scholarly journals Pentafluorophenyl Platinum(II) Complexes of PTA and its N-Allyl and N-Benzyl Derivatives: Synthesis, Characterization and Biological Activity

Materials ◽  
2019 ◽  
Vol 12 (23) ◽  
pp. 3907 ◽  
Author(s):  
Sgarbossa ◽  
Śliwińska-Hill ◽  
Guedes da ilva ◽  
Bażanów ◽  
Pawlak ◽  
...  
Keyword(s):  
Dermal Fibroblast ◽  
Human Dermal Fibroblast ◽  
Phosphine Ligands ◽  
Water Soluble ◽  
Breast Adenocarcinoma ◽  
Cytotoxic Activities ◽  
Cervix Carcinoma ◽  
X Ray Diffraction ◽  
Normal Human Dermal Fibroblast ◽  
Human Lung Carcinoma

From the well-known 1,3,5-triaza-phosphaadamantane (PTA, 1a), the novel N-allyl and N-benzyl tetrafuoroborate salts 1-allyl-1-azonia-3,5-diaza-7-phosphaadamantane (APTA(BF4), 1b) and 1-benzyl-1-azonia-3,5-diaza-7-phosphaadamantane (BzPTA(BF4), 1c) were obtained. These phosphines were then allowed to react with (Pt(μ-Cl)(C6F5)(tht))2 (tht = tetrahydrothiophene) affording the water soluble Pt(II) complexes trans-(PtCl(C6F5)(PTA)2) (2a) and its bis-cationic congeners trans-(PtCl(C6F5)(APTA)2)(BF4)2 (2b) and trans-(PtCl(C6F5)(BzPTA)2)(BF4)2 (2c). The compounds were fully characterized by multinuclear NMR, ESI-MS, elemental analysis and (for 2a) also by single crystal X-ray diffraction, which proved the trans configuration of the phosphine ligands. Furthermore, in order to evaluate the cytotoxic activities of all complexes the normal human dermal fibroblast (NHDF) cell culture were used. The antineoplastic activity of the investigated compounds was checked against the human lung carcinoma (A549), epithelioid cervix carcinoma (HeLa) and breast adenocarcinoma (MCF-7) cell cultures. Interactions between the complexes and human serum albumin (HSA) using fluorescence spectroscopy and circular dichroism spectroscopy (CD) were also investigated.

scholarly journals Synthesis, Structural, and Cytotoxic Properties of New Water-Soluble Copper(II) Complexes Based on 2,9-Dimethyl-1,10-Phenanthroline and Their One Derivative Containing 1,3,5-Triaza-7-Phosphaadamantane-7-Oxide

Molecules ◽  
2020 ◽  
Vol 25 (3) ◽  
pp. 741 ◽  
Author(s):  
Ewelina I. Śliwa ◽  
Urszula Śliwińska-Hill ◽  
Barbara Bażanów ◽  
Miłosz Siczek ◽  
Julia Kłak ◽  
...  
Keyword(s):  
Cell Line ◽  
Electrostatic Interactions ◽  
Dermal Fibroblast ◽  
Cd Spectroscopy ◽  
Water Soluble ◽  
Breast Adenocarcinoma ◽  
Cytotoxic Activities ◽  
Cervix Carcinoma ◽  
Magnetic Studies ◽  
Normal Human Dermal Fibroblast

A series of water-soluble copper(II) complexes based on 2,9-dimethyl-1,10-phenanthroline (dmphen) and mixed-ligands, containing PTA=O (1,3,5-triaza-7-phosphaadamantane-7-oxide) have been synthesized and fully characterized. Two types of complexes have been obtained, monocationic [Cu(NO3)(O-PTA=O)(dmphen)][PF6] (1), [Cu(Cl)(dmphen)2][PF6] (2), and neutral [Cu(NO3)2(dmphen)] (3). The solid-state structures of all complexes have been determined by single-crystal X-ray diffraction. Magnetic studies for the complex 1–3 indicated a very weak antiferromagnetic interaction between copper(II) ions in crystal lattice. Complexes were successfully evaluated for their cytotoxic activities on the normal human dermal fibroblast (NHDF) cell line and the antitumor activity using the human lung carcinoma (A549), epithelioid cervix carcinoma (HeLa), colon (LoVo), and breast adenocarcinoma (MCF-7) cell lines. Complexes 1 and 3 revealed lower toxicity to NHDF than A549 and HeLa cells, meanwhile compound 2 appeared to be more toxic to NHDF cell line in comparison to all cancer lines. Additionally, interactions between the complexes and human apo-transferrin (apo-Tf) using fluorescence and circular dichroism (CD) spectroscopy were also investigated. All compounds interacted with apo-transferrin, causing same changes of the protein conformation. Electrostatic interactions dominate in the 1/2 – apo- Tf systems and hydrophobic and ionic interactions in the case of 3.

