Nitrogen mustard hydrochloride Uses and synthesis methods |
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Antitumor drugs |
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Enbixin, also known as nitrogen mustard and nitrogen mustard hydrochloride, is one of the earliest drugs used in clinical tumors.
It can be used as a representative of other alkylating anti-tumor drugs, and its derivatives still occupy a certain position in clinical treatment.
This type of drug has active alkylating genes, which can react with the amino, sulfhydryl, carboxyl and phosphate groups of cells, affect cell metabolism,
and lead to cell death. It is a non-specific drug for the cell cycle. After entering the human body, this product is hydrolyzed in the body to
release chloride ions and become free radicals. Through intramolecular cyclization, it forms highly active ethyleneimine ions, which can alkylate
with deoxyribonucleic acid,affect nucleic acid metabolism, inhibit cell mitosis, and have a strong cytotoxic effect.Its disadvantage is that the
effect on tumor cells and normal cells is not much different,the selectivity is poor,so the toxicity is also high. |
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After entering the body, Enbixin dissociates quickly, and 90% of the drug in plasma disappears within 0.5 to 1 minute,so the effect is short-lived.
But its effect can last for a long time.Chemicalbook has no obvious selectivity in the distribution of the body,but it is
less distributed in the brain,and a very small amount is excreted in the urine in its original form. |
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At present, Enbixin has been clinically used in my country to treat malignant lymphomas, including Hodgkin's disease, lymphosarcoma,
reticulocyte sarcoma, giant follicular lymphoma, mycosis fungoides and lung cancer, especially for undifferentiated cancer. If combined with other drugs,
the effect is better. It also has a certain effect on chronic myeloid leukemia, chronic lymphocytic leukemia, breast cancer, ovarian cancer, choriocarcinoma, etc.
In addition, the method of abdominal aorta blockage (half-body blockage) and intravenous injection of large doses of nitrogen mustard has a good effect on the treatment of
head and neck cancer (such as nasopharyngeal carcinoma), which can protect part of the bone marrow and relatively increase the distribution of drugs in the upper body.
Local use ofits ethanol or dimethyl sulfoxide (0.05%) solution to treat psoriasis, vitiligo, and mycosis fungoides also has a good short-term effect.
It can be injected into the chest, abdomen or pericardial cavity for malignant body cavity effusion. Enbixin can also be used as an immunosuppressant. |
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Biological activity |
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Mechlorethamine is a prototype alkylating agent that works by binding to DNA, cross-linking the double strands and preventing cell replication. |
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Target |
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DNA synthesis | Value |
In vitro studies |
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In vitro studies |
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Mechlorethamine was less toxic to rat hepatocytes under nitrogen and caused less lipid peroxidation than under aerobic conditions. In primary cultures of rabbit trachea, mechlorethamine significantly inhibited cell growth and caused cell detachment associated with cytoskeletal protein rearrangement. In primary cultures of rabbit trachea, mechlorethamine caused early lipid peroxidation and cell membrane damage, which was associated with a significant increase in the activity of antioxidant enzymes associated with increased glutathione content. |
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In vivo studies |
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Mechlorethamine (1.5 mg/kg i.v.) reduced the mean white blood cell count in rabbits from 6,320 mm. Mechlorethamine (0.005 mg-0.5 mg, i.d.)
induced dose-dependent skin ulcers in mice. Immediate administration of isotonic (0.167 M) or hypertonic (0.34 M) sodium thiosulfate (0.05 mL) after mechlorethamine
injection significantly reduced the mean HN2 ulcer area and total ulcer duration. |
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Uses |
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Used as anti-tumor drugs |
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Categories |
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Toxic substances |
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Toxicity classification |
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Highly toxic |
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Acute toxicity |
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Oral-rat LD50: 10 mg/kg; Oral-mouse LD50: 20 mg/kg |
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Flammability hazard characteristics |
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Combustion produces toxic nitrogen oxides and chloride fumes; Side effects of drugs: nausea, vomiting, decreased white blood cell and platelet counts |
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Storage and transportation characteristics |
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Storage is ventilated and dry at low temperature; stored separately from food raw materials |
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Fire extinguishing agents |
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Dry powder, foam, sand, carbon dioxide, mist water |
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