scholarly journals In Vitro Schistosomicidal Activity of the Alkaloid-Rich Fraction from Ruta graveolens L. (Rutaceae) and Its Characterization by UPLC-QTOF-MS

2019 ◽  
Vol 2019 ◽  
pp. 1-8 ◽  
Author(s):  
Lara Soares Aleixo de Carvalho ◽  
Lucas Sales Queiroz ◽  
Ismael José Alves Junior ◽  
Ayla das Chagas Almeida ◽  
Elaine Soares Coimbra ◽  
...  
Keyword(s):  
Folk Medicine ◽  
Peritoneal Macrophages ◽  
Antileishmanial Activity ◽  
Parasitic Infections ◽  
Leishmania Braziliensis ◽  
Ruta Graveolens ◽  
Active Fraction ◽  
Ms Analysis ◽  
First Time

Schistosomiasis is a neglected tropical disease that affects million people worldwide, mostly in developing countries. Ruta graveolens (Rutaceae) is a plant used in folk medicine to treat several diseases, including parasitic infections. In this study, we reported the in vitro schistosomicidal activity of the R. graveolens extract (Rg) and its active fraction (Rg-FAE). Also, the characterization of Rg-FAE by UPLC-ESI-QTOF-MS analysis and its in vitro antileishmanial activity against Leishmania braziliensis were also performed. In vitro schistosomicidal assays were assessed against adult worms of S. mansoni, while cell viability against peritoneal macrophages was measured by MTT assay. Rg (100 μg/mL) exhibited noticeable schistosomicidal activity, causing 100% mortality and decreasing motor activity of all adult male and female schistosomes, but with low activity against L. braziliensis. After chromatographic fractionation of Rg, fraction Rg-FAE was obtained, showing high activity against adult schistosomes. UPLC-ESI-QTOF-MS analysis of Rg-FAE revealed the presence of eleven alkaloids and one furanocoumarin. No significant antileishmanial activity was found for Rg, while Rg-FAE exhibited activity against L. braziliensis promastigotes. We demonstrated, for the first time, that the R. graveolens extract (Rg) and its alkaloid-rich fraction (Rg-FAE) are active against adult worms of S. mansoni, with no significant cytotoxicity on macrophages. Our findings open the route to further antiparasitic studies with the active fraction of R. graveolens and its identified compounds, especially alkaloids.

Naphthoquinones and derivatives for chemotherapy: perspectives and limitations of their anti-trypanosomatids activities

2020 ◽  
Vol 26 ◽  
Author(s):  
Luíza Dantas-Pereira ◽  
Edézio F. Cunha-Junior ◽  
Valter V. Andrade-Neto ◽  
John F. Bower ◽  
Guilherme A. M. Jardim ◽  
...  
Keyword(s):  
Large Scale ◽  
Neglected Tropical Diseases ◽  
Folk Medicine ◽  
Leishmania Species ◽  
Parasitic Infections ◽  
Mechanistic Analysis ◽  
Leishmania Spp ◽  
Nanomolar Range

: Chagas disease, Sleeping sickness and Leishmaniasis, caused by trypanosomatids Trypanosoma cruzi, Trypanosoma brucei and Leishmania spp., respectively, are considered neglected tropical diseases, and they especially affect impoverished populations in the developing world. The available chemotherapies are very limited and a search for alternatives is still necessary. In folk medicine, natural naphthoquinones have been employed for the treatment of a great variety of illnesses, including parasitic infections. This review is focused on the anti-trypanosomatid activity and mechanistic analysis of naphthoquinones and derivatives. Among all the series of derivatives tested in vitro, naphthoquinone-derived 1,2,3-triazoles were very active on T. cruzi infective forms in blood bank conditions, as well as in amastigotes of Leishmania spp. naphthoquinones containing a CF3 on a phenyl amine ring inhibited T. brucei proliferation in the nanomolar range, and naphthopterocarpanquinones stood out for their activity on a range of Leishmania species. Some of these compounds showed a promising selectivity index (SI) (30 to 1900), supporting further analysis in animal models. Indeed, high toxicity to the host and inactivation by blood components are crucial obstacles to be overcome to use naphthoquinones and/or their derivatives for chemotherapy. Multidisciplinary initiatives embracing medicinal chemistry, bioinformatics, biochemistry, and molecular and cellular biology need to be encouraged to allow the optimization of these compounds. Large scale automated tests are pivotal for the efficiency of the screening step, and subsequent evaluation of both the mechanism of action in vitro and pharmacokinetics in vivo are essential for the development of a novel, specific and safe derivative, minimizing adverse effects.

