Drug intelligence / Profile preview

neogambogic acid

Development stage
Preclinical
Lead developer
Tianjin University of Traditional Chinese Medicine
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

Neogambogic acid is a natural xanthone compound derived from the resin of Garcinia species and is an active ingredient in traditional Chinese medicine gamboge. It exhibits potent antitumor and antibacterial activities. Mechanistically it induces apoptosis and inhibits cell proliferation in various cancer cell lines by modulating multiple signaling pathways including JNK and NF-kB (nuclear factor kappa-light-chain-enhancer of activated B cells), PI3K/Akt/mTOR pathway and MAPK/ERK pathway[1][6]. Neogambogic acid also suppresses osteoclastogenesis by inhibiting RANKL-induced activation of JNK and NF-kB pathways[6]. Additionally it has demonstrated significant inhibitory activity against methicillin-resistant Staphylococcus aureus (MRSA) both in vitro and in vivo by targeting the saeRS two-component system involved in bacterial virulence regulation[5]. Despite its promising pharmacological effects its clinical application is limited by poor aqueous solubility; research into advanced delivery systems such as liposomes or adiposomes aims to overcome this barrier for future therapeutic use[3][4].

Other names
2-Butenoic acid, 4-(3a,4,5,7,10,11-hexahydro-8,9-dihydroxy-3,3,11-trimethyl-13-(3-methyl-2-butenyl)-11-(4-methyl-3-pentenyl)-7,15-dioxo-1,5-methano-1H,3H,9H-furo(3,4-g)pyrano(3,2-b)xanthen-1-yl)-2-methyl-(E)-4-[10,12-dihydroxy-8,21,21-trimethyl-5-(3-methylbut-2-enyl)-8-(4-methylpent-3-enyl)-14 ,18-dioxo - 3 ,7 ,20 -trioxahexacyclo[15.4.1.02 ,15 .02 ,19 .04 ,13 .06 ,11 ]docosa - 4(13),5 ,11 ,15-tetraen -19 - yl ] - 2 - methylbut - 2 - enoic acid
02

Targets

AKT1 (Proto-oncogene serine/threonine-protein kinase Akt1)SaeRS (SaeRS two-component regulatory system)UppS (Undecaprenyl diphosphate synthase)

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