In vivo anti-inflammatory activity of BACCHARIN from BRAZILIAN green PROPOLIS.

Baccharin is one of the major compounds found in Brazilian green propolis and its botanical source, Baccharis dracunculifolia. Considering the biological effects of propolis and B. dracunculifolia, this study aims to evaluate the analgesic and anti-inflammatory potential of baccharin. The neurodepressor potential was performed by the open field test, analgesia by mechanical stimulation with Dynamic Plantar Aesthesiometer, and by thermal stimulation with Hargreaves apparatus. In addition, the anti-inflammatory potential was achieved by the paw edema assay, histopathological evaluation, and NF-kB expression. Doses of 2.5, 5, and 10 mg/kg of baccharin were evaluated. After euthanasia, plantar tissue was collected and prepared for histology. As a result, analgesic activity was observed at a dose of 10 mg/kg of baccharin in thermal stimulation under an inflammatory process and anti-inflammatory potential at a dose of 5 mg/kg of baccharin from the second hour in the paw edema test. A decrease in cellular infiltrate and down-modulation of NF-kB, besides the reduction of edema in the histopathology was observed. There was no evidence of kidney and liver toxicity and neurodepressive potential at the doses tested. Thus, baccharin has a promising anti-inflammatory effect possibly associated with antiedematogenic activity by inhibiting mediators such as prostaglandins, inhibiting the migration of polymorphonuclear cells, and modulating NF-kB expression.

Evaluation of anti-inflammatory activity of kaurenol: Experimental evaluation and mechanistic insights.

BACKGROUND: Kaurenol, a diterpene alcohol found in Copaifera langsdorffii Desf. (known as "copaiba"), is historically used in traditional medicine for inflammatory conditions. OBJECTIVES: This study aims to comprehensively assess the potential anti-inflammatory and antinociceptive properties of kaurenol. METHODS: To this end, the following experiments were conducted to evaluated toxicity: locomotor performance and acute toxicity; nociception: acetic acid-induced writhing and formalin-induced antinociception; and anti-inflammatory activity: carrageenan and dextran-induced paw edema at 10, 20, and 40 mg/kg, and measurement of nitric oxide (NO), tumor necrosis factor alpha (TNF-α), interleukin-6 (IL-6), and interleukin-10 (IL-10) in macrophages at 1, 3, and 9 µg/ml. RESULTS: Kaurenol did not show significant locomotor changes, acute toxicity, and central analgesic activity in the first phase of formalin test at dosages tested. Kaurenol showed 53%, 64%, 64%, and 58% of inhibition in the acetic acid-induced writhing, second phase of formalin test, carrageenan and dextran-induced paw edema, respectively. CONCLUSION: The anti-inflammatory activity was associated with the regulation of NO release and probably with the regulation of mediators, such as serotonin and prostaglandin in vascular permeability, as well as by being associated with the regulation of IL-6 and IL-10. Kaurenol display anti-inflammatory activity but has no analgesic activity.

Advances in the phytochemical screening and biological potential of propolis.

Propolis is a natural resinous product collected from different parts of plants by bees and mixed with their salivary secretions. The occurrence of more than 180 different chemotypes has flavonoids, phenolic acids, esters, and phenolic aldehydes, as well as balsamic resins, beeswax, pollen, and essential and aromatic oils, among others. Its biological potential documented throughout the world justifies the need, from time to time, to organize reviews on the subject, with the intention of gathering and informing about the update on propolis. In this review (CRD42020212971), phytochemical advances, in vitro, in vivo, and clinical biological assays of pharmacological interest are showcased. The focus of this work is to present propolis clinical safety assays, antitumor, analgesic, antioxidant, anti-inflammatory, and antimicrobial activities. This literature review highlights propolis' promising biological activity, as it also suggests that studies associating propolis with nanotechnology should be further explored for enhanced bioprocessing applications.

Antitumor activity of solamargine in mouse melanoma model: relevance to clinical safety.

