An Overview of Novel Bioactive Compounds with Potent Anti-Inflammatory Activity via Dual COX-2 and 5-LOX Enzyme Inhibition

2021 ◽  
Vol 18 ◽  
Author(s):  
Roopal Mittal ◽  
Shailesh Sharma ◽  
Ajay Singh Kushwah
Keyword(s):  
Bioactive Compounds ◽  
Enzyme Inhibitors ◽  
World Health Organisation ◽  
The Body ◽  
Inflammatory Activity ◽  
World Health ◽  
Quality Data ◽  
The World ◽  
Cox 2 ◽  
Anti Inflammatory

Background: Inflammation is the earliest body defence mechanism in which the immune system recognises and counters the antigens and aids in healing the disease. The World Health Organisation suggests that inflammation is one of the greatest causes of death in the world. Inflammation could be acute or chronic due to the release of inflammatory mediators i.e. prostaglandins, leukotrienes due to mitogens, antigens or cytokines found in the body. Methods: Bibliographic database using pub med cites for peer-reviewed research articles with titles containing dual COX-2 and 5-LOX enzyme inhibitors, heterocyclic moieties, with AND Boolean operator's terms since last ten years of literature work. The quality papers containing the natural or synthetic lead compounds were extracted; the detailed study and conceptual framework attracted its attention. Results: Out of 127 research and review articles evaluated, 54 articles were cited to provide high quality data regarding pharmacoactive molecules having anti-inflammatory activity via dual COX-2/5-LOX inhibition. In addition, highlighting their in silico and experimental wet laboratory studies in increasing order over the past decade with the best illustration of dual enzyme inhibitory activity. Conclusion: This review gathered details of isolated bioactive compounds such as pyrazole, coumaperine, indoles, phenanthrene derivatives that have been significantly reported for anti-inflammatory activities.

scholarly journals Sargassum Seaweed as a Source of Anti-Inflammatory Substances and the Potential Insight of the Tropical Species: A Review

Marine Drugs ◽  
2019 ◽  
Vol 17 (10) ◽  
pp. 590 ◽  
Author(s):  
Saraswati ◽  
Puspo Edi Giriwono ◽  
Diah Iskandriati ◽  
Chin Ping Tan ◽  
Nuri Andarwulan
Keyword(s):  
Bioactive Compounds ◽  
Optimal Growth ◽  
The Body ◽  
Inflammatory Activity ◽  
Sulfated Polysaccharides ◽  
Tropical Species ◽  
Tropical Region ◽  
Inflammatory Conditions ◽  
Microbial Infections ◽  
Anti Inflammatory

Sargassum is recognized both empirically and scientifically as a potential anti-inflammatory agent. Inflammation is an important response in the body that helps to overcome various challenges to body homeostasis such as microbial infections, tissue stress, and certain injuries. Excessive and uncontrolled inflammatory conditions can affect the pathogenesis of various diseases. This review aims to explore the potential of Sargassum’s anti-inflammatory activity, not only in crude extracts but also in sulfated polysaccharides and purified compounds. The tropical region has a promising availability of Sargassum biomass because its climate allows for the optimal growth of seaweed throughout the year. This is important for its commercial utilization as functional ingredients for both food and non-food applications. To the best of our knowledge, studies related to Sargassum’s anti-inflammatory activity are still dominated by subtropical species. Studies on tropical Sargassum are mainly focused on the polysaccharides group, though there are some other potentially bioactive compounds such as polyphenols, terpenoids, fucoxanthin, fatty acids and their derivatives, typical polar lipids, and other groups. Information on the modulation mechanism of Sargassum’s bioactive compounds on the inflammatory response is also discussed here, but specific mechanisms related to the interaction between bioactive compounds and targets in cells still need to be further studied.

A Collaborative Study to Establish the Second International Standard for Streptokinase

1990 ◽  
Vol 64 (02) ◽  
pp. 267-269 ◽  
Author(s):  
A B Heath ◽  
P J Gaffney
Keyword(s):  
High Purity ◽  
Collaborative Study ◽  
World Health Organisation ◽  
World Health ◽  
Clot Lysis ◽  
Current Standard ◽  
International Standard ◽  
Accelerated Degradation ◽  
The World ◽  
International Collaborative Study

SummaryAn International Standard for Streptokinase - Streptodomase (62/7) has been used to calibrate high purity clinical batches of SK since 1965. An international collaborative study, involving six laboratories, was undertaken to replace this standard with a high purity standard for SK. Two candidate preparations (88/826 and 88/824) were compared by a clot lysis assay with the current standard (62/7). Potencies of 671 i.u. and 461 i.u. were established for preparations A (88/826) and B (88/824), respectively.Either preparation appeared suitable to serve as a standard for SK. However, each ampoule of preparation A (88/826) contains a more appropriate amount of SK activity for potency testing, and is therefore preferred. Accelerated degradation tests indicate that preparation A (88/826) is very stable.The high purity streptokinase preparation, coded 88/826, has been established by the World Health Organisation as the 2nd International Standard for Streptokinase, with an assigned potency of 700 i.u. per ampoule.

