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F Velasoria - One of the best experts on this subject based on the ideXlab platform.
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serum levels of non persistent environmental pollutants and risk of incident hypertension in a sub cohort from the epic study
Environmental Research, 2021Co-Authors: Elena Salamancafernandez, L M Iribarneduran, F Velasoria, Nicolas Olea, Miguel Rodriguezbarranco, A Arrebolamoreno, Maria Jose Sanchez, Juan P ArrebolaAbstract:Abstract Background The prevalence of arterial hypertension (AHT), a well-known risk factor for cardiovascular disease, has considerably increased over last decades. Non-persistent environmental pollutants (npEPs) are a group of ubiquitous chemicals, widely used in consumer products such as food packaging and cosmetics, which have been identified as endocrine disrupting chemicals and obesogens. The aim of this study was to assess the potential associations of serum levels of three groups of npEPs with the risk of incident AHT. Methods Cohort study within a sub-cohort of Granada EPIC-Spain center (n = 670). We quantified serum concentrations of three groups of npEPs, i.e., bisphenol A (BPA), four parabens: methylparaben (MP), ethylparaben (EP), propylparaben (PP) and butylparaben (BP), and two Benzophenones: benzophenone 1 (BP1), benzophenone 3 (BP3), in samples collected at recruitment. Statistical analyses were performed by means of Cox Proportional Hazard Models. Results Median follow-up time was 23 years. BPA and MP were found in >80% of the study population. Individuals within the 4th PP quartile (0.53–9.24 ng/ml) showed a statistically significant increased risk of AHT (HR = 1.40, p = 0.015). No associations were found for the rest of pollutants. Conclusions Overall, we evidenced no associations of most npEPs with AHT risk, with the exception of an increased risk in the highest PP percentiles. Considering the limitations of using one spot serum sample for exposure characterization, further research on the potential contribution of npEPs on the development of AHT risk is warranted.
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cosmetic and personal care product use urinary levels of parabens and Benzophenones and risk of endometriosis results from the endea study
Environmental Research, 2020Co-Authors: F M Peinado, Olga Oconhernandez, L M Iribarneduran, F Velasoria, A Ubina, C Padilla, J C Mora, J Cardona, J Leon, M F FernandezAbstract:Abstract Aim: To explore the relationship of urinary concentrations of different congeners of Benzophenones and parabens with the utilization of cosmetics and personal care products (PCPs) and their impact on the risk of endometriosis, and to evaluate the influence of oxidative stress on associations found. Methods: This case-control study comprised a subsample of 124 women (35 cases; 89 controls). Endometriosis was confirmed (cases) or ruled out (controls) by laparoscopy, with visual inspection of the pelvis and biopsy of suspected lesions (histological diagnosis). Urinary concentrations of benzophenone-1 (BP-1), benzophenone-3 (BP-3), 4-hydroxibenzophenone (4-OH-BP), methyl- (MeP), ethyl- (EtP), propyl- (PrP), and butyl-paraben (BuP), and biomarkers of oxidative stress [lipid peroxidation (TBARS) and total antioxidant power (TAP)] were quantified. Information was gathered on the frequency of use of cosmetics and PCPs. Associations between the frequency of cosmetics/PCP use, urinary concentrations of Benzophenones and parabens, oxidative stress, and endometriosis risk were explored in logistic and linear multivariable regression analyses. Results: The frequency of utilization of certain cosmetics and PCPs was significantly associated with urinary concentrations of Benzophenones and parabens. After adjustment for potential confounders, the risk of endometriosis was increased in women in the second versus first terciles of MeP (OR = 5.63; p-value
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urinary levels of bisphenol a Benzophenones and parabens in tunisian women a pilot study
Science of The Total Environment, 2016Co-Authors: I Jimenezdiaz, F Velasoria, Mariana F Fernandez, Francisco Artachocordon, H Belhassen, Juan P Arrebola, R Ghali, Abderrazek Hedhili, Nicolas OleaAbstract:Bisphenol A (BPA), Benzophenones and parabens are commonly used in the production of polycarbonate plastics, as UV-filters and as antimicrobial preservatives, respectively, and they are thought to exhibit endocrine disrupting properties. Exposure to these compounds remains poorly characterized in developing countries, despite the fact that certain behaviors related to westernization have the potential to influence exposure. The aim of this pilot study was to measure urinary concentrations of BPA, six different Benzophenones and four parabens in 34 Tunisian women. In addition, we identified some socio-demographic and dietary predictors of exposure to these compounds. Chemical analyses were carried out by dispersive liquid-liquid microextraction (DLLME) and ultra-high performance liquid chromatography with tandem mass spectrometry detection (UHPLC-MS/MS). Detection frequencies of methylparaben (MP), ethylparaben (EP) and propylparaben (PP) ranged between 67.6 and 94.1%. Butylparaben (BP) was found in 38.2% of the analyzed samples; BPA in 64.7%; and benzophenone-1 (BP-1) and benzophenone-3 (BP-3) were detected in 91.2 and 64.7% of the analyzed samples, respectively. Urinary geometric mean concentrations of MP, EP, PP, and BP were 30.1, 1.4, 2.0 and 0.5ngmL(-1), respectively. Geometric mean concentrations of BPA, BP-1, and BP-3 were 0.4, 1.3 and 1.1ngmL(-1), respectively. Our results suggest that Tunisian women are widely exposed to BPA, parabens and some Benzophenones. Further studies on the general Tunisian population are needed in order to assess the levels of exposure to these compounds and to identify sources of exposure and population groups at higher risk.
