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Background The history and the discovery of the benefits of traditional medicines are fascinating over wide variety of disease. Various molecules have been erupted from traditional medicine for various diseases through reverse pharmacology. In current scenario plant-based medicines backed by modern scientific evidences are one of the most promising therapies in diabetes management. Scope and approach Garlic (allicin), European barberry (berberine), Bitter gourd (charantin, polypeptide-p), Sweet potato (adiponectin, tiliroside), Orka (quercetin, hyperin) are some plants that have been used in folk medicine as well as traditional healing systems and are being assessed for their hypoglycemic effects in modern medicine. Key findings and conclusions “Old wine in new bottle” proverb applies traditional medicine in new modern medicine. Various novel delivery aspects have modified the pharmacokinetics of phytochemicals and indirectly enhance the bioavailability, which in turn gives fruitful effect of their therapeutic action.

Allosteric activators of human glucokinase (GK) had revealed significant hypoglycemic effects for therapy of type-2 diabetes (T2D) in animal as well as human models. Some newer N-benzimidazol-2yl substituted benzamide analogues were prepared and assessed for activation of GK accompanied by molecular docking investigations for predicting the bonding interactions of these derivatives with the residues in allosteric site of GK protein. Amongst the derivatives synthesized, compounds 2 and 7 strongly increased catalytic action of GK (GK activation fold >2.0 in comparison to control) in vitro. The results of in-vitro testing were supported by the molecular docking investigations of these analogues with GK protein’s allosteric site residues (showed appreciable H-bond interactions with Arg63 residue of GK). Derivatives investigated in present study afforded few lead compounds for the discovery of harmless and strong allosteric GK activating compounds for treating T2D.

Hypoglycemic effects was observed with Spirulina (Spirulinaplatensis) when given as leaf extract in normal and alloxan diabetic rat. In this study 150 rats were included and divided into three groups of ten rats in each group. First group was normal control (A), Second group was diabetic control (B), third group was diabetic with Spirulina treated (C). The rats were treated with aqueous extract of Spirulina at a dose rate of 20 mg/kg body weight respectively for 3 weeks. During experimental period, day 0, day 7, day 14 and day 21 blood samples were collected from all groups and determined their blood sugar level using diabetic kit. The blood glucose levels were reduced from 165.5±10.65 mg/dL to 158.17±5.49 mg/dL in group C after 3 weeks treatment. On the other hand the average body weight were increased from 255.67±7.35 g to 286.17±8.56 g in group C after 3 weeks treatment. From the findings it is concluded that the Spirulina can be used as anti-diabetogenic agent in food. Res. Agric., Livest. Fish.7(3): 475-479, December 2020

Background: Diabetes mellitus (DM) is among the diseases with high morbidity and mortality The pathogenesis of DM involves pancreatic s-cell damage or insulin sensitivity disorder that result in hyperglycemia. Tapak liman (Elephantopus scaber L) is known to have high flavonoid content. Flavonoids are antioxidants that play a role in reducing pancreatic s-cell damage or damage to other tissues, which potentially reduce blood glucose levels. Objective: To determine the hypoglycemic effects of tapak liman using the DM rat models. Methods: Twenty-eight Wistar albino rats (Rattus novergicus) were divided into four groups: the normal control group (KKn), not induced by streptozotocin-nicotinamide (STZ-NA) intraperitoneal; negative control group (KK-), induced by STZ-NA; treatment group 1 (KP1), induced by STZ-NA and 150 mg/kg body weight of tapak liman plant extract; and the treatment group 2 (KP2), induced by STZ-NA and 300 mg/kg body weight of tapak liman. Blood glucose levels were measured on the 7th day after STZ-NA induction and the 28th day after the administration of tapak liman plant extract. The results were analyzed for statistical significance. Results: There was a significant decrease in blood glucose levels in KP1 and KP2 (p= 0.05). The decrease in blood glucose in KP1 had not reached normal levels compared to KP2. Conclusion: Administration of tapak liman plant extract at a dose of 300 mg/kg body weight in DM rat models reduced blood glucose levels to normal.

Background: Ammodaucus leucotrichus (Apiaceae) is a medicinal plant widely used by the Moroccan population to treat various diseases including diabetes. Aims: The aim of this study was to evaluate the antidiabetic effect of the aqueous extract prepared from the fruits of this medicinal plant. Normal and streptozotocin-induced diabetic rats were treated orally by the extract of Ammodaucus leucotrichus (A. leucotrichus) at a dose of 10 mg/kg. Methods: The blood glucose levels were determined during 6 hours and 15 days during this treatment. In addition the oral glucose tolerance test as well as the analysis of histopathological changes of liver was performed. The antioxidant activity of aqueous A. Leucotrichus extract was also valuated by the method of trapping of free radical 2,2-diphenyl-1 picrylhydrazyl (DPPH). Results: A. Leucotrichus fruit aqueous extract (ALFAE) reduced the blood glucose levels in both normal and diabetic rats. In addition, a remarkable influence on glucose tolerance was also noticed after ALFAE treatment. Moreover, ALFAE was able to exhibit a beneficial effect on histologlogical structure of liver. Finally a potential antioxidant effect has been shown in vitro. Conclusion: In conclusion, this study demonstrates the antihyperglycemic and hypoglycemic effects of A. Leucotrichus in rats supporting then its traditional use for the management of diabetes.

