ArticleLiterature Review

Gymnema sylvestre R. Br., an Indian Medicinal Herb: Traditional Uses, Chemical Composition, and Biological Activity

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Abstract

Gymnema sylvestre R. Br. is one of the most important medicinal plants that grows in tropical forests in India and South East Asia. Its active ingredients and extracts of leaves and roots are used in traditional medicine to treat various ailments and they are present in the market for pharmaceutical and parapharmaceutical products. Commercial products based on substances of plant origin that are generally connoted as natural have to be subjected to monitoring and evaluation by health authorities for their potential impacts on public health. The monitoring and evaluation of these products are critical because the boundary between a therapeutic action and a functional or healthy activity has not yet been defined in a clear and unambiguous way. Therefore, these products are considered borderline products, and they require careful and rigorous studies, in order to use them as complement and/or even replacement of synthetic drugs that are characterized by side effects and high economic costs. This review explores the traditional uses, chemical composition and biological activity of G. sylvestre extracts, providing a general framework on the most interesting extracts and what are the necessary studies for a complete definition of the range of activities.

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... In addition to this, other therapeutic biomolecules are flavones, α and βchlorophylls, phytin, formic acid, butyric acid, tartaric acid, hentri-acontane, lupeol, βamylin related glycosides, pentatriacontane and stigmasterol (Gupta and Solanki, 2015;Tiwari et al., 2014;Hong-Min et al., 1992;Wen-Cai et al., 2000;Porchezhian and Dobriyal, 2003;Khramov et al., 2008;Sangeetha and Jegadeesan, 2012;Zhen et al., 2008;Devi and Srinivasan, 2011;Devi et al., 2006;DiFabio et al., 2015;Kiran et al., 2014;Wang et al., 2014;Yew et al., 2001;Yogalakshmi et al., 2014;Zarrelli et al., 2013aZarrelli et al., , 2013b;DiFabio et al., 2015;Kiran et al., 2014). It also removes cough by inducing vomiting and paste is used as an ointment in case of insect bite (Malik et al., 2008;Khanna and Kannabiran, 2009;Malik et al., 2010;Osman et al., 2010;Tiwari et al., 2014;Gupta and Solanki, 2015;Zhen et al., 2008;Devi and Srinivasan, 2011;Devi et al., 2006). ...
... In addition to this, other therapeutic biomolecules are flavones, α and βchlorophylls, phytin, formic acid, butyric acid, tartaric acid, hentri-acontane, lupeol, βamylin related glycosides, pentatriacontane and stigmasterol (Gupta and Solanki, 2015;Tiwari et al., 2014;Hong-Min et al., 1992;Wen-Cai et al., 2000;Porchezhian and Dobriyal, 2003;Khramov et al., 2008;Sangeetha and Jegadeesan, 2012;Zhen et al., 2008;Devi and Srinivasan, 2011;Devi et al., 2006;DiFabio et al., 2015;Kiran et al., 2014;Wang et al., 2014;Yew et al., 2001;Yogalakshmi et al., 2014;Zarrelli et al., 2013aZarrelli et al., , 2013b;DiFabio et al., 2015;Kiran et al., 2014). It also removes cough by inducing vomiting and paste is used as an ointment in case of insect bite (Malik et al., 2008;Khanna and Kannabiran, 2009;Malik et al., 2010;Osman et al., 2010;Tiwari et al., 2014;Gupta and Solanki, 2015;Zhen et al., 2008;Devi and Srinivasan, 2011;Devi et al., 2006). ...
... In another study, Gholap and Kar (2005) discovered that gymnemic acid was capable of reducing corticosteroid hormones in dexamethasone-induced hyperglycemia in mice (EI-Shafey et al., 2013;Saneja et al., 2010;Venkatesham et al., 2010;Tiwari et al., 2014;Brekhman and Dardymov,1969;Cane, 1990;Warren et al., 1969;Agarwal et al., 2000;Alam et al., 2011). Gymnemic acids are thought to be responsible for its antidiabetic activity and it is the major component of an extract shown to stimulate insulin release from the pancreas (Thakur et al., 2012;Tiwari et al., 2014;Devi et al., 2006;DiFabio et al., 2015;Kiran et al., 2014). ...
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This review paper is the collection of literature updates on ethnobotany, phytochemistry and pharmacological activities of a rare medicinal plant Gymnema sylvestre R. Br., (madhunashini or sugar destroyer). Gymnema sylvestre with significant medicinal properties has played an important role in Indian traditional system of folk medicine; Ayurveda and homeopathic system of medicine. Herbal preparations of Gymnema sylvestre are presently used in tea bags (herbal-chai), health tablets, supplements, beverages, confectioneries and in food items as an effective natural remedy for diabetes, asthma, obesity, arthritis, besides being used for osteoporosis, constipation and anti-inflammatory. All the herbal products of Gymnema sylvestre are available in India and international market under brand names such as HimalayaTM Pure herbs, Bangalore, India (Gymnema-sugar desroyer tablets), Vitamin Shoppe Gymnema sylvestre (sugar destroyer), Gymnema gold (Nutrigold), NovelTM Nutrients Gymnema tablets, Sandhus, diabetic tea (India) with Gymnema sylvestre, Good' N Natural (Gymnema sylvestre tablets), Product of China (Gymnema tea), Natures Plus®, The energy supplements herbal actives, Gymnema sylvestre (tablets), Natures Answer, Gymnema sylvestre (tablets), Natures way® Gymnema sylvestre (tablets), GNC® Herbal Plus Standardized, Gymnema sylvestre (tablets), Body Slatto Tea®, Gymnema®, Gymnema Diet®, Sugar Off®, GlucosetTM, Cinndrome XTM, and PilisoftTM. In India, rural community consume different parts (leaves, roots, stem and flowers) of fresly grown Gymnema sylvestre as a chief herbal medicine for the treatment of many health disorders. Therefore, herbal medicines play an important role in a primary health care sector of many developing countries. Furthermore, novel discovery of new bioactive compounds of therapeutic activities mimicking the synthetic drugs is another challenging aspect of pharmaceutical biotechnology. This also opens a new door of alternative chief herbal medicine (bioactive compounds) for many deadly viral, bacterial, and fungal diseases. Finally, the experimentally tested pharmaceutical activitis of Gymnema sylvestre also provide an opportunity for further evaluation of the proposed drugs for establishing their candidature as alternative drugs for the treatment of many human health disorders.
... The first two fractions were analyzed by LC-MS and compounds 14-17 were identified from the water fraction and compounds 2, 3, 12 and 13 were identified from the methanol fraction (Table 1). Vanillic acid (14) Vanillic acid (14) cis-Cinnamic acid (2) 3-Butenyl isothiocyanate (5) 2,4-dihydroxy-1,4(2H)benzoxazin-3-one (DIBOA) (13) p-Coumaric acid (15) Caffeic acid (16) trans-Cinnamic acid (3) Benzyl isothiocyanate (6) Dihydrophenanthrenes (18)(19)(20) Ferulic acid (17) cis-3-Hexen-1-ol (7) Tetrahydropyrenes (21)(22) trans-2-Hexenal (8) Benzaldehyde (9) β-Ocimene (10) α-Farnesene (11) Scheme 1. Separation procedures of compounds 1-17. ...
... Many of these compounds can interfere with the germination and/or growth of other plants (14,25) and in this way they can affect structural and functional processes of coexisting plant species at community level (5,19). In particular, many studies evaluate the effects of natural substances on germination and plant growth, focusing mainly on their potential use in agroecosystem management (14,18,(31)(32)(33). ...
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This study was conducted to test five phenolic and cyanogenic glycoside compounds for growth regulating activity on the germination and seedling growth of Portulaca oleracea L., Amaranthus retroflexus L., and Lactuca sativa L. at different concentrations. Overall, the tested compounds revealed growth-regulating activity in species-specific and concentration dependent manner. The most powerful effects were much pronounced on seedling growth rather than on germination. In fact, the compounds 1 (amygdalin) and 2 (salicylic acid) were the most phytotoxic on root growth of P. oleracea, and they caused, respectively, an inhibition of 55% and 85% at 10⁻⁶ M and 10⁻⁴ M. On the other hand, the lettuce seedling growth was more sensitive than weeds growth to the compounds 4 (3,4,5-trihydroxybenzoic acid) and 5 (7-hydroxycoumarin), which exhibited a moderate inhibition at the highest concentration. This selectivity and specificity of these active allelopathic compounds could be very useful for the development of new application of natural substances to control the aggressive weeds. Thus, our findings suggest that the integration of these compounds may maintain irrigation system and reduce the massive use of agrochemicals in agro-ecosystems.
... The first two fractions were analyzed by LC-MS and compounds 14-17 were identified from the water fraction and compounds 2, 3, 12 and 13 were identified from the methanol fraction (Table 1). Vanillic acid (14) Vanillic acid (14) cis-Cinnamic acid (2) 3-Butenyl isothiocyanate (5) 2,4-dihydroxy-1,4(2H)benzoxazin-3-one (DIBOA) (13) p-Coumaric acid (15) Caffeic acid (16) trans-Cinnamic acid (3) Benzyl isothiocyanate (6) Dihydrophenanthrenes (18)(19)(20) Ferulic acid (17) cis-3-Hexen-1-ol (7) Tetrahydropyrenes (21)(22) trans-2-Hexenal (8) Benzaldehyde (9) β-Ocimene (10) α-Farnesene (11) Scheme 1. Separation procedures of compounds 1-17. ...
... Many of these compounds can interfere with the germination and/or growth of other plants (14,25) and in this way they can affect structural and functional processes of coexisting plant species at community level (5,19). In particular, many studies evaluate the effects of natural substances on germination and plant growth, focusing mainly on their potential use in agroecosystem management (14,18,(31)(32)(33). ...
Article
The study aimed to identify the mixtures of natural products to be added to the drippers (used in drip irrigation) during their preparation, so that the slow release of phytotoxic substances with the passage of water reduces or eliminates the intrusion of roots in the drippers. In field studies, we selected five phytotoxic plant species [Vetch villosa Roth., Brassica juncea L., Secale cereale L., Juncus effusus L. and Vallisneria natans L.] and their hydroalcoholic extracts were tested on two dicotyledons [Lactuca sativa L. cv Cavolo di Napoli and Lycopersicon esculentum L.] and one monocotyledon, Allium cepa L. We determined the structure of the main components of each extract. The Vetch villosa extract was most inhibitory. Further studies are required to determine whether to use the extract as such or one or more of its individual components can be used as possible additive in subsurface irrigation drip. © 2018, International Allelopathy Foundation. All rights reserved.
... The first two fractions were analyzed by LC-MS and compounds 14-17 were identified from the water fraction and compounds 2, 3, 12 and 13 were identified from the methanol fraction (Table 1). Vanillic acid (14) Vanillic acid (14) cis-Cinnamic acid (2) 3-Butenyl isothiocyanate (5) 2,4-dihydroxy-1,4(2H)benzoxazin-3-one (DIBOA) (13) p-Coumaric acid (15) Caffeic acid (16) trans-Cinnamic acid (3) Benzyl isothiocyanate (6) Dihydrophenanthrenes (18)(19)(20) Ferulic acid (17) cis-3-Hexen-1-ol (7) Tetrahydropyrenes (21)(22) trans-2-Hexenal (8) Benzaldehyde (9) β-Ocimene (10) α-Farnesene (11) Scheme 1. Separation procedures of compounds 1-17. ...
