Anticancer Applications Research Articles

Quantitative Characterization of the Effect of Biogenic silver-based Nanoparticles on Breast Cancer Cells by High Content Analysis

Background: Among the various types of cancer, breast cancer is the most incident among women. Due to the resistance to antitumor treatments, alternative treatments have been sought, such as metallic nanoparticles. Objective: This study aimed to evaluate the antitumor potential and cytotoxicity induction mechanisms of green synthesized AgCl-NPs and Ag/AgCl-NPs. Methods: The antitumor potential of nanoparticles was evaluated in breast cancer BT-474 and MDAMB- 436 cell lines treated with 0-40 μg/mL AgCl-NPs or 0-12.5 μg/mL Ag/AgCl-NPs through imagebased high content analysis method. Normal human retinal pigment epithelial 1 (RPE-1) cells were used for comparison. Results: The growth rate of the RPE-1 cells treated with nanoparticles was insignificantly affected, and no significant changes in cell viability were observed. In these cells, the nanoparticle treatments did not induce lysosomal damage, changes in ROS production, or reduction in the mitochondrial membrane potential. The level of BT-474 and MDA-MB-436 cell proliferation was markedly decreased, and cell viability was reduced by 64.19 and 46.19% after treatment with AgCl-NPs and reduced by 98.36 and 82.29% after treatment with Ag/AgCl-NPs. The cells also showed a significant increase in ROS production and loss of mitochondrial membrane potential, which culminated in an increase in the percentage of apoptotic cells. BT-474 cells also presented lysosomal damage when treated with the highest concentrations of both nanoparticle types and actin polymerization was observed after exposure to Ag/AgCl-NPs. Conclusions: Together, the results showed overall cytotoxic effects of both AgCl-NPs and Ag/AgCl- NPs towards breast cancer cells with negligible effects against healthy cells, which suggests their promising anticancer and biomedical applications.

Multifunctional metabolites of Streptomyces kunmingensis BS19 from bamboo rhizosphere soil.

A pigmented bioactive molecule from Streptomyces kunmingensis BS19 was isolated, characterized, and evaluated for anti-infective, antiproliferative, and wound-healing properties. The yellow-red pigment produced from the strain BS19 showed promising activity against methicillin-resistant Staphylococcus aureus (MRSA) and Mycobacterium tuberculosis. Extracellular bioactive pigment from the strain BS19 was produced by agar surface fermentation and purified through bioassay guided preparative HPLC-based purification. Based on the results of UV, FT-IR, GC-MS, 1H NMR, and 13C NMR spectral analyses, the purified pigment was identified as a chromopeptide class of molecule with phenoxazinone chromophore. Its molecular weight was determined as the chemical formula C64H90N12O16 and molecular weight 1283g/mol. It exhibited promising antimicrobial activity against Staphylococcus aureus (ATCC 1720) and antiproliferative activity against 14 types of human cancer cell lines. It showed good in vivo wound-healing activity in the rat model. The present study explored Streptomyces kunmingensis as a newly added source for the isolation of chromopeptide antibiotics for antimicrobial, wound-healing, and anticancer applications.

Synthesis and characterization of WO3-GO nanocomposite for hydrogen storage, electrochemical, antibacterial and anticancer applications

Tungsten trioxide nanoparticles (WO3 NPs), Graphene oxide nanosheets (GO NSs), and WO3-GO (50 mg and 100 mg) nanocomposites (NCs) were successfully synthesized by using precipitation, modified Hummer's and ultrasonication methods, respectively. Various characterization techniques were used to confirm the formation of individual and composite materials. Hydrogen storage, electrochemical, antibacterial and anticancer properties of the synthesized materials were studied. Formation of the composite was confirmed by XRD, Raman and XPS analyses. Surface area and pore size distribution of WO3 NPs and WO3-GO NC were studied by using BET analysis. Hydrogen storage capacity of WO3-GO 50 mg and WO3-GO100 mg NCs was found to be 1.05 and 2.08 wt%, respectively. XRD, Raman, elemental and TG analyses were used to examine the adsorption and desorption of hydrogen. WO3-GO NCs showed higher specific capacitance as compared to WO3 NPs. Antibacterial activity against E. coli, S. aureus bacteria and anticancer effect against human breast cancer cells of WO3 NPs and WO3-GO NC were examined. Based on the studies, it is evident that the inclusion of GO enhanced the hydrogen storage, specific capacitance, antibacterial and anticancer activities of the composite.

