Anticancer Properties Research Articles

Phytochemical composition and anticancer effect of Akebia trifoliata seed in non-small cell lung cancer A549 cells

BackgroundAkebia trifoliata is a widely distributed medicine and food homology plant. Its fruit is used to treat tumors and the seed’s weight proportion exceeds 50%. However, the anti-tumor effect of A. trifoliata seed remains poorly studied. MethodsUHPLC-Q-Orbitrap-MS was used to identify the chemical components of A. trifoliata seed water extract (WE) and ethanolic extract (EE), and their cytotoxicity was evaluated using MTT assay. Further, colony formation and cell cycle assays examined the anti-proliferative effect of A. trifoliata seed EE. Next, morphology observation, AO/EB staining, Hoechst 33,258 staining, Annexin V-PE/7-AAD staining, and JC-1 assays were employed to detect apoptosis. The influence of A. trifoliata seed EE on A549 cell metastasis was assessed by wound healing and transwell invasion tests. In addition, western blotting and network pharmacology were applied to further analyze its anticancer mechanism. ResultsEighty-two components were characterized from the A. trifoliata seed WE and EE. For anticancer activity, A. trifoliata seed EE exhibited high cytotoxicity against cancer cells A549 (IC50: 52.38 ± 1.04 μg/mL) and NCI-H1299 (IC50: 70.29 ± 0.58 μg/mL) and revealed low cytotoxicity against non-cancer cells MRC-5 (IC50: 101.28 ± 2.84 μg/mL) and L929 (IC50: 113.44 ± 0.55 μg/mL). A. trifoliata seed EE suppressed A549 cell proliferation by inducing S-phase arrest via down-regulation of CDK2 and p21 as well as up-regulation of cyclin E1 and E2. It increased the Bax/Bcl-2 ratio, reduced mitochondrial membrane potential (ΔΨm), activated caspase-9 and caspase-3, cleaved PARP, and triggered apoptosis through the mitochondrial pathway. Besides, it repressed migratory and invasive ability by reducing MMP-2, MMP-9, and N-cadherin levels. ConclusionA. trifoliata seed EE exhibits outstanding anticancer properties and has the exploitation potential as an anticancer drug in the pharmaceutical industry.

Protective and Detoxifying Effects of Resveratrol on Zearalenone-Mediated Toxicity: A Review

Zearalenone (ZEA) is a mycotoxin produced by Fusarium spp. fungi and is widely found in moldy corn, wheat, barley, and other grains. ZEA is distributed to the whole body via blood circulation after metabolic transformation in animals. Through oxidative stress, immunosuppression, apoptosis, autophagy, and mitochondrial dysfunction, ZEA leads to hepatitis, neurodegenerative diseases, cancer, abortion, and stillbirth in female animals, and decreased sperm motility in male animals. In recent years, due to the influence of climate, storage facilities, and other factors, the problem of ZEA pollution in global food crops has become particularly prominent, resulting in serious problems for the animal husbandry and feed industries, and threatening human health. Resveratrol (RSV) is a natural product with therapeutic activities such as anti-inflammatory, antioxidant, and anticancer properties. RSV can alleviate ZEA-induced toxic effects by targeting signaling pathways such as NF-κB, Nrf2/Keap1, and PI3K/AKT/mTOR via attenuating oxidative damage, inflammatory response, and apoptosis, and regulating cellular autophagy. Therefore, this paper provides a review of the protective effect of RSV against ZEA-induced toxicity and its molecular mechanism, and discusses the safety and potential clinical applications of RSV in the search for natural mycotoxin detoxification agents.

Synergistic Proliferation Effects of Xanthohumol and Niflumic Acid on Merkel and Glioblastoma Cancer Cells: Role of Cell Membrane Interactions

