Design, synthesis, and biological evaluation of N-(pyridin-3-yl)pyrimidin-4-amine analogues as novel cyclin-dependent kinase 2 inhibitors for cancer therapy.

The discovery and development of CDK2 inhibitors has currently been validated as a hot topic in cancer therapy. Herein, a series of novel N-(pyridin-3-yl)pyrimidin-4-amine derivatives were designed and synthesized as potent CDK2 inhibitors. Among them, the most promising compound 7l presented a broad antiproliferative efficacy toward diverse cancer cells MV4-11, HT-29, MCF-7, and HeLa with IC values of 0.

Paeoniflorin, the Main Monomer Component of Paeonia lactiflora, Exhibits Anti-inflammatory Properties in Osteoarthritis Synovial Inflammation.

Objective: To explore the mechanism of paeoniflorin (PF) on osteoarthritis (OA) synovial inflammation from network pharmacology to experimental pharmacology.

Methods: Targets of OA were constructed by detecting the database of network database platforms (Therapeutic Target database, DrugBank and GeneCards), and the targets of PF were constructed by PubChem and Herbal Ingredients' Targets database. Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) analysis of these co-targeted genes were conducted via Database for Annotation, Visualization, and Integrated Discovery (DAVID) database, and protein-protein interaction (PPI) networks were conducted via the search tool for the retrieval of interacting genes (STRING) database.

Urea-catalyzed N-Glycosylation of Amides/Azacycles with Glycosyl Halides.

The efficient synthesis of N-glycosides via direct N-glycosylation of amides/azacycles has been reported. The glycosylation of amides/azacycles with glycosyl halides in the presence of a catalytic amount of urea proceeded smoothly to provide the corresponding N-glycosylated amides or nucleosides in good to excellent yields with 1,2-trans-stereoselectivity. Moreover, by the addition of terpyridine, the 1,2-cis-stereoselectivity was achieved.

[Establishment and evaluation of rabbit model of closed tibial fracture].

Objective: To explore the effect of a modified three-point bending fracture device for establishing a rabbit model of closed tibial fracture.

Methods: The model of closed tibial fracture was established in 40 6-month-old male New Zealand white rabbits with a body weight of 2.5 to 3.

Toll-Like Receptor 9 Signaling Pathway Contributes to Intestinal Mucosal Barrier Injury in Mice With Severe Acute Pancreatitis.

Objectives: The purpose of this study was to investigate the role and mechanism of toll-like receptor 9 (TLR9) in intestinal mucosal barrier injury in mice with severe acute pancreatitis (SAP).

Methods: The mice were randomly divided into 3 groups: control group, SAP group, and TLR9 antagonist-treated group. The expression of tumor necrosis factor-α, interleukin-1β, interleukin-6, diamine oxidase, and endotoxin core antibodies were detected by enzyme-linked immunosorbent assay.

Efficacy and Safety of Acupuncture Combined with Herbal Medicine in Treating Gouty Arthritis: Meta-Analysis of Randomized Controlled Trials.

Background: Gouty arthritis is a common metabolic disease caused by long-term purine metabolism and elevated serum uric acid. In recent years, the incidence of gouty arthritis has been increasing year by year. As an effective method for treating gouty arthritis, acupuncture combined with herbal medicine has been widely used in clinical practice.

Advances in Experimental and Clinical Research of the Gouty Arthritis Treatment with Traditional Chinese Medicine.

Gouty arthritis (GA) is a multifactorial disease whose pathogenesis is utterly complex, and the current clinical treatment methods cannot wholly prevent GA development. Western medicine is the primary treatment strategy for gouty arthritis, but it owns an unfavorable prognosis. Therefore, the prevention and treatment of GA are essential.

Development of pteridin-7(8H)-one analogues as highly potent cyclin-dependent kinase 4/6 inhibitors: Synthesis, structure-activity relationship, and biological activity.

CDK4/6 have been validated as the cancer therapeutic targets. Here, we describe a series of pteridin-7(8H)-one analogues as potent CDK4/6 inhibitors. Among them, the most promising compound 7s demonstrated remarkable and broad-spectrum antiproliferative activities toward HCT116, HeLa, MDA-MB-231, and HT-29 cells with IC values of 0.

Responses of phytoliths in topsoil samples to temperature variation in temperate region.

