Phellopterin

Phellopterin, an orally active furocoumarin with multiple biological activities. Phellopterin is a partial agonist of the central benzodiazepine receptors. Phellopterin exerts anti-inflammatory effects by upregulating SIRT1, downregulating ICAM-1 (reducing chronic inflammation, aiding diabetic ulcer healing), inhibiting STAT3 phosphorylation (easing atopic dermatitis inflammation), regulating Akt/PKC pathways (lowering TNF-α-induced VCAM-1 to block monocyte adhesion), and inhibiting TLR4/NF-κB pathway and macrophage M2 polarization (alleviating colitis-related cancers) . Phellopterin suppresses ovarian cancer progression via inhibiting the PU.1/CLEC5A/PI3K-AKT loop (inducing cell cycle arrest, apoptosis, DNA damage) . Phellopterin alleviates murine diabetes by promoting adipocyte differentiation and increasing PPARγ. Phellopterin also has anti-HSV-1 activity. Phellopterin can be used for studying anti-inflammation, anti-cancer (e.g., ovarian cancer, colitis cancer), blood glucose lowering, anti-diabetes, and anti-virus[1][2][3][4][5][6][7][8].

Product Specifications

CAS Number

[2543-94-4]

UNSPSC

12352005

Hazard Statement

H302

Target

Akt; Apoptosis; ERK; HIV; Integrin; PI3K; PKC; PPAR; Sirtuin; STAT; Toll-like Receptor (TLR)

Type

Natural Products

Related Pathways

Anti-infection; Apoptosis; Cell Cycle/DNA Damage; Cytoskeleton; Epigenetics; Immunology/Inflammation; JAK/STAT Signaling; MAPK/ERK Pathway; Metabolic Enzyme/Protease; PI3K/Akt/mTOR; Stem Cell/Wnt; TGF-beta/Smad; Vitamin D Related/Nuclear Receptor

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/phellopterin.html

Concentration

10mM

Purity

99.94

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C1C=CC2=C(OC)C3=C(OC=C3)C(OC/C=C(C)/C)=C2O1

Molecular Formula

C17H16O5

Molecular Weight

300.31

Precautions

H302

References & Citations

[1]Nizamutdinova IT, et al. Hesperidin, hesperidin methyl chalone and phellopterin from Poncirus trifoliata (Rutaceae) differentially regulate the expression of adhesion molecules in tumor necrosis factor-alpha-stimulated human umbilical vein endothelial cells. Int Immunopharmacol. 2008 May;8 (5) :670-8.|[2]Zou J, et al. Phellopterin cream exerts an anti-inflammatory effect that facilitates diabetes-associated cutaneous wound healing via SIRT1. Phytomedicine. 2022 Dec;107:154447.|[3]Guo A, Lin J, Zhong P, Chen J, Wang L, Lin X, Feng M. Phellopterin attenuates ovarian cancer proliferation and chemoresistance by inhibiting the PU.1/CLEC5A/PI3K-AKT feedback loop. Toxicol Appl Pharmacol. 2023 Oct 15;477:116691. |[4]Han HS, Jeon H, Kang SC. Phellopterin isolated from Angelica dahurica reduces blood glucose level in diabetic mice. Heliyon. 2018 Mar 19;4 (3) :e00577.|[5]Nakamura M, et al. Stimulation of phosphorylation of ERK and CREB by phellopterin and auraptene isolated from Citrusjunos. Nat Prod Commun. 2014 Oct;9 (10) :1491-4. |[6]Dekermendjian K, et al. Characterisation of the furanocoumarin phellopterin as a rat brain benzodiazepine receptor partial agonist in vitro. Neurosci Lett. 1996 Nov 29;219 (3) :151-4.|[7]Xu X, et al. The therapeutic effect of phellopterin on colitis-associated cancer and its effects on TLR4/NF-κB pathway and macrophage M2 polarization. Cell Mol Biol (Noisy-le-grand) . 2023 Dec 31;69 (15) :51-57.|[8]Rajtar B, et al. Antiviral effect of compounds derived from Angelica archangelica L. on Herpes simplex virus-1 and Coxsackievirus B3 infections. Food Chem Toxicol. 2017 Nov;109 (Pt 2) :1026-1031.