Geranyl Dihydrochalcones from Artocarpus altilis and Their Antiausteric Activity

Abstract

Human pancreatic cancer cell lines have remarkable tolerance to nutrition starvation, which enables them to survive under a tumor microenvironment. The search for agents that preferentially inhibit the survival of cancer cells under low nutrient conditions is a novel antiausterity strategy in anticancer drug discovery. In this study, the methanolic extract of the leaves of Artocarpus altilis showed 100 % preferential cytotoxicity against PANC-1 human pancreatic cancer cells under nutrient-deprived conditions at a concentration of 50 µg/mL. Further investigation of this extract led to the isolation of eight new geranylated dihydrochalcones named sakenins A–H (1–8) together with four known compounds (9–12). Among them, sakenins F (6) and H (8) were identified as potent preferentially cytotoxic candidates with PC₅₀ values of 8.0 µM and 11.1 µM, respectively.

Key words

antiausterity agent - Artocarpus altilis - Moraceae - pancreatic cancer - PANC-1

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