Setomimycin

Setomimycin is a potent antibiotic. Setomimycin inhibits the SARS-CoV-2 Mpro enzyme with an IC50 value of 12.02 µM. Setomimycin shows anti-inflammatory and antioxidant properties. Setomimycin shows antiproliferative and antitumor activity[1][2].

Research Areas >> Cancer

Research Areas >> Infection

Signaling Pathways >> Anti-infection >> SARS-CoV

Signaling Pathways >> Anti-infection >> Bacterial

IC50: 12.02 µM (SARS-CoV-2 Mpro)[1]

Setomimycin (0.01-1 µM) 以剂量依赖性方式抑制细胞因子 IL-1β、IL-6 和 TNF-α 的释放以及一氧化氮的释放在 LPS 刺激的 RAW 264.7 细胞中[1]。 Setomimycin (compound 1) 显示出抗菌活性，对 Staphylococcus aureus, Bacillus cereus, Bacillus subtilis, Micrococcus luteus 的 MIC 分别为 8、4、16、4 μg/mL [2]. Setomimycin (0-100 µM；5 天) 显示出抗增殖活性并抑制集落形成[2]。 Setomimycin (4, 5.5, 7 µM) 降低 p-MEK、p-ERK、Bcl-2 的蛋白表达，增加 Par-4 的表达[2]。 Cell Proliferation Assay[2] Cell Line: A549; HOP-92; Panc-1; MiaPaca-2 cells Concentration: 0-100 µM Incubation Time: 44 h Result: Showed antiproliferative activity with IC50s of 11.45, >100, 48, 4.57 µM for A549; HOP-92; Panc-1; MiaPaca-2 cells, respectively. Western Blot Analysis[2] Cell Line: MCF-7, HCT-116 cells Concentration: 4, 5.5, 7 µM Incubation Time: Result: Decreased the protein expression of p-MEK, p-ERK, Bcl-2, increased the expression of Par-4 in a dose-dependent manner.

Setomimycin (20 mg/kg；i.p.；隔天给药两周) 在小鼠体内显示出抗肿瘤活性[2]。 Animal Model: 6 weeks, 25-30 g, female BALB/c mice (4T1 cells)[2] Dosage: 20 mg/kg Administration: I.p.; every other day for two weeks Result: Decreased primary tumor weight (76%) and volume (90.5%).

[1]. Manhas RS, et al. Setomimycin as a potential molecule for COVID‑19 target: in silico approach and in vitro validation. Mol Divers. 2023 Apr;27(2):619-633.  

[2]. Manhas RS, et al. Isolation and anticancer activity evaluation of rare Bisaryl anthraquinone antibiotics from novel Streptomyces sp. strain of NW Himalayan region. Chem Biol Interact. 2022 Sep 25;365:110093.