Dihydroartemisinin-d₅  (Synonyms: 双氢青蒿素-d₅; Dihydroqinghaosu-d5; β-Dihydroartemisinin-d5; Artenimol-d5)

Dihydroartemisinin-d₅ is deuterated labeled Dihydroartemisinin (HY-N0176). Dihydroartemisinin is a potent anti-malaria agent.

氢、碳和其他元素的稳定重同位素已被纳入药物分子中，主要作为药物开发过程中定量的示踪剂。氘化引起了人们的关注，因为它可能影响药物的药代动力学和代谢谱^[1]。
Dihydroartemisinin (DHA) 是一种抗疟药。Dihydroartemisinin 处理有效上调胞质 RelA/p65 蛋白水平并下调核 RelA/p65 蛋白水平，它阻断 RelA/p65 从胞质溶胶的核转运，而不是抑制 RelA/p65 蛋白合成。Dihydroartemisinin 在 RPMI 8226 细胞中诱导自噬。Dihydroartemisinin 抑制 RPMI 8226 细胞中的 NF-κB 活化。通过 EMSA 测定检查 NF-κB Dihydroartemisinin 结合活性^[3]。
RPMI 8226 细胞暴露于不同浓度的 Dihydroartemisinin (10、20 和 40 μM) 12 小时，引入 TNF-α 作为 NF-κB 激活的阳性对照。与 TNF-α^[2]相比，Dihydroartemisinin 以剂量依赖性方式抑制 NF-κB 活化。Dihydroartemisinin (DHA) 可增强光动力疗法 (PDT) 对食管癌细胞的抗肿瘤作用，用 Dihydroartemisinin (80 μM)、PDT (分别为 25 和 20 J/cm²) 或其组合处理 Eca109 和 Ec9706 细胞。Dihydroartemisinin 或 PDT 单次处理分别导致 Eca109 细胞活力降低 37±5% 或 34±6%，Ec9706 细胞活力降低 33±7% 或 34±6%。当 PDT 与 Dihydroartemisinin 联合使用时，细胞系的细胞活力分别降低了 59±6% 或 61±7%^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Dihydroartemisinin (单次口服；200、300、400 或 600 mg/kg)，在感染后第 6-8 天每天给药一次，可将总蠕虫负担减少 69.2%-90.6%，将雌性蠕虫负担减少 62.2% %-92.2%，取决于第一个实验中的剂量。在感染后第 34-36 天进行的类似处理可将总蠕虫负荷降低 73.9%-85.5%，将雌性蠕虫负荷降低 83.8%-95.3%^[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

289.38

C₁₅H₁₉D₅O₅

71939-50-9

双氢青蒿素-d₅；二氢青蒿素-d₅

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.  [Content Brief]

  [2]. Hu W, et al. Dihydroartemisinin induces autophagy by suppressing NF-κB activation. Cancer Lett. 2014 Feb 28;343(2):239-48.  [Content Brief]

  [3]. Li HJ, et al. Dihydroartemisinin-praziquantel combinations and multiple doses of dihydroartemisinin in the treatment of Schistosoma japonicum in experimentally infected mice. Ann Trop Med Parasitol. 2011 Jun;105(4):329-33.  [Content Brief]

  [4]. Li YJ, et al. Dihydroartemisinin accentuates the anti-tumor effects of photodynamic therapy via inactivation of NF-κB in Eca109 and Ec9706 esophageal cancer cells. Cell Physiol Biochem. 2014;33(5):1527-36.  [Content Brief]