The aim of this paper was to investigate the effect of terpene penetration enhancers on membrane fluidity and membrane potential using HaCaT keratinocytes, and study the potential mechanisms of these terpene compounds using as natural transdermal penetration enhancer. Six terpene compounds, namely menthol, limonene, 1,8-cineole, menthone, terpinen-4-ol and pulegone, were chosen in this study on account of their good penetration-enhancement activities. The cytotoxicity of these terpene compounds was measured using an MTT assay. The fluorescence recovery after photobleaching (FRAP) technique was employed to measure the change of membrane fluidity of HaCaT cells. The flow cytometer was used to study the alteration of membrane fluidity of HaCaT cells, and investigate the effect of terpene compounds on intracellular Ca2+. It was found that 6 terpene compounds possessed low cytotoxicity in comparison to the well-established and standard penetration enhancer azone. Those terpene compounds could significantly enhance HaCaT cells membrane fluidity and decrease HaCaT cells membrane potentials. Meanwhile, after treated with various terpene compounds, the Ca2(+)-ATPase activity and intracellular Ca2+ of HaCaT cells was decreased significantly. Terpene penetration enhancers perhaps changed the membrane fluidity and potentials of HaCaT cells by altering the Ca2+ balance of the cell inside and outside, resulting in the low skin permeability to increase the drug transdermal absorption.
Cell Line ; Drugs, Chinese Herbal ; pharmacokinetics ; Humans ; Keratinocytes ; drug effects ; metabolism ; Membrane Fluidity ; drug effects ; Skin Absorption ; drug effects ; Terpenes ; pharmacokinetics

OBJECTIVETo determine the suitable conditions for extracting alkaloidals from Aconitum carmichaili.

METHODUsing methods in Chinese Pharmacopeia for determining yields of extraction, which include spectrometry and single-factor tests, we investigated vavious factors that would affect the extraction of alkaloids from Aconiti.

RESULTThe suitable extractant was 85% ethanol, starting material was medium-size powder of aconiti, 10 times of the volume of the solvent was used in extraction for twice 1.75 h each time. The extraction yield was 1.21%, with a content of 0.33% alkaloids.

CONCLUSIONExtraction conditions determined with single factor test was consistent and feasible.

Aconitum ; chemistry ; Alkaloids ; analysis ; isolation & purification ; Ethanol ; Particle Size ; Plants, Medicinal ; chemistry ; Powders ; Technology, Pharmaceutical ; methods ; Time Factors

Genomic DNA was extracted from the blood samples of 3 patients from 1 pedigree with congenital nephrogenie diabetes insipidus (NDI) and their 12 family members.The whole coding region of the arginine vasopressin receptor 2 (AVPR2) gene was amplified by PCR and then directly sequenced,A mutation of AVPR2 gene [g1236T→C (L292P)]was found in 3 patients.The patients' mothers were found to have both mutant and normal alleles.

Objective To study effect of excessive iodine intake on sodium-iodide symporter(NIS)mRNA and protein expression of breast in lactating rats.Methods60 Wistar rats,having been weaned for one month,were randomly divided into three groups according to their body weights,I.e,①normal iodine(NI,30 rats);②ten fold high iodine(10 HI,15 rats);③one hundred fold high iodine(100 HI,15 rats).Eating food containing iodine of 300μg/L and drinking water of iodine at 5,1845,20 295μg/L,respectively.After fed for 3 months,the rats mated and had offspring,and urine and milk iodine of lactating rats were determined by As-Ce-catalytic spectrophotometric method.Their marmnary glands were sampled at lactation day 10.Then NIS mRNA expression by RT-PCR was determined and NIS protein by immunohistochemistry(SABC)was observed.Results The urine iodine of 10 HI group(3597.5μg/L)and 100HI group(25 404.3μg/L)increased obviously compared with that of NI group(344.7μg/L).The milk iodine of 10HI group(27.1×103μg/L)and 100HI group(191.0×1μg/L)was higher than that of NI group(6.0×103μg/L),but the increased fold of milk iodine was not paralleled with that of urine iodine.Difference of NIS mRNA expression was significant(F=24.19,P＜0.01)among the groups,and the NIS mRNA expression in 10HI(1.250±0.034)and 100HI(1.272±0.039)group were less than that in NI (1.532±0.044)group(P＜0.01).The breast NIS mRNA expression in lactating rats(1.532±0.044)was significantly higher than that in unlactating rats(0.879±0.018,P＜0.01).With the increasing iodine uptake,NIS protein expression decreased.Conclusions The NIS mRNA and protein in rat breasts is down-regulated by excessive iodine intake.So increasing extent of milk iodine concentration is inhibited,which is important to prevent off-spring from getting excessive iodine intake from parental generation.

