Search

Copyright of Baghdad Science Journal is the property of Republic of Iraq Ministry of Higher Education & Scientific Research (MOHESR) and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Introduction: Garlic (Allium sativum L.), has been cultivated in various countries and is valued for its medicinal and culinary properties. It contains bioactive compounds such as phenolic compounds, organic sulfides, polysaccharides, and saponins, with allicin being a particularly studied compound. These compounds have been shown to possess antioxidant, antimicrobial, antiviral, anticancer, anti-inflammatory, anti-hyperlipidemic and antihypertensive effects. Garlic has been used for over 5000 years as a curative plant and has potential applications in food science, medicine, and nutraceuticals. Aim of the Study: The aim of the study is to provide a comprehensive review of the overall impact of Allium sativum L. on human health and in order to draw attention to the benefits of regular consumption. Materials and methods: A comprehensive review of scientific and medical literature was conducted utilizing PubMed and Google Scholar databases. Searching terms were: garlic, Allium sativum L., garlic antiinflammatory, garlic anticancer, garlic health effects. Conclusion: Allium sativum L. is associated with a comprehensive range of beneficial effects on the human body. These include anti-inflammatory and antioxidant properties, positive influence on lipid profile, cardiovascular system, and the anticancer activity among others by stimulation of tumor apoptosis. As a result, garlic and its bioactive compounds hold promise as functional foods or nutraceuticals for the prevention and treatment of various diseases. [ABSTRACT FROM AUTHOR]

We describe in this review the historical evidence leading up to the concept and design of Vigil and subsequent clinical applications including safety and efficacy in a randomized, controlled Phase IIB trial. Vigil (gemogenovatucel-T) is a unique triple function targeted immunotherapy that demonstrates preclinical and clinical systemic anticancer activity. Construction of Vigil involves harvest of autologous malignant tissue for neoantigen targeting (ideally containing clonal neoantigens) followed by a two-day process involving transfection with a plasmid to provide a permissive 'training environment' for the patient's immune system. Transfected plasmid components contain an expressive human GMCSF DNA segment to enhance anticancer immune functional response and a second component expressing bi-shRNAfurin which reduces TGFβ isomers (TGFβ1 and TGFβ2) thereby reducing cancer inhibition of the targeted immune response. Results generated to date justify advancement to confirmatory clinical trials supporting product regulatory approval. Plain Language Summary Vigil is an anticancer treatment that employs three methods of enhancing the body's immune system to identify and kill cancer cells. The construction of Vigil involves cancer cells from the same person being treated (personalized therapy) in combination with added anticancer genetic signals to enhance the number and function anti-anticancer immune cells and to guide the immune cells to the cancer and not to normal organs of the body. In this manner, an army of immune cells are created that can move to attacking the cancer using blood vessels to get to the cancer anywhere it tries to grow in the body. One study (Phase I) performed with this product to determine safety and dose range demonstrated an optimal dose and schedule. Another study (Phase IIA) showed initial clinical benefit. A third more complex study (Phase IIB) in patients treated with Vigil compared with standard of care without Vigil demonstrated the ability to prolong the patients life and time without their cancer getting worse without any significant side effects associated with the treatment in a unique subset of ovarian cancer patients, those with the ability to repair their DNA. Based on the composite of these results, Vigil is an attractive targeted immunotherapy justified for late-stage clinical testing. Article highlights Vigil is a novel triple function immunotherapy designed to deliver personalized clonal neoantigens. Historical background Expression of GMCSF has been extensively studied and demonstrates safety, efficacy and immune activation in various solid tumor malignancies. Modulation of both GMCSF and TGFβ impact anticancer immune response specifically related to clinical benefit in association with GMCSF up regulation and TGFβ down regulation. bi-shRNA mechanism bi-shRNA is designed to take advantage of both cleave-dependent and cleavage independent RISC loading thus decreasing mRNA and subsequent protein expression to block signals associated with cancer progression. Vigil: mechanism Vigil is constructed from autologous tumor cells transfected with a plasmid encoding a GMCSF expressive unit, bi-shRNA directed to furin and clonal neoantigens. Clonal neoantigens are associated with increased clinical benefit to immune therapies. Vigil plasmid Vigil plasmid is produced using GMP manufacturing. Vigil construction & product delivery Vigil is constructed via a 2 day manufacturing process consisting of tissue dissociation, electroporation and irradiation. Preparation of the drug product The drug substance is formulated to appropriate concentration using freeze media. Every Vigil batch/lot is tested for product release criteria which has been verified for regulatory suitability. Vigil clinical experience 230 patients have received 1433 doses over various clinical trials in solid tumors. Vigil Phase I testing in solid tumor cancer Phase I testing of Vigil demonstrated manufacturing optimization, appropriate dose, safety and immune response in advanced solid tumor patients. Vigil Phase I/II testing in Ewing's sarcoma Vigil has been tested as monotherapy and in combination with temozolomide/irinotecan in Ewings sarcoma and demonstrated safety and evidence of efficacy. Vigil Phase IIA/IIB evaluation in ovarian cancer In Phase IIA trial in newly diagnosed Stage IIIB/IV ovarian cancer patients, Vigil demonstrated immune activation via ELISpot assay which correlated with clinical benefit. In Phase IIB trial also in newly diagnosed Stage IIIB/IV ovarian cancer patients, Vigil demonstrated improved RFS and OS in BRCA-wt patients. This benefit was further enhanced in patients with HRP molecular profile. In both trials, Vigil demonstrated no ≥ Grade 3 adverse events. Vigil-related biomarkers Several biomarkers have been identified retrospectively including TP53 mutation, and high ENTPD1 expression. Conclusion Vigil demonstrates a strong safety profile combined with durable clinical benefit. [ABSTRACT FROM AUTHOR]

The development of a pH‐responsive, biocompatible polymeric carrier for controlled delivery of bioactive agents holds significant practical value for pharmaceutical applications. In this study, we used the gelation method to make pH‐responsive polymeric microbeads using sodium alginate (SA), poly(vinylpyrrolidone‐co‐vinyl acetate) (PVPVA), and nickel zinc ferrite (NZF) nanoparticles for controlled release of doxorubicin (DOX). The generated microbeads are characterized using various techniques, including Fourier‐transform infrared spectroscopy, X‐ray diffraction, scanning electron microscopy, and transmission electron microscopy. Swelling studies reveal enhanced permeability at pH 6.4, and in vitro release studies demonstrate a higher release rate at pH 6.4 compared to pH 2.0. Cytotoxicity tests on MCF‐7 cells (a type of breast cancer cell line) showed that NZF‐loaded microbeads, especially SP‐NZFNPs‐DOX, were more effective than other carriers, indicating their potential usefulness in cancer treatment. Furthermore, biocompatibility tests demonstrate that the SA/PVPVA microbeads and nanoparticles are biocompatible with 3T3 fibroblasts. This study contributes valuable insights to the evolving landscape of nanotechnology in cancer treatment, emphasizing the synergistic role of NZF nanoparticles, SA, and PVPVA in optimizing drug delivery systems. [ABSTRACT FROM AUTHOR]

Cinnamon, an Indigenous species, is extensively used as a folk medicine in India, China, and other parts of the world due to its therapeutic potential inherited via the latent chemical composition. The vital component presented is cinnamaldehyde, along with cinnamic acid and cinnamate, which contributes to being an anti‐inflammatory, antimicrobial, antidiabetic, and anticancer agent together with the capability to control neurological syndromes like Alzheimer's and even Parkinson's diseases. Given the importance of the anticarcinogenic properties of cinnamon on various cell strains concerning the curable effect, this review focuses on evaluating different extraction methods like steam distillation, Soxhlet extraction, microwave‐assisted extraction, and more, in addition to a summary of new technologies like gas chromatography, HPLC, DART‐MS, and NMR, etc. which paved the way in characterizing the chemical composition of cinnamon. Cinnamaldehyde showed its apoptosis through various mechanistic pathways on an adequate number of cell lines and antineoplastic potential on specific multifaceted cancerous cells, which advocates for continued research and investment in this vital area of drug discovery and suggestions for future scope. [ABSTRACT FROM AUTHOR]

