Objective To increase the solubility and relieve the mucous irritation of cantharidin (CA) by preparing cantharidin-hydroxypropyl-β-cyclodextrin (CA/HP-β-CD) inclusion complex.Methods The inclusion complex was prepared by co-evaporation method and characterized by differential scanning calorimetry (DSC),X-ray diffractometry (XRD),and nuclear magnetic resonance (NMR).Results The disappearance of CA as well as the shift of exothermic peaks shown in DSC results indicated the complexation phenomenon.XRD results showed that the crystalline CA pattern had disappeared,and in NMR results,H-5 shifted from δ 3.731to 3.695 after complexation and H-2 shifted from δ 3.626 to 3.598,which suggested that part of the drug had entered the HP-β-CD cavity to form an inclusion complex.The solubility increased 10.3 times after complexation and the mucous irritation of CA was relieved remarkably.Conclusion Through complexation with HP-β-CD,the solubility and dissolution rate of CA are improved significantly,and the irritation of musous is relieved.

Objective To investigate the changes in the concentration of myocardin in children with lupus nephritis (LN) under different degree of vessel damage.Methods Forty-nine children diagnosed with LN by routine tissue immunolfuorescence, light microscope, and electron microscope were included, and 30 healthy children were included as control group. The pathological classiifcations were performed according to the ISN/RPS 2003 LN pathological classiifcation criterion. According to the Katafuchi evaluation method, the semi quantitative assessment of glomerular and kidney tubule damage was carried out, and the degree of vascular damage was evaluated at the same time. Double antibody sandwich method was used to detect the concentration of serum myocardin.Results The glomerular and kidney tubules damage in children with LN were signiifcantly aggravated with higher pathological classification (P<0.05). Glomerular damage was positively correlated with renal interstitial damage (r=0.96, P<0.01). The degree of vascular damage was related to the degree of glomerular injury and renal interstitial injury, while it was no related with the results of clinical tests. There were different concentrations of myocardin among mild-, moderate-, severe-vessel damage and control groups (F=378.61,P<0.001), and the concentration of myocardin in moderate- and severe-vessel damage groups were obviously lower than those in control group and mild-vessel damage group (P<0.01) while there was no difference between control group and mild-vessel damage group (P>0.05). According to pathological type, there were signiifcant differences in the concentration of myocardial between control group and different pathological types (F=626.793,P<0.01). FromⅡ,Ⅲ,Ⅲ+Ⅴ,Ⅳ toⅣ+Ⅴ, the concentrations of myocardial were decreased systematically, and there were statistic differences between groups (P all<0.05).Conclusion The concentration of myocardin in children with LN can relfect the renal vascular damage to a certain extent. Elevation of myocardin concentration may be helpful for the repair of vascular damage.

OBJECTIVETo study the pharmacokinetics and bioavailability of cantharidin in beagle dogs to evaluate the pharmacokinetic parameters and bioavailability of cantharidin in beagle dogs by determining dose-time curve and by comparing with the pharmacokinetics of cantharidin injection.

METHODSix beagle dogs, after protein precipitation by hydrochloric acid, ethyl acetate was applied to extract cantharidin from plasma The plasma concentration of cantharidin in beagle dogs was determined by GC-MS. The WinNonLin program was used to calculate the pharmacokinetic parameters and bioavailability.

RESULTThe main pharmacokinetic parameters of cantharidin by iv in dogs (34 mL x h(-1) x kg(-1)) were AUC (203.5 +/- 23.8) h x microg x L(-1), CL (168.8 +/- 18.6) mL x h(-1) x kg(-1), t1/2 (0.69 +/- 0.03) h. The main pharmacokinetic parameters of cantharidin by op (102 microg x kg(-1)) were: AUC (160.4 +/- 26.9) h x microg x L(-1), CL (649.1 +/- 97.7) mL x h(-1) x kg(-1), t1/2 (0.38 +/- 0.1) h., F (bioavailability) = 26.7% comparing to injection.

CONCLUSIONAs compared with cantharidin injection, the absorption of catharidin by op is poor and the bioavailability is also low, indicating that enhancement of the bioavailability will be beneficial to the clinical application.

