Anti-pseudo-allergic components in licorice extract inhibit mast cell degranulation and calcium influx / 中国天然药物

Pseudo-allergic reactions (PARs) widely occur upon application of drugs or functional foods. Anti-pseudo-allergic ingredients from natural products have attracted much attention. This study aimed to investigate anti-pseudo-allergic compounds in licorice. The anti-pseudo-allergic effect of licorice extract was evaluated in rat basophilic leukemia 2H3 (RBL-2H3) cells. Anti-pseudo-allergic compounds were screened by using RBL-2H3 cell extraction and the effects of target components were verified further in RBL-2H3 cells, mouse peritoneal mast cells (MPMCs) and mice. Molecular docking and human MRGPRX2-expressing HEK293T cells (MRGPRX2-HEK293T cells) extraction were performed to determine the potential ligands of MAS-related G protein-coupled receptor-X2 (MRGPRX2), a pivotal target for PARs. Glycyrrhizic acid (GA) and licorice chalcone A (LA) were screened and shown to inhibit Compound48/80-induced degranulation and calcium influx in RBL-2H3 cells. GA and LA also inhibited degranulation in MPMCs and increase of histamine and TNF-α in mice. LA could bind to MRGPRX2, as determined by molecular docking and MRGPRX2-HEK293T cell extraction. Our study provides a strong rationale for using GA and LA as novel treatment options for PARs. LA is a potential ligand of MRGPRX2.

The role and mechanism of gut microbiota in the occurrence of colorectal cancer / 中华消化外科杂志

Colorectal cancer is a common malignant tumor of the digestive system, accoun-ting for about 10% of all new cancer cases worldwide. In recent years, a large number of studies have proved that gut microbiota and its metabolites play an important role in the occurrence of colorectal cancer, and different pathogenic models can explain for the pathogenic mode of different gut microbiota. The authors review the role and mechanism of gut microbiota in colorectal cancer.

Clinical application of thoracodorsal artery perforator flaps in the repair of head and neck defects / 中华耳鼻咽喉头颈外科杂志

Objective: To analyse the clinical application of thoracodorsal artery perforator flaps (TDAPF) in the repair of head and neck defects. Methods: A retrospective review was conducted on 38 patients with oral and maxillofacial head and neck malignant tumors who underwent radical resection of oral and oropharyngeal carcinoma and TDAPF repair in the Department of Oral and Maxillofacial Head and Neck Oncology of the Ninth People's Hospital Affiliated to Shanghai Jiao Tong University School of Medicine from June 2017 to November 2018. Among them, 32 were males and 6 were females, aged 30-74 years. Flap size, vessel pedicle length, diameter and number of perforators, and flap fat thickness were recorded and counted. Elasti Meter and Skin Fibro Meter were applied to measure the skin elasticity and hardness in the donor areas of 4 kinds of skin flaps before the flap preparation. SPSS 19.0 statistical software was used for statistical analysis of the data. Results: All the flaps survived (100%). The mean elasticity of TDAPF [(41.2±12.9) N/m] was significantly lower than that of anterolateral thigh [(77.6±23.3) N/m, χ²=88.89, P<0.05], anterolateral thigh [(62.6±17.7) N/m, χ²=59.99, P<0.05] and or forearm flap [(51.7±8.6) N/m, χ²=37.82, P<0.05]. The hardness of TDAPF [(0.037±0.016) N] was also significantly lower than that of anterolateral femoral [(0.088±0.019) N, F=93.27, P<0.05], anteromedial femoral [(0.059±0.020) N, F=25.71, P<0.05] or forearm flap [(0.062±0.016) N, F=29.11, P<0.05]. Follow-up period ranged from 2 to 14 months. The 38 patients treated with TDAPF had a good recovery of the functions in the recipient areas, and the scars of the donor areas were not obvious after surgery, without serious complications. Conclusion: TDAPF is suitable for reconstruction of head and neck defect, with ductile texture and good recovery of the morphology and function of head and neck.

