Chalcones

4-Hydroxychalcone is an orally active flavonoid precursor. 4-Hydroxychalcone inhibits VEGF- and bFGF-induced phosphorylation of ERK1/2 and Akt. 4-Hydroxychalcone suppresses resistant hypertension by alleviating hyperaldosteronism, inflammation and renal injury in cryptochrome gene knockout mice. 4-Hydroxychalcone possesses anti-angiogenic activity.

Hesperidin methylchalcone (Hesperidin methyl chalcone) is an orally active flavonoid that has analgesic, anti-inflammatory and antioxidant properties. Hesperidin methylchalcone exhibits vasoprotective activity. Hesperidin methylchalcone inhibits oxidative stress, cytokine production and NF-κB activation. Hesperidin methylchalcone can be used for the research of gout disease.

4,4'-Dimethoxychalcone acts as a natural autophagy inducer with anti-ageing properties.

(E)-Cardamonin ((E)-Cardamomin) is a novel antagonist of hTRPA1 cation channel with an IC₅₀ of 454 nM.

Licraside, found in Glycyrrhiza glabra, is a Farnesoid X receptor (FXR) activator. Licraside activates FXR to induce upregulation of SHP and BSEP, regulates bile acid homeostasis, reduces elevated biliary and serum TBA, serum ALT, AST, GGT, ALP, and TBIL levels, and attenuates liver histopathological damage. Licraside inhibits factor Xa with an IC₅₀ of 48.54 mM. Licraside can be used for the research of cholestasis and thromboembolic diseases.

Neoisoliquiritin (Neoisoliquiritigenin) is an androgen receptor (AR) inhibitor. Neoisoliquiritin inhibits the ATPase activity of GRP78. Neoisoliquiritin induces G₀/G₁ cell cycle arrest and inhibits proliferation in cancer cells, while it also induces cell apoptosis (apoptosis). Neoisoliquiritin suppresses tumor growth in mouse models of prostate cancer and breast cancer. Neoisoliquiritin can be used in studies related to prostate cancer and breast cancer.

Chalcone is isolated from Glycyrrhiza uralensis and used to synthesize chalcone derivatives. Chalcone derivatives possess varied biological and pharmacological activity, including anti-inflammatory, antioxidative, antibacterial, anticancer, and anti-parasitic activities.

Flavokawain A is a chalcone compound and an orally active inhibitor of PRMT5 and cytochrome P450. Flavokawain A has anti-inflammatory, anti-tumor, and immunomodulatory effects. Flavokawain A can inhibit the proliferation of tumor cells and induce apoptosis. Flavokawain A can be used in the research of diseases such as bladder cancer.

(E)-Flavokawain A, a chalcone extracted from Kava, has anticarcinogenic effect. (E)-Flavokawain A induces apoptosis in bladder cancer cells by involvement of bax protein-dependent and mitochondria-dependent apoptotic pathway and suppresses tumor growth in mice.

Licochalcone C could inhibit α-glucosidase, with IC₅₀s of <100 nM and 92.43 μM for α-glucosidase and protein tyrosine phosphatase 1B (PTP1B), respectively.

Flavokawain B (Flavokavain B) is an orally active chalcone. Flavokawain B results in activation of caspase-9, -3 and -8, cleavage of PARP. Flavokawain B down-regulates Bcl-2 with concomitant increase in Bax level. Flavokawain B inhibits NF-κB, PI3K/Akt and MAPK signaling pathway. Flavokawain B exhibits Apoptotic effects. Flavokawain B inhibits MMP-9 and promotes ROS generation. Flavokawain B inhibits multiple tumors and inflammation.

Licochalcone E, a flavonoid compound isolated from Glycyrrhiza uralensis, inhibits NF-κB and AP-1 transcriptional activity through the inhibition of AKT and MAPK activation.

Isoliquiritin apioside significantly decreases PMA-induced increases in MMP9 activities and suppresses PMA-induced activation of MAPK and NF-κB. Isoliquiritin apioside auppresseses invasiveness and angiogenesis of cancer cells and endothelial cells.

