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Type 2 diabetes mellitus (T2DM) is an important metabolic disorder for which there is an urgent need for new antidiabetic drugs. α-Glucosidase inhibition is an established protocol for T2DM therapy. Because hyperglycemia causes oxidative tissue damage, the development of agents with both α-glucosidase inhibition and antioxidant activity from natural or natural-derived polyphenols such derivatives of rosmarinic acid (RA) represents an attractive therapeutic option. We report a study on amides 1-10 derived from RA and their evaluation for yeast α-glucosidase inhibition and antioxidant activity (DPPH and ORAC tests). All amides showed higher inhibitory activity than that of RA, were by far more potent than the antidiabetic drug acarbose, and proved to be effective antioxidants. A molecular docking study displayed significant binding interactions of RA amides with the active site of α-glucosidase. This in silico optimization study led to the design and synthesis of amides 9 (IC 50 = 42.3 μM) and 10 (IC 50 = 35.2 μM), showing the most potent α-glucosidase inhibition and good antioxidative properties. A kinetic study showed that 10 acts as a mixed type inhibitor.

In the present study the chemical composition of the essential oils from aerial parts of Centaurea tomentella Hand.-Mazz. and C. haussknechtii Boiss. collected in Turkey was evaluated by GC and GC-MS. The main components of C. tomentella L. were hexadecanoic acid (19.7%), caryophyllene oxide (6.6%) and spathulenol (4.8%) whereas C. haussknechtii was rich in hexadecanoic acid (26.2%), (Z,Z)-9,12-octadecadienoic acid (19.3%), heptacosane (5.3%) and nonacosane (5.1%). Antibacterial and antifungal activities against some microorganisms infesting historical art craft, were also determined.

Pancratium maritimumstems, flowers, bulbs, and fruits extracts were investigated for their antiproliferative and antioxidant properties. Total phenols and total flavonoids were also determined. Thein vitroantiproliferative activity was tested against seven cancer cell lines such as C32, HeLa, MDA-MB-231, PC3, A549, MCF-7, and LNCaP by using SRB assay. Interesting results were obtained with stems ethanol extract (ET1) against C32 cells (IC50of 27.1μg/mL) and fruits aqueous extract (AQ) against MCF-7 cell line (IC50of 36.5μg/mL). To define the antioxidant activity, four tests such as DPPH, ABTS FRAP, andβ-carotene bleaching tests were used.The most promising ABTS scavenging capacity was observed with fruits ethanol extract (ET1) that showed an IC50value of 6.9μg/mL. According to the correlation results, the phenols and flavonoids content could provide a fundamental contribution to the antioxidant and antiproliferative activity ofP. maritimumextracts.

Tropane alkaloids are molecules with a strong biological activity, which are mainly produced by the members offamily Solanaceae, but also found inother plant families (Convolvulaceae, Brasicaceae, Erythroxylaceae andEuphorbiaceae).1 More than 20 active pharmaceutical substances containingthetropane moiety have been industrially produced and applied as mydriatics, antiemetics, antispasmodics, anesthetics and bronchodilators.Nearly all of them are based on the Scopolamine structure.2 In recent years, several researchers aimed their work to the use of supramolecular systems for the inclusion of organic species, such as complex systems based on cyclodextrines or calixarenes.3They have attracted increasing interest during the past years, due to their adsorption or controlled release abilities towards various organic molecules. An interesting new class of material is calixarene-cyclodextrinenanosponges, which consists of a polymeric network of host co-monomer units crosslinked by triazole units and exhibiting cavities and nanopores in the range of nanometers. The present research work was designed to produce many derivatives of scopolamine, keeping in view their biological activity and comparing them with current tropane pharmaceuticals. Moreover, the research aims to study pharmacokinetics of these derivatives with functionalized calixarene-cyclodextrine polymers as promising drug carriers.