JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
·
2020
·
IF 3.209
Xin Qiao,Cheng Qu,Qiming Luo,Yuanzhong Wang,Jie Yang,Hua Yang,Xiaodong Wen
Rhizoma Paridis (RP) with significant anti-tumor and haemostatic effects, has been used as the raw material of many Traditional Chinese preparations. However, its active ingredients are still unclear. The present study aimed to discover bioactive ingredients from RP based on spectrum-relationship and chemometric methods. Firstly, the saponins extract was prepared by phytochemical methods. Furthermore, UHPLC-QTOF-MS and UHPLC-qMS were incorporated to establish an efficient and sensitive method for obtaining the chemical profiles of RP. A total of 34 saponins were characterized in RP and 13 of them were assigned as common peaks in 25 batches of samples. After evaluation of the anti-tumor and haemostatic activities of samples, spectrum-effect relationships were investigated by the grey relational analysis (GRA), orthogonal projections to latent structures (OPLS) and back propagation artificial neural network (BP-ANN). These analyses showed that polyphyllin VII (P27), polyphyllin II (P30), dioscin (P31) and polyphyllin I (P33) play a role in the haemostatic effects of RP whereas polyphyllin VII (P27), dioscin (P31), polyphyllin I (P33), progenin III (P34) were assigned as candidate ingredients accounting for the anti-tumor activity of RP. The anti-tumor and haemostatic activities of these screened ingredients were subsequently verified in vitro . Collectively, the present study established the spectrum-effect relationship mode of RP and discovered the bioactive compounds of RP, which could be also used for exploration of bioactive compounds in herbal medicines, especially for trace compounds.
研究领域:
药理学
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分析化学
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中药学
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产品关联
DOI
PubMed
高影响因子
MICROCHEMICAL JOURNAL
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2022
·
IF 5.304
Anqi Huang,Xiaofang Yang,Ting Xia,Daichun He,Rui Zhang,Zongtao Li,Shengchun Yang,Yong Liu,Xiaodong Wen
The excessive residue of copper ion (Cu 2+ ) has an important impact on the quality of traditional Chinese medicine (TCM). In this work, a sulfur quantum dots (SQDs) fluorescent probe was developed for rapid and sensitive detection of Cu 2+ in Paris polyphylla. Smith var. yunnanensis (Franch.) Hand. -Mazz. ( P. polyphylla var. yunnanensis ). SQDs were synthesized by the “assemble-fission” method. The synthesized SQDs were characterized by Fourier transform infrared spectroscopy (FTIR), X-ray photoelectron spectroscopy (XPS) and transmission electron microscopy (TEM), and their fluorescence properties were studied. The prepared SQDs have advantages of ultra-small size, good optical properties and excellent stability. The addition of Cu 2+ could effectively quench the fluorescence of SQDs due to the inner filter effect (IFE) between Cu 2+ and SQDs. The detection linear range of this method was 20–200 μM. The limit of detection (LOD) was 6.78 μM. It has high selectivity in the simultaneous presence of other ions, and the possible fluorescence quenching mechanism was discussed in detail. Finally, the prepared SQDs were applied to the detection of actual samples of P. polyphylla var. yunnanensis with satisfactory results, which confirmed the great potential of SQDs in the actual measurement of Cu 2+ in TCM.
