RESUMO

The aim of this work was to evaluate the pharmacological effect of seven structurally related terpenes on the contractility of cardiac muscle. The effect of terpenes was studied on isolated electrically driven guinea pig left atrium. From concentration-response curves for inotropic effect were determined the EC50 and relative potency of such terpenes. Our results revealed that all terpenes, except phytol, showed ability to reduce the contractile response of guinea pig left atrium. Further, relative potency was directly related to the number of isoprene units and to the lipophilicity of the compounds. For example, sesquiterpenes farnesol and nerolidol showed higher relative potency when compared with the monoterpenes citronellol, geraniol and nerol. We can conclude that most of the evaluated terpenes showed a promising negative inotropism on the atrial muscle. Future studies are necessary to investigate their action mechanism.

Assuntos

RESUMO

The most poisonous fish species found along the Brazilian coast is the spotted scorpionfish Scorpaena plumieri. Though hardly ever life-threatening to humans, envenomation by S. plumieri can be quite hazardous, provoking extreme pain and imposing significant socioeconomic costs, as the victims may require days to weeks to recover from their injuries. In this review we will walk the reader through the biological features that distinguish this species as well as the current epidemiological knowledge related to the envenomation and its consequences. But above all, we will discuss the challenges involved in the biochemical characterization of the S. plumieri venom and its compounds, focusing then on the successful isolation and pharmacological analysis of some of the bioactive molecules responsible for the effects observed upon envenomation as well as on experimental models. Despite the achievement of considerable progress, much remains to be done, particularly in relation to the non-proteinaceous components of the venom. Therefore, further studies are necessary in order to provide a more complete picture of the venom's chemical composition and physiological effects. Given that fish venoms remain considerably less studied when compared to terrestrial venoms, the exploration of their full potential opens a myriad of possibilities for the development of new drug leads and tools for elucidating the complex physiological processes.

RESUMO

The most poisonous fish species found along the Brazilian coast is the spotted scorpionfish Scorpaena plumieri. Though hardly ever life-threatening to humans, envenomation by S. plumieri can be quite hazardous, provoking extreme pain and imposing significant socioeconomic costs, as the victims may require days to weeks to recover from their injuries. In this review we will walk the reader through the biological features that distinguish this species as well as the current epidemiological knowledge related to the envenomation and its consequences. But above all, we will discuss the challenges involved in the biochemical characterization of the S. plumieri venom and its compounds, focusing then on the successful isolation and pharmacological analysis of some of the bioactive molecules responsible for the effects observed upon envenomation as well as on experimental models. Despite the achievement of considerable progress, much remains to be done, particularly in relation to the non-proteinaceous components of the venom. Therefore, further studies are necessary in order to provide a more complete picture of the venoms chemical composition and physiological effects. Given that fish venoms remain considerably less studied when compared to terrestrial venoms, the exploration of their full potential opens a myriad of possibilities for the development of new drug leads and tools for elucidating the complex physiological processes.(AU)

Assuntos

RESUMO

The most poisonous fish species found along the Brazilian coast is the spotted scorpionfish Scorpaena plumieri. Though hardly ever life-threatening to humans, envenomation by S. plumieri can be quite hazardous, provoking extreme pain and imposing significant socioeconomic costs, as the victims may require days to weeks to recover from their injuries. In this review we will walk the reader through the biological features that distinguish this species as well as the current epidemiological knowledge related to the envenomation and its consequences. But above all, we will discuss the challenges involved in the biochemical characterization of the S. plumieri venom and its compounds, focusing then on the successful isolation and pharmacological analysis of some of the bioactive molecules responsible for the effects observed upon envenomation as well as on experimental models. Despite the achievement of considerable progress, much remains to be done, particularly in relation to the non-proteinaceous components of the venom. Therefore, further studies are necessary in order to provide a more complete picture of the venoms chemical composition and physiological effects. Given that fish venoms remain considerably less studied when compared to terrestrial venoms, the exploration of their full potential opens a myriad of possibilities for the development of new drug leads and tools for elucidating the complex physiological processes.

