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The anti-gastric ulcer effect of Gynostemma pentaphyllum Makino
Abstract
Gynostemma pentaphyllum is an oriental medicinal herb reputed to have broad-spectrum activities. The plant's principal saponin components are structurally similar to those found in ginseng plants and this similarity is assumed to be responsible for the claimed activities. The present study was undertaken to evaluate a G. pentaphyllum butanol fraction (GPB) for its anti-gastric ulcer activity using experimental models. Oral administration of the GPB at 200 and 400 mg/kg body wt. significantly inhibited gastric ulcer formation induced by indomethacin, HCl/EtOH and water-immersion restraint stress in rats. In pylorus-ligated rats, pretreatment with the GPB had no effect on gastric volume, pH or acidity output, thus indicating a lack of anti-secretory effect. In ethanol-induced ulcerated rats, gastric wall mucus and hexosamine content were markedly preserved by GPB pretreatment. The findings indicate that the butanol fraction of G. pentaphyllum possesses gastroprotective potential related to the preservation of gastric mucus synthesis and secretion.
... Gynostemma pentaphyllum Makino, also called jiaogulan, is an herbaceous vine of the family Cucurbitaceae (cucumber or gourd family) indigenous to the southern reaches of China, northern Vietnam, southern Korea, and Japan (Hu, Chen, & Xie, 1996;Rujjanawate, Kanjanapothi, & Amornlerdpison, 2004). G. pentaphyllum is best known as an herbal medicine reputed to have powerful antioxidant and adaptogenic effects purported to increase longevity. ...
... Recently, polysaccharide obtained from G. pentaphyllum has attracted great attention owing to its antitumor activities (Zhou, Liang, & Hu, 2001), anti-gastric ulcer effect (Rujjanawate et al., 2004), immunomodulatory effect (Qian, Wang, & Tang, 1998, anti-aging (Luo & Wang, 2005), antioxidant properties (Cai, Zhang, & Wang, 2005;Wang & Luo, 2007), anti-exercise fatigue (Fu, 2000), and treating hyperlipidemia (Birgitte, Per, & Zhao, 1995). ...
... Besides constituting platelet aggregation and prevent atherosclerosis. It can also effectively improve obesity and prevent liver disease, gastric, and duodenal ulcers [17][18][19]. In the treatment of fatty liver, it has not been reported which genes can be regulated by Gyp-XLIX drugs. ...
Objective:
To perform Genome-wide analysis of Gypenoside XLIX (Gyp-XLIX) in the treatment of fatty liver cells.
Methods:
The gene profiles of 3 normal liver cells, 3 fatty liver cells, and 3 fatty liver cells treated with Gyp-XLIX were detected by high-throughput sequencing to identify the differentially expressed genes (DEGs) in fatty liver treated by Gyp-XLIX. Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) enrichment analysis were used to explore the biological functions of DEGs. By constructing lncRNA-mRNA co-expression network of DEGs, network node genes were mined. Possible target genes of differentially expressed lncRNA were predicted by cis regulation.
Results:
782 DEGs were screened out; that is, 172 genes were highly expressed in fatty liver cells, and the expression decreased to the level of normal liver cells after Gyp-XLIX treatment; 610 genes were under expressed in fatty liver cells, and the expression increased to the level of normal liver cells after Gyp-XLIX treatment. Functional analysis of KEGG and GO showed that DEGs process DNA-binding transcription factor activity and ion transmembrane transporter activity in the plasma membrane region. This mediates glycerophospholipid metabolism, bile secretion, fatty acid degradation and other signaling pathways. lncRNA analysis showed that the expression of 16 lncRNAs was low in fatty liver cells, and the expression was increased to the level of normal liver cells after Gyp-XLIX treatment. Target gene prediction showed that 16 differentially expressed lncRNAs had cis potential to regulate target genes, among which lncRNA RPARP-AS1 had a high degree of relationship with other genes. lncRNA-mRNA co-expression network results showed that lncRNA RPARP-AS1 may acted on NFKB2.
Conclusion:
LncRNA was differentially expressed in fatty liver cells and Gyp-XLIX treated fatty liver cells, and lncRNA RPARP-AS1 may be a regulatory gene in Gyp-XLIX treated fatty liver.
... The butanol fraction of G. pentaphyllum ethanol extract (GPB; 200 and 400 mg/kg) displayed protective effects on gastric ulcers in indomethacin-induced gastric ulcer rat model. Noticeably, pre-treatment with GPB did not alter stomach fluid volume and gastric pH value, but significantly preserved gastric wall mucus and secretion (Rujjanawate et al., 2004). Pre-treatment with gypenosides (200 mg/kg) were also reported to significantly reduce fecal hemoglobin and plasma haptoglobin from gastric ulceration caused by oral administration of indomethacin (10 mg/kg), and elevate the total intestinal aerobic bacteria, therefore reducing blood loss caused by gastric ulceration and protecting digestive system (Hesse et al., 2007). ...
Ethnopharmacological relevance
G. pentaphyllum, also known as Jiao-Gu-Lan, has been used traditionally as folk remedies for many diseases, including diabetes mellitus, metabolic syndrome, aging, and neurodegenerative diseases in China and some countries in East and Southeast Asia. It is considered as an "immortality herb" in Guizhou Province, because it was consumed regularly by the elderly native inhabitants. Other species of the same genus Gynostemma such as G. longipes and G. laxum have been used as alternatives to G. pentaphyllum in ethno-medicine in Vietnam and other Asian countries.
Aim of the review
The review aims to summarize up-to-date study results on Gynostemma species, including traditional usage, phytochemical profile, pharmacological activities, and toxicological studies, in order to suggest future research orientation and therapeutic applications on acute and chronic diseases.
Materials and methods
The relevant literature on the genus Gynostemma was gathered from secondary databases (Web of Science and PubMed), books, and official websites. The latest literature cited in this review was published in February 2020.
Results
The genus Gynostemma has been widely used in traditional medicine, mainly for treatment of diabetes, hypertension, obesity, and hepatosteatosis. To date, 328 dammarane-type saponins were isolated and structurally elucidated from Gynostemma species. Crude extracts, saponin-rich fractions (gypenosides), and pure compounds were reported to show a wide range of pharmacological activities in both in vitro and in vivo experiments. The most notable pharmacological effects were anti-cancer, cardioprotective, hepatoprotective, neuroprotective, anti-diabetic, anti-obesity, and anti-inflammatory activities. Toxicological studies were conducted only on G. pentaphyllum, showing that the plant extracts were relatively safe in both acute and long-term toxicity experiments at the given dosage while no toxicological studies were reported for the other species.
Conclusions
The review summarizes current studies on traditional uses, phytochemistry, biological properties, and toxicology of medicinal Gynostemma species. Till now, the majority of publications still focused only on G. pentaphyllum. However, the promising preliminary data of other Gynostemma species indicated the research potential of this genus, both in phytochemical and pharmacological aspects. Furthermore, clinical data are required to evaluate the efficacy and undesired effects of crude extracts, standard saponin fractions, and pure compounds prepared from Gynostemma medicinal plants.
... Gynostemma pentaphyllum Makino, also called 'Jiaogulan' in China, is a perennial liana in family Cucurbitaceae (Circosta et al. 2005). It has been used as a traditional Chinese medicine for a long time to alleviate various diseases such as bronchitis, asthma, hypertension and diabetes mellitus (Circosta et al. 2005;Rujjanawate et al. 2004). Various dammarane gypenosides identified in G. pentaphyllum share similar structures with those in expensive ginseng and have been demonstrated to have broad-spectrum activities such as immune regulatory activity (Huang et al. 2007), antioxidative activity (Shang et al. 2006), blood pressure regulation activity (Tanner et al. 1999), and anti-cancer activity (Lu et al. 2008). ...
Funding information should be correctly read as: “Young Talents” Project of Northeast Agricultural University (No. 17QC05), and are NOT the former two ones 17QC05 and uNPYSCT-2,018,157.
... Recently, Gynostemma pentaphyllum Makino has attracted great attention owing to its anti-tumor activities [4] , immunomodulatory effect [5] , anti-gastric ulcer effect, treating hyperlipidemia, and anti-oxidant properties [6] , and has been described as having minimal toxicity [7] . Therefore, the G. pentaphyllum green tea is presently promoted in China and is sold in Europe as an herbal tea which is ''advantageous to one's health and beauty'' [8][9] . The presence of saponins and flavonoids in G. pentaphyllum as functional components is believed to be responsible for this health-enhancing effect. ...
Gynostemma pentaphyllum Makino is a well known edible and medicinal plant in oriental countries, its dominant active constituents are mainly Gypenosides(GP). Endophytic fungi with antioxidant activity were screened and identified from gynostemma pentaphyllum, and gynostemma pentaphyllum saponin (GP) was used as host. A total of 10 strains of endophytic fungi were isolated from the root of healthy, living, and symptomless tissues of Gynostemma pentaphyllum Makino. The extract from a strain (G4) showed antioxidant activity and had the same RF value in TLC, because the retention time of real gynostemma pentaphyllum saponin (GP) and its extract was the same as that of natural gynostemma pentaphyllum (GP) in HPLC. So the strain G4 of endophytic fungus appears to produce the same components as its host.
... Gynostemma pentaphyllum Makino, also called 'Jiaogulan' in China, is a perennial liana in family Cucurbitaceae (Circosta et al. 2005). It has been used as a traditional Chinese medicine for a long time to alleviate various diseases such as bronchitis, asthma, hypertension and diabetes mellitus (Circosta et al. 2005;Rujjanawate et al. 2004). Various dammarane gypenosides identified in G. pentaphyllum share similar structures with those in expensive ginseng and have been demonstrated to have broad-spectrum activities such as immune regulatory activity (Huang et al. 2007), antioxidative activity (Shang et al. 2006), blood pressure regulation activity (Tanner et al. 1999), and anti-cancer activity (Lu et al. 2008). ...
Gynostemma pentaphyllum is a widely cultivated Chinese medicinal herb which has broad-spectrum activities. In this study, G. pentaphyllum plants with typical symptom of mosaic were found in Shaanxi province of China. The infection of Alfalfa mosaic virus (AMV) was identified by small RNA sequencing and confirmed by specific RT-PCR. We determined the complete genomic sequence of AMV-Gyn (GenBank No. MH332897-MH332899). The 3643 nt RNA1 and 2598 nt RNA2 encoded P1 protein of 1126 aa and P2 protein of 791 aa, respectively. The 2040 nt RNA3 encoded MP of 300 aa and CP of 221 aa. Phylogenetic analysis based on sequences of RNA3 and CP gene clustered AMV-Gyn into phylogroup I with the closest evolutionary relationship with AMV-Manfredi (KC881010). No recombination event was detected. To our knowledge, this is the first report of a virus infecting G. pentaphyllum.
