Echinacoside Increases Sperm Quantity in Rats by Targeting the Hypothalamic Androgen Receptor

Scientific Reports
Zhihui JiangXiaoying Zhang

Abstract

Male infertility is a major health issue with an estimated prevalence of 4.2% of male infertility worldwide. Our early work demonstrated that Cistanche extracts protect against sperm damage in mice and that echinacoside (ECH) is one of the major active components. Here we report an essential role for ECH, a natural product that reverses or protects against oligoasthenospermia in rats. ECH was assayed by HPLC, the quantity and quality of sperm was evaluated and hormone levels were determined by radioimmunosorbent assay. ECH reduced levels of androgen receptor (AR) and key steroidogenic-related genes as determined by Western blot and qPCR analysis. The interaction between ECH and AR were evaluated by indirect ELISA and molecular docking. The results show that ECH combined with hypothalamic AR in the pocket of Met-894 and Val-713 to inhibit transfer of AR from the cytoplasm to nuclei in the hypothalamus. While negative feedback of sex hormone regulation was inhibited, positive feedback was stimulated to increase the secretion of luteinizing hormone and testosterone subsequently enhancing the quantity of sperm. Taken together, these data demonstrate that ECH blocks AR activity in the hypothalamus to increase the quantity of sperm a...Continue Reading

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Citations

Aug 4, 2019·Environmental Science and Pollution Research International·Ahmed Hamed ArishaMohamed M A Hussein
Feb 2, 2021·Medicinal Research Reviews·Yuelin SongPengfei Tu
Nov 15, 2020·Biomedicine & Pharmacotherapy = Biomédecine & Pharmacothérapie·Zi-Ying WangMin Li

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Methods Mentioned

BETA
ELISA
nuclear translocation
PCR
Protein Assay

Software Mentioned

Autodock
ChemBio 3D Ultra
SPSS
Graph Pad Prism
ChemBioDraw Ultra
GraphPad
PyMOL
Vina
AutoDockTools

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