Nano Research
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2018
·Vol. 11
·期 7
·3648-3657
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IF 7.994
Xu Jing,Jie Xu,Xie Fengfeng,Yang Haimei,Wei Weili,Xia Zhining
A new type of self-targeting carbon dot (CD-Fla) for the detection of the toxic heavy metal ion Pb 2+ was synthesized via a one-pot hydrothermal route using flavonoid extracts of Ginkgo biloba leaves as the starting material. As-prepared CD-Fla exhibited excellent biocompatibility and strong blue emission with a quantum yield of 16.1% and significant fluorescence quenching selectivity for Pb 2+ without using any additional targeting molecules. CD-Fla could detect Pb 2+ quantitatively within the range 0.1–20.0 nM, with an ultrahigh sensitivity of 55 pM. The selectivity of CD-Fla for Pb 2+ was nearly one order of magnitude higher than that for other relevant metal ions. This was much better than ever reported CD-based metal ion sensors. The high sensitivity and selectivity were due to the incorporation of certain flavonoid-like moieties into CD-Fla. CD-Fla was also demonstrated to be a good probe for fluorescence tracing of intracellular Pb 2+ . The capability of CD-Fla was further improved when it was doped on agarose hydrogel. CD-Fla-doped agarose hydrogel (CD-AHG) allowed for visual fluorescence detection and removal of Pb 2+ from water. This was confirmed by testing CD-AHG in actual water samples taken from the Jialing River (Chongqing, China). The Pb 2+ adsorbed CD-AHG was regenerable in HCl solution. This study will open a new avenue for synthesizing intelligent materials capable of simultaneously targeting, detecting, and treating heavy metal ions.
研究领域:
分析化学
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环境科学
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材料科学
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SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY
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2022
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IF 4.831
Huiya Tan,Yake Zou,Jiaming Guo,Jiu Chen,Liping Zhou
Cysteine (Cys) is one of the most important biothiols that plays a crucial role in many physiological and pathological processes, and therefore it is of great importance to detect and analyze Cys in subcellular environments, such as in lysosomes. However, only a few fluorescent probes were reported to be capable of detecting Cys in lysosomes selectively. In this wok, we designed and developed a simple, accessible flavone-based fluorescent probe LFA for detecting Cys in lysosomes. Morpholine was employed as the targeting unit for lysosome, and acrylate group was chosen as the Cys-response unit. The probe was easily prepared by a two-step procedure and displayed large Stokes shift, high sensitivity, turn-on response toward Cys over homocysteine (Hcy), glutathione (GSH), and other amino acids. With low cytotoxicity and good cell permeability, the probe could be successfully applied for fluorescence imaging of Cys in living cells. Furthermore, colocalization experiment revealed that lysosomal-targetable ability of LFA was significant. These results indicated that such simple fluorescent probe could provide a promising tool for detection of lysosomal Cys in living biological systems.
研究领域:
生物化学
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细胞生物学
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医学检测
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ANALYTICA CHIMICA ACTA
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2026
·
IF 6.1
Chuansen Qin,Huan Lu,Yichen Jia,Shuisheng Cao,Hongyan Wang,Haixiang Wang
Background Citri Reticulatae Pericarpium (CRP) authentication and flavonoid-related quality evaluation commonly rely on chromatographic or spectroscopic techniques, which are accurate but require specialized instrumentation. This study aims to develop a standardized colorimetric image-based machine-learning workflow for rapid CRP origin-aging classification and flavonoid-equivalent prediction. Results Representative flavonoid monomers were used to compare chromogenic responses in aluminum chloride and sodium nitrite-aluminum nitrate systems. CRP samples were analyzed using standardized image acquisition, color reference normalization, fixed ROI extraction, engineered RGB descriptors, and inverse sRGB gamma correction for regression modeling. For CRP classification, a 480-record model-development set and a 120-record independent held-out validation set were constructed at the image-group level. Through the two chromogenic systems, RF classifier achieved held-out accuracies of 0.9500, 0.9917, and 0.9500 for geographical-origin, aging-year, and combined origin-aging classification, respectively. For flavonoid-equivalent prediction, gamma correction improved the RF external validation R 2 from 0.9502 to 0.9789 and reduced the external RMSE from 5.4186 to 3.5231. Spike-recovery values were 104.27 % ± 8.94 %, 102.07 % ± 6.36 %, and 96.74 % ± 6.45 % at the 200, 400, and 800 μg/mL addition levels, respectively. Significance The proposed workflow integrates chromogenic reaction, standardized image acquisition, color feature extraction, gamma correction, and machine learning into a low-cost analytical strategy for CRP authentication. The results indicate that the method can serve as a useful tool for rapid and efficient quality evaluation for CRP.
