Vinblastine is a dimeric indole alkaloid extracted from Catharanthus roseus. Vinblastine can be used for anti-cancer and antihypertensive, especially its anti-cancer effect has been valued and applied in clinic. Vinblastine and vincristine can reduce the synthesis of deoxyribonucleic acid (DNA), ribonucleic acid (RNA) and protein, inhibit the mitosis of cancer cells, and stop cell division in the metaphase. Therefore, tumor cells cannot increase in value. Vinblastine in Catharanthus roseus contains about four tenths of a million. It can be used to treat leukemia, Hodgkin's disease and lymphosarcoma. It has certain curative effects on breast cancer, ovarian cancer, testicular cancer and monocytic leukemia. It is also effective for reticulocyte sarcoma, nephroblastoma and malignant melanoma, and has been included in several national pharmacopoeias. Vincristine is mainly effective for malignant lymphoma, acute and chronic leukemia, small cell lung cancer and breast cancer.

    But vinblastine also has some toxic and side effects. Vinblastine combines with red blood cells, white blood cells, platelets and plasma in the blood. After treatment, 33% of vinblastine is excreted from bile as metabolites, and 21% is excreted from urine in its original form. Vincristine is mainly excreted from bile. Vinblastine adult 10mg/ time (or 6mg/m2), children 10mg/m2, 1 / week, 1 course of treatment, the total amount of 60 ~ 80mg; vincristine adult 1 ~ 2mg/ time (or 1.4mg/m2), children 75 μ g/kg, once a week, intravenous injection or infusion; LD50 vinblastine was 17mg/kg by intravenous injection in mice,Vinblastine2.1mg/kg. The main damage was myelosuppression, digestive tract reaction and peripheral neuritis. And has the following clinical manifestations:

    1. peripheral neuritis is the main adverse reaction, including limb pain, muscle tremor, disappearance of tendon reflex, numbness of finger (toe) tip, etc.

    2. Bone marrow suppression and digestive tract reaction of VCR.

    3. some have postural hypotension, hair loss, insomnia, etc.

  Once the above symptoms are found, we need to take active treatment measures. The main treatment points are as follows:

    1. strictly check the hemogram (during medication). Those with poor liver function should be reduced as appropriate.

    2. patients with severe nervous system symptoms should reduce or stop taking drugs, and choose B vitamins, calcium formyl tetrahydrofolate, etc.

    3. prevent extravasation of drug solution during intravenous injection.

    4. symptomatic and supportive treatment.

    Vinblastine has strong anti-tumor pharmacological activity, but there are also some problems such as strong cytotoxicity and poor water solubility. Therefore, while improving the curative effect, how to reduce adverse reactions and increase water solubility are the main problems to be solved. First of all, reducing the toxic and side effects of vinblastine drugs and maintaining their original pharmacological activity are the basic principles of priority in the structural modification of vinblastine drugs. Secondly, the synthetic target should have certain action sites that can bind to the corresponding parts of microtubules or cells, so as to have an effect on tumor cells and tissues. Finally, because the subtle structural differences may lead to great changes in pharmacological activities, we must pay attention to the changes in the stereoscopic configuration of functional groups in structural modification.