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.
Highlights
One of the most important microbial infections affecting the human stomach is due to Helicobacter pylori, a Gram-negative bacterium that inhabits the inner mucosa, causing gastritis and gastroduodenal ulcers and, in the more severe stages, tumors
With the aim of finding new natural or semi-synthetic antimicrobial drugs, we focused our attention on Crocus sativus L., that is a herbaceous perennial-cormous plant containing in the stigmas a great variety of bioactive compounds: the volatile oil safranal, a carotenoid derivative and its di-glycosidic esters, picrocrocin and still other components such as anthocyanins, flavonoids, vitamins, amino acids and proteins
Given our interest in this field25–28, we explored the potential anti-H. pylori, anti-malarial and anti-leishmanial effects of crocin [1] and safranal [2], which are two important products found in C. sativus, and tested some semi-synthetic derivatives of safranal (3–9, Scheme 1) in order to establish, with the support of computational studies, which modifications in the chemical structures could improve their biological activity to provide new leads for the development of promising antimicrobial and anti-parasitic agents
Summary
One of the most important microbial infections affecting the human stomach is due to Helicobacter pylori, a Gram-negative bacterium that inhabits the inner mucosa, causing gastritis and gastroduodenal ulcers and, in the more severe stages, tumors. Among the new strategies for the treatment of H. pylori infection, it can be mentioned the inhibition of urease, an enzyme that permits the survival of H. pylori in the harsh acidic environment of the stomach and its colonization of the gastric mucosa, by neutralization of the gastric acidity thanks to the ammonia production from host urea. Caffeic acid phenethyl ester, one of the principal components of propolis, was found to be a competitive inhibitor of H. pylori peptide deformylase (HpPDF), an enzyme that catalyzes the removal of the formyl group from the N-terminus of nascent polypeptide chains, which is essential for. Other targets for the treatment of H. pylori infection are as follows: [1] the type II dehydroquinase (DHQ2), the third enzyme of the shikimic acid pathway9; [2] glutamate racemase, which provides D-glutamate for the construction of
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