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BMC PLANT BIOLOGY
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2026
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IF 5.6
Zhang Yu,Geng Yingxuan,Ma Xiaoli,Huang Zhangjian,Taoerdahong Hailiqian,Chang Junmin
Background Artemisia dracunculus L. (A. dracunculus) is a distinctive plant resource in Xinjiang, possesses both medicinal and culinary value, with distinct regional characteristics. Methods In this study, total flavonoids extracted from A. dracunculus (TFAD) were obtained using a reflux method, with extraction parameters optimized through single-factor experimental design. Ultraviolet-visible spectrophotometry was used for both qualitative and quantitative assessment of TFAD. Samples collected from Jimusaer, Hami, and Tacheng in Xinjiang were analyzed for total flavonoid content and antioxidant activity. Results The optimized extraction conditions included 50% ethanol as the solvent, a solid-to-liquid ratio of 1:30, an extraction temperature of 80 °C, and a duration of 8 h. Under these conditions, the TFAD content in samples from Jimusaer, Hami, and Tacheng was 107.0146 ± 1.4986, 111.9548 ± 1.6136, and 124.8996 ± 1.3801 mg g⁻¹, respectively. Statistically significant regional differences were observed ( p < 0.01), with the highest flavonoid concentration found in samples from Tacheng. Antioxidant activities of TFAD from the three regions were assessed using in vitro free radical scavenging assays, with ascorbic acid (AA) serving as the positive control. TFAD extracted from Jimusaer exhibited the strongest antioxidant capacity, with IC₅₀ values of 31.31 ± 1.19 and 114.04 ± 5.56 µg mL⁻¹ against DPPH and ABTS⁺· radicals, respectively, compared with 7.25 ± 0.56 and 154.18 ± 9.54 µg mL⁻¹ for AA. Conclusion These results suggest that TFAD from the Jimusaer region demonstrates superior antioxidant activity, providing a basis for further exploration and potential utilization of A. dracunculus as a functional resource in Xinjiang.
