Discovery of a natural fluorescent probe targeting the Plasmodium falciparum cysteine protease falcipain-2

Lili Zhu; Lei Shan; Junsheng Zhu; Li Li; Shiliang Li; Liyan Wang; Jiawei Wang; Shoude Zhang; Hongchang Zhou; Weidong Zhang; Honglin Li

doi:10.1007/s11427-019-1581-2

Discovery of a natural fluorescent probe targeting the Plasmodium falciparum cysteine protease falcipain-2

Lili Zhu
, Lei Shan
, Junsheng Zhu
, Li Li
, Shiliang Li
, Liyan Wang
, Jiawei Wang
, Shoude Zhang
, Hongchang Zhou
, Weidong Zhang^*
, Honglin Li^*

^*Corresponding author for this work

Research output: Contribution to journal › Article › peer-review

5 Scopus citations

Abstract

The Plasmodium falciparum cysteine protease falcipain-2 (FP-2) is an attractive antimalarial target. Here, we discovered that the natural compound NP1024 is a nonpeptidic inhibitor of FP-2 with an IC₅₀ value of 0.44 μmol L⁻¹. The most exciting finding is that both in vitro and in vivo, NP1024 directly targets FP-2 in malaria parasite-infected erythrocytes as a natural fluorescent probe, thereby paving the way for an integration of malaria diagnosis and treatment.

Original language	English
Pages (from-to)	1016-1025
Number of pages	10
Journal	Science China Life Sciences
Volume	63
Issue number	7
DOIs	https://doi.org/10.1007/s11427-019-1581-2
State	Published - 1 Jul 2020
Externally published	Yes

Keywords

acylated flavonol monoglycoside
antimalarial agent
falcipain-2
fluorescent probe
malaria diagnosis

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1007/s11427-019-1581-2

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title = "Discovery of a natural fluorescent probe targeting the Plasmodium falciparum cysteine protease falcipain-2",

abstract = "The Plasmodium falciparum cysteine protease falcipain-2 (FP-2) is an attractive antimalarial target. Here, we discovered that the natural compound NP1024 is a nonpeptidic inhibitor of FP-2 with an IC50 value of 0.44 μmol L−1. The most exciting finding is that both in vitro and in vivo, NP1024 directly targets FP-2 in malaria parasite-infected erythrocytes as a natural fluorescent probe, thereby paving the way for an integration of malaria diagnosis and treatment.",

keywords = "acylated flavonol monoglycoside, antimalarial agent, falcipain-2, fluorescent probe, malaria diagnosis",

author = "Lili Zhu and Lei Shan and Junsheng Zhu and Li Li and Shiliang Li and Liyan Wang and Jiawei Wang and Shoude Zhang and Hongchang Zhou and Weidong Zhang and Honglin Li",

note = "Publisher Copyright: {\textcopyright} 2020, Science China Press and Springer-Verlag GmbH Germany, part of Springer Nature.",

year = "2020",

month = jul,

day = "1",

doi = "10.1007/s11427-019-1581-2",

language = "英语",

volume = "63",

pages = "1016--1025",

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publisher = "Science China Press ",

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}

TY - JOUR

T1 - Discovery of a natural fluorescent probe targeting the Plasmodium falciparum cysteine protease falcipain-2

AU - Zhu, Lili

AU - Shan, Lei

AU - Zhu, Junsheng

AU - Li, Li

AU - Li, Shiliang

AU - Wang, Liyan

AU - Wang, Jiawei

AU - Zhang, Shoude

AU - Zhou, Hongchang

AU - Zhang, Weidong

AU - Li, Honglin

PY - 2020/7/1

Y1 - 2020/7/1

N2 - The Plasmodium falciparum cysteine protease falcipain-2 (FP-2) is an attractive antimalarial target. Here, we discovered that the natural compound NP1024 is a nonpeptidic inhibitor of FP-2 with an IC50 value of 0.44 μmol L−1. The most exciting finding is that both in vitro and in vivo, NP1024 directly targets FP-2 in malaria parasite-infected erythrocytes as a natural fluorescent probe, thereby paving the way for an integration of malaria diagnosis and treatment.

AB - The Plasmodium falciparum cysteine protease falcipain-2 (FP-2) is an attractive antimalarial target. Here, we discovered that the natural compound NP1024 is a nonpeptidic inhibitor of FP-2 with an IC50 value of 0.44 μmol L−1. The most exciting finding is that both in vitro and in vivo, NP1024 directly targets FP-2 in malaria parasite-infected erythrocytes as a natural fluorescent probe, thereby paving the way for an integration of malaria diagnosis and treatment.

KW - acylated flavonol monoglycoside

KW - antimalarial agent

KW - falcipain-2

KW - fluorescent probe

KW - malaria diagnosis

UR - https://www.scopus.com/pages/publications/85079456143

U2 - 10.1007/s11427-019-1581-2

DO - 10.1007/s11427-019-1581-2

M3 - 文章

C2 - 32048162

AN - SCOPUS:85079456143

SN - 1674-7305

VL - 63

SP - 1016

EP - 1025

JO - Science China Life Sciences

JF - Science China Life Sciences

IS - 7

ER -

Discovery of a natural fluorescent probe targeting the Plasmodium falciparum cysteine protease falcipain-2

Abstract

Keywords

UN SDGs

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