... Many of these compounds can interfere with the germination and/or growth of other plants (14,25) and in this way they can affect structural and functional processes of coexisting plant species at community level (5,19). In particular, many studies evaluate the effects of natural substances on germination and plant growth, focusing mainly on their potential use in agroecosystem management (14,18,(31)(32)(33). ...
... [3] The plant is a slow-growing, large woody, much branded, climber with pubescent young parts. [4] It is native to India where it is found in a dry forest, South East Asia, [5] and it is found in Tropical Africa. It was reported that the major active principles in this plant are triterpene saponins. ...
... [31] Anti-inflammatory, antibacterial, [32] antimicrobial. [33] Not reported (no activity test found) 5 Not reported (no activity test found) ...
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Supercritical fluid extraction (SFE) achieves a wide range of applications since the past decade as a sustainable green technology. The present study investigates the process for producing high yield by supercritical carbon dioxide (Sc-CO2) extraction form Gymnema Sylvestre R.Br. roots. The effect of temperature and pressure on the percentage of accumulative yield is demonstrated. It is found that the highest yield is obtained at temperature of 60 °C and pressure of 10 MPa. A proper review showed that there is a lack in the study of (Sc-CO2) extraction of this plant especially for optimization of SFE process which makes this study useful and valuable. For more benefit the extract which achieves highest percentage is subjected to Gas chromatography–Mass spectrometry (GC-MS) to study its chemical composition and detect the active principle compounds which present with high concentration and expected to be responsible of the pharmaceutical properties of the extract.
... The investigation of G. sylvestre in both in vitro and in vivo found pharmacological properties, including antioxidant, anti-inflammatory, anti-cancer, antidiabetic, hypoglycemic, immunosuppressive, anti-bacterial, anti-fungal, anti-parasitic, anti-malarial, hepatoprotective and nephroprotective activities. 11 In addition, the cardio-protective effect of G. sylvestre has also been reported. The active chemical ingredients of G. sylvestre have been investigated, such as polyphenols, flavonoids, triterpenoid saponin, tannins, quinones, anthraquinones, cardiac glycosides and gymnemic acid. ...
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Malaria-associated cardiac injury has been reported to be the primary cause of death due to severe malaria. The discovery of substances showing a protective effect on cardiac injury during malaria infection is urgently needed. Hence, the purpose of this study was to evaluate the efficacy of Gymnema inodorum leaf extract (GIE) on cardiac function in mice infected with Plasmodium berghei. ICR mice were treated with 1 × 10 ⁷ infected red blood cells of P. berghei ANKA (PbANKA), administered orally with GIE in 100, 250 and 500 mg/kg body weight of mice. Creatine phosphokinase (CPK) and echocardiography were carried out. It was found that CPK and heart-weight to body-weight (HW/BW) ratios were significantly higher in untreated mice than the healthy control. Moreover, impaired cardiac function in the untreated group was observed as indicated by changes in echocardiography. Interestingly, GIE exerted a protective effect on cardiac injury induced by PbANKA infection. Our results demonstrated that the parasitemia percentage, CPK, HW/BW ratio, and echocardiography in GIE treated mice were improved. However, there was no significant difference between GIE dosages. Therefore, GIE possessed a cardio-protective effect during malaria infection in mice.
... Phytochemicals and naturally derived substances have gained an advantage due to their composition of a plethora of chemicals that may enhance wound healing in many different ways. Using plants with medicinal properties to treat wounds have been found useful in fighting against infection and accelerate wound healing (75). A recent study conducted by Nigussie et al., described Lawsonia inermis and Azadirachta indica were the most studied plant species for wound healing, and the most common in vivo techniques used for the anti-inflammatory and the wound healing assays were carrageenan-induced paw edema, and excision and incision wound models, respectively (76). ...
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Although the word wound sounds like a simple injury to tissue, individual's health status and other inherent factors may make it very complicated. Hence, wound healing has gained major attention in the healthcare. The biology wound healing is precise and highly programmed, through phases of hemostasis, inflammation, proliferation and remodeling. Current options for wound healing which includes, use of anti-microbial agents, healing promoters along with application of herbal and natural products. However, there is no efficient evidence-based therapy available for specific chronic wounds that can result in definitive clinical outcomes. Under co-morbid conditions, chronic would poses numerous challenges. Use of Complementary and Alternative Medicines (CAMs) in health care sector is increasing and its applications in wound management remains like to "separate the diamonds from ore." Attempts have been made to understand the wound at the molecular level, mainly through the analysis of signature genes and the influence of several synthetic and natural molecules on these. We have outlined a review of challenges in chronic wound healing and the role of CAMs in chronic wound management. The main focus is on the applications and limitations of currently available treatment options for a non-healing wound and the best possible alternates to consider. This information generates broader knowledge on challenges in chronic wound healing, which can be further addressed using multidisciplinary approach and combination therapies.
... ere are some medicinal plants believed to treat diabetes, and scientific studies have reported certain medicinal plants do contain antidiabetic properties, such as improved insulin sensitivity and hypoglycemic activities [12]. is is often associated with their high level of phenolic compounds, flavonoids, terpenoids, alkaloids, and glycosides, which can improve insulin secretions as well as control blood glucose [13]. ...
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Traditionally, there are some medicinal plants believed to treat diabetes, as they have been proven in research studies to possess antidiabetic properties, such as improved insulin sensitivity and hypoglycemic activities, due to their high level of phenolic compounds, flavonoids, terpenoids, alkaloids, and glycosides. We conducted a systematic review to identify potential medicinal plants used during human clinical trials in the Association of Southeast Asian Nation (ASEAN) countries on prediabetic or type 2 diabetic individuals and to potentially identify any bioactive compounds involved in effectively treating symptoms of diabetes such as lowering of blood glucose. A total of 1209 reference titles were retrieved from four selected databases (Science Direct, Scopus, Springer Link, and PubMed) and only three met the inclusion criteria. Upon evaluation of the selected articles, four medicinal plants were identified: turmeric (Curcuma longa), garlic (Allium sativum L.), bitter melon (Momordica charantia), and Rosella flower (Hibiscus sabdariffa L.). Of these, only the bitter melon study did not show any significant change in the blood glucose of participants after intervention. This review demonstrates the limitations in published articles of human clinical trials for medicinal plants’ intervention for diabetes. Upon further investigations on the four identified medicinal plants included in the animal studies, the findings showed positive effects in the management of diabetes, such as hyperglycemia. Hence, further testing and standardization of the methods in the studies can be suggested for human clinical trials for reliable data collections such as methods of extract preparation, duration of intervention, and conditions set for the study design.
... G. sylvestre is the same genus that is popular in India for suppressing glucose absorption and preventing type 2 diabetes mellitus [10,11]. e leaves of this plant also have polyphenols, flavonoids, triterpenoid saponins, anthraquinones, alkaloids, tannin, quinones, and gymnemic acids, which are the major active compounds of G. sylvestre leaf extract [12]. In vitro and in vivo studies of G. sylvestre leaf extract described the pharmacological properties, including antidiabetic, anticancer, antibacterial, antioxidant, anti-inflammatory, antimalarial, hepatoprotective, and immunosuppressive activities [13]. ...
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Malaria remains a significant cause of death in tropical and subtropical regions by serious complications with hematological abnormalities consistent with high parasitemia. Hence, this study aimed to determine the efficacy of the Gymnema inodorum leaf extract (GIE) on hematological alteration in Plasmodium berghei infection in mice. Groups of ICR mice were infected intraperitoneally with parasitized red blood cells of P. berghei ANKA (PbANKA). They were administered orally by gavage of 100, 250, and 500 mg/kg of GIE for 4 consecutive days. Healthy and untreated groups were given distilled water, while 10 mg/kg of chloroquine was treated as the positive control. Hematological parameters including RBC count, hemoglobin (Hb), hematocrit (Hct), mean corpuscular volume (MCV), mean cell hemoglobin (MCH), mean cell hemoglobin concentration (MCHC), RBC distribution width (RDW), white blood cell (WBC) count, and WBC differential count were measured. The results showed that significant decreases of RBC count, Hb, Hct, MCV, MCH, MCHC, and reticulocytes were observed in the untreated group, while RDW was significantly increased compared with the healthy control. Furthermore, the WBC, neutrophil, monocyte, basophil, and eosinophil of untreated mice increased significantly, while the lymphocyte was significantly decreased compared with the healthy control. Interestingly, GIE normalized the hematological alteration induced by PbANKA infection in GIE-treated groups compared with healthy and untreated groups. The highest efficacy of GIE was observed at a dose of 500 mg/kg. Our results confirmed that GIE presented the potential role in the treatment of hematological alteration during malaria infection.
... It has been one of the major botanicals used in Ayurvedic medicine to treat disease conditions ranging from diabetes, malaria, to snakebites [7]. In vitro and in vivo investigation G. sylvestre revealed the pharmacological potentials including antidiabetic and hypoglycemic, antihyperlipidemic, antioxidant, anti-inflammatory, antiarthritic, anticancer, antimicrobial, hepatoprotective, cardioprotective, and immunosuppressive activities [8]. ...
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Malaria is still a serious cause of mortality and morbidity. Moreover, the emergence of malaria parasite resistance to antimalarial drugs has prompted the search for new, effective, and safe antimalarial agents. For this reason, the study of medicinal plants in discovering new antimalarial drugs is important and remains a crucial step in the fight against malaria. Hence, this study is aimed at investigating the antimalarial activity of Gymnema inodorum leaf extract (GIE) in Plasmodium berghei infected mice. Aqueous crude extract of G. inodorum leaves was prepared in distilled water (DW) and acute toxicity in mice was carried out. The antimalarial activity was assessed in the five groups of ICR mice employing the 4-day suppressive and curative tests. Untreated and positive controls were given DW along with 10 mg/kg of chloroquine, respectively. Any signs of toxicity, behavioral changes, and mortality were not observed in mice given GIE up to 5,000 mg/kg. GIE significantly (P < 0.05) suppressed parasitemia by 25.65%, 38.12%, and 58.28% at 10, 50, and 100 mg/kg, respectively, in the 4-day suppressive test. In the curative test, the highest parasitemia inhibition of 66.78% was observed at 100 mg/kg of GIE. Moreover, GIE prevented packed cell volume reduction and body weight loss compared to the untreated control. Additionally, GIE was able to prolong the mean survival time of infected mice significantly. The results obtained in this study confirmed the safety and promise of G. inodorum as an important source of new antimalarial agents and justify its folkloric use for malaria treatment.
... Using plants with medicinal properties to treat wounds have been found useful in fighting against infection and accelerate wound healing [10][11][12]. e fruiting branches of Choluteca and Cilicia Boiss. and Bal., along with the leaves and fruits, have been used to heal inflammatory wounds as traditional medicine in various parts of Turkey [13]. ...
