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The purpose of this paper was to evaluate the phytochemical profile of Acacia cyclops trunk bark methanol extract using LC-MS/MS, as well as to assess its antioxidant and anti-tyrosinase activities. Thus, total phenolic and flavonoid contents of the studied extract were established and 19 compounds were detected and quantified. In addition of their antioxidant potential against DPPH and ABTS assays, in vitro and in silico studies were adopted to evaluate tyrosinase inhibitory property of A. cyclops extract. Methanol trunk bark extract showed significant total phenolic content, antioxidant potential in terms of free radical scavenging, as well as an interesting tyrosinase inhibitory action (IC50= 05.12 ± 0.41 μg/mL). The molecular docking analysis and the drug-likeness prediction of the major selected compounds supported the significant anti-tyrosinase activity of the studied extract. The obtained results suggest that A. cyclops extract could be a promising candidate in the treatment of skin hyperpigmentation disorders. [ABSTRACT FROM AUTHOR]

This study aimed to investigate the effects of combined exposure to noise (85 dB(A)) and inhaled Toluene (300 ± 10 ppm) on rat lung health. It also aimed to assess the potential therapeutic effects of Olea europaea L. leaves extract (OLE) (40 mg/kg/day) using biochemical, histopathological, and immunohistochemical (IHC) analyses, as well as determination of pro-inflammatory cytokines (TNF-α and IL-1β), and in silico Docking studies. The experiment involved forty-two male Wistar rats divided into seven groups, each exposed to a 6-week/6-hour/day regimen of noise and Toluene. The groups included a control group, rats co-exposed to noise and Toluene, and rats co-exposed to noise and Toluene treated with OLE for different durations. The results indicated that noise and Toluene exposure led to structural damage in lung tissue, oxidative harm, and increased levels of pro-inflammatory cytokines (TNF-α and IL-1β). However, the administration of OLE extract demonstrated positive effects in mitigating these adverse outcomes. OLE treatment reduced lipid peroxidation and enhanced the activities of catalase and superoxide dismutase, indicating its anti-oxidant properties. Furthermore, OLE significantly decreased the levels of pro-inflammatory cytokines compared to the groups exposed to noise and Toluene without OLE treatment. Moreover, the in silico investigation substantiated a robust affinity between COX-2 and OLE components, affirming the anti-inflammatory activity. Overall, our findings suggest that OLE possesses anti-inflammatory and anti-oxidative properties that mitigate the adverse effects of concurrent exposure to noise and Toluene. [ABSTRACT FROM AUTHOR]

Since ancient times, humans have turned to medicinal plants for treating various ailments and curing specific diseases, as these natural plants serve as the primary source of a range of phytochemicals, including triterpenes. Maslinic acid (MA), also known as (2α,3β)-2,3-dihydroxyolean-12-en-28-oic acid, is a pentacyclic triterpene acid present in numerous plants including olive, known for its high safety profile in humans. Recent experimental data increasingly suggests that MA exhibits diverse biological properties and therapeutic effects on various organ diseases, highlighting its significant potential for clinical applications due to its diverse potential pharmacological activities that promote health and resist various diseases, such as hypoglycemic, neuroprotective, anti-tumor, anti-inflammatory, antioxidant and multiple other biological activities. However, the undesirable pharmacokinetic properties of MA, such as high lipophilicity, pose a limitation to its application and development, impacting its bioavailability. Consequently, extensive research spanning decades has focused on structurally modifying MA to overcome these limitations and enhance its pharmacokinetic and therapeutic characteristics, leading to the identification of several potential lead compounds. In this review, we focus on the progress of research in recent years on MA with interest to its chemical and enzymatic modifications as well as the relationships between the modified structures or derivatives and their biological activities. [ABSTRACT FROM AUTHOR]

A new series of N-benzyl-2,5-dihydro-1H-pyrrole-linked benzopyrimidines 5 and 6 were synthesized via the 1,3-dipolar cycloaddition reaction of acetylenic dipolarophiles 3 and 4 with azomethine ylide generated in situ from N-(methoxymethyl)-N-(trimethylsilyl)benzylamine and evaluated for their in vitro antimicrobial activity. The structures of the prepared products were characterized using 1H/13C NMR, IR, and ESI-HRMS techniques. Further, the synthesized compounds were assessed for their antibacterial activity against five types of pathogenic bacteria and three fungal strains. The results show that the degree of antimicrobial effect displayed by the synthesized compounds was variable. Notably, compounds 2a, 2d, 2f, 3e, 3h, 4a, 4d, 4f, 5a, 5b, 5d, 5f, 6b, and 6c showed high activity against the bacterial strains, with MIC values ranging from 15.12 to 15.62 μg mL−1. Moreover, compounds 2a, 2f, 5a, 5b, 5d, 5g, and 5h exhibited promising antifungal activity against three Candida strains, with MIC values ranging from 62.5 to 125 μg mL−1. In addition, molecular docking studies performed to identify the most effective antibacterial compounds against B. subtilis highlighted the high binding affinity of the synthesized compounds toward Bacillus subtilis YdiB (pdb: 5MVR). [ABSTRACT FROM AUTHOR]

The present research aimed to establish the polyphenolic profile and to appraise the cytotoxic activity first by in vitro analyses, followed by a confirmatory in silico study to establish a stronger biochemical rationale for the activity of the ethyl acetate extract obtained from the bark of Tetraclinis articulata. Total phenolics and flavonoids of the ethyl acetate extract were quantified (phenolics, 65.30 mg gallic acid equivalents/g extract; flavonoids, 28.90 mg quercetin equivalents/g extract). A total of 22 polyphenolic compounds were identified in the ethyl acetate extract by HPLC-PDA/ESI-MS analysis. Tetraclinis articulata extract exerted a significant cytotoxic effect against a HeLa cell line (IC50 = 07.02 ± 1.15 μg/mL). The in silico analysis was in agreement with the in vitro study in which major constituents of ethyl acetate extract showed low binding energy and a correct mode of interaction in the active pocket of the enzyme (PDB: 4I5I). These results might be due to the synergistic action of constituents present in ethyl acetate extract or acting separately. This is the first report on the polyphenolic composition and cytotoxic activity of the extract from the bark of T. articulata. [ABSTRACT FROM AUTHOR]

A series of maslinic acid (MA) and oleanolic acid (OA)-based analogs with potent antibacterial and antibiofilm activities were designed and semi-synthesized starting from isolated pentacyclic triterpene acids as natural products from olive pomace (Olea europaea L.). These conjugates were synthesized via a last step of Cu-catalyzed azide–alkyne cycloaddition (CuAAC) between propargylated quinolone/fluoroquinolones (QN/FQNs) and MA/OA azides to achieve new triazole derivatives in overall excellent yields. The latter hybrids were screened in vitro for their antibacterial and antibiofilm activities towards two Gram-positive (Staphylococcus aureus and Enterococcus faecalis) and two Gram-negative bacteria (Escherichia coli and Pseudomonas aeruginosa). Results indicated that some of the maslinic acid derivatives exhibited significant activity against all tested strains with MIC values within a range of 3.25–30 μg mL−1. Moreover, evaluated compounds depicted moderate to significant antibiofilm activity with inhibition percentage going up to 68.75% against S. aureus biofilm formation. The molecular modeling using docking study of the antibacterial activity of synthesized compounds showed that some derivatives displayed high antibacterial potentials. [ABSTRACT FROM AUTHOR]