Carbonic Anhydrase Inhibition Potential and Some Bioactivities of The Peripherally Tetrasubstituted Cobalt(II), Titanium(IV), Manganese(III) Phthalocyanines

Author(s):  
Ayça Aktaş Karaçelik ◽  
Murat Küçük ◽  
Derya Efe ◽  
Volkan Çakır ◽  
Zekeriya Bıyıklıoğlu

Background: Peripherally tetrasubstituted cobalt(II), titanium(IV), manganese(III) phthalocyanines carrying redox-active metal centers were previously synthesized. Metallophthalocyanines (MPcs) have exhibited the potential to use in medicinal applications due to biological activities such as antibacterial, antioxidant and enzyme inhibition. Objective: This study aim was to evaluate the previously synthesized metallophthalocyanines in terms of carbonic anhydrase inhibition, antioxidant, and antimicrobial activities. Methods: Carbonic anhydrase activity was assayed by following esterase activity. The antibacterial activity was tested by the disc diffusion method against eight bacteria. The antioxidant activity was determined by two common methods, 2,2- diphenyl-1-picrylhydrazyl (DPPH•) radical scavenging and ferric ion (III) reducing/antioxidant power (FRAP) assays. Results and Discussion: In this study, the inhibition potential of the metallophthallocyanines against carbonic anhydrase (CA) enzyme, which is important for treatments of many disorders, was evaluated. The metallophthalocyanines showed high CA inhibitory activity with IC50 values in the range of 74-317 nM, which was similar or better when compared with the standard CA inhibitors sulfanilamide and acetazolamide. In addition, antibacterial and antioxidant activities were determined. The metallophthallocyanines exhibited moderate antibacterial activity, especially against S. aureus and S. epidermis. The antioxidant activities of the compounds in both tests were quite high even exceeding the standards Trolox and BHT, with SC50 values of 0.0048-0.0257 and TEAC values of 1143.3-1543.7 µM, which meant 2 to 73 fold better activity. Conclusion: In conclusion, all three metallophthalocyanines exhibited excellent carbonic anhydrase and antioxidant potential and have deserved further interest in the synthesis of new derivatives.

2018 ◽  
Vol 2018 ◽  
pp. 1-7 ◽  
Author(s):  
Kenza Ammor ◽  
Dalila Bousta ◽  
Sanae Jennan ◽  
Bahia Bennani ◽  
Abdellah Chaqroune ◽  
...  

The aim of this study is to investigate in vitro antioxidant and antibacterial activities of the aqueous and hydroethanolic extracts for aerial parts of Herniaria hirsuta. Extracts were screened for their possible antioxidant activities by three tests: DPPH free radical-scavenging, reducing power, and molybdenum systems. The screening of antibacterial activity of extracts was individually evaluated against sixteen bacteria species using a disc diffusion method. Flavonoids, total phenols, and tannins content were performed for both extracts. It shows higher content in the hydroethanolic extract. The hydroethanolic extract showed a significant antioxidant activity for the three methods studies to the aqueous extract, but nonsignificant results compared to the reference (BHT). However, both extracts have negative effect on the strains studies for the antibacterial activity.


2018 ◽  
Vol 22 (2) ◽  
pp. 140-147 ◽  
Author(s):  
Bimala Subba ◽  
Susila Thapa

Phytochemical and biological activities of methanolic extract of seven plants viz. Scindapsus officinalis Schott. , Lepisorus loriformis, Nicotiana tabacum L., Clematis buchananiana DC., Astilbe rivularis D. Don, Potentilla fulgens Wall. ex Hook and Taxus wallichiana Zucc. were carried out. The brine shrimp bioassay showed that N. tabacum, A. rivularis, and P. fulgens were pharmacologically active. The antibacterial potential was studied against Staphylococcus aureus (gram positive bacteria) and Escherichia coli (gram negative bacteria) using Agar Well Diffusion Method. Roots of P. fulgens showed inhibition against gram positive bacteria while the rhizome of A. rivularis showed inhibition against both gram positive and gram negative bacteria. Antioxidant activity was evaluated by 2, 2-diphenyl-1-picryl hydrazyl (DPPH) free radical scavenging activity and ferric reducing antioxidant power FRAP assay. Both assays showed that P. fulgens has high antioxidant activities with (IC50 =15.57 ± 3.6) lower than standard ascorbic acid.  Journal of Institute of Science and TechnologyVolume 22, Issue 2, January 2018, Page: 140-147


