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Planta Medica 2014-Feb

Geranyl dihydrochalcones from Artocarpus altilis and their antiausteric activity.

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Mai Thanh Thi Nguyen
Nhan Trung Nguyen
Khang Duy Huu Nguyen
Hien Thu Thi Dau
Hai Xuan Nguyen
Phu Hoang Dang
Tam Minh Le
Trong Huu Nguyen Phan
Anh Hai Tran
Bac Duy Nguyen

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Abstraktne

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.

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