11 research outputs found

    Triterpenic acids from Eugenia moraviana

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    A novel triterpene, characterized as 6alpha-hydroxybetulinic acid, was isolated from the leaves and stems of Eugenia moraviana (Myrtaceae), known in Brazil as Cambuí, together with three known compounds, platanic acid, betulinic acid and beta-sitosterol. Unequivocal ¹H and 13C assignments of 6alpha-hydroxybetulinic acid (3beta,6alpha-dihydroxy-20(29)-lupen-28-oic acid) and platanic acid were undertaken by spectral analysis including NOE and 2 D NMR experiments

    The Repercussions of Spinal Cord Injury on the Action of the Diaphragmatic Crura for Gastroesophageal Reflux Containment

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    Study Design. Cross-sectional and nonexperimental.Objective. To detect and compare functional abnormalities in the esophagus and esophagogastric junction in 2 groups with chronic spinal injuries, 1 with injuries at the phrenic innervation level and the other at upper thoracic levels, and to relate these to gastroesophageal reflux containment.Summary of Background Data. There are no studies on esophageal manometry with pH metering among spinal cord injury patients. Worldwide statistics reveal that the prevalence of gastroesophageal reflux disease among spinal cord injury patients is greater than among the general population, at around 22% to 27%. the diaphragmatic crura has been recognized as an important antire-flux barrier and should functionally be considered to be a muscle separated from the costal diaphragm. However, doubts remain regarding whether this difference relates to its innervation.Methods. This was a cross-sectional study on 29 patients with complete spinal cord injuries: 14 quadriplegics (level C(4)) and 15 paraplegics (levels T(1)-T(7)). Functional abnormalities of the esophagogastric junction, esophagus, and diaphragm were investigated using esophageal manometry and diaphragmatic video fluoroscopy. Presence of gastroesophageal reflux was investigated subjectively (pyrosis and regurgitation) and objectively (pH metering and endoscopy).Results. the incidence of gastroesophageal reflux disease was 27.6%, without difference between the groups. This became statistically significant when the mean diaphragmatic crural pressures were compared (quadriplegics: 37.5 +/- 17.8; paraplegics: 26.6 +/- 7.2; P = 0.048). It was also significant in relation to the prevalence of at least one of the objective and/or subjective reflux findings and/or esophageal peristaltism (quadriplegics: 85.7%; paraplegics: 40.0%; P = 0.011).Conclusion. Spinal injury at the level of the phrenic innervation did not predispose the quadriplegics toward greater risk of developing gastroesophageal reflux disease. Paradoxically, manometry showed significantly greater crural contractility among the quadriplegics.Universidade Federal de São Paulo, Discipline Emergency Med & Evidence Based Med, São Paulo, BrazilUniversidade Federal de São Paulo, Digest Physiol Sector SEFIDI, Discipline Surg Gastroenterol, São Paulo, BrazilUniversidade Federal de São Paulo, Digest Endoscopy Sector, São Paulo, BrazilUniversidade Federal de São Paulo, Hosp São Paulo, Radiol & Ultrasonog Sector, São Paulo, BrazilUniversidade Federal de São Paulo, Rehabil Ctr, Lar Escola Sao Francisco, São Paulo, BrazilUniversidade Federal de São Paulo, Dept Med, São Paulo, BrazilUniversidade Federal de São Paulo, Dept Neurol, São Paulo, BrazilUniversidade Federal de São Paulo, Discipline Emergency Med & Evidence Based Med, São Paulo, BrazilUniversidade Federal de São Paulo, Digest Physiol Sector SEFIDI, Discipline Surg Gastroenterol, São Paulo, BrazilUniversidade Federal de São Paulo, Digest Endoscopy Sector, São Paulo, BrazilUniversidade Federal de São Paulo, Hosp São Paulo, Radiol & Ultrasonog Sector, São Paulo, BrazilUniversidade Federal de São Paulo, Rehabil Ctr, Lar Escola Sao Francisco, São Paulo, BrazilUniversidade Federal de São Paulo, Dept Med, São Paulo, BrazilUniversidade Federal de São Paulo, Dept Neurol, São Paulo, BrazilWeb of Scienc

    In vitro antiproliferative and apoptotic effects of thiosemicarbazones based on (-)-camphene and R-(+)-limonene in human melanoma cells.

