Herbal Drug Technology Laboratory, Pharmacy Department, Faculty of Engineering and Technology, Vadodara, Gujarat, India.
Phytother Res. 2012 Sep;26(9):1342-7. doi: 10.1002/ptr.3721. Epub 2012 Feb 1.
The inhibitory activity of Tinospora cordifolia stem-derived alkaloids was evaluated against lens aldose reductase (AR) isolated from male Wistar rats. Anticataract potential of the alkaloids of T. cordifolia was evaluated in vitro in rat lenses, considering the activity of normal rat lenses as 100%. The biologically active constituents of T. cordifolia extract were characterized as the isoquinoline alkaloids, jatrorrhizine, palmatine and magnoflorine, by spectral analysis. The inhibitory effects varied with all chemicals and concentrations used. The inhibitory concentration (IC₅₀) values of jatrorrhizine, palmatine and magnoflorine are 3.23, 3.45 and 1.25 µg/mL respectively. The concentration of maximum activity was selected for its effect on galactose-induced polyol accumulation in vitro. The percentage inhibition of galactose-induced polyol accumulation was 62.6, 58.8 and 27.7% in the presence of jatrorrhizine, palmatine and magnoflorine, respectively. Magnoflorine may be useful as lead compounds and new agents for AR inhibition.
我们评估了三叶鬼针草茎部来源的生物碱对从雄性 Wistar 大鼠中分离出的晶状体醛糖还原酶（AR）的抑制活性。考虑到正常大鼠晶状体的活性为 100%，我们在体外评估了三叶鬼针草生物碱的抗白内障潜力。三叶鬼针草提取物的生物活性成分通过光谱分析被鉴定为异喹啉生物碱，即小檗碱、巴马汀和粉防己碱。所有化学物质和使用浓度的抑制效果均有所不同。小檗碱、巴马汀和粉防己碱的抑制浓度（IC₅₀）值分别为 3.23、3.45 和 1.25 µg/mL。选择最大活性浓度来研究其对 galactose 诱导的多元醇积累的影响。在小檗碱、巴马汀和粉防己碱存在的情况下，galactose 诱导的多元醇积累的抑制率分别为 62.6%、58.8%和 27.7%。粉防己碱可能是作为 AR 抑制的先导化合物和新药。