... In another study, Carica candamarcensis was found to prevent ulcer by inhibiting mucus depletion (Mello et al., 2008). As evidenced from many reports, cytoprotection was also found to be induced by other mucus upregulating fruits and vegetables like A. sativum, Apium graveolens, A. racemosus, Brassica oleracea, C. papaya, C. aurantium, C. lemon, Cynara scolymus, D. carota, F. glomerata, Gynostemma pentaphyllum, P. emblica, P. trifoliate, P. granatum, Trichosanthes cucumerina (Choi et al., 2014;Al-Howiriny et al., 2010;Sairam et al., 2003;Carvalho et al., 2011;Lemos et al., 2011;Mello et al., 2008;Pinto et al., 2015;Moraes et al., 2013;Polo et al., 2012;Rozza et al., 2011;Nassar et al., 2013;Ishida et al., 2010;Chandra et al., 2015;Rao et al., 2008;Rujjanawate et al., 2004;Sairam et al., 2002;Bandyopadhyay et al., 2000;Lee et al., 2009;Alam et al., 2010;Arawwawala et al., 2010). Thus cytoprotection by administration of fruits and vegetables is mostly regulated by maintaining the levels of COX-2 and PGE2 (Table 2). ...
Gastric ulcer is the damage caused to mucosal layer of the stomach under the action of various factors like high levels of acid and pepsin, invasion by Helicobacter pylori, etc. Although most cases have been controlled and the rate of ulcer occurrence has reduced over the last few decades, gastric ulcer still holds a prime concern today. A range of palliative medicines comprising proton pump inhibitors, H2 receptor antagonists, COX-2 inhibitors (coxibs) is widely in use and patients have also been administered with acid suppression therapies. But these remedies aggravate the condition of patients causing severe side effects, or rather impart temporary relief. Therefore, it is highly imperative to develop safe and effective therapies for the treatment of gastric ulcer. Nature provides us various fruits and vegetables that can combat gastric ulcer through multiple mechanisms; predominantly via antioxidant, anti-inflammatory, antisecretory, antimicrobial, anticholinergic and cytoprotective activity, inhibition of small intestinal propulsion etc. Various phytochemicals from fruits and vegetables such as phenolics, flavonoids, tannins and saponins play a vital role in the prevention and cure of gastric ulcer. This review is an attempt to compile all fruits and vegetables known for their profound antiulcer effect and their underlying mechanisms of action.
... The results of the analysis of phytotherapeutic treatment used in preclinical studies are shown in Table I. --X Reduction of gastric lesions; increased mucin content; antiinflammatory activity (reduction of pro-inflammatory markers: IL-1β, TNF-α, 5-LO and COX-2); absence of haemorrhage and necrosis Gynostemma pentaphyllum (whole plant extract), [29] --X Maintenance of gastric mucus production [6] pH ↑; total acidity and free acidity ↓ Moringa oleifera (fine aqueous leaf extract), [32] --X Prevention of ulcer by the modulation of 5-HT secretion through 5-HT 3 receptors in the gastrointestinal tract Neurolaena lobate (hydroalcoholic extract of aerial parts), [14] --X Alteration of gastric juice parameters: pH ↑ and the amount of gastric juice ↓; increase of prostaglandin synthesis and mucus amount Ocimum gratissimum (extract), [26] --X Mucus amount ↑; gastric acid secretion ↓ Peganum harmala (seeds), ...
In addition to its advantages (technological progress, high-performance medical treatment, multiple information sources, new communication systems), the 21st century brings many disadvantages, such as: professional stress due to the uncertainty of the future and to the increasingly higher professional performance indicators, the quality of interpersonal relationships, an imbalance between professional and personal life, a lack of interest in self-knowledge. Besides all these stress factors, certain drugs, inadequate nutrition both in terms of quantity and quality, a small number of meals eaten per day, a late last meal, as well as late bedtime cause an increase of gastric secretion. Depending on the psychosomatic profile of patients, these can be divided into two main categories: patients who accept drug therapy and patients who prefer alternative therapies. This review aims to present all types of alternative therapies, for which preclinical studies are available. © 2017, Romanian Society for Pharmaceutical Sciences. All Rights reserved.
... M. oleifera is rich in zeatin, quercetin, betasitosterol, caffeoylquinic acid and kaempferol, a rare combination of important bioactive compounds (Siddhuraju and Becker, 2003;Anwar et al., 2007). Various parts of this plant such as the leaves, roots, seed, bark, fruit, flowers and immature pods have been reported to act as cardiac and circulatory stimulants (Duke, 2001;Nandave et al., 2009), have antitumor (Guevaraa et al., 1999;Parvathy and Umamaheshwari, 2007), antipyretic (Hukkeri et al., 2006), anti-inflammatory (Muangnoi et al., 2012), antiulcer (Rujjanawate et al., 2004;Debnath and Guha, 2007), antispasmodic (Gilani et al., 1994), diuretic (Morton, 1991), antihypertensive (Gilani et al., 1994), cholesterol lowering (Ghasi et al., 2000), antioxidant (Singh et al., 2009), antidiabetic (Ndong et al., 2007), hepatoprotective (Pari and Kumar, 2002) and antibacterial and antifungal activities (Chuang et al., 2007;Saadabi and Abu Zaid, 2011) and for these reasons have been employed in folk and Ayurvedic traditional medicine of Africa and South Asia for a variety of medicinal purposes. In African Traditional Medicine (ATM), M. oleifera is one of the many medicinal plants employed by herbalist to treat or manage PLWHA and there are so many claims on its effectiveness in improving quality of life and in reversing the course of the HIV/AIDS disease progression. ...
Moringa oleifera Lam. (Moringaceae) is one of the many medicinal plants employed by herbalist to treat or manage people living with HIV/AIDS (PLWHA) in African Traditional Medicine (ATM) and there are many claims to the fact that it improves quality of life and reverses the course of the HIV/AIDS disease progression. This practice and the claims of efficacy spurred the present study in which the inhibitory activities of three different extracts of M. oleifera on lentiviral vector infectivity were studied on HeLA cells by measuring the expression of green fluorescent protein (GFP) transgene in the vector using flow cytometry. An infectious VSV-G-pseudotyped, human immunodeficiency virus type 1-based, self-inactivating lentiviral vector particles were generated by transient co-transfection of the vector plasmid (pHIV-1 CSCG) with packaging plasmids encoding tat, rev, gag-pol (pCMVΔR8.2), a VSV-G expression plasmid (pHIT-G), a secretory alkaline phosphate expression plasmid (pSEAP) which are all necessary for viral infectivity. The extracts studied were obtained by solvent extraction of the leaf powder of M. oleifera with ethyl ether (EM), methanol (MM) and water (AM). All the extracts (EM, MM, and AM) were active against the HIV-1 lentiviral vector and inhibited the early events of the viral replication cycle on HeLa cells in a concentration-dependent manner with IC 50 of 7.59 µg EM/ml, 7.72 µg MM/ml and 7.17 µg AM/ml, respectively. Cytotoxicity of the extracts evaluated in parallel on HeLA cells by the MTT assay method showed TC 50 values of 32.33 µg EM/ml, 38.88 µg MM/ml and 41.58 µg AM/ml with selectivity indices (SI) of 4.26, 5.04 and 5.8, respectively. In this study, M. oleifera leaf extracts showed potent and selective inhibition of early steps in HIV-1 infectivity and could serve as source of antiretroviral lead molecules. The outcome of this investigation could partly explain the benefits and improvement in quality of life claimed by PLWHA in the use of this medicinal plant as supplement.
... G. pentaphyllum is a perennial climber used for treatment of many disorders. Gypenosides, a dammarane-type saponin (Liu et al., 2005) isolated from G. pentaphyllum, are major bioactive principles which have been reported to have various activities such as anti-ulcer (Rujjanawate et al., 2004), anti-tumour (Chiu et al., 2003(Chiu et al., , 2004Chen et al., 2004); cholesterol-reducing effect (Kimura et al., 1983;Huang et al., 2005), immunopotentiating (Zhang et al., 1990;Li and Xing, 1992) and anti-inflammatory activities. This study was motivated by the beneficial effects claimed in complementary medicine of this plant extract in viral diseases, including the benefits claimed in HIV infections. ...
Three different extracts of Gynostemma pentaphyllum (Cucurbitaceae), a medicinal plant used for a variety of ailments in complementary and alternative medicine (CAM) including those caused by viral infections with claims of efficacy against HIV-1 infections were screened. These claims motivated the study in which the inhibition of viral vector infectivity of HeLa cells was assessed flow cytometrically by measuring the expression of green fluorescent protein (GFP) transgene incorporated in the lentiviral vector construct. An infectious VSV-G-pseudotyped, human immunodeficiency virus type 1-based, self-inactivating lentivirus vector particles were generated by transient co-transfection of the vector plasmid (pHIV-1 CSCG), with packaging plasmids encoding tat, rev, gag-pol (pCMV∆R8.2), a VSV-G expression plasmid (pHIT-G) and a secretory alkaline phosphate expression plasmid (pSEAP) all necessary for viral infectivity. The extracts studied were obtained by solvent extraction of the leaf powder of G. pentaphyllum with ethyl ether (EG), methanol (MG), and water (AG). The AG, MG and EG were all active against the HIV-1 lentiviral vector and inhibited the early events of the viral replication cycle on HeLa cells in a concentration-dependent manner with a IC 50 of 6.21 µg AG/ml, 8.32 µg MG/ml and 5.8 µg EG/ml, respectively. The cytotoxicity of the extracts to HeLa cells evaluated in parallel by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay method showed TC 50 values of 36.77 µg AG/ml, 38.68 µg MG/ml and 41.02 µg EG/ml with selectivity indices (SI) of 5.92, 4.65 and 7.02, respectively. The results of the study show that the extracts of G. pentaphyllum possess potent and selective anti-retroviral potentials and could serve as possible source of lead antiviral drugs against HIV.
