scholarly journals Exceptionally rapid oxime and hydrazone formation promoted by catalytic amine buffers with low toxicity

2018 ◽  
Vol 9 (23) ◽  
pp. 5252-5259 ◽  
Author(s):  
Dennis Larsen ◽  
Anna M. Kietrys ◽  
Spencer A. Clark ◽  
Hyun Shin Park ◽  
Andreas Ekebergh ◽  
...  
Keyword(s):  
Low Toxicity ◽  
Amine Buffers

A novel molecular strategy for accelerating hydrazone and oxime formations, using bifunctional buffer compounds that not only control pH but also catalyze the reaction, is presented.

Challenges of Aircraft and Drone Spray Applications

2020 ◽  
Vol 31 (2) ◽  
pp. 83-88 ◽  
Author(s):  
Fernando K. Carvalho ◽  
Rodolfo G. Chechetto ◽  
Alisson A. B. Mota ◽  
Ulisses R. Antuniassi
Keyword(s):  
Smallholder Farmers ◽  
Crop Protection ◽  
Crop Canopy ◽  
Target Species ◽  
Buffer Zones ◽  
Correct Dose ◽  
Knapsack Sprayer ◽  
Water Courses ◽  
Low Toxicity ◽  
Heavy Loads

Crop protection on major crops is now required to follow the principles of integrated pest management so the timing and accuracy of any application of a pesticide or biopesticide has to be more precise to minimize adverse effects on non-target species. The development of UAVs (unmanned aerial vehicles) provides a means of providing a more targeted application of the correct dose, especially by using formulations that are more persistent, thus minimizing loss of spray in areas subject to rain. Avoiding use of too high a dosage allows greater survival of natural enemies and reduces the selection pressure for pests becoming resistant to specific modes of action. The downward flow of air from a UAV should also provide better distribution and impaction of droplets within a crop canopy, reduce soil impaction caused by taking heavy loads of spray applied with 200 l ha–1 of water, and allow treatments when fields are too wet to access with ground equipment. In Asia, many smallholder farmers are using a drone in preference to using a knapsack sprayer. According to Matthews, it has been shown that ULV spraying can be effective, but it needs a narrow droplet spectrum with the droplets remaining stable and not shrinking to become too small. Formulation research can reduce the volatility of the spray, hence the success of oil-based sprays. However, instead of petroleum-based oils, there is a chance to develop vegetable oil carriers with micro-sized particle suspensions to deliver low toxicity pesticides in droplets that can be deposited within the crop and not drift beyond the crop boundary. Oil deposits will be less prone to loss after rain so less should be lost in neighbouring ditches and water courses, especially as rainfall patterns are forecast to change. More studies are needed to evaluate the swath for deposition, buffer zones, formulation, nozzle selection, to guide future specific legislation for UAV applications.

Cellular Uptake and Magneto-Hyperthermia Induced Cytotoxicity using Photoluminescent Fe3O4 Nanoparticle/Si Quantum Dot Hybrids

2020 ◽  
Author(s):  
Morteza Javadi ◽  
Van A. Ortega ◽  
Alyxandra Thiessen ◽  
Maryam Aghajamali ◽  
Muhammad Amirul Islam ◽  
...  
Keyword(s):  
Radio Frequency ◽  
Biomedical Applications ◽  
Short Term ◽  
Water Dispersible ◽  
Optical Responses ◽  
Si Quantum Dot ◽  
Real World Applications ◽  
Potential Benefits ◽  
Low Toxicity ◽  
Si Quantum Dots

<p>The design and fabrication of Si-based multi-functional nanomaterials for biological and biomedical applications is an active area of research. The potential benefits of using Si-based nanomaterials are not only due to their size/surface-dependent optical responses but also the high biocompatibility and low-toxicity of silicon itself. Combining these characteristics with the magnetic properties of Fe<sub>3</sub>O<sub>4</sub> nanoparticles (NPs) multiplies the options available for real-world applications. In the current study, biocompatible magnetofluorescent nano-hybrids have been prepared by covalent linking of Si quantum dots to water-dispersible Fe<sub>3</sub>O<sub>4</sub> NPs <i>via</i> dicyclohexylcarbodiimide (DCC) coupling. We explore some of the properties of these magnetofluorescent nano-hybrids as well as evaluate uptake, the potential for cellular toxicity, and the induction of acute cellular oxidative stress in a mast cells-like cell line (RBL-2H3) by heat induction through short-term radio frequency modulation (10 min @ 156 kHz, 500 A). We found that the NPs were internalized readily by the cells and also penetrated the nuclear membrane. Radio frequency activated nano-hybrids also had significantly increased cell death where > 50% of the RBL-2H3 cells were found to be in an apoptotic or necrotic state, and that this was attributable to increased triggering of oxidative cell stress mechanisms. </p>

Aggregated AA1-42 is Selectively Toxic for Neurons, Whereas Glial Cells Produce Mature Fibrils with Low Toxicity in Drosophila

