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Novel triterpenes and uses thereof

A technology of triterpene compounds and compounds, applied in steroids, medical preparations containing active ingredients, organic chemistry, etc.

Active Publication Date: 2017-04-12
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 triterpenes and uses thereof
  • Novel triterpenes and uses thereof
  • Novel triterpenes and uses 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 5.0 grams of dry weight of the abo...

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 overnight in the incubator and after the cells were attached, the cells were pretreated with 50 μM cisplatin (Cisplatin) for 4 hours. Then add formula (I) compound (50 μ g / mL or 100 μ g / mL) or the YKII-10 pharmaceutical composition (25-100 μ g / mL) of embodiment 1 respectively to treat cells, directly add 50 nM in culture medium after 24 hours DiOC6 dye was used for mitochondrial me...

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 (kidney inflammation) in mice, and then the compound of formula (I) or YKII-10 composition of the present invention was administered to evaluate its therapeutic effect on kidney inflammation. effect.

[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 formul...

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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 (AKI), also known as 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 As a result, individuals experience symptoms such as fatigue, decreased appetite, headache, nausea or vomiting, 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 clinically, so supportive treatment (...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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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