Cefiderocol: a novel siderophore cephalosporin against multi-drug resistant Gram-negative bacilli infections / 生物工程学报

Antimicrobial resistance is one of the critical public health issues in the world. There is an urgent need to develop effective broad-spectrum antibiotics to treat the infection of multi-drug resistant Gram-negative bacilli. Cefiderocol, developed by the Shionogi Inc. in Japan, is a new type of iron carrier cephalosporin antibiotics, which overcomes the drug resistance of Gram-negative bacilli due to the down-regulation of outer membrane pore protein and the up-regulation of efflux pump, and has good stability to serine- and metallo-carbapenemases. This drug has a broad spectrum and strong antibacterial activity against carbapenem-resistant Enterobacteriaceae (CRE), Pseudomonas aeruginosa, Acinetobacter baumannii, and Stenotrophomonas maltophilia. Cefiderocol can be used to treat complex urinary tract infections (including pyelonephritis), hospital-acquired pneumonia, and ventilator-associated pneumonia. By summarizing the chemical structure, antibacterial mechanism, in vitro antibacterial activity, pharmacokinetics, pharmacodynamics, and clinical treatment of cefiderocol, this review shows the application potential of cefiderocol as a new iron carrier cephalosporin in the treatment of multi-drug resistant Gram-negative bacilli infections.

Rabdosia serra alleviates dextran sulfate sodium salt-induced colitis in mice through anti-inflammation,regulating Th17/Treg balance,maintaining intestinal barrier integrity,and modulating gut microbiota / 药物分析学报

Rabdosia serra(R.serra),an important component of Chinese herbal tea,has traditionally been used to treat hepatitis,jaundice,cholecystitis,and colitis.However,the chemical composition of R.serra and its effect against colitis remain unclear.In this study,the chemical composition of the water extract of R.serra was analyzed using ultra performance liquid chromatography coupled with a hybrid linear ion trap quadrupole-orbitrap mass spectrometer(UPLC-LTQ-Orbitrap-MS).A total of 46 compounds,comprising ent-kaurane diterpenoids,flavonoids,phenolic acids,and steroids,were identified in the water extract of R.serra,and the extract could significantly alleviate dextran sulfate sodium salt-induced colitis by improving colon length,upregulating anti-inflammatory factors,downregulating proinflammatory fac-tors,and restoring the balance of T helper 17/T regulatory cells.R.serra also preserved intestinal barrier function by increasing the level of tight junction proteins(zonula occludens 1 and occludin)in mouse colonic tissue.In addition,R.serra modulated the gut microbiota composition by increasing bacterial richness and diversity,increasing the abundance of beneficial bacteria(Muribaculaceae,Bacteroides,Lactobacillus,and Prevotellaceae_UCG-O01),and decreasing the abundance of pathogenic bacteria(Turi-cibacter,Eubacterium_fissicatena_group,and Eubacterium_xylanophilum_group).Gut microbiota depletion by antibiotics further confirmed that R.serra alleviated colitis in a microbiota-dependent manner.Overall,our findings provide chemical and biological evidence for the potential application of R.serra in the management of colitis.

Effects of health education intervention in elderly patients with osteoporosis / 中华老年医学杂志

Objective To examine changes in bone mineral density,serum bone turnover markers and serum cytokines after health education intervention in elderly patients with osteoporosis.Methods Two hundred and twenty elderly patients with osteoporosis were randomly divided into two groups.The control group(n=110)was given routine treatment,including anti-osteoporosis drugs and daily supplements of calcium and vitamin D.In addition to routine drug treatment,the observation group(n=110)also underwent health education intervention,which included instructions on lifestyle,diet,and exercise.After one year follow up,levels of bone mineral density(BMD),propeptide of type Ⅰ procollagen(PINP),β crosslaps (β-CTX),parathyroid hormone (PTH),25-dihydroxyvitamin D [25(OH) VD],interleukin-2 (IL-2),and insulin-like growth factor-1 receptor (IGF-1 R) were analyzed.Results After one year follow-up,all indicators,except the β-CTX level,were significantly improved in the observation group compared with those in the control group(all P＜0.05).Mean while,compared with pre-treatment levels,both groups had significantly increased levels of BMD(both P＜ 0.05),which were markedly higher in the observation group (P ＜ 0.05).Furthermore,improvement was achieved in cognitive ability and lifestyle in the observation group (both P ＜ 0.05).Conclusions Health education intervention can effectively improve BMD in elderly patients with osteoporosis,significantly improve lifestyle,and play an important role in integrated management of osteoporosis.

