Jaboticabin and Related Polyphenols from Jaboticaba (Myrciaria cauliflora) with Anti-inflammatory Activity for Chronic Obstructive Pulmonary Disease

2019 ◽  
Vol 67 (5) ◽  
pp. 1513-1520 ◽  
Author(s):  
Da-Ke Zhao ◽  
Ya-Na Shi ◽  
Vanya Petrova ◽  
Grace G. L. Yue ◽  
Adam Negrin ◽  
...  
Author(s):  
Rahel L. Birru ◽  
Kiflai Bein ◽  
Natalya Bondarchuk ◽  
Heather Wells ◽  
Qiao Lin ◽  
...  

Bacterial infections contribute to accelerated progression and severity of chronic obstructive pulmonary disease (COPD). Apples have been associated with reduced symptoms of COPD and disease development due to their polyphenolic content. We examined if phloretin, an apple polyphenol, could inhibit bacterial growth and inflammation induced by the main pathogens associated with COPD. Phloretin displayed bacteriostatic and anti-biofilm activity against nontypeable Haemophilus influenzae (NTHi), Moraxella catarrhalis, Streptococcus pneumoniae, and to a lesser extent, Pseudomonas aeruginosa. In vitro, phloretin inhibited NTHi adherence to NCI-H292 cells, a respiratory epithelial cell line. Phloretin also exhibited anti-inflammatory activity in COPD pathogen-induced RAW 264.7 macrophages and human bronchial epithelial cells derived from normal and COPD diseased lungs. In mice, NTHi bacterial load and chemokine (C-X-C motif) ligand 1 (CXCL1), a neutrophil chemoattractant, was attenuated by a diet supplemented with phloretin. Our data suggests that phloretin is a promising antimicrobial and anti-inflammatory nutraceutical for reducing bacterial-induced injury in COPD.


2021 ◽  
Vol 31 (4) ◽  
pp. 518-529
Author(s):  
E. A. Orlova ◽  
I. P. Dorfman ◽  
M. A. Orlov ◽  
A. K. Andreeva ◽  
M. A. Abdullaev

The choice of drugs used to treat patients with chronic obstructive pulmonary disease (COPD) (inhaled β-agonists, M-anticholinergic drugs, inhaled corticosteroids (ICS)) in view of their interchangeability is reviewed in this article. This aspect is especially important for clinicians when choosing an effective and safe treatment for COPD and for increasing patient adherence to treatment.The aim of this study was to assess the ratio of the number of reference (original), interchangeable, and generic drugs used in COPD.Methods. In accordance with the Russian clinical guidelines 2018 and GOLD 2019, modern drugs for the treatment of COPD with bronchodilator and anti-inflammatory activity were selected. All trade names of the corresponding drugs for each international non-proprietary name (INN) In the State Register of Medicines website were considered. The information on the availability of reference (original) drugs and the corresponding interchangeable products, as well as their presence in the List of vital and essential drugs was analyzed.Results. A large number of generic prodcuts are registered in the State Register of Medicines, and only a few of them are interchangeable with the corresponding reference (original) drug.Conclusion. The analysis will help widen the doctors’ choice of interchangeable drugs in treatment of COPD with an equivalent effect and safety of reference drugs, as well as to increase the patients’ adherence to treatment.


2013 ◽  
Vol 20 (2) ◽  
pp. 117-120 ◽  
Author(s):  
Parameswaran Nair

Airway inflammation is a central feature of many airway diseases such as asthma, chronic bronchitis, bronchiectasis and chronic cough; therefore, it is only logical that it is measured to optimize its treatment. However, most treatment recommendations, including the use of anti-inflammatory therapies such as corticosteroids, are based on assessments of only airflow and symptoms. Over the past 10 years, methods have been developed to assess airway inflammation relatively noninvasively. Quantitative cell counts in sputum and the fraction of exhaled nitric oxide are the most validated tests. Judicious use of currently available drugs, such as corticosteroids, bronchodilators and antibiotics, and other anti-inflammatory therapies guided by sputum eosinophil and neutrophil counts, have been demonstrated to decrease exacerbations of asthma and chronic obstructive pulmonary disease, ameliorate cough, improve quality of life in patients with these diseases and is cost effective compared with treatment strategies based on guidelines that do not incorporate these measurements. Thus, it is unfortunate that this is not used more widely in the management of airway diseases, particularly in patients with severe asthma and chronic obstructive pulmonary disease who experience frequent exacerbations.


2021 ◽  
Vol 12 ◽  
Author(s):  
Fabrizio Facchinetti ◽  
Maurizio Civelli ◽  
Dave Singh ◽  
Alberto Papi ◽  
Aida Emirova ◽  
...  

Chronic respiratory diseases are the third leading cause of death, behind cardiovascular diseases and cancer, affecting approximately 550 million of people all over the world. Most of the chronic respiratory diseases are attributable to asthma and chronic obstructive pulmonary disease (COPD) with this latter being the major cause of deaths. Despite differences in etiology and symptoms, a common feature of asthma and COPD is an underlying degree of airways inflammation. The nature and severity of this inflammation might differ between and within different respiratory conditions and pharmacological anti-inflammatory treatments are unlikely to be effective in all patients. A precision medicine approach is needed to selectively target patients to increase the chance of therapeutic success. Inhibitors of the phosphodiesterase 4 (PDE4) enzyme like the oral PDE4 inhibitor roflumilast have shown a potential to reduce inflammatory-mediated processes and the frequency of exacerbations in certain groups of COPD patients with a chronic bronchitis phenotype. However, roflumilast use is dampened by class related side effects as nausea, diarrhea, weight loss and abdominal pain, resulting in both substantial treatment discontinuation in clinical practice and withdrawal from clinical trials. This has prompted the search for PDE4 inhibitors to be given by inhalation to reduce the systemic exposure (and thus optimize the systemic safety) and maximize the therapeutic effect in the lung. Tanimilast (international non-proprietary name of CHF6001) is a novel highly potent and selective inhaled PDE4 inhibitor with proven anti-inflammatory properties in various inflammatory cells, including leukocytes derived from asthma and COPD patients, as well as in experimental rodent models of pulmonary inflammation. Inhaled tanimilast has reached phase III clinical development by showing promising pharmacodynamic results associated with a good tolerability and safety profile, with no evidence of PDE4 inhibitors class-related side effects. In this review we will discuss the main outcomes of preclinical and clinical studies conducted during tanimilast development, with particular emphasis on the characterization of the pharmacodynamic profile that led to the identification of target populations with increased therapeutic potential in inflammatory respiratory diseases.


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