scholarly journals Assessment of the Potential Biological Activity of Low Molecular Weight Metabolites of Freshwater Macrophytes with QSAR

Scientifica ◽  
2016 ◽  
Vol 2016 ◽  
pp. 1-9 ◽  
Author(s):  
Evgeny A. Kurashov ◽  
Elena V. Fedorova ◽  
Julia V. Krylova ◽  
Galina G. Mitrukova

The paper focuses on the assessment of the spectrum of biological activities (antineoplastic, anti-inflammatory, antifungal, and antibacterial) with PASS (Prediction of Activity Spectra for Substances) for the major components of three macrophytes widespread in the Holarctic species of freshwater, emergent macrophyte with floating leaves,Nuphar lutea(L.) Sm., and two species of submergent macrophyte groups,Ceratophyllum demersumL. andPotamogeton obtusifolius(Mert. et Koch), for the discovery of their ecological and pharmacological potential. The predicted probability of anti-inflammatory or antineoplastic activities above 0.8 was observed for twenty compounds. The same compounds were also characterized by high probability of antifungal and antibacterial activity. Six metabolites, namely, hexanal, pentadecanal, tetradecanoic acid, dibutyl phthalate, hexadecanoic acid, and manool, were a part of the major components of all three studied plants, indicating their high ecological significance and a certain universalism in their use by various species of water plants for the implementation of ecological and biochemical functions. This report underlines the role of identified compounds not only as important components in regulation of biochemical and metabolic pathways and processes in aquatic ecological systems, but also as potential pharmacological agents in the fight against different diseases.

Author(s):  
Md Abu Bakar Siddiq

Gout is the most common form of inflammatory arthritis. Hyperuricaemia is the pre-requisite for gout and is influenced by variable modifiable and non-modifiable risk factors. Clinical features unique for gout are due to deposition of monosodium urate (MSU) crystal in articular and extra articular tissues. Among various treating agents, anti-inflammatory drugs and urate lowering therapies (ULT) are used widely and successfully, however, non-medicinal means are also effective in the disorder. In their updated guidelines, ACR (2012) and EULAR (2016) recommended both medicinal and non-medicinal approaches that could be used in treating gout, though some of the recommendations are based on lower level of evidence. Moreover, researchers’ continued effort in finding new gout managing agents appear promising, for example, role of Lesinurad in gout management (CLEAR1, CLEAR2). In this new synthesis the author is aimed to provide updated information on gout management based on a systematic review including published work within last ten years between 2008 and 2018 and for this purpose, using ‘clinical trials in gout management’ string, published worked searched in PubMed database from 1st September 2018 to 30 October 2018. Besides the recent ACR and EULAR evidence based management guidelines, the author reviewed another 91 (total 93) articles to make this new draft – 39 articles describe role of pharmacological agents and 54 describe different gout risks, pharmacokinetics/pharmacodynamics of ULT, association between raised sUA level and renal impairment, efficacy of non-pharmacological agents in reducing sUA. According to published work, anti-inflammatory agent is the most appropriate drug group in mitigating inflammatory symptoms of gout, though they often adversely affect over other vital 2 organs with impaired function. Besides ULT, uricase analogues are also found useful in non refractory gout. Since anti-inflammatory agents and ULT contraindicate in some clinical conditions, intra-articular steroid and or adrenocorticotropic hormone (ACTH) are appropriate alternatives instead. However, head-to-head comparison between different NSAIDs, NSAID and prednisolone, NSAID and colchicine are yet to perform. Use of combined anti-inflammatory preparations in gout is also based on lower level of evidence. Regarding effective maximum dose and long-standing impact of ULT on vital organs we are yet to reach a conclusion. Likewise, non-medicinal approaches are widely using in achieving target sUA level, though some of them are based on biased study outcomes and or study with inadequate power, requiring further analysis. Among non-pharmacological approaches, life-style modification, restriction of purine rich diets, avoidance of gout inciting agents are important, but inconclusive. Educating patients’ about diseases, risk factors, available treatment options and side effects from them are also important in terms of achieving sUA level, nevertheless too much counseling sometimes could be worthless.


2021 ◽  
Vol 11 (4) ◽  
pp. 141-148
Author(s):  
Noman Anwar ◽  
N. Zaheer Ahmed ◽  
Shehnaz Begum

