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Quinoline core has been shown to possess a promising role in the development of anticancer agents. However, the correlation between its broad spectrum of bioactivity and the underlying mechanism of actions is poorly understood. The present study, with the use of bioinformatics approaches, reported a series of designed molecules which integrated quinoline core and sulfonyl moiety, with the objective of evaluating the substituent and linker effects on anticancer activities and associated mechanistic targets. We identified potent compounds (1h, 2h, 5 and 8) exhibiting significant anticancer effects towards liver cancer cells (Hep3B) with the 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium (MTS) relative values of cytotoxicity below 0.40, a value in the range of doxorubicin positive control with the value of 0.12. Bulky substituents and the presence of bromine atom, as well as the presence of sulfonamide linkage, are likely the favorable structural components for molecules exerting a strong anticancer effect. To the best of our knowledge, our findings obtained from chemical synthesis, in vitro cytotoxicity, bioinformatics-based molecular docking analysis (similarity ensemble approach, SEA),and electrophoretic mobility shift assay provided the first evidence in correlation to the anticancer activities of the selected compound 5 with the modulation on the binding of transcription factor NF-κB to its target DNA. Accordingly, compound 5 represented a lead structure for the development of quinoline-based NF-κB inhibitors and this work added novel information on the understanding of the mechanism of action for bioactive sulfonyl-containing quinoline compounds against hepatocellular carcinoma.

This study reports the synthesis and characterization of quinoline derivatives. The synthesized quinoline compounds were applied to the dyeing treatment of acrylic fabrics. The color fastness to washing and light of quinoline compound-dyed fabrics was examined. Human skin HaCaT cell line was also used for the skin cytotoxicity evaluation of the quinoline compound-dyed acrylic fabrics.

Fenton oxidative wastewater treatment of CI Reactive Black 5 and CI Reactive Blue 19 effluent was performed after a simulated laboratory-scale dyeing process, and the cytotoxicity of the treated effluent was evaluated using human skin cell lines. Among the components for Fenton oxidation, the human skin cell results showed that iron(II)sulfate at 150 mm did not show any significant cytotoxic effect, while other components, such as Glauber's salt solution (20 g l−1; 14%), CI Reactive Black 5 (30 mg l−1; 24%), caustic soda (5 g l−1; 30%), CI Reactive Blue 19 (30 mg l−1; 32%), hydrogen peroxide (0.01 m) and soda ash (5 g l−1) showed cytotoxic potential; the reagent sodium sulfite (30 mm; 48%) exhibited the strongest cytotoxicity level. Fast decolorisation (>95%) was achieved within 10 min for CI Reactive Black 5, while for CI Reactive Blue 19 it took longer (1.5 h) to achieve the same decolorisation. Studies showed that decolorisation for both dyes followed second-order kinetics. In spite of the remarkable efficacy of the Fenton oxidation process in removing colour within a short period of time, the resulting treated wastewater (within a reaction time of 1.5 h) also showed cytotoxicity towards the human HaCaT skin keratinocyte cell line. This observation can be explained by the strong oxidant and intermediate species produced during the advanced oxidation process, and a treatment step using sodium sulfite and a prolonged residence time can help to reduce the cytotoxicity.

Nanotechnology manipulates therapeutic agents at the nanoscale for the development of nanomedicines. However, there are current concerns over nanomedicines, mainly related to the possible toxicity of nanomaterials used for health medications. Due to their small size, they can enter the human body more readily than larger sized particles. Green chemistry encompasses the green synthesis of drug-loaded nanoparticles by reducing the use of hazardous materials in the synthesis process, thus reducing the adverse health impacts of pharmaceutics. This would greatly expand their potential in biomedical treatments. This review highlights the potential risks of nanomedicine formulations to health, delivery routes of green nanomedicines, recent advances in the development of green nanoscale systems for biomedical applications and future perspectives for the green development of nanomedicines.

