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RSC Advances Apr 2023Phytochemicals have played a significant role in the discovery of many clinically anticancer medicines. being famous as an ornamental plant, widely cultivated, and...
Phytochemicals have played a significant role in the discovery of many clinically anticancer medicines. being famous as an ornamental plant, widely cultivated, and including a wide variety of secondary metabolites this motivated us to explore more about its potential medical applications. In this study, the total methanol extract of leaves (family Apocyanaceae) was sequentially fractionated into hexane, methylene chloride, ethyl acetate, and butanol fractions. The total phenolic content of the methanol extract of was determined spectrophotometrically and found to be 72.37 mg g, while the total flavonoid content was found to be 12.47 mg g. Fourteen polyphenolic compounds were detected by the HPLC analysis of the methanol extract, in addition to five phenolic compounds, which were isolated and identified for the first time from the EtOAc extract. They were identified as gallic acid (C1), chlorogenic acid (C2), -coumaric acid (C3), quercetin (C4), and rutin (C5). The structures were elucidated by NMR and EI/MS spectroscopic techniques. The cytotoxic activity of the methanol extract was evaluated by cell viability assay. The cytotoxicity results showed significant anticancer activity against human colon carcinoma HCT-116 with IC 39.3 μg mL and lesser activity against human lung carcinoma A-549 and human breast carcinoma MCF-7 cell lines with IC 93.4 and 110.3 μg mL, respectively.
PubMed: 37082370
DOI: 10.1039/d3ra00588g -
Beilstein Journal of Organic Chemistry 2023We have developed a catalytic aza-Nazarov reaction of -acyliminium salts generated in situ from the reaction of a variety of cyclic and acyclic imines with...
We have developed a catalytic aza-Nazarov reaction of -acyliminium salts generated in situ from the reaction of a variety of cyclic and acyclic imines with α,β-unsaturated acyl chlorides to afford substituted α-methylene-γ-lactam heterocycles. The reactions proceed effectively in the presence of catalytic (20 mol %) amounts of AgOTf as an anion exchange agent or hydrogen-bond donors such as squaramides and thioureas as anion-binding organocatalysts. The aza-Nazarov cyclization of 3,4-dihydroisoquinolines with α,β-unsaturated acyl chlorides gives tricyclic lactam products in up to 79% yield with full diastereocontrol (dr = >99:1). The use of acyclic imines in a similar catalytic aza-Nazarov reaction with 20 mol % of AgOTf results in the formation of α-methylene-γ-lactam heterocycles in up to 76% yield and with good to high diastereoselectivities (4.3:1 to 16:1). We have demonstrated the scalability of the reaction with a gram-scale example. The relative stereochemistry of the α-methylene-γ-lactam products has been determined via the single-crystal X-ray analysis of lactam . In order to shed light on the details of the reaction mechanism, we have performed carefully designed mechanistic studies which consist of experiments on the effect of β-silicon stabilization, the alkene geometry of the α,β-unsaturated acyl chloride reactants, and adventitious water on the success of the catalytic aza-Nazarov reaction.
PubMed: 36741815
DOI: 10.3762/bjoc.19.6 -
International Journal of Environmental... May 2023Dichloromethane (DCM) is recognized as a very harmful air pollutant because of its strong volatility and difficulty to degrade. Ionic liquids (ILs) are considered as...
Dichloromethane (DCM) is recognized as a very harmful air pollutant because of its strong volatility and difficulty to degrade. Ionic liquids (ILs) are considered as potential solvents for absorbing DCM, while it is still a challenge to develop ILs with high absorption performances. In this study, four carboxyl-functionalized ILs-trioctylmethylammonium acetate [N][Ac], trioctylmethylammonium formate [N][FA], trioctylmethylammonium glycinate [N][Gly], and trihexyl(tetradecyl)phosphonium glycinate [P][Gly]-were synthesized for DCM capture. The absorption capacity follows the order of [P][Gly] > [N][Gly] > [N][FA] > [N][Ac], and [P][Gly] showed the best absorption capacity, 130 mg DCM/g IL at 313.15 K and a DCM concentration of 6.1%, which was two times higher than the reported ILs [Beim][EtSO] and [Emim][Ac]. Moreover, the vapor-liquid equilibrium (VLE) of the DCM + IL binary system was experimentally measured. The NRTL (non-random two-liquid) model was developed to predict the VLE data, and a relative root mean square deviation (rRMSD) of 0.8467 was obtained. The absorption mechanism was explored via FT-IR spectra, H-NMR, and quantum chemistry calculations. It showed a nonpolar affinity between the cation and the DCM, while the interaction between the anion and the DCM was a hydrogen bond. Based on the results of the study of the interaction energy, it was found that the hydrogen bond between the anion and the DCM had the greatest influence on the absorption process.
