Design, synthesis, antibacterial evaluation of isopropylamine linked with different substituted phenol and piperazine novel derivatives.

BACKGROUND: Xanthomonas oryzae pv. oryzae (Xoo) is often considered one of the most destructive bacterial pathogens causing bacterial leaf blight (BLB), resulting in significant yield and cost losses in rice. In this study, a series of novel derivatives containing the isopropanolamine moiety linked to various substituted phenols and piperazines were designed, synthesized and screened. RESULTS: Antibacterial activity results showed that most compounds had good inhibitory effects on Xoo, among which compound W2 (EC50 = 2.74 µg mL-1) exhibited the most excellent inhibitory activity, and W2 also had a certain curative effect (35.89%) on rice compared to thiodiazole copper (TC) (21.57%). Scanning electron microscopy (SEM) results indicated that compound W2 could cause rupture of the Xoo cell membrane. Subsequently, proteomics and quantitative real-time polymerase chain reaction revealed that compound W2 affected the physiological processes of Xoo and may exert antibacterial activity by targeting the two-component system pathway. Interestingly, W2 upregulated Xoo's methyltransferase to impact on its pathogenicity. CONCLUSION: The present study offers a promising phenolic-piperazine-sopropanolamine compound as an innovative antibacterial strategy by specifically targeting the two-component system pathway and inducing upregulation of methyltransferase to effectively impact Xoo's pathogenicity. © 2024 Society of Chemical Industry.

Syndecan-2 modulates the YAP pathway in epithelial-to-mesenchymal transition-related migration, invasion, and drug resistance in colorectal cancer.

Epithelial-to-mesenchymal transition (EMT) is associated with an invasive phenotype in colorectal cancer (CRC). Here, we examined the roles of YES-associated protein (YAP) and syndecan-2 (SDC2) in EMT-related progression, invasion, metastasis, and drug resistance in CRC. The expression levels of YAP and SDC2 in CRC patient tumor tissue were quantified by PCR and western blotting. EMT-associated characteristics were assessed using Transwell assays and immunohistochemistry. Co-immunoprecipitation, glutathione S-transferase pull-down, and luciferase reporter assays were used to assess interactions between YAP and SDC2. YAP was found to be highly expressed in tumor tissue from 13/16 CRC patients, while SDC2 was highly expressed in the tumor tissue of 12/16 CRC patients. Overexpression of YAP in colon cancer cells led to increased cell viability, invasion, migration, and oxaliplatin resistance demonstrating that YAP plays a role in EMT. In addition, overexpression of YAP led to decreased expression of the large tumor suppressor kinase 1 (LATS1) and mammalian sterile 20-like kinases (MST1/2). Decreased LATS1 expression was associated with increased levels of cell proliferation. Knockdown of YAP by shRNA interference led to decreased cell invasion, migration, and drug resistance in colon cancer cells and reduced tumorigenesis in a mouse xenograft model. Finally, we established that YAP interacted with SDC2, and demonstrated that SDC2 mediated the YAP pathway through the EMT-related factors BMP4, CTGF and FOXM1.

Novel 2-Amino-1,4-Naphthoquinone Derivatives Induce A549 Cell Death through Autophagy.

A series of 1,4-naphthoquinone derivatives containing were synthesized as anti-cancer agents and the crystal structure of compound 5a was confirmed by X-ray diffraction. In addition, the inhibitory activities against four cancer cell lines (HepG2, A549, K562, and PC-3) were tested, respectively, and compound 5i showed significant cytotoxicity on the A549 cell line with the IC50 of 6.15 µM. Surprisingly, in the following preliminary biological experiments, we found that compound 5i induced autophagy by promoting the recycling of EGFR and signal transduction in the A549 cell, resulting in the activation of the EGFR signal pathway. The potential binding pattern between compound 5i and EGFR tyrosine kinase (PDB ID: 1M17) was also identified by molecular docking. Our research paves the way for further studies and the development of novel and powerful anti-cancer drugs.

