Drug intelligence / Profile preview

trilobatin

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral
01

Overview

Trilobatin is a natural dihydrochalcone glucoside, chemically described as phloretin with a β-D-glucopyranosyl at the 4' position; it occurs in the leaves of Lithocarpus polystachyus (Chinese “sweet tea”) and functions as a sweetening plant metabolite with reported antioxidant and anti‑inflammatory activities[1][8]. Preclinical studies report biological effects including improvement of DSS-induced colitis via suppression of NF‑κB signaling and modulation of gut microbiota in mice[3], regulation of glucose metabolism and insulin resistance through PI3K/Akt/GSK‑3β and Nrf2/Keap‑1 pathways in cell and STZ-mouse models[4], neuroprotection and cognitive benefit in Alzheimer’s disease models via direct binding to HMGB1 and activation of SIRT3/SOD2 signaling[6], and antidepressant-like effects in CUMS mice with identification as a naturally occurring GPR158 ligand[9][7]. It is available as a research chemical; there is no evidence of clinical approval as a pharmaceutical drug[8].

Other names
phloretin-4'-O-glucosidephloretin 4'-glucosidep-phlorizinp-phloridzin1-[4-(β-D-glucopyranosyloxy)-2,6-dihydroxyphenyl]-3-(4-hydroxyphenyl)propan-1-one3,5-dihydroxy-4-[3-(4-hydroxyphenyl)propanoyl]phenyl β-D-glucopyranosideCAS 4192-90-9CAS4192-90-9CAS-4192-90-9
02

Targets

HMGB1 (High mobility group protein B1)GPR158 (G protein-coupled receptor 158)NF-κBPI3K (Phosphoinositide-3-kinase regulatory subunit 6)KEAP1 (Kelch-like ECH-associated protein 1)AKT1 (Proto-oncogene serine/threonine-protein kinase Akt1)SIRT3 (NAD-dependent protein deacetylase sirtuin-3)gp41 (Human immunodeficiency virus type 1 glycoprotein 41)GSK3 (Glycogen synthase kinase 3 beta)NFE2L2 (Nuclear factor (erythroid-derived 2)-like 2)

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