• Nutrition Research and Practice
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• v.16 no.3
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• pp.298-313
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• 2022

BACKGROUND/OBJECTIVES: The effectiveness of natural compounds in improving athletic ability has attracted attention in both sports and research. Gynostemma pentaphyllum (Thunb.) leaves are used to make traditional herbal medicines in Asia. The active components of G. pentaphyllum, dammarane saponins, or gypenosides, possess a range of biological activities. On the other hand, the anti-fatigue effects from G. pentaphyllum extract (GPE) and its effective compound, gypenoside L (GL), remain to be determined. MATERIALS/METHODS: This study examined the effects of GPE on fatigue and exercise performance in ICR mice. GPE was administered orally to mice for 6 weeks, with or without treadmill training. The biochemical analysis in serum, glycogen content, mRNA, and protein expressions of the liver and muscle were analyzed. RESULTS: The ExGPE (exercise with 300 mg/kg body weight/day of GPE) mice decreased the fat mass percentage significantly compared to the ExC mice, while the ExGPE showed the greatest lean mass percentage compared to the ExC group. The administration of GPE improved the exercise endurance and capacity in treadmill-trained mice, increased glucose and triglycerides, and decreased the serum creatine kinase and lactate levels after intensive exercise. The muscle glycogen levels were higher in the ExGPE group than the ExC group. GPE increased the level of mitochondrial biogenesis by enhancing the phosphorylation of peroxisome proliferator-activated receptor-γ coactivator-1α (PGC-1α) protein and the mRNA expression of nuclear respiratory factor 1, mitochondrial DNA, peroxisome proliferator-activated receptor-δ, superoxide dismutase 2, and by decreasing the lactate dehydrogenase B level in the soleus muscle (SOL). GPE also improved PGC-1α activation in the SOL significantly through AMPK/p38 phosphorylation. CONCLUSIONS: These results showed that GPE supplementation enhances exercise performance and has anti-fatigue activity. In addition, the underlying molecular mechanism was elucidated. Therefore, GPE is a promising candidate for developing functional foods and enhancing the exercise capacity and anti-fatigue activity.

• Journal of Ginseng Research
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• v.43 no.3
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• pp.377-384
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• 2019

Background: Inflammation is widespread in the clinical pathology and closely associated to the progress of many diseases. Triterpenoid saponins as a key group of active ingredients in Panax notoginseng (Burk.) F.H. Chen were demonstrated to show antiinflammatory effects. However, the chemical structures of saponins in the leaves and stems of Panax notoginseng (PNLS) are still not fully clear. Herein, the isolation, purification and further evaluation of the antiinflammatory activity of dammarane-type triterpenoid saponins from PNLS were conducted. Methods: Silica gel and reversed-phase C8 column chromatography were used. Furthermore, preparative HPLC was used as a final purification technique to obtain minor saponins with high purities. MS, NMR experiments, and chemical methods were used in the structural identifications. The antiinflammatory activities of the isolated saponins were assessed by measuring the nitric oxide production in RAW 264.7 cells stimulated by lipopolysaccharides. Real-time reverse transcription polymerase chain reaction was used to measure the gene expressions of inflammation-related gene. Results: Eight new minor dammarane-type triterpene oligoglycosides, namely notoginsenosides LK1-LK8 (1-8) were obtained from PNLS, along with seven known ones. Among the isolated saponins, gypenoside IX significantly suppressed the nitric oxide production and inflammatory cytokines including tumor necrosis $factor-{\alpha}$, interleukin 10, interferon-inducible protein 10 and $interleukin-1{\beta}$. Conclusion: The eight saponins may enrich and expand the chemical library of saponins in Panax genus. Moreover, it is reported for the first time that gypenoside IX showed moderate antiinflammatory activity.

• Nutrition Research and Practice
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• v.16 no.1
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• pp.14-32
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• 2022

BACKGROUND/OBJECTIVES: Peroxisome proliferator-activated receptor-gamma co-activator-1α (PGC-1α) has a central role in regulating muscle differentiation and mitochondrial metabolism. PGC-1α stimulates muscle growth and muscle fiber remodeling, concomitantly regulating lactate and lipid metabolism and promoting oxidative metabolism. Gynostemma pentaphyllum (Thumb.) has been widely employed as a traditional herbal medicine and possesses antioxidant, anti-obesity, anti-inflammatory, hypolipemic, hypoglycemic, and anticancer properties. We investigated whether G. pentaphyllum extract (GPE) and its active compound, gypenoside L (GL), affect muscle differentiation and mitochondrial metabolism via activation of the PGC-1α pathway in murine C2C12 myoblast cells. MATERIALS/METHODS: C2C12 cells were treated with GPE and GL, and quantitative reverse transcription polymerase chain reaction and western blot were used to analyze the mRNA and protein expression levels. Myh1 was determined using immunocytochemistry. Mitochondrial reactive oxygen species generation was measured using the 2'7'-dichlorofluorescein diacetate assay. RESULTS: GPE and GL promoted the differentiation of myoblasts into myotubes and elevated mRNA and protein expression levels of Myh1 (type IIx). GPE and GL also significantly increased the mRNA expression levels of the PGC-1α gene (Ppargc1a), lactate metabolism-regulatory genes (Esrra and Mct1), adipocyte-browning gene fibronectin type III domain-containing 5 gene (Fndc5), glycogen synthase gene (Gys), and lipid metabolism gene carnitine palmitoyltransferase 1b gene (Cpt1b). Moreover, GPE and GL induced the phosphorylation of AMP-activated protein kinase, p38, sirtuin1, and deacetylated PGC-1α. We also observed that treatment with GPE and GL significantly stimulated the expression of genes associated with the anti-oxidative stress response, such as Ucp2, Ucp3, Nrf2, and Sod2. CONCLUSIONS: The results indicated that GPE and GL enhance exercise performance by promoting myotube differentiation and mitochondrial metabolism through the upregulation of PGC-1α in C2C12 skeletal muscle.

