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In this study, we explored the eco‐friendly synthesis of photoluminescent CCDs employing a direct one‐step pyrolysis process, utilizing natural Cortex Phellodendri Chinensis as the precursor material and studied their analgesic effect in mice. The synthesized carbon dots underwent comprehensive characterization through a range of spectroscopic and microscopic techniques. These included UV‐Vis, FTIR, fluorescence spectroscopy and HR‐TEM, DLS instruments. HR‐TEM results exhibited the presence of homogenous spherical‐shaped C‐dots of about 3.3 nm without aggregates. Furthermore, the prepared CCDs were studied for their in vivo analgesic effect in mice by performing tail‐immersion, hot plate and acetic acid writhing tests. Also, an MTT assay was performed to assess the in vitro cytotoxicity of CCDs against L929 cells. In vitro cytotoxicity studies revealed that L929 cells exhibited higher cell viability when treated with prepared CCDs. The cellular uptake studies revealed the phase contrast images of MG‐63 cells at wavelength 488 nm clearly depicted the aggregation of green, fluorescent CCDs within the cells while leaving nuclei unobscured. In addition, to the best of our understanding, the results presented in this paper showed that CCDs exhibited an important analgesic effect and enhanced anti‐nociceptive activity, which may be due to stimulation of the opioidergic system. Consequently, CCDs appear to be a viable analgesic alternative for traditional analgesic candidates in pain management. [ABSTRACT FROM AUTHOR]

Multiple myeloma (MM) cells express certain tumour-associated antigens (TAAs) that could serve as targets for active-specific immunotherapy. The aim of the present study was to test the MM/dendritic cell (DC) fusion as a vaccination strategy. We fused MM cells with DC to generate fusion cells (FCs) and tested their antigen presenting cell (APC) function in mixed lymphocyte reactions and cytotoxicity assays. First, the HS Sultan and SK0-007 HAT sensitive human MM cell lines and DCs generated from peripheral blood of normal donors were fused in the presence of 50% polyethylene glycol to form FCs. Next, tumour cells freshly isolated from patients were similarly fused with autologous DCs to generate FCs. The FCs demonstrated a biphenotypic profile, confirmed both by flow-cytometry and dual immunofluorescence microscopy. These FCs induced MM-specific cytotoxicity. FCs, but not MM cells or DCs alone, were potent stimulators of autologous patient T cells. More importantly, FC-primed autologous peripheral blood mononuclear cells demonstrated major histocompatibility complex-restricted MM-specific cytolysis. These studies therefore demonstrated that MM/DC FC can trigger an autologous immune response to MM cells and formed the framework for a clinical trial currently underway. [ABSTRACT FROM AUTHOR]

This research paper explores the field of nanobiotechnology, focusing on the design, characterisation, and potential dermal applications of metal oxide nanoparticles (MONPs). ZnO and FeO NPs exhibit distinctive properties that are valuable in dermato‐cosmetic applications and transdermal drug delivery. This study investigates Cannabidiol (CBD) as a capping agent for MONPs synthesis. Employing microwave‐assisted techniques, MONPs were synthesised using either CBD or polyvinylpyrrolidone (PVP) as capping agents. The TEM, SEM, FTIR, and XRD characterisation results confirmed the successful formation of CBD‐capped ZnO and FeO NPs exhibiting an average particle size of 90 and 76 nm, respectively. The cytotoxicity of CBD‐capped MONPs was evaluated on HaCaT cells over a concentration range of 100 to 6.25 μg/mL, which revealed that CBD‐capped ZnO NPs exerted a cytotoxic effect on HaCaT cells (IC50 85.34±1.17 μg/mL). In contrast, CBD‐capped FeO NPs and PVP‐capped MONPs exhibited negligible cytotoxicity (IC50 >100 μg/mL). TEM analysis revealed a noticeable structural alteration of ZnO NPs in the supplemented cell culture medium, which could contribute to enhanced NP uptake, thereby explaining the more pronounced cytotoxic effect of ZnO NPs. Therefore, the disparity in cytotoxic responses can be attributed to the protein coating adhering to the NPs surface in a biological medium. [ABSTRACT FROM AUTHOR]

