Anthraquinone Research Articles

Uptake and translocation of organic pollutants in Camellia sinensis (L.): a review.

Camellia sinensis (L.) is a perennial evergreen woody plant with the potential for environmental pollution due to its unique growth environment and extended growth cycle. Pollution sources and pathways for tea plants encompass various factors, including atmospheric deposition, agricultural inputs of chemical fertilizers and pesticide, uptake from soil, and sewage irrigation. During the cultivation phase, Camellia sinensis (L.) can absorb organic pollutants through its roots and leaves. This review provides an overview of the uptake and translocation mechanisms involving the absorption of polycyclic aromatic hydrocarbons (PAHs), pesticides, anthraquinone (AQ), perchlorate, and other organic pollutants by tea plant roots. Additionally, we summarize how fresh tea leaves can be impacted by spraying pesticide and atmospheric sedimentation. In conclusion, this review highlights current research progress in understanding the pollution risks associated with Camellia sinensis (L.) and its products, emphasizing the need for further investigation and providing insights into potential future directions for research in this field.

Influence of wood type on anthraquinone levels and quality properties of smoked chipotle pepper

This study aimed to assess the effects of pecan and mesquite wood, as well as smoking time, on anthraquinone (AQ) levels and quality properties of chipotle pepper (CHP) during the traditional smoking process. Changes in moisture content, microstructure, levels of total phenols (TPs), AQ, capsaicin (CAPS), dihydrocapsaicin (DHC), total polyphenols (TPPs), and total antioxidant activity (TAA), as well as color parameters, were measured. A wood mixture consisting of pecan, poplar, mesquite, and pine was used as the control. The CHP moisture content consistently decreased from 12 to 108 h of smoking, with long times exhibiting asymptotic trends across all treatments. Concurrently, structural changes, such as pericarp thinning and plant tissue collapse, were observed as the smoking process progressed. The wood type and processing time had a significant impact (P < 0.05) on TPs, AQ, CAPS, DHC, TAA levels, and color. TPs and AQ exhibited behavior opposite to that of the moisture content. CHP smoked in mesquite wood exhibited the highest TPs absorption rate and the lowest AQ levels. However, the AQ levels in CHP using any wood type exceeded permissible limits (0.02 mg·kg−1) at 12 h of processing, with the control exhibiting the highest AQ concentrations. The highest concentrations of CAPS and DHC were observed at 36 h in all treatments, with lower losses in mesquite wood CHP. The control exhibited the highest TAA values compared to fresh peppers. CHP color (a*, redness) decreased throughout the smoking process. The pecan and mesquite wood treatments resulted in the lowest loss of a* (P < 0.05). These results indicate that using mesquite wood for CHP production promotes higher TPs concentrations with lower AQ levels, followed by pecan wood, when compared to the control. These findings suggest the need to investigate the mechanisms of AQ formation to achieve CHP parameters within the regulatory limits with good quality.

Acryloyl esters of emodin for waterless dyeing and toxicological studies

AbstractTraditional textile dyeing processes usually require large quantities of water and energy and generate wastewater that can be harmful to the environment. Dyeing in supercritical carbon dioxide (sc‐CO2) media is promising in textile coloration due especially to it providing a waterless process and eliminating the need for an energy intensive drying step. The natural anthraquinone emodin showed promising results for dyeing different fibres through sc‐CO2 process. However, emodin is mutagenic. The aim of this study was to develop non‐mutagenic derivatives of emodin that can be applied to textiles using sc‐CO2. Emodin structure was modified incorporating acryloyl groups, which are considered suitable for decreasing potential for DNA intercalation, and thus mutagenicity. The presence of acryloyl groups would also enable atmospheric plasma induced bonding with fibres. Molecular modelling studies showed that emodin derivatives became less planar with increasing number of attached acryloyl groups, making intercalation unlikely. The derivatives produced were tested to assess mutagenicity in vitro (Salmonella/microsome assay, TA1537, 10% S9) and in vivo (micronucleus test in hemocytes of aquatic crustacean). We found that emodin can be derivatised using acryloyl chlorides to give mono‐ and di‐acrylate esters suitable for dyeing polyester fibres in sc‐CO2. However, the new dyes presented mutagenicity for both in vitro and in vivo. Although the derivatives provided greenish‐yellow alternatives to emodin for dyeing synthetic fibres, they do not appear to be viable alternatives from the point of view of preserving human and environmental health. Plasma bonding studies are underway.

