Unit:
Κατεύθυνση Φαρμακευτική ΧημείαLibrary of the School of Science
Author:
Komianou Aikaterini-Christina
Supervisors info:
Σκαλτσούνης Αλέξιος – Λέανδρος, Καθηγητής,
Παπαναστασίου Ιωάννης, Επίκουρος Καθηγητής,
Κωστάκης Ιωάννης, Επίκουρος Καθηγητής (Επιβλέπων)
Original Title:
ΣΥΝΘΕΣΗ ΑΝΑΛΟΓΩΝ ΤΗΣ ΥΔΡΟΞΥΤΥΡΟΣΟΛΗΣ ΜΕ ΑΝΤΙΜΥΚΗΤΙΑΚΗ ΔΡΑΣΗ
Translated title:
SYNTHESIS OF HYDROXYTYROSOL ANALOGUES WITH ANTIFUNGAL ACTIVITY
Summary:
Fungal infections constitute an emerging threat and a prevalent health problem due to increasing number of immunocompromised people and pharmacological or other treatments aiming at viral infections, cancer or allergies. Currently used antifungals suffer from inefficiency, toxic side effects and developing drug-resistance. Here we investigate the antifungal activity of a series of chemically synthesized Hydroxytyrosol (HT) analogues. HT is one of the major phenolic compounds in olive oil, shown to possess radical-scavenging antioxidant, antiproliferative, proapoptotic and anti-inflammatory activities. No previous report has studied HT analogues as antifungals. We analyse the chemical methods that we used for the synthesis of hydroxytyrosol analogues. We also show that specific analogues have broad and strong antifungal activity, significantly stronger than the parent compound HT. Using A. nidulans as an in vivo cellular model system, we show that antifungal HT analogues have an unprecedented efficiency in fungal plasma membrane destruction. Importantly, antifungal HT analogues did not show toxicity in a mammalian cell line, whereas no resistance to HT analogues was obtained by standard mutagenesis. Our results open the way for the development of a novel, efficient and safer class of antifungals.
Main subject category:
Science
Other subject categories:
Health Sciences
Keywords:
antifungal, hydroxytyrosol, synthesis