In this paper, we have synthesized water‐soluble peripherally tetra and octa‐({6‐[3‐(dimethylamino)phenoxy]hexyl}oxy) groups substituted zinc (II) phthalocyanines (DM‐C6‐ZnQ and o‐DM‐C6‐ZnQ). Also, we have investigated ct‐DNA binding, supercoiled plasmid DNA cleavage properties of DM‐C6‐ZnQ and o‐DM‐C6‐ZnQ by using spectrophotometric and electrophoretic methods. On the other hand, cytotoxic and phototoxic effects of DM‐C6‐ZnQ and o‐DM‐C6‐ZnQ were examined using (3‐(4,5‐dimethylthiazol‐2‐yl)‐2,5‐diphenyltetrazolium bromide (MTT) assay on human lung adenocarcinoma (A549) cell lines. In UV–Vis absorption studies, hypochromism was observed about 18% for DM‐C6‐ZnQ and 57% for o‐DM‐C6‐ZnQ on addition of increasing concentrations of ct‐DNA. The intrinsic binding constant (Kb) values of DM‐C6‐ZnQ and o‐DM‐C6‐ZnQ were 3.82 (±0.14) × 104 M−1 and 2.34 (±0.05) × 105 M−1, respectively. The supercoiled plasmid DNA cleavage studies showed that DM‐C6‐ZnQ and o‐DM‐C6‐ZnQ had no DNA damage actions in the dark. On the other hand, they caused DNA damage depending on the light dose. In the MTT assay, the compounds had low cytotoxic properties on A549 cell lines, but they showed significant phototoxic actions. These results reveal that the compounds interact with DNA and have phototoxic properties; it has been determined that they have the potential to be photosensitizing agents for photodynamic therapy. [ABSTRACT FROM AUTHOR]

There are marine cytotoxic bromotriterpenoids, named the thyrsiferol family that are structurally characterized by some tetrahydropyran (THP) and tetrahydrofuran (THF) rings. The thyrsiferol family belongs to natural products that are often difficult to determine their stereostructures even by the current, highly advanced spectroscopic methods, especially in acyclic systems including stereogenic tetrasubstituted carbon centers. In such cases, it is effective to predict and synthesize the possible stereostructures. Herein, to elucidate ambiguous stereostructures and unassigned absolute configurations of aplysiol B, laurenmariannol, and saiyacenol A, members of the thyrsiferol family, we carried out their asymmetric chemical syntheses featuring 6‐exo and 5‐exo oxacyclizations of epoxy alcohol precursors and 6‐endo bromoetherification of a bishomoallylic alcohol. In this paper, we report total assignments of their stereostructures through their asymmetric chemical syntheses and also their preliminary cytotoxic activities against some tumor cells. These results could not have been achieved without depending on asymmetric total synthesis. [ABSTRACT FROM AUTHOR]

Sugar based cationic lipids are promising carriers of nucleic acids into various cells. Particularly, abundant hydroxyl functional groups in the sugar‐like moieties are believed to enhance target oriented uptake as well as biocompatibility. Towards this direction, we have synthesized three new cationic lipid analogues with or without sugar‐like multi‐hydroxyl functional head groups. Liposomal formulations of these lipids were developed and thoroughly characterized by means of DNA binding ability, size and zeta potential. Optimal lipid‐DNA complexes were determined by their transfection efficiency in HEK‐293 (Human embryonic kidney) cells. 1,4 gluconic γ‐lactone derived lipid (TS1) and ascorbic acid derived lipid (TS2), have exhibited 25‐fold and 12‐fold increase in transfected HEPG2 (human liver cancer) cells, respectively, when compared with a control lipid without sugar‐like moiety (TA). However, this property was reversed in the case of U87 (human primary glioblastoma) cell line. The results point out that the transfection efficiencies of sugar alcohol‐based cationic lipids are cell‐dependant. Cytotoxicity of the lipid complexes revealed that the sugar‐mimicking cationic lipids are non‐toxic as ≈80 % viable cells were observed in the treated cell lines. In conclusion, the current paper adds knowledge on the sugar based cationic lipids and reiterates that these lipids could yield potential applications towards liver targeted gene delivery. [ABSTRACT FROM AUTHOR]

