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  3. Aristolochic acid A

Aristolochic acid A  (Synonyms: Aristolochic acid I; TR 1736)

Cat. No.: HY-N0510 Purity: 99.91%
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Aristolochic acid A (Aristolochic acid I; TR 1736) is the main component of plant extract Aristolochic acids, which are found in various herbal plants of genus Aristolochia and Asarum. Aristolochic acid A significantly reduces both activator protein 1 (AP-1) and NF-κB activities. Aristolochic acid A reduces BLCAP gene expression in human cell lines.

For research use only. We do not sell to patients.

CAS No. : 313-67-7

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10 mM * 1 mL in DMSO
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Customer Review

Based on 10 publication(s) in Google Scholar

Other Forms of Aristolochic acid A:

Top Publications Citing Use of Products

    Aristolochic acid A purchased from MedChemExpress. Usage Cited in: Nature. 2024 Jul;631(8020):459-466.  [Abstract]

    FLIPR Ca2+ assay responses in wild-type (WT) TAS2R14 and mutants in pockets 1, 2 and 3, following Aristolochic acid A (150 μM) stimulation. The negative logarithmic half-maximal effective concentration (pEC50) and the maximum response (Emax) values were calculated from the concentration–response curves.

    Aristolochic acid A purchased from MedChemExpress. Usage Cited in: Precis Clin Med. 2022 Sep 22;5(4):pbac023.

    Aristolochic acid A (AAI, 2 mg/kg/day). Body weight of mice in Control, AAI-4w, and AAI-8w groups.

    Aristolochic acid A purchased from MedChemExpress. Usage Cited in: Precis Clin Med. 2022 Sep 22;5(4):pbac023.

    Aristolochic acid A (AAI, 2 mg/kg/day, 4 or 8 weeks). H&E staining showed pathological changes of mice livers after AAI treatment, scale bar = 100 μm.

    Aristolochic acid A purchased from MedChemExpress. Usage Cited in: Precis Clin Med. 2022 Sep 22;5(4):pbac023.

    Aristolochic acid A (AAI, 2 mg/kg/day, 4 or 8 weeks). Liver/body weight ratio after AAI treatment (n = 5, ***P < 0.001, ns = not significant). Effects of AAI on the levels of serum ALT and AST in the indicated groups (n = 5, *P < 0.05, **P < 0.01, ns = not significant).

    Aristolochic acid A purchased from MedChemExpress. Usage Cited in: Precis Clin Med. 2022 Sep 22;5(4):pbac023.

    Aristolochic acid A (AAI, 2 mg/kg/day, 4 or 8 weeks). IF staining of p-STAT3 (red) in the three groups, and the nuclei were stained by Hoechst (blue), scale bar = 50 µm.

    Aristolochic acid A purchased from MedChemExpress. Usage Cited in: Precis Clin Med. 2022 Sep 22;5(4):pbac023.

    Aristolochic acid A (AAI, 2 mg/kg/day, 4 or 8 weeks). IF staining of Bcl-2 (green) and Bax (Red) to detect endothelial cell apoptosis in the three groups, the nucleus was labelled by Hoechst (blue), scale bar = 40 µm.

    Aristolochic acid A purchased from MedChemExpress. Usage Cited in: Precis Clin Med. 2022 Sep 22;5(4):pbac023.

    Aristolochic acid A (AAI, 2 mg/kg/day, 4 or 8 weeks). Western blot was used to detect the expression of apoptotic signaling pathway-related markers cleaved-caspase 3, Bax, and Bcl-2 in liver tissues after AAI treatment.

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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Aristolochic acid A (Aristolochic acid I; TR 1736) is the main component of plant extract Aristolochic acids, which are found in various herbal plants of genus Aristolochia and Asarum. Aristolochic acid A significantly reduces both activator protein 1 (AP-1) and NF-κB activities. Aristolochic acid A reduces BLCAP gene expression in human cell lines[1].

    Cellular Effect
    Cell Line Type Value Description References
    HEK293 EC50
    118.34 μM
    Compound: Aristolochic acid
    Cytotoxicity in HEK293 cells assessed as reduction in cell survival incubated for 48 hrs by MTT assay
    Cytotoxicity in HEK293 cells assessed as reduction in cell survival incubated for 48 hrs by MTT assay
    [PMID: 30108751]
    Neutrophil IC50
    > 10 μg/mL
    Compound: 4
    Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced elastase release after 5 mins
    Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced elastase release after 5 mins
    [PMID: 21353775]
    Neutrophil IC50
    > 10 μg/mL
    Compound: 4
    Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced superoxide anion generation after 5 mins
    Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced superoxide anion generation after 5 mins
    [PMID: 21353775]
    Panel NCI-60 (60 carcinoma cell lines) GI50
    883 nM
    Compound: Aristolochic acid
    Growth inhibitory activity against human cancer cell line in the NCI's anticancer drug screening program
    Growth inhibitory activity against human cancer cell line in the NCI's anticancer drug screening program
    [PMID: 15743190]
    In Vitro

