Guggulsterone is a plant sterol extracted from the resin of the plant Commiphora wightii. Guggulsterone can inhibit the growth of a wide variety of tumor cells and induce apoptosis through downregulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP, and survivin), modulation of cell cycle proteins (such as Cyclin D1 and c-Myc), activation of caspases, inhibition of Akt, and activation of JNK[1].
In vitro, Guggulsterone (22.28μM; 8 days) inhibits clone-forming potential of liver cancer cells[2]. Guggulsterone (0, 15, 50 and 75µM; 24h) dose-dependently inhibites SGC-7901 cell proliferation[3].
In vivo, Guggulsterone (5 or 10mg/kg; on days 1, 3, and 5 post-infection; i.p.) decreases mortality in dengue virus (DENV) infected ICR suckling mice[4]. In an in vivo xenograft mouse model, Guggulsterone (20 or 40mg/kg; 14 days; oral administration) significantly reduced tumor growth in a dose-dependent manner[5].
References:
[1] Shishodia S, Azu N, Rosenzweig JA, et al. Guggulsterone for Chemoprevention of Cancer. Curr Pharm Des. 2016;22(3):294-306.
[2] Gupta M, Ghufran SM, Kausar T, et al. Z-Guggulsterone Is a Potential Lead Molecule of Dawa-ul-Kurkum against Hepatocellular Carcinoma. Molecules. 2022 Aug 11;27(16):5104.
[3] Lv R, Zhu M, Chen K, et al. Z-Guggulsterone Induces Apoptosis in Gastric Cancer Cells through the Intrinsic Mitochondria-Dependent Pathway. ScientificWorldJournal. 2021 Jan 4;2021:3152304.
[4] Chen WC, Wei CK, Hossen M, et al. (E)-Guggulsterone Inhibits Dengue Virus Replication by Upregulating Antiviral Interferon Responses through the Induction of Heme Oxygenase-1 Expression. Viruses. 2021 Apr 20;13(4):712.
[5] Wu Y, Zhou T, Qian D, et al. Z-Guggulsterone Induces Cell Cycle Arrest and Apoptosis by Targeting the p53/CCNB1/PLK1 Pathway in Triple-Negative Breast Cancer. ACS Omega. 2023 Jan 3;8(2):2780-2792.
Guggulsterone是一种从植物Commiphora wightii的树脂中提取的植物甾醇。Guggulsterone可以抑制多种肿瘤细胞的生长，并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（如Cyclin D1和c-Myc）、激活半胱氨酸蛋白酶、抑制Akt以及激活JNK来诱导细胞凋亡[1]。
在体外实验中，Guggulsterone（22.28μM; 8天）抑制肝癌细胞的克隆形成能力[2]。Guggulsterone（0, 15, 50和75µM; 24小时）剂量依赖性地抑制SGC-7901细胞增殖[3]。
在体内实验中，Guggulsterone（5或10mg/kg; 感染后第1, 3和5天; 腹腔注射）降低了感染登革热病毒（DENV）的ICR乳鼠的死亡率[4]。在体内异种移植小鼠模型中，Guggulsterone（20或40mg/kg；14天；口服）以剂量依赖性方式显著减少了肿瘤生长[5]。