ButeinAI – Botanical Aromatase Inhibitor to reduce estrogens – 60 Caps

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butein_text contains Butein.. a chalconoid extracted from the sap of the Chinese Lacquer Tree Rhus Verniciflua Stokes (RVS). Butein found within RVS has been used in Korea for around 500 years, it has anti-oxidative, anti-inflammatory, anti-tumor, anti-fibrogenic, anti-adipogenic, anti-angiogenic, and aldose reductase/advanced glycation endproducts inhibitory effects. [1]

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Description

Butein Estrogen Inhibitor

 

butein_text is Not intended for use for children or during pregnancy or when breast feeding except under the care of a licensed medical practitioner. It should not be used with N-Acetyl Cysteine (NAC). 

Butein (2′,3,4,4′-tetrahydroxychalcone), a simple chalcone derivative, occurs in many unrelated genera including Butea, Dahlia, Coreopsis and Searsia. It is a reputed food additive and a common ingredient of botanicals used in herbal medicine formulations, particularly in Asian countries. Although a simple polyphenol, this molecule exhibits a range of pharmacological properties, most notably acting as a potent protein tyrosine kinase inhibitor and as an antineoplastic agent.

Researchers have convincingly demonstrated that butein inhibits the epidermal growth factor receptor in HepG2 cells and the tyrosine-specific protein kinase activities of the epidermal growth factor receptor.

Butein (2′,3,4,4′-tetrahydroxychalcone), a simple chalcone derivative, occurs in many unrelated genera including Butea, Dahlia, Coreopsis and Searsia. It is a reputed food additive and a common ingredient of botanicals used in herbal medicine formulations, particularly in Asian countries.

Although a simple polyphenol, this molecule exhibits a range of pharmacological properties, most notably acting as a potent protein tyrosine kinase inhibitor and as an antineoplastic agent. Researchers have convincingly demonstrated that butein inhibits the epidermal growth factor receptor in HepG2 cells and the tyrosine-specific protein kinase activities of the epidermal growth factor receptor.

In addition, it also exhibits promising anti-inflammatory, antidiabetic, antinephritic, antithrombin, anti-angiogenic and hepatoprotective activities in various animal models. Although this molecule is endowed with an impressive list of biological properties, which have acted as scientific support for its commercialization, there are no review articles that coherently discuss various aspects of this chalcanoid. This review aims to explore the pharmacological relevance of butein, together with its structure-activity relationships and mechanisms of action. In addition, the occurrence, chemical synthesis and biosynthesis of butein are discussed.

In addition, it also exhibits promising anti-inflammatory, antidiabetic, antinephritic, antithrombin, anti-angiogenic and hepatoprotective activities in various animal models. Although this molecule is endowed with an impressive list of biological properties, which have acted as scientific support for its commercialization, there are no review articles that coherently discuss various aspects of this chalcanoid.

This review aims to explore the pharmacological relevance of butein, together with its structure-activity relationships and mechanisms of action. In addition, the occurrence, chemical synthesis and biosynthesis of butein are discussed.

What botanicals are in butein_text?

Butein isolate from Rhus verniciflua Stokes (chinese lacquer tree)
(aka Toxicodendron vernicifluum) (2′,3,4,4′-tetrahydroxychalcone)
Nettle  (Urtica siccum)
Luteolin Extracts
Agaricus mushroom
Fenugreek (seeds of Trigonella foenum-graecum)
Silica
magnesium stearate

Butein
Butein is a chalconoid. It can be found in Toxicodendron vernicifluum (or formerly Rhus verniciflua).  It has antioxidative, aldose reductase and advanced glycation endproducts inhibitory effects. It is also  a sirtuin-activating compound, a chemical compound having an effect on sirtuins, a group of enzymes that use NAD+ to remove acetyl groups from proteins. It turns out that buteins possess a high ability to inhibit aromatase process in the human body, for this reason, the use of these compounds in the treatment of breast cancer on the estrogen ground has been taken into account, Butein inhibits pathways for NF-kB, VEGF, EPC and TNF-a & EGFR, and ERK1/2.

