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Antidiabetic oligocyclitols in seeds ofMucuna pruriens

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Abstract

Using a combination of chromatographic and NMR techniques, the presence of D-chiro-inositol and its two galacto-derivatives is demonstrated in Mucuna pruriens seeds. The quantities detected explain the well-established antiglycaemic effect of Mucuna pruriens seeds.

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... The Cognition enhancing activity in Zandopa (Mucuna pruriens) medicines suggests its use for anti-Parkinson's activity. Parkinson disease is the most common neurodegenerative disease being treated by using Mucuna species, having antioxidant [5], antiinflammatory [6], analgesic [5], antimicrobial [7] and antidiabetic values [8]. Mucuna belonging to family Fabaceae includes approximately 150 species of annual and perennial legumes. ...
... Diet rich in leguminous plants fulfil the requirement of protein that is the reason for common use of Mucuna species in feed and food by peoples in tropical locations [9]. In addition Mucuna species acts as green manure [10] and mainly used in production of pharmaceutical formulation [11,12] to treat several disorders like Diabetes [8], nervous disorders [13], sexual disorder [14] etc. Mucuna is a common and rich source of antioxidant compounds which helps to protect oxidative damage. Earlier reports indicates that the optimization of solvents and extraction techniques have great impact on phytochemical composition of Mucuna species [15]. ...
Article
The study was designed to demonstrate the phytochemical composition and to evaluate minerals, antioxidant and antibacterial activities of different Mucuna species. Liquid Column Mass Spectrometry (LC-MS) analysis was performed to identifies the phytoconstituents like phenolic, flavonoids, alkaloids, vitamins, amino acids, anti-cancer agent, antiretroviral agents, antidiabetic agents, anti-inflammatory and anti-Parkinson’s drug. Minerals essential for healthy functioning of the human body were resoluted from these species using atomic absorption spectroscopy. The antioxidant activity was evaluated by using the DPPH and ABTS assay. The antimicrobial activities of various M. extracts were performed against some micro-organisms (Gram positive and Gram negative) using well diffusion method. The results of the present study revealed variation between some different Mucuna species. The results of LCMS phytochemical profiling indicates flavonoids and related polyphenols responsible for various pharmacological activities were the major compounds in the Mucuna seeds. Estimated mineral content in various Mucuna species shows the importance of these new wild varieties (Mucuna bracteata).Thus serve as a great platform for the food industry due to their macro and micronutrients contents in significant amount. The strong antioxidant and antimicrobial activity present in the wild Mucuna imbricata seeds may be good alternative to the communally used of Mucuna species. They can also be used as a potential source of food and anti-Parkinson’s drug in the pharmaceutical industry. Thus, the present article puts focus on the possible use of two wild Mucuna species as a substitute for Mucuna pruriens var utilis and herbal remedy against neurodegenerative disorders.
... It is possible that methanolic extraction rends more volatile compounds in this extract regarding our extracting approach. In another study, using whole seeds and a combination of chromatographic and NMR techniques, the authors reported the presence of d-chiro-inositol and its two galactose derivatives in Mucuna pruriens [64]. Inositol and galactose derivatives may have been present in our seeds but were diluted in our seed extract. ...
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Human societies demand sustainable alternatives for goods and services. Plants are sustainable sources of important metabolites with beneficial impacts on human health. There are many reported methodologies and commercial suppliers for extract preparations from Mucuna sp. They usually claim the plant is enriched with L-dopa, its distinctive metabolite. However, many present poor characterizations of the extract’s components. Here, we present polar metabolites characterization of a Mucuna seed extract, emphasizing L-dopa identification and quantification. To obtain the extracts, we follow a green and sustainable extraction protocol. The lyophilized extract is subjected to liquid chromatography and mass spectrometry to identify its primary metabolites. Additionally, we follow thin-layer chromatography to identify carbohydrates in the sample. The resultant extract has 56% L-dopa. Other main components in the extract are arginine, stizolamine, and the fructooligosaccharides sucrose and nystose. The characterized Mucuna extract can be easily standardized using powder preparation and used in several biomedical applications.
... There is possible that the methanolic extraction rends more volatile compounds in this extract regarding 13 our extracting approach. In another study, using whole seeds and a combination of chromatographic and NMR techniques, authors report the presence of d-chiro-inositol and its two galactose derivatives in Mucuna pruriens [55]. Inositol and galactose derivatives may be present in our seeds but diluted in our seed extract. ...
Preprint
Human societies demand sustainable alternatives for goods and services. Plants are sustainable sources of important metabolites with beneficial impacts on human health. There are many reported methodologies and commercial suppliers for extract preparations from the plant Mucuna sp. They usually claim to be enriched in L-dopa, their distinctive metabolite. However, there are poor characterizations of the metabolite's components in that extracts. Here, we present the metabolite characterization of a Mucuna seed extract, emphasizing the L-dopa identification and quantification. To obtain the extracts, we follow a green and sustainable extraction protocol. The lyophilized extract was subject to liquid chromatography and mass spectrometry to identify its primary metabolites. Additionally, we follow thin-layer chromatography to identify some carbohydrates in the sample. The resultant extract has a 56% L-dopa. Other main components in the extract were arginine, stizolamine, and the fructooligosaccharides sucrose and nystose. The characterized Mucuna extract can be easily standardized as powder presentation and used in several biomedical applications.
