Antioxidant Activity of 1,2,4-Triazole and Its Derivatives: A Mini Review

Author(s):  
Anna Pachuta-Stec

: The information about the presence of free radicals in biological materials was given for the first time about 70 years ago. Since then, numerous scientific studies have been conducted and the science of free radicals was born. Today we know that free radicals are by-products of enzymatic reactions occurring in the organism. They are produced during endogenous processes such as: cell respiration, phagocytosis, biosynthesis, catalysis, and biotransformation. They can also be produced by exogenous processes (radiation, sunlight, heavy metals, bacteria, fungi, protozoa and viruses). The overproduction of free radicals affects the aging processes, oxidative stress (OS) and takes part in the pathogenesis of various diseases. Among them are cancer, rheumatoid arthritis, neurodegenerative diseases: Alzheimer and Parkinson, pulmonary diseases, atherosclerosis and DNA damage. Compounds with antioxidant activity are very important nowadays because they allow organisms to keep a balance between the production of free radicals and the speed of their neutralization in the body. Next to the natural antioxidants (flavonoids, carotenoids, vitamins, etc.), synthetic ones are also of great importance. Among synthetic compounds with antioxidant activity are 1,2,4-triazoles and its derivatives. 1,2,4-Triazoles are heterocyclic compounds with three nitrogen atoms. Due to a broad spectrum of biological activities, these derivatives have been of interest to scientists for many years. Some of them are also used as drugs. The finding of new synthetic compounds with antioxidant features in the triazole group has become important problem of medicinal chemistry.

Author(s):  
Pozdnyakovа Т.А. ◽  
Kuleshovа Е.S. ◽  
Bubenchikov R.A.

The predominance of synthetic and genetically modified foods in the diet of a modern person often leads to disruption of natural metabolic processes and the accumulation of toxic free radicals in the body, which provokes the development of various diseases. Natural antioxidants from medicinal plants can help maintain health and stop the processes of peroxidation. In our opinion, Аstragalus onobrychis can become a promising source of natural antioxidants. The aim of this study was to establish the antioxidant activity in extracts from the herb Astragalus onobrychis. In order to obtain objective and reliable results during our research, we used two methods: the method of titrimetry and spectrophotometry of free radicals. The titrimetric method is based on the chemical interaction between an oxidizing agent (potassium permanganate) and natural antioxidants present in extracts from plant raw materials, since they exhibit the properties of reducing agents. The spectrophotometric method makes it possible to assess the value of antioxidant activity and the duration of the reaction by assessing the interaction of 2,2-diphenyl-1-picrylhydrazil with plant antioxidants. To establish the relationship between the antioxidant activity and the presence of phenolic compounds in the plant, the content of flavonoids and hydroxycinnamic acids in the herb Astragalus onobrychis was determined. As a result of the studies, the total antioxidant activity of extracts from the herb Astragalus onobrychis was established and it was revealed that its value depends on the type of extractant used, since this factor is associated with the content of various groups of natural antioxidants in the extraction. The data obtained indicate the prospects of using the herb Astragalus onobrychis as a source of natural antioxidants.


2020 ◽  
Vol 11 (1) ◽  
pp. 1-27
Author(s):  
Adil Hussain

Background: There exist natural antioxidants in plants that scavenge harmful free radicals from the body. Free radicals are species of chemical origin with an unpaired electron and play a pivotal role in combating against health-related problems like lung damage, inflammation, and cardiovascular ailments etc. Antioxidants halt the development of these free radicals called the reactive oxygen species either by chelating the trace elements or by enzymes inhibition. Objectives: The aim of present review was to collect information about Pakistani medicinally important plants with the exploration of their antioxidant potential. Methodology: Total 206 papers were looked over, which were obtained from numerous sources like; Google Scholar, Medline, PubMed, Research Gate, Science Direct, Scopus and Web of Science. Results: Overall, 93 plants representing 44 families with potential antioxidant activity reported from Pakistan have been presented in this review. Maximum number of species from Asteracea, Poaceae and Rutaceae familes were scrutinized for their potential antioxidant activity from Pakistan. Conclusion: The present review clearly designates that the presence of phytochemicals and antioxidant activity of medicinal plants from Pakistan vary with the species of the plants and material/extracts used. From this review, it is recommended to perform comprehensive experimental investigations based on toxicology and ethnopharmacology on these precious plants from Pakistan. It will be advantageous in the provision of trustworthy information to patients and determine further innovative compounds for safer and new drugs development with fewer side effects.


