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Protease inhibitor

An inhibitor, cysteine ​​protease technology, applied in the direction of protease inhibitors, transferrin, peptide/protein components, etc., can solve the problem of unknown lactoferrin

Inactive Publication Date: 2005-11-02
MORINAGA MILK IND CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0034] However, lactoferrin, some of its peptides, and transferrin are not known to have cysteine ​​protease inhibitory activity

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0156] The peptide having the amino acid sequence 679-695 of SEQ ID No. 1 in the sequence table was produced according to the following steps (Fig. 3, human lactoferrin peptide Y679-K695).

[0157] The above peptide of the present invention was produced by synthesis using an automated peptide synthesizer (manufactured by Applied Biosystems, Model 433A).

[0158] With N-methylpyrrolidone (product of Applied Biosystems, hereinafter abbreviated as NMP) containing 20% ​​piperidine, the amino protecting group Fmoc- The group was cleaved and the resin was washed with NMP. Then, using the FastMoc (registered trademark) kit (product of Applied Biosystems) to make Fmoc-threonine [precisely, Fmoc-amino acid (product of Applied Biosystems) )] was condensed on the resin, and the resin was washed with NMP. The Fmoc group is then cleaved and Fmoc-alanine corresponding to the second amino acid at the C-terminal is condensed, followed by washing the resin. By further repeating the steps of...

Embodiment 2

[0162] (preparation of tablets formulated with lactoferrin)

[0163] Cystatin tablets containing the following compositions were produced as follows.

[0164] Bovine lactoferrin (product of Morinaga dairy company) 40.0%

[0165] Lactose (Morinaga Dairy Company product) 18.5%

[0166] Corn starch (Nisshin flour milling company product) 30.7%

[0167] Magnesium stearate (product of Taihei Chemical Industry Co., Ltd.) 1.4%

[0168] Carboxymethylcellulose calcium (Gotokn chemical company product) 9.4%

[0169] Add an appropriate amount of sterile purified water to knead the mixture of bovine lactoferrin, lactose, cornstarch and carboxymethylcellulose calcium), and dry the kneaded material at 50° C. for 3 hours. Magnesium stearate was then added to the obtained dry product and mixed uniformly, followed by tableting according to conventional procedures, thereby obtaining tablets.

Embodiment 3

[0171] (preparation of lactoferrin capsules)

[0172] With a 50-mesh sieve (product of Yamato Science Co., Ltd.), 600 g of lactose (product of Wako Pure Chemical Industry Co., Ltd.), 400 g of cornstarch (product of Nissnin Powder Milling Co., Ltd.), 400 g of crystalline cellulose (product of Wako Pure Chemical Industry Co., Ltd.) and 600 g One gram of bovine lactoferrin (product of Morinaga Dairy Company) was sieved, packed into a polyethylene bag with a thickness of 0.5 mm, and mixed up and down repeatedly. Using a fully automated capsule filling machine (manufactured by Cesere Pedini, press-fit type), the obtained powder is filled into capsules (Shionogi Qualicaps company product, No. 1 gelatin capsule, OP yellow No. 6 shell, empty weight 75 mg) with a capacity of 275 mg , thus obtaining 7000 capsules, each containing 82 mg of bovine lactoferrin.

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Abstract

This invention relates to a cysteine protease inhibitor comprising one or more of lactoferrin, a partial peptide of lactoferrin, and transferrin, as an active ingredient. The cysteine protease inhibitor of the present invention can be used for preventive or therapeutic drug for osteoporosis, malignant hypercalcemia etc. and used for food, drink, feed and the like.

Description

technical field [0001] The present invention relates to a cysteine ​​protease inhibitor, which comprises one or more components selected from lactoferrin, a peptide fragment of lactoferrin or transferrin as an active ingredient, which can be used to treat A preventive or therapeutic agent for diseases such as osteoporosis and malignant hypercalcemia, and can be used in food, beverage, feed and the like. Background technique [0002] Proteolytic enzymes having a sulfhydryl group in their active center are generally referred to as cysteine ​​proteases (thiol proteases). Cathepsin L, cathepsin B or cathepsin K, together with calcium-dependent neutral protease (CAMP), papain, ficin and Promelain, is one of the typical cysteine ​​proteases. Substances that are expected to have an inhibitory effect on these cysteine ​​proteases can be used as therapeutic agents for diseases related to cysteine ​​proteases, including the following diseases: muscular dystrophy, dysplasia, myocardia...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A23L33/17A23L33/18A61K38/00A61K38/02A61K38/16A61K38/40A61K38/57A61P1/02A61P3/00A61P3/14A61P9/00A61P9/10A61P13/08A61P15/00A61P19/10A61P21/00A61P21/04A61P25/00A61P25/28A61P27/12A61P31/04A61P31/12A61P31/18A61P31/22A61P35/00A61P35/04A61P37/08A61P43/00C07K14/79C07K14/81C12N9/99
CPCA23V2002/00C07K14/8139A23L1/3053A61K38/00C07K14/79A23L33/18A61P1/02A61P13/08A61P15/00A61P19/10A61P21/00A61P21/04A61P25/00A61P25/28A61P27/12A61P3/00A61P3/14A61P31/04A61P31/12A61P31/18A61P31/22A61P35/00A61P35/04A61P37/08A61P43/00A61P9/00A61P9/10Y02A50/30A23V2200/306A23V2250/54248A61K38/40A61K38/17
Inventor 胜沼信彦
Owner MORINAGA MILK IND CO LTD
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