Esterification of the free carboxylic group from the lutidinic acid ligand as a tool to improve the cytotoxicity of Ru(ii) complexes

2019 ◽  
Vol 6 (2) ◽  
pp. 376-390 ◽  
Author(s):  
João Honorato ◽  
Legna Colina-Vegas ◽  
Rodrigo S. Correa ◽  
Adriana P. M. Guedes ◽  
Marcelo Miyata ◽  
...  

The esterification of the free carboxyl group in ruthenium complexes improves the complex interactions with biomolecules, lipophilicity, and cellular uptake, making them more selective against tumor cells than cisplatin.

Molecules ◽  
2021 ◽  
Vol 26 (15) ◽  
pp. 4528
Author(s):  
Katarína Šuchová ◽  
Vladimír Puchart ◽  
Nikolaj Spodsberg ◽  
Kristian B. R. Mørkeberg Krogh ◽  
Peter Biely

Catalytic properties of GH30 xylanases belonging to subfamilies 7 and 8 were compared on glucuronoxylan, modified glucuronoxylans, arabinoxylan, rhodymenan, and xylotetraose. Most of the tested bacterial GH30-8 enzymes are specific glucuronoxylanases (EC 3.2.1.136) requiring for action the presence of free carboxyl group of MeGlcA side residues. These enzymes were not active on arabinoxylan, rhodymenan and xylotetraose, and conversion of MeGlcA to its methyl ester or its reduction to MeGlc led to a remarkable drop in their specific activity. However, some GH30-8 members are nonspecific xylanases effectively hydrolyzing all tested substrates. In terms of catalytic activities, the GH30-7 subfamily is much more diverse. In addition to specific glucuronoxylanases, the GH30-7 subfamily contains nonspecific endoxylanases and predominantly exo-acting enzymes. The activity of GH30-7 specific glucuronoxylanases also depend on the presence of the MeGlcA carboxyl, but not so strictly as in bacterial enzymes. The modification of the carboxyl group of glucuronoxylan had only weak effect on the action of predominantly exo-acting enzymes, as well as nonspecific xylanases. Rhodymenan and xylotetraose were the best substrates for exo-acting enzymes, while arabinoxylan represented hardly degradable substrate for almost all tested GH30-7 enzymes. The results expand current knowledge on the catalytic properties of this relatively novel group of xylanases.


2008 ◽  
Vol 1780 (4) ◽  
pp. 673-679 ◽  
Author(s):  
A. Kunwar ◽  
A. Barik ◽  
B. Mishra ◽  
K. Rathinasamy ◽  
R. Pandey ◽  
...  
Keyword(s):  

2014 ◽  
Vol 72 (4) ◽  
pp. 473 ◽  
Author(s):  
Ying Liu ◽  
Xiaoman Chen ◽  
Langqi Zhang ◽  
Dongdong Sun ◽  
Yanhui Zhou ◽  
...  

ChemInform ◽  
2005 ◽  
Vol 36 (8) ◽  
Author(s):  
E. E. Shalygina ◽  
M. Yu. Solovyov ◽  
K. V. Balakin ◽  
S. A. Ivanovskii ◽  
M. V. Dorogov
Keyword(s):  

RSC Advances ◽  
2015 ◽  
Vol 5 (29) ◽  
pp. 22957-22964 ◽  
Author(s):  
Xingang Guan ◽  
Xiuli Hu ◽  
Zhihong Li ◽  
Hong Zhang ◽  
Zhigang Xie

A biodegradable polymeric micelle with cRGD targeting and charge-conversional moiety could enhance the cellular uptake of pharmaceuticals and result in high cytotoxicity to tumor cells.


2020 ◽  
Vol 203 ◽  
pp. 110922
Author(s):  
Seungjo Park ◽  
Jessica L. Gray ◽  
Sarah D. Altman ◽  
Angela R. Hairston ◽  
Brianna T. Beswick ◽  
...  

Pharmaceutics ◽  
2020 ◽  
Vol 12 (4) ◽  
pp. 372 ◽  
Author(s):  
Jaeduk Park ◽  
Hyuk Lee ◽  
Yu Seok Youn ◽  
Kyung Taek Oh ◽  
Eun Seong Lee

In this study, we fabricated tumor-homing pH-sensitive extracellular vesicles for efficient tumor treatment. These vesicles were prepared using extracellular vesicles (EVs; BTEVs extracted from BT-474 tumor cells or SKEVs extracted from SK-N-MC tumor cells), hyaluronic acid grafted with 3-(diethylamino)propylamine (HDEA), and doxorubicin (DOX, as a model antitumor drug). Consequently, HDEA/DOX anchored EVs (HDEA@EVs) can interact with origin tumor cells owing to EVs’ homing ability to origin cells. Therefore, EV blends of HDEA@BTEVs and HDEA@SKEVs demonstrate highly increased cellular uptake in both BT-474 and SK-N-MC cells: HDEA@BTEVs for BT-474 tumor cells and HDEA@SKEVs for SK-N-MC tumor cells. Furthermore, the hydrophobic HDEA present in HDEA@EVs at pH 7.4 can switch to hydrophilic HDEA at pH 6.5 as a result of acidic pH-induced protonation of 3-(diethylamino)propylamine (DEAP) moieties, resulting in an acidic pH-activated EVs’ disruption, accelerated release of encapsulated DOX molecules, and highly increased cell cytotoxicity. However, EV blends containing pH-insensitive HA grafted with deoxycholic acid (HDOC) (HDOC@BTEVs and HDOC@SKEVs) showed less cell cytotoxicity for both BT-474 and SK-N-MC tumor cells, because they did not act on EVs’ disruption and the resulting DOX release. Consequently, the use of these tumor-homing pH-sensitive EV blends may result in effective targeted therapies for various tumor cells.


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