scholarly journals Evaluation of the Inhibitory Effects of Bavachinin and Bavachin on Human Monoamine Oxidases A and B

2015 ◽  
Vol 2015 ◽  
pp. 1-14 ◽  
Author(s):  
Najla O. Zarmouh ◽  
Elizabeth A. Mazzio ◽  
Faisel M. Elshami ◽  
Samia S. Messeha ◽  
Suresh V. K. Eyunni ◽  
...  

Monoamine oxidase B inhibitors (MAO-BIs) are used in the early management of Parkinson’s disease (PD). Long-term suspected side effects of MAO-B classical inhibitors established the need for safer alternative therapeutic agents. In our study, the flavanone bavachinin (BNN) and its analog bavachin (BVN) found in the seeds ofPsoralea corylifoliaL. ethanolic extract (PCSEE) were investigated for theirhumanMAO-A and MAO-B (hMAO-A andhMAO-B) inhibition. Both PCSEE and BNN effectively reducedhMAO-B activity more thanhMAO-A while BVN had activating effects. BNN showed selectivehMAO-B inhibition (IC50 ~ 8.82 μM) more thanhMAO-A (IC502009;~ 189.28 μM). BNN in the crude extract was determined by HPLC, also validated by TLC showing a yield of 0.21% PCSEE dry weight. BNN competitively inhibitedhMAO-A andhMAO-B, with a lowerhMAO-BKithanhMAO-AKiby 10.33-fold, and reducedhMAO-BKm/Vmaxefficiency ratio to be comparable to the standard selegiline. Molecular docking examination of BNN and BVN predicted an indirect role of BNN C7-methoxy group for its higher affinity, selectivity, and reversibility as an MAO-BI. These findings suggest that BNN, which is known to be a potent PPAR-γagonist, is a selective and competitivehMAO-B inhibitor and could be used in the management of PD.

2016 ◽  
Vol 11 (9) ◽  
pp. 1934578X1601100 ◽  
Author(s):  
Luiz Carlos Klein-Júnior ◽  
Carolina dos Santos Passos ◽  
Juliana Salton ◽  
Fernanda Gobbi Bitencourt de ◽  
Luís Funez ◽  
...  

In the present study, the effects were evaluated of alkaloid fractions (AFs) from Psychotria species and correlated genera, Palicourea and Rudgea, on monoamine oxidases (MAOs) and cholinesterases (ChEs). By HPLC-DAD and UPLC-DAD-MS analyses, indole alkaloids (IA) were detected in all AFs. For the Psychotria and Palicourea species, these IA corresponded to tetrahydro-β-carboline alkaloids (THβCA). On the other hand, pyrrolidinoindoline core compounds were observed for Rudgea species. Regarding their pharmacological activities, none of the AFs was able to inhibit AChE. However, the BChE activity was impaired by the Psychotria and Palicourea AFs. In addition, MAO-A was inhibited by both AFs, but only Psychotria nemorosa AF was able to inhibit significantly MAO-B. Rudgea AFs demonstrated a poor inhibitory profile on MAO-A. Taken together, our results highlighted the Psychotria and Palicourea genera as important sources of scaffolds for the development of MAO-A and BChE inhibitors aiming at the treatment of neurodegenerative and neuropsychiatric diseases.


1987 ◽  
Vol 38 (3) ◽  
pp. 307 ◽  
Author(s):  
HW Higgins ◽  
DJ Mackey

No seasonal variations were found in the concentrations of Zn, Cd, Cu, K, Ca, Mg and Na in the kelp E. radiata collected from the marine-dominated Port Hacking estuary on the east coast of Australia. Concentrations of Fe and Mn were about 60% higher in late summer. The relative distributions of all metals between different kelp tissues, however, showed no seasonal variation. Concentration factors (dry weight basis) for trace metals ranged from 2600 for Cu to 68 000 for Fe. With high biomasses common in macroalgal ecosystems, a large proportion of the non-sediment- bound trace metals can be associated with the macroalgae, which therefore act as substantial buffers for these elements. Metal concentration factors (Y, wet wt basis) were related to oceanic residence times (τ) by the equation log Y = -0.69 logτ + 5.4. The distribution of the aikaii and akaline earth metais (K, Ca, Mg and Na) was relativeiy uniform throughout the various kelp tissues. However, concentrations of Fe, Mn, Zn and Cd were significantly higher in the older extremities (holdfast and eroding tip) than in the meristematic region. Although the holdfast also had higher levels of Cu than the meristem, levels were lower in the eroding tip. The results suggest either a slow net intracellular accumulation of metals with time or an increase in potential metal- binding sites as the extremities senesce. Translocation and elimination of surplus metals through the eroding tip or holdfast was thought not to be important in E. radiata as metal concentrations did not differ between live and dead haptera of the holdfast. Likewise, storage of metals in either the holdfast or eroding tip was considered unlikely because of the constant relative tissue distribution throughout the year and lack of metal mobilization during periods of growth. Pretreatment of kelp tissue with an EDTA wash released about 90% of the total Zn and Cd, 25% of the Cu and 7% of the Fe, suggesting that a large proportion of the total kelp Zn and Cd is associated with the apparent free space (AFS). With rapid exchange between seawater and the AFS, E. radiata is therefore not generally useful as a sentinel accumulator species in pollution studies for assessing long term integrated changes of metals in the water column.