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Purpose: We aimed to evaluate and compare the efficacy of neem leaves extract with normal saline irrigation practice in wound dressing on healing outcome and clinic-physiological parameters among individuals with diabetic foot ulcer (DFU). Methods: A quasiexperimental with repeated measures design was used on two study groups. One group received neem leaf extract wound irrigation and another group received normal saline wound irrigation. Study participants were randomly assigned to each group from 100 DFU individuals. Demographic and clinical data sheets were used to collect baseline information. Random blood sugar and HbA1C measurement was performed on the initial day of visit for all participants. We used the PUSH tool for wound assessment (wound surface area, exudate amount, and tissue type), and clinic physiological parameters (temperature, pulse rate, respiration, blood pressure, wound pain, wound infection, and local warmth) assessment was performed at baseline and then at the end of each week till four weeks were completed. Participants attended a foot clinic every 3rd or 4th day for wound care. Results: Reduction of wound healing score (PUSH score) and other wound variables improved significantly in the neem leaves extract group (p < 0.001). There were no significant changes in the clinic-physiological parameters. Conclusion: Neem leaves extract irrigation for foot ulcers is considered to be very safe as it did not cause any complication systematically during the study. Neem leaf extract solution can be used as an alternative solution for normal saline. Managing DFU requires continuous foot care and early risk identification of ulcer.
... But, during the last years, the use of natural products, pure or in mixture, has increased for food, voluptuous, aesthetic or therapeutic purposes, too [15]. In the continuous scientific research of new safe and effective drugs, there has been a rediscovery of natural substances as a potential reservoir of innovative therapeutic solutions for human health with the prospect of integrating and sometimes replacing conventional drugs [16,17]. Milk thistle is a wild herbaceous plant typical of the Mediterranean regions where it grows spontaneously in almost all climates and latitudes adapting to any type of soil. ...
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The use of Silybum marianum L. for therapeutic purposes has been known since ancient times. Its phytocomplex reduces transaminases and other biohumoral indices in the course of liver disease and also in hepato-renal syndrome. In particular, the flavonolignan component has shown properties that would partially explain the ability of the phytocomplex to induce a certain regeneration of liver cells, stimulate the cellular elimination of toxins and reduce the inflammatory component, present in fatty, alcoholic and hormonal therapies with steroids. S. marianum is also successfully used in the treatment of patients with symptomatic chronic hepatitis, with complete disappearance of clinical symptoms, such as asthenia, loss of appetite, severe meteorism, dyspepsia, and with normalization of transaminases. The same results can be obtained in patients undergoing heavy chemotherapy cycles. Modern herbal medicine uses it in decoction or infusion, however with some caution in patients suffering from hypertension, due to the presence of tyramine. In addition, the extracts of the roots have antioxidant, diuretic and febrifugal properties and those of the leaves have aperitif properties. It is therefore interesting to provide a picture of the different non-flavonolignanic components (terpenes, steroids and essential oils) of the plant and their properties, which have perhaps been wrongly neglected over the past few years.
... It is reported that G. lactiferum is evidently a form of G. sylvestre. Similar to G. lactiferum, Evidence-Based Complementary and Alternative Medicine 3 leaves of G. sylvestre are widely used in the treatment of several ailments including diabetes mellitus, and this fact is further strengthened by the isolated antidiabetic components, gymnemic acids (gymnemic acid I, II, III, and IV), from G. sylvestre [39][40][41]. ...
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The use of medicinal plant extracts and their isolated bioactive compounds for the management of diabetes mellitus has been tremendously increased in recent decades. The present study aimed at providing in-depth information on medicinal flora that has been widely used in the Sri Lankan traditional healthcare system for the management of diabetes mellitus. The data of this review article were obtained from published articles from January 2000 to September 2020 in scientific databases of PubMed, Web of Science, and Google Scholar. In this review, a total number of 18 medicinal plants with the antidiabetic activity were expressed, and their isolated antidiabetic active compounds were highlighted as new drug leads. Results of the reported studies revealed that medicinal plants exert a potent antidiabetic activity via both in vitro and in vivo study settings. However, bioactive compounds and antidiabetic mechanism (s) of action of many of the reported medicinal plants have not been isolated/elucidated the structure in detail, to date. Reported antidiabetic medicinal plants with other properties such as antioxidant and antihyperlipidemic activities deliver new entities for the development of antidiabetic agents with multiple therapeutic targets. This is a comprehensive review on potential antidiabetic activities of the Sri Lankan medicinal plants that have been widely used in the traditional healthcare system. The information presented here would fill the gap between the use of them by traditional healers in the traditional medicine healthcare system in Sri Lanka and their potency for development of new drug entities in future.
... Its leaves contain gurmarin, flavonoids, triterpenoid and saponins. The most bioactive compound of this plant are gymnemic acids, a class of tri-terpenoidsaponins, which have the effect of put down the taste of sweetness on the tongue from sucrose, xylitol, stevia and made up sweeteners such as aspartame (Liu et al., 2004 andDi-Fabio et al., 2015). In Japan, there were 50 tons of GSL are consumed every year for weight loss. ...
... us, traditional medicines of plant origin have recently garnered more attention because of several factors such as easy availability, safety, affordability, and efficacy as well as cultural acceptability [3][4][5]. ...
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The rhizomes of Curcuma longa L. (CL) have been widely used in herbal medicines worldwide. It has been shown to possess prophylactic effects against oxidative stress. However, there is a paucity of information regarding the protective role of CL against oxidative stress in the absence of toxic agents. The aim of the study was to elucidate the antioxidative stress pharmacodynamics of CL. Eighteen 12-week-old Sprague-Dawley rats weighing about 300 ± 25 gm were divided equally into six groups. Four of the groups were supplemented with CL at 100 mg/kg b.w./day orally (P.O.) and labeled as 1st, 3rd, 5th, and 6th day groups. The PCx (positive control) group was given distilled water orally, and the NCx (negative control) group rats were provided with food and water ad libitum. Blood samples were collected, and rats were sacrificed on days 1, 3, 5, and 6 (2 h) posttreatment. The blood was used for oxidative stress enzyme analysis (SOD, GSH-Px, and MDA) and liver (ALT) and kidney (creatinine) function assay, and the liver was dissected for histology. The results revealed that CL exhibited an antioxidative stress effect in the liver and kidneys as indicated by the low levels of ALT and creatinine. In response to antioxidant enzymes, especially that of the 3rd-day treatment group, an increase in SOD and GSH-Px indirectly caused an alleviation of oxidative stress, leading to a much lower level of MDA. It was concluded that treatment with CL at 100 mg/kg b.w./per day for three consecutive days demonstrated the highest efficacy in abating oxidative stress in rats.
... Plants are real reservoirs of secondary metabolites belonging to different classes of substances [3][4][5], some structurally very complex [6][7][8]. The interest in the isolation and structural determination of natural compounds is strictly in relation to their possible use as herbicides [9][10], algaecides [11][12][13], insecticides or drugs [14]. The present study was designed to evaluate the antibacterial activity of several extracts of G. sylvestre leaves and eight triterpenes isolated from the most active extract. ...
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Gymnema sylvestre is a commonly used herb in Ayurvedic medicine. The demand for its extracts in the commercial and pharmaceutical fields has been steadily increasing in recent years. Its extracts are used to treat various ailments as well as for their antimicrobial properties. This study has evaluated the antimicrobial effects of different G. sylvestre extracts and of eight triterpenes isolated from the most active extract on six bacterial poultry pathogens i.e. Bacillus subtilis, Enterococcus faecalis, Staphylococcus aureus, Pseudomonas aeruginosa, Escherichia coli and Enterobacter aerogenes. In particular, it has been evaluated the minimum inhibitory concentration (MIC) and minimal bactericidal concentration (MBC) of all extracts and isolated triterpenes. Finally, the cytotoxicity activity of triterpenes was evaluated by MTT assay and their antioxidant activity in basal and oxidant conditions by DCFH-DA assay.
... Many studies refer that specific herbal extracts have shown both antioxidant and antidiabetic activities [7]. Integrated antioxidant, anti-inflammatory and antithrombotic mechanisms exerted by phytochemicals present in herbs have been referred to efficiently prevent diet-related diseases like atherosclerosis and type II diabetes [8]. Recently, studies have focused on the role of antioxidants in preventing chronic inflammatory diseases. ...
Article
Background: The present work evaluated the in vitro antioxidant, antithrombotic, antiatherogenic and antidiabetic activities of Urtica dioica, Sideritis euboea and Cistus creticus and investigated pasta fortification with the most bioactive one. The methods employed were total phenolic content (TPC) in mg of gallic acid equivalents per g of dried-herb, 2,2'-azino-bis(3-ethylbenzothiazoline- 6-sulfonic acid) (ABTS) free radical scavenging in mg of dried-herb, cupric reducing antioxidant capacity (CUPRAC) in micromol trolox equivalent per g of dried-herb, platelet aggregation inhibition (PAF-PAI); plasma oxidation inhibition (POxI); and alpha glucosidase inhibition (a-GaseI) all in mg of dried-herb. Pasta fortified with the most bioactive herb was also studied for the above activities. Methods: Cistus creticus extract was more bioactive (p < 0.05) compared to Sideritis euboea and Urtica dioica in all but antithrombotic assay, where Sideritis euboea was superior to the others (TPC: 37.9 ± 0.56 versus 9.6 ± 0.83 and 5.4 ± 0.70; SA50-ABTS: 0.040 ± 0.001 versus 0.400 ± 0.010 and 0.520 ± 0.008; ACUPRAC: 860 ± 6.23 versus 170 ± 4.25 and 80 ± 3.63; IA50-PAF: 1.8 ± 0.14 versus 1.2 ± 0.10 and 5.2 ± 0.21; POxI: 0.095 ± 0.016 versus 0.216 ± 0.021 and 0.534 ± 0.029; IA50-aGase: 0.2 ± 0.01 versus 2.1 ± 0.16 and 1.7 ± 0.12). Results: Fortified pasta with cistus creticus extract exhibited significantly higher levels (p < 0.05) in all assays compared to plain pasta (TPC: 0.392 ± 0.064 versus 0.137 ± 0.020; SA50-ABTS: 9.4 ± 0.2 versus 126.9 ± 2.7; ACUPRAC: 5.4 ± 0.5 versus 0.9 ± 0.1; IA50-PAF: 1.87 ± 0.04 versus 2.28 ± 0.06; POxI: 3.21 ± 0.18 versus 12.2 ± 0.73; IA50-aGase: 8.9 ± 1.1 versus 18.2 ± 0.9). Conclusion: The current findings add to the mounting evidence on the potential health benefits to be derived from consuming pasta fortified with herbal extracts and indicate that Cistus creticus could form an ideal raw material towards the production of fortified pasta with increased nutritional value.
... Thus, regulating phenolic compounds in fruits through mineral nutrition is more considered among health-conscious consumers, because of their higher biological properties (Wang et al., 2009;Zareei et al., 2018). Otherwise, these natural products arouse great interest from scientists for their possible use in agriculture for their allelopathic potential (Ladhari et al., 2013;Gaaliche et al., 2017), antifungal (DellaGreca et al., 2007, antioxidant (Crisosto et al., 2010;Tanwar et al., 2014) and for their use in the prevention of oxidative stress-related pathologies (Di Fabio et al., 2015). Usually, phenolic compounds are naturally occurring in fruits, which act as defense against ultraviolet radiation, and have an important attribute to determine fruit sensory qualities (colour, flavour and taste) (Del Caro and Piga, 2008). ...