ZIF-8 nanocarriers synthesized by co-encapsulating resveratrol and cellulase for biomedical applications

Drug conjugation with enzymes is one of the innovative antibacterial nanocarriers used as a delivery system for cancer therapy. Zeolitic imidazolate framework-8 (ZIF-8) was synthesized, dual encapsulated with cellulase (CL) enzyme, and resveratrol (Resv) drug formed ZIF-8@CL&Resv. Cellulase and resveratrol hydrophobic nature have bound them together and imparted a negative charge on the ZIF-8, resulting in the decrease of zeta potential from 22.7 mV (ZIF-8) to 3.82 mV (ZIF-8@CL&Resv). The cellulase like a scaffold regulated the pH-responsive release of resveratrol enhancing its bioavailability. Molecular docking studies provided evidence of the major interaction between the biofilm-related proteins with cellulase and resveratrol. The encapsulated cellulase showed high enzymatic activity and possibly exhibited antibacterial effects by dissolving the biofilm and exposing bacteria to resveratrol action. Resveratrol released sustainably exhibited significant antioxidant and antibacterial activity against selected bacterial species. ZIF-8@CL&Resv exhibited high biocompatibility and had a potent cytotoxic effect against triple-negative breast cancer cells MDA MB 231 with an IC50-value of 17.18 μg/mL compared to ZIF-8 control with 90.47 μg/mL. ZIF-8@CL&Resv treatment led to 61.81 % cell death, apoptosis induction, increased ROS generation, and decreased mitochondrial membrane potential. Overall, data demonstrated that ZIF-8@CL&Resv is a novel drug release system and a potential catalytic nanoparticle for antimicrobial and anticancer applications.

The apoptotic and anti-proliferative effects of Neosetophomone B in T-cell acute lymphoblastic leukaemia via PI3K/AKT/mTOR pathway inhibition.

The phosphatidylinositol 3-kinase/Protein Kinase B/mammalian target of rapamycin (PI3K/AKT/mTOR) signalling pathway is pivotal in various cancers, including T-cell acute lymphoblastic leukaemia (T-ALL), a particularly aggressive type of leukaemia. This study investigates the effects of Neosetophomone B (NSP-B), a meroterpenoid fungal metabolite, on T-ALL cell lines, focusing on its anti-cancer mechanisms and therapeutic potential. NSP-B significantly inhibited the proliferation of T-ALL cells by inducing G0/G1 cell cycle arrest and promoting caspase-dependent apoptosis. Additionally, NSP-B led to the dephosphorylation and subsequent inactivation of the PI3K/AKT/mTOR signalling pathway, a critical pathway in cell survival and growth. Molecular docking studies revealed a strong binding affinity of NSP-B to the active site of AKT, primarily involving key residues crucial for its activity. Interestingly, NSP-B treatment also induced apoptosis and significantly reduced proliferation in phytohemagglutinin-activated primary human CD3+ T cells, accompanied by a G0/G1 cell cycle arrest. Importantly, NSP-B did not affect normal primary T cells, indicating a degree of selectivity in its action, targeting only T-ALL cells and activated T cells. In conclusion, our findings highlight the potential of NSP-B as a novel therapeutic agent for T-ALL, specifically targeting the aberrantly activated PI3K/AKT/mTOR pathway and being selective in action. These results provide a strong basis for further investigation into NSP-B's anti-cancer properties and potential application in T-ALL clinical therapies.

