Antidiabetic Components Research Articles

Identification of antidiabetic components from Cyclocaryapaliurus

Cyclocarya paliurus (C. paliurus) is a well-known new food resource whose extraction has certain antidiabetic activity. In this study, compounds were prepared from C. paliurus and their antidiabetic activity were further evaluated in vivo and in vitro. Besides, chemical structures of these compounds were analyzed using nuclear magnetic resonance (NMR). The study showed that compounds extracted from C. paliurus showed excellent antidiabetic activity, which was shown in hypoglycemic effect, lipid metabolism regulation, antioxidant enzyme system improvement, insulin sensitivity increasing and repairment of islet cells. Two major antidiabetic compounds were identified, namely quercetin-3-O-β-D-glucuronide-6′-methyl ester (compound 1) and kaempferol-3-O-β-D-glucuronide-6′-methyl ester (compound 2), and compound 1 was firstly discovered in C. paliurus. Compounds 1 and 2 were proved great inhibition in vitro with IC50 values of 48.25 μg/mL, 66.30 μg/mL of α-amylase inhibition and 115.2 μg/mL, 136.8 μg/mL of α-glucosidase inhibition, respectively. Molecular docking analysis proved that compounds can bind to the active sites of enzymes. The results explored the antidiabetic compounds of C. paliurus, which can further help promote development of C. paliurus and enlarge kinds of therapeutic alternatives to antidiabetic recipes.

A Review of the Interactive Effects of Exercise and Medicinal Plants on Glycemic Indices and Lipid Profile in Diabetes Mellitus

Background: Diabetes is a common and non-communicable disease that is on the rise around the world due to the lifestyle and eating habits of people. Long-term complications of diabetes include retinopathy, neuropathy, nephropathy, cardiac symptoms, genitourinary symptoms, sexual symptoms, and cerebrovascular events. Based on the numerous studies to reduce the complications of diabetes, exercise and medicinal plants (due to not having the side effects of synthetic drugs) are the most important strategies to control blood glucose and hyperlipidemia; however, the simultaneous impact of these two interventions has recently been considered by researchers. Therefore, it seems necessary to review these studies in the field of sports nutrition and use these two interventions at the same time. Objective:This study aimed to review the effects of consuming 10 medicinal plants simultaneously with exercise. Methods We searched all databases, especially Web of Science, PubMed, SID, Magiran, with relevant keywords, such as "medicinal plant", "anti-diabetic component", "exercise", "training", "glycemic index", and "lipid profile", without time limit. The articles were then categorized based on exercise and herbs on carbohydrates and lipids metabolism. Results: According to the studies conducted in the databases, 564 articles related to exercise and medicinal plants were observed. However, according to the inclusion criteria (dealing with physical activity, medicinal plants, and also diabetes), 34 articles related to the effects of exercises and medicinal plants in diabetes status were selected. Among the obtained studies, 10 medicinal plants, most of which were studied simultaneously with exercises, were examined. The results showed that medicinal plants, with their antioxidant activity and mechanisms related to stimulating insulin secretion, control hyperlipidemia. They act along with exercise activities depending on the type, intensity, and duration and increase the body's antioxidant activity and glucose consumption in muscle via non-insulin-dependent pathways in diabetic conditions. Conclusion: It seems that due to the challenging nature of the exercise intervention, using plant antioxidants along with physical activity will lead to improved metabolic parameters in diabetic patients. However, to confirm the safety of consumption, besides examining the therapeutic effects of plants and their active compounds, their toxicity should also be investigated. Also, the small number of samples, failure to follow the long-term effects of simultaneous use of medical plants and exercise, and lack of precise diet control in human samples are limitations of this study. So conducting human studies in this area with caution and deleting the overcoming limitations is necessary for future research.

Antioxidant, antidiabetic and identification of phenolic constituents from Potentilla discolor Bge.

