Diosmin
Identification
- Summary
Diosmin is a citrus flavonoid medication used to support vascular health.
- Generic Name
- Diosmin
- DrugBank Accession Number
- DB08995
- Background
Chronic venous insufficiency is a common condition the western population. Compression and pharmacotherapy are frequently used to manage chronic venous insufficiency, improving circulation and symptoms of venous disease.6
Diosmin is a bioflavonoid isolated from various plants or synthesized from hesperidin. It is used for the improvement of capillary fragility or venous insufficiency, including chronic venous insufficiency (CVI) and hemorrhoids. Diosmin is widely available over-the-counter and demonstrates a favourable a favorable safety profile.7,16,20
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Diosmin (DB08995)
- Weight
- Average: 608.5447
Monoisotopic: 608.174120354 - Chemical Formula
- C28H32O15
- Synonyms
- 3',5,7-trihydroxy-4'-methoxyflavone 7-rhamnoglucoside
- 3',5,7-trihydroxy-4'-methoxyflavone-7-rutinoside
- diosmetin 7-neohesperidoside
- Diosmetin 7-O-rutinoside
- Diosmin
- Diosmina
- Diosmine
- Diosminum
- External IDs
- SE 4601
Pharmacology
- Indication
Diosmin is used over-the-counter alone or with ingredients such as hesperidin and diosmetin to support vein and capillary function.17,18
Accelerate your drug discovery research with the industry’s only fully connected ADMET dataset, ideal for:Accelerate your drug discovery research with our fully connected ADMET dataset- Associated Conditions
- Contraindications & Blackbox Warnings
Contraindications & Blackbox WarningsWith our commercial data, access important information on dangerous risks, contraindications, and adverse effects.Our Blackbox Warnings cover Risks, Contraindications, and Adverse Effects- Pharmacodynamics
Diosmin is a venoactive drug supporting circulatory health through various actions on blood vessels; it supports lymphatic drainage and improves microcirculation while increasing venous tone and elasticity. For these reasons, diosmin is frequently taken by individuals with chronic venous disease to support vascular health and has been demonstrated to improve quality of life.3,17 In addition to the above effects, diosmin exerts antioxidant activity and scavenges oxygen free radicals, reducing levels of oxidative stress normally detected through biomarkers such as prostaglandins isoprostane precursors.1
In one clinical study, mean content of TNF alpha, VEGF-C, VEGF-A IL-6, in addition to FGF2 were decreased by after the therapy with diosmin; findings were statistically significant. Additionally, a decrease in edema and mean leg circumference of patients taking diosmin for three months was observed in a clinical study.3 Diosmin has been demonstrated to enhance the metabolism of glucose in diabetic disorders.14
- Mechanism of action
Diosmin helps to maintain circulatory system structure and function, particularly vein strength and competence.17 The molecular mechanism of action of diosmin has not been established.3 Several resources indicate that diosmin binds to the aryl hydrocarbon receptor, however clinical relevance to vascular function is unknown.11,12,13 One study demonstrates that oral diosmin exerts effects on the in vitro metabolism of noradrenaline by varicose veins, potentially benefitting vascular health.9