研究领域:
中药学
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分析化学
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生物医学
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DOI
高影响因子
MICROCHEMICAL JOURNAL
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2025
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IF 5.1
Yujiao Tu,Jiaxuan Liu,Xintao Cui,Lei Jinag,Lin Yuan,Wensi Ma,Xiuling Ji
Carbendazim is primarily employed to manage crop diseases. However, excessive pesticide usage poses risks to human health. Therefore, developing a highly sensitive detection method for carbendazim is essential. Nitrogen-doped carbon dots Rhp-N CDs were synthesized through a straightforward one-step hydrothermal process, using Rhizoma paridis extracts and o -phenylenediamine as precursors. Rhp-N CDs were purified using dialysis, thin-layer chromatography, and column chromatography. Transmission electron microscopy revealed that the Rhp-N CDs displayed a spherical morphology with an average particle size of 2.19 nm. X-ray photoelectron spectroscopy analysis indicated that they were composed of carbon (C), nitrogen (N), and oxygen (O) elements. Fourier transform infrared spectroscopy showed that Rhp-N CDs contained amino groups on their surface. The linear ranges of carbendazim detection were 0–50 μg/L and 50–150 μg/L, with low detection limits of 6.81 ng/L and 20.9 ng/L, respectively. Furthermore, the fluorescence quenching mechanism of the target on Rhp-N CDs was elucidated. The nano-fluorescent probe was demonstrated to be effective in determining the content of carbendazim in samples of Snow pears, Winter jujubes, Snow peaches, and Bananas, thereby illustrating the possibility of its practical application.
研究领域:
分析化学
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环境科学
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纳米技术
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农业科学
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产品关联
DOI
高影响因子
BRITISH JOURNAL OF PHARMACOLOGY
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2023
·
IF 7.3
Rui-Fang Dong,Cheng-Jiao Qin,Yong Yin,Liang-Liang Han,Cheng-Mei Xiao,Kai-Di Wang,Rong-Yuan Wei,Yuan-Zheng Xia,Ling-Yi Kong
Background and Purpose Chaperone-mediated autophagy (CMA) is a selective type of autophagy targeting protein degradation and maintains high activity in many malignancies. Inhibition of the combination of HSC70 and LAMP2A can potently block CMA. At present, knockdown of LAMP2A remains the most specific method for inhibiting CMA and chemical inhibitors against CMA have not yet been discovered. Experimental Approach Levels of CMA in non-small cell lung cancer (NSCLC) tissue samples were confirmed by tyramide signal amplification dual immunofluorescence assay. High-content screening was performed based on CMA activity, to identify potential inhibitors of CMA. Inhibitor targets were determined by drug affinity responsive target stability-mass spectrum and confirmed by protein mass spectrometry. CMA was inhibited and activated to elucidate the molecular mechanism of the CMA inhibitor. Key Results Suppression of interactions between HSC70 and LAMP2A blocked CMA in NSCLC, restraining tumour growth. Polyphyllin D (PPD) was identified as a targeted CMA small-molecule inhibitor through disrupting HSC70–LAMP2A interactions. The binding sites for PPD were E129 and T278 at the nucleotide-binding domain of HSC70 and C-terminal of LAMP2A, respectively. PPD accelerated unfolded protein generation to induce reactive oxygen species (ROS) accumulation by inhibiting HSC70–LAMP2A–eIF2α signalling axis. Also, PPD prevented regulatory compensation of macroautophagy induced by CMA inhibition via blocking the STX17–SNAP29–VAMP8 signalling axis. Conclusions and Implications PPD is a targeted CMA inhibitor that blocked both HSC70–LAMP2A interactions and LAMP2A homo-multimerization. CMA suppression without increasing the regulatory compensation from macroautophagy is a good strategy for NSCLC therapy. Graphical
研究领域:
肿瘤学
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分子生物学
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药理学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF ETHNOPHARMACOLOGY
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2025
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IF 5.4
Jue Liu,Yue-Xuan Liu,Yu-Song Song,Chen-Kai Liu,Fei-Xue Yu,Gao Liu,Tian-Rui Xu,Jun Sang
