scholarly journals Saponins from the roots of Chenopodium bonus-henricus L. with neuroprotective and anti-α-glucosidase activities

Pharmacia ◽  
2021 ◽  
Vol 68 (2) ◽  
pp. 387-392
Author(s):  
Zlatina Kokanova-Nedialkova ◽  
Magdalena Kondeva-Burdina ◽  
Paraskev Nedialkov

Six saponins of phytolaccagenin, bayogenin, medicagenic acid, 2β-hydroxygypsogenin, and 2β-hydroxyoleanoic acid from the roots of Chenopodium bonus-henricus L. were investigated for neuroprotective and anti-α-glucosidase activities. All tested saponins (10 µM) showed statistically significant neuroprotective activities on isolated rat brain synaptosomes using a 6-hydroxydopamine in vitro model. They preserved synaptosome viability as well as the reduced glutathione level. The bayogenin glycoside (Chbhs-05) possessed the most prominent neuroprotective effect. The anti-α-glucosidase activity of the tested saponins was established by measuring the levels of the released 4-nitrophenol using LC-MS. Bonushenricoside B (Chbhs-07) showed the highest inhibitory effect against α-glucosidase (44.1%) compared to the positive control acarbose (36.3%) at a concentration of 625 µM.

1967 ◽  
Vol 54 (4) ◽  
pp. 645-662 ◽  
Author(s):  
Å. Hjalmarson ◽  
K. Ahrén

ABSTRACT The effect of growth hormone (GH) in vitro on the rate of intracellular accumulation of the non-utilizable amino acid α-aminoisobutyric acid (AIB) was studied in the intact rat diaphragm preparation. Bovine or ovine GH (25 μg/ml incubation medium) markedly stimulated the accumulation of AIB-14C by diaphragms from hypophysectomized rats, while there was no or only a very slight effect on diaphragms from normal rats. In diaphragms from rats with the pituitary gland autotransplanted to the kidney capsule GH in vitro stimulated the accumulation of AIB-14C significantly more than in diaphragms from normal rats but significantly less than in diaphragms from hypophysectomized rats. Injections of GH intramuscularly for 4 days to hypophysectomized rats made the diaphragms from these rats less sensitive or completely insensitive to GH in vitro. These results indicate strongly that the relative insensitivity to GH in vitro of diaphragms from normal rats is due to the fact that the muscle tissues from these rats has been exposed to the endogenously secreted GH. The results show that GH can influence the accumulation of AIB-14C in the isolated rat diaphragm in two different ways giving an acute or »stimulatory« effect and a late or »inhibitory« effect, and that it seems to be a time-relationship between these two effects of the hormone.


2013 ◽  
Vol 49 (4) ◽  
pp. 803-809
Author(s):  
Monica Lacerda Lopes Martins ◽  
Henrique Poltronieri Pacheco ◽  
Iara Giuberti Perini ◽  
Dominik Lenz ◽  
Tadeu Uggere de Andrade ◽  
...  

In 1820, French naturalist August Saint Hillaire, during a visit in Espírito Santo (ES), a state in southeastern Brazil, reported a popular use of Cyperaceae species as antidote to snake bites. The plant may even have a hypotensive effect, though it was never properly researched. The in vitro inhibitory of the angiotensin converting enzyme (ACE) activity of eigth ethanolic extracts of Cyperaceae was evaluated by colorimetric assay. Total phenolic and flavonoids were determined using colorimetric assay. The hypotensive effect of the active specie (Rhychonospora exaltata, ERE) and the in vivo ACE assay was measured in vivo using male Wistar Kyoto (ERE, 0.01-100mg/kg), with acetylcholine (ACh) as positive control (5 µg/kg, i.v.). The evaluation of ACE in vivo inhibitory effect was performed comparing the mean arterial pressure before and after ERE (10 mg/kg) in animals which received injection of angiotensin I (ANG I; 0,03, 03 and 300 µg/kg, i.v.). Captopril (30 mg/kg) was used as positive control. Bulbostylis capillaris (86.89 ± 15.20%) and ERE (74.89 ± 11.95%, ERE) were considered active in the in vitro ACE inhibition assay, at 100 µg/mL concentration. ACh lead to a hypotensive effect before and after ERE's curve (-40±5% and -41±3%). ERE showed a dose-dependent hypotensive effect and a in vivo ACE inhibitory effect. Cyperaceae species showed an inhibitory activity of ACE, in vitro, as well as high content of total phenolic and flavonoids. ERE exhibited an inhibitory effect on both in vitro and in vivo ACE. The selection of species used in popular medicine as antidotes, along with the in vitro assay of ACE inhibition, might be a biomonitoring method for the screening of new medicinal plants with hypotensive properties.


