In Vitro Investigation on the Effect of Dendrobine on the Activity of Cytochrome P450 Enzymes.

Dendrobine is the major active ingredient of Dendrobium nobile, Dendrobium chrysotoxum, and Dendrobium fimbriatum, all of which are used in traditional Chinese medicine owing to their antitumor and anti-inflammation activities. Hence, investigation on the interaction of dendrobine with cytochrome P450 enzymes could provide a reference for the clinical application of Dendrobium. The effects of dendrobine on cytochrome P450 enzymes activities were investigated in the presence of 0, 2.5, 5, 10, 25, 50, and 100 µM dendrobine in pooled human liver microsomes. The specific inhibitors were employed as the positive control and the blank groups were set as the negative control. The Lineweaver-Burk plots were plotted to characterize the specific inhibition model and obtain the kinetic parameters. The study reveals that dendrobine significantly inhibited the activity of CYP3A4, 2C19, and 2D6 with IC50 values of 12.72, 10.84, and 15.47 µM, respectively. Moreover, the inhibition of CYP3A4 was found to be noncompetitive (Ki = 6.41 µM) and time dependent (KI = 2.541 µM-1, Kinact = 0.0452 min-1), while the inhibition of CYP2C19 and 2D6 was found to be competitive with the Ki values of 5.22 and 7.78 µM, respectively, and showed no time-dependent trends. The in vitro inhibitory effect of dendrobine implies the potential drug-drug interaction between dendrobine and CYP3A4-, 2C9-, and 2D6-metabolized drugs. Nonetheless, these findings need further in vivo validation.

[Change in Granulation Potential and Microbial Enrichment Characteristics of Sludge Induced by Microplastics].

Microplastics (MPs), as a new type of pollutant, are widely detected in sewage treatment plants. Currently, research on MPs in traditional sewage treatment systems has mainly been focused on the pollution level and distribution characteristics, with a lack of studying the impact of MPs on the sludge granulation. In order to explore the effect of MPs on the granulation process, a microplastic exposure test was conducted by adding polyethylene terephthalate microplastics (PET-MPs), which are widespread in the environment. The operating performance of the system, extracellular polymeric substance (EPS) composition, and flora enrichment were analyzed on the sludge granulation. The results showed that the exposure of PET-MPs significantly accelerated the sludge granulation process, whereas the increase in EPS content dominated by PN enhanced the sludge surface hydrophobicity; the granulation rate and EPS secretion were proportional to the exposed particle size. Microplastics and EPS secretions synergistically promoted the formation of granular sludge. However, continuous microplastic exposure led to deterioration of the system decontamination performance and inhibited the degradation process of pollutants, with the most negative effect of nitrite nitrogen accumulation under 250 µm PET-MPs exposure, as high as (5.08±0.24) mg·L-1. The high-throughput sequencing revealed that the microbial community diversity fell in the experimental group. The dominant bacteria at the phylum level were Proteobacteria and Bacteroidota on the sludge granulation. Rhodocyclaceae, Sphingomonadaceae, Flavobacteriaceae, and Rhodanobacteraceae promoted flocculation by increasing EPS secretion. The decrease in Comamonadaceae and Chitinophagaceae weakened the ammonia and nitrite oxidation capacity of the system, whereas the decrease in Rhodobacteraceae, Hyphomonadaceae, and Xanthomonadaceae inhibited the removal of nitrate nitrogen.

National Institute of Health Stroke Scale was associated with the immediate and long-term prognosis of patients with acute ischemic stroke treated with intravenous thrombolysis.