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uhplc ms ms method for the determination of bisphenol a and its chlorinated derivatives bisphenol s parabens and Benzophenones in human urine samples
Analytical and Bioanalytical Chemistry, 2014Co-Authors: F Velasoria, O Ballesteros, A Zafragomez, L Ballesteros, A NavalonAbstract:In the present work, a new method based on a sample treatment by dispersive liquid–liquid microextraction (DLLME) for the extraction of six bisphenols (bisphenol A, bisphenol S, and monochloro-, dichloro-, trichloro-, and tetrachlorobisphenol A), four parabens (methyl-, ethyl-, propyl-, and butylparaben), and six Benzophenones (benzophenone-1, benzophenone-2, benzophenone-3, benzophenone-6, benzophenone-8, and 4-hydroxybenzophenone) in human urine samples, followed by ultrahigh-performance liquid chromatography–tandem mass spectrometry (UHPLC–MS/MS) analysis, is validated. An enzymatic treatment allows determining the total content of the target EDCs. The extraction parameters were accurately optimized using multivariate optimization strategies. Ethylparaben ring-13C6, benzophenone-d10, and bisphenol A-d16 were used as surrogates. Limits of quantification ranging from 0.1 to 0.6 ng mL−1 and interday variabilities (evaluated as relative standard deviations) from 2.0 to 13.8 % were obtained. The method was validated using matrix-matched standard calibration followed by a recovery assay with spiked samples. Recovery rates ranged from 94 to 106 %. A good linearity, for concentrations up to 300 ng mL−1 for parabens and 40 ng mL−1 for Benzophenones and bisphenols, was also obtained. The method was satisfactorily applied for the determination of target compounds in human urine samples from 20 randomly selected individuals.
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determination of Benzophenones in human placental tissue samples by liquid chromatography tandem mass spectrometry
Talanta, 2011Co-Authors: F Velasoria, O Ballesteros, A Zafragomez, A Navalon, I Jimenezdiaz, Mariana F Fernandez, R Rodriguezgomez, J L Vilchez, Nicolas OleaAbstract:Benzophenones (BPs) are a family of compounds widely used to protect the skin and hair from UV irradiation. Despite human exposure to BPs through dermal application of products containing sunscreen agents and the increasing evidence that BPs are able to interfere with endocrine systems, few studies have examined the occurrence of BPs in humans. In this work, we propose a new liquid chromatography-tandem mass spectrometry (LC-MS/MS) method to determine six BPs, namely, benzophenone-1 (BP-1), benzophenone-2 (BP-2), benzophenone-3 (BP-3), benzophenone-6 (BP-6), benzophenone-8 (BP-8) and 4-hydroxybenzophenone (4-OH-BP) in human placental tissue samples. The method involves an extraction step of the analytes from the samples using ethyl acetate, followed by a clean-up step using centrifugation prior to their quantification by LC-MS/MS using an atmospheric pressure chemical ionization (APCI) interface in the positive mode. Benzophenone-d(10) (BP-d(10)) was used as surrogate. Found detection limits (LOD) ranged from 0.07 to 0.3 ng g(-1) and quantification limits (LOQ) from 0.3 to 1.0 ng g(-1), while inter- and intra-day variability was under 5%. The method was validated using standard addition calibration and a recovery assay. Recovery rates for spiked samples ranged from 98 to 104%. This method was satisfactorily applied for the determination of BPs in 16 placental tissue samples collected from women who live in Granada (Spain).
Nicolas Olea - One of the best experts on this subject based on the ideXlab platform.
