Estudo fitoquímico das cascas do caule de Duguetia glabriuscula - Annonaceae, biomonitorado pelo ensaio de toxicidade frente a Artemia salina leach

The extract obtained from stem bark of Duguetia glabriuscula - Annonaceae was evaluated by Brine Shrimp Lethality test (BSL). The bioactive compounds, oxobufoline and lanuginosine, two oxoaporphine alkaloids were isolated by activity-guided fractionation. In addition, the compounds asaraldehyde, (+)-allo-aromadendrane-10beta, 14-diol, and two aporphine alkaloids, polyalthine and oliveridine were also obtained.

Glifosato: propriedades, toxicidade, usos e legislação

This paper supplies a compact revision on the herbicide glyphosate physic-chemistry characteristic mains, including toxicity and valid Brazilian legislation for its use.

DDT (dicloro difenil tricloroetano): toxicidade e contaminação ambiental - uma revisão

DDT and others organochlorine insecticides are very persistent substances. Clinical symptoms of intoxication have been reported in humans, although the main problem concerning such substances is bioaccumulation and biomagnification along throphic chains, leading to contamination of top predators and humans after them. In this review these characteristics are described, as well as some aspects of the control of vector borne diseases, like leishmaniasis and malaria, which were until recently, controlled by the health authorities using DDT.

Drogas anti-VIH: passado, presente e perspectivas futuras

Currently available anti-HIV drugs can be classified into three categories: nucleoside analogue reverse transcriptase inhibitors (NRTIs), non-nucleoside reverse transcriptase inhibitors (NNRTIs) and protease inhibitors (PIs). In addition to the reverse transcriptase (RT) and protease reaction, various other events in the HIV replicative cycle can be considered as potential targets for chemotherapeutic intervention: (1) viral adsorption, through binding to the viral envelope glycoprotein gp120; (2) viral entry, through blockage of the viral coreceptors CXCR4 and CCR5; (3) virus-cell fusion, through binding to the viral envelope glycoprotein gp 41; (4) viral assembly and disassembly through NCp7 zinc finger-targeted agents; (5) proviral DNA integration, through integrase inhibitors and (6) viral mRNA transcription, through inhibitors of the transcription (transactivation) process. Also, various new NRTIs, NNRTIs and PIs have been developed, possessing different improved characteristics.

A toxicidade em ambientes aquáticos: discussão e métodos de avaliação

Aquatic toxicity tests are assays performed with different aquatic organisms of different ecological organization levels. Such tests are a source of information on the toxicity of a given substance or wastewater under controlled conditions, and they complement the physico-chemical analyses. Moreover, they allow one to evaluate the risks resulting from the presence of toxic substances in the environment. Algae, crustaceans, fishes and bacteria are frequently used in toxicity tests. In this work, we will present the main aspects related to the aquatic toxicity tests and a discussion of their applicability will also be presented.

Aspectos mecanísticos da bioatividade e toxicidade de nitrocompostos

Nitrocompounds are bioactive molecules used as antibacterial, antiparasitic and antitumoral agents. In the past of years, these molecules have been broadly studied in several fields, such as medicinal chemistry, organic chemistry, biochemical, toxicology and electrochemistry. The nitrocompounds mode of action involves the biotransformation of the nitro group, releasing intermediates in the redox process. Some of those intermediates attack enzymes, membranes and DNA, providing the basis for their biological activity and adverse effects. In this report, some aspects regarding the biological activity, mechanism of action and toxicity of nitrocompounds are explored, purposing the research of new bioactive derivatives having low toxicity.

Toxicidade e atividade antioxidante de flavonoides das cascas das raízes de Lonchocarpus filipes

The phytochemical investigation of dichloromethane extract from root bark of Lonchocarpus filipes Benth (Leguminosae) afforded four flavonoids including three dibenzoylmethane derivatives rarely found in nature. The structures were established based on their spectral data (¹H and 13C NMR, 2D-NMR) as being: lanceolatin B (1), pongamol (2), (E)-7-O-methylpongamol (3) and (E)-9-O-methylpongamol (4). Compound (4) is described herein for the first time as a natural product. The extracts and the isolated compounds (1), (2) and (3) displayed high toxicity in the brine shrimp lethality assay. Only compound (2) showed antioxidant activity using a DPPH radical scavenging assay. This is the first report on the phytochemical study of Lonchocarpus filipes.

Glicoproteína-P, resistência a múltiplas drogas (MDR) e relação estrutura-atividade de moduladores

Multidrug resistance, MDR is a major obstacle for cancer chemotherapy. MDR can be reversed by drugs that vary in their chemical structure and main biological activity. Many efforts have been done to overcome MDR based on studies of structure-activity relationships and in this review we summarize some aspects of MDR mediated by P-glycoprotein (P-gp), as the most experimentally and clinically tested form of drug resistance. The most significant MDR mechanisms revealed until now are shortly discussed. Physicochemical and structural properties of MDR modulators, measures of the MDR reversal, and QSAR studies are included.

