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1.
Molecules ; 29(8)2024 Apr 19.
Article in English | MEDLINE | ID: mdl-38675696

ABSTRACT

The present study aimed to evaluate the leishmanicidal potential of the essential oil (EO) of Micromeria (M.) nervosa and to investigate its molecular mechanism of action by qPCR. Furthermore, in silicointeraction study of the major M. nervosa EO compounds with the enzyme cytochrome P450 sterol 14α-demethylase (CYP51) was also performed. M. nervosa EO was analyzed by gas chromatography-mass spectrometry (GC-MS). Results showed that α-pinene (26.44%), t-cadinol (26.27%), caryophyllene Oxide (7.73 ± 1.04%), and α-Cadinene (3.79 ± 0.12%) are the major compounds of M. nervosa EO. However, limited antioxidant activity was observed, as this EO was ineffective in neutralizing DPPH free radicals and in inhibiting ß-carotene bleaching. Interestingly, it displayed effective leishmanicidal potential against promastigote (IC50 of 6.79 and 5.25 µg/mL) and amastigote (IC50 of 8.04 and 7.32 µg/mL) forms of leishmania (L.) infantum and L. major, respectively. Molecular mechanism investigation showed that M. nervosa EO displayed potent inhibition on the thiol regulatory pathway. Furthermore, a docking study of the main components of the EO with cytochrome P450 sterol 14α-demethylase (CYP51) enzyme revealed that t-cadinol exhibited the best binding energy values (-7.5 kcal/mol), followed by α-cadinene (-7.3 kcal/mol) and caryophyllene oxide (-7 kcal/mol). These values were notably higher than that of the conventional drug fluconazole showing weaker binding energy (-6.9 kcal/mol). These results suggest that M. nervosa EO could serve as a potent and promising candidate for the development of alternative antileishmanial agent in the treatment of leishmaniasis.


Subject(s)
Antiprotozoal Agents , Molecular Docking Simulation , Oils, Volatile , Oils, Volatile/pharmacology , Oils, Volatile/chemistry , Antiprotozoal Agents/pharmacology , Antiprotozoal Agents/chemistry , Antioxidants/pharmacology , Antioxidants/chemistry , Gas Chromatography-Mass Spectrometry , Sterol 14-Demethylase/metabolism , Sterol 14-Demethylase/chemistry , Computer Simulation , Leishmania/drug effects , Leishmania/enzymology , Bicyclic Monoterpenes/pharmacology , Bicyclic Monoterpenes/chemistry
2.
J Microbiol ; 61(11): 993-1011, 2023 Nov.
Article in English | MEDLINE | ID: mdl-38048022

ABSTRACT

Listeria monocytogenes is an important food-borne pathogen that causes listeriosis and has a high case fatality rate despite its low incidence. Medicinal plants and their secondary metabolites have been identified as potential antibacterial substances, serving as replacements for synthetic chemical compounds. The present studies emphasize two significant medicinal plants, Allium cepa and Zingiber officinale, and their efficacy against L. monocytogenes. Firstly, a bacterial isolate was obtained from milk and identified through morphology and biochemical reactions. The species of the isolate were further confirmed through 16S rRNA analysis. Furthermore, polar solvents such as methanol and ethanol were used for the extraction of secondary metabolites from A. cepa and Z. officinale. Crude phytochemical components were identified using phytochemical tests, FTIR, and GC-MS. Moreover, the antibacterial activity of the crude extract and its various concentrations were tested against L. monocytogenes. Among all, A. cepa in methanolic extracts showed significant inhibitory activity. Since, the A. cepa for methanolic crude extract was used to perform autography to assess its bactericidal activity. Subsequently, molecular docking was performed to determine the specific compound inhibition. The docking results revealed that four compounds displayed strong binding affinity with the virulence factor Listeriolysin-O of L. monocytogenes. Based on the above results, it can be concluded that the medicinal plant A. cepa has potential antibacterial effects against L. monocytogenes, particularly targeting its virulence.