The objective of our research was to determine the effects of xanthohumol (XN), a flavonoid isolated from hops (Humulus lupulus), and the anti-inflammatory drug niflumic acid (NA), separately and in combination with each other, on the proliferation of human cancer cells. Additionally, so as to understand the mechanism underlying the anticancer properties of the tested compounds, their effects on the biophysical parameters of a model membrane were assessed. The cells were incubated with XN and NA at various concentrations, either individually or in combination with each other. Cell proliferation was quantified using the sulforodamine B (SRB) assay. In addition, the IC50 values for niflumic acid and xanthohumol applied separately were determined by cell proliferation tests for the following human cancer cell lines: 5637 (urinary bladder carcinoma), A-431 (epidermoid carcinoma), UM-SCC-17A (head and neck squamous carcinoma), SK-MEL-3 (melanoma), MCC13 (Merkel cell cancer), and A172 (glioblastoma), in comparison with the mouse normal fibroblasts (BALB/3T3 clone A31). The results show that the two-compound combinations of XN and NA significantly decreased the proliferation of cancer cells in a dose-dependent manner, and the effects were stronger than the additive responses to XN and NA individually. The membrane studies revealed a synergistic effect on the membrane rigidity when using the mixture of XN and NA, which may explain the observed increase in anticancer activity for the combined XN and NA. Our results suggest that NSAIDs, such as niflumic acid, may be a promising strategy for co-application with xanthohumol as anticancer drugs.

Antioxidant Properties of Postbiotics: An Overview on the Analysis and Evaluation Methods.

Antioxidants found naturally in foods have a significant effect on preventing several human diseases. However, the use of synthetic antioxidants in studies has raised concerns about their potential link to liver disease and cancer. The findings show that postbiotics have the potential to act as a suitable alternative to chemical antioxidants in the food and pharmaceutical sectors. Postbiotics are bioactive compounds generated by probiotic bacteria as they ferment prebiotic fibers in the gut. These compounds can also be produced from a variety of substrates, including non-prebiotic carbohydrates such as starches and sugars, as well as proteins and organic acids, all of which probiotics utilize during the fermentation process. These are known for their antioxidant, antibacterial, anti-inflammatory, and anti-cancer properties that help improve human health. Various methodologies have been suggested to assess the antioxidant characteristics of postbiotics. While there are several techniques to evaluate the antioxidant properties of foods and their bioactive compounds, the absence of a convenient and uncomplicated method is remarkable. However, cell-based assays have become increasingly important as an intermediate method that bridges the gap between chemical experiments and in vivo research due to the limitations of in vitro and in vivo assays. This review highlights the necessity of transitioning towards more biologically relevant cell-based assays to effectively evaluate the antioxidant activity of postbiotics. These experiments are crucial for assessing the biological efficacy of dietary antioxidants. This review focuses on the latest applications of the Caco-2 cell line in the assessment of cellular antioxidant activity (CAA) and bioavailability. Understanding the impact of processing processes on the biological properties of postbiotic antioxidants can facilitate the development of new food and pharmaceutical products.

Resveratrol enhances sensitivity of renal cell carcinoma to tivozanib: An in-vitro study

BackgroundSince tivozanib has many side effects in the treatment of kidney cancer, we decided to use resveratrol as a bioactive molecule with anticancer and antioxidant properties to make tivozanib more effective and also reduce its side effects in kidney cancer cell line. MethodIn this in vitro study, we evaluated the effect of tivozanib, resveratrol and tivozanib- resveratrol combination therapy in ACHN cell line as representatives of human kidney cancer. The assessment includes Hoechst dye staining, scratch-wound assay, 3D spheroid, 2D colony formation assay, flow cytometric analysis of apoptosis and DNA cell cycle, real-time PCR (BAX/BCL2, E-cadherin, Snail, HIF1α, VEGFC and KLK3 genes). ResultTo determine IC50 levels, ACHN cells was exposed to different concentration of tivozanib and resveratrol. Our data indicated that IC50 values for tivozanib (0.5 μM) and resveratrol (30 μM) with MTT in a dose and time-dependent manner. Due to the efficacy of resveratrol in combination with tivozanib, we used 20 μM resveratrol, and 0.25 μM tivozanib instead of 30 μM and 0.25 μM respectively. This data was approved by flow cytometry for ACHN cell line with 38.39, 14.74 and 66.06 percent apoptosis and 8.25, 5.12 and 15.6 percent subG1 for tivozanib, resveratrol and tivozanib-resveratrol combination respectively which was as a consequence of cell cycle arrest at G1/S phase. The treatment also reduced cells’ migration, fragmented nuclei, 3D spheroid and colony formation potentials in analyses. Evaluation of gene expression presented that the effect of the tivozanib and resveratrol combination in ACHN cell lines is completely different during the evaluation of apoptosis genes, BAX, P53 genes and E-Cadherin had significantly increased expression compared to single treatment groups (P < 0.01). Meanwhile, a significant decrease was observed in the expression of VEGFC and HIF1α genes in the combination group compared to the monotherapy groups (P < 0.001). ConclusionConsidering that resveratrol can increase the apoptosis of cancer cells alone and in combination with tivozanib and prevent the proliferation of cancer cells and also reduce the side effects of tivozanib, we suggest that resveratrol as a potential bioactive molecule can be used in treatment of kidney cancer should be used in combination with tivozanib.

