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Effects of ginsenoside Rh2 on growth and migration of pancreatic cancer cells  [cached]
Xi-Ping Tang,Guo-Du Tang,Chun-Yun Fang,Zhi-Hai Liang
World Journal of Gastroenterology , 2013, DOI: 10.3748/wjg.v19.i10.1582
Abstract: AIM: To investigate the effects of ginsenoside Rh2 on the human pancreatic cancer cell line Bxpc-3. METHODS: The human pancreatic cancer cell line Bxpc-3 was cultured in vitro and treated with or without ginsenoside Rh2. Growth rates for Bxpc-3 cells were assessed by methyl thiazolyl tetrazolium (MTT) and colony formation assays. Cell cycle changes were analyzed by flow cytometry. Apoptosis was measured by flow cytometry and Hoechst 33258 fluorescence staining. A scratch assay and a Matrigel invasion assay were used to detect cell migration and invasion. Expression of Bax, Bcl-2, survivin, cyclin D1, matrix metalloproteinase (MMP)-2, MMP-9, cleaved caspase-3, caspase-8, and caspase-9 mRNA were determined by reverse transcriptase-polymerase chain reaction (RT-PCR). Bax, Bcl-2, survivin, cyclin D1, cleaved caspase-3, caspase-8 and caspase-9 protein levels were examined by western blotting. Expression of MMP-2 and MMP-9 proteins in culture supernatants were determined by enzyme-linked immunosorbent assay (ELISA). RESULTS: Rh2 significantly inhibited Bxpc-3 cell proliferation in a dose- and time-dependent manner, as evaluated by the MTT (P < 0.05) and colony formation assays (P < 0.05). Compared to the control group, Rh2 significantly increased the percentage of Bxpc-3 cells in the G0/G1 phase from 43.32% ± 2.17% to 71.32% ± 1.16%, which was accompanied by a decrease in S phase (from 50.86% ± 1.29% to 28.48% ± 1.18%) and G2/M phase (from 5.81% ± 1.19% to 0.20% ± 0.05%) in a dose-dependent manner (P < 0.05), suggesting that Rh2 arrested cell cycle progression at the G0/G1 phase, as measured by flow cytometry. Compared to the control group, cells treated with Rh2 showed significantly higher apoptosis ratios in a dose-dependent manner (percentage of early apoptotic cells: from 5.29% ± 2.28% to 38.90% ± 3.42% (F = 56.20, P < 0.05); percentage of late apoptotic cells: from 4.58% ± 1.42% to 36.32% ± 2.73% (F = 86.70, P < 0.05). Rh2 inhibited Bxpc-3 cell migration and invasion, as detected by scratch wound healing assay and Matrigel invasion assay [percentages of scratch wound healing for 12 h, 24 h and 48 h (control vs experimental group): 37.3% ± 4.8% vs 18.30% ± 1.65%, 58.7% ± 3.5% vs 38.00% ± 4.09% and 93.83% ± 4.65% vs 65.50% ± 4.09%, respectively; t = 6.489, t = 6.656 and t = 7.926, respectively, P < 0.05; the number of cells invading at various concentrations (0 μmol/L, 35 μmol/L, 45 μmol/L and 55 μmol/L): 81.10 ± 9.55, 46.40 ± 6.95, 24.70 ± 6.88 and 8.70 ± 3.34, respectively (F = 502.713, P < 0.05)]. RT-PCR, western blotting or ELISA showed that mRNA and p
Stereoselective Regulations of P-Glycoprotein by Ginsenoside Rh2 Epimers and the Potential Mechanisms From the View of Pharmacokinetics  [PDF]
Jingwei Zhang, Fang Zhou, Fang Niu, Meng Lu, Xiaolan Wu, Jianguo Sun, Guangji Wang
PLOS ONE , 2012, DOI: 10.1371/journal.pone.0035768
Abstract: Chirality is an interesting topic and it is meaningful to explore the interactions between chiral small molecules and stereoselective biomacromolecules, with pre-clinical and clinical significances. We have previously demonstrated that 20(S)-ginsenoside Rh2 is an effective P-glycoprotein (P-gp) inhibitor in vitro and in vivo. Considering the stereochemistry of ginsenoside Rh2, in our present study, the regulatory effects of 20(R)-Rh2 on P-gp were assayed in vivo, and the differential regulations of P-gp by ginsenoside Rh2 epimers in vivo were compared and studied. Results showed that 20(S)-Rh2 enhanced the oral absorption of digoxin in rats in a dose-dependent manner; 20(R)-Rh2 at low dosage increased the oral absorption of digoxin, but this effect diminished with elevated dosage of 20(R)-Rh2. Further studies indicated stereoselective pharmacokinetic profiles and intestinal biotransformations of Rh2 epimers. In vitro studies showed that Rh2 epimers and their corresponding deglycosylation metabolites protopanaxadiol (Ppd) epimers all exhibited stereoselective regulations of P-gp. In conclusion, in view of the in vitro and in vivo dispositions of Rh2 and the regulations of P-gp by Rh2 and Ppd, it is suggested that the P-gp regulatory effect of Rh2 in vivo actually is a double actions of both Rh2 and Ppd, and the net effect is determined by the relative balance between Rh2 and Ppd with the same configuration. Our study provides new evidence of the chiral characteristics of P-gp, and is helpful to elucidate the stereoselective P-gp regulation mechanisms of ginsenoside Rh2 epimers in vivo from a pharmacokinetic view.
