Bio-molecular Fe(III) and Zn(II) complexes stimulate the interplay between PI3K/AKT1/EGFR inhibition and induce autophagy and apoptosis in epidermal skin cell cancer.

This study investigated the effectiveness and safety of a hybrid thiosemicarbazone ligand (HL) and its metal complexes (MnII-L, FeIII-L, NiII-HL, and ZnII-HL) against epidermoid carcinoma (A-431). The results indicated that FeIII-L is the most effective, with a high selectivity index of 8.01 and an IC50 of 17.49 ± 2.12 µM for FeIII-L. The study also revealed that the synthesized complexes effectively inhibited gene expression of the Phosphoinositide 3-kinases (PI3K), alpha serine/threonine-protein kinase (AKT1), epidermal growth factor receptor (EGFR2) axis mechanism (P < 0.0001). Additionally, these complexes trigger a chain of events that include the inhibition of proliferating cell nuclear antigen (PCNA), transforming growth factor ß1 (TGF ß1), and topoisomerase II, and leading to a decrease in epidermoid cell proliferation. Furthermore, the inhibitory activity also resulted in the upregulation of caspases 3 and 9, indicating the acceleration of apoptotic markers, and the down regulation of miRNA221, suggesting a decrease in epidermoid proliferation. Molecular modeling of FeIII-L revealed that it had the best binding energy -8.02 kcal/mol and interacted with five hydrophobic π-interactions with Val270, Gln79, Leu210, and Trp80 against AKT1. Furthermore, the binding orientation of FeIII-L with Topoisomerase II was found to be the most stable, with a binding energy -8.25 kcal/mol. This stability was attributed to the presence of five hydrophobic π-interactions with His759, Guanin13, Cytosin8, and Ala465, and numerous ionic interactions, which were more favorable than those of doxorubicin and etoposide for new regimens of chemotherapeutic activities against skin cancer.

New multifunctional hybrids as modulators of apoptosis markers and topoisomerase II in breast cancer therapy: synthesis, characterization, and in vitro and in silico studies.

Recently, molecular hybrids of two or more active pharmacophores have shown promise for designing and synthesizing anticancer drugs. Herein, a new multifunctional hybrid (PAHMQ), combining azobenzene and quinoline pharmacophores, and its M(ii) complexes (MPAHMQ) have been successfully developed and structurally characterized. The MTT assay revealed CuBHTP as the most efficient and safe breast cancer treatment, with an IC50 of 11.18 ± 0.39 µg mL-1 and a high selectivity index (SI) of 5.63 for cancer MCF-7 cells over healthy MCF10A cells. Moreover, the CuPAHMQ-treated MCF-7 cells experience a dramatic impact with regard to key apoptotic markers, including an increase in P53 and Bax expression, with a decrease in Bcl-2 expression levels compared to the untreated MCF-7 cells. Additionally, CuPAHMQ effectively halted the growth and division of MCF-7 cells by inducing cell cycle arrest in the crucial G1 and S phases, ultimately inhibiting both Topo II activity and cell proliferation. Molecular docking investigations validated the CuPAHMQ complex's groove binding and topoisomerase II binding, establishing it as a potent anticancer drug.

Correction: New multifunctional hybrids as modulators of apoptosis markers and topoisomerase II in breast cancer therapy: synthesis, characterization, and in vitro and in silico studies.

[This corrects the article DOI: 10.1039/D4RA04219K.].

Fabrication and characteristics of new quaternized chitosan nanocapsules loaded with thymol or thyme essential oil as effective SARS-CoV-2 inhibitors.

