Cu2+@CuSeO3 nanoparticles with antibiofilm and anticancer activities

BackgroundEichhornia crassipes (Mart) solms is an invasive macrophyte causing serious problems to the network of irrigation and drainage canals in the Nile Delta region. The present study aim to evaluate the potential anticancer and antioxidant activities of Eichhornia crassipes crude extract and its pure compounds.MethodsThe macrophyte was collected from El-Zomor canal, River Nile (Egypt), cleaned, air dried, grinded then extracted with methanol (crude extract). The extract was fractionated using pre-coated silica gel plates (TLC F254) with hexane/ethyl acetate (8.5: 1.5 v/v) as mobile phase. Nine fractions were separated (A-I) then scratched, eluted with the same mobile phase, filtered and the separated fractions were determined and identified using spectroscopic methods (Mass spectrum (MS), Infra red (IR) and Proton H-Nuclear magnetic resonance (H-NMR). Both the crude extract and its nine identified compounds were tested for their antioxidant (using 2, 2 diphenyl-1-picrylhydrazyl (DPPH), 2, 2′- azino-bis {ethylbenzthiazoline-6-sulfonic acid (ABTS.)} methods) and anticancer activity (using MCF-7, HeLa, Hep.G2 and EACC cell lines).ResultsThe antioxidant and anticancer activities of the crude extract exhibited the highest effect while the compounds showed variable effects which depend on the type of compound and cancer cell line. The antioxidant activity of the crude extract exhibited the highest followed in descending order by compounds D, E, G and H respectively. Concerning the anticancer potency, the crude extract showed also the highest effect while the identified compounds (A, B, C, D, E, F, G, H and I) showed variable anticancer activities against the four different cell lines. In addition, Compound I exhibited the most potent anticancer activity against HepG2 cell line while compound D exhibited high anticancer activity against HeLa cells and EACC. The results revealed the presence of different compounds (Alkaloids and terpenoids) with variable antioxidant and anticancer activities which elicited an auto-augmentation in the crude extract leading to its greatest activities. The action of the identified anticancer compounds on DNA fragmentation was studied.ConclusionThe study illustrated the potential of Eichhornia as a valuable resource for natural compounds of desirable medicinal properties (e.g. antioxidants and anticancer).

BackgroundAntibiotic resistances of pathogens and breast cancer warrant the search for new alternative strategies. Phytoextracts can eradicate microbe-borne diseases as well as cancer with lower side effects compared to conventional antibiotics.AimUnripe and ripe Azadirachta indica (neem) seed extracts were explored as potential antibiofilm and anticancer agents in combating multidrug-resistant infectious bacteria as well as anticancer agents against the MDR breast cancer cell lines.Methods Shed-dried neem seeds (both unripe and ripe) were pulverized and extracted using methanol. The chemical components were identified with FTIR and gas chromatography - mass spectrometry. Antibiofilm activity of neem seed extracts were assessed in terms of minimum biofilm inhibitory concentration (MBIC), minimum biofilm eradication concentration (MBEC), and fluorescence microscopic studies on Staphylococcus aureus and Vibrio cholerae. Bacterial cells were studied by fluorescence microscopy using acridine orange/ethidium bromide as the staining agents. Minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) values were evaluated to observe the antibacterial activities. Cytotoxicity of the extracts against human blood lymphocytes and the anticancer activity against drug-resistant breast cancer cell lines were assessed by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay and fluorescence-activated cell sorting (FACS) studies.Results 4-Ethyl-2-hydroxy-2-cyclopentene-1-one, phthalic acid, and 2-hexyl-tetrahydro thiophane were the major compounds in unripe neem seed, whereas 3,5-dihydroxy-6-methyl-2,3-dihydro-4-H-pyran-4-one and 4-ethylbenzamide were predominant in ripe neem seed. Triazine derivatives were also common for both the extracts. MBIC values of unripe and ripe neem seed extracts for S. aureus are 75 and 100 µg/mL, respectively, and for V. cholerae, they are 100 and 300 µg/mL, respectively. MBEC values of unripe and ripe seed extracts are 500 and 300 µg/mL, respectively for S. aureus and for V. cholerae the values are 700 and 500 µg/mL, respectively. Fluorescence microscopic studies at 16 and 24 h, after bacterial culture, demonstrate enhanced antibiofilm activity for the ripe seed extract than that of the unripe seeds for both the bacteria. MTT assay reveals lower cytotoxicity of both the extracts towards normal blood lymphocytes, and anticancer activity against breast cancer cell line (MDA-MB-231) with superior activity of ripe seed extract. FACS studies further supported higher anticancer activity for ripe seed extract.ConclusionsMethanolic extract of neem seeds could substantially inhibit and eradicate biofilm along with their potent antibacterial and anticancer activities. Both the extracts showed higher antibiofilm and antibacterial activity against S. aureus (gram-positive) than V. cholerae (gram-negative). Moreover, ripe seed extract showed higher antibiofilm and anticancer activity than unripe extracts.Graphical