2012 ◽  
Vol 2012 ◽  
pp. 1-4 ◽  
Author(s):  
Youwei Wang ◽  
Zhi-bo Han ◽  
Yong-ping Song ◽  
Zhong Chao Han

Mesenchymal stem cells (MSCs) hold great promise as therapeutic agents in regenerative medicine and autoimmune diseases, based on their differentiation abilities and immunosuppressive properties. However, the therapeutic applications raise a series of questions about the safety of culture-expanded MSCs for human use. This paper summarized recent findings about safety issues of MSCs, in particular their genetic stability in long-termin vitroexpansion, their cryopreservation, banking, and the role of serum in the preparation of MSCs.


2017 ◽  
Vol 2017 ◽  
pp. 1-8 ◽  
Author(s):  
Damien Maggiorani ◽  
Nicola Manzella ◽  
Dale E. Edmondson ◽  
Andrea Mattevi ◽  
Angelo Parini ◽  
...  

The advances in healthcare over the past several decades have resulted in populations now living longer. With this increase in longevity, a wider prevalence of cardiovascular diseases is more common and known to be a major factor in rising healthcare costs. A wealth of scientific evidence has implicated cell senescence as an important component in the etiology of these age-dependent pathologies. A number of studies indicate that an excess of reactive oxygen species (ROS) contributes to trigger and accelerate the cardiac senescence processes, and a new role of monoamine oxidases, MAO-A and MAO-B, is emerging in this context. These mitochondrial enzymes regulate the level of catecholamines and serotonin by catalyzing their oxidative deamination in the heart. MAOs’ expression substantially increases with ageing (6-fold MAO-A in the heart and 4-fold MAO-B in neuronal tissue), and their involvement in cardiac diseases is supposedly related to the formation of ROS, via the hydrogen peroxide produced during the substrate degradation. Here, we will review the most recent advances in this field and describe why MAOs could be effective targets in order to prevent age-associated cardiovascular disease.


2021 ◽  
Vol 9 (5) ◽  
pp. 975
Author(s):  
Claudio Foschi ◽  
Carola Parolin ◽  
Barbara Giordani ◽  
Sara Morselli ◽  
Barbara Luppi ◽  
...  

Lactobacilli-derived biosurfactants (BS) have shown promising effects as antimicrobial molecules. Since Lactobacillus crispatus plays a crucial role in maintaining vaginal eubiosis, BS from this species could represent novel therapeutic agents to counteract sexually transmitted pathogens, such as Chlamydia trachomatis (CT). The aim of the present study was to assess the inhibitory effects of a BS produced by the vaginal strain L. crispatus BC1 on the infectivity of CT elementary bodies (EBs). For concentrations ranging between 1 and 0.5 mg/mL at 60-min contact time, L. crispatus BC1 BS displayed a highly significant anti-CT activity, with about 50% reduction of EB infectivity towards HeLa cells. To identify the components responsible for chlamydial inhibition, a panel of selected fatty acids, including those present in BS lipopeptidic structure, was tested against CT EBs. Pentadecanoic acid, myristic acid, β-hydroxy-myristic acid, and β-hydroxy-palmitic acid were able to significantly reduce EBs infectivity up to 5–0.5 µg/mL, concentrations that resulted to be non-toxic for HeLa cells. These data can contribute to the understanding of the biological role of lactobacilli in the vaginal niche, as well as to promote the application of their produced BS as an innovative and antibiotic-sparing anti-chlamydial strategy.


2020 ◽  
Vol 75 (11-12) ◽  
pp. 459-466
Author(s):  
Tuba Aydin ◽  
Hulya Akincioglu ◽  
Mehmet Gumustas ◽  
Ilhami Gulcin ◽  
Cavit Kazaz ◽  
...  

AbstractThe aim of this study was to investigate the effects of extracts and pure Artemisia dracunculus L. (tarragon) metabolites on the antimonoamine oxidase and anticholinesterase activities. The compounds were characterized as stigmasterol (1), herniarin (2), (2E,4E)-1-(piperidin-1-yl)undeca-2,4-diene-8,10-diyn-1-one (3), (2E,4E)-N-isobutylundeca-2,4-dien-8,10-diynamide (4), 3,4-dehydroherniarin (5) and skimmin (6) by 1H-NMR, 13C-NMR, 1D and 2D NMR methods. The compounds 5 and 6 were isolated from tarragon for the first time. The extracts and pure compounds have inhibitory effects on the human monoamine oxidase (hMAO) A and B enzymes, whereas they did not exhibit any anticholinesterase activities. Among the tarragon compounds, only 2 and 6 compounds showed the inhibitory effects against hMAO A (IC50 = 51.76 and 73.47 μM, respectively) and hMAO B (IC50 = 0.84 and 1.63 mM, respectively). In the study, herniarin content in the extracts was also analysed by high-performance liquid chromatography and it was found that there was a relationship between the inhibition effects of the extracts and their herniarin content.