In this paper, a series of betulonic acid N‐methylpiperazinyl amide derivatives, especially holding C2‐nicotinoylidene/furfurylidene/fluorobenzylidene fragments, have been synthesized and evaluated for their cytotoxic activity against the NCI‐60 cancer cell line panel. N‐Methylpiperazinyl amide of betulinic acid 11 (GI50=0.49 μM for leukemia CCRF‐CEM cell line), 2‐(4‐pyridinoylidene)‐betulinic 9 and betulonic 14 acids (GI50=1.60 and 1.36 μM for colon cancer HCT‐116 cell line, respectively), as well as 2‐(furfurylidene)‐betulonic acid 16 (GI50=1.66 μM for melanoma LOX IMVI cell line) were found to be the lead compounds. The activity displayed for these compounds was higher than for the standard drug doxorubicin against colon cancer HCT‐15 and ovarian cancer NCI/ADR‐RES cell lines. Cell cycle analysis indicates that compound 11 promotes cytotoxic activity through the apoptosis induction both in conditionally normal (HEK293) and in cancer (A549, MCF‐7) cells, whereas compound 14 exhibits both cytostatic and cytotoxic activity, dependently on cell line evaluated. In particular, in HEK293 cells the compound 14 induces mainly apoptotic cell death, while in A549 and MCF‐7 cells cytostatic effect is dependent on cell cycle arrest in the G2/M phase. Compounds 11 and 14 are promising molecules for future antitumor drug development. [ABSTRACT FROM AUTHOR]

The paper presents results of the studies on porous composites obtained using lyophilization method based on the solutions of the following polymers: chitosan, sodium alginate and polylactide, as well as ZnO‐doped CaO–SiO2–P2O5 bioglass. The researchers took the advantage of zinc ions demonstrating the bactericidal, immune‐stimulating, and tissue‐regenerating functions in the organism. The cytotoxicity of the composites was tested on L929 cells by means of the direct and the indirect contact method. The antibacterial properties were determined against the gram‐negative bacteria Pseudomonas aeruginosa and the gram‐positive bacteria Staphylococcus aureus at 24, 48 hours, and 7 days. The study demonstrated that changes due to cytotoxicity effect of the composites depend on the type of polymer and on the duration of contact with cells. The composite with polylactide was found to be the least toxic for L929 cells. ZnO added to the chemical composition of bioglass ensured bactericidal effects. The antibacterial properties of the composites depended on the ZnO content, bioglass grain size, polymer type, and composite microstructure. The composites presented in this paper are innovative as biomaterials for filling bone cavities because they can be a matrix for cells and have an antibacterial effect while supporting the regeneration of damaged tissue. [ABSTRACT FROM AUTHOR]

In this paper, the boron‐containing mesoporous bioactive glass (MBG) nanospheres have been successfully synthesized by modified sol‐gel method assisted by surfactant, and the effect of boron substitution on structure and bioactivity was evaluated by combining experiments and ab initio molecular dynamics (AIMD) simulations. All of the samples exhibit regularly uniform mesoporous spherical microstructure with an average size of about 60 nm, and the boron‐containing MBGs show higher specific surface area with the value up to 416.20 m2/g. The simulated body fluid (SBF) immersion test confirms that the deposited hydroxyapatite (HA) evidently increases with the increasing of boron content, indicating that the biological behavior has been significantly improved resulting from incorporation of boron. Additionally, our results also reveal that B2O3 substitution has positive impact on cell proliferation of human periodontal ligament cells (hPDLCs) at lower extracted concentration. Furthermore, AIMD simulation is employed to understand the relationship between structural changes and in vitro bioactivity in terms of structural information, especially the boron coordination number. The results illustrate that the boron‐containing MBG nanospheres with excellent bioactivity are great potential for biomedical applications. [ABSTRACT FROM AUTHOR]