Redox-Active Covalent Organic Framework with Highly Accessible Aniline-Fused Quinonoid Units Affords Efficient Proton Charge Storage.

Owing to their intrinsic safety and sustainability, aqueous proton batteries have emerged as promising energy devices. Nevertheless, the corrosion or dissolution of electrode materials in AICDic electrolytes must be addressed before practical applications. In this study, we developed a cathode material based on a redox-active 2D covalent organic framework (TPAD-COF) featuring inherently regular open porous channels and excellent stability. Benefiting from its superhydrophilicity, intrinsic high proton conductivity, excellent redox reversibility of enriched aniline-fused-quinonoid units, and the insolubility of the rigid framework skeleton, TPAD-COF cathode delivers a high capacity of 126 mAh g-1 at 0.2 A g-1 , paired with long-term cycling stability with capacity retention of 84% after 5,000 cycles at 2 A g-1 . Comprehensive ex-situ spectroscopic studies correlated with density functional theory (DFT) calculations revealed that both the -NH- and C = O groups of the aniline-fused quinonoid units exhibited prominent redox activity of six electrons during the charge/discharge processes. Furthermore, the assembled punch battery consisting of a TPAD-COF//anthraquinone (AQ) all-organic system delivers a discharge capacity of 115 mAh g-1 at 0.5 A g-1 after 130 cycles, implying the potential applications of TPAD-COF cathode in aqueous proton batteries. This study provides a new perspective on the design of electrode materials for aqueous proton batteries with long-term cycling performance and high capacity. This article is protected by copyright. All rights reserved.

Emodin reduces surgical wounding-accelerated tumor growth and metastasis via macrophage suppression in a murine triple-negative breast cancer model.

It has been suspected that tumor resection surgery itself may accelerate breast cancer (BC) lung metastasis in some patients. Emodin, a natural anthraquinone found in the roots and rhizomes of various plants, exhibits anticancer activity. We examined the perioperative use of emodin in our established surgery wounding murine BC model. Emodin reduced primary BC tumor growth and metastasis in the lungs in both sham and surgical wounded mice, consistent with a reduction in proliferation and enhanced apoptosis (primary tumor and lungs). Further, emodin reduced systemic inflammation, most notably the number of monocytes in the peripheral blood and reduced pro-tumoral M2 macrophages in the primary tumor and the lungs. Consistently, we show that emodin reduces gene expression of select macrophage markers and associated cytokines in the primary tumor and lungs of wounded mice. Overall, we demonstrate that emodin is beneficial in mitigating surgical wounding accelerated lung metastasis in a model of triple-negative BC, which appears to be mediated, at least in part, by its actions on macrophages. These data support the development of emodin as a safe, low-cost, and effective agent to be used perioperatively to alleviate the surgery triggered inflammatory response and consequential metastasis of BC to the lungs.

Molecular docking analysis of HSV-1 proteins models with synthetic and plant derived compounds.

The atomic resolution model of US9, UL20, and gH protein of HSV is known. Hence, the ligand protein interaction of the US9, UL20, and gH protein models were carried out with synthetic drugs like acyclovir, bexarotene, vinorelbine, foscarnet, famciclovir, cidofovir and two plant derived natural drug acacetin and anthraquinone. Based on structure and docking study, it is predicted that protein US20 and gH binds with particular anti-HSV drug i.e. acyclovir, cidofovir, acacetin and famciclovir, acacetin respectively, while interaction of different protein is different with drugs.

Rhein attenuates cerebral ischemia-reperfusion injury via inhibition of ferroptosis through NRF2/SLC7A11/GPX4 pathway

