scholarly journals Increasing the Cytotoxicity of Ru(II) Polypyridyl Complexes by Tuning the Electronic Structure of Dioxo Ligands

2019 ◽  
Author(s):  
Anna Notaro ◽  
Marta Jakubaszek ◽  
Nils Rotthowe ◽  
Federica Maschietto ◽  
Patrick Felder ◽  
...  
Keyword(s):  
Chemical Properties ◽  
Direct Interaction ◽  
Biological Properties ◽  
Drug Candidate ◽  
Strong Impact ◽  
Biological Investigation ◽  
Physico Chemical ◽  
Severe Impairment ◽  
The Difference ◽  
High Cytotoxicity

<div>Due to the great potential expressed by an anticancer drug candidate previously reported by our group, namely Ru-sq ([Ru(DIP)2(sq)](PF6) (DIP: 4,7-diphenyl-1,10-phenanthroline, sq: semiquinonate ligand), we describe in this work a structure-activity relationship (SAR) that involves a broader range of derivatives resulting from the coordination of different catecholate-like dioxoligands to the same Ru(DIP)2 core. More in detail, we chose catechols carrying either electron-donating or electronwithdrawing groups EDG or EWG and investigated the physico-chemical and biological properties of their complexes. Several pieces of experimental evidences demonstrated that the coordination of catechols bearing EDGs led to deep red positively charged complexes 1–4 in which the preferred oxidation state of the dioxoligand is the uninegatively charged semiquinonate. Complexes 5 and 6, on the other hand, are blue/violet neutral complexes which carry an EWG substituted dinegatively charged catecholate ligand. The biological investigation of complexes 1–6 led to the conclusion that the difference in their physico-chemical properties has a strong impact on their biological activity. Thus, complexes 1–4 expressed much higher cytotoxicities than complexes 5 and 6. Complex 1 constitutes the most promising compound of the series and was selected for a more in-depth biological investigation. Apart from its remarkably high cytotoxicity (IC50 = 0.07–0.7 μM in different cancerous cell lines) complex 1 was taken up by HeLa cells very efficiently by a passive transportation mechanism. Moreover, its moderate accumulation in several cellular compartments (i.e. nucleus, lysosomes, mitochondria and cytoplasm) is extremely advantageous in the search of a potential drug with multiple modes of action. Further DNA metalation and metabolic studies pointed to the direct interaction of complex 1 with DNA and to the severe impairment of the mitochondrial function. Multiple targets, together with its outstanding cytotoxicity, make complex 1 a valuable candidate in the field of chemotherapy research.</div>

scholarly journals Increasing the Cytotoxicity of Ru(II) Polypyridyl Complexes by Tuning the Electronic Structure of Dioxo Ligands

2019 ◽  
Author(s):  
Anna Notaro ◽  
Marta Jakubaszek ◽  
Nils Rotthowe ◽  
Federica Maschietto ◽  
Patrick Felder ◽  
...  
Keyword(s):  
Chemical Properties ◽  
Direct Interaction ◽  
Biological Properties ◽  
Drug Candidate ◽  
Strong Impact ◽  
Biological Investigation ◽  
Physico Chemical ◽  
Severe Impairment ◽  
The Difference ◽  
High Cytotoxicity