• Journal of Ginseng Research
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• v.27 no.3
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• pp.135-140
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• 2003

North American ginseng (Panax quinquefolius L.) was analysed for total ginsenosides and ten major ginsenosides (R$_{0}$ , Rb$_1$, Rb$_2$, Rc, Rd, Re, Rf, Rg$_1$, pseudoginsenoside F$_{11}$ and gypenoside XVII), and variations in ginsenoside content with age of plant (over a four-year-period) and geographic location (Ontario versus British Columbia) were investigated. In the roots the total ginsenoside content increased with age up to 58-100 mgㆍg$^{-1}$ dry weights in the fourth year, but in leaves it remained constant over time. Roots and leaves, moreover, had different proportions of individual ginsenosides. The most abundant ginsenosides were Rb$_1$ (56mgㆍg$^{-1}$ for Ontario; 37mgㆍg$^{-1}$ for British Columbia) and Re (21mgㆍg$^{-1}$ for Ontario; 15 mgㆍg$^{-1}$ for British Columbia) in roots, and Rd (28-38 mgㆍg$^{-1}$ ), Re (20-25 mgㆍg$^{-1}$ ), and Rb$_2$ (13-19 mgㆍg$^{-1}$ ) in leaves. Measurable quantities of Rf were found in leaves (0.4-1.8 mgㆍg$^{-1}$ ) but not in roots or stems. Our results show that ginsenoside profiles in general, and Rf in particular, could be used for chemical fingerprinting to distinguish the different parts of the ginseng plant, and that ginseng leaves could be valuable sources of the ginsenosides Rd, Re, and Rb$_2$.

• Natural Product Sciences
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• v.21 no.2
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• pp.111-121
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• 2015

The root of Panax ginseng, is a Korea traditional medicine, which is used in both raw and processed forms due to their different pharmacological activities. As part of a continued chemical investigation of ginseng, the focus of this research is on the isolation and identification of compounds from Panax ginseng root by open column chromatography, medium pressure liquid chromatography, semi-preparative-high performance liquid chromatography, Fast atom bombardment mass spectrometric, and nuclear magnetic resonance. Dammarane-type triterpenoid saponins were isolated from Panax ginseng root by open column chromatography, medium pressure liquid chromatography, and semi-preparative-high performance liquid chromatography. Their structures were identified as protopanaxadiol ginsenosides [gypenoside-V (1), ginsenosides-Rb1 (2), -Rb2 (3), -Rb3 (4), -Rc (5), and -Rd (6)], protopanaxatriol ginsenosides [20(S)-notoginsenoside-R2 (7), notoginsenoside-Rt (8), 20(S)-O-glucoginsenoside-Rf (9), 6-O-[$\alpha$-L-rhamnopyranosyl(1$\rightarrow$2-$\beta$-D-glucopyranosyl]-20-O-$\beta$-D-glucopyranosyl-$3\beta$,$12\beta$, 20(S)-dihydroxy-dammar-25-en-24-one (10), majoroside-F6 (11), pseudoginsenoside-Rt3 (12), ginsenosides-Re (13), -Re5 (14), -Rf (15), -Rg1 (16), -Rg2 (17), and -Rh1 (18), and vinaginsenoside-R15 (19)], and oleanene ginsenosides [calenduloside-B (20) and ginsenoside-Ro (21)] through the interpretation of spectroscopic analysis. The configuration of the sugar linkages in each saponin was established on the basic of chemical and spectroscopic data. Among them, compounds 1, 8, 10, 11, 12, 19, and 20 were isolated for the first time from P. ginseng root.