Flavonoid-Mediated Suppression of Tumor Angiogenesis: Roles of Ang-Tie/PI3K/AKT.

Angiogenesis is a process involved in the formation of new blood capillaries from pre-existing ones. It is regulated by several anti-angiogenic molecules involved in tumor growth and metastasis. The endothelial angiopoietin Ang-Tie/PI3K/AKT growth receptor pathway is necessary for healthy vascular development. The activation of AKT is controlled by a multistep process involving phosphoinositide 3-kinase (PI3K). This article aims to provide an overview of the role and mechanism of the Ang-Tie/PI3K/AKT signaling pathways and the potential of flavonoids as anti-angiogenic drugs. Flavonoids have shown great potential in preventing angiogenesis by targeting signaling pathways and exhibit additional anti-cancer properties. Research studies have revealed that the currently available anti-angiogenic drugs do not meet the safety and efficacy standards for treating tumor growth. Phytocompounds have long been a valuable resource for the development of novel therapeutic drugs. This article explores recent findings explaining the role and mechanism of the Ang-Tie/PI3K/AKT signaling pathways, as well as the interaction of flavonoids with angiogenic signaling pathways as a novel therapeutic approach. Several investigations have shown that synergistic studies of natural phytocompounds have great potential to target these pathways to inhibit tumor growth. Therefore, flavonoid-based medications may offer a more effective synergistic strategy to treat cancer.

Guar gum and carboxymethyl cellulose nanocomposite loaded with piperine: A multipurpose nanoparticle with potential antibacterial and anticancer properties

Guar gum-carboxymethyl cellulose derived piperine nanocomposite (GG-CMC@PIP) was synthesized to develop a phytochemical-based nanomaterial by following a simple synthetic procedure. In this study, piperine, an alkaloid prodrug was nanonized by entrapping within guar gum-carboxymethyl cellulose derived nanocomposite (GG-CMC). GG-CMC@PIPs were of (i) size (25 ± 3) nm by TEM, (ii) zeta potential (−) 33.1 ± 0.73 mV and (iii) entrapment efficiency 86 ± 0.46 %. High loading percentage of piperine in polymeric nanocomposites revealed excellent incorporation efficiency. In addition, pH responsive release behaviour of piperine from nanocomposites exhibited sustained but faster release pattern in pH 5.5. Minimal inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of piperine loaded nanocomposite on Gram positive Enterococcus faecalis and Gram-negative Escherichia coli, Pseudomonas aeruginosa were in the range of 200–400 μg/ml. IC50 value of GG-CMC@PIP was found to be around 500 μg/ml against C6 glioma cell line. Experimental outcome confirmed excessive accumulation of reactive oxygen species (ROS) mediated cytotoxicity, mitochondrial depolarization and higher degree of nuclear damage followed by increased mortality of C6 glioma cell after treatment with piperine-loaded nanocomposite.

Therapeutic Potential of Quercetin and their Compound Against Ovarian Cancer: New Approaches &amp; Application

Ovarian cancer is an exceptionally perilous form of cancer as it develops within the female reproductive system. Finding effective therapy platforms for ovarian cancer has been difficult because to the diverse array of molecular pathways and genetic alterations involved in its development. Therefore, it is imperative to discover novel therapeutic methodologies and advance their development. Medicinal herbs possess the capacity to independently or in combination with other pharmaceuticals, effectively treat malignancies such as ovarian cancer. Quercetin possesses remarkable anti-inflammatory and anti-cancer properties, making it one among numerous natural compounds with such qualities. Quercetin has demonstrated cytotoxicity against ovarian cancer cells in both laboratory experiments (in vitro) and live animal tests (in vivo). The potential anti-cancer effects of quercetin, particularly in relation to ovarian cancer, have not been extensively studied in human trials, despite encouraging findings from laboratory and animal experiments. Hence, it seems that quercetin could potentially be utilized in clinical trials as a therapeutic agent, either on its own or in conjunction with other chemotherapeutic drugs. This article will outline the primary aspects of quercetin's anti-cancer characteristics and thereafter concentrate on its application in the treatment of ovarian cancer.