Introduction: Multifunctional nanomaterials are emerging as promising tools for treating both cancer and bacterial infections. However, integrating dual therapeutic capabilities into a single system remains challenging. This study presents multifunctional nanoparticles (ECI-NPs) based on Epigallocatechin gallate (EGCG) oligomers, Curcumin (CUR), and Indocyanine Green (ICG) for combined cancer and bacterial treatment. Methods: ECI-NPs were synthesized via oxidative coupling of EGCG, CUR, and ICG. The nanoparticles were characterized for stability, size, drug loading, and release profiles. Cellular uptake, phototoxicity in melanoma cells, and antibacterial activity against Escherichia coli and Staphylococcus aureus were also evaluated. Results: ECI-NPs demonstrated optimal stability, high drug loading, and controlled release. Cellular studies showed increased uptake and greater phototoxicity in melanoma cells compared to free drugs. ECI-NPs also exhibited enhanced anticancer effects and strong antibacterial activity, outperforming the individual components. Discussion: The polyphenol-based ECI-NPs offer synergistic therapeutic effects, overcoming the limitations of free drugs in terms of solubility and efficacy. This dual-function platform shows potential for broader biomedical applications, addressing challenges in cancer and bacterial infections. Further research will focus on in vivo studies and clinical translation. [ABSTRACT FROM AUTHOR]

Background and Purpose : Cancer remains one of the leading causes of death globally. In pursuit of alternative treatments, nature-based ones are especially in demand due to the perceived lesser toxicity and cost-effectiveness. Plumbagin, a naphthoquinone compound derived from the Plumbaginaceae family, has demonstrated significant anticancer properties. It is a yellow crystalline phytochemical that exhibits potent cytotoxic effects against various cancer cells in vitro and in vivo. Results : Its distinct anticancer mechanisms include modulating signaling pathways, such as NF-kβ, STAT3, MMP-9, VEGF, and Akt, induction of apoptosis, autophagy, cell cycle regulation etc. Furthermore, plumbagin also induces reactive oxygen species (ROS) generation and causes oxidative DNA damage. An exciting feature of plumbagin is its ability to sensitize chemo and radio resistant cancer cells. Even with significant anticancer potential, plumbagin is yet to be used in clinics due to its high lipophilicity, insolubility in water, short half-life, and low melting point. To conquer these limitations and possible exploitation of this potent natural compound, the scientific community has used several nano-based delivery systems, such as liposomes, niosomes, micelles, microparticles etc. Conclusion : Despite all these promising attributes, rigorous preclinical and clinical evaluations are essential to validate its actual anticancer potential before considering it as one of the mainstream phytotherapeutic agents. [Display omitted] • The current article is a comprehensive summary of anticancer potential of plumbagin in different cancer models. • The mechanism of action of plumbagin affecting different signaling cascade has been highlighted. • Despite their significant therapeutic potential, plumbagin is yet to be exploited in clinics. The reason and troubleshoot have been suggested. • Various nanoformulations of plumbagin have been covered that showed better efficacy compared to free plumbagin. [ABSTRACT FROM AUTHOR]

Monitoring the concentration of Fludarabine phosphate, a standard chemotherapeutic drug widely used in cancer treatment, is vital for ensuring the drug's safety and effectiveness, tailoring treatments to individual needs, and consequently improving overall patient outcomes. Regarding the limitations of conventional techniques in terms of complexity, large time measurements, and a high cost, there is an urgent need to develop simple, rapid, and cost-effective devices. In this paper, we report the design of an aptasensor for the specific and selective detection of Fludarabine. Systematic evolution of ligands by exponential enrichment (SELEX) protocol was performed to select a specific aptamer for Fludarabine. Eleven rounds were carried out, and nine sequences were selected. Based on the dissociation constant (Kd), Ful-3, exhibiting the highest affinity (18.86 nM), was chosen and integrated into a simple electrochemical aptasensing platform for Fludarabine detection. Electrochemical results demonstrated good performance of the selected aptamer in detecting Fludarabine within the analytical range of 1 to 150 pg/mL and with LOD and LOQ in the order of 0.11 pg/mL (0.31 fM) and 0.39 pg/mL (1.06 fM), respectively. The developed platform also showed good selectivity against different analogous molecules and high applicability in serum-spiked samples, with recovery percentages ranging from 96.81 to 99.04%. Considering the encouraging results, this research presents an excellent alternative in terms of simplicity, stability, ease of use, reduction of sample volume, and low cost. [ABSTRACT FROM AUTHOR]

Three groups of novel analogs of combretastatin-A4 (CA-4), viz., the N1-phenyl-pyrazoline (5a–e), N1-alkyl acetylated pyrazoline (6a–c), and N1-phenyl acetylated pyrazoline (7a–g) were designed, and synthesized in good yield. The structure of the compounds was confirmed by spectroscopic techniques. All the compounds were evaluated for their in vitro anticancer (MCF-7 cell line), antioxidant (DPPH, NO, SOR, and H2O2), and anti-inflammatory activity. Compounds 5d, 7g, 7f, 7e, 7c, 5b, 6a, 7b, and 7a showed excellent potency with GI50 ranging from 0.1 to 10.9 µM against the MCF-7 cell line. Compounds 7f, 7g, 5c, 5d, 5b, 7e, and 6a exhibited good anti-inflammatory activity. Encouraged by these results, all the compounds were also tested for their antioxidant potency. Compounds 6a, 6c, 7b, 7c, 7f, and 7g were found to be excellent scavengers of all four free radicals (DPPH, NO, SOR, and H2O2). [ABSTRACT FROM AUTHOR]

Quinoline is a N-containing heterocyclic organic compounds with significant biological importance in pharmaceuticals field as well as natural products. They exhibit excellent pharmacological activities. To synthesize quinoline and their derivatives several synthetic methods have reported, such as conventional method, ultrasonic method, microwave (MW) irradiation method, with or without catalytic reaction, which have various pharmacological and biological activities, such as antibacterial, antifungal, anticancer, anti-HIV, antimalarial, antitumor, and anti-inflammatory activity. The objective of this review is to compile various synthetic methods were used for the formation of the Quinoline derivatives and their biological importance, such as antibacterial, anticancer, anti-microbial, antimalarial, antileishmanial, antifungal, and anti-inflammatory during 2010–2023, which will help the researchers how are working in this area. [ABSTRACT FROM AUTHOR]

Purpose: Bladder cancer is a common genitourinary malignant disease worldwide. Dasatinib is a small molecule inhibitor of Src family kinases. We investigated the anticancer effect and putative molecular mechanisms of dasatinib on T24 and cisplatin-resistant T24R2 human bladder cancer cells. Materials and Methods: Cell proliferation was measured using Cell Counting Kit-8 (CCK-8) and colony formation in dasatinib treated bladder cancer cells. Flow cytometry was used to determined cell cycle arrest and apoptosis. The expression of apoptosis and autophagy related proteins were detected by western blot analysis. Results: In bladder cancer cells, dasatinib significantly reduced cell proliferation, colony formation, and induced G1-phase arrest. Dasatinib triggered apoptosis along with an increased expression of apoptosis-related genes (caspases, PARP, and cytochrome c). Down-regulation of Bcl-2 and up-regulation of Bad, which are hallmarks of apoptosis, were found to play a dominant role in mediating the effects of dasatinib treatment. We further showed that dasatinib inhibits p-Src, p-PI3K, p-Akt, and p-mTOR in bladder cancer cells. Dasatinib also increased the expression of markers of autophagy flux such as LC3-II and p62. Conclusions: These results confirmed that dasatinib is a potent chemotherapeutic drug which induces apoptosis and autophagy by suppressing the PI3K/Akt/mTOR pathway in bladder cancer cells. [ABSTRACT FROM AUTHOR]

The present research examines different techniques for isolating proteins from Cordyceps militaris fruiting body powder (COR), namely ammonium sulfate precipitation (ASP), organic solvent precipitation (OSP), and isoelectric precipitation (IEP). ASP yielded the highest protein content (78.90 %), effectively concentrating proteins, while OSP and IEP also produced substantial yields (57.41 % and 69.06 %, respectively). Color analysis revealed differences among isolates, with ASP resulting in a darker hue. ASP and IEP showed higher red and yellow components, respectively. Essential amino acid content was significantly higher in ASP isolate compared to COR, indicating effective amino acid concentration. Thermal analysis revealed different decomposition temperatures and enthalpy values among isolates. OSP displayed the highest phenolic content, while IEP exhibited the highest flavonoid content. Antioxidant assays showed ASP to have the highest DPPH-RSA and ABTS-RSA, while IEP showed the highest FRAP value. ASP demonstrated anticancer activity against HT-29 colon cancer cells inducing cell death apoptosis and inhibiting cell migration, with an IC 50 of 360.63 µg/mL, comparable to Paclitaxel. These findings suggest that Cordyceps militaris protein isolate, particularly from ASP, has significant antioxidant and anticancer potential, supporting its potential as a natural alternative to synthetic drugs with fewer side effects. [Display omitted] • ASP yields a higher protein (78.90 %) than OSP (57.41 %), and IEP (69.06 %). • ASP has a higher dark colour and essential amino acid content. • OSP has the highest total phenolic content, but IEP has the highest flavonoids. • ASP shows superior antioxidant and anticancer effects on HT-29 cells. • ASP emerges as a promising natural extract for health applications. [ABSTRACT FROM AUTHOR]

