Abstract
AbstractCancer, one of the leading causes of death worldwide, is an abnormal cell proliferation that fails to respond to the normal signals. In an effort to eradicate the growing menace of cancer, a clear understanding of fundamental biology and molecular mechanism of carcinogenesis is essential for targeted therapies. Among the devised strategies in use for cancer treatment, the one that is of immense interest is the development of plant based novel anticancer agents. Due to their tremendous availability, biological activity and efficacy, the phytochemicals deemed a gibbous future in chemoprevention. In the present study, several phenolics based structurally related compounds of steroidal and non-steroidal skeleton were synthesized and tested for their modulatory effect on ornithine decarboxylase activity, an enzyme highly upregulated in cancer. Additionally, these compounds were also examined for radical scavenging extent to establish a correlation with the anticancer property. Our result suggests that the tested compounds possessed radical scavenging activity, for being the inherent property of the phenolics. 3-(3’,4’5’-trimethoxyphenyl)-4,5,6-trimethoxyindan-1-one oxime exhibited highest inhibition of enzyme activity (91%) followed by 1-(2,4-dibromophenyl)-3-[3-methoxyestra 1,3,5(10)-trien-17-acetate,2-yl]-2-propen-1-one (85%), 2-Hydroxy, 3-(3’,4’,5’-trimethoxy phenyl)-4,5,6-trimethoxy ind-2-en-1-one (80%), 1-(3,4-methylenedioxyphenyl)-3-(3,4,5-trimethoxyphenyl)-2-propen-1-one (74%) and 1-(3,-methoxy, 4-hydroxyphenyl)-3-[3-methoxyestra 1,3,5(10)-trien-17-acetate, 2-yl]-2-propen-1-one (67%). Furthermore, it was observed that 1-(3-Methoxy, 4- hydroxyphenyl)-3-[3-methoxyestra 1,3,5 (10)-trien-17-acetate, 2-yl]-2-propen-1-one showed the highest scavenging effect (67%) in nitric oxide assay, whereas 1-(3-methylphenyl)-3-[3-methoxy, 17-hydroxyestra 1,3,5(10)-trien, 2-yl]-2-propen-1-one showed maximum inhibition of radical formation in 2,2-diphenyl-1-picrylhydrazyl analysis. Most of these compounds possessed a 3,4,5-trimethoxyphenyl unit which might be inducing enzyme inhibition and scavenging radical formation. Further investigations are on the way to establish the structure-activity relationship, so that these compounds can be developed as anticancer agents.
Highlights
In an effort to eradicate the growing menace of cancer, a clear understanding of fundamental biology and molecular mechanism of carcinogenesis is essential for targeted therapies
Among the devised strategies being in use for cancer treatment, the one that is of immense interest is the development of plant based novel anticancer agents
Several phenolics based structurally related compounds of steroidal and non-steroidal skeleton were synthesized and tested for their modulatory effect on ornithine decarboxylase activity, an enzyme highly upregulated in cancer. These compounds were examined for radical scavenging action to establish a correlation with the anticancer property
Summary
One of the leading cause of death worldwide, is an abnormal cell proliferation that fails to respond to the normal signals.In an effort to eradicate the growing menace of cancer, a clear understanding of fundamental biology and molecular mechanism of carcinogenesis is essential for targeted therapies.Among the devised strategies being in use for cancer treatment, the one that is of immense interest is the development of plant based novel anticancer agents.Due to their tremendous availability, biological activity and efficacy, the phytochemicals deemed a gibbous future in chemoprevention.In the present study, several phenolics based structurally related compounds of steroidal and non-steroidal skeleton were synthesized and tested for their modulatory effect on ornithine decarboxylase activity, an enzyme highly upregulated in cancer.these compounds were examined for radical scavenging action to establish a correlation with the anticancer property. One of the leading cause of death worldwide, is an abnormal cell proliferation that fails to respond to the normal signals. In an effort to eradicate the growing menace of cancer, a clear understanding of fundamental biology and molecular mechanism of carcinogenesis is essential for targeted therapies.
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