Subject(s)
Anti-Infective Agents , Listeria monocytogenes , Plants, Medicinal , Zingiber officinale , Animals , Onions , Milk/microbiology , RNA, Ribosomal, 16S/genetics , Molecular Docking Simulation , Anti-Infective Agents/pharmacology , Anti-Bacterial Agents/pharmacology , Plant Extracts/pharmacology , Phytochemicals/pharmacology
3.
PLoS One ; 18(11): e0293682, 2023.
Article in English | MEDLINE | ID: mdl-37943844

ABSTRACT

One of the most prevalent chronic conditions affecting older men is benign prostatic hyperplasia (BPH), causing severe annoyance and embarrassment to patients. The pathogenesis of BPH has been connected to epithelial proliferation, inflammation, deranged redox balance, and apoptosis. Diacerein (DIA), the anthraquinone derivative, is a non-steroidal anti-inflammatory drug. This study intended to investigate the ameliorative effect of DIA on the prostatic histology in testosterone-induced BPH in rats. BPH was experimentally induced by daily subcutaneous injection of testosterone propionate for four weeks. The treated group received DIA daily for a further two weeks after induction of BPH. Rats' body and prostate weights, serum-free testosterone, dihydrotestosterone, and PSA were evaluated. Prostatic tissue was processed for measuring redox balance and histopathological examination. The BPH group had increased body and prostate weights, serum testosterone, dihydrotestosterone, PSA, and oxidative stress. Histologically, there were marked acinar epithelial and stromal hyperplasia, inflammatory infiltrates, and increased collagen deposition. An immunohistochemical study showed an increase in the inflammatory TNF-α and the proliferative PCNA markers. Treatment with DIA markedly decreased the prostate weight and plasma hormones, improved tissue redox balance, repaired the histological changes, and increased the proapoptotic caspase 3 expression besides the substantial reduction in TNF-α and PCNA expression. In conclusion, our study underscored DIA's potential to alleviate the prostatic hyperplastic and inflammatory changes in BPH through its antioxidant, anti-inflammatory, antiproliferative, and apoptosis-inducing effects, rendering it an effective, innovative treatment for BPH.


Subject(s)
Prostatic Hyperplasia , Testosterone , Animals , Male , Rats , Anti-Inflammatory Agents/pharmacology , Apoptosis , Dihydrotestosterone , Oxidation-Reduction , Plant Extracts/pharmacology , Proliferating Cell Nuclear Antigen/metabolism , Prostate-Specific Antigen , Prostatic Hyperplasia/chemically induced , Prostatic Hyperplasia/drug therapy , Rats, Sprague-Dawley , Tumor Necrosis Factor-alpha/metabolism
4.
Pak J Pharm Sci ; 36(2(Special)): 673-679, 2023 Mar.
Article in English | MEDLINE | ID: mdl-37548208

ABSTRACT

Aqueous methanol extracts of Sarcococca saligna leaves and roots were used in this work to explore its phytochemical contents, antioxidant, enzyme inhibition and antibacterial activities. Total phenolic contents were found to be in higher concentrations then total flavonoids contents in aqueous methanolic extracts of leaves. Antioxidant activity was performed using DPPH radical scavenging assay. In our findings both leaves and roots extracts were found to show substantial antioxidant potential. Aqueous methanolic extracts of both the leaves and roots gave significant inhibition against butyryl cholinesterase whereas against acetyl cholinesterase extracts of roots gave significant inhibition. The results were compared with the standard drug Eserine. The aqueous methanolic extract of leaves, roots and crude saponins isolated from leaf extracts gave moderate to significant antibacterial activity against the tested bacterial strains using agar disc diffusion method. According to the conclusions, S. saligna possesses significant antioxidant, enzyme inhibition, and antibacterial activities. Hence it is assumed that S. saligna has the potential to be used in the discovery and development of new bioactive compounds.


Subject(s)
Antioxidants , Plant Extracts , Plant Extracts/pharmacology , Plant Extracts/chemistry , Cholinesterases , Anti-Bacterial Agents , Phytochemicals/pharmacology , Flavonoids/chemistry
5.
Pak J Pharm Sci ; 36(2(Special)): 699-706, 2023 Mar.
Article in English | MEDLINE | ID: mdl-37548211

