RESUMO
The aim of the present work was to evaluate the effects of Thalassia testudinum hydroethanolic extract, its polyphenolic fraction and thalassiolin B on the activity of phase I metabolizing enzymes as well as their antimutagenic effects. Spectrofluorometric techniques were used to evaluate the effect of tested products on rat and human CYP1A and CYP2B activity. The antimutagenic effect of tested products was evaluated in benzo[a]pyrene (BP)-induced mutagenicity assay by an Ames test. Finally, the antimutagenic effect of Thalassia testudinum (100 mg/kg) was assessed in BP-induced mutagenesis in mice. The tested products significantly (p < 0.05) inhibit rat CYP1A1 activity, acting as mixed-type inhibitors of rat CYP1A1 (Ki = 54.16 ± 9.09 µg/mL, 5.96 ± 1.55 µg/mL and 3.05 ± 0.89 µg/mL, respectively). Inhibition of human CYP1A1 was also observed (Ki = 197.1 ± 63.40 µg/mL and 203.10 ± 17.29 µg/mL for the polyphenolic fraction and for thalassiolin B, respectively). In addition, the evaluated products significantly inhibit (p < 0.05) BP-induced mutagenicity in vitro. Furthermore, oral doses of Thalassia testudinum (100 mg/kg) significantly reduced (p < 0.05) the BP-induced micronuclei and oxidative damage, together with an increase of reduced glutathione, in mice. In summary, Thalassia testudinum metabolites exhibit antigenotoxic activity mediated, at least, by the inhibition of CYP1A1-mediated BP biotransformation, arresting the oxidative and mutagenic damage. Thus, the metabolites of T. testudinum may represent a potential source of chemopreventive compounds for the adjuvant therapy of cancer.
Assuntos
Antimutagênicos/farmacologia , Benzo(a)pireno/toxicidade , Citocromo P-450 CYP1A1/antagonistas & inibidores , Inibidores das Enzimas do Citocromo P-450/farmacologia , Flavonoides/farmacologia , Hydrocharitaceae/metabolismo , Polifenóis/farmacologia , Salmonella typhi/efeitos dos fármacos , Ativação Metabólica , Animais , Antimutagênicos/isolamento & purificação , Benzo(a)pireno/metabolismo , Citocromo P-450 CYP1A1/metabolismo , Citocromo P-450 CYP1A2/metabolismo , Inibidores do Citocromo P-450 CYP1A2/isolamento & purificação , Inibidores do Citocromo P-450 CYP1A2/farmacologia , Inibidores das Enzimas do Citocromo P-450/isolamento & purificação , Dano ao DNA/efeitos dos fármacos , Flavonoides/isolamento & purificação , Humanos , Isoenzimas , Cinética , Micronúcleos com Defeito Cromossômico/induzido quimicamente , Testes para Micronúcleos , Estresse Oxidativo/efeitos dos fármacos , Polifenóis/isolamento & purificação , Ratos , Salmonella typhi/genéticaRESUMO
BACKGROUND: Effective postoperative pain management is a crucial component of recovery following surgery. Narcotics are a cornerstone of postoperative analgesia, but can require a redosing requirement, encompass a lengthy list of side effects and adverse reaction risks, as well as carry a dependency potential. The national focus on decreasing opioid use has directly impacted postoperative pain management. Previous studies have reported the beneficial use of a single intraoperative injection of extended-release liposomal bupivacaine in postoperative pain management, however the same results have not been extensively studied in the urogynecology literature. OBJECTIVE: We sought to evaluate cumulative postoperative vaginal pain on days 1 and 3 after posterior vaginal wall surgery comparing study medication (extended-release liposomal bupivacaine) to placebo (saline). Secondary aims were to evaluate vaginal pain on postoperative day 7 and total morphine-equivalent narcotic usage on days 1, 3, and 7. STUDY DESIGN: This is a randomized, double-blinded, placebo-controlled trial with 100 subjects recruited from Walter Reed National Military Medical Center urogynecology clinic. All subjects were age >18 years and scheduled for surgery involving the posterior vaginal wall or muscularis (including posterior colporrhaphy, colpocleisis, sphincteroplasty, perineorrhaphy), excluding those with regular narcotic usage or concurrent pain management requiring the use of epidural anesthesia. A sample size of 96 patients was calculated. Subjects were randomized to receive either 20 mL of extended-release liposomal bupivacaine (Exparel) (Pacira Pharmaceuticals Inc, Parsippany, NJ) or 20 mL of placebo (saline) at the end of surgery. Concealed syringes were used and injected immediately postoperative into the lateral vaginal wall/levator muscle area and perineal body. In-house morphine-equivalent narcotic usage was recorded along with the postoperative day 1 pain scores. Patients were contacted by telephone on postoperative days 3 and 7. Vaginal pain scores were evaluated using the Defense and Veterans Pain Rating Scale, cumulatively and on days 1, 3, and 7. Overall morphine-equivalent narcotics were compared between the 2 groups. RESULTS: From October 2014 through August 2017, 100 patients were enrolled and completed the study; 49 (49%) of the patients were randomized to the study group and 51 (51%) were in the placebo group. There was no significant difference between vaginal pain scores between the study group and the placebo group (postoperative day 1: study medication median score 1 [interquartile range 0-3], placebo median score 1 [interquartile range 0-3] [P = .59]; postoperative day 3: study medication median score 2 [interquartile range 0-3], placebo median score 1 [interquartile range 0-3] [P = .20]; postoperative day 7: study medication median score 3 [interquartile range 1-4], placebo median score 1.5 [interquartile range 0-3] [P = .06]). Cumulative pain scores postoperative day 1-7 were also not significant (study medication median score 6 [interquartile range 1-10], placebo median score 4 [interquartile range 1-8] [P = .14]). Multivariate model for the presence of vaginal pain was calculated and after controlling for body mass index, age, and combined laparoscopy surgery, there was no significant difference between the study and the placebo groups (P = .62). There was no statistically significant difference in morphine equivalents for the 2 groups: study medication 112.5 (interquartile range 45-207) and placebo 101.5 (interquartile range 37.5-195), P = .81. CONCLUSION: The use of extended-release liposomal bupivacaine in posterior vaginal wall surgeries, injected into the lateral posterior vaginal wall and perineal body, does not provide a significant decrease in postoperative pain or decrease narcotic medication usage when compared to saline.
Assuntos
Anestésicos Locais/administração & dosagem , Bupivacaína/administração & dosagem , Lipossomos/administração & dosagem , Dor Pós-Operatória/tratamento farmacológico , Vagina/cirurgia , Adulto , Preparações de Ação Retardada/administração & dosagem , Método Duplo-Cego , Feminino , Procedimentos Cirúrgicos em Ginecologia/efeitos adversos , Procedimentos Cirúrgicos em Ginecologia/métodos , Humanos , Pessoa de Meia-Idade , Derivados da Morfina/administração & dosagem , Derivados da Morfina/uso terapêutico , Oxicodona , Manejo da Dor/métodos , Medição da Dor , Placebos , Fatores de Tempo , Vagina/efeitos dos fármacosRESUMO
This study focused on isolating, identifying, and evaluating the trypanocidal potential against the hemoflagellate protozoan Trypanosoma cruzi of compounds from Parthenium incanum (Mariola), a plant used in traditional Mexican medicine to treat stomach and liver disorders. P. incanum has a wide distribution in Mexico. This study found that methanolic extracts of P. incanum, obtained by static maceration and successive reflux, had promising results. The fractions were compared using thin-layer chromatography (TLC) and those that showed similarities were mixed. A bioguided assay was performed with Staphylococcus aureus ATCC 25923, using agar diffusion and bioautography techniques to determine the preliminary biological activity. The fractions with antimicrobial activity were purified using a preparative thin-layer chromatography (PTLC) plate, obtaining the bioactive bandages that were subjected to a trypanocidal evaluation against the Ninoa strain of T. cruzi in its epimastigote stage. This revealed an IC50 of up to 45 ± 2.5 µg/mL, in contrast to the values obtained from the crude extracts of less than 100 µg/mL. The TLC, Fourier-transform infrared spectroscopy (FT-IR), and high-performance liquid chromatography coupled with mass spectrometry (HPLC-MS) techniques were used to identify the compounds, demonstrating the presence of sesquiterpene lactones, parthenin, and coronopolin. We concluded that these compounds have the potential to inhibit T. cruzi growth.
