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Luteolin can be derived from many dietary sources but is especially high in radicchio. A supplement is an easy option though. Recently, low 50mg doses over 6 months has been shown to suppress activity of so called androgen receptors in low grade, early stage prostate cancer. In a pilot study half or patients on active surveillance responded, even at low levels, and one patient experienced complete disappearance of at least one cancerous lesion. The anti- cancer actions are similar in nature to those of enzalutamide the leading androgen receptor drug therapy. A significant number of breast cancers are so called androgen receptor positive, and some respond to the same drugs used in prostate cancer. a clear signal that luteolin should be explored there.
There is also new evidence that the actions of luteolin may directly reduce progression rate of gastric cancer through actions on so called Notch1 signaling. Researchers examined the link to progression and spread in gastric cancer driven by dysfuntional levels of Nothch1 signaling. Approximately a forty percent risk reduction is found in patients maintaining lower Notch1 expression, due to decreased metastatic activity. They go on to show particularly large reductions in Notch1 from actions of luteolin in pre-clinical trials.
Dietary intake of luteolin has been seen suppressing insulin resistance and systemic inflammatory markers such as c-reactive protein. Lowering CRP is invariably linked to lowering risks. New research in early stage prostate cancer shows measurable anti-cancer activity at 50mg, the pilot study reporting a clinical benefit in patients with no adverse events at 50mg (highlight 1). Progression rates in liver, colorectal, breast cancers and more are also assocated to insulin resistance and more with inflammation including kidney and lung cancer. There are population studies in type 2 diabetes showing metabolic and cardiac health benefits even in modest dietary amounts, so far no application studies directly in cancer where effects are more likely to be seen in combining multiple active compounds.
Together with Chlorogenic acid (see Green Coffee Extract) , a commerical brand Altilix(R) has shown good evidence of cholesterol and glucose reduction for heart and liver health. Artichoke extracts are also high in luteolin, and can encourage crucial bacteria in the microbiome. Meta-analyses partly confirms lowered cancer incidence with high flavonoid diets. There is limited clinical evidence to assess luteolin specific actions in systemic health. The few studies available do confirm significant anti-inflammatory actions associated with flavanoids overall (see References).
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Daily oral supplementation with 50 mg luteolin for 6 months was found to be safe and may suppress PCA [prostate cancer] progression in patients under Active Surveillace via the attenuation of expression of AR [androgen receptor] and NKX3.1. (Both) miR-29 and miR-30 induced by luteolin have important roles in reducing AR and NKX3.1 levels, resulting in inhibiting PCA progression. In addition, miR-29 and miR-30 may be novel therapeutic targets for PCA progression in clinical practice
Luteolin treatment also significantly reduced Notch1 expression. Moreover, higher Notch1 expression was correlated with a poor OS [patient Overall Survival] and a poor time to FP [time to progression in patient data]. We propose a model for the role of Notch1 and β-catenin in GC progression. NICD interacts with β-catenin to regulate target genes, causing induction of cell proliferation and metastasis and inhibition of apoptosis. Luteolin inhibits Notch1 and β-catenin expression, thus exhib...
At the end of the study, we again found that subjects receiving Altilix® [chlorogenic acid+luteolin extracts] in relation to placebo, had a statistically significant improvement in most of the evaluated parameters. Weight and BMI improved in subjects with NAFLD, waist circumference improved in those with borderline NAFLD… Glycemic variables (HbA1c, HOMA-IR, and HOMA-β), plasma lipids (TC, TG, and LDL-C), and hepatic enzymes (AST, ALT, and AST/ALT ratio) improved in all the...
Per-unit increment of luteolin intake was found to reduce all-cause mortality by 7.0% and cardiac mortality by 22.6%  in patients with T2DM [diabetes]. An inverse dose-response association was identified between luteolin intake and mortality risk….The HbA1c level, and T2DM duration. Moreover, luteolin intake increment was also shown to be associated with a lower C-reactive protein level at baseline (β =-0.332).
