1.Clinical efficacy of anti-helicobacter pylori in treatment of type 2 diabetes mellitus with helicobacter pylori infection
Hongwei KONG ; Jing HUANG ; Yingli SHUAI
Clinical Medicine of China 2017;33(6):523-526
Objective To explore the clinical efficacy of anti-helicobacter pylori (HP) treatment on patients with type 2 diabetes mellitus and HP infection.Methods A total of 112 type 2 Diabetes patients were diagnosed with HP infection in Combine Traditional Chinese and Western Medicine Hospital of Taizhou from April 2012 to June 2016.These patients were divided into control and treatment group based on the preprandial blood glucose averages from lower to higher hierarchy.Thus,there were 56 patients in each of the two groups.The control group was given Motilium and Talcid for gastric symptoms in addition to anti-diabetes treatment,while the treatment was administered the same treatments as well as the quadruple anti-HP therapy (omeprazole,amoxicillin,clarithromycin and colloidal-bismuth-subcitrate,with Talcid stopped while colloidal-bismuth-subcitrate was administered).The anti-HP lasted for 14 days.The two groups were compared the gastric symptoms,the blood glucose levels,and the HbA1c one month after treatment.Half a year and one year post treatment,the two groups were compared the gastric mucus signs under gastroscopy.Results The improvement rates after treatment with the treatment group in abdominal pain,bloating,regurgitation,belching and diarrhea/constipation were 88.5% (23/26),83.3% (25/30),74.1% (20/27),83.9% (26/31),82.6% (19/23),respectively,and with the control group being 29.2%(7/24),32.1%(9/28),28%(7/25),30.3%(10/33),18.2% (4/22),respectively.The differences between the two groups were significant (x2=8.06,6.62,3.92,7.65,6.66,P<0.05 or P<0.01).The control group did not show significant changes in preprandial glucose levels,the glucose levels two hours post meals and the HbA1c(P>0.05) while the treatment group showed statistically significant changes(P<0.05 or P<0.01).The differences in the three indicators after treatment between the two groups were significant (t =4.07,7.85,4.16,P< 0.05).The Gastric mucus signs under gastroscopy showed improvements in both groups after treatment.The improvement rates with the treatment group were 86.2%(25/29),86.7% (13/15),77.8% (14/18),72.7% (8/11) respectively,with the control group being 36% (9/16),27.3% (3/11),13.3% (2/15),14.3% (1/7),respectively.The differences between the two groups were significant (x2 =6.71,4.12,4.38,3.85,P < 0.05 or P< 0.01).The effectiveness rate,which was based on combined improvements in gastric symptoms,glucose levels and gastric mucus signs,was 76.8% with the treatment group and 32.1% with the control group.The difference was statistically significant (x2 =6.78,P<0.01).Conclusion Anti-HP treatment can relieve the gastric symptoms,stabilize the glucose levels,and help to reverse the changed gastric mucus.All these can reduce the complications of the diabetes and improve the prognosis of the patients.
2.Efficacy and mechanism of FW-04-806 against HER2-positive gastric cancer cell lines
Min ZHANG ; Pinrong CAO ; Qundan WU ; Yingli KONG ; Lihong CHEN ; Yanmei LUO ; Wei HUANG ; Jianhua XU ; Min YE
Chinese Pharmacological Bulletin 2014;(11):1513-1520
Aim To investigate the efficacy and mech-anism of FW-04-806 against HER2-positive gastric cancer cell lines,and the combination effect of FW-04-806 with lapatinib. Methods MTT assay was used to assess cell proliferous inhibition of FW-04-806 . The in-hibitory effect of colony formation was tested by colony formation. The protein expression, apoptotic induction and cell cycle arrest were detected by flow cytometry. Co-immunoprecipitation was used to investigate protein-protein interactions. The expression change of proteins was showed by immunohistochemistry. Western blot was applied to reveal the protein expression of related pro-liferous and apoptotic signaling pathway. The tumor growth inhibition was evaluated in tumor xenograft model. Results FW-04-806 obviously inhibited cell proliferation and colony formation in HER2 positive gastric cancer cell lines NCI-N87, OE19, with IC50 of (24. 17 ± 0. 02 ) , ( 29. 61 ± 0. 03 ) μmol · L-1 , re-spectively;FW-04-806 induced G2-M arrest and apop-tosis in a dose-dependent manner;200 mg · kg-1 of FW-04-806 showed tumor growth inhibition of 48. 0%( P < 0. 01 ) . In addition, FW-04-806 dissociated Hsp90/CDC37 complex, followed by degradation of HER2 and Akt,inhibiting the phosporylation of HER2, Akt and ERK, and increasing expression of apoptotic proteins,such as cleaved caspase-3 and cleaved parp. Furthermore,the combination of FW-04-806 with lapa-tinib in vitro was synergistic in NCI-N87 , which en-hanced the inhibition of cell proliferation and increased apoptotic rates. Conclusions FW-04-806 shows po-tent efficacy against HER2-positive gastric cancer cell lines in vitro and in vivo;FW-04-806 is synergistic with lapatinib.
