Design, synthesis, characterization, and cytotoxicity activity evaluation of mono-chalcones and new pyrazolines derivatives

The development of resistance and side effects of chemotherapeutic drugs are common obstacles in the treatmentof cancer. With the expansion of health problems nowadays, there is a need to continuously develop new drugs thatare more efficient in targeting tumor cells and safe to normal cells. This study designed a series of new chalconesand pyrazoline derivatives based on their binding energy from the molecular docking study. The synthesis involvedClaisen–Schmidt condensation to form two chalcones, 1 and 2, which are then cyclized at room temperature to formeight new pyrazoline derivatives, 3–10. A one-pot reaction of acetophenone, 2-ethoxybenzaldehyde, and hydrazidederivatives (thiosemicarbazide and phenyl hydrazide) under reflux formed two new pyrazoline derivatives, 11 and12, without the isolation of chalcones. All the synthesized chalcones and pyrazolines were characterized using theFourier transform infrared spectroscopy–attenuated total reflectance and nuclear magnetic resonance (1D and 2D).The cytotoxicity activity of the chalcones and new pyrazoline compounds were investigated against breast cancercell lines (MCF-7 and MD-MB-231) and normal breast cell lines (MCF-10A). The results show that only compound7 showed the minimum inhibition against MCF-7 with IC50 6.50µM when exposed to the cell line for 24 hourscompared to the reference Gefitinib anticancer drug

Transcriptomic analysis in Anemone flaccida rhizomes reveals ancillary pathway for triterpene saponins biosynthesis and differential responsiveness to phytohormones / 中国天然药物

Anemone flaccida Fr. Schmidt is a perennial medicinal herb that contains pentacyclic triterpenoid saponins as the major bioactive constituents. In China, the rhizomes are used as treatments for a variety of ailments including arthritis. However, yields of the saponins are low, and little is known about the plant's genetic background or phytohormonal responsiveness. Using one-quarter of the 454 pyrosequencing information from the Roche GS FLX Titanium platform, we performed a transcriptomic analysis to identify 157 genes putatively encoding 26 enzymes involved in the synthesis of the bioactive compounds. It was revealed that there are two biosynthetic pathways of triterpene saponins in A. flaccida. One pathway depends on β-amyrin synthase and is similar to that found in other plants. The second, subsidiary ("backburner") pathway is catalyzed by camelliol C synthase and yields β-amyrin as minor byproduct. Both pathways used cytochrome P450-dependent monooxygenases (CYPs) and family 1 uridine diphosphate glycosyltransferases (UGTs) to modify the triterpenoid backbone. The expression of CYPs and UGTs were quite different in roots treated with the phytohormones methyl jasmonate, salicylic acid and indole-3-acetic acid. This study provides the first large-scale transcriptional dataset for the biosynthetic pathways of triterpene saponins and their phytohormonal responsiveness in the genus Anemone.

Cloning and expression analysis of GlPS1, GlPS2 gene in Glehnia littoralis / 中草药

Objective: To clone the full-length cDNA sequences of psoralen synthase (PS) genes from Glehnia littoralis so as to perform the bioinformatic and expression pattern analysis. Methods: Based on our previous transcriptome sequencing data of G. littoralis, the gene sequences GlPS1 and GlPS2 with high expression level were screened. The 3’cDNA ends of GlPS1 and GlPS2 genes were cloned by the RACE (rapid amplification of cDNA ends) method and the full-length cDNA of genes were assembled by using DNAMAN software. And then encoded GlPS proteins were analyzed by the bioinformatics tools. The issue specific expression of GlPS1 and GlPS2 genes were detected using qPCR. Results: The full-length cDNA of GlPS1 gene was 1 885 bp, which encoding a protein of 495 amino acids with a predicted molecular weight of 55 740.7 and isoelectric point of 8.28; The full-length cDNA of GlPS2 gene was 1 971 bp, which encoding a protein of 502 amino acids with a predicted molecular weight of 56 363.9 and isoelectric point of 6.62. GlPS1 and GlPS2 proteins belong to the cytochrome P450 superfamily, which share one transmembrane zone acting as hydrophilic protein. Phylogenetic analysis showed GlPS1 and GlPS2 were genetically closely related to the PS of Pastinaca sativa, Apium graveolens, Ammi majus. Higher expression of GlPS1 gene was observed in roots than leaves. However, GlPS2 gene was expressed at a relatively higher level in flowers than in roots. Conclusion: The full-length cDNA of GlPS1 and GlPS2 genes were obtained and the expression patterns were explored in G. littoralis for the first time, which provided a foundation for further studies on gene function and genetic regulatory mechanism of GlPS.

