Article

Gastroprotective effects of bitter principles isolated from Gentian root and Swertia herb on experimentally-induced gastric lesions in rats

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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.

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... 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]. ...
... Swertiamarin is a major phytoconstituent present in Enicostemma littorale [8,13,24] and reported for gastroprotective, antiulcerogenic , anticholonergic and CNS depressant activity [8] . ...
... Swertiamarin is a major active principle of Enicostemma littorale. The reported amount of Swertiamarin in E. littorale (7.7%) [16] is much more higher than that in Swertia chirata (0.94%) [24] which favors more commercial viability of the plant when swertiamarin is to be isolated. The IC 50 value of Chloroquine and Quinine [25] is around 10 and 29 µg mL −1 respectively which indicate that swertiamarin lies between the scales. ...
Article
Problem statement: Malaria is a prevalent disease in India. The proble m of drug resistance is worsening. Hence, new effective and a ffordable antimalarial drugs are very much needed. The long-established use of quinine and the more re cent introduction of artemisinin as highly effectiv e anti malarials demonstrate that plant species are a n important resource for the discovery of new anti malarial agents. Approach: Majority of the plants belonging to Gentianaceae fa mily were proven as good antimalarials containing swertiamarin as a com mon marker. Enicostemma littorale (Gentianaceae) is also known from traditional knowl edge for treatment of visham jwara and is rich in swertiamarin amongst all of the plants belonging to same family. In view of this, initial screening ha d been undertaken. Our laboratory had also been worki ng on the same for its antidiabetic activity. Results: This was first report to demonstrate anti plasmodi al activity of Enicostemma littorale (Gentianaceae) against Plasmodium falciparum . Methanolic extract of plant and swertiamarin isol ated from it showed promising results in vitro in schizont maturation inhibition assay having IC 50 of 529.045 and 12 µg mL -1 respectively. We also reported a simple and rapid method for isolation of swertiamarin which was applicable at commercial scale. Conclusion: The present study represented the potential antimalarial action of plant and its active phytoconstituent, may give new lead to researchers in field of antimalarial drug discovery .
... 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]. ...
Article
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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.
... [Ray et al., 1996), [Saha and Dass, 2005), [Ray et al., 1996; Medda et al., 1999]. Amaroswerin Gastro-shielding [Niiho Y et al., 2005]. [Niiho et al., 2005]. ...
... cid are found to be analgesic and emollient respectively. Ursolic acid has anti-inflammatory, chemoprotective and anti microbial activities. Topoisomerase inhibition , chemo-preventive and antileishmanial effects . [Ray et al., 1996), [Saha and Dass, 2005), [Ray et al., 1996; Medda et al., 1999]. Amaroswerin Gastro-shielding [Niiho Y et al., 2005]. [Niiho et al., 2005]. Gentianine Anti-inflammatory, anesthetic, antihistaminic , anticonvulsant properties, hypotensive , antipsychotic, lenitive, diuretic , antimalarial ,antiamoebic and antibacterial properties. ...
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Herbs orchestrate a resurgence and vegetal awakening is supervened every where in the world. Vegetal commodities currently illustrate assurance as compared to the factitious ones that are contemplate as alarming to humans and environment. Out of 2,50,000 higher plant species on this planet, more than 80,000 types are declared to have in some ways remedial importance and around 5000 species have characteristic analeptic value. Organized storage and commodious plowing of relevant medicinal plant species are thus of ample precedence. An important herb Swertia chirayita, is a medicinal plant aboriginal to clement Himalayas in India, Nepal and Bhutan. Its medicinal usage is declared in American and British pharmacopoeias, Indian Pharmaceutical codex and in different conventional systems of medicines like Ayurvedic, Unani and Sidha. Plants mainly utitize in Ayurveda can contribute organically active compounds and lead structures for the advancement of transformed subordinates with increased activeness and abate virulence. We are well enumerate as the most paramount chirayita producer and vendor based in India. The chief bioactives of Swertia are Xanthones, other active constituents of this genus are the secondary metabolites which played a momentous role in biological activities like being hepatoprotective, digestive, astringent, laxative, anti-inflammatory and anti-malarial. Hence this herb provides potent therapeutic lead compounds, which would be beneficial for mankind.
... 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. ...
Article
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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.
... 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. ...
Article
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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 root and rhizome of G. lutea constitute the crude drug "Gentianae Radix," which is used as an herbal stomachic worldwide. 2) Gentianae Radix is also listed as an official drug in the Japanese Pharmacopoeia. 3) Previously, phytochemical studies of this drug revealed the presence of bitter secoiridoid glycosides, including gentiopicroside, swertiamarin, and amarogentin, [4][5][6] xanthones, 7) phenolic acids, 8) flavonoids, 9) and triterpenoids. ...
... 20) Since gentiopicroside (5) was detected as the main constituent and amarogentin could not be detected owing to its level being below the detection limit, gentiopicroside (5) was considered the primary contributor to the bitter taste of the gentian root. Previously, amarogentin was reported to be one of the main bitter components of gentian 2,6) ; however, its content decreases over the cultivation period. Amarogentin content in materials cultivated for more than 5 years was between 0.2-0.4 ...
