Apigenin: Benefits, Dosage, Contraindications

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Apigenin is a natural flavonoid found in fruits (grapefruit, oranges), vegetables (onion, celery), herbs (parsley, oregano, thyme, rosemary...) and plant-based beverages (tea, wine). One of the most common sources of apigenin consumption is chamomile, which contains about 0.8 to 1.2% by weight of apigenin. In foods and medicinal plants, active apigenin is found in the form of various acylated derivatives and apigenin-7-O-glucoside. It is unstable on its own but remains stable when consumed via foods and plants. Researchers have found that apigenin plays a role in gene regulation, which results in the restoration of programmed cell death of cancer cells (process also known as apoptosis). Several studies highlight its promising potential as an anticancer agent. However, apigenin has very low water solubility, limiting its application and clinical studies. Additionally, apigenin, at non-dietary doses, is not currently available in dietary supplements. Only cosmetic use is authorized. Apigenin remains a treasure of nature and possesses several properties. It is, for example, antioxidant, anti-hyperglycemic, anti-inflammatory, as well as being anti-carcinogenic. It also has neuroprotective effects against depression and anxiety. Everyone knows the benefits of chamomile - a major source of apigenin - for calming the mind!

Other name(s) 

Apigenol, Biapigenin

Scientific name(s)

4 ', 5, 7, -trihydroxyflavone

Family or group: 

Phytosubstances


Indications

Rating methodology

EFSA approval.

Several clinical trials (> 2) randomized controlled with double blind, including a significant number of patients (>100) with consistently positive outcomes for the indication.
Several clinical trials (> 2) randomized controlled with double blind, and including a significant number of patients (>100) with positive outcomes for the indication.
One or more randomized studies or multiple cohorts or epidemiological studies with positive outcomes for the indication.
Clinical studies exist but are uncontrolled, with conclusions that may be positive or contradictory.
Lack of clinical studies to date that can demonstrate the indication.


Anxiety
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Apigenin has anxiolytic effects at doses of 3 to 10 mg / kg of body weight. A sedative effect has been observed at doses 3 times higher (30 to 100 mg / kg of body weight). A clinical study on individuals with moderate to severe generalized anxiety was conducted in two phases. In the first phase, participants took a pharmaceutical-grade chamomile extract (1500 mg per day, divided into three capsules) for 12 weeks. In the second phase, those who responded to the treatment were randomly assigned to continue with chamomile or a placebo for 26 weeks. The results showed that chamomile was safe long-term and effectively reduced anxiety symptoms, but did not significantly decrease the risk of relapse. The limitations of this study, including the small sample size and a lower than expected relapse rate in the placebo group, influenced the results. More qualitative studies are needed to better evaluate the effectiveness of chamomile and its active component - apigenin - against anxiety.

Posologie

posologieOral

posologie3 - 10 mg/kg

formulationDry extract


Dark circles
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Due to its vascular and anti-inflammatory effects, apigenin is an excellent agent for the treatment of vascular-colored dark circles. Indeed, vascular-colored dark circles are directly linked to the state of the blood network. A decrease in microcirculation translates into darker, more pronounced, and more visible blood vessels. The vascular walls become less elastic and less watertight, leading to local dilation and blood stagnation. This blood stagnation results in capillary permeability and blood leakage from capillaries into the interstitial space. Hemoglobin then accumulates in the infraorbital area and degrades by oxidation into biliverdin, bilirubin, or iron. Biliverdin is a dark green-purple pigment and bilirubin is an orange to dark reddish-brown pigment. They are responsible for this characteristic color of fatigue under our eyes by accumulating in the epidermis and dermis.

Posologie

posologieOrally

formulationgel, cream


Cancer
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A study was conducted on the association between the consumption of flavonoids (quercetin, kaempferol, myricetin, luteolin, and apigenin) and lung cancer. The relationship between antioxidant flavonoid intake and subsequent cancer risk was studied in 9,959 Finnish men and women aged 15 to 99 years initially without cancer. They found an inverse association between flavonoid intake and the incidence of all cancer sites, which also provides strong evidence for the protective role of flavonoids against lung cancer. The authors concluded that apples and onions, which are sources of apigenin, play a protective role against lung cancer. Another study was conducted on the chemopreventive potential of apigenin during 7,12-dimethylbenz[a]anthracene-induced oral carcinogenesis. Apigenin was administered simultaneously at a dose of 2.5 mg/kg body weight/day, starting one week before carcinogen exposure and continuing to the end of the experiment. The results showed that apigenin, compared to the control group, prevented tumor formation.

