Rapamycin (RAPA) is a new macrolides immunosuppressant, white solid crystal, melting point of 183-185℃, lipophile, dissolved in methanol, ethanol, acetone, chloroform and other organic solvents, very slightly soluble in water, almost insoluble in ether.
Was developed in the early 1970 s, initially was as low toxicity antifungal drugs, immunosuppressive effects of discovery in 1977, started in 1989 the RAPA as a rejection of the new drug for the treatment of organ transplantation in trial, look from animal experiment and clinical application effect, is a kind of good curative effect, low toxicity, no new immunosuppressant nephrotoxicity.
While it is often used as a drug to maintain the immune capacity of transplanted organs (especially kidney transplants) to slow the immune rejection response after organ transplantation, scientists have recently found another use for it: to treat alzheimer's disease.
Interestingly, the main component of rapamycin was also found in the bacterial product of the isolated soil on Easter island, and recent experiments showed that it restored the ability to remember defects in mice.
Rapamycin is a macrolide antibiotic with a similar structure to prozac (FK506), but with very different immunosuppressive mechanisms.
FK506 inhibits the proliferation of T lymphocytes from G0 to G1, while RAPA blocks the signaling process of T lymphocytes and other cells from G1 to S through different cytokine receptors. Compared with FK506, RAPA blocks calcium-dependent and non-calcium-dependent signaling pathways of T lymphocytes and B lymphocytes.
Medical researchers at the university of Chicago used commercially available oral rapamycin tablets combined with grapefruit juice to treat melanoma, a malignant cancer common in Europe and the United States, to significantly improve the anti-cancer effects of other chemotherapy drugs and thus prolong survival.
Studies have shown that rapamycin is easily decomposed by enzymes after entering the digestive tract, while grapefruit juice contains a large amount of furanocoumarins, which can inhibit the destruction of rapamycin by enzymes in the digestive tract, thus improving the bioavailability of rapamycin.
It is said that the earliest Dutch doctors have found: grapefruit juice has the effect of improving the oral absorption of mountain Ming, now European and American doctors will be applied to rapamycin preparations.