Target Actions Organism UAryl hydrocarbon receptor agonistHumans - Absorption
Diosmin is rapidly absorbed in the gastrointestinal tract.2 After a 900 mg single oral dose in a study using liquid chromatography with tandem mass spectrometry (LC-MS/MS) method, Cmax was 4.2±3.8 ng·mL-1, Tmax was 18.7±9.9 hours, and AUC0~96 was 185.4±166.2 ng·mL-1 in healthy volunteers.15 Another pharmacokinetic study of 5 adults revealed a Cmax of 417±94.1 ng/dL.18
- Volume of distribution
A pharmacokinetic study of 5 adults revealed a volume of distribution of 62.1±7.9 L.18
- Protein binding
Diosmin binds to serum albumin.4
- Metabolism
Degradation products of diosmin such as alkyl-phenolic acids confirm a metabolic pattern similar to that of other flavonoids.2
- Route of elimination
Pharmacokinetic data show absence of urinary elimination for diosmin and its aglycone diosmetin. Minor metabolites are found to be eliminated in the urine as glucuronic acid conjugates.2
- Half-life
Diosmin half-life ranges from 26 to 43 hours.2 One study using a liquid chromatography with tandem mass spectrometry (LC-MS/MS) method after a single 900 mg dose of diosmin demonstrated a half-life of 60.2±85.7 hours in healthy volunteers.15
- Clearance
Not Available
- Adverse Effects
Reduce medical errorsand improve treatment outcomes with our comprehensive & structured data on drug adverse effects.Reduce medical errors & improve treatment outcomes with our adverse effects data- Toxicity
The LD50 of diosmin is >3g/kg in animal studies, with an LD50 of great than 3000 mg/kg in rats.15 No cases of overdose have been reported, however, an overdose is likely to result in gastrointestinal effects such as nausea, dyspepsia, vomiting, and diarrhea.20
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbemaciclib The serum concentration of Abemaciclib can be increased when it is combined with Diosmin. Acalabrutinib The metabolism of Acalabrutinib can be decreased when combined with Diosmin. Acenocoumarol The metabolism of Acenocoumarol can be decreased when combined with Diosmin. Acetaminophen The metabolism of Acetaminophen can be decreased when combined with Diosmin. Acetohexamide The metabolism of Acetohexamide can be decreased when combined with Diosmin. Acetylsalicylic acid The metabolism of Acetylsalicylic acid can be decreased when combined with Diosmin. Afatinib The serum concentration of Afatinib can be increased when it is combined with Diosmin. Albendazole The metabolism of Albendazole can be decreased when combined with Diosmin. Alectinib The metabolism of Alectinib can be decreased when combined with Diosmin. Alosetron The metabolism of Alosetron can be decreased when combined with Diosmin. 
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- Take with or without food.
Products
Comprehensive & structured drug product infoFrom application numbers to product codes, connect different identifiers through our commercial datasets.Easily connect various identifiers back to our datasets- International/Other Brands
- Barosmin / Dalfon (Servier) / Detralex / Diosven / Dioven / Diovenor / Flebosmil / Flebosten / Insuven / Litosmil / Ven-Detrex / Venosmine
- Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image AVEFLON TABLET Diosmin (450 mg) + Hesperidin (50 mg) Tablet, film coated Oral APEX PHARMACY MARKETING SDN. BHD. 2020-09-08 Not applicable Malaysia 
Daflon 1000mg Film-Coated Tablet Diosmin (900 mg) + Hesperidin (100 mg) Tablet, film coated Oral SERVIER MALAYSIA SDN BHD 2020-09-08 Not applicable Malaysia daflon 500mg tablets Diosmin (450 mg) + Hesperidin (50 mg) Tablet, film coated Oral SERVIER MALAYSIA SDN BHD 2020-09-08 Not applicable Malaysia Davmorid Film Coated Tablet Diosmin (450 mg) + Hesperidin (50 mg) Tablet, film coated Oral Y.S.P. INDUSTRIES (M) SDN BHD 2020-09-08 Not applicable Malaysia DIOFLEX TABLET Diosmin (450 mg) + Hesperidin (50 mg) Tablet Oral PRIME PHARMACEUTICAL SDN. BHD. 2020-09-08 Not applicable Malaysia DIOKERN 450 MG/50 MG FILM KAPLI TABLET,30 ADET Diosmin (450 mg) + Hesperidin (50 mg) Tablet, coated Oral DROGSAN İLAÇLARI SAN. VE TİC. A.Ş. 2020-08-14 Not applicable Turkey 
DIOKERN 450 MG/50 MG FILM KAPLI TABLET,60 ADET Diosmin (450 mg) + Hesperidin (50 mg) Tablet, coated Oral DROGSAN İLAÇLARI SAN. VE TİC. A.Ş. 2020-08-14 Not applicable Turkey Dofomin 500mg Tablet Diosmin (450 mg) + Hesperidin (50 mg) Tablet Oral IMEKS PHARMA SDN. BHD. 2020-09-08 Not applicable Malaysia Euvein Film Coated Tablet Diosmin (450 mg) + Hesperidin (50 mg) Tablet, film coated Oral Medicell Pharmaceutical(malaysia) Sdn.bhd 2020-09-08 Not applicable Malaysia Hemaron Tablet Diosmin (450 mg) + Hesperidin (50 mg) Tablet, film coated Oral Noripharma Sdn. Bhd. 2020-09-08 Not applicable Malaysia - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Analpram Advanced Diosmin (600 mg/1) + Calcium magnesium potassium carbonate chloride hydroxide (30 mg/1) + Hydrocortisone acetate (25 mg/1g) + Pramoxine hydrochloride (10 mg/1g) Kit Topical Sebela Pharmaceuticals Inc. 2015-08-07 2016-08-31 US 
Analpram Advanced Diosmin (600 mg/1) + Calcium magnesium potassium carbonate chloride hydroxide (30 mg/1) + Hydrocortisone acetate (25 mg/1g) + Pramoxine hydrochloride (10 mg/1g) Kit Oral; Topical Sebela Pharmaceuticals Inc. 2015-08-07 2017-02-28 US Analpram Advanced Diosmin (600 mg/1) + Calcium magnesium potassium carbonate chloride hydroxide (30 mg/1) + Hydrocortisone acetate (25 mg/1g) + Pramoxine hydrochloride (10 mg/1g) Kit Oral; Topical Sebela Pharmaceuticals Inc. 2015-08-07 2017-02-28 US
Categories
- ATC Codes
- C05CA03 — Diosmin
- C05CA — Bioflavonoids
- C05C — CAPILLARY STABILIZING AGENTS
- C05 — VASOPROTECTIVES
- C — CARDIOVASCULAR SYSTEM
- Drug Categories
- Benzopyrans
- Capillary Stabilizing Agents
- Chromones
- Cytochrome P-450 CYP2C9 Inhibitors
- Cytochrome P-450 CYP2C9 Inhibitors (strength unknown)
- Cytochrome P-450 CYP2E1 Inhibitors
- Cytochrome P-450 CYP2E1 Inhibitors (strength unknown)
- Cytochrome P-450 CYP3A Inhibitors
- Cytochrome P-450 CYP3A4 Inhibitors
- Cytochrome P-450 CYP3A4 Inhibitors (strength unknown)
- Cytochrome P-450 Enzyme Inhibitors
- Flavones
- Flavonoids
- Heterocyclic Compounds, Fused-Ring
- OATP1B1/SLCO1B1 Inhibitors
- P-glycoprotein inhibitors
- Pyrans
- Vasoprotectives
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as flavonoid-7-o-glycosides. These are phenolic compounds containing a flavonoid moiety which is O-glycosidically linked to carbohydrate moiety at the C7-position.
