Pentaaza Macrocyclic Complex and Ascorbate Cancer Therapy
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Solution Overview
Problem
Current cancer treatments, such as radiation therapy and chemotherapy, lack efficacy in selectively killing cancer cells while sparing normal cells, and there is a need for enhanced methods to improve treatment outcomes for cancer patients.
Innovation Solution
Administration of a pentaaza macrocyclic ring complex, specifically a manganese-based complex, in combination with ascorbic acid or its derivatives, to enhance cancer cell killing by increasing intracellular H2O2 levels and oxidative stress, potentially used alongside conventional cancer therapies.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional cancer treatments (radiation therapy and chemotherapy) are used, then cancer cells are killed, but normal cells are also damaged and treatment efficacy is insufficient
Solution Approach 1:
The patent applies local quality by designing the pentaaza macrocyclic ring complex to selectively accumulate in cancer cells through their unique cellular environment (high NADH levels, lower glutathione levels), rather than affecting all cells uniformly. This selective accumulation allows the complex to exert its oxidative stress effect primarily in cancer cells, improving treatment efficacy while reducing damage to normal cells
Solution Approach 2:
The patent utilizes parameter changes by exploiting differences in cellular redox parameters between cancer and normal cells. Cancer cells have elevated NADH/NAD+ ratios and lower glutathione levels compared to normal cells. The pentaaza macrocyclic ring complex responds to these parameter differences by generating reactive oxygen species preferentially in cancer cells, thereby achieving selective cytotoxicity and resolving the contradiction between effective cancer cell killing and normal cell preservation
2Productivity
If higher doses of conventional chemotherapy are administered to improve cancer cell killing, then treatment efficacy increases, but toxicity to normal cells increases
Solution Approach 1:
The patent introduces an intermediary mechanism - the pentaaza macrocyclic ring complex acts as a mediator that converts endogenous NADH in cancer cells into reactive oxygen species. This intermediary approach allows cancer cell killing without requiring high doses of external cytotoxic agents, thereby achieving high productivity in cancer cell destruction while avoiding the toxicity associated with high-dose conventional chemotherapy
Solution Approach 2:
The patent applies self-service by designing the pentaaza macrocyclic ring complex to utilize the cancer cell's own metabolic products (NADH) as substrates for generating reactive oxygen species. The complex essentially makes the cancer cell kill itself through its own metabolic characteristics, eliminating the need for high external doses and the associated toxicity to normal cells
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 combination of the pentaaza macrocyclic ring complex with ascorbic acid compounds shows synergistic effects in selectively killing cancer cells, potentially improving treatment efficacy and outcomes when used in conjunction with existing cancer therapies.
Implementation Method 1
Transition metal-containing pentaaza macrocyclic ring complexes having the macrocyclic ring system corresponding to Formula A have been shown to be effective in a number of animal and cell models of human disease
Implementation Method 2
administration of a pentaaza macrocyclic ring complex, and an active agent corresponding to an ascorbate compound selected from the group consisting of ascorbic acid, an ascorbic acid derivative
Data Source
AI summary
A method of treating cancer in a subject includes administering an active agent selected from ascorbic acid, an ascorbic acid derivative, and/or a pharmaceutically acceptable salt thereof and administering a pentaaza macrocyclic ring complex corresponding to formula (I) below: