Pouillart P, Ronco G, Cerutti I, Chany C, Villa P
Laboratoire de Chimie Organique et Cinétique, UFR des Sciences, Université de Picardie, Amiens, France.
J Biol Regul Homeost Agents. 1990 Oct-Dec;4(4):135-41.
This study compares the antitumor activity of five mono- and polyesters of n-butyric acid derived from monosaccharides in the murine model of Crocker 180 TG Sarcoma. Tumor incidence at ten days, mean survival time and final survival rate were significantly affected in all cases. Combined treatment by butyric esters, alpha/beta interferon (IFN) and/or Corynebacterium parvum used as immunestimulator improved the antitumor protection. Studies of acute toxicity in mice, performed by i.p. and oral routes, showed the low toxicity of butyric esters, which were devoid of detectable side effects with no incidence on ponderal growth when administered per os in rats daily for one month. Finally, a comparative study of antitumor activity, toxicity and water-solubility of various butyric esters enabled us to select among these new molecules two isomers (carbon-3 and carbon-6 of the glucose ring substituted with n-butyric acid) derived from monoacetone glucose for further investigations of their biological mechanism in vivo and in vitro.
本研究在克罗克180 TG肉瘤小鼠模型中比较了五种由单糖衍生的正丁酸单酯和聚酯的抗肿瘤活性。在所有情况下，第10天的肿瘤发生率、平均存活时间和最终存活率均受到显著影响。丁酸酯、α/β干扰素（IFN）和/或用作免疫刺激剂的短小棒状杆菌联合治疗可提高抗肿瘤保护作用。通过腹腔注射和口服途径对小鼠进行的急性毒性研究表明，丁酸酯毒性低，口服给予大鼠一个月，未发现可检测到的副作用，对体重增长无影响。最后，对各种丁酸酯的抗肿瘤活性、毒性和水溶性进行的比较研究使我们能够从这些新分子中选择两种由单丙酮葡萄糖衍生的异构体（葡萄糖环的碳-3和碳-6被正丁酸取代），以进一步研究其体内和体外的生物学机制。
