scholarly journals Research Advances and Prospects on Mechanism of Sinomenin on Histamine Release and the Binding to Histamine Receptors

2018 ◽  
Vol 20 (1) ◽  
pp. 70 ◽  
Author(s):  
Yu-Shi Zhang ◽  
Jia-Yin Han ◽  
Omer Iqbal ◽  
Ai-Hua Liang

Sinomenine (SIN) is widely used in China to treat a variety of rheumatic diseases (RA), and has various pharmacological effects such as anti-inflammatory, analgesic, and anti-tumor effects. However, due to the histamine release characteristics of SIN, its adverse reactions such as allergic reactions, gastrointestinal reactions, and circulatory systemic reactions have been drawing increasing attention. We present here a systematic review of the chemical structure, pharmacological effects, clinical application, and adverse reactions of SIN, a detailed discussion on the relationship between histamine/histamine receptor and mechanism of action of SIN. In addition, we simulated the binding of SIN to four histamine receptors by using a virtual molecular docking method and found that the bonding intensity between SIN and receptors varied in the order shown as follows: H1R > H2R ~ H3R > H4R. The docking results suggested that SIN might exhibit dual regulatory effects in many processes such as cyclooxygenase-2 (COX-2) expression, NF-κB pathway activation, and degranulation of mast cells to release histamine, thereby exhibiting pro-inflammatory (adverse reactions)/anti-inflammatory effects. This study provides a theoretical basis for the clinical treatment of inflammations seen such as in RA using SIN, and also suggests that SIN has great potential in the field of cancer treatment and will have very important social and economic significance.

2019 ◽  
Vol 70 (7) ◽  
pp. 2534-2537
Author(s):  
Gladiola Tantaru ◽  
Mihai Apostu ◽  
Antonia Poiata ◽  
Mihai Nichifor ◽  
Nela Bibire ◽  
...  

The paper presents the synthesis of a new complex combination of a Bis-Schiff base with Mn(II) ions with great potential for antimicrobial and anti-inflammatory activity. A new complex of the Salen-type ligand, 1-ethyl-salicylidene-bis-ethylene diamine was synthetized using Mn(II) ions. The chemical structure was confirmed through 1H-NMR and IR spectroscopy. The antimicrobial activities of the Bis-Schiff base and its complex were tested in comparison with Ampicillin, Chloramphenicol, Tetracycline, Ofloxacin and Nystatin. Those compounds were found to be active against Gram-positive or Gram-negative bacteria, and had an anti-inflammatory effect comparable to that of Indomethacin.


Molecules ◽  
2021 ◽  
Vol 26 (9) ◽  
pp. 2745
Author(s):  
Peng Du ◽  
Jia Song ◽  
Huirui Qiu ◽  
Haorui Liu ◽  
Li Zhang ◽  
...  

Shanxi-aged vinegar, a traditional Chinese grain-fermented food that is rich in polyphenols, has been shown to have therapeutic effects on a variety of diseases. However, there has been no comprehensive evaluation of the anti-inflammatory activity of polyphenols extracted from Shanxi-aged vinegar (SAVEP) to date. The anti-inflammatory activities of SAVEP, both in RAW 264.7 macrophages and mice, were extensively investigated for the potential application of SAVEP as a novel anti-inflammatory agent. In order to confirm the notion that polyphenols could improve inflammatory symptoms, SAVEP was firstly detected by gas chromatography mass spectrometry (GC-MS). In total, 19 polyphenols were detected, including 12 phenolic acids. The study further investigated the protective effect of SAVEP on lipopolysaccharide-induced inflammation in RAW264.7 macrophages and ICR mice. The results showed that compared with those of the model group, SAVEP could remarkably recover the inflammation of macrophage RAW264.7 and ICR mice. SAVEP can normalise the expression of related proteins via the suppression of MAPK/NF-κB pathway activation, inhibiting the expression of iNOS and COX-2 proteins, and consequently the production of inflammatory factors, thus alleviating inflammatory stress. These results suggest that SAVEP may have a potential function against inflammation.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1184
Author(s):  
Armin Mooranian ◽  
Thomas Foster ◽  
Corina M Ionescu ◽  
Daniel Walker ◽  
Melissa Jones ◽  
...  

Introduction: Recent studies in our laboratory have shown that some bile acids, such as chenodeoxycholic acid (CDCA), can exert cellular protective effects when encapsulated with viable β-cells via anti-inflammatory and anti-oxidative stress mechanisms. However, to explore their full potential, formulating such bile acids (that are intrinsically lipophilic) can be challenging, particularly if larger doses are required for optimal pharmacological effects. One promising approach is the development of nano gels. Accordingly, this study aimed to examine biological effects of various concentrations of CDCA using various solubilising nano gel systems on encapsulated β-cells. Methods: Using our established cellular encapsulation system, the Ionic Gelation Vibrational Jet Flow technology, a wide range of CDCA β-cell capsules were produced and examined for morphological, biological, and inflammatory profiles. Results and Conclusion: Capsules’ morphology and topographic characteristics remained similar, regardless of CDCA or nano gel concentrations. The best pharmacological, anti-inflammatory, and cellular respiration, metabolism, and energy production effects were observed at high CDCA and nano gel concentrations, suggesting dose-dependent cellular protective and positive effects of CDCA when incorporated with high loading nano gel.


