Genotoxicity evaluation of HMS-01 / 药学实践与服务

Objective To provide a toxicological basis for HMS-01 in future clinical trials, through genotoxicity testing of safety evaluation. Methods The genotoxicity of HMS-01 was evaluated by Bacterial Reverse Mutation Assay （Ames test） with Salmonella typhimurium. Results HMS-01 was non-mutagenic against Salmonella typhimurium at six doses of 20.6, 61.7, 185.2, 555.6, 1666.7, and 5000 μg/dish with （or without） a metabolic activation system. Conclusion HMS-01 was not found to be mutagenic in the dose range of this experiment.

Research progress on total synthesis and activity of nitidine / 药学实践杂志

Nitidine is a benzophenanthridine alkaloid derived from Zanthorulum nitidum (Roxb .) DC root .Research shows that nitidine displays rich biological activities ,such as anti-tumor ,anti-inflammatory ,anti-malaria and etc .This paper reviewed the progress of the total synthesis methods for nitidine and recent research on bioactivities .

Configuration inversion of C-2-hydroxy in lycorine / 药学实践杂志

Objective Study configuration inversion of C-2-hydroxy in lycorine to provide a foundation for semi-synthesis of asiaticumine B .Methods Use instrumental analyses to explore the C-2-hydroxy configuration through oxidation and reduc-tion reactions .Results Accomplished configuration inversion of C-2-hydroxy in lycorine with 49% yield .Conclusion We identified a convenient and efficient method for the configuration inversion of C 2-hydroxy in lycorine .

Total synthesis of the natural product of crinumaquine / 药学实践杂志

Objective To complete the synthesis of the natural product of crinumaquine .Methods 3 ,4-methylenedioxy-phenethylamine and 2 ,5-dimthoxyphenylacetic were taken as starting material ,and chemical reactions of condensation ,cycliza-tion ,reduction ,oxidation and other reactions were conducted .Results and Conclusion The optimum synthetic route was deter-minedunder which the final yield rate was 73% .

Dietary restriction enhancesγ-aminobutyric acid and brain derived neurotrophic factor expression in the visual cortex of the cat / 解剖学报

Objective To explore the effect of DR on the expression of inhibitory neurotransmitter ,γ-aminobutyric acid ( GABA) and brain derived neurotrophic factor ( BDNF) in the primary visual cortex of young cats .Methods Totally 6 cats were wsed in this study . Nissl staining was used for cortical layer identification and cell counting . Immunohistochemical techniques were utilized to label GABA-and BDNF-positive neurons .Sections were observed under an Olympus light microscope and photographed with a digital camera .The cell density and absorbance of immunoreactivity were measured with Image-Pro Express 6.0 softwares .Results Our results showed that the mean density of Nissl-stained neurons in the primary visual cortex ( V1) of the DR group showed no significant difference from that of the control group . However , the mean density of GABA-immunoreactive neurons in each cortical layer of V 1 in DR cats was significantly higher than that in control cats .The mean immunoreactive intensity of GABA-positive neurons , as indicated by the average absorbance , increased significantly in DR cats relative to control ones . Accompanied with the elevation of GABA expression, DR enhanced BDNF expression in V1, as indicated by an increased mean density of BDNF-positive neurons and BDNF-immunoreactive average absorbance in DR cats relative to controls .Conclusion These results indicate that dietary restriction leads to a concurrent expression upregulation of GABA and BDNF , which may likely compensate for brain functional degradation during senescence and thus delay aging process .

Research progress in structural modification and pharmacological activities of berberine / 药学实践杂志

Berberine was an isoquinoline type alkaloid extracted from Chinese herbs such as Coptis chinensis.Recently, as a great many berberine derivatives had been synthesized with comprehensive physiological functions , the structural modification and ap-plication of berberine showed great promising significance .Recent literatures had been systematically analyzed and summarized in this review.With abundant pharmacological activities of berberine different sites ′derivatives had been presented , systematical information of berberine structural modification as a lead compound and new drug R&D were provided in this article .

Clinical value of multiband mucosectomy for the treatment of early esophageal cancer and precancerous lesions / 中华消化外科杂志

Objective To investigate the clinical value of multiband mucosectomy (MBM) for the treatment of early esophageal cancer and precancerous lesions.Methods The clinical data of 43 patients with early esophageal cancer or precancerous lesions (including 13 cases of early esophageal cancer and 30 cases of precancerous lesion) who were admitted to the Tengzhou Central People's Hospital from January 2010 to January 2011 were retrospectively analyzed.A total of 51 lesions were confirmed by preoperative endoscopy and mucosal biopsy,and then were treated by MBM.Results A total of 52 MBM procedures were carried out,and 180 lesions were resected.The sizes of the lesions ranged from 10 mm × 8 mm to 25 mm × 23 mm,and the mean operation time was (37 ± 5)minutes.The complete resection rate was 92.2％ (47/51).The submucosal layer of 1 patient was invaded by squamous cell carcinoma postoperatively,and the patient was treated by operation;1 patient wth squamous epithelium carcinoma was treated by radiotherapy at 2 weeks after MBM ; the other 2 lesions were treated by argon plasma coagulation (APC).Four lesions with bleeding were detected during 52 MBM procedures,and no esophageal perforation was detected during MBM.Early complications consisted of delayed bleeding (1 patient,cured by APC) and slight esophageal stenosis (1 patient,recovered at postoperative month 6).The accurate rate of pathological examinations was 51.0％ (26/51).Forty-three patients were followed up for 1 year,3 patients with tumor recurrence were treated by MBM or APC.No death occurred during the followup.Conclusion MBM is a safe and effective technique for the treatment of early esophageal cancer and precancerous lesions.

AGE-RELATED CHANGES OF GABAergic NEURONS AND ASTROCYTES IN CAT PRIMARY AUDITORY CORTEX / 解剖学报

Objective A morphometric study was carried out on GABAergic neurons and astrocytes in primary auditory cortex of 4 young cats (1-3 years old, 20-2.5 kg) and 4 old cats (10-13-year-old, 3-3.5 kg), in order to explore the age-related changes and the probably physical effects underlying these changes. Methods The same regions of the primary auditory cortex (AI) were comparatively studied. Nissl staining and immunohistochemical methods were applied to explore the differences of GABAergic neurons and astrocytes(specifically labeled by GFAP as a mark as antibody) in the primary auditory cortex(Al) between young and old cats. Serial cross-sections from two age groups were stained with Nissl for layer structure observation and demonstration of neurons; Adjacent sections were stained with anti_GABA immunohistochemistry for localizing and characterizing GABAergic and with anti-GFAP for astrocytes in AI. Results The diameter, density and number of GABAergic neurons in Al of old cats declined significantly compared with the counterpart in young cats, especially in layers Ⅱ,Ⅲ of AI; but the change in GFAP-IR cells was reversed: old cats showed clearly larger number and stronger staining of GFAP-IR cells than that in young cats. The GFAP-IR cell bodies and dendrites swelled obviously in old cats, especially in layer Ⅰ of AI and in white matter. Conclusion The result presented a direct morphological evidence for weakness of GABAergic intracortical inhibition, which is considered to be a possible mechanism for age-related acoustic function decline. The enhanced function of astrocytes may play an important role in decreasing the GABA content in AI of the old individuals.