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Chronic noncommunicable diseases are a global health problem causing increased rates of mortality and sick leaves, which can be reduced by controlling dyslipidemia and hyperglycemia. Experimental and clinical studies have demonstrated the antidiabetic, lipid-lowering, antiobesogenic, anti-inflammatory, and antihypertensive properties of cinnamon; therefore, its use in yogurt can help reverse the effects of these diseases. Our study aims to evaluate the effect of a microencapsulated aqueous extract of cinnamon (Cinnamomum zeylanicum) (MCE Cz) incorporated in a yogurt drink on metabolic syndrome (MS) in a rabbit (Oryctolagus cuniculus). Physicochemical, microbiological, and proximal chemical characterization; total phenol, flavonoid, and 2,2-diphenyl-1-picrylhydrazil activity quantification; intestinal bioaccessibility; sensory analysis; MS induction through diet; and treatment with 5, 10, and 20 mg/kg of flavonoids contained in the MCE Cz were performed to help evaluate morphological, biochemical, and lipid peroxidation measurements in the liver and heart. The results show that the addition of MCE Cz in the yogurt modified the yogurt texture, increased its adhesiveness and firmness, and imparted a characteristic cinnamon color and biological value by providing intestinally bioaccessible antioxidants with antioxidant potential by reducing lipoperoxidation in the liver and heart after treatment. MCE Cz reduced the weight of the animals by up to 38.5% and the abdominal circumference by 29%. Biochemically, it decreased glucose levels by 24.38%, total cholesterol levels by 69.2%, triglyceride levels by 72.69%, and low-density lipoprotein levels by 89.25%; it increased high-density lipoprotein levels by 67.08%. Therefore, adding MCE Cz in doses of 5 and 10 mg of flavonoids in drinkable yogurt can be an alternative to preparing functional foods with physicochemical attributes and biological properties that can be consumed at all stages of life without undesirable effects. Moreover, it can act as a potential adjuvant in the treatment of comorbidities related to MS.
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Cinnamomum zeylanicum , Síndrome Metabólico , Extractos Vegetales , Yogur , Animales , Conejos , Cinnamomum zeylanicum/química , Síndrome Metabólico/dietoterapia , Yogur/análisis , Extractos Vegetales/administración & dosificación , Extractos Vegetales/química , Extractos Vegetales/farmacología , Masculino , Alimentos Fortificados/análisis , Flavonoides/análisis , Flavonoides/administración & dosificación , Composición de Medicamentos , HumanosRESUMEN
Recently, the use of nanotechnology in food has gained great interest. Iron nanoparticles with unique chemical, physical and structural properties allow their potential use mainly as iron fortifiers, colorants and antimicrobial agents. However, in the market we can find only supplements and food colorants based on iron nanoparticles. Their use in food fortification has so far been focused only on in vitro and in vivo experimental studies, since the toxicological evaluation of these studies has so far been the basis for the proposals of laws and regulations, which are still in an early stage of development. Therefore, the aim of this work was to summarize the use of the different forms of iron nanoparticles (oxides, oxyhydroxides, phosphates, pyrophosphates and sulfates) as food additives and supplements and to resume the perspectives of legislation regarding the use of these types of nanoparticles in the food industry.
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Metabolic syndrome (MetS) predisposes individuals to chronic non-communicable diseases (NCDs) like type 2 diabetes (T2D), non-alcoholic fatty liver disease, atherosclerosis, and cardiovascular disorders caused by systemic inflammation, intestinal dysbiosis, and diminished antioxidant ability, leading to oxidative stress and compromised insulin sensitivity across vital organs. NCDs present a global health challenge characterized by lengthy and costly pharmacological treatments. Complementary and alternative medicine using herbal therapies has gained popularity. Approximately 350,000 plant species are considered medicinal, with 80% of the world's population opting for traditional remedies; however, only 21,000 plants are scientifically confirmed by the WHO. The Rubiaceae family is promissory for preventing and treating MetS and associated NCDs due to its rich content of metabolites renowned for their antioxidative, anti-inflammatory, and metabolic regulatory properties. These compounds influence transcription factors and mitigate chronic low-grade inflammation, liver lipotoxicity, oxidative stress, and insulin resistance, making them a cost-effective non-pharmacological approach for MetS prevention and treatment. This review aims to collect and update data that validate the traditional uses of the Rubiaceae family for treating MetS and associated NCDs from experimental models and human subjects, highlighting the mechanisms through which their extracts and metabolites modulate glucose and lipid metabolism at the molecular, biochemical, and physiological levels.
