Luteolin

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Luteolin flavonoid health benefit

January 2 2016 by Ray Sahelian, M.D.
Luteolin is a flavonoid, and more precisely one of the citrus bioflavonoids. Just like most flavonoids,
it has antioxidant, anti-inflammatory, and anti-tumor properties. It is found in high amounts in
parsley, thyme, peppermint, basil herb, celery and artichoke.
Among these phytochemicals, dietary flavonoids are an important and common chemical class of
bioactive products, found in several fruits and vegetables. Luteolin is an important flavone, which is
found in several plant products, including broccoli, pepper, thyme, and celery. Numerous studies
have shown that luteolin possesses beneficial neuroprotective effects both in vitro and in vivo.
Q. Your site give the appearance that parsley is highest in anti luteolin but in other sources it
appears that celery is highest?
A. I am not sure which is highest but it is not of great importance since both celery and parsley
have many other compounds that have health benefits and focusing on just one substance does
not do them justice as to their overall health benefits. One should have a wide variety of
condiments and vegetables in their diet.
How it works
Luteolin exerts a variety of pharmacological activities and anti-oxidant properties associated with its
capacity to scavenge oxygen and nitrogen species. It also shows potent anti-inflammatory activities
by inhibiting nuclear factor kappa B (NFkB) signaling in immune cells.
Luteolin and brain inflammation
University of Illinois researchers report lutelin, found in celery and green peppers, can disrupt a
component of the inflammatory response in the brain. Rodney Johnson of the University of Illinois
at Urbana-Champaign and graduate student Saebyeol Jang found that luteolin inhibits a key
pathway in the inflammatory response of microglia -- brain cells key to the body's immune defense.
Microglial cells exposed to luteolin show a significantly diminished inflammatory response and there
was reduced production of interleukin-6 -- used in cellular communication -- in the inflammatory
pathway.
Cancer prevention
Chem Biol Interact. 2014. Luteolin enhances paclitaxel-induced apoptosis in human breast cancer
MDA-MB-231 cells by blocking STAT3.
Oncol Rep. 2014. Protective effect of luteolin on cigarette smoke extractinduced cellular toxicity
and apoptosis in normal human bronchial epithelial cells via the Nrf2 pathway.
J Environ Pathol Toxicol Oncology. 2013. Luteolin induces growth arrest in colon cancer cells
through involvement of Wnt/-catenin/GSK-3 signaling.
Research
Decreased pro-inflammatory cytokine production by LPS-stimulated PBMC upon in vitro incubation
with the flavonoids apigenin, luteolin or chrysin, due to selective elimination of
monocytes/macrophages.
Biochem Pharmacol. 2005.
Apigenin and its structural analogues chrysin and luteolin were used to evaluate their capacity to
inhibit the production of pro-inflammatory cytokines by lipopolysaccharide (LPS)-stimulated human

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peripheral blood mononuclear cells (PBMC). Furthermore, flowcytometric analysis was performed
to compare the effects of apigenin, chrysin, luteolin, quercetin and naringenin on the different cell
types present in PBMC. LPS-stimulated PBMC were cultured in the presence of the flavonoids and
TNFalpha, IL-1beta and IL-6 were measured in the supernatants. In parallel, metabolic activity of
the PBMC was determined by measuring succinate dehydrogenase activity. Apigenin, chrysin and
luteolin dose-dependently inhibited both pro-inflammatory cytokine production and metabolic
activity of LPS-stimulated PBMC. With increasing concentration of apigenin, chrysin or luteolin the
monocytes/macrophages disappeared as measured by flowcytometry. This also appeared to occur
in the non-LPS-stimulated PBMC. At the same time there was an increase in dead cells. T- and
B-lymphocytes were not affected. Quercetin and naringenin had virtually no effects on cytokines,
metabolic activity or on the number of cells in the studied cell populations. In conclusion,
monocytes were specifically eliminated in PBMC by apigenin, chrysin or luteolin treatment in vitro
at low concentrations (around 8 microM), in which apigenin appeared to be the most potent.
The flavones luteolin and apigenin inhibit in vitro antigen-specific proliferation and
interferon-gamma production by murine and human autoimmune T cells.
Biochem Pharmacol. 2004.
Plant-derived flavonoids are inhibitors of various intracellular processes, notably phosphorylation
pathways, and potential inhibitors of cellular autoimmunity. In this study, the inhibiting effects of
various flavonoids on antigen-specific proliferation and interferon-gamma (IFN-gamma) production
by human and murine autoreactive T cells were evaluated in vitro. T-cell responses were evaluated
for the human autoantigen alpha B-crystallin, a candidate autoantigen in multiple sclerosis, and for
the murine encephalitogen proteolipid protein peptide PLP (139-151). The flavones apigenin and
luteolin were found to be strong inhibitors of both murine and human T-cell responses while fisitin,
quercitin, morin and hesperitin, members of the subclasses of flavonoles and flavanones, were
ineffective. Antigen-specific IFN-gamma production was reduced more effectively by flavones than
T-cell proliferation, suggesting that the intracellular pathway for IFN-gamma production in T cells is
particularly sensitive to flavone inhibition. These results indicate that flavones but not flavanoles or
flavanones are effective inhibitors of the potentially pathogenic function of autoreactive T cells. The
effects of flavones were the same for human and murine autoreactive T cells, stressing the
usefulness of animal models of autoimmunity for further studies on the effects of flavonones on
autoimmune diseases.
Determination of free radical scavenging activity of quercetin, rutin, luteolin and apigenin in
H2O2-treated human ML cells K562.
Neoplasma. 2004.
We investigated protective effects of four flavonoids against H2O2- induced DNA damage in human
myelogenous leukemia cells (K562) using the comet assay. The structural difference of studied
flavonoids -- quercetin, rutin, luteolin and apigenin -- are characterized by the number of hydroxyl
groups on the B ring. The presence of an o-dihydroxy structure on the B-ring confers a higher
degree of stability to the flavonoid phenoxyl radicals by participating in electron delocalization and
is, therefore, an important determinant for antioxidative potential. The results correlate with earlier
published data obtained in murine leukemia cell line L1210. Hydrogen peroxide induced in human
K562 cells a concentration-dependent increase of single cell DNA strand breaks. The strongest
inhibition against H2O2-induced DNA damage (44%, 42%) was found in a range of luteolin and
quercetin concentrations of 20-100 micromol/l. Protective effect of rutin was only marginal (8-10%).
Apigenin had no protective effect on DNA single strand breaks induced by H2O2. Luteolin and
quercetin are therefore effective in the protection of human single cell DNA from oxidative attack.
Flavonoids such as luteolin, fisetin and apigenin are inhibitors of interleukin-4 and interleukin-13

