Evaluation of the Antileishmanial Properties of Ixora brachiata Roxb on Leishmania major and Leishmania infantum by Colorimetric MTT Assay

Background: Leishmaniasis is a major global health problem which affects millions of people, especially in the developing countries. The incidence of leishmaniasis has increased and there is no vaccination for Leishmania infections and standard drugs for treatment of the disease have many side effects; therefore, it is necessary to find new effective alternatives. Objectives: The purpose of this study was to evaluate the in vitro antileishmanial activity of Ixora brachiata root extract against Leishmania major and Leishmania infantum promastigotes. Materials and Methods: Different doses of the selected plant extract was tested against L. major and L. infantum promastigotes using colorimetric MTT [3-(4, 5-methylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide] assay. Glucantime was used as the positive control. Results: Anti-parasitic activity was revealed for I. brachiata root on L. major and L. infantum with 50% inhibitory concentration (IC50) values of 0.91 and 2.63 µg/mL, respectively compared to the standard drugs, glucantime, which had an IC50 value of 40.2 µg/mL for L. major and 18.5 µg/ mL for L. infantum after 72 hours. Conclusion: The results of this study created a new background on the development of drug against leishmania parasite.

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Neuroprotectıve Potential of the Tubers of Corydalis triternata Zucc. Growing in Turkey

Journal of the chemical society of pakistan ◽

10.52568/000661 ◽

2020 ◽

Vol 42 (4) ◽

pp. 515-515

Author(s):

Mehtap K l c Mehtap K l c ◽

Erdal Kaya Erdal Kaya ◽

Ayhan Ibrahim Aysal Ayhan Ibrahim Aysal ◽

Bilge Sener Bilge Sener

Keyword(s):

Metabolite Profile ◽

Positive Control ◽

Anticholinesterase Activity ◽

Ex Situ ◽

In Vitro Tests ◽

Drug Candidates ◽

Ic50 Value ◽

Ic50 Values ◽

Tof Ms

The continuing research for the determination of bioactive secondary metabolites from Turkish geophytes as therapeutic agents for dementia is mainly based on the need for drug candidates affected to brain areas. In this study, the in vitro anticholinesterase activity of the alkaloidal fractions of the tubers of Corydalis triternata Zucc. was investigated for their neuroprotective potential. Furthermore, the content of the active alkaloid fractions of the tubers was determined by LC-Q-TOF-MS. The tubers of Corydalis triternata Zucc. were collected from Hatay province of Turkey. The plant species were also preserved as ex-situ in Yalova-Turkey. The alkaloidal extract was prepared from the tubers. The anticholinesterase activities of the extracts and fractions were tested by modification of the Ellman’s method. The optimization of LC-MS conditions was used in ESI in the positive ion mode. The in vitro tests were highlighted that the alkaloidal extract of the tubers exhibited the highest activity against AChE and BuChE with IC50 values of 17.56 and#177; 1.0 g/mL and 326.23 and#177; 2.6 g /mL (galanthamine 6.8 and#177; 0.5 g /mL and 344.4 and#177; 8.2 g /mL as positive control), respectively. The fractions CK-3 and 4 were showed the highest inhibitory activity against AChE with the IC50 value (6.88 and#177; 0.3 g mL and 7.26 and#177; 0.3 g /mL), the fractions CK-5,6,7 and 8 have indicated potent inhibitory activities by compared with galanthamine, which was used as positive control with IC50 value 6.8 and#177; 0.5 g /mL. Among the fractions obtained from the alkaloidal extract, protoberberine-type alkaloids were exerted the most promising activity against both cholinesterases. The present study was described for the first time the in vitro anticholinesterase activity of Corydalis triternata Zucc. as neuroprotective potential and their metabolite profile by LC-Q-TOF-MS. Besides, the anticholinesterase assays on alkaloidal extract and its fractions showed that protoberberine-type alkaloids were determined the most potent inhibitor against AChE and BuChE.

