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Please use this identifier to cite or link to this item:
http://140.112.115.32:8080/ir/handle/987654321/2795
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| Title: | Development of Benzimidazole Derivatives as Novel Anti-platelet Drugs |
| Authors: | Wei-Cheng Yao;Lan-Ting Yuan;Wen-Bin Yang;Chih-Hsuan Hsia;Li-Ting Huang;Tzu-Yin Lee;Joen-Rong Sheu;Wan-Jung Lu;Thanasekaran Jayakumar;Ray-Jade Chen |
| Contributors: | 視光學系 |
| Keywords: | Platelets;benzimidazole;thrombin;ADP;epinephrine;P-selectin;clot retraction;MAPKs. |
| Date: | 2017-08-01 |
| Issue Date: | 2025-08-11 14:43:59 (UTC+8) |
| Abstract: | Background: Benzimidazoles are privileged biomolecules which form an integral part of vitamin B12 and have been attracting numerous researchers all over the world to assess their potential therapeutic significance.
Objectives: The comparative in vitro antiplatelet activity of newly synthesized benzimidazole derivatives, M3BIM, C2BIM, and L2BIM in thrombin, adenosine diphosphate (ADP) and epinephrineinduced washed human platelets was investigated.
Method: Reversed-phase silica gel column chromatography, Aggregometry, Flow cytometry and Immunoblotting were used in this study.
Results: M3BIM exhibited a concentration (25-100 µM) dependent inhibitory effect on platelet aggregation induced by thrombin (0.01 U/mL) in washed human platelets and by epinephrine (10 µM) only at a maximum concentration of 500 µM in platelet-rich plasma (PRP); however, C2BIM and L2BIM had no response even at 500 µM against thrombin and 1mM against epinephrine-induced platelet aggregation. Moreover, all these three compounds were not inhibited platelet aggregation induced by ADP (20 µM). Additionally, these compounds showed no effects in thrombin-induced P-selectin expression and αIIbβ3 activation, as evidenced by flow cytometry and clot reaction assays, respectively. Besides, M3BIM (100 µM) significantly abolished thrombin-induced Akt and mitogen-activated protein kinases (MAPKs) phosphorylation; whereas 200 µM C2BIM and L2BIM were not effective on these proteins.
Conclusion: This study affords confirmation for the inhibitory effect of M3BIM in a low dose thrombin and epinephrine-induced platelet aggregation in vitro compared to other imidazole derivatives, C2BIM and L2BIM. These outcomes may recommend that M3BIM can be appraised as a prospective benzeimidazole compound for the treatment of thrombin -induced platelet defect and its related diseases. |
| Relation: | Current Pharmaceutical Biotechnology, 18(7), 594-605. https://doi.org/10.2174/1389201018666170821113430 |
| Appears in Collections: | [視光學系] 期刊論文
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