Hesperozygis ringens (Benth.) Epling: a study involving extraction, chemical profiling, antioxidant and biological activity.

Hesperozygis ringens is a plant of the Lamiaceae family which is restricted to the Southern region of Brazil. It is popularly used as an insecticide, but knowledge on it is very scarce. This study aimed to determine the chemical markers of H. ringens extracts obtained via ultrasound-assisted (UAE-EtOH) and supercritical fluid (SFE-CO2) extractions. UAE-EtOH and SFE-CO2 extracts were characterised by UPLC-MS and GC-MS, respectively. Both products had their antioxidant activity, cytotoxicity and genotoxicity evaluated. Twelve compounds were found in the UAE-EtOH extract, including phenolic acids and flavonoids; the SFE-CO2 extract contained terpenes and phytosterols. The UAE-EtOH extract showed a greater antioxidant activity. Neither extract presented cytotoxicity or genotoxicity against human mononuclear blood cells.

Chemical study, antioxidant activity, and genotoxicity and cytotoxicity evaluation of Ruellia angustiflora.

Ruellia angustiflora (Acanthaceae) is known as flower-of-fire, and its leaves are traditionally employed to promote wound healing. This study was aimed at extracting and characterizing the chemical constituents of the extracts of R. angustiflora obtained by ultrasound-assisted and supercritical fluid extractions, and subsequently investigate their antioxidant potential and cyto-genotoxicity. The extract obtained by ultrasound (UAE-EtOH) was characterized by ultraperformance liquid chromatography-mass spectrometer (UPLC-MS), and the extract obtained via supercritical fluid (SFE-CO2) by gas chromatograph-mass spectrometer (GC-MS). The antioxidant potential was verified by the antiradical activity against the 1,1-diphenyl-2-picrylhydrazyl radical (DPPH), and the cyto-genotoxicity evaluation to test cell viability and DNA damage was performed in peripheral blood mononuclear cells (PBMC) cultures. The SFE-CO2 extract presented some fatty acids, triterpenes, tetraterpenes, tocopherols and phytosterols. The UAE-EtOH extract contained phenolic acids and flavonoids, and showed the highest antioxidant capacity. Neither extract was genotoxic or cytotoxic at the tested concentrations.

Topical hydrogel containing Achyrocline satureioides oily extract (free and nanocapsule) has anti-inflammatory effects and thereby minimizes irritant contact dermatitis.

Inflammatory dermatoses are prevalent worldwide, with impacts on the quality of life of patients and their families. The aim of this study was to determine the anti-inflammatory effects of Achyrocline satureioides oily extracts and nanocapsules on the skin using a mouse model of irritant contact dermatitis induced by croton oil, and a skin inflammation model induced by ultraviolet B (UVB) radiation. The mice were treated with 15 mg/ear oily extract (HG-OLAS) or nanocapsules (HG-NCAS) of A. satureioides incorporated into Carbopol® 940 hydrogels. We found that HG-OLAS and HG-NCAS formulations reduced ear edema in croton oil-induced lesions with maximum inhibitions of 54±7% and 74±3%, respectively. HG-OLAS and HG-NCAS formulations decreased ear edema induced by UVB radiation (0.5 J/cm2), with maximum inhibitions of 68±6% and 76±2% compared to the UVB radiation group, respectively. HG-OLAS and HG-NCAS modulated myeloperoxidase (MPO) activity after croton oil induction. Furthermore, croton oil and UVB radiation for 6 and 24 h, respectively, stimulated polymorphonuclear cells infiltration. The topical treatments reduced inflammatory processes, as shown by histological analysis. Together, the data suggest that topical application of A. satureioides oily extracts and nanocapsules produced antiedematogenic and anti-inflammatory effects. They constitute a compelling alternative for treatment of skin injuries.

Protective effect of nerolidol-loaded in nanospheres against cerebral damage caused by Trypanosoma evansi.