Modern phytolith research is the premise to accurately reconstruct the regional paleovegetation and paleoclimate. It is thus particularly important to study the spatial distribution characteristics of the phytolith assemblages and the response of the phytolith to environmental factors. In this study, we collected 54 topsoil samples along the isohyet of 600 mm in Northeast China to examine the distribution patterns of phytolith along the gradient of single environmental factor.

Synthesis and antiproliferative evaluation of novel 8-cyclopentyl-7,8-dihydropteridin-6(5H)-one derivatives as potential anticancer agents.

Based on our previous work, a novel class of 8-cyclopentyl-7,8-dihydropteridin-6(5H)-one derivatives were synthesized and evaluated as antiproliferative agents. Structure-activity relationship analysis revealed that the greatest activities were achieved with a 4-(4-methylpiperazin-1-yl)aniline group at C-2 position of dihydropteridin-6(5H)-one core, and the most promising compound 6k demonstrated comparable antiproliferative activity with Palbociclib and more potent than our parent derivative 4 toward four cell lines including HCT-116, HeLa, HT-29, and MDA-MB-231 with IC values of 3.29, 6.

Gua sha therapy for chronic low back pain: A protocol for systematic review.

Background: Non-specific chronic low back pain (LBP) is a debilitating disease that profoundly impacts patients' daily physical function and quality of life. Gua sha therapy, as an easy-to-use and noninvasive complementary modality, has been widely used clinically in patients with non-specific chronic LBP. The aim of this study is to test the potential benefits and harms of gua sha therapy on patients with non-specific chronic LBP.

[Effect of (, TLZT) gel preparation on p53 /miR-502-5p /NF-κBp65 in synovial tissue of knee osteoarthritis].

Objective: To observe effects of (, TLZT) gel preparation on p53, miR-502-5p, NF-κBp65 in synovial tissue of knee osteoarthritis (KOA), and to explore mechanism of TLZT gel preparation in treating KOA.

Methods: Thirthy-six Wistar rats aged 8 weeks and weighed 200 to 220 g (meaned 208 g) were randomly divided into normal group, model group and traditional Chinese medicine (TCM) group, 12 rats in each group. KOA model was established by modified Hulth method.

Molecular characterization and functional analysis of a novel candidate of cuticle carboxylesterase in Spodoptera exigua degradating sex pheromones and plant volatile esters.

Odorant-degrading enzymes (ODEs) are considered to play key roles in odorant inactivation to maintain the odorant receptor sensitivity of insects. Some members of carboxylesterase (CXE) is a major sub-family of ODEs. However, only a few CXEs have been functionally characterized so far.

The benefits of expressive writing among newly diagnosed mainland Chinese breast cancer patients.

The study aimed to evaluate the effects of an expressive writing intervention on quality of life (QoL) among mainland Chinese breast cancer patients. A total of 118 Chinese breast cancer patients were randomly assigned to one of four groups: a cancer-facts writing condition (CTL group), an emotional disclosure writing condition (EMO group), a self-regulation writing condition (SR group), or a neutral control condition with no writing tasks (CON group). QoL was assessed by FACT-B at baseline, 3-, and 6-month follow-ups.

Genome-wide identification of chemosensory receptor genes in the small brown planthopper, Laodelphax striatellus.

The small brown planthopper (SBPH), Laodelphax striatellus is one of the major insect pests of rice, but little is known about the molecular-level means by which it locates its hosts. SBPH host-seeking behavior heavily relies on chemosensory receptors (CRs). In this study, we utilized genome analysis of the SBPH to identify 169 CRs, including: 133 odorant receptors (ORs), 13 gustatory receptors (GRs) and 23 ionotropic receptors (IRs).

[Lapidus operation combined with bone setting manipulation in treatment of hallux valgus in elderly patients].

Objective: To investigate the clinical effect of Lapidus operation combined with bone setting manipulation of traditional Chinese medicine in treating hallux valgus in elderly patients.

Methods: From March 2013 to October 2017, 53 elderly patients (87 feet) with hallux valgus were treated with Lapidus operation combined with bone-setting manipulation of traditional Chinese medicine, including 12 males (18 feet) and 41 females (69 feet), ranging in age from 65 to 92 years old, with an average of (76.3±4.

The impact of hydrochloric acid on the catalytic destruction behavior of 1,2-dichlorbenzene and PCDD/Fs in the presence of VWTi catalysts.