... Besides drugs used for the treatment of diabetes, several species of plants have shown hypoglycemic activity [23]. Some pharmacological studies show that the ethanol extract of the Mucuna pruriens seeds are a rich source of dietary fibers and antioxidants, and contains anti-diabetic components like saponins, squalenes, D-chiroinositol and oligocyclitols [24]. ...
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Aims: This study investigates the effect of Mucuna pruriens leaves on the liver, antioxidant parameters and lipid profile of alloxan-induced diabetic rats. Methodology: Thirty-five (35) Wistar albino rats were divided into five groups with seven (7) rats per group. The experiment was designed as follows: Group 1-NC, Normal Control; Group 2-DBC, Diabetic Control; Group 3-DG, Diabetic glibenclamide (Positive control); Group 4-DMPL Original Research Article Ibeh et al.; IRJGH, 3(3): 20-29, 2020; Article no.IRJGH.56949 21 (Diabetic Mucuna pruriens extract Low-50 mg/kg); Group 5-DMPH (Diabetic Mucuna pruriens extract High-100 mg/kg). The rats were fed with normal feed and drinking water ad libitum. The diabetic control, diabetic glibenclamide and the extract groups (50 mg/kg and 100 mg/kg) were induced with diabetes by intraperitoneal injection of 120 mg/kg bodyweight of alloxan monohydrate and confirmation was done using a glucometer. The positive control was treated with glibenclamide (6 mg/65 kg/day). Blood samples were collected from seven (7) rats in each group through the retro-orbital plexus of the eye after 28 days of treatment, thereafter, the rats were sacrificed by cervical dislocation under light ether anesthesia, and biochemical parameters were determined using standard techniques (Randox kits). Results: Mucuna pruriens leaf extract lowered blood glucose levels across the groups treated with the extract. The diabetic rat fed with Mucuna pruriens extracts showed a significant (p<0.01) reduction in hepatic ALT (Alanine Transaminase), AST (Aspartate Transaminase) and ALP (Alkaline Phosphatase) when compared to the diabetic control. Compared to the diabetic control, the extract groups showed a significant (p<0.05) reduction in serum Low-density lipoprotein (LDL) and total cholesterol with a significant (p<0.05) increase in HDL. The extract groups showed marked dose-dependent significant (p<0.05) increase in GPx over all other groups, and a significant (p<0.05) decrease in Malonaldehyde level when compared to the diabetic control group. There was no significant (p>0.05) difference in the levels of Catalase, Superoxide dismutase, and Glutathione across the groups. There is a significant (p<0.05) increase in the level of Vitamin E of extract groups when compared to the diabetic control and diabetic glibenclamide group with a significant increase (p<0.05) in Vit. C level of extract group (50 mg/kg) when compared to all other groups. Conclusion: This result of the study suggests that Mucuna pruriens have a beneficial effect on the hepatocyte and some lipid profile parameters while also increasing antioxidant defense of the body and may be of value in the management of diabetes and its complications.
... All the parts of M. pruriens plant possess medicinal value. Seeds of the plants have antidiabetics activity [20], antimicrobial activity [21], and antivenom activity [22]. The phytochemicals present in the seeds of the M. pruriens increase the fertility in men [23]. ...
Article
Objective: In recent years, herbal plants have been got more attention due to their diverse presence of phytochemicals and its biological properties. Hepatocellular carcinoma is one of the major worldwide problems primarily caused by hepatitis B and C virus infection. End-stage liver cancer treatment options are limited, thus requiring expensive liver transplantation which is not available in many countries.Methods: In the present study, the Mucuna pruriens seed extract was analyzed for phytochemicals, antioxidant activity, total phenols, and total flavonoids content. The seed extract was further analyzed for its anticancer activity by culturing liver cancer cell line. The above protocols were done by standard methods.Results: The seed extract of M. pruriens revealed more number of phytochemicals in different organic solvents. 1,1- Diphenyl- 2- picrylhydrozyl scavenging activity of plant extract was more in ethanol extract (98.051±0.547) among all other solvents. The total phenols and flavonoids content in ethanol extract were 46.442±0.353 mg gallic acid equivalent/g and 2.254±0.647 mg - quercetin equivalent /g, respectively. IC50 value of 3-(4, 5-dimethythiazol-2-yl)-2, 5-diphenyl tetrazolium bromide (MTT) analysis of Hep-2 cell line was 150 (μg/ml).Conclusion: The present study revealed about the phytochemical contents and antioxidant potential of M. pruriens seeds. Further, the MTT analysis proved that the seed extract was effective against cancer cells and also used to treat many diseases.
... Therefore, to sum up, the principal biologically active compounds (Adebowale et al., 2005;Bhat et al., 2008;Donati et al., 2005;Hope-Onyekwere et al., 2012;Manyam et al., 2004;Misra and Wagner, 2007;Shelly and Arthur, 1985) contained in Mucuna pruriens include: revista del comité científico nº 24 8 AECOSAN Scientific Committee: Allergy to Anisakis • L-Dopa (L-3,4-dihydroxyphenylalanine). It is the precursor of dopamine, and is the main constituent of the seed. ...
... It can also be used for anodyne, antiasthmatic, antispasmodic, and antitussive. It has also been used for bronchodilator, hallucinogenic, hypnotic, and mydriatic [38]. ...
