Research on the cognitive neural mechanism of privacy empowerment illusion cues regarding comprehensibility and interpretability for privacy disclosures.

In the era of artificial intelligence, privacy empowerment illusion has become a crucial means for digital enterprises and platforms to "manipulate" users and create an illusion of control. This topic has also become an urgent and pressing concern for current research. However, the existing studies are limited in terms of their perspectives and methodologies, making it challenging to fully explain why users express concerns about privacy empowerment illusion but repeatedly disclose their personal information. This study combines the associative-propositional evaluation model (APE) and cognitive load theory, using event-related potential (ERP) technology to investigate the underlying mechanisms of how the comprehensibility and interpretability of privacy empowerment illusion cues affect users' immediate attitudes and privacy disclosure behaviours; these mechanisms are mediated by psychological processing and cognitive load differences. Behavioural research results indicate that in the context of privacy empowerment illusion cues with low comprehensibility, users are more inclined to disclose their private information when faced with high interpretability than they are when faced with low interpretability. EEG results show that in the context of privacy empowerment illusion cues with low comprehensibility, high interpretability induces greater P2 amplitudes than does low interpretability; low interpretability induces greater N2 amplitudes than does high interpretability. This study extends the scopes of the APE model and cognitive load theory in the field of privacy research, providing new insights into privacy attitudes. Doing so offers a valuable framework through which digital enterprises can gain a deeper understanding of users' genuine privacy attitudes and immediate reactions under privacy empowerment illusion situations. This understanding can help increase user privacy protection and improve their overall online experience, making it highly relevant and beneficial.

Impact of the normativeness and intelligibility of privacy interpretation information on the willingness to accept targeted advertising -A cognitive load perspective.

From the perspective of the user's psychological load, this study examined the cognitive mechanism by which privacy interpretation information affects the willingness to accept targeted advertising. Our findings provide a reference for enterprises seeking to develop and improve privacy interpretation information and reduce advertising avoidance behaviour. Based on information processing theory and cognitive load theory, this study experimentally collected volunteers' electroencephalography (EEG) data, interpreted the EEG results as representing emotions and cognitive load, and analysed the impact of the normativeness and intelligibility of privacy interpretation information on the willingness to accept targeted advertising. Intelligibility significantly affected this willingness. In the case of acceptable transparency, users were more inclined to avoid targeted advertising under low interpretability. Low interpretability caused them to expend more cognitive effort, which induced a larger N2 amplitude. In the case of unacceptable transparency, the opposite conclusion was drawn. In addition, privacy information with high interpretability was more likely to arouse users' emotions and induce a greater amplitude of late positive potential. Supplementary Information: The online version contains supplementary material available at 10.1007/s12144-023-04325-6.

Design, synthesis and structure-activity relationship of dihydrobenzoquinolines as novel inhibitors against influenza A virus.

Novel dihydrobenzo[h]quinolines (DHBQs), the products of an efficient catalyst-free three-component reaction (3CR) recently developed by us, possess useful and strong aggregation-induced emission (AIE) characteristic. Here, a series of new dihydrobenzo[h]quinolines (h-DHBQs 4-1-34) and dihydrobenzo[f]quinolines (f-DHBQs 5a-e) were designed and synthesized by the 3CR to study their bioactivities as novel inhibitors against the influenza A (H1N1) virus. The structure-activity relationship (SAR) indicates that the antiviral activities of DHBQs depend on the combination of substituents and three of h-DHBQs (4-12, 4-25 and 4-27) show potent antiviral activity with IC50 = 2.52-3.79 µM. These potent h-DHBQs have low toxicity to MDCK and A549 cells (CC50 > 100 µM for 4-12 and > 50/100 µM for 4-25 and 4-27). The primary mechanism of the antiviral activities of DHBQs was studied using the most potent h-DHBQ 4-12, which indicated that 4-12 could efficiently inhibit virus-induced plaque formation and NP/PB2 protein expression in a dose-dependent way. DHBQs with simple synthetic method, useful AIE characteristic and antiviral activities are expected to be developed into potential inhibitors against influenza A virus, at the same time acting as chemical/biological fluorescent probe.

