VIROLOGICA SINICA
·
2012
·Vol. 27
·期 1
·19-25
·
IF 0
Liang Yuan-Yuan,Wang Bin,Qian Dong-Meng,Li Ling,Wang Zhi-Hao,Hu Ming,Song Xu-Xia
To investigate the inhibitory effects of Ginsenoside Rb1 (GRb1) on apoptosis caused by Herpes Simplex Virus-1(HSV-1) in Human Glioma Cells (U251), U251 cells were infected by HSV-1 at a multiplicity of infection of 5 and GRb1, GRb1+HSV-1, HSV-1 and control groups. MTT and cell apoptosis assays were used to detect the inhibitory effects of GRb1 on the apoptosis of U251 cells that caused by HSV-1 infection for various concentrations of drug and virus treatments by MTT assay. We found that in the 400 μg/mL GRb1 and 400 μg/mL GRb1+HSV-1 groups, MTT values were higher than control group at all times ( P <0. 05). Moreover, the apoptosis rate in the 400 μg/mL GRb1+HSV-1 group was lower than the HSV-1 group ( P <0. 05). These results confirmed that, at appropriate concentrations, GRb1 could inhibit nerve cell apoptosis in HSV-1 infections.
研究领域:
医学
·
病毒学
·
神经科学
·
药理学
✓ 已验证
DOI
PubMed
Biomaterials Advances
·
2025
·
IF 6
Dongmin Chen,Xiaosheng Sheng,Huili Li,Qishu Jin,Ruqi Wang,Yuanzheng Qiu,Lefeng Su,Jinfeng Xu,Jiang Chang,Yumei Que,Chen Yang
The current unavailability of efficient myocardial repair therapies constitutes a significant bottleneck in the clinical management of myocardial infarction (MI). Ginsenoside Rb1 (GRb1) has emerged as a compound with potential benefits in safeguarding myocardial cells and facilitating the regeneration of myocardial tissue. However, its efficacy in treating MI-related ischemic conditions is hampered by its low bioavailability and inadequate angiogenic properties. In this study, the therapeutic potential of GRb1 is enhanced by a mesoporous basic copper carbonate (BCC) microsphere due to its excellent drug delivery capability and steady angiogenic degradation products (copper ions, Cu 2+ ). The cell experiments revealed that GRb1 and Cu 2+ could generate synergistic impacts on anti-cardiomyocyte apoptosis and endothelial cell angiogenesis, while a mouse model of MI illustrated that GRb1 loaded BCC (BCC@GRb1) could significantly enhance cardiac function, diminish the area of infarction and myocardial hypertrophy, reduce cardiomyocyte apoptosis, and augment vascularization within myocardial tissue. This investigation is pioneering in demonstrating the beneficial outcomes of combining drugs with bioactive carriers in myocardial regeneration and introduces a novel, precisely engineered drug delivery system as a potential therapeutic strategy for ischemic heart disease.
研究领域:
心血管医学
·
药学
·
材料科学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
PHARMACOLOGICAL RESEARCH
·
2025
·
IF 10.5
Rongfang Guo,Shuying Zhang,Anyao Li,Ping Zhang,Xin Peng,Xiaoyan Lu,Xiaohui Fan
Type 2 diabetes mellitus (T2DM) is a significant public health issue with high morbidity and mortality. Ginsenoside Rb1 (Rb1) and berberine (BBR), the main bioactive compounds of Panax ginseng and Coptis chinensis , respectively, are known for their hypoglycemic effects. Nevertheless, the synergistic effects and underlying mechanism of Rb1 and BBR on T2DM remain unclear. In this study, we utilized a leptin receptor-deficient (db/db) mouse model to investigate the protective effects of their combination treatment. Our findings demonstrated that the combined use of Rb1 and BBR at a 1:4 ratio had more pronounced effects than the first-line anti-diabetic drug metformin on reducing the weight ratio of white adipose tissue, ameliorating insulin resistance, and improving glucose and lipid metabolism. Using spatial transcriptomics, we revealed that metformin treatment improved gluconeogenesis and lipogenesis only in the periportal zone, while the combination treatment induced improvements throughout the liver lobule, with distinct key targets across different zones, thus underscoring a more comprehensive modulation of hepatic metabolism. This may be the key reason why this combination therapy demonstrated superior protective effects against T2DM. Additionally, the reversed expression of the key callback gene hepcidin (HAMP) and its regulator growth differentiation factor 15 (GDF15) following the combination therapy across all zones, along with validation experiments, further suggested that GDF15/HAMP pathway might be a key mechanism underlying the beneficial effects of Rb1 and BBR against T2DM. This study also indicates a path toward innovative drug cocktails for treating T2DM, offering a holistic approach to regulate the entire liver lobule metabolism.