scholarly journals GC-MS Investigation of Amaryllidaceae Alkaloids in Galanthus xvalentinei nothosubsp. subplicatus

2013 ◽  
Vol 8 (3) ◽  
pp. 1934578X1300800
Author(s):  
Buket Bozkurt Sarikaya ◽  
Strahil Berkov ◽  
Jaume Bastida ◽  
Gulen Irem Kaya ◽  
Mustafa Ali Onur ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Anticholinesterase Activity ◽  
Amaryllidaceae Alkaloids ◽  
Acetylcholinesterase Inhibitory Activity ◽  
Aerial Parts ◽  
Ms Analysis ◽  
Ellman’S Method ◽  
First Time

A GC-MS analysis of alkaloids in the aerial parts and bulbs of Galanthus x valentinei nothosubsp. subplicatus was performed for the first time. Totally, twenty-six alkaloids were identified, of which tazettine and galanthindole were the major ones. Acetylcholinesterase inhibitory activity of the alkaloidal extracts was determined using modified in vitro Ellman's method. Significant anticholinesterase activity was observed in the tested samples (bulbs: IC50 = 21.3 μg/mL, aerial parts: IC50 = 16.3 μg/mL).

In Vitro Human Dihydroorotate Dehydrogenase Inhibitory, Anti-inflammatory and Cytotoxic Activities of Alkaloids from the Seeds of Nigella glandulifera

Planta Medica ◽  
2018 ◽  
Vol 84 (14) ◽  
pp. 1013-1021 ◽  
Author(s):  
Jun-Bo Gao ◽  
Xing-Jie Zhang ◽  
Rui-Han Zhang ◽  
Li-Li Zhu ◽  
De-Bing Pu ◽  
...  
Keyword(s):  
Folk Medicine ◽  
Positive Control ◽  
Cytotoxic Activities ◽  
Dihydroorotate Dehydrogenase ◽  
X Ray Diffraction ◽  
Ic50 Values ◽  
Pharmacologically Active ◽  
Pharmacologically Active Compounds ◽  
First Time

AbstractFour new dolabellane-type diterpene alkaloids, glandulamines A – D (1 – 4), together with twelve known compounds (5 – 16), were isolated from the seeds of Nigella glandulifera using repeated column chromatography and semipreparative HPLC. The structures of 1 – 16 were elucidated based on NMR data analysis, HRMS experiments and other spectroscopic interpretations. The absolute configuration of 5 was determined by single-crystal X-ray diffraction data for the first time. Compounds 10 and 12 showed human dihydroorotate dehydrogenase inhibitory activity with IC50 values of 61.1 ± 5.3 and 45.9 ± 3.0 µM, respectively. Molecular docking of the active compound 12 and positive control teriflunomide on the inhibitor-binding site of human dihydroorotate dehydrogenase was subsequently performed to visualize the interaction pattern. In addition, compounds 8 and 10 exhibited inhibitory effects against lipopolysaccharide-induced nitric oxide production with inhibition rates of 61 and 41%, respectively, at the concentration of 10 µM. Compounds 9 and 12 showed cytotoxic activities with cell viability varying from 29 ~ 57% at 100 µM against T98G, U87, U251, and GL261 glioma cancer cell lines. These data provide new insights on the pharmacologically active compounds of this plant widely used in folk medicine.

scholarly journals Novel Arsenic Nanoparticles Are More Effective and Less Toxic than As (III) to Inhibit Extracellular and Intracellular Proliferation ofLeishmania donovani