OBJECTIVETo explore the effects and mechanisms of multi-glycoside of Tripterygium wilfordii (GTW) on improving glomerular inflammatory lesion in rats with diabetic nephropathy (DN).

METHODDN model was induced by unilateral nephrectomy and intraperitoneal injection of STZ (35 mg x kg(-1)) twice. The rats were randomly divided into 3 groups, the sham-operated group (Sham group, n = 5), the vehicle-given group (Vehicle group, n = 5 ) and GTW-treated group (GTW group, n = 5). After the model was successfully established, the rats in GTW group were daily oral administrated with GTW suspension (50 mg x kg(-1) x d(-1)), meanwhile, the rats in Vehicle group were daily oral administrated with distilled water (2 mL) for 8 weeks. From the beginning of the administration, all rats were killed 8 weeks later. Blood and renal tissues were collected,and then UAlb, renal function, glomerular morphology characteristics and glomerular macrophages (ED1 + cells) infiltration, as well as the protein expressions of inflammatory cytokines including tumor necrosis factor(TNF)-α and interleukin(IL)-lβ, and the key molecules in p38MAPK signaling pathway including p38 mitogenactivated protein kinase (MAPK), phosphorylated p38 (p-p38MAPK) and transforming growth factor(TGF)-β1 were investigated respectively.

RESULTGTW not only ameliorated the general state of health and body weight,but also attenuated UAlb, glomerulosclerosis, the infiltration of glomerular ED1 + cells and the protein expressions of TNF-α, IL-1β, p-p38MAPK and TGF-β1 in the kidney in DN model rats.

CONCLUSIONBy means of DN model rats, we demonstrated that GTW has the protective effect on renal inflammatory damage in vivo via inhibiting inflammatory cells infiltration and inflammatory cytokines expression. Furthermore, GTW could improve renal inflammatory lesion through down-regulating the expressions of the key signaling molecules in p38MAPK pathway such as p-p38MAPK and TGF-β1 ,and inhibiting the activation of p38MAPK signaling in the kidney.

Animals ; Diabetic Nephropathies ; drug therapy ; Disease Models, Animal ; Glomerulonephritis ; drug therapy ; Glycosides ; pharmacology ; MAP Kinase Signaling System ; drug effects ; Male ; Rats ; Rats, Sprague-Dawley ; Transforming Growth Factor beta1 ; analysis ; Tripterygium ; chemistry ; p38 Mitogen-Activated Protein Kinases ; physiology

