Antiproliferative Effect of Indole Phytoalexins

Abstract

Indole phytoalexins from crucifers have been shown to exhibit significant anti-cancer, chemopreventive, and antiproliferative activity. Phytoalexins are natural low molecular antimicrobial compounds that are synthesized and accumulated in plants after their exposure to pathogenic microorganisms. Most interestingly, crucifers appear to be the only plant family producing sulfur-containing indole phytoalexins. The mechanisms underlying its anti-cancer properties are unknown. Isolation from cruciferous plants does not provide sufficient quantities of indole phytoalexins and, for biological screening, they are usually obtainable through synthesis. Understanding the molecular mechanism of the action of these substances and their structure-activity relationships is quite important in the development of new analogs with a more favorable profile of biological activities. In this review, we present the key features of indole phytoalexins, mainly their antiproliferative ativities.

Anti-cancer potential of natural products: recent trends, scope and relevance

“…Grapes have been reported to have a natural compound called as 3,4′,5-trihydroxy-trans-stilbene, polyphenolic in nature which is also known commonly as Resveratrol having widespectrum bioactive properties.This compound was shown to have anti-cancer chemoprevention property along with cardioprotective, anti-inflammatory and anti-viral actions [45][46][47][48]. More so Resveratrol displayed anti-proliferatve action along with the promotion of cell cycle arrest, and apoptosis inducer in cancer cells.This was mediated through the suppression of ERK1/2 (an extracellular signaling kinase),tumor suppressor protein p53,Rb/E2F,cell cyclins and CDKs as well.Moreover transcriptional factors involved in cell proliferation along with stress responses including NF-κB, activator protein 1 (AP1) and Egr1, mitogen-activated protein kinases (MAPKs), tyrosine kinases (Src) are reported to induce apoptosis.…”

Novel Sulfur-Containing Indole from the Leaves of Clematis Viridiflora Bertol

“…20 Sulfur-containing indoles isolated from Brassica species (Cruciferae) have previously been identified asphytoalexins, 21 they have been reported as minor constituents and possess a wide range of biological activities. 22 The main structure of these metabolites is characterized by the presence of indole nucleus substituted with one or two sulfur atoms of which one is located at C-2.…”

“…22 The main structure of these metabolites is characterized by the presence of indole nucleus substituted with one or two sulfur atoms of which one is located at C-2. 20 The basic indole is biogenetically thought to be derived from Ltryptophan, and the sulfur atoms could be incorporated through cysteine and methione. 23 Compound1, containing one sulfur atom, could share the biosynthetic pathway with that ofbrassicanal A (6) reported from Brassica campestris.…”

Regulation of the Ras-Related Signaling Pathway by Small Molecules Containing an Indole Core Scaffold: A Potential Antitumor Therapy

“…Indole is widely found in cruciferous plants and bacteria, and several indole derivatives are closely related to life activities. It plays important roles as an interspecies and interkingdom signaling pathway molecule in a wide range of antiinflammatory and antitumor activities, with minimal side effects and strong selectivity (Järvisalo and Saris, 1975;Banerjee et al, 2011;Chripkova et al, 2016;Huang et al, 2016;Patil et al, 2016;Okada et al, 2017;Singh et al, 2017;Yang et al, 2017;Yu C. P. et al, 2017;Hashmi et al, 2018;Zhao et al, 2018). Popular active natural and synthetic indole derivatives have been discovered and investigated (Figure 2; Hurdle et al, 2004;Watanabe et al, 2011;White et al, 2012;Nalamachu and Wortmann, 2014;Montserratde la Paz et al, 2016;Yu H. et al, 2017;Haque et al, 2018).…”