A wide range of bioactive compounds have been created using the versatile pharmacophore pyrimidine. In order to improve biological applications, we, therefore, envisioned adding these privileged moieties. In this work, we developed an efficient 2-aminopyrimidine derivatives. We further investigated the anticancer activity of all the compounds against colon cancer cell lines COLO-205 and HT-29. Out of several compounds synthesized, two compounds SD2 and SD4 have shown comparable potent anticancer activity when compared to standard Cabozantinib. The most potent cytotoxic compound against colon cancer cells in our study was found to be SD2 with an IC50 value of 9.57 μ M. The investigation from molecular docking showed the best binding affinity. The complex stability within an enzyme's pocket was demonstrated by the molecular dynamic simulation running for 100 ns. The work intends to critically search 2-aminopyrimidine derivatives for anticancer activity in two colon cancer cell lines (HT-29 and COLO-205). Advanced computational studies are carried out to provide more insight. Two compounds showed comparative anticancer activity in cytotoxicity and molecular modeling studies with standard. [ABSTRACT FROM AUTHOR]

Novel 2-imino-6-(aryldiazenyl)-2H-chromene-3-carboxamides 6a–e, 2-amino-4H-cyclopenta or benzo[b]thiophene-3-carboxamides 10a,b, 2,7-diaminopyrazolo[1,5-a]pyrimidine-6-carboxamides 13a–e, pyrimidine-5-carboxamides 14, 15 and 3-amino-1H-pyrazole-4-carboxamide 16 were synthesized from the reaction of 2-cyano-N-(1,3-dihydroxy-2-(hydroxyl-methyl) propan-2-yl) acetamide 2 with 4-arylazosalicylaldehydes 5a-e, cyclopentanone and/or cyclohexanone, guanidine derivatives and hydrazine hydrate, respectively. Some new compounds were evaluated for antibacterial activity in vitro, and exhibited good efficacy compared to gentamicin. Compound 4c showed greater activity against gram negative bacteria (Klebsiella pneumonia and Pseudomonas aeruginosa) than standard antibiotic. Compound 4c with two withdrawing groups also showed the higher activity (38.7 ± 0.6) against fungi (Candida albicans) than the Nystatin (20 ± 0.5). On the other hand, compounds 13a, 13c, and 13e have strong cytotoxic activity among the tested compounds in the three selected cancer cell lines (HePG2, MCF7 and Hela). Physicochemical characterization by Swiss ADME predication was also performed for some synthesized compounds exhibiting better biological and antimicrobial properties. [ABSTRACT FROM AUTHOR]

[Display omitted] • Updated the research progress of the tea's bioactivities and its health functions. • Provided an overview of the main chemical substances of tea and the pharmacological action. • Summarized the potential risk of tea and provide the suggestion of the future research and using direction. Tea (Camellia sinensis) has a rich history and is widely consumed across many countries, and is categorized into green tea, white tea, oolong tea, yellow tea, black tea, and dark tea based on the level of fermentation. Based on a review of previous literature, the commonly recognized bioactive substances in tea include tea polyphenols, amino acids, polysaccharides, alkaloids, terpenoids, macro minerals, trace elements, and vitamins, which have been known to have various potential health benefits, such as anticancer, antioxidant, anti-inflammatory, anti-diabetes, and anti-obesity properties, cardiovascular protection, immune regulation, and control of the intestinal microbiota. Most studies have only pointed out the characteristics of tea's bioactivities, so a comprehensive summary of the pharmacological characteristics and mechanisms of tea's bioactivities and their use risks are vital. This paper aims to summarize tea's bioactive substances of tea and their pharmacological characteristics and mechanisms, providing a scientific basis for the application of bioactive substances in tea and outlining future research directions for the study of bioactive substances in tea. This review summarizes the main biologically active substances, pharmacological effects, and mechanisms and discusses the potential risks. It may help researchers grasp more comprehensive progress in the study of tea bioactive substances to further promote the application of tea as a natural bioactive substance in the medical field. [ABSTRACT FROM AUTHOR]

Novel compounds with pharmacological activity were synthesized from Pd(II), Fe(III), Cr(III), Ni(II), and Cu(II) ions with 1‐cyclopropyl‐6‐fluoro‐4‐(2‐hydroxy‐phenylimino)‐7‐piperazin‐1‐yl‐1,4‐dihydro‐quinoline‐3‐carboxylic acid (CFAP). The ligand's NH and OH groups allowed it to interact with the metals as a neutral tridentate. The investigated novel compounds were described using 1H and 13C NMR spectra, FT‐IR spectrums, TGA and UV–Vis (conductance of molecules), and CHN‐analysis. Additionally, the pH profile of the CFAP complexes indicated great stability, and the complexes' stability constant was discovered in the solution. To extract important properties for CFAP and its complexes, computational research was used, CFAPCu, CFAPCr, CFAPNi, and CFAPFe have octahedral geometry, while CFAPPd has square planar geometry. To investigate the molecular geometry, density functional theory calculations (DFT) were carried out. The molar ratio and continuous fluctuation data confirmed that the (M:L) ratio was (1:1). In vitro tests were conducted to evaluate Schiff base's antimicrobial action ligand and its metal chelates against fungal and bacterial infections. The findings showed that the antimicrobial efficacy is as follows: When CFAPPd is compared to fluconazol and ofloxacin as reference medications, it is the highly inhibitor complex. The novel CFAP ligand and its complexes were investigated for In vitro carcinogenic potential against Hep‐G2, MCF‐7, and HCT‐116 cell lines. As compared to the medication vinblastine, the results once again demonstrated that CFAPPd is the most active agent. Moreover, the complexes demnstrated strong reactivity in capturing free radicals when their antioxidant activity was investigated. Viscosity, spectral investigations, and gel electrophoreses were used to identify the interaction between metal chelates and DNA. Every examined compound is shown to be an enthusiastic DNA binder by viscosity and spectrophotometric titration investigations. The heightened hydrophobic and electrostatic interactions between aromatic rings could be the cause of this. Ultimately, these compounds could be regarded as promising bioactive substances. [ABSTRACT FROM AUTHOR]

Dewatisari WF, To'bungan N. 2024. Review: Phytochemistry and ethnopharmacology of Dracaena trifasciata. Nusantara Bioscience 16: 169-184. Dracaena trifasciata (Prain) Mabb. (syn. Sansevieria trifasciata Prain.) or mother-in-law's tongue, is a species belonging to the genus Dracaena, widely cultivated and used by various communities. This plant is recognized as an ornamental, pollutant-absorbing, and textile material. Its leaves and roots have also been used as traditional remedies across Asia and Africa for cough, flu, respiratory tract inflammation, diarrhea, wound healing, and snakebites. Bioactive compounds found in the roots and leaves include alkaloids, tannins, terpenoids, saponins, steroids, phenols, methyl glucuronate acid, glycosides, cardenolides, polyphenols, carbohydrates, and abamagenin. Therefore, this review aims to provide insights into the phytochemical constituents and pharmacological potential of D. trifasciata. It also explores its use in traditional medicine and prospects for further advancement to promote the broader application. Comprehensive literature studies showed that the attributes of D. trifasciata can be applied as an antibacterial, antioxidant, and anticancer agent, having a promising source of natural compounds for novel drug development. Further investigations are needed to assess the long-term and short-term toxicity associated with the use of this plant material, thereby making it a potential source for the development of modern drugs from natural sources. Considering the extensive application of D. trifasciata as a natural remedy, further investigations are crucial to assess the pharmacological potential and safety. [ABSTRACT FROM AUTHOR]

Minor ginsenosides produced by β-glucosidase are interesting biologically and pharmacologically. In this study, new ginsenoside-hydrolyzing glycosidase from Furfurilactobacillus rossiae DCYL3 was cloned and expressed in Escherichia coli strain BL21. The enzyme converted Rb1 and Gyp XVII into Rd and compound K following the pathways: Rb1→Rd and Gyp XVII→F2→CK, respectively at optimal condition: 40 °C, 15 min, and pH 6.0. Furthermore, we examined the cytotoxicity, NO production, ROS generation, and gene expression of Gynostemma extract (GE) and bioconverted Gynostemma extract (BGE) in vitro against A549 cell lines for human lung cancer and macrophage RAW 264.7 cells for antiinflammation, respectively. As a result, BGE demonstrated significantly greater toxicity than GE against lung cancer at a dose of 500 µg/mL but in normal cells showed lower toxicity. Then, we indicated an enhanced generation of ROS, which may be boosting cancer cell toxicity. By blocking the intrinsic way, BGE increased p53, Bax, Caspase 3, 9, and while Bcl2 is decreased. At 500 µg/mL, the BGE sample was less toxic in normal cells and decreased the LPS-treated NO and ROS level to reduce inflammation. In addition, BGE inhibited the expression of pro-inflammatory genes COX-2, iNOS, IL-6, and IL-8 in RAW 264.7 cells than the sample of GE. In conclusion, FrBGL3 has considerable downstream applications for high-yield, low-cost, effective manufacture of minor ginsenosides. Moreover, the study's findings imply that BGE would be potential materials for anti-cancer and anti-inflammatory agent after consideration of future studies. [ABSTRACT FROM AUTHOR]