Article
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Gentian root extract is used as a bitter food additive in Japan. We investigated the constituents of this extract to acquire the chemical data needed for standardized specifications. Fourteen known compounds were isolated in addition to a mixture of gentisin and isogentisin: anofinic acid, 2-methoxyanofinic acid, furan-2-carboxylic acid, 5-hydroxymethyl-2-furfural, 2,3-dihydroxybenzoic acid, isovitexin, gentiopicroside, loganic acid, sweroside, vanillic acid, gentisin 7-O-primeveroside, isogentisin 3-O-primeveroside, 6'-O-glucosylgentiopicroside, and swertiajaposide D. Moreover, a new compound, loganic acid 7-(2'-hydroxy-3'-O-β-D-glucopyranosyl)benzoate (1), was also isolated. HPLC was used to analyze gentiopicroside and amarogentin, defined as the main constituents of gentian root extract in the List of Existing Food Additives in Japan.
... 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). ...
Chapter
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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.
... Sweroside is reported to be antibacterial (Siler et al., 2010), hepatoprotective (Liu et al., 1994;Luo et al., 2009), preventative in treatment for hyperpigmentation (Jeong et al., 2015), and is also suggested as a promising osteoporosis therapeutic natural product (Sun et al., 2013). Amaroswerin is known for its gastroprotective effects of the bitter principles (Niiho et al., 2006). Table 4 provides a summary focusing on the biological activity of the phytochemicals present in S. chirayita. ...
Article
Full-text available
Swertia chirayita (Gentianaceae), a popular medicinal herb indigenous to the temperate Himalayas is used in traditional medicine to treat numerous ailments such as liver disorders, malaria, and diabetes and are reported to have a wide spectrum of pharmacological properties. Its medicinal usage is well-documented in Indian pharmaceutical codex, the British, and the American pharmacopeias and in different traditional medicine such as the Ayurveda, Unani, Siddha, and other conventional medical systems. This ethnomedicinal herb is known mostly for its bitter taste caused by the presence of different bioactive compounds that are directly associated with human health welfare. The increasing high usage of Swertia chirayita, mostly the underground tissues, as well as the illegal overharvesting combined with habitat destruction resulted in a drastic reduction of its populations and has brought this plant to the verge of extinction. The increasing national and international demand for Swertia chirayita has led to unscrupulous collection from the wild and adulteration of supplies. The aim of this review is to provide a synthesis of the current state of scientific knowledge on the medicinal uses, phytochemistry, pharmacological activities, safety evaluation as well as the potential role of plant biotechnology in the conservation of Swertia chirayita and to highlight its future prospects. Pharmacological data reported in literature suggest that Swertia chirayita shows a beneficial effect in the treatment of several ailments. However, there is lack of adequate information on the safety evaluation of the plant. The pharmacological usefulness of Swertia chirayita requires the need for conservation-friendly approaches in its utilization. Providing high-quality genetically uniform clones for sustainable use and thereby saving the genetic diversity of this species in nature is important. In this regard, plant biotechnological applications such as micropropagation, synthetic seed production, and hairy root technology can play a significant role in a holistic conservation strategy. In addition to micropropagation, storage of these valuable genetic resources is equally important for germplasm preservation. However, more advanced research is warranted to determine the activities of bioactive compounds in vitro and in vivo, establish their underlying mechanisms of action and commence the process of clinical research.
... It is a known topoismerase inhibitor (Ray et al. 1996), chemopreventive and is reported to have antileishmanial (Medda et al. 1999) and gastroprotective properties (Niiho et al. 2006). ...
Article
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Swertia chirayita is an important medicinal plant from Nepal with anti-diabetic, anti-pyretic, anti-malarial and anti-inflammatory potential and used in therapeutic herbal preparations in parts of South Asia. The main phytochemicals in crude aqueous and ethanolic extracts of different plant parts of Swertia chirayita collected from nine different districts of Nepal representing West, East and Central Nepal were quantified using HPLC/DAD (High Performance Liquid Chromatography-Diode Array Detection). The quantities of these phytochemicals were also compared between wild and cultivated plant parts of Swertia chirayita. Amarogentin, mangiferin, swertiamarin were the main phytochemicals in all extracts. The highest quantity of all the three phytochemicals was found in IL (inflorescence and leaf mixture) of all the collected plants samples. There was no significant difference in the amounts of these three phytochemicals between extracts from wild and cultivated plants. The result from this study substantiates the validity of cultivated Swertia chirayita for medicinal purposes and trade.
... The genus Swertia (Gentianaceae) contains almost 700 species that are widely distributed throughout Eastern and Southern Asia, where they are used in traditional medicines to treat gastrointestinal diseases (Niiho et al. 2006). Swertia japonica is commonly referred to as Bsenburi^in Japan, where it is an important bitter stomachic containing numerous xanthones (Jamwal 2012) and secoiridoids (Kikuchi and Kikuchi 2004). ...
