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Acute pharyngitis is an inflammation of the pharyngeal mucous membrane and submucous lymphoid tissues. Unsatisfactory treatment and repeated occurrences might cause chronic pharyngitis and other complications. Syringa oblata L. (S. oblata) is a traditional Chinese medicine that exhibited a significant therapeutic effect on various inflammatory diseases. Its commercial drug Yan Li Xiao (YLX) capsule is used as a cure for the treatment of inflammatory diseases, such as bacillary dysentery, tonsillitis, bronchitis, and acute gastroenteritis. However, studies about S. oblata relieving acute pharyngitis are rare. In this study, high-performance liquid chromatography (HPLC) was used to analyze the chemical profile of S. oblata, and the bioactive phytoconstituents were isolated and identified by nuclear magnetic resonance (NMR) and mass spectrometry. An ammonia-induced acute pharyngitis rat model was established to estimate the protective effect of S. oblata in vivo for the first time. The severity of pharyngitis was observed by appearance index and HE staining. The cytokines expression was performed by ELISA. Crucial proteins expression associated with TLR4/NF-κB/MAPK and NLRP3 inflammasome signaling pathways were analyzed by western blotting and immunohistochemistry. Furthermore, the anti-inflammatory effect of isolated compounds was evaluated by suppressing lipopolysaccharide- (LPS-) induced NO generation and regulating the cytokines levels in RAW 264.7 cells. The results showed that S. oblata exhibited a protective effect in the ammonia-induced acute pharyngitis rat model, and the compounds exert potential anti-inflammatory properties against LPS-activated RAW 254.7 cells.

This paper clarified the scientific connotation of the changes in cold and heat properties of Arisaematis Rhizoma and Arisaema Cum Bile through investigating the changes of substance and energy metabolism after drug intervention in the rats with normal and cold/heat syndrome, so as to improve the method of evaluating the drug properties of Chinese medicine. After one week of adaptive feeding, healthy male SD rats were randomly divided into three parts: normal rats, heat syndrome rat models, and cold syndrome rat models. Through ice water bath and oral euthyrox(120 μg·kg~(-1)), the models of cold syndrome and heat syndrome were induced, respectively. The models were made at 9:00 am. and administrated by gavage at 3:00 pm. every day. All administration groups were administrated with Arisaematis Rhizoma and Arisaema Cum Bile decoction, respectively, and the blank group was given the same dose of normal saline. After continuous administration for 15 d, the rats were anesthetized by chloral hydrate, blood was taken from abdominal aorta, and the hearts and livers were removed and stored at-80 ℃. The changes in the body weight and anal temperature of rats during administration were detected, and the liver coefficient of rats was detected after removing the liver. Enzyme-linked immunosorbent assay(ELISA) was adopted to detect the expression level of the indexes related to substance and energy metabolism in liver and heart of rat, and Western blot was used to detect the expression of key proteins in AMPK/mTOR signaling pathway for further verification. The results showed that Arisaematis Rhizoma enhanced the expression level of enzymes related to substance and energy metabolism in the normal and cold and heat syndrome rat models, and increased anal temperature, which exhibited warm(hot) drug property. Arisaema Cum Bile inhibited the level of substance and energy metabolism in rats, and reduced anal temperature, which showed cold(cool) drug property. Chinese Pharmacopoeia has recordedquot;Arisaematis Rhizoma has warm property and Arisaema Cum Bile has cool propertyquot;, which is consistent with the phenomenon in this study. Therefore, it is feasible to evaluate the drug properties of Chinese medicine based on the substance and energy metabolism of normal and cold/heat syndrome model rats, which completes the method of evaluating drug properties of Chinese medicine.

Cattle bile

Two new (

We present a new family of nonconforming tetrahedral elements and a new family of nonconforming triangular elements for the stress-displacement system of linear elasticity problem. The local degrees of freedom of stress field only contain the normal moments on faces (sides) of element and the moments on element. The shape function spaces are simple, local, explicitly represented, and affine-equivalent. We also present two families simplified lowest-order finite elements by using the rigid motion model, and demonstrate our theory numerically in 2D area.

