Objective To study the pharmacokinetics of dihydralazine sulfate,triamterene,hydrochlorothiazide and reserpine in compound reserpine and triamterene in rats.Methods SD rats were randomly divided into three groups.Compound reserpine and triamterene was given at dose of 3.6,10.8 and 32.4 mg·kg-1 by single oral gavage,respectively.HPLC-MS was used to measure the blood concentrations of dihydralazine sulfate,triamterene,hydrochlorothiazide,and reserpine at various time points.DAS software was used to compute the pharmacokinetic parameters.Results After a single oral gavage of 3.6,10.8 and 32.4 mg·kg-1 of compound reserpine tablets triamterene,the tmax of dihydralazine sulfate in rat plasma were 1.50,1.33,and 1.42 h,and the Cmax of dihydralazine sulfate were 12.30,38.31 and 120.52 μg·L-1,respectively.The tmax of triamterene were 1.33,1.33,and 1.42 h,and the Cmax of triamterene were 20.93,67.36,and 168.64 μg·L-1,respectively.The tmax of hydrochlorothiazide were 2.00,2.00,and 1.75 h,and the Cmax of hydrochlorothiazide were 19.89,57.58,and 160.78 μg·L-1,respectively.Risperdal was found at very low levels in rat plasma,and only trace amounts were detected at 1.00 and 1.50 h of 32.4 mg·kg-1 administration.Conclusions Dihydralazine sulfate,triamterene,and hydrochlorothiazide can be eliminated quickly after compound reserpine and triamterene was given orally to rats,and their oral absorption is basically linear.The greater the dosage,the better the absorption of effective components.

Objective To study the pharmacokinetics of dihydralazine sulfate,triamterene,hydrochlorothiazide and reserpine in compound reserpine and triamterene in rats.Methods SD rats were randomly divided into three groups.Compound reserpine and triamterene was given at dose of 3.6,10.8 and 32.4 mg·kg-1 by single oral gavage,respectively.HPLC-MS was used to measure the blood concentrations of dihydralazine sulfate,triamterene,hydrochlorothiazide,and reserpine at various time points.DAS software was used to compute the pharmacokinetic parameters.Results After a single oral gavage of 3.6,10.8 and 32.4 mg·kg-1 of compound reserpine tablets triamterene,the tmax of dihydralazine sulfate in rat plasma were 1.50,1.33,and 1.42 h,and the Cmax of dihydralazine sulfate were 12.30,38.31 and 120.52 μg·L-1,respectively.The tmax of triamterene were 1.33,1.33,and 1.42 h,and the Cmax of triamterene were 20.93,67.36,and 168.64 μg·L-1,respectively.The tmax of hydrochlorothiazide were 2.00,2.00,and 1.75 h,and the Cmax of hydrochlorothiazide were 19.89,57.58,and 160.78 μg·L-1,respectively.Risperdal was found at very low levels in rat plasma,and only trace amounts were detected at 1.00 and 1.50 h of 32.4 mg·kg-1 administration.Conclusions Dihydralazine sulfate,triamterene,and hydrochlorothiazide can be eliminated quickly after compound reserpine and triamterene was given orally to rats,and their oral absorption is basically linear.The greater the dosage,the better the absorption of effective components.

Objective To study on the traits,micro-traits and microscopic identification characteristics of common cyrtomium Chinese medicines,including Dryopteridis Crassirhizomatis Rhizoma,Osmundae Rhizoma which were recorded in 2020 edition of Chinese Pharmacopoeia and their three chaotic breeds(Woodwardia unigemmata(Makino)Nakai,Woodwardia japonica(L.F.)Smith and Matteuccia struthiopteris(L.)Todaro,providing a reference for the identification and reference of cyrtomium Chinese medicine.Methods Morphological and micro-character identification methods were used in the character identification,and the normal bright field and polarized dark field contrast observation methods were used in the microscopic identification of cross-sections,combined with extended depth of field imaging and large image stitching techniques,to obtain holographic color images and local feature high definition image.The Chiral labeling methods were used to identified the images.Results The image data of the characters,micro-characters and the normal light and polarized light holographic color image data of cross-section of common cyrtomium herbs and its chaotic varieties were obtained at the first time.The main identification feature retrieval tables and correlation tables of medicinal materials,traits,micro traits and microscopic characters were made.Conclusion Common cyrtomium herbs and its three chaotic varieties can be identified by using characters,micro-characters and microscopic identification comprehensively,especially the microscopic character under polarized light of the cross-section,which has obvious identification significance.

