Synthesis and Evaluation of bis-Schiff Bases of Carbohydrazide as Antioxidant and Cytotoxic Agents

2021 ◽  
Vol 18 ◽  
Author(s):  
Sarosh Iqbal ◽  
Shumaila Kiran ◽  
Shahida Perveen ◽  
Rizwana Malik ◽  
Muhammad Taha ◽  
...  

Background & Introduction : Antioxidants are known to prevent oxidative stress-induced damage to the biomolecules and thus, delay the onset of cancers and many age-related diseases. Therefore, the development of novel and potent antioxidants is justified. Method: During this study, we synthesized symmetrical bis-Schiff bases of carbohydrazide 1-27, and evaluated their in vitro antioxidative activity and cytotoxic activity. Results: Among synthesized compounds, six compounds 20 (IC50 = 12.89 ± 0.02 µM), 16 (IC50 = 14.32 ± 0.43 µM), 17 (IC50 = 18.52 ± 0.83 µM), 19 (IC50 = 22.84 ± 0.62 µM), 24 (IC50 = 35.1 ± 0.82 µM) and 15 (IC50 = 40.03 ± 1.06 µM) showed an excellent 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity, better than the standard butylatedhydroxyanisole (BHA) (IC50 = 44.6 ± 0.6 µM). Likewise, two compounds 16 (IC50 = 4.3 ± 1.3 µM) and 20 (IC50 = 6.6 ± 1.6 µM) showed oxidative burst scavenging activity better than the standard drug ibuprofen (IC50 = 11.2 ± 1.9 µM). Some synthesized compounds showed good to moderate toxicity against prostate cancer (PC-3) cell lines. Conclusion: This study has identified potent antioxidants and good cytotoxic agents with the potential to further investigate.

INDIAN DRUGS ◽  
2014 ◽  
Vol 51 (10) ◽  
pp. 38-42
Author(s):  
N. K Choudhary ◽  
◽  
J Dwivedi ◽  
S Sharma

The present investigations were carried out to evaluate the in vitro antioxidant as well as antidiabetic activity of flowers of Calotropis gigantea. Different extracts (petroleum ether, chloroform and ethanolic extract) were prepared using successive solvent extraction method (soxhlet) and screened for its in vitro antioxidant activity using Diphenyl picryl hydrazyl (DPPH) radical scavenging activity, ABT S radical cation decolorization assay and nitric oxide (NO) radical scavenging activity and IC50 were calculated. In vitro antidiabetic activity was studied using α – amylase and α – glucosidase inhibitory assay. Chloroform extract, among the three extracts (i.e. petroleum ether, chloroform and ethanolic), showed maximum antioxidant activity with IC50 value of 151.23µg/ml, 73.56 µg/ml and 158.92µg/ml against DPPH radical scavenging activity, ABTS radical cation decolorization assay and nitric oxide (NO) radical scavenging activity respectively. The chloroform extract produced a significant in vitro antidiabetic activity with IC50 of 52.3µg/ml 18.2µg/ml against α – amylase and α – glucosidase enzymes but less inhibitory effect than standard acarbose.


Author(s):  
Md Raihan Sarkar ◽  
Moynul Hasan ◽  
Md Sariful Islam Howlader ◽  
Mohammad Saydur Rahman ◽  
Shubhra Kanti Dey

In the present study, the antioxidant and analgesic potential of the ethanolic extract of the leaves of Derris trifoliata was evaluated. The free radical scavenging activity of the crude extract on the stable radical 1, 1-diphenyl-2-picrylhydrazyl (DPPH) was determined by comparing the DPPH inhibitory capacity of the extract. In the quantitative assay, Derris trifoliata extract displayed a free radical scavenging activity in the DPPH assay (IC50 = 19 ?g/ml) which is comparable to that of ascorbic acid (IC50 = 7.80 ?g/ml), a well-known standard antioxidant. The analgesic responses of the given samples of extracts were evaluated using the Tail immersion method. In the analgesic activity test, extract at dose of 200 mg/kg and 400 mg/kg exhibited significant (P<0.05 and P<0.001 respectively) inhibition of pain by 166.82 and 184.95 after 120 and 180 minutes respectively while the standard drug Diclofenac Na inhibition was found to be 217.67 after 180 minutes at a dose of 25 mg/kg body weight DOI: http://dx.doi.org/10.3329/ijpls.v1i2.12951 International Journal of Pharmaceutical and Life Sciences Vol.1(2) 2012


2011 ◽  
Vol 140 ◽  
pp. 355-359 ◽  
Author(s):  
Yan Qiu ◽  
Jian Jun Song

The Ablmoschus manihot (L.) Medic, an edible hibiscus of the Malvaceae family, is abundant with total flavonoid. The content of total flavonoid from A. manihot flowers (TFA) was extracted by 70% ethanol (ethanol:water, 70:30). The scavenging effects of TFA on superoxide anions and hydrogen radicals were related to the total flavonoid concentrations with the IC50 values of 63.90 ±2.21 μg/mL and 266.88±28.32 μg/mL, respectively. However, the IC50 values of standard ascorbic acid were 436.52 ±14.36 μg/mL and 439.58±21.41 μg/mL, respectively. The DPPH radical scavenging activity increased with increasing of TFA concentrations and the highest inhibition was 94.63 ±3.01% at 50 μg/mL, as compared to ascorbic acid 34.94 ±1.50%. The extract also showed good reducing power. The data from this study suggest A. manihot flower extract has significant potential to use as health supplements and nutraceuticals.