IL-6 and IL-10 Are Associated With Gram-Negative and Gram-Positive Bacteria Infection in Lymphoma.

To investigate the Th1/Th2 cytokine profile in patients with lymphoma during the myelosuppression stage of infection. 52 patients with gram-negative bacterial infection (G- group), 49 patients with gram-positive bacterial infection (G+ group), 51 uninfected patients with lymphoma (uninfected group) and 20 healthy controls (healthy group) were enrolled in this study. We evaluated the quantification of Th1/Th2 cytokines with flow cytometry bead assay (CBA) in the sera to explore a rapid diagnostic method to determine the type of infection and anti-infective effect. The levels of procalcitonin (PCT) were also detected simultaneously. The four groups did not differ with regard to IL-2 and IL-4 (P>0.05). The IFN-γ and TNF-α levels of patients with lymphoma were higher than those of healthy controls (P<0.05). There was significantly upregulated IL-6 and IL-10 expression in the G- group (P<0.001). A similar trend was reflected in the IL-6 of the G+ group, which was significantly increased (P<0.001). However, no significant upregulation was observed for IL-10 in the G+ group. According to the different degrees of increased IL-6 and IL-10 levels, We proposed to use the G- Bacterial Infection Cytokine Profile (G- BICP) and the G+ Bacterial Infection Cytokine Profile (G+ BICP) for the first time to differentiate between Gram-negative and Gram-positive (G-/G+) bacterial infection in adults with lymphoma in the myelosuppression stage after chemotherapy. The IL-6, IL-10 and PCT in the G- group and the IL-6, PCT in the G+ group were significantly decreased at day 4 and day 8 compared with those at day 1. IL-6 and IL-10 are closely associated with the severity and treatment efficacy in adults with lymphomas who develop infections after chemotherapy and can help distinguish between G- and G+ bacterial infections at an early stage.

A simple iodine-DMSO-promoted multicomponent reaction for the synthesis of 2,4-disubstituted dihydrotriazole-3-ones.

A series of 2,4-disubstituted 1,2,4-triazole-3-ones 4 were prepared via an iodine-DMSO-promoted three-component reaction of formaldehyde, amines and hydrazines in moderate yields.

The successful treatment of Enterocytozoon bieneusi Microsporidiosis with nitazoxanide in a patient with B-ALL: A Case Report.

Introduction: Enterocytozoon bieneusi (E. bieneusi) Microsporidia can cause opportunistic infections in immunocompromised patients and is also an emerging disease in these individuals. Its clinical manifestations are chronic diarrhea and severe wasting syndrome, these can be extremely debilitating and carry a significant risk of death for immunocompromised patients. Often, microsporidia cannot be confirmed immediately by routine examination and culture. Effective and available treatment options are limited for infections caused by E. bieneusi in humans. Such cases are very rare in Chinese Mainland. Case presentation: A 47-year-old male had recurrent, profuse watery diarrhea and abdominal discomfort for more than 7 months, with a fever for 5 days. Two years earlier, he received treatment with a modified BFM-90 protocol for acute B cell lymphoblastic leukemia and is currently in the final stages of maintenance therapy with oral methotrexate and mercaptopurine. The leukemia was assessed as still in remission two months ago. PET/CT showed massive peritoneal fluid accumulation and a high uptake area in the diffused peritoneum (SUVmax 12.57), suggesting tumor invasion or microbial infections. However, broad-spectrum antibacterial therapies were ineffective. Metagenomic sequencing of plasma and peritoneal fluid showed no suggestion of the existence of a tumor but instead showed a high sequence number of DNA and RNA of the Microsporidia. His albendazole treatment failed and subsequent treatment with nitazoxanide successfully resolved the infection. Conclusion: This case shows that we should consider the possibility of atypical pathogen infection in patients with hematologic malignancy who repeatedly develop unexplained diarrhea with wasting. mNGS can help rule out malignant neoplasms and diagnose infections. Our results suggest that nitazoxanide effectively treats E. bieneusi microsporidia infections.

