Oxidative Medicine and Cellular Longevity
·
2022
·
IF 7.31
Yuan Liang,Jingqi Zhao,Haoyang Zou,Jie Zhang,Tiehua Zhang
As the main active ingredients of Panax ginseng, ginsenosides possess numerous bioactivities. Epidermal growth factor receptor (EGFR) was widely used as a valid target in anticancer therapy. Herein, the EGFR targeting activities of 20(S)-ginsenoside Rh2 (20(S)-Rh2) and the relationship of their structure-activity were investigated. Homogeneous time-resolved fluorescence assay showed that 20(S)-Rh2 significantly inhibited the activity against EGFR kinase. 20(S)-Rh2 was confirmed to effectively inhibited cell proliferation in a dose-dependent manner by MTT assay. Furthermore, quantitative real-time PCR and western blotting analysis revealed that 20(S)-Rh2 inhibited A549 cells growth via the EGFR-MAPK pathway. Meanwhile, 20(S)-Rh2 could promote cell apoptosis, block cell cycle, and reduce cell migration of A549 cells, respectively. In silico, the result suggested that both hydrophobic interactions and hydrogen-bonding interactions could contribute to stabilize their binding. Molecular dynamics simulation showed that the side chain sugar moiety of 20(S)-Rh2 was too flexible to be fixed at the active site of EGFR. Collectively, these findings suggested that 20(S)-Rh2 might serve as a potential EGFR tyrosine kinase inhibitor.
研究领域:
药理学
·
肿瘤学
·
分子生物学
·
生物化学
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DOI
PubMed
高影响因子
Food Chemistry-X
·
2024
·
IF 6.5
Yue E,Weimiao Li,Hongbin Guo,Xianman Zhang,Qinggele Caiyin,Yi Yuan
Yuling paste, a traditional Chinese health food derived from longan pulp and American ginseng, undergoes a unique processing method involving nine cycles of steaming and sun-drying. Ultra-high-performance liquid chromatography tandem mass spectrometry combined with widely targeted metabolomics has been used to examine the dynamic change in metabolite profiles through the processing. A total of 758 metabolites were identified. Processing significantly affects metabolite changes, and network pharmacology is subsequently used to explore potential pharmacological ingredients. After processing, the contents of active ingredients such as ginsenoside rh2, oleanolic acid, choline, d -glucose, and D-galacturonic acid were found to increase significantly. These increases can be correlated to the enhancement of five distinct pathways, and the contents of naringenin-7-O-glucoside, adenosine, pantothenic acid, and D-sucrose decreased after the processing, correlating with decreases in two different pathways. This study provides a comprehensive reference and scientific basis for understanding the health benefits associated with this traditional health food.
研究领域:
食品科学
·
中药学
·
代谢组学
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产品关联
DOI
PubMed
高影响因子
Polymers
·
2023
·Vol. 15
·期 19
·4011
·
IF 5
Huan-Jun Lu,Jian-Ke Cen,Yu Ren,Mei-Xian Li
Nanoparticle delivery of functional molecules or vaccines is an effective method for the treatment of many diseases. This study aims to design ginsenoside Rh2-conjugated O-carboxymethyl chitosan (O-CMC/Rh2) as a drug delivery system and explore its anti-nociceptive effects. O-CMC/Rh2 was synthesized with an esterification reaction, and its chemical composition and morphology were evaluated using proton nuclear magnetic resonance (1H NMR), the attenuated total reflectance-Fourier transform infrared (ATR-FTIR) spectroscopy, and scanning electron microscopy (SEM). In addition, the in vitro cumulative release of Rh2 from the O-CMC/Rh2 was also evaluated under different pH conditions. The results showed that the ginsenoside Rh2 was successfully conjugated to the O-CMC matrix and exhibited a highly porous structure after conjugation, facilitating the release of Rh2 from O-CMC. Complete Freund’s adjuvant (CFA) and burn injury-induced pain models were used to evaluate the anti-nociceptive effects of O-CMC/Rh2 on inflammatory pain. O-CMC/Rh2 reduced CFA-induced pain hypersensitivity in a dose-dependent manner and had a longer analgesic effect than Rh2. In addition, O-CMC/Rh2 also relieved the chronic pain induced by bury injury. These results indicated that O-CMC/Rh2 could be useful in reducing inflammatory pain, thus possessing a potential medicinal application in pain therapy.Keywords:O-carboxymethyl chitosan;ginsenoside Rh2;anti-nociception;inflammatory pain