3.The Hsp90 inhibitor FW-04-806 suppresses Bcr/Abl-mediated growth of leukemia cells by inhibiting proliferation and inducing apoptosis.
Yingli KONG ; Wei HUANG ; Pinrong CAO ; Lihong CHEN ; Yanmei LUO ; Bingying SHE ; Jianhua XU ; Min YE
Chinese Journal of Oncology 2015;37(12):890-898
OBJECTIVETo investigate the antitumor efficacy and mechanism of HSP90 inhibitor FW-04-806 against Bcr/Abl(+) leukemia K562 and HL60 cells and their mechanisms of action.
METHODSMTT assay was used to assess the proliferation-inhibiting effect of FW-04-806. Cell cycle was analyzed with propidium iodide by flow cytometry. Cell apoptosis was determined using the FITC mV apoptosis detection kit. Western blot was applied to reveal the protein expression of related proliferative and apoptotic signaling pathways. The changes of mitochondrial membrane potential were detected by flow cytometry. Protein-protein interactions was shown by co-immunoprecipitation. The level of mRNA was assessed by real-time RT-PCR.
RESULTSFW-04-806 obviously inhibited cell proliferation in the HL60, K562 and HL60/Bcr-Abl cell lines, with an IC50 of (30.89 ± 0.12) µmol/L, (9.76 ± 0.19) µmol/L and (8.03 ± 0.26) µmol/L, respectively (P<0.001). Compared with the vehicle group, the two increasing doses of FW-04-806 showed inhibition of tumor growth at a rate of (17.40 ± 0.34)% and (34.33 ± 5.00)%, respectively, in the K562 cell line groups (P=0.003), and (18.90 ± 1.45)% and (35.60 ± 3.55)% (P=0.001) in the HL60/Bcr-Abl cell line groups. FW-04-806 dissociated Hsp90/Cdc37 chaperon/co-chaperon complex, followed by degradation of the Hsp90 proteins through proteasome pathway without affecting mRNA expression. FW-04-806 induced apoptosis and led to G2/M arrest.
CONCLUSIONOur findings indicate that FW-04-806 displays potential antitumor effect by suppressing the proliferation and apoptosis in Bcr/Abl(+) leukemia cells in vivo.
