PaedeROSidic acid 是从鸡矢藤分离出的一种天然产物,通过诱导线粒体介导的凋亡抑制肺癌细胞,具有显着的抗肿瘤、抗惊厥和镇静作用。
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Paederosidic acid has significant anti-tumor, anticonvulsant and sedative effects. Paederosidic acid increases brain gamma-aminobutyric acid and decreases glutamic acid in the brain, and it up-regulates expressions of GAD 65, may be a promising future therapeutic agent for treatment of epilepsy.
体外活性
Paederosidic acid(PA) showed significant anti-tumor activity on lung cancer in vitro; the mechanisms were involved in inducing mitochondria-mediated apoptosis via up-regulation of caspase-3, caspase-8, caspase-9, Bid, Bax, down-regulation of Bcl-2 and stimulating the release of Cyto-C from mitochondria.JNK phosphorylation levels significantly increased concomitantly with decrease in Akt phosphorylation after treatment with PA in A549 cells. However, JNK siRNA-transfected cells diminished PA-induced caspase-3, 8 and 9, Bid and Bax activaton while enhanced the Bcl-2 activation. PA-induced JNK activation played an important functional role in apoptosis[1].
体内活性
Anticonvulsant and sedative effects of paederosidic acid isolated from Paederia scandens (Lour.) Merrill. in mice and rats.Paederosidic acid (5, 10, 20, and 40 mg/kg, ip) had significant anticonvulsant and sedative effects. paederosidic acid increased brain gamma-aminobutyric acid and decreased glutamic acid in the brain, and it up-regulated expressions of GAD 65. Paederosidic acid may be a promising future therapeutic agent for treatment of epilepsy[2].
细胞实验
The anti-proliferative effects of PA on A549 cells were evaluated by MTT method and the IC50 values were calculated. Furthermore, the PA-induced apoptosis in A549 cells was determined by fluorescence microscope via staining with DAPI and by flow cytometer via staining with FITC conjugated Annexin V/PI. The expression of apoptosis-related or signaling proteins was investigated by Western blotting[1]
动物实验
Anticonvulsant activities of paederosidic acid were evaluated by maximal electroshock and pentylenetetrazole-induced seizures in male mice. Then, pentobarbital sodium-induced sleeping time and locomotor activity tests in mice were used to evaluate the sedative effects of paederosidic acid. Finally, the mechanism of paederosidic acid was explored by evaluating the contents of Glu and GABA in the brain, and Western blot was used to measure GAD65 expression in the mouse brain[2].
Cas No.
18842-98-3
分子式
C18H24O12S
分子量
464.44
别名
鸡屎藤苷酸;异戊二酸 紫草酸
储存和溶解度
DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years