scholarly journals In Vitro Bioeffects of Polyelectrolyte Multilayer Microcapsules Post-Loaded with Water-Soluble Cationic Photosensitizer

Pharmaceutics ◽  
2020 ◽  
Vol 12 (7) ◽  
pp. 610 ◽  
Author(s):  
Alexey V. Ermakov ◽  
Roman A. Verkhovskii ◽  
Irina V. Babushkina ◽  
Daria B. Trushina ◽  
Olga A. Inozemtseva ◽  
...  
Keyword(s):  
Targeted Delivery ◽  
Dermal Fibroblast ◽  
Human Dermal Fibroblast ◽  
Water Soluble ◽  
Zinc Phthalocyanine ◽  
Bacterial Strains ◽  
Normal Human Dermal Fibroblast ◽  
Drug Dosing ◽  
Normal Human

Microencapsulation and targeted delivery of cytotoxic and antibacterial agents of photodynamic therapy (PDT) improve the treatment outcomes for infectious diseases and cancer. In many cases, the loss of activity, poor encapsulation efficiency, and inadequate drug dosing hamper the success of this strategy. Therefore, the development of novel and reliable microencapsulated drug formulations granting high efficacy is of paramount importance. Here we report the in vitro delivery of a water-soluble cationic PDT drug, zinc phthalocyanine choline derivative (Cholosens), by biodegradable microcapsules assembled from dextran sulfate (DS) and poly-l-arginine (PArg). A photosensitizer was loaded in pre-formed [DS/PArg]4 hollow microcapsules with or without exposure to heat. Loading efficacy and drug release were quantitatively studied depending on the capsule concentration to emphasize the interactions between the DS/PArg multilayer network and Cholosens. The loading data were used to determine the dosage for heated and intact capsules to measure their PDT activity in vitro. The capsules were tested using human cervical adenocarcinoma (HeLa) and normal human dermal fibroblast (NHDF) cell lines, and two bacterial strains, Gram-positive Staphylococcus aureus and Gram-negative Escherichia coli. Our results provide compelling evidence that encapsulated forms of Cholosens are efficient as PDT drugs for both eukaryotic cells and bacteria at specified capsule-to-cell ratios.

scholarly journals Evaluation of Electrospun Poly(ε-Caprolactone)/Gelatin Nanofiber Mats Containing Clove Essential Oil for Antibacterial Wound Dressing

Pharmaceutics ◽  
2019 ◽  
Vol 11 (11) ◽  
pp. 570 ◽  
Author(s):  
Irem Unalan ◽  
Stefan J. Endlein ◽  
Benedikt Slavik ◽  
Andrea Buettner ◽  
Wolfgang H. Goldmann ◽  
...  
Keyword(s):  
Essential Oil ◽  
Fiber Diameter ◽  
Dermal Fibroblast ◽  
Human Dermal Fibroblast ◽  
Gas Chromatography Mass Spectrometry ◽  
Normal Human Dermal Fibroblast ◽  
Cytotoxic Effects ◽  
Normal Human ◽  
Clove Essential Oil ◽  
Nanofiber Mats

The objective of this study was to produce antibacterial poly(ε-caprolactone) (PCL)-gelatin (GEL) electrospun nanofiber mats containing clove essential oil (CLV) using glacial acetic acid (GAA) as a “benign” (non-toxic) solvent. The addition of CLV increased the fiber diameter from 241 ± 96 to 305 ± 82 nm. Aside from this, the wettability of PCL-GEL nanofiber mats was increased by the addition of CLV. Fourier-transform infrared spectroscopy (FTIR) analysis confirmed the presence of CLV, and the actual content of CLV was determined by gas chromatography–mass spectrometry (GC-MS). Our investigations showed that CLV-loaded PCL-GEL nanofiber mats did not have cytotoxic effects on normal human dermal fibroblast (NHDF) cells. On the other hand, the fibers exhibited antibacterial activity against Staphylococcus aureus and Escherichia coli. Consequently, PCL-GEL/CLV nanofiber mats are potential candidates for antibiotic-free wound healing applications.