OBJECTIVE: The objective of this study was to examine whether the National Institute of Health Stroke Scale was associated with the short- and long-term prognosis of patients with acute ischemic stroke treated with intravenous thrombolysis. METHODS: A total of 247 patients with acute ischemic stroke admitted to the hospital from April 2019 to October 2020 were retrospectively selected as study subjects, and the immediate and long-term prognosis after thrombolysis was assessed using the modified Rankin Scale and divided into good prognosis group (119 cases) and poor prognosis group (128 cases) based on the effect of thrombolysis. Both groups were treated with alteplase, the National Institute of Health Stroke Scale of the two groups was compared, and the factors affecting the prognosis of acute ischemic stroke were analyzed. RESULTS: After intravenous thrombolysis, 24 h, and 7 days of treatment, the National Institute of Health Stroke Scale in the poor prognosis group was higher than those of patients in the good prognosis group, and the differences were statistically significant (p<0.05). The results of the multivariate analysis suggested that National Institute of Health Stroke Scale before treatment was an independent factor associated with the 3-month (OR: 1.068, 95%CI 1.015-1.123, p=0.011) and long-term poor prognosis (OR: 1.064, 95%CI 1.012-1.119, p=0.015) in patients with acute ischemic stroke receiving intravenous thrombolysis after adjustment of age, gender, body mass index, smoking, alcohol consumer, onset-to-door time, door-to-needle time, and imaging score. CONCLUSION: The National Institute of Health Stroke Scale could be a promising indicator for the prognosis, and active intervention is needed to improve the quality of life in patients with acute ischemic stroke.

Recent advances in luminescence and aptamer sensors based analytical determination, adsorptive removal, degradation of the tetracycline antibiotics, an overview and outlook.

Tetracycline antibiotics (TCs), one of the important antibiotic groups, have been widely used in human and veterinary medicines. Their residues in foodstuff, soil and sewage have caused serious threats to food safety, ecological environment and human health. Here, we reviewed the potential harms of TCs residues to foodstuff, environment and human beings, discussed the luminescence and aptamer sensors based analytical determination, adsorptive removal, and degradation strategies of TCs residues from a recent 5-year period. The advantages and intrinsic limitations of these strategies have been compared and discussed, the potential challenges and opportunities in TCs residues degradation have also been deliberated and explored.

[Post-marketed re-evaluation of fleabane injection and Dengzhan Shengmai capsule study on treatment in patients with ischemic stroke].

OBJECTIVE: To verify the efficacy and safety of post-marketed fleabane injection combined with Dengzhan Shengmai capsules in the treatment of ischemic stroke (IS). METHOD: A multicentre, prospective, practical, randomized controlled study was carried out to compare the efficacy and safety of Dengzhan group (n = 343) and western medicine group (n = 335), appling "clinical study central stochastic system". The treatment of Dengzhan group is using fleabane injection in acute stage and Dengzhan Shengmai capsules in convalescence. The primary indexes of effect evaluation are the important outcome events in 360 days' follow-up, including mortality, recurrence, disability and quality of life to reflect the effect of clinical study. The indexes of safety evaluation involve laboratory examination results and incidence of adverse events. RESULT: After 360 days' follow-up, 4 people died of IS in Dengzhan group, and the mortality rate of which is 1.17%, while 16 died in Western medicine group (WM group), and the mortality rate is 4.78%, suggesting that the mortality rate of Dengzhan group is significantly lower than WM group (P<0.05). Eleven cases recurred in Dengzhan group, and the recurrence rate of which is 3.21%, while 12 recurred in WM group, and the recurrence rate is 3.59%, indicating that the recurrence rate of Dengzhan group is slightly lower than WM group. The disability rate of Dengzhan group is 39.53%, among which the rate of severely disabled cases are 1.49%, while the disability rate of WM group is 40.13%, among which the rate of severely disabled cases are 3.13%, suggesting that the disability rate of Dengzhan group is lower and the severity of disability is also lighter than WM group. In the field of quality of life, the activity ability and the upper limb function store of stroke patients in Dengzhan group improved far much better than WM group (P<0.05). Analysis of safety suggested that, adverse events occurred in 11 cases in Dengzhan group, among which 4 cases is related with the drug treatment, the incidence of adverse events of which is 1.17%, and the main manifestations involve fever and chilling, rash, nausea, dizziness, palpitation, etc. which were all appeared after the treatment of fleabane injection, and disappeared 1 to 2 days after drug withdrawal. 13 cases occurred abnormal liver function and 2 cases abnormal kidney function in Dengzhan group. According to the judgment of clinical physicians, 3 case of ALT abnormality is possibly related to the treatment, the others are all unrelated with the treatment. CONCLUSION: Fleabane injection and Dengzhan Shengmai capsules are all safe and effective TCM in the treatment of ischemic stroke.

