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Noncytotoxic and Antitumour-Promoting Activities of Garcinia Acid Esters from Garcinia atroviridis Griff. ex T. Anders (Guttiferae).

Mackeen MM, Mooi LY, Amran M, Mat N, Lajis NH, Ali AM - Evid Based Complement Alternat Med (2012)

Bottom Line: Anders (Guttiferae), were examined.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.

View Article: PubMed Central - PubMed

Affiliation: Department of Cell and Molecular Biology, Faculty of Biotechnology and Biomolecular Sciences, Universiti Putra Malaysia, Selangor, 43400 Serdang, Malaysia.

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 (IC(50): 70 μM) showed much higher (8-fold) antitumour-promoting activity than compound 2 (IC(50): 560 μM). In addition, both compounds were nontoxic towards CEM-SS (human T-lymphoblastic leukemia) cells (CD(50): >100 μM), Raji (human B-lymphoblastoid) cells (CD(50): >600 μM), and brine shrimp (LD(50): >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.

No MeSH data available.


Related in: MedlinePlus

Antioxidant activities of compounds 1 and 2. (a) FTC assay (i) absorbance at 500 nm, (ii) ratios of antioxidant values normalized to α-tocopherol. (b) TBA assay (i) absorbance at 532 nm, (ii) ratios of antioxidant values normalized to α-tocopherol. (c) DPPH assay. The sample test concentrations in (a) to (c) are 0.6 mM, 0.2 mM, and 0.3 mM, respectively. Assays were carried out in triplicate and averaged (±0.1 absorbance units).
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fig2: Antioxidant activities of compounds 1 and 2. (a) FTC assay (i) absorbance at 500 nm, (ii) ratios of antioxidant values normalized to α-tocopherol. (b) TBA assay (i) absorbance at 532 nm, (ii) ratios of antioxidant values normalized to α-tocopherol. (c) DPPH assay. The sample test concentrations in (a) to (c) are 0.6 mM, 0.2 mM, and 0.3 mM, respectively. Assays were carried out in triplicate and averaged (±0.1 absorbance units).

Mentions: The antioxidant assays performed on both compounds showed weak activity that was slightly higher than the control. Compounds 2 and 1, respectively, reduced oxidant activity by 36 and 11% in the FTC assay (Figure 2(a)), 53 and 37% in the TBA assay (Figure 2(b)), and 5.5 and 3.4% in the DPPH assay (Figure 2(c)) but were weaker than the positive control(s) especially in the radical scavenging assay. It appeared that both these compounds were more effective inhibitors against late-stage oxidation as evidenced by the stronger antioxidant activity in the TBA assay than the FTC assay. The low antioxidant activity of both compounds ruled out the influence of oxidative-stress quenching as the dominant mechanism of action responsible for the antitumour-promoting activity of the β-lactone, although this mechanism is closely associated with antitumour-promoting activity [18]. This was further confirmed by the recurring trend of 2 showing higher activity than 1 in all the antioxidant assays whereas stronger antitumour-promoting activity was displayed by 1 than 2.


Noncytotoxic and Antitumour-Promoting Activities of Garcinia Acid Esters from Garcinia atroviridis Griff. ex T. Anders (Guttiferae).

Mackeen MM, Mooi LY, Amran M, Mat N, Lajis NH, Ali AM - Evid Based Complement Alternat Med (2012)

Antioxidant activities of compounds 1 and 2. (a) FTC assay (i) absorbance at 500 nm, (ii) ratios of antioxidant values normalized to α-tocopherol. (b) TBA assay (i) absorbance at 532 nm, (ii) ratios of antioxidant values normalized to α-tocopherol. (c) DPPH assay. The sample test concentrations in (a) to (c) are 0.6 mM, 0.2 mM, and 0.3 mM, respectively. Assays were carried out in triplicate and averaged (±0.1 absorbance units).
© Copyright Policy - open-access
Related In: Results  -  Collection

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getmorefigures.php?uid=PMC3368197&req=5

fig2: Antioxidant activities of compounds 1 and 2. (a) FTC assay (i) absorbance at 500 nm, (ii) ratios of antioxidant values normalized to α-tocopherol. (b) TBA assay (i) absorbance at 532 nm, (ii) ratios of antioxidant values normalized to α-tocopherol. (c) DPPH assay. The sample test concentrations in (a) to (c) are 0.6 mM, 0.2 mM, and 0.3 mM, respectively. Assays were carried out in triplicate and averaged (±0.1 absorbance units).
Mentions: The antioxidant assays performed on both compounds showed weak activity that was slightly higher than the control. Compounds 2 and 1, respectively, reduced oxidant activity by 36 and 11% in the FTC assay (Figure 2(a)), 53 and 37% in the TBA assay (Figure 2(b)), and 5.5 and 3.4% in the DPPH assay (Figure 2(c)) but were weaker than the positive control(s) especially in the radical scavenging assay. It appeared that both these compounds were more effective inhibitors against late-stage oxidation as evidenced by the stronger antioxidant activity in the TBA assay than the FTC assay. The low antioxidant activity of both compounds ruled out the influence of oxidative-stress quenching as the dominant mechanism of action responsible for the antitumour-promoting activity of the β-lactone, although this mechanism is closely associated with antitumour-promoting activity [18]. This was further confirmed by the recurring trend of 2 showing higher activity than 1 in all the antioxidant assays whereas stronger antitumour-promoting activity was displayed by 1 than 2.

Bottom Line: Anders (Guttiferae), were examined.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.

View Article: PubMed Central - PubMed

Affiliation: Department of Cell and Molecular Biology, Faculty of Biotechnology and Biomolecular Sciences, Universiti Putra Malaysia, Selangor, 43400 Serdang, Malaysia.

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 (IC(50): 70 μM) showed much higher (8-fold) antitumour-promoting activity than compound 2 (IC(50): 560 μM). In addition, both compounds were nontoxic towards CEM-SS (human T-lymphoblastic leukemia) cells (CD(50): >100 μM), Raji (human B-lymphoblastoid) cells (CD(50): >600 μM), and brine shrimp (LD(50): >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.

No MeSH data available.


Related in: MedlinePlus