Journal of Phytomedicine and Therapeutics

Antioxidant and antidiabetic properties of Tetrapleura tetraptera (Schum. and Thonn.) Taub. whole fruit

Daniel Akingbolabo Ogunlakin — 2024-06-27

The objective of this study is to investigate toxicity, phytochemical constituents, antioxidant and antidiabetic activities of Tetrapleura tetraptera whole fruits. Phytochemical screening of the extract identified the presence of alkaloid, saponin and flavonoid. The total phenolic contents of methanol extract, hexane, chloroform and ethyl acetate fractions are of 38.63 ± 8.11, 52.41 ± 1.92, 8.16 ± 0.36 and 5.16 ± 0.56 mg gallic acid equivalent/g of extract, respectively, while methanol extract, hexane, chloroform and ethyl acetate fractions had total flavonoid contents of 6.87 ± 0.81, 7.44 ± 0.78, 12.38 ± 0.72 and 9.32 ± 0.37 mg quercetin equivalent/g of extract, respectively. The IC₅₀ for DPPH radical scavenging activity of methanol extract, hexane, chloroform and ethyl acetate fractions are 192±2.01, 226.67±1.40, 73.33±1.86 and 127.33±3.18μg/mL respectively. The IC₅₀ value of ascorbic acid was 18.44±1.20 μg/mL. The methanol extract of T. tetraptera fruit (1g/kg bw.) produced a significant (p<0.05) reduction of fasting blood glucose level. There was an increase in the plasma level of ALT in T. tetraptera treated rats compared to the control. According to histopathological examinations of the pancreas of diabetic rats given methanol extract treatment, the pancreatic islets' size was noticeably reduced, the islets of Langerhans' outlines were atypical, and there were numerous hemorrhages throughout the organ. These results indicate that the fruit of T. tetraptera may be a source for future oral hypoglycemic drug development.

N'-(2,6-dimethoxybenzylidene)-3-(4-methoxyphenyl) acrylohydrazide abates oxidative stress and purinergic enzymes abnormality associated with iron-induced cardiotoxicity in Wistar rats: Experimental and computational perspectives

Daniel Akingbolabo Ogunlakin — 2024-06-27

The effects of N'-(2,6-dimethoxybenzylidene)-3-(4-methoxyphenyl) acrylohydrazide (KAD 9) on iron-induced cardiac injury was investigated. Evaluations of the iron chelating capability, ferric-reducing antioxidant power (FRAP), as well as DPPH free radical scavenging activity of KAD 9 were performed. The oxidative cardiac injury induced by 0.1 mM FeSO4 was treaed with varied doses of KAD 9 ex vivo. Comparing KAD 9 to conventional quercetin, the DPPH radical scavenging ability of KAD 9 significantly rises with concentration (p<0.05). The cardiac injury was generated, and this resulted in decreased malondialdehyde (MDA), catalase (CAT), ATPase, and ENTPDase activity (p<0.05). A notable increase in GSH level was seen in KAD 9 treated group. Furthermore, it was observed that KAD 9 had closer binding affinity with ATPase and ENTPDase. Due to its ability to regulate nucleotide hydrolysis and lessen oxidative stress, KAD 9 has the potential to both treat and protect against oxidative cardiac injury.

Antipsychotic property of methanol crude extract of Peperomia pellucida (L) Kunth. (Piperaceae) whole plant against ketamine induced psychosis in mice

Arowona Isimot Temitope — 2024-06-27

Medicinal plants have been discovered and used in traditional medicine practice since prehistoric times. Numerous plants contain diverse phytochemicals and possess pharmacological actions, many of which remain unassessed by rigorous scientific research of defined efficacy and safety. This study evaluated the antipsychotic activity of Peperomia pellucida methanol crude extract against ketamine induced psychosis in Swiss albino mice. The preliminary phytochemical analysis was carried out following standard procedures, while stereotypy test, Y-maze test, object recognition and forced swim test (FST), were the behavioral models used for the antipsychotic study. The Histopathology of the mice brain was also carried out. Statistical analysis was done using one-way ANOVA followed by Dunnett’s post hoc test and p < 0.05 was considered significant. Phytochemical analysis revealed the presence of saponins, tannins, flavonoids and alkaloids in the pulverized plant. The crude extract at 125 mg\kg reduced stereotype behavior in Ketamine-induced mice. The extract enhanced cognition in the animals by producing a significant dose-dependent decrease in the number of alternate arm entries and increases the time spent in recognizing a novel object compared to the negative control. In the FST model, 500 mg\kg was more effective in decreasing immobility as compared to negative control. The histopathology of the mice brain showed that the extract at the dose of 500 mg/kg produced a similar effect to the standard drug and at 250 mg/kg produced a regenerative effect on brain of the mice.
The results established that Peperomia pellucida possesses antipsychotic property against positive, negative and cognitive symptoms of psychosis.