The objective of this study was to investigate the antioxidant and enzyme inhibitory activity, and characterize the bioactive constituents of the phenolic extract of Potentilla discolor Bge. Dry material of Potentilla discolor Bge. was extracted with 80% ethanol solution to obtain the crude phenolic extract (CPE) with the total phenolic content (TPC) of 20.40 ± 0.69 mg of gallic acid equivalents per gram of dry material (mg GAE/g DM). After purified with AB-8 macroporous resin, TPC of the purified phenolic extract (PPE) (353.65 ± 5.50 mg GAE/g DM) was much higher than that of the CPE. PPE exhibited stronger 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity and 2,2′-azino-bis 3-ethylbenzothiazoline-6-sulfonic acid (ABTS) radical scavenging activity than CPE and 2,6-Di-tert-butyl-4-methylphenol (BHT), with the IC50 values of 0.030 ± 0.002 mg/mL and 0.059 ± 0.002 mg/mL, respectively. The total antioxidant activities of PPE and BHT were similar, and were higher than CPE. PPE was found to significantly inhibit α-amylase and α-glucosidase with IC50 values of 0.966 ± 0.072 and 2.431 ± 0.088 mg/mL, respectively. Finally, using UPLC-TOF–MS/MS technology, 35 compounds were tentatively identified, including 12 phenolic acids, 23 flavonoids and their derivatives, 29 of which have been discovered for the first time in Potentilla discolor Bge. These results suggested that PPE had the potential to be used as an antioxidant and anti-diabetic component in functional foods.

Antidiabetic components from the hexane extract of red kidney beans (Phaseolus vulgaris L.): isolation and structure determination.

Red kidney beans (Phaseolus vulgaris L.) contain bioactive compounds that are known to exhibit antidiabetic effects via inhibition of α-glucosidase. However, information on the nonpolar components that exhibit antidiabetic activity is limited. Here, we report the isolation and structure determination of components with α-glucosidase inhibitory activity, which were obtained from the hexane extract of red kidney beans. Triacylglycerols (TAGs) were identified as the major components exhibiting inhibitory activity against α-glucosidase. The chemical structure of TAGs was determined by a combination of GC-MS and UPLC-MS/MS. The primary TAGs identified were LnLnLn (trilinolenin) and LnLLn (1,3-dilinolenoyl-2-linoleoyl glycerol). The major fatty acids present in these TAGs were α-linolenic acid (ω-3) and linoleic acid (ω-6). These TAGs were also found to inhibit the α-glucosidase activity in a similar fashion as acarbose. These results suggest that TAGs have potency as antidiabetics and support the potential suitability of red kidney beans for diabetes treatment.

Undescribed morroniside-like secoiridoid diglycosides with α-glucosidase inhibitory activity from Corni Fructus

Corni Fructus, also known as the fruit of Cornus officinalis Sieb. et Zucc., has long been used as a traditional Chinese medicine and is widely consumed as a nutritional food in the form of function drink and wine. Recently, Corni Fructus has attracted considerable interest because of its anti-diabetic effects. A systematic phytochemical investigation of Corni Fructus was performed to find anti-diabetic components, which led to the isolation of 10 unreported iridoid glycosides, cornusdiglycosides A−J (1–8, 9a/9b and 10a/10b). Their chemical structures were determined through spectroscopic analysis (ultraviolet [UV], infrared [IR], high-resolution electrospray ionisation mass spectroscopy [HRESIMS], one-dimensional [1D] and two-dimensional [2D] nuclear magnetic resonance [NMR]). Such morroniside-type diglycosides were first reported from natural sources, and all isolates were evaluated for α-glucosidase inhibitory activity. The results showed that all compounds (1–10) exhibited α-glucosidase (from Saccharomyces cerevisiae) inhibitory activities with IC50 values ranging from 78.9 ± 4.09 to 162.2 ± 9.17 μM, whereas acarbose, the positive control, displayed α-glucosidase inhibitory activity with IC50 value of 118.9 ± 7.89 μM.

