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Salvia elegans Vahl is a plant commonly used in Mexico as a remedy for nervous disorders, inflammatory diseases, and “ringing in the ears”; the latter can be associated with arteriosclerotic conditions and arterial hypertension. Therefore, based on medicinal use, this work aimed to evaluate the hydroalcoholic extract (SeHA, 100 mg/kg) of this plant and two fractions, ethyl acetate (SeFAc, 50 mg/kg), and obtained from SeFAc fractionation denominated SeF3 (10 mg/kg), on several alterations derived from metabolic syndrome (MetS) derived from the ingestion of a high-calorie diet (high-fat diet), in ICR (Institute of Cancer Research) mice, leading to chronic inflammation that results in neurological damage such as depression. Therefore, several MetS-related parameters, such as forced swim tests, hypertension, serum corticosterone levels, glucose, triglycerides, cholesterol, adiposity index, and insulin resistance, will be evaluated. Additionally, tumor necrosis factor (TNF)-α, interleukin (IL)-1β, IL-6, and IL-10 levels were measured in kidneys, fat tissue, brains, and spleens. It was proven that all those S. elegans-derived treatments reversed the damage, showing antidepressant, antihypertensive, antihyperglycemic, and antidyslipidemic effects and decreased adiposity, insulin resistance, and serum corticosterone. They induced a modulatory response by modifying the levels of TNF-α, IL-1β, IL-6, and IL-10 in different organs. High-performance liquid chromatography (HPLC) analysis of the acetate of ethyl fraction from S. elegans (SeFAc) fraction revealed the presence of rosmarinic and caffeic acids as well as flavonoids, while the fraction from SeFAc called SeF3 Was identified by gas mass as methyl glucose, glycerol, and known sterols, among others. Thus, it was concluded that S. elegans protects against the harmful effects of MetS.

The ovicidal and larvicidal effect of a full aqueous extract (FE) and two phases: an aqueous (Aq-Ph) and an ethyl acetate (EtOAc-Ph) from Ruta chalepensis (Rc) stems and leaves against Haemonchus contortus (Hc) were assessed. The egg hatching inhibition (EHI) assay and larval mortality (LM) test were performed by triplicate in 96-well micro-titration plates (n=4 wells). The FE against Hc eggs and larvae was assessed at 1.25, 2.5, 5, 10 and 20 mg/mL; and 30, 60, 90, 120,150 and 200 mg/ mL, respectively. The ovicidal effect of Aq-F and EtOAc-F was assessed at 1.25, 2.5, 5, 10 and 20 mg/mL. Plates were incubated at 28 °C for 48 (ovicidal assay) and 72 h (larvicidal assay). The EHI results were considered based on the mean number of eggs hatching failure after 48 h exposure. The LM was recorded after 72 h exposure to the Rc phases and expressed as mortality percentage. The Rc FE caused 96 and 100% EHI at 10 and 20 mg/mL, respectively; meanwhile, 74% LM was recorded at 200 mg/mL (p

In this study, we isolated from the aerial parts of Baccharis conferta Kunth (i) a new neoclerodane, denominated “bacchofertone”; (ii) four known terpenes: schensianol A, bacchofertin, kingidiol and oleanolic acid; and (iii) two flavonoids: cirsimaritin and hispidulin. All structures were identified by an exhaustive analysis of nuclear magnetic resonance (NMR) and mass spectroscopy (MS). Extracts from aerial parts were screened for anti-inflammatory activity in the mice ear edema model of 12-O-tetradecanoylforbol-13-acetate mice. Dichloromethane extract (BcD) exhibited 78.5 ± 0.72% inhibition of edema, followed by the BcD2 and BcD3 fractions of 71.4% and 82.9% respectively, at a dose of 1 mg/ear. Kingidiol and cirsimaritin were the most potent compounds identified, with a median effective dose of 0.12 and 0.16 mg/ear, respectively. A histological analysis showed that the topical application of TPA promoted intense cell infiltration, and this inflammatory parameter was reduced with the topical application of isolated compounds.