... Jiaogulan tea, made from G. pentaphyllum leaves, has been used as an energizing agent, for treatment of common colds and infections, and for general health (Blumert, 1999). Pharmacological studies of Jiaogulan have pointed to its immunomodulatory (Suntararuks et al., 2008), antitumor (Chen et al., 2011), anti-gastric ulcer (Rujjanawate et al., 2004), anti-hyperlipidemic, hypoglycemic (Megalli et al., 2006, hepatoprotective (Lin et al., 2000) and cardiovascular disease protective effects (Circosta et al., 2005). Most of these activities are associated with the presence of antioxidants, such as saponins, flavonoids, polysaccharides and gypenosides in Jiaogulan tea (Kao et al., 2008). ...
Cyclic voltammetry, as well as four well-established spectrophotometric and fluorimetric assays, were applied to study the contribution of phenolic compounds to the antioxidant capacity of aqueous and methanol extracts of Jiaogulan tea (Gynostemma pentaphyllum). In addition, individual phenolic acid profiles of G. pentaphyllum extracts, determined using UPLC–MS/MS, were reported for the first time in this study. Methanol extraction resulted in higher contents of phenolic compounds, as well as antioxidant capacity of tested extracts. Our results suggest that G. pentaphyllum aqueous and methanol extracts have high antioxidant capacity and are rich in phenolic compounds, such as chlorogenic acid, which might play a role in the prevention of type 2 diabetes mellitus and cardiovascular disease.
... Conventional non-steroidal anti-inflammatory agents are well recognized to produce gastric mucosal damage due to their capacity to inhibit cyclooxygenase-1 (COX-1) and the synthesis of gastroprotective PG (Guo et al., 2005); a reduction in the local blood flow, topical irritation and an interference with restitution and tissue repair. The current study on indomethacin-induced gastric damage showed inhibition of gastric lesions by ASC; suggested that the ability of the cinnamon suspension to prevent ulceration is at least partly through prostaglandin biosynthesis mechanism (Rujjanawate et al., 2004). ...
The present study was carried out to evaluate the gastric antisecretory and antiulcer activities of 'Cinnamon' Cinnamomum zeylanicum in rats. The aqueous suspension of cinnamon (250 and 500 mg/kg) has been screened using pylorus ligation (Shay) rat model, necrotizing agents and indomethacin-induced ulceration in rats. Histopathological assessment was done on gastric tissue of rats. Gastric wall mucus and nonprotein-sulfhydryl contents were also estimated. Cinnamon suspension pretreatment decreased the basal gastric acid secretion volume and rumenal ulceration in pylorus ligated rats. The suspension effectively inhibited gastric hemorrhagic lesions induced by 80% ethanol, 0.2 M sodium hydroxide, and 25% sodium chloride. The cinnamon suspension also showed antiulcer activity against indomethacin. Pretreatment with cinnamon suspension offered a dose-dependent protection against various histological indices. Treatment of rats with cinnamon replenished the ethanol-induced decreased levels of gastric wall mucus and nonprotein-sulfhydryl concentrations. The gastroprotection of cinnamon observed in the present study is attributed to its effect through inhibition of basal gastric secretion (attenuation of aggressive factors) and stimulation mucus secretion (potentiation of defensive factors); and increase in nonprotein-sulfhydryl concentration probably due to prostaglandin-inducing abilities mediated through its antioxidant property.
... M. oleifera is rich in zeatin, quercetin, betasitosterol, caffeoylquinic acid and kaempferol, a rare combination of important bioactive compounds (Siddhuraju and Becker, 2003;Anwar et al., 2007). Various parts of this plant such as the leaves, roots, seed, bark, fruit, flowers and immature pods have been reported to act as cardiac and circulatory stimulants (Duke, 2001;Nandave et al., 2009), have antitumor (Guevaraa et al., 1999;Parvathy and Umamaheshwari, 2007), antipyretic (Hukkeri et al., 2006), anti-inflammatory (Muangnoi et al., 2012), antiulcer (Rujjanawate et al., 2004;Debnath and Guha, 2007), antispasmodic (Gilani et al., 1994), diuretic (Morton, 1991), antihypertensive (Gilani et al., 1994), cholesterol lowering (Ghasi et al., 2000), antioxidant (Singh et al., 2009), antidiabetic (Ndong et al., 2007), hepatoprotective (Pari and Kumar, 2002) and antibacterial and antifungal activities (Chuang et al., 2007;Saadabi and Abu Zaid, 2011) and for these reasons have been employed in folk and Ayurvedic traditional medicine of Africa and South Asia for a variety of medicinal purposes. In African Traditional Medicine (ATM), M. oleifera is one of the many medicinal plants employed by herbalist to treat or manage PLWHA and there are so many claims on its effectiveness in improving quality of life and in reversing the course of the HIV/AIDS disease progression. ...
Moringa oleifera Lam. (Moringaceae) is one of the many medicinal plants employed by herbalist to treat or manage people living with HIV/AIDS (PLWHA) in African Traditional Medicine (ATM) and there are many claims to the fact that it improves quality of life and reverses the course of the HIV/AIDS disease progression. This practice and the claims of efficacy spurred the present study in which the inhibitory activities of three different extracts of M. oleifera on lentiviral vector infectivity were studied on HeLA cells by measuring the expression of green fluorescent protein (GFP) transgene in the vector using flow cytometry. An infectious VSV-G-pseudotyped, human immunodeficiency virus type 1-based, selfinactivating lentiviral vector particles were generated by transient co-transfection of the vector plasmid (pHIV-1 CSCG) with packaging plasmids encoding tat, rev, gag-pol (pCMVΔR8.2), a VSV-G expression plasmid (pHIT-G), a secretory alkaline phosphate expression plasmid (pSEAP) which are all necessary for viral infectivity. The extracts studied were obtained by solvent extraction of the leaf powder of M. oleifera with ethyl ether (EM), methanol (MM) and water (AM). All the extracts (EM, MM, and AM) were active against the HIV-1 lentiviral vector and inhibited the early events of the viral replication cycle on HeLa cells in a concentration-dependent manner with IC50 of 7.59 μg EM/ml, 7.72 μg MM/ml and 7.17 μg AM/ml, respectively. Cytotoxicity of the extracts evaluated in parallel on HeLA cells by the MTT assay method showed TC 50 values of 32.33 μg EM/ml, 38.88 μg MM/ml and 41.58 μg AM/ml with selectivity indices (SI) of 4.26, 5.04 and 5.8, respectively. In this study, M. oleifera leaf extracts showed potent and selective inhibition of early steps in HIV-1 infectivity and could serve as source of antiretroviral lead molecules. The outcome of this investigation could partly explain the benefits and improvement in quality of life claimed by PLWHA in the use of this medicinal plant as supplement. Keywords: Antiviral activity, antiviral screening, lentiviral vector particles, Moringa oleifera , HIV-1, viral vectorbased assay. African Journal of Biotechnology Vol. 12(30), pp. 4866-4873
... cellular anti-oxidant systems. Since various biological activities of saponinssuch as acute hepatic failure induced by lipopolysaccharide and D-galactosamine in mice [29], gastric ulcer induced by HCl/EtOH [30], and oxidative injury of dopaminergic neurons induced by 1-methyl-4-phenylpyridinium ion (MPP(+) [28] are derived from their neutralizing activity against oxidative stress, DWP208 seems to have similar protective activities against these pathological symptoms. Further tests of the pharmacological actions of DWP208 in such models are now warranted. ...
DW P208 is a sodium succinate form of ZYM-201 which is a triterpenoid glycoside isolated from Sanguisorba officinalis, a medicinal plant prescribed for various diseases, such as duodenal ulcers and bleeding in East Asian counties. We demonstrated that this compound is able to normalize the altered lipid metabolism induced by hyperglycemia and a high fat diet. In this study, we determined whether hyperlipidemic conditions induced with chronically treated alcohol can also be restored by DW P208. Similar to our previous results, orally administered DWP208 (1 to 10 mg/kg) also ameliorated the hyperlipidemia that was induced by alcohol. This compound reversed the alcohol-induced hyper-lipidemia including (i) up-regulated hyperlipidemic parameters such as low-density lipoprotein (LDL), very low-density lipoprotein (VLDL), atherosclerotic index (AI), triglyceride, and total cholesterol, and (ii) down-regulated hyperlipidemic parameters such as absolute body weight, superoxide dismutase (SOD) activity, and high-density lipoprotein (HDL) in serum and liver. According to our data, the ameliorative activity of DW P208 is due to its indirect anti-oxidative activity as a result of which lipid peroxide and hydroxyl radical levels were reduced and the activity of SOD was enhanced. Therefore, our data strongly suggest that DW P208 can be used as a remedy against alcohol-induced hyper-lipidemia.
... In recent decades, pharmacological studies have revealed that G. pentaphyllum (Thunb.) Makin has many bioactivities, including antimicrobia, anti-cancer, anti-aging, antifatigue, anti-ulcer, hypolipidemic and immuno-modulatory qualities (Wang et al., 2002;Rujjanawate et al., 2004;Megalli et al., 2006;Yeo et al., 2008;Srichana et al., 2011;Schild et al., 2010;Long, 2010). G. pentaphyllum (Thunb.) ...
The purpose of this study was to evaluate the effects of Gynostemma pentaphyllum (Thunb.) Makino polysaccharides (GPMP) supplementation on exercise tolerance and oxidative stress induced by exhaustive exercise. Male rats were divided into 5 groups of 10 animals each. The first, second, third and forth groups designated as PGP treatment group was administered with GPMP of 50, 100, 200 and 400 mg/kg body weight by gavage every day, respectively. The fifth group designated as control group was administered with the equal volume of distilled water. After 30 days, exhaustive swimming exercise of rats was performed, and then the exhaustive swimming time, liver glycogen level, antioxidant enzymes activities and MDA concentrations were determined. Results of the aforementioned study showed that GPMP supplementation prolonged exhaustive swimming time and improved liver glycogen reserve, which suggested that GPMP supplementation improved exercise tolerance. Furthermore, GPMP supplementation could promote increases in the activities of super oxide dismutase (SOD), catalase (CAT) and glutathione peroxidase (GPH-Px), and reduce MDA concentrations, which suggested that PGP supplementation reduced oxidative stress induced by exhaustive exercise.
... 18 Gynostemma pentaphyllum Rujjanawate et al (2003) evaluated butanol fraction (GPB) of Gynostemma pentaphyllum for antiulcer activity using indomethacin, ethanol and stress induced ulcer in rat, and the result revealed that the butanol fraction of Gynostemma pentaphyllum possess significant gastroprotective potential as the mucous protective effect along with reduction in gastric acid volume was observed. 19 Cucurbita pepo Sarkar et al (2008) evaluated aqueous extract of Cucurbita pepo fruit pulp for ulcer healing potential against the drug (Aspirin) induced ulcers in albino rats. The result shows that pretreatment of Cucurbita pepo fruit pulp extract significantly reduced ulcerative index in animals, and established its antiulcer activity. ...
