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.

Compounds having their chemical structure based on coumarin framework have enticed much research concern not only because of the variance structural characteristic but also the pluralism of the bioactivities. In this report, four derivatives of 7halo-4-coumarinylacetic acid referred to as RY1-RY4 were synthesized, and their chemical backbones were confirmed via the employed spectrophotometers. The pharmacokinetic profiles of the synthesized halocoumarins were inspected in silico using a free online software named the pre-ADMET program. The potential of the synthesized halocoumarins as antitumor applicants was evaluated utilizing 5-fluorouracil as a reference drug and the well-authenticated protocol based on the MTT as a visible indicator against eight standard tumor-cell lines. The outcomes acquired from this assessment indicated that the synthesized halocoumarins, except RY1, have less impact as antitumor agents comparing with the standard drug. Also, the halocoumarins revealed roughly the same fashion of activity versus the test cell lines with the greatest inhibitory influence reported against MCF-7 and HeLa. From the calculated pharmacokinetic data and outcomes exhibited from antitumor assessment, the authors concluded that the synthesized halocoumarins, particularly RY1, offered potential applicants as antitumor agents with broad-ranged activity. Besides, the compounds RY1 and RY2 may provide highly valuable scaffolds for synthesizing agents with a powerful antitumor activity versus the breast and cervical cancer phenotypes.

Despite their rarity and structural complexity, natural and synthetic biscoumarins have polarized much attention from investigators particularly due to their characteristic activity as anticoagulant agents. In this work, a panel of twelve functionalized biscoumarins was synthesized in two schematic steps; the first one started by condensing various phenol-based derivatives with malonic acid via a Pechmann-type reaction yielding alkyl-substituted 4-hydroxycoumarins herein symbolized as (E1-E12). The latter compounds were undergone a self-coupling under the influence of methylene iodide to afford the target functionalized biscoumarins, which were symbolized as (EY1-EY12). The potential of the synthesized biscoumarins as anticoagulant applicants was investigated in vivo using rabbit as an animal model. The employed assay was the prothrombin time that was monitored after three and five days of the last oral treatment. The results gathered from this test revealed that the synthesized biscoumarins have a promising anticoagulant activity compared with warfarin as a standard anticoagulant drug, with privileged influence contributed to those substituted at position 7 of the coumarin framework. The authors concluded that the substitution of an alkyl group at that position of the coumarin monomer may intensify the anticoagulant activity of the prepared biscoumarins. Also, this intensity was directly proportionated to the increase in the molecular weight of this alkyl group. Accordingly, the synthesized biscoumarins possessing this property would provide an efficient base for synthesizing new compounds, which have a promising anticoagulant effect.

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