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Objective: Microbial infections and the cancer are the biggest health concerns now days. It has been reported that 19.3 million new cancer cases and approximately 10 million deaths occurred due to cancer. The pyrimidine and their derivatives have been investigated a lot by the researchers due to their versatile chemotherapeutic effects. The unmet demand for the new antimicrobial and anticancer chemotherapeutic agents and the versatile pharmacological applications of pyrimidine derivatives prompted us to perform the synthesis and biological assessment of some novel 3-(substitued)-6-(substituted)pyrimidin-2-yl)-2-phenylthiazolidin-4-one. Methods: As a part of or investigation to find out some novel antimicrobial and anticancer agents, in this paper we focused on the synthesis of some novel 3-(substitued)-6-(substituted)pyrimidin-2-yl)-2-phenylthiazolidin-4-one derivatives. Additionally, the compounds were screened virtually for the drug likeness properties and characterized by FT-IR and NMR. Antimicrobial and anticancer studies were performed using the methods of disc diffusion, macro dilution and MTT assay. Results and Discussion: The virtual screening results revealed that all the compounds were found under the zone of inhibition for an active drug molecule. It was observed that the analytical data strongly supported the structure of the aimed compounds. Among all the synthesized compounds, the compounds (IX–XII), (XIV–XVI) were possessed very good antimicrobial effects. Some of these members represented even better antimicrobial potential against some specific pathogens. The compound (XII) was observed to be the most active compound of the series against almost all bacterial pathogens. The MTT findings revealed that the compounds (III), (IX), (X), (XII) were possessed similar IC50 to the reference drug doxorubicin. Conclusions: The antimicrobial and anticancer findings were promising and it was believed that further studies with these compounds aiming in vivo analysis will be helpful in producing the novel antimicrobial and anticancer agents. [ABSTRACT FROM AUTHOR]

This review paper provides a comprehensive overview of recent advancements in the synthesis, reactivity, and applications of N-isoindoline-1,3-dione heterocycles. These aromatic compounds, characterized by an isoindoline nucleus and carbonyl groups at positions 1 and 3, have gained significant attention for their potential use in diverse fields such as pharmaceutical synthesis, herbicides, colorants, dyes, polymer additives, organic synthesis, and photochromic materials. The review focuses on the period from 2015 to 2024, highlighting the diverse synthetic strategies employed to access N-isoindoline-1,3-diones derivatives. This review discusses the innovative methodologies and transformations that have enabled the efficient construction of these compounds with various substitution patterns. Furthermore, the reactivity of N-isoindoline-1,3-diones and their potential applications in different fields are explored. The paper emphasizes the importance of understanding the structure–activity relationships and biological properties of N-isoindoline-1,3-dione derivatives, with the aim of unlocking their potential as therapeutic agents. Additionally, the review underscores the need for sustainable and environmentally friendly synthetic approaches in this field. [ABSTRACT FROM AUTHOR]

This paper reports various types of cancer, their incidence, and prevalence all over the globe. Along with the discovery of novel natural drugs for cancer treatment, these present a promising option which are eco-friendly, safe, and provide better acceptability in comparison to synthetic agents that carries multiple side effects. This paper provides an idea about various nanocarriers and phytochemicals, along with how their solubility and bioavailability can be enhanced in nanocarrier system. This report combines the data from various literature available on public domain including PubMed on research articles, reviews, and along with report from various national and international sites. Specialized metabolites (polyphenols, alkaloids, and steroids etc) from medicinal plants are promising alternatives to existing drugs. Studies have suggested that the treatment of cancer using plant products could be an alternative and a safe option. Studies have shown with the several cell lines as well as animal models, that phytomolecules are important in preventing/treating cancer. Phytochemicals often outperform chemical treatments by modulating a diverse array of cellular signaling pathways, promoting cell cycle arrest, apoptosis activation, and metastatic suppression, among others. However, limited water solubility, bioavailability, and cell penetration limit their potential clinical manifestations. The development of plant extract loaded nanostructures, rendering improved specificity and efficacy at lower concentrations could prove effective. Nanocarriers, such as liposomes, nanostructured lipids, polymers, and metal nanoparticles, have been tested for the delivery of plant products with enhanced effects. Recent advances have achieved improvement in the the stability, solubility, bioavailability, circulation time, and target specificity by nanostructure-mediated delivery of phytochemicals. Nanoparticles have been considered and attempted as a novel, targeted, and safe option. Newer approaches such as phyto-nanocarriers with carbohydrates, lignin, and polymers have been considered even more selective and effective modes of drug delivery in biomedical or diagnostic applications. [ABSTRACT FROM AUTHOR]

Anticancer chemotherapeutics are effective weapons for cancer therapy, but the continuous emergency of multidrug-resistant cancer and the side effects of current available anticancer chemotherapeutics are the major obstacles in the control and eradication of cancers. Pyrrolo[2,3-d]pyrimidines could inhibit signal transduction cascades affecting cell proliferation, migration, and angiogenesis, representing privileged scaffolds for the discovery of novel anticancer candidates. This review highlighted the recent developments of pyrrolo[2,3-d]pyrimidines with anticancer potential and discussed mechanisms of action, covering papers published from 2018 to present, to facilitate further rational design of more effective candidates. [ABSTRACT FROM AUTHOR]

Sesamol (SM), a well-known component isolated from sesame seeds (Sesamum indicum), used in traditional medicines in treating numerous ailments. However, numerous molecular investigations revealed the various mechanisms behind its activity, emphasizing its antiproliferative, anti-inflammatory, and apoptosis-inducing properties, preventing cancer cell spread to distant organs. In several cells derived from various malignant tissues, SM-regulated signal transduction pathways and cellular targets have been identified. This review paper comprehensively describes the anticancer properties of SM and SM-viable anticancer drugs. Additionally, the interactions of this natural substance with standard anticancer drugs are examined, and the benefits of using nanotechnology in SM applications are explored. This makes SM a prime example of how ethnopharmacological knowledge can be applied to the development of contemporary drugs. [ABSTRACT FROM AUTHOR]

Cancer, caused by the failure of the mechanism that controls cell growth and proliferation, is usually associated with severe health issues. Nowadays, chemotherapy still occupies an important place in clinical cancer treatment, but the multidrug resistance and low specificity of chemotherapeutics are the major obstacles that undermine effective cancer treatment. Pyrazole and pyrimidine/fused pyrimidine can be rewarded with significant anticancer activity and tampered with in a range of places whereby some of their derivatives have received approval to treat cancer. Notably, pyrazole-pyrimidine/fused pyrimidine hybrids, blending of pyrazole and pyrimidine/fused pyrimidine pharmacophores into in a new chemical entity, can act on different targets simultaneously in cancer cells and possess potent in vitro and in vivo activity against both drug-sensitive and drug-resistant cancers. Moreover, several pyrazole-pyrimidine/fused pyrimidine hybrids which are exemplified by ruxolitinib (pyrazole-pyrrolo[2,3-d]pyrimidine hybrid) have already applied in clinics for cancer therapy, demonstrating pyrazole-pyrimidine/fused pyrimidine hybrids are pharmacologically significant scaffolds for the exploration of novel anticancer agents. This review aims to shed light on the recent developments of pyrazole-pyrimidine/fused pyrimidine hybrids with anticancer potential, and their structure-activity relationships as well as mechanisms of action are also discussed, covering papers published from 2019 to present, to facilitate further rational design of more effective candidates. [ABSTRACT FROM AUTHOR]

Metal organic frameworks (MOFs) have received a lot of attention in the research community due to their unique physical properties, which make them ideal materials for targeted drug delivery systems. In this paper, we describe the synthesis of a non-toxic La-based MOF with 3,4-dihydroxycinnamic acid (3,4-DHCA) as a linker. Scanning electron microscopy (SEM), transmission electron microscopy (TEM), energy dispersive spectroscopy (EDS), fourier transform infrared (FTIR) spectroscopy, thermogravimetric analysis (TGA), nitrogen adsorption–desorption measurements, and X-ray powder diffraction (XRD) have all been used to characterize it thoroughly. The La-based MOF showed good biocompatibility with the human breast cancer cell line MDA-MB-468. The ability of 3,4-DHCA to treat MDA-MB-468 cells was confirmed by 40.35% cell viability with La-based MOF. Based on the findings, La-based MOF can be recommended as a promising candidate for anticancer delivery. [ABSTRACT FROM AUTHOR]