Química forense: perspectivas sobre novos métodos analíticos aplicados à documentoscopia, balística e drogas de abuso

In this review recent methods developed and applied to solve criminal occurences related to documentoscopy, ballistic and drugs of abuse are discussed. In documentoscopy, aging of ink writings, the sequence of line crossings and counterfeiting of documents are aspects to be solved with reproducible, fast and non-destructive methods. In ballistic, the industries are currently producing ''lead-free'' or ''nontoxic'' handgun ammunitions, so new methods of gunshot residues characterization are being presented. For drugs analysis, easy ambient sonic-spray ionization mass spectrometry (EASI-MS) is shown to provide a relatively simple and selective screening tool to distinguish m-CPP and amphetamines (MDMA) tablets, cocaine and LSD.

Análise forense: pesquisa de drogas vegetais interferentes de testes colorimétricos para identificação dos canabinoides da maconha (Cannabis Sativa L.)

Marijuana (Cannabis sativa L.) is the most cultivated, trafficked and consumed illicit drug worldwide. Estimates indicate 10% of individuals experiencing marijuana become daily users, and 20-30% use it weekly. Around 489 natural compounds have been identified in this plant, of which 70 are cannabinoids, responsible for psychic effects. The most relevant cannabinoid is Δ9-THC, recognized as the main chemical substance with psychoactive effects. The aims of this work was to investigate whether other drugs interfere with the colorimetric tests Fast Blue B and Duquenois-Levine, widely used for marijuana screening in forensic chemistry laboratories.

Drogas de abuso em águas naturais e residuárias urbanas: ocorrência, determinação e aplicações forenses

Drugs of abuse are commonly used outside medical or legal settings where their production, marketing and consumption are subject to legal summons and/or intervention. Classified as emerging contaminants, these substances have been recently detected in samples of environmental concern, such as waters and wastewaters. This review presents the state-of-the-art on the methodological approaches used in sample preparation, the main techniques applied in analytical determination at trace levels, as well as the use of information related to the drug or its metabolite concentration in sewage samples to empirically estimate the consumption of drugs of abuse in a city or region.

A química e toxicidade dos corantes de cabelo

The market for hair dye involves a growing range of products, which requires greater understanding of hair properties, mechanisms of action and color development. In this work, we present a critical analysis of the classification, physical and chemical characteristics, chemical analysis and toxicological/mutagenic potential of dyes used in the hair dyeing process. A compilation of some studies was carried out, focusing on the available knowledge about these dyes and their effects on the environment and human health.

Atividade antibacteriana in vitro e toxicidade frente à Artemia salina Leach. de alguns compostos triazenos

Bacterial resistance to antibacterial agents is currently a major concern. We report the synthesis, in vitro antibacterial activity and toxicity toward Artemia salina of six diaryltriazene compounds bearing different substituent groups. Minimal Inhibitory Concentration (MIC) and Minimal Bactericidal Concentration (MBC) values against standard strains (ATCC) and clinical isolates (including ESBL, MBL and AmpC strains) were good to very good, in the range 8 to 128 mg mL-1. Results suggest that hydroxyl, 4-carboxyl and 4-phenyldiazenil groups attached to the diaryltriazenes provide enhanced activity. Toxicity results showed very low LC50 values for three compounds (10-fold lower than DTIC).

ARSÊNIO E ARROZ: TOXICIDADE, METABOLISMO E SEGURANÇA ALIMENTAR

Arsenic is considered a semimetal, and its wide distribution in the Earth's crust in different chemical forms, including organic and inorganic species, has a great deal of influence on the mechanisms of toxicity. Exposure to arsenic can be either through occupational practice (use of pesticides) or by the consumption of water and food containing the element. Rice is considered a fundamental constituent of the basic diet of Brazilians and is usually cultivated in flooded conditions. Such a plantation system results in an increased amount of As in the soil and hence a greater accumulation of As in the plant, which is highlighted by the inorganic species' classification as highly toxic. Besides the use of mitigation techniques to reduce the toxicological risk, monitoring the concentration of As and its chemical species in rice and rice products is required through the establishment of legislation in the area. Thus, some world organizations are conducting improved research to determine and establish acceptable concentrations of As and its chemical species in rice, e. g., in 2012, FDA researchers described a chemical speciation methodology for As in rice and rice products. Hence, the application of existing chemical speciation methods and the establishment of parameters for ensuring food security and exposure risk assessment deserve particular consideration.