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Application of pentacyclic triterpene compounds to preparation of medicine for treating adiposis

A technology of pentacyclic triterpenes and compounds, which is applied in the field of obesity treatment drugs, can solve problems such as many side effects, achieve strong inhibitory effect, inhibit absorption capacity, and reduce weight gain

Active Publication Date: 2017-01-25
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At the same time, it has been reported in the literature that pelicin is safe to take, has no hemolytic properties, and no related adverse safety events have been seen
[0004] Obesity is one of the fastest growing health problems in the world. It is closely related to a series of diseases such as hyperlipidemia, diabetes, and heart disease. However, most anti-obesity drugs on the market have many side effects

Method used

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  • Application of pentacyclic triterpene compounds to preparation of medicine for treating adiposis
  • Application of pentacyclic triterpene compounds to preparation of medicine for treating adiposis
  • Application of pentacyclic triterpene compounds to preparation of medicine for treating adiposis

Examples

Experimental program
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Effect test

Embodiment 1

[0019] Preparation of tablets: Mix 60g pedicel glucoside and 20g pregelatinized starch evenly, add 50% ethanol as binder, make soft material, pass through a 20 mesh sieve, make granules, and place the obtained wet granules at 75°C Dry in an oven for 2 hours, add appropriate amount of micropowder silica gel and magnesium stearate to the granules, mix evenly, press into tablets and pack separately.

Embodiment 2

[0021] Lipase inhibition rate determination experiment: Take 100 μl of porcine pancreatic lipase (PL) solution (5 mg / mL) and add 20 μL of different concentrations of the sample solution to be tested, use Tris-HCl buffer solution with pH=7.4 to make the volume to 900 μl, mix well, Incubate at 37°C for 5 minutes, then add 100 μL of p-nitrophenylbutyrate (p-NPB) solution (10mol / L), shake well, transfer 200 μL to a 96-well microplate quickly, and use a microplate reader to determine its The absorbance at 410nm is read every 1 minute and measured at least 5 times (1 to 15 minutes). The same operation was repeated 3 times for the determination of each concentration in each group, and the absorbance was averaged. Take time as the abscissa, and take the difference between the absorbance in the experimental group and the absorbance of the corresponding blank group as the ordinate, and calculate the change rate K of the absorbance difference with time, and calculate the inhibition rate ...

Embodiment 3

[0026] Effects of similar compounds with a pentacyclic triterpene as the parent nucleus on obesity induced by high-fat diet: 54 clean-grade Wistar rats, aged 3 to 4 months, weighing 180g-200g, male, purchased from Guangdong Experimental Animal Center. The fat energy content of the basic nutrition feed is 10%, and the fat energy content of the high-fat nutrition feed is 45%. After one week of adaptive feeding with the basic nutritional feed, the mice were randomly divided into 9 groups (n=6), and the grouping situation was as follows:

[0027] Group 1: fed with basic nutrient feed for 12 weeks, as the normal group.

[0028] Group 2: fed with high-fat nutrient feed for 12 weeks, and in the last 4 weeks, the same volume of 0.5% sodium hydroxymethyl cellulose solution was given by intragastric administration every day, as a blank control group.

[0029] Group 3: fed with high-fat nutrient feed for 12 weeks, of which 10mg·kg was given daily for the last 4 weeks -1 Orlistat (orli...

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Abstract

The invention discloses application of pentacyclic triterpene compounds to preparation of medicine for treating adiposis and weight losing functional food. The pentacyclic triterpene compounds comprise pedunculoside and rotundic acid. The compounds have higher inhibition effect on lipase. Compared with synthetic medicine of Orlistat, the pentacyclic triterpene compounds have the advantages that the effect is mild; no irritation effect exists on the gastrointestinal tracts; the medicine is suitable for being taken for a long time.

Description

technical field [0001] The invention relates to a medicine for treating obesity, in particular to a class of pentacyclic triterpene compounds for treating obesity. Background technique [0002] Pedunculoside and Rotundic acid belong to pentacyclic triterpenes as compounds, with similar molecular structures, and the molecular formulas are C 36 h 58 o 10 and C 30 h 48 o 5 , with molecular weights of 650.84 and 488.71, which can be extracted from the traditional Chinese medicine Jiubiying (dried bark of Ilex rotunda Thunb.), with a relatively high content, and can also be obtained from other plants of the holly family. Iron Ilex plant resources are abundant in Lingnan region of China. [0003] Pentacyclic triterpenoids such as pedicel glucoside and basic acid have a wide range of uses. Patent document CN101961340A discloses that pelicin glucoside has the effect of treating arrhythmia, myocardial ischemia, cerebral ischemia and other diseases; , Myocardial infarction and...

Claims

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Application Information

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IPC IPC(8): C07J63/00A61P3/04A23L33/125
CPCC07J63/002A23V2002/00
Inventor 苏薇薇严曾豪苏敏敏王永刚
Owner SUN YAT SEN UNIV
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