Ultra-High-Performance Liquid Chromatography-Electrospray Ionization-High-Resolution Mass Spectrometry for Distinguishing the Origin of Ellagic Acid Extracts: Pomegranate Peels or Gallnuts.

Ellagic acid, known for its various biological activities, is widely used. Ellagic acid from pomegranate peels is safe for consumption, while that from gallnuts is only suitable for external use. However, there is currently no effective method to confirm the source of ellagic acid. Therefore, this study establishes an analysis method using ultra-high-performance liquid chromatography-electrospray ionization-high-resolution mass spectrometry (UHPLC-ESI-HR-MS) to identify the components of crude ellagic acid extracts from pomegranate peels and gallnuts. The analysis revealed that there was a mix of components in the crude extracts, such as ellagic acid, palmitic acid, oleic acid, stearic acid, and 9(10)-EpODE. Furthermore, it could be observed that ellagic acid extracted from gallnuts contained toxic substances such as anacardic acid and ginkgolic acid (15:1). These components could be used to effectively distinguish the origin of ellagic acid from pomegranate peels or gallnuts. Additionally, a rapid quantitative analysis method using UHPLC-ESI-MS with multiple reaction monitoring (MRM) mode was developed for the quality control of ellagic acid products, by quantifying anacardic acid and ginkgolic acid (15:1). It was found that one of three ellagic acid health care products contained ginkgolic acid (C15:1) and anacardic acid at more than 1 ppm.

Golgi-targeting viscosity probe for the diagnosis of Alzheimer's disease.

Early diagnosis and intervention of Alzheimer's disease (AD) are particularly important to delay the pathological progression. Although fluorescent probes have been widely employed for investigating and diagnosing AD, their biological applications are significantly restricted due to the low penetration ability of the blood-brain barrier (BBB) in vivo. In this study, we reported the first Golgi-targeted two-photon (TP) fluorescent probe, DCM-DH, for detecting viscosity in the Golgi apparatus. The probe was rationally designed to exhibit superior analytical performance including high sensitivity, specific Golgi-targeting, efficient BBB penetration ability, and deep tissue penetration (247 µm) in the brains of AD model mice. Using the probe, we demonstrated that the fluorescence intensity in the human liver cancer cell (HepG2 cells) was higher than that of human normal liver cell (LO2 cells), and the brain viscosity of AD model mice increased significantly. We anticipate that this competent tool could be easily extended to other AD biomarkers for fundamental research on this detrimental disease.

Selenium-integrated conjugated oligomer nanoparticles with high photothermal conversion efficiency for NIR-II imaging-guided cancer phototheranostics in vivo.

Second near-infrared (NIR-II) fluorescence imaging in the range of 1000-1700 nm has great prospects for in vivo imaging and theranostics monitoring. At present, few NIR-II probes with theranostics properties have been developed, especially the high-performance organic theranostics material remains underexploited. Herein, we demonstrate a selenium (Se)-tailoring method to develop high-efficient NIR-II imaging-guided material for in vivo cancer phototheranostics. Via Se-tailoring strategy, conjugated oligomer TPSe-based nanoparticles (TPSe NPs) achieve bright NIR-II emission up to 1400 nm and exhibit a relatively high photothermal conversion efficiency of 60% with good stability. Moreover, the TPSe NPs demonstrate their photothermal ablation of cancer cells in vitro and tumor in vivo with the guidance of NIR-II imaging. It is worth noting that the TPSe NPs have good biocompatibility without obvious side effects. Thus, this work provides new insight into the development of NIR-II theranostics agents.

Metallic nanoplatforms for COVID-19 diagnostics: versatile applications in the pandemic and post-pandemic era.

The COVID-19 pandemic, which originated in Hubei, China, in December 2019, has had a profound impact on global public health. With the elucidation of the SARS-CoV-2 virus structure, genome type, and routes of infection, a variety of diagnostic methods have been developed for COVID-19 detection and surveillance. Although the pandemic has been declared over, we are still significantly affected by it in our daily lives in the post-pandemic era. Among the various diagnostic methods, nanomaterials, especially metallic nanomaterials, have shown great potential in the field of bioanalysis due to their unique physical and chemical properties. This review highlights the important role of metallic nanosensors in achieving accurate and efficient detection of COVID-19 during the pandemic outbreak and spread. The sensing mechanisms of each diagnostic device capable of analyzing a range of targets, including viral nucleic acids and various proteins, are described. Since SARS-CoV-2 is constantly mutating, strategies for dealing with new variants are also suggested. In addition, we discuss the analytical tools needed to detect SARS-CoV-2 variants in the current post-pandemic era, with a focus on achieving rapid and accurate detection. Finally, we address the challenges and future directions of metallic nanomaterial-based COVID-19 detection, which may inspire researchers to develop advanced biosensors for COVID-19 monitoring and rapid response to other virus-induced pandemics based on our current achievements.

Semi-wrapped gold nanoparticles for surface-enhanced Raman scattering detection.

Researchers have struggled to develop highly reliable and sensitive surface-enhanced Raman scattering (SERS) substrates for detecting compounds in complicated systems. In this work, a strategy by constructing Au cores with incompletely wrapped Prussian blue (PB) for highly reliable and sensitive SERS substrate is proposed. The wrapped PB layers can provide the internal standard (IS) to calibrate the SERS signal floatation, whereas the exposed surface of Au cores offers the enhancement effect. The balance between the signal self-calibration and enhancement (hence the trade-off between SERS reliability and sensitivity) is obtained by the approximate semi-wrapping configuration of PB layers on Au cores (i.e., SW-Au@PB). The proposed SW-Au@PB nanoparticles (NPs) exhibit the similar enhancement factor as the pristine Au NPs and contribute to the ultralow RSD (8.55%) of calibrated SERS signals using R6G as probe molecules. The simultaneously realized reliability and sensitivity of SW-Au@PB NPs also enables the detection of hazardous pesticide residues such as paraquat and thiram in herbal plants, with the average detection accuracy up to 92%. Overall, this work mainly provides a controllable synthetic strategy for incompletely wrapped NPs, and most importantly, explores the potential with a proof-of-concept practical application in accurate and sensitive Raman detection of hazardous substances with varying solubility.

Tex Se1-x Photodiode Shortwave Infrared Detection and Imaging.

Short-wave infrared detectors are increasingly important in the fields of autonomous driving, food safety, disease diagnosis, and scientific research. However, mature short-wave infrared cameras such as InGaAs have the disadvantage of complex heterogeneous integration with complementary metal-oxide-semiconductor (CMOS) readout circuits, leading to high cost and low imaging resolution. Herein, a low-cost, high-performance, and high-stability Tex Se1- x short-wave infrared photodiode detector is reported. The Tex Se1- x thin film is fabricated through CMOS-compatible low-temperature evaporation and post-annealing process, showcasing the potential of direct integration on the readout circuit. The device demonstrates a broad-spectrum response of 300-1600 nm, a room-temperature specific detectivity of 1.0 × 1010 Jones, a -3 dB bandwidth up to 116 kHz, and a linear dynamic range of over 55 dB, achieving the fastest response among Te-based photodiode devices and a dark current density 7 orders of magnitude smaller than Te-based photoconductive and field-effect transistor devices. With a simple Si3 N4 packaging, the detector shows high electric stability and thermal stability, meeting the requirements for vehicular applications. Based on the optimized Tex Se1- x photodiode detector, the applications in material identification and masking imaging is demonstrated. This work paves a new way for CMOS-compatible infrared imaging chips.

Fluorescent noble metal nanoclusters for contaminants analysis in food matrix.

Recently, food safety issues caused by contaminants have aroused great public concern. The development of innovative and efficient sensing techniques for contaminants detection in food matrix is in urgent demand. As fluorescent nanomaterials, noble metal nanoclusters have attracted much attention because of their ease of synthesis, enhanced catalytic activity and biocompatibility, and most importantly, excellent photoluminescence property that provides promising analytical applications. This review comprehensively introduced the synthesis method of noble metal nanoclusters, and summarized the application of metal nanoclusters as fluorescent sensing materials in the detection of pollutants, including pesticides, heavy metal, mycotoxin, food additives, and other contaminants in food. The detection mechanism of pesticide residues mostly relies on the inhibition of natural enzymes. For heavy metals, the detection mechanism is mainly related to the interaction between metal ions and nanoclusters or ligands. It is evidenced that metal nanoclusters have great potential application in the field of food safety monitoring. Moreover, challenges and future trends of nanoclusters were discussed. We hope that this review can provide insights and directions for the application of nanoclusters in contaminants detection.

The safety of Chinese medicine: A systematic review of endogenous substances and exogenous residues.

