JOURNAL OF ETHNOPHARMACOLOGY
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2025
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IF 5.4
Yan Du,Yu-lang Chen,Ying Zhang,Yan-lin Zhao,Zhong Huang,Peng Jin,Shuai Ji,Dao-Quan Tang
Ethnopharmacological relevance Mulberry ( Morus alba L.) leaf is a well-known herbal medicine in China for thousands of years. Mulberry leaf can regulate arachidonic acid (ARA) metabolism disorder in obesity and type 2 diabetes mellitus. However, the active ingredients involved in this process are still unclear. Aim of study To explore the potential active ingredients in mulberry leaf against ARA metabolism disorder. Materials and methods In this research, an efficient method combining affinity ultrafiltration, molecular docking, and network pharmacology was developed and applied to explore cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX) inhibitors from mulberry leaf. Results A total 17 potential inhibitors were screened by affinity ultrafiltration assay and identified by high resolution mass spectrometry. In addition, 8 bioactive ingredients were obtained after re-evaluated by molecular docking and network pharmacology, and their inhibitory activities on COX-2 and 5-LOX were confirmed by in vitro inhibitory assays. The results of cell experiments showed that the expressions of COX-2 and 5-LOX were significantly suppressed by neochlorogenic acid, rutin, isoquercetin, and (−)-syringaresinol-4-O-glucoside. Conclusion Neochlorogenic acid, rutin, isoquercetin, and (−)-syringaresinol-4-O-glucoside may be the potential material basis of mulberry leaf in the regulation of ARA metabolism of obesity and type 2 diabetes mellitus.
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
ASIAN JOURNAL OF ANDROLOGY
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2019
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IF 2.862
Tao Li,Fu-Dong Fu,Chang-Jing Wu,Feng Qin,Run Wang,Jiu-Hong Yuan
This study aimed to explore whether and how anti-lysyl oxidase (anti-LOX) combined with a vacuum device (VD) could promote penile lengthening and to evaluate the effect on erectile function. This study was performed on four groups of adult rats: control, anti-LOX, VD (negative pressure value of −300 mmHg), and anti-LOX + VD. Penile length was measured by a modified VD method and verified on exposed length data. Intracavernous pressure (ICP) and maximum ICP/mean arterial pressure (MAP) ratio were recorded to assess erectile function. For corpus cavernosum, LOX activity and concentrations of pyridinoline, desmosine, hydroxyproline, and elastin were analyzed; transmission electron microscope and Hart's elastin staining were performed to monitor microstructural changes. Anti-LOX and VD significantly lengthened the penis by 10.8% (3.75 mm) and 8.2% (2.48 mm) compared with the control group, respectively, while anti-LOX + VD achieved the longest penile size (40.58 ± 0.40 mm) which was 17.4% longer than the control group (34.58 ± 0.54 mm). After 1-week washout, no penile retraction was observed. Meanwhile, exposed penile length data confirmed that the penis in the anti-LOX + VD group was also significantly longer. Anti-LOX inhibited LOX activity to reduce pyridinoline level, which led the penile tunica albuginea remodeling. However, it had no effect on hydroxyproline, desmosine, and elastin levels. Moreover, anti-LOX had no impact on erectile function, which was determined by ICP and ICP/MAP ratio. These results suggest that anti-LOX elongates the penis by reducing pyridinoline, which induces tunica albuginea remodeling. This lengthening effect was more obvious when combined with a VD. All procedures had no impact on erectile function.
