Quinestrol demonstrates a variety of bioactivities, exhibiting potency as a modulator of Lamin A splicing at 112.2 nM and cytotoxicity against pathogens like Streptococcus, SK(-)GAS Group A Streptococcus, and Trypanosoma cruzi with EC50 values from 1941.0 nM to 4431.0 nM. It inhibits targets such as Tau fibril formation, Mycobacterium tuberculosis, influenza NS1 protein function, human alpha-glucosidase, BAZ2B, USP1/UAF1, and FEN1 with potencies between 35480.0 nM and 79432.8 nM. Additionally, it induces DNA re-replication, promotes mRNA translation, and regulates enzymatic functions.
Moreover, Quinestrol shows significant estrogenic activities:
- In immature rats, it exhibits an estrogenic activity ratio of 1.66 relative to ethynylestradiol.
- Induces vaginal cornification in ovariectomized mature rats at 0.005 to 0.010 mg/kg orally, with 40.0% activity relative to control.
- Displaces 17beta-[3H]estradiol from rabbit uterine estrogen receptor with an IC50 of 6000.0 nM and a relative ratio to ethynylestradiol of 0.00004.
In spayed Wistar rats, Quinestrol shows uterotrophic activity with uterus weights of 39.0 mg after 1 week and 29.0 mg after 2 weeks at a 0.1 µmol oral dosage.
Its antiviral properties include:
- Inhibition of SARS-CoV-2 induced cytotoxicity in Caco-2 cells at 10 µM with 4.68% inhibition after 48 hours.
- Moderate efficacy against SARS-CoV-2 (USA-WA1/2020 strain) in HRCE cells, with a hit score of 0.3887 after 96 hours.
- Inhibition of the SARS-CoV-2 3CL-Pro protease at 20 µM with an inhibition percentage of -0.2126%.
- Inhibition of cytotoxicity in VERO-6 cells with 0.14% inhibition at 10 µM after 48 hours of exposure.
The compound also displays high binding affinity towards multiple receptors, including human NPY1R, CNR1, AVPR1A, AVPR2, BDKRB2, GHSR, NR3C1, AGTR1, CCKAR, MC3R, MC4R, and others, with AC50 values exceeding 10000.0 nM. Agonist activity at human PGR is observed with an AC50 of 221.0 nM, along with antagonist activity at receptors like CHRM2, HTR1A, ADRA2A, HTR2A, and HTR2B with AC50 values above 10000.0 nM. It also inhibits enzymes PTGS2, PDE4D, PDE3A, and MAOA in cell-free assays with AC50 values surpassing 10000.0 nM..
Note: Summary generated by AI. Data source: ChEMBL 