1.Role of gonadotropin-releasing hormone on advancing rat puberty onset induced by estradiol
Chenfeng HUA ; Rong YANG ; Yuxin LLU ; Lina HUANG ; Li ZHANG ; Tianguang ZHANG ; Dongdong TLAN ; Jun ZHAO ; Zengming ZHAO ; Yimei WANG ; Shuangqing PENG
Chinese Journal of Pharmacology and Toxicology 2015;(2):260-264
OBJECTIVE To investigate the role of gonadotropin-releasing hormone (GnRH) in es-tradiol(E2 ) induced advance of puberty onset in rats. METHODS Postnatal day 18 SD rats were given a daily intragastric administration of corn oil or E2(50 μg.kg-1 ) for consecutive 5 d. The day of vaginal opening (VO), pathological changes in ovary and protein expression levels of GnRH, G protein-coupled receptor 54 ( GPR54) and phospholipase C ( PLC) in hypothalamus were observed. RESULTS As compared to corn oil controll group, VO was advanced by about 12.2 d, corpus luteum was observed in the ovary section, and the protein expression levels of GnRH,GPR54 and PLC in hypothalamus were significantly increased by 47%, 55% and 56% in E2 group, respectively. CONCLUSION E2 induced onset of puberty advance may be closely related to regulation of the expression of GnRH, GPR54 and PLC in hypothalamus.
2.Medicinal chemistry strategies towards the development of effective SARS-CoV-2 inhibitors.
Shenghua GAO ; Tianguang HUANG ; Letian SONG ; Shujing XU ; Yusen CHENG ; Srinivasulu CHERUKUPALLI ; Dongwei KANG ; Tong ZHAO ; Lin SUN ; Jian ZHANG ; Peng ZHAN ; Xinyong LIU
Acta Pharmaceutica Sinica B 2022;12(2):581-599
Novel therapies are urgently needed to improve global treatment of SARS-CoV-2 infection. Herein, we briefly provide a concise report on the medicinal chemistry strategies towards the development of effective SARS-CoV-2 inhibitors with representative examples in different strategies from the medicinal chemistry perspective.