scholarly journals Antidiabetic Indian Plants: A Good Source of Potent Amylase Inhibitors

2011 ◽  
Vol 2011 ◽  
pp. 1-6 ◽  
Author(s):  
Menakshi Bhat ◽  
Smita S. Zinjarde ◽  
Shobha Y. Bhargava ◽  
Ameeta Ravi Kumar ◽  
Bimba N. Joshi

Diabetes is known as a multifactorial disease. The treatment of diabetes (Type II) is complicated due to the inherent patho-physiological factors related to this disease. One of the complications of diabetes is post-prandial hyperglycemia (PPHG). Glucosidase inhibitors, particularlyα-amylase inhibitors are a class of compounds that helps in managing PPHG. Six ethno-botanically known plants having antidiabetic property namely,Azadirachta indicaAdr. Juss.;Murraya koenigii(L.) Sprengel;Ocimum tenuflorum(L.) (syn:Sanctum);Syzygium cumini(L.) Skeels (syn:Eugenia jambolana);Linum usitatissimum(L.) andBougainvillea spectabiliswere tested for their ability to inhibit glucosidase activity. The chloroform, methanol and aqueous extracts were prepared sequentially from either leaves or seeds of these plants. It was observed that the chloroform extract ofO. tenuflorum; B. spectabilis; M. koenigiiandS. cuminihave significantα-amylase inhibitory property. Plants extracts were further tested against murine pancreatic, liver and small intestinal crude enzyme preparations for glucosidase inhibitory activity. The three extracts ofO. tenuflorumand chloroform extract ofM. koenigishowed good inhibition of murine pancreatic and intestinal glucosidases as compared with acarbose, a known glucosidase inhibitor.

2011 ◽  
Vol 2011 ◽  
pp. 1-9 ◽  
Author(s):  
Menakshi Bhat ◽  
Sandeepkumar K. Kothiwale ◽  
Amruta R. Tirmale ◽  
Shobha Y. Bhargava ◽  
Bimba N. Joshi

Diabetes mellitus is a metabolic syndrome characterized by an increase in the blood glucose level. Treatment of diabetes is complicated due to multifactorial nature of the disease.Azadirachta indica Adr. JussandBougainvillea spectabilisare reported to have medicinal values including antidiabetic properties. In the present study usingin vivodiabetic murine model,A. indicaandB. spectabilischloroform, methanolic and aqueous extracts were investigated for the biochemical parameters important for controlling diabetes. It was found thatA. indicachloroform extract andB. spectabilisaqueous, methanolic extracts showed a good oral glucose tolerance and significantly reduced the intestinal glucosidase activity. Interestingly,A. indicachloroform andB. spectabilisaqueous extracts showed significant increase in glucose-6-phosphate dehydrogenase activity and hepatic, skeletal muscle glycogen content after 21 days of treatment. In immunohistochemical analysis, we observed a regeneration of insulin-producing cells and corresponding increase in the plasma insulin and c-peptide levels with the treatment ofA. indicachloroform andB. spectabilisaqueous, methanolic extracts. Analyzing the results, it is clear thatA. indicachloroform andB. spectabilisaqueous extracts are good candidates for developing new neutraceuticals treatment for diabetes.


2021 ◽  
Vol 7 (1) ◽  
Author(s):  
P. Resmi ◽  
G. Jitha ◽  
Vishnu Murali ◽  
Anu Gopinath

