Identification of Escherichia coli β-glucuronidase inhibitors from Polygonum cuspidatum Siebold & Zucc

Abstract Gut bacterial β-glucuronidase (GUS) can reactivate xenobiotics that exert enterohepatic circulation- triggered gastrointestinal tract toxicity. GUS inhibitors can alleviate drug-induced enteropathy and improve treatment outcomes. We evaluated the inhibitory effect of Polygonum cuspidatum Siebold & Zucc. and its major constituents against Escherichia coli GUS (EcGUS), and characterized the inhibitory mechanism of each of the components. Trans-resveratrol 4'-O-β-D-glucopyranoside (HZ-1) and (-)-epicatechin gallate (HZ-2) isolated from P. cuspidatum were identified as the key components and potent inhibitors. These two components displayed strong to moderate inhibitory effects on EcGUS, with Ki values of 9.95 and 1.95 μM, respectively. Results from molecular docking indicated that HZ-1 and HZ-2 could interact with the key residues Asp163, Ser360, Ile 363, Glu413, Glu504, and Lys 568 of EcGUS via hydrogen bonding. Our findings demonstrate the inhibitory effect of P. cuspidatum and its two components on EcGUS, which supported the further evaluation and development of P. cuspidatum and its two active components as novel candidates for alleviating drug-induced damage in the mammalian gut.

[Analysis of innovative drug category 1.2 in traditional Chinese medicine and considerations on quality control of extracts].

In this article, the essence of innovative drug category 1.2 extracts and preparations in the new version of the New Drug Registration Category of traditional Chinese medicines(TCM) was analyzed by combing through the history of provisions on drug registration and comparing with other categories of drugs. After analyzing the characteristics of this type of preparations, the author concluded that the quality control objectives of category 1.2 extract should focus on ensuring the quality consistency of the active ingredients/components in batches, so as to guarantee the consistency of drug quality and efficacy. With reference to the relevant technical requirements for herbal medicinal products in European Medicines Agency(EMA) and botanicals in Food and Drug Administration(FDA),the key points in quality control of the extract should include the content and composition of the therapeutic constituents, the type and content of the concomitants, and the influence of exogenous contaminants on drug safety.

Effect of Exercise Prescription Implementation Rate on Cardiovascular Events.

BACKGROUND: Exercise prescription of cardiac rehabilitation (CR) is vital in patients with cardiovascular diseases (CVDs) and those carrying high risk for CVDs. However, the relation between the implementation rate of exercise prescription and cardiovascular events (CVEs) is unclear. DESIGN AND METHODS: In this retrospective study, using the administration data from the Rehabilitation Center in a hospital, patients aged ≥18 years with CVDs were consecutively enrolled from November 2018 to May 2021. Patients were divided into the high execution group (HEG) and low execution group (LEG) depending on whether they completed more than half the time of the exercise prescriptions. Baseline characteristics, ultrasonic cardiogram, cardiopulmonary exercise test, follow-up data, and CVEs were collected. RESULTS: The mean age of the 197 CR patients was 61.8 ± 13.7 years and the mean follow-up duration was 10.9 ± 4.2 months. Among them, 15 patients suffered CVEs: 4 in the HEG and 11 in the LEG. The incidence of CVEs showed significant differences between HEG and LEG (chi-square test). Free-event survival analysis using Kaplan-Meier survival plots showed that patients in LEG had poor survival. Cox proportional hazards regression analysis revealed that the prescription implementation rate was an independent predictor of CVEs. CONCLUSIONS: Our study suggested a significant effect of exercise prescription execution rate on the occurrence of CVEs. Further, the HEG of exercise prescription was associated with lower CVDs.

[Screening and identification of antagonistic Bacillus against Astragalus membranaceus root rot and its effect on microorganism community in root zone soil].

