Department of Pharmaceutical Analysis and Medicinal Chemistry, Faculty of Pharmacy, Universitas Padjadjaran, Sumedang 45363, Indonesia.
Department of Pharmacochemistry, Faculty of Pharmacy, Universitas Mulawarman, Samarinda 75119, Indonesia.
Molecules. 2022 Nov 7;27(21):7631. doi: 10.3390/molecules27217631.
Protein is one of the essential macronutrients required by all living things. The breakdown of protein produces monomers known as amino acids. The concept of conjugating natural compounds with amino acids for therapeutic applications emerged from the fact that amino acids are important building blocks of life and are abundantly available; thus, a greater shift can result in structural modification, since amino acids contain a variety of sidechains. This review discusses the data available on amino acid-natural compound conjugates that were reported with respect to their backgrounds, the synthetic approach and their bioactivity. Several amino acid-natural compound conjugates have shown enhanced pharmacokinetic characteristics, including absorption and distribution properties, reduced toxicity and increased physiological effects. This approach could offer a potentially effective system of drug discovery that can enable the development of pharmacologically active and pharmacokinetically acceptable molecules.
蛋白质是所有生物必需的宏量营养素之一。蛋白质的分解产生单体，称为氨基酸。将天然化合物与氨基酸结合用于治疗应用的概念源于以下事实：氨基酸是生命的重要组成部分，并且大量存在；因此，更大的转变可以导致结构修饰，因为氨基酸含有各种侧链。这篇综述讨论了关于氨基酸-天然化合物缀合物的可用数据，这些数据涉及它们的背景、合成方法和生物活性。几种氨基酸-天然化合物缀合物已显示出增强的药代动力学特性，包括吸收和分布特性、降低毒性和增加生理效应。这种方法可以提供一种潜在有效的药物发现系统，能够开发出具有药理活性和药代动力学可接受的分子。