This research explores the potential of encapsulating thyme essential oil (TEO) and thymol (TH) into quaternized chitosan nanocapsules to combat SARS-CoV-2. Initially, the bioactive materials, TH and TEO, were extracted from Thymus vulgaris and then structurally and phytochemically characterized by spectral and GC-MS analyses. Meanwhile, O-quaternized ultrasonic-mediated deacetylated chitosan (QUCS) was successfully synthesized and characterized. Lastly, nanobiocomposites (NBCs; NBC1 and NBC2) were fabricated using QUCS as a scaffold to encapsulate either TEO or TH, with the mediation of Tween 80. By encapsulating these bioactive materials, we aim to enhance their efficacy and targeted delivery, bioavailability, stability, and anti-COVID properties. The new NBCs were structurally, morphologically, and physically characterized. Incorporating TEO or TH into QUCS significantly increased ZP values to ±53.1 mV for NBC1 and ±48.2 mV for NBC2, indicating superior colloidal stability. Interestingly, Tween 80-QUCS provided outstanding packing and release performance, with entrapment efficiency (EE) and loading capacity (LC) values of 98.2% and 3.7% for NBC1 and 83.7% and 1.9% for NBC2. The findings of in vitro antiviral studies not only highlight the potential of these nanobiocomposites as potential candidates for anti-COVID therapies but also underscore their selectivity in targeting SARS-CoV-2.

Examining the quaternary ammonium chitosan Schiff base-ZnO nanocomposite's potential as protective therapy for rats' cisplatin-induced hepatotoxicity.

BACKGROUND: Despite cisplatin's long history as a cornerstone in cancer therapy, both acquired chemoresistance and significant impacts on healthy tissues limit its use. Hepatotoxicity is one of its side effects. Adjunct therapies have shown promise in not only attenuating liver damage caused by cisplatin but also in enhancing the efficacy of chemotherapy. In this context, a new quaternary ammonium chitosan Schiff base (QACSB) was synthesized and applied as an encapsulating agent for the in-situ synthesis of QACSB-ZnO nanocomposite. MATERIAL AND METHODS: Thirty male albino rats were classified into Group 1 (control) distilled water, Group 2 (Cisplatin-treated) (12 mg/kg, i.p), and Group 3 (QACSB-ZnO NCs/cisplatin-treated) (150 mg/kg/day QACSB-ZnO NCs, i.p) for 14 days + a single dose of cisplatin. Liver functions, tissue TNF-α, MDA, and GSH were measured as well as histopathological and immunohistochemical studies were performed. RESULTS: The QACSB-ZnO NCs significantly restore liver functions, tissue TNF-α, MDA, and GSH levels (p < 0.001). Histopathological examination showed patchy necrosis in the cisplatin-treated group versus other groups. The QACSB-ZnO NCs showed a weak TGF-ß1 (score = 4) and a moderate Bcl-2 immunohistochemistry expression (score = 6) versus the CP group. CONCLUSIONS: QACSB-ZnO NCs have been shown to protect the liver from cisplatin-induced hepatotoxicity.

Exploring the chondroitin sulfate nanogel's potential in combating nephrotoxicity induced by cisplatin and doxorubicin-An in-vivo study on rats.

In this study, we aim to unveil the potential of itaconyl chondroitin sulfate nanogel (ICSNG) in tackling chronic kidney diseases triggered by the administration of CDDP and doxorubicin (Adriamycin, ADR). To that end, the new drug delivery system (ICSNG) was initially prepared, characterized, and loaded with the target drugs. Thereafter, the in-vivo studies were performed using five equally divided groups of 100 male Sprague-Dawley (SD) rats. Biochemical evaluation and immunohistochemistry studies have revealed the renal toxicity and the ameliorative effects of ICSNG on renal function. When ICSNG-based treatments were contrasted with the CDDP and ADR infected groups, they significantly increased paraoxonase-1 (PON-1), superoxide dismutase (SOD), catalase (CAT) and albumin activity and significantly decreased nitric oxide (NO), tumor necrosis factor alpha (TNF-α), creatinine, urea, and cyclooxygenase-2 (COX-2) activity (p < 0.001). The findings of the current study imply that ICSNG may be able to lessen renal inflammation and damage in chronic kidney disorders brought on by the administration of CDDP and ADR. Interestingly, according to the estimated selectivity indices, the ICSNG-encapsulated drugs have demonstrated superior selectivity for cancer MCF-7 cells, over healthy HSF cells, in comparison to the bare drugs.

