Screening of direct thrombin inhibitors from Radix Salviae Miltiorrhizae by a peak fractionation approach

Lu, Jun Q.; Song, Hui‐Peng; Li, Ping; Zhou, Ping; Dong, Xin; Chen, Jun

doi:10.1016/j.jpba.2015.02.020

Cited by 53 publications

(34 citation statements)

References 25 publications

(29 reference statements)

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Molecular docking studies suggest that TSN binds key residues of the active pocket of thrombin and potentially blocks the interaction with its substrates. 129 In agreement with this finding, TSN inhibits collagen-and ADP-induced platelet aggregation by increasing tubulin acetylation and inhibiting of ERK-2 phosphorylation. 130 TSN also prolongs tail bleeding time in mice, 130 suggesting TSN could inhibit platelet activation in vivo.…”

Section: G Anti-thrombotic Effects Of Tsnsupporting

confidence: 74%

“…Notably, three compounds including dihydrotanshinone (IC 50 = 29.39 μM), CTS (IC 50 = 81.11 μM), and TSN (IC 50 = 66.60 μM) were identified as thrombin inhibitors. Molecular docking studies suggest that TSN binds key residues of the active pocket of thrombin and potentially blocks the interaction with its substrates . In agreement with this finding, TSN inhibits collagen‐ and ADP‐induced platelet aggregation by increasing tubulin acetylation and inhibiting of ERK‐2 phosphorylation .…”

Section: Tsn Protects Against Atherosclerotic Vascular Diseases: Novesupporting

confidence: 63%

“…Dihydrotanshinone also had anti‐angiogenic effects by blocking endothelial proliferation, migration, and tube formation . In the platelet, dihydrotanshinone had stronger thrombin inhibition effects than TSN and CTS . More recently, Zhao et al .…”

Section: Potential Atheroprotective Effects Of Other Tanshinonesmentioning

confidence: 99%

“…Using isolated porcine coronary arteries pre-contracted with the thromboxane A2 analogue U46619, the authors demonstrated that these three constituents relaxed U46619 pre-contracted aorta, suggesting the vasorelaxant effects of tanshinones. Recently, Lu et al 129 have screened direct thrombin inhibitors from Danshen using a peak fraction approach, and observed that 19 out of 91 fractions showed thrombin inhibitory effects in a dose-dependent manner. Notably, three compounds including dihydrotanshinone (IC 50 = 29.39 μM), CTS (IC 50 = 81.11 μM), and TSN (IC 50 = 66.60 μM) were identified as thrombin inhibitors.…”

Section: G Anti-thrombotic Effects Of Tsnmentioning

confidence: 99%

See 3 more Smart Citations

Atheroprotective Effects and Molecular Targets of Tanshinones Derived From Herbal Medicine Danshen

Fang

Little

2017

Medicinal Research Reviews

View full text Add to dashboard Cite

Abstract:Medicinal plant-derived bioactive compounds modulate multiple therapeutic targets in cardiovascular diseases (CVDs), rendering herb-derived phytochemicals effective against one of the major CVDs-atherosclerosis. Danshen (Salvia milthiorriza Bunge) is a Chinese medicine that has been used in cardio-and cerebro-vascular therapeutic remedies in Asian countries for many years. Emerging evidence from cellular, animal, and clinical studies suggests that major lipophilic tanshinones from Danshen can treat atherosclerotic CVDs. In this review, we highlight recent advances in understanding the molecular mechanisms of tanshinones in treating atherosclerosis, ranging from endothelial dysfunction to chronic inflammation. We also overview new molecular targets of tanshinones, including endothelial nitric oxide synthase, AMP-activated protein kinase, ABC transporter A1, heme oxygenase 1, soluble epoxide hydrolase, 11β-hydroxysteroid dehydrogenase, estrogen receptor, and proprotein convertase subtilisin/kexin type 9. Thus, this review provides a new perspective for advancing our understanding of the "ancient" herb Danshen from "modern" biomedical perspectives, supporting the possibility of exploiting tanshinones and derivatives as effective therapeutics against atherosclerosis-related cardiovascular and metabolic diseases.

show abstract

Section: G Anti-thrombotic Effects Of Tsnsupporting

confidence: 74%

Section: Tsn Protects Against Atherosclerotic Vascular Diseases: Novesupporting

confidence: 63%

Section: Potential Atheroprotective Effects Of Other Tanshinonesmentioning

confidence: 99%

Section: G Anti-thrombotic Effects Of Tsnmentioning

confidence: 99%

See 2 more Smart Citations

Atheroprotective Effects and Molecular Targets of Tanshinones Derived From Herbal Medicine Danshen

