Journal of Phytomedicine and Therapeutics

Pharmacognostic standardisation and antioxidant activity of Cassia sieberiana DC. (Fabaceae)

Mubo Adeola Sonibare — 2024-12-19

Secondary metabolites of medicinal plants can be used as dietary antioxidants, acting as free radical scavengers, radical chain reaction inhibitors, metal chelators, oxidative enzyme inhibitors and antioxidant enzyme cofactors. However, the major setback in promoting the use of medicinal plants is the lack of standardisation. This study aimed to set pharmacognostic standards and establish the antioxidant activity of Cassia sieberiana via in vitro method. Cassia sieberiana leaves methanol extract was partitioned into n-hexane, DCM, and ethyl acetate fractions. The macroscopic, microscopic and chemo-microscopic characters were assessed while antioxidant potential of the crude extract and partitioned fractions was assessed using DPPH radical scavenging assay. Total phenolic and total flavonoid contents were evaluated using gallic acid and quercetin as standards. The transverse section showed presence of bundle sheath and the parenchyma cells. The adaxial and abaxial surfaces showed straight polygonal epidermal cells and presence of palisade cells. Also, the adaxial surface showed the presence of tector trichomes while the abaxial surface showed presence of glandular trichomes. The ethyl acetate fraction had the highest antioxidant activity (IC₅₀ = 71.42 ± 0.19 μg/mL), the highest total flavonoid content (TFC) and total phenolic content (TPC) with 203.19 ± 0.03 mgQE/g and 25.10 ± 0.61 mg GAE/g, respectively. Standards have been set in this study for the identification and authentication of Cassia sieberiana, and the in vivo antioxidant activity of the plant supported the traditional use of the plant for managing different ailments, which may enhance the production of reactive oxygen in the body system.

Modulation of MSH2 gene expression and DNA global methylation in diethyl-nitrosamine induced hepatic fibrosis mouse model by cisplatin- anthocyanins combination

Rasha AbdelMawla Ghazala — 2024-12-19

Novel therapeutic approaches targeting the molecular pathways of hepatocellular carcinoma (HCC) development are highly demanded. We aimed at studying the effect of cisplatin alone and combined with cranberry extract on global DNA methylation and the MSH2 gene expression in diethyl-nitrosamine (DEN)-induced hepatic fibrosis model, as a landmark in HCC development pathway in mice. Forty male albino mice were divided into 2 groups: Group I (n=10): control, Group II (n=30): mice were injected intraperitoneal with DEN and sub-classified into 3 equal groups; IIa: untreated, IIb: intraperitoneal cisplatin, IIc: intraperitoneal cisplatin + oral cranberry-derived anthocyanin. Histopathological examination of liver, assessment of global DNA methylation and MSH2 gene expression were done. MSH2 gene expression was significantly decreased in DEN-group as compared to the control group, but significantly increased by cisplatin alone and furthermore when anthocyanin was added (p<0.001). Global DNA methylation significantly increased in DEN-group, significant decrease in cisplatin-group and further decrease when anthocyanin was added (p<0.001). A significant negative correlation was observed between global DNA methylation and MSH2 gene expression among all the studied groups (p<0.001). Histopathological examination showed improvement of liver fibrosis when anthocyanin was added to cisplatin. Improvement of histopathological findings of DEN-induced hepatic fibrosis by cranberry-derived anthocyanins was associated with global DNA hypomethylation and increased MSH2 expression. Further studies are warranted to confirm the applicability of adding anthocyanins to liver fibrosis and HCC treatment regimen.

Ethnobotanical study of medicinal plants used by pregnant women in the Beni Mellal-Khenifra region, central Morocco

Safae Abboud — 2024-12-19

Despite advances in modern medicine, limitations persist. In response, scientific research is revisiting the benefits of natural products, particularly homeotherapy. Limited healthcare access in developing countries is another factor driving the population towards traditional medicine. Herbal medicine is viewed as a viable alternative, especially among pregnant women, despite limited safety data. This study aims to document the use of medicinal plants by pregnant and postpartum women in Beni Mellal-Khenifra region and identify associated factors. A cross-sectional survey was conducted with 400 postpartum women in the maternity ward of the regional hospital of Beni Mellal. Most women (63.75%) reported using medicinal plants during pregnancy, labor, and after dilevery. Significant correlations were found between medicinal plants usage and family structure, residence, and education level (p<0.05). The study identified 20 plant species used for various health issues, with Lepidium sativum, Peganum harmala, and Trigonella foenum-graecum being the most common. Medicinal plants were used for dietary, cosmetic, and therapeutic purposes, with gastrointestinal disorders, urinary tract infections, and anemia being the most frequently treated conditions. Adverse effects were reported by 5.88% of users. Family and friends constituted the primary source of information (34.73%). Pregnant women in the Beni Mellal-Khenifra region widely utilize herbal medicine for various purposes, despite the potential risks associated with certain remedies. There is a pressing need for enhanced education and awareness regarding the safe use of herbal medicine during pregnancy.