Screening active components from Rubus amabilis for pancreatic β-cells protection

Context Rubus species (Rosaceae) have been used in folk medicine to treat diabetes due to their hypoglycaemic activity. Objective To screen the active components that act as hypoglycaemic agents in Rubus amabilis Focke and the underlying mechanisms. Materials and methods Aqueous stem extract of R. amabilis was incubated with MIN6 β-cells, PBS was used as the blank control. Then the cells were washed, cell membrane-bound components were dissociated and identified by UPLC/MS. Total procyanidins (PCs) in R. amabilis was enriched and the cytotoxicity and anti-proliferation on β-cell were evaluated by MTT assay. PCs at 25, 50, and 75 μg/mL was applied for 24 h to determine its effects on palmitate (PA)-induced apoptosis and GSIS. Western blotting was employed to detect the protein expression of PI3K/Akt/FoxO1 signalling. The antioxidant indices were also measured. Results β-Cell membrane-bound components were identified as three procyanidin B dimers and a C trimer. PCs showed no significant cytotoxicity up to a concentrations of 100 μg/mL. PCs treatment reversed the elevated apoptosis rate and impaired GSIS induced by PA. PCs markedly decreased the intracellular ROS and MDA production and increased the SOD activity. Moreover, PCs promoted the phosphorylation of Akt and FoxO1, and regulated Pdx-1 and Bax expression in MIN6 cells. Discussion and conclusion: The active components that act as hypoglycaemic agents in R. amabilis are procyanidins, which protected MIN6 cells against PA-induced apoptosis by activating PI3K/Akt/FoxO1 signalling. These results indicate that β-cell extraction, combined with UPLC/MS, is a valid method for screening antidiabetic components from herbal medicines.

(-)-O-Methylcubebin from Vitex trifolia Enhanced Adipogenesis in 3T3-L1 Cells via the Inhibition of ERK1/2 and p38MAPK Phosphorylation

In this study, for the purpose of elucidation for antidiabetic components, we isolated and identified compounds that could become lead compounds for the development of antidiabetic agents from the herbal medicine Vitex trifolia, which is used for liver protection in Myanmar. Three kinds of lignan, (-)-O-methylcubebin (MC), (-)-hinokinin, and (-)-cubebin, were isolated from the ethyl acetate extract of the leaves of V. trifolia, using various chromatography. Among the three isolated compounds, MC showed the strongest effects to increase intracellular lipid accumulation in 3T3-L1 cells. From the results of the elucidation of the MC’s effects on the adipogenesis of 3T3-L1 cells, the downsizing of adipocytes and the promotion of the expression of adipogenesis-related proteins, as well as adiponectin, were observed. On the other hand, since the activity of MC was inhibited by antagonists of PPARγ and improved by inhibitors of the classical mitogen-activated protein kinase (MAPK) pathway and p38MAPK pathway, MC was considered to be an agonist of PPARγ, and furthermore promoted adipogenesis via the inhibition of extracellular signal-regulated kinase 1/2 (ERK1/2) and p38MAPK phosphorylation. Although MC showed similar effects to those of rosiglitazone (RO) used as a positive control, RO promoted the migration of GLUT4 from the cytoplasm to the cell membrane, whereas MC did not show such an effect. From the abovementioned results, it was considered that MC could be a lead compound for the development of antidiabetic drugs that does not show weight gain, which is a side effect of RO.

Anti-hyperglycemic and anti-hyperlipidemic effects of a special fraction of Luohanguo extract on obese T2DM rats.