Article
The importance of medicinal plants in traditional health-care practices provides clues to new areas of research and in the biodiversity of conservation. Right from the beginning, the documentation of traditional knowledge, especially on the medicinal uses of plants, has provided many important drugs for the modern day. Even today, this area holds much more hidden treasure as almost 80% of the human population in developing countries depend on plant resources for health care. Keeping this in view, the present study was initiated to document the traditionally used tribal plants and their inborn antimicrobial activity which is enhanced on the synthesis of noble metal nanoparticles.
... Hyperglycemia and hyperlipidemia are considered as most critical problems in Diabetes mellitus. The observations of the present study showed the effectiveness of STZ in producing persistent hyperglycemia in experimental animals and are in concordance with studies performed by Abdollahi et al., in 2008Lee et al., in 2009 Earlier pharmacological studies shows that the ethanolic extract of the Mucuna seeds are rich source of dietary fibres and antioxidants and it contains anti diabetic components like saponins, squalenes, D-chiro-inositol and oligocyclitols (23) . The outcome of the present study showed that Mucuna pruriens seed extract and Glibenclamide treatment significantly decreases the hyperglycemia caused by STZ. ...
Article
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Aims and Objectives: The study was to evaluate the remedial effect of alcohol extract of Mucuna pruriens seeds on pancreas and liver of Streptozotocin induced diabetic rats. Materials and Method: Five day old neonate wistar rats (n-24) were used for the study. Out of this, 6 rats were kept as Normal control i.e. Group A. Remaining 18 rats were made diabetic by intraperitoneal injection of streptozotocin (65mg/kg body weight). After 12 weeks, they were divided equally into 3 groups i.e. Group B-Diabetic control, Group C-Mucuna Pruriens group (200mg/kg), Group D-Glibenclamide group (1 mg/kg body weight). Drugs were administered orally for 28 days in group C & D. Blood Glucose Level was monitored once in a week during this period. On completion of drug treatment period, animals were sacrificed for the collection of blood and visceral organs to carry out histological and biochemical investigations. Results: The Mucuna Pruriens seed extract (200mg/kg) were effectively controlled blood glucose levels in diabetic rats. Serum insulin and cholesterol levels were significantly improved when compared to diabetic group (p >0.05). In pancreas, the islets showed increase in beta cell mass and reduced necrotic changes. Liver functions were partially restored and hepatocytes showed minimal necrotic changes. Conclusion: Mucuna pruriens seeds are capable of exerting positive structural changes in pancreas & liver through its antioxi-dant and antidiabetic properties.
... and NMR techniques [26] This study involved the combination of chromatographic and NMR techniques to Neuroprotective effects of the antiparkinson drug M. pruriens [30] The present study evaluated the neuro restorative effect of M. pruriens cotyledon powder on the nigrostriatal tract of 6 hydroxydopamine 6-OHDA lesioned rats. M. pruriens cotyledon powder significantly increased the brain mitochondrial complex-I activity but did not affect the total monoamine oxidase activity (in vitro) as having Nicotine adenine dinucleotide [33] To study the effect of M. pruriens in infertile men who were under psychological stress, trial ...
Article
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Mucuna pruriens (L.) DC. belongs to the family Fabaceae is commonly known as Velvet bean, Cowitch, Cowhage in English and Kawaanch, Kavach in Hindi. It is mainly distributed in Asia, Africa, Pacific Islands and the United State. M. pruriens has been of keen interest in phytochemical and Ayurvedic research due to its excellent medicinal values. Traditionally it is used in treating diseases such as arthritis, anxiety, cancer, cough, diarrhoea, dysentery, diabetes, dysmenorrhea, delirium, gonorrhoea, gout, impotency and sexual debility, muscular pain, parasitic infections, Parkinson's disease, rheumatic disordersas an analgesic and antipyretic, to induce vomiting, to treat snakebite and scorpion stings, sterility ,tuberculosis etc. The plant exhibit wide array of phytoconstituents like alkaloids, flavonoids, tannins and phenolic compounds which are responsible for varied potent physiological and pharmacological activities. This review is in a narrative format and consists of publications relevant to M. pruriens available in public doman.
... Successivamente la L-Dopa è stata separata e purificata per "flash chromatography" e caratterizzata con la spettrometria ESI/MS come mostrato dalla figura 14. Con l'analisi ESI/MS abbiamo osservato la presenza della L-Dopa nelle varie parti del seme: tegumento (a), arillo (b) e seme decorticato (b), oltre ai ben noti oligosaccaridi (arillo: saccarosio+Na 365.0 m/z, saccarosio+K 380.9 m/z, stachiosio+K 706.5; seme decorticato: saccarosio+K 380.9 m/z, raffinosio+K 543.0 m/z) riportati in letteratura [111]. ...
... The exact phytochemical constituent(s) present in the seeds and which may be responsible for the observed antihyperglycemic activity has not been ascertained in the present study. However, oligocyclitols (d-chiroinositol and its two galacto-derivatives) with antidiabetic properties has been reported from the seeds (Donati et al., 2005). It is quite possible that the observed antihyperglycemic activity as shown in oral glucose tolerance tests could be due to these phytochemicals. ...
