Bioactive Natural Compounds with Antiplatelet and Anticoagulant Activity and Their Potential Role in the Treatment of Thrombotic Disorders

Lamponi, Stefania

doi:10.3390/life11101095

Cited by 22 publications

(11 citation statements)

References 175 publications

(176 reference statements)

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“…The aqueous extract exhibited a higher clotting time in comparison to the standard warfarin. It has been reported that organosulfur compounds and phenolic contents of garlic extract are responsible for its high anticoagulant effect (56). The one-tailed t-test was performed to statistically analyze the negative control and test sample data to assess the significance level of garlic extract for each concentration of all in vitro assays.…”

Section: Discussionmentioning

confidence: 99%

In vitro and in silico investigation of garlic’s (Allium sativum) bioactivity against 15-lipoxygenase mediated inflammopathies

Khan

Sharif

Salekeen

et al. 2023

J Herbmed Pharmacol

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Introduction: Garlic (Allium sativum) is widely used as a flavor-enhancing dietary ingredient and exhibits a wide spectrum of pharmacological effects. This study aimed to investigate the therapeutic effects of aqueous garlic extract to explore the bioactivity against 15-lipoxygenase (15-LOX) mediated inflammopathies. Methods: In this study, the antioxidant (DPPH free radical scavenging assay and reducing power assay), anti-inflammatory (hypotonicity-induced hemolysis assay and 15-LOX inhibition assay) and anticoagulation (serine protease inhibition assay and prothrombin time assay) effects of the aqueous garlic extract were investigated. Furthermore, in silico molecular docking and dynamic simulation analysis of reported small compounds of garlic against 15-LOX1 and 15-LOX2 were performed to figure out the most efficient phytochemical ligands and validate the anti-inflammatory potential. Results: The DPPH scavenging effect and the reducing power of the extract were found with the IC50 of 213.87 ± 1.49 μgmL-1 and EC50 of 124.78 ± 3.39 μgmL-1, respectively. In the hypotonicity-induced hemolysis and 15-LOX inhibition assay, the IC50 values were observed as 147.59 ± 2.98 μgmL-1 and 250.05 ± 8.48 μgmL-1, respectively. The extract inhibited serine protease activity with an IC50 of 301.33 ± 1.31 μgmL-1 and prevented blood coagulation for 10.05 ± 0.35 minutes in prothrombin time assay. The in silico study identified Rhamnetin as a potential 15-LOX1 and 15-LOX2 inhibitor, and it exhibited a stable interaction with the targets throughout the 100 ns dynamic simulation. Conclusion: The findings of this study provide molecular insights into garlic’s medicinal properties as well as its bioactive compounds, which can be potential therapeutic interventions for 15-LOX mediated inflammations.

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Section: Discussionmentioning

confidence: 99%

In vitro and in silico investigation of garlic’s (Allium sativum) bioactivity against 15-lipoxygenase mediated inflammopathies

Khan

Sharif

Salekeen

et al. 2023

J Herbmed Pharmacol

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“…Many plants and their bioactive compounds having antioxidant and anti-inflammatory potential also exhibit anticoagulant effects [27]. Various parts of C. decidua are also reported to be rich in many phyto-constituents such as flavanoids, alkaloids, phenols, terpenoids, carbohydrates, protein, crude fiber and minerals such as Na, Ca, P, Fe, Zn, Cu, Mg, and compounds like capparine, cappariline, capparisine, capparisinine, capparidisine, cadabicine, stachydrine, codonocarpine, isocodonocarpine etc.…”

Section: Discussionmentioning

confidence: 99%

Qualitative phytochemical screening and in vitro thrombolytic activity of Capparis decidua Edgew. Fruit

Kunwar¹,

Jain²,

Verma³

2022

GSC Biol. and Pharm. Sci.

