Benzophenone dimer compound and application thereof

A compound and application technology, which is applied in the field of benzophenone dimer compounds, can solve problems such as brown adipose tissue abnormalities, achieve good tyrosinase inhibitory activity, treat obesity, and have good market prospects

Active Publication Date: 2022-08-05
SOUTHWEST UNIVERSITY FOR NATIONALITIES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] 4. Abnormal brown adipose tissue

Method used

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  • Benzophenone dimer compound and application thereof
  • Benzophenone dimer compound and application thereof
  • Benzophenone dimer compound and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] The total extract was prepared by extracting the leaves of C. chinensis with pure water. After removing sugar by macroporous resin, the water-soluble chemical constituents of C. chinensis were separated by normal and reversed-phase silica gel chromatography. Combined with one-dimensional and two-dimensional nuclear magnetic resonance spectroscopy picture( 1 H-NMR, 13 C-NMR, HSQC, HMBC), mass spectrometry (MS), ultraviolet absorption spectroscopy (UV), etc. and literature data to identify the three-dimensional structure of the compound. details as follows.

[0053] Extraction and Separation:

[0054] The dried medicinal powder (5kg) was extracted with pure water at 85°C for three times (0.5 hours each time). The extracted water was mixed and concentrated under reduced pressure to obtain the total extract. The total extract was passed through a macroporous resin D-101 column for gradient elution with methanol / water (0:100, 20:80, 40:60, 60:40, 80:20, v / v), and methano...

Embodiment 2

[0063] Example 2 Lipid-lowering activity of Caenorhabditis elegans

[0064] Firstly, C. elegans was treated with compounds 1 and 2 of the present invention, and oil red O and Sudan black B were used to stain and observe the nematodes, and the lipid-lowering activity of the monomer compounds was evaluated by the accumulation of fat in the body.

[0065] Coat 100 μL of the sample solution (final concentration of 100 μg / mL) and 100 μL of activated OP50 on NGM medium, place it in a 30°C incubator for 18 hours, and inoculate the nematodes at the L1 stage by contemporaneous culture. The nematodes were stained with Oil Red O and Sudan Black B after cultured at constant temperature (20°C) on drug-free NGM medium for 72h. Finally, the stained nematodes were washed with phosphate buffer, picked on a glass slide, and placed under a microscope to take pictures to observe the fat particles in the body. Orlistat and DMSO were positive and blank controls, respectively.

[0066] Obesity is ...

Embodiment 3

[0068] Example 3 Tyrosinase inhibitory activity

[0069] Using L-dopa as the substrate, the inhibition of tyrosinase activity was detected by a microplate reader. Compounds 1, 2 were first dissolved in DMSO and then diluted to a range of concentrations with phosphate buffered saline (PBS; pH=6.8). Simultaneously, levodopa and tyrosinase were dissolved in PBS. The concentrations of levodopa and tyrosinase were 0.5 mM and 0.06 mg / mL, respectively. Compound (50 μL), tyrosinase (50 μL) and PBS (50 μL) were mixed in a 96-well plate, reacted at 30° C. for 10 min, and then levodopa was added to the mixture and reacted at 30° C. for 5 min. Then, the absorbance of each solution was measured at 475 nm. The total solution system was 250 μL, and DMSO was used as the blank control. The tyrosinase inhibition rate was calculated as follows: Inhibition rate (%)=1-[(A 2 -A 1 ) / (B 2 -B 1 )]×100%

[0070] A 1 is the absorbance of the blank at 0 min, A 2 is the absorbance of 100 blank ...

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Abstract

The invention provides a benzophenone dimer compound, or a pharmaceutically acceptable salt or an optical isomer of the benzophenone dimer compound. Meanwhile, the invention further provides application of the compound in preparation of products for lowering lipid, whitening and the like.

Description

technical field [0001] The present invention relates to a benzophenone dimer compound and its application field. Background technique [0002] Obesity is a group of common metabolic disorders. When the human body eats more calories than it consumes, the excess calories are stored in the body in the form of fat, and the amount exceeds the normal physiological requirement, and when it reaches a certain value, it evolves into obesity. Normal male adult adipose tissue weight accounts for 15% to 18% of body weight, and female adipose tissue accounts for 20% to 25%. With age, the percentage of body fat increases accordingly. Assessment methods for obesity include anthropometry, dual-energy X-ray absorptiometry, ultrasound, CT, infrared induction, etc. If there is no obvious cause, it is called simple obesity, and if there is a clear cause, it is called secondary obesity. [0003] Obesity is mainly caused by eating too much and too little activity. The calorie intake is more t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D309/10A61P3/04A61P3/06A61K31/351A61K8/49A61Q19/00A61Q17/04
CPCC07D309/10A61P3/04A61P3/06A61K8/498A61Q19/00A61Q17/04
Inventor 李丽梅
Owner SOUTHWEST UNIVERSITY FOR NATIONALITIES
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