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JOURNAL OF APPLIED MICROBIOLOGY · 2019 ·Vol. 126 ·期 3 ·740-751 · IF 2.683

Antimicrobial effects of the ginsenoside Rh2 on monospecies and multispecies cariogenic biofilms

Cao X.,Ye Q.,Fan M.,Liu C.

AimsTo investigate the effects of the ginsenoside Rh2 on monospecies and multispecies cariogenic biofilms and explore the mechanism of the antibiofilm effect of Rh2 in vitro.Methods and ResultsStreptococcus mutans, Streptococcus sobrinus and Streptococcus sanguinis were chosen to form the monospecies or multispecies biofilms. Crystal violet staining and laser scanning confocal microscopy were used to observe the effect of Rh2 on biofilms in vitro. Cytotoxicity was examined by the Cell Counting Kit‐8. The effects of Rh2 on bacterial membranes were observed via transmission electron microscopy (TEM). The isobaric tags for relative and absolute quantification (iTRAQ) method were used to profile the common differentially expressed proteins. Gene expression was analysed by reverse transcription quantitative polymerase chain reaction. In general, the treatment of cariogenic biofilms with Rh2 significantly decreased biomass accumulation by inhibiting bacterial growth and extracellular polysaccharide synthesis without any cytotoxic effects. TEM imaging showed that Rh2 could disrupt the cell membranes of these bacteria. The iTRAQ results indicated that the levels of mannose‐specific IIC/D and acetaldehyde/alcohol dehydrogenase were substantially down‐regulated, while the mRNA expression of the corresponding genes were significantly changed.ConclusionsOur data revealed a potential application for Rh2 in the protection against dental caries via the inhibition of cariogenic biofilms.Significance and Impact of the StudyThis study describes the first application of a ginsenoside against multispecies cariogenic biofilms. Rh2 may serve as an alternative agent to prevent dental caries by effectively modulating the pathogenic potentials of oral biofilms.

研究领域: 口腔微生物学 · 药理学 · 蛋白质组学
✓ 已验证 DOI 高影响因子
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Food Chemistry-X · 2024 · IF 6.5

Dynamic profiling of metabolite changes and health-promoting functions in ‘yuling paste’ during nine steaming and nine sun-drying processes

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.

CAS / MDL: 64-18-6
研究领域: 食品科学 · 中药学 · 代谢组学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Polymers · 2023 ·Vol. 15 ·期 19 ·4011 · IF 5

Evaluation of the Anti-Inflammatory Pain Effect of Ginsenoside-Conjugated O-Carboxymethyl Chitosan Particles

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

CAS / MDL: 67-56-1
研究领域: 药学 · 纳米技术 · 疼痛管理
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Molecular Catalysis · 2024 · IF 3.9

Study on synthesis of rare ginsenoside Rh2 by one-step purification and immobilization of glycosyltransferase from magnetic Ni-based MOF

Junsong Yue,Xiaochen Liu,Zhansheng Wu,Zhiyan Li,Jianwen Wang,Min Tu,Huaiqi Shi

To solve the problem that free glycosyltransferase is difficult to isolate and reuse in ginsenoside Rh2 catalysis and synthesis. In this study, we developed a magnetic nickel-based metal-organic framework (MOF) material (Fe 3 O 4/ PDA@MOF) to enable the separation of recombinant glycosyl transferase (UGT) directly from crude enzyme solutions, while simultaneously immobilizing it by utilizing the specific adsorption of Ni 2+ ions to His-tag. Our investigations demonstrated that the Fe 3 O 4 /PDA@MOF@UGT was successfully prepared, which not only maintained enzyme activity, but was reused by low-cost magnetic separation and exhibited enhanced enzyme loading and stability. Following thorough research and optimization, the immobilized enzyme achieved a rare ginsenoside Rh2 concentration of 69.68 µg/mL under optimal conditions, with an initial activity of 61.99 % after six cycles. This cost-effective, efficient, and sustainable biocomposite holds significant promise for industrial applications in enzyme purification and catalytic synthesis of ginsenoside.

