Synthesis of C3'-Foused Aryl/Penta-1,4-Dien-3-One/Amine Hybrids as HSP90C-Terminal Inhibitors.

24 C3'-focused hybrids of aryl/penta-1,4-dien-3-one/amine (APDA) were designed and synthesized. Of these hybrids, 2 n demonstrated improved antiproliferative effects on HER2-positive breast cancer cells (SKBr3 and BT474) and triple-negative breast cancer (TNBC) cells (MDA-MB-231 and MDA-MB-468) with IC values ranging from 7.45 to 10.

A silicon-containing aryl/penta-1,4-dien-3-one/amine hybrid exhibits antiproliferative effects on breast cancer cells by targeting the HSP90 C-terminus without inducing heat-shock response.

A pharmacophore-hybridized strategy based on previously reported HSP90 C-terminal inhibitors was utilized to prepare 32 aryl/penta-1,4-dien-3-one/amine hybrids. Among them, a silicon-containing compound 1z exhibited remarkable broad-spectrum antiproliferative effects on various human breast cancer cell lines. Through fluorescence polarization and AlphaScreen-based assays, we demonstrated that 1z specifically inhibited the HSP90 C-terminus without affecting HSP90 N-terminus.

Evaluating tacrolimus treatment in idiopathic membranous nephropathy in a cohort of 408 patients.

Background: The KDIGO Clinical Practice Guidelines for Glomerulonephritis recommended tacrolimus as an alternative regimen for the initial therapy for Idiopathic membranous nephropathy (IMN), however, large observational studies evaluating tacrolimus treatment in IMN remains rare.

Methods: A total of 408 consecutive IMN patients with nephrotic syndrome who were treated with tacrolimus in Jinling Hospital were included. The effectiveness and safety of tacrolimus treatment in IMN were analyzed in this study.

[Analysis of chemical speciation of heavy metals in L07-11 profile sediments of "Big Ear" Region of Lop Nor Lake].

As playa is the typical characteristic in "Big Ear" Region of Lop Nor Lake, it is significant for enriching playa heavy metal earth environmental chemical data by analyzing species distribution of heavy metal among this district. In this thesis, heavy metal Cd, Pb, Ni, Cu in L07-11 Profile Sediments of "Big Ears" Region of Lop Nor Lake are considered as research objects. Tessier sequential extraction and Graphite furnace atomic absorption method (GF-990) are used to discuss and analyze five forms of Cd, Pb, Ni, Cu among sediments.

Clinicopathological characteristics and outcomes of pediatric patients with systemic small blood vessel vasculitis.

Background: Systemic small blood vessel vasculitis (SSV) is uncommon among pediatric patients, and the predictive value of the new histopathological classification for SSV in terms of renal outcomes in these patients is unknown.

Methods: The study cohort comprised 38 pediatric patients and 285 adult patients with SSV who were treated in a medical center between 1993 and 2012.

Results: Children accounted for 11.

Heart-type fatty acid binding protein is associated with proteinuria in obesity.

Rationale: Lipid metabolism contributes to the formation of obesity-related glomerulopathy (ORG). Heart-type fatty acid binding protein (H-FABP or FABP3) is involved in lipid metabolism and was predicted to relate to renal lesions in obesity.

Methods: A total of 28 patients with ORG were investigated, and renal tissue from 7 kidney donors served as controls.

[Analysis of Cd pollution & spatial variability characteristics of typical agricultural soils in suburbs of Urumqi City, Xinjiang].

Cd content in agricultural soils from 4 townships in north suburb and 2 townships in south suburb of Urumqi City was determined with graphite furnace (GF-990) atomic absorption spectrometry, and the spatial variability of Cd content there was analyzed with geo-statistics method. The result indicates that Cd content from the sampling points in north suburb exceeds the stipulated standard and falls into medium or strong spatial variability with nugget value > 75%, which explains a weak self-correlation among those variable spaces under mainly the impact of random factors of external pollution such as local fertilization level, irrigation and cultivation etc. Cd content from the sampling points in north suburb does not exceed the stipulated standard but approaches to the critical warning value with nugget value at 50.