BACKGROUND: Safety and toxicity have become major challenges in the internationalization of Chinese medicine. Inspite of its wide application, security problems of Chinese medicine still occur from time to time, raising widespread concerns about its safety. Most of the studies either only partially discussed the intrinsic toxicities or extrinsic harmful residues in Chinese medicine, or briefly described detoxification and attenuation methods. It is necessary to systematically discuss Chinese medicine's extrinsic and intrinsic toxic components and corresponding toxicity detoxification or detection methods as a whole. PURPOSE: This review comprehensively summarizes various toxic components in Chinese medicine from intrinsic and extrinsic. Then the corresponding methods for detoxification or detection of toxicity are highlighted. It is expected to provide a reference for safeguards for developing and using Chinese medicine. METHODS: A literature search was conducted in the databases, including PubMed, Web of Science,Wan-fang database, and the China National Knowledge Infrastructure (CNKI). Keywords used were safety, toxicity, intrinsic toxicities, extrinsic harmful residues, alkaloids, terpene and macrolides, saponins, toxic proteins, toxic crystals, minerals, heavy metals, pesticides, mycotoxins, sulfur dioxide, detoxification, detection, processing (Paozhi), compatibility (Peiwu), Chinese medicine, etc., and combinations of these keywords. All selected articles were from 2006 to 2022, and each was assessed critically for our exclusion criteria. Studies describe the classification of toxic components of Chinese medicine, the toxic effects and mechanisms of Chinese medicine, and the corresponding methods for detoxification or detection of toxicity. RESULTS: The toxic components of Chinese medicines can be classified as intrinsic toxicities and extrinsic harmful residues. Firstly, we summarized the intrinsic toxicities of Chinese medicine, the adverse effects and toxicity mechanisms caused by these components. Next, we focused on the detoxification or attenuation methods for intrinsic toxicities of Chinese medicine. The other main part discussed the latest progress in analytical strategies for exogenous hazardous substances, including heavy metals, pesticides, and mycotoxins. Beyond reviewing mainstream instrumental methods, we also introduced the emerging biochip, biosensor and immuno-based techniques. CONCLUSION: In this review, we provide an overall assessment of the recent progress in endogenous toxins and exogenous hazardous substances concerning Chinese medicine, which is expected to render deeper insights into the safety of Chinese medicine.

Evaluation of the Biological Activity of Glucosinolates and Their Enzymolysis Products Obtained from Lepidium meyenii Walp. (Maca).

Glucosinolates (GLS) were extracted and purified from Lepidium meyenii (Maca) root. Purified GLS were analyzed without desulfation by UPLC-ESI-MS. Glucosinolates were decomposed into benzyl isothiocyanate (BITC) by thioglucosidase. DPPH radical scavenging activity, ABTS radical scavenging activity, and reducing power were used to evaluate antioxidant activity of Maca crude extract (MCE), total GLS, and BITC. Maca crude extract showed the highest antioxidant activity among them, and BITC showed no antioxidant activity at concentrations less than 10 mg/mL. Cytotoxicity on five human cancer cell lines and the inhibition rate of NO production were used to evaluate the activity of anti-cancer and anti-inflammatory of total GLS and BITC. The inhibition rate of NO production of 50 µg/mL BITC can reach 99.26% and the cell viability of 100 µg/mL BITC on five tumor cell lines is less than 3%. The results show that BITC may be used as a promising anti-cancer and anti-inflammatory drug.

Bioremediation of organic pollutants by white rot fungal cytochrome P450: The role and mechanism of CYP450 in biodegradation.

Cytochrome P450 (CYP450) is a well-known protein family that is widely distributed in many organisms. Members of this family have been implicated in a broad range of reactions involved in the metabolism of various organic compounds. Recently, an increasing number of studies have shown that the CYP450 enzyme also participates in the elimination and degradation of organic pollutants, by white rot fungi (WRF), a famous group of natural degraders. This paper reviews previous investigations of white rot fungal CYP450 involved in the biodegradation of organic pollutants, with a special focus on inhibitory experiments, and the direct and indirect evidence of the role of white rot fungal CYP450 in bioremediation. The catalytic mechanisms of white rot fungal CYP450, its application potential, and future prospect for its use in bioremediation are then discussed.

A two-step strategy for simultaneous dual-mode detection of methyl-paraoxon and Ni (â ¡).

