Synthesis and diverse biological activity profile of triethylammonium isatin-3-hydrazones

A series of biorelevant triethylammonium isatin hydrazones containing various substituents in the aromatic fragment have been synthesized. Their structure and composition were confirmed by NMR- and IR-spectroscopies, mass-spectrometry and elemental analysis. It was found that some representatives show activity against Staphylococcus aureus and Bacillus cereus higher or at the level of norfloxacin, including methicillin-resistant Staphylococcus aureus strains. The study also showed low hemo- and cytotoxicity (Chang Liver) and high antiaggregatory and anticoagulant activity of these compounds. The high potential of new ammonium isatin-3-acylhydrazones in the search for antimicrobial activity against phytopathogens of bacterial and fungal nature has been shown for the first time.

COELENTERATE TOXINS, ITS PHARMACEUTICAL AND THERAPEUTIC EFFECTS

Present review article emphasizes species specific coelenterate toxins, its pharmaceutical and therapeutic effects. Most of the coelenterates inflict venom accidently by using nematocysts found on arms. These animals very quickly do massive and multiple inflictions of venom which causes cardiotoxicity that leads to the death of human beings. Coelenterate venom toxin groups differ in their composition and show diverse biological activity i.e. cytolytic or neurotoxic, hemolytic, anti-parasitic activity, α-amylase inhibitor activity, and analgesic activity anti-cancerous and antitumor activity, anti-inflammatory and antimicrobial activity. Coelenterate venom initiates toxic and immunological reactions exert their effects by modifying the properties of the ion channels involved in action potential generation in nerve, heart, and skeletal muscles. This article suggests available information, on coelenterate toxins could be used to develop potential therapeutic interventions for various human diseases and disorders.

HYBRID MOLECULES BASED ON ALKALOIDS

This review has been summarized the data on the synthesis of new hybrid derivatives based on alkaloid molecules. At the same time, there have been analyzed methods for obtaining hybrid structures containing fragments of natural compounds molecules in combination with other biologically active plant metabolites, as leading compounds for the development of new pharmacologically valuable agents, with the aim of creating new original drugs. The combination of pharmacophoric residues in one molecule, namely various aromatic and heterocyclic substituents in the nucleoside position of natural alkaloids, opens up new possibilities for both the subsequent chemical modification of the polyfunctional derivatives obtained and their new diverse biological activity. Effective methods of synthesis have been developed on the basis of directed transformations of these compounds (or their precursors). A wide range of pharmaco-logical properties of combined compounds of these series with a combination of low toxicity is promising. Considering that the preparation of combined derivatives based on alkaloid molecules has been insufficiently studied, the targeted synthesis of new com-pounds is of interest both in terms of new medicinespreparation and the development of new methods of organic synthesis, as well as the molecules stereochemistry determination of a new series of compounds.

Green Chemistry Approaches To The Synthesis Of Flavonoids

: In nature, flavonoids constitute a relatively diverse family of aromatic molecules such as flavones, flavonols, flavanones, isoflavone, chalcones, and their derivatives. Natural and synthetic flavonoids have reported diverse biological activity including antimycobacterial, antimicrobial, antiproliferative, antiarrhythmic, antiviral, antihypertensive, antioxidant, and anti-inflammatory. Flavonoids have garnered much attention as potential targets for nutraceuticals and pharmaceuticals. The recent development of ‘‘Green Chemistry’’ has enabled us to manipulate biosynthetic pathways to generate a library of synthetic flavonoids and to diminish the hazards for human health and environmental pollution from conventional methods. This paper presents an exhaustive review of the green synthesis of flavonoids. Green chemistry is the need of the day; hence chalcones can be synthesized in an eco-friendly manner without using solvents. The chalcone synthesis involves the solvent-free solid-state trituration between acetophenone derivatives and substituted benzaldehydes in the presence of NaOH/KOH as a base (Claisen-Schmidt reaction). Using these chalcone derivatives, synthesis of flavonoids can be done. In the pharmaceutical arena, economical bulk production of different types of flavonoids has been successfully established by green chemistry techniques.

