Analysis of the mechanisms underlying the vasorelaxant action of kaurenoic acid in the isolated rat aorta

Tirapelli, Carlos Renato; Ambrósio, Sérgio Ricardo; Costa, Fernando B. Da; Coutinho, Silvia T; Oliveira, Dionéia Camilo Rodrigues de; Oliveira, Ana Maria de

doi:10.1016/j.ejphar.2004.04.003

Cited by 66 publications

(63 citation statements)

References 22 publications

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“…From these secondary metabolites, the kaurane-type diterpenes have been associated with several important biological properties, including antiparasitic effect [2], antispasmodic and relaxant actions on the smooth muscle [3,4], among others [5].…”

Section: Introductionmentioning

confidence: 99%

Hyphal Morphology and Elongation Alterations in <i>Aspergillus nidulans</i> Provoked by the Diterpene Kaurenoic Acid

Rafael¹,

Arakawa²,

Ambrósio³

et al. 2013

AiM

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Kaurenoic acid (KA), a kaurane-type diterpene extracted from leaves of Mikania hirsutissima, was previously reported as an inhibitor of vascular contractility mainly by blocking extracellular Ca 2+ influx. The compound is known for several other biological activities such as antiparasitic, antispasmodic and antibacterial activity. The aim of the present study was to investigate the effect of KA on Aspergillus nidulans. KA (0.3 mM) showed fungistatic activity against A. nidulans with visible hyphal elongation and morphology damage. These effects were reverted by CaCl 2 addition showing that KA interferes with intracellular Ca 2+ gradient in A. nidulans. This is the first report on the mechanism of action of KA involving calcium levels by altering the elongation of fungi hyphae.

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Section: Introductionmentioning

confidence: 99%

Hyphal Morphology and Elongation Alterations in <i>Aspergillus nidulans</i> Provoked by the Diterpene Kaurenoic Acid

Rafael¹,

Arakawa²,

Ambrósio³

et al. 2013

AiM

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“…In the present study, glibenclamide did not produce any significant effect on concentration-response curves of KV, suggesting that KATP channels are not involved in the vasorelaxation induced by the biflavonoid. Similarly, neither apamin, BaCl2 nor ouabain, blockers of SKca, KIR channels and Na + -K + ATPase, respectively (Cortes et al, 2001;Tirapelli et al, 2004;Oliveira et al, 2006) affected the concentration-response curves of KV, hence these channels and the ATPase are not involved in the vasorelaxant effects of KV. TEA and ChTX, at these concentrations are nonselective blockers of large and intermediate conductance Ca 2+ -activated K + channels (BKCa).…”

Section: Discussionmentioning

confidence: 99%

Endothelium-independent vasodilation induced by kolaviron, a biflavonoid complex from Garcinia kola seeds, in rat superior mesenteric arteries

Adaramoye¹,

Medeiros²

2009

J Smooth Muscle Res

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Previous studies have established the hepatoprotective, gastroprotective, hypolipidemic and hypoglycemic effects of kolaviron (KV), a biflavonoid complex from Garcinia kola seeds. In this study, we investigated the mechanisms involved in the vasorelaxant effects of KV in isolated superior mesenteric arteries from normotensive rats. KV (1, 10, 30, 100, 300, 500 and 1,000 µg/ml) concentration-dependently inhibited the contractions induced by phenylephrine (PHE) (10 µM) and KCl (80 mM) in both endothelium-intact (Emax = 58.3 ± 1.7% and 51.4 ± 1.3%, respectively) and -denuded rings (Emax = 59.3 ± 5.5% and 64.3 ± 2.4%, respectively). Furthermore, KV reduced CaCl2-induced contraction in Ca 2+ -free medium containing KCl 60 mM, thus acting as a Ca 2+ -antagonist. In addition, KV inhibited the transient contraction by PHE in Ca 2+ -free medium containing EGTA, suggesting a possible action on the release of intracellular Ca 2+ via the inositol-1,4,5-triphosphate (IP3) pathway.KV is not a specific α-adrenoceptor blocker, since it also caused a concentration-dependent inhibition of contractile responses to KCl, suggesting that KV also blocks the L-type Ca 2+ -channel. As a Ca 2+ antagonist, KV (100 µg/ml) potentiates the relaxant effects of nifedipine in denuded rings (Emax = 97.6 ± 1.2%; control = 75.1 ± 3.0%, P<0.05). Also, the vasorelaxation induced by KV was significantly inhibited after pre-treatment of the denuded rings with 4-aminopyridine (4-AP) 1 mM, a selective blocker of voltage-dependent K + (Kv) channels and,

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“…Ou seja, tendo o ácido caurenóico demonstrado a capacidade de estimular a quimiotaxia de GNC humanos a favor de seu gradiente, implica que essas células são dotadas de um ou mais receptores responsáveis por esta interação. Tirapelli et al (2004) relataram que o ácido caurenóico tem a propriedade de interferir em vários mecanismos da resposta celular, sendo que um desses envolve a mobilização de Ca 2+ . Interessante ressaltar que a maioria dos receptores protéicos envolvidos na migração celular pertence à família de receptores associados ao complexo heterotrimérico da proteína G e que, em regra, a transdução de sinal desses receptores se dá pela hidrólise do fosfatidil-inusitol 4,5-bifosfato em seus mensageiros intermediários, o diacilglicerol e o inusitol 1,4,5-trifosfato.…”

