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Compositions and methods for treating hypercholesterolemia using ortanique peel extract

a technology of ortanique peel and hypercholesterolemia, which is applied in the direction of biocide, plant growth regulator, plant ingredients, etc., can solve the problems of adverse effects, several adverse effects, and enormous burden on the global healthcare system, and achieve the effect of effective hypercholesterolemia and effective hypercholesterolemia treatmen

Inactive Publication Date: 2010-01-21
UNIVERSITY OF THE WEST INDIES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0008]The invention is based, in part, on the discovery that the Ortanique peel extract is effective in treating hypercholesterolemia without the side effects of existing drugs, such as statins and niacin, and in part, on the discovery that the Ortanique peel extract is more effective in treating hypercholesterolemia compared to peel extracts from other citrus fruits.

Problems solved by technology

Hypercholesterolemia is implicated in many cardiovascular diseases affecting people worldwide and pose tremendous burden on the global healthcare system.
Although these drugs are effective in lowering serum cholesterol levels, they cause several adverse effects.
Niacin can cause adverse effects such as flushing, abdominal pain, vomiting, headache, or elevated serum aminotransferase levels indicating liver damage.
A vast majority of the citrus fruits that are harvested are used for citrus juice production, which results in large quantities of citrus peel and other citrus byproducts which end up in river beds and constitute environmental problems.

Method used

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  • Compositions and methods for treating hypercholesterolemia using ortanique peel extract

Examples

Experimental program
Comparison scheme
Effect test

example 1

7.1 Example 1

Preparation of Ortanique Peel Extract

[0070]Jamaican indigenous Ortanique fruit was harvested. The fruits were thoroughly washed and peeled. The peel was dried in the sun for 4-8 days and milled to fine powder using a commercial blender. The powdered peel was then extracted with reagent grade methanol (3×500 mL) at room temperature for 24 hours with constant stirring. The mixture was filtered, and the filtrate was evaporated via rotary evaporation. The resulting solids were first air-dried, then further dried in an oven at 70° C. to provide the Ortanique peel extract (PMF-ORT) as a solid.

example 2

7.2 Example 2

Determination of the Composition of Ortanique Peel Extract

[0071]The Ortanique peel extract was characterized using reverse-phase high performance liquid chromatography (HPLC) with UV detection. Elution was carried out in the gradient mode, using a ternary mobile phase. The polymethoxylated flavone components of Ortanique citrus peel extract and their respective quantities were determined using this method.

[0072]The Ortanique PMF extract was found to contain the following combination of six different PMFs: nobiletin (5,6,7,8,3′,4′-hexamethoxyflavone), sinensetin (5,6,7,3′,4′-pentamethoxyflavone), tangeretin (5,6,7,8,4′-pentamethoxyflavone), heptamethoxyflavone (3,5,6,7,8,3′,4′-heptamethoxyflavone), hexamethyl-o-quercetagetin (3,5,7,8,3′,4′-hexamethoxyflavone) and tetramethylscutellarein (5,6,7,4′-tetramethoxyflavone), in the following proportions by weight: 18% nobiletin, 17.5% tetramethylscutellarein, 7% sinensetin, 16% tangeretin, 1.3% hexamethyl-o-quercetagetin, and 2...

example 3

7.3 Example 3

Determination of Efficacy of Ortanique Peel Extract

[0073]To determine the effects of Ortanique peel extract on various cholesterol levels, the following animal model experiments were carried out.

[0074]Thirty Sprague-Dawley rates were divided into five groups. Group 1 consisted of healthy rats fed a normal diet. Group 2 consisted of diet-induced hypercholesterolemic rats. Group 3 consisted of healthy rats fed Ortanique peel extract. Group 4 consisted of diet-induced hypercholesterolemic rats fed Ortanique peel extract. Group 5 consisted of diet-induced hypercholesterolemic rats fed niacin, a common cholesterol reducing drug. The normal diet consisted of normal rat chow. Rats were made hypercholesterolemic by being fed a diet consisting of 1% cholic acid and 4% cholesterol mixed with the normal rat chow. Rats that were fed Ortanique peel extract were fed normal rat chow mixed with Ortanique peel extract that consisted of 1.5% Ortanique peel extract by weight. Rats were fe...

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Abstract

The invention relates to compositions and methods for treating hypercholesterolemia, including methods for increasing HDL cholesterol levels, using a composition comprising an extract from the Ortanique peel. The invention also relates to compositions and methods for treating hypercholesterolemia, including methods for increasing HDL cholesterol levels, using a composition comprising substantially similar amounts of tetramethylscutellarein and nobiletin by weight and / or a composition comprising substantially similar amounts of tetramethylscutellarein, nobiletin, and tangeretin by weight.

Description

1. REFERENCE TO RELATED APPLICATIONS[0001]This application claims the benefit of priority to U.S. Provisional Patent Application No. 61 / 081,916, filed Jul. 18, 2008, the entire disclosure of which is incorporated by reference herein in its entirety.2. FIELD OF THE INVENTION[0002]The present invention relates generally to treatment and prevention of hypercholesterolemia.3. BACKGROUND OF THE INVENTION[0003]Familial hypercholesterolemia affects approximately 1 in 500 people worldwide, and the elevated serum cholesterol concentrations associated with it contributes more than 50% to the risk of fatal or non-fatal coronary heart disease by age 50 in men, and at least 30% in women aged 60 and above. The prevalence of hypercholesterolemia in Jamaica is estimated at 31 %. It is estimated that about 37%, or 101 million people in the United States suffer from hypercholesterolemia.[0004]Hypercholesterolemia is implicated in many cardiovascular diseases affecting people worldwide and pose tremen...

Claims

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Application Information

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IPC IPC(8): A61K36/752A61K31/352A61P3/06
CPCA61K31/352A61P3/06
Inventor GREEN, CURTIS O.ASEMOTA, HELEN N.
Owner UNIVERSITY OF THE WEST INDIES
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