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Amarogentin

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Chemical Structure| 21018-84-8 同义名 : 苦杏苷 ;AG
CAS号 : 21018-84-8
货号 : A647580
分子式 : C29H30O13
纯度 : 97%
分子量 : 586.541
MDL号 : MFCD06656289
存储条件:

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(179.02 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
描述 Amarogentin, a secoiridoid glycoside that is mainly extracted from Swertia and Gentiana roots, has been suggested to exhibit many biological effects, including anti-oxidative, anti-tumour, and anti-diabetic activities. Mice were orally treated with 25, 50, and 100 mg/kg amarogentin and with colchicine as a positive control. Amarogentin delayed the formation of liver fibrosis; decreased alanine aminotransferase, aspartate aminotransferase, malondialdehyde and hydroxyproline levels; and increased albumin, cyclic guanosine monophosphate, glutathione peroxidase, and superoxide dismutase levels. Moreover, amarogentin exhibited downregulation of α-smooth muscle actin and transforming growth factor-β₁ levels in immunohistochemical and Western blot analyses[4]. Amarogentin as an agonist for TAS2R1 and other TAS2Rs promotes keratinocyte differentiation. Amarogentin inhibited in LAD-2 cells substance P-induced production of newly synthesized TNF-α, but the degranulation and release of stored histamine were not affected[5]. Amarogentin induced potent, dose-dependent as well as time-dependent cytotoxic effects on the growth of SNU-16 human gastric cancer cells. Amarogentin also inhibited the colony forming capability of these tumor cells and its treatment led to morphological alterations in these cells in which the cells became withered and rounded, detached from one another and adopted irregular shapes while floating freely in the culture medium. In comparison to untreated control cells, the amarogentin treated cells with 10, 50 and 75 μM exhibited 32.5, 45.2 and 57.1 % apoptotic cells, respectively. Amarogentin induced potent and dose-dependent G2/M cell cycle arrest in these cells and led to downregulation of m-TOR, p-PI3K, PI3K, p-Akt and Akt and upregulation of cyclin D1 and cyclin E protein expressions[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.70mL

0.34mL

0.17mL

8.52mL

1.70mL

0.85mL

17.05mL

3.41mL

1.70mL

参考文献

[1]Zhang Y, et al. Protective Effects of Amarogentin against Carbon Tetrachloride-Induced Liver Fibrosis in Mice. Molecules. 2017 May 6;22(5). pii: E754.

[2]Wölfle U, et al. Amarogentin Displays Immunomodulatory Effects in Human Mast Cells and Keratinocytes. Mediators Inflamm. 2015;2015:630128.

[3]Zhao JG, et al. Amarogentin secoiridoid inhibits in vivo cancer cell growth in xenograft mice model and induces apoptosis in human gastric cancer cells (SNU-16) through G2/M cell cycle arrest and PI3K/Akt signalling pathway. J BUON. 2016 May-Jun;21(3):609-17.

[4]Zhang Y, Zhao H, Li H, Cao W, Wang F, Zhang T, Wang SW. Protective Effects of Amarogentin against Carbon Tetrachloride-Induced Liver Fibrosis in Mice. Molecules. 2017 May 6;22(5):754

[5]Wölfle U, Haarhaus B, Schempp CM. Amarogentin Displays Immunomodulatory Effects in Human Mast Cells and Keratinocytes. Mediators Inflamm. 2015;2015:630128

[6]Zhao JG, Zhang L, Xiang XJ, Yu F, Ye WL, Wu DP, Wang JF, Xiong JP. Amarogentin secoiridoid inhibits in vivo cancer cell growth in xenograft mice model and induces apoptosis in human gastric cancer cells (SNU-16) through G2/M cell cycle arrest and PI3K/Akt signalling pathway. J BUON. 2016 May-Jun;21(3):609-17. Erratum in: J BUON. 2016 Sept-Oct;21(5):1332