Aspidosperma pyrifolium, a medicinal plant from the Brazilian caatinga, displays a high antiplasmodial activity and low cytotoxicity

Abstract Background Several species of Aspidosperma plants are referred to as remedies for the treatment of malaria, especially Aspidosperma nitidum. Aspidosperma pyrifolium, also a medicinal plant, is used as a natural anti-inflammatory. Its fractionated extracts were assayed in vitro for activity against malaria parasites and for cytotoxicity. Methods Aspidosperma pyrifolium activity was evaluated against Plasmodium falciparum using extracts in vitro. Toxicity towards human hepatoma cells, monkey kidney cells or human monocytes freshly isolated from peripheral blood was also assessed. Anti-malarial activity of selected extracts and fractions that presented in vitro activity were tested in mice with a Plasmodium berghei blood-induced infection. Results The crude stem bark extract and the alkaloid-rich and ethyl acetate fractions from stem extract showed in vitro activity. None of the crude extracts or fractions was cytotoxic to normal monkey kidney and to a human hepatoma cell lines, or human peripheral blood mononuclear cells; the MDL50 values of all the crude bark extracts and fractions were similar or better when tested on normal cells, with the exception of organic and alkaloidic-rich fractions from stem extract. Two extracts and two fractions tested in vivo caused a significant reduction of P. berghei parasitaemia in experimentally infected mice. Conclusion Considering the high therapeutic index of the alkaloidic-rich fraction from stem extract of A. pyrifolium, it makes the species a candidate for further investigation aiming to produce a new anti-malarial, especially considering that the active extract has no toxicity, i.e., no mutagenic effects in the genototoxicity assays, and that it has an in vivo anti-malarial effect. In its UPLC-HRMS analysis this fraction was shown to have two major components compatible with the bisindole alkaloid Leucoridine B, and a novel compound, which is likely to be responsible for the activity against malaria parasites demonstrated in in vitro tests

VO₂FITTING:A Free and Open-Source Software for Modelling Oxygen Uptake Kinetics in Swimming and other Exercise Modalities

The assessment of oxygen uptake (VO2) kinetics is a valuable non-invasive way to evaluate cardiorespiratory and metabolic response to exercise. The aim of the study was to develop, describe and evaluate an online VO2 fitting tool (VO2FITTING) for dynamically editing, processing, filtering and modelling VO2 responses to exercise. VO2FITTING was developed in Shiny, a web application framework for R language. Validation VO2 datasets with both noisy and non-noisy data were developed and applied to widely-used models (n = 7) for describing different intensity transitions to verify concurrent validity. Subsequently, we then conducted an experiment with age-group swimmers as an example, illustrating how VO2FITTING can be used to model VO2 kinetics. Perfect fits were observed, and parameter estimates perfectly matched the known inputted values for all available models (standard error = 0; p < 0.001). The VO2FITTING is a valid, free and open-source software for characterizing VO2 kinetics in exercise, which was developed to help the research and performance analysis communities