Background Xyloglucan (XyG) is a ubiquitous polysaccharide that possesses hypoglycemic effects, antihyperlipidemia effects, gut barrier protective properties, and positive effects on coronary heart disease. As a nonstarch polysaccharide, XyG cannot be processed directly by enzymes encoded on the human genome. After being ingested, XyG transits the large intestine where it becomes food for the intestinal microbial community. The species within the intestinal microbiota use various strategies to recognize and degrade XyG. However, most current studies focus on the industrial application of XyG. We must examine the beneficial effects of XyG on human health and the roles that the gut microbiota play in XyG degradation. Scope and approach The current review summarizes the relationship between XyG and intestinal microbiota, including the degradation process of XyG by gut Bacteroidetes and the influence of XyG on the intestinal microbiota. In addition, the possible effects of XyG or its microbial degradation products on human health are presented. Key findings and conclusions XyG breakdown in the large intestine is mediated by several proteins encoded on XyG utilization loci. Surface glycan-binding proteins and glycan-degrading enzymes encoded on XyG utilization loci are the main components that utilize XyGs in the large intestine. Secondary metabolites and fermentation end products that are generated in XyG degradation by gut microbiota can improve human health. The beneficial effects of XyG on human health may be realized through its microbial degradation.

Bitter gourd (Momordica charantia L.) is a fruit that traditionally believe to have benefits on health. It is a widely used traditional remedy for the treatment of diabetes. Bitter gourd is suggested for hyperglycemia treatment due to its ability to reduce glucose levels in the body. Some of the bioactive compounds present in it possess anti diabetic effects. It contains phytochemicals with anti-diabetic properties such as charantin, p-insulin and vicine. Hypoglycemic effects of bitter gourd have been shown in clinical studies. This review will focus on the hyperglycemic properties of bitter gourd.

Pomegranate juice (PJ) has gained popularity attributed to its phenolic compounds and their medicinal properties. Its potential hypoglycemic effect has been related to enzymatic inhibition, insulin release, and the protection of pancreatic tissue. These effects depend on several aspects, such as the content and composition of phenols in pomegranate and characteristics of the organism that consumes the juice. The objective of this study was to systematically review scientific evidence investigating the hypoglycemic effect of PJ; the factors that affect bioactive compounds; and the mechanisms of action attributed to this effect. Human and rodent in vivo and in vitro studies were retrieved from PubMed, Scopus, and ScienceDirect databases. After reviewing the articles, it was identified that the methodologies and results among the scientific evidence were quite heterogeneous. Despite these limitations, many of the in vivo and in vitro studies found important hypoglycemic effects from PJ, as well as an increase in the function of β-cell, insulin secretion, a significantly lower activity of α-amylase enzyme, an inhibition of the enzyme α-glucosidase and dipeptidyl peptidase-4 (DPP-4), and the protection against DNA damage. Determining the potential health benefits of polyphenols contained in the pomegranate is limited for multiple factors that could affect the efficacy of PJ. Overall, the results of this review suggest the need for further experimentation, using controlled variable factors and testing the effect of PJ under similar experimental conditions.

The inhibition of porcine pancreatic α-amylase (PPA) by 9 galloyl-based polyphenols was evaluated via initial digestion velocity, IC50, inhibition kinetics, fluorescence quenching and molecular docking studies. The results show that the polyphenols with free galloyl moieties (GMs) exhibited a much higher inhibition effect than that with bound GMs. The inhibition was competitive mode and increased with an increase in the number of free GMs. Interestingly, all the constants that indicate the binding affinity of polyphenols to PPA, including the reciprocal of the competitive inhibition constant (1/Kic), fluorescence quenching constant (KFQ) and binding energy (Eb), increased with an increase in the number of free GMs. Besides, the respective order of 1/Kic, KFQ and Eb for the galloyl-based polyphenols was contrary to that of IC50, indicating that the polyphenol-PPA binding interactions resulted in enzyme inhibition. In addition, the binding interactions were suggested to result from the hydrogen bonding and π-π conjugation forces between the free GMs and amino acid residues at the active sites of PPA, whereas the chemical linkage of the GMs with additional polyphenol groups limited these interactions. Furthermore, the hypoglycemic effects of two polyphenols with 5 free GMs indicate that GMs may be considered a functional fragment involved in the alleviation of the symptoms of type II diabetes through α-amylase inhibition.

