Anion Exchange Protein 1, Erythrocyte ; metabolism ; Breast ; metabolism ; pathology ; surgery ; Cadherins ; metabolism ; Female ; Fibrocystic Breast Disease ; metabolism ; pathology ; surgery ; Follow-Up Studies ; Humans ; Middle Aged ; S100 Proteins ; metabolism

UNLABELLEDTo study the effect of S-3307 on the yield and main ingredients of Alisma plantago-aquatica.

METHODThe contents of 24-acetyl alisol A and the 23-acetyl alisol B in tuber were determined by HPLC.

RESULTSThe contents of 24-acetyl alisol A and the 23-acetyl alisol B as well as yield were significantly increased in all groups applied with different concentrations of S-3307 comparing with control group. The optimal concentration of S-3307 was 80 mg x kg(-1). The residues of S-3307 was detected under 0.316 8 mg x kg(-1) (detecting limit).

CONCLUSIONThe optimal concentration of S-3307 is 80 mg x kg(-1), it reached the best result when applied 36 d after seedling.

Alisma ; chemistry ; drug effects ; growth & development ; Cholestenones ; analysis ; Chromatography, High Pressure Liquid ; Plant Growth Regulators ; pharmacology

To explore an efficient strategy for further development of anticancer fluoroquinolone candidates derived from ciprofloxacin, a heterocyclic ring as the bioisosteric replacement of C3 carboxyl group led to a key intermediate, oxadiazole thiol (5), which was further modified to the bis-oxadiazole methylsulfides (7a-7h) and the corresponding dimethylpiperazinium iodides (8a-8h), respectively. Structures were characterized by elemental analysis and spectra data, and their anticancer activities in vitro against CHO, HL60 and L1210 cancer cells were also evaluated by MTT assay. The preliminary results show that piperazinium compounds (8) possess more potent activity than that of corresponding free bases (7).
Animals ; Antineoplastic Agents ; chemical synthesis ; chemistry ; pharmacology ; CHO Cells ; Cell Line, Tumor ; Cell Proliferation ; drug effects ; Ciprofloxacin ; chemistry ; Cricetinae ; Cricetulus ; Drug Design ; HL-60 Cells ; Humans ; Inhibitory Concentration 50 ; Leukemia L1210 ; Molecular Structure ; Oxadiazoles ; chemical synthesis ; chemistry ; pharmacology ; Piperazines ; chemical synthesis ; chemistry ; pharmacology

An efficient modified route based on the targeting mechanism of antibacterial fluoroquinolones for the shift from the antibacterial activity to the antitumor one was further developed. Using a fused heterocyclic ring, s-triazolothiadiazine as a carboxyl bioisostere of ciprofloxacin, the title compounds, 1-cyclopropyl-6-fluoro-7-piperazin-1-yl-3-(6-substituted-phenyl-7H-[1, 2, 4]triazolo[3, 4-b][1, 3, 4]thiadiazin-3-yl)-quinolin-4(1H)-ones (5a-5e) and their corresponding N-acetyl products (6a-6e), were designed and synthesized, separately. Meaningfully, a ring-contraction of fused six-membered thiadiazine occurred by a sulfur extrusion reaction gave new tri-acetylated fused heterocycles related to pyrazolo[5, 1-c][1, 2, 4] triazoles (7a-7e). The in vitro antitumor activity against L1210, CHO and HL60 cell lines was also evaluated for the synthesized fifteen heterocycles compared to parent ciprofloxacin by methylthiazole trazolium (MTT) assay. Interestingly, the results displayed that fifteen fused heterocyclic compounds showed more significant growth inhibitory activity (IC50 < 25.0 micromo x L(-1)) than that of parent ciprofloxacin (IC50 > 150.0 micromol x L(-1)), and the active order decreased from 7a-7e to 5a-5e to 6a-6e, respective.
Animals ; Antineoplastic Agents ; chemical synthesis ; chemistry ; pharmacology ; CHO Cells ; Cell Line, Tumor ; Ciprofloxacin ; pharmacology ; Cricetinae ; Cricetulus ; Fluoroquinolones ; chemical synthesis ; chemistry ; pharmacology ; HL-60 Cells ; Humans ; Inhibitory Concentration 50 ; Leukemia L1210 ; pathology ; Mice ; Structure-Activity Relationship ; Thiadiazines ; chemical synthesis ; chemistry ; pharmacology ; Triazoles ; chemical synthesis ; chemistry ; pharmacology

