Camptotheca acuminata is native to southern China and Tibet, where it is popularly called xi shu, which means "happy tree." Preparations made from camptotheca have been used in China as a cancer treatment, especially for cancers of the stomach and liver and leukemia.185 The National Cancer Institute evaluated camptotheca in 1958 and confirmed its anticancer properties. A quinoline alkaloid, camptothecin, was isolated in 1966, and it was found to be responsible for the anticancer activity. Studies aimed at its mode of action revealed that camptothecin inhibited DNA replication by inhibiting topoisomerase I, an enzyme that mediates the winding/unwinding action of DNA strands during cell proliferation. The first human studies were conducted using sodium salt of camptothecin, but they were abandoned later due to severe side effects. Further studies revealed that the sodium salt was several times less potent than camptothecin, yet the salt was responsible for all the toxicity. Camptothecin was chemically modified to generate an array of potent anticancer drugs, such as 9-aminocamptothecan, CPT-11, irinotecan, and topotecan. Topotecan (Hycamtin®) and irinotecan HCl (Camptosar®) are the only compounds approved by the FDA for treatment against ovarian cancer and metastatic colorectal cancers, respectively.

Without the effort of scientists who believed in the efficacy of traditional systems of natural medicine, the second-most-important source of anticancer drugs would never have been known in modern allopathic medicine.

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