scholarly journals Organometallic carbonyl clusters: a new class of contrast agents for photoacoustic cerebral vascular imaging

2014 ◽  
Vol 50 (20) ◽  
pp. 2601-2603 ◽  
Author(s):  
Kien Voon Kong ◽  
Lun-De Liao ◽  
Zhiyong Lam ◽  
Nitish V. Thakor ◽  
Weng Kee Leong ◽  
...  

The strong photoacoustic signal of a water soluble osmium carbonyl cluster allowed it to be employed as a contrast agent to image the cerebral vasculature of a rat. The high stability and low toxicity of such a compound make it an excellent candidate in such biomedical applications.

2020 ◽  
Author(s):  
Morteza Javadi ◽  
Van A. Ortega ◽  
Alyxandra Thiessen ◽  
Maryam Aghajamali ◽  
Muhammad Amirul Islam ◽  
...  

<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>


2019 ◽  
Vol 26 (30) ◽  
pp. 5609-5624
Author(s):  
Dijana Saftić ◽  
Željka Ban ◽  
Josipa Matić ◽  
Lidija-Marija Tumirv ◽  
Ivo Piantanida

: Among the most intensively studied classes of small molecules (molecular weight < 650) in biomedical research are small molecules that non-covalently bind to DNA/RNA, and another intensively studied class is nucleobase derivatives. Both classes have been intensively elaborated in many books and reviews. However, conjugates consisting of DNA/RNA binder covalently linked to nucleobase are much less studied and have not been reviewed in the last two decades. Therefore, this review summarized reports on the design of classical DNA/RNA binder – nucleobase conjugates, as well as data about their interactions with various DNA or RNA targets, and even in some cases protein targets are involved. According to these data, the most important structural aspects of selective or even specific recognition between small molecule and target are proposed, and where possible related biochemical and biomedical aspects were discussed. The general conclusion is that this, rather new class of molecules showed an amazing set of recognition tools for numerous DNA or RNA targets in the last two decades, as well as few intriguing in vitro and in vivo selectivities. Several lead research lines show promising advancements toward either novel, highly selective markers or bioactive, potentially druggable molecules.


2021 ◽  
Vol 22 (13) ◽  
pp. 7236
Author(s):  
Endah Dwi Hartuti ◽  
Takaya Sakura ◽  
Mohammed S. O. Tagod ◽  
Eri Yoshida ◽  
Xinying Wang ◽  
...  

Plasmodium falciparum’s resistance to available antimalarial drugs highlights the need for the development of novel drugs. Pyrimidine de novo biosynthesis is a validated drug target for the prevention and treatment of malaria infection. P. falciparum dihydroorotate dehydrogenase (PfDHODH) catalyzes the oxidation of dihydroorotate to orotate and utilize ubiquinone as an electron acceptor in the fourth step of pyrimidine de novo biosynthesis. PfDHODH is targeted by the inhibitor DSM265, which binds to a hydrophobic pocket located at the N-terminus where ubiquinone binds, which is known to be structurally divergent from the mammalian orthologue. In this study, we screened 40,400 compounds from the Kyoto University chemical library against recombinant PfDHODH. These studies led to the identification of 3,4-dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-6-imine and its derivatives as a new class of PfDHODH inhibitor. Moreover, the hit compounds identified in this study are selective for PfDHODH without inhibition of the human enzymes. Finally, this new scaffold of PfDHODH inhibitors showed growth inhibition activity against P. falciparum 3D7 with low toxicity to three human cell lines, providing a new starting point for antimalarial drug development.


2020 ◽  
Vol 22 (1) ◽  
pp. 279
Author(s):  
Andrzej Kuczumow ◽  
Renata Chałas ◽  
Jakub Nowak ◽  
Wojciech Smułek ◽  
Maciej Jarzębski

A series of linear profiles of the elements of the enamel in human molar teeth were made with the use of an electron microprobe and a Raman microscope. It is postulated that the enamel can be treated as the superposition of variable “overbuilt” enamel on the stable “core” enamel at the macro-, micro- and nanoscale level. The excessive values characterize the “overbuilt enamel”. All the profiles of excessive parameters along the enamel thickness from the enamel surface to the dentin enamel junction (DEJ) can be approximated very precisely with the use of exponential functions, where Ca, P, Cl and F spatial profiles are decaying while Mg, Na, K and CO32− ones are growing distributions. The “overbuilt” apatite formed on the boundary with DEJ, enriched in Na, Mg, OH and carbonates, reacts continuously with Ca, Cl and F, passing into an acid-resistant form of the “overbuilt” enamel. The apparent phases arriving in boundary regions of the “overbuilt enamel” were proposed. Microdiffraction measurements reveal relative variation of energy levels during enamel transformations. Our investigations are the milestones for a further new class of biomaterial and nanomaterial development for biomedical applications.


Pharmaceutics ◽  
2019 ◽  
Vol 11 (4) ◽  
pp. 166 ◽  
Author(s):  
Lucia Lombardi ◽  
Annarita Falanga ◽  
Valentina Del Genio ◽  
Stefania Galdiero

Peptide drugs hold great promise for the treatment of infectious diseases thanks to their novel mechanisms of action, low toxicity, high specificity, and ease of synthesis and modification. Naturally developing self-assembly in nature has inspired remarkable interest in self-assembly of peptides to functional nanomaterials. As a matter of fact, their structural, mechanical, and functional advantages, plus their high bio-compatibility and bio-degradability make them excellent candidates for facilitating biomedical applications. This review focuses on the self-assembly of peptides for the fabrication of antibacterial nanomaterials holding great interest for substituting antibiotics, with emphasis on strategies to achieve nano-architectures of self-assembly. The antibacterial activities achieved by these nanomaterials are also described.