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BACKGROUND: Preclinical and clinical evidence implies that destructive therapies in local and malignant tissue are frequently used on patients with head and neck cancer. Consequently, the microbiome of the treated and adjacent regions is affected. Disruption of the normal microbiome plays an important role not only in the disease progression but also in its emergence, therefore new therapies involving probiotics, prebiotics, and synbiotics have been developed to control or regulate this microbial disruption. OBJECTIVE: This review aims to describe the current and potential uses of probiotics at different stages of development of head and neck squamous cell carcinoma, as an adjuvant therapy to prevent common complications such as radiation-induced oral mucositis (RIOM) and its role in other areas. METHODS: Currently, there is no widely effective strategy to treat or prevent this kind of cancer. Surgery, radiation therapy, and chemotherapy are the three main treatments for head and neck cancer. Some therapies can also cause long-term health problems, or complications which might change the way you eat, talk, hear and breathe. RESULTS: The main uses for which probiotics have been studied are: Prevention and reduction of severity of RIOM, change in dental plaque to reduce dysbiosis, and reduction of complications in post-operated patients. Potential uses of probiotics include the reduction of disease initiation and progression by reducing local inflammation caused by bacteria and other organisms. CONCLUSION: The incidence and severity of RIOM may be lessened by probiotics. To establish its uses in additional clinical settings, though, more studies are necessary.
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Neoplasias de Cabeza y Cuello , Probióticos , Estomatitis , Simbióticos , Humanos , Probióticos/uso terapéutico , Neoplasias de Cabeza y Cuello/terapia , Neoplasias de Cabeza y Cuello/complicaciones , Prebióticos , Estomatitis/etiología , Estomatitis/prevención & controlRESUMEN
Pamabrom is a diuretic that is effective in treating premenstrual syndrome and primary dysmenorrhea. The aim of this study was to examine the effect of metformin and modulators of the opioid receptor-nitric oxide (NO)-cyclic guanosine monophosphate (cGMP)-K+ channel pathway on the local antinociception induced by pamabrom. The rat paw 1% formalin test was used to assess the effects. Rats were treated with local administration of pamabrom (200-800 µg/paw) or indomethacin (200-800 µg/paw). The antinociception of pamabrom or indomethacin was evaluated with and without the local pretreatment of the blockers. Local administration of pamabrom and indomethacin produced dose-dependent antinociception during the second phase of the test. Local pretreatment of the paws with naloxone (50 µg/paw), l-nitro-arginine methyl ester (10-100 µg/paw), or 1H-(1,2,4)-oxadiazolo[4,2-a]quinoxalin-1-one (10-100 µg/paw) reverted the antinociception induced by local pamabrom, but not of indomethacin. Similarly, the K+ channel blockers glibenclamide, glipizide, 4-aminopyridine, tetraethylammonium, charybdotoxin, or apamin reverted the pamabrom-induced antinociception, but not of indomethacin. Metformin significantly blocked the antinociception of pamabrom and indomethacin. Our data suggest that pamabrom could activate the opioid receptor-NO-cGMP-K+ channel pathway to produce its peripheral antinociception in the formalin test. Likewise, a biguanide-dependent mechanism could be activated by pamabrom and indomethacin to generate antinociception.
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Metformina , Naloxona , Femenino , Ratas , Animales , Naloxona/farmacología , GMP Cíclico/metabolismo , Ratas Wistar , Óxido Nítrico/metabolismo , Diuréticos , Metformina/farmacología , Indometacina , Receptores Opioides , Analgésicos/farmacología , Bloqueadores de los Canales de Potasio/farmacologíaRESUMEN
BACKGROUND: Non-alcoholic fatty liver disease (NAFLD) is now considered the most common chronic liver disease worldwide. NAFLD is related to changes in lipid metabolism and is characterized by the increase or accumulation of fat in hepatocytes that may progress to nonalcoholic steatohepatitis (NASH), which leads to the appearance of inflammatory processes. Treatment consists of changes in diet, physical activity, and weight control; however, these disorders represent a health problem and require the development of novel alternatives to treatment and prevention. NAFLD/NASH are strongly associated with other disorders, such as metabolic syndrome (MetS); in fact, NAFLD is considered the hepatic manifestation of MetS. These disorders are related to other components of MetS, including dyslipidemia, which is characterized by an imbalance in blood cholesterol and triglyceride levels. Prebiotics and probiotics benefit from treating and preventing several ailments, including liver diseases. Specifically, in dyslipidemia, NAFLD, and NASH, probiotics play a fundamental role in conducting the biotransformation of primary bile acids into secondary bile acids, which generally have important activity as immunomodulators and metabolism regulators. The mechanisms of action of pre and probiotics involve the activity of bile acid receptors, such as FXR and TGR-5, and the events resulting from their activation. Therefore, prebiotics and probiotics may be reasonable options to prevent and treat metabolic- related liver diseases.