Article
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Mucuna pruriens is an annual, climbing shrub with long vines that can reach over 15 m in length. Seeds of the plant have uses in folk medicines of Bangladesh as an antidiabetic agent and for treatment of infertile males. Towards validating the use of seeds as an antidiabetic agent, oral glucose tolerance tests were conducted in Swiss albino mice with methanolic extract of seeds of the plant. The extract when administered at doses of 50, 100, 200 and 400 mg per kg body weight to glucose-loaded mice significantly and dose-dependently inhibited the rise in blood sugar concentrations by 48.3, 50.5, 52.9 and 54.1%, respectively. By comparison, a standard antihyperglycemic drug, glibenclamide, when administered at a dose of 10 mg per kg body weight inhibited the increase in blood sugar concentration in glucose-loaded mice by 56.8%. Thus at the highest dose of the extract, the blood glucose lowering activity was comparable to that of glibenclamide. Taken together, the results not only validate the folk medicinal use of seeds as an antidiabetic agent but also suggest that further scientific studies should be carried out to identify the responsible phytochemical constituent(s) responsible for the observed blood sugar lowering effect.
... Using a combination of chromatographic and NMR techniques, the presence of D-chiro-inositol and its two galacto-derivatives having antiglycaemic effect was demonstrated in M. pruriens seeds (Donati et al., 2005). ...
Article
Full-text available
Mucuna pruriens commonly known as cow-age or cowitch or velvet bean or Alkushi, is a medicinal plant traditionally used in Indian medicine belongs to the family Leguminosae. M. pruriens seed is a natural source of the amino acid L-3,4-dihydroxy phenyl alanine (L-DOPA), the direct precursor to the neuro transmitter dopamine which is used widely in the treatment of Parkinson's disease (PD). Serotonin, oxitriptan, nicotine, N,N-DMT, and bufotenine are the other chemicals found in M. pruriens in addition to L-DOPA. According to Ancient Ayurvedic literature Mucuna is used as a potent aphrodisiac, geriatric tonic and vermifuge. It is also used for the treatment of menstruation disorders, constipation, edema, fever, tuberculosis, etc. In addition, Mucuna is also grown as food crop, ornamental plant, living mulch and green manure crop. The reviews summarize the botany, uses, phyto constituents and pharmacological activities of M. pruriens.
... , was demonstrated in M. pruriens seeds (Donati et al ., 2005). Galactopyranosyl d-chiro-inositols are relatively rare and have been isolated recently from the seeds of certain plants; they constitute a minor component of the sucrose fraction of Glycine max (Fabaceae) and lupins, and a major component of Fagopyrum esculentum (Polygonaceae) (Horbovitz et al., 1998). ...
Article
Full-text available
Mucuna pruriens (Fabaceae) is an established herbal drug used for the management of male infertility, nervous disorders, and also as an aphrodisiac. It has been shown that its seeds are potentially of substantial medicinal importance. The ancient Indian medical system, Ayurveda, traditionally used M. pruriens, even to treat such things as Parkinson's disease. M. pruriens has been shown to have anti-parkinson and neuroprotective effects, which may be related to its anti-oxidant activity. In addition, anti-oxidant activity of M. pruriens has been also demonstrated in vitro by its ability to scavenge DPPH radicals and reactive oxygen species. In this review the medicinal properties of M. pruriens are summarized, taking in consideration the studies that have used the seeds extracts and the leaves extracts.
... Increase in peripheral utilization of glucose and release of insulin in a way that differs from insulin [73]. The oligocyclitols present in seeds have antiglycaemic effect [74] 37 ...
Article
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Diabetes mellitus is a global metabolic epidemic affecting essential biochemical activities in almost every age group. Over the last century changes in human behavior and lifestyle have resulted in a dramatic increase in the incidence of diabetes world over. Traditional medicinal plants and herbs having potential anti-diabetic activity are being used as part of diet since prehistoric time. Scientific data on a number of medicinal plants have proved remarkable for cure of diabetes and its complications. The current paper is aimed at providing an overview of the most effective hypoglycemic plants and herbs of Fabaceae Family along with the safety profile of the species used.
... From the ancient times, the different parts of this plant like seeds, leaves and roots have been used for treatment of many diseases. The seeds of Mucuna pruriens containing Levodopa as an important constituent, have been reported for Anti – Parkinson's activity23456, Aphrodisiac activity78, Antidiabetic activity910111213, Hypoglycemic and Hypocholesterolemic activity [14], Antitumor activity [15], Antioxidant activity161718, Neuroprotective activity [19], Learning and memory enhancing effect [20], Antivenom activity2122, Anti inflammatory activity [23] etc. Phytochemical investigation revealed the presence of tryptamine, 5–HT, mucunine, mucunadine, prurienine and prurieninine2425. Several analytical methods have been reported for the determination of Levodopa based on non – aqueous titration2627, UV [27], HPLC2829 and HPTLC3031 in formulations and also in plant extracts. ...
