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Application of mogroside IIE in preparing trypsin inhibitors

A technology of trypsin inhibition and mogroside, which is applied in the field of medicine, can solve problems such as insufficient research, and achieve the effects of less toxic side effects, wide sources, and good bioavailability

Active Publication Date: 2019-04-12
AFFILIATED HOSPITAL OF GUILIN MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It can be seen that the activity of trypsin is crucial to the occurrence and development of pancreatitis, but at present, the research on trypsin inhibitors is not enough

Method used

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  • Application of mogroside IIE in preparing trypsin inhibitors
  • Application of mogroside IIE in preparing trypsin inhibitors
  • Application of mogroside IIE in preparing trypsin inhibitors

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Example 1: Time-effect experiment of mogroside IIE acting on AR42J cells

[0051] Rat pancreatic exocrine cell AR42J cells were purchased from the ATCC cell bank in the United States. AR42J culture conditions are: F12K medium (ATCC) and 20% fetal bovine serum (Gibco), 37°C, 5% carbon dioxide. Cell characteristics: Rat origin, adherent growth, epithelial cells, no mycoplasma, sterile.

[0052] Purchase Mogroside IIE at Chengdu Master Biotechnology Co., Ltd., in powder form, molecular weight 801, molecular formula C 42 h 72 o 14 , purity ≥ 98% (HPLC), soluble in methanol and dimethyl sulfoxide. The structural formula of the mogroside IIE is:

[0053]

[0054] In rat pancreatic exocrine cell AR42J cells, 20 μM mogroside IIE (dissolved in methanol in Examples 1-6) was added. After treatment for 0h, 1h, 3h and 6h, respectively, the activities of trypsin and cathepsin B in AR42J cells were detected.

[0055] Wherein, trypsin activity assay (the following compounds a...

Embodiment 2

[0062] Example 2: Time-effect experiment of mogroside IIE acting on primary pancreatic acinar cells

[0063] In mouse primary pancreatic acini, 20 μM mogroside IIE was added. After being treated for 0h, 1h, 3h and 6h, respectively, the activities of trypsin and cathepsin B in the cells were detected.

[0064] Depend on Figure 4 It can be seen that the trypsin activity decreased by 1.21%, 7.4% and 15.21% after mogroside IIE was treated for 1h, 3h and 6h respectively.

[0065] Depend on Figure 5 It can be seen that the activity of cathepsin B decreased by 10.13%, 13.74% and 18.26% after mogroside IIE was treated for 1h, 3h and 6h respectively.

[0066] It can be seen that mogroside IIE inhibits the activity of trypsin and cathepsin B in primary pancreatic acinar cells in a time-dependent manner.

Embodiment 3

[0067] Example 3: Concentration Effect Experiment of Mogroside IIE on AR42J Cells

[0068] In rat pancreatic exocrine cell AR42J cells, 0 μM, 5 μM, 10 μM and 20 μM mogroside IIE were added, respectively. After being treated for 6 hours, the activities of trypsin and cathepsin B in the cells were detected.

[0069] Depend on Figure 6 It can be seen that after the action of 5 μM, 10 μM and 20 μM mogroside IIE, the trypsin activity decreased by 8.57%, 18.8% and 20.89% respectively.

[0070] Depend on Figure 7 It can be seen that after the action of 5 μM, 10 μM and 20 μM mogroside IIE, the activity of cathepsin B decreased by 12.19%, 21.3% and 26.42%, respectively.

[0071] It can be seen that mogroside IIE inhibits the activity of trypsin and cathepsin B in AR42J cells in a concentration-dependent manner.

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PUM

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Abstract

The invention discloses the application of mogroside IIE in preparing trypsin inhibitors, and belongs to the technical field of medicines. After a long period of extensive trials, the inventor of thepresent application finds that the mogroside IIE can inhibit the activity of trypsin at the acinar cell background, and the inhibition has dependence on time and concentration. In addition, the mogroside IE can inhibit the activation of trypsinogen by an acute pancreatitis inducer-cerulein. At the same time, that the mogroside IE inhibits the activation of the trypsinogen is related to cathepsin B, so that the mogroside IE can be used to prepare trypsin inhibitors.

Description

technical field [0001] The invention relates to the application of mogroside IIE in the preparation of trypsin inhibitors, belonging to the technical field of medicine. Background technique [0002] Luo Han Guo belongs to the perennial herbaceous vines of Cucurbitaceae. Its fruit is edible and used as medicine. It is mainly distributed in Guangxi Zhuang Autonomous Region, Guangdong Province, Jiangxi Province, Hunan Province and Guizhou Province. Ripe Luo Han Guo extract is sweet, up to 300 times sweeter than sucrose, but it is low in calories and has no other obvious side effects, so it is a good substitute for sugar. Mogroside is the main source of sweetness of Luo Han Guo and its extract, and it is also the main active ingredient of mogroside. In addition to the commercial value of sweeteners, Mogroside has a variety of pharmacological activities, including: lowering blood sugar, which does not cause the body's blood sugar to rise after eating; lowering blood lipids, bloo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/704A61K9/08A61P1/18
CPCA61K9/0019A61K9/08A61K31/704A61P1/18
Inventor 金俊飞肖娟黄凯刘丙刚林厚民李爱丽
Owner AFFILIATED HOSPITAL OF GUILIN MEDICAL UNIV
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