Synthesis and biological activity of pyridine acylhydrazone derivatives of isopimaric acid.

Pyridine acylhydrazone derivatives of isopimaric acid were synthesized and characterized. The minimum inhibitory concentrations of the compounds against five bacteria were determined and most of the compounds displayed some degree of antibacterial activity. The results showed that antimicrobial activity against Streptococcus pneumoniae improved when halogen atoms were introduced into the isopimaric acid, especially when one bromine atom was introduced in the para-position of isopimaric acid. Compound isopimaric acid (5-bromo pyridine-2-formaldehyde) acylhydrazone exhibited a significant antitumorial activity against hepatocarcioma cells (HepG-2) and breast cancer cells (MDA-MB-231), with inhibition degrees of 74.21% and 70.39%, respectively, at 100 µM.[Formula: see text].

Signaling related with biphasic effects of bisphenol A (BPA) on Sertoli cell proliferation: a comparative proteomic analysis.

BACKGROUND: Biphasic effects on cell proliferation of bisphenol A (BPA) can occur at lesser or greater exposures. Sertoli cells play a pivotal role in supporting proliferation and differentiation of germ cells. The mechanisms responsible for inverse effects of great and low concentrations of BPA on Sertoli cell proliferation need further study. METHODS: We utilized proteomic study to identify the protein expression changes of Sertoli TM4 cells treated with 10(-8)M and 10(-5)M BPA. The further mechanisms related to mitochondria, energy metabolism and oxidative stress were investigated by qRT-PCR and Western-blotting analysis. RESULTS: Proteomic studies identified 36 proteins and two major clusters of proteins including energy metabolism and oxidative stress expressed with opposite changes in Sertoli cells treated with 10(-8)M and 10(-5)M BPA, respectively, for 24h. Exposure to 10(-5)M BPA resulted in greater oxidative stress and then inhibited cell proliferation, while ROS scavenger NAC effectively blocked these effects. Exposure to 10(-8)M BPA caused higher intercellular ATP, greater activities of mitochondria, and resulted in significant proliferation of TM4 cells, while oligomycin A, an inhibitor of ATP synthase, abolished these growth advantages. CONCLUSIONS: Our study demonstrated that micromolar BPA inhibits proliferation of Sertoli cells by elevating oxidative stress while nanomolar BPA stimulates proliferation by promoting energy metabolism. GENERAL SIGNIFICANCE: Micromolar BPA inhibits cell proliferation by elevating oxidative stress while nanomolar BPA stimulates cell proliferation by promoting energy metabolism.

Molecular and Cytogenetic Characterization of a Powdery Mildew-Resistant Wheat-Aegilops mutica Partial Amphiploid and Addition Line.

Aegilops mutica Boiss., a diploid species (2n = 2x = 14, TT), has been rarely studied before. In this research, a hexaploid wheat (cv. Chinese Spring)-Ae. mutica partial amphiploid and a wheat-Ae. mutica addition line were characterized by chromosome karyotyping, FISH using oligonucleotides Oligo-pTa535-1, Oligo-pSc119.2-1, and (GAA)8 as probes, and EST-based molecular markers. The results showed that the partial amphiploid strain consisted of 20 pairs of wheat chromosomes and 7 pairs of Ae. mutica chromosomes, with both wheat 7B chromosomes missing. EST-based molecular marker data suggested that the wheat-Ae. mutica addition line carries the 7T chromosome. Resistance tests indicated that both the partial amphiploid and the 7T addition line were highly resistant to powdery mildew, whereas the wheat control line Chinese Spring was highly susceptible, indicating the presence of a potentially new powdery mildew resistance gene on the Ae. mutica 7T chromosome. The karyotype, FISH patterns, and molecular markers can now be used to identify Ae. mutica chromatin in a wheat background, and the 7T addition could be used as a new powdery mildew resistance source for wheat breeding.

[Protective Effects of Ginkgolide N Against Glutamate-Induced Injury in PC12 Cells].