Optical Characteristics and Applications of AIE Racemic C6-Unsubstituted Tetrahydropyrimidines.

Racemic C6-unsubstituted tetrahydropyrimidines (THPs) are the products of an efficient five-component reaction that we developed. THPs show strong AIE characteristics, that is, completely no fluorescence in different solvents but strong emission with fluorescence quantum yields (Φ F) up to 100% upon aggregation. However, the Φ F values of their pure enantiomers are lower than 46%. Unlike common AIE compounds with crowded aryl rotors on a π-bond or on an aryl ring, THPs have three completely non-crowded aryl rotors on a non-aromatic chiral central ring (tetrahydropyrimidine). In this mini review, we first discuss the AIE characteristics of THPs and the influences of molecular structures on their molecular packing modes and optical properties, and then present their applications and forecast the development of other racemic AIE compounds.

Highly Efficient Multifunctional Organic Photosensitizer with Aggregation-Induced Emission for In Vivo Bioimaging and Photodynamic Therapy.

Photosensitizers play a critical role in photodynamic therapy (PDT). Multifunctional organic nanoparticles (NPs) that possess bright fluorescence in aggregates, high singlet oxygen (1O2) quantum yield, near-infrared (NIR) absorption and emission, large Stokes shift, two-photon bioimaging, specific organelle targeting, high PDT efficiency, as well as good biocompatibility and photostability are ideal candidate photosensitizers for image-guided PDT. Due to its enhanced fluorescence and high 1O2 generation efficiency in aggregate states, photosensitizers with aggregation-induced emission (AIE) characteristics have attracted increasing interest in PDT. In this study, a new AIE-active Schiff base 5-(((5-(7-(4-(diphenylamino)phenyl)benzo[c][1,2,5]thiadiazol-4-yl)thiophen-2-yl)methylene)amino)-3-methylthiophene-2,4-dicarbonitrile (TBTDC) based on a D-A-π-A skeleton has been designed and synthesized, and it can be readily encapsulated by Pluronic F-127 to form uniform nanoparticles. TBTDC NPs exhibit bright NIR emission at 825 nm with a Stokes shift up to 300 nm, impressive two-photon bioimaging capability with tissue penetration deep into 300 µm, high 1O2 generation quantum yield (0.552), specific targeting to lysosome, as well as good biocompatibility and photostability. Furthermore, TBTDC NPs present remarkable cytotoxicity for tumor cells and suppression of tumor growth in nude mice through reactive oxygen species generation upon white light irradiation. These results reveal that TBTDC NPs have great potential to become excellent candidates for multifunctional organic photosensitizers for two-photon bioimaging and image-guided PDT and are promising in future clinical applications.

A Real-World Observation of Eltrombopag and Recombinant Human Thrombopoietin (rhTPO) in Lymphoma Patients With Chemotherapy Induced Thrombocytopenia.

This real-world, observational study aimed to assess and compare the clinical efficacy and safety of eltrombopag with recombinant human thrombopoietin (rhTPO) in the treatment of chemotherapy induced thrombocytopenia (CIT) in patients with lymphoma. One hundred and fifty-three patients who experienced grade 3 or 4 thrombocytopenia after chemotherapy for lymphoma were enrolled, 51 of which were treated with eltrombopag, 50 with rhTPO, and 52 patients with no drug treatment were served as the control group. The lowest platelet level and mean platelet counts at Day 5, Day 7, and Day 10 were significantly higher in both the eltrombopag group (P=.041,.003,.000,.000) and rhTPO group (P=.005,.005,.000,.000) than the control, but there was no difference between treatment with eltrombopag and rhTPO. Similarly, days required for the recovery of platelet counts to ≥50×109/L and ≥75×109/L were not different between the two treatment groups but significantly higher than the control group (P <.05). Rates of bleeding and platelet transfusion were all significantly reduced in patients treated with eltrombopag (P=.031,.032) or rhTPO (P=.017,.009) when compared to the control. Treatment-related adverse events (AEs) were reported in 7 (13.7%) and 6 (12.0%) patients in the eltrombopag and rhTPO groups, respectively, all being mild and transient in nature. In conclusion, both eltrombopag and rhTPO were effective and safe in the treatment of thrombocytopenia after chemotherapy for lymphoma.

