Search Results (313)

Background/Objectives: Humulus lupulus (hops) are a perennial, dioecious plant widely cultivated for beer production, used for their distinguishing aroma and bitterness—traits that confer high added value status. Various hop-derived compounds have been reported to exhibit antioxidant, antimicrobial, antiproliferative and other bioactive effects. This systematic review and meta-analysis assesses the impact of hop compounds on the viability of diverse cancer cell lines. Methods: A comprehensive literature search was performed following PRISMA guidelines. Data were synthesized via multivariate meta-analysis and meta-regression, using IC₅₀ values as the effect size. Key variables included assay type (SRB, tetrazolium salt-based, crystal violet), exposure duration (24, 48, 72 h), specific hop compound and cancer cell line. Results: Of 622 articles identified, 61 met eligibility criteria, yielding 354 individual experiments. Meta-regression of xanthohumol (XN) IC₅₀ values across SRB, tetrazolium and crystal violet assays revealed no statistically significant differences at 24 h (p = 0.77), 48 h (p = 0.35) and 72 h (p = 0.70), supporting the interchangeability of the methods. Meta-analysis confirmed that hop constituents inhibit cancer cell proliferation; XN emerged as the most potent flavonoid (IC₅₀ = 16.89 μM at 72 h), while lupulone was the strongest compound overall (IC₅₀ = 5.00 μM at 72 h). Crude hop extracts demonstrated greater antiproliferative selectivity for cancer versus non-cancer cells (IC₅₀ = 35.23 vs. 43.80 μg/mL at 72 h). Conclusions: Hop compounds, and particularly bitter acids, demonstrate promising antiproliferative activity against cancer cells with comparatively low toxicity to healthy cells. Furthermore, our analysis confirms the comparability of SRB, tetrazolium-based and crystal violet assays, supporting the robust integration of antiproliferative data. Full article

Plants of the Annona genus have garnered increasing scientific interest due to their rich phytochemical profile and broad spectrum of biological activities, which include antimicrobial, antiproliferative, and cytotoxic effects. Among the most studied compounds are acetogenins and Annonacins, which exhibit potent bioactivity and have been identified as key agents in the green synthesis and stabilization of nanomaterials. In recent years, the integration of Annona plant extracts—particularly from leaves—into nanotechnology platforms has opened new avenues in the development of eco-friendly and biocompatible nanostructures for biomedical applications. This review provides a comprehensive overview of the current knowledge regarding the antimicrobial properties of nanomaterials synthesized using extracts from Annona species. This review encompasses 74 indexed articles published between 2012 and 2023, focusing on the synthesis of nanomaterials using extracts from this genus that exhibit antimicrobial and biomedical properties. The search was conducted in databases such as Google Scholar, Web of Science, and Scopus. Emphasis is placed on their antibacterial, antifungal, and anthelmintic effects, as well as additional therapeutic potentials, such as antidiabetic, antihypertensive, antiproliferative, and cytotoxic activities. The analysis of the recent literature highlights how Annona-derived phytochemicals contribute significantly to the functionalization and enhanced biological performance of these nanomaterials. This work aims to support future research focused on the rational design of Annona-based nanostructures as promising candidates in antimicrobial and therapeutic strategies. Full article

Marine algae offer environmentally friendly platforms for green nanoparticle synthesis. This study reports the biosynthesis of silver nanoparticles using polysaccharides isolated from the brown alga Chnoospora minima (PAgNPs) and evaluates their therapeutic potential. Fourier Transform Infrared Spectroscopy (FTIR) confirmed algal polysaccharide functional groups. Dynamic Light Scattering (DLS), Scanning Electron Microscopy (SEM), and Energy Dispersive X-ray (EDX) analysis characterized the nanoparticles as spherical (~84 nm average size), stable (zeta potential −18.5 mV), and containing elemental silver without nitrogen. The PAgNPs exhibited potent antioxidant activity (~100% DPPH scavenging) and significant antimicrobial efficacy, particularly against Staphylococcus aureus and Candida species. Crucially, PAgNPs displayed potent antiproliferative activity against human lung cancer cells (A549, IC₅₀: 13.59 µg/mL). In contrast, toxicity to normal Vero cells was significantly lower (IC₅₀: 300.2 µg/mL), demonstrating notable cancer cell selectivity (SI 22.1). Moderate activity was observed against MCF-7 breast cancer cells (IC₅₀: 100.7 µg/mL). These results demonstrate that C. minima polysaccharide facilitates the synthesis of biocompatible AgNPs with promising antimicrobial and selective anticancer capabilities, highlighting their potential for further development as nanotherapeutics. Full article

