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
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chemistry
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Flavones
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chemical synthesis
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chemistry
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Flavonoids
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chemistry
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Free Radical Scavengers
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chemical synthesis
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chemistry
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Triazoles
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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.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
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Blood Glucose
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Diabetes Mellitus, Experimental
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drug therapy
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Down-Regulation
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Female
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Glucose Tolerance Test
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Homeostasis
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Inflammation
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drug therapy
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Insulin
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secretion
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Insulin Resistance
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Insulin-Secreting Cells
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drug effects
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Interleukin-6
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metabolism
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Metformin
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pharmacology
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Mice
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NF-kappa B
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metabolism
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Pancreas
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drug effects
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Tumor Necrosis Factor-alpha
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metabolism
5.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
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analysis
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chemistry
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Plant Leaves
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chemistry
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Plants, Medicinal
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chemistry
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Reproducibility of Results
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Spectrophotometry, Infrared
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methods
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Spectroscopy, Fourier Transform Infrared
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methods
6.Effect of Mudan Granule on islets beta cell function in monosodium glutamate induced obese mice with insulin resistance: an experimental study.
Shuai-Nan LIU ; Su-Juan SUN ; Quan LIU ; Shao-Cong HOU ; Zhu-Fang SHEN
Chinese Journal of Integrated Traditional and Western Medicine 2014;34(7):853-858
OBJECTIVETo study the effect of Mudan Granule (MD) on the glucose metabolism and beta cell function in monosodium glutamate (MSG) induced obese mice with insulin resistance (IR).
METHODSMSG obese mice were induced by subcutaneous injecting MSG (4 g/kg for 7 successive days in neonatal ICR mice). Forty MSG mice with IR features were recruited and divided into four groups according to body weight, fasting blood glucose, triglyceride (TG), total cholesterol (TC), and the percentage of blood glucose decreased within 40 min in the IR test, i.e., the model group (Con), the low dose MD group, the high dose MD group, and the Metformin group (Met). Besides, another 10 ICR mice were recruited as the normal control group (Nor). The water solvent of 2.5 g/kg MD or 5 g/kg MD was respectively administered to mice in the low dose MD group and the high dose MD group. Metformin hydrochloride was given to mice in the Met group at 0.2 g/kg body weight. Equal dose solvent distilled water was administered to mice in the Nor group and the Con group by gastrogavage, once per day. All medication was lasted for 15 weeks. Insulin tolerance test (ITT) and oral glucose tolerance test (OGTT) were performed after 6 weeks of treatment. Beta cell function was assessed by hyperglycemic clamp technique. The morphological changes in the pancreas were evaluated by hematoxylin-eosin (HE) staining. Changes of iNOS, NF-kappaB p65, and p-NF-kappaB p65 in the pancreas were tested.
RESULTSCompared with the Nor group, the blood glucose level, AUC, and fasting blood insulin, ONOO-contents, iNOS activities, and the expression of iNOS, NF-kappaB p65 subunit, pNF-kappaB p65 subunit obviously increased; decreased percentage of blood glucose within 40 min in ITT, glucose infusion rate (GIR), Clamp 1 min insulin, and Max-Insulin obviously decreased in the Con group (P < 0.05, P < 0.01). Compared with the Con group, the aforesaid indices could be improved in the Met group (P < 0.05, P < 0.01). In the low dose MD group, AUC, iNOS activities, and the expression of iNOS and p-NF-kappaB p65 subunit obviously decreased; percentage of blood glucose within 40 min in ITT and GIR obviously increased (P < 0.05, P < 0.01). In the high dose MD group, AUC, ONOO-contents, iNOS activities, and the expression of iNOS, NF-kappaB p65 subunit, and p-NF-KB p65 subunit obviously decreased; percentage of blood glucose within 40 min in ITT, Max-Insulin, and GIR obviously increased (P < 0.05, P < 0.01).
CONCLUSIONMD could significantly improve IR and functional disorder of 3 cells in MSG obese mice, which might be associated with lowering inflammatory reaction in the pancreas.