Cardioprotective Effects of 20(S)-Ginsenoside Rh2 against Doxorubicin-Induced Cardiotoxicity In Vitro and In Vivo
Hongbo Wang,Pengfei Yu,Haitao Gou,Jianqiao Zhang,Mei Zhu,Zhen-hua Wang,Jing-wei Tian,Yong-tao Jiang,Feng-hua Fu
Evidence-Based Complementary and Alternative Medicine , 2012, DOI: 10.1155/2012/506214
Abstract: Doxorubicin (DOX) is considered as one of the best antineoplastic agents. However, its clinical use is restricted by its associated cardiotoxicity, which is mediated by the production of reactive oxygen species. In this study, 20(S)-ginsenoside Rh2 (Rh2) was explored whether it had protective effects against DOX-induced cardiotoxicity. In vitro study on H9C2 cell line, as well as in vivo investigation in one mouse and one rat model of DOX-induced cardiomyopathy, was carried out. The results showed that pretreatment with Rh2 significantly increased the viability of DOX-injured H9C2 cells. In the mouse model, Rh2 could suppress the DOX-induced release of the cardiac enzymes into serum and improved the occurred pathological changes through ameliorating the decreased antioxidant biomolecules and the cumulated lipid peroxidation malondialdehyde in heart tissues. In the rat model, Rh2 could attenuate the change of ECG resulting from DOX administration. Furthermore, Rh2 enhanced the antitumor activity of DOX in A549 cells. Our findings thus demonstrated that Rh2 pretreatment could effectively alleviate heart injury induced by DOX, and Rh2 might act as a novel protective agent in the clinical usefulness of DOX.
Study on Inhibitory Effect of Ginsenoside Rh2 on Cariogenic Bacteria Biofilms

Cao Xi-xi
, Ye Qian-lin, Zhou Li-bo, Fan Ming-wen, Liu Chang

- , 2018, DOI: 10.13701/j.cnki.kqyxyj.2018.12.010
Abstract: 摘要 目的: 通过体内外实验探究人参皂苷Rh2对致龋生物膜的作用。方法: 运用结晶紫染色法和激光共聚焦扫描显微镜观察Rh2对体外生物膜的影响。建立大鼠龋齿模型,取颌骨进行显微断层扫描,Keyes龋齿计分,评价Rh2的抗龋作用。结果: 体外实验结果表明Rh2能明显抑制生物膜上致龋菌生长,减少胞外基质。动物实验中,Rh2组磨牙体积和窝沟区域矿物密度大于对照组(P<0.05)。Rh2组磨牙龋齿计分都低于对照组(P<0.05)。结论: Rh2能在体外抑制致龋生物膜形成,体内有一定的抗龋保护能力
Advances in Ginsenoside Rh2 and Its Derivatives
人参皂苷Rh2 及其衍生物的研究进展

Cao Man,Zhang Jie,Zhao Yang,Song Xinbo,Ma Baiping,

世界科学技术-中医药现代化 , 2012,
Abstract: 人参皂苷Rh2是红参中特征性成分之一,也是一种生物活性较高的稀有皂苷。近年来,人参皂苷Rh2的制备研究由酸水解法、碱水解法、合成法逐渐转到生物转化法,微生物及酶转化法以其独特优势成为制备人参皂苷Rh2的理想方法;人参皂苷Rh2及其衍生物的生物活性、药代动力学等也均有较多研究。本文对人参皂苷Rh2及其衍生物的制备、药理活性等方面进行综述,为该化合物深入研究开发提供参考。
Microbial conversion of major ginsenoside Rb1 to minor ginsenoside Rd by Indian fermented food bacteria
K Senthil, V Veena, M Mahalakshmi, R Pulla, DC Yang, R Parvatham
African Journal of Biotechnology , 2009,