BackgroundIschemic stroke, a major cause of death and disability worldwide, results from reduced blood flow to the brain, leading to irreversible neuronal damage. Recent evidence suggests that ferroptosis, a form of regulated cell death, plays a critical role in the pathogenesis of ischemic stroke. Rhein, a natural anthraquinone compound, has demonstrated neuroprotective effects; However, its role in ferroptosis and the underlying mechanisms remain unclear. Here, we investigated the protective effects of Rhein against ischemia/reperfusion (I/R) injury in a rat model of middle cerebral artery occlusion (MCAO) and oxygen-glucose deprivation/reperfusion (OGD/R)-induced HT22 cells. Rhein treatment dose-dependently ameliorated neurological deficits, reduced infarct volume, and attenuated blood-brain barrier (BBB) disruption in the MCAO model. Furthermore, Rhein suppressed oxidative stress, intracellular ROS generation, and ferroptosis-related protein expression in both in vivo and in vitro models. Mechanistically, Rhein protected against OGD/R-induced HT22 cell injury by regulating the NRF2/SLC7A11/GPX4 signaling pathway. This effect was abolished upon NRF2 inhibition, suggesting that Rhein's neuroprotective action is NRF2-dependent. Molecular docking and microscale thermophoresis analyses further supported the direct interaction between Rhein and the ferroptosis-related protein NRF2. Collectively, our findings reveal that Rhein confers neuroprotection against cerebral I/R injury by inhibiting ferroptosis via the NRF2/SLC7A11/GPX4 axis, providing a potential therapeutic avenue for ischemic stroke. AimsTo investigate the neuroprotective effects of Rhein, a natural anthraquinone compound, against ischemia/reperfusion (I/R) injury and elucidate the underlying mechanisms involving ferroptosis and the NRF2/SLC7A11/GPX4 pathway. MethodsA rat model of middle cerebral artery occlusion (MCAO) was employed for in vivo assessments, while oxygen-glucose deprivation/reperfusion (OGD/R)-induced HT22 cells were used as an in vitro model. Comprehensive analyses, including neurological score assessment, triphenyl tetrazolium chloride staining, Evans Blue leakage assay, intracellular ROS detection, MTT assay, dual-luciferase reporter assay, oxidative stress and Fe2+ content assessment, immunofluorescence, Western blot, flow cytometry, molecular docking, and microscale thermophoresis, were performed to evaluate the effects of Rhein on I/R injury and ferroptosis. ResultsRhein conferred dose-dependent neuroprotection against cerebral I/R injury, reducing infarct volume and blood-brain barrier (BBB) disruption in the MCAO model. In both in vivo and in vitro models, Rhein suppressed oxidative stress, intracellular ROS generation, and ferroptosis-related protein expression. Furthermore, Rhein protected HT22 cells from OGD/R-induced injury by regulating the NRF2/SLC7A11/GPX4 signaling pathway, with NRF2 inhibition abolishing these therapeutic effects. Molecular docking and microscale thermophoresis analyses supported a direct interaction between Rhein and NRF2, a ferroptosis-related protein. ConclusionRhein attenuates cerebral I/R injury by inhibiting ferroptosis via the NRF2/SLC7A11/GPX4 axis, highlighting its potential as a therapeutic agent for ischemic stroke.

Lac dye-based intelligent colorimetric indicator for real-time freshness monitoring of packaged white button mushrooms (Agaricus bisporus)

The study aimed to develop an intelligent real-time freshness indicator for white button mushrooms by immobilizing the lac dye, a natural anthraquinone dye on filter paper. The indicator was characterized for its pH responsiveness; structural, mechanical, thermal properties; and color stability. During the freshness test, mushrooms were packed in punnet with an indicator placed in the package headspace and stored at two different temperatures (4 °C and 25 °C). Mushroom spoilage was monitored concurrently by indicator's color change, physicochemical indices, and volatile organic compounds (VOC) generated during storage. The FTIR results revealed that dye was immobilized on matrix via hydrogen bonding. A slight reduction in matrix crystallinity post dye immobilization was observed. However, the thermal and mechanical properties remained unaffected. Indicator showed good color stability during one month storage at 4 °C and 25 °C. The indicator changed its color from orange-red (at acidic pH) to purple (at alkaline pH) due to the inherent properties of lac dye. In the freshness test, the visual color change of indicator distinguished mushrooms into three stages: ' fresh', 'medium fresh', and 'spoiled'. Principle Component Analysis (PCA) validated the synchronization between color change of indicator and quality parameters. Partial Least Square (PLS) regression models derived from indicator's color parameter data successfully predicted the physicochemical indices of mushrooms stored at 4 °C. The lac dye-based indicators emerged as a novel and potential solution for non-destructive freshness monitoring of white button mushrooms.

A Comprehensive Review on Therapeutic Potential of a Natural Anthraquinone Derivative Emodin in Brain-related Disorders.