To explore influence of Xinmailong injection on cardiac function and vascular endothelial func‐tion in advanced aged patients with acute myocardial infarction (AMI) heart failure (HF).Methods : A total of 122 advanced aged AMI‐HF patients treated in our hospital from Mar 2015 to Jul 2017 were selected ,randomly and e‐qually divided into routine treatment group (received routine anti‐HF medication ) and Xinmailong group (received Xinmailong injection based on routine treatment group ) ,both groups were treated for 10d and then followed up for six months .LVEF ,wall motion score index (WMSI) ,serum levels of BNP , hsCRP , cTnI ,nitric oxide (NO) ,en‐dothelin (ET)‐1 and inner diameter of brachial artery were observed and compared between two groups before and after treatment .Results : Compared with before treatment ,there were significant rise in LVEF [routine treatment group : (35.42 ± 5.11)% vs. (44.62 ± 5.88)%;Xinmailong group : (36. 13 ± 5.64)% vs. (49.75 ± 6. 18)%] and serum NO level [routine treatmentgroup : (108. 35 ± 21.67) μmol／L vs. (129.68 ± 25. 83 ) μmol／L ; Xinmailong group : (110.26 ± 22.71) μmol／L vs. (156.82 ± 24. 19) μmol／L] ,and significant reductions in WMSI [routine treatment group : (2.49 ± 0.51) score vs. (1.45 ± 0.34) score ; Xinmailong group : (2.51 ± 0.42) score vs. (1. 12 ± 0.27) score] ,NYHA class (routine treatment group :3.19 ± 0. 44 vs. 2.65 ± 0.36 ;Xinmailong group :3. 21 ± 0.42 vs. 2.11 ± 0.28) ,serum levels of BNP [routine treatment group : (986. 72 ± 245.63 ) pg／ml vs. (764.42 ± 217.33) pg／ml ; Xinmailong group : (989.99 ± 243. 54 ) pg／ml vs. (607. 82 ± 198. 65 ) pg／ml ] , hsCRP [routine treatment group : (24.31 ± 3.82) mg／L vs. (14.52 ± 1. 69 ) mg／L ; Xinmailong group :(24.93 ± 3.74) mg／L vs. (7. 81 ± 0. 96) mg／L] ,cTnI [routine treatment group :(5.29 ± 0.43) μg／L vs. (3.01 ± 0. 27) μg／L ;Xinmailong group :(5.37 ± 0.64) μg／L vs. (1.42 ± 0.33) μg／L ] and ET‐1 [routine treatment group :(95. 67 ± 16. 32) ng／L vs. (76. 34 ± 17.82) ng／L ;Xinmailong group :(96.13 ± 17.21) ng／L vs. (57.29 ± 14. 63) ng／L] in two groups ;and LVEF and serum NO level of Xinmailong group were significantly higher than those of routine treatment group , WMSI ,NYHA class ,serum levels of BNP ,hsCRP ,cTnI and ET‐1 of Xinmailong group were significantly lower than those of routine treatment group , P＝0.001 all.Compared with before treatment ,there were significant rise in reactive hyperemia brachial diameter (Dhyperemia ) , fore brachial artery endothelium dependent diastolic‐systolic function (FMD) in Xinmailong group after treatment , and they were significantly higher than those of routine treatment group , P＜0. 05 or ＜0. 01 .Conclusion : Xinmailong injection can significantly improve cardiac function and vascular endothelial function in AMI‐HF patients ,which is worth extending .

AIMTo evaluate in vitro release of lycopene microcapsules. Pharmacokinetic parameters of lycopene microcapsule and lycopene powder as reference were estimated after a single dose of oral administration to dogs. The relationship between in vitro dissolution and in vivo absorption was investigated.

METHODSThe content of lycopene in the release medium was determined by UV spectroscopy method. Health hybrid male dogs were used as experiment subjects and lycopene powder used as standard to estimate the pharmacokinetics of lycopene microcapsules. HPLC method was used to assay the concentration of lycopene in dog plasma. Pharmacokinetics parameters were estimated by 3P87 program. The drug release percentage in stimulated intestinal fluid was compared with the absorption at a given time point.

RESULTSThe release profiles of lycopene from microcapsule showed that the lycopene gelatin microcapsule exhibited enteric property. The pharmacokinetics parameters estimated after oral administration of lycopene powder and lycopene microcapsule in a single dose of 2.5 mg x kg(-1) body weight to dogs were 7.30 h, 15.06 h for T1/2alpha; 28.10 h, 46.76 h for T1/2beta; 22.32 h, 41.03 h for T(max); 1.67 microg x h x L(-1), 2.08 microg x h x L(-1) for AUC(0-infinity), respectively. The concentration-time curves could be fitted to a two-compartment model for both the lycopene powder and the lycopene microcapsule analyzed by 3P87 program. The relationship between in vitro dissolution and in vivo absorption was found to have good correlation (r = 0. 981 9) was found.

CONCLUSIONIt could be concluded that lycopene microcapsule was a sustained release dosage form. The result of release in vitro could be used to predict the absorption in vivo.

Administration, Oral ; Animals ; Antioxidants ; administration & dosage ; pharmacokinetics ; Area Under Curve ; Biological Availability ; Capsules ; Carotenoids ; administration & dosage ; pharmacokinetics ; Delayed-Action Preparations ; Dogs ; Male

OBJECTIVETo explore distinctive manifestations of rheumatoid arthritis (RA) patients of cold syndrome and heat syndrome using wrist joints ultrasound.

METHODs Totally 65 RA patients were syndrome typed as cold syndrome (29 cases, cold-damp blockage syndrome) and heat syndrome (36 cases, damp-heat obstruction syndrome). Grey-scale synovitis, power doppler (PD) signals, tenosynovitis, and bone erosion were observed using wrist ultrasound. Distinctive manifestations of cold syndrome and heat syndrome were analyzed using wrist ultrasound.