Due to changes in life style and eating habits an increase in frequency to be affected by ulceration in gastric contents can be observed now a day. At the same time a number of semisynthetic and synthetic drugs like proton pump inhibitors, H2 receptor antagonists, mucosal defensive agents along with various antimicrobial agents are available for the treatment of ulcer, but clinical evaluation of these drugs has shown side effects, and drug interactions. Recently a number of approaches have been made for the development of newer ulcer healing or ulcer protective using herbal sources, as they are easily available, of low cost and have no or less side effects. This review aim to compile data on plants from cucurbetaceae family reported for their anti-ulcer or ulcer healing properties.
... Furthermore, molecular modification of polysaccharide was considered as a way to enhance the biological activities of polysaccharide. Recently, polysaccharide obtained from Gynostemma pentaphyllum Makino (GPP) has attracted great attention owing to its antitumor activities, immunomodulatory effect and antioxidant properties (Birgitte, Per, & Zhao, 1995;Qian, Wang, & Tang, 1998;Rujjanawate, Kanjanapothi, & Amornlerdpison, 2004). In our previous work, GPP with molecular mass (M w ) as 9.3 kDa was obtained containing the composition of rhamnose and xylose, whose mol ratio was 1:12.25. ...
Core-shell structured multifunctional nanocarriers (NCs) of ZnO quantum dots-conjugated gold nanoparticles (Au NPs) as core and amphiphilic hyperbranched block copolymer as shell were synthesized for targeted anticancer drug delivery. The amphiphilic hyperbranched block copolymer contained poly(l-lactide) (PLA) inner arm and folate (FA)-conjugated a sulfated polysaccharide from Gynostemma pentaphyllum Makino (GPPS-FA) outer arm. The structure and properties of core-shell structured multifunctional nanocarriers were characterized and determined by UV-visible spectra, FT-IR spectra, X-ray diffraction (XRD), fluorescence spectroscopy and TEM analyses. The release results indicated that camptothecin (CPT) release from NCs at pH 7.4 was much greater than that at pH 5.3. The cytotoxicity studies showed that both the blank NCs and the CPT-loaded NCs provided high anticancer activity against Hela cells. Furthermore, nanocarriers gained specificity to target model cancer cells in this study due to the enhanced cell uptake mediated by FA moiety. The results indicated that the NCs not only had great potential as tumor-targeted drug delivery nanocarrier, but also had an assistant role in the treatment of cancer.
... Makino (Cucurbitaceae), a perennial creeping herb distributed in Japan, Korea, China, and Southeast Asia, was once used as a sweetener in Japan and as a folk medicine in China (Yin et al., 2004). The pharmacological studies of G. pentaphyllum and/or isolated gypenosides have been reported to affect numerous activities resulting in antitumor (Ky et al., 2010;Lin et al., 2011), cholesterol-lowering (Norberg et al., 2004), immunopotentiating (Sun and Zheng, 2005), antioxidant , hypoglycemic (Huyen et al., 2010) and anti-ucler (Rujjanawate et al., 2004) effects. Unlike most plants of the Cucurbitaceae family, G. pentaphyllum does not show any significant toxic effect in vivo (Attawish et al., 2004;Choi et al., 2010). ...
Multidrug resistance (MDR) to anticancer drugs is a major obstacle to successful chemotherapy in the treatment of cancers. Identification of natural compounds capable of circumventing MDR with minimal adverse side effects is an attractive goal. Here, we found that H6, a gypenoside aglycon from Gynostemma pentaphyllum, displayed potent anti-MDR activity. Average resistant fold (RF) of H6 is 1.03 and 1.04 in KB/VCR and MCF-7/ADR cells compared to their parental cells. H6 alone ranging from 2μmol/l to 40μmol/l (μM) did not display a significant anti-proliferative effect on KB/VCR cells and other cells, while the compound at these concentrations enhanced the cytotoxicity of vincristine (VCR) to KB/VCR cells. H6 showed a significant synergistic effect in combination with VCR. By quantification of sub-G(1) fraction cells, H6 also enhanced the VCR-induced apoptosis in a dose-dependent manner. The short time treatment with H6 increased the intracellular accumulation of rhodamine 123 (Rho123) and 5(6)-carboxyfluorescein diacetate (CFDA) in KB/VCR cells. Further studies showed that H6 treatment resulted in the decrease of the RNA transcript level of P-glycoprotein (P-gp), multidrug resistance-associated protein 1 (MRP1) and breast cancer resistance protein (BCRP). H6 inhibited the function of P-gp by stimulating P-gp ATPase activity and decreased MRP1 expression with a blockade of STAT3 phosphorylation. These findings suggest that H6, a multi-targets reversal agent with no significant toxic effect, may be a potential candidate to circumvent the P-gp and MRP1-mediated MDR.
... G. pentaphyllum is a perennial climber used for treatment of many disorders. Gypenosides, a dammarane-type saponin (Liu et al., 2005) isolated from G. pentaphyllum, are major bioactive principles which have been reported to have various activities such as anti-ulcer (Rujjanawate et al., 2004), anti-tumour (Chiu et al., 2003(Chiu et al., , 2004Chen et al., 2004); cholesterol-reducing effect (Kimura et al., 1983;Huang et al., 2005), immunopotentiating (Zhang et al., 1990;Li and Xing, 1992) and anti-inflammatory activities. This study was motivated by the beneficial effects claimed in complementary medicine of this plant extract in viral diseases, including the benefits claimed in HIV infections. ...
Three different extracts of Gynostemma pentaphyllum (Cucurbitaceae), a medicinal plant used for a variety of ailments in complementary and alternative medicine (CAM) including those caused by viral infections with claims of efficacy against HIV-1 infections were screened. These claims motivated the study in which the inhibition of viral vector infectivity of HeLa cells was assessed flow cytometrically by measuring the expression of green fluorescent protein (GFP) transgene incorporated in the lentiviral vector construct. An infectious VSV-G-pseudotyped, human immunodeficiency virus type 1-based, selfinactivating lentivirus vector particles were generated by transient co-transfection of the vector plasmid (pHIV-1 CSCG), with packaging plasmids encoding tat, rev, gag-pol (pCMVΔR8.2), a VSV-G expression plasmid (pHIT-G) and a secretory alkaline phosphate expression plasmid (pSEAP) all necessary for viral infectivity. The extracts studied were obtained by solvent extraction of the leaf powder of G. pentaphyllum with ethyl ether (EG), methanol (MG), and water (AG). The AG, MG and EG were all active against the HIV-1 lentiviral vector and inhibited the early events of the viral replication cycle on HeLa cells in a concentration-dependent manner with a IC 50 of 6.21 μg AG/ml, 8.32 μg MG/ml and 5.8 μg EG/ml, respectively. The cytotoxicity of the extracts to HeLa cells evaluated in parallel by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay method showed TC 50 values of 36.77 μg AG/ml, 38.68 μg MG/ml and 41.02 μg EG/ml with selectivity indices (SI) of 5.92, 4.65 and 7.02, respectively. The results of the study show that the extracts of G. pentaphyllum possess potent and selective anti-retroviral potentials and could serve as possible source of lead antiviral drugs against HIV.
... Recently, a butanol fraction from G. pentaphyllum displayed anti-gastric ulcer properties. Pretreatment with the butanol fraction markedly preserved gastric wall mucus and hexosamine content in ethanolinduced ulcerated rats (Rujjanawate et al., 2004). In rats, gypenosides have been beneficial in reversing gastric ulcer induced by Helicobacter pylori (Zhang et al., 1999). ...
In traditional Chinese medicine, Gynostemma pentaphyllum (Thunb.) Makino is a herbal drug of extreme versatility and has been extensively researched in China. The dammarane saponins
isolated from Gynostemma pentaphyllum, namely gypenosides or gynosaponins, are believed to be the active components responsible for its various biological activities
and reported clinical effects. This review attempts to encompass the available literature on Gynostemma pentaphyllum, from its cultivation to the isolation of its chemical entities and a summary of its diverse pharmacological properties attributed
to its gypenoside content. Other aspects such as toxicology and pharmacokinetics are also discussed. In vitro and in vivo evidence suggests that Gynostemma pentaphyllum may complement the popular herbal medicine, Panax ginseng, as it also contains a high ginsenoside content and exhibits similar biological activities.
Gynostemma pentaphyllum (Thunb.) Makino (GP), also named Jiaogulan in Chinese, was known to people for its function in both health care and disease treatment. Initially and traditionally, GP was a kind of tea consumed by people for its pleasant taste and weight loss efficacy. With the passing of the centuries, GP became well known as more than just a tea. Until now, numbers of bioactive compounds, including saponins (also named gypenosides, GPS), polysaccharides (GPP), flavonoids, and phytosterols were isolated and identified in GP, which implied the great medicinal worth of this unusual tea. Both in vivo and in vitro tests, ranging from different cell lines to animals, indicated that GP possessed various biological activities including anti-cancer, anti-atherogenic, anti-dementia, and anti-Parkinson’s diseases, and it also had lipid-regulating effects as well as neuroprotection, hepatoprotective, and hypoglycemic properties. With the further development and utilization of GP, the research on the chemical constituents and pharmacological properties of GP were deepening day by day and had made great progress. In this review, the recent research progress in the bioactive compounds, especially gypenosides, and the pharmacological activities of GP were summarized, which will be quite useful for practical applications of GP in the treatment of human diseases.
Background: An ulcer is an ongoing health ailment affecting all age groups
wherein the linings of the oesophagus, stomach, and intestine are mainly affected.
Many discoveries were made for ulcer therapy but research findings on a disease
soon become irrelevant due to ever-changing pathology. Therefore, there is a need
for newer drugs for pharmacological interventions. However, discovering or
developing a new drug requires ethically and scientifically acceptable pre-clinical
tools for assessing therapeutic activity.
Objective: The review aims to compile and highlight the pre-clinical techniques/models used for assessing the efficacy of potential anti-ulcer agents.
Materials and Methods: A comprehensive theoretical survey was done from October 2019 up to April 2020. Keywords such as, ‘ulcer’, ‘in-vitro evaluations’, and ‘in vivo evaluations’ were used either alone or in combination. Academic search engines like PubMed, Science Direct, Google Scholar, Web of Science, and Scopus were utilized.
