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Ginsenoside F2 is a protopanaxadiol saponin compound with various biological activities, including antioxidant, anti-inflammatory, and anticancer properties. Ginsenoside F2 can be found in ginseng, but in low quantities. Therefore, ginsenoside F2 production predominantly relies on the biotransformation of various ginsenosides, such as ginsenosides Rb1 and Rd. In this study, we reported the production of ginsenoside F2 by gypenoside biotransformation with Aspergillus niger JGL8, isolated from Gynostemma pentaphyllum. Ginsenoside F2 could be produced by two different biotransformation pathways, namely Gyp-V–Rd–F2 and Gyp-XVII–F2. The product exhibited antioxidant activity against free radicals (DPPH) with IC50 value of 29.54 µg/mL. Optimal biotransformation conditions were a pH of 5.0, temperature of 40 °C, and 2 mg/mL of substrate. Enzyme kinetic parameters revealed that the hydrolysis rate of Gyp-V, Rd, and Gyp-XVII was 0.625, 0.588, and 0.417 mM/h, respectively. In conclusion, we demonstrated that gypenoside is a substitutable substrate for ginsenoside F2 biotransformation. [ABSTRACT FROM AUTHOR] more...

Protein tyrosine phosphatase 1B (PTP1B) is a key factor and regulator of glucose, lipid metabolism throughout the body, and a promising target for treatment of type 2 diabetes mellitus (T2DM). Gynostemma pentaphyllum is a famous oriental traditional medicinal herbal plant and functional food, which has shown many beneficial effects on glucose and lipid metabolism. The aim of the present study is to assess the inhibitory activity of five new and four known dammarane triterpenoids isolated from the hydrolysate product of total G. pentaphyllum saponins. The bioassay data showed that all the compounds exhibited significant inhibitory activity against PTP1B. The structure-activity relationship showed that the strength of PTP1B inhibitory activity was mainly related to the electron-donating group on its side chain. Molecular docking analysis suggested that its mechanism may be due to the formation of competitive hydrogen bonding between the electron-donating moiety and the Asp48 amino acid residues on the PTP1B protein. [ABSTRACT FROM AUTHOR] more...

Gynostemma pentaphylla, one of the traditional Chinese medicinal materials, which has gradually become a research hotspot due to its rich pharmacological activities such as hypolipidemic properties, anti-inflammatory, anti-cancer and etc. The main active ingredients of Gynostemma pentaphyllum are saponins (gypenoside), flavonoids and polysaccharides. The pharmacologically active dose depends on the content of the active ingredient, so it is necessary to establish a reliable quality evaluation standard for Gynostemma pentaphyllum. However, the existing Gynostemma pentaphyllum quality control methods are not perfect, Ginsenoside Rb1 was regarded as a signature ingredient of Gynostemma pentaphylla in local standards. Surprisingly, the high-performance liquid chromatogram results displayed that the content of Ginsenoside Rb1 was not suitable as a quality marker. Therefore, a triple quadrupole time-of-flight tandem mass spectrometer method was developed to explore other potential quality markers in Gynostemma pentaphylla. As a result, a total of 24 compounds was identified tentatively. While another stable and reliable component Gypenoside XLVI was found and the content was carried out. It was expected to replace Ginsenoside Rb1 to establish a more reliable and precise quality standard of Gynostemma pentaphylla. [ABSTRACT FROM AUTHOR] more...

Gynostemma pentaphyllum belongs to the family Cucurbitaceae which is native to China where it is also termed an immortal herb. It is an emerging herb gaining fame for its rich phytochemistry. It is loaded with superior phytochemicals with immense therapeutic potential. The key phytochemicals include saponins and sterols. Saponins are a wide class of bioactive found in Gynostemma pentaphyllum and 100 different saponins have been reported to date by different researchers in this herb. Several sterols have been demonstrated in this plant including ergostanol, sitosterol and stigmasterol. All these bioactive substances possess superior therapeutic and pharmacological properties that have been investigated in different studies as presented in this comprehensive review. Taxonomic classification, botanical description, and geographical distribution are briefly covered in the first section of this review. In contrast, the phytochemistry, therapeutic properties, and pharmacological features of Gynostemma pentaphyllum are thoroughly explained in the second section. [ABSTRACT FROM AUTHOR] more...