The Astragalus membranaceus root rot disease,a soil-borne disease,has become increasingly severe in Shanxi province.This study was aimed at getting antagonistic Bacillus with excellent bio-control effects,and determining its effects on bacterial communities in root zone soil. With Fusarium solani and F. acuminatum as the target,antagonistic Bacillus was selected through such tests as living body dual culture,antifungal effect of bacteria-free filtrate,mycelia growth inhibition in vitro and control effect in detached roots,and identified with morphology,physio-biochemical characteristics and 16 S r DNA sequence analysis. The results showed that the Bacillus strain SXKF16-1 had obvious antifungal effect. The diameter of inhibition zone of its bacteria-free filtrate to F. solani and F. acuminatum was( 25. 90±1. 18) mm and( 25. 86±1. 85) mm respectively,and showed a lasting inhibition effect to mycelia growth. The disease index of the protective treatment and that of the cure treatment in detached roots test to F. solani and F. acuminatum were( 37. 50±8. 58),( 41. 67±4. 90) and( 25. 00±8. 33),( 38. 89±9. 62) respectively,both being significantly different( P<0. 05) from that of the control. The strain SXKF16-1 was identified as Bacillus atrophaeus. The B. atrophaeus SXKF16-1 showed significantly inhibition effect to pathogen causing root rot and could increase the bacterial diversity in root zone soil. It has potential to be developed as a special biocontrol agent.

Association of T-helper cell cytokine level with age in patients with biliary atresia: a preliminary study.

BACKGROUND: The pathogenesis of biliary atresia (BA) is associated with an inflammatory process involving the biliary tree. This study aimed to investigate the association of T-helper cell cytokine levels with age in patients with BA. METHODS: Twenty-eight patients with BA were divided into three groups according to their age (< 2 months, 2-3 months, and ≥ 3 months). All the patients underwent Kasai portoenterostomy. Blood samples were collected from the patients preoperatively, and the liver tissue specimens were obtained during surgery. We detected serum levels of interleukin (IL)-1ß, IL-12p70, interferon (IFN)-γ, IL-6, IL-10, and transforming growth factor (TGF)-ß1 and liver expression of IL-1ß, IL-6, and TGF-ß1. RESULTS: The serum levels of IL-1ß, IL-12p70, IL-6, and IL-10 in patients aged ≥ 3 months were significantly higher than those in patients aged < 2 months. There were no significant age-related differences in the IL-1ß, IL-6 and TGF-ß1 expression levels in the liver tissue of patients with BA. CONCLUSIONS: The serum levels of IL-1ß, IL-6, IL-10 and IL-12p70 showed significant age-related differences in patients with BA. Interpretation of the role of cytokines in BA needs to take patient's age into consideration.

[Comparison and review on specifications of fermented Cordyceps sinensis products].

There are five kinds of fermented Cordyceps crude drug and their preparations that have been approved as medicine on the market. Since the initial strains of the crude drug were all isolated from natural Cordyceps sinensis， they have similar names， chemical components and even clinical applications. However， because of the different strain species and fermentation processes， there was significant difference in quality. As a result， they should be clearly distinguished in clinical use. Most of the products were researched and developed during the 1980s and 1990s， so there was difference in quality standards for different products， and their quality control levels of some products were not perfect. At present， some of the products are approved as Chinese medicine， others are approved as chemical drugs， with a confusion in products name， management and clinical application. In this paper， the approval numbers， quality standards and clinical applications， and current problems of these products were summarized and compared; some suggestions were put forward， such as standardizing the product name， unifying the management of approval number category， and increasing the specific quality control attributes， in order to provide reference for standard implementation， quality control and drug regulation for fermented Cordyceps crude drugs and their preparations.

[Correlation of TLR2 and TLR4 gene polymorphisms with the susceptibility and recurrence of condyloma acuminatum].

