Unusual anti-inflammatory meroterpenoids from the marine sponge Dactylospongia sp.

2018 ◽  
Vol 16 (36) ◽  
pp. 6773-6782 ◽  
Author(s):  
Jing Li ◽  
Fan Yang ◽  
Zhuo Wang ◽  
Wei Wu ◽  
Li Liu ◽  
...  
Keyword(s):  
Marine Sponge ◽  
Inhibitory Effects ◽  
Anti Inflammatory

Nine new meroterpenoids, dactylospongins A–D, melemeleones C–E, dysidaminone N, and 19-O-methylpelorol, were isolated from the marine sponge Dactylospongia sp., which showed potent inhibitory effects on the production of IL-6, IL-1β, IL-8, and PEG2 in LPS-induced THP-1 cells with IC50 values of 5.1–9.2 μM.

Design, Synthesis and Pharmacological Evaluation of Novel Antiinflammatory and Analgesic O-Benzyloxime Compounds Derived From Natural Eugenol

2019 ◽  
Vol 16 (10) ◽  
pp. 1157-1166
Author(s):  
Rodrigo César da Silva ◽  
Fabiano Veiga ◽  
Fabiana Cardoso Vilela ◽  
André Victor Pereira ◽  
Thayssa Tavares da Silva Cunha ◽  
...  
Keyword(s):  
Formalin Test ◽  
Docking Studies ◽  
Paw Edema ◽  
Inhibitory Effects ◽  
Structural Pattern ◽  
Design Synthesis ◽  
Drug Candidates ◽  
Anti Inflammatory ◽  
Analgesic Activities ◽  
Cox 1

Background: : A new series of O-benzyloximes derived from eugenol was synthesized and was evaluated for its antinociceptive and anti-inflammatory properties. Methods: : The target compounds were obtained in good global 25-28% yields over 6 steps, which led us to identify compounds (Z)-5,6-dimethoxy-2,2-dimethyl-2,3-dihydro-1H-inden-1-one-O-(4- (methylthio)benzyloxime (8b), (Z)-5,6-dimethoxy-2,2-dimethyl-2,3-dihydro-1H-inden-1-one-O-4- bromobenzyloxime (8d) and (Z)-5,6-dimethoxy-2,2-dimethyl-2,3-dihydro-1H-inden-1-one-O-4- (methylsulfonyl)benzyloxime (8f) as promising bioactive prototypes. Results:: These compounds have significant analgesic and anti-inflammatory effects, as evidenced by formalin-induced mice paw edema and carrageenan-induced mice paw edema tests. In the formalin test, compounds 8b and 8f evidenced both anti-inflammatory and direct analgesic activities and in the carrageenan-induced paw edema, with compounds 8c, 8d, and 8f showing the best inhibitory effects, exceeding the standard drugs indomethacin and celecoxib. Conclusion: : Molecular docking studies have provided additional evidence that the pharmacological profile of these compounds may be related to inhibition of COX enzymes, with slight preference for COX-1. These results led us to identify the new O-benzyloxime ethers 8b, 8d and 8f as orally bioactive prototypes, with a novel structural pattern capable of being explored in further studies aiming at their optimization and development as drug candidates.

Assessment of Cota altissima (L.) J. Gay for phytochemical composition and antioxidant, anti-inflammatory, antidiabetic and antimicrobial activities

2021 ◽  
Vol 0 (0) ◽  
Author(s):  
Gamze Göger ◽  
Muhammed Allak ◽  
Ali Şen ◽  
Fatih Göger ◽  
Mehmet Tekin ◽  
...  
Keyword(s):  
Fatty Acids ◽  
Essential Oil ◽  
Antioxidant Activities ◽  
Antimicrobial Activities ◽  
Antidiabetic Activity ◽  
Gram Negative Bacteria ◽  
Inhibitory Effects ◽  
Dicaffeoylquinic Acid ◽  
Anti Inflammatory ◽  
Phytochemical Profiles

Abstract Phytochemical profiles of essential oil (EO), fatty acids, and n-hexane (CAH), diethyl ether (CAD), ethyl acetate (CAE) and methanol extracts (CAM) of Cota altissima L. J. Gay (syn. Anthemis altissima L.) were investigated as well as their antioxidant, anti-inflammatory, antidiabetic and antimicrobial activites. The essential oil was characterized by the content of acetophenone (35.8%) and β-caryophyllene (10.3%) by GC-MS/FID. Linoleic and oleic acid were found as main fatty acids. The major constituents of the extracts were found to be 5-caffeoylquinic acid, 3,5-dicaffeoylquinic acid, isorhamnetin glucoside, quercetin and quercetin glucoside by LC-MS/MS. Antioxidant activities of the extracts were determined by scavenging of DPPH and ABTS free radicals. Also, the inhibitory effects on lipoxygenase and α-glucosidase enzymes were determined. Antimicrobial activity was evaluated against Gram positive, Gram negative bacteria and yeast pathogens. CAM showed the highest antioxidant activity against DPPH and ABTS radicals with IC50 values of 126.60 and 144.40 μg/mL, respectively. In the anti-inflammatory activity, CAE demonstrated the highest antilipoxygenase activity with an IC50 value of 105.40 μg/mL, whereas, CAD showed the best inhibition of α-glucosidase with an IC50 value of 396.40 μg/mL in the antidiabetic activity. CAH was effective against Staphylococcus aureus at MIC = 312.5 µg/mL. This is the first report on antidiabetic, anti-inflammatory and antimicrobial activities of different extracts of C. altissima.

scholarly journals Isoquinolinequinone Derivatives from a Marine Sponge (Haliclona sp.) Regulate Inflammation in In Vitro System of Intestine

