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Gastroprotective effects of bitter principles isolated from Gentian root and Swertia herb on experimentally-induced gastric lesions in rats
Abstract
Gentianae Radix, the dried root and rhizoma of Gentiana lutea L. (Gentianaceae), has long been used as a remedy for liver and stomach inflammation, eye troubles, etc. In this paper, the gastroprotective effects of the methanol extract of Gentian root (GM) were studied using different gastric lesion models. In pylorus-ligated rats, administration of GM in the duodenum suppressed gastric juice secretion and total acid output in a dose-dependent manner. Oral or duodenum administration of GM showed significant protection against acute gastric ulcer induced by aspirin plus pylorus ligation, water-immersion restraint stress-induced ulcers, and gastric mucosal injury induced by ethanol. Furthermore, four secoiridoid glycosides, amarogentin (A1), gentiopicroside (A2), amaroswerin (A3), and swertiamarin (A4), were obtained from Gentian root or Swertia herb, and their protective effects against stress-induced ulcers and ethanol-induced gastric mucosal injury were evaluated. The doses required for 50% inhibition (ID50) of A1, A3, and A4 on stress-induced ulcers were calculated to be 5.76, 2.58, and 167mg/kg respectively. The protective effect of A2at 250mg/kg was 26.5%. On ethanol-induced gastritis, 5.0mg/kg of A1 and A3 showed remarkable suppressive effects (33.7 and 45.4%, respectively), and 20mg/kg of A4 exhibited a suppressive effect (30.8%). The effects of A1, A3, and A4 on ethanol-induced gastric lesions were canceled by 5.0mg/kg indomethacin pretreatment. These results suggest that the therapeutic effects of Gentian root on gastric lesions are associated with enhanced mucosal defensive factors via the prostaglandin pathway in the cell membrane, and that secoiridoid glycosides contribute to this activity.
... It is a Secoiridoid glycoside collected from Swertia chirayita and found to be gastro-shielding (Niiho et al., 2005). ...
... Amaroswerin Gastro-shielding [Niiho Y et al., 2005]. [Niiho et al., 2005]. ...
... Amaroswerin Gastro-shielding [Niiho Y et al., 2005]. [Niiho et al., 2005]. ...
... Many plant extracts of this genus have been investigated for their medicinal potential and have been shown to be quite successful [18], but there is a lack of scientific evidence of S. chirayita against GI disorders. Polyhydroxylated xanthones, including chiratogenin, amarogenin, isobellidifolin, mangiferin, swerchirin, swertinin, amarogentin, gentiopicroside, and swertiamarin, are reported to be present in this species along with several additional components [19,20], out of which amarogentin, amaroswerin and swertiamarin have been reported to have a gastroprotective effect [21]. In light of existing literature, S. chirayita has been reported as an Ayurvedic plant [22]. ...
... The pharmacological efficacy of S. chirayita has been partly attributed to the biological activity of major phytoconstituents, including amarogentin, swertiamarin, mangiferin, swerchirin, sweroside, amaroswerin, and gentiopicrin [15]. In addition, amarogentin, amaroswerin, and swertiamarin isolated from S. japonica herb were reported to have gastroprotective efficiency with percentage inhibitions of 33.7%, 45.4%, and 30.8% at 20 mg/kg dose towards ethanol-induced gastric lesions in Wistar rats [21]. There is still some lack of clinical evidence and scientific validation of this species. ...
Gastrointestinal (GI) disorders encompassing conditions such as gastritis, peptic ul-cers, and inflammatory bowel disorders are major global health concerns affecting millions worldwide. Conventional treatment options often come with undesirable side effects, prompting the search for alternative therapies. The herb's influence on digestive processes, mucosal protec-tion, and modulation of gut microbiota shed light on maintaining potential GI health. Swertia chirayita (Gentianaceae), commonly known as 'Chirata', is a traditional medicinal herb that has been used for centuries in various cultures for its therapeutic benefits, particularly for GI ailments. Furthermore, this review highlights several scientific studies and clinical trials that support the traditional uses of S. chirayita in treating GI disorders. In conclusion, S. chirayita could be ben-eficial as a natural remedy with promising therapeutic potential for managing GI disorders. How-ever, there are still some scientific gaps, such as the identification of bioactive compounds, the structure-activity relationship, the mechanistic action of isolated bioactive compounds, the de-velopment of effective analytical methods for comprehensive quality control, and safety profiles, that need to be addressed. Understanding its molecular mechanisms and conducting further clin-ical trials will contribute to establishing S. chirayita as a valuable addition to the armamentarium of natural therapies for GI health.
... It is a Secoiridoid glycoside collected from Swertia chirayita and found to be gastro-shielding (Niiho et al., 2005) [6] . ...
... It is a Secoiridoid glycoside collected from Swertia chirayita and found to be gastro-shielding (Niiho et al., 2005) [6] . ...
... Flowering takes place from the last week of August to the first week of November, with the first two weeks of November being the optimal time for harvesting seeds (Raina et al., 2003). Iridoid glycosides such as gentiopicrine, gentiamarin, amaroswerin, and the alkaloid gentianine are abundant in the root and rhizome (Niiho et al., 2006). The roots contain 20% of a yellow, translucent, and brittle resin known as aucubin, aucubin, catalpol, 6-O-cinnamoyl catalpol (Sarg et al., 1991). ...
... In addition to flavonoid and phenolic content, the root extract contains additional compounds. The iridoid glycosidesamaroswerin, gentiamarin, gentiopicrine, and the alkaloid gentianine come from the roots and rhizomes (Niiho et al., 2006;Singh et al., 2008;Sarg et al., 1991). Dried roots include 20% of yellow, transparent and brittle resin (Sarg et al., 1991), catalpas, 6-o-vanillol catalpol, 6-o-cinnamoyl catalpol and aucubin (Sarg et al., 1990(Sarg et al., , 1991. ...
Gentiana kurroo Royle is an endangered bitter medicinal plant of the Indian subcontinent. This medicinal plant mainly grows in Kashmir, Himachal Pradesh, and North-west Himalayas. The medicinal plant's root and rhizome are frequently used by native people for various local remedies. This species has become critically endangered due to its endemic nature and high rate of extraction from its natural environment. In India rhizome and root of this medicinal plant are used as ant periodic, bitter tonics, anti-inflammatory, blood purifier, expectorant, antipsychotic, carminative, and stomachic. Genitiana kurroo can be propagated through micro-filtration of seeds, rhizome cutting, shoot-made segments, and somatic embryogenesis. The roots of Genitiana kurroo are rich in various ingredients such as flavonoids, alkaloids, and terpenoids which are responsible for analgesic, anticancer, and immune-modular effects. Considering these perspectives, the present review has intended to provide updated prospects of Gentiana kurroo and provides insights on the nutritional and various pharmacological properties based on updated research literature. This review explores the use of Gentiana kurroo across disciplines for its wide range of prominent-pharmacological properties.
... In fact, both secoiridoids showed a protective effect in the case of ulcers induced by immersion stress, while amarogentin was also effective in gastric lesions induced by ethanol. However, no effect was observed when indomethacin (5 mg/kg), an inhibitor of prostaglandins synthesis, was used as pre-treatment (Niiho et al., 2006). ...
... GASTROPROTECTIVE AND HEPATOPROTECTIVE ACTIVITY G. lutea extract pylorus-ligated mice 500-1000 mg/kg ↑ protective effect against gastric ulcer ↓ gastric juice ↓ total acid outputNiiho et al. (2006) Complementary and integrative medicine (CIM) practitioners MIC 0.12-0.31 mg/mL ↓ vitality Š avikin et al.(2009b) ...
Over many years, natural products have been a source of healing agents and have exhibited beneficial uses for treating human diseases. The Gentiana genus is the biggest genus in the Gentianaceae, with over 400 species distributed mainly in alpine zones of temperate countries around the world. Plants in the Gentiana genus have historically been used to treat a wide range of diseases. Still, only in the last years has particular attention been paid to the biological activities of Gentiana lutea Linn., also known as yellow Gentian or bitterwort. Several in vitro/vivo investigations and human interventional trials have demonstrated the promising activity of G. lutea extracts against oxidative stress, microbial infections, inflammation, obesity, atherosclerosis, etc..
A systematic approach was performed using Pubmed and Scopus databases to update G. lutea chemistry and activity. Specifically, this systematic review synthesized the major specialized bitter metabolites and the biological activity data obtained from different cell lines, animal models, and human interventional trials. This review aims to the exaltation of G. lutea as a source of bioactive compounds that can prevent and treat several human illnesses.
... It is also used in traditional medicine for the treatment of gastrointestinal disorders and as an official drug in the European Pharmacopoeia (European Medicines Agency, 2009;European Pharmacopoeia, 2014). There are also reports regarding choleretic (Öztürk et al., 1998), wound healing (Mathew et al., 2004), antiviral (Živković et al., 2018), antiulcerogenic (Niiho et al., 2006), radioprotective (Menković et al., 2010), and neuritogenic activity (Mustafa et al., 2015a) of G. lutea underground parts. Health benefits of G. lutea root are associated with the presence of numerous bioactive compounds including bitter-tasting secoiridoid compounds, such as gentiopicroside, swertiamarin, amarogentin and sweroside, and group of xanthones such as isogentisin, gentioside and gentisin, as well as iridoid loganic acid (Aberham et al., 2007) Considering the diversity of bioactive compounds found in G. lutea underground parts, it is necessary to design and optimize specific extraction processes in order to obtain the extract of desirable properties that can be used for the preparation of dietary supplements, functional food, pharmaceutical or cosmetic products. ...
... Health benefits of G. lutea root are associated with the presence of numerous bioactive compounds including bitter-tasting secoiridoid compounds, such as gentiopicroside, swertiamarin, amarogentin and sweroside, and group of xanthones such as isogentisin, gentioside and gentisin, as well as iridoid loganic acid (Aberham et al., 2007) Considering the diversity of bioactive compounds found in G. lutea underground parts, it is necessary to design and optimize specific extraction processes in order to obtain the extract of desirable properties that can be used for the preparation of dietary supplements, functional food, pharmaceutical or cosmetic products. According to the literature data, G. lutea roots were usually extracted by ultrasound-assisted extraction (Mustafa et al., 2015a,;Citová et al., 2008) or maceration (Niiho et al., 2006;Szucs et al., 2002;Aberham et al., 2011) using methanol as solvent for extraction. Although ultrasound-assisted extraction reduced processing time, a conventional solvent extraction https://doi.org/10. ...
Perennial plant Gentiana lutea L. is used worldwide for the preparation of pharmaceutical and food products. Health benefits of G. lutea roots are associated with the presence of major bitter-tasting secoiridoid gentiopicroside and xanthone isogentisin. The aim was to optimize the heat-assisted extraction of gentipicroside (GP), isogentisin (ISG) and total phenolics (TP) from G. lutea roots and develop models with high accuracy and prediction capacity by response surface methodology (RSM) and artificial neural networks (ANN). Extracts were prepared according to central composite design. Significant independent variables which were previously identified by Plackett-Burman screening design were varied at five levels - temperature (20−80 °C), time (8−180 min), solid-to-solvent ratio (1:10−1:50) and ethanol concentration (10–70 %). Contents of GP, ISG (by HPLC-DAD) and TP (by Folin–Ciocalteu method) were analyzed. The optimal conditions for the extraction were temperature of 65 °C, time of 129.08 min, solid-to-solvent ratio of 1:40, and ethanol concentration 49.33 %. Under these conditions, experimentally obtained results for GP (18.03 mg/g dw), ISG (8.15 mg/g dw) and TP (17.46 mg of gallic acid equivalents/g dw) content were in agreement with the values predicted by RSM and ANN. Comparison of models through the coefficient of determination (R²) and the root mean square error (RMSE) showed that ANN approach was superior to RSM in predicting and modelling GP, ISG and TP content, simultaneously. Effective heat-assisted extraction method for the extraction of GP, ISG and TP from the roots of G. lutea was designed, and models with high accuracy and good prediction capacity were developed.
