Identification of Selective Imidazopyridine CSF1R Inhibitors.

Colony stimulating factor-1 receptor (CSF1R or c-FMS), a class III receptor tyrosine kinase expressed on members of the mononuclear phagocyte system (MPS), plays a key role in the proper functioning of macrophages, microglia, and related cells. Aberrant signaling through CSF1R has been associated with a variety of disease states, including cancer, inflammation, and neurodegeneration. In this Letter, we detail our efforts to develop novel CSF1R inhibitors.

Effect of blackberry anthocyanins and its combination with tea polyphenols on the oxidative stability of lard and olive oil.

To investigate the protective effect of blackberry anthocyanins (BA), tea polyphenols (TP), and their binary mixture on the oxidative stability of edible oils during storage, BA, TP, and their binary mixture were added to lard and olive oil. The changes in peroxide value (PV), thiobarbituric acid reactive substances (TBARS), acid value (AV), and scavenging capacity of DPPH and ABTS of oil samples were evaluated during accelerated storage. BA were found to have a remarkable capability to enhance antioxidant properties, delay lipid oxidation, and inhibit the deterioration both of lard and olive oil at high-temperature processes.

Five blueberry anthocyanins and their antioxidant, hypoglycemic, and hypolipidemic effects .

The dual epidemic of obesity and diabetes mellitus is becoming an important worldwide public health issue. "Diabesity" is the term used to describe the combined detrimental health effects of both diabetes mellitus and obesity/overweight. Currently, food-derived bioactive compounds are suggested to alleviate diabesity.

[Effect of Antibiotic-Degrading Bacteria on Maturity and Bacterial Community Succession During Pig Manure Composting].

The inoculation of antibiotic-degrading bacteria into manure could promote the removal of antibiotics during composting. However, knowledge on the impact of inoculating these antibiotic-degrading bacteria on the composting process and indigenous microbial community succession is still limited. This study assessed the antibiotic removal efficiency in pig manure after inoculating a microbial inoculum with antibiotic-degrading bacteria as the key component.

Impacts of androgen deprivation therapy on the risks and outcomes of SARS-CoV-2 infection in patients with prostate cancer.

Studies have investigated the effects of androgen deprivation therapy (ADT) use on the incidence and clinical outcomes of coronavirus disease 2019 (COVID-19); however, the results have been inconsistent. We searched the PubMed, Medline, Cochrane, Scopus, and Web of Science databases from inception to March 2022; 13 studies covering 84 003 prostate cancer (PCa) patients with or without ADT met the eligibility criteria and were included in the meta-analysis. We calculated the pooled risk ratios (RRs) with 95% confidence intervals (CIs) to explore the association between ADT use and the infection risk of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) and severity of COVID-19.

Functionality of Silk Cocoon ( L.) Sericin Extracts Obtained through High-Temperature Hydrothermal Method.

Sericin, a textile waste, can be used for antioxidant and skin-whitening purposes. The hydrothermal method of extracting sericin is more eco-friendly than are chemical and enzymatic methods. In this study, silk cocoons were cut into pieces and then subjected to hydrothermal extraction at three temperatures (160, 200, and 220 °C) to obtain sericin extracts (Sericin160, Sericin200, and Sericin220, respectively).

A Solid Supported Membrane-Based Technology for Electrophysical Screening of BAT1-Modulating Compounds.

Classical high-throughput screening (HTS) technologies for the analysis of ionic currents across biological membranes can be performed using fluorescence-based, radioactive, and mass spectrometry (MS)-based uptake assays. These assays provide rapid results for pharmacological HTS, but the underlying, indirect analytical character of these assays can be linked to high false-positive hit rates. Thus, orthogonal and secondary assays using more biological target-based technologies are indispensable for further compound validation and optimization.

Modulation of gut microbiota protects against viral respiratory tract infections: a systematic review of animal and clinical studies.

Background: Earlier studies suggest that probiotics have protective effects in the prevention of respiratory tract infections (RTIs). Whether such benefits apply to RTIs of viral origin and mechanisms supporting the effect remain unclear.

Aim: To determine the role of gut microbiota modulation on clinical and laboratory outcomes of viral RTIs.

tiRNAs: A novel class of small noncoding RNAs that helps cells respond to stressors and plays roles in cancer progression.

tRNA-derived stress-induced RNAs (tiRNAs), important components of tRNA-derived fragments, are gaining popularity for their functions as small noncoding RNAs involved in cancer progression. Under cellular stress, tiRNAs are generated when mature tRNA is specifically cleaved by angiogenin and suggested to act as transducers or effectors involved in cellular stress responses. tiRNAs facilitate cells to respond to stresses mainly via reprogramming translation, inhibiting apoptosis, degrading mRNA, and generating stress granules.

Purple sweet potato anthocyanin exerts antitumor effect in bladder cancer.

Bladder cancer (BC) is the most common malignant disease. The developing of economically sustainable and available agents for the treatment of BC is required. Purple sweet potato anthocyanin (PSPA) has been shown to have antitumor abilities.

Natural Triterpenoids for the Treatment of Diabetes Mellitus: A Review.

Triterpenoids, an important group of secondary metabolites, are widely distributed in nature. Many triterpenoids have been found with potential therapeutic effect against diabetes mellitus. However, the use of triterpenoids for the treatment of diabetes has not been systematically discussed previously.

Detection and Toxicity Evaluation of Pyrrolizidine Alkaloids in Medicinal Plants Gynura bicolor and Gynura divaricata Collected from Different Chinese Locations.

Two edible plants in Southeast Asia, Gynura bicolor and G. divaricata, are not only known to be nutritive but also useful as medicinal herbs. Previous phytochemical investigation of Gynura species showed the presence of hepatotoxic pyrrolizidine alkaloids (PAs), indicating the toxic risk of using these two plants.