OBJECTIVE: To explore the correlation of the gene polymorphisms of Toll-like receptor 2 ( TLR2) and TLR4 with the susceptibility and recurrence of condyloma acuminatum (CA). METHODS: Using Snapshot, we detected the gene polymorphisms of TLR2 597(T/C), 1350(T/C), 15607(A/G), and 2258(G/A) and TLR4 896(A/G) and 1196(C/T) in the peripheral blood of 140 CA patients and 105 HPV-negative controls. We made comparisons between the CA patients and controls as well as between the cases of recurrent CA and those of non-recurrence at 6 months after treatment. RESULTS: There were 72, 48, and 20 cases of genotype TT, TC, and CC of TLR2 597 (T/C), respectively, in the CA patients, as compared with 71, 31, and 3 cases in the controls. The gene frequency of mutant C was 31. 43% in the patients, significantly higher than 17.62% in the controls (χ2 = 12.04, P < 0.01), and it was 38.68% in the recurrent cases, remarkably higher than 27.01% in the non-recurrent cases (χ2 = 4.16, P < 0.05). There were 74, 49, and 17 cases of genotype TT, TC, and CC of TLR2 1350( T/C), respectively, in the CA patients, as compared with 73, 29, and 3 cases in the controls. The gene frequency of mutant C was 29. 64% in the patients, significantly higher than 16. 67% in the controls (χ2 =11.05, P < 0.01), and it was 36.79% in the recurrent cases, markedly higher than 25. 29% in the non-recurrent cases (χ2 = 4.18, P < 0.05). There were 44, 66, and 30 cases of genotype AA, AG, and GG of TLR2 15607(A/G), respectively, in the CA patients, as compared with 26, 58, and 21 cases in the controls. There was no significant difference in the gene frequencies of mutant G between the two groups (χ2 = 0.33, P > 0.05). No mutant genes of TLR2 2508 (G/A) or TLR4 896(A/G) and 1196(C/ T) were detected in either the CA patients or the controls. Linkage disequilibrium analysis showed a tight linkage between TLR2 597 (T/C) and 1350(T/C) (D' = 1, r2 = 0.93). CONCLUSION: TLR2 597(T/C) is tightly linked to 1350(T/C), which is correlated with both the susceptibility and the recurrence of condyloma acuminatum.

Mantle Branch-Specific RNA Sequences of Moon Scallop Amusium pleuronectes to Identify Shell Color-Associated Genes.

Amusium pleuronectes (Linnaeus) that secretes red- and white-colored valves in two branches of mantle tissues is an excellent model for shell color research. High-throughput transcriptome sequencing and profiling were applied in this project to reveal the detailed molecular mechanism of this phenotype differentiation. In this study, 50,796,780 and 54,361,178 clean reads were generated from the left branch (secreting red valve, RS) and right branch (secreting white valve, WS) using the Illumina Hiseq 2000 platform. De novo assembly generated 149,375 and 176,652 unigenes with an average length of 764 bp and 698 bp in RS and WS, respectively. Kyoto encyclopedia of genes and genomes (KEGG) metabolic pathway analysis indicated that the differentially expressed genes were involved in 228 signaling pathways, and 43 genes were significantly enriched (P<0.01). Nineteen of 20 differentially expressed vitellogenin genes showed significantly high expression in RS, which suggested that they probably played a crucial role in organic pigment assembly and transportation of the shell. Moreover, 687 crystal formation-related (or biomineralization-related) genes were detected in A. pleuronectes, among which 144 genes exhibited significant difference between the two branches. Those genes could be classified into shell matrix framework participants, crystal nucleation and growth-related elements, upstream regulation factors, Ca level regulators, and other classifications. We also identified putative SNP and SSR markers from these samples which provided the markers for genetic diversity analysis, genetic linkage, QTL analysis. These results provide insight into the complexity of shell color differentiation in A. pleuronectes so as valuable resources for further research.

[Effect of matrine on Fas, VEGF, and activities of telomerase of MCF-7 cells].

OBJECTIVE: To study the effect of matrine on Fas, VEGF, and activities of telomerase of MCF-7 cells. METHODS: In vitro cultured human breast cancer MCF-7 cells were randomly divided into the experimental group and the control group. The matrine solution was added in cells of the experimental group. Equal volume of culture medium was added in cells of the control group or the negative control group. Zedoary Turmeric Oil, the telomerase inhibitor was added in cells of the positive control group. Morphological changes were observed under an inverted microscope. The telomerase activity was detected by TRAP-ELISA. Expressions of Fas and VEGF protein were detected by immunocytochemical assay. RESULTS: Matrine obviously inhibited the growth and induced apoptosis of breast cancer cells. MCF-7 cells were treated by matrine of different concentrations at 24, 48, and 72 h, the telomerase activity gradually decreased along with increased matrine concentration and prolonged action time, showing dose-effect and time-effect positive relations. Matrine could up-regulate Fas protein expression and downregulate VEGF protein expression of MCF-7 cells. CONCLUSION: Matrine showed obvious effect in inhibiting the growth of MCF-7 cells and promoting the apoptosis, which might be achieved by up-regulating the expression of Fas protein, inhibiting telomerase activity induced apoptosis of breast cancer cells, down-regulating the expression of VEGF protein, and inhibiting the tumor vascular formation.