ABSTRACT

The emergence of multidrug-resistant ESKAPE infections has emerged as a serious public health threat. Nosocomial infections are most often caused by ESKAPE bacteria. To combat multidrug-resistant ESKAPE, the research team used Valeriana Wallichii extracts and nanoparticles. The well diffusion technique was used to test antimicrobial activity on Muller Hinton agar medium. The FTIR, SEM and XRD techniques were used to characterize the nanoparticles synthesized in an environmentally benign manner. Both NPs performed better than extracts made with methanol and water in this investigation. The smallest zones of inhibition were shown against A. baumannii and Enterobacter cloacae, whereas the largest zones of inhibition were seen against E. faecium. However, NPs synthesized from shoot extracts exhibited remarkable effects against all MDR ESKAPE infections, with zones of inhibition of 23, 20, 12, 18, 22 and 14mm, respectively. Although E. faecium. had the largest inhibitory zone in both methanolic root and shoot extracts (19mm and 22mm, respectively), K. pneumonia and E. cloacae had the smallest zones when tested with these solvents. Water-based extracts inactivated multidrug-resistant bacteria. Our research show that extracts and nanoparticles have stronger antibacterial efficiency because biologically active substances including Terpenoids, Alkaloids, Phenol and Pholobutannins affect people and microbe.


Subject(s)
Alkaloids , Valerian , Humans , Anti-Bacterial Agents/pharmacology , Bacteria , Enterobacter cloacae
6.
Pak J Pharm Sci ; 36(3(Special)): 941-946, 2023 May.
Article in English | MEDLINE | ID: mdl-37587702

ABSTRACT

The current research investigation demonstrated that the aqueous leaves extract of Rosamarinus officinalis possesses cardinal phyto-chemicals to fabricate AgNPs in an eco-friendly way. The phyto-synthesized AgNPs were characterized to be stable, monodispersed, polycrystalline and mostly spheroidal in conformation. The nano-spheriods were observed to be 25-75 nm in diameter, displaying λmax peak at 430 nm. From the comparative antimicrobial investigations, it was observed that AgNPs manifested tremendous bactericidal properties against all test organisms particularly S. epidermis (89%), S. aureus (84%) and K. pneumonia (84%), owing least MIC values of 40µL. The aced fungicidal activity was also exhibited by AgNPs against all fungal test species particularly C. herbarum (90%), A. flavus (85%), R. stolonifer (85%) and C. jadinii (85%). In contrast to AgNPs, all crude ethanolic, aqueous, methanolic and n-hexanoic extracts manifested less to moderate antimicrobial activity against all test micro-organisms with three-fold escalating MIC values i.e., 160µL.


Subject(s)
Anti-Infective Agents , Metal Nanoparticles , Silver/pharmacology , Staphylococcus aureus , Anti-Infective Agents/pharmacology , Plant Leaves , Plant Extracts/pharmacology
7.
Front Nutr ; 9: 850730, 2022.
Article in English | MEDLINE | ID: mdl-35634399

ABSTRACT

This study aimed to examine the effect of canning and storage on physicochemical, mineral, and antioxidant properties and phenolic composition of apricot wholes, halves, and pulp. The findings for physicochemical properties revealed that the total soluble solids, titratable acidity, total sugars, and ascorbic acid were found higher in apricot pulp (37.15, 1.39, and 20.74% and 7.21 mg/100 g FW, respectively) followed by apricot wholes and halves throughout the storage period. The remarkable contents of potassium, phosphorous, zinc, copper, iron, and manganese were found in the apricot pulp which revealed that canning and storage slightly affected the mineral composition. Bioactive substances were identified and quantified by reversed-phase high-performance liquid chromatography, which indicated a higher presence of chlorogenic acid (34.45 mg/kg FW), quercitin-3-glucoside (16.78 mg/kg FW), neochlorogenic acid (26.52 mg/kg FW), gallic acid (5.37 mg/kg FW), kaempferol (14.22 mg/kg FW), ellagic acid (6.02 mg/kg FW), procyanidin B2 (8.80 mg/kg FW), and epicatechin (9.87 mg/kg FW) in apricot pulp followed by apricot wholes and halves throughout the storage period. The total phenolic content was found highest in apricot pulp (13.76 GAE mg/100 g FW) followed by wholes (8.09 GAE mg/100 g FW) and halves (6.48 GAE mg/100 g FW) which decreased significantly throughout the storage period. Antioxidant properties were assessed by DPPH, ABTS+, MCA, and BCBA, which were found higher in the apricot pulp (92.23 TEAC µg/g DW, 92.33 TEAC µg/g DW, 33.80 TEAC µg/g DW, and 68.40 TEAC µg/g DW, respectively) that is correlated with the higher presence of bioactive compounds. Thus, apricot pulp containing excellent sources of nutrients, minerals, phytochemicals, and antioxidant components could be used for consumption purposes that provide nutraceuticals and antioxidants globally.

