scholarly journals Nanoparticles Prepared From Pterostilbene (PTE): A New Strategy for Reducing Blood Glucose and Improving Diabetic Complications

Author(s):  
Xi Zhao ◽  
Anhua Shi ◽  
Qiong Ma ◽  
Xueyan Yan ◽  
Ligong Bian ◽  
...  

Abstract Aim: New envisions are put forward on the cross application of plant extracts and biomaterials, especially new conjectures are put forward on glucose lowering nanodrug delivery systems.Study design and methods: In this study, pterostilbene (PTE) was esterified with acryloyl chloride firstly, and then 3-acrylamidophenyl boric acid (AAPBA) and PTE esterified by acryloyl chloride were copolymerized into p(AAPBA-b-PTE). The characterization and structure of its polymer were examined. Additionally, p(AAPBA-b-PTE) nanoparticles and insulin loaded p(AAPBA-b-PTE) nanoparticles were prepared. The properties of pH, temperature and glucose sensitivity were investigated. And tested the drug loading and release of NPs. The nanoparticle toxicity was observed through cell and animal experiments, and the nanoparticle biodegradation process under physiological conditions was also observed. Finally, the effects of NPs on reducing blood sugar, antioxidation and improving micro inflammation were investigated in vivo.Results: Based on PTE, we successfully synthesized p(AAPBA-b-PTE) NPs. The NPs were basically round in shape with sizes between 150 and 250 nm. It has good pH and glucose sensitivity. The entrapment efficiency (EE) of insulin loaded NPs is about 56%, and the drug loading (LC) is about 13%. The highest release of insulin was 70%, and the highest release of PTE was 85%. Meanwhile, the insulin could undergo self-regulation according to the change of glucose concentration, thus achieving an effective and sustained release. Both in vivo and in vitro experiments showed that the NPs were safe and nontoxic. Under physiological conditions, it can be completely degraded within 40 days. Fourteen days after the mice were injected with p(AAPBA-b-PTE) NPs, there were no obvious abnormalities in the heart, liver, spleen, lung, and kidney. Moreover, the NPs can effectively reduce blood glucose, improve the antioxidant capacity and improve the micro inflammation status in mice.Conclusions: Using PTE as raw material, p(AAPBA-b-PTE) NPs were successfully prepared, which can effectively reduce blood glucose, improve antioxidant capacity, and reduce inflammatory response. It provided a new way for the combination of plant extracts and biomaterials to regulate and treat diseases through NPs or other dosage forms.

2021 ◽  
Vol 19 (1) ◽  
Author(s):  
Xi Zhao ◽  
Anhua Shi ◽  
Qiong Ma ◽  
Xueyan Yan ◽  
Ligong Bian ◽  
...  

Abstract Background Diabetes complications are the leading cause of mortality in diabetic patients. The common complications are decline in antioxidant capacity and the onset of micro-inflammation syndrome. At present, glucose-responsive nanoparticles are widely used, as they can release insulin-loaded ultrafine particles intelligently and effectively reduce blood sugar. However, the toxicology of this method has not been fully elucidated. The plant extracts of pterostilbene (PTE) have a wide range of biological applications, such as antioxidation and inflammatory response improvement. Therefore, we have proposed new ideas for the cross application of plant extracts and biomaterials, especially as part of a hypoglycaemic nano-drug delivery system. Results Based on the PTE, we successfully synthesised poly(3-acrylamidophenyl boric acid-b-pterostilbene) (p[AAPBA-b-PTE]) nanoparticles (NPs). The NPs were round in shape and ranged between 150 and 250 nm in size. The NPs possessed good pH and glucose sensitivity. The entrapment efficiency (EE) of insulin-loaded NPs was approximately 56%, and the drug loading (LC) capacity was approximately 13%. The highest release of insulin was 70%, and the highest release of PTE was 85%. Meanwhile, the insulin could undergo self-regulation according to changes in the glucose concentration, thus achieving an effective, sustained release. Both in vivo and in vitro experiments showed that the NPs were safe and nontoxic. Under normal physiological conditions, NPs were completely degraded within 40 days. Fourteen days after mice were injected with p(AAPBA-b-PTE) NPs, there were no obvious abnormalities in the heart, liver, spleen, lung, or kidney. Moreover, NPs effectively reduced blood glucose, improved antioxidant capacity and reversed micro-inflammation in mice. Conclusions p(AAPBA-b-PTE) NPs were successfully prepared using PTE as raw material and effectively reduced blood glucose, improved antioxidant capacity and reduced the inflammatory response. This novel preparation can enable new combinations of plant extracts and biomaterials to adiministered through NPs or other dosage forms in order to regulate and treat diseases. Graphic abstract


