Université Lille Nord de France, Faculté de Pharmacie, Laboratoire de Chimie Thérapeutique (EA 4481) 3, Département de Pharmacologie Médicale, rue du Professeur Laguesse, BP 83, 59006 Lille, France.
Eur J Med Chem. 2011 Jun;46(6):2575-85. doi: 10.1016/j.ejmech.2011.03.048. Epub 2011 Mar 30.
A series of β-carboline compounds were synthesized, starting from compound GWC22, their antioxidant activity was determined by inhibition of lipid peroxidation. The oxidation of LDL was induced in the presence of CuSO4 or 2,2'-azobis(2-amidinopropane) dihydrochloride (AAPH). The protective actions of these compounds against the cytotoxicity were evaluated with lactate dehydrogenase (LDH) activity in bovine aortic endothelial cells (BAECs) and cellular vitality by measuring mitochondrial activity in the presence of MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide). Most of compounds showed an higher antioxidant activity than GWC22 derivative (R=1.6 for 5 μM CuSO4). The best antioxidant activities are phenolic and benzyloxy derivatives with ratio R=1.9 to 2.8 for 1 μM CuSO4. These substances have protective actions and increase significantly the cell viability.
合成了一系列β-咔啉类化合物，以化合物 GWC22 为起始原料，通过抑制脂质过氧化反应来测定其抗氧化活性。在 CuSO4 或 2,2'-偶氮双（2-脒基丙烷）二盐酸盐（AAPH）的存在下诱导 LDL 氧化。通过测定在 MTT（3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四氮唑溴盐）存在下牛主动脉内皮细胞（BAEC）中乳酸脱氢酶（LDH）活性和细胞活力，评估这些化合物对细胞毒性的保护作用。大多数化合物显示出比 GWC22 衍生物更高的抗氧化活性（R=1.6 对于 5 μM CuSO4）。具有酚和苄氧基取代基的化合物具有最佳的抗氧化活性，对于 1 μM CuSO4，R 比值为 1.9 至 2.8。这些物质具有保护作用，可显著提高细胞活力。
