Adams E S, Rinehart K L
Roger Adams Laboratory, University of Illinois at Urbana-Champaign 61801.
J Antibiot (Tokyo). 1994 Dec;47(12):1456-65. doi: 10.7164/antibiotics.47.1456.
A new pactamycin analogue, 5"-fluoropactamycin, was prepared by directed biosynthesis. Supplementation of the fermentation medium of Streptomyces pactum, var. pactum with 3-amino-5-fluorobenzoic acid, an analogue of 3-aminobenzoic acid, an advanced precursor in pactamycin biosynthesis, resulted in co-production of pactamycin and the new pactamycin analogue. A similar feeding experiment with 3-amino-5-methylbenzoic acid did not result in formation of the corresponding methylated pactamycin analogue, but only in inhibition of pactamycin production. Comparison of antimicrobial and cytotoxic activities of pactamycin and 5"-fluoropactamycin showed no significant differences.
通过定向生物合成制备了一种新的派来霉素类似物5'-氟派来霉素。向派来链霉菌发酵培养基中添加3-氨基苯甲酸的类似物3-氨基-5-氟苯甲酸（派来霉素生物合成中的一种高级前体），导致派来霉素和新的派来霉素类似物共同产生。用3-氨基-5-甲基苯甲酸进行的类似补料实验未产生相应的甲基化派来霉素类似物，仅抑制了派来霉素的产生。派来霉素和5'-氟派来霉素的抗菌和细胞毒性活性比较显示无显著差异。