- Kingdom
- Organic compounds
- Super Class
- Phenylpropanoids and polyketides
- Class
- Flavonoids
- Sub Class
- Flavonoid glycosides
- Direct Parent
- Flavonoid-7-O-glycosides
- Alternative Parents
- 4'-O-methylated flavonoids / 3'-hydroxyflavonoids / 5-hydroxyflavonoids / Flavones / Phenolic glycosides / O-glycosyl compounds / Chromones / Disaccharides / Methoxyphenols / Phenoxy compounds show 15 more
- Substituents
- 1-benzopyran / 1-hydroxy-2-unsubstituted benzenoid / 1-hydroxy-4-unsubstituted benzenoid / 3'-hydroxyflavonoid / 4p-methoxyflavonoid-skeleton / 5-hydroxyflavonoid / Acetal / Alcohol / Alkyl aryl ether / Anisole show 31 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- rutinoside, disaccharide derivative, monomethoxyflavone, glycosyloxyflavone, dihydroxyflavanone (CHEBI:4631) / flavones (C10039)
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- 7QM776WJ5N
- CAS number
- 520-27-4
- InChI Key
- GZSOSUNBTXMUFQ-YFAPSIMESA-N
- InChI
- InChI=1S/C28H32O15/c1-10-21(32)23(34)25(36)27(40-10)39-9-19-22(33)24(35)26(37)28(43-19)41-12-6-14(30)20-15(31)8-17(42-18(20)7-12)11-3-4-16(38-2)13(29)5-11/h3-8,10,19,21-30,32-37H,9H2,1-2H3/t10-,19+,21-,22+,23+,24-,25+,26+,27+,28+/m0/s1
- IUPAC Name
- 5-hydroxy-2-(3-hydroxy-4-methoxyphenyl)-7-{[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-({[(2R,3R,4R,5R,6S)-3,4,5-trihydroxy-6-methyloxan-2-yl]oxy}methyl)oxan-2-yl]oxy}-4H-chromen-4-one
- SMILES
- COC1=C(O)C=C(C=C1)C1=CC(=O)C2=C(O)C=C(O[C@@H]3O[C@H](CO[C@@H]4O[C@@H](C)[C@H](O)[C@@H](O)[C@H]4O)[C@@H](O)[C@H](O)[C@H]3O)C=C2O1
References
- Synthesis Reference
Rajiv Sakhardande, Manmohan Nimbalkar, Navin Khatri, Subarao Patil, Santosh Bhalekar, Rajendra Patil, Pandharinath Firake (2011). Process for the preparation of diosmin (WO2010092592A2).IFI CLAIMS PATENT SERVICES.https://patents.google.com/patent/WO2010092592A2/en
- General References
- Feldo M, Wozniak M, Wojciak-Kosior M, Sowa I, Kot-Wasik A, Aszyk J, Bogucki J, Zubilewicz T, Bogucka-Kocka A: Influence of Diosmin Treatment on the Level of Oxidative Stress Markers in Patients with Chronic Venous Insufficiency. Oxid Med Cell Longev. 2018 Aug 28;2018:2561705. doi: 10.1155/2018/2561705. eCollection 2018. [Article]
- Cova D, De Angelis L, Giavarini F, Palladini G, Perego R: Pharmacokinetics and metabolism of oral diosmin in healthy volunteers. Int J Clin Pharmacol Ther Toxicol. 1992 Jan;30(1):29-33. [Article]
- Feldo M, Wojciak-Kosior M, Sowa I, Kocki J, Bogucki J, Zubilewicz T, Kesik J, Bogucka-Kocka A: Effect of Diosmin Administration in Patients with Chronic Venous Disorders on Selected Factors Affecting Angiogenesis. Molecules. 2019 Sep 12;24(18). pii: molecules24183316. doi: 10.3390/molecules24183316. [Article]
- Barreca D, Lagana G, Bruno G, Magazu S, Bellocco E: Diosmin binding to human serum albumin and its preventive action against degradation due to oxidative injuries. Biochimie. 2013 Nov;95(11):2042-9. doi: 10.1016/j.biochi.2013.07.014. Epub 2013 Jul 22. [Article]
- Gzona Bajraktari, Johanna Weiss: The aglycone diosmetin has the higher perpetrator drug-drug interaction potential compared to the parent flavone diosmin Journal of Functional Foods. [Article]
- Sliva J: Diosmin - still an important modality in the treatment of venous insufficiency. Vnitr Lek. 2019 Summer;65(7-8):524-526. [Article]
- Milano G, Leone S, Fucile C, Zuccoli ML, Stimamiglio A, Martelli A, Mattioli F: Uncommon serum creatine phosphokinase and lactic dehydrogenase increase during diosmin therapy: two case reports. J Med Case Rep. 2014 Jun 16;8:194. doi: 10.1186/1752-1947-8-194. [Article]