As emerging woody oil crops, the tree peony seeds recently have been attracting great attention for their metabolites and bioactivities. In this research, the phytochemical profiles of the seed coats of tree peonies from different production regions were investigated systematically. Twelve phytochemicals were separated and prepared, mainly belonging to stilbenes. A great variation in stilbene content was detected in the three Paeonia plants, and Paeonia ostii seed coats (POSC) had significantly higher contents of the stilbene compounds than other species. There were nineteen significant correlations between ecogeographical factors and the predominant compounds. A clear discrimination among the species was observed in their HPLC fingerprint and chemometric analysis. Furthermore, POSC extracts could significantly reduce the starch mediated PBG (postprandial blood glucose) levels in normal/diabetic mice. Meanwhile, in vitro enzyme tests revealed that the predominant compounds, suffruticosol B and ampelopsin D, could effectively and competitively inhibit α-glucosidase, indicating that POSC could be a natural source of hypoglycemics in the food and drug fields.

This present study was to evaluate the protein tyrosine phosphatase 1B (PTP1B) inhibitory activity of nine diterpenes isolated from seeds of Phalaris canariensis, as well as their effect on strepto...

The present study was undertaken to examine the antidiabetic potential of naturally occurring peptides and hydrolysate fractions from easy-to-cook (ETC) and hard-to-cook (HTC) beans. All fractions were tested regarding their in vitro inhibitory activities against α-amylase and α-glucosidase as well as in vivo anti-hyperglycemic and hypoglycemic effects. Results evidenced that the peptide fractions with the lowest molecular weight (3 kDa) have the highest inhibitory activities, and a 16.9%-89.1% inhibition of α-amylase and 34.4%-89.2% inhibition of α-glucosidase were observed. Regarding the antihyperglycemic activity, the fraction ETCNO3-10 showed a better performance than the positive control (acarbose). In addition, results from hypoglycemic activity evidenced that the tested peptide fractions were able to decrease the glucose levels at the same extension of glibenclamide, maintaining a constant basal glucose level without a postprandial hyperglycemia peak. Finally, it is possible to suggest that the naturally occurring peptides and hydrolysate fractions obtained from ETC and HTC common beans could be used in functional food production or pharmaceutical formulations to prevent diabetes.

Recently, there has an increased focus on the isolation, chemical properties and bioactivities of polysaccharides from buckwheat (Fagopyrum Mill), which is a member of the Polygonaceae family. Phytochemical and pharmacological studies have shown that polysaccharides are important biologically-active components of buckwheat, with numerous biological activities, including antioxidant, antitumor, immunomodulatory, antihypertensive and hypoglycemic effects. The purpose of this mini-review is to appraise available literature describing the extraction, separation, purification, structural characterization and biological activities of polysaccharides isolated from buckwheat. This mini-review also provides a foundation for the further investigation, production and application of buckwheat polysaccharides as functional foods and therapeutic agents.

Introduction: The aim of the current analysis was to judge the hypoglycemic action of the phyto-extracts of Lagenaria siceraria, Cynodon dactylon and Stevia rebaudiana using suitable in vitro approaches. Methods: The hypoglycemic activity of the phyto-material extracts was evaluated by employing various in-vitro methods namely glucose diffusion, amylolysis kinetics and glucose adsorption capacity. Results: The extracts of L. siceraria, C. dactylon and S. rebaudiana exhibited glucose dialysis retardation indices (GDRI) of 48.14%, 37.03% and 29.62%, respectively at 60 minutes which were reduced to 15.78%, 10.52% and 18.42%, respectively at 120 minutes. All the plant extracts used in the study adsorbed glucose and their adsorptions markedly enhanced with increase in sugar concentration. Conclusion: From the outcome of the assay it can be concluded that the extracts of L. siceraria, C. dactylon and S. rebaudiana have hypoglycemic activity as observed in various in-vitro assays. However, the beneficial actions require to be verified by adopting various in vivo techniques along with clinical trials for their efficient use as potential remedial moiety.

Dietary intervention in type 2 diabetes mellitus (T2DM) is a hotspot in international research because of potential threats to human health. Phellinus baumii, a wild fungus traditionally used as a food and medicine source, is now cultivated in certain East Asian countries, and is rich in polyphenols, which are effective anti-inflammatory ingredients useful in treatment of T2DM, with fewer side effects than drugs. To examine the hypoglycaemic effects of Phellinus baumii phenolics (PPE), the metabolite profiles of T2DM mice induced by streptozotocin after PPE intervention were systematically analyzed. Here, 10 normal mice were given normal saline as control group, and 50 model mice were randomly assigned to five groups and daily intragastric administrated with saline, metformin (100 mg/kg), and PPE (50, 100, 150 mg/kg of body weight), for 60 days. The pro-inflammatory factor contents of lipopolysaccharide stimulation of RAW 264.7 cells were decreased in a dose-dependent manner after PPE treatment, we propose that PPE could exert anti-inflammatory properties. PPE could also effectively reduce blood glucose levels, increased insulin sensitivity, and improved other glucolipid metabolism. Q-PCR results suggested that the hypoglycemic effects of PPE might be through activating IRS1/PI3K/AKT pathway in diabetic mice. These results suggest that PPE has strong potential as dietary components in the prevention or management of T2DM.

