Glioblastoma is the most fatal and insidious malignancy, due to the existence of the blood-brain barrier (BBB) and the high invasiveness of tumor cells. Abnormal mitochondrial viscosity has been identified as a key feature of malignancies. Therefore, this study reports on a novel fluorescent probe for mitochondrial viscosity, called ZVGQ, which is based on the twisted intramolecular charge transfer (TICT) effect. The probe uses 3-dicyanomethyl-1,5,5-trimethylcyclohexene as an electron donor moiety and molecular rotor, and triphenylphosphine (TPP) cation as an electron acceptor and mitochondrial targeting group. ZVGQ is highly selective, pH and time stable, and exhibits rapid viscosity responsiveness. In vitro experiments showed that ZVGQ could rapidly recognize to detect the changes in mitochondrial viscosity induced by nystatin and rotenone in U87MG cells and enable long-term imaging for up to 12 h in live U87MG cells. Additionally, in vitro 3D tumor spheres and in vivo orthotopic tumor-bearing models demonstrated that the probe ZVGQ exhibited exceptional tissue penetration depth and the ability to penetrate the BBB. The probe ZVGQ not only successfully visualizes abnormal mitochondrial viscosity changes, but also provides a practical and feasible tool for real-time imaging and clinical diagnosis of glioblastoma.

In this work, a fluorescent probe, TPABF-HS, was developed for detecting hydrogen sulfide (H2S) using a human serum albumin (HSA)-binding-based approach for amplifying the fluorescence signal and extending the linear correlation range. Compared to the most recent probes for H2S, the most interesting feature of the detection system developed herein was the especially wide linear range (0-1000 μM (0-100 eq.)), which covered the physiological and pathological levels of H2S. TPABF-HS could be used in applications high sensitivity and selectivity with an LOD value of 0.42 μM. Further, site-competition experiments and molecular docking simulation experiments indicated that signal amplification was realized by the binding of the TPABF fluorophore to the naproxen-binding site of HSA. Moreover, the extension of the measurement span could allow for applications in living cells and Caenorhabditis elegans for imaging both exogenous and endogenous H2S. This work brings new information to the strategy of signal processing by exploiting fluorescent probes.

In this work, we reported a fluorescent probe Fur-SH, a derivative of benzofuranone, which was used to detect H2S in living cells and zebrafish. Based on the three structural characteristics of the probe, the effects of different structural modifications on the optical properties of the fluorophore were compared. Then, the fluorophore FurOH was synthesized by modifying diethylamino group with benzofuranone as the main skeleton. With 2,4-dinitrofluorobenzene as the recognition group and diethylamino as the electron donor, the push-pull electron effect occurred with nitro group, which led to fluorescence quenching, and an openable fluorescent probe Fur-SH was formed. The probe Fur-SH (lambda ex = 510 nm; lambda em = 570 nm) had the advantages of smaller full width at half maxima, rapid response (5 min) and wide pH window. The quantitative properties of the probe were excellent, reaching saturation at 50 equivalents of substrate. The probe Fur-SH showed high sensitivity to H2S, with LOD of 48.9 nM and LOQ of 50 nM. At present, the probe Fur-SH had been applied to fluorescence imaging of MCF-7 cells and zebrafish. By comparing the effects of different structures on the optical properties of fluorophores, this work was expected to be helpful to the development of fluorescent probes in the future.

The fluorescent probe, GXY-ADP-2, with xanthene structure as the fluorescent core was designed and prepared for the selective detection of peroxynitrite (ONOO-). ONOO- can be produced endogenously and exogenously and is a strong oxidant with a short half-life. Oxidative modifications of biomolecules, that can be attributed to the formation of ONOO-, occur in the reactions of biomolecules with secondary ONOO(--)derived radical oxidants. Therefore, it is very important to develop a specific fluorescent probe for detecting ONOO(- )to monitor oxidative stress state. The excitation wavelength and emission wavelength of the probe are 689 nm and 739 nm respectively. In the process of co-incubation with ONOO-, generate a new substance with two internal conjugated structures through a special reaction mechanism, one giving the fluorescence with the excitation wavelength of 347 nm and the emission wavelength of 484 nm with the detection limit of 0.12 mu M, and the other that with the excitation wavelength of 433 nm and the emission wavelength of 583 nm with the detection limit of 0.077 mu M. The linear dynamic range of the probe is 0-5 mu M. Its response is not affected by the other reactive oxygen species, thus can sensitively detect ONOO- . In bioimaging experiments with HepG2 cells, the green and blue cell fluorescence signals (583 nm and 433 nm, respectively) were increased, while the red one (739 nm) was significantly reduced, under lipopolysaccharide (LPS) induced oxidative stress, proving that the probe could sensitively detect ONOO- in living cells. This work provides a new tool for the dynamic changes of ONOO(- )and oxidative stress processes in biological systems.