... The plant has also been reported to possess hypoglycaemic activity [11], anti-inflammatory activity [12], hepatoprotective activity [13], wound healing activity [14], anti-carcinogenic activity [10], anti-malarial activity [15] as well as antibacterial activity [16]. Amarogentin is a wellreported compound for antileishmanial, anticancerous, anti-diabetic and gastroprotective activity by different researchers [17][18][19][20]. Also, amaroswerin reported having gastroprotective activity [19]. ...
... Amarogentin is a wellreported compound for antileishmanial, anticancerous, anti-diabetic and gastroprotective activity by different researchers [17][18][19][20]. Also, amaroswerin reported having gastroprotective activity [19]. Due to its intense medicinal importance demand for this plant is increasing at the rate of 10 percent per year [21]. ...
Aims: The present study aims to quantify major secoiridoids (amaroswerin and amrogentin) in different parts of Swertia chirayita using HPLC to distinguish its parts having a high content of amaroswerin and amarogentin, so that these parts must be included in plant material when the plant is used for estimation or extraction of these phytoconstituents.
Study Design: Statistical comparison was performed using OP-STAT software with CRD and was considered statistically significant.
Place and Duration of Study: The plant material including all studied parts was procured form field plants were grown at Medicinal and Aromatic Plants Farm, Shilly (latitude-N 30˚54′30" and longitude E 77˚07′30", elevation 1550 m) under Department of Forest Products, UHF, Solan (H.P.) India. The study was undertaken in the Departmental laboratory and in the period between September 2016 and December 2016.
Methodology: Waters binary HPLC unit with Waters HPLC pump 515, dual λ absorbance detector 2487 and Empower II software was used for quantification of phytoconstituents under study. Samples of different plant parts were extracted by using soxhlet method with methanol as solvent.
Results: In different parts of Swertia chirayita, amaroswerin content (%) was reported highest in flowers (0.741%), followed by leaves (0.386%), roots (0.188%) and lowest in stem part (0.226%) and amarogentin content (%) was reported as highest in flowers (0.617%), followed by leaves (0.447%), stem (0.426%) and lowest in roots (0.369%) of field grown plants.
Conclusion: It is conluded that amaroswerin and amarogentin were present in all studied parts of Swertia chirayita. Amaroswerin and amarogentin content was ranged from 0.160% to 0.741% and 0.369% to 0.617% respectively in different plant parts under study.
... Methanolic extract (secoiridoid glycosides) Enhancement of the mucosal defensive factors via the prostaglandin pathway in the cell membrane. [80] Glycyrrhiza glabra Leguminosae Glycyrrhetinic acid, flavonoids and polysaccharides ...
... The gastrodefensive effect of Gentian root methanolic extract was evaluated and results indicated that healing properties of Gentian roots on gastric lesions related to boosted mucosal protective factors by prostaglandin pathway, and that secoiridoid glycosides are responsible for this action. [80] Glycirrhyza glabra Glycyrrhiza glabra L. or Liquorice (Family: Leguminosae) is a ligneous perennial shrub native of the Middle East, Mediterranean region, and Asia Minor. It is also farmed extensively in southern Russia. ...
Herbal medicines are now commonly used all over the world and this has increased global demand. Quality, safety, and efficacy of these drugs have become a serious concern. This review presents the medicinal plants cited in folklore that are used to treat gastrointestinal ulcers. Electronic databases, that is, Web of Science, PubMed, Scopus, and Google Scholar were searched to identify the gastroprotective effects of each plant. Ethnopharmacological studies have reported various botanical products with antiulcer activities, but there has been limited scientific research, presenting clinical data to validate the efficacy and safety of medicinal herbs as gastroprotective agents. Most studies centered on pharmacological properties of medicinal herbs as used animals models. This information has prompted us to compile a list of the medicinal herbs cited in folklore with gastroprotective activity.
... The roots and rhizomes of G. kurroo Royle have been recorded in the Indian pharmaceutical codex [8]. The root and rhizome are source of Iridoid glycosides-gentiopicrine, gentiamarin, amaroswerin, and the alkaloid gentianine [46][47][48]. The dried roots contain 20% of a yellow, transparent, and brittle resin [23,29,48], aucubin, catalpol, 6-O-vanilloyl catalpol, 6-O-cinnamoyl catalpol, [49,50]. ...
... In the Ayurvedic (Unani) system of medicine, the flower tops (Gule-Ghafis) are used for treatment of inflammation, pain, antipyretic and hepatitis [61,62] and in the preparation of tonics for stomachic [72]. It is also curative for the skin disease leucoderma, leprosy, dyspepsia, colic, anorexia, flatulence, helminthiosis, anti-inflammatory, amenorrhea, dysmenorrhoeal, haemorrhoids, strangury, constipation, urinary infections as an antiseptic, bitter tonic, cholagogue and bronchial asthma [46,73,74]. However, there are some scientific validations of the folkloric uses of the critically endangered medicinal plant G. kurroo Royle. ...
The present investigation was carried out to review and highlight the potential phytochemicals and medicinal phenomena of the critically endangered medicinal plant, Gentiana kurroo Royle of the western and north-western Himalayas. The medicinal plant is heavily exploited for root and rhizome. Due to its endemic nature and the high rate of exploitation from its natural habitat, this species had become critically endangered. The phytochemical screening of the plant revealed that the plant contains some vital phyto-constituents (iridoids, xanthones, C-glucoxanthone mangiferin, and C-glucoflavones) that have a medicinal value for various acute and chronic diseases. Several researchers have carried out experimental work to validate the folkloric use of the medicinal plant for different ailments like antibacterial, antioxidant, anti-arthritic, anti-inflammatory, analgesic activities and anti-diabetic activity. However, it is yet to be confirmed the antifungal activity of the same plant. Because of endemic nature and high rate of exploitation there is need for alternative method called bio-prospecting of Endophytes from the plant, to carry out the production and characterization of bioactive metabolites for pharmacological uses and can become a conservative tool for the medicinal plant.
... Of these, 16 (51.6%) were reported for their function in gastrointestinal protection, regulation, and/or motility, namely: apigenin, 39 apigenin glucoside, 40 apigenin glucuronide, 41 caffeic acid ethyl ester, 42 deoxylactucin, 43 dicaffeoylquinic acid, 44 genistein glucuronide, 39 gentiopicrin (also known as gentiopicroside), 45 imperatorin, 46,47 isoimperatorin, 47 isorosmanol, 48 nepetin glucoside (also known as nepitrin), 49 rosmarinic acid, 50 sweroside, 51 swertiamarin, 52 and tuberonic acid. 53 Of the remaining 15 unique metabolites, 13 are known for their anti-inflammatory, antioxidant, and/or antimicrobial activities, namely: apigenin glucopyranoside, 54 cynarin, 55 dimethyl rosmanol, 56 hispidulin, 57 hispidulin 7-glucuronide, 57 kaempferol rutinoside, 58 luteolin, 59 luteolin glucuronide, 59 methyl catechin, 60 mono caffeoylquinic acid, 61 ostruthin, 62 quercetin glucuronide, 63 and rosmadial. ...
Background
Impaired gastric accommodation is one of the most frequent symptoms of functional dyspepsia. The safety and efficacy of conventional treatments remain to be proven and alternative herbal therapies have been proposed to alleviate gastrointestinal symptoms. This preclinical study examined the role of herbal Amara extract (containing Artemisia absinthium, Centaurium erythraea, Cichorium intybus, Gentiana lutea, Juniperus communis, Achillea millefolium, Peucedanum ostruthium, Salvia officinalis, and Taraxacum extracts) on gastric (fundus) accommodation and the possible implication of muscarinic receptors in its regulation.
Methods
The effect of Amara extract on fundus motility was investigated in organ baths of smooth muscle strips isolated from the fundus of guinea pigs, and the role of the muscarinic receptor pathway was evaluated using functional and radioligand binding assays in cell lines expressing the M2 or M3 muscarinic receptor.
Key Results
Amara extract inhibited carbachol‐induced contraction of guinea pig smooth muscle strips in a dose‐dependent manner. This relaxant effect was not affected by the M3 antagonist J‐104129. Amara extract also inhibited M2, but not M3, receptor activity in CHO‐K1 cells (IC50 219 μg mL⁻¹), and specifically bound the M2 receptor (IC50 294 μg mL⁻¹). Of the nine herbal components of Amara extract, Juniperus communis, P. ostruthium, and Salvia officinalis inhibited M2 receptor activity (IC50 32.0, 20.8, and 20.1 μg mL⁻¹, respectively), and P. ostruthium was sufficient to reverse carbachol‐induced ex vivo contraction of guinea pig fundic smooth muscles.
Conclusion and Inferences
Amara extract relaxes gastric smooth muscles by inhibiting the M2 muscarinic receptor. This study suggests the potential benefit of Amara extract for patients with impaired gastric accommodation.
... It is a known to inhibit poismerase (Ray, S., 1996) chemo preventive and is reported to have anti-leishmanial (Mdda, S., 1999) with gastro protective properties (Niiho, Y., 2006). The amarogentin rich fraction of Swertia chirayita showed to inhibit cell proliferation and enhance apoptosis, which are major physiological process regulating tumour formation, growth and spread (Saha P, Mandal, S., Das, A., et al. 2004) and (Saha, P., Mandal, S., Das, A., et al. 2004 and. ...
Chiraito (Swertia chirayita) is one of the highly traded medicinal plants of Nepal which was chosen to investigate its functional properties. It was collected from the diverse habitats of Rasuwa district of Nepal and the specimens were checked and identified at National Herbarium and Plant Laboratories (NHPL), Godavari, Lalitpur to study its physiochemical and biological activities. The stem, root and leaves of the plant were dried, powdered and mixed at the ratio of 1: 1: 1 for extraction using methanol by cold and warm method. The percentage yield from the plant was highest in warm methanol with 3.73%, followed by cold methanol with 2.28%. Plant extract showed the presence of phytochemicals like basic alkaloids, coumarin, glycosides, steroids, quinones, flavonoid and terpenoids. Phytochemicals namely Amarogentin, Mangiferin and Swertiamarin were also determined using HPLC-DA Detector. The extract showed significant antibacterial activity towards selected pathogenic microbial species for the test. The zone of inhibition (ZOI) shown by the extracts was comparable to the standard chloramphenicol antibiotics. The antioxidant activity of the sample was found to be 62.54% at 500 µg/mL and 15.32% at 100 µg/mL by radical scavenging method and showed significant antioxidants potential. The methanolic extracts also demonstrated anti-cancer activities as compare to positive control drug 5’ fluro uracil which were evaluated by assessing the effect on cell viability by MTT assay and fluorescence microscopy. The crude extracts exhibited selectively cytotoxic effect in vitro to KELLY, MCF-7 and CACO-2 cells. The effect of 1000 μg/mL crude extract was equivalent to 1.32 μg/mL of 5-fluorouracil in MCF-7 cell to inhibit 66.21% cell whereas effect of 1000 μg/mL extract was equivalent to 2.43 μg/mL of same drugs in KELLY cell to inhibit by 38.83% and finally 1000 μg/mL of the same extract was equivalent to 2.94 μg/mL of drug to inhibit 38% CACO-2 cells. The IC50 of 5 Fluro uracil (5-FU) in MCF-7, CACO-2 and KELLY obtained by plotting a measure of cell death rate vs the concentration of the drug was 2.24 μg/mL, 2.23 μg/mL and 1.58 μg/mL respectively. The extract has been recommended in therapeutic form but its use in food industries is still under research. Finding its functional properties, Chiraito powder (669 µm particle sized) with 1.0 %, 0.10%, 0.00% and 0.01% respectively were added to wheat flour to make four different type of bread. Sensory evaluations of the breads were done using 9-points (Hedonic Rating Test). The data were statistically analyzed using SPSS for Analysis of Variance (ANOVA) at 5% level of significance. The overall quality of the finished products also showed that the herb extract didn’t affect physico-chemical properties of the product which was measured in terms of dough yield, bread volume, elasticity, acid degree, water content, crumb porosity, texture, smell and taste. Overall acceptability showed that bread (Sample D) with 0.010% was superior and liked the most. The outcome of this would support production and commercialization of innovative functional health food. The study concludes that the plant extract may be sensitive, specific and cost effective biomarkers in early prevention of breast, colon and brain cancer assessing response to treatment.
