1.Inhibition of β1-integrin on apoptosis of rabbit corneal epithelial cells
You-Dong, WANG ; Qi, SUN ; Bing-Yang, LIU ; Jin-Song, ZHANG
International Eye Science 2008;8(8):1495-1499
· AIM: To investigate the effect of β1-integrin overexpression on the apoptosis of rabbit corneal epithelial cells and the related mechanism. · METHODS: The plasmid expressing β1-integrin-GFP fusion protein was constructed by polymerase chain reaction (PCR), and this plasmid (β1 group) or the empty vector (mock group) was transfected into rabbit corneal epithelial cells, respectively. The expression of β1-integrin-GFP fusion gene was confirmed by reverse transcription-polymerase chain reaction (RT-PCR) and Western blot. The adhesion of transfected cells to extracellular matrix (ECM) proteins was determined by adhesion assay. The apoptosis of rabbit corneal epithelial cells was assayed by Hoechst 33342 staining and DNA ladder. The phosphorylation of mitogen-activated protein (MAP) kinase was examined by Western blot. · RESULTS: Rabbit corneal epithelial cells overexpressing β1 -integrin-GFP fusion gene were successfully established. Compared with mock group, β1-integrin transfection significantly promoted the adhesive of rabbit corneal epithelial cells to ECM proteins such as laminin, fibronectin, collagen Ⅰ and collagen Ⅳ. Β1-integrin overexpression inhibited apoptosis and induced MAP kinase phosphorylation in rabbit corneal epithelial cells (P<0.05).· CONCLUSION: These data suggest that overexpression of β1-integrin confers resistance to apoptosis in rabbit corneal epithelial cells, and MAP kinase pathway may play an important role in this process.
2.Synergism of an antisense oligodeoxynucleotides targeted to hTERT in combination with chemotherapeutic drugs on inhibiting the proliferation of HepG2 cells.
Ying YANG ; Qing-you DU ; Sheng-qi WANG
Chinese Journal of Hepatology 2003;11(12):719-721
OBJECTIVETo investigate the effect of a phosphorothioate antisense oligodeoxynucleotide "ASOND" combined with cis-Diamminedichloroplatinum (DDP), 5-fluorouracil (5-FU) and adriamycin (ADM) respectively on inhibiting the proliferation of HepG2 cells.
METHODSA phosphorothioate antisense oligodeoxynucleotide (5'-ACTCACTCAGG CCTCAGACT-3') targeted to human telomerase reverse transcriptase (hTERT) mRNA, which named cantide, was synthesized. ASODN was transfected into HepG2 by lipofectin. And cell growth activity was evaluated by MTT assay. SAS software and Jin Zhengjun Method were used to evaluate the interaction of ASODN and these chemotherapeutic drugs.
RESULTSCombination treatments with 0.1micromol/L ASODN reduced the IC50 of DDP, 5-FU and ADM from 1.07, 4.15 and 0.29microg/ml to 0.25, 1.52 and 0.12microg/ml respectively. The inhibitory ability of combination treatments on HepG2 cells was higher than that of these drugs alone (F=66.92, 25.96, 8.56, P<0.001). And synergism (Q>or=1.15) was observed at the lower concentration of DDP ( CONCLUSIONASODN may enhance therapeutic effectiveness of chemotherapeutic drugs in human hepatocellular carcinoma cells.
Antineoplastic Agents
;
administration & dosage
;
Cell Line, Tumor
;
Cisplatin
;
administration & dosage
;
DNA-Binding Proteins
;
Doxorubicin
;
administration & dosage
;
Drug Synergism
;
Fluorouracil
;
administration & dosage
;
Humans
;
Liver Neoplasms
;
drug therapy
;
Oligodeoxyribonucleotides, Antisense
;
administration & dosage
;
Telomerase
;
antagonists & inhibitors
;
genetics
3.Progress in research of the structural optimization of natural product-like Garcinia caged xanthones.
Yan-Yan WANG ; Xiao-Jin ZHANG ; Ying-Rui YANG ; Hao-Peng SUN ; Qi-Dong YOU
Acta Pharmaceutica Sinica 2014;49(3):293-302
Designing of natural product-like compounds using natural products as template structures is an important strategy for the discovery of new drugs. Gambogic acid (GA), which is a Garcinia natural product with a unique caged xanthone scaffold, inhibits potent antitumor activity both in vitro and in vivo. This review summarized the researches on the identification of the antitumor pharmacophore of GA, and the design, structural optimization and structure-activity relationship (SAR) of natural product-like caged xanthones based on it.
