scholarly journals Virtual Screening in Pharmacokinetics, Bioactivity, and Toxicity of the Amburana cearensis Secondary Metabolites

2021 ◽  
Vol 12 (6) ◽  
pp. 8471-8491
Keyword(s):  
Secondary Metabolites ◽  
Phenolic Acids ◽  
Stem Bark ◽  
New Drugs ◽  
Structure Property ◽  
In Vivo Models ◽  
Popular Medicine ◽  
Anti Inflammatory

Bioprospecting has contributed to the work of pharmaceutical chemists in the development and commercial disposal of new drugs. Currently, the pharmaceutical industry has emphasized drugs produced from bioactive compounds extracted from natural sources, based on popular medicine discussed in the literature, such as secondary metabolites isolated from the stem bark and seeds of the Amburana cearensis, rich in coumarin derivatives, flavonoids, and phenolic acids and is popularly used in the treatment of respiratory diseases and with anti-inflammatory and antioxidant bioactivity. This review is a study of the structure/activity and structure/property (SAR/SPA) relationship with the physicochemical properties calculated by the algorithms of the MarvinSketch software for the secondary metabolites of A. cearensis, as well as their correlation with in silico test values the SwissADME and admetSAR 2.0 servers and in vitro and in vivo models of the dataset from the PreADMET, GUSAR Online and PASS Online servers. The results showed that substances derived from coumarin, flavonoids, and phenolic acids have attributes of good permeability and low efflux, which favor their oral bioavailability, since phenolic heterosides, amburoside analogs, and biflavonoids are effective in local action as subcutaneous application, constituting promising antimicrobial, anti-inflammatory and antioxidant therapeutic actions in their proper administration routes.

scholarly journals Seaweed Secondary Metabolites with Beneficial Health Effects: An Overview of Successes in In Vivo Studies and Clinical Trials

Marine Drugs ◽  
2019 ◽  
Vol 18 (1) ◽  
pp. 8 ◽  
Author(s):  
Gonçalo P. Rosa ◽  
Wilson R. Tavares ◽  
Pedro M. C. Sousa ◽  
Aida K. Pagès ◽  
Ana M. L. Seca ◽  
...  
Keyword(s):  
Clinical Trials ◽  
Secondary Metabolites ◽  
New Drugs ◽  
In Vivo Studies ◽  
In Vivo Model ◽  
In Vivo Models ◽  
Obesity And Diabetes ◽  
Development In Vitro

Macroalgae are increasingly viewed as a source of secondary metabolites with great potential for the development of new drugs. In this development, in vitro studies are only the first step in a long process, while in vivo studies and clinical trials are the most revealing stages of the true potential and limitations that a given metabolite may have as a new drug. This literature review aims to give a critical overview of the secondary metabolites that reveal the most interesting results in these two steps. Phlorotannins show great pharmaceutical potential in in vivo models and, among the several examples, the anti-dyslipidemia activity of dieckol must be highlighted because it was more effective than lovastatin in an in vivo model. The IRLIIVLMPILMA tridecapeptide that exhibits an in vivo level of activity similar to the hypotensive clinical drug captopril should still be stressed, as well as griffithsin which showed such stunning results over a variety of animal models and which will probably move onto clinical trials soon. Regarding clinical trials, studies with pure algal metabolites are scarce, limited to those carried out with kahalalide F and fucoxanthin. The majority of clinical trials currently aim to ascertain the effect of algae consumption, as extracts or fractions, on obesity and diabetes.

Natural Anti-inflammatory compounds as Drug candidates in Alzheimer’s disease

2020 ◽  
Vol 27 ◽  
Author(s):  
Reyaz Hassan Mir ◽  
Abdul Jalil Shah ◽  
Roohi Mohi-ud-din ◽  
Faheem Hyder Potoo ◽  
Mohd. Akbar Dar ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Natural Products ◽  
Protective Action ◽  
New Drugs ◽  
Huperzine A ◽  
Brain Disorder ◽  
Anti Inflammatory

: Alzheimer's disease (AD) is a chronic neurodegenerative brain disorder characterized by memory impairment, dementia, oxidative stress in elderly people. Currently, only a few drugs are available in the market with various adverse effects. So to develop new drugs with protective action against the disease, research is turning to the identification of plant products as a remedy. Natural compounds with anti-inflammatory activity could be good candidates for developing effective therapeutic strategies. Phytochemicals including Curcumin, Resveratrol, Quercetin, Huperzine-A, Rosmarinic acid, genistein, obovatol, and Oxyresvertarol were reported molecules for the treatment of AD. Several alkaloids such as galantamine, oridonin, glaucocalyxin B, tetrandrine, berberine, anatabine have been shown anti-inflammatory effects in AD models in vitro as well as in-vivo. In conclusion, natural products from plants represent interesting candidates for the treatment of AD. This review highlights the potential of specific compounds from natural products along with their synthetic derivatives to counteract AD in the CNS.