Chemotherapeutic Activity of Imidazolium-Supported Pd(II) o-Vanillylidene Diaminocyclohexane Complexes Immobilized in Nanolipid as Inhibitors for HER2/neu and FGFR2/FGF2 Axis Overexpression in Breast Cancer Cells.

Two bis-(imidazolium-vanillylidene)-(R,R)-diaminocyclohexane ligands (H2(VAN)2dach, H2L1,2) and their Pd(II) complexes (PdL1 and PdL2) were successfully synthesized and structurally characterized using microanalytical and spectral methods. Subsequently, to target the development of new effective and safe anti-breast cancer chemotherapeutic agents, these complexes were encapsulated by lipid nanoparticles (LNPs) to formulate (PdL1LNP and PdL2LNP), which are physicochemically and morphologically characterized. PdL1LNP and PdL2LNP significantly cause DNA fragmentation in MCF-7 cells, while trastuzumab has a 10% damaging activity. Additionally, the encapsulated Pd1,2LNPs complexes activated the apoptotic mechanisms through the upregulated P53 with p < 0.001 and p < 0.05, respectively. The apoptotic activity may be triggered through the activity mechanism of the Pd1,2LNPs in the inhibitory actions against the FGFR2/FGF2 axis on the gene level with p < 0.001 and the Her2/neu with p < 0.05 and p < 0.01. All these aspects have triggered the activity of the PdL1LNP and PdL2LNP to downregulate TGFß1 by p < 0.01 for both complexes. In conclusion, LNP-encapsulated Pd(II) complexes can be employed as anti-cancer drugs with additional benefits in regulating the signal mechanisms of the apoptotic mechanisms among breast cancer cells with chemotherapeutic-safe actions.

Alginate-chitosan-microencapsulated tyrosols/oleuropein-rich olive mill waste extract for lipopolysaccharide-induced skin fibroblast inflammation treatment.

The Ca2+ ion-driven emulsification-ionotropic gelation method produced chitosan-alginate microspheres (CAMSs) with a narrow particle size distribution (PSD). Particle size distribution and zeta potential studies, as well as spectral electron microscopy, were used to assess the microspheres' physicochemical properties and morphology. The tyrosols (hydroxytyrosol (HT), tyrosol (TY), and oleuropein (OE) were loaded into these microspheres using a polyphenol extract (PPE) from Koroneki olive mill waste (KOMW). The microencapsulation efficiency and loading capacity of microspheres for PPE were 98.8% and 3.9%, respectively. Three simulated fluids, including gastric (pH = 1.2), intestinal (pH = 6.8), and colonic (pH = 7.4), were used to examine how the pH of the releasing medium affected the ability of CAMSs to release bioactive phenols. At a severely acidic pH (1.2, SGF), PPE release is nearly halted, while at pH 6.8 (SCF), release is at its maximum. Additionally, the PPE-CAMPs have ameliorated the endogenous antioxidant content SOD, GST, GPx with significant values from 0.05 to 0.01 in the treated LPS/human skin fibroblast cells. The anti-inflammatory response was appeared through their attenuations activity for the released cytokines TNF-α, IL6, IL1ß, and IL 12 with levels significantly from 0.01 to 0.001. Microencapsulation of PPE by CAMPs significantly improved its antioxidant and anti-inflammatory capabilities.

Comparison of the ameliorative roles of crab chitosan nanoparticles and mesenchymal stem cells against cisplatin-triggered nephrotoxicity.

