课件：第三十七章章：内酰胺类抗生素和其他作用于细胞壁的抗生素.ppt

English: Diagram depicting the action of the antibiotic vancomycin and one way bacteria have evolved resistance to it. Background: The bacterial cell wall consists of strands of repeating N-acetylglucosamine (NAG) and N-acetylmuramic acid (NAM) subunits. The NAM subunits have short peptide chains attached to them. (The exact composition of these can vary. The proximal alanine is usually L-ala and the distal two are usually D-ala.) These peptide chains are involved in forming cross-links between the strands of the cell wall. These cross-links are essential to a functioning cell wall. 1. Vancomycin is added to the bacterial environment while it is trying to synthesize new cell wall. Here, the cell wall strands have been synthesized, but not yet cross-linked. 2. Vancomycin recognizes and binds to the two D-ala residues on the end of the peptide chains. However, in resistant bacteria, the last D-ala residue has been replaced by a D-lactate, so vancomycin cannot bind. 3. In resistant bacteria, cross-links are successfully formed. However, in the non-resistant bacteria, the vancomycin bound to the peptide chains prevents them from interacting properly with the cell wall cross-linking enzyme. 4. In the resistant bacteria, stable cross links are formed. In the sensitive bacteria, cross-links cannot be formed and the cell wall falls apart * sepsis 英 [?seps?s] 美 [seps?s] n. 脓毒病; 脓毒疾 * * Furosemide Gentamicin ototoxicity 英 [??t??t?ks?s?t?] 美 [o?to?t?ks?s?t?] [释义] 耳毒性 phlebitis 英 [fl??ba?t?s] 美 [fl?ba?t?s] n. 静脉炎 * * * * * * 炭疽杆菌（Bacillus anthraci）白喉杆菌(Corynebacterium diphtheriae) * * * * * * * 流感嗜血杆菌是一种没有运动力的革兰氏阴性杆菌 * * * * * * * * * 含有甲基四氮唑侧链结构的头孢菌素可干扰维生素K在体内的循环，增加出血倾向。所有的广谱头孢菌素均可因抑制肠道细菌而使维生素K的合成减少而影响凝血功能。 * * * * * * * * PBP-3对细菌细胞中隔形成和细菌分裂有重要作用 * * * 头孢菌素类 cephalosporins 青霉素 头孢菌素 A)侧链 B)?-内酰胺环 C)噻唑烷环 A)侧链 B) ? - 内酰胺环 C)二氢噻嗪环 D)在3位基团 A B C A B C D 6-APA 7-ACA 7-氨基头孢烷酸 * 特点 抗菌谱广 抗菌作用强 耐青霉素酶，不易耐药 临床疗效高，部分口服 毒性低，较安全，90% penicillin 过敏者可用 价格昂贵，除口服制剂不作首选 * 头孢菌素类抗生素的体外抗菌活性 分