OBJECTIVETo investigate molding technology of total alkaloids from Sophora alopecuroides freeze-dried powders and observe its inhibition effects on liver transplantation tumor in mice.

METHODWith color, clarity, water-soluble and formability as indexes, single factor tests were adopted to screen type and amount of filler, the concentration of total alkaloids in drug liquid, pH in order to determine optimum prescription of total alkaloids from S. alopecuroides freeze-dried powders, the lowest melting point was determined and freeze drying curve was drafted. Mice hepatoma H22 ascites tumor strain was sterile inoculated in right axillary subcutaneous of mice, and antitumor effect of total alkaloids from S. alopecuroides freeze-dried powders on liver transplantation tumor H22 in mice.

RESULTWhen selected 80 g x L(-1) as mannitol as filler, the concentration of total alkaloids in drug liquid was 25 g x L(-1) and pH 6.5-7.5, freeze-dried effect was optimum with fast reconstitute speed. Average inhibition rate of the big (120 mg x kg(-1)) and medium (60 mg x kg(-1)) dose group of total alkaloids from S. alopecuroides freeze-dried powders on liver transplantation tumor H22 in mice were 56.08% and 35.49%, respectively.

CONCLUSIONPreparation technology was reasonable, reproducible and stable, total alkaloids from S. alopecuroides freeze-dried powders had significant antitumor effect and showed a dose-effect relationship.

Alkaloids ; chemistry ; pharmacology ; Animals ; Antineoplastic Agents, Phytogenic ; chemistry ; pharmacology ; Cell Line, Tumor ; Color ; Freeze Drying ; Humans ; Liver Neoplasms ; drug therapy ; Mice ; Powders ; chemistry ; Sophora ; chemistry ; Tumor Burden ; drug effects

Magnetic resonance spectroscopy (MRS) of cervical cancer can detect tumor related specific metabolic compounds such as choline,choline compounds,triglyceride,etc.MRS can be used in identification of benign or malignant lesions of cervix,diagnosis of cervical cancer and monitoring the efficacy of radiotherapy and chemotherapy,etc.It will make for the clinical diagnodis and treatment of cervical cancer.

Objective: To observe the clinical efficacy of acupoint pressure plus long-snake moxibustion for upper-limb spastic hemiplegia after cerebral infarction. Methods: A total of 100 patients were randomized into a control group and an observation group, with 50 cases in each group. Both groups were treated with the same conventional internal medicine and rehabilitation training. The control group was treated with additional acupoint pressure therapy, and the observation group was treated with long-snake moxibustion on the basis of the treatment given to the control group. The Ashworth grade, Fugl-Meyer assessment upper limb scale (FMA-UL) and Barthel index (BI) were evaluated, and the root mean square (RMS) values of biceps brachii and flexor carpi radialis on the affected side were measured before and after treatment. The efficacy was evaluated after treatment. Results: After treatment, the total effective rate of the observation group was significantly higher than that of the control group (P<0.05). After treatment, the Ashworth grade of the observation group was superior to that of the control group (P<0.05). The scores of FMA-UL and BI in both groups increased compared with those before treatment (all P<0.05), and the scores of FMA-UL and BI in the observation group were higher than those in the control group (both P<0.05). The RMS values of biceps brachii and flexor carpi radialis in both groups decreased compared with those before treatment (all P<0.05), and the RMS values of biceps brachii and flexor carpi radialis in the observation group were lower than those in the control group (both P<0.05). Conclusion: Based on conventional internal medicine and rehabilitation training, acupoint pressure plus long-snake moxibustion has great therapeutic efficacy for upper-limb spastic hemiplegia after cerebral infarction. It can improve the degree of spasticity of the affected upper limb, reduce the muscle tone of biceps brachii and flexor carpi radialis on the affected side, and enhance the mobility of the affected limb and the activities of daily living.

Diffusion-weighted imaging (DWI) is sensitive to identification of cervical lesions and lymph node metastasis.DWI can be used to predict and evaluate the therapeutic effect of cervical cancer.Using magnetic resonance imaging and DWI scans in the process of diagnosis and treatment of cervical cancer,which may contribute to the personalized treatment program and improve prognosis for patients.

