Search Results (12,515)

Fungi are a prolific source of diverse bioactive metabolites, yet many remain unexplored. Among these, depsidones are a rare class of compounds with significant biological potential, but they are seldom reported in mushrooms. This study investigated the medicinal fungus Ganoderma lucidum, known for its extensive therapeutic use in traditional medicine. Fruiting bodies were extracted using petroleum ether, ethyl acetate, n-butanol, and methanol. Extracts were screened phytochemically and assessed for total phenolic content and antioxidant activity using the DPPH assay. Ethyl acetate extract exhibited the highest phenolic yield and antioxidant potential and was subsequently evaluated for cytotoxicity against HepG2, HCT116, MCF7, and A549 cancer cell lines. It showed notable anticancer activity with minimal toxicity to normal Vero cells. UHPLC/Q-TOF-MS/MS analysis of G. lucidum ethyl acetate extract tentatively identified nine minor depsidones including mollicellin G, simplicildone I, mollicellin B, talaromyone B, simplicildone A, purpactin C, emeguisin B, mollicellin E, and simplicildone D on the basis of high-resolution negative-mode detection and characteristic MS/MS fragmentation patterns. Molecular docking revealed strong binding affinities between these compounds and cancer-related targets (AKT1, CDK2, ERK1, TNFα), with simplicildone D and mollicellin G demonstrating particularly high interactions. These findings provide mechanistic insights into the observed bioactivity and highlight G. lucidum as a promising source of therapeutic depsidones for future anticancer drug development. Full article

This paper presents the first comprehensive analysis of the composition of volatile organic compounds (VOCs) present in the liverwort Calypogeia sphagnicola belonging to the Calypogeiaceae family. Based on DNA markers, three genetically distinct groups were examined: C. sphagnicola f. sphagnicola; C. sphagnicola f. paludosa; and C. sphagnicola LC. The volatile organic compounds were determined using headspace solid-phase microextraction (HS-SPME) and analyzed by gas chromatography combined with mass spectrometry (GC-MS). A total of 65 organic compounds were detected from the tested plant material and 42 compounds were identified. The chemical analysis revealed distinct VOC profiles corresponding to three genetically defined groups. Sesquiterpenes (49.91–64.21%) and sesquiterpenoids (4.99–11.56%) dominated the VOC profiles, followed by monoterpenes (0.95–4.73%), aromatic compounds (2.43–5.12%), and aliphatic compounds (0.74–1.55%). It is noteworthy that aliphatic compounds were absent in C. sphagnicola f. paludosa, whereas the most abundant compounds were bicyclogermacrenes (20.92–33.60%) and anastreptenes (6.75–14.95%). Marker compounds were selected to allow for the rapid identification of individual genetic groups. Full article

Background: Colorectal cancer (CRC) is the third most common cancer worldwide, with liver metastasis being the leading cause of mortality. De novo fatty acid synthesis plays a critical role in CRC progression and metastasis. Bufalin, a cardiotonic steroid isolated from toad skin, has demonstrated anticancer activity in multiple preclinical models. However, the mechanisms underlying its suppression of CRC metastasis and modulation of fatty acid synthesis remain to be elucidated. Methods: The effects of bufalin on CRC cell proliferation, migration, and apoptosis were assessed via colony formation, wound healing, and flow cytometry assays. Transcriptome analysis identified bufalin-affected pathways, with changes in gene and protein expression. FASN protein levels were quantified using ELISA. Results: Bufalin inhibited proliferation and migration of CRC cells and induced the apoptosis of LoVo and HCT8 cells. Transcriptome analysis highlighted lipid metabolism pathways as potential mediators of bufalin’s anti-metastatic activity. Notably, bufalin reduced the expression of fatty acid synthase (FASN) and suppressed CRC metastasis. In vivo experiments demonstrated that bufalin attenuated CRC progression and liver metastasis by inhibiting de novo fatty acid synthesis through the PI3K/AKT-mediated SREBP1/FASN pathway. Conclusions: Bufalin inhibits de novo fatty acid synthesis via the PI3K/AKT-mediated SREBP1/FASN pathway, suppressing CRC progression and liver metastasis. Full article

