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1.
Bioorg Chem ; 128: 106055, 2022 11.
Article in English | MEDLINE | ID: mdl-35905693

ABSTRACT

In this study, we constructed and displayed a ratiometric fluorescent probe JQ-2 for detecting ONOO-. The probe JQ-2 showed a ratiometric signal for visualizing ONOO- with a rapid response and high selectivity over a panel of biological analytes. Moreover, the JQ-2 has near-infrared emission (657 nm), which provides an excellent basis for the practical application in biological systems. The probe JQ-2 possessed low cytotoxicity and excellent cell membrane permeability, which can specifically visualize the exogenous and endogenous ONOO- in vitro and vivo by emission in two channels. Meanwhile, JQ-2 can be used for diagnosing drug-induced liver injury by visualizing and monitoring the fluctuations of endogenous ONOO-. Therefore, JQ-2 provided a potential tool for precisely detecting the fluctuation of ONOO- in biological systems to understand physiological and pathological process.


Subject(s)
Chemical and Drug Induced Liver Injury , Peroxynitrous Acid , Fluorescent Dyes , Humans , Optical Imaging
2.
J Pharmacol Sci ; 143(3): 238-241, 2020 Jul.
Article in English | MEDLINE | ID: mdl-32265105

ABSTRACT

Resveratrol has been extensively studied as the anti-cancer agent. A variety of resveratrol analogues have been developed with structural modification to improve its bioactivity. In this work, resveratrol analogues, compound 1-4, were designed and synthesized with the Stille-Heck reaction. These results showed compound 1-4 had better anticancer effect than that of parent resveratrol. Especially compound 1 ((E)-4,4'-(ethene-1,2-diyl)bis(3-methylphenol)) displayed the excellent cytotoxicity and high selectivity. The mechanism research indicated compound 1 inhibited cell proliferation by binary paths of cell cycle arrest in S phase regulated by cyclin A1/A2 and apoptosis induction mediated by Bax/Bcl2 in a prooxidant manner.


Subject(s)
Antineoplastic Agents, Phytogenic/pharmacology , Apoptosis/drug effects , Cell Cycle Checkpoints/drug effects , Neoplasms/pathology , Resveratrol/analogs & derivatives , Resveratrol/pharmacology , Apoptosis/genetics , Cell Proliferation/drug effects , Cell Proliferation/genetics , HeLa Cells , Humans , MCF-7 Cells , Organic Chemistry Phenomena , Proto-Oncogene Proteins c-bcl-2/metabolism , Resveratrol/chemical synthesis , Resveratrol/chemistry , Structure-Activity Relationship , bcl-2-Associated X Protein/metabolism
3.
Int J Cancer ; 145(10): 2712-2719, 2019 11 15.
Article in English | MEDLINE | ID: mdl-30989655

ABSTRACT

The development of highly sensitive HPV-genotyping tests has opened the possibility of treating HPV-infected women before high-grade lesions appear. The lack of efficient intervention for persistent high-risk HPV infection necessitates the need for development of novel therapeutic strategy. Here we demonstrate that REBACIN®, a proprietary antiviral biologics, has shown potent efficacy in the clearance of persistent HPV infections. Two independent parallel clinical studies were investigated, which a total of 199 patients were enrolled and randomly divided into a REBACIN®-test group and a control group without treatment. The viral clearance rates for the REBACIN® groups were 61.5% (24/39) and 62.5% (35/56), respectively, for the two independent parallel studies. In contrast, the nontreatment groups showed self-clearance rates at 20.0% (8/40) and 12.5% (8/64). We further found that REBACIN® was able to significantly repress the expression of HPV E6 and E7 oncogenes in TC-1 and Hela cells. The two viral genes are well known for the development of high-grade premalignancy lesion and cervical cancer. In a mouse model, REBACIN® was indicated to notably suppress E6/E7-induced tumor growth, suggesting E6 and E7 oncogenes as a potential target of REBACIN®. Taken together, our studies shed light into the development of a novel noninvasive therapeutic intervention for clearance of persistent HPV infection with significant efficacy.