- Boisnic S, Branchet MC, Gouhier-Kodas C, Verriere F, Jabbour V: Anti-inflammatory and antiradical effects of a 2% diosmin cream in a human skin organ culture as model. J Cosmet Dermatol. 2018 Oct;17(5):848-854. doi: 10.1111/jocd.12778. Epub 2018 Sep 10. [Article]
- Araujo D, Viana F, Osswald W: Diosmin therapy alters the in vitro metabolism of noradrenaline by the varicose human saphenous vein. Pharmacol Res. 1991 Oct;24(3):253-6. doi: 10.1016/1043-6618(91)90088-f. [Article]
- Bogucka-Kocka A, Wozniak M, Feldo M, Kockic J, Szewczyk K: Diosmin--isolation techniques, determination in plant material and pharmaceutical formulations, and clinical use. Nat Prod Commun. 2013 Apr;8(4):545-50. [Article]
- Zhang S, Qin C, Safe SH: Flavonoids as aryl hydrocarbon receptor agonists/antagonists: effects of structure and cell context. Environ Health Perspect. 2003 Dec;111(16):1877-82. [Article]
- Ciolino HP, Wang TT, Yeh GC: Diosmin and diosmetin are agonists of the aryl hydrocarbon receptor that differentially affect cytochrome P450 1A1 activity. Cancer Res. 1998 Jul 1;58(13):2754-60. [Article]
- Lee J, Song KM, Jung CH: Diosmin restores the skin barrier by targeting the aryl hydrocarbon receptor in atopic dermatitis. Phytomedicine. 2021 Jan;81:153418. doi: 10.1016/j.phymed.2020.153418. Epub 2020 Nov 25. [Article]
- Hsu CC, Lin MH, Cheng JT, Wu MC: Antihyperglycaemic action of diosmin, a citrus flavonoid, is induced through endogenous beta-endorphin in type I-like diabetic rats. Clin Exp Pharmacol Physiol. 2017 May;44(5):549-555. doi: 10.1111/1440-1681.12739. [Article]
- T.T. Zhu, M-L. Du, H.M. Su, Lun Yang: Pharmacokinetics of diosmin tablets in healthy volunteers Chinese Journal of New Drugs. [Article]
- Ronald Watson, Victor Preedy (2019). Bioactive Food as Dietary Interventions for Diabetes (2nd ed.). Academic Press. [ISBN:978-0-12-813822-9]
- Xymogen product monograph: DIOVASC (Diosmin and hesperidin) oral capsules [Link]
- DailyMed label: VASCULERA (diosmiplex) oral tablets [Link]
- ECHA Europa Registration Dossier: Diosmin [Link]
- Summary of Product Characteristics: Diosmin [Link]
- External Links
- KEGG Drug
- D07858
- KEGG Compound
- C10039
- PubChem Compound
- 5281613
- PubChem Substance
- 310264956
- ChemSpider
- 4444932
- BindingDB
- 153267
- 3489
- ChEBI
- 4631
- ChEMBL
- CHEMBL231884
- ZINC
- ZINC000004098512
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Diosmin
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Completed Basic Science Chronic Venous Insufficiency (CVI) 1 4 Completed Treatment Deep Vein Thrombosis / Post Thrombotic Syndrome 1 4 Completed Treatment Venous Insufficiency 1 4 Not Yet Recruiting Treatment Pelvic Congestive Syndrome / Pelvic Varicose Veins / Venous Disease 1 4 Recruiting Treatment Lymphedema Lower Extremity 1 3 Completed Treatment Chronic Venous Disease of Lower Limbs 1 3 Unknown Status Treatment Chronic Venous Insufficiency (CVI) / Diseases 1 3 Unknown Status Treatment Chronic Venous Insufficiency (CVI) / Haemorrhoids 1 2, 3 Completed Prevention Infertility 1 1, 2 Unknown Status Treatment Hypermenorrhea 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Kit Oral; Topical Kit Topical Tablet, coated Oral Tablet, film coated Oral Tablet, film coated Oral Tablet, coated Oral Granule Cream Topical Granule, for solution Oral Tablet Oral Tablet Oral 150 MG Tablet Oral 300 MG