Discovering the Untouched Perspective of Endangered North American Herb Actaea racemosa.

Actaea racemosa (AR), sometimes also known as black cohosh, is a perennial herb that grows in the Ranunculaceae family that effloresces in the middle of summer. This herb is currently present throughout south and west North America despite being endangered in the eastern section of the continent. Certain information about the photochemistry and biological potential of this herb is available. In accordance with the scant available ethno-medical reports, this herb possesses antioxidant, antidiabetic, anti-inflammatory, antiosteoporosis, and anticancer properties. As per the available literature, caffeic acid, isoferulic acid, actein, 23-epi-26 deoxycatein, cimicifugoside, and ferukinolic acid are the key components found in different parts of AR. To date, no thorough research or systematic review has been done to highlight the traditional, biological, and phytochemical benefits of this herb. Consequently, further research is needed to gain a deeper understanding of this therapeutic herb, particularly about its separation and pharmacological screening of its insulating portion for a range of biological functions. The goal of this review was to compile the most recent data on the phytochemical presence of AR. in relation to its ethnomedical applications, methods of extraction, pharmacological applications, and future potential.

Synthesis of new pyridine based ONNO type schiff bases and Cd(II) complexes, investigation of structural, electronic and anti-cancer properties as computationally and experimentally

Pyridine based Schiff bases and their Cd(II) complexes were synthesized and characterized by spectral techniques which are ATR-IR, 1H NMR, 13C NMR, LC/QTOF-MS, and Single Crystal XRD. Structural properties and geometric parameters of these compounds were investigated both experimental and computational analyses. Electronic properties of Schiff bases were investigated by Hirshfeld surface analyses and molecular electrostatic potential (MEP) map calculations. All experimentally obtained data were supported by computational chemistry methods. B3LYP/6–31G(d) level was used for synthesized Schiff bases while B3LYP/6–31G(d)(LANL2DZ) level was used for Cd(II) complexes. Cell viability assays were performed to determine anticancer properties of related compounds against breast adenocarcinoma (MCF-7), colorectal adenocarcinoma (HT-29), and gastric carcinoma (SNU-16) cell lines. It was found that anticancer activity increased with complexation. The synthesized molecules were found to be more effective against HT-29. Furthermore, molecular docking calculations for each compounds were done against histone deacetylase 1 (HDAC1) due to the fact that expression level of HDAC1 is acceptable range.

Rhoifolin Attenuates Concanavalin A-Induced Autoimmune Hepatitis in Mice via JAKs/STATs Mediated Immune and Apoptotic Processes.

Rhoifolin (ROF) exhibits a diverse range of biological activities, encompassing anticancer, hepatoprotective, antidiabetic, antirheumatic, and antiviral properties. However, the specific protective effects and possible mechanisms of the compound against T-cell-mediated autoimmune hepatitis have not been previously elucidated. In the present study, adult male mice were administered Con A (20 mg/kg, intravenously) for 8 h. In the treated groups, mice were pretreated with ROF daily (20 mg/kg and 40 mg/kg, orally) for 7 days before Con A intoxication. The results showed that ROF significantly decreased serum biochemical indices (ALT, AST, ALP, and LDH) and regulated related oxidative stress indicators (MDA, SOD, and GSH), reduced hepatic necrosis areas and immune cells infiltration, inhibited the release of various inflammatory factors (TNF-α, IFN-γ, IL-2, and IL-17), and improved hepatic tissue apoptosis, thereby alleviating hepatic damage induced by Con A. Additionally, we have also confirmed that ROF efficiently inhibited Th1/Th17 cells polarization via modulation of the JAK2/JAK3/STAT1/STAT3 signaling pathways both in vivo and in vitro. Moreover, the molecular mechanism examination also demonstrated that ROF regulated apoptotic cascade signaling through IL-6/JAK2/STAT1/STAT3 controlling BNIP3 activity in primary hepatocytes. These effects were in good agreement with the bioinformatics analysis of ROF treatment for AIH. In conclusion, our findings provide new insights into the potential use of ROF for AIH therapy, which may result from the specific regulation of the T cell subtype polarization and the apoptosis of liver cells via modulation of the JAKs/STATs signaling pathways.

