Synthesis of Novel Benzofuran Spiro-2-Pyrrolidine Derivatives via [3+2] Azomethine Ylide Cycloadditions and Their Antitumor Activity.

A synthetic strategy of a three-component spiro-pyrrolidine compound based on benzofuran via an [3+2] azomethine ylide cycloaddition reaction is reported herein. Under mild optimal conditions, this reaction can quickly produce potentially bioactive compounds with a wide range of substrates, high yield, and simple operation. The desired products were obtained with a yield of 74-99% and a diastereomeric ratio (dr) of >20:1.

Integrating metagenomics and culturomics to uncover the soil bacterial community in cultivation.

is a medicinal plant in China, which has gained attention owing its protective effect in human health. However, there are seldom studies to systematically reveal the rhizosphere bacterial community of . In this study, we employed metagenomics and culturomics to analyze the bacterial community composition and diversity in continuous rhizosphere soil of .

High-Strength Controllable Resin Plugging Agent and Its Performance Evaluation for Fractured Formation.

Lost circulation is a common and complicated situation in drilling engineering. Serious lost circulation may lead to pressure drop in the well, affect normal drilling operations, and even cause wellbore instability, formation fluid flooding into the wellbore, and blowout. Therefore, appropriate preventive and treatment measures need to be taken to ensure the safe and smooth operation of drilling operations.

NaIO/air-initiated phosphorylation of alcohols with H-phosphine oxides for the construction of P(O)-O bonds in water.

A facile and efficient protocol for P(O)-O bond formation was discovered through NaIO/air-initiated phosphorylation of alcohols with H-phosphine oxides in water. This reaction showed good functional group tolerance and a broad substrate scope, providing an alternative method for constructing P(O)-O bonds. Mechanistic studies suggested that a phosphoryl radical-involving process from H-phosphine oxides facilitated the phosphorylation of alcohols under air.

LncRNA CCAT1 knockdown suppresses tongue squamous cell carcinoma progression by inhibiting the ubiquitination of PHLPP2.

Tongue squamous cell carcinoma (TSCC) is prevailing malignancy in the oral and maxillofacial region, characterized by its high frequency. LncRNA CCAT1 can promote tumorigenesis and progression in many cancers. Here, we investigated the regulatory mechanism by which CCAT1 influences growth and metastasis of TSCC.

In-Field Tobacco Leaf Maturity Detection with an Enhanced MobileNetV1: Incorporating a Feature Pyramid Network and Attention Mechanism.

The maturity of tobacco leaves plays a decisive role in tobacco production, affecting the quality of the leaves and production control. Traditional recognition of tobacco leaf maturity primarily relies on manual observation and judgment, which is not only inefficient but also susceptible to subjective interference. Particularly in complex field environments, there is limited research on in situ field maturity recognition of tobacco leaves, making maturity recognition a significant challenge.

Fischer's base-triggered formal (3+2) cycloadditions with 3-isothiocyanato oxindoles as acceptor-donor synthons.

Herein, previously unreported Fischer's base reactants serving as useful 2C building blocks in (3+2) cycloaddition reactions to build a library of bispiro[Fischer's base-oxindole] hybrids are described. These structurally intriguing products containing three adjacent quaternary stereocentres were smoothly afforded in up to 82% yield and >20 : 1 dr under catalyst-free conditions. Notably, the present protocol firstly employs 3-isothiocyanato oxindole serving as an acceptor and then as a donor in the formal (3+2) cycloadditions, allowing practical, straightforward access to structurally diverse cycloadducts.

Structural Elucidation and Cytotoxic Activity of New Monoterpenoid Indoles from .

Two new monoterpenoid indole alkaloids, gelselegandines F () and G (), were isolated from the aerial parts of . Their structures were elucidated by means of spectroscopic techniques and quantum chemical calculations. The ECD calculations were conducted at the B3LYP/6-311G(d,p) level and NMR calculations were carried out using the Gauge-Including Atomic Orbitals (GIAO) method.

Effect of Enhanced Recovery after Surgery (ERAS) Concept and Cluster Nursing on Psychological State and Pain of Oral Outpatients Undergoing Root Canal Therapy.

Objective: The effect of the concept of enhanced recovery after surgery (ERAS) and pain of patients undergoing root canal therapy in oral clinic.