OBJECTIVE: To study the protective effects of ginkgolide N against glutamte-induced injury in PC12 cells and its mechanisms. METHODS: The injury model was established by treating PC12 cells with glutamate, and PC12 cells were treated with different concentrations of ginkgolide N with ginkgolide B as control. The cells activity was analyzed by MTT assay. The apoptosis of PC12 cells were examined by acridine orange( AO) staining, the reactive oxygen species and mitochondrial membrane potential of PC12 cells were examined by flow cytometry. Western blot method was used to examine the expression of Cleaved Caspase-3 protein. RESULTS: Ginkgolides N of 2-8 µgmol/L inhibited PC12 cells apoptosis and ROS accumulation induced by glutamate,stabilized membrane potential of damaged PC12, and reduced the expression of Cleaved Caspase-3 protein. CONCLUSION: Ginkgolide N has a protective effect on PC12 cells injury induced by glutamate, and the mechanism may be associated with reducing ROS generation, stabilizing membrane potential and inhibiting the expression of Cleaved Caspase-3 protein.

[Research on survey analysis and development strategies of traditional Chinese preparations in Guangdong Province hospitals].

OBJECTIVE: To provide reference for the government to formulate policies and medical institution to formulate development plan, the present situation of medical institutions of traditional Chinese preparation and some countermeasures for developing the research of traditional Chinese preparation in Guangdong province were studied. METHODS: Combined with development situation of traditional Chinese preparation of medical institutions in Guangdong province in recent years, the development countermeasure of traditional Chinese preparation was discussed. RESULTS: In order to promote the development of traditional Chinese preparation of medical institutions, suggestions and countermeasures for the government and related departments were proposed. CONCLUSION: Government departments should formulate policies to support the development of traditional Chinese preparation, the medical institutions should make scientific development planning, strengthen the construction of hardware and software and develop special traditional Chinese preparation to promote the healthy development of traditional Chinese preparation.

Succession of endophytic bacterial community and its contribution to cinnamon oil production during cinnamon shade-drying process.

Cinnamon oil is a blend of secondary metabolites and is widely used as spice. Endophytic bacteria are always related to the secondary metabolites production. However, the potential of endophytic bacteria communities for cinnamon oil production during cinnamon shade-drying process is still not clear. In this study, we investigated the composition and metabolic function of endophytic bacterial community during 80-day shade-drying process. The temporal dynamics of essential oil content and its dominant constituents were analyzed. The succession of endophytic bacterial community from d0 to d80 was identified. The influence of endophytic bacterial community evolution on cinnamon oil is significant positive. Predictive functional analysis indicated that shade-drying process was rich in Saccharopolyspora that produce enzymes for the conversion of phenylalanine to cinnamaldehyde. These findings enhance our understanding of the functional bacterial genera and functional genes involved in the production of cinnamon oil during cinnamon shade-drying process.

Pollutant removal from municipal sewage by a microaerobic up-flow oxidation ditch coupled with micro-electrolysis.

The development of efficient and low-cost wastewater treatment processes remains an important challenge. A microaerobic up-flow oxidation ditch (UOD) with micro-electrolysis by waterfall aeration was designed for treating real municipal wastewater. The effects of influential factors such as up-flow rate, waterfall height, reflux ratio, number of stages and iron dosing on pollutant removal were fully investigated, and the optimum conditions were obtained. The elimination efficiencies of chemical oxygen demand (COD), ammonia nitrogen (NH4 +-N), total nitrogen (TN) and total phosphorus (TP) reached up to 84.33 ± 2.48%, 99.91 ± 0.09%, 93.63 ± 0.60% and 89.27 ± 1.40%, respectively, while the effluent concentrations of COD, NH4 +-N, TN and TP were 20.67 ± 2.85, 0.02 ± 0.02, 1.39 ± 0.09 and 0.27 ± 0.02 mg l-1, respectively. Phosphorous removal was achieved by iron-carbon micro-electrolysis to form an insoluble ferric phosphate precipitate. The microbial community structure indicated that carbon and nitrogen were removed via multiple mechanisms, possibly including nitrification, partial nitrification, denitrification and anammox in the UOD.

Suppression of Esophageal Cancer Stem-like Cells by SNX-2112 Is Enhanced by STAT3 Silencing.

