Curcumin-based antioxidant and glycohydrolase inhibitor compounds: Synthesis and in vitro appraisal of the dual activity against diabetes

2020 ◽  
Vol 16 ◽  
Author(s):  
Sajjad Esmaeili ◽  
Nazanin Ghobadi ◽  
Donya Nazari ◽  
Alireza Pourhossein ◽  
Hassan Rasouli ◽  
...  

Background: Curcumin, as the substantial constituent of the turmeric plant (Curcuma longa), plays a significant role in the prevention of various diseases, including diabetes. It possesses ideal structure features as enzyme inhibitor, including a flexible backbone, hydrophobic nature, and several available hydrogen bond (H-bond) donors and acceptors. Objective: The present study aimed at synthesizing several novel curcumin derivatives and further evaluation of these compounds for possible antioxidant and anti-diabetic properties along with inhibitory effect against two carbohydrate-hydrolyzing enzymes, α-amylase and α-glucosidase, as these enzymes are therapeutic targets for attenuation of postprandial hyperglycemia. Methods: Therefore, curcumin-based pyrido[2,3-d]pyrimidine derivatives were synthesized and identified using an instrumental technique like NMR spectroscopy and then screened for antioxidant and enzyme inhibitory potential. Total antioxidant activity, reducing power assay and 1,1-diphenyl-2-picrylhydrazyl (DPPH• ) radical scavenging activity were done to appraisal the antioxidant potential of these compounds in vitro. Results: Compounds L6-L9 showed higher antioxidant activity while L4, L9, L12 and especially L8 exhibited the best selectivity index (lowest α-amylase/α-glucosidase inhibition ratio). Conclusion: These antioxidant inhibitors may be potential anti-diabetic drugs, not only to reduce glycemic index but also to limit the activity of the major reactive oxygen species (ROS) producing pathways.

2020 ◽  
Vol 11 (4) ◽  
pp. 6262-6267
Author(s):  
Krishnamoorthy Meenakumari ◽  
Giridharan Bupesh ◽  
Mayur Mausoom Phukan

The foods from plants were known to ensure against degenerative diseases and maturing because of their antioxidant activitycredited to their high content. Information on antioxidant activity of Indian medicinal plant is abundant. To the best of our knowledge, biological properties have not been accounted in the literature for this species of . As a point, this is the first results to assess the anti-oxidant activity of the plant which belongs to the family . The antioxidant activity of Methanol, , Ethyl acetate and Aqueous extracts of E. was determined using the DPPH free radical scavenging activity, ABTS radical scavenging activity and reducing power assay. The DPPH scavenging activity showed higher activity observed in extract (63%) of E. than (54%), (44%) and aqueous (30%). the ABTS assay inhibition in extract (58%) than (43%), (38%) and aqueous (32%) extracts. The reducing power assay of different extracts was increased in extract (54%) than (40%), (34%) and aqueous (28%) extracts. Overall, the and ethyl acetate extract had higher antioxidant properties than other extract. However, in this study, extracts exhibit great potential for antioxidant activity and may be useful for their nutritional and medicinal functions.


2011 ◽  
Vol 183-185 ◽  
pp. 565-569 ◽  
Author(s):  
Jian Ren ◽  
Zhen Yu Wang

The total anthocyanin content (TAC) of pigment extracted from fruits of Padus racemosa and Padus virginiana was determined by pH-differential method. TAC in pigment from fruits of Padus racemosa was higher than that in Padus virginiana. The vitro antioxidant activity of the two kinds of pigment was evaluated by different assays, including DPPH• assay, ABTS•+assay, OH• assay and reducing power assay. The results showed that except for reducing power, pigment from fruit of Padus racemosa showed stronger ABTS•+, DPPH• and OH• radical scavenging activity than pigment from fruit of Padus virginiana. The study concluded that pigment extracted from fruit of Padus racemosa and Padus virginiana can be used as a source of natural antioxidants instead of synthetic antioxidants.


2015 ◽  
Vol 15 (1) ◽  
pp. 43 ◽  
Author(s):  
Mosmi Medpilwar ◽  
Darshil Maru ◽  
Meenakshi Upadhyay ◽  
Neha Lavania ◽  
Madhavi Vernekar ◽  
...  

The aim of our present study was to evaluate the antioxidant and anti-lipid peroxidation activity of ethanolic extracts of <em>Bougainvillea species viz B. shubhra, B. peruviana and B. bhuttiana</em> golden glow. Phytochemical constituents viz. total phenolics, flavonoids and tannins were assayed using standard protocol. The antioxidant activity was studied by DPPH assay, FRAP assay, reducing power assay and in-vitro inhibition of lipid peroxidation. Of the three species, <em>B. bhuttiana</em> golden glow showed highest amount of phenols (6.78±0.001), flavonoids (27.7±0.012) and tannin (11.08±0.008) contents. It also showed highest antioxidant activity of 15.15± 0.008 and 8.08± 0.018 as determined by FRAP assay and reducing power assay respectively. The percent DPPH radical scavenging activity was 82.72% and in-vitro inhibition of lipid peroxidation in mitochondrial membrane was also found to be highest in <em>B. bhuttiana</em> golden glow.


