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Planta Medica Nov 2018and bark extracts have been used for thousands of years in Chinese and Japanese traditional medicines and are still widely employed as herbal preparations for their... (Review)
Review
and bark extracts have been used for thousands of years in Chinese and Japanese traditional medicines and are still widely employed as herbal preparations for their sedative, antioxidant, anti-inflammatory, antibiotic, and antispastic effects. Neolignans, particularly magnolol and honokiol, are the main substances responsible for the beneficial properties of the magnolia bark extract (MBE). The content of magnolol and honokiol in MBE depends on different factors, including the plant species, the area of origin, the part of the plant employed, and the method used to prepare the extract. The biological and pharmacological activities of magnolol and honokiol have been extensively investigated. Here we review the safety and toxicological properties of magnolol and honokiol as pure substances or as components of concentrated MBE, including the potential side-effects in humans after oral intake. and genotoxicity studies indicated that concentrated MBE has no mutagenic and genotoxic potential, while a subchronic study performed according to OECD (Organisation for Economic Co-operation and Development) guidelines established a no adverse effect level for concentrated MBE > 240 mg/kg b.w/d. Similar to other dietary polyphenols, magnolol and honokiol are subject to glucuronidation, and despite a relatively quick clearance, an interaction with pharmaceutical active principles or other herbal constituents cannot be excluded. However, intervention trials employing concentrated MBE for up to 1 y did not report adverse effects. In conclusion, over the recent years different food safety authorities evaluated magnolol and honokiol and considered them safe.
Topics: Animals; Biphenyl Compounds; Drug Interactions; Humans; Lignans; Magnolia; Mutagenicity Tests; Plant Extracts; Tissue Distribution
PubMed: 29925102
DOI: 10.1055/a-0642-1966 -
Analytical Sciences : the International... 2018We report on a paper-based 2,2-diphenyl-1-(2,4,6-trinitrophenyl)hydrazyl (DPPH) assay for a simple, inexpensive, low reagent and sample consumption and high throughput...
We report on a paper-based 2,2-diphenyl-1-(2,4,6-trinitrophenyl)hydrazyl (DPPH) assay for a simple, inexpensive, low reagent and sample consumption and high throughput analysis of antioxidant activity. The paper-based device was fabricated using a lamination method to create a 5-mm in diameter circular test zone that was embedded with a DPPH reagent. The analysis was carried out in one-step by dropping an antioxidant/sample onto the test zone. After reduction by the antioxidant, the DPPH radicals become stable DPPH molecules, resulting in a change in color from deep violet to pale yellow. The violet color intensity of DPPH was inversely proportional to the antioxidant activity of the samples, and was measured using imaging software. A high precision and a low limit of detection were found in the analysis of six standard antioxidants including gallic acid, trolox, ascorbic acid, caffeic acid, vanilliic acid and quercetin. The device was then validated against the traditional spectrophotometric DPPH assay by analyzing the antioxidant activity of 7 tea samples. The results showed no significant difference for gallic acid equivalent for all 7 samples obtained from the two methods at the 95% confidence level, indicating that the developed method was reliable for antioxidant activity analysis of real samples. Finally, the paper-based DPPH device was found to be stable over 10 days when stored in a refrigerator (2 - 4°C), making it an easy-to-use device for end-users.
Topics: Antioxidants; Biphenyl Compounds; Paper; Picrates; Refrigeration
PubMed: 29998961
DOI: 10.2116/analsci.18P014 -
Journal of Clinical Hypertension... Mar 2023This study assessed the efficacy and safety of sacubitril/valsartan in 23 hemodialysis patients with hypertension (mean age 70 years; male 69.6%) after switching from...
This study assessed the efficacy and safety of sacubitril/valsartan in 23 hemodialysis patients with hypertension (mean age 70 years; male 69.6%) after switching from azilsartan, an angiotensin receptor blocker. Both at baseline and 3 months after the start of sacubitril/valsartan treatment, home blood pressure (BP), BP values during hemodialysis, and N-terminal pro-brain natriuretic peptide (NT-proBNP) level were measured. The mean dosage of azilsartan was 30 ± 10 mg/day at baseline and that of sacubitril/valsartan after 3 months of treatment was 204 ± 64 mg/day. After 3 months, significant reductions in mean morning home BP (155 ± 17/80 ± 12 to 147 ± 16/76 ± 11 mmHg), mean nighttime home systolic BP (153 ± 19 to 144 ± 16 mmHg), and median (IQRs) NT-proBNP level [8124 (2620-13 394) to 6271 (1570-9591) pg/mL] were observed (all P < .05), whereas BP values during hemodialysis did not change significantly. In hemodialysis patients, except for hypotension, sacubitril/valsartan was generally well tolerated, effectively controlled out-of-office BP, and improved NT-proBNP.
