Advances in research on anti-Müllerian tube hormone and male reproductive endocrine-related diseases / 基础医学与临床

Anti-Müllerian tube hormone(AMH), also known as Müllerian inhibitory substances, is a member of the transformation system. In males, AMH is secreted by immature Sertoli cell which promotes the degradation of male fetal Müllerian tubes,and participates in testicular development and spermatogenesis.AMH can regulate gona-dotropin-releasing hormone (GnRH), pituitary secretes follicle stimulating hormone (FSH) and luteinizing hormone (LH),testicular stromal cells secrete testosterone(T) and inhibin B causes male reproductive endocrine related diseases through HPG axis.

A new prospect in cancer therapy: targeting cancer stem cells to eradicate cancer / 癌症

According to the cancer stem cell theory, cancers can be initiated by cancer stem cells. This makes cancer stem cells prime targets for therapeutic intervention. Eradicating cancer stem cells by efficient targeting agents may have the potential to cure cancer. In this review, we summarize recent breakthroughs that have improved our understanding of cancer stem cells, and we discuss the therapeutic strategy of targeting cancer stem cells, a promising future direction for cancer stem cell research.

Synthesis of benzopyrano[3,4-c]pyridin-5-ones as dopamine D4 receptor ligands.

The dopamine D4 receptor is highly expressed in prefrontal cortex, hippocampus, amygdala, hypothalamus and is hypothesized to relate with the pathophysiology and pharmacotherapy of schizophrenia while its level in brain regions is much lower. To date, no specific ligand is available for the study of D4 receptor in vivo. In this study, we report the synthesis and in vitro receptor binding assay of three benzopyrano[3,4-c]pyridin-5-ones as potential dopamine D4 receptor ligands. These new compounds have higher affinity and selectivity toward dopamine D4 receptor and their K(i) values for D4 receptor are in the nanomolar (nM) range.

Biological evaluation of ~(18)F-FDTP as a potential dopamine D_4 receptor PET imaging agent / 中华核医学杂志

Objective To evaluate the feasibility of 3-(4-~(18)F-fluorobenzyl)-8,9-dimethoxy-1,2,3,4-tetrahydrochromeno [3,4-c]pyridin-5-one ( is F-FDTP) as a potential dopamine D4 receptor PET imaging agent.Methods ~(18)F-FDTP solution in ethanol-physiological saline was incubated with calf serum to test its in vitro stability through the determination of radiochemical purity.Normal rats were injected intravenously with ~(18)F-FDTP and then sacrificed at 2,5,10,15,30,60 and 120 min after anesthesia.Blood,organs and brain tissue samples were collected.All samples were weighed and measured for radioactivity.The uptake of samples was expressed as percentage activity of injection dose per gram of tissue ( % ID/g).Results The stability of ~(18)F-FDTP was satisfactory and its radiochemical purity was above 95% after incubation 120 min at 37℃ in calf serum.The biodistribution showed that ~(18)F-FDTP could penetrate through the blood-brain barrier and selectively accumulate in striatum,hypothalamus,frontal certex,hippocampus,cerebellum,where the D_4 receptor was reportedly located.The radioactivities in hippocampus,hypothalamus,striatum,frontal cortex,cerebellum,pons were (0.42±0.03),(0.46±0.05),(0.54±0.04),(0.39±0.04),(0.45±0.06),(0.35±0.04) %ID/g,respectively,2 min post injection.And there was difference between the normal biodistribution results and the blocking experimental results:(0.36 ±0.05),( 0.33±0.05 ),(0.55±0.05 ),(0.30±0.07 ),(0.34±0.07 ) and (0.32±0.04) % ID/g in hippocampus,hypothalamus,striatum,frontal cortex,cerebellum and pons,respectively.Conclusions ~(18)F-FDTP can penetrate through the blood-brain barrier and selectively accumulate in striatum,hypothalamus,frontal cortex,hippocampus,cerebellum,where the D_4 receptor was known to concentrate.These preliminary results suggest that ~(18)F-FDTP is a potential dopamine D_4 receptor imaging agent and further studies are needed.