Four new secoiridoids, syrretoside A (

Four new polyacetylene substances, sadivaethynes A-D, were isolated from the ethanol extract of the roots of

Two new acyclic sesquiterpenoids (

Multi-label classification aims to assign a set of proper labels for each instance, where distance metric learning can help improve the generalization ability of instance-based multi-label classification models. Existing multi-label metric learning techniques work by utilizing pairwise constraints to enforce that examples with similar label assignments should have close distance in the embedded feature space. In this paper, a novel distance metric learning approach for multi-label classification is proposed by modeling structural interactions between instance space and label space. On one hand, compositional distance metric is employed which adopts the representation of a weighted sum of rank-1 PSD matrices based on component bases. On the other hand, compositional weights are optimized by exploiting triplet similarity constraints derived from both instance and label spaces. Due to the compositional nature of employed distance metric, the resulting problem admits quadratic programming formulation with linear optimization complexity w.r.t. the number of training examples. We also derive the generalization bound for the proposed approach based on algorithmic robustness analysis of the compositional metric. Extensive experiments on sixteen benchmark data sets clearly validate the usefulness of compositional metric in yielding effective distance metric for multi-label classification.

Two new dammarane-type triterpenoids, dammar-3

Three new compounds (

We aimed to explore the association between blood pressure, intracranial atherosclerotic stenosis (ICAS) risks and ICAS burden in the Chinese population.A retrospective hospital-based multi-center case-control study with large sample size was conducted. 1055 ICAS patients and 1296 non-ICAS subjects with complete clinical information and intracranial artery evaluation were identified between 2014 and 2019. Cerebral arteries were evaluated by magnetic resonance angiography, and/or computed tomography, and/or digital subtraction angiography. Two or more neurologists were involved in reading and assessment of images. The association between ICAS and burden of ICAS with blood pressure was evaluated with univariate logistic models and multivariate logistic models.With every increase of 10 mmHg in systolic blood pressure, diastolic blood pressure and pulse pressure, the odds of ICAS increased by 32%, 28% and 35% in multivariate analysis, respectively (odds ratio = 1.32, 1.28, and 1.35 respectively, all p 0.001). Similarly, every increment of 10 mmHg in systolic blood pressure and pulse pressure was associated with an increased risk of ICAS burden (each odds ratio = 1.08, p 0.05).Systolic blood pressure, diastolic blood pressure, and pulse pressure were associated with the risk of ICAS in a dose-response manner. Moreover, higher systolic blood pressure and pulse pressure could lead to higher ICAS burdens.

Seven new glycosides (

Withanolides from six parts (flower, leaf, stem, root, seed, and peel) of Datura metel L. (D metel L.) obtained from ten production areas in China were identified and quantified by UPLC-MS/MS. A total of 85 withanolides were characterized for the first time using the UPLC-Q-TOF-MS/MS system. Additionally, a simultaneous, rapid and accurate measurement method was developed for the determination of 22 bioactive withanolides from ten production areas with the UPLC-Q-TRAP-MS/MS system. The results show the total withanolide content is highest in the leaves (155640.0 ng/g) and lowest in the roots (14839.8 ng/g). Compared with other production areas, the total content of plants from Dujiangyan was the highest at 82013.9 ng/g (value range of ten areas: 82013.9&ndash, 42278.5 ng/g). The results also show significant differences in the distribution of withanolides in the different plant parts, as well as across different production areas. This is a breakthrough report providing a simultaneous qualitative and quantitative analysis of 22 withanolides in D. metel L. It could be the basis for the more rational use of various parts of D. metel L., and the expansion of medicinal resources. This work also lays a solid foundation for research on the quality control of D. metel L.

Withanolides from six parts (flower, leaf, stem, root, seed, and peel) of Datura metel L. (D metel L.) obtained from ten production areas in China were identified and quantified by UPLC-MS/MS. A total of 85 withanolides were characterized for the first time using the UPLC-Q-TOF-MS/MS system. Additionally, a simultaneous, rapid and accurate measurement method was developed for the determination of 22 bioactive withanolides from ten production areas with the UPLC-Q-TRAP-MS/MS system. The results show the total withanolide content is highest in the leaves (155640.0 ng/g) and lowest in the roots (14839.8 ng/g). Compared with other production areas, the total content of plants from Dujiangyan was the highest at 82013.9 ng/g (value range of ten areas: 82013.9–42278.5 ng/g). The results also show significant differences in the distribution of withanolides in the different plant parts, as well as across different production areas. This is a breakthrough report providing a simultaneous qualitative and quantitative analysis of 22 withanolides in D. metel L. It could be the basis for the more rational use of various parts of D. metel L., and the expansion of medicinal resources. This work also lays a solid foundation for research on the quality control of D. metel L.

Formyl peptide receptors (FPRs) are G protein-coupled chemoattractant receptors expressed mainly in phagocytic leukocytes. High expression of FPRs has also been detected in several cancers but the functions of FPR1 in tumor invasion and metastasis is poorly understood. In this study, we investigated the expression of FPRs in primary human colorectal cancer (CRC) and analyzed the association of FPRs expression with clinicopathological parameters. The levels of FPRs mRNA, especially those of FPR1, were significantly higher in colorectal tumors than in distant normal tissues and adjacent non-tumor tissues. FPR1 mRNA expression was also associated with tumor serosal infiltration. FPR1 protein expression was both in the colorectal epitheliums and tumor infiltrating neutrophils/macrophages. Furthermore, the functions of FPR1 in tumor invasion and tissue repair were investigated using the CRC cell lines SW480 and HT29. Higher cell surface expression of FPR1 is associated with significantly increased migration in SW480 cells compared with HT29 cells that have less FPR1 membrane expression. Finally, genetic deletion of fpr1 increased the survival rate of the resulting knockout mice compared with wild type littermates in a mouse model of colitis-associated colorectal cancer. Our data demonstrate that FPR1 may play an important role in tumor cell invasion in CRC patients.

Five undescribed ergostane-type C

With the development of the Internet era, urban logistics distribution increases. At the same time, the state vigorously promotes the development of the new energy automobile industry and the continuous strengthening of people’s awareness of environmental protection, new energy vehicles began to be favored by logistics enterprises. From the analysis of the national support policy for new energy vehicles, the development of new energy vehicles in recent years and the TCO calculation of their cost advantages, this paper clarifies that new energy vehicles will occupy the mainstream position in urban logistics distribution.

Esculentoside B (EsB, also named phytolaccagenin 3- O -β- d -xylopyranoside), a pentacyclic triterpene isolated from herbal medicine Radix phytolaccae , has been found to possess multiple pharmacological activities. Nonetheless, the low content in nature and the difficulties in the total synthesis of EsB strongly limit its extensive investigations and further development as a drug candidate. This study aims to provide a practical method for highly efficient preparation of EsB using esculentoside A (EsA, phytolaccagenin 3- O -β- d -glucopyranosyl (1 → 4)-β- d -xylopyranoside) as the starting material. β- d -glucosidase from snailase was used to catalyze the formation of EsB, and the product was then purified and fully characterized by both HRMS and NMR. To prepare EsB in a more cost-effective way, response surface methodology (RSM) was used to explore the potential effects of the reaction conditions (such as reaction temperature, pH, enzyme load, and reaction time) on the conversion rates of EsA. The highest EsB yield of 0.66 mg/ml was obtained experimentally under optimized conditions as follows: temperature 48.28 °C, pH 6.4, enzyme load 4.43%, and reaction time 2.73 h. This result agreed well with the predicted yield of 0.68 mg/ml by RSM. The enzymatic kinetics of this biotransformation was characterized at the optimum pH and temperature. The S 50 value was evaluated as 167.4 μM, while the V max value was 345.6 nmol/min/mg. In summary, this study provided a mild and practical method for the highly efficient preparation of EsB from EsA, which held great promise for large scale production of EsB.

