Cotabarren Juliana, Claver Santiago, Payrol Juan Abreu, Garcia-Pardo Javier, Obregón Walter David
Centro de Investigación de Proteínas Vegetales (CIPROVE), Departamento de Ciencias Biológicas, Facultad de Ciencias Exactas, Universidad Nacional de la Plata, Buenos Aires B1900, Argentina.
Escuela Latinoamericana de Medicina, La Habana 19108, Cuba.
Pharmaceutics. 2021 Apr 8;13(4):512. doi: 10.3390/pharmaceutics13040512.
Plant cystatins (or phytocystatins) comprise a large superfamily of natural bioactive small proteins that typically act as protein inhibitors of papain-like cysteine proteases. In this report, we present the purification and characterization of the first phytocystatin isolated from (MoPI). MoPI has a molecular mass of 19 kDa and showed an extraordinary physicochemical stability against acidic pHs and high temperatures. Our findings also revealed that MoPI is one of the most potent cysteine protease inhibitors reported to date, with i and IC values of 2.1 nM and 5.7 nM, respectively. More interestingly, MoPI presents a strong antimicrobial activity against human pathogens such as and . In addition, MoPI also showed important anticoagulant activity, which is an unprecedented property for this family of protease inhibitors. These results highlight the pharmaceutical potential of this plant and its derived bioactive molecules.
植物半胱氨酸蛋白酶抑制剂（或植物胱抑素）构成了一个庞大的天然生物活性小蛋白超家族，通常作为木瓜蛋白酶样半胱氨酸蛋白酶的蛋白质抑制剂发挥作用。在本报告中，我们展示了从[具体植物名称未给出]中分离出的首个植物胱抑素（MoPI）的纯化及特性鉴定。MoPI的分子量为19 kDa，并且在酸性pH值和高温条件下表现出非凡的物理化学稳定性。我们的研究结果还表明，MoPI是迄今为止报道的最有效的半胱氨酸蛋白酶抑制剂之一，其抑制常数（Ki）和半数抑制浓度（IC50）分别为2.1 nM和5.7 nM。更有趣的是，MoPI对诸如[具体病原体名称未给出]和[具体病原体名称未给出]等人类病原体具有强大的抗菌活性。此外，MoPI还表现出重要的抗凝活性，这对于该蛋白酶抑制剂家族来说是前所未有的特性。这些结果突出了这种植物及其衍生的生物活性分子的药用潜力。