Article
A simple, sensitive, selective HPTLC -densitometric method was developed and validated for the determination of Levodopa in seeds of Mucuna pruriens and its herbal dosage form. Analysis of Levodopa was carried out on TLC plates pre-coated with silica gel 60F 254 as stationary phase. Linear ascending development of the plate was done in a pre-saturated twin trough glass chamber. The mobile phase consisted of n-butanol – glacial acetic acid – water (5:1:4, v/v/v) at room temperature (25 ± 2º C). Camag TLC scanner III was used for spectrodensitometric scanning and analysis was done in absorption mode at 280nm. The system gave compact spot for Levodopa (R f value of 0.39 ± 0.04). The polynomial regression analysis data for the calibration plots showed correlation coefficient r = 0.999 in concentration range 100 – 1000 ng/ spot with respect to peak area. According to International Conference on Harmonization (ICH) guidelines, the method was validated for precision, recovery, robustness and ruggedness. The limits of detection and quantification were determined. The statistical data analysis showed that the method is reproducible and selective for estimation of Levodopa.
... Three novel cyclitols, D-chiro-inositol (92), and its two galacto-derivatives (93 and 94), were isolated from Mucuna pruriens which is prescribed in traditional Indian medicine and has been studied for its hypoglycemic and anti-hyperglycemic activity. They showed a significant hypoglycemic effect responsible for anti-diabetic properties of this medicinal plant [81]. ...
Article
Diabetes mellitus (DM), the third killer of the mankind health along with cancer, cardiovascular and cerebrovascular diseases, is one of the most challenging diseases facing health care professionals today. The World Health Organization (WHO) has declared that a DM epidemic is underway. Primary DM and its complications are costly to manage, not only for affected individuals, but also for healthcare systems around the world. Screening of anti-diabetic agents has been extensively investigated in the past decades. Natural products (NPs) have served as a major source of drugs for centuries, and about half of the pharmaceuticals in use today are derived from natural substances. Many natural products especially plants-derived medicines have been recommended for the treatment of DM. The present paper reviews NPs appeared in the literature with potential for DM and also identifies the research needs in this area. It mainly covers the time period from January 2004 to October 2008. The current review is divided into three major sections based on classification of the natural materials involved. The first part focuses on known and some new chemical entities isolated mainly from medicinal plants possessing anti-diabetic properties, including saponins, flavonoids, alkaloids, anthraquinones, terpenes, coumarins, phenolics, polysaccharides, and some other compounds. The second part summarizes crude extract of medicinal plants which are commonly used in the traditional Chinese medical system and have been demonstrated experimental or/and clinical anti-diabetic effectiveness, mainly including Leguminosae, Cucurbitaceae, Araliaceae, Liliaceae, Chenopodiaceae, Solanaceae, Compositae, Campanulaceae, Cornaceae, Rhamnaceae, Scrophulariaceae, Euphorbiaceae, Ginkgoceae, Gramineae, Myrtaceae, Sterculiaceae, Annonaceae, Labiatae, Crassulaceae, and Miscellaneous. The third part lists some compound formulae consisting of extracts of several plants that have been reported as beneficial for the treatment of DM, major involving Xiaokeling tablet, Ba-Wei-Di-Huang-Wan and Formula 1.
... Due to high concentrations (about 15%) of L-DOPA, seed extract is used to treat Parkinson's disease (Nagashayana et al. 2000 ). D-chiro-inositol confers antidiabetic activity (Donati et al. 2005). In traditional African medicine, M. pruriens seeds are also used for oral prophylaxis against snake venom (Martz 1992; Aguiyi et al. 1998). ...
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The mobilization of storage reserves, with particular emphasis on storage proteins of Mucuna pruriens (L.) DC., cotyledons, and embryo was investigated from the ultrastructural and biochemical points of view. Proteins and starch were the two main storage substances in cotyledons, and proteins and lipids were the main ones in the embryo. Embryo protein bodies were smaller and fewer in number than those of cotyledons. Structural and ultrastructural data determined between 24 and 48 h after imbibition and between 48 and 72 h after imbibition, the end of significant embryo and cotyledon protein mobilization, respectively, indicating more precocious storage protein mobilization in the axis than cotyledons. Moreover, storage protein mobilization in embryo and cotyledons occurred before the end of germination. Water soluble proteins were separated by sodium dodecyl sulfate polyacrylamide gel electrophoresis, producing 29 bands with molecular weights from 14 to 90 KDa. Embryo extract contained more proteins than cotyledon extract, contained seven characteristic bands, and showed a higher variability of the optical density trend than cotyledon.
Chapter
Advances in the treatment of neurodegenerative diseases (NDs) are nominal. Currently available therapies are merely symptomatic treatments that cannot prevent the development of the disease. Several herbs have been found very useful for managing neurological diseases. There are immense possibilities to discover a more successful line of ND treatment. Phytochemicals from medicinal plants may play a vital role in maintaining the chemical balance of the brain by affecting the capacity of receptors for the major inhibitory neurotransmitters. A few plants have already gained popularity for the potential treatment of NDs. This volume highlights the therapeutic role of medicinal plants and their scientific validation for improving neuronal health. It presents 15 chapters that cover the herbal treatment of NDs, including Parkinson's disease and Alzheimer's disease. The contents cover a range of pharmaceutical agents like sirtuins, berberine, rosmarinic acid and resveratrol. The book serves as a reference for pharmacology and herbal medicine scholars as well as healthcare workers interested in information about alternative and complementary therapies for neurological disorders.