Human placenta-derived mesenchymal stem cell transplantation provides neuroprotection against cerebral infarction in rats / 中国组织工程研究

BACKGROUND: Bone marrow mesenchymal stem cells improve neurological functional recovery from cerebral infarction, but they are a rare population in the bone marrow with difficulty in cell separation and purification. OBJECTIVE: To investigate the neuroprotective effects and the potential mechanisms of human placenta-derived mesenchymal stem cell transplantation for cerebral infarction in rats. METHODS: Totally 120 rats subjected to middle cerebral artery occlusion were randomized into treatment group and control (n=60 per group). The rats were intravenously treated with human placenta-derived mesenchymal stem cells in the treatment group or the phosphate buffer saline in the control group. Then, a modified neurological severity score was assessed at 1, 3, 7, 14 days post transplantation, and measurement of infarct volume in the ischemic brain was performed using 2,3,5-triphenyltetrazolium chloride staining at 14 days post transplantation. The anti-human specific immunostain for mitochondria in the ischemic brain was performed and the mitochondria-positive cells were counted; TUNEL immunostaining was performed and TUNEL positive cells were counted. ELISA assays for brain-derived neurotrophic factor (BDNF), vascular endothelial growth factor (VEGF) and hepatocyte growth factor (HGF) were also performed in the ischemic brain. RESULTS AND CONCLUSION: At 1, 3, 7 and 14 days after treatment, the modified neurological severity score in the treatment group was significantly lower than that in the control group (P < 0.05). At 14 days after treatment, the infarct volume in the treatment group was significantly lower than that in the control group (P < 0.05), only few mitochondria-positive cells were present in the ischemic brain, and the number of TUNEL positive cells in the treatment group was significantly less than that in the control group (P < 0.05). At 3 and 14 days after treatment, BDNF expression levels in the treatment group were significantly higher than those in the control group (P < 0.05). At 7 and 14 days after treatment, VEGF expression levels in the treatment group were significantly higher than those in the control (P < 0.05). At 7 days after treatment, HGF expression level in the treatment group was significantly higher than that in the control group (P < 0.05). To conclude, intravenous administration of human placenta-derived mesenchymal stem cells can promote neuroprotective effects against cerebral infarction. These effects may be related to the increase of BDNF, VEGF and HGF expression and the decrease of apoptosis in the ischemic brain.

Forecasting and prevention of collapse in femur head necrosis / 中国骨伤

By discussing different ways on prediction, prevention and treatment of femur head necrosis (FHN), to provide a theory reference for future clinical application. By searching, reading and summarizing related-literatures through CNKI, VIP, CBM and foreign-related literature, to sum up the relevance methods and techniques of currently used. It was found that imaging study (especially X-ray and MRI) was of great importance in prediction. There were several ways (both non-surgical or surgical) for prevention and treatment. FHN collapse was affected by many factors, but most of the researches were all focus on one aspect of the mechanism and based on small samples. It is necessary to have a research with a large sample and to compare the effect on different treatment. Early and effective imaging inspection is needed for high risk group of FHN; possibility of collapse should be predicted for existing FHN; core decompression or vascularized bone grafting are required for collapse of high risk group. Early prediction and treatment are essential for FHN patients.

Method for screening cysteinyl leukotriene receptor 2 antagonists and preliminary screening of compounds / 浙江大学学报·医学版

