Tigloylgomisin H 是分离自S. chinensis果实中的木酚素。Tigloylgomisin H 能诱导小鼠肝癌细胞 Hepa1c1c7 中醌还原酶活性。Tigloylgomisin H 是单功能诱导剂,通过 Nrf2-ARE 途径特异性上调 II 期解毒酶 NQO1。Tigloylgomisin H 是潜在的肝癌预防剂。
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描述
Tigloylgomisin H significantly induces quinone reductase (QR) activity in Hepa1c1c7 mouse hepatocarcinoma cells. Tigloylgomisin H functions as a novel monofunctional inducer that specifically upregulates phase II enzymes through the Nrf2-ARE pathway and can be used in liver cancer prevention studies.
体外活性
In the current study, nine lignans were isolated from S. chinensis and tested for their ability to induce quinone reductase (QR) activity in Hepa1c1c7 mouse hepatocarcinoma cells. Tigloylgomisin H (TGH) and angeloylgomisin H (AGH) significantly induced QR activity and exhibited a relatively high chemoprevention index (CI) (10.80 and 4.59, respectively) as compared to control. TGH also induced QR activity in BPrc1 mouse hepatocarcinoma cells as well, which are defective in aryl hydrocarbon nuclear translocator (Arnt). In HepG2 human hepatocarcinoma cells, TGH significantly activated gene expression mediated by the antioxidant response element (ARE), a key regulatory region in the promoters of detoxification enzymes, through the nuclear accumulation of Nrf2.
Cas No.
66069-55-4
分子式
C28H36O8
分子量
500.58
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years