Department of Pharmacy, Tongji Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, PR China.
Pharm Biol. 2013 Mar;51(3):376-82. doi: 10.3109/13880209.2012.732581.
A new caffeic acid derivative, named (7'Z)-3-O-(3, 4-dihydroxyphenylethenyl)-caffeic acid (CADP), extracted from Abacopteris penangiana (Hook.) Ching.
To elucidate the neuroprotective effect of CADP against H₂O₂-induced cytotoxicity in PC12 cells and D-galactose (D-gal)-induced neurotoxicity in mice brain.
CADP was isolated from the methanol extract of the rhizomes of A. penangiana. In vitro, the protective effect of CADP (0.1-10 μM) against H₂O₂-induced oxidative damage on PC12 cells was investigated by a MTT assay. In vivo, behavioral tests and antioxidant enzymes measurements were performed to investigate the protective effect of intraperitoneal (i.p.) injection of CADP (5 or 10 mg/kg/day) for 2 weeks on D-gal-induced neurotoxicity in mice.
The results showed that CADP significantly attenuated cell toxicity in a dose-dependent manner, and the EC₅₀ value of CADP was 0.83 ± 0.02 μM. In vivo, it was found that CADP significantly improved the behavioral performance of D-gal-treated mice in both Morris water maze (MWM) test and step-down avoidance test. As compared with model group, CADP (5, 10 mg/kg/day) attenuated the decrease in superoxide dismutase (SOD) activities by 40.5 and 75.4%, respectively; attenuated the decrease in glutathione peroxidase (GPx) activities by 53.8 and 73.2%, respectively; attenuated the decrease in catalase activities by 12.0 and 53.3%, respectively; reduced the increased levels of malondialdehyde (MDA) by 38.6 and 79.9%, respectively.
The results suggested that CADP has significant neuroprotective effects which can be attributed to inhibiting the generation of free radical and enhancing the activity of endogenous antioxidant enzymes.
从观音座莲(Hook.)Ching 中提取到一种新的咖啡酸衍生物,命名为(7'Z)-3-O-(3,4-二羟基苯乙烯基)咖啡酸(CADP)。
阐明 CADP 对 H₂O₂诱导的 PC12 细胞毒性和 D-半乳糖(D-gal)诱导的小鼠脑毒性的神经保护作用。
CADP 从观音座莲根茎的甲醇提取物中分离得到。在体外,通过 MTT 测定法研究 CADP(0.1-10 μM)对 H₂O₂诱导的 PC12 细胞氧化损伤的保护作用。在体内,通过行为测试和抗氧化酶测量来研究腹腔注射 CADP(5 或 10 mg/kg/天)2 周对 D-gal 诱导的小鼠神经毒性的保护作用。
结果表明,CADP 呈剂量依赖性显著减轻细胞毒性,CADP 的 EC₅₀ 值为 0.83±0.02 μM。在体内,发现 CADP 显著改善了 D-gal 处理的小鼠在 Morris 水迷宫(MWM)测试和跳下回避测试中的行为表现。与模型组相比,CADP(5、10 mg/kg/天)分别使超氧化物歧化酶(SOD)活性降低 40.5%和 75.4%;使谷胱甘肽过氧化物酶(GPx)活性降低 53.8%和 73.2%;使过氧化氢酶活性降低 12.0%和 53.3%;使丙二醛(MDA)水平升高降低 38.6%和 79.9%。
结果表明,CADP 具有显著的神经保护作用,这归因于抑制自由基的生成和增强内源性抗氧化酶的活性。