<p><b>OBJECTIVE</b>To establish a method for screening cysteinyl leukotriene receptor 2 (CysLT(2)) antagonists and to preliminarily screen a series of synthetic compounds.</p><p><b>METHODS</b>Rat glioma cell line (C6 cells) highly expressing CysLT(2) receptor was used. Intracellular calcium concentration was measured after stimulation with the agonist LTD(4),which was used to screen compounds with antagonist activity for CysLT(2) receptor. Bay u9773, a CysLT1/CysLT(2) receptor non-selective antagonist, and AP-100984, a CysLT(2) receptor antagonist, were used as control.</p><p><b>RESULT</b>PT-PCR showed a higher expression of CysLT(2) receptor in C6 cells. LTD(4) at 1 mumol/L significantly increased intracellular calcium in C6 cells; the maximal effect was about 37.5% of ATP, a positive stimulus.LTD(4)-induced increase of intracellular calcium was blocked by CysLT(2) receptor antagonists, but not by CysLT(1) receptor antagonists. Among the synthetic compounds, D(XW-)1,2,13,23,29 and 30 inhibited LTD(4)-induced increase of intracellular calcium.</p><p><b>CONCLUSION</b>LTD(4)-induced change in intracellular calcium in C6 cells can be used as a screening method for CysLT(2) receptor antagonists. The compounds, D(XW-)1,2,13,23,29 and 30, possess antagonist activity for CysLT(2) receptor.</p>

Recent advances in the study of bioreductive drugs targeted tumor hypoxia / 药学学报

Tumor hypoxia is the necessary process in the development of solid tumors, which is the key factor for drug resistance, recurrence, attack and shift of tumor. Hypoxic tumor cells have a certain extent of tolerance to radiation and chemotherapy. Tumor hypoxia is an important target for medication therapy. In the recent years, the bioreductive drugs targeted tumor hypoxia has made great process in the treatment of tumors. The latest advances of bioreductive drugs targeted hypoxia were reviewed in this paper.

An ectopic study of tissue-engineered bone with Nell-1 gene modified rat bone marrow stromal cells in nude mice / 中华医学杂志(英文版)

<p><b>BACKGROUND</b>Tissue engineering techniques combined with gene therapy have been recently used to improve osteogenesis. NEL-like molecule-1 (Nell-1), a novel growth factor, has been reported to have specificity for osteochondral lineage. The study assessed the osteogenic differentiation of rat bone marrow stromal cells (bMSCs) after Nell-1 gene modification and examined its ectopic bone formation ability in a nude mice model with tissue engineering technique.</p><p><b>METHODS</b>bMSCs obtained from Fischer 344 rats were transduced with either AdNell-1 (Nell-1 group) or Ad-beta-galactosidase (AdLacZ, LacZ group) or left untransduced (untransduced group). The expression of Nell-1 protein was determined by Western blotting and transfer efficiency was assessed. mRNA expressions of osteopontin (OP), bone sialoprotein (BSP) and osteocalcin (OC) were assessed by real-time PCR 0, 3, 7, 14, and 21 days after gene transfer. Alkaline phosphatase (ALP) activity was measured and von Kossa test was also conducted. Finally, with a tissue engineering technique, gene transduced bMSCs, combining with beta-tricalcium phosphate (beta-TCP) at a concentration of 2 x 10(7) cells/ml, were implanted at subcutaneous sites on the back of nude mice. Four weeks after surgery, the implants were evaluated with histological staining and computerized analysis of new bone formation.</p><p><b>RESULTS</b>Under current transduction conditions, gene transfer efficiency reached (57.9 +/- 6.8)%. Nell-1 protein was detected in Nell-1 group but not in untransduced group and LacZ group. Induced by Nell-1, BSP and OP expression were increased at intermediate stage and OC expression was increased at later stage. ALP activity and the number of calcium nodules were highest in Nell-1 group. Four weeks after implanted into nude mice subcutaneously, the percentage of new bone area in Nell-1 group was (18.1 +/- 5.0)%, significantly higher than those of untransduced group (11.3 +/- 3.2)% and LacZ group (12.3 +/- 3.1)% (P < 0.05).</p><p><b>CONCLUSIONS</b>This study has demonstrated the ability of Nell-1 to induce osteogenic differentiation of rat bMSCs in vitro and to enhance bone formation with a tissue engineering technique. The results suggest that Nell-1 may be a potential osteogenic gene to be used in bone tissue engineering.</p>