Abstract Background Medicinal importance of mangrove plant Rhizophora mucronata, a red mangrove species found in the Asian countries, has long been recognised in traditional systems of medicine. The identification of its phytoconstituents can be a starting point for the drug development. The aim of the work was to extend the current knowledge of phytoconstituents from R. mucronata and to explore its pharmacological importance in the treatment of diabetes mellitus. In the present study, we analysed the chloroform extract from the bark of the mangrove plant R. mucronata for nitrogen-containing constituents using UHPLC QTOF MS profiling, and α-amylase inhibition assay was carried out. Results Four nitrogen-containing compounds were identified from the chloroform extract of the bark of R. mucronata using UHPLC QTOF MS profiling. The compounds identified were N,N′-dicyclohexyl urea, a cryptolepine derivative (C17H15N3O), an aliphatic cyclic compound with hydroxyl and amino groups (C22H43NO), and C16H19NO2 (m/z 258.1495). The anti-amylase activity, an in vitro antidiabetic bioassay, of chloroform extract showed an IC50 value of 220.09 μg/ml. Conclusions This is the first report on the identification of nitrogen-containing compounds from the chloroform extract of the bark of the R. Mucronata. One of the compounds identified was a novel cryptolepine derivative (C16H13N3O), and it falls under the rare category indoloquinoline alkaloid. The chloroform extract also showed significant activity towards α-amylase inhibition assay. Thus, the study has gone some way towards our understanding of the efficacy of bark of the R. mucronata for the treatment of diabetes mellitus and is open for further research.


Planta Medica ◽  
2021 ◽  
Author(s):  
Neil Miller ◽  
Elizabeth Joubert

AbstractPostprandial hyperglycemia is treated with the oral antidiabetic drug acarbose, an intestinal α-glucosidase inhibitor. Side effects of acarbose motivated a growing number of screening studies to identify novel α-glucosidase inhibitors derived from plant extracts and other natural sources. As “gold standard”, acarbose is frequently included as the reference standard to assess the potency of these candidate α-glucosidase inhibitors, with many outperforming acarbose by several orders of magnitude. The results are subsequently used to identify suitable compounds/products with strong potential for in vivo efficacy. However, most α-glucosidase inhibitor screening studies use enzyme preparations obtained from nonmammalian sources (typically Saccharomyces cerevisiae), despite strong evidence that inhibition data obtained using nonmammalian α-glucosidase may hold limited value in terms of identifying α-glucosidase inhibitors with actual in vivo hypoglycemic potential. The aim was to critically discuss the screening of novel α-glucosidase inhibitors from plant sources, emphasizing inconsistencies and pitfalls, specifically where acarbose was included as the reference standard. An assessment of the available literature emphasized the cruciality of stating the biological source of α-glucosidase in such screening studies to allow for unambiguous and rational interpretation of the data. The review also highlights the lack of a universally adopted screening assay for novel α-glucosidase inhibitors and the commercial availability of a standardized preparation of mammalian α-glucosidase.


Biology ◽  
2020 ◽  
Vol 9 (8) ◽  
pp. 197
Author(s):  
Saima Maher ◽  
M. Iqbal Choudhary ◽  
Farooq Saleem ◽  
Saima Rasheed ◽  
Imran Waheed ◽  
...  

Withania coagulans (W. coagulans) is well-known in herbal medicinal systems for its high biological potential. Different parts of the plant are used against insomnia, liver complications, asthma, and biliousness, as well as it is reported to be sedative, emetic, diuretic, antidiabetic antimicrobial, anti-inflammatory, antitumor, hepatoprotective, antihyperglycemic, cardiovascular, immuno-suppressive and central nervous system depressant. Withanolides present in W. coagulans have attracted an immense interest in the scientific field due to their diverse therapeutic applications. The current study deals with chemical and biological evaluation of chloroform, and n-butanol fractions of W. coagulans. The activity-guided fractionation of both extracts via multiple chromatographic steps and structure elucidation of pure isolates using spectroscopies (NMR, mass spectrometry, FTIR and UV-Vis) led to the identification of a new withanolide glycoside, withacogulanoside-B (1) from n-butanol extract and five known withanolides from chloroform extract [withanolid J (2), coagulin E (3), withaperuvin C (4), 27-hydroxywithanolide I (5), and ajugin E (6)]. Among the tested compounds, compound 5 was the most potent α-glucosidase inhibitor with IC50 = 66.7 ± 3.6 µM, followed by compound 4 (IC50: 407 ± 4.5 µM) and compound 2 (IC50: 683 ± 0.94 µM), while no antiglycation activity was observed with the six isolated compounds. Molecular docking was used to predict the binding potential and binding site interactions of these compounds as α-glucosidase inhibitors. Consequently, this study provides basis to discover specific antidiabetic compounds from W. coagulans.


