Defensamide

Defensamide is an activator of sphingosine kinase 1 (SPHK1).¹ It increases sphingosine-1-phosphate (S1P) levels in primary human keratinocytes but does not affect S1P lyase activity in the same cells when used at a concentration of 100 µM. Defensamide (100 µM) increases protein levels of cathelicidin antimicrobial peptide (CAMP), also known as LL-37 (Item No. 24461), in primary human keratinocytes. It inhibits the invasion of S. aureus into murine skin ex vivo. Defensamide has also been used as an intermediate in the synthesis of the fungal metabolites sinuxylamide A as well as compounds with anticancer and antibacterial activities.^2,3

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1. Jeong, S.K., Kim, Y.I., Shin, K.-O., et al. Sphingosine kinase 1 activation enhances epidermal innate immunity through sphingosine-1-phosphate stimulation of cathelicidin production. J. Dermatol. Sci. 79(3), 229-234 (2015).

2. Annapurna, K., Rao, K.S., and Narsaiah, A.V. Synthesis of glycoprotein inhibitory agents sinuxylamide A-E. Indian J. Chem. 61, 1039-1045 (2022).

3. Vudhgiri, S., Prasad, R.B.N., Poornachandra, Y., et al. The impact of sugar and fatty acid on the bioactivity of N-fatty acyl-L-tyrosine aglycone. J. Chem. Sci. 129(6), 663-677 (2017).