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JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
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2026
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IF 5.2
Xinyue Liu,Jianghao Yuan,Bokai Kong,Youqin Wang,Jianghong Gong,Xiangjun Shi,Weike Su
Four nilotinib-flavonoid drug-drug cocrystals were successfully prepared. • NIL-BAI cocrystal exhibited the most significant dual solubility enhancement. • NIL-BAI cocrystal improved nilotinib and baicalin bioavailability in rats. • Drug-drug cocrystals overcome the physicochemical limitations of nilotinib. This study employs a supramolecular cocrystallization strategy to simultaneously enhance the pharmaceutical performance of the poorly water-soluble anticancer drug nilotinib and pharmacologically active flavonoids. Four nilotinib cocrystals were successfully prepared via slurry and room-temperature solvent evaporation methods, using kaempferol, quercetin, baicalin, and luteolin as coformers. The four cocrystals exhibited varying degrees of solubility enhancement. Among them, the nilotinib-baicalin cocrystal demonstrated the most significant dual enhancement effect. Specifically, nilotinib solubility increased by 6.19-fold and baicalin by 1.88-fold at pH 6.8, with corresponding enhancements of 2.06-fold and 47.74-fold at pH 1.2. Critically, pharmacokinetic evaluations in rats revealed that the nilotinib-baicalin cocrystal achieved dual bioavailability enhancement: nilotinib exhibited a 9.48-fold higher C max and a 6.78-fold greater AUC 0–24h , while BAI concurrently demonstrated a 2.1-fold and 2.86-fold increase in its C max and AUC 0-24h , respectively. Overall, this work highlights drug-drug cocrystallization as a highly effective approach for developing multifunctional formulations, offering a promising strategy to overcome the physicochemical limitations of nilotinib and improve therapeutic efficacy. Download: Download high-res image (294KB) Download: Download full-size image
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Neural Regeneration Research
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2025
·Vol. 21
·期 7
·3122
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IF 6.7
Liang Yu,Xi Deshuang,Teng Yilin,Liu Pan,Feng Yanbing,Huang Qiumei,Gao Ming,Zong Shaohui
Export Rat nerve growth factor and total flavonoids from hawthorn leaf contribute to the recovery of neurological function after spinal cord injury, including traumatic, non-traumatic spinal cord injuries. However, it remains challenging to efficiently deliver nerve growth factor and total flavonoids from hawthorn leaf to spinal cord injury sites, ensure their sustained release, and minimize further damage. In the present study, we chose a biocompatible and biodegradable gelatin as the substrate, which was crosslinked with the natural biological crosslinker genipin to form a gelatin–genipin hydrogel carrier for the slow release of nerve growth factor and total flavonoids from hawthorn leaf in spinal cord injury sites. The prepared gelatin–genipin hydrogel had good injectable properties and photothermal effects. Furthermore, when the hydrogel with 2% genipin, 200 ng/mL nerve growth factor, and 320 μg/mL total flavonoids from hawthorn leaf was combined with near infrared irradiation, there was a slow release of total flavonoids from hawthorn leaf and nerve growth factor, reduced oxidative stress, an improved inflammatory microenvironment, and accelerated angiogenesis and axonal regeneration via inhibition of the nuclear factor kappa-B signaling pathway, thereby promoting recovery from spinal cord injury. Collectively, our results indicate that this new hydrogel may improve the prognosis of spinal cord injury, and may represent a new strategy for treating spinal cord injury.
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MOLECULAR PHARMACEUTICS
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2025
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IF 4.5
Jiawei Han,Wen Sun,Jiaxin Chen,Zhimin Yue,Weitao Fang,Xiaoqian Liu,Jue Wang,Gaorong Wu
Flavonoids represent an extensive group of phenolic substances in vegetables, fruits, grains, tea, flowers, etc., which show a variety of biological activities in various nutraceutical, cosmetic, and medicinal fields. Despite demonstrating multifunctional bioactive properties relevant to nutraceutical and pharmaceutical applications, their clinical utilization faces challenges due to their generally low water solubility. This study established a systematic methodology combining computational modeling and experimental validation for developing flavonoid-meglumine (MEG) coamorphous formulations. The initial screening identified 13 flavonoid compounds exhibiting favorable miscibility with MEG from 15 candidates through Hansen solubility parameter analysis. Subsequent molecular dynamics simulations revealed potential hydrogen bond formation in six selected flavonoids (BAI, HES, NAR, KAE, QUE, and ISO) with MEG. Then, six flavonoid coamorphous systems were successfully prepared via the melt-quenching method and characterized by PLM, PXRD, and differential scanning calorimetry. FTIR and radial distribution function analysis results collectively confirmed intermolecular hydrogen bond interactions within these binary systems. In vitro dissolution studies revealed significant solubility/dissolution enhancement in both pH 1.2 HCl and pH 6.8 phosphate buffers, maintaining long-term supersaturation for all six coamorphous formulations. Meanwhile, six flavonoid coamorphous systems had superior stability over individual flavonoid amorphous components, which were attributed to the stronger intermolecular interactions by higher binding energy calculation. These results indicated that the obtained flavonoid coamorphous systems performed a promising application potential in functional products. Importantly, this study presents a novel design framework integrating computational prediction, molecular modeling, and experimental validation for systematic screening of flavonoid coamorphous formulations.