HIPEREMESIS GRAVIDARUM PADA IBU HAMIL DI KLINIK BIDAN SUPRIYATI SRIBIT BERBAH SLEMAN

2019 ◽  
Vol 14 (1) ◽  
pp. 51
Author(s):  
Pramukti Dian Setianingrum ◽  
Farah Irmania Tsani
Keyword(s):  
Blood Pressure ◽  
Pregnant Women ◽  
Hyperemesis Gravidarum ◽  
Unwanted Pregnancy ◽  
The Body ◽  
Nausea And Vomiting ◽  
Daily Activities ◽  
World Health ◽  
The World

Backgroud: The World Health Organization (WHO) explained that the number of Hyperemesis Gravidarum cases reached 12.5% of the total number of pregnancies in the world and the results of the Demographic Survey conducted in 2007, stated that 26% of women with live births experienced complications. The results of the observations conducted at the Midwife Supriyati Clinic found that pregnant women with hyperemesis gravidarum, with a comparison of 10 pregnant women who examined their contents there were about 4 pregnant women who complained of excessive nausea and vomiting. Objective: to determine the hyperemesis Gravidarum of pregnant mother in clinic. Methods: This study used Qualitative research methods by using a case study approach (Case Study.) Result: The description of excessive nausea of vomiting in women with Hipermemsis Gravidarum is continuous nausea and vomiting more than 10 times in one day, no appetite or vomiting when fed, the body feels weak, blood pressure decreases until the body weight decreases and interferes with daily activities days The factors that influence the occurrence of Hyperemesis Gravidarum are Hormonal, Diet, Unwanted Pregnancy, and psychology, primigravida does not affect the occurrence of Hyperemesis Gravidarum. Conclusion: Mothers who experience Hyperemesis Gravidarum feel nausea vomiting continuously more than 10 times in one day, no appetite or vomiting when fed, the body feels weak, blood pressure decreases until the weight decreases and interferes with daily activities, it is because there are several factors, namely, hormonal actors, diet, unwanted pregnancy, and psychology.

Comparative docking of SARS-CoV-2 receptors antagonists from repurposing drugs

2020 ◽  
Author(s):  
Micael Davi Lima de Oliveira ◽  
Kelson Mota Teixeira de Oliveira
Keyword(s):  
World Health Organisation ◽  
World Health ◽  
Lung Cells ◽  
The Novel ◽  
High Modulation ◽  
Main Protease ◽  
The World ◽  
Novel Coronavirus ◽  
Viral Receptors ◽  
Theoretical Results

According to the World Health Organisation, until 16 June, 2020, the number of confirmed and notified cases of COVID-19 has already exceeded 7.9 million with approximately 434 thousand deaths worldwide. This research aimed to find repurposing antagonists, that may inhibit the activity of the main protease (Mpro) of the SARS-CoV-2 virus, as well as partially modulate the ACE2 receptors largely found in lung cells, and reduce viral replication by inhibiting Nsp12 RNA polymerase. Docking molecular simulations were performed among a total of 60 structures, most of all, published in the literature against the novel coronavirus. The theoretical results indicated that, in comparative terms, paritaprevir, ivermectin, ledipasvir, and simeprevir, are among the most theoretical promising drugs in remission of symptoms from the disease. Furthermore, also corroborate indinavir to the high modulation in viral receptors. The second group of promising drugs includes remdesivir and azithromycin. The repurposing drugs HCQ and chloroquine were not effective in comparative terms to other drugs, as monotherapies, against SARS-CoV-2 infection.

Use of Phosphatidylcholine in the Treatment of Localized Fat Deposits. Results and expectations

2017 ◽  
Vol 68 (7) ◽  
pp. 1438-1441 ◽  
Author(s):  
Sorin Berbece ◽  
Dan Iliescu ◽  
Valeriu Ardeleanu ◽  
Alexandru Nicolau ◽  
Radu Cristian Jecan
Keyword(s):  
World Health Organisation ◽  
Normal Weight ◽  
World Health ◽  
Basic Substance ◽  
Physical Exercises ◽  
Fat Deposits ◽  
The World ◽  
The Common ◽  
Global Health Problem ◽  
Over Time

Obesity represents a global health problem. According to the latest studies released by the World Health Organisation (WHO), 1.7 billion currently in excess of normal weight individuals, of which approx. 75% are overweight (body mass index - BMI 25 to 30). The common form of excess adipose tissue manifestation in overweight individuals is localized fat deposits with high (abdominal) or low (buttocks and thighs) disposition. Although the overweight can be corrected relatively easy by changing behavioral habits or food, a constant physical exercises program or following a diet food are not accessible to all through the efforts of will, financial and time involved. Several methods have been studied and tested over time to eliminate more or less invasive fat deposits with varying efficacy and adverse effects. Chemical lipolysis using phosphatidylcholine as the basic substance was initially used in hypercholesterolemia and its complications and was rapidly adopted in mesotherapy techniques for the treatment of fat deposits. This study reveals the results obtained using Dermastabilon on a sample of 16 patients, the time allocated to treatment and discomfort being minimal, and rapid and notable results. There were no side effects.