Antioxidant and Enzyme Inhibitory Activities of Areca catechu, Boesenbergia rotunda, Piper betle and Orthosiphon aristatus for Potential Skin Anti-aging Properties

2018 ◽  
Vol 17 (3) ◽  
pp. 229-235
Author(s):  
Z.A. Mat Yasin ◽  
A.S. Khazali ◽  
F. Ibrahim ◽  
N. Nor Rashid ◽  
R. Yusof
Keyword(s):  
Plant Extracts ◽  
Dermal Fibroblast ◽  
Radical Scavenging ◽  
Human Dermal Fibroblast ◽  
Piper Betle ◽  
Fibroblast Cells ◽  
Normal Human Dermal Fibroblast ◽  
Areca Catechu ◽  
Aging Properties ◽  
Normal Human

Medicinal plants have been traditionally used for various applications including skin care. In this study, Areca catechu, Boesenbergia rotunda, Piper betle and Orthosiphon aristatus were tested for antioxidant and anti-aging properties. These plant extracts were subjected to 1,1-diphenyl-picrylhydrazyl (DPPH) and 2,2ʹ-azinobis(3-ethylbenzothiazoline)-6-sulphonic acid (ABTS) radical scavenging activity analyses. The extracts were then assessed for collagenase, elastase and hyaluronidase inhibition and subjected to toxicity study in normal human dermal fibroblast cells. Lastly, bioactive compounds in these plant extracts were identified using high performance liquid chromatography. We found that Piper betle and Areca catechu possessed high total flavonoid and phenolic contents. These two extracts showed the best IC50 values for DPPH and ABTS radical scavenging activities and also demonstrated the highest elastase and collagenase inhibition when compared to the other two plant extracts. These crude plants extracts were also non-toxic to normal human dermal fibroblast cells. Our HPLC results identified several potential bioactive compounds in these plant extracts that could be crucial in mediating the observed effects. Based on our results, these plant extracts especially Piper betle and Areca catechu extracts possess significant antioxidant and anti-aging properties and could be utilized in the development of safe and cost-effective anti-aging treatments.

Attachment and Proliferation of Human Dermal Fibroblasts onto ECM-Immobilized PLGA Films

2005 ◽  
Vol 288-289 ◽  
pp. 291-294
Author(s):  
Hyun Joo Son ◽  
Dong Wook Han ◽  
H.H. Kim ◽  
Hee Joong Kim ◽  
In Seop Lee ◽  
...  
Keyword(s):  
Cell Attachment ◽  
Dermal Fibroblast ◽  
Supporting Cell ◽  
Human Dermal Fibroblast ◽  
Dermal Fibroblasts ◽  
Water Soluble ◽  
Seeding Density ◽  
Tetrazolium Salt ◽  
Cell Seeding ◽  
Plga Film

In this study, human dermal fibroblast behaviors onto non-porous PLGA (75:25) films immobilized with 1, 10 and 100 µg/ml collagen (CN) or fibronectin (FN) were investigated according to different cell-seeding densities (1,000, 10,000 and 100,000 cells/ml). Cell attachment and proliferation were assessed using water soluble tetrazolium salt. The results indicated that 1 µg/ml of FN-immobilized PLGA film demonstrated significantly (p < 0.05) superior cellular attachment to the intact PLGA film after 4 hr of incubation. Moreover, the number of attached cells was shown to be directly proportional to that of initially seeded cells. After 48 hr, the cells showed significantly (p < 0.05) higher proliferation onto 1 or 10 µg/ml of FN-immobilized PLGA films than onto other PLGA films, regardless of the initial cell-seeding density. In terms of CN-immobilization, cell proliferation was appreciably increased but it was relatively lower than FN-immobilization. These results suggested that ECM-immobilization can enhance the cell affinity of hydrophobic scaffolds and be used to potential applications for tissue engineering by supporting cell growth.

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