Polycyclic aromatic hydrocarbons (PAHs) have been reported to cause various health damages. However, some PAH derivatives are still used as agents, and some of them have hypoglycemic effects. Till now, few studies explored the relationship between urinary PAH metabolites and fasting plasma glucose (FPG). In this study, A total of 2682 non-smokers in the second follow-up of the Wuhan-Zhuhai cohort were included to explore the relationship between urinary PAH metabolites and FPG. FPG related epigenome-wide association study (EWAS) was conducted among 212 never smokers, and the mediation analysis was performed to find potential mediator cytosine-phosphoguanine (CpG) sites in the above relationship. The concentration of total urinary PAH metabolites was 3.60 (2.37, 5.85) μg/mmol Cr. The urinary PAH metabolites were negatively associated with FPG. Each 1-U increase in ln-transformed levels of 1-hydroxynaphthalene, 4-hydroxyphenanthrene, 9-hydroxyphenanthrene, or 2- hydroxyphenanthrene was associated with 0.008-, 0.007-, 0.010-, or 0.010- unit decreased in ln-transformed levels of FPG, respectively (all p 0.05). We found 28 new CpG sites related to FPG (FDR0.05) through EWAS. Mediation analysis found that cg11350141 on AMER3 mediated 41.91% of the negative association of total urinary PAH metabolites with FPG. These results provide a new clue for the development of hypoglycemic agents.

The rhizome of Polygonatum kingianum has been used as a traditional medicine in China. In this study, a novel polysaccharides (PKPs-1) was isolated from P. kingianum and characterized by its molecular weight, primary structure. The hypoglycemic activity of PKPs-1was investigated by in vitro assay with the HepG2 cell line and in vivo test using STZ-induced diabetic mice. Results showed that the average molecular weight of PKPs-1 was 14.05 kDa and is composed mainly of glucose and mannose. Methylation analysis indicated that this polysaccharides fraction consisted mainly of β1,2-link glucose. Besides, PKPs-1 exhibited significant anti-hyperglycemic activity on STZ-induced mice, improved insulin tolerance, and affected the metabolism of serum lipids. Results of real-time quantitative PCR (RT-PCR) showed that PKPs-1 significantly increased the expression of insulin receptor substrate-1 (IRS-1), phosphoinositide 3-kinase (PI3K) and protein kinase B (AKT), indicating that PKPs-1 regulates glucose metabolism by activating the PI3K/AKT signaling pathway. This study provides new insights for investigating the hypoglycemic effects of PKPs-1 and suggests that PKPs-1 could be a promising functional food or medicine for treating T2DM.

Qingzhuan tea (QZT), a post-fermented tea, has been reported to have anti-obesity and anti-hyperglycemic effects, perhaps due to bioactive compounds that inhibit lipase and α-amylase. It is unknown what chemical constituents’ changes and what bioactive compounds occur during the manufacture of QZT. The aim of this study was to determine the secondary metabolites changes that occur during post-fermentation and how these changes affect the ability of QZT to inhibit the activities of lipase and α-amylase. During the processing steps, metabolites levels and their inhibitory effects on lipase and α-amylase were assessed. Changes in content and activities suggested that the first turn over or the second turn over was critical for the formation and conversion of bioactive compounds responsible for the anti-obesity and hypoglycemic effects. The relationship between constituents and activities was further evaluated by correlation analysis, which showed that amino acids and flavonoids might be responsible for the anti-obesity and anti-hyperglycemic effects of QZT. This study clarified that compounds were altered during pile fermentation of QZT and tentatively identified the bioactive compounds formed during QZT manufacture.

To improve the oral efficiency of exenatide, we prepared polyethylene glycol-poly(lactic-co-glycolic acid) (PEG-PLGA) NPs modified with Fc (NPs-Fc) for exenatide oral delivery. Exenatide was encapsulated into the NPs by the w/o/w emulsion-solvent evaporation method. The particle size of the NPs-Fc was approximately 30 nm larger than that of the unmodified NPs with polydispersity indices in a narrow range (PDIs; PDI in vivo imaging in live mice. Therefore, Fc-targeted nano-delivery systems show great promise for oral peptide/protein drug delivery.