Trypanosoma evansi is a zoonotic parasite associated with high animal mortality that has gained importance due to its capacity to infect humans. Recently, some evidences have demonstrated that T. evansi infection causes severe genotoxic and cytotoxic damage in brain cells, contributing to the pathogenesis and clinical signs of the disease. In this sense, the aim of this study was to evaluate whether nerolidol-loaded in nanospheres, a natural compound with trypanocidal and neuroprotective effects, is able to protect the brain tissue from the cytotoxic and genotoxic effects found during T. evansi infections. Trypanosoma evansi induced brain genotoxic effects through increased damage index (DI) and frequency of damage (FD) when compared to the control group. Moreover, T. evansi induced cytotoxic effects through the reduction of brain cell viability compared to the control group. The metabolites of nitric oxide (NO x ) increased in infected animals compared to the control group. The treatment with nerolidol-loaded in nanospheres prevented the increase on brain DI, FD, and NO x levels, as well as the reduction on cell viability. Based on these evidences, these results confirm that T. evansi induces genotoxic and cytotoxic damage mediated by the upregulation of NO x levels. The most important finding is that nerolidol-loaded in nanospheres was able to prevent DNA damage and cell mortality through the modulation of brain NO x levels. In summary, this treatment can be considered an interesting approach to prevent T. evansi brain damage due its anti-inflammatory property.

Treatment with tucumã oil (Astrocaryum vulgare) for diabetic mice prevents changes in seric enzymes of the purinergic system: Improvement of immune system.

The aim of this study was to evaluate the enzymatic activity of the purinergic system in sera samples from alloxan-induced diabetic mice treated with tucumã oil (Astrocaryum vulgare). For this, the mice were divided into four groups (n=6): control/water (the group CW); control/tucumã oil (the group CT); diabetic/water (the group DW), and diabetic/tucumã oil (the group DT) treated for 14days with 5.0mLkg-1 via oral gavage. On day 14 post-treatment, mice were submitted to euthanasia and blood samples were collected by cardiac puncture. Tucumã oil treatment significantly decreased (p<0.05) blood glucose levels in the group DT compared to the group DW. These results demonstrated an increase (p<0.05) in NTPDase (adenosine triphosphate (ATP substrate) or adenosine diphosphate (ADP substrate)), 5'-nucleotidase (AMP substrate) and adenosine deaminase (ADA; adenosine substrate) activities in serum from the group DW compared to the group CW. Tucumã oil treatment prevented these alterations in the group DT compared to the group DW, and restored these parameters near to the group CW. In summary, the treatment with tucumã oil was able to modulate the alterations caused by hyperglycemia probably by the presence of carotenoids compounds, maintaining normal levels of ATP, ADP, AMP and adenosine, molecules that could exhibit anti-inflammatory properties, depending on their concentration. Thus, the tucumã oil is a promising natural compound with protective action against diabetes and its side effects, such as changes in the purinergic system, improving the immune system.

Nanoencapsulation Improves Scavenging Capacity and Decreases Cytotoxicity of Silibinin and Pomegranate Oil Association.

Silibinin (SB) and pomegranate oil (PO) present therapeutic potential due to antioxidant activity, but the biological performance of both bioactives is limited by their low aqueous solubility. To overcome this issue, the aim of the present investigation was to develop nanocapsule suspensions with PO as oil core for SB encapsulation, as well as assess their toxicity in vitro and radical scavenging activity. The nanocapsule suspensions were prepared by interfacial deposition of preformed polymer method. SB-loaded PO-based nanocapsules (SBNC) showed an average diameter of 157 ± 3 nm, homogenous size distribution, zeta potential of -14.1 ± 1.7 mV, pH of 5.6 ± 0.4 and SB content close to 100%. Similar results were obtained for the unloaded formulation (PONC). The nanocapsules controlled SB release at least 10 times as compared with free SB in methanolic solution. The SBNC scavenging capacity in vitro was statistically higher than free SB (p < 0.05). Cell viability in monocytes and lymphocytes was kept around 100% in the treatments with SBNC and PONC, while the SB and the PO caused a decrease around 30% at 50 µM (SB) and 724 µg/mL (PO). Protein carbonyls and DNA damage were minimized by SB and PO nanoencapsulation. Lipid peroxidation occurred in nanocapsule treatments regardless of the SB presence, which may be attributed to PO acting as substrate in reaction. The free compounds also caused lipid peroxidation. The results show that SBNC and PONC presented adequate physicochemical characteristics and low toxicity against human blood cells. Thereby, this novel nanocarrier may be a promising formulation for therapeutic applications.