Article
The metabolic processes involved in fig production are influenced by macro-and micronutrients supply to the trees during the growing season. Potassium is an essential plant nutrient that influences growth and fruit quality. In this study, the effect of foliar potassium sulphate (K 2 SO 4) application on biochemical composition and an-tioxidant activity of fig was assessed in cv. Bouhouli, a commonly cultivated cultivar in Djebba (Northwest of Tunisia). Foliar potassium sulphate supply at 2% on Bouhouli trees were applied twice during the fruit growth. Results exhibited that potassium fertilization induces a significant change in total phenolic, flavonoid contents and radical scavenging activity in total fruit and achenes compared to the control. A strong correlation was observed between antioxidant activity and different phenolic compounds. The total fruit and achenes methanol extracts possess, respectively, the highest values of polyphenol by 29.3 and 25.1 mg GAE/g DW compared to the control. Similarly, the flavonoids content was increased in methanol extracts, respectively, by 36 and 48%. HPLC analyses revealed the influence of potassium on concentrations of phenolic compounds in fig sprayed with K 2 SO 4. Among the polyphenols, the chlorogenic acid, cyanidin 3-rutinoside and cyanidin 3,5-diglucoside contents increased from 0.87 to 1.70 mg/g DW under potassium spray, whereas those compounds were not detected in fig achenes. The present study provides clear evidence that potassium sulphate can be used to manipulate total phenolic concentrations in fig with strong antioxidant potential that could be benefits to human health. Thus, potassium sulphate application at 2% could improve nutritional and qualitative attributes of fig.
... Traditionally, Gymnema is used to treat diabetes, dyspepsia, constipation, jaundice, haemorrhoids, cardiopathy, asthma, bronchitis and leukoderma. In addition, it has been found to contain antidiabetic, antiobesity, hypolipidaemic, antimicrobial, antioxidant, diuretic, antihelmentic and anti-inflammatory properties (69)(70)(71). Active phytoconstituents of Gymnema include triterpene saponins (gymnemic acids and gymnemasaponins, gymnemasides), flavones, anthraquinones, resins, alkaloids, etc (72,73). Gymnemic acids of Gymnema is responsible for the antidiabetic activity. ...
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Introduction: Sulfonylurea antidiabetics are insulin secretogogues useful in the treatment of type 2 diabetic patients. The probability of adverse drug interactions is high in patients taking sulfonylureas and other drugs including herbal medicines. The present review is aimed to present the herbal drugs having interacting potentials with sulfonylurea antidiabetics. Methods: The databases such as PubMed, Google Scholar, Science Direct, Directory of open access journals (DOAJ) and reference lists were searched using the keywords drug interactions, Sulfonylureas, pharmacodynamic interactions, antidiabetic herbs, pharmacokinetic interactions and CYP2C9. Results: Sulfonylureas are primarily metabolized by CYP2C9 enzyme and the herbs like St. John’s wort and Ginkgo biloba induce CYP2C9-mediated metabolism of sulfonylureas while fruit juices like Pomegranate juice and Pineapple juice inhibit their metabolism. In addition, the antidiabetic herbal supplements such as Bitter melon, Fenugreek, Cinnamon, Gymnema, Ginseng, Ginger, Garlic, Aloe vera, Sesame, Andrographis paniculata and Neem potentiate the hypoglycemic activity of sulfonylureas, pharmacodynamically. Conclusion: Some herbal supplements are capable of interacting pharmacokinetically and pharmacodynamically with sulfonylurea antidiabetics
... Gymnemic acids (GA), found in Gymnéma sylvestre (Zarrelli et al., 2013a;Di Fabio et al., 2013;Zarrelli et al., 2013b), a long standing Ayurvedic medicinal plant (Ulbricht et al., 2011;Di Fabio et al., 2014) are antagonists at tongue glucose receptors (Sanematsu et al., 2014;Di Fabio et al., 2015) thus blunting sweet taste. In a previous study (Stice et al., in press) GA were formulated in a lozenge named Crave Crush TM to mask its bitterness and administered to healthy subjects. ...
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Reduction in sugar intake can have a positive effect on body weight and increased intake a negative impact. Gymnemic acids (GA) are antagonists at tongue glucose receptors thus blunting sweet taste. In a previous study GA were formulated in a lozenge, and administered to healthy subjects. Results showed that Crave CrushTM, containing GA, significantly reduced endpoints of intake and pleasantness for high sugar foods (HSF), but desire for HSF was not significantly reduced. The present trial re-examined the lack of significance in desire in the previous study, with greater number of subjects, additional inclusion criteria and used a cross over design to assess carryover effects. Percent of subjects who choose to eat the first candy offering subsequent to Crave CrushTM dosing, total candy consumption, pleasantness and desire ratings were assessed. Desire rating for a second candy offering immediately after Crave CrushTM, but before tasting a second candy, was significantly reduced by comparison to placebo. Additionally, study design improvements broaden the demographic applicability of this lozenge GA approach. No order effects were observed during the crossover. Subjects given Crave CrushTM lozenges also ate less candy, less often and their perceived pleasantness for their preferred candy was reduced. Crave CrushTM lozenges significantly reduced desire for and consumption of HSF relative to a placebo. This study provides further support regarding the role of GA in carbohydrate intake reduction, and broadens their potential applications as aids in supporting a healthy weight. Full text at: http://www.netjournals.org/pdf/AMPR/2017/4/17-025.pdf
... Some of these aglycones are similar to those of the Chinese variety (Ye et al., 2001b), and none of these have been detected in plants of Indian origin. In addition, none of the isolates featured gymnemagenin or gymnestrogenin as the backbone, in contrast to isolates of Indian origin (Di Fabio et al., 2015;Fabio et al., 2014). Most bioactivity studies of G. sylvestre have used the Indian type, and this study provides the first demonstration of stimulatory effects of purified compounds from the Vietnamese G. sylvestre variety on 2-NBDG uptake by 3T3-L1 adipocyte cells. ...
Article
Gymnema sylvestre (Retz.) R.Br. ex Sm. (Asclepiadaceae) is a well-known Ayurvedic anti-sweet plant for the treatment of type 2 diabetes mellitus. Although it was previously proposed that G. sylvestre exhibits chemical variation based on geography, most research on G. sylvestre has used material originating from India. Morphological and anatomical descriptions, ITS1-5.8S-ITS2 DNA sequencing, and acid hydrolysis analyses showed that G. sylvestre samples from Vietnam are distinguishable from those of Indian origin and thus suggest a dissimilarity among G. sylvestre samples with different geographic distributions. An LC-MS-guided strategy targeting 3β-glucuronide oleane-triterpenes in the Vietnamese G. sylvestre variety led to the isolation of four known compounds and nine previously undescribed compounds, named gymnemosides ND1-ND9. None of the isolated compounds were reported in the Indian sample, further supporting the geo-diversity of G. sylvestre. Three compounds, gymnemosides ND7-9, exerted significant stimulatory effects on the uptake of 2-NBDG in 3T3-L1 adipocyte cells and thus have potential as lead molecules for anti-diabetes agents.
... G. sylvestre is one of the powerful medicinal plants used from prehistoric times. It is perennial, woody climber spread through in dry forest up to height of 600 m [38]. It is commonly known as Gurmar in Hindi. ...
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Calotropis procera and Gymnema sylvestre are a perennial shrub and woody climber, respectively, and belonging to the family Asclepiadaceae. They are commonly known as milkweed family herbs. The Calotropis commonly have two species, i.e., C. procera and C. gigantean. All parts of plant exude white milky latex when cut. It has been widely used in traditional medicine due to its pharmacological active compounds found in all parts of plants such as bark, roots, and leaves and especially its latex which exudes from damaged or broken stem and leaves. G. sylvestre an ayurvedic herb came to be known as “destroyer of sugar” because in ancient times Ayurveda physicians observed that chewing a few leaves of G. sylvestre suppressed the taste of sugar. It also reported to possess antidiabetic, antioxidant, and immunomodulatory, antiulcer, and anticancer potential. The gymnemic acid is the main constituent which is responsible for number of pharmacological activities. The present review assembles the data on pharmacognostic and pharmacological potential of C. procera and G. sylvestre.
... It has been known for many years that extracts of G. sylvestre can reduce the sensations of sweetness associated with sweet tastants and inhibit activation of the chorda tympani nerve in response to these tastants (Shore, 1892;Diamant et al., 1965;Warren et al., 1969), and many sweet-suppressing compounds have been isolated and identified from extracts of G. sylvestre. Many of these are triterpenoids termed gymnemic acids that have been shown to elicit biological activity in mammals (Sinsheimer et al., 1970;Di Fabio et al., 2014). An additional compound, the 35 amino acid polypeptide gurmarin isolated from G. sylvestre extracts, has also been shown to reduce responses to sweet compounds, including sucrose, in the rat (Imoto et al., 1991) and in mice (Ninomiya and Imoto, 1995). ...
Article
The detection and grading of tastes corresponding to different taste modalities can be tested in engaging laboratory sessions using students themselves as test subjects. This article describes a series of experiments in which data pertaining to the detection of salty and sweet tastes are obtained, and the ability of the herb Gymnema sylvestre to disrupt the detection of sucrose is quantified. The effects of blinding and different assay designs on EC50 estimation are also investigated. The data obtained allow for substantial data analysis, including non-linear regression using fixed and free parameters to quantify dose-response relationships, and the use of often underutilized permutation tests to determine significant differences when the underlying data display heteroscedasticity.
Article
Gymnema sylvestre is a plant included in Apocynaceae family and is located in many regions of Asia, Africa and Australia. It is known to have blood glucose lowering potential and, thus, is widely used in traditional and Ayurvedic systems of medicine. A scrutiny of literature revealed some notable pharmacological activities of the plant such as antidiabetic, antiobesity, hypolipidaemic, antimicrobial, free radical scavenging and anti-inflammatory. The phytoconstituents responsible for sweet suppression activity includes triterpene saponins known as gymnemic acids, gymnemasaponins, and a polypeptide, gurmarin. Efforts have been made to prepare gudmar dried extract. These extracts were subjected for preliminary qualitative analysis, quantitative estimation of terpenoides, alkaloids and various other compounds. The present review is an attempt to highlight the phytochemical screening as well as its extraction process. Also chromatographic studies gave the presence of different compounds which can be used in creating monograph for this species.
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Introduction This study is an effort to document extensively and systematically the ethnobotanical and ethnomedicinal knowledge in the four districts (Puri, Cuttack, Bhadrak, and Mayurbhanj) of Odisha in Eastern India. It provides new insights into the rich ethnomedicinal knowledge and plants biodiversity in these four districts. Methods The method of convenience sampling was conducted to get the ethnobotanical and ethnomedicinal knowledge of the healers. Semi-structured interviews were conducted, and the information got was quantified and documented with the aid of various databases. Eleven traditional healers endowed information on their traditional medicinal knowledge. 74 plant species belonging to 44 botanical families are documented and among these 44 botanical families, five (Rutaceae, Malvaceae, Astaraceae, Annonaceae, and Euphorbiaceae) are mostly used by the healers. The healers mainly use leaves and roots in the medicine's preparation. Results Twenty-five ailments are treated by these traditional healers, which are majorly dominated by dermatological treatments. The pharmacological mining of these 74 plants revealed that a few pharmacological and biological activities of each medicinal plant have been studied. Our study revealed that these four districts of Odisha have a rich biodiversity of medicinal plants. Conclusion Promoting the plantation of some of these species can enhance the income of the traditional healers of these districts and simultaneously make the exploitation of these plant species sustainable. We also found that the pharmacological and biological activities of many plant species are yet to be explored.
