第十一章 抗生素类药物的分析课件.pptVIP

第十一章 History of Antibiotics ~ 1495 Europeans Mercury ------ syphilis（梅毒） Chinese Moldy soybean curd ----- boils烫伤 American Indians Chewed bark of cinchona tree ---- malarial fever（疟疾） ??~ 1630 Europeans Quinine (bark of cinchona) ----- malaria 1877 Louis Pasteur Inhibition of some microbes by others 1908 Gelmo Synthesized sulfanilamide磺胺 (1st sulfonamide) ?1908-10 Paul Ehrlich Selective stains; Synthesized arsenic compound arsphenamine; (Nobel Prize) (606, Salvarsan) ----- syphilis (T. pallidum); Coined terms magic bullet, chemotherapy, chemical knife); 1928/9 Alexander Fleming Inhibition of S. aureus colonies by mold Penicillium notatum; (Nobel Prize) Discovered miracle drug penicillin ??1944/5 Selman Waksman Isolated streptomycin（氯霉素） from Streptomyces griseus (soil microbes); (Nobel Prize) Proposed term antibiotic = chemical compound made by a microorganism that inhibits or kills other microorganisms at low concentrations 1945 Florey Chain Reinvestigated, isolated and characterized penicillin; (Nobel Prize) Demonstrated practical clinical value as better means to prevent death from infection of war wounds A spore that drifted into his lab and took root on a culture dish started a chain of events that altered forever the treatment of bacterial infections Today, the penicillin class of antimicrobials? is a cornerstone of antibiotic therapy, and penicillin and its derivatives are some of the many broad-spectrum drugs available for physicians and others to prescribe. 青霉素类抗生素 抗菌作用： 革兰阳性菌：链球菌、葡萄球菌、破伤风、白喉、肺炎球菌、炭疽、消化链球菌； 革兰阴性球菌 ：脑膜炎球菌；淋球菌 嗜血杆菌属：百日咳杆菌、流感杆菌； 其 它：螺旋体。 作用机理：干扰细菌细胞壁的合成。 不良反应：毒性反应，变态反应，赫氏反应，二重感染。 头孢菌素类 优点：抗菌作用强，耐青霉素酶，临床疗效高，毒性低，过敏反应较青霉素少见。 [鉴别试验] 1. 官能团的显色反应 2. 光谱法 3. 色谱法 4. 生物学法 当抗生素在菌层培养基中扩散时，会形成抗生素浓度由高到低的自然梯度，即扩散中心浓度高而边缘浓度低。因此，当抗生素浓度达到或高于MIC（最低抑制浓度）时，试验菌就被抑制而不能繁殖，从而呈现透明的抑菌圈。根据扩散定律的推导，抗生素总量的对数值与抑菌圈直径的平方成线性关系。 一、 （二）手性C （三）共轭体系 （四）β–内酰胺环 二、 (四)色谱法 HPLC 比较供试品和对照品的保留时间(t)是否一致。 TLC 比较供试品和