2.Synthesis and antioxidative activity of flavone derivatives containing 1,2,4-triazole structure.
Zhi-fang DUAN ; Ling SHAO ; Sai-nan LI
Acta Pharmaceutica Sinica 2015;50(7):861-867
Using bioactive compounds 7-hydroxy flavone, salicylaldehyde, cinnamic acid and 4-amino-5- mercapto-1,2,4-triazoles as starting materials, three new types of flavone derivatives containing 1,2,4-triazole structure were synthesized via different step reactions. These new compounds were characterized by 1IHNMR, ESI-MS, IR and elemental analysis. Their scavenging effects on the superoxide radical (O2·-), hydroxyl radical (·OH), DPPH · radical and their total reduction activities were tested. The results showed that all of the compounds possessed some antioxidative activity at the concentration of 0.5 mg · mL(-1), but the scavenging ability of the target compounds was lower than that of the standard compound Vc.
Cinnamates
;
chemistry
;
Flavones
;
chemical synthesis
;
chemistry
;
Flavonoids
;
chemistry
;
Free Radical Scavengers
;
chemical synthesis
;
chemistry
;
Triazoles
;
chemistry
3.EFFECTS OF SOYBEAN PHOSPHOLIPIDS ON CONTENTS OF LIPIDS IN ERYTHROCYTE MEMBRANES OF MICE
Jufang GONG ; Linxiang SHAO ; Xiaohua ZHENG ; Feng SHI ; Renyan NAN
Acta Nutrimenta Sinica 1956;0(03):-
Objective: To study the effects of soybean phospholipids on fatty acids and phospholipids content in erythrocyte membranes of mice. Methods:The mice were fed with soybean phospholipids of 2 . 5, 5 . 0 , 10.0 g/kg bw respectively while control group with distilled water for 30 days. Then the mice were killed and contents of fatty acids and phospholipids in erythrocyte membranes were detected by HPLC. Results: (1)The contents of linoleic acid (C18 ∶2) and linolenic acid ( C18 ∶3), the composition of polyunsaturated fatty acid (PUFA) were increased obviously (P
4.Multi-level identification and analysis about infrared spectroscopy of lophatheri herba.
Ying SHAO ; Qi-Nan WU ; Wei GU ; Wei YUE ; Da-Wei WU ; Xiu-He FAN
China Journal of Chinese Materia Medica 2014;39(9):1644-1649
Based on the infrared spectra of Lophatheri Herba and Commelinae Herba, one-dimensional infrared spectra, second derivative spectra and two-dimensional correlated spectra were used to find out the differences between Lophatheri Herba and its imitations, respectively. The common peak ratio and variant peak ratio dual-indexes sequential were calculated and established according to infrared spectra of eleven batches of herbs. Infrared spectral data of Lophatheri Herba cluster analysis was applied to explore the similarity between each sample. The grouping results trend of sequential analysis of dual-indexes and cluster analysis was accordant. The results showed that the differences could be found by multi-level identification, and the source and the quality of the herbs could be effectively distinguished by the two analysis methods. Infrared spectroscopy, used in the present work exhibited some advantages on quick procedures, less sample required, and reliable results, which could provide a new method for the identification of traditional Chinese medicine with the imitations and adulterants, and the control of quality and origin.
Drugs, Chinese Herbal
;
analysis
;
chemistry
;
Plant Leaves
;
chemistry
;
Plants, Medicinal
;
chemistry
;
Reproducibility of Results
;
Spectrophotometry, Infrared
;
methods
;
Spectroscopy, Fourier Transform Infrared
;
methods
5.Metformin ameliorates β-cell dysfunction by regulating inflammation production, ion and hormone homeostasis of pancreas in diabetic KKAy mice.
Shuai-Nan LIU ; Quan LIU ; Su-Juan SUN ; Shao-Cong HOU ; Yue WANG ; Zhu-Fang SHEN
Acta Pharmaceutica Sinica 2014;49(11):1554-1562
This study is to evaluate the effects of the metformin (Met) on β cell function of diabetic KKAy mice. Female diabetic KKAy mice selected by insulin tolerance test (ITT) were divided randomly into two groups. Con group was orally administered by gavage with water, Met group with metformin hydrochloride at a dose of 0.2 g x kg(-1) for about 12 weeks. ITT and glucose tolerance tests (OGTT) were determined. Beta cell function was assessed by hyperglycemic clamp. Pancreatic biochemical indicators were tested. The changes of gene and protein expression in the pancreas and islets were also analyzed by Real-Time-PCR and immunostaining. Met significantly improved glucose intolerance and insulin resistance in KKAy mice. Fasting plasma glucose and insulin levels were also decreased. In addition, Met markedly increased glucose infusion rate (GIR) and elevated the Ist phase and maximum insulin secretion during clamp. It showed that Met decreased TG content and iNOS activities and increased Ca(2+) -Mg(2+)-ATPase activity in pancreas. Islets periphery was improved, and down-regulation of glucagon and up-regulated insulin protein expressions were found after Met treatment. Pancreatic mRNA expressions of inflammation factors including TLR4, NF-κB, JNK, IL-6 and TNF-α were down-regulated, p-NF-κB p65 protein levels also down-regulated by Met. And mRNA expressions of ion homeostasis involved in insulin secretion including SERCA2 and Kir6.2 were up-regulated by Met. Met increased SIRT5 expression level in pancreas of KKAy mice under the hyperglycemic clamp. These results indicated that chronic administration of Met regulated pancreatic inflammation generation, ion and hormone homeostasis and improved β cell function of diabetic KKAy mice.
