scholarly journals In vitro investigations of the potential health benefits of Australian-grown faba beans (Vicia faba L.): chemopreventative capacity and inhibitory effects on the angiotensin-converting enzyme, α-glucosidase and lipase

2012 ◽  
Vol 108 (S1) ◽  
pp. S123-S134 ◽  
Author(s):  
Siem D. Siah ◽  
Izabela Konczak ◽  
Samson Agboola ◽  
Jennifer A. Wood ◽  
Christopher L. Blanchard
Keyword(s):  
Antioxidant Activity ◽  
Angiotensin Converting Enzyme ◽  
Pancreatic Lipase ◽  
Faba Bean ◽  
Phenolic Content ◽  
Health Benefits ◽  
Converting Enzyme ◽  
Inhibitory Effects ◽  
Faba Beans

The functional properties, including antioxidant and chemopreventative capacities as well as the inhibitory effects on angiotensin-converting enzyme (ACE), α-glucosidase and pancreatic lipase, of three Australian-grown faba bean genotypes (Nura, Rossa and TF(Ic*As)*483/13) were investigated using an array of in vitro assays. Chromatograms of on-line post column derivatisation assay coupled with HPLC revealed the existence of active phenolics (hump) in the coloured genotypes, which was lacking in the white-coloured breeding line, TF(Ic*As)*483/13. Roasting reduced the phenolic content, and diminished antioxidant activity by 10–40 % as measured by the reagent-based assays (diphenylpicrylhydrazyl, 2,2′-azino-bis(3-ethylbenzthiazoline-6-sulphonic acid) and oxygen radical absorbance capacity) in all genotypes. Cell culture-based antioxidant activity assay (cellular antioxidant activity) showed an increase of activity in the coloured genotypes after roasting. Faba bean extracts demonstrated cellular protection ability against H2O2-induced DNA damage (assessed using RAW264.7 cells), and inhibited the proliferation of all human cancer cell lines (BL13, AGS, Hep G2 and HT-29) evaluated. However, the effect of faba bean extracts on the non-transformed human cells (CCD-18Co) was negligible. Flow cytometric analyses showed that faba bean extracts successfully induced apoptosis of HL-60 (acute promyelocytic leukaemia) cells. The faba bean extracts also exhibited ACE, α-glucosidase and pancreatic lipase inhibitory activities. Overall, extracts from Nura (buff-coloured) and Rossa (red-coloured) were comparable, while TF(Ic*As)*483/13 (white-coloured) contained the lowest phenolic content and exhibited the least antioxidant and enzyme inhibition activities. These results are important to promote the utilisation of faba beans in human diets for various health benefits.

scholarly journals Inhibitory Activities of Polyphenolic Extracts of Bangladeshi Vegetables against α-Amylase, α-Glucosidase, Pancreatic Lipase, Renin, and Angiotensin-Converting Enzyme

Foods ◽  
2020 ◽  
Vol 9 (7) ◽  
pp. 844
Author(s):  
Razia Sultana ◽  
Adeola M. Alashi ◽  
Khaleda Islam ◽  
Md Saifullah ◽  
C. Emdad Haque ◽  
...  
Keyword(s):  
Angiotensin Converting Enzyme ◽  
Pancreatic Lipase ◽  
Lipase Activity ◽  
Inhibitory Activity ◽  
The Other ◽  
Converting Enzyme ◽  
Inhibitory Activities ◽  
Ash Gourd ◽  
Better Than

The aim of the study was to determine the in vitro enzyme inhibition activities of aqueous polyphenolic extracts of nine popular Bangladeshi vegetables, namely ash gourd, bitter gourd, brinjal, Indian spinach, kangkong, okra, ridge gourd, snake gourd, and stem amaranth. Polyphenolic glycosides were the major compounds present in the extracts. Inhibition of α-amylase (up to 100% at 1 mg/mL) was stronger than α-glucosidase inhibition (up to 70.78% at 10 mg/mL). The Indian spinach extract was the strongest inhibitor of pancreatic lipase activity (IC50 = 276.77 µg/mL), which was significantly better than that of orlistat (381.16 µg/mL), a drug. Ash gourd (76.51%), brinjal (72.48%), and snake gourd (66.82%) extracts were the most effective inhibitors of angiotensin-converting enzyme (ACE), an enzyme whose excessive activities have been associated with hypertension. Brinjal also had a significantly higher renin-inhibitory activity than the other vegetable extracts. We conclude that the vegetable extracts may have the ability to reduce enzyme activities that have been associated with hyperglycemia, hyperlipidemia, and hypertension.

