Anticancer activity of the plant flavonoid luteolin against preclinical models of various cancers and insights on different signalling mechanisms modulated

Abstract

Various signaling mechanisms contribute significantly to the development of multiple cancers. Small molecules with the potential of influencing a wide variety of molecular targets may prove as broad-spectrum anticancer agents. Flavonoids from plant sources are strongly emerging as promising antineoplastic molecules because of their ability to hamper different cancer-driving signaling pathways. Further, these flavonoids offer an additional benefit due to their congenital antioxidant potential. This paper discusses the anticancer activity of luteolin against a number of cancers including leukemias, prostate cancer, pancreatic cancer, breast cancer, lung cancer, colorectal cancer, melanoma, liver, gastric, and brain cancer. Strong emphasis has been laid on key molecular mechanisms impacted by luteolin for exerting antineoplastic effect. Importantly, certain epigenetic targets like histone deacetylases (HDACs), DNA methylation regulator enzymes that are influenced by this befitting flavone for inducing cytotoxicity in certain preclinical cancer models, have also been made the part of this review. Additionally, the significantly improved therapeutic benefits of luteolin in combination with other therapeutics are comprehensively discussed. The current loopholes in luteolin research are also considered, which may open novel routes for further valuable studies on this promising flavone.

Phenolic-Rich Extracts from Avocado Fruit Residues as Functional Food Ingredients with Antioxidant and Antiproliferative Properties

“…Navarro-Salcedo, et al [49] reported that the effectiveness of pure sakuranetin (IC 50 = 10 to 30 µg/mL) against esophageal carcinoma EC-109 cells was comparable to that observed for the acetonitrile extract obtained from the leaves of Artemisia dracunculus plants. As for luteolin, diverse studies have shown that this flavonoid has strong antiproliferative activity against different human cancer cell lines, including lung cancer, myeloid leukemia, prostate cancer, and pancreatic cancer [50,51]. Therefore, the presence of these compounds may explain the differences observed in the antiproliferative activity of the avocado seed extracts and the seed coat extracts.…”

Cogent role of flavonoids as key orchestrators of chemoprevention of hepatocellular carcinoma: A review

“…Significantly, luteolin can regulate epigenetic targets like histone deacetylases (HDACs) and DNA methylation regulator enzymes, which are influenced by flavones, for inducing anticancer effect in certain preclinical cancer models. Additionally, the studies revealed that the therapeutic effect of luteolin is improved when it is combined with conventional anticancer treatment modalities (Ganai et al, 2021). Luteolin protects the HCC and controls the stress‐induced damage by the reactive oxygen species as reported in the case of N‐nitrosodiethylamine‐induced HCC using an animal model system (Balamurugan & Karthikeyan, 2012).…”

Histone Deacetylase, Xanthine Oxidase and Urease Inhibitory Activities of Eremurus spectabilis M. Bieb. Extracts

“…More so, over activity of this enzyme has been associated not only with cancer progression (due to enhanced cell proliferation), but also to cancer induction. Therefore, inhibition of HDAC is at the center of research and paramount for the discovery of new and safe molecules with anticancer properties (20). In our study, both ethanolic and ethyl acetate extracts of E. spectabilis were found to have much higher HDAC inhibitory activity than the VPA.…”