Evaluation and docking of indole sulfonamide as a potent inhibitor of α-glucosidase enzyme in Streptozotocin -induced diabetic albino Wistar rats

2021 ◽  
pp. 104808
Author(s):  
Muhammad Taha ◽  
Syahrul Imran ◽  
Mohammed Salahuddin ◽  
Naveed Iqbal ◽  
Fazal Rahim ◽  
...  
Keyword(s):  
2021 ◽  
Vol 27 (1) ◽  
pp. 63-70
Author(s):  
Liang Yin ◽  
Mingxue Zhang ◽  
Tiangeng He

Abstract In recent years, ALR2 (aldose reductase) inhibitors have attracted attention for their effective ability to reduce the progression of diabetes-associated cataracts. Therefore, in the present article, we intended to develop novel thiazole-sulfonamide hybrids as a potent inhibitor of ALR2. These molecules significantly inhibited the ALR2 level in the rat lenses homogenate, where the most potent compound 7b showed activity comparable to sorbinil as standard. In Wistar rats, compound 7b improved the insulin level and body weight of the experimental animal together with a reduction in the glucose output. Compound 7b showed a significant reduction in the expression of ALR2 in rat lenses in western blot analysis.


1991 ◽  
Vol 260 (2) ◽  
pp. E163-E169 ◽  
Author(s):  
L. L. Espey ◽  
N. Tanaka ◽  
R. F. Adams ◽  
H. Okamura

Hydroxyeicosatetraenoic acid methyl esters (HETEs) are lipoxygenase products of arachidonic acid that are generated along with prostaglandins (PGs) during acute inflammatory reactions. Whereas it is well known that ovarian PG levels increase during the ovulatory process, little is known about ovarian HETEs. This report compares the ovarian changes in 5-, 12-, and 15-HETE with ovarian PGE and PGF, along with progesterone, 17 alpha-hydroxyprogesterone, 4-androstene-3,17-dione, testosterone, and 17 beta-estradiol. Ovulation was induced in immature Wistar rats by sequential treatment with pregnant mare's serum gonadotropin and human chorionic gonadotropin (hCG). Follicles began rupturing 10 h after hCG treatment. The greatest correlation was among 12-HETE, 15-HETE, and progesterone, which increased to peak levels at 10 h after hCG. In contrast, the ovarian levels of 5-HETE, 17 alpha-hydroxyprogesterone, testosterone, and 17 beta-estradiol all declined sharply beginning 4 h after hCG. 2 alpha,4 alpha,7-4,5-Epoxy-17-hydroxy-4,17-dimethyl-3-oxo-androstane-2- carbonitrile (epostane), a potent inhibitor of steroid synthesis and ovulation, sharply reduced the synthesis of all five steroids within 30 min after its injection at 3 h after hCG. Among the five eicosanoids, epostane mainly inhibited 15-HETE. The results suggest that 15-HETE, along with progesterone, may have an important role in ovulation.


Gut ◽  
1997 ◽  
Vol 41 (6) ◽  
pp. 778-784 ◽  
Author(s):  
T H J Florin

Background and aims—The colons of patients with pneumatosis cystoides coli produce excessive H2. Exposure to alkyl halides could explain this. Six consecutive patients who had pneumatosis cystoides coli while taking chloral hydrate (1–5+ g/day) are reported. Patients 2 and 3 were investigated after they had ceased chloral hydrate treatment. One produced methane, the other did not. (Pneumatosis cystoides coli patients are non-methanogenic according to the literature.) Both had overnight fasting breath H2 of less than 10 ppm. A literature review disclosed just one patient who was using chloral at the time of diagnosed pneumatosis cystoides coli, but an epidemic of the disease in workers exposed to trichloroethylene.Methods—(i) In vitro experiments with human faeces: chloral or closely related alkyl halides were added to anaerobic faecal cultures derived from four methane-producing and three non-methanogenic human subjects. H2 and CH4gases were measured. (ii) In vivo animal experiment: chloral hydrate was added to drinking water of four Wistar rats, and faecal H2 compared with control rats.Results—Alkyl halides increased H2 up to 900 times in methanogenic and 10 times in non-methanogenic faecal cultures. The Ki of chloral was 0.2 mM. Methanogenesis was inhibited in concert with the increase in net H2. In the rat experiment, chloral hydrate increased H2 10 times, but did not cause pneumatosis.Conclusions—Chloral and trichloroethylene are alkyl halides chemically similar to chloroform, a potent inhibitor of H2 consumption by methanogens and acetogens. These bacteria are the most important H2-consuming species in the colon. It is postulated that exposure to these alkyl halides increases net H2 production, which sets the scene for “counterperfusion supersaturation” and the formation of gas cysts. In recent times, very low prescribing rates for chloral have caused primary pneumatosis cystoides to become extremely rare. As with primary pneumatosis, secondary pneumatosis cystoides, which occurs if there is small bowel bacterial overgrowth distal to a proximally located gut obstruction, is predicted by counterperfusion supersaturation. “Inherent unsaturation” due to metabolism of O2 is a safety factor, which could explain why gas bubbles do not form more often in tissue with high H2 tension.