The present study summarizes the current available literature regarding the viability of MCF7 breast cancer cells treated with gold (Au), silver (Ag) or zinc oxide (ZnO) nanoparticles at varying doses for 48 h. The data for this study were obtained from diverse research articles published between 2013 and 2023 using Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA) 2020 guidelines. The evaluation focused on 20 PRISMA-compliant articles concerning MCF7 cells, yielding 137 outcome measures for meta-analysis. A generalized linear mixed model meta-analysis approach was employed to glean insights into the effects of novel nanoparticles on MCF7 breast cancer cells. The analysis covered a wide range of concentrations: Ag nanoparticles from 1.25 to 1,000 µg/ml, Au nanoparticles from 50 to 150 µg/ml, and ZnO nanoparticles from 1 to 1,000 µg/ml. Both intra-nanoparticle and inter-nanoparticle comparisons were conducted to detect differences. The findings showed that when concentrations reached or exceeded 60 µg/ml, considerable variation of cell viability was observed: Treatment with Ag nanoparticles resulted in cell viability ranging from 9 to 45%, ZnO nanoparticles resulted in cell viability ranging from 20 to 40%, and Au nanoparticles resulted in cell viability ranging from 3 to 58%. These findings indicated the signifi- cance of thoroughly exploring nanoparticle dosage to acquire a comprehensive understanding of their influence on cell viability. [ABSTRACT FROM AUTHOR]

Mushrooms of the genus Hericium spp. represent a series of delicious edible mushrooms with medicinal value. Here, for the first time, the species native to Iran, the mushroom Hericium coralloides, was collected in Mazandaran province, identified, and registered with the NCBI under accession number MW136052. The production of exopolysaccharides (EPS) in submerged culture was optimized using the response surface method. Among the physicochemical and culture medium conditions tested, rotation speed and concentration of maltose and peptone of soybean significantly affected the production of EPS. The proposed model predicts maximum EPS production (0.13 g/L) at 50 g/L maltose, 3 g/L soy peptone, and 1 g/L yeast extract, pH = 6.5, 200 rpm, inoculum at 5% v/v, and 22 °C. The molecular weight of the EPS chains was 413 and 1578 Da. EPS has antioxidant action (EC50 = 6.59 mg/mL) and cytotoxic activity against cancer cells. The viability of AGS and MKN-45 cancer cell lines declined to 20 and 30% after 48 h of the EPS treatment. H. coralloides EPS could be considered a natural dietary anti-cancer supplement. Further studies are necessary to understand the mechanism of the H. coralloides EPS activity on the cell cycle of cancer cells and to prove its action in vivo. [ABSTRACT FROM AUTHOR]

Kimchi is a Korean traditional vegetable fermented food with lactic acid bacteria (LAB). Fermented kimchi contains live LAB (probiotics), dietary fibers (prebiotics) and dead LAB and fermented metabolites (postbiotics), and it may have various health benefits. The taste and functionalities of kimchi are dependent on its main ingredients and subingredients, fermentation conditions, LAB in the fermentation, etc. There are many types of kimchi, but Baechu kimchi is the most popular and commonly used kimchi in Korea. Baechu kimchi is prepared by LAB fermentation of Baechu cabbage mixed with other subingredients such as radish, green onion, red pepper powder, garlic, ginger and fermented small sea fishes. Kimchi contains high levels of vitamins, minerals, dietary fibers and other functional components and fermented metabolites. Various studies have reported on kimchi and its antimutagenic and anticancer, antioxidative and antiaging, antiatherosclerotic, antidiabetic, antiobesity, and anti-inflammatory effects. Fermented kimchi contains high levels of LAB (108–9 CFU/g) and LAB also contribute functionalities to kimchi. We will discuss the process of manufacturing kimchi, fermentation of kimchi and related microorganisms. Though it briefly discuss on the general functionalities of kimchi, we will focus on the history and functions of the antiobesity, anticancer, and anti-inflammatory effects of kimchi in detail with better taste and preservation period. To increase the antiobesity and anticancer functions of kimchi we will introduce kimchi recipes, salt kinds, other added ingredients, etc. It was finally discussed on postbiotics in kimchi and their health benefits. [ABSTRACT FROM AUTHOR]

A series of (2E)-3-[2,4-bis(2-propen-1-yloxy)phenyl]-1-phenyl]-2-propen-1-ones—chalcone derivatives with O-allyloxy groups—were synthesized in good yields and characterized by different analytical techniques. Their anticancer activity was evaluated against the A549 (lung cancer) cell line. The most active compounds of this series were the 1-(4-fluorophenyl derivative 9c (IC50 = 0.48 ± 0.07 µM) and the 1-(4-octyloxy)phenyl derivative 9f (IC50 = 0.04 ± 0.01 µM). Network pharmacology analysis using the SwissTarget and DisGeNet databases identified potential targets for 9c in the Non-Small Cell Lung Carcinoma (NSCLC) cell line. Protein–Protein Interaction (PPI) network analysis revealed seven hub genes: MAPK14, PTGS2, HSP90AA1, MAPK8, NOS2, SYK, and NR3C1. Gene ontology analysis highlighted diverse biological functions. KEGG pathway analysis implicated pathways in cancer and immunoregulation. Molecular docking analysis suggested a strong interaction between 9c with MAPK14 (calculated docking score of –8.4 kcal mol–1). Compound 9c's potent activity warrants further preclinical and clinical evaluation as a potential NSCLC therapy Based on this results, study of heterocyclic compounds with O-allyloxy groups will help to explore their impact on anticancer activity and mechanistic pathway. [ABSTRACT FROM AUTHOR]

Copyright of Rare Metals is the property of Springer Nature and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

This research investigated the physicochemical properties and biological activities of green-synthesized copper oxide nanoparticles (CuO NPs) via Moringa peregrina extract, graphene oxide (GO), and their composite (CuO–GO). SEM revealed the morphology and structure, indicating polygonal CuO NPs, thin wrinkled sheets of GO, and a combination of CuO NPs and GO in the nanocomposite. EDS confirmed the elemental composition and distribution. XRD analysis confirmed the crystalline monoclinic structure of CuO NPs and GO, as well as their composite, CuO–GO, with characteristic peaks. DLS analysis exhibited distinct size distributions, with CuO NPs showing the narrowest range. BET surface area analysis revealed mesoporous structures for all materials, with the nanocomposite showing enhanced surface area and pore volume. Anticancer assays on MCF-7 and normal NIH/3T3 cells demonstrated CuO–GO's superior cytotoxicity against cancer cells, with minimal effects on normal cells, suggesting selective cytotoxicity. Moreover, antibacterial assays against Pseudomonas aeruginosa and Staphylococcus aureus indicated CuO–GO's potent inhibitory activity. The composite's synergistic effects were evidenced by its lower minimum inhibitory concentration (MIC) compared to individual components. In conclusion, this study elucidated the promising biomedical applications of CuO NPs, GO, and their nanocomposite, particularly in cancer treatment and antibacterial therapies, showcasing their potential as multifunctional nanomaterials. [ABSTRACT FROM AUTHOR]