Methods: 200 participants in an oral clinic from March 2020 to March 2022 were enrolled in our study. The control group ( = 100) accepted ERAS-based care and the research group ( = 100) accepted ERAS concept and cluster nursing.

Pralsetinib treatment for multiple fusions in lung adenocarcinoma: a case report.

Despite recent advances in treatments and knowledge of biomarkers, patients with metastatic lung cancer have a 5-year survival rate of 5%. Rearranged during transfection () fusions occur in 1% to 2% of lung cancer patients. Pralsetinib has been used to treat non-small cell lung cancer with a single fusion; however, there have been no reports regarding its use in patients with multiple fusions.

Macrophages induce the expression of lncRNA ATB via the secretion of TGF-β to relieve ischemia-reperfusion injury in cardiomyocytes.

Cardiac ischemia-reperfusion can cause severe damage to cardiomyocytes. Previous studies have revealed that TGF-β can alleviate ischemia-reperfusion injury in cardiomyocytes by inducing the expression of long non-coding RNA (lncRNA) activated by TGF-β (ATB). However, M2 macrophages can secrete a large amount of TGF-β.

Identification of compounds with antipyretic effects and anti-endotoxin activity in different species of using spectrum-effect correlation.

Liquid chromatography (LC) is a common and straight forward approach used in the evaluation of the quality of Traditional Chinese Medicines (TCMs). Quality control is a critical step when systematically assessing the efficacy of TCMs. In the present study, the spectrum-effect correlation method was used to identify pharmacologically active substances.

Correlation between the coexpression of zinc finger and SCAN domain-containing protein 31 and transcriptional activator with PDZ-binding motif and prognosis in hepatocellular carcinoma.

Background: Transcriptional coactivator with PDZ binding motif (TAZ) regulates multiple biological processes and has been found to be related to hepatocellular carcinoma (HCC). However, common signaling pathways downstream after TAZ knockdown may also be important.

Methods: TAZ was knocked down in an HCC cell line, and its potential target genes were analyzed.

Genus Alangium - A review on its traditional uses, phytochemistry and pharmacological activities.

The species from Alangium have been used as folk medicine to treat rheumatism, skin diseases, diabetes by the people of Southeast Asia. Previous phytochemical studies have shown this genus are rich sources of alkaloids, glycosides, and terpenoids, which have attracted considerable attention of many researchers due to their markedly diverse and complex architecture. The crude extracts as well as the monomeric compounds from the title genus possess anti-tumor, anti-inflammatory, antibacterial, anti-oxidant pharmacological activities.

Study on antitumor activities of the chrysin-chromene-spirooxindole on Lewis lung carcinoma C57BL/6 mice in vivo.

The our previous study synthesized the chrysin-chromene-spirooxindole hybrids 3, and further found compound 3e had good antitumor activity against A549 cells in vitro through multi-target co-regulation of the p53 signalling pathway to inhibit the proliferation of A549 cells. This study was designed to evaluate the antitumor effects of compound 3e on Lewis lung carcinoma of C57BL/6 mice in vivo. Compound 3e significantly inhibited the growth of transplanted tumors in C57BL/6 mice and induced the apoptosis of tumor cells.

Regioselective synthesis and evaluation of 2-amino 3-cyano chromene-chrysin hybrids as potential anticancer agents.

The first example of Ca(OH)-activated p-regioselective synthesis of chrysin-fused chromene was reported through a cascade Michael/cyclization of chrysin and arylidenemalononitrile. The newly synthesized structurally diverse 2-amino 3-cyano chromene-chrysin hybrids 3 were evaluated for their in vitro anticancer activity, and some of the compounds showed stronger anti-proliferative activity against K562, PC-3, A549 and NCI-H1299 than parent compound chrysin, and demonstrated equipotent potency compared with the reference drug of cisplatin. In particular, compound 3h had the highest cytotoxicity towards K562 cells (IC = 6.

Melatonin suppresses epithelial‑to‑mesenchymal transition in the MG‑63 cell line.

Epithelial‑to‑mesenchymal transition (EMT) is a major process involved in tumor progression and metastasis. Melatonin is secreted by the pineal gland and has been documented as a potential therapeutic agent for multiple tumors. However, the effects of melatonin on EMT during osteosarcoma (OA) development remain undefined.