Subtotal colonic bypass plus colostomy with antiperistaltic cecoproctostomy for the treatment of slow transit constipation in an aged population: A retrospective control study.

AIM: To compare the efficacy, improved quality of life, and prognosis in patients undergoing either subtotal colonic bypass with antiperistaltic cecoproctostomy (SCBAC) or subtotal colonic bypass plus colostomy with antiperistaltic cecoproctostomy (SCBCAC) for the treatment of slow transit constipation. METHODS: Between October 2010 and October 2014, aged patients with slow transit constipation who were hospitalized and underwent laparoscopic surgery in our institute were divided into two groups: the bypass group, 15 patients underwent SCBAC, and the bypass plus colostomy group, 14 patients underwent SCBCAC. The following preoperative and postoperative clinical data were collected: gender, age, body mass index, operative time, first flatus time, length of hospital stay, bowel movements (BMs), Wexner fecal incontinence scale, Wexner constipation scale (WCS), gastrointestinal quality of life index (GIQLI), numerical rating scale for pain intensity (NRS), abdominal bloating score (ABS), and Clavien-Dindo classification of surgical complications (CD) before surgery and at 3, 6, 12, and 24 mo after surgery. RESULTS: All patients successfully underwent laparoscopic surgery without open surgery conversion or surgery-related death. The operative time and blood loss were significantly less in the bypass group than in the bypass plus colostomy group (P = 0.007). No significant differences were observed in first flatus time, length of hospital stay, or complications with CD > 1 between the two groups. No patients had fecal incontinence after surgery. At 3, 6, and 12 mo after surgery, the number of BMs was significantly less in the bypass plus colostomy group than in the bypass group. The parameters at 3, 6, 12, and 24 mo after surgery in both groups significantly improved compared with the preoperative conditions (P < 0.05), except NRS at 3, 6 mo after surgery in both groups, ABS at 12, 24 mo after surgery and NRS at 12, 24 mo after surgery in the bypass group. WCS, GIQLI, NRS, and ABS significantly improved in the bypass plus colostomy group compared with the bypass group at 3, 6, 12, and 24 mo after surgery (P < 0.05) except WCS, NRS at 3, 6 mo after surgery and ABS at 3 mo after surgery. At 1 year after surgery, a barium enema examination showed that the emptying time was significantly better in the bypass plus colostomy group than in the bypass group (P = 0.007). CONCLUSION: Laparoscopic SCBCAC is an effective and safe procedure for the treatment of slow transit constipation in an aged population and can significantly improve the prognosis. Its clinical efficacy is more favorable compared with that of SCBAC. Laparoscopic SCBCAC is a better procedure for the treatment of slow transit constipation in an aged population.

Rapid spread of a recently introduced virus (tomato yellow leaf curl virus) and its vector Bemisia tabaci (Hemiptera: Aleyrodidae) in Liaoning Province, China.

In Liaoning Province, China, tomato yellow leaf curl virus (TYLCV) was first detected in 2009 and in only four counties. To quantify the spread of TYLCV and to identify potential factors influencing its spread in Liaoning Province, we assayed for TYLCV within 1,055 whiteflies (Bemisia tabaci (Gennadius) complex) from 74 populations and 29 counties in 2011. The B. tabaci species of these individuals was determined based on molecular markers. TYLCV was found in 13 counties (Donggang, Liaoyang, Kazuo, Lingyuan, Heishan, Liaozhong, Kaiyuan, Taian, Dawa, Dashiqiao, Beizhen, Linghai, and Xingcheng) and was most frequently detected in the central plain. In addition, the percentage of whiteflies with TYLCV was significantly higher in B. tabaci Q than in B. tabaci B but was unrelated to the hosts (pepper, eggplant, tomato, cucumber, and kidney bean) on which the whiteflies had been collected. These results demonstrate that TYLCV has spread rapidly in Liaoning Province since its first detection and suggest that its spread is more closely associated with the introduction of B. tabaci Q than with the species of host plant. These findings also indicate that controls are now needed to reduce the further spread of TYLCV and that these controls should include the management of B. tabaci Q populations.