Subject(s)
Antiviral Agents/therapeutic use , Biological Products/therapeutic use , Papillomavirus Infections/drug therapy , Uterine Cervical Neoplasms/prevention & control , Adult , Animals , Antiviral Agents/pharmacology , Biological Products/pharmacology , Disease Models, Animal , Female , HeLa Cells , Human papillomavirus 16/drug effects , Human papillomavirus 16/pathogenicity , Humans , Mice , Middle Aged , Oncogene Proteins, Viral/antagonists & inhibitors , Papillomavirus E7 Proteins/antagonists & inhibitors , Papillomavirus Infections/virology , Repressor Proteins/antagonists & inhibitors , Treatment Outcome , Uterine Cervical Neoplasms/virology , Viral Load/drug effects
4.
Biosens Bioelectron ; 254: 116233, 2024 Jun 15.
Article in English | MEDLINE | ID: mdl-38518563

ABSTRACT

Intracellular microenvironment (viscosity and polarity) and peroxynitrite ions (ONOO-) are involved in maintaining cell morphology, cell function, and signaling so that it is crucial to explore their level changes in vitro and vivo. In this work, we designed and synthesized a mitochondria-targeted fluorescence probe XBL for monitoring the dynamic changes of viscosity, polarity, and ONOO- based on TICT and ICT mechanism. The fluorescence spectra showed obvious changes for polarity at 500 nm as well as ONOO- and viscosity at 660 nm, respectively. The XBL can image simultaneously viscosity, polarity, and ONOO- in cells, and the results showed excess ONOO- leaded to the increase of viscosity in mitochondrial. The ferroptosis process was accompanied by increase of intracellular viscosity and ONOO- levels (or decrease of polarity), which allowed us to better understand the relevant physiological and pathological processes. The XBL can distinguish normal cells and cancerous cells by the fluorescence intensity changes in green and red channels, and image viscosity in inflamed mice. Thus, XBL can provided the chemical tool to understand the physiological and pathological mechanisms of disease by simultaneous detection of viscosity, polarity and ONOO-.


Subject(s)
Biosensing Techniques , Fluorescent Dyes , Mice , Animals , Viscosity , RAW 264.7 Cells , Mitochondria , Peroxynitrous Acid
5.
Chemotherapy ; 56(4): 291-7, 2010.
Article in English | MEDLINE | ID: mdl-20714146

ABSTRACT

BACKGROUND: Particularly interesting new cysteine-histidine rich protein (PINCH), as an adapter protein of the LIM family for signal transduction in the integrin and growth factor pathway, is upregulated in the stroma of several common types of cancers and involved in promoting tumor progression. In the present study, we examined PINCH expression in normal endometrium, atypical endometrial hyperplasia and endometrioid carcinoma, and further studied the relationships of PINCH expression with clinicopathological variables in cancer patients. METHODS: PINCH expression was examined by immunohistochemistry in 23 normal endometrial samples, 18 atypical endometrial hyperplasias and 48 endometrioid endometrial carcinomas. RESULTS: The PINCH expression in the stroma of cancer (71%) was significantly increased compared to either normal endometrium (17%, p < 0.0001) or atypical hyperplasia (39%, p = 0.017), along with 9 cancers that had stronger PINCH expressions at the invasive margin of the cancers compared to the inner cancers. PINCH expression in cancer was higher in the patients with hypertension (p = 0.041) and estrogen exposure time >30 years (p = 0.021). On the other hand, PINCH expression was not related to menopausal status, gravid status, blood sugar/lipid, family background of cancer, histological grade, myometrial invasion, cervical involvement, lymph nodal metastases, growth pattern, estrogen and progestogen receptors (p > 0.05). conclusion: The results suggest that PINCH seems to play a role, presently unknown, in the tumorigenesis and development of endometrial cancer that merits further study.


Subject(s)
Carcinoma, Endometrioid/metabolism , DNA-Binding Proteins/metabolism , Endometrial Hyperplasia/metabolism , Endometrial Neoplasms/metabolism , Endometrium/metabolism , Adaptor Proteins, Signal Transducing , Adult , Aged , Carcinoma, Endometrioid/pathology , Endometrial Hyperplasia/complications , Endometrial Hyperplasia/pathology , Endometrial Neoplasms/complications , Endometrial Neoplasms/pathology , Endometrium/pathology , Estrogens/adverse effects , Female , Humans , Hypertension/complications , Immunohistochemistry , LIM Domain Proteins , Membrane Proteins , Middle Aged , Precancerous Conditions/metabolism , Precancerous Conditions/pathology , Signal Transduction , Young Adult
6.
Ying Yong Sheng Tai Xue Bao ; 31(4): 1185-1193, 2020 Apr.
Article in Zh | MEDLINE | ID: mdl-32530193

