5,7,3',4'-Tetramethoxyflavone

5,7,3',4'-Tetramethoxyflavone, an orally active polymethoxyflavones (PMFs) that can be isolated from M. exotica, possesses various bioactivities, including anti-fungal, anti-malarial, anti-mycobacterial, and anti-inflammatory activities. 5,7,3',4'-Tetramethoxyflavone exhibits chondroprotective activity by targeting β-catenin signaling^[1]. In Vitro:5,7,3',4'-Tetramethoxyflavone (5-20 μg/mL, 24 h) inhibits the expression of EP2, EP4, bcatenin and COX-2 gene in chondrocytes^[1].
5,7,3',4'-Tetramethoxyflavone (5-20 μg/mL, 48 h) inhibits the protein expression of EP/cAMP/PKA signaling pathway and β-catenin signaling pathway in chondrocytes^[1].
5,7,3',4'-Tetramethoxyflavone (5-20 μg/mL, 4 h) protects chondrocytes from apoptosis through regulating IRE1α^[2].
5,7,3',4'-Tetramethoxyflavone (5-20 μg/mL, 4 h) reverses the expression pattern of endoplasmic reticulum (ER) stress genes due to IRE1α deficiency^[2].
In Vivo:5,7,3',4'-Tetramethoxyflavone (25-100 mg/kg, i.g.) exhibits chondroprotective activity in rats^[1].
5,7,3',4'-Tetramethoxyflavone (5-20 mg/kg; i.v., p.o.) has the absolute bioavailability of 14.3 % in rats^[3].

Pharmacokinetic Analysis in Sprague-dawley Rats Model^[3]

Route	Dose (mg/kg)	AUC (min μg/mL)	AUC/Dose (min/mL)	t1/2 (h)	Tmax (h)	Cmax (ng/mL)	Bioavailability (%)
i.v.	5	161.49 ± 58.78	0.1154 ± 0.0420	62.85 ± 27.92	/	/	14.3
p.o.	50	231.43 ± 71.87	0.0165 ± 0.0051	273.76 ± 90.23	190.34 ± 24.50	0.79 ± 0.30	/