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Abnormal thrombosis plays an important role in development of ischemic heart disease and stroke. Synthetic thrombolytic agents are effective but possess some adverse effects. Therefore, the need for development of comparatively safer anti-thrombotic drugs from natural resources such as plants arises. Capparis decidua Edgew. (Family – Capparaceae) is a densely branched, xerophytic shrub and grows abundantly in arid and semiarid regions. Its fruits are major ingredient of the popular ‘Panchkuta’ vegetable of Rajasthan and also used to prepare pickle. Caper fruits are recommended for treatment of several diseases in traditional medicine including cardiac ailments and shown antioxidant and hypolipidemic potential in scientific studies and therefore, fruits of C. decidua were evaluated for their in vitro thrombolytic potential for the first time. Preliminary qualitative phytochemical screening of fruits of C. decidua; purchased from local market of Udaipur has shown the presence of flavonoids, terpenoids, phenol, phlobatanin, amino acids and carbohydrates and absence of saponin, tannins, steroids and cardiac glycosides. A significant percent clot lysis activity of 23.16±1.26 and 32.39±2.10 was exhibited by methanolic extracts (ME-I and ME-II) of fruits of C. decidua respectively as compared to the positive control streptokinase and negative control as distilled water. However, characterization of bioactive anti-thrombotic molecules as well as large scale, clinical studies is warranted to establish in vivo thrombolytic efficacy of its fruits. Thrombolytic potential of Caper berries as observed in the present study could be useful to recommend its consumption as a dietary health supplement in order to prevent from thrombotic cardiovascular diseases.

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“…Chamomilla is a popular herbaceous plant native to Europe and Western Asia, and the plant is known for its potent medicinal effects. The main phytochemicals of the chamomilla include phenolic compounds (especially flavonoids quercetin, apigenin, or luteolin, among others) [ 125 ]. Chamomilla demonstrates potent effects on platelet inhibition.…”

Section: Phytochemicals With Protective Effects Against Thrombosismentioning

confidence: 99%

Antithrombotic and antiplatelet effects of plant-derived compounds: a great utility potential for primary, secondary, and tertiary care in the framework of 3P medicine

et al. 2022

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Thromboembolism is the third leading vascular disease, with a high annual incidence of 1 to 2 cases per 1000 individuals within the general population. The broader term venous thromboembolism generally refers to deep vein thrombosis, pulmonary embolism, and/or a combination of both. Therefore, thromboembolism can affect both – the central and peripheral veins. Arterial thromboembolism causes systemic ischemia by disturbing blood flow and oxygen supply to organs, tissues, and cells causing, therefore, apoptosis and/or necrosis in the affected tissues. Currently applied antithrombotic drugs used, e.g. to protect affected individuals against ischemic stroke, demonstrate significant limitations. For example, platelet inhibitors possess only moderate efficacy. On the other hand, thrombolytics and anticoagulants significantly increase hemorrhage. Contextually, new approaches are extensively under consideration to develop next-generation antithrombotics with improved efficacy and more personalized and targeted application. To this end, phytochemicals show potent antithrombotic efficacy demonstrated in numerous in vitro, ex vivo, and in vivo models as well as in clinical evaluations conducted on healthy individuals and persons at high risk of thrombotic events, such as pregnant women (primary care), cancer, and COVID-19-affected patients (secondary and tertiary care). Here, we hypothesized that specific antithrombotic and antiplatelet effects of plant-derived compounds might be of great clinical utility in primary, secondary, and tertiary care. To increase the efficacy, precise patient stratification based on predictive diagnostics is essential for targeted protection and treatments tailored to the person in the framework of 3P medicine. Contextually, this paper aims at critical review toward the involvement of specific classes of phytochemicals in antiplatelet and anticoagulation adapted to clinical needs. The paper exemplifies selected plant-derived drugs, plant extracts, and whole plant foods/herbs demonstrating their specific antithrombotic, antiplatelet, and fibrinolytic activities relevant for primary, secondary, and tertiary care. One of the examples considered is antithrombotic and antiplatelet protection specifically relevant for COVID-19-affected patient groups.

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Bioactive Natural Compounds with Antiplatelet and Anticoagulant Activity and Their Potential Role in the Treatment of Thrombotic Disorders

Cited by 22 publications

References 175 publications

In vitro and in silico investigation of garlic’s (Allium sativum) bioactivity against 15-lipoxygenase mediated inflammopathies

In vitro and in silico investigation of garlic’s (Allium sativum) bioactivity against 15-lipoxygenase mediated inflammopathies

Qualitative phytochemical screening and in vitro thrombolytic activity of Capparis decidua Edgew. Fruit

Antithrombotic and antiplatelet effects of plant-derived compounds: a great utility potential for primary, secondary, and tertiary care in the framework of 3P medicine

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