scholarly journals New Eunicellin-Type Diterpenes from the Panamanian Octocoral Briareum asbestinum

Marine Drugs ◽  
2020 ◽  
Vol 18 (2) ◽  
pp. 84 ◽  
Author(s):  
Marcelino Gutiérrez ◽  
Ricardo Santamaría ◽  
José Félix Gómez-Reyes ◽  
Héctor M. Guzmán ◽  
Javier Ávila-Román ◽  
...  
Keyword(s):  
Inflammatory Diseases ◽  
Biological Activities ◽  
Chemical Study ◽  
Inflammatory Activity ◽  
Bocas Del Toro ◽  
Chemical Structures ◽  
Wide Range ◽  
Marine Compounds ◽  
Anti Inflammatory ◽  
New Compounds

Gorgonian octocorals are considered a prolific source of secondary metabolites with a wide range of biological activities, including anti-inflammatory activity. In particular, the genus Briareum is known for producing a wealth of diterpenes with complex chemical structures. The chemical study of the methanolic extract of Briareum asbestinum collected in Bocas del Toro, on the Caribbean side of Panama, led to the isolation of three new eunicellin-type diterpenes: briarellin T (1), asbestinin 27 (2), asbestinin 28 (3) and the previously described asbestinin 17 (4). The structures of the new compounds were determined by extensive NMR analyses and HRMS. Anti-inflammatory activity assays showed a significant reduction of the pro-inflammatory cytokines TNF-α, IL-6, IL-1β and IL-8 as well as a downregulation of COX-2 expression in LPS-stimulated THP-1 macrophages. These findings support the potential use of these marine compounds as therapeutic agents in the treatment of inflammatory diseases.

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.

scholarly journals Inclusion Complexes of β and HPβ-Cyclodextrin with α, β Amyrin and In Vitro Anti-Inflammatory Activity

Biomolecules ◽  
2019 ◽  
Vol 9 (6) ◽  
pp. 241 ◽  
Author(s):  
Walter Ferreira da Silva Júnior ◽  
Danielle Lima Bezerra de Menezes ◽  
Luana Carvalho de Oliveira ◽  
Letícia Scherer Koester ◽  
Patrícia Danielle Oliveira de Almeida ◽  
...  
Keyword(s):  
Inclusion Complexes ◽  
Biological Activities ◽  
Physicochemical Characterization ◽  
Inflammatory Activity ◽  
Scanning Calorimetry ◽  
Promising Alternative ◽  
Wide Range ◽  
Natural Mixture ◽  
Anti Inflammatory

α, β amyrin (ABAM) is a natural mixture of pentacyclic triterpenes that has a wide range of biological activities. ABAM is isolated from the species of the Burseraceae family, in which the species Protium is commonly found in the Amazon region of Brazil. The aim of this work was to develop inclusion complexes (ICs) of ABAM and β-cyclodextrin (βCD) and hydroxypropyl-β-cyclodextrin (HPβCD) by physical mixing (PM) and kneading (KN) methods. Interactions between ABAM and the CD’s as well as the formation of ICs were confirmed by physicochemical characterization in the solid state by Fourier transform infrared (FTIR), scanning electron microscopy (SEM), X-ray diffraction (XRD), thermogravimetry (TG) and differential scanning calorimetry (DSC). Physicochemical characterization indicated the formation of ICs with both βCD and HPβCD. Such ICs were able to induce changes in the physicochemical properties of ABAM. In addition, the formation of ICs with cyclodextrins showed to be an effective and promising alternative to enhance the anti-inflammatory activity and safety of ABAM.

scholarly journals New Scabimycins A-C Isolated from Streptomyces acidiscabies (Lu19992)

Molecules ◽  
2021 ◽  
Vol 26 (19) ◽  
pp. 5922
Author(s):  
Constanze Paulus ◽  
Josef Zapp ◽  
Andriy Luzhetskyy
Keyword(s):  
Natural Products ◽  
Bioactive Peptides ◽  
Biological Activities ◽  
Powerful Source ◽  
Drug Candidates ◽  
Chemical Structures ◽  
Wide Range ◽  
Streptomyces Acidiscabies ◽  
New Compounds ◽  
Important Drug

Peptide natural products displaying a wide range of biological activities have become important drug candidates over the years. Microorganisms have been a powerful source of such bioactive peptides, and Streptomyces have yielded many novel natural products thus far. In an effort to uncover such new, meaningful compounds, the metabolome of Streptomyces acidiscabies was analyzed thoroughly. Three new compounds, scabimycins A–C (1–3), were discovered, and their chemical structures were elucidated by NMR spectroscopy. The relative and absolute configurations were determined using ROESY NMR experiments and advanced Marfey’s method.

