| Summary: | Background: The genus Calophyllum and its species has received great research interest for their phytochemical content and therapeutic potential. Said interest was sparked by the discovery of compounds with anti-HIV activities in one of its extracts and the genus has since been studied for potential in treating other morbidities. Generally, species under the genus contain various coumarins, xanthones, triterpenoids, steroids, and chromanones. Extracts with said bioactive compounds can be obtained from all plant parts. This review aims to elucidate the anti-cancer activities of Calophyllum extracts and their potential in cancer treatment. Results: Independent in-vitro studies of the extracts on various cell lines have revealed the chemotherapeutic potential of the genus as shown by their cytotoxic, anti-cancer, and antitumor-promoting activities. Leukemic cancer cell lines, the most studied cell lines, have been shown to be the most sensitive to perturbations by Calophyllum extracts and compounds. Conclusion: Calophyllumderived extracts and compounds have shown promising activities against cancer cell lines, particularly leukemic cancers. The presence of prenyl moiety at C-6 and the position of the hydroxy group and hydrophobic prenyl in the compounds have been attributed to their cytotoxicity. These findings are useful in providing leads in producing naturally derived anti-cancer medication and developing potent analogs for the same purpose. © 2019 ANGIOTHERAPY, a publication of Eman Research Ltd, Australia.
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