Bifendate

Bifendate (DDB), extracted from Schisandrae chinensis, is an orally active anti-HBV agent against chronic hepatitis B. Bifendate inhibits ATG5-dependent autophagy and attenuates oleic acid-induced lipid accumulation with anti-oxidant properties in vitro. Bifendate can decrease alanine transaminase (ALT) level in mice. Bifendate attenuates hepatic steatosis in cholesterol/bile salt- and high-fat diet-induced hypercholesterolemia in mice. Bifendate potently increases the activity of cytochrome proteins (CYPs) and reverse P-gp-mediated multi-drug resistance (MDR)^{[1][2][3][4][5][6]}. In Vitro:Bifendate (0-50 μM, 12 h) inhibits autophagy degradation in a ATG5-dependent manner and inhibits lysosomal activity in Hela cells and MEFs^[2].
Bifendate (50 μM, 12 h) attenuates oleic acid (OA)-induced lipid droplet accumulation which is consistent with reduced autophagy activity and lysosome acidity in HepG2 cells^[2].
In Vivo:
Pharmacokinetic parameters of Bifendate (12 mg/kg, p.o., pills, the liquid SEDDS and the SEP) in rats (SEDDS: self-emulsifying drug delivery system; SEP: self-emulsifying pellet)^[3]

Parameters	Cmax (μg/mL)	Tmax (h)	AUC0-12 h (μg/mL)·h	MRT (h)	F0-12 h(%)
Bifendate pills	0.46±0.074	1.5±0.17	1322.29±421.85	3.43±0.74
The liquid SEDDS	0.98±0.101	0.75±0.11	3272.73±304.49	3.77±0.46	247.51±26.23
The SEP	0.83±0.215	2.0±0.12	3122.85±289.27	3.39±0.21	236.17±58.12

Bifendate (12 mg/kg, oral gavage, a single dose) from the liquid SEDDS and the SEP significantly increases oral bioavailability than that from pills in rats^[3].
Bifendate (0.03-0.3 g/kg, i.g., daily from day 6 to day 9) attenuates hepatic steatosis in cholesterol/bile salt- and high-fat diet-induced hypercholesterolemia in mice^[4].