Sains Malaysiana 50(10)(2021): 2945-2956 http://doi.org/10.17576/jsm-2021-5010-09 Sintesis, Aktiviti Antiplasmodium dan Kesitotoksikan secara in vitro Sebatian Plasmodium falciparum K1 (Synthesis, in vitro Antiplasmodial Activity and Cytotoxicity of Metalloporphyrins against Plasmodium falciparum K1 Strain) NUUR HAZIQAH MOHD RADZUAN, NUR AQILAH ZAHIRAH NORAZMI, AMATUL HAMIZAH ALI, MUNTAZ ABU BAKAR, HANI KARTINI AGUSTAR, MOHD RIDZUAN MOHD ABD RAZAK & NURUL IZZATY HASSAN* ABSTRAK Jangkitan malaria adalah penyakit berjangkit serius yang disebabkan oleh parasit plasmodium dan harus dirawat sebagai perubatan kecemasan. Sehingga kini, tiada vaksin yang sudah dikomersialkan untuk mencegah malaria. NiDDHP, NiDPP, NiTPP, ZnDHP, ZnDPP dan ZnTPP dihasilkan melalui penyejatan Lindsey sebelum dicirikan secara spektroskopi (resonans magnet nukleus, ultra secara in vitro terhadap strain rintang-klorokuina, P. falciparum K1 dinilai dan dibandingkan dengan aktiviti antiplasmodium dadah rujukan seperti klorokuina dan artemisinin. ZnDHP, ZnTPP dan Ni DPP merencat pertumbuhan parasit dengan 50% kepekatan perencatan berkesan (EC 50 ) dalam julat aktiviti antiplasmodium sederhana iaitu 21.4 sehingga 36.0 µM. Aktiviti kesitotoksikan terhadap sel mamalia Vero yang ditunjukkan oleh NiDPP, ZnDHP dan ZnTPP berada dalam julat tidak toksik iaitu 97 sehingga 587 µM. ZnDHP mempunyai nilai indeks pemilihan yang paling tinggi iaitu 27.2 µM, menunjukkan aktiviti antiplasmodium yang selektif terhadap perencatan plasmodium dan tidak toksik terhadap sel mamalia. Kata kunci: Antiplasmodium; in vitro; kesitotoksikan; P. falciparum ABSTRACT Malaria infection is a severe infectious disease caused by plasmodium parasites and should be treated as emergency medicine. Until now, no vaccine has been commercialized to prevent malaria. Six nickel(II) and zinc(II) metal porphyrin compounds based on free meso porphyrin base 5,15-diphenylporphrin (2), 5,15-dihexylporphyrin (3), and 5,10,15,20-tetraphenyl porphyrin (4), known as NiDDHP, NiDPP, NiTPP, ZnDHP, ZnDPP and ZnTPP are produced through Lindsey condensation before being characterized by spectroscopy (nuclear magnetic resonance, ultraviolet-visible spectrophotometry, mass spectrometry) and physical (melting point). In vitro antiplasmodial and cytotoxicity activities against the P. falciparum K1 strain were assessed and compared to the antiplasmodial activity of referral drugs such as chloroquine artemisinin. ZnDHP, ZnTPP and NiDPP recorded parasites’ growth with 50% effective inhibition concentration ( EC 50 ) in a range of 21.4 to 36.0 μM. Cytotoxic activities of NiDPP, ZnDHP and ZnTPP against Vero mammalian cells were in a non-toxic range of about 97 to 587 µM. ZnDHP possessed the highest selectivity index value of 27.2 µM, indicating that the compound’s Keywords: Antiplasmodial; cytotoxicity; in vitro; metalloporphyrin; P. falciparum K1 PENGENALAN Pelan Strategik Eliminasi Malaria Kebangsaan mensasarkan penurunan kejadian kes malaria dan mencapai status eliminasi malaria menjelang tahun 2020. Walau bagaimanapun, kes malaria masih lagi berlaku dalam kalangan rakyat Malaysia terutamanya di Sabah dan Sarawak disebabkan oleh kedatangan ramai pekerja asing dari negara jiran berdekatan (Hussin et al. 2020; Yong