Environmental assessment of PAHs through honey bee colonies - A matrix selection study.

The steady conditions of temperature, humidity and air flux within beehives make them a valuable location for conducting environmental monitoring of pollutants such as PAHs. In this context, the selection of an appropriate apicultural matrix plays a key role in these monitoring studies, as it maximizes the information that will be obtained in the analyses while minimizing the inaccurate results. In the present study, three apicultural matrices (honey bees, pollen and propolis) and two passive samplers (APIStrips and silicone wristbands) are compared in terms of the number and total load of PAHs detected in them. Samplings took place in a total of 11 apiaries scattered in Austria, Denmark, and Greece, with analyses performed by GC-MS/MS. Up to 14 different PAHs were identified in silicone wristbands and pollen, whereas the remaining matrices contained a maximum of five contaminants. Naphthalene, 1-methylnaphthalene, 2-methylnaphthalene, and pyrene were found to be the most prevalent substances in the environment. Recovery studies were also performed; these suggested that the chemical structure of APIStrips is likely to produce very strong interactions with PAHs, thus hindering the adequate desorption of these substances from their surface. Overall, silicone wristbands placed inside the beehives proved the most suitable matrix for PAH monitoring through honey bee colonies.

Polyphenolic Composition of Rosa canina, Rosa sempervivens and Pyrocantha coccinea Extracts and Assessment of Their Antioxidant Activity in Human Endothelial Cells.

The aim of the present study was the investigation of the antioxidant activity of plant extracts from Rosa canina, Rosa sempervivens and Pyrocantha coccinea. The results showed that the bioactive compounds found at higher concentrations were in the R. canina extract: hyperoside, astragalin, rutin, (+)-catechin and (-)-epicatechin; in the R. sempervirens extract: quinic acid, (+)-catechin, (-)-epicatechin, astragalin and hyperoside; and in the P. coccinea extract: hyperoside, rutin, (-)-epicatechin, (+)-catechin, astragalin, vanillin, syringic acid and chlorogenic acid. The total polyphenolic content was 290.00, 267.67 and 226.93 mg Gallic Acid Equivalent (GAE)/g dw, and the total flavonoid content 118.56, 65.78 and 99.16 mg Catechin Equivalent (CE)/g dw for R. caninna, R. sempervirens and P. coccinea extracts, respectively. The extracts exhibited radical scavenging activity in DPPH and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS)•⁺ assays and protection from ROO•-induced DNA damage in the following potency order: R. canina > R. sempervirens > P. coccinea. Finally, treatment with R. canina and P. coccinea extract significantly increased the levels of the antioxidant molecule glutathione, while R. canina extract significantly decreased Reactive Oxygen Species (ROS) in endothelial cells. The results herein indicated that the R. canina extract in particular may be used for developing food supplements or biofunctional foods for the prevention of oxidative stress-induced pathological conditions of endothelium.

Novel Carbonyl Analogs of Tamoxifen: Design, Synthesis, and Biological Evaluation.

Aim of this work was to provide tamoxifen analogs with enhanced estrogen receptor (ER) binding affinity. Hence, several derivatives were prepared using an efficient triarylethylenes synthetic protocol. The novel compounds bioactivity was evaluated through the determination of their receptor binding affinity and their agonist/antagonist activity against breast cancer tissue using a MCF-7 cell-based assay. Phenyl esters 6a,b and 8a,b exhibited binding affinity to both ERα and ERß higher than 4-hydroxytamoxifen while compounds 13 and 14 have shown cellular antiestrogenic activity similar to 4-hydroxytamoxifen and the known ER inhibitor ICI182,780. Theoretical calculations and molecular modeling were applied to investigate, support and explain the biological profile of the new compounds. The relevant data indicated an agreement between calculations and demonstrated biological activity allowing to extract useful structure-activity relationships. Results herein underline that modifications of tamoxifen structure still provide molecules with substantial activity, as portrayed in the inhibition of MCF-7 cells proliferation.

Pyrazoles as potential anti-angiogenesis agents: a contemporary overview.

Angiogenesis is a mulit-step process by which new blood vessels are formed from preexisting vasculature. It is a key rate limiting factor in tumor growth since new blood vessels are necessary to increase tumor size. In this context it has been shown that anti-angiogenic factors can be used in cancer therapy. Among the plethora of heterocyclic compounds administered as anti-angiogenesis agents, pyrazoles constitute one of the bottlenecks of this category. Currently, several pyrazole based compounds are administered or are in Phase II and III trials and new targets emerge. It is highly possible that the advent of the next two decades will lead to the discovery and use of additional pyrazoles whose anti-angiogenic profile will position them in the forefront of the battle of various malignancies. The present review is an attempt to focus on those pyrazoles that arise as anti-angiogenesis agents commenting both on the chemistry and bioactivity that these exhibit aiming to contribute to the perspectives that they hold for future research.

Synthesis of (R)-dihydropyridones as key intermediates for an efficient access to piperidine alkaloids.

The efficient transformation of D-glucal to (2R)-hydroxymethyldihydropyridinone 5 in seven steps and 35 % overall yield is reported. Dihydropyridone 5 constitutes a versatile chiral building block for the synthesis of various piperidine alkaloids. In this regard, 5 was converted to piperidinol 13 and piperidinone 15, that may be further elaborated for the syntheses of (+)-desoxoprosophylline (1) and deoxymannojirimycin (3) or D-mannolactam (4), respectively.