Resistance to antibiotics is on the rise, and its indiscriminate usage has resulted in human and animal management constraints. In the research for an innovative treatment to diminish antimicrobial resistance, lactic acid bacteria (LAB) throw light on diminishing this problem in public health. As a result, this paper looked at the efficacy of LAB isolates and their active metabolites to combat pathogens, reduce antibiotic use in clinical settings, and explore the anticancer potential of 8 strains of LAB isolated from dairy products. Antifungal and antibacterial potential of LAB isolates against selected crop pathogenic fungi and food pathogenic bacteria had been estimated. Results revealed that all isolates exert antioxidant efficacy relating to DPPH, NO scavenging ability, reducing power, superoxide anion, hydroxyl radical, and anti-lipid peroxidation potential. Additionally, 12B isolate exert the highest anticancer upshot with IC50 values of 43.98 ± 0.4; 36.7 ± 0.6, 43.1 ± 0.8, and 35.1 ± 0.3 μg/ml, versus Caco-2, MCF-7, HepG-2, and PC3 cell lines respectively, whereas 13B isolate significantly had the highest selectivity index between peripheral blood mononuclear cells (PBMCs) and the tested human cancer cell lines compared to 5-fluorouracil. 13B was the most apoptosis-dependent death inducer for all human cancer cell lines besides exerting the lowest percentage of apoptosis against PBMCs suggesting its safety against PBMCs. The most promising strains 12B and 13B were identified by 16S rRNA sequencing as Lactiplantibacillus plantarum ESSG1 (MZ683194.1) and Lactiplantibacillus pentosus ESSG2 (MZ683195.1). LAB and their extracts are superb substitutive, safe, and efficient antimicrobial, antioxidant, and antitumor curative agents. [ABSTRACT FROM AUTHOR]

The search for new bioactive compounds with innovative modes of action and chemistry are desperately needed to tackle the increased emergence of drug-resistant microbes. With this view, this paper was conducted for the isolation, identification, and biological evaluation of fungal endophytes of eleven different plant species. A total of 69 endophytic strains were isolated and tested for the presence of bioactive metabolites with antifungal, antibacterial, anticancer, and antioxidant properties in their extracts. Upon screening, two promising strains were found to have all the before-mentioned activities. These strains were Aspergillus sydowii isolated from the bark of Ricinus communis and Aspergillus flavus isolated from the twigs of Psidium guajava. Major compounds present in extracts of the two strains were identified by GC-Mass analyses. Several well-known bioactive compounds as well as unreported ones were identified in the fungal extracts of the two strains. Furthermore, gamma irradiation (at 1000 Gy) of the fungal cultures resulted in improved bioactivities of extracts from the two strains. These findings recommend the two fungal strains as sources of antimicrobial, anticancer, and antioxidant compounds which may aid in the development of novel drugs. The presented research also explains the high-value of fungal endophytes as untapped sources of bioactive metabolites. Keypoints: Discovery of two promising fungal endophytes with divers' range of bioactivities Extracts of the two strains showed antimicrobial, anticancer, and antioxidant activities Exposure to gamma rays at 1000 Gy significantly enhanced all the bioactivities. [ABSTRACT FROM AUTHOR]

In this paper, a new Schiff base was synthesized via the condensation reaction between 3-methyl-4-amino-5-mercapto-1,2,4 triazole and 2-hydroxy-1-naphthaldehyde. Also, the Cu(II) and Ag(I) complexes were synthesized. Besides, the CuO and Ag nanoparticles were synthesized via thermal decomposition of Cu(II) and Ag(I) complexes at 800 °C. The products were characterized using various techniques such as FT-IR, 1HNMR, elemental microanalysis, UV–Vis spectrophotometer, mass spectrophotometry, magnetic susceptibility measurements, molar conductance measurements, ESR, thermal analysis (TGA and DSC), XRD, FE-SEM, and HR-TEM. The average crystallite size of CuO and Ag nanoparticles is 55.61 and 52.07 nm, respectively. The direct band gap of the CuO and Ag samples is 2.95 and 3.20 eV, respectively. The synthesized nanoparticles were utilized as photocatalysts for the degradation of methylene blue dye in aqueous media. The % degradation of methylene blue dye (MB) is 94.25% within 20 min and 90.42% within 210 min in case of utilizing (CuO + H2O2 + UV) and (Ag + H2O2 + UV), respectively. The products were tested for studying their antimicrobial activities against some bacterial and fungal strains. The synthesized complexes and their nanoparticles show moderate activity against Escherichia coli and Staphylococcus aureus bacterial strains. All the products showed no activity against Aspergillus flavus and Candida albicans fungal strains. Also, the synthesized compounds were screened for studying their cytotoxic activity against the human breast cancer cell line (MCF-7). The results revealed that the Cu(II) complex could be nominated as a potential anticancer agent because it showed a cytotoxic activity (IC50 = 7.33 ± 0.6 μg/mL) nearly equal to that of cisplatin drug (IC50 = 5.71 μg/mL). [ABSTRACT FROM AUTHOR]

In this paper, we present a simple and feasible drug self-assembled delivery system with pH responsiveness and targeting function for cancer therapy. The drug delivery system is composed of an anticancer drug and an amphiphilic random copolymer based on phenylboronic acid, galactose, and polyethylene glycol monomethyl ether acrylate molecules and achieved through reversible addition–fragmentation chain transfer polymerization. The micelles present targeting function by introducing galactose molecules and show pH sensitivity on the basis of the interactions between phenylboronic acid and galactose molecules. Particle size, transmission electron microscopy, and drug release assays show the pH-responsive behavior of micelles at pH 6.0. Cellular uptake assay demonstrates that micelles can internalize HepG2 cells via receptor-mediated interaction. In addition, the drug-loaded micelles can considerably inhibit cancer cell proliferation as indicated by in vivo antitumor assay. The synthesized micelles may facilitate the development of valid drug delivery systems for cancer therapy. [ABSTRACT FROM AUTHOR]

Clitoria ternatea or commonly known as 'Butterfly pea' has been used traditionally in Ayurvedic medicine in which various parts of the plants are used to treat health issues such as indigestion, constipation, arthritis, skin diseases, liver and intestinal problems. The flowers of C. ternatea are used worldwide as ornamental flowers and traditionally used as a food colorant. This paper reviews the recent advances in the extraction and biological activities of phytochemicals from C. ternatea flowers. The application of maceration or ultrasound assisted extraction greatly increased the yield (16–247% of increase) of phytochemicals from C. ternatea flowers. Various phytochemicals such as kaempferol, quercetin and myricetin glycosides as well as anthocyanins have been isolated from C. ternatea flowers. Clitoria ternatea flower extracts were found to possess antimicrobial, antioxidant, anti-inflammatory, cytotoxic and antidiabetic activities which are beneficial to human health. Clitoria ternatea flower is a promising candidate for functional food applications owing to its wide range of pharmacotherapeutic properties as well as its safety and effectiveness. [ABSTRACT FROM AUTHOR]

Plumbago zeylanica L. (Plumbaginaceae) commonly known, as chitrak is pharmacologically important plant. Various studies have been undertaken to assess the pharmacological potential of different parts of the plant namely like roots, stem, flower, and leaves as antimicrobial, hepatoprotective, anticancer, antifertility, antiulcer, antifungal and wound healing. The intention of the present review is to deliver a concise account on its ethnobotanical uses, phytochemistry with an in-depth study of its phytoconstituents, facts and prospects of its potential pharmacological activities of this golden plant. An extensive literature survey was undertaken through different online platforms viz. Google Scholar and online databases namely PubMed, Science Direct and Springer. All papers based on traditional medicinal uses and pharmacological properties were included. Sixty three research articles and review articles were found to be apt for inclusion into the review. About 150 articles were retrieved for the purpose. The elaborative results vindicated that Plumbago zeylanica L. holds significant prospects in major health conditions such as diabetes, cardiovascular disorders, ulcer, liver problems, obesity, wound healing, cancer etc. [ABSTRACT FROM AUTHOR]

Currently, the development of anticancer drug resistance is significantly restricted the clinical efficacy of the most commonly prescribed anticancer drug. Malignant disease is widely prevalent and considered to be the major challenges of this century, which concerns the medical community all over the world. Consequently, investigating small molecule antitumor agents, which could decrease drug resistance and reduce unpleasant side effect is more desirable. 2-aminothiazole scaffold has emerged as a promising scaffold in medicinal chemistry and drug discovery research. This nucleus is a fundamental part of some clinically applied anticancer drugs such as dasatinib and alpelisib. Literature survey documented that different 2-aminothiazole analogs exhibited their potent and selective nanomolar inhibitory activity against a wide range of human cancerous cell lines such as breast, leukemia, lung, colon, CNS, melanoma, ovarian, renal, and prostate. In this paper, we have reviewed the progresses and structural modification of 2-aminothiazole to pursuit potent anticancers and also highlighted in vitro activities and in silico studies. The information will useful for future innovation. [ABSTRACT FROM AUTHOR]

