Browsing by Author "Ekuadzi, E."
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Item Anti-inflammatory, Antioxidant and Cytotoxic Activities of Guibourtia ehie on Human Prostate (PC-3) and Breast Cancer (MC-7) Cell Lines and in silico Studies on Its Metabolite 7,4′-Dihydroxyflavone(Springer, 2022) Amponsah, I.K.; Ramos, G.F.; Harley, B.K.; Sarkodie, J.A.; Ekuadzi, E.; Ampofo, E.K.; Ben, I.O.Guibourtia ehie (A. Chev.).Léonard (leguminosae), is a forest tree of Africa used traditionally for tumours, wound cleansing and diarrhoea. However, some of these ethnomedical uses have not been validated scientifically. The present study aimed at investigating the anti-inflammatory, antioxidant and cytotoxic effects of the plant extract. The study further evaluates the contribution of its metabolite 7,4′-dihydroxyflavone to these effects. Anti-inflammatory activity of the 70% ethanol extract of the stem bark of G. ehie was established using the carrageenan induced foot oedema in 7-day-old chicks at 30–100 mg/kg body weight with diclofenac as reference drug. The DPPH radical scavenging activity was used for the antioxidant test whereas cytotoxic effect was done using prostate cancer (PC-3) and breast cancer (MC-7) cell lines with MTT as a measure of cell viability. In silico analysis of the pharmacokinetics and toxicity of the compound isolated from the plant was also performed. The extract and reference drug diclofenac inhibited foot pad oedema by 28.58% and 61.99% respectively over the 5-hour period. The isolate showed a marginally higher activity than the extract (32.64%). The extract was cytotoxic against breast (MC-7) and prostate (PC-3) cancer cell lines with respective IC50 values of 67.43 and 61.12 µg/mL but showed poor selectivity index (SI < 2). The isolate 7,4′-dihydroxyflavone was non-cytotoxic and this was also confirmed from the in-silico studies. G. ehie and its isolate exhibit anti-inflammatory and antioxidant effect as suggested by folklore medicine. The extract was cytotoxic to breast and prostate cancer cell lines but was nonselective.Item Antiplasmodial constituents from the stem bark of Polyalthia longifolia var pendula(Phytochemistry Letters, 2014-11) Annan, K.; Ekuadzi, E.; Asare, C.; Sarpong, K.; Pistorius, D.; Oberer, L.; Gyan, B.A.; Ofori, M.Along with two known compounds (1 and 2), four new clerodane diterpenes were isolated and identified from the stem bark of Polyalthia longifolia: cleroda-3-ene pyrrole-15,16-dione (3), cleroda-3-ene, pyrrolidine-15,16-dione (4), cleroda-3,13(14)E-diene-15,16-diamide (5), and cleroda-3-ene-15,16-diamide (6). Their structures were elucidated by combinations of NMR, MS and IR. Using the WHO Mark III Microtest assay, the isolated compounds were evaluated for their antiplasmodial effects. They showed antiplasmodial effects, with IC50s ranging from 4.5 to 213.8 μM. © 2014 Phytochemical Society of Europe. Published by Elsevier B.V. All rights reserved.Item In vitro antileishmanial activity and molecular docking studies of lupeol and monostearin, isolated from Parkia biglobosa(Scientific African, 2023) Osafo, T.; Philips, T.J.; Adomako, A.K.; Borquaye, L.S.; Ekuadzi, E.; Appiah-Opong, R.; Dickson, R.A.Parkia biglobosa (Leguminosae) is used traditionally for managing leishmaniasis. However, there are no reports of the antileishmanial constituents from the plant. This study is aimed at isolating antileishmanial compounds, from the stem bark of P. biglobosa, and assessing their mechanism of action using molecular docking studies. Bioassay-guided fractionation led to the isolation of two known compounds, lupeol and monostearin. Their structures were elucidated using their mass spectra. Using the 3-(4,5-dimethylthiazol-2- yl)-5-(3-carboxymathoxyphenyl)-2-(4-sulfophenyl)-2H-tretrazolium (MTS) assay, the evaluated antileishmanial effects of lupeol (1) and monostearin (2) showed IC50 values of 164.42 and 151.99 μg/mL respectively. The antileishmanial effects of the crude extract, non-polar, mid-polar and polar fractions were determined to be 64.43, 126.25, 725.65 and 167.52 μg/mL respectively. Molecular docking studies of the two isolates within the active sites of two validated targets in the Leishmania parasite: trypanothione reductase (TR) and pteridine reductase 1 (PTR1), showed that both compounds established important interactions with key amino acid residues in both proteins. Lupeol exhibited binding affinities of -7.1 kcal/mol and -10.2 kcal/mol for TR and PTR1, respectively, better than monostearin in both cases. Our findings back the claim that P. biglobosa stem bark possesses antileishmanial effects. Furthermore, the isolates lupeol and monostearin may be partly responsible for the observed activities.