraction techniques and dosages, as evidenced by the toxicity and reduced efficacy seen in the moderate dosage concentration.
Evaluation of Associated Changes on the Uterus and Fallopian Tube Histology in Response to Graded Doses of Syzygium aromaticum (Clove) in Wistar Rats
Purpose: Syzygium aromaticum (Clove) is used as a preservative, as well as in the preparation of various spicy foods. This study aimed to evaluate the effect of graded doses of cloves on the uterus and fallopian tube histology using Wistar rats as experimental animal model. Method: Twenty (20) Wistar rats after two weeks of acclimatization were assigned into four groups (I, II, III and IV) of five animals each. Group I served as the control group and received normal saline, while Groups II, III, and IV received 2 mL, 4 mL, and 6 mL of clove extract once daily for 30 days. The body weights of the rats were monitored over the treatment period. At the end of the experimental period, the animals were fasted for 12 hours and thereafter were sacrificed, and their uterus and fallopian tubes were harvested and used for histological examination. Results: Syzygium aromaticum extract exhibited dose-dependent effect on the histoarchitecture of the female reproductive tissues, particularly, the uterus and fallopian tubes in Wistar rats. Low and moderate doses of the extract appeared to maintain normal tissue architecture, while high doses resulted in mild degenerative changes. Conclusion: These findings suggest that a high dose of Syzygium aromaticum has the potential to cause mild structural changes in the histoarchitecture of the female reproductive tissues, particularly, the uterus and fallopian tube.
Phytochemical Evaluation and Herbal Formulation of the Stem bark of Anogeissus leiocarpus (DC) Guill. & Perr. (Combretaceae)
Purpose: Anogeissus leiocarpus (Combretaceae) is a medicinal plant traditionally used by the Hausa tribe of Northern Nigeria for managing respiratory tract infections. Its antibacterial and antifungal properties have gained attention, especially during the COVID-19 pandemic. This study focuses on the phytochemical screening and formulation of tea from the powdered stem bark of A. leiocarpus. The study aimed to evaluate the phytochemical composition of the aqueous stem bark extract, formulate loose and bagged teas, and assess their quality and safety. Method: Phytochemical screening was conducted to identify bioactive compounds. Loose and bagged teas were formulated using standard procedures. Quality assessment included uniformity of mass and optimization of extraction. Acute toxicity was evaluated in Wistar rats using OECD guideline 425. Results: Phytochemical analysis revealed the presence of alkaloids, saponins, flavonoids, tannins, steroids, and triterpenes. Tannins had the highest concentration (0.117 mg/ml), while saponins had the lowest (0.030 mg/ml). The formulated tea bags passed the uniformity of mass test, with optimal extraction achieved by infusing a tea bag in 200 mL of boiled water for 10 minutes. The acute toxicity study indicated a wide margin of safety, with an LD50 greater than 5000 mg/kg body weight. Conclusion: The aqueous stem bark extract of A. leiocarpus is rich in phytochemicals and can be safely formulated into loose and bagged teas. The findings support its traditional use and potential for further development as a therapeutic agent.
Phytochemical analysis and antibacterial activity of acetone extract of Terminalia catappa Linn. leaves
Purpose: Traditional medicine has used the leaves of Terminalia catappa for various health benefits, with established antibacterial, antidiabetic, anti-inflammatory, antioxidant, antiviral, and hepatoprotective characteristics. This study aims to perform a phytochemical analysis and antibacterial assay of the acetone extract from T. catappa leaves. Methods: The dried leaves were subjected to extraction using 50 % acetone, followed by preliminary phytochemical screening, Gas chromatography-mass spectroscopy (GC-MS) analysis, and antibacterial testing of the extract. Results: Preliminary phytochemical screening identified the presence of carbohydrates, flavonoids, saponins, alkaloids, glycosides, tannins, phenols, terpenoids, and steroids/triterpenoids. GC-MS analysis showed the presence of epiglobulol and thirteen additional phytochemicals, which have been reported to possess antibacterial activity or potential, with epiglobulol exhibiting the highest concentration among all the identified phytochemicals. The diameters of the inhibition zones ranged from 0 to 15 mm for Staphylococcus aureus, 0 to 12 mm for Streptococcus pneumonia, 0 to 12 mm for Escherichia coli, and 0 to 8 mm for Pseudomonas spp, with greater extract concentrations leading to larger inhibition zones—though these were smaller than the inhibition zone diameters observed for gentamicin, which varied between 24.5 and 27 mm across the four tested organisms. Conclusion: The acetone extract of T. catappa leaves underwent phytochemical analysis, revealing numerous constituents known to exhibit antibacterial properties.
