immunomodulatory agent

Isotretinoin (13-cis-Retinoic acid) binds to and activates nuclear retinoic acid receptors (RARs); activated RARs serve as transcription factors that promote cell differentiation and apoptosis. Isotretinoin is a naturally-occurring retinoic acid with potential antineoplastic activity. This agent also exhibits immunomodulatory and anti-inflammatory responses and inhibits ornithine decarboxylase, thereby decreasing polyamine synthesis and keratinization.

Bestatin (Ubenimex) competitively inhibits many aminopeptidases, including B, N and leucine aminopeptidases. Ubenimex is a microbial metabolite and dipeptide with potential immunomodulatory and antitumor activities. Aminopeptidases has been implicated in the process of cell adhesion and invasion of tumor cells. Therefore, inhibiting aminopeptidases may partially attribute to the antitumor effect of ubenimex. This agent also activates T lymphocyte, macrophage, and bone marrow stem cell as well as stimulates the release of interleukin-1 and -2, thus further enhances its antitumor activity.

1. Telocinobufagin (Telobufotoxin) is the major endogenous digitalis-like factor. 2. Telocinobufagin significantly decreases the bacterial burdens in the spleen and prolongs the survival time of FIST-immunized mice challenged with live S. typhimurium. 3. Telocinobufagin has immunomodulatory activity, can enhance a Th1 immune response to control intracellular infections, could be developed as a novel immunotherapeutic agent to treat cancer and other immune-mediated diseases.

Dimethyl fumarate (DMF), a fumarate derivative, is used as antiinflammatory and immunomodulatory agent.

Piceatannol (Astringenin) is an anti-inflammatory, immunomodulatory and antiproliferative agent. It inhibits p56lck and syk protein tyrosine kinases and inhibits NF-κB activation and gene expression of TNF-induced. It is synthetic from the conversion of resveratrol by cytochrome P450 1B1.

Thymopentin acetate, primarily secreted by the epithelial cells of the thymic cortex and medulla, serves as an effective immunomodulatory agent. It possesses a short plasma half-life of 30 seconds and significantly enhances the generation of T-cell lineage from human embryonic stem cells (hESCs) [1] [2].