Cyperaceae Species Are Potential Sources of Natural Mammalian Arginase Inhibitors with Positive Effects on Vascular Function,Journal of Natural Products

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Cyperaceae Species Are Potential Sources of Natural Mammalian Arginase Inhibitors with Positive Effects on Vascular Function
Journal of Natural Products ( IF 3.3 ) Pub Date : 2017-08-24 00:00:00 , DOI: 10.1021/acs.jnatprod.7b00197
Kamel Arraki ₁ , Perle Totoson ₁ , Alain Decendit ₂ , Alain Badoc ₂ , Andy Zedet ₁ , Julia Jolibois ₁ , Marc Pudlo ₁ , Céline Demougeot ₁ , Corine Girard-Thernier ₁

Affiliation

The inhibition of arginase is of substantial interest for the treatment of various diseases of public health interest including cardiovascular diseases. Using an ex vivo experiment on rat aortic rings and an in vitro assay with liver bovine purified arginase, it was demonstrated that several polyphenolic extracts from Cyperus and Carex species possess vasorelaxant properties and mammalian arginase inhibitory capacities. Phytochemical studies performed on these species led to the identification of eight compounds, including monomers, dimers, trimers, and tetramers of resveratrol. The potential of these stilbenes as inhibitors of mammalian arginase was assessed. Five compounds, scirpusin B (5), ε-viniferin (4), cyperusphenol B (6), carexinol A (7), and the new compound virgatanol (1), showed significant inhibition of arginase, with percentage inhibition ranging from 70% to 95% at 100 μg/mL and IC₅₀ values between 12.2 and 182.1 μM, confirming that these stilbenes may be useful for the development of new pharmaceutical products.

中文翻译：

莎草科物种是天然哺乳动物精氨酸酶抑制剂的潜在来源，对血管功能有积极影响

精氨酸酶的抑制对于治疗包括心血管疾病在内的各种公共卫生感兴趣的疾病具有重大意义。使用大鼠主动脉环的离体实验和肝牛精氨酸酶的体外测定，证明了莎草属和Carex物种的几种多酚提取物具有血管舒张特性和哺乳动物精氨酸酶抑制能力。对这些物种进行的植物化学研究导致鉴定出八种化合物，包括白藜芦醇的单体，二聚体，三聚体和四聚体。这些stilbenes作为哺乳动物精氨酸酶抑制剂的潜力进行了评估。五种化合物，scirpusin B（5），ε-viniferin（4），cyperusphenol B（6），carexinol A（7）和新的化合物virgatanol（1）对精氨酸酶有明显的抑制作用，在100μg/ mL时抑制百分比范围为70％至95％，IC ₅₀值在12.2至182.1μM之间，这证实了这些斯蒂尔苯可能对开发新的医药产品有用。

更新日期：2017-08-24

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