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serum levels of non persistent environmental pollutants and risk of incident hypertension in a sub cohort from the epic study
Environmental Research, 2021Co-Authors: Elena Salamancafernandez, L M Iribarneduran, F Velasoria, Nicolas Olea, Miguel Rodriguezbarranco, A Arrebolamoreno, Maria Jose Sanchez, Juan P ArrebolaAbstract:Abstract Background The prevalence of arterial hypertension (AHT), a well-known risk factor for cardiovascular disease, has considerably increased over last decades. Non-persistent environmental pollutants (npEPs) are a group of ubiquitous chemicals, widely used in consumer products such as food packaging and cosmetics, which have been identified as endocrine disrupting chemicals and obesogens. The aim of this study was to assess the potential associations of serum levels of three groups of npEPs with the risk of incident AHT. Methods Cohort study within a sub-cohort of Granada EPIC-Spain center (n = 670). We quantified serum concentrations of three groups of npEPs, i.e., bisphenol A (BPA), four parabens: methylparaben (MP), ethylparaben (EP), propylparaben (PP) and butylparaben (BP), and two Benzophenones: benzophenone 1 (BP1), benzophenone 3 (BP3), in samples collected at recruitment. Statistical analyses were performed by means of Cox Proportional Hazard Models. Results Median follow-up time was 23 years. BPA and MP were found in >80% of the study population. Individuals within the 4th PP quartile (0.53–9.24 ng/ml) showed a statistically significant increased risk of AHT (HR = 1.40, p = 0.015). No associations were found for the rest of pollutants. Conclusions Overall, we evidenced no associations of most npEPs with AHT risk, with the exception of an increased risk in the highest PP percentiles. Considering the limitations of using one spot serum sample for exposure characterization, further research on the potential contribution of npEPs on the development of AHT risk is warranted.
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determination of personal care products Benzophenones and parabens in human menstrual blood
Journal of Chromatography B, 2016Co-Authors: I Jimenezdiaz, L M Iribarneduran, Olga Ocon, E Salamanca, Mariana F Fernandez, Nicolas Olea, E BarrancoAbstract:Abstract Benzophenones and parabens are synthetic chemicals used in many personal care products, foods and pharmaceuticals. Benzophenones are used to protect the skin and materials from the adverse effects of UV-radiation, and parabens are used as preservatives. Despite their widespread occurrence and proven endocrine disrupting activity, relatively little is known about human exposure to these compounds. In the present work, an analytical method based on sample treatment using dispersive liquid-liquid microextraction (DLLME) for the extraction of six Benzophenones (benzophenone-1, −2, −3, −6, −8 and 4-hydroxybenzophenone) and four parabens (methyl-, ethyl-, propyl- and butyl- paraben) from human menstrual blood samples, followed by ultrahigh performance liquid chromatography-tandem mass spectrometry (UHPLC–MS/MS) analysis, is proposed and validated. The method was validated using matrix-matched standard calibration followed by a recovery assay with spiked samples. The limits of detection ranged from 0.1 to 0.3 ng mL −1 , with recoveries of 93.8% to 108.9%, and precision (evaluated as relative standard deviation) lower than 14% for all selected compounds. This method was successfully applied for the determination of the target compounds in 25 samples of human menstrual blood. Methylparaben and benzophenone-3 were the most frequently detected compounds (96%).
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urinary levels of bisphenol a Benzophenones and parabens in tunisian women a pilot study
Science of The Total Environment, 2016Co-Authors: I Jimenezdiaz, F Velasoria, Mariana F Fernandez, Francisco Artachocordon, H Belhassen, Juan P Arrebola, R Ghali, Abderrazek Hedhili, Nicolas OleaAbstract:Bisphenol A (BPA), Benzophenones and parabens are commonly used in the production of polycarbonate plastics, as UV-filters and as antimicrobial preservatives, respectively, and they are thought to exhibit endocrine disrupting properties. Exposure to these compounds remains poorly characterized in developing countries, despite the fact that certain behaviors related to westernization have the potential to influence exposure. The aim of this pilot study was to measure urinary concentrations of BPA, six different Benzophenones and four parabens in 34 Tunisian women. In addition, we identified some socio-demographic and dietary predictors of exposure to these compounds. Chemical analyses were carried out by dispersive liquid-liquid microextraction (DLLME) and ultra-high performance liquid chromatography with tandem mass spectrometry detection (UHPLC-MS/MS). Detection frequencies of methylparaben (MP), ethylparaben (EP) and propylparaben (PP) ranged between 67.6 and 94.1%. Butylparaben (BP) was found in 38.2% of the analyzed samples; BPA in 64.7%; and benzophenone-1 (BP-1) and benzophenone-3 (BP-3) were detected in 91.2 and 64.7% of the analyzed samples, respectively. Urinary geometric mean concentrations of MP, EP, PP, and BP were 30.1, 1.4, 2.0 and 0.5ngmL(-1), respectively. Geometric mean concentrations of BPA, BP-1, and BP-3 were 0.4, 1.3 and 1.1ngmL(-1), respectively. Our results suggest that Tunisian women are widely exposed to BPA, parabens and some Benzophenones. Further studies on the general Tunisian population are needed in order to assess the levels of exposure to these compounds and to identify sources of exposure and population groups at higher risk.
