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Tropical Biomedicine Dec 2023Much of the new research and investigation in pharmacy sciences are concerned with developing therapeutic agents, and identifying and finding new drugs with their...
Much of the new research and investigation in pharmacy sciences are concerned with developing therapeutic agents, and identifying and finding new drugs with their chemical structure to treat different human diseases such as infectious diseases from natural products. Therefore, the present findings relate to isolating five new compounds the dichloromethane extract of Peperomia blanda (Jacq.) Kunth grown on Socotra Island, Yemen. two new secolignans; which have been proposed as peperomin I & J. These compounds were isolated together with the other two polyketides presented as surinone D and dindygulerione F. The chemical structures were elucidated and confirmed with nuclear magnetic resonance (NMR) and liquid chromatography-mass spectroscopy (LCMS) analysis. These compounds were first isolated and reported from this plant. These new compounds' antimicrobial activity has been evaluated, and minimum inhibitory concentration has been recorded in the range of 125-250 µg/mL. The pharmacotherapeutic spectrum of compounds was predicated using PASS software which showed potential activity.
Topics: Humans; Peperomia; Methylene Chloride; Polyketides; Plant Extracts; Biological Products
PubMed: 38308837
DOI: 10.47665/tb.40.4.015 -
The Journal of Neuroscience : the... Feb 2024Magnetic fields are being used for detailed anatomical and functional examination of the human brain. In addition, evidence for their efficacy in treatment of brain...
Magnetic fields are being used for detailed anatomical and functional examination of the human brain. In addition, evidence for their efficacy in treatment of brain dysfunctions is accumulating. Transcranial static magnetic field stimulation (tSMS) is a recently developed technique for noninvasively modifying brain functions. In tSMS, a strong and small magnet when placed over the skull can temporarily suppress brain functions. Its modulatory effects persist beyond the time of stimulation. However, the neurophysiological mechanisms underlying tSMS-induced plasticity remain unclear. Here, using acute motor cortical slice preparation obtained from male C57BL/6N mice, we show that tSMS alters the intrinsic electrical properties of neurons by altering the activity of chloride (Cl) channels in neurons. Exposure of mouse pyramidal neurons to a static magnetic field (SMF) at a strength similar to human tSMS temporarily decreased their excitability and induced transient neuronal swelling. The effects of SMF were blocked by DIDS and GlyH-101, but not by NPPB, consistent with the pharmacological profile of SLC26A11, a transporter protein with Cl channel activity. Whole-cell voltage-clamp recordings of the GlyH-101-sensitive Cl current component showed significant enhancement of the component at both subthreshold and depolarized membrane potentials after SMF application, resulting in shunting inhibition and reduced repetitive action potential (AP) firing at the respective potentials. Thus, this study provides the first neurophysiological evidence for the inhibitory effect of tSMS on neuronal activity and advances our mechanistic understanding of noninvasive human neuromodulation.
Topics: Male; Humans; Animals; Mice; Chlorides; Mice, Inbred C57BL; Magnetic Fields; Transcranial Magnetic Stimulation; Glycine; Hydrazines
PubMed: 38302440
DOI: 10.1523/JNEUROSCI.1324-22.2024 -
Analytical Chemistry Feb 2024Ion mobility spectrometry (IMS) is a reliable and sensitive technique for the detection and analysis of compounds at the trace level. Depending on the chemical...
Ion mobility spectrometry (IMS) is a reliable and sensitive technique for the detection and analysis of compounds at the trace level. Depending on the chemical composition of the sample, compounds may be positively or negatively charged to form different polarity ions and detected in positive or negative polarity of the electric field. In order to detect multiple threats simultaneously with miniaturized devices, using a single detection unit to achieve high resolving power and high sensitivity is important. In this work, a miniaturized drift tube with fast polarity switching capabilities integrated with Fourier deconvolution multiplexing techniques is proposed for the first time as a means to improve the performance of ion mobility spectrometry. The sensitivity and resolving power are improved compared to traditional polarity switching signal averaging data acquisition methods. The displayed device had a high resolving power up to 52 at a drift length of 41 mm and a drift tube voltage of 2 kV. Trinitrotoluene (TNT), methamphetamine (MA), benzene, toluene, methyl -butyl ether (MTBE), acetic acid, and methylene chloride were evaluated using the proposed fast polarity switching multiplexing spectrometer and exhibited satisfied performance.