The potential effect of irisin in endotoxemia induced cardiac injury in mouse model: role of AMPK

Alaa Kadhum Mosa — 2024-12-19

Polymicrobial sepsis is a life-threatening situation characterized by multiorgan dysfunction resulting from the body's abnormal response to microbial invasion. The assessment of irisin cardio protective potential against experimentally sepsis-caused endotoxic cardiac damage in mice was the aim of research. 24 Mice were enrolled in separated four groups (n = 6): Sham group, CLP group, ddH2O group, Irisin-treated group 10μg/kg IP, 1hr before CLP. 24 hr later, all mice were sacrificed and a cardiac sample was taken for measurement of TNF-α, MPO, caspase-11, F2 – isoprostane and serum troponin by ELISA and gene expression of AMPK by qpcr and histopathological study. Results: irisin treated group showed significant changes as compared with CLP group regarding TNF-α, MPO, CASPASE-11, F2 – ISOPROSTANE and (Ctn-I) as well as affect tissue mRNA expression of AMPK gene (p<0.05). We conclude that Irisin has cardio protective effects attributable to its anti-inflammatory and anti-oxidative action. Also, Irisin showed a cardio-protective effect as they affect tissue mRNA expression of AMPK gene.

Performance evaluation of functionalized linear peptides as potential vascular endothelial growth factor receptor inhibitors: an insilico approach

Abel K. Oyebamiji — 2024-12-19

Breast tumors have caused significant devastation in females worldwide, presenting a great challenge to researchers. In this regard, the primary goal of researchers is to design and develop efficient drug-like compounds that can act as anti-vascular endothelial growth factor receptor agents that can down-regulate cancer. It was investigated how functionalized linear peptides inhibited vascular endothelial growth factor receptors. To optimize the investigated peptides, density functional theory using the 6-31G* basis set was used. Molecular docking was done to perform molecular assessments of the peptides under study as well as the vascular endothelial growth factor receptor (PDB ID: 2vpf). ADMET screening was also done using AdMETLab to evaluate the pharmaceutical properties and the toxicity status of the peptides. The optimized investigated compounds yielded several descriptors, such as frontier molecular orbitals (highest occupied molecular orbital energy and lowest occupied molecular orbital energy), band gap, polar surface area, polarizability, lipophilicity, and many more which revealed the inhibiting potential of these compounds to act as anti-vascular endothelial growth factor receptor agent. Furthermore, the computed binding affinity showed that, in comparison to the reference medications (5-fluorouracil), the investigated compounds showed greater inhibition of the vascular endothelial growth factor receptor. Molecular dynamic simulation was used to validate the findings. The ADMET screening revealed that the studied compounds are safer and more bioavailable than the referenced drug

Detection of OMPKs 36/37 porins and other resistance determinants in extended spectrum beta-lactamases (ESBLs) -producing K. pneumoniae

Omowumi T. Akinola — 2024-12-19

The rise of β-lactamases and loss of porin by multidrug-resistant Klebsiella pneumoniae is an important global issue. This work aimed to reveal how the loss of outer membrane porin (OMP) contributes to resistance in Klebsiella pneumoniae to certain antibiotic drugs. In this study, standard microbiological techniques of phenotypic procedures were used to isolate K. pneumoniae (P10) from the hospital wastewater sample. A double disk synergy test was used for the phenotypic detection of ESBL. Whole-genome sequencing (WGS) was conducted on the Illumina platform, and the resulting raw read was de novo assembled using RAPT NCBI. The landscape of antibiotic resistance inside the genome was examined using online bioinformatics tools. The biochemical tests identified the isolate to be K. pneumoniae with 100% resistance to ceftazidime, cefepime, augmentin, and intermediate resistance to meropenem but was susceptible to gentamicin. The isolate was confirmed as an ESBL-producer by an enlarged inhibitory zone towards Augmentin-clavulanic acid. WGS results showed the isolate harbors blaTEM, and blaSHV with Ompk 36 and Ompk 37 porin loss. The K. pneumoniae (P10) isolate exhibited a multidrug-resistant profile characterized by ESBL production, additional resistance genes, and loss of OmpK36/37 porins, collectively conferring resistance to a wide range of antibiotics including carbapenem and posing significant challenges for clinical management and infection control.

Effect of lime juice extract of cashew bark on lipid biomarkers in indomethacin-induced gastric ulcerated Wistar rats

Adetoun Elizabeth Morakinyo — 2024-12-19

This study investigated the effect of lime juice extract of cashew bark (LJECB) on lipid profile in indomethacin-induced gastric ulcer in Wistar rats. Freshly pulverised Anacardium occidentale stem bark (1 kg) was soaked in freshly prepared Citrus aurantifolia fruit juice (3 L) for 48 hours inside a refrigerator (4 ^oC). The filtered solution was concentrated in vacuo using rotary evaporator to produce the crude extract labeled as LJECB. Forty-two (42) female Wistar rats (100-150 g) were randomized into seven groups (n = 6) and treated as follow. Group 1: normal control (Distilled water 1 ml/100g body weight); Group 2: 30 mg/kg indomethacin Only (ulcerated group); Group 3: 30 mg/kg indomethacin + 0.2 ml/kg Antacid; Group 4: 30 mg/kg indomethacin + 400 mg/kg LJECB; Group 5: 30 mg/kg indomethacin + 800 mg/kg LJECB. Group 6: 400 mg/kg LJECB; Group 7: 800 mg/kg LJECB. Prior to ulcer induction, the animals were fasted overnight and allowed free access to water ad libitum. Then indomethacin (30 mg/kg, 1 ml) was orally administered to the rats in Group 2 - 5. Treatment with LJECB or antacid commenced 4 hours post-induction for 14 days. After the last dose, the animals were fasted overnight and sacrificed under mild inhalation of diethyl ether. Serum samples were prepared and used for lipid biomarker analyses (total cholesterol, triglycerides, HDL-c, LDL-c, and VLDL-c). Castelli risk index-1 and 2 were calculated from an established equation to determine the cardiovascular risk of the extract. Results showed that the untreated ulcerated group had a significant reduction in total cholesterol levels compared to the normal control group. Treatment with a high dose of LJECB further caused a significant decrease in the total cholesterol levels. Also ulcerated group had a significant reduction in triglyceride levels compared to the normal control group. Treatment with 400 mg/kg dose of LJECB further lowered the triglyceride levels in ulcerated rats, however, higher dose of LJECB (800 mg/kg) increased the triglyceride levels. Untreated ulcerated rats had a significant increase in HDL compared to the normal control group. Administration of LJECB (400 mg/kg) had no significant (p<0.0001) effect on HDL levels in the ulcerated group. However, 800 mg/kg of LJECB administered to a normal control group was associated with an increase in HDL. Moreover, the LDL was significantly low across all the groups. The normal control group had a higher Castelli risk index-1 (CRI-1), while the ulcer group and LJECB-treated groups had a relatively lower CRI-1 value. The study concludes that administration of LJECB to Wistar rats was associated with a reduction in total cholesterol and LDL levels, elevated HDL levels, and low Castelli risk index, in both ulcerated and non-ulcerated rats.

