1.Drug resistance to target therapy in colorectal cancer:research advances
Ke XU ; Guojiang CHEN ; Hui PENG
Journal of International Pharmaceutical Research 2017;44(5):402-408
Colorectal cancer(CRC)ranks the third in incidence and mortality rate among human tumors. Tumor relapse,me?tastasis and drug resistance remain the main obstacle to the success of CRC treatments. Compared to traditional chemotherapy ,target therapy seems to treat tumors in more precise and rational fashion with good response and often less toxic side-effect. Although target agents provide hope for more effective therapy,recent clinical studies have shown only modest benefit from target therapy similar to tra?ditional chemotherapy. Primary and secondary resistance to target agents is still observed and contributes to CRC treatment failure. The review summarizes research progress in the mechanism of drug resistance to target therapy in CRC treatment.
2.Lung metastases of colorectal cancer boosted by bevacizumab in mice and possible mechanism
Yaqiong CHEN ; Yuanyuan LI ; Zhongling LYU ; Guojiang CHEN ; Hui PENG
Chinese Journal of Pharmacology and Toxicology 2016;30(5):564-568
OBJECTIVE To investigate the effect of bevacizumab ,an anti-human vascular endothelial growth factor monoclonal antibody,on pulmonary dissemination of colorectal cancer. METHODS A metastatic colorectal cancer mouse model was established. Mice were randomly divided into two groups(n=8). The mice in experimental group were administered ip with bevacizumab at the dosage of 5 mg · kg-1,and those in control group were given isotype IgG at the same dosage. The antibodies were administered on 2 d before initiation of model establishment and 2 d after that,then once every 5 d for 4 weeks,for a total of 7 times. Liver and lung metastases were determined by histopathological examination. The chemokine receptor C-X-C receptor 4(CXCR4)and its ligand C-X-C ligand 12(CXCL12)mRNA expression in the lung were detected by quantitative RT-PCR. Human colon cancer cells HCT116 were treated with bevacizumab(5 mg·L-1)for 24 h. The expression levels of vascular endothelial growth factor receptor 1(VEGFR1)and CXCR4/7 protein as well as CXCR3/4/7 mRNA were examined by Western blotting and quantitative RT-PCR respectively. RESULTS The number of mice(2/8) with liver metastases was reduced,while the number of mice(8/8) with lung metastases increased in experimental group compared with isotype IgG-treated group(6/8 and 2/8 respectively,P<0.05). The mRNA expression level of CXCR4 and CXCL12 in lung tissue was significantly up-regulated in bevacizumab-treated group com?pared with control group(P<0.05). The mRNA and protein expression level of CXCR4 and CXCR7 was dramatically increased in HCT116 cells treated with bevacizumab(P<0.05). CONCLUSION Bevacizumab can potentially promote lung metastases of colorectal cancer,which may be related to up-regulation of CXCR4 and CXCL12 expression.
3.1H NMR based metabonomics study on the antidepressant effect of genipin in rat hippocampus.
Guojiang PENG ; Biyun SHI ; Junsheng TIAN ; Shan GAO ; Xuemei QIN
Acta Pharmaceutica Sinica 2014;49(2):209-16
The purpose of this study is to explore depression metabolic markers in rat hippocampus and to investigate the anti-depressant effect of genipin and its mechanisms using nuclear magnetic resonance (NMR) metabonomics. Chronic unpredictable mild stress (CUMS) procedure was conducted to establish the depressive rat model. At the beginning of the third week, genipin low dose (25 mg x kg(-1)), middle dose (50 mg x kg(-1)), high dose (100 mg x kg(-1)), and venlafaxine (50 mg x kg(-1)) were given to the CUMS rats separately once daily for two weeks except control and model groups. Rat hippocampus was analyzed by 1H NMR based metabonomics after drug administration for 2 weeks. Significant differences in the metabolic profile of rat hippocampus of the CUMS treated group and the control group were observed with metabolic effects of CUMS including decreasing in glycine and N-acetylaspartate, increasing in inositol, glutamate, lactate, glutamine, taurine and alanine. Genipin showed ideal antidepressive effects at a dose of 50 mg x kg(-1) in rats, decrease of inositol, glutamate, lactate, alanine were observed, while glycine and N-acetylaspartate were increased. Important influence has been found on normal nervous system function of these significant changed metabolites, which suggests that the antidepressant effect of genipin may be played by enhancing the activity of neurons in hippocampus, repairing and improving the function of the neuron. The metabonomics approach is an effective tool for the investigation of the anti-depressant effect and pharmacologic mechanisms of genipin.
4.Investigating the killing effect of photodynamic therapy induced by different photosensitizers on human leukemia cell in vitro
Hongli CHEN ; Yingxin LI ; Huijuan YIN ; Yuxiao CUI ; Liqing ZHENG ; Peng LI ; Guojiang GAO
International Journal of Biomedical Engineering 2012;35(4):197-200
Objective To investigate and compare the killing effect of photodynamic therapy (PDT)induced by hematoporphyrin derivative (HpD),hematoporphyrin monomethyl ether (HMME) and photocarcinorin (PsD007) on human leukemia cells K562 in vitro.Methods Human leukemia cells were cultured with serial concentrations of photosensitizers followed by irradiation of different dosage of laser light,then MTT colorimetric assay was applied to measure the relative survival rate of PDT for the cells.Results Significant difference in the inhibitory between the PDT group and control group was observed (P<0.05).The survival rate of PDT for the cells elevated along with the increase in the concentration of sensitizer and dose of laser light.When the photosensitizer concentration was bigger (25 μg/ml) or the energy density was bigger (7.2 J/cm2),the effect of PsD007 was better than HMME,and they were significantly better than HpD (P<0.05).Conclusion PDT has significant killing effect on human leukemia cells K562,and its relative inhibitory rate appears to be correlated with the dose of sensitizer and laser light irritation.The effect of PDT is related to the photosensitizers.The effect of HpD-PDT is not as effective as PsD007 and HMME.On the conditions of higher energy density and larger photosensitizer concentration,the effect of PsD007-PDT is better than HMME-PDT.
