2. PI3K/Akt/mTOR Apoptosis Neuronal Signaling GPCR/G Protein
  3. Akt Bcl-2 Family Apoptosis Adrenergic Receptor
  4. 8-​O-​Acetylharpagide

8-O-Acetylharpagide is an orally active iridoid glycoside compound. 8-O-Acetylharpagide exhibits anti-aging activity at low doses and anticancer activity at high doses. 8-O-Acetylharpagide induces late-stage apoptosis and necrosis-like death in cancer cells, and downregulates anti-apoptotic proteins such as Akt, p-Akt and Bcl-2. 8-O-Acetylharpagide is mainly metabolized in rats via demethylation, hydrolysis and glucuronidation, and its active metabolites downregulate the AKT/NF-κB/MMP9 signaling axis. 8-O-Acetylharpagide exerts vasoconstrictive effects by activating vascular α-adrenoceptor.

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8-​O-​Acetylharpagide

8-​O-​Acetylharpagide Chemical Structure

CAS No. : 6926-14-3

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Based on 1 publication(s) in Google Scholar

Other Forms of 8-​O-​Acetylharpagide:

8-​O-​Acetylharpagide Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE 8-​O-​Acetylharpagide

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

8-O-Acetylharpagide is an orally active iridoid glycoside compound. 8-O-Acetylharpagide exhibits anti-aging activity at low doses and anticancer activity at high doses. 8-O-Acetylharpagide induces late-stage apoptosis and necrosis-like death in cancer cells, and downregulates anti-apoptotic proteins such as Akt, p-Akt and Bcl-2. 8-O-Acetylharpagide is mainly metabolized in rats via demethylation, hydrolysis and glucuronidation, and its active metabolites downregulate the AKT/NF-κB/MMP9 signaling axis. 8-O-Acetylharpagide exerts vasoconstrictive effects by activating vascular α-adrenoceptor[1][2][3].

Cellular Effect
Cell Line Type Value Description References
A-431 ED50
310 μM
Compound: 2
Cytotoxicity against human A431 cells by MTT assay
Cytotoxicity against human A431 cells by MTT assay
[PMID: 12027771]
In Vitro

8-O-acetylharpagide (0.5-10 μM; 48 h) dose-dependently inhibits the activity of senescence-associated β-galactosidase in senescent human dermal fibroblasts in vitro[1].
8-O-acetylharpagide (0.5-10 μM; 48 h) dose-dependently inhibits p53 expression in senescent human dermal fibroblasts[1].
8-O-acetylharpagide (1-10 μM) inhibits the elevated intracellular reactive oxygen species levels in dermal fibroblasts from elderly humans[1].
8-O-acetylharpagide (2.5 mg/mL; 0-24 h) undergoes metabolic transformation in an in vitro rat intestinal flora culture system, producing 2 metabolites via pathways including hydrolysis, reduction and glucuronidation[2].
8-O-acetylharpagide (0.01-1 mM; 24 h) exhibits more potent selective cytotoxicity against human hypopharyngeal carcinoma FaDu cells than against normal human PDL cells, with an IC50 of 0.88 mM for FaDu cells and 1.65 mM for PDL cells after 24 h of treatment[3].
8-O-acetylharpagide (1 mM; 24 h) induces significant cell rounding in human hypopharyngeal carcinoma FaDu cells, but exerts no such effect in normal human PDL cells[3].
8-O-acetylharpagide (1 mM; 6 days) completely inhibits the proliferation of human hypopharyngeal carcinoma FaDu cells[3].
8-O-acetylharpagide (0.5-1 mM; 24 h) induces dose-dependent G2/M phase arrest in human hypopharyngeal carcinoma FaDu cells and regulates the expression of cell cycle-related proteins, but exerts no effect on the cell cycle distribution of normal human PDL cells[3].
8-O-acetylharpagide (1 mM; 24 h) induces significant necroptotic cell death and late apoptosis in human hypopharyngeal carcinoma FaDu cells, downregulates anti-apoptotic proteins, but exerts minimal effects on normal human PDL cells[3].
8-O-acetylharpagide (1 mM; 24 h) significantly enhances the radiosensitivity of human hypopharyngeal carcinoma FaDu cells, but has no effect on that of normal human PDL cells[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

8-​O-​Acetylharpagide Related Antibodies

Western Blot Analysis[1]

Cell Line: old human dermal fibroblasts (HDFs)
Concentration: 0.5 μM, 1 μM, 5 μM, 10 μM
Incubation Time: 48 h
Result: Reduced p53 expression to ~90% of control at 0.5 μM.
Reduced p53 expression to ~75% of control at 1 μM.
Reduced p53 expression to ~60% of control at 5 μM.
Reduced p53 expression to ~55% of control at 10 μM, all in a dose-dependent manner.

Cell Cytotoxicity Assay[3]

Cell Line: human hypopharyngeal cancer FaDu cells, human periodontal ligament (PDL) normal cells
Concentration: 0.01, 0.1, 0.3, 0.5, 0.7, 1 mM
Incubation Time: 24 h
Result: Reduced viability of FaDu cells significantly at concentrations ≥ 0.5 mM, with an IC50 of 0.88 mM.
Reached an IC50 of 1.65 mM in PDL cells, yielding a selectivity index of ≈1.85.
Enhanced PDL cell viability at low concentrations.