... Amaroswerin belongs to the group of secoiridoids, has a bitter taste, and is found in the flowers, leaves, stems, and roots of Swertia chirayita [48]. It is known for its gastroprotective effects [49]. Based on the available data on the pharmacological potential of this molecule, we revealed that it has not yet been fully explored. ...
Alzheimer’s disease (AD) is an extremely complex, heterogeneous, and multifactorial neurodegenerative disease clinically characterized by progressive memory loss and progressive decline in cognitive function. There is currently no effective treatment for the onset and/or progression of the pathophysiological diseases of AD. The global prevalence of this disease has increased in recent years due to modern lifestyle. Therefore, there is an urgent need to develop a drug with significant neuroprotective potential. Since plant metabolites, especially polyphenols, have important pharmacological properties acting against β-amyloid (Aβ), Tau, neuroinflammation, and oxidative stress, such phytochemicals were selected in the present research. Using the Schrödinger tool (Maestro V.13.6), the drug potency of these metabolites was studied after installation in the highly configured workstation. Among the 120 polyphenols docked, amygdalin showed notable docking values of − 11.2638, followed by eriocitrin (− 10.9569), keracyanin (− 10.7086), and amaroswerin (− 9.48126). The prominent MM-GBSA values of these molecules were − 62.8829, − 52.1914, − 68.6307, and − 63.1074, respectively. The MM-GBSA energy values demonstrated the drug stability of these molecules for β-site amyloid precursor protein-cleaving enzyme 1 (BACE1)-causing AD. In the absorption and distribution assessment, these phytochemicals showed significantly better values than the inhibitors CNP520. The chosen phytochemicals have been demonstrated as non-hepatotoxic; however, the BACE1 inhibitor CNP520 is hepatotoxic. In both the molecular docking and ADMET assessments, these natural chemicals have shown optimism as potential drug candidates for Alzheimer’s disease. However, in order to understand the detailed biological metabolism of these compounds in AD, they need to be evaluated in in vivo studies to validate its efficacy.
... Gentianae radix is made up of desiccated rhizomes and roots of Gentiana lutea L. (Family: Gentianaceae), which appear as sole or branched sub cylindrical sections of various lengths and thicknesses, often 10-40 mm. The gastro-protective activity of Gentian root methanolic extract was investigated, and the results revealed that the healing effect of Gentian roots on gastric wound were linked to increased mucosal protective features via the prostaglandin pathway, with secoiridoid glycosides being accountable for this action 71,72 . ...
Peptic ulcer is a disorder that commonly has an effect on the digestive system. It is a chronic illness which has impact on
approximately, 10% of the mankind. The majority of current therapy regimens are based on western medicine. Proton pump
inhibitors (PPIs) and histamine-2 (H2) receptor antagonists, which are commonly used to treat peptic ulcers, have been
linked to side effects, relapses, and drug interactions. However, several investigations have shown that herbal medications
can efficiently heal stomach ulcers in humans and animals using different processes. As a result, this review will focus on
common plants with medicinal value which can be utilized to cure or prevent peptic ulcers.
... et al., 2010), hepatoprotective (Liu et al., 1994; Luo et al., 2009), preventative in treatment for physiological state(Jeong et al., 2015), and is additionally urged as a promising pathology therapeutic natural product(Sun et al., 2013). Amaroswerin is thought for its gastroprotective effects of the bitter principles(Niiho et al., 2006). ...
Swertia chirayita (Gentianaceae), a popular healthful herb native to the temperate, the Himalaya is utilized in ancient drugs to treat various ailments like liver disorders, malaria, and polygenic disease and area unit rumoured to possess a decent spectrum of medicine properties. Its healthful usage is well-documented in Indian pharmaceutical codex, British, and so the yank pharmacopoeias and in many ancient drugs just like the Ayurveda, Unani, Siddha, and alternative standard medical systems. This ethnomedicinal herb is understood principally for its bitter style caused by the presence of various bioactive compounds that area unit directly related to human health welfare. The increasing high usage of Swertia chirayita, principally the underground tissues, additionally as a result of the bootleg overharvesting combined with home ground destruction resulted throughout a forceful reduction of its populations and has brought this plant to the verge of extinction. The increasing national and international demand for Swertia chirayita has semiconductor diode to unscrupulous assortment from the wild and adulteration of providers. The aim of this review is to produce a synthesis of this state of information domain on the healthful uses, phytochemistry, medicine activities of Swertia chirayita and to spotlight its future prospects. Medicine knowledge rumoured in literature recommend that Swertia chirayita shows a helpful impact among the treatment of many ailments. However, there is lack of adequate data on the protection analysis of the plant. The medicine utility of Swertia chirayita needs the requirement for conservation friendly approaches in its utilization. However, a lot of advanced analysis is secure to work out the activities of bioactive compounds in vitro and in vivo, establish their underlying mechanisms of action and begin the method of clinical analysis.
... The quality of gentian root is evaluated by assessing the major bitter principle, gentiopicroside [10,11]. Antimicrobial [12], antitubercular [13], and wound healing activity [14], gastroprotective [15] and neuritogenic effects [16], and uses as a stimulant of the central nervous system [17] have been reported. ...
Natural products have been the main source of bioactive molecules for centuries. We tested the biological profile of two metabolites extracted from Gentiana lutea L. by means of computational techniques and in vitro assays. The two molecules (loganic acid and gentiopicroside) were tested in silico using an innovative technique, named Inverse Virtual Screening (IVS), to highlight putative partners among a panel of proteins involved in inflammation and cancer events. A positive binding with cyclooxygenase-2 (COX-2), alpha-1-antichymotrypsin, and alpha-1-acid glycoprotein emerged from the computational experiments and the outcomes from the promising interaction with COX-2 were confirmed by Western blot, highlighting the reliability of IVS in the field of the natural products.
... The antimicrobial activity of leaves and flowers was also recorded against Gram-positive and Gram-negative bacteria and yeast Candida albicans [11]. Extensive research of bioactive properties of Gentiana lutea extracts shows several additional effects such as anti-tubercular activity [12], radio-protective activity [13], CNS stimulation [14], anti-atherosclerotic effects [15], gastroprotective effects [16], and as ingredient in traditional remedies for atherosclerosis [15]. ...
Gentiana lutea L. is a medicinal plant the roots of which are primarily used in treatments of various human digestive disorders, but also the production of alcoholic liquors. The roots (radix) of G. lutea are described in the European Pharmacopeia, but knowledge about the chemical composition and biological activities of its aerial parts is still limited. Thus, until today aerial parts of this species have not been used in medical treatments or consumed. Therefore, flowers, leaves, and stems extracts of G. lutea obtained by using four different extraction solvents (petrol ether, chloroform, ethanol, and water) were examined for their chemical composition and biological activities. High concentrations of salicylic acid, apigenin, and naringenin were recorded for ethanol stem extracts, while significant amounts of kaempferol were detected in leaves and flowers in chloroform and water extracts, respectively. The highest antioxidant potential was recorded for flower and stem petrol ether extracts with the lowest IC50 values, ranging from 94.46 ± 9.45 to 105.38 ± 10.54 μg/mL. Ethanol extracts of flowers and stems showed moderate antioxidant activity (IC50 143.15 ± 14.32 and 146.90 ± 14.69 μg/mL) as well as strong antimicrobial activity against Candida albicans (21.00 ± 1.00 and 27.50 ± 1.78 mm inhibition zones, respectively). In addition, ethanol extracts had higher antimycotic activity compared to naturally occurring phenolic compounds that are used as positive controls. Moreover, statistical analysis of the activities of plant extracts and single compounds showed that levels of chlorogenic and caffeic acids strongly correlate with the biological activities of the extracts, i.e., they are the main carriers of these biological activities. The presented results indicate the possible use of aerial parts of G. lutea as a natural preservative, as well as a antimicrobial agent, which significantly amplifies the benefits of this medicinal crop and greatly affects the sustainability of cultivated Gentiana plantation.
... Among them, 1 was a newly reported compound. 4) To estimate the distribution of phenolic compounds in mousouchiku extract, commercial product A was analyzed by reversed-phase HPLC ( Fig. 2) with authentic original samples, and compound 13 was found to be the major ingredient. Other commercial products B-F were analyzed under the same conditions, and the peak of 2,6-dimethoxy-1,4-benzoquinone (peak DB), defined in the official list as the main constituent, was not detected among the major ingredients. ...
In Japan, existing food additives are those included in the List of Existing Food Additives specified in the Supplementary Provisions to the Law Concerning Amendments to the Food Sanitation Law and Nutrition Improvement Law. Most of the currently available food additives are natural extracts containing various ingredients. However, the characteristic and active components of existing food additives are not always properly defined due to poor characterization of the constituents of the respective raw materials. For that reason, the characteristic components of existing food additives from natural extracts have been evaluated using various methods and reported. Here we review examples of our research on the characterization of marker constituents of existing food additives from natural products.
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... 10.0, 2020). Previous studies have shown choleretic (Öztürk et al., 2002), anti-inflamtory (Mathew et al., 2004), antiulcerogenic (Niiho et al., 2006), radioprotective (Menković et al., 2010), analgesic (Öztürk et al., 2002) and antimicrobial (Pontus et al., 2006) activity of gentian root extract. Beneficial health effects of gentian root extract are associated with the presence of bitter-tasting secoiridoids (gentiopicroside, sweroside, swertiamarin, loganic acid) and biphenyl derivatives (amarogentin, amaropanin and amaroswerin), as well as phenolics i.e. xanthones (isogentisin, gentioside, gentisin), and flavonoids (isovitexin, isoorientin) (Šavikin et al., 2015; Živković et al., 2019). ...