Background: Ficus benjamina L., commonly known as the weeping fig, is a plant traditionally used for various medicinal purposes, particularly in Southeast Asia. Despite its widespread use, there is a scarcity of scientific data validating its therapeutic properties, especially its anti-inflammatory and anticancer potentials. Objective: This study aimed to investigate the phytochemical profile of Ficus benjamina L. and to evaluate its anticancer and anti-inflammatory activities to provide a scientific basis for its traditional uses. Methods: The plant materials were collected and subjected to extraction using methanol and dichloromethane. The extracts were analyzed for primary and secondary metabolites. The anticancer activity was tested using the MTT assay on HeLa cells, and anti-inflammatory activity was assessed using a luminol-enhanced chemiluminescence method. Data analysis was conducted using IBM SPSS Statistics Version 25, focusing on inferential statistics to compare the bioactivity of the extracts against standard drugs. Results: Phytochemical analysis confirmed the presence of proteins, lipids, carbohydrates, alkaloids, flavonoids, and tannins. The dichloromethane extract showed significant anti-inflammatory activity with 58.6% inhibition at a concentration of 50 µg/ml and an IC50 of 8.966±1.03. The methanol extract exhibited minimal anticancer activity with an 8.3% inhibition rate at 30 µg/ml, suggesting low efficacy against HeLa cells compared to the standard drug, Doxorubicin, which showed a 101.2% inhibition. Conclusion: The study confirms that Ficus benjamina L. contains bioactive compounds with potential anti-inflammatory benefits and limited anticancer activity. These findings support the traditional use of the plant in treating inflammatory conditions and highlight the need for further research to optimize extraction techniques and expand biological testing.

The serine/threonine kinase B-Raf is the second most frequently occurring human oncogene after Ras. Mutations of B-Raf occur with the highest incidences in melanoma, and the most common mutant, V600E, renders B-Raf constitutively active. The sodium proton exchanger isoform 1 (NHE1) is a ubiquitously expressed plasma membrane protein responsible for regulating intracellular pH, cell volume, cell migration, and proliferation. A screen of protein kinases that bind to NHE1 revealed that B-Raf bound to the cytosolic regulatory tail of NHE1. Immunoprecipitation of NHE1 from HeLa and HEK cells confirmed the association of B-Raf with NHE1 in vivo. The expressed and purified C-terminal 182 amino acids of the NHE1 protein were also shown to associate with B-Raf protein in vitro. Because treatment with the kinase inhibitor sorafenib decreased NHE1 activity in HeLa and HEK cells, we examined the role of B-Raf in regulating NHE1 in malignant melanoma cells. Melanoma cells with the B-Raf(V600E) mutation demonstrated increased resting intracellular pH that was dependent on elevated NHE1 activity. NHE1 activity after an acute acid load was also elevated in these cell lines. Moreover, inhibition of B-Raf activity by either sorafenib, PLX4720, or siRNA reduction of B-Raf levels abolished ERK phosphorylation and decreased NHE1 activity. These results demonstrate that B-Raf associates with and stimulates NHE1 activity and that B-Raf(V600E) also increases NHE1 activity that raises intracellular pH.

