Bioisosterism: Interchange of 4-OH to 4-NH2 in vanillin or homovanillin ring of capsaicinoids

A series of 4-amino Capsaicin analogs 15, 17 and 19 were prepared to investigate the bioisosteric effect of 4-amino group, and all these compounds exhibited moderate or weak potency from their analgesic test. From our previous results and others, 4-hydroxyl group as well as 3-methoxy substituent could be crucial for high analgesic activity. This biological result also shows that the activity is sensitive to alkyl chain length in hydrophobic region and the phenylacetic amides 19 are more active than the corresponding urea derivatives 17.     

The application of Ion chromatographic method for bioavailability and stability test of iron preparations

Postabsorptive serum iron level was determined after oral administration of the compounds to human. In serum and whole blood, Fe3+ was measured by ion chromatography (IC) using a pyridine-2,6-dicarboxylic acid (PDCA) as an eluent. The serum sample solutions were pretreated with I N HCI and 50% TCA. The whole blood sample solutions were treated with 3 N HCI for 30 min at 125 degrees C. The limit of detection (LOD) of the IC technique is 0.2 microM for Fe2- and 0.1 microM for Fe3+. The area under concentration (AUC) can be obtained by the above analytical condition. In addition, to compare the stability of Fe2+ to that of Fe3+ in pharmaceutical preparations, accelerated stability test was carried out. After storing the samples under 40 degrees C, 75%RH in light-resistant container for various time intervals, the contents of iron of different valencies were determined separately by the IC technique and the change and/or the interchange of among those iron species in preparations was investigated. Iron raw materials are stable, but Fe2+ in Fe3+ source materials was slightly converted to Fe3+ by oxidation. Fe2+ in Fe3+ source raw materials and Fe3+ in Fe2+ raw materials are determined as impurities. Therefore, IC technique is found to be an appropriate method for comparative evaluation of dissimilar bioavailability of Fe2+ and Fe3+, stability of Fe2+ and Fe3+ raw materials and preparations.     

论吴鞠通治疳学术思想

吴鞠通《温病条辨·解儿难》对疳疾的论治文短义深,所提治疳九妙法蕴藏着深奥的学术思想。本文从脾胃学说、升降出入学说、营卫学说等方面进行了阐发,以期能发掘其学术渊薮,指导学术研究及临床实践。     

半夏厚朴汤及其组成中药抗焦虑和抑郁研究进展

目的：综述半夏厚朴汤及其组成中药抗焦虑和抑郁研究进展。方法：查阅国内外近年来有关文献结合相关的研究成果，从半夏厚朴汤对动物焦虑和抑郁行为、神经生化机制、免疫系统功能、血脂代谢、机体氧化防御系统等层次进行阐述。结果与结论：半夏厚朴汤及其组成中药抗焦虑和抑郁具有一定的科学性。     

Interleukin-6 activates phosphatidylinositol-3 kinase, which inhibits apoptosis in human prostate cancer cell lines

BACKGROUND: A number of recent studies have identified interleukin (IL)-6 as an important regulator of prostate cancer growth. Here, we investigate the potential interaction of IL-6 with phosphatidylinositol (PI)-3 kinase, a key growth regulatory enzyme, in prostate cancer cell lines. METHODS: Tyrosine phosphorylation of p85, the regulatory subunit of PI-3 kinase, in the human prostate cancer cell lines LNCaP and PC-3 was assessed by sequential immunoprecipitation with anti-p85 antibody and immunoblotting with anti-phosphotyrosine. The effects of wortmannin, an inhibitor of PI-3 kinase, and/or IL-6 on cell growth were assessed by MTT assays. DNA laddering experiments were performed to assay for programmed cell death. RESULTS: Tyrosine phosphorylation of p85 is upregulated by IL-6 in both LNCaP and PC-3. IL-6 promotes coprecipitation of p85 with gp130, the signal-transducing component of the IL-6 receptor. Inhibition of PI-3 kinase with wortmannin induces programmed cell death in PC-3 cells. In contrast, wortmannin has no effect on LNCaP growth when used alone; however, combined with IL-6, wortmannin promotes apoptosis in these cells. CONCLUSIONS: PI-3 kinase is involved in IL-6 signal transduction and delivers an antiapoptotic signal in human prostate cancer cell lines.     

Epithelioid trophoblastic tumor of the uterus in a postmenopausal woman: a case report and review of the literature

We report an epithelioid trophoblastic tumor (ETT), a recently delineated type of gestational trophoblastic tumor (GTT), discovered in the uterus of a 66-year-old woman. She had been treated for a hydatidiform mole 17 years previously without chemotherapy. The resected uterus contained a solid/cystic tumor located entirely within the myometrium. Microscopically, there was an epithelial-like growth pattern. The tumor was circumscribed, with a pushing border, and the tumor cells grew in cords, nests, and sheets within which were aggregates of hyaline material and necrotic debris. Most tumor cells were mononuclear and had an epithelioid appearance with distinct cell borders, eosinophilic cytoplasm, and nuclei with occasional indistinct nucleoli. Scattered multinucleated cells consistent with syncytiotrophoblastic cells were also present. Immunohistochemical staining revealed strong diffuse reactivity for cytokeratins (CK7, AE1/AE3, CAM 5.2, CK18) and epidermal growth factor receptor, and focal reactivity, mainly in syncytiotrophoblastic cells, for beta-human chorionic gonadotropin, human placental lactogen, and inhibin-alpha. The histologic and immunohistochemical features were characteristic of ETT, and helped to distinguish the tumor from other trophoblastic tumors and squamous cell carcinoma. An unusual observation was a high mitotic count, reflected in a Ki-67 proliferative index of 68.6%. Our findings indicate that ETT, like other types of GTT, can occur in postmenopausal women, even years after a gestational event.     

外周原始神经外胚层肿瘤形态学免疫表型及临床预后研究

目的：探讨外周原始神经外胚层肿瘤(PNET)的临床表现，病理及免疫组织化学特点及预后。方法：对15例外周原始神经外胚层肿瘤进行临床资料及预后，病理组织形态学和超微结构特点及免疫组化表型研究。结果：患者以男性为主，男女之比约为6．5：1，年龄6～35岁，年龄中位数为16，发生部位较多，可发生在直肠，腹膜后，腹股沟，淋巴结，胸壁，睾丸，鼻腔及骨组织等；免疫组化：肿瘤均弥漫表达CD99，并不同程度地表达NSE，SYN，CgA等，但不表达CK，Desmin，LCA等，其中1例表达组织化学染色PAS，随访最长时间为24月。结论：PNET是一种发生在年轻男性，进展迅速，预后非常差的恶性小圆细胞肿瘤，认识其临床病理特点及免疫组化表型对于该恶性肿瘤的诊断及临床治疗意义重大。