Results and Discussion: The exhaustive literature study provides in vitro and in-vivo techniques for evaluating potential anti-ulcer agents. Successfully employed ulcer inducers, test drugs, biological preparations or animal models for examining the pharmacological activity of anti-ulcer agents are highlighted. Conclusion: Researchers working to discover and develop newer/safer anti-ulcer agents may utilize this literature for retrieving appropriate in vitro or in-vivo pre-clinical techniques for investigating
potential anti-ulcer agents.
In this paper, a novel acidic polysaccharide (CPS-1) was successively prepared from Gynostemma pentaphyllum using hot water isolation method to explore its antitumor and antioxidant activities. Structural characteristics of CPS-1 were evaluated by SEM, HPGPC, HPAEC-PAD, FT-IR, and NMR. The results indicated: CPS-1 was mainly composed of Ara, Gal, Glc, Xyl, Man, GalA and GlcA in a molar ratio of 1.23:2.14:0.67:0.2:0.29:0.16:0.04 with molecular weight of 3297 kDa. Combining with the results of FT-IR and NMR, it was inferred that CPS-1 was mainly possessed the five main linkages including α-D-Ara, α-D-Gal, α-D-Man, α-D-Xyl and β-D-Glc. Furthermore, MTT results exhibited that the IC50 value of CPS-1 for inhibitive effect on SPC-A-1 and MGC-803 cells for 24 h were 284.36 and 365.27 μg/mL, respectively. Microscopic observations showed that the cells exhibited significant apoptotic characteristics, such as cell shrinkage, the decreased of cell adherence and the appearance of apoptotic bodies. It was shown that CPS-1 had significant anti-tumor activity. In addition, the ability of CPS-1 to scavenge superoxide radical, ABTS and DPPH radicals was also enhanced with the increased of concentration. Therefore, it was revealed that CPS-1 might be used as a natural anticancer and antioxidant component.
Background: Peptic ulcer is a deep gastrointestinal erosion disorder that involves the entire mucosal thickness and can even penetrate the muscular mucosa. Nowadays, several plants and compounds derived from it have been screened for their antiulcer activity. In the last few years, there has been an exponential growth in the field of herbal medicine. This field has gained popularity in both developing and developed countries because of their natural origin and less side effects.
Objective: This review aims to provide a comprehensive summary of currently available knowledge of medicinal plants and phytoconstituents reported for their anti-ulcer properties.
Methods: The worldwide accepted database like SCOPUS, PUBMED, SCIELO, NISCAIR, ScienceDirect, Springerlink, Web of Science, Wiley, SciFinder and Google Scholar were used to retrieve available published literature. Results: A comprehensive review of the present paper is an attempt to list the plants with antiulcer activity. The review narrates the dire need to explore potential chemical moieties that exert an antiulcer effect, from unexploited traditional plants. Furthermore, the present study reveals the intense requirement to exploit the exact mechanism through which either the plant extracts or their active constituents exhibit their antiulcer properties.
Conclusion: This article is the compilation of the plants and its constituents reported for the treatment of peptic ulcers. The Comprehensive data will surely attract the number of investigators to initiate further research that might lead to the drugs for the treatment of ulcers. As sufficient scientific data is not available on plants, most of the herbals cannot be recommended for the treatment of diseases. This can be achieved by research on pure chemical structures derived from plants or to prepare new lead compounds with proven beneficial preclinical in vitro and in vivo effects. However, a lot remains to be done in further investigations for the better status of medicinal plants.
A new acidic polysaccharide (GPTP-3) with a molecular weight of 2.49×106 Da was extracted and purified from Gynostemma pentaphyllum tea. Monosaccharide analysis revealed that GPTP-3 mainly contained of mannose (20.4%), glucuronic acid (17.4%), glucose (33.4%) and galactose (21.4%) in the molar percentages. The immunostimulating assays indicated that GPTP-3 could markedly promote the secretion of NO, TNF-α, IL-1β and IL-6 in murine macrophage RAW264.7. TLR4 was found to be a recognized target of GPTP-3. Besides, TLR4-related mitogen-activated protein (MAPK) and phosphoinositide 3-kinase (PI3K)/Akt, including ERK, JNK, p38 and Akt, were rapidly activated by GPTP-3 in RAW264.7 cells. Moreover, GPTP-3 was found to induce the nuclear translocation of NF-κB subunit p65. All these findings suggest that MAPK, PI3K/Akt and NF-κB pathways are involved in GPTP-3-induced macrophages activation, and GPTP-3 has the potential to be developed as a functional food with immunomodulatory function.
Gynostemma pentaphyllum is a popular functional food, and it is also used as a traditional medicine in Asia. In this study, five previously undescribed triterpenes, gypensapogenin M, gypensapogenin N, gypensapogenin O, gypensapogenin P, and gypensapogenin Q, together with five known compounds were isolated from the hydrolyzate of total G. pentaphyllum saponins. The bioassay data showed that all the triterpenes exhibited significant protective activity against H2O2-induced myocardial cell injury and anti-hepatic fibrosis activity. Taken together, the discovery of these triterpenes from the hydrolyzate of total G. pentaphyllum saponins expands its use as a functional food for preventing myocardial injury and liver fibrosis.
Thailand is predominantly an agriculture-based country. Organic farming is enlisted as an important national agenda to promote food safety and international export. The present study aimed to determine the concentrations of trace elements in commercial organic fertilizers (fermented and nonfermented) composed of pig and cattle manures available in Thailand. Pig and cattle manures as well as animal feeds were also collected from either animal farms or markets. The results were compared to the literature data from other countries. Fermented fertilizer composed of pig manure contained higher concentrations of nitrogen (N) and phosphorus (P) than fertilizer composed of cattle manure. High concentrations of copper (Cu) and zinc (Zn) were also found in fertilizers and manures. Some organic fertilizers had high concentrations of arsenic (As), cadmium (Cd), and lead (Pb). The range of As concentration in these fertilizers was 0.50-24.4 mg/kg, whereas the ranges of Cd and Pb were 0.10-11.4 and 1.13-126 mg/kg, respectively. Moreover, pig manure contained As and Cd (15.7 and 4.59 mg/kg, respectively), higher than their levels in cattle manure (1.95 and 0.16 mg/kg, respectively). The use of pig manure as soil supplement also resulted in high Cd contamination in herbal tea (Gynostemma pentaphyllum Makino; GP). The Cd concentration in GP plants positively correlated with the Cd concentration in the soil. Therefore, the application of some organic fertilizers or animal manures to agricultural soil could increase some potentially toxic elements in soil, which may be absorbed by plants and, thus, increase the risk of contamination in agricultural products.
Extracts of Moringa oleifera Lam. (Moringaceae), a medicinal plant used in complementary and alternative medicine for the treatment of diverse ailments, were studied for antiviral activity on poliomyelitis virus. The dried and powdered leaves of the plant, Moringa oleifera, were extracted with methanol, water and petroleum ether using standard methods. Cytotoxicity of the extracts was evaluated using the end-point cytopathic effect assay on L20B cell lines. Phytochemical evaluations of the extracts were also carried out. The poliovirus was titrated and determination of the 50% tissue culture infective dose (TCID50) done on L20B cells. Antiviral properties were determined against the three sero-types of poliovirus (SL1, SL2 and SL3) using the end-point cytopathic effect assay on L20B cell lines. Phytochemical analysis of the extracts revealed the presence of saponins, alkaloids, glycosides, tannins, flavonoids, carbohydrates, reducing sugar, resins, fats and oil, acidic compounds and proteins. Poliomyelitis viral infectivity was inhibited by the extracts giving a range of specificity indices of 2.47 - >125. This shows that the extracts selectively inhibited the virus and that their activity against the virus was not just a consequence of toxicity to the cells. The research has shown that the plant possesses potent antiviral potentials and could serve as a possible source of lead antiviral drug against poliomyelitis since the disease has no known drug for treatment.
In order to discover ingredients for wrinkle-care cosmetics, we prepared 70% ethanol extract from Gynostemma pentaphyllum and examined its activity on collagen synthesis using fibroblast HDFn cells. The G. pentaphyllum extract induced the production of type I procollagen in a dose-dependent manner without showing cell toxicity. The active constituents were isolated from the extract by solvent fractionation and chromatographic purification procedures. NMR data and literature studies led to determine the two isolated compounds as the flavonoid glycosides such as ombuine 3-O-rutinoside (1) and quercetin 3-O-rutinoside (2). The activity screening tests showed that the isolates 1 and 2 induced the production of type I procollagen in a dose-dependent manner. These results suggested that G. pentaphyllum extract containing the flavonoids 1 and 2 could be useful as an active ingredient for wrinkle-care cosmetics.
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.
The present study examined the effects of crude Polysaccharide from Gynostemma pentaphyllum (PGP) against oxidative stress induced by swimming exercise. Male rats were administered PGP (50, 100, 200 and 400 mg kg -1) by gavage every day. After 30 days, swimming exercise of rat was performed in acrylic plastic pool. The results showed that PGP treatment prolonged exhaustive swimming time and improved liver glycogen reserve which suggested that PGP treatment influenced the performance of exhaustive exercise and improved exercise tolerance. Moreover, PGP treatment can promote increases in the activities of Super Oxide Dismutase (SOD), Catalase (CAT) and Glutathione Peroxidase (GPH-Px) and reduce lipid per-oxidation which suggest that PGP treatment was beneficial in enhancing the antioxidant status and inhibiting oxidative stress induced by exhaustive exercise.
In the present study, we investigated the neuroprotective effects of GPP1, a purified polysaccharide from Gynostemma pentaphyllum, on Aβ (25-35)-induced neuronal toxicity and explore its potential mechanisms in PC12 cells. The results showed pretreatment with GPP1 prior to Aβ (25-35) exposure significantly protected PC12 cells from Aβ (25-35)-induced cell death, lactate dehydrogenase (LDH) release, DNA damage, intracellular free calcium concentration ([Ca(2+)]i) influx, mitochondrial dysfunction and mitochondrial cytochrome c (Cyt-C) release. In addition, pretreatment with GPP1 also protected PC12 cells against Aβ (25-35)-induced the accumulation of reactive oxygen species (ROS) and lipid peroxidation product MDA, the reduction in glutathione (GSH) level and superoxide dismutase (SOD) activity, the increased Bax/Bcl-2 protein expression ratio and caspase-3 activation. Our findings suggest that GPP1 exerts a neuroprotective effect against Aβ (25-35)-induced neurotoxicity in PC12 cells, at least in part, via inhibiting oxidative stress and suppressing the mitochondrial apoptotic pathway.
