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The first wide-view image of multiple structural and phase transformations for MOFs from crystal state transformations further to the extreme limit approaching liquid/glass phase, was presented based on a square-layer framework of [Co2(pybz)2(CH3COO)2]·DMF (Co2). The process involves i) an initial crystalline transformation brings to a 3-fold interpenetrated and ordered vacancies contained framework [Co(pybz)2(CH3OH)2]·2CH3OH (CoM) due to in-situ disassemble-reassemble, ii) thermal induced departure of a pair of cis-form coordinated methanol in CoM leads to amorphous framework (a-dCoM), iii) glass transition (Tg = 566 K) to super-cooled liquid (scl-dCoM, spanning 38 K), iv) obtaining MOF glass g-dCoM upon quenching the super-cooled liquid, and v) re-crystallization of super-cooled liquid to six-fold interpenetrated dia-net framework [Co(pybz)2]6n (rec-dCoM) under heating above 604 K. The access to glass from CoM, provides a new self-perturbation strategy to create more MOF glasses without melting. The wider pore size distribution in amorphous/glassy MOFs than crystalline precursor realized the first time selective hydrocarbon gas separation by breakthrough experiments, which bring efficient separation of 1:99 C2H2/C2H4 by either a-dCoM or g-dCoM and produce polymer grade C2H4 with purity ≥ 99.5% after a single adsorption process. Furthermore, the mixture of 50:50 C3H6/C3H8 can be separated by a-dCoM.
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We report the synthesis and structural characterization of a 2D metal-organic framework with AB-packing layers, [Co2(pybz)2(CH3COO)2]·DMF (Co2, pybz= 4-(4-pyridyl)benzoate), containing a stable (4,4)-grid network fabricated by paddle-wheel nodes, ditopic pybz, and acetate ligands. After removal of the guest, the layer structure is retained but reorganized into an ABCD packing mode in the activated phase (Co2a). Consequently, the intralayer square windows (7.2 × 5.0 Å2) close, while the interlayer separation is decreased slightly from 3.69 to 3.45 Å, leaving a narrow gap. Importantly, the dangling methyl group of the acetate with H-bonds to the adjacent layers and also the well-distributed π-π interactions between the aromatic rings of neighboring layers facilitate the structural stability. These weak supramolecular interactions further allow for favorable dynamic exfoliation of the layers, which promotes efficient adsorption of C2H2 (41.6 cm3 g-1) over CO2 with an adsorption ratio of 6.3 (0.5 bar, 298 K). The effective separation performance of equimolar C2H2/CO2 was verified by cycling breakthrough experiments and was even tolerable to moisture (R.H = 52%). DFT calculations, in situ PXRD, and PDF characterization reveal that the favorable retention of C2H2 rather than that of CO2 is due to its H-bond formation with the paddle-wheel oxygen atoms that triggers the increase in interlayer separation during C2H2 adsorption.
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OBJECTIVE: To study the pharmacodynamics of Gualou Xiebai Dropping Pills and its medicinal ingredients in prescription on anti-myocardial ischemia. METHODS: SPF Rats were divided randomly into eleven groups with ten rats in each group and half male and half female, the rats were respectively given the physiological saline(blank group and model group), Gualou, Xiebai, Gualou Xiebai Baijiutang (all equivalent to the crude herb of 22. 5 g/kg), Gualou Xiebai. Dropping Pills in the doses of 3. 75,11. 25,22. 5,33. 75 and 45 g/kg and Compound Danshen Drop Pills of 0. 085 g/kg by gavage one time a day for seven days. Except blank group, other rats were given by intraperitoneal injection of isoproterenol to establish myocardial ischemia models, changes of ST segments in ECG were observed in all groups, and the levels of SOD, NO, HDL-C, MDA, CAT, LDH and CK in blood plasma were detected, and the pathological changes of myocardial tissues were observed under light microscope by HE staining. RESULTS: Compared with model group, ST segments in ECG dropped markedly at different time point which included 10,11 and 12 (P <0. 05) in Gualou Xiebai Drop Pills groups of 22. 5, 33. 75 and 45 g/kg, time points were more than those of other groups. Gualou Xiebai Dropping Pills groups of 22. 5 and 33. 75 g/kg improved the levels of SOD, MDA, CAT, NO, HDL-C, LDH and CK in blood plasma in model rats significantly (P <0. 01 or P <0. 05). Gualou Xeibai Dropping Pills improved the pathological changes of myocardial tissues at all dosages. CONCLUSION: Gualou Xiebai Drop Pills can effectively restrain the acute myocardial ischemia induced by isoproterenol in rats, compared with Gualou, Xiebai or Gualou Xiebai Baijiutang, Gualou Xiebai Drop Pills obtains a favourable effect.