A novel analogue of hybrid spirooxindoles was synthesized employing a systematic multistep synthetic approach. The synthetic protocol was designed to obtain a series of spirooxindole derivatives incorporating triazolyl- s -triazine framework via [3 + 2] cycloaddition (32CA) reaction of azomethine ylide (AY) with the corresponding chalcones (6a-d). Unexpectedly, the reaction underwent an alternate route, leading to the cleavage of the s-triazine moiety and yielding a series of spirooxindole derivatives incorporating a triazole motif. A comprehensive investigation of the 32CA reaction mechanism was conducted using Molecular Electron Density Theory (MEDT). The viability of all compounds was evaluated through an MTT assay, and the IC50 values were determined using Prism Software. The antiproliferative efficacy of the synthesized chalcones and the corresponding spirooxindole derivatives was assessed against two cancer cell lines: MDA-MB-231 (triple-negative breast cancer) and HepG2 (human hepatoma). These findings were compared with Sorafenib, which was used as a positive control. The results revealed that chalcones (6c and 6d) were the most active among the tested chalcones, with IC50 values of 7.2 ± 0.56 and 7.5 ± 0.281 µM for (6c) and of 11.1 ± 0.37 and 11.0 ± 0.282 µM for (6d) , against MDA-MB-231 and HepG2, respectively. Spirooxindoles (9b, 9c, 9h, and 9i) exhibited the highest activity with IC50 values ranging from 16.8 ± 0.37 µM to 31.3 ± 0.86 µM against MDA-MB-231 and 13.5 ± 0.92 µM to 24.2 ± 0.21 µM against HepG2. In particular, spirooxindole derivatives incorporating 2,4-dichlorophenyl moiety were the most active, with an IC50 of 16.8 ± 0.37 µM for (9h) against MDA-MB-23 and 13.5 ± 0.92 µM for (9i) against HepG2. Interestingly, the IC50 of compound (6c) (7.2 µM) exhibited better activity than that of Sorafenib (positive control) (9.98 µM) against MDA-MB-231. Molecular docking, ADMET, and molecular dynamic simulations were conducted for the promising candidates (6b, 6c, and 9h) to explore their binding affinity in the EGFR active site. [ABSTRACT FROM AUTHOR]

ABSTRACT Three novel complexes of copper(II), ruthenium(III), and thorium(IV) ions with quinaldine azo dye ligand HL were synthesized in nanoscale. Applying mass spectroscopy, electronic, infrared, 1H NMR, elemental, and thermal investigations, their structures were examined. By using azo nitrogen and hydroxyl oxygen atoms to coordinate as a monobasic bidentate, it was found that the ligand displayed bicapped square antiprism geometry with thorium(IV) metal ion, square pyramidal arrangement in copper(II) complex and octahedral configuration in ruthenium(III) complex. In order to confirm the complexes' geometrical arrangement, theoretical investigations were carried out using DFT/B3LYP/6–311 + G(d,p)/LANLDZ. The dipole moment, geometrical configuration, energetic parameters, and HOMO–LUMO gap of energy have been calculated. The compounds were formed in nanometric forms, as indicated by the mean particle sizes obtained by applying TEM. Based on TEM images for the complexes of copper(II), ruthenium(III), and thorium(IV), their average particle sizes were 11.04, 3.89, and 1.52 nm, respectively. PANC‐1 and A‐549 cells were used in the tests to evaluate the compounds' anticancer activity against the vinblastine reference. The findings confirm the great cytotoxicity effect of the free ligand and its complexes against the investigated cell lines using different doses of the examined compounds. Ru(III) and Cu(II) complexes exhibited cytotoxic effectiveness greater than that of vinblastine. The azo ligand, HL, exhibited the strongest antibacterial activity that is superior to that of the conventional medicines themselves and greater than that of its metal complexes. The most physiologically active compound's ideal conformation was found using molecular docking research, and the manner in which the Ru(III) complex and the enzyme of Panc‐1 link together was determined. It interacts in three different modes with the target receptor (PANC‐1): hydrophobic force, electrostatic force, and H‐bond. In addition to increasing the candidate activity, these interactions can be used to design and predict new, effective compounds. The capacity of the ligand and its complexes to act as heterogeneous catalysts for the oxidation of methyl violet 2B was examined. The ruthenium(III) and thorium(IV) complexes generated the greatest catalytic efficiencies. [ABSTRACT FROM AUTHOR]

To surpass the constraints associated with conventional therapeutic methods in clinical therapy, nanoparticles have been rapidly prepared and developed as a separate treatment method for diseases. In this study, we have synthesized bismuth oxide nanoparticles (BiNPs) using aqueous leaf extract of Mentha arvensis (M. arvensis) as a biogenic approach. The formation of BiNPs was confirmed by the characteristic peak observed at 276 nm in the UV–vis spectrum and PXRD analysis exhibited the crystalline nature with monoclinic phase. The TEM images revealed the quasi‐spherical shape of BiNPs with an average particle size of 12 nm. For biomedical studies, BiNPs exhibited significant cytotoxicity against A431 cell line (lung cancer) with IC50 value of 92.45 µg/mL. Further studies revealed significantly higher apoptosis, antibacterial, anti‐inflammatory, antidiabetic, and antioxidant activities of the biosynthesized BiNPs. The collective results from the study suggest that the M. arvensis mediated synthesis of multifunctional BiNPs enhances their biological potential, positioning it as a potential candidate for the multimodal therapeutic applications. [ABSTRACT FROM AUTHOR]

In response to the need for scaffolds for medical applications, synthetic chemists have developed simple and efficient methods for optimal synthesis. To investigate the synthesis of fused isoxazoles in the presence of [3+2] cycloaddition followed by C−N bond formation reaction between 3‐((4‐iodo‐3‐phenylisoxazol‐5‐yl)methyl)quinazolin‐4(3H)‐one and various nitrile oxides was carried out by previously reported conditions. The cancer activities of the synthesized compounds were then tested in vitro against two cancer cell lines, MCF‐7 and A‐549. Three of the compounds, 3‐(3,5‐dichlorophenyl) isoxazolo[4′,5′:3,4]pyrrolo[2,1‐b]quinazolin‐9(11H)‐one, 3‐(4‐fluorophenyl)isoxazolo[4′,5′:3,4]pyrrolo[2,1‐b]quinazolin‐9(11H)‐one, and 3‐(4‐(trifluoromethyl)phenyl)isoxazolo[4′,5′:3,4] pyrrolo[2,1‐b] quinazolin‐9(11H)‐one has shown superior activity against the non‐small‐cell lung cancer cell line (A‐549) than the standards 5‐fluorouracil and erlotinib. Later, in vitro EGFR results revealed that a more potent compound was more effective than the conventional medicine, erlotinib. In silico investigations of more potent compounds and erlotinib on the EGFR protein indicated that more potent compounds had comparable binding energies and inhibition constants to erlotinib. [ABSTRACT FROM AUTHOR]

Over the past 10 years, nanotechnology has emerged as a very promising technique for a wide range of biomedical applications. Green synthesized metal and metal oxide nanoparticles (NPs) are cheap, easy to produce in large quantities, and safe for the environment. Currently, efforts are being made to dope ZnO in order to improve its optical, electrical, and ferromagnetic qualities as well as its crystallographic quality. Actually, doping is one of the simplest methods for enhancing an NP's physicochemical characteristics because it involves introducing impure ions into the crystal lattice of the particle. In this study, the biosynthesis of zinc oxide NPs (ZnONPs) and metal‐doped (Mg2+ and Ag+) ZnONPs was carried out by using aqueous and water‐alcoholic extracts of Cynara scolymus L. leaves, Carthamus tinctorius L. flowers, and Rheum ribes L. (RrL) plant, which are rich in phytochemical content. Plant extracts act as a natural reducing, capping, and stabilizing agent in the production. The produced NPs were characterized using a variety of methods, such as ultraviolet‐visible spectroscopy, Fourier transform infrared (FTIR) spectroscopy, dynamic light scattering (DLS), and scanning electron microscopy (SEM). The produced metal‐doped and undoped ZnONPs exhibited characteristic absorption peaks between 365 and 383 nm due to their surface plasmon resonance bands. SEM analysis revealed that the NPs were oval, nearly spherical, and spherical. In the FTIR spectra, the Zn–O bonding peak ranges from 400 to 700 cm−1. The peaks obtained in the range of 407–562 cm−1 clearly represent the Zn–O bond. In addition, the FTIR results showed that there were notable amounts of phenol and flavonoid compounds in both the prepared extract and ZnONPs. According to DLS analysis results, the size distribution of produced NPs is between 120 and 786 nm. The antibacterial properties of green produced NPs on Gram‐positive (Staphylococcus aureus RN4220) and Gram‐negative (Escherichia coli DH10B) bacterial strains were investigated by agar well diffusion method. In studies investigating the anticancer activities of biosynthesized NPs, mouse fibroblast cells (L929) were used as healthy cells and human cervical cancer cells (HeLa) were used as cancer cells. Only the produced Ag‐ZnONPs showed potent dose‐dependent antibacterial activity (at concentrations higher than 100 µg/mL) against Gram‐positive and Gram‐negative bacteria. RrL‐ZnONP‐600 and RrL‐ZnONP‐800 NPs produced with water–ethanol extract of RrL plant and calcined at 600 and 800°C were effective at high concentrations in healthy cells and at low concentrations in HeLa cancer cells, showing that they have the potential to be anticancer agents. The study's findings highlight the potential of green synthesis techniques in the production of medicinal nanomaterials for the treatment of cancer and other biological uses. [ABSTRACT FROM AUTHOR]

