Abstract

Benthic diatoms of the genus Cocconeis contain a specific apoptogenic activity. It triggers a fast destruction of the androgenic gland in the early post-larval life of the marine shrimp Hippolyte inermis, leading to the generation of small females. Previous in vitro investigations demonstrated that crude extracts of these diatoms specifically activate a dose-dependent apoptotic process in human cancer cells (BT20 breast carcinoma) but not in human normal lymphocytes. Here, a bioassay-guided fractionation has been performed to detect the apoptogenic compound(s). Various HPLC separation systems were needed to isolate the active fractions, since the apoptogenic metabolite is highly active, present in low amounts and is masked by abundant but non-active cellular compounds. The activity is due to at least two compounds characterized by different polarities, a hydrophilic and a lipophilic fraction. We purified the lipophilic fraction, which led to the characterization of an active sub-fraction containing a highly lipophilic compound, whose molecular structure has not yet been identified, but is under investigation. The results point to the possible medical uses of the active compound. Once the molecular structure has been identified, the study and modulation of apoptotic processes in various types of cells will be possible.

Highlights

  • A variety of natural compounds with medical applications have been found in marine macro-algae [1,2], whereas the study of secondary metabolites from micro-algae and their biotechnological applications remains in its infancy [3,4]

  • We report here the results of six years of bioassay-guided investigations, leading to the purification and characterisation of the active fraction produced by diatoms collected in Ischia (Italy; Figure 1c)

  • Freeze-dried biomasses of C. scutellum parva were extracted with 80% aqueous ACN, and all the activity was found in the extract

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Summary

Introduction

A variety of natural compounds with medical applications have been found in marine macro-algae [1,2], whereas the study of secondary metabolites from micro-algae and their biotechnological applications remains in its infancy [3,4]. Chemical ecology investigations may help find compounds with defined bioactivity [5,6] present in various diatoms, in particular those derived from the oxylipin pathway [7,8,9]. These studies are mostly related to planktonic organisms, often aimed at determining possible effects of diatoms on human health [10,11]. The strong influence of food on the sex of an invertebrate has been demonstrated only in this predator–prey relationship, and it is fundamental to assure stability to natural populations of this shrimp [16]

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