研究领域:
药剂学
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计算化学
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生物医学
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PubMed
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PLANT PHYSIOLOGY AND BIOCHEMISTRY
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2023
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IF 6.5
Ruiyi Fan,Congyi Zhu,Diyang Qiu,Genlin Mao,Bernd Mueller-Roeber,Jiwu Zeng
As a well-recognized traditional Chinese medicine (TCM), immature fruits of Citrus grandis ‘Tomentosa’ (CGT) serve to cure chronic cough in humans. Specialized metabolites including flavonoids may have contribute to this curing effect. Knowledge about the molecular mechanisms underlying flavonoid biosynthesis in ‘Tomentosa’ fruits will, therefore, support the breeding of varieties with improved medicinal properties . Hence, we profiled the transcriptomes and metabolites of the fruits of two contrasting C. grandis varieties, namely ‘Zheng-Mao’ (‘ZM’) used in TCM production, and a locally cultivated pomelo, namely ‘Guang-Qing’ (‘GQ’), at four developmental stages. A total of 39 flavonoids, including 14 flavanone/flavone, 5 isoflavonoids , 12 flavonols, and 6 anthocyanins , were identified, and 16 of which were quantitatively determined in the fruits of the two varieties. We found that ‘ZM’ fruits contain more flavonoids than ‘GQ’. Specifically, rhoifolin levels were significantly higher in ‘ZM’ than in ‘GQ’. We annotated 31,510 genes, including 1,387 previously unknown ones, via transcriptome sequencing of ‘ZM’ and ‘GQ.’ A total of 646 genes were found to be differentially expressed between ‘ZM’ and ‘GQ’ throughout at all four fruit developmental stages, indicating that they are robust expression markers for future breeding programs. Weighted gene co-expression network analysis identified 18 modules. Combined transcriptional and metabolic analysis revealed 25 genes related to flavonoid biosynthesis and 16 transcriptional regulators (MYBs, bHLHs, WD40) that may be involved in the flavonoids biosynthesis in C. grandis ‘Tomentosa’ fruits.
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MOLECULES
·
2019
·Vol. 24
·期 9
·1661
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IF 3.06
Mengmeng Xia,Yajing Fang,Weiwei Cao,Fuqiang Liang,Siyi Pan,Xiaoyun Xu
P-glycoprotein (P-gp) serves as a therapeutic target for the development of inhibitors to overcome multidrug resistance (MDR) in cancer cells. In order to enhance the uptake of chemotherapy drugs, larger amounts of P-gp inhibitors are required. Besides several chemically synthesized P-gp inhibitors, flavonoids as P-gp inhibitors are being investigated, with their advantages including abundance in our daily diet and a low toxicity. The cytotoxicity of daunorubicin (as a substrate of P-gp) to KB/MDR1 cells and the parental KB cells was measured in the presence or absence of flavonoids. A two-dimensional quantitative structure–activity relationship (2D-QSAR) model was built with a high cross-validation coefficient (Q2) value of 0.829. Descriptors including vsurf_DW23, E_sol, Dipole and vsurf_G were determined to be related to the inhibitory activity of flavonoids. The lack of 2,3-double bond, 3′-OH, 4′-OH and the increased number of methoxylated substitutions were shown to be beneficial for the inhibition of P-gp. These results are important for the screening of flavonoids for inhibitory activity on P-gp.Keywords:flavonoids;P-gp;inhibitory activity;QSAR
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MEDICAL SCIENCE MONITOR
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2018
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IF 1.894
Hong Jiang,Chen Zhang,Wen He