Titanocenes are gradually proven to possess good anticancer activity. In this paper, we present a theoretical study of some properties of six promising anticancer titanocenes synthesized by the Tacke research group. The structural and electronic properties of the complexes have been investigated herein using the density functional theory (DFT) and the time-dependent DFT (TD-DFT) associated with a mixed basis sets comprising the 6-31 + G(d,p) basis set for C, H, and O atoms and the 6-31G(d) basis sets for the Ti4+ and Cl− ions. According to the results from topological analysis, even though there are strong Ti–C interactions in all complexes studied, the cyclopentadienyl derivatives are not covalently linked to the central Ti4+ ion through all of their carbon atoms. In addition, the Ti–Cl is the strongest metal-ligand bond. From the analyses of electronic spectra, it turns out that the complexes studied strongly absorb in the UV region of the electromagnetic spectrum and that the transitions are mainly LMCT, LLCT, and ILCT character. Our results are undoubtedly vital for further studies on the structure-activity relationship and mechanisms of interaction between the investigated titanocenes and DNA. [ABSTRACT FROM AUTHOR]

Severe durable changes may occur to the DNA structure caused by exogenous and endogenous risk factors initiating the process of carcinogenesis. By evidence, a large portion of malignancies have been demonstrated as being preventable. Moreover, the targeted prevention of cancer onset is possible, due to unique properties of plant bioactive compounds. Although genoprotective effects of phytochemicals have been well documented, there is an evident lack of articles which would systematically present the spectrum of anticancer effects by phytochemicals, plant extracts, and plant-derived diet applicable to stratified patient groups at the level of targeted primary (cancer development) and secondary (cancer progression and metastatic disease) prevention. Consequently, clinical implementation of knowledge accumulated in the area is still highly restricted. To stimulate coherent co-development of the dedicated plant bioactive compound investigation on one hand and comprehensive cancer preventive strategies on the other hand, the current paper highlights and deeply analyses relevant evidence available in the area. Key molecular mechanisms are presented to detail genoprotective and anticancer activities of plants and phytochemicals. Clinical implementation is discussed. Based on the presented evidence, advanced chemopreventive strategies in the context of 3P medicine are considered. [ABSTRACT FROM AUTHOR]

The gold nanoparticles (AuNPs) were synthesized via the Turkevich-Frens approach, conjugated with polyphenol moieties named quercetin (Qu), and prepared as Au-Qu NPs. In this study, we investigated the anticancer activity of the Au-Qu NPs through an apoptosis assay and a live/dead staining assay. The cell viability and apoptosis studies of the synthesized AuNPs and Au-Qu NPs were investigated on mouse embryonic fibroblast cells (NIH/3T3) and human cervical cancer cell lines (HeLa). Interestingly, minimal cytotoxicity was observed in 3T3 cells. Also, an apoptosis assay was conducted using the flow cytometry approach to investigate the cell death in both 3T3 and HeLa cells after the treatment of AuNPs and Au-Qu NPs using Annexin-FITC and propidium iodide (PI) dyes. The apoptosis studies were performed in both 3T3 and HeLa cells, and the Au-Qu NPs exhibited a reasonably increased apoptosis of 34.5% in HeLa cells as compared to AuNPs in HeLa cells (32.2%). Thus, the Au-Qu NPs are more suitable for investigating anticancer properties than AuNPs. In addition, Au-Qu NPs are displaying less early apoptosis (40.5%) than AuNPs (54.7%) in 3T3 cells, which suggests that Au-Qu NPs are biocompatible in healthy cells. The live/dead assay results obtained in 3T3 and HeLa cells in a time-dependent manner (0, 6, 12, and 24 h) have demonstrated the potential cell viability and cell toxicity in response to AuNPs and Au-Qu NPs. [ABSTRACT FROM AUTHOR]

The present investigation aimed to determine the effectiveness of bioactive components extracted from Hom herbs (Strobilanthes cusia (Nees) Kuntze) using the solvent-free microwave-assisted extraction (MAE) method. The obtained bioactive components were analyzed for total phenolic content (TPC) and active ingredient content. The Hom extracts were examined for antioxidant, antibacterial, anti-inflammatory, cytotoxic, and anticancer activities. The comparative analysis of extraction methods MAE was studied by using different solvents such as ethanol (EtOH), 50% ethanol (50EtOH) and distilled water (DW). The results obtained by the MAE method with DW as solvent show the TPC of 104.41±1.36 mg GAE/g crude and tryptanthrin 0.1138±0.0014 mg/g crude and indigo 0.0622±0.0015 mg/g crude. Comparatively, values ​​detected in the 50% EtOH extract were not significantly different at the 95% confidence level. At the same time, levels of indirubin were detected at levels equivalent to that of ethanol extracts. The DW extract from MAE had an IC50 value against the DPPH scavenging assay of 0.1927±0.0756 mg/ml, comparable to the test results of extracts of ethanol and 50% ethanol. The bioactive extracted using the MAE with water as solvent had minimum inhibitory concentration (MIC) and could suppress infection at 10 mg/disc. It was also observed that the extracts from the conventional extraction technique using ethanol as the solvent continued to be highly effective against Bacillus cereus even after employing the EtOH or 50% EtOH. Hom extract's MIC value representing inhibiting B. cereus was 0.625 mg/disc. Still, EtOH-extracted Hom demonstrated the highest cytotoxicity against 16HBEo- by reducing cell survival rate by less than 50% while the others did not. Interestingly, Hom that had been extracted using 50EtOH and DW with MAE had an anticancer impact on A549 by reducing the survival rate in a dose-dependent manner. [ABSTRACT FROM AUTHOR]

Bioconjugation is one of the most promising strategies to improve drug delivery, especially in cancer therapy. Biomolecules such as bile acids (BAs) have been intensively explored as carriers, due to their peculiar physicochemical properties and biocompatibility. BAs trafficking is regulated by intracellular lipid-binding proteins and their transport in the liver can be studied using chicken liver Bile Acid-Binding Proteins (cL-BABPs) as a reference model. Therefore, we conceived the idea of developing a BA-conjugate with Mirin, an exonuclease inhibitor of Mre11 endowed with different anticancer activities, to direct its transport to the liver. Following computational analysis of various BAs in complex with cL-BABP, we identified cholic acid (CA) as the most promising candidate as carrier, leading to the synthesis of a novel bioconjugate named CA-M11. As predicted by computational data and confirmed by X-ray crystallographic studies, CA-M11 was able to accommodate into the binding pocket of BABP. Hence, it can enter BAs trafficking in the hepatic compartment and here release Mirin. The effect of CA-M11, evaluated in combination with varying concentrations of Doxorubicin on HepG2 cell line, demonstrated a significant increase in cell mortality compared to the use of the cytotoxic drug or Mirin alone, thus highlighting chemo-sensitizing properties. The promising results regarding plasma stability for CA-M11 validate its potential as a valuable agent or adjuvant for hepatic cancer therapy. [ABSTRACT FROM AUTHOR]

A novel core–shell nanocarrier system has been designed for co-delivery of a small anticancer drug, docetaxel (DTX) and tumor suppressor (TS) miR-34a named as Exo(PAN34a+DTX). The core is formed by pH dependent polyamine salt aggregates (PSA) containing both the payloads and the shell is formed by RAW 264.7 cell derived exosomal fragments. Herein, phosphate driven polyallylamine hydrochloride (PAH, MW:17,500 Da) PSA was formed in presence of miR-34a and DTX to form PAN34a+DTX. The formulation exhibited pH dependent DTX release with only 33.55 ± 2.12% DTX release at pH 7.2 and 75.21 ± 1.8% DTX release till 144 h at pH 5.5. At 1.21 molar ratio of phosphate to the amine (known as R value), efficient complexation of miR-34a (3.6 μM) in the PAN particles was obtained. PAN34a+DTX demonstrated particle size (163.86 ± 12.89 nm) and zeta-potential value of 17.53 ± 5.10 mV which upon exosomal fragment layering changed to − 7.23 ± 2.75 mV which is similar to the zeta-potential of the exosomal fragments, i.e., − 8.40 ± 1.79 mV. The final formulation Exo(PAN34a+DTX), loaded with 40 ng/mL DTX and 50 nM miR-34a exhibited 48.20 ± 4.59% cytotoxicity in triple negative breast cancer (TNBC) cells, 4T1. Co-localization of CM-DiI (red fluorescence) stained exosomal fragments and FAM-siRNA (green fluorescence) in the cytoplasm of 4T1 cells after 6 h of Exo(PANFAM) treatment confirmed the efficiency of the designed system to co-deliver two actives. Exo(PAN34a+DTX) also reduced BCL-2 expression (target gene for miR-34a) by 8.98 folds in comparison to free DTX confirming promising co-delivery and apoptosis inducing effect of Exo(PAN34a+DTX) in 4T1. [ABSTRACT FROM AUTHOR]