PubMed: 38289229
DOI: 10.1021/acs.analchem.3c04087 -
BMC Chemistry Jan 2024Bromhexine (BR), guaiafenesin (GUF) and salbutamol (SAL) are formulated as Ventocough syrup® (with and without sugar), labeled to contain propyl paraben and sodium...
Bromhexine (BR), guaiafenesin (GUF) and salbutamol (SAL) are formulated as Ventocough syrup® (with and without sugar), labeled to contain propyl paraben and sodium benzoate as inactive ingredients. They are used to make coughing more productive and easier. A crucial element and a major issue in the pharmaceutical industry is the control of organic related impurities to obtain safe and effective treatment. Guaiacol (GUL) is reported to be GUF related impurity that was proved to be extremely toxic (toxic rating class 5), and its use should be banned. In this work, In-Silico study and ADMET estimation were conducted to predict GUL pharmacokinetic properties and its toxicity profile. Additionally, two chromatographic methods were conducted to analyze the studied components along with GUF impurity in the presence of the labeled dosage form excipients. The In-Silico study assured that GUL has oral rat acute toxicity and it is considered to be skin sensitizer. On the other hand, the developed TLC- densitometeric method depended on using a mobile phase mixture of hexane: methylene chloride: triethylamine (5.0:6.0:0.3, by volume) as a developing system. UV-Scanning was performed immediately at 275 nm for SAL, GUF and GUL, while scanning at 310 nm was used for scanning BR. Linearity was established in the ranges of 0.25-4.0, 0.25-4.0, 0.5-8.0 and 0.1-1.6 µg/band for BR, SAL, GUF and GUL, respectively. In the developed HPLC method, separation was performed on X-Bridge® C column (250 × 4.6 mm, 5 μm) using a solvent mixture of 0.05M disodium hydrogen phosphate pH 3 with aqueous phosphoric acid: methanol (containing 0.3%, v/v triethylamine) (40:60, v/v). Detection was done at 225 nm and separation was achieved within 10 min. Linearity was proved in the range of 2-50 µg/mL for the proposed drugs. Validation of the developed methods was done and all the calculated parameters were within the acceptable limits recommended by ICH guidelines. After that, methods were used to examine the potency of the selected marketed dosage forms and concentrations of all drugs were within the acceptable limits. Additionally, complete separation between the studied drugs and the additives were observed. The developed methods can be used during routine quality control analysis of the proposed drugs when the required issues concern on sensitivity, selectivity and analysis time.
PubMed: 38281055
DOI: 10.1186/s13065-024-01122-5 -
International Journal of Biological... Mar 2024In the present work, UiO-66/xanthan gum/alginate bionanocomposite adsorbent was fabricated using the in-situ crosslinking-gelation method, characterized by different...
Development of a novel bionanocomposite of UiO-66/xanthan gum/alginate crosslinked by calcium chloride for azo dye removal: Insight into adsorption kinetics, isotherms, and thermodynamics.
In the present work, UiO-66/xanthan gum/alginate bionanocomposite adsorbent was fabricated using the in-situ crosslinking-gelation method, characterized by different techniques, and finally used for the removal of methylene blue dye from aqueous solution. Adsorption studies were performed using batch experiments and the influencing operational parameters such as contact time, initial pH solution, temperature, initial dye concentration, adsorbent dose, pH, swelling, regeneration, and reuse of the adsorbent were investigated. The various kinetic models (pseudo-first-order, pseudo-second-order, Elovich, and intraparticle diffusion) and isotherm models (Langmuir, Freundlich, Temkin, and Dubinin-Radushkevich) were used to analysis of the experiment results. The results were best fitted to the pseudo-second-order kinetic and Langmuir isotherm models. The maximum adsorption capacity of dye on the adsorbent was obtained at 9.96 mg/g at pH = 11. The value of pH for the adsorbent was obtained at about 8. According to thermodynamic parameters, the dye adsorption was found as spontaneous and endothermic due to the negative value of the ΔG° and ΔH°. After 4 times of reusability cycles, the adsorption efficiency remained above 86 %, which represented a certain regeneration ability. As a result, this research indicates that UiO-66/xanthan gum/alginate bionanocomposite can be utilized as a promising bio-adsorbent for azo dye removal from contaminated wastewater.
