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... Accumulating clinical data shows that less than half of patients are beneficial from PD-1/PD-L1 blockage therapy owing to the limited infiltration of effector immune cells into the tumor and abundant of the immunosuppressive factors in the tumor microenvironment. In this study, PD-L1 inhibition therapy and BRAF-targeted therapy, which showed clinical benefit, were combined in a CXCR4-targeted nano ...
... A series of novel 14α-O-(1,4-disubstituted-1,2,3-triazolyl) ester derivatives of andrographolide (5a-n) were synthesized from andrographolide (1). For this endeavour, selective esterification at C-14 hydroxyl group of andrographolide (1) with propiolic acid via protection, deprotection strategy followed by 1,4-regioselective [1,3]dipolar cycloaddition of alkyne, azide using Cu(I) catalyzed Click c ...
... The influence of food components on nanoparticle (NP) internalization indicates a need to investigate the behaviors of NPs in a complex system. This study measured the changes of TiO₂ NP colloidal stability and quenching of anthocyanin fluorescence to indicate NP-anthocyanin interactions, and cytotoxicity, oxidative stress, expression of ABC transporters and intracellular Ti concentrations in 3D C ...
... The abnormal aggregation of human islet amyloid polypeptide (hIAPP) is a crucial pathogenic factor associated with type 2 diabetes (T2D). The development of effective inhibitors to prevent hIAPP aggregation is a common therapeutic strategy against T2D. Lithospermic acid (LA) is a natural compound with diversified biological activities. In this study, electrospray ionization coupled with ion mobili ...
K. Anand; R. Rajamanikandan; A. Selva Sharma; M. Ilanchelian; Faez Iqbal Khan; C. Tiloke; Naresh Kumar Katari; P. Boomi; C. Balakumar; M. Saravanan; S. Palanisamy; M. Ramesh; Dakun Lai; A.A. Chuturgoon
... Unique characteristics displayed by phytoconstituent conjugated nanoparticles and their crucial interactions with proteins serve to develop nanoparticle-bio-interface platform. Gold nanoparticles of 16 nm in size were generated using aqueous extracts of pine bark and further conjugated to human serum albumin. The gold nanoparticles-protein complex was characterized by surface plasmon resonance, UV ...
... In searching for drugs from natural product scaffolds has gained interest among researchers. In this study, a series of twelve halogenated thiourea (ATX 1-12) via chemical modification of aspirin (a natural product derivative) and evaluated for cytotoxic activity against nasopharyngeal carcinoma (NPC) cell lines, HK-1 via MTS-based colorimetric assay. The cytotoxicity studies demonstrated that hal ...
... Antimicrobial peptides have recently attracted much attention due to their broad-spectrum antimicrobial activity, rapid microbial effects, and minimal tendency toward resistance development. In this study, a series of new C–C terminals and C–N terminals dimer peptides were designed and synthesized by intermolecular dimerization of the partial d-amino acid substitution analogues of Anoplin, and the ...
DNA topoisomerase; X-radiation; antineoplastic activity; binding capacity; cadmium; cell lines; cell movement; chemical structure; coordination compounds; copper; cytoskeletal proteins; cytotoxicity; dose response; drug therapy; electrophoresis; electrospray ionization mass spectrometry; enzyme inhibition; gold; in vitro studies; inhibitory concentration 50; mechanism of action; neoplasm cells; neoplasms; nickel; nucleic acids; protein binding; solubility; zinc
Abstract:
... Molecular structures containing gold, such as auranofin, have been extensively studied in the diagnosis and treatment of many diseases, including cancer treatment. The pharmacological properties of the newly synthesized unique gold-ligand structures have been reported for different cancer cell lines. However, findings on bishydeten-metal salt complexes with gold are rare. In this work, the synthes ...
... Tri(1,3-dichloropropyl) phosphate (TDCPP) potentially damages the thyroid system in humans and animals. However, knowledge of its toxic effects and underlying mechanisms is limited. The present study was conducted to determine the thyroid hormone-disrupting effects of TDCPP and its major metabolite, bis(1,3-dichloro-2-propyl) phosphate (BDCPP) in rat pituitary cell lines (GH3). TDCPP and BDCPP, th ...
binding capacity; computer simulation; cytotoxicity; human serum albumin; hydrogen bonding; metabolites; persistent organic pollutants; phthalates; protein secondary structure; van der Waals forces
Abstract:
... Phthalate esters (PAEs) are a type of persistent organic pollutants and have received widespread concerns due to their adverse effects on human health. Dicyclohexyl phthalate (DCHP) and its metabolite monocyclohexyl phthalate (MCHP) were selected to explore the mechanism for interaction of PAEs with human serum albumin (HSA) through molecular docking and several spectroscopic techniques. The resul ...
