Copper-Catalyzed Domino-Double Annulation of o-Aminobenzamides with 2-Iodoisothiocyanates for the Synthesis of 12H-Benzo[4,5]thiazolo[2,3-b]quinazolin-12-ones.

A facile and efficient copper-catalyzed domino-double annulation strategy was developed from easily accessible o-aminobenzamides and 2-iodoisothiocyanates, which affords a direct pathway for the synthesis of tetracyclic fused 12H-benzo[4,5]thiazolo[2,3-b]quinazolin-12-ones in moderate to good yields without the addition of ligands, bases, and external oxidants. The reaction involves a C-N bond cleavage and the formation of a C-N/C-S bond in one step with the advantages of using an inexpensive copper catalyst and easy operation. Mechanistic studies suggest that this transformation proceeds via intermolecular condensation of o-aminobenzamides with 2-iodoisothiocyanates, followed by an intramolecular Ullmann-type cross-coupling cyclization reaction.

Palladium-Copper-Catalyzed Oxidative Intermolecular [2 + 2 + 2] Coupling-Annulation: Regioselective Synthesis of Multiaryl-Substituted Benzenes.

A palladium-catalyzed intermolecular [2 + 2 + 2] oxidative coupling-annulation of terminal alkenes and alkynes using copper(II) as the oxidant has been developed through direct C-C bond formation. These reactions provide effective access to multiaryl-substituted benzenes with high regioselectivity in the absence of any ligands. The features of this protocol are broad substrate scope, and high atom and step economy. The aggregation-induced emission properties of selected products were further investigated. These synthesized multiaryl-substituted benzenes may be worth exploring for further applications in the fields of advanced functional materials or drugs.

HOTAIR mediates cisplatin resistance in nasopharyngeal carcinoma by regulating miR-106a-5p/SOX4 axis.

This study explored the function and mechanisms of HOX transcript antisense RNA (HOTAIR) in the drug resistance of nasopharyngeal carcinoma (NPC). Quantitative PCR, Western blotting, MTT assay, flow cytometry, Transwell assay, and luciferase assay were performed. HOTAIR expression levels were upregulated in cisplatin (DDP)-resistant NPC tissues and cells. Knockdown of HOTAIR in DDP-resistant NPC cells increased cell sensitivity of DDP, as well as decreased cell viability, expression of chemoresistance-related proteins, migration and invasion, increased cell apoptosis. In addition, downregulation of microRNA 106a-5p (miR-106a-5p) expression and upregulation of SRY-box transcription factor 4 (SOX4) expression were observed in DDP-resistant NPC tissues and cells. MiR-106a-5p targets HOTAIR and SOX4; thus, silencing of HOTAIR significantly increased miR-106a-5p expression. The overexpression of miR-106a-5p significantly reversed the increase in SOX4 expression induced by HOTAIR lentivirus (Lv-HOTAIR). Knockdown of SOX4 reduced the drug resistance of DDP caused by the silencing of miR-106a-5p expression. In summary, HOTAIR enhanced DDP resistance in NPC cells by regulating the miR-106a-5p/SOX4 axis.

Molluscicides against the snail-intermediate host of Schistosoma: a review.

Schistosomiasis, a neglected tropical disease (NTD), is one of the most prevalent parasitoses in the World. Certain freshwater snail species are the intermediate host in the life cycle of schistosome species. Controlling snails employing molluscicides is an effective, quick, and convenient intervention strategy to prevent the spread of Schistosoma species in endemic regions. Advances have been made in developing both synthetic molluscicides and molluscicides derived from plants. However, at present, the development of molluscicides is not adapted to the actual demand for snails and schistosoma controlling. We undertake a systematic review of exploitation and application of synthetic molluscicides and molluscicides derived from plants to combat intermediate host snails. The detailed molluscicidal activity, structure-activity relationship, structural feature, and possible mechanism of some molluscicides are also highlighted, which may afford an important reference for the design of new, more effective molluscicides with low environmental impact and realize the aim of controlling schistosome at transmission stages.

Shufengjiedu capsules protect against neuronal loss in olfactory epithelium and lung injury by enhancing autophagy in rats with allergic rhinitis.

Shufengjiedu capsules (SFJDCs), a traditional Chinese medicine, have been widely used as an antiviral, antibacterial, antitumor, and anti-inflammatory drug. However, the roles of SFJDCs in allergic rhinitis remain unclear. The purpose of this study was to investigate the effects of SFJDCs in olfaction and lung injury in rats with allergic rhinitis. An animal model of allergic rhinitis was created by intraperitoneal injection and intranasal administration of ovalbumin to rats. All rats were divided into seven groups: a model group, a low-dose SFJDC group, a medium-dose SFJDC group, a high-dose SFJDC group, a cetirizine group, and a control group. Hematoxylin and eosin (HE) staining was used to observe pathological changes in rat lung and olfactory epithelium (OE) tissue, and peripheral blood was collected and subjected to an enzyme-linked immunosorbent assay (ELISA) to detect IgE, tumor necrosis factor alpha (TNF-α), and IL-1ꞵ levels. Western blotting, immunohistochemistry staining, and immunofluorescence staining were performed to detect inflammatory cytokines and levels of the autophagy biomarker beclin1 and the apoptosis biomarker cleaeved-caspased3 in lung and OE tissue. ELISA indicated that SFJDCs significantly decreased IgE, TNF-α, and IL-1ꞵ levels in peripheral blood, the lungs, and OE tissue. In addition, Western blotting and staining indicated that SFJDCs repair lung injury, protect against neuronal apoptosis in OE, and rescue impaired autophagy in the lungs and OE tissue. In conclusion, results indicated that SFJDCs might protect against neuronal loss in the OE and lung injury by enhancing autophagy and decreasing apoptosis in rats with allergic rhinitis. Therefore, SFJDCs might serve as an alternative treatment for allergic rhinitis.

