Drug intelligence / Profile preview

N,N'-bis(4-[(α-L-rhamnosyloxy)benzyl]thiourea)

Development stage
Preclinical
Lead developer
South China University of Technology
Modality
Small Molecules
Administration
Oral
01

Overview

N,N'-bis(4-[(α-L-rhamnosyloxy)benzyl]thiourea), also known as PG-1, is a bioactive phenolic glycoside isolated from the seeds of the *Moringa oleifera* plant. This thiourea derivative is characterized by its potent antioxidant, anti-inflammatory, and anti-cancer properties. In preclinical research, PG-1 has demonstrated significant inhibitory effects on hepatocellular carcinoma (HCC) cells, specifically the HepG2 line, by inducing mitochondrial-mediated apoptosis and arresting the cell cycle. To address challenges related to its poor aqueous solubility and low oral bioavailability, researchers have developed liposomal delivery systems (e.g., PG-1-liposomes) to enhance its pharmacokinetic profile and therapeutic efficacy. These formulations have shown promise in targeting liver cancer cells with minimal toxicity to non-malignant cells, positioning PG-1 as a potential candidate for further development in oncology and metabolic diseases.

Other names
N,N'-bis({4-[(α-L-rhamnosyloxy)benzyl]}thiourea)Phenolic glycoside 1
02

Targets

BAX (Apoptosis regulator BAX)CASP9 (Caspase-9)CASP3 (Caspase-3)

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