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determination of Benzophenones in human placental tissue samples by liquid chromatography tandem mass spectrometry
Talanta, 2011Co-Authors: F Velasoria, O Ballesteros, A Zafragomez, A Navalon, I Jimenezdiaz, Mariana F Fernandez, R Rodriguezgomez, J L Vilchez, Nicolas OleaAbstract:Benzophenones (BPs) are a family of compounds widely used to protect the skin and hair from UV irradiation. Despite human exposure to BPs through dermal application of products containing sunscreen agents and the increasing evidence that BPs are able to interfere with endocrine systems, few studies have examined the occurrence of BPs in humans. In this work, we propose a new liquid chromatography-tandem mass spectrometry (LC-MS/MS) method to determine six BPs, namely, benzophenone-1 (BP-1), benzophenone-2 (BP-2), benzophenone-3 (BP-3), benzophenone-6 (BP-6), benzophenone-8 (BP-8) and 4-hydroxybenzophenone (4-OH-BP) in human placental tissue samples. The method involves an extraction step of the analytes from the samples using ethyl acetate, followed by a clean-up step using centrifugation prior to their quantification by LC-MS/MS using an atmospheric pressure chemical ionization (APCI) interface in the positive mode. Benzophenone-d(10) (BP-d(10)) was used as surrogate. Found detection limits (LOD) ranged from 0.07 to 0.3 ng g(-1) and quantification limits (LOQ) from 0.3 to 1.0 ng g(-1), while inter- and intra-day variability was under 5%. The method was validated using standard addition calibration and a recovery assay. Recovery rates for spiked samples ranged from 98 to 104%. This method was satisfactorily applied for the determination of BPs in 16 placental tissue samples collected from women who live in Granada (Spain).
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a multiclass method for endocrine disrupting chemical residue analysis in human placental tissue samples by uhplc ms ms
Analytical Methods, 2011Co-Authors: F Velasoria, O Ballesteros, A Zafragomez, I Jimenezdiaz, Mariana F Fernandez, Nicolas Olea, R Rodriguezgomez, A NavalonAbstract:The group of compounds commonly called endocrine-disrupting chemicals covers a wide range of synthetic and natural substances able to alter the normal hormone function of wildlife and humans, consequently causing adverse health effects. Bisphenol A (BPA) and its chlorinated derivatives, Benzophenones (BPs) and parabens (PBs), belong to this group of compounds. In this work, we propose a multiclass ultra-high-performance liquid chromatography-tandem mass spectrometry (UHPLC–MS/MS) method to determine BPA, its four chlorinated derivatives (monochloro-, dichloro-, trichloro- and tetrachloro-bisphenol A), six BPs (benzophenone-1, benzophenone-2, benzophenone-3, benzophenone-6, benzophenone-8 and 4-hidroxybenzophenone) and four PBs (methylparaben, ethylparaben, propylparaben and butylparaben) in human placental tissue samples. The method involves an extraction step of the analytes from the samples using ethyl acetate, followed by a clean-up step by centrifugation prior to their quantification by UHPLC–MS/MS using an atmospheric pressure chemical ionization (APCI) interface in the negative mode. Deuterated bisphenol A (BPA-d16) was used as surrogate. The limits of detection (LOD) found ranged from 0.03 to 0.6 ng g−1, the limits of quantification (LOQ) from 0.1 to 1.4 ng g−1, while inter- and intra-day variability was under 8%. The method was validated using matrix-matched calibration standard and a spike recovery assay. Recovery rates for spiked samples ranged from 95% to 106%. This method was satisfactorily applied to the determination of these compounds in 50 placental tissue samples collected from women who live in the province of Granada (Spain).
A Navalon - One of the best experts on this subject based on the ideXlab platform.
