Anti-cancer potential of sophoridine and its derivatives: Recent progress and future perspectives

• Published in: Bioorganic chemistry 2020-06, Vol.99, p.103863-103863, Article 103863
• Main Authors: ur Rashid, Haroon, Rasool, Shagufta, Ali, Yousaf, Khan, Kamin, Martines, Marco Antonio Utrera
• Format: Article
• Language: English
• Subjects: Alkaloid; Alkaloids - chemical synthesis; Alkaloids - chemistry; Alkaloids - pharmacology; Animals; Antineoplastic Agents - chemical synthesis; Antineoplastic Agents - chemistry; Antineoplastic Agents - pharmacology; Cancer; Cell Proliferation - drug effects; Drug Screening Assays, Antitumor; Humans; Molecular Structure; Phytochemical; Quinolizines - chemical synthesis; Quinolizines - chemistry; Quinolizines - pharmacology; Sophoridine; Topoisomerase I
• ISSN: 0045-2068; 1090-2120
• DOI: 10.1016/j.bioorg.2020.103863

[Display omitted] •Cancer-related deaths are expected to increase to 11.5 million by 2030.•Sophoridine (C15H24N2O) is an alkaloid found in plants of Sophora genus.•Sophoridine and its derivatives exhibit significant anticancer activities.•Chinese Food and Drug Administration has recommended sophoridine for cancer treatment.•Sophoridine can synergistically enhance the efficacy of chemotherapy in combination with other anticancer drugs. Cancer is the second leading cause of mortality and has resulted in about 9.6 million deaths around the world in 2018. Cancer-caused deaths are expected to be 11.5 million by 2030 all over the world. Because of the fatal nature of cancer, substantial efforts are made all over the world to combat it. Phytoconstituents such as certain alkaloids, saponins, tannins, polyphenols, and terpenoids exhibit anticancer effects. Sophoridine is a tetracyclic quinolizidine alkaloid isolated from the stem and leaves of medicinal plants Sophora alopecuroides L., and Euchresta japonica Benth, and roots of Sophora alopecuroides Ait. Chinese Food and Drug Administration (CFDA) approved sophoridine as an antitumor agent in 2005. This review covers the antitumor activities of sophoridine and its derivatives. The efficacy of sophoridine analogs is expressed with respect to their half-maximal inhibitory concentration (IC50 values). Structure-activity relationship (SAR) study for most of the sophoridine derivatives has been explained. Moreover, the current market of anticancer drugs and its expected growth are discussed. Prospects provide suggestions and clues for novel sophoridine-based anticancer agents with enhanced expected efficacy and minimum toxicity.