RESUMEN
OBJECTIVES: Medicinal herbs are plants with potential medicinal and health benefits. In recent years, they are being increasingly used as a treatment alternative owing to their effectiveness against various diseases. In this study, we investigated the inhibitory effects of 15 medicinal herbs on causative bacteria for dental caries and periodontal disease. METHODS: This study evaluated the effects of the extracts of 15 medicinal herbs on growth and biofilm formation in five oral pathogenic bacterial strains. The herbs were processed into extracts, and bacterial strains were cultured. Then, bacterial growth and biofilm formation were assessed using various methods. Finally, the extract of the herb Hibiscus sabdariffa (hibiscus) was analyzed using high-performance liquid chromatography. RESULTS: Incubation of bacteria with the herbal extracts showed that hibiscus exerted a significant inhibitory effect on all the oral pathogenic bacterial strains evaluated in this study. In addition, the pigment delphinidin-3-sambubioside, which is found in hibiscus extract, was identified as a particularly important inhibitory component. CONCLUSIONS: These results lay the ground work for the potential development of novel therapeutic or preventive agents against dental caries and periodontal disease, two major oral diseases.
Asunto(s)
Caries Dental , Hibiscus , Enfermedades Periodontales , Plantas Medicinales , Humanos , Extractos Vegetales/farmacología , Extractos Vegetales/análisis , Extractos Vegetales/química , Hibiscus/química , Caries Dental/tratamiento farmacológico , Caries Dental/prevención & control , Bacterias , Enfermedades Periodontales/tratamiento farmacológico , Enfermedades Periodontales/prevención & controlRESUMEN
BACKGROUND: Evidence on efficacy of high-dose ceftriaxone monotherapy for extragenital Neisseria gonorrhoeae (NG) infection is lacking. METHODS: A cohort of men who have sex with men (MSM) were tested for NG/Chlamydia trachomatis (CT) every 3 months, in a single-center observational study in Tokyo, Japan. MSM agedâ >â 19 years diagnosed with extragenital NG infection between 2017 and 2020 were included. A single dose of 1 g ceftriaxone monotherapy was provided, while dual therapy with a single oral dose of 1 g azithromycin or 100 mg doxycycline administered orally twice daily for 7 days were given, for those coinfected with CT, according to infected sites. Efficacy of these treatments was calculated by the number of NG-negative subjects at test-of-cure divided by the number of subjects treated. Fisher exact tests were used to compare the efficacy between the 2 groups. RESULTS: Of 320 cases diagnosed with extragenital NG, 208 were treated with monotherapy and 112 were treated with dual therapy. The efficacy against total, pharyngeal, and rectal infections was 98.1% (204/208, 95% confidence interval [CI]: 95.2-99.3%), 97.8% (135/138, 95% CI: 93.8-99.4%), and 98.6% (69/70, 95% CI: 92.3-99.9%), respectively, in the monotherapy group, whereas the corresponding efficacy in the dual therapy was 95.5% (107/112, 95% CI: 90.0-98.1%), 96.1% (49/51, 95% CI: 86.8-99.3%), and 95.1% (58/61, 95% CI: 86.5-98.7%), respectively. No significant difference in the corresponding efficacy was observed between the two groups (Pâ =â .29, Pâ =â .61, Pâ =â .34, respectively). CONCLUSIONS: High-dose ceftriaxone monotherapy is as effective as dual therapy for extragenital NG among MSM.
Asunto(s)
Infecciones por Chlamydia , Gonorrea , Minorías Sexuales y de Género , Azitromicina/uso terapéutico , Ceftriaxona/uso terapéutico , Infecciones por Chlamydia/tratamiento farmacológico , Chlamydia trachomatis , Doxiciclina/uso terapéutico , Gonorrea/tratamiento farmacológico , Gonorrea/epidemiología , Homosexualidad Masculina , Humanos , Masculino , Neisseria gonorrhoeaeRESUMEN
We previously identified 2-tert-butyl-4-[(3-methoxypropyl)amino]-N-(2-methylpropyl)-N-[(3S,5R)-5-(morpholin-4-ylcarbonyl)piperidin-3-yl]pyrimidine-5-carboxamide 3 as a potent renin inhibitor. Since 3 showed unacceptably low bioavailability (BA) in rats, structural modification, using SBDD and focused on physicochemical properties was conducted to improve its PK profile while maintaining renin inhibitory activity. Conversion of the amino group attached at the 4-position of pyrimidine to methylene group improved PK profile and decreased renin inhibitory activity. New central cores with carbon side chains were explored to improve potency. We had designed a series of 5-membered azoles and fused heterocycles that interacted with the lipophilic S3 pocket. In the course of modification, renin inhibitory activity was enhanced by the formation of an additional hydrogen bonding with the hydroxyl group of Thr77. Consequently, a series of novel benzimidazole derivatives were discovered as potent and orally bioavailable renin inhibitors. Among those, compound 13 exhibited more than five-fold of plasma renin inhibition than aliskiren in cynomolgus monkeys at dose ratio.
