Search

Depressive and anxiety disorders constitute some of the most prevalent mental disorders around the world. For years, the development of new lead compounds for drug discovery in this field has been an area of great attention. Recently, a series of tetrahydrocarbazole derivatives have demonstrated important anxiolytic-like activity, associated with their structures and stereochemistry. Here, we present a study of the antidepressant effect and anxiolytic-like activity of a fused thiopyrano-piperidone-tetrahydrocarboline (compound 4). The antidepressant and anxiolytic-like effects of 4 (1–50 mg/kg p.o.) were assessed with the tail suspension test and the hole-board test, respectively. This study determined the possible mechanisms involved in the anxiolytic-like actions of 4 using inhibitors or neurotransmission and evaluated its interaction with 5HT2A receptors using a molecular docking study. As an analog to the tetrahydrocarbazole core, the tetrahydrocarboline derivative showed anxiolytic-like activity (ED50 = 13 mg/kg p.o.) in the hole-board test, with a comparable effect to the reference drug, 1.5 mg/kg clonazepam, with the possible participation of the serotonergic system. [ABSTRACT FROM AUTHOR]

Stanhopea tigrina Bateman ex Lindl. (Orchidaceae) is an orchid endemic to Mexico, known as "Calavera" or "calaverita", in the Huasteca Potosina (central region of Mexico). This plant species is used for the folk treatment of mental disorders and urological kidney disorders, according to the ethnomedicinal information obtained in this study. Ethanolic extracts of leaves (HE) and pseudobulb (PE) were obtained by microwave-assisted extraction (MAE). Gas Chromatography coupled with Mass Spectrometry (GC-MS) was used to carry out the chemical characterization of HE and PE. The pharmacological effects (antioxidant, diuretic, anxiolytic, locomotor, hypnotic, and sedative) of HE and PE were evaluated. The possible mechanism of action of the anxiolytic-like activity induced by HE was assessed using inhibitors of the GABAergic, adrenergic, and serotonergic systems. The possible mechanism of the diuretic action of HE was assessed using prostaglandin inhibitory antagonists and nitric oxide synthase (NOS) blockers. HE at 50 and 100 mg/kg exerted anxiolytic-like activity without inducing hypnosis or sedation. Flumazenil, prazosin, and ketanserin inhibited the anxiolytic-like activity shown by HE, which suggests the participation of GABA, α1-adrenergic receptors, and 5-HT2 receptors, respectively. The diuretic effect was reversed by the non-selective NOS inhibitor L-NAME, which caused the reduction in nitric oxide (NO). These results demonstrate that the ethanolic extract of S. tigrina leaves exhibited anxiolytic-like activity and diuretic effects without inducing hypnosis or sedation. This work validates the medicinal uses of this orchid species. [ABSTRACT FROM AUTHOR]

Nitrogen‐containing drugs represent one of the worldwide most extensive sources of treatments for different diseases. Indomethacin as example, is one of the most important non‐steroidal anti‐inflammatories (NSAID) indol‐containing drug. Its relevance has been demonstrated the last 50 years with excellent pharmacological results. Its efficacy as an anti‐inflammatory treatment, inspired us the exploration of indol‐containing structurally less elaborated compounds which kept and/or improve the anti‐inflammatory activity compared with indomethacin. Herein is summarized and discussed our initial findings on the synthesis and anti‐inflammatory effect of different 2,3‐diarylindoles, designed for strategically favoring the plausible and selective interactions with COX‐2, on route to new simple NSAID scaffolds. The TPA model and formalin test were used in this study to generate inflammation in mice for conducting the assays with the synthesized 2,3‐diarylindoles. Docking analysis revealed stronger N−H indolic interactions with COX‐2 for 6‐methoxy‐2‐phenyl‐3‐(4‐chlorophenyl)‐1H‐indole, one of the most active of the synthesized compounds when compared with indomethacin. This, experimentally match with the anti‐inflammatory observed effect and putatively indicates the biochemical action mechanism. [ABSTRACT FROM AUTHOR]

