Efficacy of Heparinoid PSS in Treating Cardiovascular Diseases and Beyond—A Review of 27 Years Clinical Experiences in China

Zeng, Yangyang; Yang, Dongyuan; Qiu, Peiju; Han, Zhangrun; Zeng, Pengjiao; He, Yong; Guo, Zhihua; Xu, Lingling; Cui, Yidi; Zhou, Zijing; Zhang, Meng; Hao, Jiejie; Zhang, Lijuan

doi:10.1177/1076029614551822

Cited by 24 publications

(13 citation statements)

References 6 publications

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“…Haemostatic efficacy of calcium alginate through platelets activation and thrombin generation was also displayed [156][157][158][159] enabling polymer application in wound dressings [30][31][32][33]. Furthermore, sulfated ALG derivative propylene glycol alginate sodium sulfate (PSS) is the first oral heparinoid approved by Chinese Food and Drug Administration and has been used as an anticoagulant drug for over 30 years [160].…”

Section: Alg Biological Activity and Application In Pharmaceutical Prmentioning

confidence: 99%

Alginate: Current Use and Future Perspectives in Pharmaceutical and Biomedical Applications

Szekalska

Puciłowska

Szymańska

et al. 2016

International Journal of Polymer Science

436

250

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Over the last decades, alginates, natural multifunctional polymers, have increasingly drawn attention as attractive compounds in the biomedical and pharmaceutical fields due to their unique physicochemical properties and versatile biological activities. The focus of the paper is to describe biological and pharmacological activity of alginates and to discuss the present use and future possibilities of alginates as a tool in drug formulation. The recent technological advancements with using alginates, issues related to alginates suitability as matrix for three-dimensional tissue cultures, adjuvants of antibiotics, and antiviral agents in cell transplantation in diabetes or neurodegenerative diseases treatment, and an update on the antimicrobial and antiviral therapy of the alginate based drugs are also highlighted.

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Section: Alg Biological Activity and Application In Pharmaceutical Prmentioning

confidence: 99%

Alginate: Current Use and Future Perspectives in Pharmaceutical and Biomedical Applications

Szekalska

Puciłowska

Szymańska

et al. 2016

International Journal of Polymer Science

436

250

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“…A clinically relevant sulfated derivative is the propylene glycol alg sodium sulfate (PSS), which was the first oral heparinoid drug to be approved in China in 1987, and it has been used since then in China both orally and intravenously for the treatment of cardiovascular diseases [53]. PSS derivatives with various sulfur content, molar mass, and G:M ratios were intensively investigated for their P-, L-, and E-selectin mediated binding to tumor cells [48].…”

Section: Starting Polymermentioning

confidence: 99%

Strategies to Functionalize the Anionic Biopolymer Na-Alginate without Restricting Its Polyelectrolyte Properties

