Bioflavonoid – Uses, Dosage, Side Effects, Interactions

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Bioflavonoid /Hesperidin is a disaccharide derivative that consists of hesperetin substituted by a 6-O-(alpha-L-rhamnopyranosyl)-beta-D-glucopyranosyl moiety at position 7 via a glycosidic linkage. It has a role as a mutagen. It is a disaccharide derivative, a member of 3′-hydroxyflavanones, a dihydroxyflavanone, a monomethoxyflavanone, a flavanone glycoside, a member of 4′-methoxyflavanones and a rutinoside. It derives from a hesperetin.

Hesperidin is an abundant and inexpensive by-product of Citrus cultivation and is the major flavonoid in sweet orange and lemon. In young immature oranges, it can account for up to 14% of the fresh weight of the fruit. Hesperidin is an abundant and inexpensive by-product of Citrus cultivation and is the major flavonoid in sweet orange and lemon. In young immature oranges, it can account for up to 14% of the fresh weight of the fruit due to vitamin C deficiency such as bruising due to capillary fragility was found in early studies to be relieved by crude vitamin C extract but not by purified vitamin C. The bioflavonoids, formerly called “vitamin P“, were found to be the essential components in correcting this bruising tendency and improving the permeability and integrity of the capillary lining. These bioflavonoids include hesperidin, citrin, rutin, flavones, flavonols, catechin, and quercetin. Of historical importance is the observation that “citrin”, a mixture of two flavonoids, eriodictyol, and hesperidin, was considered to possess a vitamin-like activity, as early as in 1949. Hesperidin deficiency has since been linked with abnormal capillary leakiness as well as pain in the extremities causing aches, weakness and night leg cramps. Supplemental hesperidin also helps in reducing edema or excess swelling in the legs due to fluid accumulation. As with other bioflavonoids, hesperidin works best when administered concomitantly with vitamin C. No signs of toxicity have been observed with normal intake of hesperidin. Hesperidin was first discovered in 1827, by Lebreton, but not in a pure state and has been under continuous investigation since then (PMID: 11746857).

Another Name

  • (S)-(−)-hesperidin
  • Cirantin
  • Ciratin
  • Hesperetin 7-O-rutinoside
  • Hesperidin
  • Hesperidina
  • Hesperidoside
  • Bioflavonoid,
  • Bioflavonoid Complex,
  • Bioflavonoid Concentrate,
  • Bioflavonoid Extract,
  • Bioflavonoide,
  • Bioflavonoide d Agrume,
  • Bioflavonoïdes d’Agrumes,
  • Citrus Bioflavones,
  • Citrus Bioflavonoid,
  • Citrus Bioflavonoids,
  • Citrus Bioflavonoid Extract,
  • Citrus Flavones,
  • Citrus Flavonoids,
  • Complexe de Bioflavonoides,
  • Concentré de Bioflavonoides,
  • Extrait de Bioflavonoïdes,
  • Extrait de Bioflavonoides d’Agrumes,
  • Flavonoid,
  • Flavonoïde, Hesperidin Methyl Chalcone,
  • Hesperidina, Hesperidine, Trimethylhesperidin-chalcon


Mechanism of Action of Bioflavonoid

Hesperetin reduces or inhibits the activity of acyl-coenzyme A cholesterol acyltransferase genes (ACAT1 and ACAT2) and it reduces microsomal triglyceride transfer protein (MTP) activity. Hesperetin also seems to upregulate the LDL receptor. This leads to the reduced assembly and secretion of apoB-containing lipoproteins and enhanced reuptake of those lipoproteins, thereby lowering cholesterol levels. Hesperetin is a cholesterol-lowering flavonoid found in a number of citrus juices. It appears to reduce cholesteryl ester mass and inhibit apoB secretion by up to 80%. Hesperetin may have antioxidant, anti-inflammatory, anti-allergic, hypolipidemic, vasoprotective and anticarcinogenic actions.