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Medicamentos Herbarios Chinos/farmacología , Isquemia Miocárdica/tratamiento farmacológico , Miocardio/patología , Animales , Modelos Animales de Enfermedad , Femenino , Masculino , Ratas , Salvia miltiorrhizaRESUMEN
OBJECTIVE: To determine the concentration of quercetin in mouse plasma by HPLC-DAD in different time after oral administration with Gualou Xiebai decoction and Gualou decoction, and to explore the influence of the compatibility of Gualou and Xiebai on pharmacokinetics of quercetin in Gualou. METHODS: The plasma sample was simply deproteinized with acetonitrile, extracted three times by aceticether, evaporated to dryness with a gentle N2 stream, dissolved with methanol and determined by HPLC. The pharmacokinetic parameters were separately calculated and compared with data processing software DAS 2. 0 and SPSS 11. 5 software. RESULTS: After oral administration with Gualou Xiebai decoction and Gualou decoction, the pharmacokinetics of quercetin in mouse plasma accorded with the two-compartment model, and t1/2α, t1/2ß, AUC0-t, AUC0-∞, Cmax, tmax, Ka, K10, K12, K21, CL/F and V1/F all had significant differences(P <0. 05 or P <0. 01). CONCLUSION: Xiebai in Gualou Xiebai decoction has a remarkable effect on pharmacokinetic character of quercetin in Gualou, it can promote the absorption and distribution and reduce the elimination of quercetin, in vivo, as well as increase the bioavailability of quercetin.
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Medicamentos Herbarios Chinos/química , Quercetina/farmacocinética , Animales , Disponibilidad Biológica , Cromatografía Líquida de Alta Presión , RatonesRESUMEN
OBJECTIVE: To study the relationship between HPLC characteristic spectrum and pharmacodynamics on anti-myocardial ischemia of GualouXiebai dropping pills. METHODS: HPLC characteristic spectrum of GualouXiebai dropping pills was established, dropping pills were divided into five dose groups (3.75, 11.25, 22.5, 33.75 and 45 g/kg, equivalent to the crude herb g/kg), the mice were orally administered dropping pills once daily for 7 d, 90 min after the mice were given by intraperitoneal injection of isoprenaline to establish myocardial ischemia models, the level of CK in blood plasma were detected; Then, the correlation between characteristic spectrum and biochemical index CK was studied by grey relational analysis method. RESULTS: The correlation between each common peak and CK had gradually increased with the dose increased from 3.73 g/kg to 33.75 g/kg, but when the dose reached to 45 g/kg, the correlation between each common peak and CK had decreased. The variation trends of correlation of spectrum-effect relationship for different dose were similar,but the correlation variation trend of the efficacy on the No. 8 peak in 33.75 g/kg group with the other four groups in the opposite, the change trends of the No. 11 peak in 22.5 g/kg group, the No. 24 peak in 33. 75 g/kg group and the No. 37 peak in 45 g/ kg group with 3.75 g/kg group and 11.25 g/kg group on the contrary. The relational orders of spectrum-effect relationship were not consistent, respectively( the first 15 peaks) :11 > 37 > 24 > 30 > 8 > 21 > 2 > 16 > 1 > 3 > 20 > 15 > 12 > 19 > 7;11 > 37 > 30 > 8 > 21 > 24 > 2 > 1 > 16 > 3 > 27 > 12 > 22 > 20 >10; 8 > 30 > 1 > 2 > 21 > 27 > 31 > 22 > 16 > 12 > 3 > 10 > 9 > 20 > 4; 1 > 2 > 27 > 21 > 31 > 22 > 12 > 16 > 9 > 3 > 10 > 4 > 17 > 30 > 20; 8 > 30 > 1 > 2 > 2 > 2 > 7 > 31 > 22 > 16 > 12 > 3 > 9 > 10 > 20 > 17. CONCLUSION: Anti-myocardial ischemia effect of GualouXiebai dropping pills comes from the synergistic or antagonistic effect among various active ingredients related to the dose. With the difference of the dosage, the relational orders of chemical components to play the role is not the same, but the main components to play a pharmacodynamic of five dose groups are consistent,the existence of the component groups lay a foundation for further study of GualouXiebai dropping pills.
