Synthesis and Biological Evaluation of Some Novel 2-Pyrazinoic Acidderived Esters

2019 ◽  
Vol 16 (5) ◽  
pp. 424-429
Author(s):  
Hossein Khani-Meinagh ◽  
Hossein Mostafavi ◽  
Majid Mahdavi
Keyword(s):  
Free Radical ◽  
Kojic Acid ◽  
Antioxidant Activities ◽  
Radical Scavenging ◽  
K562 Cells ◽  
Free Radical Scavenging ◽  
Leukemia Cells ◽  
Human Leukemia ◽  
Human Leukemia Cells ◽  
Ic50 Value

Pyrazine, a kojic acid having hydroxypyrone, and hydroquinone are the head compounds of different categories possessing a broad range of biological activities including anticancer and antioxidant activities, thus are interested in evaluating the cytotoxicity on K562 human leukemia cells and radical scavenging activities of these compounds in bonding together as ester compounds. Four hydroxypyrone containing-2-pyrazinoic esters along with hydroquinone containing-one were synthesized and characterized by spectral data. The cytotoxicity of these compounds on K562 human leukemia cells and free Radical scavenging activities were evaluated. The K562 cells were treated with various concentrations of each compound for a different time and cell viabilities were determined by MTT viability assay. It was observed that all compounds decreased the viability of the human leukemia K562 cells in a dose- and time-dependent manner. Hydroquinone pyrazinoate 4a with an IC50 value of 50±8.0 µM was the most active compound against the K562 cells. The compounds 4b and 4e showed higher cytotoxicity on K562 cells respectively after 72 h. Antioxidant activities of the compounds were evaluated by DPPH free radical scavenging assay. Hydroquinone ester 4a showed higher activity with an IC50 value of 0.82 mM than those of hydroxypyrone derivatives of which maltol pyrazinoate 4e showed the highest inhibition with IC50 value of 4.7 mM. Although free hydroxyl group of kojic acid was masked by ester group, 4b and 4e showed significant scavenging activities, as the same result was observed in the case of hydroquinone ester.

scholarly journals Novel cholinesterase inhibitory effect of α-spinasterol isolated from the leaves of Acacia auriculiformis A. CUNN Ex. Benth (Fabaceae)

2020 ◽  
Vol 19 (7) ◽  
pp. 1473-1479
Author(s):  
Bilqis A. Lawal ◽  
Aniefiok Udobre ◽  
Taiwo O. Elufioye ◽  
Augustine A. Ahmadu ◽  
Bolatito Olanipekun
Keyword(s):  
Ascorbic Acid ◽  
Free Radical ◽  
Antioxidant Activities ◽  
Radical Scavenging ◽  
Inhibitory Effect ◽  
Free Radical Scavenging ◽  
Acacia Auriculiformis ◽  
Ic50 Value ◽  
Potent Inhibitory Effect

Purpose: To investigate the in vitro anticholinesterase, α-glucosidase and antioxidant activities of α-spinasterol isolated from Acacia auriculiformis leaves.Methods: The powdered leaves of Acacia auriculiformis were extracted with 70 % ethanol and the dried hydroalcoholic extract was suspended in water and partitioned with ethyl acetate and n-butanol to give their soluble fractions. The in vitro inhibitory activities of α-spinasterol were determined against cholinesterase and, α-glucosidase enzymes, and free radical scavenging potentials using (1,1-diphenyl-2-picrylhydarzyl (DPPH) and 2,2-azino-bis (3-Ethylbenzothiazoline-6-sulphonic acid (ABTS) antioxidantassays.Results: The compound, α-spinasterol, exhibited moderate anticholinesterase activity (IC50 value of 44.19±2.59 μg/mL which was significantly  different at (p < 0.05) when compared to the standard galanthamine (IC50 value of 1.73 ± 1.10 μg/mL). It also displayed a good α-glucosidase  inhibitory activity with IC``` value of 8.65 ± 1.71μg/mL which was not significantly different when compared to the standard, acarbose with IC50 value of 2.79±0.81 μg/mL. This compound, however, exhibited weak free radical scavenging activities at 26.93 ± 0.00 and 35.16 ±.0.26 % inhibition of DPPH+ and ABTS+ radicals as compared to ascorbic acid and Trolox (73.88 ± 0.04 and 99.82 ± 0.00%) respectively.Conclusion: The results show that α-spinasterol isolated from Acacia auriculiformis exerts potent inhibitory effect against cholinesterase enzyme which might serve as a lead in the search for drugs against Alzheimer disease and diabetes mellitus. Keywords: Acacia auriculiformis, α-Spinasterol, Galanthamine, Acarbose, Trolox, Ascorbic acid