The roots of yellow gentian, Gentiana lutea L. (Gentianaceae) are used in traditional medicine for the treatment of gastrointestinal disorders, with the literature data indicates a local gastric effect of gentian root extract (GRE) and support the use of the solid pharmaceutical forms. Gentiopicroside, as a dominant secoiridoid in the GRE, has a short elimination half-life and low bioavailability and, consequently, its bioactivity is limited. The aim of the study was to develop gastroretentive floating delivery system with GRE, and to provide prolonged release of gentiopicroside. Floating granules with dry GRE (DGRE) were prepared by the hot-melt granulation technique, while formulations included effervescent components (citric acid and sodium bicarbonate), hydroxypropyl methylcellulose (HPMC) and meltable binders (Compritol® 888 ATO and Gelucire® 50/13). The flowability of the DGRE and prepared formulations was determined by calculating the Carr index and Hausner ratio. Floating properties and in vitro dissolution rate of gentiopicroside from investigated formulations were examined. Floating granules were characterized with improved flowability (Carr index 14-22 %; Hausner ratio 1.16-1.28) in comparison to the DGRE (Carr index 28.99 %; Hausner ratio of 1.41). Furthermore, the floating granules exhibited immediate and long-lasting buoyancy and prolonged-release of gentiopicroside (over 8 h). Compritol® 888 ATO has provided sustained release of gentiopicroside from floating granules, while HPMC has decreased release rate additionally. On the other hand, Gelucire® 50/13 has increased gentiopicroside release rate. The results have shown that hot-melt granulation technique, as a green granulation method was successfully employed for obtaining gastroretentive floating granules with DGRE.
... Amarogentin, a bitter secoiridoid derived from Swertia chirata, possesses topoisomerase inhibition, chemoprotective, and antileishmanial properties [33]. Amaroswerin also from Swertia chirata showed gastro-protective ability [34]. Xanthones are also known to possess antimicrobial, antifungal [35], hypoglycemic [36], hepatoprotective, and prehematopoietic [37] properties. ...
Hoppea fastigiata (Griseb.) C.B. Clarke, an annual medicinal herb belonging to Gentianaceae, is mostly found in South-Asian countries. The genus possesses a unique class of compounds called xanthones, which are known for their potential against Alzheimer’s and Parkinson’s diseases. Three major xanthones were isolated and structurally confirmed as 1,5,7-trihydroxy-3-methoxyxanthone, 1,5-dihydroxy-3,7-dimethoxyxanthone, and 1,3,5-trihydroxy-8-methoxyxanthone from the in vitro shoot cultures which showed potential inhibitions against acetylcholinesterase, monoamine oxidase A, and monoamine oxidase B enzymes. Upon treatment with different elicitors, yeast extract (YE) was found to be most effective which led to a 20-fold increase of 1,3,5-trihydroxy-8-methoxy xanthone. YE treatment caused a rapid burst of reactive oxygen species (ROS) and the subsequent increase in xanthone contents. Phenylalanine ammonia lyase activity remained suppressed and 4-coumarate: CoA ligase activity remained unaffected after elicitation. However, shikimate dehydrogenase and shikimate kinase activities increased after elicitation. This suggested phenylalanine-independent biosynthesis of xanthones. Subsequent treatment of shoots cultures with different inhibitors of superoxide radicals (O2−), hydrogen peroxide (H2O2) generation, and calcium channel was found to suppress accumulation of xanthones. Thus, calcium mediated generation of H2O2 followed by the activation of shikimate pathway enzymes is the key early step of xanthone biosynthesis in H. fastigiata.
... We present the comparison with scientific literature (for the complete data, please see Table S1): Achillea millefolium digestive, anti-inflammatory for several problems (stomachache, muscular pain, rash) and disinfectant [19,[23][24][25]; Achillea moschata antioxidant and antibacterial [26]; Alchemilla vulgaris anti-inflammatory [27,28]; Arnica montana anti-inflammatory for wounds, cutaneous traumas, muscular, and articular pain [29][30][31][32][33][34][35][36]; Artemisia absinthium digestive [31,[37][38][39] (however, in a review from 2016 the potential antiulcer effect, with the decrease in the production of gastric juice, is reported [40]); Artemisia genipi digestive and colds [39,41]; Betula pendula diuretic [42]; Calendula officinalis anti-inflammatory and disinfectant for wounds, rashes, and burns, improves circulation [31,[43][44][45][46][47][48]; Carduus nutans antimicrobial and anti-inflammatory [49]; Cetraria islandica expectorant [50][51][52] and anti-inflammatory [51,53]; Chelidonium majus skin tags and warts [54,55]; Cichorium intybus depurative of the urinary tract [56,57]; Epilobium spp. anti-inflammatory [58,59], depurative of the urinary tract [59]; Equisetum arvense diuretic [60][61][62], anti-inflammatory for contusions [60,61,[63][64][65][66], and analgesic [61,63,65]; Euphrasia officinalis eye inflammation [31,67,68]; Foeniculum vulgare anti-inflammatory, antispasmodic, and carminative [29,31,69,70]; Gentiana lutea digestive [29,31,37,71]; Hipericum perforatum soothing and anti-inflammatory for skin rashes and burns [23,31,72], muscular pain and contusions [72,73], and antidepressant [23,31,[73][74][75][76]; Juniperus communis digestive [77][78][79]; Lamium album subsp. album diuretic [80,81]; Lavandula angustifolia anti-inflammatory and disinfectant for wounds [29,[82][83][84][85], sedative [29,31,86]; Larix decidua anti-inflammatory and disinfectant for wounds and skin problems [31,87,88], antimicrobial [88]; Laurus nobilis gastroprotective [89][90][91] and menstrual pains [92,93]; Linum usitatissimum improves intestinal motility [94][95][96], expectorant, and decongestant [97]; Malva sylvestris gingivitis and inflammations of the oral cavity [98][99][100][101], demulcent, skin anti-inflammatory and regenerative [100][101][102][103][104][105], depurative of the urinary tract [106,107], and vaginal inflammation [101]; Matricaria chamomilla soothing and ocular anti-inflammatory [31,67], antispasmodic for the gastrointestinal tract [31,43,[108][109][110], and sedative [31,43,108,109,111,112]; Melissa officinalis menstrual pains [113,114]; Mentha x piperita anti-inflammatory [115][116][117]; Origanum vulgare anti-inflammatory [118][119][120][121]; Passiflora spp. ...
This ethnobotanical survey was carried out in Caspoggio (Valmalenco, SO, Italy) with the purpose of investigating the traditional uses of medicinal plants. Moreover, a bibliographic research meant to validate or refute the uses, focusing on the potentially responsible compounds, was performed. Fifty-nine species, attributable to 30 families (Asteraceae, Pinaceae, Malvaceae, and Lamiaceae the most cited), were mentioned. Arnica montana, anti-inflammatory for traumas and musculoskeletal pains; Pinus mugo, expectorant; Malva sylvestris, anti-inflammatory and soothing; Achillea moschata, digestive. The compounds, responsible for the therapeutic activities, are often polyphenols and terpenoids: helenanin in A. montana, α-pinene, δ-3-carene, and limonene in P. mugo, gossypin and malvin in M. sylvestris, luteolin and apigenin in A. moschata. Scientific evidence for at least one of the traditional activities described was found for 50 species but only in 26 out of 196 works consulted, it is possible to make a comparison between investigated extracts and traditional preparations. This study is thus a stimulus to new phytochemical investigations, mimicking as much as possible the traditional preparations. This work is part of the European Interreg Italy-Switzerland B-ICE project, aimed at creating a management model for the ongoing climate change and searching for new sources of territory valorization as attractions for tourists.
... Amarogentin (chirantin) Topoisomerase inhibition, chemo-preventive and antileishmanial effects . [Ray 1996), [Saha and Dass 2005), [Phoboo et al. 2013] Amaroswerin Gastro-shielding [Niiho 2005], [Phoboo et al. 2013] Gentianine Anti-infl ammatory, anesthetic, antihistaminic, anticonvulsant properties, hypotensive, antipsychotic, lenitive, diuretic, antimalarial, antiamoebic and antibacterial properties. ...
Swertia chirayita is an endangered indigenous medicinal herb. It is used in traditional medicine to treat various ailments. Swertia chirayita is found in temperate regions of the Himalaya at an altitude of 1200-3000 m from Kashmir to Nepal, Bhutan and grows in the slopes of moist shady places. The species is valued for its bitterness. The bitterness, antihelmintic, hypoglycemic and antipyretic properties are attributed to amarogentin, swerchirin, swertiamarin and other active principles of the herb. Its medicinal usage is reported in Indian pharmaceutical codex, the British and the American pharmacopoeias and in different traditional systems of medicines such as the Ayurveda, Unani and Siddha. With the passage of time there is increase in demand of this plant, so it is uprooted in its earlier stage and plant is becoming endangered. There are some biotechnological methods like in vitro propagation and in vitro conservation which can protect the medicinal plants to be extinct. These two methods help to produce maximum plants in less time and conserved the plant for long time. These are also very useful in storing valuable germplasms. This review is mainly focused on in vitro propagation and conservation of the Swertia chirayita.
... The root and rhizome are rich source of Iridoid glycosides-gentiopicrine, gentiamarin, amaroswerin, and the alkaloid gentianine (Niiho 2006). The roots contain 20% of a yellow, transparent, and brittle resin (Coventry, 1927;Anonymous, 1956), aucubin, cata-lpol, 6-O-vanilloyl catalpol, 6-O-cinnamoyl catalpol, (Sarg, 1991;Raina 2011). ...
Sustainable utilization and conservation of the threatened species is a major challenge for conservationists. For the conservation and reintroduction of species, comprehensive information on the ecological elements,
potential habitats and pharmaceutical importance of the species is essentially required. This has necessitated initiating studies on habitat and population ecology of the threatened species. In view of the above, the present study investigated populations of Gentian kurroo representing different habitats and aspects in Himachal Pradesh. Among the
populations, mean density of G. kurroo 80.75 Ind per 100m2
and range varied from 63.0-110.0 Ind 100m-2
. The density showed direct relation with soil, slope, aspect and habitat. The particular geographical distribution of the species was sub tropical indicated species habitat specificity. Biological features, aspects, slope and pressure contributed
to the critical population status of the G.. kurroo. The present investigation clearly showed that G.. kurroo populations occurred in fragmented pattern in the sub-tropical ecosystem. Species re-introduction should therefore carefully select suitable habitat with suggested setting in this study. The present study confirmed that population ecology,
habitat distribution modelling provide assistance in the species recovery plan. The study would not only help in ecorestoration of the species and habitats but also in recovering the species population and improving its conservation.
... Swertiamarin and/or gentiopicrin are the major secoiridoid glycosides and bioactive ingredients of Gentianaceae plants. Their pharmacological effects, including attenuation of gastrointestinal disorders (Niiho et al., 2006;Ruan et al., 2015), hepatoprotective (Kondo et al., 1994;Lian et al., 2010), antibacterial, antifungal (Kumarasamy et al., 2003a,b;Šiler et al., 2010, anti-inflammatory (He et al., 2015;Berkan et al., 1991), antioxidant (Đorđević et al., 2017), and gastroprotective effects (Tuluce et al., 2011), are well documented. However, there are only a few studies about the chemical composition of B. perfoliata (Nishikawa et al., 1998;Kaouadji, 1990;Kaouadji et al., 1990;Sabovljević et al., 2006;Skrzypczak et al., 1992). ...
