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8-羟基喹啉的抗活性及其与两性霉素B脱氧胆酸盐对……的协同作用

anti- activity of 8-hydroxyquinoline and its synergistic effect with amphotericin B deoxycholate against .

作者信息

Chanmol Wetpisit, Siriyasatien Padet, Intakhan Nuchpicha

机构信息

School of Allied Health Sciences, Walailak University, Nakhon Si Thammarat, Thailand.

Research Excellence Center for Innovation and Health Product, Walailak University, Nakhon Si Thammarat, Thailand.

出版信息

PeerJ. 2022 Jan 18;10:e12813. doi: 10.7717/peerj.12813. eCollection 2022.

DOI:10.7717/peerj.12813
PMID:35111411
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8781311/
Abstract

() is responsible for visceral leishmaniasis in patients with no known underlying immunodeficiency, and visceral or disseminated cutaneous leishmaniasis in HIV-infected patients. The available anti- drugs for treatment have limitations such as high toxicity and variable efficacy. To improve the therapeutic index of anti- drugs, the search for a new drug or a new natural compound in combination therapy instead of using monotherapy to reduce drug side effect and have high efficacy is required. In this study, anti- activity of 8-hydroxyquinoline (8HQN) and its synergistic effect with amphotericin B (AmB) against were evaluated for the first time. These results showed that 8HQN presented anti- activity against with IC 1.60 ± 0.28 and 1.56 ± 0.02 µg/mL for promastigotes and intracellular amastigotes, respectively. The selectivity index (SI) value of 8HQN was 79.84 for promastigotes and 82.40 for intracellular amastigotes, which highlight promising results for the use of 8HQN in the treatment of -infected host cells. Interestingly, four combinations of 8HQN and AmB provided synergistic effects for intracellular amastigotes and showed no toxic effects to host cells. These results provided information of using a combination therapy in treating this species leads to further development of therapy and can be considered as an alternative treatment for leishmaniasis.

摘要

(某病原体)在无已知潜在免疫缺陷的患者中引起内脏利什曼病,在感染HIV的患者中引起内脏或播散性皮肤利什曼病。现有的抗该病原体药物存在局限性,如毒性高和疗效不一。为提高抗该病原体药物的治疗指数,需要寻找新药物或新天然化合物用于联合治疗,而非单一疗法,以减少药物副作用并提高疗效。在本研究中,首次评估了8-羟基喹啉(8HQN)对该病原体的活性及其与两性霉素B(AmB)的协同作用。这些结果表明,8HQN对该病原体具有活性,前鞭毛体和细胞内无鞭毛体的IC分别为1.60±0.28和1.56±0.02μg/mL。8HQN对前鞭毛体的选择性指数(SI)值为79.84,对细胞内无鞭毛体为82.40,这突出了8HQN在治疗该病原体感染宿主细胞方面的良好结果。有趣的是,8HQN和AmB的四种组合对细胞内无鞭毛体具有协同作用,且对宿主细胞无毒性作用。这些结果为使用联合疗法治疗该病原体物种提供了信息,有助于进一步开发治疗方法,并可被视为利什曼病的替代治疗方法。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dacc/8781311/0981d972627f/peerj-10-12813-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dacc/8781311/007714675b5d/peerj-10-12813-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dacc/8781311/44685f87e3a4/peerj-10-12813-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dacc/8781311/ae4689cb48e5/peerj-10-12813-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dacc/8781311/0981d972627f/peerj-10-12813-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dacc/8781311/007714675b5d/peerj-10-12813-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dacc/8781311/44685f87e3a4/peerj-10-12813-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dacc/8781311/ae4689cb48e5/peerj-10-12813-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dacc/8781311/0981d972627f/peerj-10-12813-g004.jpg

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