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Heparinoids Danaparoid and Sulodexide as clinically used drugs.
Prog Mol Biol Transl Sci 2019; 163:55-74PM

Abstract

Heparin is the first glycosaminoglycan ever identified. All the heparin-like glycosaminoglycans that are also isolated from animal tissues or any polysaccharides that mimic the biological activities of heparin are called heparinoids. Heparin is the mostly sulfated glycosaminoglycan made by mast cells and an essential anticoagulant drug in modern medicine. Heparin inhibits both thrombin generation and thrombin activity, releases tissue factor pathway inhibitor, and possesses anti-inflammatory, anti-viral, anti-angiogenesis, anti-neoplastic, and anti-metastatic properties though high affinity interactions with a variety of proteins in the blood circulation. The multi-pharmacological effects of heparin are both sequence- and sulfation degree dependent. Less sulfated heparinoids have been indicated to have more physiological functions than heparin. Since the anticoagulant heparin is associated with severe side effects, such as bleeding and heparin-induced thrombocytopenia and thrombosis, it is expected that the less sulfated heparinoids might serve as alternative drugs for patients who cannot use heparin. The crude heparin isolated from animal tissues contains ~50% heparin and ~50% less sulfated heparinoids. Indeed, the less sulfated waste heparinoids 1 during heparin production is chemically degraded and developed into the clinical drug Danaparoid and the more sulfated waste heparinoids 2 during heparin production is chemically degraded and developed into the clinical drug Sulodexide. Moreover, clinical studies indicate that Danaparoid and Sulodexide have the expected pharmacological activities. We will provide an update on the chemical characteristics and clinical use of the heparinoids Danaparoid and Sulodexide. In addition, the potential clinical applications of Danaparoid and Sulodexide in other therapeutic area will also be discussed.

Authors+Show Affiliations

Systems Biology and Medicine Center for Complex Diseases, Affiliated Hospital of Qingdao University, Qingdao, China. Electronic address: douhuaiqian@hotmail.com.Department of Pediatrics, Affiliated Hospital of Qingdao University, Qingdao, People's Republic of China.Department of Ophthalmology, Affiliated Hospital of Qingdao University, Qingdao, China.Systems Biology and Medicine Center for Complex Diseases, Affiliated Hospital of Qingdao University, Qingdao, China. Electronic address: zhanglj@qduhospital.cn.

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

31030761

Citation

Dou, Huaiqian, et al. "Heparinoids Danaparoid and Sulodexide as Clinically Used Drugs." Progress in Molecular Biology and Translational Science, vol. 163, 2019, pp. 55-74.
Dou H, Song A, Jia S, et al. Heparinoids Danaparoid and Sulodexide as clinically used drugs. Prog Mol Biol Transl Sci. 2019;163:55-74.
Dou, H., Song, A., Jia, S., & Zhang, L. (2019). Heparinoids Danaparoid and Sulodexide as clinically used drugs. Progress in Molecular Biology and Translational Science, 163, pp. 55-74. doi:10.1016/bs.pmbts.2019.02.005.
Dou H, et al. Heparinoids Danaparoid and Sulodexide as Clinically Used Drugs. Prog Mol Biol Transl Sci. 2019;163:55-74. PubMed PMID: 31030761.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Heparinoids Danaparoid and Sulodexide as clinically used drugs. AU - Dou,Huaiqian, AU - Song,Aiqin, AU - Jia,Shaoyou, AU - Zhang,Lijuan, Y1 - 2019/03/21/ PY - 2019/4/30/entrez PY - 2019/4/30/pubmed PY - 2019/4/30/medline KW - Anticoagulation KW - Chemical degradation KW - Danaparoid KW - Factor Xa KW - Heparin KW - Heparinoid KW - Sulodexide KW - Thrombin SP - 55 EP - 74 JF - Progress in molecular biology and translational science JO - Prog Mol Biol Transl Sci VL - 163 N2 - Heparin is the first glycosaminoglycan ever identified. All the heparin-like glycosaminoglycans that are also isolated from animal tissues or any polysaccharides that mimic the biological activities of heparin are called heparinoids. Heparin is the mostly sulfated glycosaminoglycan made by mast cells and an essential anticoagulant drug in modern medicine. Heparin inhibits both thrombin generation and thrombin activity, releases tissue factor pathway inhibitor, and possesses anti-inflammatory, anti-viral, anti-angiogenesis, anti-neoplastic, and anti-metastatic properties though high affinity interactions with a variety of proteins in the blood circulation. The multi-pharmacological effects of heparin are both sequence- and sulfation degree dependent. Less sulfated heparinoids have been indicated to have more physiological functions than heparin. Since the anticoagulant heparin is associated with severe side effects, such as bleeding and heparin-induced thrombocytopenia and thrombosis, it is expected that the less sulfated heparinoids might serve as alternative drugs for patients who cannot use heparin. The crude heparin isolated from animal tissues contains ~50% heparin and ~50% less sulfated heparinoids. Indeed, the less sulfated waste heparinoids 1 during heparin production is chemically degraded and developed into the clinical drug Danaparoid and the more sulfated waste heparinoids 2 during heparin production is chemically degraded and developed into the clinical drug Sulodexide. Moreover, clinical studies indicate that Danaparoid and Sulodexide have the expected pharmacological activities. We will provide an update on the chemical characteristics and clinical use of the heparinoids Danaparoid and Sulodexide. In addition, the potential clinical applications of Danaparoid and Sulodexide in other therapeutic area will also be discussed. SN - 1878-0814 UR - https://www.unboundmedicine.com/medline/citation/31030761/Heparinoids_Danaparoid_and_Sulodexide_as_clinically_used_drugs L2 - https://linkinghub.elsevier.com/retrieve/pii/S1877-1173(19)30026-2 DB - PRIME DP - Unbound Medicine ER -