Shahrekord IAU Faculty Members Develop Effective Drug for Gastric Cancer Treatment

Monday, October 28, 2019 - 16:35

Faculty members of Shahrekord Islamic Azad University have developed an effective medicine for gastric cancer treatment.

According to an ISCA report, the result of the research, carried out by Farhang Tirgir in cooperation with Sadegh Farhadian, Behzad Shareghi, Somayeh Reiisi, Neda Gholamian, Lida Momeni and Ehsan Heidari, has been published in the journal of Molecular Liquids.

Based on the research, over the past decades, anti-cancer drugs consist of cytotoxic drugs, have been interested and developed. Despite the great advances in chemotherapy, there is still no certain medical treatment for cancer.

During this investigation, a novel 2,5-diketopiperazine derivative 3(R),6(S)-bis (4-hydroxy phenyl)-piperazine-2,5-dione: (BHPPD) was designed, synthesized, and evaluated. The effects on intestinal protease consist of conformation, activity, and cytotoxic effects on cancer cell lines by the various methods were assessed.

The binding interaction between BHPPD with α-Chymotrypsin (α-Chy) has been described utilizing many spectroscopic and computational approaches. Intrinsic fluorescence analyses exhibited static quenching as the primary quenching mod in α-Chy–BHPPD interaction, which is further confirmed by UV–vis analyses.

Likewise, binding and thermodynamic constants are estimated from temperature dependent fluorescence results. Furthermore, structural alterations of the enzyme upon binding with BHPPD were presented by circular dichroism (CD) analyses. The Molecular docking assessment presented the specific binding microenvironment of BHPPD in α-Chy. Besides with this research, molecular dynamics Simulation is performed to estimate the stability of α-Chy, α-Chy–BHPPD system.

These results showed the vigorous binding affinity of the drug with intestinal protease. MTT analysis of BHPPD represented high cytotoxic effect against AGS cell line compared to normal cell line. Quantitative analysis shows that BHPPD treatment significantly increased the expression of caspase3, 9, and 8 genes and decreased GR expression in AGS cell line.

Researchers hope that the results of this research will be useful for medical science and pharmacy.


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