Topics: Humans; Male; Aged; Hypertension; Tetrazoles; Valsartan; Aminobutyrates; Biphenyl Compounds; Angiotensin Receptor Antagonists; Drug Combinations; Heart Failure; Stroke Volume
PubMed: 36722379
DOI: 10.1111/jch.14635 -
Molecules (Basel, Switzerland) May 2021Selenium-containing compounds are gaining more and more interest due to their valuable and promising pharmacological properties, mainly as anticancer and antioxidant...
Selenium-containing compounds are gaining more and more interest due to their valuable and promising pharmacological properties, mainly as anticancer and antioxidant agents. Ebselen, the up to now only approved drugs, is well known to possess very good glutathione peroxidase mimicking effects. To date, the most of efforts have been directed to build pure synthetic Se containing molecules, while less attention have been devoted to Se-based semisynthetic products resembling natural compounds like terpenes, polyphenols, and alkaloids. The aim of this short communication is to report the synthesis of the first example of a Se-phenylpropanoids, namely selenoauraptene, containing a selenogeranyl side chain in position 7 of the umbelliferone core. The key step was the Newman-Kwart rearrangement to obtain a selenocarbamate in which the Se atom was directly attached to umbelliferone (replacing its 7-OH function) followed by hydrolysis to get diumbelliferyl diselenide, which was finally easily converted to the desired Se-geranyl derivative in quite a good overall yield (28.5%). The synthesized adduct displayed a greater antioxidant and a radical scavenger in vitro activity than parent auraptene. The procedure we describe herein, to the best of our knowledge for the first time in the literature, represents an easy-to-handle method for the synthesis of a wide array of seleno analogues of naturally occurring biologically active oxyprenylated secondary metabolites.
Topics: Antioxidants; Benzothiazoles; Biphenyl Compounds; Coumarins; Picrates; Proton Magnetic Resonance Spectroscopy; Selenium Compounds; Sulfonic Acids
PubMed: 34068532
DOI: 10.3390/molecules26092798 -
Journal of the American College of... Jun 2021The recent U.S. Food and Drug Administration expanded indication for sacubitril/valsartan introduces a new potential taxonomy for heart failure, with no reference to... (Review)
Review
The recent U.S. Food and Drug Administration expanded indication for sacubitril/valsartan introduces a new potential taxonomy for heart failure, with no reference to "preserved" ejection fraction but referring to "below normal" ejection fraction as those most likely to benefit. This review summarizes the evolution of nomenclature in heart failure and examines evidence showing that patients with ejection fraction in the "mid range" may benefit from neurohormonal blockade similar to those with more severely reduced (<40%) ejection fraction. Furthermore, prominent sex differences have been observed wherein the benefit of neurohormonal blockade appears to extend to a higher ejection fraction range in women compared to men. Based on emerging evidence, revised nomenclature is proposed defining heart failure with "reduced" (<40%), "mildly reduced," and "normal" (≥55% in men, ≥60% in women) ejection fraction. Such nomenclature signals consideration of potentially beneficial therapies in the largest group of patients with reduced or mildly reduced ejection fraction.
Topics: Aminobutyrates; Angiotensin Receptor Antagonists; Biphenyl Compounds; Drug Combinations; Heart Failure; Humans; Stroke Volume; Valsartan
PubMed: 34167646
DOI: 10.1016/j.jacc.2021.04.070 -
The Journal of Organic Chemistry Nov 2021In this work, we demonstrate that readily available conjugated bis-aryl cyclobutenones undergo photoelectrocyclization reactions to give the corresponding...
In this work, we demonstrate that readily available conjugated bis-aryl cyclobutenones undergo photoelectrocyclization reactions to give the corresponding dihydrophenanthrene cyclobutanones when exposed to 350 nm light, TFA, and TMSCl. We have also found that cyclobutenone electrocyclizations and cycloreversions are in equilibrium.
