Anti-proliferative Effects of a Coumarin Benjaminin on Four Human Cancer Cell Lines

Abstract

Cancer is a major health issue around the globe. Chemotherapy and radiation therapy are no longer the standard treatments for patients as these remedies lead to many adverse effects. Thus, the development of alternative effective drugs from lead compounds, especially natural products is necessary. This study aimed to isolate cytotoxic phytochemical constituents from a plant Calophyllum inophyllum, which has been used as traditional medicine since ancient time. The root of C. inophyllum was extracted and subjected for phytochemical constituent isolation. A coumarin, benjaminin (1) was isolated successfully from the chloroform extract and its structural elucidation was performed by spectroscopy analyses of MS, IR and NMR. The anti-proliferative effect of 1 on four cancer cell lines, leukemia (K562), stomach (SNU-1), liver (Hep-G2) and lung (NCI-H23) cancers were evaluated by using colorimetric MTT assay. Benjaminin (1) exhibited cytotoxic effects towards all cancer cells and showed the strongest inhibition towards SNU-1 cell proliferation with an IC 50 value of 70.42 μM. The outcome of this study revealed that 1 is a potential cytotoxic lead compound that could be further developed into anti-cancer drug. Thus, the study on the structure-activity relationship of 1 is highly recommended in due course to improve its anti-proliferative effects on cancer cells.

A review of the effects of Calophyllum spp. on cancer cells

“…Structural analyses found a link between presence of prenyl moiety in C-6 of the compounds and their anti-proliferative activity. This is seen where compounds of an extract that has a prenyl moiety located at C-6 has significantly higher cytotoxic activities compared to other compounds of the same extract where prenyl moiety is absent or located differently (Mah et al 2020;Haerani, Raksat & Pudhom 2021;Itoigawa et al 2001). Furthermore, in the context of antitumor-promoting effect, other than the presence of prenyl moiety in the molecule, the relative position of hydroxy group and hydrophobic prenyl moiety in the compound is also seen to influence the compound activity (Ito et al 2002).…”