[Post-marketing re-evaluation of Kudiezi injection study on early treatment in patients with ischemic stroke].

OBJECTIVE: To study the effect and safety of Kudiezi injection on patients with acute ischemic stroke. METHOD: Seven hundreds patients were divided into two groups by central randomization system. The study group, 346 cases, was treated with kudiezi injection plus traditional Chinese medicine (TCM) synthesis rehabilitation project, and the control group, 354 cases, was treated with synthetic rehabilitation project. The patients were treated for 10 to 21 days. Before treatment and at the 7th, 14th and 21th day of treatment, the indexes include NIHSS used for evaluating the neurological deficit degree and the motor function score (Fugl-Meyer) for evaluating motor function were observed. The safety index is defined by adverse observation event and laboratory test. The incidence of adverse events and laboratory tests results were observed before and after treatment at the same time. RESULT: Application of generalized estimating equation model, we found that as the treatment time, NIHSS score and FMI score of the two groups showed a trend of improvement. And at the 14th days and 21th days of treatment, compared to the control group the treatment group showed significant statistical difference on the impact of NIHSS and FMI (P<0.05). No serious adverse events were observed. CONCLUSION: Kudiezi injection plus TCM rehabilitation project of ischemic stroke showed some superiority to western medicine rehabilitation program on improving the neurological deficit and motor function. Kudiezi injection is safe and effective in the treatment of acute ischemic stroke.

Risk factors for ischemic stroke: differences between cerebral small vessel and large artery atherosclerosis aetiologies.

The treatment for large artery atherosclerosis (LAA) stroke is also important for patients with cerebral small vessel disease (SVD). Our aim is to clarify the risk factors for ischemic cerebral SVD and to evaluate the different risk factor profiles of the two ischemic stroke subtypes, namely, ischemic cerebral SVD and LAA. A total of 353 patients with acute ischemic stroke were assigned to two groups according to the Trial of ORG 10172 in Acute Stroke Treatment (TOAST) criteria: the ischemic cerebral SVD group and the LAA group. A total of 70 non-stroke patients admitted during the same period served as the control group. Clinical variables were collected, including age, sex, blood pressure, blood glucose, triglycerides, low-density lipoprotein, total cholesterol (TC), smoking history, drinking history, coronary atherosclerotic heart disease and family history of a high-risk disease. Multivariate logistic regression (MLR) analyses were performed. MLR analysis showed that risk factors for LAA stroke included hypertension, diabetes mellitus, high low-density lipoprotein, hypertriglyceridemia and smoking compared with the control group. The analysis also showed that the risk factors for cerebral SVD stroke were hypertension, diabetes mellitus, high TC, hypertriglyceridemia and smoking. In terms of the factors distinguishing LAA and cerebral SVD, MLR demonstrated that high TC played prominent roles in cerebral SVD. Hypertension, diabetes mellitus, high total cholesterol, hypertriglyceridemia and smoking are independent risk factors for cerebral SVD stroke. Compared with the LAA stroke group, patients with cerebral SVD stroke were more likely to have a high level of TC.

[Malonato(2-)-κO,O']bis-(1,10-phenanthroline-κN,N')zinc(II) penta-hydrate.