Article
The stress-induced α-ketol derivative of linolenic acid, identified in Lemna paucicostata as 9-hydroxy-10-oxo-12(Z),15(Z)-octadecadienoic acid (KODA), is involved in the enhancement of flower formation and the breaking of dormancy. Swertia japonica is an important bitter stomachic, and its adventitious roots contain xanthones, which are antioxidant compounds. Here, we demonstrate that KODA enhanced redifferentiation of adventitious roots from calli of S. japonica. Moreover, the effect of KODA was confirmed in liquid culture and the redifferentiation of adventitious roots was increased more than in solid culture. Conversely, KODA suppressed the biosynthesis of xanthone diglycoside, which suggests that KODA maintained the roots in an immature state under our culture conditions.
... Niiho et al. In their gastroprotective study of Gentiana suggested that the therapeutic effects of Gentian root on gastric lesions were associated with enhanced mucosal defensive factors via the prostaglandin pathway in the cell membrane, and that secoiridoid glycosides contribute to this activity [26]. PGE1 are proven for its gastroprotective activity and it is also recognized for cervical ripening property. ...
Article
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Objectives: To evaluate the efficacy of polyherbal Unani formulation for cervical ripening and induction of labour Material and Methods: A prospective, study was conducted in Govt. Nizamia Tibbia Hospital, Hyderabad. Pregnant women (n=38) with gestation age of 38-42 weeks were recruited. A polyherbal Unani formulation powder of Cinnamomum tamala 3 g, Gentiana lutea 1 g, Pinus longifolia 1 g and Peganum harmala 5 g was administrated orally at an interval of 6 hours maximum of 4 doses and a pessary of Gossypium herbaceaum 2 g, Euphorbia resinifera 0.5 g and borax 3 g, was placed in the vagina at an interval of 6 hours, maximum of 4 doses. The main outcome measure was to observe mean induction to delivery interval and spontaneous vaginal delivery. The secondary outcomes were to evaluate rate of induction failure, women given cerviprime or/and oxytocin, cesarean delivery, Apgar score and admission to the neonatal unit. Results: The mean induction to delivery interval was 12.3 ± 4.7 hours. Thirty two (84.2%) pregnant women had spontaneous vaginal deliveries. Among induction failure (15.8%), 7.8%, delivered vaginally after instillation of cerviprime and/or oxytocin and 7.8% delivered by caesarean. Apgar scores at 1 and 5 minutes were 8.9 and 9.9 respectively. None of the babies were admitted in the neonatal unit. Conclusion: The present study shows that the polyherbal Unani formulation was useful for reducing mean induction to delivery interval, and good perinatal outcome.
... The genus Swertia (Gentianaceae) consists of nearly 700 species, which are widely distributed throughout eastern and southern Asia. These plants have been used as a traditional medicine in the treatment of gastrointestinal diseases (Niiho et al. 2006). Most plants belonging to Gentianaceae are usually used as bitter stomachics and contain many kinds of secoiridoids (Rodriguez et al. 1998). ...
Article
Swertia japonica is an important Japanese folk medicine used as a remedy for stomach disease, and secoiridoids are the main active constituents. Towards producing secoiridoids using large-scale tissue culture, we investigated the effects of phytohormone conditions on callus induction and redifferentiation of adventitious roots from calli of S. japonica and the associated production of secoiridoids. Here, we report efficient conditions for induction of callus and adventitious roots and confirmed that adventitious roots produced the secoiridoids, swertiamarin, and gentiopicroside. Moreover, redifferentiation of adventitious roots was enhanced when cultured with a low concentration of auxin, while secoiridoid biosynthesis was elevated with a high concentration of cytokinin. In a time course of secoiridoid changes in adventitious roots, maximum secoiridoid production occurred 15 d after redifferentiation of adventitious roots of a 10-d-old culture, suggesting that relatively mature root development may be necessary for the in vitro production of secoiridoids in S. japonica.
... The bitter constituents belong to the class of secoiridoid glycosides, with gentiopicroside (also known as gentiamarine and gentiopicrin) as main component and lower amounts of amarogentin, swertiamarine and sweroside (Aberham et al., 2011). Secoiridoid glycosides isolated from different Gentiana species show interesting biological activities, such as antibacterial, antifungal (Kumarasamy et al., 2003), anti-inflammatory, antitumor (Ghisalberti, 1998), gastroprotective (Niiho et al., 2006) and hepatoprotective (Kondo et al., 1993;Lian et al., 2010). Phytochemical studies also revealed the presence of phenolic acids, flavoneand xanthone-C-glycosides as constituents with wide range of biological activities, including antioxidant, antitumor, antiviral, immunomodulatory and hepatoprotective activities (Singh, 2008). ...
Article
The purpose of this study was to evaluate the antioxidant potential of methanol extracts of Gentiana cru-ciata L. aerial parts and roots, as well as the stability of the phenolic compounds and antioxidant capacityof extracts during heating, at different pHs and after an in vitro digestion procedure. Also, their genotox-icity and antigenotoxicity against carbon tetrachloride in the liver of albino Wistar rats using the cometassay were evaluated. Three secoiridoid glycosides (swertiamarin, gentiopicrin, and sweroside) and fourphenolic compounds (orientin, vitexin and two isovitexin-glucosides) were identified as the major con-stituents in aerial parts and roots of G. cruciata, using UHPLC-DAD/±HESI-MS/MS analysis. The results ofantioxidant assays showed that aerial parts displayed higher antioxidant activity compared to the roots,which could be related to higher phenolics content, especially flavonoids. In general, extracts showedpH and thermal stability, while duodenal condition had more influence on total phenolic condition andantioxidant activity of extracts. Both extracts showed a protective effect against CCl4in comet assays.The roots extract showed no genotoxic activity, while aerial parts extract showed slight genotoxicity atconcentrations of 400 mg/kg b.w.
... Swertiamarin has been reported to have very low toxicity and is antibacterial (37) , anticholinergic (38) and antinociceptive (39) . Amarogentin is a known topoismerase inhibitor (40) , chemopreventive and is reported to have antileishmanial (29) and gastroprotective properties (41) .Swertia chirayita is now identified at different level of threat. Tissue culture is useful for multiplying and conserving the species, which are difficult to regenerate by conventional methods and save them from extinction (42) . ...
... In addition growth factors are bestowed with anti carcinogenic and anti-nucleolytic, cytochrome P450 2F1 inhibitory activities (Bagchi et al., 2002;Kyogoku et al., 1979). Like many other herbs viz; Quercus, Swertia herb (Niiho et al., 2006), Chinese herbal drug ''Baishouwu'' (Shan et al., 2006), Phyllanthus niruri (Abdulla et al., 2010), several studies have shown NS also as gastroprotective. A two gram dose was found almost as effective as the traditional triple therapy in eradication of H. pylori in earlier researches (Salem et al., 2010). ...
Article
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Nigella sativa (NS) or black cumin is a dark, thin, and crescent-shaped, seeded shrub belonging to the Ranunculaceae family commonly growing on Mediterranean coasts in Saudi Arabia, northern Africa and Asia. They have amazing curative and therapeutic features that make them one of the most popular, safe, non-detrimental, and cytoprotective medicinal plant that can be used for prevention and treatment of many complicated diseases. Originally, N. sativa was used to treat migraines and allergy, and researches have shown its effectiveness in destroying cancer cells as well. The gastro protective effect of NS oil and its constituents has also been reported earlier; however, the complete perception on etiology and pathogenesis of gastric ulcer is not yet clear. Herein, we attempt to unveil some of the potential mechanisms exhibited by NS in preventing problems related to gastric ulcers. Gastric ailments like ulcers and tumors are the most common disorders of the gastro-intestinal tract in present day life of the industrialized world. Gastric ulcer being a multifaceted problem exhibits complex etiology and is the fourth most common cause of cancer mortality. Drug interactions and toxicity are the main hindrances in chemotherapy. The existing merits and demerits of modern-day drugs makes us turn towards the plant kingdom which may provide a valuable resource of novel potent natural compounds for pharmaceuticals or alternately, as dietary supplements. In this context, the revered phytotherapeutic Nigella Sativa comes as a promising savior in today’s times. This review aims to summarize, both the functional and disease-related effects in the area of gastroenterology.
... Gentiopicroside is one of the most common secoiridoid glycosides presents in Gentianaceae which has been reported from 107 of 127 species in Gentianaceae, mainly in Gentiana nad Swertia genus (20). The compound has interesting pharmacological properties such as anti-inflammatory (22), protective effects against many kinds of chemical and immunological liver injuries (23)(24)(25) and stress-induced gastric ulcers (26), bile secretion promoting property (25) and smooth muscle relaxing activity (27). It also exhibits cytoprotective effect which may cause a synergism in terms of wound healing activity of Gentiana root (28). ...
Article
Background: Swertia spp. (Gentianaceae) grow widely in eastern and southern Asian countries such as Japan, China and India and are used as traditional remedy for gastrointestinal complains because of their bitter principles. Several studies have been carried out on hypoglycemic, hepatoprotective, mono amino oxidase inhibitory and antidepressant effects of these plants and it has been shown that xanthones and iridoids are responsible for their activities. Purpose of the study: In order to gain better knowledge of endemic plants of Flora Iranica, Swertia longifolia Boiss. growing in the northern parts of Iran, was subjected to phytochemical studies. Methods: Dried and milled aerial parts of the plant were extracted with petroleum ether and ethanol of which results of petroleum ether extract has been reported previously. For purification of ethanol extract, it was acidified with acetic acid and subsequently extracted with chloroform and then with n-butanol. The n-butanol extract was analyzed using different chromatographic methods and the structures of the isolated components were established by means of spectroscopic techniques. Results: Four components including an iridoid glycoside (loganic acid), a secoiridoid glycoside (gentiopicroside), a secoiridoid dilactone (gentiolactone) and a nucleoside (uridine) were isolated from n-butanol extract of the plant. Major conclusion: Similar to other species of Swertia, iridoid and secoiridoid glycosides could be considered as major constituents of Swertia longifolia Boiss.
... All of them, in different doses (p.o.), were able to prevent the lesions induced by stress and ethanol. However, pretreatment with indomethacin inhibited this activity, suggesting that the effect of 29–31 is associated with the prostaglandin pathway (Niiho et al. 2006). ...
Article
For over a century, ulcer has been a major cause of morbidity and mortality. Its treatment has progressed from vagotomy to proton pump inhibitors. However, the drugs used produce many adverse effects and are less effective than they ought to be. Therefore, there is a growing interest in alternative therapies and the use of natural products. This review emphasizes recent studies involving naturally occurring antiulcer metabolites, categorized according to their chemical structure. Both terrestrial and marine sources are included. More than a hundred and fifty different compounds are presented, and where possible, their main mechanisms of action are summarized. Considering that Helicobacter pylori is an important causal factor in the pathogenesis of ulcer disease, an overview of some natural compounds with anti-H. pylori activity is presented.
... Swertimarin, alkaloids, steroids, triterpenoids, saponins, flavonoids, xanthones, and phenolic acid were isolated from this plant [7]. Swertiamarin is a major phytoconstituent present in Enicostemma littorale [6,7,8]. Hence, this study was aimed to evaluate the anticancer activity of the methanolic extract of E. littorale in Swiss Albino Mice. ...
Article
Cancer can affect people at all ages with the risk for most types increasing with age [1]. It caused about 13% of all human deaths in 2007[2] (7.6 million)[3]. Cancers are primarily an environmental disease with 90-95% of cases due to lifestyle and environmental factors and 5-10% due to genetics [4]. Common environmental factors leading to cancer death include: tobacco (25-30%), diet and obesity (30- 35%), infections (15-20%), radiation, stress, lack of physical activity, environmental pollutants [4]. These environmental factors cause abnormalities in the genetic material of cells[5]. Many management options for cancer exist including: chemotherapy, radiation therapy, surgery, immunotherapy, monoclonal antibody therapy and other methods. In spite of advance development of synthetic anticancer drugs in recent years, some of the drugs of plant origin have still retained their importance. Plants used in folklore medicine continue to be an important source of discovery and development of novel therapeutic agents.
... In fact, amarogentin is considered the most bitter substance known to man and is used in soft drinks as an alternative bittering agent to quinine, which has a bitterness value of only 200,000 (Capasso, Gaginella, Grandolini, & Izzo, 2003;European Medicines Agency, 2009;Keil, Härtle, Guillaume, & Psiorz, 2000). Also, secoiridoid glycosides contribute to the gastroprotective effects of Gentian root on gastric lesions, as these glycosides are associated with enhanced mucosal defensive factors via the prostaglandin pathway in the cell membrane (Niiho et al., 2006). Loganic acid (iridoids) and isogentisin (xanthones) are also biologically active as anti-inflammatory and potent MAO inhibitor, respectively. ...
... The recent discovery of receptors for aromatic and pungent compounds on enterochromaffin cells as well as intestinal receptors for bitter compounds suggests that the gut figuratively "smells," "tastes," and responds to such compounds at sites quite distant from the classic olfactory and taste receptors (Braun et al. 2007;Rozengurt 2006;Nozawa et al. 2009). When detected by oronasal and gut receptors, bitter and pungent compounds initiate preventive defensive responses in the GI tract, including enhancement of gastric mucosal protection (Holzer and Pabst 1999;Niiho et al. 2006). Such enhancement of tissue health as a response to potential toxins aligns with concepts of hormesis and has been demonstrated for a variety of bitter and pungent secondary plant metabolites (Mattson 2008). ...
... Amarogentin, a secoiridoid, is a known topoismerase inhibitor (Ray et al. 1996), chemopreventive with potential antileishmanial (Medda et al. 1999) and gastroprotective properties (Niiho et al. 2006). The combined properties (such as antihypoglycemic, antilipidemic, antiatherogenic, cardioprotective, immunodilatory, cardiotonic, antiinflammatory, analgesic, antioxidant, gastroprotective, hepatoprotective, anticholerogenic) of the three phytochemicals (mangiferin, amarogentin and swertiamaria) present in S. chirayita may be responsible for its therapeutic action against type-2 diabetes and its complications. ...
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Swertia chirayita is a highly traded medicinal plant of Nepal widely used for its anti-diabetic potential. In this study, two herbs (Swertia nervosa and Andrographis paniculata) often used as adulterants and substitutes of Swertia chirayita were analyzed for their antioxidant activity, á-glucosidase inhibitory potential and total phenolic content and compared with that of Swertia chirayita. Aqueous and 12% ethanolic extracts of the three herbs showed moderate to high antioxidant activity and moderate á-glucosidase inhibitory potential. HPLC/ DAD revealed the presence of swertiamarin and mangiferin in all the Swertia species, while Andrographis paniculata contained cinnamates such as cinnamic acid, p-coumaric acid and chlorogenic acid. The antioxidant activity and á-glucosidase inhibitory potential was evident in the two herbs indicating their relevance as substitutes for Swertia chirayita for potential early stage management of type-2 diabetes and related complications.
... 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. ...
Article
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.
... 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). ...
Article
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.
... 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). ...
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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. ...
Article
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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.
... 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). ...
Article
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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.
... 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 . ...
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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] . ...
Article
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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.
... Amarogentin, a secoiridoid, is a known topoismerase inhibitor (Ray et al. 1996), chemopreventive with potential antileishmanial (Medda et al. 1999) and gastroprotective properties (Niiho et al. 2006). The combined properties (such as antihypoglycemic, antilipidemic, antiatherogenic, cardioprotective, immunodilatory, cardiotonic, antiinflammatory, analgesic, antioxidant, gastroprotective, hepatoprotective, anticholerogenic) of the three phytochemicals (mangiferin, amarogentin and swertiamaria) present in S. chirayita may be responsible for its therapeutic action against type-2 diabetes and its complications. ...
Article
Full-text available
Swertia chirayita is a highly traded medicinal plant of Nepal widely used for its anti-diabetic potential. In this study, two herbs (Swertia nervosa and Andrographis paniculata) often used as adulterants and substitutes of Swertia chirayita were analyzed for their antioxidant activity, á-glucosidase inhibitory potential and total phenolic content and compared with that of Swertia chirayita. Aqueous and 12% ethanolic extracts of the three herbs showed moderate to high antioxidant activity and moderate á-glucosidase inhibitory potential. HPLC/ DAD revealed the presence of swertiamarin and mangiferin in all the Swertia species, while Andrographis paniculata contained cinnamates such as cinnamic acid, p-coumaric acid and chlorogenic acid. The antioxidant activity and á-glucosidase inhibitory potential was evident in the two herbs indicating their relevance as substitutes for Swertia chirayita for potential early stage management of type-2 diabetes and related complications.
... 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. ...
Article
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.
... Secoiridoid glycosides (SGs), belonging to the group of monoterpenoids, show vast biological activities, such as fungitoxic, antibacterial, choleretic, anti-inflammatory, analgetic, antipyretic, pancreatic, gastroprotective and hepatoprotective [1,2], which makes them valuable for the pharmaceutical industry [3]. Because of their bitterness, plant extracts rich in these compounds are in use for the preparation of some commercial beverages [4]. ...
Article
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Secoiridoid glycosides are naturally occurring phytochemicals of great importance for the food and pharmaceutical industry because of their various biological activities. Certain Gentiana and Centaurium species, which are recognized as the most important sources of these compounds, have become critically endangered due to overexploitation. In this study we describe a laboratory-scale approach for further implementation in large-scale production of secoiridoid glycosides, using a hairy root culture system of Centaurium maritimum L. Fritch, an underutilized and phytochemically unexplored species. Hairy roots were induced by Agrobacterium rhizogenes strain A40M70GUS and grown in Erlenmeyer flasks, as well as in RITA® temporary immersion bioreactors (TIBs). About 2–4 times higher biomass production rate and up to 8 times higher total secoiridoid glycosides production rate were achieved in RITA® bioreactors. Among the selected hairy root lines, line HR3 cultured in RITA® TIBs proved to be the most efficient considering both biomass and secoiridoid glycosides production rate.
... It is a known topoismerase inhibitor (Ray et al. 1996), chemopreventive and is reported to have antileishmanial (Medda et al. 1999) and gastroprotective properties (Niiho et al. 2006). ...
Article
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Swertia chirayita is an important medicinal plant from Nepal with anti-diabetic, anti-pyretic, anti-malarial and anti-inflammatory potential and used in therapeutic herbal preparations in parts of South Asia. The main phytochemicals in crude aqueous and ethanolic extracts of different plant parts of Swertia chirayita collected from nine different districts of Nepal representing West, East and Central Nepal were quantified using HPLC/DAD (High Performance Liquid Chromatography-Diode Array Detection). The quantities of these phytochemicals were also compared between wild and cultivated plant parts of Swertia chirayita. Amarogentin, mangiferin, swertiamarin were the main phytochemicals in all extracts. The highest quantity of all the three phytochemicals was found in IL (inflorescence and leaf mixture) of all the collected plants samples. There was no significant difference in the amounts of these three phytochemicals between extracts from wild and cultivated plants. The result from this study substantiates the validity of cultivated Swertia chirayita for medicinal purposes and trade.
... 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). ...
Article
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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. ...
Article
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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.
