To study the binding capacity of active ingredients of Daidai lipid-lowering flavonoid extract and plasma protein,investigate the ways to improve the traditional formula for calculating protein binding rates based on ultrafiltration,and increase the stability and reliability of the experimental results. UPLC-MS/MS was used to establish a quantitative analysis method for simultaneous determination of active ingredients( neohesperidin and narngin) in ultrafiltrate. The protein binding rates were calculated by the traditional ultrafiltration formula. The correction factors( F) were introduced later,and the binding rates calculated with the correction factors were compared with those without the correction factors. The binding capacity of the extract and plasma protein was evaluated. The quantitative analysis method established by UPLC-MS/MS had a good specificity. The standard curve and linear range,method accuracy,precision and lower limit of quantitation all met the requirements. The method met the requirement for quantitative detection of the active ingredients in ultrafiltrate after the rat plasma was filtrated in the ultrafiltration tube. Under the experimental conditions,the binding rates of both active ingredients( neohesperidin and narngin) were higher than 90%. The active ingredients and rat plasma protein were bound in a concentration-dependent manner,with statistically significant differences( P<0. 01). There was no statistically significant difference between the protein binding abilities of the two active ingredients with rat plasma protein. Therefore,the active ingredients of Daidai lipid-lowering flavonoid extract had a relatively strong binding strength with rat plasma protein,and they were bound in a concentration-dependent manner. Additionally,when calculating protein binding rates by the traditional ultrafiltration formula,the correction factors could be introduced to effectively reflect the errors of multiple ingredient groups in traditional Chinese medicine extracts.This correction method could provide a reference thinking and practical reference for the improvement of the determination method of the traditional Chinese medicine plasma protein binding ability based on ultrafiltration.
Animals ; Blood Proteins ; Chromatography, High Pressure Liquid ; Drugs, Chinese Herbal ; pharmacology ; Flavonoids ; pharmacology ; Hypolipidemic Agents ; pharmacology ; Lipids ; Rats ; Reproducibility of Results ; Tandem Mass Spectrometry

Objective To compare the scalp nerve block versus local infiltration of incision for in-tracranial aneurysm clipping under general anesthesia. Methods Fifty-seven American Society of Anesthe-siologists physical statusⅠorⅡpatients of both sexes, aged 18-64 yr, scheduled for elective intracranial aneurysm clipping under general anesthesia, were divided into 3 groups ( n=19 each) using a random num-ber table method:control group ( group C) , scalp nerve block group ( group S) and local infiltration of in-cision group ( group I) . Anesthesia was induced by intravenously injecting propofol, sufentanil and cisatra-curium. Bilateral supraorbital nerve (2 ml), supratrochlear nerve (2 ml), zygomaticotemporal nerve (2 ml), auriculotemporal nerve (2 ml), greater occipital nerve (3 ml), lesser occipital nerve (3 ml) and the third occipital nerve ( 1 ml) blocks were performed with 0. 75％ ropivacaine after tracheal intubation in group B. Local infiltration of incision was carried out with 0. 75％ ropivacaine 15 ml in group I. Anesthesia was maintained by intravenously infusing propofol and remifentanil to maintain bispectral index value at 40-60. The fluctuation range of mean arterial pressure and heart rate was not more than 20％ of the baseline, and vasoactive agents were administered when necessary. Oxycodone 0. 1 mg∕kg was intravenously injected at 30 min before the end of surgery to perform preemptive analgesia. When visual analogue scale score>3 with-in 48 h after surgery, oxycodone 2 mg was intravenously injected as rescue analgesic, and administration was repeated when necessary ( at an interval>15 min) . The intraoperative consumption of propofol, remifen-tanil and vasoactive agents was recorded. Arterial blood samples were collected before anesthesia induction and at 3, 12, 24, 48 and 72 h after surgery for determination of serum interleukin-6 ( IL-6) , IL-10 and C-reactive protein ( CRP ) concentrations by enzyme-linked immunosorbent assay. The time of the first postoperative requirement for oxycodone and consumption of oxycodone within 48 h after surgery were recor-ded. The development of adverse reactions such as postoperative fever, nausea and vomiting, dizziness, respiratory depression, pruritus, local anesthetic intoxication, subcutaneous hematoma, and scalp infec-tion was also recorded. Results Compared with group C, the intraoperative consumption of remifentanil and requirement for nicardipine were significantly decreased, the concentration of serum IL-6 was decreased at 3 h after surgery, the concentration of serum CRP was decreased at 12 h after surgery, the concentration of serum IL-10 was increased at 12 and 24 h after surgery, the time of the first postoperative requirement for rescue analgesia was prolonged, the consumption of oxycodone was reduced, and the incidence of nausea and vomiting was decreased in group B, and the intraoperative consumption of remifentanil was significantly reduced in group I (P<0. 05). Compared with group I, the intraoperative consumption of remifentanil was significantly reduced, the requirement for nicardipine was decreased, the concentration of serum IL-6 was decreased at 3 h after surger-y, the concentration of serum CRP was decreased at 12 h after surgery, the concentration of serum IL-10 was in-creased at 12 and 24 h after surgery, the time of the first postoperative requirement for rescue analgesia was pro-longed, the consumption of oxycodone was reduced, and the incidence of nausea and vomiting was decreased in group B (P<0. 05). Conclusion Compared with local infiltration of incision, scalp nerve block is helpful in carrying out anesthetic model of low-consumption opioids and in maintaining intraoperative hemodynamics stable and is more helpful in inhibiting perioperative inflammatory and pain responses when used for the patients under-going intracranial aneurysm clipping under general anesthesia.