Thermal-mediated [1,3]-hydrogen transfer as the key step: access to oxindole-chromone hybrid collection with structural diversity.

Inspired by the chemistry and biology of chromone and oxindole derivatives, herein we report the first example of thermal-mediated [1,3]-hydrogen transfer as the key step for the efficient synthesis of oxindole-chromone hybrid collections 2, which avoids additional catalyst and solvent conditions. All the oxindole-chromones 2 are smoothly obtained in >99% yields in all cases, avoiding column chromatography purification. In particular, the products 2 can act as potential synthons for further elaboration in structural diversity, which might be valuable in organic and medicinal chemistry.

The potential value of CDV3 in the prognosis evaluation in Hepatocellular carcinoma.

CDV3 is correlated with tumorigenesis and may affect some biological process in cancer. In this study, we explore the role of CDV3 in HCC. According to the TCGA data base, CDV3 is over-expressed in HCC tissues.

Packed-Nanofiber solid phase extraction coupled with gas chromatography-mass spectrometry for the determination of phthalate esters in urines from children.

In this paper, we developed a rapid and safe method based on packed-fiber solid-phase extraction (PFSPE) system coupled with gas chromatography-mass spectrometry for the determination of four phthalate esters (PAEs), diethyl-o-phthalate (DEP), dibutyl-o-phthalate (DBP), di (2-ethylhexyl) phathalate (DEHP), di-n-octyl phthalate (DNOP), in urine samples. The PAEs in urine samples (500μL) were rapidly cleaned up from urines using polystyrene (PS) nanofibers packed micro-columns fitted on a PFSPE pretreatment device, which can process up to 12 samples simultaneously in 5min. Under optimum conditions, satisfied recovery and relative standard deviation values (RSDs) were in the range of 80.

Simultaneous quantification of cortisol and cortisone in urines from infants with packed-fiber solid-phase extraction coupled to HPLC-MS/MS.

Cortisol and cortisone are two important glucocorticoids in human body, their interconversion is controlled by two isotypes of 11β-hydroxy steroid dehydrogenase (11β-HSD1 and 11β-HSD2). The ratio of urinary cortisol to cortisone can be used to assess the activity of 11β-HSDs. An analytical method to quantify urinary cortisol and cortisone using high performance liquid chromatographic tandem mass spectrometry following a packed-fiber solid-phase extraction (PFSPE) was developed.

β-elemene regulates endoplasmic reticulum stress to induce the apoptosis of NSCLC cells through PERK/IRE1α/ATF6 pathway.

Endoplasmic reticulum stress (ERs) has been regarded as an important cause for the pathogenesis of non-small-cell lung cancer (NSCLC). β-elemene is an active component in the essential oil extracted from a medicinal herb, Curcuma wenyujin, and has been reported to be effective against non-small-cell lung cancer (NSCLC). However, the potential effect and underlying mechanisms of β-elemene on regulating ERs to inhibit NSCLC are still unclear.

Rapid, microwave-accelerated synthesis and anti-osteoporosis activities evaluation of Morusin scaffolds and Morusignin L scaffolds.

Described herein is a facile and efficient methodology toward the synthesis of Morusin scaffolds and Morusignin L scaffolds 4-9 and 12via a novel three-step approach (Michael addition or prenylation, cyclization and cyclization) and use a rapid, microwave-accelerated cyclization as the key step. Furthermore, their biological activities have been preliminarily demonstrated by in vitro evaluation for anti-osteoporosis activity. These Morusin, Morusignin L and newly synthesized compounds 5b, 6a, 8e, 8f greatly exhibited the highest potency, especially at the 10mol/L (P<0.

Clinical observation of laser ablation combined with chemotherapy in postoperative colorectal cancers with liver metastasis.

Background: This study is to evaluate the efficacy and adverse reaction of a combination therapy of chemotherapy and laser thermal ablation (LTA) on liver metastases from colorectal cancer.

Methods: Eighty-five cases colorectal cancer liver metastases were assigned to the treatment group (43 cases) and to the control group (42 cases). The treatment group patients received LTA combined with FOLFIRI regimen chemotherapy, and the control group patients only received FOLFIRI regimen chemotherapy.