Introduction: The presence of a positional compression of the neurovascular bundle in the outlet between the thorax and the upper limb during arm movements (mainly abduction) is common but remains asymptomatic in most adults. Nevertheless, a certain number of subjects with thoracic outlet positional compression will develop incapacitating symptoms or clinical complications as a result of this condition. Symptomatic forms of positional neurovascular bundle compression are referred to as "thoracic outlet syndrome" (TOS). Materials and methods: This paper aims to review the literature and discuss the interactions between aspects of patients' lifestyles in TOS. The manuscript will be organized to report (1) the historical importance of lifestyle evolution on TOS; (2) the evaluation of lifestyle in the clinical routine of TOS-suspected patients, with a description of both the methods for lifestyle evaluation in the clinical routine and the role of lifestyle in the occurrence and characteristics of TOS; and (3) the influence of lifestyle on the treatment options of TOS, with a description of both the treatment of TOS through lifestyle changes and the influence of lifestyle on the invasive treatment options of TOS. Results: We report that in patients with TOS, lifestyle (1) is closely related to anatomical changes with human evolution; (2) is poorly evaluated by questionnaires and is one of the factors that may induce symptoms; (3) influences the sex ratio in symptomatic athletes and likely explains why so many people with positional compression remain asymptomatic; and (4) can sometimes be modified to improve symptoms and potentially alter the range of interventional treatment options available. Conclusions: Detailed descriptions of the lifestyles of patients with suspected TOS should be carefully analysed and reported. [ABSTRACT FROM AUTHOR]

Gymnosperma glutinosum (Spreng) Less (Asteraceae) is a shrub used in traditional medicine for the treatment of inflammatory and renal diseases. The ent‐dihydrotucumanoic acid (DTA) is a diterpene obtained from G. glutinosum. This study evaluated the antioxidant, genotoxic, and diuretic properties of DTA, as well as its in vitro and in vivo anti‐inflammatory actions. The antioxidant actions of DTA were assessed with the 2,2′‐azino‐bis (3‐ethylbenzothiazoline‐6‐sulphonic acid) (ABTS), ferric reducing antioxidant power (FRAP), and 2,2′‐diphenyl‐1‐picrylhydrazyl (DPPH) assays, the genotoxic action was assessed with the comet assay, and the diuretic effects of DTA were assessed using metabolic cages. The anti‐inflammatory actions were evaluated using primary murine peritoneal macrophages stimulated with LPS and the λ‐carrageenan‐induced hind paw edema test. DTA lacked antioxidant (IC50 > 25,000 μg/mL) activity in the ABTS, FRAP, and DPPH assays. DTA at 500–1,000 μg/mL showed moderate genotoxicity. In LPS‐stimulated macrophages, DTA showed IC50 values of 74.85 μg/mL (TNF‐α) and 58.12 μg/mL (NO), whereas the maximum inhibition of IL‐6 (24%) and IL‐1β (36%) was recorded at 200 μg/mL. DTA induced in vivo anti‐inflammatory effects with ED50 = 124.3 mg/kg. The in vitro anti‐inflammatory activity of DTA seems to be associated with the decrease in the release of TNF‐α and NO. DTA promoted the excretion of urine (ED50 = 86.9 mg/kg), Na+ (ED50 = 66.7 mg/kg), and K+ (ED50 = 8.6 mg/kg). The coadministration of DTA with L‐NAME decreased the urinary excretion shown by DTA alone. Therefore, the diuretic activity is probably associated with the participation of nitric oxide synthase. In conclusion, DTA exerted anti‐inflammatory and diuretic effects, but lacked antioxidant effects. [ABSTRACT FROM AUTHOR]

This paper provides evidence of the effects of urban wastewater discharges on the trophic state and environmental quality of a coastal water body in a semiarid subtropical region in the Gulf of California. The concentrations of dissolved inorganic nutrients and organic matter from urban wastewater primary treatment were estimated. La Salada Cove was the receiving water body and parameters measured during an annual cycle were temperature, salinity, dissolved oxygen, nitrite, nitrate, ammonia, orthophosphate, and chlorophyll a. The effects of sewage inputs were determined by using Trophic State Index (TRIX) and the Arid Zone Coastal Water Quality Index (AZCI). It was observed that urban wastewater of the city of Guaymas provided 1,237 ton N yr(-1) and 811 ton P yr(-1) and TRIX indicated that the receiving water body showed symptoms of eutrophication from an oligotrophic state to a mesotrophic state; AZCI also indicated that the environmental quality of the water body was poor. The effects of urban wastewater supply with insufficient treatment resulted in symptoms of eutrophication and loss of ecological functions and services of the coastal ecosystem in La Salada Cove. [ABSTRACT FROM AUTHOR]

