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Investigating interactions between chloroquine/hydroxychloroquine and their single enantiomers and angiotensin-converting enzyme 2 by a cell membrane chromatography method.
Jia, Qianqian; Fu, Jia; Liang, Peida; Wang, Saisai; Wang, Yamin; Zhang, Xin; Zhou, Huaxin; Zhang, Liyang; Lv, Yanni; Han, Shengli.
  • Jia Q; School of Pharmacy, Xi'an Jiaotong University, Xi'an, 710061, P. R. China.
  • Fu J; Institute of Pharmaceutical Science and Technology, Western China Science &Technology Innovation Harbour, Xi'an, 710000, P. R. China.
  • Liang P; School of Pharmacy, Xi'an Jiaotong University, Xi'an, 710061, P. R. China.
  • Wang S; Institute of Pharmaceutical Science and Technology, Western China Science &Technology Innovation Harbour, Xi'an, 710000, P. R. China.
  • Wang Y; School of Pharmacy, Xi'an Jiaotong University, Xi'an, 710061, P. R. China.
  • Zhang X; Institute of Pharmaceutical Science and Technology, Western China Science &Technology Innovation Harbour, Xi'an, 710000, P. R. China.
  • Zhou H; School of Pharmacy, Xi'an Jiaotong University, Xi'an, 710061, P. R. China.
  • Zhang L; Institute of Pharmaceutical Science and Technology, Western China Science &Technology Innovation Harbour, Xi'an, 710000, P. R. China.
  • Lv Y; School of Pharmacy, Xi'an Jiaotong University, Xi'an, 710061, P. R. China.
  • Han S; Institute of Pharmaceutical Science and Technology, Western China Science &Technology Innovation Harbour, Xi'an, 710000, P. R. China.
J Sep Sci ; 45(2): 456-467, 2022 Jan.
Article in English | MEDLINE | ID: covidwho-1499288
ABSTRACT
Chloroquine and hydroxychloroquine have been studied since the early clinical treatment of SARS-CoV-2 outbreak. Considering these two chiral drugs are currently in use as the racemate, high-expression angiotensin-converting enzyme 2 cell membrane chromatography was established for investigating the differences of two paired enantiomers binding to angiotensin-converting enzyme 2 receptor. Molecular docking assay and detection of SARS-CoV-2 spike pseudotyped virus entry into angiotensin-converting enzyme 2-HEK293T cells were also conducted for further investigation. Results showed that each single enantiomer could bind well to angiotensin-converting enzyme 2, but there were differences between the paired enantiomers and corresponding racemate in frontal analysis. R-Chloroquine showed better angiotensin-converting enzyme 2 receptor binding ability compared to S-chloroquine/chloroquine (racemate). S-Hydroxychloroquine showed better angiotensin-converting enzyme 2 receptor binding ability than R-hydroxychloroquine/hydroxychloroquine. Moreover, each single enantiomer was proved effective compared with the control group; compared with S-chloroquine or the racemate, R-chloroquine showed better inhibitory effects at the same concentration. As for hydroxychloroquine, R-hydroxychloroquine showed better inhibitory effects than S-hydroxychloroquine, but it slightly worse than the racemate. In conclusion, R-chloroquine showed better angiotensin-converting enzyme 2 receptor binding ability and inhibitory effects compared to S-chloroquine/chloroquine (racemate). S-Hydroxychloroquine showed better angiotensin-converting enzyme 2 receptor binding ability than R-hydroxychloroquine/hydroxychloroquine (racemate), while the effect of preventing SARS-CoV-2 pseudovirus from entering cells was weaker than R-hydroxychloroquine/hydroxychloroquine (racemate).
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Full text: Available Collection: International databases Database: MEDLINE Main subject: Chloroquine / Chromatography, High Pressure Liquid / Angiotensin-Converting Enzyme 2 / Hydroxychloroquine Type of study: Experimental Studies / Prognostic study Limits: Humans Language: English Journal: J Sep Sci Year: 2022 Document Type: Article

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Full text: Available Collection: International databases Database: MEDLINE Main subject: Chloroquine / Chromatography, High Pressure Liquid / Angiotensin-Converting Enzyme 2 / Hydroxychloroquine Type of study: Experimental Studies / Prognostic study Limits: Humans Language: English Journal: J Sep Sci Year: 2022 Document Type: Article