Article
Gymnema is a genus of the Apocynaceae with more than 50 species. Some of its species such as G. sylvestre and G. latifolium have been reported for their medicinal value. In this study, the genetic diversity of 20 samples of four species of Gymnema in Vietnam was evaluated using the Random Amplification of Polymorphic DNA (RAPD) and the internal transcribed spacer of nuclear ribosomal DNA (ITS-rDNA). Amplified bands obtained with primers UBC701, UBC709, and OPC4 were the highest polymorphic in RAPD analysis. The phylogenetic trees were built grouping the 20 samples into four clusters corresponding to the four Gymnema species according to morphological classification. A number of characteristic SNPs were identified for each species which can be used for authentication and differentiation. The results showed the consensus and usefulness of the two barcoding techniques in the molecular identification and characterization of the Gymnema genus.
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Wild mushrooms are an important source of secondary metabolites possessing a broad range of biological activities. In this study, eight new compounds, named furanopaxin A–F (1–6), deoxybisinvolutone (7), and coumarinvol (8) along with two known compounds were isolated from fruiting bodies of the wild mushroom Paxillus involutus (Batsch) Fr. Their structures were established based on HR-ESI-MS and 1D and 2D NMR spectroscopic data. The results of hypoglycemic assays indicated that compounds 5–8 possessed significant α-glucosidase inhibitory activities, with IC50 values ranging from 14.65 ± 1.68 to 47.55 ± 1.47 μM, and each compound could enhance glucose consumption in insulin-resistance HepG2 cells. Further analysis by molecular docking implied that compounds 5–8 could interact with the amino acid residues of α-glucosidase, supporting the hypoglycemic activity of the compounds.
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Current treatment for diabetic wounds remains a major clinical challenge. The present work was aimed at the fabrication of a novel scaffold consisting of curcumin and Gymnema sylvestre incorporated graphene oxide-polyhydroxybutyrate‑sodium alginate (GO-PHB-SA-CUR&GS) composite as an extracellular matrix platform. The novel graphene oxide-polyhydroxybutyrate‑sodium alginate composite scaffold was prepared by solution casting, into which curcumin and Gymnema sylvestre was incorporated to improve healing of normal and diabetic wounds for better tissue regeneration application. The GO-PHB-SA-CUR&GS composite was evaluated for particle size, surface charge (zeta potential), crystalline nature (XRD), and morphology (SEM). In-vitro studies with normal and diabetic fibroblast cells confirmed that the GO-PHB-SA-CUR&GS composite showed good biocompatible characteristics in terms of increased migration of wounded cells. Thus, the GO-PHB-SA-CUR&GS composite could significantly accelerate the healing of normal and diabetic wounds.
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D.E.I. Herbal Garden is situated at Dayalbagh, Agra (Uttar Pradesh) of semi-arid climate. Department of Botany, Faculty of Science, Dayalbagh Educational Institute has already established an "Herbal Garden". Around 110 medicinal plant species spread over 53 families are being grown since January 2014. Some of the important plants recorded at D.E.
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Stability study on Gymnema sylvestre extract under WHO recommended accelerated and long-term conditions for 6 and 30 months, respectively was carried out by taking gymnemagenin as a marker and by evaluating antidiabetic activity through different models. Gymnemagenin was not detected in any stability sample indicating that gymnemic acids (GAs) remain stable in the extract under the test conditions. The extract and its GA rich fraction exhibited mild α-glucosidase inhibitory activity (18–27%) that remained same during the study. Neither hypoglycemic nor anti-hyperglycemic effect was induced by the extract in normal rats in oral glucose tolerance test. The extract and GA rich fraction showed significant antidiabetic activity in alloxan-induced diabetic rats that remained same in all stability samples. Based on these findings, a shelf-life of at least 30 months is suggested for G. sylvestre extract under long-term conditions, and gymnemagenin as a marker for shelf-life assessment of products derived from the plant.
Chapter
Oxidative stress is associated with increased production of reactive oxygen species (ROS) that can pose a threat to cells by causing lipid peroxidation, protein oxidation, nucleic acid damage, enzyme inhibition and activation of cell death pathways. An uncontrollable production of ROS may lead to organ dysfunction and diseases. It has been well documented in the last few decades that antioxidant compounds are the major agents that eliminate/scavenge ROS hence inhibiting oxidative stress and hindering the onset and development of non communicable chronic diseases (NCDs). Naturally occurring antioxidant compounds in plants may contribute to their potential dietary, nutritious and curative activities against ROS-induced oxidative cellular damage and NCDs. India is endowed with a variety of natural resources and flora with antioxidant principles that can be used in traditional medicine aimed at maintaining health and curing NCDs. Indian plants are important sources of alkaloids and phenolic compounds with potential antioxidant activities. Ancient texts of Ayurveda and Charaka Samhita mention innumerable herbal formulations in the treatment of NCDs that we know are caused due to oxidative stress and free-radical damage. Scientists around the world have shown interest in the Indian system of medicine and have realized the potential of Indian plants against ROS-induced cellular damage and NCDs. Plants mentioned in the texts of Indian traditional medicine are discussed here so as to project a picture of Indian flora as potential sources of antioxidants in the prevention and management of human NCDs.
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ABSTRACT The present study was undertaken to evaluate the phytochemicals presence, total phenolic contents and in vitro antioxidant potential of methanolic extract of Gymnema sylvestre R. Br. leaves. Gymnema sylvestre commonly known as gudmar belongs to the family Asclepiadaceae. In vitro antioxidant potential was evaluated by using DPPH, hydroxyl radical, nitric oxide radical scavenging as well as ferric reducing power assays. The extract showed significant activities in a concentration dependent manner when compared with standard drug Butylated hydroxy anisole. The total phenolic content in methanolic extract of G. sylvestre leaves was 2.2 μg/mg of Catechol equivalent. The IC50 value of the DPPH method, hydroxyl radical and nitric oxide radical scavenging activity was 450, 625.33, 1723.96 μg/ml respectively. In ferric reducing power methanolic extract of G. sylvestre showed absorbance 0.13 at 500 μg/ml. Results revealed that the methanolic extract of G. sylvestre showed significant antioxidant activity. Phytochemical screening showed the presence of phenolic compound such as flavonoids, tannins and saponins which may be responsible for the activity. The results suggest that extract may act as a natural antioxidant agent and offering effective protection from free radicals. Keywords: Antioxidant activity, Gymnema sylvestre, Methanolic extract, Total phenolic content
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Diabetes is associated with the generation of reactive oxygen (ROS) and oxidative damage to various tissues. Although the mechanisms underlying the development of complication in diabetes remain unclear, much attention has been focused on the role of oxidative stress in this disease. In our on going search for therapeutic approach to the treatment of diabetes .We screened 8 extracts from tradional medical herbs for antioxidant course of this investigation, aqueous extracts of Stevia, Gymnema sylvestre, Momordica charantia, Eugenia jambolana, Trigonella foenum graecum, Swertia chirayita karst, Ocimum sanctum, Azadiracta indica exhibits high antioxidant activates and cell-protective effect. All herbs traditionally been used as medicine for treatment of inflammatoryrelated disease and recent studies have been reported that their extracts possess antioxidant, antiinflammatory and anti-diabetic effects. These herbs contain large number of active compounds, such as phenolic acid, flavonoids, triterpenoid saponins, hydroxycitric acid, tannins, urosolic acid, gymnemic acid, glycosides and slevioside, which have known ROS scavenging effects.
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In honour of Professor Lucio Previtera's 70th birthday. Abstract: Because plants are estimated to produce over 200,000 metabolites, research into new natural substances that can be used in the pharmaceutical, agrochemical and agro-industrial production of drugs, biopesticides and food additives has grown in recent years. The global market for plant-derived drugs over the last decade has been estimated to be approximately 30.69 billion USD. A relevant specific example of a plant that is very interesting for its numerous pharmacological properties, which include antidiabetic, anticarcinogenic, and neuroprotective effects is Gymnema sylvestre, used as a medicinal plant in Asia for thousands of years. Its properties are attributed to triterpenoidic saponins. In light of the considerable interest generated in the chemistry and pharmacological properties of G. sylvestre triterpenes and their analogues, we have undertaken this review in an effort to summarise the available literature on these promising bioactive natural products. The review will detail studies on the isolation, chemistry and bioactivity of the triterpenoids, which are presented in the tables. In particular the triterpenoids oxidised at C-23; their isolation, distribution in different parts of the plant, and their NMR spectral data; their names and physico-chemical characterisation; and the biological properties associated with these compounds, with a focus on their potential chemotherapeutic applications.
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Lignans and lignins are among the main metabolic products of phenylpropanoid metabolism in vascular plants. They are compounds representing the building blocks of plant cell walls. Moreover they have a broad range of biological activities such as antitumoral, antimitotic, antiviral and cytotoxic and are thought to be involved in the plant defense against pathogens and pests. In this paper we report a survey of the past and current literature about lignans and neolignans and their germination inhibitory activity on cultivated and wild species from plants of the Med-iterranean area. Some examples of synthetic method-ologies of these molecules have also been reported.
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To determine the larvicidal activity of various extracts of Gymnema (G.) sylvestre against the Japanese Encephalitis vector, Culex tritaeniorynchus in Tamilnadu, India. To identify the active principle present in the promising fraction obtained in Chlorofom:Methanol extract of Fraction 2. The G. Sylvestre leaf extracts were tested, employing WHO procedure against fourth instar larvae of C. tritaeniorhynchus and the larval mortalities were recorded at various concentrations (6.25 microg/ml); the 24h LC50 values of the G. Sylvestre leaf extracts were determined following Probit analysis. It was noteworthy, that treatment level 100 ppm exhibited highest mortality rates for the three different crude extracts and was significantly different from the mean mortalities recorded for the other concentrations. The LC50 values of 34.756 microg/ml (24.475-51.41), 31.351 microg/ml (20.634-47.043) and 28.577 microg/ml (25.159-32.308) were calculated in acetone, chloroform and methanol extract with the chi-square values of 10.301, 31.351 and 4.093 respectively. The present investigation proved that G. Sylvestre could be possibly utilized as an important component in the Vector control Programme.