Ruxolitinib combined with doxorubicin, etoposide, and dexamethasone for the treatment of the lymphoma-associated hemophagocytic syndrome.

PURPOSE: Case reports suggest that ruxolitinib-containing treatment could increase the clinical response rate of patients with hemophagocytic syndrome (HPS). This study aimed to explore the effect of ruxolitinib-containing treatment for patients with lymphoma-associated hemophagocytic syndrome (LAHS). METHODS: This was a retrospective study of patients with LAHS hospitalized at the First Affiliated Hospital of Guangdong Pharmaceutical University between October 2017 and September 2019. Patients were treated with HLH-94 (etoposide and dexamethasone) or R-DED regimen (ruxolitinib, doxorubicin, etoposide, and dexamethasone). The clinical characteristics, treatment responses, and overall survival (OS) were compared. The patients were divided into the HLH-94 group (n = 34) and the R-DED group (n = 36). RESULTS: Compared with HLH-94, R-DED might effectively improve the clinical manifestations, including fever and splenomegaly in patients with LAHS, and control the systemic cytokine storm. The response rate at 2 weeks was 54.8% in the HLH-94 group, which was lower than in the R-DED group (83.3%) (p = 0.011). The OS was significantly prolonged in the R-DED group compared with the HLH-94 group (median, 5 vs. 1.5 months, p = 0.003). The multivariable analysis showed that lower IL-10 levels [hazard ratio (HR)] = 1.000, [95% confidence interval (CI)] 1.000-1.000, p = 0.012), R-DED regimen (HR = 0.196, 95% CI 0.084-0.457, p < 0.001), and non-NK/T-cell lymphoma (HR = 0.254, 95% CI 0.102-0.628, p = 0.003) were associated with better OS. The prognosis of patients with LAHS was generally poor. CONCLUSION: Ruxolitinib can be combined with chemotherapy in HPS. It is feasible, with no early signals of increased toxicity.

A series of octahydroquinazoline-5-ones as novel inhibitors against dengue virus.

A series of octahydroquinazoline-5-ones (OHQs 1-50) were designed and synthesized via an improved five-component reaction (5CR). Their bioactivities against dengue virus (DENV) were evaluated by determining lacate dehydrogenase (LDH) in the BHK-21 cells infected with DENV-2. Primary structure-activity relationship showed that six of OHQs with suitable substituents displayed good activities with EC50 = 1.31-1.85 µM. The primary bioactivity mechanism was investigated using the most potent OHQ 23. Experimental results indicate that 23 could efficiently reverse the DENV-2-induced cytopathic effect and suppress the expression of viral structure E protein, but showed no interaction with the MTase and RdRp domain of NS5, a protein plays an important role in viral genome transcription and viral protein translation. The efficient synthetic method, novel structures as DENV inhibitors and good activities are expected to be developed potential DENV inhibitors.

Discovery of dihydropyrrolidones as novel inhibitors against influenza A virus.

More effective prophylactic and therapeutic strategies to combat influenza viruses are urgently required worldwide because the conventional anti-influenza drugs are facing drug resistance. Here, dihydropyrrolidones (DHPs), the products of an efficient multi-components reaction, were found to possess good activities against influenza A virus (IAV). Primary structure-activity relationship indicated that the activities of DHPs were greatly influenced by substituents and four of them had IC50 values lower than 10 µM (DHPs 5-2, 8, 14 and 19: IC50 = 3.11-9.23 µM). The activities against multiple IAV strains and mechanism of DHPs were further investigated by using 5-2 (IC50 = 3.11 µM). It was found that 5-2 possessed antiviral effects against all the investigated subtypes of IAVs with the IC50 values from 3.11 to 7.13 µM. Moreover, 5-2 showed very low cytotoxicity with CC50 > 400 µM. Results of mechanism study indicated that 5-2 could efficiently inhibit replication of IAV, up-regulate the expression of key antiviral cytokines IFN-ß and antiviral protein MxA, and suppress the production of the NDAPH oxidase NOX1 in MDCK cells. These results indicated that 5-2 could be used as a potential inhibitor against wide subtypes of IAVs.