Argemone ochroleuca Sweet (Papaveraceae) is used in folk medicine as a sedative and hypnotic agent. This study aimed to evaluate the anxiolytic-like, sedative, antidepressant-like, and anticonvulsant activities of a dichloromethane extract of A. ochroleuca stems (AOE), chemically standardized using gas chromatography–mass spectrometry (GC–MS), and its active compound dihydrosanguinarine (DHS). The anxiolytic-like, sedative, antidepressant-like, and anticonvulsant activities of the AOE (0.1–50 mg/kg p.o.) and DHS (0.1–10 mg/kg p.o.) were evaluated using murine models. A possible mechanism for the neurological actions induced by the AOE or DHS was assessed using inhibitors of neurotransmission pathways and molecular docking. Effective dose 50 (ED50) values were calculated by a linear regression analysis. The AOE showed anxiolytic-like activity in the cylinder exploratory test (ED50 = 33 mg/kg), and antidepressant-like effects in the forced swimming test (ED50 = 3 mg/kg) and the tail suspension test (ED50 = 23 mg/kg), whereas DHS showed anxiolytic-like activity (ED50 = 2 mg/kg) in the hole board test. The AOE (1–50 mg/kg) showed no locomotive affectations or sedation in mice. A docking study revealed the affinity of DHS for α2-adrenoreceptors and GABAA receptors. The anxiolytic-like and anticonvulsant effects of the AOE are due to GABAergic participation, whereas the antidepressant-like effects of the AOE are due to the noradrenergic system. The noradrenergic and GABAergic systems are involved in the anxiolytic-like actions of DHS. [ABSTRACT FROM AUTHOR]

Introduction The surgical management that achieves minimal morbidity and mortality for patients with glomus and non-glomus tumors involving the jugular foramen (JF) region requires a comprehensive understanding of the complex anatomy, anatomic variability, and pathological anatomy of this region. Objective The aim of this study is to propose a rational guideline to expose and preserve the lower cranial nerves (CNs) in the lateral approach of the JF. Methods The technique utilized is the gross and microdissection of 4 fixed cadaveric heads to revise the JF's surgical anatomy and high part of the carotid sheath compared with surgical cases to understand and preserve the integrity of lower CNs. The method involves radical mastoidectomy, microdissection of the JF, facial nerve, and high neck just below the carotid canal and the JF. The CNs IX, X, XI, and XII are microscopically dissected and kept in sight up to the JF. Results This study realized well the surgical and applied anatomy of the lower CNs with relation to the facial nerve and JF. Conclusions The JF anatomy is complicated, and the key to safely operate on it and preserving the lower CNs is to find the posterior belly of the digastric muscle, to skeletonize the facial nerve, to remove the mastoid tip preserving the stylomastoid foramen, to skeletonize the sigmoid sinus and posterior fossa dura not only anterior but also posteroinferior to reach and drill the jugular tubercle. [ABSTRACT FROM AUTHOR]

The prevailing tectonic setting in the Gulf California suggests the presence of an undetermined number of short spreading centres with associated hydrothermal systems. However, to date, active seafloor spreading phenomena have been documented in only three of the eight tectonically active basins. Here we report heat flow values as high as 15,436?mW?m?2 in two of the northernmost basins of the Gulf of California, providing evidence of intense hydrothermal activity associated with the transition from continental rifting to seafloor spreading. The mean heat flow for the Wagner and Consag basins area is 1,875?mW?m?2, more than 15 times higher than the mean value for oceanic crust (105.4?mW?m?2). Additional evidence for vigorous hydrothermal circulation and a shallow heat source includes intense gas discharge (CO2 and CH4), widespread low pH (average 7.7), locally high 222Rn concentrations in the bottom water and a high extent of organic matter maturation in the sediments. [ABSTRACT FROM AUTHOR]

