Obesity and Metabolic Syndrome Treatment with Tanshinone Derivatives Which Increase Metabolic Activity

a technology of tanshinone and metabolic syndrome, which is applied in the direction of pill delivery, plant/algae/fungi/lichens ingredients, dispersion delivery, etc., can solve the problems of metabolic syndrome, inability of cells to perform normal functions, and insufficient glucose supply of insulin to cells, so as to prevent and treat metabolic syndrome and activate metabolism. , the effect of

Inactive Publication Date: 2007-10-25
MD BIOALPHA CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0017] The present inventors have conducted a variety of extensive and intensive study and experimentation. As a result of such extensive investigation, the inventors have found that tanshinone derivatives, extracted from Danshen (Salvia miltiorrhiza), have efficacy activating metabolism in cells and tissues, and further found that when ob / ob mice, a model of obesity caused by decreased secretion of leptin, db / db mice, a model of obesity / diabetes, and DIO (diet-induced obesity) mice, caused by high fat dietary conditions, are treated with tanshinone derivatives, these materials are effective for preventing and treating metabolic syndrome including obesity and diabetes mellitus. The present invention has been completed based on these findings.
[0066] The term “a health and functional food” used throughout the specification of the present invention refers to a food in which tanshinone derivatives are added to general foods to improve functions thereof. Tanshinone derivatives may be added to general foods or may be prepared in the form of capsules, powders, suspensions and the like. Intake of such a health and functional food containing tanshinone derivatives provides beneficial effects for health, and exhibits advantages in that there are no side effects caused by prolonged use of drugs because food material is used as the raw material, unlike conventional drugs.

Problems solved by technology

Insulin resistance refers to a phenomenon wherein, even though insulin is normally secreted in vivo, insulin does not induce sufficient supply of glucose to cells.
Therefore, glucose in the blood cannot enter cells, thus causing hyperglycemia, and thereby cells cannot perform normal functions due to a shortage of glucose, leading to the manifestation of metabolic syndrome.
At present, there are no drugs available for the treatment of metabolic syndrome.
Attempts have been made to treat metabolic syndrome using therapeutic agents for diabetes, hyperlipidemia and hypertension, but these drugs have limited effectiveness in treating metabolic syndrome as the drug.
Due to high calorie intake from processed foods and fast foods, compared to insufficient exercise, surplus energy is accumulated in the form of fat and thereby becomes an underlying cause of various diseases including metabolic disorders.
It was proposed that such dysregulation leads to alterations in cellular fatty-acid metabolism that in turn cause abnormal lipid accumulation, cellular dysfunction and ultimately disease.

Method used

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  • Obesity and Metabolic Syndrome Treatment with Tanshinone Derivatives Which Increase Metabolic Activity
  • Obesity and Metabolic Syndrome Treatment with Tanshinone Derivatives Which Increase Metabolic Activity
  • Obesity and Metabolic Syndrome Treatment with Tanshinone Derivatives Which Increase Metabolic Activity

Examples

Experimental program
Comparison scheme
Effect test

example 1

Isolation of Tanshinone Derivatives

[0094] 5 kg of Danshen (Salvia miltiorrhiza) material was purchased from a Chinese medicinal herb shop and other necessary materials were collected in fields and mountains or were purchased from the shop. Danshen was eluted with 50 L of methanol for 24 hours and concentrated under reduced pressure. 1500 mL of water was added to the resulting material. Then, an equal amount of n-hexane, dichloromethane (CH2Cl2) and ethyl acetate (EtOAc) were added and sequentially extracted two times so as to obtain a gelatinous red extract. When activity was examined on the respective layers thus obtained, the activity was highest in the dichloromethane layer.

[0095] Silica gel (Kieselgel 60, 230 to 460 mesh, Merck) was sufficiently swelled with 100% n-hexane and then packed into a column (530 cm high). 50 g of the extract obtained from the CH2Cl2 layer was dissolved in a trace amount of EtOAc and n-hexane and the resulting sample was loaded onto the column. After...

example 2

Structural Analysis of Separated Active Material

[0098] NMR analysis was performed to determine structures of cryptotanshinone, tanshinone I, tanshinone IIA and 15,16-dihydrotanshinone I separated in Example 1, respectively.