Animals
;
Blood Glucose
;
Diabetes Mellitus, Experimental
;
drug therapy
;
Down-Regulation
;
Female
;
Glucose Tolerance Test
;
Homeostasis
;
Inflammation
;
drug therapy
;
Insulin
;
secretion
;
Insulin Resistance
;
Insulin-Secreting Cells
;
drug effects
;
Interleukin-6
;
metabolism
;
Metformin
;
pharmacology
;
Mice
;
NF-kappa B
;
metabolism
;
Pancreas
;
drug effects
;
Tumor Necrosis Factor-alpha
;
metabolism
6.Six cases of hypophosphataemic osteomalacia induced by adefovir dipivoxil
Nan ZHANG ; Mingwei SHAO ; Ai HUANG ; Xialian LI ; Guijun QIN ; Lijuan WANG
Chinese Journal of Endocrinology and Metabolism 2013;(5):414-416
[Summary] An analysis of clinical data was performed in 6 patients diagnosed as adefovir dipivoxil (ADV)-induced nephropathy in recent 14 months.The results showed that all of six patients suffered from pain over multiple joints after taking ADV 10-20 mg/d for 2-3 years,along with hypophosphatemia,hypouricemia,and raised osteogenesis index.One case had increased serum creatinine,5 cases had hypokalemia,renal glycosuria,and4 cases had albuminuria.Imageological examination showed osteoporosis,osteomalacia,and pseudo fracture.After discontinuance of ADV treatment,joint pain was obviously relieved within 3-6 weeks,blood uric acid level returned to normal within 1-2.5 months,and renal glycosuria and albuminuria disappeared by 1-2 months.The results suggest that after taking ADV for more than two years,attention should be paid to the nephropathy induced by ADV and regular monitoring of renal function,blood electrolyte,and urine should be mandatory.Hypouricemia is a reliable index of diagnosis and treatment in this event.
7.Reliability of mannitol for fluid responsiveness test in patients undergoing intracranial surgery
Xinxin SHAO ; Nan JIANG ; Lu YANG ; Xianjun HUANG ; Lijun NIU ; Liangcan XIAO
Chinese Journal of Anesthesiology 2015;35(4):457-459
Objective To evaluate the reliability of mannitol for fluid responsiveness test in the patients undergoing intracranial surgery.Methods Sixty-two ASA physical status Ⅰ or Ⅱ patients,aged 18-64 yr,with body mass index of 18-25 kg/m2,scheduled for elective intracranial surgery,were enrolled in the study.The patients were mechanically ventilated after induction of anesthesia.The radial artery and central vein were cannulated,and FloTracTM/VigileoTM system was connected for stroke volume variation monitoring.Before infusion of mannitol,effective circulating blood volume was confirmed according to stroke volume variation.20% mannitol 250 ml was infused over 20 min starting from onset of craniotomy.The fluid responsiveness test was recorded at the end of mannitol infusion.Results The sensitivity of fluid responsiveness test was 43%,and the specificity of fluid responsiveness test was 44%.Conclusion Mannitol can not be used for fluid responsiveness test in the patients undergoing intracranial surgery.
8.The value of serum galectin 3 detected by nanomagnetic beads sorting time resolved fluoroimmunoassay tandem analysis in the diagnosis of pancreatic cancer
Nan SHAO ; Xiaoyan LI ; Mingbing XIAO ; Feng JIANG ; Wenkai NI ; Cuihua LU ; Runzhou NI
Chinese Journal of Pancreatology 2013;13(5):303-306
Objective To study the value of serum galectin-3 detected by nanomagnetic beads sorting time resolved fluoroimmunoassay (TRFIA) tandem analysis in the diagnosis of pancreatic cancer.Methods The serum of 88 cases of pancreatic cancer,50 cases of acute pancreatitis,10 cases of pancreatic cysts,and 20 cases of healthy volunteers as control were collected.First,galectin-3 antibody coupled nanomagnetic-beads was used to sort the semm,then TRFIA was applied to detect the level of galectin 3,and the result was compared with that of routine TRFIA.ROC curve was constructed to determine the cutoff value and sensitivity for pancreatic cancer diagnosis.Results The method of nanomagnetic beads sorting TRFIA detected the level of galectin 3 between O.78 and 100 ng/ml in a linear manner,the intra-CV was ≤6.38%,and inter-CV was ≤7.22%,and average recovery rate was 105.3%.The serum level of galectin-3 in control group by nanomagnetic beads sorting TRFIA was 0.38 (0.02 ~ 3.06) ng/ml,which was significantly higher than that detected by routine TRFIA [0.18 (0.00 ~ 2.64) ng/ml,P =0.000).The serum levels of galectin-3 by nanomagnetic beads sorting TRFIA in pancreatic cancer,acute pancreatitis,pancreatic cysts and healthy volunteers were 4.85(0.00 ~42.67),0.69(0.00~ 13.62),0.70(0.00 ~ 14.54),0.38(0.02 ~ 3.06) ng/ml,and the level of galectin-3 in pancreatic cancer was significantly higher than that in acute pancreatitis,pancreatic cysts and healthy volunteers group (P <0.01),while the difference among the other three group was not significantly different.The AUC of galectin-3 for pancreatic cancer was 0.851 ± 0.040,95% CI:0.772 ~ 0.929.While using 1.07 ng/ml as the cut-off value,the positive rates for the diagnosis of pancreatic cancer,acute pancreatitis,pancreatic cysts and healthy volunteers were 84.1% (74/88),34.0% (17/50),20.0% (2/10),10.0% (2/20),and the sensitivity for diagnosis of pancreatic cancer was significantly higher than those in other 3 groups (P < 0.01).Conclusions Nanomagnetic beads sorting TRFIA tandem analysis method can enrich serum galectin-3,and increase the sensitivity of detection for pancreatic cancer and enhance the diagnostic value of galectin-3 for pancreatic cancer.