scholarly journals Cytotoxicity and Antioxidant Effects of Celastrus hindsii Benth. Leaf Extract

2020 ◽  
Vol 36 (1) ◽  
Author(s):  
Bui Thi Thanh Duyen ◽  
Vu Manh Hung ◽  
Bui Thanh Tung
Keyword(s):  
Free Radical ◽  
Cancer Cells ◽  
Leaf Extract ◽  
Antioxidant Activities ◽  
Publishing House ◽  
Radical Scavenging ◽  
Antioxidant Effect ◽  
Ic50 Value ◽  
Etoac Fraction ◽  
Antioxidant Effects

Celastrus hindsii Benth et Hook. is known as a herbal medicine for the treatment of cancer. In this study we evaluated the cytotoxic and antioxidant effects of Celastrus hindsii Benth et Hook. leaf extract. Samples of Celastrus hindsii were extracted with 90 % ethanol and subsequently fractionated with n-hexane, ethyl acetate (EtOAc) and n-butanol (n-BuOH) solvents. To evaluate the cytotoxic effect, we performed MTT (3- (4,5 dimethylthiazol-2 - yl) - 2,5 - diphenyltetrazolium) assay on the three cell lines human liver Hep G2 (HB - 8065TM), lung LU-1 (HTB - 57TM), breast MCF-7 (HTB - 22TM).  The antioxidant effect was evaluated by screening DPPH (2,2-diphenyl-1-picryhydrazyl) free radical assay. The results showed that the EtOAc fraction had the strongest cytoxicity effects on liver cancer cells and lung cancer cells with an IC50 value of 33,7 ± 1,5 mg/mL and 13,0 ± 0,5 mg/mL. The BuOH fraction showed a weaker effect on lung cancer cells with IC50 value of 64,0 ± 2,2 mg/mL. The antioxidant results indicated that the EtOAc fraction had the best antioxidant effect with IC50  value of 46,9 ± 2,5 µg/mL. The EtOH total extract also has strong antioxidant activity with IC50 value of 48,5 ± 2,3 µg/mL. Our study showed that Celastrus hindsii leaf extract has the strong cytotoxicity and antioxidant activities. Keywords Celastrus hindsii Benth et Hook., cytotoxicity, MTT, antioxidant, DPPH. References [1] Ministry of health, General oncology. 2009: Vietnam Education Publishing House Limited Company, 9-10.[2] N.V. Tuyen, Pharmaceutical chemistry curriculum, 2014, Science and Technics Publishing House. 222-223.[3] V.V. Chi. Dictionary of Vietnamese medicinal plants. Medical Publishing House 1 (2012).[4] V. Gan, G. Chen, W. Zhang, J. Zhou . Oleanen induces apoptosis of cervical cancer cells by up-regulation of Bim. International Journal of Gynecologic Cancer 22(1) (2012) 38.[5] Y.H. Kuo, L.M.Y. Kuo. Antitumour and anti-AIDS triterpenes from Celastrus hindsii. Phytochemistry 44(7) (1997) 1275.[6] T. Mosmann, Rapid colorimetric assay for cellular growth and survival: application to proliferation and cytotoxicity assays 65(1-2) (1983) 55.[7] P. Mahakunakorn, M. Tohda, Y. Murakami, K. Matsumoto, H.J.B. Watanabe, P. Bulletin, Antioxidant and free radical-scavenging activity of Choto-san and its related constituents 27(1) (2004) 38.[8] P.T. Thuong, M.K. Na, N.H. Dang, T.M. Hung, P.T. Ky, T.V. Thanh, et al. Antioxidant activities of Vietnamese medicinal plants 12(1) (2006) 29.[9] X.Q. Hu, W. Han, Z.Z. Han, Q.X. Li, X.K. Xu, P. Fu, et al. A new macrocyclic lactone and a new quinoflavan from Celastrus hindsii. Phytochemistry letters 7 (2014) 169.[10] A.C. Spivey, M. Weston, Woodhead SJCSR. Celastraceae sesquiterpenoids: biological activity and synthesis 31(1) (2002) 43.[11] T.L. Ngoc, Technology. Separation process of rosmarinic acid and their derivatives from Celastrus hindsii benth leaves. Vietnam Journal of Science 54(2C) (2016) 380.[12] F.R. Mowsumi, A. Rahaman, N.C. Sarker, B.K. Choudhury, Hossain SJWJPPS. In vitro relative free radical scavenging effects of Calocybe indica (milky oyster) and Pleurotus djamor (pink oyster). 4(07) (2015).[13] T.D. Viet, T.D. Xuan, T.M. Van, Y. Andriana, R. Rayee, H.D. Tran. Comprehensive Fractionation of Antioxidants and GC-MS and ESI-MS Fingerprints of Celastrus hindsii Leaves. Medicines 6(2) (2019) 64.[14] T.N. Ly, M. Shimoyamada, Yamauchi RJJoa, chemistry f. Isolation and characterization of rosmarinic acid oligomers in Celastrus hindsii Benth leaves and their antioxidative activity 54(11) (2006) 3786.    

