The antileishmanial activity of novel oxygenated chalcones and their mechanism of action
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The antileishmanial activity of novel oxygenated chalcones and their mechanism of action. / Zhai, L; Chen, M; Blom, J; Theander, T G; Christensen, S B; Kharazmi, A.
I: Journal of Antimicrobial Chemotherapy, Bind 43, Nr. 6, 1999, s. 793-803.Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › fagfællebedømt
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TY - JOUR
T1 - The antileishmanial activity of novel oxygenated chalcones and their mechanism of action
AU - Zhai, L
AU - Chen, M
AU - Blom, J
AU - Theander, T G
AU - Christensen, S B
AU - Kharazmi, A
N1 - Keywords: Animals; Antiprotozoal Agents; Chalcone; Cricetinae; Drug Evaluation, Preclinical; Humans; Leishmania donovani; Leishmania major; Leishmaniasis, Cutaneous; Leishmaniasis, Visceral; Macrophages; Male; Mesocricetus; Mitochondria; Oxidoreductases; Respiration
PY - 1999
Y1 - 1999
N2 - Our previous studies have shown that licochalcone A, an oxygenated chalcone, has antileishmanial and antimalarial activities, and alters the ultrastructure and function of the mitochondria of Leishmania spp. parasites. The present study was designed to investigate the antileishmanial activity and the mechanism of action of a group of new oxygenated chalcones. The tested oxygenated chalcones inhibited the in-vitro growth of Leishmania major promastigotes and Leishmania donovani amastigotes. Treatment of hamsters infected with L. donovani with intraperitoneal administration of two oxygenated chalcones resulted in a significant reduction of parasite load in the liver and the spleen compared with untreated control animals. The oxygenated chalcones also inhibited the respiration of the parasite and the activity of mitochondrial dehydrogenases. Electron microscopic studies illustrated that they altered the ultrastructure of the mitochondria of L. major promastigote. The data clearly indicate that this group of oxygenated chalcones has a strong antileishmanial activity and might be developed into a new antileishmanial drug. The antileishmanial activity of oxygenated chalcones might be the result of interference with function of the parasite mitochondria.
AB - Our previous studies have shown that licochalcone A, an oxygenated chalcone, has antileishmanial and antimalarial activities, and alters the ultrastructure and function of the mitochondria of Leishmania spp. parasites. The present study was designed to investigate the antileishmanial activity and the mechanism of action of a group of new oxygenated chalcones. The tested oxygenated chalcones inhibited the in-vitro growth of Leishmania major promastigotes and Leishmania donovani amastigotes. Treatment of hamsters infected with L. donovani with intraperitoneal administration of two oxygenated chalcones resulted in a significant reduction of parasite load in the liver and the spleen compared with untreated control animals. The oxygenated chalcones also inhibited the respiration of the parasite and the activity of mitochondrial dehydrogenases. Electron microscopic studies illustrated that they altered the ultrastructure of the mitochondria of L. major promastigote. The data clearly indicate that this group of oxygenated chalcones has a strong antileishmanial activity and might be developed into a new antileishmanial drug. The antileishmanial activity of oxygenated chalcones might be the result of interference with function of the parasite mitochondria.
M3 - Journal article
C2 - 10404318
VL - 43
SP - 793
EP - 803
JO - Journal of Antimicrobial Chemotherapy
JF - Journal of Antimicrobial Chemotherapy
SN - 0305-7453
IS - 6
ER -
ID: 7695364