2020 ◽  
Vol 21 (7) ◽  
pp. 605-612
Author(s):  
Lin Fan ◽  
Yani Fan ◽  
Hongwei Fan ◽  
Kaizong Huang

Objective: Frequent administrations for DPPIV-resistant GLP-1 analogs are necessary to maintain the blood concentrations due to the short half-life of less than 5 minutes. However, most delivery systems that possess the ability of sustainable release of GLP-1 have drawbacks such as low yield, high cost and undesirable side effects. Therefore, we aimed to prepare a simple and efficient delivery system that could be feasibly applied to reduce blood glucose. Methods: A novel GLP-1 delivery system (GLP-1-ELPs-SA) was prepared and characterized by circular dichroism. Furthermore, the activity and property of GLP-1-ELPs-SA were evaluated in vitro and in vivo. Results: GLP-1-ELPs-SA are easily expressed in E. coli in a soluble formulation and purified through the inverse transition cycle. GLP-1-ELPs-SA spontaneously generated depot under physiological conditions. GLP-1-ELPs-SA was also found to be dispersed in the blood vessels from the depot and showed a high affinity to bind with mice (C57BL/6J) albumin, which shows that GLP-1-ELPs-SA has a long circulation time in vivo. Conclusions: Our delivery system could markedly decrease the clearance of recombinant proteins based on serum albumin, without substantially increasing the protein molecular weight and remarkably reducing the blood glucose within 120 h.


2019 ◽  
Vol 9 (1) ◽  
Author(s):  
Li Yan Chan ◽  
Masaki Takahashi ◽  
Pei Jean Lim ◽  
Shinya Aoyama ◽  
Saneyuki Makino ◽  
...  

AbstractType 2 diabetes mellitus (T2DM) is a chronic disease, and dietary modification is a crucial part of disease management. Okara is a sustainable source of fibre-rich food. Most of the valorization research on okara focused more on the physical attributes instead of the possible health attributes. The fermentation of okara using microbes originated from food source, such as tea, sake, sufu and yoghurt, were explored here. The aim of this study is to investigate fermented okara as a functional food ingredient to reduce blood glucose levels. Fermented and non-fermented okara extracts were analyzed using the metabolomic approach with UHPLC-QTof-MSE. Statistical analysis demonstrated that the anthraquinones, emodin and physcion, served as potential markers and differentiated Eurotium cristatum fermented okara (ECO) over other choices of microbes. The in-vitro α-glucosidase activity assays and in-vivo mice studies showed that ECO can reduce postprandial blood glucose levels. A 20% ECO loading crispy snack prototype revealed a good nutrition composition and could serve as a fundamental formulation for future antidiabetes recipe development, strengthening the hypothesis that ECO can be used as a novel food ingredient for diabetic management.


Jurnal Kimia ◽  
2020 ◽  
pp. 5
Author(s):  
N. W. I. Paramitha ◽  
I. M. Sukadana ◽  
S. R. Santi

Buni (Antidesma bunius L. Spreng) is one of the traditional medicinal plants whose stem bark has been proven in vitro as an antidiabetic by inhibiting the activity of the ? glucosidase enzyme. This study aims to determine the potential of ethanol extract of buni bark to reduce blood glucose levels in wistar rats in vivo induced by alloxan. Two groups of control rats K (+) and K (-), and three groups of treated rats (P1, P2, and P3) which were given the extract with a dose of 50, 100, and 200 mg/ kg BW respectively, were induced with 150 mg / kg BW alloxan monohydrate to make the rats hyperglycemic. On the 14th day of the trial (posttest) the average blood glucose level was tested using ANOVA with a = 0.05 and Tamhane's. It was concluded that the 200 mg / kg BW ethanol extract of buni bark was able to reduce blood glucose levels to closer to the normal condition when compared to negative control K(-). Keywords: antidiabetic,  Antidesma bunius L. Spreng., GC-MS, stem barks


2012 ◽  
Vol 67 (4) ◽  
pp. 377-383 ◽  
Author(s):  
Eva Schrader ◽  
Silvia Wein ◽  
Karsten Kristiansen ◽  
Lars P. Christensen ◽  
Gerald Rimbach ◽  
...  