Spine implant infections portend disastrous outcomes, as diagnosis is challenging and surgical eradication is at odds with mechanical spinal stability. Current imaging modalities can detect anatomical alterations and anomalies but cannot differentiate between infection and aseptic loosening, diagnose specific pathogens, or delineate the extent of an infection. Herein, a fully human monoclonal antibody 1D9, recognizing the immunodominant staphylococcal antigen A on the surface of Staphylococcus aureus, was assessed as a nuclear and fluorescent imaging probe in a preclinical model of S. aureus spinal implant infection, utilizing bioluminescently labeled bacteria to confirm the specificity and sensitivity of this targeting. Postoperative mice were administered 1D9 probe dual labeled with 89-zirconium (89Zr) and a near infrared dye (NIR680) (89Zr-NIR680-1D9), and PET-CT and in vivo fluorescence and bioluminescence imaging were performed. The 89Zr-NIR680-1D9 probe accurately diagnosed both acute and subacute implant infection and permitted fluorescent image-guided surgery for selective debridement of infected tissue. Therefore, a single probe could noninvasively diagnose an infection and facilitate image-guided surgery to improve the clinical management of implant infections.

Objective: This study was conducted to investigate the antinociceptive and anti-inflammatory effect of ethyl acetate fraction of Oenothera rosea (EAOr) and the mechanism involved, in mice.Materials and Methods: The antinociceptive activity was tested using chemical- and heat-induced nociception models. The anti-inflammatory activity was tested using carrageenan-induced edema and inflammatory cytokines were measured.Results: EAOr reduced the licking time on the second phase of the formalin test (100 and 177 mg/kg). The antinociception of EAOr was prevented by L-NAME (10 mg/kg), 1H-[1, 2, 4]-oxadiazolo [4, 3-a]-quinoxalin-1-one (ODQ, 0.1 mg/kg), glibenclamide (10 mg/kg) and bicuculline (1 mg/kg), but not by naloxone (2 mg/kg). Also, EAOr decreased licking time in capsaicin induced-nociception. EAOr did not have effect on withdrawal latency in tail-flick test. Carrageenan-induced paw edema was reduced by EAOr, and TNF-α and IL-1β levels were reduced in mice treated with EAOr by 72.2 and 32.8%, respectively. Furthermore, EAOr did not present side effects as sedation nor gastric injury. Chemical analysis of this fraction showed the presence of glycosylated quercetin derivatives such as quercetin glucoside and quercetin rhamnoside in a 2.5% concentration.Conclusion: This study demonstrates antinociceptive and anti-inflammatory effect of an organic fraction of O. rosea and its possible interaction with the NO-cGMP-K+ channels and GABAergic system and thus, it could be considered a therapeutic alternative.

Salvia elegans Vahl is a plant commonly used in Mexico as a remedy for nervous disorders, inflammatory diseases, and "ringing in the ears"; the latter can be associated with arteriosclerotic conditions and arterial hypertension. Therefore, based on medicinal use, this work aimed to evaluate the hydroalcoholic extract (SeHA, 100 mg/kg) of this plant and two fractions, ethyl acetate (SeFAc, 50 mg/kg), and obtained from SeFAc fractionation denominated SeF3 (10 mg/kg), on several alterations derived from metabolic syndrome (MetS) derived from the ingestion of a high-calorie diet (high-fat diet), in ICR (Institute of Cancer Research) mice, leading to chronic inflammation that results in neurological damage such as depression. Therefore, several MetS-related parameters, such as forced swim tests, hypertension, serum corticosterone levels, glucose, triglycerides, cholesterol, adiposity index, and insulin resistance, will be evaluated. Additionally, tumor necrosis factor (TNF)-α, interleukin (IL)-1β, IL-6, and IL-10 levels were measured in kidneys, fat tissue, brains, and spleens. It was proven that all those S. elegans-derived treatments reversed the damage, showing antidepressant, antihypertensive, antihyperglycemic, and antidyslipidemic effects and decreased adiposity, insulin resistance, and serum corticosterone. They induced a modulatory response by modifying the levels of TNF-α, IL-1β, IL-6, and IL-10 in different organs. High-performance liquid chromatography (HPLC) analysis of the acetate of ethyl fraction from S. elegans (SeFAc) fraction revealed the presence of rosmarinic and caffeic acids as well as flavonoids, while the fraction from SeFAc called SeF3 Was identified by gas mass as methyl glucose, glycerol, and known sterols, among others. Thus, it was concluded that S. elegans protects against the harmful effects of MetS. [ABSTRACT FROM AUTHOR]