2020 ◽  
Vol 19 (1) ◽  
pp. 163-168
Author(s):  
Lin Ling ◽  
Chen Ling ◽  
Hua Wu

Purpose: To investigate the anti-tuberculosis potential of twelve commercially available pyridone analogues against Mycobacterium tuberculosis H37Rv strain.Methods: Twelve commercially available pyridone-based compounds were screened against M. tuberculosis H37Rv using different susceptibility tests. The most active or lead compound was further evaluated in detail for its anti-tuberculosis (anti-TB) potential. Kill kinetics was used to determine the dynamics of its anti-TB activity in vitro.Results: Compounds d, j and k were potent against M. tuberculosis H37Rv, with minimum inhibitory concentrations (MICs) of 10, 5 and 10 μg/mL, respectively. The standard anti-TB drugs used in this study (positive control drugs) demonstrated MIC of 2.5 μg/mL. The anti-TB effect of compound j was comparable with those of the standard drugs (RIF, LVX, AMK, EMB and INH). The minimum bactericidal concentration (MBC) of compound j was 10 μg/mL. It produced an MIC of 5 μg/mL in agar proportion method (APM). However, its MIC in Middlebrook 7H9 broth supplemented with 10 % fetal bovine serum (FBS) and 4 % bovine serum albumin (BSA) increased 4- and 8-fold, respectively. The bactericidal effect of compound j was time- and concentration-dependent at dilutions above 2x MIC. Combination of compound j with RIF, LVX or AMK exhibited fractional inhibitory concentration index (ΣFIC) of 1, indicative of additive drug-drug interactions. However, combination with INH or EMB produced a ΣFIC of 2. None of the tested drug combinations was antagonistic.Conclusion: Compound j exhibits potent time- and concentration-dependent antimicrobial effect against M. tuberculosis H37Rv. Thus, it may be suitable as an adjunct to current treatment of drug sensitive and drug-resistant TB. Keywords: Tuberculosis, Mycobacterium tuberculosis, Pyridone analogs, Antimicrobial activity, Antibiotics


2014 ◽  
Vol 9 (4) ◽  
pp. 1934578X1400900 ◽  
Author(s):  
Gordana S. Stojanović ◽  
Miroslava Stanković ◽  
Igor Ž. Stojanović ◽  
Ivan Palić ◽  
Vesna Milovanović ◽  
...  

Three lichen secondary metabolites atranorin (1), evernic acid (2), and usnic acid (3), were evaluated for their in vitro clastogenic and antiproliferative effects on human lymphocytes using the cytochalasin-B blocked micronucleus (CBMN) assay at concentrations of 2 μg/mL, 4 μg/mL and 6 μg/mL of final culture solution. The frequency of micronucleus (MN) was scored in binucleated cells, and cytokinesis-block proliferation index (CBPI) was calculated. Among the tested compounds, 3 exhibited the most prominent effect decreasing the frequency of MN in the range of 42.5% - 48.9%, that is about double of the positive control amifostin WR-2721 that reduces MN frequency for 22.0%. The effect of evernic acid was approximately equal to action of amifostin (23.2% −32.9%). Atranorin at concentrations of 2 μg/mL and 4 μg/mL decreasing the frequency of MN only for 11.1% and 1.8%, while in concentration of 6 μg/mL increases the frequency of MN for 9.6 %. The comparable CBPI values of the investigated compounds and control suggested that they did not show a statistically significant inhibitory effect on lymphocyte cell proliferation at applied concentrations.


2019 ◽  
Vol 37 (2) ◽  
pp. 286-297 ◽  
Author(s):  
Magdalena Kurnik-Łucka ◽  
Gniewomir Latacz ◽  
Adrian Martyniak ◽  
Andrzej Bugajski ◽  
Katarzyna Kieć-Kononowicz ◽  
...  

AbstractSalsolinol (6,7-dihydroxy-1-methyl-1,2,3,4-tetrahydroisoquinoline), widely available in many edibles, is considered to alter the function of dopaminergic neurons in the central nervous system and thus, multiple hypotheses on its either physiological and/or pathophysiological role have emerged. The aim of our work was to revisit its potentially neurotoxic and/or neuroprotective role through a series of both in vitro and in vivo experiments. Salsolinol in the concentration range 10–250 μM did not show any significant release of lactate dehydrogenase from necrotic SH-SY5Y cells and was able in the concentration of 50 and 100 μM to rescue SH-SY5Y cells from death induced by H2O2. Its neuroprotective effect against neurotoxin 6-hydroxydopamine was also determined. Salsolinol was found to decrease significantly the reactive oxygen species level in SH-SY5Y cells treated by 500 μM H2O2 and the caspase activity induced by 300 μM of H2O2 or 100 μM of 6-hydroxydopamine. Serum levels of TNFα and CRP of salsolinol-treated rats were not significantly different from control animals. Both TNFα and CRP served as indirect markers of neurotoxicity and/or neuroprotection. Although the neurotoxic properties of salsolinol have numerously been emphasized, its neuroprotective properties should not be neglected and need greater consideration.