Síndrome poliglandular autoinmunitario tipo II (síndrome de Schmidt): enfermedad de Addison y tiroiditis de Hashimoto asociado con vitíligo / Polyglandular autoimmune syndrome type II (Schmidt syndrome): Addison's disease and Hashimoto's thyroiditis associated to vitiligo

Resumen Los síndromes poliglandulares autoinmunitarios son afecciones poco frecuentes que se distinguen por la coexistencia de al menos dos enfermedades glandulares autoinmunitarias. Se clasifican en tipo I (o juvenil) y tipos II y III (o del adulto). El tipo II o síndrome de Schmidt se caracteriza por enfermedad de Addison, enfermedad tiroidea autoinmunitaria o diabetes mellitus tipo 1 que pueden vincularse con otras alteraciones de naturaleza autoinmunitaria, como vitíli go, hepatitis autoinmunitaria, miastenia gravis, anemia perniciosa, enfermedad celiaca y alopecia areata, entre otras. Se comunica el caso de una paciente de 61 años de edad con vitíligo a quien se le diagnosticó enfermedad de Addison y tiroiditis de Hashimoto (síndrome de Schmidt).

Abstract Autoimmune polyglandular syndromes are rare conditions characterized by the coexistence of at least two autoimmune glandular diseases. They can be classified in type I (or juvenile) and type II and III (or adult). Type 2 or Schmidt's syndrome is characterized by Addison's disease, autoimmune thyroid disease and/or type 1 diabetes mellitus and may be associated with other disorders of autoimmune nature, such as vitiligo, autoimmune hepatitis, myasthenia gravis, pernicious anemia, celiac disease or alopecia areata, among others. We communicate the case of a 61 year-old woman with vitiligo diagnosed with Addison's disease and Hashimoto's thyroiditis (Schmidt's syndrome).

Evaluation of water quality at the source of streams of the Sinos River Basin, southern Brazil / Avaliacão da qualidade da água das nascentes de arroios da Bacia do Rio dos Sinos, região sul do Brasil

The Sinos River Basin (SRB) is located in the northeastern region of the state of Rio Grande do Sul (29º20' to 30º10'S and 50º15' to 51º20'W), southern Brazil, and covers two geomorphologic provinces: the southern plateau and the central depression. It is part of the Guaíba basin, has an area of approximately 800 km² and contains 32 counties. The basin provides drinking water for 1.6 million inhabitants in one of the most important industrial centres in Brazil. This study describes different water quality indices (WQI) used for the sub-basins of three important streams in the SRB: Pampa, Estância Velha/Portão and Schmidt streams. Physical, chemical and microbiological parameters assessed bimonthly using samples collected at each stream source were used to calculate the Horton Index (HI), the Dinius Index (DI) and the water quality index adopted by the US National Sanitation Foundation (NSF WQI) in the additive and multiplicative forms. These indices describe mean water quality levels at the streams sources. The results obtained for these 3 indexes showed a worrying scenario in which water quality has already been negatively affected at the sites where three important sub-basins in the Sinos River Basin begin to form.

A Bacia Hidrográfica do Rio dos Sinos (BHRS) está localizada na região Nordeste do Estado do Rio Grande do Sul (29º20' to 30º10'S and 50º15' to 51º20'W), na região Sul do Brasil, envolvendo duas regiões geomorfológicas, o planalto Sul e a depressão central. Esta bacia faz parte da Bacia do Guaíba e tem uma área de aproximadamente 800 km², atingindo 32 municípios. A BHRS fornece água de abastecimento para cerca de 1.6 milhões de habitantes e para um dos mais importantes centros industriais do Brasil. Este artigo apresenta a determinação de diferentes índices de qualidade de água (IQA) para as regiões de nascente de três importantes sub-bacias pertencentes à BHRS: arroios Pampa, Estância Velha/Portão e Schmidt. Utilizando parâmetros físicos, químicos e microbiológicos, analisados em amostras coletadas bimestralmente em cada ponto próximo à nascente, foram calculados os índices de Horton (IH), de Dinius (ID) e o índice de qualidade de água da National Sanitation Foundation, EUA (IQANSF) usando os métodos somatório e produtório. Os resultados foram analisados para verificação da qualidade da água nos pontos amostrais a fim de comparar e classificar a água na região das nascentes das três sub-bacias. Uma avaliação conjunta dos índices calculados indicou que a água nos três pontos amostrais apresenta qualidade média. Os resultados dos três índices convergem a um cenário preocupante que indica que, desde os pontos iniciais de formação de três importantes sub-bacias do rio dos Sinos, já ocorrem problemas de qualidade de água.