Evaluation of synergistic cytotoxic potential of Zingiber officinale and Allium sativum on Wistar rats testes

Joseph Oyepata Simeon — 2024-06-27

Plants decoction has been used since ancient times for various disease manifestations. It is usually believed that combining different plants source ensures efficacy. Garlic and ginger combination have been used in treating various illness such as cold, growth, immunity and infections. The combined effects of Zingiber officinale and Allium sativum extracts were tested on the testicles of Wistar rats by evaluating haematological, cell viability and histopathological parameters. The study was done by dividing male Wistar rats into 4 groups. Each group received different concentrations of extracts (group 1; 100 mg (ginger) + 150 mg/kg garlic, group 2. 200 mg + 300 mg/kg, group 3; and group 4; 400 mg + 450 mg). Cell isolation, cell viability and histological analysis were performed in the testicles. Compared with the control group, there was no increase in RBC (P<0.05) but a decrease in WBC (P<0.05) in all groups given GG extract. Compared with the control group, there was no significant difference in the level of living cells in groups 2 and 3 (P<0.05), while in group 4 the level of dead cells decreased slightly compared to the control group (P<0.05). No significant change in superoxide dismutase was seen in molecular tests. Histological examination showed a significant improvement in cellularity. The results show that taking garlic and ginger extract has no effect on tumor function.

Evaluation of the effects of co-processed Manihot Esculenta starch on the tablet properties of directly compressed diclofenac and paracetamol formulations

Olayemi J Olubunmi — 2024-06-27

Advancements in tablet manufacture has increased the demand for versatile excipients with multifunctional applications. Co-processing is fast evolving into the tool for development of these excipients with unique functional properties. The aim of this study is to evaluate the effect of co-processed Manihot esculenta starch and povidone on tablet properties of diclofenac and paracetamol formulations. Starch extracted from Manihot esculenta tubers was modified either by pre-gelatinization or gelatinization and then co-processed by co-dispersion with povidone to yield EXP-A and EXP-B respectively. The developed excipients were assessed for their flow properties, moisture contents, swelling indices, hydration capacities and particle densities. The co-processed excipients and a physical mixture of the excipients were incorporated into diclofenac and paracetamol tablet formulations by direct compression. The tablets were evaluated for uniformity of weight, hardness, friability, disintegration time and in vitro drug release. Possible drug-excipient interaction was also investigated by Fourier Transform Infrared Spectroscopy (FT-IR). Results showed that EXP-B possessed better flow properties, higher swelling index and hydration capacity and lower moisture content than EXP-A. All the tablets had uniform weights, tablet hardness was between 4.5 and 11 kp; tablets containing higher amounts of EXP-A or EXP-B had higher hardness. Friability was between 0.45 and 4.02 with tablets containing EXP-A having lower values than the other batches. Disintegration time was between 1.45 and 12.77 min with tablets containing unmodified starch in both formulations having the least values. Dissolution profile was similar for tablets containing co-processed excipients. Co-processing starch from Manihot esculenta tubers with povidone produced robust tablets which may be better suited for modified-release tablet formulations.

Evaluation of the Analgesic, Anti-inflammatory and Anti-haemorrhoidal Activities of Àgbo jẹ̀dí.

Lucy B John-Africa — 2024-06-27

Herbal medicines find patronage among both rural and urban populaces. Despite the popularity of these herbal remedies, claims of their therapeutic value remain without validation. Àgbo jẹ̀dí (AJ) is an herbal mixture often marketed for the treatment of lower back pain and haemorrhoids. Preliminary phytochemical testing was carried out using standard protocol. Acute toxicity test was done using the OECD No 423 guidelines. Analgesic and anti-inflammatory studies were performed using acetic acid-induced abdominal writhing and formalin-induced paw licking and paw oedema in mice. The effects of AJ on croton oil-induced haemorrhoids in Wistar rats was also tested. Qualitative phytochemical analysis showed presence of tannins, saponins, terpenes, steroids, flavonoids and anthraquinone glycosides. Elemental analysis was positive for K (25.95) > Mg (12.51) > Na (12.04) > Ca (4.01) > Zn (0.3805) ele. No abnormal signs of toxicity or lethality were observed at 20 ml/kg. AJ significantly reduced acetic acid-induced pain by 49.64, 47.45 and 64.23 % at 1.2, 2.4 and 4.8 ml/kg respectively, and diclofenac (10 mg/kg) reduced pain by 88.32%. Àgbo jẹ̀dí also exerted 66.67%, 66.67% and 73.33% reduction of formalin-induced pain at 55 - 60 min post pain induction while diclofenac was 88.00%. Paw volume was decreased by 31.5%, 53.93%, 50.79% at 1.2, 2.4 and 4.8 ml/kg doses respectively. Similarly, diclofenac produced 69.84%. Histological assessment showed mild protective actions by AJ as the intensity of damage to recto-anal tissues were not significantly altered. In conclusion, in-vivo acute toxicity test carried out showed 'àgbo jẹ̀dí' to be relatively safe on acute oral administration. It was observed to exhibit analgesic and anti-inflammatory activity but devoid of substantial anti-haemorrhoidal actions.