Asunto(s)
Bencimidazoles/química , Piperidinas/química , Inhibidores de Proteasas/síntesis química , Renina/antagonistas & inhibidores , Administración Oral , Animales , Bencimidazoles/metabolismo , Bencimidazoles/farmacocinética , Sitios de Unión , Disponibilidad Biológica , Cristalografía por Rayos X , Diseño de Fármacos , Evaluación Preclínica de Medicamentos , Semivida , Humanos , Enlace de Hidrógeno , Simulación de Dinámica Molecular , Piperidinas/metabolismo , Piperidinas/farmacocinética , Inhibidores de Proteasas/metabolismo , Inhibidores de Proteasas/farmacocinética , Estructura Terciaria de Proteína , Ratas , Renina/metabolismo , Relación Estructura-ActividadRESUMEN
PURPOSE: The purpose of this study was to determine the content of sucrose, glucose, total sugar, and pH in a range of popular contemporary Japanese soft drinks and compare their changes in different periods. METHODS: The pH value and content of sucrose and glucose of popular Japanese soft drinks were determined, and this study's results were compared with the previous data of beverages in 1978, 1981, 1985, and 1997. RESULTS: Coffee drinks showed the highest content of sucrose, while carbonated diet drinks showed the lowest. Energy drinks showed the highest content of glucose and total sugar, while carbonated diet drinks showed the lowest. Coffee and energy drinks showed the highest and lowest pH levels, respectively. The total sugar content of a soft drink has remained unchanged over the years, but the sucrose content of soft drinks has decreased over the years. CONCLUSIONS: All drinks showed pH values below 7, with a very wide variety of sugar content; sugar content of soft drinks has generally decreased since the 1980s in Japan.
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Bebidas/análisis , Carbohidratos/análisis , Bebidas Gaseosas/análisis , Café/química , Frutas/química , Glucosa/análisis , Concentración de Iones de Hidrógeno , Japón , Sacarosa/análisis , Té/químicaRESUMEN
BACKGROUND: Saireito consists of components of shosaikoto and goreisan. There are several reports of liver injury caused by shosaikoto and saireito, whereas cases caused by goreisan are rarely seen. PATIENT: A 70-year-old woman suffered from sicca of the eyes and oral cavity that arose in 2003. In June 2004, we diagnosed her as having Sjögren syndrome on the basis of Schirmer's test, salivary scintigraphy, presence of anti-SS-A/Ro antibody, and subjective symptoms. Although a muscarinic agonist was commenced, her sicca symptoms did not improve. INTERVENTIONS: In February 2008, 7.5 g/day of shosaikoto extract granules (for ethical use, Tsumura & Co., Tokyo, Japan) was introduced. Her symptoms and laboratory data did not change. The next month, the treatment was replaced by 9.0 g/day of saireito extract granules (for ethical use, Tsumura & Co., Tokyo, Japan). RESULTS: After 10 weeks, elevation of liver enzymes was observed. On suspicion of drug-induced liver injury (DILI), saireito was withdrawn, and the patient's liver enzymes returned to normal the next month. Drug-induced lymphocyte stimulation tests (DLSTs) for saireito, shosaikoto, and goreisan were all positive. CONCLUSIONS: The clinical course suggested allergy to the goreisan component of saireito. It is important to be aware of the limitation of DLST as a diagnostic tool for DILI, especially for herbal medicines.
Asunto(s)
Enfermedad Hepática Inducida por Sustancias y Drogas/etiología , Hipersensibilidad a las Drogas/complicaciones , Medicamentos Herbarios Chinos/efectos adversos , Hígado/efectos de los fármacos , Fitoterapia/efectos adversos , Síndrome de Sjögren/tratamiento farmacológico , Anciano , Femenino , Humanos , Hígado/enzimología , Hígado/inmunología , Activación de Linfocitos , Síndrome de Sjögren/inmunologíaRESUMEN
We performed correction for bowing deformity of the lower extremities due to vitamin D-resistant hypophosphatemic rickets of three adults, six segments. The operative method was gradual correction and lengthening using distraction osteogenesis by Ilizarov external fixator or Heidelberg external fixator. The orders of the corrections were simultaneous correction of the bilateral femur for one patient, simultaneous correction of the ipsilateral leg for one patient, and diagonal correction of the bilateral leg for one patient. The mean correction angle was 30.5 degrees. The mean external fixation period was 146 days. Each orders of the corrections had its merits and demerits. All patients obtained a physiological alignment and good bone formation by taking Vitamin D and oral phosphate supplements even an adult patient. All the patients had articular pain, such as hip, knee, and ankle, however, these pains healed up. All the patients were satisfied with the outcomes at the time of the final follow-up interview in terms of their cosmetic improvement. Distraction osteogenesis for bowing deformity of the lower extremities due to vitamin D-resistant hypophosphatemic rickets was very effective method and could be applied to adult patients. However, the order of the corrections should be considered carefully depending on each patient.