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Prostate cancer is a significant global health concern and one of the leading causes of death from diseases in men. There is a growing interest in exploring new therapeutic approaches to enhance patient treatment outcomes and quality of life. Snake venom-derived compounds have emerged as promising candidates for anticancer treatment due to their potential to be selective and reduce adverse effects. In this article, we conduct a literature review on prostate cancer and discuss the investigation of snake venoms as potential alternatives in treatments to minimize toxicity and maximize efficacy. The potential of snake venom toxins in modulating key processes such as cell apoptosis, inhibition of cell migration, and angiogenesis is highlighted. This comprehensive exploration reaffirms the importance of advancing research into snake venom-based therapies to combat prostate cancer, transform treatment paradigms, and improve the well-being of affected individuals. [ABSTRACT FROM AUTHOR]

Autodynamic cancer therapy possesses tremendous potential for enhancing therapeutic efficacy by initiating the treatment process autonomously within targeted cells. However, challenges related to biocompatibility and targeted delivery have hindered its clinical translation owing to the induction of adverse effects and cytotoxicity in healthy cells. In this study, a novel approach for auto‐initiated dynamic therapy by conjugating zwitterionic near‐infrared fluorophores to a cell‐penetrating peptide is proposed. This enables efficient cellular uptake and specific targeting of therapy to desired cells while avoiding off‐target uptake. The zwitterionic bioconjugate causes cancer‐specific toxicity following its internalization into the targeted cells, triggered by specific intracellular conditions in lysosomes. This innovative approach enables selective targeting of lysosomes in malignant cells while minimizing cytotoxic effects on normal cells. By targeting lysosomes, the method overcomes inherent risks and side effects associated with conventional cancer treatments, offering a selective and effective approach to cancer therapy. [ABSTRACT FROM AUTHOR]

Background: Various medicinal plants and their bioactive compounds exhibited promising anticancer activities by inducing apoptosis, inhibiting angiogenesis, and modulating several signaling pathways in cancer cells. This study aims to assess whether two medicinal plant extracts have anticancer properties, Suaeda Palaestina and Zygophyllum album. Methods: This study used Ehrlich solid tumor mice as its in vivo model. We divided male mice into five groups (n = 5 per group). Group I was used as a control for Ehrlich ascites carcinoma (EAC). Groups 2 and 3 were given Z. album extract 180 mg/kg and 360 mg/kg body weight intraperitoneally. Groups 4 and 5 were given the same dose of S. palaestina and treated three times a week for 2 weeks, starting on day 10 after EAC implantation. After 3 weeks, we collected blood samples and thigh skeletal muscle, homogenized them, and processed them for analysis. The results showed that Ehrlich solid rats (EST) treated with low-dose dichloromethane extracts from Z. album and S. palaestina had significantly smaller tumor sizes than the control group. Protein expression levels of p53, caspase 3, and Bcl-2 were quantified by western blotting. Results: The extracts from both plants induced the hunger mechanism, leading to increased expression of p53 and caspase 3 and decreased expression of Bcl-2 at the protein level in EST mice treated with Z. album and S. palaestina. In addition, the comet assay indicated that these plants have a genotoxic potential for solid tumor cells. The T3 and T4 levels in EST blood samples revealed that both plants had significantly reduced the concentration of T3 and significantly increased T4 compared to the EST mice untreated group. Furthermore, these results showed that Z. album and S. palaestina had antiproliferative effects in EST mice through apoptosis-mediated genotoxicity. Conclusions: These findings indicated that S. palaestina and Z. album could be considered potential natural sources of anticancer agents. [ABSTRACT FROM AUTHOR]

Cancer cell mitochondria are functionally different from those in normal cells and could be targeted to develop novel anticancer agents. The aryl-ureido fatty acid CTU (16({[4-chloro-3-(trifluoromethyl)phenyl]-carbamoyl}amino)hexadecanoic acid) is the prototype of a new class of targeted agents that enhance the production of reactive oxygen species (ROS) that disrupt the outer mitochondrial membrane (OMM) and kill cancer cells. However, the mechanism by which CTU disrupts the inner mitochondrial membrane (IMM) and activates apoptosis is not clear. Here, we show that CTU-mediated ROS selectively dysregulated the OMA1/OPA1 fusion regulatory system located in the IMM. The essential role of ROS was confirmed in experiments with the lipid peroxyl scavenger α-tocopherol, which prevented the dysregulation of OMA1/OPA1 and CTU-mediated MDA-MB-231 cell killing. The disruption of OMA1/OPA1 and IMM fusion by CTU-mediated ROS accounted for the release of cytochrome c from the mitochondria and the activation of apoptosis. Taken together, these findings demonstrate that CTU depolarises the mitochondrial membrane, activates ROS production, and disrupts both the IMM and OMM, which releases cytochrome c and activates apoptosis. Mitochondrial-targeting agents like CTU offer a novel approach to the development of new therapeutics with anticancer activity. [ABSTRACT FROM AUTHOR]

Chitinases, a glycosyl hydrolase family 18 members, have a wide distribution in both prokaryotes and eukaryotes, including humans. Regardless of the absence of endogenous chitin polymer, various chitinases and chitinase-like proteins (CLPs) have been reported in mammals. However, several other carbohydrate polymers, such as hyaluronic acid and heparan sulfate, show structural similarities with chitin, which could be a potential target of chitinase and CLPs. Heparan sulfate is part of the integral membrane proteins and involves in cell adherence and migration. Hence, to demonstrate the effect of chitinase on cancer cell progression, we selected two chitinases from Serratia marcescens, ChiB and ChiC, which function as exo- and endo-chitinase, respectively. The ChiB and ChiC proteins were produced recombinantly by cloning chiB and chiC genes from Serratia marcescens. The cell viability of the Michigan Cancer Foundation-7 (MCF-7) cells was studied using different concentrations of the purified recombinant proteins. Cell viability assay was performed using 3-(4, 5-dimethyl thiazolyl-2)-2, 5-diphenyltetrazolium bromide and water-soluble tetrazolium salt, and the effect of ChiB and ChiC on cell proliferation was studied by clonogenic assay. The cell migration study was analysed by wound healing, transwell migration, and invasion assays. Cell cycle analysis of propidium iodide–stained cells and cell proliferation markers such as pERK1/2, pAKT, and SMP30 were also done. It was observed that both ChiB and ChiC were able to impede cell viability, cell migration, and invasion significantly. These observations and our in silico molecular docking analysis suggest that ChiC is a potential anticancer agent and is more efficient than ChiB. Since the ChiC is able to inhibit both cancer cell proliferation and migration, it could be a potential candidate for the treatment of metastatic cancer. [ABSTRACT FROM AUTHOR]

Spontaneous forward–reverse mutations were reported by us earlier in clinical samples from various types of cancers and in HeLa cells under normal culture conditions. To investigate the effects of chemical stimulations on such mutation cycles, the present study examined single nucleotide variations (SNVs) and copy number variations (CNVs) in HeLa and A549 cells exposed to wogonin-containing or acidic medium. In wogonin, both cell lines showed a mutation cycle during days 16–18. In acidic medium, both cell lines displayed multiple mutation cycles of different magnitudes. Genomic feature colocalization analysis suggests that CNVs tend to occur in expanded and unstable regions, and near promoters, histones, and non-coding transcription sites. Moreover, phenotypic variations in cell morphology occurred during the forward–reverse mutation cycles under both types of chemical treatments. In conclusion, chemical stresses imposed by wogonin or acidity promoted cyclic forward–reverse mutations in both HeLa and A549 cells to different extents. [ABSTRACT FROM AUTHOR]