Apoptosis ; drug effects ; Cell Cycle ; Cell Proliferation ; drug effects ; Fusion Proteins, bcr-abl ; HL-60 Cells ; HSP90 Heat-Shock Proteins ; antagonists & inhibitors ; Humans ; K562 Cells ; Leukemia ; drug therapy ; metabolism ; pathology ; Membrane Potential, Mitochondrial ; Oxazoles ; pharmacology ; RNA, Messenger ; metabolism ; Signal Transduction
4.Optimization of processing technology and quality characterization of wine-steamed Taxillus chinensis
Huifeng LI ; Hui LI ; Shuang MENG ; Xiaotao WANG ; Zhiwei WANG ; Xiangpeng KONG ; Haixian ZHAN ; Yingli WANG
China Pharmacy 2024;35(11):1320-1326
OBJECTIVE To optimize the steaming and processing technology of wine-steamed Taxillus chinensis, and to characterize its quality. METHODS Using the content of avicularin, quercitrin, quercetin and appearance traits as evaluation indicators, the analytic hierarchy process (AHP)-entropy weight method was used to determine the weights of each indicator, and the comprehensive scores of those indicators were used as response values. Box-Behnken response surface method was used to investigate the effects of solid-liquid ratio (g/mL), soaking time, and steaming time on the processing technology of wine-steamed T. chinensis, optimize the best processing technology, and verify it. Fifteen batches of T. chinensis decoction pieces from different origins were used to prepare wine-steamed T. chinensis using the best processing technology, and their qualities were characterized. RESULTS The optimal processing technology for wine-steamed T. chinensis was to take 100 g of T. chinensis decoction pieces, add 20 mL of yellow wine, seal and moisten for 2 h, steam at normal pressure for 1 h, take out and dry at 50 ℃. The surface of wine-steamed T. chinensis prepared by the optimal processing technology was reddish brown or brownish, and its powder was dark brown, with a hard or brittle texture that was easy to break, and had a slight aroma of alcohol, and an astringent taste. Results of microscopic and thin-layer identification for the stem cross-section of wine-steamed T. chinensis were the same as those of raw T. chinensis. The contents of moisture, total ash and acid-insoluble ash were 3.92%-8.75%, 2.27%-5.08%, and 0.19%-0.82%, respectively; the contents of water-soluble extract were 11.28%-18.56%, and the contents of alcohol-soluble extract were 3.36%-8.58%; the contents of avicularin, quercitrin, and quercetin were 0.22-1.64, 0.26-2.45, and 0.01-0.38 mg/g, respectively. CONCLUSIONS This study successfully optimized the processing technology of wine-steamed T. chinensis and preliminarily characterized its quality, which can provide reference for the standardized processing and establishment of quality standards for wine-steamed T. chinensis decoction mail:wyl@sxtcm.edu.cn pieces.
5.Optimization of processing technology and quality characterization of wine-steamed Taxillus chinensis
Huifeng LI ; Hui LI ; Shuang MENG ; Xiaotao WANG ; Zhiwei WANG ; Xiangpeng KONG ; Haixian ZHAN ; Yingli WANG
China Pharmacy 2024;35(11):1320-1326
OBJECTIVE To optimize the steaming and processing technology of wine-steamed Taxillus chinensis, and to characterize its quality. METHODS Using the content of avicularin, quercitrin, quercetin and appearance traits as evaluation indicators, the analytic hierarchy process (AHP)-entropy weight method was used to determine the weights of each indicator, and the comprehensive scores of those indicators were used as response values. Box-Behnken response surface method was used to investigate the effects of solid-liquid ratio (g/mL), soaking time, and steaming time on the processing technology of wine-steamed T. chinensis, optimize the best processing technology, and verify it. Fifteen batches of T. chinensis decoction pieces from different origins were used to prepare wine-steamed T. chinensis using the best processing technology, and their qualities were characterized. RESULTS The optimal processing technology for wine-steamed T. chinensis was to take 100 g of T. chinensis decoction pieces, add 20 mL of yellow wine, seal and moisten for 2 h, steam at normal pressure for 1 h, take out and dry at 50 ℃. The surface of wine-steamed T. chinensis prepared by the optimal processing technology was reddish brown or brownish, and its powder was dark brown, with a hard or brittle texture that was easy to break, and had a slight aroma of alcohol, and an astringent taste. Results of microscopic and thin-layer identification for the stem cross-section of wine-steamed T. chinensis were the same as those of raw T. chinensis. The contents of moisture, total ash and acid-insoluble ash were 3.92%-8.75%, 2.27%-5.08%, and 0.19%-0.82%, respectively; the contents of water-soluble extract were 11.28%-18.56%, and the contents of alcohol-soluble extract were 3.36%-8.58%; the contents of avicularin, quercitrin, and quercetin were 0.22-1.64, 0.26-2.45, and 0.01-0.38 mg/g, respectively. CONCLUSIONS This study successfully optimized the processing technology of wine-steamed T. chinensis and preliminarily characterized its quality, which can provide reference for the standardized processing and establishment of quality standards for wine-steamed T. chinensis decoction mail:wyl@sxtcm.edu.cn pieces.