COLLOIDS AND SURFACES B-BIOINTERFACES
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2019
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IF 3.973
Najaf Ali Soomro,Qiao Wu,Safdar Ali Amur,Hao Liang,Aziz Ur Rahman,Qeping Yuan,Yun Wei
In this study, we have encapsulated natural physcion (PHY) drug loading into metal-organic frameworks MOFs , zeolitic imidazolate frameworks (ZIFs) through straight-forward nano-precipitation technique. The synthesized PHY@ZIF-8 indicated high drug loading encapsulation efficiency i.e. 88%, whereas, drug loading capacity was found to be 11.49%. The characterization of PHY loaded-ZIF 8 (PHY@ZIF-8) was carried out by powder x-ray diffraction (PXRD), transmission electron microscopy (TEM), scanning electron microscopy (SEM), thermal gravimetric analysis (TGA), and FT-IR methods. The release of PHY loaded in ZIF-8 was 88.72% at pH 5.0 which is approximately three time higher than its release in physiological system with pH 7.4 (27.61%). The remarkable stability of PHY@ZIF-8 NPs even after 25 days stem it as an effective and stable candidate. Furthermore, the antibacterial activity of pure PHY, ZIF-8 and PHY@ZIF-8 were investigated against gram negative strains and gram positive strain. The PHY@ZIF-8 showed maximum growth inhibition zones against all microorganism as compare to pure PHY. We hope that this model drug could have the potential ability for treatment of various infectious diseases.
研究领域:
材料科学
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药理学
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微生物学
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产品关联
DOI
PubMed
高影响因子
SCIENCE OF THE TOTAL ENVIRONMENT
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2018
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IF 4.61
Bingjie Zhang,Jiawen Ji,Xue Liu,Changsheng Li,Meng Yuan,Jingyang Yu,Yongqiang Ma
In this study, nano zirconium carbide (n-ZrC) was synthesized by preceramic polymers method, and it was used to adsorb emodin and physcion from solutions for the first time. The prepared material was characterized by various technologies . The adsorption experiment was carried out to investigate the emodin and physcion removal performance. The results indicate that the pseudo-second-order kinetic model and the Langmuir model correlated satisfactorily to the experimental data, and the thermodynamic parameters are also calculated. Especially, n-ZrC can remove >95% of emodin or physcion in a minute under the optimal conditions, it is the fastest adsorption rate compared to other commonly used adsorbents (commercial zirconium carbide, activated carbon, C18, PSA, GCB and florisil). The adsorption mechanism was discussed, which suggests that Van der Waals' forces are the primary driving power during the adsorption process. Moreover, n-ZrC is stable at different pH and it can be reused at least fifteen times.
研究领域:
环境科学
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材料科学
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药物化学
✓ 已验证
DOI
高影响因子
PESTICIDE BIOCHEMISTRY AND PHYSIOLOGY
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2025
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IF 4
Duo Lai,Delin Wang,Jian Qin,Qingli Zhuang,Xuehua Shao,Weiqiang Xiao
Emblica blue mold, a fungal disease caused by Penicillium choerospondiatis , poses a major threat to the industry of Phyllanthus emblica . Currently, resistance to chemical fungicides has been a challenge to its effectiveness on this disease. To explore an effective botanical fungicide as alternatives for chemical fungicides to inhibit P. choerospondiatis , 10 botanical fungicides were selected for antifungal activity test against P. choerospondiatis mycelial growth. Results showed that physcion was the most effective one with a 50 % effective concentration (EC 50 ) of 3.30 mg/L. Furthermore, physcion had a strong inhibition activity to spore germination and pathogenicity of P. choerospondiatis , both in vitro and in vivo . Its antifungal mechanisms investigations indicated that physcion could alter the mycelium morphology, disrupt cell membrane integrity, increase cell membrane permeability, reduce ergosterol content, and induce excessive reactive oxygen species (ROS). Moreover, transcriptome analysis revealed that physcion might interfere with ergosterol biosynthesis and oxidoreductase activity, leading to significant cell membrane dysfunction and oxidative stress in P. choerospondiatis . This study lays the groundwork for elucidating how physcion harms the pathogen and provides promising insights into eco-friendly alternatives for controlling this postharvest disease in P. choerospondiatis .
研究领域:
植物病理学
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真菌学
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采后病害防治
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天然产物化学
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真菌生理学
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转录组学
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产品关联
DOI
PubMed
高影响因子
BIOLOGICAL RESEARCH
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2025
·Vol. 58
·期 1
·1-22
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IF 4.6
Chen Hanbin,Li Guanghong,Deng Lin,Li Shuli,Huang Songqiang,Lee Simon Ming-Yuen,Nie Xiaowei,Bian Jin-Song
Background Pain serves as a vital protective mechanism triggered by tissue damage. While NSAIDs and opioids offer relief, their prolonged usage is hindered by adverse effects. Developing analgesics with fewer side effects is crucial for effective pain treatment. The TRPV1 channel is a key target for pain relief, with its inhibitors effectively reducing hyperalgesia in animals. This research utilized virtual screening to identify TRPV1-selective natural compounds for potent analgesic properties. Results The physcion exhibited the notable affinity for TRPV1 compared to the compounds examined. After conducting molecular dynamics simulations, physcion emerged as the compound demonstrating the highest binding affinity towards TRPV1, a finding corroborated by calcium imaging, which validated its inhibitory impact. Furthermore, physcion mitigated the stretch number in the acetic acid-induced stretching model, prolonged the latency period in the hot water tail-flick and hot plate assays, and heightened the pain withdrawal threshold lowered by complete Freund’s adjuvant (CFA). Notably, physcion exerted a marked effect in ameliorating bone cancer-induced pain in the hot plate and von Frey tests. Additionally, physcion diminished the levels of inflammatory cytokines and the mRNA expression of both inflammatory and calcium-related genes in the CFA-induced murine model. Furthermore, physcion downregulated the expression of inflammatory genes induced by tumor necrosis factor-α (TNF-α) in RAW264.7 cells. The underlying mechanism potentially involves the suppression of the NF-κB and MAPK signaling cascades. Conclusions Our investigation underscores the potential of physcion as a promising candidate for analgesic therapy.