AIM: In the present investigation, we compared the effects of mesenchymal stem cells extracted from bone marrow (BMSCs) and crab chitosan nanoparticles (CCNPs) on renal fibrosis in cisplatin (CDDP)-induced kidney injury rats. MATERIAL AND METHODS: 90 male Sprague-Dawley (SD) rats were divided into two equal groups and alienated. Group I was set into three subgroups: the control subgroup, the CDDP-infected subgroup (acute kidney injury), and the CCNPs-treated subgroup. Group II was also divided into three subgroups: the control subgroup, the CDDP-infected subgroup (chronic kidney disease), and the BMSCs-treated subgroup. Through biochemical analysis and immunohistochemical research, the protective effects of CCNPs and BMSCs on renal function have been identified. RESULTS: CCNPs and BMSC treatment resulted in a substantial rise in GSH and albumin and a decrease in KIM-1, MDA, creatinine, urea, and caspase-3 when compared to the infected groups (p < 0.05). CONCLUSION: According to the current research, chitosan nanoparticles and BMSCs may be able to reduce renal fibrosis in acute and chronic kidney diseases caused by CDDP administration, with more improvement of kidney damage resembling normal cells after CCNPs administration.

Therapeutic potential and protection enhancement of mesenchymal stem cell against cisplatin-induced nephrotoxicity using hyaluronic acid-chitosan nanoparticles as an adjuvant.

A newly synthesized nanoplatform of hyaluronic acid and chitosan nanoparticles (HA/CNPs) was applied to improve the therapeutic efficacy and protection of bone marrow mesenchymal stem cells (BM-MSCs) against cisplatin (CDDP)-induced nephrotoxicity in rats. CDDP administration causes significant increases in levels of serum creatinine (SCr), urea, and KIM-1 coupled with significant albumin level falls, as indicative of acute renal dysfunction. Moreover, the level of the antioxidant enzyme (GSH) was significantly decreased, while the levels of lipid peroxidation (MDA) and inflammatory (IL-6) and apoptotic (caspase-3) markers were significantly increased, indicating a decline in the kidney's antioxidant defense and increased inflammation. In contrast, when rats were pre-treated with either MSCs or MSCs-HA/CNPs before receiving CDDP, the levels of SCr, urea, KIM-1, MDA, IL-6, and caspase-3 were significantly decreased with simultaneous significant rises in GSH and albumin, impelling a great improvement in the antioxidant and anti-inflammatory defenses of the kidney as well as its functions. Intriguingly, MSCs-HA/CNPs were more effective against caspase-3 than MSCs alone, revealing the high anti-apoptotic capability of HA/CNPs. This finding suggests that HA/CNPs could effectively protect MSCs from oxidative stress and apoptosis and thus increase their stability and longevity.

Novel imidazolium-thiohydantoin hybrids and their Mn(iii) complexes for antimicrobial and anti-liver cancer applications.

We present the effective synthesis and structural characterization of three novel imidazolium-thiohydantoin ligands (IMTHs, 5a-c) and their Mn(iii) complexes (Mn(iii)IMTHs, 6a-c) in this study. The findings of elemental analyses, spectral analyses and magnetic measurements will be used to infer the stoichiometry, coordination styles, and geometrical aspects of Mn(iii)IMTHs. The new compounds were evaluated for their chemotherapeutic potential against ESKAPE pathogens and liver cancer (HepG2). According to the MIC and MBC values, the bactericidal and bacteriostatic activities of IMTHs have been significantly improved following coordination with the Mn(iii) ion. The MTT assay results showed that all Mn(iii)IMTHs had the potential to reduce the viability of liver carcinoma (HepG2) cells in a dose-dependent manner, with the BF4-supported complex (6b) outperforming its counterparts (6a and 6c) as well as a clinical anticancer drug (VBL). Additionally, Mn-IMTH2 (6b) showed the highest level of selectivity (SI = 32.05) for targeting malignant cells (HepG2) over healthy cells (HL7702).

The diminution and modulation role of water-soluble gallic acid-carboxymethyl chitosan conjugates against the induced nephrotoxicity with cisplatin.

