The study examined the antiinflammatory and antinociceptive effects of the sesquiterpene (-)-α-bisabolol (BISA). The antiinflammatory effect was evaluated on acute models of dermatitis induced by Croton oil, arachidonic acid, phenol and capsaicin, respectively, in mouse ear. BISA inhibited the dermatitis induced by all noxious agents, except capsaicin. BISA was assessed in two established mouse models of visceral nociception. Mice were pretreated orally with BISA, and the pain-related behavioral responses to intraperitoneal cyclophosphamide or to intracolonic mustard oil were analyzed. BISA showed a dose-unrelated significant antinociception. Collectively, the results suggest that BISA may be an topical antiinflammatory and visceral antinociceptive agent.
The purpose of this study was to evaluate the effects of Spirulina Platensis supplementation on selected blood markers of oxidative stress, muscle damage, inflammation, and performance in trained rats. Rats (250 g-300 g) were submitted to a strength training program (eight weeks), divided into four groups: control (GT) (trained without supplementation), trained with daily-supplementation of 50 mg/ kg (GT50), 150 mg/kg (GT150) and 500 mg/kg (GT500). Training consisted of a jump protocol in PVCcylinder containing water, with increasing load over experimental weeks. We evaluated the markers of oxidative stress (malondialdehyde-MDA and antioxidant capacity) and inflammation (C-reactive protein) at the end of the training. Among groups submitted to strength training, concentration of C-reactive protein decreased after 8 weeks of intervention in the trained group and GT500. Strength training enhanced plasma MDA concentration of malondialdehyde with supplementation of S. platensis in GT150 and GT500. In plasma analysis, strength training enhanced the percentage of oxidation inhibition, with spirulina supplementation in rates of 150 and 500 mg/kg. Spirulina supplementation for 8 weeks (in a dose-effect manner) improved antioxidant capacity as well as attenuated exercise-induced increases in ROS and inflammation. As a practical application, the use as high doses did not cause a reduction in positive physiological adaptations to exercise training. Additional studies are necessary to test the application of Spirulina Platensis in other contexts, as collective sports (basketball, football, soccer). Spirulina platensis is a microalga with biological activity as antioxidant, immunomodulatory, and anti-inflammatory and nowadays is used to produce nutritional supplements 1-3. S. platensis is composed of protein (55%-70%) 4 , carbohydrates (15%-20%) 5 , lipids (approximately 7%) 5 , fiber, ash, and water including various minerals, vitamins, γ-linolenic acid, chlorophyll, carotenoids, and phycocyanin 2,6. Recently, some researchers have reported that the latter played a crucial role in the antioxidative action of S. platensis 2 .
The possible mechanism is involved in the effects of Spirulina platensis on vascular reactivity. Animals were divided into sedentary group (SG) and sedentary groups supplemented with S. platensis at doses of 50 (SG50), 150 (SG150), and 500 mg/kg (SG500). To evaluate reactivity, cumulative concentration-response curves were constructed for phenylephrine and acetylcholine. To evaluate the involvement of the nitric oxide (NO) pathway, aorta tissue was preincubated with L-NAME and a new curve was then obtained for phenylephrine. Biochemical analyses were performed to evaluate nitrite levels, lipid peroxidation, and antioxidant activity. To contractile reactivity, only SG500 (pD2 = 5.6 ± 0.04 vs. 6.1 ± 0.06, 6.2 ± 0.02, and 6.2 ± 0.04) showed reduction in phenylephrine contractile potency. L-NAME caused a higher contractile response to phenylephrine in SG150 and SG500. To relaxation, curves for SG150 (pD2 = 7.0 ± 0.08 vs. 6.4 ± 0.06) and SG500 (pD2 = 7.3 ± 0.02 vs. 6.4 ± 0.06) were shifted to the left, more so in SG500. Nitrite was increased in SG150 and SG500. Lipid peroxidation was reduced, and oxidation inhibition was increased in all supplemented groups, indicating enhanced antioxidant activity. Chronic supplementation with S. platensis (150/500 mg/kg) caused a decrease in contractile response and increase in relaxation and nitrite levels, indicating greater NO production, due to decreased oxidative stress and increased antioxidant activity.
