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This work describes the use of Colubrina greggii as a model to investigate the use of chemometric analysis combined with data from a leishmanicidal bioassay, using Principal Component Analysis (PCA) and Orthogonal Projections to Latent Structures (O-PLS), to detect biologically active natural products in crude extracts from plants having little or no phytochemical information. A first analysis of the HPLC-UV profiles of the extract and its semi-purified fractions using both Principal Component Analysis (PCA) and Orthogonal Partial Least Squares (O-PLS) indicated that the components at tR 48.2, 48.7, 51.8min correlated with the variation in bioactivity. However, a further O-PLS analysis of the HPLC-UV profiles of fractions obtained through a final semi-preparative HPLC purification showed two components at tR 48.7 and 49.5min which correlated with the variation of the bioactivity in a high performance predictive model, with high determination coefficient, high correlation coefficient values (R(2) and Q(2)=0.99) and a low root mean square error (RMSE=0.018). This study demonstrates that the association of chemometric analysis with bioassay results can be an excellent strategy for the detection and isolation of bioactive metabolites from phytochemically unknown plant crude extracts., (Copyright © 2015. Published by Elsevier B.V.)

Betulinic acid (1), isolated from the crude extract of the leaves of Pentalinon andrieuxii (Apocynaceae), together with betulinic acid acetate (2), betulonic acid (3), betulinic acid methyl ester (4), and betulin (5) were evaluated for their antiprotozoal activity. The results showed that modifying the C-3 position increases leishmanicidal activity while modification of the C-3 and C-28 positions decreases trypanocidal activity., (Copyright 2009 Elsevier GmbH. All rights reserved.)

Aqueous and organic extracts of twenty-seven species of marine algae (14 species of Rhodophyta, 5 species of Phaeophyta and 8 species of Chlorophyta) collected from the Gulf of Mexico and Caribbean coast of the Yucatan Peninsula (Mexico) were evaluated for their antileishmanial in vitro activity against Leishmania mexicana promastigote forms. The cytotoxicity of these extracts was also assessed using brine shrimp. Organic extracts from Laurencia microcladia (Rhodophyta), Dictyota caribaea, Turbinaria turbinata and Lobophora variegata (Phaeophyta) possessed promising in vitro activity against L. mexicana promastigotes (LC(50) values ranging from 10.9 to 49.9 microg/ml). No toxicity of algal extracts against Artemia salina was observed with LC50 ranging from 119 to >or=1000 microg/ml. Further studies on bio-guided fractionation, isolation and characterization of pure compounds from these species as well as in vivo experiments are needed and are already in progress.