Abstract: Ginsenoside Rb1 is the predominant secondary metabolite (saponin) in Panax ginseng. Hydrolysis of the sugar residues in Rb1 yields more pharmaceutically active ginsenosides like Rd, Rg3, F2, Rh2 and C-K. Among them, the minor ginsenoside Rd enhances the differentiation of neural stem cells, protects neurons from neurotoxic chemicals, decreases urea nitrogen and creatinine in kidney. It also protects the kidney from apoptosis and DNA fragmentation caused by cancer and chemical drugs and is more useful therapeutically than the major ginsenoside Rb1. Bacteria showing b-glucosidase activity were isolated from fermented Indian food using esculin-MRS agar. Bacteria from Amla in sugar syrup and Boiled Amla in jaggery syrup converted ginsenoside Rb1 to minor ginsenoside Rd. TLC and HPLC analysis showed that with increase in incubation time the conversion of Rb1 to Rd also increased. The 16s rDNA sequence was determined and the bacteria showed 93% sequence similarity to Brumimicrobium mesophilum.
Isolation, Synthesis and Structures of Ginsenoside Derivatives and Their Anti-Tumor Bioactivity  [PDF]
Mei Han,Jin-Gang Hou,Cheng-Ming Dong,Wei Li,Hao-Lun Yu,Yi-Nan Zheng,Li Chen
Molecules , 2010, DOI: 10.3390/molecules15010399
Abstract: Protopanaxatriol saponins obtained with AB-8 macroporous resin mainly consisted of ginsenosides Rg1 and Re. A novel mono-ester of ginsenoside-Rh1 (ginsenoside-ORh1) was synthesized through further enzymatic hydrolysis and octanoyl chloride modifications. A 53% yield was obtained by a facile synthetic method. The structures were identified on the basis of 1D-NMR and 2D-NMR, as well as ESI-TOF-MS mass spectroscopic analyses. The isolated and synthetic compounds were applied in an anti-tumor bioassay, in which ginsenoside ORh1 showed moderate effects on Murine H22 Hepatoma Cells.
Fungal biotransformation of ginsenoside Rg3

Xiuli Wu,Yan Wang,Wenqian Zhao,Yixuan Zhang,

微生物学报 , 2008,
Abstract: Objective] Ginsenosides are important bioactive compounds in Ginseng. Sugar chains of ginsenosides are closely related to the bioactivity. Rare ginsenosides can be achieved by modifying sugar chains through biotransformation . Samples of Ginseng root soils, collected from Changbai Mountain, were used to screen active microorganism which can transform total ginsenosides and single ginsenoside, so as to obtain anti-tumor components. Methods] The strains were isolated and screened on solid transfer medium and yield transfer process for active strains. Then the active strains were tested for their biotransformation properties by using different purified ginsenosides, including ginsenoside Rg3. The biotransformation products were separated and purified through column chromatography on silica gel (300mesh), and identified by spectral analysis and physical constants. Simultaneously, the active strain was identified based on morphological characteristics of colonies, conidium and conidiophore, as well as ITS-5.8S rDNA sequences. Results] Total 68 fungal strains were isolated and 12 active strains showed positive activity on total ginsenosides. One strain, SYP2353, was found to have the strong activity on Rg3. Conclusion] The active strain SYP2353 was identified as Myrothecium verrucaria, and the bio-transformation products of Rg3 were identified to be rare ginsenoside Rh2 and aglycon PPD.
