A new species of Alpioniscus Bedek, Jana; Gottstein, Sanja; Taiti, Stefano
Subterranean biology,
09/2019
3
Journal Article
Peer reviewed
In the Dinaric Karst, Alpioniscus (Illyrionethes) is the taxon with the largest number of troglobiotic species (19), one of which is new and described here: A. busljetai sp. nov., found in two caves ...in the coastal area of North Dalmatia. Both caves are threatened by human activities (IUCN threats 1.1, 9.1.1). Keywords: Adriatic coast, cave fauna, new species, terrestrial isopods, Trichoniscinae , troglobiotic
4-Chloropyrazolo1,5-аpyrazines reacted with anthranilic acids forming 8Ð-pyrazolo5',1':3,4pyrazino2,1-bquinazolin-8-ones representing a new heterocyclic system.
In the context of a program to identify selective adenosine A2B receptor antagonists, we have obtained a focused library of 4-substituted 3,4-dihydropyrimidin-2(1H)-ones and its affinity for the four ...human adenosine receptor subtypes was determined. The synthesis was accomplished by using an experimentally simple and efficient Biginelli approach. The biological evaluation of the library revealed that all the documented derivatives exhibit low or negligible affinity for the A.sub.2B receptor, thus highlighting the critical importance of the substituent at position 4 of the 3,4-dihydropyrimidin-2(1H)-one chemotype.
In recent years, great attention has been paid to polyphenols due to their positive effects on health. One of the most widely-studied phenolic compounds is resveratrol. This molecule, which is ...naturally present in some foods, shows beneficial effects on various physiological and biochemical processes, thus representing a potential tool for the prevention or the treatment of diseases highly prevalent in our society. Several of these beneficial effects have been observed in human beings, but others only in pre-clinical studies so far, and therefore, it is mandatory to continue with the scientific research in this field. Indeed, new knowledge concerning these issues could enable the development of novel functional foods or nutraceuticals, incorporating resveratrol, suitable for preventing or treating diseases such as cancer, cardiovascular diseases, obesity, dislipemia, insulin resistance and diabetes, liver diseases, etc.
Synthetic approaches to 4--ones MieriÅa, Inese; Jure, Mara; Stikute, Agnese
Chemistry of heterocyclic compounds (New York, N.Y. 1965),
08/2016, Volume:
52, Issue:
8
Journal Article
Peer reviewed
This review summarizes strategies for the synthesis of 4-(het)aryl-3,4-dihydroquinolin-2(1H)-ones which are of interest due to their biological activity. It covers methods elaborated particularly for ...obtaining the title heterocycles, as well as procedures where these compounds are formed as side products. 4-Aryl-3,4-dihydroquinolin-2(1H)-one derivatives have been used for the synthesis of valuable molecules, e.g., anticancer drug tipifarnib.
3--ones: synthesis and structure Pelipko, Vasilii V; Makarenko, Sergey V; Berestovitskaya, Valentina M ...
Chemistry of heterocyclic compounds (New York, N.Y. 1965),
08/2016, Volume:
52, Issue:
8
Journal Article
Peer reviewed
Reactions of ethyl 3-nitroacrylate with o-phenylenediamine and its substituted derivatives were used for the synthesis of 3-(nitromethyl)-3,4-dihydroquinoxalin-2(1H)-ones, followed by structural ...characterization. These compounds were found to undergo elimination of nitromethane, leading to quinoxalin-2(1H)-ones.