Author(s):  
D. J. McComb ◽  
J. Beri ◽  
F. Zak ◽  
K. Kovacs

Investigation of the spontaneous pituitary adenomas in rat have been limited mainly to light microscopic study. Furth et al. (1973) described them as chromophobic, secreting prolactin. Kovacs et al. (1977) in an ul trastructural investigation of adenomas of old female Long-Evans rats, found that they were composed of prolactin cells. Berkvens et al. (1980) using immunocytochemistry at the light microscopic level, demonstrated that some spontaneous tumors of old Wistar rats could contain GH, TSH or ACTH as well as PRL.


Author(s):  
G. Ilse ◽  
K. Kovacs ◽  
N. Ryan ◽  
T. Sano ◽  
L. Stefaneanu ◽  
...  

Germfree state and food restriction have been shown to increase life span and delay tumor occurrence in rats. We report here the histologic, immunocytochemical and electron microscopic findings of adenohypophyses of aging, male Lobund-Wistar rats raised at Lobund Laboratories. In our previous study, the morphologic changes in the adenohypophyses of old rats have been extensively investigated by histology, immunocytochemistry and electron microscopy. Lactotroph adenomas were frequent in Long-Evans and Sprague-Dawley rats, whereas gonadotroph adenomas were frequent in Sprague-Dawley and Wistar rats.Male Lobund-Wistar rats were divided into four groups: 1) conventional, which were raised under normal non-germfree environment and received food ad libitum; 2) germfree-food ad libitum; 3) conventional environment-food restricted and 4) germfree-food restricted. The adenohypophyses were removed from 6-month-, 18-month- and 30-month-old rats. For light microscopy, adenohypophyses were fixed in formalin and embedded in paraffin.


Author(s):  
R. C. Kaufmann ◽  
F. K. Khosho ◽  
K. S. Amankwah

Diabetes decreases the fertility of females, but the mechanisms are not completely understood. In our investigations, we have found that 13% of the female BB Wistar rats that spontaneously developed chemical diabetes had persistent estrous. In this study the ovaries of these rats were examined by scanning electron microscopy(SEM) and compared to normal-cycling controls as well as to rats that had developed polycystic ovaries(PCO) by exposure to constant 1ight.


Author(s):  
I. Stachura ◽  
M. Pardo ◽  
J. Costello ◽  
D.M. Landwehr

Under experimental conditions severe reduction of renal mass results in the hyperfiltration of the remaining nephrons leading to a progressive renal insufficiency. Similar changes are observed in patients with various renal disorders associated with a loss of the functioning nephrons. The progression of renal damage is accelerated by high protein and phosphate intake, and may be modified by the dietary restrictions.We studied 50 five-sixth nephrectarrized male Wistar rats on a standard diet (Rodent Laboratory Chow 5001 Ralston Purina Co., Richmond, Indiana; containing 23.4% protein) over a 20 week period.


Author(s):  
S.K. Aggarwal ◽  
J.M. Fadool

Cisplatin (CDDP) a potent antitumor agent suffers from severe toxic side effects with nephrotoxicity being the major dose-limiting factor, The primary mechanism of its action has been proposed to be through its cross-linking DNA strands. It has also been shown to inactivate various transport enzymes and induce hypocalcemia and hypomagnesemia that may be the underlying cause for some of its toxicities. The present is an effort to study its influence on the parathyroid gland for any hormonal changes that control calcium levels in the body.Male Swiss Wistar rats (Crl: (WI) BR) weighing 200-300 g and of 60 days in age were injected (ip) with cisplatin (7mg/kg in normal saline). The controls received saline injections only. The animals were injected (iv) with calcium (0.5 ml of 10% calcium gluconate/day) and were killed by decapitation on day 1 through 5. Trunk blood was collected in heparinized tubes.


Author(s):  
D.N. Collins ◽  
J.N. Turner ◽  
K.O. Brosch ◽  
R.F. Seegal

Polychlorinated biphenyls (PCBs) are a ubiquitous class of environmental pollutants with toxic and hepatocellular effects, including accumulation of fat, proliferated smooth endoplasmic recticulum (SER), and concentric membrane arrays (CMAs) (1-3). The CMAs appear to be a membrane storage and degeneration organelle composed of a large number of concentric membrane layers usually surrounding one or more lipid droplets often with internalized membrane fragments (3). The present study documents liver alteration after a short term single dose exposure to PCBs with high chlorine content, and correlates them with reported animal weights and central nervous system (CNS) measures. In the brain PCB congeners were concentrated in particular regions (4) while catecholamine concentrations were decreased (4-6). Urinary levels of homovanillic acid a dopamine metabolite were evaluated (7).Wistar rats were gavaged with corn oil (6 controls), or with a 1:1 mixture of Aroclor 1254 and 1260 in corn oil at 500 or 1000 mg total PCB/kg (6 at each level).


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