8.
Proc Natl Acad Sci U S A ; 119(20): e2122660119, 2022 05 17.
Article in English | MEDLINE | ID: mdl-35561226

ABSTRACT

The transcriptome represents an attractive but underused set of targets for small-molecule ligands. Here, we devise a technology that leverages fragment-based screening and SHAPE-MaP RNA structure probing to discover small-molecule fragments that bind an RNA structure of interest. We identified fragments and cooperatively binding fragment pairs that bind to the thiamine pyrophosphate (TPP) riboswitch with millimolar to micromolar affinities. We then used structure-activity relationship information to efficiently design a linked-fragment ligand, with no resemblance to the native ligand, with high ligand efficiency and druglikeness, that binds to the TPP thiM riboswitch with high nanomolar affinity and that modulates RNA conformation during cotranscriptional folding. Principles from this work are broadly applicable, leveraging cooperativity and multisite binding, for developing high-quality ligands for diverse RNA targets.


Subject(s)
RNA Folding , Riboswitch , Small Molecule Libraries , Base Pairing , Ligands , Small Molecule Libraries/chemistry , Structure-Activity Relationship , Thiamine Pyrophosphate/chemistry , Transcription, Genetic
9.
Plants (Basel) ; 11(6)2022 Mar 08.
Article in English | MEDLINE | ID: mdl-35336596

ABSTRACT

The genus Salsola L. (Russian thistle, Saltwort) includes halophyte plants and is considered one of the largest genera in the family Amaranthaceae. The genus involves annual semi-dwarf to dwarf shrubs and woody tree. The genus Salsola is frequently overlooked, and few people are aware of its significance. The majority of studies focus on pollen morphology and species identification. Salsola has had little research on its phytochemical makeup or biological effects. Therefore, we present this review to cover all aspects of genus Salsola, including taxonomy, distribution, differences in the chemical constituents and representative examples of isolated compounds produced by various species of genus Salsola and in relation to their several reported biological activities for use in folk medicine worldwide.

10.
Environ Res ; 210: 112883, 2022 07.
Article in English | MEDLINE | ID: mdl-35123973

ABSTRACT

Selective and sensitive optical sensor based on surface plasmon resonance for detection of various heavy metals in water using polyvinylpyrolidone modified silver nanoparticles was explained in this present study. The prepared nanoparticles were characterized by UV-visible spectroscopy (UV-vis), Fourier transform infrared spectroscopy (FTIR) and Transmission electron microscopy (TEM). UV-visible spectra show the surface plasmon resonance (SPR) peak at 409 nm corresponding to silver nanoparticles. Crystalline nature of the nanoparticles was evident from TEM images and XRD analysis. TEM images showed average size of 10 nm for prepared silver nanoparticles. FTIR analysis provides the presence of various functional groups responsible for the reduction and stability of the prepared silver nanoparticles. SERS gives the molecular orientation of the adsorbed pyridine molecules via its nitrogen lone pair of electrons on the surface of silver. Prepared polyvinylpyrolidone modified silver nanoparticles (AgNPs) are demonstrated to detect the concentration of heavy metal contaminant Fe3+ ions in water based on linear change in surface plasmon resonance absorption strength. In addition, AgNPs showed promising activity towards E.coli. These observed optical properties suggest the possible utilization of prepared nanoparticles in the application of water purification.