Abnormal skin pigmentation can cause significant esthetic concerns and impact quality of life. As melanin determines pigmentation, melanogenesis is a key target to manage pigmentation disorders. This study investigated the effects of extracts from the rhizome of Iris ×germanica L. var. florentina Dykes (often called Iris florentina L.) on melanogenesis. Active phytochemicals were identified by combining LC-MS-MS metabolic profiling with subsequent bioassay-directed fractionation of chromatographic eluent collected into 96-well plates. Fractions 41–43 increased melanin and contained germanaism B, providing evidence that it is a melanogenesis stimulator. In contrast, fractions 90–93 reduced melanin and contained iriflorental and iripallidal, identified as prospective melanogenesis inhibitors. To explore extract-based applications, the plant was subjected to ethanolic, chloroform, and supercritical carbon dioxide (SC-CO₂) extractions and tested in skin equivalent tissues. The ethanolic extract (rich in germanaism B) increased pigmentation, while the chloroform extract (higher in iriflorental and iripallidal) decreased it. The SC-CO₂ extract, with minimal germanaism B and enriched iriflorental and iripallidal, showed stronger depigmenting effect. This study is the first to report that rhizome of I. florentina contains phytochemicals with opposing effects on melanogenesis. Through different extraction processes, targeted extracts from a single botanical can address both hyper- and hypopigmentation, offering a novel approach to pigmentation modulation. Full article

The integration of essential oils (EOs) with biological control agents offers a promising alternative to synthetic pesticides, though compatibility remains unclear. This study evaluated nutmeg (Myristica fragrans, NM), cinnamon (Cinnamomum verum, CIN), and clove (Syzygium aromaticum, CL) specifically on S. oryzae and L. distinguendus. Olfactory and behavioral responses to whole EOs and major constituents (myristicin, cinnamaldehyde, eugenol) were analyzed using the area preference method (APM) and two-choice behavioral bioassay (TCB), with confirmation by gas chromatography–mass spectrometry (GC-MS). In S. oryzae, APM showed attraction to all three EOs (PI = 0.14 to 0.56). A paradox emerged, however, as single constituents were mostly repellent (eugenol: PI = −0.58 to −0.70; cinnamaldehyde: PI shifted from 0.16 to −0.20), underscoring the complexity of EO mixtures where multiple compounds act jointly rather than individually. In contrast, L. distinguendus strongly avoided CL and CIN in TCB, with fewer than 30% of parasitoids choosing the EO-treated side (χ² test, p < 0.05). CIN therefore demonstrated selective potential, simultaneously attracting S. oryzae while repelling L. distinguendus. These findings highlight the dual role of EOs as botanical pest control tools, while stressing the need to consider non-target effects before practical application. Full article

The incorporation of bioactive compounds from plant-based by-products into staple foods represents a sustainable strategy to enhance both nutritional quality and health benefits. The aim of this study was to evaluate the effect of buckwheat husk addition (1.5%, 3.0%, 4.5%) on the antioxidant activity, total phenolic content (TPC) and its profile, color parameters, and sensory attributes of wheat and wholemeal breads. Increasing the husk content significantly (p ≤ 0.05) enhanced antioxidant activity, especially in the lipid-soluble fraction, with the highest values observed at 4.5% addition. In terms of TPC, wheat bread showed a significant (p ≤ 0.05) increase (16.5%) only at 3.0% husk addition, while wholemeal breads exhibited consistent TPC growth at all levels, reaching a 35.2% increase at 4.5% enrichment. Phenolic profiling revealed syringic acid as the dominant compound, constituting up to 64.4% of total phenolic acids in wholemeal bread with 4.5% husk. Flavonoids content increased with husk addition, with rutin, catechin, and orientin most prominent. Color analysis indicated a reduction in lightness and hue angle, an increase in browning index and total color difference with higher husk addition. Addition of husk modified aroma, color, and mouthfeel. Wholemeal breads with 1.5% and 4.5% buckwheat husk had the highest acceptability, enhancing nutritional and functional quality without affecting preference. Buckwheat husk effectively enhances bread’s nutritional and functional quality. Full article

