Anti-inflammatory effect and potential mechanism of betulinic acid on λ-carrageenan-induced paw edema in mice

Ou, Zhaoping; Zhao, Jing; Zhu, Lijuan; Huang, Lin; Ma, Yurong; Ma, Chaoyang; Luo, Chenxi; Zhu, Zihan; Yuan, Zhihang; Wu, Jing; Li, Rongfang; Yi, Jine

doi:10.1016/j.biopha.2019.109347

Cited by 98 publications

(70 citation statements)

References 39 publications

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“…Betulinic acid, a lupane-type triterpenoid, as one of the main compounds in LF, showed good antiin ammatory and analgesic effect [4]. According to the results of our preliminary research, LF showed good inhibitory effect on RA rats, suggesting that LF may be used as a potential anti-RA drug.…”

Section: Introductionmentioning

confidence: 71%

Network pharmacology-based identification of potential targets of Triterpenoids from Liquidambaris Fructus on the treatment of Rheumatoid Arthritis

Li¹,

Qian²,

Li³

et al. 2020

Preprint

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Background Rheumatoid arthritis (RA) is a chronic inflammatory autoimmune disease, and its exact etiology and pathogenesis are still unclear by now, therefore it is urgent to develop new therapeutic targets for RA treatment. Liquidambaris Fructus (LF) is used for joint pain, numbness and edema, and triterpenoids, the main effective compounds of LF, have a clear anti-inflammatory effect. The aim of this study was to clarify the mechanism of triterpenoids from LF on the treatment of RA. Methods A comprehensive network pharmacology strategy that consists of three sequential modules (pharmacophore matching, enrichment analysis and molecular docking) was carried out. Results We collected 21 triterpenoids from LF and predicted 61 targets strongly correlated with 15 biological processes and 8 related pathways. SYK and MAPK14 were key targets related to triterpenoids from LF and RA. LCK and GSK3B were potential targets and two effective triterpenoids from LF played a crucial role in the process of RA by targeting LCK and GSK3B. Conclusions The comprehensive strategy can serve as a universal method to illuminate the mechanism of triterpenoids from LF acting on treatment of RA by identifying the targets and pathways, and provided new ideas for RA treatment and evidence for clinical research and application of LF.

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Section: Introductionmentioning

confidence: 71%

Network pharmacology-based identification of potential targets of Triterpenoids from Liquidambaris Fructus on the treatment of Rheumatoid Arthritis

Li¹,

Qian²,

Li³

et al. 2020

Preprint

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“…Our results demonstrated that AE extract was able to inhibit the increase of paw edema due to CAR injection. Acute inflammation, due to CAR injection, caused in the paw a deterioration of muscle fibers and inflammatory cell infiltration [ 55 ]. However, the administration of AE extract visibly reduced the histological damage induced by CAR, decreasing the morphological alterations of tissue architecture and the presence of neutrophil infiltrate that was also confirmed by MPO level [ 56 ], a local mediator of tissue damage and the resulting inflammation in many inflammatory diseases [ 48 , 57 ].…”

Section: Discussionmentioning

confidence: 99%

Properties of a New Food Supplement Containing Actinia equina Extract

et al. 2020

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Marine species represent a great source of biologically active substances; Actinia equina (AE), an Anthozoa Cnidaria belonging to the Actinidiae family, have been proposed as original food and have already been included in several cooking recipes in local Mediterranean shores, and endowed with excellent nutraceutical potential. The aim of this study was to investigate some unexplored features of AE, through analytical screening and an in-vitro and in-vivo model. An in-vitro study, made on RAW 264.7 stimulated with H2O2, showed that the pre-treatment with AE exerted an antioxidant action, reducing lipid peroxidation and up-regulating antioxidant enzymes. On the other hand, the in-vivo study over murine model demonstrated that the administration of AE extracts is able to reduce the carrageenan (CAR)-induced paw edema. Furthermore, the histological damage due to the neutrophil infiltration is prevented, and this highlights precious anti-inflammatory features of the interesting food-stuff. Moreover, it was assessed that AE extract modulated nuclear factor kappa-light-chain-enhancer of activated B cells (NF-kB) and The nuclear factor erythroid 2–related factor 2 (Nrf-2) pathways. In conclusion, our data demonstrated that thanks to the antioxidant and anti-inflammatory properties, AE extract could be used as a new food supplement for inflammatory pathology prevention.

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“…COX-2 is the enzyme responsible for the peroxidation reactions that will generate prostaglandins [46,47]. PGE2 is one of the main mediators involved in the appearance of the inflammatory process signs and symptoms, causing increased vascular permeability, vasodilation and edema, in addition to increasing the sensitivity of nociceptive endings, causing pain [48,49]. IL-1β is associated with increased excitability and sensitization of nociceptive endings, in addition to inducing apoptosis processes during inflammatory and carcinogenic responses.…”

Section: Biological Activitymentioning

confidence: 99%

(E)-2-Cyano-3-(1H-Indol-3-yl)-N-Phenylacrylamide, a Hybrid Compound Derived from Indomethacin and Paracetamol: Design, Synthesis and Evaluation of the Anti-Inflammatory Potential

Silva

Almeida

Silva

et al. 2020

IJMS

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The compound (E)-2-cyano-3-(1H-indol-3-yl)-N-phenylacrylamide (ICMD-01) was designed and developed based on the structures of clinically relevant drugs indomethacin and paracetamol through the molecular hybridization strategy. This derivative was obtained by an amidation reaction between substituted anilines and ethyl 2-cyanoacetate followed by a Knoevenagel-type condensation reaction with indole aldehyde that resulted in both a viable synthesis and satisfactory yield. In order to assess the immunomodulatory and anti-inflammatory activity, in vitro assays were performed in J774 macrophages, and significant inhibitions (p < 0.05) of the production of nitrite and the production of cytokines (IL-1β and TNFα) in noncytotoxic concentrations were observed. The anti-inflammatory effect was also studied via CFA-induced paw edema in vivo tests and zymosan-induced peritonitis. In the paw edema assay, ICMD01 (50 mg kg−1) showed satisfactory activity, as did the group treated with dexamethasone, reducing edema in 2–6 h. In addition, there was no significant inhibition of PGE2, IL-1β or TNFα in vivo. Moreover, in the peritonitis assay that assesses leukocyte migration, ICMD-01 exhibited promising results. Therefore, these preliminary studies demonstrate this compound to be a strong candidate for an anti-inflammatory drug together with an improved gastrointestinal safety profile when compared to the conventional anti-inflammatory drugs.

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Anti-inflammatory effect and potential mechanism of betulinic acid on λ-carrageenan-induced paw edema in mice

Cited by 98 publications

References 39 publications

Network pharmacology-based identification of potential targets of Triterpenoids from Liquidambaris Fructus on the treatment of Rheumatoid Arthritis

Network pharmacology-based identification of potential targets of Triterpenoids from Liquidambaris Fructus on the treatment of Rheumatoid Arthritis

Properties of a New Food Supplement Containing Actinia equina Extract

(E)-2-Cyano-3-(1H-Indol-3-yl)-N-Phenylacrylamide, a Hybrid Compound Derived from Indomethacin and Paracetamol: Design, Synthesis and Evaluation of the Anti-Inflammatory Potential

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