Kim S H, Kim J H, Alfieri A A, He S Q, Young C W
Cancer Res. 1985 Dec;45(12 Pt 1):6338-40.
Gossypol, a polyphenolic aldehyde extracted from cotton plants, is a potent antifertility agent in humans. Since we have previously reported that several male antifertility agents including 5-thio-D-glucose and lonidamine demonstrate hyperthermic sensitizing effects in HeLa cells, we wished to determine whether gossypol also exhibits the hyperthermic sensitization. Gossypol was not cytotoxic up to 4 h at 37 degrees C (10 micrograms/ml). When HeLa cells were exposed to gossypol at 41 degrees and 42 degrees C, significant potentiation of hyperthermia induced cytotoxicity was observed. The magnitude of the potentiation was dependent on the drug concentration, pH of the culture medium, glucose concentration, temperature, and duration of treatment. The hyperthermic sensitizing effect of gossypol was increased by an acidic pH and glucose deprivation. These data suggest that the sensitizing effect of the drug may be mediated through the lowering of cellular energy level by the inhibition of both glycolysis and oxidative phosphorylation.
棉酚是从棉花植物中提取的一种多酚醛，对人类是一种有效的抗生育剂。由于我们之前报道过几种男性抗生育剂，包括5-硫代-D-葡萄糖和氯尼达明，在HeLa细胞中表现出热敏化作用，我们希望确定棉酚是否也表现出热敏化作用。在37摄氏度（10微克/毫升）下，长达4小时棉酚没有细胞毒性。当HeLa细胞在41摄氏度和42摄氏度下暴露于棉酚时，观察到热诱导细胞毒性的显著增强。增强的程度取决于药物浓度、培养基的pH值、葡萄糖浓度、温度和处理持续时间。酸性pH值和葡萄糖剥夺会增强棉酚的热敏化作用。这些数据表明，该药物的敏化作用可能是通过抑制糖酵解和氧化磷酸化来降低细胞能量水平介导的。