2012 ◽  
Vol 506 ◽  
pp. 371-374 ◽  
Author(s):  
S. Sanpa ◽  
Krit Sutjarittangtham ◽  
T. Tunkasiri ◽  
Sukum Eitssayeam ◽  
P. Chantawannakul

Propolis is the mixture of resins that honeybees collect from plant buds, leaves and exudates. Antimicrobial and antioxidant properties of propolis have been widely studied, however, there have few reports on Thai propolis. To increase the efficient extraction of organic propolis compounds, extraction methods have been developed. We applied the ultrasound technology to reduce extraction time and increase extraction yields of propolis. The propolis was extracted using ultrasound technology for 15-60 minutes and the propolis extracts were examined to compare their biological activities. Antimicrobial activities of the propolis were investigated using the agar well diffusion method. The free radical-scavenging and antioxidant activities of propolis extracts were measured using the DPPH and FolinCiocalteau colorimetric methods. The propolis extracted using ultrasound for 15 and 30 minutes showed inhibitory effects on tested fungi and bacteria as well as antioxidant activities.


Molecules ◽  
2021 ◽  
Vol 26 (5) ◽  
pp. 1205
Author(s):  
Adesola A. Adeleke ◽  
Sizwe J. Zamisa ◽  
Md. Shahidul Islam ◽  
Kolawole Olofinsan ◽  
Veronica F. Salau ◽  
...  

A series of fifteen silver (I) quinoline complexes Q1–Q15 have been synthesized and studied for their biological activities. Q1–Q15 were synthesized from the reactions of quinolinyl Schiff base derivatives L1–L5 (obtained by condensing 2-quinolinecarboxaldehyde with various aniline derivatives) with AgNO3, AgClO4 and AgCF3SO3. Q1–Q15 were characterized by various spectroscopic techniques and the structures of [Ag(L1)2]NO3Q1, [Ag(L1)2]ClO4Q6, [Ag(L2)2]ClO4Q7, [Ag(L2)2]CF3SO3Q12 and [Ag(L4)2]CF3SO3Q14 were unequivocally determined by single crystal X-ray diffraction analysis. In vitro antimicrobial tests against Gram-positive and Gram-negative bacteria revealed the influence of structure and anion on the complexes′ moderate to excellent antibacterial activity. In vitro antioxidant activities of the complexes showed their good radical scavenging activity in ferric reducing antioxidant power (FRAP). Complexes with the fluorine substituent or the thiophene or benzothiazole moieties are more potent with IC50 between 0.95 and 2.22 mg/mL than the standard used, ascorbic acid (2.68 mg/mL). The compounds showed a strong binding affinity with calf thymus-DNA via an intercalation mode and protein through a static quenching mechanism. Cytotoxicity activity was examined against three carcinoma cell lines (HELA, MDA-MB231, and SHSY5Y). [Ag(L2)2]ClO4Q7 with a benzothiazole moiety and [Ag(L4)2]ClO4Q9 with a methyl substituent had excellent cytotoxicity against HELA cells.


Author(s):  
Nuriye Korkmaz ◽  
Sıla Ozlem Sener ◽  
Nuray Balturk ◽  
Seyda Kanbolat ◽  
Merve Badem ◽  
...  

The goal of our study was to examine of antioxidant, antimicrobial, anticholinesterase activities, and phenolic composition of Psephellus huber-morathii. The antioxidant activities of extracts have been assessed by Ferric reducing antioxidant power (FRAP), cupric reducing antioxidant capacity (CUPRAC), and 2,2-diphenylpicrylhydrazyl (DPPH) radical scavenging. Phenolic constituents were measured using reverse phase-high performance liquid chromatography (RP-HPLC), and antimicrobial activity was investigated using the agar well diffusion method. Total phenolic content, FRAP, and CUPRAC results of aqueous extract have been better than methanolic extract, except for DPPH activity. Benzoic acid, and p-coumaric acid as major phenolic compounds were specified. Methanolic extract was especially effective against all microorganisms tested except for Yersinia pseudotuberculosis. The methanolic extract have been displayed inhibitory effect on tyrosinase. All extracts have been exhibited lower acetylcholinesterase, and butyrylcholinesterase inhibitory activities than galantamine. P. huber-morathii can be considered in the food, and drug industries due to antioxidant capacity and antimicrobial activities of the species. It can be potential source as anti-browning agents  because of its average tyrosinase inhibitory activity.