scholarly journals Design, Synthesis, Antimicrobial, and Antioxidant Activities of Novel-{4, 5-(substituted diphenyl)-4H-1, 2, 4-triazol-3-ylthio} Acetyl Chloride

2017 ◽  
Vol 15 (2) ◽  
pp. 157-167
Author(s):  
Prabhakar Kumar VERMA ◽  
Mukesh KUMAR ◽  
Nelam MALIK ◽  
Priyanka DHIMAN ◽  
Anurag KHATAHAR
Keyword(s):  
Free Radical ◽  
Acetyl Chloride ◽  
Antioxidant Activities ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Free Radical Scavenging ◽  
Biologically Active ◽  
Free Radical Scavenging Activity ◽  
Scavenging Activity ◽  
Standard Drug

A series of 20 new biologically active derivatives of 2-{4, 5-(substituted diphenyl)-4H-1,2,4-triazol-3-ylthio}acetyl chloride has been synthesized, with the aim to investigate antimicrobial, free radical scavenging activity. All the synthesized compounds were characterized by spectroscopic data and elemental analysis. The final compounds were tested for antibacterial activity against Gram-positive bacteria: Staphylococcus aureus MTCC 3160, Bacillus subtilis MTCC 441; Gram-negative bacteria: Escherichia coli MTCC 443, and, for antifungal activity, against Candida albicans MTCC 227 and Aspergillus niger MTCC 281, taking ciprofloxacin as antibacterial and fluconazole as antifungal standard drugs. Compound 7a6 was found to be the most effective antibacterial (MIC = 3.12 µg/ml), and compounds 7a2 and 7d1 (MIC = 3.12 and 6.25 µg/ml) had the most effective antifungal effects on the selected strains, as compared to the standard drugs. The results of antioxidant studies revealed that compound 7b1 was found to be most active antioxidant, with 40.4±0.687 µg/ml, and compounds 7b3, 7d7, and 7d4 also showed promising free radical scavenging activity, as compared with the standard drug ascorbic acid.

scholarly journals Antioxidant activities of traditional plants in Sri Lanka by DPPH free radical-scavenging assay

