Browsing by Author "Akande, Akinsola"
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- Item2-Aryl benzimidazoles: Synthesis, In vitro alpha-amylase inhibitory activity, and molecular docking study(Elsevier, 2018-03-06) Akande, AkinsolaDespite of many diverse biological activities exhibited by benzimidazole scaffold, it is rarely explored for the -amylase inhibitory activity. For that purpose, 2-aryl benzimidazole derivatives 1-45 were synthesized and screened for in vitro -amylase inhibitory activity. Structures of all synthetic compounds were deduced by various spectroscopic techniques. All compounds revealed inhibition potential with IC50 values of 1.48 ± 0.38-2.99 ± 0.14 M, when compared to the standard acarbose (IC50 = 1.46 ± 0.26 M). Limited SAR suggested that the variation in the inhibitory activities of the compounds are the result of different substitutions on aryl ring. In order to rationalize the binding interactions of most active compounds with the active site of -amylase enzyme, in silico study was conducted.
- ItemChemical Composition and Toxicity of Essential Oil of Vitellaria paradoxa (C.F. Gaertn.) from Nigeria(Taylor & Francis, 2013-06-24) Akande, AkinsolaThe essential oils from the leaves and stem-bark of Vitellaria paradoxa C. F. Gaertn. obtained by hydrodistillation were analyzed by GC/GC-MS. A total of 68 and 33 compounds representing 90.1 % and 95.1 % of the total oils were identified in the leaves and stem bark, respectively. The major constituent in the two oils was linalool (12.2 to 15.0 %). The essential oil has LC50 value between 160.098 and 171.240 μg/ml indicating moderate toxicity.
- ItemChemical Composition, Toxicity and Antibacterial activity of the Essential Oils of Garcinia mangostana from Nigeria(Taylor & Francis, 2013-06-04) Akande, AkinsolaThe chemical composition of the essential oils obtained from the leaves and stem-bark of Garcinia mangostana Linn. extracted by hydrodistillation were analyzed by GC and GC-MS. A total of 64 and 101 constituents, representing 96.1 % and 97.5 % of the total oil were identified in the leaves and stem-bark essential oils, respectively. β-caryophyllene (17.3 % - 21.1 %) was the most abundant constituent common in both oils. The essential oils were toxic to Artemia salina with LC50 value of 1.70 μg/ml and 5.15 μg/ml for leaves and stem bark oils, respectively. The antibacterial activities of the essential oils were carried out using agar well diffusion method. Garcinia mangostana stem-bark essential oil was more active against the tested bacteria.
- ItemChemical constituents, toxicity and antimicrobial activities of the essential oil from the leaves of tectona grandis(Elixir, 2013-07-28) Akande, AkinsolaThe leaves of Tectona grandis (Verbanaceae) was subjected to hydrodistillation in order to obtain the essential oil from the plant. The pale yellow essential oil gave a percentage yield of 0.184%. Relative percentages of individual component were analyzed by GC/GC-MS. A total of fifty-four (54) constituents were identified representing 86.5% of the total essential oil fraction. Oxygenated monoterpenes, sesquiterpene hydrocarbons, oxygenated sesquiterpenes, apocarotenoids, phenylpropanoids and non-terpene derivatives were the various classes of compounds identified. The LC50 value from the brine shrimp toxicity assay was 183.29μg/ml. The oil extract was also subjected to antibacterial assay and it showed significant activities against all the clinical test organisms used except Pseudomonas aeruginosa.
- ItemConstituents and Anthelmintic Activity Evaluation of Albizia Adiantifolia (Schumach) W.F. Wright Essential Oils FromNigeria(Canadian Center of Science and Education, 2018-03-30) Akande, AkinsolaAlbizia adiantifolia (Schumach) W.F. Wright (Fabaceae) is a plant used traditionally in treating different health ailments which includes worm infections. The essential oils (EOs) were obtained by hydrodistillation in an all glass Clevenger apparatus, and characterized by gas chromatography (GC) and gas chromatography-mass spectrometry analysis (GC-MS). In vitro petri-dish anthelmintic activity was carried out using adult earthworm, Eudrilus eugeniae. The leaves, stem bark and root bark EOs afforded a total of 40, 26 and 20 constituents representing 90.9%, 94.1% and 90.9% of the total oil fractions respectively. The classes of compounds identified in the leaves, stem bark and root bark are oxygenated monoterpenes (4.1%, 1.7% and 4.0% respectively), sesquiterpene hydrocarbons (39.5%, 67.3% and 42.6% respectively), oxygenated sesquiterpenes (18.7%, 22.3% and 30.1% respectively), non-terpene derivatives (12.1%, 2.6% and 14.2% respectively) and apocarotenoids (16.5% and 0.2% in the leaves and stem-bark). β-caryophyllene (23.0%), E-geranylacetone (7.4%), acorenone (6.4%), viridiflorol (6.4%), α-zingiberene (6.3%) and ar-curcumene (4.6%) were the major constituents in the leaves oil, β-caryophyllene (39.3%), selin-11-en-4-α-ol (10.4%), α-zingiberene (9.6%), ar-curcumene (7.2%), caryophyllene oxide (6.4%) and α-humulene (5.6%) were the major constituents in the stem bark oil, while β-caryophyllene (32.1%), selin-11-en-4-α-ol (13.1%), caryophyllene oxide (8.4%), pentadecanal (6.1%) and α -humulene (4.4%) were the major constituents in the root bark oil. β -caryophyllene dominated the oils. The leaf EO was the most active against E. eugeniae worm. All the oils showed a relatively higher activity compared to Albendazole, in a concentration dependent manner. There was significant difference (p<0.001) in activity.