Brain-related disorders are one of the world's most important and complex health problems today. These brain-related disorders are responsible for a massive number of morbidities and death all around the world. However, researchers have devoted a large amount of time to investigating these diseases and found positive results; nevertheless, there are currently quite a few medications available to treat them. Emodin (EM), a polyphenol compound, has many health benefits. It is a biologically active monomer derived from rhubarb root that exhibits anti-inflammation, anti-oxidation, anticancer, and neuroprotective properties. A series of preclinical trials have shown EM to have protective benefits against many brain-related diseases. This review has evaluated the potential of EM as a pharmacological agent for the treatment and management of various brain-related disorders based on the findings of multiple pre-clinical studies and taking into account the compound's therapeutic properties.

Facet-engineered photo-induced charge transfer dynamics at the interface of cubic CsPbBr3 and organic acceptor molecules

Perovskite, particularly halide perovskite shows tremendous application in the field of optoelectronic devices such as Light emitting diode (LED) and solar cells. Semiconducting nanomaterials like perovskite nanomaterials have photoactive components and are used as electron as well as hole donors. A hybrid combination of organic acceptors such as Anthraquinone (AQ) and Tetracyanoquinodimethane (TCNQ) with CsPbX3 (X = Cl, Br, I) perovskite nanomaterials at the interface is a unique path for charge separation. The surface of the perovskite nanomaterial plays an important role in the electron-hole charge separation. The surface of the perovskite nanomaterial is responsible for the interaction between this redox couple. Only those molecules show better charge separation which interacts more efficiently with the excited state of the perovskite nanocrystals (PNCs), but very few organic molecules show this kind of redox properties. In the present study, we employed AQ and TCNQ to extract charges from PNCs. We performed photoluminescence (PL) and time-correlated single photon count spectroscopy (TCSPC) to investigate the impacts of both organic acceptor molecules on the lifetime and photoluminescence (PL) of PNCs. PNCs possessed distinct lifetime and luminous characteristics prior to and after the incorporation of quenchers, however, in the case of TCNQ, improved charge separation occurred, as evidenced by PL and TCSPC. We additionally employed SEM (scanning electron microscopy) and TEM (transmission electron microscopy) to investigate the influence of the quencher on morphology.

RNA Sequencing and Bioinformatics Analysis Reveals the Downregulation of DNA Replication Genes by Morindone in Colorectal Cancer Cells.

Morindone, a natural anthraquinone compound, has been reported to have significant pharmacological properties in different cancers. However, its anticancer effects in colorectal cancer (CRC) and the underlying molecular mechanisms remain obscure. In this study, RNA sequencing was used to assess the differentially expressed genes (DEGs) following morindone treatment in two CRC cell lines, HCT116 and HT29 cells. Functional enrichment analysis of overlapping DEGs revealed that negative regulation of cell development from biological processes and the MAPK signalling pathway were the most significant Gene Ontology terms and Kyoto Encyclopaedia of Genes and Genome pathway, respectively. Seven hub genes were identified among the overlapping genes, including MCM5, MCM6, MCM10, GINS2, POLE2, PRIM1, and WDHD1. All hub genes were found downregulated and involved in DNA replication fork. Among these, GINS2 was identified as the most cancer-dependent gene in both cells with better survival outcomes. Validation was performed on seven hub genes with rt-qPCR, and the results were consistent with the RNA sequencing findings. Collectively, this study provides corroboration of the potential therapeutic benefits and suitable pharmacological targets of morindone in the treatment of CRC.

A mannitol-modified emodin nano-drug restores the intestinal barrier function and alleviates inflammation in a mouse model of DSS-induced ulcerative colitis

