Apigenin: benefits, dosage, contraindications
Other name(s)
Apigenol, Biapigenin
Scientific name(s)
4',5,7-trihydroxyflavone
Family or group:
Phytochemicals
Indications
Scoring methodology
EFSA approval.
Anxiety ✪✪✪✪✪
Apigenin has anxiolytic effects at doses of 3 to 10 mg/kg of body weight. A sedative effect has been observed at doses three times higher (30 to 100 mg/kg of body weight). nnA clinical study in people with moderate to severe generalized anxiety disorder 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 treatment were randomized to continue with chamomile or a placebo for 26 weeks.nnThe results showed that chamomile was safe for long-term use and effectively reduced anxiety symptoms, but did not significantly reduce the risk of relapse. The limitations of this study, notably the small sample size and a lower-than-expected relapse rate in the placebo group, affected the results. nnMore rigorous studies are needed to better assess the effectiveness of chamomile and its active component — apigenin — against anxiety.nn
Posologie
Orally
3 - 10 mg/kg
dry extract
Apigenin, a component of Matricaria recutita flowers, is a central benzodiazepine receptors-ligand with anxiolytic effects.
Quercetin, kaempferol and biapigenin from Hypericum perforatum are neuroprotective against excitotoxic insults.
Under-eye circles ✪✪✪✪✪
Because of its vascular and anti-inflammatory effects, apigenin is an excellent active ingredient for treating vascular-colored dark circles. Vascular-colored dark circles are directly linked to the condition of the vascular network. A decrease in microcirculation leads to darker, more pronounced and more visible blood capillaries. The vascular walls then become less elastic and less tight, causing local dilation and blood stagnation. This stagnation leads to increased capillary permeability and leakage of blood from the capillaries into the interstitial space. Hemoglobin then accumulates in the infra-orbital area and is degraded by oxidation into biliverdin, bilirubin or iron. Biliverdin is a dark greenish-violet pigment and bilirubin an orange to dark reddish-brown pigment. They are responsible for this characteristic tired-looking discoloration under the eyes as they accumulate in the epidermis and dermis.
Posologie
Oral administration
gel, cream
Inhibition of mammalian collagenase, matrix metalloproteinase-1, by naturally-occurring flavonoids.
Suppression of inducible cyclooxygenase and inducible nitric oxide synthase by apigenin and related flavonoids in mouse macrophages
Cancer ✪✪✪✪✪
A study was conducted on the association between flavonoid consumption (quercetin, kaempferol, myricetin, luteolin, and apigenin) and lung cancer. The relationship between antioxidant flavonoid intake and the risk of subsequent cancer was studied in 9,959 Finnish men and women aged 15 to 99 years who were initially cancer-free. 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 as well as onions, which are sources of apigenin, have a protective role against lung cancer. Another study was conducted on the chemopreventive potential of apigenin in induced buccal pouch carcinogenesis. Apigenin was administered concurrently at a dose of 2.5 mg/kg body weight/day, starting one week before carcinogen exposure and continuing until the end of the experiment. The results showed that apigenin, compared with the control sample, prevented tumor formation.
Posologie
Orally
2.5 - 50 mg/kg
20 - weeks
dry extract
Properties
Anticancer
Apigenin is known as one of the bioflavonoid compounds that has a high selectivity for inducing 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 function of mitochondria, the cell's powerhouses, in a way that triggers apoptosis of cancer cells. This process involves the release of a substance called cytochrome C, which then activates a cascade leading to the destruction of the cancer cell. Like other bioflavonoid compounds, apigenin can reduce oxidative stress. Apigenin may decrease the activity of certain molecules that normally bind in response to oxidative stress, which is a defensive strategy against oxidative stress, such as the scavenging of free radicals. Apigenin also increases the production of enzymes that protect against cellular damage caused by oxidative stress, such as GSH-synthase, catalase, and SOD. Furthermore, apigenin has protective effects against damage that can lead to cancer. It also appears to prevent the spread of cancer (metastasis) and the formation of new blood vessels needed for tumor growth (angiogenesis). It acts by interacting with specific cellular signaling pathways known as the MAPK pathways.
Usages associés
Anti-inflammatory
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 COX2 enzyme helps produce substances called prostaglandins and thromboxane, which are involved in inflammatory processes. By inhibiting COX2, apigenin helps reduce inflammation. In addition, apigenin also limits the production of interleukin-4, another substance involved in inflammatory reactions.
Usages associés
Anxiolytic
Apigenin has anxiolytic effects but does not cause 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 the 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 from damage caused by overstimulation from excitatory neurotransmitters, a process known as excitotoxicity. Additionally, apigenin may also play a role in regulating an enzyme called MAO (monoamine oxidase). Abnormal activity of this enzyme is associated with various psychiatric and neurological disorders. By inhibiting this enzyme, apigenin could act as an antidepressant and reduce anxiety.
Usages associés
Microcirculatory effect
Apigenin exerts beneficial effects on blood vessels. It strengthens small blood vessels, called capillaries, by supporting the dermal matrix that surrounds them. In laboratory studies, apigenin has the ability to increase the solubility and elimination of certain substances that are difficult to dissolve in the body. Because of this property, it could promote the removal of pigments that form when hemoglobin, a protein in the blood, is degraded.
Usages associés
Hypoglycemic
The antidiabetic properties of apigenin can be attributed to its ability to inhibit the activity of α-glucosidase, an enzyme involved in carbohydrate digestion. It also helps increase insulin production, a well-known hormone that controls blood sugar levels. In addition, apigenin neutralizes certain harmful substances within cells, known as reactive oxygen species, which together help prevent diabetic complications. Finally, it provides a moderate level of nitric oxide to the cells of blood vessels, which may reduce damage caused by high blood glucose levels.
Neurological
Apigenin has antioxidant, anti-inflammatory, anti-amyloidogenic and neuroprotective properties. Apigenin exerts antioxidant effects by removing free radicals. In particular, apigenin has a neuroprotective effect against oxidative stress in neurological disorders, such as cerebral ischemia. It may also help prevent the formation of amyloid plaques, which are involved in the development of Alzheimer's disease. Apigenin is considered a promising substance to delay the onset of Alzheimer's disease or slow its progression.
Antiviral
Apigenin, alongside other flavonoids such as quercetin and rutin, has shown antiviral effects. These properties appear to be mainly associated with non-glycosylated flavonoid compounds, that is, those not bound to a sugar. In addition, the presence of a hydroxyl group (an oxygen and hydrogen atom) at a specific position on this class of molecules, namely position 3, seems to be essential for this antiviral activity
Safe dosage
Adults 18 years and older: 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 and nutrition program, which recommends five servings of fruits and vegetables each day, one ingests between 150 and 300 mg of flavonoids. The amount present in a food varies depending on the method of harvesting and preparation. Apigenin is a flavonoid found almost everywhere in plants. For example, chamomile is an important source of apigenin. Therapeutic use of flavonoids should be avoided in children.
Precautions
Pregnant women: avoid
Therapeutic use of flavonoids should be avoided in pregnant women.
Breastfeeding women: avoid
Therapeutic use of flavonoids should be avoided in breastfeeding women.
Children up to 18 years: avoid
No apparent toxicity has been reported for the doses found in food. Outside of normal dietary intake, taking apigenin should be avoided in children.
