scholarly journals Discovery of Some Emerging Free Radical Scavenging Candidates Bearing 2-(P-hydroxyphenyl)-4–(Substitutedphenyl)-1H-1,5–Benzodiazepines Pharmacophore

Author(s):  
Animeshchandra G. M. Haldar ◽  
Santosh S. Chhajed ◽  
Debarshi Kar Mahapatra ◽  
Debarshi Kar Mahapatra

In the present investigation, the synthesis of few novel leads bearing 2-(p-hydroxyphenyl)-4–(substitutedphenyl)-1H-1,5–benzodiazepine pharmacophore is described. The substituted chalcone and their derivatives 3(a-j) were synthesized by base catalyzed Claisen-Schmidt condensation between p-hydroxy-acetophenone and appropriate aldehydes. The dibromostyryl ketones 4(a-j) were obtained by the reaction the chalcone with bromine in acetic acid. The dibromostyryl ketone were reacted with methanol in presence of sodium methoxide followed by acidic hydrolysis give 1-(4-hydroxyphenyl)-3-(substitutedphenyl)-1,3-propanediones. The targeted compounds; the substituted 1,5-benzodiazepines were synthesized with o-phenylenediamine and synthesized 1,3-propanediones. The structures of synthesized compounds were confirmed by spectroscopic and analytical techniques (IR, 1H-NMR, and MS). The free radical scavenging activity of the synthesized analogs was monitored by in vitro antioxidant activity protocol. The derivatives 6f, 6g, 6i, and 6j were found to exhibit good antioxidant activity with 59.07%, 41.33%, 68.3% and 60.4% scavenging activity respectively as compared to standard ascorbic acid which demonstrated 79.73% activity. The current research revealed the potential of 2-(p-hydroxyphenyl)-4–(substituted-phenyl)-1H-1,5–benzodiazepine as emerging free radical scavengers. The study helped to establish a structure-activity relationship (SAR) where the substitution on the phenyl moiety of the 1,5-benzodiazepine was found to play profound role and influence over biological activity. The research will open new avenues for the development of antioxidant moieties having perspectives in cancer, inflammation, and several other ailments.

2017 ◽  
Vol 9 (4) ◽  
pp. 615
Author(s):  
Mukesh Kumar Yadav ◽  
Santosh Kumar Singh ◽  
JS Tripathi ◽  
YB Tripathi

<p><em>Centella asiatica</em> also known as <em>mandukparni </em>or Indian pennywort or <em>jalbrahmi</em>, which has been used as a medicine in the Ayurveda from ancient times and mentioned in many classical texts of Ayurveda. <em>Centella asiatica</em> has long been used to improve memory and cognitive function.</p><p>The study aimed to identify the phytochemicals present in different solvent extracts of <em>Centella asiatica </em>(i.e. PECA- Petroleum ether extract of <em>C. asiatica, </em>CCA- Chloroform extract of <em>C. asiatica, </em>EACA- Ethyl acetate extract of <em>C. asiatica,</em> ECA- Ethanolic extract of <em>C. asiatica, </em>HACA- Hydro-alcoholic extract of <em>C. asiatica</em>)<em> </em>and evaluate the respective in-vitro antioxidant potentials. <em></em></p><p>The phytochemical screening of extracts was done with standardized procedures and the antioxidant potential of different solvent extracts of <em>Centella asiatica</em> was assessed by its free radical scavenging activity 2, 2-diphenyl -1- picrylhydrazyl (DPPH) as well as hydrogen peroxide scavenging assay respectively for reducing capability.</p><p>In all different solvent extracts of <em>C. asiatica</em> revealed excellent free radical scavenging activity as revealed by 2-2- diphenyl-1-picryl-hydrazyl (DPPH) assay with  EC<sub>50</sub> values for ECA=128.752±1.85 μg/ml, HACA=274.884±1.21 μg/ml and hydrogen peroxide assay against the standard (Butylated hydroxytoluene) BHT, with the EC<sub>50</sub> values ECA=429.69±0.92 μg/ml HACA=458.08±0.58 μg/ml while rest solvent extracts shown very less antioxidant activity.</p><p> The present study indicates that the <em>Centella asiatica</em> extracts have good antioxidant activity which can be used in stress and anxiety and also a good source to be used as natural drugs.</p>


Author(s):  
Vinay M. ◽  
Seethalakshmi S. ◽  
Vijay Kumar

Background: Ormeloxifene (Centchroman) is a Selective Estrogen Receptor Modulator (SERM) which acts as estrogen antagonist and having anti progestogenic activity also. It is being used in the management of dysfunctional uterine bleeding and as nonhormonal oral contraceptive. It is also being investigated for the indications such as osteoporosis, breast and endometrial carcinoma. In this study, we have evaluated the Antioxidant potential of drug by using DPPH and NO synthase Assay. It was found that ormeloxifene has significant antioxidant activity which could be cause for its use in various gynaecological and other conditions.Methods: In this study, we have demonstrated in vitro antioxidant activity of ormeloxifene. DPPH and NO synthase assay tests were done for different concentrations of ormeloxifene.Results: In our study, it showed that the free radical scavenging activity of ormeloxifene was less in lower concentration and increased in the higher concentration in DPPH assay. The free radical scavenging activity of drug ormeloxifene was 22% at 100µg/ml and 27% for the concentrations of 1000µg/ml in DPPH assay. No scavenging activity was 3% at 100µg/ml and 11% at 1000µg/ml.Conclusions: The invitro antioxidant analysis of ormeloxifene, was proved to be a potent antioxidant.


