Pyranopyridone alkaloids, methods for preparing the same and use thereof in the preparation of anti-tumor drugs

By isolating and purifying novel pyranopyranopyridone alkaloid compounds 1-3 from the fermentation culture of Penicillium sp. SCSIO 41320, the problem of insufficient targeted therapy in the treatment of small cell lung cancer has been solved, and significant anti-tumor activity has been achieved, which promotes the development of marine microbial drug resources.

CN121135735BActive Publication Date: 2026-06-09SOUTH CHINA SEA INST OF OCEANOLOGY CHINESE ACAD OF SCI
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Patent Information

Application Number
CN202511391411.2
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2025-09-26
Publication Date
2026-06-09
Estimated Expiration
2045-09-26

AI Technical Summary

Technical Problem

Existing targeted therapies are not effective enough in the treatment of small cell lung cancer (SCLC), there is a lack of significant new anti-tumor drugs, and the pharmacological potential of pyranopyridone alkaloids has not been fully utilized.

Method used

Novel pyranopyridone alkaloid derivative compounds 1, 2, and 3 were isolated and prepared from the fermentation culture of Penicillium sp. SCSIO 41320. They were purified by multi-step column chromatography and high-performance liquid chromatography with gradient elution to obtain compounds with significant antitumor activity, which can be used to prepare drugs against small cell lung cancer.

Benefits of technology

Compounds 1-3 exhibit significant inhibitory activity against small cell lung cancer cell lines H446, H1048, H69AR, and H82, with low IC50 values, demonstrating good antitumor activity and possessing the potential to serve as lead compounds for the development of antitumor drugs, thus promoting the development of marine microbial drug resources.

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Abstract

The application discloses pyrano pyridone alkaloids, a preparation method thereof and application thereof in preparation of antitumor drugs. Three pyrano pyridone compounds 1-3 with antitumor activity are prepared from Penicillium sp. SCSIO 41320, and the structural formulae are as shown in formula (I). Experiments prove that the compounds 1-3 have good antitumor activity and can be used for development of antitumor drugs. The application provides alternative compounds for development of new antitumor drugs, and has important significance for development of marine microbial drug resources in China.
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