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Jiaogulan (Gynostemma Pentaphyllum) is age old herb in traditional Chinese herbology. It has been widely researched. It is true Rasayan (Rejuvenator / Antiaging) herb as it is immunomodulator, adaptogen, antioxidant, anti-cancer, neuroprotective, nootropic and hepatoprotective. The only one Rasayan therapeutic activity about which there was no research reference is aphrodisiac.
Heat-processed Gynostemma pentaphyllum and its main dammaran-type saponins, gypenoside L, gypenoside LI, damulin B, and damulin A, possess non-small cell lung carcinoma A549 cell inhibitory activity. We established in this study a method by ultra-high performance liquid chromatography with tandem mass spectrometry for determination of the saponins and also investigated their content change in heat-processed G. pentaphyllum. The main saponins increased with increasing heating temperature and time. Further investigation showed that they were produced from gypenoside XLVI and gypenoside LVI by undergoing hydrolysis during the heat treatment.
The aim of the present study was to explore the neuroprotective effects of Gynostemma pentaphyllum polysaccharides (GP) in a 1-methyl-4-phenylpyridiniumion (MPP(+))-induced cellular model of Parkinson's disease (PD) and the underlying mechanisms. Our results indicated that exposure of PC12 cells to 1mM MPP(+) significantly decreased the cell viability when examined by MTT assay, LDH assay, and annexin-V-FITC and propidium iodide (PI) apoptosis detection assays. MPP(+)-induced apoptosis in PC12 cells was accompanied by an increased Bax/Bcl-2 ratio, release of mitochondrial cytochrome c into the cytosol, activation of caspase-3/9 and cleavage of poly (ADP-ribose) polymerase (PARP). However, pretreatment of PC12 cells with 50μg/ml GP prior to MPP(+) exposure effectively attenuated the cytotoxicity and improved cell viability via inhibiting elevated Bax/Bcl-2 ratio, as well as the release of cytosolic cytochrome c. Furthermore, GP was effective in attenuating caspase-3/9 activation and cleavage of PARP in MPP(+)-exposed PC12 cells. These results suggest that the GP has protective effects against MPP(+)-induced neuronal apoptosis in PC12 cells by suppressing apoptosis-related protein, and therefore, might likely be a promising candidate for the treatment of Parkinson's disease (PD).
A neutral polysaccharide fraction (CGPP) was extracted from Gynostemma pentaphyllum by water extraction and ethanol precipitation. Gas chromatography (GC) analysis showed that the CGPP was mainly composed of mannose, glucose, arabinose, rhamnose, galactose and glucuronic acid in molar ratios of 2.0:2.2:1.3:2.2:1.2:2.5. The present study aimed at evaluating the antitumor potentials of CGPP on the growth of H22 tumor transplanted in mice and the underlying mechanism. The results showed that CGPP (50 and 200mg/kg) could effectively inhibit the solid tumor growth of H22 hepatocarcinoma transplanted in ICR mice. Besides, the body weight, spleen/thymus indexes and splenocytes proliferation of H22 tumor bearing mice were also improved in CGPP-treated groups. Furthermore, the level of the cytokines, such as IL-2, TNF-α and IFN-γ, as well as the activity of natural killer (NK) cells and cytotoxic T lymphocytes (CTL) in tumor-bearing mice were markedly promoted by CGPP oral administration. In addition, CGPP treatment greatly prolonged the survival period in H22 ascites tumor-bearing mice. Taken together, these findings indicate that CGPP has antitumor activity in vivo at least partly via improving immune responses of host organism, and seems to be a safe and effective supplementary agent for the treatment of hepatocellular carcinoma (HCC).
A novel polysaccharide (GPP-S), with a molecular mass of 1.2×106 Da, was isolated from the tetraploid Gynostemma pentaphyllum Makino by alkali extraction followed by purifications using DEAE and Sephacryl S-400 column chromatographies. The monosaccharide composition of GPP-S was determined as rhamnose, arabinose, glucose and galactose with a molar ratio of 1.00:3.72:19.49:7.82. The structural analysis suggested that the backbone of GPP-S is (1→4)-linked-glucose and (1→6)-linked-galactose with a (1→4, 6) - linked-glucose branch every six monosaccharide residues. The terminals were 1- )-α- arabinose, glucuronic acid and other monosaccharides. GPP-S exhibited scavenging capacities against hydroxyl, peroxyl and DPPH• radicals in vitro. GPP-S also had inhibitory activities on IL-1β, IL-6 and COX-2 gene expressions in RAW 264.7 mouse macrophage cells. These results suggested that GPP-S could be developed as a bioactive ingredient for functional foods and dietary supplements.
The water-soluble crude polysaccharide GM, obtained from the Gynostemma pentaphyllum Makino by boiling-water extraction and ethanol precipitation, was fractionated by DEAE–Sepharose CL-6B column chromatography, and purified by Sephadex G-100 column chromatography, giving three polysaccharide fractions termed GMA, GMB and GMC. The monosaccharide components of them were studied by PC and GC. On the basis of superoxide radical assay, hydroxyl radical assay and self-oxidation of 1,2,3-phentriol assay, the antioxidant activities of GM, GMA, GMB and GMC were investigated. Among these contents, GMC had the higher scavenging effects on superoxide radicals and inhibitory effects on self-oxidation of 1,2,3-phentriol, and so should be explored as a novel potential antioxidant.
The exhumation history of the central Himalaya is well documented, but lateral variations in exhumation remain poorly constrained. In this study, we identify sediment source areas and examine the late Neogene exhumation history of the eastern Himalaya from the synorogenic sedimentary record of its foreland basin. We present Nd and Hf isotopic data as well as apatite and zircon fission-track analyses from the Miocene–Pliocene Siwalik Group along the recently dated Kameng River section in Arunachal Pradesh, northeastern India. Our isotopic data show that Siwalik Group sediments deposited between 13–7 and <2.6 Ma in Arunachal Pradesh were mainly derived from Higher Himalayan source rocks. In contrast, sediments deposited between ca. 7 and 3 Ma have far less negative εNd and εHf values that require involvement of the Gangdese Batholith and Yarlung suture zone source areas via the Brahmaputra River system. Consequently, these sediments should also record incision of the Namche Barwa massif by this river. Source-area exhumation rates of Himalayan-derived sediments, determined from detrital zircon fission-track data, were on the order of 1.8 km/m.y. in the fastest-exhuming areas. These rates are very similar to those calculated for the central Himalaya and have been relatively constant since ca. 13 Ma. Our results do not support the hypothesis of a major change in exhumation rate linked to either local or regional climate change or to Shillong Plateau uplift during the Miocene, as reported elsewhere. The zircon fission-track data further suggest that exhumation of the Namche Barwa massif between 7 and 3 Ma was much slower than the ∼10 km/m.y. rate recorded in the recent past. Detrital apatite fission-track data indicate deformation of the Siwaliks due to forward propagation of the frontal thrust since around 1 Ma.
To differentiate the sweet and bitter taste variants of a Chinese medicinal tea Gynostemma pentaphyllum (GP), a method for the quantitative analysis of ginsenosides Rb1, Rb3, Rd and F2 in GP by using UPLC-Q-TOF-MS was developed. According to the different contents of the four ginsenosides, chemical differentiation of the two taste variants of GP was achieved by principal components analysis (PCA). A supplementary quantitative analysis method of using HPLC-ELSD for determination of 20(S)-panaxadiol in the hydrolysates of GP was also developed. Similarly, chemical differentiation based on different amounts of 20(S)-panaxadiol was established and the result was well consistent with that based on the analysis of the four ginsenosides. It was found that the amounts of the four ginsenosides and 20(S)-panaxadiol in the sweet taste variant were significantly higher than those in the bitter one. The significant difference between the sweet and bitter taste variants of GP was easily visualized in 3D-PCA score plots. The PCA loading plot also indicated the contributions among the four ginsenosides (Rd > Rb3 > F2 > Rb1) for distinguishing the two taste variants. This is the first report to describe the use of these two quantitative methods (UPLC-Q-TOF-MS and HPLC-ELSD) for the accurate authentication and quality control of GP.
Two kinds of core-shell structured multifunctional nanocarriers of gold nanoclusters (Au NCs) as core and folate (FA)-conjugated amphiphilic hyperbranched block copolymer as shell based on poly(l-lactide) (PLA) inner arm and FA-conjugated sulfated polysaccharide (GPPS-FA) outer arm (Au NCs-PLA-GPPS-FA) were synthesized for targeted anticancer drug delivery. The structure and properties of Au NCs-PLA-GPPS-FA copolymers were characterized and determined by (1)H NMR spectrum, FT-IR spectra, dynamic light scattering (DLS), fluorescence spectroscopy, and transmission electron microscopic (TEM) analyses. The anticancer drug, camptothecin (CPT) was used as a hydrophobic model anticancer drug. In vitro, two kinds of the nanocarriers presented a relatively rapid release in the first stage (up to 1 h) followed by a sustained release period (up to 15 h), and then reached a plateau at pH 5.3, 7.4, and 9.6. The release results indicated that CPT release from two kinds of the nanocarriers at pH 9.6 was much greater than that at both pH 5.3 and 7.4. The cytotoxicity studies showed that the CPT-loaded nanocarriers provided high anticancer activity against Hela cells. Furthermore, nanocarriers gained specificity to target some cancer cells because of the enhanced cell uptake mediated by FA moiety. The fluorescent images studies showed that the nanocarriers could track at the cellular level for advance therapy. The results indicated that the Au NCs-PLA-GPPS-FA copolymers not only had great potential as tumor-targeted drug delivery carrier, but also had an assistant role in the treatment of cancer.
A native polysaccharides (GPP2) was isolated from Gynostemma pentaphyllum Makino. Four sulfated derivatives of GPP2 (GPP2-s1 to s4) were prepared by chlorosulfonic acid method with ionic liquids (ILs) as solvent and 4-dimethylaminopyridine (DMAP) as catalyst. The structures of the sulfated derivatives were analyzed by FT-IR spectra and 13C NMR spectra, which indicated that the sulfated groups were introduced mainly at the C-6 position as well as at the C-2 position. The products showed different degree of substitution (DS) ranging from 0.79 to 1.34, and different weight-average molecular mass (Mw) ranging from 8.64 to 11.2 Da. The sulfated derivatives inhibited the growth of HepG2 cells and Hela cells in vitro significantly. Furthermore, they had no obvious influence on 293 cells, which indicated that they had low toxicity. Flow cytometric studies revealed that treatment of the sulfated derivatives with Hela cells could mediate the cell-cycle arrest in the S phase.
