1.Controversies and focus on surgical treatment of pancreatic cancer
Chinese Journal of Digestive Surgery 2009;8(4):254-257
Pancreatic cancer is a common disease with a poor prognosis. Despite recent advance in the field of diagnos-tic technique, surgical resection and adjuvant therapy for pan-creatic cancer, the overall 5-year survival rate is still less than 5%. This is due to its aggressive growth behavior, early local invasion and metastasis, and resistance to chemotherapy and radiation therapy. Surgical treatment is still regard as the only chance for curing pancreatic cancer. Many new strategies in the surgical treatment of pancreatic cancer, including extended lymphadeneetomy, vascular resection, the use of laparoscopy, surgery for metastastic or recurrent disease, and neoadjuvant therapy, are currently under debate. In this review, we discuss the current status of surgical treatment for pancreatic cancer, and highlight the controversies and focus.
2.Delayed open reduction and internal fixation for the Cotton's fracture
Rui XIA ; Rong KONG ; Shiyuan FANG
Orthopedic Journal of China 2006;0(12):-
0.05).The activities degrees of ankle joint also had no statistical difference.[Conclusion]According to the extent of the displacement of Cotton's fracture,we should make the right operative order and the incision,thus we can get results with anatomic reduction and shorten the operative time,which can help the patients make early exercises and get satisfactory effect.
3.86 Cases Study: Treatment of Stroke Constipation with ZengYeChengQi Decoction (ZYCQD)and BuYangHuan Wu Decoction (BYHWD)
Rui CHEN ; Guangyi WANG ; Tingting KONG
International Journal of Traditional Chinese Medicine 2009;31(2):139,149-
Objective To observe the effects of a-eating stroke constipation with ZengYeChengQi Decoction (ZYCQD) and BuYangHuanWu Decoction(BYHWD). Methods 86 cases of stroke constipation were recruited to receive ZengYeChengQi Decoction (ZYCQD) and BuYangHuanWu Decoction (BYHWD) orally for one therapeutic course, and observe the therapeutic effects. Results Among 86 cases, 65 cases were totally recovery, 16 cases had obvious improvement, and 5 cases were inefficacy. The total effective rate was 94.19%. Conclusion Oral ZengYeChengQi Decoction (ZYCQD) and BuYangHuanWu Decoction (BYHWD) can improve constipation symptom score and improve the clinical therapeutic effect.
4.Immunopharmacological actions of capsule bushenyanshou in mice
Hui WANG ; Jin-He CHEN ; Rui KONG ; Qi-Xiong LI ; Rui KONG ;
Chinese Journal of Clinical Pharmacology and Therapeutics 1999;0(04):-
Aim The effect of capsule bushenyanshou (BSYS), a compound of traditional Chinesemedicine, on the immunopharmacological activities of mice was investigated. MethodsThe indexes of immunopharmacological activity, such as the clearance rate of charcoalparticles, the lymphocyte transformation and the content of serum hemolysin, were mea-sured. Results Capsule BSYS (400, 800 mg?kg-1, qd ? 12) markedly increased theclearance rate of iv charcoal particles and 1he lymphocyte transformation stimulated invivo by PHA in mice. In hydrocortisone -treated mice(15 mg? kg-1, sc, qd ? 5), capsuleBSYS significantly enhanced the content of serum hemolysin and the weights of spleenand thymus. The results also demonstrated capsule BSYS performed a sighted inhibition ofthe delayed type hypersensitivity in mice. Conclusion Capsule BSYS has the capacity ofimmunological intensification and regulation.
5.Dose distribution of 125Ⅰ seed sources in brachytherapy prostate cancer model
Rui MA ; Shuyu YUAN ; Linghai KONG ; Liangan ZHANG
Chinese Journal of Radiological Medicine and Protection 2011;31(4):485-488
Objective To study the dose distribution of the radioactive 125Ⅰ seeds sources in the treatment of prostate cancer and also to explore the more effective method for improving treatment planning system (TPS).Methods Choose the designated TPS and use TLDs dosimeter based on a prostate cancer model.Finally stimulated measurement was focused on dose distribution in prostate cancer.The number of 125Ⅰ seed sources implanted was 89, each with 1.37 × 107 ( ± 5% ) Bq.Results Maximum dose of every layer ranged from 151 to 241 Gy, by 4.1% to 66.0% higher than the prescribed dose (145 Gy).The Minimum dose of every layer ranged from 101 to 128 Gy, by 12% to 30% higher than the prescribed dose.The maximum dose of normal tissue at 10 mm from the edge of model ranged from 46 to 91 Gy.The deviation was 44% -63% compared with the prescribed dose.Conclusions The designated TPS shows that it could be used as a practical guide for treatment of prostate cancer with the radioactive 125Ⅰ seed sources.The research methods offered by the study can provide evaluation of the TPS.