Au@hydroxyapatite nanocomposite as a novel apoptosis Inducer and NF-κB translocation Inhibitor in prostate cancer cell line

In the current study, we used an environmentally friendly method called pulsed laser irradiation for the preparation of AuNPs and hydroxyapatite NPs alone and as a composite nanomaterials. The optical, morphology, and chemical bonding possessions of prepared AuNPs, hydroxyapatite NPs, and Au-hydroxyapatite composites were studied using different techniques like Transmission Electron Microscopy (TEM), Ultraviolet–visible Spectram (UV–VIS), and Fourier transform infrared spectroscopy (FTIR). The anticancer activity of prepared Au NPs, hydroxyapatite NPs, and Au-hydroxyapatite composites against prostate cancer cell line (PC-3 cells) was evaluated by MTT assay as well the possible mechanisms underlying the induction of apoptosis. The consequences suggest that the nanoparticles can act against an antiproliferative agent against PC-3 cells-induced apoptosis by activating caspase-8 and reducing the NF-κB translocation pathway. The current study demonstrates the potential role of an Au-hydroxyapatite composite for anticancer applications via the activation of the apoptosis pathway through extrinsic and intrinsic pathways.

Sonodynamic Cancer Therapy by Mn(I)-tricarbonyl Complexes via Ultrasound-triggered CO Release and ROS Generation.

A novel ferrocene conjugated Mn(I)-tricarbonyl complex viz [Mn(Fc-tpy)(CO)3Br] (Mn2) where, Fc-tpy=4'-ferrocenyl-2,2':6',2''-terpyridine was synthesized and fully characterized along with its non-ferrocene analog [Mn(Ph-tpy)(CO)3Br] Ph-tpy=4'-phenyl-2,2':6',2''-terpyridine (Mn1) for ultrasound (US) activated anticancer applications. The X-ray structure of Mn2 confirmed its distorted octahedral geometry. Mn1 and Mn2, for the first time, showed US-triggered release of CO and ROS generation (1O2 and ⋅OH) in an aqueous solution from any Mn(I)-tricarbonyl complexes, indicating its potential for synergetic CO gas therapy and sonodynamic therapy. The above-mentioned in-solution chemistry was successfully translated into in vitro cellular models. These complexes showed unprecedented US-triggered toxicity against T-cell lymphoma and human breast cancer cells (IC50 for Mn2<1 μM) while were minimally toxic without US or against normal spleen and human embryonic kidney cells. Mn2 was ca. 12 fold more anticancer active than Mn1, indicating that the ferrocene conjugation augmented the US sensitivity. The apoptotic sonotoxicity of Mn2 was due to US-promoted mitochondrial depolarization via ROS generation and CO release. The apoptosis was triggered by caspase 3 activation. This is the first report of Mn(I)-tricarbonyl-based sonosensitizers for cancer SDT. Overall, this study, for the first time, establishes the effectiveness of 3d metal carbonyls in SDT.

Bio-inspired synthesis of ZnO nanoparticles using Taraxacum officinale for antibacterial, antifungal, and anticancer applications

A green synthesis method was developed to fabricate ZnO nanomaterials using Taraxacum officinale (Dandelion) leaf extract as a reducing agent and zinc sulfate heptahydrate as a precursor. Characterization by XRD, EDAX, FTIR, FESEM, and UV–vis spectroscopy confirmed the successful formation of ZnO nanocrystals with enhanced crystallinity following annealing. The ZnO nanomaterials exhibited significant bioactivity, demonstrating 85 % antibacterial efficiency against Escherichia coli and Staphylococcus aureus, along with 70 % antifungal activity. Furthermore, the nanomaterials showed promising anticancer effects, achieving a 60 % reduction in human cancer cell viability. This eco-friendly approach minimizes the use of toxic chemicals typically involved in nanoparticle synthesis, providing a sustainable alternative for producing functional oxide nanoparticles. The use of plant-based reducing agents not only makes the process safer and more biocompatible but also enhances the potential for biomedical applications. ZnO nanomaterials produced through this method offer great promise for antimicrobial therapies and cancer treatment. This efficient, green synthesis method can be further scaled for various applications, highlighting its relevance in fields such as nanomedicine, where bioactivity and eco-friendly synthesis are essential.

Blazing Carbon Dots: Unfolding its Luminescence Mechanism to Photoinduced Biomedical Applications.