研究领域:
药学
·
纳米技术
·
疼痛管理
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产品关联
DOI
PubMed
高影响因子
Journal of Oncology
·
2021
·
IF 4.375
Xiaodan Sun,Peiyan Zhao,Hui Li,Yan Liu,Tianming Wang,Ying Cheng
Ginsenoside Rh2 (Rh2) is one of the pharmacologically active components of ginseng with an antitumor effect. However, its effect on non-small-cell lung cancer (NSCLC), especially on aerobic glycolysis, which plays a crucial role in the proliferation and progression of tumor cells, has not been characterized. Here, we demonstrated that Rh2 inhibited the proliferation and metastasis of NSCLC cells by promoting apoptosis and suppressing epithelial-mesenchymal transition, respectively. Notably, Rh2 exerted a glycolysis inhibition effect through regulating GLUT1, PKM2, and LDHA, which are key enzymes of the glycolysis process. Furthermore, the metabolic shift function of Rh2 was dependent on the STAT3/c-Myc axis in NSCLC. This novel regulatory role of Rh2 provides a new perspective for NSCLC treatment and highlights the potentiality of Rh2 to be used as a tumor energy blocker. The combination of Rh2 with an STAT3 or c-Myc inhibitor revealed a promising therapeutic approach for patients with NSCLC.
研究领域:
肿瘤学
·
药理学
·
代谢途径
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DOI
PubMed
高影响因子
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
·
2026
·
IF 6.7
Chen Zinuo,Xie Wei,Ye Fenglin,Chen Qingsheng,He Jingyu,Cao Yufei,Lou Wen-Yong
Rare
ginsenoside Rh2 has attracted increasing interest for its
antitumor, anti-inflammatory, and metabolic regulatory activities.
Enzymatic biotransformation provides a green and selective route for
Rh2 production, but current systems suffer from inefficient cascade
conversion and limited enzyme stability. Here, two β-glucosidases
enabling the stepwise and selective conversion of 20(S)-ginsenoside
Rd to 20(S)-ginsenoside Rh2 were identified and assembled into a fusion
biocatalyst through linker engineering. Compared with the parental
two-enzyme cascade under equimolar enzyme loading, the optimized fusion
enzyme reduced the accumulation of the intermediate Rg3 and increased
20(S)–Rh2 production rate by 40%. A Zn–Ni metal–organic
framework was further introduced to enable simultaneous purification
and immobilization. The immobilized fusion enzyme showed enhanced
operational stability, retaining 82% of its initial activity after
seven successive substrate-feeding intervals. This study presents
a multiscale strategy integrating enzyme fusion and MOF immobilization
for the efficient, operationally stable, and sustainable production
of 20(S)-ginsenoside Rh2.
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DOI
高影响因子
ENZYME AND MICROBIAL TECHNOLOGY
·
2026
·
IF 3.9
Fan Xu,Yuting Liao,Yulei Zhang,Nanyu Han,Junmei Ding,Li Wan,Wanmeng Mu
Ginsenoside Rh2, a potential anticancer agent originally isolated from the medicinal plant Panax ginseng , has low natural abundance and is difficult to extract, making biosynthetic production a promising alternative. UDP-glycosyltransferases (UGTs) that specifically catalyze protopanaxadiol (PPD) glycosylation to produce Rh2 have been widely identified in plants and microorganisms. In this study, we report that Barbarea vulgaris UGT73C21 effectively catalyzes this reaction. The enzyme was expressed in Escherichia coli and purified to electrophoretic homogeneity via Ni 2 ⁺-affinity chromatography. It exhibited optimal activity at pH 8.0 (100 mM HEPES) and 45 °C. Mn 2 ⁺, Mg 2 ⁺, and Ca 2 ⁺ significantly enhanced enzyme activity, whereas other tested metal ions reduced it. The kinetic parameters K m , V max , k cat , and k cat / K m were determined as 231.92 μM, 5.68 μM min −1 , 0.053 s −1 , and 228 M −1 s −1 , respectively. In a reaction containing 0.2 mg/mL UGT73C21, 1 mM PPD, and 5 mM UDP-Glucose in HEPES buffer (pH 8.0), 0.55 mM Rh2 was produced within 1 h, corresponding to a 55% conversion rate. These results demonstrate that B. vulgaris UGT73C21 is an efficient biocatalyst for ginsenoside Rh2 biosynthesis.