Background: Cancer is a persistent global health challenge, demanding continuous exploration of innovative therapeutic strategies. Hydroxytyrosol (HT), derived from olive oil, has garnered attention for its potent antioxidant and anti-inflammatory properties, revitalizing interest due to recent breakthroughs in comprehending its intricate anticancer mechanisms. Main Body: This review conducts a detailed analysis of hydroxytyrosol's molecular mechanisms in cancer. Delve into the complex pathways and processes underlying its anticancer properties, including its impact on critical cellular events such as inhibiting cancer cell growth, proliferation, metastasis, and apoptosis. We meticulously evaluate HT efficacy and safety through scrutiny of preclinical and clinical studies. Additionally, we explore the potential synergistic effects of combining HT with conventional cancer therapies to improve treatment outcomes while reducing side effects, offering a comprehensive approach to cancer management. Conclusion: This review stands as a valuable resource for researchers, clinicians, and policymakers, providing profound insights into HT potent anticancer activity at the molecular level. It underscores the immense potential of natural compounds in the intricate realm of cancer management and highlights the urgent need for further research to translate these discoveries into effective clinical applications. Ultimately, it fosters the development of targeted and personalized therapeutic approaches, reigniting hope in the ongoing battle against cancer and enhancing the quality of life for those afflicted by this relentless disease. [ABSTRACT FROM AUTHOR]

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Abstract Background Various medicinal plants and their bioactive compounds exhibited promising anticancer activities by inducing apoptosis, inhibiting angiogenesis, and modulating several signaling pathways in cancer cells. This study aims to assess whether two medicinal plant extracts have anticancer properties, Suaeda Palaestina and Zygophyllum album. Methods This study used Ehrlich solid tumor mice as its in vivo model. We divided male mice into five groups (n = 5 per group). Group I was used as a control for Ehrlich ascites carcinoma (EAC). Groups 2 and 3 were given Z. album extract 180 mg/kg and 360 mg/kg body weight intraperitoneally. Groups 4 and 5 were given the same dose of S. palaestina and treated three times a week for 2 weeks, starting on day 10 after EAC implantation. After 3 weeks, we collected blood samples and thigh skeletal muscle, homogenized them, and processed them for analysis. The results showed that Ehrlich solid rats (EST) treated with low-dose dichloromethane extracts from Z. album and S. palaestina had significantly smaller tumor sizes than the control group. Protein expression levels of p53, caspase 3, and Bcl-2 were quantified by western blotting. Results The extracts from both plants induced the hunger mechanism, leading to increased expression of p53 and caspase 3 and decreased expression of Bcl-2 at the protein level in EST mice treated with Z. album and S. palaestina. In addition, the comet assay indicated that these plants have a genotoxic potential for solid tumor cells. The T3 and T4 levels in EST blood samples revealed that both plants had significantly reduced the concentration of T3 and significantly increased T4 compared to the EST mice untreated group. Furthermore, these results showed that Z. album and S. palaestina had antiproliferative effects in EST mice through apoptosis-mediated genotoxicity. Conclusions These findings indicated that S. palaestina and Z. album could be considered potential natural sources of anticancer agents.

Abstract Background Cancer is a persistent global health challenge, demanding continuous exploration of innovative therapeutic strategies. Hydroxytyrosol (HT), derived from olive oil, has garnered attention for its potent antioxidant and anti-inflammatory properties, revitalizing interest due to recent breakthroughs in comprehending its intricate anticancer mechanisms. Main Body This review conducts a detailed analysis of hydroxytyrosol’s molecular mechanisms in cancer. Delve into the complex pathways and processes underlying its anticancer properties, including its impact on critical cellular events such as inhibiting cancer cell growth, proliferation, metastasis, and apoptosis. We meticulously evaluate HT efficacy and safety through scrutiny of preclinical and clinical studies. Additionally, we explore the potential synergistic effects of combining HT with conventional cancer therapies to improve treatment outcomes while reducing side effects, offering a comprehensive approach to cancer management. Conclusion This review stands as a valuable resource for researchers, clinicians, and policymakers, providing profound insights into HT potent anticancer activity at the molecular level. It underscores the immense potential of natural compounds in the intricate realm of cancer management and highlights the urgent need for further research to translate these discoveries into effective clinical applications. Ultimately, it fosters the development of targeted and personalized therapeutic approaches, reigniting hope in the ongoing battle against cancer and enhancing the quality of life for those afflicted by this relentless disease.

Abstract Spontaneous forward–reverse mutations were reported by us earlier in clinical samples from various types of cancers and in HeLa cells under normal culture conditions. To investigate the effects of chemical stimulations on such mutation cycles, the present study examined single nucleotide variations (SNVs) and copy number variations (CNVs) in HeLa and A549 cells exposed to wogonin-containing or acidic medium. In wogonin, both cell lines showed a mutation cycle during days 16–18. In acidic medium, both cell lines displayed multiple mutation cycles of different magnitudes. Genomic feature colocalization analysis suggests that CNVs tend to occur in expanded and unstable regions, and near promoters, histones, and non-coding transcription sites. Moreover, phenotypic variations in cell morphology occurred during the forward–reverse mutation cycles under both types of chemical treatments. In conclusion, chemical stresses imposed by wogonin or acidity promoted cyclic forward–reverse mutations in both HeLa and A549 cells to different extents.

Oral squamous cell carcinoma (OSCC) is a disease of significant concern with higher mortality rates. Conventional treatment approaches have several drawbacks, leading to the opening of new research avenues in the field of nanoparticle-based cancer therapeutics. The study aimed at the synthesis of gold nanoparticles (Pm-AuNPs) from the aqueous bark extract of Pterocarpus marsupium, followed by its characterization and in vitro anticancer evaluation against OSCC. The synthesized Pm-AuNPs were characterized using UV–visible spectroscopy, particle size analyser, zeta potential, FTIR and SEM techniques. The anticancer potential of the Pm-AuNPs was evaluated against OSCC cell lines (SCC29b, SSC154 and OECM-1) through in vitro assays. The IC50 value was found to be 25 ± 1.2, 45 ± 1.5 and 75 ± 2.1 µg/mL for the three OSCC cell lines, elucidating Pm-AuNPs cytotoxic effects and mechanism of action. Intracellular ROS and SOX detection, mitochondrial transmembrane potential analysis and apoptosis detection were used to confirm the activity of Pm-AuNPs against OSCC. Acute toxicity studies on Wistar rats confirmed the non-toxic nature of the Pm-AuNPs at a higher dose concentration up to 2000 mg/kg body weight. The findings underscore Pm-AuNPs as promising candidates for future anticancer therapeutics, providing insights into their mechanism of action and therapeutic efficacy against OSCC.

Microbial synthesis offers a sustainable and eco-friendly approach for nanoparticle production. This study explores the biogenic synthesis of zinc oxide nanoparticles (ZnO-NPs) utilizing the actinomycete Saccharopolyspora hirsuta (Ess_amA6) isolated from Tapinoma simrothi. The biosynthesized ZnO-NPs were characterized using various techniques to confirm their formation and properties. UV–visible spectroscopy revealed a characteristic peak at 372 nm, indicative of ZnO-NPs. X-ray diffraction (XRD) analysis confirmed the crystalline structure of the ZnO-NPs as hexagonal wurtzite with a crystallite size of approximately 37.5 ± 13.60 nm. Transmission electron microscopy (TEM) analysis showed the presence of both spherical and roughly hexagonal ZnO nanoparticles in an agglomerated state with a diameter of approximately 44 nm. The biogenic ZnO-NPs exhibited promising biomedical potential. They demonstrated selective cytotoxic activity against human cancer cell lines, demonstrating higher efficacy against Hep-2 cells (IC50 = 73.01 µg/mL) compared to MCF-7 cells (IC50 = 112.74 µg/mL). Furthermore, the biosynthesized ZnO-NPs displayed broad-spectrum antimicrobial activity against both Pseudomonas aeruginosa and Staphylococcus aureus with clear zones of inhibition of 12.67 mm and 14.33 mm, respectively. The MIC and MBC values against P. aeruginosa and S. aureus ranged between 12.5 and 50 µg/mL. These findings suggest the potential of S. hirsuta-mediated ZnO-NPs as promising biocompatible nanomaterials with dual applications as antimicrobial and anticancer agents. [ABSTRACT FROM AUTHOR]

