Prenylated Flavonoids with Selective Toxicity against Human Cancers

The antiproliferative activity of xanthohumol ( ), a major prenylated chalcone naturally occurring in hops, and its aurone type derivative ( )-6,4'-dihydroxy-4-methoxy-7-prenylaurone ( ) were investigated. Both flavonoids, as well as cisplatin as a reference anticancer drug, were tested in vivo...

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Bibliographic Details
Published in:International journal of molecular sciences 2023-04, Vol.24 (8), p.7408
Main Authors: Tronina, Tomasz, Bartmańska, Agnieszka, Popłoński, Jarosław, Rychlicka, Magdalena, Sordon, Sandra, Filip-Psurska, Beata, Milczarek, Magdalena, Wietrzyk, Joanna, Huszcza, Ewa
Format: Article
Language:English
Subjects:
Animals
anticancer selectivity
Antimitotic agents
Antineoplastic agents
Antineoplastic Agents - pharmacology
Antineoplastic Agents - therapeutic use
antiproliferative activity
aurone
Breast Neoplasms - drug therapy
Cancer
Care and treatment
Cell Line, Tumor
Cell Proliferation
Chalcones - pharmacology
Cisplatin - pharmacology
Cisplatin - therapeutic use
Colon cancer
Female
Flavonoids - pharmacology
Flavonoids - therapeutic use
human carcinoma
Humans
Instrument industry
Isoflavones
Leukemia
Lung cancer
Mice
Prostate cancer
xanthohumol
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Summary:The antiproliferative activity of xanthohumol ( ), a major prenylated chalcone naturally occurring in hops, and its aurone type derivative ( )-6,4'-dihydroxy-4-methoxy-7-prenylaurone ( ) were investigated. Both flavonoids, as well as cisplatin as a reference anticancer drug, were tested in vivo against ten human cancer cell lines (breast cancer (MCF-7, SK-BR-3, T47D), colon cancer (HT-29, LoVo, LoVo/Dx), prostate cancer (PC-3, Du145), lung cancer (A549) and leukemia (MV-4-11) and two normal cell lines (human lung microvascular endothelial (HLMEC)) and murine embryonic fibroblasts (BALB/3T3). Chalcone and aurone demonstrated potent to moderate anticancer activity against nine tested cancer cell lines (including drug-resistant ones). The antiproliferative activity of all the tested compounds against cancer and the normal cell lines was compared to determine their selectivity of action. Prenylated flavonoids, especially the semisynthetic derivative of xanthohumol ( ), aurone were found as selective antiproliferative agents in most of the used cancer cell lines, whereas the reference drug, cisplatin, acted non-selectively. Our findings suggest that the tested flavonoids can be considered strong potential candidates for further studies in the search for effective anticancer drugs.
ISSN:1422-0067
1661-6596
1422-0067
DOI:10.3390/ijms24087408