Molecular docking and ADMET profiling of Carbazole-rhodanine hybrid as anticancer agent

Ehimen A. Erazua — 2024-12-19

Drug resistance and lack of specificity of currently available chemotherapeutics for cancer cells contribute to the failure of cancer chemotherapy. This highlights the pressing need to develop novel anticancer agents. This research aims to investigate the inhibiting potential of Carbazole and rhodanine derivatives against Human papillomaviruses (HPVs) and Breakpoint Cluster Region (BCR), with Abelson murine leukemia (ABL) tyrosine kinase to manage human cervical cancer and human chronic myeloid leukemia (CML), respectively. Some carbazole-rhodanine hybrids were evaluated in silico against human cervical cancer (Hela) and human CML (K562) cells. In this study, Molecular docking was used to determine binding affinity, bonding, and nonbonding interaction between the studied compounds and the target. Additionally, in-silico ADMET (adsorption, distribution, metabolism, excretion, and toxicity) screening was performed to explore the bioavailability, pharmacokinetic properties, and toxicity of the carbazole-rhodanine hybrids. The structure of the compounds was also discussed relative to their bioactivity. The molecular docking revealed that the test compounds except D, E, and L demonstrated better binding affinity, hence better inhibition efficiency towards Hela and K562 cell lines than the reference drug (etoposide). Compound G with a cyano substituent showed the highest binding affinity with the two receptors used, with a binding energy of -7.9 kcal mol^-1 against hela (6HKS) and -10.0 against K562 (5HU9). This was in accordance with the experimental result. The SAR illustrated that a strong electron-withdrawing substituent attached to the para-position of the phenyl ring increased the activity. The ADMET profiling showed that compounds E, G, and J had superior drug-likeness, pharmacokinetic, and toxicity properties. Based on the results, compound G may be a good candidate to be developed further into a therapeutic agent to treat chronic myeloid leukemia and cervical cancer.

Neuroprotective and anti-oxidant properties of Waltheria americana leaf in male Wistar rats

Idowu Olumorin Owemidu — 2024-12-19

Neurodegenerative disorders are linked with neuroinflammation in specific areas of the brain. Waltheria americana is used in folkloric medicine for the treatment of pain and inflammation. Most drugs used in managing neuroinflammation are expensive and associated with adverse effects thereby necessitating the need for safe, potent and affordable agents. This study, therefore, evaluated the neuroprotective and anti-oxidant properties of methanol extract of Waltheria americana leaf (MEWA) in laboratory rodents.

Leaves of W. americana were obtained at the College of Agriculture, Kabba, Kogi State, and authenticated at the Herbarium, Forestry Research Institute of Nigeria, Ibadan (FHI:111064). The leaves were extracted by maceration in methanol and concentrated. Neuroinflammation was induced by intra-peritoneal injection of Lipopolysaccharide (2 mg/kg) in 15 rats and were grouped (n=5) as follows: Group1 (MEWA 200 mg/kg), Group 2 (Quercetin 50 mg/kg), Group 3 received vehicle only (control 10 mL/kg) while another group (not induced) received vehicle only. The treatment was done for 30 days. Memory function was assessed using Y Maze Test (YMT). At termination, Striatum, Prefrontal cortex (PFC) and Hippocampus were sectioned. Glutathione, malondialdehyde and acetylcholinesterase were evaluated by spectrophotometry. Nissl stains were used for neuronal morphology. Data were analysed using ANOVA at α _0.05.

The MEWA (200 mg/kg) significantly increased percentage alternation. The MEWA (200 mg/kg) significantly increased glutathione level (μmol/g tissue) in PFC (67.38±7.11) and Hippocampus (105.40±4.80) compared to control PFC (39.75±8.30), Hippocampus (55.54±2.0) and significantly decreased malondialdehyde level (ηmol/g tissue), acetylcholinesterase activity (μmol/min/g tissue), in Striatum (52.69±7.95, 7.96±0.31), PFC (57.94±3.81, 23.81±0.37), Hippocampus (111.0±12.90, 68.01±0.73), compared to control Striatum (83.51±3.85, 13.21±0.78), PFC (146.30±7.71, 32.27±1.49) and Hippocampus (151.40±8.80, 73.85±1.40), respectively. The MEWA 200 mg/kg preserved neuronal morphology.

Waltheria americana leaf extract ameliorated neurodegeneration in striatum, prefrontal cortex and hippocampus by reducing levels of free radicals, acetylcholinesterase and preventing neuronal damage in laboratory rodents.

