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Novel triterpene compound and application thereof

A kind of technology of triterpenoid compound and composition, applied in the field of novel triterpenoid compound

Active Publication Date: 2016-01-27
TRINEO BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is currently no clear and specific drug to treat AKI clinically, so supportive treatment (such as dialysis) is often used, with the main purpose of alleviating symptoms

Method used

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  • Novel triterpene compound and application thereof
  • Novel triterpene compound and application thereof
  • Novel triterpene compound and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0068] Embodiment 1 Compound of the present invention and pharmaceutical composition

[0069] 1.1 Separation and purification of formula (I) compound

[0070]

[0071] After the Chizhi fruiting body with a dry weight of 50g is crushed with a pulverizer, the Chizhi powder is placed in a vibrating extraction device, and ethanol is added at a ratio of dry weight of Chizhi fruiting body powder: alcohol volume = 1:24, and then 37 After soaking for one day at ℃, concentrate. The aforementioned extraction steps were repeated several times, and the resulting extracts were filtered, combined, concentrated under reduced pressure and dried to obtain 5 grams of alcohol-soluble crude extract of Chizhi fruiting bodies with a yield of about 10%. The alcohol-soluble crude extract of the red lucidum fruit body obtained above was suction-filtered overnight in a vacuum drying system at a constant temperature of 40°C to remove residual solvent.

[0072] Add the ethyl acetate (ethylacetate) c...

Embodiment 2

[0086] Embodiment 2 formula (I) compound and YKII-10 pharmaceutical composition can effectively alleviate or improve the renal inflammation induced by cisplatin

[0087] In this example, cisplatin (cisplatin) was used to induce apoptosis of renal cells in vitro or in vivo, and then the compound of formula (I) or YKII-10 composition of the present invention was administered to evaluate its therapeutic effect on renal diseases. effect.

[0088] 2.1 Renal cell apoptosis induced by cisplatin

[0089] Take 1×10 5 MDCK canine kidney cells were inoculated in a flat-bottomed 6-well culture dish, cultured in the incubator overnight, and after the cells were attached, the cells were pretreated with 50 μM cisplatin (Cisplatin) for 4 hours, and then the cells were treated with 50 μM cisplatin (Cisplatin) for 4 hours. Add the compound of formula (I) (50 μg / mL or 100 μg / mL) or the YKII-10 pharmaceutical composition (25-100 μg / mL) of embodiment 1 respectively to treat the cells, and direct...

Embodiment 3

[0094] The compound of formula (I) in embodiment 3 and the YKII-10 pharmaceutical composition of embodiment 1 can effectively alleviate or improve the nephritis induced by lipopolysaccharide in vivo

[0095] In this example, lipopolysaccharide (lipopolysaccharide, LPS) was used to induce kidney inflammation (kidneyinflammation) in mice, and then the compound of formula (I) or YKII-10 composition of the present invention was administered to evaluate its efficacy in treating kidney inflammation .

[0096] In this experiment, 6-week-old BLb / c mice were used. The day before the experiment, the animals were divided into groups according to body weight, and after grouping, it was confirmed that there was no statistically significant difference in body weight among the groups. After the experiment started, LPS (2.5 mg / Kg) was injected intraperitoneally into the mice every day for 5 consecutive days to induce inflammation in the mouse kidneys. Simultaneously, give the formula (I) com...

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Abstract

The invention discloses a novel triterpene compound and application thereof to treat or prevent kidney diseases. The disclosed novel triterpene compound is capable of reducing biochemical indexes (such as content of urea nitrogen (BUN) or creatinine (CRE) in serum) related to kidney inflammation and improving glomerulus filtration rate (GFR), therefore the novel triterpene compound can be used to manufacture medicines capable of treating or preventing kidney diseases.

Description

technical field [0001] The present disclosure relates to a novel triterpene compound and its use for the preparation of a medicament for treating kidney diseases such as acute kidney injury and chronic kidney disease. Background technique [0002] Acute kidney injury (acute kidney injury, AKI), also known as acute kidney failure (acute kidney failure), is caused by the rapid destruction of the kidney's filtering function, resulting in the rapid accumulation of metabolites of nitrogenous substances in the body (such as urea or creatinine acid) in the blood. Cause symptoms such as fatigue, loss of appetite, headache, nausea or vomiting in individuals, accompanied by decreased urine output. AKI is prevalent in hospitalized patients, especially those who are seriously ill. There are many causes of AKI, such as reperfusion after tissue ischemia, severe injury, kidney disease or kidney transplantation. However, there is currently no clear and specific drug to treat AKI clinicall...

Claims

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Application Information

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IPC IPC(8): C07J9/00A61K31/575A61P13/12
Inventor 黄政博陈登海陈光地苏钧陶
Owner TRINEO BIOTECH
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