INDIAN DRUGS ◽  
2020 ◽  
Vol 57 (05) ◽  
pp. 74-79
Author(s):  
A. K Srivastava ◽  
D. Kaushik ◽  
V. K. Lal

Free radicals are reactive molecules involved in many physiological processes and have been associated with many diseases, such as ageing, cancer, arthritis and liver injury and cardiac complications. In polyherbal formulations HAF-I and HAF-II, described below, the total phenolics content were found to be 34.4±0.10 and 27.6±1.20 mg gallic acid equivalent (GAE)/g and total flavonoids contents, total tannin contents were 24.7±0.25 and 18.1±1.20 RE/g and 12.31±0.25 and 9.48±1.85 GAE/g, respectively. Free radical scavenging activity was determined according to the elimination of DPPH radicals. Total phenol content was determined by the Folin–Ciocalteu reaction. The relative antioxidant ability of the polyherbal formulations were investigated through two in vitro models, namely, antioxidant capacity by radical scavenging activity using α, α-diphenyl-β-picrylhydrazyl (DPPH) and nitric oxide (NO) methods. The extracts were used at 20, 40, 60, 80 and 100 μg/mL concentrations and radical scavenging activity was determined in terms of inhibition percentage. The IC50 (concentration required for 50% inhibition) were calculated for each radical. The present study was designed to evaluate the free radical scavenging activity of hydro-alcoholic extracts of polyherbal formulations (HAF-I & HAF-II) various in-vitro models using ascorbic acid and rutin as references. The in vitro free radical DPPH activities were found to be 74.17±0.18 & 75.30±0.18 and NO antioxidant activity were found to be 75.3±1.10 & 76.17±1.24 at maximum concentration of 100 μg/mL. The in-vitro anti-oxidant activity of these polyherbal formulations may be due to the presence of polyphenols.


INDIAN DRUGS ◽  
2018 ◽  
Vol 55 (06) ◽  
pp. 56-62
Author(s):  
A. K Srivastava ◽  
◽  
D. Kaushik ◽  
V. K. Lal ◽  

Free radicals are reactive molecules involved in many physiological processes and have been associated with many diseases, such as ageing, cancer, arthritis and liver injury and cardiac complications. The total phenolics content were found to be 34.4±0.10 and 27.6±1.20 mg gallic acid equivalent (GAE)/g and total flavonoids contents, total tannin contents were 24.7±0.25 & 18.1±1.20 RE/g and 12.31±0.25 & 9.48±1.85 GAE/g, respectively of polyherbal formulations (HAF-I & HAF-II). Free radical scavenging activity was determined according to the elimination of DPPH radicals and total phenol content was determined by the Folin–Ciocalteu reaction. The relative antioxidant ability of the polyherbal formulations were investigated through two in vitro models, such as antioxidant capacity by radical scavenging activity using, α, α-diphenyl-β-picrylhydrazyl (DPPH) and nitric oxide (NO) methods. The extracts were used at concentration 20, 40, 60, 80 and 100 μg/mL concentrations and radical scavenging activity was determined in terms of inhibition percentage. The IC50 (concentration required for 50% inhibition) were calculated for each radicals. The present study was designed to evaluate the free radical scavenging activity of hydro-alcoholic extracts of polyherbal formulations (HAF-I & HAF-II) various in vitro models using Ascorbic acid and Rutin as a reference. The In vitro free radical DPPH activities were found to 74.17±0.18 & 75.30±0.18 and NO antioxidant activity were found to 75.3±1.10 & 76.17±1.24 at maximum concentration of 100 μg/mL. The In vitro anti-oxidant activity of these polyherbal formulations may be due to the presence of polyphenols.


2019 ◽  
Vol 4 (1) ◽  
pp. 1
Author(s):  
Husni Mubarok ◽  
Komang Ayu Nocianitri ◽  
I Dewa Gede Mayun Permana