ObjectiveTo investigate the effect of hypoxia-inducible factor-1α (HIF-1α) on the stemness and epirubicin sensitivity of hepatoma cells. MethodsHepatoma cells were selected for experiment. HepG2 hepatoma cells transfected with HIF-1α overexpression plasmid were selected as experimental group, and those transfected with pcDNA3.1 empty plasmid were selected as control group; HepG2 cells alone were selected as HepG2 group. Quantitative real-time PCR was used to measure the mRNA expression of HIF-1α; Western blot was used to measure the protein expression of HIF-1α; flow cytometry was used to measure the expression of CD133 on the surface of hepatoma cells. The three groups of cells were treated with epirubicin at different concentrations (0, 6.25, 12.5, 25, and 50 μmol/L) for 24 hours; MTT assay was used to measure cell viability, and flow cytometry was used to measure apoptosis after treatment with epirubicin (50 μmol/L). A one-way analysis of variance was used for comparison of continuous data between multiple groups, and the t-test was used for further comparison between two groups. ResultsCompared with the HepG2 group and the control group, the experimental group had a significant increase in the mRNA expression of HIF-1α (both P＜0.001), and Western blot showed high expression of HIF-1α in the experimental group. The percentage of CD133 cells was 0.040%±0.003% in the HepG2 group, 0.030%±0.010% in the control group, and 20.110%±0.600% in the experimental group, and the experimental group had a significantly higher positive rate of CD133+ than the HepG2 group and the control group (both P＜0.001). At an epirubicin concentration of 25 and 50 μmol/L, the HepG2 group and the control group had significantly inhibited cell viability and a significantly lower cell viability than the experimental group (both P＜005). After the treatment with 50 μmol/L epirubicin for 48 hours, the experimental group had a significantly lower cell apoptosis rate than the HepG2 group (67.9%±2.5% vs 93.6%±1.5%, P＜0.001) and the control group (67.9%±2.5% vs 93.0%±1.2%, P＜0001). ConclusionHepG2 cells are successfully transfected with HIF-1α overexpression plasmid, and HIF-1α can increase the percentage of liver cancer stem cells and improve their resistance to epirubicin.

Salvianolic acid A (SalA) is an effective compound extracted from traditional Chinese medicine Bunge. The Forkhead box O3a (FOXO3a) signaling pathway plays crucial roles in the modulation of ischemia-induced cell apoptosis. However, no information about the regulatory effect of SalA on FoxO3a is available. To explore the anti-cerebral ischemia effect and clarify the therapeutic mechanism of SalA, SH-SY5Y cells and Sprague-Dawley rats were applied, which were exposed to oxygen glucose deprivation/reoxygenation (OGD/R) and middle cerebral artery occlusion/reperfusion (MCAO/R) injuries, respectively. The involved pathway was identified using the specific inhibitor LY294002. Results showed that SalA concentration-dependently inhibited OGD/R injury triggered cell viability loss. SalA reduced cerebral infarction, lowered brain edema, improved neurological function, and inhibited neuron apoptosis in MCAO/R rats, which were attenuated by the treatment of phosphatidylinositol-4,5-bisphosphate 3-kinase (PI3K) specific inhibitor LY294002. SalA time- and concentration-dependently upregulated the phosphorylation levels of protein kinase B (AKT) and its downstream protein FOXO3a. Moreover, the nuclear translocation of FOXO3a was inhibited by SalA both and , which was also reversed by LY294002. The above results indicated that SalA fought against ischemia/reperfusion damage at least partially the AKT/FOXO3a/BIM pathway.

Algorithms ; Crystallography, X-Ray ; Disulfides ; chemistry ; Models, Molecular ; Protein Conformation ; Proteins ; chemistry

Objective To investigate the mechanism and cause of the inactivation of tumor suppressor gene RNF180 in prostate cancer cell line by observing the effect of 5-Aza-CdR on the RNF180 gene in prostate cancer cell line DU145. Methods MTT method was adopted to study the effect of 5-Aza-CdR(0,1,2,5,10,15 and 20μmoI/L)on the proliferation of prostate cancer cells. Western blotting,real-time PCR,and methyla-tion specific PCR(MSP)were separately used to detect the expression of RNF180 in prostate cancer cells before and after the treatment of the most suitable drug concentration(5μmoI/L). Results In a certain range,the effect of 5-Aza-CdR on the proliferation of prostate cancer cell line DU145 was increased with the increase of drug concentration and the time of drug treatment(P<0.05). After the treatment of the most suitable drug concentration,the protein and mRNA expression of RNF180 in prostate cancer cells was significantly increased(P<0.05),but the methyla-tion of the promoter region was obviously decreased. Conclusion 5-Aza-CdR can reverse the methylation status of RNF180 gene in DU145 pros-tate cancer cell line,and relieve the silencing status of RNF180gene expression.

