Saturday, January 21, 2023

Cholesterol

 Cholesterol

Introduction

Cholesterol from the Ancient Greek chole (bile) and stereos (solid), followed by the chemical suffix -ol for an alcohol is an organic molecule. Cholesterol is biosynthesized by all animal cells and is an essential structural component of animal cell membranes. It is a complex monohydric secondary alcohol of the sterol class. With fatty acids it forms waxes.

Chemistry and Properties

It is a sterol (or modified steroid), a type of lipid. It is a stable white, crystalline substance, insoluble in water but readily soluble in chloroform, ether, alcohol and other fat-solvents. The crystals have a rhombic or rectangular shape, with one corner broken off.

Distribution

The distribution of cholesterol is as follows-

(1) It is present in all cells-both in the cell membrane and cytoplasm. It is a part of the element constant

(2) All body fluids contain cholesterol excepting cerebrospinal fluid (CSF) in which the amount is negligible.

(3) It may exist in the Free State as well as in the form of esters, but these two forms are not equally distributed everywhere. In bile it is present only in the free form.

 (4) Brain contains 17% of it and it is mainly in free form and suprarenal glands contain the largest amount.

(5) Blood cholesterol Normal blood cholesterol varies between 150-200 mg per 100 ml which is equally distributed between plasma and corpuscles. But in the corpuscles it is present chiefly in the free form, while in the plasma the major part remains as esters.

(6) The free cholesterol content of a tissue is characteristic and normally remains very constant but the cholesterol esters may vary in amount.

(7) The distribution of cholesterol in different types of muscles is directly proportional to their degree of activity. The cardiac and smooth muscles have more cholesterol content than the voluntary muscles. Moreover, the amount of cholesterol in any tissue is roughly proportional to their degree of activity.

(8) Cholesterol and phospholipids always remain together. Moreover, there appears to be a definite ratio between phospholipids and cholesterol for each tissue.

Synthesis of cholesterol

The sequence of reactions in the path of cholesterol synthesis is given below-

1. Activation of acetate to acetyl CoA.

2. Condensation of two acetyl CoA molecules to form acetoacetyl CoA.

3. Formation of HMG CoA.

4. Formation of mevalonic acid.

5. Mevalonic acid is phosphorylated by ATP to form 3-diphosphomevalonic acid.

6. The diphosphomevalonic acid after losing CO and H₂O gives rise to isopentenyl pyrophosphate.

7. The above compound isomerizes to form 3-3-dimethylallyl pyrophosphate which combines with isopentenyl pyrophosphate to give geranyl pyrophosphate.

8. Another molecule of isopentenyl pyrophosphate combines with geranyl pyrophosphate to form farnesyl pyrophosphate.

9. Two molecules of farnesyl pyrophosphate combine to forms qualene.

10. An oxidocyclase converts squalene to lanosterol.

11. Lanosterol is converted to cholesterol via either of two pathways, the Bloch pathway, or the Kandutsch-Russell pathway.
 

Absorption and Storage

More than 50% and sometimes up to 80% of cholesterol which is absorbed from intestines is secreted by liver and is a part of bile. Ingested cholesterol requires fat for its absorption from the lumen of the intestine into the lymphatics. These are esterified with fatty acids in the intestinal epithelium during their passage into the lymphatics.

A human male weighing 68 kg (150 lb) normally synthesizes about 1 gram (1,000 mg) of cholesterol per day, and his body contains about 35 g, mostly contained within the cell membranes. Typical daily intake in diet is 300 mg daily for average person.

Most ingested cholesterol is esterified, which causes it to be poorly absorbed by the gut. The body also compensates for absorption of ingested cholesterol by reducing its own cholesterol synthesis. For these reasons, cholesterol in food, seven to ten hours after ingestion, has little effect on concentrations of cholesterol in the blood.  During the first seven hours after ingestion of cholesterol, as absorbed fats are being distributed around the body within extracellular water by the various lipoproteins (which transport all fats in the water outside cells), the concentrations increase.

Plants make cholesterol in very small amounts. In larger quantities they produce phytosterols, chemically similar substances which can compete with cholesterol for reabsorption in the intestinal tract, thus potentially reducing cholesterol reabsorption. When intestinal lining cells absorb phytosterols, in place of cholesterol, they usually excrete the phytosterol molecules back into the GI tract, an important protective mechanism.

The intake of naturally occurring phytosterols, which encompass plant sterols and stanols, ranges between 200–300 mg/day depending on eating habits. A good portion of cholesterol remains in the cells of reticulo endothelial system. It is utilized in various body functions and mostly recycled.

Functions of cholesterol

1. Essential constituent of all cells-It is a part of the element constant of the cells. Cholesterol composes about 30% of all animal cell membranes. It is required to build and maintain membranes and modulates membrane fluidity over the range of physiological temperatures.

The hydroxyl group of each cholesterol molecule interacts with water molecules surrounding the membrane, as do the polar heads of the membrane  phospholipids and Sphingolipids, while the bulky steroid and the  hydrocarbon chain are embedded in the membrane, alongside the non polar fatty-acid chain of the other lipids.

Through the interaction with the phospholipid fatty-acid chains, cholesterol increases membrane packing, which both alters membrane fluidity and maintains membrane integrity so that animal cells do not need to build cell walls (like plants and most bacteria). The membrane remains stable and durable without being rigid, allowing animal cells to change shape and animals to move.

2. Controls cell permeability and transport-As it maintains integrity of cell membrane it controls the permeability of the cells. Within the cell membrane, cholesterol also functions in intracellular transport, cell signaling and nerve conduction.

3. Prevents haemolysis- Low blood cholesterol is associated with haemolysis.

4. Defensive action- Cholesterol is intimately related to the defensive mechanism of the body. During acute infections blood cholesterol falls and tends to rise during recovery.

5. Fat transport- A large part of fat is transported through blood as cholesterol esters.

6. Formation of cholic acid (bile salts) -Cholesterol is the mother substance from which cholic acid is synthesized. Cholic acid is a constituent of bile salts.

7. Antilipotropic action- Cholesterol feeding increases the deposition of fat in the liver. This effect is due to the formation of cholesterol esters and depression of phospholipid formation in the liver.

8. Controls cell division-Rapidly growing tissues are very rich in cholesterol, such as, the granulation tissues of healing ulcer and rapidly growing tumours, etc.

9. Antagonistic to phospholipids-Its physicochemical properties are antagonistic to phospholipids; hence, they are always found together.

10. Parent substance-It is a parent substance of all the steroid hormones of sex glands, adrenal cortex as well as Vitamin D.

Excretion of cholesterol

Excretion takes place in the following ways:

(1) Through bile-It is found as free cholesterol but a good part of it is reabsorbed from the intestine.

(2) Through feces-A part of the bile cholesterol undergoes bacterial putrefaction in the intestine and is excreted as coprosterol. But a small amount of free cholesterol is also found in the stool.

(3) Through urine-It appears in the urine only in traces, but appears in larger amounts in different diseases namely in hypercholesteremia.

(4) Through skin-Sebum, secretion of the sebaceous glands of the skin contains large quantities of cholesterol and thus drying of the skin is prevented by sebum due to its cholesterol constituent.

Blood cholesterol in pregnancy- During pregnancy blood cholesterol rises and rapidly comes back to normal after delivery. It may be that this rise is due to hyperactivity of the adrenal cortex, produced during pregnancy and the exact function is not known. It may be associated with the rapid cell division and the tissue differentiation of the foetus. This high cholesterol ensures the supply of the mother substance from which large amounts of sex hormones are manufactured during pregnancy.

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