Ginkgetin is a natural biflavonoid isolated from leaves of Ginkgo biloba L; effects of anti-inflammation and anticancer have been reported.IC50 value:Target:in vitro: Ginkgetin inhibits COX-2 dependent phases of prostaglandin D(2) (PGD(2)) generation in bone marrow-derived mast cells (BMMC) in a concentration-dependent manner with IC(50) values of 0.75 microM. Ginkgetin consistently inhibited the production of leukotriene C(4) (LTC(4)) in a dose dependent manner, with an IC(50) value of 0.33 microM. Ginkgetin also inhibited degranulation reaction in a dose dependent manner, with an IC(50) value of 6.52 microM [1]. Ginkgetin inhibited both inducible and constitutively activated STAT3 and blocked the nuclear translocation of p-STAT3 in DU-145 prostate cancer cells. Furthermore, ginkgetin selectively inhibited the growth of prostate tumor cells stimulated with activated STAT3. Ginkgetin induced STAT3 dephosphorylation at Try705 and inhibited its localization to the nucleus, leading to the inhibition of expression of STAT3 target genes such as cell survival-related genes (cyclin D1 and survivin) and anti-apoptotic proteins (Bcl-2 and Bcl-xL) [2]. Ginkgetin suppressed the viability of PC-3 cells in a concentration-dependent manner and also significantly increased the sub-G1 DNA contents of cell cycle in PC-3 cells. Ginkgetin activated caspase-3 and attenuated the expression of survival genes such as Bcl-2, Bcl-xL, survivin and Cyclin D1 at protein and mRNA levels [3]. Ginkgetin (1 - 10 microM) and the biflavonoid mixture (10 - 50 microg/ml), mainly a 1 : 1 mixture of ginkgetin and isoginkgetin, from G. biloba leaves, inhibited production of prostaglandin E2 from lipopolysaccharide-induced RAW 264.7 cells [4].in vivo: Ginkgetin inhibited tumor growth in xenografted nude mice and down-regulated p-STAT3Tyr705 and survivin in tumor tissues [2]. At total doses of 1,000 microg/site on the dorsal skin (15 mm x 15 mm), ginkgetin inhibited prostaglandin E2 production by 65.6 % along with a marked suppression of COX-2 induction. In addition, ginkgetin and the biflavonoid mixture (100 - 1,000 microg/ear) dose-dependently inhibited skin inflammation of croton oil induced ear edema in mice by topical application [4].
Sagittatoside A is a natural compound isolated from traditional Chinese herb Yinyanghuo (Herba Epimdii).
Miquelianin (Quercetin 3-O-glucuronide) is a metabolite of quercetin and a type of natural flavonoid.
Proanthocyanidins are a class of polyphenols with antibacterial, antifungal and antiviral activities, which can be used in the treatment of chronic venous insufficiency, capillary fragility, sunburn and retinopathy.
Baicalin is a flavonoid glycoside isolated from Scutellaria baicalensis. Baicalin reduces the expression of NF-κB.
Biochanin A is a naturally occurring fatty acid amide hydrolase (FAAH) inhibitor, which inhibits FAAH with IC50s of 1.8, 1.4 and 2.4 μM for mouse, rat, and human FAAH, respectively.
Eriodictyol is a flavonoid isolated from the Chinese herb, with antioxidant and anti-inflammatory activity. Eriodictyol induces Nrf2 signaling pathway.
Isoquercitrin is an effective antioxidant and an eosinophilic inflammation suppressor.
Luteolin-3-O-beta-D-glucuronide is a luteolin glucosiduronic acid consisting of luteolin having a beta-D-glucosiduronic acid residue attached at the 3'-position.
Isomangiferin, a natural product, is reported to have antiviral activity.
Isoorientin is a potent inhibitor of COX-2 with an IC50 value of 39 μM.
Sophoricoside is an isoflavone glycoside isolated from Sophora japonica and has anti-inflammatory, anti-cancer and immunosuppressive effects.
Scutellarin, a main active ingredient extracted from Erigeron breviscapus (Vant.) Hand-Mazz., has been wildly used to treat acute cerebral infarction and paralysis induced by cerebrovascular diseases.
Complanatuside is a flavonoid found in the traditional Chinese medicine Semen Astragali Complanati.
(-)-Epigallocatechin Gallate is an antioxidant polyphenol flavonoid form green tea, and inhibits the activation of EGFR, HER2 and HER3, with antitumor activity.
Procyanidin B2 is a natural flavonoid, with anti-cancer, antioxidant activities.
IKarisoside A(Icarisoside-A) is a natural compound isolated from Epimedium koreanum (Berberidaceae); has anti-inflammatory properties.IC50 value:Target: in vitro: Ikarisoside A inhibited the expression of LPS-stimulated inducible nitric oxide synthase (iNOS) and the production of nitric oxide (NO) in LPS-stimulated RAW 264.7 cells and mouse bone marrow-derived macrophages (BMMs) in a concentration-dependent manner. In addition, Ikarisoside A reduced the release of pro-inflammatory cytokines, such as tumor necrosis factor-alpha (TNF-alpha) and interleukin-1 beta (IL-1 beta). Furthermore, Ikarisoside A inhibited the activity of p38 kinase and nuclear factor-kappaB (NF-kappaB) [1]. Ikarisoside A is a potent inhibitor of osteoclastogenesis in RANKL-stimulated RAW 264.7 cells as well as in bone marrow-derived macrophages.The inhibitory effect of Ikarisoside A resulted in decrease of osteoclast-specific genes like matrix metalloproteinase 9 (MMP9), tartrate-resistant acid phosphatase (TRAP), receptor activator of NF-kappaB (RANK), and cathepsin K. Moreover, Ikarisoside A blocked the resorbing capacity of RAW 264.7 cells on calcium phosphate-coated plates. Ikarisoside A also has inhibitory effects on the RANKL-mediated activation of NF-kappaB, JNK, and Akt [2].
Isotanshinone I has inhibitory activity against α-glucosidase and formation of AGE, with IC50s of 1.13, 0.432 μM for α-glucosidase and AGE, respectively.
Naringenin is the predominant flavanone in grapefruit; displays strong anti-inflammatory and antioxidant activities.
Isoliquiritigenin is an anti-tumor flavonoid from the root of Glycyrrhiza glabra, which inhibits aldose reductase with an IC50 of 320 nM.
Nobiletin is a citrus flavonoid with anti-inflammatory, anti-cancer, cholesterol lowering, memory protection activities.
6-shogaol, an active compound isolated from Ginger (Zingiber officinale Rosc), exhibits a variety of biological activities including anticancer, anti-inflammation, and anti-oxidation.
Safflower yellow is extracted from the flowers of the plant safflower (Carthamus tinctorius) and as the traditional Chinese medicine it has been extensively used for the treatment of cardio cerebrovascular diseases.
Pomiferin, a flavonoid from the fruits of Maclura pomifera, acts as an potential inhibitor of HDAC, with an IC50 of 1.05 μM, and also potently inhibits mTOR (IC50, 6.2 µM).
Isosakuranetin is a flavanone flavonoid which can be found in the fruit of Citrus bergamia.
Wogonin is a naturally occurring mono-flavonoid, can inhibit the activity of CDK8 and Wnt, and exhibits anti-inflammatory and anti-tumor effects.
7-Methoxyisoflavone is an isoflavone derivative and also an activator of adenosine monophosphate-activated protein kinase (AMPK).