Seaweed Secondary Metabolites In Vitro and In Vivo Anticancer Activity

• Main Authors: Djenisa H. A. Rocha, Ana M. L. Seca, Diana C. G. A. Pinto
• Format: Article
• Language: English
• Published: MDPI AG 2018-10-01
• Series: Marine Drugs
• Subjects: seaweeds; secondary metabolites; cytotoxic activity; cancer; terpenoids; bromophenols; dictyolactone; cholest-5-en-3β,7α-diol; halomon; laurebiphenyl
• Online Access: https://www.mdpi.com/1660-3397/16/11/410

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.