Design and Synthesis of Benzopyranopyrimidinyl Phosphonates as Cytotoxic and Antioxidant Agents

2019 ◽  
Vol 16 (7) ◽  
pp. 721-733
Author(s):  
Sarva Santhisudha ◽  
Gundluru Mohan ◽  
Tenkayala Sobha Rani ◽  
Peddaiahgari Vasu Govardhana Reddy ◽  
Cirandur Suresh Reddy
Keyword(s):  
Antioxidant Activity ◽  
Cytotoxic Activity ◽  
Carbon Nitride ◽  
Antioxidant Activities ◽  
Design And Synthesis ◽  
Antioxidant Agents ◽  
Green Conditions ◽  
Mcf 7 ◽  
In Vitro Antioxidant Activity

Background: A concatenation of bioactive diethyl(2-hydroxyphenylsubstituted) benzopyrano pyrimidinyl phosphonates were synthesized under eco-friendly green conditions in the presence of palladium doped graphitic carbon nitride (Pd@g-C3N4) as catalyst. Methods: he title compounds were evaluated for cytotoxic activity against MCF-7, SW-480, HeLa and HL-7702 cell lines and in-vitro antioxidant activity by DPPH, NO and H2O2 methods. Results: he synthesized compounds manifested robust cytotoxic and antioxidant activities. Conclusion: Some of them showed much higher bioactivity than the standards.

scholarly journals Phytochemical Investigations of Lonchocarpus Bark Extracts from Monteverde, Costa Rica

2014 ◽  
Vol 9 (4) ◽  
pp. 1934578X1400900 ◽  
Author(s):  
Caitlin E. Deskins ◽  
Bernhard Vogler ◽  
Noura S. Dosoky ◽  
Bhuwan K. Chhetri ◽  
William A. Haber ◽  
...  
Keyword(s):  
Fatty Acids ◽  
Antioxidant Activity ◽  
Costa Rica ◽  
Bacillus Cereus ◽  
Cytotoxic Activity ◽  
Antioxidant Activities ◽  
Antimicrobial Activities ◽  
Mcf 7

The acetone bark extracts of three species of Lonchocarpus from Monteverde, Costa Rica, L. atropurpureus, L. oliganthus, and L. monteviridis, were screened for antibacterial, cytotoxic, and antioxidant activities. L. orotinus extract was antibacterial against Bacillus cereus (MIC = 39 μg/mL), while L. monteviridis exhibited the most antioxidant activity. None of the Lonchocarpus extracts showed cytotoxic activity against MCF-7 cells. Fatty acids and atraric acid were isolated and purified from L. atropurpureus bark, fatty acids and loliolide from L. oliganthus bark, and leonuriside A and β-D-glucopyranos-1-yl N-methylpyrrole-2-carboxylate from L. monteviridis bark. Atraric acid showed cytotoxic and antimicrobial activities.

scholarly journals CYTOTOXIC AND ANTIOXIDANT ACTIVITIES OF SECONDARY METABOLITES FROM PULICARIA UNDULATA

2016 ◽  
Vol 8 (9) ◽  
pp. 150 ◽  
Author(s):  
Taha A. Hussien ◽  
Sayed A. El-toumy ◽  
Hossam M. Hassan ◽  
Mona H. Hetta
Keyword(s):  
Antioxidant Activity ◽  
Secondary Metabolites ◽  
Antioxidant Activities ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Hep G2 ◽  
Structure Activity ◽  
Dpph Method ◽  
Mcf 7

