The advent of Camptothecin added a new dimension in the field anticancer drug development containing quinoline motif. Quinoline scaffold plays an important role in anticancer drug development as ...their derivatives have shown excellent results through different mechanism of action such as growth inhibitors by cell cycle arrest, apoptosis, inhibition of angiogenesis, disruption of cell migration, and modulation of nuclear receptor responsiveness. The anti-cancer potential of several of these derivatives have been demonstrated on various cancer cell lines. In this review we have compiled and discussed specifically the anticancer potential of quinoline derivatives, which could provide a low-height flying bird's eye view of the quinoline derived compounds to a medicinal chemist for a comprehensive and target oriented information for development of clinically viable anticancer drugs.
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•Quinoline scaffold as an attractive target for anticancer drug development.•An overview about the progress of quinoline derivatives as anticancer agent from Camptothecin till date.•The mode of action of various quinoline derivatives is discussed.•This review will help to get ideas on structural requirement of quinoline scaffold as anticancer agent.
This review presents the detailed account of factors leading to cancer and design strategy for the synthesis of benzimidazole derivatives as anticancer agents. The recent survey for cancer treatment ...in Cancer facts and figures 2017 American Chemical Society has shown progressive development in fighting cancer. Researchers all over the world in both developed and developing countries are in a continuous effort to tackle this serious concern. Benzimidazole and its derivatives showed a broad range of biological activities due to their resemblance with naturally occurring nitrogenous base i.e. purine. The review discussed benzimidazole derivatives showing anticancer properties through a different mechanism viz. intercalation, alkylating agents, topoisomerases, DHFR enzymes, and tubulin inhibitors. Benzimidazole derivatives act through a different mechanism and the substituents reported from the earlier and recent research articles are prerequisites for the synthesis of targeted based benzimidazole derivatives as anticancer agents. The review focuses on an easy comparison of the substituent essential for potency and selectivity through SAR presented in figures. This will further provide a better outlook or fulfills the challenges faced in the development of novel benzimidazole derivatives as anticancer.
During the COVID-19 pandemic, one of the major concerns was a medical emergency in human society. Therefore it was necessary to control or restrict the disease spreading among populations in any ...fruitful way at that time. To frame out a proper policy for controlling COVID-19 spreading with limited medical facilities, here we propose an
SEQAIHR
model having saturated treatment. We check biological feasibility of model solutions and compute the basic reproduction number (
R
0
). Moreover, the model exhibits transcritical, backward bifurcation and forward bifurcation with hysteresis with respect to different parameters under some restrictions. Further to validate the model, we fit it with real COVID-19 infected data of Hong Kong from 19th December, 2021 to 3rd April, 2022 and estimate model parameters. Applying sensitivity analysis, we find out the most sensitive parameters that have an effect on
R
0
. We estimate
R
0
using actual initial growth data of COVID-19 and calculate effective reproduction number for same period. Finally, an optimal control problem has been proposed considering effective vaccination and saturated treatment for hospitalized class to decrease density of the infected class and to minimize implemented cost.
The present study demonstrated the systematic adaptation of quality by design-integrated approach for the development of novel nanostructured lipid carrier (NLC) of an anti-hypertensive drug ...isradipine (ISD) to address the inherent challenges such as low solubility and low oral bioavailability. Plackett-Burman design was used for preliminary screening of significant process and formulation variables (p <0.05), which were further processed using Box-Behnken design for the attainment of optimization goal that is, mean particle size (85.7 ± 7.3 nm), drug entrapment efficiency (87.4 ± 3.29%), and in vitro drug release characteristics (92.89 ± 5.47%). The optimized ISD-NLC formulation also demonstrated well-dispersed uniform-shaped particles (polydispersity index 0.207 ± 0.029), high gastrointestinal fluid stability (zeta potential -10.17 ± 0.59 mV), and higher in vitro gut permeation (21.69 ± 2.38 μg/cm
of ISD-NLC as compared to 11.23 ± 1.74 μg/cm
in ISD suspension). Furthermore, lipolysis studies were performed for the purpose of in vivo fate, and significantly higher drug content of ISD from ISD-NLC in aqueous phase was found (72.34 ± 4.62%) as compared to drug suspension (3.01 ± 0.91%). Relative bioavailability of ISD-NLC and ISD suspension was increased by 4.2-fold and 1.78-fold in the absence and presence of cycloheximide which is a lymphatic uptake inhibitor revealing lymphatic uptake of ISD-NLC in bioavailability improvement. Hence, systematic adaptation of quality by design integrated approach improved gut permeation and potential solubilizaton fate (dynamic lipolysis) of ISD-NLC, which further improved the lymphatic uptake and biodistribution of drug thereby promisingits in vivo prospect and clinical efficacy.