6.The technologies of small molecule ligand-target protein interaction and high throughput ligand screening
Rui-fang DONG ; Yuan-zheng XIA ; Ling-yi KONG
Acta Pharmaceutica Sinica 2023;58(11):3242-3253
The interaction of drug and target protein is a critical part of new drug discovery. It is the premise for drugs to exert therapeutic effects by targeting specific binding sites of target proteins and thereby affecting its pharmacological activity. Currently, a variety of techniques are exploited to detect the interaction between drug ligands and target proteins. For example, cellular thermal shift assay (CETSA) and differential scanning fluorimetry (DSF) based on thermodynamics, mass spectrometry and nuclear magnetic resonance technology, etc. In addition, high-throughput ligand screening technology provides technical convenience for the search of specific ligand, and is a powerful tool to efficiently identify the interaction between drug ligand and target protein. Here, we summarize the detection techniques of interaction between small molecules and target proteins, and discuss the application of high-throughput ligand screening technology in drug research.
7.Label-free target identification for natural products based on proteomics
Rui-fang DONG ; Yuan-zheng XIA ; Ling-yi KONG
Acta Pharmaceutica Sinica 2023;58(8):2000-2015
Target identification and verification of natural products is an important and challenging work in the field of chemical biology. It is also an important job for researchers to apply chemical proteomics technology to biomedicine in order to identify target proteins of natural products. Target identification is critical to understanding its mechanisms and developing natural products as molecular probes and potential therapeutic drugs. Traditional approaches of small molecule target identification based on affinity have been shown to be successful, such as click-chemical probes, radioisotope labeling or photosensitized small-molecule probes. Nevertheless, these technologies require purified candidate target proteins, and modified small molecules with probes or linkers, such as adding agarose beads, biotin labels, fluorescent labeling or photo-affinity labeling. Many structure-activity relationship studies should be performed to ensure that the addition of small molecule labels undisturbed the original biological activity of the small molecules. Unfortunately, all these modifications are likely to alter their biological activity or binding specificity. To overcome the bottleneck of "target recognition", researchers have developed a series of new techniques for unmodified drug target identification. In this article, we reviewed the target identification techniques of natural product without structural modification in order to provide reference for the development of natural products.
8.Progress in nanobody and its application in diagnosis.
Qingming KONG ; Yabo YAO ; Rui CHEN ; Shaohong LU
Chinese Journal of Biotechnology 2014;30(9):1351-1361
Nanobodies are derived from the variable domain of the heavy-chain antibodies (HCAbs) that occur naturally in the serum of Camelidae. They are the smallest antibody fragments capable to bind antigens. With the characteristics of their increased solubility, increased domain stabilities, nanomolar affinities, easy crossing the blood-brain barrier, easy generation, engineering, optimization and tailoring, easy humanization, nanobodies have extensive application prospects in diagnosis and detection. Although nanobody has demonstrated tremendous success, a number of practical challenges limit its broader applications in disease diagnosis and detection, including construction of a phage library and selection of nanobody fragments with high affinity and immunogold labeling technique. Here, we review several recent findings on the use of nanobodies in molecular diagnostics and suggest some practical strategies in resolving the current challenges in this attractive research area, particularly to optimize the affinity, solubility, humanization of nanobodies.
Humans
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Immunoglobulin Heavy Chains
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chemistry
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Single-Domain Antibodies
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chemistry
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drug effects
9.Inhibition of microRNA195 attenuates high-glucose induced neonatal cardiomyocytes hypertrophy in vitro.