Topics: Azo Compounds; Calcium Chloride; Adsorption; Alginates; Water Pollutants, Chemical; Thermodynamics; Indicators and Reagents; Kinetics; Hydrogen-Ion Concentration; Metal-Organic Frameworks; Phthalic Acids; Polysaccharides, Bacterial
PubMed: 38278391
DOI: 10.1016/j.ijbiomac.2024.129729 -
Viruses Dec 2023Coronaviruses (CoVs) belong to the group of enveloped positive-sense single-strand RNA viruses and are causative agents of respiratory, gastro-intestinal, and central...
Coronaviruses (CoVs) belong to the group of enveloped positive-sense single-strand RNA viruses and are causative agents of respiratory, gastro-intestinal, and central nervous systems diseases in many host species, i.e., birds, mammals, and humans. Beta-CoVs revealed a great potential to cross the barrier between species by causing three epidemics/pandemics among humans in the 21st century. Considering the urgent need for powerful antiviral agents for decontamination, prevention, and treatment of BCoV infections, we turned our attention to the possibility of photodynamic inactivation with photosensitizers in combination with light irradiation. In the present study, we evaluated, for the first time, the antiviral activity of toluidine blue O (TBO) against Beta-coronavirus 1 (BCoV) in comparison to methylene blue (MB). First, we determined the in vitro cytotoxicity of MB and TBO on the Madin-Darby bovine kidney (MDBK) cell line with ISO10993-5/Annex C. Thereafter, BCoV was propagated in MDBK cells, and the virus titer was measured with digital droplet PCR, TCID assay and plaque assay. The antiviral activity of non-toxic concentrations of TBO was estimated using the direct inactivation approach. All effects were calculated in MAPLE 15 mathematical software by developing programs for non-linear modeling and response surface analysis. The median inhibitory concentration () of TBO after 72 h of incubation in MDBK cells was 0.85 µM. The antiviral activity of TBO after the direct inactivation of BCoV ( = 1) was significantly stronger than that of MB. The median effective concentration (EC) of TBO was 0.005 µM. The cytopathic effect decreased in a concentration-dependent manner, from 0.0025 to 0.01 µM, and disappeared fully at concentrations between 0.02 and 0.3 µM of TBO. The number of virus particles also decreased, depending on the concentration applied, as proven by ddPCR analysis. In conclusion, TBO exhibits significant potential for direct inactivation of BCoV in vitro, with a very high selectivity index, and should be subjected to further investigation, aiming at its application in veterinary and/or human medical practice.
Topics: Humans; Cattle; Animals; Coronavirus, Bovine; Photosensitizing Agents; Tolonium Chloride; Coronavirus; Coronavirus Infections; Methylene Blue; Pandemics; Antiviral Agents; Mammals
PubMed: 38257748
DOI: 10.3390/v16010048 -
Chemistry & Biodiversity Mar 2024Felicia abyssinica L., family Asteraceae, is widely used in folk medicine. This represents the first study to investigate its phytoconstituents and pharmacological...
Felicia abyssinica L., family Asteraceae, is widely used in folk medicine. This represents the first study to investigate its phytoconstituents and pharmacological effects. Phytoconstituents identified by GC-MS, LC-ESI-MS/MS-based metabolomics, and NMR (1D & 2D). GC-MS of the (FAMEs) revealed mainly the identification of 55 fatty acids. LC-ESI-MS/MS analysis resulted in the tentative identity of 13 compounds representing flavonoids, phenolics, and fatty acids. Ethyl acetate fraction exhibited the highest total flavonoids 66.19 mg/mL Rutin equivalent, while the methanolic fraction showed the highest phenolics 87.70 mg/mL gallic acid equivalent, and the total condensed tannins were 64.35 μg CE/mg catechins equivalent. A flavonoid and a cinnamic acid derivative were identified as quercetin 3-O-(2'''-O-acetyl) rutinoside (Mumikotin A) (1) and Methyl sinapate (2). Biological evaluation of antioxidant and cytotoxic activities was carried out. Cytotoxicity was examined on HepG-2 cell lines where the average cell viability was 91.42 % and 52.48 % for concentrations 10 and 100 μg/mL respectively. Methylene chloride and methanolic fractions showed the highest antioxidant activity 225 μg/mL Ascorbic acid equivalents. It is hypothesized that high phenolics, flavonoid content, and oxygenated identified compounds contribute to the antioxidant activity and can be regarded as a promising species for nutraceuticals active antioxidants with potential value for remedy.