Many studies have demonstrated that cancer stem cells (CSCs) or tumor-initiating cells (TICs) are responsible for tumor cell proliferation, chemotherapy resistance, metastasis, and relapse in various cancers. We, and others, have previously shown that the signal transducer and activator of transcription 3 (STAT3) signaling pathway is responsible for CSCs and TICs growth. Recent reports have indicated that the heat shock protein 90 (Hsp90) is also essential for the survival of CSCs and TICs. SNX-2112 is an Hsp90 inhibitor. However, it remains unclear whether proliferation of esophageal cancer stem-like cells (ECSLCs) is suppressed by SNX-2112 with knockdown of STAT3 (shSTAT3). Here, we explored the association between SNX-2112 with shSTAT3 and the suppression of ECSLCs growth. We found that the expression level of both STAT3 and p-STAT3 was higher in clinical esophageal cancer tissue than in the adjacent normal tissue, using western blot and qPCR analysis. Furthermore, differential expression analysis demonstrated that STAT3 was overexpressed in clinical specimens. We demonstrated that SNX-2112 inhibited cancer cell proliferation, decreased ABCB1 and ABCG2 gene expression levels and reduced the colony formation capacity of ECSLCs, which was enhanced by STAT3 silencing. Flow cytometry analysis revealed that the combination of SNX-2112 and shSTAT3 significantly induced apoptosis and cell cycle arrest at G2/M phase in ECSLCs. Levels of proliferation pathway proteins, including p38, c-Jun N-terminal kinase (JNK), and extracellular signal-regulated kinase (ERK) which were also client proteins of Hsp90, were also reduced. In addition, SNX-2112 with shSTAT3 inhibited the proliferation of ECSLCs in vivo. Finally, STAT3 overexpression eliminated the apoptotic and antiproliferative effects of SNX-2112 on ECSLCs. Hence, these results provide a rationale for the therapeutic potential of the combination of SNX-2112 with shSTAT3 in esophageal cancer, and may indicate new targets for clinical intervention in human cancer.

1,4a,7-Trimethyl-7-vinyl-1,2,3,4,4a,4b,5,6,7,8,10,10a-dodeca-hydro-phenanthrene-1-carboxylic acid.

The title compound, also known as isopimaric acid, C(20)H(30)O(2), was isolated from slash pine rosin. There are two unique mol-ecules in the unit cell. The two cyclo-hexane rings have classical chair conformations. The cyclo-hexene ring represents a semi-chair. The mol-ecular conformation is stabilized by weak intra-molecular C-H⋯O hydrogen-bonding inter-actions. The mol-ecules are dimerized through their carboxyl groups by O-H⋯O hydrogen bonds, forming R(2) (2)(8) rings.

1,4a,7-Trimethyl-7-vinyl-1,2,3,4,4a,4b,5,6,7,9,10,10a-dodeca-hydro-phenanthrene-1-carboxylic acid.

The title compound, pimaric acid, C(20)H(30)O(2), was isolated from a mixture of resin acids. There are three rings in the structure. The two cyclo-hexane rings have classical chair conformations with trans-fused ring junctions. The cyclo-hexene ring appears as a semi-chair.

(E)-(4-Chloro-benzyl-idene){[(1R,4aS,10aR)-7-isopropyl-1,4a-dimethyl-1,2,3,4,4a,9,10,10a-octa-hydro-1-phenanthryl]-methyl}amine.

The title compound, C(27)H(34)ClN, has been synthesized from 4-chloro-benzaldehyde and dehydro-abietylamine. There are two unique mol-ecules in the unit cell. Each mol-ecule has three chiral centres, which exhibit R, S and R absolute configurations. The two cyclo-hexane rings form a trans ring junction with classical chair and half-chair conformations.

[Study on effects of curcumin on expressions of PDGF-BB, PDGFRbeta and ERK1 of HSC].

OBJECTIVE: To observe the effects of curcumin on expression of PDGF-BB, PDGFRbeta and ERK1 of rat Hepatic stellate cell (HSC-T6). METHODS: The cultured HSC were divided into control group, each curcumin treating group. The influence of curcumin on HSC proliferation was detected by MTT assay. The protein levels of PDGF-BB, PDGFRbeta and ERK1 was detected by immunhistochemical examination; The influence of curcumin on expression of PDGF-BB, PDGFRbeta and ERK1 mRNA was detected by RT-PCR. RESULTS: Immunohistiochemical results showed that normal cultured HSC-T6 cell expressed PDGF-BB, PDGFRbeta and ERK1 remarkably. After the intervention of different concentration of curcumin,the masculine degrees of PDGF-BB, PDGFRbeta and ERK1 and the masculine cell population decreased obviously. The RT-PCR results indicated that the expressions of PDGF-BB, PDGFRbeta and ERK1 mRNA could be obviously seen in control and TGF-beta1 stimulus group. After the intervention of different concentration of curcumin, the expression of PDGF-BB, PDGFRbeta and ERK1 mRNA decreased in a dose-dependent manner. CONCLUSION: Curcumin could inhibit the expression of PDGF-BB, PDGFRbeta and ERK1 which might be the mechanism of action curcumin on anti-fibrosis.

