Guggulsterone

Guggulsterone 是一种植物甾醇，来自于 Commiphora wightii 的树胶树脂。 Guggulsterone 通过下调抗凋亡基因产物（IAP1、xIAP、Bfl-1/A1、Bcl-2、cFLIP 和 survivin），调节细胞周期蛋白（cyclin D1 和c-Myc)，激活半胱天冬酶和 JNK，抑制 Akt。 Guggulsterone 是一种法尼醇 X 受体 (FXR) 拮抗剂，可降低 CDCA 诱导的 FXR 活化，对 Z- 和 E-Guggulsterone 的 IC50

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库存: 现货

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10mg

￥1412.00

1130.00

- +
50mg

￥4312.00

3450.00

- +

已选 0 种 0 瓶

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Background

Guggulsterone is a plant sterol derived from the gum resin of the tree Commiphora wightii. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt[1]. Guggulsterone, a farnesoid X receptor (FXR) antagonist, decreases CDCA-induced FXR activation with IC50s of 17 and 15 μM for Z- and E-Guggulsterone, respectively[2].

Guggulsterone (0.5-20 μM; 24 hours) suppresses TREM-1, TLR4 and TNF-α expression as well as the phosphorylation of IκBα and NF-κB p65 by LPS[2].

Guggulsterone (orally; 100 mg/kg once per day for 8 days) significantly improved the survival rates of wild-type mice with TNBS-induced colitis[2].

参考文献:
[1]. Shishodia S, et al. Guggulsterone for Chemoprevention of Cancer. Curr Pharm Des. 2016;22(3):294-306.
[2]. Che X, et al. Protective effects of guggulsterone against colitis are associated with the suppression of TREM-1 and modulation of macrophages. Am J Physiol Gastrointest Liver Physiol. 2018 Jul 1;315(1):G128-G139.