Animals ; Disease Models, Animal ; Drugs, Chinese Herbal ; pharmacology ; Female ; Insulin Resistance ; Insulin-Secreting Cells ; drug effects ; metabolism ; Male ; Metformin ; pharmacology ; Mice ; Mice, Inbred ICR ; Mice, Obese ; Obesity ; chemically induced ; metabolism ; Pancreas ; cytology ; drug effects ; Sodium Glutamate
8.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.
9.Phenotype of Chinese patients with Gitelman syndrome and the effect of gender on the Phenotype
Ling QIN ; Leping SHAO ; Hong REN ; Weiming WANG ; Wen ZHANG ; Nan CHEN
Chinese Journal of Nephrology 2009;25(7):532-537
Objective To investigate the clinical features and the effect of gender differences on phenotype of Giteiman syndrome (GS) patients. Methods Clinical features and biochemical parameters were compared and analyzed to look for correlation between male and female GS patients. Results More male patients suffered from nocturia than female patients (P < 0.05), and there were no statistical differences in other clinical features between males and females. The level of serum creatinine was higher in male patients than that in female ones [(82.7±43.3) μmol/L vs (58.7±12.7) μmol/L], but estimated glomerular filtration rate was male patients and female patients. The urinary potassium and chloride excretion fraction were higher in male group than those in female group (33.0%±22.9% vs 17.0%±4.7%;2.30%±1.59% vs 1.23%±0.39%, P< 0.05, respectively). Statistical differences were not observed in other laberatory parameters. Three patients with impaired renal function were all male. Conclusions More male patients suffer from nocturia than female patients. Male patients seem to be prone to impaired renal function. It is speculated that different density of sodium-chloride cotransporter in renal tubule may account for gender differences.
10.Therapetic effects of freeze-dried human fibrin glue on xerophthalmia in perimenopausal female rabbit
Quan ZHOU ; Kangcheng LIU ; Lei YE ; Shuangshuang ZHOU ; Xuexiang ZOU ; Gang TAN ; Nan JIANG ; Yi SHAO
Recent Advances in Ophthalmology 2017;37(5):406-410
Objective To explore prevention and cure effects of the freeze-dried human fibrin glue as the way of the lacrimal duct embolization on xerophthalmia in perimenopausal female rabbit.Methods A total of 72 female rabbits,after anti infection treatment and were cut off third eyelid,were made into perimenopausal xerophthalmia rabbit models.After surgery,all of these rabbits were randomly divided into 6 groups (12 rabbits per group):No treatment group after surgery (group A),PBS prevention group (group B),freeze-dried human fibrin prevention group (group C);no treatment group after modeling (modeling time:Two weeks after surgery,group D),PBS treatment group (group E),freeze-dried human fibrin treatmentgroup (group F).The Schirmer test (SIT),corneal fluorescein (FL) and corneal confocal microscope were performed before and 2 weeks,4 weeks,6 weeks after injection.Results There were statistical differences in FL score and SIT in group A,group B and group C among different time points (F =27.346,10.608;P =0.000,0.001);There were statistical differences between FL scores and SIT among three groups (F =7.579,6.786;P =0.002,0.007);There was significant difference in FL scores and SIT trends among three groups(F =44.897,3.424;P =0.000,0.045).The FL score and SIT of group D,group E and group F were significantly improved after treatment for 2 weeks,4 weeks and 6 weeks,the differences were statistically significant (t =2.906,3.654,4.504;P =0.022,0.017,0.013.t =4.573,5.759,7.231;P =0.032,0.019,0.008);The difference between FL score and SIT in group E and group F was statistically significant after treatment (t =2.776,4.124,5.324;P =0.032,0.026,0.017.t =1.969,3.122,4.324;P =0.038,0.023,0.009).After injection of 6 weeks,the epithelial basal cells (F =17.306,P =0.002) and inflammatory cells (F =34.024,P =0.000) of group A,B and C were significant changed,the differences were statistically significant.After injection of 6 weeks,the epithelial basal cells (F =3.749,P =0.042)and inflarnmatory cells(F=8.806,P =0.005) of group D,E and F were significant changed,the differences were also statistically significant.Conclusion Lacrimal duct embolization with freeze-dried human fibrin glue is effective for the xerophthalmia.