Biomolecules ◽  
2020 ◽  
Vol 10 (3) ◽  
pp. 400 ◽  
Author(s):  
Alvaro Martinez-Gomez ◽  
Isabel Caballero ◽  
Carlos A. Blanco

Beer is one of the most consumed drinks around the world, containing a variety of compounds that offer both appreciated sensorial characteristics and health advantages. Important healthy compounds in beer are those with antioxidant properties that attenuate the content of free radicals produced as by-products in the human metabolism, exerting an appreciable effect against cancers or cardiovascular diseases. This work details a study of antioxidant compounds present in beer, focusing on the two main groups: phenols (including polyphenolic forms) and melanoidins, formed specifically during brewing as Maillard products. The fundaments of the most important methods to evaluate beer antioxidant activity, the main antioxidant compounds present in beer—especially those with healthy properties—and the new trends to increase beer antioxidant activity are also discussed.


2019 ◽  
Vol 22 (5) ◽  
pp. 206-212
Author(s):  
Sogandi Sogandi ◽  
Rabima Rabima

Antioxidants are compounds that can inhibit oxidation reactions by binding to free radicals and highly reactive molecules. One form of reactive oxygen compounds is free radicals, these compounds are formed in the body and are triggered by various factors. Noni fruits have been used by the community as a medicine for high blood pressure, beriberi, urinating, inflammation of bile, inflammation of the intestine, dysentery, constipation, spleen pain, liver pain, diabetes and lumbago. Nevertheless, research on the identification of the active compounds of noni fruit which act as antioxidants yet. This study aims to extract and fractionation of Noni fruit, determine the antioxidant activity of Noni fruit extract, and identify the types of bioactive compounds that act as antioxidants. Noni fruit was extracted used maceration technique with 96% ethanol and then fractionated using n-hexane, chloroform and ethyl acetate solvents. Antioxidant activity from the results of noni fruit fractionation was measured by the DPPH (1.1 diphenyl-2-picrylhydrachyl) method and identification of bioactive compounds was carried out by GCMS. The results showed the greatest antioxidant activity was found in chloroform fraction with a percentage of inhibition of 78.19%. For the first time this study revealed the types of bioactive compounds from noni fruit ethyl acetate fraction which act as antioxidants are n-hexadecanoic acid, squalene, pyridin-3-carboxamide, oxime, n- (2-trifluoro methyl phenyl), and beta-sitosterol