H2S has been reported to play essential roles in a variety of physiological and pathological procedures. In this work, a novel fluorescent probe, Rho-HS, for detecting H2S was developed by introducing the ortho-halogen to activate the least reactive recognition group 2,4-dinitrophenyl moiety. In combination of the structures from both Rhodamine B and fluorescein, Rho-HS could generate both the colorimetric and fluorescent responses. This feature was not frequently achieved and could lead to the quantitative and convenient for the end-user. In comparison with recent probes for H2S, the major advantages of Rho-HS included suiting wide pH range (6.0-10.0), relatively rapid response (within 15 min) and the high selectivity among the competing species including the biothiols. With low cytoxicity, Rho-HS was further applied in the biological imaging in living MCF-7 cells and Caenorhabditis elegans. We hope that the designing strategy in this work might provide useful information for more preferable implements in this field.

A novel benzofuranone fluorescent probe, BFO-SFT, for monitoring sulfite in living cells and mice is described which operates over a wide pH range and exhibits a red-shifted emission maximum. The response of the probe BFO-SFT was relatively rapid (within 20 min) and exhibited a good linear correlation of 0-10 Eq (100 mu M) with reliable accuracy (R-2 = 0.9934). The probe also showed high sensitivity (Limit of detection = 152 nM) and selectivity. With low cytotoxicity, BFO-SFT was successfully applied into the biological imaging of sulfite in living MCF-7 cells and in BALB/C Nude mice.

Correction for ‘A highly selective AIEgen fluorescent probe for visualizing Cys in living cells and C. elegans’ by Ya-Xi Ye et al., New J. Chem., 2021, 45, 19073–19081.

Cysteine (Cys), one of the biological thiols, which plays critical roles in biological system regulating the balance of redox homeostasis. In order to monitor the level of Cys in the living cells and organisms, a chromogenic fluorescence probe Rhocl-Cys based on Rhodamine chloride exhibiting the preferable performance of fluorescence turn-on response reacting with Cys was presented. Rhocl-Cys responded rapidly to Cys within 20 min, and had stable fluorescence intensity within pH 6.0-10.0, high selectivity towards Cys and the anti-inference capability with a low detection limit of 0.80 mu M. In particular, Rhocl-Cys could qualitatively and quantitatively monitor the level of endogenous and exogenous Cys in living cells and successfully apply to zebrafish detecting Cys. Therefore, these results might further provide the basis exploring the role of Cys in biological system and facilitate as clinical diagnostic molecular tools.

Sulfite (SO32-) is considered as a monitor of a wide range of physiological processes. However, cells and tissues are adversely affected when the body ingests high level of sulfite. Here, we designed and synthesized a "turn on" fluorescent probe ImiSft-1 with 2-cyano-N-methylacetamide as the specific recognition site of SO32-. This probe predominantly achieved high response intensity to SO32- and desirable properties such as large Stokes shift (∼180 nm), fast response time (within 15 s), and high sensitivity (LOD = 0.12 μM). Importantly, the probe was highly selective for sulfite from other bio-species including biological thiols. Other functional properties included broad pH adaptability (5.0-10.0) and low cytotoxicity. Given these advantages and the fluorescence imaging in living MCF-7 cells, it was demonstrated that probe ImiSft-1 could monitor the changes of sulfite concentration in living cells.

Bone metastasis of malignant solid tumors has become one of the most serious complications, especially in breast cancer, which was particularly challenging for early detection and treatment in clinical practice. In this work, we reported a new fluorescently labeled bisphosphonate for bone metastasis detection of breast cancer. The designed probes were based on Rhodamine B and bisphosphonate as recognition group, which can specifically target hydroxyapatite (HA) existed in bone tissue. After the osteoclasts were adsorbed on the bone surface, the sur-rounding microenvironment was acidified, causing the HA to locally dissolve. The probe bound to the HA was then released, and realized the fluorescence turn on under acidic conditions. In vitro experiments showed that G0 was more excellent than G2 owing to shorter connecting arm. Subsequently, we proved that G0 could combine with HA rapidly and exhibit excellent response in solid state. More importantly, we established a model of bone metastasis with MDA-MB-231 cells which was similar to the clinical cases and evaluated the theranostics value of G0 prospectively, which provide the potential application prospect in clinical.