The paper explores the connection of Graph-Lagrangians and its maximum cliques for 3-uniform hypergraphs. Motzkin and Straus showed that the Graph-Lagrangian of a graph is the Graph-Lagrangian of its maximum cliques. This connection provided a new proof of Turan classical result on the Turan density of complete graphs. Since then, Graph-Lagrangian has become a useful tool in extremal problems for hypergraphs. Peng and Zhao attempted to explore the relationship between the Graph-Lagrangian of a hypergraph and the order of its maximum cliques for hypergraphs when the number of edges is in certain range. They showed that if G is a 3-uniform graph with m edges containing a clique of order t − 1, then λ(G) = λ([t − 1](3)) provided $$\left( {\begin{array}{*{20}{c}} {t - 1} \\ 3 \end{array}} \right) \leqslant m \leqslant \left( {\begin{array}{*{20}{c}} {t - 1} \\ 3 \end{array}} \right) + \left( {\begin{array}{*{20}{c}} {t - 2} \\ 2 \end{array}} \right)$$ . They also conjectured: If G is an r-uniform graph with m edges not containing a clique of order t − 1, then λ(G) < λ([t − 1](r)) provided $$\left( {\begin{array}{*{20}{c}} {t - 1} \\ r \end{array}} \right) \leqslant m \leqslant \left( {\begin{array}{*{20}{c}} {t - 1} \\ r \end{array}} \right) + \left( {\begin{array}{*{20}{c}} {t - 2} \\ {r - 1} \end{array}} \right)$$ . It has been shown that to verify this conjecture for 3-uniform graphs, it is sufficient to verify the conjecture for left-compressed 3-uniform graphs with $$m = \left( {\begin{array}{*{20}{c}} {t - 1} \\ 3 \end{array}} \right) + \left( {\begin{array}{*{20}{c}} {t - 2} \\ 2 \end{array}} \right)$$ . Regarding this conjecture, we show: If G is a left-compressed 3-uniform graph on the vertex set [t] with m edges and |[t − 1](3) E(G)| = p, then λ(G) < λ([t− 1](3)) provided $$m = \left( {\begin{array}{*{20}{c}} {t - 1} \\ 3 \end{array}} \right) + \left( {\begin{array}{*{20}{c}} {t - 2} \\ 2 \end{array}} \right)$$ and t ≥ 17p/2 + 11.

To develop a practical method to prepare tilianin by highly selective and efficient hydrolysis of the C-7 rhamnosyl group from linarin.Naringinase was utilized to selectively catalyze the formation of tilianin using linarin as the starting material. The reaction conditions, including temperature, pH, metal ions, substrate concentration and enzyme concentration, were optimized. At 60 °C, naringinase showed enhanced α-L-rhamnosidase activity while the β-D-glucosidase activity was abrogated. The addition of Mg(2+), Fe(2+) and Co(2+) was also beneficial for selective biotransformation of linarin to tilianin. Under the optimized conditions (pH 7.0 at 60 °C), linarin could be nearly completely transformed to tilianin with excellent selectivity (98.9 %), while that of the by-product acacetin was less than 1.1 %. In addition, the structure of target product tilianin was fully characterized by HR-MS and (1)H-NMR.A highly selective and efficient biotransformation of linarin to tilianin was developed by the proper control of incubation temperature, which enhanced the α-L-rhamnosidase activity of naringinase and blocked its β-D-glucosidase activity.

A generalized mathematical model, which describes the process of lithium extraction/insertion in active material particles of insertion cathodes, is developed from linear non-equilibrium thermodynamics and the principle of electroneutrality. The model reveals theoretical relations between the intrinsic and apparent transport parameters of lithium-ions and electrons. Calculation formulas for apparent lithium-ion diffusion coefficient D 1 ⁎ are deduced from the model. A simple trial calculation is introduced to evaluate the cross-phenomenological coefficient of the Onsager reciprocal relationship. By means of referenced intrinsic diffusion coefficients, calculated by ab initio methods, calculations of D 1 ⁎ upon charge/discharge for the lithium iron phosphate cathode material (FePO 4 /LiFePO 4 ) are presented. The calculated values of D 1 ⁎ are within those previously measured experimentally. In the range of lithium ion contents 0.02 ≤ x ≤ 1.0, the values of D 1 ⁎ during charge/discharge vary in the range 10 − 12 –10 − 14 cm 2 s − 1 and decrease with increasing x . The mean value of D 1 ⁎ is about 10 − 13 cm 2 s − 1 , which is five to six orders of magnitude lower than the intrinsic diffusion coefficients. The calculation results indicate that lithium ion diffusion in the active material particles is coupled with electron conduction, and the co-diffusion of lithium ions and electrons is limited by the electron conduction due to the low intrinsic conductivity of FePO 4 /LiFePO 4 .