Ethnopharmacological relevance Paris polyphylla Smith var. yunnanensis (Franch.) Hand.-Mazz., known as “Chonglou” in traditional Chinese medicine, is clinically used in cancer therapy, with saponins identified as the key antitumor constituents. However, the therapeutic potential and mechanisms of the total saponins from P. polyphylla var. yunnanensis (PPT) against bladder cancer, particularly their ability to overcome chemoresistance, remain unexplored. Aim of the study This study aimed to investigate PPT's anti-bladder cancer effects and mechanisms, with a focus on its potential to overcome cisplatin resistance. Materials and methods We established a UPLC-DAD method for saponin profiling and developed an eco-friendly extraction protocol using hydroxypropyl- β -cyclodextrin-assisted extraction combined with macroporous resin purification to prepare PPT. Anti-cancer efficacy was assessed in bladder cancer cell lines, mouse/zebrafish xenograft models, and cisplatin-resistant models. Mechanistic investigations integrated network pharmacology, metabolomics, molecular docking, and experimental validations (siRNA silencing, western blotting, flow cytometry, molecular dynamics simulations, cellular thermal shift assay, and surface plasmon resonance). Results The hydroxypropyl- β -cyclodextrin-based extraction system enhanced PPT purity by 15-fold, with the purified fraction showing dose-dependent anti-bladder cancer activity in vitro and in vivo . Mechanistically, PPT exerted anti-proliferative, pro-apoptotic, anti-lipogenic, and chemosensitizing effects by inhibiting the growth factor receptor binding protein 2 (GRB2)-mediated Akt-SREBP1 signaling axis. Notably, polyphyllin VII, a key constituent of PPT, was identified as a novel GRB2 inhibitor, potently suppressing bladder cancer progression and overcoming cisplatin resistance. Conclusion This study demonstrates that targeting the GRB2-Akt-SREBP1 signaling axis is a promising strategy for bladder cancer therapy, further establishing PPT as a multicomponent phytomedicine and PPVII as a novel GRB2 inhibitor with high translational potential.
研究领域:
癌症研究
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药理学
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分子生物学
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民族药理学
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生物信息学
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信号转导
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DOI
PubMed
高影响因子
BMC Complementary and Alternative Medicine
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2016
·Vol. 16
·期 1
·1-10
·
IF 1.987
Liu Jingjing,Li Xican,Lin Jian,Li Yunrong,Wang Tingting,Jiang Qian,Chen Dongfeng
Background Sarcandra glabra (Caoshanhu) is a traditional Chinese herbal medicine used for treating various oxidative-stressed diseases. The present work evaluated its protective effect on mesenchymal stem cells (MSCs) from oxidative stress and then discussed possible mechanisms underlying this observation. Methods Ethanolic extract of S. glabra (ESG) was investigated by chemical methods for its content of total phenolics, rosmarinic acid, and astilbin. ESG, along with rosmarinic acid and astilbin, was investigated for the effect on the viability of Fenton-treated MSCs using 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyl (MTT) assay. The observed cell protective effect was further explored by mechanistic chemistry using various antioxidant assays, including DNA protection, •OH-scavenging, •O 2 − -scavenging, FRAP (ferric ion reducing antioxidant power), ABTS + •-scavenging, DPPH•-scavenging, and Fe 2+ -chelating assays. Results Analysis of ESG revealed a content of 46.31 ± 0.56 mg quercetin/g total phenolics, 0.78 ± 0.01 % rosmarinic acid, and 3.37 ± 0.01 % astilbin. Results from the MTT assay revealed that three compounds (rosmarinic acid>astilbin>ESG) could effectively increase the survival of Fenton-treated MSCs. Similarly, in •O 2 − -scavenging, DPPH•-scavenging, and Fe 2+ -chelating assays, rosmarinic acid exhibited more activity than astilbin; while in FRAP, ABTS + •-scavenging assays, astilbin was stronger than rosmarinic acid. Conclusion S. glabra can prevent MSCs from •OH-induced oxidative stress. Such protective effect can be attributed to its antioxidant ability and the presence of two kinds of phytophenols, i.e. caffeoyl derivatives and flavonoids. As the respective representatives of caffeoyl derivatives and flavonoids, rosmarinic acid and astilbin may exert the antioxidant action via direct ROS-scavenging and indirect ROS-scavenging (i.e. Fe 2+ -chelating). The direct ROS-scavenging ability involves hydrogen atom transfer (HAT) and/or electron transfer (ET) pathway. Astilbin engages the latter pathway more, which can be attributed to the larger planar conjugation in A/C fused rings. Rosmarinic acid, on the other hand, shows more HAT and Fe 2+ -chelating potential, which may be due to rosmarinic acid bearing one more catechol moiety whereas astilbin has steric-hindrance from 3-α-L-rhamnose and an H-bonding between 4,5 sites. The antioxidant features of rosmarinic acid can be generalized to other caffeoyl derivatives, while that of astilbin cannot be generalized to other flavonoids because of the difference in chemical structures.