Plant Parasitic Nematodes (PPNs), such as Meloidogyne incognita, cause significant agricultural losses worldwide. Conventional nematicides like methyl bromide are being phased out due to environmental and health concerns, prompting the search for safer alternatives. In previous studies, chalcones 17, 25, and 30, flavonoid compounds, were shown to effectively kill the model nematode Caenorhabditis elegans at concentrations of 10⁻⁴ M. However, the potential of these chalcones to act synergistically at lower concentrations has not been explored. In this study, the nematicidal efficacy of chalcones 17, 25, and 30 was evaluated individually and in combination at concentrations as low as 10⁻⁶ M. The results demonstrate a strong synergistic effect, with combinations achieving 90–100% mortality in C. elegans within 3 days. Additionally, the combination index method revealed significant toxic effects against M. incognita with chalcones 17 and 30 in binary and ternary combinations. To assess the effects of these chalcones on nontarget organisms, chalcones were also tested for antimicrobial activity against soil bacteria; analysis of soil microbiota using 16S rRNA sequencing indicated that chalcones did not significantly disrupt microbial populations. Furthermore, tests on human pluripotent stem cells (hPSCs) reveal no major effects on the viability of these cells at concentrations as high as the concentrations needed to kill nematodes. These findings highlight the potential of chalcones 17, 25, and 30 for effective nematode control without harming soil bacteria or human cells. Full article

Background: This systematic review aims to evaluate the effectiveness of various treatments and strategies for managing infections caused by Vibrio parahaemolyticus and Vibrio alginolyticus in whiteleg shrimp (Penaeus vannamei). Shrimp aquaculture faces significant challenges from these pathogens, resulting in substantial economic losses. Vibrio species are known for their ability to form biofilms, enhancing their resistance to conventional treatments. Methods: The review follows the PRISMA guidelines, searching Scopus and PubMed databases for relevant studies on antibiotics and plant extracts used against these pathogens. Data were extracted and analysed to assess the effectiveness of different treatments, including antibiotics, plant extracts, and combined therapies. Results: The review found that while antibiotics remain widely used, the emergence of antibiotic-resistant strains necessitates alternative strategies. Plant extracts, rich in bioactive compounds such as flavonoids, showed promising antimicrobial activity. Combined therapies involving antibiotics and plant extracts were also explored for their potential to enhance treatment efficacy and reduce resistance. Conclusions: The findings underscore the importance of addressing biofilm formation in managing Vibrio-related infections and highlight the need for further research to develop sustainable and effective treatment protocols for shrimp aquaculture. Full article

Development of paclitaxel-induced neuropathic pain (PINP) during chemotherapy may lead to paclitaxel discontinuation, potentially compromising effective anticancer therapy. PINP can manifest as allodynia. One recently discovered key factor in paclitaxel-induced mechanical allodynia (PIMA) pathogenesis is the elevated activity of monoacylglycerol lipase (MAGL), an enzyme that metabolizes the endocannabinoid 2-arachidonoylglycerol (2-AG). Thus, inhibiting MAGL serves as a potential analgesic target. Notoginsenoside R1 (NGR1), a metabolite of Panax notoginseng, has shown promise in reducing oxidative stress and neuronal apoptosis in nerve injury models. However, its effects on PIMA and MAGL activity have not yet been explored. This study is a proof-of-concept preclinical study investigating the antiallodynic effects of NGR1 on PIMA in female BALB/c mice and also examining its effect on MAGL activity. The effect of treatment of mice with NGR1 intraperitoneally on the development of PIMA was evaluated. Molecular docking using CB-Dock2 compared the binding energies to MAGL of NGR1 and pristimerin, a triterpene MAGL inhibitor. The effects of NGR1 on human recombinant MAGL activity, as well as the MAGL activity in mice paw skin tissues, were assessed using MAGL inhibitor screening and MAGL activity assay kits, respectively. NGR1 prevented the development of PIMA in a dose-dependent manner. The docking scores showed that NGR1 has a good affinity for MAGL (−7.8 kcal/mol, binding energy) but less affinity than pristimerin (−10.3 kcal/mol). NGR1 inhibited the human recombinant MAGL activity in a reversible and concentration-dependent manner, although the inhibition was in a reverse order. Treatment of mice with NGR1 showed a non-significant trend in reducing the paclitaxel-induced increase in MAGL activity in the paw skin. This study shows for the first time that NGR1 prevents the development of PIMA and suggests that NGR1 has affinity for and inhibits human recombinant MAGL activity with a paradoxical inhibition pattern. More mechanistic studies are needed to fully elucidate the molecular mechanisms of NGR1 in preventing PIMA. Full article