研究领域:
医学
·
分子生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF CHROMATOGRAPHY A
·
2021
·
IF 4.759
Xiuhong Wu,Boquan Qu,Yongkang Liu,Xingxuan Ren,Shaoyan Wang,Yanling Quan
In this study, an enzyme immobilization method for the effective biotransformation of ginsenoside Rb1 to impart activity and stability was developed. Using a hydrolase enzyme model, β-glucosidase from Aspergillus niger , immobilization within chemically affinity-linked amino-based silica provided an immobilization efficiency 5.86-fold higher than that of free enzyme. Compared with the free enzyme, the immobilized enzyme functioned optimally at a wider pH range and had higher thermostability. The optimum pH for the free and immobilized enzymes was 5.5. The optimal reaction temperature of the immobilized enzyme was 45 °C, which was 5 °C higher than that of the free enzyme. The Michaelis constant ( K m ) values before and after immobilization were 0.482 mmol•L −1 and 0.387 mmol•L −1 , respectively. The catalytic rate ( K cat ) for the immobilized and free enzymes was 22.269 mmol•L −1 and 8.800 mmol•L −1 , respectively, and the catalytic efficiency ( K cat / K m ) activity of the immobilized enzyme was 3.30-fold higher than that of the free enzyme. The immobilized enzyme could preserve 97 % of the activity after 45 cycles of repeated use. The high catalytic activity and significant operational stability are beneficial for industrial applications.
研究领域:
生物化学
·
酶工程
✓ 已验证
DOI
高影响因子
APPLIED BIOCHEMISTRY AND BIOTECHNOLOGY
·
2024
·
IF 3.1
An Le,Yu Yang,He Long,Xiao Xu,Li Pengcheng
There are numerous therapeutic applications for ginsenoside Rb1 (GRb1), the primary saponin derived from ginseng root. According to earlier research, ginsenoside Rb1 causes apoptosis and reduces the cell cycle. Its adverse effects, especially those on the development of the embryo, still need to be thoroughly studied. A host’s lifestyle choices, including smoking, drinking too much alcohol, using tobacco products, and having an HPV infection, can increase the risk of oral squamous cell carcinoma (OSCC), one of the most prevalent malignancies of the oral cavity. To address this challenge, this investigation focuses on the design of GRb1 for treating OSCC. In vitro cytotoxicity studies confirmed that GRb1 was more effective in PCI-9A and PCI-13 cells, with reduced toxicity in non-cancerous cells. Further verification of cellular morphology was achieved through various biochemical staining methods. The mechanism of cell death was investigated by Annexin V-FITC and PI methods. Additionally, the antimetastatic attributes of GRb1 have been evaluated using both migration scratch and Transwell migration assays, which have collectively revealed excellent antimetastatic potential. The DNA fragmentation of the PCI-9A and PCI-13 cells was assessed using a comet assay. Ginsenoside Rb1 improved ROS levels and caused mitochondrial membrane potential alterations and DNA damage, which resulted in apoptosis. OSCC administration significantly reduced the levels of SOD, GSH, GPx, and CAT, increasing the levels of PCI-9A and PCI-13 cells, while GRb1 improved this situation. Therefore, we propose that Ginsenoside Rb1 could be an alternative therapeutic strategy for OSCC therapy.
