Buddleja glycoside with URAT1 inhibitory activity and its preparation method and application

Through supercritical carbon dioxide extraction and C18 reverse phase silica gel column purification technology, high-purity monomerin was extracted from blackberry leaves, solving the problems of low extraction efficiency and major side effects in the prior art, and providing a safe and effective URAT1 inhibitor.

CN116903688BActive Publication Date: 2025-08-15QINGDAO HAIJI RUNSHENG BIOTECHNOLOGY CO LTD
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Patent Information

Application Number
CN202310141077.X
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2023-02-21
Publication Date
2025-08-15
Estimated Expiration
2043-02-21

AI Technical Summary

Technical Problem

In the prior art, the extraction method of Mimondrin has problems such as large organic solvent consumption, long extraction time, low extraction rate and large side effects. The existing URAT1 inhibitors such as benzylbromalone have hepatotoxicity and limitations in use.

Method used

Supercritical carbon dioxide extraction technology combined with C18 reverse phase silica gel column purification was used to extract and purify monsoside from blackberry leaves. By controlling the extraction temperature, pressure, time and entrainer concentration, the extraction efficiency and purity were improved.

Benefits of technology

It has achieved efficient preparation of high-purity monomerin, which has strong urate transporter 1 inhibitory activity, is cheap, safe and environmentally friendly, and provides new resources for urate transporter 1 inhibitors and reduces side effects.

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Abstract

The present invention discloses a budding glycoside having URAT1 inhibitory activity, and its preparation method and application. The preparation method comprises the following steps: washing and drying blackberry leaves, crushing and sieving to obtain blackberry leaf powder; subjecting the blackberry leaf powder to supercritical extraction and collecting the extract; concentrating the extract under reduced pressure to obtain a concentrate; purifying and eluting the concentrate and collecting the eluate; concentrating the eluate under reduced pressure and drying to obtain budding glycoside. The yield of budding glycoside is 0.84%, the HPLC purity is as high as 99.9%, and the preparation method is safe, environmentally friendly and low-cost. The present invention has also been experimentally verified to have budding glycoside with urate transporter 1 inhibitory activity, providing a new resource for the development of urate transporter 1 inhibitors, and also providing a new use for the high-value utilization of blackberry leaves.
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