Methylglyoxal (MGO)-induced carbonyl stress and pro-inflammatory responses have been suggested to contribute to endothelial dysfunction. Curcumin (Cur), a polyphenolic compound from Curcuma longa L., may protect endothelial cells against carbonyl stress-induced damage by trapping dicarbonyl compounds such as MGO. However, Cur-MGO adducts have not been studied in depth to date and it remains to be known whether Cur-MGO adducts are able to attenuate endothelial damage by trapping MGO. In the present study, 1,2-diaminobenzene was reacted with MGO to ensure the reliability of the reaction system. Cur was demonstrated to trap MGO at a 1:1 ratio to form adducts 1, 2 and 3 within 720 min. The structures of these adducts were identified by high-performance liquid chromatography/electrospray ionization tandem mass spectrometry. The kinetic curves of Cur (10(-7), 10(-6) and 10(-5) M) were measured from 0-168 h by fluorescent intensity. Cur significantly inhibited the formation of advanced glycation end products (AGEs). The differences in oxidative damage and the levels of pro-inflammatory cytokines following MGO + HSA or Cur-MGO treatment were investigated in human umbilical vein endothelial cells (HUVECs). Exposure of HUVECs to the Cur-MGO reaction adducts significantly reduced the intracellular ROS levels and improved cell viability compared with MGO alone. Furthermore, there was a significant reduction in the expression levels of transforming growth factor-β1 and intercellular adhesion molecule(-1) following treatment with Cur-MGO adducts compared with MGO alone. These results provide further evidence that the trapping of MGO by Cur inhibits the formation of AGEs. The current study indicates that the protective effect of Cur on carbonyl stress and pro-inflammatory responses in endothelial damage occurs via the trapping of MGO.

In this paper, we construct two simplest conforming rectangular elements for the linear elasticity problem under the Hellinger-Reissner variational principle. One is a rectangular element in 2D with only 8 degrees of freedom for the stress and 2 degrees of freedom for the displacement. Another one is a cubic element in 3D with only 18?+?3 degrees of freedom. We prove that the two elements are stable and anisotropic convergent. Numerical test is presented to illustrate the element is stable and effective.

A novel topology circuit of active compensation was discussed to be used to manage negative sequence caused by locomotive load in electrified railway. The main circuit used a three-phase two-leg compensator as active elements of shunt hybrid active compensator topology. The number of switch device in this topology was reduced by comparing with three-phase full-bridge active inverter and the cost was lower. The simulation model was developed with SIMULINK. The simulating results indicates that the shunt hybrid active compensator can restrain the problem of negative sequence which generated by locomotive load, and reduces the effect of reactive power, negative sequence, improves electric energy quality and verifies the correctness of the proposed structure and control method.

Autophagy plays an important role in the pathogenesis of Alzheimerʼs disease. In the present study, the blockade mechanism of emodin on amyloid-β 25–35-induced neurotoxicity was explored. Cell viability of PC12 cells was evaluated by the MTT assay and neuro damage by the lactate dehydrogenase leakage assay. Gene silencing by small interfering RNA, cDNA constructs and transfection, as well as Western blot were performed to assess protein expression levels. AβPP/PS1 mice were administered orally with emodin (50 mg/kg/day), and LC3-II positive cells in their brain cortex sections were detected by immunohistochemical staining. Emodin could significantly inhibit the LC3-I/LC3-II conversion ratio and cell viability while decreasing the lactate dehydrogenase level in AβPP/PS1 mice and PC12 cells. LC3II positive cells in the cortex were decreased significantly by the treatment with both emodin and 3-methyladenine. Furthermore, emodin and 3-methyladenine could increase B-cell lymphoma 2 while decreasing Beclin-1 and hVps34 expressions, which were induced by amyloid-β 25–35. Small interfering gene silencing Beclin-1 and B-cell lymphoma 2 confirmed this signaling pathway. We also found that the phosphatidylinositol 3-kinase inhibitor LY294002 could block LC3-I/LC3-II conversion and increase B-cell lymphoma 2 while decreasing hVps34 and Beclin-1 expressions. The results suggest that the blockade of emodin on amyloid-β 25–35-induced autophagy may occur via the activation of the class III phosphatidylinositol 3-kinase/Beclin-1/B-cell lymphoma 2 pathway. Our results provide confirmatory evidence for the application of emodin in the prevention and treatment of Alzheimerʼs disease.

