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Deguelin

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Chemical Structure| 522-17-8 同义名 : 魚藤素 ;(-)-Deguelin;(-)-cis-Deguelin;(−)-cis-Deguelin
CAS号 : 522-17-8
货号 : A139886
分子式 : C23H22O6
纯度 : 99%+
分子量 : 394.417
MDL号 : MFCD01740600
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(266.22 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • PI3K

  • Akt
描述 Deguelin is one of four major naturally occurring rotenoids isolated from root extracts and is best recognized as a NADH: ubiquinone oxidoreductase (complex I) inhibitor, resulting in significant alterations in mitochondrial function, and it is also a potential PI3K/AKT inhibitor[3]. As a natural agent for chemotherapy, deguelin remarkably suppresses proliferation in numerous solid cancers. Nevertheless, the molecular mechanisms of its suppression are still insufficient[4]. In the mouse skin study, deguelin reduced tumor incidence from 60% in the control group to 10% in the group treated with a dose of 33 µg, and multiplicity was reduced from 4.2 in the control group to 0.1 in the treatment group. When the dose was increased 10-fold to 330 µg, no tumors were observed in the treatment group[5]. Deguelin has been reported to elicit PD-like symptoms (degeneration of the dopaminergic pathway) in rats administered with deguelin (6 mg/kg/day for 6 days), possibly through the inhibition of mitochondrial complex I[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.54mL

0.51mL

0.25mL

12.68mL

2.54mL

1.27mL

25.35mL

5.07mL

2.54mL
参考文献

[1]Kim JH, Kim JH, et al. Antiangiogenic effect of deguelin on choroidal neovascularization. J Pharmacol Exp Ther. 2008 Feb;324(2):643-7. Epub 2007 Oct 29.

[2]Bortul R, Tazzari PL, et al. Deguelin, A PI3K/AKT inhibitor, enhances chemosensitivity of leukaemia cells with an active PI3K/AKT pathway. Br J Haematol. 2005 Jun;129(5):677-86.

[3]Boyd J, Han A. Deguelin and Its Role in Chronic Diseases. Adv Exp Med Biol. 2016;929:363-375. doi: 10.1007/978-3-319-41342-6_16. PMID: 27771933.

[4]Wang A, Wang W, Chen Y, Ma F, Wei X, Bi Y. Deguelin induces PUMA-mediated apoptosis and promotes sensitivity of lung cancer cells (LCCs) to doxorubicin (Dox). Mol Cell Biochem. 2018 May;442(1-2):177-186. doi: 10.1007/s11010-017-3202-y. Epub 2017 Oct 13. PMID: 29030732.

[5]Udeani GO, Gerhauser C, Thomas CF, Moon RC, Kosmeder JW, Kinghorn AD, Moriarty RM, Pezzuto JM. Cancer chemopreventive activity mediated by deguelin, a naturally occurring rotenoid. Cancer Res. 1997 Aug 15;57(16):3424-8. PMID: 9270008.