Background: Oenothera rosea L'Her Ex. Aiton, presenting antioxidant and anti-inflammatory activities, is traditionally used to treat bruises and headaches and as a healing agent. This study aimed to investigate whether its organic fraction (EAOr) has neuroprotective properties against neuroinflammation in the context of ischemia/reperfusion. Methods: The chemical composition of EAOr was determined using HPLC techniques, and its neuroprotective activities were evaluated in a common carotid-artery ligation model for the induction of ischemia/reperfusion (I/R). The animals were supplemented with EAOR for 15 days. On the last day, the animals were rested for one hour, following which the common carotid-artery ligation procedure was performed to induce I/R. The neurological deficit was evaluated at 24 h after I/R using Bederson's scale, and the relative expression of inflammatory genes and structure of hippocampal neurons were analyzed at 48 h. Results: The chemical analysis revealed five major compounds in EAOr: gallic acid, rutin, ellagic acid, and glucoside and rhamnoside quercetin. EAOr prevented neurological deficit 24 h after I/R; led to the early activation of the AIF and GFAP genes; reduced Nfkb1, IL-1beta, Il-6 and Casp3 gene expression; and protected hippocampal neurons. Conclusions: Our findings demonstrate that EAOr contains polyphenol-type compounds, which could exert a therapeutic effect through the inhibition of neuroinflammation and neuronal death genes, thus maintaining hippocampal neurons. [ABSTRACT FROM AUTHOR]

