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Amino acid-tuned self-assembly has become an attractive strategy for constructing various functional materials. Here, a series of dibenzocyclooctyne (DIBO) functionalized amphiphilic amino acid derivatives are designed and screened as building blocks of functional supramolecular self-assembly nanoparticles for cancer immunotherapy. One top-performing supramolecular self-assembly material (named DA6C1) is identified through combinatorial screening, and spherical nanoparticles can be easily prepared by this material tuned multicomponent synergistic self-assembly of ovalbumin (OVA) and CpG oligonucleotide. DA6C1 based nanovaccine can significantly enhance the cellular uptake of OVA and CpG into the same bone marrow derived dendritic cells (BMDCs) and greatly improve the activation of DCs. Moreover, after subcutaneous injection, this nanovaccine flows rapidly to the lymph nodes and elicits strong immune responses to achieve effective prophylactic and therapeutic effect. Therefore, our work highlights the great potential of clickable amino acid derivatives as a convenient and powerful tool to construct nanovaccine for effective immunotherapy.

Photocontrolled polymerization offers a convenient way to direct the reaction progress and tailor the polymer structures. Nevertheless, conjugated polymers are yet to be utilized as the photocatalyst in associated reactions. Herein, we employed poly(boron dipyrromethene

Due to the excellent properties including high specificity, low side-effect and good biocompatibility, conjugated polymer nanomaterials have been served as efficient anticancer reagents in the past decades. According to the developed anticancer systems based on conjugated polymer nanomaterials, it could be summarized into three main cancer therapy strategies: photodynamic therapy(PDT), photothermal therapy(PTT) and combination therapy. In this mini review, we provide a brief introduction to three different cancer therapy modes, their mechanisms and potential biological applications. Furthermore, some perspectives on the further development of conjugated polymer nanomaterials are proposed in the territory of anticancer precision medicine.

Molecular biomarkers, especially DNA methylation, are crucial discoveries for early detection of cancer. Compared with a single biomarker detection mode, using the conjoint detection mode can allow researchers to easily assess the association of the biomarkers with specific cancer. In this paper, we calculated the methylation status of

In this work, we designed and synthesized a new cationic conjugated polyfluorene tagging with phenylboronic acid groups (PFP–PBA) for controllable cell membrane imaging. By balancing the synergistic effect of dynamic covalent bonds and electrostatic interactions between positively charged PFP–PBA and negatively charged cell membrane, the controllable cell membrane imaging could be realized. These findings demonstrated that conjugated polymers could be used as effective materials for regulating interactions with cells to develop controllable self-assembly systems for various biological applications.

Hydrogen-bonded drug conjugation is highly expected as the next-generation smart therapeutic agent that remains stable in biological medium. A carrier design strategy of hydrogen-bonded drug conjugates as pendants in conjugated polymer nanogel is developed. The H-bond acceptor uracil-functionalized poly(

Cationic conjugated polymers (CCPs) have been attracting a lot of attention in biomedical applications because of their good photoelectric properties and good cell viability. However, positively charged components may reduce the electrostatic repulsion among red blood cells (RBCs) and induce RBC aggregation, which may lead to thrombus. Herein, in this work, we prepared the complexes of CCPs and outer membrane vesicles (OMVs) to inhibit RBC aggregation induced by CCPs and improve the biocompatibility of CCPs. A poly(fluorene-co-phenylene) derivative (PFP), a poly(p-phenylenevinylene) derivative (PPV), and a poly(thiophene) derivative (PMNT) were chosen as the model CCPs, and OMVs were used as the representative of a cell membrane. The CCP–OMV complexes were formed mainly driven by electrostatic interactions. Besides, the electrostatic CCP–OMV complexes were proved to be able to prevent the RBC aggregation induced by CCPs while maintaining the hydrophobic interactions between CCPs and RBCs.

Misfolding and abnormal assembly of proteins cause many intractable diseases. The modulation of the assembly process of these proteins could contribute to understanding and controlling amyloid protein aggregation. Previous works focused mainly on the inhibition of the assembly process. To broaden the interaction modality of modulators with proteins for developing new modulators, in this work, we designed and synthesized two reactive poly ( p-phenylene vinylene) polymers, respectively, functionalized with N-hydroxysuccinimide ester (PPV-NHS) and pentafluorophenol ester (PPV-PFP), which exhibited the prevention or co-assembly effect on the aggregation process of islet amyloid polypeptide (IAPP). Cell assays demonstrated that both of the two polymers could effectively eliminate the cytotoxicity of IAPP. Moreover, PPV-NHS also could irreversibly disrupt preformed IAPP fibrils. We envision that PPV-NHS and PPV-PFP might offer a new design method for the modulation of protein assembly.

Owing to the misuse of antibiotics and slow development of new drugs, antibiotic-resistant pathogens have become a serious threat to human health. With the aim of developing new antimicrobial agents, we designed and synthesized a new conjugated polymer (PFPhim), which possesses an imidazolium containing backbone. The cationic backbone enables it to strongly interact with bacterial membrane leading to an antimicrobial ability that is more potent than that of a conjugated polymer containing a neutral backbone. PFPhim also displays strong photodynamic antimicrobial activity.

