Singh M P, Petersen P J, Jacobus N V, Maiese W M, Greenstein M, Steinberg D A
Natural Products Research Section, American Cyanamid Company, Pearl River, New York 10965.
Antimicrob Agents Chemother. 1994 Aug;38(8):1808-12. doi: 10.1128/AAC.38.8.1808.
The bioxalomycins, a novel complex of broad-spectrum antibiotics, were isolated from fermentations of Streptomyces viridodiastaticus subsp. "litoralis" LL-31F508. Bioxalomycin alpha 2, the major component of this complex, exhibited antibacterial activity. The MICs ranged from < or = 0.002 to 0.008 micrograms/ml for gram-positive organisms and from 0.50 to 4 micrograms/ml for gram-negative organisms. Bioxalomycin alpha 2 was found to be bactericidal and to inhibit bacterial DNA synthesis preferentially. Bioxalomycin alpha 2 protected mice from a lethal challenge with Staphylococcus aureus Smith. The 50% effective dose of bioxalomycin alpha 2 administered orally was 10 times greater than that when the drug was given subcutaneously or intravenously. These data suggest a stability or bioavailability problem when the compound is administered orally.
生物草霉素是一种新型的广谱抗生素复合物，从绿色产色链霉菌亚种“滨海链霉菌”LL - 31F508的发酵产物中分离得到。该复合物的主要成分生物草霉素α2具有抗菌活性。对革兰氏阳性菌的最低抑菌浓度（MIC）范围为≤0.002至0.008微克/毫升，对革兰氏阴性菌的MIC范围为0.50至4微克/毫升。发现生物草霉素α2具有杀菌作用，并优先抑制细菌DNA合成。生物草霉素α2可保护小鼠免受金黄色葡萄球菌史密斯菌株的致命攻击。口服生物草霉素α2的半数有效剂量比皮下或静脉给药时大10倍。这些数据表明该化合物口服时存在稳定性或生物利用度问题。