Potential of butein, a tetrahydroxychalcone to obliterate cancer – Read the report showing Butein on a variety of cancers here

There are several reports on the various biological activities of butein in which around 43 articles reported that butein shows potential anti-proliferative effect against a wide range of neoplasms and the molecular target varies with cancer types. Most often it targets NF-kB and its downstream pathways. In addition, butein induces the expression of genes which mediate the cell death and apoptosis in cancer cells. It also inhibits tumor angiogenesis, invasion and metastasis in prostate, liver and bladder cancers through the inhibition of MMPs, VEGF etc. Moreover, it inhibits the overexpression of several proteins and enzymes such as STAT3,  CXCR4, COX-2, Akt, Ras etc. involved in tumorigenesis.

Collectively, all these findings suggest the enormous potential and efficacy of butein as a multitargeted chemotherapeutic, chemopreventive and chemosensitizing agent against a wide range of cancers with minimal or no adverse side effects. [Cancer Biology Laboratory, Department of Biosciences and Bioengineering, Assam, India ]

Nettle
It has been demonstrated that the leaf of Stinging nettle can decrease MCF-7 cell line proliferation (17, 34). Therefore there is not always a direct relationship between the amounts of antioxidant components such as flavonoids and phenolics with cancer treatment efficiency. This may also be due to differences in the amounts of various cell surface receptors or signal transduction constituents within each cell type. Our findings also demonstrate that depending on the type of cancer cell line, certain parts of the plant may be efficient. Consequently, it is worth to examine the cytotoxic effect of extracts belonging to different parts of each plant before deepening such studies by fractionation of extract constituents. [23 below]

One of the ways nettle leaf extract blocks proinflammatory signaling by inhibiting the genetic transcription factor that activates TNF-alpha and IL-1 beta in synovial tissue. This proinflammatory transcription factor, known as nuclear factor kappa beta (NF-kb), is elevated in chronic inflammatory diseases and is essential to activation of TNF-alpha. Nettle is thought to work by preventing degradation of the natural inhibitor of NF-kb in the body. TNF-alpha also activates NF-kb in synovial cells, leading to the suggestion that a cycle of cross-activation between TNF-alpha and NF-kb may sustain and amplify the disease process in rheumatoid arthritis. [4]

Here we demonstrate that treatment of different cells with IDS23 potently inhibits NF-kappaB activation. An inhibitory effect was observed in response to several stimuli, suggesting that IDS23 suppressed a common NF-kappaB pathway. Inhibition of NF-kappaB activation by IDS23 was not mediated by a direct modification of DNA binding, but rather by preventing degradation of its inhibitory subunit IkappaB-alpha. Our results suggests that part of the antiinflammatory effect of Urtica extract may be ascribed to its inhibitory effect on NF-kappaB activation. Nettle contains the follow compounds: polysaccharides, vitamin C and carotene, beta-sitosterol, and the flavonoids quercetin, rutin, kaempferol, and beta-sitosterol. (http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2322858/)