Cryptotanshinone

[0099] 1H-NMR (CDCl3): δ 7.42 (2H, ABq, J=8.0 Hz), 4.83 (1H, t, J=9.2 Hz), 4.31 (1H, dd, J=9.2 and 6.0 Hz), 3.55 (1H, m), 3.17 (2H, br t), 1.65 (4H, m), 1.40 (3H, d, J=6.8 Hz), 1.28 (6H, s)

[0100] 13C-NMR (CDCl3): δ 9.58 (C-1), 19.00 (C-2), 37.73 (C-3), 34.76 (C-4), 143.57 (C-5), 132.48 (C-6), 122.43 (C-7), 128.30 (C-8), 126.19 (C-9), 152.28 (C-10), 184.16 (C-11), 175.59 (C-12), 118.21 (C-13), 170.66 (C-14), 81.38 (C-15), 34.54 (C-16), 18.74 (C-17), 31.85 (C-18), 31.80 (C-19)

Tanshinone II-A

[0101] 1H-NMR (CDCl3, 300.40 MHz) δ 7.63 (1H, d, J=8.2 Hz), 7.54 (1H, d, J=8.2 Hz), 7.22 (1H, s), 3.18 (2H, t, J=6.6 Hz), 2.26 (3H, s), 1.78 (2H, m), 1.65 (2H, m), 1.31 (6H, s).

[0102] 13C-NMR (CDCl3, 75.45 MHz) δ 184.29, 176.43, 162.38, 150.80, 145.14, 14...

example 3

Determination of AMPK Activity

[0107] Myoblast cells, C2C12, were cell cultured in DMEM containing 10% bovine calf serum. When cell density reached a range of about 85% to 90%, the culture medium was replaced with 1% bovine calf serum medium to induce differentiation of cells. Enzymatic activity of AMPK was determined as follows. C2C12 cells were lysed to obtain protein extracts and then ammonium sulfate was added to a final concentration of 30%, followed by precipitation of proteins. Protein precipitates were dissolved in a buffer (62.5 mM Hepes, pH 7.2, 62.5 mM NaCl, 62.5 mM NaF, 1.25 mM Na pyrophosphate, 1.25 mM EDTA, 1 mM DTT, 0.1 mM PMSF, and 200 μM AMP). Thereafter, 200 μM SAMS peptide (HMRSAMSGLHLVKRR: the underlined serine residue is a phosphorylation site, as an AMPK phosphorylation site of acetyl-CoA carboxylase) and [γ-32P]ATP were added thereto and reactants were reacted for 10 minutes at 30° C. This was followed by spotting of the resulting reaction solution on p81 phos...

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Abstract

The present invention relates to a composition for preventing and treating metabolic syndrome, containing tanshinone derivatives as an effective ingredient. More specifically, the present invention relates to a composition for preventing and treating metabolic syndrome, containing tanshinone derivatives that exhibit superior activity in enhancing metabolic activity, as an effective ingredient.

Description

FIELD OF THE INVENTION [0001] The present invention relates to a composition for preventing and treating metabolic syndrome, containing tanshinone derivatives as an effective ingredient. More specifically, the present invention relates to a composition for preventing and treating metabolic syndrome, containing tanshinone derivatives that exhibit superior activity in enhancing metabolic activity, as an effective ingredient. BACKGROUND OF THE INVENTION [0002] Metabolic syndrome refers to syndrome involving health risk factors such as hypertriglyceridemia, hypertension, glycometabolism disorder, blood coagulation disorder and obesity. Metabolic syndrome itself is not fatal, but indicates a predisposition to severe diseases such as diabetes and ischemic cardiovascular diseases, and has emerged as the most threatening diseases among modern people. Metabolic syndrome was once lmown by various other names including Syndrome X, due to lack of knowledge about causes of such syndrome, but was...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K36/537A61P3/04A23C9/152A23L1/30A23L2/02A23L2/52A61K9/00A61K31/343A61K36/00
CPCA23C9/152A23L1/3002A23L2/02A23L2/52A23V2002/00A61K8/4973A61K9/0095A61K9/2054A61K31/343A61K36/537A61Q19/06A61K2300/00A23V2250/0606A23V2250/032A23V2250/704A23V2200/332A23V2200/328A23V2200/326A23V2250/708A23V2250/606A23V2250/5042A23L33/105A61P1/04A61P1/16A61P11/00A61P13/12A61P15/08A61P15/10A61P17/18A61P19/02A61P25/00A61P25/08A61P25/16A61P25/28A61P27/02A61P27/12A61P29/00A61P3/02A61P3/04A61P35/00A61P3/06A61P39/06A61P43/00A61P7/02A61P7/06A61P9/00A61P9/04A61P9/10A61P9/12A61P3/10
Inventor KWAK, TAEHWANPARK, MYUNGGYU
Owner MD BIOALPHA CO LTD
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