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The aminosalicylate - folate connection.

Robert E London¹

¹Genome Integrity and Structural Biology Laboratory, National Institute of Environmental Health Sciences, NIH, Research Triangle Park, North Carolina, USA.

Drug Metabolism Reviews

|January 17, 2024

Summary

p-aminosalicylate (PAS) and 5-aminosalicylate (5AS, mesalamine) are aminosalicylate isomers with distinct pharmacological actions. PAS targets tuberculosis by inhibiting folate metabolism, while 5AS acts as a gut bacteria-directed antifolate for inflammatory bowel diseases.

Keywords:

5-aminosalicylate Ulcerative colitis inflammatory bowel disease mesalamine p-aminosalicylate tuberculosis

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Area of Science:

Pharmacology
Microbiology
Medicinal Chemistry

Background:

Aminosalicylate isomers, p-aminosalicylate (PAS) and 5-aminosalicylate (5AS), exhibit significant pharmacological activities.
PAS is an anti-tubercular agent, while 5AS (mesalamine) treats ulcerative colitis and inflammatory bowel diseases.

Purpose of the Study:

To review studies on PAS metabolism and its mechanisms of inhibiting Mycobacterium tuberculosis dihydrofolate reductase (mtDHFR).
To explore the role of 5AS as a pABA antagonist and its impact on bacterial folate biosynthesis.
To elucidate the antifolate activity of mesalamine against gut bacteria.

Main Methods:

Review of existing literature on PAS and 5AS metabolism and mechanisms of action.
Analysis of structural data to support the interaction of 5AS with dihydropteroate synthase (DHPS).

Main Results:

PAS is incorporated into folate metabolism by M. tuberculosis, yielding a dihydrofolate analog and inhibiting mtDHFR.
5AS acts as a pABA antagonist, potentially blocking pABA binding or forming adducts with DHPS.
Mesalamine functions as a gut bacteria-specific antifolate, targeting rapidly growing, folate-dependent species.

Conclusions:

Both PAS and 5AS interfere with bacterial folate biosynthesis through distinct mechanisms.
PAS selectively targets Mycobacterium tuberculosis, while 5AS offers a targeted approach for gut bacteria in IBD treatment.
Understanding these antifolate mechanisms provides insights into drug development for infectious diseases and inflammatory conditions.