Abstract
Propolis, is a gummy material produced by honey bees from different parts of plants and is enriched with varied biological active compounds like flavonoids, phenolics and phenolic acids with wide applicability in the food, pharmaceutical and cosmetics industries. The current report is focused on the characterisation of propolis collected from Asir region, South-west of Saudi Arabia and its effect on Trypanosoma brucei (the causative organism of African sleeping sickness) and cytotoxic effect against U937 human leukemia cells. The Chemical composition and spectral characteristics of Saudi propolis was studied by Liquid Chromatography Mass Spectrometry (LC–MS) and High-performance liquid chromatography–evaporative light scattering detector (HPLC–ELSD).The two main active compounds isolated from Saudi propolis via column chromatography and size exclusion chromatography were fisetinidol and ferulic acid. High resolution electrospray ionization–mass spectrophotometer (HRESI–MS) and nuclear magnetic resonance (NMR) were used to elucidate the structures of the isolated compounds. All crudes extracts, fractions as well as isolated compounds were subjected for biological testing against Trypanosoma brucei (S427 WT), and their cytotoxicity against U937 human leukemia cells. Amongst the various samples investigated, S-6 fraction demonstrated highest anti-trypanosomal activity at 2.4 µg/ml MIC followed by fisetinidol at 4.7 µg/ml reflecting that the anti-trypanosomal activity is attributable to the presence of fisetinidol in the fraction. Similarly, all the tested samples exhibited cytotoxicity with an IC50 > 60 µg/ml. S-6 fractions exhibited highest cytotoxic activity against U937 cells with an IC50 of 58.7 µg/ml followed by ferulic acid with an IC50 87.7 µg/ml indicating that the cytotoxic effect of propolis might be due to the presence of ferulic acid. In conclusion, the biological activity of propolis could be attributed to the synergistic action of the two active compounds-ferulic acid and fisetinidol. The data obtained in the study is thus indicative of the role of propolis as potential anti-trypanosomal and anticancer agent for effective cancer therapy.
Highlights
Propolis, is a gummy material produced by honey bees from different parts of plants and is enriched with varied biological active compounds like flavonoids, phenolics and phenolic acids with wide applicability in the food, pharmaceutical and cosmetics industries
The chromatograms of the crude samples run on HPLC–UV–ELSD (Fig. 1b) show a wide diversity in the chemical composition of propolis samples from Saudi Arabia
The present study demonstrated the anti-trypanosomal and anticancer properties of various propolis extracts crude and pure fractions, and the highest activity was found in the S-6 fractions
Summary
Propolis, is a gummy material produced by honey bees from different parts of plants and is enriched with varied biological active compounds like flavonoids, phenolics and phenolic acids with wide applicability in the food, pharmaceutical and cosmetics industries. S-6 fractions exhibited highest cytotoxic activity against U937 cells with an IC50 of 58.7 μg/ml followed by ferulic acid with an IC50 87.7 μg/ml indicating that the cytotoxic effect of propolis might be due to the presence of ferulic acid. Ethanol is mostly used to obtain low wax propolis extracts rich in biologically active compounds. Data on the anticancer and anti-trypanosomal activity of Saudi propolis is scarce. In view of the above, the present study was undertaken to chemically characterize the compounds in Saudi propolis and evaluate its anti-trypanosomal and anticancer properties
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