研究领域:
肿瘤学
·
药理学
·
细胞生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
BRAIN RESEARCH
·
2018
·
IF 3.125
Guo-Li Wang,Ying-Ping Wang,Jing-Yu Zheng,Lian-Xue Zhang
Ginsenoside Rb1 (Rb1), as the major bioactive ingredient of Panax ginseng C.A. Meyer, elicited a novel antidepressant-like effect in the forced swim test (FST) in chronic unpredictable mild stress (CUMS) rats in our previous study. To further explore the molecular mechanism of Rb1 on the neurotransmitters such as 5-hydroxytryptamine (5-HT), 5-hydroxyindole-3-acetic acid (5-HIAA), norepinephrine (NE), dopamine (DA), homovanillic acid (HVA), dihydroxyphenylacetic acid (DOPAC), glutamate (Glu) and gamma-aminobutyric acid (GABA) in this antidepressant-like effect, the neurochemical changes in the monoaminergic and aminoacidergic receptors were investigated in the present pharmacological study by using reuptake inhibitors, receptors agonists and antagonists. The results showed that a sub-effective dose of Rb1 (5 mg/kg, p.o.) co-administered with fluoxetine (1 mg/kg, i.p., a selective serotonin reuptake inhibitor), reboxetine (2.5 mg/kg, i.p., a noradrenalin reuptake inhibitor), bupropion (10 mg/kg, i.p., a dopaminergic reuptake inhibitor), Mk-801 (0.05 mg/kg, i.p., an N-methyl- d -aspartic acid (NMDA) receptor antagonist) or baclofen (0.1 mg/kg, i.p., a selective GABA agonist) significantly decreased the immobility time in the FST. In addition, pretreating mice with NAN190 (0.5 mg/kg, i.p., a 5-HT 1A receptor antagonist), ketanserin (5 mg/kg, i.p., a 5-HT 2A/2C receptor antagonist), ondansetron (1 mg/kg, i.p., a 5-HT 3A receptor antagonist), prazosin (1 mg/kg, i.p., an α 1 -adrenoceptor antagonist), yohimbine (1 mg/kg, i.p., an α 2 -adrenoceptor antagonist), SCH23390 (0.05 mg/kg, i.p., a selective D 1 receptor antagonist), haloperidol (0.2 mg/kg, i.p., a non-selective D 2 receptor antagonist), NMDA (75 mg/kg, i.p., an agonist at the glutamate site) or bicuculline (4 mg/kg, i.p., a competitive GABA antagonist) reversed the antidepressant-like effect of Rb1 (10 mg/kg, p.o.) in the FST. The results obtained for the neurotransmitters in the mouse hippocampus (CA3) and prefrontal cortex showed that Rb1 up-regulated the levels of 5-HT, 5-HIAA, NE, DA, and GABA and decreased the level of Glu. However, there were no significant differences in HVA or DOPAC. Furthermore, there were no significant alterations in the total path of spontaneous locomotor activity in all treatments. These results suggest that both monoaminergic (serotonergic, noradrenergic and dopaminergic) and aminoacidergic (glutamatergic and GABAergic) receptors may be involved in the antidepressant-like effect of Rb1.
研究领域:
药理学
·
神经科学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
STEROIDS
·
2015
·
IF 2.639
Xinxin Zhang,Zengjun Guo,Jing Li,Yoichiro Ito,Wenji Sun
A specific high performance liquid chromatography tandem mass spectrometry (HPLC–MS/MS method) was established for determining the concentration of protodioscin (PG) in rat plasma after intragastric administration of its standard form. Ginsenoside Rb 1 was selected as the internal standard (IS). The plasma sample was prepared using one-step deproteinization procedure by adding three parts of acetonitrile to precipitate proteins. The chromatographic separation was accomplished on an Inersil ODS-3 C 18 column (250 × 4.6 mm, 5 μm) with a mobile phase composed with acetonitrile and water containing 0.1% formic acid under a gradient elution mode at a flow rate of 1 mL min −1 . A 3:1 portion of the eluent after a microsplit was detected on a triple quadrupole tandem mass spectrometer coupled with electrospray ionization (ESI) in positive ion and multiple reaction monitoring (MRM) scanning modes. The mass transitions were selected as 888.1 → 1050.2 for PG and 948.2 → 1110.3 for IS, respectively. After careful validation, the plasma samples were always stable under different storage conditions. These analytical results rendered sensitive, selective, and reliable values by this established method which displayed high accuracy, adequate extracted recoveries, and almost negligible matrix effects. This method was applied to the pharmacokinetic studies on PG level in the rat plasma and its pharmacokinetic effect. The results of our studies suggest that the present method may be a useful tool for further clinical study of PG.
研究领域:
分析化学
·
药物代谢
·
生物医学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Food Bioscience
·
2021
·
IF 4.24
Qilong Wang,Yaping Wang,Yujiao Xie,Michael Adu-Frimpong,Chunmei Wei,Xia Yang,Xia Cao,Wenwen Deng,Elmurat Toreniyazov,Hao Ji,Ximing Xu,Jiangnan Yu
In the present study, a novel nonionic surfactant vesicles (NSVs) system consisting of cholesterol, Tween 80 and Span 80 was developed for the delivery of Ginsenoside Rb 1 with an improved oral bioavailability. The prepared vesicles were hollow and spherically shaped with acceptable diameter (264.68 ± 4.17 nm), zeta potential (−11.58 ± 0.87 mV) and encapsulation efficiency (69.034 ± 0.045%). XRD analysis provided affirmed the encapsulation of Rb 1 in the vesicles. The in vitro release profile of Rb 1 from the vesicles in the two different media (double distilled water, pH 7.0, phosphate buffer solution, pH 7.4) showed statistical insignificant difference when compared with the free Ginsenoside Rb 1 . Notably, the pharmacokinetic analysis of optimized Ginsenoside Rb 1 -NSVs exhibited a higher C max (9.55 ± 0.5 μg/mL versus 6.22 ± 0.53 μg/mL) with 1.82-fold increase in relative oral bioavailability. Collectively, these findings revealed that the developed vesicles could be a novel alternative in improving the oral bioavailability of Ginsenoside Rb 1 and extending its application in the clinical setting.
