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[Determination of polybrominated diphenyl ethers in serum using isotope internal standard-gas chromatography-high resolution dual-focus magnetic mass spectrometry].

A method for the determination of 14 polybrominated diphenyl ethers (PBDEs) in human serum using isotope internal standard-gas chromatography-high resolution dual-focus magnetic mass spectrometry (GC-HRMS) was developed. After thawed to room temperature, 0.5 mL serum samples were mixed with 13C-labeled isotopic internal standard. Subsequently, methanol was added to precipitate the proteins in the samples. The effects of three kinds of acids on the removal of cellulite from the serum samples and the corresponding recoveries were compared, and the results revealed that sulfuric acid was the most

Chiral pesticides: identification, description, and environmental implications.

Of the 1,693 pesticides considered in this review, 1,594 are organic chemicals, 47 are inorganic chemicals, 53 are of biological origin (largely non chemical; insect,fungus, bacteria, virus, etc.), and 2 have an undetermined structure. Considering that the EPA's Office of Pesticide Programs found 1,252 pesticide active ingredients(EPA Pesticides Customer Service 2011), we consider this dataset to be comprehensive; however, no direct comparison of the compound lists was undertaken. Of all pesticides reviewed, 482 (28%) are chiral; 30% are chiral when considering only the organic chemical pestic

Marine Natural Products as Potent Anticancer Agents (2020-2024): Structural Diversity, SARs and Target Prediction.

In recent years, Marine Natural Products (MNPs) have emerged as a significant source for anticancer drug discovery, as many natural products can offer structural diversity, unique mechanisms of action, and relatively low toxicity. This article provides a systematic review of MNPs with reported anticancer activities from 2020 to 2024. These compounds are classified into seven major categories: terpenoids, alkaloids, sterols, polyketides, peptides and proteins, polysaccharides, and macrolides. For each category, we elaborate on the marine sources, structural identification, in vitro anticancer a

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… D-ring opening and bromination greatly enhance selectivity and cytotoxicity. … Furthermore, elements such as bromine, sulfur, and chlorine are present in some molecules, reflecting the structural characteristics of MNPs. …

Perflubron emulsion improves hepatic microvascular integrity and mitochondrial redox state after hemorrhagic shock.

Hemorrhagic shock is associated with decreased systemic oxygen delivery, but also with impaired microvascular perfusion, which can result in diminished local oxygen availability even in the presence of adequate cardiac output after resuscitation. Beside surgical interventions to control blood loss, transfusion of stored packed red blood cells represents the current standard of care in the management of severe hemorrhagic shock. Because stored red blood cells are less deformable and show a higher O2 affinity that affects the O2 off-load to tissues, perfluorocarbon-based artificial oxygen carrie

Phosphorus flame retardants: properties, production, environmental occurrence, toxicity and analysis.

Since the ban on some brominated flame retardants (BFRs), phosphorus flame retardants (PFRs), which were responsible for 20% of the flame retardant (FR) consumption in 2006 in Europe, are often proposed as alternatives for BFRs. PFRs can be divided in three main groups, inorganic, organic and halogen containing PFRs. Most of the PFRs have a mechanism of action in the solid phase of burning materials (char formation), but some may also be active in the gas phase. Some PFRs are reactive FRs, which means they are chemically bound to a polymer, whereas others are additive and mixed into the polyme

Exposure and effects assessment of persistent organohalogen contaminants in arctic wildlife and fish.

Persistent organic pollutants (POPs) encompass an array of anthropogenic organic and elemental substances and their degradation and metabolic byproducts that have been found in the tissues of exposed animals, especially POPs categorized as organohalogen contaminants (OHCs). OHCs have been of concern in the circumpolar arctic for decades. For example, as a consequence of bioaccumulation and in some cases biomagnification of legacy (e.g., chlorinated PCBs, DDTs and CHLs) and emerging (e.g., brominated flame retardants (BFRs) and in particular polybrominated diphenyl ethers (PBDEs) and perfluorin

Ah receptor agonists in UV-exposed toluene solutions of decabromodiphenyl ether (decaBDE) and in soils contaminated with polybrominated diphenyl ethers (PBDEs).

GOAL, SCOPE AND BACKGROUND: The use of polybrominated diphenyl ethers (PBDEs) as flame retardants increases the risk for emissions of other brominated compounds, such as polybrominated dibenzodioxins (PBDDs) and dibenzofurans (PBDFs). The large homology in structure of PBDD/Fs and mechanism of toxic action, i.e. the capacity to activate the Ah receptor (AhR) pathway, compared to their well-studied chlorinated analogues, justifies a raised concern to study the environmental levels and fate of these compounds. Decabromodiphenyl ether (decaBDE) is the most widely used PBDE today. Studies on photo

Preliminary characterization of a murine model for 1-bromopropane neurotoxicity: Role of cytochrome P450.

