Pharmaceutical Chemistry- Scholarly Publications

Permanent URI for this collection

https://ir.unilag.edu.ng/handle/123456789/3749

Browse

Recent Submissions

Now showing 1 - 5 of 111
  • Item
    Open Access
    Chemical and Biological Insights on Phaulopsis falcisepala: A Source of Bioactive Compounds with Multifunctional Anticancer Potentials
    (Springer, 2022-12-06) Oladipupo, A.R; Alaribe, S.C.; Ogunlaja, A.S.; Beniddir, M.A.; Ogah, C.O.; Okpuzor, J.; Coker, H.A.
    In spite of remarkable progress and success made in anticancer research, major challenges in treatment of cancer remain recurrence of tumour and adverse efects of anticancer drugs. The search for novel, efective and safe anticancer agents, therefore remains important. This study investigated the chemical constituents of Phaulopsis falcisepala, a plant used in ethnomedicine to treat cancer; and evaluated anticancer and drug-likeness potentials of the constituents against selected non-small cell lung cancer (NSCLC), breast cancer, and chronic myelogenous leukemia (CML) targets. Lupeol and a mixture of stigmasterol and β-sitosterol were isolated from P. falcisepala and characterized using NMR, MS and IR data. Additional ffteen compounds, including piperine, piperanine, feruloyltyramine, asperglaucide and 6,7-dihydrofavopereirine were putatively identifed in the plant by analysis of its MS/MS data against tandem MS/MS data repository using the Global Natural Products Social Molecular Networking tool (GNPS). Using molecular docking, stigmasterol (‒ 7.8 to ‒ 10.1 Kcal/ mol), β-sitosterol (‒7.0 to ‒ 9.9 Kcal/mol), and lupeol (‒ 8.2 to ‒ 9.2 Kcal/mol) showed considerable binding afnities against non-small cell lung cancer and breast cancer molecular targets when compared to the reference inhibitors (‒ 8.4 to ‒ 10.8 Kcal/mol). Piperine (‒ 8.5 to ‒ 9.8 Kcal/mol), piperanine (‒ 8.5 to ‒ 9.6 Kcal/mol), and 6,7-dihydrofavopereirine (‒ 8.0 to ‒ 10.2 Kcal/mol) exerted good interactions with the active site, allosteric site and mutant form of BCR-ABL, an important target in chronic myelogenous leukemia. Many of the compounds in P. falcisepala were shown to possess fair to favourable drug likeness and ADME properties. However, lupeol, stigmasterol and β-sitosterol were predicted to have poor oral absorption.
  • Item
    Open Access
    Ameliorative influence of atorvastatin in transgenic Drosophila Melanogaster model of neurodegenerative diseases
    (Pharmaceutical Society of Nigeria, 2021-03-31) Ishola, I.O.; Badru, W.A.; Ofi, E.O.; Akinleye, M.O.; Adeyemi, O.O.
    Background: The common features in the pathogenesis of Alzheimer's disease (AD) and Parkinson disease (PD) (two most common neurodegenerative diseases) are chronic and progressive aggregation and accumulation of misfolded proteins (amyloid-beta and tau proteins in AD as well as α-synuclein in PD) leading to the destruction of vulnerable neurons and synaptic connections and ultimately neuronal cell death brain mass loss. Despite our knowledge of the molecular mechanisms implicated in AD and PD pathogenesis and primary target of therapeutic intervention being the misfolded protein aggregates, no efficient treatments are available. The fruit fly, Drosophila melanogaster (Drosophila), is a valuable model organism for neurodegenerative disease owing to its short lifespan and plethora of genetic tools for exquisite targeted manipulation of the genome. Thus, in this study the protective action of atorvastatin on genetic model of AD and PD in mice. Methods: To model PD and AD in Drosophila, the bipartite system of GAL4 transcriptional activator was placed under a cell-type specific promoter; embryonic lethal abnormal visual systemGAL4 (ELAV-GAL4) or dopa decarboxylase (Ddc-GAL4) for expression of amyloid-beta (Aβ42) or α-synuclein, respectively, under the control of the upstream activating sequence (UAS) in Drosophila. The flies were was either maintained on media supplemented with vehicle or atorvastatin (85, 170 or 340µM; HMG-CoA reductase inhibitor – antihyperlipidemic drug). The effect of treatments on larva motility, climbing activity, fecundity and lifespan were recorded. Results: Supplementation of fly media with different concentration of atorvastatin ameliorated the deficits in larva motility and climbing activity. Moreover, supplementation of fly media with atorvastatin prolonged the survival of drosophila but atorvastatin (384µM) reduced fecundity. Conclusion: Findings from this study showed that atorvastatin improved spontaneous motor activity and prolonged lifespan in Drosophila possibly through reduction of misfolded protein aggregates