Thiazolo[2, 3-f]purine derivatives and their analogs – dihydrothiazolo[2, 3-f]purine, 7-(thietan-3-yl)purine, and 8-(2-hydroxypropylthio)purine derivatives – were synthesized. The compounds synthesized here had no effects on protein glycation reactions using glucose; they gave weak inhibition of glycogen phosphorylase; they had no hemorheological activity. Substances with hypotensive activity greater than that of Dibazol were found. A number of substances had hypoglycemic effects greater than those of chlorpropamide and Adebit. Two compounds inhibited dipeptidylpeptidase-4, but were less active than reference agent vildagliptin.

Aim: A semisynthetic primary bile acid (PBA) has exerted hypoglycemic effects in Type 1 diabetic animals, which were hypothesized to be due to its anti-inflammatory and cellular glucose-regulatory effects. Thus, the research purpose aimed to examine antidiabetic effects of a PBA, in terms of cellular inflammation and survival and insulin release, in the context of supporting β-cell delivery and Type 1 diabetic treatment. Materials & methods: 10 formulations were prepared, five without PBA (control) and five with PBA (test). Formulations were used to microencapsulate pancreatic β cells and the microcapsules were examined for morphology, cell viability, insulin release and inflammation. Results & conclusion: PBA improved cell viability, insulin release and reduced inflammation in a formulation-dependent manner, which suggests potential use in cell delivery and diabetes treatment. [Formula: see text]

Polygonum multiflorum (PM) has been used as a tonic edible plant and is a popular anti-ageing dietary supplement. Trans-2,3,5,4′-tetrahydroxystilbene 2-O-β-glucopyranoside (trans-THSG) is the major active compound in PM. It was found to have potent anti-inflammatory effects in RAW 264.7 macrophage cells and in TPA-induced mouse ear edema model. Research in the significance and rational of traditional process of post-harvested PM has been neglected. With the aid of modern analytical technology, we studied the major phytochemical transformation of PM solution from trans- to cis-THSG under UV light, reminiscent of traditional process, and further evaluated the hypoglycemic effects of the processed PM extract. In a high fat diet-induced type 2 diabetic mice model, processed PM extract containing cis- and trans-THSG (ratio = 2:3) exhibited significant hypoglycemic capacity, while pure trans-THSG and unprocessed PM extract (cis-/trans-THSG ratio = 1:20) did not, suggesting the importance of anti-diabetic effect of cis-THSG and PM natural process.

Morus alba L. is an edible fruit with multiple medical function. To reveal the geographic variation pattern of polysaccharide content in the mulberry fruits and its antioxidant and hypoglycemic activities, the fruit samples were collected and analyzed from seven geographic locations throughout the distribution areas in China. The polysaccharide content in the mulberry fruits ranged from 4.13 ± 0.04% to 1.07 ± 0.07%. All the polysaccharides derived from mulberry fruit showed certain antioxidant and hypoglycemic activities with a significant variation. Significant differences were observed among polysaccharide content, antioxidant activity, and sunshine hours, but no clear geographical or polysaccharide content variation patterns were observed for hypoglycemic activity. Pearson correlation analysis indicated that the annual average sunshine hours was significantly correlated to the polysaccharide content and antioxidant activity. According to the polysaccharide contents and bioactivities, certain natural populations of M. alba L. such as Xinjiang, Hunan, and Anhui were recommended for food and medical use in future. PRACTICAL APPLICATIONS: Morus alba L. belonging to the family Moraceae, is cultivated across an extensive range of geographical, climatic, and soil conditions. Polysaccharides from mulberry fruit have been proved to have the function of enhancing immunity, antiaging, anti‐inflammatory, antioxidant, hypolipidemic, and hypoglycemic effects with no toxic record in clinic. It has been reported that the phytochemicals accumulation in plants is greatly affected by genetic, climatic, and harvesting factors during the growing period. We revealed the geographic variation pattern of polysaccharide content in the mulberry fruits and its antioxidant activity. Based on the polysaccharide contents and bioactivities, certain natural populations of M. alba L. such as Xinjiang, Hunan, and Anhui were recommended for food and medical use in future. The information obtained by this study could be useful for the selection of natural populations with adequate polysaccharide content, as well as high food and medical use for M. alba L.

Phenolic compounds are carbon-based phytochemicals that are present in many plants as secondary metabolites and, according to recent studies, they are supposed to have antimicrobial, anti-inflammatory, anticancer, and antiviral action as well as hypolipidemic and hypoglycemic effects. Nowadays, there are numerous extraction processes, which are widely used in order to extract those compounds from medicinal and aromatic plants. The most common methods that are reported in the literature are maceration, infusion, digestion, decoction, percolation, Soxhlet extraction, aqueous alcoholic extraction by fermentation, countercurrent extraction, ultrasound extraction, supercritical fluid extraction, and phytonics process. In order to select an appropriate extraction method, both chemical and economical parameters have to be taken into account in order to prove the suitability of the method. In this chapter, we aim to present an overview of those techniques that are widely used in order to extract phenolic compounds from medicinal and aromatic plants.

