Water Soluble, Core-Modified Porphyrins. 3. Synthesis, Photophysical Properties, and in Vitro Studies of Photosensitization, Uptake, and Localization with Carboxylic Acid-Substituted Derivatives

2003 ◽  
Vol 46 (17) ◽  
pp. 3734-3747 ◽  
Author(s):  
Youngjae You ◽  
Scott L. Gibson ◽  
Russell Hilf ◽  
Sherry R. Davies ◽  
Allan R. Oseroff ◽  
...  
RSC Advances ◽  
2018 ◽  
Vol 8 (31) ◽  
pp. 17224-17236 ◽  
Author(s):  
Anastasia I. Solomatina ◽  
Shih-Hao Su ◽  
Maria M. Lukina ◽  
Varvara V. Dudenkova ◽  
Vladislav I. Shcheslavskiy ◽  
...  

Novel water-soluble iridium complexes with sulfonated diphosphine allow in vitro and in vivo lifetime hypoxia imaging.


ACS Omega ◽  
2019 ◽  
Vol 4 (1) ◽  
pp. 1685-1689 ◽  
Author(s):  
Martin Fries ◽  
Meike Mertens ◽  
Nico Teske ◽  
Markus Kipp ◽  
Cordian Beyer ◽  
...  

2016 ◽  
Vol 441 ◽  
pp. 42-49 ◽  
Author(s):  
Kaplan Kirakci ◽  
Pavel Kubát ◽  
Monika Kučeráková ◽  
Václav Šícha ◽  
Helena Gbelcová ◽  
...  

2021 ◽  
Vol 22 (23) ◽  
pp. 13092
Author(s):  
Michał Abram ◽  
Marcin Jakubiec ◽  
Anna Rapacz ◽  
Szczepan Mogilski ◽  
Gniewomir Latacz ◽  
...  

We report herein a series of water-soluble analogues of previously described anticonvulsants and their detailed in vivo and in vitro characterization. The majority of these compounds demonstrated broad-spectrum anticonvulsant properties in animal seizure models, including the maximal electroshock (MES) test, the pentylenetetrazole-induced seizure model (scPTZ), and the psychomotor 6 Hz (32 mA) seizure model in mice. Compound 14 showed the most robust anticonvulsant activity (ED50 MES = 49.6 mg/kg, ED50 6 Hz (32 mA) = 31.3 mg/kg, ED50scPTZ = 67.4 mg/kg). Notably, it was also effective in the 6 Hz (44 mA) model of drug-resistant epilepsy (ED50 = 63.2 mg/kg). Apart from favorable anticonvulsant properties, compound 14 revealed a high efficacy against pain responses in the formalin-induced tonic pain, the capsaicin-induced neurogenic pain, as well as in the oxaliplatin-induced neuropathic pain in mice. Moreover, compound 14 showed distinct anti-inflammatory activity in the model of carrageenan-induced aseptic inflammation. The mechanism of action of compound 14 is likely complex and may result from the inhibition of peripheral and central sodium and calcium currents, as well as the TRPV1 receptor antagonism as observed in the in vitro studies. This lead compound also revealed beneficial in vitro ADME-Tox properties and an in vivo pharmacokinetic profile, making it a potential candidate for future preclinical development. Interestingly, the in vitro studies also showed a favorable induction effect of compound 14 on the viability of neuroblastoma SH-SY5Y cells.


2020 ◽  
Vol 19 (2) ◽  
pp. 193-206 ◽  
Author(s):  
K. T. Kazantzis ◽  
K. Koutsonikoli ◽  
B. Mavroidi ◽  
M. Zachariadis ◽  
P. Alexiou ◽  
...  

Increased absorption maximum for the dimethylaminocurcumin with strong PD effect on prostate cancer cells; Intense PD effect of curcumin III on prostate cancer cells; Exciting biphasic PD response by curcumin I and cinnamaldehyde-derived curcumin.


2011 ◽  
Vol 40 (16) ◽  
pp. 4067-4079 ◽  
Author(s):  
Sinem Tuncel ◽  
Fabienne Dumoulin ◽  
Jürgen Gailer ◽  
Melani Sooriyaarachchi ◽  
Devrim Atilla ◽  
...  

2021 ◽  
Vol 22 (6) ◽  
pp. 3255
Author(s):  
Amina Ben Mihoub ◽  
Samir Acherar ◽  
Céline Frochot ◽  
Catherine Malaplate ◽  
Frances T. Yen ◽  
...  

Self-aggregation of Curcumin (Cur) in aqueous biological environment decreases its bioavailability and in vivo therapeutic efficacy, which hampers its clinical use as candidate for reducing risk of neurodegenerative diseases. Here, we focused on the design of new Cur- β-Cyclodextrin nanoconjugates to improve the solubility and reduce cell toxicity of Cur. In this study, we described the synthesis, structural characterization, photophysical properties and neuron cell toxicity of two new water soluble β-CD/Cur nanoconjugates as new strategy for reducing risks of neurodegenerative diseases. Cur was coupled to one or two β-CD molecules via triazole rings using CuAAC click chemistry strategy to yield β-CD@Cur and (β-CD)2@Cur nanoconjugates, respectively. The synthesized nanoconjugates were found to be able to self-assemble in aqueous condition and form nano-aggregates of an average diameter size of around 35 and 120 nm for β-CD@Cur and (β-CD)2@Cur, respectively. The photophysical properties, water solubility and cell toxicity on rat embryonic cortical neurons of the designed nanoconjugates were investigated and compared to that of Cur alone. The findings revealed that both new nanoconjugates displayed better water solubility and in vitro biocompatibility than Cur alone, thus making it possible to envisage their use as future nano-systems for the prevention or risk reduction of neurodegenerative diseases.


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