Synthesis and Biological Activity of the Pyridine-Hexacyclic-Steroid Derivative on a Heart Failure Model

Background: Several drugs with inotropic activity have been synthesized; however, there is very little information on biological activity exerted by steroid derivatives in the cardiovascular system. Objective: The aim of this research was to prepare a steroid-pyridine derivative to evaluate the effect it exerts on left ventricular pressure and characterize its molecular interaction. Methods: The first stage was carried out through the synthesis of a steroid-pyridine derivative using some chemical strategies. The second stage involved the evaluation of the biological activity of the steroid-pyridine derivative on left ventricular pressure using a model of heart failure in the absence or presence of the drugs, such as flutamide, tamoxifen, prazosin, metoprolol, indomethacin, and nifedipine. Results: The results showed that steroid-pyridine derivative increased left ventricular pressure in a dose-dependent manner (0.001-100 nM); however, this phenomenon was significantly inhibited only by nifedipine at a dose of 1 nM. These results indicate that positive inotropic activity produced by the steroid-pyridine derivative was via calcium channel activation. Furthermore, the biological activity exerted by the steroid-pyridine derivative on the left ventricle produces changes in cAMP concentration. Conclusion: It is noteworthy that positive inotropic activity produced by this steroid-pyridine derivative involves a different molecular mechanism compared to other positive inotropic drugs. Therefore, this steroid could be a good candidate for the treatment of heart failure.

Aurones: A Golden Resource for Active Compounds

Deemed as poorly represented in nature, aurones have been often overlooked by researchers compared to other members of the flavonoid superfamily. However, over the past two decades, they have been reassessed by the scientific community, who are increasingly appreciating their ability to modulate several biological pathways. This review summarizes the recent literature on this class of compounds, which has been analyzed from both a chemical and a functional point of view. Original articles, reviews and editorials featured in Pubmed and Scifinder over the last twenty years have been taken into account to provide the readers with a view of the chemical strategies to obtain them, their functional properties, and their potential of technological use. The resulting comprehensive picture aims at raising the awareness of these natural derivatives as effective drug candidates, fostering the development of novel synthetic analogues.

Chemical strategies for triggering the immune response to the mycotoxin patulin

Mycotoxins represent a major concern for human and animal health because of their harmful effects and high occurrence in food and feed. Rapid immunoanalytical methods greatly contribute to strengthening the safety of our food supply by efficiently monitoring chemical contaminants, so high-affinity and specific antibodies have been generated for almost all internationally regulated mycotoxins. The only exception is patulin, a mycotoxin mainly produced by Penicillium expansum for which such a target has not yet been achieved. Accordingly, no point-of-need tests commonly used in food immunodiagnostics are commercially available for patulin. In the present study, three functionalized derivatives conforming to generally accepted rules in hapten design were firstly tested to generate suitable antibodies for the sensitive immunodetection of patulin. However, these conventional bioconjugates were unable to elicit the desired immune response, so an alternative strategy that takes advantage of the high electrophilic reactivity of patulin was explored. Patulin was reacted with 4-bromothiophenol, and the obtained adduct was used to produce antibodies with nanomolar affinity values. These results demonstrated for the first time that targeting the adduct resulting from the reaction of patulin with a thiol-containing compound is a promising approach for developing user-friendly immunoanalytical techniques for this elusive mycotoxin.

Synthesis of an Adamantyl Derivative and their Theoretical Interaction with both COX-1 and COX-2 Enzymes

Various drugs have been used to treat pain; nevertheless, several drugs can produce side effects such as bronchospasm, thinning, and angioedema. In the search for new therapeutic alternatives, some drugs have been elaborated using different reagents that are difficult to handle and require special conditions such as different pH and higher temperatures. Therefore, this research aimed to prepare an adamantyl derivative (compound 4) from 1-Adamantyl bromomethyl ketone using some chemical strategies. Besides, a theoretical evaluation of the interaction of compound 4 with both cyclooxygenase enzymes (COX-1 and COX-2) was evaluated using either 4cox or 5jw1 proteins as theoretical models. In addition, both indomethacin and celecoxib drugs were used as controls in a docking model. The results showed that compound 4 has a higher affinity by both 4cox and 5jw1 proteins surface compared with either indomethacin or celecoxib drugs. In conclusion, these data suggest that 4 could be a good candidate for pain treatment.

Design and Synthesis of Two Azete Derivatives Using some Chemical Strategies

There are several methods for preparing nitrogen-containing four-membered heterocycles using some reagents that require special conditions such as higher temperatures or differences in the pH. This research aimed to prepare two azete derivatives from 1-Bromo-3,5-dinitrobenzene using some chemical strategies. The chemical structure was characterized by NMR spectroscopic methods. The results indicate that protocols used to synthesize two azete analogs do not require special conditions to give a good yielding. In conclusion, is reported a facile method for the synthesis of two azete derivatives.

A Brief Insight into Microbial Corrosion and its Mitigation with Eco-friendly Inhibitors

Corrosion results from the electrochemical reactions between the metal and its existing environment. Corrosion results in severe and expensive damage to a wide spectrum of industries. When microbes are involved in corrosion it is seldom possible to economically evaluate its impact. Microbially influenced corrosion is recognized to cause catastrophic failures contributing to approximately 20% of the annual losses. In many engineering applications, microbially influenced corrosion control is of prime importance. Expensive, toxicity and sometimes, even ineffectiveness of the current chemical strategies to mitigate microbially influenced corrosion have shifted the interest towards eco-friendly inhibitors. The present review discusses microbial induced corrosion in various metals and its inhibition through eco-friendly inhibitors. In addition, the study also reviews the morphological and electrochemical impedance results.

Species Identification of Wireworms (Agriotes spp.; Coleoptera: Elateridae) of Agricultural Importance in Europe: A New “Horizontal Identification Table”

Wireworms are yellowish soil-dwelling larvae that damage a wide range of arable crops. The most common wireworms found in European cultivated fields (except for the Caucasus) belong to the genus Agriotes (Coleoptera: Elateridae). In several European countries, environment-impacting insecticides are applied on a prophylactic basis to control them. However, before any treatment can be applied, European legislation requires that an assessment is done when pest population levels exceed a damage threshold. The threshold substantially depends on wireworm species, thus quick reliable larval identification is needed to implement the appropriate integrated pest management practices. Furthermore, research into non-chemical strategies involves carrying out tests with live and identified wireworms. Thus, thousands of wireworms were observed in a bid to identify live larvae so that larval density could be assessed and compared with species-specific thresholds before sowing, and laboratory experiments were carried out. This work led to a horizontal identification table that allows for quick and accurate identification of live larvae. This key, unlike traditional dichotomous keys, simultaneously considers a set of multiple discriminating morphological characters in order of stability. The key can be reliably used by less experienced users and, once minimum familiarity is acquired, most larvae can be identified rapidly, with high precision.