2.Synthesis and tumor resistance reverse activities ofα-hederagenin-type ring-A fused pyrazine derivatives
Xiao WANG ; Xian-Xuan LIU ; Yan-Ting YANG ; Hong-Bo WANG ; Yi BI
Chinese Journal of Pharmacology and Toxicology 2018;32(4):308-308
α-Hederagenin (H), derived from Hedera nepalensis var.sinensis, is a pentacyclic oleane-type triterpenoid that exhibits clear cytotoxicity to different tumor cell lines.In this study,a series of novel C-28 derivatives of hederagenin (H) were designed and synthesized in attempt to develop potent tumor resistance reverse activities agents. Previous research showed that H6 displayed robust reverse activity for paclitaxel resistance in KBV cells. Importantly, Co-treatment of paclitaxel with H6 significantly reduced the tumor weight to 42%. Pleasingly, H6 enhanced the efficacy of paclitaxel against KBV cancer cell-derived xenograft tumors in nude mice.Mechanism studies had found that H6 activated permeability glycoprotein(P-gp)ATPase,reduced intracellular ATP levels and inhibited efflux of P-gp substrates,thus enhancing the antitumor activity of paclitaxel on KBV cells.Molecular docking analysis of homology P-gp and H6 then conducted using the Surflex-Dock module.H6 showed a high binding affinity docking score with a total score of 5.4148,much higher than that of H(0.1414).The nov-el C-28 derivatives of H was synthesized from H6 via three-step reaction. The reversal activity of all synthesized H derivatives were tested using the MTT assay.The results showed that the derivatives of nitrogen groups at C-28 displayed same even potent activity than parent compound H6.In addition,its underlying mechanism of action and in vivo activity are in explore.
3.The Effect of Low Molecular Protein Iron on Iron Deficiency Anemia
Xian-Hua CHENG ; Hong PIAO ; Yong-Bo WANG
Journal of Experimental Hematology 2001;9(3):240-242
Objective is designed to observe the effect of the low molecular protein "SL Hong-Xin Blood-Increasing Capsules" on human iron deficiency anemia. Altogether 110 school children, 7 - 12 years old, with iron deficiency anemia (Hb < 120 g/L) were enrolled in this trial and were randomly and evenly divided into two groups. In the treatment group (n = 55), the "SL Hong-Xin Blood-Increasing Capsules" were orally adminitered for 30 days, two capsules at one time and two times a day, whereas in the control group (n = 55) blank capsules were given to the children in the same way as in the treatment group. Before and at the end of the trial period, peripheral blood samples were taken from fringers of the children to determine Hb content, hematocrit percentage, and free protoporphyrin content in red blood cells. Results showed that after trial the Hb content was (15.9 +/- 9.6) g/L in the treatment group, while that of the control group was only (5.3 +/- 4.3) g/L (P < 0.001). The hematocrit percentage markedly increased (P < 0.001) and protoporphyrin level markedly decreased (P < 0.001). In conclusion the active ingredient of "SL Hong-Xin Blood-Increasing Capsules" is low molecular protein iron, which is markedly effective for elevating Hb content and hematocrit percentage, and effective for decresing protoporphyrin content of children with iron deficiency anemia. Hence, the capsules could be used to improve nutritional anemia in children based on the "Functional Evaluation Procedure and Test Methods For Health-Care Food".
4.Discussion of Chinese syndrome typing in acute hepatic failure model.
Jin-liang ZHANG ; Hui ZENG ; Xian-bo WANG
Chinese Journal of Integrated Traditional and Western Medicine 2011;31(5):659-662
OBJECTIVETo study Chinese syndrome typing of acute hepatic failure (AHF) mice model by screening effective formulae.
METHODSLipoplysaccharides (LPS)/D-galactosamine (D-GaIN) was intraperitoneally injected to mice to establish the AHF mice model. Yinchenhao Decoction, Huanglian Jiedu Decoction, Buzhong Yiqi Decoction, and Xijiao Dihuang Decoction were administered to model mice respectively by gastrogavage. The behavior and the survival rate were monitored. The liver function and pathological changes of liver tissues were detected.
RESULTSIn all the tested classic recipes, the survival rate was elevated from 10% to 60% by administration of Xijiao Dihuang Decoction. Five h after modeling, the serum alanine aminotransferase (ALT) level was (183.95 +/- 52.00) U/L, and aspartate aminotransferase (AST) (235.70 +/- 34.03) U/L in Xijiao Di-huang Decoction Group, lower than those of the model control group, but with insignificant difference (ALT: 213.32 +/- 71.93 U/L; AST: 299.48 +/- 70.56 U/L, both P > 0.05). Xijiao Dihuang Decoction could obviously alleviate the liver injury.
CONCLUSIONSXijiao Dihuang Decoction was an effective formula for LPS/D-GaIN induced AHF model. According to syndrome typing through formula effect, heat toxin and blood stasis syndrome dominated in the LPS/D-GalN induced AHF mice model.
