&lt;p&gt;Enzyme Inhibitory, Antioxidant And Antibacterial Potentials Of Synthetic Symmetrical And Unsymmetrical Thioureas&lt;/p&gt;

Naz, Sumaira; Zahoor, Muhammad; Umar, Muhammad Naveed; Ali, Barkat; Ullah, Riaz; Shahat, Abdelaaty A.; Mahmood, Hafiz Majid; Sahibzada, Muhammad Umar Khayam

doi:10.2147/dddt.s225311

Cited by 19 publications

(18 citation statements)

References 19 publications

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“…Up-till now, many plants have been investigated extensively to search natural antioxidants to prevent/minimize the destructive process caused by the oxidative stress [64]. Several natural products are reported here which have proven antioxidant attributes including thioureas derivatives [57] trans-13-Octadecenoic acid, methyl ester, 9-Octadecenoic acid (Z)-, methyl ester [42], uleine [43], acetamide derivatives [65] and squalene [46]. Thus, the Rhazya stricta root extracts displayed its potential for DM by lowering blood glucose level through different mechanisms that might be a synergistic effect of many of the phytoconstituents present in the extracts.…”

Section: Discussionmentioning

confidence: 99%

“…Interestingly, among the identified compounds in the SCL fraction, five have already been documented as antihyperglycemic compounds namely; Hexadecane [ 40 ], n-Hexadecanoic acid [ 41 ], Vinburnine, Vincamine [ 44 ] and Squalene [ 45 ]. Some other classes of compounds have also been identified and derivatives of which are reported of antidiabetic potential like Benzofuran [ 51 ], Quinoxaline [ 52 ] Quinoline [ 53 , 54 ], Pyridine [ 55 ], Sydnones [ 56 ] Thioureas [ 57 ] and Isoquinolines [ 58 ]. Moreover, Berberine, that is an Isoquinoline alkaloid isolated from Rhizoma coptidis has shown hypoglycemic and anti-dyslipidemic activities [ 58 ].…”

Section: Discussionmentioning

confidence: 99%

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Assessment of antidiabetic potential and phytochemical profiling of Rhazya stricta root extracts

Mahmood

Kayani

Ahmed

et al. 2020

BMC Complement Med Ther

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Background Diabetes mellitus is a chronic disease characterized by hyperglycemia that may occur due to genetic, environmental or lifestyle factors. Natural remedies have been used to treat diabetes since long and many antidiabetic compounds of varied efficacies have been isolated from medicinal plants. Rhazya stricta has been used for decades for the treatment of diabetes mellitus and associated ailments. Considering the folkloric use of R. stricta against diabetes, it was aimed to investigate the effectiveness of its root extracts against diabetes through in vitro assays and in vivo studies using animal model along with phytochemical profiling through GCMS. Methods Various fractions of Rhazya stricta obtained through column chromatography were evaluated for a variety of assays including α-glucosidase, Dipeptidyl peptidase-IV (DPP-IV), β-secretase and Glucagon-like peptide-1 (GLP-1) secretion studies. For the in vivo studies the alloxan-induced diabetic mice were treated with root extracts and blood glucose levels, HbA1C, and other biochemical markers along with the histological study of the liver were done. The phytochemical identification was performed using an Agilent 7890B GC coupled to a 7010 Triple Quadrupole (MS/MS) system. GraphPad Prism software version 5.01 was used for statistical analysis. Results Majority of the extract fractions showed excellent results against diabetes by inhibiting enzymes DPP-IV (Up to 61%) and β-secretase (Up to 83%) with IC50s 979 μg/ml and 169 μg/ml respectively with increase in the GLP1 secretion. The results of in vivo studies indicated a marked reduction in blood glucose and HbA1c levels along with positive effects on other parameters like lipid profile, liver functions and renal functions of extract-treated mice as compared to control. The histological examination of the liver demonstrated hepatoprotective effects against diabetes led changes and various classes of phytochemicals were also identified through GCMS in different fractions. Conclusion The results revealed strong antidiabetic activity of R. stricta root with the potential to protect body organs against diabetic changes. Moreover, a variety of phytochemicals has also been identified through GCMS that might be responsible for the antidiabetic potential of Rhazya stricta root. Graphical abstract

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Assessment of antidiabetic potential and phytochemical profiling of Rhazya stricta root extracts

Mahmood

Kayani

Ahmed

et al. 2020

BMC Complement Med Ther

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“…9,10 Thus, Al promotes aggregation of insoluble amyloid-b-protein, hyperphosphorylated tau-protein and causes more pathological changes in cholinergic system. 11,12 This might be the possible way by which aluminum involving in pathological process of dementia. In the management of dementia, acetylcholinesterase inhibition and oxidative stress inhibition are the important therapeutic strategies.…”