Objective To clarify the significance of RNF180 expression in carcinogenesis and progression of prostate cancer by detection of RNF180 promoter methylation. Methods RNF180 expression was detected in human prostate cancer cell lines(PC3,LNCap,and DU145)and normal prostate cells(RWPE?1)via Western blotting,RT?PCR,methylation?specific PCR(MSP),bisulfite?sequeneing PCR(BSP),respectively, while RNF180 expression in human prostate cancer tissues and paired adjacent non?tumor tissue was detected via immunohistochemistry. Results The expressions of RNF180 mRNA and protein in prostate cancer cells were significantly lower than those in normal prostate cells(P<0.05),op?posite to what was observed for the methylation level of the RNF180 promoter. Additionally,the RNF180 expression in prostate cancer tissue was significantly lower than that in paired adjacent non?tumor tissue. Conclusion The RNF180 promoter is incompletely methylated in prostate can?cer cells,which may be a reason for the decline or silencing of RNF180 expression in cancer cells and tissues.

Objective · To compare the short and medium-term efficiency and safety of 1470 nm laser with foam sclerotherapy with ligation of great saphenous vein and 808 nm laser with foam sclerotherapy to treat varicose veins of lower extremity. Methods · Seventy-seven hospitalized patients patients and twenty-one day-surgery patients were retrospectively analyzed. Results · There was no obvious difference in the closure of great saphenous vein for short to medium-term efficiency between the day-surgery group and hospitalized group. The postoperative complications and recurrence rate of day-surgery group was not higher than that of the hospitalized group, but the degree of perioperative comfort, economic cost and the time returning to normal life of day-surgery group were superior to that of the hospitalized group. Conclusion · 1470 nm laser with foam sclerotherapy with ligation of great saphenous vein and 808 nm laser with foam sclerotherapy to treat varicose veins of lower extremity had similar clinical effect, but the degree of safety and comfort was higher and trauma was less. The day surgery with 1470 nm laser to treat varicose vein of lower extremity could also simplify the procedure of hospitalization and reduce the cost of health care, which could be a new option for patients.

Objective To compare the short term clinical efficacy of percutaneous resection and laparoscopic deroofing of renal cysts.Methods From October 2013 to June 2016,the data from 39 cases with renal cysts were followed for approximately 22 months (ranging 5-36 months).Patients were randomized into two groups.In the resectoscopic group(17 pts),the mean age of those patients was 57 years (ranging 34-81 years).The mean size of these cysts was 6.4cm (ranging 5.4-8.2 cm).The mean preoperative creatinine was 66.5μmol/L (ranging 38.1-108.8μ mol/L).The mean preoperative sodium was 141.4μ mol/L(ranging 135.6-145.1μmol/L).The mean preoperative potassium was 4.0μmol/L (ranging 3.4-4.7 μmol/L).In the latter laparoscope (22pts),the mean age of these patients was 60 years (ranging 46-73 years).The mean size of these cysts was 6.8cm (ranging 4.3-8.9cm).The mean preoperative creatinine was 74.8μmol/L (ranging 48.6-141.9μmol/L).The mean preoperative sodium was 141.5μmol/L(ranging 135.0-146.1 μmol/L).The mean preoperative potassium was 4.0μmol/L (ranging 3.1-4.8μmol/L).The operative time,blood loss,days of drainage,hospital stay and complications were compared with the two groups.Results All of the 39 cases were accepted the procedure successfully without open conversion.Compared the resectoscopic group with Laparoscopic,the mean operative time was 29.7 min (ranging 15-50 min) and 63.0min (ranging 20-1 00 min),mean blood loss was 36.6ml(ranging 10-80 ml) and 60.4ml(ranging 10-200 ml),days of drainage was 2.3 days and 3.1 days,hospital stay was 3.7 days and 5.1 days,the mean postoperative creatinine was 67.4 μmol/L(ranging 43.8-95.5 μmol/L) and 68.9μmol/L(ranging 46.5-157.6 μmol/L),the mean postoperative sodium was 141.2μmol/L(ranging 136.0-147.2 μmol/L) and 141.6 μmol/L(ranging 136.0-147.2 μmol/L),the mean postoperative potassium was 3.8 μmol/L (ranging 3.2-4.3 μmol/L) and 3.8μmol/L (ranging 3.3-4.3 μmol/L).The overall postoperative pathology was renal cysts.All cases were followed for approximately 19 months (ranging 6-35 months) and 22 months (ranging 5-36 months) in reseetoscopic and laparoscopic group respectively.No cysts recurrence was found by ultrasound.Conclusions Compared with laparoscopic deroofing,use of resectoscopic technology significantly enhances the possibility of achieving better intraoperative results in all patients with renal cysts.Percutaneous resection of simple renal cysts is safe and feasible.