Luteolin
Encyclopedia
Luteolin is a yellow crystalline compound. It is a flavonoid
Flavonoid
Flavonoids , are a class of plant secondary metabolites....

; to be specific, it is one of the more common flavones
Flavones
Flavones , are a class of flavonoids based on the backbone of 2-phenylchromen-4-one shown on the right....

. From preliminary research, it is thought to play a role in the human body possibly as an antioxidant
Antioxidant
An antioxidant is a molecule capable of inhibiting the oxidation of other molecules. Oxidation is a chemical reaction that transfers electrons or hydrogen from a substance to an oxidizing agent. Oxidation reactions can produce free radicals. In turn, these radicals can start chain reactions. When...

, a free radical scavenger, a promoter of carbohydrate
Carbohydrate
A carbohydrate is an organic compound with the empirical formula ; that is, consists only of carbon, hydrogen, and oxygen, with a hydrogen:oxygen atom ratio of 2:1 . However, there are exceptions to this. One common example would be deoxyribose, a component of DNA, which has the empirical...

 metabolism, or an immune system
Immune system
An immune system is a system of biological structures and processes within an organism that protects against disease by identifying and killing pathogens and tumor cells. It detects a wide variety of agents, from viruses to parasitic worms, and needs to distinguish them from the organism's own...

 modulator. If applicable to the human condition, these characteristics may inhibit cancer
Cancer
Cancer , known medically as a malignant neoplasm, is a large group of different diseases, all involving unregulated cell growth. In cancer, cells divide and grow uncontrollably, forming malignant tumors, and invade nearby parts of the body. The cancer may also spread to more distant parts of the...

 mechanisms. Basic research
Basic Research
Basic Research is an herbal supplement and cosmetics manufacturer based in Salt Lake City, Utah that distributes products through a large number of subsidiaries. In addition, their products are sold domestically and internationally through a number of high-end retailers. Dennis Gay is the...

 results indicate luteolin as an anti-inflammatory
Anti-inflammatory
Anti-inflammatory refers to the property of a substance or treatment that reduces inflammation. Anti-inflammatory drugs make up about half of analgesics, remedying pain by reducing inflammation as opposed to opioids, which affect the central nervous system....

 agent with other potential effects on septic shock
Septic shock
Septic shock is a medical emergency caused by decreased tissue perfusion and oxygen delivery as a result of severe infection and sepsis, though the microbe may be systemic or localized to a particular site. It can cause multiple organ dysfunction syndrome and death...

. It has been suggested for multiple sclerosis
Multiple sclerosis
Multiple sclerosis is an inflammatory disease in which the fatty myelin sheaths around the axons of the brain and spinal cord are damaged, leading to demyelination and scarring as well as a broad spectrum of signs and symptoms...

 on the basis of in vitro work.

Luteolin is most often found in leaves, but it is also seen in celery, thyme, dandelion, rinds, bark
Bark
Bark is the outermost layers of stems and roots of woody plants. Plants with bark include trees, woody vines and shrubs. Bark refers to all the tissues outside of the vascular cambium and is a nontechnical term. It overlays the wood and consists of the inner bark and the outer bark. The inner...

s, clover
Clover
Clover , or trefoil, is a genus of about 300 species of plants in the leguminous pea family Fabaceae. The genus has a cosmopolitan distribution; the highest diversity is found in the temperate Northern Hemisphere, but many species also occur in South America and Africa, including at high altitudes...

 blossom, and ragweed
Ragweed
Ragweeds are flowering plants in the genus Ambrosia in the sunflower family Asteraceae. Common names include bitterweeds and bloodweeds....

 pollen. It has also been isolated from Salvia
Salvia
Salvia is the largest genus of plants in the mint family, Lamiaceae, with approximately 700-900 species of shrubs, herbaceous perennials, and annuals. It is one of several genera commonly referred to as sage. When used without modifiers, sage generally refers to Salvia officinalis ; however, it is...

 tomentosa
.
Dietary sources include celery, green pepper, thyme, perilla
Perilla
Perilla is the common name of the herbs of the genus Perilla of the mint family, Lamiaceae. In mild climates, the plant reseeds itself. There are both green-leafed and purple-leafed varieties, which are generally recognized as separate species by botanists. The leaves resemble stinging nettle...