Green tomatoes contain significant levels of steroidal glycoalkoids (SGA) such as α-tomatine and green pigment chlorophyll. Tomatine is an admixture of two glycoalkoids; alpha tomatine and dehydrotomatine reported various health beneficial biological activities. Moreover, a hydrolyzed product of tomatine also contributes to age-related atrophy, and muscle weakness and helps the elderly recover from illness and injuries related to age. However, there is a lack of evidence regarding the absorption of tomatine in the human body concerning proposed biological activity, which should be an area of interest in the future. Once, the absorption study is established compounds concentrated in green tomatoes are potentially involved as protective compounds for several diseases and also used for functional food. To facilitate the use of green tomatoes in food processing, this comprehensive review provides data on the nutritional value of green tomatoes, with emphasis on the evolution of the physiological chemistry, analytical, medicinal, and pharmacological effects of the α-tomatine and chlorophyll in an experimental model. The broad aim of this review is to evaluate the health benefits of green tomatoes in addition to their nutritional value and to study the several features of the role of α-tomatine and chlorophyll in human health. [ABSTRACT FROM AUTHOR]

Ocimum tenuiflorum, commonly known as Tulsi, is revered in Ayurveda for its extensive medicinal properties. However, there is a need to consolidate current knowledge on its phytochemical constituents and their pharmacological activities to identify potential areas for further research and drug development. This review aims to bridge this gap by providing a comprehensive analysis of the bioactive secondary metabolites found in O. tenuiflorum, such as rosmarinic acid, oleanolic acid, luteolin, ursolic acid, and limonene, and their associated therapeutic effects. The review will highlight the pharmacological importance of these metabolites, which exhibit antioxidant, neuroprotective, anticancer, and anti‐inflammatory properties. Additionally, this study will explore the plant's wide range of beneficial qualities, including anti‐inflammatory, antioxidant, anticholinergic, pain‐relieving, antimicrobial, stress‐reducing, antidiabetic, anticancer, liver‐protective, ulcer‐inhibiting, antifungal, and wound‐healing attributes. Furthermore, this review focuses on the plant's potential in treating conditions such as asthma, persistent fever, tuberculosis, malaria, skin discoloration, itching, digestive issues, hemorrhoids, bone fractures, gout, urinary tract infection, and diabetes. By reviewing the current literature, the aim is to identify the gaps in the existing research and propose directions for future studies. This comprehensive review will serve as a valuable resource for researchers in the development and investigation of novel drugs derived from O. tenuiflorum. [ABSTRACT FROM AUTHOR]

Scorpion venom may include pharmacological substances that have the potential to provide benefits. Multiple scientific investigations have shown that particular scorpion venoms induce apoptosis and inhibit the development of cancerous cells. The present study investigated the potential anticancer properties of the crude venom derived from Hottentotta saulcyi (H. saulcyi) on both in vivo mice models and in vitro breast carcinoma cells. The venom of scorpions belonging to the species H. saulcyi was obtained with the application of electrical stimulation at voltages of 8 and 10 V. The determination of the Average Lethal Dose 50 (LD50) was conducted. The present work assessed the in vitro cytotoxicity and morphological characteristics of H. saulcyi venom using fluorescence microscopy, MTT assay, and flow cytometry assessment. Additionally, research was performed to assess the cytotoxic effects in vivo on a mouse model with breast cancer. The examination of MCF-7 cells treated with scorpion venom at a microscopic level revealed the existence of cells undergoing apoptosis. The venom of H. saulcyi has anticancer properties, as shown by the observation that MCF-7 cells had a 62.12% apoptotic rate when exposed to a dose of 1.47 mg/L. Based on the results obtained, it can be shown that the viability of MCF-7 cells has exhibited a substantial reduction (P < 0.01). Furthermore, the findings indicated that the venom of H. saulcyi resulted in a significant increase in the synthesis of TNF-α, IL-6, IL-10, TGF-β, and caspase (P < 0.05). The treatment groups administered with H. saulcyi venom exhibited a significant augmentation in the expression of proapoptotic genes compared to the control group of healthy individuals. The transcription of the BCL2 gene exhibited a statistically significant increase in the healthy control group compared to both the healthy venom-treated group (P < 0.05) and the malignant venom-treated group (P < 0.01). The crude venom of H. saulcyi has considerable promise in demonstrating anticancer properties. Further investigation may be warranted to explore the potential of using H. saulcyi crude venom as a medicinal platform for the prevention of breast cancer. [ABSTRACT FROM AUTHOR]

It has been known since the 1990s that the introduction of a ferrocenyl–type substituent into compounds with proven biological activity can improve their properties. More recently, it was also shown that a carbon bridge connecting the two cyclopentadienyl rings in ferrocene derivatives could enhance the biological properties of the new compounds compared to those without them. However, the synthesis of ferrocenes with this additional linker, known as ansa–ferrocenes, is more difficult due to advanced synthetic protocols and the phenomenon of planar chirality in ring–substituted compounds. As a result, research into the formation of hybrids, conjugates and other ansa–ferrocene derivatives has not been widely conducted. This review discusses the potential biological properties of these units, covering scientific articles published between 1980 and 2024. [ABSTRACT FROM AUTHOR]

Approximately 20 million new instances of cancer and 10 million cancer-related deaths were reported in 2023, making cancer one of the leading causes of mortality globally. The number of deaths due to cancer worldwide is expected to double by 2050 to an estimated 18.5 million, compared to 9.7 million in 2022. Though there are heaps of new advanced techniques and therapies present for the treatment or control of cancer exist; however, complete treatment is not yet available. Chemotherapy and radiation-based therapy are examples of cancer treatments that function by eradicating or damaging cancer cells, which may sometimes negatively affect as well as harm normal cells throughout the process. Phyto-pharmaceuticals have shown promising results in the management of cancer due to potential anticancer efficacy. There is a large variety of medicinal herbs that exhibit anticancer properties; however, few are known and not yet evaluated in humans. Recently these bioactive compounds were combined with modified medications driven by nanotechnology (NT), and drug delivery systems are being fabricated and commercialized to improve the management of cancer with positive results. Drug delivery to cancer cells can be made more effective using nano-carriers with prolong medication half-lives, improve solubility and stability, and lessen side effects in organs other than the target. The review focuses on a new nano-enabled approach to delivering the medication that leverages bioactive compounds in either entrapped or tagged to carriers. Additionally, the review provides a sense of the obstacles and constraints associated with conventional cancer therapy, as well as the bioavailability of bioactive compounds. [ABSTRACT FROM AUTHOR]

ABSTRACT A thiophosphoric triamide (SPT) ligand P(S)[NH‐2Py]3 was synthesized and utilized as a ligand to make novel binuclear and mononuclear Co2+ and Cd2+ complexes. The compounds are the first examples of discrete chelate SPT complexes with a [N]3P(S)‐based backbone in which the SPT acts as a flexible tridentate N,N,N‐donor or N,N,O‐donor ligand. The metal cation features a hexacoordinate environment M(N)3(Cl)3/M(N)4(O)2 adopting a distorted octahedral geometry. Hirshfeld surface analysis affirms that the pyridinyl nitrogen is a more dominant H‐bond acceptor than the thiophosphoryl sulfur atom. The inhibitory activity against the MDA‐MB‐231 cancer cell line in vitro indicated a good inhibitory effect for all compounds. The mononuclear Co2+ complex showed a stronger inhibitory activity against cancer cells than other studied compounds with an IC50 of 62 ± 1.4 nM. Antioxidant and antihemolytic activity of the compounds showed appreciable performance with the highest activities for the Cd2+ complex. A computational DNA binding study by molecular docking indicated a good affinity of the compounds with the DNA receptor by a mixed mode of interactions. Docking was also performed on SARS‐CoV‐2 and monkeypox (Mpox), resulting in binding energies (−5.5 to −8.9 kcal/mol) that are competitive with current effective drugs. [ABSTRACT FROM AUTHOR]

ABSTRACT This work reports the preparations and anticancer activities of a set of platinum (II) complexes. Two types of bidentate ligands, azadiphosphine (PNP) and diphosphine (PP), were applied to afford different kinds of platinum centers, the homoleptic complexes, [Pt (PNP)2]2+ (1 and 2) and [Pt (PP)2]2+ (4), and the hybrid complex, [Pt (PNP)(PP)]2+ (3). All these complexes are characterized by various analytical techniques, and their structures were validated using single‐crystal X‐ray diffraction analysis. Notably, the stability of the complexes 1–4 is differentiated both in phosphate‐buffered saline (PBS) and in the culture media (RPMI‐1640), relative to the type of coordinated diphosphine ligands, specifically, the more PNP ligands, the less stability. The bite angles of P‐Pt‐P bonds in 1–4 would be reliant on their stability, so that complexes 1 and 2 with small bite angles tend to be labile. A mechanistic understanding on the decomposition of 2 is proposed with the aid of mass analysis. As a result, their anticancer activities should be also associated with their stability so that the chelated ligands, with more PNP ligands, lead to more cytotoxicity. Mechanistically, the poisonous platinum (II) derivatives of complex 2 should interact with the nucleus DNA, whereas the intact complex 4 is not traceable, confirming from a γ‐H2AX‐related immunofluorescence staining kit. Additionally, complex 2 exhibits severe toxicity toward several cancer cells as well as a normal cell. Furthermore, complex 2 has inhibited the formation and viability of three‐dimensional T24 mammospheres, reminding it of a promising candidate for anticancer treatments. Overall, the present work provides a way for the systematic investigation to elucidate how a bidentate diphosphine ligand modulates the stability and the anticancer activities of the corresponding square‐planner platinum (II) complex. [ABSTRACT FROM AUTHOR]