Cell surface engineering with functional polymers is an effective strategy to modulate cell activity. Here, a bio-palladium catalyzed polymerization strategy was developed for in situ synthesis of conjugated polymers on living cell surfaces. Through Sonagashira polymerization, photoactive polyphenyleneethynylene (PPE) is synthesized on the cell surface via cell-generated bio-Pd catalyst. The in situ formed PPE is identified by excellent light-harvest capacity and blue fluorescence on the surfaces of E. coli and C. pyrenoidosa. Besides imaging microbes for tracing the polymerization process, PPE also exhibits enhanced antibacterial activity against E. coli. It can also augment the ATP synthesis of C. pyrenoidosa through enlarging the light absorption and accelerating the cyclic electron transport of the algae. With this bio-metal catalyzed polymerization method, functional polymers can be synthesized in situ on the living cell surface.

Nucleic acids are natural biopolymers of nucleotides that store, encode, transmit and express genetic information, which play central roles in diverse cellular events and diseases in living things. The analysis of nucleic acids and nucleic acids-based analysis have been widely applied in biological studies, clinical diagnosis, environmental analysis, food safety and forensic analysis. During the past decades, the field of nucleic acids analysis has been rapidly advancing with many technological breakthroughs. In this review, we focus on the methods developed for analyzing nucleic acids, nucleic acids-based analysis, device for nucleic acids analysis, and applications of nucleic acids analysis. The representative strategies for the development of new nucleic acids analysis in this field are summarized, and key advantages and possible limitations are discussed. Finally, a brief perspective on existing challenges and further research development is provided.

A thermo-responsive conjugated polymer, PFBT-gPA is synthesized by grafting the poly(N-isopropylacrylamide) (PNIPAAm) to the side chains of a conjugated polyfluorene derivative through atom transfer radical polymerization (ATRP). PFBT-gPA undergoes a reversible phase transition in water below and above the lower critical solution temperature (LCST) and the process is studied by differential scanning calorimetry (DSC) analysis and UV/vis absorption spectra. PFBT-gPA shows a good photostability under UV light irradiation especially above the LCST. Moreover, the photosensitizing performance of PFBT-gPA could be tuned simply by changing temperature. The unique properties of PFBT-gPA promise its potential applications in sensing and photodynamic therapy.

The construction of intelligent self-assembly systems with cancer targeting photodynamic therapy abilities is highly required for increasing the precise therapeutic efficiency in clinical treatment. Herein, a cationic water soluble conjugated polymer (PFT-SH) functionalized with thiol groups was designed and synthesized via a palladium-catalyzed Suzuki coupling reaction. Firstly, PFT-SH can enter cells and form loose aggregations by hydrophobic and π–π stacking interactions. Secondly, a high level of H2O2 in cancer cells oxidizes sulfhydryl groups to disulfide bonds and then forms more and larger aggregations. Finally, PFT-SH showed remarkable ROS producing ability under white light irradiation with 78% quantum yields (ΦΔ). Due to this unique self-aggregation property, PFT-SH was successfully used to achieve in situ self-assembly specifically inside cancer cells for targeted imaging. Both the specific aggregation of PFT-SH in cancer cells and its ROS producing ability led to its use in the targeted killing of cancer cells through efficient photodynamic therapy.

Carriers that can afford tunable physical and structural changes are envisioned to address critical issues in controlled drug delivery applications. Herein, photo-responsive conjugated polymer nanoparticles (CPNs) functionalized with donor-acceptor Stenhouse adduct (DASA) and folic acid units for controlled drug delivery and imaging are reported. Upon visible-light (λ=550 nm) irradiation, CPNs simultaneously undergo structure, color, and polarity changes that release encapsulated drugs into the cells. The backbone of CPNs favors FRET to DASA units boosting their fluorescence. Notably, drug-loaded CPNs exhibit excellent biocompatibility in the dark, indicating perfect control of the light trigger over drug release. Delivery of both hydrophilic and hydrophobic drugs with good loading efficiency was demonstrated. This strategy enables remotely controlled drug delivery with visible-light irradiation, which sets an example for designing delivery vehicles for non-invasive therapeutics.

To take advantage of the excellent optical properties of conjugated polymers (CPs) or conjugated oligomers (COs) for biological applications, there is still a requirement to find new ways to deliver these conjugated molecular materials into cells in a facile, controllable, and noninvasive manner. Herein, a photoactive oligo( p-phenylenevinylene) (OPV) derivative was covalently attached with phospholipid units (OPV-lipid) to enhance its dispersion in water and facilitate its internalization by cells. OPV-lipid could be delivered into either the cell membrane or cytoplasm controllably through the assistance of liposomes with different formulas. It could also act as a fluorescent probe for cell imaging and visualization of the delivery process. This work shows a good potential for delivering functional conjugated molecular materials into cells in a controllable way.

