| Description | Gossypetin, a hexahydroxylated flavonoid extractable from Rhodiola rosea Linn. is a potent MKK3 and MKK6 inhibitor that strongly attenuates the MKK3/6-p38 signaling pathway.Gossypetin exhibits antimutagenic, antiatherosclerotic, antioxidant, as well as cytoprotective and antimicrobial effects.It inhibits bone resorption by downregulating lysosomal caspase K activity and inducing autophagy-associated proteins in actin ring osteoclasts. Gossypetin has anti-mutagenic, anti-atherosclerotic, anti-oxidant, cytoprotective and antibacterial effects, and it inhibits bone resorption by down-regulating lysosomal caspase K activity and by inducing autophagy-associated protein in actin ring osteoblasts. |
| In vitro | Gossypetin (60 μM; 3 h; KYSE30 and KYSE410 cells) strongly inhibits p38 activity in a dose-dependent manner and demonstrates that Gossypetin directly inhibits MKK3 or MKK6 activity. [1]Gossypetin (20-60 μM; 48 h; KYSE30, KYSE450, and KYSE510 cells) strongly inhibits anchorage-dependent esophageal cancer cell growth in a dose-dependent manner. [1]Gossypetin (20-40 μM; 48 h; KYSE450 and KYSE510 cells) reduces the S phase and induces cell cycle arrest in the G2 phase in a dose-dependent manner. [1]Gossypetin (20-40 μM; 72 h; esophageal carcinoma cells) induces intrinsic apoptosis in esophageal carcinoma cells. [1] |
| In vivo | Gossypetin (100 mg/kg; p.o.; 5 times a week; for 21 days; (SCID) female mice) leads to a notable reduction in the growth volume of esophageal tumors, while not causing a significant decline in body weight. Moreover, Gossypetin induces a notable decrease in Ki67 expression. Observable morphological distinctions between mouse tissues in treated and untreated groups were absent. Furthermore, Gossypetin treatment strongly suppresses the phosphorylation of p38, an immediate downstream protein of MKK3/6.[1] |
| molecular weight | 318.24 |
| Molecular formula | C15H10O8 |
| CAS | 489-35-0 |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| References | 1. Xie X, et al. Gossypetin is a novel MKK3 and MKK6 inhibitor that suppresses esophageal cancer growth in vitro and in vivo. Cancer Lett. 2019;442:126-136. 2. Antika L D, et al. Dietary compound gossypetin inhibits bone resorption through down-regulating lysosomal cathepsin K activity and autophagy-related protein induction in actin ring-bearing osteoclasts. Journal of Functional Foods. 2016;24:390-402. 3. Wang L, et al. Gossypetin Inhibits Solar-UV Induced Cutaneous Basal Cell Carcinoma Through Direct Inhibiting PBK/TOPK Protein Kinase. Anticancer Agents Med Chem. 2019;19(8):1029-1036. 4. Lin HH. In Vitro and in Vivo Atheroprotective Effects of Gossypetin against Endothelial Cell Injury by Induction of Autophagy. Chem Res Toxicol. 2015;28(2):202-215. 5. Samant NP, et al. Gossypetin- based therapeutics for cognitive dysfunction in chronic unpredictable stress- exposed mice. Metab Brain Dis. 2022;37(5):1527-1539. |