Flavonones

(-)-Epigallocatechin Gallate (EGCG) is a major polyphenol in green tea, which can inhibit cell proliferation and induce cell apoptosis. (-)-Epigallocatechin Gallate inhibits glutamate dehydrogenase 1/2 (GDH1/2, GLUD1/2) activity. (-)-Epigallocatechin Gallate has a potent anticancer, antioxidant and anti-inflammatory properties against various types of cancers such as colorectal cancer, myeloid leukemia, thyroid carcinoma.

Naringenin is the predominant flavanone in Citrus reticulata Blanco; displays strong anti-inflammatory and antioxidant activities. Naringenin has anti-dengue virus (DENV) activity.

Hesperidin (Hesperetin 7-rutinoside), a flavanone glycoside, is isolated from citrus fruits. Hesperidin has numerous biological properties, such as decreasing inflammatory mediators and exerting significant antioxidant effects. Hesperidin also exhibits antitumor and antiallergic activities.

Hesperetin is a natural flavanone that can be found in citrus, and acts as a potent and orally active broad-spectrum inhibitor against human UGT activity. Hesperetin induces apoptosis via p38 MAPK activation. Hesperetin displays a range of bioactivities including antioxidant, anti-inflammatory, and anti-cancer. Hesperetin is found to induce cell-cycle arrest at G2/M phase. Hesperetin can reduce Bcl-2 and enhance BaxM. Hesperetin induces apoptosis through inhibiting NF-κB receptor.

Naringin is a major flavanone glycoside obtained from tomatoes, grapefruits, and many other citrus fruits. Naringin exhibits biological properties such as antioxidant, anti-inflammatory, and antiapoptotic activities. Naringin also inhibits proliferation and invasion and induces apoptosis in human osteosarcoma cells by inhibiting zinc finger E-box binding homeobox 1 (Zeb1).

Duartin is an isoflavan that exists in the heartwood of Dalbergia odorifera T. Chen, Machaerium opacum, and Machaerium villosum Vog. Duartin shows no obvious inhibitory effect on prostaglandin biosynthesis, fails to alleviate rat paw edema induced by carrageenan, dextran, or histamine, and cannot inhibit carrageenan-induced pleurisy in rats, reduce exudate volume, or suppress leukocyte migration.

Brutieridin (Compound 1) is a flavanone glycoside that can be isolated from the juice of bergamot (Citrus bergamia). Brutieridin reduces the level of NPC1L1 in intestinal epithelial cells. Brutieridin decreases cholesterol uptake by intestinal epithelial cells. Brutieridin reduces HMGR activity. Brutieridin can be used in the research of hypercholesterolemia.

Kuwanon L is an HIV-1 integrase (HIV-1 integrase) inhibitor, with IC₅₀ values of 42 μM and 34 μM for LEDGF-dependent and LEDGF-independent integrase, respectively. Kuwanon L blocks the interaction between HIV-1 integrase and LEDGF/p75, with an IC₅₀ of 22 μM. Kuwanon L inhibits HIV-1 replication in immune cells. Kuwanon L is applicable to research related to HIV-1 infection.

Liquiritin, a flavonoid isolated from Glycyrrhiza uralensis, is a potent and competitive AKR1C1 inhibitor with IC₅₀s of 0.62 μM, 0.61 μM, and 3.72μM for AKR1C1, AKR1C2 and AKR1C3, respectively. Liquiritin efficiently inhibits progesterone metabolism mediated by AKR1C1 in vivo. Liquiritin acts as an antioxidant and has neuroprotective, anti-cancer and anti-inflammatory activity.

Eriodictyol ((±)-Huazhongilexone; Dihydroluteolin) is an orally active TRPV1 receptor antagonist (IC₅₀=44-47 nM, rTRPV1) with antioxidant and anti-inflammatory activities. Eriodictyol effectively inhibits lipid peroxidation and the release of proinflammatory cytokines by specifically antagonizing the TRPV1 receptor and activating the Nrf2 signaling pathway. Eriodictyol reduces the levels of ICAM-1, VEGF, eNOS and TNF-α in the retina and maintains the integrity of the blood-retinal barrier. Eriodictyol alleviates oxidative stress-induced apoptosis and hyperalgesia, enhances the activity and cytotoxicity of immune cells (such as B lymphocytes, NK cells and macrophages), and increases the levels of antioxidant enzymes simultaneously. Eriodictyol can be used in the research of diabetic retinopathy, acute lung injury and various pain-related diseases.

Liquiritigenin, a flavanone isolated from Glycyrrhiza uralensis, is a highly selective estrogen receptor β (ERβ) agonist with an EC₅₀ of 36.5 nM for activation of the ERE tk-Luc.

Pinocembrin ((+)-Pinocoembrin) is a flavonoid found in propolis, acts as a competitive inhibitor of histidine decarboxylase, and is an effective anti-allergic agent, with antioxidant, antimicrobial and anti-inflammatory properties.

Eriocitrin is a flavonoid isolated from lemons that is a powerful antioxidant. Eriocitrin inhibits the proliferation of liver cancer cells by arresting the cell cycle in the S phase by upregulating p53, cyclin A, cyclin D3 and CDK6. Eriocitrin triggers apoptosis by activating intrinsic signaling pathways involving mitochondria.

Farrerol is a bioactive constituent of Rhododendron, with broad activities such as anti-oxidative, anti-inflammatory, anti-tumor, neuroprotective and hepatoprotective effects.

Neohesperidin is a flavonoid compound abundant in citrus plants with antioxidant and anti-inflammatory effects. Neohesperidin can upregulate the Wnt/β-catenin signaling pathway, enhance the nuclear translocation of β-catenin and the differentiation of bone marrow stromal cells.

Narirutin, one of the active constituents isolated from citrus fruits, has antioxidant and anti-inflammatory activities. Narirutin is a shikimate kinase inhibitor with anti-tubercular potency.

Didymin, a flavonoid glycoside, possesses antioxidant and anticancer properties. Didymin induces apoptosis by inhibiting N-Myc and upregulating RKIP in neuroblastoma.

Alpinetin is a flavonoid isolated from cardamom and possesses antitumor, antiinflammation, hepatoprotective, cardiovascular protective, lung protective, antibacterial, antiviral, neuroprotective properties. Alpinetin inhibits lipopolysaccharide (LPS)-induced inflammation, activates PPAR-γ, activates Nrf2, and inhibits TLR4 expression to protect LPS-induced renal injury.

Bavachin, a flavonoid first isolated from seeds of P. corylifolia, acts as a phytoestrogen that activates the estrogen receptors ERα and ERβ with EC₅₀s of 320 and 680 nM, respectively.

Bavachinin is agonist of pan-peroxisome proliferator-activated receptor (PPAR), with the IC₅₀ value of 21.043 μM, 12.819 μM, and 0.622 μM to PPAR-α, RRAR-β/δ, and PPAR-γ, respectively. Bavachinin is an inhibitor of HIF-1α. Bavachinin exhibits antitumor activity against non-small cell lung cancer by targeting RRAR-γ. Bavachinin is a natural compound with anti-inflammatory and anti-angiogenic activities. Bavachinin has orally bioactivity..