Luteolin
Luteolin, a novel natural inhibitor of tumor progression locus 2 serine/threonine kinase, inhibits tumor necrosis factor-alpha-induced cyclooxygenase-2 expression in JB6 mouse epidermis cells. Targeting tumor necrosis factor (TNF)-a-mediated signal pathways may be a promising strategy for developing chemopreventive agents, because TNF-a-mediated cyclooxygenase (COX)-2 expression plays a key role in inflammation and carcinogenesis. Luteolin [2-(3,4-dihydroxyphenyl)-5,7- dihydroxy-4-chromenone] exerts anticarcinogenic effects, although little is known about the underlying molecular mechanisms and specific targets of this compound. In the present study, we
found that luteolin inhibited TNF-a-induced COX-2 expression by down-regulating the transactivation of nuclear factor-?B and activator protein-1. Furthermore, luteolin inhibited TNF-a-induced phosphorylation of mitogen-activated protein kinase/extracellular signal-regulated kinase (ERK) kinase 1/ERK/p90(RSK), mitogen-activated protein kinase kinase 4/c-Jun N-terminal kinase/c-Jun, and Akt/p70(S6K). However, it had no effect on the phosphorylation of p38. These effects of luteolin on TNF-a-mediated signaling pathways and COX-2 expression are similar to those achieved by blocking tumor progression locus 2 serine/threonine kinase (TPL2) using pharmacologic inhibitors and small interfering RNAs. Luteolin inhibited TPL2 activity in vitro and in TPL2 immunoprecipitation kinase assays by binding directly in an ATP-competitive manner. Overall, these results indicate that luteolin exerts potent chemopreventive activities, which primarily target TPL2.
http://www.ncbi.nlm.nih.gov/pubmed/21705614

Clinical Studies

1. Inhibitory Effect of the Compounds Isolated from Rhus verniciflua on Aldose Reductase and Advanced Glycation Endproducts
https://www.jstage.jst.go.jp/article/bpb/31/8/31_8_1626/_article

2. Butein Inhibits Angiogenesis of Human Endothelial Progenitor Cells
http://www.hindawi.com/journals/ecam/2013/943187/

3. The chalcone butein from Rhus verniciflua Stokes inhibits clonogenic growth of human breast cancer cells co-cultured with fibroblasts.
http://www.ncbi.nlm.nih.gov/pubmed/15757513

4. Luteolin, a novel natural inhibitor of tumor progression locus 2 serine/threonine kinase, inhibits tumor necrosis factor-alpha-induced cyclooxygenase-2 expression in JB6 mouse epidermis cells.
http://www.ncbi.nlm.nih.gov/pubmed/21705614

5. Butein downregulates chemokine receptor CXCR4 expression and function through suppression of NF-kB activation in breast and pancreatic tumor cells.
http://www.ncbi.nlm.nih.gov/pubmed/20699088

6. A novel anticancer effect of butein: Inhibition of invasion through the ERK1/2 and NF-kB signaling pathways in bladder cancer cells However it happens, over-activity of the MAPK1 gene and its ERK1/2 protein can spur the growth of cancers in organs throughout the body. But that means the pathway gives us a place to hit cancer where it hurts. In fact, statin drugs taken by many people for their cholesterol-lowering effects incidentally seem to protect against cancer and cancer-related deaths, apparently by dampening the MAPK signal.
Scientists have been working on drugs to target components of the MAPK pathway much more intentionally. They liken cancer’s dependency on MAPK and other molecular pathways to addictions. If cancer were to suddenly lose its molecular pathway (or “drug”) of choice, then perhaps those malignant cells would flounder and die.

http://www.sciencedirect.com/science/article/pii/S0014579308003773 ,
http://www.abcam.com/cancer/erk12-signaling-in-cancer (MAP)
https://www.cureforward.com/stories/gene-stories/mapk1-erk1-2/ (simple explanation)
7. 2′,4′,6′-Tris(methoxymethoxy) chalcone attenuates hepatic stellate cell proliferation by a heme oxygenase-dependent pathway
http://www.ncbi.nlm.nih.gov/pubmed/16982036

8. Butein, a plant polyphenol, induces apoptosis concomitant with increased caspase-3 activity, decreased Bcl-2 expression and increased Bax expression in HL-60 cells.
http://www.scopus.com/record/display.uri?eid=2-s2.0-0034997805&origin=inward&txGid=0

9. Cytotoxic effect of butein on human colon adenocarcinoma cell proliferation.
http://www.ncbi.nlm.nih.gov/pubmed/8033070

