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Polyvanadate alkoxy derivative with insulin sensitization activity as well as preparation method and application of polyvanadate alkoxy derivative

A technology of polyvanadate and insulin sensitization, which is applied in the field of animal medicine and can solve the problems of long-term toxicity and low oral bioavailability

Active Publication Date: 2021-04-27
SOUTH CHINA UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

BMOV and BEOV are currently the only VCs that have entered clinical trials but were blocked in phase II clinical trials due to extremely low oral bioavailability (average 1%) and potential long-term toxicity

Method used

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  • Polyvanadate alkoxy derivative with insulin sensitization activity as well as preparation method and application of polyvanadate alkoxy derivative
  • Polyvanadate alkoxy derivative with insulin sensitization activity as well as preparation method and application of polyvanadate alkoxy derivative
  • Polyvanadate alkoxy derivative with insulin sensitization activity as well as preparation method and application of polyvanadate alkoxy derivative

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] Synthesis of POV derivatives. 1mmol hexavanadate ((Bu 4 N) 2 [V 6 o 13 {(OCH 2 ) 3 CCH 2 OH} 2 ]) and 2mmol acetic anhydride were mixed evenly, and then 0.1g of DMAP, 2mmol triethylamine and 20mLCH were added 3 CN, the reaction was stirred at 80°C for 48h. After cooling to room temperature, the product mixture obtained by the reaction was poured into 50 mL of deionized water, and the red precipitate was collected by filtration. Exchanged by cation exchange resin to H + For cationic polyvanadate alkoxy derivatives, H[V 6 o 13 {(OCH 2 ) 3 CCH 2 OCOCH 3} 2 ].

Embodiment 2

[0057] Synthesis of POV derivatives. 1mmol hexavanadate ((Bu 4 N) 2 [V 6 o 13 {(OCH 2 ) 3 CCH 2 OH} 2 ]), and 2mmol acetic anhydride are mixed evenly, then add 0.1g DMAP, 2mmol triethylamine and 20mLCH 3 CN, the reaction was stirred at 80°C for 48h. After cooling to room temperature, the product mixture obtained by the reaction was poured into 50 mL of deionized water, and the red precipitate was collected by filtration. Exchanged by cation exchange resin to H + The polyvanadate alkoxy derivatives that are cationic, and then exchanged with Al by ion exchange 3+ As a cationic polyvanadate alkoxy derivative, Al 2 [V 6 o 13 {(OCH 2 ) 3 CCH 2 OCOCH 3} 2 ] 3 , denoted as V6-C2.

Embodiment 3

[0059] Synthesis of POV derivatives. 1mmol hexavanadate ((Bu 4 N) 2 [V 6 o 13 {(OCH 2 ) 3 CCH 2 OH} 2 ]), and 2mmol decanoic anhydride were mixed evenly, then added 0.25g of DMAP, 2mmol triethylamine and 20mLCH 3 CN, the reaction was stirred at 80°C for 48h. After cooling to room temperature, the product mixture obtained by the reaction was poured into 50 mL of deionized water, and the red precipitate was collected by filtration. exchanged with Na by cation exchange resin + As a cationic polyvanadate alkoxy derivative, Na[V 6 o 13 {(OCH 2 ) 3 CCH 2 OCO(CH 2 ) 8 CH 3} 2 ], recorded as V6-C10.

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PUM

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Abstract

The invention discloses a polyvanadate alkoxy derivative with insulin sensitization activity as well as a preparation method and application of the polyvanadate alkoxy derivative. According to the method, anhydride or fatty acid or benzoic acid and vanadate or vanadate are subjected to a one-step esterification reaction to prepare the polyvanadate alkoxy derivative. The polyvanadate alkoxy derivative can rapidly reduce the blood sugar of diabetic mice, the combined use of the polyvanadate alkoxy derivative and insulin can better control the blood sugar than the single use of insulin, and the promotion of the glucose responsiveness and the lasting activity of the insulin is realized, so that the administration frequency of the insulin can be reduced, and the experience that animals suffer from hyperglycemia and hypoglycemia at the same time is reduced, so that the fidelity of blood glucose control for insulin treatment is further improved.

Description

technical field [0001] The invention belongs to the field of veterinary medicine, and in particular relates to a polyvanadate alkoxy derivative with insulin-sensitizing activity and a preparation method and application thereof. Background technique [0002] In recent years, the number of dogs and cats suffering from diabetes in pet hospitals has gradually increased. Diabetes in dogs and cats is an endocrine disease, clinically characterized by hyperglycemia, diabetes, polyuria, polydipsia, and gluttony, and in the final stage, it can cause cataracts, blindness, hair loss, heart failure and other cardiovascular diseases in pets. Insulin resistance plays a crucial role in the pathophysiology of canine and feline diabetes and vascular disease. To control blood sugar, exogenous insulin is used clinically in diabetic dogs and cats. However, it is difficult for diabetic dogs and cats to strictly abide by the insulin regimen, and severe complications will cause diabetic dogs and ...

Claims

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Application Information

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IPC IPC(8): C07C69/28C07C67/08A61P5/50
CPCC07C69/28A61P5/50
Inventor 陈坤殷盼超刘媛
Owner SOUTH CHINA UNIV OF TECH
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