Exogenous pollution of Chinese medicinal materials by pesticide residues and heavy metal ions has attracted great attention. Relying on the rapid development of nanotechnology and multidisciplinary fields, fluorescent techniques have been widely applied in contaminant detection and pollution monitoring due to their advantages of simple preparation, low cost, high throughput and others. Most importantly, synchronous detection of multi-targets has always been pursued as one of the major goals in the design of fluorescent probes. Herein, we firstly develop a simultaneous sensing method for methyl-paraoxon (MP) and Nickel ion (Ni, Ⅱ) by using carbon based fluorescent nanocomposite with ratiometric signal readout and nanozyme. Notably, the designed system showed excellent effectiveness even when the two pollutants co-exist. Under the optimum conditions, this method provides low limits of detection of 1.25 µM for methyl-paraoxon and 0.01 µM for Ni (Ⅱ). To further verify the reliability, recovery studies of these two analytes were performed on ginseng radix et rhizoma, nelumbinis semen, and water samples. In addition, smartphone-based visual analysis has been introduced to expand its applicability in point of care detection. This work not only expands the application of the dual-mode approach to pollutant detection, but also provides insights into the analysis of multiple pollutants in a single assay.

DNAzyme-based biosensors for mercury (â ¡) detection: Rational construction, advances and perspectives.

Mercury contamination is one of the most severe issues in society due to its threats to public health and the ecological system. However, traditional methods for mercury ion detection are still limited by their time-consuming procedures, requirement of expensive instruments, and low selectivity. In recent decades, tremendous progress has been made in the development of functional nucleic acid-based, especially DNAzyme sensors for mercury (Ⅱ) (Hg2+) determination, including RNA-cleaving DNAzymes and G-quadruplex-based DNAzymes in particular. Researchers have heavily studied the construction of Hg2+ sensors, mainly originating from in vitro selection-derived DNAzymes, by incorporating T-Hg2+-T recognition moieties in existing DNAzyme scaffolds, and interfacing Hg2+-sensitive sequences with nanomaterials. In the last case, the employment of materials (as quenchers, signal transducers and DNA immobilizers) enriches the application scenarios of current Hg2+-DNAzymes, due to a combination of their functions. We summarize a broad range of sensing approaches, including optical, electrochemical, and other sensing methods, and compare their features. This review elaborates on the rational design strategies for engineering DNAzymes to selectively sense Hg2+, critically discusses their properties in different application scenarios, and summarizes recent advances in this field. Additionally, current progress, challenges and future perspectives are also discussed. This minireview provides deeper insights into the chemistry of these functional nucleic acids when working with Hg2+, explains the design ideas of DNAzyme-sensors in each platform, and reveals potential opportunities in developing more advanced DNAzyme sensors for the highly selective and sensitive recognition of Hg2+. ENVIRONMENTAL IMPLICATION: Mercury is one of the most toxic metallic contaminants due to its high toxicity, non-biodegradability, and serious human health risks when accumulated in the body. In the recent decade, intensive studies have focused on exploring mercury sensors by combining DNAzymes with various sensing methods, paving a promising avenue to gain ultra-high sensitivity and selectivity. However, so far, no review has introduced the recent advances on DNAzyme-based sensors for mercury detection in a critical way. In this review, we comprehensively summarized the studies on DNAzyme-based sensors for mercury detection using various sensing techniques including optical, electrochemical and other sensing methods.

Pyrolysis Behaviors and Residue Properties of Iron-Rich Rolling Sludge from Steel Smelting.

Iron-rich rolling sludge (FeRS) represents a kind of typical solid waste produced in the iron and steel industry, containing a certain amount of oil and large amounts of iron-dominant minerals. Pyrolysis under anaerobic environment can effectively eliminate organics at high temperatures without oxidation of Fe. This paper firstly investigated comprehensively the pyrolysis characteristics of FeRS. The degradation of organics in FeRS mainly occurred before 400 °C. The activation energy for pyrolysis of FeRS was extremely low, ca. 5.44 kJ/mol. The effects of pyrolytic temperature, atmosphere, heating rate, and stirring on pyrolysis characteristics were conducted. Commonly, the yield of solid residues maintained around 85 wt.%, with approximately 13 wt.% oil and 2 wt.% gas. Due to the low yield of oil and gas, their further utilization remains difficult despite CO2 introduction which could upgrade their quality. The solid residues after pyrolysis exhibited porous properties with co-existence of micropores and mesopores. Combined with the high content of zero-valent iron, magnetic property, hydrophobic characteristic, and low density, the solid residues could be further utilized for water pollution control and soil remediation. Moreover, the solid residues were suitable for sintering to recover valuable iron resources. However, the solid residues also contained certain heavy metals, such as Cd, Cr, Cu, Ni, Pb, and Zn, which might cause secondary pollution during their utilization. In particular, the toxic Cr possessed high content, which should be treated with detoxification and removal. This paper provides fundamental information for pyrolysis of FeRS and utilization of solid residues.

