Citrus Bioflavonoids supplement health benefit by Ray Sahelian, M.D.
April 8 2015

Bioflavonoids are a group of plant pigments that are responsible for the colors of many flowers and fruits. Citrus bioflavonoids are those bioflavonoids, or flavonoids, found in citrus fruits such as lemon, orange, tangerine, grapefruit, etc. These substances possess antioxidant activities, which help fight poor health and aging.

Citrus bioflavonoids have been investigated for their biological activity, with both anti-inflammatory and -carcinogenic effects being reported. Flavonoids are a subset of a larger group of beneficial plant substances known as polyphenols.

The common citrus bioflavonoids include:
Apigenin -- found in high amounts in parsley, thyme, and peppermint and many other herbs including lemon balm.
Hesperidin -- found in citrus peel and pulp. Commercial orange juice provides 440 mg/l hesperidin.
Hesperitin --
Narirutin -- commercial orange juice provides 96 mg narirutin per liter.
Nobiletin -- a citrus bioflavonoid isolated from tangerines
Quercetin is found in high amounts in onions, kale, hot peppers, and rutabagos.
Rutin is chemically related to quercetin.


Heart and blood vessel health
Curr Opin Lipidol. 2013 Feb. Citrus flavonoids and lipid metabolism. Citrus bioflavonoids are polyphenolic compounds with powerful biological properties. This review aims to summarize recent advances towards understanding the ability of citrus flavonoids to regulate lipid metabolism and other metabolic parameters relevant to the metabolic syndrome, type 2 diabetes and cardiovascular disease. Recent studies suggest an important role of citrus flavonoids in the treatment of dyslipidemia, insulin resistance, hepatic steatosis, obesity and atherosclerosis. The favorable outcomes are achieved through multiple mechanisms. Human studies focused on dose, bioavailability, efficacy and safety are required to propel the use of these promising therapeutic agents into the clinical arena.

Skin health
J Photochem Photobiol B. 2014. Protective effects of citrus and rosemary extracts on UV-induced damage in skin cell model and human volunteers. Ultraviolet radiation absorbed by the epidermis is the major cause of various cutaneous disorders, including photoaging and skin cancers. Although topical sunscreens may offer proper skin protection, dietary plant compounds may significantly contribute to lifelong protection of skin health, especially when unconsciously sun UV exposed. A combination of rosemary and citrus bioflavonoids extracts was used to inhibit UV harmful effects on human HaCaT keratinocytes and in human volunteers after oral intake. Survival of HaCaT cells after UVB radiation was higher in treatments using the combination of extracts than in those performed with individual extracts, indicating potential synergic effects. The combination of extracts also decreased UVB-induced intracellular radical oxygen species (ROS) and prevented DNA damage in HaCaT cells by comet assay and decreased chromosomal aberrations in X-irradiated human lymphocytes. The oral daily consumption of 250 mg of the combination by human volunteers revealed a significant minimal erythema dose (MED) increase after eight weeks. Stronger protection was achieved after 12 weeks. The combination of citrus flavonoids and rosemary polyphenols and diterpenes may be considered as an ingredient for oral photoprotection.

Eyesight Rx with Citrus Bioflavonoids
Improves day and night vision

Unlike some vision products that provide nutrients and herbs for long term healthy eyesight support, and prevention of visual impairment, but don't seem to have much of an immediate effect on visual acuity, Eyesight Rx was formulated to provide a noticeable eyesight improvement within days of use. Reports from Eyesight Rx users indicate enhanced clarity of vision, colors being brighter, better focus, and overall improvement in close and distance vision. Most people notice improved eyesight within a few days.


Vitamin C (Ascorbic acid)
Citrus bioflavonoids complex (eriocitrin, hesperidin, flavonols, flavones, flavonoids, naringenin, and quercetin)
Mixed carotenoids (alpha carotene, astaxanthin, beta carotene, cryptoxanthin,
Lutein, Lycopene, Zeaxanthin)
Bilberry extract (Vaccinium myrtillus)
Eyebright extract (Euphrasia officianales)
Jujube extract (Zizyphus jujube)
Ginkgo biloba (Ginkgo biloba)
Suma extract (Pfaffia paniculata)
Mucuna pruriens extract (Cowhage)
Cinnamon (Cinnamomum zeylanicum)
Lycium berry extract (Lycium Barbarum) also known as Goji Berry
Sarsaparila (Sarsaparilla Smilax)
Alpha Lipoic Acid comes in r lipoic and s lipoic versions