A Review on Opuntia Species and its Chemistry, Pharmacognosy, Pharmacology and Bioapplications

2020 ◽  
Vol 16 (8) ◽  
pp. 1227-1244
Author(s):  
Dharmendra Kumar ◽  
Pramod K. Sharma
Keyword(s):  
Human Consumption ◽  
In Vivo Models ◽  
Sugar Amino Acids ◽  
Opuntia Species ◽  
Therapeutic Uses ◽  
Anti Inflammatory ◽  
Online Library ◽  
Different Parts

Background:: Opuntia species, locally known as prickly pear was used for various purposes as food, medicine, beverage, source of dye and animal food. Many studies have revealed its pharmacology activity from time to time. This review is a collection of chemistry, pharmacognosy, pharmacology and bioapplications of the cactus family. Methods: Many sources were used to collect information about Opuntia species such as Pub med, Google scholar, Agris, science direct, Embase, Merk index, Wiley online library, books and other reliable sources. This review contains studies from 1812 to 2019. Results: The plants from the cactus family offer various pharmacological active compounds including phenolic compounds, carotenoids, betalains, vitamins, steroids, sugar, amino acids, minerals and fibers. These bioactive compounds serve various pharmacological activities such as anticancer, antiviral, anti-diabetic, Neuroprotective, anti-inflammatory, antioxidant, Hepatoprotective, antibacterial, antiulcer and alcohol hangover. According to various studies, Opuntia species offer many bioapplications such as fodder for animal, soil erosion, prevention, human consumption and waste water decontamination. Finally, different parts of plants are used in various formulations that offer many biotechnology applications. Conclusion: Different parts of Opuntia plant (fruits, seeds, flowers and cladodes) are used in various health problems which include wound healing, anti-inflammatory and urinary tract infection from ancient times. Nowadays, researches have extended several pharmacological and therapeutic uses of Opuntia species as discussed in this review. Many in-vitro and in-vivo models are also discussed in this review as the proofs of research findings. Various research gaps have been observed in current studies that require attention in the future.

scholarly journals Anti-Inflammatory Potential of Daturaolone from Datura innoxia Mill.: In Silico, In Vitro and In Vivo Studies

2021 ◽  
Vol 14 (12) ◽  
pp. 1248
Author(s):  
Muhammad Waleed Baig ◽  
Humaira Fatima ◽  
Nosheen Akhtar ◽  
Hidayat Hussain ◽  
Mohammad K. Okla ◽  
...  
Keyword(s):  
In Silico ◽  
Therapeutic Potential ◽  
In Vivo Studies ◽  
Metabolic Reaction ◽  
Datura Innoxia ◽  
In Vivo Models ◽  
Immobility Time ◽  
Anti Inflammatory

Exploration of leads with therapeutic potential in inflammatory disorders is worth pursuing. In line with this, the isolated natural compound daturaolone from Datura innoxia Mill. was evaluated for its anti-inflammatory potential using in silico, in vitro and in vivo models. Daturaolone follows Lipinski’s drug-likeliness rule with a score of 0.33. Absorption, distribution, metabolism, excretion and toxicity prediction show strong plasma protein binding; gastrointestinal absorption (Caco-2 cells permeability = 34.6 nm/s); no blood–brain barrier penetration; CYP1A2, CYP2C19 and CYP3A4 metabolism; a major metabolic reaction, being aliphatic hydroxylation; no hERG inhibition; and non-carcinogenicity. Predicted molecular targets were mainly inflammatory mediators. Molecular docking depicted H-bonding interaction with nuclear factor kappa beta subunit (NF-κB), cyclooxygenase-2, 5-lipoxygenase, phospholipase A2, serotonin transporter, dopamine receptor D1 and 5-hydroxy tryptamine. Its cytotoxicity (IC50) value in normal lymphocytes was >20 µg/mL as compared to cancer cells (Huh7.5; 17.32 ± 1.43 µg/mL). Daturaolone significantly inhibited NF-κB and nitric oxide production with IC50 values of 1.2 ± 0.8 and 4.51 ± 0.92 µg/mL, respectively. It significantly reduced inflammatory paw edema (81.73 ± 3.16%), heat-induced pain (89.47 ± 9.01% antinociception) and stress-induced depression (68 ± 9.22 s immobility time in tail suspension test). This work suggests a possible anti-inflammatory role of daturaolone; however, detailed mechanistic studies are still necessary to corroborate and extrapolate the findings.

scholarly journals ANTI-INFLAMMATORY ACTIVITY OF KNEMA ATTENUATA (HOOK. F. AND THOMSON) WARB ETHANOLIC STEM BARK EXTRACT IN ALBINO WISTAR RATS

