Amino-Acid-Conjugated Natural Compounds: Aims, Designs and Results

Abstract

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.

Targeting yeast topoisomerase II by imidazo and triazoloacridinone derivatives resulting in their antifungal activity

“…Unfortunately, due to the presence of a fungal cell wall and variances in membrane permeability, certain potent yTOPOII inhibitors face challenges in reaching their intended molecular target 16 – 18 . Unfavorable properties can be eliminated by modifying the lead structure for example by changing the lipophilicity or combining it with amino acids, which increases their bioavailability and decreases cytotoxicity 17 , 19 – 21 . An example of such an approach is the modification of nitroacridine derivative by lysine moiety that led to increased activity of the compound against fluconazole-resistant fungal cells 17 .…”

“…With this in mind, we have decided to modify the structures of the previously studied compounds 16 including C-1305 , C-1311 , as well as C-1330 , and more thoroughly analyzed the properties of a new group of triazoloacridinones ( IKE1-8 ) C-1305 derivatives and imidazoacridinones ( IKE9-14 ) C-1311 derivatives in terms of their influence on yTOPOII activity as well as their ability to affect fungal growth. Modifying the structure of a potential drug compound by conjugation with lysine is also proposed as an efficient approach to increase the ability to penetrate the fungal cell and decrease cytotoxicity 19 , 20 .…”

Quercetin as a Promising Antiprotozoan Phytochemical: Current Knowledge and Future Research Avenues

“…In this respect, the Que–glutamic acid conjugate exhibited a remarkable resistance to hydrolases, resulting in a much longer half-life (180 min). When compared with Que, the Que–aspartic acid and Que–glutamic acid conjugates demonstrated an enhanced intestinal permeability in Madin-Darby canine kidney (MDCK) cells [ 164 ]. Que-metal complexes (metals such as germanium, vanadium, and copper) also showed better pharmacokinetic properties and have been successfully tested for their activity on diverse human cancer cell lines [ 158 ].…”

Effect of Sustainable Pretreatments on the Nutritional and Functionality of Chickpea Protein: Implication for Innovative Food Product Development

“…Tey are essential to the structure and function of all living organisms. Amino acids are made up of an amino group (-NH2), a carboxyl group (-COOH), and a side chain (R group) that is unique to each amino acid [42]. Te amino acid composition of chickpeas contributes to their superior protein quality.…”