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Bauhinia bauhinioides Kallikrein Inhibitor Fragments with Bradykinin-Like Activities

机译:Bauhinia Bauhinioides Kallikrein抑制剂片段与Bradykinin样活动

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Medicinal plants extracts contain many proteinase inhibitors that could be an interesting source of new drugs. Structural modifications in some of this kind of macromolecule could also lead to compounds with interesting biological properties [1]. In this work, we studied one peptide fragment (BbKIsi-62) of Bauhinia bauhinioides kallikrein inhibitor (BbKI) [2,3] and its analogue (P2) that was designed by the insertion of a proline residue in order to mimic the TV-terminal region of the bradykinin (BK) molecule. Both retro inverso counterparts Ri-BbKIsira and Ri-P? were also included. We evaluated the capability of the peptides to induce contraction on stomach fundus of mouse as well as their capability to induce calcium release from guinea pig ileum cell culture. Both biological effects induced by the fragments were compared with the ones caused by BK.
机译:药用植物提取物含有许多蛋白酶抑制剂,可能是新药物的有趣来源。一些这种大分子的结构修饰也可能导致具有有趣的生物学性质的化合物[1]。在这项工作中,我们研究了紫荆花型葡萄酮蛋白抑制剂(BBKI)[2,3]的一种肽片段(BBKISI-62)及其类似物(P2),其通过插入脯氨酸残留物而设计,以模仿电视 - Bradykinin(BK)分子的末端区域。 ri-bbkisira和ri-p都是复古inverso对应者也包括在内。我们评估了肽在胃部诱导小鼠的胃底诱导患者的能力以及它们诱导豚鼠感应细胞培养物的钙释放的能力。将片段诱导的生物学效应与由BK引起的碎片进行比较。

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