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Paclitaxel (PTX) is a potent chemotherapeutic agent limited by poor solubility and adverse effects. To address these challenges, we developed a novel nanocomposite combining PTX purified from the endophytic fungus A. fumigatiaffinis PP235788.1 with biosynthesized silver nanoparticles (AgNPs) from the same fungal strain. The PTX-AgNP conjugate (28.48 ± 0.13 nm) was characterized by UV-Vis, XRD, and TEM, revealing monodisperse AgNPs (14.50 ± 0.58 nm) as the core component. In vitro studies demonstrated significant cytotoxicity against MCF-7 breast cancer cells (IC₅₀= 1.7 µg/mL, p  < 0.001), with 5-10-fold greater efficacy than AgNPs alone. Annexin V/PI staining and DNA fragmentation assays confirmed apoptosis induction, highlighting the conjugate’s enhanced anticancer activity. This eco-friendly nano platform synergizes PTX’s therapeutic effects with AgNP-mediated targeting, offering a promising strategy to reduce side effects while improving tumor-specific cytotoxicity for advanced cancer therapy.

The Nickel Oxide (NiO) nanoparticles are synthesized using the green synthesis method utilizing Brassica oleracea L. var. capitata leaf extracts. The X-ray diffraction studies revealed that synthesized NiO-NPs exhibit face-centered cubic structure. SEM images of NiO-NPs exhibited agglomerated structures. TEM images of NiO-NPs revealed spherical morphology with variable sizes ranging from 5-50 nm. FT-IR spectrum was used to confirm the various functional groups. The absorbance spectral studies reveal the existence of three important peaks at wavelength 545 nm, 589 nm, and 636 nm. The antibacterial activity of NiO-NPs against Gram +ve Staphylococcus aureus (NCIM2079), Bacillus subtilis (NCIM2250), and Gram –ve Pseudomonas aeruginosa (MTCC3541), Escherichia coli (NCIM2065) was further studied. The anticancer activity of NiO-NPs against lung cancer cells (NRU-A549) was examined. The IC50 value was found to be 326.4 µg/mL. The synthesized NiO-NPs were further studied for electrochemical and supercapacitor applications.

New 1-thia-azaspiro[4.5]decane derivatives, their derived thiazolopyrimidine and 1,3,4-thiadiazole compounds were synthesized. The thioglycoside derivatives of the synthesized (1,3,4-thiadiazolyl)thiaazaspiro[4.5]decane and thiazolopyrimidinethione compounds were synthesized by glycosylation reactions using acetylated glycosyl bromides. The anticancer activity of synthesized compounds was studied against the cell culture of HepG-2 (human liver hepatocellular carcinoma), PC-3 (human prostate adenocarcinoma) and HCT116 (human colorectal carcinoma) cell lines and a number of compounds showed moderate to high inhibition activities.

Nowadays, cancer is an important public health problem in all countries. Limitations of current chemotherapy for neoplastic diseases such as severe adverse reactions and tumor resistance to the chemotherapeutic drugs have been led to a temptation for focusing on the discovery and development of new compounds with potential anticancer activity. The importance of thiophene and thiadiazole rings as scaffolds present in a wide range of therapeutic agents has been well reported and has driven the synthesis of a large number of novel antitumor agents. A series of new 1,3,4-thiadiazoles were synthesized by heterocyclization of N-(4-nitrophenyl)thiophene-2-carbohydrazonoyl chloride with a variety of hydrazine-carbodithioate derivatives. The mechanisms of these reactions were discussed and the structure of the new products was elucidated via spectral data and elemental analysis. All the new synthesized compounds were investigated for in vitro activities against human hepatocellular carcinoma (HepG-2) and human lung cancer (A-549) cell lines compared with cisplatin standard anticancer drug. Moreover, molecular docking using MOE 2014.09 software was also carried out for the high potent compound with the binding site of dihydrofolate reductase (DHFR, PDB ID (3NU0)). The results showed that compound has promising activities against HepG-2 and A-549 cell lines (IC50 value of 4.37±0.7 and 8.03±0.5 μM, respectively) and the results of molecular docking supported the biological activity with total binding energy equals -1.6 E (Kcal/mol). Overall, we synthesized a new series of 1,3,4-thiadiazoles as potential antitumor agents against HepG-2 and A-549 cell lines.