Application, benefits, and limitations of herbal garment in natural medicine administration

Daniel Ogunlakin Akingbolabo — 2024-12-19

Natural dyes are becoming increasingly common for practical finishes that encourage an eco-friendly lifestyle. Natural dyes are renewable materials safe for the environment and do not cause toxicity, cancer, or allergic reactions. Transdermal Drug Delivery offers a pain-free method for delivering medication systemically by administering a drug formulation to intact, healthy skin. Herbal clothing dyed with these herbs has anti-inflammatory, antibacterial, and antioxidant qualities that help the skin and treat dermatitis. Herbal textiles/garments have immense potential in the worldwide textile industry and may one day become a significant textile product. Using herbs and textiles to achieve health while being ecologically conscious is a fantastic way to live a healthy lifestyle. Herbal clothing is becoming increasingly fashionable all around the world. Herbal-treated textiles are one of the most effective approaches to strengthen and extend the worldwide textile market share of the batik business. Herbal clothing is also non-toxic, non-carcinogenic, biodegradable, and eco-friendly, making it an appealing option for modern, well-informed shoppers seeking therapy. Furthermore, developing bio-colorants to meet rising demand will compel entrepreneurs to enter this sector in search of bigger profits, resulting in more employment creation. However, there is a need for standardization of dosages of extract to be used in dying clothes meant for the treatment of specific disease conditions.

Experimental evaluation of effect of Drakshasava on memory and learning of Wistar rats

Jayshree Dawane — 2024-12-19

Drakshasava is a traditional herbal preparation used in Ayurveda as a general tonic to treat various ailments. It primarily consists of draksha (grapes), along with multiple other herbal ingredients. During the manufacturing of the asava the alcohol is generated. There are claims about enhancement of the effect of Drakshasava by this self-generated alcohol. Present study was undertaken with the objective to evaluate the effects of Drakshasava, an Ayurvedic fermented formulation, on memory and learning in Wistar rats. Thirty-two Wistar rats were allocated into four groups: a control group, Drakshasava-LD & HD and standard drug treated. The Drakshasava-treated group received 2 ml/kg and 4ml/kg body weight and Piracetam was given to standard drug group orally for 21 days. Behavioral assessments were conducted using the Elevated Plus Maze and Morris Water Maze (MWM) to evaluate spatial learning, memory retention, and recall abilities. Rats treated with Drakshasava showed significant improvement in the EPM, Drakshasava-treated rats demonstrated improved retention and recall, evidenced by prolonged step-through latency. In the MWM test, no significant reduction in escape latency and time spent in the target quadrant compared to the control groups, indicating no effect on spatial learning and memory. Drakshasava enhances cognitive function moderately in Wistar rats, as evidenced by improved performance in behavioral tests. These findings support the potential use of Drakshasava as an antianxiety agent but not as a cognitive enhancer.

Aluminium chloride-induced cerebral toxicity in Wistar rats: anticholinesterase and antioxidant effects of ascorbic acid

Clinton Iria Ebhodaghe — 2024-12-19

Numerous literature evidence suggests that aluminium is a toxic metal that induces direct damage to primary human neural cells, leading to genotoxic effects while promoting neurodegeneration in different regions of the brain. However, the use of exogenous antioxidants to counteract neurodegeneration has been widely reported. Ascorbic acid (AA), also known as Vitamin C, is a water-soluble vitamin reported to exert antioxidant, anti-inflammatory and anti-apoptotic effects. Accordingly, this study investigated its protective activity against aluminium chloride (AlCl₃)-induced neurotoxicity in Wistar rats. Forty-eight Wistar rats were randomly divided into six groups (n=8) and treated as follows: A (control); B (100 mg/kg bw AlCl₃); C (100 mg/Kg bw AA + 100 mg/kg bw AlCl₃); D (200 mg/Kg bw AA + 100 mg/kg bw AlCl₃); E (100 mg/Kg bw AA); F (100 mg/Kg bw AA). The administration, via an oral gavage, lasted for 28 days. Thereafter, the weights, neurobehavioral, antioxidant enzymes, lipid peroxidation, acetylcholinesterase and histological assessments were carried out. Findings showed significantly (p < 0.05) impaired weights, neurobehavioural, and antioxidant enzymes as well as elevated lipid peroxidation and acetylcholinesterase in the AlCl₃-exposed rats when compared to control. Also, the cerebral cortex of AlCl₃-exposed rats displayed severe cytoplasmic vacuolations and degenerating cells, indicating cerebral dysfunction. However, pretreatment of AlCl₃-exposed rats with AA significantly (p < 0.05) attenuated these adverse effects. Altogether, AA exerted neuroprotective effects against AlCl₃-induced cerebral toxicity, possibly through its potent antioxidant and anticholinesterase activity.

Identification of compounds with potential angiotensin converting enzyme inhibitory activity in Adansonia digitata L. fruit pulp

