Vasconcellea chilensis Planch. ex A. DC., an endemic Chilean wild relative of mountain papaya ( V. pubescens ) adapted to extreme coastal environments, is largely unexplored for fruit phytochemistry. The ethanol extract yielded six 27- O -caffeoyl lupane triterpenoids ( 1 – 6 ), including two novel C-28 methyl esters, vasconcellates A and B ( 5 , 6 ), and one known lignan ( 7 ). This is the first report of caffeoyl lupanes in the Caricaceae family. Compounds 1 – 7 were evaluated for inhibition of the Wingless/Integrated (Wnt)/β-catenin signaling pathway in a colorectal cancer model. Compound 4 (27- O - E -caffeoylbetulinic acid) showed marked activity by disrupting Frizzled 4 (FZD4) and Dishevelled 1 (DVL1) interaction (EC₅₀ = 16.2 ± 1.1 μM), suppressing Wnt target gene transcription (IC₅₀ = 12.1 ± 0.7 μM), and reducing CaCo-2 cell proliferation by 40% at 30 μM after 48 h. Docking indicated binding to the FZD4 cholesterol pocket, suggesting allosteric modulation. These results identify V. chilensis fruit as a novel source of bioactive triterpenoids with potential for colorectal cancer prevention.
Lupane triterpenes isolated from Vasconcellea chilensis (wild papaya) inhibit colorectal cancer cell growth by targeting the Wnt/β-catenin signaling pathway / Scaletta, F., Formisano, C., Madrid, A., Montenegro, I., Izzo, L., Samavat, M.S., Afra, S., Stornaiuolo, M., Taglialatela-Scafati, O., Sirignano, C., Rigano, D.. - In: Fitoterapia. - ISSN 0367-326X. - 192:(2026). [10.1016/j.fitote.2026.107294]
Lupane triterpenes isolated from Vasconcellea chilensis (wild papaya) inhibit colorectal cancer cell growth by targeting the Wnt/β-catenin signaling pathway
Scaletta, FlaviaPrimo
;Formisano, Carmen;Izzo, Luana;Stornaiuolo, Mariano;Taglialatela-Scafati, Orazio;Sirignano, Carmina
;Rigano, DanielaUltimo
2026
Abstract
Vasconcellea chilensis Planch. ex A. DC., an endemic Chilean wild relative of mountain papaya ( V. pubescens ) adapted to extreme coastal environments, is largely unexplored for fruit phytochemistry. The ethanol extract yielded six 27- O -caffeoyl lupane triterpenoids ( 1 – 6 ), including two novel C-28 methyl esters, vasconcellates A and B ( 5 , 6 ), and one known lignan ( 7 ). This is the first report of caffeoyl lupanes in the Caricaceae family. Compounds 1 – 7 were evaluated for inhibition of the Wingless/Integrated (Wnt)/β-catenin signaling pathway in a colorectal cancer model. Compound 4 (27- O - E -caffeoylbetulinic acid) showed marked activity by disrupting Frizzled 4 (FZD4) and Dishevelled 1 (DVL1) interaction (EC₅₀ = 16.2 ± 1.1 μM), suppressing Wnt target gene transcription (IC₅₀ = 12.1 ± 0.7 μM), and reducing CaCo-2 cell proliferation by 40% at 30 μM after 48 h. Docking indicated binding to the FZD4 cholesterol pocket, suggesting allosteric modulation. These results identify V. chilensis fruit as a novel source of bioactive triterpenoids with potential for colorectal cancer prevention.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
