Pharmacology of Diosmin, a Citrus Flavone Glycoside: An Updated Review

Gerges, Samar H.; Wahdan, Sara A.; Elsherbiny, Doaa A.; El‐Demerdash, Ebtehal

doi:10.1007/s13318-021-00731-y

Cited by 43 publications

(35 citation statements)

References 93 publications

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“…All of them are flavonoid drugs bought from Sigma-Aldrich (Sigma-Aldrich Chemical, Madrid, Spain) and the solvent, DMSO, from Dismadel (Dismadel, S.L., Madrid, Spain). The concentrations employed (0.33 mM, 0.83 mM, 1.0 mM, 1.25 mM, and 1.5 mM) were based on the therapeutical dose of Daflon ® [ 37 ].…”

Section: Methodsmentioning

confidence: 99%

Flavonoids: Antiplatelet Effect as Inhibitors of COX-1

et al. 2022

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Flavonoids are compounds with a benzopyranic structure that exhibits multiple pharmacological activities. They are known for their venotonic activity, but their mechanism of action remains unclear. It is thought that, as this mechanism is mediated by prostaglandins, these compounds may interfere with the arachidonic acid (AA) cascade. These assays are designed to measure the antiplatelet aggregation capacity of quercetin, rutin, diosmetin, diosmin, and hidrosmin, as well as to evaluate a potential structure−activity ratio. In this paper, several studies on platelet aggregation at different concentrations (from 0.33 mM to 1.5 mM) of different flavone compounds are conducted, measuring platelet aggregation by impedance aggregometry, and the cyclooxygenase (COX) activity by metabolites generated, including the activity of the pure recombinant enzyme in the presence of these polyphenols. The results obtained showed that quercetin and diosmetin aglycones have a greater antiplatelet effect and inhibit the COX enzyme activity to a greater extent than their heterosides; however, the fact that greater inhibition of the pure recombinant enzyme was achieved by heterosides suggests that these compounds may have difficulty in crossing biological membranes. In any case, in view of the results obtained, it can be concluded that flavonoids could be useful as coadjuvants in the treatment of cardiovascular pathologies.

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Section: Methodsmentioning

confidence: 99%

Flavonoids: Antiplatelet Effect as Inhibitors of COX-1

et al. 2022

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“…Intestinal flora transforms DSM glycoside to aglycone moiety, which is then rapidly absorbed through the gastrointestinal tract. In humans, the half-life of DSM is 26 to 43 hours when given through the oral route [ 15 ]. It is a venoactive drug that improves microcirculation, lymphatic drainage, and enhances the flexibility of veins by attenuating norepinephrine metabolism by catechol- O -methyl transferase.…”

Section: Introductionmentioning

confidence: 99%

“…It is a venoactive drug that improves microcirculation, lymphatic drainage, and enhances the flexibility of veins by attenuating norepinephrine metabolism by catechol- O -methyl transferase. DSM abrogates microvascular permeability, leukocyte extravasation, and the appearance of adhesion molecules, such as ICAM-1 and VCAM-1 [ 14 , 15 ]. Several studies indicated free radical rummaging and immune harmonizing properties of DSM in the brain [ 16 , 17 ].…”

Section: Introductionmentioning

confidence: 99%

“…Several studies indicated free radical rummaging and immune harmonizing properties of DSM in the brain [ 16 , 17 ]. Clinical evidence recommends that DSM is a well-tolerable, safe, and nontoxic drug [ 15 ]. In nutraceuticals, DSM (Daflon) is often proposed to treat venous disorders, including hemorrhoids and hyperglycemic conditions.…”

Section: Introductionmentioning

confidence: 99%

“…Previous findings indicated that DSM could stimulate insulin release from the β -cells, carbohydrate metabolism, and the expression of glucose transporters (GLUTs). Also, it decreases diabetic complications [ 15 ]. It attenuates dyslipidemia and hepatic gluconeogenesis [ 16 ].…”

Section: Introductionmentioning

confidence: 99%

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Mechanistic Insight into Diosmin-Induced Neuroprotection and Memory Improvement in Intracerebroventricular-Quinolinic Acid Rat Model: Resurrection of Mitochondrial Functions and Antioxidants

Huang

Singh²,

Kainth³

et al. 2022

Evidence-Based Complementary and Alternative Medicine

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Neurodegeneration is the final event after a cascade of pathogenic mechanisms in several brain disorders that lead to cognitive and neurological loss. Quinolinic acid (QA) is an excitotoxin derived from the tryptophan metabolism pathway and is implicated in several ailments, such as Alzheimer’s, Parkinson’s, Huntington’s, and psychosis disease. Diosmin (DSM) is a natural flavonoid possessing such properties that may halt the course of neurodegenerative progression. In past studies, free radical scavenging, along with properties, such as antihyperglycemic, anti-inflammatory, and vasoactive properties, of DSM were pragmatic. Hence, in the current experimentations, the neuroprotective activity of DSM was investigated in the QA rat prototype. QA was administered through the intracerebroventricular route (QA-ICV) in rats on day one, and DSM (50 and 100 mg/kg, intraperitoneal route) was given from day 1 to 21. Memory, gait, sensorimotor functions, and biomarkers of oxidative mutilation and mitochondrial functions were evaluated in the whole brain. Results showed significant deterioration of sensorimotor performance, gait, and working- and long-term memory in rats by QA-ICV. These behavioral anomalies were significantly attenuated by DSM (50 and 100 mg/kg) and donepezil (standard drug). QA-ICV-induced decrease in body mass (g), diet, and water ingestion were also attenuated by DSM or donepezil treatments. QA-ICV inhibited mitochondrial complex I and II activities that caused an increase in oxidative and nitrosative stress along with a reduction in endogenous antioxidants in the brain. DSM dose-dependently ameliorated mitochondrial functions and decreased oxidative stress in QA-ICV-treated rats. DSM can be a possible alternative in treating neurodegenerative disorders with underlying mitochondrial dysfunction pathology.

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