Oki T, Tenmyo O, Hirano M, Tomatsu K, Kamei H
Bristol-Myers Research Institute, Ltd., Tokyo Research Center, Japan.
J Antibiot (Tokyo). 1990 Jul;43(7):763-70. doi: 10.7164/antibiotics.43.763.
Pradimicins A, B and C specify novel antibiotics produced by Actinomadura hibisca No. P157-2 (ATCC 53557) possessing potent and broad antifungal activity in vivo. They showed moderate in vitro antifungal activity against a wide variety of fungi and yeasts including clinically important pathogens, and were highly effective in systemic infection with Candida albicans in mice after iv and im administrations. Pradimicin A showed in vivo therapeutic activity against C. albicans, Cryptococcus neoformans and Aspergillus fumigatus in both normal and immunocompromized mice. 5-Fluorocytosine- and azole-resistant C. albicans strains were susceptible to pradimicin A. This antibiotic also demonstrated therapeutic efficacy against lung candidiasis and aspergillosis, vaginal candidiasis and skin Trichophyton mentagrophytes infection in mice with iv or topical treatment. The LD50 values after a single iv or im administration were 120 mg/kg and more than 400 mg/kg, respectively. Against various cultured mammalian cells, pradimicin A was noncytotoxic at 100 or 500 micrograms/ml, and showed potent anti-influenza virus activity with an IC50 value of 6.8 micrograms/ml.
普拉地米星A、B和C是由 hibisca 马杜拉放线菌P157-2号菌株（ATCC 53557）产生的新型抗生素，在体内具有强大且广泛的抗真菌活性。它们对包括临床重要病原体在内的多种真菌和酵母表现出中等程度的体外抗真菌活性，并且在静脉注射和肌肉注射后，对小鼠白色念珠菌全身感染具有高效。普拉地米星A在正常和免疫受损小鼠体内均对白色念珠菌、新型隐球菌和烟曲霉表现出治疗活性。对5-氟胞嘧啶和唑类耐药的白色念珠菌菌株对普拉地米星A敏感。这种抗生素在静脉注射或局部治疗的小鼠中，对肺部念珠菌病和曲霉病、阴道念珠菌病以及皮肤须癣毛癣菌感染也显示出治疗效果。单次静脉注射或肌肉注射后的半数致死量（LD50）值分别为120毫克/千克和超过400毫克/千克。对于各种培养的哺乳动物细胞，普拉地米星A在100或500微克/毫升时无细胞毒性，并且显示出强大的抗流感病毒活性，半数抑制浓度（IC50）值为6.8微克/毫升。
