Dhananjaya Bhadrapura Lakkappa, Shivalingaiah Sudharshan
Venom Research Unit, Adichunchanagiri Biotechnology and Cancer Research Institute, Karnataka, India.
An Acad Bras Cienc. 2016 Mar;88(1):197-209. doi: 10.1590/0001-3765201620140574. Epub 2016 Mar 4.
The standard aqueous stem bark extract is consumed as herbal drink and used in the pharmaceutical formulations to treat patients suffering from various disease conditions in Cuba. This study was carried out to evaluate the modulatory effect of standard aqueous bark extract of M. indica on Group IA sPLA2. M. indica extract, dose dependently inhibited the GIA sPLA2 (NN-XIa-PLA2) activity with an IC50 value 8.1 µg/ml. M. indica extract effectively inhibited the indirect hemolytic activity up to 98% at ~40 µg/ml concentration and at various concentrations (0-50 µg/ml), it dose dependently inhibited the edema formation. When examined as a function of increased substrate and calcium concentration, there was no relieve of inhibitory effect on the GIA sPLA2. Furthermore, the inhibition was irreversible as evidenced from binding studies. It is observed that the aqueous extract ofM. indica effectively inhibits sPLA2 and it is associated inflammatory activities, which substantiate their anti-inflammatory properties. The mode of inhibition could be due to direct interaction of components present in the extract, with sPLA2 enzyme. Further studies on understanding the principal constituents, responsible for the anti-inflammatory activity would be interesting to develop this into potent anti-inflammatory agent.
在古巴，标准水提茎皮提取物被用作草药饮品，并用于药物制剂中治疗患有各种疾病的患者。本研究旨在评估印度楝标准水提树皮提取物对IA组分泌型磷脂酶A2（sPLA2）的调节作用。印度楝提取物以剂量依赖性方式抑制GIA sPLA2（NN-XIa-PLA2）活性，IC50值为8.1 µg/ml。印度楝提取物在浓度约为40 µg/ml时可有效抑制间接溶血活性达98%，并且在各种浓度（0 - 50 µg/ml）下，它以剂量依赖性方式抑制水肿形成。当作为底物和钙浓度增加的函数进行检测时，对GIA sPLA2的抑制作用没有减轻。此外，结合研究表明这种抑制是不可逆的。据观察，印度楝水提取物可有效抑制sPLA2及其相关的炎症活性，这证实了它们的抗炎特性。抑制模式可能是由于提取物中存在的成分与sPLA2酶直接相互作用。进一步研究了解负责抗炎活性的主要成分，对于将其开发成有效的抗炎剂将是有意义的。