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Dislipidemias , Síndrome Metabólico , Enfermedad del Hígado Graso no Alcohólico , Probióticos , Humanos , Enfermedad del Hígado Graso no Alcohólico/terapia , Enfermedad del Hígado Graso no Alcohólico/metabolismo , Prebióticos , Hígado/metabolismo , Probióticos/uso terapéutico , Síndrome Metabólico/metabolismo , Dislipidemias/tratamiento farmacológico , Dislipidemias/metabolismo , Ácidos y Sales Biliares/metabolismoRESUMEN
OBJECTIVE: Primary dysmenorrhea has a high prevalence among the student population. The objective of this study was to determine the prevalence of dysmenorrhea, its severity and its impact on academic performance in Mexican university students. METHODS: Cross-sectional study. An anonymous multiple-choice questionnaire was applied in class hours in the classrooms. The visual pain scale (VAS) was used for the measurement of pain. A descriptive and inferential analysis of the variables studied was carried out using the program SPSS® IBM. RESULTS: A total of 2154 (n=2154) students were surveyed. The average age of the women was 20.4 ±1.9years. The general prevalence of dysmenorrhea was 78.9%, with psychology students having the highest value (83.7%). The VAS mean pain score was of 64.0. The severity of menstrual pain in students was reported as mild in 9.0%, and moderate-severe in 91.0%. The VAS mean pain scores and intensity of pain of gerontology students were significantly higher than those reported by dentistry and medicine students (P<.05). Limitation of daily activities was reported in 90.4% of women, with medical students reporting the highest percentage (93.3%). Women reported school absenteeism in 37.0%, with medical students presenting the highest percentage (41.4%). The severity of menstrual pain as a risk factor (independent variable) positively influenced various dependent variables involved in students' academic performance (P<.05), including: stop doing their activities due to pain in 1 to 6 menstruations a year, minor concentration, absenteeism, low school performance, and lower grades during dysmenorrhea. CONCLUSION: A high prevalence of dysmenorrhea was observed and it is concluded that the severity of the symptomatology significantly interferes with the academic performance of the participants.
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Rendimiento Académico , Estudiantes de Medicina , Adolescente , Adulto , Estudios Transversales , Dismenorrea/epidemiología , Dismenorrea/psicología , Femenino , Humanos , Universidades , Adulto JovenRESUMEN
Objetivo: La dismenorrea primaria tiene una alta prevalencia entre la población estudiantil. El objetivo de este estudio fue determinar la prevalencia de la dismenorrea, su gravedad y su impacto en el rendimiento académico en estudiantes universitarias mejicanas. Métodos: Estudio transversal. Se aplicó un cuestionario anónimo de opción múltiple durante las horas lectivas de clase. La escala visual del dolor (EVA) fue usada para la medición del dolor. Se realizó un análisis descriptivo e inferencial de las variables a estudio mediante el programa SPSS® IBM. Resultados: Se encuestó a un total de 2.154 estudiantes, con una edad media de 20,4 ±1,9años. La prevalencia general de dismenorrea fue del 78,9%, encontrándose la mayor prevalencia en las estudiantes de psicología (83,7%). La puntuación media de dolor de la escala EVA fue de 64,0. Se encontró que la gravedad del dolor menstrual en las estudiantes fue leve en el 9,0% y moderada-severa en el 91,0%. Las puntuaciones medias de dolor de la EVA y la intensidad del dolor de los estudiantes de gerontología fueron significativamente más altas que las reportadas por las estudiantes de odontología y medicina (p<0,05). La limitación de las actividades diarias se informó en el 90,4% de las mujeres y las estudiantes de medicina fueron el porcentaje más alto (93,3%). Las mujeres informaron absentismo escolar en el 37,0%, siendo las estudiantes de medicina las que presentaron el porcentaje más alto (41,4%). La severidad del dolor menstrual como factor de riesgo (variable independiente) influyó positivamente en varias variables dependientes involucradas en el rendimiento académico de las estudiantes (p<0,05), incluyendo: dejar de hacer sus actividades (30min a 6h) debido al dolor en 1 a 6 menstruaciones al año, concentración menor, absentismo, rendimiento escolar bajo y calificaciones más bajas durante la dismenorrea.(AU)