Luohanguo (LHG), a traditional Chinese medicine, could clear heat, moisten the lung, soothe the throat, restore the voice, and lubricate intestine and open the bowels. LHG has been utilized for the treatment of sore throats and hyperglycemia in folk medicine as a homology of medicine and food. The hypoglycemic pharmacology of LHG has attracted considerable attention, and mogrosides have been considered to be active ingredients against diabetes mellitus. We have found that these mogrosides could be metabolized into their secondary glycosides containing 1-3 glucose residues in type 2 diabetes mellitus (T2DM) rats in previous studies. These metabolites may be the antidiabetic components of LHG in vivo. Thus far, no reports have been found on reducing blood glucose of mogrosides containing 1-3 glucose residues. The aim of this study was to confirm that mogrosides containing 1-3 glucose residues were the active components of LHG for antidiabetic effects and to understand their potential mechanisms of action. First, the special fraction of mogrosides containing 1-3 glucose residues was separated from a 50% ethanol extract of LHG, and the chemical components were identified by ultra-performance liquid chromatography (UPLC) and named low-polar Siraitia grosvenorii glycosides (L-SGgly). Second, the antidiabetic effects of L-SGgly were evaluated by HFD/STZ-induced (high-fat diet and streptozocin) obese T2DM rats by indexing fasting blood glucose (FBG), fasting insulin (FINS), and insulin resistance, and then compared with other fractions in the separation process. The changes in serum lipid levels were also detected. Finally, possible mechanisms of antidiabetic activity of L-SGgly were identified as increasing GLP-1 levels and activating liver AMPK in T2DM rats. The chemical analysis of L-SGgly showed that they contain 11-oxomogroside V, mogroside V, mogroside III, mogroside IIE, mogroside IIIA1, mogroside IIA1, and mogroside IA1, respectively. The total content of the mogrosides in L-SGgly was 54.4%, including 15.7% mogroside IIA1 and 12.6% mogroside IA1. L-SGgly showed excellent effects on obese T2DM rats compared with the other fractions of LHG extract, including significantly reducing the levels of FBG (p < 0.001) and modifying insulin resistance (p < 0.05). Meanwhile, they could significantly decrease the content of triglyceride (p < 0.01), total cholesterol (p < 0.01), low-density lipoprotein cholesterol (p < 0.01) and free fatty acid (p < 0.001) and increase the content of high-density lipoprotein cholesterol (p < 0.001) in serum of T2DM rats. Moreover, L-SGgly can significantly increase (p < 0.01) GLP-1 levels and decrease (p < 0.01) IL-6 levels in T2DM rat serum. AMPK-activating activity in T2DM rats was also upregulated by L-SGgly, but no statistical significance was shown. L-SGgly, fractions separated from LHG extract, were verified to have obvious anti-hyperglycemic and anti-hyperlipidemic effects on T2DM rats. Furthermore, L-SGgly regulated insulin secretion in T2DM rats by increasing GLP-1 levels. These findings provide an explanation for the antidiabetic role of LHG.

Inhibitory effect of corosolic acid on α-glucosidase: kinetics, interaction mechanism, and molecular simulation.

The suppression of α-glucosidase activity to retard glucose absorption is an important therapy for type-2 diabetes. Corosolic acid (CRA) is a potential antidiabetic component in many plant-based foods and herbs. In this study, the interplay mechanism between α-glucosidase and corosolic acid was investigated by several methods, including three-dimensional fluorescence spectra, circular dichroism spectra, and molecular simulation. Corosolic acid significantly inhibited α-glucosidase reversibly in an uncompetitive manner and its IC50 value was 1.35 × 10-5 mol L-1 . A combination of CRA with myricetin exerted a weak synergy against α-glucosidase. The intrinsic fluorescence of α-glucosidase was quenched via a static quenching course and the binding constant was 3.47 × 103 L mol-1 at 298 K. The binding of CRA to α-glucosidase was mainly driven by hydrophobic forces and resulted in a partial extension of the protein polypeptide chain with a loss of α-helix content. The molecular simulation illustrated that CRA bound to the entrance part of the active center of α-glucosidase and interacted with the amino acid residues Ser157, Arg442, Phe303, Arg315, Tyr158, and Gln353, which could hinder the release of substrate and catalytic reaction product, eventually suppressing the catalytic activity of α-glucosidase. These results may suggest new insights into corosolic acid from food sources as a potential α-glucosidase inhibitor that could better control diabetes. © 2019 Society of Chemical Industry.

Network pharmacology-based analysis on bioactive anti-diabetic compounds in Potentilla discolor bunge

