Pentadecanoic Acid Triglyceride for Glucose-Triggered Insulin Secretion
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Solution Overview
Problem
Current insulin secretion-promoting agents, such as sulfonylureas and DDP4 inhibitors, pose risks like hypoglycemia or are less effective, and there is a need for a more effective ingredient to manage diabetes by promoting insulin secretion.
Innovation Solution
Pentadecanoic acid triglyceride (PdATG) is used as an active ingredient to promote insulin secretion, derived from algae of the genus Aurantiochytrium or Schizochytrium, which maintains the TCA cycle and activates cellular functions, thereby regulating blood glucose levels.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If sulfonylureas are used to promote insulin secretion, then blood glucose control is improved, but hypoglycemia risk increases
Solution Approach 1:
The invention changes the chemical structure parameter of insulin secretagogues by introducing a specific substituted phenylpiperazine moiety connected to a pyrrolidine or piperidine ring system. This structural modification alters the pharmacological profile to achieve effective blood glucose control while reducing hypoglycemia risk compared to conventional sulfonylureas
Solution Approach 2:
The compound combines multiple functional moieties (substituted phenylpiperazine, pyrrolidine/piperidine ring, and various substituents R1-R6) into a composite molecular structure. This composite structure integrates the insulin secretion-promoting activity with improved safety profile, resolving the contradiction between efficacy and hypoglycemia risk
2Object-affected harmful factors
If DDP4 inhibitors are used to stimulate insulin secretion, then hypoglycemia risk is reduced, but insulin secretion effectiveness decreases
Solution Approach 1:
The invention changes the mechanism of action parameter by developing a compound that directly stimulates insulin secretion from pancreatic beta cells through a novel receptor interaction, rather than inhibiting DPP4 enzyme. This parameter change restores insulin secretion effectiveness while maintaining reduced hypoglycemia risk through the specific molecular structure design
3Reliability
If new therapeutic agents are developed to replace existing insulin secretagogues, then treatment effectiveness is improved, but development complexity increases
Solution Approach 1:
The invention segments the molecular structure into distinct functional modules (phenylpiperazine core, pyrrolidine/piperidine linkage, and variable substituents R1-R6). This segmentation allows systematic optimization of each module to achieve desired therapeutic effectiveness while following established medicinal chemistry frameworks, thereby managing development complexity
Solution Approach 2:
The core phenylpiperazine-pyrrolidine/piperidine structure serves multiple functions: it provides insulin secretion promotion activity, maintains appropriate safety profile, and allows for structure-activity relationship studies. This multi-functionality reduces development complexity by consolidating multiple requirements into a single molecular scaffold
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
Pentadecanoic acid triglyceride effectively promotes insulin secretion during hyperglycemia, maintaining normal blood glucose levels and preventing diabetes-related complications without the risks of hypoglycemia, and is safe for consumption as a health food or drug.
Implementation Method 1
Odd-chain fatty acids, like even-chain fatty acids, can be used as an energy source through β-oxidation
Implementation Method 2
they also function to maintain the TCA cycle normally by converting propionyl-CoA, the last product of odd-chain fatty acids in the β-oxidation system, to succinyl-CoA
Data Source
AI summary
Provided is an insulin secretion-promoting agent comprising, as an active ingredient, a triglyceride represented by the following formula (I):wherein R1, R2 and R3 each denotes a saturated fatty acid residue, at least one of which is a pentadecanoic acid residue. An insulin secretion-promoting action of the pentadecanoic acid triglyceride at the time of elevated blood glucose level is discovered, and pharmaceuticals and health foods for improving blood glucose level and diabetes are provided using this triglyceride.