Uniform Design was used to optimize the effects of processing parameters of extraction from Gynostemma pentaphyllum Makino on the yield of polysaccharides. Four independent variables such as extraction time (min), solid:liquid ratio (g/ml), immersing time (min), and extraction temperature (°C) were study. The optimal conditions were determined and Three-dimensional response surfaces were plotted from the mathematical models. The t-value and p-value indicated that both immersing time and water extraction time (X2X4) had interaction effects on the response value, followed by the linear terms of water extraction time (X4), and the interaction effects of immersing time and water extraction temperature(X2X3). Considering the efficiency, the optimum conditions of polysaccharides extraction were liquid:solid ratio of 1:67, immersing time of 10 min, water extraction temperature of 95 °C, and water extraction time of 15 min. Under optimized conditions, the experimental yield 11.29% agreed closely with the predicted yield. Therefore, application of Uniform Design in the extraction of polysaccharides from Gynostemma pentaphyllum Makino dramatically reduced extraction time.
From an acid hydrolysate of the crude saponins of Gynostemma pentaphyllum, three triterpenes, including a new compound (23S)-3β-hydroxydammar-20,24-dien-21-oic acid 21,23-lactone (1) and two known aglycons (20S, 23R)-3β,20β-dihydroxydamma-24-dien-21-oic acid 21,23-lactone (2) and (20S, 24S)-20,24-epoxydammarane-3β,12β,25-triol (3), were isolated. Their structures were established on the basis of extensive spectral evidence (HR-ESI-MS, IR, 1D and 2D-NMR experiments). In bioactive assays in vitro, compound 1 was found to have potent cytotoxicity against the human breast cancer cells MDA-MB-435, whereas compounds 2 and 3 exhibited modest inhibitory activity toward porcine pancreatic lipase. The results indicated that acid treatment of G. pentaphyllum extract could produce diverse structures with interesting bioactivity.
The crude polysaccharide was obtained from Gynostemma pentaphyllum Makino by water extraction followed by ethanol precipitation. The polysaccharide was successively purified by chromatography on DEAE-52 and SephadexG-150 column, and three polysaccharide fractions were obtained and termed GPP1-a, GPP2-b, and GPP3-a, respectively. The administration with GPP1-a markedly prolonged exhaustive exercise time of the mice. Structural features of GPP1-a were investigated by a combination of instrumental and chemical analyses, including atomic force microscope (AFM), scanning electron microscope (SEM), partial acid hydrolysis, periodate oxidation, Smith degradation, methylation analysis, gas chromatography–mass spectrometry (GC–MS) analysis and NMR spectroscopy. The results indicate that GPP1-a has a backbone of (1 → 4)-linked α-d-Glucose residues, which occasionally branches at O-6. The branches are mainly composed of (1 → 6)-linked α-d-Glucose, (1 → 3)-linked β-d-Galactose and (1 → 6)-linked α-d-Galactose residues, and terminated with β-d-Galactose residues and β-l-Arabinose residues.
A reversed-phase high-performance liquid chromatographic (HPLC) method is described for the simultaneous determination of aldoses and uronic acids. The separation was carried out on a RP-C18 column (4.6 mm i.d. × 250 mm, 5 μm, Venusil, USA) using precolumn derivatization with 1-phenyl-3-methyl-5-pyrazolone (PMP) and UV detection at 250 nm, and the 10 PMP derivatives of mannose, ribose, rhamnose, glucuronic acid, galacturonic acid, glucose, xylose, galactose, arabinose and fucose were baseline separated within 40 min. Furthermore, the described method was applied to the quantitative analysis of component monosaccharides in the water-soluble polysaccharides extracted from Gynostemma pentaphyllum Makino tea and the result showed that the tea polysaccharide was a typical heteropolysaccharide and consisted of mannose, ribose, rhamnose, glucuronic acid, galacturonic acid, glucose, xylose, galactose and arabinose in the molar contents of 16.3, 10.3, 47.1, 5.6, 24.0, 128.4, 25.0, 101.4 and 71.1 μM, respectively. Quantitative recoveries of the component monosaccharides in the tea polysaccharide were in the range of 94.6–108.0% and the RSD values were lower than 4.9%. The results demonstrated that the proposed HPLC method was precise and practical for the analysis of the G. pentaphyllum tea polysaccharide.
Water-soluble polysaccharide from Gynostemma pentaphyllum herb tea (PSGP) was isolated by hot-water extraction and ethanol precipitation. The chemical components and preliminary immunomodulating activity of PSGP were investigated both in vitro and in vivo. Capillary zone electrophoresis analysis showed that PSGP was a typical nonstarch heteropolysaccharide, with glucose being the main component monosaccharide (23.2%), followed by galactose (18.9%), arabinose (10.5%), rhamnose (7.7%), galacturonic acid (4.7%), xylose (3.9%), mannose (3.1%), and glucuronic acid (1.2%). PSGP could significantly stimulate peritoneal macrophages to release nitric oxide, reactive oxygen species, and tumor necrosis factor-alpha in a dose-dependent manner. This immunostimulating activity of PSGP was further demonstrated by its inhibition on the proliferation of human colon carcinoma HT-29 and SW-116 cells incubated with the supernatant of PSGP-stimulated macrophage culture. It is evident that PSGP is a very important ingredient responsible for at least in part the immunomodulating activity of G. pentaphyllum herb tea.
Gynostemma pentaphyllum was investigated to determine its antimicrobial activities against human.and animal pathogens that produce aflatoxin, fumonisin, and diarrheal disease. The fungi were Aspergillusflavus, Aspergillus parasiticus and Fusarium verticillioides. The bacteria were Vibrio, Salmonella, Shigella, Escherichia coli and Staphylococcus aureus. G. pentaphyllum was extracted by five different methods. The obtained extracts were designated Extracts A, B, C, D and E. The results of the antifungal assay against A.flavus andA. parasiticus showed Extracts A and B at 10,000 ppm inhibited growth at 8-28%. Extracts A and B at 10,000 ppm also showed activity against F. verticillioides at 41-43%. Extract A, B and C were able to inhibit the tested strains better than the Extracts D and E. The MIC values of the extracts against gram-negative bacteria ranged from <or=0.98 to 31.25 mg/ml and MIC values against S. aureus, a gram-positive bacteria, was 3.9-15.62 mg/ml. G. pentaphyllum extracts had activity against bacterial and fungal infections and could be used to control these organisms.
New saponins, named gypenosides I (1), II (2), V (5), VI (6), VII (7), IX (9), X (10), XI (11), XIII (13), XIV (14), besides the known ginsenosides-Rb1 (3), -Rb3 (4), -Rd (8) and -F2 (12), were isolated from Gynostemma pentaphyllum MAKINO. On enzymatic hydrolysis, all saponins yielded 20-O-β-D-glucopyranoside of 20 (S)-protopanaxadiol (compound K) as a prosapogenin. The configuration of the sugar linkages in each saponin was established on the basis of chemical and spectroscopic evidence.
6"-Malonylginsenosides-Rb1, (6), -Rd (7) and 6"-malonylgypenoside V (8) were isolated from the fresh leaves of Gynostemma pentaphyllum selected from wild plants. It was found that the saponin content of dry leaves was markedly reduced because of decomposition of saponins, by intracellular glycosidases.
New saponins, named gypenosides XV (1), XVI (2), XVII (3), XVIII (4), XIX (5), XX (6) and XXI (7) were isolated from Gynostemma pentaphyllum MAKINO. On enzymatic hydrolysis, 1, 2, and 3 yielded 20-O-β-D-glucopyranoside of 20 (S)-protopanaxadiol (compound K) (8), and 4, 5, 6 and 7 afforded 20-O-β-D-glucopyranoside of dammar-24-ene-3β, 12β, 20 (S), 26-tetraol (9) as a prosapogenin. The configuration of the sugar linkages in each saponin was established on the basis of chemical and spectroscopic evidence.
The antiulcerogenic effect of aescine was studied on cold restraint, pylorus-ligated and absolute ethanol induced ulcers in comparison to ranitidine and carbenoxolone. Gastric mucus output, total protein and hexosamines content were measured, In pyloric-ligated animals, acidity, as well as biochemical assay of pepsin, histamine, sodium and potassium electrolytes were also determined. Oral treatment with aescine was found to be effective in the prevention of gastric ulceration induced by absolute ethanol, although mucus secretion was not enhanced. In pyloric-ligated animals aescine showed a considerable reduction in the number and severity of ulcers. A significant reduction in gastric secretion was also observed.
1.1. [i14C]Glucosamine incorporation into acid-precipitable glycoprotein by intestinal slices was linear for 5 h, maximal at 18 mM medium glucosamine concentration, and temperature dependent. Incorporation was enhanced by bicarbonate, l-glutamine, sodium-l-glutamate and inhibited by phosphate, glucose and pyruvate present in the incubation medium.2.2. The acid-soluble intermediate pattern was similar at i, 3 and 5 h. Radioactivity in UDP-N-acetylhexosamines accounted for less than 10% of the total acid-soluble radioactivity. N-Acetylhexosamine was labelled in preference to glucosamine 6-phophate.3.3. Preincubation for 15 min with 10−4 M cycloheximide protein synthesis by 92% and glucosamine incorporation by 60%. This residual glucosamine incorporation was unaffected by greater concentrations of cycloheximide or prolonged preincubation.4.4. Transfer of acid-precipitable label from microsomes to brush border occurred between 1 and 3 h of incubation. Soluble labelled glycoprotein with chromatographic properties of secreted glycoprotein was present in the medium surrounding the slices at i h and to a greater extent at 3 h.5.5. These results indicate that intestinal slices synthesize glycoprotein as well as incorporate glucosamine independently of protein synthesis. Intracellular transport of plasma membrane glycoproteins and glycoprotein secretion take place in vitro.
The correlation between acid secretion and mucosal blood flow in the rat stomach during stress loading was determined to provide clues to the etiology of the gastric ulceration which thus occurs. The gastric acid output was increased remarkably by water-immersion stress at 23 degrees C, and this increase lasted while the stress was given, yet the mucosal blood flow did not show a corresponding increase. In rats stressed for 3 hr, ulcerative changes were observed in the glandular portion of the stomach. The stress-induced increase in acid output correlated well with the severity of erosions. Pretreatment of animals with atropine 10 microgram/kg, given subcutaneously, or vagotomy, inhibited the increase in acid output and also inhibited the ulcer formation caused by the stress: however, the mucosal blood flow in these animals decreased significantly. These results suggest that when there is an elevation of gastric acid secretion with no parallel increase in mucosal blood flow, gastric ulceration may occur under conditions of stress.
