Drug intelligence / Profile preview

genipin

Development stage
Phase 3
Modality
Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral (investigational/experimental Use)
01

Overview

Genipin is a naturally occurring iridoid monoterpenoid aglycone derived from the hydrolysis of geniposide found in the fruit of *Gardenia jasminoides* and *Genipa americana*[1][3][6][9]. It is best known as a natural cross-linking agent for proteins such as collagen and gelatin due to its low toxicity compared to synthetic alternatives like glutaraldehyde[1][2][3][5]. Genipin has demonstrated diverse pharmacological activities including anti-inflammatory, antioxidative, neuroprotective, neurotrophic effects[3], choleretic action (promoting bile secretion)[6], and inhibition of lipid peroxidation and nitric oxide production[6]. Mechanistically, genipin inhibits mitochondrial uncoupling proteins UCP2 (and also UCP1/UCP3), thereby affecting mitochondrial proton transport and energy metabolism[2][6]. It has been used in traditional Chinese medicine for various indications such as inflammation reduction and liver disease. Genipin-cross-linked hydrogels are widely researched for drug delivery applications due to their biocompatibility and biodegradability[5].

Other names
genipin(+)-genipinmethyl (1R,4aS,7aS)-1-hydroxy-7-(hydroxymethyl)-1,4a,5,7a-tetrahydrocyclopenta[c]pyran-4-carboxylate
02

Targets

UCP2 (Uncoupling protein 2)UCP3 (Mitochondrial uncoupling protein 3)

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