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产品关联
DOI
高影响因子
Nanomedicine
·
2019
·
IF 4.717
Xin Jin,Qing Yang,Ning Cai,Zhenhai Zhang
Aim: Lung cancer has a very high incidence rate, and thus, there is an urgent need for novel and effective therapies. Materials & methods: In this study, we proposed a potential treatment option by combining four natural products in liposome systems. Results:In vitro studies indicated that the combination of betulinic acid, parthenolide, honokiol and ginsenoside Rh2 exhibited a synergistic action. When these four natural products were loaded into liposome systems, we observed an increased effect. The relative action was also observed in vivo. The cisplatin group presented obvious kidney damage, whereas both cocktail therapy and cocktail liposome therapy were safer. Conclusion: Therefore, we propose cocktail liposome systems may provide a more efficient and safer treatment for lung cancer.
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DOI
高影响因子
Molecular Medicine Reports
·
2017
·Vol. 17
·期 2
·3062-3068
·
IF 1.692
Kai‑Fei Li,Chun‑Min Kang,Xiao‑Feng Yin,Hai‑Xia Li,Zhuo‑Yu Chen,Yao Li,Qiong Zhang,Yu‑Rong Qiu
Ginsenoside Rh2 (G‑Rh2), the main bioactive component in American ginseng, is known to exert a wide variety of biological activities. Accumulating evidence suggests that G‑Rh2 inhibits cell proliferation and induces apoptosis of tumor cells. However, the possible mechanism through which G‑Rh2 exerts its action on malignant glioma cells have not been completely elucidated. The findings of the present study demonstrated that G‑Rh2 decreased the viability of glioma cells in a dose‑ and time‑dependent manner, and induced cell cycle arrest. G‑Rh2‑induced cell cycle arrest was accompanied by the downregulation of cyclin‑dependent kinase 4 and Cyclin E. In addition, G‑Rh2 markedly reduced the expression of total‑ RAC‑α serine/threonine‑protein kinase (Akt) and the levels of phosphorylated‑Akt. These findings provide mechanistic details of how G‑Rh2 acts on glioma cells and suggest that G‑Rh2 may function as a potential anti‑cancer drug for glioma treatment.
研究领域:
肿瘤学
·
细胞生物学
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药理学
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DOI
PubMed
高影响因子
RSC Advances
·
2015
·Vol. 5
·期 96
·78874-78879
·
IF 3.84
Hui-da Wan,Dan Li
A preliminary study on the enzymatic biotransformation of ginsenosides is evaluated. β-Galactosidase from Aspergillus sp. displayed β-glucosidase activity, which was responsible for its ability to transform major ginsenoside Rb1 to rare ginsenoside F2 via ginsenoside Rd. The Rb1 conversion, Rd and F2 yields reached 100%, 80.7% and 14.3% after 60 h at 60 °C, respectively. Ginsenoside Rg3 can be selectively hydrolyzed and only Rh2 was obtained with this β-galactosidase as well. Before hydrolysis, an Rg3 inclusion complex was prepared with hydroxypropyl-β-cyclodextrin (HP-β-CD) to improve the aqueous solubility. The solubility of Rg3 increased 74.6 fold, and the phase solubility curve displayed a typical AL-type, which indicates the formation of a 1 : 1 inclusion complex. Using an enzyme loading of 500 U g−1 Rg3, the highest Rg3 conversion of 90.6% and Rh2 yield of 88.5% were obtained after 24 h at 60 °C. These results indicate that β-galactosidase from Aspergillus sp. could be useful for the mass production of rare ginsenosides.