Synthesis and AchE inhibitory activity of 2-phenoxy-indan-1-one derivatives / 药学学报

<p><b>AIM</b>To design and synthesize novel AchE inhibitors.</p><p><b>METHODS</b>The condensation of 2-bromo-5, 6-dimethoxy-indan-1-one with various aminoalkyl phenols in the presence of K2CO3 and acetonitrile gave the corresponding title compounds, and the in vitro AchE and BchE inhibitory activities were evaluated by the modified Ellman method.</p><p><b>RESULTS</b>Sixteen novel target compounds 8a - p were synthesized, their structures were confirmed by 1H NMR, MS, IR and elemental analysis. Preliminary pharmacological test demonstrated that most of these compounds displayed high AchE inhibitory activities, the IC50 of the most potent inhibitor 8h was 50.0 nmol x L(-1), similar to that of Huperzine A (IC50 = 53.0 nmol x L(-1)), while all the compounds were almost inactive against BchE.</p><p><b>CONCLUSION</b>2-Phenoxy-indan-1-one derivatives exhibit high activities of AchE inhibition and are worthy of further investigation.</p>

Synthesis and antitumor activity of arylsubstituted imidazolin-2-one derivatives / 药学学报

<p><b>AIM</b>To design and synthesize new arylsubstituted imidazolin-2-one analogues as antitumor compounds.</p><p><b>METHODS</b>Arylsubstituted imidazolin-2-ones were prepared by condensation the appropriate omega-amino-acetophenone hydrochloride with arylisocyanate in toluene. The target compounds prepared in this study were tested for cytotoxicity against PC-3, A549, HO-8910, Hela, HL60, K562 and HL60R cancer cell lines, and mechanism of one of the products 4y was further evaluated with its mechanium.</p><p><b>RESULTS</b>Thirty-six new compounds were synthesized and confirmed by 1H NMR, MS and elemental analysis. One of the synthesized products, compound 4y, displayed an encouraging selective activity against HL60 cells, and it was partlydue to the cell cycle arrest and cell apoptosis.</p><p><b>CONCLUSION</b>Compound 4y is worthy to be intensively studied.</p>

Synthesis and vasorelaxation action of flavonoids / 药学学报

<p><b>AIM</b>To search for flavonoids which possess stronger vasorelaxation action.</p><p><b>METHODS</b>Four quercetin glycosides (1a - d) were synthesized from quercetin in three steps i. e. selective protection of quercetin, condensation with corresponding acetyiglycosyl bromide, and then removal of the protecting group; Six flavone compounds (2a - f) were prepared from phloroglucinol according to the conventional methods; The structures of synthetic compounds were confirmed by IR, 1H NMR, 13C NMR and MS. Vasorelaxation action of ten synthetic quercetin derivatives (or analogues) and four natural flavonoids compounds were examined on the isolated rat thoracic aorta rings; Comparative octanol-water partition coefficients (logP) were measured using a reversed-phase HPLC method.</p><p><b>RESULTS</b>Most of the tested flavonoids showed concentration dependent relaxation effects against PE-induced contractions of rat aortic rings. These compounds had stronger action with the augment of logP values.</p><p><b>CONCLUSION</b>Compound 3-bromo-5 ,7-dihydroxyflavone (2d) was identified to have the most potent vasodilating action. These compounds exert vasodilating effects that are related to the logP values. A structure-activity relationship of flavonoids was suggested.</p>

An improved novel method of venlafaxine synthesis / 浙江大学学报·医学版

<p><b>OBJECTIVE</b>To synthesize venlafaxine with an improved novel method.</p><p><b>METHODS</b>p-methoxypheny lethyl-acid was reacted with SOCl(2) to produce acyl chloride which was reacted with N,N-dimethylamine solution to get amide; then through Ivanov reaction and reduction by KBH(4)/BF(3).Et(2)O to yield venlafaxine.</p><p><b>RESULT</b>Venlafaxine was successfully synthesized by using this method with an yield rate of 50.3%.</p><p><b>CONCLUSION</b>The improved method is suitable for industrial production of venlafaxine.</p>