The use of tucumã oil (Astrocaryum vulgare) in alloxan-induced diabetic mice: effects on behavior, oxidant/antioxidant status, and enzymes involved in brain neurotransmission.

The aim of this study was to investigate the effects of tucumã oil (Astrocaryum vulgare) on memory, enzymatic activities of sodium-potassium pump (Na+, K+-ATPase) and acetylcholinesterase (AChE) in the brain of alloxan-induced diabetic mice. The animals were divided into four groups (n = 6 each): the group A (non-diabetic/water), the group B (non-diabetic/tucumã oil), the group C (diabetic/water), and the group D (diabetic/tucumã oil) treated 14 days with 5.0 mL kg-1 via oral gavage. Untreated diabetic mice (the group C) showed memory deficit, increased levels of thiobarbituric acid reactive species (TBARS) and protein carbonylation (PC), and decreased (p < 0.05) catalase (CAT), superoxide dismutase (SOD), and the Na+, K+-ATPase activities, while acetylcholinesterase (AChE) activity showed a significant increase (p < 0.05) compared to non-diabetic mice (the group A). Tucumã oil prevented these alterations in diabetic mice treated with tucumã oil (the group D) compared to diabetic mice (the group C). Our findings suggest that tucumã oil can modulate cholinergic neurotransmission resting membrane potential of neurons by modulating enzymatic antioxidant defenses. In conclusion, the present data showed that treatment with tucumã oil is beneficial to diabetic mice, demonstrating that this oil can modulate cholinergic neurotransmission and consequently improve or avoid memory deficits.

Antihyperglycemic, antioxidant activities of tucumã oil (Astrocaryum vulgare) in alloxan-induced diabetic mice, and identification of fatty acid profile by gas chromatograph: New natural source to treat hyperglycemia.

The aim of the study was to investigate the effect of the oral administration of tucumã oil (Astrocaryum vulgare) on glucose and insulin levels, oxidative status, and pancreatic genotoxic parameters of alloxan-induced diabetic mice. The animals were divided into four groups (n = 6 each): control/water; control/tucumã oil; diabetic/water; diabetic/tucumã oil treated for 14 days with 5.0 mL kg-1 via oral gavage. Gas chromatograph characterization demonstrated that oleic/elaidic fatty acid is the most abundant component present in this oil, followed by palmitic and stearic fatty acids. Our results demonstrated an increase (p < 0.05) in water and food intake, blood glucose, thiobarbituric acid reactive species (TBARS) levels, damage index, and frequency of damage; conversely body weight, insulin levels, catalase (CAT) and superoxide dismutase (SOD) activities, and cell viability were decreased in the diabetic/water group compared to the control/water group. The treatment with tucumã oil prevented these alterations in the diabetic/tucumã oil group compared to the diabetic/water group, and restored these parameters near to the control/water group. In summary, our findings demonstrated that treatment with tucumã oil causes a hypoglycemic effect improving insulin levels and antioxidant/oxidant status, and has a protector effect against pancreatic damage induced by oxidative stress in alloxan-induced diabetic mice.

Trypanocidal activity of the compounds present in Aniba canelilla oil against Trypanosoma evansi and its effects on viability of lymphocytes.

Aniba canelilla (H.B.K.) Mez, popularly known as "casca-preciosa" (precious bark), is a plant of the Lauraceae family, widely distributed in the Amazon region. Its major constituent is 1-nitro-2-phenylethane, a rare molecule in plants which is responsible for this plant's cinnamon scent. The present study aimed to report the chemical characterization of the oil extracted from Aniba canelilla using gas-chromatography/mass spectrometry and to assess its in vitro trypanocidal activity against Trypanosoma evansi, a prevalent haemoflagellate parasite that affects a broad range of mammal species in Africa, Asia and South America. The oil presented 1-nitro-2-phenylethane (83.68%) and methyleugenol (14.83%) as the two major components. The essential oil as well as both major compounds were shown to exert trypanocidal effect. Methyleugenol was slightly more active than 1-nitro-2-phenylethane. In vitro studies showed that the oil extracted from the stems of A. canelilla may be regarded as a potential natural treatment for trypanosomosis, once proven their in vivo action, may be an interesting alternative in the treatment of infected animals with T. evansi.

