Key words meroterpenoid; marine sponge; antibacterial activity; DysideaMarine organisms such as sponges represent a largely unexploited source of a wide variety of natural meroterpenoids.1) Sponges of the genus Dysidea are a rich source of bioactive meroterpenoids, the majority of which are sesquiterpene quinones/quinols.2) This class of compounds frequently consist of sesquiterpene moieties linked to quinones, quinols, or structural analogues.3) The sesquiterpene unit is of biosynthetic interest, as it usually features a drimane-or a 4,9-friedodrimane-type skeleton comprising a trans-or a less common cis-fused ring junction.3) These compounds have attracted much interest due to their structural diversity and varied biological activities, including anti-human immunodeficiency virus (HIV), 4) antibacterial, 5) antifungal, 6) antioxidative, 7) antitumor, 8) anti-inflammatory, 9) inhibition against protein tyrosine kinase (PTK) and protein tyrosine phosphatase 1B (PTP1B), 10,11) and activation of hypoxia-inducible factor-1 (HIF-1) activities.
12)During our search for bioactive metabolites from tropical sponges, we encountered a purple-colored encrusting Dysidea sp. off the south China sea. The crude extract of this sponge showed significant antibacterial activity against Staphylococcus aureus (25923) with the minimum inhibitory concentration (MIC) value of 25 µg/mL. Chemical investigation of bioactive extracts of this sponge led to the isolation of three new sesquiterpene phenols (1−3) and one new sesquiterpene aminoquinone (4), together with four known sesquiterpene derivatives (5−8). Herein, we report the details of the purification and structure elucidation of these compounds, as well as the evaluation of antibacterial activity (Fig. 1).
Results and Discussion
Amphiphilic block copolymers-based mixed micelles established as new drug-loading system showed superior characteristics in delivering drug such as improved solubility, enhanced stability, multifunctional carrier materials, targeting ability, and high bioavailability. Recently, there are increasing focuses on exploration and study of noninvasive routes, and the results present perfect feasibility, improved compliance and fewer aches and pains. The aim to apply mixed micelles to noninvasive alternative routes has driven massive pharmaceutical attention. Recently, various studies of micelles strategy for noninvasive routes have been conducted to overcome the inherent barriers for uptake across the gastrointestinal tract, mucosal membranes and other in vivo noninvasive barriers, and the result argues well. The objective of this article is to summary these studies and developments of mixed micelles used on noninvasive drug delivery and provide a reference for further research.
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