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uhplc ms ms method for the determination of bisphenol a and its chlorinated derivatives bisphenol s parabens and Benzophenones in human urine samples
Analytical and Bioanalytical Chemistry, 2014Co-Authors: F Velasoria, O Ballesteros, A Zafragomez, L Ballesteros, A NavalonAbstract:In the present work, a new method based on a sample treatment by dispersive liquid–liquid microextraction (DLLME) for the extraction of six bisphenols (bisphenol A, bisphenol S, and monochloro-, dichloro-, trichloro-, and tetrachlorobisphenol A), four parabens (methyl-, ethyl-, propyl-, and butylparaben), and six Benzophenones (benzophenone-1, benzophenone-2, benzophenone-3, benzophenone-6, benzophenone-8, and 4-hydroxybenzophenone) in human urine samples, followed by ultrahigh-performance liquid chromatography–tandem mass spectrometry (UHPLC–MS/MS) analysis, is validated. An enzymatic treatment allows determining the total content of the target EDCs. The extraction parameters were accurately optimized using multivariate optimization strategies. Ethylparaben ring-13C6, benzophenone-d10, and bisphenol A-d16 were used as surrogates. Limits of quantification ranging from 0.1 to 0.6 ng mL−1 and interday variabilities (evaluated as relative standard deviations) from 2.0 to 13.8 % were obtained. The method was validated using matrix-matched standard calibration followed by a recovery assay with spiked samples. Recovery rates ranged from 94 to 106 %. A good linearity, for concentrations up to 300 ng mL−1 for parabens and 40 ng mL−1 for Benzophenones and bisphenols, was also obtained. The method was satisfactorily applied for the determination of target compounds in human urine samples from 20 randomly selected individuals.
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determination of Benzophenones in human placental tissue samples by liquid chromatography tandem mass spectrometry
Talanta, 2011Co-Authors: F Velasoria, O Ballesteros, A Zafragomez, A Navalon, I Jimenezdiaz, Mariana F Fernandez, R Rodriguezgomez, J L Vilchez, Nicolas OleaAbstract:Benzophenones (BPs) are a family of compounds widely used to protect the skin and hair from UV irradiation. Despite human exposure to BPs through dermal application of products containing sunscreen agents and the increasing evidence that BPs are able to interfere with endocrine systems, few studies have examined the occurrence of BPs in humans. In this work, we propose a new liquid chromatography-tandem mass spectrometry (LC-MS/MS) method to determine six BPs, namely, benzophenone-1 (BP-1), benzophenone-2 (BP-2), benzophenone-3 (BP-3), benzophenone-6 (BP-6), benzophenone-8 (BP-8) and 4-hydroxybenzophenone (4-OH-BP) in human placental tissue samples. The method involves an extraction step of the analytes from the samples using ethyl acetate, followed by a clean-up step using centrifugation prior to their quantification by LC-MS/MS using an atmospheric pressure chemical ionization (APCI) interface in the positive mode. Benzophenone-d(10) (BP-d(10)) was used as surrogate. Found detection limits (LOD) ranged from 0.07 to 0.3 ng g(-1) and quantification limits (LOQ) from 0.3 to 1.0 ng g(-1), while inter- and intra-day variability was under 5%. The method was validated using standard addition calibration and a recovery assay. Recovery rates for spiked samples ranged from 98 to 104%. This method was satisfactorily applied for the determination of BPs in 16 placental tissue samples collected from women who live in Granada (Spain).
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a multiclass method for endocrine disrupting chemical residue analysis in human placental tissue samples by uhplc ms ms
Analytical Methods, 2011Co-Authors: F Velasoria, O Ballesteros, A Zafragomez, I Jimenezdiaz, Mariana F Fernandez, Nicolas Olea, R Rodriguezgomez, A NavalonAbstract:The group of compounds commonly called endocrine-disrupting chemicals covers a wide range of synthetic and natural substances able to alter the normal hormone function of wildlife and humans, consequently causing adverse health effects. Bisphenol A (BPA) and its chlorinated derivatives, Benzophenones (BPs) and parabens (PBs), belong to this group of compounds. In this work, we propose a multiclass ultra-high-performance liquid chromatography-tandem mass spectrometry (UHPLC–MS/MS) method to determine BPA, its four chlorinated derivatives (monochloro-, dichloro-, trichloro- and tetrachloro-bisphenol A), six BPs (benzophenone-1, benzophenone-2, benzophenone-3, benzophenone-6, benzophenone-8 and 4-hidroxybenzophenone) and four PBs (methylparaben, ethylparaben, propylparaben and butylparaben) in human placental tissue samples. The method involves an extraction step of the analytes from the samples using ethyl acetate, followed by a clean-up step by centrifugation prior to their quantification by UHPLC–MS/MS using an atmospheric pressure chemical ionization (APCI) interface in the negative mode. Deuterated bisphenol A (BPA-d16) was used as surrogate. The limits of detection (LOD) found ranged from 0.03 to 0.6 ng g−1, the limits of quantification (LOQ) from 0.1 to 1.4 ng g−1, while inter- and intra-day variability was under 8%. The method was validated using matrix-matched calibration standard and a spike recovery assay. Recovery rates for spiked samples ranged from 95% to 106%. This method was satisfactorily applied to the determination of these compounds in 50 placental tissue samples collected from women who live in the province of Granada (Spain).