The current pandemic caused by SARS-CoV-2 has led to a massive change in every aspect of our lives. It has grossly affected the healthcare system, business and world trade, disruption of movement and supply of essential goods and has crippled the global economy. Although few vaccines have been approved for the control of disease, targeted therapy options for this virulent disease still remain limited and elusive. Exhaustive search for potent therapeutic candidate is in progress, for which herbal armory are also being explored. Medicinal plants and their products play a vital role in alleviating various diseases and have been reported to exhibit a wide range of biological activities. Plant-based drugs with antiviral, anti-inflammatory and immunomodulotry activities were hypothetically considered as potential drugs to prevent and mitigate the prevailing situation caused by SARS-CoV-2. Arq Ajīb ‘a Unani formulation’ presents compelling approach in treating numerous diseases. The ingredients of Arq Ajīb and their phytocompounds have been reported for wide-ranging pharmaco-biological activities including antiviral, anti-inflammatory, immunomodulotry, anti-allergic, antitussive and bronchodilatory activities. Scientific data available on the formulation ingredients and their phytocompounds indicates that the formulation may have a significant role in augmenting the immune status of individual, protecting them from infection and providing symptomatic relief to patients affected with COVID-19. Hence, it may be considered as a potential drug for the development of novel therapeutic candidate for SARS-CoV-2 infection. This multi-faceted review highlights the therapeutic significance and pharmacological actions of Arq Ajīb and its ingredients to demonstrate the plausible role of the formulation in combating COVID-19. Keywords: Arq Ajīb, COVID-19, Pudina, Ajwain, Camphor, Unani formulation


1980 ◽  
Vol 44 (01) ◽  
pp. 006-008 ◽  
Author(s):  
D Bergqvist ◽  
K-E Arfors

SummaryIn a model using an isolated rabbit mesenteric preparation microvessels were transected and the time until haemostatic plugs formed was registered. Perfusion of platelet rich plasma gave no haemostasis whereas whole blood did. Addition of chlorpromazine or adenosine to the whole blood significantly prolonged the time for haemostasis, and addition of ADP to the platelet rich plasma significantly shortened it. It is concluded that red cells are necessary for a normal haemostasis in this model, probably by a combination of a haemodynamic and ADP releasing effect.The fundamental role of platelets in haemostatic plug formation is unquestionable but there are still problems concerning the stimulus for this process to start. Three platelet aggregating substances have been discussed – thrombin, adenosine diphosphate (ADP) and collagen. Evidence speaking in favour of thrombin is, however, very minimal, and the discussion has to be focused on collagen and ADP. In an in vitro system using polyethylene tubings we have shown that "haemostasis" can be obtained without the presence of collagen but against these results can be argued that it is only another in vitro test for platelet aggregation (1).To be able to induce haemostasis in this model, however, the presence of red blood cells is necessary. To further study this problem we have developed a model where haemostatic plug formation can be studied in the isolated rabbit mesentery and we have briefly reported on this (2).Thus, it is possible to perfuse the vessels with whole blood as well as with platelet rich plasma (PRP) and different pharmacological agents of importance.


2019 ◽  
Author(s):  
Chem Int

Coumarin and its derivatives are widely spread in nature. Coumarin goes to agroup as benzopyrones, which consists of a benzene ring connected to a pyronemoiety. Coumarins displayed a broad range of pharmacologically useful profile.Coumarins are considered as a promising group of bioactive compounds thatexhibited a wide range of biological activities like anti-microbial, anti-viral,antiparasitic, anti-helmintic, analgesic, anti-inflammatory, anti-diabetic, anticancer,anti-oxidant, anti-proliferative, anti-convulsant, and antihypertensiveactivities etc. The coumarin compounds have immense interest due to theirdiverse pharmacological properties. In particular, these biological activities makecoumarin compounds more attractive and testing as novel therapeuticcompounds.


2019 ◽  
Author(s):  
Chem Int

A series of heterocyclic compounds incorporating pyridazine moiety were for diverse biological activities. Pyridazines and pyridazinones derivatives showed wide spectrum of biological activities such as vasodialator, cardiotonic, anticonvulsant, antihypertensive, antimicrobial, anti-inflammatory, analgesic, anti-feedant, herbicidal, and various other biological, agrochemical and industrial chemical activities. The results illustrated that the synthesized pyridazine/pyridazine compounds have diverse and significant biological activities. Mechanistic insights into the biological properties of pyridazinone derivatives and various synthetic techniques used for their synthesis are also described.


2019 ◽  
Author(s):  
A. EL Moussaoui ◽  
F. Jawhari ◽  
K. EL Ouahdani ◽  
I. Es-Safi ◽  
D. Bousta ◽  
...  

Our present study focuses on the evaluation of the analgesic, anti-inflammatory and healing activity of Withania frutescens L. The anti-inflammatory result has an inhibition percentage of 78.87% ± 7.08 at 450 mg/kg and 75.14% ± 6.39 at 400 mg/kg and 89.75% ± 3.44 for diclofenac (1%). When applied locally, the 10% cream has an inflammation inhibition of 96.87% ± 5.85 and 76.14% ± 7.88 for the 5% cream with 89.87 ± 6.20 of reference (Indomethacin). The abdominal contractions of rats treated with the root extract are significantly lower than those of the control group that received only physiological NaCl solution, with 41.20 ± 2.30 for the extract and 82.20 ± 5.04 for NaCl and 53.40 ± 4.94 for the reference. The healing activity of the studied extract records a percentage of contraction of about 93.20% ± 3.36 (Extract 10%), 84.50% ± 3.84 (Extract 5%), 48.47% ± 2.15 (control) and 81.88 ± 2.24 for the reference.


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