Objective To understand the treatment circumstance of ST-elevation myocardial Infarction (STEMI) patients at public hospitals in Shenzhen.Methods Directed by Public Hospital Administration at Shenzhen Municipality (PHASM) and led by Chest Pain Treatment Quality Control Center at Shenzhen People's Hospital (CPTQCC-SZ),25 public hospitals in Shenzhen, including 15 PCI-capable hospitals and 10 non-PCI-capable hospitals,we investigated on the overall treatment conditions and the STEMI patient treatment situations from October to December 2015 in these hospitals. A regression analysis was performed between a few factors and the success rate of STEMI treatment was reviewed. Results 383 STEMI cases twere registered between October to December 2015 in the 25 public hospitals in Shenzhen,with 324 case treated in PCI-capable hospitals and 59 cases in non-PCI-capable hospitals. There were statistical differences between the PCI-capable hospitals and non-PCI-capable hospital in fields of total number of senior cardiologists (work year ≥ 3 year),total number of beds in general cardiology beds and number of beds in cccu(all P<0.01). There was no difference in the time of obtaining the first ECG at patient arrival between hospitals(P=0.052).Time for laboratory results availability for troporin was significantly shorter in PCI-capable hospital[(25.0±4.2)min vs.(58.0±2.8)min,P=0.002] .Among the PCI-capable hospitals,the mean D-to-B time was 320 minutes, and mean F-to-B time was 380 minutes. In non-PCI-capable hospitals,D-to-N time ranged from 20 to 350 minutes and F-to-N time ranged from 25 to 380 minutes. Conclusions There are gaps among the overall conditions of the public hospitals in Shenzhen. The overall conditions and chest pain treatment conditions of non-PCI-capable hospitals had bigger gaps with PCI-capable hospitals.

Objective: To evaluate the effects of Testosterone Undecanoate Pills (TUP) on insulin resistance (IR) in type-2 diabetes men with hypogonadism. METHODS: We randomly divided 82 type-2 diabetes patients with hypogonadism into a treatment (n = 42) and a control group (n = 40), both maintaining their glucose- and lipid-reducing therapies, while the former treated orally with TUP in addition. After 6 months of medication, we compared the body mass index (BMI), waist circumference (WC), blood glucose level, HbA1c, lipid profile, IR index obtained by homeostatic model assessment (HOMA-IR), insulin sensitivity index (ISI), sex hormone levels, and sexual function scores between the two groups of patients. RESULTS: Compared with the baseline, the patients in the treatment group showed significant decreases after medication in BMI (［26.71 ± 2.39］ vs ［25.15 ± 2.28］ kg/m2, P <0.05), WC (［89.96 ± 9.13］ vs ［85.03 ± 9.58］ cm, P <0.05), HbA1C (［7.73 ± 1.31］ vs ［7.01 ± 1.25］ %, P <0.05), and triglyeride (［1.97 ± 0.83］ vs ［1.41 ± 0.69］ mmol/L, P <0.05), a markedly elevated level of total testosterone (［7.16 ± 2.21］ vs ［14.22 ± 2.63］ nmol/L, P <0.05), and remarkable improvement in HOMA-IR (3.76 ± 1.18 vs 2.55 ± 1.03, P <0.05), ISI (96 ± 51 vs 138 ± 53, P <0.05) and total scores of the Aging Males' Symptoms (P <0.05). But no significant changes were observed in the scores of the International Index of Erectile Function (IIEF) after treatment (13.28 ± 6.38 vs 14.95 ± 6.08, P >0.05). CONCLUSIONS TUP can significantly improve insulin resistance in type-2 diabetes men with hypogonadism.
Androgens ; administration & dosage ; therapeutic use ; Blood Glucose ; analysis ; Body Mass Index ; Diabetes Mellitus, Type 2 ; blood ; complications ; drug therapy ; Glycated Hemoglobin A ; analysis ; Humans ; Hypogonadism ; blood ; drug therapy ; Insulin Resistance ; Lipids ; blood ; Male ; Testosterone ; administration & dosage ; analogs & derivatives ; therapeutic use ; Waist Circumference