Animals ; Disease Models, Animal ; Drugs, Chinese Herbal ; Liver Failure, Acute ; diagnosis ; drug therapy ; Male ; Medicine, Chinese Traditional ; Mice ; Mice, Inbred C57BL ; Phytotherapy
5.Intervening and therapeutic effect of cordyceps mycelia extract on liver cirrhosis induced by dimethylnitrosamine in rats.
Xian-Bo WANG ; Ping LIU ; Zhi-Peng TANG
Chinese Journal of Integrated Traditional and Western Medicine 2008;28(7):617-622
OBJECTIVETo explore the intervening and therapeutic effect of Cordyceps mycelia extract (CME) on liver cirrhosis induced by dimethylnitrosamine (DMN) in rats.
METHODSRat liver cirrhosis model was established by peritoneal injection of DMN at a dose of 10 microg/kg, once daily in the first 3 days of every week for 4 successive weeks. Experimental study on CME-intervention was conducted from the beginning of modeling to the end of the 4th week, while the CME-treatment experiment was carried out from the 4th week of modeling, when terminating the modeling factor, to the end of the 8th week, by administering CME at a dose of 0. 74 g/( kg d) once a day. Animals were killed in batches on the 3rd day, the 2nd (T1), 4th (T2), 6th (T3) and 8th (T4) week after modeling, to observe the histopathologic change in liver and the immunohistochemical staining of alpha-smooth muscle actin (alpha-SMA) and collagen type I (Col I), determine the content of hydroxyproline (Hyp) in liver, and the liver function was tested as well.
RESULTSCME-intervention experiment showed that as compared to those in the modeled rats at corresponding time points, in rats at T1 and T2, serum alanine aminotransferase (ALT), aspartate aminotransferase (AST) activity and total bilirubin (TBIL) content were significantly lower, and albumin (Alb) obviously higher; while at T2, Hyp content, ct-SMA and Col I positive expression were significantly lower (P < 0.05), the proliferation of collagen fibre attenuated. CME-treatment experiment showed that as compared to those in the modeled rats at corresponding time points, lower serum ALT, AST activity and TBIL content, and higher serum level of Alb were shown in rats at T1; and lower Hyp content, liver collagen fibre, and alpha-SMA positive expression were shown at T1 and T2; while less Col I positive expression at T2 was also shown in them (all P < 0.05).
CONCLUSIONCME could not only prevent the development of liver cirrhosis induced by DMN in rats, but also effectively promote the reversion of already formed liver cirrhosis, having a favourable prospect of clinical application.
Alanine Transaminase ; genetics ; metabolism ; Animals ; Aspartate Aminotransferases ; genetics ; metabolism ; Biological Factors ; therapeutic use ; Cordyceps ; chemistry ; Dimethylnitrosamine ; adverse effects ; Humans ; Liver ; metabolism ; Liver Cirrhosis ; chemically induced ; drug therapy ; enzymology ; genetics ; Male ; Moths ; chemistry ; Mycelium ; chemistry ; Random Allocation ; Rats ; Rats, Wistar ; Treatment Outcome
6.Imaging diagnosis of skull epidermoid cyst:analysis of four cases
Xun-Ze SHEN ; Xiang-Yang GONG ; Xian-Yi CHEN ; Bo-Yin WANG ;
Chinese Journal of Radiology 2001;0(03):-
Objective To study the CT and MR imaging features of skull epidermoid cyst. Methods CT and MR findings of 4 cases of pathologically proved skull epidermoid cyst were analyzed and correlated with operative and pathologic reports.Results CT and MR appearances of skull epidermoid cyst were as follows:(1)crater-form or scalloping deossification with sclerotic border and fatty density focus was detected on CT.(2)The lesions were isointense to hypointense relative to normal white matter in T1-weighted image,prominent hyperintense in T_2-weighted image,mild to moderate hyperintense in diffusion-weighted imaging(DWI),and isointense to hypointense in apparent diffusion coefficient(ADC) map on MR.Proton MRS revealed lactate(Lac)peaks at 1.3 ppm and amino acids(AAs)at 0.9 ppm. (3)No enhancement was found in substance region of all tumors on both enhanced CT and enhanced MR examinations.Conclusion CT and MR appearances of skull epidermoid cyst have unique features which are very helpful in the diagnosis of skull epidermoid cyst.