Evaluation of water quality at the source of streams of the Sinos River Basin, southern Brazil

p>The Sinos River Basin (SRB) is located in the northeastern region of the state of Rio Grande do Sul (29º20' to 30º10'S and 50º15' to 51º20'W), southern Brazil, and covers two geomorphologic provinces: the southern plateau and the central depression. It is part of the Guaíba basin, has an area of approximately 800 km sup>2 /sup> and contains 32 counties. The basin provides drinking water for 1.6 million inhabitants in one of the most important industrial centres in Brazil. This study describes different water quality indices (WQI) used for the sub-basins of three important streams in the SRB: Pampa, Estância Velha/Portão and Schmidt streams. Physical, chemical and microbiological parameters assessed bimonthly using samples collected at each stream source were used to calculate the Horton Index (HI), the Dinius Index (DI) and the water quality index adopted by the US National Sanitation Foundation (NSF WQI) in the additive and multiplicative forms. These indices describe mean water quality levels at the streams sources. The results obtained for these 3 indexes showed a worrying scenario in which water quality has already been negatively affected at the sites where three important sub-basins in the Sinos River Basin begin to form. /p>

p>A Bacia Hidrográfica do Rio dos Sinos (BHRS) está localizada na região Nordeste do Estado do Rio Grande do Sul (29º20' to 30º10'S and 50º15' to 51º20'W), na região Sul do Brasil, envolvendo duas regiões geomorfológicas, o planalto Sul e a depressão central. Esta bacia faz parte da Bacia do Guaíba e tem uma área de aproximadamente 800 km sup>2 /sup>, atingindo 32 municípios. A BHRS fornece água de abastecimento para cerca de 1.6 milhões de habitantes e para um dos mais importantes centros industriais do Brasil. Este artigo apresenta a determinação de diferentes índices de qualidade de água (IQA) para as regiões de nascente de três importantes sub-bacias pertencentes à BHRS: arroios Pampa, Estância Velha/Portão e Schmidt. Utilizando parâmetros físicos, químicos e microbiológicos, analisados em amostras coletadas bimestralmente em cada ponto próximo à nascente, foram calculados os índices de Horton (IH), de Dinius (ID) e o índice de qualidade de água da National Sanitation Foundation, EUA (IQANSF) usando os métodos somatório e produtório. Os resultados foram analisados para verificação da qualidade da água nos pontos amostrais a fim de comparar e classificar a água na região das nascentes das três sub-bacias. Uma avaliação conjunta dos índices calculados indicou que a água nos três pontos amostrais apresenta qualidade média. Os resultados dos três índices convergem a um cenário preocupante que indica que, desde os pontos iniciais de formação de três importantes sub-bacias do rio dos Sinos, já ocorrem problemas de qualidade de água. /p>

Evaluation of water quality at the source of streams of the Sinos River Basin, southern Brazil / Avaliacão da qualidade da água das nascentes de arroios da Bacia do Rio dos Sinos, região sul do Brasil

The Sinos River Basin (SRB) is located in the northeastern region of the state of Rio Grande do Sul (29º20' to 30º10'S and 50º15' to 51º20'W), southern Brazil, and covers two geomorphologic provinces: the southern plateau and the central depression. It is part of the Guaíba basin, has an area of approximately 800 km 2 and contains 32 counties. The basin provides drinking water for 1.6 million inhabitants in one of the most important industrial centres in Brazil. This study describes different water quality indices (WQI) used for the sub-basins of three important streams in the SRB: Pampa, Estância Velha/Portão and Schmidt streams. Physical, chemical and microbiological parameters assessed bimonthly using samples collected at each stream source were used to calculate the Horton Index (HI), the Dinius Index (DI) and the water quality index adopted by the US National Sanitation Foundation (NSF WQI) in the additive and multiplicative forms. These indices describe mean water quality levels at the streams sources. The results obtained for these 3 indexes showed a worrying scenario in which water quality has already been negatively affected at the sites where three important sub-basins in the Sinos River Basin begin to form.

