UM  > 中華醫藥研究院
Supramolecular strategy for reducing the cardiotoxicity of bedaquiline without compromising its antimycobacterial efficacy
Kuok, Kit Ieng1,2; Ng, Phoebe Choi In1,2; Ji, Xia3; Wang, Chunming1,2; Yew, Wing Wai4; Chan, Denise P. C.4; Zheng, Jun3; Lee, Simon M. Y.1,2; Wang, Ruibing1,2
2018-09
Conference Name3rd International Symposium on Phytochemicals in Medicine and Food (ISPMF)
Source PublicationFOOD AND CHEMICAL TOXICOLOGY
Volume119
Pages425-429
Conference DateAUG 25-30, 2018
Conference PlaceKunming, PEOPLES R CHINA
Publication PlaceTHE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLAND
PublisherPERGAMON-ELSEVIER SCIENCE LTD
Abstract

Bedaquiline (BDQ) is a newly approved anti-tuberculosis drug in treating multidrug-resistant tuberculosis. However, it has very poor aqueous solubility and several case reports have proposed that BDQ has potential risk of cardiotoxicity to patients. In this present study, we have explored into employing host-guest interactions between a synthetic receptor, cucurbit[7]uril (CB[7]), and BDQ aiming to improve the solubility and reduce the inherent cardiotoxicity of BDQ. HPLC-UV test on the solubility of BDQ in the absence and in the presence of increasing concentrations of CB[7] suggested a host-dependent guest-solubility enhancements. Cardiovascular studies using an in vivo zebrafish model demonstrated that the cardiotoxicity of BDQ was indeed alleviated upon its complexations by the synthetic receptor. Furthermore, our in vitro antibacterial studies suggested that CB[7] formulated BDQ preserved its antimycobacterial efficacy against Mycobacterium smegmatis. Therefore, CB[7] may become a suitable pharmaceutical excipient in formulating BDQ for improving its physiochemical properties (such as solubility), and for alleviating its side effects (such as cardiotoxicity), while the antimycobacterial efficacy of BDQ may be well maintained.

KeywordCucurbit[7]Uril Bedaquiline Supramolecular Formulation Cardiotoxicity Antimycobacterial
DOIhttp://doi.org/10.1016/j.fct.2017.12.022
URLView the original
Indexed BySCI ; CPCI
Language英语
WOS Research AreaFood Science & Technology ; Toxicology
WOS SubjectFood Science & Technology ; Toxicology
WOS IDWOS:000443664200051
The Source to ArticleWOS
Fulltext Access
Citation statistics
Document TypeConference paper
CollectionInstitute of Chinese Medical Sciences
Affiliation1.Univ Macau, State Key Lab Qual Res Chinese Med, Taipa, Macau, Peoples R China
2.Univ Macau, Inst Chinese Med Sci, Taipa, Macau, Peoples R China
3.Univ Macau, Fac Hlth Sci, Taipa, Macau, Peoples R China
4.Chinese Univ Hong Kong, Stanley Ho Ctr Emerging Infect Dis, Hong Kong, Hong Kong, Peoples R China
First Author AffilicationUniversity of Macau
Recommended Citation
GB/T 7714
Kuok, Kit Ieng,Ng, Phoebe Choi In,Ji, Xia,et al. Supramolecular strategy for reducing the cardiotoxicity of bedaquiline without compromising its antimycobacterial efficacy[C]. THE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLAND:PERGAMON-ELSEVIER SCIENCE LTD,2018:425-429.
Related Services
Recommend this item
Bookmark
Usage statistics
Export to Endnote
Google Scholar
Similar articles in Google Scholar
[Kuok, Kit Ieng]'s Articles
[Ng, Phoebe Choi In]'s Articles
[Ji, Xia]'s Articles
Baidu academic
Similar articles in Baidu academic
[Kuok, Kit Ieng]'s Articles
[Ng, Phoebe Choi In]'s Articles
[Ji, Xia]'s Articles
Bing Scholar
Similar articles in Bing Scholar
[Kuok, Kit Ieng]'s Articles
[Ng, Phoebe Choi In]'s Articles
[Ji, Xia]'s Articles
Terms of Use
No data!
Social Bookmark/Share
File name: Kuok-2018-Supramolecular-strategy-for-reducin (1).pdf
Format: Adobe PDF
All comments (0)
No comment.
 

Items in the repository are protected by copyright, with all rights reserved, unless otherwise indicated.