In the title complex, [Zn(C(3)H(2)O(4))(C(12)H(8)N(2))(2)]·5H(2)O, the Zn(II) cation displays a distorted octa-hedral geometry, being coordinated by four N atoms from two 1,10-phenanthroline ligands and two O atoms from different carboxyl-ate groups of the chelating malonate dianion. In the crystal, the complexes are linked into a three-dimensional supra-molecular network by both O-H⋯O hydrogen-bonding inter-actions between water mol-ecules and the uncoordinated carboxyl-ate O atoms of neighboring mol-ecules, and aromatic π-π stacking inter-actions between neighboring phenanthroline rings with centroid-centroid distances of 3.4654 (17) and 3.697 (2) Å.

Bis{µ-1,3-bis-[2-(5-bromo-2-oxidobenzyl-idene-amino)ethyl]-2-(5-bromo-2-oxido-phenyl)-1,3-imidazolidine}dineo-dymium(III) N,N-dimethyl-formamide hexa-solvate.

In the title centrosymmetric dinuclear complex, [Nd(2)(C(27)H(24)Br(3)N(4)O(3))(2)]·6C(3)H(7)NO, the Nd(III) ion is coordinated in a slightly distorted square-anti-prismatic geometry by four N atoms and four O atoms from two centrosymmetrically-related 1,3-bis-[2-(5-bromo-2-oxidobenzyl-amino)eth-yl]-2-(5-bromo-2-oxidophen-yl)-1,3-imidazolidine ligands. The Nd⋯Nd separation is 4.5012 (12) Å.

{4,4'-Dibromo-2,2'-[ethane-1,2-diylbis(nitrilo-methyl-idyne)]diphenolato}copper(II).

In the title compound, [Cu(C(16)H(12)Br(2)N(2)O(2))], the Cu(II) atom is coordinated in a slightly distorted square-planar geometry by two O and two N atoms of the tetra-dentate dianionic 4,4'-dibromo-2,2'-[ethane-1,2-diylbis(nitrilo-methyl-idyne)]diphen-olate Schiff base ligand.

Withdrawal Notice: STK33-Dependent Transcriptional Regulation of SFTA3 Induces Cisplatin-Resistance in Lung Adenocarcinoma

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A dinuclear copper complex: bis-(µ-4-amino-benzoato)bis-[aqua(1,10-phenanthroline)copper(II)] dichloride bis(4-amino-benzoic acid) dihydrate.

The title complex, [Cu(2)(C(7)H(6)NO(2))(2)(C(12)H(8)N(2))(2)(H(2)O)(2)]·2C(7)H(7)NO(2)·2H(2)O, consists of a dinuclear [Cu(2)(C(7)H(6)NO(2))(2)(C(12)H(8)N(2))(2)(H(2)O)(2)](2+) cation, two Cl(-) anions, two 4-amino-benzoic acid mol-ecules and two disordered water mol-ecules (site occupancy factors 0.5). The Cu(II) ion adopts a distorted square-pyramidal geometry formed by two N atoms from the 1,10-phenanthroline ligand and two O atoms of the two 4-amino-benzoic acid ligands and one water O atom. The Cu⋯Cu separation is 3.109 (2) Å. A twofold axis passes through the mid-point of the Cu⋯Cu vector.

National Institute of Health Stroke Scale was associated with the immediate and long-term prognosis of patients with acute ischemic stroke treated with intravenous thrombolysis

