Purification and Characterization of a Novel Antiplatelet Peptide from Deinagkistrodon acutus Venom
Animal venoms are considered as one of the most important sources for drug development. Deinagkistrodon acutus is famous for its toxicity to the human hematological system and envenomed patients develop a coagulation disorder with the symptoms of hemorrhage and microthrombi formation. The purpose of...
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MDPI AG
2018-08-01
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| Series: | Toxins |
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| Online Access: | http://www.mdpi.com/2072-6651/10/8/332 |
| _version_ | 1798024374865887232 |
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| author | Yi Kong Qing Sun Qi Zhao Yaqiong Zhang |
| author_facet | Yi Kong Qing Sun Qi Zhao Yaqiong Zhang |
| author_sort | Yi Kong |
| collection | DOAJ |
| description | Animal venoms are considered as one of the most important sources for drug development. Deinagkistrodon acutus is famous for its toxicity to the human hematological system and envenomed patients develop a coagulation disorder with the symptoms of hemorrhage and microthrombi formation. The purpose of this study was to separate antiplatelet peptides from D. acutus venom using a combination of an ultrafiltration technique and reversed-phase high performance liquid chromatography (HPLC), which was guided by monitoring antiplatelet aggregation bioactivity. A novel octa-peptide named DAA-8 was found. This peptide inhibited protease-activated receptor1 (PAR-1) agonist (SFLLRN-NH2) induced platelet aggregation and it also inhibited platelet aggregation induced by thrombin, ADP, and collagen. Furthermore, DAA-8 showed significant antithrombotic activity and resulted in a slightly increased bleeding risk in vivo. This is the first report of a peptide derived from snake venom, which inhibited PAR-1 agonist-induced platelet aggregation. This peptide may provide a template to design a new PAR-1 inhibitor. |
| first_indexed | 2024-04-11T18:01:26Z |
| format | Article |
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| issn | 2072-6651 |
| language | English |
| last_indexed | 2024-04-11T18:01:26Z |
| publishDate | 2018-08-01 |
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| spelling | doaj.art-df5b04011d4148899f85932ab72e6fca2022-12-22T04:10:27ZengMDPI AGToxins2072-66512018-08-0110833210.3390/toxins10080332toxins10080332Purification and Characterization of a Novel Antiplatelet Peptide from Deinagkistrodon acutus VenomYi Kong0Qing Sun1Qi Zhao2Yaqiong Zhang3School of Life Science and Technology, China Pharmaceutical University, 24 Tong Jia Street, Nanjing 210009, ChinaSchool of Life Science and Technology, China Pharmaceutical University, 24 Tong Jia Street, Nanjing 210009, ChinaSchool of Life Science and Technology, China Pharmaceutical University, 24 Tong Jia Street, Nanjing 210009, ChinaSchool of Life Science and Technology, China Pharmaceutical University, 24 Tong Jia Street, Nanjing 210009, ChinaAnimal venoms are considered as one of the most important sources for drug development. Deinagkistrodon acutus is famous for its toxicity to the human hematological system and envenomed patients develop a coagulation disorder with the symptoms of hemorrhage and microthrombi formation. The purpose of this study was to separate antiplatelet peptides from D. acutus venom using a combination of an ultrafiltration technique and reversed-phase high performance liquid chromatography (HPLC), which was guided by monitoring antiplatelet aggregation bioactivity. A novel octa-peptide named DAA-8 was found. This peptide inhibited protease-activated receptor1 (PAR-1) agonist (SFLLRN-NH2) induced platelet aggregation and it also inhibited platelet aggregation induced by thrombin, ADP, and collagen. Furthermore, DAA-8 showed significant antithrombotic activity and resulted in a slightly increased bleeding risk in vivo. This is the first report of a peptide derived from snake venom, which inhibited PAR-1 agonist-induced platelet aggregation. This peptide may provide a template to design a new PAR-1 inhibitor.http://www.mdpi.com/2072-6651/10/8/332Deinagkistrodon acutusDAA-8antiplateletPAR-1 |
| spellingShingle | Yi Kong Qing Sun Qi Zhao Yaqiong Zhang Purification and Characterization of a Novel Antiplatelet Peptide from Deinagkistrodon acutus Venom Toxins Deinagkistrodon acutus DAA-8 antiplatelet PAR-1 |
| title | Purification and Characterization of a Novel Antiplatelet Peptide from Deinagkistrodon acutus Venom |
| title_full | Purification and Characterization of a Novel Antiplatelet Peptide from Deinagkistrodon acutus Venom |
| title_fullStr | Purification and Characterization of a Novel Antiplatelet Peptide from Deinagkistrodon acutus Venom |
| title_full_unstemmed | Purification and Characterization of a Novel Antiplatelet Peptide from Deinagkistrodon acutus Venom |
| title_short | Purification and Characterization of a Novel Antiplatelet Peptide from Deinagkistrodon acutus Venom |
| title_sort | purification and characterization of a novel antiplatelet peptide from deinagkistrodon acutus venom |
| topic | Deinagkistrodon acutus DAA-8 antiplatelet PAR-1 |
| url | http://www.mdpi.com/2072-6651/10/8/332 |
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