New prenylated quinones from Peperomia galioides

Two new prenylated quinones, piperogalone and galopiperone, and a new prenylated dihydroquinone, hydropiperone, were isolated from #Peperomia galioides H.B.K (#Piperaceae). Hydropiperone exhibited potent antiparasitic activity against three species of #Leishmania$. (Résumé d'auteur

In vitro and in vivo leishmanicidal studies of Peperomia galioides (Piperaceae)

Petroleum ether and methylene chloride extracts of #Peperomia galioides and three phenylated diphenols, grifolic acid, grifolin and piperogalin exhibited in vitro antileishmanial activity. During the course of infection of BALB/c mice with #Leishmania amazonensis, the treatments with each of these compounds did not influence the progression of the disease. (Résumé d'auteur

Impact of safety-related dose reductions or discontinuations on sustained virologic response in HCV-infected patients: Results from the GUARD-C Cohort

BACKGROUND: Despite the introduction of direct-acting antiviral agents for chronic hepatitis C virus (HCV) infection, peginterferon alfa/ribavirin remains relevant in many resource-constrained settings. The non-randomized GUARD-C cohort investigated baseline predictors of safety-related dose reductions or discontinuations (sr-RD) and their impact on sustained virologic response (SVR) in patients receiving peginterferon alfa/ribavirin in routine practice. METHODS: A total of 3181 HCV-mono-infected treatment-naive patients were assigned to 24 or 48 weeks of peginterferon alfa/ribavirin by their physician. Patients were categorized by time-to-first sr-RD (Week 4/12). Detailed analyses of the impact of sr-RD on SVR24 (HCV RNA <50 IU/mL) were conducted in 951 Caucasian, noncirrhotic genotype (G)1 patients assigned to peginterferon alfa-2a/ribavirin for 48 weeks. The probability of SVR24 was identified by a baseline scoring system (range: 0-9 points) on which scores of 5 to 9 and <5 represent high and low probability of SVR24, respectively. RESULTS: SVR24 rates were 46.1% (754/1634), 77.1% (279/362), 68.0% (514/756), and 51.3% (203/396), respectively, in G1, 2, 3, and 4 patients. Overall, 16.9% and 21.8% patients experienced 651 sr-RD for peginterferon alfa and ribavirin, respectively. Among Caucasian noncirrhotic G1 patients: female sex, lower body mass index, pre-existing cardiovascular/pulmonary disease, and low hematological indices were prognostic factors of sr-RD; SVR24 was lower in patients with 651 vs. no sr-RD by Week 4 (37.9% vs. 54.4%; P = 0.0046) and Week 12 (41.7% vs. 55.3%; P = 0.0016); sr-RD by Week 4/12 significantly reduced SVR24 in patients with scores <5 but not 655. CONCLUSIONS: In conclusion, sr-RD to peginterferon alfa-2a/ribavirin significantly impacts on SVR24 rates in treatment-naive G1 noncirrhotic Caucasian patients. Baseline characteristics can help select patients with a high probability of SVR24 and a low probability of sr-RD with peginterferon alfa-2a/ribavirin

Impact of Safety-Related Dose Reductions or Discontinuations on Sustained Virologic Response in HCV-Infected Patients: Results from the GUARD-C Cohort.

BACKGROUND: Despite the introduction of direct-acting antiviral agents for chronic hepatitis C virus (HCV) infection, peginterferon alfa/ribavirin remains relevant in many resource-constrained settings. The non-randomized GUARD-C cohort investigated baseline predictors of safety-related dose reductions or discontinuations (sr-RD) and their impact on sustained virologic response (SVR) in patients receiving peginterferon alfa/ribavirin in routine practice. METHODS: A total of 3181 HCV-mono-infected treatment-naive patients were assigned to 24 or 48 weeks of peginterferon alfa/ribavirin by their physician. Patients were categorized by time-to-first sr-RD (Week 4/12). Detailed analyses of the impact of sr-RD on SVR24 (HCV RNA <50 IU/mL) were conducted in 951 Caucasian, noncirrhotic genotype (G)1 patients assigned to peginterferon alfa-2a/ribavirin for 48 weeks. The probability of SVR24 was identified by a baseline scoring system (range: 0-9 points) on which scores of 5 to 9 and <5 represent high and low probability of SVR24, respectively. RESULTS: SVR24 rates were 46.1% (754/1634), 77.1% (279/362), 68.0% (514/756), and 51.3% (203/396), respectively, in G1, 2, 3, and 4 patients. Overall, 16.9% and 21.8% patients experienced ≥1 sr-RD for peginterferon alfa and ribavirin, respectively. Among Caucasian noncirrhotic G1 patients: female sex, lower body mass index, pre-existing cardiovascular/pulmonary disease, and low hematological indices were prognostic factors of sr-RD; SVR24 was lower in patients with ≥1 vs. no sr-RD by Week 4 (37.9% vs. 54.4%; P = 0.0046) and Week 12 (41.7% vs. 55.3%; P = 0.0016); sr-RD by Week 4/12 significantly reduced SVR24 in patients with scores <5 but not ≥5. CONCLUSIONS: In conclusion, sr-RD to peginterferon alfa-2a/ribavirin significantly impacts on SVR24 rates in treatment-naive G1 noncirrhotic Caucasian patients. Baseline characteristics can help select patients with a high probability of SVR24 and a low probability of sr-RD with peginterferon alfa-2a/ribavirin.This study was sponsored by F. Hoffmann-La Roche Ltd, Basel, Switzerland. Support for third-party writing assistance for this manuscript, furnished by Blair Jarvis MSc, ELS, of Health Interactions, was provided by F. Hoffmann-La Roche Ltd, Basel, Switzerland