- ItemEssential Oils: Therapeutic Effects as Anthelmintics(Nova Science, 2020) Akande, AkinsolaThe rate at which ignorance of hygiene and sanitary practices is being neglected in the suburban and rural areas of developing regions of the world never seem to reduce. Lack of adequate sanitation and health facilities together with deficiency in educating these rural dwellers on how to maintain proper hygiene has made the prevalence and impact of helminthiasis on public health and animal production a great socio-economic problem. Often associated with these problems are conditions such as anaemia, malnutrition, vitamin deficiencies, poor cognitive ability, less intellectual and mental development which are prominent in underage children and pregnant women. Animal health care and husbandry has also been hit as a result of this inadequate hygiene and sanitary practices which thus pose great challenge in food production. Most of the domestic animals serve as primary host to infectious helminths (worms) from which they are transmitted into humans. However, many naturally occurring secondary metabolites (phytochemicals) of plants such as terpenoids from essential oils, alkaloids, flavonoids, glycosides and tannins have been explored as leads to develop medicines for a disease-free and healthy society. Plants essential oils are ingredients present in formulations used ethno-medicinally, pharmaceutically, in food and cosmetic industries due to their potential bioactive and therapeutic activities against a wide spectrum of pathogenic organisms. Results from many reported researches as well as from our research findings, using the essential oils of plants from the Fabaceae species, showed the efficacy of some of these plant constituents as anthelminthics against various test organisms. The essential oils explored from plants of choice premised on their ethnobotanical survey in the treatment of one or more gastrointestinal troubles (GIT). The different essential oils studied demonstrated varying inhibitory activities (in vitro and in vivo) against different classes of helminth parasites (nematodes, cestodes, trematodes) and annelids which could be a lead to developing potent anthelmintics. As a result of these findings, the discovery of natural plant constituents should be kept on-going.
- ItemA Measurement of Selected Polycyclic Aromatic Hydrocarbons in Petroleum Product Contaminated Soils Using a Gas Chromatograph(Taylor & Francis, 2015) Akande, AkinsolaOil contaminated soils around refined petroleum products depot and retailing stations were investigated for selected polycyclic aromatic hydrocarbons (PAHs) to determine their levels in the soils. Soil samples were collected using standard analytical procedures and the petroleum hydrocarbons extracted using standard method, while the PAHs (benzo[a]pyrene, benz[a]anthracene, chrysene, benzo[b]fluoranthene, and anthracene) contents of the extracted petroleum hydrocarbons were determined using SNR 8126 gas chromatograph equipped with a flame ionization detector (FID). The results indicated that benz[a]anthracene has the highest concentrations in both the oil depot contaminated soils (59.1 ± 3.3 mg/kg) and oil retailing station contaminated soils (20.8 ± 2.1 mg/kg). The results also showed that the oil depot contaminated soils were burdened with the analyzed PAHs than oil retailing station contaminated soils; this was confirmed by the results of t test analysis. Comparison of the values of the PAHs in the oil impacted soils with their background levels showed that their values in the two sets of oil impacted soils were excessive; this was corroborated with their high pollution (PI) and geoaccumulation (Igeo) index values, except chrysene, which moderately polluted the soils (low PI and Igeo values); this was clear indication of indiscriminate discharge of petroleum fuels and petrochemicals into the soils.