2018 ◽  
Author(s):  
Maria Jonson ◽  
Sofie Nystrrm ◽  
Alexander Sandberg ◽  
Marcus Carlback ◽  
Wojciech Michno ◽  
...  
Keyword(s):  
Glial Cells ◽  
Low Toxicity

Click Reactions in Chemistry of Triterpenes - Advances Towards Development of Potential Therapeutics

2018 ◽  
Vol 25 (5) ◽  
pp. 636-658 ◽  
Author(s):  
Jan Pokorny ◽  
Lucie Borkova ◽  
Milan Urban
Keyword(s):  
Biological Activities ◽  
Synthetic Approach ◽  
Clinical Use ◽  
New Approach ◽  
Click Reactions ◽  
Drug Candidates ◽  
The Past ◽  
Low Toxicity ◽  
New Compounds ◽  
Potential Therapeutics

Triterpenoids are natural compounds with a large variety of biological activities such as anticancer, antiviral, antibacterial, antifungal, antiparazitic, antiinflammatory and others. Despite their low toxicity and simple availability from the natural resources, their clinical use is still severely limited by their higher IC50 and worse pharmacological properties than in the currently used therapeutics. This fact encouraged a number of researchers to develop new terpenic derivatives more suitable for the potential clinical use. This review summarizes a new approach to improve both, the activity and ADME-Tox properties by connecting active terpenes to another modifying molecules using click reactions. Within the past few years, this synthetic approach was well explored yielding a lot of great improvements of the parent compounds along with some less successful attempts. A large quantity of the new compounds presented here are superior in both activity and ADME-Tox properties to their parents. This review should serve the researchers who need to promote their hit triterpenic structures towards their clinical use and it is intended as a guide for the chemical synthesis of better drug candidates.

Carbon Dots for Bacterial Detection and Antibacterial Applications-A Minireview

2020 ◽  
Vol 25 (46) ◽  
pp. 4848-4860 ◽  
Author(s):  
Anisha Anand ◽  
Gopinathan Manavalan ◽  
Ranju Prasad Mandal ◽  
Huan-Tsung Chang ◽  
Yi-Ru Chiou ◽  
...  
Keyword(s):  
Optical Properties ◽  
Carbon Dots ◽  
Antibacterial Effect ◽  
Bacterial Detection ◽  
High Brightness ◽  
Photo Catalysis ◽  
Wide Range ◽  
Prevention And Treatment ◽  
Low Toxicity ◽  
Conventional Antibiotics

: The prevention and treatment of various infections caused by microbes through antibiotics are becoming less effective due to antimicrobial resistance. Researches are focused on antimicrobial nanomaterials to inhibit bacterial growth and destroy the cells, to replace conventional antibiotics. Recently, carbon dots (C-Dots) become attractive candidates for a wide range of applications, including the detection and treatment of pathogens. In addition to low toxicity, ease of synthesis and functionalization, and high biocompatibility, C-Dots show excellent optical properties such as multi-emission, high brightness, and photostability. C-Dots have shown great potential in various fields, such as biosensing, nanomedicine, photo-catalysis, and bioimaging. This review focuses on the origin and synthesis of various C-Dots with special emphasis on bacterial detection, the antibacterial effect of CDots, and their mechanism.

Anticancer Activity of Natural Flavonoids: Inhibition of HIF-1α Signaling Pathway

2020 ◽  
Vol 23 (26) ◽  
pp. 2945-2959 ◽  
Author(s):  
Xiangping Deng ◽  
Yijiao Peng ◽  
Jingduo Zhao ◽  
Xiaoyong Lei ◽  
Xing Zheng ◽  
...  
Keyword(s):  
Transcription Factor ◽  
Secondary Metabolites ◽  
Anticancer Agents ◽  
Hypoxia Inducible Factor ◽  
Tumor Hypoxia ◽  
Pharmacological Activities ◽  
Hypoxia Inducible Factor 1 ◽  
The Past ◽  
Low Toxicity ◽  
Tumor Blood Vessels

Rapid tumor growth is dependent on the capability of tumor blood vessels and glycolysis to provide oxygen and nutrients. Tumor hypoxia is a common characteristic of many solid tumors, and it essentially happens when the growth of the tumor exceeds the concomitant angiogenesis. Hypoxia-inducible factor 1 (HIF-1) as the critical transcription factor in hypoxia regulation is activated to adapt to this hypoxia situation. Flavonoids, widely distributed in plants, comprise many polyphenolic secondary metabolites, possessing broadspectrum pharmacological activities, including their potentiality as anticancer agents. Due to their low toxicity, intense efforts have been made for investigating natural flavonoids and their derivatives that can be used as HIF-1α inhibitors for cancer therapy during the past few decades. In this review, we sum up the findings concerning the inhibition of HIF-1α by natural flavonoids in the last few years and propose the idea of designing tumor vascular and glycolytic multi-target inhibitors with HIF-1α as one of the targets.