RESUMO
This research is aimed to search for suitable probiotic plus prebiotic combinations for food applications. Sixteen bacteria were tested for resistance to low pH, bile salts and antibiotics, and their adhesion to Caco-2 cells, in order to select potential probiotics. Then, two bacteria were selected to study short chain fatty acids production in a starch-based soluble corn fiber or inulin media. Lactiplantibacillus plantarum V3 and L. acidophilus La3 manifested the best probiotic features with a remarkable adhesion ability (23.9% and 17.3%, respectively). Structural differences between fibers have an impact on how each one is metabolized, both in their capacity of being easily fermented and in the short chain fatty acids profile obtained: L. acidophilus La3 in inulin fermentation yielded the highest total short chain fatty acids (85.7 mMol/L), and, in starch-based soluble corn fiber fermentation, yielded the highest butyric acid content (0.31 mMol/L). This study provides valuable information for future design of synbiotics for food applications.
RESUMO
Entamoeba histolytica is an intestinal parasite that causes dysentery and amebic liver abscess. E. histolytica has the capability to invade host tissue by union of virulence factor Gal/GalNAc lectin; this molecule induces an adherence-inhibitory antibody response as well as to protect against amebic liver abscess (ALA). The present work showed the effect of the immunization with PEΔIII-LC3-KDEL3 recombinant protein. In vitro, this candidate vaccine inhibited adherence of E. histolytica trophozoites to HepG2 cell monolayer, avoiding the cytolysis, and in a hamster model, we observed a vaccine-induced protection against the damage to tissue liver and the inhibition of uncontrolled inflammation. PEΔIII-LC3-KDEL3 reduced the expression of TNF-α, IL-1ß, and NF-κB in all immunized groups at 4- and 7-day postinfection. The levels of IL-10, FOXP3, and IFN-γ were elevated at 7 days. The immunohistochemistry assay confirmed this result, revealing an elevated quantity of +IFN-γ cells in the liver tissue. ALA formation in hamsters immunized was minimal, and few trophozoites were identified. Hence, immunization with PEΔIII-LC3-KDEL3 herein prevented invasive amebiasis, avoided an acute proinflammatory response, and activated a protective response within a short time. Finally, this recombinant protein induced an increase of serum IgG.
Assuntos
Entamoeba histolytica/imunologia , Abscesso Hepático Amebiano/prevenção & controle , Proteínas de Protozoários/administração & dosagem , Vacinas Protozoárias/administração & dosagem , Proteínas Recombinantes de Fusão/administração & dosagem , Animais , Anticorpos Antiprotozoários/sangue , Modelos Animais de Doenças , Entamoeba histolytica/genética , Humanos , Imunogenicidade da Vacina , Lectinas/genética , Lectinas/imunologia , Fígado/imunologia , Fígado/parasitologia , Fígado/patologia , Abscesso Hepático Amebiano/sangue , Abscesso Hepático Amebiano/parasitologia , Abscesso Hepático Amebiano/patologia , Masculino , Mesocricetus , Proteínas de Protozoários/genética , Proteínas de Protozoários/imunologia , Vacinas Protozoárias/genética , Vacinas Protozoárias/imunologia , Proteínas Recombinantes de Fusão/genética , Proteínas Recombinantes de Fusão/imunologia , Vacinas Sintéticas/administração & dosagem , Vacinas Sintéticas/genética , Vacinas Sintéticas/imunologiaRESUMO
PURPOSE: We examined ethnic differences in female pelvic disorders in an equal access health care system. MATERIALS AND METHODS: An electronic medical record review was performed for patients with pelvic floor disorders at a military female pelvic medicine and reconstructive surgery division for a 1-year period. Primary diagnosis codes and patient reported race were reviewed. RESULTS: Mean +/- SD cohort age was 55 +/- 16.3 years. A total of 720 patients were identified, of whom 68.8% were white and 18.6% were black. Pelvic organ prolapse was the primary diagnosis in 34.2% of the women, while 19.7% had stress urinary incontinence and 10.8% had urge urinary incontinence. There was no difference in the prevalence of prolapse between black and white women. However, of patients with incontinence there was a statistically significant difference with urge incontinence in more black women (51.2%) and stress incontinence in more white women (66.2%) (chi-square p <0.05). CONCLUSIONS: There is a similar ethnic distribution of pelvic organ prolapse in an equal access health care system. Of women with incontinence there was a higher prevalence of urge urinary incontinence in black women and a higher prevalence of stress urinary incontinence in white women.