Carbon dots (CDs) are carbon-based nanomaterials that have garnered immense interest due to their exceptional photophysical and optoelectronic properties. They have been employed extensively for biomedical imaging and phototherapy due to their superb water dispersibility, low toxicity, outstanding biocompatibility, and exceptional tissue permeability. This review summarizes the luminescence mechanism of CDs. The modification in CDs via various doping routes is comprehensively reviewed, and the effect of such alterations on their photophysical properties, such as photoluminescence (PL), absorbance, and reactive oxygen species generation ability, is also highlighted. This review also aims to summarize the role of CDs in cellular imaging and fluorescence lifetime imaging for cellular metabolism. Subsequently, recent advancements and the future prospects of CDs as nanotheranostic agents have been discussed. Herein, we have discussed the role of CDs in photothermal, photodynamic, and synergistic therapy of anticancer, antiviral, and antibacterial applications. The overall summary of the review highlights the future prospects of CD-based research in bioimaging and biomedicine.

Germacrone: A Multi-targeting Sesquiterpene with Promising Anti-cancer and Chronic Disease Applications.

Germacrone, a naturally occurring active compound found in essential oils extracted from medicinal plants within the Zingiberaceae family, has garnered attention for its potential therapeutic applications. Extensive research has highlighted its multi-targeting capabilities, positioning it as a promising treatment for various chronic diseases, including cancer, cardiovascular conditions, and neurodegenerative disorders like Alzheimer's disease. This review aims to provide a comprehensive overview of germacrone as a scaffold for developing multi-targeting drugs with therapeutic potential against a range of chronic disorders. The study delves into the molecular mechanisms that underlie the therapeutic effects of germacrone and explores its potential targets, including NF-κB, PI3K/AKT/mTOR, p53, JAK/STAT, caspase, apoptosis, and autophagy induction. A systematic review of literature databases was conducted to gather relevant studies on germacrone and its therapeutic applications. The molecular mechanisms and potential targets of germacrone were examined to elucidate its multi-targeting capabilities. Germacrone exhibits significant potential in the management of chronic diseases, with demonstrated effects on various cellular pathways. The review highlights its impact on NF-κB, PI3K/AKT/mTOR, p53, JAK/STAT, caspase, apoptosis, and autophagy induction, showcasing its versatility in targeting multiple pathways associated with chronic conditions. Germacrone has emerged as a promising candidate for the treatment of diverse chronic diseases. The understanding of its multi-targeting capabilities, coupled with its natural origin, positions it as a valuable scaffold for developing therapeutics. The exploration of germacrone as a structural framework for multi-targeting drugs offers a potential avenue to enhance efficacy while minimizing potential side effects. Further research and clinical trials are warranted to validate the therapeutic potential of germacrone in diverse medical contexts.

The green formulation of silver nanoparticles for the anticancer and lupus nephritis treatment applications and reducing the inflammatory cytokines in the rat periodontal model

In this study, a novel bio-inspired synthesis for the preparation of Ag NPs by Calendula persica flower extract has been researched. Also, the effects of the recent composite on lupus nephritis by following the TGF-β1 signaling pathway in mice and gingival amounts of IL1-β and TNF-α in the animal periodontal model were determined. To assess the crystal nature, morphology and size of the prepared nanoparticles, X-ray diffraction (XRD), transmission electron microscopy (TEM), ultraviolet–visible (UV–Vis) and field emission-scanning electron microscopy (FE-SEM) analyses were applied in this study. The prepared Ag NPs was employed for its effectiveness against colon cancer cell line (C26). The bio-synthesized Ag NPs had also cytotoxic property versus colon cancer based on MTT protocol. Collectively, the Ag NPs fabricated by biological way has potential applications in inflammatory treatment. In lupus nephritis section, indexes in animal tissues and serum were identified using specific kits, while pathological alterations in the mice kidney were examined through H&E staining. Additionally, qPCR was employed to determine the expression related to TGF-β 1 in kidney, thereby providing further insight into the silver nanoparticles mechanism. The findings indicated that silver nanoparticles reduced the mRNA expression levels of TGF-β 1 and NF-κB in the kidneys, while simultaneously increasing the Mn-SOD and IκB-α expression. Histological examination of H&E-stained sections revealed that silver nanoparticles mitigated the morphological abnormalities of the glomeruli and the inflammatory infiltration associated with nephritis. Silver nanoparticles demonstrated an inhibitory effect on the dsDNA positive rate in animal suffering from nephritis. Silver nanoparticles were found to reduce the increase in urinary protein and the pro-inflammatory cytokines concentrations in both the kidney and serum. In the periodontal model study, 0-3 ligatures were applied to induce the inflammatory periodontitis in right mandibular first molar neck in rats. The levels of inflammatory cytokines (IL1-β, CINC-1, IL-10 and TNF-α) were determined by common immunological test, ELISA. The findings revealed that Ag NPs administration could decease the IL1-β and TNF-α production in the rat periodontal model gum tissue. In addition, the outcome of this research indicated that IL1-β and TNF-α levels raised in the rat periodontal model gum tissue compared to control group. Ag NPs increased the levels of superoxide dismutase, catalase, and plasma bone alkaline phosphatase and reduced the IL1-β, TNF-α, inducible nitric oxide synthase and RANK genes mRNA expression. The results indicate that pre/post-treatment with Ag NPs because of its direct activity on pro-inflammatory cytokines inhibition improved the inflammatory symptoms in the periodontitis and lupus nephritis animals.

