Guggulipid

Source

Guggulipid is a standardized extract of the oleo gum resin of the mukul myrrh tree, Commiphora mukul (Burseraceae), native to India. Shuddha guggulu is a processed form of the resin used in traditional Ayurvedic medicine for the treatment of epilepsy, ulcers, obesity, rheumatoid arthritis and atherosclerosis since 600 BC.

The gummy resin exudate is harvested from the plants’ bark through tapping. This product called gum guggulu is used in incense and perfumes for its fragrance. It is processed to separate the essential oil and the gum from the resinous portion.

Chemically guggulu is a complex mixture of steroids, diterpenoids, aliphatic esters, carbohydrates and several inorganic ions. Extracts of the oleoresin contain compounds known to have hypolipidaemic activity such as guggulusterols I, II and III and stereoisomeric guggulusterones (Z and E). Other biologically active constituents include myrrhanol A and myrrhanone – known to have anti-inflammatory activity – and two ferulic acid esters – (Z)-5-tricosene-1,2,3,4-tetraol and (Z)-5-tetracosene-1,2,3,4-tetraol – reported to have anti-tumour properties.

Uses

Research studies showed that guggul is beneficial in cardiovascular disease. Guggulsterones were comparable to cardioprotective drugs propanolol and nifedipine in protecting from myocardial necrosis induced by isoproterenol in rats. Guggul reduced the stickiness of platelets, and is reported to be used in the treatment of hyperlipoproteinemia. Fractions of guggulu rich in guggulusterones are known to have hypocholesterolemic activity. They inhibit cholesterol synthesis in the liver via antagonism of the farnesoid X receptor and the bile-acid receptor. Guggulusterones up-regulate the bile salt export pump (BSEP), an efflux transporter responsible for the removal of cholesterol metabolites and bile acids from the liver. This favours the metabolism of cholesterol into bile acids. Guggulusterones inhibit the activation of nuclear factor kappa B, a critical regulator of inflammatory responses. There are some patents for the use of guggulu in cosmetics.

Description

The oleoresin present in ducts under the soft bark tissue when tapped oozes out as a pale yellow, aromatic fluid that turns into an ‘agglomerate of tears or stalactic pieces’ that are reddish brown, golden brown or dull green. An average of about 700 to 900 g resin may be collected from each tree. This product called gum guggulu is processed to separate the essential oil and the gummy portion. This is normally done by hot expression at 120–130°C, with a yield of 51%, or by solvent extraction, with a yield of 61%.

The oleo resin of gum guggulu occurs as an off white to pale yellow dusty powder or granules. Like other resins it fuses on heating and forms a milky emulsion with hot water. It mixes well with vegetable waxes, stearic acids and other resins.

It has an acrid odour and a bitter taste. It is soluble in water, alcohol (≥60%w/w) and petroleum ether, ethyl acetate, castor oil, drying oils and turpentine (≥40%w/w). A 1%w/v solution in water has a pH of 5–7. The resin of gum guggulu also acts as a binding agent and there is no need to add a binding agent when it is being formulated into tablets.

The purified resin contains 2% guggulsterones. Guggulusterones when purified occur as white amorphous powder poorly soluble in water and soluble in DMSO.


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