To date, various species of Erigeron genus have been used both in the ethnopharmacology of numerous nations across the world and in contemporary herbal practices. The objective of this study is to revise the phytochemical data on the essential oils (EOs) of various fleabanes species and to evaluate the variability of their biological activities. Up to June 2025, this review provides an updated overview of 105 literature sources (published during last 25 years) related to 14 Erigeron sp. (native, naturalized, or invasive) which have been investigated extensively and are of the greatest significance. It summarizes the compositional variability of the EOs and their pharmacological and toxic effects, such as anti-inflammatory, anticancer, antiproliferative, skin regeneration, antioxidant, antifungal, antibacterial, insecticidal, larvicidal, repellent, and allelopathic activity. The EOs of each Erigeron species were characterized, and a chemical structure of 43 major constituents is presented herein. The most characteristic and prevalent compounds were found to be limonene, δ-3-carene, matricaria ester, lachnophyllum ester, germacrene D, β-caryophyllene, β-farnesene, α-bergamotene, allo-aromadendrene, etc., in the EOs from the E. acris, E. annuus, E. bonariensis, E. canadensis, E. floribundus E. mucronatus, and E. speciosus plants. Major constituents, such as borneol, bornyl acetate, modhephen-8-β-ol, cis-arteannuic alcohol, β-caryophyllene, and τ-cadinol, were found in the oils of E. graveolens (Inula graveolens). A paucity of data concerning E. incanus EOs was revealed, with the prevalence of 3-hydroxy-4-methoxy cinammic acid and thymol acetate noted in the oils. The EOs from E. multiradiatus and E. sublyratus were comprised mainly of matricaria and lachnophyllum esters. The available data on EOs of E. ramosus is limited, but the main constituents are known to be α-humulene, 1,8-cineole, eugenol, and globulol. The EOs containing appreciable amounts of matricaria and lachnophyllum esters exhibited strong anticancer, anti-inflammatory, antimicrobial, larvicidal, and repellent activities. Repellence is also related to borneol, bornyl acetate, caryophyllene derivatives, τ-cadinol, modhephen-8-β-ol, and cis-arteannuic alcohol. Cytotoxicity was determined due to the presence of limonene, δ-3-carene, α- and β-farnesene, (E)-β-ocimene, ledene oxide, sesquiphellandrene, and dendrolasin in the fleabanes EOs. Skin regeneration and antifungal properties were related to germacrene D; and anti-inflammatory effects were determined due to high amounts of limonene (E)-β-ocimene, lachnophyllum ester, and germacrene D. The antimicrobial properties of the oils were conditioned by appreciable quantities of limonene, β-pinene, 1,8-cineole, carvacrol, thymol acetae, β-eudesmol, 2,6,7,7α-tetrahydro-1,5-dimethyl-1H-indene-3-carboxaldehyde, caryophyllene and its oxide, allo-aromadendrene, α-humulene, farnesene, carvacrol, and eugenol. This review provides a foundation for further studies on volatile secondary metabolites to explore the potential sources of new biologically active compounds in Erigeron sp. Full article