Biochemical reactivity and Inhibiting studies on cyclopentane-anthraquinone based compounds as potential Vascular endothelial growth factor Inhibitors

Abel K. Oyebamiji — 2024-06-27

Introduction: The efficiency of heterocyclic compounds as potential vascular endothelial growth factor inhibitor has drawn the attention of scientists globally.
Objective of study: this work is aimed at identifying the most proficient anticancer cyclopentane-anthraquinone based compound via density functional theory and molecular modeling analysis.
Method: In this work, the inhibiting capacities of cyclopentane-anthraquinone based compounds were examined using insilico method. The optimization was carried out using density functional theory and the molecular modeling studies were executed via induce fit docking and molecular dynamics simulation methods.
Result: Compound 13 among other compounds have highest binding affinity compared to 5-FU (Standard) via induce fit docking study; however, the report by binding energy, root mean square deviation and root mean square fluctuation via molecular dynamic simulation study revealed otherwise. The pharmacokinetic study on compound 13 and 5-FU was examined and reported. Conclusion: These discoveries may provide perception into developing more potent potential library of drug-like triazole-based compounds as proficient anti-diabetic agents.

Integrated approach for studying anti-angiotensin converting enzyme activity of triazole derivatives to down-regulate diabetes

Abel K. Oyebamiji — 2024-06-27

The effects of triazole and its derivatives as anti-angiotensin converting enzyme activity were investigated using combined computational approach. This work is directed at examining the anti-angiotensin converting enzyme activity of the studied triazole derivatives via density functional theory and molecular modeling studies using in silico approach. This work was executed using Spartan 14 for optimization. The downloaded receptor (human angiotensin-converting enzyme (PDB ID: 3NXQ)) from protein data bank by removing water molecules and other small molecules downloaded with the target before subjecting it to docking calculation and molecular dynamic simulation studies. In this work, we discovered that addition of methyl and 2-ethyl-1H-indole to triazole as parent compound enhanced the activity of compound 4 and this was revealed via the predicted highest occupied molecular orbital (HOMO) (-4.53 eV) and energy gap (3.73 eV). More so, Compound 4 with -10.5 kcal/mol possess the highest strength to impede human angiotensin-converting enzyme (PDB ID: 3NXQ) than other investigated compound and the metformin. The developed quantitative structure activity relationship (QSAR) with squared correlation coefficient (R²) of 0.745234 and adjusted R² of 0.617852 proved to be valid and predictable which was confirmed via the predicted percentage inhibiting concentration (%IC₅₀). The molecular dynamic simulation and pharmacokinetic studies of the compound ((Compound 4) and the reference drug (metformin)) that possess the highest binding affinity were investigated and reported. These findings may give insight into developing library of drug-like triazole-based compounds as proficient anti-diabetic agents.

Antioxidant, anti-inflammatory and anti-glycation activities of some 4-aminoantypyrine derivatives: In vitro and in silico study

