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Sains Malaysiana
51(10)(2022):
http://doi.org/10.17576/jsm-2022-5110-28
Konsep Penghibridan 4-Aminokuinolina sebagai Alternatif Agen Antiplasmodium
(4-Aminoquinoline Hybridization Concept as Alternative
Antiplasmodial Agent)
NURFARAHANIM MUHAMMAD ZUBIR1,
MOHD RIDZUAN MOHD ABD RAZAK2, AMATUL HAMIZAH ALI1, MUKRAM
MOHAMED MACKEEN1,3 & NURUL IZZATY HASSAN1,*
1Department of Chemical Sciences, Faculty of Science &
Technology, Universiti Kebangsaan Malaysia, 43600 UKM Bangi, Selangor Darul
Ehsan, Malaysia
2Herbal Medicine Research Centre, Institute for Medical
Research, National Institute of Health (NIH) Complex, Ministry of Health
Malaysia, 40170 Shah Alam, Selangor
3Institute of Systems Biology, Universiti Kebangsaan
Malaysia, 43600 UKM Bangi, Selangor Darul Ehsan, Malaysia
Received: 24 February 2022/Accepted: 29 June 2022
Abstrak
Kemunculan strain
parasit yang rintang terhadap hampir semua ubatan antimalaria telah mendorong
para saintis mengkaji penggantian mekanisme tindakan alternatif yang lebih
berkesan. Keberkesanan rawatan semasa antimalaria adalah terhad dari segi bio
ketersediaan ubat yang rendah, ketoksikan ubat yang tinggi dan kadar
keterlarutan dalam air yang rendah. Penghibridan adalah satu strategi menarik
bagi mengembangkan konsep penemuan ubat antimalaria. Kerangka 4-aminokuinolina
telah disasarkan dalam kebanyakan proses reka bentuk agen antiplasmodium kerana
kos sintesisnya yang murah, selamat dan kurang toksik sejak 20 tahun yang lalu.
Penemuan hibrid antiplasmodium menggunakan kerangka 4-aminokuinolina dan
pelbagai moieti seperti artemisinin, piperidin, indolin, pirimidin telah
menunjukkan aktiviti antiplasmodium yang baik. Walau bagaimanapun, sehingga
kini penemuan hibrid ini masih tidak dapat dibangunkan dan memasuki ujian
percubaan klinikal. Ulasan ini meringkaskan penemuan hibrid antiplasmodium yang telah diterbitkan dalam tempoh sebelas tahun ke belakang (2011-2021).
Kelebihan dan kelemahan konsep penghibridan sebagai pengganti agen
antiplasmodium sedia ada dibincangkan. Analisis kajian menunjukkan hibrid
4-aminokuinolina mempunyai aktiviti antiplasmodium yang setanding atau lebih
baik secara in vitro berbanding
rawatan profilaksis klorokuina. Hibrid kuinolina kelas IV adalah yang paling
kerap dikaji dan diperoleh dalam kajian ini sepanjang tempoh sebelas tahun ke
belakang. Kekurangan data praklinikal terperinci
mengenai hibrid yang disintesis telah menghalang kajian lanjut dalam ujian
klinikal.
Kata kunci: Hibrid; literatur sistematik; malaria; Plasmodium falciparum; 4-aminokuinolina
Abstract
The emergence of
parasitic strains’ resistant to
almost all antimalarial drugs has prompted scientists to study more effective
alternative mechanisms of action. Current antimalarial treatment is limited due
to poor drug bioavailability, high drug toxicity, and low aqueous solubility.
Hybridization is an exciting strategy in antimalarial drug discovery. The
4-aminoquinoline framework has been targeted in the design of various
antiplasmodial agents because its synthesis is low cost, safe and has been used over the past 20 years. The
discovery of antiplasmodial hybrids using the 4-aminoquinoline framework and
various moieties such as artemisinin, piperidine, indoline, and pyrimidine have
shown good antiplasmodial activity. However, these hybrids are still not fully
developed for clinical trials. This literature review
summarises the findings of antiplasmodial hybrids published over the past
eleven years (2011-2021). The advantages and disadvantages of hybridization as
a substitute for existing antiplasmodial agents are discussed. This review reports that
4-aminoquinoline hybrids had comparable or better in vitro antiplasmodial activity than the
chloroquine prophylaxis treatment. Class IV quinoline hybrids were the most
frequently studied and obtained in this study over the past eleven years. The
lack of detailed preclinical data on
the synthesised hybrids has hampered further studies in clinical trials.
Keywords: Hybrid; malaria; Plasmodium falciparum; systematic literature; 4-aminoquinoline
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*Corresponding
author; email: drizz@ukm.edu.my
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