Estradiol Benzoate is a HBx protein inhibitor and inhibits androgen and hepatitis B virus (HBV) transcription, replication. Estradiol Benzoate shows antifertility effects, anti- Toxoplasma gondii activity and can improve memory behavior of Ovariectomy (Ovx) female mice[1][2][3][4].
Estradiol Benzoate (0-500µM; 48h) delays or stops the cell cycle of tachyzoites by blocking progression from G1 to S phase in HFF cells[1]. Estradiol Benzoate (35-75µM; 2d) significantly reduced the production of HBeAg, HBsAg, HBV pgRNA, and HBV DNA in HepG2 cells in a dose-dependent manner and inhibited HBV activity[2].
After male mice were exposed to Estradiol Benzoate (5, 10mg/kg, SC), as the concentration of Estradiol Benzoate increased, the number of TUNEL-positive cells in the testes of Estradiol Benzoate-treated mice significantly increased, and pro-apoptotic factors (Fas, TNF, Cytochrome C , Apaf1, Chop, Caspase-3, Caspase-8, Caspase-9 and Caspase-12) and estrogen receptor (ER) signaling pathway key genes (ER α, ER β, Erk1/2, Hsp90 and DAX-1) The mRNA expression level of was significantly up-regulated in the testis of the treatment group[3]. In an ovariectomy model, Estradiol Benzoate (20-200µg/kg for 4-5weeks) effectively normalised ovariectomy-induced changes in female rats, including a reduction in the width of the synaptic gap, an expansion in the thickness of the postsynaptic dense substance (PSD) and an increase in the number of presynaptic mid-synaptic vesicles in the Fr1 and hippocampal CA1 regions of the cerebral cortex[4].
References:
[1]. Lu D, Zhang N Z, Yao Y, et al. Investigation of antiparasitic activity of two marine natural products, estradiol benzoate, and octyl gallate, on Toxoplasma gondii in vitro[J]. Frontiers in Pharmacology, 2022, 13: 841941.
[2]. He J, Wu J, Chen J, et al. Identification of estradiol benzoate as an inhibitor of HBx using inducible stably transfected HepG2 cells expressing HiBiT tagged HBx[J]. Molecules, 2022, 27(15): 5000.
[3]. Lei X, Cui K, Liu Q, et al. Exogenous estradiol benzoate induces spermatogenesis disorder through influencing apoptosis and oestrogen receptor signalling pathway[J]. Reproduction in domestic animals, 2016, 51(1): 75-84.
[4]. Xu X, Zhang Z. Effects of estradiol benzoate on learning-memory behavior and synaptic structure in ovariectomized mice[J]. Life sciences, 2006, 79(16): 1553-1560.
Estradiol Benzoate是一种HBx蛋白抑制剂，可抑制雄激素和乙型肝炎病毒(HBV)的转录和复制。Estradiol Benzoate具有抗生育作用、抗弓形虫活性，并能改善卵巢切除(Ovx)雌性小鼠的记忆行为[1][2][3][4]。
Estradiol Benzoate（0-500µM；48h）通过阻断HFF细胞从G1期到S期的进展来延迟或停止弓形虫速殖子的细胞周期[1]。Estradiol Benzoate（35-75µM；2d）以剂量依赖性的方式显著降低HepG2 细胞中HBeAg、HBsAg、HBV pgRNA和HBV DNA的产生，并抑制 HBV活性[2]。
雄性小鼠暴露于Estradiol Benzoate（5、10mg/kg）后，随着Estradiol Benzoate浓度的增加，Estradiol Benzoate组小鼠睾丸中TUNEL阳性细胞数显著增加，促凋亡因子(Fas、TNF、细胞色素C、Apaf1、Chop、Caspase-3、Caspase-8、Caspase-9和Caspase-12)和雌激素受体(ER)信号通路关键基因(ERα、ERβ、Erk1/2、Hsp90和DAX-1)的mRNA表达水显著上调[3]。在卵巢切除模型中，Estradiol Benzoate（20-200µg/kg，4-5weeks）有效地使雌性大鼠卵巢切除引起的变化正常化，包括减少突触间隙的宽度，扩大突触后致密物（PSD）的厚度，并增加大脑皮层Fr1和海马CA1区突触前中突触小泡的数量[4]。