Influence factors on the critical micelle concentration determination using pyrene as a probe and a simple method of preparing samples.

The critical micelle concentration (CMC) is an important parameter of widely used surfactants and needs to be measured in the application and development of surfactants. Fluorometric method is a widely used method determining CMC values owing to the advantages of highly sensitivity, fast response and wide application range. There are two common methods (I and II) of preparing samples for CMC fluorometric determination. In the process of developing CMC probes with aggregation-induced emission (AIE) characteristics, we found that methods I and II were not suitable for CMC probes with AIE charateristics and developed a new sample preparation method (III), which is not only suitable for CMC probes with AIE characteristic but also decreases operation procedures and errors owing to omitting the addition of micro amount of dyes into each sample. To ascertain if method III is also suitable for other CMC probes without AIE characteristics, the CMC values of surfactants were determined by fluorometric method using widely used pyrene without AIE charateristic as probe and methods I-III to prepare samples. The obtained experimental results proved that method III not only was suitable for preparation of samples for CMC determination of surfactants using pyrene as probe but also led to the least average deviation (methods I-III led to ±0.13, ±0.34 and ±0.05 mM deviation for the CMC determination of sodium dodecyl sulfate (SDS), respectively). The CMC determination using pyrene as probe is based on its change in the ratio (I FIII/I FI) of its emission peaks I and III with surfactant concentration. Unexpectedly, it was found that the I FIII/I FI value of pyrene in surfactant solutions is sensitive to the measurement conditions changing exciting light energy, such as slit widths and sample-measured number. In addition, it was found that surfactant SDS or cetrimonium bromide from different suppliers not only has significantly different CMC values but also leads to very different I FIII/I FI values of pyrene in a certain concentration of surfactant, which can be used as a simple method to distinguish the same surfactant with different CMC values.

Self-reversible mechanofluorochromism of AIE-active C6-unsubstituted tetrahydropyrimidine derivatives.

The mechanofluorochromic properties of three C6-unsubstituted tetrahydropyrimidines (THPs), namely, diethyl 1,2,3-triphenyl-1,2,3,6-tetrahydropyrimidine-4,5-dicarboxylate (1), dimethyl 1,2,3-tri(4-trifluoromethylphenyl)-1,2,3,6-tetrahydropyrimidine-4,5-dicarboxylate (2), and dimethyl 1,2,3-tri(3-trifluoromethylphenyl)-1,2,3,6-tetrahydropyrimidine-4,5-dicarboxylate (3), with aggregation-induced emission (AIE) characteristics were investigated. The blue-green/cyan emissions of the three THPs can be switched reversibly by a grinding-fuming/heating process, with the change in maximum emission wavelength (λ em) up to 57 nm and the decrease of fluorescence quantum yields (Φ F). Interestingly, the green or cyan fluorescence of the ground powder (λ em is located at 481, 470 and 477 nm for 1b, 2 and 3, respectively) can spontaneously recover to the original blue (λ em is located at 434, 442 and 436 nm for 1b, 2 and 3, respectively) in 1-2 d at room temperature without any external stimulation. X-ray single-crystal diffraction, powder X-ray diffraction (XRD) and differential scanning calorimetry (DSC) studies demonstrate that the conversion between the molecular packing modes is the main reason for the mechanofluorochromism and the spontaneously recoverable mechanofluorochromism relates to intermolecular hydrogen bonds. The sensitively and/or spontaneously recoverable mechanofluorochromism of these THPs is expected to have great potential in sensing, optical recording and self-healing fluorescent materials.