In this study, a novel green microencapsulation system was used to develop Phyllanthus urinaria (PU) extract containing microcapsules. Agar was used with gelatin as the wall matrix materials of microcapsules to prevent the use of toxic crosslinker formaldehyde. Microencapsulated PU extract was developed to improve the potential antifungal activities of PU water extracts. The active components and surface morphology of PU extract containing microcapsules were analyzed by liquid chromatography/mass spectrometry and scanning electron microscopy, respectively. The in vitro release study demonstrated that approximately 80% of drug was released after 120 h. PU loaded microcapsules were shown to have a stronger anti-Aspergillus niger activity than the free drug.

The use of chitosan as the wall of microcapsule designed for delivery of encapsulated celecoxib is reported. Microcapsules were characterised with respect to size and encapsulation efficiency of celecoxib. In vivo animals demonstrated that both free celecoxib administration and chitosan/celecoxib microcapsules administration lead to a significant inhibition of cyclooxygenase-2 protein expression in the hepatocytes when compared with vehicle control mice. Interestingly, microcapsule containing celecoxib showed a better inhibition of cyclooxygenase-2 protein expression when compared with a simple oral administration of free celecoxib. Gas-chromatography-mass-spectrometry analysis showed that in mice treated with free celecoxib or chitosan/celecoxib microcapsules, their plasma concentration of celecoxib was similar. Microcapsules-based biomaterials as oral drug delivery vehicles may help to improve the absorption efficiency of therapeutic drugs.

Chitosan microcapsules containing calendula oil are prepared by a simple coacervation method. The results show that the performance of the microcapsules, including encapsulation efficiency and particle size, is affected by the change of various processing parameters of microcapsule manufacture. Under the optimal parameter combinations: the chitosan concentration is 1.5 % w/v; the core/wall ratio is 0.1 g mL–1; the stirring speed is 1200 rpm; and the pH value is 10. The compositions and surface morphology of the microcapsules are examined using scanning electron microscope and FTIR spectroscopy. The in vitro cytotoxicity evaluation demonstrates that the microcapsules exhibit no significant cytotoxic effects on human keratinocytes. The in vivo toxicology analysis on mice proves that the microcapsules do not exert any significant necrosis to the liver. It is suggested that our microcapsules could be used as a safe drug carrier both topically and orally.

The safety issues of biomedical applications have been a major concern in recent years. Drug delivery associated with microencapsulation technology has been focused on as microencapsulated drugs are believed to promote comparative therapeutic efficiency on human absorption and prolong the life cycle of drugs. The most commonly applied crosslinker is formaldehyde in a gelatin microencapsulation system, which is considerably toxic to the human body. To reduce the risks involved when using formaldehyde, agar was associated with gelatin as the wall matrix materials of microcapsules as it could crosslink with gelatin to give a gel network in the microcapsules formation. Here we report the development, characterization and safe use of agar–gelatin microcapsules. We further demonstrate that both oral and topical applications are possible using the berberine HCl and gallic acid loaded microcapsules respectively. Microcapsules containing both drugs were prepared combining the optimal parameters identified. The mean drug loading efficiency and the mean particle sizes of the berberine HCl loaded microcapsules were 78.16% and 16.75 μm respectively, while those of gallic acid loaded microcapsules were 70.28% and 21.98 μm respectively. The compositions and surface morphology of berberine HCl and gallic acid containing microcapsules were examined using Fourier transform infrared (FTIR) spectroscopy and scanning electron microscopy (SEM). The in vitro controlled release models demonstrated that the drugs could be gradually released from the microcapsules. The minimum inhibitory concentrations (MICs) and anti-Staphylococcus aureus activity also proved that the berberine HCl loaded microcapsules exhibited better antibacterial activity towards Staphylococcus aureus when compared with those of the original drugs. The in vitro drug delivery model also demonstrated the delivery of berberine HCl from microcapsule treated textiles into nude mice skin. The in vivo mice disease model also showed that gallic acid loaded microcapsules were helpful in the treatment of acute liver and kidney toxicity after an overdose administration of acetaminophen. The development of agar–gelatin microcapsules was demonstrated to be an efficient, deliverable tool for both oral and topical applications.