In-vitro anti-inflammatory activities of 3-methoxy quercetin isolated from Nigerian mistletoe parasitic on Garcinia kola Heckel, Clusiaceae

Purpose: To evaluate the in vitro anti-oxidant and anti-inflammatory potential of the most potent and abundant metabolite, 3-methoxy quercetin (3-MQ), from extract fractions of mistletoe, Loranthus micranthus Linn (Loranthaceae) parasitic on Kola acuminata Schott & Endl, (Malvaceae), also known as Garcinia kola Heckel, (Clusiaceae).Methods: Compounds isolated through a combination of chromatographic techniques were screened for in vitro antioxidant potential using the diphenyl picrazyl hydrazine (DPPH) radical-based model. Cell viability at 1–1000 μM 3-MQ in 24 h was evaluated by 3-(4, 5-dimethylthiazol-2-yl)-2, 5- diphenyltetrazolium bromide (MTT) test. Lipopolysaccharide (LPS), phorbol 12-myristate 13-acetate (n = 5) five (5) replicates.Results: Ten (10) known compounds including 3-MQ (1) were isolated and characterized. 3-MQ exhibited highly significant (p < 0.05) antioxidant activity with 50 % inhibitory concentration (IC50) of 15.0 μM; concentrations ≤ 100 μM did not exert cytotoxic effect. 3-MQ, at 25 and 125 μM concentrations, significantly (p < 0.05) inhibited the production of TNF-α by 82 and 100 %, respectively, compared to controls.Conclusion: The results demonstrate the potent anti-inflammatory activity of 3-MQ and suggests its use as a potential alternative therapy for inflammation and related diseases.Keywords: Loranthus micranthus, Kola acuminata, Garcinia kola, Anti-inflammatory, Cytotoxicity, Chemiluminescence, Antioxidant, TNF-

Anti-inflammatory activity and accelerated stability studies of crude extract syrup of Cannabis sativa

Purpose: To formulate Cannabis sativa-based syrup and investigate its anti-inflammatory potential and the stability of the formulation under stress conditions.Methods: The syrup was prepared using different combinations of crude C. sativa resin, propylene glycol, aspartame, sucrose, sodium metabisulphite (SMBs) and ethylenediaminetetraacetic acid (EDTA). The stability of the formulations was determined under accelerated temperature conditions. The anti-inflammatory activity of the resin and different formulations were evaluated by the egg albumin induced paw edema model in rats. Biochemical assay was determined by Reitman and Frankel colorimetric assay method while hematological assay was evaluated by standard protocols.Results: EDTA-containing syrup (CE) was the most stable with estimated shelf-life of 2204 days (K25ºC, 4.78 x 10-5/day). Higher propylene glycol levels significantly improved anti-inflammatory activity compared to those containing a lower amount. All the formulations showed anti-inflammatory activity higher than the crude resin with a dose-dependent inhibition of paw edema compared with the control. There was no significant difference (p < 0.05) between the serum glutamate-oxaloacetate transaminase (SGOT, 13.821 ± 0.190 - 16.008 ± 1.012), serum glutamate-pyruvate transaminase (SGPT, 19.241 ± 1.027 - 22.901 ± 1.093) and urea (9.812 ± 0.252 - 10.054 ± 0.252) levels of the treated and 16.856 ± 1.053, 24.960 ± 0.101 and 10.654 ± 0.925 units/L of the control animals respectively. With the exception of eosinophil that disappeared from the blood in the third week, all the hematological parameters showed a gradual increase in lymphocytes, neutrophils, monocytes, packed cell volume (PCV), white and red blood cell counts in the third week compared to control.Conclusion: Formulation of C. sativa as syrup using efficient carriers improves the pharmacological activity of the crude extract. SMBs and EDTA significantly enhance the stability of the syrup with no observable biochemical and hematological changes in treated animalsKeywords: Cannabis sativa, Syrup, Anti-inflammatory, Stability, Hematologica

Organisational Branding, A Strategic Tool for Engineering Customer Satisfaction in Service Industry: A Study of Selected Banks

Effective brand strategies cannot be developed without the customers in mind, hence the need to examine how brand strategies affect the behaviours of these customers to yield a good result. The objective of this study is to evaluate the impact of organisational branding on the levels of customer patronage. A descriptive and survey design was adopted for the study. The population for this study consist of customers from Wema and Zenith bank within Lagos metropolis. The questionnaire was used in eliciting information from respondents, which contained two sections. Two research questions and hypotheses were raised and tested. The data collected was analysed using Statistical Package for Social Sciences (SPSS version 20.0), for frequency distribution. Further analysis was carried out using linear regression and correlation analysis. From the findings made in the study, there is a significant role played by brand identity in meeting customer expectation and there is a significant effect of brand culture on customer satisfaction. It was recommended that management should be conscious of their peculiar corporate identity once established in order to capitalize on their strengths and opportunities, as well as improve on their weaknesses and address their threats in good time and Managers should strive to create a peculiar brand culture in line with their given brand identity, as the creation of a strong brand culture will enable the staff of the organisation to deliver quality service for good customer satisfaction

Synthesis, characterization, and biological evaluation of some metal complexes containing N and S donor atoms