[alpha]-Amyrin, a natural pentacyclic triterpene, has an antihyperglycemic effect in mice and dual PPARS/y action in 3T3-L1 adipocytes, and potential in the control of type 2 diabetes (T2D). About 80% of glucose uptake occurs in skeletal muscle cells, playing a significant role in insulin resistance (IR) and T2D. Peroxisome-proliferator activated receptors (PPARs), in particular PPAR[delta] and PPAR[gamma], are involved in the regulation of lipids and carbohydrates and, along with adenosine-monophosphate (AMP) - activated protein kinase (AMPK) and protein kinase B (Akt), are implicated in translocation of glucose transporter 4 (GLUT4); however, it is still unknown whether [alpha]-Amyrin can affect these pathways in skeletal muscle cells. Our objective was to determine the action of [alpha]-Amyrin in PPARS, PPAR[gamma], AMPK, and Akt in C2C12 myoblasts. The expression of PPAR[delta], PPAR[gamma], fatty acid transporter protein (FATP), and GLUT4 was quantified using reverse transcription quantitative PCR and Western blot. [alpha]-Amyrin increased these markers along with phospho- AMPK (p-AMPK) but not p-Akt. Molecular docking showed that [alpha]-Amyrin acts as an AMPK-allosteric activator, and may be related to GLUT4 translocation, as evidenced by confocal microscopy. These data support that [alpha]-Amyrin could have an insulin-mimetic action in C2C12 myoblasts and should be considered as a bioactive molecule for new multitarget drugs with utility in T2D and other metabolic diseases. Key words: [alpha]-Amyrin, p-AMPK activation, dual PPAR[delta]/[gamma], GLUT4 translocation, triterpene. L'[alpha]-Amyrine, un triterpene pentacyclique naturel, a des effets anti-hyperglycemiques chez les souris et une double action PPAR[delta]/[gamma] dans les adipocytes 3T3-L1, avec le potentiel de participer a la maitrise du diabete de type 2 (DT2). Environ 80 % de la captation du glucose survient dans les cellules musculaires squelettiques, ce qui joue un role important dans la resistance a l'insuline et le DT2. Les recepteurs des proliferateurs de peroxysome actives (PPAR), en particulier les PPAR[delta] et les PPAR[gamma], participent a la regulation des lipides et des glucides et, de meme que la proteine kinase activee par l'adenosine monophosphate (AMPK) et que la proteine kinase B (Akt), jouent un role dans la translocation par le GLUT4 (pour << glucose transporter 4 >>). Cependant, on ne sait toujours pas si l'[alpha]-Amyrine peut affecter ces voies de signalisation dans les cellules musculaires squelettiques. L'objectif de ce travail etait d'etablir l'action de l'[alpha]-Amyrine sur les PPARS, les PPAR[gamma], l'AMPKet l'Akt dans des myoblasts C2C12. Nous avons quantifie l'expression des PPAR[delta], des PPAR[gamma], de FATP et de GLUT4 a l'aide de la technique de PCR quantitatif en temps reel et de l'immunobuvardage de Western. L'[alpha]-Amyrine entrainait une hausse de ces marqueurs avec celle de p-AMPK, mais pas de p-Akt. A l'aide de l'arrimage moleculaire, nous avons observe que l' [alpha]-amyrine agit comme un activateur allosterique de l'AMPK, et qu'elle peut etre liee a la translocation par le GLUT4, telle que mise en evidence par la microscopie confocale. Ces donnees viennent appuyer le fait que l'[alpha]-Amyrine pourrait mimer l'action de l'insuline dans les myoblasts C2C12 et que l'on devrait la considerer comme etant une molecule bioactive pour de nouveaux medicaments a cibles multiples dotes d'une utilite dans le DT2 et autres maladies du metabolisme. [Traduit par la Redaction] Mots-cles: [alpha]-Amyrine, activation de p-AMPK, double PPARS/y, translocation par le GLUT4, triterpene., Introduction The [alpha]-Amyrin, a pentacyclic triterpene found in a variety of medicinal plants, has hepatoprotective (Nogueira et al. 2019), anti-inflammatory (Da Silva Junior et al. 2017), and antihyperglycemic properties (Giacoman-Martinez [...]

Malva parviflora has shown anti-inflammatory, antihypertensive, antihyperlipidemic, and hypoglycemic effects. This study is aimed to evaluate the anti-adipogenic effect of M. parviflora on 3T3-L1 adipocytes. Fibroblast differentiation was induced either in the absence or presence of M. parviflora fractions (F3, F4, F7, F12, F13, F17, F18 and F19) for 4 days; F17 and 18 were the most effective fractions in reducing intracellular lipid accumulation (by 25.6% and 23.1%, respectively). EC50 of F17 and F18 (14 μg/mL and 17 μg/mL, respectively) were used to evaluate their anti adipogenic effect. After 10 days of inducing differentiation in the absence or presence of the extracts at the EC50 of F17 and F18, lipid accumulation, the concentration of interleukin 6 (IL-6) were measured in the culture medium; the presence of PPAR-γ, AKT, and p-AKT was also determined. In differentiated adipocytes (C2), F17 maintained intracellular lipid concentration at levels comparable to metformin, while decreasing PPAR-γ and increasing p-AKT presence; it also prevented IL-6 expression. F17 consists of alanine, valine, phenylalanine, and proline. On the other hand, F18 reduced intracellular lipid concentrations, prevented the increase of PPAR-γ and p-AKT, and maintained IL-6 expression at similar levels as metformin. F18 is mainly constituted by alanine, valine, proline, and sucrose. In conclusion, M. parviflora fractions (F17 and F18) control the process of adipogenesis, lipogenesis, and cellular dysfunction. [ABSTRACT FROM AUTHOR]

