Estrogen receptors (ERs) are members of nuclear receptors and related to several diseases such as cancer, inflammation and osteoporosis. ERs have two forms, ERα and ERβ, which have different functions and organism distributions. Compounds selectively targeting ERβ can regulate important physiological functions and avoid the side effects caused by targeting ERα. Therefore, selective ERβ ligands have received considerable research interest in recent years. In this article, different kinds of selective ERβ ligands were summarized and their structure-activity relationships were also analyzed.
Estrogen Receptor beta ; chemistry ; Humans ; Ligands ; Structure-Activity Relationship

OBJECTIVETo investigate the material base and underlying mechanism of the effect of cluster needling of scalp acupuncture on the neuronal plasticity in rats with focal cerebral infarction.

METHODSThe model rats with acute cerebral infarction were made by blocking the middle cerebral artery with monofilament. One hundred and thirty two Wistar rats were randomly divided into 4 groups: sham-operation group (A), model group (B), point-to-point scalp acupuncture group (C) and cluster-needling of scalp acupunture group (D). Puncturing from "Baihui (GV 20)" to "Qubin (GB 7)" was used in group C. Cluster needling of scalp acupuncture was used in group D, in which needles were inserted forward and slantingly into "Baihui (GV 20)" and its left and right sides at 4 mm. In both groups, the treatment was carried out with rapid twirling reinforcing-reducing for 1 min then retaining needle for 30 min, once a day, 6 days in one course, for treating 4 courses. There was no treatment for group A and B. The change of neurological function was evaluated with Bederson score, while the expression of microtubule-associated protein 2 (MAP-2) in the ischemic penumbra was examined with immunohistochemistry (streptavidin-peroxidase method).

RESULTSIn comparison,with group B, the score of neurological function in group D decreased on 7th day (P<0.05), while the scors in group C and D also decreased on 14th and 28th days (both P<0.05). As compared with group C, the score of neurological function in group D obviously decreased on 28th days (P<0. 05). Comparing with group B, the expression of MAP-2 on the ischemic cortex was significantly increased in group D and C on 7th, 14th and 28th days (all P<0. 05), however, this expression in group D was higher than that in group C on 14th and 28th days (P<0. 05).

CONCLUSIONCluster needling of scalp acupuncture can improve the neurological function of rats with focal cerebral infarction, and increase the expression of MAP-2 in the ischemic penumbra.

Acupuncture Therapy ; methods ; Animals ; Cerebral Infarction ; ethnology ; metabolism ; physiopathology ; therapy ; Disease Models, Animal ; Male ; Microtubule-Associated Proteins ; metabolism ; Random Allocation ; Rats ; Rats, Wistar ; Scalp

OBJECTIVETo investigate the ultrastructure and the alkaline phosphatase (ALP) activity changes of NIH3T3 cells incubated with secretive human bone morphogenetic protein-2 (hBMP-2) that is induced by gene transfection through transwell system.

METHODSEukaryotic expression vector (pcDNA3.1-B2) was transduced into NIH3T3 cells by Sofast, a positive compound transfection agent. The positive cell clones were selected with G418. The cytoplasmic and extracellular expression of BMP-2 in the NIH3T3 cells were determined by immunohistochemical and enzyme-linked immunosorbent assay (ELISA). NIH3T3 cells were co-cultured with hBMP-2 gene transfecting cells through transwell system, and the ultrastructure and ALP activity (the markers of osteogenetic differentiation) changes were observed.

RESULTSThere were cytoplasmic and extracellular expression of BMP-2 in transfecting NIH3T3 cells. The ultrastructure changes and the high expression of ALP suggested the osteogenetic differentiation tendency of NIH3T3 cells co-cultured with transfecting NIH3T3 cells.

CONCLUSIONSSecretive BMP-2 that is induced by gene transfection could promote the osteogenetic differentiation of fibroblast cells.

Alkaline Phosphatase ; metabolism ; Animals ; Bone Morphogenetic Protein 2 ; genetics ; Coculture Techniques ; Fibroblasts ; cytology ; ultrastructure ; Humans ; Mice ; NIH 3T3 Cells ; Osteogenesis ; Transfection

OBJECTIVETo set up thalassemia population intervention model in order to decrease the birth of thalassemia major, relying on population and family planning service system.

METHODSPregnant women and their husbands were educated about thalassemia, and participated in screening and prenatal diagnosis if the couple were carriers of thalassemia in the areas of Huangpu, Panyu, Zengcheng and Tianhe districts of Guangzhou.

