Browsing by Author "Iweala, Emeka Joshua"

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Acute oral toxicity and antimalarial studies of 7-[(7-methoxy- 4,5-dihydro-1H-benzo[g]indazol-3-yl)carbonyl]-2-phenyl- 5,6,7,8-tetrahydropyrazolo[1,5-a]pyrido[4,3-d]pyrimidin-9 (1H)-one in mouse models
(Scientific African, 2024) Oladejo, David O; Dokunmu, Titilope M; Tebamifor, Mercy E; Omunagbe, Mercy B; Okafor, Esther O; Iweala, Emeka Joshua
Ethnopharmacological relevance, phytochemistry, potential health benefits and toxicity profile of Ananas comosus (L.) Merr (pineapple)
(Pharmacological Research - Natural Products 10 ( Elsevier), 2026) Ugbogu, Eziuche A.; Iweala, Emeka Joshua; Ukachukwu, Chukwudi Eke; Babayo, Christy; Dania, Omoremime Elizabeth; Isreal, Chollom Longs; Omonhinmin, Conrad A.; Cleanclay, Wisdom D.; Okoro, Benedict Chukwuebuka
In traditional medicine, the cortexes of A. comosus are used as an alexipharmic, antitussive, and antidiarrheal agent, while the leaves are commonly used as a remedy for indigestion. This review provides a thorough and upto- date literature on the ethnopharmacological uses, phytochemistry, and potential health benefits of A. comosus. The articles used for this study were obtained from databases such as ScienceDirect, Frontiersin, PubMed, Springer, and MDPI. In addition, only articles written in English were included in this review. Phytochemical analysis revealed that A. comosus contains numerous biologically active compounds, including n-hexadecanoic acid, bromelain, n-heptadecanol-1, methyl ester, hexadecanoic acid, squalene, α-tocopherol, tetradecane, 5- hydroxymethylfurfural, dihydroxyacetone, dodecane, DL-α-tocopherol, furan methanol, dodecanoic acid, and 2,4,6-cycloheptatrien-1-one, among others. Various in vivo and in vitro biochemical studies have also shown that A. comosus possesses antioxidant, anti-inflammatory, anticancer, antidiarrheal, antimicrobial, antimalarial, cardioprotective, anthelmintic, and antidiabetic properties. Therefore, this review shows the biologically active compounds in A. comosus and the potential of different parts of A. comosus to prevent and treat various diseases. While A. comosus has shown promise in animal studies, human clinical trials are needed to determine safe and effective doses. Further research may reveal additional uses for this versatile plant as a functional food and in modern healthcare as a traditional and complementary alternative medicine.
Gene expression levels and inhibitory effect of 7-[(7-methoxy- 4,5-dihydro-1H-benzo[g]indazol-3-yl)carbonyl]-2-phenyl- 5,6,7,8-tetrahydropyrazolo[1,5-a]pyrido[4,3-d]Pyrimidin-9 (1H)-one (MCL) against AP2-I and BDP1 in malaria experimental models
(Scientific African, 2024) Oladejo, David O; Anzaku, Dorathy O; Mamudu, Collins O; Elugbadebo, Temitope; Dokunmu, Titilope M; Adebiyi, Ezekiel F; Iweala, Emeka Joshua
Resistance to antimalarial drugs leads a global recurrence of malaria, posing a significant challenge to malaria control. This study aimed to assess gene expression and resistance profiles in clinical isolates, and validate the inhibitory effect of MCL compound against PbAP2-I and PbBDP1 genes in vivo. Malaria prevalence rate throughout the clinical study period stood at 12.24%. Blood samples were obtained from 182 malaria outpatients and 30 P. berghei-infected mice treated with varying MCL concentrations. DNA and RNA were extracted. PfAP2-I, PfBDP1, PfMDR1, and PfK13 genes were amplified using Real-time qPCR and sequenced for mutation profiling. Relative gene expression of AP2-I and BDP1 genes in P. falciparum and P. berghei-treated mice was carried out by Reverse-transcription PCR. The data were analyzed using ANOVA at P<0.05 indicating a significant difference. Relative gene expression results from clinical isolates showed PfAP2-I and PfBDP1 are highly expressed in the trophozoite and schizont stages. The clinical isolates show conserved nucleotide sequences for PfAP2-I, PfBDP1, and PfK13 genes compared to the 3D7 strain. However, Asn86Tyr mutation implicated in antimalarial drug resistance and Leu1312Iso mutation not previously reported to be associated with antimalarial drug resistance were observed for the PfMDR1 gene. MCL inhibited the expression of PbAP2-I (by 4.52 and 8.08 folds) and PbBDP1 (by 37.92 and 79.07 folds) at 40μM and 50μM concentrations after a 7-day, single oral daily dose. Our findings validate MCL’s inhibitory activity against AP2-I and BDP1 genes, hence representing potential new targets of antimalarial therapy for controlling malaria parasite invasion.
