Flavokawain B

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^{[1][2][3][4][5][6][7][8][9][10][11][12][13]}. In Vitro: Flavokawain B (1-5 µg/mL, 18-24 h) inhibits human brain endothelial cell (HUVEC) migration and tube formation^[1].
Flavokawain B (1.25-20 µg/mL, 18 h) induces proliferation inhibition and apoptosis in multiple B-cell lymphoma cell lines through downregulating the PI3K/Akt axis^[3].
Flavokawain B (5-40 µM, 1 h) shows anti-inflammatory activities, with inhibiting production of NO and PGE2 in LPS-induced RAW 264.7 cells^[4].
Flavokawain B (17.6-70.4 μM, 24 h) results in apoptosis of KB cells, evidenced by loss of cell viability, profound morphological changes, genomic DNA fragmentation and sub-G1 phase accumulation^[5].
Flavokawain B (2.5-7.5 µg/mL, 24 h) induces apoptosis in synovial sarcoma cell lines^[6].
Flavokawain B (2.5-7.5 µg/mL, 24 h) inhibits growth of human osteosarcoma cells (143B and saos-2) through G2/M cell cycle arrest and apoptosis^[7].
Flavokawain B (1.25-10 μg/mL, 24 h) induces apoptosis in human oral carcinoma HSC-3 cells through the intracellular ROS generation and downregulation of the Akt/p38 MAPK signaling pathway^[8].
Flavokawain B (2.5-5 μg/mL, 24 h) exhibits robust apoptotic effects and induces G2/M arrest of a uterine leiomyosarcoma cell line SK-LMS-1 and ECC-1^[9].
In Vivo: Flavokawain B (1-2.5 µg/mL, 24 h) suppresses angiogenesis in a zebrafish model^[1].
Flavokawain B (50-200 mg/kg, i.p.) shows anti-inflammatory activities in LPS-induced mice^[4].
Flavokawain B (0.35-0.75 mg/kg, i.p., every 2 days, 27 days) significantly inhibits in vivo growth of human KB cell-derived tumor xenografts in nude mice^[5].
Flavokawain B (20-40 mg/kg, p.o., 7 days) inhibits NF-κB inflammatory signaling pathway activation in colitis mice by targeting TLR2^[10].
Flavokawain B (25 mg/kg, p.o., daily for a week) induces GSH-sensitive oxidative stress in mice through modulation of IKK/NF-κB and MAPK signaling pathways^[11].
Flavokawain B (10-20 mg/kg, i.g., 3 consecutive days) alleviates LPS-induced acute lung injury in mice via targeting myeloid differentiation factor 2^[12].
Flavokawain B (25 mg/kg, i.p., twice-a-week for 2 weeks) in combination with Cisplatin (HY-17394)/Gemcitabine (HY-17026) significantly inhibits tumor growth in a xenograft mouse (SNU-478 cells) model^[13].