研究领域:
泌尿学
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药理学
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生物医学工程
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DOI
PubMed
高影响因子
Advanced Healthcare Materials
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2024
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IF 10
Xiaotong Xu,Huimin Li,Binghua Tong,Weijie Zhang,Xiaofei Wang,Yue Wang,Geng Tian,Zhaowei Xu,Guilong Zhang
Herein, we designed a ccRCC targeting nanodrug to enhance chemodynamic therapy (CDT) as well as activate cuproptosis and tumor immunotherapy via ccRCC cell membrane modifying CuO@Gd 2 O 3 yolk-like particles (CGYL) loaded with lactate oxidase (LOx) (mCGYL-LOx). Benefiting from the homologous targeting effect of Renca cell membranes, the mCGYS-LOx could be effectively internalized by Renca cells, opened the “gate”, and then released LOx and copper ions. LOx could catalyze excessive lactate in Renca cells into H 2 O 2 , following that the produced H 2 O 2 was further converted by copper ions to the highly toxic ·OH, contributing to tumor CDT. Meanwhile, the excessive copper ions effectively triggered tumor cuproptosis. These synergistic effects induced the release of damage associated molecular patterns and activated immunogenic cell death, leading to DC maturation and infiltration of immune effector cells. Moreover, LOx-mediated lactate consumption downregulated the expression of PD-L1, crippling tumor immune escape. In addition, the mCGYL-LOx improved T 1 -weighted MRI signal, allowing for accurate diagnosis of ccRCC. This study demonstrated that the mCGYL-LOx had great potential for improving therapy of ccRCC via the synergistic actions of CDT and cuproptosis as well as immunotherapy. This article is protected by copyright. All rights reserved
研究领域:
肿瘤学
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纳米技术
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免疫疗法
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生物医学工程
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分子生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
BIOORGANIC CHEMISTRY
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2022
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IF 5.307
Hanjing Liang,Qingmei Feng,Hui Guo,Jiangnan Lv,Lingxia Zhang,Qingxia Li,Jun Chi,Qiuyan Liu,Zhimin Wang,Liping Dai
Nine new cadinane-type sesquiterpenoids ( 1 – 9 ) and three new eucalyptane -type sesquiterpenes ( 10 – 12 ) were isolated from the ethyl acetate extract of Burdock leaves, which were commonly used for preventing or treating atherosclerosis in China. Their structures were confirmed by extensive spectroscopic analysis, single-crystal X-ray diffraction analysis and ECD calculations. Compound 1 possessed the rare large conjugated skeleton. All the isolates were evaluated for anti-inflammatory and cholesterol-lowering activities by the LPS- and oxidized-low-density-lipoprotein-stimulated RAW 264.7 cells, respectively. As the results, all isolates could decrease the productions of NO, and down-regulate the accumulation of cholesterol. Among them, 4 showed the most potent cholesterol-lowering effect. For the high content of 4 in the herb, mechanistic study of 4 was performed and the results showed that 4 markedly reduced the release of pro-inflammatory mediators which was probably associated with inhibition of the PI3K/Akt and 5-LOX signaling pathways. The findings of this study demonstrated the anti-inflammatory/cholesterol-lowering effects of the new sesquiterpenes from burdock leaves, which provides chemical basis and scientific evidence for the herb used as anti-atherosclerosis agents for the further study. The sesquiterpene lactones of burdock leaves are expected to become new small molecule inhibitors for the treatment of AS .
研究领域:
药理学
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化学
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分子生物学
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植物科学
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产品关联
DOI
PubMed
高影响因子
PHYTOMEDICINE
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2024
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IF 6.7
Junling Ren,Xia Wang,Yuran Sun,Le Yang,Hui Sun,Ye Sun,Ling Kong,Guangli Yan,Ying Han,Xijun Wang
Background Danggui Sini Decoction (DGSND) is a classic prescription for treating primary dysmenorrhea (PD), while, the ameliorating effects of DGSND on PD and its mechanisms are not yet fully understood. Purpose The present study is devoted to investigate the protective effect of DGSND against PD and the possible mechanism from the perspective of metabolomics as well as lipidomics. Methods DGSND was characterized by UPLC-Q-TOF/MS. The PD rat model was induced by estradiol benzoate and oxytocin, and traditional pharmacology, including writhing times, latency time, biochemical index, organ index, and histopathology were performed to evaluated the efficacy of DGSND on PD. Urine metabolomics strategy combined with functional analysis was adopted to delineate the therapeutic effect of DGSND on PD rats and anchor the crucial pathway, and lipidomics analysis was further performed with the uterine tissue as the research object to elucidate the protective mechanism of DGSND from the perspective of lipid homeostasis. Finally, western blot analysis was used to validate the expression of key metabolic enzymes in lipid metabolism. Results DGSND was effective in ameliorating writhing times, latency time, the value of prostaglandin F 2α (PGF 2α )/PGE 2 , uterus index, and morphological changes of PD rats. Metabolic signature of PD rats was primarily characterized by the disturbance of steroid hormone metabolism, amino acid metabolism, and lipid metabolism. Functional analysis revealed the urine biomarkers of PD were most related with lipid abnormality. Further lipidomics analysis indicated DGSND exerted anti-PD effects by remodeling lipid homeostasis, which might be due to the significant correlations between different kinds of lipids, especially the extremely high correlation of phosphatidylethanolamine, phosphatidylcholine, and fatty acids. Moreover, the key metabolic enzymes expression of CK, PLA 2 , LPCAT3, COX-2, and 5-LOX can be greatly downregulated by DGSND. Conclusion Our findings demonstrated a novel protective mechanism of DGSND against PD by regulating lipid homeostasis.