As essential biological thiols in organisms, Cys, Hcy, and GSH are closely related to each other, and they can be involved in various pathological processes if expression levels are abnormal.

Most of the ONOO- fluorescent probes have restricted applications because of their aggregation-caused quenching (ACQ) effect, long response time and low fluorescence enhancement. Herein, we developed a novel AIEgen fluorescent probe (PE-XY) based on a benzothiazole and quinolin scaffold with high sensitivity and selectivity for imaging of ONOO-. The results indicated that probe PE-XY exhibited fast response towards ONOO- with 2000-fold enhancement of fluorescence intensity ratio in vitro. Moreover, PE-XY exhibited a relatively high sensitivity (limit of detection: 8.58 nM), rapid response (<50 s), high fluorescence quantum yield (δ = 0.81) and excellent selectivity over other analytes towards ONOO-in vitro. Furthermore, PE-XY was successfully applied to detect endogenous ONOO- levels in living HeLa cells, C. elegans and inflammatory mice with low cytotoxicity. Overall, this work provided a novel fast-response and highly selective AIEgen fluorescent probe for real-time monitoring ONOO- fluctuations in living systems.

Cysteine (Cys) is an indispensable small organic molecule containing sulfhydryl groups, which has essential regulatory effects on the physiological process of human body. In this work, a red emission fluorescent probe TCFQ-Cys was designed and exploited based on 2-(3-cyano-4,5,5-trimethylfuran-2(5H)-ylidene) malononitrile-derivatives. The probe could effectively monitor Cys through the typical acrylate cleavage. The detecting system showed a red emission at 633 nm and the fluorescence was stable within the pH range of 6-9. The detection could be completed in 30 min. TCFQ-Cys presented high sensitivity with a detection limit of 0.133 tM and high selectivity towards Cys from other biological mercaptans. The most important feature was that the system had a wide linear range of 0-300 mu M, which covered the physiological requirements of Cys detection. Subsequently, we conducted the biological imaging of Cys in MCF-7 cells and Caenorhabditis elegans (C. elegans). Therefore, TCFQ-Cys had a practical application prospect for further investigating the physiological function of Cys. (C) 2021 Elsevier B.V. All rights reserved.

Hypochlorite, as one of reactive oxygen species, has drawn much attention due to its essential roles in special biological events and disorders. The exogenous hypochlorite remains a risk for human, animals and plants. In this work, a novelwater soluble quinolin-containing nitrone derivative T has been developed for fluorometric sensing hypochlorite. The response mechanismof T towards ClO- was reported for the first time. In comparison with the reported sensors for ClO-, the sensor T in this work exhibited advantages including high selectivity (80 fold over other analytes), rapid response (within 5 s) and lipid-water distribution transformation (LogP from 2.979 to 6.131). Further biological applications suggested that T was capable of monitoring both exogenous and endogenous ClO- in living cells. The imaging in Arabidopsis thaliana indicated that the absorption and transmission of ClO- in plant could be monitored by this sensor through the chlorine-related mechanism. This work might raise referable information for further investigations in the physiological and pathological events in both tumor and plants. (C) 2020 Elsevier B.V. All rights reserved.

国花是被选作一国表征的花卉植物,用以反映人民的传统感情.当前,中国是世界上唯一尚未确认国花的大国.提出了国花评选原则和标准,对比了世界127个国家国花的特点;分析了中国优良花卉丰富而导致国花难以确定的原因;回顾了40年国花评选历史.重点阐述梅花牡丹双国花的四大理由(生物学属性、地域分布及应用价值;深厚的社会历史民族基础;完整中国形象和传统文化代表;中华民族精神象征);讨论了梅花牡丹双国花推动实现中华民族伟大复兴的重大意义.最后,提出了科技创新推动梅花产业高质量发展的目标任务、主要内容、实施路线图、实现途径和保障措施.

