scholarly journals Rational Design 2-Hydroxypropylphosphonium Salts as Cancer Cell Mitochondria-Targeted Vectors: Synthesis, Structure, and Biological Properties

Molecules ◽  
2021 ◽  
Vol 26 (21) ◽  
pp. 6350
Author(s):  
Vladimir F. Mironov ◽  
Andrey V. Nemtarev ◽  
Olga V. Tsepaeva ◽  
Mudaris N. Dimukhametov ◽  
Igor A. Litvinov ◽  
...  
Keyword(s):  
Targeted Delivery ◽  
Rational Design ◽  
Phosphonium Salt ◽  
Boron Trifluoride Etherate ◽  
Biological Properties ◽  
High Yield ◽  
Phosphonium Salts ◽  
Duodenal Adenocarcinoma ◽  
Wide Range ◽  
High Antitumor Activity

It has been shown for a wide range of epoxy compounds that their interaction with triphenylphosphonium triflate occurs with a high chemoselectivity and leads to the formation of (2-hydroxypropyl)triphenylphosphonium triflates 3 substituted in the 3-position with an alkoxy, alkylcarboxyl group, or halogen, which were isolated in a high yield. Using the methodology for the disclosure of epichlorohydrin with alcohols in the presence of boron trifluoride etherate, followed by the substitution of iodine for chlorine and treatment with triphenylphosphine, 2-hydroxypropyltriphenylphosphonium iodides 4 were also obtained. The molecular and supramolecular structure of the obtained phosphonium salts was established, and their high antitumor activity was revealed in relation to duodenal adenocarcinoma. The formation of liposomal systems based on phosphonium salt 3 and L-α-phosphatidylcholine (PC) was employed for improving the bioavailability and reducing the toxicity. They were produced by the thin film rehydration method and exhibited cytotoxic properties. This rational design of phosphonium salts 3 and 4 has promising potential of new vectors for targeted delivery into mitochondria of tumor cells.

SLS-catalyzed Multi-component One-pot Reactions for the Convenient Synthesis of Spiro[indoline-3,4’-pyrano [2,3-c]pyrazole] Derivatives

2020 ◽  
Vol 07 ◽  
Author(s):  
Archana Dhakar ◽  
Archana Rajput ◽  
Ghazala Khanum ◽  
Dau D. Agarwal
Keyword(s):  
Anticancer Agents ◽  
Heterocyclic Compounds ◽  
Ethyl Cyanoacetate ◽  
Reaction Times ◽  
Thermal Conditions ◽  
Biological Properties ◽  
High Yield ◽  
Spectroscopic Techniques ◽  
One Pot ◽  
Wide Range

Background,Objective: : spiro[indoline-3,4′-pyrano[2,3-c]pyrazoles] derivatives are an important heterocyclic compounds. These compounds shows wide range of biological properties and exhibits varied pharmaceutical applications. Pyranopyrazoles, which are basically fused heterocyclic compounds and act as vasodilators, hypertensive, hypoglycaemic, and anticancer agents. Methods: An efficient and micelle-promoted surfactant catalyzed synthesis of spiro[indoline-3,4′-pyrano[2,3-c]pyrazoles] derivatives have been achieved via one-pot four-component reaction of hydrazine hydrate (phenyl hydrazine), ethyl acetoacetate, malononitrile (ethyl cyanoacetate) and isatin under thermal conditions (at 60°C) in water as a solvent. Results: Sodium lauryl sulphate (SLS) used has been found to be an efficient and green catalyst. The compounds reported during this work were obtained in excellent yield, in a short duration of time and ease of work up. They were purified by recrystalization from ethanol, and also the synthesized compounds were characterized by various spectroscopic techniques. Conclusion: The method offers several advantages such as safe, cost-effective and catalyst easily recovered and reused for a minimum of five cycles, that confirms its good stability. Short reaction times, high yield and usage of eco-friendly catalyst and solvent are the key features of this methodology.

Natural-based Hydrogels: A Journey from Simple to Smart Networks for Medical Examination

2020 ◽  
Vol 27 (16) ◽  
pp. 2704-2733
Author(s):  
Javad Tavakoli ◽  
Jing Wang ◽  
Clarence Chuah ◽  
Youhong Tang
Keyword(s):  
Mechanical Properties ◽  
Targeted Delivery ◽  
Biological Properties ◽  
Medical Examination ◽  
Fine Tuning ◽  
Historical Evolution ◽  
Self Healing ◽  
Physiological Conditions ◽  
Wide Range ◽  
Fluorescent Bioprobes

