Avaliação toxicológica aguda e screening hipocrático da epiisopilosina, alcalóide secundário de Pilocarpus microphyllus Stapf.

Lucio, E. M. R. de A.; Rosalen, Pedro Luis; Sharapin, Nikolai; Brito, Alba Regina Monteiro Souza

doi:10.1590/s0102-695x2000000100003

Cited by 14 publications

(11 citation statements)

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“…Changes in body and organ weights are a clear indicative of damage caused by the substance test (Berenguer-Rivas et al, 2013), while the hippocratic screening provides a general estimate of pharmacological and toxicological nature (Lucio et al, 2000). After the acute toxicity test, the dose of 2000 mg/kg (limit test -OECD, 2008a) of OPAC did not cause the death of any animal.…”

Section: Resultsmentioning

confidence: 99%

Acute and subacute (28 days) oral toxicity assessment of the oil extracted from Acrocomia aculeata pulp in rats

Traesel

Souza

Barros

et al. 2014

Food and Chemical Toxicology

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Acrocomia aculeata, popularly known as “bocaiúva”, is a species used for nutritional purposes and for the treatment of various diseases, as it has, among other things, high levels of antioxidant compounds. This study aimed to assess the toxicological profile of A. aculeata, through acute and subacute toxicity tests. Male and female rats (Wistar) received by gavage 2000 mg/kg of oil extracted from the pulp of A. aculeata (OPAC) for the acute toxicity test and 125, 250, 500 or 1000 mg/kg of OPAC for subacute toxicity test. In the acute toxicity study no mortality or behavioral changes were observed in rats treated with 2000 mg/kg, indicating that the LD50 is higher than this dose. In the subacute toxicity test, the tested doses produced no significant changes in hematological, biochemical or histopathological parameters in the animals exposed. These results demonstrate the absence of acute and subacute toxicity after oral exposure to A. aculeata oil in rats. However, further studies in animals and in humans are needed in order to have sufficient safety evidence for its use in humans.

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Section: Resultsmentioning

confidence: 99%

Acute and subacute (28 days) oral toxicity assessment of the oil extracted from Acrocomia aculeata pulp in rats

Traesel

Souza

Barros

et al. 2014

Food and Chemical Toxicology

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“…O screening hipocrático é um ensaio bastante útil e comumente usado na triagem preliminar de plantas para detectar atividades farmacológicas e toxicológicas (Lucio et al, 2000). O extrato etanólico das folhas (EEF) e o látex de Synadenium umbellatum demonstraram influenciar a atividade geral e consciência dos animais, que ficaram mais quietos durante a primeira hora de observação.…”

Section: Tabela 3 Hábitos Fisiológicos Diários De Ratas Tratadas Comunclassified

Avaliação da toxicidade aguda e subaguda, em ratos, do extrato etanólico das folhas e do látex de Synadenium umbellatum Pax.

Cunha¹,

Azeredo²,

Mendonça³

et al. 2009

Rev. bras. farmacogn.

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RESUMO:O uso de plantas medicinais tem sido muito significativo nos últimos anos, sendo incentivado pela Organização Mundial de Saúde (OMS). Synadenium umbellatum Pax, Euphorbiacea (vulgo cola-nota, cancerola, milagrosa) tem o látex usado empiricamente como antitumoral e antiinflamatório. Por existir espécies tóxicas nesta família e visando à segurança no uso de extratos vegetais, tal estudo avaliou a toxicidade pré-clínica do látex e do extrato etanólico das folhas (EEF) de S. umbellatum, por via oral, em ratas Wistar. O estudo seguiu diretrizes do Guideline 423 (toxicidade aguda) e Guideline 407 (toxicidade subaguda) da OECD (Organisation for Economic Cooperation and Development). Na toxicidade aguda do látex e do EEF, não se observou letalidade nem alterações fisiológicas e comportamentais das ratas na dose de 2000 mg/ kg, sendo praticamente atóxico. Porém, na análise histopatológica, o látex ocasionou congestão e infiltrado leucocitário nos rins, fígado e pulmões, efeitos não observados com o EEF. Na toxicidade subaguda, doses de 50, 100 e 200 mg/kg de EEF não produziram alterações dose-dependentes significativas nos parâmetros laboratoriais e fisiológicos, nem alterações macroscópicas e histopatológicas nos órgãos das ratas. Contudo, o uso crônico da planta S. umbellatum merece mais estudos.Unitermos: Synadenium umbellatum, toxicidade aguda, toxicidade subaguda, toxicidade pré-clinica.ABSTRACT: "Acute and subacute toxicity studies of the latex and of the ethanolic extract of the leaves of Synadenium umbellatum Pax in rats". The use of medicinal plants has been being very significant in the last years, being the use encouraged by WHO. Synadenium umbellatum Pax, Euphorbiacea (popularly known as cola-note, cancerola, miraculous) has the latex used empirically as anti-cancerous and anti-inflammatory. For there being toxic species in this family and aiming at the safety in the use of vegetable extracts, such study evaluated the pre-clinical toxicity of the latex and of the ethanolic extract of the leaves (EEL) of S. umbellatum, administrated by oral route, in Wistar female rats. The study followed OECD's Guidelines for test of acute toxicity (Guideline 423) and for subacute toxicity (Guideline 407). In the acute toxicity of latex and EEL, behavioral and physiological alterations were not observed neither animal's death in the dose level of 2,000 mg/kg. However, the latex caused congestion and leukocytes infiltration of the kidneys, liver and lungs, effects not observed with EEL. In the subacute toxicity, dose levels of 50, 100 and 200 mg/kg of EEL did not produced significant dose-dependent alterations in the lab results and no physiologic, macroscopic and hystopathological alterations. EEL of S. umbellatum is practically poisonless in acute exposure; already the latex can cause hystological damages. The chronic use of S. umbellatum needs more specific studies.

