• Advances in Traditional Medicine
• /
• 제6권4호
• /
• pp.286-292
• /
• 2006

In this study, we evaluated the antiproliferative effects of Panax notoginseng, ginsenoside Rb1, and notoginsenoside R1 in the human breast carcinoma MCF-7 cell line. Our results indicated that both Panax notoginseng radix extract (NRE) and Panax notoginseng rhizoma extract (NRhE) possess significant antiproliferative activities in MCF-7 cells. Compared to control group (100%), at the concentrations of 0.05, 0.5, and 1.0 mg/ml NRE, cell growth was concentration-dependently reduced to 81.0 ${\pm}$ 6.1 (P < 0.01), 34.2 ${\pm}$ 4.8 (P < 0.001), and 19.3 ${\pm}$ 1.9 (P < 0.001), respectively. Similar results with NRhE at concentrations of 0.5 and 1.0 mg/ml were obtained in these MCF-7 cells. To identify the responsible chemical constituent, we tested the antiproliferation effects of two representative saponins, ginsenoside Rb1 and notoginsenoside R1, on the MCF-7 cells. The data showed that ginsenoside Rb1 was endowed with antiproliferative properties, while notoginsenoside R1 did not have an inhibitory effect in the concentrations tested. Our studies provided evidence that Panax notoginseng extracts and ginsenoside Rb1 may be beneficial, as adjuvants, in the treatment of human breast carcinoma.

• Journal of Applied Biological Chemistry
• /
• 제62권4호
• /
• pp.315-322
• /
• 2019

Seasonal ginsenoside flux in the leaves of 5-year-old Panax ginseng was analyzed from the field-grown ginseng, for the first time, to study possible biosynthesis and translocation of ginsenosides. The concentrations of nine major ginsenosides, Rg1, Re, Rh1, Rg2, R-Rh1, Rb1, Rc, Rb2, and Rd, were determined by UHPLC during the growth in between April and November. It was confirmed total ginsenoside content in the dried ginseng leaves was much higher than the roots by several folds whereas the composition of ginsenosides was different from the roots. The ginsenoside flux was affected by ginseng growth. It quickly increased to 10.99±0.15 (dry wt%) in April and dropped to 6.41±0.14% in May. Then, it slowly increased to 9.71±0.14% in August and maintained until October. Ginsenoside Re was most abundant in the leaf of P. ginseng, followed by Rd and Rg1. Ginsenosides Rf and Ro were not detected from the leaf. When compared to the previously reported root data, ginsenosides in the leaf appeared to be translocated to the root, especially in the early vegetative stage even though the metabolite translocated cannot be specified. The flux of ginsenoside R-Rh1 was similar to the other (20S)-PPT ginsenosides. When the compositional changes of each ginsenoside in the leaf was analyzed, complementary relationship was observed from ginsenoside Rg1 and Re, as well as from ginsenoside Rd and Rb1+Rc. Accordingly, ginsenoside Re in the leaf was proposed to be synthesized from ginsenoside Rg1. Similarly, ginsenosides Rb1 and Rc were proposed to be synthesized from Rd.

• Journal of Microbiology and Biotechnology
• /
• 제18권6호
• /
• pp.1081-1089
• /
• 2008

A novel ginsenoside-hydrolyzing ${\beta}$-glucosidase was purified from Paecilomyces Bainier sp. 229 by a combination of Q-Sepharose FF, phenyl-Sepharose CL-4B, and CHT ceramic hydroxyapatite column chromatography. The purified enzyme was a monomeric protein with a molecular mass estimated to be 115 kDa. The optimal enzyme activity was observed at pH 3.5 and $60^{\circ}C$. It was highly stable within pH 3-9 and at temperatures lower than $55^{\circ}C$. The enzyme was specific to ${\beta}$-glucoside. The order of enzyme activities against different types of ${\beta}$-glucosidic linkages was ${\beta}$-(1-6)>${\beta}$-(1-2)>${\beta}$-(1-4). The enzyme converted ginsenoside Rb1 to CK specifically and efficiently. An 84.3% amount of ginsenoside Rb1, with an initial concentration of 2 mM, was converted into CK in 24 h by the enzyme at $45^{\circ}C$ and pH 3.5. The hydrolysis pathway of ginsenoside Rb1 by the enzyme was $Rb1{\to}Rd{\to}F2{\to}CK$. Five tryptic peptide fragments of the enzyme were identified by a newly developed de novo sequencing method of post-source decay (PSD) matrix-assisted laser desorption/ionization (MALDI) mass spectrometry. By comparing the five identified peptide sequences with the NCBI database, this purified ${\beta}$-glucosidase proves to be a new protein that has not been reported before.