Natural hydrogels, due to their unique biological properties, have been used extensively for various medical and clinical examinations that are performed to investigate the signs of disease. Recently, complex-crosslinking strategies improved the mechanical properties and advanced approaches have resulted in the introduction of naturally derived hydrogels that exhibit high biocompatibility, with shape memory and self-healing characteristics. Moreover, the creation of self-assembled natural hydrogels under physiological conditions has provided the opportunity to engineer fine-tuning properties. To highlight recent studies of natural-based hydrogels and their applications for medical investigation, a critical review was undertaken using published papers from the Science Direct database. This review presents different natural-based hydrogels (natural, natural-synthetic hybrid and complex-crosslinked hydrogels), their historical evolution, and recent studies of medical examination applications. The application of natural-based hydrogels in the design and fabrication of biosensors, catheters and medical electrodes, detection of cancer, targeted delivery of imaging compounds (bioimaging) and fabrication of fluorescent bioprobes is summarised here. Without doubt, in future, more useful and practical concepts will be derived to identify natural-based hydrogels for a wide range of clinical examination applications.

Facile Synthesis of a Diverse Library of Mono-3-substituted β-Cyclodextrin Analogues

2018 ◽  
Author(s):  
Kathryn Kellett ◽  
Brendan M. Duggan ◽  
Michael Gilson
Keyword(s):  
High Yield ◽  
Facile Synthesis ◽  
Wide Range

We have described simple, high-yield, protocols, which require only commonly accessible equipment, to synthesize a wide range of β-CD derivatives mono-substituted at the secondary face. These derivatives may be useful in their own right, and they are also scaffolds for further modification, and examples of the far broader array of derivatives that may be accessed by these procedures.

BOTANICAL COMPOSITION AND PRODUCTIVITY OF PERENNIAL GRASSES AGROPHYTOCENOSES WITH TETRAPLOID MEADOW CLOVER

1970 ◽  
pp. 59-62
Author(s):  
N. I. Kasatkina ◽  
Zh. S. Nelyubina
Keyword(s):  
Dry Weight ◽  
Single Species ◽  
Lotus Corniculatus ◽  
Specific Weight ◽  
Biological Properties ◽  
Phleum Pratense ◽  
Perennial Grasses ◽  
High Yield ◽  
Botanical Composition ◽  
The Third

The biological properties of plants, their mutual relations under different growth conditions and at different periods of their life, must be known for obtaining highly productive agrophytocenoses with participation of a meadow clover (Trifolium pratense L.). Botanical composition and fodder productivity of perennial grasses in agrocenoses with participation of meadow tetraploid clover Kudesnik were studied in 2014-2017. It was revealed that in the first and second years of use the agrophytocenosis, the yield of green mass was formed due to meadow tetraploid clover, the share of its participation in the first mowing was at level of 71-87% and 64-97% respectively. Specific weight of clover in multispecies agrocenoses considerably decreased by the third year of use: in the first mowing up to 32-68%, in the second - up to 8-52%. At the same time, the percentage of long-term herbaceous grasses increased: meadow timothy (Phleum pratense L.) - up to 34-54%, eastern galega (Galéga orientális Lam.) - up to 33%, changeable alfalfa (Medicago x varia Martyn) - up to 22-54%, lotus corniculatus (Lotus corniculatus L.) - up to 14-19%. The proportion of weed admixture in single-species clover planting was 12%, in agrocenoses - 2-14%. The grass mixtures clover + timothy and clover + alfalfa + timothy were less infested by weeds. High yield of dry weight of single-species sowing of meadow tetraploid clover was obtained in the first two years of use - 7.8 and 6.5 tons / ha, respectively. By the third year of use, the productivity of clover has decreased to 2.9 t / ha. On average, for three years of use, the highest yield (6.2-6.3 t / ha) was formed by agrocenoses meadow tetraploid clover + meadow timothy and meadow tetraploid clover + changeable alfalfa + meadow timothy.

α-Alkoxyalkyl Triphenylphosphonium Salts: Synthesis and Reactions

2019 ◽  
Vol 23 (16) ◽  
pp. 1738-1755
Author(s):  
Humaira Y. Gondal ◽  
Zain M. Cheema ◽  
Abdul R. Raza ◽  
Ahmed Abbaskhan ◽  
M. I. Chaudhary
Keyword(s):  
Carbonyl Compounds ◽  
Claisen Rearrangement ◽  
Alder Reaction ◽  
Coupling Reactions ◽  
Phosphonium Salts ◽  
Organic Transformations ◽  
Enol Ethers ◽  
Wide Range ◽  
Synthetic Methodologies ◽  
Alkoxy Groups