研究领域:
药剂学
·
中药学
✓ 已验证
DOI
高影响因子
JOURNAL OF ETHNOPHARMACOLOGY
·
2025
·
IF 5.4
Yingying Song,Xiaojuan Zhang,Xinyan Han,Gaorui Wang,Mengxue Wang,Hui Wu,Xiaojun Wu
Ethnopharmacological relevance The traditional Chinese herb Panax ginseng recorded in "Shennong Herbal Classic" is renowned for its purported vascular regulatory properties and immune-enhancing capabilities. Ginsenoside Rb1 (Rb1), a prominent bioactive compound in Panax, has demonstrated significant neuropharmacological activities. However, its impact on multiple sclerosis (MS) and blood-brain barrier (BBB) damage remains inadequately investigated. Aim of the study Inflammation and BBB disruption are pivotal to MS. Tightly packed brain capillary endothelial cells are fundamental to the structural and functional integrity of the BBB. Rb1 has been shown to alleviate BBB damage in stroke rats, but its effect on BBB damage in MS is not well understood. The objective of this study was to examine the role and mechanism of Rb1 on BBB injury in experimental autoimmune encephalomyelitis (EAE) mice. Materials and methods The BBB protection effect and mechanism of Rb1 were evaluated in LPS-treated bEnd.3 cells and EAE model mice. The mRNA expression levels of the inflammatory factor and the protein expressions of matrix metalloproteinases 9 (MMP9), zona occludens 1 (ZO-1), inhibitor of NF-κB (IκBα), occludin, Jun-amino-terminal kinase (JNK), and nuclear factor-κB (NF-κB) in bEnd.3 cells and mouse cerebral cortex were quantified. The permeability of bEnd.3 cells was examined by measuring trans-endothelial electrical resistance (TEER) and sodium fluorescein (NaF) leakage. Results Rb1 administration in the early stages of EAE postponed the disease's onset and lessened its severity. Rb1 inhibited the destruction of the BBB in brain cortex of EAE mice. Rb1 reduced the lipopolysaccharide (LPS)-induced hyperpermeability of bEnd.3 cells and prevented the downregulation of TJ proteins. In addition, in LPS-induced bEnd.3 cells, Rb1 decreased the overproduction of reactive oxygen species. Moreover, Rb1 suppressed the phosphorylation of JNK, ERK, NF-κB, and IκB in vivo and in vitro. Furthermore, the JNK agonist anisomycin was observed to partially abolish the protective effect of Rb1 in bEnd.3 cells treated with LPS. Conclusions Taken together, we demonstrated that Rb1 improved demyelination and BBB damage in EAE mice by modulating JNK/ERK/NF-κB signaling pathway. This study can offer a theoretical foundation for the use of Rb1 in the treatment of EAE by preventing BBB injury.
研究领域:
神经药理学
·
免疫学
·
中医药学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
AMERICAN JOURNAL OF CHINESE MEDICINE
·
2024
·
IF 4.8
Qing Zheng,Feng-Ping Lei,Shan Hui,Ming Tong,Li-Hui Liang
Cellular senescence is an adverse factor in the development of pulmonary fibrosis (PF). Ginsenoside Rb1 has been found to inhibit both cellular senescence and PF. This study aimed to elucidate the molecular mechanisms by which ginsenoside Rb1 regulates cellular senescence and PF. A PF mouse model was established by Bleomycin (BLM) administration, and a cell model of senescence was constructed using MRC-5 cells treated with Adriamycin RD (ARD) administration. Hematoxylin and Eosin (HE) staining and Masson staining were employed to evaluate cellular structure and collagen fiber content. RT-qPCR and western blotting were used to detect mRNA and protein expression of the target genes. Enzyme-linked Immunosorbent Assay (ELISA) was applied to measure the protein concentration of IL-1 β and IL-18. SA- β -gal staining was used to evaluate cellular senescence. Our results show that ginsenoside Rb1 effectively suppressed BLM-induced PF in mice. ARD administration to induce cellular senescence reduced NRF2, QKI, and SMAD7 expression in MRC-5 cells. By inducing NRF2 overexpression, ARD-induced cellular senescence and fibrosis in MRC-5 cells were relieved. Notably, NRF2 knockdown abolished the mitigating effects of ginsenoside Rb1 on ARD-induced cellular senescence and fibrosis in MRC-5 cells. Mechanistically, NRF2 increased SMAD7 mRNA stability through the transcriptional regulation of QKI. As expected, ginsenoside Rb1 alleviated ARD-induced senescence and fibrosis in MRC-5 cells by activating the NRF2/QKI/SMAD7 axis. Therefore, it was found that ginsenoside Rb1 mitigates cellular senescence and fibrosis during PF progression by activating the NRF2/QKI/SMAD7 axis. This study provides a potential therapeutic strategy for the treatment of PF and elucidates its mechanism of action.