In this paper, we present systematic studies concerning the synthesis protocol, functionalisation process, characterisation and cytotoxic effects of thioglucose‐modified gold nanoparticles (TG‐AuNPs). The characterisation of AuNPs and TG‐AuNPs was performed using: scanning transmission electron microscopy (STEM), Dynamic Light Scattering (DLS) and Ultraviolet‐visible spectroscopy (UV‐vis). The modification of AuNPs with TG was confirmed by Fourier‐Transform Infrared Spectroscopy (FT‐IR) and the surface coverage was determined with High‐Performance Liquid Chromatography (HPLC). Prepared bio‐conjugates with increasing and controlled amounts of TG on AuNPS were then biologically investigated: the cell viability using the MTT assay; the uptake of AuNPs in cell culture by Inductively Coupled Plasma Optical Emission Spectroscopy (ICP‐OES); the incorporation of AuNPs in cell structures by confocal microscopy. The obtained results suggest that bio‐conjugates disclose both good biocompatibility and low cytotoxicity, and further‐can target the cancer cells and may constitute promising potential nanocarriers of anticancer drugs. [ABSTRACT FROM AUTHOR]

The present paper describes the synthesis, anti‐plasmodial, and cytotoxic evaluation of 7‐chloroquinoline‐based conjugates with isatins/indoles/ nitroimidazoles, obtained via Cu‐promoted 1,3‐dipolar cycloadditions. On contemplating SAR of the synthesized series, the inclusion of indole and nitroimidazole‐core improved the anti‐plasmodial activities while the isatin seemed to have a lesser effect. The conjugate with a nitroimidazole‐core and hexyl chain length as a spacer between the two pharmacophores was found to be most potent among the synthesized series and displayed an IC50 of 0.12 µM and a selectivity index of 1748. [ABSTRACT FROM AUTHOR]

This study aimed to perform a systematic review and meta‐analysis of papers discussing the efficacy of microbial synthesised metallic nanoparticles (MNPs) against cancerous and normal cell lines by exploiting Bayesian generalised linear (BGL) model. Data was systematically collected from published papers via Cochrane library, Web of Science, PubMed, Science Direct, ProQuest, Scopus, and Embase. Impressively, most of the studies were carried out on HeLa and A549 cancer cell lines. Specifically, a hefty 65.67% of studies employed bacteria to biofabricate MNPs. Significantly, BGL meta‐analysis represented highly valuable information. Hence, based on adjusted analysis, the MNPs with the size of 25–50 nm were found to be far less cytotoxic than the MNPs with the size of ≤25 nm (OR = 0.233, P ˂ 0.05) against either cancerous or normal cell lines. Interestingly, it was found that the odds of cytotoxicity in cancerous cell lines were practically nine times more than normal cell lines, representing the substantially more cytotoxicity of MNPs in cancerous cell lines (OR = 9.004, P ˂ 0.001). Green MNPs mentioned here may be developed as novel anti‐cancer agents, which could lead to a revolution in the treatment of cancer. [ABSTRACT FROM AUTHOR]

Abstract: Curcumin, a natural compound extracted from the rhizomes of Curcuma longa, displays pronounced anticancer properties but lacks good bioavailability and stability. In a previous study, we initiated structure modification of the curcumin scaffold by imination of the labile β‐diketone moiety to produce novel β‐enaminone derivatives. These compounds showed promising properties for elaborate follow‐up studies. In this work, we focused on another class of nitrogen‐containing curcuminoids with a similar objective: to address the bioavailability and stability issues and to improve the biological activity of curcumin. This paper thus reports on the synthesis of new pyridine‐, indole‐, and pyrrole‐based curcumin analogues (aza‐aromatic curcuminoids) and discusses their water solubility, antioxidant activity, and antiproliferative properties. In addition, multivariate statistics, including hierarchical clustering analysis and principal component analysis, were performed on a broad set of nitrogen‐containing curcuminoids. Compared to their respective mother structures, that is, curcumin and bisdemethoxycurcumin, all compounds, and especially the pyridin‐3‐yl β‐enaminone analogues, showed better water solubility profiles. Interestingly, the pyridine‐, indole‐, and pyrrole‐based curcumin derivatives demonstrated improved biological effects in terms of mitochondrial activity impairment and protein content, in addition to comparable or decreased antioxidant properties. Overall, the biologically active N‐alkyl β‐enaminone aza‐aromatic curcuminoids were shown to offer a desirable balance between good solubility and significant bioactivity. [ABSTRACT FROM AUTHOR]