Kong BIAO ; Shen DONGLI ; Rui TAO ; Zhang GUOHUI
Chinese Journal of Cardiology 2015;43(8):712-717
OBJECTIVETo investigate the effects of micro(mi) RNA-195 on high-glucose induced neonatal cardiomyocyte hypertrophy and to explore the related mechanism.
METHODSThe potential target gene of miRNA-195 (Smad7) was predicted by TargetScan5. 1 software. Cardiomyocytes were isolated from neonatal SD rats and cells were then randomly divided into three groups: cells treated by culture medium containing 5 mmol/L glucose (control group) , by culture medium containing 25 mmol/L glucose (high glucose group) and treated by culture medium containing 25 mmol/L glucose and miRNA-195 inhibitor transfection (miRNA-195 inhibitor group). After 24, 48, or 72 h of in vitro culture, the morphology of cardiomyocytes was examined under phase contrast microscope. Micrographs were captured and the cell surface was calculated. The mRNA expressions of miRNA-195 and myosin heavy chain β (β-MHC), a biomarker for cardiomyocyte hypertrophy, in cardiomyocytes were detected by RT-PCR. The protein expression of Smad7 was determined by Western blot. The concentration of transforming growth factor-β1 (TGF-β1) in the supernatant of culture medium was measured by ELISA.
RESULTSCross-sectional area of cardiomyocytes, expression of miRNA-195 and β-MHC and secretion of TGF-β1 were significantly increased in high glucose-treated cells (P < 0.05 vs. normal control). The protein expression of Smad7 was significantly downregulated in cells exposed to high glucose for 48 h (P < 0.05 vs. normal control). Downregulation of miRNA-195 partly reversed the high glucose-induced effects. The expression of Smad7 was negatively correlated with miRNA-195 in high glucose control group (correlation coefficient: -0.945, P < 0.05).
CONCLUSIONOur results demonstrate that Smad7 could be the target gene of miRNA-195. miRNA-195 might play a crucial role in the development and progression of diabetic cardiomyopathy possibly through downregulating the expression of Smad7 and modulating TGF-β/Smad pathways.
Animals ; Down-Regulation ; Glucose ; Hypertrophy ; MicroRNAs ; Myocytes, Cardiac ; Rats ; Rats, Sprague-Dawley ; Transfection ; Transforming Growth Factor beta1
10.EFFECTS OF 18α-GLYCYRRHIZIC ACID ON RAT LIVER CYTOCHROME P450 ISOENZYMES AND PHASE II TRANSFERASE
Jing YANG ; Renxiu PENG ; Rui KONG ; Jieping YU
Acta Pharmaceutica Sinica 2001;36(5):321-324
AIM To study the effect of 18α-glycyrrhizic acid (18α-GL) on hepatic microsomal drug metabolizing enzymes in rats. METHODS 18α-GL (12.5, 50.0 mg*kg-1*d-1) were given ip to male Wistar rats for 3, 6 or 12 consecutive days. The rats were sacrificed 24 h after the last dose and the liver microsomes were prepared for analysis of cytochrome P450 (CYP) isozymes and phase II transferase activites. RESULTS Aniline hydroxylase (CYP2E1) activities in the rats treated with 18α-GL (12.5, 50.0 mg*kg-1) for 6 days decreased dose-dependently by up to 53.2%; For 3, 6 or 12 days 7-ethoxyresorufin O-deethylase (CYP1A1) activities in the rats of 50 mg*kg-1 dose group decreased time-dependently by 17.6%, 38.3% and 47.3%, respectively; Erythromycin N-demethylase (CYP3A) activities was significantly inhibited from 23.1% to 34.3%. UDP-glucuronosyltransferase activities toward 7-hydroxy-4-methylcoumarin significantly increased ranging from 19.3% to 29.9%. UDP-glucuronosyltransferase activities toward 4-phenylphenol in the rats treated with 18α-GL (12.5, 50.0 mg*kg-1) for 6 days increased by 45.9% and 70.3%. Glutathione S-transferase (GST) activities in the rats treated with 18α-GL (12.5,50.0 mg*kg-1) for 6 days increased by 13.7% and 48.3% in dose-dependent manner. CONCLUSION 18α-GL inhibited rat liver microsomal cytochrome P450 while induced phase II transferase.