Following numerous applications of Wittig reaction now functionalized phosphonium salts are gaining attention due to their characteristic properties and diverse reactivity. This review is focused on α-alkoxyalkyl triphenylphosphonium salts: an important class of functionalized phosphonium salts. Alkoxymethyltriphenylphosphonium salts are majorly employed in the carbon homologation of carbonyl compounds and preparation of enol ethers. Their methylene insertion strategy is extensively demonstrated in the total synthesis of a wide range of natural products and other important organic molecules. Similarly enol ethers prepared thereof are important precursors for different organic transformations like Diels-Alder reaction, Claisen rearrangement, Coupling reactions, Olefin metathesis and Nazarov cyclization. Reactivity of these α-alkoxyalkylphosphonium salts have also been studied in the nucleophilic substitution reactions. A distinctive application of this class of phosphonium salts was recently reported in the phenylation of carbonyl compounds under very mild conditions. Synthesis of structurally diverse alkoxymethyltriphenylphosphonium salts with variation in alkoxy groups as well as counter anions are reported in literature. Here we present a detailed account of different synthetic methodologies for the preparation of this unique class of quaternary phosphonium salts and their applications in organic synthesis.

scholarly journals 99mTc Labelling Strategies for the Development of Potential Nitroimidazolic Hypoxia Imaging Agents

Inorganics ◽  
2019 ◽  
Vol 7 (11) ◽  
pp. 128 ◽  
Author(s):  
Giglio ◽  
Rey
Keyword(s):  
Rational Design ◽  
Biological Properties ◽  
Fine Tuning ◽  
Oxidation States ◽  
Hypoxia Imaging ◽  
Biological Target ◽  
99Mtc Radiopharmaceuticals ◽  
99Mtc Labelling

Technetium-99m has a rich coordination chemistry that offers many possibilities in terms of oxidation states and donor atom sets. Modifications in the structure of the technetium complexes could be very useful for fine tuning the physicochemical and biological properties of potential 99mTc radiopharmaceuticals. However, systematic study of the influence of the labelling strategy on the “in vitro” and “in vivo” behaviour is necessary for a rational design of radiopharmaceuticals. Herein we present a review of the influence of the Tc complexes’ molecular structure on the biodistribution and the interaction with the biological target of potential nitroimidazolic hypoxia imaging radiopharmaceuticals presented in the literature from 2010 to the present. Comparison with the gold standard [18F]Fluoromisonidazole (FMISO) is also presented.

scholarly journals Self-assembling ferritin-dendrimer nanoparticles for targeted delivery of nucleic acids to myeloid leukemia cells

2021 ◽  
Vol 19 (1) ◽  
Author(s):  
Federica Palombarini ◽  
Silvia Masciarelli ◽  
Alessio Incocciati ◽  
Francesca Liccardo ◽  
Elisa Di Fabio ◽  
...  
Keyword(s):  
Nucleic Acid ◽  
Targeted Delivery ◽  
Myeloid Leukemia ◽  
Electrostatic Interactions ◽  
Archaeoglobus Fulgidus ◽  
Leukemia Cells ◽  
Cellular Delivery ◽  
Self Assembling ◽  
Wide Range ◽  
Hybrid Nanoparticle

Abstract Background In recent years, the use of ferritins as nano-vehicles for drug delivery is taking center stage. Compared to other similar nanocarriers, Archaeoglobus fulgidus ferritin is particularly interesting due to its unique ability to assemble-disassemble under very mild conditions. Recently this ferritin was engineered to get a chimeric protein targeted to human CD71 receptor, typically overexpressed in cancer cells. Results Archaeoglobus fulgidus chimeric ferritin was used to generate a self-assembling hybrid nanoparticle hosting an aminic dendrimer together with a small nucleic acid. The positively charged dendrimer can indeed establish electrostatic interactions with the chimeric ferritin internal surface, allowing the formation of a protein-dendrimer binary system. The 4 large triangular openings on the ferritin shell represent a gate for negatively charged small RNAs, which access the internal cavity attracted by the dense positive charge of the dendrimer. This ternary protein-dendrimer-RNA system is efficiently uptaken by acute myeloid leukemia cells, typically difficult to transfect. As a proof of concept, we used a microRNA whose cellular delivery and induced phenotypic effects can be easily detected. In this article we have demonstrated that this hybrid nanoparticle successfully delivers a pre-miRNA to leukemia cells. Once delivered, the nucleic acid is released into the cytosol and processed to mature miRNA, thus eliciting phenotypic effects and morphological changes similar to the initial stages of granulocyte differentiation. Conclusion The results here presented pave the way for the design of a new family of protein-based transfecting agents that can specifically target a wide range of diseased cells. Graphic abstract

scholarly journals Isobornylchalcones as Scaffold for the Synthesis of Diarylpyrazolines with Antioxidant Activity

Molecules ◽  
2021 ◽  
Vol 26 (12) ◽  
pp. 3579
Author(s):  
Svetlana A. Popova ◽  
Evgenia V. Pavlova ◽  
Oksana G. Shevchenko ◽  
Irina Yu. Chukicheva ◽  
Aleksandr V. Kutchin
Keyword(s):  
Antioxidant Activity ◽  
Antioxidant Properties ◽  
Biological Properties ◽  
High Reactivity ◽  
Biologically Active ◽  
Brain Lipids ◽  
Wide Range ◽  
Privileged Structure ◽  
Vitro Model