Simple Summary: This review comprehensively examines curcumin's therapeutic potential in cancer treatment. It addresses the limitations of curcumin therapy due to its low bioavailability and potential side effects. It discusses how modern approaches can overcome these limitations to support its consistent and effective use in cancer therapy. Indeed, the role of curcumin in photodegradation and photodynamic therapy is emphasized through its use in combination with phototherapy. In addition, improved therapeutic efficacy, increased cellular uptake, and enhanced cytotoxicity have been demonstrated in various cancer models using curcumin-loaded nanoparticle drug delivery. Overall, the present review highlights the promising impact of curcumin in cancer treatment and the importance of optimizing its therapeutic efficacy, considering potential interactions with drugs used to manage side effects and collateral effects of cancer treatment. Curcumin, a polyphenolic compound derived from Curcuma longa, exhibits significant therapeutic potential in cancer management. This review explores curcumin's mechanisms of action, the challenges related to its bioavailability, and its enhancement through modern technology and approaches. Curcumin demonstrates strong antioxidant and anti-inflammatory properties, contributing to its ability to neutralize free radicals and inhibit inflammatory mediators. Its anticancer effects are mediated by inducing apoptosis, inhibiting cell proliferation, and interfering with tumor growth pathways in various colon, pancreatic, and breast cancers. However, its clinical application is limited by its poor bioavailability due to its rapid metabolism and low absorption. Novel delivery systems, such as curcumin-loaded hydrogels and nanoparticles, have shown promise in improving curcumin bioavailability and therapeutic efficacy. Additionally, photodynamic therapy has emerged as a complementary approach, where light exposure enhances curcumin's anticancer effects by modulating molecular pathways crucial for tumor cell growth and survival. Studies highlight that combining low concentrations of curcumin with visible light irradiation significantly boosts its antitumor efficacy compared to curcumin alone. The interaction of curcumin with cytochromes or drug transporters may play a crucial role in altering the pharmacokinetics of conventional medications, which necessitates careful consideration in clinical settings. Future research should focus on optimizing delivery mechanisms and understanding curcumin's pharmacokinetics to fully harness its therapeutic potential in cancer treatment. [ABSTRACT FROM AUTHOR]

Background: The scientific literature has reported an inverse association between broccoli consumption and the risk of suffering from several types of cancer; however, the results were not entirely consistent across studies. A systematic review and meta-analysis of observational studies were conducted to determine the association between broccoli consumption and cancer risk with the aim of clarifying the beneficial biological effects of broccoli consumption on cancer. Methods: PubMed/MEDLINE, Web of Science, Scopus, Cochrane Library (CENTRAL), and Epistemonikos databases were searched to identify all published papers that evaluate the impact of broccoli consumption on the risk of cancer. Citation chasing of included studies was conducted as a complementary search strategy. The risk of bias in individual studies was assessed using the Newcastle-Ottawa Scale. A random-effects model meta-analysis was employed to quantitatively synthesize results, with the I2 index used to assess heterogeneity. Results: Twenty-three case–control studies (n = 12,929 cases and 18,363 controls; n = 31,292 individuals) and 12 cohort studies (n = 699,482 individuals) were included in the meta-analysis. The results suggest an inverse association between broccoli consumption and the risk of cancer both in case–control studies (OR: 0.64, 95% CI from 0.58 to 0.70, p < 0.001; Q = 35.97, p = 0.072, I2 = 30.49%—moderate heterogeneity; τ2 = 0.016) and cohort studies (RR: 0.89, 95% CI from 0.82 to 0.96, p = 0.003; Q = 13.51, p = 0.333, I2 = 11.21%—low heterogeneity; τ2 = 0.002). Subgroup analysis suggested a potential benefit of broccoli consumption in site-specific cancers only in case–control studies. Conclusions: In summary, the findings indicate that individuals suffering from some type of cancer consumed less broccoli, suggesting a protective biological effect of broccoli on cancer. More studies, especially cohort studies, are necessary to clarify the possible beneficial effect of broccoli on several types of cancer. [ABSTRACT FROM AUTHOR]

ONIOM2 approach put together molecular dynamics simulations and molecular docking was conducted to the investigation of the interaction of some the novel azaspironenone derivatives with Caspase-3 protein. The active sites of the protein that resulted from molecular docking are applied for computations of ONIOM2 and molecular dynamics. The best pose of the configuration of studied azaspironenone derivatives in the active sites of Caspase-3 protein results in negative binding energies. Also, the stability of the compounds was confirmed by ONIOM2 calculations. The data showed that the residues of Gly94, Thr34, and Cys135 participated in the formation of hydrogen bonds. In addition, MD simulation was done on the stable complexes with high binding energy to recognize the structural changes on azaspironenone derivatives-Caspase-3 protein complexes. The silico studies illustrated that the properties of docking of azaspironenone derivatives could be used as a potential therapeutic agent against the A549 human lung cancer cells. [ABSTRACT FROM AUTHOR]

Abstract Autodynamic cancer therapy possesses tremendous potential for enhancing therapeutic efficacy by initiating the treatment process autonomously within targeted cells. However, challenges related to biocompatibility and targeted delivery have hindered its clinical translation owing to the induction of adverse effects and cytotoxicity in healthy cells. In this study, a novel approach for auto‐initiated dynamic therapy by conjugating zwitterionic near‐infrared fluorophores to a cell‐penetrating peptide is proposed. This enables efficient cellular uptake and specific targeting of therapy to desired cells while avoiding off‐target uptake. The zwitterionic bioconjugate causes cancer‐specific toxicity following its internalization into the targeted cells, triggered by specific intracellular conditions in lysosomes. This innovative approach enables selective targeting of lysosomes in malignant cells while minimizing cytotoxic effects on normal cells. By targeting lysosomes, the method overcomes inherent risks and side effects associated with conventional cancer treatments, offering a selective and effective approach to cancer therapy.

Being a component of the Ras/Raf/MEK/ERK signaling pathway crucial for cellular responses, the VRAF murine sarcoma viral oncogene homologue B1 (BRAF) kinase has emerged as a promising target for anticancer drug discovery due to oncogenic mutations that lead to pathway hyperactivation. Despite the discovery of several small-molecule BRAF kinase inhibitors targeting oncogenic mutants, their clinical utility has been limited by challenges such as off-target effects and suboptimal pharmacological properties. This study focuses on identifying miniprotein inhibitors for the oncogenic V600E mutant BRAF, leveraging their potential as versatile drug candidates. Using a structure-based de novo design approach based on binding affinity to V600E mutant BRAF and hydration energy, 39 candidate miniprotein inhibitors comprising three helices and 69 amino acids were generated from the substructure of the endogenous ligand protein (14-3-3). Through in vitro binding and kinase inhibition assays, two miniproteins (63 and 76) were discovered as novel inhibitors of V600E mutant BRAF with low-micromolar activity, with miniprotein 76 demonstrating a specific impediment to MEK1 phosphorylation in mammalian cells. These findings highlight miniprotein 76 as a potential lead compound for developing new cancer therapeutics, and the structural features contributing to its biochemical potency against V600E mutant BRAF are discussed in detail. [ABSTRACT FROM AUTHOR]

