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In vivo antimalarial activity and pharmacokinetics of artelinic acid-choline derivative liposomes in rodents

Published online by Cambridge University Press:  26 September 2019

Shuai Duan Open the ORCID record for Shuai Duan [Opens in a new window] ,
Ruili Wang ,
Rongrong Wang ,
Jiaqi Tang ,
Xiaoyang Xiao ,
Ning Li ,
Wenju Guo ,
Qingshan Yang ,
Guolian Ren  and
Shuqiu Zhang Open the ORCID record for Shuqiu Zhang [Opens in a new window]
Shuai Duan
Affiliation:
School of Pharmacy, Shanxi Medical University, 56 Xinjian South Road, Taiyuan030001, Shanxi, China
Ruili Wang
Affiliation:
School of Pharmacy, Shanxi Medical University, 56 Xinjian South Road, Taiyuan030001, Shanxi, China
Rongrong Wang
Affiliation:
School of Pharmacy, Shanxi Medical University, 56 Xinjian South Road, Taiyuan030001, Shanxi, China
Jiaqi Tang
Affiliation:
School of Pharmacy, Shanxi Medical University, 56 Xinjian South Road, Taiyuan030001, Shanxi, China
Xiaoyang Xiao
Affiliation:
School of Pharmacy, Shanxi Medical University, 56 Xinjian South Road, Taiyuan030001, Shanxi, China
Ning Li
Affiliation:
School of Pharmacy, Shanxi Medical University, 56 Xinjian South Road, Taiyuan030001, Shanxi, China
Wenju Guo
Affiliation:
School of Pharmacy, Shanxi Medical University, 56 Xinjian South Road, Taiyuan030001, Shanxi, China
Qingshan Yang
Affiliation:
School of Pharmacy, Shanxi Medical University, 56 Xinjian South Road, Taiyuan030001, Shanxi, China
Guolian Ren*
Affiliation:
School of Pharmacy, Shanxi Medical University, 56 Xinjian South Road, Taiyuan030001, Shanxi, China
Shuqiu Zhang*
Affiliation:
School of Pharmacy, Shanxi Medical University, 56 Xinjian South Road, Taiyuan030001, Shanxi, China
*
Authors for correspondence: Shuqiu Zhang, E-mail: shuqiu.zhang@sxmu.edu.cn; Guolian Ren, E-mail: glren2007@126.com
Authors for correspondence: Shuqiu Zhang, E-mail: shuqiu.zhang@sxmu.edu.cn; Guolian Ren, E-mail: glren2007@126.com
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Abstract

It is urgent to develop new antimalarial drugs with good therapeutic effects to address the emergence of drug resistance. Here, the artelinic acid-choline derivative (AD) was synthesized by dehydration reaction and esterification reaction, aimed to avoid the emergence of drug resistance by synergistic effect of artemisinins and choline derivative, which could compete with choline for rate-limiting enzymes in the phosphatidylcholine (PC) biosynthetic pathway. AD was formulated into liposomes (ADLs) by the thin-film hydration method. Efficacy of ADLs was evaluated by Peters 4-day suppression test. The suppression percentage against Plasmodium yoelii BY265 (PyBY265) in ADLs group was higher than those of positive control groups (dihydroartemisinin liposomes, P < 0.05) and other control groups (P ⩽ 0.05) at the doses of 4.4, 8.8, 17.6 µmol (kg·d)−1, respectively. The negative conversion fraction, recrudescence fraction and survival fraction of ADLs group were superior to other control groups. Pharmacokinetics in rats after intravenous injection suggested that ADLs exhibited higher exposure levels (indexed by area under concentration-time curve) than that of AD solution, artelinic acid liposomes or artelinic acid solution (P < 0.01). Taken together, ADLs exhibited promising antimalarial efficacy and pharmacokinetic characteristics.

Keywords

Antimalariaartelinic acidcholine derivativepharmacokinetics
Type
Research Article
Information
Parasitology , Volume 147 , Issue 1 , January 2020 , pp. 58 - 64
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Copyright
Copyright © Cambridge University Press 2019

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Footnotes

*

Both authors had contributed equally to this work.

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