• Journal of Ginseng Research
• /
• 제45권2호
• /
• pp.334-343
• /
• 2021

Background: Gut microbiota mainly function in the biotransformation of primary ginsenosides into bioactive metabolites. Herein, we investigated the effects of three prebiotic fibers by targeting gut microbiota on the metabolism of ginsenoside Rb1 in vivo. Methods: Sprague Dawley rats were administered with ginsenoside Rb1 after a two-week prebiotic intervention of fructooligosaccharide, galactooligosaccharide, and fibersol-2, respectively. Pharmacokinetic analysis of ginsenoside Rb1 and its metabolites was performed, whilst the microbial composition and metabolic function of gut microbiota were examined by 16S rRNA gene amplicon and metagenomic shotgun sequencing. Results: The results showed that peak plasma concentration and area under concentration time curve of ginsenoside Rb1 and its intermediate metabolites, ginsenoside Rd, F2, and compound K (CK), in the prebiotic intervention groups were increased at various degrees compared with those in the control group. Gut microbiota dramatically responded to the prebiotic treatment at both taxonomical and functional levels. The abundance of Prevotella, which possesses potential function to hydrolyze ginsenoside Rb1 into CK, was significantly elevated in the three prebiotic groups (P < 0.05). The gut metagenomic analysis also revealed the functional gene enrichment for terpenoid/polyketide metabolism, glycolysis, gluconeogenesis, propanoate metabolism, etc. Conclusion: These findings imply that prebiotics may selectively promote the proliferation of certain bacterial stains with glycoside hydrolysis capacity, thereby, subsequently improving the biotransformation and bioavailability of primary ginsenosides in vivo.

• 한국식품과학회지
• /
• 제37권3호
• /
• pp.508-512
• /
• 2005

고려인삼의 수출확대를 위해서 백삼 및 태극삼의 사포닌(saponin) 함량에 대한 중국 고려인삼 수입의약품 둥록기준 설정의 기초 자료를 얻고자 조사하였다. 백삼 50구의 크기에 따른 초특대편, 특대편, 대편, 중편 및 소편의 ginsenoside-Rg1, -Re 및 -Rb1의 평균 함량은 각각 664.7, 796.9, 674.7, 839.0 및 646.6 mg%이었으며, Rg1/Re의 비율은 각각 1.0, 1.2, 0.8, 1.0 및 1.0의 분포였다. 태극삼 13구의 ginsenoside-Rg1, -Re및 -Rb1의 평균 함량은 755.1 mg%, Rg1/Re의 비율은 1.28이었다. 그리고 백삼 50구의 Rg1 평균값은 $232.7{\pm}110.2 mg%$, Re평균값은 $235.3{\pm}101.5 mg%$, Rb1 평균값은 $280.1{\pm}121.3 mg%$으로 이들의 합은 $748.2{\pm}299.4 mg%$이었으며, Rg1/Re의 비율은 1.02이었다. 또한 태극삼 13구의 사포닌 성분의 분석결과, Rg1 평균값은 $262.1{\pm}127.2 mg%$, Re 평균값은 $213.1{\pm}55.7 mg%$, Rb1 평균값은 $279.9{\pm}92.1 mg%$으로 이들의 합은 $755.1{\pm}233.6 mg%$이었다. 백삼과 태극삼의 사포닌 조성 및 함량은 중국수입의약품 등록기준인 ginsenoside-Rg1, -Re 및 -Rb1 값의 합이 0.4% 이상이라는 기준규격에 적합하였고, HPLC-ELSD로 분석시 인삼의 분석방법별 기준인 ginsenoside -Rg1과 -Re의 함량비($Rg1/Re{\Leq}3.87$)에 부합되었다.