CAS / MDL: 62-31-7
研究领域: 生物化学 · 药学 · 合成生物学
✓ 已验证 产品关联 DOI 高影响因子
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DRUG DELIVERY · 2017 · IF 6.402

Preliminary study on fabrication, characterization and synergistic anti-lung cancer effects of self-assembled micelles of covalently conjugated celastrol–polyethylene glycol–ginsenoside Rh2

Peng Li,XiaoYue Zhou,Ding Qu,Mengfei Guo,Chenyi Fan,Tong Zhou,Yang Ling

The aim of this study was to develop an amphipathic polyethylene glycol (PEG) derivative that was bi-terminally modified with celastrol and ginsenoside Rh2 (Celastrol-PEG-G Rh2). Such derivative was capable of forming novel, celastrol-loaded polymeric micelles (CG-M) for endo/lysosomal delivery and thereby synergistic treatment of lung cancer. Celastrol-PEG-G Rh2 with a yield of 55.6% was first synthesized and characterized. Its critical micellar concentration was 1 × 10−5 M, determined by pyrene entrapment method. CG-M had a small particle size of 121.53 ± 2.35 nm, a narrow polydispersity index of 0.214 ± 0.001 and a moderately negative zeta potential of –23.14 ± 3.15 mV. Celastrol and G Rh2 were rapidly released from CG-M under acidic and enzymatic conditions, but slowly released in normal physiological environments. In cellular studies, the internalization of celastrol and G Rh2 by human non-small cell lung cancer (A549) cells treated with CG-M was 5.8-fold and 1.8-fold higher than that of non-micelle control. Combinational therapy of celastrol and G Rh2 using CG-M exhibited synergistic anticancer activities in cell apoptosis and proliferation assays via rapid drug release within endo/lysosomes. Most importantly, the celastrol in CG-M exhibited a long elimination half-life of 445.3 ± 43.5 min and an improved area under the curve of 645060.8 ± 63640.7 ng/mL/h, that were 1.03-fold and 2.44-fold greater than those of non-micelle control, respectively. These findings suggest that CG-M is a promising vector for precisely releasing anticancer drugs within the tumor cells, and thereby exerts an improved synergistic anti-lung cancer effect.

CAS / MDL: 298-93-1
研究领域: 药学 · 肿瘤学 · 纳米技术 · 药物递送系统
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Cancer Medicine · 2023 · IF 4

Ginsenoside Rh2 attenuates the progression of non-small cell lung cancer by sponging miR-28-5p/STK4 axis and inactivating Wnt/β-catenin signaling

Jun Ma,Di Zhao,Dahai Yu,Wei Song,Xiaofang Yang,Haitao Yin

Background Ginsenoside Rh2 (G-Rh2) exerts anti-tumor activity in non-small cell lung cancer (NSCLC). microRNAs (miRNAs, miRs) play pivotal roles in NSCLC. We aimed to investigate whether G-Rh2 inhibited NSCLC progression by targeting miRNA. Methods Cell viability, apoptosis and cycle were determined by Cell Counting Kit-8, 6-diamidino-2-phenylindole (DAPI) staining and flow cytometry. The potential target miRNAs of G-Rh2 were screened by real-time quantitative polymerase chain reaction (RT-qPCR). The difference in miR-28-5p expression between lung adenocarcinoma (LUAD) tissues and normal tissues or lung squamous cell carcinoma (LUSC) tissues and normal tissues was retrieved from TCGA-LUAD and TCGA-LUSC, respectively. Kaplan–Meier Plotter was conducted to analyze the survival rate for different serine/threonine-protein kinase 4 (STK4) expressions with different prognostic risks. immunohistochemistry of STK4 expression in non-tumor and tumor tissues was analyzed from the HPA database. RT-qPCR and Western blot were adopted for detecting mRNA and protein expression. TargetScan V7.2, miRanda and PITA were adopted for predicting targets of miR-28-5p, overlapped genes were subjected to GO analysis. The interactions of miR-28-5p-Wnt and miR-28-5p-STK4 were detected by TOP/FOP luciferase reporter assay and dual luciferase reporter assay, respectively. Results Current study observed that G-Rh2 reduced miR-28-5p expression in NSCLC cells dose-dependently. miR-28-5p was upregulated in NSCLC tissues and cells. The target genes of miR-28-5p were enriched in negative regulation of Wnt signaling. miR-28-5p inhibitor inactivated Wnt signaling, inhibited cell viability and cell cycle, while enhanced cell apoptosis of NSCLC cells by targeting STK4. G-Rh2 exerted the similar effects with miR-28-5p inhibitor by reducing miR-28-5p. G-Rh2 and miR-28-5p inhibitor exerted a synergistic effect on inhibiting NSCLC tumor growth. Conclusion In conclusion, G-Rh2 attenuates NSCLC development by affecting miR-28-5p/STK4 axis and inactivating Wnt signaling. Taken together, we project out a novel therapeutic target for NSCLC.