Author(s):  
Abdul Sadat ◽  
Mayukh Hore ◽  
Kaushik Chakraborty ◽  
Subhrajyoti Roy

Objective: The present study was carried out to evaluate the in vitro preliminary phytochemical analysis and antioxidant activity of methanolic leaf extracts of Corchorus olitorius L. The in vitro antioxidant activity was evaluated by DPPH radical scavenging activity method.Methods: Fresh jute leaves (immature, mature and senescence) were collected, air dried and the crude powder was prepared for phytochemical and antioxidant analysis. The powder was mixed with 70% methanol and the supernatant was separated. The antioxidant activity of this methanolic extract was measured on the basis of the scavenging activity of the stable 1, 1-diphenyl 2-picrylhydrazyl (DPPH) free radical with slight modifications. Phytochemical analysis was performed according to standard laboratory protocol.Results: The results indicated the presence of different phytochemicals viz. glycosides, steroids, cholesterol, alkaloids, phenols, flavonoids, riboflavin, saponins and terpenoids. The sample also showed antioxidant activity by inhibiting DPPH radical. The significant antioxidant activity of methanolic leaf extract of might be due to the presence of saponins, phenols, flavonoids and alkaloids found in the preliminary phytochemical analysis.Conclusion: Present study reveals that the jute leaf possesses different phytonutrients and exhibited DPPH radical scavenging activity, and therefore, may be used for therapeutic purposes.


Author(s):  
Padma S Vankar

Nyctanthes arbor-tristis (Harshingar, Parijat) belongs to the family Oleaceae. The flower has white petals with an orange calyx. Nyctanthes stems have been found to be a rich source of antioxidant. The aqueous extracts of the flower, calyx and petals were evaluated and found to be dose-dependent and showed an increase in DPPH free radical scavenging activity in vitro. The extracts, which showed strong DPPH radical scavenging activity, are in the order Calyx > flower > petals. This signifies that the main antioxidant activity is in the orange colored calyx of the flower. We have attempted an innovative study with the Nyctanthes flower as a part of an exploration for a cheap natural source of antioxidants which can be used at the industrial scale of the food industry.


Author(s):  
Pallavi Pal ◽  
Ajeet Singh

Aim: In this study antioxidant and anti-inflammatory effect of ethanolic extract of Quisqualis indica leaves was evaluated. Study Design: In-vitro analysis of Quisqualis indica leaf extract. Place and Duration of Study: Molecular Biology laboratory, Department of Biotechnology, G.B Pant Engineering College, Pauri, between July 2015 and July 2016. Methods: Non-enzymatic and enzymatic assays such as DPPH (1, 1diphenyl-2-picryl hydrazyl), FRAP assay, superoxide dismutase SOD (EC 1.15.1.1), catalase (EC 1.11.1.6), for radical scavenging activity of ethanolic extracts of Quisqualis indica Linn. plant leaves had done. For estimation of anti-inflammatory action, two methods were employed: protein denaturation method and membrane stabilization method. Results: Ethanolic extract of leaves on higher concentration had better antioxidant potential when compared with reference standard ascorbic acid. They exhibited strong antioxidant radical scavenging activity values for ethanolic extract of leaves. Results of anti-inflammatory method suggested better potential values for ethanolic extract and compared with standard drug diclofenac sodium respectively. A significant relationship between antioxidant, anti-inflammatory capacity and total phenolic content was examined, indicating that phenolic compounds are the major contributors for the antioxidant and anti-inflammatory properties of this plant. Conclusion: Ethanolic extract of Q. indica exhibited strong anti-inflammatory and antioxidant activity and this can be used for designing novel drug inhibitors with better efficacy.


Molecules ◽  
2012 ◽  
Vol 17 (12) ◽  
pp. 14882-14898 ◽  
Author(s):  
Francisco Martínez-Martínez ◽  
Rodrigo Razo-Hernández ◽  
Ana Peraza-Campos ◽  
Manuel Villanueva-García ◽  
Maria Sumaya-Martínez ◽  
...  

2020 ◽  
Vol 7 (3) ◽  
pp. 222-229
Author(s):  
Syed Tajudeen Syed Ameen ◽  
Anbalagan Vilvanathan ◽  
Syed Zameer Ahmed Khader ◽  
Gayathri Mahalingam

Background: A series of β-diketone hydrazones have been synthesized via condensation of isoniazid with series of β-diketone. The structures of the Schiff bases are established by elemental and spectroscopic techniques. The prepared compounds were screened for antibacterial and antioxidant potential by DPPH free-radical scavenging activity and Ferric reducing antioxidant power (FRAP) assays. Methods: β-diketone hydrazine derivatives were synthesized by simple condensation between various β-diketones and isoniazid. The titled compounds were synthesized following both conventional and microwave irradiation methods. The in vitro antibacterial activity of synthesized derivatives was evaluated against gram-positive (B. subtilis, S. aureus and S. pyogenes) and gram-negative (E. coli, and K. pneumonia) bacterial strains and expressed in terms of zone of inhibition and also screened for antioxidant activity. Results: The yield of products was appreciably increased in shorter reaction times with the aid of microwave-assisted synthesis. Therefore, it follows the green chemistry approach by making the above reactions eco-friendly. The synthesized compounds were characterized using FT-IR, 1H NMR, 13C NMR, and elemental analysis techniques. The spectroscopic techniques showed the formation of β-diketone hydrazone compounds. Theoretical data show good agreement with the experimental results. Some of the compounds displayed significant antibacterial and antioxidant potentials when compared to the standard drug. Conclusion: In the present research work, we report the synthesis of some novel β-diketone hydrazone derivatives. A high yield of compounds was noted under microwave-assisted reaction in shorter reaction times. The results revealed that the synthesized Schiff bases showed good radical scavenging activity.


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