In the present study the authors' main goal is to avoid the corrosive attack of the chloride ions of 3.5% NaCl solution in saline medium on the mild steel (MS), by addition of small amount of a new derivative of the hydrazide called ligand (HL), as a corrosion inhibitor. This study had been achieved by employing different electrochemical measurements such as, open circuit potential (OCP), electrochemical impedance spectroscopy (EIS) and potentio-dynamic polarization (PDP) methods. The results of the electrochemical test (OCP), showed that, the open circuit potential of the mild steel in saline solution, was guided to more positive direction in presence of the ligand (HL), at its ideal concentration (1 × 10−3 M), compared to the (OCP), of the mild steel in absence of (HL). The results of the electrochemical methods, EIS and PDP presented that, the ligand (HL), was acted as a good corrosion inhibitor for hindering the corrosion process of the mild steel in 3.5% sodium chloride, as it was recorded a good percentage of the inhibition efficiency (77.45%, 53.41%, by EIS and PDP techniques respectively), at its optimum concentration (1 × 10−3 M). Also, the corrosion rate of the mild steel in the saline medium without (HL), was listed about (0.0017 mm/year), while in existence of (HL), was decreased to a value about (0.00061 mm/year). As well, some of electrical properties of (HL), and its derivative [Pd(II), Cr(III), and Ru(III)], complexes were investigated such as; the activation energy (Ea(ac)), which recorded values in the range of 0.02–0.44 (eV) range and electrical conductivity which listed values at room temperature in the range of 10−5–10−8 S.cm−1. The results of the AC and DC electrical conductivity measurements for (HL), and its derivative [Pd(II), Cr(III) and Ru(III)] complexes indicate semiconducting nature which suggests that these compounds could be used in electronic devices. Also, the complexes exhibited higher conductivity values than (HL). Photophysical studies showed good florescence properties of HL that indicated that it can be used to determine most of the drugs with no fluorescence properties by quenching and calculating quantum yield. Moreover, the hydrazide ligand (HL), has shown selectivity as an active anticancer candidate drug for both breast and colon cancer in humans. Density function theory demonstrated that, the frontier molecular orbital HOMOs of the complexes have exhibited similar behavior and the charge density has localized in the metallic region of all the studied complexes. Also, the values of the energy gap of the ligand (HL), and its complexes Pd(II), Cr(III) and Ru(III), had been arranged in this order HL > Cr(III) > Ru(III) > Pd(II). All characterization using different spectroscopic techniques were reported to elucidate the proposed structures such as; thermal analysis, elemental analysis of C, H, and N atoms, spectral analysis using IR, UV, 1H NMR techniques, scanning electron microscopy and energy dispersive X-ray analyses. [ABSTRACT FROM AUTHOR]

Nanoparticles (NPs) have experienced an explosive global growth as a key byproduct of nanotechnologies over the last ten years due to their remarkable physiochemical qualities. Bimetallic nanoparticles are a promising combination of two kinds of nanoparticles that often display synergetic behaviors. In the current study, a technology that is beneficial to the environment was used to biosynthesize copper oxide and gold nanoparticles (CuO@Au NPs) utilizing a fungus isolate. Using carboxymethylcellulose (CMC) and chitosan (Ch), formed nanoparticles were turned into biopolymers (nanocomposite) using a green method. CuO@Au NPs and nanocomposite qualities were investigated using physical and chemical methods including FITR and XRD, as well as topographical methods like FESEM and HRTEM. About 20 nm-diameter bimetallic NPs were identified in the nanocomposite, which was also determined to have verified nanostructures. CuO@Au NPs exhibited less antimicrobial activities with inhibition zones of 15, 27, 8, and 25 mm than nanocomposite with inhibition zones of 16, 26, 29, and 14 mm against E. coli, E. faecalis, C. albicans, A. flavus, and M. circinelloid respectively. CuO@Au NPs reflected more MIC value against S. aureus, (62.5 µg/mL), S. typhi (62.5 µg/mL), E. faecalis (31.25 µg/mL) than MIC value of nanocomposite against the same bacteria. Moreover, the MBC values of CuO@Au NPs were more (ranged from 31.25 to 125 µg/mL) than that of nanocomposite (ranged from 15.62 to 62.5 µg/mL) against tested bacteria. DPPH scavenging % indicated that nanocomposite was promising than CuO@Au NPs with IC50 value of 116.87 µg/mL and 173.34 µg/mL, respectively. Effect of CuO@Au NPs and nanocomposite on Wi38 reflected high IC50 of 585.15 ± 1.58 µg/mL and 587.14 ± 0.29 µg/mL, respectively against Wi38 cells. However, the recorded IC50 values of CuO@Au NPs were less (166.56 ± 2.91 µg/mL) than IC50 (181.8 ± 4.27 µg/mL) of the nanocomposite against MCF-7 cells. [ABSTRACT FROM AUTHOR]

Ethnomedicinal plants are thought to have better prospects of harboring endophytes that produce natural products with pharmacological activities. This study aimed to investigate the antiplasmodial and anticancer properties of secondary metabolites of endophytic fungi from three medicinal plants. The endophytic fungi included Lasiodiplodia theobromae isolated from Cola acuminata, Curvularia lunata Bv4 isolated from Bambusa vulgaris, and Curvularia lunata Eg7 isolated from Elaeis guineensis. The identification of the fungi was based on the internal transcribed spacer (ITS-rDNA) sequence. The fungi were subjected to solid-state fermentation and the secondary metabolites were extracted with ethyl acetate. In vitro antiplasmodial screening of extracts was performed using the SYBR green I-based fluorescence assay on the chloroquine-resistant Plasmodium falciparum strain DD2. The cytotoxicity of the extracts on human red blood cells and Jurkat (leukemia) cells was assessed using the tetrazolium-based colorimetric MTT assay. Gas chromatography-mass spectrometry (GC–MS) analysis was used to identify the constituents of the fungal extracts. The extract of L. theobromae showed the best antiplasmodial activity against chloroquine-resistant P. falciparum (IC50 = 5.4 µg/mL) and was not harmful to erythrocytes (CC50 > 100 µg/mL). All three fungal extracts showed a weak cytotoxic effect against Jukart cell lines (CC50 > 100 µg/mL). GC–MS analysis of the three endophytic fungal extracts revealed the presence of forty major bioactive compounds, including: oxalic acid, isobutyl nonyl ester, 2,4-di-tert-butylphenol, and hexadecanoic acid, among others. The endophytic fungi from the medicinal plants in this study were promising sources of bioactive compounds that could be further evaluated as novel drugs for the treatment of malaria caused by P. falciparum-resistant strains. [ABSTRACT FROM AUTHOR]

Background: Triple-negative breast cancer (TNBC) is an aggressive subtype of breast cancer. Radiation therapy (RT) is a modality for TNBC management. Radiosensitizers can mitigate the adverse effects of RT. Applying green-synthesized silver nanoparticles (Ag-NPs) from biological sources such as plants is a potential strategy to sensitize cancer cells to radiotherapy due to the low toxicity. Therefore, identifying novel natural sources for synthesizing stable and broadly applicable green-Ag-NPs has gained more attention in cancer therapy. In the present study, we synthesized green- Ag-NPs from pumpkin peel extract and elucidated the impact of green-synthesized Ag-NPs as a radiosensitizer in MDA-MB 231 cells (a model of TNBC). Results: The prepared Ag-NPs had a spherical shape with an average size of 81 nm and a zeta potential of − 9.96 mV. Combination of green-synthesized Ag-NPs with RT exhibited synergistic anticancer effects with an optimum combination index (CI) of 0.49 in MDA-MB-231 cells. Green-synthesized Ag-NPs synergistically potentiated RT-induced apoptosis in MDA-MB-231 cells compared to the corresponding monotherapies. Morphological features of apoptosis were further confirmed by the DAPI–TUNEL staining assay. HIF-1α expression was decreased in cells subjected to combination therapy. Bax and p53 expression increased, whereas Bcl-2 genes decreased. Combination therapy significantly increased the protein level of PERK and CHOP while decreasing cyclin D1 and p-ERK/total ERK levels compared to monotherapies. Conclusion: These findings indicate the potential effect of green-synthesized Ag-NPs as a radiosensitizer for TNBC treatment. [ABSTRACT FROM AUTHOR]