Cell Proliferation Assay[3]

Cell Line: human hypopharyngeal cancer FaDu cells
Concentration: 1 mM
Incubation Time: 6 days
Result: Completely suppressed the proliferation of FaDu cells over the 6-day period, while vehicle-treated cells showed continuous growth.

Cell Cycle Analysis[3]

Cell Line: human hypopharyngeal cancer FaDu cells, human periodontal ligament (PDL) normal cells
Concentration: 0.5, 1 mM
Incubation Time: 24 h
Result: Induced dramatic G2/M phase arrest and an increased sub-G1 population in FaDu cells treated with 1 mM, with a dose-dependent effect from 0.5-1 mM.
Upregulated CHK1 (1.32-fold), Cyclin B (1.3-fold), and p21 (1.74-fold), and downregulated CDK1 (0.58-fold) relative to GAPDH in FaDu cells.
Showed no significant changes in cell cycle distribution or cell cycle-related protein expression in PDL cells at the same concentrations.

Apoptosis Analysis[3]

Cell Line: human hypopharyngeal cancer FaDu cells, human periodontal ligament (PDL) normal cells
Concentration: 1 mM
Incubation Time: 24 h
Result: Induced a significant increase in necrosis-like cell population and late apoptosis, with no significant change in early apoptosis in FaDu cells.
Downregulated AKT (0.56-fold), phospho-AKT (0.64-fold), and BCL-2 (0.7-fold) relative to GAPDH in FaDu cells.
Caused only a small increase in necrosis-like cells and no significant changes in apoptosis or apoptosis-related protein expression in PDL cells.

Cell Cytotoxicity Assay[3]

Cell Line: human hypopharyngeal cancer FaDu cells, human periodontal ligament (PDL) normal cells
Concentration: 1 mM
Incubation Time: 24 h (pre-incubation); 48 h (post-irradiation incubation)
Result: Enhanced the radiosensitivity of FaDu cells significantly, with cell viability decreasing more sharply with increasing radiation dose compared to vehicle-treated FaDu cells.
Showed no enhancement of radiosensitivity in PDL cells.
In Vivo

8-O-acetylharpagide (75-150 mg/kg; p.o.; once daily; for 4 consecutive weeks) significantly inhibits the AKT/NF-κB/MMP9 signaling axis in 4T1 breast cancer-bearing Balb-C mice[2].
8-O-acetylharpagide (low dose; p.o.) inhibits senescent phenotypes in aged mice[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Balb-C (female, 4 weeks old, weight 22 g, subcutaneous injection of 4T1 cells)[2]
Dosage: 75 mg/kg; 150 mg/kg
Administration: p.o.; once daily; 4 weeks
Result: Significantly reduced relative protein levels of AKT, p-AKT, NF-κB p65, and MMP9 compared to the control group.
Significantly reduced the p-AKT/AKT ratio compared to the control group.
Further significantly reduced relative protein levels of AKT, p-AKT, NF-κB p65, and MMP9 compared to the control group.
Molecular Weight

406.38

Formula

C17H26O11
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O[C@@]([C@@H]1O)(C=CO2)[C@]([C@](OC(C)=O)(C)C1)([H])[C@@H]2O[C@]([C@@H]([C@@H](O)[C@@H]3O)O)([H])O[C@@H]3CO
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (61.52 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4608 mL 12.3038 mL 24.6075 mL
5 mM 0.4922 mL 2.4608 mL 4.9215 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.

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.15 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 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.15 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 μL DMSO 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:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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.
 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.
Purity & Documentation

Purity: 99.75%

SDS (392 KB)

COA (259 KB) HNMR (119 KB) CNMR (123 KB) RP-HPLC (168 KB) MS (122 KB)

Handling Instructions (2659 KB)
References

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4608 mL 12.3038 mL 24.6075 mL 61.5188 mL
5 mM 0.4922 mL 2.4608 mL 4.9215 mL 12.3038 mL
10 mM 0.2461 mL 1.2304 mL 2.4608 mL 6.1519 mL
15 mM 0.1641 mL 0.8203 mL 1.6405 mL 4.1013 mL
20 mM 0.1230 mL 0.6152 mL 1.2304 mL 3.0759 mL
25 mM 0.0984 mL 0.4922 mL 0.9843 mL 2.4608 mL
30 mM 0.0820 mL 0.4101 mL 0.8203 mL 2.0506 mL
40 mM 0.0615 mL 0.3076 mL 0.6152 mL 1.5380 mL
50 mM 0.0492 mL 0.2461 mL 0.4922 mL 1.2304 mL
60 mM 0.0410 mL 0.2051 mL 0.4101 mL 1.0253 mL
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8-​O-​Acetylharpagide Related Classifications

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  • Do most proteins show cross-species activity?

    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.

Keywords:

8-​O-​Acetylharpagide6926-14-3AktBcl-2 FamilyApoptosisAdrenergic ReceptorPKBProtein kinase BBeta ReceptorAKTPDL cellsFaDu cellsMMP9NF-κB p65old human dermal fibroblastsp53hypopharyngeal cancer cellsα-adrenoceptor4T1 breast cancer-bearing Balb-C miceInhibitorinhibitorinhibit

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