2014 ◽  
Vol 2014 ◽  
pp. 1-10 ◽  
Author(s):  
Sudipta Chakraborty ◽  
Kaushik Bhar ◽  
Sandip Saha ◽  
Rajarshi Chakrabarti ◽  
Anjali Pal ◽  
...  
Keyword(s):  
Leishmania Donovani ◽  
Protozoan Parasite ◽  
Antileishmanial Activity ◽  
Macrophage Cell Line ◽  
Macrophage Cell ◽  
Vector Borne ◽  
First Time ◽  
Intracellular Proliferation ◽  
Mouse Macrophage Cell Line

Visceral leishmaniasis, a vector-borne tropical disease that is threatening about 350 million people worldwide, is caused by the protozoan parasiteLeishmania donovani. Metalloids like arsenic and antimony have been used to treat diseases like leishmaniasis caused by the kinetoplastid parasites. Arsenic (III) at a relatively higher concentration (30 μg/mL) has been shown to have antileishmanial activity, but this concentration is reported to be toxic in several experimental mammalian systems. Nanosized metal (0) particles have been shown to be more effective than their higher oxidation state forms. There is no information so far regarding arsenic nanoparticles (As-NPs) as an antileishmanial agent. We have tested the antileishmanial properties of the As-NPs, developed for the first time in our laboratory. As-NPs inhibited thein vitrogrowth, oxygen consumption, infectivity, and intramacrophage proliferation ofL. donovaniparasites at a concentration which is about several fold lower than that of As (III). Moreover, this antileishmanial activity has comparatively less cytotoxic effect on the mouse macrophage cell line. It is evident from our findings that As-NPs have more potential than As (III) to be used as an antileishmanial agent.

scholarly journals Design, synthesis and biological evaluation of N-oxide derivatives with potent in vivo antileishmanial activity

PLoS ONE ◽  
2021 ◽  
Vol 16 (11) ◽  
pp. e0259008
Author(s):  
Leandro da Costa Clementino ◽  
Guilherme Felipe Santos Fernandes ◽  
Igor Muccilo Prokopczyk ◽  
Wilquer Castro Laurindo ◽  
Danyelle Toyama ◽  
...  
Keyword(s):  
Parasite Burden ◽  
Peritoneal Macrophages ◽  
Biological Evaluation ◽  
Antileishmanial Activity ◽  
Dual Effect ◽  
Design Synthesis ◽  
Murine Peritoneal Macrophages ◽  
Synthesis And Biological Evaluation

Leishmaniasis is a neglected disease that affects 12 million people living mainly in developing countries. Herein, 24 new N-oxide-containing compounds were synthesized followed by in vitro and in vivo evaluation of their antileishmanial activity. Compound 4f, a furoxan derivative, was particularly remarkable in this regard, with EC50 value of 3.6 μM against L. infantum amastigote forms and CC50 value superior to 500 μM against murine peritoneal macrophages. In vitro studies suggested that 4f may act by a dual effect, by releasing nitric oxide after biotransformation and by inhibiting cysteine protease CPB (IC50: 4.5 μM). In vivo studies using an acute model of infection showed that compound 4f at 7.7 mg/Kg reduced ~90% of parasite burden in the liver and spleen of L. infantum-infected BALB/c mice. Altogether, these outcomes highlight furoxan 4f as a promising compound for further evaluation as an antileishmanial agent.

scholarly journals In vitro anticancer potential and GC-MS analysis of Drimia nagarjunae, an endangered medicinal plant

2015 ◽  
Vol 10 (2) ◽  
pp. 303 ◽  
Author(s):  
Narendranath Alluri ◽  
Mala Majumdar
Keyword(s):  
Ethyl Acetate ◽  
Anticancer Activity ◽  
Human Colon ◽  
Human Colon Cancer ◽  
Ms Analysis ◽  
Endangered Medicinal Plant ◽  
Colon Cancer Cell Lines ◽  
Total Growth ◽  
First Time