2015 ◽  
Vol 2015 ◽  
pp. 1-7 ◽  
Author(s):  
Hui Liao ◽  
Linda Banbury

Objective.To study the effect of different proportions of Huangqi (Radix Astragali Mongolici) and Honghua (Flos Carthami) injection onα-glucosidase andα-amylase activity simultaneously.Methods.The injections were prepared according to the standards of the China Food and Drug Administration. The assay for potentialα-glucosidase inhibitors was based on the hydrolysis of 4-methylumbelliferyl-α-D-glucopyranoside (4-MUG). Theα-amylase EnzChek assay kit was used to determine potentialα-amylase inhibitors. Acarbose was the positive control.Results.The half maximal (50%) inhibitory concentration (IC50) of acarbose againstα-glucosidase andα-amylase was (1.8±0.4)μg/mL and (227±32)μg/mL, respectively. Honghua showed significant inhibition ofα-glucosidase activity compared with Huangqi (P<0.01). Honghua inhibitedα-amylase activity, but Huangqi did not. IC50s forα-glucosidase inhibition by mixtures at 10 : 1, 5 : 1, and 2 : 1 were significantly lower than those at the 20 : 1 mixture (P<0.01).α-Amylase inhibition by the 2 : 1 mixture was significantly higher than that by the 20 : 1, 10 : 1, and 5 : 1 mixtures at 500 μg/mL and 1000 μg/mL (P<0.01), with 5 : 1 significantly higher than 20 : 1 and 10 : 1 at 1000 μg/mL (P<0.01).Conclusion.Honghua significantly inhibitedα-glucosidase activity compared with Huangqi (P<0.01). For simultaneous inhibition ofα-glucosidase andα-amylase activities, the mixtures at 2 : 1 and 5 : 1 exhibited significant effects compared with those at 20 : 1 (P<0.01).


2017 ◽  
Vol 11 (1) ◽  
Author(s):  
J. Kozonova ◽  
L. Telegenko ◽  
N. Stavnicha

The comparative analysis of the micronutrient diet compositions of the patients with type II diabetes and healthy people were held. It was found that in a diet it is necessary to enrich the following micronutrients: B vitamins, biotin, vitamin A, E, D, C, minerals magnesium, zinc, calcium, selenium, manganese, chromium, sulfur. At the same time, it is necessary to reduce the content of sodium, iron and fluoride. You can find the recommendations for the creation of software for the development of individual diets for the prevention and treatment of diabetes type II. In addition to these selected criteria (Micronutrient) it is recommended to enter the following: the total number of proteins, fats, carbohydrates, as well as the minimum content of omega-3 fatty acids, and the maximum content of simple carbohydrates and starch. The analysis of the chia seeds chemical composition on the content of diabet essential micronutrients were held. It is shown that the use of chia seeds in products for the prevention and treatment of diabetes is extremely important.


2019 ◽  
Vol 12 (3) ◽  
pp. 102 ◽  
Author(s):  
Niken Pujirahayu ◽  
Debu Kumar Bhattacharjya ◽  
Toshisada Suzuki ◽  
Takeshi Katayama

This study reports on the antioxidant activity and α-glucosidase inhibitory activity of five cycloartane-type triterpenes isolated from Indonesian stingless bee (Tetragonula sapiens Cockerell) propolis and their structure–activity relationships. The structure of the triterpenes was determined to include mangiferolic acid (1), Cycloartenol (2), ambonic acid (3), mangiferonic acid (4), and ambolic acid (5). The inhibitory test results of all isolated triterpenes against α-glucosidase showed a high potential for inhibitory activity with an IC50 range between 2.46 and 10.72 µM. Among the compounds tested, mangiferonic acid (4) was the strongest α-glucosidase inhibitor with IC50 2.46 µM compared to the standard (–)-epicatechin (1991.1 µM), and also had antioxidant activities with IC50 values of 37.74 ± 6.55 µM. The study on the structure–activity relationships among the compounds showed that the ketone group at C-3 and the double bonds at C-24 and C-25 are needed to increase the α-glucosidase inhibitory activity. The carboxylic group at C-26 is also more important for increasing the inhibitory activity compared with the methyl group. This study provides an approach to help consider the structural requirements of cycloartane-type triterpenes from propolis as α-glucosidase inhibitors. An understanding of these requirements is deemed necessary to find a new type of α-glucosidase inhibitor from the cycloartane-type triterpenes or to improve those inhibitors that are known to help in the treatment of diabetes.


