Chalcones are indeed a versatile scaffold in medicinal chemistry. Their structure, featuring an α,β-unsaturated carbonyl group, makes them highly reactive and capable of interacting with various biological targets. This reactivity is a key reason why chalcones and their derivatives are of such interest in drug discovery. The continued exploration of chalcone derivatives in medicinal chemistry will likely yield new insights and therapeutic candidates, given their broad spectrum of biological activities and the flexibility in modifying their structures. As chalcone derivatives, pyranochalcones and chromanchalcones are members of a subclass of flavonoids that are widely distributed. Several scientific databases were investigated to compile articles that illustrated the biological functions of chromenochalcones and their derivatives. Preclinical research on chromenochalcones and their derivatives is well covered in this review, highlighting the compounds with enormous significance as antimalarial, anti-inflammatory, antileishmanial, cytotoxic, antibacterial, antifungal, and antioxidant agents. In addition, the article briefly discusses the synthetic pathways employed for the total synthesis of selected pyranochalcones, including mallaophilippens C and E, citrunobin, and lesperol. Consequently, this overview may help research and design novel, potent therapeutic medications based on previously developed methodologies. This review is intended to provide a thorough, authoritative, and critical assessment of the chromenochalcone template for the chemistry community.

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Methicillin-resistant Staphylococcus aureus (MRSA) infections are prevalent in hospitals and often lead to significant health complications. This study aimed to explore the chemical composition of the aerial part of Crotalaria madurensis and evaluate its antioxidant and antibacterial properties. The impact of gamma irradiation on the antibacterial properties of the plant extract and metabolite 1 against MRSA was also examined. Fourier-transform infrared (FTIR) analysis was conducted on the filtrates of untreated MRSA and MRSA treated with the plant extract and metabolite 1. Four flavonol glycosides were identified as gossypetin 8-methoxy, 3-O-β-D-xylopyranoside (metabolite 1), gossypetin 8-O-β-D-glucopyranoside (metabolite 2), kaempferol 3-O-β-D-glucpyranoside (Astragalin, metabolite 3), and herbacetin 7-methoxy-3-O-β-D-glucopyranoside (metabolite 4). All metabolites exhibited significant antioxidant properties using different assays. The antibacterial efficacy of the extract and metabolite 1, which showed substantial antioxidant properties compared to the other isolated metabolites, was evaluated. Both the plant extract and metabolite 1 significantly reduced the viability and cell count of MRSA at concentrations of 1.0 and 0.5 mg/ml. The antibacterial activity of the plant extract and metabolite 1 was assessed after gamma irradiation at 50 and 100 Gy, which did not significantly affect the antibacterial efficiency. FTIR analysis indicated that the plant extract and metabolite 1 significantly altered the band frequency values, bandwidth, and peak intensity % of the treated MRSA filtrate. Molecular docking studies suggested that metabolite 1 exhibited the highest antioxidant and anti-MRSA activity, with strong binding scores like the ligand, indicating an effective interaction and high affinity between metabolite 1 and the target molecule.

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Plants provide an unlimited source of bioactive compounds, possessing tremendous applications in the pharmaceutical industry. In the search for sources of antioxidants and antimicrobial agents against human pathogens, ethanol extracts of Crotalaria juncea flowers (CJ flower extract) were evaluated. The highest total phenolic (5.65 μg GAE/ml) and flavonoid (0.43 μg QE/ml) contents were observed in the 100 μg/ml CJ flower extract. To assess antioxidant activity, three in vitro antioxidant tests were employed: DPPH radical-scavenging, ABTS + radical-scavenging, and hydroxyl radical-scavenging assay. The CJ flower extract demonstrated significant ( P Microsporum gypseum and five Gram-positive bacteria ( Propionibacterium acnes , Staphylococcus aureus , Staphylococcus epidermidis , Streptococcus pyogenes , and Streptococcus mutans ), as well as one Gram-negative bacterium ( Escherichia coli ). The CJ flower extract inhibited the growth of both fungal and bacterial pathogens. The cytotoxicity of the CJ flower extract was measured using a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay, and the highest concentration of the extract (100 μg/ml) did not affect L929 cell viability. Moreover, the CJ flower extract demonstrated the ability to suppress H 2 O 2 -induced toxicity in L929 cells. Overall, the CJ flower extract has potential as an alternative source for exploring new antioxidants, antimicrobial agents, and cytoprotectants that could prove valuable for biomedical applications.

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Chalcones are among the leading bioactive flavonoids with a therapeutic potential implicated to an array of bioactivities investigated by a series of preclinical and clinical studies. In this article, different scientific databases were searched to retrieve studies depicting the biological activities of chalcones and their derivatives. This review comprehensively describes preclinical studies on chalcones and their derivatives describing their immense significance as antidiabetic, anticancer, anti-inflammatory, antimicrobial, antioxidant, antiparasitic, psychoactive, and neuroprotective agents. Besides, clinical trials revealed their use in the treatment of chronic venous insufficiency, skin conditions, and cancer. Bioavailability studies on chalcones and derivatives indicate possible hindrance and improvement in relation to its nutraceutical and pharmaceutical applications. Multifaceted and complex underlying mechanisms of chalcone actions demonstrated their ability to modulate a number of cancer cell lines, to inhibit a number of pathological microorganisms and parasites, and to control a number of signaling molecules and cascades related to disease modification. Clinical studies on chalcones revealed general absence of adverse effects besides reducing the clinical signs and symptoms with decent bioavailability. Further studies are needed to elucidate their structure activity, toxicity concerns, cellular basis of mode of action, and interactions with other molecules.

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Two new compounds, crotmadine (1) and crotmarine (3); a known pyrrolizidine alkaloid, fulvine (8), and three other known compounds, trans-3,4,3',5'-tetra methoxystilbene (5), dihydroalpinumisoflavone (6), and 4',5,7-trihydroxy-3-methoxyflavone (7), have been isolated from the leaves and stems of Crotalaria madurensis. Both crotmadine (1) and crotmarine (3) exhibit antifungal activity against Trichophyton mentagrophytes.

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