Honey, a concentrated natural product, is produced by honeybees (Apis mellifera) from the nectar of flowers. It contains over 200 compounds that exert various biological or pharmacological activities, ranging from antioxidant, anti-inflammatory, antimicrobial, and antihypertensive to hypoglycemic effects. Due to the presence of a plethora of bioactive compounds, as well as unique physicochemical properties, honey has been widely used as medicine throughout human history along with its extensive utilization as common food and flavoring agent. The application of neat honey for therapeutic purpose, however, poses some difficulties such as the maintenance of a required therapeutic concentration over an adequate timeframe due to the problem of liquefaction and leakage. This has driven researchers to incorporate honey into a range of formulations, for example, hydrogels, dressings, ointments, pastes, or lozenges. After a brief discussion of the chemistry and medicinal use of honey, this review focuses on commercial honey-based medicinal formulations as well as in vitro, in vivo, and clinical studies on noncommercial honey formulations for the treatment of various ailments. In addition to this, it also covers the application of honey formulations and the evidence underpinning their use.

Enhydra fluctuans is one of the medicinal plants of the Minangkabau tribe, West Sumatra, Indonesia which is widely used by the community to treat various diseases including diabetes mellitus. However, scientific studying of its hypoglycemic activity is very limited. In this study, we evaluated the hypoglycemic activity of E. fluctuans aerial ethanol using an oral glucose tolerance test (OGTT) in stable hyperglycemia rats and its phytochemical screening. Twenty-five diabetic rats were divided into five groups with five replications: negative control, positive control (glibenclamide), ethanol extract dosage of 250, 500, and 1000 mg/kg. Blood glucose is measured at 0, 30, 60, 120, and 180 minutes. Blood glucose level, the area under the curve (AUC) value, and the percentage of blood glucose reduction is calculated. It was found that a dosage of 500 mg/kg was the best hypoglycemic activity in stable hyperglycemia rats and significantly different (pE. fluctuans aerial ethanol extract contained saponins, phenolic, terpenoids, steroids, and coumarin compounds. Our findings demonstrate that E. fluctuans have potent hypoglycemic effects in diabetes.

This research established an optimized method for the extraction and enrichment of flavonoids from R. corchorifolius fruit. Under the optimized extraction conditions, 12 flavonoids (1–12) were isolated, of which six (2–4, 9–10, 12) were obtained from R. corchorifolius for the first time. Compound 4 showed significant α-glucosidase (4.96 μM) and α-amylase (8.04 μM) inhibitory effects. Molecular modeling revealed that compound 4 exhibits strong binding with the active sites of α-glucosidase and α-amylase. Lineweaver-Burk plot analysis and surface plasmon resonance revealed the possible dynamic binding mechanism of the flavonoids with α-glucosidase and α-amylase. The enriched flavonoids and compound 4 showed significant hypoglycemic effects in mice administered a high dose of glucose. In this study, a variety of flavonoids with hypoglycemic activity were found for the first time, revealing the rich chemical composition of R. corchorifolius fruit and highlighting the potential value of R. corchorifolius fruit flavonoids as dietary supplements.

Background: Our study aims at exploring the hypoglycemic effect, efficacy, and possible mode of action of ethanol extract of Alpinia nigra (EEAN) as an antidiabetic agent in an animal model. Methods: Oral glucose tolerance test (OGTT) was used to identify primary hypoglycemic effect in mice. Three tests (glucose absorption, sucrose absorption, and disaccharidase activity) were carried out by gut perfusion and six segments studies to assess carbohydrate absorption and glucose utilization. Results: In OGTT, at 400 mg/kg and 800 mg/kg dose of EEAN extract significantly improved oral glucose tolerance among normal mice at 60 min and 90 min with compared to control. Both doses of extract significantly (P < 0.01) reduced blood glucose level and showed the hypoglycemic effect by retarding 11.43% and 20.82% of blood glucose level after 2 h of administration in glucose-induced mice, respectively. In situ perfused rat intestinal model demonstrated reduced glucose absorption at a 500 mg/kg dose. Inhibition of intestinal disaccharidase was also found by the extract. This was confirmed, yet again, via the six segment study. Throughout the length of the gastrointestinal tract, sucrose digestion was found to be inhibited which is also evident in the six segment study. Conclusions: This study suggests that the EEAN has hypoglycemic effects in a dose-dependent manner by inhibiting intestinal glucose absorption, and these may be effective in the treatment of diabetes. Further study is required to explicate the effect this extract or the active compounds have on the individual glucose transporters and the precise mechanism.