RESULTSIn RA patients of cold syndrome, the positive rate of synovitis, PD, tenosynovitis, and bone erosion was 51.72%, 20.68%, 51.72%, and 37.93%, respectively, while they were 97.22%, 91.67%, 75.0%, and 63.89%, respectively in RA patients of heat syndrome. Compared with patients of cold syndrome, the positive rate of synovitis, PD, and bone erosion increased in patients of heat syndrome (P < 0.01, P < 0.01, P < 0.05). There was no statistical difference in the positive rate of tenosynovitis between the two groups (P > 0.05). Compared with the cold syndrome group, there was statistical difference in the constituent ratio of synovitis, PD, and bone erosion in the heat syndrome group (P < 0.01, P < 0.01, P < 0.05), but with no statistical difference in the constituent ratio of tenosynovitis (P > 0.05). Results of the ROC curve showed that the sensitivity was 86.1% and the specificity was 62.1% in judging heat syndrome, when the total score of synovitis in two wrists was more than 1.5; the sensitivity was 80.0% and the specificity was 93.1% in judging heat syndrome, when the total score of PD in two wrists was more than 1.5.

CONCLUSIONSPositive rates of synovitis, PD, and bone erosion were significantly higher in RA patients of heat syndrome than those of cold syndrome. Especially serious manifestations were more often seen in RA patients of heat syndrome. The total score of synovitis or PD in the two wrist joints higher than 1.5 was characteristic manifestations of heat syndrome using wrist ultrasound.

Arthritis, Rheumatoid ; therapy ; Hot Temperature ; Humans ; Medicine, Chinese Traditional ; ROC Curve ; Sensitivity and Specificity ; Syndrome ; Synovitis ; Ultrasonography ; Wrist ; diagnostic imaging ; Wrist Joint ; diagnostic imaging

OBJECTIVETo provide the foundation for reasonable utilization by analyzing the essential oils of Ligularia virgaurea.

METHODThe essential oils were extracted by using steam distillation and separated with GC capillary columns. The components were quantitatively determined with normalization method, and were identified with GC-MS.

RESULT41 components were identified, which took up 72.73% of the essential oils.

CONCLUSIONThe main components of essential oils were 4-methyl-1-(1-methylethyl)-3-cyclohexen-1-ol(14.369%), crotonic acid, 2,2-dimethyl-butanoic acid, 1-methyl-3-(1-methylethyl)-benzene, (1s-endo)-1,7,7-trimethyl-bicyclo[2,2,1]heptan-2-ol, trans-1-methyl-4-(1-methylethyl)-2-cyclohexen-1-ol, alpha-cadinol and alpha,alpha,4-trimethyl-3-cyclohexene-1-methanol.

Asteraceae ; chemistry ; Butyrates ; analysis ; Crotonates ; analysis ; Gas Chromatography-Mass Spectrometry ; Oils, Volatile ; chemistry ; isolation & purification ; Plant Oils ; chemistry ; isolation & purification ; Plants, Medicinal ; chemistry ; Terpenes ; analysis

OBJECTIVETo summarize the clinical experience from treatment of patients with severe acute respiratory syndrome (SARS).

METHODSRetrospective analysis of seven patients with SARS in Ditan hospital treated since April 22 in 2004 was performed.

RESULTSIn the 7 patients, 2 were male, 5 were female, and the average age was (35.3 plus/minus 11.3) years. The main clinical manifestations were fever, cough, minor or serious dyspnea, nausea, signs of injury to other organs, and so on. The treatment regiments included oxygen, small dosage and short period of methylprednisolone (1 to 2 mg/kg), use of ventilator, psychological intervention, and treatment of underlying diseases, after which, all the 7 patients recovered.

CONCLUSIONRational use of methylprednisolone and timely use of ventilator were the key steps of treatment.

Adult ; Anti-Inflammatory Agents ; therapeutic use ; Combined Modality Therapy ; Cross Infection ; drug therapy ; therapy ; transmission ; Female ; Humans ; Infectious Disease Transmission, Patient-to-Professional ; Male ; Methylprednisolone ; therapeutic use ; Middle Aged ; Oxygen Inhalation Therapy ; Retrospective Studies ; Severe Acute Respiratory Syndrome ; therapy ; transmission ; Ventilators, Mechanical