Arthrobotrys oligospora is a nematode-trapping fungus belonging to the family Orbiliaceae and one of the main antagonists of nematodes in soil, including plant and animal parasitic nematodes and free-living nematodes. This species develops three-dimensional adhesive nets in which nematodes are trapped, destroyed and consumed by the fungus. It also possesses other strategies to immobilise, kill and degrade nematodes, i.e. nematode-attractant substances, cuticle adhesion polymers and a number of nematocidal metabolites. The objective of this study was to assess the in vitro nematocidal activity of a strain of A. oligospora through its predatory activity and its liquid culture filtrates (LCF) against the ruminant parasite Haemonchus contortus (HcL3) and to investigate the presence of myco-compounds with potential nematocidal activity. Predatory activity (PA) was assessed in agar plates; 200 HcL3 were placed on agar plates with the fungus and a control group and incubated for 10 days. The LCF confrontation with nematodes was performed in microtiter plates. Two media, Czapek-Dox Broth (Cz-DB) and potato dextrose broth, were assessed. Three concentrations (25, 50 and 100 mg/mL) were assessed at 48 and 72 h (n = 4, per concentration). The experiment was performed in triplicate. The results showed 73.6 ± 2.7% PA and the highest mortality (83%) with the LCF in Cz-DB after 72 h. Gas chromatography–mass spectrometry (GC–MS) analysis revealed that the A. oligospora ethyl acetate phase was composed of 1,2-benzenedicarboxylic acid, bis (2-methylpropyl) ester, (M) 1,4-benzenedicarboxylic acid, bis (2-methylpropyl) ester and (M) decanedioic acid (2-ethylexyl) ester. These compounds could be responsible for nematocidal activity. [ABSTRACT FROM AUTHOR]

Haemonchus contortus is a blood-feeding gastrointestinal parasite that impacts grazing sheep, causing economic losses in animal production. Due to its anthelmintic resistance, alternative antiparasitic treatments like plant-based anthelmintics are necessary to explore. Artemisia cina (Asteraceae) is a plant whose n-hexane extract and ethyl acetate extract exhibit anthelmintic activity against H. contortus, the n-hexane more active. To discover additional bioactive metabolites, a chemical analysis was performed on ethyl acetate extract, which presented an LC90 of 3.30 mg/mL and allowed the isolation of 11-[(1R,5S,7R,8R,10S,)-1,8-dihydroxy-5,10-dimethyl-4-oxodecahydroazulen-7-yl] acrylic acid. This new sesquiterpene was identified through one and two-dimensional NMR. The compound was named cinic acid and displayed an LC50 of 0.13 (0.11–0.14) mg/mL and LC90 of 0.40 (0.37–0.44) mg/mL, which, compared with ethyl acetate extract larvicidal activity, was 256-fold more active at LC50 and 15.71-fold at LC90. In this study, a new sesquiterpene with larvicidal activity against H. contortus L3 infective larvae was isolated from the ethyl acetate extract of Artemisia cina. [ABSTRACT FROM AUTHOR]

Haemonchus contortus, a blood-feeding parasite in grazing sheep, causes economic losses. Drug resistance necessitates exploring plant-based anthelmintics like Artemisia cina (Asteraceae). The plant, particularly its ethyl acetate extract, shows anthelmintic activity against H. contortus. However, there is limited information on pharmacodynamic interactions in ethyl acetate compounds. The study aims to identify pharmacodynamic interactions in the ethyl acetate extract of A. cina with anthelmintic effects on H. contortus eggs and L3 larvae using binary mixtures. Bioactive compounds were isolated via chromatography and identified using spectroscopic techniques. Pharmacodynamic interactions were assessed through binary mixtures with a main compound. Four bioactive compounds were identified: 1-nonacosanol, hentriacontane, peruvin, and cinic acid. Binary mixtures, with peruvin as the main compound, were performed. Peruvin/1-nonacosanol-hentriacontane and peruvin/cinic acid mixtures demonstrated 1.42-fold and 4.87-fold increased lethal effects in H. contortus L3 infective larvae, respectively, at a 0.50LC25/0.50LC25 concentration. In this work, we determined the synergism between bioactive compounds isolated from the ethyl acetate extract of A. cina and identified unreported compounds for the specie. [ABSTRACT FROM AUTHOR]