Therapeutic overview of sudachitin.

Citrus fruits are extensively cultivated and eaten both raw and in refined forms. Citrus fruit peels are highly concentrated in polyphenolic substances. This makes them useful resources. Polymethoxyflavones (PMFs), found in citrus peels, belong to a specific subclass of flavonoids where most or all hydroxyl groups are methylated. PMFs have been documented to possess chemopreventive actions, anticancer, anti-inflammatory, and anti-atherosclerosis properties, as well as neuroprotective effects. Sudachitin, a PMF, is primarily found in Citrus sudachi. Japan's Tokushima prefecture is home to this famous fruit. In recent years, there has been a growing interest among researchers in exploring the potential health benefits of sudachitin, spurred by its presence in traditional diets and its association with various positive health outcomes. Studies conducted over the past decade have revealed promising effects of sudachitin in multiple health conditions, including cancer, skin disorders, inflammatory conditions, diabetes, obesity, and neurodegenerative disorders. Although these promising results exist, there is still a need for thorough preclinical and clinical research to confirm sudachitin's effectiveness in treating chronic conditions. This review seeks to summarize animal and cell studies exploring sudachitin's pharmacological properties and the potential molecular pathways underlying its therapeutic effects. Through this, we aim to clarify the clinical potential of sudachitin across various disorders, paving the way for future research and the development of sudachitin-based therapies.

Vanillin and Its Derivatives: A Critical Review of Their Anti-Inflammatory, Anti-Infective, Wound-Healing, Neuroprotective, and Anti-Cancer Health-Promoting Benefits

Inflammation and thrombosis are implicated in several non-communicable chronic disorders, including cardiovascular diseases, diabetes, renal and neurodegenerative disorders, skin diseases, and especially in cancer. Natural bioactives and especially phytochemicals like phenolic compounds have been proposed to reduce the inflammatory burden with several health benefits against these disorders. Vanillin is a phenolic compound found in the seeds of various species of vanilla plants. It has been known since ancient times for its aromatic and soothing properties; however, recent outcomes have outlined several other pleiotropic actions for this phenolic bioactive compound. Within this article, the potent anti-inflammatory activities of vanillin and its derivatives are thoroughly reviewed, with emphasis on their anti-cancer, anti-infective, wound-healing, and neuroprotective health-promoting properties. The mechanisms of their action(s), along with recent outcomes from in vitro and in vivo studies and clinical trials, on the benefits of these vanillin-based phenolic bioactives against each of these disorders, and especially against specific types of cancer, are also outlined. Limitations and future perspectives of their use solely as bioactive ingredients, as ingredients in several functional products—such as functional foods, supplements, nutraceuticals, or even cosmetics and drugs—and even as adjuvant therapies are also discussed.

3-Deazaneplanocin A (DZNep): A Drug That Deserves a Second Look.

The emerging data compiled during the past five years on 3-deazaneplanocin (DZNep) provide compelling evidence to reevaluate this drug as a better alternative over the specific catalytic inhibitors of histone methyl transferases (HTMs). The indirect mechanism of DZNep via inhibition of AdoHcy-ase, once considered a liability due to possible side effects, has now shown to be rather beneficial as additional pathways targeted by DZNep are important contributors to its superior anticancer properties. Furthermore, DZNep has demonstrated the ability to induce proteasomal degradation of its target and reduce toxicity in combination with well-established antitumor therapies in animal models. In addition, DZNep has shown important effects in suppressing fibrosis and inflammation in liver, kidney, peritoneum, and airways. Finally, inhibition of mRNA m6A methylation by DZNep suppresses the synthesis of the viral genome in SARS-Cov-2 infection and promises to have important therapeutic value when combined with its potent antiviral efficacy and anti-inflammatory effects.

Synthesis, DFT, ADMET, and Docking studies of Novel Sulfonyl Piperidine Analogues containing 2,3-Dihydrobenzofuran-5-Carboxamide.