Antineoplastic Agents
;
chemical synthesis
;
chemistry
;
pharmacology
;
Biological Products
;
chemical synthesis
;
chemistry
;
isolation & purification
;
pharmacology
;
Cell Line, Tumor
;
Cell Proliferation
;
drug effects
;
Drug Screening Assays, Antitumor
;
Garcinia
;
chemistry
;
Humans
;
Molecular Structure
;
Structure-Activity Relationship
;
Xanthones
;
chemical synthesis
;
chemistry
;
isolation & purification
;
pharmacology
4.KAP of residents on schistosomiasis control in transmission-interrupted areas
Genquan QI ; Guanghan HU ; Rensheng YANG ; Changzheng YOU ; Ju ZHANG ; Jun GE
Chinese Journal of Schistosomiasis Control 1989;0(01):-
Objective To investigate knowledge, attitude and practice (KAP) on schistosomiasis control in transmission-interrupted areas in order to provide basis for making out intervention strategies of preventing re-epidemic of schistosomiasis. Methods A questionnaire survey was carried out for residents’ KAP on schistosomiasis control in the transmission-interrupted areas. A total of 608 residents were surveyed. Results The residents’ understanding rates of each item of schistosomiasis control were under 25.00% without exception. Residents refusing schistosomiasis examination, never surveying snails and never reporting snails accounted for 52.30%, 95.23% and 97.86% respectively. Conclusions Residents treat schistosomiasis control with indifference in transmission-interrupted areas. Therefore, intervention strategies of pertinent health education should be adopted to improve residents’ compliance to schistosomiasis examination and snail survey and report, and to prevent schistosomiasis re-epidemic.
5.Thirty-two cases of blow-out fracture with orbital floor repaired by auto-cranial pedicle flap
Zhong-You ZHOU ; Qi ZHU ; Xin-Ji YANG ; Wen GOU ; Xin-Li JIANG ; Zhi-Peng YAN ;
Ophthalmology in China 2006;0(06):-
2cm~2.Conclusions The auto-cranial pedicle flap via endonasal repairing blow-out fractures of or- bital inferior wails is an effective technique.The results are good for improving eye movement especially for fracture ranged≤2cm~2. (Ophthalmol CHN,2007,16:388-390)
6.THE DEVELOPMENT AND APPLICATION OF YUNNAN STRAIN INFORMATION SYSTEM
Bin ZHOU ; Liyuang YANG ; Zhiying LI ; Shaolan LI ; You CHEN ; Qi ZHANG ;
Microbiology 1992;0(04):-
Yunnan Strain Information System has been developed by using the Programming Lan guage and Database Engine It includes information of over 10,000 strains that are stored in Yunnan University Institute of Microbiology Strain Library The S ystem makes a convenience for management of Strain Library and supply i mportant information for study these
7.Treatment of acute radiation pneumonia with Qingfei Huatan Quyu method.
Sheng-You LIN ; Xiu-Hua HAN ; Qi-Chu YANG
Chinese Journal of Integrated Traditional and Western Medicine 2008;28(5):414-417
OBJECTIVETo observe the therapeutic effect of Qingfei Huatan Quyu method (QHQ, a Chinese medicinal therapy for clearing Fei-heat and dissolving phlegm-stasis) combined with hormone-antibiotic therapy (HAT) on radiation pneumonia (RP).
METHODSEighty-one patients with RP were randomized into two groups, 41 patients in the control group and 40 in the treatment group were treated with HAT alone and HAT combined with QHQ respectively for 21 days. The severity of RP was evaluated before and after treatment according to the criteria of the radiation therapy oncology group. The effect on TCM symptoms and chest roentgenogram, as well as on plasma levels of interleukin-6 ( IL-6) and transform growth factor-beta (TGF-beta) were detected.
RESULTSAfter treatment, number of patients with RP graded as 0, 1, 2, 3, and 4 in the treatment group was 23, 10, 4, 2, and 1, respectively, while in the control group, 14, 9, 11, 4, and 3, respectively. The combined therapy showed effects in improving RP grading (P <0.01) and TCM syndromes were superior to those of HAT respectively (P < 0.05). Besides, levels of IL-6 and TGF-beta were lowered after treatment in the treatment group, showing a significant difference to those in the control group (P <0.05).