S型与R型人参皂苷Rh2对人肺腺癌A549细胞增殖和凋亡的影响  [PDF]
中国中药杂志 , 2011,
Abstract: 目的:探讨人参皂苷Rh2(S型与R型)对人肺腺癌A549细胞增殖和凋亡的影响,以阐述人参活性成分抗肿瘤活性的构效关系及可能机制。方法:采用MTT实验测定细胞增殖;碘化丙啶(PI)单染流式细胞仪分析细胞周期中各时期的细胞百分数,观察人参皂苷Rh2对人肺腺癌A549细胞增殖周期的影响。AnnexinⅤ-PI双染流式细胞术检测细胞凋亡,采用免疫荧光实验对作为细胞凋亡标志的Caspase-3活性进行测定。结果:人参皂苷Rh2对人肺腺癌A549细胞毒活性明显存在构效关系,其中25mg·L-1的20(R)-人参皂苷Rh2和20(S)-人参皂苷Rh2作用48h对肿瘤细胞株A549的增殖抑制率分别为28.5%,33.6%,IC50值分别为33.4,28.5mg·L-1。20mg·L-1的20(S)-人参皂苷Rh2作用A549细胞24h后G0/G1期细胞比例显著高于对照组(P<0.01),S期细胞比例显著低于对照组(P<0.01),G2/M期细胞比例与对照组比较无显著性差异,说明20(S)-人参皂苷Rh2能阻滞细胞周期于G1期。30mg·L-1的S型和R型人参皂苷Rh2作用A549细胞24h后,无论是早期还是晚期凋亡率均明显高于正常组细胞(P<0.05),并且20(S)-人参皂苷Rh2组早期凋亡率明显高于20(R)-人参皂苷Rh2组,表现出明显的构效效应(P<0.05)。20(R)-人参皂苷Rh2和20(S)-人参皂苷Rh2作用6h的A549细胞中标记Caspase-3活性的荧光亮度明显增强,说明Caspase-3的激活参与了人参皂苷Rh2诱导的A549细胞凋亡。结论:S型和R型人参皂苷Rh2均可剂量依赖性地抑制A549细胞增殖,并且20(S)-人参皂苷Rh2的抗肿瘤活性明显强于20(R)-人参皂苷Rh2,阻滞细胞周期于G1期,具有构效效应;S型和R型人参皂苷Rh2均具有促进A549细胞凋亡作用,并且20(S)-人参皂苷Rh2组早期凋亡率明显高于20(R)-人参皂苷Rh2组,具有构效效应。
Biotransformation of ginsenosides Rb1, Rg3 and Rh2 in rat gastrointestinal tracts
Tianxiu Qian, Zongwei Cai
Chinese Medicine , 2010, DOI: 10.1186/1749-8546-5-19
Abstract: High performance liquid chromatography-mass spectrometry (LC-MS) and tandem mass spectrometry (MS-MS) techniques, particularly liquid chromatography electrospray ionization mass spectrometry (LC-ESI-MS), were used to identify the metabolites.Six metabolites of Rb1, six metabolites of Rg3 and three metabolites of Rh2 were detected in the feces samples of the rats. Rh2 was a metabolite of Rb1 and Rg3, whereas Rg3 was a metabolite of Rb1. Some metabolites such as protopanaxadiol and monooxygenated protopanaxadiol are metabolites of all three ginsenosides.Oxygenation and deglycosylation are two major metabolic pathways of the ginsenosides in rat gastrointestinal tracts.Panax ginseng (Renshen) is used in Chinese medicines to treat various conditions such as debility, ageing, stress, diabetes, insomnia and sexual inadequacy [1-3]. The major bioactive components of P. ginseng are O-glycosides of the triterpen dammarane saponins known as ginsenosides [4,5] which exhibit properties such as anti-inflammation and anti-tumor [6-8]. Over 80 ginsenosides have been isolated from P. ginseng [9]. Rb1, Rg3 and Rh2 are three major ginsenosides with various bioactivities.Rb1, which is the most abundant (0.22-0.62%) among all ginsenosides [5], protects against free radical damage, maintains normal cholesterol and blood pressure [10] and inhibits the induction phase of long-term potentiation by high frequency stimulation in the dentate gyrus of the brain [11]. Rb1 also rescues hippocampal neurons from lethal ischemic damage [12] and delays neuronal death from transient forebrain ischemia in vitro [13]. Rg3 is used as the major active component in an anti-tumor and anti-cancer drug in China [14]. The cytotoxicity of ginsenoside Rg3 against tumor cells increases when Rg3 is metabolized into Rh2 or protopanaxadiol [15]. The metabolic transformation of Rg3 into protopanaxadiol also increases the activity against Helicobacter pylori. Recently, in vitro biotransformation of ginsenosides was re
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