Jurnal Agrium ◽  
2018 ◽  
Vol 15 (1) ◽  
pp. 34
Author(s):  
Safrizal Safrizal ◽  
Nazimah Nazimah ◽  
Rina Resssi

Red chili is a major vegetable both in Indonesia and abroad due to its benefits to the needs of nutrition and health through cooking spices. Utilization of home garden yard is an effective way to cultivate pepper plants. On the other hand, every household produces household waste which is difficult to decompose for instance diapers, so that it can cause environmental pollution in long-term. This study was conducted to investigate the role of planting media such as diapers of on chili growth. The results showed that the use of diapers of diapers as planting media gave no significant different to plant height at 1, 4, 7, 10, 13 and 16 week after application.  It also did not increase the number of leaves at the age of 1, 7, 10, 13 and 16 week after application.  There were no changes in leaf length at ages 1, 4, 7, 10 and 16 week after application. It also happened to also its leaf width at ages 1, 4, 7, 10, 13 and 16 week after application and number of branches at ages 1, 4, 7, 13 and 16 week after aplication. However, it showed a significant different to the number of leaves at age 4 week after planting and its leaf length at age 13 week after planting.   The interaction of using diapers as planting media gave significantly different response to root number, root length, wet root weight and plant canopy, and dry weight roots and plant canopy.


Molecules ◽  
2020 ◽  
Vol 25 (10) ◽  
pp. 2356 ◽  
Author(s):  
Jong Min Oh ◽  
T. M. Rangarajan ◽  
Reeta Chaudhary ◽  
Rishi Pal Singh ◽  
Manjula Singh ◽  
...  

Previously synthesized novel chalcone oxime ethers (COEs) were evaluated for inhibitory activities against monoamine oxidases (MAOs) and acetylcholinesterase (AChE). Twenty-two of the 24 COEs synthesized, except COE-17 and COE-24, had potent and/or significant selective inhibitory effects on MAO-B. COE-6 potently inhibited MAO-B with an IC50 value of 0.018 µM, which was 105, 2.3, and 1.1 times more potent than clorgyline, lazabemide, and pargyline (reference drugs), respectively. COE-7, and COE-22 were also active against MAO-B, both had an IC50 value of 0.028 µM, which was 67 and 1.5 times lower than those of clorgyline and lazabemide, respectively. Most of the COEs exhibited weak inhibitory effects on MAO-A and AChE. COE-13 most potently inhibited MAO-A (IC50 = 0.88 µM) and also significantly inhibited MAO-B (IC50 = 0.13 µM), and it could be considered as a potential nonselective MAO inhibitor. COE-19 and COE-22 inhibited AChE with IC50 values of 5.35 and 4.39 µM, respectively. The selectivity index (SI) of COE-22 for MAO-B was higher than that of COE-6 (SI = 778.6 vs. 222.2), but the IC50 value (0.028 µM) was slightly lower than that of COE-6 (0.018 µM). In reversibility experiments, inhibitions of MAO-B by COE-6 and COE-22 were recovered to the levels of reference reversible inhibitors and both competitively inhibited MAO-B, with Ki values of 0.0075 and 0.010 µM, respectively. Our results show that COE-6 and COE-22 are potent, selective MAO-B inhibitors, and COE-22 is a candidate of dual-targeting molecule for MAO-B and AChE.


Cells ◽  
2020 ◽  
Vol 9 (3) ◽  
pp. 675 ◽  
Author(s):  
Juliana Ferreira Floriano ◽  
Gareth Willis ◽  
Francesco Catapano ◽  
Patrícia Rodrigues de Lima ◽  
Fabiana Vieira Duarte Souza Reis ◽  
...  

Gestational diabetes Mellitus (GDM) is a complex clinical condition that promotes pelvic floor myopathy, thus predisposing sufferers to urinary incontinence (UI). GDM usually regresses after birth. Nonetheless, a GDM history is associated with higher risk of subsequently developing type 2 diabetes, cardiovascular diseases (CVD) and UI. Some aspects of the pathophysiology of GDM remain unclear and the associated pathologies (outcomes) are poorly addressed, simultaneously raising public health costs and diminishing women’s quality of life. Exosomes are small extracellular vesicles produced and actively secreted by cells as part of their intercellular communication system. Exosomes are heterogenous in their cargo and depending on the cell sources and environment, they can mediate both pathogenetic and therapeutic functions. With the advancement in knowledge of exosomes, new perspectives have emerged to support the mechanistic understanding, prediction/diagnosis and ultimately, treatment of the post-GMD outcomes. Here, we will review recent advances in knowledge of the role of exosomes in GDM and related areas and discuss the possibilities for translating exosomes as therapeutic agents in the GDM clinical setting.


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