CONCLUSIONQHQ combined with HAT has a definite therapeutic effect on RP. It could efficiently decrease the plasma levels of IL-6 and TGF-beta in patients with RP.
Anti-Bacterial Agents ; therapeutic use ; Drug Therapy, Combination ; Drugs, Chinese Herbal ; therapeutic use ; Humans ; Interleukin-6 ; blood ; Medicine, Chinese Traditional ; Radiation Pneumonitis ; drug therapy ; Transforming Growth Factor beta ; blood
8.Co-load of silybin and doxorubicin by MoS2 nanosheets for synergetic chemotherapy and photothermal therapy of lung cancer
Hong CHEN ; Min GUO ; Zhi-huai CHEN ; Xin-qi WEI ; You-rui YANG ; Jian LIU ; Wei XU
Acta Pharmaceutica Sinica 2023;58(3):560-570
The active ingredient of traditional Chinese medicine, silybin (SBN), can inhibit the proliferation of cancer cells and enhance the anticancer effect of doxorubicin (DOX). However, due to non-targeting and short half-life of SBN and DOX, as well as different administration routes and pharmacokinetic processes, this combination drug cannot act on the tumor in the set order, seriously eliminating the synergistic effect between them and limiting the effect
9.Design, synthesis, and biological activities of histone deacetylase inhibitors with diketo ester as zinc binding group.
Hui LU ; Hong SU ; Bo YANG ; Qi-Dong YOU
Acta Pharmaceutica Sinica 2011;46(3):293-298
Histone deacetylases (HDACs) inhibition causes hyperacetylation of histones leading to growth arrest, differentiation and apoptosis of tumor cells, representing a new strategy in cancer therapy. Many of previously reported HDACs inhibitors are hydroxamic acid derivatives, which could chelate the zinc ion in the active site in a bidentate fashion. However, hydroxamic acids occasionally have produced problems such as poor pharmacokinetics, severe toxicity and low selectivity. Herein we describe the identification of a new series of non-hydroxamate HDACs inhibitors bearing diketo ester moieties as zinc binding group. HDACs inhibition assay and antiproliferation assays in vitro against multiple cancer cell lines were used for evaluation. These compounds displayed low antiproliferative activity against solid tumor cells, while good antiproliferative activity against human leukemic monocyte lymphoma cell line U937. Compound CPUYS707 is the best with GI50 value of 0.31 micromol x L(-1) against U937 cells, which is more potent than SAHA and MS-275. HDACs inhibition activity of these compounds is lower than that expected, further evaluation is needed.
Antineoplastic Agents
;
chemical synthesis
;
chemistry
;
pharmacology
;
Benzamides
;
pharmacology
;
Biphenyl Compounds
;
chemical synthesis
;
chemistry
;
pharmacology
;
Cell Line, Tumor
;
Cell Proliferation
;
drug effects
;
Drug Design
;
Esters
;
chemistry
;
Histone Deacetylase Inhibitors
;
chemical synthesis
;
chemistry
;
pharmacology
;
Histone Deacetylases
;
metabolism
;
Humans
;
Hydroxamic Acids
;
pharmacology
;
Molecular Structure
;
Pyridines
;
pharmacology
;
U937 Cells
;
drug effects
;
Zinc
;
chemistry
10.The research practice of anti-arrhythmic agents targeting on potassium ion channel.
Qian YANG ; Xiao-Jian WANG ; Yi-Qun TANG ; Qi-Dong YOU
Acta Pharmaceutica Sinica 2011;46(1):12-18
Due to the complicated pathogenesis of cardiac arrhythmia, the safe and effective therapeutic strategies for cardiac arrhythmia remain an urgent medical problems in the recent years. In this paper, we introduced the research practice of anti-arrhythmic agents targeting on potassium ion channel. The research progress of anti-arrhythmic agents in up-to-date literatures were also reviewed and prospected.
Amiodarone
;
analogs & derivatives
;
chemistry
;
pharmacology
;
therapeutic use
;
Animals
;
Anti-Arrhythmia Agents
;
chemistry
;
pharmacology
;
therapeutic use
;
Arrhythmias, Cardiac
;
drug therapy
;
physiopathology
;
Humans
;
Hydantoins
;
Imidazolidines
;
chemistry
;
pharmacology
;
therapeutic use
;
Molecular Structure
;
Piperazines
;
chemistry
;
pharmacology
;
therapeutic use
;
Potassium Channel Blockers
;
pharmacology
;
therapeutic use
;
Potassium Channels
;
drug effects