Planta Med 2011; 77 - P_62
DOI: 10.1055/s-0031-1273591

Novel Method using Multivariate Data Analysis to Identify Antiplatelet Compounds from Medicinal Plant Extract

J Ching 1, WL Soh 1, JF Lee 2, JYC Tan 1, J Yang 2, CH Tan 2, CW Yap 1, HL Koh 1
  • 1Department of Pharmacy, National University of Singapore, 18 Science Drive 4, Singapore 117543
  • 2Department of Pharmacology, Yong Loo Lin School of Medicine, National University of Singapore, 10 Medical Drive, Singapore 117597

Conventional methods of drug discovery from natural products include bioassay guided fractionation which is tedious and has low efficiency. The aim of this work is to develop a platform method to rapidly identify bioactive compounds from crude plant extracts and their partially purified fractions using multivariate data analysis (MVDA). Ardisia elliptica is traditionally used by Malays to relieve ailments such as pain in the region of the heart, parturition complications, fever, diarrhoea, liver poisoning etc. [1]. The plant was used as a model herb in this work. Soxhlet extraction and liquid-liquid fractionation were used to prepare different extracts and fractions from the leaves of A. elliptica. The extracts and fractions were analyzed using gas chromatography-mass spectrometry and their ability to inhibit platelet aggregation was investigated using a whole blood aggregometer.

Two MVDA methods, namely the Consensus method and the Correlation method, were developed and optimized to analyze the results. A list of compounds, including α- and β-amyrin, was identified to be potentially antiplatelet by the 2 MVDA methods. β-amyrin was subsequently isolated, purified and confirmed to possess antiplatelet effects by independent bioassays. It was previously reported to be more active than aspirin in inhibiting platelet aggregation [2]. This work demonstrates the feasibility of using MVDA to predict antiplatelet components from plant extracts without the need for bioassay guided fractionation. This platform method can be developed and optimized for other plant extracts and biological activities, thus reducing time and cost of drug discovery while improving efficiency.

Acknowledgements: The financial support from the Academic Research Fund R-148–000–079–112 (Koh HL), as well as a graduate research scholarship (Ching J) from the National University of Singapore is acknowledged.

References: [1] Herbal Medicine Research Centre (HMRC) and Institute for Medical Research (IMR) (2002) Compendium of medicinal plants used in Malaysia Volume 1. HMRC and IMR. Kuala Lumpur. [2] Ching J, Chua TK, et al. (2010) Indian J of Experimental Biol, 48: 275–279.