Assessment of Cytotoxic/Antitumour Potential and in silico Study of Salazinic Acid Isolated from Parmotrema concurrens.

INTRODUCTION: Despite numerous scientific advances, cancer continues to be one of the main causes of death in the world. This situation has driven the search for promising molecules. Lichen substances have been widely described for their pharmacological potential. OBJECTIVE: The present study evaluated the antitumour potential of a depsidone isolated from Parmotrema concurrens- salazinic acid (SAL) - through in vitro, in vivo and in silico studies. METHODS: The molecule was isolated from the acetonic extract of the lichen and recrystallized in acetone. The macrophage J774, sarcoma-180 and MDA-MB-231 cell lines were used for the MTT cytotoxicity assay. The antitumor assay used a murine model (Swiss albino mice) with sarcoma-180. The animals were treated for seven consecutive days with doses of SAL (25 and 50 mg/kg) and 5-fluorouracil (20 mg/kg). RESULTS: Its purity was determined using high-performance liquid chromatography (94%), and its structure was confirmed by H1 and C13 nuclear magnetic resonance. SAL was not considered toxic to cancer cell lines, showing cell viability rates of 79.49 ± 4.15% and 86.88 ± 1.02% for sarcoma-180 and MDA-MB-231, respectively. The tumour inhibition rate was greater than 80% in the animals treated with SAL and 65% for those that received 5-fluorouracil. Simulations of molecular dynamics to estimate the flexibility of the interactions between human thymidylate synthase and derivatives of SAL and 5-fluorouracil revealed that SAL exhibited greater enzymatic interaction capacity, with highly favourable energy, compared to 5-fluorouracil. CONCLUSION: The present results demonstrate the potential of salazinic acid as a tumour inhibition agent.

Formaldehyde exposure and atmospheric biomonitoring with lichen Cladonia verticillaris in an anatomy laboratory.

Formaldehyde is one of the most toxic contaminants of indoor environments and very common in the anatomy laboratory. In this work, we investigated the level of formaldehyde exposure to staff and students who attended an anatomy lab and in nearby environments in the same university building. We also performed atmospheric biomonitoring of the sites with the lichen Cladonia verticillaris. Quantification samplings were performed over four weeks, on 7 days with and 7 days without practical classes, totaling 70 samples. The samples were collected in five different locations, three points inside the laboratory and two points outside the laboratory, representing nearby and susceptible environments to contamination. The results showed CHOH concentrations from 0.20-3.76 ppmv for days with practical courses and 0.17-3.06 ppmv for days without practical classes. Although the laboratory was more contaminated than the surrounding environments, the concentration of formaldehyde in these areas is not negligible, showing a dispersion of formaldehyde from the laboratory. Potential dose (PD) and cancer risk (CR) were calculated for an individual exposed to the same levels analyzed for 8 h daily and 30 years of work. The study on C. verticillaris lasted 90 days and evaluated the variation of chlorophyll and pheophytin (photosynthetic pigments). The results showed a significant difference in the production of chlorophylls a and b and total chlorophyll when compared to control, and there was also a progressive increase of the total pheophytin/total chlorophyll ratio. The results also showed the correlation between the increase in chlorophylls and the studied environments with less ventilation since these places provided greater accumulation of formaldehyde in the long run. Thus, measurable evidence was obtained of biological disorders in a living organism caused by exposure to formaldehyde.

Cladia aggregata (lichen) from Brazilian northeast: chemical characterization and antimicrobial activity

The chemical composition and antimicrobial activity of the Cladia aggregata (Sw.) Nyl. were evaluated. Barbatic acid, depside obtained from C. aggregata, was spectroscopically analyzed and tested, as well as organic extracts. The extracts and purified substance were tested against four Staphylococcus aureus multi-resistant strains. The structure of barbatic acid was confirmed through NMR (¹H; 13C) and elemental ® analysis. Biochromatographic assays showed action of this compound, along with other substances contained in organic extracts, suggesting a synergic action, MIC assays placed barbatic acid in the same level of inhibition to other studied lichen substances.