Resveratrol (RV) is a well-known polyphenolic compound in various plants, including grape, peanut, and berry fruits, which is quite famous for its association with several health benefits such as ...anti-obesity, cardioprotective neuroprotective, antitumor, antidiabetic, antioxidants, anti-age effects, and glucose metabolism. Significantly, promising therapeutic properties have been reported in various cancer, neurodegeneration, and atherosclerosis and are regulated by several synergistic pathways that control oxidative stress, cell death, and inflammation. Similarly, RV possesses a strong anti-adipogenic effect by inhibiting fat accumulation processes and activating oxidative and lipolytic pathways, exhibiting their cardioprotective effects by inhibiting platelet aggregation. The RV also shows significant antibacterial effects against various food-borne pathogens (Listeria, Campylobacter, Staphylococcus aureus, and E. coli) by inhibiting an electron transport chain (ETC) and F0F1-ATPase, which decreases the production of cellular energy that leads to the spread of pathogens. After collecting and analyzing scientific literature, it may be concluded that RV is well tolerated and favorably affects cardiovascular, neurological, and diabetic disorders. As such, it is possible that RV can be considered the best nutritional additive and a complementary drug, especially a therapeutic candidate. Therefore, this review would increase knowledge about the blend of RV as well as inspire researchers around the world to consider RV as a pharmaceutical drug to combat future health crises against various inhumane diseases. In the future, this article will be aware of discoveries about the potential of this promising natural compound as the best nutraceuticals and therapeutic drugs in medicine.
We studied whether the function of presynaptic inhibitory cannabinoid CBsub.1 receptors on the sympathetic nerve fibres innervating resistance vessels is increased in spontaneously hypertensive rats ...(SHR) like in deoxycorticosterone (DOCA)–salt hypertension. An increase in diastolic blood pressure (DBP) was induced by electrical stimulation of the preganglionic sympathetic neurons or by phenylephrine injection in pithed SHR and normotensive Wistar–Kyoto rats (WKY). The electrically (but not the phenylephrine) induced increase in DBP was inhibited by the cannabinoid receptor agonist CP55940, similarly in both groups, and by the endocannabinoid reuptake inhibitor AM404 in SHR only. The effect of CP55940 was abolished/reduced by the CBsub.1 receptor antagonist AM251 (in both groups) and in WKY by endocannabinoid degradation blockade, i.e., the monoacylglycerol lipase (MAGL) inhibitor MJN110 and the dual fatty acid amide hydrolase (FAAH)/MAGL inhibitor JZL195 but not the FAAH inhibitor URB597. MJN110 and JZL195 tended to enhance the effect of CP55940 in SHR. In conclusion, the function of presynaptic inhibitory CBsub.1 receptors depends on the hypertension model. Although no differences occurred between SHR and WKY under basal experimental conditions, the CBsub.1 receptor function was better preserved in SHR when the endocannabinoid tone was increased by the inhibition of MAGL or the endocannabinoid transporter.
The polyphenol trans‐resveratrol (t‐RES) is present as t‐RES‐3‐O‐β‐D‐glycoside, termed piceid, in several plant‐derived foods. Although data on the metabolism and on in vivo effects of t‐RES have ...been reported, quantitative data on the metabolites formed after dietary intake of t‐RES or piceid are still lacking. In this study, 85.5 mg of piceid per 70 kg of body weight (bw) were administered to healthy volunteers in a bolus dose. t‐RES metabolites formed in plasma and urine were identified and quantified by LC‐MS/MS, NMR, and HPLC‐DAD analysis using chemically synthesized t‐RES conjugate standards. In addition, the amount of t‐RES metabolites bound noncovalently to plasma proteins was determined for the first time in humans. The metabolites identified and quantified were t‐RES‐3‐sulfate, t‐RES‐3,4′‐disulfate, t‐RES‐3,5‐disulfate, t‐RES‐3‐glucuronide and t‐RES‐4′‐glucuronide, with t‐RES‐sulfates being the dominant conjugates in plasma and urine. Besides these metabolites, two novel t‐RES‐C/O‐conjugated diglucuronides have been identified and quantified in plasma and urine. Moreover, it could be shown that up to 50% of the plasma t‐RES‐3‐sulfate, t‐RES‐disulfates, and the novel t‐RES‐C/O‐diglucuronides were bound to proteins. Total recovery of the dietary administered piceid in urine ranged between 13.6 and 35.7%.
PDF