Citrus Bioflavonoid Research
Hesperidin, a citrus bioflavonoid, inhibits bone loss and decreases serum and hepatic lipids in ovariectomized mice.
J Nutr. 2003.
The purpose of this study was to examine whether hesperidin inhibits bone loss in ovariectomized mice (OVX), an animal model of postmenopausal osteoporosis. Hesperidin administration did not affect the uterine weight. These results suggest a possible role for citrus bioflavonoids in the prevention of lifestyle-related diseases because of their beneficial effects on bone and lipids.

Biological properties of citrus bioflavonoids pertaining to cancer and inflammation.
Curr Med Chem. 2001. US Citrus and Subtropical Products Laboratory, USDA, ARS, SAA, Winter Haven, FL
Citrus bioflavonoids encompass a diverse set of structures, including numerous flavanone and flavone O- and C-glycosides and methoxylated flavones. Each of these groups of compounds exhibits a number of in vitro and in vivo anti-inflammatory and anticancer actions. These biological properties are consistent with their effects on the microvascular endothelial tissue. Evidence suggests that the biological actions of the citrus flavonoids are possibly linked to their interactions with key regulatory enzymes involved in cell activation and receptor binding. The citrus bioflavonoids show little effect on normal, healthy cells, and thus typically exhibit remarkably low toxicity in animals. Citrus bioflavonoid extend their influence in vivo through their induction of hepatic phase I and II enzymes, and through the biological actions of their metabolites. Evidence clearly indicates to the potential health promoting properties of these dietary compounds.

Antiproliferative activities of citrus bioflavonoids against six human cancer cell lines.
J Agric Food Chem. 2002. U.S. Citrus and Subtropical Products Laboratory, South Atlantic Area, Agricultural Research Service, U.S. Department of Agriculture, Winter Haven, Florida
Citrus fruits contain high concentrations of several classes of phenols, including numerous hydroxycinnamates, flavonoid glycosides, and polymethoxylated flavones. The latter group of compounds occurs without glycosidic linkages and has been shown to inhibit the proliferation of a number of cancer cell lines. This antiproliferative property was further demonstrated against additional human cancer cell lines, and the antiproliferative actions of a series of synthetic methoxylated flavones were also studied. Similar to the naturally occurring compounds, the synthetic compounds exhibited strong antiproliferative activities. In many cases the IC(50) values occurred below 10 microm. Other hydroxylated flavone and flavanone aglycons also exhibited antiproliferative activities against the cancer cell lines, with the flavones showing greater activities than the flavanones. Glycosylation of these compounds removed their activity. The strong antiproliferative activities of the polymethoxylated flavones suggest that they may have use as anticancer agents in humans.

Citrus fruits are well known for providing ample amounts of vitamin C. But they also supply citrus 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. 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, leg ulcers, easy bruising, nosebleeds, and lymphedema following breast cancer surgery. Citrus bioflavonoids are thought to work by strengthening the walls of blood vessels.

Citrus bioflavonoid supplement questions
Q. You recommend cycling off of certain supplements. Would this apply to citrus bioflavonoid supplements? I have been taking citrus bioflavonoids for years and last year added a diosmin product for hemorrhoids. They work wonders, and would therefore like to continue taking them. Each day I take: TwinLab 700 mg. of Citrus Bioflavonoid Complex (containing 50% total bioflavonoids consisting of flavones (hesperidin, erocitrin, naringen and naringenin), flavanols and flavones), and rutin (50 mg.). Circulation and Vein Support: Total flavonoids: 320 mg. as Diosmin 300 mg. as Hesperidin 50 mg. as Rutin 10 mg as Quercetin 10 mg. Grape seed extract standardized to 90% polyphenols 20 mg. Silicon (from silicon dioxide/soluble organic silicon) 10 mg. Any suggestions would be greatly appreciated. In the meantime, I'll continue to read and learn from your research and wisdom.
   A. It is very difficult to know the long term benefits and side effects of taking citrus bioflavonoids and other supplements for many months and years since we have little or no human research to give us ideas. As a general rule, it is a good idea to take a day or two off each week from supplements and perhaps a week off every two or three months. But there are a number of factors that influence this guideline since each person has a completely different biochemistry and diet.