CAS / MDL: 30525-89-4 9002-93-1
研究领域: 肿瘤学 · 分子生物学 · 药理学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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AMERICAN JOURNAL OF CHINESE MEDICINE · 2025 ·Vol. 53 ·期 02 ·475-499 · IF 5.5

Ginsenoside Rh2 Ameliorates Myocardial Infarction by Regulating Cardiomyocyte Pyroptosis Based on Network Pharmacology, Molecular Docking, and Experimental Verification

Bing Li,Shuanglong Mou,Chenrui Zhang,Tingting Zhu,Xingwei Hu,Mengsha Li

Myocardial infarction (MI) is a significant threat to human health worldwide. Following MI, cardiomyocytes (CMs) undergo pyroptosis, exacerbating the damage caused by infarction. Ginseng may play a role in alleviating CM pyroptosis. However, further exploration is needed regarding its main active ingredients and effects. By employing network pharmacology on the active ingredients of ginseng, MI and pyroptosis, and employing molecular docking between such ingredients and pyroptosis-related proteins, we screened for the main ingredient of ginseng. Through network pharmacology and molecular docking, we identified ginsenoside Rh2, which acts on MI and cell pyroptosis, as the most likely active ingredient that stably binds to pyroptosis-related proteins. We subsequently constructed a neonatal rat CM oxygen–glucose deprivation (OGD) model in vitro and an MI mouse model in vivo . Ginsenoside Rh2 was administered, with losartan used as a positive control. In the in vitro OGD model, ginsenoside Rh2 increased the viability of primary rat CMs and mitigated OGD-induced pyroptosis. In the in vivo MI model, ginsenoside Rh2 reduced CM pyroptosis, decreased infarct size, and subsequently improved cardiac function. Our study provides a novel therapeutic strategy for MI by attenuating CM pyroptosis.

CAS / MDL: 78214-33-2 114798-26-4
研究领域: 药理学 · 心脏病学 · 分子生物学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Stem Cell Research & Therapy · 2025 ·Vol. 16 ·期 1 ·683 · IF 7.3

Ginsenoside Rh2 inhibits mesenchymal stem cell senescence by regulating mitochondrial and lysosomal function

Zhuang Jianjian,Li Yue,Huang Yi Ling,Wang Xiang,Lin Neng Ming

Background Mesenchymal stem cells (MSCs) undergo senescence after expansion and in vitro culture under oxidative stress, which limits their clinical application. Ginsenoside Rh2 has been confirmed to regulate mitochondrial function, but its role in modulating the senescence of MSCs has not been clearly investigated. Purpose This study aims to explore the effects and underlying mechanisms of Rh2 in inhibiting the senescence of MSCs. Methods Transmission electron microscopey (TEM) and fluorescence staining assays were used to monitor changes in mitochondrial and lysosomal morphology and function in Rh2-treated senescent MSCs. Quantitative reverse transcription polymerase chain reaction (qRT-PCR) and Western blot analyses were performed to evaluate the expression levels of senescence-related cytokine genes and proteins. Results Rh2 can inhibited the senescence of MSCs by activating Sirtuin 1(SIRT1). At the molecular level, SIRT1 regulated the Pink1/Parkin-mediated mitophagy pathway and suppressed the secretion of senescence-associated cytokines (IL-6 and IL-8). Additionally, Rh2 influenced lysosomal stability and sultimately inhibited exosome secretion through direct activation of SIRT1. Conclusion These findings provide a potential strategy for using Rh2 to overcome the senescence of MSCs, thereby enhancing their clinical application. Graphical

✓ 已验证 DOI PubMed 高影响因子
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DRUG DELIVERY · 2020 · IF 4.902

Increased antitumor efficacy of ginsenoside Rh2 via mixed micelles: in vivo and in vitro evaluation

Xiaojing Xia,Jin Tao,Zhuwa Ji,Chencheng Long,Ying Hu,Zhiying Zhao

The aim of this work is to apply Solutol® HS15 and TPGS to prepare self-assembled micelles loading with ginsenoside Rh2 to increase the solubility of ginsenoside Rh2, hence, improving the antitumor efficacy. Ginsenoside Rh2-mixed micelles (Rh2-M) were prepared by thin film dispersion method. The optimal Rh2-M was characterized by particle size, morphology, and drug encapsulation efficiency. The enhancement of in vivo anti-tumor efficacy of Rh2-M was evaluated by nude mice bearing tumor model. The solubility of Rh2 in self-assembled micelles was increased approximately 150-folds compared to free Rh2. In vitro results demonstrated that the particle size of Rh2-M is 74.72 ± 2.63 nm(PDI = 0.147 ± 0.15), and the morphology of Rh2-M is spherical or spheroid, and the EE% and LE% are 95.27 ± 1.26% and 7.68 ± 1.34%, respectively. The results of in vitro cell uptake and in vivo imaging showed that Rh2-M could not only increase the cell uptake of drugs, but also transport drug to tumor sites, prolonging the retention time. In vitro cytotoxicity and in vivo antitumor results showed that the anti-tumor effect of Rh2 can be effectively improved by Rh2-M. Therefore, Solutol® HS15 and TPGS could be used to entrapping Rh2 into micelles, enhancing solubility and antitumor efficacy.