研究领域:
药理学
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细胞生物学
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药物化学
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中医药
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF ETHNOPHARMACOLOGY
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2024
·
IF 4.8
Mengqin Yi,Zhenglang Zhang,Zhenhui Luo,Anqi Luo,Hekun Zeng,Peiyang Li,Tingting Wang,Jingwen Yang,Hong Nie
Ethnopharmacological relevance PolyphyllinVI (PPⅥ) is the main bioactive component of Chonglou which is a traditional Chinese herbal with various effects, including antitumor, anti-inflammatory, and analgesia. Aim of the study This study aimed to investigate the properties and mechanisms of the analgesia of PPⅥ by using neuropathic pain (NPP) mice. Materials and methods The potential targets and mechanisms of PPⅥ in alleviating NPP were excavated based on the network pharmacology. Subsequently, the construction of a spared nerve injury (SNI) mice model was used to evaluate the effect of PPⅥ on NPP and the expression of the P2X3 receptor. We identified the signaling pathways of PPⅥ analgesia by RNA sequencing. Results The results of network pharmacology showed that BCL2, CASP3, JUN, STAT3, and TNF were the key targets of the analgesic effect of PPⅥ. PPⅥ increased the MWT and TWL of SNI mice and decreased the level of P2X3 receptors in the dorsal root ganglion (DRG) and spinal cord (SC). Additionally, PPⅥ reduced the release of pro-inflammatory mediators (TNF-α, IL-1β, and IL-6) in the DRG, SC, and serum. Based on the KEGG enrichment of differentially expressed genes (DEGs) identified by RNA-Seq, PPVI may relieve NPP by regulating the AMPK/NF-κB signaling pathway. Western blotting results showed that the AMPK signaling pathway was activated, followed by inhibition of the NF-κB signaling pathway. Conclusion PPⅥ increased the MWT and TWL of SNI mice maybe by inhibiting the expression of the P2X3 receptor and the release of inflammatory mediators. The properties of the analgesia of PPⅥ may be based on the AMPK/NF-κB pathway.
研究领域:
药理学
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神经科学
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民族药理学
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分子生物学
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DOI
PubMed
高影响因子
SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY
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2025
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IF 4.6
Zongtao Li,Shaodui Ye,Leshou Zhang,Zhenjuan Duan,Shengchun Yang,Yong Liu,Xiaodong Wen
Heavy metal residues in Chinese herbal medicines (CHMs) have raised significant concerns due to their inherent toxicological implications for human health. Therefore, there is an imperative requirement to establish an effective and sensitive method for detecting heavy metal ions. In this study, sulfur quantum dots (SQDs) were fabricated through a sonication-assisted H 2 O 2 etching approach, and the spectral characteristics of SQDs in deep eutectic solvent (DES) micelles were studied. This study found that SQDs significantly aggregate in the long alkyl chains of surfactant-like DES, thereby enhancing the luminescent intensity of SQDs. A fluorescent probe that acts as a “turn-off” was developed using DES-sensitized SQDs to determine Pb 2+ . The detection mechanism of this probe for Pb b+ was further analyzed. Under optimized experimental conditions, the linear range of Pb 2+ concentrations was determined to be 20–100 μM, with a detection limit of 1.61 μM. Validation studies of the method demonstrated that the sensitivity of the established sensor was 1.7-fold greater than that of the bare SQDs probe. Furthermore, the established method was verified using Pb 2+ in Paris polyphylla as the research subject, yielding a satisfactory recovery rate. In short, the DES-sensitized SQDs fluorescent platform is a sensitive, simple, and effective method for detecting Pb 2+ in complex samples.