... Monoclonal antibodies can effectively target to tumors in patients, as validated by antibody–drug conjugates (ADCs). The clinically used ADCs, nevertheless, are restricted to toxins only and suffer from low drug content, excessive use of antibody, and high cost. Here, we report on trastuzumab-decorated disulfide-cross-linked polymersomes (Tra-Ps) for specific delivery of epirubicin hydrochloride ( ...
... Based on the transcriptome database, we screened out four ferritin subunit genes (MnFer2-5) from the oriental river prawn Macrobrachium nipponense, which encode two non-secretory and two secretory peptides. MnFer2 and 4 possess a strictly conserved ferroxidase site, and MnFer3 has a non-typical ferroxidase site. MnFer5 seems to be a number of ferritin families, which has a distinct dinuclear metal ...
... AIMS: We hypothesized and confirmed that tannic acid (TA) reverses carbapenem resistance by inhibiting carbapenemases in class A and B carbapenemase‐producing Enterobacteriaceae. METHODS AND RESULTS: Minimum inhibitory concentrations of carbapenems in the presence and absence of TA and other efflux pump inhibitors, TA‐carbapenemases inhibition assays and computational studies showed that TA had th ...
Papaver; alcohol oxidoreductases; binding capacity; cell proliferation; cell viability; chemical constituents of plants; computer simulation; cytotoxicity; human cell lines; inhibitory concentration 50; mevalonic acid; receptor protein-tyrosine kinase; screening
Abstract:
... This study revealed that the Papaver lacerum extract strongly inhibited HeLa cell proliferation, resulting in 13% cell viability. As a result of phytochemical studies, one known compound, Tyrosol-1-O-β-xylopyranosyl-(1→6)-O-β-glucopyranoside) (I), and one new compound, 5-O-(6-O-α-rhamnopyronosyl-β-glucopyronosyl) mevalonic acid (II), were isolated. Compounds I and II were found to possess a modera ...
... Disulfide modified lipopeptide assemblies with an arginine-rich dendritic periphery provide a promising platform for effective gene transfer. Dendritic arginine peptides that mimic the cell-penetrating peptides of a virus envelope are vital for complexation, interaction with physical barriers, and final gene release. Here, we report three lipopeptides with different-generation dendritic peripherie ...
... The progressive degeneration of cartilage marks the advancement of osteoarthritis (OA), which requires specific targeted treatment for effective cartilage repair. However, there is still no efficient cartilage delivery system or novel magnetic resonance (MR) contrast agent (CA). Herein, we report the synthesis of a novel class of MR CA, Gd2(CO3)3-based nanoparticles (NPs), from a simpler and “gree ...
... The performance of non-viral gene delivery vehicles, especially cationic polymers, is often challenged by the multiple cellular barriers that pose inconsistent requirements for material properties. A most pronounced inconsistency is exemplified by the molecular weight (MW)-related transfection efficiency and cytotoxicity. In this study, we report the development of photo-degradable, branched poly( ...
... One new amino acid derivative, (–)-β-homoarginine anhydride 1, as well as nine known compounds were isolated from Trichosanthes truncata. The structures of the isolates were elucidated by spectroscopic methods. Among them, compounds 5 and 11 could notably dose-dependently inhibit ROS productions in HaCaT keratinocyte cells without cytotoxicity in the concentration range of 0.2–20 μM. In cell-free ...
... Rhodium metalloinsertors are a unique set of metal complexes that bind specifically to DNA base pair mismatches in vitro and kill mismatch repair (MMR)-deficient cells at lower concentrations than their MMR-proficient counterparts. A family of metalloinsertors containing rhodium–oxygen ligand coordination, termed “Rh–O” metalloinsertors, has been prepared and shown to have a significant increase i ...
binding capacity; breast neoplasms; cell viability; cytotoxicity; detection limit; health hazards; humans; hypochlorites; image analysis; ions; mitochondria; monitoring; neoplasm cells; phosphorescence; surfactants; viability assays; water solubility
Abstract:
... Monitoring hypochlorite anion (ClO⁻) in living cells is particularly meaningful and valuable, because over-exposure of the ClO⁻ may cause a potential health hazard towards animals and humans. Considering the special structure and properties of the gemini surfactant, a novel amphiphilic gemini-iridium complex Ir[(ppy-iso)₂(bpy-tma₂Br₂)] (Ir-iso) with isoniazide as a recognition site for ClO⁻ was de ...