BackgroundUlcerative colitis (UC) is an inflammatory disease of the colon that is characterized by mucosal ulcers. Given its increasing prevalence worldwide, it is imperative to develop safe and effective drugs for treating UC. Emodin, a natural anthraquinone derivative present in various medicinal herbs, has demonstrated therapeutic effects against UC. However, low bioavailability due to poor water solubility limits its clinical applications.MethodsEmodin-borate nanoparticles (EmB) were synthesized to improve drug solubility, and they modified with oligomeric mannitol into microgels (EmB-MO) for targeted delivery to intestinal macrophages that express mannose receptors. UC was induced in a mouse model using dextran sulfate sodium (DSS), and different drug formulations were administered to the mice via drinking water. The levels of inflammation-related factors in the colon tissues and fecal matter were measured using enzyme-linked immunosorbent assay. Intestinal permeability was evaluated using fluorescein isothiocyanate dextran. HE staining, in vivo imaging, real-time PCR, and western blotting were performed to assess intestinal barrier dysfunction.ResultsBoth EmB and EmB-MO markedly alleviated the symptoms of UC, including body weight loss, stool inconsistency, and bloody stools and restored the levels of pro- and anti-inflammatory cytokines. However, the therapeutic effects of EmB-MO on the macroscopic and immunological indices were stronger than those of EmB and similar to those of 5-aminosalicylic acid. Furthermore, EmB-MO selectively accumulated in the inflamed colon epithelium and restored the levels of the gut barrier proteins such as ZO-1 and Occludin.ConclusionsEmB-MO encapsulation significantly improved water solubility, which translated to greater therapeutic effects on the immune balance and gut barrier function in mice with DSS-induced UC. Our findings provide novel insights into developing emodin-derived drugs for the management of UC.

Unraveling the Relevance of Electron and Hole Transfer in Lead Halide Perovskite Nanocrystals on Current Conduction.

Optimization of perovskite-based optoelectronic performance demands prudent engineering in the device architecture with facile transport of generated charge carriers. Herein, we explore the charge transfer (CT) kinetics in perovskite nanocrystals (PNCs), CsPbBr3, with two redox-active quinones, menadione (MD) and anthraquinone (AQ), and its alteration in halide exchanged CsPbCl3. With a series of spectroscopic and microscopic measurements, we infer that both electron and hole transfer (ET-HT) prevail in CsPbCl3 with quinones, resulting in a faster CT, while ET predominates for CsPbBr3. Furthermore, current-sensing atomic force microscopy measurements demonstrate that the conductance across a metal-PNC-metal nanojunction is improved in the presence of quinones. The contributions of ET and HT to current conduction across PNCs are well supported and validated by theoretical calculations of the density of states. These outcomes convey a new perspective on the relevance of ET and HT in the optimal current conduction and optoelectronic device engineering of perovskites.

Natural Anthraquinones as Promising MAPK3 Inhibitors for Complementary Cancer Therapy

Objective. MAPK3 activates several nuclear transcription factors, including c-Jun and c-fos, by phosphorylating its downstream cytoplasmic protein, thereby contributing to cell proliferation and survival. Different carcinomas’ initiation, progression, cancer cell metastasis, and drug resistance have been associated with MAPK3 overexpression. Given the need for new and potent MAPK3 inhibitors, this study aimed to explore the potential of anthraquinones (AQs) as organic compounds capable of inhibiting MAPK3. Methods. Using AutoDock 4.0 software, the binding affinity of 21 AQs to the receptor’s active site was evaluated. AQs were ranked based on their ΔGbinding values to the receptor’s active site, with the highest rankings receiving the most favorable scores. The Discovery Studio Visualizer tool was used to demonstrate the interaction modes between the highest-ranked AQs and the MAPK3 catalytic site. Furthermore, a 100-nanosecond molecular dynamics (MD) computer simulation was performed to assess the stability of the docked pose of the most potent enzyme inhibitor identified in this study. Results. The binding affinity of emodin-8-glucoside, aloe-emodin 8-glucoside, pulmatin, rhodoptilometrin, and hypericin to the receptor’s ATP binding cleft was noteworthy, as the ΔGbinding values were &lt; − 10 kcal/mol. In addition, emodin-8-glucoside, aloe-emodin 8-glucoside, and pulmatin were found to have inhibition constant values at the picomolar concentration. According to our computer simulation results, the docked pose of emodin-8-glucoside within the active site of MAPK3 achieved a stable state after 70 ns. In other words, the root mean square deviation (RMSD) graph indicated stability within the 70–100 ns timeframe. Conclusion. Inhibition of MAPK3 by emodin-8-glucoside, aloe-emodin 8-glucoside, pulmatin, rhodoptilometrin, and hypericin may have therapeutic potential in cancer treatment.