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A prior national survey documented the high prevalence and costs of alternative medicine use in the United States in 1990. To document trends in alternative medicine use in the United States between 1990 and 1997. Nationally representative random household telephone surveys using comparable key questions were conducted in 1991 and 1997 measuring utilization in 1990 and 1997, respectively. A total of 1539 adults in 1991 and 2055 in 1997. Prevalence, estimated costs, and disclosure of alternative therapies to physicians. Use of at least 1 of 16 alternative therapies during the previous year increased from 33.8% in 1990 to 42.1% in 1997 (P < or = .001). The therapies increasing the most included herbal medicine, massage, megavitamins, self-help groups, folk remedies, energy healing, and homeopathy. The probability of users visiting an alternative medicine practitioner increased from 36.3% to 46.3% (P = .002). In both surveys alternative therapies were used most frequently for chronic conditions, including back problems, anxiety, depression, and headaches. There was no significant change in disclosure rates between the 2 survey years; 39.8% of alternative therapies were disclosed to physicians in 1990 vs 38.5% in 1997. The percentage of users paying entirely out-of-pocket for services provided by alternative medicine practitioners did not change significantly between 1990 (64.0%) and 1997 (58.3%) (P=.36). Extrapolations to the US population suggest a 47.3% increase in total visits to alternative medicine practitioners, from 427 million in 1990 to 629 million in 1997, thereby exceeding total visits to all US primary care physicians. An estimated 15 million adults in 1997 took prescription medications concurrently with herbal remedies and/or high-dose vitamins (18.4% of all prescription users). Estimated expenditures for alternative medicine professional services increased 45.2% between 1990 and 1997 and were conservatively estimated at $21.2 billion in 1997, with at least $12.2 billion paid out-of-pocket. This exceeds the 1997 out-of-pocket expenditures for all US hospitalizations. Total 1997 out-of-pocket expenditures relating to alternative therapies were conservatively estimated at $27.0 billion, which is comparable with the projected 1997 out-of-pocket expenditures for all US physician services. Alternative medicine use and expenditures increased substantially between 1990 and 1997, attributable primarily to an increase in the proportion of the population seeking alternative therapies, rather than increased visits per patient.
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Plants have a rich history as medicines for human use. Recently introduced plant-derived drugs include paclitaxel from Taxus (Taxaceae) species for the treatment of cancers, artemisinin for malaria therapy and the alkaloid galanthamine for the management of Alzheimer's disease. A judicious combination of chemical and biological screening techniques can provide a steady supply of lead compounds for the improved treatment of human ailments. By this means, candidate compounds can be rapidly selected for further development, as is the case for xanthones from gentians and coumarins from Peucedanum ostruthium (Apiaceae), which may be of relevance in Alzheimer's disease. Encouraging results are also being obtained for hypericin from Hypericum perforatum (Hypericaceae) in the photodynamic therapy of cancer. An aspect that must not be forgotten is that the usual biological screening procedures do not pick up prodrugs which have to be metabolized by the human body into active analogues. A good example is salicin from Salix species (Salicaceae) which is metabolized in the body to give the anti-inflammatory and analgesic compound salicylic acid. Investigations which include simulation of metabolism are thus of primordial importance.
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To determine the larvicidal activity of various extracts of Gymnema sylvestre against the Japanese Encephalitis vector, Culex tritaeniorynchus in Tamilnadu, India. To identify the active principle present in the promising fraction obtained in Chlorofom:Methanol extract of Fraction 2. The G. sylvestre leaf extracts were tested, employing WHO procedure against fourth instar larvae of C. tritaeniorhynchus and the larval mortalities were recorded at various concentrations (6.25, 12.5, 25.0, 50 and 100 µg/mL); the 24h LC50 values of the G. Sylvestre leaf extracts were determined following Probit analysis. It was noteworthy that treatment level 100 µg/mL exhibited highest mortality rates for the three different crude extracts and was significantly different from the mean mortalities recorded for the other concentrations. The LC50 values of 34.756 µg/mL (24.475-51.41), 31.351 µg/mL (20.634-47.043) and 28.577 µg/mL (25.159-32.308) were calculated for acetone, chloroform and methanol extract with the chi-square values of 10.301, 31.351 and 4.093 respectively. The present investigation proved that G. Sylvestre could be possibly utilized as an important component in the Vector Control Program.
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The rapid identification and antimicrobial susceptibility testing (AST) of bacteria in clinical blood cultures is crucial to optimise antimicrobial therapy. A previous study involving small sample numbers revealed that the addition of saponin to blood cultures, further referred to as the new method, shortened considerably the turn-around time for the identification and AST of Gram-positive cocci as compared to the current method involving an overnight subculture. Here, we extend previous results and compare the identification and AST of blood cultures containing Gram-negative bacilli by the new and current methods. The identification and AST of 121 Gram-positive and 109 Gram-negative bacteria in clinical monomicrobial blood cultures by the new and current methods and, in the case of Gram-negative bacilli, by direct (no additions) inoculation into an automated system (rapid method) was assessed using the Vitek 2 system. Discrepancies between the results obtained with the different methods were solved by manual methods. The new method correctly identified 88 % of Gram-positive and 98 % of Gram-negative bacteria, and the rapid method correctly identified 94 % of Gram-negative bacteria. The AST for all antimicrobials by the new method were concordant with the current method for 55 % and correct for an additional 9 % of Gram-positive bacteria, and concordant with the current method for 62 % and correct for an additional 21 % of Gram-negative bacilli. The AST by the rapid method was concordant with the current method for 62 % and correct for an additional 12 % of Gram-negative bacilli. Together, saponin-treated monomicrobial blood cultures allow rapid and reliable identification and AST of Gram-positive and Gram-negative bacteria.
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Acquired immunodeficiency syndrome (AIDS), caused by human immunodeficiency virus (HIV), is an immunosuppressive disease that results in life-threatening opportunistic infections and malignancies. Despite continuous advances made in antiretroviral therapy, AIDS has become the leading cause of death in Africa and fourth worldwide; the number of people with HIV is increasing at an alarming rate in India and Southeast Asia. Biodiversity of the plant kingdom has always provided a source of new drug candidates for almost all disease areas. The number of compounds exhibiting anti-HIV activity and isolated from natural sources is increasing steadily. Calanolide A, a coumarin isolated from Callophyllum lanigerum and two other natural product-derived molecules, DSB and 3-hydroxymethyl- 4-methyl DCK are phase II clinical candidates, with potential to come up as drugs for treatment of HIV infection. Here, the natural products possessing anti-HIV activity have been discussed, with main focus on recent outcomes from natural sources as anti-HIV agents.
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Gymnema sylvestre (CS 149), known to be a rich source of saponins and other valuable phytochemicals, has been analysed for antimicrobial activity. The chloroform extracts of aerial and root parts of G. sylvestre exhibited higher antimicrobial activity as compared to diethyl ether and acetone. The root extracts of chloroform have shown competitive minimum inhibitory concentration and minimum bactericidal concentration values in the range of 0.04-1.28 mg mL(-1) and 0.08-2.56 mg/mL, respectively, towards the pathogens. The GC-MS analysis of chloroform extracts has shown the presence of compounds like eicosane, oleic acid, stigmasterol and vitamin E.
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We examined the antiobesity effect of a saponin-rich fraction of a Gymnema sylvestre R. Br. aqueous leaf extract (SGE) using cafeteria and high-fat diet-induced obese rats for a period of eight weeks. SGE was orally administered at a dose of 100 mg/kg body weight once a day to the treatment group. It significantly decreased the body weight, food consumption, visceral organs weight, and the levels of triglycerides, total cholesterol, low-density lipoproteins, very low-density lipoproteins, atherogenic index, glucose, and increased the levels of high-density lipoproteins. There was no significant difference with respect to all parameters of the study in case of normal (N) diet and N diet + SGE rats. In vitro, SGE inhibited the pancreatic lipase activity. The present study gave clear evidence that the SGE has a significant antiobese action, supporting its use in traditional medicine, and can be used as a substitute for synthetic drugs.
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The use of botanicals and dietary supplements derived from natural substances as an adjunct to an improved quality of life or for their purported medical benefits has become increasingly common in the United States. This review addresses the safety assessment and regulation of food products containing these substances by the U.S. Food and Drug Administration (FDA). The issue of safety is particularly critical given how little information is available on the toxicity of some of these products. The first section uses case studies for stevia and green tea extracts as examples of how FDA evaluates the safety of botanical and herbal products submitted for consideration as Generally Recognized as Safe under the Federal Food, Drug, and Cosmetics Act. The 1994 Dietary Supplement Health Education Act (DSHEA) created a regulatory framework for dietary supplements. The article also discusses the regulation of this class of dietary supplements under DSHEA and addresses the FDA experience in analyzing the safety of natural ingredients described in pre-market safety submissions. Lastly, we discuss an ongoing interagency collaboration to conduct safety testing of nominated dietary supplements.
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Dietary supplement use has steadily increased over time since the 1970s; however, no current data exist for the U.S. population. Therefore, the purpose of this analysis was to estimate dietary supplement use using the NHANES 2003-2006, a nationally representative, cross-sectional survey. Dietary supplement use was analyzed for the U.S. population (≥1 y of age) by the DRI age groupings. Supplement use was measured through a questionnaire and was reported by 49% of the U.S. population (44% of males, 53% of females). Multivitamin-multimineral use was the most frequently reported dietary supplement (33%). The majority of people reported taking only 1 dietary supplement and did so on a daily basis. Dietary supplement use was lowest in obese adults and highest among non-Hispanic whites, older adults, and those with more than a high-school education. Between 28 and 30% reported using dietary supplements containing vitamins B-6, B-12, C, A, and E; 18-19% reported using iron, selenium, and chromium; and 26-27% reported using zinc- and magnesium-containing supplements. Botanical supplement use was more common in older than in younger age groups and was lowest in those aged 1-13 y but was reported by ~20% of adults. About one-half of the U.S. population and 70% of adults ≥ 71 y use dietary supplements; one-third use multivitamin-multimineral dietary supplements. Given the widespread use of supplements, data should be included with nutrient intakes from foods to correctly determine total nutrient exposure.
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In present study, we investigated hypoglycemic and antihyperglycemic potential of five extracts (water, ethanol, methanol, hexane, and chloroform) of four plants (i.e., seeds of Eugenia jambolana, fruits of Momordica charantia, leaves of Gymnema sylvestre, and seeds of Trigonella foenum graecum) alone and/or in combination with glimepiride in rats. Ethanol extract of E. jambolana, water extract of M. charantia, ethanol extract of G. sylvestre, and water extract of T. graecum exhibited highest hypoglycemic and antihyperglycemic activity (most active) in rats among all the extracts, while hexane extracts exhibited least activities. Most active extracts were further studied to dose-dependent (200, 100, and 50 mg/kg body weight (bw)) hypoglycemic and antihyperglycemic effects alone and in combination with glimepiride (20, 10, and 5 mg/kg bw). The combination of most active extracts (200 mg/kg bw) and lower dose of glimepiride (5 mg/kg bw) showed safer and potent hypoglycemic as well as antihyperglycemic activities without creating severe hypoglycemia in normal rats, while higher doses (200 mg/kg bw of most active extracts, and 10 and 20 mg/kg bw of glimepiride) were generated lethal hypoglycemia in normal rats. From this study, it may be concluded that the ethanol extract of E. jambolana seeds, water extract of M. charantia fruits, ethanol extract of G. sylvestre leaves, and water extract of T. graecum seeds have higher hypoglycemic and antihyperglycemic potential and may use as complementary medicine to treat the diabetic population by significantly reducing dose of standard drugs.
