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PHYTOESTROGENS

Under the Guidance of, Prepared By,Mrs.Sandhya.M, M.PHARM., Lakshmi Sindhura.A

Associate professor. Reg.No.10T21S0107

CMR COLLEGEOF PHARMACY KANDLAKOYA (V), HYDERABAD - 501401

CONTENTS

Introduction

Estrogen

Clinical uses of Estrogens

Disadvantages of Estrogens

Menopause

Phytoestrogens

Mechanism of action

Advantages

Products

Conclusion

PHYTOESTROGENS:

Plant derived xenoestrogens.

Not generated within endocrine system.

Also called “DIETARY ESTROGENS”.

Structural similarity with Estradiol.

ESTROGEN:

Main sex hormone in women. Essential to the menstrual cycle. Estrone, estradiol, estriol. Contributes to the development of secondary sex

characteristics. Important to a woman’s health. Reduces after menopause.

BIOSYNTHESIS:

MECHANISM OF ACTION:

Readily diffuses across cell membrane.

Activate estrogen receptors.

ER-a and ER-b.ER-a Uterus, testis, pituitary, ovary, epididymis, and

adrenal gland.

ER-bBrain, kidney, prostrate, ovary, lung, bladder,

intestine, and epididymis.

ESTROGEN RECEPTORS:

MENOPAUSE:

Transition period.

Between ages of 45 and 55.

Body produces less estrogen and

progesterone.

Premature menopause

Perimenopause

Surgical menopause

Symptoms:

Hot flashes, Osteoporosis, Skin dryness.

CLINICAL USES:

Oral contaceptives.

Hormone replacement therapy.

Bulimia nervosa.

Estrogen preparations:

Ethinyl estradiol

Micronized estradiol

Diethylstilbestrol

SIDE EFFECTS DURING HORMONE REPLACEMENT THERAPY:

Risk of vein clots in legs by 2-3 fold

Uterine cancer

Breast cancer

Heart diseases

Abnormal vaginal bleeding

Stroke

High blood pressure

Gallstones.

These adverse effects diverted the attention from conventional estrogens and increased interest in phytoestrogens.

Natural and basically derived from food products.

However the efficacy of conventional estrogens in treating acute vasomotor and psychometric symptoms is much superior to that of phytoestrogens.

The rule of thumb is to use conventional estrogen for alleviation of grater efficacy and phytoestrogens should be used for long-term prevention as they are slow-acting, but safer on extended use.

PHYOESTROGENS

Dietary estrogens.

ADVANTAGES:

Easily broken down not stored in tissues and spend very little time in the body, thus they are unlikely to cause cancer.

Exert natural balancing levels in body.

The US Institute of health sciences announced that long use of synthetic estrogens increased healthy women’s risk of a sroke by 41%,heart attack by 29%, breast cancer by 24%

STRUCTURE:

Large group of substituted natural phenolic compounds.

Isoflavones, coumestons, lignans.

FOOD SOURCES:Soy food and flax seed have the highest amount of phytoestrogen.

Below is a short list of phytoestrogen food sources.

Flax-seed

Soy beans

Tofu

Soy yogurt

Sesame seed

Flax bread

Multigrain bread

EXTRACTION OF PHYTOESTROGENS FROM FOOD SOURCES:

To determine total phytoestrogen content , enzymatic hydrolysis with Aspergillums nigercellulase is carried out.

Acidified solvent extraction:

Raw soybean seeds with their seed coats are ground, mixed with 2ml 0.1N Hcl and 10ml of Acetonitrile, stirred for 2hrs at room temperature and filtered.

The filtrate is taken to dryness under vaccum at a temperature below 300c.

The dried material is redesolved and filtered and the filtrate is analysed through HPLC.

EXTRACTION OF LIGNANS:

Alkaline extraction of 0.1g of dry food is performed.

After extraction, the pH is adjusted to 5-6 with 750μ l of 100%glacial acetic acid and the extract is centrifuged at 4,500g for 10mins at 100c.

An aliquot is taken and methanol is evaporated from this at 600c.

A 1ml of aliquot is hydrolyzed by addition of Helix pomatia b glucuronidase and incubated over night at 370c.

Samples are transferred to HPLC vials for LC-MRM-MS analysis.

MECHANISM OF ACTION:

Phytoestrogens display somewhat higher affinity for ER-β compared to ER-α.

The key structural elements that enable phytoestrogens to bind with high affinity to estrogen receptors and display estradiol-like effects are:

The phenolic ring that is indispensable for binding to estrogen receptor.

Low molecular weight similar to estrogens (MW=272).

METABOLISM:

The two main isoflavonoids (genistien and diadzen) are present in all soy bean foods either as aglycone or as beta-glycoside(conjugated).

These glycosides are readily hydrolyzed to estrogenically active aglycones.

Genistien is further metabolized in gut to p-ethyl phenol, diadzein to equol, dihydrodiadzien to o-methylangolensin.

Further metabolism of isoflavonoids takes place by conjugating the aglycone with glucouronic acid and to lesser extent sulfuric acid.

Urinary isoflavonoid excretions range from about 0.3-30 μM/day.

Though phytoestrogens can be measured in urine, plasma, feces, semen, bile, saliva, and breast milk, the concentration of their metabolites differ widely among individuals.

This is due to gut microflora, antibiotic use, gender difference and concamitent dietary intake.

Urinary secretions of vegetarians may contain 1000 times higher phytoestrogens than total urinary steroid estrogens

USES:

Phytoestrogen supplements have a number of uses.

Menopause

Osteoporosis

Reduces risk of stroke

Reduces risk of cancer

PHYTOESTROGEN PRODUCTS:

Emerita PhytoEstrogen Cream: Hot Flashes Night Sweats Mood Swings Vaginal Dryness Urinary Incontinence

CHATTEM - REJUVEX (DISC), 30 CAPLETS: 

Rejuvex supplies 500mg of magnesium - essential for the support of strong healthy bones.

PHYTOESTROGEN &IPRIFLAVONES:

Use only as directed. Take two capsules daily with a meal or glass of water. Store in a cool, dry place.

CONCLUSION

Because of the adverse effects caused by harmone replacement therapy now a days there is diversion in attention from conventional estrogens and increase in interest in phytoestrogens. The great promise of phytoestrogen use is that they are natural and basically derived from food products; they can be successfully used in all stages of menopause, without any serious harmful effects. Today more and more people are turning to these naturally-occurring compounds as an alternative to man-made and potentially dangerous hormone replacement treatments.

 

REFRENCES

WWW.WIKIPEDIA.ORG 

WWW.MENOPAUSE-METAMORPHOSIS.COM 

WWW.DIETARYFIBERFOOD.COM 

WWW.JKSCIENCE.ORG  

WWW.IJP-ONLINE.COM 

WWW.NCBI.NLM.NIH.GOV

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