Design, synthesis and cytotoxic activity of novel lipophilic cationic derivatives of diosgenin and sarsasapogenin.

Novel lipophilic cationic derivatives including quaternary ammonium salt and triphenylphosphine series were designed and synthesized using diosgenin (1) and sarsasapogenin (2) as substrates to improve the cytotoxicity and selectivity. Most of the derivatives showed higher cytotoxicity against all cancer cell lines tested, compound 13 exhibited the most superior activity against A549 cells with an IC value of 0.95 μM, which was 34-fold of diosgenin.

Four new steroidal glycosides from Lilium lancifolium Thunb. and their antitumor activity.

Four new steroidal glycosides (1-4), including two steroidal saponins named lililancifoloside B and C (1-2), one pregnane glycoside named lililancifoloside D (3), and one C22-steroidal lactone glycoside named lililancifoloside E (4), together with five known ones (5-9), were isolated from the bulbs of Lilium lancifolium Thunb. By using spectroscopic analysis, including 1D, 2D NMR, and HR-ESI-MS, the structures of 1-4 were elucidated. All isolates were tested for their cytotoxic potential against the MCF-7, MDA-MB-231, HepG2, and A549 cell lines.

Jaridon 6, a new diterpene from Rabdosia rubescens (Hemsl.) Hara, can display anti-gastric cancer resistance by inhibiting SIRT1 and inducing autophagy.

Tumor resistance is the main cause of treatment failure and is associated with many tumor factors. Jaridon 6, a new diterpene extracted from Rabdosia rubescens (Hemsl.) Hara, which has been previously extracted by our research team, has been tested having more obvious advantages in resistant tumor cells.

[Up-Regulation of PI3K/Akt Signaling Pathway in H929 Cell Line by Doxycycline Not Beneficial to Its Anti-Myeloma Effect].

Objective: To investigate the effect and possible mechanism of up-regulation of p-Akt by doxycycline (DOX) on myeloma cell line H929.

Methods: Multiple myeloma cell line H929 was treated with DOX at different concentrations for different times, and cell proliferation rate was measured by CCK-8 assay. The protein expression level of p-Akt, PTEN, p-PDK1, p-mTOR, p-GSK-3β, and p-BAD was analyzed by Western blot.

An effective classifier based on convolutional neural network and regularized extreme learning machine.

An effective classifier combining convolutional neural network and regularized extreme learning machine (called as CNN-RELM) is presented in this paper. Firstly, CNN-RELM trains the convolutional neural network (CNN) using the gradient descent method until the learning target accuracy reaches. Then the fully connected layer of CNN is replaced by regularized extreme learning machine (RELM) optimized by genetic algorithm and the rest layers of the CNN remain unchanged.

Generation and characterization of a paclitaxel-resistant human gastric carcinoma cell line.

The main aim of this study was to establish a novel paclitaxel (PTX)-resistant human gastric carcinoma cell line and to investigate its biological significance. A cell line, MGC803/PTX, was established by gradually increasing PTX density on the basis of MGC803 over a period of 10 months. In addition, a pair of resistant cell lines (SW620 and SW620/PTX) were added to further explain the resistant mechanism of PTX.

Folded short azapeptide for conformation switching-based fluorescence sensing.

Herein, we report a conformation switching-based fluorescence sensing scheme using dipeptide-based amidothioureas (azapeptides) that contain a folded β-turn structure. Amidothiourea is equipped at its two termini with an electron acceptor and an electron donor or two fluorophores, such that it exhibits enhanced exciplex or excimer emission because of the turn structure in which the two termini are brought into close proximity; on the other hand, it exhibits a dramatic ratiometric fluorescence response upon anion binding to the thiourea moiety because of the resultant extended conformation of the anion binding complex.

Structure-Activity Relationship Studies of β-Lactam-azide Analogues as Orally Active Antitumor Agents Targeting the Tubulin Colchicine Site.

We have synthesized a series of new β-lactam-azide derivatives as orally active anti-tumor agents by targeting tubulin colchicine binding site and examined their structure activity relationship (SAR). Among them, compound 28 exhibited the most potent antiproliferative activity against MGC-803 cells with an IC value of 0.106 μM by induction of G2/M arrest and apoptosis and inhibition of the epithelial to mesenchymal transition.

