Study On The Compound Inhibiting The Yeast Ca²⁺-signal Pathway From Safflower

An immunosuppressant is any substance that performs immunosuppression of the immune system. When the immune system function is suppressed, they will regulate the immunoreactions by act on T-Cells, B-Cells or other related cells. Immunosuppressants are applied as a countermeasure:the side-effect is that the body becomes more vluerable to infections and malignancy, like versus-host disease, rheumatoid arthritis, lupus sebaceous, dermatomycosis, membranous glomerulonephritis, inflammatory bowel disease, and autoimmune hemolytic anemia. At present, the wildly used immunosuppressions, like Ciclosporin A and Tacrolimus, are act on the calcineurin which could regulate the Ca2+-signal pathway, resulting in increases the activity of genes coding for IL-2and related cytokines.This experiment uses a new screen model-yeast positive screen model to screen the compounds which specially inhibit the Ca2+-signal pathway. By screening a series of plants, we found that the safflower crude extracts show strong activity. And then we purified the safflower crude extracts by liquid-liquid extract, silica column chromatograph, Sephadex LH-20column chromatograph, SPE, HPLC. Finally,4active peaks had been found, and Compound A was purified from No.3peak, the molecular weight is309.2505.Compound A show the good stability, it could store for a long time at the natural condition. Even if locate in the high level concentration of metal ion condition, compound A wouldn’t react on the metal ions. However, the structure and function of compound A will be changed, when the temperature higher than80℃and keep to a certain time. After illuminated for8days, the activity of compound A also is weakened in a certain degree. Compound A will be destroyed by strong acid or strong base, when the pH=2, the function of inhibit the yeast Ca2+-signal pathway of compound A was lost, and when the pH=12, the structure and function of compound A has been changed.Compound A, like FK506, by acts on the calcineurin, regulate the calcium ion pathway and take effect on the Ca2+-siganl-mediated cell-cycle. On account of compound A could regulate the ca2+-signal-mediated cell-cycle like FK506and good stability in natural condition, it is a good candidate drug of immunosuppressant.