The development of effective anti-cancer medicines with low side effects is imperative as cancer continues to be a leading cause of death globally. By obstructing the survival and growth of cancer cells, small-molecule medications have made tremendous progress in the field of cancer research. Several bioactive heterocyclic compounds, including derivatives of piperidine and 2,3-dihydrobenzofuran, have shown great promise and are found in various anti-cancer medications. Cancer growth and metastasis are hindered by these small molecule inhibitors, which interfere with vital signals that drive cancer cell proliferation. This study focuses on the synthesis and evaluation of novel Sulfonyl Piperidine Analogues containing 2,3-Dihydrobenzofuran-5-Carboxamide as potential anti-- cancer agents. The synthesized compounds were characterized using spectroscopic techniques such as 1H NMR and ESI-MS. Protein-drug interaction studies, DFT analysis, and target prediction techniques were employed. The anti-cancer properties of the compounds were evaluated in vitro against MCF-7 cell lines. Compounds 5 and 7 were specifically investigated for their growth-inhibitory effects on MCF7 breast cancer cells. Compounds5 and 7 demonstrated strong binding affinity towards both mutated BRCA1 (PDB ID: 1N5O) and BRCA2 (PDB ID:8BR9). Furthermore, they displayed notable efficacy against MCF-7 cell lines. Synthesized compounds displayed activity against MCF-7 cell lines, supporting findings from in-silico predictions. Further investigations are warranted to elucidate the mechanisms of action of these selected molecules against MCF-7 cell types.

Timosaponin AIII Disrupts Cell-Extracellular Matrix Interactions through the Inhibition of Endocytic Pathways.

Timosaponin AIII (TAIII), a steroidal saponin isolated from the root of Anemarrhena asphodeloides Bunge, exhibits various pharmacological activities, including anti-cancer properties. TAIII inhibits the migration and invasion of various cancer cell types. However, the mechanism underlying how TAIII regulates the motility of cancer cells remains incompletely understood. In this study, we demonstrate that TAIII disrupted cell-extracellular matrix (ECM) interactions by inhibiting internalization of cell surface proteins, such as integrins. We found that TAIII inhibited cell adhesion on various ECMs. Structure-activity relationship analysis demonstrated that TAIII exhibited unique activity among the saponins from Anemarrhena asphodeloides Bunge and that the number and position of saccharide moieties were important for TAIII to exert its activity. Time lapse imaging revealed that TAIII also suppressed cell spreading on the ECM, membrane ruffling, and lamellipodia formation. Furthermore, we examined integrin β1 behaviors in response to TAIII treatment and found that TAIII blocked its internalization. These findings contribute to delineating the potential molecular mechanisms by which TAIII exerts anti-metastatic activity.

Characterization, biological activity and photodegradation efficacy of synthesized tryptophan capped silver nanoparticles

Tryptophan capped Silver nanoparticles (AgNPs) were synthesized through a sonochemical method, utilizing tryptophan as a biocompatible and non-toxic capping agent. Based on UV–visible spectra, the optical band gap of the nanoparticles was found to be roughly 3.01 eV. The TEM and XRD measurements of the particle sizes showed a range of 10–22 nm. Under sun irradiation, these nanoparticles showed notable photocatalytic activity, destroying Methylene Blue (MB) dye by more than 79.4 %. With a pseudo-first-order apparent rate constant of 1.5×10−2min-1, the degradation kinetics were observed. The photocatalysis of MB dye was investigated using liquid chromatography in conjunction with electrospray ionization time-of-flight mass spectrometry (LC-ESI-TOF-MS) to determine the products generated and to clarify the degradation processes. Additionally, the antibacterial, anticancer potential showed thate the nanoparticles exhibited good antibacterial and notable anticancer properties. Furthermore, the antidiabetic activity was investigated through α-glucosidase inhibition, demonstrating a significant inhibition rate of 53.98 %. Antioxidant capabilities were also tested using ABTS and DPPH assays, revealing antioxidant activities of 73.9 % and 52.04 %, respectively. Overall, the synthesized tryptophan-capped AgNPs show promising applications in environmental remediation, as well as potential therapeutic uses.