5.Medication Compliance Investigation and Pharmaceutical Care for 50 Cases of Hypertension
Jianjun ZHOU ; Guojiang PENG ; Yi CAO ; Shiyun WANG ; Xiaojin HUANG ; Pingmei DENG
China Pharmacist 2017;20(8):1414-1416
Objective: To understand the medication compliance of inpatients with essential hypertension, analyze the influencing factors in medication compliance of the patients and perform the targeted medication education and pharmaceutical care.Methods: Medication education and guide were conducted in 50 cases of patients with essential hypertension based on the main contents in guidelines for prevention of hypertension.Every patient completed regular follow-ups in two months after being recruited.The relevant information about the treatment and medication were collected and analyzed.Results: Through the medication education and pharmaceutical care, the patients had a better understanding on the relevant knowledge of hypertension, rational drug use and treatment.Among the 50 patients, the percentage of completely following the doctor's advice on the hypertension medication was 86%, that of quitting smoking and limiting alcohol was 82%, and that of optimized life way was 78%, and totally 82% of the patients effectively controlled blood pressure or improved markedly when compared with the situation on admission.Conclusion: Medication education and pharmaceutical care conducted by clinical pharmacists is very important for the patients with high blood pressure.It can help patients build a good lifestyle or improve the quality of life by improving the medication compliance of patients, alleviating complications and reducing adverse drug reactions.
6.The effect of surface free energy parameters of diamond-like carbon films deposited on medical polyethylene terephthalate on bacterial adhesion.
Jin WANG ; Changjiang PAN ; Peng LI ; Yongxiang LENG ; Junying CHEN ; Guojiang WAN ; Ping YANG ; Hong SUN ; Nan HUANG
Journal of Biomedical Engineering 2006;23(2):342-345
Diamond-like carbon (DLC) films were deposited by acetylene plasma immersion ion implantation-deposition (PIII-D) on biomedical polyethylene terephthalate (PET). The capacities of Staphylococcus aureus (SA), Staphylococcus epidermidis (SE), Escherichia coli (EC), Pseudomonas aeruginosa (PA) and Candida albicans (CA) for adhesion to PETs are quantitatively determined by the plate counting and Gamma-ray counting of 125I radio labeled bacteria in vitro. The results indicate that the capacities of five types of bacteria for adhesion to PETs are all suppressed by C2H2 PIII-D (P<0.05). The surface energy components of the various substrates and bacteria are calculated based on measurements in water, formamide and diiodomethane and Lifshitz-van del Waals/acid-base approach (LW-AB). The surface free energies obtained are used to calculate the interfacial free energies of adhesion (deltaF(adh)) of five kinds of bacteria on various substrates, and the results show that it is energetically unfavorable for bacterial adhesion to the DLC films already deposited on PET by C2H2 PIII-D.
Bacterial Adhesion
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drug effects
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physiology
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Carbon
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chemistry
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Coated Materials, Biocompatible
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chemistry
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Diamond
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chemistry
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Escherichia coli
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drug effects
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Heart Valve Prosthesis
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microbiology
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Materials Testing
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Polyethylene Terephthalates
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chemistry
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Staphylococcus aureus
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drug effects
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Staphylococcus epidermidis
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drug effects
7.Deep learning-based recognition of stained tongue coating images
ZHONG Liqin ; XIN Guojiang ; PENG Qinghua ; CUI Ji ; ZHU Lei ; LIANG Hao
Digital Chinese Medicine 2024;7(2):129-136
Objective:
To build a dataset encompassing a large number of stained tongue coating images and process it using deep learning to automatically recognize stained tongue coating images.
Methods:
A total of 1 001 images of stained tongue coating from healthy students at Hunan University of Chinese Medicine and 1 007 images of pathological (non-stained) tongue coating from hospitalized patients at The First Hospital of Hunan University of Chinese Medicine with lung cancer, diabetes, and hypertension were collected. The tongue images were randomized into the training, validation, and testing datasets in a 7 : 2 : 1 ratio. A deep learning model was constructed using the ResNet50 for recognizing stained tongue coating in the training and validation datasets. The training period was 90 epochs. The model’s performance was evaluated by its accuracy, loss curve, recall, F1 score, confusion matrix, receiver operating characteristic (ROC) curve, and precision-recall (PR) curve in the tasks of predicting stained tongue coating images in the testing dataset. The accuracy of the deep learning model was compared with that of attending physicians of traditional Chinese medicine (TCM).
Result:
The training results showed that after 90 epochs, the model presented an excellent classification performance. The loss curve and accuracy were stable, showing no signs of overfitting. The model achieved an accuracy, recall, and F1 score of 92%, 91%, and 92%, respectively. The confusion matrix revealed an accuracy of 92% for the model and 69% for TCM practitioners. The areas under the ROC and PR curves were 0.97 and 0.95, respectively.
Conclusion
The deep learning model constructed using ResNet50 can effectively recognize stained coating images with greater accuracy than visual inspection of TCM practitioners. This model has the potential to assist doctors in identifying false tongue coating and preventing misdiagnosis.