2020 ◽  
Vol 10 (1) ◽  
pp. 90
Author(s):  
Nur Ariska Nugrahani

Radikal bebas yang berbahaya jika konsentrasi ROS akan meningkat sehingga akan mengakibatkan stress oksidatif. Stress oksidatif biasanya disebabkan oleh konsentrasi tinggi dari radikal bebas dalam sel dan jaringan yang dapat diinduksi oleh beberapa faktor negatif seperti gamma, UV, radiasi sinar-X, tekanan psiko-emosional dan makanan yang tercemar.Untuk meminimalisir radikal bebas dalam tubuh diperlukan antioksidan alami seperti ekstrak buah kiwi dan ekstrak buah apel. Uji aktivitas antioksidan pada masing- masing ekstrak dilakukan dengan metode DPPH (1,1- difenil-2-pikrihidazil). Hasil menunjukkan bahwa nilai IC50 dari ekstrak buah kiwi lebih rendah daripada IC50 ekstrak buah apel. Hal ini menunjukkan bahwa ekstrak buah kiwi mempunyai aktivitas antioksidan lebih kuat dari ekstrak buah apel. Keyword : Radikal bebas, DPPH, Ekstrak buah kiwi, Ekstrak buah apel Free radicals will be dangerous if the ROS concentration will increase and causes oxidative stress. Oxidative stress is usually caused by high concentrations of free radicals in cells and tissues which can be induced by several negative factors such as gamma, UV, X-ray radiation, psycho-emotional pressure and contaminated food. To minimize free radicals in the body natural antioxidants such as kiwi fruit extract and apple extract. The antioxidant activity test on each extract was carried out by the DPPH method (1,1-diphenyl-2-picrihydazyl). The results showed that IC50 value of kiwi fruit extract was lower than IC50 of apple fruit extract. This shows that kiwi fruit extract has stronger antioxidant activity than apple extract. Keyword : free radicals, DPPH, kiwi fruit extract, apple fruit extract


2019 ◽  
Vol 16 (3) ◽  
pp. 194-201 ◽  
Author(s):  
Renu Bala ◽  
Vandana Devi ◽  
Pratibha Singh ◽  
Navjot Kaur ◽  
Pawandeep Kaur ◽  
...  

Background: Tetrahydroindazole, a member of the fused-pyrazole system, is a least studied class of heterocyclic compounds owing to its scarcity in nature. However, a large number of synthetically prepared tetrahydroindazoles are known to show a variety of biological activities such as interleukin- 2 inducible T-Cell kinase inhibitors, AMPA receptor positive allosteric modulators, antitumor, antituberculosis, anti-inflammatory and antimicrobial activities. Vilsmeier-Haack reaction is one of the most important chemical reactions used for formylation of electron rich arenes. Even though Vilsmeier- Haack reaction was studied on a wide variety of hydrazones derived from active methylene compounds, literature lacks the examples of the use of 4-substituted cyclohexanones as a substrate for the synthesis of 4,5,6,7-tetrahydroindazoles. The study of the reaction of Vilsmeier-Haack reagent with hydrazones derived from cyclic keto compounds having active methylene has been considered the interested topic of investigation. In the present study, ethyl cyclohexanone-4-carboxylate was treated with one equivalent of various hydrazines for two hours and the resulted hydrazones were further treated with an OPC-VH reagent (Vilsmeier-Haack reagent isolated from phthaloyl dichloride and N,Ndimethylformamide) afforded 4,5,6,7-tetrahydroindazoles in excellent yields. The synthesized compounds 4a-f and 5a-f were screened for their antioxidant activities using the DPPH radical scavenging assay. The target compounds were synthesized regioselectively using 4+1 approach in excellent yields. A number of experiments using both conventional heating as well as microwave irradiation methods were tried and on comparison, microwave irradiation method was found excellent in terms of easy work up, high chemical yields, shortened reaction times, clean and, no by-products formation. Some of the synthesized compounds showed significant antioxidant activity. The microwave assisted synthesis of 4,5,6,7-tetrahydroindazoles from ethyl cyclohexanone-4-carboxylate has been reported under mild conditions in excellent yield. Easy work up, high chemical yield, shortened reaction times, clean and no by-products formation are the major advantages of this protocol. These advantages may make this method useful for chemists who are interested in developing novel 4,5,6,7-tetrahydroindazole based drugs.