The pyrazoline ring is defined as a “privileged structure” in medicinal chemistry. A variety of pharmacological properties of pyrazolines is associated with the nature and position of various substituents, which is especially evident in diarylpyrazolines. Compounds with a chalcone fragment show a wide range of biological properties as well as high reactivity which is primarily due to the presence of an α, β-unsaturated carbonyl system. At the same time, bicyclic monoterpenoids deserve special attention as a source of a key structural block or as one of the pharmacophore components of biologically active molecules. A series of new diarylpyrazoline derivatives based on isobornylchalcones with different substitutes (MeO, Hal, NO2, N(Me)2) was synthesized. Antioxidant properties of the obtained compounds were comparatively evaluated using in vitro model Fe2+/ascorbate-initiated lipid peroxidation in the substrate containing brain lipids of laboratory mice. It was demonstrated that the combination of the electron-donating group in the para-position of ring B and OH-group in the ring A in the structure of chalcone fragment provides significant antioxidant activity of synthesized diarylpyrazoline derivatives.

scholarly journals Bioactive potential of natural biomaterials: identification, retention and assessment of biological properties

2021 ◽  
Vol 6 (1) ◽  
Author(s):  
Kieran Joyce ◽  
Georgina Targa Fabra ◽  
Yagmur Bozkurt ◽  
Abhay Pandit
Keyword(s):  
Tissue Engineering ◽  
Therapeutic Potential ◽  
Biological Properties ◽  
Biological Assessment ◽  
Cross Linking ◽  
Natural Polymers ◽  
Drug Delivery Device ◽  
Biomedical Device ◽  
Wide Range ◽  
Bioactive Potential

AbstractBiomaterials have had an increasingly important role in recent decades, in biomedical device design and the development of tissue engineering solutions for cell delivery, drug delivery, device integration, tissue replacement, and more. There is an increasing trend in tissue engineering to use natural substrates, such as macromolecules native to plants and animals to improve the biocompatibility and biodegradability of delivered materials. At the same time, these materials have favourable mechanical properties and often considered to be biologically inert. More importantly, these macromolecules possess innate functions and properties due to their unique chemical composition and structure, which increase their bioactivity and therapeutic potential in a wide range of applications. While much focus has been on integrating these materials into these devices via a spectrum of cross-linking mechanisms, little attention is drawn to residual bioactivity that is often hampered during isolation, purification, and production processes. Herein, we discuss methods of initial material characterisation to determine innate bioactivity, means of material processing including cross-linking, decellularisation, and purification techniques and finally, a biological assessment of retained bioactivity of a final product. This review aims to address considerations for biomaterials design from natural polymers, through the optimisation and preservation of bioactive components that maximise the inherent bioactive potency of the substrate to promote tissue regeneration.

scholarly journals MXenes for future nanophotonic device applications

Nanophotonics ◽  
2020 ◽  
Vol 9 (7) ◽  
pp. 1831-1853
Author(s):  
Jaeho Jeon ◽  
Yajie Yang ◽  
Haeju Choi ◽  
Jin-Hong Park ◽  
Byoung Hun Lee ◽  
...  
Keyword(s):  
Solar Cells ◽  
Transition Metal ◽  
Wide Spectrum ◽  
Building Blocks ◽  
Optoelectronic Device ◽  
High Yield ◽  
Saturable Absorption ◽  
Nanophotonic Device ◽  
Wide Range ◽  
Device Applications

AbstractTwo-dimensional (2D) layers of transition metal carbides, nitrides, or carbonitrides, collectively referred to as MXenes, are considered as the new family of 2D materials for the development of functional building blocks for optoelectronic and photonic device applications. Their advantages are based on their unique and tunable electronic and optical properties, which depend on the modulation of transition metal elements or surface functional groups. In this paper, we have presented a comprehensive review of MXenes to suggest an insightful perspective on future nanophotonic and optoelectronic device applications based on advanced synthesis processes and theoretically predicted or experimentally verified material properties. Recently developed optoelectronic and photonic devices, such as photodetectors, solar cells, fiber lasers, and light-emitting diodes are summarized in this review. Wide-spectrum photodetection with high photoresponsivity, high-yield solar cells, and effective saturable absorption were achieved by exploiting different MXenes. Further, the great potential of MXenes as an electrode material is predicted with a controllable work function in a wide range (1.6–8 eV) and high conductivity (~104 S/cm), and their potential as active channel material by generating a tunable energy bandgap is likewise shown. MXene can provide new functional building blocks for future generation nanophotonic device applications.

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