Ethnopharmacological relevancePotentilla discolor Bunge (PDB) is a commonly used herbal for alleviating diabetes mellitus and its complications. Although accumulating evidences show the anti-diabetic efficacy of PDB, the vital anti-diabetic compounds and their functional targets remain elusive. Aim of the studyTo investigate the anti-diabetic ingredients and their functional mechanisms in PDB, gas chromatograph-mass spectrometry analysis was performed on PDB extract and 21 were testified as anti-diabetic compounds. Materials and methodsSubsequently their potential protein targets were also identified. The bioinformatics analysis was implemented by network pharmacology-based approaches. STRING analysis was performed to reveal enrichment of these target proteins, protein-protein interactions, pathways and related diseases. Cytoscape was used to determine the potential protein targets for these components in PDB, indicating that 21 anti-diabetic compounds in PDB regulate 33 diabetes-related proteins in 28 signal pathways and involve 21 kinds of diabetes-related diseases. Among the 21 potential anti-diabetic components predicted by network analysis, tricetin was firstly experimentally validated at the molecular and cellular level. ResultsResults indicated that this active small-molecule compound may have beneficial effects on improving glucose uptake. ConclusionsWe envisage that network analysis will be useful in screening bioactive compounds of medicinal plants.

Effect-directed profiling of aqueous, fermented plant preparations via high-performance thin-layer chromatography combined with in situ assays and high-resolution mass spectrometry

Aqueous, fermented preparations from a vast range of medical plants are among the active pharmaceutical ingredients of homoeopathic medicinal products. In this study aqueous, fermented plant preparations from Chamomilla recutita L. (C.r.), Allium cepa L. (A.c.), Equisetum arvense L. (E.a.) and Hamamelis virginiana L. (H.v.) of different years of harvest were screened using a generic high-performance thin-layer chromatography (HPTLC) method hyphenated to effect-directed analysis (EDA) and high-resolution mass spectrometry (HRMS). Using 2,2-diphenyl-1-picrylhydrazyl radical (DPPH•), Gram-positive Bacillus subtilis and α-/β-glucosidase assays, followed by recording of elution head-based HPTLC-ESI-HRMS spectra, a fast assignment of multi-potent compounds was possible. This was exemplified for herniarin identified in C.r. and gallic acid in H.v. preparations. Strong radical scavenging and β-glucosidase inhibiting effects were observed for E.a. and H.v. preparations, whereas the most pronounced antibiotic activity against Gram-positive bacteria was found in C.r. and E.a. preparations. Besides the successful screening for radical-scavenging, antibiotic and anti-diabetic components, HPTLC-UV/Vis/FLD-EDA-HRMS provided profound information on aqueous, fermented plant preparations. Batch-to-batch variations of the plant preparations were not necessarily obvious from their HPTLC chromatograms, but could be substantiated based on their respective (bio)autograms. It became clear that effect-directed fingerprints allow the visualization and control of the fermentation processes in a meaningful sense.

Relationship of phenolic composition of selected purple maize (Zea mays L.) genotypes with their anti-inflammatory, anti-adipogenic and anti-diabetic potential

This study aimed to investigate the associations between phenolic composition of selected purple maize genotypes and their anti-inflammatory, anti-adipogenic and anti-diabetic properties in vitro. Anthocyanin-rich water extracts (PMWs) from 20 purple maize genotypes were evaluated in RAW 264.7 macrophages and 3T3-L1 adipocytes under different conditions. Cyanidin-3-O-glucoside (C3G), pelargonidin-3-O-glucoside (Pr3G), peonidin-3-O-glucoside (P3G) and corresponding acylated forms were major anthocyanins in PMW, accompanied by ten tentatively identified non-anthocyanin phenolics. Correlation studies showed that C3G, P3G, and derivatives, but not Pr3G and its acylated form contributed to the biological properties of PMW. Besides anthocyanins, quercetin, luteolin, and rutin were the dominant anti-inflammatory and anti-diabetic components, in terms of down-regulating pro-inflammatory mediator production in inflamed macrophages and adipocytes, modulating diabetes-related key enzymes and improving insulin sensitivity in insulin-resistant adipocytes. Quercetin and phenolic acids, especially vanillic acid and protocatechuic acid, were closely associated with anti-adipogenic properties of PMW via inhibition of the preadipocyte-adipocyte transition.