    Aristolochic acid A (150, 200 μM, 24 hours) inhibits the cell viabilities of kidney cells HEK293 and HK-2[1].
    Aristolochic acid A (100, 200 μM, 24 hours) causes a concentration-dependent decrease in bladder cancer-associated protein (BLCAP) mRNA levels in kidney cells (HEK 293 and HK-2) , and bladder cancer cell line (HT-1376)[1].
    Aristolochic acid A (100, 200 μM, 24 hours) weakens the BLCAP protein signals in a dose-dependent manner in both HEK293 and HT-1376 cells[1].

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

    Cell Viability Assay[1]

    Cell Line: Kidney cells (HEK 293 and HK-2)
    Concentration: 50, 100, 150, 200 μM
    Incubation Time: 24 hours
    Result: The cell viabilities of HEK293 and HK-2 were lower than that of vehicle-treated cultures until 150 μM and 200 μM.

    RT-PCR[1]

    Cell Line: Kidney cells (HEK 293 and HK-2), and bladder cancer cell line (HT-1376)
    Concentration: 100, 200 μM
    Incubation Time: 24 hours
    Result: Down regulated the levels of BLCAP mRNA.

    Western Blot Analysis[1]

    Cell Line: HEK293 and HT-1376 cells
    Concentration: 100, 200 μM
    Incubation Time: 24 hours
    Result: Reduced the BLCAP protein expression in a dose-dependent manner.
    In Vivo

    Note:
    Please do not refer to only one article to determine the experimental conditions. It is recommended to determine the optimal experimental conditions (animal strain, age, dosage, frequency and cycle, detection time and indicators, etc.) through preliminary experiments before the formal experiment.

    Aristolochic acid A can be used to induce nephrotoxicity models. Pharmacokinetic studies show that in male C57BL/6 mice, the concentration of Aristolochic acid A in the kidneys is higher than in the liver 30 minutes after intraperitoneal administration (10 mg/kg). The plasma concentration of Aristolochic acid A also peaks approximately 30 minutes after administration[2].

    Induction of Nephrotoxicity [2][3]
    Background
    The pathogenesis of Aristolochic acid Anephropathy remains unclear. Research shows that Aristolochic acid A mainly damages renal tubular epithelial cells and renal tules, leading to interstitial fibrosis, thereby producing nephrotoxicity.
    Specific Modeling Methods
    Mice: C57BL/6J • 8 weeks of age
    Administration: 10 mg/kg • i.p. • 3-5 days[3]
    Modeling Indicators
    Pathology changs: H&E stain shows renal tissue structure is disordered, glomerular edema, pyknosis, and proximal tubule epithelial cell shedding
    Biochemistry changes: Scr and blood urea nitrogen (BUN) contents increases

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

    Molecular Weight

    341.27

    Formula

    C17H11NO7

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to orange

    SMILES

    OC(C1=CC2=C(OCO2)C3=C4C(C(OC)=CC=C4)=CC([N+]([O-])=O)=C31)=O

    Structure Classification
    Initial Source
    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, protect from light

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

    Solvent & Solubility
    In Vitro: 

    DMSO : 16.67 mg/mL (48.85 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 2.9302 mL 14.6512 mL 29.3023 mL
    5 mM 0.5860 mL 2.9302 mL 5.8605 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, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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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: ≥ 2.08 mg/mL (6.09 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
    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, 1 year; -20°C, 6 months (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: 99.91%

    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, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.9302 mL 14.6512 mL 29.3023 mL 73.2558 mL
    5 mM 0.5860 mL 2.9302 mL 5.8605 mL 14.6512 mL
    10 mM 0.2930 mL 1.4651 mL 2.9302 mL 7.3256 mL
    15 mM 0.1953 mL 0.9767 mL 1.9535 mL 4.8837 mL
    20 mM 0.1465 mL 0.7326 mL 1.4651 mL 3.6628 mL
    25 mM 0.1172 mL 0.5860 mL 1.1721 mL 2.9302 mL
    30 mM 0.0977 mL 0.4884 mL 0.9767 mL 2.4419 mL
    40 mM 0.0733 mL 0.3663 mL 0.7326 mL 1.8314 mL
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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.

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