Subject(s)
Metal Nanoparticles , Silver , Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/pharmacology , Escherichia coli , Metal Nanoparticles/chemistry , Microbial Sensitivity Tests , Silver/chemistry , Spectroscopy, Fourier Transform Infrared , Water
11.
Environ Res ; 208: 112723, 2022 05 15.
Article in English | MEDLINE | ID: mdl-35063434

ABSTRACT

Diclofenac is an anti-inflammatory drug and has been frequently detected from the wastewater. In the present study, factors affecting diclofenac adsorption on sewage sludge was evaluated. At 1 mg/L initial diclofenac concentration, more than 80% diclofenac removal was achieved. Adsorption increased at higher concentration (100 mg/L concentration) and more than 99% diclofenac was adsorbed from the wastewater. Significant removal of diclofenac was observed after 5 min contact time. The adsorption efficacy was more than 98% after 50 and 60 min. Pseudo-first and second order kinetics revealed reasonable regression value (0.9) indicated that the model is best fitted. Diclofenac adsorption was extremely high at acidic pHs than alkaline range. The sludge samples showed the presence of multi drug resistant bacteria. Vancomycin-resistant enterococcus stains were 27%, Methicillin-resistant Staphylococcus aureus positive strains were 16.5% and Extended-spectrum betal-lactamase-harbouring Enterobacteriacea were 65.4% in the sludge. The drug resistance Enterobacteriaceae revealed 14 Klebsiella pneumonia strains, 11 strains from E. coli and two from the genus Enterobacter. To conclude, the activated sludge could be effectively utilized for the removal of diclofenac from wastewater.


Subject(s)
Methicillin-Resistant Staphylococcus aureus , Water Pollutants, Chemical , Adsorption , Diclofenac , Escherichia coli , Sewage/microbiology , Wastewater/analysis , Water Pollutants, Chemical/analysis
12.
Environ Res ; 205: 112553, 2022 04 01.
Article in English | MEDLINE | ID: mdl-34902381

ABSTRACT

The indiscriminate application of various pesticides leads to toxicity to the humans, animals, fishes and threatens the environment and ecosystem. The present study was aimed to investigate pesticide degrading bacteria from the pesticide contaminated sample and to localize organophophate hydrolase activity from the bacteria. Sediment sample was selected as the source of microorganism for the degradation of chlorpyrifos. Enterobacter aerogenes CP2 and Streptococcus pyogenes CP11 isolated from the contaminated sample removed 77 ± 1.8%, 74.2 ± 3.1 chlorpyrifos. These strains have the potential to utilize pesticide as the source of carbon and energy. The pesticides inoculated with both CP 2 and CP 11 enhanced biodegradation of chlorpyrifos at optimized condition. E. aerogenes CP2 and S. pyogenes CP11 produced organophosphate hydrolase activity and localized enzyme biosynthesis. Organophosphate hydrolase activity was high in intracellular, followed by outer membrane and extracellular sample for both bacteria. The treated wastewater has no impact on the seed germination indicated normal cell division, cell elongation and indole-3 acetic acid synthesis. The strain CP2 has the rapid rate of organophosphate degradation among Enterobacter species.


Subject(s)
Chlorpyrifos , Pesticides , Animals , Biodegradation, Environmental , Chlorpyrifos/metabolism , Ecosystem , Pesticides/metabolism , Wastewater , Water
13.
Lasers Med Sci ; 35(4): 807-812, 2020 Jun.
Article in English | MEDLINE | ID: mdl-31463818

ABSTRACT

Asthma affects children related to trace elements. Our aim was to investigate the levels of trace elements using laser-induced breakdown spectroscopy (LIBS). The study included 120 children aged 4-12 years from both sexes. They were divided into three groups: Group 1 of 40 children was diagnosed as cases of controlled asthma. Group 2 consisted of 40 children diagnosed as cases of uncontrolled asthma. Group 3 consisted of 40 children as normal control. Asthmatic children were classified according to GINA 2015. They were analyzed for serum levels of total IgE, eosinophil count, and trace metals (Zn, Cu, Pb, Mg, and Fe) by using LIBS. There was significant decrease in serum levels of Zn, Mg and Fe in children with asthma than in normal children. There was a significant decrease in uncontrolled asthmatic children than in controlled asthmatic children. But the Cu and Pb concentration in children with asthma was significantly higher than that in normal children, and there was a significant increase in uncontrolled asthmatic children than in controlled asthmatic children. Furthermore, we examined the peak flow meter, eosinophil count, and total IgE and found that the peak flow metric study had shown a significant difference in controlled cases, total eosinophil count, and IgE; the difference was more significant in the uncontrolled group than in the controlled group, and the total levels were higher in the uncontrolled group. Asthma is a common pediatric disease that is related to deficiency of Fe, Zn, and Mg and occurs with increased Pb and Cu. LIBS is a safe and rapid technique that helps in detecting asthma.


