Insulin releasing action of 2-[2-(4,5-dihydro-1H-imadazol-2-yl)-1-phenylethyl] pyridine dihydrochloride sesquihydrate (DG-5128), a new, orally effective hypoglycaemic agent

1982 ◽  
Vol 99 (3) ◽  
pp. 410-415 ◽  
Author(s):  
Kin-ya Kameda ◽  
Shin-etsu Ono ◽  
Isao Koyama ◽  
Yasushi Abiko

Abstract. 2-[2-(4,5-dihydro-1H-imidazol-2-yl)-1-phenyl-ethyl] pyridine dihydrochloride sesquihydrate (DG-5128) is a new orally effective hypoglycaemic agent structurally unrelated to the known hypoglycaemics. DG-5128 was found to decrease blood glucose levels by stimulating insulin release, like the sulphonylurea hypoglycaemics. However, the study with the rat Langerhans islets in vitro indicated a great difference in mode of stimulation of insulin release between DG-5128 and a sulphonylurea hypoglycaemic, tolbutamide. DG-5128 significantly reversed α-adrenergic inhibition of the glucose-primed insulin release from the islets, while tolbutamide did not. From the comparison with the effects of phentolamine, yohimbine and prazosine, DG-5128 was strongly suggested to stimulate the glucose-primed insulin release through antagonizing at α2-adrenoreceptors on the B cells.

2017 ◽  
Vol 36 (4) ◽  
pp. 433
Author(s):  
Nurhidajah Nurhidajah ◽  
Nurrahman Nurrahman

The process of germination of grains such as rice, could increase some nutritional values of  amino acids and dietary fiber. Red rice and its sprouts are believed to be able to decrease blood glucose in patients with diabetes mellitus (DM). The aim of this study was to evaluate the hypoglycemic effect of red rice sprouts in STZ-NA induced diabetic rats on blood glucose level, insulin level, and HOMA-IR and HOMA-β index. This experimental study was conducted based on randomized post test only control group design using 24 male Wistar rats aged 2.5 months. Rats were divided into 4 groups, one group without induction of STZ-NA fed with a standard diet (control) and three groups of STZ- NA induced with a standard diet, red rice and red rice germ. Experiments were conducted for 6 weeks. The results showed that sprouted red rice lowered blood glucose levels by 61.88 % and the value of HOMA-IR (insulin resistance parameters) by 56.82%. Insulin level increased by 16.35 % and HOMA-β by 763.6 %. This study showed that red rice germ was able to decrease blood glucose levels and increase insulin resistance of DM rats and the strength of the pancreatic beta cells. ABSTRAKProses perkecambahan biji-bijian seperti beras, dapat meningkatkan beberapa nilai gizi seperti asam amino dan serat pangan. Beras merah dan kecambahnya diyakini mampu menurunkan glukosa darah pada penderita diabetes melitus (DM). Tujuan penelitian ini adalah mengevaluasi efek hipoglikemik kecambah beras merah pada tikus diabetes yang diinduksi STZ-NA terhadap kadar glukosa darah, insulin, serta indeks HOMA-IR dan HOMA β. Penelitian ini bersifat eksperimental in vivo pada hewan coba tikus Wistar jantan usia 2,5 bulan sebanyak 24 ekor dengan desain penelitian randomized post test only control group. Tikus dibagi menjadi 4 kelompok, masing-masing 1 kelompok tanpa induksi STZ-NA dengan diet standar dan 3 kelompok diinduksi STZ-NA dengan diet standar, beras merah dan kecambah beras merah. Percobaan dilakukan selama 6 minggu. Hasil penelitian menunjukkan kecambah beras merah mampu menurunkan kadar glukosa darah sebesar 61,88 % dan nilai HOMA-IR (parameter resistensi insulin) 56,82 %. Kadar insulin meningkat 16,35 % dan HOMA β 763,6 %. Disimpulkan, kecambah beras merah mampu menurunkan kadar glukosa darah dan memperbaiki kondisi resistensi insulin tikus DM, dan kekuatan sel beta pankreas.


