| Camptothecin  Chemical Name:
4(S)-Ethyl-4-hydroxy-1H-pyrano-[3',4':6,7]indolizino[1,2-b]quinoline-3,14
(4H,12H)-dione (1) Molecular Formula: C20H16N2O4 (2) Molecular Weight: 348.36 (3) Melting Point: 259~263¡æ (4) Compared to curls: +31~32o (5) Contents(HPLC): ¡Ý98% (6) Loss of drying: ¡Ü0.5% (7) Sulphated ash: ¡Ü0.1% (8) Heavy Metal: ¡Ü10ppm (9) As: ¡Ü2ppm (10) Total plate count: ¡Ü1000cfu/g (11) E.Coli: NEG (11) Salmosella: NEG 2. Chemical and Physical Index It is light yellow powder or light yellow crystalline powder. It is easy to deteriorate when it meets light. It is east to be moistened. It owns the nature of indirect in the solution of Chloroform and Methanol(8: 2).It slightly dissolve in Ethanol and Chloroform etc. It is hardly dissolve in water and easy dissolve in sparse alkaline solution. 3. Function and Purpose 1) It mainly been applied for cancer of Digestive System, for example cancers of the stomach, gullet, cardia, intestines and liver cancer etc. 2) It is also used in cancers of oral cavity, nake, face and head, bladder cancer and lung cancer etc. 4. Usage: Pharmaceuticals Intermediates. 5. Storage: Kept away from light 6. Descripting: Camptothecin is a quinoline-based alkaloid found in the barks of the chinese camptotheca tree and the Asian nothapodytes tree. Camptotheca acuminate as the fruit and root of the Chinese dove tree with cold nature and bitter flavor. In "Chinese herds" which is described as "cancer-curable, calculus exploded, curing the cancer in stomach, rectum and cystic, also has the good effects for chronic granulocytic leukemia. The whole Chinese dove tree contains the alkaloid-Camptothecin.Anti-cancer is the major pharmacodynamic effect. The anti-cancer presented is ¦Á-hydroxyl-lactone ring. In the human-mouse test of l-165 reticulum cell sarcoma ars abdominal dropsy and viral leukemia, camptothecin may reduce the number of white blood cells, ease the splenomegaly, reduce abdominal dropsy and the number of the active tumor cells in which. Camptothecin (CPT) is a monoterpenoid indole alkaloid originally isolated from Camptotheca acuminata Decne, a deciduous tree native to south China. Irinotecan (CPT-11) and topotecan (TPT), two water-soluble derivatives of CPT, have gained approval by the Food and Drug Administration of the United States of America (FDA) for treating colorectal and ovarian cancer. Other camptothecins--such as 9-aminocamptothecin (9AC), 9-nitrocamptothecin (9NC), and 7-(4-methyl piperazino-methylene)-10,11-ethylenedioxycamptothecin (GG211)--have also showed remarkable potential in the treatment of carcinoma. Camptothecins are lauded as one of the most promising anticancer drugs of the twenty-first century. Camptothecin and derivative of camptothecin are known as inhibitors,that of nucleat topoisomerase I by binding to and trapping the topoisomerase-DNA covalent complex,so cancer cells are killed. Camptothecin is a potent broad spectrum antitumor agent which is of interest due to a variety of camptothecin derivatives currently being used in a variety of clinical protocols. Camptothecin functions by effectively converting DNA topoisomerase I into a DNA damaging poison, causing it to irreversibly bind DNA midway through its catalytic action, leading to a double-stranded break when encountered by a replication fork. We have found that cells containing a mutant histone H4 compromised for N-terminal acetylation become hypersensitive to killing by camptothecin. Camptothecin and its derivatives are active against carcinomas of the
stomach, colon, head, neck and bladder. Camptothecin and derivative of
camptothecin exhibited remarkable antitumour and antileukaemia
activity,its are in clinical trials to treat breast and coloncancers,small-cell
lung cancer and leukemia etc.though camptothecin is limited because of
serious side effects and poor water-solubity in clinic,either
semi-synthetic or synthetic camptothecin drug(such as FDA approved
irinptecan and topotecan)are satisfactory in curative effects.
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