Olive oil and its derivatives, particularly polyphenol-rich extracts, are valued for their antioxidant, anti-inflammatory, and regenerative properties. Olive mill wastewater (OMWW), a byproduct of olive oil production, traditionally seen as an environmental pollutant, has emerged as a promising source of high-value dermatological ingredients. Key polyphenols such as hydroxytyrosol, oleuropein, and tyrosol exhibit potent antioxidant, anti-inflammatory, antimicrobial, and photoprotective effects. These compounds mitigate oxidative stress, prevent collagen degradation, modulate NF-κB and MAPK signaling, and promote cellular repair and regeneration. Skin health is increasingly recognized as crucial to overall well-being, driving interest in cosmeceuticals that combine cosmetic benefits with dermatological activity. This review examines the cosmeceutical and dermatological potential of OMWW, highlighting its incorporation into innovative topical formulations like oil-in-water nanoemulsions, liposomes, and microneedles that enhance skin penetration and bioavailability. Additionally, OMWW fractions have shown selective antiproliferative effects on melanoma cells, suggesting potential for skin cancer prevention. Valorization of OMWW through biorefinery processes aligns with circular-economy principles, converting agro-industrial waste into sustainable cosmeceutical ingredients. This approach not only meets consumer demand for natural, effective products, but also reduces the ecological footprint of olive oil production, offering a scalable, eco-friendly strategy for next-generation dermatological applications. Full article

Background/Objectives: Agave amica (Medik.) Thiede & Govaerts (Asparagaceae family) is an ornamental bulbous species, widely used for its fragrance but less studied as a medicinal species. This study is aimed at assessing the phenolic profile and selected biological properties of ethanolic extracts obtained from the aerial parts and bulbs of A. amica cultivated in Romania. Methods: The phenolic composition was characterized by spectrophotometric methods and LC/MS analysis. The antioxidant activity was evaluated by DPPH (2,2-diphenyl-1-picrylhydrazyl radical scavenging capacity) and FRAP (Ferric reducing antioxidant power) tests, while the in vitro antimicrobial capacity was investigated by the agar-well diffusion, the broth microdilution, and the antibiofilm assays. Cytotoxicity was tested on a colorectal adenocarcinoma cell line (DLD-1) by a CCK-8 assay. Results: Both ethanolic extracts showed important polyphenol content and caffeic acid as their main compound. Significantly higher amounts of total polyphenols (44.25 ± 1.08 mg/g), tannins (12.55 ± 0.34 mg/g), flavonoids (9.20 ± 0.19 mg/g), caffeic acid derivatives (19.95 ± 0.05 mg/g), and also antioxidant activity (IC₅₀ = 0.82 ± 0.02 mg/mL, and 79.75 ± 1.80 µM TE/g, respectively) were found for the aerial parts extract compared to the bulbs one (p < 0.001). Notable anti-Candida albicans activity and moderate efficacy against Listeria monocytogenes and Staphylococcus aureus were displayed by both extracts against planktonic cells and biofilm. A dose-dependent cytotoxicity towards the colorectal adenocarcinoma cell line was recorded as well. Conclusions: This study brings novelty to the scientific literature by characterizing the phenolic profile and in vitro antimicrobial, antibiofilm, antioxidant, and antiproliferative activities of the ethanolic extracts obtained from A. amica, thus highlighting this herbal species’s medicinal potential. Full article

Centaurea calcitrapa is a well-known plant with antioxidant, anti-proliferative, and antimicrobial properties. The plant contains various phenolic compounds, flavonoids, and other bioactive molecules contributing to its medicinal properties. However, little is known about its antidiabetic activity. The study's purpose is the isolation and identification of active compounds of C. calcitrapa aerial parts in diabetic rats induced by streptozotocin. The ethyl acetate extract (E2) was separated into eight subfractions by column chromatography. The subfractions were evaluated for their antidiabetic activity using diabetic-induced rats. The most active subtraction was purified, and the active compounds were identified using UV spectrophotometry, Fourier Transform Infrared Spectroscopy, Mass spectrophotometry, and HPLC. Subfraction E2-VIII showed the most effective reduction in blood glucose levels, comparable to metformin. In HPLC analysis, subfraction E2-VIII showed three main compounds: nepetin, kaempferide, and Luteolin. The nepetin flavonoid was examined using molecular docking, and it showed a high affinity to α-amylase. In conclusion, the aerial parts of C. calcitrapa extract and isolated compounds especially nepetin present promising antidiabetic agents this is probably mediated by its strong antioxidants and α-amylase inhibitory effect. Full article

