VZL 2008, 77(4):160-168

Cardiotoxic Glycosides

Jiří Patočka ORCID...
Katedra radiologie a toxikologie Zdravotně sociální fakulty Jihočeské univerzity, České Budějovice

Kardioaktivní steroidy se nacházejí v rostlinách, živočiších a hmyzu. Kardioaktivní glykosidy se váží na Na+-K+-ATPázu kterou inhibují, což vede k regulaci koncentračního gradientu Na+ a K+ na plazmatické membráně zvané sarkolema. Po více než 200 let sloužily kardioaktivní glykosidy pro svůj pozitivně inotropní účinek v terapii selhávajícího srdce. Současný pohled na jejich účinek je, že inhibice Na+-K+-ATPázy vede ke zvýšení [Na+]i a následnému zvýšení koncentrace kalcia v buňce a sarkoplazmatickém retikulu. Jejich afinita k Na+-K+ ATPáze je ovlivněna typem laktonu na uhlíku 17 steroidní kostry: ty s pětičlenným laktonovým kruhem, zvané kardenolidy, jsou rostlinného původu, ty s šestičlenným laktonovým kruhem, zvané bufadienolidy, jsou většinou živočišného původu.

Keywords: Kardiotoxiké glykosidy; Kardioaktivní steroidy; Kardenolidy; Bufadienolidy; Chemie; Toxikologie

Cardioactive steroids are found in plants, animals, and insects. Cardioactive glycosides selectively bind to and inhibit the Na+-K+-ATPase, which regulates the trans-sarcolemmal Na+ and K+ concentration gradients. Cardioactive glycosides have been important in treating congestive heart failure for more than 200 years, in large part because of a positive inotropic effect. The now traditional view is that direct Na+-K+-ATPase inhibition leads to elevation of [Na+]i with consequent gain of cellular and sarcoplasmic reticulum [Ca2+]. Their affinity for Na+-K+-ATPase is influenced by the type of lactone at carbon 17 (C17) of the steroid backbone: those with 5-membered lactone rings, or cardenolides, are derived mostly from plants with those 6-membered rings from animals with bufadienolides.

Keywords: Cardiotoxic glycosides; Cardiotoxic steroids; Cardenolides; Bufadienolides; Chemistry; Toxicology

Received: January 31, 2008; Published: December 1, 2008  Show citation

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Patočka, J. (2008). Cardiotoxic Glycosides. Vojenské Zdravotnické Listy77(4), 160-168
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