Liman Abubakar Alhaji — 2024-12-19

The study employed bioassay-guided fractionation to identify novel angiotensin-converting enzyme inhibitory compounds from Adansonia digitata fruit pulp, potentially responsible for its antihypertensive effects. A. digitata Fruit pulp was extracted using the solvents n-hexane, ethylacetate, methanol, and water. The percentage weight, in vitro Angiotensin Converting Enzyme (ACE) inhibitory activities and IC₅₀ values of the extracts were determined. Fractionation and phytocompound identification were performed by thin layer chromatography (TLC), column chromatography techniques, and gas chromatography-mass spectrometry (GC-MS) techniques. The yields obtained from solvent extractions using n-hexane, ethylacetate, methanol, and water were 0.14%, 1.17%, 4.30%, and 21.80%, respectively. The IC₅₀ values of Ramipril®, n-hexane, ethylacetate, methanol, and water extracts were found to be 101.40μg/ml, 116.70μg/ml, 40.53μg/ml, 47.25μg/ml, and 81.05μg/ml, in that order. The most potent ACE inhibitory activity was found in methanol extract of A. digitata Fruit (MEADF), which was chosen for bioassay-guided fractionation. From the assay, two fractions (Fraction I and III), among others, showed low IC₅₀s of 11.77±0.10 μg/ml and 11.96±0.16 μg/ml, respectively, and significant ACE inhibitory activity. The most relatively abundant compounds found in Fractions I and III) were 9, 12, octadecadienoic acid methyl ester (conjugated linoleic acid isomers), cis-Vaccenic acid, 3H-Pyrazol-3-one, 4-benzoyl-2, 4-dihydro-5-methyl-2-phenyl (a pyrazole), and Hexadecanoic acid methyl ester (aromatic acid ester).

The study reveals valuable compounds in the methanol extract of Baobab fruit pulp, which could be a promising source for developing antihypertensive foods.

In-vitro assessment of the antioxidant potentials of cyanocobalamin (vitamin B12): A comparative study with ascorbic acid

Peluola O. Ayeni — 2024-12-19

Cyanocobalamin is a form of vitamin B₁₂, which is a water-soluble vitamin that is naturally present in some foods and available as a dietary supplement as well as prescription medication to manage some illnesses. This study aimed to examine the ability of cyanocobalamin to scavenge free radicals using in vitro methods in comparison to ascorbic acid (control). Biochemical tests such as 1'1 diphenyl-2 picryl hydrazine (DPPH) radical, Ferric Reducing Antioxidant Power (FRAP), Fe²⁺ chelation, hydroxyl radical (OH^•), nitric oxide (NO^•), and inhibition of lipid peroxidation assays were carried using established procedures. The results revealed that ascorbic acid control scavenged DPPH radical (EC₅₀ = 1.514 mM) and OH^• radical (EC₅₀ = 1.562 mM) better than cyanocobalamin (EC₅₀ = 3.751 mM), (EC₅₀ = 1.942 mM) while cyanocobalamin chelated Fe²⁺ (EC₅₀ = 3.849 mM), scavenged NO^• radical (EC₅₀ = 1.812 mM) and also inhibited lipid peroxidation (EC₅₀ = 1.787 mM) better than the ascorbic acid. No significant difference was observed (p < 0.05) as both the cyanocobalamin and ascorbic acid control had similar FRAP. These findings suggest that cyanocobalamin may be utilized as a supplement to manage oxidative stress- mediated diseases.

Ethanol root extract of Uvaria chamae down-regulates Ki-67 in cadmium chloride-induced prostate pre-malignancy in Wistar rats

Donatus Gabriel Edem — 2024-12-19

Prostate malignancy is one of the most diagnosed malignancies in men worldwide and a major health problem to men in both developed and developing world. Currently, several medicinal plants have been reported to possess anti-malignant property, hence we decided to investigate this property in Uvaria chamae (UC) on Ki-67 which is a prognostic factor in prostate malignancy. Emphasis was also placed on oxidative stress markers. A total of sixty (60) Wistar rats were used for this investigation and were randomly divided into ten (10) groups of six (6) animals each. Group 1 served as control and received distilled water alone, group 2-6 were induced with pre-malignancy using 3mg/kg of cadmium chloride (Cdcl₂) for twenty-eight (28) days. Group 3-6 were subsequently treated with 150mg/kg of casodex, 2500mg/kg, 1500mg/kg and 1000mg/kg of UC root extract respectively, after the initial induction of pre-malignancy. Group 7-10 received 150mg/kg of casodex, 2500mg/kg, 1500mg/kg and 1000mg/kg Uvaria chamae root extract alone, respectively. After sacrifice, prostate tissues were removed for immunohistochemical assay of Ki-67 and oxidative stress studies. Results obtained from this study showed ki-67 up-regulation in prostate tissues induced with pre-malignancy, similarly a significant down-regulation of Ki-67 marker was observed in prostate tissues of Uvaria chamae treated groups after pre-malignancy. Ki-67 marker remained low in Uvaria chamae alone treated group. Furthermore, ethanol root extract of U. chamae down-regulated tissue level of MDA but up-regulated tissue levels of SOD, CAT and GPx in Cdcl₂-induced prostate pre-malignancy. The results established that, U. chamae root exhibit strong anti-cancer property in prostate pre-malignancy.

Mercury chloride-induced hippocampal toxicity in Wistar rats: antioxidant activity of folic acid

Adaze Bijou Enogieru — 2024-12-19

Mercury chloride (HgCl2) is a well-known neurotoxicant with detrimental effects on the central nervous system, particularly the hippocampus, a region crucial for learning and memory processes. Folic acid (FA), also known as the synthetic form of vitamin B9, plays a crucial role in various bodily functions. Accordingly, this study investigated the possible neuroprotective activity of FA against HgCl₂-induced hippocampal toxicity in Wistar rats. Forty-eight Wistar rats were assigned into six groups (n=8) with the following treatment regimen for 28 days: A (control); B (4 mg/kg bw HgCl₂); C (5 mg/Kg bw FA + 4 mg/kg bw HgCl₂); D (10 mg/kg bw FA + 4 mg/kg bw HgCl₂)_; E (5 mg/kg bw FA); F (10 mg/kg bw FA). After treatment, neurobehavioral, antioxidant enzymes, lipid peroxidation, mercury concentration, and histological assessments were done. Results showed significantly (p < 0.05) impaired cognition and antioxidants, as well as elevated lipid peroxidation and mercury concentration in the HgCl₂-treated rats when compared to the control. In addition, the hippocampus of HgCl₂-treated rats exhibited severe atrophy and vacuolated pyramidal cells and astrocytes, signifying hippocampal dysfunction. However, pretreatment of HgCl₂-treated rats with FA significantly (p < 0.05) mitigated these neurobehavioural, biochemical, and histological alterations. Taken together, the neuroprotective activity of FA against HgCl₂-induced hippocampal toxicity is mediated, possibly through its antioxidant and metal-chelation effects.