10. Butein blocks tumor necrosis factor a-induced interleukin 8 and matrix metalloproteinase 7 production by inhibiting p38 kinase and osteopontin mediated signaling events in HT-29 cells.
http://www.sciencedirect.com/science/article/pii/S0024320507007370

11. Butein induces apoptosis and inhibits prostate tumor growth in vitro and in vivo.
http://europepmc.org/abstract/MED/22114764

12. Butein (2′,3,4,4′-tetrahydroxychalcone), a simple chalcone derivative, occurs in many unrelated genera including Butea, Dahlia, Coreopsis and Searsia.It is a reputed food additive and a common ingredient of botanicals used in herbal medicine formulations, particularly in Asian countries. Although a simple polyphenol, this molecule exhibits a range of pharmacological properties, most notably acting as a potent protein tyrosine kinase inhibitor and as an antineoplastic agent. Researchers have convincingly demonstrated that butein inhibits the epidermal growth factor receptor in HepG2 cells and the tyrosine-specific protein kinase activities of the epidermal growth factor receptor.

In addition, it also exhibits promising anti-inflammatory, antidiabetic, antinephritic, antithrombin, anti-angiogenic and hepatoprotective activities in various animal models. Although this molecule is endowed with an impressive list of biological properties, which have acted as scientific support for its commercialization, there are no review articles that coherently discuss various aspects of this chalcanoid.

This review aims to explore the pharmacological relevance of butein, together with its structure-activity relationships and mechanisms of action. In addition, the occurrence, chemical synthesis and biosynthesis of butein are discussed.
http://www.alvaroviljoen.com/Project_338_publications.html

13. Potential of butein, a tetrahydroxychalcone to obliterate cancer.
“Our search retrieved several reports on the various biological activities of butein in which around 43 articles reported that butein shows potential anti-proliferative effect against a wide range of neoplasms and the molecular target varies with cancer types. Most often it targets NF-κB and its downstream pathways. In addition, butein induces the expression of genes which mediate the cell death and apoptosis in cancer cells. It also inhibits tumor angiogenesis, invasion and metastasis in prostate, liver and bladder cancers through the inhibition of MMPs, VEGF etc. Moreover, it inhibits the overexpression of several proteins and enzymes such as STAT3, ERK, CXCR4, COX-2, Akt, EGFR, Ras etc. involved in tumorigenesis.”

CONCLUSION:
Collectively, all these findings suggest the enormous potential and efficacy of butein as a multitargeted chemotherapeutic, chemopreventive and chemosensitizing agent against a wide range of cancers with minimal or no adverse side effects.
http://www.ncbi.nlm.nih.gov/pubmed/26598915

FULL TEXT: https://www.researchgate.net/publication/283525832_Potential_of_butein_a_tetrahydroxychalcone_to_obliterate_cancer

Trials with Chemotherapy Drugs

Butein with Cisplatin (Aug 2015)
“Overall, the findings of this study reveal a new function of butein that enhances the sensitization of cervical cancer cells to cisplatin in vitro and in vivo, which may be related to the AKT and ERK/p38 MAPK pathways, at least to a certain extent, through the regulation of FoxO3a. This data sheds some light on the synergistic antitumor effects of butein and cisplatin and verify the potential clinical use of butein.”
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4564095

 

Suggested Usage

2 capsules a day, 1 capsule serving separated from each by at least
8 hours. Total daily amount of 2 capsules should not be exceeded unless under supervision of an experienced health professional.

butein_textmight best be used as part of the full RTKAI protocol* which includes the addition of AROMHIB, Extra Virgin Olive Oil, Purple Corn Extract, CurcuminC3, decaf Green Tea Extract , liver & colon detoxing, parasite cleansing, probiotics, enzymes and exercise.

These statements have not been evaluated by the Food & Drug Administration. This product is not intended to diagnose, treat, cure or prevent any disease.

Additional information

Weight 50 g
Size

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