1990 ◽  
Vol 258 (6) ◽  
pp. G967-G973 ◽  
Author(s):  
J. C. Fernandez-Checa ◽  
T. Maddatu ◽  
M. Ookhtens ◽  
N. Kaplowitz

The inhibition of efflux of intracellular reduced glutathione (GSH) by methionine was determined in isolated rat hepatocytes suspended either in Krebs-Henseleit buffer or in modified Fisher's medium. Methionine (1 mM) added to Krebs-Henseleit suspensions of isolated rat hepatocytes inhibited GSH efflux, with greater retention of GSH in the cells compared with control. Results were similar with methionine and 0.3 mM propargylglycine cystathionase inhibitor), suggesting no net synthesis of GSH from methionine. In Fisher's medium, the inhibitory effect of methionine on GSH efflux was masked due to increasing cellular GSH; however, the inhibitory effect of methionine was unmasked by propargylglycine, which prevented the utilization of methionine for GSH synthesis. The addition of serine (0.1 mM) to methionine in Krebs-Henseleit buffer raised cellular GSH, overcoming the inhibition of GSH efflux. In the perfused liver, infusion of 1 and 5 mM methionine initially inhibited GSH efflux, but the inhibition was reversed with continued methionine infusion. After removal of methionine, GSH efflux increased immediately. The reversal and rebound were blocked by propargylglycine, revealing concentration-dependent inhibition of sinusoidal GSH efflux by methionine. Thus, when methionine is utilized to promote GSH synthesis, its inhibitory effect on GSH efflux tends to be overcome.


Author(s):  
NIRAJ VYAS ◽  
KANAN GAMIT ◽  
MANAN RAVAL ◽  
SAMIR PATEL

Objective: Present study was aimed to isolate and chemically characterize bioactive constituent from alkaloid enriched fraction, prepared from roots of Argyreia speciosa Linn. Materials and methods: Literature review revealed presence of ergoline type of alkaloids in roots. Alkaloidal fraction was prepared and screened for its action on testosterone biosynthesis, in- vitro, using isolated rat leydig cells. Dehydroepiandosterone was used as positive control. This bioactive fraction was subjected to open column chromatography followed by flash chromatography, to isolate constituent. One compound (A1) was isolated from the fraction and its purity was ascertained using TLC and HPLC studies. A1 was chemically characterized by IR, Mass and 1H-NMR studies, to elucidate probable chemical structure. A1 was screened for action on testosterone synthesis too, using isolated rat Leydig cells model. The fraction was standardized with respect to amount of A1 present.   Results: Alkaloidal fraction (1000 µg/ml) incubated Leydig cells showed nearly, 22 fold increase in testosterone content as compared to untreated cells. The studies also yielded increase in testosterone content, in cells treated with test fractions and as observed in case of positive control. TLC studies indicated that A1 might possess ergoline moiety in the structure. IR, Mass and 1H NMR spectral studies suggested that A1 might be N-methyl ergometrine. This was the first report included isolation and chemical characterization of N-methyl ergometrine from Argyreia speciosa. A1 (1000 µg/ml) was found to stimulate testosterone content, by 14.62 fold, in culture media of Leydig cells after incubation. Conclusion: The results of in vitro studies, confirmed that the standardized alkaloid fraction as well as A1 had ability to stimulate Leydig cells to secrete testosterone. A1 might be N-methyl ergometrine and being ergometrine derivative it might act through oxytocine receptors expressed on the Leydig cells and stimulates testosterone synthesis.


Pharmacia ◽  
2019 ◽  
Vol 66 (4) ◽  
pp. 233-236
Author(s):  
Magdalena Kondeva-Burdina ◽  
Ilina Krasteva ◽  
Georgi Popov ◽  
Vasil Manov

The aim of the study was to investigate the possible neuroprotective and antioxidant activity of purified saponins’mixture (PSM), isolated from Astragalus glycyphylloides (Fabaceae), in a model of 6-hydroxydipamine (6-OHDA)-induced oxidative stress on isolated rat brain synaptosomes. Synaptosomes were incubated with 3 different concentrations of PSM: 60 µg/mL; 6 µg/mL; 0.6 µg/mL. The effects of PSM were compared to those of silymarin (S), at the same concentrations. The main parameters, characterized functional and metabolic status of synaptosomes, were investigated: viability (MTT-test) and level of reduced glutathione (GSH). At isolated rat brain synaptosomes, in conditions of 6-OHDA-induced oxidative stress (150 μМ), PSM revealed statistically significant, concentration-dependent, neuroprotective and antioxidant effects, compared to those of silymarin. Effects were most prominent at concentration 60 µg/mL. These neuroprotective effects of PSM might be due to the possible activity as scavenger of reactive oxygen species (ROS), produced by p-quinone (toxic metabolite of 6-OHDA).


