Bioactivity of Some Natural and Semisynthetic Coumarin Derived Compounds

Abstract

A couple of natural coumarins was identified in the seeds of two apples’ cultivars commonly known as Granny Smith and Red Delicious. The effect of the phenolic hydroxyl moieties found in these products was evaluated on the bioactivity. This evaluation included the structural alteration of these moieties into less hydrophilic ones to explore the significance of the parent moieties on the biological activity. The investigated biopotentials were antioxidant, antiproliferative, antibacterial, and antifungal effects. The antioxidant potential was investigated by detecting the ability of the natural and semisynthetic coumarins to trap the free hydroxyl and DPPH radicals. The antiproliferative potential was assessed via an MTT-depended assay versus eight cancerous-cell lines, included HeLa, SK-OV-3, AR42J, MCF-7, AB12, KYSE-30, LC540, and AMN3. The antibacterial potential was tested versus six common pathogenic bacterial strains via a well-defined disc diffusion assay. These pathogens were Escherichia coli, Salmonella typhi, Klebsiella pneumonia, Haemophilus influenzae, Shigella dysenteriae, and Pseudomonas aeruginosa. The antifungal potential was also screened by utilizing a similar microbiological technique versus three pathogenic fungi, involved Candida albicans, Aspergillus flavus, and Aspergillus niger. It is concluded that the investigated chemical moiety has a positive influence on the antioxidant and antiproliferative potentials of the natural derivatives, and a negative one on their antibacterial and antifungal potentials.

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“…As a result, eating Citrullus lanatus as a snack or nutritional drink may increase the human body's antioxidant potential and help enhance cell signaling adhesion and other biological processes. Furthermore, the antioxidant capacity of polyphenols is determined by their chemical structure, quantity, absorption, and bioavailability [51,52]. High-performance liquid chromatography combined with electrospray ionization-quadrupole time-of-flight mass spectrometry was used to analyze phytochemicals contained in a methanolic isolate of Citrullus lanatus [51].…”

“…High-performance liquid chromatography combined with electrospray ionization-quadrupole time-of-flight mass spectrometry was used to analyze phytochemicals contained in a methanolic isolate of Citrullus lanatus [51]. Furthermore, the research assessed phytonutrients have recognized antioxidant properties like whole lycopene (3.74 to 6.80 mg/100 g), carotenoids (4.90 to 8.06 mg/100 g), flavonoids (55.60 to 100.93 mg/100 g distill water), tannin (35.07 to 60.83 mg/100 g distill water), and phenol content (16.77 to 21.41 mg/g distill water) [51][52][53]. In comparison to the yellow-fleshed melon (vitamin C: 52.05 mg/kg, lycopene: 0.04 mg/kg), the red-fleshed melon had greater levels of vitamin C (86.32 mg/kg) and lycopene (9.50 mg/kg), which corresponded with anti-oxidant capability [54,55].…”

“…Cancer is a terrible illness with a high mortality rate worldwide. The molecular process of tumorgenesis in a living process can be influenced by the relationship between the active components of food and the regulation of gene expression in many metabolic processes [56,57]. For example, lycopene, the isolated product of Citrullus lanatus, can help to prevent malignancy by inhibiting DNA mutations and preventing metastasis [58].…”

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“…This is owing to the robust relationship between oxidative stress and various tenacious diseases, such as cancer, diabetes, and inflammatory disorders. Accordingly, the development of semisynthetic compounds from well-known natural antioxidants has piqued the attendance of the medical profession [51][52][53].…”

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“…Ozen et al [72] created a Schiff-base linker in twelve albocarbon-based compounds. Several techniques were used to test these hybrids' free radical scavenging capability, including metal chelating, phosphomolybdenum, reducing power, lipid peroxidation, and H2O2 scavenging activity experiments [59][60][61][62][63][64][65][66][67][68][69][70][71]. Compared to the control, the hybrids symbolized as NAPH5, NAPH10, and NAPH12 (Figure 43) were the most effective antioxidants at 10 and 50 mM doses.…”