immunosuppressant

Rapamycin (AY 22989) is a natural product of macrolides, an mTOR inhibitor with specificity (HEK293 cells: IC50=0.1 nM). Rapamycin has immunosuppressive activity and induces autophagy.

Cyclosporin A is a naturally occurring cyclic polypeptide that is the active metabolite of a fungus. Cyclosporin A is an immunosuppressant that binds to procyclins and inhibits calcineurin (IC50=7 nM).

trans-Benzylideneacetone (Acetocinnamone) is used in various synthetic preparations.

Cortisone (17-Hydroxy-11-dehydrocorticosterone) is a corticosteroid with potent glucocorticoid activity.

Mizoribine (NSC-289637) belongs to the family of 1-Ribosyl-imidazolecarboxamides. Mizoribine has been investigated for the treatment of Rheumatoid Arthritis.

Cortisone Acetate is a synthetic or semisynthetic analog of the naturally occurring cortisone hormone produced by the adrenal glands with anti-inflammatory and immunomodulating properties. Cortisone acetate (NSC-49420) diffuses through the cell membrane and binds to nuclear glucocorticoid receptors. The receptor-ligand complex binds to promotor regions of certain genes and initiates RNA transcription. This results in an induction of synthesis of certain anti-inflammatory proteins while inhibiting the synthesis of certain inflammatory mediators.

Tacrolimus (Fujimycin) can bind FKBP12 to form a high-affinity complex (Ki: 0.2 nM) which inhibits the activity of the calcium calmodulin-dependent protein phosphatase.

Microcolin B, an acylpeptide immunosuppressant, is a highly potent and biologically unique compound containing proline. It is derived from the blue-green alga Lyngbya majuscule.

Ascomycin (Immunomycin)(Immunomycin, FR-900520, FK520) is an ethyl analog of tacrolimus (FK506) with strong immunosuppressant properties.

Cyclosporin C (Cs-C) is a fungal metabolite against filamentous phytopathogenic fungi. Cyclosporin C has antifungal, antiviral, and immunosuppressant properties.

Homodestcardin is a cyclic depsipeptide fungal metabolite that has been found in T. roseum and has immunosuppressant activity. It inhibits concanavalin A-induced proliferation of isolated mouse T cells.

Plipastatin A1, a lipopeptide isolated from B. cereus, demonstrates enzyme inhibitory and immunosuppressant properties. It effectively inhibits enzymes phospholipase A2 (PLA2), phospholipase C (PLC), and phospholipase D (PLD) with half-maximal inhibitory concentrations (IC50s) of 2.9, 1.3, and 1.4 µM, respectively. Additionally, at a concentration of 100 µg/ml, plipastatin A1 inhibits lipopolysaccharide (LPS)-induced B cell blastogenesis and T cell blastogenesis triggered by concanavalin A. In vivo studies reveal that a dose of 0.1 mg/animal effectively suppresses delayed-type hypersensitivity in mice.

Isogarcinol is a natural polyisoprenylated benzophenone first isolated from plant species in the genus Garcinia. It has immunosuppressant actions, inhibiting the protein phosphatase calcineurin (IC50 = 36 μM) and suppressing the proliferation of T cells. Oral administration of isogarcinol in mice decreases delayed type hypersensitivity, prolongs graft survival in allogeneic skin transplants, suppresses inflammation in collagen-induced arthritis, and reduces clinical symptoms in experimental autoimmune encephalomyelitis. Isogarcinol inhibits the proliferation of HL-60 and PC-3 cancer cells (IC50s = 4 and 8 μg ml, respectively) through cell cycle arrest and apoptosis.