5 research outputs found
The cardiovascular protective effects of rooibos (Aspalathus linearis) extract on diesel exhaust particles induced inflammation and oxidative stress involve NF-κB- and Nrf2-dependent pathways modulation
Studies have shown that diesel exhaust particles (DEP) induced oxidative stress and inflammation. This present study examined the molecular effects of aqueous rooibos extract (RE) on the cardiovascular toxic effect of methanol extract of DEP in exposed Wistar rats. The results showed that DEP caused significant (p < 0.001) increase in MDA and CDs levels in the aorta and heart but this increase was significantly (p < 0.001) attenuated by rooibos extract. DEP induced IL-8, TNFα, IL-1β and decreased IL-10 gene expressions, all of which were reversed in the presence of rooibos extract. The expression of NF-κB, and IκKB genes were also significantly (p < 0.001) induced by DEP in both tissues, but pre-treatment with RE attenuated these effects. In contrast, DEP repressed IκB mRNA level, which was significantly (p < 0.001) reversed by rooibos extract pre-treatment. In addition, pre-treatment with rooibos extract attenuated the increased Nrf2 and HO-1 mRNA levels caused by DEP. This indicates the potential of rooibos extract to protect against DEP-induced cardiovascular toxicity
Molecular docking and pharmacokinetic studies of phytocompounds from Nigerian Medicinal Plants as promising inhibitory agents against SARS-CoV-2 methyltransferase (nsp16)
Abstract Background Since the index case was reported in China, COVID-19 has led to the death of at least 4 million people globally. Although there are some vaccine cocktails in circulation, the emergence of more virulent variants of SARS-CoV-2 may make the eradication of COVID-19 more difficult. Nsp16 is an S-adenosyl-L-Methionine-dependent methyltransferase that plays an important role in SARS-CoV-2 viral RNA cap formation—a crucial process that confers viral stability and prevents virus detection by cell innate immunity mechanisms. This unique property makes nsp16 a promising molecular target for COVID-19 drug design. Thus, this study aimed to identify potent phytocompounds that can effectively inhibit SARS-CoV-2 nsp16. We performed in silico pharmacokinetic screening and molecular docking studies using 100 phytocompounds—isolated from fourteen Nigerian plants—as ligands and nsp16 (PDB: 6YZ1) as the target. Results We found that only 59 phytocompounds passed the drug-likeness analysis test. However, after the docking analysis, only six phytocompounds (oxopowelline, andrographolide, deacetylbowdensine, 11, 12-dimethyl sageone, sageone, and quercetin) isolated from four Nigerian plants (Crinum jagus, Andrographis paniculata, Sage plants (Salvia officinalis L.), and Anacardium occidentale) showed good binding affinity with nsp16 at its active site with docking score ranging from − 7.9 to − 8.4 kcal/mol. Conclusions Our findings suggest that the six phytocompounds could serve as therapeutic agents to prevent viral survival and replication in cells. However, further studies on the in vitro and in vivo inhibitory activities of these 6 hit phytocompounds against SARS-CoV-2 nsp16 are needed to confirm their efficacy and dose
Comparative research performance of top universities from the northeastern Brazil on three pharmacological disciplines as seen in scopus database
Objectives: Postgraduate programmes around the world are periodically subjected to research performance evaluation through bibliometric indicators. In this research, we characterized and compared the research performance of 15 universities from Northeastern Brazil, in which 13 were among the top Universities of the Latin America. Methods: Specifically, total documents, citations and the h-index of each university were retrieved from the Elsevier Scopus database and were analysed not only for historical scientific achievement but also across the period of the past 6 years (2010â2015). Using these bibliometric indicators, we also investigated the performance of programmes at these Universities that have their papers indexed in the Scopus database under the category of âPharmacology, Toxicology and Pharmaceuticalsâ for the same period. Results: We found that the Federal University of Pernambuco (UFPE) and the Federal University of Ceará (UFC) were the most productive institutions, producing 17847 and 15048 documents, respectively. The number of papers published by each of these universities in the past six years represented more than 50% of their entire productivity. With regards to their scientific output in âPharmacology, Toxicology and Pharmaceuticsâ, UFC showed the highest number of published documents followed by UFPE and the Federal University of ParaÃÂba (UFPB). UFC received the highest h-index (with and without self-citations) and number of citations and shared their most cited papers with foreign institutions from the USA and Germany. However, papers from UFC were published in journals with lower impact factors (2.322). Conclusions: The present study shows where each of these universities stands and can be helpful in identifying potential collaborators in these areas of knowledge. Keywords: Citations, CNPq, h-index, Northeastern Brazil, UF