<p><strong>Objective:</strong><strong> </strong>To evaluate the <em>in vitro</em> cytotoxicity, antioxidant activities and structure-activity relationship of secondary metabolites isolated from <em>Pulicaria undulata</em>.</p><p><strong>Methods: </strong>The methylene chloride-methanol (1:1) extract of the air-dried aerial parts of <em>Pulicaria undulata</em> was fractionated and separated to obtain the isolated compounds by different chromatographic techniques. Structures of the isolated compounds were determined on the basis of the extensive spectroscopic analysis, including 1D and 2D NMR and compared with the literature data. The crude extract and the isolated compounds were evaluated for <em>in vitro</em> antioxidant activity using the 2,2 diphenyl dipicryl hydrazine (DPPH) method and cytotoxic assay using human breast cancer (MCF-7) and hepatoma (Hep G2) cell line.</p><p><strong>Results: </strong>Nine secondary metabolites were isolated from <em>Pulicaria undulata</em> in this study. Of which two terpenoidal compounds; 8-epi-ivalbin and 11β, 13-dihydro-4H-xanthalongin 4-<em>O</em>-β-D-glucopyranoside firstly isolated from the genus <em>pulicaria</em> and three flavonoids; eupatolitin, 6-methoxykaempferol, and patulitrin firstly isolated from <em>P. undulata</em>. 6-methoxykaempferol (IC<sub>50</sub> 2.3 µg/ml) showed the most potent antioxidant activity. The highest cytotoxic effect against MCF-7 and Hep G2 cells was obtained with eupatolitin (IC<sub>50</sub> 27.6 and 23.5 µg/ml) respectively. The structure-activity relationship was also examined and the findings presented here showed that 3, 5, 7, 4' and 3, 5, 4', 5'-hydroxy flavonoids were potent antioxidant and has cytotoxic activity.</p><p><strong>Conclusion: </strong><em>Pulicaria undulata</em> is a promising medicinal plant, and our study tends to support the therapeutic value of this plant as antioxidant drug and in the treatment of cancer.</p>

In vitro Antioxidant Capacities of Two Benzonaphthoxanthenones: Ohioensins F and G, Isolated from the Antarctic Moss Polytrichastrum alpinum

2009 ◽  
Vol 64 (3-4) ◽  
pp. 197-200 ◽  
Author(s):  
Hari Datta Bhattarai ◽  
Babita Paudel ◽  
Hong Kum Lee ◽  
Hyuncheol Oh ◽  
Joung Han Yim
Keyword(s):  
Antioxidant Activity ◽  
Methanolic Extract ◽  
Antioxidant Activities ◽  
Reducing Power ◽  
Commercial Application ◽  
Moss Species ◽  
Antioxidant Capacities ◽  
Antioxidant Agents ◽  
Antarctic Moss

Antioxidant agents against reactive oxygen species can be used for several cosmetic and medicinal applications. This study’s objective was to evaluate the antioxidant activities of Polytrichastrum alpinum (Hedw.) G. L. Sm. (Polytrichaceae), an Antarctic moss species collected from King George Island (Antarctica). The identifi cation of the moss species was performed on the basis of morphological characteristics and molecular sequencing of the 18S rRNA gene. Two benzonaphthoxanthenones: ohioensins F and G, were isolated from the extract after several chromatographic procedures. The various in vitro antioxidant capacities of a methanolic extract of P. alpinum and the isolated compounds were evaluated by analyzing the scavenging capacities of free radicals of 2,2-azino-bis(3-ethylbenzthiazoline- 6-sulfonic acid) (ABTS) and 2,2-diphenyl-1-picrylhydrazyl (DPPH), the total phenol assay with Folin-Ciocalteu reagent, the ferric ion (Fe3+) reducing power and the nitric oxide (NO) scavenging activity and compared to those of commercial standards for each assay. The experimental data showed that even the crude extract of P. alpinum exhibited potent antioxidant activity. The antioxidant activity was increased two- to seven-fold for the purified compounds. The antioxidant activities of both purified compounds were found to be more or less the same in all experiments. However, the obtained data showed that the Fe3+ reducing power of the purified compounds and crude methanolic extract was almost the same suggesting the presence of other stronger reducing agents in the methanolic extract which could not be isolated in the present experiment. Therefore, further work on the isolation of these stronger antioxidant agents from this moss specimen of the extreme environment is warranted. Developments of laboratory mass culture techniques are anticipated to achieve bulk production of the active constituents for commercial application.

One-pot construction of sterically challenging and diverse polyarylphenols via transition-metal-free benzannulation and their potent in vitro antioxidant activity

2017 ◽  
Vol 15 (9) ◽  
pp. 2052-2062 ◽  
Author(s):  
Shizuka Mei Bautista Maezono ◽  
Tej Narayan Poudel ◽  
Yong Rok Lee
Keyword(s):  
Antioxidant Activity ◽  
Transition Metal ◽  
Antioxidant Activities ◽  
One Pot ◽  
Metal Free ◽  
Novel Synthesis ◽  
In Vitro Antioxidant Activity

One pot novel synthesis of highly functionalized polyarylphenols via benzannulation under transition-metal-free conditions and their antioxidant activities are described.

scholarly journals Green Synthesis, Characterization and In-vitro Antioxidant Property of Silver Nanoparticles Using the Aqueous Leaf Extract of Justicia carnea

