Continued research and development of natural small molecule anti-cancer! Inventory of anti-tumor natural product molecules

Since the 1940s, human beings began to use small molecule drugs to treat tumors Alkylating agents, fluorouracil, methotrexate, cyclophosphamide and a series of other drugs have been put on the market one after another However, most of these molecules have large side effects Since the 1950s, researchers in many countries and regions, including the United States, began to focus on natural small components Anti cancer For example, in 1960, NCI commissioned US Department of agriculture (USDA) botanists to provide 1000 plants to the national cancer chemotherapy service (ccnsc) for screening of anticancer drugs Over the years of efforts, natural products have made great progress in anti-cancer, many natural small molecules have been successfully listed, and become the star treatment drugs in the corresponding fields Next, I'd like to take you to check the natural anti-tumor product molecules 1、 Paclitaxel: the first tubulin inhibitor At first, researchers found toxic components of white alkaloids in the branches and leaves of Taxus chinensis (pig) Rehd But the specific substances were unknown Later, Barclay, a US researcher, specially extracted Taxus samples for activity screening and found that they had significant antitumor activity Activity; further extraction research, the researchers found the most active white crystal monomer in the extract, and named it taxol Since then, paclitaxel has been found to have tubulin inhibition, which is also the first tubulin inhibitor discovered by humans In 1984, FDA approved the clinical trial of paclitaxel, which was officially approved in 1992; China also approved the listing of new paclitaxel drugs in 1995, which is the second country to be approved At present, paclitaxel has been recognized as a broad-spectrum anti-tumor drug in the world, and further drug development of paclitaxel has not stopped For example, in 2004, the FDA approved the listing of docetaxel, a derivative of paclitaxel 2、 Camptothecin: camptothecin from Davidia family is isolated from Camptotheca acuminata, which has significant antitumor effect Because camptothecin is different from common chemotherapy drugs, the activity of topoisomerase I has aroused great interest of researchers Since the 1960s, many drug researchers including Chinese researchers have developed camptothecin and its derivatives For example, hydroxycamptothecin has higher activity and lower toxicity than camptothecin in Shanghai Institute of pharmaceutical research, Chinese Academy of Sciences, and obtained new drug approval number in 1986, which is also the first camptothecin derivative independently researched and developed in China; in addition, FDA has approved camptothecin derivative topotecan and irinotecan to be listed in succession, so as to make camptothecin anti-tumor We have made great contributions to the development of our country 3、 Homoharringtonine: still effective in imatinib resistant population There is a long history of cancer treatment by Cephalotaxus fortunei, a plant of Cephalotaxus in China Follow-up studies have shown that cephalotaxine, homoharringtonine, ISOHARRINGTONINE, deoxyharringtonine and pseudodeoxyharringtonine, which are the chemical components of cephalotaxine, have a significant inhibitory effect on leukemia As early as 1990, homoharringtonine was listed in the Pharmacopoeia as an anticancer drug in China In 2012, FDA also accelerated the approval of homoharringtonine for leukemia treatment In particular, homoharringtonine is still effective for imatinib resistant population, so homoharringtonine has gained great attention and success 4、 Ginsenoside Rg3: a new anti-tumor drug, Ginsenoside Rg3, which was independently developed in China, is a kind of damatane type tetracyclic triterpenoid saponin Its chemical structure was determined in 1983, and then it was proved to have anti-tumor effect Dalian Fusheng Pharmaceutical Co., Ltd., a Chinese pharmaceutical company, obtained the new drug certificate in 2000 It is a kind of new anti-tumor drug developed by our country, and has obtained many patents in the world It is also one of the representative anti-tumor drugs of natural products 5、 Vinblastine, colchicine, vinblastine and vincristine were isolated from Catharanthus roseus, which has been proved to have significant antitumor effect Lilly has invested a lot of energy in this field Through clinical trials, it was approved by FDA in 1963 It's also a classic drug in the history of anti-cancer In addition, colchicine is also an anti-cancer drug In addition to the field of tumor, it has also entered the clinical application in the field of fibrosis and inflammation In addition to the drugs mentioned above, podophyllotoxin, stephanide, indirubin, berbamine, nongjililine, anethole and gossypol are all the natural product molecules that have been listed and play an important role in their respective fields Moreover, in recent years, with the promotion of many policies such as the modernization of traditional Chinese medicine, as well as the further deepening of the recognition and emphasis on natural products in the pharmaceutical research and development community, many new opportunities have been brought to the development of natural anti-tumor molecules, such as chlorogenic acid, magnolol and other natural product components have also begun to emerge in the field of anti-cancer We can be sure that in the future, natural drugs will be in the field of anti-tumor The field plays a greater role.