Ultrasmall nanoparticles (diameter 2 nm) of silver, platinum, and bimetallic nanoparticles (molar ratio of Ag:Pt 0:100; 20:80; 50:50; 70:30; 100:0), stabilized by the thiolated ligand glutathione, were prepared and characterized by transmission electron microscopy, differential centrifugal sedimentation, X-ray photoelectron spectroscopy, small-angle X-ray scattering, X-ray powder diffraction, and NMR spectroscopy in aqueous dispersion. Gold nanoparticles of the same size were prepared as control. The particles were fluorescently labeled by conjugation of the dye AlexaFluor-647 via copper-catalyzed azide-alkyne cycloaddition after converting amine groups of glutathione into azide groups. All nanoparticles were well taken up by HeLa cells. The cytotoxicity was assessed with an MTT test on HeLa cells and minimal inhibitory concentration (MIC) tests on the bacteria Escherichia coli and Staphylococcus xylosus. Notably, bimetallic AgPt nanoparticles had a higher cytotoxicity against cells and bacteria than monometallic silver nanoparticles or a physical mixture of silver and platinum nanoparticles. However, the measured release of silver ions from monometallic and bimetallic silver nanoparticles in water was very low despite the ultrasmall size and the associated high specific surface area. This is probably due to the surface protection by a dense layer of thiolated ligand glutathione. Thus, the enhanced cytotoxicity of bimetallic AgPt nanoparticles is caused by the biological environment in cell culture media, together with a polarization of silver by platinum.

The prevalent life-threatening microbial and cancer diseases and lack of effective pharmaceutical therapies created the need for new molecules with antimicrobial and anticancer potential. Bee venom (BV) was collected from honeybee workers, and melittin (NM) was extracted from BV and analyzed by urea-polyacrylamide gel electrophoresis (urea-PAGE). The isolated melittin was hydrolyzed with alcalase into new bioactive peptides and evaluated for their antimicrobial and anticancer activity. Gel filtration chromatography fractionated melittin hydrolysate (HM) into three significant fractions (F1, F2, and F3), that were characterized by electrospray ionization mass spectrometry (ESI-MS) and evaluated for their antimicrobial, anti-biofilm, antitumor, and anti-migration activities. All the tested peptides showed antimicrobial and anti-biofilm activities against Gram-positive and Gram-negative bacteria. Melittin and its fractions significantly inhibited the proliferation of two types of cancer cells (Huh-7 and HCT 116). Yet, melittin and its fractions did not affect the viability of normal human lung Wi-38 cells. The IC50 and selectivity index data evidenced the superiority of melittin peptide fractions over intact melittin. Melittin enzymatic hydrolysate is a promising novel product with high potential as an antibacterial and anticancer agent.

Quercetin and gallic acid mediated synthesis of bimetallic (silver and selenium) nanoparticles and their antitumor and antimicrobial potential

BackgroundThe anticancer and immunomodulatory activity of mung bean sprouts (MBS) and the underlying mechanisms against human cervical and hepatocarcinoma cancer cells were explored.MethodsMBS cytotoxicity and MBS-induced anticancer cytokines, TNF-α and IFN-β from cancer cells, and immunological cytokines, IL-4, IFN-γ, and IL-10 from peripheral mononuclear cells (PMNC) were assessed by MTS and ELISA assays. Apoptotic cells were investigated by flow cytometry. The expression level of apoptotic genes (Bax, BCL-2, Capsases 7–9) and cell cycle regulatory genes (cyclin D, E, and A) and tumor suppressor proteins (p27, p21, and p53) was assessed by real-time qPCR in the cancer cells treated with extract IC50.ResultsThe cytotoxicity on normal human cells was significantly different from HeLa and HepG2 cells, 163.97 ± 5.73, 13.3 ± 0.89, and 14.04 ± 1.5 mg/ml, respectively. The selectivity index (SI) was 12.44 ± 0.83 for HeLa and 11.94 ± 1.2 for HepG2 cells. Increased levels of TNF-α and IFN-β were observed in the treated HeLa and HepG2 culture supernatants when compared with untreated cells. MBS extract was shown to be an immunopolarizing agent by inducing IFNγ and inhibiting IL-4 production by PBMC; this leads to triggering of CMI and cellular cytotoxicity. The extract induced apoptosis, in a dose and time dependent manner, in treated HeLa and HepG2, but not in untreated, cells (P < 0.05). The treatment significantly induced cell cycle arrest in G0/G1 in HeLa cells. The percentage of cells in G0/G1 phase of the treated HeLa cells increased from 62.87 ± 2.1%, in untreated cells, to 80.48 ± 2.97%. Interestingly, MBS IC50 induced the expression of apoptosis and tumor suppressor related genes in both HeLa and HepG2 cells. MBS extract succeeded in inducing cdk-inhibitors, p21, p53, and p27 in HeLa cells while it induced only p53 in HepG2 cells (P < 0.05). This is a clue for the cell type- specific interaction of the studied extract. These proteins inhibit the cyclin-cdk complexes apart from the presence of some other components that might stimulate some cyclins such as cyclin E, A, and D.ConclusionMBS extract was shown to be a potent anticancer agent granting new prospects of anticancer therapy using natural products.

