Aporphine and amide alkaloids from Illigera parviflora.

Three undescribed alkaloids (+)-9-hydroxy-N-acetylnordicentrine (1), illigeparvinine (2), and deca-(2E,4Z)-2,4-dienoic acid 4-hydroxy-2-phenethyl amide (3), along with 19 known analogues (4-22), were isolated from the ethnic medicinal plant Illigera parviflora. Their structures were established using NMR, MS, and other spectroscopic analyses as well as X-ray diffraction. Moderate inhibition of human gastric carcinoma (MGC-803) and breast adenocarcinoma (T-47D) cell lines proliferation was observed for actinodaphnine (4) with IC50 values of 28.74 and 11.65 µM, respectively. These findings contribute new anticancer potential compounds and expand the chemical diversity known from the valuable traditional medicinal plant I. parviflora.

[Non-invasive chromosome screening for male infertility patients with severe oligo-astheno-teratozoospermia].

Objective: To explore the value of non-invasive embryo chromosome screening (NICS) in improving the outcomes of clinical pregnancy after assisted reproduction in men with severe oligo-astheno-teratozoospermia (OAT). METHODS: We randomly selected 170 cases of assisted reproduction due to severe OAT from January 2017 to December 2020, 85 undergoing NICS treatmentand the other 85 receiving intracytoplasmic sperm injection (ICSI). We made comparisons between the two groups in the female age, body mass index (BMI), anti-Müllerian hormone level (AMH), basal antral follicle count (AFC), infertility duration, male age, sperm concentration, percentages of progressively motile sperm (PMS) and morphologically normal sperm (MNS), sperm DNA fragmentation index (DFI), numbers of oocytes retrieved and high-quality blastocysts, and rates of normal fertilization, clinical pregnancy and abortion. RESULTS: No statistically significant differences were observed between the two groups in the female age, female BMI, AMH, AFC, infertility duration, male age, sperm concentration, percentages of PMS and MNS, sperm DFI, numbers of oocytes retrieved and high-quality blastocysts, or normal fertilization rate (P > 0.05). The rate of definite diagnosis was 88.24%, and that of embryo chromosome euploidy was 48.56% in the NICS group. The rate of clinical pregnancy after selected euploid embryo transfer was significantly higher in the NICS than in the ICSI group (66.28% vs 51.09%, P < 0.05), while that of abortion remarkably lower in the former than in the latter (12.28% vs 29.79%, P < 0.05). CONCLUSIONS: For male infertility patients with severe OAT, NICS technology can improve the rate of clinical pregnancy and reduce the risk of abortion.

Characterizing Hotspots and Frontier Landscapes of Diabetes-Specific Distress from 2000 to 2018: A Bibliometric Study.

OBJECTIVES: This work aims to comprehensively characterize hotspots and frontier landscapes concerning diabetes-specific distress from 2000 to 2018. Materials and Methods. Firstly, diabetes-specific distress-related literature was retrieved and downloaded from the Web of Science Core Collection (WoSCC). Secondly, WoSCC self-contained toolkits and GraphPad Prism7 were conducted to analyze general characteristics, including literature products, countries, institutes, authors, and journal resource. Finally, CiteSpace V Toolkits was put forward to implement advanced analysis, consisting of keyword-term frequency and co-occurrence, references-cited frequency and co-occurrence, and burst detection for keyword terms and references cited, which uncovers the hotspots and frontiers of diabetes-specific distress. RESULTS: After preprocessing, our study included a total of 1051 papers concerning diabetes-specific distress. Publication outputs increased smoothly year by year. Compared with other journals, diabetic medicine delivered the largest number of documents. The United States occupied the leading positions, and the most productive institution was the University of California System in terms of literature products. Fisher L. has the highest references-cited frequency. Prevalence of diabetes-specific distress, diabetes-specific distress and glycemic control, diabetes-specific distress and depression comorbidity, and diabetes-specific distress and risk factors were the research hotspots, whereas the measure of diabetes-specific distress and latent and serious/severe diabetes-specific distress was the research frontiers. CONCLUSIONS: Overall, our study may inspire researchers to show great interest in diabetes-specific distress in the next few years.

A comparative analysis of derivatization strategies for the determination of biogenic amines in sausage and cheese by HPLC.