INDIAN DRUGS ◽  
2021 ◽  
Vol 58 (10) ◽  
pp. 34-41
Author(s):  
Kanthlal S. K. ◽  
Jipnomon Joseph ◽  
Bindhu P. Paul ◽  
Vijayakumar M ◽  
Rema Shree A. B. ◽  
...  

Amomum subulatum, commonly known as large or black cardamom, is a commonly used spice in Indian kitchens and is traditionally used to treat various ailments. To add more knowledge about the medicinal values of the fruit, this study was conducted to evaluate the in vitro antioxidant activities of aqueous, methanol, ethanol, hydro alcohol, ethyl acetate, acetone and chloroform extracts of the fruit. Preliminary assessment was done to detect the presence of phytoconstituents using identification tests. The antioxidant activity was measured by employing methods such as diphenylpicrylhydrazyl (DPPH) radical scavenging assay, total antioxidant activity equivalent to ascorbic acid, reducing power assay and superoxide anion scavenging assay. The antioxidant activities were compared with their respective phenol and flavonoid contents. Preliminary assessment revealed that large cardamom fruit is a good source of all the bioactive constituents as well as phenol and flavonoid essential for medicinal values. The extract obtained by polar solvents showed the highest antioxidant efficacy in relation to its phenol content. Also, all the solvent-soluble fractions showed a concentration-dependent antioxidant effect. Results from our study prove that large cardamom can alleviate oxidative stress, suggesting the potential of large cardamom as a functional food


2008 ◽  
Vol 5 (s2) ◽  
pp. 1123-1132 ◽  
Author(s):  
H. Vijay Kumar ◽  
C. R. Gnanendra ◽  
Nagaraja Naik ◽  
D. Channe Gowda

Dibenz[b,f]azepine and its five derivatives bearing different functional groups were synthesized by known methods. The compounds thus synthesized were evaluated for antioxidant potential through different in vitro models such as (DPPH) free radical scavenging activity,ß-carotene-linoleic acid model system, reducing power assay and phosphomolybdenum method. Under our experimental condition among the synthesized compounds dibenz[b,f]azepine (a) and 10-methoxy-5H-dibenz[b,f]azepine (d) exhibited potent antioxidant activity in concentration dependent manner in all the above four methods. Butylated hydroxyl anisole (BHA) and ascorbic acid (AA) were used as the reference antioxidant compounds. The most active compounds like dibenz[b,f]azepine and its methoxy group substituent have shown more promising antioxidant and radical scavengers compared to the standards like BHA and ascorbic acid. It is conceivable from the studies that the tricyclic amines,i.e. dibenz[b, f]azepine and some of its derivatives are effective in their antioxidant activity properties.


2019 ◽  
Vol 2019 ◽  
pp. 1-7 ◽  
Author(s):  
Terence Nguema Ongone ◽  
Redouane Achour ◽  
Mostafa El Ghoul ◽  
Latyfa El Ouasif ◽  
Meryem El Jemli ◽  
...  

The aim of this work is to deepen the pharmacological effect of 4-phenyl-1,5-benzodiazepin-2-one derivatives which have a similar structure to nonionic surfactants: 4-phenyl-1,5-benzodiazepin-2-one is the hydrophilic head, and the carbon chain is hydrophobic tail. The antinociceptive activity of 4-phenyl-1,5-benzodiazepin-2-one derivatives was determined using acetic acid-induced writhing and tail immersion tests. In addition, the in vitro antioxidant activities of the tested derivatives were determined by using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging method and ferric reducing power assay. A single oral administration of these compounds at the doses of 50 and 100 mg/kg significantly reduced the number of abdominal writhes induced by acetic acid injection. Acute pretreatment with 4-phenyl-1,5-benzodiazepin-2-one derivatives at the dose of 100 mg/kg caused a significant increase in the tail withdrawal latency in the tail immersion test. Additionally, a significant scavenging activity in DPPH and reducing power was observed in testing antioxidant assays. Finally, we carried out a study of the antioxidant activity of these derivatives. The results of this study reveal that these compounds have a low antioxidant activity compared to the BHT. It decreases with the polarity of the molecule. The present study suggests that 4-phenyl-1,5-benzodiazepin-2-one derivatives possess potent antinociceptive and antioxidant effects, which suggest that the tested compounds may be useful in the treatment of pain and oxidation disorders.


