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Application of two phenylethanoid glycoside compounds to preparation of antidiabetic drugs

An anti-diabetic and compound technology, applied in the field of medical applications, can solve problems such as unclear specific mechanisms

Inactive Publication Date: 2020-10-23
内蒙古自治区中医医院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] At present, the activity research of the aforementioned two compounds is mainly focused on anti-inflammation, anti-cancer, anti-aging and other aspects. It is not clear whether they can protect and repair the damage of pancreatic islet β cells, and the specific mechanism of their specific effects; that is, Can these two compounds be developed into drugs for protecting and repairing pancreatic β-cell damage, promoting insulin secretion of damaged pancreatic β-cells, reducing free radical damage caused by alloxan to pancreatic β-cells, enhancing islet cell activity, and improving cell Survival drugs are still a blank in this field

Method used

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  • Application of two phenylethanoid glycoside compounds to preparation of antidiabetic drugs
  • Application of two phenylethanoid glycoside compounds to preparation of antidiabetic drugs
  • Application of two phenylethanoid glycoside compounds to preparation of antidiabetic drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Embodiment 1: The preparation method of compound verbascoside and isoverbacoside

[0026] 1.1 Plant source

[0027] In this experiment, both verbascoside and isobracoside were extracted from Cymbaria daurica L., a plant of the genus Cymbaria L. in the family Scrophulariaceae. Daurica daurica was obtained in June 2018 In the last ten days, it was collected from Maxi Lahada, Hesi Geula Farm, East Ujimqin Banner, Xilin Gol League, Inner Mongolia Autonomous Region. It was identified as Cymbaria daurica L. by Professor Zhang Chunhong from the Department of Pharmacognosy, Baotou Medical College. .

[0028] 1.2 Extraction and separation

[0029] 1) Weigh 1450g of the dried Dawuli Sinba whole herb, and grind it into medium-fine powder (through a No. 4 sieve). Using heating and reflux method, extract with 70% ethanol for 1 h (material ratio 1:10). After standing to cool, filter the extract. Repeat the extraction 3 times according to the above method. The extracts were comb...

Embodiment 2

[0034] Example 2: Protective and repairing effects of compounds verbascoside and isoverbacoside on alloxan-induced damage to NIT-1 islet β cells

[0035] 2.1 Experimental cells

[0036] NIT-1 cells: Mouse NIT-1 insulinoma β cell line was purchased from Tongpai (Shanghai) Biotechnology Co., Ltd.

[0037] 2.2 Instruments and reagents

[0038] 1640 medium, fetal bovine serum, penicillin-streptomycin, phosphate buffered saline (PBS), 0.25% trypsin (Gibco, USA); DMSO (Hyclone Biochemical (Beijing) Co., Ltd.); rosiglitazone (US sigma company); MTT powder, alloxan. Thermo Scientific Multiskan FC microplate reader (Thermo Company); HHS21-8 electric constant temperature water bath (Beijing Changan Scientific Instrument Factory); 1 / 100,000 electronic balance (Shanghai Precision Scientific Instrument Co., Ltd.).

[0039] 2.3 Experimental method

[0040] 1) NIT-1 islet β cell culture

[0041] Place NIT-1 islet β cells in RPMI1640 medium containing 10% fetal bovine serum, 100U / mL peni...

Embodiment 3

[0050] Example 3: Research on the Mechanism of Anti-diabetic Activity of Actascoside and Isovacoside

[0051] 3.1 Effects of verbascoside and isoverbacoside on alloxan-induced insulin secretion in NIT-1 cells

[0052] Take NIT-1 cells in logarithmic growth phase, press 1×10 5 cells / mL were inoculated in 6-well cell culture plates, and after the cells adhered to the wall, the experimental grouping and treatment were as follows: ① normal control group: without any treatment, normal culture for 24 hours; ② alloxan model group (ALX): 12mmol / L ALX damaged cells for 24 hours; ③ Positive control group: add 10 μmol / L rosiglitazone for pretreatment for 4 hours, then add 12 mmol / L ALX to damage cells for 24 hours; ④ drug treatment group: add serial concentrations (6.25 μmol / L, 25 μmol / L L, 100 μmol / L) verbascoside and isoverbacoside were pretreated for 4 hours, and then 12 mmol / L ALX was added to injure the cells for 24 hours. After culturing for 24 hours, the supernatant was collect...

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Abstract

The invention discloses an application of two phenylethanoid glycoside compounds, namely verbascoside and isoacteoside to preparation of antidiabetic drugs. Monomeric compounds of verbascoside and isoacteoside can be extracted from various plants, so that the source is wide, the toxicity is low, and the stability is good. An inventor proves by experiments that (1) the verbascoside and the isoacteoside can protect and repair an injury of an NIT-1 pancreatic beta-cell caused by alloxan, and promote insulin secretion of the injured pancreatic beta-cell in a dose-dependent manner; (2) a free radical injury of the pancreatic beta-cell caused by the alloxan can be reduced; and (3) the activity of the pancreatic cell can be enhanced, the survival rate of the cell is improved, and the mechanisms of the verbascoside and the isoacteoside can activate transcription of an apoptosis-inhibiting gene Bcl-2 mRNA and inhibit transcription of an apoptosis-promoting gene Bax mRNA and finally inhibit transcription of a Caspase-3 gene and expression of Caspase-3 and Bax proteins, thereby inhibiting apoptosis of the pancreatic cell injured by the alloxan. Therefore, the two phenylethanoid glycoside compounds, namely the verbascoside and the isoacteoside disclosed by the invention have potential value of being developed into antidiabetic candidate drugs.

Description

technical field [0001] The invention belongs to the technical field of medical applications, and relates to the application of two phenylethanol glycoside compounds in the preparation of antidiabetic drugs, specifically the application of verbascoside and isoverbacoside in the preparation of antidiabetic drugs. Background technique [0002] Diabetes mellitus is a common clinical metabolic disease characterized by hyperglycemia caused by defects in insulin secretion or its biological action, which seriously endangers human life and health. Its main symptoms are reduced tolerance to glucose and disturbance of lipid and protein metabolism. Diabetes will produce many complications such as retinopathy and optic nerve system lesions, and it will increase the risk of cardiovascular disease and stroke. Once you get sick, you will take medicine for life, which will bring a heavy burden to yourself and your family. In recent years, with the development of urbanization, changes in peo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7034A61P5/50A61P3/10
CPCA61K31/7034A61P5/50A61P3/10
Inventor 李旻辉张春红吕丽娟张明旭李雪石如玉蒋林林臧二欢
Owner 内蒙古自治区中医医院
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