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Ref Type Journal Article
PMID (27333990)
Authors Rabi T, Catapano CV
Title Aphanin, a triterpenoid from Amoora rohituka inhibits K-Ras mutant activity and STAT3 in pancreatic carcinoma cells.
Journal Vol Issue Date Pages Journal Short Title
Tumour biology : the journal of the International Society for Oncodevelopmental Biology and Medicine 37 9 2016 Sep 12455-12464 Tumour Biol
URL
Abstract Text Mutations of the K-Ras gene occur in over 90 % of pancreatic carcinomas, and to date, no targeted therapies exist for this genetically defined subset of cancers. STAT3 plays a critical role in KRAS-driven pancreatic tumorigenesis, suggesting its potential as a therapeutic target in this cancer. Therefore, finding novel and potential drugs to inhibit oncogenic K-Ras is a major challenge in cancer therapy. In an attempt to develop novel anti-KRAS mutant chemotherapeutics, we isolated three novel triterpenoids from Amoora rohituka stem and their chemical structures were characterized by extensive 1H-NMR, 13C-NMR, Mass, IR spectroscopic studies and chemical transformations. Aphanin (3 alpha-angeloyloxyolean-12-en-28-oic acid) is one of the isolated novel triterpenoid compounds. We found aphanin exhibited antiproliferative effects, caused G0-G1 cell cycle arrest, inhibits K-Ras G12D mutant activity by decreased STAT3, p-STAT3, Akt, p-Akt, cyclin D1 and c-Myc expressions, and induced apoptosis in pancreatic cancer HPAF-II (ΔKRAS G12D ) cells. The apoptosis proceeded through depletion of GSH with a concomitant increase in the reactive oxygen species production. The results of our study have important implications for the development of aphanin as potential novel agent for the treatment of K-Ras mutant pancreatic cancer, and STAT3-cMyc-cyclinD1 axis may serve as an important predictive biomarker for the therapeutic efficacy.

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Molecular Profile Treatment Approach
Gene Name Source Synonyms Protein Domains Gene Description Gene Role
Therapy Name Drugs Efficacy Evidence Clinical Trials
Aphanin Aphanin 0 0
Drug Name Trade Name Synonyms Drug Classes Drug Description
Aphanin echinenone Akt Inhibitor (Pan) 21 c-MYC Inhibitor 12 KRAS Inhibitor 15 STAT3 Inhibitor 26 Aphanin is a triterpenoid derived from the plant Amoora rohituka that inhibits proliferation and induces apoptosis in cancer cells through inhibition of mutant Kras, Stat3, Akt, and Myc signaling, and regulation of reactive oxygen species (PMID: 27333990).
Gene Variant Impact Protein Effect Variant Description Associated with drug Resistance
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References