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Medicamentos Herbarios Chinos/farmacología , Isquemia Miocárdica/tratamiento farmacológico , Animales , Cromatografía Líquida de Alta Presión , Modelos Animales de Enfermedad , RatonesRESUMEN
In cancer, gene silencing via hypermethylation is as common as genetic mutations in p53. Understanding the relationship between mutant p53 and hypermethylation of other tumor suppressor genes is essential when elucidate mechanisms of tumor development. In this study, two isogenic human B lymphoblast cell lines with different p53 status include TK6 containing wild-type p53 and WTK1 with mutant p53 were used and contrasted. Lower levels of p16(ink4A) protein were detected in WTK1 cells than in TK6 cells, which were accompanied by increased DNA (cytosine-5)-methyltransferase 1 (DNMT1) gene expression as well as hypermethylation of the p16 ( ink4A ) promoter. siRNA experiments to transiently knock down wild-type p53 in TK6 cells resulted in increase of DNMT1 expression as well as decrease of p16(ink4A) protein. Conversely, siRNA knockdown of mutant p53 in WTK1 cells did not alter either DNMT1 or p16(ink4A) protein levels. Furthermore, loss of suppression function of mutant p53 to DNMT1 in WTK1 was caused by the attenuation of its binding ability to the DNMT1 promoter. In summary, we provide evidences to elucidate the relationship between mutant p53 and DNMT1. Our results indicate that mutant p53 loses its ability to suppress DNMT1 expression, and thus enhances methylation levels of the p16 ( ink4A ) promoter and subsequently down-regulates p16(ink4A )protein.
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Linfocitos B/metabolismo , Inhibidor p16 de la Quinasa Dependiente de Ciclina/metabolismo , ADN (Citosina-5-)-Metiltransferasas/metabolismo , Regulación hacia Abajo , Neoplasias/metabolismo , Proteína p53 Supresora de Tumor/metabolismo , Línea Celular Tumoral , Inhibidor p16 de la Quinasa Dependiente de Ciclina/genética , ADN (Citosina-5-)-Metiltransferasa 1 , ADN (Citosina-5-)-Metiltransferasas/genética , Metilación de ADN , Humanos , Mutación , Neoplasias/genética , Regiones Promotoras Genéticas/genética , ARN Interferente Pequeño/genética , Proteína p53 Supresora de Tumor/antagonistas & inhibidores , Proteína p53 Supresora de Tumor/genéticaRESUMEN
In this study we describe the identification and characterization of a novel cytosolic protein of the guanine exchange factor (GEF) family. The human cDNA corresponds to predicted human protein FLJ00128/FLJ10357 located on chromosome 14q11.2. The deduced protein sequence contains in its C-terminus a RhoGEF domain followed by a pleckstrin domain. Its N-terminus, central region and RhoGEF/pleckstrin domain are homologous to the recently identified zebrafish Quattro protein, which is involved in morphogenetic movements mediated by the actin cytoskeleton. Based on the homology of our protein's RhoGEF domain to the RhoGEF domains of Trio, Duo and Duet and its homology with Quattro, we named it Solo. The Solo mRNA is ubiquitously expressed but enriched in brain, its expression peaks perinatally and it undergoes extensive alternative splicing. In both myoblasts and neuroblastoma cells, the Solo protein is concentrated around the nucleus.