Pharmaceutical composition comprising shikonin derivatives from lithospermum erythrorhizon for treating or preventing diabetes mellitus and the use thereof

A technology of shikonin and composition, applied to the pharmaceutical composition comprising shikonin derivatives derived from shikonidum for treating or preventing diabetes and the field of use thereof, can solve the problem of no published compound research, no anti-diabetic effect. issues such as disclosure or teaching

Inactive Publication Date: 2010-02-10
珍岛郡
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] Isobutyrylshikonin, β,β-dimethylacryloylshikonin, isovalerylshikonin, α-methyl-n-butyrylshikonin and β-hydroxyisovalerylshikonin are Compounds contained in comfrey roots, but no research on these compounds has been disclosed, either at home or abroad, especially for their anti-diabetic effects.

Method used

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  • Pharmaceutical composition comprising shikonin derivatives from lithospermum erythrorhizon for treating or preventing diabetes mellitus and the use thereof
  • Pharmaceutical composition comprising shikonin derivatives from lithospermum erythrorhizon for treating or preventing diabetes mellitus and the use thereof
  • Pharmaceutical composition comprising shikonin derivatives from lithospermum erythrorhizon for treating or preventing diabetes mellitus and the use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0070] Example 1: Preparation of comfrey extract

[0071]1 kg of comfrey purchased from Kyung-dong market in Seoul was washed, cut into 1 cm size, dried in a freeze dryer, and kept at -20°C in a refrigerator. Take 100g of dry samples and carry out ultrasonic extraction with 1000g of 85% alcohol for 1h to obtain 350g of comfrey extract ( figure 1 ).

Embodiment 2

[0072] Example 2: Purification and isolation of shikonin compounds

[0073] For the 350g comfrey extract obtained in Example 1, the organic solvent was dried under reduced pressure, and the residue was suspended in water, and separated into an aqueous layer using chloroform:ethanol (2:1) solution and pure water and the chloroform-ethanol fraction, of which the chloroform-ethanol (2:1) fraction was subjected to HPLC analysis. HPLC analysis conditions included passing 60% acetonitrile and 40% distilled water through the column during 0-15 minutes, and then gradually increasing the amount of acetonitrile to 100% during 15-30 minutes. During 30-40 minutes, the acetonitrile ratio was kept at 100%, but was reduced back to 60% after the 40 minute mark.

[0074] Using semi-preparative HPLC under the above analysis conditions, the components were separated to obtain compounds represented by the following Chemical Formulas 1 to 4 ( figure 2 ).

[0075] 2-1. Isobutyrylshikonin (Nac...

reference example 1

[0099] Reference Example 1: Culture of HIT-T15 cells

[0100] HIT-T15 cells used in the following test examples were incubated in 5% CO 2 In an incubator at 37°C, cultured in RPMI1640 medium containing 10% (v / v) horse serum, 2.5% fetal bovine serum (v / v) and 1% penicillin-streptomycin white.

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Abstract

The present invention relates to a composition comprising shikonin compounds, especially, isobutyryl shikonin, ss,ss-dimethylacryl shikonin, isovaleryl shikonin, and a-methyl-n-butyryl shikonin as anactive ingredient for the prevention and treatment of diabetes mellitus and the use thereof. The composition of the present invention showed stimulating effect on the release of insulin in the beta cell of the pancreas due to inhibitory effect on K ATP ion channel of beta cell in pancreas together with promoting effect on the increase of calcium concentration. Therefore, it can be used as the therapeutics, health functional food or food additive for treating and preventing diabetes mellitus.

Description

technical field [0001] The present invention relates to pharmaceutical compositions comprising shikonin compounds for preventing or treating diabetes and uses thereof. Background technique [0002] Diabetes can be divided into two categories. One is insulin-dependent diabetes mellitus (type I), which accounts for about 10% of diabetic patients. Because it occurs in young adults aged 20 or younger, it is considered inherited and is called neonatal diabetes. This type of diabetes often leads to weight loss and the potential for ketoacidosis. This type of diabetes can be treated by administering insulin. This type often presents in an acute form, and symptoms are more severe in children than in adults. [0003] The other is non-insulin-dependent diabetes (type II), which occurs mainly in people aged 40 years or older. Due to lack of exercise, obesity, overeating, mental stress, etc., peripheral organs such as muscle or adipose tissue are less sensitive to insulin, resultin...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/122A61P3/10
CPCA61K31/122A61P3/10
Inventor 朴智浩金善砺姜东昊黄银珠姜撤勋
Owner 珍岛郡
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