Isochamaejasmin 是一种双黄酮类化合物，具有抗癌、抗疟原虫和杀虫活性。Isochamaejasmin 显示出有效的NF-κB(NF-κB) 激活活性。Isochamaejasmin 可通过线粒体途径引起 AW1 细胞 DNA 损伤并诱导细胞凋亡 (apoptosis)。Isochamaejasmin 还具有中等抗疟原虫活性 (对恶性疟原虫的IC50为 7.3 μM) 和相对较低的细胞毒性 (CC50为 29.0 μM)。
| 生物活性 | Isochamaejasmin is a biflavonoid with anti-cancer, antiplasmodial and insecticidal activities. Isochamaejasmin displays a potentNF-κB(NF-κB) activation activity. Isochamaejasmin could cause DNA damage and induceapoptosisvia the mitochondrial pathway in AW1 cells[1][2]. Isochamaejasmin also has a moderate antiplasmodial activity (IC50of 7.3 μM forP. falciparum) and relatively low cytotoxicity (CC50of 29.0 μM)[3]. |
体外研究
(In Vitro) | Isochamaejasmin (6.25-100μM; 24-72 h) 通过时间和剂量依赖性方式显示出对 AW1 细胞的潜在毒性。Isochamaejasmin (1000 mg/L, 500 mg/L, 250 mg/L, 125 mg/L, 62.5 mg/L; 24 h, 48 h, 72 h, and 96 h) 对H. zea幼虫具有随时间的潜在毒性和剂量依赖性行为[1]。
Isochamaejasmin (40-80μM; 24 h) 导致 DNA 损伤并增加 AW1 细胞中 γH2AX 和 OGG1 的水平。使细胞周期停滞在G2/M期[1]。
Isochamaejasmin (20-80μM; 24 h) 剂量依赖性诱导 AW1 细胞凋亡[1]。
Isochamaejasmin (20-80μM; 24 h) 显示 MMP 下降，Bax/Bcl-2 表达上调，导致细胞色素 c 释放到胞质溶胶中，caspase-3/9 激活，PARP 裂解[1]。
Isochamaejasmin 显示 AW1 细胞中活性氧 (ROS) 水平的剂量依赖性升高、脂质过氧化产物的积累和抗氧化酶的失活[1]。
Isochamaejasmin 在转染的 HeLa 细胞中诱导 NF-κB 定向报告基因的表达，EC50为 3.23 μM。Isochamaejasmin 刺激的 NF-κB 报告基因活性伴随着 NF-κB 蛋白的核转位，并被 IκBα 的显性失活结构阻断。Isochamaejasmin 还诱导丝裂原活化蛋白激酶 ERK1/2 和 p38 以及 PKCδ的时间依赖性磷酸化[2]。
Cell Viability Assay[1] | Cell Line: | Larvae and neuronal cells (AW1) | | Concentration: | 6.25 μM, 12.5 μM, 25 μM, 50 μM and 100 μM | | Incubation Time: | 24 h, 48 h and 72 h | | Result: | Had potential toxicity against H. zea both in vivo and in vitro via time- and dose-dependent manners. |
Cell Cycle Analysis[1] | Cell Line: | Neuronal cells (AW1) | | Concentration: | 40 μM and 80 μM | | Incubation Time: | 24 h | | Result: | The cell cycle was arrested at the G2/M phase. |
Apoptosis Analysis[1] | Cell Line: | Neuronal cells (AW1) | | Concentration: | 20 μM, 40 μM, and 80 μM | | Incubation Time: | 24 h | | Result: | Induced apoptosis via the mitochondrial pathway in AW1 cells. |
Western Blot Analysis[1] | Cell Line: | Neuronal cells (AW1) | | Concentration: | 20 μM, 40 μM, and 80 μM | | Incubation Time: | 24 h | | Result: | Showed upregulation of Bax/Bcl-2 expression resulting in the release of cytochrome c into the cytosol, activation of caspase-3/9, and cleavage of PARP. |
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| 结构分类 | - Flavonoids
- Other Flavonoids
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| 来源 | - Plants
- Thymelaeaceae
- Stellera chamaejasmeLinn.
- Plants
- Urticaceae
- Stellera chamaejasmeLinn.
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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