2019 ◽  
pp. 330-334
Author(s):  
SUPRIYA RAJA H
Keyword(s):  
Stem Bark ◽  
Inflammatory Activity ◽  
Assay Method ◽  
Bark Extract ◽  
Raw 264.7 ◽  
Myeloperoxidase Activity ◽  
Stem Bark Extract ◽  
Anti Inflammatory

Objective: Knema attenuata (Myristicaceae), popularly known as “wild nutmeg,” is an endemic tree species from Western Ghats, which has been used in folk medicine. Conventionally, the stem bark of K. attenuata is used for treating inflammatory conditions without any scientific information available for the same. The present study was undertaken to evaluate the anti-inflammatory activity of the ethanolic stem bark extract (ESBE) of K. attenuata using in vivo and in vitro screening models. Methods: The ethanolic extract of stem bark was prepared by soxhlation, and its cytotoxicity in RAW 264.7 cell line was assessed using MTT assay method. In vivo anti-inflammatory effect of extract was estimated in rats using carrageenan-induced paw edema model and cotton pellet-induced granuloma model. The in vitro anti-inflammatory activity of the extract was evaluated by cyclooxygenase and lipoxygenase inhibition assay, estimation of myeloperoxidase activity, and determination of cellular nitrite levels in lipopolysaccharide-stimulated RAW 264.7 macrophage cells. Results: Toxic symptoms were not observed for the ESBE. The extract demonstrated significant anti-inflammatory activity in both in vivo and in vitro models. The anti-inflammatory action exhibited by the extract was a result of the inhibition of leukocyte migration and nitric oxide pathway and partially by inhibition of mediators such as prostaglandins and leukotrienes. Conclusion: Findings from the study provide the evidence for the popular use of stem bark extract of K. attenuata as a potential anti-inflammatory agent.

Anti-inflammatory, anti-proliferative and anti-atherosclerotic effects of quercetin in human in vitro and in vivo models

2011 ◽  
Vol 218 (1) ◽  
pp. 44-52 ◽  
Author(s):  
Robert Kleemann ◽  
Lars Verschuren ◽  
Martine Morrison ◽  
Susanne Zadelaar ◽  
Marjan J. van Erk ◽  
...  
Keyword(s):  
In Vivo Models ◽  
Anti Inflammatory

Probiotic yeast Kluyveromyces marxianus CIDCA 8154 shows anti-inflammatory and anti-oxidative stress properties in in vivo models

2016 ◽  
Vol 7 (1) ◽  
pp. 83-93 ◽  
Author(s):  
D.E. Romanin ◽  
S. Llopis ◽  
S. Genovés ◽  
P. Martorell ◽  
V.D. Ramón ◽  
...  
Keyword(s):  
Oxidative Stress ◽  
Kluyveromyces Marxianus ◽  
Intestinal Inflammation ◽  
In Vivo Models ◽  
Benzene Sulfonic Acid ◽  
Bowel Diseases ◽  
Probiotic Yeast ◽  
Anti Inflammatory

Inflammatory bowel diseases (IBDs) are complex affections with increasing incidence worldwide. Multiple factors are involved in the development and maintenance of the symptoms including enhanced oxidative stress in intestinal mucosa. The conventional therapeutic approaches for IBDs are based on the use anti-inflammatory drugs with important collateral effects and partial efficacy. In the present work we tested the anti-inflammatory capacity of Kluyveromyces marxianus CIDCA 8154 in different models. In vitro, we showed that the pretreatment of epithelial cells with the yeast reduce the levels of intracellular reactive oxygen species. Furthermore, in a murine model of trinitro benzene sulfonic acid-induced colitis, yeast-treated animals showed a reduced histopathological score (P<0.05) and lower levels of circulating interleukin 6 (P<0.05). The capacity to modulate oxidative stress in vivo was assessed using a Caenorhabditis elegans model. The yeast was able to protect the nematodes from oxidative stress by modulating the SKN-1 transcription factor trough the DAF-2 pathway. These results indicate that K. marxianus CIDCA 8154 could control the intestinal inflammation and cellular oxidative stress. Deciphering the mechanisms of action of different probiotics might be useful for the rational formulation of polymicrobial products containing microorganisms targeting different anti-inflammatory pathways.

scholarly journals In vitro and In vivo Models for Anti-inflammation: An Evaluative Review

2019 ◽  
pp. 3-15 ◽  
Author(s):  
Fabian Ifeanyi Eze ◽  
Philip F. Uzor ◽  
Peter Ikechukwu ◽  
Bonaventure C. Obi ◽  
Patience O. Osadebe
Keyword(s):  
Inflammatory Activity ◽  
Assay Method ◽  
In Vivo Models ◽  
Synthetic Drugs ◽  
Mediators Of Inflammation ◽  
In Vivo Animal Models ◽  
Anti Inflammatory ◽  
Anti Inflammation