scholarly journals Anti-Inflammatory Activity of Dried Ginger Mediated Iron Nanoparticles

2020 ◽  
pp. 14-19
Author(s):  
Sai Sree Lasya Ganta ◽  
M. Jeevitha ◽  
S. Preetha ◽  
S. Rajeshkumar
Keyword(s):  
Iron Nanoparticles ◽  
Size Range ◽  
Catalytic Properties ◽  
Inflammatory Diseases ◽  
Biological Activities ◽  
Inflammatory Activity ◽  
Inflammatory Agent ◽  
Vis Spectroscopy ◽  
Anti Inflammatory ◽  
Inflammatory Effect

Nanotechnology is a branch of science and technology relating to the matter on the atomic and molecular scale in the size range between 1-100 nm. Iron nanoparticles have diverse diagnostic and potential therapeutic applications with unique magnetic and catalytic properties and potent biological activities. The present study aimed to analyse the anti-inflammatory activity of iron nanoparticles synthesized from dried ginger. The synthesized iron nanoparticles were characterized using UV-vis spectroscopy and evaluated for anti-inflammatory activity by inhibition of albumin denaturation assay. The nanoparticles showed maximum absorbance at 360 nm and revealed potent anti-inflammatory effect with maximum of 83.5% inhibition at lowest concentration of 50 µl and thus can be used as an anti-inflammatory agent in various inflammatory diseases.

scholarly journals Heterocornols from the Sponge-Derived Fungus Pestalotiopsis heterocornis with Anti-Inflammatory Activity

Marine Drugs ◽  
2021 ◽  
Vol 19 (11) ◽  
pp. 585
Author(s):  
Hui Lei ◽  
Xiaoxu Bi ◽  
Xiuping Lin ◽  
Jianglian She ◽  
Xiaowei Luo ◽  
...  
Keyword(s):  
Chemical Study ◽  
Antimicrobial Activities ◽  
Sea Salt ◽  
Inflammatory Activity ◽  
Raw 264.7 Cells ◽  
Dependent Manner ◽  
Inos Protein Expression ◽  
Anti Inflammatory ◽  
New Compounds ◽  
Dose Dependent

One strain-many compounds (OSMAC) manipulation of the sponge-derived fungus Pestalotiopsis heterocornis XWS03F09 resulted in the production of new secondary metabolites. The chemical study of the fermentation, cultivated on 3% artificial sea salt in the rice media, led to the isolation of twelve compounds, including eight new polyketide derivatives, heterocornols Q–X (1–8), one new ceramide (9), and three known analogues (10–12). The structures and absolute configurations of the new compounds were elucidated by spectroscopic data and calculated ECD analysis. Heterocornols Q (1) and R (2) are novel 6/5/7/5 tetracyclic polyketide derivatives featuring dihydroisobenzofuran and benzo-fused dioxabicyclo [4.2.1] nonane system, which might be derived from the acetyl-CoA by epoxidation, polyene cyclization, and rearrangement to form the core skeleton. Compound 12 showed moderate or weak antimicrobial activities against with MIC values ranging from 25 to 100 μg/mL. Heterocornols T and X (7 and 8) could inhibit the production of LPS-induced NO significantly, comparable to dexamethasone. Further Western blotting analysis showed 7 and 8 markedly suppressed the iNOS protein expression in LPS-induced RAW 264.7 cells in a dose-dependent manner. The result showed that 7 and 8 might serve as potential leads for development of anti-inflammatory activity.

scholarly journals Phytochemical Evaluation and Anti-Inflammatory Activity of Ethanolic Extract of Calotropis procera Leaves

2020 ◽  
Vol 11 (1) ◽  
pp. 1-6
Author(s):  
Naveed Aslam Dogar ◽  
Hamza Shahid ◽  
Hafiz Usama Shaukat ◽  
M. Abubakar Khan ◽  
Farooq Saleem
Keyword(s):  
Inflammatory Diseases ◽  
Biological Activities ◽  
Diclofenac Sodium ◽  
Ethanolic Extract ◽  
Inflammatory Activity ◽  
Calotropis Procera ◽  
Anti Cancer ◽  
Ethanolic Extraction ◽  
Anti Inflammatory