Blackstonia perfoliata (L.) Huds. is known as a highly bitter secoiridoid glycosides-containing plant and as a possible substitute for some Gentianaceae plants in herbal preparations. Nevertheless, its bioactive properties are still unknown. The present study aimed to characterize both, secoiridoid glycosides and phenolic constituents, and to investigate antioxidant, antimicrobial, anti-inflammatory, and cytotoxic activities of B. perfoliata methanolic extract. The secoiridoid glycosides swertiamarin, gentiopicrin, and sweroside were found to be the dominant compounds of the extract, while 23 phenolic compounds were identified in much lower concentrations. Among phenolics, flavanols were the most abundant, which represents a unique feature among Gentianaceae species. The extract showed moderate to weak antioxidant activity with better performance in inhibition of lipid peroxidation than in free radical scavenging activities. The extract showed generally better antifungal properties compared with its antibacterial potential. Also, B. perfoliata demonstrated in vitro anti-inflammatory activity, the extract (50 μg/mL) showed inhibition of cyclooxigenases, COX-1 and COX-2, activities (19.65 and 48.02%, respectively). It also displayed biocompatibility on the immortalized and cancer cells, as no cytotoxic effect was observed. For the first time, the bioactive potential of this species was demonstrated, justifying its usage in pharmaceutical and food products as an alternative for some overexploited and endangered species from the Gentianaceae family.
... Gentiana lutea L. is a medicinal plant which belongs to family Gentianaceae with gastro-protective effects (Aberham et al. 2011;Niiho et al. 2006). The roots of this plant are used in food products and also traditional medicine to stimulate appetite and for better digestion (Leung 1980). ...
The twentieth century witnessed deterioration of biodiversity and loss of natural habitats of many plant species. However, it was also an era of significant progress in tissue culture technology which opened further vistas for multiplication and conservation of plant species. Synthetic seed technology is one such method which involves selection of a suitable explant and encapsulating it in an apposite matrix for successful germination and conversion into a healthy plantlet. The underlying basis of synthetic seed technology is to imitate natural plant development that occurs through seed germination. This method has been successfully employed for propagation and storage of various forest, medicinal, and vegetable plant species. The technique is of pivotal importance for species which produce non-viable seeds, recalcitrant seeds, or have limited and rare seed production. Threatened and endangered plant species are one such category which has several bottlenecks in seed development, reproduction, and establishment in their natural environments that have undergone disruptive changes. This review aims to explore and assess the potential of synthetic seed technology as an effective approach to support conservation strategies for endangered plant species.
... Gentiopicroside and amarogentin are the secoiridoid which have been isolated from G. lutea's root [28]. Secoiridoidal glycosides isolated from different Gentiana species exhibited several important biological activities since amarogentin and amaroswerin have revealed the strongest gastroprotective effects among the other secoiridoidals [29]. Gentiopicrin and xanthone isogentisin and mangiferin isolated from leaves and flowers of G. lutea exhibited considerable antimicrobial activities [30]. ...
Introduction
Cancer is a disease with increasing incidence and is the second cause of death worldwide. Phytotherapy is based on the use of plants to treat diseases and is important in the development of new therapeutic strategies such as anti-cancer drugs. The aim of this work was to perform a study on the effect of aqueous and ethanolic extracts of Gentiana lutea in two human cancer cell lines, human cervical cancer (HeLa) and breast adenocarcinoma (MCF-7).
Methods
The aqueous and ethanolic extracts were prepared both with MEM culture medium at different concentrations as follow: 31.25 μg/ml, 62.5 μg/ml, 125 μg/ml, 250 μg/ml and 500 μg/ml. Cells were plated in 96-multiwell culture plates at a density of 10⁴ and 10⁵ cells/well for each extract concentration. Untreated cancer cells acted as a control group.
Results
The results exhibited a hyperbolic relationship between growth inhibition for HeLa /and MCF-7 cell lines and ethanol extract concentration revealed the highest inhibition observed at 500 μg/ml for both cell concentrations. MCF-7 cell line was inhibited when exposed to the ethanol extract of Gentiana lutea (highest growth inhibition of 25%). Aqueous plant extracts exhibited a different behavior since there was an increase (15–20%) in cell growth at low extract concentrations while a cell growth inhibition (15–25%) was only observed at the highest extract concentration.
Conclusion
The present results strongly suggest growth inhibition of carcinoma cell lines by the hyperbolic relationship for both plant extracts and it will require a detailed future research to understand its molecular mechanism.
... Hepatoprotective activity was reported for root and rhizome extracts of G. cruciate, G. manshurica, G. scabra, and G. lutea (Mihailović et al. 2013(Mihailović et al. , 2014Pan et al. 2016). Niiho et al. (2006) confirmed gastroprotective effects of the methanol extract of G. lutea roots. The extracts from roots of G. macrophylla and G. straminea, acetone extract from G. striata, ethanol extract from flowers of G. kurroo, and ethanol and petroleum ether extracts of G. lutea rhizomes possessed potent anti-inflammatory activities (Pan et al. 2016;Mirzaee et al. 2017). ...
Extracts of the aerial parts and roots of the wild-growing medicinal plant Gentiana asclepiadea were analysed for their antimicrobial, antibiofilm, and antioxidant activity with quantification of the total phenolic and total flavonoid content. Antimicrobial activity was tested against pathogenic and spoilage bacteria, yeasts, and moulds using the microdilution method. The strongest antibacterial activity was detected on Bacillus species, where minimum inhibitory concentrations (MICs) of from 0.16 mg/mL to 5 mg/mL were obtained, while antifungal activity was low to moderate, with MICs between 1.25 and 20 mg/mL. In the crystal violet assay, the extracts inhibit 50% biofilm formation in the concentration range of from 2.12 to 37.04 mg/mL. Staphylococcus aureus, S. aureus ATCC 25923, and Pseudomonas aeruginosa ATCC 27853 biofilms were the most sensitive to the presence of extracts. The extracts rich in phenolic compounds showed good DPPH-scavenging activity, with EC 50 values between 181.3 and 614.3 μg/mL for extracts of aerial parts and from 426.67 to >1000 μg/mL for root extracts. Even though G. asclepiadea has long been traditionally used, its biological activity is still insufficiently explored, so the obtained results are significant for contributing new knowledge about the plant's medicinal properties.
... Main SG present in aerial parts of C. erythraea and other centauries are extremely bitter compounds sweroside (3), swertiamarin (4) and gentiopicrin (5) (Šiler et al., 2012;van der Sluis, 1985). These compounds exhibit fungitoxic, antibacterial (Šiler et al., 2010), gastroprotective (Niiho et al., 2006), hepatoprotective (Kondo et al., 1994), sedative (Bhattacharya et al., 1976), and antitumor (Ishiguro et al., 1988) activities. ...
While bioactive properties of Centaurium erythraea Rafn secoiridoid glucosides (SG) are widely recognized, many aspects related to their biochemistry, metabolism and relationship to the overall plant physiology are not yet understood. Here we present for the first time an insight into the molecular background of organ-specific and genotype-dependent constitutive biosynthesis of secoiridoids in C. erythraea, by comparing chemical profiles and secoiridoid glucosides-related gene expression. Genes encoding enzymes for intermediate steps of secoiridoids biosynthesis up to secologanin have been identified by analysing transcriptomic data from C. erythraea leaves. Results suggest an organ-specific capacity for the production and accumulation of secoiridoid glucosides, and highlight leaves as the main biosynthesis site. They also point out that significant differences in SG content among various C. erythraea genotypes, are, at least partially, determined by different expression patterns of SG-related genes. The biosynthesis of SG in C. erythraea leaves is enhanced upon treatments with methyl jasmonate (MeJA), which causes reprogramming of SG-related gene expression, leading to an increased production of valuable bioactive compounds. The present study unveiled several rate-limiting genes (encoding GES, G8O, 8HGO, IS and 7DLGT) in SG biosynthesis. SLS and CPR are highlighted as important genes/enzymes that might regulate biosynthetic flux through SG pathway. Information gathered within this study will help us gain deeper insight into the SG metabolism and develop strategies for enhanced biosynthesis of specific secoiridoid glucosides in homologous or heterologous systems.
... Main SG present in aerial parts of C. erythraea and other centauries are extremely bitter compounds sweroside (3), swertiamarin (4) and gentiopicrin (5) (Šiler et al., 2012;van der Sluis, 1985). These compounds exhibit fungitoxic, antibacterial (Šiler et al., 2010), gastroprotective (Niiho et al., 2006), hepatoprotective (Kondo et al., 1994), sedative (Bhattacharya et al., 1976), and antitumor (Ishiguro et al., 1988) activities. ...
Plant species Centaurium erythraeaRafn (fam. Gentianaceae) is characterized by the presence of secoiridoid glucosides (SGs) as dominant secondary metabolites. The SG biosynthetic pathway has not yet been fully elucidated, despite the great pharmacological importance of this species. Here, an insight into the SG biosynthesis is achieved by comparing chemical profiles and secoiridoid-related gene expression patterns of different C. erythraea genotypes and plant organs. The results revealed that leaves are the main site of secoiridoid biosynthesis and accumulation in C. erythraea. The key function in the secoiridoid glucoside biosynthetic pathway has been assigned to genes encoding GES, G8O, 8HGO, 7DLGT and 7DLH2, while for SLSand CPRa potential biosynthetic-flux regulatory role has been determined. The correlation between the levels of these genes’ expression and SG content is evident in different plant organs. Also, the analysis of SG high- and low-productive genotypes of C. erythraea points out that chemical variability existing at intra-species level is, at least partially, determined by the different patterns of expression of SG-related genes in different genotypes. Taking into consideration the biological activity of secoiridoid glucosides, not only is the information obtained in this study of importance for further SG biosynthesis elucidation, but it also shows a great potential for future biotechnology-based sustainable production of these valuable metabolites.
... The extracts were dissolved in 50% (v/v) MeOH and partitioned with hexane. The aqueous layer was then partitioned with CHCl 3 , followed by ethyl acetate, to obtain an ethyl acetate fraction ($4.3 g) containing AS. Reverse-phase chromatography using Cosmosil 75C 18 -OPN (Nacalai Tesque, Kyoto, Japan) with 50% (v/v) MeOH and silica gel 60 (0.063- 0.200 mm; Merck, Darmstadt, Germany) chromatography with a mixture of CHCl 3 and MeOH (CHCl 3 /MeOH ¼ 8/2) was per- formed to obtain AS ($210 mg). NMR spectra were recorded on a Varian Unity 500 plus apparatus (Varian, Palo Alto, CA, USA) operating at 500 MHz for 1 H NMR and 125 MHz for 13 C NMR in methanol-d 4 . ...
Amarogentin (AG) is a naturally occurring secoiridoid glycoside produced mainly in the plant genera Swertia and Gentiana. Extracts of these plants have a long history of use in Japan as bitter stomachics because of their strong bitterness. Because the AG content directly reflects the potential activity of the extract, the quality control of these plant extracts through the quantitative analysis of AG is important. In the present study, we aimed to develop a quantitative analysis of AG using a monoclonal antibody (MAb) against AG (MAb 1E9) in the plant family Gentianaceae. Surprisingly, production of MAb 1E9 was successfully achieved by immunizing AG–bovine serum albumin (BSA) conjugates into mice although the number of AG bound to BSA was only one. The characterization of MAb 1E9 revealed that it shows high specificity to AG, enabling the development of an icELISA for the specific determination of AG. In addition, the detectable concentration of AG in the developed icELISA ranged from 1.95 to 62.5 ng mL⁻¹ with a limit of detection of 1.28 ng mL⁻¹, which is approximately 30–625 times higher in sensitivity compared with the conventional HPLC method. Validation analysis revealed that the icELISA using MAb 1E9 is precise (intra-assay variation <3.9%, inter-assay variation <8.8%) and accurate (recovery rates of spiked samples were between 91.0% and 106.4%). This method can be used for the quality control of plant extracts using AG as an index.