Jiaosu is a healthy food that has received increasing attention in recent years, while it mainly uses fruits as raw materials. In order to explore the feasibility of using Chinese medicinal plants to make Jiaosu, the study took Houttuynia cordata and Gynostemma pentaphyllum as examples to make Jiaosu products, and measured the main components and antioxidant capacity. The results showed that the color of the Jiaosu was dark yellow and the pH was acidic. Jiaosu products were rich in total protein, total sugar, vitamin E, and total0 phenols, of which total protein content was the highest. At the same time, Jiaosu products had strong antioxidant capacity. Enriching the form of healthy food is of great significance for maintaining human health in the post-epidemic era and the ageing era. [ABSTRACT FROM AUTHOR] more...

Heat-processed Gynostemma pentaphyllum has shown strong activity against human lung carcinoma A549 cells. In this study, two dammarane-type saponins together with two known compounds were isolated from the ethanol extract of the heat-processed leaves of G. pentaphyllum. They were identified as 2α,3β,12β-trihydroxydammar-20(22),24-diene-3-O-β-D-glucopyranoside (1, namely damulin E), 2α,3β,12β-trihydroxydammar-20,24-diene-3-O-β-D-glucopyranoside (2, namely damulin F), damulin A (3) and damulin B (4), respectively, using NMR and mass spectra. Damulin E and damulin F showed moderate activity against A549, H1299, T24, SH-SY5Y and K562 cell lines in vitro using CCK-8 assay. [ABSTRACT FROM AUTHOR] more...

Polysaccharide from Gynostemma pentaphyllum Makino (GPP) could prevent H22 tumour growth and have immunostimulatory in mice, but the mechanism is largely unknown. In this study, we further investigated whether GPP prevents tumour growth by inducing cytotoxicity to the tumour cells or enhancing immunity in H22 ascites tumour-bearing mice. The results showed that GPP prevented the H22 ascites tumour growth in vivo, but showed little effect on cell viability and cycles to H22 cells in vitro. GPP improved the proportion and mitochondrial level of T cells, and promoted the secretion of IL-2 and IFN-γ in the ascites of the mice. Furthermore, GPP in vitro enhanced the cell viability and promoted activation (in particular T cells), proliferation, and the secretion of IL-2 and IFN-γ of lymphocyte. Taken together, our results demonstrated that GPP prevents H22 ascites tumour growth by enhancing immunity rather than cytotoxicity in mice. [ABSTRACT FROM AUTHOR] more...

Gypensapogenin H (Gyp H) is a novel dammarane-type triterpene, isolated from hydrolyzate of total saponins from Gynostemma pentaphyllum. Our previous work demonstrated that Gyp H exhibited potent growth inhibitory effects on tumor cells. It significantly inhibited the growth of human breast cancer cells (MDA-MB-231), while having low toxicity to normal human breast epithelial cells, MCF-10a. Further mechanistic study demonstrated that Gyp H decreased survival, inhibited proliferation, migration, induced apoptosis and led to cell cycle arrest. For the MDA-MB-231 cell lines, Gyp H increased expression of P21, Bax and cytochrome c, induced PARP cleavage and activated caspases. Gyp H also reduced expression of CDK2/4, CyclinD1, E2F1 and Bcl2, which associated with the cell cycle arrest. Thus, our finding may be useful for understanding the mechanism of action of Gyp H on breast cancer cells and suggest that Gyp H would be a leading agent for the treatment of breast cancer. [ABSTRACT FROM AUTHOR] more...