The naturally occurring neocryptolepine (5-Methylindolo [2,3-b]quinoline) and its analogs exhibited prominent anticancer and antimalarial activity. However, the main problem of this class of compounds is their poor aqueous solubility, hampering their bioavailability and preventing their clinical development. To overcome the problem of insolubility and to improve the physicochemical and the pharmacological properties of 5-Methylindolo [2,3-b]quinoline compounds, this work was designed to encapsulate such efficient medical compounds into mesoporous silica oxide nanoemulsion (SiO2NPs). Thus, in this study, SiO2NPs was loaded with three different concentrations (0.2 g, 0.3, and 0.6 g) of 7b (denoted as NPA). The findings illustrated that the nanoparticles were formed with a spherical shape and exhibited small size (less than 500 nm) using a high concentration of the synthesized chemical compound (NPA, 0.6 g) and good stabilization against agglomeration (more than −30 mv). In addition, NPA-loaded SiO2NPs had no phase separation as observed by our naked eyes even after 30 days. The findings also revealed that the fabricated SiO2NPs could sustain the release of NPA at two different pH levels, 4.5 and 7.4. Additionally, the cell viability of the produced nanoemulsion system loaded with different concentrations of NPA was greater than SiO2NPs without loading, affirming that NPA had a positive impact on increasing the safety and cell viability of the whole nanoemulsion. Based on these obtained promising data, it can be considered that the prepared NPA-loaded SiO2NPs seem to have the potential for use as an effective anticancer drug nanosystem.

N-rich organic materials bearing polyphenolic moieties in their building networks and nanoscale porosities are very demanding in the context of designing efficient biomaterials or drug carriers for the cancer treatment. Here, we report the synthesis of a new triazine-based secondary-amine- and imine-linked polyphenolic porous organic polymer material TrzTFPPOP and explored its potential for in vitro anticancer activity on the human colorectal carcinoma (HCT 116) cell line. This functionalized (-OH, -NH-, -C=N-) organic material displayed an exceptionally high BET surface area of 2140 m2 g−1 along with hierarchical porosity (micropores and mesopores), and it induced apoptotic changes leading to high efficiency in colon cancer cell destruction via p53-regulated DNA damage pathway. The IC30, IC50, and IC70 values obtained from the MTT assay are 1.24, 3.25, and 5.25 μg/mL, respectively.

Non-small cell lung cancer (NSCLC) is the leading cause of cancer-related death throughout the world. Due to the shortcomings of traditional chemotherapy, targeted therapies have come into prominence for the management of NSCLC. In particular, epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) therapy has emerged as a first-line therapy for NSCLC patients with EGFR-activating mutations. In this context, new indenopyrazoles, which were prepared by an efficient microwave-assisted method, were subjected to in silico and in vitro assays to evaluate their potency as EGFR TK-targeted anti-NSCLC agents. Compound 4 was the most promising antitumor agent towards A549 human lung adenocarcinoma cells, with an IC50 value of 6.13 µM compared to erlotinib (IC50 = 19.67 µM). Based on its low cytotoxicity to peripheral blood mononuclear cells (PBMCs), it can be concluded that compound 4 exerts selective antitumor action. This compound also inhibited EGFR TK with an IC50 value of 17.58 µM compared to erlotinib (IC50 = 0.04 µM) and induced apoptosis (56.30%). Taking into account in silico and in vitro data, compound 4 stands out as a potential EGFR TKI for the treatment of NSCLC.