Subject(s)
Asthma/diagnosis , Lasers , Spectrum Analysis/methods , Asthma/blood , Body Height , Body Weight , Child , Child, Preschool , Eosinophils , Female , Humans , Male , Trace Elements/analysis
14.
Iran J Pharm Res ; 16(Suppl): 46-57, 2017.
Article in English | MEDLINE | ID: mdl-29844775

ABSTRACT

Passiflora species were known by their anticonvulsant, anxiolytic and sedative activities. The aim of this study was to investigate the chemical composition of the most active leaf extract of Passiflora caerulea L. grown in Egypt. The ethanolic extract of the leaves exhibited higher activity than aqueous extract as anticonvulsant (63% potency relative to carbamazepine), analgesic (70% potency relative to indomethacin), antioxidant (71% potency relative to vitamin E), anti-inflammatory (90% potency relative to indomethacin) and antipyretic (90% potency relative to paracetamol). Fractions obtained successively from the ethanolic extract were then subjected to the same biological testing demonstrating that the ethyl acetate fraction was the most active in all activities (50, 96, 80, 63 % potency relative to reference standards used in each of the selected activity, respectively) followed by n-butanol then n-hexane and chloroform fractions. Purification of the anticonvulsant sub-fractions obtained by column chromatography of ethyl acetate fraction, led to the isolation of three compounds that were identified by physical and spectroscopic techniques as Lucenin II (1), 4-hydroxycinnamic acid (2) and Chrysin 6-C-ß-D-glucoside (3). The amount of Chrysin 6-C-ß-D-glucoside was found to be 0.0184 g % w/w of the dried leaves using HPLC method that showed linearity (R2 = 0.9996) over the range 0.015-0.25 mg/mL. C-glycosyl flavones and hydroxycinnamic acid derivatives may thus be the responsible principles for the biological activity of the plant under investigation. Moreover, RAPD technique was performed for the genetic characterization and authentication of the plant, where 106 fragments were recorded after DNA amplification with fifteen primers.

15.
Mar Drugs ; 14(8)2016 Aug 18.
Article in English | MEDLINE | ID: mdl-27548191

ABSTRACT

As a part of our continuing work to find out bioactive lead molecules from marine invertebrates, the CHCl3 fraction of the organic extract of the Red Sea sponge Theonella mirabilis showed cytotoxic activity in our primary screen. Bioassay-guided purification of the active fractions of the sponge's extract resulted in the isolation of two new glycerides, mirabolides A and B (1 and 2), together with the reported 4-methylene sterols, conicasterol (3) and swinhosterol B (4). The structures of the compounds were assigned by interpretation of their 1D (¹H, (13)C), 2D (COSY, HSQC, HMBC, ROESY) NMR spectral data and high-resolution mass determinations. Compounds 1-4 displayed marked cytotoxic activity against human breast adenocarcinoma cell line (MCF-7) with IC50 values of 16.4, 5.18, 6.23 and 3.0 µg/mL, respectively, compared to 5.4 µg/mL observed by doxorubicin as reference drug.


Subject(s)
Antibiotics, Antineoplastic/pharmacology , Glycerides/pharmacology , Theonella/chemistry , Animals , Antibiotics, Antineoplastic/chemistry , Antibiotics, Antineoplastic/isolation & purification , Cholesterol/analogs & derivatives , Cholesterol/isolation & purification , Cholesterol/pharmacology , Doxorubicin/pharmacology , Female , Glycerides/chemistry , Glycerides/isolation & purification , Humans , Indian Ocean , Inhibitory Concentration 50 , MCF-7 Cells , Molecular Structure , Nuclear Magnetic Resonance, Biomolecular
16.
Z Naturforsch C J Biosci ; 71(11-12): 375-380, 2016 Nov 01.
Article in English | MEDLINE | ID: mdl-27206319

