Please use this identifier to cite or link to this item:
http://hdl.handle.net/10397/95459
DC Field | Value | Language |
---|---|---|
dc.contributor | Department of Applied Biology and Chemical Technology | en_US |
dc.creator | Wong, ILK | en_US |
dc.creator | Wang, XK | en_US |
dc.creator | Liu, Z | en_US |
dc.creator | Sun, W | en_US |
dc.creator | Li, FX | en_US |
dc.creator | Wang, BC | en_US |
dc.creator | Li, P | en_US |
dc.creator | Wan, SB | en_US |
dc.creator | Chow, LMC | en_US |
dc.date.accessioned | 2022-09-19T02:22:06Z | - |
dc.date.available | 2022-09-19T02:22:06Z | - |
dc.identifier.issn | 0223-5234 | en_US |
dc.identifier.uri | http://hdl.handle.net/10397/95459 | - |
dc.language.iso | en | en_US |
dc.publisher | Elsevier Masson | en_US |
dc.rights | © 2021 Elsevier Masson SAS. All rights reserved. | en_US |
dc.rights | © 2021. This manuscript version is made available under the CC-BY-NC-ND 4.0 license http://creativecommons.org/licenses/by-nc-nd/4.0/. | en_US |
dc.rights | The following publication Wong, I. L. K., Wang, X.-k., Liu, Z., Sun, W., Li, F.-x., Wang, B.-c., Li, P., Wan, S.-b., & Chow, L. M. C. (2021). Synthesis and evaluation of stereoisomers of methylated catechin and epigallocatechin derivatives on modulating P-glycoprotein-mediated multidrug resistance in cancers. European Journal of Medicinal Chemistry, 226, 113795 is available at https://dx.doi.org/10.1016/j.ejmech.2021.113795. | en_US |
dc.subject | Catechin (C) | en_US |
dc.subject | Epicatechin (EC) | en_US |
dc.subject | Epigallocatechin (EGC) | en_US |
dc.subject | Gallocatechin (GC) | en_US |
dc.subject | P-glycoprotein (P-gp) | en_US |
dc.title | Synthesis and evaluation of stereoisomers of methylated catechin and epigallocatechin derivatives on modulating P-glycoprotein-mediated multidrug resistance in cancers | en_US |
dc.type | Journal/Magazine Article | en_US |
dc.identifier.volume | 226 | en_US |
dc.identifier.doi | 10.1016/j.ejmech.2021.113795 | en_US |
dcterms.abstract | P-glycoprotein (P-gp; ABCB1)-mediated drug efflux causes multidrug resistance in cancer. Previous synthetic methylated epigallocatechin (EGC) possessed promising P-gp modulating activity. In order to further improve the potency, we have synthesized some novel stereoisomers of methylated epigallocatechin (EGC) and gallocatechin (GC) as well as epicatechin (EC) and catechin (C). The (2R, 3S)-trans-methylated C derivative 25 and the (2R, 3R)-cis-methylated EC derivative 31, both containing dimethyoxylation at ring B, tri-methoxylation at ring D and oxycarbonylphenylcarbamoyl linker between ring D and C3, are the most potent in reversing P-gp mediated drug resistance with EC50 ranged from 32 nM to 93 nM. They are non-toxic to fibroblast with IC50 > 100 μM. They can inhibit the P-gp mediated drug efflux and restore the intracellular drug concentration to a cytotoxic level. They do not downregulate surface P-gp protein level to enhance drug retention. They are specific for P-gp with no or low modulating activity towards MRP1- or BCRP-mediated drug resistance. In summary, methylated C 25 and EC 31 derivatives represent a new class of potent, specific and non-toxic P-gp modulator. | en_US |
dcterms.accessRights | open access | en_US |
dcterms.bibliographicCitation | European journal of medicinal chemistry, 15 Dec. 2021, v. 226, 113795 | en_US |
dcterms.isPartOf | European journal of medicinal chemistry | en_US |
dcterms.issued | 2021-12-15 | - |
dc.identifier.scopus | 2-s2.0-85115974185 | - |
dc.identifier.pmid | 34597896 | - |
dc.identifier.eissn | 1768-3254 | en_US |
dc.identifier.artn | 113795 | en_US |
dc.description.validate | 202209 bcww | en_US |
dc.description.oa | Accepted Manuscript | en_US |
dc.identifier.FolderNumber | ABCT-0008 | - |
dc.description.fundingSource | RGC | en_US |
dc.description.fundingSource | Others | en_US |
dc.description.fundingText | NSFC; NSFC-Shandong Joint Fund for Marine Science Research Centers; Special Fund for Marine Scientific Research in the Public Interest of China; Qingdao National Laboratory for Marine Science and Technology; PolyU | en_US |
dc.description.pubStatus | Published | en_US |
dc.identifier.OPUS | 61090482 | - |
dc.description.oaCategory | Green (AAM) | en_US |
Appears in Collections: | Journal/Magazine Article |
Files in This Item:
File | Description | Size | Format | |
---|---|---|---|---|
Wong_Synthesis_Evaluation_Stereoisomers.pdf | Pre-Published version | 3.58 MB | Adobe PDF | View/Open |
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