The emergence of drug-resistant bacterial strains makes antimicrobial treatment a big challenge. Thus, more novel and effective antimicrobial agents and treatments are urgently desired. Herein, we developed a facile and rapid photothermal antimicrobial nanoplatform based on near-infrared (NIR)-active and photothermal-responsive conjugated polymer nanoparticles (CPNs) functionalized with cell-penetrating peptide (CPNs-Tat). With a positively charged Tat peptide, CPNs-Tat could enhance the interaction with bacteria cells with the formation of CPNs-Tat/bacteria aggregation. Under NIR irradiation, CPNs-Tat could convert the light into heat efficiently and produce local hyperthermia to kill bacteria within a few minutes. This photothermal-responsive strategy offers a rapid and effective modality for combating bacterial infections.

A conjugated polymer-based supramolecular system is designed for discrimination of virus and microbes. The supramolecular system is composed of cationic polythiophene derivative (PT) and barrel-shaped macrocyclic molecular cucurbit[7]uril (CB[7]). Because PT and PT/CB[7] complexes possess different interaction manners toward virus and microbes, the rapid and simple discrimination of virus and microbes was realized through polymer fluorescence intensity change assisting with standard linear discriminant analysis (LDA). The supramolecular strategy would expand the idea of designing biological probes and further promote the extensive application of conjugated polymer materials in biosensor field.

In this work, a new photoelectrochemical (PEC) cytosensor was constructed by using cationic polyfluorene derivative, poly(9,9-bis(6'-(N,N,N,-trimethylammonium)hexyl)fluorene-co-alt-1,4-phenylene)bromide (PFP) as the photoelectric-responsive material for sensitive cell detection. Positive-charged PFP with high photoelectric conversion efficiency can generate robust photocurrent under light illumination. In the PEC cytosensor, 3-phosphonopropionic acid was linked to the indium tin oxide electrode, followed by modification with antiepithelial-cell-adhesion-molecule (EpCAM) antibody via amide condensation reaction. Thus, target SKBR-3 cells with overexpressed EpCAM antigen could be captured onto the electrode via the specific antibody-antigen interactions. Upon adding cationic PFP, a favorable electrostatic interaction between cationic PFP and negatively charged cell membrane led to a turn-on detection signal for target SKBR-3 cells. This new cytosensor not only exhibits good sensitivity because of the good photoelectric performance of conjugated polymers, but also offers decent selectivity to target cells by taking advantage of the specific antibody-antigen recognition.

In recent years, conjugated polymers (CPs) characterized with excellent optical properties and versatile chemical structures have become popular species for biological sensing and imaging. Many creative strategies have been proposed to furnish CPs with distinguished properties or integrate CPs with other functional moieties to form multifunctional materials, which have been widely applied in different biological conditions, ranging from in vitro to in vivo experiments. This review provides a brief introduction to recent strategies for constructing these CP-based materials for biological sensing and imaging applications, where the design strategies of the two basic components (backbones and side chains) of CPs are firstly highlighted, followed by the construction of CP-based composites including nanoparticle strategies and hybridization strategies. The challenges and opportunities in this field are also discussed in this review.

Unraveling the transformation of coagulants and their interaction with contaminants at the micro-level is vital to advancing our understanding of the coagulation mechanism. To the best of our knowledge, the coagulation effectiveness of [AlO4Al12(OH)24(H2O)12]7+ (Al13), regarded as the dominant species in polyaluminum chloride (PACl), is highly related to its aggregation characteristic, but the detailed process of Al13 aggregation in coagulation time scale was not well studies. Here we systematically studied the deprotonation and aggregation processes of Al13 by alkaline titration to simulate the reaction in coagulation case. By reacting with OH−, Al13 can continuously lose protons regardless of pH until its positive charge was well neutralized. The initial Al13 aggregates (Al13agg) appeared at B of 2.70 and large Al13agg was generated by coalescence of small initial Al13agg. Most Al13 polycations kept their main structure unchanged during aggregation and part was decomposed into monomers or oligomers. Density functional theory (DFT) results reveal that Al13 becomes unstable after deprotonation, but the aggregation of Al13 bridged by Al monomers can stabilize the polycations. Al13 needs to be hydrolyzed before interacting with colloidal particles, but particles can promote the aggregation of Al13 by weakening the repulsion force between the polymers. Strong and compact flocs can be generated induced by in-situ aggregation of Al13 in neutral and alkaline conditions. This study can provide a deep understanding about the role of Al13agg in removing particles and instruct the development of new efficient coagulants against the various water qualities.