2019 ◽  
Vol 20 (6) ◽  
pp. 1517 ◽  
Author(s):  
Kai Wang ◽  
Yu Su ◽  
Yuting Liang ◽  
Yanhui Song ◽  
Liping Wang

Type 2 diabetes mellitus (T2DM) is associated with pancreatic β-cell dysfunction which can be induced by oxidative stress. Deuterohemin-βAla-His-Thr-Val-Glu-Lys (DhHP-6) is a microperoxidase mimetic that can scavenge reactive oxygen species (ROS) in vivo. In our previous studies, we demonstrated an increased stability of linear peptides upon their covalent attachment to porphyrins. In this study, we assessed the utility of DhHP-6 as an oral anti-diabetic drug in vitro and in vivo. DhHP-6 showed high resistance to proteolytic degradation in vitro and in vivo. The degraded DhHP-6 product in gastrointestinal (GI) fluid retained the enzymatic activity of DhHP-6, but displayed a higher permeability coefficient. DhHP-6 protected against the cell damage induced by H2O2 and promoted insulin secretion in INS-1 cells. In the T2DM model, DhHP-6 reduced blood glucose levels and facilitated the recovery of blood lipid disorders. DhHP-6 also mitigated both insulin resistance and glucose tolerance. Most importantly, DhHP-6 promoted the recovery of damaged pancreas islets. These findings suggest that DhHP-6 in physiological environments has high stability against enzymatic degradation and maintains enzymatic activity. As DhHP-6 lowered the fasting blood glucose levels of T2DM mice, it thus represents a promising candidate for oral administration and clinical therapy.


2020 ◽  
Vol 2020 ◽  
pp. 1-13
Author(s):  
Rafael Grassi de Alcântara ◽  
Heidge Fukumasu ◽  
Paulo Cesar Fabricio Raspantini ◽  
Leonila Ester Reinert Raspantini ◽  
Caroline Joy Steel ◽  
...  

The consumption of composite flour, such as green banana and corn flour, is related to maintain stable blood glucose levels, due to high resistant starch levels. However, most of these studies have conducted analyses of unprocessed food such as flour. Therefore, this study aimed to evaluate the effect of baking on resistant starch concentration and digestion from bread produced with partial wheat flour substitution. Response surface methodology was used to evaluate bread physical-chemical characteristics, and then, sensorial and nutritional qualities of the bread were evaluated. The feasibility of incorporating 40% of corn flour was demonstrated, while incorporation of 20% produced bread with similar characteristics to the control; for green banana flour, these levels were 20 and 10%, respectively. Resistant starch levels of composite breads were also enhanced by in vitro analyses. On the other hand, in vivo blood glucose levels evidenced that the ingestion of breads produced with partial wheat flour substitution by green banana or corn flour promoted a more important peak in blood glucose levels in comparison with control bread, which was never previously presented in the literature. Bread ingestion rapidly increased the blood glucose levels of rats; once during the baking process, starch granules become gelatinized and therefore easily digestible. Furthermore, this study also highlighted the lack and need for future investigation of wheat flour-substituted baked goods, in order to better understand mechanical properties formation and also product digestibility.


mBio ◽  
2020 ◽  
Vol 11 (2) ◽  
Author(s):  
Rebecca J. Marshall ◽  
Pornthida Armart ◽  
Katina D. Hulme ◽  
Keng Yih Chew ◽  
Alexandra C. Brown ◽  
...  

ABSTRACT People with diabetes are two times more likely to die from influenza than people with no underlying medical condition. The mechanisms underlying this susceptibility are poorly understood. In healthy individuals, small and short-lived postprandial peaks in blood glucose levels occur. In diabetes mellitus, these fluctuations become greater and more frequent. This glycemic variability is associated with oxidative stress and hyperinflammation. However, the contribution of glycemic variability to the pathogenesis of influenza A virus (IAV) has not been explored. Here, we used an in vitro model of the pulmonary epithelial-endothelial barrier and novel murine models to investigate the role of glycemic variability in influenza severity. In vitro, a history of glycemic variability significantly increased influenza-driven cell death and destruction of the epithelial-endothelial barrier. In vivo, influenza virus-infected mice with a history of glycemic variability lost significantly more body weight than mice with constant blood glucose levels. This increased disease severity was associated with markers of oxidative stress and hyperinflammation both in vitro and in vivo. Together, these results provide the first indication that glycemic variability may help drive the increased risk of severe influenza in people with diabetes mellitus. IMPORTANCE Every winter, people with diabetes are at increased risk of severe influenza. At present, the mechanisms that cause this increased susceptibility are unclear. Here, we show that the fluctuations in blood glucose levels common in people with diabetes are associated with severe influenza. These data suggest that glycemic stability could become a greater clinical priority for patients with diabetes during outbreaks of influenza.