<div>Due to the great potential expressed by an anticancer drug candidate previously reported by our group, namely Ru-sq ([Ru(DIP)2(sq)](PF6) (DIP: 4,7-diphenyl-1,10-phenanthroline, sq: semiquinonate ligand), we describe in this work a structure-activity relationship (SAR) that involves a broader range of derivatives resulting from the coordination of different catecholate-like dioxoligands to the same Ru(DIP)2 core. More in detail, we chose catechols carrying either electron-donating or electronwithdrawing groups EDG or EWG and investigated the physico-chemical and biological properties of their complexes. Several pieces of experimental evidences demonstrated that the coordination of catechols bearing EDGs led to deep red positively charged complexes 1–4 in which the preferred oxidation state of the dioxoligand is the uninegatively charged semiquinonate. Complexes 5 and 6, on the other hand, are blue/violet neutral complexes which carry an EWG substituted dinegatively charged catecholate ligand. The biological investigation of complexes 1–6 led to the conclusion that the difference in their physico-chemical properties has a strong impact on their biological activity. Thus, complexes 1–4 expressed much higher cytotoxicities than complexes 5 and 6. Complex 1 constitutes the most promising compound of the series and was selected for a more in-depth biological investigation. Apart from its remarkably high cytotoxicity (IC50 = 0.07–0.7 μM in different cancerous cell lines) complex 1 was taken up by HeLa cells very efficiently by a passive transportation mechanism. Moreover, its moderate accumulation in several cellular compartments (i.e. nucleus, lysosomes, mitochondria and cytoplasm) is extremely advantageous in the search of a potential drug with multiple modes of action. Further DNA metalation and metabolic studies pointed to the direct interaction of complex 1 with DNA and to the severe impairment of the mitochondrial function. Multiple targets, together with its outstanding cytotoxicity, make complex 1 a valuable candidate in the field of chemotherapy research.</div>

Chitosan-Nanocellulose Composites for Regenerative Medicine Applications

2020 ◽  
Vol 27 (28) ◽  
pp. 4584-4592 ◽  
Author(s):  
Avik Khan ◽  
Baobin Wang ◽  
Yonghao Ni
Keyword(s):  
Regenerative Medicine ◽  
Preparation Method ◽  
Chemical Properties ◽  
Biological Properties ◽  
Next Generation ◽  
Structure Property ◽  
Physico Chemical ◽  
Structure Property Relationship ◽  
Attractive Candidate ◽  
Fundamental Understanding

Regenerative medicine represents an emerging multidisciplinary field that brings together engineering methods and complexity of life sciences into a unified fundamental understanding of structure-property relationship in micro/nano environment to develop the next generation of scaffolds and hydrogels to restore or improve tissue functions. Chitosan has several unique physico-chemical properties that make it a highly desirable polysaccharide for various applications such as, biomedical, food, nutraceutical, agriculture, packaging, coating, etc. However, the utilization of chitosan in regenerative medicine is often limited due to its inadequate mechanical, barrier and thermal properties. Cellulosic nanomaterials (CNs), owing to their exceptional mechanical strength, ease of chemical modification, biocompatibility and favorable interaction with chitosan, represent an attractive candidate for the fabrication of chitosan/ CNs scaffolds and hydrogels. The unique mechanical and biological properties of the chitosan/CNs bio-nanocomposite make them a material of choice for the development of next generation bio-scaffolds and hydrogels for regenerative medicine applications. In this review, we have summarized the preparation method, mechanical properties, morphology, cytotoxicity/ biocompatibility of chitosan/CNs nanocomposites for regenerative medicine applications, which comprises tissue engineering and wound dressing applications.

scholarly journals Exploring the difference in xerogels and organogels through in situ observation

2018 ◽  
Vol 5 (1) ◽  
pp. 170492
Author(s):  
Binglian Bai ◽  
Zhiming Li ◽  
Haitao Wang ◽  
Min Li ◽  
Yukihiro Ozaki ◽  
...  
Keyword(s):  
Liquid Crystalline ◽  
Fluorescence Spectra ◽  
Chemical Properties ◽  
Columnar Structure ◽  
In Situ Observation ◽  
Physico Chemical ◽  
Aggregation Structure ◽  
Ft Ir ◽  
The Difference

