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.

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.

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

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

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

Cyclosporin A is a natural product and an active fungal metabolite, classified as a cyclic polypeptide immunosuppressant. It binds to cyclophilin and inhibits the activity of calcineurin (IC₅₀ = 7 nM) as well as CD11a/CD18 adhesion molecules. It is commonly used to induce uremia models.

Tacrolimus (FK506, Fujimycin) is a macrolide immunosuppressant that binds to FKBP12 to form a high-affinity complex (Ki = 0.2 nM), which inhibits calcineurin phosphatase activity, thereby suppressing T lymphocyte signal transduction and the transcription and release of IL-2. It exerts potent immunosuppressive effects and can be used to induce immunosuppression models.

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

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

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.

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.

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.

Lymphostin is an immunosuppressant that inhibits lymphocyte kinase, with an IC50 of 0.05 μM, and also suppresses mixed lymphocyte reactions, demonstrating an IC50 of 0.009 μM. Lymphostin exhibits no effects on both Gram-positive and Gram-negative bacteria.

Cytoxazone is an immunosuppressant that also acts as a cytokine regulator. At concentrations ranging from 6.25 to 25 μg/mL, Cytoxazone inhibits the production of IL-4 and IL-10 induced by Pokeweed mitogen (PWM), while not affecting the PWM-induced production of GM-CSF.