ABSTRACT

Biochar is a potential source for improving soil fertility and crop yield by enhancing phosphorus (P) availability. But the information on quantitative effect of biochar addition on soil P availability is still limited. To address this query, we conducted a meta-analysis with 507 data from 95 eligible literature. The results showed that irrespective of biochar characters (raw material, C:N ratio, pyrolysis temperature, application rate), soil characteristics (texture, pH, organic carbon content), and fertilizer application, biochar addition significantly improved soil available P content by 57.6%. Meanwhile, biochar addition promoted P utilization of crops. The response ratios of plant P concentration to biochar addition were generally lower than those of soil available P. The average response ratio of plant P concentration was 30.6%. The biochars, derived from livestock manure, low-temperature pyrolysis, with lower C:N ratio, alkaline, or higher application rate, were more effective to improve soil available P content and plant P concentration in sandy and loamy soils. For main enzymes involved in P cycle, biochar addition increased activity of alkaline phosphatase (2.8%) but decreased the acid phosphatase activity (17.8%). Overall, biochar addition positively affects soil available and plant P concentration, but has a minute effect on soil phosphatase. The improvement of soil P availability might mainly be ascribed to a great amount of active P fractions in biochar itself.


Subject(s)
Phosphorus , Soil , Charcoal , Fertilizers
7.
BMC Chem ; 14(1): 13, 2020 Dec.
Article in English | MEDLINE | ID: mdl-32099972

ABSTRACT

With the improvement and advance in cancer diagnosis and treatment, the cancer is still a major cause of morbidity and mortality throughout the world. Obviously, new breakthroughs in therapies remain be urgent needed. In this work, we designed and synthesized the compound 1-4, namely resveratrol analogues with methylation of hydroxy distyrene, to further explore its new anti-cancer potential. Encouragingly, compound 1 ((E)-4,4'-(ethene-1,2-diyl)bis(3,5-dimethylphenol)) exhibited cytotoxicity superior to resveratrol in MCF 7 cells. More importantly, the compound 1 showed greater toxicity to tumor cells than that to normal cells, which proved that it could selectively kill tumor cells. The favorable results encouraged us to explore the inhibitory mechanism of compound 1 on MCF 7 cells. The research finding indicated the compound 1 inhibited tumor cell proliferation by both arresting cell cycle in S phase and apoptosis via a prooxidant manner. In addition, the results further verified compound 1 caused cell cycle arrest in S phase and apoptosis by down-regulation of the cycling A1/cycling A2 expression and the rise of Bax/Bcl-2 ratio in a p21-dependant pathway in MCF 7 cells. Therefore, these results are helpful for the effective design of anticancer reagents and the better understanding of their mechanism of action.

8.
Spectrochim Acta A Mol Biomol Spectrosc ; 202: 301-304, 2018 Sep 05.
Article in English | MEDLINE | ID: mdl-29800893

ABSTRACT

In this work, we have designed and synthesized the fluorescent probe 1, which showed a highly selective and sensitive response to Cys over Hcy/GSH in the test. Moreover, the color of probe solution has changed dramatically from colorless to pink with the addition of Cys within 10 min. Meanwhile, the fluorescence intensity exhibited perfectly positive correlation with concentration of Cys from 0 to 200 µM, which offered the important condition for quantitative analysis. Finally, the bioimaging and fluorescence response of probe 1 for fetal calf serum are a powerful safeguard for practical detection of Cys. Therefore, this near-infrared probe will be of great benefit for detecting Cys in the biological systems.


Subject(s)
Cysteine/analysis , Fluorescent Dyes/chemistry , Glutathione/analysis , Homocysteine/analysis , Spectroscopy, Near-Infrared , HeLa Cells , Humans , Imaging, Three-Dimensional , Spectrometry, Fluorescence , Spectrophotometry, Ultraviolet , Time Factors
9.
Ying Yong Sheng Tai Xue Bao ; 27(2): 525-31, 2016 Feb.
Article in Zh | MEDLINE | ID: mdl-27396127

ABSTRACT

Based on the data of soil moisture content and indoor soil surface spectral reflectance from five sampling sites of coastal saline soil, this paper analyzed the relationship between soil moisture content and soil spectrum in wavelength 350-2500 nm. We determined spectral parameters under ratio spectral index (RSI), normalized difference spectral index (NDSI) and difference spectral index (DI), and established the quantitative model of soil moisture content. The results showed significant negative correlation between spectral reflectance and soil moisture content, and the maximum negative correlation was near 1930 nm (r=0.86). By comparison of the regression equation of RSI, NDSI and DI, it was found that the regression equation of exponential function (y=0.00001e9.7203x) built by soil moisture content based on RSI (R1407, R1459) presented the maximum R2 (0.780) and the minimum SE (0.016). The established model based on RSI (R1407, R1459) could be used to monitor soil moisture content accurately in Jiangsu coastal saline soils.


