Heterocycle-functional steroidal derivatives: Design, synthesis, bioevaluation and SARs of steroidal pyrazolo[1,5-a]pyrimidines as potential ALK inhibitors.

Two series of heterocyclic steroidal pyrazolo[1,5-a]pyrimidines derived from dehydroepiandrosterone (DHEA) and epiandrosterone (EPIA) were designed and synthesized, and these compounds were screened for their potential antiproliferation activities. The preliminary bioassay indicated that some of target compounds exhibited significantly good antiproliferation activities against human melanoma cell line (A875) and human hepatocellular carcinoma (Huh-7) cell lines compared with 5-fluorouracil (5-FU), and some of which present good antiproliferative activities as potential ALK inhibitors. The detailed analysis of structure-activity relationships (SARs) based on the inhibition activities, kinase assay, and molecular docking demonstrated that the antiproliferation activities of these steroidal pyrazolo[1,5-a]pyrimidine might be affected by the β-hydroxyl group of steroidal scaffold and the N atom of pyridine heterocycle.

BSC2 modulates AmB resistance via the maintenance of intracellular sodium/potassium ion homeostasis in Saccharomyces cerevisiae.

Previous studies on BSC2 have shown that it enhances yeast cell resistance to AmB via antioxidation and induces multidrug resistance by contributing to biofilm formation. Herein, we found that BSC2 overexpression could reverse the sensitivity of pmp3Δ to AmB and help the tested strains restore the intracellular sodium/potassium balance under exposure to AmB. Meanwhile, overexpression of the chitin gene CHS2 could simulate BSC2 to reverse the sensitivity of pmp3Δ and nha1Δ to high salt or AmB.

Contrast-enhanced ultrasound for the preoperative prediction of pathological characteristics in breast cancer.

Objective: We aimed to investigate the value of contrast-enhanced ultrasound (CEUS) in the preoperative prediction of the histological grades and molecular subtypes of breast cancer.

Methods: A total of 183 patients with pathologically confirmed breast cancer were included. Contrast enhancement patterns and quantitative parameters were compared in different groups.

The Effect of Empagliflozin on Janus Kinase 2/Signal Transducer and Activator of Transcription 3 Pathway in Patients with Type 2 Cardiorenal Syndrome.

Background: Empagliflozin (EMPA) demonstrates cardioprotective effects on the patients with heart failure, but its effects in cardiorenal syndrome (CRS) remain unspecified. The purpose of the exploratory study was to investigate the effect of EMPA on patients with type 2 CRS and type 2 diabetes mellitus (DM).

Methods: This study was a randomized trial of patients with type 2 CRS and DM done between December 2020 and January 2022.

Copper(I)-Catalyzed Three-Component Selenosulfonation of Maleimides with Sulfonyl Hydrazides and Diselenides via Radical Relay.

By employing Cu(CHCN)PF as the catalyst and -butyl hydroperoxide as the oxidant, we realized a three-component radical selenosulfonation of substituted maleimides, sulfonyl hydrazides, and diphenyl diselenides, providing a series of 3,4-selenosulfonylated succinimides in moderate to good yields. This reaction features broad substrate scopes, high functional-group tolerability, and feasibility of gram-scale synthesis, enabling one-step construction of C-SO and C-Se bonds under mild reaction conditions. Preliminary mechanistic studies support the free-radical-induced pathway.

BSC2 induces multidrug resistance via contributing to the formation of biofilm in Saccharomyces cerevisiae.

Biofilm plays an important role in fungal multidrug resistance (MDR). Our previous studies showed that BSC2 is involved in resistance to amphotericin B (AMB) through antioxidation in Saccharomyces cerevisiae. In this study, the overexpression of BSC2 and IRC23 induced strong MDR in S.

Iodine-Catalyzed Regioselective Oxidative Cyclization of Aldehyde Hydrazones with Electron-Deficient Olefins for the Synthesis of Mefenpyr-Diethyl.

A regioselective synthesis of polysubstituted dihydropyrazoles and pyrazoles through an iodine-catalyzed oxidative cyclization strategy of aldehyde hydrazones with electron-deficient olefins is described. The protocol adopts very mild reaction conditions and provides desirable yields. The reaction is supposed to proceed via a cascade C-H functionalization, C-N bond formation, and oxidation sequential processes.

Mass spectrometry-based proteomic analysis reveals the interacting partners of lipin1.

As a lipin family founding member, lipin1 exerts dual functions as a phosphatidate phosphatase enzyme and/or a co-transcriptional regulator in lipid metabolism. In fact, it is also involved in many other cell processes. In this study, we utilized pull down assay coupled with mass spectrometry (MS) to unravel protein-protein interaction networks of lipin1 in 293T human embryonic kidney cells.

