Camptothecin( 7689-03-4)

Alkaloids: Camptothecin is an alkaloid extracted from the seeds or root bark of Camptotheca acuminata, a deciduous plant of Davidia involucrata family. It can directly destroy the DNA structure and DNA binding, making DNA vulnerable to the attack of endonuclease, while inhibiting the DNA polymerase and affecting the replication of DNA. It is mainly sensitive to proliferating cells. It is a cell cycle-specific drug, which acts on the S phase and has a slight killing effect on G1, G2 and M phase cells. It has an inhibitory effect on a variety of animal tumors, and has no cross-resistance with common anti-tumor drugs. When combined with monoamine glycyrrhizinate, it can reduce toxicity without reducing efficacy. The mechanism of external treatment of psoriasis is to inhibit the mitosis of rapidly dividing keratinocytes, make the hyperplastic spinous cell layer thinner, the incomplete keratinization disappear, and the granular layer resume to form. After intravenous injection, most of the drugs are combined with plasma protein, and the half-life in plasma, kidney and liver is 30 minutes. The content of gastrointestinal, bone marrow and kidney is the highest. This product is excreted slowly, mainly by urine in its original form, and can be excreted by 17% in 48 hours. It is mainly used for gastric cancer, colon cancer, rectal cancer, head and neck cancer, bladder cancer, etc

Physical and chemical properties: pale yellow acicular crystal. Melting point 264~267 ℃[ α] D20+31.3 ° (chloroform: methanol=1 ∶ 2). Insoluble in water, soluble in chloroform, methanol and ethanol. Its solution shows purple-blue fluorescence under the ultraviolet lamp. It is easy to deteriorate when exposed to light and slightly hygroscopic. It shows yellow-green fluorescence when exposed to concentrated sulfuric acid. It is diluted with distilled water to produce yellow-green fluorescence, which is alkaline. It reacts with potassium bismuth iodide to form orange-red complex salt precipitation. It is extracted from the roots of Camptotheca acuminata or fruit powder with organic solvent. Due to its high toxicity, it should be carefully extracted and has anti-tumor activity. 10-hydroxycamptothecin is less toxic in the treatment of intestinal cancer, rectal cancer, gastric cancer and leukemia. Figure 1 shows the structural formula of camptothecin.

Indications: It is mainly used for digestive tract tumors and has good curative effect on gastric cancer, rectal cancer and colon cancer. It can improve the chance of surgical resection of advanced gastric cancer. It has certain curative effect on cylindrical adenocarcinoma of head and neck, bladder cancer cancer and lung adenocarcinoma. For primary liver cancer, the tumor can be reduced, intravenous injection of camptothecin emulsion can increase the chance of resection of liver cancer, and it is also effective for malignant hydatidiform mole and choriocarcinoma. Antitumor alkaloids. Irreversibly combine with DNA-topoisomerase I complex, inhibit the rebinding of DNA after topoisomerase I cleavage, and make the enzyme form covalent connection with DNA. A cytotoxic antitumor drug.

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