Synthesis, Characterization and Biological Screening of Ferulic Acid Derivatives

Abstract

According to WHO, cancer is a leading cause of death worldwide, accounting for 8.2 million deaths in 2012. Among several factors involved in the pathogenesis of cancer, free radical formation followed by damage to DNA and cell protein is one of the causes. Natural plant products have gained enormous interest in the prevention or treatment of chronic diseases. Ferulic acid, like other phenolic acids (caffeic acid, sinapic acid) possess anti cancer activity. A series of ferulic esters (FE1 -FE11) and ferulic amides (FA1 -FA10) were synthesized and evaluated for their cytotoxic activity.

Quantitative Structure-Activity Relationship Study of Ester-Based Ferulic Acid Derivatives Against Cervical Cancer Cell (Hela)

“…FE5 and FE6 have chloroethyl and bromoethyl substituent, respectively, which are shown in Figure 2. These compounds resulted in the relatively higher anticancer activity against HELA cell lines compared with other ferulic acid derivatives with longer alkyl chain studied [8,13].…”

“…The structure of ferulic acid derivatives including the ones with methyl, ethyl, n-propyl, n-butyl, bromo-ethyl, and chloro ethyl, is shown in Figure 2. These compounds were observed for their activities against HELA cancer lines as being studied by Kiran et al (2015).…”

“…Thus, ester derivatives of ferulic acid are favorable in used as drugs, as reported by Serafim et. al (2011) cafeic and ferulic acid ester derivatives exerted cytotoxicity to the breast cancer cells compared with the parent compound as well as the study for HELA cells [13]. Modification of the carboxylic group with a different alkyl group of ferulic acid including methyl, ethyl, npropyl, n-butyl, bromo ethyl, and chloroethyl affected the anticancer activity [13,15].…”

“…Ferulic acid has shown to regulate the key enzymes which were responsible for free radical-induced cell damage [13]. Ferulic acid is biosynthesized from amino acid phenylalanine ISSN:XXXX-XXXX through a shikimic acid pathway.…”

Bioactive compounds from marine Streptomyces sp.: Structure identification and biological activities

“…Due to its abundance, these foods may have beneficial effects against disorders related to oxidative stress, such as diabetes, cancer, and neurodegenerative diseases, [29] platelet aggregation (PA)-inhibitory, angiotensin converting enzyme, (ACE)-inhibitory, tyrosinase-inhibitory, superoxide dismutase (SOD)like, [30] anticancer activities. [31] FA is considered as antioxidant agent, and commonly found in commelinid plants. [32] A combination of commercial enzymes that shows FA esterase activity with several Streptomyces carbohydrate-hydrolyzing enzymes, were reported to enhancing the enzymatic production of FA from defatted rice bran.…”