研究领域:
药理学
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疼痛研究
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分子生物学
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计算生物学
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炎症研究
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神经药理学
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肿瘤学
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药物研发
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产品关联
DOI
PubMed
高影响因子
PHARMACEUTICAL BIOLOGY
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2015
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IF 1.241
Nian-Gui Xu,Zhi-Jie Xiao,Ting Zou,Zhi-Ling Huang
Context: Polygonum cuspidatum Sieb. Et Zucc. (Polygonaceae) has been traditionally used in folk medicine to treat various diseases.Objective: This study investigates the ameliorative effects of physcion 8-O-β-glucopyranoside (PSG) isolated from P. cuspidatum on learning and memory in dementia rats induced by Aβ1–40.Materials and methods: Dementia rats were prepared by intracerebroventricular injection of Aβ1–40. PSG (5, 10, 20, and 40 mg/kg/d, for 5 d) was administered orally. Ameliorative activity of PSG in dementia rats was evaluated by the Morris water maze (MWM) test, and its mechanisms were explored by evaluating AchE activity, levels of DA, NE, and 5-HT in hippocampus, and drebrin protein expressions in hippocampus.Results: Our results indicated that PSG (5, 10, 20, and 40 mg/kg/d) significantly inhibited the prolonged latency in dementia rats (p < 0.05), and inhibitory rates were 16.5, 22.7, 33.0, and 44.8% after 5 d of learning, indicating that PSG improves learning and memory of dementia rats. Furthermore, PSG significantly decreased AchE activity (10, 20, and 40 mg/kg/d; p < 0.05), increased 5-HT (20 and 40 mg/kg/d, p < 0.05), NE (10, 20, and 40 mg/kg/d; p < 0.05), and DA levels (5, 10, 20, and 40 mg/kg; p < 0.05) in the hippocampus. Additionally, PSG obviously decreased the Aβ contents in hippocampus (10, 20, and 40 mg/kg/d; p < 0.05), and up-regulated drebrin protein expressions (5, 10, 20, and 40 mg/kg/d; p < 0.05).Conclusions: PSG can significantly enhance learning and memory in Aβ1–40-induced dementia rats, and the mechanisms may be related to increase levels of Ach, 5-HT, NE, and DA, decrease Aβ contents, and up-regulation of drebrin proteins in hippocampus.
研究领域:
药理学
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神经科学
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传统医学
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产品关联
DOI
PubMed
高影响因子
Frontiers in Pharmacology
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2025
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IF 4.8
Zhihui Li,Yanqiu Gu,Jianbo Yang,Shaozhan Wang,Shengnan Li,Panpan Chen,Ru Yao,Fangbin Liu,Ying Wang,Rong Wang,Yongfang Yuan
Introduction Polygonum multiflorum Thunb. (PM) is a representative traditional Chinese medicine (TCM) that exerts different effects in raw and processed forms. The hepatotoxicity of PM is markedly reduced after processing, whereas its hepatoprotective effects are enhanced. Purpose This study aimed to establish a novel comprehensive two-dimensional (2D) biochromatography system based on farnesoid X receptor (FXR), which is an important target in cholestatic liver injury (CLI), to investigate the material basis and mechanisms underlying the enhanced hepatoprotection and reduced hepatotoxicity of processed PM (P-PM). Methods A comprehensive 2D FXR biochromatography system was established by immobilizing FXR on 3-mercaptopropyltrimethoxysilane (MPTS)-modified silica gel. This system was used to identify the FXR-binding components in raw PM (R-PM) and P-PM. Molecular docking, surface plasmon resonance, and frontal affinity chromatography were used to validate the interactions. The hepatoprotective effects of emodin and physcion were assessed in α-naphthylisothiocyanate (ANIT)-induced CLI mouse models, and an FXR antagonist (Z-guggulsterone) rescue experiment was performed. The expression of FXR signaling-related proteins, including FXR, small heterodimer partner (SHP), bile salt export pump (BSEP), Na+-taurocholate cotransporting polypeptide (NTCP), and inflammatory cytokines, was assessed by Western blotting, real-time quantitative reverse transcription PCR, and immunofluorescence. Results The comprehensive 2D FXR biochromatography system successfully identified emodin and physcion as key FXR-binding components, with significantly increased content in P-PM. These components may contribute to the enhanced hepatoprotection and reduced hepatotoxicity of P-PM. In vivo , emodin and physcion alleviated ANIT-induced CLI, as evidenced by improved histopathological features and decreased serum levels of liver function markers. Mechanistically, both components upregulated the expression of FXR, BSEP, SHP, and NTCP while suppressing inflammatory cytokine expression. Their hepatoprotective effects and FXR-related upregulation could be disrupted by FXR antagonist Z-guggulsterone. These results suggest that emodin and physcion are key components contributing to the hepatoprotective effects of P-PM, likely through activation of the FXR signaling pathway and suppression of inflammation. Conclusion This study established a novel, efficient, rapid, and accurate comprehensive 2D FXR biochromatography system, which is suitable for screening targeted components in TCM, and can be extended to research on other TCMs.
研究领域:
生药学
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中医药学
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分子药理学
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天然产物化学
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肝脏疾病研究
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色谱分离技术
✓ 已验证
产品关联
DOI
PubMed
高影响因子