The Undiscovered Potential of Essential Oils for Treating SARS-CoV-2 (COVID-19)

2020 ◽  
Vol 26 (41) ◽  
pp. 5261-5277
Author(s):  
Peter J. Wilkin ◽  
Minnatallah Al-Yozbaki ◽  
Alex George ◽  
Girish K. Gupta ◽  
Cornelia M. Wilson
Keyword(s):  
Essential Oils ◽  
Clinical Symptoms ◽  
Synergistic Effects ◽  
World Health Organisation ◽  
Diagnostic Techniques ◽  
World Health ◽  
Clinical Aspects ◽  
Traditional Use ◽  
In Silico Studies ◽  
The World

On 11th March 2020, the World Health Organisation (WHO) announced a pandemic caused by a novel beta-coronavirus SARS-CoV-2, designated COVID-19. The virus emerged in December 2019 in Wuhan, China, has spread across the world as a global pandemic. The traditional use of medicines from plants can be traced back to 60,000 years. Global interest in the development of drugs from natural products has increased greatly during the last few decades. Essential oils (EOs) have been studied through the centuries and are known to possess various pharmaceutical properties. In the present review, we have highlighted the current biology, epidemiology, various clinical aspects, different diagnostic techniques, clinical symptoms, and management of COVID-19. An overview of the antiviral action of EOs, along with their proposed mechanism of action and in silico studies conducted, is described. The reported studies of EOs' antiviral activity highlight the baseline data about the additive and/or synergistic effects among primary or secondary phytoconstituents found in individual oils, combinations or blends of oils and between EOs and antiviral drugs. It is hoped that further research will provide better insights into EOs' potential to limit viral infection and aid in providing solutions through natural, therapeutically active agents.

Design, Synthesis, Characterization and in silico molecular docking studies and in vivo anti-inflammatory Activity of Pyrazoline clubbed Thiazolinone Derivatives

2020 ◽  
Vol 17 ◽  
Author(s):  
Deepak Kumar Singh ◽  
Mayank Kulshreshtha ◽  
Yogesh Kumar ◽  
Pooja A Chawla ◽  
Akash Ved ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Biological Activities ◽  
Inflammatory Activity ◽  
Standard Drug ◽  
Docking Score ◽  
Chemical Structures ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Cox 1

Background: The pyrazolines give the reactions of aliphatic derivatives, resembling unsaturated compounds in their behavior towards permanganate and nascent hydrogen. This nucleus has been associated with various biological activities including inflammatory. Thiazolinone is a heterocyclic compound that contains both sulfur and nitrogen atom with a carbonyl group in their structure.Thiazolinone and their derivatives have attracted continuing interest because of their various biological activities, such as anti-inflammatory, antimicrobial, anti-proliferative, antiviral, anticonvulsant etc. The aim of the research was to club pyrazoline nucleus with thiazolinone in order to have significantanti-inflammatory activity. The synthesized compounds were chemically characterized for the establishment of their chemical structures and to evaluate as anti-inflammatory agent. Method: In the present work, eight derivatives of substituted pyrazoline (PT1-PT8) were synthesized by a three step reaction.The compounds were subjected to spectral analysis by Infrared, Mass and Nuclear magnetic resonance spectroscopy and elemental analysis data. All the synthesized were evaluated for their in vivo anti-inflammatory activity. The synthesized derivatives were evaluated for their affinity towards target COX-1 and COX-2, using indomethacin as the reference compound molecular docking visualization through AutoDock Vina. Results: Compounds PT-1, PT-3, PT-4 and PT-8 exhibited significant anti-inflammatory activity at 3rd hour being 50.7%, 54.3%, 52.3% and 57% respectively closer to that of the standard drug indomethacin (61.9%).From selected anti-inflammatory targets, the synthesized derivatives exhibited better interaction with COX-1 and COX-2 receptor, where indomethacin showed docking score of -6.5 kJ/mol, compound PT-1 exhibited highest docking score of -9.1 kJ/mol for COX-1 and compound PT-8 having docking score of 9.4 kJ/mol for COX-2. Conclusion: It was concluded that synthesized derivatives have more interaction with COX-2 receptors in comparison to the COX-1 receptors because the docking score with COX-2 receptors were very good. It is concluded that the synthesized derivatives (PT-1 to PT-8) are potent COX-2 inhibitors.

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