Aspirin (Acetylsalicylic Acid) lithium 是一种口服有效的不可逆的环氧合酶COX-1和COX-2抑制剂，IC50分别为 5 和 210 μg/mL. Aspirin lithium 诱导细胞凋亡 (apoptosis)。Aspirin lithium 可抑制NF-κB的活化。Aspirin lithium 还抑制血小板前列腺素合成酶 (prostaglandin synthetase)，可预防冠状动脉和脑血管血栓形成。
| 生物活性 | Aspirin (Acetylsalicylic Acid) lithium is an orally active, potent and irreversible inhibitor of cyclooxygenaseCOX-1andCOX-2, withIC50values of 5 and 210 μg/mL, respectively. Aspirin lithium inducesapoptosis. Aspirin lithium inhibits the activation ofNF-κB. Aspirin lithium also inhibits plateletprostaglandin synthetase, and can prevent coronary artery and cerebrovascular thrombosis[1][2][3][4][5][6]. |
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体外研究
(In Vitro) | Aspirin lithium inhibits COX-1 and COX-2 in human articular chondrocytes, with IC50values of 3.57 μM and 29.3 μM, respectively[2].
Aspirin lithium acetylates serine-530 of COX-1, thereby blocking thromboxane A synthesis in platelets and reducing platelet aggregation[3].
Aspirin lithium inhibits COX-2 protein expression through interference with binding of CCAAT/enhancer binding protein beta (C/EBPbeta) to its cognate site on COX-2 promoter/enhancer[3].
Aspirin lithium inhibits NF-κB-dependent transcription from the lgκ enhancer and the human immunodeficiency virus (HIV) long terminal repeat (LTR) in transfected T cells[4].
Aspirin lithium induces apoptosis by the activation of caspases, the activation of p38 MAP kinase, release of mitochondrial cytochrome c, and activation of the ceramide pathway[6].
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体内研究
(In Vivo) | Aspirin lithium (5-150 mg/kg, PO, once) shows significant antipyretic activity in adult yeast-fevered male rats[7].
| Animal Model: | Male albino Charles River rats (200-250 g, 8 animals/group, fever was induced by 20 ml/kg of a 20 % aqueous suspension of brewer’s yeast which was injected SC in the back below the nape of the neck)[7] | | Dosage: | 5, 25, 50, 100 and 150 mg/kg | | Administration: | PO, once | | Result: | Produced a statistically significant decrease of 0.23 ℃ at 15 min post-drug at the dose of 150 mg/kg. Antipyretic effect gradually increased in magnitude until a peak effect of 1.96 ℃ was reached at 120 min post-drug. The ED50 of aspirin was found to be 10.3 mg/kg with confidence limits of 1.8-23.0 mg/kg. The antipyretic response to aspirin is dependent on the dose of the compound administered. |
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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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