2020 ◽  
Vol 10 (2) ◽  
pp. 145-152 ◽  
Author(s):  
Imane Rihab Mami ◽  
Rania Belabbes ◽  
Mohammed El Amine Dib ◽  
Boufeldja Tabti ◽  
Jean Costa ◽  
...  

Background: Carthamus caeruleus belongs to the Asteraceae family. The roots are traditionally used as healing agents. They help to heal burns and treat skin diseases. They are also used against joint inflammation and are very effective against diseases such as irritable bowel syndrome for cancer patients. Objectives: The purpose of this work was i) to study the chemical composition of i) the essential oil and hydrosol extract of Carthamus caeruleus, ii) to isolate the major component of both extracts and iii) to evaluate their antioxidant, antifungal and insecticidal activities. Methods: The essential oil and hydrosol extract obtained from the roots were studied by GC and GC/MS. The antioxidant activities were performed using two different methods i) Radical scavenging activity (DPPH) and ii) the Ferric-Reducing Antioxidant Power (FRAP), using BHT as a positive control. Whereas, the antifungal activity of the essential oil and Carlina oxide was investigated against plant fungi. The fumigation toxicity of C. caeruleus essential oil besides Carlina oxide was evaluated against adults of Bactrocera oleae better known as the olive fly. Results: The essential oil and hydrosol extract were mainly represented by acetylenic compounds such as carline oxide and 13-methoxy carline oxide. Carlina oxide was isolated and identified by 1H and 13C NMR spectroscopic means. The results showed that Carlina oxide presented interesting antioxidant and antifungal properties, while C. caeruleus root essential oil had better insecticidal activity. Furthermore, Carlina oxide has demonstrated promising in vivo antifungal activity to control infection of apples by Penicillium expansum. Conclusion: Carlina oxide can be used as a natural food preservative and alternative to chemical fungicides to protect stored apple against Penicillium expansum.


2020 ◽  
Vol 42 (1) ◽  
pp. 109-109
Author(s):  
Hao Zang Hao Zang ◽  
Qian Xu Qian Xu ◽  
Luyun Zhang Luyun Zhang ◽  
Guangqing Xia Guangqing Xia ◽  
Jiaming Sun and Junyi Zhu Jiaming Sun and Junyi Zhu

A series of hydroxytyrosol (HT) derivatives were synthesized by modification of alcohol hydroxyl group of HT, twenty-five target compounds were obtained and characterized by NMR and HRMS. The antioxidant activities of those compounds were evaluated in three different assays. Except 3e and 3y, all other compounds demonstrated significant 2,2and#39;-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) free radical cation scavenging activity ranging from IC50 3.4 to 24.4 μM, which were more potent than L-ascorbic acid (IC50=24.8 μM). Compounds 3b-3d, 3f-3k, 3m-3x were better than Trolox (18.3 M). Moreover, the ferric reducing antioxidant power (FRAP) of all compounds were discovered to be more potent than L-ascorbic acid (40.7 mmol/g), except 3e, all other compounds (141.5-202.1 mmol/g) were better than Trolox (94.7 mmol/g). Compounds 3a-3d, 3f-3j, 3l-3m, 3o, 3q, 3t, 3v-3y exhibited more potent hydroxyl radical scavenging activity (IC50=245.1-475.1 M) than L-ascorbic acid (554.4 M) and Trolox (500.4 M). Compounds 3q, 3t and 3y exhibited more potent -Glucosidase inhibition activity (39.1-52.4 M) than Acarbose (60.9 M). Compounds 3a, 3d, 3f-3m, 3s-3t, 3v-3y showed some acetylcholinesterase inhibition activities, compounds 3a, 3d, 3f-3j, 3l-3m, 3o-3p, 3s-3t, 3w showed some butyrylcholinesterase inhibition activities.