研究领域:
生物化学
·
药学
·
酶学
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产品关联
DOI
高影响因子
BIOMACROMOLECULES
·
2017
·
IF 5.246
Ding Qu,Lixiang Wang,Meng Liu,Shiyang Shen,Teng Li,Yuping Liu,Mengmeng Huang,Congyan Liu,Yan Chen,Ran Mo
The aim of this study is to demonstrate the enhanced therapeutic efficacy of anticancer drugs on drug-resistant breast cancer using multicomponent microemulsions (ECG-MEs) as an oral delivery system. The etoposide-loaded ECG-MEs were composed of coix seed oil and ginsenoside Rh2 (G-Rh2), both of which possess not only the synergistic antitumor effect with etoposide, but also have excipient-like properties. Orally administrated ECG-MEs were demonstrated to be able to accumulate at the tumor site following crossing the intestines as intact vehicles into the blood circulation. The spatiotemporal controlled release characteristics of ECG-MEs brought about the efficient P-gp inhibition by the initially released G-Rh2 and the increased intracellular accumulation of the sequentially released etoposide. The combination antitumor activity of etoposide, G-Rh2 and coix seed oil using ECG-MEs was verified on the xenograft drug-resistant breast tumor mouse models. In addition, the safety evaluation studies indicated that treatment with ECG-MEs did not cause any significant toxicity in vivo. These findings suggest that ECG-MEs as an oral formulation may offer a promising strategy to treat the drug-resistant breast cancer.
研究领域:
药学
·
肿瘤学
·
纳米技术
·
药物递送系统
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DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2025
·
IF 5.2
Shengxia Hu,Dan Sun,Ling Tang,Liang Kong,Yang Liu,Fang Liu,Dongmei Tang,Xuhong Lu,Yuanyuan Wang
Introduction The silent killer epithelial ovarian cancer (EOC) is a lethal malignancy with high mortality rate and often diagnosed at an advanced stage. Traditional chemotherapy for EOC remains unsatisfactory as the tumor microenvironment (TME) is complicated and contains multiple factors such as tumor associated macrophages (TAMs). Therefore, a drug delivery system which codelivery chemotherapy drug and immune modulator for EOC treatment is urgently needed. Methods Follicle-stimulating hormone peptide-conjugated paclitaxel and ginsenoside Rh2 codelivery liposomes (FSH@PTX-Rh2-Lips) were prepared in this study. FSH was decorated on the liposomal surface to enhance cellar uptake, PTX was used to kill cancer cells, and Rh2 was added to induce macrophages repolarization as well as a member material. The targeting, anti-tumor effect and impact on macrophage repolarization of FSH@PTX-Rh2-Lips were evaluated in vitro and in vivo. Results With the ideal physicochemical properties, FSH@PTX-Rh2-Lips displayed increased cellular uptake, strong cytotoxicity to ID8 cells, inhibitory effect of tumor cell metastasis, and ability to induce macrophage repolarization from M2 to M1 in vitro. The tumor-bearing mice model suggested FSH@PTX-Rh2-Lips showed significant effect on antitumor and tumor recurrence, and the mechanism of FSH@PTX-Rh2-Lips in treatment of EOC was related to inhibiting tumor growth and inducing macrophage repolarization. Conclusion FSH@PTX-Rh2-Lips with function of affecting TAMs repolarization and altering the TME were successfully prepared and might offer an effective therapeutic strategy against EOC.
研究领域:
肿瘤学
·
药学
·
免疫学
·
癌症治疗
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产品关联
DOI
PubMed
高影响因子
ACS Applied Materials & Interfaces
·
2022
·
IF 10.383
Zhenzhong Li,Huating Jiang,Jinxiu Liu,Tiantian Ning,Nam T. S. Phan,Fang Zhang
Conformational dynamics of active sites in enzymes enable great control over the catalytic process. Herein, we constructed a metal–organic framework with conformationally dynamic active sites (Rh2-ZIF-8). The active sites in Rh2-ZIF-8 were composed of the imidazolate-bridged bimetallic center with a catalytic dirhodium moiety and structural zinc site. Even though the coordination sphere of the dirhodium species was saturated with two circularly arranged esp groups and two axial 2-MeIm ligands, it could still effectively catalyze the direct synthesis of N–H aziridines from olefins with high activity. We found that such a self-adaptive catalytic process was based on the dynamic breakage and reformation of the rhodium–zinc imidazolate bridges. Interestingly, the in situ generated dirhodium site with a unique Rh2(esp)2(2-MeIm)1 configuration was able to exhibit obviously enhanced selectivity compared to homogeneous catalyst Rh2(esp)2. Furthermore, the surrounding zinc imidazolate groups could effectively protect the dirhodium moieties from harsh environments, and this ultimately endowed it with high stability.
研究领域:
化学
·
材料科学
·
催化
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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）