Catalytic oxidation is regarded an effective technique to control the emissions of chlorinated benzenes (CBzs) and polychlorinated dibenzo-p-dioxins and dibenzofurans (PCDD/Fs) from waste incinerators. Among the numerous factors affecting the degradation efficiency of CBzs and PCDD/Fs, limited attention has been paid to the impact of hydrochloric acid (HCl) present in the flue gas. This study investigates how HCl affects the catalytic degradation of 1,2-dichlorbenzene (1,2-DCBz) at different reaction times and temperature regimes.

Synthesis and biological evaluation of novel indole-pyrimidine hybrids bearing morpholine and thiomorpholine moieties.

Based on our previous screening hit compound 1, a series of novel indole-pyrimidine hybrids possessing morpholine or thiomorpholine moiety were synthesized via an efficient one-pot multistep synthetic method. The antiproliferative activities of the synthesized compounds were evaluated in vitro against four cancer cell lines including HeLa, MDA-MB-231, MCF-7, and HCT116. The results revealed that most compounds possessed moderate to excellent potency.

[Progress on establishment of animal model of osteoarthritis by intra-articular injection].

Osteoarthritis (Osteoarthritis, OA) is a common clinical degenerative joint disease with increased incidence rate in recent years. Animal experiment is one of the important ways to explore pathogenesis and treatment of OA, while induced animal model is the most important part in animal experiment. Intra-articular injection of drugs is a classical method for establishing animal model of OA.

[Soft tissue changes observed through musculoskeletal ultrasound in the treatment of knee osteoarthritis with needle-knife].

Objective: To study soft tissue changes observed through musculoskeletal ultrasound (MSUS) in the treatment of knee osteoarthritis with needle-knife, so as to provide MSUS basis for needle-knife in the treatment of knee osteoarthritis.

Methods: Forty patients with knee osteoarthritis treated in the Third Affiliated Hospital of Beijing University of Chinese Medicine from December 2011 to December 2012 were selected according to inclusion and exclusion criteria. All the patients were treated with needle-knife release method.

Clinical factors associated with postictal headache in Chinese patients with partial epilepsy.

Purpose: To investigate the incidence of postictal headache (PIH) and the factors potentially related to the occurrence of PIH in a Chinese epileptic center.

Methods: Consecutive adult patients with epilepsy, referred to the outpatient clinic of the Epilepsy Center of the PLA General Hospital between February 01, 2012, and May 10, 2013, were recruited to this study. 854 patients with partial epilepsy completed a questionnaire regarding headache, 466 patients with temporal lobe epilepsy (TLE), 82 patients with occipital lobe epilepsy (OLE) and 306 patients with frontal lobe epilepsy (FLE).

[Analysis of X-rays of cervical imbalances syndrome before and after the treatment of osteopathy and traction intervention in 187 youth cases].

Objective: To observe X-ray features of before and after treatment of cervical imbalance syndrome with osteopathy and traction intervention in youth patients, then to investigate the clinical effect of the treatment of the cervical imbalances syndrome in youth by osteopathy.

Methods: From September 2007 to December 2010, one hundred and eighty-seven students of 19 to 22 years (means 21 years) with neck pain as the main symptom in Beijing university of Chinese medicine were selected and divide them into osteopathy group and traction groups randomly. In osteopathy group, there were 94 patients including 40 males and 54 females; in traction group, there were 93 patients including 42 males and 51 females.

[Multiple linear regression analysis of X-ray measurement and WOMAC scores of knee osteoarthritis].

Objective: To perform Multiple Linear Regression analysis of X-ray measurement and WOMAC scores of knee osteoarthritis, and to analyze their relationship with clinical and biomechanical concepts.

Methods: From March 2011 to July 2011, 140 patients (250 knees) were reviewed, including 132 knees in the left and 118 knees in the right; ranging in age from 40 to 71 years, with an average of 54.68 years.

Targeted delivery of insoluble cargo (paclitaxel) by PEGylated chitosan nanoparticles grafted with Arg-Gly-Asp (RGD).

Poor delivery of insoluble anticancer drugs has so far precluded their clinical application. In this study, we developed a tumor-targeting delivery system for insoluble drug (paclitaxel, PTX) by PEGylated O-carboxymethyl-chitosan (CMC) nanoparticles grafted with cyclic Arg-Gly-Asp (RGD) peptide. To improve the loading efficiency (LE), we combined O/W/O double emulsion method with temperature-programmed solidification technique and controlled PTX within the matrix network as in situ nanocrystallite form.