2020 ◽  
Vol 9 (1) ◽  
pp. 1118-1136
Author(s):  
Zhenjia Huang ◽  
Gary Chi-Pong Tsui ◽  
Yu Deng ◽  
Chak-Yin Tang

AbstractMicro/nano-fabrication technology via two-photon polymerization (TPP) nanolithography is a powerful and useful manufacturing tool that is capable of generating two dimensional (2D) to three dimensional (3D) arbitrary micro/nano-structures of various materials with a high spatial resolution. This technology has received tremendous interest in cell and tissue engineering and medical microdevices because of its remarkable fabrication capability for sophisticated structures from macro- to nano-scale, which are difficult to be achieved by traditional methods with limited microarchitecture controllability. To fabricate precisely designed 3D micro/nano-structures for biomedical applications via TPP nanolithography, the use of photoinitiators (PIs) and photoresists needs to be considered comprehensively and systematically. In this review, widely used commercially available PIs are first discussed, followed by elucidating synthesis strategies of water-soluble initiators for biomedical applications. In addition to the conventional photoresists, the distinctive properties of customized stimulus-responsive photoresists are discussed. Finally, current limitations and challenges in the material and fabrication aspects and an outlook for future prospects of TPP for biomedical applications based on different biocompatible photosensitive composites are discussed comprehensively. In all, this review provides a basic understanding of TPP technology and important roles of PIs and photoresists for fabricating high-precision stimulus-responsive micro/nano-structures for a wide range of biomedical applications.


2001 ◽  
Vol 675 ◽  
Author(s):  
Jeong-Seo Park ◽  
Han-Chang Kang ◽  
Kurt E. Geckeler

ABSTRACTAs [60]fullerene is a very hydrophobic macromolecule, there have been a number of attempts to make it more hydrophilic for biomedical applications. By attaching hydrophilic moieties such as poly(oxyethylene)(POE) chains and cyclodextrin molecules to [60]fullerene, novel water-soluble and biocompatible materials have been successfully prepared [1,2].The synthesis of novel macrocyclic fullerene conjugates which are water-soluble is reported. The telechelic fullerene derivatives have been prepared via addition reaction of POE-based arms with covalently bonded β-cyclodextrin (CD) to [60]fullerene. To this end, a mono-tosylated CD derivative has been prepared in pyridine and then reacted with an amino-functional POE in the presence of triethylamine. The subsequent reaction of [60]fullerene with the hydrophilic POE-conjugated CD-derivative yielded the macrofullerene after separation and purification procedures.The macrocyclic [60]fullerene derivatives obtained were soluble in water and characterized by UV-VIS and FT-IR spectroscopy as well as light scattering measurements and thermogravimetric analysis.


Author(s):  
Rajiv Sharma ◽  
Vikram Jeet Singh ◽  
Pooja A Chawla

Background: The platinum (II) complexes as anticancer agents have been well explored for the development of novel analogs. Yet, none of them achieved clinical importance in oncology. At present, anticancer compounds containing platinum (II) complexes have been employed in the treatment of colorectal, lung, and genitourinary tumors. Among the platinum-based anticancer drugs, Cisplatin (cis-diamine dichloroplatinum (II), cis-[Pt(NH3)2Cl2]) is one of the most potent components of cancer chemotherapy. The nephrotoxicity, neurotoxicity and ototoxicity, and platinum compounds associated resistant cancer are some major disadvantages. Objective: With the rapidly growing interest in platinum (II) complexes in tumor chemotherapy, researchers have synthesized many new platinum analogs as anticancer agents that show better cytotoxicity, and less off-target effects with less cellular resistance. This follows the introduction of oxaliplatin, water-soluble carboplatin, multinuclear platinum and newly synthesized complexes, etc. Method: This review emphasizes recent advancements in drug design and development, the mechanism of platinum (II) complexes, their stereochemistry, current updates, and biomedical applications of platinum-based anticancer agents. Conclusion: In the last few decades, the popularity of platinum complexes as potent anti-cancer agents has risen as scientists have synthesized many new platinum complexes that exhibit better cytotoxicity coupled with less off-target effects.


2021 ◽  
Author(s):  
Salim Albukhaty ◽  
Hassan Al-Karagoly ◽  
alireza allafchian ◽  
Seyed Amir Hossein Jalali ◽  
Thair Alkelabi ◽  
...  

Abstract Electrospun polyvinyl alcohol and Tragacanth Gum were used to develop nanofibrous scaffolds containing poorly water-soluble beta-sitosterol. Different Concentration and Ratio of Polymeric composite: (10%) of β-S concentration in (PVA) 8 %, (TG) 0.5%, and 1% respectively were added, prepared and electrospun. The methods have included four parameters (Solution concentration, feeding rate, voltage, and distance of the collector to the tip of the needle) for designing and compared the nanofibers' average diameters. The nanofibers collected were identified via SEM, FTIR, and XRD measurements. A contact angle measurement described the hydrophilicity of the scaffold. MTT test was assessed for obtained nanofibers by using L929 normal fibroblast cells. The %age of mechanical strength, porosity, and deterioration of the scaffolds was well discussed. The average nanofibre ranged from 63 ± 20 nm to 97 ± 46 nm in diameters. The nanofibers loaded with β-S were freely soluble in water and displayed a short release lag time. The dissolution was related to an immediate dissolution, submicron-level recrystallization of β-S with sufficient conditions for nanofibers for L929 cell culture that could be used in biomedical applications. It concluded that electrospinning is a promising technique for poorly water-soluble β-S formulations that could be used in biomedical applications.


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