Angiopteris helferiana, a fern with great potential medicinal value: Antiadipogenic, anti-inflammatory, and anti-diabetic activity

Background: Angiopteris helferiana is used as a traditional medicine in some parts of Nepal and South-Asian countries. It is also used in traditional Chinese medicine system. Objective: In this study, we evaluated its anti-oxidant, anti-inflammatory, anti-obesity, and antidiabetic activity in cell and animal mode. Materials and Methods: The rhizome of A. helferiana was extracted with methanol and fractionated to give dichloromethane, ethyl acetate (EA), butanol (BuOH), and water fractions. The residue was again re-extracted with water to give water extract. The anti-oxidant property was measured using 1, 1-diphenyl-2-picryl-hydrazyl assay. The extract and fractions were evaluated for the α-glycosidase inhibition activity. The antiadipogenic and anti-inflammatory activity was studied in 3T3-L1–L1 and RAW 264.7 cells, respectively. The inhibition of expression of adipogenic markers peroxisome proliferator-activated receptor gamma (PPARγ), CCAAT enhancer binding protein alpha (C/EBPα) was studied in 3T3-L1 cells. The anti-obesity and antidiabetic study was done in high-fat diet mice model. Results: The EA, BuOH fraction, and water extract showed good anti-oxidant and α-glycosidase inhibition activity. EA fraction showed good anti-inflammatory activity. EA and BuOH fraction showed good antiadipogenic activity, reducing significantly, the lipid and adipogenic markers (PPARγ, C/EBPα) in 3T3-L1 cells. The BuOH fraction at 300 mg/kg/day dose showed good anti-obesity and antidiabetic activity in the in-vivo study after the evaluation of body weight, blood lipid, blood glucose, and lipid accumulation in adipose tissue and liver. Conclusion: Overall, A. helferiana is a good source of anti-oxidative, anti-inflammatory, anti-obesity, and antidiabetic component.

Antidiabetic-Like Effects of Naringenin-7-O-glucoside from Edible Chrysanthemum 'Kotobuki' and Naringenin by Activation of the PI3K/Akt Pathway and PPARγ.

Obesity is directly associated with cancer, cardiovascular injury, hypertension, and type 2 diabetes. To date, Yamamoto identified that hot water extracts of edible Chrysanthemum (EC) induced cell size reduction, up-regulation of adiponectin expression, and glucose absorption inhibition in 3T3-L1 cells during adipocyte differentiation. Furthermore, EC showed antidiabetic effects such as improvement in insulin resistance and the down-regulation of the blood glucose level and liver lipid content in type 2 diabetes model mice. In this study, we attempted to identify the antidiabetic components in EC. The methanol fraction from EC that showed relatively strong biological activity was purified by chromatography to obtain acacetin-7-O-glucoside, apigenin-7-O-glucoside, kaempferol-7-O-glucoside, and naringenin-7-O-glucoside. Among the isolated compounds and their aglycones, naringenin (NA) and naringenin-7-O-glucoside (NAG) up-regulated the intracellular accumulation of lipid and adiponectin-secretion and down-regulated the diameter of 3T3-L1 cells during adipocyte differentiation. Because the PPARγ antagonist BADGE and PI3K/Akt inhibitors wortmannin and LY29004 inhibited the intracellular lipid accumulation by NA and NAG associated with adipogenesis, it was considered that NA and NAG showed the above-mentioned activities via the activation of PPARγ as well as phosphorylation of the PI3K/Akt pathway.

Evaluation of antidiabetic activity of Ipomoea batatas L. extract in alloxan-induced diabetic rats.

Different allopathic drugs are being used for the treatment of diabetes mellitus but more emphasis are being placed on the use of medicinal plants, herbs, and natural extracts of fruits and vegetables due to their easy availability, easy consummation with low cost, and with no well-reported side effects. White skinned sweet potato (WSSP; Ipomoea batatas L.) peel-off was selected to find out its antidiabetic potential as well as to explore the effects on selected biochemical parameters in diabetes-induced Wistar rats. In young (3–4 months) and old (up to 1 year) diabetic Wistar rats, it was found that WSSP (I. batatas L.) peel-off significantly (P < 0.05) decreased blood glucose level, protein glycation level, total cholesterol, triglycerides, and low-density lipoprotein (LDL)-cholesterol. A significant (P < 0.05) increase in high-density lipoprotein (HDL)-cholesterol level after treatment was also reported. Furthermore, it was also found that WSSP peel-off also had beneficial effects on total protein concentration, albumin, globulin, and liver enzymes (serum glutamic oxaloacetic transaminase (SGOT) and serum glutamic pyruvic transaminase (SGPT)). It might be concluded that antidiabetic potential of WSSP extract is due to the presence of bioactive compounds like glycoprotein, anthocyanins, alkaloids, and flavonoids, which act as insulin-like molecules or insulin secretagogues constituents in sweet potatoes peel-off and these antidiabetic proteins were extracted out in more concentration in methanol due to its organic nature. Further research is needed to purify and quantify the antidiabetic components responsible for antidiabetic effects of WSSP and it should be available in compact dose form for the treatment of diabetic patients.

