Planta Medica Letters 2016; 3(01): e10-e13
DOI: 10.1055/s-0035-1568332
Letter
Georg Thieme Verlag KG Stuttgart · New York

Structural Derivatization of Clusianone and In Vitro Cytotoxicity Evaluation Targeting Respiratory Carcinoma Cells

Sree Vaneesa Nagalingam
Centre for Natural and Medicinal Product Research, School of Pharmacy, Faculty of Science, University of Nottingham Malaysia Campus, Semenyih, Selangor, Malaysia
,
Kok Wai-Ling
Centre for Natural and Medicinal Product Research, School of Pharmacy, Faculty of Science, University of Nottingham Malaysia Campus, Semenyih, Selangor, Malaysia
,
Khoo Teng-Jin
Centre for Natural and Medicinal Product Research, School of Pharmacy, Faculty of Science, University of Nottingham Malaysia Campus, Semenyih, Selangor, Malaysia
› Author Affiliations
Further Information

Publication History

received 29 July 2015
revised 19 November 2015

accepted 18 December 2015

Publication Date:
11 February 2016 (online)

Abstract

Clusianone (1) was isolated from Garcinia parvifolia and structurally modified using semisynthetic methods to obtain compounds 24. The structural derivatization included methylation (2), hydrogenation (3), and the addition of a methylamine group [(4) to (1)]. Cytotoxic effects of these compounds were assessed on MRC5 fibroblasts, A549 lung adenocarcinoma, HK1 squamous nasopharynx carcinoma, and NP69 normal nasopharyngeal epithelial cell lines. Clusianone (1) showed cytotoxic activity against A549 cells with an IC50 value of 3.06 µM. Compound (4) showed cytotoxic activities against both A549 and HK1 cells with IC50 values of 4.09 µM and 3.43 µM, respectively. The results of the cytotoxicity assay provide a correlation on the structure activity relationship of clusianone against HK1 and A549 cells, which can be further investigated as a potential antiproliferative compound.

Supporting Information