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Neurodegenerative diseases (NDs) are characterized by progressive neuronal loss (structurally and/or functionally) in different regions of the brain. NDs represent one of the most important public health concerns, as they are the growing cause of death around the world, especially among the elderly. Aging has led to an increase in NDs, such as Alzheimer's disease, dementia, cerebrovascular impairment, seizure disorders, head injury, and Parkinson's disease, which are becoming critical due to their irreversibility, lack of effective medication, and the resulting social and financial burdens. Indeed, despite the noteworthy achievements in our understanding of NDs, there has been little achievement in formulating suitable therapies. Currently, the available treatments for NDs seem to be ineffective, as they only work to ease the symptoms but cannot prevent the disease's progression. The use of medicinal herbs is emerging as an alternative or integrative therapeutic against NDs because of the preconception that medicinal herbs are consequently safe. Phytochemicals from medicinal plants assume an indispensable job in keeping up the chemical balance of the brain by affecting the capacity of receptors for the major inhibitory neurotransmitters. In a conventional act of medication, a few plants have been accounted for to treat NDs. This volume highlights various homegrown medications and their scientific validation to maintain neuronal wellbeing, utilized in Ayurveda practices and Chinese medication. This book summarizes different phytochemicals from various medicinal herbs that are used as promising therapeutic agents for NDs due to their anti-inflammatory and anti-oxidative as well as anticholinesterase activities. Even though the affinity of receptors or carriers for polyphenols or different phytochemicals of the homegrown arrangements in cerebrum tissues remains to be found out, numerous candidates show up as a potential and promising class of therapeutics for the treatment of ailments with a multifactorial etiology. Adopting the ethnomedicinal approach, this book addresses the intersection between recent therapeutics for NDs and personalized medicine that will allow a broader range of interventions, including evidence-based natural products.
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Reactions that form sec-sec ethers are well known, but few lead to compounds with dense functionality around the O-linkage. Replacement of the α-glucopyranosyl unit of adenophostin A, a potent D-myo-inositol 1,4,5-trisphosphate (IP3R) agonist, with a D-chiro-inositol surrogate acting substantially as a pseudosugar, leads to “D-chiro-inositol adenophostin”. At its core, this cyclitol-nucleoside trisphosphate comprises a nucleoside sugar linked via an axial D-chiro-inositol 1-hydroxyl-adenosine 3'-ribose ether linkage. A divergent synthesis of D-chiro-inositol adenophostin has been achieved. Key features of the synthetic strategy to produce a triol for phosphorylation include a new selective mono-tosylation of racemic 1,2:4,5-di-O-isopropylidene-myo-inositol using tosyl imidazole; subsequent conversion of the product into separable camphanate ester derivatives, one leading to a chiral myo-inositol triflate used as a synthetic building block and the other to L-5-O-methyl-myo-inositol [L-(+)-bornesitol] to assign the absolute configuration; the nucleophilic coupling of an alkoxide of a ribose pent-4-ene orthoester unit with a structurally rigid chiral myo-inositol triflate derivative, representing the first sec-sec ether formation between a cyclitol and ribose. Reaction of the coupled product with a silylated nucleobase completes the assembly of the core structure. Further protecting group manipulation, mixed O- and N-phosphorylation, and subsequent removal of all protecting groups in a single step achieves the final product, avoiding a separate N6 protection/deprotection strategy. D-chiro-Inositol adenophostin evoked Ca2+ release through IP3Rs at lower concentrations than adenophostin A, hitherto the most potent known agonist of IP3Rs.
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Ocimum basilicum and Ocimum gratissimum (Lamiaceae) are used to treat diabetes mellitus in Africa. In a previous work, we identified chicoric acid as a hypoglycemic substance in O. gratissimum. This study aims to compare the chemical metabolite profile and the hypoglycemic activity of unfractionated aqueous extracts from leaves of both Lamiaceae species. The metabolite composition of OB and OG decoctions (10% w/v) was analyzed using HPLC-DAD and NMR tools. Chicoric acid showed to be the major phenolic in both extracts, besides caftaric, caffeic, and rosmarinic acids; nevertheless, there is approximately three times more of this substance in OG. From 1D- and 2D-NMR analyses, 19 substances were identified in OB, while 12 in OG. The in vivo acute hypoglycemic activity of the extracts was assessed intraperitoneally in streptozotocin (STZ)-induced diabetic mice. The doses of 100 and 200 mg/kg of both extracts significantly reduced their glycemia, compared to controls (P < 0.05). OB was a little more effective than OG, despite the lower content of chicoric acid in OB. This result strongly suggests that components other than chicoric acid contribute to the hypoglycemic activity of the two extracts. Despite the abundance of caffeic and rosmarinic acids in OB, their hypoglycemic activity observed at 8.3 μmol/kg was low. This is the first chemical profile of crude extracts from Ocimum species by NMR. Our findings confirmed the potential of both species in DM treatment in spite of marked differences in their chemical composition. However, long-term studies are necessary in order to identify the most promising of the two species for the development of an herbal medicine.