A series of flavanols were synthesized to assess their biological activity against human non-small cell lung cancer cells (A549). Among the sixteen synthesized compounds, it was observed that compounds 6k (3.14 ± 0.29 µM) and 6l (0.46 ± 0.02 µM) exhibited higher potency compared to 5-fluorouracil (5-Fu, 4.98 ± 0.41 µM), a clinical anticancer drug which was used as a positive control. Moreover, compound 6l (4'-bromoflavonol) markedly induced apoptosis of A549 cells through the mitochondrial- and caspase-3-dependent pathways. Consequently, compound 6l might be developed as a candidate for treating or preventing lung cancer. [ABSTRACT FROM AUTHOR]

Brazilin is the main compound in Caesalpinia sappan and Haematoxylum braziletto, which is identified as a homoisoflavonoid based on its molecular structure. These plants are traditionally used as an anti-inflammatory to treat fever, hemorrhage, rheumatism, skin problems, diabetes, and cardiovascular diseases. Recently, brazilin has increased its interest in cancer studies. Several findings have shown that brazilin has cytotoxic effects on colorectal cancer, breast cancer, lung cancer, multiple myeloma, osteosarcoma, cervical cancer, bladder carcinoma, also other cancers, along with numerous facts about its possible mechanisms that will be discussed. Besides its flavonoid content, brazilin is able to chelate metal ions. A study has proved that brazilin could be used as an antituberculosis agent based on its ability to chelate iron. This possible ironchelating of brazilin and all the studies discussed in this review will lead us to the statement that, in the future, brazilin has the potency to be a chemo-preventive and anticancer agent. The article review aimed to determine the brazilin mechanism and pathogenesis of cancer. [ABSTRACT FROM AUTHOR]

Spirulina platensis is blue-green algae received significant attention for its high nutritional value, it is a source of powerful antioxidants. The cytotoxicity of crude extract is not well recorded. The aim of current study to evaluate the cytotoxicity of S. platensis extracts on colon cancer (CaCo-2), hepatic cancer (HepG2) cell lines, normal fibroblast cells line (HdFn) and also antioxidant activity. The percent of 1-diphenyl-2-picrylhydrazyl (DPPH) scavenging activity was determined for serial concentrations of extract ranging from 3.125 to 200 µg/ml. Cell lines were treated for 24 hours with different concentrations of extract ranging from 25 to 400 µg/ml. Cell viability testing using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay which determined how the extract affected caspase 9 activity. The results revealed that extract had moderate antioxidant activity, showing the DPPH scavenging activity reached 58% in a concentration of 200µg/ml, and IC50 was 95.84 µg/ml. The extract significantly decreased CaCo-2 cell viability with IC50 99.12 µg/ml, compared to HdFn viability with IC50 157.6 µg/ml. On CaCo-2 cells, the extract's cytotoxicity was more evident (P< 0.05) than HdFn cells. The extract had more significant (P<0.05) cytotoxicity on cancer cell lines and also significantly decreased the viability of HepG2 cells with IC50 167.4 µg/ml, than the viability of HdFn with IC50 214.9 µg/ml. The extract revealed significantly higher (P< 0.05) cytotoxicity against HepG2 cells than the normal HdFn cells. This study concluded that the extract exerted a dose-dependent anti-proliferation effect on CaCo-2 cells and HepG2 cells by comparing them with HdFn cells. [ABSTRACT FROM AUTHOR]

ABSTRACTThere is a significant load of degenerative and chronic illnesses, especially cancer, which is one of the main reasons for morbidity and death globally. Polyphenolic phytochemicals found in many plant diets have been shown in epidemiologic and preclinical studies to have chemopreventive activities against numerous cancer types. As a result, there is growing interest in possible cancer chemopreventive medicines derived from natural compounds, such as polyphenols, which may provide a novel, cost-effective way to reduce the global cancer burden. Various epidemiologic researchers have found a link between a soy-rich diet and tumor avoidance, which has been linked to the existence of genistein, a phenolic component found in soy-based diets. Genistein controlled strong anti-inflammatory actions through the blocking of different signaling pathways such as (PGs) Prostaglandins, pro-inflammatory (ROS) reactive oxygen species and cytokines, (iNOS) inducible nitric oxide synthase and (NF-κB) nuclear factor kappa-B. Furthermore, therapeutic effects of genistein have been conveyed in various pathological situations through modifying intracellular paths such as Akt, mTOR, PI3K, PPARγ, NF-κB, Nrf2 and AMPK. Genistein works as a chemotherapeutic drug against several cancers, primarily through modifying the cell cycle, apoptosis, and angiogenesis, as well as limiting metastasis. Genistein also exhibits a synergistic attitude with renowned anticancer medicines including adriamycin, tamoxifen and docetaxel indicating a possible role in grouping treatment. The study presents the recent data available on genistein’s beneficial effects against various forms of cancers.

Strophanthidin (SPTD), one of the cardiac glycosides, is refined from traditional Chinese medicines such as Semen Lepidii and Antiaris toxicaria, and was initially used for the treatment of heart failure disease in clinic. Recently, SPTD has been shown to be a potential anticancer agent, but the underlying mechanism of action is poorly understood. Herein, we explored the molecular mechanism by which SPTD exerts anticancer effects in A549 human lung adenocarcinoma cells by means of mass spectrometry-based quantitative proteomics in combination with bioinformatics analysis. We revealed that SPTD promoted the expression of tumor necrosis factor (TNF)-related apoptosis-inducing ligand receptor 2 (TRAIL-R2, or DR5) in A549 cells to activate caspase 3/6/8, in particular caspase 3. Consequently, the activated caspases elevated the expression level of apoptotic chromatin condensation inducer in the nucleus (ACIN1) and prelamin-A/C (LMNA), ultimately inducing apoptosis via cooperation with the SPTD-induced overexpressed barrier-to-autointegration factor 1 (Banf1). Moreover, the SPTD-induced DEPs interacted with each other to downregulate the p38 MAPK/ERK signaling, contributing to the SPTD inhibition of the growth of A549 cells. Additionally, the downregulation of collagen COL1A5 by SPTD was another anticancer benefit of SPTD through the modulation of the cell microenvironment. [ABSTRACT FROM AUTHOR]

Background: Oral cancer remains one of the most dreadful diseases in developing nations. Currently, there has been a rise in the prevalence of tongue squamous cell carcinoma (SCC), with a poor prognosis. The use of standard treatment approaches against oral cancer patients brings about several side effects. In recent years, nanomedicine has provided a versatile platform for developing new targeted therapeutic modalities. However, safety remains a concern in the synthesis of nanoparticles (NPs). Therefore, the present study aims to synthesize safer phytoconstituent-mediated gold NPs (AuNPs) utilizing leaf extracts of Annona muricata, where the biochemical components of the plant leaf act as the reducing and capping agents in the synthesis of NPs, and to evaluate its anti-cancer activity against SCC. Materials and Methods: In this in vitro experimental study, AuNPs were synthesized through an effective, simple, and ecologically sound green synthesis method. After characterization of these synthesized AuNPs, in vitro assays such as 3-(4, 5-dimethylthiazole2-yl)-2, 5-biphenyl tetrazolium bromide, wound healing, and clonogenic assays were carried out to investigate the anti-cancer potential of green synthesized AuNPs in the human tongue SCC cell line (SCC-15), and the possible mechanism of action was evaluated through gene and protein expression analysis of Bax, Bcl-2, and p53 genes. The results were expressed as mean ± standard deviation using Statistical Package for Social Sciences (SPSS) 20.0 software and Student's t-test was performed for experimental data. P ≤0.05 were considered statistically significant. Results: The in vitro assays demonstrated that the synthesized AuNPs are exhibiting anti-cancer activity by apoptosis of SCC-15 cells in a dose-dependent manner. Further, it also revealed a highly significant decrease in anti-apoptotic Bcl-2 gene expression, whereas pro-apoptotic genes p53 and Bax revealed a highly significant increase, which is statistically significant compared to the control (P < 0.05). Conclusion: Our findings demonstrated that the AuNPs synthesized from A. muricata leaf extract could act as a novel anticancer agent, particularly against SCC, after further scrutiny. [ABSTRACT FROM AUTHOR]