The SEIQHR model, introduced in this study, serves as a valuable tool for anticipating the emergence of various infectious diseases, such as COVID-19 and illnesses transmitted by insects. An analysis ...of the model’s qualitative features was conducted, encompassing the computation of the fundamental reproduction number, R0. It was observed that the disease-free equilibrium point remains singular and locally asymptotically stable when R0<1, while the endemic equilibrium point exhibits uniqueness when R0>1. Additionally, specific conditions were outlined to guarantee the local asymptotic stability of both equilibrium points. Employing numerical simulations, the graphical representation illustrated the influence of model parameters on disease dynamics and the potential for its eradication across different noninteger orders of the Caputo derivative. In essence, the adoption of a fractional epidemic model contributes to a deeper comprehension and enhanced biological insights into the dynamics of diseases.
•Impact of global warming on marine ecosystems described via mathematical modeling.•Model formulation, Analysis, Simulations, and Case study approach in detail.•Global warming is rapidly damaging ...marine plankton along with fishery resources.•Marine plankton can enrich fishery resources by reducing global warming.•The future of marine ecosystems as a result of rapid global warming.
A mathematical model with time-varying parameters is newly proposed to describe the potential effects of rapid global warming on marine ecosystems. The time-varying parameters are assumed to vary in time, for example, environmental factors or a change in marine organisms. The existence of the proposed model is verified, as well as the stability of each equilibrium point is investigated. Beside, simulations, as well as a case study, are also carried out to justify the findings of this study comparing with others. It is found that global warming, because of the rapid concentration of greenhouse gases (GHGs), is leading marine ecosystems to an imbalanced situation by reducing significantly the marine plankton and fishery resources. Moreover, it is shown that if the density of marine plankton or its ability to absorb carbon dioxide (CO2) can be increased, it can improve marine fishery resources by reducing global warming. Beside, this study could explain how marine ecosystems may change in the future as a result of rapid global warming. This study predicts that if the present situation of rapid global warming continues for the next 50 years unabated, it can damage marine ecosystems especially fishery resources in the long run. Overall, this study establishes a mathematical relationship between the environment and marine ecosystems that could contribute to environmental and fisheries management.
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A new mathematical model on human resources divided employees into two compartments, namely, fresher and expert employees, has been designed and analyzed. A system of ordinary nonlinear differential ...equations has three state variables including vacancies. This model describes the dynamics of the number of fresher employees and expert employees as well as vacancies and shows the impacts of training programs and benefits of provided facilities for employees. The equilibria of this proposed model are determined, and its stability at these points is checked. Moreover, characteristics of state variables with respect to parameters have been discussed. Using two optimal control variables, this study finds the maximum number of experts including the minimum cost of provided facilities as well as the training program based on Pontryagin’s maximum principle.
The world suffers from the acute respiratory syndrome COVID-19 pandemic, which will be scary if other co-existing illnesses exacerbate it. The co-occurrence of the COVID-19 virus with kidney disease ...has not been available in the literature. So, further research needs to be conducted to reveal the transmission dynamics of COVID-19 and kidney disease. This study aims to create mathematical models to understand how COVID-19 interacts with kidney diseases in specific populations. Therefore, the initial step was to formulate a deterministic Susceptible-Infected-Recovered (SIR) mathematical model to depict the co-infection dynamics of COVID-19 and kidney disease. A mathematical model with seven compartments has been developed using nonlinear ordinary differential equations. This model incorporates the invariant region, disease-free and endemic equilibrium, along with the positivity solution. The basic reproduction number, calculated via the next-generation matrix, allows us to assess the stability of the equilibrium. Sensitivity analysis is also utilised to understand the influence of each parameter on disease spread or containment. The results show that a surge in COVID-19 infection rates and the existence of kidney disease significantly enhances the co-infection risks. Numerical simulations further clarify the potential outcomes of treating COVID-19 alone, kidney disease alone, and co-infected cases. The study of the potential model can be utilised to maximise the benefits of simulation to minimise the global health complexity of COVID-19 and kidney disease.
The development of useful biomaterials has resulted in significant advances in various fields of science and technology. The demand for new biomaterial designs and manufacturing techniques continues ...to grow, with the goal of building a sustainable society. In this study, two types of DNA-cationic surfactant complexes were synthesized using commercially available deoxyribonucleic acid from herring sperm DNA (hsDNA, <50 bp) and deoxyribonucleic acid from salmon testes DNA (stDNA, ~2000 bp). The DNA-surfactant complexes were blended with a polylactic acid (PLA) biopolymer and electrospun to obtain nanofibers, and then copper nanoparticles were synthesized on nanofibrous webs. Scanning electron microscopic images showed that all nanofibers possessed uniform morphology. Interestingly, different diameters were observed depending on the base pairs in the DNA complex. Transmission electron microscopy showed uniform growth of copper nanoparticles on the nanofibers. Fourier-transform infrared spectroscopy spectra confirmed the uniform blending of both types of DNA complexes in PLA. Both stDNA- and hsDNA-derived nanofibers showed greater biocompatibility than native PLA nanofibers. Furthermore, they exerted significant antibacterial activity in the presence of copper nanoparticles. This study demonstrates that DNA is a potentially useful material to generate electrospun nanofibrous webs for use in biomedical sciences and technologies.
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