**Background**
Serious infections caused by Gram-positive bacteria, particularly Methicillin-resistant Staphylococcus aureus (MRSA) and Enterococcus aureus, pose significant challenges to global healthcare due to increasing antibiotic resistance. Beyond bacterial pathogens, the emergence of viral threats such as HIV-1 and coronaviruses (SARS-CoV-1 and SARS-CoV-2) has highlighted the need for therapeutic agents with broad-spectrum activity. Recent research has explored the repurposing of existing antibiotics to target viral entry mechanisms, specifically by inhibiting host proteases required for viral release. In this context, we will introduce a glycopeptide antibiotic with both antibacterial and antiviral properties – Teicoplanin.
**Definition**
Teicoplanin is a glycopeptide antibiotic derived from the microorganism Actinoplanes teichomyceticus that targets the bacterial cell wall and exhibits antiviral activity against several pseudotyped viruses.
**In Vitro and In Vivo Studies**
According to the Teicoplanin description, this compound functions as a glycopeptide that inhibits the bacterial cell wall. In terms of Teicoplanin biological activity, it has demonstrated significant antiviral potential. Teicoplanin in vitro studies showed that the compound inhibits HIV-1 in human CEM cell cultures with an $\text{EC}_{50}$ value of $17\text{ }\mu\text{M}$. Furthermore, in HEK293T cells and A549 cells, it exhibited $\text{IC}_{50}$ values of $0.39\text{ }\mu\text{M}$ for HIV-luc/SARS-CoV-S pseudotyped viruses and $1.66\text{ }\mu\text{M}$ for 2019-nCoV-Spike-pseudoviruses, respectively, while the $\text{IC}_{50}$ for SARS-CoV-2 in Vero E6 cells was $15.7\text{ }\mu\text{M}$. The mechanism involves the inhibition of cathepsin L protease via the interaction of the teicoplanin lipophilic moiety with the enzyme, thereby stopping the release of SARS-CoV from the late endosome. Regarding its antibacterial properties, Teicoplanin shows anti-MRSA activity with a minimum inhibitory concentration (MIC) of $0.5\text{ mg/L}$ in MRSA ATCC 43300.
Teicoplanin In Vivo research utilized a murine MRSA thigh infection model (Male CD1 mice, 20-30 g, infected with $2 \times 10^6\text{ cfu/mL}$ MRSA 43300). Administration of Teicoplanin (10, 30 mg/kg; i.v.; once every 12 h) resulted in a dose-dependent decline in total bacterial density. A total bactericidal effect was achieved at dosages $\ge 10\text{ mg/kg/day}$, and suppression of resistance was observed at dosages $\ge 30\text{ mg/kg/day}$. In conclusion, Teicoplanin is a versatile glycopeptide antibiotic effective against resistant Gram-positive bacteria and various viral strains.
Keywords
Teicoplanin, 61036-62-2, Antibiotic MDL-507, MDL-507, Antibiotic MDL507, Antibiotic MDL 507, MDL507, MDL 507, Bacterial, Antibiotic, Inhibitor, inhibitor, inhibit
References
[1] Vimberg V. Teicoplanin-A New Use for an Old Drug in the COVID-19 Eral Pharmaceuticals (Basel). 2021 Nov 26;14(12):1227.
[2] Ramos-MartÃn V, et al. Pharmacodynamics of teicoplanin against MRSA. J Antimicrob Chemother. 2017 Dec 1;72(12):3382-3389.