The aim of the present study was to investigate the biological activities of the ultrasound‐assisted extracts obtained from pulp and seed of jujube (Ziziphus jujuba) fruits. To reach this purpose, total phenolic content (TPC), total flavonoid content (TFC), total pro‐anthocyanin, DPPH radical scavenging activity, rancimat test, as well as antimicrobial activity and cytotoxicity test of both jujube pulp and seed extracts were evaluated. Total phenolic content (TPC), total flavonoid content (TFC), and total pro‐anthocyanin in pulp extract were higher than those obtained from seed extract. In addition, DPPH radical scavenging activity of pulp extract (IC50 = 53.97 µg/ml) was higher than that of seed extract (IC50 = 88.68 µg/ml). Furthermore, the highest antimicrobial activity was observed against Escherichia coli and Staphylococcus aureus (MIC = 20 mg/ml) for both seed and pulp extracts. In vitro cytotoxicity evaluation on seven cell lines revealed that pulp and seed extracts of jujube had no cytotoxic activity. The present results suggested the promising antioxidant properties of jujube, which can be used in the fabrication of functional bioactive ingredients for different purposes. [ABSTRACT FROM AUTHOR]

Background and Aim: In the present paper, the toxicity of prolamines derived from three cereals with a different genome was investigated in human colon cancer Caco-2/TC7 and human myelogenous leukemia K562(S) cells. The purpose of this study was to investigate if species from ancient wheat could be considered as healthy food crops devoid or poor in cytotoxic prolamines for celiac disease. Methods: Cytotoxicity was measured in terms of inhibition of cell growth, activation of apoptosis, release of nitric oxide (NO), detection of tissue transglutaminase (TG II) and alteration of transepithelial electrical resistance (TEER) on Caco-2/Tc7 and K562 (S) cell agglutination. Peptic-tryptic (PT) digest from bread wheat ( T. aestivum S. Pastore) was used as a positive control. Results: PT digests of prolamins from spelt wheat ( T. aestivum ssp. spelta) were found to exert toxic effects on Caco-2/TC7 cells and to agglutinate K562(S) cells. Increased amounts of NO and TG II expression were observed in Caco-2/TC7 cells exposed to 1 mg/mL of spelt prolamins, suggesting that spelt wheat can induce cellular mechanisms implicated in the pathogenesis of celiac disease. By contrast, the PT digests from monoccum wheat ( Triticum monococcum) and farro wheat ( T. turgidum ssp. dicoccum) did not exhibit any negative effects on Caco-2/TC7 and K562(S) cells. Conclusions: The results have shown a constant and significant toxic effect of spelt wheat which is not shared by the two other ancient cereals. Future studies on celiac intestinal organ cultures are needed to increase the prospects of breeding programs aimed at developing wheat cultivars potentially tolerated by most celiac patients. [ABSTRACT FROM AUTHOR]

The immunogenetic enigma of maternal acceptance of the fetal semiallograft has been termed an immunological paradox. The first trimester decidua is heavily infiltrated with CD56brightCD16− uterine natural killer (uNK) cells which must be prepared to respond to potential pathogen challenges and still be able to control immune responses that allow the development of the fetus. The significant presence of cytolytic mediators, perforin and Fas/Fas ligand (FasL), at the maternal–fetal interface raises a question of their role(s) in the immunological interrelations between maternal tissues and trophoblast cells. As uNK cells in vitro lyse target cell lines (K562, P815 and P815Fas) using these effector molecules, it seems that, although immunocompetent, their cytotoxicity is not directed against trophoblast during normal pregnancy. Therefore, it is generally believed that the hormonal and Th1/Th2 cytokine balance plays an important role in the tolerance and maintenance of pregnancy. This paper gives an overview of the recent findings on the complex immunological events that occur at the maternal–fetal interface. [ABSTRACT FROM AUTHOR]