- ItemMeasurements of Physicochemical, Elemental, and Total Petroleum Hydrocarbon Contents as Pollution Indicators of Soils in Petroleum Products Retailing Station Surrounding Areas(Taylor & Francis, 2015) Akande, AkinsolaSoils around petroleum products retailing stations were analyzed for their physicochemical, elemental, and total petroleum hydrocarbon contents with a notion to assess the contamination level of the soils. Samples were collected using standard analytical procedures and the elemental contents of the soils were determined using bulk scientific atomic absorption spectrometry/atomic emission spectrometry techniques, while total petroleum hydrocarbon and physicochemical parameters contents were determined using standard analytical techniques. Ten elements were analyzed and detected and their concentrations, enrichment factors, pollution index, and geoaccumulation index (Igeo) values established. The concentrations of most of the analyzed elements were higher in the oil-contaminated soils than those of other Nigerian soils, while the values of the analyzed physicochemical parameters followed the same trend. The results of the Igeo indicated that the soils were very heavily polluted (6.2–18.0) with all the metal, except V, which was heavily polluted (4.2). Very high enrichment factors and pollution index were obtained for Mn, Zn, K, Cu, Ni, Cr, and Pb. This was corroborated by their values, which were excessive when compared with their tolerable limits. The clustering results indicated that the elements were fairly correlated, indicating chemical affinity and/or similar sources. These were supported by the cross plot results (R2 = 0.5), and the results of Pearson correlation matrices for the elements. Average total petroleum hydrocarbons level (1,233.0 mg/kg) of the soils was high when compared to studies of similar settings. The overall results showed that the soils were highly contaminated and may pose a threat to public health.
- ItemSubstituted Benzimidazole Analogues as Potential α‑Amylase Inhibitors and Radical Scavengers(American Chemical Society, 2021-08-26) Akande, AkinsolaBenzimidazole scaffolds are known to have a diverse range of biological activities and found to be antidiabetic and antioxidant. In this study, a variety of arylated benzimidazoles 1−31 were synthesized. Except for compounds 1, 6, 7, and 8, all are new derivatives. All compounds were screened for α-amylase inhibitory, 2,2′-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), and 2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activities. In vitro screening results revealed that all molecules demonstrated significant α-amylase inhibition with IC50 values of 1.86 ± 0.08 to 3.16 ± 0.31 μM as compared to standard acarbose (IC50 = 1.46 ± 0.26 μM). However, compounds showed significant ABTS and DPPH radical scavenging potentials with IC50 values in the range of 1.37 ± 0.21 to 4.00 ± 0.10 μM for ABTS and 1.36 ± 0.09 to 3.60 ± 0.20 μM for DPPH radical scavenging activities when compared to ascorbic acid with IC50 values of 0.72 ± 0.21 and 0.73 ± 0.05 μM for ABTS and DPPH radical scavenging potentials, respectively. Structure−activity relationship (SAR) was established after critical analysis of varying substitution effects on α-amylase inhibitory and radical scavenging (ABTS and DPPH) potentials. However, molecular docking was also performed to figure out the active participation of different groups of synthetic molecules during binding with the active pocket of the α-amylase enzyme.
- ItemVariations in Chemical Constituents and Anthelmintic Activity of Albizia zygia (DC.) J.F. Macbr. Essential oils from Ibadan, Nigeria(2018) Akande, AkinsolaThe widespread and impact of helminth infection on public health is a socio-economic problem in developing nations. Albizia zygia (DC.) J.F Macbr. (Fabaceae; Sub-family – Mimosoideae) is a gum producing tree often useful in the treatment of stomach troubles, as anti-parasitic, antidote, purgative and vermifuge purposes in traditional medicine. This study however, was designed to evaluate the chemical constituents and anthelmintic activity of A. zygia essential oils. The leaves, stem bark and root bark essential oils (EOs) of the plant were extracted by hydrodistillation, analysed by Gas Chromatography (GC) and Gas Chromatography-Mass Spectrometry (GC-MS) techniques and further subjected to an in vitro petri-dish anthelminthic assay. The EOs yield range from 0.254 to 0.268%, a total of 38 (97.6%), 37 (92.2%) and 37 (97.2%) constituents of the total oil fractions were identified in the leaves, stem bark and root bark respectively. Oxygenated sesquiterpenes (28.0%) dominated the leaf oil while non-terpene derivatives (44.4% and 27.8%) dominated the stem bark and root bark oils respectively. Major constituents identified include limonene (11.1%), acorenone (10.9%), -caryophyllene (10.6%), valerianol (6.4%) and 1,8-cineole (5.8%) in the leaves oil, 2,6,10-trimethylpentadecane (26.5%), 1,8-cineole (12.4%), (E)--ionone (6.3%) and acorenone (6.0%) in the stem bark oil, while 1,8-cineole (14.8%), 2,6,10-trimethylpentadecane (12.1%), limonene (10.6%), -caryophyllene (7.1%) and viridiflorene (5.8%) were identified in the root bark oil. A. zygia EOs obtained from this study and from literature in two different years, vary significantly in chemical composition. The oils exhibit anthelmintic activity against Eudrilus eugeniae worms in vitro. Paralysis and death of worms occurred faster as EO concentrations were increased. The root bark EO showed the best activity. Significant difference (p<0.001) in activity was observed between the oils and the standard drug, Albendazole. Thus, suggests that A. zygia EOs showed promising anthelmintic properties.