Dimerization guaiane sesquiterpene lactone and preparation method and application thereof

By synthesizing dimerized guaiacol sesquiterpene lactone 1-25 and forming a pharmaceutical composition with a pharmaceutical carrier, the problem of lack of effective synthesis and insufficient treatment of liver cancer in the prior art has been solved, and a strong inhibitory effect and high inhibition rate on liver cancer cells have been achieved.

CN120965619APending Publication Date: 2025-11-18KUNMING INST OF BOTANY CHINESE ACAD OF SCI
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Patent Information

Application Number
CN202511267672.3
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2025-09-05
Publication Date
2025-11-18

AI Technical Summary

Technical Problem

Existing technologies lack effective methods for the synthesis of dimerized guaiacol sesquiterpene lactones and their synthesis, and existing liver cancer drugs have shortcomings in terms of therapeutic efficacy, drug resistance, and side effects, failing to meet clinical needs.

Method used

Dimeric guaiacol sesquiterpene lactone 1-25 was synthesized by using agrabin-derived dienes and divinyl ketone via a Diels-Alder reaction and a dedimethylamine process, and then mixed with a pharmaceutically acceptable carrier to form a pharmaceutical composition.

Benefits of technology

A series of novel dimerized guaiacol sesquiterpene lactone compounds were provided, showing strong inhibitory activity against hepatocellular carcinoma cells with IC50 values ​​ranging from 1.1 to 18.7 μM. In particular, compound 17 inhibited tumor growth by up to 84% in a nude mouse xenograft tumor model.

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Abstract

The invention provides dimerized guaiane sesquiterpene lactone 1-25 shown in a structural formula as well as a pharmaceutical composition, a preparation method and application thereof, and belongs to the technical field of medicines. The preparation method disclosed by the invention comprises the following steps: carrying out Diels-Alder reaction / deprotection on guaiane diene and divinyl ketone, so as to obtain the dimerization guaiane sesquiterpene lactone 1 to 25. The dimerized guaiane sesquiterpene lactone has inhibitory activity on human hepatoma cell lines HepG2, Huh7 and SK-Hep-1, and the compound 17 can significantly inhibit growth of transplanted tumors in nude mice, can form a pharmaceutical composition with a pharmaceutically acceptable carrier, and can be used for preparing anti-hepatoma drugs.
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