... As per oral or duodenum administration of methanol extract exhibits significant action against acute gastric ulcer induced by aspirin plus pylorus ligation, water-immersion restraint stress-induced ulcers, and gastric mucosal injury induced by ethanol. Furthermore, four secoiridoid glycosides, amarogentin, gentiopicroside, amaroswerin, and swertiamarin, were obtained from Gentian root or Swertia herb, and their protective effects against stress-induced ulcers and ethanolinduced gastric mucosal injury were evaluated [56] . ...
Gentiana lutea Lin. commonly known as yellow gentian, bitter root and bitterwort belonging to family Gentianaceae is a common traditional medicine freely available in hilly areas in Japan, Europe and adjoining continents, its medicinal properties are also mentioned in Ayurveda. The plant is reported to posse's antioxidant, antifungal, anti-inflammatory, stomachic, appetizer and immunomodulatory properties etc.Gentiana lutea is an important source of bitter phytoconstituents such as amarogentin, gentiopicrinor gentiopicroside, gentiolutelin and its dimethyl acetal, gentioluteol, gentanine, amaroswerin, gentioside including a new iridoid named gentiolutelin. Traditionally the plant is used as stomachic tonic, bitter tonic, dyspepsia, gastric inefficiency in infants, digestive tonic, catarrhal diarrhoea, anaemia, malarial disease etc. The present review is an effort to generate an interest among the mosses regarding its immense potential in preventing and treating several diseases.
... Gentian root (Gentianae Radix), which is prepared from the roots of Gentiana lutea by a drying and/or fermentation procedure, is an herbal medicine used as a bitter stomachic and sedative in Europe and Asia [1][2][3]. Demand for Gentian root is increasing, and exhaustion of the wild stock is a concern [4]. Therefore, G. lutea has recently been cultivated for the purposes of industrial production. ...
Based on NOE experiments, the structure of naphthodipyranodione from Gentianaceae plants was revised to 1,2-dihydro-4H,6H,8H-naphto[1,2-d:4,5- c'd']dipyrano-4,8-dione. Naphthodipyranodione was assumed to be formed by the degradation of gentiopicroside by enzymatic hydrolysis at low water concentration. The degradation pathway was a unique domino-reaction triggered by enzymatic hydrolysis. Naphthodipyranodione may become an index compound for the drying and/or fermenting procedure of Gentian root.
... Amarogentin and amaroswerin have the strongest gastroprotective effects among the other secoiridoidals. 46 Gentiopicrin and xanthone isogentisin, mangiferin from leaves and flowers of G. lutea have considerable antimicrobial activities. 49 The hepatoprotective activities are related to, sweroside, swertiamarin and gentiopicrin, constituents of Gentiana root (Fig. 7). ...
Gentiana, a cosmopolitan and important genus of the Gentianaceae family, comprises 400 species distributed among the world. Based on the studies of Iranian traditional medicine texts, there are some promising bioactivities for this genus that is unknown in modern medicine and some of them are still the basis of new remedies. In traditional medicine texts, Gentiana's different exclusive forms of preparations are effective for treatment of some disorders such as menstrual over-bleeding, conjunctivitis, vitiligo, animals venom poisoning, injuries, infected wounds, pain and swelling of liver, spleen, stomach and sprains of muscles. There are some activities that are the same in traditional and modern medicine such as anti-inflammatory, hepatoprotective and diuretic effects. Phytochemical investigations on the title genus have led to characterization many secondary metabolites. Secoiridoidal and iridoid glycosides such as gentiopicroside, xanthones, monoterpene alkaloid; polyphenol and flavones are the constituents that have been shown the pharmacological activities in different gentian species. This article studies the Gentiana according to the Iranian traditional and modern medicine.
... Another major phytoconstituent of this plant is swerchirin, a member of the xanthone family, which has been found to exhibit antimalarial and hypoglycaemic properties [23]. Further, other bio-active compounds such as amaroswerin, swertanone and chiratol are present in this plant that protect against gastro-intestinal [24] problems and shows anti-infl ammatory [25,26] properties as well. ...
Background: Swertia chirata Buch.-Ham. ex Wall. is an endangered medicinal herb native to the temperate Himalayan region. The species holds immense ethnobotanical importance in India, Nepal, Bangladesh and Bhutan. The herb is known to host a plethora of bioactive phytoconstituents that imbue it with a wide variety of medicinal properties. Modern research has proven that extracts of S. chirata possess antioxidative, anticarcinogenic, antimalarial, anti-infl ammatory and hypoglycaemic activities. The present article aims at highlighting the medicinal importance of S. chirata along with a brief discussion about its bioactive phytoconstituents. The research work carried out for improving the germplasm conservation strategies for S. chirata have also been elucidated in this review.
... The gastroprotective effects of the methanol extract of GM were studied using different gastric lesion models by Niiho and co-workers [47]. Four secoiridoid glycosides, amarogentin (A1), GPS (A2), amaroswerin (A3), and swertiamarin (A4) (Scheme (7)), were obtained from Gentian root or Swertia herb, and their protective effects against stress-induced ulcers and ethanol-induced gastric mucosal injury were evaluated. ...
Gentiopicroside is a secoiridoid compound isolated from Gentiana lutea which is called Qin Jiao in Chinese. It is one of the most common herbal medicines used in China. In this article, we review the pharmacological and biological activity (antiviral, anti-inflammatory, analgesia, antihepatotoxic and choleretic), as well as biotransformation of the gentiopicroside. In addition, attempt towards the total synthesis of gentiopicroside is also presented.
Wound care will always be among the main tasks in all surgical specialties. Several medicinal plants have proven efficacy to cure wounds. Ethnobotanical research and ethnopharmacological research have virtually endless potential to find new lead compounds. The aim of this research review is to assess the potential of some Gentiana species as sources of promising active compounds to support wound healing. Gentians are among the most popular medicinal plants used in many countries for a wide spectrum of health conditions. Traditionally, those used to cure wounds are Gentiana lutea, G. punctata, G. asclepiadea, G. cruciata, G. oliverii, G. septemphida, and G. gelida. Candidate compounds with skin regeneration and wound-healing potential isolated from gentians are isogentisin, isoorientin, mangiferin, lupeol, pinoresinol, syringaresinol, eustomoside, and sweroside. Based on the rich source of traditional knowledge on the properties of gentians to cure various skin and soft tissue complications; only very few modern pharmacological studies have been performed to test this potential. Our review demonstrates that this field deserves further investigation. Many gentians are declining in number and have high IUCN conservation status, and cultivation and micropropagation methods are the only solution for the development of new drugs based on gentian extracts.
Native to the temperate Himalayas, the well-known medicinal plant Swertia chirayita (Roxb. ex Flem) is used in traditional medicine to cure a number of ailments, such as liver illnesses, malaria, and diabetes, and is reported to have a wide range of pharmacological effects. Its therapeutic uses are well-documented in the Indian Pharmaceutical Codex, the British, and American Pharmacopoeias, as well as in several traditional medical practices including Ayurveda, Unani, Siddha, and other conventional medical systems. This ethnomedicinal herb is most known for its bitter taste, which is brought on by the presence of several bioactive substances that are directly linked to the welfare of human health. Among the various parts of Swertia chirayita, its roots have been more extensively studied. The plant is in danger of getting extinct due to a rapid fall in its population brought on by illegal overharvesting and habitat deterioration. Swertia chirayita is in high demand on a national and international level, which has resulted in unethical wild collecting practices and the adulteration of supply. The purpose of this chapter is to inform readers and disseminate scientific information about the taxonomy, flowering season, global distribution, morphology, medicinal applications, phytochemistry, pharmacological activities, safety assessment, and potential contributions of plant biotechnology to the conservation of Swertia chirayita and its future prospects.Keywords
Swertia chirayita
Pharmacological effectsHuman healthPhytochemistry
Introduction: Scientific evidence about biological profile of natural products can support their traditional uses. The current work was aimed to assess phytochemical and biological profile of nine medicinal plants collected from Herbalists. Methods: Extracts prepared in different solvents were subjected to phytochemical, antioxidant, enzyme inhibitory, cytotoxic, and antimicrobial activities. Reverse phase-high performance liquid chromatography (RP-HPLC) analysis was performed for the quantification of polyphenols. Results: Results showed methanol extract (M) being potent as compared to others. Gentian lutea M showed maximum extract recovery (15.00 ± 0.11 % w/w) and TFC (30.82 ± 0.21 μg QE/mg extract). Nigella sativa M displayed highest TPC (44.99 ± 0.43 μg GAE/mg extract) and TAC (334.72 ± 0.35 μg AAE/ mg extract). Results showed noteworthy quantities of vanillic acid, rutin, kaempferol, emodin in ethyl acetate (EA) and methanol (M) extracts of plants assessed by RP-HPLC. Gentisic acid was highest (11.75 µg/mg extract) in T. arjuna M extract. Similarly, maximum %FRSA (82.28 ± 0.03 %) and TRP (160.40 ± 0.38 μg AAE/ mg extract) were depicted by Terminalia chebula and Chamomilla recutita, respectively. Moreover, Mentha longifolia and G. lutea M demonstrated noteworthy (p
Ethnopharmacological relevance
Swertiamarin (SW), which belongs to iridoid glycosides, is one of the main components of Swertia plants in Gentianaceae family, including Swertia pseudochinensis H. Hara and Swertia mileensis T. N. Ho et W. L. Shi. There are mainly used in traditional Chinese medicine for the treatment of hepatic and biliary disease such as jaundice.
Aim of this study
This experiment aimed to explore the protective mechanism of SW on cholestasis induced by alpha-naphthylisothiocyanate in rats.
Materials and methods
Healthy rats were randomly divided into the control, model (ANIT, 50 mg/kg), ursodeoxycholic acid (UDCA, 80 mg/kg), and low-dose (SW, 80 mg/kg), medium-dose (SW, 100 mg/kg), and high-dose (SW, 150 mg/kg) groups. The hepatic protective effect of SW was preliminarily evaluated by measurement of serum biochemical indicators and liver morphological evaluation. Moreover, metabolomics and proteomics analysis were used to explore the protective mechanism of SW on cholestasis. The expression of related proteins was determined by Western blot and polymerase chain reaction, and the important proteins were verified by cell experiments in vitro.
Results
SW (100 mg/kg) can reduce the serum levels of the model group. The hepatocyte of the medium-dose treatment group was arranged neatly without evident inflammation. SW can partially reverse the changes in cholestasis metabolites, such as taurocholic acid, SM (d18:1/16:0), all-trans-retinoic acid and other products of rats. The main metabolic pathways affected were primary bile acid synthesis, glycerophospholipid metabolism, sphingolipid metabolism and retinol metabolism. SW medium-dose treatment group showed effective reversal of 25 related proteins and it can remarkably reduce the contents of NTCP and CYP27A1 in rat liver and increase the protein expressions of CYP7A1, CYP8B1, bile salt export pump, multidrug resistance-associated protein and FXR.
Conclusions
SW can alleviate ANIT-induced cholestasis, which by activating the farnesoid X receptor and bile acid excretion pathway.