In vitro medicinal potentials of Bryum capillare, a moss sample, from Turkey.

Background Cervical cancer is the third most prevalent cancer globally, with high incidence and mortality rates. Current treatments often result in severe side effects and drug resistance. While Solanecio mannii ( S. mannii ) roots have been traditionally used in cancer treatment, there is a lack of scientific validation of their anticancer potential. Therefore, the present study sought to analyze the metabolomics profile of the extracts and evaluate its anticancer and pro-apoptotic potential. Methods S. mannii roots were collected, freeze-dried, and extracted using diethyl-ether: methanol ( v:v ) for total extraction, and hexane and ethyl acetate for fractionation. This study analyzed the metabolomic profiles of S. mannii root extracts using gas chromatography coupled to mass spectrometry and evaluated their selective cytotoxic effect on human cervical cancer cell lines, specifically Henrietta Lacks (HeLa) cell lines. Moreover, this study investigated the extracts’ potential to modulate autophagy and induce apoptosis. The pro-apoptotic effect of S. mannii was evaluated by analyzing chromatin morphological changes, the expression of Bcl-2 homologous antagonist/killer (BAK) and BCL2-Associated X (BAX) genes, and the activity of caspases. Results S. mannii exhibited selective anticancer and anti-proliferative activities against HeLa cells, with IC 50 values of 113 ± 0.28 µg/mL for the total extract, 38.94 ± 0.87 µg/mL for the hexane fraction, and 12.16 ± 0.52 µg/mL for the ethyl acetate fraction. Additionally, S. mannii root extracts modulated autophagosome formation and autophagy-related genes. Furthermore, extracts exhibited an intrinsic pro-apoptotic potential by upregulating BAK and BAX and increasing the activity of caspase-9, −3, and −7 in a time- and dose-dependent manner. These effects are attributed to the bioactive phytocompounds identified in the extracts, including syringic acid, 4-coumaric acid, caffeic acid, vanillin, hydroquinone, oleic acid, beta-sitosterol, and stearic acid, among others. Conclusion This study showed the selective anticancer and pro-apoptotic activity of S. mannii root for the management of cervical cancer.

Piperine (1-piperoylpeperdine), a nitrogenous pungent substance, is present in the fruits of black pepper (Piper nigrum Linn.) and long pepper (Piper longum Linn.). It possesses several pharmacological properties and has been extensively explored for its anti-cancerous activities. The mechanism underlying its anti-cancer potential in human cervical adenocarcinoma (HeLa) cells is not well interpreted. The anti-proliferative effect and the mode of action of piperine were investigated through some potent markers of apoptosis viz.reactive oxygen species (ROS) generation, cellular apoptosis and loss of mitochondrial membrane potential (MMP). DNA fragmentation, cell cycle kinetics, caspase-3 activity and cell migration assays were also conducted to observe the efficacy of piperine against HeLa cells. The results showed that piperine exposure induces apoptosis significantly in a dose-dependent manner and inhibits the growth of HeLa cells with an increase in ROS generation, nuclear condensation and delayed wound healing. In addition, piperine also encourages cell death by the loss of MMP, DNA fragmentation and the activation of caspase-3. Growth inhibition of HeLa cells was found to be associated with G2/M phase arrest and sub-G1 accumulation. The present study provides useful insight into the apoptotic potential of piperine and further in vivo and clinical studies will be needed for its validation and in the finding of more effective and least toxic regimens against cervical cancer.