Achyrocline satureioides essential oil-loaded in nanocapsules reduces cytotoxic damage in liver of rats infected by Trypanosoma evansi.

The aim of this study was to evaluate whether the treatment with Achyrocline satureioides essential oil-loaded in nanocapsules (AS-NC) is able to protect the hepatic tissue against cytotoxic damage caused by Trypanosoma evansi. Thus, the rats were divided into four groups (n = 6 per group): uninfected/saline, uninfected/AS-NC, infected/saline, and infected/AS-NC. At day 4 post-infection (PI), the animals were euthanized and liver and sera samples were collected to perform the hepatic cell viability assay, and to determine seric levels of reactive oxygen species (ROS) and nitric oxide metabolites (NOx). Cell viability decreased (p < 0.05) in the infected/saline group compared to uninfected/saline group, while the treatment with AS-NC avoided this alteration in infected rats. Seric ROS and NOx levels increased (p < 0.05) in the infected/saline group compared to uninfected/saline group, while the treatment with AS-NC avoided this effect on ROS levels of infected rats. In summary, the treatment with AS-NC was able to protect the liver tissue against the cytotoxic effect caused by the parasite by avoiding exacerbated production of ROS.

Treatment with essential oil of Achyrocline satureioides in rats infected with Trypanosoma evansi: relationship between protective effect and tissue damage.

The aim of this study was to evaluate the effects of treatment with free and nanoencapsulated essential oil of Achyrocline satureioides on trypanosomosis and its oxidative/antioxidants variables in liver and kidney of rats infected experimentally with Trypanosoma evansi. For that, 48 rats were divided into six groups (A-F), eight animals each group. Groups A, C and D were composed of uninfected animals, while animals in groups B, E and F were inoculated intraperitoneally with T. evansi. Groups A and B were used as controls, negative and positive, respectively. Groups C and E receive oil (orally), as well as the animals in groups D and F were treated with nanoencapsulated essential oil. The treatment was not able to eliminate the parasites, but it remained the levels of parasitemia low. The carbonyl levels in liver and kidney did not differ between groups. Infected animals (group B) showed an increase in the TBARS levels and a decrease in the CAT activity and NPSH levels in liver and kidney, compared with the same parameters in the control (group A). Treatment with A. satureioides (groups C and D) did not influence the TBARS levels and CAT activity in the liver, but it increased the CAT activity in kidneys of the animals of group C. NPSH levels decreased in liver in the groups treated with nanoencapsulated essential oil (groups D and F). An interesting result observed was that the animals infected and then treated with essential oil of A. satureioides (groups E and F) did not differ from animals of group A for TBARS, CAT and NPSH, unlike what happened with the animals of group B. Therefore, the treatment with essential oil did not eliminate the parasites from the bloodstream, but it reduced the number of trypanosomes, mainly by its nanoencapsulated form. The same occurred with the lipid peroxidation in the liver. However, the treatments reduced the oxidative damage, and it led to the activation of the antioxidant enzymes. We believe that the association of this natural product with a trypanocidal drug may enhance its curative effect.

In vitro trypanocidal activity of macela (Achyrocline satureioides) extracts against Trypanosoma evansi.

The aim of this study was to verify the trypanocidal effectiveness of aqueous, methanolic, and ethanolic extracts of Achyrocline satureioides against Trypanosoma evansi in vitro. A. satureioides extracts, known as macela, were used on trypomastigotes at different concentrations (1, 5, 10, 50, 100, 500, and 1,000 µg/ml) and exposure times (0, 1, 3, 6, and 9 hr). A dose-dependent effect was observed when the 3 extracts were tested. The concentrations of 1, 5, and 10 µg/ml were not able to kill trypomastigotes until 3 hr after exposure, and the highest concentrations (500 and 1,000 µg/ml) were able to kill all trypomastigotes after 1 hr. When the time of exposure was increased up to 9 hr, the concentrations at 50 and 100 µg/ml were 100% effective to 3 extracts. The chemical analysis of the extracts revealed the presence of flavonoids, a trypanocidal compound already described. Based on the results, we can conclude that the A. satureioides extracts exhibit trypanocidal effects.