2021 ◽  
pp. 20-30
Author(s):  
I. O. Salaudeen ◽  
M. O. Olajuwon ◽  
A. B. Ajala ◽  
T. O. Abdulkareem ◽  
S. A. Adeniyi ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Silver Nanoparticles ◽  
Leaf Extract ◽  
Antioxidant Activities ◽  
Silver Ions ◽  
Antioxidant Property ◽  
Biological Macromolecules ◽  
Aqueous Leaf Extract ◽  
In Vitro Antioxidant Activity

This study investigated the synthesis, characterization and in vitro antioxidant activity of silver nanoparticles (AgNPs) using the aqueous leaf extract of Justicia carnea.  The aqueous leaf extract of J. carnea was used as a potential reducing and capping agent. To identify the compounds responsible for the reduction of silver ions, the functional groups present in the plant extract were subjected to FTIR. The in vitro antioxidant activity of synthesized nanoparticles was evaluated in terms of ferric reducing antioxidant potential (FRAP), DPPH (1,1-diphenyl-2-picrylhydrazyl) and ABTS (2,2`-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) free radicals scavenging assays. The surface plasmon resonance confirmed the formation of AgNPs with maximum absorbance at kmax = 446 nm. FTIR revealed the biological macromolecules of J. carnea leaf extract involved in the synthesis and stabilization of AgNPs. UV-Visible spectrophotometer showed absorbance peak in the range of 436-446 nm. The silver nanoparticles exhibited moderate antioxidant activities compared to standard antioxidants (ascorbic acid and BHT). These results confirmed this protocol as simple, eco-friendly, nontoxic and an alternative for conventional physical and chemical methods. It can be concluded that J. carnea leaf extract can be used effectively in the production of potential antioxidant AgNPs which could be useful in various bio-applications such as cosmetics, food and biomedical industry.

Estimation of Total Phenolics and Flavonoid Content and In-vitro Antioxidant Activity of Drypetes sepiaria Stem (Wight and Arn.) Pax and K. Hoffm.

2015 ◽  
Vol 5 (1) ◽  
Author(s):  
Packia M. ◽  
Daffodil D. ◽  
Tresina S. ◽  
Mohan R.
Keyword(s):  
Antioxidant Activity ◽  
Total Phenolics ◽  
Antioxidant Activities ◽  
Reducing Power ◽  
Model Systems ◽  
Aluminium Chloride ◽  
Total Phenolic ◽  
Ethanol Extracts ◽  
In Vitro Antioxidant Activity

The total phenolics, flavonoids and in vitro antioxidant activity of petroleum ether, benzene, ethyl acetate, methanol and ethanol extracts of stem of Drypetes sepiaria were determined using various antioxidant model systems viz, DPPH, hydroxyl, superoxide, ABTS and reducing power. Total phenolic content was estimated by Folin-Ciocalteau method. Flavonoids were determined by Aluminium chloride method. The total phenolics and flavonoids contents were found to be 0.81 g 100 g-1 and 1.12g 100 g-1 respectively in the methanol extract. Among the solvent tested, methanol and ethanol extracts of D. sepiaria stem showed potent in vitro antioxidant activities. This investigation explored that D. sepiaria stem is a potential source of natural antioxidant.

Vitamin C in Acerola and Red Plum Extracts: Quantification via HPLC, in Vitro Antioxidant Activity, and Stability of their Gel and Emulsion Formulations

2018 ◽  
Vol 101 (5) ◽  
pp. 1461-1465 ◽  
Author(s):  
Letícia Caramori Cefali ◽  
Ludmila de Oliveira Maia ◽  
Rebeca Stahlschimidt ◽  
Janaína Artem Ataide ◽  
Elias Basile Tambourgi ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Free Radicals ◽  
Vitamin C ◽  
Antioxidant Activities ◽  
Accelerated Aging ◽  
Stability Study ◽  
Transparent Glass ◽  
Glass Containers ◽  
In Vitro Antioxidant Activity

