scholarly journals In vitro evaluation of hydroalcoholic extracts of Capparis Spinosa L., Ricinus communis, and Solanum luteum on Leishmania major (MRHO/IR/75/ER) promastigotes.

2021 ◽  
Vol In Press (In Press) ◽  
Author(s):  
Hedieh Zadeh - Abbasi Zarandi ◽  
Leila Shirani-Bidabadi ◽  
Abass Aghaei - Afshar ◽  
Mustafa Eghbalian ◽  
Jaafar Zolaala ◽  
...  
Keyword(s):  
Leishmania Major ◽  
Ricinus Communis ◽  
Positive Control ◽  
Hydroalcoholic Extract ◽  
Percentage Difference ◽  
Capparis Spinosa ◽  
Viability Percentage ◽  
High Concentrations ◽  
Higher Doses

Background: Plant extracts or compounds derived from plants are a valuable source for finding new anti-leishmaniasis drugs. Objective: In this study, Capparis spinosa L., Ricinus communis, and Solanum luteum were used as lethal agents for the promastigotes of Leishmania major parasites in the culture medium. Methods: Diluted extracts of 12.5, 100, and 500 mg/mL were prepared from medicinal plant dried extracts. Glucantime at a concentration of 500 mg/mL was used as a positive control. Results: For all three extracts, concentrations of 100 and 500 mg/mL could kill promastigotes at higher rates and speeds compared to other concentrations. The high concentrations of extracts (500 mg/mL) presented similar effects. According to the findings, hydroalcoholic extract of C. Spinosa L. presented considerably lower antiparasitic effects, and S. luteum and R. communis extracts were could kill most of the parasitic promastigotes at higher doses. The ANOVA test did not show any significant viability percentage difference of Leishmania extracts between different extract types. Conclusions: In this study, the lethal effects of R. communis and S. luteum hydroalcoholic extracts on L. major promastigotes were found to be stronger than the C. Spinosa L. extract.

In vitro larvicidal and in vivo anthelmintic effects of Oxalis tetraphylla (Oxalidaceae) hydroalcoholic extract against Haemonchus contortus in lambs

2017 ◽  
Vol 92 (3) ◽  
pp. 309-316 ◽  
Author(s):  
B.J. González-Cruz ◽  
M. Rodríguez-Labastida ◽  
M. González-Cortázar ◽  
A. Zamilpa ◽  
M.E. López-Arellano ◽  
...  
Keyword(s):  
Haemonchus Contortus ◽  
Larval Mortality ◽  
Anthelmintic Activity ◽  
Positive Control ◽  
Plate Method ◽  
Hydroalcoholic Extract ◽  
Stage 1 ◽  
Two Stages

AbstractThe in vitro larvicidal and in vivo anthelmintic effects of Oxalis tetraphylla hydroalcoholic extract (HE), against Haemonchus contortus in experimentally infected lambs, were assessed. We used a microtitration plate method, comprising the following two stages. Stage 1: 20 μl of water containing 200 sheathed H. contortus infective larvae (ShHcl) were deposited in every well of three series; then, the series 2 and 3 wells were treated with 80 μl 1% ivermectin and O. tetraphylla HE at 20 mg/ml, respectively. Stage 2: the same procedure was performed replacing the ShHcl with exsheathed larvae (ExShHcl). Evaluations were performed after 24 and 48 h. The total numbers of dead and live larvae were counted. A second experiment evaluated the reduction in nematode egg populations in the faeces of lambs treated orally with the O. tetraphylla HE. The 27 lambs used were divided into Groups 1, 2 and 3 (n = 9), which were administered water (positive control), levamisole 1 m (7.5 mg/kg body weight (BW), as a unique dose) and O. tetraphylla HE (20 mg/kg BW), respectively. The plant HE was administered daily for 8 days. The in vitro assay showed 80.9% and 86.5% larval mortality of ShHcl after 24 and 48 h, respectively, while the corresponding mortality values for ExShHcl were 97 and 99%, respectively. The in vivo assay showed variability in the eggs/gram of faeces (epg) values; however, at the end of the trial, the average reduction in the epg values of the O. tetraphylla HE group was 45.6% (P < 0.05). Oxalis tetraphylla HE contains compounds that belong to the flavonol group with anthelmintic activity.

scholarly journals Antifungal Effects of Paraquat and Glyphosate on Rhizoctonia solani (Kühn) in Potato in vitro Condition