Topics: Ionic Liquids; Methylene Chloride; Spectroscopy, Fourier Transform Infrared; Anions
PubMed: 37239516
DOI: 10.3390/ijerph20105787 -
Asian Pacific Journal of Cancer... Apr 2023Houttuynia cordata Thunb (HCT) is a medicinal herb used in Southeast Asia. Aim of this work: This study aimed at investigating the cytotoxicity of this plant extract and...
BACKGROUND
Houttuynia cordata Thunb (HCT) is a medicinal herb used in Southeast Asia. Aim of this work: This study aimed at investigating the cytotoxicity of this plant extract and fractions towards human breast cancer MDA-MB-231 and MCF-7 cells. HCT's phytoactive compounds are determined.
MATERIALS AND METHODS
Cell viability was determined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. The mode of cell death was measured by staining with annexin V-FITC and propidium iodide (PI) employing flow cytometry technique. The oxidative stress was measured by using 2',7'-dihydrodichlorofluorescein diacetate (DCFH-DA) and dihydroethidium (DHE+) fluorescent probes and using a fluorescence microplate reader. HCT phytochemicals were characterized by high performance liquid chromatography (HPLC).
RESULTS
The proliferation of MDA-MB-231 and MCF-7 cells was dramatically decreased by the crude extract and individual fraction of HCT. Ethyl acetate was the solvent fraction with the highest toxicity against MCF-7 cells, followed by dichloromethane, crude, and hexane fractions, respectively, whereas in MDA-MB231 cells, dichloromethane, crude, hexane, and ethyl acetate fractions each had the strongest impact, respectively. The methanol fraction had no effect on either cell line up to 200 μg/ml. The extract and fractions were less harmful to the NIH3T3 normal murine fibroblast cell line. The mode of both cell death was apoptosis evidenced by the increase of cell population stained with annexin V-FITC and PI. The fluorescence probes of both DCFH-DA and DHE in MDA-MB-231 cell line were enhanced. Phenolic acids included chlorogenic acid (CA), gallic acid (GA), transcoumaric acid (TCA), vanillic acid (VA), and syringic acid (SA), as well as flavonoids like quercetin and rutin, were identified as the active phytochemicals in the crude and fractions by using HPLC method.
CONCLUSION
MDA-MB-231cells underwent apoptosis via oxidative stress when induced with HCT hexane fraction. Phenolic acids and flavonoids were identified in HCT's extract and fractions.
Topics: Humans; Animals; Mice; Female; Breast Neoplasms; Houttuynia; Hexanes; Cell Line, Tumor; Methylene Chloride; NIH 3T3 Cells; Plant Extracts; Apoptosis; Flavonoids; Phytochemicals
PubMed: 37116149
DOI: 10.31557/APJCP.2023.24.4.1265 -
Anaesthesia Feb 2015
Topics: Chemistry, Physical; Drug Compounding; Methylene Blue; Phenylephrine; Sodium Chloride
PubMed: 25583189
DOI: 10.1111/anae.12983 -
Frontiers in Pharmacology 2021(TFG) is used as an antidiarrheal traditional medicine in Western Kenya. This study aimed to investigate the antidiarrheal activity of its aqueous extracts and the...