Posologie

posologieOrally

posologie2.5 - 50 mg/kg

duration20 - weeks

formulationdry extract


Properties


Anticancer

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Apigenin is known as one of the bioflavonoid compounds that has a high selectivity to induce selective programmed cell death (apoptosis) of cancer cells in vivo. Apigenin induces cell cycle arrest at different stages of proliferation. It acts by modifying the activity of certain proteins and genes involved in cell growth. It also has the ability to influence the functioning of mitochondria, the energy powerhouses of cells, in a way that triggers apoptosis of cancer cells. This process involves the release of a substance called cytochrome C, which then activates a chain reaction leading to the destruction of the cancer cell. Like other bioflavonoid compounds, apigenin can reduce oxidative stress. Apigenin might decrease the activity of certain molecules that normally bind in response to oxidative stress, which is a defense strategy against oxidative stress, such as trapping free radicals. Apigenin also increases the production of enzymes that protect against cell damage caused by oxidative stress, such as GSH-synthase, catalase, and SOD enzymes. Moreover, apigenin has protective effects against damage that can lead to cancer. It also seems to prevent cancer spread (metastasis) and the formation of new blood vessels necessary for tumor growth (angiogenesis). It acts by interacting with specific cell signaling pathways, known as MAPK pathways.

Usages associés

Cancer

Anti-inflammatory

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Apigenin has anti-inflammatory properties. It works by preventing the production of an enzyme called COX2 in macrophages, which are a type of immune cell. Normally, the enzyme COX2 helps create substances called prostaglandins and thromboxane, which are involved in inflammatory processes. By inhibiting COX2, apigenin helps reduce inflammation. Additionally, apigenin also limits the production of interleukin-4, another substance involved in inflammatory reactions.

Usages associés

Dark circles

Anxiolytic

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Apigenin has anxiolytic effects without causing muscle relaxation or drowsiness at normal doses. It acts as a type of molecule that binds to the same receptors in the brain as common anxiolytic drugs (benzodiazepines), particularly to GABA-A receptors. However, at higher doses, apigenin can cause drowsiness. Furthermore, when present in a particular form called biapigenin, apigenin can protect nerve cells against damage caused by overstimulation from excitatory neurotransmitters, a process known as excitotoxicity. Moreover, apigenin may also play a role in regulating an enzyme named MAO (MonoAmine Oxidase). Abnormal activity of this enzyme is associated with various psychiatric and neurological disorders. By inhibiting this enzyme, apigenin might act as an antidepressant and reduce anxiety.

Usages associés

Anxiety

Microcirculatory effect

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Apigenin exerts benefits on blood vessels. It strengthens small blood vessels, called capillaries, by supporting the dermal matrix surrounding them. In laboratory studies, apigenin has the capacity to increase the solubility and elimination of certain substances that are difficult to dissolve in the body. Thanks to this property, it could promote the elimination of pigments formed when hemoglobin, a protein in the blood, is degraded.

Usages associés

Dark circles

Hypoglycemic

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The antidiabetic properties of apigenin can be attributed to its ability to inhibit the activity of α-glucosidase, an enzyme involved in the digestion of carbohydrates. It also helps increase insulin production, a well-known hormone that controls blood sugar levels. Additionally, apigenin neutralizes certain harmful substances in cells, known as reactive oxygen species, which together contribute to preventing diabetic complications. Finally, it provides a moderate level of nitric oxide to blood vessel cells, which can reduce the damage caused by high blood sugar in the blood.


Neurological

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Apigenin possesses antioxidant, anti-inflammatory, anti-amyloidogenic, and neuroprotective properties. Apigenin exerts antioxidant effects by eliminating free radicals. In particular, apigenin has a neuroprotective effect against oxidative stress in neurological disorders, such as cerebral ischemia. It can also help prevent the formation of amyloid plaques, which are involved in the genesis of Alzheimer's disease. Apigenin is considered a promising substance for delaying the onset of Alzheimer's disease or slowing its progression.


Antiviral

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Apigenin, along with other flavonoids like quercetin and rutin, has shown antiviral effects. These properties seem to be mainly associated with non-glycosidic flavonoid compounds, that is, those not bound to a sugar. Additionally, the presence of a hydroxyl group (an oxygen and hydrogen molecule) in a specific position on this class of molecules, specifically position 3, appears to be essential to this antiviral activity.


Safety dosage

Adult from 18 years: 150 mg - 300 mg

No apparent toxicity has been reported for the doses found in food. When following the official recommendations of the national health nutrition program, which advocates five servings of fruits and vegetables every day, one ingests between 150 and 300 mg of flavonoids. The amount present in food varies according to the method of harvest and preparation. Apigenin is a flavonoid found almost everywhere in plants. For example, chamomile is an important source of apigenin. The therapeutic use of flavonoids should be avoided in children.


Precautions

Pregnant woman: avoid

The therapeutic use of flavonoids should be avoided in pregnant women.

Breastfeeding woman: avoid

The therapeutic use of flavonoids should be avoided in breastfeeding women.

Child up to 18 years: avoid

No apparent toxicity has been reported for the doses found in food. Apart from normal food intake, the use of apigenin should be avoided in children.