Aim: To determine whether the use of 3D anatomical models is helpful to students and enhances their anatomical knowledge. Methods: First year undergraduate students on the speech therapy or hearing aid practitioner courses attended either a lecture alone or a lecture followed by a 3D anatomy based tutorial, the latter which was also attended by ENT residents. Participants who received the tutorial were free to use the 3D model on the university computers or on their home computer and were then asked to answer a satisfaction questionnaire. At the end of the first year examinations, the grades of the undergraduate students were compared between the lecture alone group and lecture plus tutorial group. Results: Generally, all participants found this new tool interesting and user-friendly for the learning of temporal bone anatomy. However, most also considered the help of a teacher indispensable to guide them through the virtual dissection. First year undergraduate students who received the 3D anatomy tutorial performed significantly better during their end of year examination compared to those receiving a lecture alone, particularly concerning the more difficult questions. Conclusion: The 3D anatomical software, used in parallel with traditional teaching methods, such as lectures and cadaver dissection, appears to be a promising tool to improve student learning of temporal bone anatomy. [ABSTRACT FROM AUTHOR]

Background: Pediatric self-medication is based on the subjective interpretation of symptoms in children by the mother or an adult, the decision to self-medicate is made by a third party. The objective of this work is to provide information on the factors and practices associated with the self-medication of children among parents in Mexico. Methods: A cross-sectional and descriptive study was conducted between June 2020 and December 2021 on Mexican parents with children under 12 years of age. Online questionnaires were completed with sections on sociodemographic characteristics, use of medicines or medicinal plants and their treated symptoms, sources of collection, and their recommendation. Results: A total of 9905 online surveys were completed with representation from the 32 states of Mexico, and the prevalence of self-medication was 49.6% (n = 4908). Associated factors were age, having two or more children, children with chronic illnesses, medium educational level, unemployment or employment unrelated to health, medium and high socioeconomic level, and lack of medical security. Respondents self-medicated their children on the recommendation of a family member or friend (55.8%), and own initiative (28%). The most used medication was VapoRub (61.3%), followed by paracetamol (56.9%) and chamomile (33.1%), and the most prevalent symptoms were flu/flow (47.7%) followed by cough (34.2%). The main reasons were perceiving symptoms as not serious (69.9%) and reusing medications (51.9%). Conclusions: There is a high prevalence of self-medication in children in Mexico, mainly associated with children with chronic diseases and families with three or more children. [ABSTRACT FROM AUTHOR]

Objectives: To assess the importance of 2 variables, transducer tip diameter and resection of the round window (RW) niche, affecting the optimization of the mechanical stimulation of the RW membrane with an active middle ear implant (AMEI). Materials and Methods: Ten temporal bones were prepared with combined atticotomy and facial recess approach to expose the RW. An AMEI stimulated the RW with 2 ball tip diameters (0.5 and 1.0 mm) before and after the resection of the bony rim of the RW niche. The RW drive performance, assessed by stapes velocities using laser Doppler velocimetry, was analyzed in 3 frequency ranges: low (0.25–1 kHz), medium (1–3 kHz) and high (3–8 kHz). Results: Driving the RW produced mean peak stapes velocities (HEV) of 0.305 and 0.255 mm/s/V at 3.03 kHz, respectively, for the 1- and 0.5-mm tips, with the RW niche intact. Niche drilling increased the HEV to 0.73 and 0.832 mm/s/V for the 1- and 0.5-mm tips, respectively. The tip diameter produced no difference in output at low and medium frequencies; however, the 0.5-mm tip was 5 and 6 dB better than the 1-mm tip at high frequencies before and after niche drilling, respectively. Drilling the niche significantly improved the output by 4 dB at high frequencies for the 1-mm tip, and by 6 and 10 dB in the medium- and high-frequency ranges for the 0.5-mm tip. Conclusion: The AMEI was able to successfully drive the RW membrane in cadaveric temporal bones using a classical facial recess approach. Stimulation of the RW membrane with an AMEI without drilling the niche is sufficient for successful hearing outputs. However, the resection of the bony rim of the RW niche significantly improved the RW stimulation at medium and higher frequencies. Drilling the niche enhances the exposure of the RW membrane and facilitates positioning the implant tip. Copyright © 2010 S. Karger AG, Basel [ABSTRACT FROM AUTHOR]

