3'-Hydroxypterostilbene 是 Pterostilbene (HY-N0828) 的类似物。3'-Hydroxypterostilbene 抑制 COLO 205，HCT-116 和 HT-29 细胞的生长，IC50分别值为 9.0，40.2 和 70.9 μM。3'-Hydroxypterostilbene 显著下调PI3K/Akt和MAPKs信号通路并通过诱导细胞凋亡和自噬抑制人结肠癌细胞生长。3'-Hydroxypterostilbene 可用于癌症的研究。
| 生物活性 | 3'-Hydroxypterostilbene is aPterostilbene(HY-N0828) analogue. 3'-Hydroxypterostilbene inhibits the growth of COLO 205, HCT-116 and HT-29 cells withIC50s of 9.0, 40.2 and 70.9 μM, respectively. 3'-Hydroxypterostilbene significantly down-regulatesPI3K/AktandMAPKssignaling pathways and effectively inhibits the growth of human coloncancercells by inducingapoptosisandautophagy. 3'-Hydroxypterostilbene can be used for the research ofcancer[1]. |
| IC50& Target | IC50: 9.0 μM (COLO 205),40.2 μM (HCT-116), 70.9 μM (HT-29)[1] |
体外研究
(In Vitro) | 3'-Hydroxypterostilbene (5-50 μM; 24 h) affects cell proliferation of COLO 205, HCT-116 and HT-29[1].3'-Hydroxypterostilbene (5-100 μM; 24 h) induces cell apoptosis and the concentration of ROS plays an important role as an early mediator in 3'-Hydroxypterostilbene-induces apoptosis[1].3'-Hydroxypterostilbene (5-50 μM; 24 h) induces caspase-9 cleavage, increases caspase-3 activity and inhibits the mTOR/p70S6K, PI3K/Akt and MAPKs signaling pathways in COLO 205 cells[1].3'-Hydroxypterostilbene (25-50 μM; 24 h) induces autophagy in COLO 205 cells[1].
Cell Proliferation Assay[1] | Cell Line: | COLO 205, HCT-116 and HT-29 cell lines | | Concentration: | 5, 10, 25 and 50 μM | | Incubation Time: | 24 hours | | Result: | Inhibited cell proliferation of COLO 205, HCT-116 and HT-29 cells with IC50s of 9.0, 40.2 and 70.9 μM, respectively. |
Apoptosis Analysis[1] | Cell Line: | COLO 205 cells | | Concentration: | 5-100 μM | | Incubation Time: | 24 hours | | Result: | Induced apoptosis in human colorectal carcinoma cells. |
Western Blot Analysis[1] | Cell Line: | COLO 205 cells | | Concentration: | 5-50 μM | | Incubation Time: | 24 hours | | Result: | Degraded 116 kDa PARP into 85 kDa fragments and induced DFF-45 protein degradation and increased the amounts of LC3B I/II proteins than pterostilbene. Markedly decreased phosphorylation of mTOR, p70S6K (Thr389), PI3K, Akt and p38 MAPK in cells. |
Cell Autophagy Assay[1] | Cell Line: | COLO 205 cells | | Concentration: | 25 and 50 μM | | Incubation Time: | 24 hours | | Result: | Showed an inducing effect on autophagy than pterostilbene in COLO 205 cells. |
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体内研究
(In Vivo) | 3'-Hydroxypterostilbene (10 mg/kg; i.p. once per day for 15 days) strongly inhibits tumor growth in vivo[1].
| Animal Model: | 3-4 week old BALB/c nude mice with human colorectal carcinoma COLO 205 tumor xenografts[1] | | Dosage: | 10 mg/kg | | Administration: | Intraperitoneal injection; 10 mg/kg once per day for 15 days | | Result: | Significantly inhibited tumor volume and tumor weight after 15 days treatment compared with the pterostilbene-treated mice, and decreased the protein levels of COX-2, MMP-9, VEGF, cyclin D1 and pro-caspase-3 in mice. |
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| 来源 | - Plants
- Leguminosae
- Sphaerophysa salsula
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| 溶解性数据 | In Vitro: DMSO : 125 mg/mL(459.05 mM;Need ultrasonic) 配制储备液 | 1 mM | 3.6724 mL | 18.3621 mL | 36.7242 mL | | 5 mM | 0.7345 mL | 3.6724 mL | 7.3448 mL | | 10 mM | 0.3672 mL | 1.8362 mL | 3.6724 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (7.64 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (7.64 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (7.64 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (7.64 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (7.64 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (7.64 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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