Biflavones

Isoginkgetin is a pre-mRNA splicing inhibitor inhibitor. Isoginkgetin also inhibits activities of both Akt, NF-κB and MMP-9. Isoginkgetin inhibits the activity of the 20S proteasome, induces apoptosis and activates autophagy.

Amentoflavone (Didemethyl-ginkgetin) is a potent and orally active GABA(A) negative modulator. Amentoflavone also shows anti-inflammatory, antioxidative, anti-viral, anti-tumor, anti-radiation, anti-fungal, antibacterial activity. Amentoflavone induces apoptosis and cell cycle arrest at sub-G1 phase.

Procyanidin B2 is a natural flavonoid, with anti-cancer, antioxidant activities.

Procyanidin C1 (PCC1), a natural polyphenol with oral activity, causes DNA damage, cell cycle arrest and induces apoptosis. Procyanidin C1 decreases the level of Bcl-2, but enhances BAX, caspase 3 and 9 expression in cancer cells. Procyanidin C1 shows senotherapeutic activity and increases lifespan in mice.

Proanthocyanidin (Procyanidin) are a class of polyphenolic that are widely distributed in higher plants, consisted of an electrophilic flavanyl unit. Proanthocyanidin can be used as antioxidant and anti-cancers agent. Proanthocyanidin also exhibit anti-inflammatory, cardioprotective, antibacterial and antifungal properties, which can be used in the treatment of chronic venous insufficiency, capillary fragility, sunburn and retinopathy..

Kolaflavanone is an biflavonoid allosteric inhibitor of Eg5. Kolaflavanone inhibits the ATPase and tyrosinase activities of Eg5 under both basal and microtubule-activated conditions, suppresses microtubule sliding activity, binds to the L5/α2/α3 allosteric pocket of Eg5, induces conformational changes of Eg5 and microtubule dissociation, interacts with aldehyde dehydrogenase, inhibits the ATPase activity of kinesin-1, and binds to HSA via pH-dependent forces. Kolaflavanone exhibits antihepatotoxic activity and can be used in studies related to Phalloidin (HY-P0028)-induced liver injury.

(2''S)-2'',3''-Dihydrodelicaflavone is a biflavonoid compound present in the whole herb of Selaginella doederleinii, which exhibits antiproliferative and apoptosis-inducing activities against non-small cell lung cancer cells. (2''S)-2'',3''-Dihydrodelicaflavone can be used in the research of non-small cell lung cancer.

(2''S)-6''-Methyl-2'',3''-Dihydrodelicaflavone is a biflavonoid compound present in the whole herb of Selaginella doederleinii. (2''S)-6''-Methyl-2'',3''-Dihydrodelicaflavone exhibits antiproliferative activity against non-small cell lung cancer cells (IC₅₀ = 3.1-6.8 μM) with low cytotoxicity toward normal cells. (2''S)-6''-Methyl-2'',3''-Dihydrodelicaflavone can be used in studies related to non-small cell lung cancer.

Ginkgetin, a biflavone, is isolated from Ginkgo biloba leaves. Ginkgetin exhibit anti-tumor, anti-inflammatory, neuroprotective, anti-fungal activities. Ginkgetin is also a potent inhibitor of Wnt signaling, with an IC₅₀ of 5.92 μΜ.

Procyanidin B1 is a polyphenolic flavonoid isolated from commonly eaten fruits, binds to TLR4/MD-2 complex, and has anti-inflammatory activity.

Hinokiflavone is a novel modulator of pre-mRNA splicing activity extracted from plants with anti-inflammatory, anti-tumor and antiviral activities. Hinokiflavone is also a potent inhibitor for matrix metalloproteinases (MMPs). Hinokiflavone attenuates the virulence of Methicillin (HY-121544)-resistant staphylococcus aureus by inhibiting caseinolytic protease P (ClpP) with an IC₅₀ value of 34.36 mg/mL. Hinokiflavone induces apoptosis via the reactive oxygen species-mitochondria-mediated apoptotic pathway and inhibits tumor cell migration and invasion. Hinokiflavone is a SUMO protease inhibitor against sentrin-specific protease 1 (SENP1) activity.

Bilobetin, an active component of Ginkgo biloba, can reduce blood lipids and improve the effects of insulin. Bilobetin ameliorated insulin resistance, increased the hepatic uptake and oxidation of lipids, reduced very-low-density lipoprotein triglyceride secretion and blood triglyceride levels, enhanced the expression and activity of enzymes involved in β-oxidation and attenuated the accumulation of triglycerides and their metabolites in tissues. Bilobetin also increased the phosphorylation, nuclear translocation and activity of PPARα accompanied by elevated cAMP level and PKA activity.

Procyanidin A2 is a flavonoid found in grapes, with anti-cancer, antioxidant, antimicrobial and anti-inflammation activity.

Sciadopitysin is a type of biflavonoids in leaves from ginkgo biloba. Sciadopitysi inhibits RANKL-induced osteoclastogenesis and bone loss by inhibiting NF-κB activation and reducing the expression of c-Fos and NFATc1.

Procyanidin A1 (Proanthocyanidin A1) is a procyanidin dimer, which inhibits degranulation downstream of protein kinase C activation or Ca²⁺ influx from an internal store in RBL-213 cells. Procyanidin A1 has antiallergic effects.

Procyanidin B3 is a natural product with antioxidant activity and oral bioavailability, possessing good blood-brain barrier penetration. Procyanidin B3 is a selective inhibitor of histone acetyltransferase (HAT). By inhibiting p300 HAT-mediated acetylation of the androgen receptor (androgen receptor). Procyanidin B3 alleviates intervertebral disc degeneration (IVDD) by inhibiting the formation of the TLR4/MD-2 complex. Procyanidin B3 can be used in research on prostate cancer and arthritis.

Cinnamtannin A2, a tetrameric procyanidin, can increases GLP-1 and insulin secretion in mice. Cinnamtannin A2 could upregulate the expression of corticotrophin releasing hormone. Cinnamtannin A2 exhibits antioxidant, anti-diabetic and nephroprotective effect.

4'-O-Methylochnaflavone is a biflavonoid isolated from Lonicera japonica, suppresses mouse lymphocyte proliferation.

Podocarpusflavone A is a biflavonoid present in the leaves of Podocarpus henkelii, with anti-tumor, topoisomerase I inhibitory, antibacterial and antifungal activities. Podocarpusflavone A exhibits antibacterial activity against Enterococcus faecalis and Pseudomonas aeruginosa. Podocarpusflavone A shows weak activity against fungal pathogens. Podocarpusflavone A targets topoisomerase I and induces cell cycle arrest and apoptosis in MCF-7 cells. Podocarpusflavone A can be used for studies on cancer, bacterial and fungal infections.

Chamaejasmine is a biflavonoid that can be isolated from the roots of Stellera chamaejasme L. Chamaejasmine has antitumor activity. Chamaejasmine induces cell apoptosis, autophagy and ROS production, and activates the activity of AMPK/mTOR signal pathway.