Aim To investigate the effect of microinjection of EX527, a selective SIRT1 antagonist, into the ventrolateral orbital cortex (VLO) on morphine-induced conditioned place preference (CPP), and to explore the role of CREB/BDNF in it. Methods The cannulas were implanted bilaterally in the VLO of rats by brain stereotaxis surgery, and the model of morphine-induced CPP was established. The behavioral experiment consisted of four stages:habituation (d 1), pre-test (d 2-4), conditioning training (d 5-14) and test (d 15). At the stage of conditioning training, EX527 (1 μL, 5 g·L

Pectin methylesterase (PME) is an important pectinase that hydrolyzes methyl esters in pectin to release methanol and reduce the degree of methylation of pectin. At present, it has broad application prospects in food processing, tea beverage, paper making and other production processes. With the in-depth study of PME, the crystal structures with different sources have been reported. Analysis of these resolved crystal structures reveals that PME belongs to the right-hand parallel β-helix structure, and its catalytic residues are two aspartic acids and a glutamine, which play the role of general acid-base, nucleophile and stable intermediate, in the catalytic process. At the same time, the substrate specificity is analyzed to understand the recognition mechanism of the substrate and active sites. This paper systematically reviews these related aspects.
Carboxylic Ester Hydrolases ; chemistry ; metabolism ; Catalytic Domain ; Crystallography ; Pectins ; metabolism ; Protein Structure, Tertiary ; Substrate Specificity

Usnic acid and its derivatives, a group of organic molecules with great importance, are characteristic to lichens, possessing pharmacological activities such as anti-virus, anti-bacteria, anti-humor, anti-inflammatory, analgesic, and anaesthetic effects. Many of them have been widely used as medicine, but also bring side effects such as dermatitis and liver damages. In the past decades, great efforts by isolation, organic synthesis, and structure modification methods were put on discovery of UA derivatives with higher biological activities or less side effects. This paper describes herein the most progress on natural sources, isolation and structure elucidation, structural characteristics, synthesis and modification results, pharmacological activities and toxicities of UA and its derivatives, hopefully to provide valuable reference for further research.
Benzofurans ; chemistry ; pharmacology ; Biological Products ; Lichens ; chemistry

The present study was aimed to investigate the role of necroptosis in the pathogenesis of acute respiratory distress syndrome (ARDS). The rat model of ARDS was induced by intravenous injection of oleic acid (OA), and observed for 4 h. The lung injury was evaluated by arterial blood gas, lung wet-dry weight ratio (W/D) and histological analyses. Simultaneously, bronchoalveolar lavage fluid (BALF) was collected for total and differential cell analysis and total protein determination. Tumor necrosis factor alpha (TNF-α) level in BALF was determined with a rat TNF-α ELISA kit. Expressions of receptor interacting protein kinase 1 (RIPK1), RIPK3 and mixed lineage kinase domain-like protein (MLKL) in lung tissue were determined by Western blot and immunohistochemical staining. The interaction between RIPK1 and RIPK3 was explored by immunoprecipitation. The results showed that, compared with those in control group, total white blood cells count (WBC), polymorphonuclear percentage (PMN%), total protein concentration, TNF-α level in BALF, W/D, and the alveolar-arterial oxygen tension difference (P(A-a)O) in OA group were significantly increased at 4 h after OA injection. Western blot and immunostaining further showed remarkably increased expressions of RIPK1, RIPK3 and MLKL in lung tissue from OA group. Additionally, immunoprecipitation results indicated an enforced interaction between RIPK1 and RIPK3 in OA group. Collectively, the TNF-α level in BALF and the RIPK1-RIPK3-MLKL signaling pathway in lung tissue were found to be upregulated and activated with the process of ARDS. These findings implicate that RIPK1/RIPK3-mediated necroptosis plays a possible role in the pathogenesis of ARDS, which may provide a new idea to develop novel drugs for the therapy of ARDS.
Acute Disease ; Animals ; Bronchoalveolar Lavage Fluid ; Disease Models, Animal ; Lung Diseases ; Necrosis ; Oleic Acid ; Rats ; Receptor-Interacting Protein Serine-Threonine Kinases ; Respiration Disorders ; Signal Transduction ; Tumor Necrosis Factor-alpha