Eight new bipyridine adducts of Zn(II) and Ni(II) dithiocarbamate complexes have been prepared from the reaction of Zn(II) and Ni(II) complexes of N-ethyl-N-phenyldithiocarbamate and 4,4′ dipyridine, 4,4′-dimethyl-2,2′-bipyridine, 4,4′-dimethoxy-2,2′-bipyridine, 4,4′-ditertbutyl-2,2′-bipyridine. The resulting adducts were represented as [M(L1)2(DP)], [M(L1)2(DMeB)], [M(L1)2(DMxB)] and [M(L1)2(DTB)] respectively (where M = Zn or Ni). The structural configuration of these adducts was established using various spectroscopic techniques. The obtained data from the spectroscopic studies revealed a change in the tetrahedral configuration of the parent complexes to octahedral coordination in the adducts due to an additional metal-nitrogen bond. The formation of this bond was established by a considerable shift in the peaks around the metal-nitrogen (M−N) coordination upon the formation of the adducts. The study of biological properties including cytotoxicity, antioxidant, and anti-inflammatory properties were carried out. No noticeable trends were reported in all the studies despite the concentration-dependent profile shown in the assays and the structural similarities of the compounds. These adducts, nevertheless, showed good antioxidant activity in the DPPH assay, with IC50 ranging between 3.78 and 4.87 µg/mL which is better than the standard ascorbic acid (4.96 µg/mL). Also, in the cytotoxicity study, the adducts [Zn(L)2DMeBp] (1) and [Ni(L)2 DTBp] (6) showed the best activity against the mutating human cervical cancer (HeLa) and embryo kidney (HEK 293) cell lines and better than the standard 5-Flurouracil. The molecular docking studies further revealed that the adducts had a good binding affinity to the drug targets used for the study

Novel anti-inflammatory and analgesic agents: synthesis, molecular docking and in vivo studies

Twelve new derivatives of benzothiazole bearing benzenesulphonamide and carboxamide were synthesised and investigated for their in vivo anti-inflammatory, analgesic and ulcerogenic activities. Molecular docking showed an excellent binding interaction of the synthesised compounds with the receptors, with 17c showing the highest binding energy (–12.50 kcal/mol). Compounds 17c and 17i inhibited carrageenan-induced rat paw oedema at 72, 76, and 80% and 64, 73, and 78% at 1 h, 2 h, and 3 h, respectively. In the analgesic activity experiment, compounds 17c, 17 g, and 17i had ED50 (µM/kg) of 96, 127, and 84 after 0.5 h; 102, 134, and 72 after 1 h and 89, 156, and 69 µM/kg after 2 h, respectively, which were comparable with 156, 72, and 70 µM/kg for celecoxib. The ulcerogenic index of the most active derivatives 17c and 17i were 0.82 and 0.89, respectively, comparable to 0.92 for celecoxib. The physicochemical studies of the new derivatives showed that they will not have oral bioavailability problems

Angular Phenozaxine Ethers as Potent Multi-microbial Targets Inhibitors: Design, Synthesis, and Molecular Docking Studies

The reaction of diaza-5H-benzo[a]phenoxazin-5-one and 5H-benzo[a]phenoxazin-5-one with various phenols catalyzed by Pd/t-BuXPhos/K3PO4 system gave previously unknown ether derivatives (7a–f and 8a–f) in good yields. UV-visible, FTIR, and 1H NMR data were used to confirm structures of the synthesized compounds. The parent compounds and the derivatives were screened in-silico for their drug-likeness and binding affinities to the microbial targets through molecular docking. Molinspiration software and AutoDock were used for the drug-likeness and docking studies, respectively. All the synthesized compounds showed strong drug-likeness. They also showed excellent binding affinities with glucosamine-6-phosphate synthase (2VF5), AmpC beta-lactamase (1KE4), and Lanosterol-14α-demethylase (3JUV), with compound 7e having the highest binding energies −9.5, −9.3, and −9.3 kcal/mol, respectively. These were found to be higher than the binding energies of the standard drugs. The binding energies of ciprofloxacin with 2VF5 and 1KE4 were −7.8 and −7.5 kcal/mol, respectively, while that of ketoconazole with 3JUV was −8.6 kcal/mol. The study showed that the synthesized compounds have multi-target inhibitory effects and can be very useful in multi-drug resistance cases. A 2D quantitative structural activity relationship (QSAR) model against target Glucosamine-6-phosphate synthase (2VF5) was developed using partial least squares regression (PLS) with good internal prediction (R2 = 0.7400) and external prediction (R2_ predicted = 0.5475) via Molecular Operating Environment (2014)

A Review on the Molecular Mechanisms of Action of Natural Products in Preventing Bone Diseases

The drugs used for treating bone diseases (BDs), at present, elicit hazardous side effects that include certain types of cancers and strokes, hence the ongoing quest for the discovery of alternatives with little or no side effects. Natural products (NPs), mainly of plant origin, have shown compelling promise in the treatments of BDs, with little or no side effects. However, the paucity in knowledge of the mechanisms behind their activities on bone remodeling has remained a hindrance to NPs’ adoption. This review discusses the pathological development of some BDs, the NP-targeted components, and the actions exerted on bone remodeling signaling pathways (e.g., Receptor Activator of Nuclear Factor κ B-ligand (RANKL)/monocyte/macrophage colony-stimulating factor (M-CSF)/osteoprotegerin (OPG), mitogen-activated protein kinase (MAPK)s/c-Jun N-terminal kinase (JNK)/nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB), Kelch-like ECH-associated protein 1 (Keap-1)/nuclear factor erythroid 2–related factor 2 (Nrf2)/Heme Oxygenase-1 (HO-1), Bone Morphogenetic Protein 2 (BMP2)-Wnt/β-catenin, PhosphatidylInositol 3-Kinase (PI3K)/protein kinase B (Akt)/Glycogen Synthase Kinase 3 Beta (GSK3β), and other signaling pathways). Although majority of the studies on the osteoprotective properties of NPs against BDs were conducted ex vivo and mostly on animals, the use of NPs for treating human BDs and the prospects for future development remain promising