Laboratory of Pharmacognosy and Pharmaceutical Analysis, Department of Pharmaceutical Sciences, Faculty of Pharmaceutical, Biomedical and Veterinary Sciences, University of Antwerp, Universiteitsplein 1, 2610 Antwerp, Belgium.
J Ethnopharmacol. 2010 Jan 8;127(1):112-7. doi: 10.1016/j.jep.2009.09.039. Epub 2009 Sep 30.
Oxidative stress has been associated with many pathological disorders such as atherosclerosis, diabetes and cancer. Supplementation with exogenous antioxidants, including phenolic compounds from plant sources, may help to restore the pro-oxidative/antioxidative balance. To take into account effects of absorption, metabolisation, plasma protein binding, distribution, and elimination, antioxidative research should not be limited to in vitro assays but be extended to in vivo models.
In the present work a quantified 50% EtOH root extract of Pueraria lobata (Willd.) Ohwi (Fabaceae) was selected to determine its in vivo antioxidative activity in a diabetic rat model, where diabetes and the accompanying oxidative stress were induced by intraperitoneal administration of streptozotocin. This root extract was found to contain 10.42+/-0.15% puerarin as the main constituent and smaller amounts of the related isoflavonoids 3'-hydroxypuerarin, 3'-methoxypuerarin, 6''-xylosylpuerarin, daidzin, genistin, daidzein and genistein, as determined by a validated HPLC method. This extract was administered orally at a daily dose of 500 mg/kg root extract, corresponding to 50mg/kg puerarin, during 3 weeks. In addition the effect on the plasma concentration of some fat-soluble antioxidants (co-enzyme Q(9), alpha- and gamma-tocopherol) was evaluated.
The level of malondialdehyde (MDA) in plasma, used as a marker of oxidative damage to lipids, was reduced to the same level as in healthy control animals, and as in the positive control group treated daily with 50mg/kg alpha-tocopherol acetate. No obvious signs of toxicity were observed by administration of 10x the treatment dose.
氧化应激与许多病理紊乱有关，如动脉粥样硬化、糖尿病和癌症。补充外源性抗氧化剂，包括植物来源的酚类化合物，可能有助于恢复促氧化/抗氧化平衡。为了考虑吸收、代谢、血浆蛋白结合、分布和消除的影响，抗氧化研究不应仅限于体外测定，而应扩展到体内模型。
本工作中选择了定量的 50%乙醇葛根提取物（Willd.）Ohwi（豆科），以确定其在糖尿病大鼠模型中的体内抗氧化活性，其中糖尿病和伴随的氧化应激是通过腹腔内给予链脲佐菌素诱导的。该根提取物被发现含有 10.42+/-0.15%葛根素作为主要成分，以及较小量的相关异黄酮 3'-羟基葛根素、3'-甲氧基葛根素、6''-木糖基葛根素、大豆苷、染料木苷、大豆苷元和染料木黄酮，如通过验证的 HPLC 方法确定。该提取物以 500mg/kg 根提取物的日剂量口服给予，相当于 50mg/kg 葛根素，持续 3 周。此外，还评估了对一些脂溶性抗氧化剂（辅酶 Q(9)、α-和γ-生育酚）的血浆浓度的影响。
血浆中丙二醛（MDA）的水平，作为脂质氧化损伤的标志物，降低到与健康对照动物相同的水平，并且与每天用 50mg/kg α-生育酚乙酸酯治疗的阳性对照组相同。给予 10 倍治疗剂量时，未观察到明显的毒性迹象。
