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A polyvanadate alkoxy derivative with insulin-sensitizing activity and its preparation method and application

An insulin-sensitizing and polyvanadate alkane technology is applied in the field of veterinary medicine, which can solve the problems of long-term toxicity and low oral bioavailability, and achieve the effects of regulating blood sugar level, easy control of product process quality, and beneficial to industrial production.

Active Publication Date: 2022-01-18
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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  • A polyvanadate alkoxy derivative with insulin-sensitizing activity and its preparation method and application
  • A polyvanadate alkoxy derivative with insulin-sensitizing activity and its preparation method and application
  • A polyvanadate alkoxy derivative with insulin-sensitizing activity and its preparation method and application

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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-sensitizing activity, a preparation method and application thereof. The method prepares polyvanadate alkoxy derivatives through one-step esterification reaction of acid anhydride or fatty acid or benzoic acid with vanadic acid or vanadate. The polyvanadate alkoxy derivatives of the present invention can rapidly reduce blood sugar in diabetic mice, and the combined use of polyvanadate alkoxy derivatives and insulin can better control blood sugar than using insulin alone, and realize the promotion of glucose responsiveness of insulin And long-lasting activity, which can reduce the number of insulin dosing, and reduce the experience of animals suffering from hyperglycemic and hypoglycemic states at the same time, thereby further improving the fidelity of glycemic control for insulin therapy.

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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Patent Type & Authority Patents(China)
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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