Untitled Document

Records of Natural Products

Year: 2014 Volume: 8 Issue: 1

SHORT REPORT

Antitubercular and Cytotoxic Constituents from Goniothalamus gitingensis

Allan Patrick G. Macabeo, Amier Dayle A. Lopez, Sebastian Schmidt, Jörg Heilmann, Hans-Martin Dahse, Grecebio Jonathan D. Alejandro and Scott G. Franzblau

Phytochemsitry and Organic Synthesis Laboratory, Research Center for the Natural and Applied Sciences, University of Santo Tomas, Espana St., 1015 Manila, Philippines

Institut für Pharmazeutische Biologie, Fakultät Pharmazie und Chemie, Universität Regensburg, Universitätsstr. 31, D-93053 Regensburg, Germany

Leibniz-Institute for Natural Product Research and Infection Biology, Hans-Knöll-Institute (HKI), Beutenbergstraße 11a, D-07745 Jena, Germany

Plant Sciences Laboratory, Research Center for the Natural and Applied Sciences, University of Santo Tomas, Espana St., 1015 Manila, Philippines

Institute for Tuberculosis Research, College of Pharmacy, University of Illinois at Chicago, 833 South Wood St., Chicago, Illinois, 60612 USA

Abstract: Phytochemical studies on the leaves of the Philippine endemic Annonaceae plant, Goniothalamus gitingensis enabled the isolation and identification of four secondary metabolites corresponding to three styryllactones, isoaltholactone (1), altholactone (2) and goniopypyrone (3), and the alkaloid liriodenine (4). Structure identification was facilitated through various spectroscopic experiments such as NMR ( 1H, 13C, COSY, HSQC, HMBC and NOESY), LR-EIMS, X-ray and through comparison with literature values. Our study accounts the first report of all compounds in this plant species. The extracts together with the isolated compounds (1-4) were tested for antituberculosis activity using MABA and cytotoxic activity using the CellTiter-Blue1 assay. The majority of the samples tested indicated good inhibitory activity against Mycobacterium tuberculosis H 37Rv (MIC up to 16 m g/mL). Liriodenine (4) showed the most excellent antimycobacterial activity (MIC=16 m g/mL) followed by 1 and the 5:4 mixture of 1 and 2. Their cytotoxicity against three human cancer cell lines, human umbilical vein endothelial cell line (HUVEC), human leukemia cell line (K-562) and HeLa cells were also assessed. The crude extract, alkaloid extract, petroleum ether sub-extract and EtOAc sub-extract showed moderate cytotoxicity against the cancer cell-lines. In addition, the results showed that compounds 1, 4 and the mixture of 1 and 2 exhibited highest cytotoxicity against HUVEC, K-562 and HeLa cell lines with GI 50 values up to 4 μg/mL (vs. HUVEC and/or K-562) and CC 50 values up to 25.1 μg/mL (vs. HeLa).