Lipid-lowering agent-1

Lipid-lowering agent-1 is a potent lipid-lowering agent. Lipid-lowering agent-1 has significant pharmacological effects on the inhibition of low-density lipoprotein cholesterol (LDLC) and promotion of high-density lipoprotein cholesterol (HDLC) production. Lipid-lowering agent-1 shows potent hypolipidemic effect in high-fat diet rats[1].

Research Areas >> Others

Signaling Pathways >> Others >> Others

Lipid-lowering agent-1 (compound 1m) (12.5 μM; 72 hours) does not exhibit significant toxicity to both HepG2 and 3T3-L1 cells at a high concentration[1]. Lipid-lowering agent-1 (10 μM; 24 hours) has significant pharmacological effects on the inhibition of LDLC and promotion of HDLC production[1]. Lipid-lowering agent-1 (10 μM; 24 hours) inhibits the conversion of 3T3-L1 cells from pre-adipose to adipose-like with the inhibition of triglycerides (TG) by 70.4%[1]. Lipid-lowering agent-1 (10 μM; 10 days) decreases yellow lipid droplets effectively in 3T3-L1 cells[1]. Cell Cytotoxicity Assay Cell Line: HepG2 and 3T3-L1[1] Concentration: 12.5 μM Incubation Time: 72 hours Result: Did not exhibit significant toxicity to both HepG2 and 3T3-L1 cells at a high concentration. Cell Differentiation Assay Cell Line: 3T3-L1 cells[1] Concentration: 10 μM Incubation Time: 24 hours Result: Inhibited the conversion of 3T3-L1 cells from pre-adipose to adipose-like with the inhibition of triglycerides (TG) by 70.4%

Lipid-lowering agent-1 (15 mg/kg; i.g., daily for 40 or 80 days) reduces blood cholesterolby, triglycerides and LDLC by 19.6%, 34.52%, and 41.49% after dosing 40 days, moreover the three indexes is still better than that of berberine after dosing 80 days[1]. Animal Model: High-fat diet (HFD) rats[1] Dosage: 15 mg/kg Administration: i.g., daily for 40 or 80 days Result: Reduced blood cholesterolby, triglycerides and LDLC by 19.6%, 34.52%, and 41.49% after dosing 40 days, moreover the three indexes was still better than that of berberine after dosing 80 days.

[1]. Kong Y, et al. Discovery and structural optimization of 9-O-phenylsulfonyl-berberines as new lipid-lowering agents. Bioorg Chem. 2022;121:105665.