Kobayashi H, Endou K, Nakajima Y
Hokkaido Institute of Pharmaceutical Sciences, Japan.
Yakugaku Zasshi. 1994 Dec;114(12):1015-20. doi: 10.1248/yakushi1947.114.12_1015.
Using Staphylococcus aureus ISP447 strain, which shows inducible resistance to macrolide-lincosamide-streptogramin B (MLS) antibiotics, the extent of MLS-resistance induced by several macrolide antibiotics [erythromycin (EM), oleandomycin (OL), or roxithromycin (RXM)] was determined in terms of a relative ratio of a growth rate of the induced cells in the presence of a challenging drug, rokitamycin (RKM), to that of uninduced cells in the absence of RKM. The ratio was referred to as a relative inducibility (%). The inducibility was obtained at an optimum-induced condition by considering the following factors: (1) exponentially growing cells, (2) the optimum concentration of an inducer drug, i.e., 50, 150, and 150 ng/ml for EM, OL, and RXM, respectively, (3) a 3-h previous incubation at 37 degrees C in the presence of the inducer, and (4) 300 ng of RKM/ml, which is found to be optimum for induced cells to challenge, because of having no inducer activity. Using these qualification methods, inducibilities of EM, OL, and RXM as an inducer were 100.4, 27.9 and 81.1%, respectively. This method is allowed to be useful for the analysis of a structure-inducibility relationship.
使用对大环内酯-林可酰胺-链阳菌素B(MLS)抗生素表现出诱导抗性的金黄色葡萄球菌ISP447菌株,根据诱导细胞在存在挑战性药物罗他霉素(RKM)时的生长速率与未诱导细胞在不存在RKM时的生长速率的相对比率,测定了几种大环内酯抗生素[红霉素(EM)、竹桃霉素(OL)或罗红霉素(RXM)]诱导的MLS抗性程度。该比率称为相对诱导率(%)。通过考虑以下因素在最佳诱导条件下获得诱导率:(1)指数生长的细胞,(2)诱导剂药物的最佳浓度,即EM、OL和RXM分别为50、150和150 ng/ml,(3)在37℃下在诱导剂存在下预先孵育3小时,以及(4)300 ng RKM/ml,由于其没有诱导活性,被发现是诱导细胞进行挑战的最佳浓度。使用这些鉴定方法,EM、OL和RXM作为诱导剂的诱导率分别为100.4%、27.9%和81.1%。该方法可用于分析结构-诱导率关系。