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首页> 外文期刊>Journal of Inorganic Biochemistry: An Interdisciplinary Journal >Characterisation of synthetic beta-haematin and effects of the antimalarial drugs quinidine, halofantrine, desbutylhalofantrine and mefloquine on its formation.
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Characterisation of synthetic beta-haematin and effects of the antimalarial drugs quinidine, halofantrine, desbutylhalofantrine and mefloquine on its formation.

机译：合成β-haematin的表征以及抗疟药奎尼丁，氟替林，去丁基氟替丁和甲氟喹对其形成的影响。

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Infrared spectroscopy, elemental analysis and X-ray powder diffraction showed that the product of 30 minutes of reaction of haematin in 4.5 M acetate, pH 4.5 at 60deg C was identical to beta-haematin prepared in 4.5 M acetic acid at 70deg C overnight (pH2.6). There was no evidence for formation of haem-acetate complex, which could not be isolated, even from 11.4 M acetate solution. Quinidine, halofantrine, desbutylhalofantrine and mefloquine inhibited formation of beta-haematin, whereas 5-, 6- and 8-aminoquinolines and quinoline had no effect. Quinidine formed a complex with ferriprotoporphyrin IX in 40% DMSO with log K=5.02±0.03. Log K values for halofantrine and desbutylhalofantrine were 5.29±0.02 and 5.15±0.02 respectively (solutions containing 30%acetonitrile in addition to DMSO to solubilise these drugs), which are both stronger than chloroquine under the same conditions (log K=4.56±0.02).
机译：红外光谱，元素分析和X射线粉末衍射分析表明，血红素在4.5 M乙酸盐（pH为4.5的溶液中）在60℃下反应30分钟的产物与在4.5 M醋酸中在70℃过夜（pH2 .6）。没有证据表明形成血红素乙酸盐复合物，即使从11.4 M乙酸盐溶液中也无法分离出。奎尼丁，氟丁嘌呤，去丁基氟丁啶和甲氟喹抑制β-血红素的形成，而5-，6-和8-氨基喹啉和喹啉则无作用。奎尼丁与铁原卟啉IX在40％DMSO中形成络合物，log K = 5.02±0.03。氟丁汀和去丁基氟丁胺的Log K值分别为5.29±0.02和5.15±0.02（除了DMSO之外，还含有30％乙腈的溶液以溶解这些药物），在相同条件下均比氯喹强（log K = 4.56±0.02） 。

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