Uses of hydroxyl polymethoxylflavones (HPMFs) and derivatives thereof

a technology of hydroxyl polymethoxylflavones and derivatives, which is applied in the direction of biocide, drug composition, metabolic disorders, etc., can solve the problems of large cost of body weight reduction surgery such as cosmetic surgery and laparoscopic gastric bypass surgery, and the occurrence of many chronic illness diseases. , to achieve the effect of inhibiting lipogenesis and decreasing the lipid accumulation surrounding

Active Publication Date: 2015-02-19
PAN MIN HSIUNG +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0006]The present invention relates a hydroxyl polymethoxylflavones compound, hereinafter referred to as a HPMFs compound, which is extracted from citrus fruits. The HPMFs compound has ability for inhibition of lipogenesis and adipocyte differentiation, and decreasing the lipid accumulation surrounding the internal organs without alteration on the rate of food intake. Therefore, the HPMFs compound or derivative thereof can serve as an active ingredient of a composition for treating or preventing obesity-related diseases.

Problems solved by technology

In Taiwan, the nutritional health reports from 2004 to 2008 had suggested that the excessive nutrition would cause the occurrence of many chronic illness diseases.
Therefore, the rush modern life style makes it difficult to low body weight through exercise and calorie control.
Furthermore, the cost of the surgeries for lowing body weight such as cosmetic surgery and laparoscopic gastric bypass surgery are quite expansive.
In addition to the expansive cost, the surgeries may bring some uncertain risk for the safety of patients.
However, intake of these drugs for a long term will bring some side effects to the subjects.
Because these indicated natural extracts do not achieve the purpose for lowing weight through controlling the cell cycle of adipocytes, inhibiting adipocytes differentiation, promoting the lipolysis in adipocytes, the functions of these extracts are not efficient and obvious.

Method used

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  • Uses of hydroxyl polymethoxylflavones (HPMFs) and derivatives thereof
  • Uses of hydroxyl polymethoxylflavones (HPMFs) and derivatives thereof
  • Uses of hydroxyl polymethoxylflavones (HPMFs) and derivatives thereof

Examples

Experimental program
Comparison scheme
Effect test

example 1

Preparation of the HPMFs Compound

[0049]10 grams of orange peel extract that contained HPMFs for more than 40% was dissolved in 95% ethanol and added with 3M of hydrochloric acid (HCl). The indicated mixture was incubated with heating circumfluence and monitored by using TLC and LC / MS for 12 hours. Until the reaction finished and cooled, ethanol was removed by vacuum device. In the following step, ethyl acetate and water were added for separation and extraction. An organic solvent phase of the extract was collected, first. The remained aqueous phase was further extract by acetyl acetate again for isolating the organic solvent phase.

[0050]The organic solvent phases were pulled together, diluted with sodium bicarbonate solution, water and 30% NaCl solution for wash, and then dehydrated with sodium sulfate. After filtration, decompression concentration and lyophilized, the gained pale yellow solid substance is a HPMFs compound.

example 2

Culture of 3T3-L1 Pre-Adipocytes

[0051]The 3T3-L1 pre-adipocytes were cultured in 10 cm culture dish with DMEM medium, which contains 10% fetal bovine serum (FBS), 10000 unit / mL of penicillium and 10000 μg / mL streptomycin, at 37° C., 5% CO2, incubator. When the growing cells occupied 70%-80% area of the cultured dish, depletion of cultured medium was followed by PBS washing. The cultured cells were added trypsin-EDTA at 37° C. After the enzymatic digestion, the cultured cells were disassociated from the dish by gentle beats and then adding fresh FBS-containing medium to terminate the enzymatic activity of trypsin-EDTA. The disassociated cells were further well separated by pipetting using pipetman several times. The cells were evenly distributed in the culture dishes and then incubated at 37° C., 5% CO2 incubator.

example 3

Differentiation Test of 3T3-L1 Pre-Adipocytes

[0052]The 3T3-L1 pre-adipocytes seeded into 24-wells plate were cultured in FBS-containing DMEM medium for 3 days. In the following step, the original medium was replaced by another fresh FBS-containing medium for 2 days extension culture. The day after 2 days extension culture is destined as the “day 0”.

[0053]On day 0, the 3T3-L1 pre-adipocytes cultured with different conditions were treated with DMI inductance (DEX+MIX+insulin) for 2 days (day 2) to induce the adipocyte differentiation. After the induction of adipocyte differentiation, the induction medium was replaced by a fresh DMEM medium that contains 10% FBS and 5 μg / mL INS for at least 2 days culture (day 4). On day 4, day 6 and day 8, the culture medium was further replaced by the new 10% FBS-containing DMEM medium.

[0054]During the culture from day 0 to day 8, the morphology of the 3T3-L1 pre-adipocytes was observed every 2 days and the results were shown in FIG. 1A-1E. In additi...

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Abstract

The invention discloses the uses of hydroxyl polymethoxylflavones and derivative thereof that are relative to inhibit adipogenesis and lower lipid accumulation, wherein the hydroxyl polymethoxylflavones is obtained from the peels of Citrus genus plants. Therefore, the hydroxyl polymethoxylflavones that of a therapeutically effective amount not only can be a medical compound for treatment obesity or fatty liver, but also can be a food element.

Description

CROSS-REFERENCE TO RELATED APPLICATION[0001]The current application claims a foreign priority to the patent application of Taiwan No. 102129499 filed on Aug. 16, 2013.FIELD OF THE INVENTION[0002]The present invention relates generally to the uses of the nature compound. In particular, the present invention relates to uses of hydroxyl polymethoxylflavones (HPMFs) and derivatives thereof.BACKGROUND OF THE INVENTION[0003]According to the previous reports, obesity is resulted from that assimilated calorie is much than consumption. The excessive calorie is stored as triglyceride (hereinafter referred to as TG) in adipose tissue and thereby accumulated in pancreas, liver, skeleton muscle. The accumulation of triglyceride in these indicated organs causes obesity and metabolic syndrome such as cardiovascular diseases, hypertension, hyperlipidemia and type II diabetes. Currently, WHO has been categorized obesity as a chronic illness disease. In Taiwan, the nutritional health reports from 200...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/353A61K36/752
CPCA61K36/752A61K31/353A61K2236/00A61K31/352A61P1/16A61P3/00A61P3/04
Inventor PAN, MIN-HSIUNGWU, CHIA-LI
Owner PAN MIN HSIUNG
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