Objective: Primary dysmenorrhea has a high prevalence among the student population. The objective of this study was to determine the prevalence of dysmenorrhea, its severity and its impact on academic performance in Mexican university students. Methods: Cross-sectional study. An anonymous multiple-choice questionnaire was applied in class hours in the classrooms. The visual pain scale (VAS) was used for the measurement of pain. A descriptive and inferential analysis of the variables studied was carried out using the program SPSS® IBM. Results: A total of 2154 (n=2154) students were surveyed. The average age of the women was 20.4 ±1.9years. The general prevalence of dysmenorrhea was 78.9%, with psychology students having the highest value (83.7%). The VAS mean pain score was of 64.0. The severity of menstrual pain in students was reported as mild in 9.0%, and moderate-severe in 91.0%. The VAS mean pain scores and intensity of pain of gerontology students were significantly higher than those reported by dentistry and medicine students (P<.05). Limitation of daily activities was reported in 90.4% of women, with medical students reporting the highest percentage (93.3%). Women reported school absenteeism in 37.0%, with medical students presenting the highest percentage (41.4%). The severity of menstrual pain as a risk factor (independent variable) positively influenced various dependent variables involved in students academic performance (P<.05), including: stop doing their activities due to pain in 1 to 6 menstruations a year, minor concentration, absenteeism, low school performance, and lower grades during dysmenorrhea. Conclusion: A high prevalence of dysmenorrhea was observed and it is concluded that the severity of the symptomatology significantly interferes with the academic performance of the participants.(AU)
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Humanos , Masculino , Femenino , Adolescente , Adulto Joven , Rendimiento Académico , Dismenorrea , Estudiantes , Dimensión del Dolor , Absentismo , México , Estudios Transversales , Encuestas y CuestionariosRESUMEN
The components of metabolic syndrome (MetS) and hepatogastrointestinal diseases are widespread worldwide, since many factors associated with lifestyle and diet influence their development and correlation. Due to these growing health problems, it is necessary to search for effective alternatives for prevention or adjuvants in treating them. The positive impact of regulated microbiota on health is known; however, states of dysbiosis are closely related to the development of the conditions mentioned above. Therefore, the role of prebiotics, probiotics, or symbiotic complexes has been extensively evaluated; the results are favorable, showing that they play a crucial role in the regulation of the immune system, the metabolism of carbohydrates and lipids, and the biotransformation of bile acids, as well as the modulation of their central receptors FXR and TGR-5, which also have essential immunomodulatory and metabolic activities. It has also been observed that they can benefit the host by displacing pathogenic species, improving the dysbiosis state in MetS. Current studies have reported that paraprobiotics (dead or inactive probiotics) or postbiotics (metabolites generated by active probiotics) also benefit hepatogastrointestinal health.
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Microbioma Gastrointestinal , Síndrome Metabólico , Probióticos , Disbiosis/complicaciones , Disbiosis/terapia , Humanos , Síndrome Metabólico/complicaciones , Síndrome Metabólico/terapia , Prebióticos , Probióticos/uso terapéuticoRESUMEN
AIM: To determine through a systematic review and meta-analysis the level of knowledge about pain of nursing health professionals based on their scores on the Knowledge and Attitudes Survey Regarding Pain tool and its subdimensions in different settings. BACKGROUND: Adequate pain management is closely related to the degree of knowledge about pain of the healthcare personnel. Therefore, pedagogical programs on pain have been implemented in diverse health setting. However, several studies have found significant deficiencies in the knowledge of pain in health professionals, including nurses. DESIGN: Systematic review and meta-analysis. The study protocol was developed, registered and published in the international prospective register of systematic reviews (PROSPERO). DATA SOURCES: Scopus, PubMed, Embase, Web of Science, Cochrane Library and Google Scholar databases were searched up to June 2021. Studies from 2010 to 2021 were included in the analysis. METHODS: This study was conducted according to the Report Article for Systematic Reviews and Meta-analysis (PRISMA) guidelines and the quality evaluation was realized by the Mix Methods Appraisal Tool (MMAT). A random effects model analyzed the data, due on the heterogeneity among the studies. The I2 index and Cochran's Q test were employed to inspect the heterogeneity between the studies. For the Cochran's Q test, the P-value was set at 0.05. RESULTS: Eighteen studies with 7942 nurses were included in the systematic review and meta-analysis. The percentage of total pain knowledge was 52.9 % (95 % CI: 47.2-58.6). The highest and the lowest knowledge scores were for the spiritual/cultural dimension (69.9 %, 95 % CI: 63.4-76.0) and the intervention dimension (36.8 %, 95 % CI: 28.1-45.9), respectively. The score of total knowledge of the six domains in nurses in the area of oncology (58.6 %, 95 % CI: 45.3-71.2) was higher than that of nurses of the other areas. CONCLUSIONS: The knowledge of the nursing professionals about pain was lower that the suggested level of 80 %. Our study found that the pain knowledge is positively related to the prior pain training. Therefore, there is an urgent need to include continuing educational initiatives to improve the knowledge level about pain management in all the health personnel, including the nursing professionals.