The changes of serum cyclophilin A (CyPA), its receptor CD147 and the downstream signaling pathway during the process of cardiac hypertrophy remain unknown. The present study aims to investigate the relationships between CyPA-CD147-ERK1/2-cyclin D2 signaling pathway and the development of cardiac hypertrophy. Left ventricular hypertrophy was prepared by 2-kidney, 2-clip in Sprague-Dawley rats and observed for 1 week, 4 and 8 weeks. Left ventricular hypertrophy was evaluated by ratio of left ventricular heart weight to body weight (LVW/BW) and cardiomyocyte cross sectional area (CSA). CyPA levels in serum were determined with a rat CyPA ELISA kit. Expressions of CyPA, CD147, phospho-ERK1/2 and cyclin D2 in left ventricular myocytes were determined by Western blot and immunostaining. Compared with sham groups, systolic blood pressure reached hypertensive levels at 4 weeks in 2K2C groups. LVW/BW and CSA in 2K2C groups were significantly increased at 4 and 8 weeks after clipping. ELISA results indicated a prominent increase in serum CyPA level associated with the degree of left ventricular hypertrophy. Western blot revealed that the expressions of CyPA, CD147, phospho-ERK1/2 and cyclin D2 in left ventricular tissues were also remarkably increased as the cardiac hypertrophy developed. The results of the present study demonstrates that serum CyPA and CyPA-CD147-ERK1/2-cyclin D2 signaling pathway in ventricular tissues are time-dependently upregulated and activated with the process of left ventricular hypertrophy. These data suggest that CyPA-CD147 signaling cascade might play a role in the pathogenesis of left ventricular hypertrophy, and CyPA might be a prognosticator of the degree of left ventricular hypertrophy.
Animals ; Basigin ; metabolism ; Blood Pressure ; Cyclin D2 ; Cyclophilin A ; metabolism ; Hypertension ; Hypertrophy, Left Ventricular ; metabolism ; Mitogen-Activated Protein Kinase 1 ; metabolism ; Mitogen-Activated Protein Kinase 3 ; metabolism ; Myocytes, Cardiac ; Rats ; Rats, Sprague-Dawley ; Signal Transduction ; Up-Regulation

BACKGROUNDIntraperitoneal lymphangioma (IL) used to be thought of as a benign lymphatic malformation with a low rate of preoperative diagnosis. This retrospective study aimed to explore the connection between the cysts and clinical manifestation and imaging characteristics, and to study diagnostic confusion, therapeutic principles and potential recurrent reasons, to further enhance the comprehension of this rare disease.

METHODSHere, we retrospectively reviewed 21 patients diagnosed with IL. Age, sex, complaints, physical findings, and imaging features of each patient were documented. The therapies, postoperative complications and treatments were discussed.

RESULTSSymptomatology included eight patients (38%) with intermittent dull pain in the abdomen, and three patients (14%) complained of abdominal persistent pain. The physical examination revealed an abdominal mass in 16 patients (76%), and eight (38%) were reported no discomfort. IL was correctly established preoperatively in 19 patients (90%). Patients were treated using laparotomy, except one who was treated with laparoscopy. Two recurrences were noted during follow-up.

CONCLUSIONSIL should be suspected in any patient with a mobile abdominal mass and surgery is required immediately after discovery of the tumor.

Abdomen ; pathology ; Adolescent ; Adult ; Aged ; Aged, 80 and over ; Child ; Child, Preschool ; Diagnosis, Differential ; Female ; Humans ; Laparoscopy ; Lymphangioma ; diagnosis ; surgery ; Male ; Middle Aged ; Postoperative Complications ; Retrospective Studies ; Young Adult

OBJECTIVETo objectively evaluate the efficacy and safety of Yimusake Tablet in the treatment of premature ejaculation (PE) through a multi-centered large-sample trial.

METHODSWe conducted a multi-centered, open, fixed-dose, and self-compared clinical trial among 300 patients with diagnosed PE. The trial lasted 12 weeks, including 4 weeks without any medication and 8 weeks of treatment with Yimusake Tablet, 2 pills (1 g) per night. We observed the intravaginal ejaculation latency time (IELT) before and after treatment, evaluated the safety of medication, and performed a questionnaire investigation on the patients' satisfaction.

RESULTSOf the 300 PE patients, 288 accomplished the clinical trial. The patients ranged in age from 22 to 60 years, averaging at 31.6 years. The mean IELT of the patient was 62.5 seconds at baseline, 168.9 seconds after 4 weeks of treatment with Yimusake Tablet, and 222.2 seconds after 8 weeks of medication. Among the 157 patients with normal erectile function (IIEF >21), the mean IELT was 71.4 seconds before treatment, 147.4 seconds after 4 weeks of medication, and 172.5 seconds after 8 weeks of medication. The patients' satisfaction was significantly increased after treatment. Those complicated by mild to moderate erectile dysfunction achieved different degrees of improvement in the IIEF-5 score, with a mean increase of 3.8. Only a few patients experienced mild adverse events, including constipation, dry mouth, nose bleeding, abdominal pain, and lumbosacral pain, which were all relieved without drug withdrawal.