Assuntos

RESUMO

The most poisonous fish species found along the Brazilian coast is the spotted scorpionfish Scorpaena plumieri. Though hardly ever life-threatening to humans, envenomation by S. plumieri can be quite hazardous, provoking extreme pain and imposing significant socioeconomic costs, as the victims may require days to weeks to recover from their injuries. In this review we will walk the reader through the biological features that distinguish this species as well as the current epidemiological knowledge related to the envenomation and its consequences. But above all, we will discuss the challenges involved in the biochemical characterization of the S. plumieri venom and its compounds, focusing then on the successful isolation and pharmacological analysis of some of the bioactive molecules responsible for the effects observed upon envenomation as well as on experimental models. Despite the achievement of considerable progress, much remains to be done, particularly in relation to the non-proteinaceous components of the venom. Therefore, further studies are necessary in order to provide a more complete picture of the venom's chemical composition and physiological effects. Given that fish venoms remain considerably less studied when compared to terrestrial venoms, the exploration of their full potential opens a myriad of possibilities for the development of new drug leads and tools for elucidating the complex physiological processes.(AU)

Assuntos

RESUMO

The essential oils obtained by steam distillation from the roots, stems, leaves and fruits of Ocotea duckei had their composition analyzed by GC-MS. The pharmacological activity of these oils was also evaluated showing significant cardiovascular effects. Forty-nine substances were identified, consisting of a complex mixture of monoterpenes (45 percent) and sesquiterpenes (55 percent). The fruits yielded (1.9 percent) more essential oil than the stems (1.0 percent), roots (0.8 percent) and leaves (0.7 percent). The main component in the oil of the leaves was trans-caryophyllene (60.54 percent), in the stem bark beta-eudesmol (27.51 percent) and in the fruits, dl-limonene (30.12 percent). The predominant essential oil component in the roots was elemol (24.31 percent). In non-anaesthetized normotensive rats, the essential oils from different parts of Ocotea duckei (leaves, fruits, stem and roots) induced significant (p < 0.05) hypotension followed by bradycardia.

O óleo essencial obtido da destilação por vapor de água das folhas, caule, raíz e frutos de Ocotea duckei teve sua composição química analisada através de CG-EM. A atividade farmacológica desses óleos também foi avaliada, mostrando significantes efeitos cardiovasculares. Quarenta e nove substâncias foram identificadas, constituída por uma mistura complexa de monoterpenos (45 por cento) e sesquiterpenos (55 por cento). Os frutos forneceram (1,9 por cento) mais óleo essencial do que os caules (1,0 por cento), raízes (0,8 por cento) e folhas (0,7 por cento). O principal componente encontrado nas folhas foi o trans-cariofileno (60,54 por cento), nas cascas do caule, beta-eudesmol (27,51 por cento) e nos frutos, dl-limoneno (30,12 por cento). O componente predominante do óleo essencial das raízes foi elemol (24,31 por cento). Em ratos normotensos, não anestesiados, o óleo essencial de diferentes partes de Ocotea duckei (folhas, frutos, caule e raiz) induziu significante (p < 0,05) hipotensão seguido de bradicardia.

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RESUMO

Das partes aéreas de Herissantia tiubae (K. Schum.) Brizicky foram isolados, através de métodos cromatográficos, dois flavonóides glicosilados, canferol 3,7-di-O-a-L-ramnopiranosídeo e canferol 3-b-O-D-(6’’-E-p-cumaroil) glicosídeo. As estruturas foram identificadas com o uso de técnicas espectroscópicas de IV, RMN ¹H e 13C incluindo métodos bidimensionais, além de comparações com dados da literatura. O canferol 3,7-di-O-a-L-ramnopiranosídeo foi submetido a testes farmacológicos preliminares com a finalidade de avaliar o seu efeito sobre o sistema cardiovascular.

From the aerial parts of Herissantia tiubae (K. Schum.) Brizicky two flavonol glycosides were isolated by means of chromatographic methods, kaempferol 3,7-di-O-a-L-rhamnopyranoside and kaempferol 3-O-b-D-(6’’-E-p-coumaroyl) glucoside. Their structural identification was made by IV, ¹H and 13C NMR spectroscopy, including two dimensional techniques, together with comparison with literatura data. Preliminary tests were carried out with kaempferol 3,7-di-O-a-L-rhamnopyranoside in order to study its possible cardiovascular effect.