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https://www.researchgate.net/publication/389324825 | 4 | Daily oral supplementation with 50 mg luteolin for 6 months was found to be safe and may suppress PCA progression in patients under AS via the attenuation of expression of AR and NKX3.1. miR-29 and miR-30 induced by luteolin have important roles in reducing AR and NKX3.1 levels, resulting in inhibiting PCA progression. In addition, miR-29 and miR-30 may be novel therapeutic targets for PCA pro- gression in clinical practice | And after 180 days of daily luteolin treat- ment, the positive lesion had completely disappeared (Figures 2(i), 2(j), and 2(k)). At a repeated protocol biopsy for the FR1 patient, for a precise estimation of the eec- tiveness of luteolin, in addition to the systematic 12-core biopsy, two cores of TRUS/mpMRI-targeted fusion biopsies based on mpMRI mapping at diagnosis were also added; however, no cancer cores existed in the protocol biopsy | ![]() |
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5327575/ | 3.5 | In this study, we found that luteolin significantly suppressed GC progression by inhibiting cell proliferation, migration, and invasion; inducing apoptosis; and reversing the EMT. Meanwhile, the Akt, β-catenin, and Notch signaling pathways were inhibited by luteolin. Furthermore, the effects of downregulation of Notch1 were similar to those observed upon treatment of GC cells with luteolin. In addition, higher Notch1 expression correlated with a poor OS. Luteolin suppressed tumor growth and Notch1 signaling in vivo. Therefore, luteolin may be an effective drug for GC treatment. | We also observed that the cytoskeleton of GC cells shrank upon treatment with luteolin. F-actin staining was used to confirm the changes in the cytoskeleton of GC cells treated with luteolin, and the results suggest that luteolin might inhibit GC motility by reversing EMT in a manner similar to that observed in pancreatic and ovarian cancers [7]. As expected, upon luteolin treatment, the epithelial biomarker E-cadherin was increased. In the contrast, the mesenchymal biomarkers N-cadherin, vimentin, and Snail were reduced in a dose-dependent manner | ![]() |
https://pmc.ncbi.nlm.nih.gov/articles/PMC6893885/ | 3 | A recent preclinical study reported the impact of flavonol derivatives rich in quercetin and kaempferol on fat storage in the liver. These molecules suppressed some signaling pathways involved in lipogenesis and adipogenesis, as well in the expression of key proteins of lipogenic liver metabolism [27]. Our results point out the presence of such synergistic effects, showing an improvement in anthropometric (body weight, BMI, and waist circumference), glycemic, lipid, and liver parameters in Altilix® (based on chlorogenic acid and its derivatives, and luteolin and its derivatives) supplemented subjects vs. placebo. | Our experimental data, for the first time, show the effect of artichoke extract on the improvement of two early atherosclerotic markers: cIMT and FMD, evidencing the clinical importance of the treatment as well as its nutraceutical properties on vascular function and remodeling, including beneficial action on the cardiovascular system and hepatoprotective activity [10]. Firstly, after 6 months of Altilix® supplementation, we found a significant improvement in endothelial function, and subsequently, we confirmed a preliminary observation of a beneficial effect of artichoke juice on brachial FMD, in a small group of hyperlipidemic subjects [29]. | |
https://iris.unipa.it/retrieve/b1dbb910-9bf6-44de-8e2a-2409ff38ba39/altilix.pdf | 3 | All subjects received the Altilix® supplement (150 mg/day) or placebo using a computer-based random allocation system. After six months of treatment Altilix® significantly reduced body weight, glycemic, and lipid parameters (total cholesterol, triglycerides, LDL-cholesterol) and improved hepatic functionality, CIMT, and FMD. In conclusion, these results confirm that Altilix® supplementation has a significant effect on cardiometabolic parameters not only in obese subjects but also in pre-obesity subjects | Altogether, our data demonstrate that Altilix® supplementation strongly improved quality of life of both MetS and NAFLD patients, ameliorating some key biomarkers obtained through a very rigorous randomized, double-blind, placebo-controlled study. Therefore, we suggest Altilix® supplementation as a valid and safe approach in the prevention and management of cardiometabolic and hepatic alterations, such as NAFLD and MetS. | |
