Dehydrodiisoeugenol (DHIE) is a neolignan found in more than 17 plant species, including herbs, fruit, and root. DHIE was, for the first time, isolated from Myristica fragrans bark in 1973. Since then, many methodologies have been used for the obtention of DHIE, including classical chemistry synthesis using metal catalysts and biocatalytic synthesis; employing horseradish peroxidase; peroxidase from Cocos nucifera; laccase; culture cells of plants; and microorganisms. Increasing evidence has indicated that DHIE has a wide range of biological activities: anti-inflammatory, anti-oxidant, anti-cancerogenic, and anti-microbial properties. However, evidence in vivo and in human beings is still lacking to support the usefulness potential of DHIE as a therapeutic agent. This study’s review was created by searching for relevant DHIE material on websites such as Google Scholar, PubMed, SciFinder, Scholar, Science Direct, and others. This reviews the current state of knowledge regarding the different synthetical routes and biological applications of DHIE.

Lignans and neolignans are plant’s secondary metabolites, widely distributed in the plant kingdom, and have been identified in more than 70 plant families. These compounds are mainly localized in lignified tissues, seeds, and roots. Lignans and neolignans present a great variety of biological activities, such as antioxidant, anti-inflammatory, antineurodegenerative, antiviral, antimicrobial, and antitumor. By 2040, it is estimated that the number of new cancer cases per year will rise to 29.5 million; therefore, the development of new anticancer agents and adjuvants is essential. Lignans and neolignans have also indicated a reduction in the risk of cancer at different stages. The objective of this review is to search and analyze the cytotoxic and antitumor activity of lignans and neolignans that can be an important source of new antitumor drugs. We have made a comprehensive summary of 113 lignans and neolignans, obtained from 44 plants and divided between 34 families, which demonstrated cytotoxic activity in several human cancer cell lines evaluated through various in vitro studies and other in vivo models, by inducing mitochondrial apoptosis and cell cycle arrest, inhibiting NF-κβ activity and activation of metalloproteinases (MMPs), among other processes. Overall, 13 compounds, methoxypinoresinol, arctigenin, trachelogenin, 4-O-methylhonokiol, honokiol, bifidenone, (−)-trachelogeninit, deoxypodophyllotoxin, matairesinol, bejolghotin G, H, and I, and hedyotol-B, showed the best anticancer activity.