Animals ; Biological Availability ; Cantharidin ; pharmacokinetics ; Coleoptera ; chemistry ; Dogs ; Male ; Models, Animal

Objective To analyze the characteristics of clinical manifestations, risk factors, therapies and acute outcomes in patients with cerebral venous sinus thrombosis complicated by cerebral hemorrhage. Methods Seventy-five patients with cerebral venous sinus thrombosis were included in the study. According to the radiological findings on the brain image, patients were divided into two subgroups:cerebral hemorrhage group and non-hemorrhage group. The demo?graphic data, potential risk factors, clinical manifestations, radiological features, therapeutic strategies and acute out?comes were compared between two subgroups, and high risk factors were also analyzed. Results There were seventy-five patients with cerebral venous sinus thrombosis in the present study. Twenty-eight patients of them (37.2%) had cerebral hemorrhage whereas the remaining forty-seven patients (62.7%) did not have cerebral hemorrhage. Pregnancy/puerperi?um were significantly higher in patients with cerebral hemorrhage (with vs without;28.6%vs. 6.4%, P=0.015), while in?fection was markedly higher in patients without cerebral hemorrhage (with vs without;7.1% vs. 29.8%, P=0.021). Head?ache (92.9% vs. 70.2%, P=0.021), unconsciousness (25.0% vs. 6.4%,P=0.034), seizures (53.6% vs. 19.1%, P=0.002) and motor deficits (35.7% vs. 12.8%, P=0.019) were more common in patients with cerebral hemorrhage. Moreover, mul?tiple sinus involvement (1.4% vs. 44.7%, P=0.024) was significantly higher and the acute outcomes(mRS≥3: 46.4%vs.17.0%, P=0.006)were poorer in patients with cerebral hemorrhage. Binary Logistic analysis showed that pregnancy/pu?erperium (P=0.004) and multiple sinus involvement were positively, whereas infection was negatively correlated with cere?bral venous sinus thrombosis and hemorrhage ( P=0.007;P=0.03). Conclusions Pregnancy/puerperium, headache, uncon?sciousness, seizures, motor deficits and multiple sinus involvement are more frequently in patients with cerebral venous sinus thrombosis and hemorrhage, and the acute outcomes are poorer in patients with cerebral venous sinus thrombosis complicated by cerebral hemorrhage.

Objective: To investigate the expression of lncRNA01296 in esophageal cancer (EC) tissues and its effect on the proliferation and migration of EC TE-2 cells. Methods:Atotal of 36 pairs of esophageal cancer tissues and corresponding para-cancerous tissues were collected from EC patients admitted to the Department of Thoracic Surgery,Affiliated Hospital of Chengde Medical College from January 2017 to September 2018. The human normal esophageal epithelial (HEEC) cells and human esophageal cancer cell lines ECA109, TE-1 and TE-2 were cultured. qPCR was used to detect the mRNAexpressions of lincRNA01296, SNRPA(small nuclear ribonucleoproteinA) and NGF (nerve growth factor) in EC tissues and cells. Recombinant lentiviral interference vectoror control vector were used to transfect EC cell lines, as sh-lncRNA01296#1,#2 and Mock groups. WB was used to detect the protein expressions of SNRPAand NGF in transfected cells. MTS assay was used to detect cell proliferation, and Transwell assays were used to detect cell invasion and migration of TE-2 cells after transfection. Results: The mRNAexpressions of lncRNA01296, SNRPAand NGF were significantly increased in esophageal cancer tissues and cell lines (all P<0.01), and these expressions in poorly differentiated TE-2 cells were higher than those in highly differentiated ECA109 and TE-1 cells (all P<0.05). The mRNAexpressions of lncRNA01296 and NGF in sh-lncRNA01296#1 and sh-lncRNA01296#2 groups were significantly lower than those in Mock group (all P<0.01), while the mRNAexpression of SNRPAshowed no statistical difference among three groups (P>0.05). The protein expressions of lncRNA01296 and NGF in sh-lncRNA01296#1 and sh-lncRNA01296#2 groups were significantly lower than those in Mock group (all P<0.01). The relative proliferation ability of cells in sh-lncRNA01296#1 and shlncRNA01296#2 groups was significantly lower than that of Mock group at 48 and 72 h after transfection (P<0.05 or P<0.01). The number of invasive cells was (72.0±6.3), (36.6±4.3) and (33.9±3.7) in Mock, sh-lncRNA01296#1 and sh-lncRNA01296#2 groups, respectively; and the number of migrated cells was (85.2±9.9), (47.5±8.1) and (43.8±6.5), respectively, indicating that the numbers of invasive and migrated cells in sh-lncRNA01296#1 and sh-lncRNA01296#2 groups were significantly less than those in Mock group(all P<0.01). Conclusion: lncRNA01296 can up-regulate SNRPAexpression to promote NGF-mediated proliferation and metastasis of EC cells, which may provide new target for the diagnosis and treatment of esophagealcancer.