(E)-N'-(2-Hydroxy-benzyl-idene)-3,4,5-trimethoxy-benzohydrazide.

The title compound, C(17)H(18)N(2)O(5), was synthesized from 3,4,5-trimethoxy-benzohydrazide and 2-hydroxy-benzaldehyde. The dihedral angle between the planes of the two benzene rings is 29.9 (2)°. The crystal structure involves intra-molecular O-H⋯N, and inter-molecular N-H⋯O and C-H⋯O hydrogen bonds.

(E)-N'-(5-Bromo-2-hydroxy-benzyl-idene)-3,4,5-trimethoxy-benzohydrazide.

The mol-ecule of the title compound, C(17)H(17)BrN(2)O(5), assumes an E configuration, with the 5-bromo-2-hydroxy-phenyl and benzohydrazide units located on opposite sites of the C=N double bond. The dihedral angle between the planes of the two benzene rings is 32.48 (15)°. The crystal structure is stabilized by intra-molecular O-H⋯N and inter-molecular N-H⋯O hydrogen bonds.

(E)-N'-(4-Chloro-benzyl-idene)-3,4,5-trimethoxy-benzohydrazide.

The title compound, C(17)H(17)ClN(2)O(4), was synthesized from 3,4,5-trimethoxy-benzohydrazide and 4-chloro-benzaldehyde. In the crystal structure, packing is stabilized by intramolecular C-H⋯O and inter-molecular N-H⋯O and C-H⋯O hydrogen-bonding inter-actions.

An efficient synthesis method targeted to a novel aziridine derivative of p-menthane from turpentine and its herbicidal activity.

A novel aziridine compound N-acetyl-1,2-azacyclo-p-menthane d was synthesised using turpentine as raw material and characterised by FT-IR, 1H NMR, 13C NMR, ESI+-MS and HRMS. The pre-emergence herbicidal activities of d and its synthetic intermediates cis- and trans-N,N'-diacetyl-p-menthane-1,8-diamine (b2 and b1) were determined. The result showed that d exhibited much higher herbicidal activities against annual ryegrass, Digitaria sanguinalis and Ixeris denticulate than b2 and b1. The IC50 of d against the root and shoot growth of these three plants were lower than 1 mmol L-1. In contrast, the IC50 of b1 and b2 against the root and shoot growth of these plants were more than 10 mmol L-1.

Rapid and Sensitive Determination of the Major Steroidal Saponins of Ypsilandra thibetica Franch by Ultra High-Performance Liquid Chromatography Coupled with Triple Quadrupole Mass Spectrometry.

A rapid and validated method using ultra high-performance liquid chromatography coupled with a triple quadrupole mass spectrometry (UHPLC-QQQ MS) was developed for simultaneous determination of four active steroidal saponins, i.e., dichotomin ( 1: ), pennogenin 3-O-α-l-arabinofuranosyl-(1→4)-[α-l-rhamnopyranosyl-(1→2)]-ß-d-glucopyranoside ( 2: ), pennogenin 3-O-α-l-rhamnopyranosyl-(1→2)-[α-l-rhamnopyranosyl-(1→4)-α-l-rhamnopyranosyl-(1→4)]-ß-d-glucopyranoside ( 3: ) and diosgenin 3-O-α-l-rhamnopyranosyl-(1→2)-[α-l-rhamnopyranosyl-(1→4)-α-l-rhamnopyranosyl-(1→4)]-ß-d-glucopyranosidein ( 4: ), in Ypsilandra thibetica Franch. The optimized sample preparation and UHPLC-QQQ MS conditions were chosen for quantitative analysis. The separation was performed on an Agilent Zorbax Eclipse Plus C18 column (2.1 mm × 50 mm, 1.8 µm) with gradient elution of acetonitrile-0.1% formic acid in water. All calibration curves showed good linear regression (r> 0.9985) within the test range. The limits of detection and quantification were in the range of 0.02-4.40 and 0.04-22.0 ng/mL, respectively. The proposed method was applied to analyze two batches of Y. thibetica samples for target compounds within 10 min. This work promoted the quality control method for raw material or preparations of Y. thibetica.