The chemical composition of leaf essential oil of the harmful invasive species Chromolaena odorata collected in Vietnam was analyzed by GC/MS and chiral GC. All three essential oil samples (O1, O2 and O3) in this study fell into chemotype I characterized by α-pinene/geigerene/germacrene D/(E)-β-caryophyllene from a total of six different chemotypes. Chemotype I demonstrated larvicidal effects against Aedes aegypti (Linnaeus, 1762), Aedes albopictus Aedes albopictus (Skuse, 1894), Culex fuscocephala (Theobald, 1907) and Culex quinquefasciatus (Say, 1823), with 24 h LC₅₀ values ranging from 11.73 to 69.87 µg/mL. In contrast, its microemulsion formulation exhibited enhanced toxicity, yielding 24 h LC₅₀ values between 11.16 and 32.43 µg/mL. This chemotype also showed repellent efficacy against Ae. aegypti, with protection times ranging from 70.75 to 122.7 min. Fumigant toxicity was observed against Aedes aegypti, with LC₅₀ values of 40.27% at 0.5 h and 0.34% at 24 h. Molluscicidal activity was recorded with 48 h LC₅₀ values between 3.82 and 54.38 µg/mL against Indoplanorbis exustus (Deshayes, 1833), Pomacea canaliculate (Lamarck, 1822), Physa acuta (Draparnaud, 1805). Additionally, the chemotype exhibited acetylcholinesterase inhibitory activity, with an IC₅₀ value of 70.85 µg/mL. Antimicrobial potential was also demonstrated, with MIC values ranging from 2.0 to 128.0 µg/mL against Enterococcus faecalis, Staphylococcus aureus, Bacillus cereus, Escherichia coli, Salmonella enterica, and Candida albicans. The C. odorata essential oil can be considered as a potential bioresource for human health protection strategies. Full article

Despite the great structural diversity, plant lignans, coumarins, and xanthones share numerous biological activities, ranging from antimicrobial, anti-inflammatory, and antioxidant to antineoplastic and neuroprotective. The compounds, products of the shikimic acid biosynthetic pathway, also play an important role in plant–environment interactions. In a search for sustainable and renewable sources of these valuable plant products, numerous in vitro culture systems were investigated, including hairy root cultures. The Rhizobium rhizogenes-transformed root cultures of over 40 plant species representing 17 families of the plant kingdom were studied in this respect. The present review focuses on the hairy roots that may be efficient producers of valuable plant products with the prospect of use in the pharmaceutical, food, or cosmetics industry. In vitro culture systems based on hairy roots, which were used to elucidate the biosynthesis pathways of the high-added-value plant compounds, were also considered. Full article

Antibiotic resistance is one of the major threats to public health in the twenty-first century. In this line of work, plants represent a priceless source of antimicrobial compounds since they house chemically different metabolites with a wide range of therapeutic applications. This study reports the bioactivity-guided fractionation, characterization, and evaluation of the efficacy of antimicrobial compounds from leaf acetone extracts of the traditional medicinal plant Terminalia catappa against bacterial clinical isolates and dermatophytes. The acetone extract of T. catappa was subjected to column chromatography for the separation and purification of the phytocompounds. The fractions were analyzed using a thin-layer chromatography–bioautography assay to detect the antimicrobial potency of the eluted compounds. The efficacy of the antimicrobial compounds was evaluated by the minimum inhibitory concentration, minimum bactericidal concentration, and minimum fungicidal concentration. Spectral characterization and structure elucidation of the compound were also achieved. The leaf acetone extract, when subjected to gradient elution by column chromatography, resulted in eight fractions. The fraction Fr-2 was subjected to thin-layer chromatographic elution, which resulted in the elution of phytocompound with Rf value of 0.50 and the phytocompound exhibited antimicrobial activity in the TLC–bioautography assay, and it was isolated in pure form and confirmed as Apigenin 7-O-ß-D-glucopyranoside. The compound exhibited significant inhibition of the clinical isolate Staphylococcus aureus and Methicillin-resistant Staphylococcus aureus 1503 at 9.5 µg/mL. Dermatophytes, viz., Microsporum gypseum and Microsporum canis, were inhibited at 312 µg/mL. The present study successfully achieved the bioactivity-guided isolation and characterization of the flavone compound Apigenin 7-O-ß-D-glucopyranoside from T. catappa. Furthermore, the plant T. catappa represents a promising candidate for the exploration of antimicrobial compounds that could serve as potential plant-derived lead molecules for antimicrobial agents. Full article