OLE1 reduces cadmium-induced oxidative damage in Saccharomyces cerevisiae.

Cadmium has been shown to be an important environmental pollutant. Our previous studies have shown that the regulation of OLE1 in the synthesis of unsaturated fatty acids may act as a positive feedback mechanism to help yeast cells counter the lipid peroxidation and cytoplasmic membrane damage induced by cadmium. However, the involvement of OLE1 in cadmium-induced oxidative stress is still unclear.

Studies on the acaricidal mechanism of the active components from neem (Azadirachta indica) oil against Sarcoptes scabiei var. cuniculi.

Octadecanoic acid-3,4-tetrahydrofuran diester, isolated from neem (Azadirachta indica) oil, exhibited potent acaricidal activity against Sarcoptes scabiei var. cuniculi. In this paper, the acaricidal mechanism of octadecanoic acid-3,4-tetrahydrofuran diester against Sarcoptes scabiei var.

Three new xanthones from the resin of Garcinia hanburyi.

Three new xanthones, 22,23-dihydroxydihydrogambogenic acid (1), 12-hydroxygambogefic acid A (2), and hanburixanthone (3), along with thirteen known compounds were isolated from the resin of Garcinia hanburyi. The structures of the new compounds were determined by detailed analysis of 1D and 2D NMR spectra and by comparison with related model compounds. All compounds were tested for their cytotoxicities against A549, HCT116, and MDA-MB-231, and most of them showed significant effects on the cell lines.

Cytotoxic alkoxylated xanthones from the resin of Garcinia hanburyi.

Three new xanthones, garcinolic acid (1), 10α-ethoxy-9,10-dihydromorellic acid (2), and 10α-ethoxy-9,10-dihydrogambogenic acid (3), along with six known compounds were isolated from the resin of Garcinia hanburyi. These compounds were tested for their cytotoxicities against A549, HCT116, SK-BR-3 and HepG2, and showed high inhibitory effects on the cell lines.

3-Eth-oxy-carbonyl-2-hy-droxy-6-meth-oxy-4-methyl-benzoic acid.

The title compound, C(12)H(14)O(6), a substituted isophthalic acid monoester which was isolated from the lichen Thamnolia vermicularis var. subuliformis, displays intra-molecular carbox-yl-meth-oxy O-H⋯O and hy-droxy-carboxyl O-H⋯O hydrogen-bonding inter-actions. The terminal methyl group of the ethyl ester is disordered over two sets of sites with occupancies of 0.

Acaricidal activity of petroleum ether extract of neem (Azadirachta indica) oil and its four fractions separated by column chromatography against Sarcoptes scabiei var. cuniculi larvae in vitro.

The petroleum ether extract of neem oil and its four fractions separated by column chromatography was diluted at different concentrations with liquid paraffin. The acaricidal bioassay was conducted using a dipping method. The results indicated that the median lethal concentration (LC50) of the petroleum ether extract (at the concentration of 500.

Composition analysis and application of degradation products of whole feathers through a large scale of fermentation.

Purpose: Feathers are one of the most abundant bioresources. They are discarded as waste in most cases and could cause environmental pollution. On the other hand, keratin constituted by amino acids is the main component of feathers.

A new lignan and other constituents from Zanthoxylum armatum DC.

A new lignan (1), named armatumin, along with 25 known compounds, was isolated from Zanthoxylum armatum. The structure of compound 1 was elucidated using spectroscopic methods. Compounds 7, 8, 11, 13, 16, 20 and 21 were first isolated from Z.

Antinociceptive and anti-inflammatory activities of ethyl acetate fraction from Zanthoxylum armatum in mice.

Zanthoxylum armatum DC. is a traditional Chinese medicine that is prescribed to alleviate pain and treat inflammatory disorders. This species is distributed mainly in the southeast and southwest regions of China.

[Study on purification of total flavonoids from seed residue of Hippophae rhamnoides with macroporous resin].

Objective: To study the conditions and parameters of purifying total flavonoids from seed residue of H. rhamnoides.

Method: Absorption capacity of three resins for total flavonoids was compared.

[Effect of flavonoids from the seed and fruit residue of Hippophae rhamnoides L. on glycometabolism in mice].

Objective: To investigate the effect of flavonoids from the seed residue and fruit residue of Hippophae rhamnoides L. (FSH and FFH) on glycometabolism in mice.

Method: The healthy male mice were randomly divided into control group, three FSH treatment groups and three FFH treatment groups.