P11-038 Phytochemical, antioxidant and mitochondrial permeability transition analysis of fruit skin ethanolic extract of Annona muricata Linn. (Soursop)
(Abstracts / Toxicology Letter, 2025) Iyanda-Joel, W.; Adegbite, O.; Ajetunmobi, O.; Chinedu, S.; Iweala, Emeka Joshua; Rotimi, S.
Question: Annona muricata Linn. contains a group of bioactive long chain fatty acid derivatives called Annonaceous acetogenins, which have shown selective cytotoxicity against several cancer cell lines and other abnormal cells by a known mechanism. The current study analyzed the phytochemical and antioxidant properties of the fruit skin ethanolic extract of Annona muricata (ESA) and its effect on the opening of rat liver mitochondrial membrane permeability transition (MMPT) pore in vitro. Methods: Tests for the phytochemical constituents of the extract and antioxidant assays were carried out following standard protocols while the opening of the MMPT pore in the presence of varying concentrations of the extract was spectrophotometrically assayed under succinate-energized conditions. Calcium chloride (CaCl2) solution and spermine at specified concentrations were employed to trigger and inhibit MMPT pore opening respectively. Results: The results show that terpenoids, steroids and glycosides were found present in the fruit skin ethanolic extract and the extracts were found to have very low antioxidizing properties at the tested concentrations based on the diphenyl-1-picryhydrazy (DPPH) radical scavenging activity assay. Lipid peroxidation was induced in a concentration-dependent manner on both the cytosolic and mitochondrial hepatocyte fractions in vitro. In the absence of triggering agent, 0.84 mg/ml concentration of ESA induced the opening of the pore by 129% whereas the other three lower concentrations (0.12 mg/ml, 0.36 mg/ml and 0.60 mg/ml) did not induce MMPT pore opening. In the presence of the triggering agent, the extracts showed no inhibitory activity; rather there was a greater increase in the induction with increasing concentration of extracts. Conclu- sions: From the foregoing, the fruit skin ethanolic extract of Annona muricata may possibly contain bioactive components that are likely to induce apoptosis thereby adding to the growing list of naturefriendly chemopreventive and curative therapy of cancer.
Phytochemical composition, acute and subacute toxicity profile of Persea amaricana seed oil in albino Wistar rats
(Toxicology Reports, 2025) Iweala, Emeka Joshua; Okore, Finian Uchenna; Okoro, Benedict Chukwuebuka; Dania, Omoremime Elizabeth; Amuji, Doris Nnenna; Ugbogu, Eziuche Amadike
Objective: This study investigated the phytochemical composition and toxicity profile of Persea americana seed oil (PASO) in albino Wistar rats. Methods: Chromatography-mass spectrometry (GC-MS) was used to analyse the chemical constituents of PASO. For the acute toxicity test, PASO was administered orally in a single dose of up to 3000 mg/kg body weight (bw). For the subacute toxicity test, the rats were divided into four (4) groups. Group I (normal control), while groups II, III and IV received 200, 300 and 400 mg/kg PASO daily, respectively, for 14 days. Results: In the acute toxicity test, the lethal dose (LD50) of PASO was estimated to be 1477.83 mg/kg. In the subacute toxicity test, PASO significantly increased (p < 0.05) aspartate aminotransferase, creatine phosphokinase, alanine aminotransferase, creatinine, alkaline phosphatase, urea, malondialdehyde, high density lipoprotein, interleukin 1-beta (IL-1β), tumour necrosis factor (TNF-α) and cardiac troponin and significantly decreased glutathione, red blood cells (RBC), packed cell volume (PCV), superoxide dismutase and catalase compared to the control group. Conclusion: Our study showed that the LD50 of PASO is 1477.83 mg/kg body weight, which classifies it as a moderately toxic substance. In subacute toxicity, our results revealed that treatment with PASO resulted in an increase in liver enzymes, urea and creatinine, and inflammatory markers, and a decrease in antioxidant enzymes, suggesting that PASO impairs liver and kidney functions and may cause cardiac or muscle damage in albino Wistar rats.
Protein biomarkers for diagnosis of breast cancer
(Scientific African, 2024) Iweala, Emeka Joshua; Amuji, Doris Nnenna; Nnaji, Faith Chinasaokwu
Breast cancer remains a major global health challenge, demanding better diagnostic tools. Traditional methods like mammography have limitations, highlighting the need for specific, noninvasive approaches. Protein biomarkers offer a promising avenue for early and accurate detection, potentially leading to improved patient outcomes and personalized treatment. This review explores key protein biomarkers, including Estrogen Receptor (ER), Progesterone Receptor (PR), Human Epidermal Growth Factor Receptor 2 (HER-2), and Cancer Antigen 27.29(CA27.29), focusing on the proteomic methodologies used in their discovery and validation. However, challenges exist, such as variability in biomarker expression and limitations in abundance, stability, and specificity, which hinder clinical use. The review discusses innovative strategies to overcome these challenges, emphasizing the importance of translating biomarker research into practical applications for personalized medicine in breast cancer diagnosis and therapy. This exploration contributes to the evolving field of breast cancer diagnostics, paving the way for future discoveries and improved patient care.