Acetylshikonin

Acetylshikonin is an oral active anti-cancer, anti-inflammatory, antioxidant, anti-fertility, antibacterial, and neuroprotective agent. Acetylshikonin is a inhibitor of acetylcholinase (AChE) (IC₅₀=34.6 μM) and nonselective cytochrome P450. Acetylshikonin can induce Apoptosis and Autophagy in cancer cells. Acetylshikonin regulates blood glucose, liver fat metabolism, and renal fibrosis, and is used in the study of diabetes, diabetic nephropathy (DN), obesity, and nonalcoholic fatty liver disease (NAFLD)^{[1][2][3][4][5][6][7][8][9]}. IC50 & Target:IC50: 1.4-4.0 μM (all P450s)^[2]
IC50: 34.6 μM (AChE)^[8].
In Vitro:Acetylshikonin(1.6-100 μM) inhibits the proliferation of oral cancer cells KB-R5 with IC₅₀ 40 μM^[6].
Acetylshikonin (20-80 μM; 24 h) can induce Apoptosis and (20-80 μM) Autophagy of KB-R5 cells, and block mTOR/PI3K/AKT signaling pathway in KB-R5 cells^[6].
Acetylshikonin (1-10 μM; 12 h) inhibits H₂O₂ (500 μM; 4 h) H₂O₂- (500 μM; 4 h ) induced Apoptosis of neuroblastoma SH-SY5Y and pc12 cells^[8].
Acetylshikonin (0.01-5 μM/L; 2 h) has anti-CoxSackievirus A16 (CVA16) activity in the adsorption/invasion stage with EC₅₀ was 0.04 μmol/L. However, has no effective in the pre-infection, replication and release stages^[2].
Acetylshikonin (0.01-1 μM; 30 min) promotes glucose uptake by skeletal muscle cells L6 through PLC-β3/PKCδ mediation, thereby reducing blood glucose level^[3].
Acetylshikonin (1-5 μg/mL; 48 h) inhibits TGF-β1 (5 ng/mL) induced renal fibrosis in HK2 cells^[5].
In Vivo:Acetylshikonin (50 mg/kg; Intraperitoneal injection; Three times per week for 6 weeks) significantly inhibited tumor growth in BALB/c nude mice in a concentration-dependent manner^[6].
Acetylshikonin (270-1080 mg/kg; Intragastric administration; Once a day for 30 days) reduces D-galactose-induced (150 mg/kg) cognitive impairment and hippohippoal aging by reducing oxidative stress and neuroinflammation and inhibiting the activation of the p53/p21 signaling pathway in mice^[1].
Acetylshikonin (2 mg/kg; Intramuscular injection; Single dose) inhibits Coxsackievirus A16 (CVA16) replication in mice^[2].
Acetylshikonin (100 mg/kg; Intragastric administration; Once a day for eight weeks) inhibits renal fibrosis by inhibiting TGF-β1/Smad pathway without affecting blood glucose, thus reducing the damage of renal function in streptozotocin (STZ) -induced diabetic C57BL/6 mice^[5].
Acetylshikonin (10 mk/kg; Intraperitoneal injection; Once a day for three days) reduces alloxouracil- (180 mg/kg; Intraperitoneal injection; Single dose) induced blood glucose level in diabetic mice^[3].
Acetylshikonin (540 mg/kg; Oral administration; Once a day for eight weeks) reduces liver fat accumulation by regulating fat metabolism and liver inflammation in obese C57BL/6J mice, thereby improving obesity and nonalcoholic fatty liver disease (NAFLD)^[4].
Acetylshikonin (120-1080 mg/kg; Intragastric administration;) doesn’t affect the ability of pregnancy in Sprague-Dawley rats at low doses (120 mg/kg and 360 mg/kg), but inhibits the ability of pregnancy in Sprague-Dawley rats at high doses (1080 mg/kg) by affecting the secretion of gonadotropin (GTH) and reducing the levels of serum follicle-stimulating hormone (FSH) and luteinizing hormone (LH)^[7].