[Speciation analysis of Cd in PM10 and PM2.5 during heating period in Urumqi].

PM2.5 and PM10 samples were collected on campus of Xinjiang Agricultural University during Dec. 14-28, 2009, and the speciation of Cd in PM10 and PM2.

[Research on the relevance of earthworms inducing soil Cd2+ absorbed by perennial ryegrass].

Through the method of simulating the heavy metal pollution in farmland, the graphite oven (GF-990) atomic absorption was used for analyzing the regulations of the earthworms inducing the soil Cd2+ absorbed by the perennial ryegrass. The result indicated: (1) under the circumstance of the soil Cd2+ density of 3-6 mg x kg(-1), the positive relevance appeared extremely remarkably that the contents of Cd2+ in underground portions of the perennial ryegrass relate to the earthworm quantity (r = 0.883 2-0.

[Comparative analysis of endogenous hormones between two species of Ammopiptanthus seedlings around germination and under Pb2+ stress].

The changes in three endogenous hormones, phytohormones gibberrelic acid (GA3), indoles-3-acid (IAA) and abscisic acid (ABA), were studied around germination and under tress of different density of Pb2+ between two species of Ammopiptanathus. It was found that (1) around germination, in Xinjiang Ammopiptanthus the rate IAA decreased 77.80%, and the rate of ABA decreased 98.

Triptolide reduces proteinuria in experimental membranous nephropathy and protects against C5b-9-induced podocyte injury in vitro.

Membranous nephropathy is a major cause of nephrotic syndrome in adults where podocyte injuries were found to mediate the development of proteinuria. Triptolide, a major active component of Tripterygium wilfordii Hook F, has potent immunosuppressive, anti-inflammatory and antiproteinuric effects. To study its antiproteinuric properties, we established an experimental rat model of passive Heymann nephritis and a C5b-9 injury model of podocytes in vitro.

Mercury-induced membranous nephropathy: clinical and pathological features.

Background And Objectives: Long-term contact with mercury may induce membranous nephropathy (MN); however, the clinical pathologic features and pathogenesis of mercury-induced MN have not been investigated.

Design, Setting, Participants, & Measurements: The present study retrospectively evaluated 11 cases of mercury-induced MN to analyze its causes and its clinical and pathologic features.

Results: A total of 10 women and 1 man ages 15 to 45 years were enrolled in the present study.

[Analysis of the microelements contents in melons and fruits of Xinjiang].

Through the atom absorption and emission spectrum analysis, it is detected 8 trace elements contents in eleven species of melons and fruits in Xinjiang. On comparative analysis with biological standard of China, it is found that the zinc quantity in apples is 66.75 mg x kg(-1), the strontium quantity in jujubes is 8.

Triptolide protects podocytes from puromycin aminonucleoside induced injury in vivo and in vitro.

Extracts of Tripterygium wilfordii Hook F have been used to treat glomerulonephritis for more than 30 years in China with dramatic antiproteinuric effects. Triptolide, a diterpene triepoxide, is one of the major active components of these extracts. To clarify its antiproteinuric effects we induced podocyte injury by puromycin aminonucleoside.

[The corn seedlings are affected by the heavy metal Pb2+].

The corn seedlings in hydroponic culture are treated with the lead acetate solutions of various concentrations, the content of Pb2+ in the roots, stems and leafs of the corns at 10th day, 20th day and 30th day is measured. The analyzing conclusions are that the contents of Pb2+ in the corns display a sequence of root>leaf>stem, the contains of chlorophyll in corns fall off, the raising of Pb2+ in solutions, the membrane penetrability of the corns increased along a sequence of root>leaf>stem, and the harmful rate of Pb2+ display a sequence of root>leaf>stem in corns. The data of the study gives some references for the further researches of the crops, relating the endurance and the distributing of corns with Pb2+.