In Silico Investigation of the Anti-Inflammatory Activity of Some Diarylheptanoids
Purpose: The search for potentially non-toxic and efficacious anti-inflammatory agents has been of keen interest among researchers due to the side effects of existing anti-inflammatory agents, making their long-term use unsuitable. This study aimed to explore the mechanisms of the anti-inflammatory activity of some diarylheptanoids. Methods: We performed molecular docking and MM/GBSA binding free energy calculations to assess the binding affinity of selected diarylheptanoids against nuclear factor-kB (PDB ID: 1NFK) and COX-2 (PDB ID: 3LN1). The stability of the lead complexes was evaluated using molecular dynamics simulations for 200ns. The SwissADME web tool and HyperChem 8.0 were used to predict the physicochemical and pharmacokinetic properties. Results: The results revealed that platyphylloside and hirsutenone were potential NF-kB inhibitors with docking scores of -4.76 and -4.48 Kcal/mol; and binding free energies of -15.84 and -31.17 Kcal/mol. Furthermore, hirsutenone and yakuchinone were identified as potential inhibitors of cyclooxygenase 2 enzyme with docking scores of -11.81 and -10.63 Kcal/mol; and binding free energies of -54.72 and -45.95 Kcal/mol. The types of interactions between the diarylheptanoids’ atoms and amino acid residues in the target protein active site were the same as those of the reference inhibitors; dexamethasone for NF-kB, and Celecoxib for COX-2, thus further confirming their potential as NF-kB and COX-2 inhibitors. Conclusion: Inhibition of NF-kB remains a promising strategy in the treatment of inflammation, and hirsutenone has been identified as a potentially safe and effective anti-inflammatory agent for treating chronic inflammatory conditions, whose anti-inflammatory properties may include both NF-kB and cyclooxygenase 2 inhibition.
Selected Preclinical Studies on Picralima nitida Stem Bark Extract
Purpose: Traditional medicine has utilized Picralima nitida (Apocynaceae) to treat a variety of illnesses, including microbial and pain-induced infections, diabetes, inflammation, and malaria. Methods: The phytochemical screening, haematological, and histological studies were carried out using already established methods. Results: Alkaloids, saponins, tannins, proteins, carbohydrates flavonoids, reducing sugars, and terpenoids detected in the extract. The histology of the organ treated by the stem bark extract showed no form of organ damage and toxic damage when treated with the plant extract and when compared to the control. Haematological studies of the effects of the stem bark of P. nitida extract on the red blood cell and it’s components; hamacrite (HCT), haemoglobin (HGB) and red blood cell (RBC) at 200, 400 and 800 mg/kg showed slight increase in RBC showing that P. nitida stem bark extract can increase the ability of the blood to transport oxygen and hence, could be effective in treating certain diseases like anaemia. All the mice that received the plant extract experienced an increase in WBC counts. White blood cells are involved in battling illness and the extracts may stimulate their production. The result of the white blood cell demonstrates that the P. nitida extract significantly affected the white blood cells (WBC), lymphocyte (LYM), and granulocyte (GR) counts. Conclusion: The study revealed that Picralima nitida could serve as an intoxicating source of haematinic agent and as such; further studies should be carried out on the isolation of the active agents responsible for this potency
Chemical Profiling, In-vitro and Computational analysis of the Ethanol Extract of Mangifera indica Bark in the search for new antidiabetic agents
Purpose: Diabetes mellitus is a global health challenge requiring novel therapeutic agents. The inhibition of α-amylase and α-glucosidase enzymes is a key strategy for controlling postprandial hyperglycemia. While synthetic inhibitors exist, their adverse effects necessitate safer alternatives. This study evaluates the chemical composition and antidiabetic potential of Mangifera indica bark extract through in vitro and computational analyses. Methods: High-Performance Liquid Chromatography (HPLC) and Gas Chromatography-Mass Spectrometry (GC-MS) were used to identify phytochemicals in the extract. The α-amylase and α-glucosidase inhibitory activities were assessed using enzyme inhibition assays, with IC50 values determined. Molecular docking studies were conducted using AutoDock Vina to evaluate the binding affinity of key phytoconstituents, and pharmacokinetic properties were analyzed using SwissADME. Results: HPLC and GC-MS identified gallic acid (0.58 g/g) and Mangiferin (0.03 g/g) as major bioactive compounds. The extract exhibited strong α-amylase inhibition (IC50 = 16.11 µg/mL) and α-glucosidase inhibition (IC50 = 6.96 µg/mL), outperforming Acarbose. Molecular docking revealed Mangiferin as the primary bioactive compound, with binding affinities of -9.1 kcal/mol and -7.8 kcal/mol for α-glucosidase and α-amylase, respectively. ADME analysis indicated favorable pharmacokinetics and drug-likeness properties. Conclusion: Mangifera indica bark extract demonstrated potent antidiabetic activity through enzyme inhibition, with Mangiferin identified as a promising lead compound. These findings support its potential as a natural therapeutic agent for diabetes management, warranting further pharmacological and clinical investigations.