The aim of this research work was to carry out a comparative study on the aqueous extracts of the leaves and fruits of Garden egg (Solanum melongena) using alloxan induced diabetic guinea pigs. Blood glucose level analysis was used as diabetic indices. Z-test was used in comparing the mean fasting blood glucose level of alloxan induced diabetic guinea pigs after administration of aqueous leaf extracts and that of the aqueous extracts of the fruits of Garden egg (Solanum melongena) against the negative control (0.9%N/S) and positive control group (Glibenclamide solution).The results showed that there was a significant difference between the group that had oral administration of aqueous leaf extracts and the negative control group (p 0.05).

Our previous in vitro reports showed that crude extract prepared with 50% ethanol (ethanol crude extract, ECE) from Mongolian oak cups possessed excellent antioxidant capacities as well as inhibitory activities against α-glucosidase, α-amylase and protein glycation caused by its enrichment in phenolics, including mainly ellagic acid, kaempferol and their derivatives. Nevertheless, few in vivo studies on antidiabetic activities of these phenolics were conducted. The present study investigated hypoglycemic effects with normal and diabetic rats being administrated orally without or with ECE at 200 and 800 mg/kg for 15 days. In normal rats, no significant differences were exhibited after ECE administration in body weight, fasting blood glucose level, levels of chelesterol, triglyceride, LDL and AST in serum, organ indexes, and levels of GSH and MDA in organs. In diabetic rats, the fasting blood glucose level, indexes of heart and liver, and levels of chelesterol and triglyceride in serum and MDA in heart tissue were significantly decreased. Moreover, HDL levels in serum and SOD activities in the four organs of diabetic rats were significantly improved after ECE administration at 800 mg/kg. Thus, in addition to inhibiting α-glucosidase, α-amylase and protein glycation reported previously, oak cups might contain novel dietary phytonutrients in preventing abnormal changes in blood glucose and lipid profile and attenuating oxidant stress in vivo. The results also implied that it is ellagic acid, kaempferol and their derivatives enriched in ECE that might play vital roles in managing type 1 as well as type 2 diabetes.

Background Berberine is one of the most important examples of a Chinese traditional medicine that has hypoglycemic effects but there have been no randomized controlled trials of the drug in a larger sample. In addition, the use of probiotic biotherapy to maintain an appropriate intestinal flora may represent an effective early intervention for hyperglycemia. Unfortunately, there has been a shortage of relevant research on this possibility at the population level. This study was designed to determine the hypoglycemic effect and safety of both bifidobacteria and berberine administration to newly diagnosed patients with pre-diabetes or diabetes mellitus. Methods/design This is a multicenter, double-blind, randomized, and parallel-controlled study that includes a run-in period of 2 weeks and a treatment period of 16 weeks, which will be conducted between June 2015 and October 2018. The 300 randomized patients will be assigned to the following four groups for 16 weeks’ treatment: Bifidobacterium, berberine, Bifidobacterium combined berberine, and placebo control groups. The primary outcome is the absolute value of fasting plasma glucose compared with baseline after 16 weeks of treatment. Discussion This is the first randomized controlled trial to determine the hypoglycemic effect and safety of both bifidobacteria and berberine administration to newly diagnosed patients with pre-diabetes or diabetes mellitus. It may provide support for the use of berberine and bifidobacteria in the treatment of diabetes. Trial registration ClinicalTrials.gov, ID: NCT03330184. Retrospectively registered on 18 October 2017. Electronic supplementary material The online version of this article (doi:10.1186/s13063-018-2438-5) contains supplementary material, which is available to authorized users.

Three new acetophenones, named cynwilforones A–C (1–3), together with cynandione A (4) were isolated from the root bark of Cynanchum wilfordii (Maxim.) Hemsl. Their structures were deduced based on spectroscopic analysis and chemical methods. Compounds 1 and 4 exhibited potential hypoglycemic effects through inhibition of hepatic gluconeogenesis by down-regulating the expression of phosphoenolpyruvate carboxykinase and glucose-6-phosphatase. This is the first report that acetophenones from the root bark of C. wilfordii possesses potential hypoglycemic activity in vitro.

Xylaria nigripes (XN) is a medicinal fungus with a high-economic value. The aim of this study was to explore the hypoglycemic effects and mechanisms of the XN aqueous extract in steroid-induced insulin-resistant (SIIR) rats. Significant hypoglycemic effects were observed 60 min after administration of XN aqueous extract. In normal Wistar, hypoglycemic effects were 21% (the plasma glucose level decreased from 128.6 ± 12.5 to 100.9 ± 10.7 mg/dL). In SIIR, hypoglycemic effects were 26% (the plasma glucose level decreased from 177.6 ± 12.5 to 133.3 ± 29.7 mg/dL) rats refer to their baseline. The signaling proteins for insulin-receptor substrate-1 and glucose transporter-4 increased 0.51-fold and 1.12-fold, respectively, as determined by Western blotting; the increase in the proteins was 13% and 9%, respectively, as determined by immunohistochemistry. The serotonin antagonist, α-p-chlorophenylalanine, effectively blocked the hypoglycemic effects and increased the signaling protein levels. After XN administration, none of the animals showed significant changes in plasma-free fatty acids in 60 min. In summary, the XN extract may have hypoglycemic effects in normal Wistar and SIIR rats that may have a serotonin-related hypoglycemic effect and enhance insulin sensitivity in the SIIR rats. Copyright © 2015 John Wiley & Sons, Ltd.