CONCLUSIONYimusake Tablet is a safe and effective medicine for the treatment of PE.

Adult ; Drugs, Chinese Herbal ; therapeutic use ; Ejaculation ; drug effects ; physiology ; Erectile Dysfunction ; drug therapy ; Humans ; Male ; Middle Aged ; Patient Satisfaction ; Penile Erection ; Phytotherapy ; Premature Ejaculation ; drug therapy ; Surveys and Questionnaires ; Tablets ; Time Factors

Diabetes Mellitus ; etiology ; Hepatitis, Viral, Human ; complications ; Humans ; Insulin Resistance

BACKGROUNDDiabetes mellitus (DM) is a common disease accompanied with a high incidence of hind limb ischemia (HLI). In recent years, numerous studies demonstrated that endothelial progenitor cells (EPCs) are involved in angiogenesis and maintenance of vascular integrity following HLI. On the other side, it has been proved that Astragalus polysaccharide (APS) could promote angiogenesis. In the present study, we aimed to evaluate the effect of APS and EPCs on enhancing angiogenesis after experimental HLI caused by femoral artery ligation in rats with streptozotocin (STZ)-induced diabetes.

METHODSRats (n = 110) were randomly assigned to the following groups: sham group, ischemia group, APS group, EPCs group and APS+EPCs group. APS, EPCs or an equal volume of vehicle was administered intramuscularly after HLI induction, and 6 rats were assessed by angiography at 28 days after induction of HLI, 6 rats were sacrificed at the same time point to take histological studies, biochemical tests were also performed at that point in the rest rats.

RESULTSAPS or EPCs treatment induced an increase, respectively, in the protein expression of vascular endothelial growth factor (VEGF) (36.61%, 61.59%), VEGF receptor-1 (VEGFR-1) (35.50%, 57.33%), VEGFR-2 (31.75%, 41.89%), Angiopoietin-1 (Ang-1) (37.57%, 64.66%) and Tie-2 (42.55%, 76.94%) (P < 0.05), after HLI injury. And combined therapy of APS and EPCs enhanced the effort of angiogenesis after HLI induction in diabetic rats, through elevating protein expression of VEGF (99.67%), VEGFR-1 (105.33%), VEGFR2 (72.05%), Ang-1 (114.30%) and Tie-2 (111.87%) (P < 0.05). Similarly, mRNA expression of VEGF, VEGFR-1, VEGFR2, Ang-1, Tie-2 also show similar trends as well as protein expression (P < 0.05).

CONCLUSIONAPS or EPCs could enhance angiogenesis, and the combined treatment leads to better effort, at least, partially via VEGF/VEGFR and Ang-1/Tie-2 signaling pathway.

Animals ; Astragalus Plant ; chemistry ; Diabetes Mellitus, Experimental ; drug therapy ; therapy ; Endothelial Progenitor Cells ; physiology ; Hindlimb ; pathology ; Ischemia ; drug therapy ; therapy ; Male ; Polysaccharides ; therapeutic use ; Rats

OBJECTIVETo observe the efficacy of the combination of Qilin Pills and levofloxacin in the treatment of asthenospermia accompanied with accessory sex gland infection.

METHODSWe randomly assigned 80 asthenospermia patients with accessory sex gland infection to groups 1 and 2 of equal number, the former treated with Qilin Pills + levofloxacin, and the latter with levofloxacin only. Qilin Pills were administered at the dose of 6 g tid for 30 days, and levofloxacin at the dose of 0.5 g qd for 20 days. We obtained semen parameters, including the percentage of progressively motile sperm and peroxidase-positive white blood cell (WBC) count, before and after medication, and compared the clinical effects between the two groups.

RESULTSAll the patients accomplished the clinical trial. The therapeutic effectiveness rates in improving progressive sperm motility were 60% in group 1 and 17.5% in group 2, with statistically significant differences between the two groups (P < 0.05). As for the peroxidase-positive WBC count in semen, the effectiveness rates were 87.5% and 82.5%, respectively, with no significant differences between the two groups (P > 0.05).

CONCLUSIONFor the treatment of asthenospermia accompanied with accessory sex gland infection, Qilin Pills combined with levofloxacin is evidently better than levofloxacin alone in improving sperm motility, and it has no obvious adverse effects.

Adult ; Asthenozoospermia ; complications ; drug therapy ; Drugs, Chinese Herbal ; therapeutic use ; Humans ; Infertility, Male ; drug therapy ; Levofloxacin ; therapeutic use ; Male ; Phytotherapy ; Reproductive Tract Infections ; drug therapy ; Treatment Outcome ; Young Adult