Molecular Docking, ADME and SAR Analysis of 383 Phytochemicals in the Quest for Lead Antidiabetic Inhibitors Targeting α-Amylase and α-Glucosidase Enzymes
Purpose: Diabetes mellitus remains a global health challenge, necessitating the exploration of safe and effective therapeutic agents. The inhibition of α-amylase and α-glucosidase enzymes plays a crucial role in controlling postprandial hyperglycemia. While synthetic inhibitors exist, they often cause gastrointestinal side effects, prompting the search for novel, naturally derived inhibitors. This study evaluates the molecular interactions of 383 phytochemicals, focusing on alkaloids, terpenes, and flavonoids, for their potential as lead antidiabetic compounds. Methods: Molecular docking studies were performed using AutoDock Vina to assess the binding affinity of selected phytochemicals against human pancreatic α-amylase (PDB ID: 5EMY) and α-glucosidase (PDB ID: 2QMJ). The physicochemical and pharmacokinetic properties of the top-performing compounds were analyzed using SwissADME, following Lipinski’s Rule of Five and Verber’s rules. Structure-activity relationship (SAR) analysis was conducted to elucidate key functional groups responsible for enzyme inhibition. Results: Flavonoids exhibited superior inhibitory potential, with binding affinities outperforming the standard inhibitor Acarbose. The most potent compounds, Amentoflavone (-9.5 kcal/mol), Hesperidin (-9.5 kcal/mol), Eriocitrin (-9.5 kcal/mol), and Diosmin (-9.4 kcal/mol), showed strong interactions with key amino acid residues. SAR analysis highlighted the significance of glycosylation and flavone / flavanol moieties in enhancing binding affinity. ADME analysis revealed favorable pharmacokinetic properties, with Amentoflavone demonstrating the highest synthetic accessibility and drug-likeness. Conclusion: This study identifies flavonoids as promising dual inhibitors of α-amylase and α-glucosidase, with Amentoflavone emerging as a lead candidate for further development as a novel antidiabetic agent, contributing to the search for safer alternatives to conventional therapies.
The Use of Intensive Therapeutic Lifestyle Management of Metabolic Syndrome: A Case Study
Purpose: Metabolic syndrome (MetS) is a major cause of morbidity and mortality. We present a case of metabolic syndrome in a 55 year old driver that was managed with intensive therapeutic lifestyle modification. Methods: A 55-year-old driver with obesity who was not a known hypertensive or diabetic presented to our facility with a two weeks history of weakness and dizziness. He was diagnosed with metabolic syndrome (hypertension, diabetes and dyslipidaemia). Patient had three months of intensive lifestyle modification intervention consisting of low calorie, high fibre diet from locally sourced natural food, salt reduction, brisk walking daily from an initial 20minutes per day to 40 minutes per day for a minimum of six days a week, stopping alcohol intake, together with strong family support, mostly from his wife. He was also placed on medications for his hypertension, diabetes and dyslipidaemia. Results: Three months after commencement of therapy and intensive lifestyle modification, patient improved significantly loosing 10 kg body weight from class II obesity to class I, with associated reduction in waist circumference (from 1.09 to 1.02m), becoming normotensive (120/80mmHg) and fasting blood sugar significantly reduced (138 mg/dl) compared to baseline (440mg/dl). His lipid profile also improved will all the parameters within normal limits. Conclusion: Intensive Therapeutic Lifestyle Intervention led to remission in hypertension and improvement in glycaemic control and lipid panel leading to reduction in the number and doses of medications taken. It is important therefore that clinicians incorporate lifestyle medication prescription in routine clinical practice particularly for patients with chronic medical conditions.