Optimization of enzymatic preparation of glucose 1-phosphate by response surface methodology / 生物工程学报

With glucose as substrate, sodium tripolyphosphate as the phosphorus acylating agent, and phosphorylase of Solanum tuberosum as the catalyst, glucose 1-phosphate was synthesized. Based on a three-level, three-variable Box-Behnken experimental design, response surface methodology was used to evaluate the effects of temperature, molar ratio of glucose to sodium tripolyphosphate and time on the production. The structure of the product was confirmed by 1H NMR spectra. The results show that the optimum conditions were as follows: temperature 35 degrees C, molar ratio of glucose to sodium tripolyphosphate 1.35:1 and time 19 h.

Effects of total alkaloid of Sophora alopecuroides on serum IL-1beta and IL-4 expression in mice with acute ulcerative colitis / 中国中药杂志

<p><b>OBJECTIVE</b>To investigate the effects of total alkaloid of Sophora alopecuroides (TASA) on expression of serum IL-1beta and IL-4 in mice with DSS-induced acute ulcerative colitis.</p><p><b>METHOD</b>C57BL/C mice were randomly divided into six groups: normal group, model group, SASP group, low, middle and high dosage TASA group. Acute ulcerative colitis was induced by administrating 5% dextran sulfate sodium (DSS) solution as drinking water freely for 8 days. Mice were given drug by stomach at the same time and sacrificed after 8 days. The general morphological and histopathological changes were observed during the experiments. Daily disease activity index (DAI) was assessed. The serum levels of IL-1beta and IL-4 were detected by ELISA.</p><p><b>RESULT</b>In UC mice, the expression of serum IL-1beta was significantly increased whereas IL-4 was decreased when compared with the normal group (P < 0.01). In all treatment groups, TASA could reduce the expression of IL-1beta (P < 0. 01) , increase the level of IL-4 and alleviate the symptom of UC and decrease the DAI.</p><p><b>CONCLUSION</b>TASA can effectively attenuate DSS-induced acute ulcerative colitis through the decreasing the over-expression of pro-inflammatory cytokine levels.</p>

The effect of electro-acupuncture on sodium channel Na (v) 1.1 in rats after acute cerebral ischemia / 中华物理医学与康复杂志

Objective To observe the effect of electro-acupuncture therapy (ET) on the expression of sodium channel Na(v) 1.1 in rats after acute cerebral ischemia and the mechanism of any protective function of ET.Methods A model of focal acute cerebral ischemia was established by occluding the right middle cerebral artery.One hundred and eighty healthy SD rats were randomly divided into a sham operation control (SC) group, an ischemia control (IC) group, a real ET group and a false ET group, with 45 in each group. Immunohistochemistry and real-time polymerase chain reaction (PGR) methods were used to detect Na(v)1. 1 expression. 2,3,5-triphenyl tetrazolium chloride (TTC) staining was used to detect infarct volume. Neurological examination and grading was carried out at 6 hours and then 1, 2, 3 and 7 days after inducing ischemia. Results The gradings and infarction volume ratios of the rats in the IC group were the most serious, while in the real ET group the severity was much less at each time point. Compared with the SC group, the expression of Na(v) 1.1 was significantly up-regulated in the IC group. The expression of Na(v) 1.1 was increased at the 6th hour, then down-regulated to the lowest level at day 1,then from the 2nd to the 7th day was up-regulated again. The expression of Na(v) 1.1 in the real ET group was significantly lower than in the IC group. Although the expression of Na(v)1.1 in the false ET group was low compared with the IC group, the difference was not significant. The difference between the real ET group and the false ET group was significant, however. Conclusions ET can reduce damage from cerebral ischemia and benefit the recovery of neural function. ET can also could regulate the expression of Na(v)1.1 after acute cerebral ischemia, which may be an important mechanism for neural function recovery.

Studies on antibacterial constituents of Discocleidion rufescens (2) / 中国中药杂志

<p><b>OBJECTIVE</b>To screen effective constituents of Discocleidion rufescens against bacteria.</p><p><b>METHOD</b>Compounds were isolated by bioassay-guided fractionation method with various chromatographic methods and their structures were determined by spectral analysis and chemical evidence.</p><p><b>RESULT</b>Seven compounds were isolated from the Et2O and n-BuOH extracts and identified as 5,7-dihydroxy-4'-methoxy flavone (1), quercetin (2), apigenin-7-O-beta-D-glucopyranoside (3), apigenin-7-O-neohesperidoside (4), luteolin-7-O-neohesperidoside (5), gallic acid (6) and beta-daucosteol (7).</p><p><b>CONCLUSION</b>Compounds 1-6 were isolated from genus Discocleidion for the first time and exhibited certain inhibitory activity against Escherichia coli. Compound 6 also showed antibacterial activity against Staphylococus aureus.</p>