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Inhibition of Protein Tyrosine Phosphatase 1B by Lutein Derivatives isolated from Mexican Oregano (Lippia graveolens)

Phytothérapie ◽

10.3166/phyto-2018-0074 ◽

2018 ◽

Vol 17 (3) ◽

pp. 134-139

Author(s):

R.M. Perez-Gutierrez

Keyword(s):

Protein Tyrosine Phosphatase ◽

Inhibitory Activity ◽

Spectroscopic Data ◽

Methanol Extract ◽

Tyrosine Phosphatase ◽

Positive Control ◽

Protein Tyrosine Phosphatase 1B ◽

Protein Tyrosine ◽

Ic50 Value ◽

Ic50 Values

Methanol extract from Lippia graveolens (Mexican oregano) was studied in order to identify inhibitory bioactives for protein tyrosine phosphatase 1B (PTP1B). Known flavone as lutein (1), and another flavone glycoside such as lutein-7-o-glucoside (2), 6-hydroxy-lutein-7-ohexoside (3) and lutein-7-o-ramnoide (4) were isolated from methanol extract of aerial parts of the Lippia graveolens. All isolates were identified based on extensive spectroscopic data analysis, including UV, IR, NMR, MS and compared with spectroscopic data previously reported. These flavones were evaluated for PTP1B inhibitory activity. Among them, compounds 1 and 3 displayed potential inhibitory activity against PTP1B with IC50 values of 7.01 ± 1.25 μg/ml and 18.4 μg/ml, respectively. In addition, compound 2 and 4 showed moderate inhibitory activity with an IC50 value of 23.8 ± 6.21 and 67.8 ± 5.80 μg/ml respectively. Among the four compounds, luteolin was found to be the most potent PTP1B inhibitor compared to the positive control ursolic acid, with an IC50 value of 8.12 ± 1.06 μg/ml. These results indicate that flavonoids constituents contained in Lippia graveolens can be considered as a natural source for the treatment of type 2 diabetes.

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Synthesis and Structure−Activity Relationship Studies of N-monosubstituted Aroylthioureas as Urease Inhibitors

Medicinal Chemistry ◽

10.2174/1573406416999200818152440 ◽

2020 ◽

Vol 16 ◽

Author(s):

Wei-Wei Ni ◽

Hai-Lian Fang ◽

Ya-Xi Ye ◽

Wei-Yi Li ◽

Li Liu ◽

...

Keyword(s):

Regression Analysis ◽

Mammalian Cells ◽

Intact Cell ◽

Linear Regression Analysis ◽

Positive Control ◽

Acetohydroxamic Acid ◽

Urease Inhibitors ◽

Ic50 Value ◽

Ic50 Values ◽

Low Cytotoxicity

Background: Thiourea is a classical urease inhibitor usually as a positive control, and many N,N`-disubstituted thioureas have been determined as urease inhibitors. However, due to steric hindrance, N,N`-disubstituted thiourea motif could not bind urease as thiourea. On the contrary, N-monosubstituted thioureas with a tiny thiourea motif could theoretically bind into the active pocket as thiourea. Objective: A series of N-monosubstituted aroylthioureas were designed and synthesized for evaluation as urease inhibitors. Methods: Urease inhibition was determined by the indophenol method and IC50 values were calculated using computerized linear regression analysis of quantal log dose-probit functions. The kinetic parameters were estimated viasurface plasmon resonance (SPR) and by nonlinear regression analysis based on the mixed type inhibition model derived from Michaelis-Menten kinetics. Results: Compounds b2, b11and b19 reversibly inhibited urease with a mixed mechanism, and showed excellent potency against both cell-free urease and urease in intact cell, with IC50 values being 90-to 450-fold and 5-to 50-fold lower than the positive control acetohydroxamic acid, respectively. The most potent compound b11 showed IC50 value of 0.060 ±0.004μM against cell-free urease, which bound to urea binding site with a very low KDvalue (0.420±0.003nM) and a very long residence time (6.7 min). Compound b11was also demonstrated having very low cytotoxicity to mammalian cells. Conclusion: These results revealed that N-monosubstituted aroylthioureas clearly bind the active site of urease as expected, and represent a new class of urease inhibitors for the development of potential therapeutics against infections caused by ure-ase-containing pathogens.

