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将特非那定重新用作新型抗贾第虫化合物。

Repurposing Terfenadine as a Novel Antigiardial Compound.

作者信息

Suárez-Rico Daniel Osmar, Munguía-Huizar Francisco Javier, Cortés-Zárate Rafael, Hernández-Hernández José Manuel, González-Pozos Sirenia, Perez-Rangel Armando, Castillo-Romero Araceli

机构信息

Departamento de Fisiología, Centro Universitario de Ciencias de la Salud, Universidad de Guadalajara, Calle Sierra Mojada 950, Independencia Oriente, Guadalajara 44340, Mexico.

Departamento de Microbiología y Patología, Centro Universitario de Ciencias de la Salud, Universidad de Guadalajara, Sierra Mojada 950, Col. Independencia, Guadalajara 44340, Mexico.

出版信息

Pharmaceuticals (Basel). 2023 Sep 21;16(9):1332. doi: 10.3390/ph16091332.

DOI:10.3390/ph16091332
PMID:37765140
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10535608/
Abstract

is a highly infectious protozoan that causes giardiasis, a gastrointestinal disease with short-term and long-lasting symptoms. The currently available drugs for giardiasis treatment have limitations such as side effects and drug resistance, requiring the search for new antigiardial compounds. Drug repurposing has emerged as a promising strategy to expedite the drug development process. In this study, we evaluated the cytotoxic effect of terfenadine on trophozoites. Our results showed that terfenadine inhibited the growth and cell viability of trophozoites in a time-dose-dependent manner. In addition, using scanning electron microscopy, we identified morphological damage; interestingly, an increased number of protrusions on membranes and tubulin dysregulation with concomitant dysregulation of were observed. Importantly, terfenadine showed low toxicity for Caco-2 cells, a human intestinal cell line. These findings highlight the potential of terfenadine as a repurposed drug for the treatment of giardiasis and warrant further investigation to elucidate its precise mechanism of action and evaluate its efficacy in future research.

摘要

是一种高度传染性的原生动物，可引起贾第虫病，这是一种具有短期和长期症状的胃肠道疾病。目前用于治疗贾第虫病的药物存在副作用和耐药性等局限性，需要寻找新的抗贾第虫化合物。药物重新定位已成为加快药物开发过程的一种有前景的策略。在本研究中，我们评估了特非那定对滋养体的细胞毒性作用。我们的结果表明，特非那定以时间-剂量依赖性方式抑制滋养体的生长和细胞活力。此外，使用扫描电子显微镜，我们发现了形态学损伤；有趣的是，观察到膜上突起数量增加以及微管蛋白失调，并伴有 失调。重要的是，特非那定对人肠道细胞系Caco-2细胞显示出低毒性。这些发现突出了特非那定作为一种重新定位用于治疗贾第虫病的药物的潜力，并值得进一步研究以阐明其确切作用机制并在未来研究中评估其疗效。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d0b/10535608/7f63195495d4/pharmaceuticals-16-01332-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d0b/10535608/4bf33dfdcb79/pharmaceuticals-16-01332-g0A1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d0b/10535608/93b63df46a51/pharmaceuticals-16-01332-g0A2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d0b/10535608/05bd0e8e726f/pharmaceuticals-16-01332-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d0b/10535608/6ab1726639ae/pharmaceuticals-16-01332-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d0b/10535608/cb2a3463f70b/pharmaceuticals-16-01332-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d0b/10535608/b025df4d74fd/pharmaceuticals-16-01332-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d0b/10535608/821a164f24b7/pharmaceuticals-16-01332-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d0b/10535608/2cc243354d27/pharmaceuticals-16-01332-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d0b/10535608/3f69350ec9e4/pharmaceuticals-16-01332-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d0b/10535608/7f63195495d4/pharmaceuticals-16-01332-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d0b/10535608/4bf33dfdcb79/pharmaceuticals-16-01332-g0A1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d0b/10535608/93b63df46a51/pharmaceuticals-16-01332-g0A2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d0b/10535608/05bd0e8e726f/pharmaceuticals-16-01332-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d0b/10535608/6ab1726639ae/pharmaceuticals-16-01332-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d0b/10535608/cb2a3463f70b/pharmaceuticals-16-01332-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d0b/10535608/b025df4d74fd/pharmaceuticals-16-01332-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d0b/10535608/821a164f24b7/pharmaceuticals-16-01332-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d0b/10535608/2cc243354d27/pharmaceuticals-16-01332-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d0b/10535608/3f69350ec9e4/pharmaceuticals-16-01332-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d0b/10535608/7f63195495d4/pharmaceuticals-16-01332-g008.jpg

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