Marine Drugs ◽  
2021 ◽  
Vol 19 (2) ◽  
pp. 90
Author(s):  
Yun Kim ◽  
Yeong Ji ◽  
Na-Hyun Kim ◽  
Nguyen Van Tu ◽  
Jung-Rae Rho ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Marine Sponge ◽  
Nuclear Translocation ◽  
Hydroxyl Group ◽  
Subsequent Increase ◽  
Inflammatory Bowel ◽  
Anti Inflammatory ◽  
Key Functional Groups ◽  
Oxide Synthase

Using bio-guided fractionation and based on the inhibitory activities of nitric oxide (NO) and prostaglandin E2 (PGE2), eight isoquinolinequinone derivatives (1–8) were isolated from the marine sponge Haliclona sp. Among these, methyl O-demethylrenierate (1) is a noble ester, whereas compounds 2 and 3 are new O-demethyl derivatives of known isoquinolinequinones. Compound 8 was assigned as a new 21-dehydroxyrenieramycin F. Anti-inflammatory activities of the isolated compounds were tested in a co-culture system of human epithelial Caco-2 and THP-1 macrophages. The isolated derivatives showed variable activities. O-demethyl renierone (5) showed the highest activity, while 3 and 7 showed moderate activities. These bioactive isoquinolinequinones inhibited lipopolysaccharide and interferon gamma-induced production of NO and PGE2. Expression of inducible nitric oxide synthase, cyclooxygenase-2, and the phosphorylation of MAPKs were down-regulated in response to the inhibition of NF-κB nuclear translocation. In addition, nuclear translocation was markedly promoted with a subsequent increase in the expression of HO-1. Structure-activity relationship studies showed that the hydroxyl group in 3 and 5, and the N-formyl group in 7 may be key functional groups responsible for their anti-inflammatory activities. These findings suggest the potential use of Haliclona sp. and its metabolites as pharmaceuticals treating inflammation-related diseases including inflammatory bowel disease.

scholarly journals Anti-inflammatory and Matrix Metallopeptidase-1-Inhibitory Effects of the Cassia obtusifolia L. Seed Extract on Particulate Matter-induced Skin

2021 ◽  
Vol 19 (3) ◽  
pp. 355-363
Author(s):  
Jung-Wook Kang ◽  
In-Chul Lee
Keyword(s):  
Particulate Matter ◽  
Seed Extract ◽  
Enzyme Linked Immunosorbent Assay ◽  
No Production ◽  
Dependent Manner ◽  
Inhibitory Effects ◽  
Cassia Obtusifolia ◽  
Tnf Α ◽  
Matrix Metallopeptidase ◽  
Anti Inflammatory

Purpose: This study aimed to investigate the effects of the Cassia obtusifolia L. seed extract (CSE) on particulate matter (PM)-induced skin.Methods: The effects of CSE on cell viability were evaluated using a skin cell line. To determine the anti-inflammatory effects and matrix metallopeptidase-1 (MMP-1)-inhibitory effects of CSE on PM-induced skin, NO and MMP-1 expressions were measured using an enzyme-linked immunosorbent assay (ELISA) kit. Also, the effects of CSE was investigated the induction of IL-8 and TNF-α treated PM on reconstructed human full thickness skin models.Results: It was observed that CSE decreased NO production in PM-induced RAW 264.7 cells without cytotoxicity. In addition, CSE decreased the expression of MMP-1 in PM-induced cells in a dose-dependent manner. CSE decreased IL-8 and TNF-α production in a PM-reconstructed human skin model.Conclusion: These results indicate that CSE could be used as a cosmetic material to induce anti-inflammation and inhibition of MMP-1 in PM-induced skin.

scholarly journals Structural characterization, anti-inflammatory and glycosidase inhibitory activities of two new polysaccharides from the root of Pueraria lobata

RSC Advances ◽  
2021 ◽  
Vol 11 (57) ◽  
pp. 35994-36006
Author(s):  
Jiale Cai ◽  
Xiaoting Zhong ◽  
Jiayin Liang ◽  
Can Xu ◽  
Huanzheng Yu ◽  
...  
Keyword(s):  
Structural Characterization ◽  
Pueraria Lobata ◽  
Inhibitory Effects ◽  
Isolation And Purification ◽  
Molecular Weights ◽  
Inhibitory Activities ◽  
Anti Inflammatory

Through the extraction, isolation and purification of Pueraria lobata, we identified two new polysaccharides with molecular weights of 9.1 × 103 Da and 3.8 × 103 Da, and found that they have excellent anti-inflammatory and glycosidase inhibitory effects.

scholarly journals Phenolic Derivatives from Radix Astragali and their Anti-inflammatory Activities

2014 ◽  
Vol 9 (11) ◽  
pp. 1934578X1400901
Author(s):  
Wei Chen ◽  
Ying-Ying Zhang ◽  
Zhuo Wang ◽  
Xiao-Hua Luo ◽  
Wan-Chun Sun ◽  
...  
Keyword(s):  
Spectroscopic Analysis ◽  
Peritoneal Macrophages ◽  
Inos Mrna ◽  
Radix Astragali ◽  
Inhibitory Effects ◽  
Tnf Α ◽  
Cox 2 ◽  
Phenolic Derivatives ◽  
Anti Inflammatory ◽  
Mouse Peritoneal Macrophages

Two new (3, 4) and two known phenolic derivatives (1, 2) were isolated from Radix Astragali. The structures of 1–4 were elucidated by extensive spectroscopic analysis. The anti-inflammatory activities of the isolated compounds were evaluated in LPS-induced mouse peritoneal macrophages. All four compounds exhibited potent inhibitory effects on TNF-α production and TNF-α, COX-2, IL-1β, IL-6 and iNOS mRNA expression at 50 μM.

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