9.Inhibition of HepG2 cell growth by LHRH-MPG△NLS/CDK2-siRNA nanoparticles
Xinxiao QIAO ; Nan SHAO ; Xia DONG ; Lanxia LIU ; Dunwan ZHU ; Xigang LENG
International Journal of Biomedical Engineering 2014;37(2):85-88
Objective To detect the size distribution and Zeta potential of LHRH-MPG△NLS/CDK-siRNA nanoparticles,to observe the effect of different solvents on the nanoparticle size,and to investigate the inhibitory effect of nanoparticles on HepG2 cell growth.Methods LHRH-MPG △NLS and CDK2-siRNA were mixed by continuous stirring to form nanoparticles at different N/P ratios (10/1,20/1 and 40/1).The size distribution and Zeta potential of LHRH-MPG△NLS/CDK2-siRNA nanoparticles were detected by dynamic light scattering,and the stability of the nanoparticles in normal saline,10% glucose and pure water was discussed.Finally,the inhibitory effect of the nanoparticles on HepG2 cells was determined by CCK8 kit.Results The mean size of the nanoparticles was within 200 nm,and the Zeta potentials were (70±5) mV (N/P=10/1),(120±5) mV (N/P=20/1) and (130±5) mV (N/P=40/1),respectively.The size of the nanoparticles in normal saline was significantly increased,which demonstrated that strong electrolytes had a great impact on the nanoparticles size.When nanoparticle concentration was 200 nmol/L,LHRH-MPG△NLS/CDK2-siRNA nanoparticles (N/P=10/1) showed significantly inhibitory effect on HepG2 cell growth.Conclusions The mean size of the LHRH-MPG△NLS/CDK2-siRNA nanoparticles was within 200 nm,which was ideal for cellular uptake.The Zeta potential of nanoparticles revealed that nanoparticles could be stable in aqueous solution,while strong electrolytes would affect nanoparticle size.When nanoparticle concentration was 200 nmol/L,LHRH-MPG△NLS/CDK2-siRNA nanoparticles (N/P=10/1) showed significantly inhibitory effect on HepG2 cell growth.
10.MRI demonstrates abnormalities of motor nerves and extraocular muscles in congenital fibrosis syndrome due to mutations in KIF21 A
Yong-Hong, JIAO ; Shao-Qin, WU ; Feng-Yuan, MAN ; Hong-Yan, JIA ; Gang, LIU ; Nan, LIN
International Eye Science 2014;(8):1426-1429
AIM:To observe the structural basis of ocular motility abnormalities in patients with congenital fibrosis of the extraocular muscles type Ⅰ ( CFEOM Ⅰ) due to missense mutations in the developmental kinesin KIF21A using high - resolution magnetic resonance imaging ( MRI) .
METHODS: Totally 11 affected individuals reported KIF21A mutations were correlated with MRI studies demonstrating extraocular muscles ( EOMs ) size, location, contractility, and innervation. EOMs and the motor nerve in the orbits were imaged with T1 weighted in a triplanar scan using a dual-phased coils with 2. 0mm thick. Motor nerves were imaged at the brainstem using head coils and 3D-FIESTA with 0. 6-mm thick.
RESULTS: Patients with CFEOM Ⅰ exhibited different degrees of hypoplasia of oculomotor nerve, the abducens nerve and the trochlear nerve were also affected, of which 8 cases of orbital section could see the signal of abnormal nerve dominated by oculomotor nerve to lateral rectus. The both sides of six EOMS in all patients exhibited variable atrophy and abnormal bright internal signal on T1 imaging, particularly severe for the superior rectus and levator muscles.
CONCLUSION: High - resolution MRI can directly demonstrate pathology of motor nerves,affected EOMs, and ‘Pulley' hypoplasia caused by CFEOM Ⅰ due to mutations in KIF21A,and these findings suggest that the neuronal hypoplasia is the etiological factor of CFEOM.