| Description | Fudosteine is a cysteine derivative that interferes with the increase in goblet cell number, expression of the mucin MUC5AC, and subsequent mucin secretion, in airways agonized with tobacco smoke, isoproterenol, lipopolysaccharide, TNF-α, or oxidants. Fudosteine, which is a thiol compound with antioxidant properties, limits NF-κB signaling and reduces inflammatory gene expression. It has greater bioavailability than N-acetyl-cysteine and increases cysteine levels in cells. |
| Description | Fudostein was launched in Japan as a new mucoactive agent for thetreatment of bronchitis and respiratory congestion. This cysteine derivative was obtainedfrom L-cysteine by condensation with either allylic alcohol in the presence of potassiumpersulfate or the corresponding bromoalcohol in the presence of a base. Fudostein wasshown to significantly reduce mucus glycoprotein hypersecretion and inhibit infiltration ofairway mucosa by lymphocytes and inflammatory cells in bronchitic rats. When given tobronchitic rabbits, an oral dose of 500 mg/kg daily potently decreased the fucose/ N-acetylneuraminicacid in sputa, so exhibiting mucoregulatory properties. In another studywith SO2-exposed rabbits, fudostein suppressed blood flow of tracheal microvasculatureincreased by SO2, partly due to scavenging of superoxide anion. |
| Chemical Properties | Off-White Powder |
| Originator | SS Pharmaceutical/Mitsubishi Pharma (Japan) |
| Uses | An antiinflammatory expectorant MUC5 mucin obstructive pulmonary disease. |
| Uses | Fudosteine is a novel mucoactive agent and a MUC5AC mucin hypersecretion inhibitor. MUC5AC mucin synthesis and the expression of the MUC5AC gene were increased by LPS in rats or TNF-α in NCI-H292 cells; these effects were inhibited by fudosteine treatment |
| Uses | An antiinflammatory expectorant used in the treatment of MUC5 mucin obstructive pulmonary disease. |
| Uses | A demonstrated antiinflammatory |
| Uses | Fudosteine is a cysteine derivative that interferes with the increase in goblet cell number, expression of the mucin MUC5AC, and subsequent mucin secretion, in airways agonized with tobacco smoke, isoproterenol, lipopolysaccharide, TNF-α, or oxidants. Fudosteine, which is a thiol compound with antioxidant properties, limits NF-κB signaling and reduces inflammatory gene expression. It has greater bioavailability than N-acetyl-cysteine and increases cysteine levels in cells. |
| Definition | ChEBI: Fudosteine is an organic molecular entity. |
| Brand name | Cleanal, Spelear (Mitsubishi Pharma) |
| Hazard | A reproductive hazard. |
| Synthesis | Fudosteine is synthesized by condensation of L-cysteine with 3-bromopropyl alcohol in aqueous NaOH, or by condensation of L-cysteine with allyl alcohol by means of aqueous potassium persulfate.
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| References | [1] KOICHI TAKAHASHI . Effects of SS320A, a New Cysteine Derivative, on the Change in the Number of Goblet Cells Induced by Isoproterenol in Rat Tracheal Epithelium[J]. Japanese journal of pharmacology, 1998, 77 1: Pages 71-78. DOI: 10.1254/jjp.77.71
[2] C K RHEE. Effect of fudosteine on mucin production.[J]. European Respiratory Journal, 2008: 1195-1202. DOI: 10.1183/09031936.00018508
[3] RAHMAN I. Pharmacological antioxidant strategies as therapeutic interventions for COPD[J]. Biochimica et biophysica acta. Molecular basis of disease, 2012, 1822 5: Pages 714-728. DOI: 10.1016/j.bbadis.2011.11.004 |