ABSTRACT

Phytochemical investigation of the semi-parasitic plant, Plicosepalus curviflorus (Loranthaceae) growing in Saudi Arabia resulted in the isolation of a new catechin-gallic acid derivative of inositol, plicosepalin A (1) [(+) catechin-4'-O-(1″-O-galloyl-5″-O-methyl)-myo-inositol], along with seven known compounds: methyl gallate (2), catechin (3), quercetin (4), gallic acid (5), lupeol (6), ß-sitosterol (7), and ursolic acid (8). Their structures were elucidated on the basis of spectroscopic analyses, including HRESIMS, ESIMS, 1H and 13C NMR, HSQC, and HMBC, as well as comparison with reported data. The antioxidant and antimicrobial activities of 1 were evaluated using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and the disc diffusion assay, respectively. Compound 1 exhibited potent free radical scavenging activity with an IC50 value of 9.0 ± 0.27 µM. Moreover, significant activities against Staphylococcus aureus and Bacillus subtilis were recorded.


Subject(s)
Antioxidants/isolation & purification , Catechin/analogs & derivatives , Catechin/chemistry , Gallic Acid/chemistry , Inositol/analogs & derivatives , Inositol/chemistry , Loranthaceae/chemistry , Antioxidants/chemistry , Antioxidants/pharmacology , Catechin/isolation & purification , Catechin/pharmacology , Inositol/isolation & purification , Inositol/pharmacology
17.
Z Naturforsch C J Biosci ; 71(5-6): 141-54, 2016.
Article in English | MEDLINE | ID: mdl-27096779

ABSTRACT

Ethanolic and aqueous leaf extracts of Ficus cyathistipula significantly reduced blood-glucose level, improved triglycerides and cholesterol levels of dyslipidemia in diabetic-rats. They similarly reduced the inflammation of paw-edema and stomach-ulcers in rats. Fractions obtained by successive partition of ethanolic extract were assessed for their cytotoxicity, antioxidant and antimicrobial activities; Petroleum ether fraction was the most cytotoxic (IC(50) = 4.43 ± 0.2, 17.3 ± 2.22 and 15.5 ± 3.67 µg/ml on MCF7, HepG2 and HeLa cell lines, respectively). Ethyl acetate fraction was the strongest antioxidant in DPPH assay (IC(50) = 100 µg/ml). All samples exhibited low to strong antimicrobial activity. Chemical investigation of leaf extracts led to the isolation of α-amyrin palmitate (1), lupeol acetate (2), taraxerol (3), ß-sitosterol (4), protocatechuic acid (5) and 3-O-caffeoyl quinic acid (6) that were identified via spectral and chromatographic analyses. Metabolite profiling was performed via UPLC-PDA-MS and revealed the presence of flavonoid glycosides, phenolic acids, isoflavones, coumarins and fatty acids. Quantitative determination revealed 593 ± 0.5 mg BSE, 348.1 ± 0.09 mg GAE, 238.7 ± 0.5 mg rutin and 9 ± 0.5 g tannins per 100 g d.wt. of leaves. GLC analysis of lipid fraction revealed identification of phytosterols (15.6%), saturated (51.71%) and unsaturated (41.9%) fatty acids. Galactose, glucose, arabinose and glucoronic acid (36.98%, 28.86%, 22.56% and 1.06%, respectively) were identified by HPLC analysis of mucilage-hydrolysate.


Subject(s)
Anti-Infective Agents , Anti-Inflammatory Agents , Ficus/chemistry , Hypoglycemic Agents , Plant Extracts , Plant Leaves/chemistry , Animals , Anti-Infective Agents/chemistry , Anti-Infective Agents/pharmacology , Anti-Inflammatory Agents/chemistry , Anti-Inflammatory Agents/pharmacology , HeLa Cells , Hep G2 Cells , Humans , Hypoglycemic Agents/chemistry , Hypoglycemic Agents/pharmacokinetics , Hypoglycemic Agents/pharmacology , MCF-7 Cells , Male , Plant Extracts/chemistry , Plant Extracts/pharmacology , Rats , Rats, Wistar
18.
Pak J Pharm Sci ; 28(6): 2061-74, 2015 Nov.
Article in English | MEDLINE | ID: mdl-26639479

