Leonurine

SKU: orb1225528

Description

Leonurine (SCM-198) is a natural alkaloid that exhibits cardio-and neuronal-protective effects both in vitro and in vivo, occupies the caspase recruitment site of Apaf-1, blocks its interaction with procaspase-9; attenuates doxorubicin-induced apoptosis in H9c2 cardiac muscle cells, protects middle cerebral artery occluded rats through antioxidant effect and regulation of mitochondrial function, attenuates myocardial fibrotic response via inhibition of NADPH oxidase 4 (Nox4).

Key Properties

• CAS Number: 24697-74-3
• MW: 311.338
• Purity: >98% (HPLC)
• Formula: C₁₄H₂₁N₃O₅
• SMILES: O=C(OCCCCNC(N)=N)C1=CC(OC)=C(O)C(OC)=C1
• Target: Apaf-1
• Solubility: DMSO : 6 mg/mL 19.27 mM

Bioactivity

• In Vivo:
  Leonurine (10 mg/kg/d, p.o.) significantly increases the expressions of PPARγ, LXRα, ABCA1 and ABCG1, and decreases both TG and TC levels in serum of mice. Leonurine hydrochloride (50, 100, 200 mg/kg) improves intracellular lipid accumulation via activating AMPK/SREBP1 pathway, enhances biochemical parameters, reduces hepatic lipoperoxide and increases antioxidant levels in mice. Leonurine (20 mg/kg, p.o.) ameliorates osteoarthritis development in mouse DMM model.
• In Vitro:
  Leonurine (0, 5, 10, 20, 40, 80 μM) causes diminution in lipid accumulation, cellular cholesterol content, including total cholesterol (TC), free cholesterol (FC) and cholesteryl ester (CE), and increase in apoA-I- or HDL-mediated cholesterol efflux after treatment for 24 h. Leonurine also significantly and dose-dependently increases the expressions of ABCA1 and ABCG1 at the mRNA and protein levels in human THP-1 macrophages, and such effect is involved in PPARγ. Leonurine hydrochloride (LH) shows protective effect on cell viability of HepG2 and HL-7702 cells incubated with palmitic acid (PA) of free fatty acid (FFA) for 24 h. Leonurine hydrochloride (125, 250, 500 μM) improves cellular lipid accumulation in HepG2 and HL-7702 cells via activating AMPK/SREBP1 pathway. Leonurine (5, 10, 20 μM) inhibits the expression of iNOS, COX-2, PGE2, NO, TNF-α, and IL-6 in IL-1β-induced human chondrocytes, suppresses ECM degradation in human OA chondrocytes, and blocks IL-1β-induced PI3K and Akt phosphorylation in a dose-dependent manner.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SCM-198

Quick Database Links

Gene Symbol

Apaf-1