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Evaluating the Effect of Cinnarizine on Promastigotes and Amastigotes forms of Leishmania major

Infectious Disorders - Drug Targets ◽

10.2174/1871526518666181113114820 ◽

2020 ◽

Vol 20 (4) ◽

pp. 550-555 ◽

Cited By ~ 1

Author(s):

Lima Asgharpour Sarouey ◽

Parvaneh Rahimi-Moghaddam ◽

Fatemeh Tabatabaie ◽

Khadijeh Khanaliha

Keyword(s):

Flow Cytometry ◽

Cutaneous Leishmaniasis ◽

Leishmania Major ◽

Inhibitory Effect ◽

Control Group ◽

Secondary Infections ◽

Ic50 Values ◽

J774 Cells ◽

Mtt Assays

: As an important global disease, cutaneous leishmaniasis is associated with complications such as secondary infections and atrophic scars. The first line treatment with antimonials is expensive and reported to have serious side effects and enhance resistance development. The main objective of this study was to evaluate the effect of Cinnarizine on standard strains of Leishmania major because of paucity of information on this subject. Methods: In this experimental study, four concentrations of the drug (5, 10, 15 and 20 μg/ml) were added to Leishmania major cultures at 24, 48 and 72 hours intervals. MTT assays were performed to determine parasite viability and drug toxicity. Leishmania major promastigotes were augmented to the in vitro cultured macrophages (J774 cells) and then incubated for 72 hours. Half maximal inhibitory concentration (IC50) was ascertained by counting parasites. The inhibitory effect of the drug was compared with that of Glucantime. Flow-cytometry was performed to investigate apoptosis. Each test was repeated thrice. Results: The IC50 values of Cinnarizine after 72 hours were calculated to be 34.76 μg/ml and 23.73 μg/ml for promastigotes and amastigotes, respectively. The results of MTT assays showed 48 % promastigote viability after 72 hour-exposure to Cinnarizine at 20 μg/ml concentration. Programmed cell death in promastigote- and amastigote-infected macrophages was quantified to be 13.66 % and 98.7 %, respectively. Flow- cytometry analysis indicated that Cinnarizine induced early and late apoptosis in parasites. All treatments produced results which differed significantly from control group (P<0.05). Conclusion: Cinnarizine showed low toxicity with anti-leishmanial and apoptosis effects on both promastigote and intracellular amastigote forms. Therefore, we may suggest further assessment on animal models of this drug as candidates for cutaneous leishmaniasis therapy.

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In vitro cytotoxicity of Aspilia pluriseta Schweinf. extract fractions

BMC Research Notes ◽

10.1186/s13104-021-05472-4 ◽

2021 ◽

Vol 14 (1) ◽

Author(s):

Sospeter N. Njeru ◽

Jackson M. Muema

Keyword(s):

Biological Activities ◽

Vero Cells ◽

In Vitro Cytotoxicity ◽

Root Extract ◽

Lack Of Information ◽

Information Gap ◽

Diphenyltetrazolium Bromide ◽

Potential Use

Abstract Objectives We and others have shown that Aspilia pluriseta is associated with various biological activities. However, there is a lack of information on its cytotoxicity. This has created an information gap about the safety of A. pluriseta extracts. As an extension to our recent publication on the antimicrobial activity and the phytochemical characterization of A. pluriseta root extracts, here we report on cytotoxicity of tested solvent fractions. We evaluated the potential cytotoxicity of these root extract fractions on Vero cell lines by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Results We show that all solvent extract fractions (except methanolic solvent fractions) had cytotoxic concentration values that killed 50% of the Vero cells (CC50) greater than 20 µg/mL and selectivity index (SI) greater than 1.0. Taken together, we demonstrate that, A. pluriseta extract fractions’ earlier reported bioactivities are within the acceptable cytotoxicity and selective index limits. This finding scientifically validates the potential use of A. pluriseta in the discovery of safe therapeutics agents.

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Characterization and selective inhibition of myristoyl-CoA:protein N-myristoyltransferase from Trypanosoma brucei and Leishmania major

Biochemical Journal ◽

10.1042/bj20051886 ◽

2006 ◽

Vol 396 (2) ◽

pp. 277-285 ◽

Cited By ~ 46

Author(s):

Chrysoula Panethymitaki ◽

Paul W. Bowyer ◽

Helen P. Price ◽

Robin J. Leatherbarrow ◽

Katherine A. Brown ◽

...