The effective removal of humic acid (HA) by coagulation has been extensively investigated for water treatments. However, the limitations of pH variation and excessive residual aluminum issues were still factors needed to be considered. In this study, to investigate the coagulation mechanism for removing HA by Al13 and optimize Al13 operation for removing HA, Al13 and preformed Al13 aggregates (Al13agg) were applied to remove HA at different pH conditions. The results showed that preformed Al13agg exhibited superior HA removal performance than Al13 due to its wide pH range and low residual Al level. During coagulation, Al13 and Al13agg interacted with HA in their original status, but the DSlope325-375 difference implied that the complexation capacity between HA and Al13agg was stronger than Al13. The new peaks of HPSEC representing larger molecular weight substances were formed under acidic and neutral conditions, which indicated that HA firstly aggregated into larger complexed molecules by interacting with Al13 or its hydrolysates and was subsequently removed by forming large flocs which was completely different from Al13agg situation. Therefore, the different coagulation mechanisms played the roles in HA removal for Al13 and Al13agg which were studied in this paper. It was believed that the complexation and charge neutralization effects dominated coagulation process for Al13 while sweep flocculation and adsorption coagulation were main driving force for Al13agg in HA removing. This work provides significant understanding of HA removal by Al13 and Al13agg coagulation, which can help to design and optimize the high efficiency coagulant based on Al polycations.

Conjugated polymers (CPs) are referred to a kind of fluorescent polymer materials with delocalized π-conjugated backbones. For the last decades, cationic CPs (CCPs) have been widely used in biosensor, imaging and biomedical fields due to their good photophysical properties and solubility in water medium resulting from side chain modification with ionized moieties. In this mini-review, we mainly introduced the applications of CCPs in detection and inactivation of pathogen with typical examples, and also briefly discussed the relevant mechanisms. We hold the expectation that this mini-review can offer researchers a general reference and inspire them to construct new systems with high performances of pathogen detection and antimicrobial activity.

Optical imaging, as an important molecular imaging modality, has emerged many attractions in studying the biological or molecular events both in cell level and living subject because of its high resolution and sensitivity, noninvasive manner and low cost. Herein, we bring novel insights into a water-soluble conjugated polyelectlyte by deeply studying its properties in cells. Poly(9, 9-bis (6'- N,N,N -trimethylammonium hexyl)fluorene phenylene) (PFP), a good biosensing material, was studied in this paper. The biocompatibility of PFP was investigated in different cells, and cell cycle analysis was carried out to explore the reasons of different biocompatibility of PFP to cells. After irradiation, fluorescence enhancement of blue emission and turn-on of long-wavelength emission of PFP in HepG2 cells was observed, which was first reported as far as we know. The differentiated biocompatibility of PFP and its particular imaging properties in cancer cells can help to guide the application of conjugated polymers in cells and provide a new dimension in designing sensitive and responsive imaging materials.

Two β-cyclodextrin-attached cationic ammonium surfactants bearing a dodecyl chain (APDB) and a hexadecyl chain (APCB) were synthesized to reduce the cytotoxicity of cationic surfactants to mammalian cells and endow the surfactants with host–guest recognition sites, and three kinds of guest molecules were utilized to improve the antibacterial ability of APDB and APCB via host–guest interaction by regulating the electrostatic or hydrophobic interaction of APDB or APCB with bacteria. The guest molecules include AD-NH3+ carrying one positive charge, DB with a benzene ring group and a dodecyl chain, and single chain cationic ammonium surfactant DTAB or CTAB. Either AD-NH3+ or DB increases the killing efficacy of APCB against S. aureus at 50 μM from 59% to about 75%, while DTAB or CTAB improves the killing efficacy of APCB to more than 90%. In particular, only a very small amount CTAB can improve the antibacterial activity of APCB to a very high level, but keeps very low cytotoxicity. However, the mixtures of t...

Polymers are mostly trapped in lysosomes when they enter cells and are then expelled, otherwise they were designed to be degradable to small molecules or to sabotage lysosomes. Therefore, they have reached the limit of the unique functionalities as a whole. Different from other escaping strategies, we introduced the polarity exchanging approach to rigid-backboned conjugated polymer for controlled penetrating through endosome or lysosome membranes. With the aid of pH-sensitive cleavage of water-soluble side chain, the rigid conjugated polymer turns highly hydrophobic after it is internalized into lysosomes and then accomplishes escaping. Thus, polarity exchange of CPs could become a new strategy for their application on chemotherapeutics.

Apart from sensing and imaging, luminogens with aggregation-induced emission (AIE) are also interesting for photosensitizing. The photosensitizing behavior and bacteria-killing performance of a pyridinium-substituted tetraphenylethylene with an alkyne group (TPE-A-Py+ ) is reported herein. Interestingly, TPE-A-Py+ exhibits higher photosensitizing efficiency than TPE-Py+ (without alkyne group) when I- was used as a counteranion. This is well explained by the fact that the ΔEST between the excited singlet state (S1 ) and triplet state (T1 ) was lower for TPE-A-Py+ than for TPE-Py+ , according to theoretical calculations. Moreover, replacement of I- with other anions (PF6- , N(SO2 CF3 )2- and BPh4- ) led to a decrease of photosensitizing efficiency for TPE-A-Py+ . Notably, TPE-A-Py+ could be used as an efficient photosensitizer to photo-inactivate ampicillin-resistant (ampr ) E. coli at low concentration under white-light irradiation very quickly.