A Bacia Hidrográfica do Rio dos Sinos (BHRS) está localizada na região Nordeste do Estado do Rio Grande do Sul (29º20' to 30º10'S and 50º15' to 51º20'W), na região Sul do Brasil, envolvendo duas regiões geomorfológicas, o planalto Sul e a depressão central. Esta bacia faz parte da Bacia do Guaíba e tem uma área de aproximadamente 800 km 2, atingindo 32 municípios. A BHRS fornece água de abastecimento para cerca de 1.6 milhões de habitantes e para um dos mais importantes centros industriais do Brasil. Este artigo apresenta a determinação de diferentes índices de qualidade de água (IQA) para as regiões de nascente de três importantes sub-bacias pertencentes à BHRS: arroios Pampa, Estância Velha/Portão e Schmidt. Utilizando parâmetros físicos, químicos e microbiológicos, analisados em amostras coletadas bimestralmente em cada ponto próximo à nascente, foram calculados os índices de Horton (IH), de Dinius (ID) e o índice de qualidade de água da National Sanitation Foundation, EUA (IQANSF) usando os métodos somatório e produtório. Os resultados foram analisados para verificação da qualidade da água nos pontos amostrais a fim de comparar e classificar a água na região das nascentes das três sub-bacias. Uma avaliação conjunta dos índices calculados indicou que a água nos três pontos amostrais apresenta qualidade média. Os resultados dos três índices convergem a um cenário preocupante que indica que, desde os pontos iniciais de formação de três importantes sub-bacias do rio dos Sinos, já ocorrem problemas de qualidade de água.

Study on antimicrobial activity and classification of endophytic fungi from Glehnia littoralis / 中草药

Objective: To screen the endophytic fungi with antimicrobial activity from Glehnia littoralis and identify the taxonomy of these fungi. Methods: The endophytic fungi were isolated from G. littoralis by method of tissue isolation. The oxford-cup test was used in screening the endophytic fungi with antimicrobial activity for Escherichia coli, Staphylococcus aureus, and Candida albicans respectively. And the rDNA ITS1-5.8S-ITS2 sequences were applied for the taxonomy of endophytic fungi. Results: Nineteen strains of fungi with antimicrobial activity were attributed to four genera, five families, seven orders, and eight species. In these fungi, there were four strains with antimicrobial activity to E. coli (the max d/D value was 1.07), Fifteen strains with antimicrobial activity to S. aureus (the max d/D value was 0.65), and three strains with antimicrobial activity to C. albicans (the max d/D value was 1.27). Conclusion: Many kinds of fungi with antimicrobial activity inhabit in G. littoralis. This study is helpful to develop the recourses of endophytic fungi and to evaluate the genuineness of G. littoralis.

Induction and anatomical observation of callus of Asarum heterotropoides / 中草药

Objective: To optimize the proper condition for callus induction of Asarum heterotropoides var. mandshuricum. Methods: The effects of different explants, medium types, and plant growth regulators on the callus induction of A. heterotropoides var. mandshuricum were studied by using the petioles and leaves as explants. Also we aimed to discover the morphology characteristics of callus in different periods through paraffin method. Results: The efficient callus induction medium was 1/2 MS + 0.6 mg/L 6-BA + 0.15 mg/L NAA while using petioles and leaves during young period as explants. Callus induction from young leaves lasted so long time. Furthermore it was found that the induced calli were embryogenic for they were composed of compact, small and irregular arrangement cells. Subsequently these calli could be differentiated to develop the regeneration plantlet. Conclusion: Young petiole is the optimal explant for callus induction of A. heterotropoides var. mandshuricum, and the efficient callus induction condition we optimized would provide a basis for establishing the subsequent regeneration system.

A study on the immunocytochemical localization of neurofascin in rat sciatic nerve

We examined the localization of neurofascin (NF) in the sciatic nerve of rat. In the myelinated fibers, neurofascin localizes strongly in the nodal axolemma except the small central cleft and also expresses in the paranodes, and weakly in the Schmidt-Lanterman incisures. In the paranodes, NF localizes around the axolemma and it expresses in the apposing membrane of paranodal loops. Axoplasm, compact myelin and cytoplasm of Schwann cell do not express NF at all. In the Schmidt-Lanterman incisures, NF is expressed weakly along the Schwann cell membrane. We propose that neurofascin may be a plasmalemmal integral protein of Schwann cell in the paranode and plays some important roles for the maintenance of axo-glial junctions at the paranode. It may also have some roles for maintaining the structure of Schmidt-Lanterman incisure and have some relations with proteins localizing in the node.

A Case of Digoxin-like Immunoreactive Substance(DLIS) Poisoning After Ingestion of Fried Water Toad (Bufo Stejnegeri Schmidt) / 대한내과학회지

Everybody knows that toads are not eatable because of their toxins. But water toads are very similar to frogs morphologically, so fried water toads are eaten by some people on occasion. It has been studied that the granular glands of the toads secrete toxins known as digoxin-like immunoreactive substances (DLIS) such as bufogenins and bufotoxins. DLIS have cross-reactivity with micro particle enzyme immunoassay for the quantitative mea surement of digoxin. We report a case of DLIS poisoning in 56-year-old male patient who showed vomiting, syn cope, and marked bradyarrhythmia with block (heart rate down to 29 beats per minute) after ingestion of the fried water toads (Bufo stejnegeri Schmidt).