Antiplasmodial Activity of ß-Ionone and the Effect of the Compound on Amelioration of Anaemia and Oxidative Organ Damage in Mice Infected with Plasmodium berghei.

INTRODUCTION: Owing to evolution of parasite strains that are resistant to existing antimalarial drugs, research for novel antimalarial medicines is progressing on numerous fronts. PURPOSE: Herein, we evaluated the in vivo anti-Plasmodium berghei activity of ß-ionone including its ameliorative potential towards P. berghei-associated anaemia and oxidative organ damage. METHODS: Mice were infected with chloroquine-sensitive strain of P. berghei and then treated with ß-ionone at doses of 10 and 20 mg/kg body weight (BW) for seven days. The parasitemia, packed cell volume and redox sensitive biomarkers in the liver, brain and spleen were estimated. RESULTS: Our result showed that ß-ionone, in a dose-dependent fashion, significantly (p < 0.05) repressed the multiplication of P. berghei. More so, the compound, at doses of 10 and 20 mg/kg BW, significantly (p < 0.05) mitigated anaemia and organ damage induced by P. berghei. CONCLUSION: Overall, the findings demonstrated that ß-ionone has antiplasmodial actions and plays a mitigative role against P. berghei-induced anaemia and oxidative organ damage.

Boswellia Essential Oil: Natural Antioxidant as an Effective Antimicrobial and Anti-Inflammatory Agent.

The research aimed to determine the chemical composition, the antioxidant and anti-inflammatory activity as well as the antimicrobial activity against Gram-positive, Gram-negative and two fungal Candida ATCC strains of a commercial Boswellia essential oil (BEO) containing Boswellia carteri, Boswellia sacra, Boswellia papryfera, and Boswellia frereana. Additionally, molecular docking was carried out to show the molecular dynamics of the compounds identified from the essential oil against three bacterial protein targets and one fungal protein target. The major components identified by GC-MS (Gas Chromatography-Mass Spectrometry) were represented by α-pinene, followed by limonene. Evaluation of antioxidant activity using the DPPH (2,2-Diphenyl-1-Picrylhydrazyl) method showed high inhibition comparable to the synthetic antioxidant used as a control. Oxidative stability evaluation showed that BEO has the potential to inhibit primary and secondary oxidation products with almost the same efficacy as butylated hydroxyanisole (BHA). The use of BEO at a concentration of 500 ppm provided the best protection against secondary oxidation during 30 days of storage at room temperature, which was also evident in the peroxide value. Regarding the in vitro anti-inflammatory activity, the membrane lysis assay and the protein denaturation test revealed that even if the value of protection was lower than the value registered in the case of dexamethasone, the recommendation of using BEO as a protective agent stands, considering the lower side effects. Gram-positive bacteria proved more sensitive, while Pseudomonas aeruginosa presented different sensitivity, with higher MICs (minimal inhibitory concentration). Haemophilus influenzae demonstrated a MIC at 2% but with consecutive inhibitory values in a negative correlation with the increase in concentration, in contrast to E. coli, which demonstrated low inhibitory rates at high concentrations of BEO. The computational tools employed revealed interesting binding energies with compounds having low abundance. The interaction of these compounds and the proteins (tyrosyl-tRNA synthetase, DNA gyrase, peptide deformylase, 1,3-ß-glucan synthase) predicts hydrogen bonds with amino acid residues, which are reported in the active sites of the proteins. Even so, compounds with low abundance in BEO could render the desired bioactive properties to the overall function of the oil sustained by physical factors such as storage and temperature. Interestingly, the findings from this study demonstrated the antioxidant and antimicrobial potential of Boswellia essential oil against food-related pathogens, thus making the oil a good candidate for usage in food, feed or food-safety-related products.

Therapeutic activity of eugenol towards mitigation of anaemia and oxidative organ damage caused by Plasmodium berghei.

