Liquiritigenin

Catalog No.S3929 Synonyms: 4',7-Dihydroxyflavanone

Liquiritigenin Chemical Structure

Molecular Weight(MW): 256.25

Liquiritigenin, the most active estrogenic compound from the root of Glycyrrhizae uralensis Fisch, selectively binds to ERβ with an IC50 value of 7.5 μM and activates multiple ER regulatory elements and native target genes with Erβ but not ERα.

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Biological Activity

Description Liquiritigenin, the most active estrogenic compound from the root of Glycyrrhizae uralensis Fisch, selectively binds to ERβ with an IC50 value of 7.5 μM and activates multiple ER regulatory elements and native target genes with Erβ but not ERα.
Targets
ERβ [2]
()
VEGF [3]
()
In vitro

Liquiritigenin-treated murine osteoblastic MC3T3-E1 cells shows an increased alkaline phosphatase activity and enhances phosphorylation of Smad1/5 compared with untreated cells. Moreover, liquiritigenin inhibits osteoclast differentiation, its bone-resorption activity through slightly decreases the phosphorylation of extracellular signal-regulated kinase, c-Jun N-terminal kinase, and inhibitor of nuclear factor kappa B-α ; however, the phosphorylation of Akt and p38 slightly increase in bone marrow-derived osteoclasts. The expression levels of the osteoclast marker proteins nuclear factor of activated T-cell cytoplasmic-1, Src, and cathepsin K diminish. Liquiritigenin is shown to exert the following pharmacological effects: increased cell growth, increased alkaline phosphatase activity, promotion of collagen synthesis, and the mineralization of osteoblastic MC3T3-E1 cells[1]. Liquiritigenin inhibits serum-induced HIF-1α and VEGF expression via the AKT/mTOR-p70S6K signaling pathway in HeLa cells[2].

In vivo Liquiritigenin inhibits the growth of tumors in nude mice originating from human cervical cancer cell line HeLa cells, and reduces angiogenesis in a dose dependent manner[2]. Liquiritigenin effectively reduces the levels of pro-inflammatory cytokines and the expressions of p-p65NF-κB and p-IκBα. Furthermore, liquiritigenin preconditioning could down-regulate the immobility time in tail suspension test (TST), forced swimming test (FST) and up-regulate BDNF and TrkB contents in hippocampus. Thus, liquiritigenin has antidepressant activity that might be attributed to its anti-inflammatory property and BDNF/TrkB signaling pathway[4].

Protocol

Cell Research:[1]
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  • Cell lines: Murine osteoblastic MC3T3-E1 cells
  • Concentrations: 0-100 μM
  • Incubation Time: 72 h
  • Method: Cells seeded in 96-well cell culture plates are incubated with the Cell Counting Kit-8 for 1 h, and then the absorbance at 450nm is measured with a microplate reader.
    (Only for Reference)
Animal Research:[3]
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  • Animal Models: nude BALB/c mice.
  • Formulation: 5% sodium carboxymethycellulose
  • Dosages: 10, 20, 40 mg/kg
  • Administration: intragastrically
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 51 mg/mL (199.02 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 256.25
Formula

C15H12O4

CAS No. 578-86-9
Storage powder
in solvent
Synonyms 4',7-Dihydroxyflavanone

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01199250 Not yet recruiting Other: Laboratory Biomarker Analysis Lynch Syndrome|Recurrent Uterine Corpus Carcinoma|Stage I Uterine Corpus Cancer|Stage II Uterine Corpus Cancer|Stage III Uterine Corpus Cancer|Stage IV Uterine Corpus Cancer Gynecologic Oncology Group|National Cancer Institute (NCI) January 2100 --
NCT02442752 Suspended Drug: Dexlansoprazole Pediatric Gastroesophageal Reflux Disease Takeda June 15 2025 Phase 1
NCT03643887 Not yet recruiting Drug: FMT Capsule DE|Drug: Placebo oral capsule Clostridium Difficile Infection University of Wisconsin Madison September 1 2022 Phase 2
NCT03986086 Not yet recruiting Drug: MPH966|Drug: Placebo Hematologic Malignancy Nelson Chao|Mereo BioPharma|National Center for Advancing Translational Science (NCATS)|Duke University September 2021 Phase 1|Phase 2
NCT00424866 Not yet recruiting Drug: FGF-1|Drug: Placebo Peripheral Arterial Disease|Stenosis|Intermittent Claudication CardioVascular BioTherapeutics Inc. December 2020 Phase 1|Phase 2
NCT03086525 Not yet recruiting Other: Diagnosis/Prognosis Musculoskeletal Pain University of Malaga December 2020 --

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Estrogen/progestogen Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID