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V9302（一种跨膜谷氨酰胺通量竞争性拮抗剂）对乳腺癌细胞系耐药逆转的影响

Impact of V9302, a Competitive Antagonist of Transmembrane Glutamine Flux on Reversal of Resistance in Breast Cancer Cell Lines.

作者信息

Szemerédi Nikoletta, Schelz Zsuzsanna, Horvath Dária Antónia, Rácz Bálint, Szatmári András G, Muddather Hiba F, Bózsity Noémi, Zupkó István, Spengler Gabriella

机构信息

Department of Medical Microbiology, Albert Szent-Györgyi Health Center and Albert Szent-Györgyi Medical School, University of Szeged, Semmelweis utca 6, 6725 Szeged, Hungary.

Institute of Pharmacodynamics and Biopharmacy, Faculty of Pharmacy, University of Szeged, Eötvös utca. 6, 6720 Szeged, Hungary.

出版信息

Pharmaceutics. 2024 Jun 29;16(7):877. doi: 10.3390/pharmaceutics16070877.

DOI:10.3390/pharmaceutics16070877
PMID:39065573
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11280048/
Abstract

Chemotherapy is a known treatment modality that improves the long-term survival of breast cancer patients. However, due to the resistance to numerous anticancer drugs, alternative chemotherapeutic strategies are required. Regarding antimetabolic drugs, several compounds have proven anticancer properties, such as statins. The present study aimed to investigate the in vitro effects of V9302, a competitive antagonist of glutamine flux, on different subtypes of breast cancers (estrogen, progesterone, and HER2 receptor-positive or negative, and Pgp-negative and Pgp-overexpressing). The interactions of V9302 with standard chemotherapeutic drugs (doxorubicin and cisplatin) were also determined by MTT staining on breast cancer cell lines. Furthermore, the influence of V9302 on the cell cycle of MCF-7 and its Pgp-overexpressing counterpart KCR was monitored by flow cytometry. It was shown that V9302 exerted synergistic interactions with doxorubicin in all breast cancer cell lines. In cell cycle analysis, the KCR cell line was more sensitive to V9302. After 48 h, cell proliferation was completely blocked, and elevated G1, suppressed S, and decreased G2/M could be detected. Inhibition of glutamate transport can be assumed to block resistance related to Pgp.

摘要

化疗是一种已知的治疗方式，可提高乳腺癌患者的长期生存率。然而，由于对多种抗癌药物存在耐药性，需要 alternative chemotherapeutic strategies。关于抗代谢药物，有几种化合物已被证明具有抗癌特性，如他汀类药物。本研究旨在研究谷氨酰胺通量的竞争性拮抗剂V9302对不同亚型乳腺癌（雌激素、孕激素和HER2受体阳性或阴性，以及Pgp阴性和Pgp过表达）的体外作用。还通过MTT染色在乳腺癌细胞系上确定了V9302与标准化疗药物（阿霉素和顺铂）的相互作用。此外，通过流式细胞术监测V9302对MCF-7及其Pgp过表达对应物KCR细胞周期的影响。结果表明，V9302在所有乳腺癌细胞系中均与阿霉素产生协同相互作用。在细胞周期分析中，KCR细胞系对V9302更敏感。48小时后，细胞增殖完全受阻，可检测到G1期升高、S期受抑制和G2/M期降低。可以推测，抑制谷氨酸转运可阻断与Pgp相关的耐药性。 （注：“alternative chemotherapeutic strategies”这里原英文表述有误，推测可能是“alternative chemotherapeutic strategies”，直译为“替代化疗策略”，但从语境看可能是“其他化疗策略”之类更通顺的表达）

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/40d5/11280048/fbd8b747dd95/pharmaceutics-16-00877-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/40d5/11280048/f2beed91cab9/pharmaceutics-16-00877-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/40d5/11280048/c7b8a99a8b37/pharmaceutics-16-00877-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/40d5/11280048/e83a146fa7b2/pharmaceutics-16-00877-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/40d5/11280048/fbd8b747dd95/pharmaceutics-16-00877-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/40d5/11280048/f2beed91cab9/pharmaceutics-16-00877-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/40d5/11280048/c7b8a99a8b37/pharmaceutics-16-00877-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/40d5/11280048/e83a146fa7b2/pharmaceutics-16-00877-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/40d5/11280048/fbd8b747dd95/pharmaceutics-16-00877-g004.jpg

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