Topics: Biphenyl Compounds; Cyclobutanes
PubMed: 34586823
DOI: 10.1021/acs.joc.1c01809 -
International Journal of Molecular... Oct 2023In patients with heart failure (HF), the neuroendocrine systems of the sympathetic nervous system (SNS), the renin-angiotensin-aldosterone system (RAAS) and the arginine... (Review)
Review
In patients with heart failure (HF), the neuroendocrine systems of the sympathetic nervous system (SNS), the renin-angiotensin-aldosterone system (RAAS) and the arginine vasopressin (AVP) system, are activated to various degrees producing often-observed tachycardia and concomitant increased systemic vascular resistance. Furthermore, sustained neurohormonal activation plays a key role in the progression of HF and may be responsible for the pathogenetic mechanisms leading to the perpetuation of the pathophysiology and worsening of the HF signs and symptoms. There are biomarkers of activation of these neurohormonal pathways, such as the natriuretic peptides, catecholamine levels and neprilysin and various newer ones, which may be employed to better understand the mechanisms of HF drugs and also aid in defining the subgroups of patients who might benefit from specific therapies, irrespective of the degree of left ventricular dysfunction. These therapies are directed against these neurohumoral systems (neurohumoral antagonists) and classically comprise beta blockers, angiotensin-converting enzyme (ACE) inhibitors/angiotensin receptor blockers and vaptans. Recently, the RAAS blockade has been refined by the introduction of the angiotensin receptor-neprilysin inhibitor (ARNI) sacubitril/valsartan, which combines the RAAS inhibition and neprilysin blocking, enhancing the actions of natriuretic peptides. All these issues relating to the neurohumoral activation in HF are herein reviewed, and the underlying mechanisms are pictorially illustrated.
Topics: Humans; Neprilysin; Tetrazoles; Angiotensin Receptor Antagonists; Heart Failure; Angiotensin-Converting Enzyme Inhibitors; Drug Combinations; Renin-Angiotensin System; Natriuretic Peptides; Aminobutyrates; Biphenyl Compounds
PubMed: 37895150
DOI: 10.3390/ijms242015472 -
ChemMedChem Nov 2022We identified 2,4-dinitro-biphenyl-based compounds as new inhibitors of leukotriene C synthase (LTC S) and 5-lipoxygenase-activating protein (FLAP), both members of the...
We identified 2,4-dinitro-biphenyl-based compounds as new inhibitors of leukotriene C synthase (LTC S) and 5-lipoxygenase-activating protein (FLAP), both members of the "Membrane Associated Proteins in Eicosanoid and Glutathione metabolism" (MAPEG) family involved in the biosynthesis of pro-inflammatory eicosanoids. By molecular docking we evaluated the putative binding against the targets of interest, and by applying cell-free and cell-based assays we assessed the inhibition of LTC S and FLAP by the small molecules at low micromolar concentrations. The present results integrate the previously observed inhibitory profile of the tested compounds against another MAPEG member, i. e., microsomal prostaglandin E synthase (mPGES)-1, suggesting that the 2,4-dinitro-biphenyl scaffold is a suitable molecular platform for a multitargeting approach to modulate pro-inflammatory mediators in inflammation and cancer treatment.
Topics: Molecular Docking Simulation; Glutathione Transferase; 5-Lipoxygenase-Activating Proteins; Biphenyl Compounds; Prostaglandin-E Synthases
PubMed: 36111583
DOI: 10.1002/cmdc.202200327 -
Dermatologic Therapy Aug 2022Honokiol is one of the natural extracts of Magnolia officinalis. It is a small molecule, lipophilic compound with extensive biological effects. It has been used in the... (Review)
Review
Honokiol is one of the natural extracts of Magnolia officinalis. It is a small molecule, lipophilic compound with extensive biological effects. It has been used in the treatment of multisystem diseases, including digestive diseases, endocrine diseases, nervous system diseases, and various tumors. This paper reviews the biological effects of honokiol on the treatment of skin diseases in recent years, including anti-microbial, anti-oxidant, anti-inflammatory, anti-tumor, anti-fibrosis, anti-allergy, photo-protection, and immunomodulation. Most current researches are focused on the effects of anti-melanoma and photo-protection. Therefore, we summarized the specific mechanisms about these two effects. On the other side of treating skin diseases, the advantages of topical drugs cannot be replaced. As a small molecule fat-soluble compound, honokiol is suitable for external use. We reviewed the advantages and disadvantages of the topical mixed cream and various improved methods. These improvements include physical and chemical penetration enhancers, drug carriers, and chemical derivatives. In conclusion, honokiol has a wide range of effects, and its topical preparation provides a safe and effective way for treating skin diseases.
Topics: Allyl Compounds; Antioxidants; Biphenyl Compounds; Dermatology; Humans; Lignans; Phenols; Skin Diseases
PubMed: 35726011
DOI: 10.1111/dth.15658 -
Value in Health : the Journal of the... May 2020
Topics: Aminobutyrates; Biphenyl Compounds; Cost-Benefit Analysis; Drug Combinations; Germany; Tetrazoles; Valsartan
PubMed: 32389235
DOI: 10.1016/j.jval.2019.12.013