, chamomile
Chamomile
Chamomile or camomile is a common name for several daisy-like plants of the family Asteraceae. These plants are best known for their ability to be made into an infusion which is commonly used to help with sleep and is often served with either honey or lemon. Because chamomile can cause uterine...

 tea, carrots, olive oil, peppermint, rosemary, navel oranges, and oregano.

Luteolin acts as a monoamine transporter
Monoamine transporter
Monoamine transporters are protein structures that function as integral plasma membrane transporters to regulate concentrations of extracellular monoamine neurotransmitters. Three major classes of MATs are responsible for the reuptake of their associated amine neurotransmitters...

 activator, and is one of the few chemicals demonstrated to possess this property.

Glycosides

  • Orientin
    Orientin
    Orientin is a flavone, a chemical flavonoid-like compound found in the passion flower, the Açaí palm, in Adonis vernalis and Anadenanthera peregrina. Orientin is also reported in millets and in the Phyllostachys nigra bamboo leaves....

    , the 8-C glucoside of luteolin
  • Isoorientin, the 6-C glucoside
  • Luteolin-7-glucoside (Cynaroside
    Cynaroside
    Cynaroside is a flavone, a flavonoid-like chemical compound. It is a 7-O-glucoside of luteolin and can be found in dandelion coffee, in Ferula varia and F. foetida in Campanula persicifolia and C...

    ) and Luteolin-7-diglucoside found in dandelion coffee
    Dandelion coffee
    Dandelion coffee is an infusion or herbal tea, and coffee substitute, made from the root of the dandelion plant. The roasted dandelion root pieces and the beverage have some resemblance to coffee in appearance and taste.-History:...

  • Luteolin-7-rutinoside (Veronicastroside)

Mechanism of action

Luteolin is a PDE4 inhibitor
PDE4 inhibitor
A phosphodiesterase type 4 inhibitor, commonly referred to as a PDE4 inhibitor, is a drug used to block the degradative action of phosphodiesterase 4 on cyclic adenosine monophosphate . It is a member of the larger family of PDE inhibitors. The PDE4 family of enzymes are the most prevalent PDE in...

 and a general phosphodiesterase inhibitor
Phosphodiesterase inhibitor
A phosphodiesterase inhibitor is a drug that blocks one or more of the five subtypes of the enzyme phosphodiesterase , therefore preventing the inactivation of the intracellular second messengers cyclic adenosine monophosphate and cyclic guanosine monophosphate by the respective PDE...

, and an Interleukin 6
Interleukin 6
Interleukin-6 is a protein that in humans is encoded by the IL6 gene.IL-6 is an interleukin that acts as both a pro-inflammatory and anti-inflammatory cytokine. It is secreted by T cells and macrophages to stimulate immune response, e.g. during infection and after trauma, especially burns or other...

 inhibitor.

It significantly reversed the xylazine
Xylazine
Xylazine is a drug that is used for sedation, anesthesia, muscle relaxation, and analgesia in animals such as horses, cattle and other non-human mammals. An analogue of clonidine, it is an agonist at the α2 class of adrenergic receptor....

/ketamine
Ketamine
Ketamine is a drug used in human and veterinary medicine. Its hydrochloride salt is sold as Ketanest, Ketaset, and Ketalar. Pharmacologically, ketamine is classified as an NMDA receptor antagonist...

-induced anesthesia in mice.

Preclinical studies have shown that luteolin may possess pharmacological activities, including antioxidant, anti-inflammatory, antimicrobial, and anticancer activities. From preliminary research, the ability of luteolin to inhibit angiogenesis, to induce apoptosis, to affect carcinogenesis in animal models, to possibly reduce tumor growth in vivo, and to sensitize tumor cells to the cytotoxic effects of some anticancer drugs suggests that this flavonoid may have cancer chemopreventive and chemotherapeutic potential. Modulation of ROS levels, inhibition of topoisomerases I and II, reduction of NFkappaB and AP-1 activity, stabilization of p53, and inhibition of PI3K, STAT3, IGF1R, and HER2 are possible mechanisms involved in the putative biological activities of luteolin.

Side-effects

Gastrointestinal adverse effects, such as nausea, vomiting and gastric hypersecretion, may occur.
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