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Competencia Clínica , Enfermeras y Enfermeros , Actitud , Personal de Salud/educación , Humanos , DolorRESUMEN
Pomegranate is a polyphenol-rich fruit. Studies have shown that extracts prepared from its juice or from different parts of the pomegranate plant have various biological activities including antioxidant, antimicrobial, anti-inflammatory, anticarcinogenic, cardioprotective, and antidiabetic. The therapeutic potential has been attributed to various phytochemicals, including ellagic acid, punicic acid, flavonoids, anthocyanidins, anthocyanins, flavonols, and flavones. This review focuses on the scientific evidence of pomegranate juice as hypoglycemic, emphasizing the chemical composition and the possible mechanisms of action associated with this effect. Studies were identified using the PubMed, Scopus, and ISI Web of Science databases to identify relevant articles focused on the hypoglycemic effect of pomegranate juice. The physiological responses to pomegranate juice are reported here, including a decrease of oxidative stress damage, an increase of insulin-dependent glucose uptake, maintenance of ß-cell integrity, inhibition of nonenzymatic protein glycation, an increase of insulin sensitivity, modulation of peroxisome proliferator-activated receptor-gamma, inhibition of α-amylase, inhibition of α-glucosidase and dipeptidyl peptidase-4, and decreases in inflammation. Overall, we found a significant hypoglycemic effect of pomegranate in in vitro and in vivo studies and we summarize the potential mechanisms of action.
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The objective of the present study was to scrutinize the effect of nitric oxide (NO), cyclic GMP (cGMP), potassium channel blockers, and metformin on the citral-produced peripheral antinociception. The rat paw 1% formalin test was used to assess nociception and antinociception. Rats were treated with local peripheral administration of citral (10-100 µg/paw). The antinociception of citral (100 µg/paw) was evaluated with and without the local pretreatment of naloxone, NG-L-nitro-arginine methyl ester (L-NAME, a NO synthesis inhibitor), 1H-(1,2,4)-oxadiazolo(4,2-a)quinoxalin-1-one (ODQ, a soluble guanylyl cyclase inhibitor), metformin, opioid receptors antagonists, and K+ channel blockers. Injection of citral in the rat paw significantly decreased the nociceptive effect of formalin administration during the two phases of the test. Local pretreatment of the paws with L-NAME and ODQ did not reduced the citral-induced antinociception. Glipizide or glibenclamide (Kir6.1-2; ATP-sensitive K+ channel blockers), tetraethylammonium or 4-aminopyridine (KV; voltage-gated K+ channel blockers), charybdotoxin (KCa1.1; big conductance calcium-activated K+ channel blocker), apamin (KCa2.1-3; small conductance Ca2+-activated K+ channel antagonist), or metformin, but not the opioid antagonists, reduced the antinociception of citral. Citral produced peripheral antinociception during both phases of the formalin test. These effects were due to the activation of K+ channels and a biguanide-dependent mechanism.
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GMP Cíclico , Metformina , Monoterpenos Acíclicos , Analgésicos/farmacología , Analgésicos/uso terapéutico , Animales , GMP Cíclico/metabolismo , Metformina/farmacología , Óxido Nítrico/metabolismo , Nocicepción , Dimensión del Dolor , Bloqueadores de los Canales de Potasio/farmacología , Ratas , Ratas Wistar , Receptores Opioides/metabolismoRESUMEN
Cereals have phytochemical compounds that can diminish the incidence of chronic diseases such as hypertension. The angiotensin-converting enzyme 2 (ACE2) participates in the modulation of blood pressure and is the principal receptor of the virus SARS-CoV-2. The inhibitors of the angiotensin-converting enzyme (ACE) and the block receptors of angiotensin II regulate the expression of ACE2; thus, they could be useful in the treatment of patients infected with SARS-CoV-2. The inferior peptides from 1 to 3 kDa and the hydrophobic amino acids are the best candidates to inhibit ACE, and these compounds are present in rice, corn, wheat, oats, sorghum, and barley. In addition, the vitamins C and E, phenolic acids, and flavonoids present in cereals show a reduction in the oxidative stress involved in the pathogenesis of hypertension. The influence of ACE on hypertension and COVID-19 has turned into a primary point of control and treatment from the nutritional perspective. The objective of this work was to describe the inhibitory effect of the angiotensin-converting enzyme that the bioactive compounds present in cereals possess in order to lower blood pressure and how their consumption could be associated with reducing the virulence of COVID-19.
