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Estrone

Sex Hormones & TRT
E1Oestrone

Overview

Estrone (E1), also known as oestrone, is an endogenous estrogen hormone and a member of the steroid hormone family. It is primarily produced in the ovaries, adipose tissue, and adrenal glands. As a naturally occurring estrogen, estrone is one of the three major estrogens in the human body, alongside estradiol and estriol. It is a key component of the estrogenic activity in postmenopausal women, where it becomes the predominant form of estrogen due to decreased ovarian production of estradiol. Estrone is also available in synthetic forms for therapeutic use. Researchers have found that estrone plays a crucial role in the regulation of the menstrual cycle and reproductive system. It is involved in the development of secondary sexual characteristics and the maintenance of the female reproductive tissues. Estrone has been studied for its potential effects on bone density, cardiovascular health, and its role in hormone replacement therapy (HRT) for menopausal symptoms. The mechanism of action of estrone involves binding to estrogen receptors, primarily estrogen receptor alpha (ERα) and estrogen receptor beta (ERβ). Upon binding, it activates these receptors, which then interact with specific DNA sequences to regulate gene expression. This process influences various biological pathways, including those involved in cell growth, differentiation, and reproductive function. Estrone's pharmacokinetic properties include a circulating half-life of approximately 70 minutes. It is metabolized primarily in the liver and undergoes enterohepatic circulation. Oral bioavailability is limited due to first-pass metabolism, while transdermal and injectable forms offer more consistent absorption. Clinically, estrone is used in hormone replacement therapy, particularly for postmenopausal women. It is regulated as a prescription medication in many countries, with specific guidelines for its use in managing menopausal symptoms and other estrogen-deficient conditions. Researchers have observed its efficacy in improving quality of life for women experiencing menopause-related symptoms, though its use must be carefully monitored due to potential risks associated with estrogen therapy.

Mechanism of Action

Estrone acts on estrogen receptors ERα and ERβ, initiating a cascade that regulates gene expression. This activation influences pathways related to cell growth and reproductive function.

Molecular Data

FormulaC18H22O2
Molecular Weight270.4 g/mol
CAS Number53-16-7
PubChem CID5870

Half-Life & Pharmacokinetics

EndogenousCirculating half-life ~70 minutes
TransdermalSteady-state after 24-48h
OralPoor bioavailability due to first-pass

Estrone's pharmacokinetics vary by administration route; oral forms have limited bioavailability.

Storage

Temperature

Store at room temperature (15-30°C)

Light

Protect from light

Form

Oil solution stable for 2+ years

Notes

Ensure containers are tightly sealed to prevent degradation.

Solubility

Estrone is poorly soluble in water but soluble in ethanol and oils, relevant for formulation in various delivery systems.

Legal Status

🇩🇪DE

Prescription only (verschreibungspflichtig); not a controlled substance under BtMG.

🇺🇸US

FDA-approved for specific indications; prescription required.

🇦🇺AU

TGA Schedule 4 (S4) - prescription only.

🇬🇧UK

Prescription only medicine (POM); regulated by MHRA.

Legal status information is provided for general reference only and may not reflect the most current regulatory changes. Always verify with official government sources before making any decisions.

10 Research Publications

Estrone-mediated lowering of ROS and NOX4 improves endothelial function in ovariectomized wistar rats.

Animal

Naunyn-Schmiedeberg's archives of pharmacology · 2024

Researchers observed that estrone (E1), a form of estrogen, improved blood vessel function and reduced oxidative stress in ovariectomized rats, which mimic postmenopausal conditions. E1 treatment also helped lower body weight and cholesterol levels, suggesting potential benefits for cardiovascular health in postmenopausal women.

  • E1 treatment decreased body weight and fat in ovariectomized rats.
  • E1 improved blood vessel function and reduced oxidative stress.
  • E1 helped lower cholesterol levels in the treated rats.
PubMed

Reproductive hormones in relation to white matter hyperintensity volumes among midlife women.

Unknown

Alzheimer's & dementia : the journal of the Alzheimer's Association · 2024

Researchers found that higher levels of estradiol (E2) and estrone (E1) are linked to lower volumes of white matter hyperintensities in the brains of midlife women, while higher levels of follicle-stimulating hormone (FSH) are associated with greater volumes. These findings highlight the significant role of reproductive hormones in women's brain health during midlife.

  • Higher E2 and E1 levels are associated with lower white matter hyperintensity volumes.
  • Higher FSH levels are linked to greater white matter hyperintensity volumes.
  • The relationships between E1 and FSH with white matter hyperintensity volumes persist even when considering cardiovascular disease risk factors.
PubMed

Conversion of estriol to estrone: A bacterial strategy for the catabolism of estriol.

Unknown

Ecotoxicology and environmental safety · 2024

Researchers found that a specific bacterium, Novosphingobium sp. ES2-1, can break down estriol, a natural estrogen that can pollute water and soil. They identified the products formed during this process using advanced laboratory techniques, contributing to our understanding of how bacteria can help in the degradation of potentially harmful substances in the environment.