Multifunctional lanthanum oxide-doped carboxymethyl cellulose nanocomposites: A promising approach for antimicrobial and targeted anticancer applications

This study presents the synthesis and characterization of lanthanum oxide (La₂O₃)-doped carboxymethyl cellulose (CMC) nanocomposites via a solution casting method, designed to offer an eco-friendly, multifunctional material with significant potential in biomedical applications. Structural analysis using FTIR, XRD, and EDX confirmed successful La₂O₃ integration, with FTIR spectra indicating a distinctive LaO stretching peak at 628.2 cm−1, XRD patterns revealing enhanced crystallinity with notable peaks at 16.6°, 27.6°, and 49.8°, and EDX showing a uniform lanthanum distribution with a 10.41 mass% concentration. These enhancements in structural stability and crystalline properties underscore the composite's functional robustness. Biological assessments revealed the composite's substantial antimicrobial efficacy, demonstrating inhibition zones up to 31 mm against pathogenic strains such as E. coli, S. aureus, E. faecalis, K. pneumoniae, and C. albicans at a 15 wt% La₂O₃ concentration—surpassing conventional antimicrobial agents. Minimum inhibitory concentration (MIC) tests supported these findings, showing MIC values as low as 7.82 μg/mL, further validating the composite's heightened antimicrobial potency compared to pure CMC. In vitro cytotoxicity assays indicated selective anticancer effects of the La₂O₃/CMC nanocomposites, with IC₅₀ values of 327.7 μg/mL and 189.8 μg/mL against PC-3 prostate and A549 lung cancer cells, respectively. Remarkably, the composite showed minimal impact on normal lung fibroblasts (Wi-38), with an IC₅₀ value of 956.8 μg/mL, emphasizing its selectivity towards cancer cells. Collectively, these results highlight the La₂O₃/CMC composite as a biocompatible and multifunctional material suitable for both antimicrobial and targeted anticancer applications, aligning with the growing demand for safe, effective biomedical solutions.

A Detailed Review on the Green Synthesis of Selenium Nanoparticles Using Plant Extracts and Their Anticancer Applications

AbstractNanobiotechnology is a field of science with tremendous promising applications in cancer chemotherapy, targeted drug delivery, molecular diagnosis, and molecular imaging. Selenium, one of the critical trace elements, participates in the structure of selenocysteine protein, which plays an important role in maintaining redox balance due to its oxidoreductase activity. Elemental selenium (Se0) has significantly lower toxicity values than its oxyanions, selenite, and selenate forms. For this reason, it is important to convert elemental selenium into atomic form in biological studies. In particular, their role in regulating the immune system makes selenium nanoparticles (SeNPs) superior to others. SeNPs have been discussed effectively in the literature in anticancer activity applications. SeNPs green synthesis is focused on a more economical, biocompatible, and environmentally friendly application by using, reducing, and stabilizing agents in plants. The aim of this review is to highlight the anticancer activity applications of SeNPs synthesized with plant extracts in the last 6 years (i.e., between 2019 and 2024). In addition, it aims to shed light on the green synthesis mechanism of NPs by using plant extracts and to highlight the factors affecting green synthesis and its advantages and disadvantages.