2021 ◽  
Vol 10 (1) ◽  
pp. 16
Author(s):  
José L. Arispe Vázquez ◽  
Abiel Sánchez Arizpe ◽  
Ma E. Galindo Cepeda ◽  
Cristina Trejo Ramos
Keyword(s):  
Rhizoctonia Solani ◽  
Petri Dish ◽  
Factor B ◽  
Morphological Criteria ◽  
Statistical Program ◽  
The Mean ◽  
High Concentrations ◽  
Open Markets ◽  
Higher Doses

Potato is one of the main crops worldwide. It this research, antifungal activity in vitro of paraquat and glyphosate were evaluated for Rhizoctonia solani control. R. solani was identified from potato tubers collected out from at open markets in Saltillo, Coahuila, Mexico. Two types of herbicides were applied: paraquat and glyphosate, at four different dosage treatments of: 10, 100, 1 000 and 10 000 &mu;L. One 5 mm diameter PDA disc with R. solani mycelium was placed at the center of the Petri dish, with a radial registry fungal every 24 h for 192 h. Pathogen was identified by morphological criteria and the data was evaluated randomly with a factorial arrangement, on which, herbicides represented factor A and dosage treatments were represented by factor B. Thus experimental design had two levels for factor A and five levels for factor B with six replications. The results were analyzed by the SAS version 9.1 statistical program, the mean separation with the Tukey test (p=0.05). Glyphosate achieved inhibition of R. solani by 35.5882% and paraquat up to 80.0399%. Results reveal the importance of the need for more studies of these herbicides as fungicides. High concentrations of paraquat (10 000 &mu;L) inhibits R. solani, and glyphosate does not affect R. solani mycelium development at low dosages (10 and 100 &mu;L) and inhibits it at higher doses (10 000 &mu;L).

Anti-Leishmanial Activity of Novel Homo- and Heteroleptic Bismuth(III) Thiocarboxylates

2013 ◽  
Vol 66 (10) ◽  
pp. 1297 ◽  
Author(s):  
Philip C. Andrews ◽  
Peter C. Junk ◽  
Lukasz Kedzierski ◽  
Roshani M. Peiris
Keyword(s):  
Mammalian Cells ◽  
Leishmania Major ◽  
Lone Pair ◽  
Phenyl Group ◽  
Distorted Octahedral Geometry ◽  
X Ray Crystallography ◽  
Highly Active ◽  
Thiobenzoic Acid ◽  
High Concentrations

Two new thiocarboxylic acids, p-bromothiobenzoic BTA and thionaphthoic acid TNA, and five new homo- and heteroleptic bismuth(iii) compounds derived from thiocarboxylic acids: [Bi{S(C=O)C6H4Br}3] 1, [PhBi{S(C=O)C6H4Br}2] 2, [Bi{S(C=O)C10H7}3] 3, [PhBi{S(C=O)C10H7}2] 4, and [Ph2Bi{S(C=O)C10H7}] 5 were synthesised and fully characterised. The solid-state structure of complex [PhBi{S(C=O)C6H4Br}2] 2 was confirmed by X-ray crystallography. In complex 2, the two thiocarboxylate ligands are coordinated to the bismuth(iii) centre in a didentate fashion, forming a distorted octahedral geometry in which the phenyl group and the lone pair are oriented axial to the plane formed by the two thiocarboxylate ligands. Long-range Bi–S interactions (3.54 Å) link these monomeric units to form a one-dimensional polymer. These compounds, in addition to six previously synthesised complexes: [Bi{SC(=O)C6H5}3] 6, [PhBi{SC(=O)C6H5}2] 7, [Ph2Bi{SC(=O)C6H5}] 8, [Bi{SC(=O)C6H4NO2}3] 9, [PhBi{SC(=O)C6H4NO2}2] 10, and [PhBi{SC(=O)C6H4SO3}] 11, and the thiocarboxylic acids themselves, were assessed for their in vitro activity against Leishmania major promastigotes, and for general toxicity against human fibroblast cells. The thiocarboxylic acids, with the exception of thiobenzoic acid and sulfothiobenzoic acid, were toxic to both L. major parasites and the mammalian cells at high concentrations of 50–100 μM. The bismuth(iii) thiocarboxylate derivatives proved to be more active than the corresponding acids. Among these, the heteroleptic phenyl-substituted bismuth(iii) complexes 2, 4, 5, and 7 were highly active, showing IC50 (half maximal inhibitory concentration) values ranging from 0.39 to 4.69 μM, and a clear ligand dependence on activity.

scholarly journals In vitro study of the efficacy of Solanum nigrum against Leishmania major

