Abstract
Nowadays, the beneficial role of a healthy lifestyle, particularly emphasizing the quality of foods and cancer management, is accepted worldwide. Polyphenols and oleic acid play a key role in this context, but are still scarcely used as anti-cancer agents due to their bio-accessibility limits. Therefore, we aimed to synthesize a set of new oleoyl-hybrids of quercetin, morin, pinocembrin, and catechin to overcome the low bioavailability of polyphenols, throughout a bio-catalytic approach using pancreatic porcine lipase as a catalyst. The in vitro assays, using a wide panel of human cancer cell lines showed, mainly for two novel regioisomer oleoyl-hybrids of quercetin, a remarkable increase in apoptotic cell populations. We suggested that the DNA damage shown as ɣH2AX signals might be the major cause of apoptotic cell death. Finally, we demonstrated convincing data about two novel polyphenol-based hybrids displaying a highly selective anti-cancer cytotoxicity and being superior compared to their reference/parental compounds.
Highlights
Colorectal cancer (CRC) is a multistep process involving several genetic or epigenetic changes culminating in the transformation of normal into malignant cells characterized mainly by the uncontrolled proliferation [1,2]
We aimed to synthesize a set of new oleoyl-hybrids of quercetin, morin, pinocembrin, and catechin to overcome the low bioavailability of polyphenols, throughout a bio-catalytic approach using pancreatic porcine lipase as a catalyst
In many countries the Mediterranean diet it is not accessible and the preventive effects of these kinds of foods against cancer should have been lost. To overcome these strong limits, several hybrid compounds were designed and synthesized, using a bio-catalytic approach, oleoyl ester-based of QUE, morin, pinocembrin, and catechin to explore their antiproliferative activity in a wide panel of human cancer cell lines and to propose a possible mechanism of action (Figure 1)
Summary
Colorectal cancer (CRC) is a multistep process involving several genetic or epigenetic changes culminating in the transformation of normal into malignant cells characterized mainly by the uncontrolled proliferation [1,2]. Catechin, especially (+)-catechin, the form present in tea leaves, has many beneficial properties for human health such as anticancer, anti-obesity, antidiabetic, cardiovascular, anti-infectious, hepatoprotective, and neuroprotective effects [20,21] Another important natural compound is oleic acid (OLAC) available in high contents in extra virgin olive oil, the main fat used in the Mediterranean diet, to which amazing healthy properties are ascribed. In many countries the Mediterranean diet it is not accessible and the preventive effects of these kinds of foods against cancer should have been lost To overcome these strong limits, several hybrid compounds were designed and synthesized, using a bio-catalytic approach, oleoyl ester-based of QUE, morin, pinocembrin, and catechin to explore their antiproliferative activity in a wide panel of human cancer cell lines and to propose a possible mechanism of action (Figure 1)
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