• Proceedings of the Plant Resources Society of Korea Conference
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• 2008.11a
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• pp.37-51
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• 2008

인삼은 재배적지에 대한 선택성이 매우 강한 식물이며, 기후 토양 등의 자연환경이 적당하지 않으면 인삼의 생육이 곤란하고, 생육이 가능하더라도 생산된 인삼의 형태, 품질 및 약효에서 현저한 차이를 나타내고 있다. 이러한 인삼의 식물학적 특성이 우리나라에서는 최적의 환경조건으로 인정되어 고려인삼은 세계적으로 최고의 품질로 높이 평가되는 이유이다. 하지만 실질적인 인삼의 생리활성물질에 대한 연구는 서구열강 및 일본에 의해 대다수 연구, 발표되었으며 또한 인삼의 우수성을 인정하여 넓은 영토와 수많은 과학적 지식으로 고려인삼의 우수한 품질을 앞서가려 하고 있는 것이 현실정이다. 특히 중국의 넓은 인삼재배면적에서 값싸게 생산된 인삼이 한국시장을 위협하고 있으며, 미국과 캐나다에서 수많은 연구비를 투자하여 자국삼인 화기삼의 홍보를 대대적으로 함으로서 전세계의 인삼시장의 변화를 유도하고 있고, 호주, 뉴질랜드에서도 청정인삼을 내세워 한국 및 전세계 인삼시장을 잠식해가고 있다. 이런 변화에 의하여 한때 인삼의 종주국으로 전세계의 인삼시장을 석권했던 한국의 고려인삼이 과거의 위상을 점차 잃어 가고 있는 실정이다. 따라서 인삼재배면적이 경쟁국과 비교해 상대적으로 열세인 한국의 고려인삼이 선택할수 있는 방법은 비록 생산은 적더라도 고부가가치인삼을 생산하여 명품화로 가야 할 것으로 생각된다. 명품화를 위해서는 우선 고려인삼의 효능을 밝혀 고기능성을 입증해야하고, 재배생산단계에서부터 농약, 중금속등에 노출되지 않고 병에 자유로운 청정재배를 통해 명품화를 이룩해야 하며, 특히 제품의 생산 및 유통단계에서 표준화를 통해서 전세계의 소비자가 믿고 사용할수 있도록 해야 할 것이다. 또한 인삼에만 함유된 인삼사포닌(ginsenoside)은 배당체로서 여러 미생물에 의하여 당사슬이 끊어짐으로서 새로운 사포닌이 등장하게 되는데 이러한 사포닌이 각종 함암, 면적, 치매, 관절등에 탁월한 효능을 보임으서 많은 연구들이 진행중에 있으며, 특히 인삼에만 함유된 것으로 알고 있었던 ginsenoside가 돌외(한약재명 칠엽담)에도 함유되어 있고 일부 성분은 미생물을 통해서 변환시킴으로 서 값비싼 인삼사포닌을 생장이 빠르면 비교적 값싼 돌외 사포닌으로부터 생산할수 있게 되었다. 본 세미나에서는 각종 미생물을 이용하여 인삼의 사포닌을 변환시키고 돌외 사포닌인 gypenoside를 ginsenoside로 변환시켜 대량생산할 수 있는 방법을 제시하고자 한다.

• Journal of Ginseng Research
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• v.36 no.3
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• pp.291-297
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• 2012

Ginsenoside (ginseng saponin), the principal component of ginseng, is responsible for the pharmacological and biological activities of ginseng. We isolated lactic acid bacteria from Kimchi using esculin agar, to produce ${\beta}$-glucosidase. We focused on the bio-transformation of ginsenoside. Phylogenetic analysis was performed by comparing the 16S rRNA sequences. We identified the strain as Lactobacillus (strain 6105). In order to determine the optimal conditions for enzyme activity, the crude enzyme was incubated with 1 mM ginsenoside Rb1 to catalyse the reaction. A carbon substrate, such as cellobiose, lactose, and sucrose, resulted in the highest yields of ${\beta}$-glucosidase activity. Biotransformations of ginsenoside Rb1 were analyzed using TLC and HPLC. Our results confirmed that the microbial enzyme of strain 6105 significantly transformed ginsenoside as follows: Rb1${\rightarrow}$gypenoside XVII, Rd${\rightarrow}$F2 into compound K. Our results indicate that this is the best possible way to obtain specific ginsenosides using microbial enzymes from 6105 culture.

• Journal of Ginseng Research
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• v.40 no.4
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• pp.344-350
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• 2016

Background: Mountain-cultivated ginseng (MCG) and cultivated ginseng (CG) both belong to Panax ginseng and have similar ingredients. However, their pharmacological activities are different due to their significantly different growth environments. Methods: An ultra-performance liquid chromatography/quadrupole time-of-flight mass spectrometry (UPLC-QTOF-MS/MS)-based approach was developed to distinguish MCG and CG. Multivariate statistical methods, such as principal component analysis and supervised orthogonal partial-least-squares discrimination analysis were used to select the influential components. Results: Under optimized UPLC-QTOF-MS/MS conditions, 40 ginsenosides in both MCG and CG were unambiguously identified and tentatively assigned. The results showed that the characteristic components of CG and MCG included ginsenoside Ra3/isomer, gypenoside XVII, quinquenoside R1, ginsenoside Ra7, notoginsenoside Fe, ginsenoside Ra2, ginsenoside Rs6/Rs7, malonyl ginsenoside Rc, malonyl ginsenoside Rb1, malonyl ginsenoside Rb2, palmitoleic acid, and ethyl linoleate. The malony ginsenosides are abundant in CG, but higher levels of the minor ginsenosides were detected in MCG. Conclusion: This is the first time that the differences between CG and MCG have been observed systematically at the chemical level. Our results suggested that using the identified characteristic components as chemical markers to identify different ginseng products is effective and viable.