The parasite responsible for causing malaria infection, Plasmodium, is known to exhibit resistance to a number of already available treatments. This has prompted the continue search for new antimalarial drugs ranging from medicinal plant parts to synthetic compounds. In lieu of this, the mitigative action of the bioactive compound, eugenol towards P. berghei-induced anaemia and oxidative organ damage was investigated following a demonstration of in vitro and in vivo antiplasmodial effects. Mice were infected with chloroquine-sensitive strain of P. berghei and thereafter treated with eugenol at doses of 10 and 20 mg/kg body weight (BW) for seven days. The packed cell volume and redox sensitive biomarkers in the liver, brain and spleen were measured. Our result demonstrated that eugenol significantly (p < 0.05) ameliorated the P. berghei-associated anaemia at a dose of 10 mg/kg BW. In addition, the compound, at a dose of 10 mg/kg BW, significantly (p < 0.05) alleviated the P. berghei-induced organ damage. This evidently confirmed that eugenol plays an ameliorative role towards P. berghei-related pathological alterations. Hence, the study opens up a new therapeutic use of eugenol against plasmodium parasite.

Molecular study of rabies virus in slaughtered dogs in Billiri and Kaltungo local government areas of Gombe state, Nigeria.

Rabies is one of the most dreadful diseases and a major viral zoonosis which has been shown to cause an almost 100% fatality rate in infected victims. It is characterized by acute progressive encephalitis in mammals. This study determined the genotypic characteristics of rabies virus in dogs slaughtered for human consumption based on sequence of a fragment of nucleoprotein gene. Brain tissues were collected from 50 dogs slaughtered in Billiri and Kaltungo Local Government Areas of Gombe State, Nigeria. Direct fluorescent antibody test (DFAT) was used to screen for the presence of rabies virus antigen. Viral RNA isolated from DFAT positive brain tissues were subjected to the reverse transcription polymerase chain reaction (RT-PCR) followed by sequencing of the amplicons. Maximum Likelihood (ML) was used to construct a phylogenetic tree for sequences obtained with 1000 bootstrap replicates. The DFAT detected rabies antigen in 3 (6%) of the 50 dog brain tissues, from which 1 (2%) was positive by RT-PCR. ML phylogeny approach of the nucleotide sequences inferred members as originating lyssavirus genus and dog species. Essentially, MK234794 in this study displayed 99.3% sequence similarity with other related rabies viruses in the Africa 2 cluster (Nigeria, Cameroon, Chad and Niger). Interestingly, MK234794 showed no cluster relation with the Africa 1a, 1b, 3 and Africa 4 clades, respectively. This indicates there is in-country and trans-boundary circulation of the rabies viruses with no co-circulation between the Africa lineages, especially as dogs are continuously being traded due to consumption of dog meat in West Africa. This finding has given additional insight into the molecular epidemiology of rabies virus in Nigeria, therefore providing more baseline information for future design of rabies control programs in the country.

The chemotherapeutic potential of chalcones against leishmaniases: a review.

Leishmaniases are endemic diseases in tropical and sub-tropical regions of the world and are considered by the World Health Organization (WHO) to be among the six most important neglected tropical diseases. The current therapeutic arsenal against the disease is associated with a series of chemotherapeutic setbacks. However, since the early 1990s, naturally occurring chalcones with promising antileishmanial effects have been reported, and several other synthetic chalcones and chalcone-hybrid molecules have been confirmed to possess potent activity against various Leishmania species. This paper is a comprehensive review covering the antileishmanial activity of 34 naturally occurring chalcones, 224 synthetic/semisynthetic chalcones and 54 chalcone-hybrid molecules. Several chalcones in the synthetic/semisynthetic category had IC50 values < 5 µM, with very good selectivity against parasites, and the structure-activity relationships as well as the proposed mechanism of action are discussed. We identified knowledge-gaps with the hope of providing future direction for the discovery of novel antileishmanial drugs from chalcones.