Topics: Gas Chromatography-Mass Spectrometry; Antioxidants; Tandem Mass Spectrometry; Plant Extracts; Flavonoids; Phenols; Asteraceae; Methanol; Plant Components, Aerial; Fatty Acids
PubMed: 38244212
DOI: 10.1002/cbdv.202301347 -
European Review For Medical and... Jan 2024The aim of the study was to assess the disinfection efficacy, bond integrity, and nano hardness of caries-affected dentin (CAD) surface bonded to resin cement when...
Disinfection by methylthionine chloride and chitosan in combination with Photo radiation therapy on caries affected dentin nano hardness, adhesive integrity, and bond failure.
OBJECTIVE
The aim of the study was to assess the disinfection efficacy, bond integrity, and nano hardness of caries-affected dentin (CAD) surface bonded to resin cement when disinfected with chlorhexidine (CHX), Methylene blue activated by Photodynamic therapy (MB-PDT), chitosan, silver diamine fluoride (SDF), chitosan activated by PDT, and SDF-diode laser against S. mutans.
MATERIALS AND METHODS
A total of 60 human mandibular molars were extracted non-traumatically and gathered using ICDAS criteria. The dentin surface was prepared, leaving CAD to receive a disinfection procedure. After inoculation with S. mutans, the CAD samples were divided into six groups and disinfected with various disinfectants (n = 10) CHX, MB-PDT, chitosan, chitosan-PDT, SDF, and SDF+ diode laser. Survival rates of S. mutans were analyzed following the restoration of samples with resin cement via the etch and rinse method to assess SBS. Also, nano hardness was analyzed. Statistical analysis was performed by using the ANOVA and the Tukey multiple test (p<0.05). The Kruskal-Wallis test was used to evaluate the change in survival rate.
RESULTS
Related to the survival rates, the SDF+ diode laser displayed the highest reduction in S. mutans levels and chitosan presented the lowest level of disinfection. The intergroup comparison revealed that CHX and chitosan-PDT displayed comparable outcomes of S. mutans survival rate to that of SDF+ diode laser (p>0.05). Likewise, MB-PDT and SDF displayed a comparable survival rate of S. mutans to Chitosan disinfection (p>0.05). Considering SBS and nano hardness, the highest SBS and NH were exhibited by the SDF+ diode laser, and the lowest SBS and NH values were exhibited by MB-PDT. The intragroup comparison revealed that CAD specimens disinfected with Chitosan-PDT showed comparable SBS and NH values to the SDF+ diode laser (p>0.05). CHX, chitosan, and SDF exhibited bond values and NH comparable to MB-PDT (p<0.05).
CONCLUSIONS
Synergistic use of Silver diamine fluoride with diode laser and chitosan activated by PDT can be used as an alternative to CHX for controlling S. mutans growth, promoting enhanced bond efficacy and nano hardness for bonding resin cement to the caries-affected dentin.
Topics: Humans; Methylene Blue; Dentin; Disinfection; Chitosan; Adhesives; Resin Cements; Dental Caries Susceptibility; Chlorhexidine; Photochemotherapy; Materials Testing; Photosensitizing Agents; Quaternary Ammonium Compounds; Fluorides, Topical; Silver Compounds
PubMed: 38235896
DOI: 10.26355/eurrev_202401_34889 -
Cureus Jan 2024Introduction Ultrasound-guided fascial plane blocks are nowadays the gold standard technique for regional anesthesia and postoperative analgesia. Despite their high...