Lung cancer is the most diagnosed malignant neoplasm worldwide and it is associated with great mortality. Currently, developing antineoplastic agents is a challenging, time-consuming, and costly process. Computational methods can speed up the early discovery of anti-lung-cancer chemicals. Here, we report a perturbation theory machine learning model based on a multilayer perceptron (PTML-MLP) model for phenotypic early antineoplastic drug discovery, enabling the rational design and prediction of new molecules as virtual versatile inhibitors of multiple lung cancer cell lines. The PTML-MLP model achieved an accuracy above 80%. We applied the fragment-based topological design (FBTD) approach to physicochemically and structurally interpret the PTML-MLP model. This enabled the extraction of suitable fragments with a positive influence on anti-lung-cancer activity against the different lung cancer cell lines. By following the aforementioned interpretations, we could assemble several suitable fragments to design four novel molecules, which were predicted by the PTML-MLP model as versatile anti-lung-cancer agents. Such predictions of potent multi-cellular anticancer activity against diverse lung cancer cell lines were rigorously confirmed by a well-established virtual screening tool reported in the literature. The present work envisages new opportunities for the application of PTML models to accelerate early antineoplastic discovery from phenotypic assays. [ABSTRACT FROM AUTHOR]

This study's objective was to evaluate the chemical characterization and biological activities of sulphated polysaccharides isolated from Grateloupia catenata. The sulphated polysaccharide yield was 28.71±09%, with carbohydrate, protein, ash, and moisture content of 92.05±32%, 0%, 21.08±06%, and 4.03±29%. Carbon, hydrogen, nitrogen, and sulphur content of the sulphated polysaccharide were determined to be 33.07±21%, 4.21%±05, 2.15%±38, and 3.98±15%, correspondingly. The polysaccharide's functional group was investigated using FT-IR. The sulphated polysaccharide demonstrated commendable antioxidant activity such as DPPH radicals, ABTS radicals, superoxide radicals, and hydroxyl radicals' activity were 18.31–71.38%, 20.73–70.01%, 19.81–72.01%, and 18.72%–73.22% at the concentration of 50–250 μg/ml. Sulphated polysaccharide's anticancer action against the A549 cell line was 21.98–70.41% at the concentrations of 50–250μg/ml. The results show that the sulphated polysaccharide exhibits strong antioxidant and anticancer action. As a consequence, the sulphated polysaccharide from G. catenata may serve as a food supplement, a natural antioxidant and anticancer, or as an ingredient in the pharmaceutical sector. [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]

Quinazolinone and thiouracil derivatives are key scaffolds in anticancer development. This study used a molecular hybridization approach to synthesize new quinazolinone‐thiouracil derivatives and evaluated their anticancer activity against three human cancer cell lines, namely breast, lung, and glioblastoma, using SRB assay. Structural elucidation was performed using IR spectroscopy, 1H‐NMR, 13C‐NMR, mass spectrometry, and elemental analysis. Most compounds show moderate to significant cytotoxic effects, with compound 5d displaying the highest potency (IC50 values of 5.28, 4.02, and 2.88 µM, respectively). Compound 5d also demonstrated comparable potency to positive controls cisplatin and temozolomide in lung and glioblastoma cancer cell lines and was nearly as effective as mitochondrial division inhibitor‐1 (mdivi‐1). Furthermore, molecular docking analyses revealed strong binding interactions of the synthesized compounds with dynamin‐related protein‐1 (drp1). Protein–ligand stability studies and all‐atom simulation confirmed the stable binding of compound 5d with drp1. In conclusion, this study identified compound 5d as a potent drp1 inhibitor and promising anticancer drug candidate, deserving further investigation. [ABSTRACT FROM AUTHOR]

Nine new coumarin derivatives of 2‐(7‐hydroxy‐2‐oxo‐2H‐chromen‐4‐yl)acetic acid 6a–i have been successfully synthesized through amide coupling with various substituted anilines and 2‐aminopyridines. The synthesized derivatives were screened for anticancer activity using MTT assay on MCF‐7 cell line. The results showed that compound 6b inhibited MCF‐7 cell growth in a dose‐dependent manner and reached 47% inhibition at 40 µM, being better than starting material 5 and references 3 and 5FU drug. Moreover, 6b inhibited significantly 3D tumorsphere formation. The para‐Br substitution of 6b seems to be important for activity. Docking study suggests estrogen receptor and/or 3a‐HSD type 3 protein could be the target(s) for anticancer activity of this class of compounds. Further optimization of compound 6b should lead to more potent compound. [ABSTRACT FROM AUTHOR]

Cancer is a longstanding worldwide issue, current chemotherapeutic treatments have limited effectiveness and high toxicity. An extensive investigation has revealed a significant potential link between ITK and the development of cancer. Hence, it is recommended to prioritize investigating ITK to develop and produce novel inhibitors for treating diseases associated with T cells. In our study, we have designed and synthesized two new series of compounds, which consist of cinnamic acid, carbohydrazide, and cyclopropanamide groups in a single compound. We have developed a facile method to synthesize 20 new derivatives of two series of innovative 1‐phenyl‐N'‐(3‐phenylacryloyl)cyclopropane carbohydrazide derivatives with good yields and purity. The Synthesized derivatives are conformed by analytical techniques (FT‐IR, 1H NMR, 13C NMR, elemental analysis) and their biological evaluation data is provided. The synthesized compounds displayed favorable docking scores in comparison to the ITK inhibitor, Ibrutinib. The in vitro cancer investigation shows that these compounds have good IC50 values, causing cytotoxicity against malignant cell lines. [ABSTRACT FROM AUTHOR]

During extensive field explorations of the Lateritic area in West Bengal, one remarkable wild Russuloid macrofungus, ethnically termed "Kend Patra," was collected. The species was known to enrich the diet of the local people, being considered as income source for some tribal groups. Using morphological characters and molecular analysis of this collection, provide a unique placement of the taxon in the Russula subgenus Compactae (Fr.) Bon. Further in order to find functional constituents for biopharma applications, methanolic extract was prepared that shows the existence of a substantial amounts of phenol, flavonoid, ascorbic acid and carotenoids. Antioxidant activity was determined where the fraction demonstrated strong DPPH, ABTS, and nitric oxide radical scavenging activities, high Fe2+ ion chelating ability, and a reducing power with EC50 values ranging from 538.69 to 891.75 µg/ml. The extract was found to be effective against Listeria monocytogenes, Bacillus subtilis, Pseudomonas aeruginosa, Escherichia coli, Salmonella typhi and Staphylococcus aureus. In addition, the extract exhibited potent anticancer activities as it inhibited A549 cell proliferation, caused morphological changes, elevated ROS levels, hindered the clonogenic ability and migratory potential of cancerous cells, arrested cell cycle progression at S phase, and induced apoptosis by modulating the intrinsic mitochondrial pathway. Overall, this study contributes a new species to the world's myco-diversity and presents an exciting opportunity for future researchers to conduct comprehensive investigations on this unique species in order to uncover potential new medications for human use. [ABSTRACT FROM AUTHOR]

Background: Cancer is the most lethal disease in humans, accounting for one out of every six fatalities. The most frequent type of cancer among women is breast cancer, followed by cervix cancer. Iron oxide nanoparticles, due to their superparamagnetic traits, are one of the most widely used nanomaterials for diagnosing and treating breast cancer. For site-specific medication delivery, biotin was coupled with magnetite nanoparticles. Materials and Methods: The dextran-coated IONP was synthesized by a simple coprecipitation process and biotin was attached to the surface of dextran via a carboxylic/amine group. X-ray Diffractometer, Thermal gravimetric Analysis, Fourier Transformed Infrared Spectrometer, Atomic Force Microscopy and Vibrating Sample Magnetometer were used to investigate the structural, morphological, and magnetic properties of the produced materials. Results and Discussion: The iron oxide nanoparticle particle size was determined to be 325 nm. The MTT assay of IONPs and dextran-coated biotin-conjugated IONPs with low IC50 values of 24.18 μg/mL and 1.66 μg/mL exhibit cytotoxicity toxicity against MCF 7 cells, whereas the cytotoxicity of biotin-linked IONPs higher when compared with pure iron oxide. Conclusion: Iron oxide nanoparticle and dextran-coated biotin-conjugated iron oxide nanoparticle results confirmed the anti-breast cancer efficacy on human breast cancer cells by causing effective cytotoxicity and ensuring the drug delivery to a specific site. [ABSTRACT FROM AUTHOR]