The polysaccharide (HUP-1) was fractionated and purified from crude polysaccharide of Hypsizygus ulmarius by using ion-exchange and gel-permeation chromatography. The chemical composition analysis of the HUP-1 noted 60.07% of carbohydrate, 2.22% of protein, 11.08% of uronic acid, and 4.39% of sulfate content respectively. The molecular weight of HUP-1 was 27,887 Da, and its monosaccharide composition disclosed 44.4% of mannose, 36.4% of glucose, and 19.18% of fucose. Further, the HUP-1 was examined for the structural characterization through the FTIR, 1H-NMR, 13C NMR, XRD, and SEM analysis. The HUP-1 showed the DPPH and ABTS scavenging activity were 16.38–61.60% and 21.33–85.08% at 1–5mg/ml concentration, with the EC50 values which were 4.160 and 2.245mg/ml and the significant value which was p < 0.05. The anticancer activity of HUP-1 reported 70% at 100μg/ml concentration against human lung carcinoma A549 cells. Hence, the above results of the HUP-1 showed good antioxidant and anticancer activity; it was well correlated for their molecular weight and monosaccharide composition such as mannose, glucose, and fucose. So, the good antioxidant and anticancer activity of the HUP-1 suggested that may be an effective chemotherapeutic treatment for lung cancer in the future pharmacological industry. [ABSTRACT FROM AUTHOR]

Chemotherapy plays a role in many cancer therapies, including breast cancer, but due to its significant side effects, alternate treatment approaches have been investigated. One such alternative is photodynamic therapy (PDT), which employs a combination of oxygen, a photosensitizer (PS), and light of a specific wavelength. Transition metal complexes and SBL have gained interest in PDT. In this study aimed to assess the potential antitumor activity and underlying mechanism of a newly synthesized Schiff base ligand (SBL)-mediated PDT on MCF-7 cells, comparing its efficacy to cisplatin. We synthesized and characterized two novel Pd-conjugated SBL compounds (complex-1 and 2). Following the treatment of MCF-7 cells with these compounds, a light-emitting diode (LED) was utilized to deliver a light dose of 14.8 J/cm2. In MCF-7 cells, we also looked at cytotoxicity, cell death rates, and ROS levels. Results indicated a significant increase in cytotoxicity (IC50:12.5 µM) (p < 0.05) and ROS levels (258.33%) (p < 0.05) in the group treated with complex-1-mediated PDT compared to control. The late apoptotic (29.78%) (p < 0.05) and necrotic (24.23%) (p < 0.05) cell death also increased significantly compared to the control group (1.86 ± 0.92, 1.89 ± 0.32, respectively). In conclusion, our study suggests that the complex-1 compound may serve as a promising candidate for anticancer agents in PDT for MCF-7 cells. In contrast, complex-2-mediated PDT did not demonstrate any observable anticancer activity. [ABSTRACT FROM AUTHOR]

Styphnolobium japonicum leaves are considered a rich source of flavonoids, which are the prospective basis for various therapeutic effects. However, there has been a lack of comprehensive cytotoxic studies conducted on these leaves. Therefore, this ongoing investigation aimed to detect and isolate the flavonoids present in S. japonicum leaves, and assess their antioxidant and anticancer properties. The defatted extract from S. japonicum leaves was analyzed using HPLC, which resulted in the identification of seven phenolics and six flavonoids. Rutin and quercetin were found to be the most abundant. Furthermore, a comprehensive profile of flavonoids was obtained through UPLC/ESI–MS analysis in negative acquisition mode. Fragmentation pathways of the identified flavonoids were elucidated to gain relevant insights into their structural characteristics. Furthermore, genistein 7-O-glucoside, quercetin 3-O-rutinoside, and kaempferol 3-O-α-L-rhamnopyranosyl-(1 → 6)-β-D-glucopyranosyl-(1 → 2)-β-D-glucopyranoside were isolated and characterized. The defatted extract rich in flavonoids exhibited significant antioxidant, iron-reducing, free radicals scavenging impacts, and remarkable cytotoxicity against the liver cell line (IC50 337.9μg/ mL) and lung cell line (IC50 55.0 μg/mL). Furthermore, the antioxidant and anticancer capacities of the three isolated flavonoids have been evaluated, and it has been observed that their effects are concentration-dependent. The findings of this research highlight the promising impact of flavonoids in cancer therapy. It is recommended that future scientific investigations prioritize the exploration of the distinct protective and therapeutic characteristics of S. japonicum leaves, which hold significant potential as a valuable natural resource. [ABSTRACT FROM AUTHOR]

Research into the anticancer activity of quantum-sized carbon dots (CDs) has emerged as a promising avenue in cancer research. This CDs delves into the opportunities and challenges associated with harnessing the potential of these nanostructures for combating cancer. Quantum-sized carbon dots, owing to their unique physicochemical properties, exhibit distinct advantages as potential therapeutic agents. Opportunities lie in their tunable size, surface functionalization capabilities, and biocompatibility, enabling targeted drug delivery and imaging in cancer cells. However, we include challenges, a comprehensive understanding of the underlying mechanisms, potential toxicity concerns, and the optimization of synthesis methods for enhanced therapeutic efficacy. A succinct summary of the state of the research in this area is given in this review, emphasizing the exciting possibilities and ongoing challenges in utilizing quantum-sized carbon dots as a novel strategy for cancer treatment. [ABSTRACT FROM AUTHOR]

In this study, the Ag-incorporated TiO2 nanoparticles were synthesized using Carica papaya leaf extract, intending to evaluate their potential efficacy against the MCF-7 breast cancer cell line. The physio-chemical features of the biogenic-produced Ag-TiO2 nanoparticles are investigated using several analytical techniques, including UV-Vis spectroscopy, X-ray Diffraction (XRD), Fourier-transform Infrared Spectroscopy (FTIR), Transmission Electron Microscopy (TEM), Selected Area Electron Diffraction (SAED), Field Emission Scanning Electron Microscopy (FE-SEM), Energy-dispersive X-ray Spectroscopy (EDAX), Zeta potential analysis, and Particle size analysis. The Ag-TiO2 nanoparticles exhibit a spherical morphology and possess an average diameter of 8-12 nm. Additionally, their surface is characterized by a negative charge, which contributes to their rough texture. The results of the in-vitro anticancer experiments demonstrated that the Ag-TiO2 nanoparticles (NPs) induce vacuolization in cancer cells, alter the shape of the cell nucleus, degrade nucleic acids, and arrest the synthetic phase of cancer cells in the cell cycle. The degradation capacity of pure and Ag-TiO2 NPs was also assessed in relation to the degradation of Methylene Blue (MB) dye when exposed to solar irradiation. The results indicated that 3% Ag-TiO2 shows 63% of dye decolorization within a time frame of 3 hours. Therefore, the synthesized Ag-TiO2 NPs could reduce toxicity, be eco-friendly and have exceptional utility in two distinct domains that significantly have a major impact on the environment. [ABSTRACT FROM AUTHOR]

Erlotinib is a reversible epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor that acts by inhibiting signaling pathways, resulting in the disruption of cancerous cell proliferation. Erlotinib is a promising anticancer agent mainly utilized in the mitigation of non-small cell lung cancer cells (NSCLC) and pancreatic tumor. Apart from NSCLC and pancreatic tumor, erlotinib has also been employed in different malignancies, including metastatic colorectal cancer, malignant glioma, breast cancer, gastrointestinal cancers, etc. Despite erlotinib's distinctive qualities as a targeted drug, its applications are still limited by poor solubility, variable oral bioavailability, a high daily dose requirement, large protein binding, and primitive or acquired therapeutic resistance. Nanotechnology is a favorable approach to increase therapeutic effectiveness of erlotinib. It is one of the newest scientific field directed toward the diagnosis and targeted treatment of cancer. This technology aids in the distinction between normal and malignant cells, which overlays the strategy for targeted delivery. This manuscript discussed the advances of erlotinib nanoformulations in the management of different cancers. Moreover, the manuscript also comprises various research outcomes of erlotinib nanoformulations with other therapeutic agents as combinational therapy. Erlotinib can be delivered to a precise target in the body utilizing different polymers, lipids, and metals. [ABSTRACT FROM AUTHOR]

We investigate the therapeutic potential of Aloin A and Aloin B, two natural compounds derived from Aloe vera leaves, focusing on their neuroprotective and anticancer properties. The structural differences between these two epimers suggest that they may exhibit distinct pharmacological properties. Our investigations revealed that both epimers are not stable in aqueous solution and tend to degrade rapidly, with their concentration decreasing by over 50% within approximately 12 h. These results underscore the importance of addressing issues such as the need for encapsulation into effective drug delivery systems to enhance stability. ThT fluorescence experiments showed that neither compound was able to inhibit Aβ amyloid aggregation, indicating that other mechanisms may be responsible for their neuroprotective effects. Next, an equimolar mixture of Aloin A and Aloin B demonstrated an ability to inhibit proteasome in tube tests, which is suggestive of potential anticancer properties, in accordance with antiproliferative effects observed in neuroblastoma SH-SY5Y and HeLa cell lines. Higher water stability and increased antiproliferative activity were observed by encapsulation in carbon dot nanoparticles, suggesting a promising potential for further in vivo studies. [ABSTRACT FROM AUTHOR]

