CAS |
No.55659-75-1 |
中文名称 |
三角叶薯蓣皂苷 |
英文名称 |
Deltonin |
分子式 |
C45H72O17 |
分子量 |
885.04 |
溶解性 |
Soluble in DMSO ≥5mg/mL |
纯度 |
≥98% |
外观(性状) |
White to off-white Solid |
储存条件 |
Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year |
靶点 |
ERK;Akt |
通路 |
MAPK;PI3K/Akt/mTOR |
背景说明 |
Deltonin 是一种甾体皂苷,能够抑制 ERK1/2 和 AKT 的活化,具有抗肿瘤的活性。 |
生物活性 |
Deltonin, a steroidal saponin, isolated from Dioscorea zingiberensis, has antitumor activity; Deltonin inhibits ERK1/2 and AKT activation.[1-2] |
In Vitro |
Deltonin inhibits ERK1/2 and AKT activation. Deltonin (0.5-8 μM) significantly inhibits the proliferation of several colon cancer cell lines including SW480, SW620, LOVO and C26, with IC50s of 1.3, 1.29, 2.11 and 1.22 μM. Deltonin also causes G2-M phase arrest and induces apoptosis in C26 cells[1]. Deltonin (0-5 μM) decreases the phosphorylation of AKT and ERK1/2 levels in MDA-MB-231 cells. Deltonin (0.5-8 μM) also dose-dependently inhibits the proliferation, and causes apoptosis with ROS production in MDA-MB-231 cells[2]. |
In Vivo |
Deltonin (20 and 40 mg/kg, p.o.) reduces the tumor growth of 37.7% and 56.7%, and causes a 50-day survival rate of 60% and 50%, respectively, in mice. Deltonin also inhibits tumor angiogenesis in mice[1]. |
细胞实验 |
The cytotoxicity of Deltonin on colon cancer cells is determined by the MTT assay. Cells are seeded at a density of 3 × 103 per well in 96-well plates. After incubation overnight, cells are treated with Deltonin in various concentrations (0.5, 1, 2, 4, 8 μM), and carrier DMSO (50) is calculated[1]. |
动物实验 |
Mice[1]Briefly, 5 × 105 C26 cells are s.c. injected into 4- to 6-wk-old male BALB/c mice. The mice are randomly divided into four groups of 10 mice. One week after C26 implantation, the treatment groups receive their first doses of Deltonin dissolved in a vehicle solution of DMSO (. Briefly, Deltonin is given via oral administration to tumor-bearing mice at 10, 20 and 40 mg/kg every day for 3 weeks (between day 8 and 28). In parallel, the control group receives the vehicle (DMSO, 2, where “a” is the long diameter and “b” is the short diameter. The mice are sacrificed when they become moribund, and the sacrifice date is recorded to calculate the survival time. To detect the apoptosis protein expression and microvessel density, tumor tissues are removed, fixed in 10% formalin or not and snap-frozen in liquid nitrogen immediately[1]. |
数据来源文献 |
[1]. Tong QY, et al. Deltonin, a steroidal saponin, inhibits colon cancer cell growth in vitro and tumor growth in vivo via induction of apoptosis and antiangiogenesis. Cell Physiol Biochem. 2011;27(3-4):233-42. [2]. Zhang S, et al. Deltonin induces apoptosis in MDA?MB?231 human breast cancer cells via reactive oxygen species?mediated mitochondrial dysfunction and ERK/AKT signaling pathways. Mol Med Rep. 2013 Mar;7(3):1038-44. |
规格 |
1mg 5mg 10mg |
单位 |
瓶 |