Quantitative structure-activity relationships in MAO-inhibitory 2-phenylcyclopropylamines: Insights into the topography of MAO-A and MAO-B

Ten (E)-and (Z)-isomers of 2-phenylcyclopropylamine (PCA), 1-Me-PCA, 2-Me-PCA, N-Me-PCA, and N, N-diMe-PCA and fifteeno ⁻, m⁻, p⁻ isomers of (E)-PCA with substituents of Me, Cl, F, OMe, OH were synthesized in this laboratory and tested for the inhibition of rat brain mitochondrial MAO-A and MAO-B. The effects of substituents, their positions, and stereochemistry on the inhibition were assessed for the compounds with substituents at cyclopropyl and amino groups and QSAR analyses were performed using the potency data of ring-substituted compounds. The best correlated QSAR equations are as follows: pI₅₀=0.804 Π² Blo−1.069 Blm+0.334 Lp−1.709 HDp+7.897 (r=0.945, s=0.211, F=16.691, p=0.000) for the inhibition of MAO-A; pI₅₀=1.815 π-0.825 Π² R+0.900 Es²+0.869 Es³+0.796 Es⁴−0.992 HDp+0.562 HAo+3.893 (r=0.982, s=0.178, F=23.351, p=0.000) for the inhibition of MAO-B. Based on the potency difference between stereoisomers of cyclopropylamine-modified compounds and on QSAR results, it is proposed that the active sites of MAO-A are composed of one deep hydrophobic cavity near para position, two hydrophobic cavities interacting with Me group, a hydrophobic area accomodating phenyl and cyclopropyl backbone, steric boundaries, a hydrogen-acceptor site near para position, and an amino group binding site and that in addition to the same two hydrophobic cavities, hydrophobic area, steric boundaries, hydrogen-acceptor site, and amino group binding site, another steric boundary near para position and a hydrogen donating site near ortho position constitute active sites of MAO-B.     

Changes of Intestinal Caicitonin Gene-related Peptide in Acute Intestinal Radiation Sickness in Rats

The characteristic distribution of calcitonin gone-related peptide(CGRP)inthe small intestine of rats and its changes in acute intestinal radiation sickness(AIRS)were studied with immunocytochemistry(whole mount stretch preparations of the smallintestine and cryostat sections)and radio-immunoassay.It was found that in all the lay-ers of the intestinal walls,there were large amounts of CGRP immunoreactive(CGRP-I)nerve fibers which existed in especiaUy high density in the myenteric,submucosal andmucosal plexuses.There was also a rather high density of the nerves around the smallvessels of the small intestine and the intestinal crypts.Some CGRP-I neurons were seenin the myenteric and submucosal plexuses.In AIRS,the intestinal CGRP showed a dip-hasic change,in a lower level in the 24th h and a higher level in the 48th and 72nd h af-ter irradiation.The results indicate that CGRP may be related to the regulation of the motility,se-cretion,absorption,sensation,and regional blood flow of the gastrointestinal tract.Pro-bably,CGRP is released under the stress of AIRS and participates in the mechanism ofinjury through many ways especially through the influence on the regional blood flowand the increase of the permeability of blood vessels.     

定坤丹的显微鉴定研究

对定坤丹(蜜丸)进行了显微鉴定研究,将29种组成药物全部检出,对各组成药物的显微鉴别特征作了简明描述,并附显微特征图。     

自制新荧光剂EPQS的性能测试

作者对自制新荧光剂EPQS进行了性能测试。结果:量子产率为0.21;最大激发波长和荧光波长分别为375nm和484nm,stokes位移109nm;检测生物化合物常用的缓冲溶液对荧光峰位无影响,对荧光强度影响很小;温度的影响也小(18～43℃,FRI61.5～58.1),PH的影响也不大。说明EPQS不仅荧光参数好,而且稳定性也好。适合在较广泛的环境条件下使用。     

Solitary Small Hepatic Angiosarcoma: Initial and Follow-up Imaging Findings

We report an uncommon case of solitary, small hepatic angiosarcoma that was initially considered as a hemangioma. We present the imaging findings, with an emphasis on the initial and follow-up CT and MR findings, as well as report on the more suggestive findings of angiosarcoma than those of a hemangioma.     

Access to primary health care for Australian young people: service provider perspectives.

BACKGROUND: To adequately address the complex health needs of young people, their access to services, and the quality of services received, must be improved. AIMS: To explore the barriers to service provision for young people and to identify the training needs of primary healthcare service providers in New South Wales (NSW), Australia. DESIGN OF STUDY: A cross-sectional, qualitative study of the perspectives of a range of health service providers. SETTING: A range of primary healthcare organisations across NSW. METHODS: Samples of general practitioners (GPs), youth health workers, youth health coordinators, and community health centre staff were drawn from urban and rural clusters across NSW. Focus groups and interviews were used to identify barriers to service provision and the training needs of service providers. Data were tape recorded, transcribed, and analysed. RESULTS: Barriers to service provision among GPs and community health centre staff included inadequate time, flexibility, skills, and confidence in working with young people, and poor linkages with other relevant services. Training needs included better knowledge of and skills in adolescent health requirements, working with adolescents, and working with other services. Barriers to service provision for youth health workers and coordinators included lack of financial resources and infrastructure. There were few linkages between groups of service providers. CONCLUSION: Models of service provision that allow stronger linkages between service providers, sufficient time for consultation with young people, adequate training and support of health professionals, and flexibility of service provision, including outreach, should be explored and evaluated.     

壮骨肾宝对实验性小鼠高脂血症的影响

目的观察由黄芪、白术、淫羊藿组成的复方制剂(壮骨肾宝)对实验性小鼠高脂血症的影响。方法用蛋黄乳液快速致小鼠单纯性高胆固醇血症和喂养高脂饲料致高脂血症模型 ,观察预防性给予不同剂量的壮骨肾宝后对血清总胆固醇(TC)、甘油三酯(TG)和高密度脂蛋白胆固醇(HDL -ch)的影响。结果壮骨肾宝中、高剂量能使血清TC降低(P<0.05),HDL -ch升高(P<0.01) ,但对TG的影响不大。结论壮骨肾宝有一定降血脂作用 ,并与剂量有关     

THE HISTOLOGIC FEATURES AND HISTOGENESIS OF MALIGNANT OVARIAN BRENNER TUMOR

Eight cases of malignant and 12 0f benign Bren- ner tumor are reported, patient ages ranged 31 69 and 39-53 years. The malignant tumor was bilateral in 6 0f 8 cases, and the benign in l of 12. The greatest diameter of the malignant tumors averaged around 11 cm, and the benign 10. Six of the malignant Brenner tumor patients died, one was lost to follow up, and one survived for 10 years. Pathologic and microscopic findings were pre- sented in some detail. Based on the analysis of the association between the histologic features and type of Mullerian epithelium, we believe that the so called Brenner tumor is in effect a tumor arising from the Mullerian epithelium with a tendency to differentiate into vaginocervical type epithelium.