This narrative review aims to systematize the current knowledge on the dual role of reactive oxygen species and reactive nitrogen species in cancer processes, from their physiological function in redox signaling to their pathological impact in oxidative distress. The mechanisms of biomolecule damage, particularly DNA, and deregulation of signaling pathways induced by excessive ROS/RNS concentrations, which promote neoplastic transformation, are presented. The importance of diet and endogenous antioxidants in cancer prevention is also discussed, emphasizing the role of natural antioxidants in prevention and adjunctive therapy. In this context, oleanolic acid emerges as a promising compound with dual action modulating oxidative stress, capable of balancing cellular redox responses. We discuss the most important antioxidant mechanisms of oleanolic acid, the interconnection of oxidative stress with carcinogenesis-related pathways, anticancer mechanisms mediated by oxidative stress modulation, and structural modifications and modern application techniques that improve its bioavailability, as well as future perspectives on oleanolic acid research in the context of its antioxidant and anticancer activity. Overall, available experimental and preclinical data indicate that oleanolic acid, through pleiotropic modulation of oxidative stress and signaling networks, holds promise as an adjuvant agent in cancer prevention and therapy.

The amide derivatives of nonsteroidal anti-inflammatory drugs have been reported to possess antitumor activity. The present work describes the synthesis of dexibuprofen amide analogues ( ) as potential anticancer agents. The title amides ( ) were obtained by simple nucleophilic substitution reaction of dexibuprofen acid chloride with substituted amines in good yield and chemical structures were confirmed by FTIR, 1H NMR, 13C NMR and mass spectral data. The brine shrimp lethality assay results showed that all of the synthesized compounds are non-toxic to shrimp larvae. The inhibitory effects on tumor growth were evaluated and it was observed that N-(2,5-dichlorophenyl)-2-(4-isobutylphenyl) propionamide ( ) and N-(2-chlorophenyl)-2-(4-isobutylphenyl) propionamide ( ) exhibited excellent antitumor activity compared to all other derivatives. The compound bearing 2,5-dichloro substituted phenyl ring and possesses 2-chloro substituted phenyl ring exhibited 100% inhibition of the tumor growth. The anticancer activity was evaluated against breast carcinoma cell line (MCF-7) and it was observed that derivative exhibited excellent growth inhibition of cancer cells with IC value of 0.01±0.002 µm, which is better than the standard drugs. The docking studies against breast cancer type 1 susceptibility protein BRCA1 (PDBID 3K0H) exhibited good binding affinities, which are in good agreement with the wet lab results. The compounds and showed the binding energy values of -6.39 and -6.34 Kcal/mol, respectively. The molecular dynamic (MD) simulation was also carried out to evaluate the residual flexibility of the best docking complexes of compounds and . The MD simulation analysis assured that the formed a more stable complex with the target protein than the . The synthesized amide derivatives exhibited were devoid of gastrointestinal side effects and no cytotoxic effects against human normal epithelial breast cell line (MCF-12A) were found. Based upon our wet lab and dry lab findings we propose that dexibuprofen analogue may serve as a lead structure for the design of more potent anticancer drugs.

This work was designed to study the free and immobilized partial purified lovastatin in various applications. The results of HMG-CoA reductase inhibition showed enzyme inhibition at 10 mM of standard and partial purified lovastatin with specific activity 0.056 and 0.062 U/mg protein respectively, compared with specific activity 0.277 U/mg protein without inhibitor. The results of the thermal stability and storage time on lovastatin for inhibition of HMG-CoA reductase demonstrated that the standard and partial purified lovastatin were stabled in temperatures between 20-40 ᵒC, then the stability begun to decrease at 45 ᵒC, while lovastatin was stable in storage time between 1- 8 hours, then the stability begun to decrease after ten hours at 40 ºC. The results of MIC for lovastatin were demonstrated that most tested concentration were showed antibacterial activity of free and immobilized partial purified lovastatin against Candida albicans, Escherichia coli, and Staphylococcus aureus with MIC values ranging from 15 to 75 µg/ml. Whereas the results of minimum bactericidal concentration (MBC) and minimum fungicidal concentration (MFC) showed that C. albicans, E. coli, and S. aureus had no growth with concentration ranging from 55 to 75, 55 to 75, and 30 to 75 µg/ml, respectively. As well as the results of the cytotoxic impact using MTT experiment indicated that partial purified lovastatin caused a reduction in cells viability (p ≤ 0.05) at a dose-dependent manner on MCF-7 cell lines, with a calculating IC50 of 138.1 µg/ml, compare with normal cell line (WRL 68 Cell Line) at IC50 of 198.7 µg/ml.