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Use of compounds isolated from morus bark

A technology of mulberry white peel and separation, which is applied in the directions of active ingredients of hydroxy compounds, active ingredients of heterocyclic compounds, and medical preparations containing active ingredients, etc., and can solve problems such as unknown effects.

Inactive Publication Date: 2013-12-25
DONG WHA PHARM CO LTD
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0033] Morusignin L (morusignin L) is shown in the following chemical formula 7, and its structure was determined in 1993 (Yoshio H., et.al., 1993, Heterocycles36 (6) 1359–1366), but its effect is unknown

Method used

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  • Use of compounds isolated from morus bark
  • Use of compounds isolated from morus bark
  • Use of compounds isolated from morus bark

Examples

Experimental program
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Effect test

Embodiment 1

[0065] Preparation and analysis of Moran furan G in Cortex Morus alba

[0066] 1-1: Morus alba methanol extract

[0067] Dried Morus alba (3kg) was extracted with 10L of methanol and refluxed repeatedly for 3 times, each time for 4 hours, filtered and then concentrated under reduced pressure to obtain 150g of methanol extract.

[0068] 1-2: Preparation of organic solvent isolate from Cortex Morus alba extract

[0069] Dissolve and disperse the Morus Alba methanol extract (150 g) prepared in 1-1 in 6 liters of water, and extract with n-hexane (3 liters 3 times) and ethyl acetate (3 liters 3 times) successively to obtain n-hexane extraction Extract (50g) and ethyl acetate extract (50g). The ethyl acetate extract was subjected to silica gel column chromatography (silica gel column 500g), and dichloroethane (CH 2 Cl 2 )-methanol (70%:30%, 50%:50%, 30%:70%, 10%:90%, 0:100%) solvent system gradient elution, and 25 isolates (MAE-01~25 ).

[0070] 1-3: Preparation of active iso...

Embodiment 2

[0077] Preparation and analysis of Morus furan K in Cortex Morus alba

[0078] The ethyl acetate part MA.E-14 prepared in 1-2 in Example 1 was subjected to reversed-phase silica gel (RP-18) column chromatography (methanol:water=1:1→3:1 methanol, gradient washing Off), to obtain 20 isolates (MA.E-1401 ~ 1420). The obtained isolate MA.E-1417~1418 was subjected to reversed-phase silica gel chromatography (RP-18, methanol:water=1:1 (2000ml→2:1 (1000ml), separated and refined into 2 parts, and the chemical formula Moranfuran K (20㎎) in 2.

[0079] Moranfuran K: Pale yellow crystalline powder.

[0080] 1H-NMR (400MHz, DMSO-d6): 1.24 (3H, s, H-24″), 1.29 (3H, s, H-25″), 1.74 (3H, s, H-1″), 1.92 (1H , dd, J=11.4, 16.2Hz, H-6″), 2.68 (1H, brs, H-6″), 2.77 (1H, m, H-5″), 3.18 (1H, brs, H-3″ ), 3.23 (1H, dd, J=11.5Hz, H-4″), 5.67 (1H, d, J=9.9Hz, H-22″), 6.23 (1H, brs, H-17″), 6.24 ( 1H, d, J=8Hz, H-13″), 6.31 (1H, brd, J=4.4Hz, H-2″), 6.41 (1H, dd, J=2.4, 8.4Hz, H-19″), 6.57 (1H,...

Embodiment 3

[0083] Preparation and Analysis of Morus alba G in Cortex Morus alba

[0084] The ethyl acetate part MA.E-17 prepared in 1-2 in Example 1 was subjected to reversed-phase silica gel (RP-18) column chromatography (methanol:water=1:1→2:1 methanol, gradient washing Off), to obtain 12 isolates (MA.E-1701 ~ 1712). The thus obtained isolate MA.E-1710 was subjected to preparative high performance liquid chromatography (HPLC, C18, 5μm, 19×150㎜i.d., 60% acetonitrile, 285nm, 5ml / min), after separation and purification, the phin flavonoid G (30㎎) in the chemical formula 3 was obtained.

[0085] Phin flavonoid G: Amorphous red powder.

[0086]1H-NMR (500MHz, acetone-d6): 7.34 (1H, H-14″), 7.27 (1H, H-6′), 6.76 (1H, H-20″), 6.65 (1H, H-3′) , 6.55 (1H, H-5′), 6.18 (1H, H-17″), 6.06 (1H, H-19″), 6.00 (1H, H-6), 5.96 (1H, H-11″), 5.93 (1H, H-13″), 5.20 (1H, H-2″), 5.16 (1H, H-12), 4.62 (1H, H-6″), 4.42 (1H, H-1″), 3.70 (1H, H-7″), 3.15 (1H, H-11), 3.14 (1H, H-11), 1.59 (3H, H-14), 1.51 ...

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Abstract

The present invention relates to advanced glycation end product (AGE) inhibitors or health functional foods for inhibiting an occurrence of diabetic complications, comprising a compound isolated from Morus Bark as active ingredients. Particularly, the present invention comprises a compound selected from the group consisting of mulberrofuran G, mulberrofuran K, kuwanon G, kuwanon Z, oxyresveratrol, 2',4',5,7-tetrahydroxyflavanone, morusignin L and dihydromorin isolated from Morus Bark. The compounds disclosed above inhibit the production of AGE which is a causative substance of diabetic complications. Thus, the compounds could be used as an AGE inhibitor and a health functional food for inhibiting diabetic nephropathy, diabetic retinopathy and diabetic neuropathy.

Description

technical field [0001] The invention relates to a final saccharification product formation inhibitor or health functional food containing a compound isolated from Cortex Morus alba as an active ingredient and capable of inhibiting the onset of diabetic complications. Background technique [0002] As one of the representative adult diseases worldwide, diabetes is caused by abnormal secretion of insulin and is characterized by a state of persistent hyperglycemia. Recently, in South Korea, the incidence of diabetes has been increasing rapidly due to the Westernization of dietary activities and the increase in the elderly population. [0003] Complications caused by diabetes can be roughly divided into acute diseases and chronic diseases. Acute diseases include diabetic ketoacidosis (diabetic ketoacidosis), diabetic hyperosmolar syndrome (hyperglycemic hyperosmolar syndrome), etc. Chronic diseases include diabetic nephropathy, diabetic retinopathy, diabetic neuropathy, which b...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/353
CPCA61K31/05A61K31/353A23L33/10A61P13/12A61P25/00A61P27/02A61P5/48A61P3/10A61K36/605A61K31/36A61K31/352
Inventor 张桓凤尹周炳李贤镛崔贤植李荧馥
Owner DONG WHA PHARM CO LTD
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