Simple Summary: DNA repair inhibition constitutes a promising anticancer strategy, particularly in triple-negative breast cancer (TNBC), ovarian cancer and pancreatic ductal adenocarcinoma (PDAC). XGAc is a xanthonoside previously described as a potent cancer cell growth inhibitor. Herein, we aimed to evaluate the antitumor activity of XGAc in TNBC, ovarian cancer and PDAC cells, either alone or in combination with the poly(ADP-ribose) polymerase inhibitor (PARPi) olaparib. XGAc exhibits antiproliferative activity in TNBC, ovarian cancer and PDAC cells, also proving to be effective against patient-derived ovarian cancer cells and drug-resistant cancer cells. XGAc inhibited cancer cell migration, induced apoptosis and S-phase cell cycle arrest, and triggered genotoxicity by inhibiting the expression of homologous recombination DNA repair proteins in TNBC, ovarian cancer and PDAC cells. Importantly, XGAc displayed synergistic effects with olaparib, demonstrating its potential in combination therapy. Altogether, XGAc reveals itself to be a valuable anticancer agent for hard-to-treat cancers. Dysregulation of the DNA damage response may contribute to the sensitization of cancer cells to DNA-targeting agents by impelling cell death. In fact, the inhibition of the DNA repair pathway is considered a promising anticancer therapeutic strategy, particularly in combination with standard-of-care agents. The xanthonoside XGAc was previously described as a potent inhibitor of cancer cell growth. Herein, we explored its antitumor activity against triple-negative breast cancer (TNBC), ovarian cancer and pancreatic ductal adenocarcinoma (PDAC) cells as a single agent and in combination with the poly(ADP-ribose) polymerase inhibitor (PARPi) olaparib. We demonstrated that XGAc inhibited the growth of TNBC, ovarian and PDAC cells by inducing cell cycle arrest and apoptosis. XGAc also induced genotoxicity, inhibiting the expression of DNA repair proteins particularly involved in homologous recombination, including BRCA1, BRCA2 and RAD51. Moreover, it displayed potent synergistic effects with olaparib in TNBC, ovarian cancer and PDAC cells. Importantly, this growth inhibitory activity of XGAc was further reinforced in a TNBC spheroid model and in patient-derived ovarian cancer cells. Also, drug-resistant cancer cells showed no cross-resistance to XGAc. Additionally, the ability of XGAc to prevent cancer cell migration was evidenced in TNBC, ovarian cancer and PDAC cells. Altogether, these results highlight the great potential of acetylated xanthonosides such as XGAc as promising anticancer agents against hard-to-treat cancers. [ABSTRACT FROM AUTHOR]

A novel series of twelve aromatic bis-ureido-substituted benzenesulfonamides was synthesised by conjugation of aromatic aminobenzenesulfonamides with aromatic bis-isocyanates. The obtained bis-ureido-substituted derivatives were tested against four selected human carbonic anhydrase isoforms (hCA I, hCA II, hCA IX and hCA XII). Most of the new compounds showed an effective inhibitory profile against isoforms hCA IX and hCA XII, also having some selectivity with respect to hCA I and hCA II. The inhibition constants of these compounds against isoforms hCA IX and XII were in the range of 6.73–835 and 5.02–429 nM, respectively. Since hCA IX and hCA XII are important drug targets for anti-cancer/anti-metastatic drugs, these effective inhibitors reported here may be considered of interest for cancer related studies in which these enzymes are involved. [ABSTRACT FROM AUTHOR]

Background and Objectives: Cancer is the second-most-important deadly disease in the world, leading to severe socioeconomic consequences and posing a public threat. Consequently, breast and colorectal cancers are significant cancer types that affect women and men more commonly, respectively. Treatment failure or recurrent diseases frequently occur due to resistance, in addition to the side effects of the currently available anticancer agents. Therefore, in this study, herbal melanin anticancer activity was investigated against human breast adenocarcinoma (MDA-MB-231) and human colorectal (HCT 116) cell proliferation and the expression of downregulated anti-apoptotic proteins and upregulated pro-apoptotic p53. Materials and Methods: MDA-MB-231 and HCT 116 cells were monitored for their real-time proliferation properties using Xcelligence. Herbal melanin of various concentrations significantly inhibited MDA-MB-231 and HCT 116 cell proliferation. Then, the expression of proapoptotic and anti-apoptotic proteins such as p53, Bcl-2 and Bcl-xl was studied using Western blotting. Results: The Bcl-2 and Bcl-xl expressions were downregulated, while the p53 expression was upregulated after treatment with herbal melanin. Similarly, the expression of apoptotic proteins such as Bcl-2, Bcl-xl, XIAP, Survivin, Bid, Bax, p53, Cytochrome C, PARP genes and mRNA was studied after herbal melanin treatment using real-time PCR, which revealed the downregulation of Bcl-2, Bcl-xl, XIAP and Survivin and the upregulation of Bid, Bax, p53, Cytochrome C and PARP apoptotic protein expression. Also, caspase 3 and 9 expressions were monitored after the treatment with herbal melanin, which revealed the upregulation of both the MDA-MB-231 and HCT 116 cell types. Conclusions: Overall, herbal melanin can be used as an alternative anticancer agent against the MDA-MB-231 and HCT 116 cell types. [ABSTRACT FROM AUTHOR]

Brazilin is the main compound in Caesalpinia sappan and Haematoxylum braziletto, which is identified as a homoisoflavonoid based on its molecular structure. These plants are traditionally used as an anti-inflammatory to treat fever, hemorrhage, rheumatism, skin problems, diabetes, and cardiovascular diseases. Recently, brazilin has increased its interest in cancer studies. Several findings have shown that brazilin has cytotoxic effects on colorectal cancer, breast cancer, lung cancer, multiple myeloma, osteosarcoma, cervical cancer, bladder carcinoma, also other cancers, along with numerous facts about its possible mechanisms that will be discussed. Besides its flavonoid content, brazilin is able to chelate metal ions. A study has proved that brazilin could be used as an antituberculosis agent based on its ability to chelate iron. This possible iron-chelating of brazilin and all the studies discussed in this review will lead us to the statement that, in the future, brazilin has the potency to be a chemo-preventive and anticancer agent. The article review aimed to determine the brazilin mechanism and pathogenesis of cancer.

Microbial synthesis offers a sustainable and eco-friendly approach for nanoparticle production. This study explores the biogenic synthesis of zinc oxide nanoparticles (ZnO-NPs) utilizing the actinomycete Saccharopolyspora hirsuta (Ess_amA6) isolated from Tapinoma simrothi. The biosynthesized ZnO-NPs were characterized using various techniques to confirm their formation and properties. UV–visible spectroscopy revealed a characteristic peak at 372 nm, indicative of ZnO-NPs. X-ray diffraction (XRD) analysis confirmed the crystalline structure of the ZnO-NPs as hexagonal wurtzite with a crystallite size of approximately 37.5 ± 13.60 nm. Transmission electron microscopy (TEM) analysis showed the presence of both spherical and roughly hexagonal ZnO nanoparticles in an agglomerated state with a diameter of approximately 44 nm. The biogenic ZnO-NPs exhibited promising biomedical potential. They demonstrated selective cytotoxic activity against human cancer cell lines, demonstrating higher efficacy against Hep-2 cells (IC50 = 73.01 µg/mL) compared to MCF-7 cells (IC50 = 112.74 µg/mL). Furthermore, the biosynthesized ZnO-NPs displayed broad-spectrum antimicrobial activity against both Pseudomonas aeruginosa and Staphylococcus aureus with clear zones of inhibition of 12.67 mm and 14.33 mm, respectively. The MIC and MBC values against P. aeruginosa and S. aureus ranged between 12.5 and 50 µg/mL. These findings suggest the potential of S. hirsuta-mediated ZnO-NPs as promising biocompatible nanomaterials with dual applications as antimicrobial and anticancer agents.