Cellulose nanocrystals (CNCs) are an environmentally friendly natural material, consisting of rod‐like crystalline nanoparticles, called whiskers, or nanocrystalline cellulose. The derivation of different natural sources, aligned to their biocompatibility, biodegradability, and versatility, make them a class of fascinating materials with widespread industrial use. In addition, the cellulose species possess intriguing physicochemical and mechanical properties. This paper provides an overview of recent progress in the area of cellulosic nanocomposites, along with details of their structure and liquid crystalline behavior as nematic and cholesteric lyotropic materials. Guidance is subsequently provided for the physicochemical analysis of these materials, including X‐ray diffraction, transmission electron microscopy, optical evaluation, thermogravimetric analysis, and differential scanning calorimetry. Additionally, the functional chemical and physical properties of CNCs are correlated to the resulting nanotoxicity in in vitro and in vivo assays. This review points to relevant concerns, such as sources for the synthesis of CNCs, the nanomaterial size, and the surface chemistry, that must be overcome in order to attain safe use of CNC‐based nanomaterials. The challenging perspectives on the ongoing research are presented in order to explore the technological and industrial perspectives on the use of CNC for the generation of cost‐effective advanced nanomaterials based on cellulosic fibers. [ABSTRACT FROM AUTHOR]

Fusicoccin, a phytotoxic diterpene glucoside, was converted to a series of antiproliferative agents for tumor cells by removing 12‐hydroxyl group semi‐synthetically. These compounds were shown to upregulate interaction of 14‐3‐3 and a phospholigand in a sequence‐specific manner. More information can be found in the Full Paper by J. Ohkanda et al. on page 16066. [ABSTRACT FROM AUTHOR]

Medicinal plants have been used for a long time for therapeutic benefit in treating or preventing diseases. Due to its geographical location, Thailand is endowed with a great biological diversity. These bioresources can provide an array of natural products for the development of new drugs. In their Full Paper on page   910   ff., Somsak Ruchirawat, Chulabhorn Mahidol et   al. report on the exceptional potency of cardinane sesquiterpenes isolated from Alangium salviifolium plants on aromatase inhibition. The data of the study suggest that these compounds might represent aromatase inhibitors for breast cancer and could be leads for further drug development. [ABSTRACT FROM AUTHOR]

A phenomenon of enantiodivergence was found in lepadiformine marine alkaloids isolated from a single species marine tunicate Clavelina moluccensis. The enantioselective total syntheses have been achieved by key mercury(II) triflate‐catalyzed cycloisomerization reaction from a functionalized linear substrate to a 1‐azaspiro[4.5]decane compound, and cytotoxic activities of synthesized lepadiformines and their synthetic intermediates were also evaluated. More information can be found in the Full Paper by Y. Morimoto et al. on page 9535. [ABSTRACT FROM AUTHOR]

Gold(I) complexes of ClickPhos [2.2]paracyclophane ligands were systematically studied with respect to their cytotoxic properties. Their efficiency in cytotoxicity was investigated in HeLa, MCF7 and HCT116 cells displaying different mechanisms of action, which involve apoptosis, necrosis, and DNA damage. The gold ‐ based cytostatics induce double ‐ strand DNA breaks (DSB) as shown by H2AX phosphorylation at foci of DSBs. More information can be found in the Full Paper by U. Schepers, P. W. Roesky et al. on page 6315 ff. [ABSTRACT FROM AUTHOR]

The cover picture shows the new metal–organic frameworks (MOFs) ZJU‐64 and ZJU‐64‐CH3, which exhibit low totoxicity, high stability, and temperature‐controlled drug‐release behaviors. The findings provide a strategy to enhance the therapeutic efficacy of these MOFs because of their capacity for combining drug and thermal therapies. More details can be found in the Full Paper by Guodong Qian and co‐workers on page 804 in Issue 8, 2016 (DOI: 10.1002/cplu.201600142). [ABSTRACT FROM AUTHOR]

DNA Condensation The condensation of DNA in a controlled manner is one of the key steps in gene delivery and gene therapy. As described in their Full Paper on page 1895   ff., Yu Liu and co ‐ workers designed and constructed a water ‐ soluble and nontoxic nanometer ‐ sized conjugate comprising gold nanoparticles, β ‐ cyclodextrins, and anthryl adamantanes (see the Inside Cover). This conjugate exhibits a good condensation ability toward DNA through the intercalation of the anthryl groups into the DNA double helix. Significantly, the condensation efficiency of the supramolecular nanostructure towards DNA could be conveniently controlled by adjusting the ratio between gold nanoparticles and anthryl adamantane grafts. [ABSTRACT FROM AUTHOR]