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10039598/ | 2.5 | The current study prospectively examined the association of luteolin intake with all-cause and cardiac mortality among 2,461 patients with T2DM. During the follow-up period (median, 8.7 years), per-unit increment of luteolin intake (Ln-transformed) contributed to a 7.0% reduction in all-cause mortality (P = 0.024) and a 22.6% reduction in cardiac mortality (P = 0.001). This association was independent of other flavonoid intakes and consistent across the stratified population. The anti-inflammatory effect of luteolin was also identified at baseline, which may account for the remarkable prognostic improvement. | Consistently, for the first time, this population-based study confirmed that dietary luteolin intake increment contributed to a risk reduction in both all-cause and cardiac mortality among patients with T2DM. Therefore, it is recommended that T2DM patients consume more luteolin-rich food in their daily diet. To consume more luteolin-rich foods may be a promising dietary intervention strategy for T2DM. Compared to using anti-diabetic drugs, dietary intervention could be safer and can be more easily accepted by patients. Besides, given its anti-diabetic effects, luteolin-rich dietary strategy is also optional for pre-diabetes patients who do not require anti-diabetic drugs | ![]() |
https://www.nature.com/articles/tp2015142 | 2.5 | Nevertheless, serum IL-6 levels were significantly lower (14.68±19.22 pg ml−1) in children with ASDs after treatment with luteolin in comparison to their levels before the beginning of treatment (61.95±94.76 pg ml−1). Serum TNF levels were significantly (P=0.045) elevated (313.8±444.3 pg ml−1) in children with ASDs as compared with normotypic controls (52.78±34.62 pg ml−1) | Here we report that treatment with a luteolin-containing dietary formulation normalized serum IL-6 and TNF in those children that showed the most benefit from the use of luteolin. We recently reported that the structural analog of luteolin 3′,4′,5,7-tetramethoxy flavone was more potent than luteolin in its ability to inhibit mediator release from human MCs.35 Luteolin is structurally closely related to 7,8-dihydroflavone, which was shown to have brain-derived neurotrophic factor (BDNF)-like activity | |
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9862908/ | 2 | ..we believe that the main results of the present study are of great clinical importance since we have found that this nutraceutical has a number of beneficial effects on lipid, glucose, hepatic and vascular parameters in pre-obesity subjects, which can be easily translated into the everyday clinical practice of our patients with pre-obesity. | We demonstrated that Altilix® could be a valid and safe approach to the prevention and management of cardiometabolic and hepatic alterations. The results pushed us to continue the investigation by performing the present study, a sub-analysis of the Altilix study in which the examination is of subjects with the pre-obesity condition. Here, the use of Altilix improved glycemic and lipid metabolism, liver parameters, and vascular function in pre-obesity individuals. Since this clinical study has had a very rigorous randomized, placebo-controlled, double-blind design, our results emphasize the role of nutraceuticals with proven efficacy in daily practice on subjects with pre-obesity |
A recent pilot study in five patients in early phase prostate cancer and PSA below 15ng/L. With both non cancerous and cancerous lesions, 4 were initally judged low and 1 intermediate risk. During active surveillance, luteolin was adminstered at a low dose, only 50mg daily for 6 months. This amount is only 4 to 5oz of radicco. Even so there were promising effects reported here.
Two patients showed clear responses, and one achieved stable disease. These actions include both reduction in so called Androgen Receptor activity levels, and increased molecules identified as miR-29 and miR-30, often seen acting as tumor suppressors. In one patient, the report includes complete disappearence of a cancerous lesion, remarkable to say the least and at low dose. No side effects were detected and its probable that at least some or even all of these anti-cancer actions are dose dependent. The data below clearly shows that responders had androgen receptor activity suppressed with luteolin.
The androgen receptor targeting drug enzalutamide operates in a similar way. Luteolin has no reported side effects, in fact its likely to have other positive effects.
This study firstly shows around 40% lower progression rates in patients with low activity in the so called “notch-1” pathway. Upregulated signaling of notch-1 is linked to growth and metastatic spread in many cancers. Here the patient data shows a large effect (below)
The evidence for luteolin being able to reduce this signaling is convincingly shown in mouse models, where a large effect is reported. Mice with luteolin show much lower rates of progression.
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