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喹啉衍生物增强人类精子活力并提高功能能力。

Quinoline Derivative Enhances Human Sperm Motility and Improves the Functional Competence.

机构信息

Department of Clinical Embryology, Kasturba Medical College, Manipal, Manipal Academy of Higher Education, Manipal, Karnataka, 576 104, India.

Department of Studies in Chemistry, Karnatak University, Dharwad, Karnataka, 580 003, India.

出版信息

Reprod Sci. 2021 May;28(5):1316-1332. doi: 10.1007/s43032-020-00382-5. Epub 2020 Nov 25.

Abstract

In this study, we aimed to explore the beneficial properties of novel quinoline derivatives on human sperm motility and its functional competence. Nine novel quinoline derivatives were screened for their effect on motility in human spermatozoa from normozoospermic ejaculates. Compounds with impressive sperm motility enhancement properties were further assessed for their effect on functional competence of human spermatozoa. To determine the effect on the fertilizing ability of spermatozoa processed with quinoline derivatives and to assess developmental competence of embryos derived, in vitro fertilization (IVF) was performed using mouse model. Among the nine quinoline derivatives, 2 compounds (6MQT and 2,6DQT) exhibited significant enhancement in sperm progressive motility and survival at 24 h. Further, non-significant increase in curvilinear velocity (VCL), straight line velocity (VSL), and amplitude of lateral head displacement (ALH) was observed. Capacitation, intracellular cAMP level and tyrosine phosphorylated sperm proteins were significantly higher in 6MQT (P < 0.05) and 2,6DQT (P < 0.001) compared to control. In vitro fertilization (IVF) experiments using Swiss albino mice revealed that spermatozoa processed with 6MQT had non-significantly higher blastocyst rate and a superior blastocyst quality, while, 2,6DQT resulted in significantly lower blastocyst rate (P < 0.05) compared to control. Quinoline derivative 6MQT has significant motility enhancement property under in vitro conditions. Graphical abstract.

摘要

在这项研究中,我们旨在探索新型喹啉衍生物对人精子运动能力及其功能能力的有益特性。从正常精子中筛选了 9 种新型喹啉衍生物,以研究它们对人精子运动的影响。对具有显著精子运动增强特性的化合物进行了进一步评估,以研究它们对人精子功能能力的影响。为了确定用喹啉衍生物处理的精子的受精能力的影响,并评估胚胎的发育能力,使用小鼠模型进行了体外受精(IVF)。在这 9 种喹啉衍生物中,有 2 种化合物(6MQT 和 2,6DQT)在人精子的渐进性运动和 24 小时存活率方面表现出显著增强。此外,观察到曲线速度(VCL)、直线速度(VSL)和头部侧向位移幅度(ALH)的非显著增加。与对照组相比,6MQT(P<0.05)和 2,6DQT(P<0.001)中的精子获能、细胞内 cAMP 水平和酪氨酸磷酸化精子蛋白显著升高。使用瑞士白化病小鼠进行的体外受精(IVF)实验表明,用 6MQT 处理的精子具有非显著更高的囊胚率和更高质量的囊胚,而 2,6DQT 导致囊胚率显著降低(P<0.05)与对照组相比。喹啉衍生物 6MQT 在体外条件下具有显著的运动增强特性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/85b3/8076127/ab45f20256ec/43032_2020_382_Figa_HTML.jpg

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