Herbs & Supplements:
Citrus Bioflavonoids
Supplement Forms / Alternate Names
•
Diosmetin, Diosmin, Hesperidin, Naringin, Narirutin, Neohesperidin, Nobiletin, Rutin, Tangeretin, Bioflavonoid
Principal Proposed Uses
•
Hemorrhoids, Chronic Venous Insufficiency
Other Proposed Uses
•
Easy Bruising, Nosebleeds, Lymphedema Following Breast Cancer Surgery
Citrus fruits are well known for providing ample amounts of vitamin C. But they also supply bioflavonoids, substances that are not required for life but that may improve health. The major bioflavonoids found in citrus fruits are diosmin, hesperidin, rutin, naringin, tangeretin, diosmetin, narirutin, neohesperidin, nobiletin, and quercetin.
This article addresses the first five bioflavonoids listed above. Please see the article on quercetin for information on this supplement. A modified form of rutin, oxerutin, is also discussed in its own article.
Citrus bioflavonoids and related substances are widely used in Europe to treat diseases of the blood vessels and lymph system, including hemorrhoids, chronic venous insufficiency, easy bruising, nosebleeds, and lymphedema following breast cancer surgery. These compounds are thought to work by strengthening the walls of blood vessels.
Requirements/Sources
Citrus fruits contain citrus bioflavonoids in varying proportions. Even different brands of citrus juice may vary widely in their bioflavonoid concentrations and composition.1 For use as a supplement, bioflavonoids are extracted either from citrus fruits or other plant sources, such as buckwheat.
Therapeutic Dosages
A typical dosage of citrus bioflavonoids is 500 mg twice daily. The most studied citrus bioflavonoid treatment is a special combination of diosmin (90%) and hesperidin (10%).
Therapeutic Uses
Double-blind trials suggest that a special micronized combination preparation of diosmin and hesperidin may be helpful for hemorrhoids.2–6
Diosmin and hesperidin, as well as the bioflavonoid rutin, may also be helpful for chronic venous insufficiency, a condition in which the veins in the legs begin to weaken.7–10,34,35
At least one good double-blind trial found diosmin and hesperidin also to be helpful for individuals who develop bruises or nosebleeds easily.13
Citrus bioflavonoids have also been tried, with some success, for treating lymphedema (arm swelling) following breast cancer surgery.14
Note: Do not use bioflavonoid combinations containing tangeretin if you are taking tamoxifen for breast cancer.
In addition, highly preliminary evidence suggests that citrus bioflavonoids may help reduce cholesterol levels,15,16 control inflammation,17 benefit individuals with diabetes,18 reduce allergic reactions,19 and prevent cancer.20
What Is the Scientific Evidence for Citrus Bioflavonoids?
Hemorrhoids
A 2-month double-blind placebo-controlled trial of 120 individuals with recurrent hemorrhoid flare-ups found that treatment with combined diosmin and hesperidin significantly reduced the frequency and severity of hemorrhoid attacks.21 Another double-blind placebo-controlled trial of 100 individuals had positive results with the same bioflavonoids in relieving symptoms once a flare-up of hemorrhoid pain had begun.22 A 90-day double-blind trial of 100 individuals with bleeding hemorrhoids also found significant benefits for both treatment of acute attacks and prevention of new ones.23 Finally, this bioflavonoid combination was found to compare favorably with surgical treatment of hemorrhoids.24 However, less impressive results were seen in a double-blind placebo-controlled study in which all participants were given a fiber laxative with either combined diosmin and hesperidin or placebo.25
Chronic Venous Insufficiency
A two-month, double-blind, placebo-controlled trial of 200 individuals with relatively severe chronic venous insufficiency found that treatment with diosmin/hesperidin significantly improved symptoms as compared to placebo.34
Another double-blind, placebo-controlled trial of diosmin/hesperidin enrolled 101 individuals with relatively mild chronic venous insufficiency.35 The results showed little difference between the two groups; the authors theorize that diosmin/hesperidin might be generally more effective in severe chronic venous insufficiency.
A 2-month, double-blind, placebo-controlled trial evaluated the effects of diosmin/hesperidin in 107 individuals with nonhealing leg ulcers (sores) caused by venous insufficiency or other conditions.26 The results indicated that treatment significantly improved the rate of healing.
Also, a 3-month, double-blind, placebo-controlled trial of 67 individuals evaluated buckwheat tea (a good source of rutin) for chronic venous insufficiency.27 The results showed less leg swelling in the treated group.
Easy Bruising
Some individuals bruise particularly easily due to fragile capillaries. A 6-week double-blind placebo-controlled study of 96 people with this condition found that combined diosmin and hesperidin decreased symptoms of capillary fragility, such as bruising and nosebleeds.28
Two rather poorly designed studies from the 1960s found benefits with a combination of vitamin C and citrus bioflavonoids for decreasing bruising in collegiate athletes.29
Safety Issues
Extensive investigations of diosmin and hesperidin have found them to be essentially nontoxic and free of drug interactions.30 The combination has been given to 50 pregnant women in a research study, without apparent harm to mothers or babies.31
However, the citrus bioflavonoid tangeretin appears to interfere with the action of tamoxifen, a drug used to treat breast cancer.32
One highly preliminary study suggests that citrus bioflavonoids in the diet of pregnant women might increase the risk of infant leukemia; however, hesperidin did not produce this effect, and diosmin was not tested.33
Interactions You Should Know About
If you are taking tamoxifen for breast cancer, you should avoid citrus fruits and juices and the citrus bioflavonoid tangeretin.
View References
Last reviewed April 2002 by Medical Review Board
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