In the present work, a simple and efficient stirring method was used to successfully synthesize a novel multifunctional carbon dots-drug delivery system AMP-CDs@5-Fu in the form of intertwined filaments. The results showed that AMP-CDs@5-Fu had the highest final release in the medium mimicking the physiological environment of the human small intestine compared to that of 5-Fu and that the drug release behaviors followed a zero-grade drug release within the first 3 h. The results also showed that AMP-CDs@5-Fu could be used to reduce the toxicity of 5-Fu while significantly improving the anticancer ability. In vitro hemolysis and anticancer assays showed that AMP-CDs@5-Fu could significantly improve the anticancer ability while decreasing the toxicity of 5-Fu, and the hemolysis rate of AMP-CDs@5-Fu was significantly lower than that of 5-Fu; their IC50 against 4T1 cancer cells were 201.63 ± 8.94 µg 5-Fu/mL and 241.24 ± 11.05 µg 5- Fu/mL. In addition, AMP-CDs@5-Fu allowed clear cell imaging. Therefore, AMP-CDs@5-Fu is expected to improve the bioavailability of 5-Fu as a novel oral agent with fluorescent properties and very promising as a novel fluorescence tracking drug loading system, which is expected to be used in the field of anticancer targeted therapy and fluorescence tracking to monitor the distribution of drugs. [ABSTRACT FROM AUTHOR]

Background: Carbazoles are an important class of heterocyclic aromatic compounds that contain nitrogen atom in the ring. They have a large-conjugated system, attractive "electrical and charge-transport properties", and the ability to efficiently incorporate different functional groups into the structurally inflexible carbazolyl ring. Main text: Carbazole derivative ECCA acts as an anticancer agent by reactivating the P53 molecular signaling pathway; similarly, some other derivatives of carbazole show antifungal activity by acting on the RAS-MAPK pathway. Carbazole derivatives also show their effect on inflammation by inhibiting the p38 mitogen-activated protein kinase signaling pathway by stopping the conversion of DAXX protein into ASK-1. By modifying the AKT molecular signaling pathway through boosting protein phosphatase activity in the brain, they show anti-Alzheimer's activity and also by translocating the GLUT4 these are effective against diabetes. Conclusion: After exploring the literature on carbazole, it was found that carbazole has an immeasurably great potential for the treatment of various diseases as the carbazole nucleus leads to various synthesized derivatives which are used for their pharmacological activities. So there is a need to explore carbazole for some newer drugs. [ABSTRACT FROM AUTHOR]

Background: Hepatic cancer endures a major health scourge as the consequence of a high incidence of > 1 million cases by 2025. Plant-based products are typically effective in ameliorating health conditions. Pomegranate peel extract (PE) with its high polyphenolic content has anticancer effects against different types of cancer. Herein, we aimed to maximize the PE chemotherapeutic efficacy by loading it in a suitable delivery system to overcome the limitations of PE, to control its release and to achieve liver targeting. Method: A nanoprecipitation procedure was adopted to incorporate PE into biodegradable and biocompatible natural polymeric zein (ZN)-based nanoparticles (NPs) (PE-ZN NPs). A full factorial design (22 × 31) was developed to study the effects of the formulation variables, namely pH of dispersion, PE-to-ZN ratio and surfactant concentration. Results: The optimization revealed a surfactant-free stable PE-ZN NPs formula with a small particle size of 99.5 ± 6.43 nm, high PE encapsulation efficiency % of 99.31% ± 3.64 (w/w) and controlled release of PE over 24 h. Conclusion: Moreover, the cytotoxicity of the optimum formula against hepatic cancer HepG2 cell lines was assessed and attained about a 2.5-fold reduction in the inhibitory concentration (IC50) values compared to the free PE affording a promising green platform to combat hepatic cancer. [ABSTRACT FROM AUTHOR]

Objective: It is well known that E. officinalis (Amla) has anti-oxidant, tonifying, anti-aging, detoxifying, and anti-cancer properties in addition to acting as a broad spectrum antibiotic against various infectious diseases. This wonder plant contains antioxidants which aid in the clearing of toxins from the body (The liver is where toxins are found in abundance) and may also protect the liver from the resulting damage. However, the effects of E.officinalis on normal human liver cells along with cancer human liver cells remain largely unknown. The purpose of this study is to look into the hapto-protective and anticancer effects of E. officinalis on normal as well as cancer liver cell line. Methodology: approaching the same, aqueous extract of E. officinalis fruit extract was prepared for anticancer screening. The hepatoprotective and anticancer effect of amla on cell viability, cytotoxicity and cell proliferation of normal human liver cells (Wrl-68) and cancer human liver cell (HepG2) was analyzed using trypan blue dye exclusion test, MTT & WST assay as well as by fluorescent staining with PI & DAPI. ROS and Apoptosis was analyzed by DCFDA and Annexin V/PI assay and expression of apoptosis-regulating proteins was evaluated by immunoblotting. Results: The study demonstrated that 50 μg/ml of fruit extract of E.officinalis inhibited cell viability and induced cytotoxicity, simultaneously triggers apoptosis in cancer cells by generation of intracellular ROS species in HepG2 cells without any toxic effect on normal liver cell after 48 h of incubation. Conclusion: E.officinalis fruit shows tremendous pharmacological and medicinal application along with cheap or cost effective clinical validation for the treatment of both organ specific tumors as well as for various types of leukemia. [ABSTRACT FROM AUTHOR]

Electrophilic and nucleophilic reactions of benzocaine are the most common procedures to construct a library of benzocaine derivatives, which have promising features that could be correlated with their biological activities. This critical review documents the synthesis of benzocaine and its reactions. These reactions provide structures with antimicrobial, anti-inflammatory, anticancer activities, as a result of inhibition of acetylcholine esterase, cyclooxygenase, fatty acid transport protein, and human immunodeficiency virus. Recent studies presented some bioactive modification of benzocaine as leteprinim for the treatment of neurodegenerative disorders such as Alzheimer's, Parkinson's disease, stroke and (-)-vincadifformine as antitumor. [ABSTRACT FROM AUTHOR]

In this paper, a series of bis(2,3-dihydroquinazolin-4(1 H)-one) derivatives ( 4a-i, 10a-k) were synthesized by the one-pot pseudo-five-component reaction of isatoic anhydride with aromatic aldehydes and aromatic amines under reflux in glacial acetic acid. The synthesized compounds were screened for their antioxidant properties using the DPPH radical scavenging method. Compounds 4i and 10h showed potent radical scavenging activities at 20 $$\upmu \hbox {g}/\hbox {mL}$$ compared to BHA and ascorbic acid. The anticancer activity of compound 4f was evaluated against human breast cancer cell line (MCF 7), and the observed $$\hbox {GI}_{50}$$ was found to be 11.4 $$\upmu \hbox {m}$$ . The redox behaviour of some analogues was evaluated by cyclic voltammetric methods, and it is found that compound 7d possesses the maximum redox potential. Graphical Abstract : [ABSTRACT FROM AUTHOR]

The incidence and mortality of breast cancer are growing which indicates the inefficiency of the current chemotherapy drugs. Due to the anticancer potential of Zn and Ag and the magnetic feature of iron oxide, in this work, we synthesized ZnFe2O4-Ag nanocomposite using Chlorella vulgaris and investigated its anticancer effect on breast cancer cell line. Physicochemical characterization was performed by FT-IR, XRD, SEM, TEM, VSM, EDS mapping, UV, and zeta potential assays. Cell cytotoxicity and apoptosis frequency were studied by the MTT and flow cytometry assays. Also, cell cycle analysis, Hoechst staining, and measuring ROS (reactive oxygen species) level were performed. The synthesized particles were almost spherical with a size range of 14–52 nm. The FT-IR and XRD assays confirmed the proper synthesis of the particles and VSM analysis showed that particles had magnetic property and the maximum saturation magnetization was 0.8 Emu/g. Also, the EDS mapping of the nanocomposite showed the Zn, Fe, O, and Ag elements. The MTT assay showed that the 50% inhibitory concentration (IC50) of ZnFe2O4-Ag for breast cancer and normal cells were 28 and 154 µg/mL, respectively, and the nanocomposite had stronger anticancer activity than cisplatin (IC50 = 84 µg/mL). Flow cytometry analysis showed that the exposure to the nanocomposite induced cell apoptosis by 77.5% and significantly induced ROS generation. Also, treating breast cancer cells with the nanocomposite induced cell cycle arrest and apoptotic features, including chromatin condensation and fragmentation. In conclusion, ZnFe2O4-Ag nanocomposite synthesized by C. vulgaris could suppress the proliferation of breast cancer cells by the generation of oxidative stress, apoptosis induction, and cell cycle arrest. [ABSTRACT FROM AUTHOR]