Swertia chirayita, a medicinal herb (critically endangered) of the Himalayan region, occurring between 1200 and 2100 m above mean sea level from Kashmir to Bhutan, has been used as a potent anti-diabetic plant in traditional as well as modern medical systems. The anti-diabetic efficacy of Swertia chirayita is mainly attributed to its compounds amarogentin, mangiferin, and swerchirin. Its prevalent curative uses in traditional and modern medical approaches have led to its over-exploitation from its natural habitat, ultimately making it one of the most traded plant species in South Asia. The excessive over-exploitation and unsolved difficulties of seed viability and germination has lead S. chirayita to the verge of extinction. Consequently, alternate propagation approaches are urgently required to reduce industrial/market pressure on wild stocks. Therefore, for the harvest of desirable medicinal active compounds of plants, many in vitro propagation efforts are going on. Although the development of these effective micropropagation protocols have ensured a satisfactory supply of S. chirayita plants to industrial/commercial demands with a succeeding decrease in hysterical harvesting burden on wild populations. Apropos, this chapter highlights trends in biotechnological interventions such as synthetic seed technology, development of somatic embryogenesis protocol from different explants with the effect of plant growth hormones, followed by acclimatization, to produce true-to-type regenerates throughout the year.
Amarogentin is well known to be among the most bitter naturally occurring compound. Either as an individual one or extracts, amarogentin is used as a food additive and as a dietary supplement. The aim of the present investigation is to set-up a convenient process to selectively isolate amarogentin from the ethanolic roots extract of Gentiana lutea. The process consisted in the treatment of an aqueous suspension of such an extract with a panel of 21 solid inorganic / organic sorbents followed by filtration, desorption, and high performance liquid chromatography (HPLC) analyses. Among the solid materials tested, those containing Mg⁺² in the frame of a lamellar structure provided very good adsorption yields in the range 86.4 % - 99.9 % (p < 0.05 at Student’s t-test). The method we set up could be in principle useful to obtain a pure nature-derived food additive to provide bitter taste to foods and beverages.
Gentiana kurroo Royle is a critically endangered medicinal herb of the Indian Himalaya. It has bioactive seco-iridoid glycosides, notably gentiopicroside, in the rhizome and roots. In this study, we report on the in vitro production of gentiopicroside (GPD) from adventitious (AD) roots induced directly from the leaf, nodal, and suspension cell cultures of G. kurroo. Murashige and Skoog (MS) media fortified with Indole-3-butyric acid (IBA) 2 mg L−1 + Naphthaleneacetic acid (NAA) 0.5 mg L−1 and IBA 2 mg L−1 + Indole-3-acetic acid (IAA) 1 mg L−1 produced the maximum number of roots. Suspension cell cultures derived AD roots showed a 1.41-fold higher biomass production than adventitious roots induced from leaf and nodal explants. Among the various concentrations of MS media salts evaluated, half-strength MS suspension media favored the higher biomass and GPD accumulation. The maximum accumulation of GPD (2.58 mg g –l dry weight (DW)) and AD root biomass (18.96 g L−1 DW) was observed on the 48th day. Furthermore, GPD produced from AD root cultures were separated by using TLC, characterized using Nuclear Magnetic Resonance (NMR) and High-Resolution Liquid Chromatograph-Mass Spectrometer (HR LC-MS) and quantified with High-Performance Liquid Chromatography (HPLC).
A Burgundian Chardonnay wine was enriched with Gentiana lutea root powders originating from two French mountain sites (Massif Central and Jura) in order to prepare semi-dry gentian aromatized Chardonnay wine-based drinks. These novel alcoholic beverages were chemically and sensorially characterized for evaluating if the gentian geographic origin influenced bitter and elemental and volatile composition and sensory profiles in the final products. For that, the chemical fingerprint of gentian powders and wines were carried by headspace solid phase microextraction gas chromatography coupled to mass spectrometry (HS–SPME–GC), liquid chromatography coupled to diode array detector (LC–DAD) and inductive coupled plasma optical emission spectroscopy (ICP–OES). The mineral and volatile analysis show that the geographic distinction is more obvious in gentian powders compared to gentian macerated wines. Interestingly the maceration process in Chardonnay wine involves extraction processes revealing statistical distinctions in other chemical markers of gentian origin, like for amarogentin and loganic acid or some mineral elements such as barium and aluminum that affect undoubtedly bitterness perception and sensory properties in macerated wines compared to unmacerated wine. Additionally, the gentian volatile 2-methoxy-3-sec-butylpyrazine and the Chardonnay wine volatile ethyl-9-decenoate differentiated, respectively by extraction and powder adsorption mechanisms could be responsible of more subtle sensory differentiations between macerated wines from two distinct gentian origins.
Swertia (Gentianaceae), a diverse genus, is mentioned as a potential herbal drug in Ayurvedic, Unani, and Siddha traditional systems of medicine. Since time immemorial, 70 Swertia species have been used worldwide to cure several health illnesses associated with malaria, cancer, diabetes, inflammation, liver complications, different kinds of fever, etc. Swertia herb is used as the principal component in several marketed herbal/polyherbal formulations. Medicinal usage of Swertia is endorsed to the miscellaneous compounds, viz. xanthones, iridoids, seco-iridoids, and triterpenoids. Swertia is one of the most imperative trade herbs since its market value rises by 10% yearly. A chain of systematic isolation of bioactive compounds and their diverse range of pharmacological effects during the last 10–15 years proved this genus as an industrially important plant. This chapter makes an effort to present the comprehensive assessment on distribution, ethnopharmacology, biological activities, phytochemistry, extraction, and analysis of major bioactive compounds in selected species of Swertia in the past few years, and thus to explore the conventional and nonconventional ways of isolation and evaluation of pharmacologically significant bioactive compounds and to screen out the elite variety of Swertia spp.
Gentiana macrophylla Pall. (GM) (Fam. – Gentianaceae) is found all over the world and comprise many pharmacologically significant compounds. Its aerial parts are used in traditional medicine and in the preparation of bitter tonics. The several species of Gentiana including Gentiana macrophylla, Gentiana triflora, Gentiana algida, Gentiana lutea, Gentiana olivieri, Gentiana decumbens, Gentiana asclepiadea, and Gentiana kurroo are considered in folk medicine to treat digestive illnesses, jaundice, pneumonia, constipation, pain, cough, and fever. An efficient hairy root culture system of G. scabra and the influence of different plant growth regulators on the production of gentiopicroside, swertiamarin, and loganic acid constituents have been documented. Among various solid and liquid media, B5 liquid medium enhanced maximum root biomass in four weeks.
In many Asian and European countries, medicinal plants have been used for a long time for the treatment of different ailments and diseases. In 400 bc, Greek physician Hippocrates, known as the Father of Medicine, said ‘Food should be medicine and medicine should be food’ and elaborated on several dietary plants that could be prospective sources of medicine. Iridoids, an important class of secondary plant metabolites, have been found in several dietary folk medicinal plants of angiosperm plant families.
Gentianine is a metabolite of gentiopicroside and swertiamarin. Several biological activities have been reported for gentianine, such as antiinflammatory and antidiabetic activity, and hypotensive effect. Gentiopicroside is found in 0.9–9.8% content in Gentian root or Gentian scabra root, and Swertiamarin is contained in Swertia herb in 2–10%. These natural products can be potential starting materials for the synthesis of gentianine. This study describes the β-glucosidase-catalyzed hydrolysis of gentiopicroside and swertiamarin in the presence of hydroxylamine to afford gentianine N-oxide, which can be a synthetic precursor of gentianine derivatives. Enzymatic hydrolysis of swertiamarin selectively afforded gentianine N-oxide in 81% yield, whereas gentiopicroside afforded gentianine N-oxide and gentianol N-oxide. Plausible reaction pathways leading to gentianine, gentianol, and their N-oxides were also investigated.
Amarogentin (AG) is one of the bitter secoiridoid glycosides, which exerts various pharmacological activities as a bitter stomachic. Recently, there is an increasing demand for AG-containing plants in Japan due to their use as folk medicines and food additives; hence, it is crucial to develop analytical techniques that are specific for AG. In this study, a new magnetic particles-based enzyme immunoassay (MPs-EIA) using a specific monoclonal antibody against AG (MAb 1E9) for the rapid determination of AG in plants of the family Gentianaceae was described. AG directly immobilized onto magnetic particles (MPs) was used as a competitor for free AG against MAb 1E9, thereby increasing the surface area of the solid phase and decreasing the immunoreaction time. In addition, the blocking step required in case of the conventional enzyme-linked immunosorbent assay could be avoided in the proposed MPs-EIA, which enables an even more rapid performance for the immunoassay. In the developed MPs-EIA, AG exhibited linearity in the range of 15.6–500 ng mL⁻¹, with a limit of detection of 8.58 ng mL⁻¹. Validation analysis revealed that MPs-EIA is a sufficiently sensitive and rapid for the quantitative analysis of AG in plant samples. To the best of our knowledge, this is the first MPs-EIA that has been applied to plant samples.
p>Este artículo es una revisión actualizada sobre los metabolitos secundarios de la familia de las Gentianaceae. Estas plantas se emplean en la medicina tradicional de numerosos países y presentan actividad biológica interesante. Después de haber detallado botánicamente esta familia de plantas, que ha sido y que sigue siendo muy estudiada, se recogen los estudios toquímicos sobre numerosas especies. Los metabolitos característicos son los xantonas, una clase de compuestos no muy difundidos en el mundo vegetal. Son característicos también derivados de los seco-iridoides, y algunos alcaloides.</p
Anti-ulcer effects of cetraxate, a new compound possessing anti-plasmin, anti-casein and anti-trypsin actions were investigated by using experimental gastric ulcer models in rats. Cetraxate, 300 mg/kg p.o. showed significant inhibitory effects of 65.3%, 70.0%, 30.2%, and 67.1% against aucte types of ulcers producing by aspirin, phenylbutazone, indomethacin, and pyloric ligature (Shay's ulcer), respectively. These effects were greater than those obtained by gefarnate and aluminum sucrose sulfate may be mainly attributed to the protecting action of this drug on gastric mucosa. Ctraxate further revealed remarkable inhibitory effects on chronic types of ulcers produced by acetic acid, clamping, and clamping-cortisone. In acetic acid ulcer in particular, cetraxate was found to have a dose-dependent inhibitory effect at doses over 50 mg/kg. Of test drugs including L-glutamine and methylmethionine sulfonium chloride, cetraxate showed the most remarkable inhibitory effect on beta-glucuronidase activity in ulcer tissue of these three types of ulcers. These findings suggest that cetraxate may prevent the connective tissue in the ulcer location from decomposition due to lysosomal enzymes such as beta-glucuronidase, thereby accelerating the recovery from ulcer.
Various procedures have been reported on the biossay of antiulcer drugs . Pylorus ligation of the rat (1-3), restraint of the rat (4, 5), water immersion of the restrained rat (7) and the application of ulcerogenic agents on various animals (8-11) were used for producing experimental ulcers. In these methods the drug had been administered to the animal before the ulcer production and the preventive effect on the ulcer producing processes was tested. Although some drugs such as glutamine or methylmethionine sulfonium chloride were recently introduced to promote the repair of the ulcer which had existed already, suitable methods are lacking for their pharmacological test, and so it was hoped to develop a new method for pharmacological assay of curative activity of the drugs on existing ulcers. In the present paper curative effects of some drugs on the stress ulcer of the rat are reported.