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“…[6] In Brazil, the Pilocarpus microphyllus Stapf ex Wardleworth leaves have been explored as a source of pilocarpine by the industry. Recently, a chemical study of the waste produced by pilocarpine extraction from P. microphyllus allowed the isolation of two imidazole alkaloids structurally similar: epiisopilosine (EPIIS) [7,8] and epiisopiloturine (EPI) [9,10] (Figure 1). EPI has several pharmacological properties, including antiparasitic, [9,11] antibacterial, antiproliferative activities.…”

Section: Introductionmentioning

confidence: 99%

Imidazole alkaloids inhibit the pro-inflammatory mechanisms of human neutrophil and exhibit anti-inflammatory propertiesin vivo

Rocha

Machado

Sousa

et al. 2019

Journal of Pharmacy and Pharmacology

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Objectives Epiisopiloturine (EPI) and epiisopilosine (EPIIS) are side products in the pharmaceutical industry. The present study aimed to investigate the anti‐inflammatory potential of the alkaloids EPI and EPIIS in human neutrophils and mechanical hyperalgesia in mice. Methods Neutrophils (5 × 106 cells/ml) incubated with EPI and EPIIS and stimulated by the addition of N‐formyl‐methionyl‐leucyl‐phenylalanine or phorbol 12‐myristate‐13‐acetate. The release of myeloperoxidase (MPO), reactive oxygen species (ROS) production, calcium influx, gene expression of NF‐κB and pro‐inflammatory cytokines production were evaluated. It was also investigated the effect these alkaloids on carrageenan‐induced mechanical hyperalgesia model in mice. Key findings We demonstrated that both EPI and EPIIS inhibited the degranulation of activated neutrophils. This effect was accompanied by the reduction in ROS, the prevention of the increase in intracellular Ca2+ and decrease in the density of cytosolic NF‐κB, and inhibition of TNF‐α and IL‐6 production. Evaluating hypernociception in mice, EPI and EPIIS inhibited carrageenan‐induced inflammatory hypernociception and reduced MPO levels. Conclusions The results obtained suggest EPI and EPIIS not only inhibit neutrophils functions in vitro, but also exhibits anti‐inflammatory properties in vivo, acting through the modulation of the activation and/or accumulation of neutrophils in the inflammatory focus. Thus, EPI and EPIIS possess promising anti‐inflammatory therapeutic potential.

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Avaliação toxicológica aguda e screening hipocrático da epiisopilosina, alcalóide secundário de Pilocarpus microphyllus Stapf.

Cited by 14 publications

References 0 publications

Acute and subacute (28 days) oral toxicity assessment of the oil extracted from Acrocomia aculeata pulp in rats

Acute and subacute (28 days) oral toxicity assessment of the oil extracted from Acrocomia aculeata pulp in rats

Avaliação da toxicidade aguda e subaguda, em ratos, do extrato etanólico das folhas e do látex de Synadenium umbellatum Pax.

Imidazole alkaloids inhibit the pro-inflammatory mechanisms of human neutrophil and exhibit anti-inflammatory propertiesin vivo

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