The toxicity of cisplatin (CDDP) toward the renal tubules and its severe effects on the proximal tubules limits its further use in cancer therapy. The current study was undertaken to evaluate the protective effects of gallic acid-grafted O-carboxymethyl chitosan (GA@CMCS) against nephrotoxicity induced by CDDP in rats. Renal injury was assessed in the GA@CMCS/CDDP-treated rats using kidney injury molecule-1 (KIM-1). Moreover, the levels of reduced glutathione (GSH), malondialdehyde (MDA), and nitric oxide (NO) were measured. The comet assay was performed to measure the DNA damage. The renoprotective activity of GA@CMCS was supported by histo- and immuno-pathological studies of the kidney. GA@CMCS significantly normalized the increases in kidney homogenate of KIM-1, MDA, and NO-induced by CDDP and significantly increased GSH as compared with the CDDP group. GA@CMCS also significantly protects rat kidneys from CDDP-induced histo- and immuno-pathological changes. Both biochemical findings and histo- and immuno-pathological evidence showed the renoprotective potential of GA@CMCS against CDDP-induced oxidative stress, inflammation, and renal dysfunction in rats. In conclusion, GA@CMCS has been shown to mitigate the nephrotoxicity impact of CDDP in cancer therapy.

Cellulosic fabrics modified with polyphosphonium chitosan hydrazone-TiO2-Ag nanobiocomposites for multifunctional applications.

Bionanocomposites (BNC1,2) of binary (PPCH-Ag) and ternary (PPCH-TiO2-Ag) (PPCH = polyphosphonium chitosan-hydrazone) have been synthesized and immobilized on cellulosic fabrics (CFs) using an environmentally friendly single-step in situ methodology. The results of FTIR, TGA, EDX, SEM, and TEM investigations showed that PPCH and its BNCs were successfully formed on the surface layer of fabrics. Moreover, the BNC2-coated cloth exhibited a superhydrophobic behavior as revealed from the values of water contact angle (WCA) 152.1° and slide angle (SA) 8.7°. The cytotoxicity experiments on epithelial cells confirmed the safety of treated fabrics for human cells. The antimicrobial capabilities of the BNCs-treated textiles were greatly enhanced, with a small preference for BNC1-coated fabric, as compared to the native or other treated fabrics. In contrast, the BNC2-coated fabric demonstrated the highest anti-UV protection capabilities as indicated by its great capacity to reduce the UV transmission (UV-A, 2.1 %; UV-B, 1.8 %) as well as its UPF value (49.2). The durability tests revealed the high resistance of BNC2-CF against harsh washing conditions and their acquired functions sustainability up to 20 washing cycles.

Quaternized Chitosan Thiol Hydrogel-Thickened Nanoemulsion: A Multifunctional Platform for Upgrading the Topical Applications of Virgin Olive Oil.

(1) Background: Virgin olive oil (VOO) has attracted the attention of many researchers due to its nutritional and medicinal values. However, VOO's biological applications have been limited due to a lack of precise chemical profiling and approach to increase the physicochemical characteristics, bioactivity, and delivery of its bioactive components; (2) Methods: The current study intended to evaluate the chemical composition of VOO using the GC-MS technique and determine its major components. Furthermore, the effect of incorporating VOO into Tween 80-lecithin nanoemulsion (OONE) and a quaternized trimethyl chitosan-thiol (TMCT) hydrogel-thickened nanoemulsion system (OOHTN) on its physicochemical characteristics and biological potentials will be investigated; (3) Results: The VOO-based NEs' physicochemical properties (particle size and zeta potential) were steady during storage for four weeks owing to the inclusion of the protective TMCT hydrogel network to OONE. Excessive fine-tuning of olive oil nanoemulsion (OONE) and the TMCT protective network's persistent positive charge have contributed to the oil's improved antimicrobial, anti-biofilm, and antioxidant potentials; (4) Conclusions: The Tween 80-lecithin-TMCT nanosystem might provide a unique and multifunctional nanoplatform for efficient topical therapy as well as the transdermal delivery of lipophilic bioactive compounds.

Upgrading the Transdermal Biomedical Capabilities of Thyme Essential Oil Nanoemulsions Using Amphiphilic Oligochitosan Vehicles.

