Table 1.

Agents that target SREBP-mediated lipogenesis.

Drug	Disease	Mechanism	Targets	Cell Lines Tested	Mouse Models Tested (Dose)	Clinical Trials	Reference
Xanthohumol	Fatty liver	Impairs ER–Golgi translocation of the SCAP–SREBP complex by binding to SEC23 and SEC24 and blocking SCAP–SREBP incorporation into common coated protein II vesicles	SREBP1	Huh-7	HFD-induced fatty liver in male C57BL/6J mice (0.2% or 0.4%)	/	[37]
Antrodan	NAFLD	Reduces HFD-induced NAFLD via the AMPK–SREBP1c–PPARγ pathway	SREBP1	none	(20–40 mg/kg)	/	[36]
Betulin	HCC	Inhibits cell glucose metabolism to prevent metastatic potential and facilitate the inhibitory effect of sorafenib	SREBP1	MHCC97-H	MHCC97-H xenograft tumors (2 mg/kg)	/	[84]
	HCC	Inhibits ER–Golgi translocation of SREBPs	SREBP1	none	Diethylnitrosamine-induced HCC in mice (50 mg/kg)	/	[77]
Emodin	HCC	Induces apoptosis and reduces mitochondrial membrane potential; anti-cancer effects	SREBP1 and its downstream targets, ACLY, ACCa, FASN, and SCD1	Bel-7402	none	/	[87,88]
Sorafenib	HCC	Reduces cell viability	SREBP1 and its target SCD1	human Huh-7.5 liver cancer cells	Huh-7.5 xenograft tumors (20 mg/kg/d)	Phase 4 completed NCT01098760	[83]
Cinobufotalin	HCC	Induces cell cycle G2–M arrest and apoptosis; inhibits cell proliferation by inhibiting de novo lipid synthesis	SREBP1	HepG2, SMMC-7721	SMMC-7721 xenograft tumors (2.5 mg/kg, 5 mg/kg)	Phase 3 NCT03236636	[86]
Ursolic acid	HCC	Activates SREBP2 and cholesterol biosynthesis-related genes and enzymes to lower cholesterol in cells	SREBP2	SK-HEP-1, Hep3B	none	/	[89]

HFD, high-fat diet.