Keyword(s):

Trypanosoma Brucei ◽

Leishmania Major ◽

Homo Sapiens ◽

Selective Inhibition ◽

Fungal Species ◽

Chemotherapeutic Agents ◽

Human Pathogens ◽

Ic50 Values

The eukaryotic enzyme NMT (myristoyl-CoA:protein N-myristoyltransferase) has been characterized in a range of species from Saccharomyces cerevisiae to Homo sapiens. NMT is essential for viability in a number of human pathogens, including the fungi Candida albicans and Cryptococcus neoformans, and the parasitic protozoa Leishmania major and Trypanosoma brucei. We have purified the Leishmania and T. brucei NMTs as active recombinant proteins and carried out kinetic analyses with their essential fatty acid donor, myristoyl-CoA and specific peptide substrates. A number of inhibitory compounds that target NMT in fungal species have been tested against the parasite enzymes in vitro and against live parasites in vivo. Two of these compounds inhibit TbNMT with IC50 values of <1 μM and are also active against mammalian parasite stages, with ED50 (the effective dose that allows 50% cell growth) values of 16–66 μM and low toxicity to murine macrophages. These results suggest that targeting NMT could be a valid approach for the development of chemotherapeutic agents against infectious diseases including African sleeping sickness and Nagana.

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Study on α-glucosidase inhibitory activity of 40 kinds of vegetables, tubers, and fruits in An Giang

Vietnam Journal of Science Technology and Engineering ◽

10.31276/vjste.63(4).42-46 ◽

2021 ◽

Vol 63 (4) ◽

pp. 42-46

Author(s):

Thi-My-Linh Lam ◽

◽

Minh-Tuan Le ◽

Manh-Ha Bui ◽

◽

...

Keyword(s):

Glycine Max ◽

Inhibitory Activity ◽

Positive Control ◽

Syzygium Cumini ◽

Inhibition Rate ◽

Ic50 Value ◽

Areca Catechu ◽

Ic50 Values

A study on the α-glucosidase inhibitory activity of 40 kinds of vegetables, tubers, and fruits found in the An Giang province was conducted. The results indicated that all 40 extracted samples displayed α-glucosidase inhibitory activity at a concentration of 250 μg ml-1, 36 extracted samples showed an inhibition rate greater than 50% at 250 μg ml-1, 25 extracted samples had over 50% at 100 μg ml-1, 17 extracted samples possessed more than 50% at 50 μg ml-1, 7 extracted samples sampled showed over 50% at 25 μg ml-1, 5 extracted samples were greater than 50% at 10 μg ml-1, and 1 extracted sample was greater than 50% at 1 μg ml-1. Among the 40 samples, those taken from the seeds of Areca catechu, the fruits of Cassia grandis, the fruits of Syzygium cumini, the seeds of Glycine max,andthe stems of Enydra fluctuansexhibited the strongest α-glucosidase inhibitory activity in methanol, with IC50 values of 0.15, 2.54, 4.05, 5.17 and 8.68 μg ml-1, respectively, which were stronger than the positive control acarbose with an IC50 value of 214.5 μg ml-1

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Synthesis and Biological Evaluation of Novel 4-Phenylaminobenzofuro[2,3-d]pyrimidine Derivatives

Journal of the chemical society of pakistan ◽

10.52568/000659 ◽

2020 ◽

Vol 42 (4) ◽

pp. 564-564

Author(s):

Ju liu Ju liu ◽

Jun Li Jun Li ◽

Jian tao Shi Jian tao Shi ◽

Jie Li Jie Li ◽

Xue chen Hao Xue chen Hao ◽

...

Keyword(s):

Cell Lines ◽

A549 Cells ◽

Positive Control ◽

Biological Evaluation ◽

Dependent Manner ◽

Pyrimidine Derivatives ◽

Concentration Dependent Manner ◽

Ic50 Value ◽

Synthesis And Biological Evaluation

A series of novel 4-phenylaminobenzofuro[2,3-d]pyrimidine derivatives had been prepared and assessed for their in vitro antiproliferative activities against three lung cancer cell lines (A549, H460 and H1975). The bioassay results showed most of the designed compounds exhibited potential antiproliferation activities. Among them, compound 8f exhibited remarkable inhibitory activity against A549 and H460 cell lines with IC50 value of 2.54 μM and 2.68 μM, respectively, which was comparable to that of the positive control sorafenib (IC50 = 2.69 μM for A549 and 3.71 μM for H460). AO/EB staining suggests that compound 8f could induce apoptosis in A549 cells. Furthermore, cell cycle analyses show that compound 8f increased G0/G1 A549 cells arrest in a concentration-dependent manner. The preliminary structure-activity relationships (SARs) studies indicated that mono-electron-withdrawing groups (mono-EWGs) on the phenyl ring are positive on the antitumor activity.