Aqueous Tuber Extracts of (Kotschy ex Schweinf.) Torre and Hillc. (Fabaceae). Possess Significant Antidiarrheal Activity and Spasmolytic Effect Possibly Mediated by Modulation of Nitrous Oxide System, Voltage-Gated Calcium Channels, and Muscarinic Receptors.
(TFG) is used as an antidiarrheal traditional medicine in Western Kenya. This study aimed to investigate the antidiarrheal activity of its aqueous extracts and the putative mechanism (s) of action using Sprague-Dawley rats and New Zealand white rabbits respectively. The antidiarrheal effects of the extract were evaluated in castor oil-induced diarrhea, the castor oil-induced enteropooling, and phenol red gastric motility tests. On the other hand, isolated rabbit's jejunal segments were used to evaluate the spasmolytic effect of TFG on spontaneous contraction, in acetylcholine-induced contraction, in presence of 80mMK, calcium chloride-induced contraction as well as in presence of the following antagonists: naloxone, methylene blue, L-NAME, prazosin, and propranolol in the studies. The data were express as Mean ± S.E.M and analyzed by one-way ANOVA and Tukey's post hoc test in cases of significance which was set at < 0.05. The extract was phytochemically characterized using Liquid chromatography Mass spectroscopy (LC-MS).The extract possessed significant inhibitory effect in the experiments. The extract exhibited significant spasmolytic effect on both spontaneous contraction and in jejunal segment pre-contracted acetylcholine as well as in presence of 80mMK solution. It also attenuated the spasmogenic effect of various concentration of calcium chloride. The extract's spasmolytic effect was, however, significantly attenuated in presence of several antagonists (methylene blue and L-NAME) but the adrenergic blockers (prazosin and propranolol) had no significant effect in the LC-MS identified thirty compounds where Proathocyanidin (11.54%), Syringic acid (7.30%), and 4-Hydroxybenzoic acid (6.19%) had the highest percentage abundance. In conclusion, the results obtained in this study partially validate the traditional uses of the tubers of this plant species as an antidiarrheal. These antidiarrheal effects are probably mediated via modulation of nitrous oxide pathway, voltage gated calcium channels, and muscarinic receptors.
PubMed: 33796023
DOI: 10.3389/fphar.2021.636879 -
MethodsX 2022A modified sol-gel method was developed for the synthesis of pure and transition-metal-doped titanium dioxide. The process involves the hydrolysis of titanium...
A modified sol-gel method was developed for the synthesis of pure and transition-metal-doped titanium dioxide. The process involves the hydrolysis of titanium tetraisopropoxide, which was used as a catalyst precursor, and molybdenum chloride, which was used as a doping agent. The shape and size of the final product were characterized by scanning electron microscopy, and the catalyst activity for the photocatalytic degradation of methylene blue in aqueous solutions was tested. The results indicate significant improvements in both the morphology and performance of the catalyst synthesized by the proposed method when compared to those obtained via the conventional approach using the same materials and quantities.•The main highlights of the proposed method are as follows.•Utilization of a double-jacketed cooling system to control and prevent temperature fluctuations during hydrolysis.•Ultrasonication during the reaction minimizes particle agglomeration during nanoparticle formation.•The use of two different alcohols and separation into two mixtures were experimentally demonstrated to delay gel formation, and hence, morphologically homogeneous catalyst nanoparticles were achieved.
PubMed: 35677843
DOI: 10.1016/j.mex.2022.101742 -
Plants (Basel, Switzerland) Mar 2022Cyanobacteria comprise a good natural resource of a potential variety of neuro-chemicals, including acetylcholinesterase inhibitors essential for Alzheimer's disease...
