Erectcyanthins A-C from marine sponge Hyrtios erectus: anti-dyslipidemic agents attenuate hydroxymethylglutaryl coenzyme A reductase.

Bioactivity-steered chromatographic purification of the solvent extract of marine sponge Hyrtios erectus (Thorectidae) led to the isolation of three undescribed cyanthiwigin-type diterpenoids, erectcyanthins A-C. Erectcyanthin B exhibited comparable attenuation activity against 3-hydroxy-3-methylglutaryl-coenzyme A reductase (IC50 0.07 mM) with that displayed by anti-dyslipidemic agent atorvastatin (IC50 0.08 mM). Comparatively greater antioxidant properties of erectcyanthin B (IC50 ∼ 0.4 mM) than that displayed by erectcyanthin A (IC50 ∼ 0.5 mM), erectcyanthin C and the standard α-tocopherol (IC50 1.5-1.7 mM) against oxidants also corroborated its promising bioactivity. Erectcyanthin B exhibited considerably greater anti-inflammatory activities (IC50 0.88-1.09 mM) than other erectcyanthin analogues in the series. The potential anti-dyslipidemic activity of erectcyanthins was linearly correlated with electronic parameter (topological polar surface area ∼ 74.6) along with balanced hydrophilic-lipophilic properties (logarithmic octanol-water partition coefficient 1.76). This study recognized the anti-dyslipidemic property of erectcyanthin B as a promising pharmaceutical lead.

Citation

Kajal Chakraborty, Prima Francis. Erectcyanthins A-C from marine sponge Hyrtios erectus: anti-dyslipidemic agents attenuate hydroxymethylglutaryl coenzyme A reductase. Natural product research. 2021 Dec 09:1-12

PMID: 34879770

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