Search engine for discovering works of Art, research articles, and books related to Art and Culture
Javascript must be enabled to continue!
Evaluation of DNA Binding and Topoisomerase I Inhibitory Activities of 16’‐Decarbomethoxydihydrovoacamine from Tabernaemontana corymbosa
View through CrossRef
AbstractAn iboga‐vobasine bisindole alkaloid, 16’‐decarbomethoxydihydrovoacamine (1) isolated from the stem bark extract of Tabernaemontana corymbosa exhibited strong cytotoxicity against colorectal cancer cell lines in our preliminary study. As an initial step to elucidate its anti‐proliferative mechanism, the DNA binding and topoisomerase I (topo1) inhibitory activities of the bisindole 1 were investigated. The results of the in vitro DNA binding studies and molecular docking calculations collectively suggested that 1 binds to the DNA minor groove via hydrophobic interactions with a binding constant (Kb) of 7.40×105 M−1. Treatment of Escherichia coli topo1 with 1 did not inhibit the enzyme from relaxing the supercoiled plasmid DNA pBR322, indicating that the cytotoxicity of 1 in colorectal cancer cells is independent of topo1. The bisindole is predicted to possess substantial bioavailability without major toxicity. Moreover, the cytotoxicity of 1 is selective towards the colorectal cancer cells as evaluated using the MTT assay.
Title: Evaluation of DNA Binding and Topoisomerase I Inhibitory Activities of 16’‐Decarbomethoxydihydrovoacamine from Tabernaemontana corymbosa
Description:
AbstractAn iboga‐vobasine bisindole alkaloid, 16’‐decarbomethoxydihydrovoacamine (1) isolated from the stem bark extract of Tabernaemontana corymbosa exhibited strong cytotoxicity against colorectal cancer cell lines in our preliminary study.
As an initial step to elucidate its anti‐proliferative mechanism, the DNA binding and topoisomerase I (topo1) inhibitory activities of the bisindole 1 were investigated.
The results of the in vitro DNA binding studies and molecular docking calculations collectively suggested that 1 binds to the DNA minor groove via hydrophobic interactions with a binding constant (Kb) of 7.
40×105 M−1.
Treatment of Escherichia coli topo1 with 1 did not inhibit the enzyme from relaxing the supercoiled plasmid DNA pBR322, indicating that the cytotoxicity of 1 in colorectal cancer cells is independent of topo1.
The bisindole is predicted to possess substantial bioavailability without major toxicity.
Moreover, the cytotoxicity of 1 is selective towards the colorectal cancer cells as evaluated using the MTT assay.
Related Results
Topoisomerase Assays
Topoisomerase Assays
AbstractTopoisomerases are enzymes that play essential roles in DNA replication, transcription, chromosome segregation, and recombination. All cells have two major forms of DNA top...
Genome wide hypomethylation and youth-associated DNA gap reduction promoting DNA damage and senescence-associated pathogenesis
Genome wide hypomethylation and youth-associated DNA gap reduction promoting DNA damage and senescence-associated pathogenesis
Abstract
Background: Age-associated epigenetic alteration is the underlying cause of DNA damage in aging cells. Two types of youth-associated DNA-protection epigenetic mark...
Evaluation of Oxalis Corymbosa Extracts from Different Plant Parts and Seasons as a Potential Source of Antioxidants
Evaluation of Oxalis Corymbosa Extracts from Different Plant Parts and Seasons as a Potential Source of Antioxidants
Oxalis corymbosa is an important medicinal and edible perennial herb widely distributed throughout the world. The aim of this study was to evaluate the phenolic contents and antiox...
Echinococcus granulosus in Environmental Samples: A Cross-Sectional Molecular Study
Echinococcus granulosus in Environmental Samples: A Cross-Sectional Molecular Study
Abstract
Introduction
Echinococcosis, caused by tapeworms of the Echinococcus genus, remains a significant zoonotic disease globally. The disease is particularly prevalent in areas...
Human papillomavirus type 16 E7 protein inhibits DNA binding by the retinoblastoma gene product.
Human papillomavirus type 16 E7 protein inhibits DNA binding by the retinoblastoma gene product.
The human papillomavirus E7 gene can transform murine fibroblasts and cooperate with other viral oncogenes in transforming primary cell cultures. One biochemical property associate...
Analysis of topoisomerase II‐mediated DNA cleavage of the c‐myc gene during HL60 differentiation
Analysis of topoisomerase II‐mediated DNA cleavage of the c‐myc gene during HL60 differentiation
We have investigated the effect of mAMSA, a potent topoisomerase II inhibitor, on the c‐myc proto‐oncogene of the acute promyelocytic leukemia HL60 cell line during its differentia...
Identification of host proteins required for hepatitis B virus covalently closed circular DNA biosynthesis by a chemogenetic approach
Identification of host proteins required for hepatitis B virus covalently closed circular DNA biosynthesis by a chemogenetic approach
Chronic hepatitis B virus (HBV) infection relies on stable maintenance and proper functioning of a nuclear episomal form of viral genome called covalently closed circular (ccc) DNA...
Abstract 3500: Nucleolytic processing of Topoisomerase 2 covalent complexes
Abstract 3500: Nucleolytic processing of Topoisomerase 2 covalent complexes
Abstract
The generation of elevated levels of enzyme: DNA covalent complexes is the key event in cell killing by many drugs targeting DNA topoisomerases. These agent...