A ratiometric fluorescent sensing system for the selective and ultrasensitive detection of pesticide residues via the synergetic effects of copper nanoclusters and carbon quantum dots.

Agricultural products, such as foodstuffs and herbal medicines, may be contaminated by pesticides. Therefore, developing sensitive methods for pesticide detection are urgently needed for the assurance of food safety. In this study, a ratiometric fluorescent sensing system based on blue-emitted nitrogen-doped carbon quantum dots (N-CQDs) and red-emitted copper nanoclusters (CuNCs) complex was fabricated for pesticide detection. The selective detection of thiram and paraquat, two typical widely used pesticides, can be easily realized by changing the solvent environment. The detection limit can be reached as low as 7.49 nM and 3.03 nM, respectively. A good linear correlation was found over the concentration range from 10 to 500 nM for thiram and 5 to 100 nM for paraquat. More interestingly, fast and visual detection of thiram and paraquat can be achieved via smartphone-based colorimetric analysis, which has provided an effective implementation for on-site monitoring of the levels of pesticide residues in food.

Copper ions assisted fluorescent detection of some dithiocarbamates based on nickel nanocluster with aggregation-induced emission enhancement behavior.

Pesticide residue contamination has become an urgent issue since it threatens both the natural environment and public health. In this study, a fluorescent method for detecting dithiocarbamate (DTC) compounds was constructed based on novel nickel nanoclusters (Ni NCs) and copper ions (Cu2+). The water-soluble fluorescent Ni NCs were synthesized for the first time through a one-pot method using glutathione as stabilizer and ascorbic acid as reducing agent. The as-prepared Ni NCs exhibited a maximum fluorescence emission at 445 nm when excited by 380 nm. And they displayed aggregation-induced emission enhancement when ethylene glycol was introduced into the nanocluster aqueous solution. Based on the Ni NCs, a label-free fluorescence quenching sensor was established for sensitive and selective detection of DTC compounds with the assistance of Cu2+. The complex formed by DTC and Cu2+ led to fluorescence quenching of Ni NCs through inner filter effect. The sensing method was successfully applied to two typical DTC compounds, thiram and disulfiram, with good linearity over a wide linear range and a low detection limit. Moreover, the proposed approach was capable of thiram detection in real samples, which confirms the potential of this sensing method as a platform for DTC compound detection.

A sensitive and simple HPLC-FLD-based method for the measurement of intracellular glucose uptake.

Glucose is a primary source of energy used in most organisms. Thus, development of reliable approaches to measure intracellular glucose uptake is an important research issue. 2-[N-(7-nitrobenz-2-oxa-1,3-diazol-4-yl) amino]-2-deoxy-d-glucose (2-NBDG), as a fluorescent glucose derivative, has been widely used to track intracellular glucose uptake by fluorescence imaging and measuring in mammalian cells. However, the avoid-less cross-interference of intrinsic autofluorescence background and tested fluorescent compounds limits its ability to provide trustworthy information on intracellular glucose uptake. By the extraction, separation and detection of 2-NBDG, a simple, sensitive and accurate HPLC-FLD method was established and validated for the measurement of intracellular glucose uptake in HepG2 cells. The developed method has been employed successfully to assess the glucose uptake activity of anti-diabetic drugs and fluorescent natural products. A fit-for-purpose partial validation was further performed for quantification and comparison of glucose uptake in AML12, LO2 hepatocytes, L6 myoblasts and 3T3-L1 preadipocytes.

Antiproliferative activity of berberine in HepG2 cells via inducing apoptosis and arresting cell cycle.