A new series of 1,2,3-Triazole bearing Indole derivatives (6a–j, 8a & 9a) was developed and examined for their preliminary anticancer effects against five human cancer cell lines such as breast cancer cell line (MCF-7), human lung cancer cell line (A549), human colon cancer cell line (Colo-205), human prostate cancer cell line (DU-145) and human breast cancer cell line (MDA MB-231). The well-known chemotherapeutic agent as etoposide used as a positive control. Among synthesized compounds, six compounds (6a, 6b, 6c, 6d, 6f and 8a) were possessed more potent anticancer activities than standard drug.

A novel series of twelve aromatic bis-ureido-substituted benzenesulfonamides was synthesised by conjugation of aromatic aminobenzenesulfonamides with aromatic bis-isocyanates. The obtained bis-ureido-substituted derivatives were tested against four selected human carbonic anhydrase isoforms (hCA I, hCA II, hCA IX and hCA XII). Most of the new compounds showed an effective inhibitory profile against isoforms hCA IX and hCA XII, also having some selectivity with respect to hCA I and hCA II. The inhibition constants of these compounds against isoforms hCA IX and XII were in the range of 6.73–835 and 5.02–429 nM, respectively. Since hCA IX and hCA XII are important drug targets for anti-cancer/anti-metastatic drugs, these effective inhibitors reported here may be considered of interest for cancer related studies in which these enzymes are involved.

Simple Summary: This study summarizes the current state of knowledge about the anticancer potential of the curcumin analog EF24, including its pharmacokinetic profile, therapeutic efficacy, underlying mechanisms, and advancements in nanoformulations for effective drug delivery. EF24 and its nanoformulations hold great promise as novel and effective therapeutic strategies for cancer treatment and provide hope for patients to fight this devastating disease. More preclinical and clinical investigations are needed to fully unlock their potential and integrate them into clinical practice. EF24, a synthetic monocarbonyl analog of curcumin, shows significant potential as an anticancer agent with both chemopreventive and chemotherapeutic properties. It exhibits rapid absorption, extensive tissue distribution, and efficient metabolism, ensuring optimal bioavailability and sustained exposure of the target tissues. The ability of EF24 to penetrate biological barriers and accumulate at tumor sites makes it advantageous for effective cancer treatment. Studies have demonstrated EF24's remarkable efficacy against various cancers, including breast, lung, prostate, colon, and pancreatic cancer. The unique mechanism of action of EF24 involves modulation of the nuclear factor-kappa B (NF-κB) and nuclear factor erythroid 2-related factor 2 (Nrf2) signaling pathways, disrupting cancer-promoting inflammation and oxidative stress. EF24 inhibits tumor growth by inducing cell cycle arrest and apoptosis, mainly through inhibiting the NF-κB pathway and by regulating key genes by modulating microRNA (miRNA) expression or the proteasomal pathway. In summary, EF24 is a promising anticancer compound with a unique mechanism of action that makes it effective against various cancers. Its ability to enhance the effects of conventional therapies, coupled with improvements in drug delivery systems, could make it a valuable asset in cancer treatment. However, addressing its solubility and stability challenges will be crucial for its successful clinical application. [ABSTRACT FROM AUTHOR]

The study aims to contribute to drug design and development by analyzing protein-drug interactions. It has been reported that 1,3-benzodioxole-based ionic liquid derivatives possess cytotoxic effects against human cancer cell lines. The derivatives are microtubule-targeted chemotherapeutic agents that can suppress microtubule dynamics leading to apoptosis and mitotic blocking. We have focused attention on neomycin-based Ionic Liquids. We report here the screening of a set of derivatives to identify suitable inhibitors against protein function based on binding affinity, and physicochemical and pharmacokinetic studies. The tubulin protein structure was evaluated and validated using various validation tools for proteins viz. VADAR, Verify3D. The molecular docking of 1,3-benzodioxole-based neomycin-tagged ionic liquids was accomplished with tubulin protein to illustrate the interactions of the most potent compound, followed by pharmacokinetic and pharmacological studies. 3-(benzo[d][1,3]dioxol-5-ylmethyl)-2-nitro-1H-imidazol-3-ium dimethyl phosphate was found to be a tubulin polymerization inhibitor revealing the binding energy -327.18 kcal/mol. 3-(benzo[d][1,3]dioxol-5-ylmethyl)-2-nitro-1H-imidazol-3-ium dimethyl phosphate has shown 69.78% intestinal absorption, -1.29 log BB, -2.73 logKp, maximum tolerated dose: 0.22 log mg/kg/day, LD50: 2.89 mol/kg. The results revealed that these compounds interact efficiently with the receptor and that compound 1 can be evaluated as a potential therapeutic candidate. [ABSTRACT FROM AUTHOR]

Katarzyna Malarz,1,&ast; Julia Korzuch,2,&ast; Tainah Dorina Marforio,3 Katarzyna Balin,1 Matteo Calvaresi,3 Anna Mrozek-Wilczkiewicz,1 Robert Musiol,2 Maciej Serda2 1A. Che&lstrok;kowski Institute of Physics, University of Silesia in Katowice, Chorzów, Poland; 2Institute of Chemistry, University of Silesia in Katowice, Katowice, Poland; 3Department of Chemistry “Giacomo Ciamician”, University of Bologna, Bologna, Italy&ast;These authors contributed equally to this workCorrespondence: Maciej Serda; Katarzyna Malarz, Email maciej.serda@us.edu.pl; katarzyna.malarz@us.edu.plIntroduction: Thanks to recent advances in synthetic methodology, water-soluble fullerene nanomaterials that interfere with biomolecules, especially DNA/RNA and selected proteins, have been found with tremendous potential for applications in nanomedicine. Herein, we describe the synthesis and evaluation of a water-soluble glycine-derived [60]fullerene hexakisadduct (HDGF) with Th symmetry, which is a first-in-class BTK protein inhibitor.Methods: We synthesized and characterized glycine derived [60]fullerene using NMR, ESI-MS, and ATR-FT-IR. DLS and zeta potential were measured and high-resolution transmission electron microscopy (HRTEM) observations were performed. The chemical composition of the water-soluble fullerene nanomaterial was examined by X-ray photoelectron spectrometry. To observe aggregate formation, the cryo-TEM analysis was carried out. The docking studies and molecular dynamic simulations were performed to determine interactions between HDGF and BTK. The in vitro cytotoxicity was evaluated on RAJI and K562 blood cancer cell lines. Subsequently, we examined the induction of cell death by autophagy and apoptosis by determining the expression levels of crucial genes and caspases. We investigated the direct association of HDGF on inhibition of the BTK signalling pathway by examining changes in the calcium levels in RAJI cells after treatment. The inhibitory potential of HDGF against non-receptor tyrosine kinases was evaluated. Finally, we assessed the effects of HDGF and ibrutinib on the expression of the BTK protein and downstream signal transduction in RAJI cells following anti-IgM stimulation.Results: Computational studies revealed that the inhibitory activity of the obtained [60]fullerene derivative is multifaceted: it hampers the BTK active site, interacting directly with the catalytic residues, rendering it inaccessible to phosphorylation, and binds to residues that form the ATP binding pocket. The anticancer activity of produced carbon nanomaterial revealed that it inhibited the BTK protein and its downstream pathways, including PLC and Akt proteins, at the cellular level. The mechanistic studies suggested the formation of autophagosomes (increased gene expression of LC3 and p62) and two caspases (caspase-3 and − 9) were responsible for the activation and progression of apoptosis.Conclusion: These data illustrate the potential of fullerene-based BTK protein inhibitors as nanotherapeutics for blood cancer and provide helpful information to support the future development of fullerene nanomaterials as a novel class of enzyme inhibitors.Graphical Abstract: Keywords: fullerenes, BTK inhibitor, anticancer agent, autophagy, apoptosis