Probiotik merupakan organisme hidup yang mampu memberikan efek yang menguntungkan bagi kesehatan inangnya. Lactobacillus rhamnosus yang diisolasi dari feses bayi sehat merupakan bakteri asam laktat (BAL) yang diketahui memiliki potensi sebagai probiotik. Tujuan dari penelitian ini adalah untuk mengetahui aktivitas antioksidan dari isolat L. rhamnosus FBB secara in vitro. Isolat L. rhamnosus FBB tersebut antara lain:  L. rhamnosus FBB nomor 21, 26, 52, 59, 75, dan 81. Uji konfirmasi menunjukkan bahwa keseluruhan isolat L. rhamnosus FBB termasuk bakteri homofermentatif, bakteri gram positif, katalase negatif dan memiliki bentuk morfologi batang berantai. Aktivitas antioksidan ditentukan dengan mengukur kemampuan penangkapan radikal bebas 1,1-diphenyl-2-picrylhydrazil (DPPH) dengan membandingkan subjek penelitian yakni supernatant, intact cell dan cell lysate. Hasil penelitian menunjukkan bahwa penangkapan radikal bebas pada supernatant, intact cell dan cell lysate masing-masing adalah 39,00-66,71%, 15,76-21,28% dan 4,79-10,86%. L. rhamnosus FBB 75 dan L. rhamnosus FBB 81 menunjukkan aktivitas antioksidan tertinggi dibandingkan dengan isolat lainnya. Aktivitas penangkapan  radikal bebas DPPH pada supernatant, intact cell dan cell lysate pada  L. rhamnosus FBB 75 adalah  66,71%, 15,76%, 10,86% dan aktivitas  antioksidan pada L. rhamnosus FBB 81 adalah 66,43%, 21,28% 9,37%. Hasil penelitian ini membuktikan bahwa L. rhamnosus FBB 75 dan L. rhamnosus FBB 81 merupakan strain yang potensial untuk dikembangkan sebagai probiotik antioksidan.   Probiotics are living organisms that can have a beneficial effect on the health of their hosts. Lactobacillus rhamnosus isolated from healthy infant feces is lactic acid bacteria (BAL) that has potential as a probiotic. The purpose of this study was to determine the antioxidant activity of L. rhamnosus FBB bacterial isolates in vitro. Isolates of L. rhamnosus FBB bacteria are: L. rhamnosus FBB number 21, 26, 52, 59, 75, and 81. From the confirmatory test, the overall isolates of L. rhamnosus FBB included homofermentative bacteria, gram-positive bacteria, negative catalase and morphological form of chain stems. Antioxidant activity was determined by measuring the capability of scavenging free radical 1,1-diphenyl-2-picrylhydrazil (DPPH) with comparison of research subjects with supernatant, intact  cell and cell  lysate. The results showed that free radical scavenging activity on supernatant, intact  cell and cell  lysate were 39,00-66,71%, 15,76 - 21,28% and 4,79 - 10,86% respectively. L. rhamnosus FBB 75 and L. rhamnosus FBB 81 showed higher antioxidant activity than other isolates. DPPH free radical scavenging activity on the supernatant, intact cell and cell  lysate in L. rhamnosus FBB 75 was 66,71%, 15,76%, 10,86% and antioxidant activity in L. rhamnosus FBB 81 was 66,43%, 21,28% , 9,37%. The results of this study prove that L. rhamnosus FBB 75 and L. rhamnosus FBB 81 are potential strains to be developed as antioxidant probiotics.


Author(s):  
Khetbadei Lysinia Hynniewta Hadem ◽  
Arnab Sen

Objective: Study of antioxidant activity of a crude aqueous-methanol extract of Aristolochia tagala and its fractions and identification of the compounds with antioxidant activity.Methods: The antioxidant activity was assayed by the ability to scavenge free radicals such as superoxide, nitric oxide and ABTS radical cation and the identification of compounds was carried out by LC/MS analysis.Results: Fraction I of Aristolochia tagala showed the highest free radical scavenging activity and compounds responsible for its activity were identified as magnoflorine, apigenin dimethyl ether, aristolone, and N-trans-feruloyldopamine.Conclusion: The free radical scavenging property of the compounds present in Aristolochia tagala may be one mechanism that contributed to medicinal property exhibited by this plant.


2021 ◽  
Vol 8 (1) ◽  
pp. 69-72
Author(s):  
Betty T ◽  
Sumathi P ◽  
Indhumathi T ◽  
Prabavathi B ◽  
Devadharshini B

The aim of present study was to investigate the in vitro antioxidant potential and total extractive yield of Mussaenda luteola Delile leaves. Antioxidant activity was assessed by using 2,2- diphenyl-1-picryl-hydrazyl (DPPH• ) assay, reducing power activity and [2,2’-azino-bis (3-ethylbenzthiazoline-6-sulphonic acid)] ABTS•+ assay. Here ascorbic acid (ASA) and rutin were used as standard antioxidants. The results of the study indicates that the chloroform extracts of the leaf of Mussaenda luteola possesses significant scavenging activity against DPPH• (17.56) and reducing power activity (0.759) at 700nm absorbance. The ethanolic leaf extracts holds high free radical scavenging activity (ABTS•+) at 735nm (94.59). The free radical scavenging and antioxidant activities may be attributed to the presence of adequate phenolic and flavonoid compounds. The ethanolic leaf extract of M. luteola yields maximum extractive yield percentage (37.08%). This study revealed that the leaf extracts of Mussaenda luteola has demonstrated significant antioxidant activity.


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