Solvent–gelator interactions play a key role in mediating organogel formation and ultimately determine the physico-chemical properties of the organogels and xerogels. The ethanol organogels of 1,4-bis[(3,4,5-trihexyloxy phenyl)hydrazide]phenylene (TC6) were investigated in situ by FT-IR, Raman and fluorescence spectra, and XRD, and it was confirmed that the intermolecular interaction and aggregation structure of TC6 ethanol organogels were quite different from those of xerogels. Simultaneously, unprecedented phase transition from organogel to suspension upon heating was observed in ethanol organogel, and the suspension phase exhibited lytropic liquid crystalline behaviour with a rectangular columnar structure. This study may open the possibility to design new gelators with a new dimension of versatility.

scholarly journals Synthesis, physico-chemical properties of 3-thio and 3-thio -4-amino derivatives of 1,2,4-triazole

2019 ◽  
pp. 28-44
Author(s):  
V. V. Parchenko
Keyword(s):  
Chemical Properties ◽  
Biological Properties ◽  
Modern Medicine ◽  
Toxic Substances ◽  
Triazole Derivatives ◽  
Synthetic Drugs ◽  
Physico Chemical ◽  
Methods Of Synthesis ◽  
Amino Derivatives ◽  
Derivatives Of

Modern medicine and pharmacy has at its disposal highly efficient synthetic drugs. Large extent of these drugs accounted for derivatives of 1,2,4-triazole. The purpose of the work was an attempt to summarize the literature in recent years related to the methods of synthesis and study of physico-chemical properties 3-thio- and 3-thio-4-amino derivatives of 1,2,4-triazole. Studies national scientists in recent years indicates prospects of the search in this direction, since this class of organic compounds is interest not only to scientists pharmaceutical, medical and veterinary field, but also among researchers of engineering, metallurgical and agricultural areas. 1,2,4-triazole derivatives are also widely used in practice for optical materials, photosensitizers are used as coloring agents, antioxidants, additives for fuels and oils, some of which are widely used as corrosion inhibitors for controlling various pests in agriculture. In addition, 1,2,4-triazole derivatives belong to the class low toxic or essentially non-toxic substances. The presence of a growing number of publications about methods of synthesis, reactions, physico-chemical and biological properties of 1,2,4-triazole, inspires scientists around the world search for perspective molecules of substituted 1,2,4-triazole. It should be noted that in spite of a sufficient amount of information about the derivatives of 1,2,4-triazole, some issues related to the generalization of data in the literature synthesis presented insufficient.

In vitro elucidation of suppression effects of composts to soil-borne pathogen Phytophthora nicotianae on pepper plants using 16S amplicon sequencing and metaproteomics

2018 ◽  
Vol 35 (2) ◽  
pp. 206-214 ◽  
Author(s):  
Margarita Ros ◽  
Josefa Blaya ◽  
Petr Baldrian ◽  
Felipe Bastida ◽  
Hans H Richnow ◽  
...  
Keyword(s):  
Chemical Properties ◽  
Amplicon Sequencing ◽  
Biological Properties ◽  
Phytophthora Nicotianae ◽  
Wall Structure ◽  
Inorganic Ion ◽  
Physico Chemical ◽  
Phylogenetic Level ◽  
Pepper Plants

AbstractCompost production is a critical component of organic waste management. One of the most important properties of compost is its ability to suppress soil-borne pathogens such as Phytophthora nicotianae in pepper plants. Both the physico-chemical and biological properties of composts can be responsible for the suppression of pathogens, although biological properties are the main driver. In this study, we analyzed composts with various levels of suppressiveness against P. nicotianae. We analyzed both physico-chemical properties like pH and electrical conductivity and biological properties like microbial activity, amplicon sequencing and metaproteomics. We believed that the link between community structures and proteins could provide deep insights into the mechanism of compost suppressiveness. Our results indicate that there are differences between suppressive and non-suppressive composts at the phylogenetic level (sequencing) and at the functional level (based on analysis of the cluster of orthologous groups, COGs). The proteins identified were assigned to the carbohydrate process, cell wall structure and inorganic ion transport and metabolism. Proteobacteria could also be new indicators of P. nicotianae suppression.

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