Article
Objectives: Radix Gentianae is a traditional Chinese medicine derived from medicinal plants of the family Gentianaceae. Its pharmacological effects have been primarily attributed to the presence of a number of secoiridoid glycosides, in particular gentiopicroside and swertiamarin. In this study, a rapid and sensitive method based on ultrafast liquid chromatography-tandem mass spectrometry has been developed for the simultaneous determination of gentiopicroside and swertiamarin in rat plasma using paeoniflorin as internal standard (IS). Methods: After liquid-liquid extraction with ethyl acetate-isopropanol (95 : 5, v/v), separation was achieved on a Shim-pack XR-ODS C18 column (75 mm × 3.0 mm, 2.2 μm) with a mobile phase consisting of methanol : 0.1% formic acid (30 : 70, v/v) at a flow rate of 0.4 ml/min. Detection on an API 3200 QTRAP mass spectrometer equipped with an electrospray ionization source operated in the negative ionization mode was performed by multiple reaction monitoring of the precursor-to-product ion transitions of gentiopicroside, swertiamarin and IS at m/z 401.0 → 179.0, 419.0 → 179.1 and 525.1 → 121.0 respectively. The calibration curves were linear over the concentration range of 20-10 000 and 2-1000 ng/ml for gentiopicroside and swertiamarin with corresponding lower limits of quantification of 20 and 2 ng/ml. The limits of detection were 4 and 0.5 ng/ml for gentiopicroside and swertiamarin, respectively. The intraday and interday precisions were below 11.9% for gentiopicroside and below 9.5% for swertiamarin in terms of relative standard deviation, and the accuracy was within ±8.3% for gentiopicroside and within ±10.2% for swertiamarin in terms of relative error. Extraction recovery, matrix effect and stability were satisfactory in rat plasma. The method was fully validated and applied to a pharmacokinetic study involving oral administration of a Radix Gentianae extract to groups of male and female rats. Key findings: Results showed that in female rats, both compounds were absorbed to a greater extent and eliminated more slowly than in male rats, although the rate of absorption was similar in the two groups. Conclusions: There were remarkable differences in pharmacokinetic properties of gentiopicroside and swertiamarin between male and female rats. The results will provide helpful information for the development of suitable dosage forms and clinical references on rational administration.
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Methanol extracts of aerial parts and roots of five centaury species (Centaurium erythraea, C. tenuiflorum, C. littorale ssp. uliginosum, C. pulchellum, and Schenkia spicata) were analysed for their main secondary metabolites: secoiridoid glycosides, a group of monoterpenoid compounds, and phenolics (xanthones and flavonoids), and further investigated for antioxidant capacity and antimicrobial activity. The results of ABTS, DPPH, and FRAP assays showed that above ground parts generally displayed up to 13times higher antioxidant activity compared to roots, which should be related to higher phenolics content, especially flavonoids, in green plant organs. Secoiridoid glycosides showed no antioxidant activity. All the tested extracts demonstrated appreciative antibacterial (0.05-0.5 mg ml(-1)) and strong antifungal activity (0.1-0.6 mg ml(-1)). Our results imply that above ground parts of all centaury species studied, could be recommended for human usage as a rich source of natural antioxidants and also in food industry as strong antimicrobial agents for food preservation.
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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.
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Swertia chirayita is an essential medicinal plant from Rangpur, Bangladesh with anti-diabetic, antipyretic, anti-malarial and anti-inflammatory potential and used in therapeutic herbal preparations in parts of South Asia. Ethanolic extracts of fresh stem of Swertia chirayita collected from rangpur region of Bangladesh. Antibacterial activities against 8 pathogenic bacteria, 4 Gram positive and 4 Gram negative, by disc diffusion method. The produced zone of inhibition for ethanolic extract against Staphylococcus aureus, Bacillus megaterium and Escherichia coli were 8mm, 9mm and 9mm at 30μg/disc dose respectively. At 90 μg/disc dose, the produced zone of inhibition against the same bacteria was 15mm, 13mm and 12mm respectively
Article
The biotransforamtion of swertiamarin has been carried out using Aspergillus Niger. The results showed that 60% swertiamarin were metabolized into two metabolites during the 5 days of biotransformation. The metabolites were identified as erythrocentaurin and 5-ethylidene-8-hydroxy-3,4,5,6,7,8-hexahydro-1Hpyrano[3,4-c]-pyridine-1-one, a novel alkaloid, with NMR and MS. The hydrolysis of glucosidic bond catalyzed by β-D-glucosidase was found to be the rate-limiting reaction in pathway of biotransformation of swertiamarin.
Chapter
Gentian root (Gentianae radix) consists of the dried rhizomes and roots of Gentiana lutea L. (Gentianaceae). It occurs as single or branched subcylindrical pieces of various lengths and usually 10–40 mm in thickness. The smooth, transversely cut surface shows a bark, occupying about one-third of the radius, separated by the well-marked cambium from an indistinctly radiate and parenchymatous xylem. Powdered gentian roots show specific diagnostic characters, namely fragments of the subero-phellodermic layer, cortical and ligneous parenchymatous cells, and lignified vessels . The raw material contains gentiopicroside (also known as gentiopicrin), swertiamarin and sweroside, and a very small amount of amarogentin, which causes the bitter taste. Also present are xanthones (gentisin , isogentisin, gentioside), phytosterols, phenolic acid, trisaccharides (gentianose), polysaccharides (pectin), and essential oil. The bitterness of the raw material stimulates secretions in the gastrointestinal tract, especially of gastric juice. Traditionally, Gentianae radix is used to increase the appetite during recovery from acute atonic dyspepsia. Its antihepatotoxic, adaptogenic, and anti-inflammatory activities are also postulated from many experiments. Possible effects on the central nervous system of Gentianae radix have been investigated such as antidepressant and analgesic activities in mice. Extract of G. lutea showed radioprotective activity, probably due to its antioxidant activity.
