hesperidin

Botanicalexperimental

Hesperidin is a flavanone glycoside found in citrus fruits. Its aglycone form is called hesperetin. Its name is derived from the word "hesperidium", for fruit produced by citrus trees. Hesperidin was first isolated in 1828 by French chemist Lebreton from the white inner layer of citrus peels (mesocarp, albedo). As a flavanone found in citrus fruits (such as oranges, lemons or pummelo fruits), hesperidin is under laboratory research for possible biological properties. One area of research is focused on the possible chemopreventive effects of hesperidin, but there is no current proof that hesperidin has this role in human cancer mechanisms. Hesperidin was effective in an animal model of Alzheimer's, alleviating pathological changes induced by aluminum. Early research suggests that taking one tablet of a specific product (Daflon 500, Les Laboratoires Servier) containing hesperidin and diosmin by mouth for 45 days decreases blood sugar levels and improves blood sugarcontrol in women with type 2 diabetes. For Rheumatoid arthritis (RA): early research suggests that drinking a beverage containing alpha-glucosyl hesperidin for 12 weeks improves symptoms of RA. Orally, hesperidin can cause gastrointestinal side effects, including abdominal pain, diarrhea, and gastritis. Headache can also occur in some patients. The possible anti-inflammatory action of hesperidin is probably due to the possible anti-inflammatory action of its aglycone hesperetin. Hesperetin appears to interfere with the metabolism of arachidonic acid as well as with histamine release. Hesperetin appears to inhibit phospholipase A2, lipoxygenase and cyclo-oxygenase. There is evidence that hesperetin inhibits histamine release from mast cells, which would account for the possible anti-allergic activity of hesperidin. The possible hypolipidemic effect of hesperidin is probably due to hesperetin's possible action in lipid lowering. Hesperetin may reduce plasma cholesterol levels by inhibition of 3-hydroxy-3-methylglutaryl coenzyme A (HMG CoA) reductase, as well as acyl coenzyme A: cholesterol acytransferase (ACAT). Inhibition of these enzymes by hesperetin has been demonstrated in rats fed a high cholesterol diet. The mechanism of hesperidin's possible vasoprotective action is unclear. Animal studies have shown that hesperidin decreases microvascular permeability. Hesperidin, itself or via hesperetin, may protect endothelial cells from hypoxia by stimulating certain mitochondrial enzymes, such as succinate dehydrogenase. The mechanism of hesperidin's possible anticarcinogenic action is also unclear. One explanation may be the inhibition of polyamine synthesis. Inhibition of lipoxygenase and cyclo-oxygenase is another possibility. — NCATS

Chemistry & pharmacology

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SMILES

COC1=CC=C(C=C1O)[C@@H]2CC(=O)C3=C(O)C=C(O[C@@H]4O[C@H](CO[C@@H]5O[C@@H](C)[C@H](O)[C@@H](O)[C@H]5O)[C@@H](O)[C@H](O)[C@H]4O)C=C3O2
Mol. weight
610.5606 g/mol

Oral

No

Parenteral

No

Topical

No

Sources

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT07185386N/AMay 28, 2025Ekalab S.r.l.
NCT07300735N/AMar 1, 2025Alexandria University
NCT07293767N/ANov 16, 2024Ain Shams University
NCT06584799Phase 3Sep 30, 2024Pirogov Russian National Research Medical University
NCT05756179Phase 3Jul 18, 2023Alexandria University
NCT06367166N/AApr 1, 2023Ryazan State Medical University
NCT06402032N/ASep 1, 2022Cairo University
NCT05243706Phase 3Mar 1, 2022Ain Shams University
NCT05158192Phase 1Nov 4, 2021Grunenthal
NCT04715932Phase 2Feb 18, 2021Ingenew Pharmaceuticals Inc., University of Montreal
NCT04358497Phase 4Oct 1, 2020Centro Cardiovascular Universitario, Hospital de Clínicas Dr. Manuel Quintela, Hospital Pereyra Rossell, Montevideo, University of the Republic, Uruguay
NCT04933591N/ASep 1, 2020Pirogov Russian National Research Medical University
NCT04452799Early Phase 1 (Phase 1)Jul 1, 2020Tanta University
NCT04316390N/AApr 30, 2020Hochschule Geisenheim University, University of Kiel
NCT04145102N/ANov 1, 2019Al Azhar University
NCT04360889Phase 4Sep 1, 2019Ryazan State Medical University
NCT03984916N/AJun 30, 2019Centro Tecnológico de Nutrición y Salud (Eurecat_Reus). Reus, Tarragona, Spain., Eurecat, Rovira i Virgili University
NCT04597983N/ASep 22, 2018Universidad Católica San Antonio de Murcia
NCT03734874N/AJun 1, 2018National Nutrition and Food Technology Institute
NCT03734835N/AApr 1, 2018National Nutrition and Food Technology Institute
Showing 20 of 28 trials
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Organizations

Research & Development (30)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
National Nutrition and Food Technology InstituteGovernment6612017
Ain Shams UniversityAcademic/Hospital2222022
Alexandria UniversityAcademic/Hospital2222023
Pirogov Russian National Research Medical UniversityAcademic/Hospital2222020
Ryazan State Medical UniversityAcademic/Hospital2222019
Universidad Católica San Antonio de MurciaAcademic/Hospital2112015
Al Azhar UniversityAcademic/Hospital1112019
Albert Einstein Israelite HospitalAcademic/Hospital1012017
Cairo UniversityAcademic/Hospital1112022
Centro Cardiovascular UniversitarioAcademic/Hospital1012020
Centro Tecnológico de Nutrición y Salud (Eurecat_Reus). Reus, Tarragona, Spain.Academic/Hospital1012019
Ekalab S.r.l.For profit1112025
EurecatFor profit1012019
Fundação Educacional Serra dos ÓrgãosAcademic/Hospital1112017
FytexiaAcademic/Hospital1112015
GrunenthalFor profit1112021
Hochschule Geisenheim UniversityAcademic/Hospital1012020
Hospital de Clínicas Dr. Manuel QuintelaAcademic/Hospital1112020
Hospital Pereyra Rossell, MontevideoAcademic/Hospital1012020
Ingenew Pharmaceuticals Inc.Academic/Hospital1012021
30 organizations
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