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Cytotoxic constituents of Glycosmis ovoidea collected in Vietnam by Peter J. Blanco Carcache; Gerardo D. Anaya Eugenio; Tran Ngoc Ninh; Curtis E. Moore; José Rivera-Chávez; Yulin Ren; Djaja D. Soejarto; A. Douglas Kinghorn is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

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Compounds derived from natural sources have been major contributors to the area of cancer chemotherapy for decades. As part of an ongoing effort to discover anticancer drug leads from tropical plants, a large-scale collection of Glycosmis ovoidea Pierre (Rutaceae), was made at Nui Chua National Park, Vietnam. Activity-guided fractionation of the chloroform-soluble fractions led to the isolation of nine coumarins, including the new compound, 1-(7-methoxy-2-oxo-2H-chromen-8-yl)-3-methyl-1-oxobut-2-en-2-yl (S)-2-methylbutanoate (1). An close analogue of 1, namely, kincuongin (2), was deemed as non-cytotoxic (IC > 10 μM) against five different cancer cell lines. However, co-administration of kimcuongin (2) showed an approximately 100 times potentiation of the MCF-7 breast cancer cell cytotoxicity of the previously reported flavonoid, 5,3'-dihydroxy-3,6,7,8,4'-pentamethoxyflavone (10). To provide a mechanistic basis for the cancer cell line inhibition enhancement observed, an initial in silico study on compound 10 indicated that it interacts with isoforms of the NF-κB complex. In a confirmatory western blot experiment conducted, kimcuongin (2) was found to potentiate the effects of flav

Who reads Cytotoxic constituents of Glycosmis ovoidea collected in Vietnam?

Author

Peter J. Blanco Carcache; Gerardo D. Anaya Eugenio; Tran Ngoc Ninh; Curtis E. Moore; José Rivera-Chávez; Yulin Ren; Djaja D. Soejarto; A. Douglas Kinghorn

Publisher

Elsevier BV

Published

2022

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)