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ACS Omega May 2022A high internal phase emulsion (HIPE) method was used to produce adsorbents with an interconnected porous structure. HIPE was prepared using vinyl benzyl chloride (VBC),...
A high internal phase emulsion (HIPE) method was used to produce adsorbents with an interconnected porous structure. HIPE was prepared using vinyl benzyl chloride (VBC), divinylbenzene (DVB), -butyl acrylate, and Span80 as the organic phase and water with KSO and CaCl as the water phase. The polymerization of the organic phase produced highly porous polymers called polyHIPE, carrying two functional groups. As a result of the template method, polyHIPEs have a low surface area. To overcome this drawback, polyHIPE was hyper-cross-linked through VBC to create meso- and micropores, resulting in a higher surface area. Then the polymer surface was tailored with carboxylic acid groups by simple hydrolysis of -butyl acrylate. The adsorption performances of the acidic functional hyper-cross-linked polyHIPEs prepared for the various reaction times of 0, 15, and 60 min were compared for methylene blue. The hyper-cross-linked polyHIPEs showed an enhanced adsorption kinetics for methylene blue, and the 15 min hyper-cross-linking reaction increased the rate of methylene blue adsorption significantly. It was proven that the polyHIPE adsorbent can be reused by treating it with an aqueous acidic solution in ethanol.
PubMed: 35571856
DOI: 10.1021/acsomega.2c01472 -
Regulatory Toxicology and Pharmacology... Mar 2021Dichloromethane (DCM) is a high production volume chemical (>1000 t/a) mainly used as an industrial solvent. Carcinogenicity studies in rats, mice and hamsters have... (Review)
Review
Dichloromethane (DCM) is a high production volume chemical (>1000 t/a) mainly used as an industrial solvent. Carcinogenicity studies in rats, mice and hamsters have demonstrated a malignant tumor inducing potential of DCM only in the mouse (lung and liver) at 1000-4000 ppm whereas human data do not support a conclusion of cancer risk. Based on this, DCM has been classified as a cat. 2 carcinogen. Dose-dependent toxicokinetics of DCM suggest that DCM is a threshold carcinogen in mice, initiating carcinogenicity via the low affinity/high capacity GSTT1 pathway; a biotransformation pathway that becomes relevant only at high exposure concentrations. Rats and hamsters have very low activities of this DCM-metabolizing GST and humans have even lower activities of this enzyme. Based on the induction of specific tumors selectively in the mouse, the dose- and species-specific toxicokinetics in this species, and the absence of a malignant tumor response by DCM in rats and hamsters having a closer relationship to DCM toxicokinetics in humans and thus being a more relevant animal model, the current classification of DCM as human carcinogen cat. 2 remains appropriate.
Topics: Administration, Inhalation; Animals; Biotransformation; Carcinogens; Cricetinae; Disease Models, Animal; Dose-Response Relationship, Drug; Drug Evaluation, Preclinical; Humans; Methylene Chloride; Mice; Rats; Species Specificity
PubMed: 33387565
DOI: 10.1016/j.yrtph.2020.104858 -
Iranian Journal of Basic Medical... 2024The newest virus from the SARS family of viruses called acute syndrome-coronavirus-2 (SARS-CoV-2), which causes COVID-19 disease, was identified in China at the end of... (Review)
Review
The newest virus from the SARS family of viruses called acute syndrome-coronavirus-2 (SARS-CoV-2), which causes COVID-19 disease, was identified in China at the end of 2019. In March 2020, after it spread to 29 additional countries, it was declared a pandemic by the World Health Organization (WHO). SARS-CoV-2 infection mainly starts through the respiratory tract and causes a wide spectrum of symptoms from asymptomatic infections to acute respiratory distress syndrome with multi-organ failure and vasoplegic shock. Among the many immunomodulatory and antiviral drugs that have been studied for the treatment of COVID-19, methylene blue (MB) may play an influential role. This article reviews the history of MB applications, the antiviral effects of MB against SARS-CoV-2, and the results of and studies of the use of MB in COVID-19. Based on studies, MB can simultaneously affect most of the host's harmful responses caused by SARS-CoV-2 infection due to its multiple properties, including anti-hypoxemia, anti-oxidant, immune system modulator, and antiviral. The use of MB is associated with a reduction in the possibility of getting infection, and mortality, and can be used as a safe, effective, cheap, and available treatment option with minimal side effects for the clinical management of COVID-19.