Article
Histochemical localization using the β-Glc Yariv reagent and immunolocalization with arabinogalactan protein (AGP) reactive antibodies (LM2, JIM13, JIM15, JIM16, MAC207) were performed during morphogenic induction in root cultures of Centaurium erythraea Rafn cultured on half-strength MS medium without plant growth regulators. The observations revealed that β-Glc Yariv reagent specifically bound to AGPs in cells of the root epidermis and central cylinder. Monoclonal antibodies recognizing AGPs were localized in epidermal cells and cells of the central cylinder (LM2 , JIM16), vascular tissue (JIM15), globular somatic embryos (LM2, MAC207), and de novo-formed meristematic centers in the root cortex (JIM16). The effect of β-Glc Yariv reagent was investigated after supplementation (0–75 μM) in the culture medium. The morphogenetic potential was increased at lower concentrations (15–25 μM) of treatment with β-Glc Yariv reagent but inhibited (40 %) at the highest concentration. These results implicate that AGPs play a significant role during the development of somatic embryos and adventitious shoots in root cultures of C. erythraea.
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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.
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Kunisuke Izawa was born in Hyogo, Japan, in 1945, and received his B.A. in 1968 and Ph.D. in 1973 from Osaka University under the direction of Professor Takayuki Fueno. He then joined the Central Research Laboratories of Ajinomoto Co., Inc., where he studied the cobalt-catalyzed amidocarbonylation (Wakamatsu) reaction. After studying a natural product synthesis as a postdoctoral fellow at MIT (with Professor George H. Buchi) for 2 years, he returned in 1981 to Basic Research Laboratories in the same company aiming at the discovery of new methodology for pharmaceuticals. In 1990, he moved to the Process Research Laboratories as a general manager. Since then, he has been engaged in the process development of pharmaceutical fine chemicals in Ajinomoto. In 2006, he became an advisor at AminoScience Laboratories in the same company, after serving as a corporate executive fellow for 7 years. He is also serving as regional president in the Society of Synthetic Organic Chemistry, Japan, from 2007. His research interest is in the field of organic synthesis utilizing amino acids, nucleosides, and carbohydrates.
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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.
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One of the plant genera with the longest tradition in human medicine history is a popular panacea, Centaurium, named according to Pliny because the plant's medicinal properties were reputedly discovered by Chiron the centaur. In 17th century, Culpeper has claimed that its inward or outward usage was so safe that no one could fail in the using of this wholesome plant. Centauries owe this tremendous quality to their secondary metabolites, terpenoid and phenolic compounds. Among them, secoiridoid glycosides are appearing as most abundant class of terpenoids, while pharmaceutically highly appreciated xanthones and flavonoids mostly represent the class of phenolics. A period of momentous exploration of these compounds in the genus Centaurium was the 1960s of the last century. In parallel, vast area of medicinal studies started to apply isolated compounds and herbal extracts, as well to investigate the principles of their positive influence to many human health issues, such as diabetes, digestive and neurological disorders, cancer, and cardiovascular diseases. In modern times, centauries and the compounds they produce still represent the subject of many medicinal and/or pharmacological studies. Their significance is highlighted by the metaanalysis: Google Scholar returns 72 academic titles (without citations), which in the same time contain either the word Centaurium or “centaury” and are dealing with some phytochemical analytics and/or medicinal aspects of herbal extracts. In only last 5 years, totally 15 studies were engaged in elucidation of medicinal or biological activity of centauries, such as antidiabetic activity—five studies; antimicrobial activity—four studies; toxicity (including cytotoxicity)—three studies; and hepatoprotective, gastroprotective, and vasodilatory effects—one study of each. Hence, there is an evident tendency and scientific interest for in-depth research on phytochemistry of the genus Centaurium s.l. and extensive insight into their modes of action to the human health. This study will offer a comprehensive and comparative overview on the secondary metabolites' analytics throughout the genus, with a contextual respect to the biotechnological enhancement of their accumulation. It will also review to-date accomplishments regarding application of various herbal extracts and isolated compounds in (bio)medicinal studies.
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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.
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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
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)
  • Namba
Namba T (1993) Wakan–Yaku Hyakka–Jiten. (The encyclo-pedia of Wakan–Yaku, Japanese–Chinese herbal drugs) (in Japanese). Hoikusha, Tokyo, pp 188–189
Castellion AW (1975) Protective effect of Pepto-Bismol liquid on the gastric mucosa of rats
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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.
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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.
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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.
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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.
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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.
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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.
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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.
Article
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.
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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.
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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.
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.
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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.