Novel Thiazole-Fused [4,5-g] or [5,4-g]Quinazolin-8-ones and Their Quinazoline Analogues: Synthesis and Biological Evaluation.

Background/Objectives: In connection with previous work on V-shaped polycyclic thiazolo[5,4-f]quinazolin-9-one and [5,4-f]quinazoline derivatives that can modulate the activity of various kinases, the synthesis of straight thiazole-fused [4,5-g] or [5,4-g]quinazolin-8-ones and quinazoline derivatives hitherto undescribed was envisioned. Methods: An innovative protocol allowed to obtain the target structures. The synthesis of inverted thiazolo[4,5-h] and [5,4-h]quinazolin-8-one derivatives was also explored with the aim of comparing biological results. The compounds obtained were tested against a representative panel of eight mammalian protein kinases of human origin: CDK9/CyclinT, Haspin, Pim-1, GSK-3β, CK-1ε, JAK3, CLK1 and DYRK1A. Results and Conclusions: The results obtained show that the novel linear thiazoloquinazolines are not kinase inhibitors. The cytotoxicity of these newly synthesized compounds was assessed against seven representative tumor cell lines (human cancers: Huh7-D12, Caco-2, HCT-116, MCF-7, MDA-MB-231, MDA-MB-468 and PC-3). The majority of these novel molecules proved capable of inhibiting the growth of the tested cells. The 7-Benzyl-8-oxo-7,8-dihydrothiazolo[5,4-g]quinazolinones 5b and 6b are the most potent, with IC50 values in the micromolar range. None of these compounds showed toxicity against normal cells. A larger program of investigations will be launched to investigate the real potential interest of such compounds in anticancer applications.

Synthesis of nanohybrid consisting of taurine derived carbon dots and nanoceria for anticancer applications

Here, we first synthesized carbon dots (CDs) from taurine and then a nanohybrid with ceria (CeO2) nanoparticles using thermal decomposition method for checking their antineoplastic efficacy against human triple negative mammary carcinoma cells, MDA-MB-231. The in vitro study demonstrated significant dose-dependent antineoplastic activity of the nanohybrids within a range of concentration from 10 to 50 μg/mL after 48 h of treatment. The cellular morphology analysis clearly depicted substantial amount of cell death which seems to stem from increased intracellular reactive oxygen species (ROS) production. However, the maximum anticancer activity of the nanohybrid as compared to bare CDs and CeO2 is supposed to be due to the combined anticancer effect of both CDs and CeO2 (a well-established antitumor agent). Further we have performed molecular docking study to reveal the anticancer mechanism of CDs which exhibited high binding capacity towards several proapoptotic and antiapoptotic protein molecules. The binding affinity values were found to be – 8.7 kcal/mol, – 7.9 kcal/mol, – 9.6 kcal/mol, – 9.5 kcal/mol, – 12 kcal/mol and – 11.1 kcal/mol for BAD, BCl-2, p53, Caspase-8, Caspase-9 and Caspase-3 respectively. Taken together, our synthesized CDs-CeO2 nanohybrid could be thought as a potential anticarcinogenic option in the field of breast cancer therapeutics.

Recent progress in cellulose derivatives and cellulose-based composites for bioimaging and anticancer applications (2020–2024)

Recent progress in cellulose derivatives and cellulose-based composites for bioimaging and anticancer applications (2020–2024)

Demystifying the Potential of Embelin-Loaded Nanoformulations: a Comprehensive Review.

Phytoconstituent based therapies have the potential to reduce the adverse effects and enhance overall patient compliance for different diseased conditions. Embelin (EMB) is a natural compound extracted from Embelia ribes that has demonstrated high therapeutic potential, particularly as anti-inflammatory and anticancer therapeutic applications. However, its poor water solubility and low oral bioavailability limitations make it challenging to use in biomedical applications. Nanostructure-based novel formulations have shown the potential to improve physicochemical and biological characteristics of active pharmaceutical ingredients obtained from plants. Different nanoformulations that have been utilized to encapsulate/entrap EMB for various therapeutic applications are nanoliposomes, nanostructured lipid carriers, niosomes, polymeric nanoparticles, nanosuspensions, phytosomes, self nanoemulsifying drug delivery system, silver nanoparticles, microparticles, solid lipid nanoparticle, gold nanoparticles and nanomicelles. The common methods reported for the preparation of EMB nanoformulations are thin film hydration, nanoprecipitation, ethanol injection, emulsification followed by sonication. The size of nanoformulations ranged in between 50 and 345nm. In this review, the mentioned EMB loaded nanocarriers are methodically discussed for size, shape, drug entrapment, zeta potential, in vitro release & permeation and in vivo studies. Potential of EMB with other drugs (dual drug approach) incorporated in nanocarriers are also discussed (physicochemical and preclinical characteristics). Patents related to EMB nanoformulations are also presented which showed the clinical translation of this bioactive for future utilization in different indications.