Section: Figura 4 Efeitos Do Extrato Deunclassified

“…Os principais grupos de compostos presentes em extratos preparados de cascas (Oliveira et al, 2002), caules (Chen et al, 2004), folhas (Oliveira et al, 2002) e frutos (Chang et al, 1998;Chen et al, 2004) são os alcalóides, as acetogeninas e os diterpenos. Dentre estes, o ácido caurenóico (I), ou ácido caur-ent-16-en-19-oico, é um dos mais estudados, para o qual várias atividades biológicas já foram descritas, desde a inibição Potencial antiinflamatório de Annona glabra, Annonaceae da replicação do vírus HIV em linfócitos (Chang et al, 1998), como agente citotóxico (Costa-Lotufo et al, 2002;Zhang et al, 2004), trypanosomicida (Alves et al, 1995;Vieira et al, 2002), larvicida (Slimestrad et al, 1995), antimicrobiano (Padmaja et al, 1995;Velikova et al, 2000), vermífugo, esporicida (Padmaja et al, 1995), analgésico (Block et al, 1998), contraceptivo (Page et al, 1992), relaxante da musculatura lisa vascular aórtica de ratos (Tirapelli et al, 2004), até como agente antiinflamatório (Paiva et al, 2002).…”

Section: Introductionunclassified

Potencial antiinflamatório de Annona glabra, Annonaceae

Siebra¹,

Nardin²,

Florão³

et al. 2009

Rev. bras. farmacogn.

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RESUMO:Annona glabra Linneau, Annonaceae, é uma árvore de pequeno porte encontrada em todo território brasileiro, principalmente nas áreas costeiras e conhecida popularmente como araticum-do-brejo e araticum-bravo. Este trabalho teve como objetivos investigar os efeitos do extrato de A. glabra e do ácido caurenóico dele purificado sobre a migração de granulócitos humanos e seu potencial imunomodulatório. Os resultados demonstraram que o extrato de A. glabra inibe a migração natural de granulócitos, de acordo com a dose, sugerindo potencial antiinflamatório, enquanto o ácido caurenóico demonstrou estimulá-la de forma significativa. Em contraste, nenhum efeito foi observado com relação a imunomodulação. Os efeitos apresentados ainda não foram descritos e, dessa forma, contribuem para ampliar a lista de atividades biológicas descritas não só do extrato de A. glabra, como também para o ácido caurenóico.Unitermos: Annona glabra, Annonaceae, ácido caurenóico, leucócitos humanos, quimiotaxia, imunomodulação.ABSTRACT: "Anti-inflammatory potential of Annona glabra, Annonaceae". Annona glabra Linneau, Annonaceae, is a small tree that grows over the Brazilian territory particularly in its coast, and is known as "araticum-do-brejo" and "araticum-bravo". The aim of this study was to evaluate the effects of the extract of A. glabra and its purified kaurenoic acid on the locomotion of human granulocytes and their immunomodulatory potential. The results herein presented showed a dose-dependent inhibition of the granulocyte migration for the extract, suggesting an anti-inflammatory activity, in contrast with a striking stimulation observed for the kaurenoic acid. When focusing immunomodulation properties, no activity could be drawn. The effects presented in this work are reported for the first time and extend the list of biological activities already described for the A. glabra extract as well as for the kaurenoic acid.

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Analysis of the mechanisms underlying the vasorelaxant action of kaurenoic acid in the isolated rat aorta

Cited by 66 publications

References 22 publications

Hyphal Morphology and Elongation Alterations in <i>Aspergillus nidulans</i> Provoked by the Diterpene Kaurenoic Acid

Hyphal Morphology and Elongation Alterations in <i>Aspergillus nidulans</i> Provoked by the Diterpene Kaurenoic Acid

Endothelium-independent vasodilation induced by kolaviron, a biflavonoid complex from Garcinia kola seeds, in rat superior mesenteric arteries

Potencial antiinflamatório de Annona glabra, Annonaceae

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Analysis of the mechanisms underlying the vasorelaxant action of kaurenoic acid in the isolated rat aorta

Cited by 66 publications

References 22 publications

Hyphal Morphology and Elongation Alterations in &lt;i&gt;Aspergillus nidulans&lt;/i&gt; Provoked by the Diterpene Kaurenoic Acid

Hyphal Morphology and Elongation Alterations in &lt;i&gt;Aspergillus nidulans&lt;/i&gt; Provoked by the Diterpene Kaurenoic Acid

Endothelium-independent vasodilation induced by kolaviron, a biflavonoid complex from Garcinia kola seeds, in rat superior mesenteric arteries

Potencial antiinflamatório de Annona glabra, Annonaceae

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Product

Resources

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Hyphal Morphology and Elongation Alterations in <i>Aspergillus nidulans</i> Provoked by the Diterpene Kaurenoic Acid

Hyphal Morphology and Elongation Alterations in <i>Aspergillus nidulans</i> Provoked by the Diterpene Kaurenoic Acid