Chalcones

Isoliquiritigenin is an anti-tumor flavonoid from the root of Glycyrrhiza uralensis Fisch., which inhibits aldose reductase with an IC₅₀ of 320 nM. Isoliquiritigenin is a potent inhibitor of influenza virus replication with an EC₅₀ of 24.7 μM.

Rottlerin, a natural product purified from Mallotus Philippinensis, is a specific PKC inhibitor, with IC₅₀ values for PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM. Rottlerin acts as a direct mitochondrial uncoupler, and stimulates autophagy by targeting a signaling cascade upstream of mTORC1. Rottlerin induces apoptosis via caspase 3 activation. Rottlerin inhibits HIV-1 integration and Rabies virus (RABV) infection.

Hydroxysafflor yellow A (Safflomin A) is a natural product of flavonoids isolated from safflower. Hydroxysafflor yellow A can inhibit cell proliferation and promote apoptosis through the autophagy pathway. Hydroxysafflor yellow A has anti-inflammatory, antioxidant and antitumor effects. Hydroxysafflor yellow A can be used in the study of cardiovascular disease.

Licochalcone A (LCA), a chalconoid, presents obvious anti-cancer effects, displays broad-spectrum inhibition against UDP-glucuronosyltransferases (UGTs). Licochalcone A (LCA) exhibits strong inhibitory effects against UGT1A1, 1A3, 1A4, 1A6, 1A7, 1A9, and 2B7 (both IC₅₀ and K_i values lower than 5 μM) .

Xanthohumol is one of the principal flavonoids isolated from hops, the inhibitor of diacylglycerol acetyltransferase (DGAT), COX-1 and COX-2, and shows anti-cancer and anti-angiogenic activities. Xanthohumol also has antiviral activity against bovine viral diarrhea virus (BVDV), rhinovirus, HSV-1, HSV-2 and cytomegalovirus (CMV).

Xanthoangelol F is a prenylated (geranylated) chalcone and Antibacterial agent. Xanthoangelol F can be isolated from Angelica keiskei. Xanthoangelol F inhibits the growth of Gram-positive bacteria Bacillus subtilis, Staphylococcus epidermidis, and Micrococcus luteus, with an MIC of 64 μg/mL.

Sophoradin is an isoprenyl chalcone and component of Guang-Dou-Gen (Shan-Dou-Gen). Sophoradin can be found in the roots of Sophora subprostrata CHUN et T. CHEN (Leguminosae). Sophoradin can be used for the research of tumors.

Licoagrochalcone A is a PTP1B inhibitor. Licoagrochalcone A exerts protective effects against liver cell injury induced by carbon tetrachloride and Acetaminophen (HY-66005). Licoagrochalcone A is applicable to the research of type 2 diabetes, obesity and liver injury.

Butein is a cAMP-specific PDE inhibitor with an IC₅₀ of 10.4 μM for PDE4. Butein is a specific protein tyrosine kinase inhibitor with IC₅₀s of 16 and 65 μM for EGFR and p60^c-src in HepG2 cells. Butein sensitizes HeLa cells to Cisplatin through AKT and ERK/p38 MAPK pathways by targeting FoxO3a. Butein is a SIRT1 activator (STAC).

Echinatin is a chalcone isolated from the Chinese herbal medicine Gancao with hepatoprotective and anti-inflammatory effects. Echinatin can be quickly absorbed and eliminated and extensively distributed with an absolute bioavailability of approximately 6.81% in Rat.

Licochalcone B is an extract from the root of Glycyrrhiza uralensis. Licochalcone B inhibits amyloid β (₄₂) self-aggregation (IC₅₀=2.16 μM) and disaggregate pre-formed Aβ₄₂ fibrils, reduce metal-induced Aβ₄₂ aggregation through chelating metal ionsLicochalcone B inhibits phosphorylation of NF-κB p65 in LPS signaling pathway. Licochalcone B inhibits growth and induces apoptosis of NSCLC cells. Licochalcone B specifically inhibits the NLRP3 inflammasome by disrupting NEK7‐NLRP3 interaction.

Isobavachalcone (Corylifolinin) is derived from Psoralea corylifolia Linn. and is a potent inhibitor of Akt signaling pathway, which induces apoptosis in human cancer cells (Inhibits OVCAR-8 cell growth with an IC₅₀ value of 7.92 μM). Isobavachalcone also induces Reactive Oxyen Species (ROS) generation in OVCAR-8 cells and has exhibit cancer anti-promotive and anti-proliferative activity.

Okanin, effective constituent of the flower tea Coreopsis tinctoria, attenuates LPS-induced microglial activation through inhibition of the TLR4/NF-κB signaling pathways.

Cardamonin can be found from cardamom, and can target various signaling molecules, transcriptional factors, cytokines and enzymes. Cardamonin can inhibit mTOR, NF-κB, Akt, STAT3, Wnt/β-catenin and COX-2. Cardamonin shows anticancer, anti-inflammatory, antimicrobial and antidiabetic activities.

Naringenin chalcone is an orally active intermediate in flavonol biosynthesis. Naringenin chalcone induces Apoptosis. Naringenin chalcone inhibits the production of MCP-1 and NO. Naringenin chalcone exhibits anticancer activity against glioblastoma. Naringenin chalcone has anti-inflammatory and anti-allergic properties.

Isoliquiritin, isolated from Licorice Root, inhibits angiogenesis and tube formation. Isoliquiritin also exhibits antidepressant-like, anti-oxidative, anti-Inflammatory effects and antifungal activity.

Licochalcone D, a flavonoid compound mainly existing in the root of Glycyrrhiza uralensis, is a potent and orally active inhibitor of NF-kappaB (NF-κB) p65. Licochalcone D possesses antioxidant, anti-inflammatory, anti-cancer properties.

4-Hydroxyderricin, the major active ingredients of Angelica keiskei Koidzumi, is an orally active, potent selective MAO-B (Monoamine oxidase inhibitors) inhibitor with an IC₅₀ of 3.43 μM. 4-Hydroxyderricin also mildly inhibits dopamine β (DBH)-hydroxylase activity. 4-Hydroxyderricin has antidepressant activity, anti-allergic, anti-diabetic, anti-oxidant, and antitumor effects. 4-Hydroxyderricin promotes apoptosis and cell cycle arrest through regulating PI3K/AKT/mTOR pathway in hepatocellular cells. 4-Hydroxyderricin inhibits osteoclast formation and accelerates osteoblast differentiation. 4-Hydroxyderricin is promising for research of inflammatory diseases.

Helichrysetin is isolated from the flower Helichrysum odoratissimum. Helichrysetin is an ID2 (DNA binding inhibitor 2) inhibitor. Helichrysetin induces apoptosis. Helichrysetin has anti-tumor and antioxidant activity.

Xanthoangelol, extracted from Angelica keiskei, suppresses obesity-induced inflammatory responses. Xanthoangelol possesses antibacterial activity. Xanthoangelol inhibits monoamine oxidases. Xanthoangelol induces apoptosis in neuroblastoma and leukemia cells.