F1000Research ◽  
2018 ◽  
Vol 7 ◽  
pp. 1329 ◽  
Author(s):  
Christine N. Mutoro ◽  
Johnson K. Kinyua ◽  
Joseph K. Ng'ang'a ◽  
Daniel W. Kariuki ◽  
Johnstone M. Ingonga ◽  
...  
Keyword(s):  
Leishmania Major ◽  
In Vitro Study ◽  
Vero Cells ◽  
Solanum Nigrum ◽  
Therapeutic Interventions ◽  
Phlebotomine Sandflies ◽  
High Concentrations ◽  
Antileishmanial Activities

Leishmania parasites (Kinetoplastida: Trypanosomatidae) are obligate intracellular parasites of macrophages that causes visceral and cutaneous leishmaniases. Currently, there is inadequate therapeutic interventions to manage this endemic tropical disease, transmitted mainly by phlebotomine sandflies hence there is need to develop affordable and effective therapeutic measures. This study determined the in vitro efficacy of Solanum nigrum methanolic and aqueous plant extracts on Leishmania major parasites.  Cytotoxic effects of the extracts were determined using vero cells and reported as percentage viability of the cells. The promastigote parasites of Leishmania major were cultured and grown for 3 days in different concentrations of extracts to determine the MIC and IC50 values. The in vitro antileishmanial efficacy was done on macrophages infected with L. major amastigote parasites and then treated with extracts in varying concentrations. The study revealed that all the test extracts had lower toxicity than control drugs, pentostam (IC50= 0.0 92 mg/ml) and amphotericin B (IC50=0.049 mg/ml).  The extracts tended to show a dose dependent cytotoxic effect which corresponded to high vero cells viability as their concentration increased.  Methanolic extract of S. nigrum from Kisii seemed to be more efficacious in vitro since it knocked out the promastigotes at a lower MIC level (0.5 mg/ml) when compared to all other extracts whose effective MIC level was ≥ 1 mg/ml. High concentrations of the test extracts and control drugs resulted to low infectivity and multiplication of L. major amastigotes. Findings from this study demonstrate that S. nigrum extracts have potential antileishmanial activities however; further investigation needs to be done on pure compound isolation, in vivo assays and clinical trials so as to use the promising compounds as effective antileishmanial agents.

252 VITRIFICATION OF BOVINE BLASTOCYSTS PRODUCED AFTER OOCYTE MATURATION IN MEDIA CONTAINING FATTY ACIDS

2008 ◽  
Vol 20 (1) ◽  
pp. 205
Author(s):  
M. A. Shehab-El-Deen ◽  
J. L. M. R. Leroy ◽  
D. Maes ◽  
A. Van Soom
Keyword(s):  
Fatty Acids ◽  
Fatty Acid ◽  
Stearic Acid ◽  
Dairy Cows ◽  
In Vitro Maturation ◽  
Embryo Quality ◽  
Positive Control ◽  
High Concentrations ◽  
Carry Over

High concentrations of non-esterified fatty acids (NEFA) during negative energy balance (NEB) in high yielding dairy cows have been proven to be partially responsible for reduced fertility. This hypothesis has been tested by the addition of NEFAs to in vitro maturation medium at concentrations present in follicular fluid during NEB. We aimed to evaluate whether high concentrations of palmitic acid (C16:0) (PA), stearic acid (C18:0) (SA), or oleic acid (C18:1) (OA) during oocyte maturation could have a carry-over effect on embryo quality and could subsequently affect embryo cryotolerance. Cumulus–oocyte complexes (n = 4600) were matured in serum-free TCM199 plus epidermal growth factor (EGF, 20 ng mL–1; negative control), supplemented with ethanol alone (positive control) or with 0.133 mmol L–1 PA, 0.067 mmol L–1 SA, or 0.200 mmol L–1 OA (NEFAs dissolved in ethanol). The three NEFAs were tested separately in 4 replicates for PA and 5 replicates for OA or SA. Each fatty acid tested per replicate including a negative and a positive control group. After the embryos were cultured for 7 days in SOF medium, the number of blastocysts was recorded and classified as expanded, hatching, or hatched. Then, blastocysts were cryopreserved by open pulled straw vitrification using the two-step approach described by Vajta et al. (1998 Mol. Reprod. Dev. 51, 53–58). Vitrified warmed embryos were cultured in groups of <25 per 50-μL droplet of modified SOF medium with 5% fetal calf serum (FCS) under mineral oil for 48 h and examined for re-expansion and hatching. The percentages of survival in the different treatment groups were analyzed using logistic regression analyses, including the effect of replicates. Survival or not was included as the dependent variable and group was the independent variable. For every fatty acid a separate model was used. For all analyses, differences were considered to be statistically significant at the P < 0.05 level. Addition of OA to in vitro maturation media had no significant effects on cryotolerance of embryos. However, addition of PA or SA to in vitro maturation media (Table 1) significantly (P < 0.05) decreased the survival of bovine blastocysts from 79% in the positive control to 57% in PA and from 61% to 53% in SA. The results of the present study indicate that maturation of oocytes in the presence of NEB-associated concentrations of PA and SA can have carry-over effects on embryo quality, leading to reduced cryotolerance. We suggest that elevated NEFA concentrations in the follicular fluid may be one of the factors through which NEB exerts its negative effects on fertility in high yielding dairy cows. Table 1. Survival percentage (mean ± SD) of vitrified expanded bovine blastocysts matured in palmitic acid (C16:0) or stearic acid (C18:0) The authors thank J. Mestach and G. Spaepen for their excellent technical support. This research was supported by the Ministry of the Flemish Community, Belgium, in cooperation with the Ministry of Higher Education, Egypt.

