Estévez M D, Vieytes M R, Botana L M
Departamento de Farmacología, Facultad de Veterinaria, Lugo, Spain.
Agents Actions. 1994 Oct;42(3-4):86-91. doi: 10.1007/BF01983470.
Adriamycin (ADR) induces nonimmunological and noncytotoxic histamine release from peritoneal and pleural rat mast cells. This secretion is unaffected by the pretreatment with pertussis toxin, cholera toxin and benzalkonium chloride. Histamine release induced by compound 48/80, was markedly inhibited by pertussis toxin, cholera toxin, benzalkonium chloride and neuraminidase. The ADR dose-response curve is significantly shifted to the right when cells were preincubated with the unspecific phosphodiesterase inhibitor IBMX. The activation of protein kinase C (PKC) with the phorbol esther TPA increases the response to ADR, while PKC inhibition with trifluoperazine decreases histamine release. The pretreatment of mast cells with okadaic acid did not modify the response to ADR. These results suggest that ADR elicits histamine release with a mechanism notably different from compound 48/80.
阿霉素(ADR)可诱导大鼠腹膜和胸膜肥大细胞释放非免疫性且无细胞毒性的组胺。这种分泌不受百日咳毒素、霍乱毒素和苯扎氯铵预处理的影响。化合物48/80诱导的组胺释放,受到百日咳毒素、霍乱毒素、苯扎氯铵和神经氨酸酶的显著抑制。当细胞与非特异性磷酸二酯酶抑制剂异丁基甲基黄嘌呤(IBMX)预孵育时,ADR剂量 - 反应曲线显著右移。用佛波酯TPA激活蛋白激酶C(PKC)可增加对ADR的反应,而用三氟拉嗪抑制PKC则会减少组胺释放。用冈田酸预处理肥大细胞不会改变对ADR的反应。这些结果表明,ADR引发组胺释放的机制与化合物48/80明显不同。