With numerous pharmacological and biological functions bio-flavonoids gain appreciable attention in diabetes and other therapeutic research. Among several beneficial flavonoids quercetin exhibits impressive hypoglycemic effects, with significant improvement, stabilization of long sustaining insulin secretion and regeneration of human islets in the pancreas without producing serious health hazards. However, in oral delivery poor solubility, stability in biological milieu, low permeation, short biological half-life, and insignificant bioavailability limit its wide application in anti diabetic research. Over the last few decades polymeric carrier systems have been widely studied for improvement of quercetin bioavailability. Natural polymers are more preferred in this regard as they possess several favourable properties like biocompatibility, biodegradability, mucoadhesiveness, non-immunogenicity and non-toxicity. This review focuses on quercetin in anti-diabetic research and the progress in the synthesis of polymer-based formulations for efficient quercetin delivery, with an emphasis on producing an improved biological efficacy of the flavonoid. Diabetic complications, probable mechanisms of quercetin absorption, regulation and anti diabetic effects, obstacles to produce desired bio-efficacy and possible remedies are also brought into focus. To overcome these barriers encapsulation of quercetin within various safe polymeric vehicles are discussed. Further, this review sheds light on enhancing the efficacy of quercetin in novel ways for successful diabetes treatment and others.

A surface extract of the aerial parts of Salvia chamaedryoides afforded 13 diterpenes (1-13), with seven compounds (1, 3, 4, 7-9, 12) described for the first time. The structures of the new compounds were established using 1D and 2D NMR spectroscopic methods, HRESIMS, and ECD data. The potential hypoglycemic effects of the crude extract, fractions, and pure compounds from S. chamaedryoides were investigated by inhibition of α-glucosidase and α-amylase enzymes. The extract and its fractions showed a moderate dose-dependent inhibition; the pure compounds exhibited differential inhibitory activity against these two enzymes. Molecular modeling studies were also performed to suggest the interaction mode of compound 3 in the α-glucosidase enzyme active site. The antimicrobial activity of the purified compounds was investigated against 26 clinical pathogens. No activity was detected for the Gram-negative species tested nor on Candida albicans and C. glabrata, while variable susceptibilities were observed using Gram-positive staphylococcal and enterococcal species.

Four new 5 beta,19-epoxycucurbitacins, kuguacins T-W (1-4, resp.), along with nine known cucurbitane derivatives, 5-13, were obtained from the fresh fruit of Momordica chrantia. Structures of the new metabolites were elucidated as 5 beta,19-epoxy-25-hydroxycucurbitane-3,7,23-trione (1), 5 beta,19-epoxy-3,7-dioxo-23,24,25,26,27-pentanorcucurbitan-22-oic acid (2), 5 beta,19-epoxy-3 beta-hydroxycucurbit-24-ene-7,23-dione (3), and 5 beta, 19-epoxy-25-hydroxycucurbit-23-ene-3,7-dione (4), by extensive spectroscopic investigations, which were confirmed by a single-crystal X-ray diffraction analyses in the case of compound 4.

The present study was carried out to establish the optimum microwave-assisted extraction (MAE) conditions of polysaccharides from root ofRhodiola sachalinensisA. BOR (RSPs) by using o orthogonal analysis methodology. Moreover, the hypoglycemic effects of RSPs were investigated. The results indicated that the optimal extraction conditions of RSPs were liquid-solid ratio of 45:1 mL/g, irradiation power of 480 W, and irradiation time of 8 min. The animal experiment results demonstrated that RSPs could significantly increase body weights, serum insulin levels, and reduce fasting blood glucose (FBG) levels, which suggested that RSPs possesses hypoglycemic effects,.

Buckwheat is rich in active substances with hypoglycemic effects. Submerged fermentation, as the method of brewing buckwheat vinegar, not only has the advantages of shortening production cycle, saving materials etc, but also has high functional active substances. In this study, the process of the submerged fermentation of acetic acid fermentation was optimized by the orthogonal experiments of L9 (34), which was also on the basis of single factor experiments. The results indicated that the conversion rate of acetic acid can become 95.8% when the initial alcohol at 6% (v / v), inoculum at 10%, fermentation temperature 30°Cand fermentation time 60 h.