Ricin-resistant mutants ofLeishmania majorwhich express modified lipophosphoglycan remain infective for mice

Parasitology ◽  
1994 ◽  
Vol 108 (4) ◽  
pp. 397-405 ◽  
Author(s):  
R. Cappai ◽  
L. Morris ◽  
T. Aebischer ◽  
A. Bacic ◽  
J. M. Curtis ◽  
...  
Keyword(s):  
Slow Rate ◽  
Leishmania Major ◽  
Karyotype Analysis ◽  
Ricinus Communis ◽  
Chromosome Band ◽  
Lesion Development ◽  
Altered Expression ◽  
Resistant Mutants ◽  
Band Number

SUMMARYGlycosylation variants of the virulentLeishmania majorclone VI21 were generated by mutagenesis withN-methyl-N-nitroso-N-nitroguanidine and selected using the galactose-specific lectinRicinus communisII (RCA II). Three mutants, 4B9, 1D1 and 1C12, which failed to bind RCA II, were found to have an altered expression of lipophosphoglycan (LPG), a molecule implicated in the attachment to host macrophages and survival within the phagolysosome. There were differences in the antigenicity, molecular weight and localization of LPG from mutant parasites as compared to V121. Expression of gp63, a surface molecule also implicated in attachment to macrophages, was unaltered. All 3 mutants caused disease when injected into genetically susceptible BALB/c mice but lesions developed at a much slower rate than those caused by the virulent V121 clone. This slow rate of lesion development did not correlate with promastigotes' ability to invade macrophagesin vitro. Karyotype analysis showed that there was a reduction in the size of chromosome band number 2 in all 3 mutants. The differences in LPG and chromosome band 2 were retained by mutant clones following passage through mice, suggesting that these phenotypes are stable. Although the mutant parasites were infective and caused lesions, the changed structure of the LPG appeared to influence the virulence of the parasites.

Lack of in Vitro Inactivation of Tobramycin by Imipenem/Cilastatin

1992 ◽  
Vol 26 (9) ◽  
pp. 1075-1077 ◽  
Author(s):  
Robert E. Ariano ◽  
Diamond A. Kassum ◽  
Robert C. Meatherall ◽  
Ward D. Patrick
Keyword(s):  
Half Life ◽  
Positive Control ◽  
Serum Concentrations ◽  
Beta Lactam ◽  
Percent Loss ◽  
Degradation Rates ◽  
High Concentrations ◽  
Vitro Model

OBJECTIVE: Inactivation of aminoglycosides by beta-lactam antimicrobials both in vitro and in vivo has been documented. Such an interaction has not previously been documented between carbapenems and aminoglycosides. Examination of serum concentrations of tobramycin in a patient receiving both agents suggested that this interaction might exist. The purpose of this study was to look at this question in an in vitro model. METHODS: Low concentrations of tobramycin (10 μg/mL) were incubated with imipenem/cilastatin (concentrations of 10, 20, and 40 μg/mL) in human serum at 37°C. Aliquots of these solutions were withdrawn at 0, 6, 24, 72, and 120 hours and assayed for tobramycin concentrations using a fluorescence polarization immunoassay. Aliquots of tobramycin 10 μg/mL and carbenicillin 200 μg/mL were analyzed in the same manner, as a positive control. High concentrations of tobramycin (800 μg/mL) and imipenem (5000 μg/mL)/cilastatin were incubated together at 21°C and sampled at 0, 6, 24, and 72 hours for tobramycin concentrations. RESULTS: The degradation rates for low-concentration tobramycin and the various concentrations of imipenem/cilastatin were not statistically different from those of the controlled incubations. In contrast, carbenicillin significantly enhanced the degradation rate of tobramycin at this concentration (half-life 72 hours and a 34 percent loss at 24 hours, p=0.0028). Higher in vitro concentrations of imipenem (5000 μg/mL)/cilastatin and tobramycin (800 μg/mL) resulted in significant, but moderate degradation over controlled incubations (half-life 80 hours and 10 percent loss at 12 hours, p=0.0031). CONCLUSIONS: These results suggest that inactivation of tobramycin is not a problem at common clinically achievable imipenem serum concentrations in patients.