2020 ◽  
Vol 38 ◽  
Author(s):  
M. AKBAR ◽  
I.N. SHERAZI ◽  
M.S. IQBAL ◽  
T. KHALIL ◽  
H.M. WAQAS

ABSTRACT: In the present study, antibacterial and antioxidant [1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging activity] activities of a weed, slender amaranth (Amaranthus viridis L.) were investigated. Extracts of different plant parts were prepared in n-hexane, chloroform and ethyl acetate. Antibacterial activity was measured by using 100 mg mL-1 concentration extracts against 4 deadly phytopathogenic bacterial species viz. Pseudomonas syringae Van Hall, Ralstonia solanacearum Smith, Erwinia carotovora (Jones), Holland and Xanthomonas axonopodis Hasse. In antioxidants assays, 10, 20 and 30 mg mL-1 extracts were used keeping DPPH as control. In these bioassays, ethyl acetate fraction of A. viridis leaf exhibited the best antibacterial and antioxidants activity. Ethyl acetate leaf fraction showed the highest inhibition zone diameter (IZD) where it caused 21 mm IZD against P. syringae and 19 mm IZD against E. carotovora. This extract also showed 22, 52 and 84% antioxidant activity at 10, 20 and 30 mg mL-1 concentrations, respectively. Previously there is no report available that describes antibacterial activity of root extract of A. viridis against P. syringae. Moreover, antioxidant activity of stem and root extracts in n-hexane, chloroform and ethyl acetate was investigated first time in the world. It was concluded that the biological activities observed during the present investigation may be due to the presence of bioactive constituents that can be harnessed as natural antibacterials and antioxidants.


2019 ◽  
Vol 41 (1) ◽  
pp. 161-161
Author(s):  
Farzana Nighat and Zahid Mushtaq Farzana Nighat and Zahid Mushtaq

Humans and plants are experiencing different kinds of diseases. Many of these diseases are mainly caused by microorganisms like fungi, bacteria and viruses that adversely affect their hosts. Bioactive compounds produced by bacteria can be used to treat the infections caused by these microorganisms. Free radicals that can cause serious damage to the cell can be repressed by antioxidants that are produced by bacteria as secondary compounds. The current case study was therefore planned to investigate the antimicrobial and antioxidant potentials of the organic and aqueous extracts of Bacillus clausii KP10 isolated recently by our group from hot springs of Tatta Pani, Poonch, Azad Kashmir. The antimicrobial activities were assessed using well diffusion method against two Gram positive bacteria; B. subtilis, and S. aureus, and two Gram negative bacteria; E. coli and P. multocida and three fungal strains; A. niger, A. parasiticus and A. ustus. Antioxidant activities of the extracts were done by DPPH free radical scavenging assay. In our experiments the maximum zones of inhibition were shown by ethanolic extract against P. multocida (21 mm), S. aureus (13 mm) and methanol soluble fraction showed zone of inhibition against A. ustus (21 mm) as compared to the standard ciprofloxacin for bacteria and as antifungal agents with terbinafine. In our studies n-hexane fraction of B. clausii KP10 showed maximum 88.67% antioxidant activity. Finally, results were analyzed statistically through analysis of variance (ANOVA). Hence it is proved that the bioactive fractions obtained from B. clausii KP10 are good source of antimicrobials and antioxidants and they can be used as medicines in future for the respective treatments.


Chemija ◽  
2020 ◽  
Vol 31 (1) ◽  
Author(s):  
Kęstutis Dabrovolskas ◽  
Ilona Jonuškienė ◽  
Simona Sutkuvienė ◽  
Dalius Gudeika

Seven compounds were synthesized by known methods, and their antibacterial activity was evaluated against Bacillus subtilis and Escherichia coli using a disk diffusion method. Antioxidative activity was evaluated using free 1,1-diphenyl-2-picryl-hydrazyl radical scavenging assay and ferric reducing antioxidant power methods. The disk diffusion method revealed that 6 out of 7 tested compounds showed antibacterial activity against tested strains, they inhibited the growth of bacteria at various concentrations, from 31.25 to 250 μg/ml. 3-Cyano-9H-carbazole, 3-iodo-9Hcarbazole and 3,6-diiodo-9H-carbazole showed a stronger antibacterial activity against Bacillus subtilis compared to the reference drug amoxicillin. 1,3,6-Tribromo-9H-carbazole showed a stronger activity against Escherichia coli. All tested compounds showed a weak antioxidative activity by the 1,1-diphenyl-2-picryl-hydrazyl radical scavenging assay and ferric reducing antioxidant power assay methods.


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