4'-Hydroxychalcone is a chalcone isolated from licorice root, with hepatoprotective activity. 4'-Hydroxychalcone inhibits TNFα-induced NF-κB activation via proteasome inhibition. 4'-Hydroxychalcone induces a rapid potassium release from mitochondrial vesicles and causes deterioration of respiratory control and oxidative phosphorylation of isolated rat liver mitochondria.

Flavokawain C is an orally active natural chalcone. Flavokawain C inhibits the proliferation of various cancer cells. Flavokawain C upregulates GADD153 in cancer cells, inhibits the phosphorylation of Akt and JNK, suppresses early ERK phosphorylation, activates late ERK phosphorylation, activates caspase related subtypes, induces PARP-1 cleavage, causes upregulation of p21 and p27, downregulation of mutant p53 and anti-apoptotic IAP proteins, elevates intracellular ROS levels, reduces SOD activity, and induces apoptosis. Flavokawain C downregulates FABP4, induces autophagy in cancer cells, and activates the AMPK/mTOR pathway. Flavokawain C decreases the expression of glycolysis-related proteins GLUT1 and HK2, and inhibits glycolysis in nasopharyngeal carcinoma cells. Flavokawain C inhibits the activation of the EGFR/PI3K/Akt/mTOR signaling pathway and reduces the expression of HSP90B1. Flavokawain C inhibits angiogenesis by decreasing the expression of angiogenic proteins Ang-1 and VEGF in human umbilical vein endothelial cells. Flavokawain C increases γ-H2AX levels in cells, inhibits the phosphorylation of FAK, PI3K and AKT in cells, and induces DNA damage in cells. Flavokawain C exerts anti-tumor activity in multiple tumor xenograft mouse models. Flavokawain C is applicable to research related to colorectal cancer, colon adenocarcinoma, nephroblastoma, nasopharyngeal carcinoma and liver cancer.

Marein has the neuroprotective effect due to a reduction of damage to mitochondria function and activation of the AMPK signal pathway. Marein improves insulin resistance induced by high glucose in HepG2 cells through CaMKK/AMPK/GLUT1 to promote glucose uptake, through IRS/Akt/GSK-3β to increase glycogen synthesis, and through Akt/FoxO1 to decrease gluconeogenesis. Marein is a HDAC inhibitor with an IC₅₀ of 100 μM. Marein has beneficial antioxidative, antihypertensive, antihyperlipidemic and antidiabetic effects.

3-Deoxysappanchalcone is a natural chalcone compound isolated from the heartwood of Caesalpinia sappan L. 3-Deoxysappanchalcone induces cell cycle arrest, ROS production, and apoptosis. 3-Deoxysappanchalcone exhibits anti-inflammatory, anti-allergic, anticoagulant, and antithrombotic activities. 3-Deoxysappanchalcone is applicable to research related to lung cancer, esophageal squamous cell carcinoma, thrombosis, and influenza virus infection.

Tetrahydroxymethoxychalcone is a phenolic and flavonoid compound. Tetrahydroxymethoxychalcone is found to enhance myoblast proliferation and differentiation. Tetrahydroxymethoxychalcone plays important roles in myogenesis and muscle regeneration.

Pinocembrin chalcone (2',4',6'-Trihydroxychalcone) is an antibacterial compound from Helichrysum Trilineatum. Pinocembrin chalcone facilitates AMP-activated protein kinase (AMPK) activation, improves glucose tolerance, increases muscle FAO and reduces fat accumulation in the liver and skeletal muscles in high-fat diet-induced (HFD) diabetic mice. Pinocembrin chalcone is promising for research of gastric ulcers and diabetes.

Broussochalcone A is an antioxidant and an inhibitor of Xanthine Oxidase (IC₅₀=2.21 μM), with free radical scavenging activity. Broussochalcone A inhibits iron-induced lipid peroxidation and nitric oxide synthesis in lipopolysaccharide (LPS) -activated macrophages. Broussochalcone A also induces Apoptosis of human renal carcinoma cells by increasing ROS levels and activating FOXO3 signaling pathways.