Copper(II) complexes containing hydrazone and bipyridine/phenanthroline ligands for anticancer application against breast cancer cells

In this work, mixed ligand Cu(II) complexes containing hydrazone and bipyridine ligands (CB1-CB5), or hydrazone and phenanthroline ligands (CP1-CP5) have been synthesized and characterized by spectroscopic and analytical techniques. Single crystal X-ray structure of complex CB1 revealed that two nitrogen atoms from bipyridine, one carbonyl oxygen, one azomethine nitrogen and one hydroxyl oxygen from the hydrazone ligand coordinated to Cu(II) ion, adopting a distorted square pyramidal geometry. Interaction of these complexes with calf thymus (CT) DNA and bovine serum albumin (BSA) was analyzed by absorption and emission studies. Further, the in vitro anticancer activity of the complexes was investigated exclusively against the breast cancer cells namely MCF7, T47D and MDA MB 231, and a normal breast MCF 10a cell line. The phenanthroline bearing complexes (CP1-CP5) displayed better activity than their bipyridine counterparts as seen from the IC50 values. In addition, the most active complex CP1 having an IC50 value of 5.8 ± 0.3 μM against T47D cancer cells was investigated for its mode of cell death through acridine orange/ethidium bromide(AO/EB), 4′,6-diamidino-2-phenylindole (DAPI) and Annexin-V fluorescein isothiocyanate (FITC) staining assays which revealed apoptosis. Lastly, the cell cycle analysis revealed that complex CP1 induced cell death in T47D cancer cells at the G0/G1 phase.

Lepidium peruvianum as a Source of Compounds with Anticancer and Cosmetic Applications

Lepidium peruvianum—an edible herbaceous biennial plant distributed in the Andes—has been used for centuries as food and as a natural medicine in treating hormonal disorders, as an antidepressant, and as an anti-osteoporotic agent. The presented study aims to prove its beneficial cosmetic and chemopreventive properties by testing the antiradical, whitening, cytotoxic, and anticancer properties of differently colored phenotypes that were extracted using three solvents: methanol, water, and chloroform, with the help of the chemometric approach to provide evidence on the impact of single glucosinolanes (seven identified compounds in the HPLC-ESI-QTOF-MS/MS analysis) on the biological activity of the total extracts. The tested extracts exhibited moderate antiradical activity, with the methanolic extract from yellow and grey maca phenotypes scavenging 49.9 ± 8.96% and 48.8% ± 0.44% of DPPH radical solution at a concentration of 1 mg/mL, respectively. Grey maca was the most active tyrosinase inhibitor, with 72.86 ± 3.42% of the enzyme activity calculated for the water extract and 75.66 ± 6.21% for the chloroform extract. The studies in cells showed no cytotoxicity towards the human keratinocyte line HaCaT in all studied extracts and a marked inhibition of cell viability towards the G361 melanoma cell line, which the presence of pent-4-enylglucosinolate, glucotropaeolin, and glucoalyssin in the samples could have caused. Given all biological activity tests combined, the three mentioned compounds were shown to be the most significant positive contributors to the results obtained, and the grey maca water extract was found to be the best source of the former compound among the tested samples.

Harnessing Bacterial Metabolites for the Synthesis of Cu-silicate NPs: A Sustainable Route to Antimicrobial and Anticancer Application

Harnessing Bacterial Metabolites for the Synthesis of Cu-silicate NPs: A Sustainable Route to Antimicrobial and Anticancer Application