Profiling methyl jasmonate-responsive transcriptome for understanding induced systemic resistance in whitebark pine (Pinus albicaulis).

RNA-seq analysis on whitebark pine needles demonstrated that methyl jasmonate (MeJA)-triggered transcriptome re-programming substantially overlapped with defense responses against insects and fungal pathogens in Pinus species, increasing current knowledge regarding induced systemic resistance (ISR) to pathogens and pests in whitebark pine. Many whitebark pine populations are in steep decline due to high susceptibility to mountain pine beetle and the non-native white pine blister rust (WPBR). Resistance, including induced systemic resistance (ISR), is not well characterized in whitebark pine, narrowing the current options for increasing the success of restoration and breeding programs.

Gene expression profiling and pathway network analysis of anti-tumor activity by Jaridon 6 in esophageal cancer.

Jaridon 6, a novel ent-kaurene diterpenoid derived from Rabdosia rubescens (Hemsl.) Hara, possesses strong anti-tumor activity in esophageal cancer cells. In this study, we explored the underlying molecular events of the anti-tumor activity of Jaridon 6.

Characterization of Five Novel Mitoviruses in the White Pine Blister Rust Fungus Cronartium ribicola.

The white pine blister rust (WPBR) fungus Cronartium ribicola (J.C. Fisch.

Changes of ribbon synapses number of cochlear hair cells in C57BL/6J mice with age(Δ).

To investigate the changes of ribbon synapses (RS) number in cochlear hair cells in C57BL/6J mice with age. Basilar membranes within the cochlea of C57BL/6J mice aged 2, 6, 10 and 12 months were harvested (5 mice in each age group). The presynaptic and postsynaptic membranes were subject to double immunohistochemical staining and observed with a laser confocal microscope.

Effects of silencing the ATP-binding cassette protein E1 gene by electroporation on the proliferation and migration of EC109 human esophageal cancer cells.

In the present study, the gene expression of ATP-binding cassette protein E1 (ABCE1) in the EC109 human esophageal cancer cell line was silenced using electroporation to examine the effect if the ABCE1 gene on the growth migration and cell cycle of cancer cells. The small interference (si)RNA sequence of ABCE1 was designed and synthesized to transfect the EC109 cells by electroporation. The mRNA and protein expression levels of ABCE1 were then detected by reverse transcription quantitative polymerase chain reaction (RT-qPCR) and western blot analysis.

Radiosensitivity enhancement by arsenic trioxide in conjunction with hyperthermia in the EC-1 esophageal carcinoma cell line.

Objective: To explore the effect on radiosensitivity of arsenic trioxide (As₂0₃) in conjunction with hyperthermia on the esophageal carcinoma EC-1 cell line.

Method: Inhibition of EC-1 cell proliferation at different concentrations of As₂0₃ was assessed using the methyl thiazolyl blue colorimetric method (MTT method), with calculation of IC₅₀ value and choice of 20% of the IC₅₀ as the experimental drug concentration. Blank control, As₂0₃, hyperthermia, radiotherapy group, As₂0₃ + hyperthermia, As₂0₃ + radiotherapy, hyperthermia + radiotherapy and As₂0₃ + hyperthermia + radiotherapy groups were established, and the cell survival fraction (SF) was calculated from flat panel colony forming analysis, and fitted by the 'multitarget click mathematical model'.

[Analysis of prognostic factors in 68 patients with cancer of unknown primary site].

Objective: The aim of this study was to analyze the clinical characteristics and prognostic factors in patients with cancer of unknown primary site (CUP).

Methods: The clinical and follow-up data of 68 CUP patients (46 adenocarcinoma patients, 22 squamous cell carcinoma patients), were retrospectively analyzed. Univariate and multivariate analysis were conducted to determine the correlation of survival with clinical features, tumor markers, blood test, liver function and so on.

[Effects of Qingshi Cream on chronic dermatitis-eczema in mice].

Objective: To explore the effects of Qingshi Cream, a compound traditional Chinese herbal medicine, on chronic dermatitis-eczema in mice induced by 2,4-dinitrochlorobenzene (DNCB).

Methods: Thirty BALB/C mice were randomly divided into vaseline group, 0.1% mometasone furoate cream group and Qingshi Cream group.