Catalpol exhibits a range of biological activities. It demonstrates antiproliferative effects against various human cell lines, including A2780, HBL100, HeLa, SW1573, T47D, and WiDr, with a GI50 value exceeding 100,000.0 nM for all tested lines based on the SRB assay results, suggesting limited cytotoxic effects at these concentrations. Additionally, it displays significant antihyperglycemic effects in streptozotocin-induced diabetic Wistar rats by reducing plasma glucose levels, with reductions of 24.33% at 0.1 mg/kg dosage and 8.53% at 0.01 mg/kg dosage.
In terms of insecticidal activity, Catalpol is effective against Tribolium castaneum larvae, showing a pupal stage duration of 8.2 days and a mortality rate of 73.3% at 60 ug/uL. It also exhibits antifeedant activities such as a relative growth rate of -0.01 mg/mg/day and a relative consumption rate of 0.017 mg/mg/day at 200 ug/disk, along with an efficiency of conversion of ingested food of -66.1%.
Catalpol inhibits Thermus aquaticus-DNA polymerase with an IC50 of 47800.0 nM and shows activity in a qHTS assay for GCN5L2 inhibitors with a potency of 39810.7 nM. It possesses estrogenic activity in human MVLN cells, with activity levels of 54.03% at 100 ug/mL and 75.78% at 20 ug/mL compared to estradiol. The compound shows moderate inhibitory activity against COX1 (44.2%-63.7%) and weak inhibitory action against COX2 (less than 30%).
Additionally, Catalpol exhibits hepatoprotective activity against APAP-induced toxicity in human HepG2 cells, resulting in a 69.1% cell survival rate, and demonstrates inhibition of LPS-induced NO production in mouse BV2 cells with an IC50 of 7300.0 nM. It also shows cytotoxicity against mouse BV2 cells (86.1% activity) and various human cell lines (e.g., A2780, BGC823, HT-29, A549, and Bel7402) with IC50 values greater than 10,000.0 nM..
Note: Summary generated by AI. Data source: ChEMBL 