A novel supramolecular system based on conjugated polymers was developed to realize specific targeting and imaging of organelles in living cells. The carboxyl group-modified polythiophene derivative (PT) forms a complex with six histidine equipped Tat peptide via Ni2+ ion chelation, hydrogen bonds and electrostatic interactions (PT/Ni2+/Tat-His6). The complex can reassemble with RFP-His10 due to the relatively high affinity of Ni2+ towards His10-tag compared to His6-tag. Thus, the PT/Ni2+/Tat-His6 complex could selectively label and image organelles expressing His10-tag in living cells with high stability.

It is challenging to design metal catalysts for in situ transformation of endogenous biomolecules with good performance inside living cells. Herein, we report a multifunctional metal catalyst, ruthenium-coordinated oligo(p-phenylenevinylene) (OPV-Ru), for intracellular catalysis of transfer hydrogenation of nicotinamide adenine dinucleotide (NAD+ ) to its reduced format (NADH). Owing to its amphiphilic characteristic, OPV-Ru possesses good self-assembly capability in water to form nanoparticles through hydrophobic interaction and π-π stacking, and numerous positive charges on the surface of nanoparticles displayed a strong electrostatic interaction with negatively charged substrate molecules, creating a local microenvironment for enhancing the catalysis efficiency in comparison to dispersed catalytic center molecule (TOF value was enhanced by about 15 fold). OPV-Ru could selectively accumulate in the mitochondria of living cells. Benefiting from its inherent fluorescence, the dynamic distribution in cells and uptake behavior of OPV-Ru could be visualized under fluorescence microscopy. This work represents the first demonstration of a multifunctional organometallic complex catalyzing natural hydrogenation transformation in specific subcellular compartments of living cells with excellent performance, fluorescent imaging ability, specific mitochondria targeting and good chemoselectivity with high catalysis efficiency.

Apart from the wide applications in the field of electronic and optoelectronic devices, conjugated molecules have been established as useful functional materials for biological applications. By introducing hydrophilic side chains to conjugated backbones, water-soluble conjugated polymers or oligomers (CPs or COs) inherit the attractive optical and electronic properties from conjugated molecules, while their water solubility ensures interaction with biological substrates such as biomacromolecules, microorganisms, and living cells for further biological applications. Benefiting from high brightness, large extinction coefficients, excellent photostability, low cytotoxicity, stability in bodily fluids, and versatile structural modifications, water-soluble conjugated polymers and oligomers have offered powerful alternatives in a variety of biological applications including biological and chemical sensors, fluorescence imaging, disease diagnostics, and therapy. This Account will focus on our recent advances in design, synthesis, and interdisciplinary biological applications of a series of new water-soluble CP and CO materials, starting with a brief introduction to water-soluble CPs and COs and various methods and strategies developed for the preparation of advanced water-soluble CPs and COs. Since their properties can be tuned by rational design and synthesis at the level of the conjugated repeat unit and versatile pendant groups, CPs and COs provide a diverse toolbox for satisfying interdisciplinary biological applications. The application of water-soluble CPs and COs in the past five years can be broadly categorized into four areas. Specifically, integrating the unique optoelectronic properties of water-soluble CPs and COs with self-assembly and supramolecular strategies, efficacy regulation of antibiotic and anticancer drugs has been achieved, meanwhile drug resistance could be overcome and drug resistant "superbacteria" can be inhibited. For applications regulating cellular functions and biological processes, we introduce CPs and COs with the ability to regulate intracellular oxidative stress, cell-cell communication, cellular proliferation, cell membrane permeability, and quorum sensing of bacteria cells. By covalent linkage of reactive groups upon CPs and COs, these molecules are endowed with abilities like disassembly of amyloid polypeptides, biased distribution in cells, selective imaging of organelles, and distinguished interactions with biomolecules. For photothermal therapy (PTT) applications, photothermal-responsive conjugated polymer materials have been utilized for remote control of gene expression in living cells and in vivo photothermal therapy of cancer. Beyond these applications, we have achieved new interdisciplinary applications of water-soluble CP and CO materials for biological optoelectronic devices including photosynthesis, photocatalysis, and bioenergy. Specific features or properties of water-soluble CPs and COs are leveraged to bring opportunities for each of these applications. These studies open a new frontier for development of new functional conjugated molecule materials and provide better understanding of their interactions with biological systems as well as structure/property relationships. Current limitations confronted by CPs and COs are raised, and developmental direction for the future is proposed.

Photodynamic therapy (PDT) is a promising method for cancer treatment. Two parameters that influence the efficacy of PDT are the light source and oxygen supply. Herein, we prepared a system for PDT using hemoglobin (Hb)-linked conjugated polymer nanoparticles (CPNs), which can luminesce and supply oxygen. Hb catalyzes the activation of luminol, the conjugated polymer poly[2-methoxy-5-(2-ethylhexyloxy)-1,4-phenylenevinylene] (MEH-PPV) nanoparticles can absorb the chemiluminescence of luminol through chemiluminescence resonance energy transfer (CRET) and then sensitize the oxygen supplied by Hb to produce reactive oxygen species that kill cancer cells. This system could be used for the controlled release of an anticancer prodrug. The system does not need an external light source and circumvents the insufficient level molecular oxygen under hypoxia. This work provides a proof-of-concept to explore smart and multifunctional nanoplatforms for phototherapy.

