Bioactive compounds ofCrocus sativusL. and their semi-synthetic derivatives as promising anti-Helicobacter pylori, anti-malarial and anti-leishmanial agents

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 antibacterial 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.

Phenolic Composition and Evaluation of the Antimicrobial Activity of Free and Bound Phenolic Fractions from a Peruvian Purple Corn (Zea mays L.) Accession

“…H. pylori , is a Gram‐negative, microaerophilic bacterium which has been considered as the cause of one of the most important infections affecting the human stomach because this bacterium inhabits the inner mucosa, causing not only gastritis but also gastroduodenal ulcers and, in the more severe stages, tumors (De Monte and others ). Because of the increase in antibiotic resistance and host‐linked side effects associated to common H. pylori therapies, the investigation of naturally occurring antimicrobial compounds from food diversity could potentially be an alternative or used in synergy with drugs for preventing and treating H. pylori infection and also countering antibiotic resistance.…”

Synthesis, biological evaluation and molecular docking of N-phenyl thiosemicarbazones as urease inhibitors

“…The activtiy of semicarbanzone-based compounds against bacteria (i.e. Helicobacter pylori, Escherichia coli and Pseudomonas aeruginosa), [28,29] viral and many other pathogenic diseases is well-known. [30] Benzofurane derivatives also exhibit potent activities against many diseases induced by various microbes and enzymes.…”

Effect of propolis in gastric disorders: inhibition studies on the growth ofHelicobacter pyloriand production of its urease

“…However, the commercially available urease inhibitors, such as phosphorodiamidates, hydroxamic acid derivatives and imidazoles, are toxic and have poor stability, features that prevent their clinical use 7,8 . In addition to this, one of the reasons for the failure of H. pylori eradication in many countries is the increasing antibiotic resistance 2 . The prevalence of antibiotic-resistant H. pylori strains and the side effects associated with the present chemotherapeutic approach driven the search for alternatives to currently available anti-H. pylori drugs, especially regarding safe and effective non-antibiotic agents 9 .…”

“…Helicobacter pylori (H. pylori) is a Gram-negative, flagellated, spiral-shaped, urease-producing bacterium that grows in the digestive tract and has a tendency to attack the stomach lining 1,2 . For acid acclimation of H. pylori, two types of enzymes, urease and carbonic anhydrase (CA), play a central role.…”