Drug intelligence / Profile preview

tyrosine and proline conjugated trolox + hydroxy-cinnamic acid + diclofenac

Development stage
Preclinical
Modality
Peptide-Drug Conjugates → Peptide Conjugates → Peptides, Small Molecules
Administration
Intraperitoneal, Oral (potential/formulation Dependent)
01

Overview

A synthetic hybrid compound containing tyrosine- and proline-conjugated trolox, hydroxy-cinnamic acid, and diclofenac, designed to integrate antioxidant, anti-inflammatory, and hypolipidemic activities. Trolox (a water-soluble vitamin E analog) is conjugated with the amino acids tyrosine and proline to enhance antioxidant capacity, while hydroxy-cinnamic acid contributes further antioxidant and metabolic effects. Diclofenac, a non-steroidal anti-inflammatory drug (NSAID), provides additional anti-inflammatory efficacy. The combined hybrid demonstrates high radical scavenging capability, lipid peroxidation inhibition (up to 12-fold that of parent antioxidants), and strong anti-inflammatory and hypolipidemic effects in preclinical models. In vivo, it reduces inflammation and plasma lipid levels significantly, outperforming reference drugs in some cases. This multi-functional profile is proposed for conditions characterized by concurrent oxidative stress, inflammation, and dyslipidemia[1][4].

02

Targets

15-LOX (Lysyl Oxidase)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)PGHS-1 (Prostaglandin G/H Synthase 1)

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