Objective To find out whether conversation analysis helps to differentiate psychogenic nonepileptic seizure (PNES) from epileptic seizure in Chinese patients.Methods Twelve unselected patients from Peking Union Medical College Hospital during 2014 to 2016 with diagnostic uncertainty were included.Interactions following standard protocol were carried out.A linguist blinded to all medical data and a neurologist studied videos and transcripts of the interactions.Using a diagnostic scoring aid which includes 17 conversation features summarized from previous researches, they attempted to predict the medical diagnosis of those patients independently.Results Accurate diagnosis was predicted in 10/12 patients by both raters.Average scores of patients with epileptic seizures were 8.00 (linguist) and 6.75 (neurologist), while average scores of paitents with PNES were-5.75 (linguist) and-7.88 (neurologist).Both raters agreed on most individual items (81.86%, 167/204).To demonstrate different features between these two groups, a case comparison was made between one patient with frontal lobe epilepsy and one patient with PNES.Conclusion In Chinese patients, conversation analysis can help differentiate between epileptic seizure and PNES.

OBJECTIVETo observe the expression and distribution of adult rat axon guidance cues Netrin-1 and Slit2 at different time points after spinal cord injury and to investigate the guidance mechanism of regenerated axons.

METHODSTwenty adult Sprague Dawley (SD) rats were divided randomly into five groups with 4 in each. Four groups of them were used to make Allen's spinal cord punch models and we took materials randomly from one of them on the 2nd, 4th, 7th and 14th day respectively after operation. The left one group was taken as the control group. Immunofluorescence laser confocal scan was used to examine the co-expression and localization of Netrin-1 and Slit2 proteins in the injured site of the spinal cord.

RESULTSWithin two weeks after SCI, the expression of Netrin-1 and Slit2 proteins increased temporarily and there was co-expression of them on the neuron plasma membrane.

CONCLUSIONSSynchronous high expression and co-expression of axon attractant Netrin-1 and repellent Slit2 are found in the adult rat injured spinal cord in the damaged local and vicinity parts, and probably, they act as the key regulators of axon guidance regeneration.

Animals ; Female ; Intercellular Signaling Peptides and Proteins ; analysis ; Male ; Microscopy, Confocal ; Nerve Growth Factors ; analysis ; Nerve Regeneration ; physiology ; Nerve Tissue Proteins ; analysis ; Netrin-1 ; Random Allocation ; Rats ; Rats, Sprague-Dawley ; Spinal Cord Injuries ; metabolism ; Tumor Suppressor Proteins ; analysis

BACKGROUND:Endoplasmic reticulum stress participates in the occurrence and development of many diseases, such as atherosclerosis, diabetes, and Alzheimer’s disease. GRP78 is a marker of endoplasmic reticulum stress. The expression of GRP78 reflects the degree of endoplasmic reticulum stress.
OBJECTIVE:To investigate the effect of cyclic stretch on GRP78 expression of L6 rat myoblasts, and to identify the relationship between cyclic stretch and endoplasmic reticulum stress.
METHODS:In vitro culture-tensile stimulation models of myoblasts of L6 rats were established successful y. The expression of GRP78 of myoblasts exposed to cyclic stretch was determined by reverse transcription-PCR and western blot assay. Stretch groups were subjected to 15%surface elongation at a frequency of 10 cycles per minute, over a period of 1, 6, 12 and 24 hours. cells were simultaneously seeded on a plate in the control and experimental groups with no stimulation.
RESULTS AND CONCLUSION:The expression of GRP78 mRNA was continuously elevated over time after stretched treatment, and significant differences were detected as compared with the control group (P<0.05). GRP78 protein expression began to increase at 1 hour after stretched treatment, was significantly increased at 6 hours, peaked at 24 hours, and significant differences were visible as compared with the control group (P<0.05). In conclusion, cyclic stretch induced the occurrence of endoplasmic reticulum stress, which was enhanced with prolonged time. However, prolonged stretch caused severe endoplasmic reticulum stress and leaded to apoptosis of myoblasts.

BACKGROUND:The adaptive reconstruction of maxil ofacial muscles would happen when functional orthopedic treatment is done to cure micromaxil ary deformity. The myoblast is the main responder in the process of adaptive reconstruction, and cyclic stretch can induce apoptosis of myoblasts. Caspase-9 is an important factor in the mitochondrial apoptosis pathway.
OBJECTIVE:To investigate the expression of Caspase-9 in different cyclic stretch.
METHODS:Based on myoblasts cultured in vitro-mechanical stimulation model, the rat L6 myoblasts were loaded stretch for 1, 6, 12 and 24 hours through multi-channel cellstress loading system, while the control group received no stretch. The morphological change and growth of myoblasts were observed under inverted phase contrast microscope;the expression of the mRNA and protein of Caspase-9 were detected by RT-PCR and western blot analysis, respectively.
RESULTS AND CONCLUSION:Under inverted phase contrast microscope, the rat L6 myoblasts at cyclic stretch maintained a good growth state and biological characteristics;there was no celldegeneration;and the loss rate was extremely low, which could demonstrate that myoblast in vitro-mechanical stimulation model was established successful y. The results of RT-PCR and western blot analysis showed that, the expression of Caspase-9 mRNA and Cleaved Caspase-9 protein was significantly increased as the loading time prolonged, and the expression of Procaspase-9 protein was significantly decreased as the time. We can conclude that Caspase-9 is involved in the mechanical signal transduction of cyclic stretch.