Background: Medicinal plants have been used since centuries to cure various diseases. There is a huge potential to investigate the medicinal impacts of different parts of plants. Roots, stem, leaves and fruits of Calotropis procera are known for their biological activities. Calotropis procera plant shows multiple pharmacological activities like anti-cancer, anti-microbial, antioxidant, anti-malarial, hepatoprotective and anti-diabetic activities. Objectives: The objective of the current research was ethanolic extraction of Calotropis procera leaves and to study the phytochemistry and anti-inflammatory activity. Methodology: In this effort, we used the extract of Calotropis procera leaves for detection of phytochemicals and anti-inflammatory activity in vitro by hypotonicity induced hemolysis on 2% HRBC suspension, using UV-Vis spectrophotometer. Results: Phytochemicals like alkaloids, terpenoids, and flavonoids were present in large amount while tannins, saponins, steroids and cardiac glycosides were in small amount, whereas phlobatannins and anthraquinone were not detected. The potential of the ethanolic extract of Calotropis procera leaves was compared with Diclofenac sodium (100μl/ml, 200μl/ml). The leaves extract of Calotropis procera (100, 200, 300, 400, 500μl/ml each) showed significant anti-inflammatory activity by hypotonicity induced hemolysis on 2% HRBC suspension. Conclusion: The Calotropis procera leaves have potential to cure inflammatory diseases and can be used as anti-inflammatory medicine and analgesic.

Flavonolignan 2, 3-dehydroderivatives from Oenanthe javanica and their anti inflammatory activities

2021 ◽  
Vol 0 (0) ◽  
Author(s):  
Rong-Rui Wei ◽  
Qin-Ge Ma
Keyword(s):  
Data Analysis ◽  
Spectroscopic Data ◽  
Biological Activities ◽  
Inflammatory Activity ◽  
Macrophage Cells ◽  
Oenanthe Javanica ◽  
Anti Inflammatory ◽  
New Compounds ◽  
First Time ◽  
Raw264.7 Macrophage

Abstract Flavonolignans, for example, silymarin and silybin, have interesting biological activities. For the first time, three new flavonolignans named oenanthenoid A-C (1–3) and nine known flavonolignan derivatives (4–12) were isolated from Oenanthe javanica. Comprehensive spectroscopic data analysis and references were used to identify all of the compounds. The anti inflammatory activities of these isolates (1–12) on RAW264.7 macrophage cells were investigated. Three new compounds (1–3) demonstrated anti inflammatory activity with IC50 values ranging from 6.5 ± 0.6 to 14.7 ± 1.6 µM. Furthermore, two compounds (11 and 12) demonstrated moderate anti inflammatory activity, with IC50 values ranging from 24.1 ± 1.2 to 62.5 ± 1.9 µM.

Synthesis and Biological Evaluation of Andrographolide Derivatives as Anti-inflammatory Agent

2018 ◽  
Vol 24 (30) ◽  
pp. 3529-3533 ◽  
Author(s):  
Zeyu Zhu ◽  
Haibing Duan ◽  
Mei Jing ◽  
Lipeng Xu ◽  
Pei Yu
Keyword(s):  
Bacterial Infections ◽  
Inflammatory Diseases ◽  
Cell Activity ◽  
Biological Evaluation ◽  
Inflammatory Activity ◽  
Special Effects ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
New Compounds ◽  
Synthesis And Biological Evaluation

Background: Andrographolide (Andro) is a main active ingredient of the natural plant Andrographis paniculata, which has special effects on bacterial infections and inflammatory diseases. Objective: We previously synthesized Andrographolide derivatives AL-1 and investigated its anti-inflammatory activity. For further research, we decided to modify the structure of AL-1 and expected to have better antiinflammatory activity. Methods: By conjugating with anti-inflammatory and anti-bacterial group, we designed and synthesized the andrographolide derivative AL-2, AL-3 and AL-4. The anti-inflammatory activity of AL-2, AL-3 and AL-4 was also evaluated by detecting cell activity and Nitric Oxide (NO) release. <p> Results: The new compounds AL-2, AL-3 and AL-4 increased cell viability in lipopolysaccharide (LPS)-induced RAW 264.7 cell, which could have a certain anti-inflammatory activity, and inhibited the release of NO in cells to reduce the inflammatory response of cells. Conclusion: The new compounds AL-2, AL-3 and AL-4 may be candidates of anti-inflammatory drugs in the future.

