Cellular uptake and intracellular activity of antibiotics against Haemophilus influenzae type b.

Cellular uptake and intracellular activity of antibiotics against Haemophilus influenzae type b.
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针对 b 型流感嗜血杆菌的抗生素的细胞摄取和细胞内活性。

DOI:
10.1093/infdis/145.2.152
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发表时间:
1982
期刊:
The Journal of infectious diseases
影响因子:
--
通讯作者:
Smith,AL
Smith,AL
中科院分区:
--
文献类型:
--
作者:
Jacobs,RF;Wilson,CB;Laxton,JG;Haas,JE;Smith,AL

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本文研究了青霉素和氯霉素进入人多形核白细胞(PMNLs)的能力及其对B型流感嗜血杆菌的抗菌活性。青霉素被排除,而氯霉素集中在PMNL;氯霉素摄取不依赖于PMNL能量,并且不受未标记药物的竞争性抑制。吞噬调理素H.培养24小时后,检测B型流感病毒。电镜下观察到PMNLs中有B型流感病毒。这些PMNLs含有104.5个H.流感病毒B型添加4倍、10倍或40倍最低杀菌浓度(MBC)的青霉素或氨苄青霉素可使该密度从104.5cfu降至103.5cfu。相比之下,以MBC的四倍添加氯霉素将密度降低至~ 100 cfu;以MBC的10倍添加氯霉素将密度降低至~10 cfu。因此,脂溶性抗生素如氯霉素被浓缩,并且在PMNL内具有生物活性。这种抗生素在细胞水平上可能具有显著的优势。
The ability of penicillins and chloramphenicol to enter human polymorphonuclear leukocytes (PMNLs) and their antibacterial activity against intracellularHaemophilus influenzaetype b were studied. Penicillin was excluded whereas chloramphenicol was concentrated in PMNLs; chloramphenicol uptake was not dependent on PMNL energy and was not competitively inhibited by unlabeled drug. PMNLs that had phagocytized opsonizedH. influenzaetype b were examined after incubation for 24 hr. In the absence of antibiotics, intact intracellularH. influenzaetype b organisms were observed in PMNLs by electron microscopy. These PMNLs contained 104.5colony-forming units (cfu) ofH. influenzaetype b. Addition of penicillin or ampicillin at four, 10, or 40 times the minimal bactericidal concentration (MBC) decreased this density from 104.5to 103.5cfu. In contrast, addition of chloramphenicol at four times the MBC reduced the density to ~lO0 cfu; at 10 times the MBC it reduced the density to ~10 cfu. Thus, lipidsoluble antibiotics such as chloramphenicol are concentrated and are bioactive within PMNLs. Such antibiotics may have a significant advantage at the cellular level.
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