Introduction Ultrasound-guided fascial plane blocks are nowadays the gold standard technique for regional anesthesia and postoperative analgesia. Despite their high success rate, cases of partial or total failure of this method have been reported. This experimental study aims to address the corresponding ultrasound signs and their association with fascial plane block efficacy. Methods After capturing the appropriate sonographic image that included muscle layers and their fasciae, an 18-gauge epidural needle penetrated the cadaveric porcine tissue and was forwarded until the tip of the needle reached the target fascial plane. The infusion of methylthioninium chloride or methylene blue dye was performed, causing tissue hydro dissection. The documentation of the generated ultrasound images was followed by surgical exposure of the tip of the needle. Results The distribution of the dye into the plane of interest (double-edge sign) was equivalent to block success, whereas the single-edge sign (accumulation of the dye between fascia and epimysium) indicated total block failure. The intermediate-edge sign, a combination of the previous ultrasound signs, is related to partial failure of block performance. Conclusion The identification of the three novel sonographic signs is an accurate predictive factor of peripheral nerve block efficacy. The respective data are expected to aid the rapid improvement of interfascial plane block accuracy and techniques, leading to their more effective execution and simultaneously eliminating the failure rates. Thereby, the amelioration of intra and postoperative analgesia will be accomplished, expediting the patient's hospital discharge and reducing or even avoiding opioid consumption.
PubMed: 38205088
DOI: 10.7759/cureus.51858 -
Molecules (Basel, Switzerland) Dec 2023Cannabis is considered ( L.) a sacred herb in many countries and is vastly employed in traditional medicine to remedy numerous diseases, such as diabetes. This research...
Cannabis is considered ( L.) a sacred herb in many countries and is vastly employed in traditional medicine to remedy numerous diseases, such as diabetes. This research investigates the chemical composition of the aqueous extracts from L. seeds. Furthermore, the impact of these extracts on pancreatic α-amylase and lipase, and intestinal α-glucosidase enzymes is evaluated, as well as their antihyperglycemic effect. Analysis of the chemical composition of the aqueous extract was conducted using high-performance liquid chromatography with a photodiode array detector (HPLC-DAD). In contrast, the ethanol, hexanic, dichloromethane, and aqueous extract compositions have been established. Additionally, the inhibitory effects of ethanolic, dichloromethane, and aqueous extracts on pancreatic α-amylase and lipase, and intestinal α-glucosidase activities were evaluated in vitro and in vivo. The results of HPLC analysis indicate that the most abundant phenolic compound in the aqueous cannabis seed extract is 3-hydroxycinnamic acid, followed by 4-hydroxybenzoic acid and rutin acid. Moreover, administration of ethanolic and aqueous extracts at a dose of 150 mg/Kg significantly suppressed postprandial hyperglycemia compared to the control group; the ethanolic, dichloromethane, and aqueous extracts significantly inhibit pancreatic α-amylase and lipase, and intestinal α-glucosidase in vitro. The pancreatic α-amylase test exhibited an inhibition with values of 16.36 ± 1.24 µg/mL, 19.33 ± 1.40 µg/mL, 23.53 ± 1.70 µg/mL, and 17.06 ± 9.91 µg/mL for EAq, EDm, EET, and EHx, respectively. EET has the highest inhibitory capacity for intestinal α-glucosidase activity, with an of 32.23 ± 3.26 µg/mL. The extracts inhibit porcine pancreatic lipase activity, demonstrating their potential as lipase inhibitors. Specifically, at a concentration of 1 mg/mL, the highest inhibition rate (77%) was observed for EDm. To confirm these results, the inhibitory effect of these extracts on enzymes was tested in vivo. The oral intake of aqueous extract markedly reduced starch- and sucrose-induced hyperglycemia in healthy rats. Administration of the ethanolic extract at a specific dose of 150 mg/kg significantly reduced postprandial glycemia compared with the control group. It is, therefore, undeniable that cannabis extracts represent a promising option as a potentially effective treatment for type 2 diabetes.
Topics: Animals; Rats; Swine; Hypoglycemic Agents; Cannabis; Pancreatic alpha-Amylases; alpha-Glucosidases; Diabetes Mellitus, Type 2; Methylene Chloride; Lipase; Hallucinogens; Hyperglycemia; Cannabinoid Receptor Agonists; Ethanol; Plant Extracts
PubMed: 38202676
DOI: 10.3390/molecules29010093