2. Neuronal Signaling Metabolic Enzyme/Protease NF-κB Immunology/Inflammation Apoptosis Anti-infection
  3. Cholinesterase (ChE) Lipase Reactive Oxygen Species (ROS) Apoptosis Bacterial
  4. Aspulvinone H

Aspulvinone H is an orally active inhibitor of AChE, pancreatic lipase, glutamic-oxaloacetic transaminase 1, and α-glucosidase, with IC50 values of 25.95 μM, 47.06 μM, 5.91/6.91 μM, and 4.6 μM, respectively. It has a Ka of 2.14 μM against GOT1 and a Ki of 6.58 μM against α-glucosidase. Aspulvinone H inhibits cancer cell proliferation, interferes with glutamine metabolism, elevates ROS levels, and induces cell apoptosis and S-phase arrest. Aspulvinone H exhibits antibacterial activity against Staphylococcus aureus. Aspulvinone H inhibits the growth of pancreatic ductal adenocarcinoma xenografts. Aspulvinone H reduces postprandial blood glucose in mice. Aspulvinone H can be used in research related to pancreatic ductal adenocarcinoma, diabetes, and Staphylococcus aureus infection.

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Aspulvinone H

Aspulvinone H Chemical Structure

CAS No. : 57744-69-1

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Aspulvinone H Related Antibodies

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Description

Aspulvinone H is an orally active inhibitor of AChE, pancreatic lipase, glutamic-oxaloacetic transaminase 1, and α-glucosidase, with IC50 values of 25.95 μM, 47.06 μM, 5.91/6.91 μM, and 4.6 μM, respectively. It has a Ka of 2.14 μM against GOT1 and a Ki of 6.58 μM against α-glucosidase. Aspulvinone H inhibits cancer cell proliferation, interferes with glutamine metabolism, elevates ROS levels, and induces cell apoptosis and S-phase arrest. Aspulvinone H exhibits antibacterial activity against Staphylococcus aureus. Aspulvinone H inhibits the growth of pancreatic ductal adenocarcinoma xenografts. Aspulvinone H reduces postprandial blood glucose in mice. Aspulvinone H can be used in research related to pancreatic ductal adenocarcinoma, diabetes, and Staphylococcus aureus infection[1][2][3][4].

In Vitro

Aspulvinone H (Compound 4) moderately inhibits acetylcholinesterase and pancreatic lipase in vitro, with IC50 values of 25.95 μM and 47.06 μM, respectively[1].
Aspulvinone H (Compound 6) inhibits the enzymatic activity of recombinant human GOT1 with IC50 values of 5.91 μM and 6.91 μM, respectively. It also binds directly to GOT1 with a Kd of 2.14 μM[2].
Aspulvinone H (0.1-100 μM; 48 h) selectively inhibits the proliferation of SW1990, PANC-1 and AsPC-1 pancreatic ductal adenocarcinoma cells (IC50 6.32-10.47 μM), while exhibits extremely low toxicity to non-malignant HPDE6C7 cells (IC50 >100 μM after 48 h treatment)[2].
Aspulvinone H (10-40 μM) disrupts glutamine metabolism, reduces the NADPH/NADP+ ratio in SW1990 pancreatic ductal adenocarcinoma cells, and increases their ROS levels[2].
Aspulvinone H (10-40 μM; 48 h) induces dose-dependent apoptosis and S-phase cell cycle arrest, inhibits cell proliferation, and suppresses migration in a dose- and time-dependent manner in SW1990 pancreatic ductal adenocarcinoma cells[2].
Aspulvinone H (Compound 4) (0.1 μM-10 mM; 10 min enzyme incubation, 15 min substrate incubation) potently inhibits α-glucosidase derived from Saccharomyces cerevisiae via a mixed-type inhibition mechanism, with an IC50 value of 4.6 μM, and exhibits higher affinity for the free enzyme than for the enzyme-substrate complex[3].
Aspulvinone H (40 μg/disc; 24 h) exhibits antibacterial activity against Staphylococcus aureus, producing an 11 mm inhibition zone after incubation at 38 °C for 24 h[4].

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

Aspulvinone H Related Antibodies

Cell Viability Assay[2]

Cell Line: Pancreatic ductal adenocarcinoma cell lines SW1990, PANC-1, AsPC-1; nonmalignant human pancreatic duct epithelial cell line HPDE6C7
Concentration: 0.1-100 μM
Incubation Time: 48 h
Result: Inhibited growth of PDAC cell lines with IC50 values of 6.32 μM (SW1990), 10.47 μM (PANC-1), and a value between these for AsPC-1.
Exhibited minimal cytotoxicity to nonmalignant HPDE6C7 cells, with an IC50 value over 100 μM.

Apoptosis Analysis[2]

Cell Line: SW1990 PDAC cells
Concentration: 10-40 μM
Incubation Time: 48 h
Result: Induced apoptosis in a dose-dependent manner, with apoptosis rates of 9.5% (10 μM), 28.3% (20 μM), and 80.2% (40 μM).
Induced S-phase cell cycle arrest, increasing S-phase cell proportion to 32.5% (10 μM), 38.6% (20 μM), and 43.9% (40 μM), while decreasing G0/G1 phase proportion to 59.4% (10 μM), 48.6% (20 μM), and 43.5% (40 μM).
In Vivo

Aspulvinone H (2.5-5 mg/kg; i.p.; once daily; for 14 consecutive days) significantly inhibits the growth of pancreatic ductal adenocarcinoma xenografts, regulates tumor glutamine metabolism, and causes no significant in vivo toxicity[2].
Aspulvinone H (25 mg/kg; oral gavage; single administration) reduces the postprandial blood glucose AUC0-t and inhibits blood glucose elevation in female C57BL/6J mice subjected to oral sucrose and maltose tolerance tests[3].

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

Animal Model: CB-17/SCID (male, 8 weeks old, subcutaneous injection of 3×106 SW1990 cells)[2]
Dosage: 2.5 mg/kg; 5 mg/kg
Administration: i.p.; daily; 14 days
Result: Reduced tumor volumes significantly compared to control.
Decreased oxaloacetate (OAA) and malate levels in tumor tissue.
Increased aspartate (Asp) and glutamine (Gln) levels in tumor tissue.
Decreased NADPH/NADP+ ratio in tumor tissue.
Caused no significant changes in mouse body weight or histomorphology.
Animal Model: C57BL/6J (female, 6 weeks old, 16-20 g)[3]
Dosage: 25 mg/kg
Administration: i.g.; single dose
Result: Significantly suppressed the rise in blood glucose levels at 30 and 60 minutes after sucrose loading compared to the negative control group.
Reduced the area under the blood glucose concentration-time curve (AUC) over 0-120 minutes by 13.2%.\nSignificantly reduced the postprandial blood glucose peak compared to the negative control group.
Reduced the AUC of postprandial blood glucose over 0-120 minutes by 19.7%.
Molecular Weight

432.51

Formula

C27H28O5
CAS No.
SMILES

OC1=C(C2=CC(C/C=C(C)\C)=C(C=C2)O)C(O/C1=C\C3=CC(C/C=C(C)\C)=C(C=C3)O)=O
Structure Classification
Initial Source

Aspergillus terreus ASM-1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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Aspulvinone H 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:

Aspulvinone H57744-69-1Cholinesterase (ChE)LipaseReactive Oxygen Species (ROS)ApoptosisBacterialPancreatic Lipase/Acetylcholinesterase/Glutamic-oxaloacetic Transaminase 1/Alpha-glucosidase InhibitorapoptosisCB-17/SCID miceC57BL/6J miceInhibitorinhibitorinhibit

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