Oral administration to fasted rats of either absolute ethanol, 0.6 N hydrochloric acid, 0.2 N sodium hydroxide, 25% sodium chloride, or boiling water produced extensive necrosis of the gastric mucosa. Pretreatment with several prostaglandins of the A, E, or F type, either orally or subcutaneously, prevented such necrosis, and the effect was dose-dependent. This property of prostaglandins is called "cytoprotection." The protective effect against oral administration of absolute ethanol was already maximal 1 min after PGE2 given orally, and 15-30 min after PGE2 given subcutaneously. Cytoprotection by prostaglandins is unrelated to the inhibition of gastric acid secretion since, (a) it is maximal at doses that have no effect on gastric secretion, and (b) anti-secretory compounds (cimetidine, methscopolamine bromide) and antacids are not cytoprotective. Although the mechanism of gastric cytoprotection is unknown, prostaglandins appear to increase the resistance of gastric mucosal cells to the necrotizing effect of strong irritants. These results suggest that certain prostaglandins, by a mechanism other than the inhibition of gastric acid secretion, maintain the cellular integrity of the gastric mucosa, and might be beneficial in the treatment of a variety of diseases in which gastric mucosal injury is present.
The effects of ginger, a pungent stomachic natural medicine, on HCl/ethanol-induced gastric lesions in rats, were examined. The orally administered acetone extract at 1000 mg/kg and zingiberene, the main terpenoid from acetone extract, at 100 mg/kg significantly inhibited gastric lesions by 97.5 and 53.6%, respectively. 6-Gingerol, the pungent principle, at 100 mg/kg significantly inhibited gastric lesions by 54.5%. These results suggest that zingiberene, the terpenoid and 6-gingerol are important constituents in stomachic medications containing ginger.
The effects of verapamil on gastric wall mucus and ulceration were studied in rats which were restrained and exposed to 4 degrees C (stress). Stress for 2 h significantly depleted stomach wall mucus and produced marked gastric glandular ulcers. Verapamil pretreatment (2, 4, 8 or 16 mg/kg), injected intraperitoneally 30 min before experimentation, significantly prevented stress-induced mucus depletion and gastric ulceration; however, it did not itself influence stomach wall mucus levels in nonstressed animals. Intragastric administration of carbenoxolone (100 or 200 mg/kg), also given 30 min before stress, exhibited similar actions as verapamil. A 15% solution of N-acetylcysteine (10 ml/kg), given orally, strongly decreased the mucus content in both nonstress and stress conditions; it induced ulcers in nonstressed rats, and worsened stress ulceration. These effects were not reversed by verapamil pretreatment. The influence of multiple-dose pretreatment with verapamil or carbenoxolone on mucus content and ulceration in the gastric glandular mucosa during stress is also discussed. It is concluded that gastric wall mucus depletion is likely to play an important role in stress ulcer formation; the antiulcer action of verapamil could partly be due to the preservation of mucus.
The interrelationships of core body temperature, blood viscosity, gastric mucosal blood flow, surface pH of the corpus mucosa, and acute gastric mucosal lesions in rats after up to 3 h of hypothermic stress were investigated. Three groups of rats were studied: (a) control rats restrained at room temperature, (b) conscious rats under restraint and varying degrees of hypothermia, and (c) anesthetized rats under hypothermia. Under hypothermic stress both restrained and anesthetized rats manifested a sharp decline in core temperature, a marked increase in blood viscosity with a mirror-image decrease in gastric mucosal blood flow, a significant decline in gastric mucosal surface pH, and similar frequencies and severities of acute gastric mucosal lesions. In the control group, neither mucosal lesions nor changes in physiologic measurements were observed, except for a decline in mucosal surface pH. An increase in blood viscosity identical to that in rats subjected to hypothermia was observed in vitro when blood temperature was lowered in the viscometer. These findings indicate that hypothermia but not restraint led to an increase in blood viscosity, which in turn resulted in a decrease in mucosal blood flow and the development of gastric mucosal lesions. Also, hyperacidity was found to be a permissive factor in the pathogenesis of mucosal lesions.
It was found that dammarane-saponin composition of rhizomes of Panax japonicus C. A. MEYER collected in Miyazaki-ken, Kyushu (South-West Province of Japan) was remarkably different from that of specimens (Japanese name : Chikusetsu-ninjin) collected at other places in Japan. From rhizomes of this specimen (local name : "Satsuma-ninjin"), four biologically active major dammarane-saponins of Ginseng roots, ginsenosides-Rg1 (11), -Re (12), -Rc (16) and -Rb1 (17) and two dammarane-saponins of Sanchi-Ginseng, notoginsenosides-R1 (13) and -R2 (9) as well as gypenoside-XVII (14) were isolated together with the saponins of oleanolic acid (1), chikusetsusaponins-IV (3) and -V (5), both of which have already been isolated from Chikusetsuninjin. From Chikusetsu-ninjin, none of 9, 11, 12, 13, 14, 16 and 17 has been isolated, while in "Satsuma-ninjin, "chikusetsusaponins-Ia (6), -III (7), which are the characteristic dammaranesaponins of Chikusetsu-ninjin, were not identified. The present isolation of the major dammarane-saponins of Ginseng roots from "Satsumaninjin"in relatively high yields is significant not only from the viewpoint of the geographical relation of Japanese P. japonicus with Chinese and Himalayan Panax spp. but also from the viewpoint of the pharmacological importance of this specimen in oriental traditional medicine.
Alterations in gastric mucosal hemodynamics during the development of restraint-induced gastric erosions in the rat were studied using the indicator fractionation technic with86Rb. Cardiac output, gastric flow fractions and gastric blood flow were determined in rats subjected to zero (control), 1/2, 4 and 24 hours of restraint. No correlation was found between gastric mucosal blood flow changes and the natural development of restraint erosions. The possible role of local microcirculatory adjustments, independent of total mucosal flow, in the genesis of restraint lesions is discussed.
The effects of natural and synthetic detergents (sodium taurocholate, bile, decyl sulfate) and urea in breaking the gastric mucosal barrier were studied by irrigating the separated, vagally denervated pouches of the oxyntic glandular area of the dog stomach first with a test solution of 100 mm HCl + 54 mm NaCl, then with a solution of the detergent or urea, and again with the acid test solution. Fluxes of Na⁺, K⁺, and H⁺ were measured, and changes over the control fluxes were taken as evidence that the barrier had been broken. Bile salts (10, 20, and 40 mm in neutral solution, 40 mm in a liquid meal, and 10 mm in acid solution), decyl sulfate (10 or 20 mm in neutral solution), and urea (1, 2, and 4 lvt in neutral solution) all break the gastric mucosal barrier.
The participation of polyamines and nonprotein sulfhydryls in the gastric cytoprotective mechanisms was studied using gastric mucosal lesions produced by acidified ethanol in rats as an experimental model. Treatment with prostaglandin E2 (PGE2), but not cimetidine, prevented the formation of gastric mucosal lesions. Oral administration of cadaverine, spermidine and spermine prevented the lesion formation by acidified ethanol in a dose-dependent manner. Indomethacin or acetazolamide had no influence on the cytoprotective effect of spermine, whereas sulfhydryl blockers such as iodoacetamide and N-ethylmaleimide partially blocked it. Sulfhydryl compounds such as cysteine, reduced glutathione (GSH), and cysteamine prevented the lesion formation induced by acidified ethanol. The concentration of nonprotein sulfhydryls in the gastric mucosa was significantly decreased at 1 hr after administration of acidified ethanol, and this decrease was partially prevented by spermine or PGE2. These results suggest that the cytoprotective effect of spermine may not be mediated by endogenous prostaglandins or alkaline secretion in the gastric mucosa, but may be partially related to endogenous sulfhydryl compounds.
Human fundic mucosa generates various prostaglandins (PGs), particularly PGE2, and tromboxanes. This generation appears to be significantly lower in gastric ulcer patients than in duodenal ulcer patients or normal subjects. Nonsteroidal antiinflammatory compounds (NOSAC), such as aspirin or indomethacin, greatly reduce the PG biosynthesis and cause mucosal damage, including mucosal erosions and hemorrhages observed at endoscopy, increased gastric microbleeding and DNA loss. In contrast, paracetamol or carprofen, a novel NOSAC, fails to affect mucosal generation of PGs and does not influence gastric mucosal integrity. This study indicates that endogenous PGs may be involved in the pathogenesis of gastric ulcer and that normal generation of mucosal PGs is essential for the mucosal integrity.
Indomethacin produces gastric corpus erosions in the fasted rat and small intestinal ulcers in the conventionally fed rat. We found that in rats fed chow pellets for 1 h after a 24-h fast, indomethacin given within 2 h after refeeding produced lesions in the gastric antrum, primarily along the lesser curvature, and also in the small intestine. The antral lesions reached a maximum size in 6-10 h, penetrated the muscularis mucosae within 3 days, and did not diminish for at least 7 days. The formation of the antral ulcer was prevented by prostaglandins or adrenalectomy, but was not affected by cimetidine, atropine, and/or vagotomy. In contrast, the gastric corpus erosions produced by indomethacin in the fasted rat were prevented by antisecretory drugs or vagotomy, and were aggravated by adrenalectomy. It is concluded that: (a) the chronic antral ulcers produced by indomethacin in a refed rat mimic human gastric ulcer with regard to location and histology; and (b) the mechanism of antral ulcer formation is different from corpus erosion formation, in that it was resistant to antisecretory drugs and vagotomy and was prevented by adrenalectomy. This experimental ulcer model could prove useful for studies of the etiology and therapy of gastric ulcer disease.
Four main dammarane-type aglycones of gypenosides, extracted from the aerial parts of Gynostemma pentaphyllum were identified by gas chromatography-mass spectrometry. By detecting these aglycones as well as the aglycones of ginsenosides, a difference in sapogenin composition between Gynostemma pentaphyllum and Panax species was observed, which can be used in the differentiation of these plant drugs.
A simple and reliable method for production of gastric ulcer on rats by stress was described. Rats fixed on boards were immersed in water of 25°to the depth of xiphoide. After 20 hours, marked gastric erosions were found in the glandular portion of the stomach. This stress is more favourable than other stresses as cold, restraint, or emotional stress by stress box in view of incidence and mortality. Anticholinergics or central depressants effectively inhibited the ulceration and combination of both drugs suppressed it more effectively than single administration of each drug.
Gynostemma pentaphyllum
- Cui
- D Glick