Mechanism of antiulcerogenic activity of semi-synthetic crotonin obtained from Croton cajucara Benth.

Almeida, Ana Beatriz Albino de; Miotto, Alexandre Marcucci; Nunes, Domingos Sávio; Spadari-Bratifisch, Regina C.; Brito, Alba Regina Monteiro Souza

doi:10.1590/s0102-695x2002000300050

Cited by 12 publications

(9 citation statements)

References 24 publications

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“…(Euphorbiaceae) (Nardi et al 2003), antileishmanial, antinociceptive, antiulcerogenic and cytotoxic activities of Croton cajucara Benth. (Euphorbiaceae) (Campos et al 2002;Almeida et al 2003;Rosa et al 2003), antimicrobial and the antimalarial effects Croton kongensis Gagnep. (Thongtan et al 2003), antinociceptive and anti-inflammatory properties of Croton malambo Karst.…”

Section: Introductionmentioning

confidence: 99%

Oxidant effects and toxicity of Croton campestris in Drosophila melanogaster

Júnior

Macedo

Zemolin

et al. 2016

Pharmaceutical Biology

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Context: Croton campestris A.St.-Hil. (Euphorbiaceae) is a species native to Northeast Brazil used by traditional communities for the treatment of a variety of health problems. However, potential toxicological effects of this plant are unknown. Objective: The potential toxicity of the hydroalcoholic extract of C. campestris leaves on Drosophila melanogaster insect model, additionally with phytochemical constitution and cellular mechanisms mediating the action of extract were analysed in this study. Materials and methods: Constituents of the extract were evaluated by HPLC. In vitro antioxidant potential of extract was analysed by DPPH, ABTS and FRAP. Flies injected culture medium mixed with extract (0.1-50 mg/mL) for 72 h. After, ROS production was evaluated by DCF-DA oxidation. Phosphorylation of MAPK signalling pathway was investigated by Western blotting method. Activity of antioxidant enzymes was analysed in homogenates.Results: Major components of the extract include quercetin (38.11 ± 0.06 mg/g), caffeic acid (20.06 ± 0.17 mg/g) and kaempferol (15.45 ± 0.05 mg/g). Consumption of the extract impaired locomotor performance and induced fly death of flies (LC 50 of 26.51 mg/mL). Augmented ROS formation and SOD, CAT and GST activity were observed from 0.1 mg/mL. JNK and p38 kinases phosphorylation was modulated and Paraquat-induced toxicity was augmented by extract. Discussion and conclusion: Our data show important toxicological effects of C. campestris leading to increased mortality and impaired locomotor performance accompanied by induction of cell stress markers in flies. The study draws attention to the indiscriminate use of plant extracts. ARTICLE HISTORY

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Section: Introductionmentioning

confidence: 99%

Oxidant effects and toxicity of Croton campestris in Drosophila melanogaster

Júnior

Macedo

Zemolin

et al. 2016

Pharmaceutical Biology

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“…A atividade antiulcerogênica foi também comprovada, para o 19-nor-clerodano trans-crotonina, que difere da DCTN apenas pela ausência da insaturação Δ 3,4 do anel A do sistema decalínico, bem como para o óleo fi xo das cascas do caule do Croton cajucara (Almeida et al, 2003;Hiruma-Lima et al, 2000;Hiruma-Lima et al, 2002). Como os clerodados CTN, cis-cajuarina B e transcajuarina B foram evidenciados em baixos percentuais, neste óleo, (Souza et al, 2006) deve existir uma ação conjunta destes clerodanos para o efeito gastroprotetor deste óleo.…”

Section: Atividade Antiulcerogênicaunclassified

Uma revisão das atividades biológicas da trans-desidrocrotonina, um produto natural obtido de Croton cajucara

Costa¹,

Magalhães²,

Gomes³

et al. 2007

Rev. bras. farmacogn.

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RESUMO:Croton cajucara Beth (Euphorbiaceae) uma espécie medicinal nativa da região Amazônica do Brasil, onde é vulgarmente conhecida como 'sacaca', representa um recurso terapêutico efi caz no tratamento e cura de várias doenças. O metabólito majoritário transdesidrocrotonina (DCTN), isolado das cascas do caule desta planta, encontra-se correlacionado com grande parte das propriedades medicinais da sacaca. Este artigo de revisão, descreve os resultados fi toquímicos e farmacológicos que foram realizados com o diterpeno do tipo clerodano DCTN, bem como seus derivados semi-sintéticos. Adicionalmente, apresenta perspectivas para a biodisponibilização deste protótipo de fármaco em nanosistemas. Unitermos:Croton cajucara, trans-desidrocrotonina, DCTN, fi toquímica, atividade biológica, nanobiotecnologia.ABSTRACT: "A review of the biologic activities of trans-dehydrocrotonin, a natural product obtained from Croton cajucara". Croton cajucara Beth (Euphorbiaceae) is a plant found in the Amazonian Region of North Brazil, where it is popularly known as sacaca. The major secondary metabolite, trans-dehydrocrotonin (DCTN) a clerodane-type diterpene, isolated from the stem bark is a chief bioactive compound of Croton cajucara. This review describes results of extensive pharmacological studies of DCTN, as well as its semi-synthetic derivatives, and also presents insights into the use of DCTN as a therapeutic agent and some potential advantages of its incorporation in drug delivery systems.