2018 ◽  
Author(s):  
◽  
Nkululeko Xaba

Background Due to the rise of antibiotic resistant bacterial infections, alternative methods of treatment need to be explored. Homoeopathic medicine is based on the principle of ‘like cures like’ (O’Reilly, 1996) i.e. the symptoms the substance can cause, it can cure which is the underlying rationale for this study. Colibacillinum is a remedy prepared from an enteropathogenic strain of E. coli, this remedy is already used in clinical practice against chronic cystitis (Leupen, 2010) caused by E. coli, however, an extensive literature search has revealed there to be no empirical investigation into its antibiotic capacity. This study aimed to show whether or not this remedy demonstrates antimicrobial capacity against E. coli in an in vitro setting. Parallell homoeopathic potencies of this remedy and one prepared from a uropathogenic strain of E. coli were tested for antimicrobial effects against enteropathogenic and uropathogenic strains of E. coli in vitro using the disc diffusion method. Aim of the study The aim of this controlled in vitro study is to determine the antimicrobial effectiveness of parallel potencies of the homoeopathic remedy Colibacillinum (manufactured from a uropathogenic strain and enteropathogenic strains respectively) against uropathogenic and enteropathogenic cultures of E. coli in vitro by means of the disc diffusion assay method. Methodology Measurements were by means of the disc diffusion essay. For this experiment thirty Mueller-Hinton plates were prepared and inoculated with each test bacteria in turn. Fifteen plates were inoculated with Uropathogenic strain of E. coli and the remaining 15 plates were inoculated with Uropathogenic strain of E. coli. A sterile 5mm Whatman® filter paper number 4 discs were individually inoculated with test substances 3CH,9CH,30CH and 200CH potencies and the controls, negative (43% ethanol) and positive control (Ciprofloxacin) using a micropipette, before being allowed to dry in the incubator. A Ciprofloxacin antibiotic (positive control) was included in the experiment with sole purpose of accounting for plate-plate variations in the pharmacological sensitivity of the same specie of bacteria. The plates were incubated at 37°C, and the zones of inhibition measured with a pair of Vernier calipers at 24 hours. Data entry was done using the SPSS statistical package. ANOVA was used to compare the differences between the test and control groups, Mauchly’s Test of Sphericity for Uropathogenic prepared strain, Mauchly’s Test of Sphericity for Enteropathogenic prepared strain, Normality test. Results The results obtained from this study showed that the Homoeopathic remedy Colibacillinum prepared from both Uropathogenic and Enteropathogenic strains displayed inhibitory effects against Enteropathogenic and Uropathogenic strains of E. coli, and exhibited statistically significance. The control group (ciprofloxacin) had the highest inhibitory effect (42.3±0.58mm) against Enteropathogenic and Uropathogenic E. coli, while the negative control (43% ethanol) had the lowest inhibitory effect (0.67±1.15mm). Colibacillinun 200CH prepared from a Uropathogenic strain of E-coli (Coli-b_U 200CH) displayed statistically significant antimicrobial effects against uropathogenic E.coli; such antimicrobial effects were significantly greater than 43% ethanol (negative control); the antimicrobial effect was however inferior to Ciprofloxacin (positive control). Colibacillinum 9CH prepared from Enteropathogenic strain of E-coli (Coli-b_E 9CH) also displayed statistically significant antimicrobial effects against enteropathogenic E.coli which were significantly greater than 43% ethanol (negative control) but inferior to Ciprofloxacin. Conclusion This study concluded that Colibacillinum prepared from Uropathogenic and Enteropathogenic strains of E. coli, are effective in inhibiting the in vitro growth of E.coli when evaluated by means of disc diffusion. The study further confirmed that the biological (anti-microbial) activity of an ultra-high homoeopathic dilution (Coli-b_U 200CH) (1:10400) and in the case of Coli-b_U the findings support existing literature which suggests that the anti-microbial properties of homeopathic nosodes increase with potency; all hypotheses for this remedy were thus accepted. This trend was not noted for Coli-b_E in which the potency with the greatest anti-microbial effect was the 9CH, thus Colibacillinum prepared from Enteropathogenic strain (Coli-b_E) did not conform with hypothesies one, two and four that were proposed in chapter one. Despite this the confirmation of significant antimicrobial effects of a substance at this level of deconcentration (1:1018) is noteworthy.


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