Oxidative stress is a major contributor to skin aging and related disorders. This study comparatively evaluated the bioefficacy of Schinus terebinthifolius Raddi leaf extracts prepared using three extraction techniques: conventional extraction (CE), accelerated solvent extraction (ASE), and pulsed electric field (PEF) extraction, with 50% (v/v) ethanol and water as green solvents. Among all tested conditions, the CE-derived extract (C-4), obtained with 50% (v/v) ethanol for 120 min, exhibited the highest extraction yield (29.7%). It also showed the highest total phenolic (668.56 ± 11.52 mg gallic acid equivalent (GAE)/g dry material (DM)) and flavonoid content (2629.92 ± 112.61 mg quercetin equivalent (QE)/100 g DM), and potent antioxidant activity against 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical (12,645.50 ± 60.31 µmol Trolox equivalent (TE)/g DM) and oxygen radical absorbance capacity assay (ORAC: 7180.27 ± 101.79 µM TE/100 g DM). Liquid Chromatography coupled with Mass Spectrometry (LC-MS) analysis revealed a diverse phytochemical profile rich in polyphenols, including gallic acid, p-coumaric acid, rutin, rosmarinic acid, caffeic acid, and epicatechin. Cellular assays in hydrogen peroxide (H₂O₂)-induced HaCaT keratinocytes demonstrated that C-4 extract significantly enhanced cell viability and upregulated endogenous antioxidant genes (superoxide dismutase (SOD1), catalase (CAT), glutathione peroxidase (GPX)), with effects comparable to established antioxidants such as epigallocatechin gallate (EGCG) and ascorbic acid. These findings highlight the influence of extraction parameters on phytochemical yield and biological activity, supporting the potential application of CE-derived S. terebinthifolius extracts as effective, sustainable ingredients for cosmeceutical formulations targeting oxidative stress-mediated skin aging. Full article

The continuous increase in microbial resistance to therapeutic agents has become one of the greatest challenges to global health. In this context, the present study investigated the bioactivity of 25 chroman-4-one and homoisoflavonoid derivatives—17 of which are novel—against pathogenic microorganisms, including Staphylococcus epidermidis, Pseudomonas aeruginosa, Salmonella enteritidis, Candida albicans, C. tropicalis, Nakaseomyces glabratus (formerly C. glabrata), Aspergillus flavus, and Penicillium citrinum. Antimicrobial assay was performed using the microdilution technique in 96-well microplates to determine the minimum inhibitory concentration (MIC). Thirteen compounds exhibited antimicrobial activity, with compounds 1, 2, and 21 demonstrating greater potency than the positive control, especially against Candida species. Molecular modeling suggested distinct mechanisms of action in Candida albicans: 1 potentially inhibits cysteine synthase, while 2 and 21 possibly target HOG1 kinase and FBA1, key proteins in fungal virulence and survival. Our findings indicated that the addition of alkyl or aryl carbon chains at the hydroxyl group at position 7 reduces antimicrobial activity, whereas the presence of methoxy substituents at the meta position of ring B in homoisoflavonoids enhances bioactivity. These findings highlight key structural features of these compound classes, which may aid in the development of new bioactive agents against pathogenic microorganisms. Full article

Hamamelis virginiana (witch hazel) is traditionally used in dermatology for its antibacterial and anti-inflammatory effects. However, the number of studies on its chemical composition and potentials in skin protection remains limited. This study aimed to investigate the qualitative and quantitative composition of polyphenolic compounds in the leaves and bark of the plant, as well as to explore their antioxidant, anti-inflammatory, and extracellular matrix (ECM)-protective activities in skin-relevant cell models. Human dermal fibroblasts and keratinocytes were exposed to oxidative and inflammatory stimuli and pretreated with leaf and bark extracts. ROS levels, antioxidant enzyme activity (SOD, GPx, CAT), pro-inflammatory cytokines (IL-6, IL-1β, TNF-α), and inhibition of collagenase, hyaluronidase, and elastase were assessed. Both extracts strongly reduced ROS levels, enhanced SOD activity, and significantly decreased pro-inflammatory cytokines. Bark extract also exhibited potent inhibitory activity against collagenase and elastase. UPLC-DAD-MS analysis revealed that both plant parts contained high levels of tannins; however, the leaf extract showed a more diverse composition, including more complex tannin forms and a significant amount of flavonoids from the quercetin and kaempferol class. In conclusion, H. virginiana leaf and bark extracts demonstrate multifunctional antioxidant and anti-inflammatory properties, supporting their potential use in cosmeceuticals and dermatological formulations targeting skin aging and inflammation. Full article