Oral administration of protein is very challenging for therapeutic applications due to its instability and easy degradation in the gastrointestinal tract. Herein, we reported an approach to encapsulate native anti-inflammatory proteins in wind chimes like cyclodextrin (WCC) for efficient oral protein delivery. The amphiphilic WCC can self-assemble into nanoparticles in aqueous solution and achieve superior encapsulation of two antioxidant enzymes such as superoxide dismutase (SOD) and catalase (CAT) by simply mixing with protein solution, avoiding any extra cumbersome steps that might inactivate protein. WCC nanovehicles can effectively protect enzyme activity and enhance their intracellular delivery. SOD and CAT co-loaded WCC nanoparticles (SC/WCC) can integrate the synergistic effect of SOD and CAT for enhancing the removal of reactive oxygen species (ROS), effectively inhibit the inflammatory response by reducing the secretion of proinflammatory factors and protect cells from ROS-induced oxidative damage. In the mouse colitis model, SC/WCC administered orally was able to efficiently accumulate in the inflamed colon, significantly inhibited the expression of proinflammatory mediators and notably alleviated the symptoms related to colitis. Therefore, we believe that the strategies we described here may provide a convenient and powerful platform for the treatment of other inflammatory diseases.

Photothermal therapy (PTT) holds great promise for noninvasive cancer treatment. To fulfill this goal, highly effective and low-risk photothermal agents have been intensively explored. Here, we present a new PTT material based on conjugated polymer dots (Pdots) that exhibit strong near-infrared (NIR) absorption and high photostability. The Pdots result in a thermal response upon illumination with a NIR laser, leading to a high photothermal conversion efficiency of 65%. Thus, the photothermal ablation of cancer cells using the Pdots both in vitro and in vivo can be achieved, highlighting the potential of Pdots as a nanoplatform for clinical therapy. They also open up a new avenue to develop new photothermal therapeutic materials.

In this work, a multifunctional platform based on the versatile function of cationic poly(p-phenylene vinylene) (PPV) derivative has been developed for white light-enhanced siRNA delivery in a remote control manner. Conjugated polyelectrolyte PPV, which possesses cationic and amphipathic features, can effectively self-assemble with siRNA and deliver siRNA into living cells. More importantly, PPV can sensitize surrounding oxygen into reactive oxygen species (ROS) upon exposure to white light and disrupt the endosomal membrane, and the resulting enhanced endosomal escape increases the gene silencing ability of siRNA. Besides, due to high fluorescent emission, PPV can also be used to image the siRNA delivery and intracelluar location. Therefore, by taking full advantage of PPV, this strategy provides a new enhanced siRNA delivery in a non-invasive and spatiotemporal photochemical manner.

Oxidative stress stimulated by angiotensin II (Ang II) plays an important role in the progression of inflammation and cardiovascular disease. In this work, polythiophene modified with dihydropyridine groups (PTDHP) realized the control of oxidative stress induced by Angiotensin II stimulation in living cells, by inhibiting the activity of NADPH oxidase via DHP groups. Upon light irradiation, the PTDHP could sensitize surrounding oxygen molecules to generate reactive oxygen species (ROS). The generated ROS oxidized the pendant DHP of polythiophene into pyridine group, which inactivated the control ability of DHP to oxidative stress in living cells. Thus, PTDHP can not only control the intracellular oxidative stress effectively and suppress ROS to some degree in dark, but also regulate its anti-oxidative effect under light irradiation.

The detection of pathogens plays a crucial role in clinical applications. In recent years, conjugated polymers are favorable in chemical and biological detections due to their remarkable light harvesting and optical signal amplification characteristics. However, most of the conjugated polymers exhibit cytotoxicity due to their rigid and hydrophobic backbone. To circumvent these deficiencies, one promising strategy is to develop a non-conjugated polymer with fluorescence, low-toxic and water-soluble characteristics. In this paper, we describe the synthesis and characterization of a novel water-soluble non-conjugated polymer (P1) containing chromophores with groups of quaternary ammonium cations in the side-chains and non-conjugated linkers of oligo(ethylene glycol) (OEG), the capability of which would not only increase the flexibility and hydrophilicity of the main-chain, but also reduce nonspecific adsorption to proteins and cell surfaces of microbial pathogens. Thus, through the balance between pendent groups of quaternary ammonium cations and OEG linkers, self-luminous P1 molecules could realize visual optical discrimination and detection of three kinds of microbial pathogens rapidly and simply by using a fluorescence microscope.

