4-aminobenzoic acid (PABA), an essential nutrient for many human pathogens, but dispensable for humans, and its derivatives have exhibited various biological activities. In this study, we combined two pharmacophores using a molecular hybridization approach: this vitamin-like molecule and various aromatic aldehydes, including salicylaldehydes and 5-nitrofurfural, via imine bond in one-step reaction. Resulting Schiff bases were screened as potential antimicrobial and cytotoxic agents. The simple chemical modification of non-toxic PABA resulted in constitution of antibacterial activity including inhibition of methicillin-resistant Staphylococcus aureus (minimum inhibitory concentrations, MIC, from 15.62 µM), moderate antimycobacterial activity (MIC ≥ 62.5 µM) and potent broad-spectrum antifungal properties (MIC of ≥ 7.81 µM). Some of the Schiff bases also exhibited notable cytotoxicity for cancer HepG2 cell line (IC50 ≥ 15.0 µM). Regarding aldehyde used for the derivatization of PABA, it is possible to tune up the particular activities and obtain derivatives with promising bioactivities.

• Klíčová slova
• 4-aminobenzoic acid, Schiff bases, antibacterial activity, antifungal activity, cytotoxicity, synthesis, vitamin,
• MeSH
• antibakteriální látky chemie   farmakologie   MeSH
• buňky Hep G2 MeSH
• cytotoxiny chemie   farmakologie   MeSH
• kyselina 4-aminobenzoová chemie   farmakologie   MeSH
• kyselina listová chemie   farmakologie   MeSH
• lidé MeSH
• methicilin rezistentní Staphylococcus aureus účinky léků   růst a vývoj   MeSH
• mikrobiální testy citlivosti MeSH
• viabilita buněk účinky léků   MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• Názvy látek
• antibakteriální látky MeSH
• cytotoxiny MeSH
• kyselina 4-aminobenzoová MeSH
• kyselina listová MeSH

Neurodegenerative disorders (NDD) have become the common global health burden over the last several decades. According to World Health Organization (WHO), a staggering 30 million people will be affected by Alzheimer's disease in Europe and the USA by 2050. Effective therapies in this complex field considering the multitude of symptoms associated with NDD indications, have not been found yet. Based on the results of NDD related studies, prevention appears to be the promise alternative. Antioxidative and anti-inflammatory properties are hypothesized for natural phenolics, a group of plant secondary products that may positively impact neurodegenerative diseases. In these studies, phenolic-rich extracts from less common fruit species: Blue honeysuckle (Lonicera edulis, Turcz. ex. Freyn), Saskatoon berry (Amelanchier alnifolia Nutt.), and Chinese hawthorn (Crateagus pinnatifida Bunge) were obtained and analyzed to detect neuroprotective substances content and establish a potential therapeutic value. High performance liquid chromatography with electrochemical detection was optimized and further applied on analysis of the extracts of less common fruit species. It was observed that Chinese hawthorn and Blue honeysuckle extracts are potent source of neuroprotective phenolic antioxidants. In accordance the results, it appears that the fruit or formulated products may have the potential for the prevention of neurodegenerative diseases.

• MeSH
• antioxidancia analýza   terapeutické užití   MeSH
• Crataegus chemie   MeSH
• elektrochemie přístrojové vybavení   MeSH
• kyselina 4-aminobenzoová analýza   MeSH
• kyselina gallová analýza   MeSH
• Lonicera chemie   MeSH
• neurodegenerativní nemoci farmakoterapie   prevence a kontrola   MeSH
• ovoce chemie   MeSH
• quercetin analýza   MeSH
• Rosaceae chemie   MeSH
• rutin analýza   MeSH
• vysokoúčinná kapalinová chromatografie přístrojové vybavení   metody   MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• Názvy látek
• antioxidancia MeSH
• kyselina 4-aminobenzoová MeSH
• kyselina gallová MeSH
• quercetin MeSH
• rutin MeSH