Synergistic Antidiabetic Effects of Vernonia amygdalina Leaves and Glibenclamide on Alloxan-Induced Wistar Rats
Purpose: One chronic illness that affects millions of people worldwide is diabetes mellitus. If left untreated, it can hasten the body's degenerative processes. Vernonia amygdalina (V. amygdalina) is used as a vegetable and herb, mostly found in tropical Africa. V. amygdalina is one of the many plants with anti-diabetic properties. The study’s objective was to understand the anti-diabetic activity of V. amygdalina leave’s methanol extract and its synergistic effect with glibenclamide on alloxan-induced rats. Methods: Injection of alloxan monohydrate (160 mg/kg) intraperitoneally (i.p.) led to the induction of diabetes in the Wistar rats. The rats were grouped into five: normal (group 1) and diabetic (group 2) controls, glibenclamide at 2 mg/kg (group 3), 200 and 2 mg/kg of V. amygdalina and glibenclamide (group 4), respectively and methanol extract of V. amygdalina’s 200 mg/kg (group 5). Each treatment was orally. The consequence of V. amygdalina on blood glucose, lipid profile, oxidative stress markers, haematological, and renal function indices was determined by standard methods. Results: At p < 0.05, V. amygdalina extract significantly reduced the fasting blood glucose concentration in alloxan-induced rats relative to untreated/diabetic rats. Group 4 showed relatively lower concentrations of TCL, LDL, VLDL, and TAG compared to group 5. Higher levels of reduced glutathione and catalase was observed in group 4 relative to group 1 and group 5. Equally, a comparatively higher level of malondialdehyde were observed in group 5 than in group 4. In the haematological profile, the extract-treated groups exhibited relative elevation in RBC count, PCV, and Hb concentration compared to group 2. Conclusion: The most promising treatment group is group 4 rats treated with extract and glibenclamide. The results demonstrated that sulphonylurea medications like glibenclamide can increase the potential anti-diabetic impact of V. amygdalina leaves.
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Fumarate ameliorated doxorubicin-induced nephrotoxicity: The role of pro-inflammatory cytokines and endothelial nitric oxide synthase signaling pathway
Purpose: Nephrotoxicity is a deleterious effect of doxorubicin (dox). This study investigated the renoprotective property of the tricarboxylic acid cycle metabolite, fumarate, in dox-induced nephrotoxicity. Methods: Male Wistar rats were randomly divided into four groups containing eight animals each; I: distilled water (10 ml/kg, po), II: dox (10 mg/kg stat. ip), III: dox (10 mg/kg, ip) + fumarate (50 mg/kg, po) and IV: dox (10 mg/kg, ip) + fumarate (100 mg/kg, po). The animals were treated for 10 days and euthanised on the last day. The kidneys were excised and immediately frozen for molecular analysis. A kidney section was fixed in formalin + saline solution for the histological assay. Results: Fumarate at 50 mg/kg caused a 23. 2 %, p<0.01 reduction in kidney injury molecule (KIM) expression in dox-treated rats. There was a reduction in the expression of interleukin (IL)-1β expression in nephrotoxic rats at 100 mg/kg of fumarate, (32.4±0.6 vs 28.5±0.0, p<0.05). Similarly, IL-6 expression was decreased in a dose-dependent manner in dox-treated rats. The initial fall in superoxide dismutase (SOD) activity at 50 mg/kg of fumarate was reversed at 100 mg/kg (27.7±0.9 vs 28.6±0.4, p>0.05) in rats treated with dox. Endothelial nitric oxide synthase (eNOS) expression was significantly reduced in fumarate-treated dox rats at 50 mg/kg only, (27.1±0.7 vs 23.2±0.7, p<0.05). Histological sectioning of the kidney revealed distortions in the glomerulus of dox-treated rats and fumarate reversed these changes. Conclusion: Data from this study show that fumarate ameliorated dox-induced nephrotoxicity by reducing eNOS and cytokine signaling.