7.The clinical efficacy evaluation of transcatheter hardening treatment for varicose veins of lower extremity
Jun-Hui CHEN ; Yi REN ; Ping HE ; Hong-Li XIONG ; Li WANG ; Xian-Bo ZHOU ;
Chinese Journal of Radiology 2001;0(08):-
Objective To explore the clinical efficacy and safety of transcatheter absolute ethanol injection treatment on varicose veins of lower extremity.Methods twenty-there patients with 25 varicose veins of lower extremity were treated by puncture of great saphenous vein above 1—2 cm of complicated inner ankle,perforating catheter to the point below the 3—4 cm of the conjunction of great saphenous vein and Femoral vein and pressing the conjunction of these two veins.Under the monitor of DSA,inject the absolute ethenal slowly while retrieve the catheter little by little(one limb with varicose veins injected total volume 15—20 ml),in the mean time,using contrast agent to monitor the level of embolism until the formation of total embolism in the all great saphenous veins.Results All the cases were retrospectively followed up with CDFI examination after 3—12 months of the surgery,No blood flow were seen in the 25 embolismic great saphenous vein.Clinical symptom were alleviated obviously after 2—3 weeks of treatment;varicose veins were collapse after 3 to 7 days.Two eases of leg ulceration were healed after 4 to 6 weeks of operation.20 limbs were found mild swelling in the 2 day after the surgery.However,all the cases were disappeared after 1 to 2 weeks;4 treated limbs developed delayed paresthesia in the 3 day after the surgery,and recovered totally in the 2 weeks.No complications of deep vein thrombosis,lung thrombosis etc al,were found after operation.Conclusions Using transcatheter injection of absolute ethanol to treat varicose veins of lower extremity has the advantage of less invasion,more safety and low appearance of complications.The short term efficacy is solid while the long term effect needs further evaluation.
9.Clinical application research: color doppler flow image and three dimensional color power angiography in the diagnosis of thyroid nodules
Hong, WANG ; Ying, WANG ; Hong-bo, WANG ; Xiao-lei, WANG ; Xiu-juan, HOU ; Xian-li, ZHOU ; Jia-wei, TIAN
Chinese Journal of Endemiology 2010;29(4):452-454
Objective To evaluate the clinical value of color doppler flow image (CDFI) and three-dimension color power angiography(3D-CPA) in the diagnosis of thyroid nodules. Methods A total of 62 pathologically confirmed thyroid nodules of 30 patients were analyzed. All the patients underwent ultrasound examination and operation in the Second Affiliated Hospital of Harbin Medical University between January, 2008 and May, 2009. Both CDFI and 3D-CPA were performed before the operation. All the nodules were divided into three groups including nodular goiters, thyroid adenomas and thyroid cancers according to the pathological results. The hemodynamic features and the vascular morphology characteristics of nodules in different groups were compared. Results 3D-CPA showed that blood vessels of nodular goiters commonly distributed surrounding the mass and the inner vessels were thin and regular, thyroid adenomas were bulb-shaped and netted structure, and malignant thyroid nodules displayed distorted and irregular distributed vessels. Peak systolic velocity (PSV)of the three groups were (39.43±11.17a), (46.39±12.98) and (65.17±9.23)cm/s, respectively. Resistance index(RI) of the three groups were (0.32±0.08), (0.41±0.06) and (0.69±0.07)cm/s, respectively. Both PSV and RI in malignant thyroid nodules were higher than in nodular goiters and in thyroid adenomas and the difference were statistical significant (all P < 0.05). The blood flow grade of malignant nodules was also higher in malignant nodules than in other two groups(χ2 = 17.11, 12.79, 23.05, 15.41, P< 0.01). Conclusions CDFI and 3D-CPA could visually demonstrate the characteristic and distribution of the inner and outer blood vessels, display the vessels structures, and they are benefit the differential diagnosis of thyroid nodules.
10.Research on the methods for titrating respiratory syncytial virus.
Xiao-Bo WANG ; Jin-Sheng HE ; Yuan-Hui FU ; Xian-Xian ZHENG ; Xuan FANG
Chinese Journal of Experimental and Clinical Virology 2010;24(2):147-149
OBJECTIVERespiratory syncytial virus (RSV) is the most common cause of lower respiratory infection in infants. It is very important to quantitative assay of RSV titer in the study on RSV pathogenesis, candidate vaccine and antiviral treatment. Therefore, we develop Real-time Quantitative PCR (Q-PCR) assay and enzyme immunospots (EIS) for titrating RSV and compare them with traditional 50% tissue culture infectious doses (TCID50).
METHODSQ-PCR, based upon the RSV-L genes, and EIS were utilized to titrate samples from RSV culture supernatants and RSV infected mouse lungs. Then, the results were compared with TCID50.
RESULTSFor the samples from RSV culture supernatants, the ratio of Q-PCR and EIS (plaque forming unit, pfu) was 10:1 and the ratio of EIS and TCID50 was 10:1 when TCID50 was converted as pfu. For the samples from RSV infected mouse lungs, the ratio of Q-PCR and EIS was 1000:1 and the ratio of EIS and TCID50 was 5:1.
CONCLUSIONWe have successfully established Q-PCR and EIS to titrate RSV and compared them with TCID50. We concluded EIS is a cost-effective method to titrate RSV.
Cell Line ; Humans ; Immunoenzyme Techniques ; Polymerase Chain Reaction ; Respiratory Syncytial Viruses ; genetics ; immunology