Selective reflection of Airy beam at an interface between dielectric and homogeneous atomic medium.

We examine selective reflection (SR) spectrum of an Airy beam at an interface between a dielectric and a homogeneous atomic medium. It is shown that both the general reflection (GR) and the SR of Airy beams exhibit accelerating dynamics with a parabolic trajectory, however, the accelerating rate for the SR is slightly greater than that for the GR. Due to interaction of atoms and the Airy beams at the interface between dielectric and resonant atoms, the SR beams can create far-field interference patterns. We also show that the amplitude of the SR can be dramatically modified by the detuning of the incident fields, the reduced x-coordinate and the distance from the interface. The SR at the resonant medium interface of Airy beams can probably be a powerful tool in the use of optical power delivering, resonant particle manipulation and spatial spectrum detection of a resonant medium at an interface.

Evaluation of neuro-intensive care unit performance in China: predicting outcomes of Simplified Acute Physiology Score II or Glasgow Coma Scale.

BACKGROUND: Severity scoring systems are useful tools for measuring the severity of the disease and its outcome. This pilot study was to verify and compare the prognostic performance of the Simplified Acute Physiology Score II (SAPS II) and Glasgow Coma Scale (GCS) in neuro-intensive care unit (N-ICU) patients. METHODS: A total of 1684 patients consecutively admitted to the N-ICU at Xuanwu Hospital between January 1, 2005 and December 31, 2011 were enrolled in this study. The data-base included admission data, at 24-, 48-, and 72-hour SAPS II and GCS. Repeated measure data analysis of variance, Logistic regression analysis, the Hosmer-Lemeshow goodness-of-fit statistic, and the area under the receiver operating characteristic were used to evaluate the performance. RESULTS: There was a significant difference between the SAPS II or GCS score at four time points (F = 16.110, P = 0.000 or F = 8.108, P = 0.000). The SAPS II scores or GCS score at four time points interacted with the outcomes with significant difference (F = 116.771, P = 0.000 or F = 65.316, P = 0.000). Calibration of the SAPS II or GCS score at each time point on all patients was good. The percentage of a risk estimate prediction corresponding to observed mortality was also good. The 72-hour score have the greatest consistency. Discriminations of the SAPS II or GCS score at each time were all satisfactory. The 72-hour score had the greatest discriminative power. The cut-off value was 33 (sensitivity of 85.2% and specificity of 74.3%) and 6 (sensitivity of 70.6% and specificity of 65.0%). The SAPS II at each time point on all patients showed better calibration, consistency and discrimination than GCS. The binary Logistic regression analysis identified physiological variables, GCS, age, and disease category as significant independent risk factors of death. After the two variables including underlying disease and type of admission were excluded, we built the simplified SAPS II model. A correlation was suggested between the simplified SAPS II score at each time point and outcome, regardless of the diagnosis. CONCLUSIONS: The GCS scoring system tends to be a little weaker in the predictive power than the SAPS II scoring system in this Chinese cohort of N-ICU patients. The advantage of SAPS II scoring system still exists that it dose not need to take into account the diagnosis or diseases categories, even in the special N-ICU. The simplified SAPS II scoring system is considered a new idea for the estimation of effectiveness.

[Study on concentration quenching and energy transfer in Ln3+ (Ln = Tb, Tm, Eu) in Y2O3 nanocrystal powders].

