Teicoplanin is a glycopeptide antibiotic of the vancomycin class obtained from fermentation by Actinoplanes teichomyceticus. Teicoplanin binds to the D-Ala-D-Ala terminus of peptidoglycan precursors to block cell wall cross-linking and inhibit cell wall synthesis of Gram-positive bacteria, and enhances antibacterial effects through its hydrophobic side chain interfering with lipid II and cell membrane permeability. Teicoplanin can be used in research on infective endocarditis, osteomyelitis, septicemia caused by drug-resistant Gram-positive bacteria such as MRSA, and Clostridium difficile-associated diarrhea[1-4].
In vitro, Teicoplanin (1nM-100μM) treated Vero cells infected with EBOV Zaire GP/HIV core pseudovirus for 72h. Teicoplanin dose-dependently inhibited pEBOV infection with CC50>125μM[5]. Teicoplanin (130, 520, 890μg/mL) treated MCF-7 human breast cancer cells for 68h. Teicoplanin downregulated the mRNA expression of c-myc and c-fos in cells[6].
In vivo, Teicoplanin (1-120mg/kg; 4, 6, 8, 12, 24h intervals; 5 doses total) was intravenously administered 2h post-inoculation to cyclophosphamide-induced neutropenic mice with thigh Staphylococcus aureus infection (MSSA ATCC 29213 or MRSA ATCC 43300) for 24h treatment. Teicoplanin inhibited S. aureus burden growth in mouse thigh tissues[7]. Teicoplanin (100, 200, 500μg; single injection) was intracerebroventricularly injected (4μL/mouse; within 4min) into male ICR mice (5-6 weeks old; 25-30g). Teicoplanin induced behavioral seizures such as head twitching and forelimb clonus, accompanied by high-voltage polyspike waves in frontal cortex, hippocampus and amygdala[8].
References:
[1] Shea KW, Cunha BA. Teicoplanin. Med Clin North Am. 1995 Jul;79(4):833-44. doi: 10.1016/s0025-7125(16)30042-6.
[2] Parenti F, Schito GC, Courvalin P. Teicoplanin Chemistry and Microbiology. J Chemother. 2000 Nov;12 Suppl 5:5-14.
[3] Yushchuk O, Ostash B, Truman AW, et al. Teicoplanin biosynthesis: unraveling the interplay of structural, regulatory, and resistance genes. Appl Microbiol Biotechnol. 2020 Apr;104(8):3279-3291.
[4] Greenwood D. Microbiological properties of teicoplanin. J Antimicrob Chemother. 1988 Jan;21 Suppl A:1-13.
[5] Wang Y, Cui R, Li G, et al. Teicoplanin inhibits Ebola pseudovirus infection in cell culture. Antiviral Res. 2016 Jan;125:1-7.
[6] Ashouri S, Khujin MH, Kazemi M, et al. Effect of teicoplanin on the expression of c-myc and c-fos proto-oncogenes in MCF-7 breast cancer cell line. Adv Biomed Res. 2016 Nov 28;5:172.
[7] Watanabe E, Matsumoto K, Ikawa K, et al. Pharmacokinetic/pharmacodynamic evaluation of teicoplanin against Staphylococcus aureus in a murine thigh infection model. J Glob Antimicrob Resist. 2021 Mar;24:83-87.
[8] Takechi K, Ishikawa T, Kamei C. Epileptogenic activity induced by teicoplanin and effects of some antiepileptics in mice. J Pharmacol Sci. 2008 Aug;107(4):428-33.