Dodonaea viscosa (Sapindaceae), a Hawaiian local medicinal plant, has been traditionally used to treat rashes and skin diseases. The study aimed to discover and characterize bioactive compounds from D. viscosa flowers extract with antimicrobial and antitumor properties. Thirteen compounds were isolated from the methanol extract of D. viscosa flowers, and their structures were characterized using spectroscopy data, comparing their NMR spectroscopic profiles with previously reported data. Subsequent antibacterial assays revealed that one particular compound, 12, exhibited significant antimicrobial activity against Gram-positive bacteria. Notably, it demonstrated a minimum inhibitory concentration (MIC) of 2 μg/mL, indicating its potent antibacterial potential. In addition to antimicrobial properties, the isolated compounds demonstrated dose-dependent antiproliferative effects in breast cancer cell lines. Notably, inflammatory breast cancer (IBC) cell lines, a highly aggressive subtype, were more sensitive to compound 6, with IC₅₀ values of 4.22 μM (BCX-010), 6.74 μM (SUM190), and 7.73 (SUM149), compared to non-IBC cell line. These findings highlight the dual antibacterial and anticancer potential of compounds from D. viscosa, emphasizing their promise as candidates for therapeutic development. Full article

The synthesis and antimicrobial and anticancer activity of 3,3′-((3-hydroxyphenyl)azanediyl)dipropionic acid derivatives (2–25) against drug-resistant bacterial pathogens and FaDu head and neck cancer cells were investigated. The derivatives were synthesized through various methods, including esterification, hydrazinolysis, and condensation reactions. The compounds demonstrated structure-dependent antimicrobial activity, predominantly targeting Gram-positive pathogens. Compounds containing 4-nitrophenyl, 1-naphthyl, and 5-nitro-2-thienyl groups exhibited enhanced activity against S. aureus and E. faecalis. Additionally, compounds 5, 6, and 25 showed antiproliferative activity in cisplatin-resistant FaDu cells at low micromolar concentrations. The in silico modeling revealed that compound 25 interacts with the HER-2 and c-MET proteins. These compounds also induced significant oxidative stress in FaDu cells and demonstrated low cytotoxic activity in non-cancerous HEK293 cells. These results highlight the potential of N-aryl-substituted β-amino acid derivatives as promising scaffolds for the further development of novel amino acid-based antimicrobial and anticancer agents targeting drug-resistant pathogens and cancers. Full article

Extensive use of classical antibiotics has led to the growing emergence of many resistant strains of pathogenic bacteria. To combat this challenge, researchers have turned to the antimicrobial peptides (AMPs). Aurein 1.2 (GLFDIIKKIAESF-NH2) was demonstrated to have broad spectrum bi-functionality against bacterial and cancer cells. The Solid Phase Peptide Synthesis (Fmoc-strategy) was used for the synthesis of new analogs of aurein 1.2. The purity of all compounds was monitored by HPLC, and their structures were proven using mass spectrometry. Cytotoxicity and antiproliferative effects were studied using 3T3 NRU and MTT tests, respectively. The antibacterial activity was estimated against Gram-positive and Gram-negative bacteria using broth microdilution method in concentrations from 0 to 320 µg/mL to determine the minimal inhibitory concentration (MIC) and minimal bactericidal concentration (MBC). The antiproliferative activity test shows that the peptide analog EH [Orn]⁸ has the highest activity (IC₅₀ = 44 ± 38 μM) for the three cell lines studied (MCF-12F, MCF-7, and MDA-MB-231). The same compound exhibited good antimicrobial activity. The obtained results reveal that replacement of Lys with non-proteinogenic amino acids can increase both the potency and activity spectra of natural template peptides, making them suitable candidates for new drug development. Full article