AIM: To observe the changes of MMP-9 expression in rabbit retina after laser irradiation at different thresholds of 577nm.METHODS: Twenty-six pigmentation rabbits were randomly divided into normal control group(n=2), conventional photocoagulation group (n=6) and subliminal micropulse laser photocoagulation group (n=18).The conventional photocoagulation group was treated with 577nm laser photocoagulation, subcutaneous micro-pulsed laser photocoagulation at a working loading rate of 9%, 12% and 15%, respectively.Eighteen rabbits were again divided into three subgroups according different powers of subthreshold working loading rate of 9%(n=6), 12%(n=6) and 15%(n=6) that undertook, respectively.The expression of MMP-9 on the retina of rabbit eyes was detected by immunohistochemistry.RESULTS: In the conventional photocoagulation group, the expression of MMP-9 in the RPE layer and the visual cell layer was strongly positive, which was significantly higher than that in the sub-micro pulse group(P<0.05).Less MMP-9 positive expression of RPE layer and visual cell layer in the working loading rate of 9% subgroup, and more MMP-9 positive expression of RPE layer and visual cell layer in the working loading rate of 12% subgroup;little expression was also noted in the nucleus of RPE and visual cell layer.Moderate MMP-9 positive expression of RPE layer and visual cell layer was observed in the working loading rate of 15% subgroup.There were no significant differences between the three subgroups (P>0.05).CONCLUSION: The 577nm subliminal micro-pulsed photocoagulation has high selectivity to retinal pigment epithelium at working load rate of 9%, 12% and 15%, and no damage to retinal nerve fiber layer, which is safer than conventional 577nm laser photocoagulation.

A series of adefovir mono-L-amino acid esters, mono non-steroidal anti-inflammatory drugs carboxylic ester prodrugs with more potent anti-HBV activity and lower nephrotoxicity were designed and synthesized. Adefovir bis (L-amino acid) ester was used as lead compound, according to pathological and pharmacological findings that non-steroidal anti-inflammatory drugs can effectively inhibit the organic anion transporter 1 (hOAT1)-mediated adefovir phosphonic acid pairs of anion transport across tubular basement membrane thereby reducing the nephrotoxicity of adefovir. Flatten design principle was used to introducing non-steroidal anti-inflammatory drugs structural fragments to design and synthesize target adefovir mixture ester prodrugs. HepG2 2.2.15 cell line was used as in vitro anti-HBV activity evaluation model. Five compounds exhibited antiviral activity, and compound 18 showed the most potent anti-HBV activity and relatively high selective index (EC50 3.92 micromol L(-1), SI 9.97). HK-2 cell line was used as in vitro model to evaluate nephrotoxicity. Results suggested the target compounds have lower cytotoxicity than the positive control. Moreover, by analyzing the primary structure and activity relationship of these compounds, it could suggest that mono-L-amino acid ester, mono non-steroidal anti-inflammatory drugs carboxylic ester prodrugs strategy has significant potential in the acyclic nucleoside phosphonates prodrug design.

Objective To establish a rat model of coal-burning-borne fluorosis,and to observe the expression changes of bone morphogenetic protein-2 (BMP-2) and bone morphogenetic protein-3 (BMP-3) in the serum of rat treated with different dose of fluoride and different treatment duration.Methods A total of 120 clean grade SD rats(body mass between 80 to 120 g) weaned for 4 weeks were randomly assigned into four groups,which were control,low-dose fluorid,medium-dose fluorid and high-dose fluorid groups,respectively,and 30 rats in each group (female 15,male 15).All of the rats were fed with coal drying corn from fluorosis area.Ten rats were killed by femoral artery bleeding 30 d,90 d and 180 d after exposed to fluoride,respectively.Serum BMP-2 and BMP-3 level was tested by enzyme-linked immunosorbent assay (ELISA).Results ①Results of BMP-2:after exposed to fluoride for 90 d and 180 d,the differences of serum BMP-2 level between groups were statistically significant(F=385.08,173.98,all P ＜ 0.01).In low-dose fluorid,medium-dose fluorid and high-dose fluorid groups,the expression of serum BMP-2 at 90 d[(18.80 ± 0.43),(22.22 ± 0.85),(25.14 ± 0.69)μg/L] and 180 d[(7.98 ± 0.68),(8.97 ± 0.78),(15.04 ± 0.89)μg/L] was higher than that of control group[(12.54 ± 1.29),(7.53 ± 0.97)μg/L,all P ＜ 0.05],and the level of BMP-2 increased with increasing dose of fluoride (all P ＜ 0.05).Within each group,the difference of serum BMP-2 was statistically significant(F =55.42,511.58,686.35,671.64,all P ＜ 0.01).The expression of BMP-2 in each group at 90 d [(12.54 ± 1.29),(18.80 ± 0.43),(22.22 ± 0.85),(25.14 ± 0.69)μg/L] was higher than that at 30 d[(11.75 ± 1.15),(11.42 ± 1.07),(11.38 ± 0.92),(11.15 ±1.03)μg/L,all P ＜ 0.05].The expression of BMP-2 in each group at 180 d[(7.53 ± 0.97),(7.98 ± 0.68),(8.97 ± 0.78),(15.04 ± 0.89) μg/L] was lower than that at 90 d.②Results of BMP-3:the difference between groups was not statistically significant at every experimental stage(F =0.7215,1.2951,0.0964,all P ＞ 0.05).Conclusions Longer excessive fluoride intake stimulates the expression of BMP-2 in rats,but with prolonged fluoride intake,the stimulation becomes weak.The effect of fluoride on BMP-3 is not as sensitive as that on BMP-2.

