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Troxerutin
Published in Anton C. de Groot, Monographs in Contact Allergy, 2021
Troxerutin is a rutoside, a naturally occurring flavonoid. Flavonoids are polyphenolic compounds that are present in most fruits and vegetables. Although flavonoids are devoid of classical nutritional value, they are increasingly viewed as beneficial dietary components that act as potential protectors against human diseases such as coronary heart disease, cancers, and inflammatory bowel disease. Troxerutin has been used in trials studying the treatment of chronic venous insufficiency. It is also used in topical products, together with Ginkgo biloba leaf extract, as analgesic for temporary relief of pain, swelling and bruising.
Effects of Antithrombotic and Results of Drug Screening
Published in Josef Hladovec, Antithrombotic Drugs in Thrombosis Models, 2020
The selected representative of the bioflavonoid group, troxerutin, is a semisynthetic derivative of rutin (trihydroxyethylrutoside). The group can be more widely defined chemically as benzopyrones.572 It includes coumarin derivatives (not identical with oral anticoagulants which are mostly 4-hydroxy derivatives of coumarin), flavone derivatives, such as (+)-catechin, cromoglycate, silymarin, hesperidin, quercetin, aescin, as well as some drugs which are chemically not benzopyrones but can be included from the pharmacological point of view, such as the two synthetic compounds, calcium dobesilate and ethymsylate.
Pharmacological Treatment of Lymph Stasis
Published in Waldemar L. Olszewski, Lymph Stasis: Pathophysiology, Diagnosis and Treatment, 2019
In one trial that began in 1972 in Switzerland, 133 patients were followed for an average duration of over 6 years. It was the first large-scale trial initiated using the benzopyrones. While this trial had control and experimental groups, it was not a double-blind one. The reason was that the investigators were so convinced by pilot studies about the effectiveness of the benzopyrones that they did not believe it would be ethical to withhold them from the patients. As with most of the early trials, the dose was low (2 tablets each a.m. with each tablet containing 15 mg of coumarin and 90 mg of Troxerutin).40 This preparation is commercially available as Venalot® (Schaper and Brummer, Salzgitter-Ringelheim, Germany).
Neuroprotective effects of troxerutin and cerebroprotein hydrolysate injection on the neurovascular unit in a rat model of Middle cerebral artery occlusion
Published in International Journal of Neuroscience, 2021
Hóngyi Zhào, Ru Wang, Yan Zhang, Yu Liu, Yonghua Huang
Troxerutin, a naturally occurring flavonoid, is known mainly for its anti-inflammatory, antioxidative, antithrombotic, antineoplastic, and anti-apoptotic activities [13, 14]. Cerebroprotein hydrolysate (containing abundant bioactive peptides) has been demonstrated to facilitate the distribution of troxerutin and has a positive synergistic effect with troxerutin against traumatic brain injury [15]. Our group recently set-up a new in vitro NVU model that consists of neurons, astrocytes and brain endothelial cells. Troxerutin and cerebroprotein hydrolysate (TCH) at a concentration of 10 μM rescued the NVU components, reduced the inflammatory factors and downregulated the pro-apoptotic factors induced by oxygen-glucose deprivation and reoxygenation-induced injury in vitro [16]. The present study aimed to investigate the protective effects of TCH injection on a rat model of middle cerebral artery occlusion (MCAO) and the possible mechanism.
Anti-inflammatory effects of troxerutin are mediated through elastase inhibition
Published in Immunopharmacology and Immunotoxicology, 2020
Ramachandran Vidhya, Carani Venkatraman Anuradha
Troxerutin (TX), a derivative of bioflavonoid rutin has anti-obesity effect. TX is abundantly present in flower buds of Sophora japonica, tea, coffee, cereal grains and in a wide variety of fruits and vegetables [11]. Literature search reveals that TX also has antioxidant [12], anti-inflammatory [13], anti-diabetic [14] and anti-cancer properties [15]. Previous studies show that TX attenuates diet-induced oxidative stress and lipid changes in the heart of high-fat, high-fructose diet-fed mice [16]. We hypothesize that the anti-inflammatory properties of TX are mediated through inhibition of elastase. To verify this hypothesis, we investigated the effect of TX on elastase activity and the expression of adipokines in 3T3-L1 adipocytes treated with TNFα, an obesity-associated inflammatory cytokine. Elastatinal (ELAS), an elastase inhibitor [17] and sodium salicylate (SAL), a non-steroidal anti-inflammatory drug [18] were included in the study for comparison. The elastase inhibitory potential of TX was assessed by in vitro enzyme assay. Molecular docking analysis of HNE crystal structure (PDB ID: 3Q76) with TX and ELAS was done using Schrödinger maestro suite of Glide [19] for comparing the binding properties.
Orally delivered rutin in lipid-based nano-formulation exerts strong antithrombotic effects by protein disulfide isomerase inhibition
Published in Drug Delivery, 2022
Dan Chen, Yurong Liu, Peiwen Liu, Yang Zhou, Longguang Jiang, Cai Yuan, Mingdong Huang
Much effort has been devoted to improve the bioavailability of rutin over the past few decades. Troxerutin, a trihydroxyethylated derivative of rutin, was synthesized and intravenously injected to treat chronic venous insufficiency diseases in China (Panat et al., 2016). However, serious side effects of troxerutin are reported in clinical practice. Salt formation is another commonly applied approach to increase the solubility and dissolution rate of acidic and basic drugs. To achieve this goal, careful attention must be paid to selecting and identifying the optimal salt forms for the drug, which is still a trial and error process (Serajuddin, 2007). Meanwhile, nanotechnology engineering holds great potential to overcome the obstacles in drug delivery, including polymeric nanoparticles, liposomes, dendrimers, lipid-based formulations, and nanocrystals (Machado et al., 2021). Lipid-based nano-formulations, such as self-nanoemulsifying drug delivery system (SNEDDS), have been extensively explored as an efficient approach to improve the dissolution and oral absorption of drugs with low water solubility and poor permeability (Porter et al., 2008). SNEDDS, a homogeneous mixture of the drug, oils, surfactants, and co-surfactants, spontaneously disperses in gastrointestinal fluids and forms nanoemulsion under gentle peristalsis (Date et al., 2010). In addition, the small droplet size and deformability makes SNEDDS capable of penetrating mucus and overcoming the absorption barrier of epithelial lining (Griesser et al., 2018). Therefore, this kind of lipid-based nano-formulation could be a promising strategy to address the drawbacks of natural rutin used as an oral antithrombotic agent.