  • Item
    Open Access
    Determination of Metals by Atomic Absorption Spectrometry in Unripe Plantain Peels Ash and Comparative Genotoxicity Studies with Kaun “Potash” Using Gel Electrophoresis and Diphenylamine Assay
    (JOURNAL OF CHEMICAL SOCIETY OF NIGERIA, 2019) Alaribe, C.S; Oladipupo, A.R; Gbadamosi, S.; Toye, E.T; Bashiru, K.A
    Every segment of society uses minerals and mineral resources each day for various purposes, including in diet and medications. One of such minerals is kaun, a crude mixture of various salts. Kaun, which is mainly a hydrated sodium carbonate but erroneously locally called “potash”, is the second most popularly used salt to sodium chloride in Nigeria. Interestingly, plantain peel ash has served as an alternative to kaun. Of concern, is the fact that most tribes use these substances in their diet without considering the harmful effect as a result of high intake and also the fact that they may be contaminated with heavy metals and other toxic substances. This study was done to investigate and compare the genotoxic effects of kaun and unripe plantain peels ash (UPPA) on the liver and kidney of mice and to evaluate the phytochemicals and metal content of UPPA. Phytochemical study revealed that tanins and carbohydrates were present in UPPA. Elemental analyses showed that UPPA contained high level of magnesium (32.481 ± 0.007 ppm), low levels of manganese, sodium, zinc and iron (2.285 – 0.720 ppm) and trace levels of chromium, copper, lead and cadmium (0.100 – 0.001 ppm). Acute toxicity study indicated that the LD50 values of kaun and UPPA are greater than 3000 and 6000 mg/kg, respectively. Genotoxicity assessment revealed that kaun and UPPA showed comparable effects on hepatic and renal cells and indicated that both substances may elicit genotoxic effect on hepatic cells, with no toxic effect on renal cells within the same doses and period.
  • Item
    Open Access
  • Item
    Open Access
    Investigation of selected metallic impurities in antimalarial Herbal Decoctions ‘AGBO IBA’ collected from four locations in Lagos State, Nigeria
    (UNILAG, Unilag Journal of Medicine, Science and Technology, 2019) Alaribe, S.C.; Oladipupo, A.R.; Musah, A.; Coker, H.A.
    Herbs constitute a common medicinal alternative for disease treatment in many cultures around the world. In Nigeria, these medicinal herbs are widely used in the treatment and prevention of various ailments including malaria, a global disease endemic to the tropics. In spite of their cultural trust and claimed medicinal properties, lack of standardization and poor-quality presentation make medicinal scientists to be wary of herbal medicinal preparations. However, due to their increasing patronage, the safety and quality of these herbal medicines have become increasingly important for health authorities, scientific community and the public alike. Thus this study was aimed at determining the amount of selected heavy metals in a herbal antimalarial decoction popularly known as ‘Agbo iba’ consumed in selected areas of Lagos. The investigated heavy metals: Pb, Ni, Hg and Cd were detected using Atomic Absorption Spectroscopy (AAS) after sample pretreatment with wet digestion using HNO3. Heavy metal concentrations in the decoctions were found to be in the range of 0.331 - 0.896 mg/L for Pb, 0.185 - 0.338 mg/L for Ni, 1.612 - 17.894 mg/L for Hg, while cadmium was not detected in the samples. These concentrations exceeded the World Health Organization (WHO) Permissible Limits (PL) and sources of contamination could be from sources of plants, harvest and transport conditions, method of preparations, to mention but a few. These products should be governed by standards of safety, quality, and efficacy that are equivalent to those required for other medicinal products of international standard.