scholarly journals Montivipera bornmuelleri Venom: Inhibitory Effect on Staphylococcus epidermidis and Escherichia coli F1F0-ATPases and Cytotoxicity on HCT116 Cancer Cell Lines

Sci ◽  
2021 ◽  
Vol 3 (3) ◽  
pp. 31
Author(s):  
Milena Kfoury ◽  
Charbel Mouawad ◽  
Mariam Rifi ◽  
Riyad Sadek ◽  
Jean-Marc Sabatier ◽  
...  

In this work, we pursued the biological characterization of the venom of Montivipera bornmuelleri, a viper from the Lebanese mountains. In relation to its antibacterial potential, the inhibitory effect of this venom on the F1F0-ATPase enzymes of Gram-positive Staphylocoocus epidermidis and Gram-negative Escherichia coli bacteria was examined. In order to determine the degree of cytotoxicity of the venom on the HCT116 human colon cancer cell lines, the biological MTT proliferation and cell viability test were implemented. After validation of the enzymatic F1F0-ATPase model by the spectrophotometric method, using quercetin as the reference ligand, results revealed that M. bornmuelleri venom is able to inhibit the activity of the enzyme of these two bacteria with a concentration of the order of 100–150 µg/mL. In addition, a venom concentration of 10 µg/mL was sufficient to kill the totality of HCT116 cell lines cultivated in vitro. These data show that M. bornmuelleri venom is a mixture of diverse molecules presenting activities of interest, and is a potential source to explore in order to discover new drug candidates.

Author(s):  
Milena Kfoury ◽  
Charbel Mouawad ◽  
Mariam Rifi ◽  
Riyad Sadek ◽  
Jean-Marc Sabatier ◽  
...  

In this work, we pursued the biological characterization of the venom of Montivipera born-muelleri, a viper from the Lebanese mountains. In relativity to its antibacterial potential, the in-hibitory effect of this venom on the F1F0-ATPase enzymes of Gram-positive Staphylocoocus epider-midis and Gram-negative Escherichia coli bacteria was examined. In order to determine the de-gree of cytotoxicity of the venom on the HCT116 human colon cancer cell lines, the biological MTT proliferation and cell viability test were implemented. After validation of the enzymatic F1F0-ATPase model by the spectrophotometric method, using quercetin as the reference ligand, re-sults revealed that M. bornmuelleri venom is able to inhibit the activity of the enzyme of these two bacteria with a concentration of the order of 100-150 µg/mL. In addition, a venom concentration of 10 µg/mL was sufficient to kill the totality of HCT116 cell lines cultivated in vitro. These data show that M. bornmuelleri venom is a mixture of diverse molecules presenting activities of interest and is a potential source to explore in order to discover new drug candidates.


2010 ◽  
Vol 62 (8) ◽  
pp. 1007-1016 ◽  
Author(s):  
Weimin Guo ◽  
Lin Nie ◽  
Dayong Wu ◽  
Mitchell L. Wise ◽  
F. William Collins ◽  
...  

2018 ◽  
Vol 18 (8) ◽  
pp. 1156-1162
Author(s):  
Da-You Ma ◽  
Li-Chao Zhang ◽  
Kun-Jian Peng ◽  
Jiang Zeng ◽  
Li-Jun Liu ◽  
...  

Background: The heptaprotective flavonolignan silibinin and dehydrosilibinin have exhibited moderate antiproliferative activities toward many cancer cell lines. Considering of the nontoxic profile of these natural products, chemical modification to enhance the anticancer potentials is promising. Method: A series of 7-O-aminoalkyl-2,3-dehydrosilibinin derivatives were synthesized and evaluated for their antiproliferative activities against several cancer cell lines. Results: A number of the synthesized dehydrosilibinin derivatives exhibited greatly enhanced potency with 50% growth inhibition at low micromolar concentrations. Structure activity study indicated that the distance between N and 7-O on the side chain has a limited influence on the antiproliferative activity, while the presence of a morpholino group decreases the antiproliferative activities dramatically. Flow cytometry based assays on human colon cancer HCT116 cells revealed that 6a and 6c, two of the most potent derivatives, effectively arrested the cell cycle in the G2 phase and stimulated cell apoptosis. Conclusion: Our findings suggest that attaching an appropriate tertiary amino alkyl side chain through 7-Oalkylation on 2,3-dehydrosilibinin, would be a viable strategy for the development of silibinin derivatives as anticancer agents.


2005 ◽  
Vol 15 (17) ◽  
pp. 3930-3933 ◽  
Author(s):  
Rosaria Ottanà ◽  
Stefania Carotti ◽  
Rosanna Maccari ◽  
Ida Landini ◽  
Giuseppa Chiricosta ◽  
...  

2012 ◽  
Vol 12 (6) ◽  
pp. 8062-8070 ◽  
Author(s):  
FENG-QI FANG ◽  
HUI-SHU GUO ◽  
JIE ZHANG ◽  
LI-YING BAN ◽  
JI-WEI LIU ◽  
...  

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