Rhodionin

Rhodionin is an orally active, multifunctional antivirulence and cytoprotective agent that targets and inhibits Lipase, sortase A (SrtA), CYP2D6 (IC₅₀=0.761 μM), AChE (IC₅₀=2.43-57.5 μM), and DPPH free radicals (IC₅₀=19.49 μM). Rhodionin is isolable from the roots of Rhodiola crenulata. Rhodionin reduces postprandial serum triglyceride levels in mice by inhibiting lipase activity. Rhodionin also binds directly to SrtA to inhibit its transpeptidase activity, thereby reducing the fibrinogen adhesion and surface protein A levels of MRSA, effectively inhibiting biofilm formation and protecting against MRSA-induced cell damage. Rhodionin improves the survival rate of infected mice without affecting MRSA growth, and finds wide application in studies related to hyperlipidemia, exogenous obesity, and pneumonia induced by methicillin-resistant Staphylococcus aureus (MRSA)^[1][2]. IC50 & Target:IC50: 0.761 μM (cytochrome P450 2D6)^[1]；57.50-2.43 μg/mL (AChE)^[2]；19.49 μM (DPPH free radical scavenging)^[3] In Vitro:Rhodionin (0-256 μg/mL; 1 h) potently inhibits the activity of purified recombinant SrtA ΔN59 protein with an IC₅₀ of 22.85 μg/mL, achieving 84.24% inhibition at 64 μg/mL^[2].
Rhodionin (64 μg/mL; 24 h) has no effect on the growth of S. aureus USA300, and its MIC against this strain is greater than 512 μg/mL^[2].
Rhodionin (16-128 μg/mL; 24 h viability, 5 h infection protection) is non-toxic to A549 cells at concentrations up to 128 μg/mL and provides dose-dependent protection against S. aureus USA300-induced A549 cell injury^[2].
Rhodionin (16-128 μg/mL) does not affect the expression of SrtA protein in S. aureus USA300 at concentrations up to 128 μg/mL^[2]. In Vivo:Rhodionin (150 mg/kg; p.o.; single dose) significantly reduces postprandial blood triglyceride elevation in olive oil-loaded mice, with a maximum suppression of 45.6% at 60 minutes after administration^[1].
Rhodionin (100 mg/kg; s.c.; every 12 hours) confers significant protection against MRSA-induced pneumonia in C57BL/6J mice, increasing the 96-hour survival rate to 50% while reducing bacterial load, pulmonary edema, and inflammatory responses^[2].