The employment of physical light sources in clinical photodynamic therapy (PDT) system endows it with a crucial defect in the treatment of deeper tissue lesions due to the limited penetration depth of light in biological tissues. In this work, we constructed for the first time an electric driven luminous system based on electrochemiluminescence (ECL) for killing pathogenic bacteria, where ECL is used for the excitation of photosensitizer instead of a physical light source to produce reactive oxygen species (ROS). We named this new strategy as ECL-therapeutics. The mechanism for the ECL-therapeutics is dependent on the perfect spectral overlap and energy transfer from the ECL generated by luminol to photosensitizer, cationic oligo(p-phenylenevinylene) (OPV), to sensitize the surrounding oxygen molecule into ROS. Furthermore, taking into account the practical application of our ECL-therapeutics, we used flexible hydrogel to replace the liquid system to develop hydrogel antibacterial device. Because the chemical reaction is a slow process in the hydrogel, the luminescence could last for more than 10 min after only electrifying for five seconds. This unique persistent luminescence characteristic with long afterglow life makes them suitable for persistent antibacterial applications. Thus, stretchable and persistent hydrogel devices are designed by integrating stretchable hydrogel, persistent ECL and antibacterial function into hydrogel matrices. This novel strategy avoids the employment of external light source, making it simple, convenient and controllable, which exploits a new field for ECL beyond sensors and also opens up a new model for PDT.

A new functional polyfluorene derivative containing quinoline skeleton and quarternary ammonium group (QAG) modified side chains (PFPQ) was synthesized and characterized. The multimodal antimicrobial effect toward Gram-negative E. coli was achieved by the dark toxicity resulting from the quinoline skeleton, QAG, and light toxicity resulting from reactive oxygen species (ROS) produced by the main backbone of PFPQ under white light. The mechanism of interaction between PFPQ and bacteria was also demonstrated. PFPQ bound to E. coli mainly through electrostatic interactions causing nearly 50% bacterial death in the absence of light irradiation, and the huge capability of PFPQ to generate ROS under white light opened another bactericidal mode. The killing efficiency was more than 99% upon relatively mild irradiation under white light (400-800 nm) with a light dose of 18 J·cm(-2). PFPQ with the incorporation of quinoline into the backbones will provide a new versatile strategy to achieve the multimodal antimicrobial effect to fight against resistant bacteria.

Conjugated polymers (CPs) have gained increasing attention as an optical platform for sensitive detection of biomacromolecules and fluorescent imaging in cellular and animal level due to its excellent light-harvesting and light-amplifying properties. Over the past decades, in order to meet the needs of multi-color fluorescent detection and imaging, researchers have designed and developed a series of multicolor fluorescent systems based on the fluorescence resonance energy transfer properties of conjugated polymers (CPs-FRET). The advantages of these systems include high brightness, excellent photostability, and low cytotoxicity. Multicolor fluorescence encoded detection of target molecules and fluorescence imaging can be achieved using such systems under a single excitation wavelength. In this tutorial review, we describe the FRET mechanism of CPs and the preparation of CPs-FRET based multicolor fluorescent systems, provide a brief review of the recent research progress of such systems in biochemical detection and cell imaging, and discuss the current problems and future direction of such systems.

A new water-soluble conjugated poly(fluorene-co-phenylene) derivative (PFP-FB) modified with boronate-protected fluorescein (peroxyfluor-1) via PEG linker has been designed and synthesized. In the presence of H2O2, the peroxyfluor-1 group can transform into green fluorescent fluorescein by deprotecting the boronate protecting groups. In this case, upon selective excitation of PFP-FB backbone at 380 nm, efficient fluorescence resonance energy transfer (FRET) from PFP-FB backbone to fluorescein occurs, and accordingly, the fluorescence color of PFP-FB changes from blue to green. Furthermore, the emission color of PFP-FB and the FRET ratio change in a concentration-dependent manner. By taking advantage of PFP-FB, ratiometric detection of choline and acetylcholine (ACh) through cascade enzymatic reactions and further dynamic monitoring of the choline consumption process of cancer cells have been successfully realized. Thus, this new polymer probe promotes the development of enzymatic biosensors and provides a simpler and more effective way for detecting the chemical transmitter of living cells.

An optical nanoruler system based on a conjugated polyelectrolyte-silver nanoprism pair is developed for label-free protein detection by taking advantage of the metal-enhanced fluorescence effect of silver nanostructures. Antibody-antigen interactions induce a change in the metal-fluorophore distance, followed by the response of a fluorescent signal of the conjugated polyelectrolyte. The system is used to detect target antigens sensitively and selectively.

A conjugated polymer (PTDHP) was synthesized by modifying the side chain of cationic polythiophene (PT) with a dihydropyridine (DHP) group via a click reaction. PTDHP has a unique ROS self-scavenging ability through the oxidation of the DHP into a pyridine structure upon light irradiation. Thus, PTDHP achieves cell imaging with good photo-stability and low photo-cytotoxicity.

In this work, we developed a kind of novel nontoxic soft particle self-assembled by gemini surfactant (SDHC) and conjugated polymer (PMNT). The soft particle shows strong ability in incorporating into cell membrane, and alters the membrane permeability, especially under light irradiation. The anticancer activities of doxorubicin (DOX) were enhanced 6–9 times after cancer cells were treated with the soft particles under light irradiation. The cell viabilities of three kinds of cancer cells testify that this effect of the soft particles on chemotherapy is universal. This work provides a new strategy to enhance the anticancer activities of drugs.