A series of flavanols were synthesized to assess their biological activity against human non-small cell lung cancer cells (A549). Among the sixteen synthesized compounds, it was observed that compounds 6k (3.14 ± 0.29 µM) and 6l (0.46 ± 0.02 µM) exhibited higher potency compared to 5-fluorouracil (5-Fu, 4.98 ± 0.41 µM), a clinical anticancer drug which was used as a positive control. Moreover, compound 6l (4’-bromoflavonol) markedly induced apoptosis of A549 cells through the mitochondrial- and caspase-3-dependent pathways. Consequently, compound 6l might be developed as a candidate for treating or preventing lung cancer.

Breast cancer is a leadingcause of cancer-related deaths in women globally, with triple-negative breast cancer (TNBC) being an aggressive subtype that lacks targeted therapies and is associated with a poor prognosis. Polyphenols, naturally occurring compounds in plants, have been investigated as a potential therapeutic strategy for TNBC. This review provides an overview of the anticancer effects of polyphenols in TNBC and their mechanisms of action. Several polyphenols, including resveratrol, quercetin, kaempferol, genistein, epigallocatechin-3-gallate, apigenin, fisetin, hesperetin and luteolin, have been shown to inhibit TNBC cell proliferation, induce cell cycle arrest, promote apoptosis, and suppress migration/invasion in preclinical models. The molecular mechanisms underlying their anticancer effects involve the modulation of several signalling pathways, such as PI3K/Akt, MAPK, STATT, and NF-κB pathways. Polyphenols also exhibit synergistic effects with chemotherapy drugs, making them promising candidates for combination therapy. The review also highlights clinical trials investigating the potential use of polyphenols, individually or in combination therapy, against breast cancer. This review deepens the under-standing of the mechanism of action of respective polyphenols and provides valuable insights into the potential use of polyphenols as a therapeutic strategy for TNBC, and lays the groundwork for future research in this area.

Cancer, a leading global cause of death, necessitates the exploration of safer and more effective anticancer drugs due to the adverse side effects associated with current cytotoxic treatments. Quinazoline and its derivatives have emerged as a promising class of drugs with demonstrated efficacy against diverse tumor types. In light of these advancements, this comprehensive review aims to outline recent developments in the utilization of quinazoline derivatives as anticancer agents. Additionally, the article offers valuable insights into the potential for novel quinazoline derivatives to serve as future anticancer drugs. By delving into the structure‐activity relationship study, this review equips researchers with a thorough understanding necessary for designing a substantial number of impactful quinazoline compounds, which hold great potential in the treatment of various life‐threatening disorders. [ABSTRACT FROM AUTHOR]

Cisplatin-based chemotherapy is a common regimen for bladder cancer, a life-threatening cancer with more than 500,000 new cases worldwide annually. Like many other metallodrugs, cisplatin causes severe side effects for its general toxicity. Organoruthenium is known for its structural stability, good anticancer activity, and possible low general toxicity. Here, we have prepared and characterized a series of water-soluble ruthenium-arene complexes with N,N′-chelating ligands: [Ru(II)-η6-arene-(4,4′-(X)2-2,2′-bipyridine)Cl]Cl (arene = p-cymene, X = C4H9 (1), COOH (2), COOCH3 (3), COOC2H5 (4); arene = benzene, X = C4H9 (5), COOCH3 (6), COOC2H5 (7)). These complexes are carefully characterized using single-crystal X-ray diffraction, UV-vis, IR, 1H NMR, and MALDI-TOF MS spectroscopy. Their DFT-calculated structural and thermodynamic properties are consistent with the experimental observations. Biophysicochemical studies of complex interaction with CTDNA and BSA supported by molecular docking simulations reveal suitable properties of 1–7 as anticancer agents. Cytotoxicities of 1–7 are evaluated on healthy human MCF-10a-breast epithelial and African green monkey Vero cells, and carcinoma human HepG-2-hepatic, T24-bladder, and EAhy-926-endothelial cells. All complexes exhibit much higher cytotoxicity for T24 than cisplatin. Particularly, 1 and 2 are also highly selective toward T24. Fluorescence imaging and flow cytometry demonstrate that 1 and 2 penetrate T24 cell membrane and induce early apoptosis at their respective IC50 concentrations, which ultimately lead to cell death. Statistical analysis suggests that the order of importance for T24 cell antiproliferation is protein binding, Log p, Ru–Cl bond length, while DNA binding is the least important. This study is the first to report the anti-bladder cancer efficacy of Ru-arene-2,2′-bipyridine complexes, and may provide insights for rational design of organoruthenium drugs in the enduring search for new chemotherapeutic agents. [ABSTRACT FROM AUTHOR]

Background: Syzygium aromaticum, also known as clove, and its essential oil has already been proved to have antioxidant, anti-inflammatory and anticancer properties. Clove is used in various foods owing to its potent antimicrobial and antioxidant properties. Essential oil extracted from clove has been used in traditional medicine for treating various ailments. Results: In silico analysis predicted that phytochemicals of clove have good interactions with the apoptosis related proteins of breast cancer. In vitro assay confirmed the cytotoxic effect of the synthesized CL-AgNPs on breast cancer cells using the MCF-7 cell line with the IC50 value of 58.64 μg/ml. Conclusion: In vitro analysis of the anticancer activity of CL-AgNPs in MCF-7 cell line supports the in silico study by proving active interactions between the phytochemicals of clove and target proteins of the breast cancer and hence Syzygium aromaticum has been proved to possess potential anticancer property. Further research is needed to consider clove-silver nanoparticles as a novel drug for treating breast cancer. [ABSTRACT FROM AUTHOR]

Background: Green silver nanoparticles offer a reliable and secure alternative to drugs and prevent cancer. The floral part of Clitoria ternatea is traditionally well known for its application as a medicine and food in various cultures around the world. Phytochemicals of these floral extracts are enriched with various properties. Floral extracts can be utilized as an alternative that can target the proteins and other molecules involved in the progression of cancer. Methods: Silver nanoparticles (CT-AgNPs) were synthesized from the extracts of blue flowers of Clitoria ternatea (CT). The synthesized CT-AgNPs were characterized by various physicochemical methods that revealed the size, shape, and stability of the nanoparticles. Docking was performed between the phytocompounds of Clitoria ternatea and apoptotic proteins involved in breast cancer such as APAF-1, BCL-2, and BAX, to determine the ability of phytocompounds present in the floral extract to control breast cancer by binding to the targets. Results: Based on the docking results, the binding energies ranged from -6.2 Kcal/mol to -7 Kcal/mol with Quercetin having the highest binding energies. Toxicity analysis of CT-AgNPs in Artermia nauplii and Vigna radiata seedlings confirmed that these nanoparticles were not toxic to both the model systems. Free radical scavenging activity assay revealed the antioxidant nature of CT-AgNPs was similar to that of standard ascorbic acid. In vitro cytotoxicity analysis using MCF-7 breast cancer cell lines revealed that CT-AgNPs were cytotoxic. Conclusion: In vitro antioxidant and cytotoxicity analysis using MCF-7 breast cancer cell lines revealed that CT-AgNPs were potent antioxidant and cytotoxic, correlating with the results of in silico analysis and hence demonstrating the anticancer potential of Clitoria ternatea floral mediated nanoparticles. [ABSTRACT FROM AUTHOR]

