A ratiometric fluorescent probe for selective detection of thiophenol derivatives.

Though a number of on-off or off-on fluorescent probes have been developed for the detection of thiophenol by using its unique recognition groups, such as 2, 4-dinitrophenyl ether, 2, 4-dinitrophenyl sulfonamide, and 2, 4-dinitrophenyl sulfonate, up to now, there are few probes that can detect thiophenol by the proportional fluorescence signal. We developed a ratiometric fluorescent probe with coumarin pyridine derivative as fluorophore and 2, 4-dinitrophenyl ether moiety as the sensing unit which could be used to detect thiophenol derivatives by the aromatic nucleophilic substitution reaction. This probe (CPBPN) displayed significant change in fluorescence ratio (256 fold) to result in a more reliable analysis by self-calibration and a relatively low detection limit of 24 nM toward 4-methylthiophenol (MTP) within 30 min to achieve more sensitivity. Besides, the probe was also applied to detect the presence of thiophenol derivatives in actual water samples and fluorescence imaging in living cells. The present work is of great importance for monitoring environmental pollutants and studying their biological function.

A fluorescent probe based on ICT for selective detection of benzenethiol derivatives.

This work presented a benzothiazole-based fluorescent probe for the detection of benzenethiol derivatives using 2, 4-dinitrobenzene moiety as a sensing unit. This probe (NCABT) was able to instantaneously respond to 4-methylbenzenethiol (MTP) within 5 min. In detecting MTP, this probe displayed a low limit of detection (49 nM). Furthermore, the probe has been proved to have the potential to detect benzenethiol derivatives with electron-donating group in real water samples.

Nanostructured SL9-CpG Lipovaccines Elicit Immune Response for the Treatment of Melanoma.

Antigen peptides and adjuvants have been extensively investigated for cancer immunotherapy, and they are expected to elicit specific immune responses for cancer treatment. However, the anti-cancer efficacy of antigen peptide and adjuvant-based cancer vaccines has been limited due to the inefficient delivery to draining lymph nodes after administration. Therefore, it is necessary to develop a suitable delivery system to transport antigen peptides and adjuvants. Here, we report a novel type of nanostructured lipovaccines for the treatment of melanoma by delivering antigen peptide (SL9) and oligodeoxynucleotide adjuvant (CpG) to the lymphatic vessels and to the draining lymph node. The SL9-CpG lipovaccines were characterized using dynamic laser scattering (DLS) and transmission electron microscopy (TEM). The lymph uptake, immune response elicitation and treatment effects were evaluated on melanoma-bearing C57BL/6 mice using flow cytometry (FCM), enzyme-linked immunosorbent assay (ELISA) and tumor inhibitory efficacy. The SL9-CpG lipovaccines were uniform with a nanoscale size (~70 nm), had high encapsulation efficiency, and exhibited effective lymph uptake, resulting in activation of specific cytotoxic CD8+ T cells, and release of IFN-γ, and a robust inhibition of tumor growth. Therefore, the nanostructured SL9-CpG lipovaccines offer a promising strategy for melanoma treatment.

Development of double strand RNA mPEI nanoparticles and application in treating invasive breast cancer.

Triple negative breast cancer (TNBC) has been characterized as a very heterogeneous subtype, and is more invasive and non-expressing of the genes for the estrogen receptor (ER), progesterone receptor (PR) and HER2/neu, with poor prognosis, and hence the efficacy of regular chemotherapy is very limited. Here, we report a kind of double strand RNA (dsRNA) mPEI nanoparticle for treatment of invasive TNBC. The studies were performed on TNBC cells in vitro and in TNBC cancer-bearing mice. The results showed that dsRNA mPEI nanoparticles were able to effectively transfect cells, and demonstrated a strong capability in knocking-down the Fra-1 gene and down-stream MMP-1 and MMP-9 genes in TNBC cells and TNBC cancer-bearing mice, thereby inhibiting the invasion and migration of cells. After intratumoral injection, dsRNA mPEI nanoparticles exhibited a robust anticancer efficacy in TNBC cancer-bearing mice, and the anticancer efficacy was superior to that of paclitaxel. In conclusion, dsRNA mPEI nanoparticles are able to effectively treat aggressive TNBC, and the mechanism studies reveal that they take effect by knocking-down Fra-1 relevant genes, hence interfering in transcription and translation of the genes, which are necessary for growth and metastasis of TNBC. Therefore, the present study offers a new and promising formulation and strategy for effective treatment of TNBC.

Direct intramolecular amination of tryptophan esters to prepare pyrrolo[2,3-b]indoles.

A metal-free iodine-catalyzed intramolecular amination has been developed for the practical synthesis of pyrrolo[2,3-b]indoles from readily available tryptophan esters. The transformation has been applied to a wide array of substrates and can be performed on gram scale under very mild conditions.

Evaluation of Short-Term Efficacy of Concurrent Chemoradiotherapy in Primary Fallopian Tube Carcinoma by Diffusion-Weighted Imaging: A Retrospective Study.

BACKGROUND: This study aims to evaluate the short-term efficacy of concurrent chemoradiotherapy (CCRT) in primary fallopian tube carcinoma (PFTC) using magnetic resonance diffusion-weighted imaging (MR-DWI). PATIENTS AND METHODS: Total abdominal irradiation was performed for 61 PFTC patients after surgery, and paclitaxel and carboplatin were used for CCRT. According to the response evaluation criteria in solid tumors (RECIST1.1), patients were divided into a sensitive (n = 36) and a resistant group (n = 25). Pearson correlation analysis was conducted to assess the correlations of tumor regression rate with apparent diffusion coefficient (ADC)pre, ADCpost, and ∆ADCpost. The efficacy of CCRT in PFTC using MR-DWI was evaluated by ROC curve, logistic regression analysis, Kaplan-Meier survival curve, and Cox regression model. RESULTS: The ADCpre in both the sensitive and the resistant group was negatively associated with the tumor regression rate (r = -0.508), while the ADCpost (r = 0.454) and ∆ADCpost (r = 0.769) were positively associated with the tumor regression rate (all p < 0.05). Histopathological type, FIGO stage, lymphatic metastasis, tumor regression rate, ADCpre, ADCpost, and ∆ADCpost were confirmed as key factors for CCRT in PFTC (all p < 0.05). CONCLUSION: Our retrospective study demonstrates the predictive value of MR-DWI in CCRT for PFTC patients.