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Oral diseases are major health problems with dental caries and periodontal diseases among the most important preventable global infectious diseases. Oral health influences the general quality of life and poor oral health is linked to chronic conditions and systemic diseases. The association between oral diseases and the oral microbiota is well established. Of the more than 750 species of bacteria that inhabit the oral cavity, a number are implicated in oral diseases. The development of dental caries involves acidogenic and aciduric Gram-positive bacteria (mutans streptococci, lactobacilli and actinomycetes). Periodontal diseases have been linked to anaerobic Gram-negative bacteria ( Porphyromonas gingivalis , Actinobacillus , Prevotella and Fusobacterium ). Given the incidence of oral disease, increased resistance by bacteria to antibiotics, adverse affects of some antibacterial agents currently used in dentistry and financial considerations in developing countries, there is a need for alternative prevention and treatment options that are safe, effective and economical. While several agents are commercially available, these chemicals can alter oral microbiota and have undesirable side-effects such as vomiting, diarrhea and tooth staining. Hence, the search for alternative products continues and natural phytochemicals isolated from plants used as traditional medicines are considered as good alternatives. In this review, plant extracts or phytochemicals that inhibit the growth of oral pathogens, reduce the development of biofilms and dental plaque, influence the adhesion of bacteria to surfaces and reduce the symptoms of oral diseases will be discussed further. Clinical studies that have investigated the safety and efficacy of such plant-derived medicines will also be described.
Book
Antimicrobial Resistance in Developing Countries, edited by Drs. Anibal Sosa and Denis Byarugaba, and their associate editors is unique in focusing on antimicrobial resistance as it relates to, and threatens developing countries. It is curious that it has taken this long to produce a book dedicated to antibiotic resistance in this part of the world. One can ask why? since resistance is and has been so common there. In fact, whereas resistance has been addressed for the past four decades by experts in the industrialized world, studies describing the problem and the public health situation in the developing world have lagged behind. Although we have learned much from studies of the genetics and molecular biology of the problem from investigations in industrialized countries, it is in developing countries where more studies and efforts are needed. With travel encouraging the transport of microbes, the information in this book will have wide sweeping benefit, not only for developing countries, but also for the world at large. Surveillance of resistance and the prevention of resistance need attention on a worldwide basis. Improving antibiotic use requires a global effort. © 2010 Springer Science Business Media, LLC. All rights reserved.
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The medicinal plant Gymnema sylvestre R. Br. is known for its antidiabetic potential. Preliminary phytochemical screening of stem and leaf samples of the herb showed positive testforflavonoids, hydrolysable tannins, phenols, saponins, sterols and terpanoids. The ash value is below the prescribed limit according to Ayurvedic Pharmacopeia. Antimicrobial activity was checked using agar well diffusion method. Water, methanoland ethanol extracts showed activity against Staphylococcus aureus. Bacillus subtilis is sensitive to hydroalcoholic and ethanolic extracts. The gram negative bacteria were resistant to the extracts. The antioxidant potential was assessed by DPPH assay method. The results provide evidence that Gymnema sylvestre leaf extract might indeed be potential source of free radical scavenger.
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Adsorption characteristics of three kinds of adsorption resins such as D101, NKA and AB-8 for total saponins of Gymnema sylvestre were investigated. D101 resin had the best adsorption capacity for total saponins with 93.90 mg/g. The results of adsorption thermodynamic and dynamic studies of D101 resin for total saponins of Gymnema sylvestre.showed that the adsorption balance could be described by Langmuir type, the time of adsorption balance was eight hours, and adsorption ratio was stable gradually after two and a half hours. The optimal conditions of isolation and purification for the total saponins of Gymnema sylvestre by D101 resin were obtained. The crude total saponins extract solution with the concentration of 7.73 g/L was first subjected to D101 resin adsorption at the flow rate of 1.5 mL/min. Then the inpurities were eluted down by distilled water and 10% ethanol. The adsorbed total saponins were eluted down by 50% ethanol. The purity of the resulting total saponins of Gymnema sylvestre was 56.10%. The yield of the total saponins was 83.83%. The total saponins of Gymnema sylvestre could be isolated and purified by D101 resin.
Article
In this study the antibacterial activity of Gymnema sylvestre (Retz.) and Andrographis paniculata collected from Western Ghats, Kanyakumari district, South India was made against common bacterial pathogens by filter paper disc-agar diffusion procedure. Both the plants showed considerable levels of antibacterial activity. Hexane extract of Gymnema sylvestre showed maximum inhibition against Serratia marcescens MTCC 86 and the Andrographis paniculata was effective against penicillin resistant Staphylococcus aureus MTCC 87. Phytochemical study revealed the presence of steroids/ terpenoids and coumarins in the extracts of both the plants. The bio-active compounds in the medicinal plants were extracted with Hexane and Chloroform (99 %) and further resolved by thin layer chromatography. Hexane extract of Gymnema sylvestre (Retz.) have 15 compounds and in its chloroform extract 25 compounds whereas 19 compounds in Chloroform extract and five compounds with Hexane extract was found in Andrographis paniculata. Further research is needed to characterize the compounds obtained and their mechanism of action on the bacterial pathogens.
Article
Diabetes is associated with the generation of reactive oxygen (ROS) and oxidative damage to various tissues. Although the mechanisms underlying the development of complication in diabetes remain unclear, much attention has been focused on the role of oxidative stress in this disease. In our on going search for therapeutic approach to the treatment of diabetes .We screened 8 extracts from tradional medical herbs for antioxidant course of this investigation, aqueous extracts of Stevia, Gymnema sylvestre, Momordica charantia, Eugenia jambolana, Trigonella foenum graecum, Swertia chirayita karst, Ocimum sanctum, Azadiracta indica exhibits high antioxidant activates and cell-protective effect. All herbs traditionally been used as medicine for treatment of inflammatory-related disease and recent studies have been reported that their extracts possess antioxidant, antiinflammatory and anti-diabetic effects. These herbs contain large number of active compounds, such as phenolic acid, flavonoids, triterpenoid saponins, hydroxycitric acid, tannins, urosolic acid, gymnemic acid, glycosides and slevioside, which have known ROS scavenging effects.
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Saponins rich fraction of Caralluma adscendens, Gymnema sylvestre & their combination (C+G), was investigated for transdermal enhancer activity by using human cadaver skin in vitro with aceclofenac as the model drug. Moreover, FT-IR studies were conducted to understand to possible enhancement mechanism. Results shows significantly increased flux of the drug compared to control (p<0.05). Similarly permeability coefficient (Kp), cumulative amount release (Q 24) and enhancement ratio (ER) shown significant increase over control sample. FT-IR studies reveal that Gymnema & Caralluma combination (C+G) reduces peak area by 89.00 % and 75.76 % for symmetric and asymmetric stretching peaks. In addition significantly reduces percentage of secondary structures of keratin at amide I band. These results indicate that Caralluma & Gymnema enhances transdermal permeation of aceclofenac by biphasic mechanism involving partial extraction of stratum corneum (SC) lipid and interaction with SC keratin.
Article
The medicinal plant Gymnema sylvestre is famous for its antidiabetic potential in the herbal world is concerned. The Macroscopic, Physiochemical parameters, phytochemical screenings were carried out to facilitate quick identification and selection of the drug from various adulterants. The extracts prepared using successive solvent extraction techniques were screened for its antimicrobial activity by Agar well diffusion method against Streptococcus mutans, Staphylococcus aureus, Streptococcus mitis and Candida albicans with the doses 25, 50 and 100 mg/ml. The methanol extract showed strong antimicrobial activity with the zone of inhibition ranges from 12-23mm at 25mg/ml. The successive extracts of Gymnema sylvestre R.Br. was screened for its particle size, total microbial load, investigation with GC-MS and HPTLC studies. The Gymnema sylvestre hydro alcoholic extract and paste base, tooth powder base were used in the formulation of " Gurmar Herbal tooth paste " and " Gurmar Herbal Tooth powder " results found to be within the limits. This proves that the extract can be useful to treat the dental caries with the scientific documentation.
Article
In the literature there are hundreds of articles, the first dating back to 1866 and the last to 2014, on gymnemic acid, isolated from Gymnnema sylvestre, from its isolation to the determination of its biological activities. Gymnemic acid has a CAS number but its structure is not specified. Studies during the second half of the 1970s clearly demonstrated that what was being referred to as gymnemic acid is actually a very complex mixture of dozens of substances, belonging to different classes of natural compounds. This plant, whose infusions or complex mixtures of its metabolites are the basis for many formulas sold in pharmacies and by herbalists, has anti-diabetic and slimming effects. It is certainly misleading to talk about gymnemic acid as a specific molecule. There may be doubts about the exact composition of the products, and consequently about their origin and the claimed effects.
Article
Natural products have been the single most productive source of leads for the development of drugs. Over a 100 new products are in clinical development, particularly as anti-cancer agents and anti-infectives. Application of molecular biological techniques is increasing the availability of novel compounds that can be conveniently produced in bacteria or yeasts, and combinatorial chemistry approaches are being based on natural product scaffolds to create screening libraries that closely resemble drug-like compounds. Various screening approaches are being developed to improve the ease with which natural products can be used in drug discovery campaigns, and data mining and virtual screening techniques are also being applied to databases of natural products. It is hoped that the more efficient and effective application of natural products will improve the drug discovery process.
Article
Phytochemical investigation of the aerial parts of Gymnema sylvestre has led to the isolation of seven new triterpenes, six oleane types (5, 7–11) and a new lupane type (12), and of the six known analogues 1–4, 6, and 13. The structures and relative configurations of these compounds were elucidated by spectroscopic analyses, including 1D- and 2D-NMR spectroscopy and mass spectrometry, and by the comparison of their NMR data with those of related compounds.
Article
Gymnema sylvestre R. Br., one of the most important medicinal plants of the Asclepiadaceae family, is a herb distributed throughout the World, predominantly in tropical countries. The plant, widely used for the treatment of diabetes and as a diuretic in Indian proprietary medicines, possesses beneficial digestive, anti-inflammatory, hypoglycemic and anti-helmentic effects. Furthermore, it is believed to be useful in the treatment of dyspepsia, constipation, jaundice, hemorrhoids, cardiopathy, asthma, bronchitis and leucoderma. A literature survey revealed that some other notable pharmacological activities of the plant such as anti-obesity, hypolipidemic, antimicrobial, free radical scavenging and anti-inflammatory properties have been proven too. This paper aims to summarize the chemical and pharmacological reports on a large group of C-4 gem-dimethylated pentacyclic triterpenoids from Gymnema sylvestre.
Article
Diabetes mellitus (DM) is a progressive disease characterized by insulin deficiency and insulin resistance. The targets insulin receptor and PPARγ associated protein [PDB: 1IRK, 3KDU] were obtained from protein data bank. Chemsketch 12.0 software was used to draw the three dimensional structure of the phytocompounds. The drug likenesses of the compounds were evaluated by checking the Lipinski and ADMET properties by using Accord for Excel. Among the 11 compounds, eight compounds were satisfied and 4 were not satisfied the Lipinski properties. In the prediction of ADMET [Absorption, Distribution, Excretion, Metabolism, Toxicology] properties for the chosen compounds, catechin, costunolide, eremanthin, saponin were found to be toxic. After screening 4 ligands namely novel gymnemic diacetate, novel gymnemic triacetate, novel dihydroxy gymnemic triacetate, gallic acid were tested, through molecular docking interactions using Discovery Studio 2.1 version. All the 4 compounds interacted with insulin receptor and were predicted to promote the insulin signaling pathway. At the same time only 2 compounds interacted with PPARγ and were predicted to promote PPAR signaling pathway. Hence, these 2 novel compounds namely gymnemic diacetate and gymnemic triacetate were identified as potent medicinal compounds as dual agonistic ligands for insulin receptor and PPARγ.
