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Abstract

The incidence of many human disorders, such as cancer, oxidative stress, diabetes mellitus, and inflammatory diseases, has been mountingly increased because of many factors, including environmental pollution, static lifestyle, and unhealthy feeding. In an attempt to explore a scaffold with multiple biomedical activities, four natural phenolic acids, namely vanillic-, protocatechuic-, ferulic-, and caffeic-acid, were selected to construct twelve derived coumarins. The skeletal formulas of the semi-synthesized coumarins were confirmed by analyzing their spectra afforded via various spectrophotometers. The biomedical characteristics of these coumarins were investigated and included their antioxidant, anti-inflammatory, antidiabetic, and anticancer activities. The antioxidant activity was quantified by monitoring the potential of these coumarins to reduce DPPH and hydroxyl oxidants and provide an electron in the redox reaction. The anti-inflammatory activity was detected by specifying the inhibitory and selectivity of these coumarins on two COX isozymes. The antidiabetic activity was determined by examining the capacity of these coumarins to suppress two enzymes involved in blood glucose regulation. The anticancer activity and cytotoxicity were examined via MTT-based methodology versus four cancer cell lines and one normal cell line. The findings revealed that the semi-synthesized coumarins exhibited potent antioxidant and anticancer activities with low-induced cytotoxicity. Also, these coumarins showed modest antidiabetic potential and inhibitory effects versus the COX isozymes, with some selectivity toward the inhibition of COX-2. The authors concluded that these coumarins, specifically YC11, provide a valid structural template for synthesizing multi-functional agents effective in treating health situations in which oxidative stress, inflammation, diabetes, and cancer are combined.

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“…Many ancient societies have embraced the use of herbal products due to their safety and feasibility, allowing them to gain benefits from their biological activity [23]. More specifically, aqueous extracts derived from various sections of a variety of plants are commonly used in traditional home treatments [24][25][26][27].…”

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“…By dividing the values of Measure II and Measure I over each other, a third variable denominated as activity evidence (Measure III) was calculated for individual extract versus every employed bacterial type. To meliorate the results, the utilized methodology was repeated for three times [32].…”

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“…Different doses of the compound under investigation (2 mg/mL) were generated prior to performing these two experiments. With MeOH as a solvent, concentration levels of 1000, 800.00, 400.00, 200.00, 100.00, 50.00, and 25.00 μM were generated [33][34][35][36][37].…”