Abstract Background: The fruits acerola and red plum are known to be good sources of antioxidants, particularly vitamin C. Antioxidants are compounds that protect organisms from biomolecular damage, such as accelerated aging, caused by free radicals. Objective: The objective of this study was to extract vitamin C from acerola and red plum, incorporate these extracts into different topical formulations, and evaluate the physicochemical stabilities of these formulations under stress conditions. Methods: Vitamin C was extracted from acerola and red plum via dynamic maceration for 2 h at 50 ± 2°C and was quantified via HPLC. In vitro antioxidant activities were evaluated using DPPH assays. The extracts were then incorporated into emulsion and gel formulations in two types of packaging, and stability studies were carried out. Results: Red plum and acerola extracts were orange and red and contained vitamin C concentrations of 2732.70 ± 93.01 mg/100 g and 2.60 ± 1.2 mg/100 g, respectively. In vitro antioxidant activity resulted in over 90.0% inhibition of free radicals at 0.01 mL/mL acerola extract and 0.1 mL/mL red plum extract. In the stability study, pH values decreased for both acerola formulations when stored in the oven or in transparent glass containers. Formulations containing red plum extract were stable under all conditions. Acerola extracts contained a higher concentration of vitamin C than red plum extracts. Both extracts possessed antioxidant activity, although the acerola-based formulation was unstable when stored at high temperatures or in transparent glass containers. Highlights: Extracts from red plum and acerola contained vitamin C; antioxidant activity of the extracts resulted in over 90.0% inhibition of free radicals. Formulations containing red plum were stable under all tested conditions, and formulations containing acerola were unstable when stored in the oven or in transparent glass containers.

scholarly journals Design and Synthesis of π-Extended Resveratrol Analogues and In Vitro Antioxidant and Anti-Inflammatory Activity Evaluation

Molecules ◽  
2021 ◽  
Vol 26 (3) ◽  
pp. 646
Author(s):  
Ki Yoon Nam ◽  
Kongara Damodar ◽  
Yeontaek Lee ◽  
Lee Seul Park ◽  
Ji Geun Gim ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Antioxidant Activities ◽  
Biological Effects ◽  
Drug Candidates ◽  
Design And Synthesis ◽  
Study Results ◽  
Resveratrol Analogues ◽  
Anti Inflammatory ◽  
Nitrogen Substitution

The research on resveratrol (1) has been conducted intensively over a long time due to its proven antioxidant activity and disease-fighting capabilities. Many efforts have also been made to increase these biological effects. In the present study, six new extended aromatic resveratrol analogues containing naphthalene (2) and its bioisosteres quinoline (3 and 4), isoquinoline (5) quinoxaline (6) and quinazoline (7) scaffolds were designed and synthesized using an annulation strategy. The antioxidant and anti-inflammatory activities of these compounds were investigated. All compounds showed better antioxidant activity than resveratrol in ABTS assay. As for the anti-inflammatory test, 5 and 7 exhibited better activity than resveratrol. It is worth noting that nitrogen substitution on the extended aromatic resveratrol analogues has a significant impact on cell viability. Taking the antioxidant activities and NO inhibition activities into consideration, we conclude that isoquinoline analogue 5 may qualify for the further investigation of antioxidant and anti-inflammatory therapy. Furthermore, our study results suggest that in order to improve the biological activity of polyphenolic compounds, extended aromaticity and nitrogen substitution strategy could be a viable method for the design of future drug candidates.

Antioxidant Components and Antioxidant Activities of Hydroglyceroalcoholic Extract from Fresh Mushroom Mycelium

2017 ◽  
Vol 68 (3) ◽  
pp. 534-540
Author(s):  
Emanuel Vamanu
Keyword(s):  
Antioxidant Activity ◽  
Phenolic Compounds ◽  
Phenolic Acid ◽  
Antioxidant Activities ◽  
Submerged Cultivation ◽  
Active Components ◽  
Gentisic Acid ◽  
Polyphenolic Acids ◽  
In Vitro Antioxidant Activity

The in vitro antioxidant activity, as well as the hydroglyceroalcoholic extracts main active components from mycelia of Pleurotus ostreatus and Coprinus comatus, were determined. The mycelium submitted for extraction was obtained by submerged cultivation in a bioreactor. The hydroglyceroalcoholic extracts, in particular, those of P. ostreatus PSI101109 and PQMZ91109 mycelium had a considerable antioxidant activity, and was compared to the overall constituent of flavonoids plus phenolic compounds. According to the extracts HPLC assessment, the key phenolic acid evident from the extracts was gentisic acid. The homogentisic, gallic and protocatechuic acids were also determined. Catechin was identified as well, except for C. comatus M8102 and P. ostreatus PBS281009 mycelia extracts. Since catechol and gentisic acid levels were high, respectively, there was a correlation with the absence of carotenoid compounds in hydroglyceroalcoholic extracts (P. ostreatus PSI101109). There is a correspondence between the hydroglyceroalcoholic extracts� key antioxidant activities with the catechin and polyphenolic acids levels identified in each extract.

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