scholarly journals ANTIHYPERTENSIVE EFFECT OF RUTIN: PHARMACOLOGICAL AND COMPUTATIONAL APPROACH

2019 ◽  
pp. 87-92
Author(s):  
GANGA RAJU M ◽  
PREM PRASAD GOUD ◽  
SUVARCHALA REDDY NVL
Keyword(s):  
Antioxidant Activity ◽  
Angiotensin Converting Enzyme ◽  
Binding Affinity ◽  
Antihypertensive Effect ◽  
Antihypertensive Activity ◽  
Angiotensin Converting Enzyme Inhibition ◽  
Converting Enzyme ◽  
Vitro Assay

Objective: Phenolic compounds, such as flavonoids, have aroused great scientific interest due to their diverse pharmacological activities. Several studies suggested that flavonoids act as antihypertensive by inhibiting angiotensin-converting enzyme (ACE). In the present study, rutin, which is a citrus flavonoid, was evaluated for its antihypertensive activity using in vivo and in vitro models. Rutin was screened for in vitro assay procedures such as diphenylpicrylhydrazyl and nitroblue tetrazolium (NBT) for its antioxidant activity. Methods: Its antihypertensive effect was investigated in Nω-Nitro-l-arginine methyl ester hydrochloride-induced hypertensive rats, and various parameters such as blood pressure and heart rate were measured; in vitro ACE inhibitory activity was carried out against ACE, aiming at a better understanding of the interaction of this flavonoid with the enzyme. To understand its binding affinity with the angiotensin-converting enzyme, molecular docking studies were carried out using ligand fit of Maestro 9.1 (Schrodinger Software Inc.). An in silico study of rutin was performed for the prediction of Absorption, distribution, metabolism and elimination (ADME) by utilizing a web-based program (www.swissadme.ch). This software computes physicochemical descriptors as well as predicts pharmacokinetic properties and drug-like nature of one or multiple small molecules (blood–brain barrier, cytochromes P450, and P-glycoproteins). Results: Rutin at different dose levels of 200 and 400 mg/kg was tested, and the results have shown its antihypertensive, hypotensive, and negative chronotropic effects. Its antihypertensive activity might be mediated through angiotensin-converting enzyme inhibition (half maximal inhibitory concentration=66.01 μg/mL). In vitro studies also revealed the antioxidant activity of rutin, thus playing a major role in reducing oxidative stress associated with hypertension. The rutin showed optimum binding affinity with a molecular target (angiotensin-converting-enzyme) with the binding energy of −9.0 kcal/mol as compared to the standard (−6.3 kcal/mol). These results indicated that rutin is one of the potential ligands to treat hypertension. ADME results revealed the three violations of rutin (such as molecular mass, hydrogen donor, and acceptors) of five, and the standard captopril has got zero violations which clearly indicated the probability for its higher oral bioavailability. Conclusion: From the above, it is concluded that rutin possesses antioxidant and antihypertensive activities.

ASSOCIATION OF BDKRB2 AND ACE GENE POLYMORPHISM WITH ERYTHROCYTE ADRENOREACTIVITY IN YOUNG MEN WITH DIFFERENT MOTOR ACTIVITY

2020 ◽  
pp. 96-107
Author(s):  
A.Z. Dautova ◽  
E.A. Khazhieva ◽  
V.G. Shamratova ◽  
L.Z. Sadykova
Keyword(s):  
Gene Polymorphism ◽  
Angiotensin Converting Enzyme ◽  
Motor Activity ◽  
Receptor Gene ◽  
Young Men ◽  
Converting Enzyme ◽  
Ace Gene ◽  
Ace Gene Polymorphism ◽  
Physically Inactive

