环孢霉素.ppt

Cyclosporin A — A review on fermentative production, downstream processing and pharmacological applications
Shrikant A. Survase, Lalit D. Kagliwal, Uday S. Annapure, Rekha S. Singhal
Contents
Brief introduction
Fermentative production
Isolation , purification and analysis.
ics and toxicity
Therapeutic uses
Brief introduction
Immunosuppressants are a class of drugs which are capable of inhibiting the body's immune drugs are used an transplant patients to prevent rejection of an by the body by decreasing the body's own natural defense to foreign bodies, and are also useful in the treatment of autoimmune is one of the monly prescribed immunosuppressive drugs for the treatment of patients an transplantation and autoimmune diseases including AIDS owing to its superior T-cell specificity and low levels of myelotoxicity.

In 1973, CyA was purified from the fungal extract of T. inflatum.
in 1975 ,complete structural analysis was established.
in 1983 ,CyA was approved by the USFDA for clinical use to prevent.
graft rejection in transplantation.
In 1984, synthetic CyA was produced.
structure and Physical properties
It is made up of eleven amino acids, ten of which are known aliphatic amino acids but the amino acid at position one was unknown.
molecular weight:
melting point: 148 - 151 °C
(natural)
and 149 °C -150 °C (synthetic)
solubility:slightly soluble in water and soluble anic solvents is easy.

A possible mechanism of CyA synthesis:
• Synthesis of all 11 constituent amino acids
• Activation of each amino acid
• N-methylation and peptide bond formation, and finally
• The cyclization reaction
Exogenous supply of amino acid precursors in the fermentation medium to strongly influence the cyclosporin biosynthesis.
of action
Immunosuppressants affect ponents of the immune system such as T-helper, T-effector cell function, antigen presentation and B-lymphocyte cell function.
It was init