Neurotoxicity of 1-bromopropane (1-BP) has been reported in both human cases and animal studies. To date, neurotoxicity of 1-BP has been induced in rats but not in mice due to the lethal hepatotoxicity of 1-BP. Oxidization by cytochromes P450 and conjugation with glutathione (GSH) are two critical metabolism pathways of 1-BP and play important roles in toxicity of 1-BP. The aim of the present study was to establish a murine model of 1-BP neurotoxicity, by reducing the hepatotoxicity of 1-BP with 1-aminobenzotriazole (1-ABT); a commonly used nonspecific P450s inhibitor. The results showed that

Halogenated flame-retardant concentrations in settled dust, respirable and inhalable particulates and polyurethane foam at gymnastic training facilities and residences.

Halogenated flame-retardants (FRs) are used in a wide array of polymer-containing products. Animal studies and structure-activity modeling exercises suggest that FR exposure may result in detrimental toxicological effects. Workers with extended contact with such polymers (e.g., electronic dismantlers, carpet installers and aircraft personnel) have previously been observed to exhibit elevated body burdens of FRs, e.g., polybrominated diphenyl ethers (PBDEs). Recently, elevated PBDE blood levels were also reported in a non-occupational exposure group, gymnasts. These levels were hypothesized to

Essential Medicinal Chemistry of Essential Medicines.

Since 1977, the World Health Organization publishes a list of essential medicines, i.e., those that satisfy the priority health care needs of the population and are selected with regard to disease prevalence and public health relevance, evidence of clinical efficacy, and safety, as well as comparative costs and cost-effectiveness. The Essential Medicines List (EML) is an invaluable tool for all countries to select those medicines that have an excellent risk/benefit ratio and that are reputed to be of pivotal importance to health. In the present perspective, we describe the chemical composition

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… The plant kingdom rarely incorporates halogens in its biosynthetic pathways, and this is the reason for which no natural compound displays fluorine, while three EMs contain chlorine, but they originate from sources other than plants (vancomycin, griseofulvin, chloramphenicol). 25 In the EML, bromine … In particular, bromine is found in halothane, the only inhalational anesthetic containing this element, and in bedaquiline, a drug effective in tuberculosis (TB) that was approved in 2012, representing the first new medicine for TB in more than 40 years. 26 Iodine is present in the antiarrhythmic amiodarone …

An Updated Review on Marine Anticancer Compounds: The Use of Virtual Screening for the Discovery of Small-Molecule Cancer Drugs.

Marine secondary metabolites are a promising source of unexploited drugs that have a wide structural diversity and have shown a variety of biological activities. These compounds are produced in response to the harsh and competitive conditions that occur in the marine environment. Invertebrates are considered to be among the groups with the richest biodiversity. To date, a significant number of marine natural products (MNPs) have been established as antineoplastic drugs. This review gives an overview of MNPs, both in research or clinical stages, from diverse organisms that were reported as bein

A Review of the Regulatory Challenges of Personalized Medicine.

Personalized medicine integrates genomics with clinical and familial histories, revolutionizing healthcare by tailoring treatments to individual patient characteristics. At its core, pharmacogenomics enables the customization of medication prescriptions based on genetic profiles, enhancing drug efficacy and safety. This precision medicine approach addresses disease diagnosis, prevention, and treatment, offering targeted therapies for conditions like autoimmune disorders, rheumatoid arthritis, and neoplastic conditions. Examples of pharmacogenomics and personalized medicine include treatment fo

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… Radioactive particles like iodine-124 and bromine-76 undergo decay and cellular elimination. The TKI-PET method is employed to visualize affected cells, focusing specifically on EGFR. …

Advanced Technologies for Large Scale Supply of Marine Drugs.

Marine organisms represent a source of unique chemical entities with valuable biomedical potentialities, broad diversity, and complexity. It is essential to ensure a reliable and sustainable supply of marine natural products (MNPs) for their translation into commercial drugs and other valuable products. From a structural point of view and with few exceptions, MNPs of pharmaceutical importance derive from the so-called secondary metabolism of marine organisms. When production strategies rely on marine macroorganisms, harvesting or culturing coupled with extraction procedures frequently remain t

NTP Toxicology and Carcinogenesis Studies of Decabromodiphenyl Oxide (CAS No. 1163-19-5) In F344/N Rats and B6C3F1 Mice (Feed Studies).

Toxicology and carcinogenesis studies of decabromodiphenyl oxide, a flame retardant for plastics and other materials, were conducted by exposing groups of 50 male and 50 female F344/N rats and B6C3F1 mice at 0, 25,000, and 50,000 ppm in the diet for 103 weeks. These concentrations were selected because no toxicity was observed at any dose in the 14-day or 13-week studies and 50,000 ppm chemical in the diet is considered to be the highest dose to which rats and mice can be exposed for extended periods of time without reducing the nutritional value of the diet. No compound-related gross or micro

The Greenhouse effect: impacts of ultraviolet-B (UV-B) radiation, carbon dioxide (CO2), and ozone (O3) on vegetation.