研究领域:
分析化学
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环境科学
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纳米技术
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药物分析
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生物传感
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产品关联
DOI
PubMed
高影响因子
DALTON TRANSACTIONS
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2022
·Vol. 51
·期 14
·5624-5634
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IF 4.569
Jia Wang,Xiange Huang,Hegen Li,Deyue Yan,Wei Huang
Here two Zn(II) coordination polymers [Zn20(DMCA)12]O12 (DMCA = demethylcantharic acid, DMCA-Zn1) and [Zn(DMCA)](H2O)2 (DMCA-Zn2) are synthesized from a broad-spectrum anticancer drug norcantharidin (NCTD) and Zn(NO3)2·6H2O under solvothermal conditions. By mechanical grinding with a biocompatible polymeric surfactant F127, ultrasonic treatment and filtration, DMCA-Zn1 and DMCA-Zn2 can be transformed into stable nanoparticles (DMCA-Zn1 NPs and DMCA-Zn2 NPs) suspended in water with average diameters of around 190 nm and 162 nm for drug delivery. The in vitro evaluation indicates that DMCA-Zn1 NPs and DMCA-Zn2 NPs can enter into HepG2 and Hep3B cancer cells via endocytosis and inhibit their proliferation. Meanwhile they exhibit relatively low toxicity to L927 normal cells. The in vivo evaluation confirms that DMCA-Zn1 NPs and DMCA-Zn2 NPs can more effectively inhibit the growth of Hep3B tumors with relatively few side effects compared with free NCTD. This approach can be extended to other anticancer drugs to construct nanodrug delivery systems for cancer treatment.
研究领域:
化学
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材料科学
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药理学
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肿瘤学
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产品关联
DOI
PubMed
高影响因子
Molecular Medicine Reports
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2024
·Vol. 30
·期 6
·1-11
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IF 3.4
Weiwei Miao,Zhixiong Wang,Jianwen Gao,Yuko Ohno
Paridis Rhizoma saponins (PRS) are significant components of Rhizoma Paridis and have inhibitory effects on various tumors, such as bladder, breast, liver and colon cancer. Polyphyllin II (PPII), one of the PRS, has an unclear effect on breast cancer. The present study aimed to explore the effect and mechanism of PPII in breast cancer. A network pharmacology approach was employed to predict the core components and breast cancer‑related targets of PRS. Moreover, a xenograft tumor model was established to determine the anti‑breast cancer effect of PPII in vivo. The viability of MDA‑MB‑231 cells was determined by a Cell Counting Kit‑8 assay. Apoptosis was analyzed using annexin V/PI double staining. Additionally, Transwell and scratch assays were performed to evaluate invasion and migration. The potential mechanism was predicted by Kyoto Encyclopedia of Genes and Genomes enrichment analysis and molecular docking analysis and verified by western blot analysis. The effect of PPII on aerobic glycolysis in breast cancer cells was detected by lactic acid and pyruvate kits and Western blotting of glycolytic rate‑limiting enzymes. Network pharmacology analysis revealed 26 core targets involved in breast cancer and that PPII was the core active component of PRS. The in vivo studies showed that PPII could inhibit the growth of breast cancer in mice. In vitro experiments confirmed that PPII induced cancer cell apoptosis and inhibited invasion and migration. Furthermore, PPII was capable of suppressing the expression of key proteins in the PI3K/Akt signaling pathway, reducing the generation of aerobic glycolytic products, and diminishing the protein expression levels of hexokinase 2 and pyruvate kinase M2. The results indicated that PPII inhibited aerobic glycolysis in breast cancer cells through the PI3K/Akt signaling pathway, thereby inhibiting breast cancer growth.
