Abstract

Isolation, finding or discovery of novel anticancer agents is very important for cancer treatment, and seaweeds are one of the largest producers of chemically active metabolites with valuable cytotoxic properties, and therefore can be used as new chemotherapeutic agents or source of inspiration to develop new ones. Identification of the more potent and selective anticancer components isolated from brown, green and red seaweeds, as well as studies of their mode of action is very attractive and constitute a small but relevant progress for pharmacological applications. Several researchers have carried out in vitro and in vivo studies in various cell lines and have disclosed the active metabolites among the terpenoids, including carotenoids, polyphenols and alkaloids that can be found in seaweeds. In this review the type of metabolites and their cytotoxic or antiproliferative effects will be discussed additionally their mode of action, structure-activity relationship and selectivity will also be revealed. The diterpene dictyolactone, the sterol cholest-5-en-3β,7α-diol and the halogenated monoterpene halomon are among the reported compounds, the ones that present sub-micromolar cytotoxicity. Additionally, one dimeric sesquiterpene of the cyclolaurane-type, three bromophenols and one halogenated monoterpene should be emphasized because they exhibit half maximal inhibitory concentration (IC50) values between 1–5 µM against several cell lines.

Highlights

  • Cancer is one of the deadliest diseases, and its influence on European and USA mortality is 20%and 14% respectively [1]

  • In the last two decades, seaweed chemical profiles have demonstrated that they are rich in terpenoids, alkaloids, polyphenols, steroids, pigments and polysaccharides and some biological assays showed that several of these metabolites have promising pharmacological activities [23,24,25,26] including in cancer therapy [27,28,29]

  • This review aims to highlight the secondary metabolites isolated from seaweeds with the highest cytotoxic/antiproliferative activity

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Summary

Introduction

Cancer is one of the deadliest diseases, and its influence on European and USA mortality is 20%. Lung cancer is the most common, both in terms of incidence and mortality, followed by female breast and colorectal cancers These types of cancers account, each, for nearly 2 million diagnoses in 2018 [1,3]. In the last two decades, seaweed chemical profiles have demonstrated that they are rich in terpenoids, alkaloids, polyphenols, steroids, pigments and polysaccharides and some biological assays showed that several of these metabolites have promising pharmacological activities [23,24,25,26] including in cancer therapy [27,28,29]. This review aims to highlight the secondary metabolites isolated from seaweeds with the highest cytotoxic/antiproliferative activity. Their activity level, chemical structures, putative mechanisms of action will be discussed. Exceptions can be mentioned if they are rare cases or the mechanism of action is elucidated

Secondary Metabolites from Seaweeds with in Vitro Cytotoxic Activity
Carotenoid
Phenolic Compounds
Phlorotannins
Bromophenols
Alkaloids
Secondary Metabolites from Seaweeds with In Vivo Antitumor Activity
Findings
Conclusions

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