Ehimen Annastasiaa Erazua — 2024-06-27

Aminoantipyrine exhibits antioxidant and anti-inflammatory effects. However, its potential as an anti-glycating agent has not been extensively studied. This research aims to investigate the antioxidant, anti-inflammatory, and anti-glycation properties of specific derivatives of 4-amino antipyrine through experimental and theoretical methods. Thirteen Schiff bases were synthesized by reacting 4-aminoantipyrine with substituted benzaldehydes, and seven ether derivatives were obtained from these Schiff bases via Williamson ether synthesis. The compounds were characterized using FT-IR, UV-visible, EI-MS, and ¹H NMR analyses. Cytotoxicity assessments were conducted using brine shrimp and 3T3 mouse fibroblast cell lines. Molecular descriptors were obtained from Density Functional Theory (DFT) calculations, and molecular docking was used to determine binding affinity. Additionally, in-silico ADMET (adsorption, distribution, metabolism, excretion, and toxicity) screening was performed. The synthesized compounds were evaluated for anti-inflammatory, antioxidant, and anti-glycation properties. The results showed promising activities for three compounds in the anti-inflammatory assay. Five compounds demonstrated significant antioxidant effects, while eight exhibited moderate anti-glycation properties. Compounds S1 and S13 show potential inhibition against the anti-inflammatory, antioxidant, and anti-glycation activities. DFT calculations and molecular docking identified S6, S7, and S9 as the most active compounds. All compounds displayed favorable results in terms of oral bioavailability, lipophilicity, pharmacokinetics, and toxicity prediction. These derivatives of 4-aminoantipyrine were non-toxic and showed potential as drug candidates due to their anti-inflammatory, antioxidant, and anti-glycation properties.

Quantification of selected polyphenols in hydroethanolic garlic extract using high performance liquid chromatography and their effects on drosophila neuropeptides: a molecular docking study

Ademola O. Ayeleso — 2024-06-27

Garlic (Allium sativum) is a bulbous plant, which has been established to possess diverse medicinal properties. The neuropeptides of Drosophila melanogaster function to control major metabolic activities of the fruit flies. Thus, this study aimed to identify polyphenols that can distort the expression of some selected neuropeptides that are responsible for satiety in Drosophila melanogaster . High Performance Liquid Chromatography (HPLCHPLC) analysis was performed on hydroethanolic garlic extract, after which an in silico pharmacokin etics screening and molecular docking studies were performed using 10 selected polyphenols in garlic as ligands, and UDP 2 , Hugin and dNPF as neuropeptide targets responsible for satiety. The hydroethanolic garlic extract had gallic acid to be most abundant , followed by isovallinic acid and protocatechuic acid (7.736, 3.024 and 2.235 ppm respectively). The least present polyphenols are quercetin, rutin, orientin and isoorientin (0.561, 0.907, 0.948 and 0.913 ppm respectively). However, after docking analysis , isoorientin showed the best binding affinity with all the neuropeptide targets that were analysed at their respective binding site with docking score of upto 7.8 kcal/mol. This study predicted that isoorientin could serve as therapeutic agents to control satiety.

Hematological, biochemical and histological evaluation of sub-chronic administration of ethanol leaf extract of Canscora decussate on kidney and stomach of Wistar rats

Joseph Opeyemi Tosin — 2024-06-27

Canscora decussate is traditionally believe to relieve renal and gastro intestinal tract disorder. Ethanol leaf extract of Canscora decussate was tested for chronic effect on Kidney and Stomach of wistar rats by evaluating the hematological, biochemical and histological parameters of these organs. The study was done by grouping the animals in to 4 groups with each group receiving different concentrations of the extract (100-400mg/kg) respectively for 28 days, physical observation of the rats was carried out every day of the study. Mean corpuscular volume, and red blood cell levels decreased significantly (P≤0.05) at 200 and 400 mg/kg doses, but not basophiles, neutrophils, eosinophils, or platelets. There was no significant change (p≤0.05) in serum sodium chloride, potassium creatinine and urea when compared to the control group at all doses delivered. Slight lymphocyte hyperplasia with normal kidney histology architecture observed at all doses and the control (10 ml/kg). Canscora decussateis relatively safe for use as it does not possess danger against traditional use.

Unveiling cyclic tetra amino acids-based peptides as insulin degrading enzyme inhibitors: insight from Insilico approach

Faith Eniola Olujinmi — 2024-06-27

Type II diabetes has become one of the ailment that poses a grave universal wellbeing trial and the desire to curtail its dangerous activities has drawn the attention of various researchers globally. Several resistances developed by type II diabetes to series of previous drug-like small molecules has trigger the desire of researchers to attempt the use of tetra-amino acid based peptides to combat this menace. Thus, inhibiting activity of tetra amino acid based-peptides against insulin degrading enzyme (pdb id: 4re9) resulted into series of binding affinities values and (3R,6S,9S)-9-((R)-1-(benzyloxy)ethyl)-3-(((4-chlorophenyl)thio)methyl)-6-methyl-1,4,7,10-tetraazacyclododecane-2,5,8,11-tetraone (compound F) with -8.16984558kcal/mol proved to have greatest strength to inhibit the studied target. The calculated binding energy generated from molecular dynamic simulation (MDS) supported the efficiency of compound F than referenced compound (Metformin). The report from ADMET investigations were presented and interpreted accordingly.