Shaukath Ara Khanum - One of the best experts on this subject based on the ideXlab platform.
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Synthesis and antiproliferative activity of benzophenone tagged pyridine analogues towards activation of caspase activated DNase mediated nuclear fragmentation in Dalton's lymphoma.
Bioorganic Chemistry, 2016Co-Authors: Mohammed Al-ghorbani, Prabhu Thirusangu, H.d. Gurupadaswamy, Vasupradha Girish, H.g. Shamanth Neralagundi, B.t. Prabhakar, Shaukath Ara KhanumAbstract:A series of Benzophenones possessing pyridine nucleus 8a–l were synthesized by multistep reaction sequence and evaluated for antiproliferative activity against DLA cells by in vitro and in vivo studies. The results suggested that, compounds 8b with fluoro group and 8e with chloro substituent at the benzoyl ring of benzophenone scaffold as well as pyridine ring with hydroxy group exhibited significant activity. Further investigation in mouse model suggests that compounds 8b and 8e have the potency to activate caspase activated DNase (endonuclease) which is responsible for DNA fragmentation, a primary hallmark of apoptosis and thereby inhibits the Dalton’s lymphoma ascites tumour growth.
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Synthesis and tumor inhibitory activity of novel coumarin analogs targeting angiogenesis and apoptosis
European Journal of Medicinal Chemistry, 2014Co-Authors: B.r. Vijay Avin, V. Lakshmi Ranganatha, Aiyesha Firdouse, Prabhu Thirusangu, B.t. Prabhakar, Shaukath Ara KhanumAbstract:A sequence of coumarin analogs 5a-j was obtained by multi step synthesis from hydroxy Benzophenones (1a-j). The in vitro antiproliferative effect of the title compounds was tested against Ehrlich ascites carcinoma (EAC) and Daltons lymphoma ascites (DLA) cell lines. Among the series, compound 5c with bromo group in the benzophenone moiety was endowed with excellent antiproliferative potency with significant IC50 value. Further, in vivo antitumor effect of compound 5c against murine EAC and solid DL tumor model system was evident by the extended survivality. The tumor inhibitory mechanism of compound 5c was due to the antiangiogenesis and promotion of apoptosis. These results suggest possible applications of compound 5c which could be developed as a potent anticancer drug in the near future.
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design synthesis and anticancer properties of novel benzophenone conjugated coumarin analogs
Archiv Der Pharmazie, 2013Co-Authors: Lakshmi V Ranganatha, H.d. Gurupadaswamy, Farhan Zameer, S Meghashri, N D Rekha, V Girish, Shaukath Ara KhanumAbstract:In the current scenario, development of anticancer drugs with specific targets is of prime importance in modern chemical biology. Observing the importance of benzophenone and coumarin nucleus, it would be worthwhile to design and synthesize novel benzophenone derivatives (8a-o) bearing the coumarin nucleus. Further, they were screened for prospective anticancer activities in vitro against the Michigan Cancer Foundation-7 (MCF-7) and Ehrlich's ascites tumor (EAT) cell lines and their biomarkers, followed by in silico studies regarding phosphoinositide 3-kinase (PI3K) and caspase by molecular docking. Benzophenones have been reported as potential drugs targeting tumor angiogenesis; thus, the formation of neovessels in an in vivo model system like CAM, which is angiogenesis dependent, was observed in the presence of compounds 8a-o. The above findings would help in understanding their putative potential as therapeutic agents for cancer patients.
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Antiangiogenic effect of 2-benzoyl–phenoxy acetamide in EAT cell is mediated by HIF-1α and down regulation of VEGF of in-vivo
Investigational New Drugs, 2006Co-Authors: B.t. Prabhakar, Shaukath Ara Khanum, S Shashikanth, Bharathi P SalimathAbstract:Benzophenones and its analogues are known for wide range of biological properties. Synthetic benzophenone analogue 2-benzoyl -phenoxy acetamide (BP-1) is proven to be potent antitumor and proapoptotic activity against EAT cells in-vivo . In the present report, we studied the antiangiogenic effect of BP-1 in EAT cells induced angiogenesis. Treatment with BP-1 in-vivo was demonstrated by the down regulation of the secretion of VEGF from EAT cells and inhibition of blood vessels formation indicating the potential angioinhibitory effect of BP-1 in EAT cells. HIF-1α protein, a transcription factor known to be key a regulator in hypoxia-induced angiogenesis was also down regulated by BP-1. Our findings indicated that, HIF-1α nuclear sequestration is repressed by BP-1 through inhibition of nuclear translocation. We postulate that diminished HIF-1α nuclear presence and activity in BP-1 treated EAT cells could be responsible for decreased VEGF expression and antiangiogenic effects.
