ABSTRACT
@#New Delhi metallo-β-lactamase-1 (NDM-1) is capable of hydrolyzing nearly all β-lactam antibiotics, posing an emerging threat to public health. There are currently less effective treatment options for treating NDM-1 positive “superbug”, and no promising NDM-1 inhibitors were used in clinical practice. In this study, structure–activity relationship based on thiosemicarbazone derivatives was systematically characterized and their potential activities combined with meropenem (MEM) were evaluated. Compounds 19bg and 19bh exhibited excellent activity against 10 NDM-positive isolate clinical isolates in reversing MEM resistance. Further studies demonstrated compounds 19bg and 19bh were uncompetitive NDM-1 inhibitors with Ki = 0.63 and 0.44 μmol/L, respectively. Molecular docking speculated that compounds 19bg and 19bh were most likely to bind in the allosteric pocket which would affect the catalytic effect of NDM-1 on the substrate meropenem. Toxicity evaluation experiment showed that no hemolysis activities even at concentrations of 1000 mg/mL against red blood cells. In vivo experimental results showed combination of MEM and compound 19bh was markedly effective in treating infections caused by NDM-1 positive strain and prolonging the survival time of sepsis mice. Our finding showed that compound 19bh might be a promising lead in developing new inhibitor to treat NDM-1 producing superbug.
ABSTRACT
Alpha-ketoglutarate (AKG) is a key molecule in the Krebs cycle determining the overall rate of the citric acid cycle of the organism. It is a nitrogen scavenger and a source of glutamate and glutamine that stimulates protein synthesis and inhibits protein degradation in muscles. AKG as a precursor of glutamate and glutamine is a central metabolic fuel for cells of the gastrointestinal tract as well. AKG can decrease protein catabolism and increase protein synthesis to enhance bone tissue formation in the skeletal muscles and can be used in clinical applications. In addition to these health benefits, a recent study has shown that AKG can extend the lifespan of adult Caenorhabditis elegans by inhibiting ATP synthase and TOR. AKG not only extends lifespan, but also delays age-related disease. In this review, we will summarize the advances in AKG research field, in the content of its physiological functions and applications.
Subject(s)
Adult , Humans , Adenosine Triphosphate , Bone and Bones , Caenorhabditis elegans , Citric Acid Cycle , Gastrointestinal Tract , Glutamic Acid , Glutamine , Insurance Benefits , Metabolism , Muscle, Skeletal , Muscles , Nitrogen , ProteolysisABSTRACT
Objective To observe the effects of Shuangliao Houfeng Powder on complications of dental extraction .Methods 280 patients who need dental extraction were recruited into a treatment group and a control group. The treatment group was applied with Shuangliao Houfeng Powder externally on alveolus dentalis after dental extraction, while the control group received no post-treatment after dental extraction. Wound healing and incidence of complications were observed after three days. Results Wound healing in stage 1 showed better results in the treatment group than the control group (P<0.05). Postoperative bleeding time of the treatment group was significantly shorter than the control group (P<0.01) . Besides the treatment group got better improvements in such symptoms as gingival swelling, pain, and difficulty in mouth opening than the control group (P< 0.05). Conclusion Shuangliao Houfeng Powder is effective on complications of dental extraction and worthy of promotion in clinic.
ABSTRACT
Objective To study the effect of Jiaweiyunvjian on periodontitis in the old.Methods A total of 180 periodontitis patients were randomly recruited into a treatment group and a control group,90 patients in each.The control group was treated with calculus removal and oral metronidazole,while the treatment group was treated with Jiaweiyunvjian on the basis ofthe control group.After both groups were treated for 7 days,therapeutic effects were observed.Results The total effective rate was 90.4%and 73.3%in the treatment group in the control group respectively.There was significant diffefence (P<0.01).In the 6-month follow-up,there were 7 cases(7.4%)relapsed in the treatment group and 16 cases(18.6%)relapsed in the control group,also showing significant difference(P<0.05).Conclusion Jiaweiyunvjian has curative effects on periodontitis of the old people.
ABSTRACT
OBJECTIVE To observe the incidence of facial nerve injury and its relationship to the types of operation. METHODS The clinical data of 116 patients who underwent parotid surgery from 1999 to 2006 were analyzed retrospectively. RESULTS The facial injury rate in total parotidectomy(66.7 %) was significantly higher than that in superfacial parotidectomy(39.2 %) and partial parotidectomy(12.5 %). The facial nerve injury rate in the mandibular branch(31.9 %) was higher than that in the buccal branch(9.2 %) and the zygomaticofacial branch(2.9 %). CONCLUSION The injury of facial nerve branches was correlated with the surgical managements. A proper surgical managements and operative extent would reduce the incidence of facial nerve injury and decrease the complications of the operation.