2020

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The natural anionic polyelectrolyte alginate and its derivatives are of particular interest for pharmaceutical and biomedical applications. Most interesting for such applications are alginate hydrogels, which can be processed into various shapes, self-standing or at surfaces. Increasing efforts are underway to functionalize the alginate macromolecules prior to hydrogel formation in order to overcome the shortcomings of purely ionically cross-linked alginate hydrogels that are hindering the progress of several sophisticated biomedical applications. Particularly promising are derivatives of alginate, which allow simultaneous ionic and covalent cross-linking to improve the physical properties and add biological activity to the hydrogel. This review will report recent progress in alginate modification and functionalization with special focus on synthesis procedures, which completely conserve the ionic functionality of the carboxyl groups along the backbone. Recent advances in analytical techniques and instrumentation supported the goal-directed modification and functionalization.Polymers 2020, 12, 919 2 of 23 Physicochemical and Polyelectrolyte Characteristics of AlginateThe composition, internal structure, and molar mass of the alg backbone govern the functional properties [9]. The solubility of alg in water depends on the pH value and the type of the counterions of the carboxyl groups. At pH < 3, both the M-and G-structures will precipitate as alginic acid. However, alternating M-and G-structures precipitate at lower pH values compared to the alg containing Polymers 2020, 12, 919 3 of 23 more homogeneous block structures. Neutralization of the alginic acid occurs at pH > 4, where it is converted into its corresponding salt [10]. Na-alg is an example of a water-soluble alg.Na-alg behaves in aqueous solution as a typical linear homogeneously charged polyelectrolyte. The chain conformation and consequently the solution viscosity strongly depend on the ionic strength, i.e., on both the alg concentration and the simultaneous presence of low molar mass salt. The intramolecular electrostatic repulsion between the neighboring negatively charged carboxyl groups of each monomer unit forces alg molecules into an extended random coil conformation in aqueous solution [11]. This results in highly viscous solutions even at relatively low alg concentration. The dynamic viscosity increases exponentially with the molar mass, while the intrinsic flexibility of the alg chains in solution increases in the order GG < MM < MG [12]. On the other hand, the selectivity for cation-binding and gel-forming properties strongly depends on the composition and sequence. Divalent cations preferably bind to the G-blocks. The ability to form ionotropic gels is based on this selective binding of cations. Mixing solutions of Na-alg with solutions of cationic polyelectrolytes yields precipitates of polyelectrolyte complexes.The rheological behavior of Na-alg solutions is important for a number of technologies and depends on both the concentration and th...

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“…Propylene glycol alginate sodium sulfate (PSS) is a heparin-like drug that was approved by the China Food and Drug Administration (CFDA) over 30 years ago to treat hyperlipidemia and ischemic cardio-cerebrovascular diseases [14]. PSS is obtained from alginate polysaccharide of Laminaria with multiple chemical modifications.…”

Section: Introductionmentioning

confidence: 99%

The Inhibitory Effect of Propylene Glycol Alginate Sodium Sulfate on Fibroblast Growth Factor 2-Mediated Angiogenesis and Invasion in Murine Melanoma B16-F10 Cells In Vitro

Qiu

et al. 2019

Marine Drugs

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Melanoma is one of the most malignant and aggressive types of cancer worldwide. Fibroblast growth factor 2 (FGF2) is one of the critical regulators of melanoma angiogenesis and metastasis; thus, it might be an effective anti-cancer strategy to explore FGF2-targeting drug candidates from existing drugs. In this study, we evaluate the effect of the marine drug propylene glycol alginate sodium sulfate (PSS) on FGF2-mediated angiogenesis and invasion. The data shows that FGF2 selectively bound to PSS with high affinity. PSS inhibited FGF2-mediated angiogenesis in a rat aortic ring model and suppressed FGF2-mediated invasion, but not the migration of murine melanoma B16-F10 cells. The further mechanism study indicates that PSS decreased the expression of activated matrix metalloproteinase 2 (MMP-2) and matrix metalloproteinase 9 (MMP-9), and also suppressed their activity. In addition, PSS was found to decrease the level of Vimentin in B16-F10 cells, which is known to participate in the epithelial–mesenchymal transition. Notably, PSS did not elicit any changes in cancer cell viability. Based on the results above, we conclude that PSS might be a potential drug to regulate the tumor microenvironment in order to facilitate the recovery of melanoma patients.

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Efficacy of Heparinoid PSS in Treating Cardiovascular Diseases and Beyond—A Review of 27 Years Clinical Experiences in China

Cited by 24 publications

References 6 publications

Alginate: Current Use and Future Perspectives in Pharmaceutical and Biomedical Applications

Alginate: Current Use and Future Perspectives in Pharmaceutical and Biomedical Applications

Strategies to Functionalize the Anionic Biopolymer Na-Alginate without Restricting Its Polyelectrolyte Properties

The Inhibitory Effect of Propylene Glycol Alginate Sodium Sulfate on Fibroblast Growth Factor 2-Mediated Angiogenesis and Invasion in Murine Melanoma B16-F10 Cells In Vitro

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