Estrogen Block: The Best Natural Aromatase Inhibitor

An enzyme in fat tissue, called aromatase, converts other hormones in the body https://labisa.in/2024/12/19/steroids-pharmacological-understanding-their-role-18/ into estrogen. In doing so, the drugs lower the amount of estrogen in the body by as much as 95%. Overall, the available studies suggest that the differences in lipid profile between tamoxifen and AIs may be due to the lipid-lowering capacity of tamoxifen rather than to increases in lipid levels due to AIs. However, the true difference in changes of lipid parameters between patients receiving tamoxifen and AIs still has to be defined and therefore no exact recommendation concerning the monitoring of lipid metabolism may at present be given. A couple of trends are discernible when comparing the aromatase inhibitory activity of structures within the chalcone compound class.

In part, this approach was supported by previously published reports demonstrating that isoflavones and other phytoestrogens compounds had antiestrogenic, antiproliferative, and antiaromatase activities. Also, the fact that breast cancer is the predominant type of cancer in industrialized countries, the second leading cause of cancer-related deaths in women, and the increased public awareness of breast cancer campaign galvanized research efforts along this path. In conclusion, E-Block is a natural supplement that provides hormone imbalance support for both men and women. It is an effective estrogen blocker and aromatase inhibitor that helps to reduce the excess estrogen in the body.

The extract is known to be more powerful compared to many anti-aromatase drugs available on the market. A non-significant increase in the incidence of cardiovascular disease was also reported in patients switching to exemestane in the IES trial, including a 2.5-fold increase in the number of myocardial infarctions (Coombes et al 2007). Data on lipid profile were not systematically collected in the ATAC trial; however, the prevalence of low grade hypercholesterolemia was reported to be 2.6 fold higher in patients receiving anastrozole than in those taking tamoxifen (ATAC Trialists’ Group 2005). Over time, levels of the hormones testosterone and estrogen can become imbalanced in males, potentially causing health problems. Medications called estrogen blockers are among the treatment options for those with low testosterone and higher estrogen.

Patient 2 (sister of index patient)

ERα is the subtype of ER that is required for most of the known estrogenic responses 3. With the presence of ligand, ERα is displaced from the heat shock proteins and interacts either directly through specific estrogen response elements (EREs) or indirectly through transcriptional factors like AP1, SP1, and NF-κB 1, 4. Beside its genomic action, recent data demonstrated that ER also has non-genomic activity by acting as a component of membrane and cytoplasmic signaling cascades 5. Even with the improved efficacy of AIs or other endocrine therapies, postmenopausal breast cancer patients eventually develop resistance to AIs causing relapse of the disease 59–64, 80. Generally, resistance involves tumor regrowth after 12–18 months of treatment and stable disease.

Review Criteria

Trastuzumab alone did not have anti-tumor activity in the parental endocrine responsive MCF-7Ca and the upfront combination of trastuzumab and letrozole did not prolong or avert the resistance 105. Analysis of protein expression levels (figure 2B) in the tumors at the end of treatment showed reduced levels of HER2 with trastuzumab alone or in combination and increased expression of ER. However, in presence of the combined treatment, the effect of trastuzumab to increase ER expression and aromatase was blocked by letrozole resulting in reduced tumor growth (figure 2A). In contrast to premenopausal women, in whom most of the estrogen is produced in the ovaries, in postmenopausal women estrogen is mainly produced in peripheral tissues of the body. The heightened gonadotropin levels also upregulate the aromatase promoter, increasing aromatase production in the setting of increased androgen substrate. This would counteract the effect of the aromatase inhibitor in premenopausal women, as total estrogen would increase.

• It has actually been found that about 80% of estrogen in men is from testosterone, through aromatization.
• Many women will turn to their internists for advice about whether to take these drugs, as well as help in preventing and managing adverse events.
• Aromatase inhibitors lower estrogen levels in the body by blocking aromatase, an enzyme that converts other hormones into estrogen.
• There is not sufficient evidence to state that red wine is a safe, effective treatment for breast cancer in postmenopausal women or that it is a safe and effective chemopreventive dietary product in humans 38.
• The lowest costs found using coupons or prescription-assistance programs are also listed.

This analysis showed that in hormone-receptor positive populations the improvement in disease control with anastrozole with respect to tamoxifen was maintained for over three years after treatment cessation (ATAC Trialists’ Group 2008). There have been 43 miscellaneous natural product compounds tested for aromatase inhibition in the literature (Table 16, Fig. 17). Fourteen benzenoids were tested, with TAN-931 (269) isolated from the bacterium Penicillium funiculosum No. 8974 165, being weakly active in microsomes.

In order to understand how AI’s work, it’s first important to understand what the aromatase enzyme does in the body. In short, aromatase works as a catalyst to synthesize androgens into estrogens. The main mechanism of action is to turn testosterone into estradiol and androstenedione into estrone.

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More than half of all breast cancers are driven by the hormone estrogen, which makes them ideal candidates for treatment with a class of drugs called aromatase inhibitors, or AIs. These are prescribed for post-menopausal women after surgery and are taken for a period of five to 10 years. This approach has proven effective, reducing the chance of breast cancer coming back by about half. For example, before the crystal structure of the aromatase enzyme was reported in 2009, some investigators used three-dimensional modeling techniques of aromatase for structure-based drug design 84. From such studies numerous reports have confirmed the potential of flavones as aromatase inhibitors 67, such as naringenin, hesperetin, eriodictyol, and naringin. However, in general, flavones are more potent aromatase inhibitors than flavanones 85.

Considered together, these data seem to demonstrate that drugs such as azoles and antiepileptics may potentiate the action of aromatase inhibitors, further inhibiting the enzyme activity. In addition, Cannabis sativa and its correlates can reduce the formation of the substrate androstenedione and also potentiate the action of aromatase inhibitors. On the other hand, alcohol consumption can increase aromatase activity or expression. Considering the increased prescription of both aromatase inhibitors in adolescents with short stature, the aim of this review is to discuss the possible drug interactions between anastrozole and letrozole and other drugs. In addition, a brief description of the pharmacokinetic profile of both inhibitors was included in this review in order to understand the emergence of possible drug interactions related to absorption, metabolism, half-life and excretion of these drugs.