AIMTo study the expression pattern of the retinoic acid metabolizing enzymes RALDH2 and CYP26b1 during mouse postnatal testis development at both mRNA and protein levels.

METHODSReal-time polymerase chain reaction and Western blot analysis were performed to determine the relative quantity of RALDH2 and CYP26b1 at both mRNA and protein levels at postnatal day 1, 5, 10, 20, and in adult mice (70 days testes). Testicular localization of RALDH2 and CYP26b1 during mouse postnatal development was examined using immunohistochemistry assay.

RESULTSAldh1a2 transcripts and its protein RALDH2 began to increase at postnatal day 10, and remained at a high level through postnatal day 20 to adulthood. Cyp26b1 transcripts and CYP26b1 protein did not change significantly during mouse postnatal testis development. RALDH2 was undetectable in the postnatal 1, 5 and 10 day testes using immunohistochemistry assay. At postnatal day 20 it was detected in pachytene spermatocytes. Robust expression of RALDH2 was restricted in round spermatids in the adult mouse testis. In the developing and adult testis, CYP26b1 protein was confined to the peritubular myoepithelial cells.

CONCLUSIONOur results indicate that following birth, the level of retinoic acid in the seminiferous tubules might begin to increase at postnatal day 10, and maintain a high level through postnatal day 20 to adulthood.

Aldehyde Oxidoreductases ; genetics ; metabolism ; Animals ; Cytochrome P-450 Enzyme System ; genetics ; metabolism ; Gene Expression Regulation, Developmental ; Male ; Mice ; Mice, Inbred BALB C ; RNA, Messenger ; metabolism ; Rabbits ; Retinoic Acid 4-Hydroxylase ; Seminiferous Epithelium ; cytology ; metabolism ; Sensitivity and Specificity ; Spermatids ; cytology ; metabolism ; Testis ; cytology ; growth & development ; metabolism

OBJECTIVETo investigate the effect of "Xuebijing injection" (Xuebijing in brief) on expression of hepatic high mobility group box-1 protein (HMGB1) and acute liver injury in rats with scald injury.

METHODSSeventy-eight rats were divided into sham scald group (n = 18), scald group (n = 30), and Xuebijing treatment group (n = 30). Rats in the latter 2 groups were subjected to 30% full-thickness scald injury followed with delayed resuscitation. These rats were sacrificed at 8th, 24th, and 72nd post-injury hour (PIH) to collect specimens. The hepatic pathological changes were observed. Serum levels of ALT and AST were detected. HMGB1 mRNA level in hepatic tissue was detected by the reverse transcription polymerase chain reaction. Protein relative expression quantity of HMGB1 in hepatic tissue was determined with Western blot and immunohistochemistry. Outcomes were denoted in integral absorbance ratio and absorbance value respectively.

RESULTSMassive infiltration of inflammatory cells in hepatic tissues was observed in scald group under light microscope, especially at 24th PIH, and it was decreased in quantity in Xuebijing treatment group. Compared with those of sham scald group, both mRNA and protein expressions of HMGB1 in hepatic tissue of scald group were significantly enhanced during 8-72 PIH (P < 0.05 or P < 0.01), along with markedly increased serum levels of ALT and AST (P < 0.05 or P < 0.01). Compared with those in scald group at 24h and 72nd PIH, hepatic HMGB1 mRNA expressions (0.75 +/- 0.12 vs. 0.60 +/- 0.15 and 0.78 +/- 0.11 vs. 0.55 +/- 0.07, respectively) and protein values (200 +/- 13 vs. 163 +/- 13 and 175 +/- 14 vs. 160 +/- 16, respectively) in Xuebijing treatment group were markedly down-regulated (P < 0.05 or P < 0.01), and serum levels of ALT and AST decreased in different degrees (P < 0.05 or P < 0.01).

CONCLUSIONSHMGB1, the delay-appearing inflammatory mediator, is involved in the pathogenesis of inflammatory response in hepatic tissue in severely scalded rats. Treatment with Xuebijing can markedly down-regulate hepatic HMGB1 expression and protect liver against acute injury induced by delayed resuscitation.

Animals ; Burns ; drug therapy ; metabolism ; pathology ; Drugs, Chinese Herbal ; pharmacology ; HMGB1 Protein ; metabolism ; Liver ; pathology ; Male ; Phytotherapy ; RNA, Messenger ; genetics ; Rats ; Rats, Wistar