Background: To study the characters of high-frequency oscillations (HFOs) in the seizure onset zones (SOZ) and the nonseizure onset zones (NSOZ) in the electrocorticography (ECoG) of patients with neocortical epilepsy. Methods: Only patients with neocortical epilepsy who were seizure-free after surgery as determined with ECoG were included. We selected patients with normal magnetic resonance imaging before surgery in order to avoid the influence of HFOs by other lesions. Three minutes preictal and 10 min interictal ECoG as recorded in 39 channels in the SOZ and 256 channels in the NSOZ were analyzed. Ripples and fast ripples (FRs) were analyzed by Advanced Source Analysis software (ASA, The Netherlands). Average duration of HFOs was analyzed in SOZ and NSOZ separately. Results: For ripples, the permillage time occupied by HFOs was 0.83 in NSOZ and 1.17 in SOZ during the interictal period. During preictal period, they were 2.02 in NSOZ and 7.93 in SOZ. For FRs, the permillage time occupied by HFOs was 0.02 in NSOZ and 0.42 in SOZ during the interictal period. During preictal period, they were 0.03 in NSOZ and 2 in SOZ. Conclusions: High-frequency oscillations are linked to SOZ in neocortical epilepsy. Our study demonstrates the prevalent occurrence of HFOs in SOZ. More and more burst of HFOs, especially FRs, means the onset of seizures.

This project is to investigate lignans from the dried fruits of Xanthium sibiricum (Xanthii Fructus). The chemical constituents were extract by 70% ethanol and isolated by silica gel, ODS, Sephadex LH-20, MCI column chromatography. Based on comparison of their spectral data with those reported in literature, they were elucidated as (-)-pinoresinol (1), balanophonin A (2), diospyrosin (3), dehydrodiconiferyl alcohol (4), 2-(4-hydroxy-3-methoxyphenyl)-3-(2-hydroxy-5-methoxyphenyl)-3-oxo-1-propanol (5), (-)-simulanol (6), (-)-7R,8S-dehydrodiconiferyl alcohol (7), chushizisin E (8), dihydrodehydrodiconiferyl alcohol (9), 7R,8S-dihydrodehydrodiconiferyl alcohol 4-O-β-D-glucopyranoside (10), erythro-1,2-bis(4-hydroxy-3-methoxyphenyl)-1,3-propanediol (11), leptolepisol D (12), 8-O-4' neolignan 4-O-β-glucopyranoside (13), (-)-1-O-β-D-glucopyranosyl-2-{2-methoxy-4-[1-(E)-propen-3-ol]phenoxyl}-propane-3-ol(14), 1-(4-hydroxy-3-methoxy)-phenyl-2-[4-(1,2,3-trihydroxypropyl)-2-methoxy]-phenoxy-1,3-propandiol (15), threo-dihydroxy dehydrodiconiferyl alcohol (16), (-)-(2R)-1-O-β-D-glucopyranosyl-2-{2-methoxy-4-[(E)-formylviny1]phenoxyl} propane-3-ol (17). Compound 2-17 were isolated from the genus Xanthium for the first time. Compound 1 were isolated form Xanthii Fructus for the first time.

In this paper, the observability analysis method based on meter placement was employed. Each consumer is classified, and the Distributed Generation (DG) is considered as a special negative load with constant power, which contains two types: photovoltaic (PV) power and wind turbine generation (WTG). The load variation is represented using typical load patterns. An efficient graph partitioning method is adopted to partition the weighted tree in the performing meter placement to achieve the network observability. Then an algorithm of optimization meter placement based on observability degree is presented to improve the state estimation accuracy. Finally, the validity of the proposed method has been tested in the IEEE 33-bus distribution network.

In this paper, we proposed a novel hidden Markov model (HMM) to approximate the characteristic of the Nakagami Fading channel. Our study is based on a Hidden Markov Model (HMM). The channel switches between ‘good’ and ‘bad’ channel situation. The transition between the sub-states of the channel is governed by a Markov Chain, which some self-return state is hidden. The performance of the model is studied by simulating probability density functions (PDF), cumulative distribution functions (CDF), level cross rate (LCR) and average fade duration (AFD).