scholarly journals Improvement of Water Solubility of Mercaptoundecahydrododecaborate (BSH)-Peptides by Conjugating with Ethylene Glycol Linker and Interaction with Cyclodextrin

Processes ◽  
2021 ◽  
Vol 9 (1) ◽  
pp. 167
Author(s):  
Mizuki Kitamatsu ◽  
Ayaka Nakamura-Tachibana ◽  
Yoshimichi Ishikawa ◽  
Hiroyuki Michiue

We previously developed a conjugate consisting of 10B cluster BSH and tri-arginine peptide (BSH-3R). This could potentially be used as a boron agent for boron neutron capture therapy; however, it possesses poor water solubility and thus needs to be improved for use as medicine. In this study, we devised several means of improving the water solubility of BSH-3R. As one of them, we used cyclodextrin (CD), which was expected to improve the water solubility resulting from interaction of the BSH-3R with CD. We evaluated the solubility of BSH-3R in aqueous CD solution by using reverse-phase high-performance liquid chromatography. As we expected, the solubility of BSH-3R was increased in a manner dependent on the addition of β-CD and γ-CD in aqueous solution. Furthermore, we synthesized BSH conjugated to oligoarginine having various chain lengths (BSH-nR) and BSH-3R with ethylene glycol linkers introduced between BSH and 3R (BSH-nEg-3R). The water solubility of these BSH peptides was also evaluated and the results showed that the introduction of nEg to BSH-3R markedly improved the water solubility. Furthermore, we found that the water solubility of these peptides can be further improved by also applying CD.

1992 ◽  
Vol 70 (6) ◽  
pp. 1827-1832 ◽  
Author(s):  
Garry W. Buchko ◽  
Jean Cadet

Benzophenone-mediated photosensitization of 2′-deoxyguanosine (dG) and thymidylyl-(3′-5′)-2′-deoxyguanosine (d(TpG)) at 350 nm in oxygen-saturated aqueous solution produces 2-deoxy-D-ribono-1,4-lactone (dL) and thymidylyl-(3′-5′)-2-deoxy-D-ribono-1,4-lactone (d(TpL)), respectively. These photoproducts have been isolated by reverse phase high-performance liquid chromatography and characterized by proton magnetic resonance spectroscopy and fast atom bombardment mass spectroscopy. Conformational analysis of d(TpG) and d(TpL) in aqueous solution using coupling constant data suggests no major conformational differences between the two dinucleoside monophosphates.


2020 ◽  
Vol 16 ◽  
Author(s):  
Kirubanandam Grace Pavithra ◽  
Vasudevan Jaikumar ◽  
Ponnusamy Senthil Kumar ◽  
PanneerSelvam SundarRajan

Background: Many antibiotics were widely used as medication based on their distinctive features. Among them, sulphonamides were commonly used, however their recalcitrant nature makes them difficult to dispose. Hence, their interaction with environment and analytic technique requires considerable attention globally. Objective: Therefore, this review aimed to provide detailed discussion about environmental as well as human health behaviour and analytic techniques corresponding to sulphonamides. Methods: Various results and discussion were extracted from technical journals and books published by different researchers from all over the world. The cited bibliographic references were intentionally investigated in order to extract relevant information related to proposed work. Results: In this review, the determination techniques such as UV-spectroscopy, Enthalpimetry, Immunosensor, Chromatography, Chemiluminescence, Photoinduced fluorometric determination, Capillary electrophoresis for sulphonamide determination were discussed in detail. Among them, High performance liquid chromatography (HPLC) and UV-spectroscopy was effective and extensively used for screening sulphonamide. Conclusion: Knowing the quantification and behaviour of sulphonamide in aqueous solution is mandatory to opt the suitable wastewater treatment required. Hence, choosing appropriate high precision and feasible screening techniques is necessary, which can be attained with this review.


2015 ◽  
Vol 1718 ◽  
pp. 97-102 ◽  
Author(s):  
Toralf Roch ◽  
Konstanze K. Julich-Gruner ◽  
Axel T. Neffe ◽  
Nan Ma ◽  
Andreas Lendlein

ABSTRACTPolymer-based therapeutic strategies require biomaterials with properties and functions tailored to the demands of specific applications leading to an increasing number of newly designed polymers. For the evaluation of those new materials, comprehensive biocompatibility studies including cyto-, tissue-, and immunocompatibility are essential. Recently, it could be demonstrated that star-shaped amino oligo(ethylene glycol)s (sOEG) with a number average molecular weight of 5 kDa and functionalized with the phenol-derived moieties desaminotyrosine (DAT) or desaminotyrosyl tyrosine (DATT) behave in aqueous solution like surfactants without inducing a substantial cytotoxicity, which may qualify them as solubilizer for hydrophobic drugs in aqueous solution. However, for biomedical applications the polymer solutions need to be free of immunogenic contaminations, which could result from inadequate laboratory environment or contaminated starting material. Furthermore, the materials should not induce uncontrolled or undesired immunological effects arising from material intrinsic properties. Therefore, a comprehensive immunological evaluation as perquisite for application of each biomaterial batch is required. This study investigated the immunological properties of sOEG-DAT(T) solutions, which were prepared using sOEG with number average molecular weights of 5 kDa, 10 kDa, and 20 kDa allowing analyzing the influence of the sOEG chain lengths on innate immune mechanisms. A macrophage-based assay was used to first demonstrate that all DAT(T)-sOEG solutions are free of endotoxins and other microbial contaminations such as fungal products. In the next step, the capacity of the different DAT(T)-functionalized sOEG solutions to induce cytokine secretion and generation of reactive oxygen species (ROS) was investigated using whole human blood. It was observed that low levels of the pro-inflammatory cytokines interleukin(IL)-1β and IL-6 were detected for all sOEG solutions but only when used at concentrations above 250 µg·mL-1. Furthermore, only the 20 kDa sOEG-DAT induced low amounts of ROS-producing monocytes. Conclusively, the data indicate that the materials were not contaminated with microbial products and do not induce substantial immunological adverse effectsin vitro,which is a prerequisite for future biological applications.


1986 ◽  
Vol 153 (2) ◽  
pp. 230-234 ◽  
Author(s):  
Koon-Sea Hui ◽  
Maria Hui ◽  
Fung-Chow Chiu ◽  
Miriam Banay-Schwartz ◽  
Teresita Deguzman ◽  
...  

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