OBJECTIVE: The objective of this study was to examine whether the National Institute of Health Stroke Scale was associated with the short- and long-term prognosis of patients with acute ischemic stroke treated with intravenous thrombolysis. METHODS: A total of 247 patients with acute ischemic stroke admitted to the hospital from April 2019 to October 2020 were retrospectively selected as study subjects, and the immediate and long-term prognosis after thrombolysis was assessed using the modified Rankin Scale and divided into good prognosis group (119 cases) and poor prognosis group (128 cases) based on the effect of thrombolysis. Both groups were treated with alteplase, the National Institute of Health Stroke Scale of the two groups was compared, and the factors affecting the prognosis of acute ischemic stroke were analyzed. RESULTS: After intravenous thrombolysis, 24 h, and 7 days of treatment, the National Institute of Health Stroke Scale in the poor prognosis group was higher than those of patients in the good prognosis group, and the differences were statistically significant (p<0.05). The results of the multivariate analysis suggested that National Institute of Health Stroke Scale before treatment was an independent factor associated with the 3-month (OR: 1.068, 95%CI 1.015-1.123, p=0.011) and long-term poor prognosis (OR: 1.064, 95%CI 1.012-1.119, p=0.015) in patients with acute ischemic stroke receiving intravenous thrombolysis after adjustment of age, gender, body mass index, smoking, alcohol consumer, onset-to-door time, door-to-needle time, and imaging score. CONCLUSION: The National Institute of Health Stroke Scale could be a promising indicator for the prognosis, and active intervention is needed to improve the quality of life in patients with acute ischemic stroke.

Knockdown of RRS1 by lentiviral-mediated RNAi promotes apoptosis and suppresses proliferation of human hepatocellular carcinoma cells.

In recent years it was found that the synthesis and biological activity of ribosomes are closely associated with tumor cell growth, tumorigenesis, and malignant transformation. However, the role of regulator of ribosome synthesis 1 (RRS1) in hepatocellular carcinoma (HCC) has not yet been reported. In the present study, we aimed to examine the potential role of RRS1 in tumor cell growth by using a lentivirus-mediated RNA interference (RNAi) system in the HCC cell line SMMC-7721 in vitro. Compared with that of the negative control group (Lv-shCon), the mRNA and protein expression levels of RRS1 in SMMC-7721 cells transfected with Lv-shRRS1 were significantly decreased. Further experiments found that silencing of RRS1 gene expression in SMMC-7721 cells significantly suppressed cell proliferation, inhibited colony formation capacity, increased apoptosis and arrested cells in the G1 phase. These results suggest that the RRS1 gene plays a critical role in cell proliferation, colony formation, cell apoptosis and cell cycle distribution in human HCC cells, and that silencing of RRS1 by RNAi is a promising therapeutic approach for the treatment of HCC, and should be further developed.

[Plum-blossom needle tapping at Jiaji(EX-B 2) combined with rehabilitation for ataxia of cerebellar apoplexy: a randomized controlled trial].

OBJECTIVE: To compare the effects between plum-blossom needle tapping at Jiaji (EX-B 2) combined with rehabilitation and simple rehabilitation for ataxia of cerebellar apoplexy. METHODS: Sixty patients with ataxia of cerebellar apoplexy were randomly divided into an observation group,and a control group,30 cases in each one. Conventional rehabilitation training was applied in the control group. While based on the treatment as that of the control group, plum-blossom needle tapping at Jiaji (EX-B 2) was used in the observation group. All the treatment was given for 4 weeks. International cooperative ataxia rating scale (ICARS), Berg balance scale (BBS) and Barthel index (BD were observed before treatment,after 2-week treatment and 4-week treatment. Also, clinical effects After treating for 2 weeks and for 4 weeks, the results of ICARS,BBS and BI were obvi were compared. RESULTS: After treating for 2 weeksand for 4 weeks, the results of ICARS, BBS and BI were obviously better than those before treatment in the two groups (all P<0.05). After 2-week treatment,there was no sta tistical significance between the two groups (all P>0. 05). After 4-week treatment,all the scores of the observation group were apparently superior to those of the control group (all P<0. 05). The total effective rate was 96. 7% (29/30) in the observation group, better than 80. 0% (24/30) in the control group after 4-week treatment (P<0. 05). CCONCLUSION:Plum-blossom needle tapping at Jiaji(EX-B 2) combined with rehabilitation training markedly improve the coordination and balance functions and activities of daily life, which are better than simple rehabilitation.