Synthesis of (3 S ,4 S ,5 S )-trihydroxylpiperidine derivatives as enzyme stabilizers to improve therapeutic enzyme activity in Fabry patient cell lines

2018 ◽  
Vol 144 ◽  
pp. 626-634 ◽  
Author(s):  
Huang-Yi Li ◽  
Jay-Der Lee ◽  
Chiao-Wen Chen ◽  
Ying-Chieh Sun ◽  
Wei-Chieh Cheng
2009 ◽  
Vol 32 (3) ◽  
pp. 424-440 ◽  
Author(s):  
E. R. Benjamin ◽  
J. J. Flanagan ◽  
A. Schilling ◽  
H. H. Chang ◽  
L. Agarwal ◽  
...  

Author(s):  
Aslıhan Kurt-Kızıldoğan ◽  
Çiğdem Otur ◽  
Can Yılmaz ◽  
Sevki Arslan ◽  
Dogukan Mutlu ◽  
...  

Background:: Indoles probably represent one of the most important heterocyclic structures that have been attracting the interest of many scientists in drug discovery. Methods:: Pd-catalyst Sonogashira coupling reactions, MTT Assay, Antioxidant capacity test, Antimicrobial test, GST enzyme activity test. Results and Discussion:: 1-ethyl-2-phenyl-3-(phenylethynyl)-1H-indole had antioxidant and antimicrobial properties. It displayed significant induction in glutathione S-transferases (GST) enzyme activity in human liver cancer cell lines (HepG2), but cytotoxic effect on all tested cancer cell lines could not be observed. Conclusion:: All of these results showed that 1-ethyl-2-phenyl-3-(phenylethynyl)-1H-indole had antioxidant and antimicrobial properties without cytotoxic effect, which could make it a promising active component.


1988 ◽  
Vol 58 (4) ◽  
pp. 437-440 ◽  
Author(s):  
J Carmichael ◽  
JB Mitchell ◽  
N Friedman ◽  
AF Gazdar ◽  
A Russo

1988 ◽  
Vol 7 (7) ◽  
pp. 1965-1972 ◽  
Author(s):  
Z. Yang ◽  
R. S. Accolla ◽  
D. Pious ◽  
B. J. Zegers ◽  
J. L. Strominger

Nutrients ◽  
2020 ◽  
Vol 12 (1) ◽  
pp. 159
Author(s):  
Sonali Nashine ◽  
Anthony B. Nesburn ◽  
Baruch D. Kuppermann ◽  
Maria Cristina Kenney

Resveratrol is a phytoalexin, stilbenoid compound with antioxidant properties attributable to its bioactive trans-resveratrol content. This study characterized the effects of over-the-counter (OTC) resveratrol nutritional supplements and a HPLC-purified resveratrol formulation, in human transmitochondrial age-related macular degeneration (AMD) retinal pigment epithelial (RPE) patient cell lines. These cell lines, which were created by fusing blood platelets obtained from dry and wet AMD patients with mitochondria-deficient (Rho0) ARPE-19 cells, had identical nuclei (derived from ARPE-19 cells) but different mitochondria that were derived from AMD patients. After resveratrol treatment, the levels of cell viability and reactive oxygen species production were measured. Results demonstrated that treatment with different resveratrol formulations improved cell viability and decreased reactive oxygen species generation in each AMD patient cell line. Although further studies are required to establish the cytoprotective potential of resveratrol under different physiological conditions, this novel study established the positive effects of OTC resveratrol supplements in macular degeneration patient cybrid cell lines in vitro.


1994 ◽  
Vol 73 (8) ◽  
pp. 1407-1415 ◽  
Author(s):  
C.Y. Yang ◽  
C.L. Meng

Prostaglandins may inhibit or promote tumor cell replication, depending on the cell system that is investigated. In our laboratory, we have established and characterized four different specific human cancer cell lines. The objectives of this study were to examine and compare the prostaglandin endoperoxide synthase (PG synthase, EC 1.14.99.1) activity of these cell lines by measuring the conversion of arachidonate to 3H-PGE2 and 3H-PGF2α. We found that the oral epidermal carcinoma cell line (OEC-M1) had a moderate degree of PG synthase activity. Enzyme activity could be partially blocked (statistically significant) by the addition of epidermal growth factor (EGF) at 20 ng/mL and almost completely inhibited by platelet-derived growth factor at (PDGF) 20 mU/mL. By contrast, we discovered that the human breast adenocarcinama cell line (BC-M1) did not contain significant PG synthase, and enzyme activity could be significantly activated by the addition of epidermal growth factor at 20 ng/mL and platelet-derived growth factor at 20 mU/mL. We also found that the human stomach adenocarcinoma cell line (SCM-1) had a significant amount of PG synthase activity, and these PG synthase activities were not activated or inhibited by EGF at 20 ng/mL or PDGF at 20 mU/mL. Furthermore, the human fibrosarcoma (FS-Ml) cell line also contained a moderate degree of PG synthase activity, which could be significantly inhibited by PDGF at 20 mU/mL but was not inhibited by EGF at 20 ng/mL. The results suggest that EGF and PDGF may be involved in the regulation of the PG synthase activities of human oral, breast, stomach, and fibrosarcoma cancer cells.


2012 ◽  
Vol 27 (12) ◽  
pp. 855-860 ◽  
Author(s):  
Celestino Prospero de Souza Sobrinho ◽  
Alfredo Gragnani ◽  
Ivan Dunshee Abranches Oliveira Santos ◽  
Andrea Fernandes Oliveira ◽  
Monica Vanucci Nunes Lipay ◽  
...  

PURPOSE: To evaluate telomerase activity and proliferation of HS839.T melanoma cells, subjected to the action of AZT. METHODS: Cells were grown in triplicate, AZT at different concentrations: 50, 100 and 200μM, was added and left for 24 and 48 hours, and its effects were compared with the control group. Telomerase activity was detected by PCR and cell proliferation was evaluated by MTT. RESULTS: After 24 hours, there was no inhibition of cell proliferation or telomerase activity when compared to the control group. After 48 hours, there was a momentary decrease, suggesting that the cell lines used in this study are sensitive to AZT, but quickly recover both the enzyme activity and cell proliferation. CONCLUSION: The action of AZT on the melanoma cells studied, at the concentrations and times tested, did not inhibit telomerase activity nor affect cell proliferation.


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