[Endoscopic transsphenoidal surgery versus microsurgery for the resection of pituitary adenomas: a systematic review].

OBJECTIVE: To evaluate the efficacy and safety between endoscopic and microscopic surgery for transsphenoidal pituitary adenoma. METHODS: Randomized or semi-random controlled trials comparing endoscopic with microscopic surgery for transsphenoidal pituitary adenoma and published between January 2000 and July 2013 were recruited. This meta-analysis (RevMan 5.1 software) was conducted to estimate short-term and long-term complications. Fixed random effect model or semi-random effect model was established to analyse the data. RESULTS: Twelve randomized or semi-random controlled trials were included in this study. Among 848 patients studied, 380 of them were treated with endoscopic and 468 were treated with microscopic. The analysis of the basic characteristics of these patients included in these studies showed that: compared with microscopic, the follow-up of patients in endoscopic group was shorter [OR = -2.29, 95%CI (-4.18, -0.39), P = 0.02], while there were no significant difference in gender proportion and the age of patients between the two groups (P > 0.05) . Also, compared with endoscopic, there was a significant addition in the incidence of diabetes insipidus [OR = 0.45, 95%CI(0.30,0.66), P < 0.0001] and other complications [OR = 0.26, 95%CI ( 0.12, 0.57), P = 0.0008] in the microscopic group, the blood loss during surgery was more [OR = -0.62, 95%CI(-1.19, 0.05), P = 0.03], the rate of complete tumor resection lower [OR = 0.61, 95%CI(0.39, 0.96), P = 0.03], and the hospitalization [OR = -1.53, 95%CI(-2.18, -0.88), P < 0.00001] was also significantly longer, there was no significant difference in the incidence of cerebrospinal fluid leakage, operation time and vision improvement rate (P > 0.05). CONCLUSION: For patients with pituitary tumors, endoscopic surgery may be more suitable compared with microscopic.

[Expression of IL-17 in laryngeal squamous cell carcinoma tissues and the clinical significance].

OBJECTIVE: To investigate the expression of interleukin 17 in laryngeal squamous cell carcinoma tissues, and to evaluate the value of interleukin-17 in the biological behavior and prognosis of laryngeal squamous cell carcinoma. METHOD: Expressions of IL-17 were analyzed in 71 laryngeal squamous cell carcinoma samples and 21 cases of adjacent tissues of carcinoma as control by immunohistochemistry. RESULT: The expression of IL-17 in laryngeal squamous cell carcinoma tissues was obviously higher than that in adjacent tissues (P < 0.05). The expression of IL-17 was associated with tumor T staging, tumor differentiation, regional lymph node metastasis, distant metastasis and recurrence (P < 0.05). Log-rank test showed that the prognosis of patients was related to the primary tumor site, tumor stage, regional lymph node metastasis, distant metastasis and IL-17 expression (P < 0.05), While Cox multiple factors analysis showed that IL-17 was not an independent prognostic factors. CONCLUSION: The expression of IL-17 may be the vital index in laryngeal squamous cell carcinoma, and it can provide some theoretical basis for the anti-tumor immunotherapy for laryngeal squamous cell carcinoma.

Expression of T-helper-associated cytokines in the serum of pituitary adenoma patients preoperatively and postperatively.

Pituitary adenomas are benign tumors, However, 30% of them may develop into invasive tumors by invading the surrounding tissues. The studies have shown that several cytokines were expressed in human anterior pituitary adenomas, therefore, we speculate that the cytokines are important in human anterior pituitary tumorigenesis. The current study is designed to investigate expression profiles of cytokines in the serum of patients with pituitary adenomas. This was done by selecting 75 cases with pituitary adenoma, including invasive and non-invasive pituitary adenomas and collected blood samples of preoperative, 1 month, 3 months, and 6 months after surgery, respectively. We used the cell flow instrument to detect the level of Lymphocytes and subsets and immunoglobulin and complement in the peripheral blood, and by ELISA detecting the content of cytokines (IL-17, IL-4, IL-5, TNF-α, INF-γ) in the serum of pituitary adenoma patients. The results show that the level of IL-4, IL-5 and IL-17 was increased substantially before surgery but they decreased substantially after surgery, IFN-γ, TNF-a was increased after surgery, the ratio of Th1/Th2 (IFN-γ/IL-4) was significantly lower before surgery and increased distinctly post-operation. These data indicated that there is some cross-regulation among Th1, Th2 and Th17 subsets and that cytokines are important in tissue inflammatory lesions of pituitary adenomas and promoting invasive development.

Giant Chondroma of the Saddle Area: Case Report and Literature Review.

A 63-year-old man presented with sexual dysfunction of 6-year duration, 5-year history of bilateral vision loss, and left nasal obstruction for 3 years. Brain computed tomography and magnetic resonance imaging showed a large mass lesion in the saddle area and extending upward to the dorsum sellae, bilateral cavernous sinus, and suprasellar region, and down into the sphenoid sinus and nasal cavity; the optic nerves and optic chiasm were elevated upward and compressed. Endocrine tests indicated that all serum level of anterior pituitary hormones decreased. The preoperative diagnosis included invasive pituitary adenoma, chordoma, osteosarcoma, chondrosarcoma, and craniopharyngioma. The tumour was subtotally removed through transsphenoidal approach. Histopathology examination revealed a chondroma. Postoperatively, the patient was stable and his visual acuity and visual field defect improved and his pituitary function return to normal except for hypothyroidism.