Essential oils (EOs) of three native species Baccharis uncinella, B. retusa and B. calvescens, obtained through hydrodistillation, were analyzed by GC-MS and GC-FID for seasonality, and the antimicrobial and anti-proliferative activities were evaluated. EO of B. calvescens and B. uncinella consisted mainly of oxygenated sesquiterpenes, while in the EO of B. retusa, monoterpene hydrocarbons were predominant. The highest antimicrobial activity was observed for spring B. uncinella EO against S. aureus, C. albicans and summer B. uncinella EO against C. albicans and B. subtilis. Essential oils of B. calvescens showed more effective anti-proliferative activity than B. retusa EO and B. uncinella EO. This is the first study of the EO of B. retusa, and it was demonstrated that the majority composition was different in all seasons of the year, justifying the importance of the seasonal study. Furthermore, the summer and spring EO showed potent cytostatic effects against the K562 and OVCAR-03 cell lines, respectively. For each species, PCA differentiated the EO chemical composition seasonally. PCA of all samples distinguished the three species. This study underscores the importance of assessing seasonal variation in the chemical composition and biological activities of essential oils, highlighting the potential of compounds spathulenol, caryophyllene oxide, limonene and α-pinene for achieving the desired product properties. Full article

Coordination compounds, characterized by the coordination of metal ions with ligands, represent a pivotal area of research in chemistry due to their diverse structures and versatile applications. This review delves into the synthesis, characterization, biological evaluation, and practical applications of these compounds. A variety of synthetic methodologies (traditional solution-based techniques) are discussed to highlight advancements in the field. Investigations into the structural, electronic, and spectral properties of coordination compounds are emphasized to provide insights into their functional attributes. The biological evaluation section focuses on their roles in antimicrobial, anticancer, and enzyme-inhibitory activities, underscoring their potential in therapeutic development. Attention is paid to nanoparticles, which are increasingly used for the treatment of oncological diseases. The metal complexes have been shown to have antibacterial, antifungal, antiviral, antioxidant, and antiproliferative properties. Additionally, the review explores their applications across domains such as catalysis, illustrating their multifaceted utility. By synthesizing recent findings and trends, this article aims to bridge the gap between fundamental chemistry and applied sciences, paving the way for innovative uses of coordination compounds in both biological and industrial contexts. Full article

In recent years, the incidence of acute and chronic inflammatory diseases has increased significantly worldwide, intensifying the search for new therapeutic agents, especially anti-inflammatory drugs. Therefore, the aim of this work was to synthesize, biologically assess, and explore the structure–activity relationships of new compounds containing the cyclohex-1-ene-1-carboxylic acid moiety. Six new derivatives, 2a–2f, were synthesized through the reaction of amidrazones 1a–1f with 3,4,5,6-tetrahydrophthalic anhydride. Their toxicity was evaluated in cultures of human peripheral blood mononuclear cells (PBMCs). Additionally, their antiproliferative properties and effects on the synthesis of TNF-α, IL-6, IL-10, and IL-1β were assessed in mitogen-stimulated PBMCs. The antimicrobial activity of derivatives 2a–2f was determined by measuring the minimal inhibitory concentration (MIC) values against five bacterial strains—Staphylococcus aureus, Mycobacterium smegmatis, Escherichia coli, Yersinia enterocolitica, and Klebsiella pneumoniae—and the fungal strain Candida albicans. All compounds demonstrated antiproliferative activity, with derivatives 2a, 2d, and 2f at a concentration of 100 µg/mL being more effective than ibuprofen. Compound 2f strongly inhibited the secretion of TNF-α by approximately 66–81% at all studied doses (10, 50, and 100 µg/mL). Derivative 2b significantly reduced the release of cytokines, including TNF-α, IL-6, and IL-10, at a high dose (by approximately 92–99%). Compound 2c exhibited bacteriostatic activity against S. aureus and M. smegmatis, while derivative 2b selectively inhibited the growth of Y. enterocolitica (MIC = 64 µg/mL). Some structure–activity relationships were established for the studied compounds. Full article