Plants ◽  
2021 ◽  
Vol 10 (5) ◽  
pp. 952
Author(s):  
Małgorzata Chrząszcz ◽  
Barbara Krzemińska ◽  
Rafał Celiński ◽  
Katarzyna Szewczyk

The genus Cephalaria, belonging to the Caprifoliaceae family, is a rich source of interesting secondary metabolites, including mainly saponins which display a variety of biological activities, such as immunomodulatory, antimicrobial and hemolytic effects. Besides these compounds, flavonoids and phenolic acids were identified in Cephalaria species. Cephalaria is employed in traditional medicine e.g., to cure cardiac and lung diseases, rheumatism, and regulate menstruation. In this review we focus on the phenolic compound composition and antioxidative activity of Cephalaria species. The antioxidant effect can be explained by flavonoids present in all parts of these plants. However, future efforts should concentrate more on in vitro and in vivo studies and also on clinical trials in order to confirm the possibility of using these plants as natural antioxidants for the pharmacology, food or cosmetic industries.


2021 ◽  
Vol 332 ◽  
pp. 08005
Author(s):  
Aminah Dalimunthe ◽  
Dewi Pertiwi ◽  
Mahatir Muhammad ◽  
Denny Satria

Free radicals also play a role in the pathology of various degenerative diseases such as cancer, rheumatism, coronary heart disease, cataracts, and others. Free radicals can come from within the body (endogenous) and outside the body (exogenous). Litsea cubeba (Lour,) is a Lauraceae family plant which have contents volatile oils which used as antimicrobial, anticancer on breast cancer, pesticide, antideppressants, antiinflammation, antioxidant, and neuro pharmacology. The extract was prepared using water with the soxhletation method. The antioxidant activity was determined with the 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2’-Azinobis [3-ethylbenzothiazoline-6)-sulfonic acid] -diammonium salt (ABTS) and Ferric Reducing Antioxidant Power (FRAP) methods. Total flavonoid and total phenolic content were determined with colorimetric methods. Antioxidant activity measured as IC50 was 23.37 ± 0.42 µg/mL; 111.21 ± 0.42 and 109.01 ± 0.28 respectively. The extract was found to contain high levels of total phenolic (282.93 ± 0.33 mg GAE/g) and total flavonoid 7.49 ± 0.51 mg QE/g). The results reveal that ethanol extract of Litsea cubeba Lour. Bark has antioxidant potential. The further analysis is to isolation antioxidant compound.


10.5219/1132 ◽  
2019 ◽  
Vol 13 (1) ◽  
pp. 515-523 ◽  
Author(s):  
Amina Aly ◽  
Rabab Maraei ◽  
Omneya Abou El-Leel

Berries are wealthy in bioactive compounds like phenolic compounds and flavonoids that are deemed antioxidants and are great important to health. This research was performed to examine, recognize and compare bioactive compounds in certain types of berries and their antioxidant activity. The data show that blue berry, black berry and Egyptian black mulberry contain the highest content of most bioactive compounds such as phenolic compounds, flavonoids and tannins, while long mulberry and red currant berry have the lowest content for most of these compounds. They therefore, contain the highest value of antioxidant activity. The chemical composition of the berries varies depending on cultivar, variety, location of growth, environmental conditions and harvest time, as well as post-harvest treatments therefore the composition differed from berry fruit to another. Thus, berry fruits are very useful in nutrition to protect the body from many diseases because of its containment of these compounds, which act as free radicals scavenger that harm the body and thus rid the body of many harmful toxins.


2019 ◽  
Vol 14 (5) ◽  
pp. 1934578X1984413 ◽  
Author(s):  
Soraia I. Falcão ◽  
Mélissa Lopes ◽  
Miguel Vilas-Boas

Propolis is a natural product derived from plant resins collected by honeybees and used in the beehive as a construction and defensive material. The broad spectrum of biological activities is dependent on the chemical diversity of its composition which is determined by the floral sources at the site of collection. For the first time, the chemical composition of Guinean propolis as well as its physicochemical properties, phenolic composition, and antioxidant activity was assessed. Eight compounds were identified through LC/DAD/ESI-MS n , mostly isoflavonoids, resembling Nigerian and Brazilian red propolis from the genus Dalbergia.


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