Numerous chemical compounds used in cancer treatment have been isolated from natural herbs to address the ever-increasing cancer incidence worldwide. Therein is icariin, which has been extensively studied for its therapeutic potential due to its anti-inflammatory, antioxidant, antidepressant, and aphrodisiac properties. However, there is a lack of comprehensive and detailed review of studies on icariin in cancer treatment. Given this, this study reviews and examines the relevant literature on the chemopreventive and therapeutic potentials of icariin in cancer treatment and describes its mechanism of action. The review shows that icariin has the property of inhibiting cancer progression and reversing drug resistance. Therefore, icariin may be a valuable potential agent for the prevention and treatment of various cancers due to its natural origin, safety, and low cost compared to conventional anticancer drugs, while further research on this natural agent is needed. [ABSTRACT FROM AUTHOR]

The near‐infrared (NIR) light‐absorbing AgBiS2 nanoparticles can be excited by single‐wavelength light, which is the primary characteristic of a photo responsive platform. Chemical synthesis of nanomaterials inevitably requires long‐chain organic surfactants or polymers to stabilize them in the nano regime. These stabilizing molecules barricade the interaction of nanomaterials with biological cells. We have produced stabilizer‐free (sf‐AgBiS2) and polymer‐coated (PEG‐AgBiS2) nanoparticles; and assessed their NIR mediated anticancer and antibacterial activity to evaluate the effect of stabilizers. sf‐AgBiS2 showed better antibacterial activity against Gram‐positive Staphylococcus aureus (S. aureus) and displayed excellent cytotoxicity against HeLa cells and live 3‐D tumour spheroids compared to PEG‐AgBiS2 both in presence and absence of NIR radiation. The photothermal therapy (PTT) results illustrated the tumour ablation ability of sf‐AgBiS2, which converted light into heat effectively up to 53.3 °C under NIR irradiation. This work demonstrates the importance of synthesizing stabilizer‐free nanoparticles to produce safe and highly active PTT agents. [ABSTRACT FROM AUTHOR]

In the treatment of bacterial contamination, the problem of multi-drug resistance is becoming an increasingly pressing concern. Nanotechnology advancements enable the preparation of metal nanoparticles that can be assembled into complex systems to control bacterial and tumor cell growth. The current work investigates the green production of chitosan functionalized silver nanoparticles (CS/Ag NPs) using Sida acuta and their inhibition efficacy against bacterial pathogens and lung cancer cells (A549). Initially, a brown color formation confirmed the synthesis, and the chemical nature of the synthesized NPs were examined by UV-vis spectroscopy, Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM) coupled with energy dispersive spectroscopy (EDS), and transmission electron microscopy (TEM). FTIR demonstrated the occurrence of CS and S. acuta functional groups in the synthesized CS/Ag NPs. The electron microscopy study exhibited CS/Ag NPs with a spherical morphology and size ranges of 6–45 nm, while XRD analysis demonstrated the crystallinity of Ag NPs. Further, the bacterial inhibition property of CS/Ag NPs was examined against K. pneumoniae and S. aureus, which showed clear inhibition zones at different concentrations. In addition, the antibacterial properties were further confirmed by a fluorescent AO/EtBr staining technique. Furthermore, prepared CS/Ag NPs exhibited a potential anti-cancer character against a human lung cancer cell line (A549). In conclusion, our findings revealed that the produced CS/Ag NPs could be used as an excellent inhibitory material in industrial and clinical sectors. [ABSTRACT FROM AUTHOR]

In this study, the biological activities of whole herb extract of a medicinal plant named Smirnovia Iranica were investigated. The extraction was performed using Supercritical CO2 and phytochemical compounds, total phenolic content (TPC), total flavonoid content (TFC), antioxidant, anti-bacterial, and anti-cancer effect were determined in the extract. Based on the results, high TPC concentration (120.36 mg GAE/100 g FW) and TFC (17.41 mg quercetin/100g FW) were obtained in the extract. Besides, the extract showed significant antioxidant activity (IC50=53.97 µg mL-1). Moreover, the extract showed a notable inhibitory effect against Escherichia coli (MIC=15.63 mg mL-1) and Salmonella enterica (MIC=31.25 mg mL-1). On the other hand, this extract showed the cytotoxic effect on glioblastoma cancer cell lines in the MTT assay. This is the first, yet comprehensive, scientific report about the chemical composition and pharmacological properties of the extract of Smirnovia Iranica whole herb. According to current results, the Smirnovia Iranica extract has excellent antioxidant properties for application as bioactive components for various objects such as as food supplements. The experiment confirmed the efficacy of the extracts as natural antimicrobials and suggested the possibility of employing them in drugs for the treatment of infectious diseases caused by the test organisms. [ABSTRACT FROM AUTHOR]

Background: Acute lymphoblastic leukemia represents a great crusader of death for children globally. Aspergillus niger is the source of the L-asparaginase enzyme from various soil environments. Similar to the human L-asparaginase enzyme. L-asparaginase enzyme in bacteria, commonly produced by Erwinia chrysanthemum or Escherichia coli, is currently used for acute lymphoblastic leukemia management and to reduce carcinogenic acrylamide creation during food preparation. Study Objectives: Manufacture of fungal L-asparaginase enzyme as an antineoplastic factor. Methodology: In the current study, fungal Lasparaginase was produced on mineral asparagine agar (MAM) selective medium (only fungi that utilize asparagine as a sole source for carbon and nitrogen can grow on it) at PH 6.5, temperature 250C, and incubation for 3 days. Malt agar medium was used for sub-culturing fungal L-asparaginase-producing strains. The biological activity and cytotoxicity activity were obstinate through nessleriazation and MTT[(dimethylthiazol-2-yl) diphenyl tetrazonium] assays respectively. Results: L-asparaginase in fungi showed high potency and bioavailability as an anticancer agent. According to morphological and biochemical tests and DNA blot hybridization, the major fungal isolate producing this enzyme was Aspergillus niger. The molecular mass was 65 KDa as discovered aside from a mass spectrometer. Vmax of 163.8 UML−1 min−1 and a Km value of 3.41 × 10−3 M were displayed via L-asparaginase. Conclusion: This was a promising approach study and fungal L-asparaginase was generated without hypersensitivity reactions and glutaminase-like effects with superior bioactivity to bacteria. [ABSTRACT FROM AUTHOR]

Abstract The study’s goal was to look into the protective properties of quercetin (QU) in natural form and QU nanoparticles-loaded chitosan nanoparticles (QU-CHSNPs) against cardiotoxicity. The ionotropic gelation approach was adopted to form QU-CHSNPs. The characterizations were performed using advanced techniques. In vitro, the release profile of QU was studied. Cardiotoxicity was induced by doxorubicin (DOX) and protected via concurrent administration of QU and QU-CHSNPs. The heart's preventive effects of QU and QU-CHSNPs were manifested by a decrease in elevated serum activities of cardiac enzymes, as well as an improvement in the heart's antioxidant defence system and histological changes. The findings substantiated QU-CHSNPs' structure with an entrapment efficiency of 92.56%. The mean of the zeta size distribution was 150 nm, the real average particle size was 50 nm, and the zeta potential value was − 27.9 mV, exhibiting low physical stability. The percent of the free QU-cumulative release was about 70% after 12 h, and QU-CHSNPs showed a 49% continued release with a pattern of sustained release, reaching 98% after 48 h. And as such, QU and QU-CHSNPs restrained the induced cardiotoxicity of DOX in male Wistar rats, with the QU-CHSNPs being more efficient.