Water-DMSO-promoted one-pot synthesis of two new series of dihydropyrrolo[2,3-h]quinolines.

Pyrrolo[2,3-h]quinolines are important heterocycles with various biological activities. Here, two new series of dihydropyrrolo[2,3-h]quinolines with more substituents on the quinoline ring (4 and 6) were efficiently synthesized via the catalyst-free three-component reaction (3CR) of but-2-ynedioates, 4-aminoindoles and aldehydes or isatins in a DMSO-water (volume ratio: 2.5 : 1) mixture in moderate to good yields. A possible mechanism was proposed based on the crucial and promoted effects of water and DMSO in the 3CR, respectively. In addition, it was found that dihydropyrrolo[2,3-h]quinolines 4 could be quantitatively oxidized into new pyrrolo[2,3-h]quinolines 10 at room temperature using Cu(NO3)2 as an oxidant. This work affords efficient synthesis methods for constructing a library of new pyrrolo[2,3-h]quinolines (4, 6 and 10) and is expected to promote the research on the bioactivities of pyrrolo[2,3-h]quinolines.

Determining the Critical Micelle Concentration of Surfactants by a Simple and Fast Titration Method.

Critical micelle concentration (CMC) is a crucial parameter of widely used surfactants, and many methods have been developed for CMC determination. However, the current methods for CMC determination, such as conductive, surface tension, and fluorometric methods, are tedious and time- and sample-consuming because a series of samples with different concentrations of surfactants need to be prepared and measured. Although an economical, simple, and fast titration method for CMC determination (only one sample and several minutes are needed) was reported using changes in the color/fluorescence of ionic organic dyes, it has not been used in practical CMC determination owing to the disadvantages of these dyes: very narrow application range (only suitable for cationic or anionic surfactants) and difficult to identify titration end point, especially using different concentrations (10-300 µM) for the same kind surfactants. Here a C6-unsubstituted tetrahydropyrimidine (THP-T1) was found to possess unique and excellent characteristics in titrated surfactant solutions: above CMC, preferring to dissolve in micelles and showing no emission, and not until near/at CMC, being released from micelles and instantly forming aggregates with strong fluorescence. The fluorescence-turn-on change at CMC (titration end point) is so sensitive that it can be clearly observed without comparison of blank and control of dye concentration, and the concentration (c'THP) of THP-T1 in titrated solution at CMC is only about 1 µM for zwitterionic surfactants and 2.5 µM for other kinds of surfactants. The CMC values determined by the THP-T1-based titration method are almost the same as those determined by the fluorometric method using THP-T1 as probe. THP-T1 overcomes the disadvantages of reported dyes for CMC titration and realizes the economical, simple and fast CMC titration of different kinds of surfactants for the first time.

Discovery of Dihydropyrrol-2-ones as Novel G0/G1-Phase Arresting Agents Inducing Apoptosis.

A series of dihydropyrrol-2-ones (DHPs) were designed and synthesized via an efficient multicomponent reaction at room temperature for evaluation of their bioactivities against four human cancer lines (MCF-7, RKO, HeLa, and A549) in vitro. Preliminary structure-activity relationship studies showed that R4 = 3-MeO-4-OH-Ph is a crucial group for increasing cytotoxicities against RKO cells and the influences of R1-R3 depend on their combination. It was found that DHPs 5a, 5q, and 5s showed the best antiproliferative activities against A549, RKO, and all four studied cell lines, respectively (IC50 = 1.9, 0.8, and 0.9-2.4 µM). They can be used as new lead compounds for developing potentially selective or broad spectrum anticancer agents. 5q proves as a potent G0/G1-phase arresting agent inducing cell apoptosis by increasing/decreasing the levels of p53 and p21/cyclin D1.

Q63, a novel DENV2 RdRp non-nucleoside inhibitor, inhibited DENV2 replication and infection.

