人参皂苷Rd

人参皂苷Rd用途

Ginsenoside Rd 抑制 TNFα 诱导的 NF-κB 转录活性,IC50 为 12.05±0.82 μM。Ginsenoside Rd 抑制 COX-2 和 iNOS mRNA 的表达。Ginsenoside Rd 还抑制 Ca2+ 内流。Ginsenoside Rd 抑制CYP2D6,CYP1A2,CYP3A4 和 CYP2C9,IC50 分别为 58.0±4.5 μM,78.4±5.3 μM,81.7±2.6 μM 和 85.1±9.1 μM。

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人参皂苷Rd名称

[ CAS 号 ]:
52705-93-8

[ 中文名 ]:
人参皂苷Rd

[ 英文名 ]:
ginsenoside Rd

[中文别名 ]:

人参皂甙 Rd

[英文别名 ]:

GINSENOOSIDERD
ginsenoside Rd
Herba Gynostemmatis Pentaphylli
Gypenoside VIII
GinsenosideRd
EINECS 258-118-5
ginsenoside--Rd standard
MFCD00210508

人参皂苷Rd生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 钙通道

信号通路 >> 代谢酶/蛋白酶 >> 细胞色素P450

研究领域 >> 心血管疾病

研究领域 >> 炎症/免疫

天然产物 >> 萜类化合物和糖苷

[ 靶点 ]

NF-κB:12.05 μM (IC50, in HepG2 cells)

COX-2

L-type calcium channel

CYP2D6:58 μM (IC50)

CYP1A2:78.4 μM (IC50)

CYP3A4:81.7 μM (IC50)

CYP2C9:85.1 μM (IC50)

[体外研究]

人参皂苷(Ginsenoside Rd)是人参最丰富的成分之一。人参皂甙Rd显着抑制TNF-α诱导的NF-κB转录活性,HepG2细胞的IC50为12.05±0.82。人参皂甙Rd还以剂量依赖性方式抑制COX-2和iNOS mRNA以及iNOS启动子活性的表达。为了确定无毒浓度,用各种浓度(0.1,1和10μM)的化合物(例如,人参皂甙Rd)处理HepG2细胞,并使用MTS测定法测量细胞活力。没有化合物在高达10μM时具有显着的细胞毒性,表明NF-κB抑制不是由细胞毒性引起的[1]。人参皂苷Rd是人参中最丰富的成分之一,通过多种机制保护心脏,包括抑制Ca2 +内流。人参皂甙Rd以浓度依赖性方式降低ICa,L峰值振幅(IC50 = 32.4±7.1μM)[2]。人参皂苷Rd对人肝微粒体中CYP2D6的活性具有抑制作用,IC50为58.0±4.5μM,对人肝微粒体中CYP1A2,CYP3A4和CYP2C9活性的抑制作用较弱,IC50分别为78.4±5.3,81.7±2.6分别为85.1±9.1,对人肝微粒体中CYP2A6活性的抑制作用更弱,IC50值大于100μM[4]。

[体内研究]

Ginsenosides Rd是从绞股蓝中分离出的主要化合物,可在整体上改善肠道微环境并诱导ApcMin/+小鼠的抗息肉病。在肠息肉出现之前,对6周龄小鼠进行人参皂苷Rd处理。监测所有小鼠的食物摄入量,耗水量和体重变化。在整个实验中,未观察到小鼠中Rb3 /人参皂苷Rd相关的体重减轻。此外,没有一只处理过的小鼠表现出食物和水消耗的变化。然而,人参皂甙Rd处理有效地减少了息肉的数量和大小[3]。

[细胞实验]

MTS测定用于分析化合物对细胞活力的影响。将HepG2细胞在96孔板（1×10 4细胞/孔）中培养过夜。在添加化合物（例如，人参皂苷Rd; 0.1,1和10μM）24小时后评估细胞活力。在加入MTS 30分钟后，活细胞数由溶解的甲product产物的A490nm确定[1]。

[动物实验]