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Homoadamantane and Adamantane Acylphloroglucinols from Hypericum hirsutum

Planta Medica ◽

10.1055/a-1617-7573 ◽

2021 ◽

Author(s):

Julianna Max ◽

Jörg Heilmann

Keyword(s):

Petroleum Ether Extract ◽

2D Nmr ◽

Positive Control ◽

Ionization Mass ◽

2D Nmr Spectroscopy ◽

Vitro Assay ◽

Ionization Mass Spectroscopy ◽

Ic50 Values ◽

Adamantane Skeleton

Abstract 1H NMR-guided fractionation of the petroleum ether extract of the aerial parts from Hypericum hirsutum yielded to the isolation of 19 polyprenylated polycyclic acylphloroglucinols. Structure elucidation based on 1D and 2D NMR spectroscopy together with high-resolution electrospray ionization mass spectroscopy revealed 14 acylphloroglucinols with a homoadamantane scaffold (1–14), while 5 further compounds showed an adamantane skeleton (15–19). Except for hookerione C (15), all isolated metabolites are hitherto unknown. While structurally-related metabolites have been isolated from other Hypericum species, it is the first report of admantan and homoadamantan type acylphloroglucinols in section Taeniocarpium Jaub. & Spach (Hypericaceae). The isolated compounds have been tested in a crystal violet-based in vitro assay on their properties to reduce the proliferation of human microvascular endothelial cells compared to hyperforin as the positive control. They showed a moderate reduction of proliferation with IC50 values in the range ~ 3 – 22 µM, with the homoadamantane-based compounds 2 and 4 being the most active. In addition, inhibition of the TNF-α-induced ICAM-1 expression was determined for 1 – 5, 7, and 10 – 12. Substances 3 and 12 reduced the ICAM-1 expression significantly (to 46.7% of control for 3, 62.3% for 12, at 50 µM).

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COMPARATIVE EVALUATION OF IN VITRO ANTIOXIDANT AND IN VIVO HEPATOPROTECTIVE ACTIVITIES OF ETHANOLIC LEAF AND ROOT EXTRACTS OF CLEOME GYNANDRA

INDIAN DRUGS ◽

10.53879/id.56.04.11629 ◽

2019 ◽

Vol 56 (04) ◽

pp. 50-56

Author(s):

K Ravishankar ◽

Y.V.V.M. Lakshmi Prasanna ◽

G.V.N. Kiranmayi ◽

Keyword(s):

Carbon Tetrachloride ◽

Hepatoprotective Activity ◽

Root Extract ◽

Serum Glutamic Oxaloacetic Transaminase ◽

Root Extracts ◽

Cleome Gynandra ◽

Ic50 Values ◽

Ethanolic Leaf Extract

In vitro antioxidant and in vivo hepatoprotective activities of Cleome gynandra ethanolic leaf and root extracts were assessed. In vitro antioxidant activity was carried by DPPH, Nitric oxide, hydroxyl radical and phosphomolybdenum assays. Hepatoprotective activity was evaluated by Carbon tetrachloride (CCl4) induced hepatotoxicity in albino rats.The animals were divided into seven groups (Four test groups - Ethanolic Leaf and Root Extracts of Cleome gynandra of 100 mg/kg and 200 mg/kg, standard silymarin (100 mg/kg), toxic control-carbon tetrachloride and vehicle). On the eight day, the blood was collected and parameters like serum glutamic oxaloacetic transaminase (SGOT), Serum glutamic pyruvic transaminase (SGPT), Alkaline phosphatase (ALP) and Total bilirubin (TB) were estimated. Significant antioxidant status with good IC50 values similar to standard ascorbic acid was obtained. A significant decrease in liver enzymes was observed in test groups comparable to silymarin. From the results obtained, ethanolic leaf extract has contributed better hepatoprotection compared with root extract in experimental rats.

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