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19-(Benzyloxy)-19-oxojolkinolide B (19-BJB), an ent-abietane diterpene diepoxide, inhibits the growth of bladder cancer T24 cells through DNA damage
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19-(Benzyloxy)-19-oxojolkinolide B (19-BJB), an ent-abietane diterpene diepoxide, inhibits the growth of bladder cancer T24 cells through DNA damage
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19-(Benzyloxy)-19-oxojolkinolide B (19-BJB), an ent-abietane diterpene diepoxide, inhibits the growth of bladder cancer T24 cells through DNA damage
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Journal Article
19-(Benzyloxy)-19-oxojolkinolide B (19-BJB), an ent-abietane diterpene diepoxide, inhibits the growth of bladder cancer T24 cells through DNA damage
2021
Overview
Diterpenoids jolkinolide A and B, were first isolated from Euphorbia fischeriana . In our previous research, 19-(Benzyloxy)-19-oxojolkinolide B (19-BJB), a derivative of jolkinolides, was synthesized as a novel ent -abietane diterpene diepoxide. In this study, 19-BJB showed strong in vitro activity against bladder cancer cell lines. DNA damage which was observed through the interaction of 19-BJB with nucleotide chains and affected DNA repair resulted in the activation of checkpoint kinase 1 (Chk1) and checkpoint kinase 2 (Chk2) in bladder cancer cell lines. In vivo testing in nude mice also proved that 19-BJB revealed a potential inhibitory effect on tumor growth. Additionally, the 3D-QSAR models of jolkinolides were established. Briefly, we proved that 19-BJB could potentially be used as a drug to inhibit the growth of bladder tumor.
Publisher
Public Library of Science,Public Library of Science (PLoS)
Subject
/ Animals
/ Antineoplastic Agents, Phytogenic
/ Bladder
/ Cancer
/ Checkpoint Kinase 1 - metabolism
/ Checkpoint Kinase 2 - metabolism
/ Diterpenes - therapeutic use
/ DNA
/ Drugs, Chinese Herbal - pharmacology
/ Drugs, Chinese Herbal - therapeutic use
/ Ethanol
/ Ethylenediaminetetraacetic acids
/ Funding
/ Humans
/ Male
/ Medicine
/ Medicine and Health Sciences
/ Mice
/ Molecular Docking Simulation
/ R&D
/ Research and analysis methods
/ Salts
/ Sodium
/ Traditional Chinese medicine
/ Trypsin
/ Urinary Bladder Neoplasms - drug therapy