Article
A new lignan epoxide together with the seven known lignans: pinoresinol, pinoresinol-O-β-d-glucopyranoside, pinoresinol monomethyl ether-O-β-d-glucopyranoside, lariciresinol, lariciresinol-4-O-β-d-glucopyranoside, lariciresinol-4′-O-β-d-glucopyranoside, and syringaresinol monoglucopyranoside were isolated from the hydroalcoholic and organic extracts of the whole plant of Phillyrea angustifolia L. (Oleaceae). The structure of the new constituent was elucidated by spectroscopic methods (UV, IR, and 1D- and 2D-NMR) and by mass spectrometry (HR-ESI-MS), mainly using 2D-NMR techniques.The effects of these compounds on germination and growth of dicotyledon Lactuca sativa L. (lettuce) were studied in the 10−4 to 10−7M concentration range.
Article
Methyl-α-D-mannopyranoside is a glycoside with a bitter-sweet taste. Adaptation to sucrose reduces the sweetness and adaptation to quinine sulphate reduces the bitterness of methyl-α-Dmannopyranoside. Application of Gymnema sylvestre reduces the sweetness of methyl-α-D-mannopyranoside without reducing its bitterness. These results, predicted by previous studies, contradict a recent hypothesis and report by Birch and Mylvaganam.
Article
The antimicrobial activity of saponin fractions from the leaves of Gymnema sylvestre and Eclipta prostrata was evaluated against pathogenic bacteria and fungi in an invitro condition. A series of concentrations of crude and pure saponin fractions were tested for antimicrobial activity by zone of inhibition method. The pure saponin fractions were found to be more effective against tested bacterial pathogens when compared to crude saponin fractions. The minimum inhibitory concentration (MIC) exhibited by the pure saponin fraction of G.sylvestre was found to be in the range of 600–1,200mg/l against bacterial strains and 1,400mg/l for fungal isolates. In the case of E.prostrata, the range was 1,000–1,200mg/l for bacteria and 1,400mg/l for fungal isolates. The susceptibility of bacterial pathogens for saponin fractions was in the order of P.aeruginosa, E.coli, S.typhi, K.pneumoniae, P.mirablis, S.aureus and for fungal pathogens A.fumigatus followed by A.niger and A.flavus. Whereas, A.niger was more susceptible to inhibition by E.prostrata saponin fractions, followed by A.flavus and A.fumigatus. The antimicrobial potential of saponin fractions was compared with antibiotics, Chloramphenicol and Amphotericin-B with respect to bacteria and fungi. The present study suggests that the saponin fractions G.sylvestre and E.prostrata possess significant antibacterial and antifungal activity. Our results further suggest that saponins of G.sylvestre and E.prostrata can be used as a potential fungicide against pathogenic fungi.
Article
The potential of tannins from 21 medicinal and aromatic plant leaves as antimethanogenic additives in ruminant feeds was investigated. The effect of tannin from these leaves on rumen fermentation parameters, protozoa population and methanogenesis was studied by incubating the samples [200 mg dry matter (DM)] without and with polyethylene glycol (PEG)-6000 (400 mg DM) as a tannin binder during 24-h incubation in the in vitro Hohenheim gas method. Based on the methane percentage estimated in the total gas produced, methane production in millilitre was calculated [methane volume (ml) = methane % × total gas produced (ml) in 24 h]. In the samples, crude protein and neutral detergent fibre (g/kg DM) ranged from 113 to 172 and from 352 to 444 respectively. The total phenol (TP; g/kg DM) content was highest in Terminalia chebula (274) followed by Hemigraphis colorata (71) and Sapindus laurifolia (51) respectively. In the remaining samples, it was <43 g/kg DM. Activity of tannins, as represented by the increase in gas volume on addition of PEG, ranged from 0 to 133%, with the highest being recorded in T. chebula. The per cent increase in methane on PEG addition was 0 for Ammi majus, Aristolochia indica, Cascabela thevetia, Ipomea nil and Lantana camara, illustrating that tannins present in these samples had no effect on methane concentration. The PEG addition increased the total protozoa count by >50% in A. indica and C. thevetica. One of the important findings of our study was that of the 21 samples screened, Entodinia population increased in 12 with PEG as compared to 7 where Holotricha increased, indicating higher susceptibility of Entodinia to tannin. There was no increase in the protozoa population with PEG when incubating Cardiospermum halicacabum, Clerodendrum inerme, Dioscorea floribunda, Nerium oleander and Selastras paniculatus, which strongly suggested that methane suppression recorded in these samples was not because of a defaunating effect of their tannins per se. The fermentation pattern reflected increased total volatile fatty acid (TVFA) concentration from 0 to 28.3% with PEG addition among the leaves. Our results confirmed further observations that methanogenesis in vitro is not essentially related to density of protozoa population. Secondly, medicinal and aromatic plants such as C. inerme, Gymnema sylvestre and Sapindus laurifolia containing tannins appear to have a potential to suppress in vitro methanogenesis.
Article
To review the clinical trial literature on the use and effects of natural products for cancer prevention. Clinical trials published in PubMed. There is a growing body of literature on the use of natural products for cancer prevention. To date, few trials have demonstrated conclusive benefit. Current guidelines recommend against the use of natural products for cancer prevention. Clinicians should ask patients about their use of natural products and motivations for use. If patients are using natural products for cancer prevention, they should be counseled on the current guidelines, as well as their options for other cancer prevention strategies.
Article
The effect of a herbomineral formulation (HMF) on early diabetic nephropathy was investigated. Diabetes was induced in Wistar rats by administering streptozotocin (55 mg/kg, intraperitoneally). The occurrence of early diabetic nephropathy in rats was revealed by high plasma glucose and depleted liver glycogen, decreased glucose uptake by peripheral tissue, impaired renal function, increased antioxidants and lipid peroxidation in kidney. These changes were accompanied by elevated malondialdehyde, glutathione and superoxide dismutase activity in kidney. Furthermore, increased total urine volume, urinary albumin excretion rate, urinary albumin to creatinine ratio, increased relative kidney weight, decreased glomerular filtration rate (GFR) and urinary creatinine were also observed in diabetic nephropathy rats. HMF treatment significantly lowered blood glucose, glycosylated hemoglobin, creatinine, blood urea nitrogen, triglycerides, total cholesterol, serum albumin level, total urine volume, urinary albumin excretion rate, urinary albumin to creatinine ratio and relative kidney weight, and increased urinary creatinine and GFR. Altered levels of antioxidants, viz. lipid peroxidation, glutathione and superoxide dismutase (SOD), in kidney of diabetic nephropathy rats were restored. Histopathological findings indicated dense mesangial matrix in the glomeruli of diabetic nephropathy rats, which may be due to over-activation of matrix metalloproteinases and was reduced following HMF treatment. Our experimental findings clearly demonstrate that HMF has an ability to prevent the progression of early diabetic nephropathy. Such protective effect of HMF might be due to the presence of flavonoids (catechin, quercetin, rutin) and triterpene saponins (oleanolic acid and gymnemic acid) which are known to possess potent antioxidant properties.
Article
Silybin is the major flavonolignan of silymarin and it displays a plethora of biological effects, generally ascribed to its antioxidant properties. Herein we shall describe an efficient synthetic strategy to obtain a variety of new and more water-soluble silybin and 2,3-dehydrosilybin (DHS) derivatives in which the 23-hydroxyl group was converted to a sulfate, phosphodiester, or amine group, using a solution-phase approach. Furthermore a new and efficient method for the preparation of DHS from silybin was developed and optimised. The antioxidant properties of the new compounds were evaluated in a cellular model in vivo and they displayed an antioxidant activity comparable to or higher than silybin and DHS, being able to prevent H(2)O(2)-induced generation of intracellular reactive oxygen species (ROS). Most of the derivatives also displayed a better hydrophilicity while retaining the biological activities of silybin and they might broaden the in vivo applications of this class of natural compounds.
Article
The inhibition of intestinal breast cancer resistance protein (BCRP), which restricts the absorption of xenobiotics, may increase the systemic availability of its substrates. The aim of this study was to evaluate the inhibitory effects of herbal extracts and their constituents on BCRP-mediated transport. The inhibitory effects of 9 herbal extracts and 23 isoflavonoids, including soybean-derived isoflavones, on BCRP-mediated methotrexate (MTX) transport were evaluated using BCRP-expressing membrane vesicles. The structure-inhibitory potency relationship was investigated by multiple factor analysis. Extracts of soybean, Gymnema sylvestre, black cohosh and passion flower and rutin strongly inhibited BCRP-mediated transport of MTX at 1 mg/ml, while inhibition by chlorella, milk thistle and Siberian ginseng extracts was weak. Among the 23 isoflavonoids examined, all of which inhibited BCRP-mediated transport, coumestrol showed the most potent inhibition (IC(50)=63 nM). The inhibitory potencies of 6 isoflavonoid glucosides were 10- to 100-fold lower than those of the corresponding aglycones. The addition of a 5-hydroxyl or 6-methoxyl moiety tended to potentiate the inhibition. The inhibitory potency of daidzein was decreased 100-fold by 7-glucuronidation, but was virtually unaffected by 4'-sulfation. Thus, some herbal and dietary supplements and isoflavonoids may increase the systemic availability of BCRP substrates when concomitantly given orally.
Article
Hydro alcoholic dry extracts of Gymnema sylvestre, Mentha arvensis, Solanum surratense, for treatment of a dental caries were screened for antimicrobial activity by Agar well diffusion method against Streptococcus mutans, Staphylococcus aureus,Streptococcus mitis, and Candida albicans. Among them the extracts of Gymnema sylvestre dry extract showed strong antimicrobial activity against the bacteria and fungi with the zone of inhibition ranges from 16-20mm at 25mg/ml. The other extracts such as Solanum surratense, Mentha arvensis showed concentration–dependent activity against all the tested micro-organisms with the zone of inhibition ranges from 12-24mm at various concentrations.
Article
During the screening of Mediterranean invasive plants, Oxalis pes-caprae was identified as promising species. The fresh leaves and twigs of the plant were crumbled and extracted with AcOEt. The solution was concentrated, and separated into acidic and neutral fractions. The crude neutral residue was fractionated by chromatographic procedures, followed by structure elucidation on the basis of 1H- and 13C-NMR, and MS data analysis, and six new phenyl cinnamate derivatives were identified. The phytotoxic effects of the isolated compounds on the germination and growth of the dicotyledon Lactuca sativa L. (lettuce) were studied in the concentration range from 10(-4) to 10(-7) M.
Article
Natural products have been the single most productive source of leads for the development of drugs. Over a 100 new products are in clinical development, particularly as anti-cancer agents and anti-infectives. Application of molecular biological techniques is increasing the availability of novel compounds that can be conveniently produced in bacteria or yeasts, and combinatorial chemistry approaches are being based on natural product scaffolds to create screening libraries that closely resemble drug-like compounds. Various screening approaches are being developed to improve the ease with which natural products can be used in drug discovery campaigns, and data mining and virtual screening techniques are also being applied to databases of natural products. It is hoped that the more efficient and effective application of natural products will improve the drug discovery process.