Antimalarial and β-hematin formation inhibitory activities of chromone derivatives
2
1
Issued Date
2019
Resource Type
Language
eng
Rights
Mahidol University
Rights Holder(s)
Faculty of Pharmacy Mahidol University
Suggested Citation
Chirattikan Maicheen, Jiraporn Ungwitayatorn, จิรภรณ์ อังวิทยาธร (2019). Antimalarial and β-hematin formation inhibitory activities of chromone derivatives. Retrieved from: https://repository.li.mahidol.ac.th/handle/123456789/49689
Title
Antimalarial and β-hematin formation inhibitory activities of chromone derivatives
Abstract
A series of chromone derivatives were evaluated as antimalarial and β-hematin
formation inhibitory activities. The in vitro antimalarial activity was evaluated using the
microculture radioisotope assay. The three most potent antimalarial compounds were 34, 36
and 39 with IC50 = 3.82, 0.95 and 4.87 μM, respectively. Compound 36, the most active,
showed higher potency than primaquine and tafenoquine. For β-hematin formation inhibitory
activity assay, the top six most potent compounds, 23-28 (IC50 = 1.41, 1.76, 2.30, 2.54, 4.60
and 3.69 μM, respectively) were more potent than chloroquine, dihydroartemisinin, and
mefloquine. The ability of chromone compounds to interact and form complex with heme was
investigated by the continuous variation technique (Job’s plot). Compounds 28, 38 and 42
interacted with heme with stoichiometric ratio of chromone:heme = 1:1, same ratio as
dihydroartemisinin. Compounds 3, 4, 23, 24, 27 and 43 showed the stoichiometric ratio = 1:2,
same as chloroquine and mefloquine and compound 36 showed stoichiometric ratio = 1:3.
Description
The 1st Pharmaceutical Sciences Asia Conference 2019 Theme : Pharmaceutical Sciences toward Health Innovation in the Disruptive Era. Bangkok Midtown Hotel, Thailand. August 22, 2019, page 30