Auxin-dependent regulation of growth via rolB-induced modulation of the ROS metabolism in the long-term cultivated pRiA4-transformed Rubiacordifolia L. calli

Gene transfer from Agrobacterium to plants is the best studied example of horizontal gene transfer (HGT) between prokaryotes and eukaryotes. The rol genes of A. rhizogenes (Rhizobium rhizogenes) provide uncontrolled root growth, or “hairy root” syndrome, the main diagnostic feature. In the present study, we investigated the stable pRiA4-transformed callus culture of Rubia cordifolia L. While untransformed callus cultures need PGRs (plant growth regulators) as an obligatory supplement, pRiA4 calli is able to achieve long-term PGR-free cultivation. For the first time, we described the pRiA4-transformed callus cultures' PGR-dependent ROS status, growth, and specialized metabolism. As we have shown, expression of the rolA and rolB but not the rolC genes is contradictory in a PGR-dependent manner. Moreover, a PGR-free pRiA4 transformed cell line is characterised as more anthraquinone (AQ) productive than an untransformed cell culture. These findings pertain to actual plant biotechnology: it could be the solution to troubles in choosing the best PGR combination for the cultivation of some rare, medicinal, and woody plants; wild-type Ri-plants and tissue cultures may become freed from legal controls on genetically modified organisms in the future. We propose possible PGR-dependent relationships between rolA and rolB as well as ROS signalling targets. The present study highlighted the high importance of the rolA gene in the regulation of combined rol gene effects and the large knowledge gap in rolA action.

PULPING AND PAPERMAKING PROPERTIES OF ZARA PLANT

The fast-growing Zara plant (a putative hybrid of Pennisetum purpureum Schumach.) is usually planted for cattle fodder. For the first time, Zara plant was evaluated for its pulping potential based on anatomical, chemical, and morphological characteristics. This plant was characterized by an acceptable amount of α-cellulose (40.32%) and lignin (18.4%), with medium fiber length (1.09 mm). Soda–anthraquinone (AQ) pulping of Zara plant was investigated. Anatomically, stems of Zara plant had porous structure, mainly composed of vascular bundles surrounded by parenchyma tissue. Consequently, they were easier to delignify and defibrate, and a pulp yield of 46.54% was obtained, with kappa number 15.45 under the conditions of 14% alkali charge for 120 min of cooking at 150 °C. Good papermaking properties were observed, the tensile index was 78.9 N.m/g at 43 °SR. The resulting pulps showed good bleachability in elemental chlorine-free (ECF) bleaching sequences (D0(EP)D1). Pulp brightness of 81.5%, with the viscosity of 16.0 mPaS, was obtained, with the consumption of 25 kg ClO2/ton of pulp.

Inside the History of Italian Coloring Industries: An Investigation of ACNA Dyes through a Novel Analytical Protocol for Synthetic Dye Extraction and Characterization.

The introduction of synthetic dyes completely changed the industrial production and use of colorants for art materials. From the synthesis of the first synthetic dye, mauveine, in 1856 until today, artists have enjoyed a wider range of colors and selection of chemical properties than was ever available before. However, the introduction of synthetic dyes introduced a wider variety and increased the complexity of the chemical structures of marketed dyes. This work looks towards the analysis of synthetically dyed objects in heritage collections, applying an extraction protocol based on the use of ammonia, which is considered favorable for natural anthraquinone dyes but has never before been applied to acid synthetic dyes. This work also presents an innovative cleanup step based on the use of an ion pair dispersive liquid-liquid microextraction for the purification and preconcentration of historical synthetic dyes before analysis. This approach was adapted from food science analysis and is applied to synthetic dyes in heritage science for the first time in this paper. The results showed adequate recovery of analytes and allowed for the ammonia-based extraction method to be applied successfully to 15 samples of suspected azo dyes from the Azienda Coloranti Nazionali e Affini (ACNA) synthetic dye collection, identified through untargeted HPLC-HRMS analyses.

Emodin‐Based Nanoarchitectonics with Giant Two‐Photon Absorption for Enhanced Photodynamic Therapy

AbstractTwo‐photon‐excited photodynamic therapy (TPE‐PDT) has significant advantages over conventional photodynamic therapy (PDT). However, obtaining easily accessible TPE photosensitizers (PSs) with high efficiency remains a challenge. Herein, we demonstrate that emodin (Emo), a natural anthraquinone (NA) derivative, is a promising TPE PS with a large two‐photon absorption cross‐section (TPAC: 380.9 GM) and high singlet oxygen (1O2) quantum yield (31.9 %). When co‐assembled with human serum albumin (HSA), the formed Emo/HSA nanoparticles (E/H NPs) possess a giant TPAC (4.02×107 GM) and desirable 1O2 generation capability, thus showing outstanding TPE‐PDT properties against cancer cells. In vivo experiments reveal that E/H NPs exhibit improved retention time in tumors and can ablate tumors at an ultra‐low dosage (0.2 mg/kg) under an 800 nm femtosecond pulsed laser irradiation. This work is beneficial for the use of natural extracts NAs for high‐efficiency TPE‐PDT.

