cox-2-in-41

COX-2-IN-41 (compound 5e) is a selective COX-2 inhibitor with an IC50 value of 1.74 μM. It demonstrates selectivity over COX-1, with a selectivity ratio of IC50(COX-1)/IC50(COX-2) = 16.32.

Etodolac (AY-24236) inhibits the activity of cyclooxygenase I and II, thereby preventing the formation of prostaglandin which is involved in the induction of pain, fever, and inflammation. Etodolac is a pyranocarboxylic acid and non-steroidal anti-inflammatory drug (NSAID) with antipyretic and analgesic activities. It also inhibits platelet aggregation by blocking platelet cyclooxygenase and the subsequent formation of thromboxane A2.

SARS-CoV-2 Mpro-IN-41 (Compound 7e) is an orally active inhibitor targeting COX-2 and SARS-CoV-2 Mpro, with respective IC50 values of 9.66 μM and 13.24 μM. It also demonstrates inhibitory activity against COX-1 (IC50: 46.11 μM). This compound significantly suppresses the expression of inflammation-related cytokines such as TNF-α, IL-6, and IL-1β, exhibiting anti-inflammatory properties. By selectively inhibiting COX-2 and SARS-CoV-2 Mpro, SARS-CoV-2 Mpro-IN-41 exerts both anti-inflammatory and antiviral effects, making it a potential candidate for research in inflammation and COVID-19 treatment.

Talaromyketide B is a polyketide compound identified in the soil bacterium Talaromyces sp. KYS-41, known for its anti-inflammatory properties. It inhibits the activation of NF-κB and MAPK signaling pathways and can dose-dependently suppress pro-inflammatory cytokines, such as IL-1β, IL-6, IL-10, and TNF-α, as well as the transcriptional activity of inflammatory mediators [including iNOS and COX-2]. Talaromyketide B shows promise for research in the fields of immunity and inflammatory diseases.