The antithrombotic activity of natural and synthetic coumarins

Gao, Leilei; Wang, Fang; Chen, Yanjun; Li, Fang; Han, Bangxing; Liu, Dong

doi:10.1016/j.fitote.2021.104947

Cited by 33 publications

(21 citation statements)

References 105 publications

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“…The literature indicates that OST possesses various biological activities: 58 anti-inflammatory 2 , 59 , 60 antibacterial, 61 antiviral, 6 antifungal, 62 , 63 antioxidant, 64 , 65 antithrombotic, 66 antidiabetic, 67 antispasmodic, 68 , 69 and anti-tumor. 4 , 70 , 71 Coumarins are considered as drug candidates with diverse pharmacological activities benefiting from their attractive properties such as low molecular weight, simple structure, high solubility, low side effects, low drug resistance, high bioavailability, broad spectrum of activity, and better curative effect.…”

Section: Discussionmentioning

confidence: 99%

Osthole Regulates Secretion of Pro-Inflammatory Cytokines and Expression of TLR2 and NF-κB in Normal Human Keratinocytes and Fibroblasts

Kordulewska

Topa

Cieślińska

et al. 2022

JIR

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Introduction Osthole (OST), an active compound isolated from Cnidium monnieri , is used in traditional Chinese medicine to treat a variety of human diseases. Although OST has a good therapeutic effect, the underlying mechanism of its action in inflammatory skin diseases in humans is still unknown. Purpose The present study aimed to test the hypothesis that OST can be used as an herbal substance that minimizes skin inflammation and barrier dysfunction. In this study, histamine and LPS were used to induce inflammation in skin keratinocytes and fibroblasts to test whether OST can inhibit their responses. Methods Cell migration was analyzed using a wound healing assay. Changes in cell monolayer integrity were assessed by the measurement of transepithelial electrical resistance. Secretion of IL-1β, IL-6, IL-8, TNF-α, CCL2/MCP-1, CCL5/RANTES, and COX-2 was measured by ELISA, while expression of TLR2, NF-κB , and COX -2 was analyzed by qPCR. Results OST decreased the level of IL-1β, TNF-α, CCL2/MCP-1 and CCL5/RANTES, and expression of TLR2, NF-κB and COX-2 during histamine/LPS-induced inflammation in human keratinocytes and fibroblasts. OST also improved cell migration and cell barrier function. Conclusion Our results suggest that OST suppresses inflammatory responses via regulation of IL-1β, TNF-α, CCL2/MCP-1 and CCL5/RANTES secretion, and TLR2 , and COX-2 expression.

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Section: Discussionmentioning

confidence: 99%

Osthole Regulates Secretion of Pro-Inflammatory Cytokines and Expression of TLR2 and NF-κB in Normal Human Keratinocytes and Fibroblasts

Kordulewska

Topa

Cieślińska

et al. 2022

JIR

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“…Coumarin dyes are widely used in uorescent probes because of their low biotoxicity, high uorescence sensitivity, good photostability and easy modi cation of the main chain [22][23][24][25][26][27][28][29][30] . Coumarin derivatives can also be used as uorescence markers or imaging agents to identify tumor lesions and study the subcellular localization of drugs [31][32][33][34][35][36][37][38][39][40][41][42] . In this paper, two novel uorescent probes were synthesized using coumarin with an aldehyde (CHO group) as the uorophore.…”

Section: Introductionmentioning

confidence: 99%

Two Novel coumarin-based fluorescent probes for the detection of Cu2+ and biological applications

Zhang

Huang

Wang

et al. 2023

Preprint

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Large accumulations of copper (Cu) ions in the human body may cause damage, including organ and brain damage. In recent years, studies have proven that a large accumulation of Cu ions can lead to Parkinson's disease and Alzheimer's disease, therefore it is great important to develop novel strategies for detecting trace Cu in environmental and biological samples. In this work, we designed two new coumarin-based colorimetric and fluorescent probes HQ1 and HQ2. These two probes could selectively respond to Cu2+ with obvious color and fluorescence changes, and the presence of other metal ions had no effect on these changes. The two probes also exhibited high sensitivity for Cu2+, with a detection limit as low as 1.81×10-8 M/ 1.57×10-8 M. Notably, the two probes showed potential practical applications and were successfully used for detecting Cu2+ in a test strip, A549 cells and living zebrafish larvae.

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“…11 , 12 Synthetic coumarins have a vital role in the drug discovery and development process. 13–15 One coumarin derivative iminocoumarin, has anticancer, anti-inflammatory, and analgesic activities. 16–18 Several selective, non-toxic organic compounds, including thiosemicarbazide, 19 acetophenone, 20 aminothiadiazole, 21–23 hydrazone derivatives, 24 and p-aminobenzoic acid have anti-inflammatory and analgesic activity.…”

Section: Introductionmentioning

confidence: 99%

Design, Synthesis, and Anti-Inflammatory Activity of Some Coumarin Schiff Base Derivatives: In silico and in vitro Study

Hamid¹,

Salih²

2022

DDDT

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Introduction Inflammation is a fundamental response of the immune system during tissue damage or pathogen infection to protect and maintain tissue homeostasis. However, inflammation may lead to life-threatening conditions. The most common treatment of inflammation is non-steroidal anti-inflammatory drugs (NSAIDs). Nowadays, the development of safer new NSAIDs is critical as most of the existing NSAIDs have serious adverse effects, such as gastrointestinal (GI) toxicity and cardiotoxicity. In the present study, four compounds as Schiff base derivatives of 7-hydroxy-4-formyl coumarin and 7-methoxy-4-formyl coumarin were designed and synthesized aiming to develop a lead compound that exhibits anti-inflammatory activity and circumvents the side effects of NSAIDs, especially GI toxicity. Materials and Methods Lipinski’s rule of five was applied for each designed molecule to evaluate the drug-likeness properties. Molecular docking studies were performed using the ligands and the cyclooxygenase-2 (COX-2) protein to select the best-scored molecule using AutoDock 4.2.6. The molecules were then synthesized and characterized. An in vitro anti-inflammatory assay of the compounds against the COX-2 receptor was realized through a protein denaturation assay. Results and Discussion All four synthesized ligands passed Lipinski’s rule of five and exhibited higher binding free energy compared to the positive standard control (ibuprofen), and the K i values of compounds 5, 7, and 8 were in the nanomolar range. However, only compounds 6 and 7 obtained a higher percentage of inhibition of protein denaturation relative to ibuprofen. Conclusion The present study suggested that compound 7 may be a lead molecule because this ligand not only exhibited the best computational and experimental results but also exhibited the strongest correlation between the concentration and percentage of protein denaturation (R = 0.986 and R 2 = 0.972) with the lowest P-value (0.014).

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The antithrombotic activity of natural and synthetic coumarins

Cited by 33 publications

References 105 publications

Osthole Regulates Secretion of Pro-Inflammatory Cytokines and Expression of TLR2 and NF-κB in Normal Human Keratinocytes and Fibroblasts

Osthole Regulates Secretion of Pro-Inflammatory Cytokines and Expression of TLR2 and NF-κB in Normal Human Keratinocytes and Fibroblasts

Two Novel coumarin-based fluorescent probes for the detection of Cu2+ and biological applications

Design, Synthesis, and Anti-Inflammatory Activity of Some Coumarin Schiff Base Derivatives: In silico and in vitro Study

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