1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. Calcium Channel
  3. Nothofagin

Nothofagin, a dihydrochalcone, is isolated from rooibos (Aspalathus linearis). Nothofagin downregulates NF-κB translocation through blocking calcium influx. Nothofagin has antioxidant activity and ameliorates various inflammatory responses such as the septic response and vascular inflammation.

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Nothofagin Chemical Structure

Nothofagin Chemical Structure

CAS No. : 11023-94-2

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Description

Nothofagin, a dihydrochalcone, is isolated from rooibos (Aspalathus linearis)[1]. Nothofagin downregulates NF-κB translocation through blocking calcium influx. Nothofagin has antioxidant activity and ameliorates various inflammatory responses such as the septic response and vascular inflammation[2].

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
0.0119 μM
Compound: 12h
Inhibition of human SGLT2 expressed in HEK293 cells assessed as reduction in 2-deoxyglucose uptake pretreated for 10 mins followed by 2-deoxyglucose addition in presence of sodium buffer measured after 1 hr by resazurin dye based fluorescence assay
Inhibition of human SGLT2 expressed in HEK293 cells assessed as reduction in 2-deoxyglucose uptake pretreated for 10 mins followed by 2-deoxyglucose addition in presence of sodium buffer measured after 1 hr by resazurin dye based fluorescence assay
[PMID: 28098449]
HEK293 IC50
19 μM
Compound: 12h
Inhibition of human SGLT1 expressed in HEK293 cells assessed as reduction in 2-deoxyglucose uptake pretreated for 10 mins followed by 2-deoxyglucose addition in presence of sodium buffer measured after 1 hr by resazurin dye based fluorescence assay
Inhibition of human SGLT1 expressed in HEK293 cells assessed as reduction in 2-deoxyglucose uptake pretreated for 10 mins followed by 2-deoxyglucose addition in presence of sodium buffer measured after 1 hr by resazurin dye based fluorescence assay
[PMID: 28098449]
In Vitro

Nothofagin pre-treatment (0.1, 1, 10 μM) decreases the level of histamine release in RBL-2H3 and RPMCs cells. The production of cytokines are downregulated bynothofagin pre-treatment Nothofagin (TNF-α: 1-10 μM; IL-4: 0.1-10 μM, IL-6: 1-10 μM)[1].
Pre-treatment of DNPHSA-stimulated RBL-2H3 with Nothofagin (10 μM) markedly suppresses the phosphorylation of Lyn, Syk, and Akt[1].
Nothofagin (30 μM; for 6 hours) results in inhibited formation of LPS-induced (100 ng/mL; 4 hours) paracellular gaps with the formation of dense F-actin rings in HUVECs[2].
Nothofagin suppresses IgE-mediated mast cell degranulation both in vitro and in vivo[1].

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

In Vivo

Nothofagin (1 mg/kg; orally; once a day; for 7 days) significantly increases the urinary volume of both normotensive (NTR) and spontaneously hypertensive rats (SHR)[3].

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

Animal Model: Male Wistar normotensive and spontaneously hypertensive rats (3-4 months old) [3]
Dosage: 1 mg/kg
Administration: Orally; once a day; for 7 days
Result: Significantly increased the urinary volume of both NTR and SHR.
Molecular Weight

436.41

Formula

C21H24O10

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC1=C([C@@H]([C@@H]([C@H]2O)O)O[C@@H]([C@H]2O)CO)C(O)=CC(O)=C1C(CCC(C=C3)=CC=C3O)=O

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation

Purity: ≥98.0%

References
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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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Nothofagin
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HY-113919
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