Gas chromatography-mass spectrometry analysis, druggability and in-silico dermatopharmacokinetics screening of Mitracarpus scaber extract.

Friday Attah — 2024-12-19

Medicinal plants are an important source of natural compounds used in the development of drugs to treat infectious diseases. The plant Mitracarpus scaber has traditionally been used to treat various ailments, including skin disorders. In this study, GC-MS (gas chromatography-mass spectrometry) analysis was used to identify eighteen bioactive components in the methanolic extract of Mitracarpus scaber whole plants. To assess the druggability and skin pharmacokinetics of these phytocompounds, in silico screening was performed using online programs such as Swiss ADME, pkCSM, ADMETLab 2.0, and StopTox. The druggability assessment of the identified compounds met the requirements of Lipinski's Rule of Five, which is a set of standards used to estimate the likelihood of good oral drug absorption. The pharmacokinetic factors such as skin sensitization, acute inhalation toxicity, acute dermal toxicity, skin irritation and corrosion, skin permeability, Ames toxicity, carcinogenicity, eye corrosion, eye irritation, and oral acute toxicity were screened. Results indicated that the plant may be safe for therapeutic use since they do not exhibit acute oral toxicity and Ames toxicity and also had less acute dermal toxicity and acute inhalation toxicity. However, direct eye contact with the compounds should be avoided due to its potential to cause eye corrosion and eye irritation. Therefore, this in-silico screening method should be encouraged for the preclinical study of medicinal plants to avoid costly mistakes in the course of drug discovery and development

Antioxidant activity of Brachiaria sabia and Brachiaria marandu and molecular docking of constituents targeting insulin-like growth factor 1 receptor (IGF-1R) for cancer treatment

Daniel Akingbolabo Ogunlakin — 2024-12-19

The methanol extracts of Brachiaria sabia, and Brachiaria marandu leaves were evaluated for its ability to scavenge free radicals, reduce ferric iron, and function as an iron chelator. The extracts were subjected to HPLC analysis. The two Brachiaria species possessed strong antioxidant activity, with B. marandu had a higher percentage (%) of phenolic content than Brachiaria gayana. In silico studies revealed that the two Brachiaria grasses tested enhanced insulin-like growth receptor factor-1 receptors (IGF-1R). Quercetin, which is consistent compound in the two grasses, had highest binding affinity to insulin-like growth factor-1 receptors with value of -40.5971. This study therefore reveals that Brachiaria sabia, and Brachiaria marandu are good antioxidant and Quercetin, a constituent of Brachiaria grasses, binds to insulin-like growth factor-1 receptors (IGF-1R) which plays an important role in cancer cell proliferation. In vivo and in vitro research are also necessary to validate this in silico result.

Bioactive compounds in methanol extract of Newbouldia laevis leaf inhibit alpha-glucosidase and enhance antioxidant status in fructose/alloxan-induced type 2 diabetic rats.

Aanuoluwa James Salemcity — 2024-12-19

Newbouldia laevis (NL) has been folklorically known to be used for managing diabetes mellitus. Its mechanism of action against this disease has not been fully proven. The study was therefore designed to investigate the effect of NL bioactive compounds on diabetic parameters in vivo and in silico. For in vivo study, twenty-five rats divided into five groups (n = 5) were given 20% fructose solution for two weeks and grouped as follows: normal control (NC) received 10ml/kg olive oil; diabetes was induced in groups 2 (Diabetic control- DC), 3, 4 and 5 using 80mg/kg alloxan, and they were administered 10ml/kg olive oil, 250mg/kg, 500mg/kg MENL, and 5mg/kg glibenclamide, respectively. Methanol extract of NL (MENL) was characterized using Gas Chromatography Mass Spectrometry (GC-MS). Molecular docking was done on bioactive compounds obtained from GC-MS analysis against α-glucosidase to unravel probable mechanism of action of the extract. Serum insulin and antioxidant were determined using ELISA and spectroscopy techniques respectively. As against DC, blood glucose level was significantly low while insulin was high in MENL treated groups. Antioxidant increased significantly in MENL treated groups compared to DC. Four hit molecules inhibited α-glucosidase more than acarbose. It could be inferred that bioactive compounds in NL may exhibit their normoglycemic effect by inhibiting α-glucosidase, improving insulin sensitivity and enhancing antioxidant status.

In vitro-in vivo correlation(IVIVC) study for ibuprofen liquisolid tablet using a convolution-based modeling approach.