<p>The aim of the present study was to investigate the anticancer activity of <em>Drimia nagarjunae</em> (Liliaceae) extracts against Colo205 human colon cancer cell lines by SRB assay for the first time. The bulbs and leaves of the plant were sequentially extracted using solvents with increasing polarities (hexane&gt; chloroform&gt;ethyl acetate&gt;methanol&gt;water). Ethyl acetate and chloroform bulb extracts showed potent anticancer activity compared to standard, adriamycin. Both the extracts exhibited total growth inhibition of cell at 20.1 µg/mL and 32.1 µg/mL whereas adriamycin shown 33.1 µg/mL and 50% lethal concentration was found to be 61.5 µg/mL and &gt;80 µg/mL respectively. The active extracts were subjected to GC-MS analysis for identification of phytocompounds and it showed seven and ten major compounds respectively. Therefore, the present study demonstrated that <em>D. nagarjunae</em> can be a promising candidate as an anticancer agent.</p><p> </p>

Secondary metabolites of Helichrysum plicatum DC. subsp. plicatum flowers as strong carbonic anhydrase, cholinesterase and α-glycosidase inhibitors

2020 ◽  
Vol 75 (5-6) ◽  
pp. 153-159
Author(s):  
Tuba Aydin
Keyword(s):  
Secondary Metabolites ◽  
Carbonic Anhydrase ◽  
Folk Medicine ◽  
Inhibitory Effect ◽  
Glycosidase Inhibitors ◽  
Meoh Extract ◽  
Chemical Structures ◽  
Liquid Chromatography Tandem Mass ◽  
First Time

AbstractHelichrysum plicatum species are used in Turkish folk medicine as lithagogue, diuretic, and nephritic. Research on the methanol (MeOH) extract of flowers of H. plicatum DC. subsp. plicatum resulted in the isolation of eight known compounds (1–8). The chemical structures of the compounds were determined as β-sitosterol (1), apigenin (2), nonacosanoic acid (3), astragalin (4), β-sitosterol-3-O-β-D-glucopyranoside (5), helichrysin A (6), helichrysin B (7), and isosalipurposide (8) by spectroscopic and chromatographic/spectrometric methods, including 1D and 2D nuclear magnetic resonance and liquid chromatography-tandem mass spectrometry. Nonacosanoic acid (3) was isolated for the first time from H. plicatum DC. subsp. plicatum. The MeOH extract and isolated compounds were evaluated for their in vitro human carbonic anhydrase I (hCAI) and II (hCAII), acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and α-glycosidase inhibitory activities. The IC50 values of H. plicatum DC. subsp. plicatum MeOH extract for hCAI, hCAII, AChE, BChE, and α-glycosidase were found to be 77.87, 52.90, 115.50, 117.46, and 81.53 mg/mL, respectively. The compounds showed IC50 values of 1.43–4.47, 1.40–4.32, 1.69–2.90, 1.09–3.89, and 1.61–3.80 μM against hCAI, hCAII, AChE, BChE, and α-glycosidase, respectively. In summary, H. plicatum DC. subsp. plicatum secondary metabolites demonstrated strong inhibitory effects especially against hCAI and hCAII, whereas the MeOH extract showed a weak inhibitory effect on all enzymes.

scholarly journals Oleuropein-Rich Leaf Extract as a Broad Inhibitor of Tumour and Macrophage iNOS in Apc Mutant Rat Model

2021 ◽  
Author(s):  
Jessica Ruzzolini ◽  
Sofia Chiccoli ◽  
Noemi Monaco ◽  
Silvia Peppicelli ◽  
Elena Andreucci ◽  
...  
Keyword(s):  
Peritoneal Macrophages ◽  
Leaf Extracts ◽  
Inos Activity ◽  
Anti Cancer ◽  
Inflammatory State ◽  
Anti Inflammatory ◽  
First Time ◽  
Mutant Rat