Fang

Little

2017

Medicinal Research Reviews

View full text Add to dashboard Cite

show abstract

“…The biological actions of these compounds isolated from S. miltiorrhiza have been clarified over the last few years, and several mechanisms have been proposed for the cardiovascular protection effects [67] of this plant, including anti-inflammation [1], antioxidation [65, 68] anti-thrombosis [69], anti-proliferation of vascular smooth muscle cells, inhibition of the expression of adhesion molecules in vascular endothelium and leukocytes [64, 69-71], improvement of acute myocardial ischemia [72], and so on [73]. …”

Section: Phytochemistry Of Salvia Miltiorrhizamentioning

confidence: 99%

Salvia miltiorrhiza: A Potential Red Light to the Development of Cardiovascular Diseases

Wang

Liu

et al. 2017

CPD

194

125

View full text Add to dashboard Cite

Salvia miltiorrhiza Bunge, also known as Danshen in Chinese, has been widely used to treat cardiovascular diseases (CVD) in China and other Asia countries. Here, we summarize literatures of the historical traditional Chinese medicine (TCM) interpretation of the action of Salvia miltiorrhiza, its use in current clinical trials, its main phytochemical constituents and its pharmacological findings by consulting Pubmed, China Knowledge Resource Integrated, China Science and Technology Journal, and the Web of Science Databases. Since 2000, 39 clinical trials have been identified that used S. miltiorrhiza in TCM prescriptions alone or with other herbs for the treatment of patients with CVD. More than 200 individual compounds have been isolated and characterized from S. miltiorrhiza, which exhibited various pharmacological activities targeting different pathways for the treatment of CVD in various animal and cell models. The isolated compounds may provide new perspectives in alternative treatment regimes and reveal novel chemical scaffolds for the development of anti-CVD drugs. Meanwhile, there are also some rising concerns of the potential side effects and drug-drug interactions of this plant. The insights gained from this study will help us to better understanding of the actions of this herb for management of cardiovascular disorders. As an herb of red root, S. miltiorrhiza will act as a potential red light to prevent the development of CVD.

show abstract

Evaluation inhibitory activity of catechins on trypsin by capillary electrophoresis–based immobilized enzyme microreactor with chromogenic substrate

Zhang

Lü

Jiang

et al. 2020

J of Separation Science

View full text Add to dashboard Cite

In this study, a capillary electrophoresis‐based online immobilized enzyme microreactor was developed for evaluating the inhibitory activity of green tea catechins and tea polyphenol extracts on trypsin. The immobilized trypsin activity and other kinetic parameters were evaluated by measuring the peak area of the hydrolyzate of chromogenic substrate S‐2765. The results indicated that the activity of the immobilized trypsin remained approximately 90.0% of the initial immobilized enzyme activity after 30 runs. The value of Michaelis–Menten constant (Km) was (0.47 ± 0.08) mM, and the half‐maximal inhibitory concentration (IC50) and inhibition constant (Ki) of benzamidine were measured as 3.34 and 3.00 mM, respectively. Then, the inhibitory activity of four main catechins (epicatechin, epigallocatechin, epicatechin gallate, and epigallocatechin gallate) and three tea polyphenol extracts (green tea, white tea, and black tea) on trypsin were investigated. The results showed that four catechins and three tea polyphenol extracts had potential trypsin inhibitory activity. In addition, molecular docking results illustrated that epigallocatechin gallate, epicatechin gallate, epicatechin, and epigallocatechin were all located not only in the catalytic cavity, but also in the substrate‐binding pocket of trypsin. These results indicated that the developed method is an effective tool for evaluating inhibitory activity of catechins on trypsin.

show abstract

Screening of direct thrombin inhibitors from Radix Salviae Miltiorrhizae by a peak fractionation approach

Cited by 53 publications

References 25 publications

Atheroprotective Effects and Molecular Targets of Tanshinones Derived From Herbal Medicine Danshen

Atheroprotective Effects and Molecular Targets of Tanshinones Derived From Herbal Medicine Danshen

Salvia miltiorrhiza: A Potential Red Light to the Development of Cardiovascular Diseases

Evaluation inhibitory activity of catechins on trypsin by capillary electrophoresis–based immobilized enzyme microreactor with chromogenic substrate

Contact Info

Product

Resources

About