Melanoma is the most aggressive type of skin cancer, and thus it is important to develop new drugs for its treatment. The present study aimed to examine the antitumor effects of solamargine a major alkaloid heteroside present in Solanum lycocarpum fruit. In addition solamargine was incorporated into nanoparticles (NP) of yttrium vanadate functionalized with 3-chloropropyltrimethoxysilane (YVO4:Eu3+:CPTES:SM) to determine antitumor activity. The anti-melanoma assessment was performed using a syngeneic mouse melanoma model B16F10 cell line. In addition, systemic toxicity, nephrotoxic, and genotoxic parameters were assessed. Solamargine, at doses of 5 or 10 mg/kg/day administered subcutaneously to male C57BL/6 mice for 5 days, decreased tumor size and frequency of mitoses in tumor tissue, indicative of a decrease in cell proliferation. Treatments with YVO4:Eu3+:CPTES:SM significantly reduced the number of mitoses in tumor tissue, associated with no change in tumor size. There were no apparent signs of systemic toxicity, nephrotoxicity, and genotoxicity initiated by treatments either with solamargine alone or plant alkaloid incorporated into NP. The animals treated with YVO4:Eu3+:CPTES:SM exhibited significant increase in spleen weight accompanied by no apparent histological changes in all tissues examined. In addition, animals treated with solamargine (10 mg/kg/day) and YVO4:Eu3+:CPTES:SM demonstrated significant reduction in hepatic DNA damage which was induced by tumor growth. Therefore, data suggest that solamargine may be considered a promising candidate in cancer therapy with no apparent toxic effects.

Disinfectants in a Hemodialysis Setting: Antifungal Activity Against Aspergillus and Fusarium Planktonic and Biofilm Cells and the Effect of Commercial Peracetic Acid Residual in Mice.

Aspergillus and Fusarium cause a broad spectrum of infections in humans, mainly in immunocompromised patients. Among these, patients undergoing hemodialysis are highly susceptible to infections, requiring a constant and adequate environmental disinfection program. Nevertheless, monitoring the residual disinfectants can contribute to the morbidity and mortality reduction in these patients. Here, we evaluated the susceptibility of Aspergillus spp. (n=19) and Fusarium spp. (n=13) environmental isolates against disinfectants (acetic acid, citric acid, peracetic acid, sodium hypochlorite, and sodium metabisulphite) at different concentrations and time exposures. Also, we investigated the in vivo toxicity of the peracetic acid residual concentration in mice. Fusarium isolates were identified by F. equiseti, F. oxysporum and F. solani while Aspergillus presented clinically relevant species (A. fumigatus, A. niger and A. terreus) and environmental ones. Against planktonic cells, only two disinfectants (acetic acid and sodium hypochlorite) showed a fungicidal effect on Fusarium spp., while only one (sodium hypochlorite) was effective against Aspergillus spp. Both fungi formed robust in vitro biofilms with large amounts of the extracellular matrix, as evidenced by electron micrographs. Exposure of fungal biofilms to disinfectants showed sensitivity to three (acetic, citric, and peracetic acids), although the concentrations and times of exposure varied according to the fungal genus. Mice exposure to the residual dose of peracetic acid during 60 weeks showed anatomopathological, hematological, and biochemical changes. The implementation of news control measures and those that already exist can help reduce infections, the second cause of death and morbidity in these patients, besides providing safety and well-being to them, a priority of any quality health program.

Incorporation of indomethacin into a mesoporous silica nanoparticle enhances the anti-inflammatory effect Indomethacin into a mesoporous silica.

PURPOSE: We evaluated the analgesic, anti-inflammatory and toxicological effects of indomethacin incorporated into mesoporous silica nanoparticles (IND+NP). METHODS: Nociception was evaluated by the formalin assay. The anti-inflammatory potential was assessed by cell migration and paw edema assays, modulation of nitric oxide and cytokines (IL-6, IL-10 and TNF-α) by macrophages production. Toxicity was evaluated in peritoneal macrophages and by the locomotion assay and assessment of gastric injuries, presence of occult blood and hepatic and renal markers. RESULTS: IND+NP reduced nociception during phases 1 by 53% and 2 by 79% of the formalin assay and the influx of peritoneal cells by 94%, indicating an analgesic and anti-inflammatory effect more efficiently than indomethacin alone. Indomethacin, but not IND+NP, caused macroscopic gastric injuries, the presence of fecal occult blood, and an increase of ALT levels. In the paw edema assay, IND+NP reduced edema by 21%. IND+NP has no effect on the LPS-induced production of nitric oxide, IL-6, IL-10 and TNF-α on no cytotoxic concentrations. CONCLUSIONS: The incorporation of indomethacin into mesoporous silica nanoparticles effectively increased the activity of the drug observed in the formalin and cell migration assays and prevented the gastric and hepatic damage associated with its use.

