February 23, 2024

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Novel conjugates – Amino acid, Peptides, Oligonucleotides, Polymer & Phytocompounds

Medical research

Plants are being recognized as potential source of drug discovery and more than 80% of modern drugs are derived directly from natural sources (plants, microbes, cells etc.) or their molecules/compounds. Phyto-derived bio-active compounds, known for their varied health benefits, enhance antibacterial, antifungal, anticarcinogenic, and anti-inflammatory biological actions. Currently there is huge tendency of conjugating amino acid/peptide residues with small phyto-derived bio-active compounds in the field of medical research. The conjugation of different amino acids/peptides to various biologically active phytocompounds has fetched the outstanding results as are very promising drug candidates. Additionally, the amino acid/peptide based drugs have low toxicity, ample bioavailability and permeability, modest potency and good metabolic and pharmacokinetic properties.

Cosmetic applications

Phytocompounds used in cosmeceuticals include catechins, gallic acids, epicatechins, curcumin, hydroxylbenzoic and cinnamic acids, quercetin, ascorbic acids, luteolin, alpha and beta carotene, complex polysaccharides, and fatty acids.  Even though various macrosized phytobioactive compounds are used in cosmeceutical formulations, their solubility and formulation type have limitations in enhancing the effect of phyto-based cosmeceuticals and therapy The major limitations of phyto-based cosmeceutical therapy include less skin penetration, lower prolongevity, less final quality and lower whitening effects. These qualities depend on the solubility and size of the active phytocompounds. This leads us in search of novel amino acid/peptide-phytocompounds for enhanced skin health efficiency of cosmeceutical products.

Conjugation method

Conjugation based on amide bond formation, used in the earliest works, has been supplemented with “click” chemistry, thiol‐maleimide reactions and several other methods, like oxime formation, Schiff base formation and “living” polymer chain end termination. Conjugates have also been prepared by non-covalent coupling of functionalised polymers and proteins using biorecognition.

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