2021 ◽  
Vol 338 ◽  
pp. 109425
Author(s):  
Yijia Xu ◽  
Wenwen Li ◽  
Yunuo Han ◽  
Hongyu Liu ◽  
Suli Zhang ◽  
...  

2022 ◽  
Vol 146 ◽  
pp. 354-364
Author(s):  
Meryem Slighoua ◽  
Ismail Mahdi ◽  
Fatima ez-zahra Amrati ◽  
Nabil Boucetta ◽  
Francesca Di Cristo ◽  
...  

2018 ◽  
Vol 26 (1) ◽  
pp. 8-18
Author(s):  
Min Sun Kim ◽  
Nam Seok Kim ◽  
Jin Kwon ◽  
Ha Rim Kim ◽  
Da Young Lee ◽  
...  

Author(s):  
M. L. Maksimov ◽  
N. M. Kiseleva ◽  
D. G. Semenikhin ◽  
B. K. Romanov

Non-steroidal anti-inflammatory drugs (NSAIDs) are included in a pharmacological group of drugs with different chemical structures providing anti-inflammatory, analgesic and antipyretic actions, as well as antiplatelet action to a certain degree. Unfortunately, NSAIDs can cause a wide range of adverse reactions (AR) posing a serious risk to the health and life of patients. Therefore, the rational use of NSAIDs should include methods for effective prevention of drug complications. Many NSAIDs have a pronounced therapeutic effect, simultaneously causing many undesirable effects, so the drug shall be chosen considering the development of predicted side effects and modern algorithms. According to clinical recommendations, risk factors and administration of safer NSAIDs shall be considered as the main prevention method. Besides, it is possible to protect the patient from the upper gastrointestinal tract complications using proton pump inhibitors. It should be noted that there are no effective medication methods for kidney and liver protection to reduce the risk of NSAID-associated complications.


2014 ◽  
Vol 63 (7) ◽  
pp. 569-580 ◽  
Author(s):  
Natássia Albuquerque Ribeiro ◽  
Ticiana Monteiro Abreu ◽  
Hellíada Vasconcelos Chaves ◽  
Mirna Marques Bezerra ◽  
Helena Serra Azul Monteiro ◽  
...  

2021 ◽  
Vol 12 ◽  
Author(s):  
Jiaji Hu ◽  
Hanglu Ying ◽  
Jie Yao ◽  
Longhe Yang ◽  
Wenhui Jin ◽  
...  

Nonalcoholic steatohepatitis (NASH) has become one of the serious causes of chronic liver diseases, characterized by hepatic steatosis, hepatocellular injury, inflammation and fibrosis, and lack of efficient therapeutic agents. Palmitoylethanolamide (PEA) is an endogenous bioactive lipid with various pharmacological activities, including anti-inflammatory, analgesic, and neuroprotective effects. However, the effect of PEA on nonalcoholic steatohepatitis is still unknown. Our study aims to explore the potential protective role of PEA on NASH and to reveal the underlying mechanism. In this study, the C57BL/6 mice were used to establish the NASH model through methionine- and choline-deficient (MCD) diet feeding. Here, we found that PEA treatment significantly improved liver function, alleviated hepatic pathological changes, and attenuated the lipid accumulation and hepatic fibrosis in NASH mice induced by MCD diet feeding. Mechanistically, the anti-steatosis effect of PEA may be due to the suppressed expression of ACC1 and CD36, elevated expression of PPAR-α, and the phosphorylation levels of AMPK. In addition, hepatic oxidative stress was greatly inhibited in MCD-fed mice treated with PEA via enhancing the expression and activities of antioxidant enzymes, including GSH-px and SOD. Moreover, PEA exerted a clear anti-inflammatory effect though ameliorating the expression of inflammatory mediators and suppressing the NLRP3 inflammasome pathway activation. Furthermore, the impaired autophagy in MCD-induced mice was reactivated with PEA treatment. Taken together, our research suggested that PEA protects against NASH through the inhibition of inflammation and restoration of autophagy. Thus, PEA may represent an efficient therapeutic agent to treat NASH.


2021 ◽  
Vol 5 (2) ◽  
pp. 96-101
Author(s):  
V.B. Vasilyuk ◽  
◽  
G.I. Syraeva ◽  
M.V. Faraponova ◽  
◽  
...  

Gout is one of the most common forms of inflammatory arthritis. Medical care for gout includes non-steroidal anti-inflammatory drugs (NSAIDs). This paper reviews the efficacy and safety of NSAIDs prescribed for the acute attack of gout, in particular, AMBENIUM® parenteral. It was demonstrated that phenylbutazone is a powerful NSAID that provides significant analgesic and anti-inflammatory effects. Considering a broad spectrum of adverse reactions of NSAIDs, these agents should be prescribed and used under in-depth analysis of patient’s condition, comorbidities and the level of their decompensation, and potential drug interactions. In addition, optimal dosages and duration of NSAID treatment are of particular importance. The authors conclude that AMBENIUM® parenteral is an effective and safe therapeutic modality for gout. Its profile and risk/benefit ratio are regarded as “favorable” compared to other NSAIDs. KEYWORDS: gout, arthritis, pain, non-steroidal anti-inflammatory drugs, parenteral, efficacy, safety. FOR CITATION: Vasilyuk V.B., Syraeva G.I., Faraponova M.V. Efficacy and safety of non-steroidal anti-inflammatory drugs for acute attack of gout. Russian Medical Inquiry. 2021;5(2):96–101. DOI: 10.32364/2587-6821-2021-5-2-96-101.


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