A potent natural combretastatin, combretastatin A-4 (COMA4) targets the condylon active pocket to produce anticancer effects. Studies on inflammation and oxidative stress have been linked to cancer, indicating that lowering these risk variables may have an adverse effect on the progression of cancer. This study utilized COMA4 as a building block to create 28 coumarins with improved therapeutic effects. The first coumarin derivative, COMA4-COU-1, was activated by thionyl chloride and then coupled with various phenols, resulting in 27 COMA4-COU derivatives. Biomedical-related activities were conducted using COMA4 as a reference, including anticancer activity assayed against eight cancerous cellular populations, antioxidant activity evaluated on H2O2-treated human SH-SY5Y populations, and anti-inflammatory activity tested against three enzymatic mediators of inflammation. The biosafety studies included testing the effects of COMA4 and its coumarins on the normal growth of three cell populations and on human erythrocyte hemolysis. Finally, the pharmacokinetic indexes of the building block and its derivatives were computerized using two web-based programs. The results indicated that the biomedical activities are directly improved by the presence of an electron-donating group on the off-side aromatic ring. Also, these activities were increased when this group substituted at the para or meta position. The maximum activities were revealed when this aromatic ring was trisubstituted with this group type, with privilege activities for the trimethoxy aromatic ring. Concerning the biocompatibility studies, the synthetic coumarins demonstrated a high level of compatibility with the tested normal cells and also with human erythrocytes. Moreover, the in silico analysis demonstrated the capacity of the synthetic coumarins to present potential drug candidates. The author concluded that the coumarin-structural modification can open the door for developing new, potent, and biosafe COMA4 derivatives. In this regard, this study afforded many insights about the structure–function relationships of the synthesized compounds that can guide future research about COMA4-based derivatives. [ABSTRACT FROM AUTHOR]

Background: Saraca asoca (Asoka) is reported to possess phytoestrogenic components with anticancer properties. The phytoestrogens are recognized as natural agonists for ERβ, which acts as an antagonist to ERα. Despite the absence of ERα, studies have identified ERβ in 50–80% of triple negative breast cancers (TNBC). Thus, the present study is intended to reveal the role of phytoestrogens of Asoka on TNBC. The cytotoxic effect of Asoka methanol bark extract was analyzed on different breast cancer cell lines by MTT assay. Estrogen-screen assay was employed to determine the proliferative/antiproliferative effect. Identification of phytoestrogens in Asoka was accomplished using LC-MS analysis and in silico docking studies were performed to investigate possible interactions of phytoestrogens with ERα and β. Results: The extract of Asoka was found to be cytotoxic against TNBC cell line, MDAMB-231 with IC50 of 70.22 ± 1.89 μg/mL and towards HER+ breast cancer cell line, SKBR3 with IC50 of 98.41 ± 2.31 μg/mL, respectively. Whereas the extract did not show any cytotoxicity towards ERα cell line, MCF-7 even up to the concentration 300 μg/mL. Estrogen-screen assay emphasized an estrogenic effect of the extract on MCF-7 and an anti-estrogenic/antiproliferative effect on MDAMB-231 cells. LC–MS analysis identified phytoestrogens such as β-sitosterol, quercetin, kaempferol and others. The docking results revealed good binding efficacy of phytoestrogens with ERβ than ERα and quercetin shows more affinity with the highest docking score of − 9.220. Strikingly, it was found that the S. asoca methanol extract was preferentially cytotoxic to TNBC cells. Conclusion: The study demonstrates selective anticancer properties of S. asoca methanol extract on TNBC, which indicates a selective impact on ER subtypes. The identification of phytoestrogens, such as β-sitosterol, quercetin and kaempferol, in the Asoka methanol bark extract provides a molecular basis for its observed effects. In silico studies further support the view that these phytoestrogens may preferentially interact with ERβ rather than ERα. Quercetin, in particular, demonstrated the highest binding efficacy with ERβ, suggesting its potential role in mediating the anticancer effects observed in TNBC cells. Further research is warranted to explore the full therapeutic potential of phytoestrogens in breast cancer treatment. [ABSTRACT FROM AUTHOR]

Cancer is responsible for approximately 10 million deaths worldwide, with 70% of the deaths occurring in low- and middle-income countries; as such safer and more effective anti-cancer drugs are required. Therefore, the potential benefits of Ziziphus nummularia and Ziziphus spina-christi as sources of anti-cancer agents were investigated. Z. nummularia and Z. spina-christi extracts were prepared using chloroform, ethanol, ethyl acetate, and water. The extracts' anti-cancer properties were determined using the MTT Cell Viability Assay in four cancer cell lines: breast (KAIMRC2 and MDA-MB-231), colorectal (HCT8), and liver (HepG2). The ApoTox-Glo Triplex Assay and high-content imaging (HCI)-Apoptosis Assay were used to assess KAIMRC2 and HCT8 cells further. In addition, KAIMRC2 cells were tested for microtubule staining, and AKT/mTOR protein expression was determined by western blot analysis. Liquid chromatography-mass spectrometry (LC–MS) was performed to identify the secondary metabolites in the ethanol and ethyl acetate extracts, followed by in silico techniques to predict molecular targets and interactions, safety, and pharmacokinetic profile for identified metabolites. Out of the eight extracts, the ethanolic extract of Z. nummularia, exhibited the most potent activity against KAIMRC2 cells with an IC50 value of 29.2 μg/ml. Cancer cell treatment with the ethanolic extract of Z. nummularia resulted in a dose-dependent decrease in cell viability with increased apoptosis and cytotoxic effects. Microtubule staining showed a disrupted microtubular network. The ethanolic extract treatment of KAIMRC2 cells led to upregulated expression of pAKT and pmTOR. In silico studies predicted luteolin-7-O-glucoside to be a ligand for tubulin with the highest docking score (− 7.686) and similar binding interactions relative to the native ligand. Further computational analysis of the metabolites showed acceptable pharmacokinetic and safety profiles, although ethanolic extract metabolites were predicted to have cardiotoxic effects. Ethanolic extraction is optimal for solubilizing active anticancer metabolites from Z. nummularia, which may act by causing M-phase arrest via inhibition of tubulin polymerization. Luteolin-7-O-glucoside is the lead candidate for further research and development as an anti-cancer agent. In addition, this study suggests that herbal treatment could switch on mechanisms of adaptation and survival in cancer cells. [ABSTRACT FROM AUTHOR]

Collagen nanoparticles (collagen-NPs) are promising biological polymer nanoparticles due to their exceptional biodegradability and biocompatibility. Collagen-NPs were bio-fabricated from pure marine collagen using the cell-free supernatant of a newly isolated strain, Streptomyces sp. strain NEAA-3. Streptomyces sp. strain NEAA-3 was identified as Streptomyces plicatus strain NEAA-3 based on its cultural, morphological, physiological properties and 16S rRNA sequence analysis. The sequence data has been deposited under accession number OR501412.1 in the GenBank database. The face-centered central composite design (FCCD) was used to improve collagen-NPs biosynthesis. The maximum yield of collagen-NPs was 9.33 mg/mL with a collagen concentration of 10 mg/mL, an initial pH of 7, an incubation time of 72 h, and a temperature of 35 °C. Using the desirability function approach, the collagen-NPs biosynthesis obtained after FCCD optimization (9.53 mg/mL) was 3.92 times more than the collagen-NPs biosynthesis obtained before optimization process (2.43 mg/mL). The TEM analysis of collagen-NPs revealed hollow sphere nanoscale particles with an average diameter of 33.15 ± 10.02 nm. FTIR spectra confirmed the functional groups of the collagen, collagen-NPs and the cell-free supernatant that are essential for the efficient capping of collagen-NPs. The biosynthesized collagen-NPs exhibited antioxidant activity and anticancer activity against HeP-G2, MCF-7 and HCT116 cell lines. Collagen-NPs assessed as an effective drug loading carrier with methotrexate (MTX), a chemotherapeutic agent. The TEM analysis revealed that the average size of MTX-loaded collagen-NPs was 35.4 ± 8.9 nm. The percentages of drug loading (DL%) and encapsulation efficiency (EE%) were respectively 22.67 and 45.81%. [ABSTRACT FROM AUTHOR]

