Flavokawain A, a natural product isolated and purified from the roots of Piper methysticum with anti-tumor and anti-inflammatory activities, can significantly reduce the expression of CDK1-inhibitory kinases, Myt1 and Wee1, and cause cyclin B1 protein accumulation leading to CDK1 activation in T24 cells.
Flavokawain A/卡瓦胡椒素A 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Syo-I
10 μg/ml
24 or 72 hours
Inhibition of cell proliferation and invasion
Transl Oncol. 2020 Oct;13(10):100809
Hssy-II
10 μg/ml
24 or 72 hours
Inhibition of cell proliferation and invasion
Transl Oncol. 2020 Oct;13(10):100809
T24
40 μM
different times
FKA inhibits PRMT5 expression, thereby inhibiting the growth and inducing apoptosis of bladder cancer cells.
J Exp Clin Cancer Res. 2022 Oct 5;41(1):293
UMUC3
40 μM
different times
FKA inhibits PRMT5 expression, thereby inhibiting the growth and inducing apoptosis of bladder cancer cells.
J Exp Clin Cancer Res. 2022 Oct 5;41(1):293
mouse chondrocytes
20 μM and 40 μM
24 hours
To evaluate the effect of FKA on inflammation and metabolism in chondrocytes. FKA reduced the expression of inflammatory factors (COX2 and iNOS) and catabolic enzymes (ADAMTS5 and MMPs), and upregulated the expression of anabolic proteins (Col2, Aggrecan, and SOX9).
Front Bioeng Biotechnol. 2022 Dec 5;10:1071776
MCF10A
>100 μM
72 hours
FKA has minimal effect on the growth of non-malignant breast epithelial cells.
Molecules. 2017 Mar 14;22(3):462
MDA-MB-468
45 μM
24 hours
FKA inhibits cell growth.
Molecules. 2017 Mar 14;22(3):462
MCF7
38.4 μM
24 hours
FKA induces G1 arrest.
Molecules. 2017 Mar 14;22(3):462
MCF7/HER2
13.6 μM
24 hours
FKA induces G2M arrest by inhibiting phosphorylation of Cdc2 and Cdc25C, downregulating expression of Myt1 and Wee1, and increasing Cdc2 kinase activity.
Molecules. 2017 Mar 14;22(3):462
SKBR3
10 μM
24 hours
FKA induces G2M arrest by inhibiting phosphorylation of Cdc2 and Cdc25C, downregulating expression of Myt1 and Wee1, and increasing Cdc2 kinase activity. Additionally, FKA induces apoptosis in SKBR3 cells by increasing protein expression of Bim and BAX and decreasing expression of Bcl-2, Bcl-X/L, XIAP, and survivin.
Molecules. 2017 Mar 14;22(3):462
STC-1 cells
100 μM
1 hour
stimulated GLP-1 secretion and inhibited DPP-4 enzyme activity
Pharmaceuticals (Basel). 2022 Dec 12;15(12):1543
B16/F10 melanoma cells
25 µM
72 hours
To evaluate cytotoxicity and melanogenesis inhibition, results showed FLA at 25 µM significantly reduced melanin content and tyrosinase activity
Molecules. 2020 Jul 28;25(15):3403
HUVECs
5-25 µmol
24 hours
To evaluate the protective effect of FKA against OTA-induced endothelial cell injury, results showed that FKA significantly inhibited OTA-induced apoptosis and oxidative stress.
Toxins (Basel). 2021 Oct 21;13(11):745
HepG2
50 μM
24 h
To test for subsequent resistance to oxidative stress, FKA pretreatment mitigated cell death after a subsequent challenge with H2O2, being similar to SFN.
Pharm Biol. 2016 Sep;54(9):1503-12
HepG2
2–100 μM
24–48 h
To assess the toxicity of FKA and FKB in HepG2 cells, FKA (≤100μM) was not toxic to HepG2, whereas FKB caused significant cell death (IC50=23.2±0.8μM).
Pharm Biol. 2016 Sep;54(9):1503-12
A7r5 cells
2-30 μM
24 hours
To evaluate the anti-fibrotic and antioxidant properties of FKA in TGF-β1-stimulated A7r5 cells. Results showed that FKA treatment suppressed TGF-β1-induced α-SMA and fibronectin expression and inhibited cell migration and invasion.
J Cell Mol Med. 2019 Feb;23(2):775-788
Flavokawain A/卡瓦胡椒素A 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Balb/c nude mice
Subcutaneous xenograft model
Intraperitoneal injection
30 mg/kg
Every 3 days for 24 days
FKA significantly inhibited tumor growth, reducing tumor volume and weight.
J Exp Clin Cancer Res. 2022 Oct 5;41(1):293
Mice
UPII-mutant Ha-ras transgenic mice
Oral
6 g/kg food
Daily, for 6 months
To evaluate the chemopreventive efficacy of FKA against mutant Ha-ras-driven urothelial tumorigenesis. Results showed that FKA significantly increased the survival rate of male mice, reduced bladder weight (tumor burden), and decreased incidences of hydronephrosis and hematuria.
Pharmaceutics. 2022 Feb 24;14(3):496
SCID mice
Subcutaneous xenograft model
Oral
600 mg/kg/day
Once daily for 6 weeks
Inhibition of tumor growth
Transl Oncol. 2020 Oct;13(10):100809
C57BL/6J male mice
Destabilization of the medial meniscus (DMM) model
Intra-articular injection
50 mg/kg
Once weekly for 8 weeks
To evaluate the therapeutic effect of FKA on OA mice. FKA significantly reduced cartilage damage and increased the expression of Aggrecan and Col2.
Front Bioeng Biotechnol. 2022 Dec 5;10:1071776
Zebrafish (Danio rerio)
IBMX-induced melanogenesis model
Dissolved in embryo media
25 µM
From 9 hpf to 144 hpf
To assess toxicity and melanogenesis inhibition, results showed FLA at 25 μM was non-toxic and effectively inhibited melanogenesis
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