Avaliação do potencial quimioprotetor do fruto de Psidium guajava contra os efeitos genotóxicos da doxorrubicina / Evaluation of Psidium guajava fruit chemoprotective against the genotoxic effects of doxorubicin

Resumo Introdução A goiaba é um fruto amplamente utilizado como alimento e é considerada planta medicinal em países tropicais e subtropicais. Pesquisas têm mostrado que o fruto contém constituintes químicos com abrangente uso clínico. Além disso, a maior parte das substâncias utilizadas no tratamento contra câncer foi isolada a partir de produtos naturais. Objetivo Avaliar o potencial citotóxico, mutagênico, antimutagênico e quimioprotetor da fruta liofilizada de Psidium guajava, a goiaba, in vivo. Método A citotoxicidade, a mutagenicidade e a antimutagenicidade foram avaliadas em três diferentes dosagens (0,625, 1,25 e 2,50 g/kg) de goiaba. Resultados Os resultados mostraram que a goiaba não apresentou atividade citotóxica e mutagênica no ensaio de micronúcleo em sangue periférico e que não houve alterações nos valores de ALT e AST, indicando ausência de toxicidade hepática. Nos animais tratados com a goiaba, a dose de 0,625 mg/kg significativamente reduziu os danos induzidos pela doxorrubicina. Conclusão Esses resultados mostraram que o consumo de goiaba é seguro e capaz de proteger o material genético de alterações genômicas.

Abstract Background Guava is a fruit widely used as food and is considered a medicinal plant in the tropical and subtropical countries. Scientific research has shown that the fruit contains chemical constituents with comprehensive clinical use. In addition, most of the substances used in cancer treatment have been isolated from natural products. Objective To evaluate the cytotoxic, mutagenic, antimutagenic, and chemoprotective potential of the freeze-dried fruit of Psidium guajava, guava, in vivo. Method Cytotoxicity, mutagenicity, and antimutagenicity were evaluated in three different dosages (0.625, 1.25, 2.50 g/kg) of guava. Results The results show that guava does not present cytotoxic 2 and mutagenic activity in the micronucleus assay in peripheral blood and there were no alterations in ALT and AST values showing the absence of hepatic toxicity. In animals treated with guava, the dose of 0.625 mg/kg significantly reduced the damage induced by doxorubicin. Conclusion These results show that guava consumption is safe as it is also capable of protecting the genetic material from changes.

In vivo methods for the evaluation of anti-inflammatory and antinoceptive potential / Métodos in vivo para avaliação do potencial anti-inflamatório e antinociceptivo

ABSTRACT BACKGROUND AND OBJECTIVES: The constant search for bioactive compounds with anti-inflammatory and antinociceptive activities are of interest to research centers. For the characterization of these activities, trials on guinea pigs are necessary. Therefore, the purpose of this study was to demonstrate some methods to evaluate the anti-inflammatory and antinociceptive potential of natural products. CONTENTS: A stimulus is required to evaluate these activities, and the induction of inflammatory or nociceptive process can be by chemical inducers like formaldehyde, carrageenan, among others, or electronic equipment such as the hot plate. For all assays, the baseline and post-dose measurement of the studied compound is always compared with a control group. The planning of the experiment, as well as its conduct in accordance with well-established protocols, are important tools in the success of the work. The tests presented evaluated the antinociceptive and anti-inflammatory activity as well as the mechanisms involved. CONCLUSION: It was possible to evaluate that the tests present in the literature today meet the researcher's need for the elucidation of the anti-inflammatory and antinociceptive activity of new compounds.

RESUMO JUSTIFICATIVA E OBJETIVOS: A busca constante por compostos bioativos com atividade anti-inflamatória e antinociceptiva são de interesse dos centros de pesquisas. Para a caracterização dessas atividades são necessários ensaios em cobaias. Frente a isso, o objetivo deste estudo foi demonstrar alguns métodos para a avaliação do potencial anti-inflamatório e antinociceptivo de produtos naturais. CONTEÚDO: Para a avaliação dessas atividades é necessário um estímulo, sendo que a indução de processo inflamatório ou nociceptivo pode ser por indutores químicos como formol, carragenina, entre outros, ou ainda, equipamentos eletrônicos como placa quente. Para todos os ensaios, sempre é realizada a mensuração basal e posterior à administração do composto que está sendo estudado em comparação com um grupo controle. O planejamento do experimento, assim como toda a condução conforme protocolos já bem ilustrados, são ferramentas importantes no êxito do trabalho. Os testes apresentados avaliaram atividade antinociceptiva e anti-inflamatória assim como mecanismos envolvidos. CONCLUSÃO: Foi possível avaliar que os testes presentes na literatura hoje, atendem a necessidade do pesquisador na elucidação da atividade anti-inflamatória e atividade antinociceptiva de novos compostos.