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The aim of this study was to examine if the peripheral antinociception of α-bisabolol involves the participation of nitric oxide (NO) and cyclic guanosine monophosphate (cGMP) synthesis followed by K+ channel opening in the formalin test. Wistar rats were injected in the dorsal surface of the right hind paw with formalin (1%). Rats received a subcutaneous injection into the dorsal surface of the paw of vehicles or increasing doses of α-bisabolol (100-300 µg/paw). To determine whether the peripheral antinociception induced by α-bisabolol was mediated by either the opioid receptors or the NO-cGMP-K+ channels pathway, the effect of pretreatment (10 min before formalin injection) with the appropriate vehicles, naloxone, naltrexone, NG-nitro-l-arginine methyl ester (L-NAME), 1H-[1,2,4]-oxadiazolo[4,2-a]quinoxalin-1-one (ODQ), glibenclamide, glipizide, apamin, charybdotoxin, tetraethylammonium, or 4-aminopyridine on the antinociceptive effects induced by local peripheral α-bisabolol (300 µg/paw) were assessed. α-Bisabolol produced antinociception during both phases of the formalin test. α-Bisabolol antinociception was blocked by L-NAME, ODQ, and all the K+ channels blockers. The peripheral antinociceptive effect produced by α-bisabolol was not blocked by the opioid receptor inhibitors. α-Bisabolol was able to active the NO-cGMP-K+ channels pathway to produce its antinoceptive effect. The participation of opioid receptors in the peripheral local antinociception induced by α-bisabolol is excluded.
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Analgésicos/farmacología , GMP Cíclico/metabolismo , Sesquiterpenos Monocíclicos/farmacología , Óxido Nítrico/metabolismo , Nocicepción/efectos de los fármacos , Canales de Potasio/metabolismo , Receptores Opioides/metabolismo , Animales , Masculino , Bloqueadores de los Canales de Potasio/farmacología , Canales de Potasio/química , Canales de Potasio/genética , Ratas , Ratas Wistar , Receptores Opioides/química , Receptores Opioides/genéticaRESUMEN
Despite the wide application of carvacrol (CAR) in different biological and medical areas, there is still insufficient electrophysiological data on the mechanisms of action of CAR, particularly in the pregnant uterine function. The aim of this study was to evaluate the in vitro tocolytic effect of CAR on the contractility of isolated pregnant rat uterus in the presence of a calcium channel antagonist (nifedipine) and a cyclooxygenase inhibitor (indomethacin). The uteri were isolated from pregnant Wistar rats at 16-18 days of pregnancy and suspended in an isolated organ bath chamber containing a Ringer's physiological solution and aerated with 95% O2and 5% CO2. Samples were used in functional tests to evaluate the inhibitory effect of CAR at increasing concentrations on the rhythmic spontaneous, oxytocin-induced phasic, K+-induced tonic, and Ca2+-induced contractions. The differences in inhibitory concentration-50 and Emaxamong the compounds were determined using the one-way ANOVA followed by a post hoc Student-Newman-Keuls or Bonferroni test, in all casesP < 0.05 was considered statistically significant. Nifedipine was used as positive controls where required. CAR caused a significant concentration-dependent inhibition of the uterine contractions induced by the pharmaco- and electro-mechanic stimuli. We showed that the inhibitory effects of CAR depends on the type of muscle contraction stimuli, and that it acts stronger in spontaneous rhythmic activity and in contractions of isolated rat uterus induced by Ca2+. Nifedipine was more potent than CAR and indomethacin on the uterine contractility (P < 0.05), but none of them was more effective than nifedipine. Therefore, the tocolytic effect induced by CAR was associated with the blockade of the calcium channels in the pregnant rat uterus. This property placed CAR as a potentially safe and effective adjuvant agent in cases of preterm labor, an area of pharmacological treatment that requires urgent improvement.
