Aspirin

Aspirin (Acetylsalicylic Acid) 是一种 COX 抑制剂，抑制 COX1 和 COX2 (IC50=5 210 μg mL)，具有选择性、不可逆性和口服活性。Aspirin 也是一种组蛋白去乙酰化酶抑制剂，可上调细胞周期阻滞蛋白 p21。Aspirin 具有抗炎、解热镇痛、抗血小板聚集能多种活性。

Aspirin DL-lysine is a non-steroidal anti-inflammatory drug. It also may inhibit cancer growth. Aspirin DL-lysine is a water-soluble, injectable aspirin derivative.

Se-Aspirin (Se-NSAID-8) 具有抗癌活性和胃保护作用，抑制促炎和促生存NF-ĸB通路的激活，抑制NF-ĸB下游抗凋亡靶标（如Bcl-xL、Mcl-1和存活素）的表达。Se-Aspirin 诱导细胞周期停滞和细胞凋亡的激活，可加速溃疡愈合，可用于研究胰腺癌和结直肠癌。

Aspirin calcium is the prototypical analgesic used in the treatment of mild to moderate pain. It has anti-inflammatory and antipyretic properties and acts as an inhibitor of cyclooxygenase which results in the inhibition of the biosynthesis of prostaglandins. Aspirin also inhibits platelet aggregation and is used in the prevention of arterial and venous thrombosis. (From Martindale, The Extra Pharmacopoeia, 30th ed, p5)

Resolvins are a family of potent lipid mediators derived from both eicosapentaenoic acid and docosahexaenoic acid.[1] In addition to being anti-inflammatory, resolvins promote the resolution of the inflammatory response back to a non-inflamed state.[2] Resolvin D1 is produced physiologically from the sequential oxygenation of DHA by 15- and 5-lipoxygenase.[1] 17(R)-RvD1 is an aspirin-triggered epimer of RvD1 that reduces human polymorphonuclear leukocyte (PMN) transendothelial migration, the earliest event in acute inflammation, with equipotency to RvD1 (EC50 = ~30 nM).[3] 17(R)-RvD1 exhibits a dose-dependent reduction in leukocyte infiltration in a mouse model of peritonitis with maximal inhibition of ~35% at a 100 ng dose.[3] In contrast to RvD1, the aspirin-triggered form resists rapid inactivation by eicosanoid oxidoreductases. Analytical and biological comparisons of synthetic 17(R)-RvD1 with endogenously derived 17(R)-RvD1 have confirmed its identity as matching the natural product.[4]

17(R)-Resolvin D1 (17(R)-RvD1) is an aspirin-triggered epimer of RvD1 that equivalently inhibits human polymorphonuclear leukocyte migration across the endothelium (EC50= ~30 nM), a precursor to acute inflammation. Unlike RvD1, it resists rapid degradation by eicosanoid oxidoreductases. In a mouse peritonitis model, 17(R)-RvD1 dose-dependently reduces leukocyte infiltration, achieving up to a 35% decrease with a 100 ng dose. Additionally, its methyl ester derivative, designed to enhance its pharmacokinetic and distribution properties as a more lipophilic prodrug, can be converted back into the active acid form by intracellular esterases.

17(R)-Resolvin D3 (17(R)-RvD3) is an aspirin-triggered epimer of resolvin D3, produced from docosahexaenoic acid (DHA) through the action of COX-2 in the presence of aspirin, via a 17(R)-hydroperoxy DHA (17(R)-HDHA) intermediary. Identified in mouse inflammatory exudates, 17(R)-RvD3 notably inhibits the transmigration of isolated human polymorphonuclear cells (PMNs) and fosters the efferocytosis of apoptotic PMNs by macrophages. Furthermore, in a mouse model of zymosan-induced peritonitis, 17(R)-RvD3 administration (10 ng animal) significantly curtails neutrophil infiltration into the peritoneal cavity and modulates cytokine levels by reducing IL-6 and increasing IL-10 in the inflammatory exudate. It engages GPR32, evidenced by activation in a β-arrestin reporter assay and augments phagocytosis more effectively in CHO cells overexpressing GPR32 compared to controls. Additionally, 17(R)-RvD3 enhances the clearance of etoposide-induced tumor cell debris by monocyte-derived macrophages in H460 human lung carcinoma.