The aim of the paper was to study the association of polymorphic variants of rs4646994 (I/D) of the angiotensin converting enzyme gene (ACE) and rs5810761 (+9/-9) of the bradykinin B2 receptor gene (BDKRB2) with erythrocyte adrenoreactivity (ARE) in athletes and untrained young men. Materials and Methods. The study involved 61 young men (aged 21–23) with different levels of motor activity (MA). ARE was evaluated according to the erythrocyte sedimentation rate (ESR) change under adrenaline in vitro at final concentrations 10-5, 10-6, 10-7, 10-9, 10-11, 10-13 g/ml of venous blood. According to the effect observed and ESR shifts under adrenaline, we distinguished 3 ARE types: antiaggregative (AnAg), areactive (Ar) and aggregative (Ar). Results. The results of comparative and correlation analyses demonstrated that young athletes with +9/-9 (BDKRB2) genotype were characterized by a higher aggregative resistance of erythrocytes to the effects of both physiological (<10-9 g/ml) (physiological adrenaline concentration, PAC) and stressful doses (>10-9 g/ml) of adrenaline (stress adrenaline concentration, SAC), as well as by predominance of AnAg and Ar ARE types. In athletes, among the representatives of different genotypes of АСЕ gene I/D polymorphism, the erythrocyte response to adrenaline did not have any statistically significant differences. In physically inactive students, namely individuals with the D/D genotype, maximal ESR deviation under PAC was less than in those with I/D genotype. Conclusion. Athletes with *-9 allele (+9/-9 genotype) in their genotype can be considered more stress-resistant, which is provided by optimal adaptive and compensatory body mechanisms. Apparently, resistance of cells to the adrenaline contributes much to the work of these mechanisms. As for the ACE gene polymorphism, its effect on the suspension characteristics of erythrocytes is less pronounced not only in physically inactive young men, but in athletes as well. Keywords: erythrocyte adrenoreactivity (ARE), stress tolerance, β2 bradykinin receptor gene (BDKRB2), angiotensin converting enzyme (ACE) gene, motor activity. Цель работы – изучить ассоциацию полиморфных вариантов rs4646994 (I/D) гена ангиотензинпревращающего фермента (АСЕ) и rs5810761 (+9/-9) гена рецептора брадикинина 2 типа (BDKRB2) с адренореактивностью эритроцитов (АРЭ) у спортсменов и юношей, ведущих физически малоактивный образ жизни. Материалы и методы. В исследовании принял участие 61 юноша с разным уровнем двигательной активности (ДА) в возрасте 21–23 лет. Оценку АРЭ проводили по изменению скорости оседания эритроцитов (СОЭ) под действием адреналина in vitro в конечных концентрациях 10-5, 10-6, 10-7, 10-8, 10-9, 10-11, 10-13 г/мл венозной крови. По характеру наблюдаемого эффекта в соответствии с направленностью сдвигов СОЭ в присутствии адреналина мы выделили 3 типа АРЭ: антиагрегационный (АнАг), ареактивный (Ар) и агрегационный (Аг). Результаты. По результатам сравнительного и корреляционного анализа установлено, что юноши-спортсмены с генотипом +9/-9 (BDKRB2) характеризуются более высокой агрегативной устойчивостью эритроцитов к воздействию как физиологических (10-9 г/мл и ниже), так и повышенных (стрессовых) доз (выше 10-8 г/мл крови) адреналина, а также преобладанием АнАг- и Ар-типов АРЭ. У представителей разных генотипов полиморфизма I/D гена АСЕ реакция эритроцитов на адреналин не имела статистически значимых различий в группе спортсменов, тогда как в группе малоактивных студентов у лиц с генотипом D/D максимальное отклонение СОЭ при ФКА было меньше, чем при генотипе I/D. Выводы. Спортсменов, имеющих в своём генотипе аллель *-9 (+9/-9 генотип), можно считать более стрессоустойчивыми, что обеспечивается оптимальными адаптивно-компенсаторными механизмами организма, существенная роль в обеспечении которых, по-видимому, принадлежит устойчивости клеток к действию адреналина. Что касается полиморфизма гена АСЕ, то его влияние на суспензионные характеристики эритроцитов выражено слабее не только у физически малоактивных юношей, но и у спортсменов. Ключевые слова: адренореактивность эритроцитов (АРЭ), стрессоустойчивость, ген рецептора брадикинина β2 (BDKRB2), ген ангиотензинпревращающего фермента (АСЕ), двигательная активность.

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