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anti tumor and proapoptotic effect of novel synthetic benzophenone analogues in ehrlich ascites tumor cells
Bioorganic & Medicinal Chemistry, 2006Co-Authors: B.t. Prabhakar, Shaukath Ara Khanum, K Jayashree, Bharathi P Salimath, S ShashikanthAbstract:Abstract A series of substituted benzophenone analogues, (2-aroyl-4-methylphenoxy)acetamides 4a–e, have been synthesized via three-step synthesis sequence beginning with the 2-hydroxyBenzophenones 1a–e in excellent yield. 1a–e on reaction with ethyl chloroacetate afford ethyl (2-aroyl-4-methylphenoxy)acetates 2a–e which on alkaline hydrolysis afforded (2-aroyl-4-methylphenoxy)ethanoic acid 3a–e. Compounds 3a–e on condensation with p-chloroaniline furnished benzophenone analogues 4a–e. In the present report, we investigated the anti-tumor and proapoptotic effect of Benzophenones in Ehrlich ascites tumor (EAT) cells. Treatment of Benzophenones in vivo resulted in inhibition of proliferation of EAT cells and ascites formation. Further, we demonstrate that the induction of apoptosis in EAT cells is mediated through activation of caspase-3. These results suggest a further possible clinical application of these synthetic compounds as potent anti-tumor and proapoptotic compounds.
Mariana F Fernandez - One of the best experts on this subject based on the ideXlab platform.
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determination of personal care products Benzophenones and parabens in human menstrual blood
Journal of Chromatography B, 2016Co-Authors: I Jimenezdiaz, L M Iribarneduran, Olga Ocon, E Salamanca, Mariana F Fernandez, Nicolas Olea, E BarrancoAbstract:Abstract Benzophenones and parabens are synthetic chemicals used in many personal care products, foods and pharmaceuticals. Benzophenones are used to protect the skin and materials from the adverse effects of UV-radiation, and parabens are used as preservatives. Despite their widespread occurrence and proven endocrine disrupting activity, relatively little is known about human exposure to these compounds. In the present work, an analytical method based on sample treatment using dispersive liquid-liquid microextraction (DLLME) for the extraction of six Benzophenones (benzophenone-1, −2, −3, −6, −8 and 4-hydroxybenzophenone) and four parabens (methyl-, ethyl-, propyl- and butyl- paraben) from human menstrual blood samples, followed by ultrahigh performance liquid chromatography-tandem mass spectrometry (UHPLC–MS/MS) analysis, is proposed and validated. The method was validated using matrix-matched standard calibration followed by a recovery assay with spiked samples. The limits of detection ranged from 0.1 to 0.3 ng mL −1 , with recoveries of 93.8% to 108.9%, and precision (evaluated as relative standard deviation) lower than 14% for all selected compounds. This method was successfully applied for the determination of the target compounds in 25 samples of human menstrual blood. Methylparaben and benzophenone-3 were the most frequently detected compounds (96%).
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urinary levels of bisphenol a Benzophenones and parabens in tunisian women a pilot study
Science of The Total Environment, 2016Co-Authors: I Jimenezdiaz, F Velasoria, Mariana F Fernandez, Francisco Artachocordon, H Belhassen, Juan P Arrebola, R Ghali, Abderrazek Hedhili, Nicolas OleaAbstract:Bisphenol A (BPA), Benzophenones and parabens are commonly used in the production of polycarbonate plastics, as UV-filters and as antimicrobial preservatives, respectively, and they are thought to exhibit endocrine disrupting properties. Exposure to these compounds remains poorly characterized in developing countries, despite the fact that certain behaviors related to westernization have the potential to influence exposure. The aim of this pilot study was to measure urinary concentrations of BPA, six different Benzophenones and four parabens in 34 Tunisian women. In addition, we identified some socio-demographic and dietary predictors of exposure to these compounds. Chemical analyses were carried out by dispersive liquid-liquid microextraction (DLLME) and ultra-high performance liquid chromatography with tandem mass spectrometry detection (UHPLC-MS/MS). Detection frequencies of methylparaben (MP), ethylparaben (EP) and propylparaben (PP) ranged between 67.6 and 94.1%. Butylparaben (BP) was found in 38.2% of the analyzed samples; BPA in 64.7%; and benzophenone-1 (BP-1) and benzophenone-3 (BP-3) were detected in 91.2 and 64.7% of the analyzed samples, respectively. Urinary geometric mean concentrations of MP, EP, PP, and BP were 30.1, 1.4, 2.0 and 0.5ngmL(-1), respectively. Geometric mean concentrations of BPA, BP-1, and BP-3 were 0.4, 1.3 and 1.1ngmL(-1), respectively. Our results suggest that Tunisian women are widely exposed to BPA, parabens and some Benzophenones. Further studies on the general Tunisian population are needed in order to assess the levels of exposure to these compounds and to identify sources of exposure and population groups at higher risk.