Gynostemma pentaphyllum has gained increasing interest in recent years for its widespread use as a medicinal plant, dietary supplement, herbal tea, and vegetable in China. This herb possesses many beneficial functions, such as anti-tumor, anti-inflammatory, cholesterol lowering, strengthening of the immune system, and blood pressure regulating activities. However, due to an absence of information, the major material components of Gynostemma pentaphyllum remain unknown. A method for the comprehensive profiling of components in Gynostemma pentaphyllum is reported using high performance liquid chromatography – electrospray ionization – quadrupole time-of-flight tandem mass spectrometry (HPLC-ESI-QTOF-MS/MS) in this study. As a result, a total of 36 compounds including flavonoid glycosides and gypenosides were characterized or tentatively identified. Four gypenosides were tentatively identified as potentially new compounds in Gynostemma pentaphyllum. These results provided a reference for comprehensive characterization of ingredients in Gynostemma pentaphyllum and are significant for the utilization of Gynostemma pentaphyllum. [ABSTRACT FROM AUTHOR] more...

Three novel dammarane-type saponins, 2α,3β,12β,20(S),24(S)-pentahydroxydammar-25-ene-3-O-β-D-glucopyranosyl-(1→2)-β-D-glucopyranosyl-20-O-β-D-glucopyranoside (1, namely gypenoside J1), 2α,3β,12β,20(S),25-pentahydroxydammar-23-ene-3-O-β-D-glucopyranosyl-(1→2)-β-D-glucopyranosyl-20-O-β-D-glucopyranoside (2, namely gypenoside J2) and 2α,3β,12β,20(S)-tetrahydroxydammar-25-en-24-one-3-O-β-D-glucopyranosyl-(1→2)-β-D-glucopyranosyl-20-O-β-D-xylopyranosyl-(1→6)-β-D-glucopyranoside (3, namely gypenoside J3) along with one known gypenoside (gypenoside LVII) were isolated from the aerial parts of G. pentaphyllum using various chromatographic methods. Their structures were elucidated on the basis of IR, 1D- (1H and 13C), 2D-NMR spectroscopy (HSQC, HMBC and COSY), and mass spectrometry (ESI-MS/MS). Their activity was tested using CCK-8 assay. These four compounds showed little anti-cancer activity with IC50 values more than 100 μM against four types of human cancer lines. The effects of them against H2O2-induced oxidative stress in human neuroblastoma SH-SY5Y cells were evaluated and they all showed potential neuroprotective effects with 3.64–18.16% higher cell viability than the H2O2-induced model group. [ABSTRACT FROM AUTHOR] more...

Phytochemical investigation of hydrolysate of total G. pentaphyllum saponins led to the isolation of four novel triterpenes, Gypensapogenin U (1), Gypensapogenin V (2), Gypensapogenin W (3) and Gypensapogenin X (4). The structures of these compounds were identified by 1D, 2D-NMR and HR-ESI-MS evidences. Additionally, the protective activity of these new compounds against cardiomyocytes injury induced by H2O2 and their cytotoxic activity against t-HSC/Cl-6 cells were evaluated. [ABSTRACT FROM AUTHOR] more...

Gynostemma pentaphyllum, a traditional herbal tea, and its flavonoids possess antioxidant activities. This study was carried out to isolate and identify these flavonoids from G. pentaphyllum and determinate the contents of the main flavonoids and their antioxidant activities. Nine flavonoids were determinated rapidly from G. pentaphyllum using medium-pressure liquid chromatography combined with other simple chromatographic methods. And nine flavonoids were identified as rutin (1), 4′-O-methyl-kaempferol-3-O-rutinoside (2), ombuoside (3), kaempferol-3-β-D-O-rutinoside (4), isorhamnetin-3-O-β-D-rutinoside (5), quercetin-3-O-β-D-glucoside (6), isorhamnetin (7), kaempferol (8), and quercetin (9) by liquid chromatography mass spectrometry-ion trap time of flight and 13C nuclear magnetic resonance spectroscopy, respectively. All of them displayed various potent antioxidant effects against the DPPH radical and A549 cell injury by using H2O2-generate peroxyl radicals in vitro. A sensitive and specific ultra-performance liquid chromatography coupled with multiple-reaction monitoring mode was utilized to rapidly analyze the main six flavonoids of the ethanol extract of G. pentaphyllum within less than 8 min using a Waters Acquity UPLC BEH C18 column. The contents of them were from 57.11 to 12907.74 µg/g in G. pentaphyllum. [ABSTRACT FROM AUTHOR] more...

