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| Product name | Camptothecin (CPT) 99% |
| Botanical Name | Camptotheca acuminata Decne. |
| CAS Number | 7689-03-4 |
| Molecular Formula | C20H16N2O4 |
| Synonyms | Camptotheca acuminata Decne,cancer tree, tree of life, |
| Appearance | Pale yellow crystalline powder |
| Part used | Bark, stem and leaves |
| Specification | Camptothecin 99% HPLC |
| Dosage | 10mg |
| Main benefits | Potent DNA topoisomerase I inhibitor; An anticancer agent |
| Applied industries | pharmaceuticals, APIs, drugs |
What is Camptothecin?
Discovered in 1966 by M. E. Wall and M. C. Wani in systematic screening of natural products for anticancer drug, as one kind of alkaloids, Camptothecin is derived from the bark, stem and leaves of the Chinese Happy tree Camptotheca acuminata Decne, which is native to China.
C. acuminata also goes by the names cancer tree and tree of life. These names are appropriate considering the anticancer properties of camptothecin. The Chinese have used C. acuminata in traditional medicine for thousands of years. It was commonly prescribed for psoriasis, leukemia and liver, gallbladder, spleen and stomach disease.
Also modern research has shown camptothecin and its derivatives are unique in their ability to inhibit DNA Topoisomerase I, by stabilizing a covalent reaction intermediate termed the cleavable complex which ultimately causes tumor cell death.
Camptothecin and nuclear topoisomerase I
Nuclear DNA topoisomerase I (TOP1) is an essential human enzyme. It is the only known target of the camptothecin, from which the potent anticancer agent irinotecan and topotecan are derived. As camptothecins bind at the interface of the TOP1-DNA complex, they represent a paradigm for interfacial inhibitors that reversibly trap macromolecular complexes.
In Fig 1, normally, topoisomerases I introduces a nick in the DNA backbone allowing the rotation of one strand around another. This releases the torsional strain which otherwise accumulates in front of the advancing replication fork (the large arrow). The DNA break is extremely transient and is religated as it release the other strand.
In Fig 2, when camptothecin is present (black oval with C), it binds to the topoisomerase I-nicked DNA complex. This prevents the religation of the nicked strand and the release of the enzyme. Eventually, the replication fork collides with the complex, causing the formation of a double-strand break.
How Camptothecin Works
Camptothecin was originally isolated from the stem wood of the Camptotheca acuminata tree and was shown to exhibit antileukemic/antitumour activity, and reversibly inhibit Mitochondrial Topo I (nuclear Topo I (topoisomerase I)) by binding to and stabilizing the topoisomerase-DNA covalent complex. Advancing replication forks are believed to interact with these complexes leading to double strand breaks, which is thought to be responsible for much of the cytotoxicity; other research has shown that some of the antitumor activity could be derived from the inhibition of NOS2 (iNOS or inducible nitric oxide synthase) which generates nitric oxide, an important regulator of angiogenesis and other biochemical pathways. The discovery of Camptothecin spurred the development of many derivatives with superior activity and solubility, including Irinotecan (sc-202186) and Topotecan (sc-204919).
What are the Benefits of taking Camptothecin?
Camptothecin Anti-cancer
Several camptothecin and non-camptothecin derivatives are being developed to further increase anti-tumour activity and reduce side effects. The mechanisms and molecular determinants of tumour response to TOP1 inhibitors are reviewed, and rational combinations of TOP1 inhibitors with other drugs are considered based on current knowledge of repair and checkpoint pathways that are associated with TOP1-mediated DNA damage.
Side effects of taking Camptothecin
If dosage is upper 100mg, it may cause inappetence, nausea, emesis, gastroenteritis;
Inhibits bone marrow, Also can cause hemorrhagic cystitis.
Dosages of taking Camptothecin
10mg, dissolved in normal saline 20ml, intravenous injection, 1 time per day.