Chapter
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The effect of soaking, cooking and autoclaving on the levels of certain antinutritional factors present in the tribal pulse, Mucuna pruriens, were studied. The amount of reduction of total free phenolics was found to be greater in sodium bicarbonate solution (56%) compared to distilled water (47%); subjected to cooking and autoclaving these were further reduced to 49%. Autoclaving (45 min) significantly reduced the tannin content (71%). Insignificant reduction in content of L-DOPA was observed in all the processes. Distilled water soaking was found to be ineffective in eliminating lectin activity; whereas very significant reduction was noticed against all the human blood groups ABO without any specificity in samples subjected to cooking and autoclaving. Soaking in distilled water was more effective (27% reduction) than sodium bicarbonate solution (17% reduction) in lowering the contents of phytic acid. Cooking for 90 min and autoclaving for 45 min resulted in eliminating phytic acid to the extent of 18% and 44%, respectively. Loss of HCN was greater under autoclaving (75%) than the other processes studied. Of the three oligosaccharides analysed, soaking effected maximum reduction in the level of stachyose followed by verbascose and raffinose. Autoclaving effected greater reduction (59-81%) compared to ordinary cooking (40-60% reduction). Of all the different treatments studied, autoclaving seemed to be the best method in eliminating the investigated antinutrients more efficiently except L-DOPA.
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O-alpha-D-Galactopyranosyl-(1-->2)-D-chiro-inositol, herein named fagopyritol B1, was identified as a major soluble carbohydrate (40% of total) in buckwheat (Fagopyrum esculentum Moench, Polygonaceae) embryos. Analysis of hydrolysis products of purified compounds and of the crude extract led to the conclusion that buckwheat embryos have five alpha-galactosyl D-chiro-inositols: fagopyritol A1 and fagopyritol B1 (mono-galactosyl D-chiro-inositol isomers), fagopyritol A2 and fagopyritol B2 (di-galactosyl D-chiro-inositol isomers), and fagopyritol B3 (tri-galactosyl D-chiro-inositol). Other soluble carbohydrates analyzed by high-resolution gas chromatography included sucrose (42% of total), D-chiro-inositol, myo-inositol, galactinol, raffinose and stachyose (1% of total), but no reducing sugars. All fagopyritols were readily hydrolyzed by alpha-galactosidase (EC 3.2.1.22) from green coffee bean, demonstrating alpha-galactosyl linkage. Retention time of fagopyritol B1 was identical to the retention time of O-alpha-D-galactopyranosyl-(1-->2)-D-chiro-inositol from soybean (Glycine max (L.) Merrill, Leguminosae), suggesting that the alpha-galactosyl linkage is to the 2-position of D-chiro-inositol. Accumulation of fagopyritol B1 was associated with acquisition of desiccation tolerance during seed development and maturation in planta, and loss of fagopyritol B1 correlated with loss of desiccation tolerance during germination. Embryos of seeds grown at 18 degrees C, a condition that favors enhanced seed vigor and storability, had a sucrose-to-fagopyritol B1 ratio of 0.8 compared to a ratio of 2.46 for seeds grown at 25 degrees C. We propose that fagopyritol B1 facilitates desiccation tolerance and storability of buckwheat seeds.
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While much work remains, the evidence has become strong that IPG generation following insulin action is a significant signaling mechanism. A considerable body of data has established IPG release by insulin and other growth factors from cell membranes, cells and in human blood and muscle biopsies in vivo. Two separate IPG species containing D-chiro-inositol and myo-inositol have been separated by ion exchange. These IPGs have separate actions in vitro and are both active as insulin surrogates in vivo. A deficiency of the chiro-inositol system has been demonstrated in urine and tissues in humans and directly related to insulin resistance. Accordingly, D-chiro-inositol was administered to STZ diabetic rats and rhesus monkeys and shown to decrease hyperglycemia and enhance glucose disposal. Two trials in humans with impaired glucose tolerance and women with PCOS have now also proven successful. Thus, the pathophysiology in the chiro-inositol system related to insulin resistance and its reversal by chiro-inositol administration, in addition to the basic work, argues strongly for the physiological significance of this novel signaling system in the control of glucose metabolism.
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The effect of various domestic processing methods on antinutrients and starch fractions and in vitro protein and starch digestibilities of white and black varieties of Mucuna pruriens var. utilis was studied. Cooking or autoclaving of both raw seeds and presoaked seeds in different solutions (water, tamarind extract, sodium bicarbonate, and citric acid) significantly (p < 0.05) reduced the content of total phenolics, phytic acid, trypsin inhibitor and chymotrypsin inhibitor activities, and L-dopa compared to soaking or dry heating techniques. The germination processes (24 and 48 h) were also effective in the reduction of various antinutrients, although this reduction appeared to be more pronounced in a prolonged period of germination (72 h). Water soaking followed by dehusking was found to be ineffective in the reduction of trypsin and chymotrypsin inhibitor activities in both varieties. All of the treatments were effective in significantly (p < 0.05) reducing the resistant starch content in the presently investigated samples. Cooking as well as autoclaving brought about a more significant (p < 0.05) improvement in the digestibility of protein and starch compared to germination and dry heat treatment. Moreover, among the different processing techniques, soaking in sodium bicarbonate solution followed by cooking (29.6-34.8%) or autoclaving (33.0-37.2%) seemed to be the best method for improving starch digestibility.