The therapeutic targets of berberine for hepatocellular carcinoma (HCC) and its detailed mechanisms remain unexplored. Here, an integration of network pharmacology, proteomic, bioinformatic and in vitro biochemical approach was proposed to reveal therapeutic targets and pathways underlying the antiproliferative activity of berberine against HepG2 cells. Results indicated that berberine caused the cytotoxicity and inhibited the growth of HepG2 cells with IC50 values ranging from 92 µM to 118 µM. Network pharmacology analysis revealed that targeting apoptosis and cell cycle pathways by berberine contributed to its antitumor efficacy against HCC. Proteomic analysis demonstrated that mitochondria-related apoptosis pathways were involved in the cytotoxic action of berberine, as evidenced by the expression of mitochondrial dysfunction-mediated proteins. Moreover, a total of 160 significantly altered proteins were screened, among which AKAP12 presented significantly increased levels under berberine treatment. Bioinformatic analysis of various public datasets showed that expression of AKAP12 in HCC liver tissues was downregulated, emphasizing its role as a tumor suppressor. Immunoblotting validated the increased levels of AKAP12, while co-immunoprecipitation identified its interaction with Cyclin D1. These data, together with flow cytometry analysis, suggested that AKAP12 mediated cell cycle arrest, thereby suppressing cell proliferation. Altogether, the antiproliferative action of berberine in HepG2 cells involves both apoptosis and cell cycle arrest. Regulating AKAP12 signalling by berberine might provide a promising strategy for HCC treatment.

Electrochemical detection of methyl-paraoxon based on bifunctional cerium oxide nanozyme with catalytic activity and signal amplification effect.

A new electrochemical sensor for organophosphate pesticide (methyl-paraoxon) detection based on bifunctional cerium oxide (CeO2) nanozyme is here reported for the first time. Methyl-paraoxon was degraded into p-nitrophenol by using CeO2 with phosphatase mimicking activity. The CeO2 nanozyme-modified electrode was then synthesized to detect p-nitrophenol. Cyclic voltammetry was applied to investigate the electrochemical behavior of the modified electrode, which indicates that the signal enhancement effect may attribute to the coating of CeO2 nanozyme. The current research also studied and discussed the main parameters affecting the analytical signal, including accumulation potential, accumulation time, and pH. Under the optimum conditions, the present method provided a wider linear range from 0.1 to 100 µmol/L for methyl-paraoxon with a detection limit of 0.06 µmol/L. To validate the proof of concept, the electrochemical sensor was then successfully applied for the determination of methyl-paraoxon in three herb samples, i.e., Coix lacryma-jobi, Adenophora stricta and Semen nelumbinis. Our findings may provide new insights into the application of bifunctional nanozyme in electrochemical detection of organophosphorus pesticide.

A review of the study of active components and their pharmacology value in Lepidium meyenii (Maca).

Lepidium meyenii (Maca) contains several active components, including alkaloids, glucosinolates, isothiocyanates, polysaccharides, polyphenols, and sterols, which make it have the traditional therapeutic uses. In this paper, we summarized the analytical progress of the active components associated with alkaloids, polysaccharides, glucosinolates, sterols, free fatty acids, flavonoids, and natural phenols in Maca by mass spectrometry (MS). Due to the effect of color and type on active components in Maca, we summarized the study of quality evaluation about Maca according to the type and the content of active components such as glucosinolates, essential oils, macamides, and macaenes by MS. Additionally, the research on the change of active components in Maca at different growth stages by MS will be beneficial to full utilization of active components in Maca and other natural resources. We reviewed the study in the visible distribution of amino acids, amide alkaloids, imidazolium alkaloids, and saccharides in Maca by imaging mass spectrometry (IMS). We also reviewed the pharmacology value associated with improvement of reproductive function, anti-stress response, anti-osteoporosis, antitumor activity, clinical research and toxicity of Maca, and so forth. Nevertheless, due to individual differences and limitations of the subjects, further high-quality studies are needed to confirm the clinical efficacy of the plant.

Conjugated Polymers: Optical Toolbox for Bioimaging and Cancer Therapy.

Conjugated polymers (CPs) are capable of coordinating the electron coupling phenomenon to bestow powerful optoelectronic features. The light-harvesting and light-amplifying properties of CPs are extensively used in figuring out the biomedical issues with special emphasis on accurate diagnosis, effective treatment, and precise theranostics. This review summarizes the recent progress of CP materials in bioimaging, cancer therapeutics, and introduces the design strategies by rationally tuning the optical properties. The recent advances of CPs in bioimaging applications are first summarized and the challenges to clear the future directions of CPs in the respective area are discussed. In the following sections, the focus is on the burgeoning applications of CPs in phototherapy of the tumor, and illustrates the underlying photo-transforming mechanism for further molecular designing. Besides, the recent progress in the CPs-assistant drug therapy, mainly including drug delivery, gene therapeutic, the optical-activated reversion of tumor resistance, and synergistic therapy has also been discussed elaborately. In the end, the potential challenges and future developments of CPs on cancer diagnosis and therapy are also illuminated for the improvement of optical functionalization and the promotion of clinical translation.