PubMed: 38800024
DOI: 10.22038/IJBMS.2024.71871.15617 -
Biomedicine & Pharmacotherapy =... Nov 2023Clivia miniata (Lindl) is a member of the family Amaryllidaceae known for its chemically diverse alkaloids with a wide range of biological activities. Many reports...
Clivia miniata (Lindl) is a member of the family Amaryllidaceae known for its chemically diverse alkaloids with a wide range of biological activities. Many reports revealed a direct role of oxidative stress in the early stage of Alzheimer's disease (AD). Meanwhile, β-site amyloid precursor protein cleavage enzyme 1 (BACE-1) is a molecular target for the treatment of AD. We aimed to investigate C. miniata root, bulb, and aerial part chemical profiling, antioxidant, BACE-1, and AChE enzyme inhibitory activities. Results showed that the total root had the most potent radical scavenging activity as compared to the total bulb and aerial part, respectively. Ethanol root extract had the most potent BACE-1 inhibitory activity (IC = 0.02 ± 0.001 µg/mL) as compared to the bulb and aerial part (IC = 0.93 ± 0.13, 1.80 ± 0.24 µg/mL), respectively. Moreover, the total root extract mitigated AChE enzyme activity more than total bulb and aerial fractions with IC values of (0.06 ± 0.02, 0.58 ± 0.3, and 1.89 ± 0.42 µg/mL, respectively. Bioassay-guided acid-base fractionation confirmed superior BACE-1 inhibitory activity of the root fractions particularly, methylene chloride and ethyl acetate fractions with (IC values of 0.21 ± 0.60 and 0.01 ± 0.001 µg/mL), respectively. UPLC-MS analysis of ethyl acetate and methylene chloride fractions of C. miniata root led to the identification of eight phenolics and thirteen alkaloids, respectively. Molecular docking studies against BACE-1 protein revealed that lycorine di-hexoside, miniatine, and cliviaaline were the most promising hits. Further investigation of anti-AD potential of the aforementioned small molecules is required.
Topics: Antioxidants; Molecular Docking Simulation; Chromatography, Liquid; Methylene Chloride; Tandem Mass Spectrometry; Alkaloids; Plant Extracts; Alzheimer Disease; Plant Components, Aerial; Amaryllidaceae; Cholinesterase Inhibitors
PubMed: 37778271
DOI: 10.1016/j.biopha.2023.115382 -
Journal of Traditional Chinese Medicine... Aug 2022To evaluate Sterculia diversifolia stem bark and leaves for phytotoxic, genotoxic and enzymes inhibition potential.
OBJECTIVE
To evaluate Sterculia diversifolia stem bark and leaves for phytotoxic, genotoxic and enzymes inhibition potential.
METHODS
Phytotoxic activity of both stem bark and leaves were screened using Lemna minor. The genotoxic activity of Sterculia diversifolia stem bark and leaves extracts were tested using comet assay protocol while enzyme inhibition activity of crude extract and various fractions of both stem bark and leaves were evaluated using acetyl cholinesterase, lipoxygenase, β-glu-curonidase, urease, xanthine oxidase and carbonic anhydrase.
RESULTS
Phytotoxic activity showed significant results in dose dependant manner in both stem bark (ethyl acetate and n-butanol) and leaves (ethyl acetate, n-butanol and n-hexane) fractions. In genotoxic activity, dichloromethane fraction showed significant activity followed by ethyl acetate fraction. Acetyl cholinesterease inhibitory activity showed significant results in both stem bark and leaves fractions, while significant lipoxygenase inhibition was shown by ethyl acetate, dichloromethane, crude extract and n-hexane fractions of both stem bark and leaves. β-glucuronidase, urease and carbonic anhydrase inhibitory activity showed highly significant results in ethyl acetate fraction of both stem bark and leaves, while xanthine oxidase inhibition was shown by dichloromethane fraction of stem bark and leaves extracts.