감국(Chrysanthemum indicum L.) 추출물과 분획물의 항산화 및 α-Glucosidase 와 PTP1B 저해 활성

In this study, we evaluated the polyphenol content, flavonoid content, antioxidant and biological of 70% EtOH extract and its fractions (dichloromethane, ethyl acetate and water) of the plant Chrysanthemum indicum L. (CI) belonging to family chrysanthemum. antioxidant activity was determined 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2’-azino-bis-3-ethylbenzthiazoline-6-sulphonic acid (ABTS), and superoxide scavenging activity. The biological activity tests included measurement of α-glucosidase and PTP1B. The results show that content of polyphenol and flavonoid in 70% EtOH of CI 30.20 mg and 31.58 mg, respectively. Among the different samples, ethyl acetate (EA) fraction showed the highest level of polyphenol (87.87 mg) and flavonoid (65.12 mg). The DPPH, ABTS and superoxide dismutase(SOD) antioxidant assay of EA fraction showed 93.84%, 93.38% and 84.68% inhibition respectively. The EA fraction also showed the highest antioxidant activity compared to 70% EtOH extract and other fractions. EA fraction (20 μg/mL) showed the highest 30.29% and 99.24%, respectively compared to other samples. The results of this study show that the EA fraction contained more antioxidant and antidiabetic components than 70% EtOH extract and other fractions. In conclusion, we believe that CI may be useful natural antioxidant and functional material.

Comparative In vitro antidiabetic and antioxidant activity of Pulicaria wightinia, Curcuma inodora, Derris scandens leaf extracts

In preventing the progression of various metabolic diseases, medicinal plants play very important role. The present study was focused on three different medicinal plants, Pulicaria wightiania, Derris scandens and Curcuma inodora commonly found in Narsapur forest of Medak district Telangana, (India), were screened for the potency of antioxidant and antidiabetic activity by various In-vitro methods. Three plants leaves were extracted using methanol and ethanol as solvents based on their solubility. Methanol extracts of Pulicaria wightiania, Derris scandens and ethanolic extract of Curcuma inodora plants leaves were examined. Antioxidant activities of three different extracts were evaluated by DPPH scavenging assay and putative antidiabetic activity was determined by in-vitro methods such as Glucose uptake by Yeast cells method, a-glucosidase inhibition activity assays. A dose dependent significant DPPH scavenging activity was found with three different plants when compared with standard drug ascorbic acid. The three plants leaf extracts exhibited a significant inhibitory action on a-glucosidase enzyme. The data obtained clearly suggests that the plant extract is capable of effectively enhancing glucose uptake which in turn suggests that it is capable of enhancing effective glucose utilization thereby controlling blood glucose level. The results suggest that these plants possess potential antioxidant and antidiabetic components.

Lignosulfonic acid promotes hypertrophy in 3T3-L1 cells without increasing lipid content and increases their 2-deoxyglucose uptake.