研究领域:
肿瘤学
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药理学
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分子生物学
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细胞生物学
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产品关联
DOI
PubMed
高影响因子
FOOD AND CHEMICAL TOXICOLOGY
·
2025
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IF 3.5
Qile Xia,Beiqiong Hao,Chenxing Liu,Yan Cao
Polygonatum cyrtonema Hua (PcH) is a traditional medicinal and edible homologous plant. Here, the anticancer activity of different purified PcH saponins (PcHs) on the ovarian cancer (OC) cell A2780 were investigated. The PcHs were purified by AB-8. Their effects on the apoptosis, migration and invasion of A2780 were explored by CCK8, wound healing assay, Hoechst 33258 staining, Annexin V-FITC/PI and intracellular reactive oxygen species (ROS) measurement. Moreover, western blot and realtime-PCR confirmation were performed for the associated protein and mRNA targets. The results showed that the content of PcHs increased from 0.31 ± 0.02 mg/mL to 0.79 ± 0.02 mg/mL after purification. The inhibition rate of purified PcHs on A2780 could reach 66.76 ± 0.56%. Specifically, it promoted cell apoptosis, disturbed the cell cycle, increased the ROS levels, regulated the expression levels of pro-apoptotic and anti-apoptotic proteins. PcHs can also regulate the expression level of proteins related to the invasion and migration characteristics of A2780, the mRNA expression level related to the P13K-Akt signal transduction process, and the extracellular matrix-receptor interaction pathway, as well as drug resistance. Overall, this study provides a new idea for the treatment of OC.
研究领域:
肿瘤学
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药理学
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细胞生物学
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传统中药
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF ETHNOPHARMACOLOGY
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2025
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IF 5.4
Fang-Ning Qiu,Qiao-Lei Wang,Ping Li,Qiu-Yi Pu,Hui-Jun Li
Ethnopharmacological relevance Paridis Rhizoma, derived from two pharmacopoeial Paris species viz. Paris polyphylla Smith var. yunnanensis (Franch.) Hand. - Mazz. (PPY) and P. polyphylla Smith var. chinensis (Franch.) Hara (PPC), has the traditional efficacy of heat-clearing and detoxifying, and is recognized for its anti-inflammatory and hemostatic effects. Despite significant chemical differences, these two species are clinically prescribed without discrepancy, potentially limiting optimal therapeutic outcomes. Aim of the study The aim was to compare the anti-inflammatory and hemostatic bioactive ingredients of two pharmacopoeial Paris species, providing a foundation for more precise medicinal application. Materials and methods Chemical profiling of PPY and PPC was conducted using UHPLC-QTOF-MS. Anti-inflammatory and hemostatic activities were assessed in zebrafish models. Active compounds were identified through partial least squares-regression (orthogonal partial least squares-regression) and Spearman correlation analyses, and their structure-activity relationships were subsequently elucidated. Network pharmacology, RT-qPCR and Western blot were employed to explore potential targets and pathways. HPLC-UV quantitative method was established to compare active component contents between two species. Results Spectrum-effect analysis identified 5 anti-inflammatory and 3 hemostatic steroidal saponins from two species. Structural features such as the C17-OH group, C3 oligosaccharide chain and F-ring were critical to bioactivity. Paris saponin II and polyphyllin I, enriched in PPY, demonstrate stronger anti-inflammatory effects via the NF-κB signaling pathway. Chonglouoside H and polyphyllin VI, abundant in PPC, exhibited better hemostatic activity, potentially related to tnfa downregulation. Conclusions This study elucidated distinct bioactivity bias of PPY and PPC due to their difference in chemical compositions, suggesting the necessity of precise medication.
研究领域:
民族药理学
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植物化学
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药理学
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药物化学
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系统生物学
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产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）