RESULTSThe network of thalassemia intervention mainly dependent on family planning service system was set up in these regions. A total of 10 695 families participated in thalassemia screening and 16 thalassemia major fetuses were diagnosed in the last two years. No one was thalassemia major in the 8360 newborn.

CONCLUSIONThalassemia population intervention model was set up relying on family planning service system and it significantly decreased the birth of thalassemia major.

Family Planning Services ; methods ; Female ; Genetic Counseling ; Heterozygote ; Humans ; Infant, Newborn ; Male ; Mass Screening ; methods ; Pregnancy ; Prenatal Diagnosis ; methods ; Spouses ; Thalassemia ; diagnosis ; genetics ; prevention & control

Adolescent ; Adult ; Age Factors ; Aged ; Body Mass Index ; China ; epidemiology ; Fatty Liver ; diagnostic imaging ; epidemiology ; etiology ; Female ; Humans ; Male ; Mass Screening ; Middle Aged ; Prevalence ; Sex Factors ; Ultrasonography

Farnesoid X receptor (FXR) belongs to the nuclear receptor superfamily. It is highly related to the formation of metabolic syndrome and the glucose homeostasis, and therefore represents an important drug target against metabolic diseases and diabetes. In recent years, great progress has been made in the agonists, antagonists, and crystal structures of FXR. The diverse FXR ligands and their structure-activity relationship are reviewed in this article. The advances in the crystal structures of FXR in complex with different ligands are also introduced.
Animals ; Anticholesteremic Agents ; chemical synthesis ; chemistry ; pharmacology ; Azepines ; chemical synthesis ; chemistry ; pharmacology ; Benzene Derivatives ; chemical synthesis ; chemistry ; pharmacology ; Chenodeoxycholic Acid ; analogs & derivatives ; chemical synthesis ; chemistry ; pharmacology ; Crystallization ; Humans ; Indoles ; chemical synthesis ; chemistry ; pharmacology ; Isoxazoles ; chemical synthesis ; chemistry ; pharmacology ; Ligands ; Molecular Structure ; Multienzyme Complexes ; chemical synthesis ; chemistry ; pharmacology ; Pregnenediones ; chemical synthesis ; chemistry ; pharmacology ; Receptors, Cytoplasmic and Nuclear ; agonists ; antagonists & inhibitors ; metabolism ; Structure-Activity Relationship

BACKGROUNDBone morphogenetic proteins (BMPs), which belong to the transforming growth factor beta superfamily, are powerful regulators of cartilage and bone formation. This study investigated the biological changes of NIH3T3 cells incubated with secretive BMP2 that was induced by gene transfection through transwell.

METHODSEukaryonic expression vector (pcDNA3.1-B2) was transfered into NIH3T3 cells with Sofast, a positive compound transfection agent. The positive cell clones were selected with G418. The cytoplasmic and extracellular expressions of BMP2 were determined by immunohistochemical stain and enzyme-linked immunosorbent assay. NIH3T3 cells were co-cultured with hBMP2 gene transfecting cells through transwell, and the ultrastructure, alkaline phosphatase activity and the expression of osteocalcin (the marker of osteogenetic differentiation) changes were observed.

RESULTSThere were cytoplasmic and extracellular expressions of BMP2 in transfecting NIH3T3 cells. The ultrastructural changes, the high activity of alkaline phosphatase and the positive stain of osteocalcin suggested the osteogenetic differentiation tendency of NIH3T3 cells co-cultured with transfecting NIH3T3 cells.

CONCLUSIONSecretive BMP2 that is induced by gene transfection could promote the osteogenetic differentiation of fibroblast cells.

Alkaline Phosphatase ; metabolism ; Animals ; Bone Morphogenetic Protein 2 ; Bone Morphogenetic Proteins ; analysis ; genetics ; Cell Differentiation ; Enzyme-Linked Immunosorbent Assay ; Fibroblasts ; cytology ; Immunohistochemistry ; Mice ; Microscopy, Electron, Transmission ; NIH 3T3 Cells ; Osteocalcin ; analysis ; Osteogenesis ; Transfection ; Transforming Growth Factor beta ; analysis ; genetics