Nano-powders Y2O3 with various particle sizes and different doping concentrations of Ln (Ln = Tb, Tm, Eu) were prepared by using a combustion technique. The bulky powders doped with concentrations corresponding to nano-powders were obtained by annealing the nano-powders at high temperature. The emission spectra, XRD spectra and TEM were used in the present study. The concentration quenching of luminescent centers and energy transfer between luminescent centers in Y2O3 : Ln nanocrystal powders were investigated. It was found that the behaviors of luminescence concentration quenching for 5D4 --> 7F5 : Tb3+ and 5D0 --> 7F2 : Eu3+ in nano-powders are similar to that in bulky powders. On the contrary, the quenching concentrations for 5D3 --> 7F5 : Tb3+ and 1D2 --> 3H4 : Tm3+ are distinctly higher than that in bulk powders. This owes to the size confinement effect: the interface of nanocrystal particles can stop a portion of the energy transfer, which happens in the bulk ones, between luminescent centers. The size confinement effect can bring different influences to the different types of energy transfer. For instance, it will restrain the energy transfer (governed by electric dipole-dipole interaction) between the ions in long distances, and will hardly affect the energy transfer (governed by exchange interaction) between the ions locating at near intervals.

[Preparation of alpha-Gd2 (MoO4)3 red emitting phosphor for white light emitting diodes and its luminescence study].

A novel red phosphor alpha-Gd2 (MoO4)3: Eu was synthesized by conventional solid state reaction method with the starting materials: Gd2O3, MoO3 and Eu2O3. The effects of flux and Eu concentration on the crystal structure, morphology and luminescent properties of the phosphors were investigated. The results showed that non-agglomeration phosphors with regular morphology and fine size were produced after the mixture being calcined at 800 degrees C for 4h with 3% NH4F as flux. The main emission peak of the samples is at 613 nm. The excitation spectrum showed that this phosphor can be effectively excited by ultraviolet (UV) (395 nm) and blue (465 nm) light, nicely fitting in with the widely applied output wavelengths of ultraviolet or blue LED chips. The alpha-Gd2 (MoO4)3 phosphor may be a good candidate phosphor for solid state lighting application.

[Quantum efficiency of the 5D0 level of Eu3+ at C2 site in cubic nanocrystalline Y2O3].

In the present the authors are trying to work out how the quantum efficiency depends on the nanocrystalline size. Cubic nanocrystalline Y2O3 : Eu3+ samples were prepared by chemical self-combustion. The bulk Y2O3 : Eu3+ was obtained by annealing the nanocrystalline at 1 000 degrees C for 2 h. The emission spectra, XRD and fluorescence decay showed that the emission intensities are increased and fluorescence decay becomes slow with an increase in particle diameter of the samples. Two routes were used to estimate the quantum efficiency of the 5D0 level of Eu3+ at C2 site. The quantum efficiencies of 5D0 level of Eu3+ at C2 site in the samples depend on the nanocrystalline sizes. Finally, a detailed discussion about these two approaches for estimating the quantum efficiencies was made.

[Experimental studies on the preparation techniques of Tongjingshu babu sticking plaster].

OBJECTIVE: to establish the optimum preparation procedure for Tongjingshu babu sticking plaster. METHOD: Orthogonal design was used to observe the adhesion power, cohesion by the multi-electronic experimental equipment. RESULT: The best formulation is composed of ointment, polypropylene acid, glycerin, bond and its proportion is 0.2:4:8:1.2, the final plaster contains 35% water with idea stability to the skin. CONCLUSION: The formulation of Tongjing-shu babu sticking plaster is resonable and its preparation is simple and rapid.

[Synthesis and luminous characteristics of Y (P, V)O4: Eu3+ phosphors for PDP].

Y(P, V)O4 :Eu3+ phosphors with good morphology for plasma display panels have been prepared via coprecipitation reaction. The phosphor was characterized by SEM and photoluminescence under UV (325 nm)and VUV (147 nm) excitation. The emission spectra depending on temperature under 325 nm excitation by laser indicated that there exist energy transfer between VO4(3-) group and Eu3+ ion. Under 147 nm excitation, the most intense emission peaks of commercial (Y,Gd)BO3 :Eu3+ phosphor range around 593 nm, and those of Y(P, V)O4 :Eu3+ phosphors prepared by coprecipitation reaction ranged around 619 nm. The red emission color purity of Y(P, V)O4 :Eu3+ phosphor is much better than that of (Y,Gd)BO3: Eu3+, and its relative emission intensity is almost close to that of the commercial phosphor.