Data in Brief ◽  
2018 ◽  
Vol 17 ◽  
pp. 870-875 ◽  
Author(s):  
Kotaro Hara ◽  
Takao Someya ◽  
Katsura Sano ◽  
Yoshimasa Sagane ◽  
Toshihiro Watanabe ◽  
...  
Keyword(s):  
Free Radical ◽  
Sri Lanka ◽  
Antioxidant Activities ◽  
Radical Scavenging ◽  
Free Radical Scavenging ◽  
Free Radical Scavenging Assay ◽  
Radical Scavenging Assay

scholarly journals Domestic Cooking Effects of Bambara Groundnuts and Common Beans in the Antioxidant Properties and Polyphenol Profiles

2017 ◽  
Vol 6 (2) ◽  
pp. 24 ◽  
Author(s):  
V. Nyau ◽  
S. Prakash ◽  
J. Rodrigues ◽  
J. Farrant
Keyword(s):  
Free Radical ◽  
Methanolic Extract ◽  
Antioxidant Activities ◽  
Antioxidant Properties ◽  
Radical Scavenging ◽  
Free Radical Scavenging ◽  
Esi Ms ◽  
Positive Effects ◽  
Phytochemical Profiles

Processing of legumes before consumption has several effects on micronutrients, macronutrients and phytonutrients. This study was undertaken to investigate the effect of domestic processing on antioxidant activities and phenolic phytochemicals of the red bambara groundnuts and red beans. The study employed in vitro antioxidant assays (DPPH and FRAP) to screen for antioxidant properties, HPLC-PDA-ESI-MS and Folin Ciocalteu assay to screen for phenolic phytochemical profiles. Domestic cooking displayed positive effects on the antioxidant activity and phenolic phytochemical profiles of the two legumes. The free radical scavenging speed increased 10-fold in the methanolic extract from cooked red bambara groundnuts compared to uncooked. By contrast, the free radical scavenging speed increased 20-fold in the methanolic extract from cooked red beans compared to uncooked. HPLC-PDA-ESI-MS profiles of the cooked red bambara groundnuts and red beans revealed a number of emergent phenolic compounds, mainly flavonoids. These data indicate that cooking appear to enhance the nutraceutical profiles of the legumes investigated.

scholarly journals ANTIOXIDANT ACTIVITIES OF ROPINIROLE AND PRAMIPEXOLE NOVEL DRUGS USED IN TREATMENT OF PARKINSONISM: AN IN VITRO APPROACH

2016 ◽  
Vol 9 (9) ◽  
pp. 105 ◽  
Author(s):  
Preetha Selva ◽  
Srinivasan Vengadassalapathy
Keyword(s):  
Free Radical ◽  
Dopamine Agonist ◽  
Antioxidant Activities ◽  
Radical Scavenging ◽  
Free Radical Scavenging ◽  
Novel Drugs ◽  
Dpph Method ◽  
Selective Dopamine ◽  
Free Radical Scavenging Activities

ABSTRACTObjective: The objective of this study is to evaluate and compare the free radical scavenging activities of selective dopamine agonist namely ropiniroleand pramipexole.Methods: The antioxidant activity of ropinirole and pramipexole at various concentrations was done by 1, 1-diphenyl-2picrylhydrazyl (DPPH) freeradical scavenging assay comparing it with ascorbic acid which was taken as standard.Results: The free radical scavenging property as measured by DPPH method showed that ropinirole and pramipexole have got a potent free radicalscavenging activity with that of ascorbic acid.Conclusion: Novel drugs such as pramipexole and ropinirole are promising molecules in the field of oxidative damage related neurodegenerativedisorders providing us an optimistic targeted approach toward neuroprotection.Keywords: Free radical scavenging, 1, 1-diphenyl-2picrylhydrazyl assay, Anti-Parkinson’s, Dopamine agonist.

Free radical scavenging reactions and antioxidant activities of silybin: Mechanistic aspects and pulse radiolytic studies

2009 ◽  
Vol 43 (9) ◽  
pp. 887-897 ◽  
Author(s):  
Haiying Fu ◽  
Mingzhang Lin ◽  
Yusa Muroya ◽  
Kuniki Hata ◽  
Yosuke Katsumura ◽  
...  
Keyword(s):  
Free Radical ◽  
Antioxidant Activities ◽  
Radical Scavenging ◽  
Free Radical Scavenging
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