Study on ultrasonic extraction techniques of flavonoids in Chrysanthemum morifolium / 中国中药杂志

<p><b>OBJECTIVE</b>To optimize the ultrasonic extraction condition for flavonoids from Chrysanthemum morifolium.</p><p><b>METHOD</b>The extraction rate of flavonoids optimized condition (ethanol concentration, ultrasonic time, solvent quantity and extraction times) was determined by orthogonal design. UV-Spectrophotometry was used for the determination.</p><p><b>RESULT</b>The order of factors to affect the flavonoid extraction was ethanol concentration > extraction times > solvent quantity > ultrasonic time.</p><p><b>CONCLUSION</b>The optimum ultrasonic extractions were: A2 B2 C3 D3. Compared with traditional extraction, ultraction method can save time, be easy to operate, improve extraction rates and need no heating.</p>

Study on extraction technology for extract and flavonoids in Chrysanthemum morifolium by orthogonal design / 中国中药杂志

<p><b>OBJECTIVE</b>To ascertain extraction technology condition for extract and flavonoids from Chrysanthum morifoliwn.</p><p><b>METHOD</b>The optimizing ultrasonic extraction condition on the basis of extractive yield and flavonoids were determined by orthogonal design.</p><p><b>RESULT</b>The order of factors which affected the flavonoid extraction was extraction times > ethanol concentration > ultrasonic time > solvent quantity.</p><p><b>CONCLUSION</b>The optimum ultrasonic extractions are A2B3C3D3. Compared with traditional extraction, ultraction method is timesaving, simple to operate, stable and need not be heated.</p>

Predictive value of serum N-tenninal pro-brain natriuretic peptide in acute myocardial infarction patients for left ventricular remodeling / 中华检验医学杂志

Objective To evaluate the forecasting capability of serum N-terminal pro-brain natriuretic peptide ( NT-proBNP) level for Left ventricular ( LV) remodeling of patients with acute myocardial infarction (AMI) through observation of the relationship between serum NT-proBNP on the 3rd day and LV remodeling following onset of AMI. Methods Electrochemilumin-escence was adopted to determine the serum NT-proBNP level on the 3rd day after AMI attack for 106 cases of patients with anterior, anteroseptal and anterolateral AMI, with echocardiography performed to detect LV end-diastolic diameter (LVDd) and leftventricular ejection fraction (LVEF) respectively on the 3rd day and 3 months after the attack. Results The serum NT-proBNP level of AMI patients on the 3rd day averaged 1039. 28 (241. 50-1 184. 25) ng/L For AMI patients on the 3rd day and 3 months after, LVDd rose to (53?7) mm (P 0.05) from (53?8) %. NT-proBNP concentration on the 3rd day after AMI onset was positively correlated with△LVDd significantly, r =0. 403 (P 5mm during the 3 months and LVEF at the 3rd month≤40 % , AUC was 0. 893. Conclusion The test results showed serum NT-proBNP level for AMI patients on the 3rd day may be used as one of forecasting indexes of LV remodeling for AMI of advanced stage.