Abstract: Oleuropein, the major compound of olive leaves, has been reported to exert numerous pharmacological properties, including anti-inflammatory, antidiabetic and anticancer. The purpose of this study is to evaluate, for the first time, the effect of oleuropein-rich leaf extracts (ORLE) in already-developed colon tumours colon tumours arising in an Apc (adenomatous polyposis coli) mutated PIRC rats (F344/NTac-Apcam1137). Here, we were able to investigate in parallel the anti-cancer effect of ORLE, both in vivo and in vitro, and its anti-inflammatory effect on macrophages, which represents a critical and abundant population in most solid tumours microenvironment. We found that in vivo ORLE treatment promoted apoptosis and attenuated iNOS activity both in colon tumours as in peritoneal macrophages of PIRC rats. We confirmed in vitro using primary RAW264.7 cells: ORLE reduced iNOS activity in parallel with COX-2 and pro-inflammatory cytokines, such as IL-1, IL-6 and TGF-. These findings suggest that ORLE possess a strong anti-inflammatory activity, which could be crucial for dampening the pro-tumourigenic activity elicited by a chronic inflammatory state generated by either tumour cells or tumour-associated macrophages.

scholarly journals (+)-Spectaline, a Piperidine Alkaloid from Senna spectabilis DC. Effective in Reducing the In Vitro Infection of Leishmania major

2016 ◽  
Vol 3 ◽  
pp. 1-8
Author(s):  
Amyra Amat Sain ◽  
Azimah Amanah ◽  
Zuriati Zahari ◽  
Roshan Jahn Mohd Salim ◽  
Sharif Mahsufi Mansor ◽  
...  
Keyword(s):  
Ethyl Acetate ◽  
Leishmania Major ◽  
Ethyl Acetate Extract ◽  
Folk Medicine ◽  
2D Nmr ◽  
Selectivity Index ◽  
Antileishmanial Activity ◽  
Solvent Fractionation ◽  
Senna Spectabilis

Senna spectabilisis known to have antimicrobial, laxative, antiulcerogenic, analgesic, and anti-inflammatory properties in folk medicine. Piperidine alkaloids extracted from various parts of this plant have been shown to have anticonvulsant (iso-6-spectaline), antinociceptive [(-)-spectaline] and lipid peroxidation [(+)-3-O-feruloylcassine, (-)-spectaline and (-)-3-O-acetylspectaline] activities. In our study, the ethyl acetate extract fromS. spectabilisexhibited antileishmanial activity via intracellular promastigote assay or leishmanicidal assay and was further fractionated by using bioassay-guided isolation approach. The antiprotozoal principle was isolated from the ethyl acetate portion through solvent fractionation and a few series of chromatographic processes. The isolated active compound 1 was identified as (+)-spectaline on the basis of its spectral analysis (MS, 1D & 2D NMR) with EC50value of 0.063 ± 0.005 µM for antileishmanial activity and selectivity index of 3.76.

scholarly journals In Vitro Antileishmanial Activity and GC-MS Analysis of Whole Plant Hexane Fraction of Achillea wilhelmsii (WHFAW)

2019 ◽  
Vol 2019 ◽  
pp. 1-26
Author(s):  
Jahangir Khan Achakzai ◽  
Muhammad Anwar Panezai ◽  
Abdul Manan Kakar ◽  
Basira Akhtar ◽  
Ali Akbar ◽  
...  
Keyword(s):  
Leishmania Major ◽  
Inhibitory Concentration ◽  
Antileishmanial Activity ◽  
Hexane Fraction ◽  
Aqueous Fraction ◽  
Ms Analysis ◽  
Whole Plant ◽  
Vector Borne ◽  
Achillea Wilhelmsii

In this study, GC-MS analysis has shown that whole plant hexane fraction of Achillea wilhelmsii (WHFAW) consists of 66 compounds which exhibited antileishmanial activity. Antileishmanial bioassay was the method used for determining antileishmanial activity. The inhibitory concentration (IC50) which was observed for whole plant hexane fraction of Achillea wilhelmsii (WHFAW) against parasitic and vector-borne disease, leishmaniasis, is 58.27 ± 0.52 μg/mL. For leishmanicidal assay, Leishmania major is the species used for analysis. Whole plant methanol extract of Achillea wilhelmsii (WMEAW) and whole plant aqueous fraction of Achillea wilhelmsii (WAFAW) exhibited no antileishmanial activity.

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