Mangiferin is a bioactive substance present in high concentration in mangoes and also in some other fruits. Owing to its potential as a chemopreventive and chemotherapeutic agent against several types of cancer, this unique, significant, and well‐researched polyphenol has received a lot of attention recently. It possesses the ability to treat cancers, including rectal cancer, prostate cancer, ovarian cancer, leukemia, gastric cancer, liver cancer, chronic pancreatitis, and lung cancer. It can control/regulate multiple key signaling pathways, such as signal transducer and activator of transcription 3 (STAT3), second mitochondria‐derived activator of caspases/direct inhibitor of apoptosis (IAP)‐binding protein with low propidium iodide (pl) (Smac/DIABLO) nuclear factor kappa B (NF‐κB), phosphatidylinositol 3 kinase/protein 3 kinase (PI3K/Akt), transforming growth factor beta/suppressor of mothers against decapentaplegic (TGF‐β/SMAD), c‐jun N‐terminal kinase/p38 mitogen‐activated protein kinase (JNK/p38‐MAPK), and phosphor‐I kappa B kinase (p‐IκB), which are crucial to the development of cancers. By triggering apoptotic signals and halting the advancement of the cell cycle, it can also prevent some cancer cell types from proliferating and developing. It has been revealed that mangiferin targets a variety of adhesion molecules, cytokines, pro‐inflammatory transcription factors, kinases, chemokines, growth factors, and cell‐cycle proteins. By means of preventing the onset, advancement, and metastasis of cancer, these targets may mediate the chemopreventive and therapeutic effects of mangiferin. Mangiferin has confirmed potential benefits in lung, cervical, breast, brain, and prostate cancers as well as leukemia whether administered alone or in combination with recognized anticancer compounds. More clinical trials and research investigations are required to completely unleash the potential of mangiferin, which may lower the risk of cancer onset and act as a preventive and therapeutic alternative for a number of cancers. [ABSTRACT FROM AUTHOR]

Many naturally derived compounds are currently used in oncotherapy. Besides official medicine, complementary and alternative medicine practices, including old herbal remedies, are widely used and accepted as additional tools in cancer treatment. Angelica gigas Nakai (AGN), a medicinal herb in Asia, has roots historically used in medicine. This review focuses on key bioactive compounds from AGN roots – decursin, decursinol angelate (DA), and decursinol (DOH). Exploring their source, biosynthesis, and therapeutic mechanisms, the review highlights their role in cancer treatment. Biotechnological strategies for enhanced production and semisynthetic derivatives with anticancer properties are discussed. The study emphasizes the promising pharmacological potential of decursin, DA, and DOH in various therapeutic applications, particularly cancer treatment. The review also underscores innovative approaches to increase production and explores semisynthetic derivatives as a promising avenue for future natural product‐based drug discovery. This concise overview provides valuable insights into the potential of AGN‐derived compounds in the field of natural product‐based therapeutics. [ABSTRACT FROM AUTHOR]

A series of new 2-(2-aryl amino) phenyl acetamide derivatives were synthesized and their chemical structures were identified using spectroscopic techniques (UV-VIS, FTIR, 1HNMR, and MS). Computational studies have been carried out for prediction reactivity and density function theory (DFT) calculations for the acetamide derivatives, as well as the spatial electron distribution of the highest occupied molecular orbital (HOMO) and lowest unoccupied molecular orbital (LUMO) were computed. The docking study against prostaglandin synthetase-2 (COX-II coenzyme) was computed, and four compounds (D, F, H, and L) gave high scores (Kcal/mol). Some of these synthetic compounds were evaluated for their biological activities in vitro (antimicrobial, antioxidant, anticancer, and anti-inflammatory). Finally, the compounds B, D, F, and K have a good correlation between theoretical and experimental studies as cyclooxygenase inhibitors and weak to moderate antimicrobial, antioxidant, and cancer activities. [ABSTRACT FROM AUTHOR]

Yohimbine is a potent bioactive indole alkaloid, isolated from a variety of biological sources and has long been used as a natural stimulant and aphrodisiac, particularly to treat erectile dysfunction. However, some literature also points toward its anticancer effect in different experimental models. The current study aimed to address a clinical concern on the therapeutic utilization of yohimbine as a repurposed drug. We employed 7,12‐dimethylbenz[a]anthracene (DMBA)‐induced hamster buccal pouch carcinogenesis model juxtaposed with biochemical investigation of several detoxification and antioxidant markers, such as Cyt p450, Cyt b5, thiobarbituric acid reactive substance (TBARS), glutathione (GSH), glutathione reductase (GR), glutathione S transferase (GST), DT‐diaphorase, vitamin C, vitamin E, superoxide dismutase (SOD), catalase (CAT), and glutathione peroxidase (GPx). The immunohistochemical assessment of cyclooxygenase‐2 (COX‐2), interleukin‐6 (IL‐6), proliferating cell nuclear antigen (PCNA), and cyclin D1 expression were also performed to observe the effect of yohimbine on these markers. The hamsters treated with DMBA presented the growth of tumors in the buccal pouches, accompanied by significant changes in the liver and buccal mucosa levels of Phase I & II detoxification enzymes and lipid peroxidation (LPO). A significant rise in the range of 2‐ to 3.5‐fold was observed in Cyt p450, Cyt b5, and LPO in DMBA‐treated animals. However, oral administration of yohimbine significantly restored the LPO, antioxidant, and detoxifying enzyme activities. Additionally, the levels of COX‐2, IL‐6, PCNA, and cyclin D1 were also found to be downregulated by yohimbine treatment. In conclusion, yohimbine improved the biochemical and immunohistochemical markers of DMBA‐induced oral cancer and reverted to near normal values via ameliorating the underlying inflammation and oxidative stress conditions. Our study highlighted the potential of yohimbine as anticancer agent, especially against oral cancer and suggested its possible use as repurposed drug. Summary: In this study, we have used hamster model to evaluate potential of yohimbine against oral carcinogenesis.Yohimbine reinstated DMBA‐induced oral carcinogenesis and facilitated detoxification by modulating the Phase I and Phase II enzyme activities.The upregulated expression of Cox‐2, IL‐6, PCNA, and cyclin D1 was also found to be reverted to near normal by yohimbine treatment. [ABSTRACT FROM AUTHOR]

Indole derivatives have become an important class of compounds in medicinal chemistry, recognized for their wide-ranging biological activities and therapeutic potential. This review provides a comprehensive overview of recent advances in the evaluation of indole-based compounds in the last five years, highlighting their roles in cancer treatment, infectious disease management, anti-inflammatory therapies, metabolic disorder interventions, and neurodegenerative disease management. Indole derivatives have shown significant efficacy in targeting diverse biological pathways, making them valuable scaffolds in designing new drugs. Notably, these compounds have demonstrated the ability to combat drug-resistant cancer cells and pathogens, a significant breakthrough in the field, and offer promising therapeutic options for chronic diseases such as diabetes and hypertension. By summarizing recent key findings and exploring the underlying biological mechanisms, this review underscores the potential of indole derivatives in addressing major healthcare challenges, thereby instilling hope and optimism in the field of modern medicine. [ABSTRACT FROM AUTHOR]

Naphthylimides play a pivotal role as aromatic heterocyclic compounds, serving as the foundational structures for numerous pharmacologically significant drugs. These drugs encompass antibacterial, antifungal, anticancer, antimalarial, antiviral, anti-inflammatory, antithrombotic, and antiprotozoal agents. The planar and heteroaromatic characteristics of naphthylimides grant them a strong ability to intercalate into DNA. This intercalation property renders naphthylimide derivatives highly valuable for various biological activities. The advantageous pharmacological activity and ease of synthesis associated with naphthylimides and their derivatives provide significant benefits in the design and development of new compounds within this class. Currently, only a few such molecules are undergoing preclinical and clinical evaluations. In this paper, we have compiled the literature on naphthylimides reported by researchers from 2006 to 2024. Our focus lies on exploring the pharmacological activities of their analogues from a drug development and discovery perspective, while examining their structure–activity relationship and mechanisms of action. [ABSTRACT FROM AUTHOR]