Drug intelligence / Profile preview

methyl amooranin

Development stage
Preclinical
Lead developer
Enzyme Bio-Systems
Modality
Small Molecules
Administration
Oral, Intravenous, Intraperitoneal, Intramuscular, Subcutaneous, Topical
01

Overview

**Methyl amooranin** is a novel synthetic oleanane triterpenoid derived from modifications of amooranin (AMR), a natural triterpenic acid extracted from the stem bark of *Amoora rohituka*, used in Ayurvedic medicine for malignancies. It exhibits potent cytotoxicity against various tumor cell lines, including breast cancer cells (e.g., MCF-7, MDA-MB-231, MDA-MB-468), inducing **G2/M cell cycle arrest**, **apoptosis** via caspase activation (e.g., caspase-3/7, caspase-8), upregulation of pro-apoptotic proteins (p53, Bax, JNK, MAPK), downregulation of anti-apoptotic (Bcl-2) and cell cycle proteins (cyclin A, cyclin B1), and inhibition of COX-2 mRNA expression. At lower doses, it reverses multidrug resistance by blocking P-glycoprotein-mediated drug efflux, potentiates chemotherapy like doxorubicin in xenografts, suppresses tumor growth and inflammatory cascades, inhibits metastatic breast cancer cell migration (IC50 66.4 μM in MDA-MB-231), and modulates genes involved in drug transport, signaling, cytochrome C release, and angiogenesis. Early clinical trial potential noted for human cancers.[1][2][3][4][5][6][7][8]

Other names
AMR-Memethyl-25-hydroxy-3-oxoolean-12-en-28-oatemethyl25-hydroxy-3-oxoolean-12-en-28-oatemethyl 25-hydroxy-3-oxoolean-12-en-28-oate
02

Targets

ABCB1 (P-glycoprotein)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)

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