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Cimenos/farmacología , Contracción Muscular/efectos de los fármacos , Tocolíticos , Útero/efectos de los fármacos , Animales , Femenino , Fenoles , Embarazo , Ratas , Ratas Wistar , Tocolíticos/farmacologíaRESUMEN
The aim of this study was to examine if the peripheral antinociceptive effects of the opioid agonist/antagonist nalbuphine and buprenorphine involve the sequential participation of nitric oxide (NO) and cyclic guanosine monophosphate (cGMP) synthesis followed by K+ channel opening in the formalin test. Wistar rats (180-220 g) were injected in the dorsal surface of the right hind paw with formalin (1%). Rats received a subcutaneous (s.c.) injection into the dorsal surface of the paw of vehicles or increasing doses of nalbuphine (50-200 µg/paw) or buprenorphine (1-5 µg/paw) 20 min before formalin injection into the paw. Nalbuphine antinociception was reversed by the s.c. injection into the paw of the inhibitor of NO synthesis (NG-nitro-l-arginine methyl ester (L-NAME)), by the inhibitor of guanylyl cyclase (1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one (ODQ)), by the Kir6.1-2, ATP-sensitive K+ channel inhibitors (glibenclamide and glipizide), by the KCa2.1-3, small conductance Ca2+-activated K+ channel blocker (apamin), by the KCa1.1, large conductance Ca2+-activated K+ channel blocker (charybdotoxin), and by the KV, voltage-dependent K+ channel inhibitors (4-aminopyridine (4-AP) and tetraethylammonium chloride (TEA)). The antinociceptive effect produced by buprenorphine was blocked by the s.c. injection of 4-AP and TEA but not by L-NAME, ODQ, glibenclamide, glipizide, apamin, or charybdotoxin. The present results provide evidence for differences in peripheral mechanisms of action between these opioid drugs.
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Analgésicos Opioides/farmacología , Antagonistas de Narcóticos/farmacología , Nocicepción/efectos de los fármacos , Dolor/tratamiento farmacológico , Transducción de Señal/efectos de los fármacos , Animales , Buprenorfina/farmacología , GMP Cíclico/metabolismo , Modelos Animales de Enfermedad , Gliburida/administración & dosificación , Humanos , Inyecciones Subcutáneas , Canales KATP/antagonistas & inhibidores , Canales KATP/metabolismo , Masculino , NG-Nitroarginina Metil Éster/administración & dosificación , Nalbufina/farmacología , Óxido Nítrico/metabolismo , Nocicepción/fisiología , Dolor/inducido químicamente , Dolor/diagnóstico , Dimensión del Dolor , Bloqueadores de los Canales de Potasio/administración & dosificación , Ratas , Receptores Opioides/metabolismo , Transducción de Señal/fisiologíaRESUMEN
Background and Objectives: Prostate cancer is the second most harmful disease in men worldwide and the number of cases is increasing. Therefore, new natural agents with anticancer potential should be examined and the response of existing therapeutic drugs must be enhanced. Stevia pilosa and Stevia eupatoria are two species that have been widely used in traditional medicine, but their effectiveness on cancer cells and their interaction with antineoplastic drugs have not been studied. The aim of this study was to evaluate the anticancer activity of Stevia pilosa methanolic root extract (SPME) and Stevia eupatoria methanolic root extract (SEME) and their effect, combined with enzalutamide, on prostate cancer cells. Materials and Methods: The study was conducted on a human fibroblast cell line, and on androgen-dependent (LNCaP) and androgen-independent (PC-3) prostate cancer cell lines. The cell viability was evaluated using a Trypan Blue exclusion test for 48 h, and the migration by a wound-healing assay for 24, 48, and 72 h. Results: The results indicate that SPME and SEME were not cytotoxic at concentrations less than 1000 µg/mL in the human fibroblasts. SPME and SEME significantly reduced the viability and migration of prostate cancer cells in all concentrations evaluated. The antiproliferative effect of the Stevia extracts was higher in cancer cells than in normal cells. The enzalutamide decreased the cell viability in all concentrations tested (10-50 µM). The combination of the Stevia extracts and enzalutamide produced a greater effect on the inhibition of the proliferation and migration of cancer cells than the Stevia extracts alone, but not of the enzalutamide alone. Conclusion: The results indicate that SPME and SEME have an inhibitory effect on the viability and migration of prostate cancer cells and do not interfere with the enzalutamide anticancer effect. The data suggest that Stevia extracts may be a potential source of molecules for cancer treatment.
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Neoplasias de la Próstata/prevención & control , Factores Protectores , Stevia , Proliferación Celular/efectos de los fármacos , Humanos , Masculino , Células PC-3/efectos de los fármacos , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Neoplasias de la Próstata/tratamiento farmacológico , Cicatrización de Heridas/efectos de los fármacosRESUMEN
The liver is considered the laboratory of the human body because of its many metabolic processes. It accomplishes diverse activities as a mixed gland and is in continuous cross-talk with the endocrine system. Not only do hormones from the gastrointestinal tract that participate in digestion regulate the liver functions, but the sex hormones also exert a strong influence on this sexually dimorphic organ, via their receptors expressed in liver, in both health and disease. Besides, the liver modifies the actions of sex hormones through their metabolism and transport proteins. Given the anatomical position and physiological importance of liver, this organ is evidenced as an immune vigilante that mediates the systemic immune response, and, in turn, the immune system regulates the hepatic functions. Such feedback is performed by cytokines. Pro-inflammatory and anti-inflammatory cytokines are strongly involved in hepatic homeostasis and in pathological states; indeed, female sex hormones, oral contraceptives, and phytoestrogens have immunomodulatory effects in the liver and the whole organism. To analyze the complex and interesting beneficial or deleterious effects of these drugs by their immunomodulatory actions in the liver can provide the basis for either their pharmacological use in therapeutic treatments or to avoid their intake in some diseases.