Dengue virus (DENV) annually infects 400 million people worldwide. Unfortunately, there is lack of widely protective vaccine or drugs against DENV. The viral RNA-dependent RNA polymerase (RdRp) of NS5 protein is highly conserved among different DENV subtypes, thus presenting itself as an attractive target for drug design. In the current research, SPRi was performed to screen compounds against DENV2 RdRp and 5(1H)-Quinazolinone,2-(4-bromophenyl)-2,3,4,6,7,8-hexahydro-7,7-dimethyl-1,3-diphenyl (Q63) was successfully screened out with a KD of 0.9 µM. Then, ITC and molecular docking assay was performed to access the binding mechanism between Q63 and DENV2 RdRp. Meanwhile, Q63 also decreased the intermediate dsRNA production, which was the product of RdRp. Further the antiviral effects of Q63 were evaluated on mosquito C6/36 cells and mammalian BHK-21 cells. Q63 reduced CPE and cell toxicity effect after DENV2 infection on C6/36 and BHK-21 cells, with an EC50 of 2.08 µM. Time of addition assay revealed that Q63 affected the early genome RNA replication stage, including genome RNA replication. In addition, Q63 down-regulated STAT1 phosphorylation, ISG15 and ISG54 after DENV2 infection. In summary, Q63 was found to be a novel RdRp non-nucleoside inhibitor and a potential lead compound for coping with DENV infectious disease in the future.

A hydrophobic organelle probe based on aggregation-induced emission: Nanosuspension preparation and direct use for endoplasmic reticulum imaging in living cells.

Organic fluorophores have a wide range of biological uses and are usually needed to be prepared as water-soluble compounds or nanoparticles for applications in aqueous biosystems owing to their hydrophobic properties, which often is a complex, time-consuming and high-cost process. Here, the nanoparticle preparation of hydrophobic fluorophores and their application in cell imaging have been investigated. It was found: a) fetal bovine serum (FBS) shows an excellent dispersion effect on hydrophobic small-molecule organic compounds; b) a hydrophobic C6-unsubstituted tetrahydropyrimidine (Me-THP-Naph) can be prepared as nanosuspensions utilizing cell culture medium with 10% FBS and directly be used as a specific real-time imaging probe for the endoplasmic reticulum (ER), a dynamic organelle playing a crucial role in many cellular processes. Compared with existing ER-targeted organic fluorescent probes, Me-THP-Naph, a product of an efficient five-component reaction that we developed, has unconventional aggregation-induced emission characteristics and shows advantages of low cost, long-term staining, good photostability, high signal-to-noise ratio and excellent biocompatibility, which make it a potential specific probe for real-time ER imaging. More importantly, this work affords a simple strategy for direct application of hydrophobic organic compounds in aqueous biological systems.

One-Pot Synthesis and Structure-Property Relationship of Aminomaleimides: Fluorescence Efficiencies in Monomers and Aggregates Easily Tuned by Switch of Aryl and Alkyl.

Organic fluorophores have attracted great interest owing to their wide applications. They usually contain an electron-conjugated system with an aromatic moiety and show high emission in dilute solutions but weaker or even no emission upon aggregation. Here, a simple one-pot, three-component reaction (3CR) (method I) for the synthesis of various di- and monosubstituted aminomaleimides (DAMIs and MAMIs) has been developed, and the reported 3CR (method II) has been found to be efficient only for the synthesis of MAMIs with R2 = alkyl. Twelve AMIs were designed and synthesized for investigation of the influence of structures on their optical properties in monomers and aggregates. It was found that alkyl MAMIs, alkyl DAMIs, and aryl AMIs/DAMIs show very different fluorescence efficiencies in different solvents, and only MAMIs with butyl and oleyl show high emissions in powders similar to those in nonpolar solutions. Single-crystal structures indicate that their fluorescence efficiencies in aggregates mainly correlate with molecular packing modes. The efficient synthesis method, the sensitive fluorescence on-off response to protic solvents or polar solvents, and the unusual high emissions of AMI without any aromatic moiety in both monomer and aggregates are expected to attract great interest in the fields of application and theory.