Assuntos
Asiático , Negro ou Afro-Americano , Atenção à Saúde , Doenças dos Genitais Femininos/epidemiologia , Hispânico ou Latino , Diafragma da Pelve , População Branca , Feminino , Humanos , Pessoa de Meia-Idade , Estudos RetrospectivosRESUMO
Effects of agave fructans as carrier agents on the encapsulation of blue corn anthocyanins using spray-drying were evaluated. Blue corn extract was mixed with 6%, 8%, 10%, and 12% (w/v) of agave fructans in duplicate and dried at 150 °C. The extract showed good contents of anthocyanins, polyphenols, and antioxidant activity. The increase of agave fructans in the encapsulated powders caused a significant increase (p < 0.05) in the humidity, water activity (aw), pH, bulk density, water solubility index (WSI), and color L* values. On the contrary, the agave fructan addition decreased the hygroscopicity, water absorption index (WAI), antioxidant activity, total anthocyanin, total polyphenol, and individual anthocyanin contents. The encapsulation of blue corn extract with 6% agave fructans (w/v) resulted in good physical, thermal, morphological, and high antioxidant properties. The results suggest that the use of agave fructans as wall material represents advantages in the conservation of anthocyanins and other bioactive compounds from blue corn extract during their encapsulation. The application of blue corn anthocyanin encapsulated powders as a food ingredient is promising for food pigmentation, representing additional advantages for their contribution as a soluble fiber that can benefit the health of consumers.
RESUMO
BACKGROUND: Patients affected with persistent genital arousal disorder report unprovoked, excessive, and unremitting genital arousal unrelated to sexual desire. Those afflicted experience severe physical and psychological distress with significant feelings of shame, guilt, and frustration. Definitive treatment options for this disorder are limited. CASE: We present the case of a 32-year-old woman, gravida 1 para 1, with persistent genital arousal disorder after treatment of an uncomplicated urinary tract infection while in a military-deployed environment. After numerous treatment modalities failed, she responded to an implanted sacral neuromodulator. CONCLUSION: Persistent genital arousal disorder may be the result of upregulated sacral nerve pathways. We report the use of sacral neuromodulation using unique program settings, which may be an effective alternative in the treatment of this distressing disorder.
Assuntos
Terapia por Estimulação Elétrica , Disfunções Sexuais Fisiológicas/terapia , Bexiga Urinária Hiperativa/terapia , Inibidores da Liberação da Acetilcolina/administração & dosagem , Administração Intravesical , Adulto , Toxinas Botulínicas Tipo A/administração & dosagem , Eletrodos Implantados , Feminino , Humanos , Plexo Lombossacral , Disfunções Sexuais Fisiológicas/complicações , Disfunções Sexuais Fisiológicas/psicologia , Bexiga Urinária Hiperativa/complicaçõesRESUMO
BACKGROUND: : Transient groin pain is a therapeutically challenging complication associated with transobturator sling procedures. CASE: : We present the case of a 37-year-old woman who presented with debilitating left groin pain and dyspareunia following placement of transobturator sling. Pelvic floor physical therapy, medications, and trigger point injections failed to provide relief. Workup included magnetic resonance imaging of the pelvis, complex cystometrics, and additional trigger point injections. Surgical removal of the complete left side of the tape including the portion imbedded in the obturator foramen was performed with a combined vaginal-transcutaneous approach. Extirpation of the mesh arm brought prompt and full resolution of the patient's symptoms. CONCLUSIONS: : Surgical removal of the transobturator tape through the obturator foramen can be safely performed using a combined vaginal-transcutaneous approach.