Simultaneous determination of five triterpene acids in rat plasma by liquid chromatography-mass spectrometry and its application in pharmacokinetic study after oral administration of Folium Eriobotryae effective fraction.

Folium Eriobotryae effective fraction (FEA), the extract of Folium Eriobotryae, had been used as anti-hyperglycemia and anti-hyperlipemia medicine in China. A previous study indicated that euscaphic acid, maslinic acid, corosolic acid, oleanolic acid and ursolic acid, the five structurally similar triterpene acids (containing two groups of structural isomers), are the major components of FEA. In the present study, we developed a specific and reliable LC-MS method for simultaneous determination of the five triterpene acids in rat plasma, and further investigated their pharmacokinetic properties after oral administration of FEA.

Natural flavonoids as potential herbal medication for the treatment of diabetes mellitus and its complications.

Diabetes mellitus, together with its various complications, is becoming a serious threat to human health. Natural products are secondary metabolites widely distributed in plants, having a broad range of biological activities. The development of antidiabetic medication from natural products, especially those originating from plants with a traceable folk-usage history in treating diabetes, is receiving more attention.

[Response surface optimization of ultrasonic-assisted pigment extraction from Coreopsis tinctoria].

Response surface methodology (RSM) was used to optimizing the ultrasonic-assisted extraction technology of pigment from Coreopsis tinctoria. The results showed that the flavonoids were the main constituents of the pigment Based on single factor experiments, a four-factor-level experiment design were developed by box-benhnhen central composite design method with causal factors of ultrasonic temperature, ultrasonic time, ratio of liquid to raw material, the concentrations of ethanol in solvent and the extract absorbance value for the response. The interactive effects of four crucial technological parameters were assessed by response surface methodology (RSM).

[Preparation of solid dispersion of triterpenoid acids from Eriobotrya japonica leaf and study on their dissolution in vitro].

Unlabelled: To prepare the solid dispersion of Eriobotrya japonica leaf triterpenoid acids(EJA) in order to enhance their dissolution characteristics in vitro.

Methods: Taking ursolic acid and oleanolic acid in vitro dissolution as an indicator, the influence of factors including different water-soluble carriers (PEG 6000, PVPk30 and P188) and the drug/carrier weight ratio for the preparation of solid dispersion were examined using single factor experiment. Differential scanning calorimetry (DSC) and X-ray diffraction (X-RD) were used to describe the characterization of solid dispersion.

Profiling and elucidation of the phenolic compounds in the aerial parts of Gynura bicolor and G. divaricata collected from different Chinese origins.

Gynura bicolor and G. divaricata are not only known to be nutritive as cultured vegetables, but also beneficial as folk medicines in East Asia. As demonstrated by the current phytochemical knowledge, the genus Gynura is a promising source of phenolics with multiple medicinal activities.

Sulfonic acid functionalized nano-γ-Al2O3: a new, efficient, and reusable catalyst for synthesis of 3-substituted-2H-1,4-benzothiazines.

A simple and efficient synthetic protocol has been developed for the synthesis of 3-substituted-2H-1,4-benzothiazines by using a novel sulfonic acid functionalized nano-γ-Al2O3 catalyst, devoid of corrosive acidic, and basic reagents. The developed method has the advantages of good to excellent yields, short reaction times, operational simplicity, and a recyclable catalyst. The catalyst can be prepared by a simple procedure from inexpensive and readily available nano-γ-Al2O3 and has been shown to be recoverable and reusable up to six cycles without any loss of activity.

One-pot synthesis of 2'-aminobenzothiazolo-arylmethyl-2-naphthols catalyzed by NBS under solvent-free conditions.

To develop a new facile protocol for the synthesis of 2'-aminobenzothiazolo-arylmethyl-2-naphthol derivatives, N-bromosuccinimide (NBS) was used as an efficient catalyst for the one-pot synthesis of 2'-aminobenzothiazolo-arylmethyl-2-naphthols in excellent yields from β -naphthol (1 mmol), aromatic aldehydes (1 mmol), and 2-aminobenzothiazole (1 mmol) at 60°C under solvent-free conditions.

Analysis of genetic variability and relationships among Mentha L. using the limonene synthase gene, LS.

The genus Mentha comprises a group of aromatic plants with worldwide distribution. Because of frequent interspecific hybridization, the genetic relationships within the genus are not clearly understood. Limonene synthase, which catalyses the first committed step in the essential oil monoterpene biosynthetic pathway, is considered to be a possible rate limiting enzyme.

Chemical constituents from the aerial parts of Gynura bicolor.

Gynura bicolor (Willd.) DC., is used in folk recipes for the treatment of diabetes mellitus in Jiangsu, Zhejiang and Sichuan province in the south of China.

Investigation of the volatile constituents of different Gynura species from two Chinese origins by SPME/GC-MS.

GC-MS analyses of the volatile constituents obtained by solid phase microextraction (SPME) of two Gynura species, i.e., G.

Studies on the chemical constituents of Anabasis aphylla L.

The investigation on the chemical constituents of Anabasis aphylla L. was carried out by using various chromatographies, such as silica gel, Sephadex LH-20 and RP-C18 column chromatography. Further detailed investigation on the fraction of the ethanol extract of Anabasis aphylla L.

Two new prenylated isoflavones from Sedum aizoon L.

Investigation of a methanol extract from the Chinese endemic species Sedum aizoon L. led to the isolation of two new isoflavone derivatives that were named sedacin A and B (1 and 2). Their structures were elucidated by the basis of spectroscopic analysis.

The anti-hyperglycemic effect of plants in genus Gynura Cass.

Gynura divaricata (L.) DC and G. bicolor DC are used as secret recipes to treat diabetes mellitus in some parts of China.