Depending upon the origin of the stimuli which signal the secretion of gastric juice, three distinct aspects of secretion have been elucidated: the cephalic, gastric and intestinal. The efferent cholinergic mechanism is involved in the cephalic phase of gastic secretion, because cutting of the vagi just above the stomach completely eliminates the secretion. On the other hand, participation of gastrin to the gastric phase of secretion and its chemical structure have recently been demonstrated (1). However, the gastric secretion mechanism is more complicated. It is possible that the intact cholinergic innervation (2) and the presence of endogenous monoamines in the gastric wall (3) are the prerequisite to the gastrin-induced gastric secretion. There are controversial reports regarding the effect of adrenergic stimuli on the gastric secretion (4-7). In the mucous membrane of the glandular portion of the rat stomach, dopa-decarboxylase activity is high (8), but the high activity is not explained by the number of mast cells (9) and adrenergic nerves (10, 11) in the gastric mucosa. The distribution of the enterochromaffin cells is also different from that of gastric dopa decarboxylase (8). Intraperitoneal injection of dopa or 5-hydroxytryptophan (5-HTP) to rats causes a marked increase in the concentration of dopamine and 5-hydroxytryptamine (5-HT) in the gastric mucosa, and the amines are located to an enterochromaffin-like cell system in the pyloric part of the gastric mucosa (8). However, the physiological significance of the uptake and decarboxylation of dopa or 5-HT remains to be settled. In the present experiments the distribution of the endogenous monoamines in the structures of the gastric wall of the rat was studied using a formaldehyde fluorescence technique (12, 13). The temporal changes of the monoamine fluorescence were also followed in the course of formation of the gastric ulcers in the Shay rat and the restraint, cold-exposed rat.
The fact that, of the approximately 600,000 plant species existing on the earth, only some 5 % have been specifically investigated chemically or pharmacologi cally, is a challenge to chemists spezializing in na tural substances and to pharmacologists. In view of the limited number of research capacities and the ever diminishing financial means, this challenge can only be met if, together with an improvement and refinement of methods of analysis, medicinal plant research is carried out on a broader interdisciplinary basis, with comparable, scientifically recognized screening methods, and if it is better coordinated, with greater use of modern documentation means. It is thus necessary in the future to concentrate specifically on projects leading to the development of new medicinal prepara tions. The plenary lectures hold in the present symposium of the 1st International Congress for Research on Medi cinal Plants reflect these efforts and tendencies. At the same time they provide a survey of some of the fields of medicinal plant research which are at present most actual and most intensively researched. They range from plant screening, isolation and structure eluci dation of new principles, to the therapeutical opti mization of a natural product. The lectures given at this congress show clearly the necessity, in addition to national phytochemical so cieties, for a central international organisation, in which all active medicinal plant researchers in the world are included. Their aim should be to provide the impulse for more optimal, rational research, aimed at the solution of specific projects.
Various fractions of Picrasma quassioides Bennett were assayed for their antigastric ulcer activity in rats. A MeOH extract of the wood prevented the secretion of gastric juice in a dose dependent manner. The MeOH extract also showed the same effects on rats having aspirin-induced gastric ulcer. Then, the MeOH extract was further extracted with CHCl3 and EtOAc. The protective effects were detected in the CHCl3-soluble fraction and their effective components were identified as nigakilactone (1) and methylnigakinone (2). The CHCl3-insoluble fraction, espesially the EtOAc-soluble fraction, showed a protective effect on the mucous membrane. We also examined the effects of quassinoids of the Picrasma genus on the aspirin-induced ulcer in rats.
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• An 10 gesunden Versuchspersonen wurden die Auswirkungen des Zusatzes geschmacksäquivalenter Mengen von Enzian und Wermut auf die Sekretorik und Motorik des Magens, die Motorik des Darms und die Motorik der Gallenblase 4 Stunden lang röntgenologisch verfolgt.Als geschmacksäquivalent (= geschmacklich gleich intensiv wirksam) und geschmacksstark, aber doch noch gut genießbar, erwiesen sich bei Prüfung durch mehrere Degustatoren 0,20 g Enzianwurzel und 0,025 g getrocknete Wermutblätter. Die Versuchspersonen nahmen die Drogen in Gestalt eines in 50 ml Wasser gelösten alkoholischen Extraktes 5 Minuten vor einer Mahlzeit von gekochtem Reis (70 g Rohgewicht).
• Während der ersten 30 Minuten bewirkte Wermut und vor allen Dingen Enzian eine Stimulierung der Magensaftsekretion. Unter dem Einfluß von Wermut und Enzian wird die Magenverdauung in einem größeren, den Mageninhalt durchdringenden und über dem Mageninhalt stehenden Sekretvolumen bewerkstelligt als bei ungewürzter Mahlzeit. Bittermittelzusatz bedeutet also Intensivierung der (Protein– und Fett–) Verdauung im Magen.Die sekretions–stimulierende Wirkung des Enzians ist schwächer als diejenige einer geschmacksäquivalenten Senfmenge. Die Entleerunggeschwindigkeit des Magens wird durch Wermut und Enzian nicht beeinflußt.
• Unbeeinflußt durch Wermut– und Enzian–Zusatz bleibt die Passagegeschwindigkeit durch Jejunum und Ileum.
• Enzian wirkt deutlich cholagog (gallenblasenentleerend). Seine Wirkung ist jedoch weniger stark als die des stärksten natürlichen Cholagogums, des Eigelbs. Sowohl Enzian als Wermut intensivieren die Cholerese (Gallenzufluß aus der Leber).
Summary
The bitter drugs Radix Gentianae and Herba Absinthii were pharmacologically tested in man. 5 minutes before a meal of rice taste–equivalent doses of the bitter tonics were given orally. After the meal the secretion and motility of stomach and intestine, the motility of the gall bladder and the gall secretion of the liver were followed radiologically. Both bitter tonics stimulate gastric secretion; this way they intensify protein and probably fat digestion in the stomach. Gentian shows cholagogue activity, gentian and vermouth, in addition, possess choleretic activity.
The structures of valeriana and plumeria iridoids, miscellaneous iridoid-like compounds, simple secoiridoids, terpene- and phenolic-conjugated secoiridoids, bis- and tris-secoiridoids, and other miscellaneous secoiridoids published for the first time during 1980-1989 are listed with available physical and spectral data: mp, [α]D, uv, 1H nmr, 13C nmr. Also included are revisions of structures originally published prior to 1980. The compounds are indexed alphabetically and by molecular weight, and a plant source index is included.
A method for the rapid estimation of gentiopicroside in crude drugs, Gentianae scabrae radix and Gentianae radix, was established by the use of high-speed liquid chromatography. Gentiopicroside is separated on the 25 cm column of Zorbax ODS, using a liquid chromatograph (Shimadzu-Du Pont Model LC-3A) with 5% tetrahydrofuran as the desorption solution, and the separation is completed within 8 min. Gentiopicroside in the crude drugs is extracted with water and the aqueous extract is injected into the column. The content of gentiopicroside was calculated from calibration curves previously prepared using the standard. Precision of the determination is about ±1% and detection limit is 2 ng (S/N ratio, 3). This method is considered to be useful for the evaluation of these crude drugs.
The pharmacological effect of a methanolic extract of Swertia japonica, swertiamarin being the main secoiridoid glucoside of this herb and gentianine obtained from swertiamarin in aqueous ammonia, were investigated in mice and rats. Gentianine was found to exert depression of the central nervous system and anti-ulcerogenic action, as well as inhibitory action against gastric secretion, whereas the others had no appreciable action.
Two new methods for the determination of gentiopicroside in gentian radix and Gentiana scabra radix were developed by the combination of thin-layer chromatography (TLC) and spectrophotometry. In the preparative TLC-ultraviolet (UV) method, gentiopicroside contained in the methanol extract ofsamples is quantitatively separated by preparative TLC (detection by a PAN UV lamp) and the amount is determined from the absorbance at 270 nm by using a calibration graph. In the TLC-densitometer (DM) method, the methanol extract containing gentiopicroside is developed on the TLC plate, and the amount of gentiopicroside (Rf=ca. 0.4) is measured by TLC densitometry using a dual-wavelength TLC scanner. By these two methods, the content of gentiopicroside vras determined as 1-2% in gentian idix (Osaka market product), 1-3% in Gentiana scabra radix (Osaka market product), and 7-10% in the fresh root of Gentiana scabra BUNGE.
Pepto-Bismol liquid (primary active constituent, bismuth subsalicy-late) protected the gastric mucosa of rats against the formation of hemorrhagic lesions or erosions in response to cold + restraint stress, to a combination of aspirin and cold + restraint stress, and to ethyl alcohol. The protective effect of Pepto-Bismol in these studies was clearly demonstrated. Although the mechanism of action of Pepto-Bismol was not delineated, there was a suggestion that the degree of coating of the gastric mucosa was related to protection.
One gram of SM powder consists of 167.8 mg of Coptidis Rhizoma Pulveratum, 250 mg of Cinnamomi Cortex Pulveratus, 67.1 mg of Foeniculi Fractus Pulveratus, 33.6 mg of Caryophylli FLos Pulveratus, 82.1 mg of Zingiberis Rhizoma Pulveratus, 3.4 mg of Zanthoxyli Fructus Pulveratus, and 396 mg of Glycyrrhizae Radix Pulberata. SM powder (2 g/kg, i.d.) significantly inhibited gastric secretion in pylorus-ligated rats and the development of Shay ulcers and indomethacin-induced gastric lesions. The mechanism of the anti-lesion activity of SM powder appears to be due to its antisecretory effect. SM powder also markedly inhibited ethanol- or NaOH-induced gastric lesions at doses (30 or 100 mg/kg) which had little effect on gastric secretion. SM powder appears to have a cytoprotective activity which is unrelated to endogenous prostaglandins. However, SM powder had no effect on water-immersion stress- or aspirin-induced gastric lesions and mepirizole-induced duodenal ulcers. Gentiana Radix Pulverata, used as a reference stomatic, had also an antisecretory effect and anti-lesion activity on Shay ulcers, aspirin-, ethanol- and NaOH-induced gastric lesions. However, it had no effect on water-immersion stress- or indomethacin-induced gastric lesions and mepirizole-induced duodenal ulcers.
Sodium salicylate (SA), contrary to acetylsalicylic acid (ASA, aspirin), was not ulcerogenic in rats. SA was also found to be cytoprotective: it prevented formation of gastric mucosal necrosis produced by either absolute ethanol or 0.6 M HCl, and formation of gastric ulcers produced by acidified ASA. The degree of protection was dose dependent. The mechanism of this cytoprotection is unknown, but unlike cytoprotection elicited by mild irritants, e.g., 20% ethanol or 0.35 M HCl, whose effects appear to be due to endogenous formation of PG by the stomach, SA acts through a different mechanisms, since its protective effect was not blocked by indomethacin.
Gentiopicroside (GPS), a main bitter secoiridoid constituent of roots of Gentiana macrophylla Pall., was tested for therapeutic effects on the two hepatic injury models, the CCl4-induced and lipopolysaccharide (LPS)/bacillus Calmette-Guerin (BCG)-induced hepatitides. An increase in serum level of hepatic aminotransferases (GOT: EC 2.6.1.1. and GPT: EC 2.6.1.2.) induced by a p.o. treatment of CCl4 was suppressed by pretreatment with GPS at 30-60 mg/kg/day for 5 consecutive days. An increase of these enzymes triggered by an i.v. treatment with LPS in mice primed with bacillus Calmette-Guerin (BCG) was also inhibited by GPS pretreatment at the same dose of GPS. In the BCG/LPS model, tumor necrosis factor (TNF), a major inflammatory mediator, was increased in serum with a peak at 90-120 min, followed by an increase of serum transaminase activities. GPS treatment significantly suppressed the increase of TNF in serum at the therapeutic doses, suggesting that GPS protected against hepatitis by inhibiting the production of TNF.
Reconsideration of anti-secretory drugs in peptic ulcer
- A Miyoshi
Wakan-Yaku (in Japanese)
- Akamatsu
The encyclo-pedia of Wakan–Yaku, Japanese–Chinese herbal drugs)
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