Subject(s)
Soil/chemistry , Water/analysis , Models, Theoretical , Salinity , Spectrum Analysis
10.
Int J Clin Exp Med ; 8(11): 20829-36, 2015.
Article in English | MEDLINE | ID: mdl-26885007

ABSTRACT

The acute myocardial infarction (AMI) model in Chinese miniswine was built by percutaneous coronary artery occlusion. Pathological observation of AMI was performed, and the expression of tumor necrosis factor alpha (TNF-α) in the infarct sites was detected at different days after modeling in Chinese miniswine. The experimental findings may be used as the basis for blood flow reconstruction and intervention after AMI. Seven experimental Chinese miniswine were subjected to general anesthesia and Seldinger right femoral artery puncture. After coronary angiography, the gelfoam was injected via the microtube to occlude the obtuse marginal branch (OM branch). At 1 d, 3 d, 5 d, 7 d, 10 d, 14 d and 17 d after modeling, hetatoxylin-eosin (HE) staining was performed to observe the pathological changes and to detect the expression of TNF-α in the myocardial tissues. Cytoplasmic acidophilia of the necrotic myocardial tissues at 1 d after modeling was enhanced, and cytoplasmic granules were formed; at 3 d, the margins of the necrotic myocardial tissues were infiltrated by a large number of inflammatory cells; at 5 d, the nuclei of the necrotic myocardial cells were fragmented; at 7 d, extensive granulation tissues were formed at the margin of the necrotic myocardial tissues; at 10 d, part of the granulation tissues were replaced by fibrous scar tissues; at 14-17 d, all granulation tissues were replaced by fibrous scar tissues. Immunohistochemical detection indicated that no TNF-α expression in normal myocardial tissues. The TNF-α expression was first detected at 3 d in the necrotic myocardial tissues and then increased at 5 d and 7 d. After reaching the peak at 10 d, the expression began to decrease at 14 d and the decrease continued at 17 d. Coronary angiography showed the disappearance of blood flow at the distal end of OM branch occluded by gelfoam, indicating that AMI model was constructed successfully. The repair of the infarcted myocardium began at 10-17 d after modeling with safe blood flow reconstruction. TNF-α expression in the infarcted myocardium was the highest at 10 d, which can be explained by inflammation and repair of the infarcted myocardium.

11.
Ying Yong Sheng Tai Xue Bao ; 20(4): 879-86, 2009 Apr.
Article in Zh | MEDLINE | ID: mdl-19565770

ABSTRACT

Field experiments with different maturity cotton cultivars and sowing dates were conducted at different sites to quantitatively study the effects of cultivar characteristics, weather conditions (air temperature and solar radiation), and crop management variable (N application rate) on the cotton boll maturation period and cottonseed biomass accumulation. The cotton boll maturation period was simulated by using the scale of physiological development time. Based on the hypothesis of sink-determined, the cottonseed biomass accumulation model was then developed. The subtending leaf N concentration of cotton boll was simulated with a semi-empirical equation, and used as the direct indicator of the N nutrition effect on cottonseed growth and development. The model was tested by independent field data obtained in the Yellow River Valley (Xuzhou and Anyang) and the lower reaches of Yangtze River Valley (Huaian) in 2005. The simulated values of boll maturation period showed reasonable agreement with observed values, with a root mean square error (RMSE) of 2.25 days for cultivar DSC-1, of 2.61 days for cultivar KC-1, and of 2.75 days for cultivar AC-33B. The RMSE of cottonseed dry mass prediction was 9.5 mg x seed(-1) for KC-1 and 8.2 mg x seed(-1) for AC-33B, indicating that the model had a good prediction precision.


Subject(s)
Biomass , Gossypium/growth & development , Models, Biological , Seeds/metabolism , Ecosystem , Forecasting
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