Cyanobacteria comprise a good natural resource of a potential variety of neuro-chemicals, including acetylcholinesterase inhibitors essential for Alzheimer's disease treatment. Accordingly, eight different cyanobacterial species were isolated, identified, and evaluated on their growth on different standard nutrient media. It was found that the modified medium supported the highest growth of the test cyanobacteria. The effects of methylene chloride/methanol crude extracts of the test cyanobacteria on acetylcholinesterase activity were examined and compared. (KU696637.1) crude extract recorded the highest acetylcholinesterase inhibition (62 ± 1.3%). medium chemical components were optimized through a Plackett-Burman factorial design. The biomass of increased significantly when grown on the optimized medium compared to that of control. The chemical analysis of the fractions derived from showed the presence of two compounds in significant amounts: the flavonoid 5,7-dihydroxy-2-phenyl-4H-chrome-4-one and the alkaloid 4-phenyl-2-(pyridin-3-yl) quinazoline. Molecular docking studies revealed that both compounds interact with the allosteric binding site of acetylcholinesterase at the periphery with π-π stackings with Tyr341 and Trp286 with good, predicted partition coefficient. The compounds obtained from this study open the door for promising drug candidates to treat Alzheimer's disease for their better pharmacodynamics and pharmacokinetic properties.
PubMed: 35336618
DOI: 10.3390/plants11060735 -
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 -
BMC Complementary and Alternative... Aug 2017Onchocerciasis is one of the tropical neglected diseases (NTDs) caused by the nematode Onchocerca volvulus. Control strategies currently in use rely on mass...
Phytochemical analysis and in vitro anthelmintic activity of Lophira lanceolata (Ochnaceae) on the bovine parasite Onchocerca ochengi and on drug resistant strains of the free-living nematode Caenorhabditis elegans.
BACKGROUND
Onchocerciasis is one of the tropical neglected diseases (NTDs) caused by the nematode Onchocerca volvulus. Control strategies currently in use rely on mass administration of ivermectin, which has marked activity against microfilariae. Furthermore, the development of resistance to ivermectin was observed. Since vaccine and safe macrofilaricidal treatment against onchocerciasis are still lacking, there is an urgent need to discover novel drugs. This study was undertaken to investigate the anthelmintic activity of Lophira lanceolata on the cattle parasite Onchocerca ochengi and the anthelmintic drug resistant strains of the free living nematode Caenorhabditis elegans and to determine the phytochemical profiles of the extracts and fractions of the plants.
METHODS
Plant was extracted in ethanol or methanol-methylene chloride. O. ochengi, C. elegans wild-type and C. elegans drug resistant strains were cultured in RPMI-1640 and NGM-agar respectively. Drugs diluted in dimethylsulphoxide/RPMI or M9-Buffer were added in assays and monitored at 48 h and 72 h. Worm viability was determined by using the MTT/formazan colorimetric method. Polyphenol, tannin and flavonoid contents were determined by dosage of gallic acid and rutin. Acute oral toxicity was evaluated using Swiss albino mice.
RESULTS
Ethanolic and methanolic-methylene chloride extracts killed O. ochengi with LC values of 9.76, 8.05, 6.39 μg/mL and 9.45, 7.95, 6.39 μg/mL respectively for leaves, trunk bark and root bark after 72 h. The lowest concentrations required to kill 50% of the wild-type of C. elegans were 1200 and 1890 μg/mL with ethanolic crude extract, 1000 and 2030 μg/mL with MeOH-CHCl for root bark and trunk bark of L. lanceolata, respectively after 72 h. Leave extracts of L. lanceolata are lethal to albendazole and ivermectin resistant strains of C. elegans after 72 h. Methanol/methylene chloride extracted more metabolites. Additionally, extracts could be considered relatively safe.
CONCLUSION
Ethanolic and methanolic-methylene chloride crude extracts and fractions of L. lanceolata showed in vitro anthelmintic activity. The extracts and fractions contained polyphenols, tannins, flavonoids and saponins. The mechanism of action of this plant could be different from that of albendazole and ivermectin. These results confirm the use of L. lanceolata by traditional healers for the treatment of worm infections.
Topics: Albendazole; Animals; Anthelmintics; Caenorhabditis elegans; Cattle; Drug Resistance; Flavonoids; Ivermectin; Mice; Nematode Infections; Ochnaceae; Onchocerca; Onchocerciasis; Phytotherapy; Plant Bark; Plant Extracts; Plant Roots; Plant Stems; Polyphenols; Saponins; Tannins
PubMed: 28806951
DOI: 10.1186/s12906-017-1904-z