(1) Background: Thymus vulgaris L. (thyme) essential oil (TEO) has gained much attention because of its long history of medicinal usage. However, the lack of precise chemical profiling of the TEO and methods to optimize the bioactivity and delivery of its constituents has hampered its research on quality control and biological function; (2) Methods: The current study aimed to analyze the TEO's chemical composition using the GC-MS method and identify its key components. Another objective of this work is to study the impact of the protective layer of amphiphilic oligochitosan (AOC) on the physicochemical stability and transdermal potentials of TEO multilayer nanoemulsions formulated by the incorporation of TEO, Tween80, lecithin (Lec), and AOC; (3) Results: The AOC protective layer significantly improved the stability of TEO-based NEs as revealed by the constancy of their physicochemical properties (particle size and zeta potential) during storage for a week. Excessive fine-tuning of thyme extract NEs and the AOC protective layer's persistent positive charge have been contributed to the thyme extract's improved anti-inflammatory, transdermal, and anti-melanoma potentials; (4) Conclusions: the AOC-coated NEs could offer novel multifunctional nanoplatforms for effective transdermal delivery of lipophilic bioactive materials.

Phenylboronic Acid-Grafted Chitosan Nanocapsules for Effective Delivery and Controllable Release of Natural Antioxidants: Olive Oil and Hydroxytyrosol.

Olives and virgin olive oil (VOO) are a staple of Mediterranean diets and are rich in several beneficial phenolic compounds, including hydroxytyrosol (HT). Therefore, VOO was extracted from Koroneiki olive fruits, and its volatile as well as phenolic components were identified. Meanwhile, in order to upgrade the pharmaceutical capabilities of VOO and HT, a new conjugate phenylboronic acid-chitosan nanoparticles (PBA-CSNPs, NF-1) was fabricated and applied as nanocapsules for implanting high loading and efficient delivery of VOO and HT nanoformulations (NF-2 and NF-3). Due to the H-bonding interactions and boronate ester formation between the hydroxyl groups of the phenolic content of VOO or HT and the PBA groups in the nanocapsules (NF-1), VOO and HT were successfully loaded into the PBA-CSNPs nanocapsules with high loading contents and encapsulation efficacies. The NF-2 and NF-3 nanoformulations demonstrated physicochemical stability, as revealed by their respective zeta potential values, and pH-triggered drug release characteristics. The in vitro studies demonstrated that the nascent nanocapsules were almost completely nontoxic to both healthy and cancer cells, whereas VOO-loaded (NF-2) and HT-loaded nanocapsules (NF-3) showed efficient anti-breast cancer efficiencies. In addition, the antimicrobial and antioxidant potentials of VOO and HT were significantly improved after nanoencapsulation.

Chemotherapeutic and chemopreventive potentials of ρ-coumaric acid - Squid chitosan nanogel loaded with Syzygium aromaticum essential oil.

One of the most important trends in chemotherapy is the development of green chemotropic drugs with maximal activity and minimal side effects. The nanoencapsulation of phytochemical oils with natural polymers has been documented as a promising approach to producing nanodrugs with sustainable bioactivity and prolonged stability. In this context, Syzygium aromaticum essential oil (SAEO) and ultrasound-assisted deacetylated chitosan (UCS3) were successfully extracted from clove buds and squid pens, respectively. Grafting of UCS3 by ρ-coumaric acid (ρCA) has been performed to fabricate the ρCACS nanogel which was used for nanoencapsulation of SAEO to yield SAEO-loaded nanogel (ρCACS@SAEO). The findings of spectral, thermal, and morphological analyses have confirmed the success of the formation of new materials and SAEO encapsulation, as well. Based on the findings of the in vitro antimicrobial, antioxidant, and anticancer studies, the nanoencapsulation of SAEO by ρCACS has significantly boosted its chemotherapeutic effects, compared to unencapsulated oil. Therefore, ρCACS@SAEO nanogel could be considered as a multifunctional chemotherapeutic/chemopreventive agent for prevention or therapy of pathologies induced by oxidative stress, microbial infection, and breast and skin cancer.

Co-delivery of imidazolium Zn(II)salen and Origanum Syriacum essential oil by shrimp chitosan nanoparticles for antimicrobial applications.