A Convenient Synthesis, Reactions and Biological Activities of Some Novel Thieno[3,2-e]pyrazolo[3,4-b]pyrazine Compounds as Anti-microbial and Antiinflammatory Agents

2018 ◽  
Vol 15 (6) ◽  
pp. 863-871 ◽  
Author(s):  
Remon M. Zaki ◽  
Remon M. Zaki ◽  
Adel M. Kamal El-Dean ◽  
Adel M. Kamal El-Dean ◽  
Shaban M. Radwan ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Biological Activities ◽  
Ring Closure ◽  
Inflammatory Activity ◽  
Activity Data ◽  
E Coli ◽  
Chemical Structures ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
High Antifungal Activity

Aim and Objective: We reported in this manuscript, synthesis of novel pyrazolopyrazinothienopyrimidines. The o-amino-thienopyrazolopyrazine-carbonitrile 4 was used as a versatile precursor for synthesis of new heterocyclic compounds. Due to development of resistance to the current antimicrobial therapy and non-steroidal anti-inflammatory drugs (NSAIDs), continues research for more effective agents is interesting. Hence, the suspected promising biological activities of pyrazolopyrazine compounds persuaded us to study the anti-microbial and anti-inflammatory activities in comparison with standard drugs. Materials and Methods: The chemical structures of the newly synthesized compounds were confirmed by elemental and spectral analyses. Activities of the synthesized compounds against a number of Gram-negative and Gram-positive bacterial strains were investigated. The fungal strains were obtained from some cases of human dermatophytosis. The antimicrobial activities were determined according to the Kwon-Chung and Bennett method. Anti-inflammatory activity was evaluated using carrageenan induced paw edema method. Results: The antibacterial screening of the synthesized compounds represented that the o-amino-carbonitrile 4 and triazepinone 11 have the highest activity towards E. coli & S. aureus and S. pneumonia. The amino-imino 6 was very effective against E. coli. Ring closure of 6 to triazolopyrimidine 7 increases the antibacterial activity against E. coli & K. pneumonia, their inhibition zones were higher than ciprofloxacin. Also, the triazolopyrimidines 7 and 10 exhibited high antifungal activity against all tested strains. Compounds 6 and 11 revealed high antifungal activity against S. racemosum and T. rubrum. The anti-inflammatory activity data indicated that all the tested compounds 4, 6, 7, 10 & 11 revealed the highest anti-inflammatory effect after 4 hrs. of carrageenan injection. Conclusion: we found that most of the examined novel thieno- pyrazolopyrazine compounds exhibited promising antibacterial, antifungal and anti-inflammatory activities which can be used as potential antibacterial, antifungal and anti-inflammatory drugs.

Sulfonamides and Sulphonyl Ester of Quinolines as Non-Acidic, Non- Steroidal, Anti-inflammatory Agents

2020 ◽  
Vol 17 ◽  
Author(s):  
Bilquees Bano ◽  
Kanwal ◽  
Khalid Mohammed Khan ◽  
Almas Jabeen ◽  
Aisha Faheem ◽  
...  
Keyword(s):  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Inhibitory Effect ◽  
Inflammatory Activity ◽  
Spectroscopic Techniques ◽  
Wide Range ◽  
Anti Inflammatory ◽  
Hydroxy Quinoline ◽  
Synthetic Derivatives ◽  
Derivatives Of

Background:: Quinolines are important class of heterocyclic compounds possessing wide range of biological activities. Previously, we had identified Schiff bases of quinoline as potential anti-inflammatory agents, thus the current work is the continuation of our previous study. Objective:: In the current study 3-, 5-, and 8-sulfonamide and 8-sulfonate derivatives of quinoline (1-50) were synthesized and their antiinflammatory potential was evaluated. These synthetic analogs were evaluated for their anti-inflammatory activity via ROS (Reactive oxygen species) inhibitory effect produced from phagocytes from human whole blood. Methods:: The sulfonamide and sulfonate derivatives of quinoline were synthesized via treating 5-, 3-, 8-amino, and 8-hydroxy quinoline with different substituted sulfonyl chlorides in pyridine. The synthetic molecules were characterized using various spectroscopic techniques and screened for their anti-inflammatory potential. Results and Discussion:: Among the synthetic derivatives 1-50, six compounds showed good to moderate anti-inflammatory activity. Compounds 47 (IC50 = 2.9 ± 0.5 μg/mL), 36 (IC50 = 3.2 ± 0.2 μg/mL), and 24 (IC50 = 6.7 ± 0.3 μg/mL) exhibited enhanced activity as compared to the standard ibuprofen (IC50 = 11.2 ± 1.9 μg/mL). Compounds 20 (IC50 = 25.5 ± 0.7 μg/mL), 50 (IC50 = 42.9 ± 5.6 μg/mL), and 8 (IC50 = 53.9 ± 3.1 μg/mL) were moderately active, however, rest of the compounds were found to be inactive. Conclusion:: The sulfonamide and sulfonate derivatives of quinoline were found to have promising anti-inflammatory activity. Further studies on the modification of these molecules may leads to the discovery of new and potential anti-inflammatory agents.

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