Background Dracocephalum heterophyllum Benth flavonoid (DHBF) is a Tibetan and Uighur traditional medicine used to treat various disorders such as hypertension, lung heat, cough, and bronchitis; it has good antioxidant activity. Previous studies have shown that DHBF can reduce blood pressure in renovascular hypertensive rats, improve left ventricular systolic and diastolic function, and improve myocardial contractility. Therefore, we aimed to study the effect of DHBF on cardiomyocyte hypertrophy in cultured cells. Material/Methods Neonatal rat cardiomyocytes were cultured, and hypertrophy was induced by angiotensin II (Ang II), with or without varying concentrations of the DHBF extract. Cell Counting Kit-8 assay was used to assess cell viability, RT-qPCR was used to determine mRNA levels, confocal laser scanning microscopy was used to measure cell surface area and intracellular Ca 2+ concentrations ([Ca 2+ ] i ), and colorimetric assays were used to assess nitric oxide (NO) levels and nitric oxide synthase (NOS) activity. Results Ang II treatment of cardiomyocytes reduced cell viability to ~75% that of controls. Ang II treatment also increased cell surface area; increased mRNA expression of c-jun, atrial natriuretic peptide (ANP), brain natriuretic peptide (BNP), and β-myosin heavy chain (β-MHC); increased [Ca 2+ ] i ; and reduced NOS activity and NO production. DHBF treatment could reverse these effects in a concentration-dependent manner. Conclusions These results showed that DHBF can ameliorate cardiomyocyte hypertrophy induced by Ang II, as indicated by the downregulation of cardiac hypertrophy genes ( ANP , BNP , and β -MHC ) and reduction in cell surface area. The mechanism may be related to NO release and [Ca 2+ ] I regulation.
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JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
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2013
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IF 1.495
Weiqiang Lu,Junsheng Zhu,Shien Zou,Xi Li,Jin Huang
Human skin fibroblast collagenase also known as Matrix Metalloproteinase-1 (MMP-1) is a key enzyme in remodeling and degradation of extracellular matrix, and the inhibitors of human MMP-1 are effective drug candidates for the treatment of cancer. In this study, we report an improved method for high-level expression of soluble human MMP-1 catalytic domain (cd-MMP-1) in E.coli. The enzymatic activity is found maximum at pH 7.5 and temperature 40°C with a Km value of 13.02 µM. Effects of 17 structure-related flavonoids on MMP-1 activity are evaluated using a fluorescent assay, 6 inhibitors are identified with IC50 < 10 µM. Fisetin is the most active agent with an IC50 value of 1.35 µM and is identified as a mixed type inhibitor. Our improved soluble cd-MMP-1 expression method provides a basis for inhibitors identification and may be beneficial to discover novel anti-cancer agent targeting human MMP-1.
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JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
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2016
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IF 3.169
Bo Zhuang,Li-Li Dou,Ping Li,E-Hu Liu
Deep eutectic solvents (DESs) are emerging as alternatives to conventional ionic liquids and organic solvents due to their unique advantages. In the present study, the tuneability of DESs as tailor-made solvents to efficiently extract polar and non-polar bioactive compounds from Platycladi Cacumen was detailedly investigated. Totally 12 types of choline chloride-, betaine-, and l-proline-based DESs were synthesized for initial screening, and extraction conditions was optimized by single-factor experiment. Experiments with different DESs and principal components analysis demonstrated that the extractability of both flavonoid glycosides and aglycones was greater with certain designed DESs than conventional solvents. In addition, the water content in DESs led to significantly different extraction yields of flavonoid compounds. The target compounds were recovered from DESs by macroporous resin LX-38 with a satisfactory yield between 77.44% and 98.92%. The knowledge acquired in this study could contribute to further DES application in extraction of bioactive compounds from natural sources.
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