The six biogenic amines in sausage and cheese were analyzed by HPLC with UV detection after off-line derivatization with dansyl chloride, 9-fluorenylmethoxycarbonyl chloride, benzoyl chloride and dabsyl chloride, respectively. The results showed that both the off-line 9-fluorenylmethoxycarbonyl and dabsyl derivatization were not suitable for HPLC analysis of biogenic amines when batch injection was used because the derivatives were instable, whereas both the off-line dansyl and benzoyl derivatization were suitable for HPLC analysis of biogenic amines when batch injection was used, but the latter needed to maintain the derivatives at 4 °C to ensure that benzoylated tyramine was not degraded when waiting for the analysis. The off-line dansyl derivatization had an obvious advantage in the analysis of biogenic amines in sausage and cheese samples by HPLC combined with batch injection because the method has a wider linear range and higher sensitivity, accuracy, precision and stability of the derivatives.

Outpatient Experience of Human Caring Scale (OEHC-Scale): Improvement by Delphi Method.

Based on the outpatient interview and literature review, the initial framework of the outpatient experience of human caring scale was formed with 9 dimensions of outpatient process. The research aim was to improve the scale by Delphi method. Sixteen experts in medical management, human caring or medical education were invited to evaluate the importance of the dimensions and items of the scale and provided some expertise via filling out the Delphi consultation questionnaires twice in the consulting round. In the first round, the recovery rate showing the experts' positivity was 80%; the coefficient of reliability (Cr) ascertaining the authority of the evaluation was 0.92; the mean and full mark ratios responding the concentration of the evaluation were 2.88-4.94 and 6.25%-93.75% respectively; the coefficients of variation (CV) and the Kendall's W determining the concordance of the evaluation were 5.06%-52.15% and 0.21-0.24 respectively. In the second round, the recovery rate was 93.75%; the Cr was 0.93; the mean was 3.93-4.93; the full mark ratios were 26.67%-93.33%; the Kendall's W was 0.14-0.31, the CV was 5.25%-23.61%. Via the two-round Delphi study, the scale that included 10 dimensions and 61 items has been improved. Ten dimensions are pre-hospital medical service, guidance, registration, waiting, diagnosis & treatment, paying, inspection & assay, medicine receiving, therapy/injection/transfusion and global evaluation. It was concluded that Chinese scholars have paid high attention to human caring and outpatient experience. The experts have given high agreements about the dimensions which were established with Chinese outpatient process. The dimensions are different from the similar researches about outpatient experience study. In the future, it is necessary to survey the outpatients to test the construct validity, internal consistency reliability and others of the scale to improve the scale.

A retrospective case series of segmental zoster paresis of limbs: clinical, electrophysiological and imaging characteristics.

BACKGROUND: Segmental zoster paresis (SZP) of limbs, characterized by focal weakness of extremity, is recognized as a rare complication of herpes zoster (HZ). The following study analyzes the clinical characteristics and data from electromyography and MRI scans in patients with motor weakness after zoster infection. METHODS: One thousand three hundred ninety-three patients from our database (Shandong Provincial Qianfoshan Hospital) suffering from HZ were retrospectively reviewed from June 2015 to July 2017. Patients who fulfilled the diagnostic criteria for SZP were included in the analysis. The clinical characteristics, as well as electromyography findings and MRI scans were analyzed. RESULTS: SZP was present in 0.57% of patients with HZ (8/1393). The average age of symptom onset in 8 SZP patients was 69 years old (SD: 13, range 47-87). The severity of muscle weakness ranged from mild to severe. The electrophysiological testing revealed the characteristics of axonopathy. Radiculopathy (2/8), plexopathy (2/8), radiculoplexopathy (3/8) and combined radiculopathy and mononeuropathy (1/8) were also identified. MRI revealed hyperintensity of the affected spinal dorsal horns, nerve roots or peripheral nerves. CONCLUSIONS: SZP is associated with obvious limb weakness, nerve axons lesions and localization to nerve roots, plexus or peripheral nerves.

Lethal (2) giant larvae regulates pleural mesothelial cell polarity in pleural fibrosis.

Pleural fibrosis is barely reversible and the underlying mechanisms are poorly understood. Pleural mesothelial cells (PMCs) which have apical-basal polarity play a key role in pleural fibrosis. Loss of cell polarity is involved in the development of fibrotic diseases. Partition defective protein (PAR) complex is a key regulator of cell polarity. However, changes of PMC polarity and PAR complex in pleural fibrosis are still unknown. In this study, we observed that PMC polarity was lost in fibrotic pleura. Next we found increased Lethal (2) giant larvae (Lgl) bound with aPKC and PAR-6B competing against PAR-3A in PAR complex, which led to cell polarity loss. Then we demonstrated that Lgl1 siRNA prevented cell polarity loss in PMCs, and Lgl1 conditional knockout (ER-Cre+/-Lgl1flox/flox) attenuated pleural fibrosis in a mouse model. Our data indicated that Lgl1 regulates cell polarity of PMCs, inhibition of Lgl1 and maintenance of cell polarity in PMCs could be a potential therapeutic treatment approach for pleural fibrosis.