Nitroaspirin (NCX 4016) 是一氧化氮供体和阿司匹林的硝基衍生物，与 Aspirin 结合可抑制环氧合酶=，可作为 COX-1 的直接和不可逆抑制剂。 它通过下调 EGFR PI3K STAT3 信号传导和调节 Bcl-2 家族蛋白，显着诱导顺铂耐药人卵巢癌细胞的细胞周期停滞和凋亡，具有抗血栓和抗血小板特性。

Aspirin Aluminum is an intermolecular compound that can inhibit gastrointestinal mucosal disorders induced by NSAIDs.

ZINC40099027 是特异性黏着斑激酶 （FAK） 激活剂，通过激活黏着斑激酶促进持续性阿司匹林相关胃损伤的胃粘膜修复，通过加速FAK激酶结构域的酶活性来激活人黏着斑激酶，激活细胞 FAK 并促进肠上皮伤口闭合。

6'-GNTI dihydrochloride 是一种κ-阿片受体（KOR）激动剂，它偏向于激活 G 蛋白介导的信号传导，而不是β-阿司匹林2的募集。6'-GNTI dihydrochloride 只能激活纹状体神经元中的 Akt 通路。

Salicylamide(2-Hydroxybenzamide) 是一种止痛剂和抗热解药剂，是一种微粒体 UDP-葡糖醛酸基转移酶抑制剂。

Triflusal (UR1501) 能够利用乙酰化COX-1途径，不可逆地减少血小板中血栓素B2的生成。

Pyrocatechuic acid (Catecholcarboxylic acid) 是一种存在于血浆中的苯甲酸代谢物，当摄入阿司匹林后，它的含量会提高。

2-Hydroxy-6-methoxybenzoic acid (6-Methoxysalicylic acid) 可用于动物血浆中乙酸水杨酸及其主要代谢物水杨酸含量的测定，表现出较好的抗缓解疼痛活性。

ABzOH 是一种苯甲酸衍生物，结构类似于阿司匹林等非甾体抗炎药，具有抗炎、抗肿瘤和抗增殖作用。ABzOH 不仅可以抑制肿瘤坏死因子- α (TNF-a)、白细胞介素-1β (IL-1β)和白细胞介素-6 (IL-6)等促炎细胞因子的表达还对乳腺癌、肺癌和胰腺癌具有抑制作用。

Vicagrel 是一种有效的、具有口服活性抗血小板化合物，通过不可逆地抑制 P2Y12 受体，降低代谢失活，增强了阿司匹林对啮齿类动物血小板聚集和血栓形成起抑制作用。Viagrel 可用于治疗冠状动脉疾病、外周血管疾病和脑血管疾病中血栓。

ISOGINKGETIN (4',4'''-Dimethylamentoflavone) 是一种MMP9抑制剂，也是一种Pre-mRNA Splicing 抑制剂。

Fendosal (HP-129) 是一种非甾体抗炎药。在预防性和治疗性辅助诱导的慢性炎症多关节炎模型中，它的活性是阿司匹林的 6.9 至 9.5 倍。

Tri-Salicylic acid 是一种和水杨酸具有相似性质的化合物。它对肥胖、炎症及心血管疾病具有潜在的研究价值。

Gaultherin 是一种分离自 Gaultheria yunnanensis 中的天然水杨酸酯衍生物。它是一种非甾体类抗炎药，具有止痛和抗炎作用，与 Aspirin 相比没有胃溃疡作用。

GTCpFE 由Dimethyl fumarate(DMF) 和 Aspirin(ASA) 组成，它能优效抑制 NF-κB 通路中的 IKKα β 和阻断 p65 进入细胞核，展现出显著的抗炎效果。此外，GTCpFE 对乳腺癌干细胞表现出显著抑制作用，通过减少乳腺球体的生长和 CD44+CD24- 免疫表型的调控，表现出针对癌症干细胞 (CSC) 的选择性活性，这对于治疗侵袭性癌症具有重要意义，尤其是在 NFκB 和 PGE2 依赖的表型中。

KF 392 is antiulcer. It was found that KF-392 given orally to rats at 1.0 to 5.0 mg kg had a marked suppression on the developments of Shay ulcer as well as the aspirin-, stress-, and reserpine-induced gastric lesions.

Nocloprost (SH 475) 是一种前列腺素 E2 (PGE2) 类似物，是一种 EP1 和 EP3 受体激动剂，具有局部胃保护和溃疡愈合活性，可减少阿司匹林诱导的人类胃肠道病变，诱导人血小板激活，可用于研究心血管疾病。