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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).
For research use only. We do not sell to patients.
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
AChE
Cellular Effect
Cell Line
Type
Value
Description
References
RD
CC50
9.4 μM
Compound: AS
Cytotoxicity against human RD cells assessed as reduction in cell viability after 12 hrs by CCK8 assay
Cytotoxicity against human RD cells assessed as reduction in cell viability after 12 hrs by CCK8 assay
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Increased the expression of Beclin-1 and LC3-II and inhibited the expression of p62. However, had no effect on the expression of LC3-I and Vps34.
Decreased the expression of p-mTOR, p-PI3K and p-AKT in a concentration-dependent manner.
Significantly up-regulated phosphorylation of PKCδ.
Up-regulates the expression of glucose transporter 4 (GLUT4).and PLC-β3.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
D-galactose (D-gal)-induced sub-acuteaging mouse model of Alzheimer’s disease (AD)[1]
Dosage:
270 mg/kg, 540 mg/kg, 1080 mg/kg
Administration:
Intragastrical administration (i.g.); Once daily for 30 days. After D-gal treatment (150 mg/kg; Subcutaneous injection (s.c.); Once daily for 30 days)
Result:
Decreased levels of the pro-inflammatory cytokines IL-1β and TNF-α.
Decreased the content of MDA and increased the activity of SOD.
Significantly mitigated D-Gal-induced downregulation of SIRT1 in hippocampal neurons.
Significantly inhibited the expression of p53, acetyl-p53, and p21 in mice (all proteins associated with hippocampal aging).
Intramuscular injection (i.m.); Single dose. After CVA16 treatment (10[5.5] TCID50/g; Intramuscular injection (i.m.); Single dose )
Result:
Delayed death of the mice (6 days post-infection and 7 dpi), and eventually resulted in a survival rate of 50% and 70% for the mice in the treatment and prevention groups, respectively (the death of the control mice began at 4 days after infection and all died at 6 days after infection).
Reduced body mass index (BMI) and food efficiency in obese mice by 17.1% and 48.2%, respectively.
Decreased plasma glucose, CHE, AST and ALT levels by 34.1%, 45.5% and 27.2%, respectively.
Significantly inhibited the levels of serum proinflammatory cytokines TNF-α, IL-6 and IL-1β by 49.1%, 41.1% and 45.6%, respectively.
DMSO : 50 mg/mL (151.36 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Preparing Stock Solutions
ConcentrationSolventMass
1 mg
5 mg
10 mg
1 mM
3.0273 mL
15.1364 mL
30.2728 mL
5 mM
0.6055 mL
3.0273 mL
6.0546 mL
10 mM
0.3027 mL
1.5136 mL
3.0273 mL
View the Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day. The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Protocol 1
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.57 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage
mg/kg
Animal weight (per animal)
g
Dosing volume (per animal)
μL
Number of animals
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO+
%
+
%
Tween-80
+
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO,
. All of co-solvents are available by MedChemExpress (MCE).
, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.
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