A composição química e a atividade antimicrobiana da Cladia aggregata (Sw.) Nyl. foram avaliadas. O ácido barbático, um depsideo obtido da C. aggregata, foi espectroscopicamente analisado e testado, bem como o extrato orgânico. o extrato e a substância purificada foram testadas contra 4 linhagens de Staphylococcus aureus multi resistentes. A estrutura do ácido barbático foi confirmada através de ensaios de CCD, CLAE, IV, RMN (¹H;13C), UV e analise elementar (r). O biocromatograma mostrou a ação deste composto junto com outras substâncias contidas no extrato orgânico, sugerindo a ação sinérgica, a CMI do ácido barbático mostrou o mesmo nível de inibição de outras substâncias liquênicas.

Análise do líquen cladonia verticillaris (RADDI) Fr: em condiçôes de laboratório sob efeito do estireno e ciclohexano / Analysis of the lichen cladonia verticillaris (RADDI) FR: in laboratory conditions under styrene and ciclohexane effect

Cladonia verticillaris (Raddi) Fr. colectada en suelos arenosos en el municipio de Alhandra, Paraíba, fue sometida, bajo condiciones de laboratorio, a la aplicación de 4ml de estireno, ciclohexano y agua desionizada. Estratos orgánicos de muestras con 3,5,10 y15 días, fueron analizados en ensayos de cromatografía en capa delgada (CCD) y cromatografía líquida de alta eficiencia (CLAE). Estas muestras fueron también analizadas por microscopía electrónica de barrido (MEB) para análisis de alteraciones morfológicas. Los resultados evidenciaron la producción de algunas sustancias intermediarias y reducción del ácido fumarprotocetrárico y atranorina. El análisis de la superficie externa del liquen demostró alteraciones morfológicas con exhibición de las hifas corticales. Este estudio ratifica los datos obtenidos en el ambiente, y caracteriza el potencial de C. Verticillaris como bioindicador inmediato para polución atmosférica.

Nanoencapsulation of usnic acid: An attempt to improve antitumour activity and reduce hepatotoxicity.

Despite the recognised antiproliferative and antitumour properties of usnic acid, its therapeutic application has yet to be introduced. In fact, the high hepatotoxicity and low water solubility of usnic acid have somewhat restricted its practical use in anticancer therapy. The aim of this study was therefore to investigate the antitumour activity of usnic acid encapsulated into nanocapsules prepared with lactic co-glycolic acid polymer. Usnic acid-loaded nanocapsules were obtained using the interfacial deposition of a preformed polymer. The antitumour activity was confirmed on an ascitic tumour (Sarcoma-180) implanted in Swiss mice and estimated by means of the tumour inhibition. The results of antitumour activity confirmed that the encapsulation of usnic acid into PLGA-nanocapsules produced a 26.4% increase in tumour inhibition as compared with the standard free usnic acid treatment. Vacuolization of hepatocytes and a mild lymphocytic infiltration in portal spaces were observed in animals treated with free usnic acid. However, this hepatotoxicity was substantially reduced when animals were treated with usnic acid-loaded nanocapsules. No histological changes were noticed in the kidneys or spleen of animals treated either with usnic acid or usnic acid-loaded nanocapsules. These results suggest that nanoencapsulation may be a way of enabling usnic acid to be used in chemotherapy.

Atividade antimicrobiana e citotóxica de extratos brutos de Fuligo septica (L.) Wigg. E Tubifera microsperma (Berk. & Curt.) Martin (Myxomycetes) / Antibiotic and cytotoxic activities of crude extracts from Fuligo septica (L.) Wigg. and Tubifera microsperma (Berk. & Curt.) Martin (Myxomycetes)

Este trabalho apresenta as atividades citotóxica e antimicrobiana de extratos clorofórmico, acetônico e metanólico de Fuligo septica (L.) Wigg. e extrato metanólico de Tubifera microsperma (Berk. & Curt.) Martin contra bactérias Gram negativas, Gram positivas, álcool-ácido resistentes, fungos filamentosos e leveduras. Os extratos de F. septica foram ativos contra Bacillus subtilis e Candida albicans, enquanto o extrato de T. microsperma inibiu S. aureus, Mycobacterium smegmatis e C. albicans. A atividade citotóxica em células da linha contínua KB foi mais eficiente com o extrato acetônico de F. septica (DI50÷22µg/ml)