• 한국식품영양과학회지
• /
• 제41권12호
• /
• pp.1753-1757
• /
• 2012

LC-MS/MS를 사용함으로써 인체 혈장에서 ginsenoside Rb1의 분석법을 개발하고 검증하였다. 유속 0.9 mL/min에 이동상 0.1% formic acid가 첨가된 water와 methanol을 사용하여 기울기 용리 조건으로 설정하였으며 사용한 분석 칼럼은 C 18($4.6mm{\times}150mm$, particle size 5 ${\mu}m$)을 사용하여 분리하였다. MRM(multiple reaction monitoring) 방법의 전기 분무 이온화 이온 분석기로 모니터링 하여 분석하였다. 인체 혈장 샘플은 액체-액체 추출방법에 의해 acetone과 water가 섞인 용액으로 추출하였다. 이 분석의 검량선 범위는 10~500 ng/mL이며 상관계수는 0.9995를 나타냈다. 일내, 일간의 정밀성 농도범위는 상관계수 5.8% 그리고 정확성은 96.0~104.6%로 나타났다. 이 LC-MS/MS를 이용한 인체 혈장의 ginsenoside Rb1의 연구가 약동학 연구에 적용할 수 있을 거라 생각한다.

• Journal of Ginseng Research
• /
• 제35권4호
• /
• pp.487-496
• /
• 2011

Good manufacturing practice (GMP)-based quality control is an integral component of the common technical document, a formal documentation process for applying a marketing authorization holder to those countries where ginseng is classified as a medicine. In addition, authentication of the physico-chemical properties of ginsenoside reference materials, and qualitative and quantitative batch analytical data based on validated analytical procedures are prerequisites for certifying GMP. Therefore, the aim of this study was to propose an authentication process for isolated ginsenosides $Rb_1$ and $Rg_1$ as reference materials (RM) and for these compounds to be designated as RMs for ginseng preparations throughout the world. Ginsenoside $Rb_1$ and $Rg_1$ were isolated by Diaion HP-20 adsorption chromatography, silica gel flash chromatography, recrystallization, and preparative HPLC. HPLC fractions corresponding to those two ginsenosides were recrystallized in appropriate solvents for the analysis of physico-chemical properties. Documentation of the isolated ginsenosides was made according to the method proposed by Gaedcke and Steinhoff. The ginsenosides were subjected to analyses of their general characteristics, identification, purity, content quantitation, and mass balance tests. The isolated ginsenosides were proven to be a single compound when analyzed by three different HPLC systems. Also, the water content was found to be 0.940% for $Rb_1$ and 0.485% for $Rg_1$, meaning that the net mass balance for ginsenoside $Rb_1$ and $Rg_1$ were 99.060% and 99.515%, respectively. From these results, we could assess and propose a full spectrum of physicochemical properties for the ginsenosides $Rb_1$ and $Rg_1$ as standard reference materials for GMP-based quality control.

• Journal of Ginseng Research
• /
• 제40권4호
• /
• pp.366-374
• /
• 2016

Background: In this study, we screened and identified an endophyte JG09 having strong biocatalytic activity for ginsenosides from Platycodon grandiflorum, converted ginseng total saponins and ginsenoside monomers, determined the source of minor ginsenosides and the transformation pathways, and calculated the maximum production of minor ginsenosides for the conversion of ginsenoside Rb1 to assess the transformation activity of endophyte JG09. Methods: The transformation of ginseng total saponins and ginsenoside monomers Rb1, Rb2, Rc, Rd, Rg1 into minor ginsenosides F2, C-K and Rh1 using endophyte JG09 isolated by an organizational separation method and Esculin-R2A agar assay, as well as the identification of transformed products via TLC and HPLC, were evaluated. Endophyte JG09 was identified through DNA sequencing and phylogenetic analysis. Results: A total of 32 ${\beta}$-glucosidase-producing endophytes were screened out among the isolated 69 endophytes from P. grandiflorum. An endophyte bacteria JG09 identified as Luteibacter sp. effectively converted protopanaxadiol-type ginsenosides Rb1, Rb2, Rc, Rd into minor ginsenosides F2 and C-K, and converted protopanaxatriol-type ginsenoside Rg1 into minor ginsenoside Rh1. The transformation pathways of major ginsenosides by endophyte JG09 were as follows: $Rb1{\rightarrow}Rd{\rightarrow}F2{\rightarrow}C-K$; $Rb2{\rightarrow}C-O{\rightarrow}C-Y{\rightarrow}C-K$; $Rc{\rightarrow}C-Mc1{\rightarrow}C-Mc{\rightarrow}C-K$; $Rg1{\rightarrow}Rh1$. The maximum production rate of ginsenosides F2 and C-K reached 94.53% and 66.34%, respectively. Conclusion: This is the first report about conversion of major ginsenosides into minor ginsenosides by fermentation with P. grandiflorum endophytes. The results of the study indicate endophyte JG09 would be a potential microbial source for obtaining minor ginsenosides.