Revealing the molecular mechanism of baohuoside I for the treatment of breast cancer based on network pharmacology and molecular docking

Ethnopharmacological relevanceIn Traditional Chinese Medicine (TCM), there are many prescriptions for treating breast cancer (BC) that utilize the herb Epimedium brevicornum Maxim, which warms and replenishes kidney yang. Baohuoside I (BI) is a flavonoid compound found in Epimedium brevicornum Maxim. As a single glycoside, it is not easily hydrolyzed in the intestine and is typically absorbed as a precursor. As a natural product with potential anti-cancer properties, studies have shown that BI possesses anti-cancer activity and can inhibit the invasion and migration of BC cells. However, its underlying mechanisms remain unclear, thus further research is needed to validate its modern mechanisms for traditional uses. Aim of the studyThis study aimed to explore the regulatory mechanism of BI in the signaling pathways of BC cells through network pharmacology (NP), molecular docking (MD) techniques and cellular experiments. MethodsPotential targets were predicted using public databases, and a protein-protein interaction (PPI) network was constructed. Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) enrichment analyses were performed. Key signaling pathways were validated through MD techniques, cellular experiments, RNA interference and Western blot (WB) analysis. ResultsTreatment-associated targets included SRC, MAPK1, HSP90AA1, PIK3CA, TP53, AKT1, and EGFR. GO enrichment, KEGG enrichment analyses, and MD results indicated that BI exerts its anti-breast cancer effects by inhibiting the tyrosine kinase activity of EGFR, as well as through downstream MAPK signaling pathway and PI3K-Akt signaling pathway pathways. In vitro experiments confirmed that BI primarily induce cell apoptosis through the EGFR-mediated MAPK signaling pathway and PI3K-Akt signaling pathway. ConclusionBI can inhibit EGFR activation and promote BC cell apoptosis through the MAPK signaling pathway and PI3K-Akt signaling pathway, thereby exerting therapeutic effects on BC. This study not only provides experimental evidence for the accuracy of NP but also offers an effective approach for rational utilization of Baohuoside I-like flavonoid compounds as anti-breast cancer drugs.

Development of quercetin loaded biosynthesized chitosan grafted iron oxide nanoformulation and their antioxidant, antibacterial, and anti-cancer properties

In this study, we report the development and characterization of a novel nanoformulation composed of quercetin-loaded biosynthesized chitosan-grafted iron oxide nanoparticles (CH-Fe3O4 NCs). The synthesis of chitosan-grafted iron oxide nanoparticles was achieved through a green synthesis approach, utilizing chitosan derived from crustacean shells and biosynthesized iron oxide nanoparticles. Quercetin, a natural flavonoid with known antibacterial, anti-cancer, and antioxidant properties, was loaded onto the nanoparticles through physical adsorption. The optical property, crystal structure, morphology, chemical composition and surface charge were thoroughly characterized using various analytical techniques including UV–visible spectroscopy, X-ray diffractometer, scanning and transmission electron microscopy, fourier-transform infrared spectroscopy and zeta potential analyzer. The antibacterial activity of the nanoformulation was evaluated against a panel of bacterial strains using standard microbiological assays, revealing promising inhibitory effects against both Gram-positive and Gram-negative bacteria. The antibacterial activity of CH-Fe3O4 NCs was evaluated against E. coli and S. aureus bacterial species. CH-Fe3O4 NCs have a greater ability to inhibit the E.coli than S. aureus. Furthermore, the CH-Fe3O4 NCs demonstrated dose-dependent cytotoxicity and caused apoptotic cell death in the H522 cell line. Additionally, the antioxidant properties of the nanoformulation were evaluated through scavenging assays, highlighting its ability to effectively neutralize free radicals. Overall, our results suggest that the quercetin-loaded biosynthesized chitosan-grafted iron oxide nanoformulation exhibits potent antibacterial, anti-cancer, and antioxidant properties, making it a promising candidate for further development as a multifunctional therapeutic agent.

Green synthesis of silver nanoparticles from mulberry leaf through hot melt extrusion: Enhanced antioxidant, antibacterial, anti-inflammatory, antidiabetic, and anticancer properties

Green synthesis of silver nanoparticles from mulberry leaf through hot melt extrusion: Enhanced antioxidant, antibacterial, anti-inflammatory, antidiabetic, and anticancer properties