2020 ◽  
Vol 8 (4) ◽  
pp. 153
Author(s):  
Joice Karina Otênio ◽  
Geysse Kelle de Oliveira ◽  
Rosselyn Gimenes Baisch ◽  
Guilherme Donadel ◽  
Emerson Luiz Botelho Lourenço ◽  
...  

The present study was carried out through a bibliographic survey of medicinal species, Asystasia gangetica, Catharanthus roseus, Arctium minus, Cynara scolymus, Anredera baselloides, Opuntia ficus-indica, Carica papaya, Ipomoea carnea, Ocimum gratissimum, Abelmoschus esculentus, Musa paradisiaca, Psidium cattleyanum, Syzygium cumini, Bougainvillea glabra, Bougainvillea spectabilis, Phyllanthus niruri, Capsicum baccatum var. pendulum and Zingiber officinale grown in the medicinal garden of Campus 2 of Universidade Paranaense, located in Umuarama, Paraná State, Brazil. The following databases were used for the bibliographic review: Scielo, Medline/Pubmed, and Google Scholar. All the species presented have hypoglycemic activity verified with preclinical and/or clinical pharmacological studies and have great potential for use in the treatment of diabetes or in combination with allopathic drugs. However, despite the pharmacological records found, additional scientific investigations are still needed to be able to use these species more safely and effectively.


Author(s):  
Majdoleen Al Switi ◽  
Bahaaldeen Alshraideh ◽  
Abedalrhman Alshraideh ◽  
Abudalla Massad ◽  
Mohammad Alshraideh

<p>Chronic diseases is an important research field because of the growth of the number of affected people around the world. When someone has diabetes, the body either does not make enough insulin or cannot use its own insulin as well as it should. This causes sugar to build up in blood leading to complications like heart disease, stroke, and neuropathy. Poor circulation leading to loss of limbs, blindness, kidney failure, nerve damage, and death. Diagnosis plays vital role in diabetes treatment otherwise it leads to long term complications in terms of costs of the treatment of the patients and leads to many risks over the patient himself as mentioned above. In this research we propose new methodology to extract the best testing sequence evaluation mechanism for helping doctors to evaluate their patient’s cases and make the best decisions about the medicine being given. We managed to create chromosomes population each of which consists of binary decision tree, as this implementation considered being the best scenario of our problem. The system proves its efficiency by applying it on 50 patients and the results shows accuracy percentage of 95.4%.</p>


2020 ◽  
Vol 32 (7) ◽  
pp. 1756-1762
Author(s):  
K.M. Sachin ◽  
Sameer A. Karpe ◽  
Man Singh ◽  
Ajaya Bhattarai

The interaction of an α-glucosidase inhibitors class of drug acarbose with globular proteins like bovine serum albumin (BSA), human serum albumin (HSA) and haemoglobin studied by fluorescence, circular dichroism (CD) spectroscopic methods. Acarbose is used for the treatment of diabetes mellitus type 2 and in some countries, prediabetes. The quenching constant (kq) values were calculated by using fluorescence data, higher with haemoglobin (at λext = 405 nm). It indicates the quenching process for the acarbose-haemoglobin interaction. Thus, the binding constants (kb), infers that the electrostatic, hydrogen bonding, and intermolecular interactions play an important role in the proteins, and drug interaction. The number of binding sites (n), between BSA, HSA and haemoglobin with acarbose was estimated by fluorescence data, the highest binding sites (15.55) of acarbose-haemoglobin at (λext = 405nm) indicates that the strong interaction or high quenching interaction. The interactions between BSA, HSA and haemoglobin with acarbose were confirmed by spectroscopic analysis and thermodynamic determination. The circular dichroism (CD) spectra implied the significant change in the conformation of BSA, HSA and haemoglobin upon binding with acarbose.


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