J. Isaac Ajeh — 2024-12-19

This study aimed to develop an in vitro-in vivo procedure for ibuprofen liquisolid tablet and evaluate its predictability via in vivo outcome of a bioequivalence study. By varying the excipient ratio (R), we prepared different batches of ibuprofen liquisolid (LS) tablets and subjected them to pre and post compression studies to select the optimized formulation, after which we compared and investigated the predicted plasma concentration-time profiles of ibuprofen prototype drug from in vitro dissolution results using mathematical convolution approach for In vitro-in vivo correlation (IVIVC) study. Compatibility studies using Fourier transform infra-red (FTIR) and differential scanning calorimetry (DSC) returned no major interactions between the drug and excipients. All formulations demonstrated acceptable flow properties. Tablet weight variations were insignificant, while assay and friability testing were within compendial specifications. Formulation F16 was nearest to the reference brand (Nurofen tablet^® ; Reckitt Benckiser, UK) at every dissolution sampling time hence it was chosen as the optimal formula. Area Under the Curve (AUC) percentage predicted errors were similar for both the test and reference product, while their peak plasma concentration (C_max) deviates by +6.73 and -1.77 percent from the authentic reference values derived from the literature. The percentage of predicted errors achieved revealed the convolution technique as a proficient procedure for predicting plasma drug levels of ibuprofen LS.

Total phenolic content in monofloral honey varieties from Beni Mellal-Khenifra, Central Morocco: variability and determinants

Mourad Chikhaoui — 2024-12-19

Honey is valued not only for its taste and nutritional properties but also for its health benefits, primarily due to its phenolic compound content. Environmental and biological factors influences this content. This study investigates the total polyphenol content of monofloral honey varieties from the Beni Mellal-Khenifra region and its relationship with botanical origin, geographic location, color, and harvesting period. The results showed highly significant differences in total phenolic content among honey samples with varying botanical and geographical origins (p < 0.0001). The study revealed a strong correlation (r
= 0.985*, p<0.05) between total phenolic content and the location of honey collection. Honey from lower altitudes, such as citrus and anis honey, showed lower total polyphenol content levels (13.53 ± 0.004 and 19.10 ± 0.004 mg EAG/100g, respectively), while honey from higher altitudes, such as euphorbia and carob honey, exhibited higher total phenolic content levels (30.61 ± 0.009 and 28.62 ± 0.003 mg EAG/100g, respectively). Additionally, a highly significant correlation was observed between total phenolic content and honey color (r = 0.996**, p<0.01), indicating that darker honey contains higher phenolic levels. Conversely, no significant association was found between total phenolic content and harvesting period (r = 0.486, p>0.05). These results highlight the impact of environmental factors on honey’s phenolic composition and underscore the importance of considering geographic and botanical influences in honey quality assessment.

A comprehensive Colorectal Cancer Medicinal Plants and Metabolites Database: CRCMMDB

Pankaj Kumar Tripathi — 2024-12-19

Colorectal cancer (CRC) represents a significant health challenge due to the complexities of treatment, which often result in low efficacy and adverse side effects. Medicinal plants, rich in bioactive compounds, offer promising alternatives but the relevant data is scattered across various sources. Our Colorectal Cancer Medicinal Plants and Metabolites Database (CRCMMDB), consolidates this information into an accessible platform, facilitating the integration of genomic data, natural drugs, and medicinal plant metabolites that show promise in treating CRC. This resource aims to support more focused and effective research on natural therapies for CRC. The database integrates genome information, specific natural drugs for CRC, details on medicinal plants and their metabolites, along with associated pathways and activity in carcinoma, and FDA drug target genes for CRC. Employing one-to-many relationships throughout the data frame facilitates unrestricted connections. We utilized Django v4.3.2 and integrated SQLite3 for web development. The study reveals that CRCMMDB provides extensive data on genomics, CRC-specific natural drugs, medicinal plants, bioactive compounds, and FDA drug target genes. The 'natural drug' section includes curated therapeutic substances with details like PMID, drug ID, chemical structure, source plant, and mechanism of action. It also offers comprehensive coverage of CRC's stages, risk factors, preventive measures, symptoms, and related conditions. Users can explore plant-derived compounds like alkaloids and polyphenols, known to modulate oncogenic pathways like PI3K and Akt. Each plant entry is cross-referenced with NCBI, serving as a valuable resource for natural treatment research. CRCMMDB stands as a vital resource in CRC investigation, addressing the need for centralized data on natural medications. With increasing CRC prevalence globally, there's a critical demand for readily available information. CRCMMDB (http://crcmmdb.in) offers an easily navigable interface promoting the discovery of natural compounds for CRC treatment.

Safety and antioxidant potential of Ziziphus mauritiana leaf extract: an acute toxicity and DPPH scavenging study

Deepak Jha — 2024-12-19

The current study aimed to assess the toxicological profile and antioxidant potential of the ethanolic extract of Ziziphus mauritiana (Z. mauritiana) leaves, evaluating its safety and therapeutic properties. The toxicological assessment followed the Organization for Economic Cooperation and Development 423 guidelines, using female Wistar rats to evaluate acute oral toxicity. The extract was administered in doses of 5, 50, 300, and 2000 mg/kg body weight, with physiological responses and mortality observed over 14 days. Antioxidant potential was assessed through total phenolic content (TPC), total flavonoid content (TFC), and 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity (RSA) assays. TPC and TFC were measured using gallic acid and quercetin as standards, respectively. No signs of toxicity or mortality were observed across all dose levels, indicating the extract’s safety even at high doses. Antioxidant analysis revealed significant TPC and TFC values, reaching 5.24 mg gallic acid equivalent per gram (GAE/g) and 4.17 mg quercetin equivalent per gram (QE/g), respectively. The extract exhibited strong DPPH RSA, with a half-maximal inhibitory concentration (IC₅₀) value of 128.17 μg/mL, indicating potent antioxidant efficacy. The ethanolic extract of Z. mauritiana leaves demonstrated substantial antioxidant activity and an absence of acute toxicity, supporting its potential use as a natural antioxidant agent in medicinal applications. Future studies should explore its bioactive components and effects in disease models.