2006 ◽  
Vol 1 (5) ◽  
pp. 1934578X0600100 ◽  
Author(s):  
Lindy L. Esterhuizen ◽  
Riaan Meyer ◽  
Ian A. Dubery

Coleonema album, a member of the South African ‘Fynbos’ biome, was evaluated for its antioxidant and free radical scavenging activity. Ethanol- and acetone-based extracts from plant material obtained from two different geographical areas were analysed. A bioassay-guided fractionation methodology was followed for screening of active compounds. The 1,1-diphenyl-2-picrylhydrazyl (DPPH)-TLC method revealed the presence of a number of antioxidants which were quantified by the DPPH-spectrophotometric assay and the oxygen radical absorbance capacity (ORAC) assay. The C. album extracts possessed significant in vitro antioxidant activity, a large portion of which appeared to be contributed by the phenolic compounds. In contrast, the reducing power of the extracts could not be correlated with the observed antioxidant activity. Identification and structural information of the active components were obtained by a combination of preparative TLC and LC-MS which revealed the presence of coumarin aglycones and glycosides. The results of this study indicate that C. album contains strong antioxidants that warrant further investigation into the relationship between the structure and activity of the active coumarin metabolites.


Author(s):  
Rajendran Raja Priya ◽  
N. Bhadusha ◽  
Veramuthu Manivannan ◽  
Thanthoni Gunasekaran

Objective: To evaluate the preliminary phytochemical content and antioxidant potential of the hydroalcoholic leaf extracts of Hemionitis arifolia. Methods: Total phenolic, flavonoid and alkaloid contents were evaluated using spectrophotometric methods. The free radical scavenging activity of the leaf hydroalcoholic extract were evaluated against DPPH+, ABTS+, Reducing power assay and nitric oxide assay were determined. Results: The hydroalcoholic concentrate of H. arifolia uncovered the most elevated polyphenol content when contrasted and the other phytoconstituents. Absolute phenol content of the hydroalcoholic separate was observed to be 31.78%, flavonoid content is 1.02% and Alkaloid content is 30.40% individually. The Solvent concentrates showed huge cell reinforcement movement, with hydroalcoholic extract. ABTS Assay, DPPH assay, Reducing power assay and Nitric oxide assay where the Inhibition concentration were 667.75µg/ml, 734.25 µg/ml, 791.58 µg/ml and 899.67 µg/ml. Conclusion: This study suggests that hydroalcoholic leaf extracts of H. arifolia could be a potential source of natural antioxidant and justifies its use in ethno-medicine.


2017 ◽  
Vol 12 (4) ◽  
pp. 1934578X1701200 ◽  
Author(s):  
Ryszard Amarowicz ◽  
Magdalena Karamać ◽  
Montserrat Dueñas ◽  
Ronald B. Pegg

The activities of the crude acetonic extract of red bean and its two fractions were determined using a β-carotene-linoleate model system as well as the total antioxidant activity (TAA), the total phenolics content (TPC), the DPPH radical-scavenging activity, and the reducing power assays. Results from the in vitro assays showed the highest values when tannins (fraction II) were tested. Specifically, the TAA of the tannins fraction was 4.37 mmol Trolox eq./g fraction; whereas, the crude extract and fraction I were 0.481 and 0.093 μmol Trolox eq./mg extract or fraction, respectively. The content of total phenolics in fraction II was the utmost (612 mg/g); the tannins content, assayed by the vanillin method and expressed as absorbance units at 500 nm per 1 g, was 938. RP-HPLC-PAD-MS profiling revealed the presence of 33 compounds: quercetin arabinoglucoside, quercetin rutinoside, quercetin, p-hydroxybenzoic acid, and kaempferol rutinoside were the most abundant phenolics in the extract.


2015 ◽  
Vol 2015 ◽  
pp. 1-8 ◽  
Author(s):  
Rabia Kanwal ◽  
Muhammad Arshad ◽  
Yamin Bibi ◽  
Saira Asif ◽  
Sunbal Khalil Chaudhari

Zanthoxylum armatumDC. (syn.Z. alatumRoxb.) is an important medicinal plant commonly called Timur or Indian prickly ash. The ethnopharmacological study ofZ. armatumrevealed the use of different plant parts for curing various ailments including cholera, chest infection, fever, indigestion, stomach disorders, gas problems, piles, toothache, gum problems, dyspepsia, as carminative, antipyretic, aromatic, tonic, and stomachic. Keeping in view the medicinal potential of the plant, the antioxidant activity was evaluated using 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging, reducing power, and phosphomolybdate assay using different concentrations (7.81 μg/mL–250 μg/mL). Ascorbic acid was taken as standard. The results indicated that the free radical scavenging activity ranged from 40.12% to 78.39%, and the reductive potential ranged from 0.265 nm to 1.411 nm while the total antioxidant activity ranged from 0.124 nm to 0.183 nm. The antioxidant potential evaluated by three assays increased in a concentration dependent manner and ascorbic acid showed better antioxidant activity than leaf extract. Results obtained through different tests confirmed redox protective activities ofZanthoxylum armatum. Further in vitro and in vivo research should be performed, so this plant can be further utilized in drug development.


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