  • Novosphingobium sp. ES2-1 can metabolize estriol.
  • The study identified the breakdown products of estriol.
  • This research enhances knowledge of bacterial roles in environmental cleanup.
PubMed

Exposure to estrone disrupts the endocrine system of western mosquitofish (Gambusia affinis).

Unknown

Aquatic toxicology (Amsterdam, Netherlands) · 2023

Researchers observed that exposure to estrone, a natural estrogen, significantly disrupted the endocrine system of western mosquitofish. High levels of estrone led to a complete female population and inhibited female growth, while lower levels caused male fish to develop female-like traits. Additionally, changes were noted in reproductive cell development and gene expression related to sex differentiation.

  • High estrone exposure resulted in 100% female mosquitofish and stunted growth in females.
  • Lower estrone levels caused males to develop female-like physical traits.
  • Estrone exposure altered reproductive cell development and gene expression related to sex differentiation.
PubMed

A Novel Estrone Degradation Gene Cluster and Catabolic Mechanism in Microbacterium oxydans ML-6.

Unknown

Applied and environmental microbiology · 2023

Researchers found that a specific bacterium, Microbacterium oxydans ML-6, can effectively break down estrone, a harmful chemical contaminating soil and water due to animal manure use. They identified a new set of genes involved in this degradation process, which could help develop better methods for cleaning up contaminated environments.

  • Microbacterium oxydans ML-6 can efficiently degrade estrone.
  • A new gene cluster related to estrone breakdown was discovered.
  • This research could lead to improved bioremediation strategies for contaminated soils.
PubMed

Migration and abiotic transformation of estrone (E1) and estrone-3-sulfate (E1-3S) during soil column transport.

Unknown

Environmental geochemistry and health · 2022

Researchers observed that estrone-3-sulfate (E1-3S) moves through soil more easily than estrone (E1), which raises concerns about its potential impact on groundwater. They also found that E1-3S can transform into other estrogen compounds in soil, highlighting the need to understand how these substances behave in the environment.

  • E1-3S migrates more readily through soil compared to E1.
  • E1-3S has a high potential to leach into groundwater.
  • E1-3S can transform into other estrogen compounds in sterilized soil.
PubMed

Estrone sulfatase and its inhibitors.

Review

Anti-cancer agents in medicinal chemistry · 2009

Researchers observed that about 40% of breast cancers rely on the hormone estradiol, which is produced from estrone. They found that while current treatments target one enzyme to reduce estradiol, another enzyme, estrone sulfatase, also contributes to its production in tumors. This has led to the development of new inhibitors that could help in treating hormone-dependent breast cancer more effectively.

  • Approximately 40% of breast cancers are hormone-dependent.
  • Current treatments do not fully prevent estradiol production in tumors.
  • New inhibitors targeting estrone sulfatase are being developed to improve treatment.
PubMed

New development in intracrinology of breast carcinoma.

Review

Breast cancer (Tokyo, Japan) · 2006

Researchers observed that certain enzymes in breast tumors, particularly 17beta-HSD type 1, play a crucial role in producing estrogens that can fuel cancer growth. They found that targeting these enzymes, along with aromatase, may offer new treatment options for breast cancer patients, especially postmenopausal women. The study highlights the variability of these enzymes in different patients, suggesting personalized approaches to therapy.

  • 17beta-HSD type 1 is linked to increased estrogen levels in breast tumors.
  • Inhibiting 17beta-HSD type 1 could reduce tumor growth by lowering estrogen.
  • The presence of estrogen sulfotransferase (EST) is associated with better prognosis in breast cancer.
PubMed

Absorption and metabolism of estrogens from the stomach and duodenum of pigs.

Unknown

Domestic animal endocrinology · 1994

Researchers observed that when 17 beta-estradiol (E2) was introduced into the stomach of pigs, it was quickly converted into other forms before entering the bloodstream. They found that most of the E2 was metabolized in the stomach and liver, with significant levels of its metabolites detected in the blood. Additionally, the presence of gut bacteria influenced the absorption and metabolism of estrogens from bile.

  • Most E2 was converted to other forms before entering the bloodstream.
  • The stomach and liver play key roles in metabolizing estrogens.
  • Gut bacteria affect the absorption and metabolism of estrogens from bile.
PubMed

Pharmacokinetics of oestrogens and progestogens.

Review

Maturitas · 1990

Researchers observed significant variations in hormone levels from both natural and synthetic steroids, influenced by how they are taken. They found that oral steroids affect liver metabolism more than other methods, and that different forms of estrogen and progestin have varying impacts on hormone activity and effectiveness.

  • Oral steroids have a stronger effect on liver metabolism than other administration routes.
  • Oestrone and oestradiol can convert into each other, but oestrone is a weaker estrogen.
  • Different progestogens affect liver metabolism differently, with some being more potent at lower doses.
PubMed

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This page is for informational and research purposes only. All information is based on published scientific literature. Nothing on this page constitutes medical advice or replaces consultation with a qualified healthcare professional.