The evaluation of acute toxicity,antimicrobial activity of 1‐phenyl‐5‐p‐tolyl‐1H‐1, 2, 3‐triazole,and binding to human serum albumin |
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| Authors: | Hong‐Ye Duan Jian‐Ling Li Lu‐Yong Wu Huo‐Ming Shu Yu‐Xue Chen Guo‐Hua Ding Run‐Cong Dong Hong‐Zong Si Xia Zhong Wen‐Ying He |
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| Affiliation: | 1. Key Laboratory of Tropical Medicinal Plant Chemistry of Ministry of Education, Hainan Normal University, Haikou, People's Republic of China;2. Hainan College of Economics and Business, Haikou, People's Republic of China;3. Research Center for Drug Safety Evaluation of Hainan Province, Haikou, People's Republic of China;4. Institute for Computational Science and Engineering, Qingdao University, Qingdao, People's Republic of China;5. School of Pharmaceutical Science, Hainan Medical University, Haikou, People's Republic of China |
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| Abstract: | 1‐Phenyl‐5‐p‐tolyl‐1H‐1, 2, 3‐triazole (PPTA) was a synthesized compound. The result of acute toxicities to mice of PPTA by intragastric administration indicated that PPTA did not produce any significant acute toxic effect on Kunming strain mice. It exhibited the various potent inhibitory activities against two kinds of bananas pathogenic bacteria, black sigatoka and freckle, when compared with that of control drugs and the inhibitory rates were up to 64.14% and 43.46%, respectively, with the same concentration of 7.06 mM. The interaction of PPTA with human serum albumin (HSA) was studied using fluorescence polarization, absorption spectra, 3D fluorescence, and synchronous spectra in combination with quantum chemistry and molecular modeling. Multiple modes of interaction between PPTA and HSA were suggested to stabilize the PPTA–HSA complex, based on thermodynamic data and molecular modeling. Binding of PPTA to HSA induced perturbation in the microenvironment around HSA as well as secondary structural changes in the protein. |
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| Keywords: | 1‐Phenyl‐5‐p‐tolyl‐1H‐1 2 3‐triazole acute toxicity antimicrobial activities binding human serum albumin |
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