Objective; The aim of this study is to determine the effect of vestibular neurotomy in the evolution of unilateral Meniere'disease towards bilaterality and in hearing preservation in such selected patients. Materials & Methods; Retrospective chart review of 328 incapacitating Meniere's disease patients who underwent retrosigmoïd vestibular neurotomy between 1993 to 2006. The main duration of the follow up time was 4 years (1 to 15 years). Results; Out of 328 patients, 18 (5,5 %) presented a bilateral disease with the following group distribution. Group I : 5 patients (1,6 %) developed bilateral Meniere after unilateral vestibular neurotomy. On the operated side, hearing was preserved in 60 % (3/5) and worsened in 40 % (2/5). Group II : 11 bilateral Meniere's disease patients before vestibular neurotomy on the active side. On the operated side, hearing was preserved in 73 % (8/11) and worsened in 27 % (3/11). Groupe III : 2 patients with bilateral vestibular neurotomy. Conclusion; Vestibular neurotomy is not only an effective procedure to control vertigo but also for reducing both the rate of developing Meniere's disease in the uninvolved ear (5 out 315 patients, 1,6 %) and the rate of hearing impairment on the operated ear. [ABSTRACT FROM AUTHOR]

Summary: The present study was undertaken to develop an improved cryoembedding method for analysis of mice and rat cochleae, which permits high-quality cryosections and preserves overall structure and cellular resolution as shown by hematoxylin/eosin staining. The preservation of morphology and antigenicity is mandatory to achieve optimal results. A total of 20 male cd/1 mice and 14 male Sprague-Dawley rats were used in experiments for optimization of preservation, fixative, decalcification, embedding and cryosectioning of cochleae from adult and aged rodents. In addition, a novel immunohistochemical procedure (using Hydroxyprobe™-1 kit) was developed for detecting regions of hypoxia in mice and rat cochlea. This method employs a primary fluorescent-conjugated monoclonal antibody directed against pimonidazole protein adducts that are created in hypoxic tissues. Subsequent studies of hypoxia inducible factor-1α (HIF-1α) by immunofluorescence in the cochlea of these animals were performed in order to confirm that immunochemical detection of pimonidazole protein is representative of a hypoxic environment. We conclude that the present method results in high-quality cryosections of cochlear tissues presenting good anatomical and histological preservation. Furthermore, our optimized procedures provide novel tools for the investigation of neuro-sensory-epithelium in physio-pathological situations associated with hypoxia and/or ischemia, such as inner ear development, plasticity, regeneration and senescence. [Copyright &y& Elsevier]

The first iodine(III)-based procedure for the benzylic oxidation of different arenes is described by using the (PhIO)n/Al(NO3)3 system under catalytic conditions leading to the formation of the corresponding carbonyl derivatives. The method proceeds under mild, operationally simple, room temperature, short reaction times, and open flask conditions. In light of the organocatalysis relevance and the novelty of our protocol, we wish to communicate our initial results of this novel oxidation. [ABSTRACT FROM AUTHOR]

Abstract Ethnopharmacological relevance Mexico ranks second in the world for obesity prevalence. In Mexico, obese and overweight subjects commonly seek alternative treatments for weight-loss, including the use of herbal products. Aim of the study The main objective of this study was to evaluate the prevalence of self-medication with herbal products for weight-loss among overweight and obese subjects residing in four states (Guanajuato, San Luis Potosi, State of Mexico, and Mexico City) from central Mexico. In addition, the factors related to self-medication among patients were studied. Materials and methods A total of 1404 overweight and obese subjects were interviewed. A chi-square test examined associations between socio-demographic and socio-economic information, and self-medication with herbal products for weight-loss. Results The prevalence of self-medication was 42.9% among the participants who used herbal products for weight-loss. The female gender was the strongest factor (OR: 2.20 (1.75–2.77) associated with self-medication for weight-loss, followed by a low educational level (elementary and middle school) [OR: 1.80 (1.31–2.44)], and a middle-socioeconomic status [OR: 1.75 (1.21–2.52)]. The main herbal products used for weight-loss were based on: i) green tea, Camellia sinensis (12.7% of frequency), ii) aceitilla, Bidens odorata (6.6%), and iii) soybean, Glycine max (5.3%). In addition, 65% of the respondents considered herbal products ineffective for weight-loss after 6 months of use. Conclusion Due to the high incidence of overweight and obesity in Mexico, there is a high prevalence (42.9%) of self-medication using natural products for weight-loss, particularly in women from Central Mexico. This study indicates the important need to educate patients about the harmful effects of consuming these products. Graphical abstract fx1 [ABSTRACT FROM AUTHOR]