Tigecycline is a third-generation tetracycline-derived antibiotic [1]. Tigecycline binds to the bacterial 30S ribosomal subunit, blocking aminoacyl-tRNA binding to the ribosomal A site, thereby inhibiting protein synthesis [2]. Tigecycline exhibits broad-spectrum antibacterial activity against a variety of Gram-positive, Gram-negative, and anaerobic bacteria [3-4].
In GAM-016 cells, Tigecycline (1-10μM; 72h) inhibits the proliferation of gastric cancer cells in a dose-dependent manner [5]. In AsPC-1 cells, Tigecycline (1-40μM; 72h) inhibits the proliferation of cancer cells in a dose-dependent manner [6].
In C57BL/6J mice, Tigecycline (0-100mg/kg; ip; 5 weeks) effectively reduces excessive alcohol consumption in dependent and nondependent female and male mice [7]. In M. abscessus infection mouse model, inhaled Tigecycline (0.25-2.50mg; 50μL; aerosol therapy; 4 weeks) has potent antibacterial activity against M. abscessus [8].
References:
[1]. Rose W E, Rybak M J. Tigecycline: first of a new class of antimicrobial agents[J]. Pharmacotherapy: The Journal of Human Pharmacology and Drug Therapy, 2006, 26(8): 1099-1110.
[2]. Anandabaskar N. Protein synthesis inhibitors[M]//Introduction to basics of pharmacology and toxicology: volume 2: essentials of systemic pharmacology: from principles to practice. Singapore: Springer Nature Singapore, 2021: 835-868.
[3]. Slover C M, Rodvold K A, Danziger L H. Tigecycline: a novel broad-spectrum antimicrobial[J]. Annals of Pharmacotherapy, 2007, 41(6): 965-972.
[4]. Yaghoubi S, Zekiy A O, Krutova M, et al. Tigecycline antibacterial activity, clinical effectiveness, and mechanisms and epidemiology of resistance: narrative review[J]. European Journal of Clinical Microbiology & Infectious Diseases, 2022, 41(7): 1003-1022.
[5]. Tang C, Yang L, Jiang X, et al. Antibiotic drug tigecycline inhibited cell proliferation and induced autophagy in gastric cancer cells[J]. Biochemical and biophysical research communications, 2014, 446(1): 105-112.
[6]. Yang J, Dong Z, Ren A, et al. Antibiotic tigecycline inhibits cell proliferation, migration and invasion via down‐regulating CCNE2 in pancreatic ductal adenocarcinoma[J]. Journal of cellular and molecular medicine, 2020, 24(7): 4245-4260.
[7]. Bergeson S E, Nipper M A, Jensen J, et al. Tigecycline Reduces Ethanol Intake in Dependent and Nondependent Male and Female C57 BL/6J Mice[J]. Alcoholism: Clinical and Experimental Research, 2016, 40(12): 2491-2498.
[8]. Pearce C, Ruth M M, Pennings L J, et al. Inhaled tigecycline is effective against Mycobacterium abscessus in vitro and in vivo[J]. Journal of Antimicrobial Chemotherapy, 2020, 75(7): 1889-1894.
Tigecycline是第三代四环素类抗生素 [1]。Tigecycline与细菌核糖体30S亚基结合，阻断氨酰-tRNA与核糖体A位点的结合，从而抑制蛋白质合成 [2]。Tigecycline素对多种革兰氏阳性菌、革兰氏阴性菌和厌氧菌均具有广谱抗菌活性 [3-4]。
在GAM-016细胞中，Tigecycline（1-10μM；72h）以剂量依赖性方式抑制胃癌细胞增殖 [5]。在AsPC-1细胞中，Tigecycline（1-40μM；72h）以剂量依赖性方式抑制癌细胞增殖 [6]。
在C57BL/6J小鼠中，Tigecycline（0-100mg/kg；ip；5周）有效减少依赖性和非依赖性雌性和雄性小鼠的过量饮酒 [7]。在小鼠脓肿分枝杆菌感染模型中，吸入Tigecycline（0.25-2.50mg；50μL；气雾疗法；4周）对脓肿分枝杆菌具有强效抗菌活性 [8]。