Photosensitizing Agent with Sugar Chain for Tumor Accumulation
Solution Overview
Problem
Current photodynamic therapy and diagnosis techniques using photosensitizing agents face limitations in tumor selectivity and efficiency, as existing compounds do not effectively accumulate in tumor sites, limiting their therapeutic and diagnostic efficacy.
Innovation Solution
Development of a compound represented by General Formula (I), which incorporates a silicon substituent and a sugar chain, enhancing tumor tropism and accumulation, allowing for improved photodynamic therapy and diagnosis by generating singlet oxygen and emitting fluorescence.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional photosensitizing agents are used, then photodynamic therapy and diagnosis can be performed, but tumor selectivity and accumulation efficiency are insufficient
Solution Approach 1:
The patent combines a porphyrin derivative (photosensitizing agent) with a sugar chain (tumor-targeting moiety) into a single conjugated compound. This merging allows the compound to simultaneously exhibit photosensitizing activity and tumor-selective accumulation, resolving the contradiction between therapeutic function and targeting efficiency
Solution Approach 2:
The invention creates a composite molecular structure consisting of a porphyrin core linked to a sugar chain through a connecting group. This composite structure integrates the optical properties of porphyrin with the biological recognition properties of sugar chains, enabling both effective photodynamic therapy and enhanced tumor accumulation
2Ease of operation
If photosensitizing agents are administered systemically, then treatment can be applied, but accumulation in tumor sites is limited
Solution Approach 1:
The sugar chain component is specifically designed to recognize and bind to receptors on tumor cell surfaces, creating local affinity at the tumor site. This local quality enhancement ensures that while the compound is administered systemically, it selectively accumulates at the target location, increasing local concentration without complicating the administration process
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The compound effectively accumulates in tumor sites, enhancing the efficiency of singlet oxygen generation and fluorescence emission, thereby improving cancer treatment and diagnosis outcomes.
Implementation Method 1
a compound that can generate singlet oxygen (photosensitizing agent) is administered to a patient with cancer or the like and then is irradiated with light of an appropriate wavelength to generate singlet oxygen
Implementation Method 2
many photosensitizing agents also emit fluorescence, and photodynamic diagnosis is also known in which such agents are irradiated with light of an appropriate wavelength and fluorescence emitted therefrom is observed
Data Source
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AI summary
There is provided with a compound represented by Formula (I) or a salt thereof; where A is a linking group represented as -X-NHCO- where X is a C1 to C6 alkylene group, each of R1, R2, R4, R5, R7, R8, R10, and R11 is a hydrogen atom, each of R3, R6, and R9 is a substituent of Formula; R12 is selected from a group of substituents represented by Formulae, R13 is a sulfo group, Ra, Rb, and Rc are substituents independently selected from C1 to C6 alkyl groups, and Rd is a hydrogen atom or a C1 to C6 alkyl group, and Rx is a substituent represented by General Formula. The compound is useful in cancer treatment, as a photosensitizing agent, and as a fluorescent probe. It has improved uptake by cancer cells.