Isolation, cytotoxic and alpha-glucosidase inhibitory activities of new coumarins from calophyllum incrassatum

• Main Authors: Aminudin, Nurul Iman, Ahmad, Farediah, Bakhtiar, M. Taher, Mohamed Zulkifli, Razauden
• Format: Conference or Workshop Item
• Language: English; English
• Published: 2018
• Subjects: RS192 Materia Medica-Pharmaceutical Technology
• Online Access: http://irep.iium.edu.my/57430/1/57430_Isolation%2C%20cytotoxic.pdf; http://irep.iium.edu.my/57430/7/69556.pdf; http://irep.iium.edu.my/57430/; http://www.icnp2018.usm.my/
• Institution: Universiti Islam Antarabangsa Malaysia

Calophyllum is a pan-tropical genus belongs to the Guttiferae family and known by Malay local folks as ‘bintangor’. There has been a continual interest to further investigate the phytochemicals of Calophyllum species since this genus is a rich source of active secondary metabolites such as coumarin, chromanone carboxylic acid and flavonoid which showed anti-HIV, cytotoxicity and antimicrobial properties. In this study, phytochemicals studies on the barks and leaves of Calophyllum incrassatum M.R. Henderson & Wyatt-Smith were carried out. Cold extraction method was employed by using dichloromethane, ethyl acetate and methanol to give the respective crude extracts. Four new 4-substituted coumarins, namely, incrassamarin A, B, C and D were successfully isolated from the dichloromethane extracts of the barks and leaves by size-exclusion recycling HPLC and column chromatography techniques. The structures of the compounds were elucidated by spectral analysis including NMR, IR, MS and X-ray crystallography. The compounds were tested for their cytotoxic activity towards human breast adenocarcinoma (MCF-7) and human non-small cell lung carcinoma (A-549) cell lines by MTT assay and α-glucosidase enzymatic inhibitory activity. Incrassamarin A displayed cytotoxic activity against A-549 cell lines with IC50 87.71 mg/ml and showed inhibition towards α-glucosidase enzymatic activity with IC50 93.25 mM.