In situ Detection of Human Monocyte/ Macrophage Serine Esterase-1 mRNA Expression in Human Tissues

Abstract

Human monocyte/macrophage serine esterase (HMSE) can be distinguished from esterases of other blood cells by a specific isoelectric focusing pattern of five enzyme variants. Using a HMSE-1 cDNA, expression of mRNA was investigated by nonradioactive in situ hybridization of human biopsy specimens and cytospin preparations. HMSE-1 transcripts could be detected in the myelomonocytic cell line U-937, blood monocytes and in tissue macrophages. Immune accessory cells of the monocyte/macrophage lineage did not express detectable amounts of HMSE-1 mRNA. These results indicate that HMSE-1 represents a cell-lineage-specific enzyme which can be used to characterize physiological and neoplastic variants of the human monocyte/macrophage cell system. The method described will enable further insight into the physiological function of HMSE-1.

Intramuscular Administration of Paliperidone Palmitate Extended-Release Injectable Microsuspension Induces a Subclinical Inflammatory Reaction Modulating the Pharmacokinetics in Rats

“…The macrophages themselves might therefore act as a source of sustained drug release. It is important to note that the intracellular concentrations of free (i.e., hydrolysable) PPP remain extremely low, whereas esterase expression in macrophages and skeletal muscle tissue is pronounced . It is consequently improbable that the enzymatic hydrolysis process gets saturated and becomes rate limiting.…”

Drug Targeting to Monocytes and Macrophages Using Esterase-Sensitive Chemical Motifs

“…One of these, human carboxylesterase-1 (hCE-1), has a restricted expression profile in humans (Satoh et al, 1999;Uphoff and Drexler, 2000;Su et al, 2004;Li et al, 2005), with cells of the monocytemacrophage lineage being the principal source of the enzyme outside the hepatocyte. We postulated that tissue exposure to a drug-ester conjugate that is a specific substrate for hCE-1 might lead to intracellular ester hydrolysis and production of a pharmacologically active acid only within those cell types.…”

Carboxylesterase 1 (Ces1): from monocyte marker to major player

“…If it is a hepatocyte enzyme it would be foolish to postulate that monocyte Ces1 could represent total Ces1 potential activity. However, the use of in situ hybridisation with digoxigenin-labelled human macrophage serine esterase/CES1 cDNA has demonstrated Ces1 mRNA in monocytes and macrophages only, the latter including the Kupffer cells of the liver 42. The large diffuse Kupffer cell content of the liver and its intimacy with hepatocytes could potentially cause confusion in the attribution of Ces1 activity of liver microsomes to hepatocytes in pharmacological studies.…”