Nano Phytomedicine Based Delivery System for CNS Disease

2020 ◽  
Vol 21 (9) ◽  
pp. 661-673 ◽  
Author(s):  
Mohammed Asadullah Jahangir ◽  
Chettupalli Anand ◽  
Abdul Muheem ◽  
Sadaf Jamal Gilani ◽  
Mohamad Taleuzzaman ◽  
...  
Keyword(s):  
Herbal Medicine ◽  
Low Cost ◽  
Herbal Medicines ◽  
Herbal Drugs ◽  
Widespread Acceptance ◽  
The Central Nervous System ◽  
Low Toxicity ◽  
Ancient Times ◽  
Plant Sources ◽  
Herbal Formulations

Herbal medicines are being used since ancient times and are an important part of the alternative and traditional medicinal system. In recent decades, scientists are embracing herbal medicines based on the fact that a number of drugs that are currently in use are derived directly or indirectly from plant sources. Moreover, herbal drugs have lesser side effects, albeit are potentially strong therapeutic agents. The herbal medicine market is estimated to be around US $62 billion globally. Herbal medicine has gained widespread acceptance due to its low toxicity, low cost, ease of accessibility and efficacy in treating difficult diseases. Safety and efficacy are another important factors in the commercialization process of herbal medicines. Nanotechnology has been shown to be potentially effective in improving the bioactivity and bioavailability of herbal medicines. Development of nano-phytomedicines (or by reducing the size of phytomedicine), attaching polymers with phytomedicines and modifying the surface properties of herbal drugs, have increased the solubility, permeability and eventually the bioavailability of herbal formulations. Novel formulations such as niosomes, liposomes, nanospheres, phytosomes etc., can be exploited in this area. This article reviews herbal medicines, which have prominent activity in the Central Nervous System (CNS) disorders and reported nano-phytomedicines based delivery systems.

Recent Advances on Therapeutic Peptides for Breast Cancer Treatment

2020 ◽  
Vol 21 ◽  
Author(s):  
Samad Beheshtirouy ◽  
Farhad Mirzaei ◽  
Shirin Eyvazi ◽  
Vahideh Tarhriz
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Tumor Cells ◽  
Breast Cancer Cells ◽  
Specific Binding ◽  
High Specificity ◽  
The Novel ◽  
Anti Cancer ◽  
Therapeutic Peptides ◽  
Low Toxicity

: Breast cancer is a heterogeneous malignancy which is the second cause of mortality among women in the world. Increasing the resistance to anti-cancer drugs in breast cancer cells persuades researchers to search the novel therapies approaches for the treatment of the malignancy. Among the novel methods, therapeutic peptides which target and disrupt tumor cells have been of great interest. Therapeutic peptides are short amino acids monomer chains with high specificity to bind and modulate a protein interaction of interest. Several advantages of peptides such as specific binding on tumor cells surface, low molecular weight and low toxicity on normal cells make the peptides as an appealing therapeutic agents against solid tumors, particularly breast cancer. Also, National Institutes of Health (NIH) describes therapeutic peptides as suitable candidate for the treatment of drug-resistant breast cancer. In this review, we attempt to review the different therapeutic peptides against breast cancer cells which can be used in treatment and diagnosis of the malignancy. Meanwhile, we presented an overview of peptide vaccines which have been developed for the treatment of breast cancer.

Coumarin Hybrids: Promising Scaffolds in the Treatment of Breast Cancer

2019 ◽  
Vol 19 (17) ◽  
pp. 1443-1458 ◽  
Author(s):  
Rohit Bhatia ◽  
Ravindra K. Rawal
Keyword(s):  
Breast Cancer ◽  
Lung Cancer ◽  
Therapeutic Agents ◽  
Toxicity Profile ◽  
Biological Targets ◽  
Organ Systems ◽  
Hybrid Molecules ◽  
Cause Of Deaths ◽  
Low Toxicity ◽  
Diverse Mode

: Breast cancer is the most common invasive cancer in women, and the second main cause of deaths in women, after lung cancer. There is continuous advancement in the development of therapeutic agents against breast cancer in recent years and it is still in progress. Development of hybrid molecules by combining different pharmacophores to obtain significant biological activity is an excellent approach. Coupling of coumarin scaffold with other distinct motifs has led to the design of newer compounds against breast cancer. These distinct pharmacophores possess a diverse mode of action as well as selectivity. It has been reported in the literature that coumarin hybrids possess significant potency against breast cancer by binding to various biological targets which are associated with breast cancer. Due to low toxicity profile on various organ systems, coumarin hybrids have nowadays attracted the keen attention of researchers to explore their therapeutic ability against breast cancer. Reported coumarin hybrids include coupling with isoxazole, thiazole, monastrol, chalcone, triazole, sulphonamide, triphenylethylene, benzimidazole, pyran, imidazole, stilbene, oestrogen, phenylsulphonylfuroxan, etc. In the present review, a description of various coumarin hybrid molecules has been presented along with their structural-activity relationships.

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