Rapamycin powder (RAPA) is a new type of macrolide immunosuppressant. It is a white solid crystal with a melting point of 183-185℃. It is lipophilic and soluble in organic solvents such as methanol, ethanol, acetone, and chloroform. It is very slightly soluble in water and almost insoluble in ether. It was developed as early as the 1970s. It was initially used as a low-toxic antifungal drug. In 1977, it was found to have an immunosuppressive effect. In 1989, RAPA was tried as a new drug for the treatment of organ transplant rejection. From the results of animal experiments and clinical applications, it is a new type of immunosuppressant with good efficacy, low toxicity, and no nephrotoxicity. It is now often used as a drug to maintain the immune capacity of transplanted organs (especially kidney transplants) to slow down the immune rejection reaction after organ transplant surgery. The latest experiments show that the substance can restore memory defects when applied to experimental mice.
Rapamycin powder is synthesized from seven units of acetate and seven units of propionate through the polyketide pathway, and the required O-methyl group comes from methionine. In fact, the nitrogen source is a derivative of shikimic acid after reduction. The integrity of the cyclohexane group is retained in the process of forming cyclohexane derivatives from shikimic acid. Lysine is first deaminated to form carboxylic acid piperidine, which is then connected to the polyketide acetyl bond and amide bond to form the initial structure of Rapamycin powder.
Item | Test Standard | Testing Result |
Appearance | 99% | Complies |
Color | White Powder | Complies |
Particle Size | 100% pass 80 mesh | Complies |
Oder | Characteristic | Complies |
Taste | Characteristic | Complies |
Loss on Drying | ≤5.0% | 2.20% |
Residue on Ignition | ≤0.1% | 0.05% |
Residual | ≤0.1% | Complies |
Residual Ethanol | ≤0.5% | Complies |
Heave Mentals | ≤10ppm | Complies |
Na | ≤0.1% | <0.1% |
Pb | ≤3 ppm | Complies |
Total Plate | <1000CFU/g | Complies |
Yeast & Mold | <100 CFU /g | Complies |
E. Coli | Negative | Complies |
Salmonella | Negative | Complies |
1. Anti-tumor effect
Rapamycin powder works by blocking the mammalian target of rapamycin (mTOR) signaling pathway. mTOR is involved in cell growth, division and survival, and plays a key role in tumor occurrence and development. The drug can be used to treat a variety of solid tumors and hematological malignancies. Patients can use it under the guidance of a doctor.
2. Immunosuppression
Rapamycin can inhibit the activation and proliferation of T lymphocytes, thereby reducing the body's immune response. For patients with organ transplantation or autoimmune diseases, it can reduce rejection and disease activity. Patients need to monitor their infection risk and adjust their immune status.
3. Anti-proliferation
Rapamycin can interfere with the cell cycle process, preventing cells from entering the S phase from the G1 phase, thereby inhibiting cell mitosis. The drug is suitable for the treatment of certain specific types of cancer, such as renal cell carcinoma. Close observation of the patient's hematopoietic function and possible side effects is required.
4. Anti-angiogenesis
Rapamycin can inhibit endothelial cell migration and new blood vessel formation, which is due to its influence on the proliferation and migration of smooth muscle cells and the survival of endothelial cells. Therefore, rapamycin is widely used in ophthalmology to control abnormal blood vessel growth in diabetic retinopathy. When using it, attention should be paid to possible blurred vision or other eye side effects.
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