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Indications of Bioflavonoid

  • For lowering cholesterol  – and, possibly, otherwise favorably affecting lipids. In vitro research also suggests the possibility that hesperetin might have some anticancer effects and that it might have some anti-aromatase activity, as well as an activity again.
  • Beneficial effects on blood vessels – It’s touted as a natural remedy for a number of health problems, including allergies, hemorrhoids, high blood pressure, hot flashes, hay fever, sinusitis, symptoms associated with menopausal changes, premenstrual syndrome, and varicose veins. Hesperidin is also said to improve circulation, reduce inflammation, and help fight cancer.
  • Poor circulation can cause the legs to swell (chronic venous insufficiency or CVI) – Taking a particular product containing hesperidin methyl chalcone, butcher’s broom, and vitamin C by mouth seems to relieve the symptoms of poor circulation in the legs. Also, taking a different product containing hesperidin and diosmin by mouth for 2-6 months seems to improve CVI symptoms, although taking the drug Venoruton might be more effective for treating this condition.
  • Hemorrhoids – Some research suggests that taking hesperidin and diosmin improves symptoms of anal hemorrhoids. It may also prevent hemorrhoids from coming back after they have healed and may help in an emergency worsening of hemorrhoids.
  • Leg sores caused by weak blood circulation (venous leg ulcer) – Taking a specific product containing hesperidin and diosmin by mouth for 2 months seems to improve the healing of small venous stasis ulcers when used along with compression dressings.
  • High cholesterol Some research shows that taking hesperidin does not affect cholesterol.
  • Obesity – Some research shows that taking glucosyl hesperidin for 12 weeks does not reduce body weight in people that are modestly overweight.
  • Diabetes Early research suggests that taking one tablet of a specific product containing hesperidin and diosmin by mouth for 45 days decreases blood sugar levels and improves blood sugar control in women with type 2 diabetes. Other research suggests that taking hesperidin each day might lower blood pressure by a small amount in people with diabetes.
  • High blood pressure – Early research suggests that taking hesperidin by mouth or drinking orange juice containing hesperidin can decrease diastolic blood pressure (the bottom number) but does not decrease systolic blood pressure (the top number) in people with or without high blood pressure.
  • Swelling in the arms or legs caused by damage to the lymph system (lymphedema) – Early research suggests that taking a specific product containing butcher’s broom root extract, hesperidin methyl chalcone, and vitamin C by mouth for 90 days reduces swelling in the upper arm and forearm and improves mobility and heaviness in women with swelling of the arm after breast cancer treatment. However, other research shows that taking a different product containing hesperidin and diosmin by mouth does not reduce arm swelling in women following breast cancer surgery.
  • Rheumatoid arthritis (RA) – Early research suggests that drinking a beverage containing alpha-glucosyl hesperidin for 12 weeks improves symptoms of RA.
  • Varicose veins
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Contraindications of Bioflavonoid

  • a high amount of oxalic acid in the urine
  • iron metabolism disorder causing increased iron storage
  • sickle cell anemia
  • anemia from pyruvate kinase and G6PD deficiencies

Allergies

  • Ascorbic Acid (Vitamin C)
  • Rutin Analogues
  • Hesperidin

Side Effects Of Bioflavonoid

The most common

Common

  • unusual bruising,
  • unexplainable bruises
  • bruises that grow in size
  • nosebleeds
  • bleeding gums
  • bleeding from cuts that take a long time to stop
  • heavier than normal menstrual or vaginal bleeding
  • pink or brown urine
  • red or black stools
  • coughing up blood
  • vomiting blood

Less common

Dosage of Bioflavonoid

The following doses have been studied in scientific research

BY MOUTH

  • For poor circulation that can cause the legs to swell (chronic venous insufficiency or CVI) – A specific combination product containing hesperidin methyl chalcone 150 mg, butcher’s broom root extract 150 mg, and ascorbic acid 100 mg has been used. Also, a combination of 100-150 mg of hesperidin with 900-1350 mg of diosmin taken daily for 2-6 months has been used.
  • For hemorrhoids – A combination of 150 mg of hesperidin plus 1350 mg of diosmin twice daily for 4 days, followed by 100 mg of hesperidin and 900 mg of diosmin twice daily for 3 days has been used. Also, a combination of 50 mg of hesperidin plus 450 mg of diosmin twice daily for 3 months has been used to prevent the return of hemorrhoids.
  • For sores caused by weak blood circulation (venous leg ulcer) – A combination of 100 mg of hesperidin and 900 mg of diosmin daily for up to 2 months has been used.
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Drug Interactions of Bioflavonoid

Hesperidin might decrease blood pressure. Taking hesperidin along with medications used to lower high blood pressure might cause your blood pressure to go too low.

  • nifedipine (Adalat, Procardia), verapamil (Calan, Isoptin, Verelan), diltiazem (Cardizem), isradipine (DynaCirc), felodipine (Plendil), amlodipine (Norvasc), and others.
  • etoposide, paclitaxel, vinblastine, vincristine, vindesine, ketoconazole, itraconazole, amprenavir, indinavir, nelfinavir, saquinavir, cimetidine, ranitidine, diltiazem, verapamil, corticosteroids, erythromycin, cisapride (Propulsid), fexofenadine (Allegra), cyclosporine, loperamide (Imodium), quinidine, and others.
  • aspirin, clopidogrel (Plavix), diclofenac (Voltaren, Cataflam, others), ibuprofen (Advil, Motrin, others), naproxen (Anaprox, Naprosyn, others), dalteparin (Fragmin), enoxaparin (Lovenox), heparin, warfarin (Coumadin), and others.
  • include alprazolam (Xanax), clonazepam (Klonopin), diazepam (Valium), lorazepam (Ativan), midazolam (Versed), temazepam (Restoril), triazolam (Halcion), and others.
  • pentobarbital (Nembutal), phenobarbital (Luminal), secobarbital (Seconal), thiopental (Pentothal), fentanyl (Duragesic, Sublimaze), morphine, propofol (Diprivan), and others.

Pregnancy Category of Bioflavonoid

Pregnancy and breast-feeding

  • Hesperidin is POSSIBLY SAFE for pregnant or breast-feeding women when taken by mouth with diosmin.

Bleeding disorder

Hesperidin might slow blood clotting and increase the risk of bleeding. In theory, hesperidin might make bleeding disorders worse.  Hesperidin might lower blood pressure. In theory, taking hesperidin might make blood pressure become too low in people who already have low blood pressure. Hesperidin might prolong bleeding. There is concern that hesperidin might increase the risk of bleeding during and after surgical procedures. Stop taking hesperidin at least 2 weeks before a scheduled surgery.

References

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