Oroxylin A

Oroxylin A (CAS No.: 480-11-5) is a flavonoid derived from Oroxylum indicum and Scutellaria baicalensis, featuring multi-target regulatory properties. Its core therapeutic targets include signaling pathways such as NF-κB, MAPK, ERK1/2, Wnt/β-catenin, and PTEN/PI3K/Akt, as well as molecules like PPARγ, HDAC1, TKT, HIF-1α, caspases, MMP-2/-9, and VEGF. Its IC₅₀ values are cell line-dependent, ranging from 6.8 to 200 μM, with hepatocellular carcinoma cells (HepG2: 17.2~39.79 μM, SMMC-7721: 6.8~7.72 μM), colorectal cancer cells (HCT116: 25~200 μM), cervical cancer cells (HeLa: 19.4±0.7 μM), breast cancer cells (MDA-MB-231: 10~250 μM), and glioma cells (U251: 50 μM) being sensitive to it. The effective in vitro concentration is concentrated at 25~200 μM, and the in vivo therapeutic dose is 10~200 mg/kg (oral or intravenous injection) in mice, which can be used alone or in combination with 5-fluorouracil, cisplatin, etc. Its biological activities include anti-tumor effects (inducing tumor cell apoptosis, G1/S or G2/M phase arrest, inhibiting invasion, metastasis, and angiogenesis), anti-inflammatory effects (downregulating cytokines such as TNF-α and IL-6), neuroprotection, hepatoprotection, reversal of chemotherapy resistance (e.g., P-gp-mediated multidrug resistance), and low toxicity to normal cells (no significant killing at concentrations below 100 μM).

References:

[1] Sajeev A, Hegde M, Girisa S, Devanarayanan TN, Alqahtani MS, Abbas M, Sil SK, Sethi G, Chen JT, Kunnumakkara AB. Oroxylin A: A Promising Flavonoid for Prevention and Treatment of Chronic Diseases. Biomolecules. 2022 Aug 26;12(9):1185. doi: 10.3390/biom12091185. PMID: 36139025; PMCID: PMC9496116.

[2] Wang PX, Mu XN, Huang SH, Hu K, Sun ZG. Cellular and molecular mechanisms of oroxylin A in cancer therapy: Recent advances. Eur J Pharmacol. 2024 Apr 15;969:176452. doi: 10.1016/j.ejphar.2024.176452. Epub 2024 Feb 28. PMID: 38417609.