There is a fast growing and an extremely serious international scientific, public and political concern regarding man's influence on the global climate. The decrease in stratospheric ozone (O3) and the consequent possible increase in ultraviolet-B (UV-B) is a critical issue. In addition, tropospheric concentrations of 'greenhouse gases' such as carbon dioxide (CO2), nitrous oxide (N2O) and methane (CH4) are increasing. These phenomena, coupled with man's use of chlorofluorocarbons (CFCs), chlorocarbons (CCs), and organo-bromines (OBs) are considered to result in the modification of the earth's…

Molecular Diversity of Lupane Hybrids in Drug Design and Materials Science.

The need for new, more effective drugs to treat cancer, infectious diseases, various parasitic infestations, and metabolic disorders requires innovative approaches to the design of promising molecules. One of these areas is the creation of hybrid structures. Lupane triterpenoids are of significant interest for such research due to their high abundance in natural sources and their renewable nature, their molecular architecture, presence of several easily modifiable functional groups, enantiomeric purity, broad spectrum of biological activity, and low toxicity. Active research into the biologica

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… Acylation of the 3-OH group in BA, followed by allylic bromination using NBS, produced 3β-acetoxy-30-bromo-lup-20(29)-en-28-oic acid. At a concentration of 100 μM, this compound inhibited the viability of L. amazonensis promastigote forms by 47.41%. … Introduction of a bromine atom into the triterpene scaffold enhanced antileishmanial activity, as the parent compound BA was ineffective at 100 μM under the tested conditions [ 146 ]. …

NTP Toxicology and Carcinogenesis Studies of Polybrominated Biphenyls (CAS No. 67774-32-7)(Firemaster FF-1(R)) in F344/N Rats and B6C3F1 Mice (Feed Studies).

Polybrominated biphenyls are synthetic chemicals used as flame retardants. The technical product used in these studies, Firemaster FF-1(R)), is a mixture of brominated biphenyls. Firemaster FF-1(R)) is a known liver carcinogen in rats and mice and is one of three compounds chosen by the National Toxicology Program to investigate the potential value of perinatal exposures in assessing chemical carcinogenicity. Chronic toxicity and carcinogenicity studies of polybrominated biphenyls (Firemaster FF-1(R)) were conducted in F344/N rats and B6C3F1 mice of each sex. The studies were designed to deter

Dioxin- and POP-contaminated sites--contemporary and future relevance and challenges: overview on background, aims and scope of the series.

BACKGROUND, AIM AND SCOPE: Once they have been generated, polychlorinated dibenzo-p-dioxins (PCDDs) and dibenzofurans (PCDFs) and other persistent organic pollutants (POPs) can persist in soils and sediments and in waste repositories for periods extending from decades to centuries. In 1994, the US EPA concluded that contaminated sites and other reservoirs are likely to become the major source of contemporary pollution problems with these substances. With this in mind, this article is the first in a new series in ESPR under the title 'Case Studies on Dioxin and POP Contaminated Sites--Contempor

Oncogenic Roles and Inhibitors of DNMT1, DNMT3A, and DNMT3B in Acute Myeloid Leukaemia.

Epigenetic alteration has been proposed to give rise to numerous classic hallmarks of cancer. Impaired DNA methylation plays a central role in the onset and progression of several types of malignancies, and DNA methylation is mediated by DNA methyltransferases (DNMTs) consisting of DNMT1, DNMT3A, and DNMT3B. DNMTs are frequently implicated in the pathogenesis and aggressiveness of acute myeloid leukaemia (AML) patients. In this review, we describe and discuss the oncogenic roles of DNMT1, DNMT3A, and DNMT3B in AML. The clinical response predictive roles of DNMTs in clinical trials utilising hy

Cuproptosis Inducers in Cancer Therapy: State of the Art and Challenges.

Cancer continues to be the primary cause of death despite significant progress in medicine, and finding effective therapies remains a challenge. New treatments are needed to minimize the harmful effects on the body and increase the selectivity of drugs. These therapies must also overcome cancer cell resistance and prevent metastasis. Metal-based drugs are becoming increasingly crucial for treating tumors, and copper ion-based systems and nanoparticles have been identified as having unique properties and anticancer potential. Given the key role exerted by Cu in the etiology, severity, and progr

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… X‐ray crystallography reveals that complex 1 is tetra‐coordinated with Cu(I), involving two PPh 3 ligands, one bromine atom, and one sulfur atom, arranged in a trigonal pyramidal geometry. … Among the low‐molecular‐ weight inducers of cuproptosis, a Cu(I) complex featuring a bromine atom and three coordinated PPh 3 groups has been recently reported [ 114 ]. …