Tablet, film coated Oral 600 mg Tablet Oral Tablet Oral 450 mg Powder, for suspension Oral Capsule Powder, for suspension Oral Tablet, coated Oral 500 mg Tablet, coated Oral 450 mg - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 277-278 https://www.chemsrc.com/en/cas/520-27-4_329710.html boiling point (°C) 926.8±65.0 https://www.chemsrc.com/en/cas/520-27-4_329710.html water solubility 0.019 ± 0.005 mg/L https://echa.europa.eu/registration-dossier/-/registered-dossier/21071/4/9 logP 2.05 https://www.chemsrc.com/en/cas/520-27-4_329710.html pKa 6.10±0.40 https://www.chemicalbook.com/ChemicalProductProperty_EN_CB6443258.htm - Predicted Properties
Property Value Source Water Solubility 1.54 mg/mL ALOGPS logP 0.08 ALOGPS logP -0.44 ChemAxon logS -2.6 ALOGPS pKa (Strongest Acidic) 8.48 ChemAxon pKa (Strongest Basic) -3.6 ChemAxon Physiological Charge 0 ChemAxon Hydrogen Acceptor Count 15 ChemAxon Hydrogen Donor Count 8 ChemAxon Polar Surface Area 234.29 Å2 ChemAxon Rotatable Bond Count 7 ChemAxon Refractivity 142.39 m3·mol-1 ChemAxon Polarizability 59.17 Å3 ChemAxon Number of Rings 5 ChemAxon Bioavailability 0 ChemAxon Rule of Five No ChemAxon Ghose Filter No ChemAxon Veber's Rule No ChemAxon MDDR-like Rule Yes ChemAxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Targets
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Agonist
- General Function
- Transcription regulatory region dna binding
- Specific Function
- Ligand-activated transcriptional activator. Binds to the XRE promoter region of genes it activates. Activates the expression of multiple phase I and II xenobiotic chemical metabolizing enzyme genes...
- Gene Name
- AHR
- Uniprot ID
- P35869
- Uniprot Name
- Aryl hydrocarbon receptor
- Molecular Weight
- 96146.705 Da
References
- Zhang S, Qin C, Safe SH: Flavonoids as aryl hydrocarbon receptor agonists/antagonists: effects of structure and cell context. Environ Health Perspect. 2003 Dec;111(16):1877-82. [Article]
- Ciolino HP, Wang TT, Yeh GC: Diosmin and diosmetin are agonists of the aryl hydrocarbon receptor that differentially affect cytochrome P450 1A1 activity. Cancer Res. 1998 Jul 1;58(13):2754-60. [Article]
- Lee J, Song KM, Jung CH: Diosmin restores the skin barrier by targeting the aryl hydrocarbon receptor in atopic dermatitis. Phytomedicine. 2021 Jan;81:153418. doi: 10.1016/j.phymed.2020.153418. Epub 2020 Nov 25. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inducer
- Curator comments
- Data supported by in vitro studies only. Clinical relevance is unknown.
- General Function
- Vitamin d 24-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP1A1
- Uniprot ID
- P04798
- Uniprot Name
- Cytochrome P450 1A1
- Molecular Weight
- 58164.815 Da
References
- Gzona Bajraktari, Johanna Weiss: The aglycone diosmetin has the higher perpetrator drug-drug interaction potential compared to the parent flavone diosmin Journal of Functional Foods. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Steroid hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP2C9
- Uniprot ID
- P11712
- Uniprot Name
- Cytochrome P450 2C9
- Molecular Weight
- 55627.365 Da
References
- Gzona Bajraktari, Johanna Weiss: The aglycone diosmetin has the higher perpetrator drug-drug interaction potential compared to the parent flavone diosmin Journal of Functional Foods. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Steroid hydroxylase activity
- Specific Function
- Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic ...
