Structure-activity relationship study of new carbazole sulfonamide derivatives as anticancer agents with dual-target mechanism.

A series of novel carbazole sulfonamide derivatives were synthesized and evaluated for antiproliferative activity. Among them, compounds 7 and 15 showed strong potency (IC values of 0.81-31.

Assessing Aptamer-Analyte Binding Kinetics by Microfluidic Fluorescence Microscopy.

Kinetic measurement plays a crucial role in understanding aptamer binding mechanisms and identifying appropriate aptamers for clinical and research applications. Current techniques, while well established, generally require large sample volumes, bulky and expensive instruments operated by trained personnel, and are hence not readily accessible to resource-limited research laboratories. This paper presents a fluorescence microscopy-based microfluidic assay for measuring aptamer-analyte binding kinetics in a simple and cost-effective manner.

Study on CO source identification and spontaneous combustion warning concentration in the return corner of working face in shallow buried coal seam.

Coal spontaneous combustion is a common problem faced by many coal mines. Spontaneous combustion in goaf releases a large amount of harmful gases, polluting the environment while causing a large amount of wasted resources, and even endangering the lives of workers. Due to the collapse of the interior of the mining area, it is impossible to measure the internal gas composition directly.

Hepatic-Specific FGF21 Knockout Abrogates Ovariectomy-Induced Obesity by Reversing Corticosterone Production.

Increased glucocorticoid (GC) levels act as a master contributor to central obesity in estrogen-depleted females; however, what factors cause their increased GC production is unclear. Given (1) liver fibroblast growth factor 21 (FGF21) and GCs regulate each other's production in a feed-forward loop, and (2) circulating FGF21 and GCs are parallelly increased in menopausal women and ovariectomized mice, we thus hypothesized that elevation of hepatic FGF21 secretion causes increased GGs production in estrogen-depleted females. Using the ovariectomized mice as a model for menopausal women, we found that ovariectomy (OVX) increased circulating corticosterone levels, which in turn increased visceral adipose expression, thus causing visceral obesity in females.

The prevention effects of cryptotanshinone nanoemulsion on postoperative peritoneal adhesions.

The purpose of this study was to prepare a novel cryptotanshinone-loaded nanoemulsion (Cry LN) and to evaluate its prevention effect on the postoperative peritoneal adhesions (PPA). The Cry LN was prepared by high-pressure homogenization method, and various methods were used to investigate the physicochemical properties. The results showed that Cry LN has nanoscale particle size with uniform distribution and could slowly release the incorporated drug compared with Cry solution.

Preparation of Ru(ii)@oligonucleotide nanosized polymers as potential tumor-imaging luminescent probes.

The development of Ru(ii) complexes as luminescent probes has attracted increasing attention in recent decades. In this study, the nanosized polymers of two Ru(ii) complexes [Ru(phen)(dppz)](ClO) (1, phen = 1,10-phenanthrolin; dppz = dipyrido[3,2-:2',3'-]phenazine) and [Ru(phen)(Br-dppz)](ClO) (2, Br-dppz = 11-bromodipyrido[3,2-:2',3'-]phenazine) with oligonucleotides were prepared and investigated as potential tumor-imaging probes. The formation of the nanosized polymers, which had an average width of 125-438 nm and an average height of 3-6 nm, for 1 and 2@oligonucleotides were observed through atomic force microscopy.

Evaluation of Tanshinone IIA Developmental Toxicity in Zebrafish Embryos.

Tanshinone IIA (Tan-IIA) is derived from the dried roots of Bunge, a traditional Chinese medicine. Although has been applied for many years, the toxicity of the mono-constituent of , tanshinone IIA, is still understudied. This study evaluated the cardiotoxicity and developmental malformations of Tan-IIA by using zebrafish normal embryos and dechorionated embryos.

Inhibition of PKR protects against HO-induced injury on neonatal cardiac myocytes by attenuating apoptosis and inflammation.

Reactive oxygenation species (ROS) generated from reperfusion results in cardiac injury through apoptosis and inflammation, while PKR has the ability to promote apoptosis and inflammation. The aim of the study was to investigate whether PKR is involved in hydrogen peroxide (HO) induced neonatal cardiac myocytes (NCM) injury. In our study, NCM, when exposed to HO, resulted in persistent activation of PKR due to NCM endogenous RNA.

Ruthenium(II) Complexes as Potential Apoptosis Inducers in Chemotherapy.

Herein, the development of ruthenium complexes as potential apoptosis inducers, as well as their underlying mechanism has been reviewed. In recent years, various ruthenium complexes have been designed and their in vitro and in vivo inhibitory activities against various types of tumor cells have been evaluated extensively. It's demonstrated that ruthenium complexes can induce apoptosis of tumor cells through the signal pathway of mitochondria-mediated, death receptor-mediated, and/or endoplasmic reticulum (ER) stress pathways.

Efficacy and mechanism of tanshinone IIA liquid nanoparticles in preventing experimental postoperative peritoneal adhesions in vivo and in vitro.

Up to 90% of patients develop adhesion following laparotomy. Upregulating fibrinolysis within the peritoneum reduces adhesions. Tanshinone IIA (Tan IIA) promotes fibrinolysis in hepatic fibrosis and the cardiovascular system and may play a role in preventing adhesions.

Prevention of experimental postoperative peritoneal adhesions through the intraperitoneal administration of tanshinone IIA.

Postoperative adhesions develop after nearly every abdominal surgery. The formation of adhesions is associated with the inflammatory response, fibrinolytic system, and extracellular matrix deposition in response to injury. Tanshinone IIA is one of the major extracts obtained from Salvia miltiorrhiza, which has anti-inflammatory effects on many diseases.

Receptor-mediated, tumor-targeted gene delivery using folate-terminated polyrotaxanes.

Safe and effective gene delivery is essential to the success of gene therapy. We synthesized and characterized a novel nonviral gene delivery system in which folate (FA) molecules were functioned as blockers on cationic polyrotaxanes (PR) composed of poly(ethylenimine) (PEI)(600)-grafted α-cyclodextrin rings linearized on polyethylene glycol to form FA-terminated PR-PEI(600) (FPP). The FA terminal caps of FPP target cell surfaces abundant in FA receptor (FR), a common feature of tumor cells.

Paeoniflorin inhibits growth of human colorectal carcinoma HT 29 cells in vitro and in vivo.

The aim of the therapy of human malignancies is the inhibition of cell proliferation and/or induction of apoptosis. In present experiment, we investigated the in vitro and in vivo anticancer effects and associated mechanisms of paeoniflorin (PF), isolated from the paeony root, against colorectal cancer. In vitro, cell growth assay obviously showed the inhibition of tumor cell growth in a dose-dependent manner.

Hypoglycemic efficacy of pulmonary delivered insulin dry powder aerosol in rats.

Aim: To observe the hypoglycemic efficacy of pulmonary delivery of insulin in dry powder aerosol form.

Methods: Insulin dry powder, made of insulin and other proper materials, was insufflated in rat lung from an incision in the throat. Meanwhile, insulin injection was administered to other rats.