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The purpose of the study was to investigate the effects of daily oral feeding Momordica charantia (MC) (200 mg/kg), Eugenia jambolana (EJ) (200 mg/kg), Mucuna pruriens (MP) (200 mg/kg) and Tinospora cordifolia (TC) extracts for 40 days on blood glucose concentrations and kidney functions in streptozotocin (STZ)-diabetic rats. Plasma glucose levels, body weight, urine volume and urinary albumin levels were monitored on every 10th day over a 40-day period while plasma creatinine levels were assessed at the beginning and end of experiment. Renal hypertrophy was assessed as the ratio between the kidney weight and total body weight. Plasma glucose concentrations in STZ-diabetic mice were reduced by the administration of extracts of MC, EJ, TC and MP by 24.4, 20.84, 7.45 and 9.07%, respectively (P<0.005 for MC, EJ, MP and P<0.05 for TC). Urine volume was significantly higher (P<0.005) in diabetic controls and MC, EJ, MP and TC treatment prevented polyuria (P<0.001, 0.0001, 0.01 and 0.001, respectively). After 10 days of STZ administration urinary albumin levels (UAE) were over 6 fold higher in diabetic controls as compared to normal controls. Treatment with MC, EJ, MP and TC significantly prevented the rise in UAE levels from day 0 to 40 in comparison to diabetic controls (P<0.0001, 0.0001, 0.05, 0.05, respectively). Renal hypertrophy was significantly higher in diabetic controls as compared to non-diabetic controls. MC and EJ partially but significantly (P<0.05) prevented renal hypertrophy as compared to diabetic controls. TC and MP failed to modify renal hypertrophy. Results indicate that these plant drugs should be studied further.
Article
Since ancient times, plants have been an exemplary source of medicine. Ayurveda and other Indian literature mention the use of plants in treatment of various human ailments. India has about 45000 plant species and among them, several thousands have been claimed to possess medicinal properties. Research conducted in last few decades on plants mentioned in ancient literature or used traditionally for diabetes have shown anti-diabetic property. The present paper reviews 45 such plants and their products (active, natural principles and crude extracts) that have been mentioned/used in the Indian traditional system of medicine and have shown experimental or clinical anti-diabetic activity. Indian plants which are most effective and the most commonly studied in relation to diabetes and their complications are: Allium cepa, Allium sativum, Aloe vera, Cajanus cajan, Coccinia indica, Caesalpinia bonducella, Ficus bengalenesis, Gymnema sylvestre, Momordica charantia, Ocimum sanctum, Pterocarpus marsupium, Swertia chirayita, Syzigium cumini, Tinospora cordifolia and Trigonella foenum graecum. Among these we have evaluated M. charantia, Eugenia jambolana, Mucuna pruriens, T. cordifolia, T. foenum graecum, O. sanctum, P. marsupium, Murraya koeingii and Brassica juncea. All plants have shown varying degree of hypoglycemic and anti-hyperglycemic activity.
Article
The Indian traditional system of medicine prescribed traditional plant therapies. Two such plants, i.e. Momordica charantia (MC) and Mucuna pruriens (MP), earlier shown to reduce hyperglycaemia, were assessed for their anti hyperglycaemic effect on varying degrees of hyperglycaemia and diabetic complications. Alcohol and aqueous extracts of MC (50, 100 and 200 mg/kg/day) and only an alcohol extract of MP (100, 200 and 400 mg/kg/day) were evaluated in a pilot study (plasma glucose >180 mg/dL, 21 days), a chronic study in alloxanized rats (plasma glucose >280mg/dL, 120 days) and streptozotocin (STZ) mice (plasma glucose >400 mg/dL, 60 days). In the pilot study, the maximum antihyperglycaemic effect occurred with an aqueous extract of MC at week 3 and an alcohol extract of MP at week 6 at a dose of 200 mg/kg/day. In chronic alloxanized rats, the selected dose of MC led to a significant fall of 64.33%, 66.96%, 69.7% and 70.53% in plasma glucose levels at 1, 2, 3 and 4 months, respectively. MP showed a decrease of 40.71%, 45.63%, 50.33% and 51.01% at the same time period. In chronic STZ diabetic mice, MC led to a mean reduction of 15.37%, 18.68% and 22.86% in plasma glucose levels on days 40, 50 and 60 of sampling while MP had no significant effect. The alteration in hepatic and skeletal muscle glycogen content and hepatic glucokinase, hexokinase, glucose-6-phosphate and phosphofructokinase levels in diabetic mice were partially restored by MC but not by MP. The mechanism of action of MC and MP is discussed.
Article
The efficacy of Momordica charantia (MC), Eugenia jambolana (EJ), Tinospora cordifolia (TC) and Mucuna pruriens (MP) was assessed in the prevention of murine alloxan dibetic cataract. Alloxan (120 mg/kg) was used as the diabetogenic agent. While controls and diabetic controls did not receive any plant extract, treated rats received lyophilized aqueous extract of MC and EJ (200 mg/kg p.o.), alcohol extract of TC (400 mg/kg) and MP (200 mg/kg p.o.) every day until 4 months. Serum glucose concentration was assessed and cataracts examined with both the naked eye and through a slit lamp. Of the eight animals in the diabetic control group, four developed cortical cataract (stage IV) by day 90 while the remaining four developed it by day 100. The incidence rate of cataract in MC, EJ, TC and MP treated groups at 120 days was only 0, 0, 1 and 2. Oral feeding of MC, EJ, TC and MP extracts for 1 month produced a fall of 64.33%, 55.62%, 38.01% and 40.17%, respectively, in the serum glucose levels in comparison with the 48 h level. After 2 months of treatment, the respective values were 66.96%, 59.85%, 40.41% and 45.63%. MC and EJ prevented the development of cataract while the protective effect was less with TC and MP along with a significant reduction of plasma glucose levels (p < 0.001).
  • Ortmeyer