ObjectiveAdipose tissue plays a key role in the development of obesity and diabetes. We previously reported that lignosulfonic acid suppresses the rise in blood glucose levels through the inhibition of α-glucosidase activity and intestinal glucose absorption. The purpose of this study is to examine further biological activities of lignosulfonic acid.MethodsIn this study, we examined the effect of lignosulfonic acid on differentiation of 3T3-L1 cells.ResultsWhile lignosulfonic acid inhibited proliferation (mitotic clonal expansion) after induction of differentiation, lignosulfonic acid significantly increased the size of accumulated lipid droplets in the cells. Semi-quantitative reverse transcription polymerase chain reaction analysis showed that lignosulfonic acid increased the expression of the adipogenic transcription factor, peroxisome proliferator-activated receptor gamma (PPARγ), leading to increased glucose transporter 4 (Glut-4) expression and 2-deoxyglucose uptake in differentiated 3T3-L1 cells. Additionally, feeding lignosulfonic acid to diabetic KK-Ay mice suppressed increase of blood glucose level.ConclusionLignosulfonic acid may be useful as a functional anti-diabetic component of food.

Anti-diabetic activity in type 2 diabetic mice and α-glucosidase inhibitory, antioxidant and anti-inflammatory potential of chemically profiled pear peel and pulp extracts (Pyrus spp.)

Total phenolic acids, total flavonoids, total triterpenes contents, and eleven monomeric compounds, derived from eight different pears' peel and pulp, were qualitatively and quantitively profiled utilizing HPLC and HPLC-MS. All the chemical components found in the peel were approximately 2 to 18 folds concentrated than those in the pulp. Their antioxidant (reducing power and 2, 2-diphenyl-1-picrylhydrazyl/DPPH assay) and anti-inflammatory (xylene-induced mouse ear edema assay) activities were comparatively evaluated. Correlation analysis and principal component analysis were utilized to seek bioactive components in antioxidant and anti-inflammatory activities. Subsequently, Yaguang pear (Pyrus ussuriensis Maxim, with high polyphenols content) was selected to investigate in vitro and in vivo anti-diabetic potential (α-glucosidase inhibition assay and hypoglycemic assay in streptozocin-induced type 2 diabetic mice). Eleven monomeric compounds were seriatim examined for α-glucosidase inhibitory activity to fish out anti-diabetic components. For the first time, this study delineated pear peel's anti-diabetic prospect of treatment for type 2 diabetes.

Comparison on hypoglycemic and antioxidant activities of the fresh and dried Portulaca oleracea L. in insulin-resistant HepG2 cells and streptozotocin-induced C57BL/6J diabetic mice

Ethnopharmacological relevanceFresh Portulaca oleracea L. (family: Portulacaceae; POL) has been used as a folk medicine for the treatment of diabetes mellitus for a long time. More bioactive components with higher activity could be retained in fresh medicinal herbs compared to the dried ones. The present study was conducted to compare different antidiabetic activity between fresh and dried POL, including hypoglycemic and antioxidant activities both in vivo and in vitro. Furthermore, in order to explore which components were responsible for the antidiabetic activity, the difference on chemical components between fresh and dried POL was analyzed and compared. Materials and methodsInsulin-resistant HepG2 cells induced by insulin were used to evaluate the promoting effect of the fresh and dried POL on glucose utilization in vitro. Streptozotocin (STZ)-induced C57BL/6J diabetic mice were used to compare the differences on hypoglycemic and antioxidant activities of fresh and dried POL, including the fasting blood glucose, glucose tolerance, serum insulin level, malondialdehyde (MDA) level and superoxide dismutase (SOD) activity in vivo. UPLC/Q-TOF–MS method was performed to analyze the difference of antidiabetic components between fresh and dried POL. ResultsCompared with the dried POL extract, the fresh POL extract significantly increased the consumption of extracellular glucose in insulin-resistant HepG2 cells (P<0.05). In STZ-induced C57BL/6J diabetic mice, both fresh and dried extracts decreased markedly the fasting blood glucose (FBG) levels, and improved significantly oral glucose tolerance test (OGTT), as well as enhanced significantly insulin secretion and antioxidative activities (P<0.05; P<0.01). Furthermore, the fresh extract showed stronger antidiabetic activity (P<0.05). The UPLC/Q-TOF–MS analysis results also revealed that the relative contents of polyphenols and alkaloids in the fresh herbs were more abundant than those in the dried POL. ConclusionOur results indicated that both fresh and dried POL possessed antidiabetic activities, besides stronger activity was observed in the fresh herb. These findings provided evidence for the application and development of fresh POL in the treatment of diabetes mellitus.