Inhibition of angiotensin II and calpain attenuates pleural fibrosis.

Pleural fibrosis is associated with various inflammatory processes such as tuberculous pleurisy and bacterial empyema. There is currently no ideal therapeutic to attenuate pleural fibrosis. Some pro-fibrogenic mediators induce fibrosis through inflammatory processes, suggesting that blockage of these mediators might prevent pleural fibrosis. The MeT-5A human pleural mesothelial cell line (PMC) was used in this study as an in vitro model of fibrosis; and intra-pleural injection of bleomycin with carbon particles was used as an in vivo mouse model of pleural fibrosis. Calpain knockout mice, calpain inhibitor (calpeptin), and angiotensin (Ang) II type 1 receptor (AT1R) antagonist (losartan) were evaluated in prevention of experimental pleural fibrosis. We found that bleomycin and carbon particles induced calpain activation in cultured PMCs. This in vitro response was associated with increased collagen-I synthesis, and was blocked by calpain inhibitor or AT1R antagonist. Calpain genetic or treatment with calpeptin or losartan prevented pleural fibrosis in a mouse model induced by bleomycin and carbon particles. Our findings indicate that Ang II signaling and calpain activation induce collagen-I synthesis and contribute to fibrotic alterations in pleural fibrosis. Inhibition of Ang II and calpain might therefore be a novel strategy in treatment of pleural fibrosis.

Nrf2 inhibition affects cell cycle progression during early mouse embryo development.

Brusatol, a quassinoid isolated from the fruit of Bruceajavanica, has recently been shown to inhibit nuclear factor erythroid 2-related factor 2 (Nrf2) via Keap1-dependent ubiquitination and proteasomal degradation or protein synthesis. Nrf2 is a transcription factor that regulates the cellular defense response. Most studies have focused on the effects of Nrf2 in tumor development. Here, the critical roles of Nrf2 in mouse early embryonic development were investigated. We found that brusatol treatment at the zygotic stage prevented the early embryo development. Most embryos stayed at the two-cell stage after 5 days of culture (P < 0.05). This effect was associated with the cell cycle arrest, as the mRNA level of CDK1 and cyclin B decreased at the two-cell stage after brusatol treatment. The embryo development potency was partially rescued by the injection of Nrf2 CRISPR activation plasmid. Thus, brusatol inhibited early embryo development by affecting Nrf2-related cell cycle transition from G2 to M phase that is dependent on cyclin B-CDK1 complex.

Protective effects of DL­3­n­butylphthalide in the lipopolysaccharide­induced mouse model of Parkinson's disease.

DL­3­n­butylphthalide (NBP) is extracted from rapeseed and exhibits multiple neuroprotective effects, exerted by inhibiting the inflammatory process, including reducing oxidative stress, improving mitochondrial function and reducing neuronal apoptosis. The present study aimed to investigate the neuroprotective effects of NBP in a lipopolysaccharide (LPS)­induced mouse model of Parkinson's disease (PD). The behavior of mice was assessed using the rotarod test and open­field test, the amount of tyrosine hydroxylase in the substantia nigra pars compacta was evaluated by immunohistochemistry, and the levels of phosphorylated c­Jun N­terminal kinase (JNK), mitogen­activated protein kinase 14 (p38) and extracellular signal­regulated kinase 1 were determined by western blotting. It was demonstrated that the LPS­induced behavioral deficits were significantly improved. LPS­induced dopaminergic neurodegeneration was relieved following treatment with NBP, as determined from tyrosine hydroxylase­positive cells. Phosphorylation of JNK and p38 was significantly inhibited following treatment with NBP. Therefore in the present study, a role for NBP has been established in the treatment of a PD murine model, laying the experimental basis for the treatment of PD with this agent.

ANTITUMOR AND APOPTOTIC EFFECTS OF CUCURBITACIN A IN A-549 LUNG CARCINOMA CELLS IS MEDIATED VIA G2/M CELL CYCLE ARREST AND M-TOR/PI3K/AKT SIGNALLING PATHWAY.