Mitigation of acute lung injury by semaglutide: role of inflammatory and oxidative stress pathways

Ekhlas Sabah Hassan — 2024-12-19

Endotoxic disease Increased production of pro-inflammatory cytokines during bacterial infection is caused by high endotoxin levels, the protective effect of semaglutide on endotoxemia-induced acute lung injury was investigated in this research. twenty-four adult mice of the Swiss-Albano strain, aged 8-14 weeks and weighing between 25- 40 grams, were randomly divided into four groups. The groups were as follows: control (undergoing laparotomy without cecal ligation and puncture), endotoxemia (undergoing cecal ligation and puncture), vehicle (receiving normal saline for 1 week), and treatment (receiving semaglutide at a dose of 0.06mg/kg once daily subcutaneously for 1 week prior to cecal ligation and puncture). The scarification of animals was done 24 hours following the CLP treatment, and their lung tissues were utilized for histological investigation as well as the assessment of inflammatory mediators (IL-6, TNF-α, IL-1B, and NF-KB) and oxidative markers (MDA). The levels of lung tissue, inflammatory mediators, and oxidative stress were considerably elevated (P<0.05) in both the endotoxemia and vehicle groups compared to the control group. The treatment group exhibited significantly reduced levels of inflammatory and oxidative stress mediators compared to the endotoxemia and vehicle groups, with a statistical significance of P<0.05. Microscopically, mice in the endotoxemia and vehicle groups exhibited pronounced lung tissue damage. However, this damage was significantly (P<0.05) mitigated in the group treated with semaglutide. Semaglutide had the capacity to alleviate acute lung damage in male mice exposed to endotoxemia generated by CLP through a decrease in pro-inflammatory cytokines (such as interleukin-1β, interleukin-6, TNF-alpha, and NF-KB) as well as oxidative stress marker (MDA) inside the lung tissue.

Phytosterol-enriched fraction of Morinda lucida extract inhibits testosterone-induced benign prostatic hyperplasia in rats.

James Aanuoluwa Salemcity — 2024-12-19

Benign prostatic hyperplasia (BPH) is a prevalent disorder among ageing men and could lead to prostatic carcinoma if not managed early and properly. Although orthodox drugs have been used for managing BPH, they have various side effects which necessitated the search for alternatives, especially from plant sources. Plants such as Morinda lucida have been forklorically used to manage the condition. This study was designed to investigate the effect of the phytosterol-rich extract of Morinda lucida leaf on testosterone-induced BPH in rats. Thirty rats were administered treatment for twenty-eight days as follows: Normal control (NC), BPH control, 200 mg/kg Morinda lucida Phytosterol-enriched Extract (MLPE), 400 mg/kg MLPE extract, and 1 mg/kg Finasteride group . After twenty-eight days, BPH control, 200mg/kg, 400mg/kg extract, and finasteride groups received 5mg/kg testosterone subcutaneously for another twenty-eight days along their various treatments. The rats were fasted overnight, sacrificed, and the testes were excised. Sperm parameters were carried out under light microscopy. Antioxidant assays were done using spectrophotometry. Inflammatory biomarkers were assayed via the Enzyme Linked Immunosorbent Assay method. The results showed a significant reduction in the sperm motility, count and viability status of BPH control relative to NC. However, BPH rats treated with MLPE significantly increased the parameters. Malondialdehyde concentration was high, while GSH level, GPx, and catalase activities were low in BPH rats relative to NC. Conversely, antioxidant status was normalized as a result of MLPE administration. Elevation in TNF-α and interleukin-1β was observed in BPH control compared to NC. Nevertheless, there were significant decreases in the inflammatory biomarkers in groups administered MLPE relative to BPH rats.The above results suggest that MLPE exerts its effects via free radical scavenging, antioxidant and anti-inflammatory activities . It could therefore be concluded that MLPE could serve as a promising therapeutic agent for the prevention and management of BPH.

Evaluation of acute toxicity and DPPH radical scavenging activity of Bauhinia racemosa leaf extract

Deepak Jha — 2024-12-19

Medicinal plants have long been integral to traditional medicine, and Bauhinia racemosa is recognized for its therapeutic and antioxidant potential. This study evaluates the acute toxicity and antioxidant activity of the ethanolic extract from B. racemosa leaves to assess its safety and therapeutic potential. Acute toxicity was assessed following Organization for Economic Cooperation and Development (OECD) 423 guidelines, with female Wistar rats receiving oral doses of 5, 50, 300, and 2000 mg/kg. The rats were monitored for physiological and behavioral changes over 14 days. Antioxidant activity was evaluated by determining the total phenolic content (TPC) and total flavonoid content (TFC) using the Folin-Ciocalteu and aluminum chloride assays, respectively, and by measuring radical scavenging activity (RSA) through the 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay. No adverse effects or mortality were observed at any dosage level, indicating the absence of acute toxicity. The TPC and TFC of the extract were 6.42 mg GAE/g and 7.39 mg QE/g, respectively. The DPPH assay revealed a dose-dependent increase in RSA, with an IC₅₀ value of 206.56 μg/mL, confirming substantial antioxidant potential. The results suggest that B. racemosa ethanolic leaf extract is both safe and potent as a natural antioxidant, supporting its potential for therapeutic applications. Further studies on chronic toxicity and bioactive compound identification are needed to fully validate its efficacy in treating oxidative stress-related diseases.