CONCLUSIONS
This study emphasizes the important phytotoxic, genotoxic and enzyme inhibition effects of Sterculia diversifolia stem bark and leaves. Hence, it is clear that Sterculia diversifolia stem bark and leaves possess phytotoxic, genotoxic and enzyme inhibitory agents.
Topics: 1-Butanol; Alkaloids; Carbonic Anhydrases; DNA Damage; Humans; Lipoxygenases; Methylene Chloride; Plant Bark; Plant Extracts; Plant Leaves; Urease; Xanthine Oxidase
PubMed: 35848976
DOI: 10.19852/j.cnki.jtcm.2022.04.005 -
Molecules (Basel, Switzerland) Sep 2022Lam (syn. .) leaves are globally acclaimed for their nutritional content and mitigation of malnutrition. In most impoverished rural communities including Limpopo,...
Lam (syn. .) leaves are globally acclaimed for their nutritional content and mitigation of malnutrition. In most impoverished rural communities including Limpopo, Mpumalanga and KwaZulu Natal of South Africa, powdered leaves of are applied as a nutritional supplement for readily available food such as porridge for malnourished children and even breast-feeding mothers. Widely practiced and admired is also the use of the plant seed in the do-it-yourself purification of water by rural South Africans. This study aimed at identifying the chemical and nutritional marker compounds present in South African seed oils using high resolution 1-2-dimension gas chromatography in order to give scientific validation to its uses in cosmetics and particularly in culinary practices. Results obtained from two-dimension tandem mass spectrometry chemical signature revealed over 250 compounds, five times more than those reported from one-dimension gas chromatography. Whereas previous reports from gas chromatography-mass spectrometry analysis reported oleic acid (70-78%) as the major compound from oil samples from other countries, seed oil from South Africa is marked by 13-octadeaconic acid with 78.62% and 41.9% as the predominant monounsaturated fatty acid in the hexane and dichloromethane extracts respectively. This was followed by vaccenic acid, an isomer of oleic acid at 51% in the acetone extract, 9-octadecanoic acid-(z)-methyl ester at 39.18%, 21.34% and 10.06% in dichloromethane, hexane and acetone extracts respectively. However, a principal component analysis with R = 0.98 of the two-dimension tandem mass spectrometry cum chemometric analysis indicated n-hexadecanoic acid, oleic acid, 9-octadecanoic acid-(z)-methyl ester and -vaccenic acid with a probability of 0.96, 0.88, 0.80 and 0.79 respectively as the marker compounds that should be used for the quality control of seed oils from South Africa. This study demonstrates that South African oils contain C-18 monounsaturated fatty acids similar to oils from Egypt (76.2%), Thailand (71.6%) and Pakistan (78.5%) just to mention but a few. These fatty acids are sunflower and olive oil type-compounds and therefore place seed oil for consideration as a cooking oil amongst its other uses.
Topics: Acetone; Child; Esters; Fatty Acids; Gas Chromatography-Mass Spectrometry; Hexanes; Humans; Methylene Chloride; Moringa; Moringa oleifera; Oleic Acid; Olive Oil; Palmitic Acid; Plant Extracts; Plant Oils; Seeds; South Africa; Stearic Acids; Water
PubMed: 36144484
DOI: 10.3390/molecules27185749 -
Tetrahedron Chem Dec 2022The emergence and rapid spread of coronavirus disease 2019 (COVID-19), a potentially fatal disease, caused by severe acute respiratory syndrome coronavirus-2...