Sulfur-containing species are essential in the composition and the metabolism of the organisms, thus developing a full set of implements to cover all of them is still a favorable choice. Herein, we chose imidazo [1,5-alpha] pyridine moiety as the basic fluorophore for the detection of sulfite, and preliminarily completed the toolset since biothiols (GSH, Cys, Hcy), H2S, and PhSH could be detected by sensors based on the same backbone. The designed sensor, IPD-SFT, with structural novelty and large Stokes shift (130 nm), indicated the most attractive advantages of remarkably rapid response period (within 1 min) and high selectivity for sulfite from all the sulfurcontaining species. Other practical properties included high sensitivity (LOD = 50 nM) and wide pH adaptability (5.0-11.0). Furthermore, IPD-SFT could monitor both exogenous and endogenous sulfite. It not only raised a potential tool for sulfite detection, but also preliminarily completed the toolset for all the sulfur-containing species. The development of such toolsets might reveal the sulfur-containing metabolism and corresponding physiology and pathological procedures.

Due to the three domains of the colchicine-site which is conducive to the combination with small molecule compounds, colchicine-site on the tubulin has become a common target for antitumor drug development, and accordingly, a large number of tubulin inhibitors binding to the colchicine-site have been reported and evaluated over the past years. In this study, tubulin inhibitors targeting the colchicine-site and their application as antitumor agents were reviewed based on the literature from 2015 to 2019. Tubulin inhibitors were classified into ten categories according to the structural features, including colchicine derivatives, CA-4 analogs, chalcone analogs, coumarin analogs, indole hybrids, quinoline and quinazoline analogs, lignan and podophyllotoxin derivatives, phenothiazine analogs, N-heterocycle hybrids and others. Most of them displayed potent antitumor activity, including antiproliferative effects against Multi-Drug-Resistant (MDR) cell lines and antivascular properties, both in vitro and in vivo. In this review, the design, synthesis and the analysis of the structure-activity relationship of tubulin inhibitors targeting the colchicine-site were described in detail. In addition, multi-target inhibitors, anti-MDR compounds, and inhibitors bearing antitumor activity in vivo are further listed in tables to present a clear picture of potent tubulin inhibitors, which could be beneficial for medicinal chemistry researchers.

In this work, a primary method was constructed for detecting hydrazine in plant, thus accomplished the closed-loop monitoring of hydrazine circulation within manufacture, environment, plants, animals and human. From a series of sensors, QYL-1 was selected to present the hydrazine sensing properties. As a preliminary tool, QYL-1 suggested the ultra-wide linear range (0-20.0 equivalent) and high selectivity, which were extremely essential for linking the monitoring in various scale and field. For the first time, concentration-dependent tracking of hydrazine was successfully performed in Arabidopsis Thaliana root tips. Afterwards applications in water samples and living MCF-7 cells then fulfilled the demonstration of closing the loop by linking both the upstream and downstream nodes. More than raising a practical method, this work offered initial information for the closed-loop monitoring of hydrazine circulation, which might be significant for the ideal systematic managing in future. (C) 2019 Elsevier B.V. All rights reserved.

Several novel cycloalkyl-fused 2,3-diaryl pyrazole derivatives were designed, synthesized, and evaluated as potential anti-tubulin agents. Compound A10 exhibited the most potent antiproliferative activity against a panel of cancer lines (IC50  = 0.78-2.42 μM) and low cytotoxicity against 293T & L02 (CC50 values of 131.74 and 174.89 μM, respectively). Moreover, A10 displayed inhibition of tubulin polymerization in vitro, arrested the G2/M phase of the cell cycle, changed morphology of tubulin, increased intracellular reactive oxygen species, and induced apoptosis of HeLa cells. Docking simulation and 3D-QSAR models were performed to elaborate on the anti-tubulin mechanism of the derivatives. The inhibition of monoclonal colony formation provided more intuitional data to verify the possibility of A10 as a novel tubulin assembling inhibitor.

Palladium(Pd) has drawn worldwide attentions because its connections to industry, chemistry, biological material and public health. Quantitative and selective detection tools for Pd and its ion forms are in urgent necessity. Here an umbelliferone derivative Umb-Pd2 was provided as a small, steady, safe and selective sensor for detecting Pd(II). It indicated advantages including sensitive (LOD 1.1 nM), wide pH tolerance (5.0-10.0), applicable linear range (0-1.8 equivalent) and low toxicity. The most attractive point was its explicit selectivity towards Pd(II) from Pd(0) in both independent and coexistence systems. This distinguishing ability was further utilized in imaging in living cells, raising this work as a rare and important example among all the published papers on palladium sensing. Thus, Umb-Pd2 supplied a potential approach for further improvement and applications in both daily chemistry and public health. (C) 2019 Published by Elsevier B.V.