小鼠[3]使用杂合雄性ApcMin / +（C57BL / 6J-ApcMin / +）小鼠。将总共32只雄性ApcMin / +小鼠（6周龄）分成三组;对照组中的10只小鼠和22只小鼠等分为Rb3和Rd处理。每天用20mg / kg的单剂量人参皂甙Rb3或人参皂甙Rd或溶剂对照管饲。治疗连续进行8周。

[参考文献]

[1]. Song SB, et al. Inhibition of TNF-α-mediated NF-κB Transcriptional Activity in HepG2 Cells by Dammarane-type Saponins from Panax ginseng Leaves. J Ginseng Res. 2012 Apr;36(2):146-52.

[2]. Lu C, et al. Inhibition of L-type Ca²⁺ current by ginsenoside Rd in rat ventricular myocytes. J Ginseng Res. 2015 Apr;39(2):169-77.

[3]. Huang G, et al. Ginsenosides Rb3 and Rd reduce polyps formation while reinstate the dysbiotic gut microbiota and the intestinal microenvironment in Apc^Min/+ mice. Sci Rep. 2017 Oct 2;7(1):12552.

[4]. Liu Y, et al. Ginsenoside metabolites, rather than naturally occurring ginsenosides, lead to inhibition of human cytochrome P450 enzymes. Toxicol Sci. 2006 Jun;91(2):356-64.

[相关活性小分子]

人参皂苷Rd物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 沸点 ]:
1015.6±65.0 °C at 760 mmHg

[ 熔点 ]:
207 °C(dec.)

[ 分子式 ]:
C₄₈H₈₂O₁₈

[ 分子量 ]:
947.154

[ 闪点 ]:
568.0±34.3 °C

[ 精确质量 ]:
946.550110

[ PSA ]:
298.14000

[ LogP ]:
3.24

[ 外观性状 ]:
固体;White to Almost white powder to crystal

[ 蒸汽压 ]:
0.0±0.6 mmHg at 25°C

[ 折射率 ]:
1.611

[ 储存条件 ]:
2-8°C

人参皂苷RdMSDS

详细MSDS(安全技术说明书)

人参皂苷Rd毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: LZ5858000

CHEMICAL NAME :: beta-D-Glucopyranoside, (3-beta,12-beta)-20-(beta-D-glucopyranosyloxy)-12-hyd roxydammar-24- en-3-yl 2-O-beta-D-glucopyranosyl-

CAS REGISTRY NUMBER :: 52705-93-8

LAST UPDATED :: 199312

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C48-H82-O18

MOLECULAR WEIGHT :: 947.30

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 324 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 25,343,1975

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人参皂苷Rd安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
R22

[ 安全声明 (欧洲) ]:
S2-S45

[ 危险品运输编码 ]:
NONH for all modes of transport

人参皂苷Rd合成路线

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人参皂苷Rd文献

Transcriptome analysis of Panax vietnamensis var. fuscidicus discovers putative ocotillol-type ginsenosides biosynthesis genes and genetic markers.

BMC Genomics 16 , 159, (2015)

P. vietnamensis var. fuscidiscus, called "Yesanqi" in Chinese, is a new variety of P. vietnamensis, which was first found in Jinping County, the southern part of Yunnan Province, China. Compared with ...

Protective effects of ginsenoside Rd on PC12 cells against hydrogen peroxide.

Biol. Pharm. Bull. 31(10) , 1923-7, (2008)

Oxidative stress-induced cell damage has been implicated in a variety of neurodegenerative disorders. In the current study, we investigated the protective role of ginsenoside Rd against the cytotoxici...

Bioconversion of ginsenoside Rc into Rd by a novel α-L-arabinofuranosidase, Abf22-3 from Leuconostoc sp. 22-3: cloning, expression, and enzyme characterization.

Antonie van Leeuwenhoek 103(4) , 747-54, (2013)

A novel α-L-arabinofuranosidase (Abf22-3) that could biotransform ginsenoside Rc into Rd was obtained from the ginsenoside converting Leuconostoc sp. strain 22-3, isolated from the Korean fermented fo...

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