BACKGROUND: The main aim of this study was to demonstrate the antitumor potential of cucurbitacin A on A-549 NSCLC (non-small cell lung cancer cells). The effects of Cucurbitacin A on apoptotic induction, cell physic, cell cycle failure and m-TOR/PI3K/Akt signalling pathway were also investigated in the present study. MATERIALS AND METHODS: MTT assay and clonogenic assay were carried out to study effects of this compound on cell cytotoxicity and colony forming tendency in A-549 cells. Moreover, phase and fluorescence microscopic techniques were used to examine the effects on cell morphology and induction of apoptosis. The effects on cell cycle phase distribution were investigated by flow cytometry and effects on m-TOR/PI3K/Akt signalling proteins were assessed by western blot analysis. RESULTS: Results showed that cucurbitacin A induced dose-dependent cytotoxic effects along with suppressing the colony forming tendency in these cells. Cucurbitacin A also induced morphological changes in these cells featuring chromatin condensation, cell shrinkage and apoptotic body formation. G2/M phase cell cycle collapse was also induced by Cucurbitacin A along with inhibition of expression levels of m-TOR/PI3K/Akt proteins. CONCLUSIONS: In conclusion, cucurbitacin A inhibits cancer growth in A-549 NSCLC cells by inducing apoptosis, targeting m-TOR/PI3K/Akt signalling pathway and G2/M cell cycle.

Comparative Genomic Analysis of Enterovirus 71 Revealed Six New Potential Neurovirulence-associated Sites.

In the present study, the complete genomes of four common (4/EV71/Wenzhou/CHN/2014, 15/ EV71/Wenzhou/CHN/2014, 116/EV71/Wenzhou/ CHN/2014, and 120/EV71/Wenzhou/CHN/2014) and two virulent (11/EV71/Wenzhou/CHN/2014 and 109/EV71/Wenzhou/CHN/2014) enterovirus 71 (EV71) isolates were sequenced and described. They are 7405 bp in length and belong to EV71 sub-genotype C4 (C4a cluster). Nucleotide sequence alignment revealed six nucleotide variations (GP151→TP151, GP199→AP199, GP261→TP261, AP328→CP328, GP422→AP422, and GP437→TP437) in the two virulent isolates within the 5'UTR of the IRES element. RNA secondary structure predictions of IRES and FCE indicated that the common isolates shared similar structures, which were different from those of the virulent isolates. Moreover, the GP114→CP114 and GP151→TP151 mutations in the virulent isolates contributed to the formation of the unique RNA secondary structures in SL II. Furthermore, nucleotide/amino acid sequence alignments of 82 EV71 isolates indicated that six sites (TP488 and CP577 in the 5'UTR; AsnP57 in 2A; IleP56 in 3C; CP10 and AP47 in the 3'UTR) are potentially associated with the neurovirulence of EV71. Finally, the 3D structures of 2A were analogous, whereas the structures of VP1 and 3C were variable.

Application of molecularly imprinted polymers in wastewater treatment: a review.

Molecularly imprinted polymers are synthetic polymers possessing specific cavities designed for target molecules. They are prepared by copolymerization of a cross-linking agent with the complex formed from a template and monomers that have functional groups specifically interacting with the template through covalent or noncovalent bonds. Subsequent removal of the imprint template leaves specific cavities whose shape, size, and functional groups are complementary to the template molecule. Because of their predetermined selectivity, molecularly imprinted polymers (MIPs) can be used as ideal materials in wastewater treatment. Especially, MIP-based composites offer a wide range of potentialities in wastewater treatment. This paper reviews the latest applications of MIPs in wastewater treatment, highlights the development of MIP-based composites in wastewater, and offers suggestions for future success in the field of MIPs.

[Protective effect of epigallocatechin gallate against sperm abnormality in mice].

OBJECTIVE: To investigate the protective effect of epigallocatechin gallate (EGCG) on mouse sperm in vivo. METHODS: A total of 64 six-week-old male Kuming mice were randomly divided into eight groups of equal number to be treated with normal saline (negative control), Cyclophosphamide (CP) at 30 mg/kg (positive control), and CP followed by EGCG (experimental) at 20, 40, and 80 mg/kg, respectively, given every other day for 10 days. At 4 and 5 weeks after treatment, the bilateral testes of the mice were harvested for examination of sperm abnormality. RESULTS: EGCG did not increase the rate of CP-induced sperm abnormality in the mice, but reduced it instead with the prolonged time of treatment. CONCLUSION: EGCG protects mouse sperm in vivo.