- Gene Name
- CYP2E1
- Uniprot ID
- P05181
- Uniprot Name
- Cytochrome P450 2E1
- Molecular Weight
- 56848.42 Da
References
- Gzona Bajraktari, Johanna Weiss: The aglycone diosmetin has the higher perpetrator drug-drug interaction potential compared to the parent flavone diosmin Journal of Functional Foods. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Vitamin d3 25-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- Gzona Bajraktari, Johanna Weiss: The aglycone diosmetin has the higher perpetrator drug-drug interaction potential compared to the parent flavone diosmin Journal of Functional Foods. [Article]
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Binder
- General Function
- Toxic substance binding
- Specific Function
- Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
- Gene Name
- ALB
- Uniprot ID
- P02768
- Uniprot Name
- Serum albumin
- Molecular Weight
- 69365.94 Da
References
- Barreca D, Lagana G, Bruno G, Magazu S, Bellocco E: Diosmin binding to human serum albumin and its preventive action against degradation due to oxidative injuries. Biochimie. 2013 Nov;95(11):2042-9. doi: 10.1016/j.biochi.2013.07.014. Epub 2013 Jul 22. [Article]
- Naso L, Martinez VR, Lezama L, Salado C, Valcarcel M, Ferrer EG, Williams PAM: Antioxidant, anticancer activities and mechanistic studies of the flavone glycoside diosmin and its oxidovanadium(IV) complex. Interactions with bovine serum albumin. Bioorg Med Chem. 2016 Sep 15;24(18):4108-4119. doi: 10.1016/j.bmc.2016.06.053. Epub 2016 Jun 28. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
- Gene Name
- ABCB1
- Uniprot ID
- P08183
- Uniprot Name
- Multidrug resistance protein 1
- Molecular Weight
- 141477.255 Da
References
- Yoo HH, Lee M, Chung HJ, Lee SK, Kim DH: Effects of diosmin, a flavonoid glycoside in citrus fruits, on P-glycoprotein-mediated drug efflux in human intestinal Caco-2 cells. J Agric Food Chem. 2007 Sep 5;55(18):7620-5. doi: 10.1021/jf070893f. Epub 2007 Aug 4. [Article]
- Neerati P, Bedada SK: Effect of diosmin on the intestinal absorption and pharmacokinetics of fexofenadine in rats. Pharmacol Rep. 2015 Apr;67(2):339-44. doi: 10.1016/j.pharep.2014.09.010. Epub 2014 Oct 1. [Article]
- Rajnarayana K, Venkatesham A, Krishna DR: Influence of some bioflavonoids on the transport of nitrendipine. Drug Metabol Drug Interact. 2008;23(3-4):299-310. doi: 10.1515/dmdi.2008.23.3-4.299. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- Curator comments
- This information is supported by in vitro data only. Clinical relevance is unknown.
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostagland...
- Gene Name
- SLCO1B1
- Uniprot ID
- Q9Y6L6
- Uniprot Name
- Solute carrier organic anion transporter family member 1B1
- Molecular Weight
- 76447.99 Da
References
- Gzona Bajraktari, Johanna Weiss: The aglycone diosmetin has the higher perpetrator drug-drug interaction potential compared to the parent flavone diosmin Journal of Functional Foods. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Curator comments
- This information is supported by in vitro data only. Clinical relevance is unknown.
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Mediates the Na(+)-independent uptake of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotre...
- Gene Name
- SLCO1B3
- Uniprot ID
- Q9NPD5
- Uniprot Name
- Solute carrier organic anion transporter family member 1B3
- Molecular Weight
- 77402.175 Da
References
- Gzona Bajraktari, Johanna Weiss: The aglycone diosmetin has the higher perpetrator drug-drug interaction potential compared to the parent flavone diosmin Journal of Functional Foods. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Curator comments
- This information is supported by in vitro data only. Clinical relevance is unknown.
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Mediates the Na(+)-independent transport of organic anions such as taurocholate, the prostaglandins PGD2, PGE1, PGE2, leukotriene C4, thromboxane B2 and iloprost.
- Gene Name
- SLCO2B1
- Uniprot ID
- O94956
- Uniprot Name
- Solute carrier organic anion transporter family member 2B1
- Molecular Weight
- 76709.98 Da
References
- Gzona Bajraktari, Johanna Weiss: The aglycone diosmetin has the higher perpetrator drug-drug interaction potential compared to the parent flavone diosmin Journal of Functional Foods. [Article]
Drug created on June 16, 2014 18:43 / Updated on April 16, 2021 04:48