This study reports preparation and physicochemical characterization of natural antimicrobials (Origanum Syriacum essential oil (OSEO), shrimp chitosan nanoparticles (CSNPs)) and new imidazolium ionic liquid-supported Zn(II)Salen. These antimicrobials were separately or co-encapsulated by CSNPs to fabricate novel antimicrobial nanoplatforms "NPFs" (OSEO-loaded CSNPs (NPF-1), Zn(II)Salen-loaded CSNPs (NPF-2), and Zn(II)Salen@OSEO-loaded CSNPs (NPF-3)). The finding of loading, encapsulation, and antimicrobial release studies confirm the suitability of CSNPs for nanoencapsulation of Zn(II)Salen and OSEO. All NPFs can significantly suppress the growth of microbial species with performances dependent upon the microbial strain and nanoplatform concentration. The susceptibility of microbes toward new antimicrobials was as follows; Gram-positive bacteria > Gram-negative bacteria > fungi. The amazing physicochemical features of new nanoplatforms and their bioactive ingredients (Zn(II)Salen, OSEO, and CSNPs) signify the importance of our designs for developing a new generation of nanopharmaceuticals supported both natural products and biogenic ionic metal cofactors, targeting the multidrug resistant (MDR) pathogens.

Fine-tuning of the pharmacological potential of novel thiazolium ionic liquids by anion alteration.

A novel series of thiazolium ionic liquids (TILs) bound to chloride (2a-c), tetrafluoroborate (BF4) (3a-c), and bis-(trifluoromethanesulfonimide) (Tf2N) anions (4a-c) was synthesized and their physicochemical characteristics were investigated using various microanalytical techniques. The pharmacological potential of the new TILs was assessed as chemotherapeutic agents for bacterial infections and ovarian cancer (SKOV-3). Notably, ILs with the same cations become more bactericidal upon their binding with the strongest chaotropic anion (TN2f). The in vitro toxicity of the TILs toward ovarian carcinoma cell lines (SKOV-3) and normal human skin fibroblast cells (HSF) revealed that all tested TILs have the capacity to induce a dose- and time-dependent decline in SKOV-3 cell viability, with Tf2N-linked TILs (4a-c) having a preferable efficacy. In addition, the new compounds showed excellent selectivity for cancer cells (SKOV-3) over healthy cells (HSF). [iPBzTh][Tf2N] (4b) is the most cytotoxic and specific one and may act as a promising anti-ovarian cancer agent.

Suppressing of milk-borne pathogenic using new water-soluble chitosan-azidopropanoic acid conjugate: Targeting milk-preservation quality improvement.

Dairy animals are major reservoirs for many milk-borne pathogens (MBPs) such as Staphylococcus aureus (S. aureus) and Escherichia coli (E. coli O157:H7). Thus, dairy industries dedicate most of their processes to eliminate or minimize microbial contamination. Although pasteurization may offer an ideal solution for microbial decontamination; nevertheless, it may negatively impact organoleptic and nutritive values of dairy products. In this context, this work aimed to develop an innovative strategy, to tackle this challenge, based on the chemical preservation of milk. In this endeavor, we have succeeded to design a new safe multifunctional bio-preservative based on natural antimicrobials (water-soluble chitosan (WSC) and 2-azidopropanoic acid (APA), (WSC-APA) conjugate). Interestingly, the minimum inhibitory concentrations (MICs) of WSC-APA have the capacity to completely suppress the proliferation of E. coli O157:H7 and S. aureus cells (100% bacterial reduction) in refrigerated milk samples during 20 and 24 h, respectively. Moreover, no Staphylococci species could be detected in refrigerated milk samples remediated with WSC-APA (0.25 mg/mL) after 6 storage days. Meanwhile, the coliform count has reduced by 99.7% in conjugate-treated milk samples during 10 storage days. Thus, new bio-preservative (WSA-APA) can be safely used to increase the shelf-life of milk without sacrificing its organoleptic and nutritive values.