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determination of Benzophenones in human placental tissue samples by liquid chromatography tandem mass spectrometry
Talanta, 2011Co-Authors: F Velasoria, O Ballesteros, A Zafragomez, A Navalon, I Jimenezdiaz, Mariana F Fernandez, R Rodriguezgomez, J L Vilchez, Nicolas OleaAbstract:Benzophenones (BPs) are a family of compounds widely used to protect the skin and hair from UV irradiation. Despite human exposure to BPs through dermal application of products containing sunscreen agents and the increasing evidence that BPs are able to interfere with endocrine systems, few studies have examined the occurrence of BPs in humans. In this work, we propose a new liquid chromatography-tandem mass spectrometry (LC-MS/MS) method to determine six BPs, namely, benzophenone-1 (BP-1), benzophenone-2 (BP-2), benzophenone-3 (BP-3), benzophenone-6 (BP-6), benzophenone-8 (BP-8) and 4-hydroxybenzophenone (4-OH-BP) in human placental tissue samples. The method involves an extraction step of the analytes from the samples using ethyl acetate, followed by a clean-up step using centrifugation prior to their quantification by LC-MS/MS using an atmospheric pressure chemical ionization (APCI) interface in the positive mode. Benzophenone-d(10) (BP-d(10)) was used as surrogate. Found detection limits (LOD) ranged from 0.07 to 0.3 ng g(-1) and quantification limits (LOQ) from 0.3 to 1.0 ng g(-1), while inter- and intra-day variability was under 5%. The method was validated using standard addition calibration and a recovery assay. Recovery rates for spiked samples ranged from 98 to 104%. This method was satisfactorily applied for the determination of BPs in 16 placental tissue samples collected from women who live in Granada (Spain).
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a multiclass method for endocrine disrupting chemical residue analysis in human placental tissue samples by uhplc ms ms
Analytical Methods, 2011Co-Authors: F Velasoria, O Ballesteros, A Zafragomez, I Jimenezdiaz, Mariana F Fernandez, Nicolas Olea, R Rodriguezgomez, A NavalonAbstract:The group of compounds commonly called endocrine-disrupting chemicals covers a wide range of synthetic and natural substances able to alter the normal hormone function of wildlife and humans, consequently causing adverse health effects. Bisphenol A (BPA) and its chlorinated derivatives, Benzophenones (BPs) and parabens (PBs), belong to this group of compounds. In this work, we propose a multiclass ultra-high-performance liquid chromatography-tandem mass spectrometry (UHPLC–MS/MS) method to determine BPA, its four chlorinated derivatives (monochloro-, dichloro-, trichloro- and tetrachloro-bisphenol A), six BPs (benzophenone-1, benzophenone-2, benzophenone-3, benzophenone-6, benzophenone-8 and 4-hidroxybenzophenone) and four PBs (methylparaben, ethylparaben, propylparaben and butylparaben) in human placental tissue samples. The method involves an extraction step of the analytes from the samples using ethyl acetate, followed by a clean-up step by centrifugation prior to their quantification by UHPLC–MS/MS using an atmospheric pressure chemical ionization (APCI) interface in the negative mode. Deuterated bisphenol A (BPA-d16) was used as surrogate. The limits of detection (LOD) found ranged from 0.03 to 0.6 ng g−1, the limits of quantification (LOQ) from 0.1 to 1.4 ng g−1, while inter- and intra-day variability was under 8%. The method was validated using matrix-matched calibration standard and a spike recovery assay. Recovery rates for spiked samples ranged from 95% to 106%. This method was satisfactorily applied to the determination of these compounds in 50 placental tissue samples collected from women who live in the province of Granada (Spain).