Bergamot [Citrus × limon (L.) Osbeck, syn. C. × bergamia (Risso) Risso & Poit.] is primarily cultivated in the Calabria region of Italy and exploited in the food and perfumery industry. The epicarp of its fruit is a rich source of essential oil (BEO) containing mainly monoterpenes, which are known for their diverse biological activities, including antimicrobial, anti-inflammatory, antiproliferative, and neuromodulatory effects. Emerging evidence suggests that oxidative stress plays a central role in the pathogenesis of neurodegenerative diseases, particularly Alzheimer’s disease (AD), where it contributes to neuronal dysfunction and cell death. Moreover, heavy metal exposure has been identified as a key environmental factor exacerbating oxidative stress and neurodegeneration in AD. This study aimed to explore whether BEO could mitigate heavy metal (Cd²⁺, Hg²⁺, and Pb²⁺)-induced neurotoxicity in SH-SY5Y cells, a model system for brain cells. MTT and calcein-AM assays were performed to examine the viability of the SH-SY5Y cells after exposure to each heavy metal itself, or in combination with BEO, whereas the LDH assay was carried out to determine the effects of BEO towards necrotic cell death induced by heavy metals. Furthermore, DCFH-DA was performed to determine whether BEO could protect SH-SY5Y from heavy metal-induced oxidative stress. This study also investigated the antibacterial properties of BEO on different Gram-positive and Gram-negative bacterial strains belonging to the ATCC collection. These results suggest that BEO may help counteract heavy metal-induced neuronal damage, particularly Cd²⁺ toxicity, potentially reducing one of the environmental risk factors associated with AD. Additionally, its antimicrobial properties reinforce its relevance in preventing infections that may contribute to neuroinflammation in AD. Full article

Background/Objectives: With growing antimicrobial resistance, the overuse of antibiotics, and stagnation in the discovery of new antibiotics, a novel alternative is required to overcome hard-to-treat infections. Antimicrobial peptides (AMPs) show great potential as a possible alternative to standard chemotherapeutics. Temporins are a group of AMPs that have been under the spotlight in numerous studies. Herein, we report the design and synthesis of Temporin A modified in position 1, where the proteinogenic amino acid Phe is replaced by Tyr or fluorinated Phe. In addition, in other analogues, in position 10, the Ser residue is replaced by Tyr or Thr. The aim of all modifications in the primary structure of the native Temporin A is to study the influence of the changes made on the antibacterial properties, antiproliferative activity, and hydrolytic stability of the newly synthesized molecules. Methods: The Fmoc/OBu^t SPPS strategy was employed for the synthesis of the novel-designed analogues. The antibacterial activity was evaluated with both disk diffusion and broth microdilution methods. The BALB 3T3 NRU test and MTT dye reduction assay were used to determine safety and antiproliferative activity. Results: The investigated analogues have low toxicity and are photosafe. The greatest selectivity was shown by DTTyr10 towards MCF-7 cells. DT4F, containing fluorinated Phe in position 1, was the most effective antibacterial agent among the new compounds. The incorporation of Thr in position 10, in comparison with the natural Ser residue, led to an increase in the antiproliferative effect of the new peptide. Conclusions: The obtained structure–activity relationship data show that the most promising compound in the tested series is FLPLIGRVL-Y-GILNH₂, where the Ser residue in position 10 is replaced by a more hydrophobic OH-containing Tyr residue. The analogue containing fluorinated Phe in position 1, DT4F, has the highest antiproliferative effect against both tested tumor cell lines, combined with good antibacterial properties at the lowest MIC (80 µg/mL), but it is more cyto- and phototoxic than the parent DTA molecule and is not stable at pH 9 for a 24 h period. Full article