Electroacupuncture at ST36 ameliorates gastric emptying and rescues networks of interstitial cells of Cajal in the stomach of diabetic rats.

Depletion of interstitial cells of Cajal (ICC) is certified in the stomach of diabetic patients. Though electroacupuncture (EA) at ST36 is an effective therapy to regulate gastric motility, the mechanisms of EA at ST36 on gastric emptying and networks of ICC remain to be elucidated. The aims of this study were to investigate the effects of EA on gastric emptying and on the alterations of ICC networks. Rats were randomized into the control, diabetic rats (DM), diabetic rats with sham EA (DM+SEA), diabetic rats with low frequency EA (DM+LEA) and diabetic rats with high frequency EA groups (DM+HEA). The expression of c-kit in each layer of gastric wall was assessed by western blotting. The proliferation of ICC was identified by immunolabeling of c-kit and Ki67 as the apoptosis of ICC was examined by TUNEL staining. The results were as follows: (1) Gastric emptying was severely delayed in the DM group, but accelerated in the LEA and HEA group, especially in the LEA group. (2) The expression of c-kit in each layer was reduced apparently in the DM group, but also up-regulated in the LEA and HEA group. (3) Plentiful proliferated ICC (c-kit+/Ki67+) forming bushy networks with c-kit+ cells were observed in the LEA and HEA group, while the apoptotic cells (c-kit+/TUNEL+) were hardly captured in the LEA and HEA group. Collectively, low and high frequency EA at ST36 rescue the damaged networks of ICC by inhibiting the apoptosis and enhancing the proliferation in the stomach of diabetic rats, resulting in an improved gastric emptying.

The complete mitochondrial genome of the giant pill millipede, Sphaerotheriidae sp. (Myriapoda: Diplopoda: Sphaerotheriida).

The complete mitochondrial genome (mitogenome) of the millipede Sphaerotheriidae sp. has been studied. The genome is 14,970 bp long and contains the typical complement of 13 protein-coding genes, 22 transfer RNA genes, and 2 ribosomal RNA genes. Gene order in Sphaerotheriidae sp. mitogenome is assumed to represent the myriapod ground pattern, which is shared by myriapod-chelicerate clade.

[The role of octahedral montone in colonic barrier protection in severe acute pancreatitis rat model.].

OBJECTIVE: To investigate the protective mechanism of octahedral montone in rats with acute pancreatitis. METHODS: Seventy-two SD rats were randomly divided into a sham-operation (SO) group, a severe acute pancreatitis (SAP) group and a treatment with octahedral montone group. Retrograde pancreatic ductal injection of 5% cholate sodium in rats was used to establish SAP models. Sham operation was done with intraperitoneal injection of normal saline. In the treated group octahedral montone was given through enema half hour before inducing SAP model. Then, we evaluate the pancreatic injury and detect the level of TNF-alpha, diamine oxidase (DAO) and endotoxin. Western blot and RT-PCR were used to determine the expressions of the tight junction protein occludin in the endothelial cells of intestinal mucosa at the time of hour 3, 6, 12 after operation. RESULTS: (1) The pathological scores of pancreatitis were significantly higher in the SAP group than those in the treatment group and SO group (P < 0.05). (2) Compared with the SO group, the level of TNF-alpha in the SAP group and the treatment group was much higher (P < 0.05), but the level in the treatment group was lower than that in the SAP group (P < 0.05). (3) The serum concentration of DAO and endotoxin was significantly increased in the SAP group, and the concentration in treatment group was higher than that in the SO group (P < 0.01), but lower than that in the SAP group (P < 0.01). The occludin protein and mRNA expression in the SAP group was the lowest and the expression in the treatment group was higher than that in the SAP group (P < 0.01), but lower than that in the SO group (P < 0.01). CONCLUSIONS: Octahedral montone can improve the colonic barrier function, reduce the endotoxemia, and ameliorate the inflammation during acute pancreatitis.

2-Amino-4-tert-butyl-5-(4-chloro-benz-yl)thia-zole.

In the title compound, C(14)H(17)ClN(2)S, the dihedral angle between the planes of the thia-zole and chloro-phenyl rings is 88.86 (3)°. In the crystal, inversion dimers occur, linked by pairs of N-H⋯N hydrogen bonds.