How to reduce the resistance of certain tumor cells to paclitaxel (PTX) and related taxoid anticancer drugs is a major challenge for improving cure rates. An oligo(p-phenylenevinylene) unit with thiol groups and a PTX unit (OPV-S-PTX), which enhances drug efficacy and reverses resistance is thus designed. The mechanism involves diffusion of OPV-S-PTX into the cell, where π-π interactions lead to aggregation. Cross-linking of the aggregates via oxidation of thiol groups is favored in tumor cells because of the higher reactive oxygen species (ROS) concentration. Cross-linked aggregates "chemically lock" the multichromophore particle for a more persistent effect. The IC50 of OPV-S-PTX for tumor cell line A549 is reduced down to 0.33 × 10-9 m from that observed for PTX itself (41 × 10-9 m). Enhanced efficacy by OPV-S-PTX is proposed to proceed via acceleration of microtubule bundle formation. A549/T-inoculated xenograft mice experiments reveal suppression of tumor growth upon OPV-S-PTX treatment. Altogether, these results show that the internal cross-linking of OPV-S-PTX through ROS provides a means to discriminate between tumor and healthy cells and the formation of the chemically locked particles enhances drug efficacy and helps in reducing resistance.

Development of Raman-active materials with enhanced and distinctive Raman vibrations in the Raman-silent region (1800-2800 cm-1) is highly required for specific molecular imaging of living cells with high spatial resolution. Herein, water-soluble cationic conjugated polymers (CCPs), poly(phenylene ethynylene) (PPE) derivatives, are explored for use as alkyne-state-dependent Raman probes for living cell imaging due to synergetic-enhancement effect of alkyne vibrations in Raman-silent region compared to alkyne-containing small molecules. The enhanced alkyne signals result from the integration of alkyne groups into the rigid backbone and the delocalized π-conjugated structure. PPE-based conjugated polymer nanoparticles (CPNs) were also prepared as Raman-responsive nanomaterials for distinct imaging application. This work opens a new way into the development of conjugated polymer materials for enhanced Raman imaging.

Conjugated polymers have great potential applications in bioimaging. However, the aggregation of conjugated polymers driven by electrostatic and hydrophobic interactions in aqueous media results in the reduction of photoluminescence quantum efficiency. In present work we synthesized a carboxylate gemini surfactant [sodium 2,6-didodecyl-4-hydroxy-2,6-diaza-1,7-heptanedicarboxylate (SDHC)] to adjust the aggregation behaviors and fluorescence properties of conjugated polymers [anionic poly(2-methoxy-5-propyloxy sulfonate phenylene vinylene) (MPS-PPV) and cationic poly(3-alkoxy-4-methylthiophene) (PMNT)]. This gemini surfactant shows very low critical micellar concentration (CMC) in aqueous solution and forms vesicles above CMC. In neutral and acidic conditions, MPS-PPV combines with the SDHC vesicles mainly via hydrophobic interactions and forms the aggregates in which the photoluminescence quantum efficiency of MPS-PPV is highly enhanced from 0.1% to 27%. As to PMNT, the molecules are located in the bilayer of SDHC vesicles through both electrostatic and hydrophobic interactions, and this structure prevents the production and release of reactive oxygen species. Moreover, SDHC is nontoxic and can effectively decrease the dark- and photocytotoxicity of MPS-PPV and PMNT, laying a good foundation for their bioimaging application. The living cell imaging indicates that the surfactant/conjugated polymer aggregates can stain the MCF-7 cells with main location in the lysosome. This work provides insight into how to improve the fluorescence properties and bioimaging applications of conjugated polymers by surfactants.

In this work, we demonstrate that water-soluble conjugated polymers (PFP) have the ability to inhibit biofilm formation and eradicate mature established biofilm using reactive oxygen species (ROS) produced by PFP under white light irradiation. Upon addition of PFP to planktonic Staphylococcus aureus (S. aureus), electrostatic interactions bring cationic PFP to the surface of S. aureus, which possesses negative charges. As the amount of PFP coated on S. aureus becomes saturated, the interactions of bacteria to bacteria and bacteria to surface may be disrupted, resulting in reduced biofilm formation. After the biofilm matures, those PFP on the surface of the biofilm can generate ROS under white light irradiation, which has the ability to inactivate bacteria nearby. Once the biofilm is broken, PFP can penetrate throughthe biofilm and continuously generate ROS under irradiation, resulting in biofilm disruption. As a consequence, this makes conjugated polymers a very promising material for the disruption of biofilm in biomedical and industrial applications.

Smart hydrogels have received increasing attention for many applications. Here, we synthesized a class of cationic peptide amphiphiles that can self-assemble into hydrogels by ring-opening polymerization (ROP) and post-modification strategy. The incorporation of cationic lysine residues suppresses the formation of fibril-like structure and further the gelation ability of the samples. Sodium alginate (SA) is used to enhance the rheology performance of the hydrogels. The hydrogels exhibit pH-dependent self-assembly and the gelation behavior that enables them to be ideal smart hydrogel systems for biomedical applications. Furthermore, the as-prepared hybrid peptide hydrogels show antibacterial activity.