COVID‑19 (Coronavirus disease 2019) is a contagious disease caused by the virus severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). Importantly, COVID-19 transmits when infectious particles are breathed in or come into contact with the eyes, nose, or mouth. Particularly, The symptoms of COVID-19 are variable but often include fever, cough, headache, fatigue, breathing difficulties, loss of smell, and loss of taste. Moreover, The virus is spreading rapidly and has greatly affected people’s lives. So, Given emerging variants from time to time, there is a pressing need for effective COVID-19 therapeutics.

Setomimycin is a potent antibiotic for the research of COVID‑19.

Setomimycin is a potent antibiotic and inhibits the SARS-CoV-2 Mpro enzyme with an IC₅₀ value of 12.02 µM. Besides, Setomimycin (0-100 µM; 44 h) shows antiproliferative activity with IC₅₀s of 11.45, >100, 48, 4.57 µM for A549; HOP-92; Panc-1; MiaPaca-2 cells, respectively. Furthermore, Setomimycin Setomimycin (0.01-1 µM) inhibits the release of cytokines IL-1β, IL-6, and TNF-α and nitric oxide release from LPS stimulated RAW 264.7 cells in a dose-dependent manner.

Setomimycin shows antimicrobial activity with MICs of 8, 4, 16, and 4 μg/mL for Staphylococcus aureus, Bacillus cereus, Bacillus subtilis, and Micrococcus luteus, respectively. Moreover, Setomimycin (0-100 µM; 5 days) shows antiproliferative activity and inhibits colony formation. In addition, Setomimycin (4, 5.5, 7 µM) decreases the protein expression of p-MEK, p-ERK, and Bcl-2, and increases the expression of Par-4 in a dose-dependent manner in MCF-7, HCT-116 cells. Moreover, Setomimycin (20 mg/kg; i.p.; alternate days for two weeks) shows antitumor activity in mice.

All in all, Setomimycin is a potent antibiotic and inhibits the SARS-CoV-2 Mpro enzyme. Besides, Setomimycin shows anti-inflammatory, antioxidant, antiproliferative, and antitumor activity.

Reference：

[1] Manhas RS, et al. Mol Divers. 2023 Apr;27(2):619-633.

[2] Manhas RS, et al. Chem Biol Interact. 2022 Sep 25;365:110093.