Anti-inflammatory activity study involves developing a model that mimics, or provokes the production or release of, the biochemical mediators of inflammation, and monitoring the response of these biochemicals to the test drugs. This report constitutes an updated review of the in vitro and in vivo study models for assessing anti-inflammatory activity in plant extracts and synthetic drugs. The materials, instrumentation, and methods involved, as well as the mechanism of anti-inflammatory activity tested in each model, are extensively described. The merits and limitations of each method have also been discussed. A comparative assessment of the in vivo animal models vis-à-vis, the in vitro enzyme models have been made to assist scientists and researchers in the choice of assay method in terms of sensitivity, reliability, duration of test, ethical, and cost considerations.

scholarly journals Prohibitin‐1 Is a Dynamically Regulated Blood Protein With Cardioprotective Effects in Sepsis

2021 ◽  
Author(s):  
Taylor A. Mattox ◽  
Christine Psaltis ◽  
Katie Weihbrecht ◽  
Jacques Robidoux ◽  
Brita Kilburg‐Basnyat ◽  
...  
Keyword(s):  
Mitochondrial Dysfunction ◽  
Blood Protein ◽  
Nuclear Factor ◽  
In Vivo Models ◽  
Endotoxin Challenge ◽  
Atp Production ◽  
Anti Inflammatory ◽  
Prohibitin 1

Background In sepsis, circulating cytokines and lipopolysaccharide elicit mitochondrial dysfunction and cardiomyopathy, a major cause of morbidity and mortality with this condition. Emerging research places the PHB1 (lipid raft protein prohibitin‐1) at the nexus of inflammation, metabolism, and oxidative stress. PHB1 has also been reported in circulation, though its function in this compartment is completely unknown. Methods and Results Using a wide‐ranging approach across multiple in vitro and in vivo models, we interrogated the functional role of intracellular and circulating PHB1 in the heart during sepsis, and elucidated some of the mechanisms involved. Upon endotoxin challenge or sepsis induction in rodent models, PHB1 translocates from mitochondria to nucleus in cardiomyocytes and is secreted into the circulation from the liver in a manner dependent on nuclear factor (erythroid‐derived 2)‐like 2, a key transcriptional regulator of the antioxidant response. Overexpression or treatment with recombinant human PHB1 enhances the antioxidant/anti‐inflammatory response and protects HL‐1 cardiomyocytes from mitochondrial dysfunction and toxicity from cytokine stress. Importantly, administration of recombinant human PHB1 blunted inflammation and restored cardiac contractility and ATP production in mice following lipopolysaccharide challenge. This cardioprotective, anti‐inflammatory effect of recombinant human PHB1 was determined to be independent of nuclear factor (erythroid‐derived 2)‐like 2, but partially dependent on PI3K/AKT  signaling in the heart. Conclusions These findings reveal a previously unknown cardioprotective effect of PHB1 during sepsis, and illustrate a pro‐survival, protective role for PHB1 in the circulation. Exploitation of circulating PHB1 as a biomarker and/or therapeutic could have widespread benefit in the clinical management of sepsis and other severe inflammatory disorders.

scholarly journals Medium Chain Triglyceride (MCT) Oil Affects the Immunophenotype via Reprogramming of Mitochondrial Respiration in Murine Macrophages

Foods ◽  
2019 ◽  
Vol 8 (11) ◽  
pp. 553 ◽  
Author(s):  
Yu ◽  
Go ◽  
Kim
Keyword(s):  
Inflammatory Responses ◽  
Medium Chain Triglyceride ◽  
Metabolic Reprogramming ◽  
Activation Markers ◽  
In Vivo Models ◽  
Medium Chain ◽  
Anti Inflammatory ◽  
Alternatively Activated

Medium chain triglyceride (MCT) oil has been postulated to modulate inflammatory responses, but the detailed mechanisms have not been fully elucidated. Based on recent studies demonstrating that mitochondrial metabolic reprogramming and immune responses are correlated, the current study sought to determine whether MCT oil controls inflammatory responses through modulation of mitochondria using both in vitro and in vivo models. The mitochondrial metabolic phenotypes of macrophages were assessed according to oxygen consumption rate (OCR). Inflammatory responses were assessed for production of cytokines and expression of activation markers. MCT oil was more rapidly oxidized as observed by increased OCR in macrophages. The production of pro-inflammatory cytokines was down-regulated and anti-inflammatory cytokine was elevated by MCT oil. In addition, classically activated M1 and alternatively activated M2 markers were reciprocally regulated by MCT intervention. Overall, up-regulated β-oxidation by MCT contributes to the anti-inflammatory M2-like status of macrophages, which may aid in the dietary prevention and/or amelioration of inflammation.

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