Riehle M, Bereiter-Hahn J, Boller B
Cinematic Cell Research Group, Johann Wolfgang Goethe-Universität, Frankfurt/Main, Fed. Rep. of Germany.
Arzneimittelforschung. 1991 Apr;41(4):378-84.
The effect of digitoxin (CAS 71-63-6) and ouabain (g-strophantin, CAS 630-60-4) on respiration, morphology and beating activity of cardiomyocytes in culture derived from embryonic chick hearts has been investigated. The drugs were applied in a perfusion system using a protein- and substrate-free perfusion medium (BSS) at two concentration of K+ (5.4 and 4 mmol/l). In either K+ concentration oxygen consumption was 0.13 +/- 0.05 nmol O2 h-1 per 1000 cells. During 3 h of perfusion with BSS oxygen consumption declines only slightly to 79 +/- 15% of the initial value. No relation was found between beating frequency and oxygen consumption. Increase in respiration ranged from 5 to 45% and lasted between 5 and 120 min. At concentrations being inhibitory to the Na+/K(+)-ATPase (greater than or equal to 1 mumol/l) ouabain stimulated respiration by about 20% at 4 mmol/l K+ and 10% at 5.4 mmol/l K+ while digitoxin was effective at 5.4 mmol/l only (a transient increase of 20%). At 0.1 nmol/l, (a concentration below the KD of the high affinity binding site of the Na+/K(+)-ATPase) ouabain caused a long lasting activation of respiration by about 30%, digitoxin induced a transient rise of up to 20% at 5.4 mmol/l K+. At 4 mmol/l K+ digitoxin did not affect respiration while ouabain caused a transient increase. The lowest concentration of ouabain inducing a reproducible activation of oxygen consumption was 0.1 pmol/l. At this concentration digitoxin was no longer effective. At 1 fmol/l respiration was stimulated only occasionally.(ABSTRACT TRUNCATED AT 250 WORDS)
研究了洋地黄毒苷（CAS 71-63-6）和哇巴因（g-毒毛旋花子苷，CAS 630-60-4）对源自胚胎鸡心脏的培养心肌细胞的呼吸、形态和搏动活性的影响。在使用无蛋白和无底物灌注培养基（BSS）的灌注系统中，于两种钾离子浓度（5.4和4 mmol/L）下应用这些药物。在任一钾离子浓度下，每1000个细胞的耗氧量为0.13±0.05 nmol O₂ h⁻¹。在用BSS灌注3小时期间，耗氧量仅略有下降至初始值的79±15%。未发现搏动频率与耗氧量之间存在关联。呼吸增加范围为5%至45%，持续时间为5至120分钟。在对Na⁺/K⁺-ATP酶具有抑制作用的浓度（≥1 μmol/L）下，哇巴因在4 mmol/L钾离子时刺激呼吸约20%，在5.4 mmol/L钾离子时刺激10%，而洋地黄毒苷仅在5.4 mmol/L时有效（短暂增加20%）。在0.1 nmol/L（低于Na⁺/K⁺-ATP酶高亲和力结合位点的KD的浓度）时，哇巴因引起呼吸的长期激活约30%，洋地黄毒苷在5.4 mmol/L钾离子时诱导短暂升高高达20%。在4 mmol/L钾离子时，洋地黄毒苷不影响呼吸，而哇巴因引起短暂增加。诱导耗氧量可重复激活的哇巴因最低浓度为0.1 pmol/L。在此浓度下，洋地黄毒苷不再有效。在1 fmol/L时，呼吸仅偶尔受到刺激。（摘要截断于250字）
