Application of a proximate and 2-position simultaneously substituted derivative of hypocrellin in the preparation of a photodynamic anti-tumor drug

By developing simultaneous substitution of erythromycin and 2-position, the problems of complex components and limited therapeutic effects in tumor treatment have been solved, and efficient killing and fluorescence-guided surgical positioning of multiple tumors are achieved, especially significant therapeutic effects on high-risk tumors such as brain glioma.

CN116135229BActive Publication Date: 2025-07-25TECHNICAL INST OF PHYSICS & CHEMISTRY - CHINESE ACAD OF SCI
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Patent Information

Application Number
CN202111372447.8
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2021-11-18
Publication Date
2025-07-25
Estimated Expiration
2041-11-18

AI Technical Summary

Technical Problem

Among the existing photodynamic therapies, photosensitizers such as porphyrin compounds used in tumor treatment have difficulty in isolating geometric isomers, which leads to complex drug components, difficulty in drug metabolism and toxicological analysis, and limited therapeutic effects, especially in poor treatment for high-risk malignant tumors such as brain glioma.

Method used

Derivatives of simultaneous substitution of erythromycin and 2-position are developed, and through specific structural modification, they have strong light absorption capacity in the phototherapy window, can efficiently produce reactive oxygen species, specifically enriched in tumor cells, and guide surgical resection through fluorescence positioning, and are used in photodynamic anti-tumor drugs.

Benefits of technology

This derivative shows efficient killing effects in a variety of tumor cells, especially for gastrointestinal tract, head, neck, face, skin, and genital urinary system tumors, and can prolong the postoperative survival of high-risk tumors such as brain glioma, providing fluorescence-guided surgical positioning guidance.

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Abstract

The present invention discloses the application of a derivative with simultaneous substitution at the meso-position and 2-position of hypocrellin as a photodynamic drug in the photodynamic therapy of various tumors. The maximum absorption wavelength of such derivatives is around 630 nm, and the molar extinction coefficient can reach 20,000 - 40,000 M-1 cm-1, showing strong light absorption ability in the phototherapy window; under photosensitizing conditions, it can efficiently generate reactive oxygen species such as singlet oxygen. Such derivatives can efficiently kill a variety of tumor cells, such as esophageal cancer, gastric cancer, lung cancer, liver cancer, cholangiocarcinoma, and colon cancer cells related to digestive tract tumors; brain cancer, head and neck cancer, tongue cancer, nasal cancer, oral cancer, and glioblastoma cells related to head and neck tumors; basal cell carcinoma, squamous cell carcinoma, cutaneous T-cell lymphoma, and melanoma cells related to skin tumors; prostate cancer and bladder cancer cells related to genitourinary tumors. At the same time, such derivatives have good enrichment effects in various tumor cells, can specifically accumulate in tumor cells or tissues, and can locate the position of tumor tissues through the self-fluorescence of the photosensitizer, for fluorescence-guided surgical resection of tumors. Under the same conditions, the derivatives in the present invention have higher photodynamic effects in treating tumors than commercial porphyrin-based photosensitizing drugs.
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