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production by activated human basophils.

Int Arch Allergy Immunol. 2004.
We have previously shown that fisetin, a flavonol, inhibits IL-4 and IL-13 synthesis by allergen- or
anti-IgE-antibody-stimulated basophils. This time, we investigated the inhibition of IL-4 and IL-13
production by basophils by other flavonoids. We additionally investigated whether flavonoids
suppress leukotriene C4 synthesis by basophils and IL-4 synthesis by T cells in response to
anti-CD3 antibody. Highly purified peripheral basophils were stimulated for 12 h with anti-IgE
antibody alone or anti-IgE antibody plus IL-3 in the presence of various concentrations of 18
different kinds of flavones and flavonols. IL-4 and IL-13 concentrations in the supernatants were
then measured. Leukotriene C4 synthesis was also measured after basophils were stimulated for 1
h in the presence of flavonoids. Regarding the inhibitory activity of flavonoids on IL-4 synthesis by T
cells, peripheral blood mononuclear cells were cultured with flavonoids in anti-CD3-antibody-bound
plates for 2 days. Luteolin, fisetin and apigenin were found to be the strongest inhibitors of both IL-4
and IL-13 production by basophils but did not affect leukotriene C4 synthesis. At higher
concentrations, these flavonoids suppressed IL-4 production by T cells. Based on a hierarchy of
inhibitory activity, the basic structure for IL-4 inhibition by basophils was determined. Due to the
inhibitory activity of flavonoids on IL-4 and IL-13 synthesis, it can be expected that the intake of
flavonoids, depending on the quantity and quality, may ameliorate allergic symptoms or prevent the
onset of allergic diseases.
Characteristic rat tissue accumulation of nobiletin, a chemopreventive polymethoxyflavonoid, in
comparison with luteolin.
Biofactors. 2002.
Nobiletin, a polymethoxyflavonoid, is an effective anti-inflammatory and chemopreventive
phytochemical found in citrus fruits. We compared the absorption and metabolism characteristics of
nobiletin with those of luteolin in male SD rats. Our results suggest that the metabolic properties of
polymethoxyflavonoids are distinct from those of other general flavonoids, because of their wide
distribution and accumulation in tissue.
Luteolin supplement questions
Q. Is it okay to take graviola or mangosteen while taking a luteolin supplement? What about
5-HTP?
A. These supplements are probably safe to take while taking luteolin, as long as the amounts
ingested are not excessive. 5-HTP is often taken in the evening, and luteolin is most often used in
the morning.
Q. I want to take luteolin for my immune system. Is the NOW product, Entrox, the best way to take
it? Is the amount of luteolin sufficient? Any other product that you would suggest? Could you share
that with me and the proper general dosage.
A. Each person's immune system is different and may respond differently to various herbs and
supplements. There has not been enough human studies with luteolin supplements to determine
the idea dosage or the long term side effects. See immune system for more information.

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