Nanomedicine has emerged as a revolutionary regimen for moderating communicable as well as non-communicable diseases. This study demonstrated the phytosynthesis of silver nanoparticles using M. citrifolia leaf extract (MC-AgNPs) and their in vitro antioxidant, antibacterial and anticancer potential. The Biosynthesis of MC-AgNPs was studied by spectroscopy and characterized by SEM, TEM, XRD and FTIR analysis. The antibacterial activity was checked by minimum inhibition concentration assay. The HeLa and MCF-7 cancer cell lines were used to explore the cytotoxicity and genotoxicity activity of biogenic MC-AgNPs. The free radical scavenging potential of MC-AgNPs was studied by in vitro DPPH and ABTS assays, which confirmed significant radical scavenging activity in a dose-dependent manner with IC50 of 17.70 ± 0.36 μg/mL for DPPH and 13.37 ± 3.15 μg/mL for ABTS radicals. The bactericidal effects of MC-AgNPs confirmed by MIC showed 0.1 mg/mL concentration of MC-AgNPs with greater sensitivity for E.coli (93.33 ± 0.89), followed by K. pneumoniae (90.99 ± 0.57), S. aureus (87.26 ± 2.80) and P. aeruginosa strains (44.68 ± 0.73). The cytotoxicity results depicted strong dose and timedependent toxicity of biogenic MC-AgNPs against cancer cell lines fifty percent inhibitory concentration MC-AgNPs against HeLa cells were 13.56 ± 1.22 μg/mL after 24h and 5.57 ± 0.12 μg/mL after 48 h exposure, likewise 16.86 ± 0.88 μg/mL and 11.60 ± 0.97 μg/mL respectively for MCF-7 cells. The present study revealed the green synthesis of silver nanoparticles using M. citrifolia and their significant antioxidant, antibacterial and anticancer activities.

One of the recent and actively researched areas is the synthesis of bimetallic nanoparticles (BMNPs). Silver and gold BMNPs are prepared from aqueous AgNO3 and HAuCL4 as the precursors using the as prepared culture filtrate of Rhodopseudomonas faecalis as a reducing agent in aqueous medium. An ambient temperature of 25°C is maintained throughout the process, where the AgNO3 and HAuCL4 solution in 1:1 v/v is stirred continuously and culture filtrate is added. The synthesis of gold and silver nanoparticles is shown by the brown color which indicates the formation of composite nanoparticles. The characterization is done using different kinds of techniques. Synthesized nanoparticles size is in the range between 31.71 and 153.7 nm. Scanning electron microscopy (SEM) analysis shows that the nanoparticles are in small and round in shape. The anticancer and antimicrobial activities of the BMNPs are investigated. Anticancer activity of composite nanoparticles reveals that the composite nanoparticles show more cytotoxicity toward cancer cell lines HT‐29 and MCF‐7. The synthesized composite nanoparticles can be used as efficient antimicrobials and anticancer agents for diagnosis, treatment of various infections, and cancers.

Cervical and breast cancers are two of the most common cancer affecting women. In Indonesia, there are 65,858 cases of breast cancer and 36,633 cases of cervical cancer have been recorded. Chemotherapy, using agents such as cisplatin and doxorubicin, is one of the main cancer therapies and works by targeting cancer cells. However, this therapy lacks selectivity and damages normal cells, leading to adverse side effects. An alternative chemopreventive treatment is Myricetin, a compound predicted to potentially target VEGF, a critical factor in angiogenesis, making it a promising anticancer agent. This study aims to evaluate the safety of Myricetin on Vero cells (normal cells), assess its anticancer activity on T47D and HeLa cells, and predict its mechanism of action. The anticancer activity was evaluated using the Microculture Tetrazolium Technique (MTT) assay on HeLa, T47D, and Vero cells. VEGF receptors were identified through a Network Pharmacology approach. The study also involved the Molecular Docking of Myricetin, cisplatin, and doxorubicin compounds with the 5DXH receptor. The results showed that Myricetin exhibited high cytotoxic activity against HeLa and T47D cells, with IC50 values of 22.70 μg/mL and 51.43 μg/mL, respectively, while demonstrating significantly lower cytotoxicity against Vero cells, with a CC50 value of 1445.2 μg/mL. In comparison, the CC50 values for cisplatin and doxorubicin against Vero cells were 6.53 μg/mL and 13.76 μg/mL, respectively, indicating that Myricetin is considerably less toxic to normal cells. Myricetin's Selectivity Index (SI) was 63.64 for HeLa cells and 28.09 for T47D cells, demonstrating superior selectivity compared to cisplatin and doxorubicin. These findings suggest that Myricetin has promising anticancer potential with a better safety profile than conventional chemotherapeutic agents.

Anticancer activity in HeLa and MCF-7 cells via apoptopic cell death by a sterol molecule Cholesta-4,6-dien-3-ol (EK-7), from the marine ascidian Eudistoma kaverium