Synthesis, in vitro Antiplasmodial Activity and Cytotoxicity of Metalloporphyrins against Plasmodium falciparum K1 Strain

被引:3
|
作者
Radzuan, Nuur Haziqah Mohd [1 ]
Norazmi, Nur Aqilah Zahirah [1 ]
Ali, Amatul Hamizah [1 ]
Abu Bakar, Muntaz [1 ]
Agustar, Hani Kartini [2 ]
Abd Razak, Mohd Ridzuan Mohd [3 ]
Hassan, Nurul Izzaty [1 ]
机构
[1] Univ Kebangsaan Malaysia, Fac Sci & Technol, Dept Chem Sci, Ukm Bangi 43600, Selangor Darul, Malaysia
[2] Univ Kebangsaan Malaysia, Fac Sci & Technol, Dept Earth Sci & Environm, Ukm Bangi 43600, Selangor Darul, Malaysia
[3] Minist Hlth Malaysia, Natl Inst Hlth NIH Complex, Inst Med Res, Herbal Med Res Ctr, Shah Alam 40170, Selangor Darul, Malaysia
来源
SAINS MALAYSIANA | 2021年 / 50卷 / 10期
关键词
Antiplasmodial; cytotoxicity; in vitro; metalloporphyrin; P. falciparum K1; ANTIMALARIAL ACTIVITY; ARTEMISININ; COMPLEXES; MALARIA;
D O I
10.17576/jsm-2021-5010-09
中图分类号
O [数理科学和化学]; P [天文学、地球科学]; Q [生物科学]; N [自然科学总论];
学科分类号
07 ; 0710 ; 09 ;
摘要
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 (EC50) in a range of 21.4 to 36.0 mu M. Cytotoxic activities of NiDPP, ZnDHP and ZnTPP against Vero mammalian cells were in a non-toxic range of about 97 to 587 mu M. ZnDHP possessed the highest selectivity index value of 27.2 mu M, indicating that the compound's antiplasmodial effect was a selective plasmodial inhibition and non-toxic to the mammalian cells.
引用
收藏
页码:2945 / 2956
页数:12
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