CAS / MDL: 9002-96-4
研究领域: 药学 · 肿瘤学 · 纳米技术
✓ 已验证 产品关联 DOI PubMed 高影响因子
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EUROPEAN JOURNAL OF MEDICAL RESEARCH · 2024 ·Vol. 29 ·期 1 ·1-14 · IF 2.8

Ginsenoside Rh2 suppresses ferroptosis in ulcerative colitis by targeting specific protein 1 by upregulating microRNA-125a-5p

Zhao Xun,Yuan WenQiang,Yang LiuChan,Yan Fang,Cui DeJun

Background Worldwide, ulcerative colitis (UC) is becoming increasingly fast growing. Ginsenoside Rh2 has been reported to alleviate UC. However, the latent biological mechanism of Rh2 in the treatment of UC remains uncertain. In this study, the goal was to determine the therapeutic effect of Rh2 on dextran sulfate sodium (DSS)-induced UC. Methods A DSS-induced UC mouse model was established and divided into 7 groups for Rh2 gavage and/or miR-125a-5p lentivirus injection (n = 10 per group). Colonic specimens were collected for phenotypic and pathological analysis. miR-125a-5p and specific protein 1 (SP1) expression, inflammation-related factors IL-6 and IL-10, and apoptosis were detected in mice. Human normal colon epithelial cell line NCM460 was treated with H 2 O 2 and ferric chloride hexahydrate to construct an in vitro cell model of colitis and induce ferroptosis. Independent sample t-test was used to compare cell proliferation, cell entry, apoptosis, and oxidative stress between the two groups. One way analysis of variance combined with the least significant difference t test was used for comparison between groups. Multiple time points were compared by repeated measurement analysis of variance. Results DSS-induced UC mice had significantly decreased body weight, increased disease activity index, decreased colon length, and decreased miR-125a-5p expression (all P  < 0.05). In the DSS-induced mouse model, the expression of miR-125a-5p rebounded and ferroptosis was inhibited after Rh2 treatment (all P  < 0.05). Inhibition of miR-125a-5p or upregulation of SP1 expression counteracted the protective effects of Rh2 on UC mice and ferroptosis cell models (all P  < 0.05). Conclusions Rh2 mitigated DSS-induced colitis in mice and restrained ferroptosis by targeting miR-125a-5p. Downregulating miR-125a-5p or elevating SP1 could counteract the protective impacts of Rh2 on ferroptotic cells. The findings convey that Rh2 has a latent application value in the treatment of UC. Graphical Abstract

研究领域: 药理学 · 分子生物学 · 免疫学 · 胃肠病学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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ACS Omega · 2023 · IF 4.1

Structure Modification of Ginsenoside Rh2 and Cytostatic Activity on Cancer Cells

Junyu Liang,Xiaodong Tang,Shanhe Wan,Jiayin Guo,Peng Zhao,Ling Lu

Ginsenoside Rh2 (Rh2) is one of the most effective anticancer components extracted from red ginseng, but the poor solubility limits its clinical application. In this paper, ginsenoside Rh2 was modified with maleimidocaproic acid or maleimidoundecanoic acid with functional groups at both ends. The structures of derivatives were determined by analysis of 1D and 2D nuclear magnetic resonance, Fourier transform infrared, and high-resolution mass spectrometry. Antiproliferative cell experiments showed that Rh2 modified with maleimidocaproic acid (C–Rh2) displayed higher cytostatic activity against different tumor cells compared with Rh2, while Rh2 modified with maleimidoundecanoic acid (U–Rh2) did not exhibit obvious cytotoxicity. The results suggest that the length of the spacer arm may play an important role in the cytostatic activity of the Rh2 derivatives.

CAS / MDL: 1122-58-3
研究领域: 药理学 · 肿瘤学 · 化学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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BIOMACROMOLECULES · 2017 · IF 5.246

Oral Nanomedicine Based on Multicomponent Microemulsions for Drug-Resistant Breast Cancer Treatment

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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