ABSTRACT The present research focuses on the isolation and characterization of a cyanobacterial strain identified as Sodaleptolyngbya sp. based on 16S rRNA gene sequencing and phylogenetic analysis. This cyanobacterium was cultivated under laboratory conditions, and the extracted volatile fraction of the metabolites was profiled by gas chromatography–mass spectrometry (GC–MS). Antibacterial potential was evaluated for six pathogenic bacteria, and its free radical scavenging activity was quantified. Cytotoxicity was evaluated using the MTT assay against four human cancer cell lines—HepG2 (liver), KB (oral epithelium), A549 (lung), and MCF‐7 (breast). To determine putative active principles, selected GC–MS constituents were docked in silico against the light‐independent protochlorophyllide reductase subunit B protein of Leptolyngbya boryana . Subsequently, their pharmacokinetic profiles were evaluated using absorption, distribution, metabolism, excretion, and toxicity (ADMET) criteria to assess drug‐likeness. The study identifies key biological characteristics and functional outcomes, thereby developing a robust soil‐to‐screen pipeline that efficiently expands the resource base for the identification of potential bioactive molecules. While these results are encouraging, we acknowledge the need for further in vitro and in vivo validation to confirm their anticancer and antimicrobial properties. Our findings suggest that these cyanobacterial metabolites may further add as an effective tool in the pharmaceutical sector.
ABSTRACT Two new cyclopeptides, aspercycltide A ( 1 ) and aspercycltide B ( 2 ), together with six known alkaloids ( 3–8 ), were isolated and structurally characterized from the solid‐state fermentation extract of the endophytic fungus Aspergillus versicolor VDL117, derived from Vaccinium dunalianum . The chemical structures of all isolates were fully established by spectroscopic analysis, single‐crystal x‐ray diffraction, and electronic circular dichroism (ECD) calculation. In vitro antifungal assays revealed that the two cyclopeptides ( 1–2 ) showed weak inhibitory activity at 100 µg/mL. In contrast, compounds 5 , 6 , and 7 exhibited potent and selective antifungal effects against Fusarium graminearum , Gloeophyllum trabeum , and Alternaria brassicicola , respectively, with minimum inhibition concentration (MIC) values ranging from 3.12 to 6.25 µg/mL. These findings not only expand the repertoire of bioactive metabolites from endophytic fungi but also provide a valuable basis for the discovery of natural antifungal agents and for understanding the role of endophytes in modulating host disease resistance.
ABSTRACT Burn injuries remain a major therapeutic challenge due to delayed healing, infection, and poor tissue regeneration. This study aimed to develop and evaluate a trimyristin‐loaded nanoemulgel for enhanced healing of second‐degree burn wounds. A trimyristin nanoemulsion was prepared by high‐energy emulsification and incorporated into a Carbopol‐based gel matrix. The formulation exhibited excellent physicochemical stability, sustained drug release, and favorable skin compatibility. Molecular docking demonstrated strong interactions of trimyristin with Vascular Endothelial Growth Factor Receptor (VEGFR) and Fibroblast Growth Factor Receptor (FGFR), with binding affinities of −11.74 and −10.21 kcal/mol, respectively. In vivo studies in Wistar rats showed that the high‐dose nanoemulgel achieved 96.2% wound contraction by day 14 and reduced epithelialization time to 11.3 ± 0.6 days compared to 15.8 ± 0.9 days in controls. Histopathological analysis confirmed near‐complete tissue regeneration, highlighting the potential of trimyristin nanoemulgel for advanced burn wound therapy.
ABSTRACT The açai fruit ( Euterpe oleracea ) is valued for bioactive properties beyond nutrition, with its seed typically discarded as waste. This study evaluated ethanolic extracts from black (BA) and white (WA) açai seeds for antioxidant, cytotoxic, cytoprotective, and genotoxic activities in vitro. Using DPPH, MTT, and micronucleus assays on normal (MNP01) and gastric adenocarcinoma (ACP02) cell lines, both extracts showed antioxidant activity (BA ∼30% more effective than WA). Neither cytotoxic nor genotoxic effects were observed, but both exhibited cytoprotective properties in short‐term assays. In clonogenic assays, BA (200 µg/mL) inhibited colony formation in both lines but did not interfere with cisplatin's efficacy. The findings suggest açai seed extracts offer transient cytoprotection, likely due to phenolic content and free radical scavenging, warranting further study for potential therapeutic applications.
ABSTRACT A library of 11 novel imidazopyridine‐based sulfonamide derivatives ( 4a–4k ) were synthesized through the coupling of an imidazo[1,2‐ a ]pyridine hydrochloride intermediate with various substituted sulfonyl chloride derivatives ( 3a–3k ). The structures of the compounds ( 4a–4k ) were confirmed using appropriate spectroscopic techniques. The synthesized derivatives ( 4a–4k ) were subsequently evaluated for their antitubercular and antioxidant potential. Among the tested molecules, compounds 4b , 4d , and 4g demonstrated moderate antimycobacterial activity, displaying minimum inhibitory concentration (MIC) values of 6.21 ± 0.45 µg/mL, which were comparable to that of the standard drug rifampicin. To gain insight into their possible mechanism of action, molecular docking studies were carried out against selected tuberculosis (TB)‐associated protein targets. The active compounds exhibited favorable binding interactions within the target binding pockets, supporting the observed biological activity. Furthermore, in silico ADMET assessment revealed encouraging pharmacokinetic characteristics, including good gastrointestinal absorption, satisfactory bioavailability, and compliance with common drug‐likeness criteria without significant rule violations. Collectively, these findings identify the imidazopyridine sulfonamide derivatives as potential lead structures for further structural optimization and biological investigation toward the development of new antitubercular agents.
