Abstract

The in vitro antitumour-promoting, cytotoxic, and antioxidant activities of two ester derivatives of garcinia acid, that is, 2-(butoxycarbonylmethyl)-3-butoxycarbonyl-2-hydroxy-3-propanolide (1) and 1′,1′′-dibutyl methyl hydroxycitrate (2), that had been previously isolated from the fruits of Garcinia atroviridis Griff. ex T. Anders (Guttiferae), were examined. Based on the inhibition of Epstein-Barr virus early antigen (EBV-EA) activation, compound 1 (IC50: 70 μM) showed much higher (8-fold) antitumour-promoting activity than compound 2 (IC50: 560 μM). In addition, both compounds were nontoxic towards CEM-SS (human T-lymphoblastic leukemia) cells (CD50: >100 μM), Raji (human B-lymphoblastoid) cells (CD50: >600 μM), and brine shrimp (LD50: >300 μM). Although the antitumour-promoting activity of compound 1 is moderate compared with the known antitumour promoter genistein, its non-toxicity suggests the potential of compound 1 and related structures as chemopreventive agents. The weak antioxidant activity displayed by both compounds also suggested that the primary antitumour-promoting mechanism of compound 1 did not involve oxidative-stress quenching.

Highlights

  • IntroductionAnders (Guttiferae) is a medium-sized fruit tree endemic to Peninsular Malaysia

  • The in vitro antitumour-promoting, cytotoxic, and antioxidant activities of two ester derivatives of garcinia acid, that is, 2(butoxycarbonylmethyl)-3-butoxycarbonyl-2-hydroxy-3-propanolide (1) and 1,1 -dibutyl methyl hydroxycitrate (2), that had been previously isolated from the fruits of Garcinia atroviridis Griff. ex T

  • In the antitumour-promoting assay, compound 1, a βlactone, strongly inhibited (IC50: 70 μM) Epstein-Barr virus (EBV) activation compared with compound 2 (IC50: 560 μM)

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Summary

Introduction

Anders (Guttiferae) is a medium-sized fruit tree endemic to Peninsular Malaysia. This species grows wild throughout Peninsular Malaysia but is widely cultivated especially in the northern states owing to its economic and medicinal values. G. atroviridis is used as a post-partum medication and to treat earache, throat irritation, cough, dandruff, and stomach pains associated with pregnancy. Sun-dried slices of the fruits are commercially available and are popularly used as a seasoning in curries, sour relish and for dressing fish. The young leaves are used for culinary purposes and as a traditional vegetable [1]

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