Plants ◽  
2020 ◽  
Vol 10 (1) ◽  
pp. 64
Author(s):  
Alexandra Epure ◽  
Alina E. Pârvu ◽  
Laurian Vlase ◽  
Daniela Benedec ◽  
Daniela Hanganu ◽  
...  

The present study analyzed the methanol extract and tincture obtained from the spontaneous Romanian Cichorium intybus species, in order to evaluate polyphenols content and some biological properties. Chromatographic and spectrophotometric methods were used for the analysis of polyphenols and the antioxidant capacity was assessed in vitro with DPPH● (2,2-diphenyl-picrylhydrazil) and FRAP (ferric-reducing antioxidant power) tests. The cardio-protective effects of Cichorii herba tincture on myocardial ischemia induced by isoprenaline and nephroprotection on renal failure induced by gentamicin were evaluated on rats. Also, aspartate aminotrasferase (AST), alanine aminotransferase (ALT), creatine kinase-MB (CK-MB) and creatinine clearance (CrCl) were measured. The antioxidant effect was evaluated by determining total oxidative stress (TOS), oxidative stress index (OSI, total antioxidant capacity (TAC), malondyaldehide (MDA), total thiols (SH) and total nitrites and nitrates (NOx). Cichoric acid was the main polyphenolic compound. The extracts had moderate in vitro antioxidant activity but the in vivo antioxidant and anti-inflammatory effects were significant and associated with myocardial and renal dysfunction improvement. The results were attributed to the content of polyphenols in the extracts, for which reason C. intybus may be considered an important raw material for pharmaceuticals formulations recommended in the prevention or treatment of heart or kidney diseases.


2018 ◽  
Vol 6 (12) ◽  
pp. 3219-3230 ◽  
Author(s):  
Zhenwei Yuan ◽  
Sisi Qu ◽  
Yuanyuan He ◽  
Yue Xu ◽  
Li Liang ◽  
...  

A phase-change material was used to design CuS-DOX-MBA@PCM nanoparticles, which could release the drug quickly in physiological conditions.


2012 ◽  
Vol 82 (3) ◽  
pp. 228-232 ◽  
Author(s):  
Mauro Serafini ◽  
Giuseppa Morabito

Dietary polyphenols have been shown to scavenge free radicals, modulating cellular redox transcription factors in different in vitro and ex vivo models. Dietary intervention studies have shown that consumption of plant foods modulates plasma Non-Enzymatic Antioxidant Capacity (NEAC), a biomarker of the endogenous antioxidant network, in human subjects. However, the identification of the molecules responsible for this effect are yet to be obtained and evidences of an antioxidant in vivo action of polyphenols are conflicting. There is a clear discrepancy between polyphenols (PP) concentration in body fluids and the extent of increase of plasma NEAC. The low degree of absorption and the extensive metabolism of PP within the body have raised questions about their contribution to the endogenous antioxidant network. This work will discuss the role of polyphenols from galenic preparation, food extracts, and selected dietary sources as modulators of plasma NEAC in humans.


2019 ◽  
Author(s):  
Hamilton Lee ◽  
Jenica Lumata ◽  
Michael A. Luzuriaga ◽  
Candace Benjamin ◽  
Olivia Brohlin ◽  
...  

<div><div><div><p>Many contrast agents for magnetic resonance imaging are based on gadolinium, however side effects limit their use in some patients. Organic radical contrast agents (ORCAs) are potential alternatives, but are reduced rapidly in physiological conditions and have low relaxivities as single molecule contrast agents. Herein, we use a supramolecular strategy where cucurbit[8]uril binds with nanomolar affinities to ORCAs and protects them against biological reductants to create a stable radical in vivo. We further over came the weak contrast by conjugating this complex on the surface of a self-assembled biomacromolecule derived from the tobacco mosaic virus.</p></div></div></div>


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