Inhibitory Effect of Triterpenoids from Panax ginseng on Coagulation Factor X

Xiong, Lingxin; Zeng, Qi; Zheng, B. Z.; Li, Zhuo; Wang, Fang; Liu, Jinping; Li, Pingya

doi:10.3390/molecules22040649

Cited by 24 publications

(13 citation statements)

References 25 publications

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“…10 Four drugs have currently received widespread approval by national or supranational medicinal agencies (apixaban, dabigatran, edoxaban, and rivaroxaban; ►Table 1), one agent has currently been approved in the United States but not in Europe or Australia (betrixaban), other compounds are at different stages of clinical evaluation (darexaban, eribaxaban, letaxaban, and nokxaban; ►Table 2), while the development of some other drugs has been discontinued for different reasons (fidexaban, LY517717, odiparcil, otamixaban, TTP889, and ximelagatran; ►Table 3). Preclinical studies based on other natural or synthetic direct FXa inhibitors have been completed with promising results, 63,64 thus paving the way to planning randomized clinical trials for testing their efficacy and safety profiles in vivo. Notably, although most of these new compounds act as direct FXa inhibitors, encouraging evidence is also emerging on some antithrombotic molecules and aptamers targeting intrinsic pathway factors (i.e., FIXa, FXIa, and FXIIa), as recently reviewed elsewhere, [65][66][67] while no additional direct thrombin inhibitors seem to be in the pipeline of the pharmacological industry to the best of our knowledge.…”

Section: Resultsmentioning

confidence: 99%

Current and Emerging Direct Oral Anticoagulants: State-of-the-Art

Lippi

Gosselin

Favaloro

2019

Semin Thromb Hemost

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Anticoagulant drugs comprise a specific subcategory of antithrombotic agents that act to inhibit blood coagulation at various stages, reducing clot development and ultimately lowering the risk of developing new-onset or recurrent thrombosis. Although the long history of anticoagulant drugs has been characteristically shaped by coumarin and heparin derivatives, a new generation of direct oral anticoagulants (DOACs), which specifically inhibit thrombin or activated factor X, combine many advantages of their progenitor drugs, and hence are prepotently revolutionizing the landscape of antithrombotic therapy. Several drugs (apixaban [BMS-562247], dabigatran [BIBR953], edoxaban [DU-1766], rivaroxaban [BAY 59–7939]) have already received widespread approval by national or supranational medicinal agencies. This narrative article provides a state-of-the-art for these and for several other DOACs at different stages of clinical evaluation (betrixaban, darexaban, eribaxaban, letaxaban, nokxaban), and certain others whose development has been discontinued (AZD-0837, fidexaban, LY517717, odiparcil, otamixaban, TTP889, and ximelagatran). What clearly emerges from our analysis is that DOACs sharing very similar mechanisms of action are still characterized by different efficacy and safety profiles. This not only depends on biochemical, biological, and pharmacokinetic characteristics, but also on lack of standardization between different clinical trials in terms of targeted disease, patient recruitment, sample size, duration and endpoints, as well as lack of harmonization around procedures used for drug licensing. These factors contribute to challenging the minds of physicians, who may find difficulty navigating their way through multiple indications, different pharmacological profiles, various side effects, and specific drug-to-drug interactions. Such considerations also burden laboratory professionals, who may face organizational and economic challenges in developing and/or implementing multiple assays to assess the pharmacodynamics (effect on coagulation) or pharmacokinetics (drug levels) of DOACs.