One new dammarane-type triterpene, gypsapogenin A (1), was isolated from the acid hydrolyzate of total saponins fromGynostemma pentaphyllum(Thunb.) Makino, together with two known compounds, (20S,24S)-3β,20,21β,23β,25-pentahydroxy-21,24-cyclodammarane (2) and (23S)-3β-hydroxydammar-20,24-dien-21-oic acid 21,23-lactone (3). Its structural elucidations were accomplished mainly on the basis of the interpretation of spectroscopic data, such as IR, HR-TOF-MS, and NMR. The cytotoxic activities were evaluated against HepG2 and A549 human cancer cell lines. [ABSTRACT FROM PUBLISHER] more...

ContextGynostemma pentaphyllum(Thunb.) Makino has been used in traditional medicine for the treatment of hyperlipidaemic with a long history. Objective:The objective of this study was to evaluate the influence ofGynostemma pentaphyllum(GP) and atorvastatin on amino acids from the plasma and liver tissue of hyperlipidaemic rats. Materials and methodsThe rats were fed a high-fat diet continuously for 11 weeks for the construction of hyperlipidaemic model. The hyperlipidaemic rats were treated withGynostemma pentaphyllum(120 mg/kg) and atorvastatin (1.8 mg/kg) for 4 weeks, and the rats were intragastric administration one time every day. Chromatographic separation was performed on a Shim-pack XR-ODSIII C18 analytical column (75 mm × 2.0 mm i.d., 1.6 μm, Shmadazu Corp., Tokyo, Japan). The biomarkers of amino acids were identified by principal component analysis (PCA) and partial least squares discriminant analysis (PLS-DA). ResultsAfter feeding with a high-fat diet, the TC and LDL-C values of the hyperlipidaemic mode rats increased dramatically (p < 0.01). The established method allowed a target analysis of 12 kinds of amino acids. PCA studies showed that the plasma amino acids had not returned to normal after GP treatment, but those had recovered slightly after atorvastatin treatment. GP has almost no impact on the metabolism of amino acids, while atorvastatin can modify the metabolism of amino acids via self-regulatory mechanisms. Discussion and conclusionUPLC/DAD combined with SCX-SPE can be successfully used for profiling analysis of amino acids. By the comparison of biomarkers following treatment with GP and atorvastatin, the influence of the two drugs on biomarkers is revealed. [ABSTRACT FROM PUBLISHER] more...

The most promising strategies to overcome bacterial drug resistance are the use of nanoparticles (NPs). In this paper, the extract of Gynostemma pentaphyllum Makino was prepared and used as reducing as well as stabilising agent to obtain silver NPs (AgNPs). The active phytochemicals present in the herb were responsible for the quick reduction in silver ion (Ag+) to metallic AgNPs (Ag0). The method is green and rapid, and the whole synthesis process can be finished within 15 min at 60°C. An intense surface plasmon resonance band in 420–450 nm range clearly revealed the formation of AgNPs. The obtained AgNPs were further characterised using X-ray diffraction, transmission electron microscopy (TEM), Fourier transform infrared (FTIR) spectroscopy and zeta potential. Moreover, the as prepared AgNPs have a superior antibacterial activity against four kinds of aquatic pathogenic bacteria, which shows great potential in aquaculture field. [ABSTRACT FROM AUTHOR] more...