Section: Introductionmentioning

confidence: 99%

Naringin Attenuates Aluminum Induced Cognitive Deficits in Rats

Orsu¹

2020

IJPER

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Aim: The exposure of aluminum for longer period in brain can lead to impaired cognition and behavioral changes. The present study was aimed to investigate the aluminum induced cognitive deficits and possible protective outcomes of naringin. Materials and Methods: Aluminum chloride in a dose of 100 mg/kg i.p was employed for 60 days to induce cognitive deficits in Westar rats. The animals were divided into groups each group contain six animals, as normal, aluminum treated, naringin treated (25, 50, 100 mg/kg). These animals were used to estimate behavioral characters such as Open field, eight arm radial maze, Morris water maze and Rota-rod tests and also used to assess the biochemical parameters such as acetylcholine esterase activity, malondialdehyde, superoxide dismutase and catalase. Results: Aluminum intoxicated rats showed significantly reduced exploratory and spontaneous locomotors activities in open field test and significant impairment in working and learning memory assessed by Morris water maze and radial arm maze tests. It also significantly increased acetylcholine esterase activity and malondialdehyde. The superoxide dismutase and catalase were also decreased significantly. Naringin was given (25, 50 and 100 mg/kg PO) to the aluminum intoxicated rats for a period of 30 days. The naringin treatment has shown significant improvements in spontaneous locomotors and exploratory activities and memory performance tasks of rats. Conclusion: The oxidative stress (reduced lipid peroxidation, restored reduced superoxide dismutase and catalase) and acetylcholine esterase activity were significantly decreased in the naringin group. Thus, these findings supported that naringin has showed potential neuroprotection against aluminum induced oxidative stress and cognitive deficit.

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“…The area is yet to be explored and researched further. There is a need to find out the potential inhibitors from different classes of organic compounds that can be effective and safe to inhibit any of the different enzymes involved in carbohydrate metabolism ( Naz et al, 2019 ).…”

Section: Introductionmentioning

confidence: 99%

“…In our previous work, where 3 out of 5 thioureas showed promising antidiabetic potential in term of inhibiting alpha amylase and glucosidase enzymes ( Naz et al, 2019 ). In connection to that work, the current study is concerned with i n vitro and in vivo inhibition of glucose-6-phosphatase by the previously synthesized compounds, and their toxicological evaluation in Swiss albino mice.…”

Section: Introductionmentioning

confidence: 99%

In vivo glucose-6-phosphatase inhibitory, toxicity and antidiabetic potentials of 2-picolylamine thioureas in Swiss albino mice

Naz

Zahoor

Umar

et al. 2020

Saudi Journal of Biological Sciences

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The 2-picolylamine is a simplest analogue of the alkaloid that has secondary and tertiary nitrogen function in its cyclic structure like that of alkaloids that can be derivatized to a number of biologically active compounds. In connection to our previous work, in the present work, three thiourea derivatives ( I = 1,3- bis (2-benzyl-3-phenyl-1-(pyridine-2-yl) propyl) thiourea, II = 1,3-bis (pyridin-2-ylmethyl) thiourea, and III = 1-(2-benzyl-3-phenyl-1-(pyridine-2-yl) propyl)-3-phenylthiourea) were synthesized using 2-picolylamine template which is a readily available synthetic analogue of naturally occurring alkaloid. The biological effect of the synthesized derivatives were monitored on the activity of glucose-6-phosphatase in Swiss albino mice (21-days). The derivatives were also tested for their potential toxicity in a 28-days sub-chronic toxicity studies by assessing their effects on different parameters like hematological, serum biochemistry and liver histology. The therapeutic effect of the safe derivative ( I ) was examined in streptozotocin-induced diabetic mice as well. The derivatives showed inhibition of the enzyme activity from good to an excellent degree. Compound I had the highest inhibition with 21.42 ± 5.113 mg of the released phosphate as compared to that of the positive control group (84.55 ± 3.213 mg). Only I turned out to be safe for use in animals without exerting any toxic or lethal effects on any of the assessed parameters in the used animal model. Compound I efficiently reversed the effects like hyperglycemia, hyperlipidemia and weight loss in the test animals. Out of these three-tested compounds, I was found safe to be use as therapeutic agent in diabetes complications. However, further toxicological studies in other animal models are needed as well.

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<p>Enzyme Inhibitory, Antioxidant And Antibacterial Potentials Of Synthetic Symmetrical And Unsymmetrical Thioureas</p>

Cited by 19 publications

References 19 publications

Assessment of antidiabetic potential and phytochemical profiling of Rhazya stricta root extracts

Assessment of antidiabetic potential and phytochemical profiling of Rhazya stricta root extracts

Naringin Attenuates Aluminum Induced Cognitive Deficits in Rats

In vivo glucose-6-phosphatase inhibitory, toxicity and antidiabetic potentials of 2-picolylamine thioureas in Swiss albino mice

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