Impact of safety-related dose reductions or discontinuations on sustained virologic response in HCV-infected patients: Results from the GUARD-C Cohort

Background: Despite the introduction of direct-acting antiviral agents for chronic hepatitis C virus (HCV) infection, peginterferon alfa/ribavirin remains relevant in many resource-constrained settings. The non-randomized GUARD-C cohort investigated baseline predictors of safety-related dose reductions or discontinuations (sr-RD) and their impact on sustained virologic response (SVR) in patients receiving peginterferon alfa/ribavirin in routine practice. Methods: A total of 3181 HCV-mono-infected treatment-naive patients were assigned to 24 or 48 weeks of peginterferon alfa/ribavirin by their physician. Patients were categorized by time-to-first sr-RD (Week 4/12). Detailed analyses of the impact of sr-RD on SVR24 (HCV RNA <50 IU/mL) were conducted in 951 Caucasian, noncirrhotic genotype (G)1 patients assigned to peginterferon alfa-2a/ribavirin for 48 weeks. The probability of SVR24 was identified by a baseline scoring system (range: 0-9 points) on which scores of 5 to 9 and <5 represent high and low probability of SVR24, respectively. Results: SVR24 rates were 46.1 % (754/1634), 77.1% (279/362), 68.0% (514/756), and 51.3% (203/396), respectively, in G1,2, 3, and 4 patients. Overall, 16.9% and 21.8% patients experienced 651 sr-RD for peginterferon alfa and ribavirin, respectively. Among Caucasian noncirrhotic G1 patients: female sex, lower body mass index, pre-existing cardiovascular/pulmonary disease, and low hematological indices were prognostic factors of sr-RD; SVR24 was lower in patients with 651 vs. no sr-RD by Week 4 (37.9% vs. 54.4%; P = 0.0046) and Week 12 (41.7% vs. 55.3%; P = 0.0016); sr-RD by Week 4/12 significantly reduced SVR24 in patients with scores <5 but not 655. Conclusions: In conclusion, sr-RD to peginterferon alfa-2a/ribavirin significantly impacts on SVR24 rates in treatment-naive G1 noncirrhotic Caucasian patients. Baseline characteristics can help select patients with a high probability of SVR24 and a low probability of sr-RD with peginter-feron alfa-2a/ribavirin

Bisbenzylisoquinoline alkaloids from Guatteria boliviana (Annonaceae)

Together with known alkaloids, five new bisbenzylisoquinoline derivatives were isolated from the stem bark of #Guatteria boliviana (Annonaceae), puertogalines-A 1 and -B 2, (+)-guatteboline 3, philogaline 4 and (-)-antioquine 5. Their structures were elucidated by spectrometric methods and their antiparasitic activity was evaluated in vitro on #Leishmania sp., #Trypanosoma cruzi and #Plasmodium falciparum. Their cytotoxic activity aws also measured in KB cell line. (Résumé d'auteur

A thorough spectroscopic study of luminescent precursor solution of Y3Al5O12: Tb3+: influence of acetylacetone

International audienceUndoped and Tb3+-doped precursor solutions of Y3Al5O12 (YAG) have been prepared by the sol–gel process using alkoxide precursors stabilized by a chelating agent: acetylacetone (acacH), with various complexation ratios RC = 0, 1, 2 and 3 defined as the ratio between [Al(OPri)3] and [acacH]. Combining in situ UV-visible investigation of the hydrolysis process of these sols with X-ray diffraction study on the powders extracted after water addition to the sols, drying and subsequent heating, an optimal RC value has been determined. It leads to sols stable over a long period of time and resulting in a pure YAG phase. Structural and optical properties of Tb3+-doped precursor sols characterized by RC = 0 (as a reference for the influence of acacH) and RC = 1 (determined optimal value) were studied by means of X-ray Absorption Spectroscopy (XAS) and photoluminescence, respectively. Y K and Tb L3 edges XAS results show the presence of double heterometallic Y or Tb/Al alkoxides for the sol with RC = 1 involving pre-nuclei cluster with YAG structure. Emission and excitation spectra as well as decay curves were recorded and compared. Results revealed that the stabilized sol is much more efficient upon UV excitation than its unmodified counterpart thanks to an efficient energy transfer from acetylacetonate groups to active ions. Upon a 485 nm excitation, acac-modified samples remain the most efficient ones. It could be related to the dissimilar Tb local environments of the sols suggested by both UV-visible and photoluminescence excitation results

ANTIMALARIAL ACTIVITY OF SWARTZIA MADAGASCARIENSIS DESV. (LEGUMINOSAE), COMBRETUM GLUTINOSUM GUILL. & PERR. (COMBRETACEAE) AND TINOSPORA BAKIS MIERS. (MENISPERMACEAE), BURKINA FASO MEDICINAL PLANTS.

Swartzia madagascariensis   , Combretum glutinosum   and Tinospora bakis   are three plants of the folk medicine used by healers in Burkina Faso for the treatment of malaria. A scientific validation of this utilization was not previously made. Aqueous, methanol, hydromethanol extracts from the roots bark of S. madagascariensis, methanol and hydromethanol extracts from the leaves of C. glutinosum and aqueous and alkaloidal extracts from the roots of T. bakis were also made and their antimalarial activity was screened against Plasmodium falciparum   chloroquine-resistant strain W2 in vitro. The screening showed that the methanol and hydromethanol extracts of Swartzia madagascariensis, hydromethanol extracts of Combretum glutinosum and alkaloidal extracts of Tinospora bakis were active(5μg/ml < IC50 < 50 μg/ml)