Aromatase is a key enzyme responsible for in vivo estrogen biosynthesis. Inhibition of the activity of the aromatase has become an alterative way for treatment of breast cancer. In this review, the structure and catalytic mechanism of the aromatase is briefly introduced followed by thorough review of the progress in the study of the steroidal and non-steroidal aromatase inhibitors. This review is focused on the natural compounds that exhibit the aromatase inhibition, which include flavonoids, xanthones, coumarins, and sesquiterpenes. The structure-activity relationship of these compounds is also discussed.
Androstenedione ; analogs & derivatives ; Antineoplastic Agents ; chemistry ; pharmacology ; therapeutic use ; Aromatase ; chemistry ; metabolism ; pharmacology ; Aromatase Inhibitors ; chemistry ; classification ; pharmacology ; therapeutic use ; Breast Neoplasms ; drug therapy ; Catalysis ; Coumarins ; chemistry ; pharmacology ; Estrogens ; biosynthesis ; Flavonoids ; chemistry ; pharmacology ; Humans ; Inhibitory Concentration 50 ; Nitriles ; chemistry ; pharmacology ; Sesquiterpenes ; chemistry ; pharmacology ; Structure-Activity Relationship ; Triazoles ; chemistry ; pharmacology ; Xanthones ; chemistry ; pharmacology

OBJECTIVETo investigate whether Candida albicans-native phospholipomannan (PLM) induce an inflammation response through Toll-like receptor(TLRé2 in human acute monocytic leukemia cell line (THP-1) cells.

METHODSHuman THP-1 monocytes were challenged with PLM in vitro. The mRNA expressions of TLR2, TLR4, proinflammatory cytokine [interleukin(IL)-6], and chemokine (IL-8) were assayed by real time reverse transcription polymerase chain reaction. The secretions of IL-6 and IL-8 were measured by enzyme-linked immunosorbent assay. The expression of TLR2 was analyzed with Western blot.

RESULTSPLM increased the mRNA expressions and secretions of proinflammatory cytokines (IL-6) and chemokines (IL-8) in THP-1 cells (all P=0.0000). PLM up-regulated the mRNA and protein levels of TLR2 (P=0.0000), whereas the mRNA level of TLR4 was not altered. PLM hydrolyzed with β-D-mannoside manno hydrolase failed to induce gene and protein expressions of TLR2, IL-6, and IL-8. Anti-TLRS-neutralizing antibody blocked the PLM-induced secretions of IL-6 and IL-8 in THP-1 cells (P = 0.0003, P = 0.0010).

CONCLUSIONCanidada albicans-native PLM may contribute to the inflammatory responses during Candida infection in a TLR2-dependent manner.

Candida albicans ; chemistry ; Cells, Cultured ; Glycolipids ; pharmacology ; Humans ; Interleukin-6 ; metabolism ; Interleukin-8 ; metabolism ; Monocytes ; drug effects ; immunology ; metabolism ; Toll-Like Receptor 2 ; metabolism ; Toll-Like Receptor 4 ; metabolism

Objective To investigate the relationship between the activation of RhoA and thrombin-induced neuron injury in the cortex of fetal rats. Methods The neurons from the fetal ratcortex were culturedin vitro for 8 d; and then,they were treated by thrombin at different concentrations (0,1,10,30 and 100 U/mL) for 3 h,and by 30 U/mL thrombm at different times (0,0.5,1,3 and 6 h);Western blotting was used to examine the effects of these different treatments on the activation of RhoA.The neurons were pretreated with Exoenzyme C3,the RhoA inhibitor,for 0.5 h,and incubated with 30 U/ml thrombin for 3 h; and then,Western blotting was employed to examine the activation of Rho A; besides that,the injuries of these neurons with the presence and absence of Exoenzyme C3 were observed by Hoechst33258 staining and CCK-8 assay.Results The activation of RhoA expressing in membrane with the treatment of 30 U/mL thrombin for 3 h was significantly increased as compared with that under the treatment of 0 U/mL (P＜0.05); and the total RhoA showed no significant changes with the treatment of all concentrations. The 3 h site with thrombin (30 U/mL) could more significantly induce R hoA expression as compared with other time sites (P＜0.05),and the total RhoA showed no significant changes under the treatment of all time sites. Pretreatrnent of neurons with Exoenzyme C3 could significantly down-regulate RhoA level as compared with those without pretreatment (P＜0.05); meanwhile,Hoechst33258 staining indicated that the number of brightly stained neurons in the Exoenzyme C3presence group was dramatically decreased as compared with that in the Exoenzyme C3 absence group (P＜0.05), and CCK-8 assay showed that the cell survival rate in Exoenzyme C3 absence group significantly decreased as compared with that in the Exoenzyme C3 presence group (P＜0.05).Conclusion RhoA in membrane is related to the thrombin-induced neuron injury in the cortex of fetal