ABSTRACT

Medicago sativa L. (Alfalfa) is traditionally used to treat diabetes. This study was designed to investigate the potential antihyperlipidemic and antihyperglycemic activity of M. sativa sprouts in streptozotocin (STZ) induced diabetes via i.p. injection of 55 mg/kg of STZ. Experimental animals were divided into the following groups: GP1 (normal), GP2 (STZ-hyperlipidemic), GP3 (rouvastatin), GP4 (metformin), GP 5-9 (diabetic treated with methanolic, petroleum ether, chloroform, ethyl acetate and butanol extracts). The administration of the total methanolic extract (500 mg/kg), the petroleum ether (32.5mg) and butanol fractions (60 mg) for 4 weeks significantly decreased (p<0.05) triglycerides (TG), total cholesterol (TC), low-density lipoproteins (LDL) and very low density lipoproteins (VLDL) in comparison to rouvastatin. Petroleum ether fraction proved to exhibit the best activity as antihyperlipidemic agent (12.23%). On the other hand, ethyl acetate fraction retained the best activity (vs. metformin) as antihyperglycemic agent. Histopathological evidences on liver, pancreas and spleen were in agreement with the above mentioned results. Purification, characterization, and identification of isolated compounds from the active fractions afforded 9 compounds: ß-sitosterol and stigmasterol from the petroleum ether fraction; 10-hydroxy-coumestrol, apigenin, genistein, p-hydroxy-benzoic-acid, 7, 4'- dihydroxyflavone, quercetin-3-glucoside and sissotrin from the ethyl acetate fraction.


Subject(s)
Blood Glucose/drug effects , Diabetes Mellitus, Experimental/drug therapy , Hyperlipidemias/drug therapy , Hypoglycemic Agents/pharmacology , Hypolipidemic Agents/pharmacology , Lipids/blood , Medicago sativa , Plant Extracts/pharmacology , Animals , Biomarkers/blood , Blood Glucose/metabolism , Diabetes Mellitus, Experimental/blood , Diabetes Mellitus, Experimental/diagnosis , Hyperlipidemias/blood , Hyperlipidemias/diagnosis , Hypoglycemic Agents/isolation & purification , Hypolipidemic Agents/isolation & purification , Liver/drug effects , Liver/metabolism , Liver/pathology , Male , Medicago sativa/chemistry , Methanol/chemistry , Pancreas/drug effects , Pancreas/metabolism , Pancreas/pathology , Phytotherapy , Plant Extracts/isolation & purification , Plant Shoots , Plants, Medicinal , Rats, Wistar , Solvents/chemistry , Spleen/drug effects , Spleen/metabolism , Spleen/pathology , Time Factors
19.
Pharmacognosy Res ; 7(1): 14-7, 2015.
Article in English | MEDLINE | ID: mdl-25598629

ABSTRACT

Investigation of the chloroform extract of Euphorbia ammak leaves led to the isolation of three compounds: euphol (1), α-glutinol (2) and stigmasterol (3) Their structures were elucidated by 1D and 2D NMR, as well as by comparison with the reported data. Compounds 1-3 exhibited cytotoxicity in vitro against human cervical adenocarcinoma (Hela), among which, compound 1 showed the best activity.

20.
Nat Prod Res ; 28(15): 1134-41, 2014.
Article in English | MEDLINE | ID: mdl-24831420

ABSTRACT

Chemical investigation of the Red Sea sponge Dragmacidon coccinea led to the isolation of a new nucleoside, dragmacidoside (1), along with eight known compounds: adenosine (2), inosine (3), deoxycytidine (4), methyl-α-d-glucopyranoside (5), clionasterol (6), stigmasterol (7), campesterol (8) and brassicasterol (9). The compounds were isolated from chloroform and ethyl acetate fractions of the methanolic extract of the sponge, and their structures were established based on various spectroscopic data including MS, 1D and 2D NMR (COSY, HSQC and HMBC). Biological testing revealed that the chloroform fraction possesses significant anti-inflammatory activity in the carrageenan-induced hind paw oedema in rats.


Subject(s)
Nucleosides/isolation & purification , Porifera/chemistry , Animals , Anti-Inflammatory Agents/chemistry , Carrageenan/adverse effects , Edema/chemically induced , Edema/drug therapy , Indian Ocean , Marine Biology , Molecular Structure , Nucleosides/chemistry , Nucleosides/pharmacology , Rats , Sitosterols , Stigmasterol
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