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Anticonceptivos Orales/metabolismo , Hormonas/metabolismo , Inmunomodulación , Hígado/inmunología , Hígado/metabolismo , Fitoestrógenos/metabolismo , Anticonceptivos Orales/farmacología , Femenino , Hormonas/farmacología , Humanos , Sistema Inmunológico/efectos de los fármacos , Sistema Inmunológico/inmunología , Sistema Inmunológico/metabolismo , Inmunomodulación/efectos de los fármacos , Hígado/efectos de los fármacos , Estructura Molecular , Fitoestrógenos/farmacología , Factores SexualesRESUMEN
Chia seeds (Salvia hispanica L.) are rich in omega fatty acids. Dyslipidemia and steatohepatitis are diseases that require effective treatments in obese and non-obese patients. The aim was to evaluate the effect of chia intake on acute tyloxapol (TI)-induced dyslipidemia, on acute carbon tetrachloride (TC)-induced steatohepatitis, and on mixed damage (TC+TI) in non-obese rats. Four experimental groups were fed for 4 weeks a diet with established rodent food (DE), and four groups were fed a diet with 15% added chia (DC). Plasma samples were analyzed for total cholesterol, triglycerides, glucose, biochemical liver damage markers, and tumor necrosis factor-α (TNF-α). Liver samples were used to quantify glycogen, catalase, lipid peroxidation, and TNF-α. A histopathological analysis was performed. DC intake partially or totally prevented steatohepatitis, and reduced lipids in the dyslipidemic groups. The hypolipidemic and hepatoprotective effects of chia may be correlated to its high content of α-linolenic acid (omega-3) and phenolics. PRACTICAL APPLICATIONS: Metabolic syndrome is associated with non-alcoholic fatty liver disease (NAFLD) and non-alcoholic steatohepatitis (NASH), which are currently the most common causes of chronic liver disease, cirrhosis, and hepatocellular carcinoma (HCC) worldwide. Dyslipidemia is a significant risk factor for NAFLD and NASH. Non-obese patients may have NAFLD or NASH. Metabolic syndrome and dyslipidemia are more strongly associated with NAFLD in non-obese than in obese patients. This is the first study evaluating the hypolipidemic and hepatoprotective effects of chia seed intake on acute dyslipidemia and/or steatohepatitis caused by the individual or combined administration of the inducers tyloxapol and carbon tetrachloride, respectively, in non-obese rats. The pharmacological effects of dietary chia are correlated to its high content of omega-3 and omega-6 (1:1), protein, dietary fiber, and phenolics. The results suggest that inclusion of chia in diets of non-obese patients with dyslipidemia and/or NAFLD/NASH may improve their health state and preventing cirrhosis or HCC.
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Dislipidemias/tratamiento farmacológico , Hígado Graso/tratamiento farmacológico , Salvia/química , Semillas/química , Alimentación Animal/análisis , Animales , Dieta/veterinaria , Masculino , Ratas , Ratas WistarRESUMEN
ß-Sitosteryl (S)-ibuprofenate (2), stigmasteryl (S)-ibuprofenate (3), ergosteryl (S)-ibuprofenate (4), and cholesteryl (S)-ibuprofenate (5) were prepared in 70-75% yields by Steglich esterification and were characterized by 1D and 2D NMR, as well as by MS. The new esters were evaluated in in vivo pain models of antinociception and anti-inflammation using the writhing, formalin, and carrageenan tests, in mice and rats, and the results were compared with those of (S)-ibuprofen (1). Damage to the gastric mucosa of animals was also assessed. The results indicated that 2-5 have comparable or eventually better activity than 1 at the same mg/kg doses. Since the molecular weight ratio of esters 2-5 to ibuprofen is about 3-1, the amount of truly incorporated ibuprofen was roughly one third to achieve similar effects. This resulted in minimal gastrointestinal damage in the stomach of the animals, in contrast to the large gastric injury caused by (S)-ibuprofen.