Studies have shown that supplementation with Spirulina platensis improves vascular reactivity. However, it is unclear whether in association with strength training this effect can be enhanced. Thus, this study aimed to determine the effects of strength training and S. platensis on the reactivity of the aorta from Wistar rat and the possible mechanisms involved. The animals were supplemented with S. platensis and divided into sedentary (SG, SG50, SG150, and SG500) and trained groups (TG, TG50, TG150, and TG500). Nitrite, malondialdehyde (MDA) and antioxidant activity were determined by biochemical assays. To evaluate vascular response, cumulative concentration—response curves to phenylephrine (PHE) and acetylcholine (ACh) were constructed. L-NAME was used to assess the participation of nitric oxide (NO). It was observed that the PHE contractile potency was reduced in TG50, TG150, and TG500 groups compared to SG50, SG150, and SG500 groups, respectively. However, the presence of L-NAME increased the contractile response in all groups. Strength training potentiated the increase in relaxing activity induced by S. platensis, where the pCE50 values of ACh increased in TG150 and TG500. These responses were accompanied by increased nitrite production, MDA reduction and increased antioxidant activity in the aorta of both TG150 and TG500 groups. Thus, the present study demonstrated that combined with strength training, S. platensis potentiates vascular improvement through the participation of NO and reduction of oxidative stress.
Graphical Abstract AbstractAnnona leptopetala R. E. Fries (basynonymy Rollinia leptopetala R. E. Fries) is an endemic tree or shrub from Brazil. Some Annona species such as Annona muricata and Annona squamosa showed uterus activities. Thus, in the search for new agents to combat the uterine disorders, it was aimed to investigate a possible AL-EO tocolytic effect on isolated rat uterus and the underlying mechanisms. Uterine horns were removed, cleaned of adhering fat and connective tissue, and suspended by in organ baths containing Locke-Ringer solution, bubbled with carbogen mixture and the contractions were registered using a force transducer. All experimental procedures were previously approved by Ethic Comission on Animal Use of UFPB (protocol n° 0104/2014). AL-EO was more potent to relax pre-contracted uterus with oxytocin than with KCl. Moreover, AL-EO shifted to the right, in a non-parallel manner, oxytocin induced cumulative contraction curves, with Emax reduction, indicating a pseudo-irreversible noncompetitive antagonism of oxytocin receptors. In the presence of propranolol, β-adrenergic antagonist, an AL-EO action increase was MOL2NET, 2019, 5, ISSN: 2624-5078 2 http://sciforum.net/conference/mol2net-05 observed. Nitric oxide and cyclooxygenase pathways participation were assessed and discarded. The tocolytic potency of AL-EO was attenuated by CsCl, a non-selective K + channel blocker, suggesting a positive modulation of these channels. Additionally, in the presence of 4aminopyridine (4-AP) but not in apamin, glibenclamide or tetraethylammonium (1 mM), the relaxant potency of AL-EO was reduced, indicating the voltage-dependent potassium channels participation, but not small-or big-conductance Ca 2+ -activated and ATP sensitive potassium channels. Tocolytic mechanism of AL-EO on rat uterus involves pseudo-irreversible noncompetitive antagonism of oxytocin receptor and β adrenergic receptors and positive modulation of voltage-dependent potassium channels. Thus, AL-EO is presented as a promising drug with activity on uterine conditions, as dysmenorrhea, and after further evaluation in clinical studies, it would be used as an alternative drug on current pharmacotherapy.
Thymol and carvacrol are the main compounds found in Lippia mycrophylla essential oil (LM-OE) and have presented some spasmolytic effects. This work was designed to explore a possible vasorelaxant effect of LM-OE and its major monoterpenes constituents on rat pulmonary artery. For that, the organ was in vitro stimulated with phenylephrine (Phe) 3 mM and over the tonic contraction the relaxant effect of LM-OE, carvacrol and thymol was observed in both intact and denuded-endothelium. Moreover, atropine, L-NAME, indomethacin, 2,3-O-isopropylidene adenosine, H-89 and Y-27632 were incubated before the relaxant curve of thymol over Phe-tonic contraction. Furthermore, the effects of thymol on KCl 30 or 80 mM and S-(−)-Bay K8644-induced tonic contractions were evaluated, as well as its inhibitory effect on CaCl2-induced cumulative contractions. LM-OE, carvacrol and thymol presented relaxant effect on pulmonary artery, thymol was the most potent and its relaxant potency in intact-endothelium preparations was reduced by atropine, L-NAME, indomethacin, 2,3-O-isopropylidene adenosine and H-89, despite there was not change on its maximum relaxat effect. Also, the monoterpene relaxed equipotently KCl 30 or 80 mM pre-contracted pulmonary artery, antagonized CaCl2-induced cumulative contractions and relaxed S-(−)-Bay K8644 pre-contracted organ. Ultimately, thymol relaxant potency was not modified by Y-27632. Therefore, thymol acts by endothelium-dependent and independent mechanisms, possibly positively modulating the endothelial cholinergic pathway, prostanoids release and further activation of AC/PKA and also inhibiting Ca2+ influx through CaV.
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