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人血小板中的奎纳克林和碱性胺:亚细胞区室化及其对5-羟色胺的影响

Quinacrine and basic amines in human platelets: subcellular compartmentation and effects on serotonin.

作者信息

Costa J L, Fay D D, Kirk K L

出版信息

Res Commun Chem Pathol Pharmacol. 1984 Jan;43(1):25-42.

PMID:6701402
Abstract

Human platelets appear to accumulate quinacrine both in a thrombin-releasable compartment (dense bodies or amine storage vesicles) and in another compartment from which it is released by agents known to collapse pH gradients (possibly lysosomes with an acidic interior). Approximately 61% of the total amount of quinacrine present in human platelets resides in dense bodies and 14+ in lysosomes, with the remainder probably present in the cytoplasm. Other basic amines are accumulated in the three compartments to widely varying extents, suggesting that several factors besides the existence of pH gradients act to determine the distribution of these substances within the cell. The fluorescence emission of quinacrine excited with 420 nm light is completely quenched for quinacrine inside both dense bodies and lysosomes, and the absorption of 440 nm light is decreased by approximately 25%. Quinacrine added to dense bodies at 37 degrees C induces the efflux of 5-hydroxytryptamine (5HT) from the bodies. There is, however, no 5HT loss following quinacrine entry at 0 degree C, and the relationship between the two types of amine movement varies according to incubation time at 0 degree C and 37 degrees C. This action of quinacrine therefore does not appear to be associated with stoichiometric exchange of 5HT and quinacrine, but rather to modulation of the passive permeability of the dense body membrane for 5HT.

摘要

人类血小板似乎会在可被凝血酶释放的区室(致密体或胺储存囊泡)以及另一个区室中积累喹吖因,已知能破坏pH梯度的试剂可从该另一个区室释放喹吖因(可能是内部呈酸性的溶酶体)。人类血小板中存在的喹吖因总量中,约61%存在于致密体中,14%存在于溶酶体中,其余可能存在于细胞质中。其他碱性胺在这三个区室中的积累程度差异很大,这表明除了pH梯度的存在外,还有几个因素决定了这些物质在细胞内的分布。用420nm光激发时,致密体和溶酶体内的喹吖因的荧光发射完全淬灭,440nm光的吸收减少约25%。在37℃下添加到致密体中的喹吖因会诱导5-羟色胺(5HT)从致密体中流出。然而,在0℃时喹吖因进入后没有5HT损失,并且两种胺类物质移动之间的关系根据在0℃和37℃下的孵育时间而变化。因此,喹吖因的这种作用似乎与5HT和喹吖因的化学计量交换无关,而是与致密体膜对5HT的被动通透性调节有关。

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