Improved method of fluvoxamine synthesis / 浙江大学学报·医学版

<p><b>OBJECTIVE</b>To modify the synthetic method of fluvoxamine.</p><p><b>METHODS</b>Fluvoxamine was synthesized from 4-trifluoromethylbenzonitrile by the steps of Grignard reaction, hydrolysis and oximation.</p><p><b>RESULT</b>The chemical structure of the synthesized product was confirmed by (1)HNMR, and the total yield reached to 36.16%.</p><p><b>CONCLUSION</b>The results indicate that the synthetic route is practical.</p>

Improved method of epalrestat synthesis / 浙江大学学报·医学版

<p><b>OBJECTIVE</b>To synthesize epalrestat and to improve the method of synthesis.</p><p><b>METHODS</b>Glycine reacted with carbondisulfide,then with ClCH(2)COONa to give 3-carboxymethylrhodanine. PhCHO reacted with CH(3)CH(2)CHO in NaOH/EtOH solution to produce 2-methylcinnamaldehyde.3-carboxymethylrhodanine and 2-methylcinnamaldehyde were treated with NH(3).H(2)O to obtain epalrestat.</p><p><b>RESULT</b>The described method was effective in synthesis of Epalrestat and the yield was higher than that of in references.</p><p><b>CONCLUSION</b>The results suggest that this method is suitable for industrial production.</p>

Synthesis of hirsutrin and hyperin / 浙江大学学报·医学版

OBJECTIVE: To investigate an easier method for preparation of hirsutrin and hyperin. METHODS: Rutin was utilized as the starting material. The target compounds were produced via benzoylation, hydrolysis, glycosidation and deproteination. RESULTS: The yield of key intermediate 5,7,3',4'-tetra-O-benzoyl quercetin was improved by reducing the hydrolysis time of 5,7,3',4'-tetra-O-benzoyl rutin in HCl/EtOH. Hirsutrin and hyperin were synthesized. CONCLSION: Hirsutrin can be synthesized and the yield of hyperin improved by this method.

Preparation of albendazole sulfoxide--- an active metabolite / 浙江大学学报·医学版

OBJECTIVE: To investigate the facile method for preparation of albendazole sulfoxide, an active metabolite in vivo. METHODS: The reaction condition was investigated according to evaluations to the results of the experiment through temperature, solvent, oxidation agent, reaction time and impurity. RESULTS: The target compound was obtained by oxidation of albendazole with the presence of sodium metaperiodate in glacial acetic acid under low temperature and was free from contamination by impurity albendazole sulfone. Pure product (content >98%) and high yield (>90%percnt;) have been achieved due to reaction selection. CONCLUSION: Oxidation condition is essential to the preparation of albendazole sulfoxide.

Mutation of cystathionine beta-synthase gene(CBS G919A/T833C)in patients with diabetic nephropathy detected by amplification refractory mutation system-real time PCR / 中华检验医学杂志

Objective To develop a TaqMan fluorogenic probe based amplification refractory mutation system (TaqMan-ARMS) for the detection of the C BS gene G919A and T833C mutations,and to investigate whether the mutations are associated with diabetic nephropathy in Chinese population. Methods According to the principle of amplification refractory mutation system,the cycle threshold (Ct) of wild (Wct) and mutation (Mct) allele-specific primers between the two PCR reactions in real-time PCR were monitored and genotype detection criteria were established based on the threshold ratio Act (?ct= Wct/ Mct) or an appearance of exponential amplification.With this technique,the G919A and T833C mutations in the CBS gene were analyzed in 94 patients with diabetic nephropathy and 140 control subjects. Results The detection criteria of TaqMan-ARMS assay for T833 allele were ?ct40,for T833C allele 0.940,respectively.The criteria for G919 allele were ?ct40,for G919A allele 0.9240,respectively.The T833C rates of TT,TC and CC genotypes were 98.94%, 1.06% and 0 in the patients and 99.29%,0.71% and 0 in the controls.The 833C allele frequencies were 0.53% in the patients and 0.36% in the controls.No significant differences in both genotypes and allele of T833C mutation were observed between the two groups.The G919A point mutation was not observed in all subjects.Conclusions A TaqMan-ARMS assay for the detection of the CBS gene GA919A and T833C mutations has been developed.The assay is accurate and sensitive,and is suitable for high-throughput detection of the point mutations.The G919A and T833C point mutations of CBS gene may not be related to diabetic nephropathy in Chinese.