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    A series of 38 thiosemicarbazone derivatives based on camphene and limonene were evaluated for their antiproliferative activity. Among them, 19 were synthesized and characterized using proton and carbon-13 nuclear magnetic resonance (1H and 13C NMR). For initial compound selection, human melanoma cells (SK-MEL-37) were exposed to a single concentration of a compound (100 μM) for 24, 48, and 72 hours, and cell detachment was visually observed. Cell viability was determined using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method. Nineteen compounds (4, 6, 8, 11, 13, 14, 15, 16, 17, 18, 20, 22, 25, 26, 31, 3', 4', 6', and 9') yielded cell viability below 20%. Subsequently, IC50 values for these compounds were determined, ranging from 11.56 to 55.38 μM, after 72 hours of treatment. Compound 17 (o-hydroxybenzaldehyde (-)-camphene-based thiosemicarbazone) demonstrated the lowest IC50 value, followed by compound 4 (benzaldehyde (-) camphene-based thiosemicarbazone) at 12.84 μM. Regarding compound 4, we observed the induction of a characteristic ladder pattern of DNA fragmentation through gel electrophoresis. Furthermore, fluorescence, flow cytometry and scanning microscopy assays revealed morphological changes consistent with apoptosis induction. Additionally, the measurement of caspase 6 and 8 activity in cellular extracts after treatment for 2, 4, 6, and 24 hours suggested the potential involvement of the extrinsic apoptosis pathway in the mechanism of action of compound 4. Further investigations, including molecular docking studies, are required to fully explore the potential of compound 4 and the other selected compounds, highlighting their promising role in future melanoma therapy research

    Antitrypanosomal Activity of Novel Benzaldehyde-Thiosemicarbazone Derivatives from Kaurenoic Acid †

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    A series of new thiosemicarbazones derived from natural diterpene kaurenoic acid were synthesized and tested against the epimastigote forms of Trypanosoma cruzi to evaluate their antitrypanosomal potential. Seven of the synthesized thiosemicarbazones were more active than kaurenoic acid with IC50 values between 2-24.0 mM. The o-nitro-benzaldehyde-thiosemicarbazone derivative was the most active compound with IC50 of 2.0 mM. The results show that the structural modifications accomplished enhanced the antitrypanosomal activity of these compounds. Besides, the thiocyanate, thiosemicarbazide and the p- methyl, p-methoxy, p-dimethylamine, m-nitro and o-chlorobenzaldehyde-thiosemicarbazone derivatives displayed lower toxicity for LLMCK2 cells than kaurenoic acid, exhibing an IC50 of 59.5 mM

    Synthesis of novel (-)-Camphene-based thiosemicarbazones and evaluation of anti-<i>Mycobacterium tuberculosis</i> activity

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    <p>In this work the aim of study was the synthesis and evaluation of <i>in vitro</i> anti-<i>Mycobacterium tuberculosis</i> activity as well as the cytotoxicity in VERO cells of a series of 17 novel thiosemicarbazones derived from the natural monoterpene (-)-camphene by REMA and MTT methods. Overall, the majority of tested compounds exhibited considerable inhibitory effects on the growth of <i>M. tuberculosis</i> H<sub>37</sub>Rv, especially the derivatives <b>3</b>, <b>4a–c</b>, <b>4f</b>, <b>4i</b>, <b>4k</b>, <b>5</b> and <b>6a–b</b>. MIC values of 20 tested compounds ranged from 3.9 to > 250 μg/mL. It was found that when inserting new nitrogenous groups to the (-)-camphene increased the anti-<i>M. tuberculosis</i> activity of some compounds. The SI was calculated for all compounds that showed highly potent anti-<i>M. tuberculosis</i> activity and the best SI values were 21.36, 26.92 and 31.62 (<b>4b</b>, <b>6a</b> and <b>6b</b>), and may be considered potential candidates for future antituberculosis drugs.</p

    CHEMICAL STUDY AND ANTIPROLIFERATIVE, TRYPANOCIDAL AND LEISHMANICIDAL ACTIVITIES OF Maxillaria picta

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    The chemical study of the orchid Maxillaria picta resulted in the isolation of the bioactive stilbenes phoyunbene B and phoyunbene C, in addition to four phenolic acids, one xanthone, steroidal compounds and two triterpenes. Crude extract, fractions, subfractions and the isolated xanthone were evaluated for anticancer activity against human tumor cell lines and against evolutionary forms of T. cruzi and L. amazonensis. The structures of the compounds were determined by GC-MS, and ¹H NMR, 13C NMR spectral methods as well as bidimensional techniques
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