In this research, palladium (II) and platinum (II), as well as their bimetallic nanoparticles were synthesized using medicinal plants in an eco-friendly manner. Rosemary and Ginseng extracts were chosen due to their promising anticancer potential. The synthesized nanoparticles underwent characterization through FT-IR spectroscopy, DLS, XRD, EDX, SEM, and TEM techniques. Once the expected structures were confirmed, the performance of these nanoparticles, which exhibited an optimal size, was evaluated as potential anticancer agents through in vitro method on colon cancer cell lines (Ls180, SW480). MTT assay studies showed that the synthesized nanoparticles induced cell death. Moreover, real-time PCR was employed to investigate autophagy markers and the effect of nanoparticles on the apoptosis process, demonstrating a significant effect of the synthesized compounds in this regard. [ABSTRACT FROM AUTHOR]

Mucuna pruriens (MP) which is commonly known as "Velvet Bean" is an underutilized legume traditionally used to treat Parkinson's disease and male fertility issues. Extracts of MP have also been identified for their antidiabetic, antioxidant, and antineoplastic effects. Commonly, the antioxidant and anticancer properties of a drug are linked together as antioxidants scavenge free radicals and prevent the cellular DNA damage which could result in cancer development. In this investigation, comparative assessment of the anticancer and antioxidant potentials of methanolic seed extracts from two common varieties of MP, Mucuna pruriens var. pruriens (MPP) and Mucuna pruriens var. utilis (MPU) against human colorectal cancer adenocarcinoma cells COLO-205, was carried out. The highest antioxidant potential was recorded with MPP with an IC50 of 45.71 μg/ml. The in vitro antiproliferative effects of MPP and MPU on COLO-205 showed an IC50 of 131.1 μg/ml and 246.9 μg/ml respectively. Our results revealed intervention of the MPP and MPU extracts in growth kinetics of the COLO-205 cells in concomitance with apoptosis induction up to 8.73- and 5.58-folds respectively. The AO/EtBr dual staining and the flow cytometry results also confirmed the better apoptotic efficacy of MPP over MPU. MPP at a concentration of 160 μg/ml exhibited highest apoptosis and cell cycle arrest. Furthermore, effect of the seed extracts on p53 expression was investigated by quantitative RT-PCR and a maximum upregulation of 1.12-fold was recorded with MPP. [ABSTRACT FROM AUTHOR]

Zerumbone (ZER) is a phytochemical isolated from plants of the Zingiberaceae family. Numerous studies have demonstrated its diverse pharmacological properties, particularly its potent antitumorigenic activity. This study aimed to assess the antiproliferative effects of ZER on HT-29 cells cultivated in both two-dimensional (2D) monolayer and three-dimensional (3D) spheroid culture systems. The evaluation of growth (size), cell death, and cell cycle arrest in 3D spheroid HT-29 cells was correlated with mRNA expression data. Treatment of 2D cells revealed that ZER exhibited cytotoxicity at concentrations above 30 µM, and an IC50 of 83.54 µM (24-h post-ZER treatment) effectively suppressed cell migration. In the 3D model, ZER induced an increase in spheroid volume over a 72-h period attributed to disaggregation and reconfiguration of characteristic zones. Analysis of cell death demonstrated a significant rise in apoptotic cells after 24 h of ZER treatment, along with cell cycle arrest in the G1 phase. Furthermore, ZER treatment resulted in alterations in mRNA expression, affecting key signaling pathways involved in cell death (BCL2 and BBC3), endoplasmic reticulum stress (ERN1), DNA damage (GADD45A), cell cycle regulation (CDKN1A, NFKB1, MYC, and TP53), and autophagy (BECN1 and SQSTM1). These findings suggested that ZER holds promise as a potential candidate for the development of novel anticancer agents that can modulate crucial cell signaling pathways. Additionally, the use of the 3D culture system proved to be a valuable tool in our investigation. [ABSTRACT FROM AUTHOR]

In this paper, a novel series of N-hydroxybenzimidazoles as potential anticancer agents were designed and synthesized. The in vitro enzymatic assays suggested N-hydroxy-6-(3-nitrophenyl)-benzimidazole-2-carboxylic acid had good inhibitory potency (IC = 0.25 μM) to human lactate dehydrogenase A. Cytotoxic assay revealed that this compound gave the best potency (IC = 2.2 μM) to inhibit BGC-823 cell proliferation. Furthermore, molecular docking study showed it had strong interactions with lactate dehydrogenase A, which was in line with our experimental results. Graphical abstract: [Figure not available: see fulltext.] [ABSTRACT FROM AUTHOR]

This paper presents synthesis, characterization, computational and biological (anti-bacterial, antifugal, and anti-cancer) assessment studies of vital metal ions [Ca(II), Zn(II), Pt(II), Pd(II), and Au(III)] complexes of albendazole (Alb). Structures of the titled complexes cited herein were elucidated using elemental analysis, IR, Raman, H and C NMR, and electronic spectra. The results indicated formation of albendazole complexes by three fashions and albendazole reaction as a bidentate ligand bound to Ca(II), Zn(II), Pd(II), and Au(III) ions via the carbamide oxygen and/or benzimidazole nitrogen. Pt(II) ions coordinated with albendazole ligand via deprotonated benzimidazole ring. The molar conductance measurements confirmed non-electrolyte nature of 1 : 1 metal : ligand (Alb) complexes of Ca(II), Zn(II), and Au(II) and 1 : 2 complexes of Pt(II) and Pd(II). Thus, the complexes could be presented as [Ca(Alb)(Cl)(HO)], [Zn(Alb)(Cl)], [Pt(Alb)(HO)], [Pd(Alb)], and [Au(Alb)(Cl)]. Based on the Coats-Redfern and Horowitz-Metzeger methods the kinetic thermodynamic parameters of thermal decomposition have been deduced. The narrow size distribution in nanoscale range for the albendazole complexes is discussed using X-ray powder diffraction (XRD), scanning electron microscopy (SEM), X-ray energy dispersive spectrometery (EDX), and transmission electron microscopy (TEM). Computational studies data for the synthesized complexes are considered. [ABSTRACT FROM AUTHOR]

Metals chelation to biologically active molecules can be used as a medical model of enhancement of their antimicrobial activity. This paper is devoted to synthesis, physicochemical characterization, computational and antimicrobial studies of some complexes of vital metal ions including Ca(II), Fe(III), Pd(II), and Au(III) with levofloxacin (LFX) ligand. Structures of such complexes were elucidated with the help of elemental analyses and spectral measurements (IR, Raman, H NMR, C NMR and electronic). The accumulated data confirmed that formation of LFX complexes had two coordination pathways as bidentate ligands. One of those proceeded via deprotonation of the carboxylic group followed by bounding to Ca(II) or Fe(III) ion via the carbonyl group and carboxylate oxygen atoms. Alternatively, LFX acted as a neutral ligand bound to Pd(II) or Au(III) ion via nitrogen atoms of the piperazine ring. Molar conductance measurements of the 1: 1 complexes in DMSO had non-electrolyte nature with the exception of Au(III) complex. Formulae assigned to the complexes were [Ca(LFX)(Cl)(HO)] ( I), [Fe(LFX)(Cl)(HO)]·6HO ( II), [Pd(LFX)(Cl))] ( III), and [Au(LFX)(Cl)]·Cl ( IV). The nano-scale nature of Pd(II) and Au(III) complexes has been elucidated on the basis of X-ray powder diffraction (XRD), scanning electron microscope (SEM) and transmission electron microscopy (TEM). The antimicrobial tests of the complexes I-IV demonstrated some activity against several kinds of bacteria and fungi. Cytotoxic activity of the complex IV was tested against the human colon carcinoma (HCT-116) and human hepatocellular carcinoma (HepG-2) tumor cell lines. [ABSTRACT FROM AUTHOR]

Flavonoid-metal complexes have anticancer activities. However, the quantitative structure-activity relationship (QSAR) of flavonoid-metal complexes and their anticancer activities has not been known so far. Based on the 14 structures of flavonoid-metal complexes and their anticancer activities for HepG2 from the references, we optimised their structures using the density functional theory (DFT) method, and subsequently calculated 19 quantum chemical descriptors, such as dipole, charge, and energy. Then, we chose several quantum chemical descriptors that are very important for IC which represents the anticancer activities of flavornoid-metal complexes for HepG2 through the stepwise linear regression method. Meanwhile, we obtained six new variables through the principal component analysis. Finally, we built QSAR models based on those important quantum chemical descriptors, six new variables as independent variables, and IC as a dependent variable using an artificial neural network (ANN). At last, we validated the models using the experimental data from the references. The results show that models presented in this paper are accurate and predictive. [ABSTRACT FROM AUTHOR]