An Overview of the Role of Long Non-Coding RNAs in Human Choriocarcinoma

Choriocarcinoma (CC), a subtype of trophoblastic disease, is a rare and highly aggressive neoplasm. There are two main CC subtypes: gestational and non-gestational, (so called when it develops as a component of a germ cell tumor or is related to a somatic mutation of a poorly differentiated carcinoma), each with very diverse biological activity. A therapeutic approach is highly effective in patients with early-stage CC. The advanced stage of the disease also has a good prognosis with around 95% of patients cured following chemotherapy. However, advancements in diagnosis and treatment are always needed to improve outcomes for patients with CC. Long non-coding (lnc) RNAs are non-coding transcripts that are longer than 200 nucleotides. LncRNAs can act as oncogenes or tumor suppressor genes. Deregulation of their expression has a key role in tumor development, angiogenesis, differentiation, migration, apoptosis, and proliferation. Furthermore, detection of cancer-associated lncRNAs in body fluids, such as blood, saliva, and urine of cancer patients, is emerging as a novel method for cancer diagnosis. Although there is evidence for the potential role of lncRNAs in a number of cancers of the female genital tract, their role in CC is poorly understood. This review summarizes the current knowledge of lncRNAs in gestational CC and how this may be applied to future therapeutic strategies in the treatment of this rare cancer.

Antioxidant Extracts of Three Russula Genus Species Express Diverse Biological Activity

This study explored the biological properties of three wild growing Russula species (R. integra, R. rosea, R. nigricans) from Serbia. Compositional features and antioxidant, antibacterial, antibiofilm, and cytotoxic activities were analyzed. The studied mushroom species were identified as being rich sources of carbohydrates and of low caloric value. Mannitol was the most abundant free sugar and quinic and malic acids the major organic acids detected. The four tocopherol isoforms were found, and polyunsaturated fatty acids were the predominant fat constituents. Regarding phenolic compounds, P-hydroxybenzoic and cinnamic acids were identified in the prepared methanolic and ethanolic extracts, which displayed antioxidant activity through the inhibition of thiobarbituric acid reactive substances (TBARS) formation and oxidative hemolysis; the highest activity was attributed to the R. nigricans ethanolic extract. This is the first report on the antibacterial and antibiofilm potential of the studied species, with the most promising activity observed towards Streptococcus spp. (0.20–0.78 mg/mL as the minimal inhibitory concentration, MIC). The most promising cytotoxic effect was caused by the R. integra methanolic extract on non-small cell lung cancer cells (NCI-H460). Therefore, due to the observed in vitro bioactive properties, the studied mushrooms arise as a source of functional ingredients with potential to be used in novel nutraceutical and drug formulations, which can be used in the treatment of various diseases and health conditions.

Interleukin-6 inhibitors

Interleukin 6 (IL-6) is a pleiotropic cytokine which has diverse biological activity, with wide-ranging effects on the immune system, homeostasis, and metabolism. It is the most abundant pro-inflammatory cytokine in the synovial joints and sera of patients with active rheumatoid arthritis (RA) and has been found to play a central role in the pathogenesis of the disease, causing joint inflammation and destruction, as well as systemic manifestations. Inhibition of IL-6 signalling has been investigated and developed as a potential treatment strategy for RA. Clinical trials have demonstrated the efficacy and safety of tocilizumab, a humanized monoclonal antibody directed against the IL-6 receptor, showing therapeutic benefit both in early RA and those considered to have refractory disease. The success of tocilizumab has spurred the development of an array of new biologic agents targeting the IL-6 pathway in RA.

The Importance of 2-AminoThiazole Schiff Bases as Antimicrobial and Anticancer Agents

The pharmacophore 2-aminothiazole has an interesting role in pharmaceutical chemistry as this led to the synthesis of many types of compounds with diverse biological activity. Schiff base derivatives at the same time contribute to drug evolution importantly. In this review, the Schiff base derivatives of 2-aminothiazole formed and some of their metal complexes are being focused on, and the antimicrobial and anticancer activity of them is being illustrated.

Current Advances on the Extraction and Identification of Bioactive Components of Sage (Salvia spp.)

Common sage (Salvia spp., with the most common species Salvia officinalis L., Lamiaceae) is an important medicinal and aromatic plant, with antioxidant, antimicrobial, anti-inflammatory and anticancer properties. The polyphenolic compounds are mainly responsible for its diverse biological activity. Many different methods for extraction and identification of sage bioactive compounds, using various solvents, have been developed in recent years. The total phenolic content is usually measured and identified by various technical methodologies with different sensitivity and specificity. In this aspect, the present review is aimed to critically summarize and discuss various technical approaches for the extraction and identification of sage bioactive components in order to point out the more appropriate approaches of them.