scholarly journals Comparative Neuropharmacology and Pharmacokinetics of Methamphetamine and Its Thiophene Analog Methiopropamine in Rodents

2021 ◽  
Vol 22 (21) ◽  
pp. 12002
Author(s):  
Silja Skogstad Tuv ◽  
Marianne Skov-Skov Bergh ◽  
Jannike Mørch Andersen ◽  
Synne Steinsland ◽  
Vigdis Vindenes ◽  
...  
Keyword(s):  
Pharmacokinetic Profile ◽  
Structural Analog ◽  
Psychoactive Substance ◽  
Psychomotor Activity ◽  
Clinical Toxicity ◽  
High Concentrations ◽  
Presynaptic Nerve Terminals ◽  
Higher Doses

Methiopropamine is a novel psychoactive substance (NPS) that is associated with several cases of clinical toxicity, yet little information is available regarding its neuropharmacological properties. Here, we employed in vitro and in vivo methods to compare the pharmacokinetics and neurobiological effects of methiopropamine and its structural analog methamphetamine. Methiopropamine was rapidly distributed to the blood and brain after injection in C57BL/6 mice, with a pharmacokinetic profile similar to that of methamphetamine. Methiopropamine induced psychomotor activity, but higher doses were needed (Emax 12.5 mg/kg; i.p.) compared to methamphetamine (Emax 3.75 mg/kg; i.p.). A steep increase in locomotor activity was seen after a modest increase in the methiopropamine dose from 10 to 12.5 mg/kg, suggesting that a small increase in dosage may engender unexpectedly strong effects and heighten the risk of unintended overdose in NPS users. In vitro studies revealed that methiopropamine mediates its effects through inhibition of norepinephrine and dopamine uptake into presynaptic nerve terminals (IC50 = 0.47 and 0.74 µM, respectively), while the plasmalemmal serotonin uptake and vesicular uptake are affected only at high concentrations (IC50 > 25 µM). In summary, methiopropamine closely resembles methamphetamine with regard to its pharmacokinetics, pharmacodynamic effects and mechanism of action, with a potency that is approximately five times lower than that of methamphetamine.

scholarly journals Coumarins and Polar Constituents from Eupatorium triplinerve and Evaluation of Their α-Glucosidase Inhibitory Activity

2020 ◽  
Vol 2020 ◽  
pp. 1-8
Author(s):  
Do Thi Viet Huong ◽  
Phan Minh Giang ◽  
Vu Minh Trang
Keyword(s):  
2D Nmr ◽  
Positive Control ◽  
Water Soluble ◽  
In Vitro Test ◽  
Leaf Extracts ◽  
Ic50 Value ◽  
Vitro Test ◽  
High Concentrations ◽  
First Time

In our study of antidiabetic compounds from the leaves of Eupatorium triplinerve Vahl. (Asteraceae), ten compounds were isolated from the methanol leaf extract. They were determined to be β-sitosterol (1), stigmasterol (2), β-sitosterol 3-O-β-D-glucopyranoside (3), ayapanin (4), ayapin (5), thymoquinol 5-O-β-D-glucopyranoside (6), thyrsifloside (8), (E)-4-methoxymelilotoside (9), and kaempferol 3,7-di-O-β-D-glucopyranoside (10) by using ESI-MS, 1D (1H-, 13C-, DEPT) and 2D NMR (HSQC, HMBC, and NOESY) techniques. This is the first report of water-soluble compounds from E. triplinerve and compounds 6–10 were isolated for the first time from E. triplinerve. NMR profiling and HPLC analysis are fast and reliable methods to screen phytochemicals in plant samples. Due to their high concentrations in the leaf extracts of E. triplinerve, coumarins 4 and 5 could be fast screened by NMR profiling and RP-HPLC-PDA analysis. In the in vitro test for α-glucosidase inhibition of compounds 4–9, compounds 4, 5, and 7 showed the enzymatic inhibition of 40%, 46%, and 81%, respectively, at 256 μg/mL. An IC50 value of 58.65 ± 1.20 μg/mL (302 μM) was calculated for compound 7 which is lower than that of the positive control acarbose (IC50 197.33 ± 2.51 μg/mL; 306 μM).

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