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“…The biological importance of natural and semisynthetic CTN has been reported (Grynberg et al, 1999;Maciel et al, 2000;Hiruma-Lima et al, 2002;Almeida et al, 2002;Anazetti et al, 2003). Regarding to AAA biological importance, this compound proved to possess antibiotic (Addae-Mensah et al, 1992) and antibacterial (Peres et al, 1997) activities.…”

Section: Introductionmentioning

confidence: 99%

Comparative anti-inflammatory and antinociceptive effects of terpenoids and an aqueous extract obtained from Croton cajucara Benth

Perazzo¹,

Carvalho²,

Rodrigues³

et al. 2007

Rev. bras. farmacogn.

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RESUMO: "Avaliação comparativa dos efeitos anti-infl amatório e antinociceptivo de terpenóides e de extrato aquoso obtidos de Croton cajucara Benth". O 19-nor-clerodano trans-crotonina (CTN) e o triterpeno ácido acetil aleuritólico (AAA), isolados das cascas do caule de Croton cajucara Benth (Euphorbiaceae), uma planta tradicional da Região Amazônica do Brasil, bem como o extrato aquoso (EA) das cascas do caule deste Croton, foram submetidos a experimentos farmacológicos utilizando animais, para avaliação das atividades anti-infl amatória e antinociceptiva. A administração oral de AAA (50 mg/kg), CTN (50 mg/kg) ou AE (300 mg/ kg) inibiram as contorções em ratos, induzidas por ácido acético. Os terpenóides AAA e CTN, bem como o extrato polar EA, inibiram signifi cativamente o edema de pata em ratos, induzido por carragenina. As inibições foram observadas em todos os intervalos de medições, tendo sido evidenciado melhores inibições para os terpenóides AAA (47,7%, após a primeira hora) e CTN (54,4%, após a segunda hora). Evidenciou-se ainda, após 90 minutos do estímulo, signifi cante inibição no edema induzido por dextrana (31,9% para CTN e 28,5% para AAA) e por histamina (43,2% para CTN e 40,5% para AAA). Estes resultados confi rmam o uso popular de Croton cajucara na região Amazônica do Brasil, no combate a infl amações. Unitermos:Croton cajucara, ácido acetil aleuritólico, trans-crotonina, anti-infl amatório, antinociceptivo. ABSTRACT:The 19-nor-clerodane trans-crotonin (CTN) and the triterpene acetyl aleuritolic acid (AAA), isolated from the stem bark of Croton cajucara Benth (Euphorbiaceae), a traditional medicinal plant from Amazon region of Brazil, as well as the aqueous extract (AE) from its stem bark, were submitted to pharmacological screening for anti-infl ammatory and antinociceptive activities in animal models. The oral administration of AAA (50 mg/kg), CTN (50 mg/kg) or AE (300 mg/kg) inhibited the acetic acid-induced writhing in mice. The AE, CTN and AAA had shown signifi cant inhibition of carrageenin-induced edema in rats, in all time intervals measured after the injection of the stimulus, with the greatest inhibition at the fi rst hour for AAA (47.7%) and the second hour for CTN (54.4%). They have also exhibited signifi cant inhibition in the dextran-induced edema 90 minutes after the stimulus: 31.9% for CTN and 28.5% for AAA. In the histamine-induced edema, the inhibition showed by CTN and AAA were 43.2% and 40.5%, respectively, 90 minutes after the injection of stimulus. This study extends and supports the popular medicine and folkloric uses of Croton cajucara in the Amazon region of Brazil.

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Mechanism of antiulcerogenic activity of semi-synthetic crotonin obtained from Croton cajucara Benth.

Cited by 12 publications

References 24 publications

Oxidant effects and toxicity of Croton campestris in Drosophila melanogaster

Oxidant effects and toxicity of Croton campestris in Drosophila melanogaster

Uma revisão das atividades biológicas da trans-desidrocrotonina, um produto natural obtido de Croton cajucara

Comparative anti-inflammatory and antinociceptive effects of terpenoids and an aqueous extract obtained from Croton cajucara Benth

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