[Primary investigation on the changing mode of plasma specific IgG antibody in SARS patients and their physicians and nurses].

OBJECTIVES: To primarily investigate the changing mode of anti-SARS coronavirus IgG antibody in clinically diagnosed SARS patients and the possibility of subclinical infection in physicians and nurses through close association with SARS patients. METHODS: The plasma levels of anti-SARS coronavirus IgG antibody of 57 normal subjects, 127 physicians and nurses worked in SARS wards for one month and 73 SARS patients with different course of SARS were measured by enzyme linked immunosorbent assay. RESULTS: Plasma anti-SARS coronavirus IgG antibody was not detected in normal subjects and the clinical personnel. After 0-7 days, 8-10 days, 11-14 days, 15-20 days of onset of disease, the positive rates were 0.33%, 52%, 86% respectively, and the general positive rate was 61%. CONCLUSION: The specificity and sensitivity of ELISA to detect plasma anti-SARS IgG antibody were satisfactory. Cases with positive reaction could be diagnosed as patients already infected by the virus. The specific IgG antibody didn't emerge in some patients in the early stage of the disease, and the negative results didn't indicate that they were not infected. And follow-up investigation should be made in those patients. Unlike common epidemic infectious diseases, SARS probably hadn't the potentiality of subclinical infection.

[Pathologic study of circulating blood leukocytes in severe acute respiratory syndrome].

OBJECTIVE: To study the pathologic characteristics and pathogenesis of circulating blood leucocytes infected by severe acute respiratory syndrome associated coronavirus (SARS CoV or SCV) in SARS patients. METHODS: Blood samples of 22 SARS patients were studied, and 4 healthy blood samples were observed as negative controls. The white blood cells were collected from whole blood. The ultrastructural characteristics were observed by transmission electron microscopy. CD45RO antibody was used for pre-embedding immunoelectron microscopy. The SARS viral sequence was detected with real-time polymerase chain reaction (RT-PCR). RESULTS: Coronavirus-like particles were founded in the leukocytes in 6 of the 22 blood samples. Five of them gave positive results in the real-time PCR. The number of granulocytes was increased (P < 0.05) and that of lymphocytes was decreased (P < 0.05) respectively. Immunoelectron microscopy showed that CD45RO positive T lymphocyte decreased to 6% - 7%. Circulating lymphocytes had the highest percentage of infection. The morphologic characteristics of coronavirus-like particles were spherical or oval in shape, about 80 - 120 nm in diameter, with a dense round core and a clear halo around the core. A distinct membrane and club-shaped surface projections were seen in the periphery. The particles were located in the cytoplasm, the cisternae of endoplasmic reticulum, Golgi apparatus and vesicles. Virus entered cells by endocytosis or membrane fusion and was released through a budding process. CONCLUSION: Our data suggested that lymphocytes, particularly T cells, were probably the target cells of SARS CoV. The viruses may actively infected the immune cells during SARS CoV acute infection phase and the destruction of target cells may be one of the important reasons for the death of the circulating leukocytes in SARS.

[Autophagy inhibitor 3-MA decreases the production and release of infectious enterovirus 71 particles].

OBJECTIVE: To determine whether or not enterovirus 71 (enteroviurs 71, EV71) may induce autophagy and affect the production and release of EV71 after the treatment of autophagy inhibitor. METHODS: Western blots were performed to examine the conversion of LC3-I to LC3- II and the degradation of P62 after the RD-A cells were infected with EV71. CCID50 was determined by checking the virus titer in the supernatant of cells that treated with autophagy inhibitor 3-MA. RESULTS: EV71 infection enhances the type conversion of LC3 and degradation of P62. The infectious virus particles were decreased after the treatment of 3-MA. CONCLUSION: EV71 infection could induce cell autophagy and the autophagy might contribute to the production and release of infectious EV71 particles.