研究领域:
药理学
·
呼吸病学
·
分子生物学
·
细胞生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
WORLD JOURNAL OF MICROBIOLOGY & BIOTECHNOLOGY
·
2011
·Vol. 28
·期 3
·857-863
·
IF 1.214
Ye Li,Zhang Chunyan,Li Jiyang,Shi Xunlong,Feng Meiqing
Calcium is a known signalling molecule in eukaryotic cells and plays a central role in the regulation of many cellular processes. In the following study, we report on the effect of external calcium treatments on the biotransformation of ginsenoside Rb1 to ginsenoside Rd by Paecilomyces bainier 229-7. We observed that the intracellular calcium content of P . bainier 229-7 mycelia was increased in response to exposure to high external Ca 2+ concentrations. Both ginsenoside Rd biotransformation and β-glucosidase activity were both found to be dependent on the external calcium concentration. At an optimal Ca 2+ concentration of 45 mM, maximal ginsenoside Rd bioconversion rate of 92.44% was observed and maximal β-glucosidase activity of 0.1778 U was reached in a 72-h biotransformation. The Ca 2+ channel blocker Verapamil blocked the trans-membrane influx of calcium and decreased ginsenoside Rd biotransformatiom. In addition, β-glucosidase activity and ginsenoside Rd content decreased by 36.0 and 29.2% respectively after a 72-h incubation in the presence of 0.05 mM Calmodulin (CaM) antagonist Perphenazine. These results suggest that both Ca 2+ channels and CaM are involved in ginsenoside Rd biotransformation via regulation of β-glucosidase activity. This is the first report regarding the effects of calcium signal transduction on biotransformation and enzyme activity in fungi.
研究领域:
药理学
·
微生物学
·
生物化学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Journal of Ginseng Research
·
2021
·
IF 6.06
Jingui Hu,Ling Zhang,Fei Fu,Qiong Lai,Lu Zhang,Tao Liu,Boyang Yu,Junping Kou,Fang Li
Background Ginsenoside Rb1, a bioactive component isolated from the Panax ginseng, acts as a remedy to prevent myocardial injury. However, it is obscure whether the cardioprotective functions of Rb1 are related to the regulation of endogenous metabolites, and its potential molecular mechanism still needs further clarification, especially from a comprehensive metabolomics profiling perspective. Methods The mice model of acute myocardial ischemia (AMI) and oxygen glucose deprivation (OGD)-induced cardiomyocytes injury were applied to explore the protective effect and mechanism of Rb1. Meanwhile, the comprehensive metabolomics profiling was conducted by high-performance liquid chromatography and quadrupole time-of-flight mass spectrometry (HPLC-Q/TOF-MS) and a tandem liquid chromatography and mass spectrometry (LC-MS). Results Rb1 treatment profoundly reduced the infarct size and attenuated myocardial injury. The metabolic network map of 65 differential endogenous metabolites was constructed and provided a new inspiration for the treatment of AMI by Rb1, which was mainly associated with mitophagy. In vivo and in vitro experiments, Rb1 was found to improve mitochondrial morphology, mitochondrial function and promote mitophagy. Interestingly, the mitophagy inhibitor partly attenuated the cardioprotective effect of Rb1. Additionally, Rb1 markedly facilitated the phosphorylation of AMP-activated protein kinase α (AMPKα), and AMPK inhibition partially weakened the role of Rb1 in promoting mitophagy. Conclusions Ginsenoside Rb1 protects acute myocardial ischemia injury through promoting mitophagy via AMPKα phosphorylation, which might lay the foundation for the further application of Rb1 in cardiovascular diseases.
研究领域:
药理学
·
心脏病学
·
代谢组学
·
分子生物学
✓ 已验证
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）