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Obesity and metabolic syndrome treatment with tanshinone derivatives which increase metabolic activity

A technology for metabolic syndrome and derivatives, applied in metabolic diseases, drug combinations, organic active ingredients, etc.

Inactive Publication Date: 2007-01-24
MD BIOALPHA CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] 1. Sugar metabolism

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

Embodiment 1

[0109] Embodiment 1: the separation of tanshinone derivatives

[0110] Buy 5kg of Danshen (Salvia miltiorrhiza) from the Chinese medicine store, and collect from the fields and mountains or buy other necessary materials from the Chinese medicine store. Salvia miltiorrhiza was eluted with 50 L of methanol for 24 hours, and concentrated under reduced pressure. To the resulting material was added 1500 mL of water. Then, add an equal amount of n-hexane, dichloromethane (CH 2 Cl 2 ) and ethyl acetate (EtOAc), followed by sequential extraction twice to obtain a gelatinous red extract. When the activity was measured on the different layers obtained here, the activity was highest in the dichloromethane layer.

[0111] Silica gel (Kieselgel 60, 230-460 mesh, Merck) was well swelled with 100% n-hexane and loaded into a column (530 cm high). Will be from the CH 2 Cl 2 50 g of the extract obtained from the layer was dissolved in traces of EtOAc and n-hexane, and the resulting sampl...

Embodiment 2

[0114] Embodiment 2: Structural analysis of various active materials

[0115] The structures of cryptotanshinone, tanshinone I, tanshinone IIA and 15,16-dihydrotanshinone I in Example 1 were respectively determined by NMR analysis.

[0116] Cryptotanshinone

[0117] 1H-NMR (CDCl 3 ): δ7.42 (2H, ABq, J = 8.0Hz), 4.83 (1H, t, J = 9.2Hz), 4.31 (1H, dd, J = 9.2 and 6.0Hz), 3.55 (1H, m), 3.17 (2H, br t), 1.65 (4H, m), 1.40 (3H, d, J=6.8Hz), 1.28 (6H, s)

[0118] 13C-NMR (CDCl 3 ): δ9.58(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)

[0119] Tanshinone IIA

[0120] 1H-NMR (CDCl 3 , 300.40MHz) δ7.63 (1H, d, J = 8.2Hz), 7.54 (1H, d, J = 8.2Hz), 7.22 (1H, s), 3.18 (2H, t, J = 6.6Hz), 2.26 (3H, s), 1.78 (2H, m), 1.65 (2H, m), 1.31 (6H, s).

[0121] 13C-NMR (CDCl 3 , 75.45MHz) δ184.2...

Embodiment 3

[0128] Embodiment 3: Determination of AMPK activity

[0129] Myoblasts, C2C12, were cultured in DMEM medium containing 10% calf serum. When the cell density reached about 85%-90%, the medium was replaced with a medium with 1% calf serum, thereby inducing differentiation of the cells. The enzymatic activity of AMPK was then assayed as follows. C2C12 cells were lysed to obtain a protein extract, and then ammonium sulfate was added to a final concentration of 30%, followed by protein precipitation. The protein pellet was dissolved in buffer (62.5 mM Hepes, pH 7.2, 62.5 mM NaCl, 62.5 mM NaF, 1.25 mM sodium pyruvate, 1.25 mM EDTA, 1 mM DTT, 0.1 mM PMSF and 200 μM AMP). Then, 200 μM SAMS peptide (HMRSAM S GLHLVKRR: The underlined serine residue is the phosphorylation site, as the AMPK phosphorylation site of acetyl CoA carboxylase) and [γ-32P]ATP, and the reaction was reacted at 30°C for 10 minutes. The resulting reaction solution was then sprayed onto p81 phosphocellulose paper...

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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 invention [0001] The present invention relates to a composition for preventing and treating metabolic syndrome, which contains a tanshinone derivative as an effective component. More specifically, the present invention relates to a composition for the prevention and treatment of metabolic syndrome comprising, as an active ingredient, a tanshinone derivative exhibiting excellent activity in enhancing metabolic activity. Background of the invention [0002] Metabolic syndrome refers to a syndrome including health risk factors such as hypertriglyceridemia, hypertension, glucose metabolism disorder, blood coagulation disorder, and obesity. Metabolic syndrome is not fatal, but it indicates a predisposition to serious diseases such as diabetes and ischemic cardiovascular disease, and has evolved into the most threatening disease of the modern population. Due to lack of understanding of the etiology of this syndrome, metabolic syndrome was once known by a variety of other...

Claims

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Application Information

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IPC IPC(8): A61K31/343A61K36/537A61P3/04
Inventor 郭泰焕朴明奎
Owner MD BIOALPHA CO LTD
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