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Section: Resultsmentioning

confidence: 99%

Current and Emerging Direct Oral Anticoagulants: State-of-the-Art

Lippi

Gosselin

Favaloro

2019

Semin Thromb Hemost

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“…For GLIDE docking, the prepared structure of EGF, NOS2, and ligand (Rg3) were imported to the workspace using GLIDE v6.7 from Schrödinger Suite [17], [18], [19]. Extra precision (XP) docking was carried out, and the parameters of scaling factor and partial charge cutoff were set at the default values 0.80 and 0.15, respectively [20]. Figures of the docking results were subsequently prepared using PyMOL (Schrödinger).…”

Section: Methodsmentioning

confidence: 99%

Evaluation of the gastroprotective effects of 20 (S)-ginsenoside Rg3 on gastric ulcer models in mice

Zhang

Liu

Wang

et al. 2019

Journal of Ginseng Research

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BackgroundGastric ulcer (GU) is a common gastrointestinal disease that can be induced by many factors. Finding an effective treatment method that contains fewer side effects is important. 20 (S)-ginsenoside Rg3 is a kind of protopanaxadiol and has shown superior antiinflammatory and antioxidant effects in many studies, especially cancer studies. In this study, we examined the treatment efficacy of 20 (S)-ginsenoside Rg3 on GU.MethodsThree kinds of GU models, including an alcohol GU model, a pylorus-ligated GU model, and an acetic acid GU model, were used. Mouse endothelin-1 (ET-1) and nitric oxide (NO) levels in blood and epidermal growth factor (EGF), superoxide dismutase, and NO levels in gastric mucosa were evaluated. Hematoxylin and eosin staining of gastric mucosa and immunohistochemical staining of ET-1, inducible nitric oxide synthase (NOS2), and epidermal growth factor receptors were studied. Ulcer index (UI) scores and UI ratios were also analyzed to demonstrate the GU conditions in different groups. Furthermore, Glide XP from Schrödinger was used for molecular docking to clarify the interactions between 20 (S)-ginsenoside Rg3 and EGF and NOS2.Results20 (S)-ginsenoside Rg3 significantly decreased the UI scores and UI ratios in all the three GU models, and it demonstrated antiulcer effects by decreasing the ET-1 and NOS2 levels and increasing the NO, superoxide dismutase, EGF, and epidermal growth factor receptor levels. In addition, high-dose 20 (S)-ginsenoside Rg3 showed satisfactory gastric mucosa protection effects.Conclusion20 (S)-ginsenoside Rg3 can inhibit the formation of GU and may be a potential therapeutic agent for GU.

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“…Moreover, Panax ginseng and part of its major functional components (ginsenosides) also have anticoagulation effects as indicated by the delay of human blood clotting time [117]. For instance, chromogenic substrates assay showed ginsenosides Rg2 and Rg3 exhibited anti-FXa activities.…”

Section: Panax Ginsengmentioning

confidence: 99%

Traditional Chinese medicine in the treatment of high incidence diseases in cold areas: the thrombotic diseases

Tang

Liu

Monayo

et al. 2021

Frigid Zone Medicine

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Thrombotic diseases are the leading causes of death worldwide, especially in cold climates. Traditional Chinese medicine (TCM)-based therapies have gained increasing popularity worldwide, but also raised some concerns about its efficacy, safety profile and exact mechanisms. TCM has been traditionally used in the management of thrombosis and convincingly proven effective in modifying thrombosis progression, particularly the platelet function, coagulation system and fibrinolytic system. This review article focuses on TCM regulation of thrombosis with brief discussion on the fundamental aspects and relevant background information for better understanding of the subject. In addition to its antithrombotic effects, we will dive insight into the cellular and molecular mechanisms of TCM as pharmacological regulators of platelet aggregation, coagulation, and fibrinolysis. With increasing awareness and understanding of the benefits and potentials of TCM, TCM products will in no doubt gain its broader applications in the treatment of thrombosis and associated disorders, which in turn will deepen our understanding of its pharmacological and molecular mechanisms. Finally, current review provides a perspective view on the future directions to TCM research on thrombosis.

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Inhibitory Effect of Triterpenoids from Panax ginseng on Coagulation Factor X

Cited by 24 publications

References 25 publications

Current and Emerging Direct Oral Anticoagulants: State-of-the-Art

Current and Emerging Direct Oral Anticoagulants: State-of-the-Art

Evaluation of the gastroprotective effects of 20 (S)-ginsenoside Rg3 on gastric ulcer models in mice

Traditional Chinese medicine in the treatment of high incidence diseases in cold areas: the thrombotic diseases

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