Emodin-Based Nanoarchitectonics with Giant Two-Photon Absorption for Enhanced Photodynamic Therapy.

Two-photon-excited photodynamic therapy (TPE-PDT) has significant advantages over conventional photodynamic therapy (PDT). However, obtaining easily accessible TPE photosensitizers (PSs) with high efficiency remains a challenge. Herein, we demonstrate that emodin (Emo), a natural anthraquinone (NA) derivative, is a promising TPE PS with a large two-photon absorption cross-section (TPAC: 380.9 GM) and high singlet oxygen (1 O2 ) quantum yield (31.9 %). When co-assembled with human serum albumin (HSA), the formed Emo/HSA nanoparticles (E/H NPs) possess a giant TPAC (4.02×107 GM) and desirable 1 O2 generation capability, thus showing outstanding TPE-PDT properties against cancer cells. In vivo experiments reveal that E/H NPs exhibit improved retention time in tumors and can ablate tumors at an ultra-low dosage (0.2 mg/kg) under an 800 nm femtosecond pulsed laser irradiation. This work is beneficial for the use of natural extracts NAs for high-efficiency TPE-PDT.

Time-dependent laxative effect of sennoside A, the core functional component of rhubarb, is attributed to gut microbiota and aquaporins.

Sennoside A is a natural anthraquinone component mainly derived from rhubarb and has been routinely used as a clinical stimulant laxative. However, long-term application of sennoside A may lead to drug resistance and even adverse reactions, thus limiting its clinical use. Therefore, to reveal the time-dependent laxative effect and potential mechanism of sennoside A is of critical importance. This study was conducted to investigate the time-dependent laxative effect of sennoside A and unveil its underlying mechanism from the perspective of gut microbiota and aquaporins (AQPs). Based on a mouse constipation model, 2.6mg/kg sennoside A was administered orally for 1, 3, 7, 14 and 21 days, respectively. The laxative effect was assessed by the fecal index and fecal water content, the histopathology of the small intestine and colon was evaluated by hematoxylin-eosin staining. Gut microbiota changes was observed by 16S rDNA sequencing, and colonic AQPs expression was analyzed by quantitative real-time polymerase chain reaction and western blotting. Partial least-squares regression (PLSR) was used to screen out the effective indicators contributing to the laxative effect of sennoside A. The effective indicators were then fitted to time by a drug-time curve model to analyze the trend of efficacy of sennoside A, and the optimal time of administration was derived by comprehensive analysis with a three-dimensional (3D) time-effect image. Sennoside A had a significant laxative effect at 7 days of administration with no pathological changes in the small intestine or colon; however, at 14 or 21 days of administration, the laxative effect diminished and slight damage to the colon was observed. Sennoside A affects the structure and function of gut microbes. The alpha diversity showed that the abundance and diversity of gut microorganisms reached the highest value after 7 days of administration. Partial least squares discriminant analysis showed that the composition of the flora was close to normal when administered for less than 7 days, but was closest to the composition of constipation over 7 days. The expression of aquaporin 3 (AQP3) and aquaporin 7 (AQP7) decreased gradually after the administration of sennoside A, with the lowest expression at 7 days, and then increased gradually afterwards, while the expression of aquaporin 1 (AQP1) was the opposite. The PLSR results showed that AQP1, AQP3, Lactobacillus, Romboutsia, Akkermansia and UCG_005 contributed more to the laxative effect of the fecal index, and after fitting with the drug-time curve model, each index showed a trend of increasing and then decreasing. The comprehensive evaluation of the 3D time-effect image concluded that the laxative effect of sennoside A reached its best after 7 days of administration. Sennoside A should be used in regular dosages for less than one week, as it provides significant relief of constipation and exhibits no colonic damage within 7 days of administration. In addition, Sennoside A exerts its laxative effect by regulating gut microbiota of Lactobacillus Romboutsia, Akkermansia and UCG_005 and water channels of AQP1 and AQP3.