The emergence and rapid spread of coronavirus disease 2019 (COVID-19), a potentially fatal disease, caused by severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2), has swiftly led to public health crisis worldwide. Hence vaccines and antiviral therapeutics are an important part of the healthcare response to combat the ongoing threat by COVID-19. Here, we report an efficient synthesis of nirmatrelvir (PF-07321332), an orally active SARS-CoV-2 main protease inhibitor.
PubMed: 36276807
DOI: 10.1016/j.tchem.2022.100033 -
International Journal of Molecular... May 2021The synthesis of new phenothiazine derivatives, analogs of Methylene Blue, is of particular interest in the design of new drugs, as well as in the development of a new...
The synthesis of new phenothiazine derivatives, analogs of Methylene Blue, is of particular interest in the design of new drugs, as well as in the development of a new generation of agents for photodynamic therapy. In this study, two new derivatives of phenothiazine, i.e., 3,7-bis(4-aminophenylamino)phenothiazin-5-ium chloride dihydrochloride () and 3,7-bis(4-sulfophenylamino)phenothiazin-5-ium chloride (), are synthesized for the first time and characterized by NMR, IR spectroscopy, HRMS and elemental analysis. The interaction of the obtained compounds and with salmon sperm DNA is investigated. It is shown by UV-Vis spectroscopy and DFT calculations that substituents in arylamine fragments play a crucial role in dimer formation and interaction with DNA. In the case of , two amine groups promote H-aggregate formation and DNA interactions through groove binding and intercalation. In the case of , sulfanilic acid fragments prevent any dimer formation and DNA binding due to electrostatic repulsion. DNA interaction mechanisms are studied and confirmed by UV-vis and fluorescence spectroscopy in comparison with Methylene Blue. The obtained results open significant opportunities for the development of new drugs and photodynamic agents.
Topics: Amines; DNA; Dimerization; Intercalating Agents; Magnetic Resonance Spectroscopy; Methylene Blue; Models, Molecular; Molecular Conformation; Molecular Structure; Spectrometry, Fluorescence; Structure-Activity Relationship
PubMed: 34072560
DOI: 10.3390/ijms22115847 -
Current Problems in Pediatric and... Nov 2014In the past decade, the number of epidemiological publications addressing environmental chemical exposures and autism has grown tremendously. These studies are important... (Review)
Review
In the past decade, the number of epidemiological publications addressing environmental chemical exposures and autism has grown tremendously. These studies are important because it is now understood that environmental factors play a larger role in causing autism than previously thought and because they address modifiable risk factors that may open up avenues for the primary prevention of the disability associated with autism. In this review, we covered studies of autism and estimates of exposure to tobacco, air pollutants, volatile organic compounds and solvents, metals (from air, occupation, diet, dental amalgams, and thimerosal-containing vaccines), pesticides, and organic endocrine-disrupting compounds such as flame retardants, non-stick chemicals, phthalates, and bisphenol A. We included studies that had individual-level data on autism, exposure measures pertaining to pregnancy or the 1st year of life, valid comparison groups, control for confounders, and adequate sample sizes. Despite the inherent error in the measurement of many of these environmental exposures, which is likely to attenuate observed associations, some environmental exposures showed associations with autism, especially traffic-related air pollutants, some metals, and several pesticides, with suggestive trends for some volatile organic compounds (e.g., methylene chloride, trichloroethylene, and styrene) and phthalates. Whether any of these play a causal role requires further study. Given the limited scope of these publications, other environmental chemicals cannot be ruled out, but have not yet been adequately studied. Future research that addresses these and additional environmental chemicals, including their most common routes of exposures, with accurate exposure measurement pertaining to several developmental windows, is essential to guide efforts for the prevention of the neurodevelopmental damage that manifests in autism symptoms.
Topics: Child Development Disorders, Pervasive; Environmental Pollutants; Female; Humans; Maternal Exposure; Metals, Heavy; Pesticides; Pregnancy; Prenatal Exposure Delayed Effects; Risk Factors; Nicotiana; Vaccination
PubMed: 25199954
DOI: 10.1016/j.cppeds.2014.06.001