研究领域:
药理学
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代谢组学
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脂质组学
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中医
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动物模型
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF DAIRY SCIENCE
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2021
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IF 4.034
Meng Wei,Ruo-Lin Zhou,Ting Luo,Ze-Yuan Deng,Jing Li
ABSTRACT Dairy fat intake has been considered as a risk factor for cardiovascular disease. Rodent models show that trans fatty acids in industrial hydrogenated oil and ruminant milk have different effects on cardiovascular diseases. One of the main reasons is that the distributions of trans fatty acids in triacylglycerols from dairy products and from industrial hydrogenated oil are different, which affects lipid absorption and metabolism. This study investigated the effects of 1,3-olein-2-elaidin (OEO, representing industrial hydrogenated oil triacylglycerols) and 1-vaccenic-2,3-olein (OOV, representing ruminant triacylglycerols in dairy products) on the function of human umbilical vein endothelial cells (HUVEC), including cell viability, lactate dehydrogenase (LDH) exudation rate, and nitric oxide secretory and nitric oxide synthase relative activity. We found that the detrimental effect of OEO on HUVEC was significantly greater than that of OOV. The results also showed that the absorption rate of OEO in HUVEC (78.25%) was significantly greater than that of OOV (63.32%). Mechanistically, based on phospholipidomics analysis, we found that calcium-independent phospholipase A2 (iPLA2) played a key role with regard to the OOV-mediated arachidonic acid (ARA)/COX-2/PG pathway, whereas secretory phospholipase A2 (sPLA2) and cytoplasmic phospholipase A2 (cPLA2) are responsible for the OEO-mediated ARA/COX-2/PG pathway. Moreover, OEO had a greater effect on the protein expression of COX-2 and PG secretion than OOV. In addition, iPLA2, sPLA2, and cPLA2 could mediate the ARA/CYP4A11 pathway in OOV-treated HUVEC, but only iPLA2 could mediate this pathway in HUVEC treated with OEO. We also found that sPLA2 could mediate the ARA/5-LOX pathway in HUVEC treated with OOV, but none of these 3 forms of PLA2 could mediate this pathway in HUVEC treated with OEO. On the other hand, after OOV treatment, trans -11 C18:1 was converted to beneficial forms of fatty acids in HUVEC, including conjugated linoleic acid (CLA) and trans -9 C16:1. In conclusion, we elucidated the potential mechanisms that might account for the diverse effects of triacylglycerols from industrial hydrogenated oil and ruminant milk on the function of HUVEC.
研究领域:
营养学
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心血管生物学
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细胞生物学
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生物化学
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产品关联
DOI
PubMed
高影响因子
Nano Today
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2022
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IF 18.962
Ziyou Wang,Bingwen Du,Xiangyu Gao,Yiling Huang,Meng Li,Zhaohan Yu,Jiyao Li,Xiuyuan Shi,Yi Deng,Kunneng Liang
Invasive bacterial infection interferes the normal orchestrated course of healing cascades during cutaneous regeneration. Hypoxia in the deep-seated infection microenvironment (IME) considerably precludes photonic disinfection efficacy, especially antibacterial photodynamic therapy (aPDT). Herein we develop IME-unlocked oxygen-evolving bio-catalytic fabrics composed of electrospun poly(ε-caprolactone) scaffolds, MXene/SnS 2 bio-heterojunctions (MX/SnS bio-HJs), and lactate oxidase (LOx) for deep-seated bacteria-infected cutaneous regeneration. LOx can deplete lactic acid produced by bacteria at infected site and yield hydrogen peroxide (H 2 O 2 ). The MX/SnS bio-HJs not only catalyze H 2 O 2 to produce hydroxyl radicals (·OH) through Fenton-like reaction, but also generate oxygen (O 2 ) to fortify aPDT under Near-infrared (NIR) light irradiation, consequently, expeditious disinfection is achieved. Moreover, in vivo results reveal that the bio-catalytic fabrics exert benign cutaneous regeneration ability by slaughtering bacteria, promoting hemostasis and collagen deposition. This work provides a tactic to instill fabrics with an IME-unlocked catalytic sterilization capability through endogenous O 2 evolution for remedying infected wounds.
研究领域:
生物医学工程
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材料科学
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光生物学
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伤口愈合
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细菌感染
✓ 已验证
产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）