1997 ◽  
Vol 27 (8) ◽  
pp. 685-689 ◽  
Author(s):  
J. J. M. LIGTENBERG ◽  
C. E. VENKER ◽  
W. J. SLUITER ◽  
W. D. REITSMA ◽  
T. W. VAN HAEFTEN

2018 ◽  
Vol 10 (3) ◽  
pp. 636-641
Author(s):  
Anisa Rachma Sari ◽  
Tyas Rini Saraswati ◽  
Enny Yusuf Wachidah Yuniwarti

Insulin leave (Tithonia diversifolia (Hemsl.) A. Gray) empirically used by people as antihyperglycemic drugs. The study was aimed to evaluate antihyperglycemic activity as well as to determine the most optimum dose of T. diversifolia to reduce blood glucose levels. Hyperglycemic condition was induced to male Rattus norvegicus rats by intraperitoneal injection of alloxan at a dose of 150 mg/kg bw (body weight). In this study, completely randomized design was performed with three treatment groups and five times repetition. Group P1 received glibenclamide 10 mg/kg bw, P2 received aqueous extract of T. diversifolia at a dose of 150 mg/kg bw, P3 received aqueous extract of T. diversifolia at a dose of 300 mg/kg bw. Administration of both glibenclamide and aqueous extract of T. diversifolia was conducted orally for 28 days. Data were analyzed using Anova and Duncan’s test with 95% confidence level (α = 0.05). The results showed that the mean percentage of decrease in blood glucose levels, drink intake and body weight of all treatment groups were not significantly different (p>0.05). Data of feed intake showed that P1 was significantly different from P2 (p<0.05), but P2 was not significantly different from P3 (p>0.05). Based on the result of this research, it was found that the low doses of aqueous extract of T. diversifolia has the same ability to decrease blood glucose level compared to glibenclamide. Futhermore, this study provide some information that can be used as preclinical analysis to determine effective doses of aqueous extract of T. diversifolia to decrease blood glucose levels.  


2019 ◽  
Vol 13 (2) ◽  
Author(s):  
Irfani Rahmi ◽  
Roslizawaty Roslizawaty ◽  
Azhar Azhar ◽  
Razali Daud ◽  
Syafruddin Syafruddin ◽  
...  

Author(s):  
Aymen Owais Ghauri ◽  
Saeed Ahmad ◽  
Tayyeba Rehman

AbstractBackgroundDiabetes is the one of the leading cause of morbidity and mortality. Traditionally phytotherapy is widely being used for diabetes treatment and highly valued. Citrus colocynthis has known anti-diabetic potential. However, anti-diabetic potential of hydro-ethanolic extract of C. colocynthis pulpy flesh with seeds is not reported yet.MethodsThe extract of C. colocynthis pulpy flesh with seeds was done by maceration method using 70% ethanol. To evaluate anti-diabetic and antioxidant potential of the seeded fruit in vitro, α-glucosidase and DPPH inhibition assays was done, respectively. In vivo study used streptozotocin (STZ) induced diabetes model of rats. Rats were randomized in five groups i. e. normal control, negative control, standard control, C. colocynthis 150 and 300 mg/kg. STZ was administered to all groups except normal control. After wards, plant extract and glibenclamide is continued for 14 days. Blood samples were collected from rat tail vein daily and from Cardiac puncture at the end of study. The blood glucose levels were monitored daily by using one-touch blood glucose monitoring system. The blood glucose level was monitored on 0, 1st, 5th, 8th, 11th, and 14th day of induction.ResultsHydro-ethanolic extract of C. colocynthis pulpy flesh with seeds was able to decolorize DPPH and therefore possess antioxidant potential, continuous administration for 14 days showed a marked decrease in serum glucose levels (p 0.01) it is found to be somewhat less effective as glibenclamide (standard control) (p 0.001). A time-dependent decrease in blood glucose levels was observed (351.3 ± 4 to 258 m/kg).ConclusionHydro-ethanolic extract of C. colocynthis pulpy flesh with seeds lowered the serum triglyceride and cholesterol levels in diabetic rats significantly as compared to negative control. The hypoglycemic effect of hydro-ethanolic extract of C. colocynthis pulpy flesh with seeds is may be due to α-glucosidase inhibition potential.


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