Bilberries as valuable sources of polyphenols with health-promoting properties

Subject of research: Vaccinium uliginosum L. (swamp blueberry) and Vaccinium myrtillus L. (black blueberry) are species of the Vaccinium genus belonging to the Ericaceae family. The fruits of these plants are characterized by a high content of biologically active polyphenols, in particular anthocyanins. These chemical compounds are responsible for the therapeutic potential of the berries and their red-purple-blue coloration. Anthocyanins from blueberries have been shown in studies to have strong antioxidant properties as well as biological potential that can be used in the prevention of cancer and lifestyle diseases. There are also studies indicating the antibacterial activity of polyphenols found in berries. Bilberry berries are used to produce jams and juices commonly available in Europe. These products may constitute a valuable source of polyphenols. However, it should be noted that the method of blueberry breeding and processing affects the final content of active substances in the product. Research goal: Systematizing the currently available knowledge regarding polyphenols found in the fruits of V. uliginosum and V. myrtillus. Methods: In preparation of the literature review for this work, the PubMed search engine using the MEDLINE database was used. The article includes articles from the last 20 years. Results: This study reviews the latest literature on the content and identification of anthocyanins, flavonols, flavanols and phenolic acids in black bilberry and bog bilberry. Works on the biological activity of polyphenols present in V. uliginosum and V. myrtillus, demonstrated in in vivo and in vitro tests, are also described. Polyphenols derived from berries of the Vaccinium genus may also be an active ingredient in dietary supplements designed to support the proper functioning of the eyes and blood vessels. Clinical studies confirm the benefits of using V. uliginosum and V. myrtillus supplementation while maintaining a proper diet. Conclusions: Due to their therapeutic values and rich phytochemical composition, blueberry fruit extracts and products are a potential ingredient of functional food. Such preparations could be targeted at patients at risk of metabolic (diabetes) and cancer diseases

4-Ethyl-3-(2-thienylmeth­yl)-Δ2-1,2,4-triazoline-5-thione

The title compound, C9H11N3S2, exists in the thione form in the crystal structure. The central triazole ring is almost perpendicular to the thio­phene ring which is disordered over two orientations [dihedral angles of 88.5 (7) and 85.7 (8)° for the two orientations]. The crystal structure is stabilized by strong inter­molecular N—H⋯S hydrogen bonds, forming centrosymmetric dimers, and by some weak C—H⋯S inter­actions

Cytotoxic effect and molecular docking of 4-ethoxycarbonylmethyl-1-(piperidin-4-ylcarbonyl)-thiosemicarbazide—a novel topoisomerase II inhibitor

The preliminary cytotoxic effect of 4-ethoxycarbonylmethyl-1-(piperidin-4-ylcarbonyl)-thiosemicarbazide hydrochloride (1)—a potent topoisomerase II inhibitor—was measured using a MTT assay. It was found that the compound decreased the number of viable cells in both estrogen receptor-positive MCF-7 and estrogen receptor-negative MDA-MB-231breast cancer cells, with IC(50) values of 146 ± 2 and 132 ± 2 μM, respectively. To clarify the molecular basis of the inhibitory action of 1, molecular docking studies were carried out. The results suggest that 1 targets the ATP binding pocket. [Figure: see text] ELECTRONIC SUPPLEMENTARY MATERIAL: The online version of this article (doi:10.1007/s00894-012-1679-6) contains supplementary material, which is available to authorized users

Sinteza i antimikotsko djelovanje 4-supstituiranih 3-(tiofen-2-il-metil)- Δ2-1,2,4-triazolin-5-tiona

In the reaction of hydrazide of thiophene-2-acetic acid (1) with isothiocyanates, the respective thiosemicarbazides 2a-g were obtained. Further cyclization with 2% NaOH led to formation of 4-substituted-3-(thiophene-2-yl-methyl)-delta2-1,2,4-triazoline-5-thiones (3a-g). These compounds showed promising antimycotic activity.Rekacijom hidrazida tiofen-2-octene kiseline (1) s izotiocijanatima sintetizirani su odgovarajući tiosemikarbazidi (2a-2g), a njihovom ciklizacijom u 2% NaOH 4-supstituirani 3-(tiofen-2-il-metil)-Δ2-1,2,4-triazolin-5-tioni (3a-3g). Ti spojevi su potencijalni antimikotici

Pharmacological and Structure-Activity Relationship Evaluation of 4-aryl-1-Diphenylacetyl(thio)semicarbazides

This article describes the synthesis of six 4-aryl-(thio)semicarbazides (series a and b) linked with diphenylacetyl moiety along with their pharmacological evaluation on the central nervous system in mice and computational studies, including conformational analysis and electrostatic properties. All thiosemicarbazides (series b) were found to exhibit strong antinociceptive activity in the behavioural model. Among them, compound 1-diphenylacetyl-4-(4-methylphenyl)thiosemicarbazide 1b was found to be the most potentan algesic agent, whose activity is connected with the opioid system. For compounds from series a significant anti-serotonergic effect, especially for compound 1-diphenylacetyl-4- (4-methoxyphenyl)semicarbazide 2b was observed. The computational studies strongly support the obtained results

Pharmacological and Structure-Activity Relationship Evaluation of 4-aryl-1-Diphenylacetyl(thio)semicarbazides

This article describes the synthesis of six 4-aryl-(thio)semicarbazides (series a and b) linked with diphenylacetyl moiety along with their pharmacological evaluation on the central nervous system in mice and computational studies, including conformational analysis and electrostatic properties. All thiosemicarbazides (series b) were found to exhibit strong antinociceptive activity in the behavioural model. Among them, compound 1-diphenylacetyl-4-(4-methylphenyl)thiosemicarbazide 1b was found to be the most potent analgesic agent, whose activity is connected with the opioid system. For compounds from series a significant anti-serotonergic effect, especially for compound 1-diphenylacetyl-4-(4-methoxyphenyl)semicarbazide 2b was observed. The computational studies strongly support the obtained results

Can We Improve Diosmetin Activity? The State-of-the-Art and Promising Research Directions

Diosmetin is a natural substance widely distributed in nature, with documented multidirectional biological effects. The wide spectrum of biological activity of diosmetin gives hope that derivatives of this flavonoid may also be used as drugs or dietary supplements used in many diseases. Modification of the structure may, on the one hand, lead to an increase in biological potency, new biological activity, or an increase in solubility and thus bioavailability. This is an important direction of research because the use of pure diosmetin is limited due to its low bioavailability. This work is an attempt to collect information on the possibility of modifying the structure of diosmetin and its impact on biological activity

2-{[4-(4-Bromophenyl)piperazin-1-yl)]methyl}-4-(3-chlorophenyl)-5-(4-methoxyphenyl)-2,4-dihydro-3H-1,2,4-triazole-3-thione

The novel compound 2-{[4-(4-bromophenyl)piperazin-1-yl)]methyl}-4-(3-chlorophenyl-5-(4-methoxyphenyl)-2,4-dihydro-3H-1,2,4-triazole-3-thione is obtained in good yield via a three-step protocol. The product’s structure is assigned by HRMS, IR, 1H and 13C NMR experiments