• Journal of Ginseng Research
• /
• 제46권2호
• /
• pp.206-213
• /
• 2022

Ginsenoside Rb2 is an active protopanaxadiol-type saponin, widely existing in the stem and leave of ginseng. Rb2 has recently been the focus of studies for pharmaceutical properties. This paper provides an overview of the preclinical and clinical pharmacokinetics for Rb2, which exhibit poor absorption, rapid tissue distribution and slow excretion through urine. Pharmacological studies indicate a beneficial role of Rb2 in the prevention and treatment of diabetes, obesity, tumor, photoaging, virus infection and cardiovascular problems. The underlying mechanism is involved in an inhibition of oxidative stress, ROS generation, inflammation and apoptosis via regulation of various cellular signaling pathways and molecules, including AKT/SHP, MAPK, EGFR/SOX2, TGF-β1/Smad, SIRT1, GPR120/AMPK/HO-1 and NF-κB. This work would provide a new insight into the understanding and application of Rb2. However, its therapeutic effects have not been clinically evaluated. Further studies should be aimed at the clinical treatment of Rb2.

• 한국식품영양학회지
• /
• 제23권3호
• /
• pp.405-410
• /
• 2010

인삼의 저장 가공 방법을 개발하기 위해 마이크로파 단독처리로 수삼을 처리한 후 일반 성분, 색도, 밀도, 사포닌의 조성 및 미세구조 등 품질 특성을 조사하였다. 마이크로웨이브 출력을 100 Watt와 200 Watt에서 각각 1시간과 3시간 동안 수삼을 처리하고 $60^{\circ}C$ 열풍건조기에서 96시간 건조한 후 성분 함량을 측정하였다. 수삼의 초기 수분 함량인 76.26%에서 마이크로파 가열 처리 조건에 따라 13.12~10.77%까지 건조되었다. 마이크로파로 처리한 수삼의 회분 함량은 처리 과정에 따른 차이는 보이지 않았다. 지방의 경우 마이크로파 출력과는 상관없이 처리 시간에 따라 조금씩 감소하였다. 단백질 함량은 마이크로파 가열 후 건조하기 전 수삼의 단백질 함량과 비교하여 큰 차이를 나타내지 않았다. 마이크로파로 처리한 수삼의 총 식이섬유 함량은 대조군보다 증가함을 보이고 있으나, 처리 시간이나 출력과의 유의성은 보이지 않는다. 처리군의 색도는 대조군에 비해 더 어두운 색을 나타내었다. 마이크로파 가열 처리 후 인삼의 색도의 변화는 출력보다 가열 처리 시간에 따라 변하는 양상을 보였다. 마이크로파 가열 처리 후 수삼의 밀도는 감소하는 경향을 보였고, 가열 시간이나 출력에 따른 뚜렷한 차이는 찾을 수 없었다. 사포닌 ginsenoside-$Rb_1$과 $Rb_2+Rb_3$, Rc, Rd, Re, Rf, $Rg_1$, $Rg_2+Rh_1$, $Rg_3$의 함량은 대조군에 비해 감소하는 경향을 보였고, 100 Watt에서 가열한 처리구들보다 200 Watt에서 가열한 처리구들의 함량이 높은 값을 나타냈다. 예외적으로 200 Watt에서 가열했을 때, ginsenoside-$Rb_2+Rb_3$와 ginsenoside-Rc의 함량은 대조군에 비해 증가하였다. 미세구조는 마이크로파 건조 후 더 치밀한 조직이 관찰되었다.