Abstract: Objective　To investigate the clinical and laboratory characteristics of pulmonary infection caused by Nocardia otitidiscaviarum. Methods　The clinical data of a patient with pulmonary infection caused by Nocardia otitidiscaviarum were reported, and the clinical characteristics, laboratory characteristics and drug sensitivity of pulmonary infection caused by Nocardia otitidiscaviarum were summarized in combination with the relevant literature at home and abroad from January 2010 to December 2022. Results　A 67-year-old female patient was admitted to the hospital on June 30, 2020 because of "repeated chest tightness and shortness of breath for 3 years, aggravated cough, expectoration and fever". The sputum, alveolar lavage fluid and blood of the patient were collected for culture, and the detected pathogenic bacteria were identified. There are pathogenic bacteria growing in sputum and alveolar lavage fluid, which are identified as Nocardia otitidiscaviarum by Autof ms mass spectrometer. According to the results of pathogenic bacteria and the patient's condition, meropenem combined with compound sulfamethoxazole tablets were given anti-infection treatment, and the patient's condition improved and discharged. Conclusion　The clinical manifestations and imaging features of nocardiosis are lack of specificity, and are prone to misdiagnosis and missed diagnosis. Etiology is the key to disease diagnosis, and clinical examination and culture should be conducted in time.

Equipment Design ; Facial Injuries ; therapy ; First Aid ; instrumentation

OBJECTIVETo discuss the changes in Wnt pathway inhibiting factors in esophageal precancerosis lesions induced by methyl benzyl nitrosamine (MBNA) and the effect of Gexia Zhuyu decoction.

METHODWistar rats were subcutaneously injected with MBNA (3.5 mg x kg(-1) for twice per week to establish the model. Since the 1st day after the model establishment, they were orally administered with Gexia Zhuyu decoction (16, 8 mg x kg(-1)). At the 10th week, esophageal tissues were collected to observe the pathological changes of esophageal mucosa, detect SFRP1, sFRP4, Axin1, Axin2 and GSK-3β mRNA levels.by fluorescent quantitation PCR analysis and β-catenin protein level by Western blotting.

RESULTBeing induced by MBNA, rats in the model group showed slight atypical hyperplasia in the histopathological examination. Compared with the normal group, Gexia Zhuyu decoction dose high and low groups showed no significant pathomorphological and histological changes. The model group showed lower gene transcription levels of esophageal tissues sFRP1, sFRP4, Axin1 and Axin2 (P < 0.05 or P < 0.01) and higher β-catenin protein expression level (P < 0.01) than the normal control group. The Gexia Zhuyu decoction low dose group showed higher gene transcription levels of esophageal tissues sFRP1, sFRP4, Axin1 and Axin2 (P < 0.05 or P < 0.01) and lower β-catenin protein expression level (P < 0.01) than the normal control group.

CONCLUSIONUp-regulated β-catenin protein level and down-regulated Wnt pathway could enhance Wnt pathway activity of MBNA-induced esophageal precancerous lesions. Gexia Zhuyu decoction could down-regulate the β-catenin protein level and up-regulate the transcription level of Wnt pathway inhibiting factors, but could not block MBNA-induced esophageal precancerosis lesions.

Animals ; Axin Protein ; genetics ; metabolism ; Drugs, Chinese Herbal ; administration & dosage ; Esophageal Diseases ; drug therapy ; genetics ; metabolism ; pathology ; Glycogen Synthase Kinase 3 ; genetics ; metabolism ; Glycogen Synthase Kinase 3 beta ; Humans ; Male ; Necrosis ; Nitrosamines ; adverse effects ; Proteins ; genetics ; metabolism ; Rats ; Rats, Wistar ; Wnt Proteins ; genetics ; metabolism ; Wnt Signaling Pathway ; drug effects