7 research outputs found
Identification of new lead compounds for the treatment of African trypanosomiasis
No abstract available
Chemical and antimicrobial profiling of propolis from different regions within Libya.
Extracts from twelve samples of propolis collected from different regions of Libya were tested for their activity against Trypanosoma brucei, Leishmania donovani, Plasmodium falciparum, Crithidia fasciculata and Mycobacterium marinum and the cytotoxicity of the extracts was tested against mammalian cells. All the extracts were active to some degree against all of the protozoa and the mycobacterium, exhibiting a range of EC50 values between 1.65 and 53.6 μg/ml. The toxicity against mammalian cell lines was only moderate; the most active extract against the protozoan species, P2, displayed an IC50 value of 53.2 μg/ml. The extracts were profiled by using liquid chromatography coupled to high resolution mass spectrometry. The data sets were extracted using m/z Mine and the accurate masses of the features extracted were searched against the Dictionary of Natural Products (DNP). A principal component analysis (PCA) model was constructed which, in combination with hierarchical cluster analysis (HCA), divided the samples into five groups. The outlying groups had different sets of dominant compounds in the extracts, which could be characterised by their elemental composition. Orthogonal partial least squares (OPLS) analysis was used to link the activity of each extract against the different micro-organisms to particular components in the extracts
PCA with HCA based on the 300 most intense features obtained in negative ion mode for the 12 propolis samples R<sup>2</sup>X 0.689, Q<sup>2</sup> 0.48.
<p>PCA with HCA based on the 300 most intense features obtained in negative ion mode for the 12 propolis samples R<sup>2</sup>X 0.689, Q<sup>2</sup> 0.48.</p
OPLS plot of observed against predicted activity against <i>P</i>. <i>falciparum</i> based on five compounds (A-E).
<p>OPLS plot of observed against predicted activity against <i>P</i>. <i>falciparum</i> based on five compounds (A-E).</p
Activity of samples P1-P12 against <i>P</i>.<i>falciparum</i> (n = 3).
<p>Activity of samples P1-P12 against <i>P</i>.<i>falciparum</i> (n = 3).</p
Libyan map showing the collection points Libyan Propolis samples P1 (Alagoria), P2 (Gaminis), P3 (Byda), P4 (Quba), P5,P6, P7 (Kufra), P8(Ghadames), P9 (Tripoli), P10 (Khasr Khiar), P11, P12 (Khumas).
<p>Libyan map showing the collection points Libyan Propolis samples P1 (Alagoria), P2 (Gaminis), P3 (Byda), P4 (Quba), P5,P6, P7 (Kufra), P8(Ghadames), P9 (Tripoli), P10 (Khasr Khiar), P11, P12 (Khumas).</p
Most important variables determining the activity of P2 in anti-protozoal and anti-microbial tests and important variables determining cellular toxicity based on sample P8 which was the most cytotoxic sample.
<p>Most important variables determining the activity of P2 in anti-protozoal and anti-microbial tests and important variables determining cellular toxicity based on sample P8 which was the most cytotoxic sample.</p