Cepharanthine

Cepharanthine is diclofenac quinoline alkaloid isolated from rhizome of Stephania japonica, which was first recorded in “Bencao shiyi” and functions as clearing heat, promoting diuresis and detumescence in traditional Chinese medicine. Cepharanthine is a pure and natural extract of the Stephania cepharantha Hayata plant, a rare species that is native to Kotosho Island, southeast of Taiwan. In 1914, the renowned botanist, Bunzo Hayata reported the plant for the first time. Two decades later, Dr. Heisaburo Kondo purified its active ingredient and named it “Cepharanthine.” Stephania japonica was used to treat tuberculosis and other consumptive diseases which provided a clue for its development on lung disease.

Appearance: light yellow or yellow powder. Solubility: soluble in acidic aqueous solution and ether, acetone, and other organic solvents; insoluble in petroleum ether. Melting point: 148–150?°C. Specific optical rotation: +277°.

Promoting leukocytosis of cepharanthine in tuberculosis patients was first recorded in the proceeding Institute of Chemotherapy by the Japanese scholar Yamaguchi in 1946. In 1948, Chinese scholar Yuhuang Zhao also received this compound and published it in D.M.?Med.
It is thought that cepharanthine may stimulate the reticuloendothelial system, then activate hematopoietic tissue, and promote myeloproliferation. Therefore, the number of white blood cells in the peripheral blood increased significantly. Due to its good safety, cepharanthine is currently widely used in cancer patients with granulocytopenia or leukopenia embolism after radiotherapy and chemotherapy and so on.
In addition, Chinese scientists extracted five kinds of dibenzylisoquinoline alkaloids from Chinese herbal medicine in 1977, which could significantly improve the silicosis symptoms in rat . In 1993, it was issued as anti-pneumoconiosis drug by CFDA and is used for delaying the progress of pneumoconiosis in clinic.

Cepharanthine is a biscoclaurine alkaloid that has antiinflammatory, antineoplastic, hepatoprotectant, radiopropective and other biological functions. It is used to treat many acute and chronic diseases, including pit viper bites, alopecia areata, and leucopenia in radiation therapy.

ChEBI: Cepharanthine is a bisbenzylisoquinoline alkaloid from tubers of Stephania; stimulates recovery of immunologic function in lymphatic system after administration of antineoplastic agents or x-irradiation. It is a member of isoquinolines and a bisbenzylisoquinoline alkaloid.

The pharmacological effects of cepharanthine are very broad, mainly for the promotion of leukocytosis, antitumor, anti-inflammation, improvement of the body immunity, and other aspects of efficacy. Improvement of leukocytosis is the most widely studied among them, and the mechanism may be to stimulate the reticular endothelium system, activate hematopoietic tissue, and promote bone marrow hyperplasia .
Cepharanthine is also a good antitumor drug sensitizer. It can significantly improve their efficacy and reduce their side effects when combined with other antitumor drugs, as manifested by increasing the concentration of FT-207 metabolite (5-Fu) in tumor tissue under cepharanthine and FT-207 combination therapy, which was significantly higher than that in blood , suggesting that cepharanthine has the potential to improve the efficacy of antitumor drugs.

The major clinical application of cepharanthine is to improve their immunity impaired by chemotherapy or radiotherapy in tumor patients. In addition, cepharanthine can increase the sensitivity to antitumor drugs, and itself also has a certain antitumor effect. Now, it is commonly used as adjuvant drug for anticancer treatment.