Journal of Enzyme Inhibition and Medicinal Chemistry 2015-12-01

Bioactive compounds of Crocus sativus L. and their semi-synthetic derivatives as promising anti-Helicobacter pylori, anti-malarial and anti-leishmanial agents.

Celeste De Monte, Bruna Bizzarri, Maria Concetta Gidaro, Simone Carradori, Adriano Mollica, Grazia Luisi, Arianna Granese, Stefano Alcaro, Giosuè Costa, Nicoletta Basilico, Silvia Parapini, Maria Maddalena Scaltrito, Carla Masia, Francesca Sisto

Index: J. Enzyme Inhib. Med. Chem. 30 , 1027-33, (2015)

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Abstract

Crocus sativus L. is known in herbal medicine for the various pharmacological effects of its components, but no data are found in literature about its biological properties toward Helicobacter pylori, Plasmodium spp. and Leishmania spp. In this work, the potential anti-bacterial and anti-parasitic effects of crocin and safranal, two important bioactive components in C. sativus, were explored, and also some semi-synthetic derivatives of safranal were tested in order to establish which modifications in the chemical structure could improve the biological activity. According to our promising results, we virtually screened our compounds by means of molecular modeling studies against the main H. pylori enzymes in order to unravel their putative mechanism of action.