Drug intelligence / Profile preview

gigantol

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral, Intravenous, Intraperitoneal
01

Overview

Gigantol is a bibenzyl phenolic compound primarily extracted from plants in the genus Dendrobium, particularly from the stem of Dendrobium aurantiacum and other medicinal orchids. It is used in traditional Chinese medicine and has demonstrated multiple bioactivities including anticancer, anti-osmotic, antimutagenic, and immunomodulatory properties. The compound has shown promising therapeutic potential against various cancer types, particularly lung cancer and hepatocellular carcinoma. Gigantol exerts its anticancer effects through multiple mechanisms including inhibition of the PI3K/Akt/NF-κB signaling pathway, suppression of the Wnt/β-catenin pathway, induction of apoptosis, and reduction of cancer stem cell-like phenotypes. It has also been reported to inhibit aldose reductase and shows potential as a neuroprotective agent. The molecular formula is C16H18O4 with a molecular weight of 274.31 g/mol.

Other names
5-(2-(3-hydroxy-5-methoxyphenyl)ethyl)-2-methoxyphenolPhenol, 5-[2-(3-hydroxy-5-methoxyphenyl)ethyl]-2-methoxy-5-(3-hydroxy-5-methoxyphenethyl)-2-methoxyphenol3,3'-dihydroxy-5,4'-dimethoxybibenzyl
02

Targets

AKT (RAC-alpha serine/threonine-protein kinase)ESR1 (ERα)GSK3 (Glycogen synthase kinase 3 beta)HSP90AA1 (Heat shock protein HSP90-alpha)PI3K (Phosphoinositide-3-kinase regulatory subunit 6)XIAPmTOR (Mammalian target of rapamycin kinase)AR (Adrenergic receptors)Sucrase-IsomaltaseBAX (Apoptosis regulator BAX)CASP3 (Caspase-3)DEK (DEK proto-oncogene)LRP6 (Low-density lipoprotein receptor-related protein 6)NF-κBPARP1 (Poly (adp-ribose) polymerase 1)TP53 (Cellular Tumor Antigen p53 R175H)

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