1. Apoptosis
    Cell Cycle/DNA Damage
    Anti-infection
    Autophagy
    NF-κB
    Metabolic Enzyme/Protease
  2. Apoptosis
    Topoisomerase
    HIV
    Autophagy
    Mitophagy
    NF-κB
    Endogenous Metabolite
  3. Betulinic acid

Betulinic acid (Synonyms: Lupatic acid; Betulic acid)

Cat. No.: HY-10529 Purity: 98.18%
Handling Instructions

Betulinic acid is a natural pentacyclic triterpenoid, acts as a eukaryotic topoisomerase I inhibitor, with an IC50 of 5 μM, and possesses anti-HIV, anti-malarial, anti-inflammatory and anti-tumor properties. Betulinic acid acts as a new activator of NF-kB.

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

Betulinic acid Chemical Structure

Betulinic acid Chemical Structure

CAS No. : 472-15-1

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10 mM * 1  mL in DMSO USD 70 In-stock
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Customer Review

Based on 7 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Betulinic acid purchased from MCE. Usage Cited in: Front Pharmacol. 2019 Sep 13;10:1017.

    Immunofluorescence is performed to determine the LC3II expression level to show the autophagosomes in the cells of the skin flaps: autophagosomes (green) in the dermis in area II; nuclei counterstained with DAPI (blue).

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    • Biological Activity

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    • References

    • Customer Review

    Description

    Betulinic acid is a natural pentacyclic triterpenoid, acts as a eukaryotic topoisomerase I inhibitor, with an IC50 of 5 μM, and possesses anti-HIV, anti-malarial, anti-inflammatory and anti-tumor properties[1][2][3][4]. Betulinic acid acts as a new activator of NF-kB[5].

    IC50 & Target

    Topoisomerase I

    5 μM (IC50)

    HIV-1

    1.4 μM (EC50)

    NF-κB

     

    Human Endogenous Metabolite

     

    In Vitro

    Betulinic acid is a eukaryotic topoisomerase I inhibitor, with an IC50 of 5 μM, and prevents topoisomerase I-DNA interaction[1]. Betulinic acid (10, 20, 40, 80, and 160 µM) significantly suppresses MDA-MB-231 cell viability in a time- and dose-dependent manner after treatment for 24 or 48 h. Betulinic acid (20, 40 µM) causes decrease in Bcl-2 expression of MDA-MB-231 cells. Betulinic acid also induces morphological changes of MDA-MB-231 cells at 20 µM, and leads to ultrastructure changes of MDA-MB-231 cells at 40 µM[2]. Betulinic acid shows anti-HIV activities, with an EC50 of 1.4 µM in acutely infected H9 lymphocytes[4].

    In Vivo

    Betulinic acid (10 and 30 mg/kg, p.o.) significantly abrogates colon shortening, and reduces malondialdehyde (MDA) and lipid hydroperoxide levels in dextran sulfate sodium (DSS)-induced colitis in mice. Betulinic acid (30 mg/kg, p.o.) restores superoxide dismutase (SOD), catalase activity and glutathione (GSH) content to control levels in DSS-induced colitis in mice. Betulinic acid (30 mg/kg, p.o.) also inhibits the DSS-induced increase in inflammatory markers. Betulinic acid (3, 10, 30 mg/kg, p.o.) suppresses acetic acid-induced writhing responses and mustard oil (MO)-induced visceral nociception in mice[3].

    Clinical Trial
    Molecular Weight

    456.70

    Formula

    C₃₀H₄₈O₃

    CAS No.

    472-15-1

    SMILES
    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 : 60 mg/mL (131.38 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1896 mL 10.9481 mL 21.8962 mL
    5 mM 0.4379 mL 2.1896 mL 4.3792 mL
    10 mM 0.2190 mL 1.0948 mL 2.1896 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: 2.5 mg/mL (5.47 mM); Suspended solution; Need ultrasonic

    • 2.

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

      Solubility: 2.5 mg/mL (5.47 mM); Suspended solution; Need ultrasonic

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (5.47 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Cell Assay
    [2]

    CCK-8 is used in the assay. MDA-MB-231 cells are cultured in 96-well plates at a density of 2 × 103 cells/well and then treated with DMSO vehicle or various concentrations of Betulinic acid ranging from 5 µM to 160 µM in 100 µL of medium for the indicated times. After the treatment period, the medium in each well is replaced with 110 µL of medium containing 10 µL of the CCK-8 mixture, and the plates are incubated for 1 h and 30 min at 37°C. The absorbance at a wavelength of 450 nm is measured with a microplate reader[2].

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

    Animal Administration
    [3]

    Female Swiss albino mice are administered vehicle (5% v/v DMSO in peanut oil) or Betulinic acid (3, 10 or 30 mg/kg) in vehicle, orally. After 1 h, acetic acid (300 mg/kg) is administered by intraperitoneal route and number of writhing response of each animal is counted for 20 min by an observer who is blind to the treatments. Writhing response is when animal rubs its abdomen on surface of table/floor with elongation of the body and extension of the hind limbs[3].

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

    References
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    Keywords:

    Betulinic acidLupatic acidBetulic acidApoptosisTopoisomeraseHIVAutophagyMitophagyNF-κBEndogenous MetaboliteHuman immunodeficiency virusMitochondrial AutophagyNuclear factor-κBNuclear factor-kappaBInhibitorinhibitorinhibit

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