Departamento de Farmacia, División de Ciencias Naturales y Exactas, Universidad de Guanajuato, Campus Guanajuato, Guanajuato, Gto. CP 36050, Mexico.
CONACyT-Instituto de Investigaciones Biomédicas, Departamento de Inmunología, Universidad Nacional Autónoma de México, CDMX. CP 04510, Mexico.
Molecules. 2019 Jul 21;24(14):2643. doi: 10.3390/molecules24142643.
The present study aims to evaluate the antiarthritic activity of diacetylcurcumin (DAC), a synthetic derivative where the free phenolic groups of curcumin are derivatized by acetylation, thereby conferring greater lipophilicity to the parent molecule and partially overcoming the limited systemic bioavailability of curcumin. Antiarthritic activity was evaluated on a Freund's complete adjuvant (FCA)-induced murine model of arthritis. Oral administration of DAC (60 and 120 mg/kg) resulted in a significant inhibition of inflammation in the acute and chronic phases, respectively, demonstrating an improved and sustained anti-inflammatory effect, comparable to that of curcumin (150 mg/kg) in the chronic stage at a lower dose. Phenylbutazone (80 mg/kg) was used as a reference drug. The pharmacological consequence of DAC or curcumin treatment is the prevention of secondary lesions commonly associated with this biological model.
本研究旨在评估二乙酰基姜黄素（DAC）的抗关节炎活性，这是一种合成衍生物，其中姜黄素的游离酚基团通过乙酰化衍生化，从而使母体分子具有更大的亲脂性，并部分克服了姜黄素有限的全身生物利用度。在弗氏完全佐剂（FCA）诱导的关节炎小鼠模型上评估了抗关节炎活性。DAC（60 和 120mg/kg）的口服给药分别在急性和慢性阶段显著抑制炎症，表现出改善和持续的抗炎作用，在慢性阶段以较低剂量与姜黄素（150mg/kg）相当。苯丁唑酮（80mg/kg）用作参考药物。DAC 或姜黄素治疗的药理后果是预防与这种生物模型相关的常见继发性病变。