Elution-extrusion counter-current chromatography (EECCC) was successfully applied for screen and separation of four flavonoids fromGynostemma pentaphyllumtea, a popular herbal tea extract in China. With the hexane/ethyl acetate/methanol/water 5/6/5/6 (v/v) system, 300 mg ofG. pentaphyllumtea extract were fractionated on a 180 mL-capacity preparative hydrodynamic CCC column. Satisfactory separation efficiency was achieved, producing milligram-amounts of quercetin, isorhamnetin, and cirsiliol over 90% pure in one EECCC process. Due to the hydrophilic property, the major flavonoid glycoside, rutin, was co-eluted with the solvent front as a mixture. Therefore, another carefully selected biphasic liquid system composed of ethyl acetate/n-butanol/water (4/1/5, v/v) was employed, yielding 35 mg of rutin with 97.1% purity. Structures of all separated compounds were identified by ESI-MS,1H NMR, and13C NMR. [ABSTRACT FROM AUTHOR] more...

Two new dammarane-type triterpene saponins, gypenbiosides A (1) and B (2), were isolated from the aerial parts of Gynostemma pentaphyllum (Thunb.) Makino. Their structural elucidations were accomplished mainly on the basis of the interrelation of spectroscopic methods, such as IR, HR-TOF-MS, and NMR. The cytotoxic activity was evaluated against one human cancer cell line HL-60 using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. [ABSTRACT FROM AUTHOR] more...

The objective of this study was to explore the effects of Gynostemma pentaphyllum on Zearalenone-induced apoptosis in mouse male germ cells. Fifty Kunming male mice at 25-days-old were classified into five groups: group A was the control (10% ethanol, 0.5 ml/day); group B with 10 µg Zearalenone/day; group C with 10 µg Zearalenone and 50 mg/kg/day Gynostemma pentaphyllum; group D with 10 µg Zearalenone and 100 mg/kg/day Gynostemma pentaphyllum; and group E with 10 µg Zearalenone and 200 mg/kg/day Gynostemma pentaphyllum. It was found that Gynostemma pentaphyllum has a marked effect on protecting male germ cells against Zearalenone-induced apoptosis, as evidenced by a reduced apoptosis rate of male germ cells and Bax expression as well as an enhancement of Bcl-2 expression in Gynostemma pentaphyllum-treated groups compared to the control. In addition, Gynostemma pentaphyllum remarkably improved pathologic changes of testicular tissue, reduced the content of malondialdehyde (MDA), and increased the activity of superoxide dismutase (SOD) caused by Zearalenone. Taken together, these results suggest that Gynostemma pentaphyllum protects against toxicity caused by Zearalenone through anti-oxidation and anti-apoptosis via the regulation of Bax and Bcl-2 expression. [ABSTRACT FROM AUTHOR] more...

Gynostemma pentaphyllum (Cucurbitaceae) is a perennial medicinal herb widely distributed in China. It's well known for its medicinal values due to contains important medicinal components gypenosides. Here, we first report and characterize its complete chloroplast genome based on Illumina paired-end sequencing data. The complete plastid genome was 154,457 bp, which contained inverted repeats (IR) of 25,603 bp separated by a large single-copy (LSC) and a small single copy (SSC) of 84,998 bp and 18,253 bp, respectively. The cpDNA contains 132 genes, comprising 81 protein-coding genes, 37 tRNA genes, 8 rRNA genes and six processed pseudogenes. The overall GC content of the plastome is 37.1%. The phylogenetic analysis of 17 selected chloroplast genomes demonstrated that G. pentaphyllum is closely related to the congeneric G. compressum. [ABSTRACT FROM AUTHOR] more...

We report the complete chloroplast genome sequence ofGynostemma pentaphyllum, a well-known traditional Chinese medicine, which produces triterpenoid saponins similar to Panax ginseng. The assembled chloroplast genome (cpDNA) was 157,654 bp in length and structurally divided into four distinct regions, namely, large single copy region (86,794 bp), small single copy region (18,654 bp) and a pair of inverted repeat regions (26,103 bp). A total of 143 genes were annotated, including 87 protein-coding genes, 10 tRNA genes and 46 rRNA genes. Phylogenetic analysis revealed that the chloroplast genome sequence ofG. pentaphyllumis most closely related to Cucumis melo. [ABSTRACT FROM PUBLISHER] more...