scholarly journals Chemical Constituents with Leishmanicidal Activity from a Pink-Yellow Cultivar of Lantana camara var. aculeata (L.) Collected in Central Mexico

2019 ◽  
Vol 20 (4) ◽  
pp. 872 ◽  
Author(s):  
Ronna Delgado-Altamirano ◽  
Rosa López-Palma ◽  
Lianet Monzote ◽  
José Delgado-Domínguez ◽  
Ingeborg Becker ◽  
...  
Keyword(s):  
Chemical Constituents ◽  
Lantana Camara ◽  
New Drugs ◽  
Significant Activity ◽  
Leishmanicidal Activity ◽  
Lead Compounds ◽  
Tiglic Acid ◽  
Organic Extracts ◽  
Bioassay Guided Fractionation

Lantana camara (L.) is employed by several ethnical groups to treat numerous diseases. Although there are no ethnomedical reports on its use against leishmaniasis, organic extracts prepared from L. camara were shown to display leishmanicidal activity. In the present study, we carried out a bioassay-guided fractionation of the dichloromethane extract from Mexican L. camara in order to identify the compounds responsible for the leishmanicidal activity. Eighteen chromatographic fractions (FI–FXVIII) were evaluated in vitro against Leishmania mexicana and L. amazonensis. FII, FX, FXI, FXV, and FXVI showed significant activity against both Leishmania strains, the most potent of which was FXV. Eicosane (1), squalene (2), β-ionone (3), caryophyllene oxide (4), β-caryophyllene (5), hexanoic acid (6), tiglic acid (7), a mixture of lantanilic (8) and camaric (9) acids, and lantadene B (10) were identified and obtained from the active fractions and evaluated for their leishmanicidal activity. The mixture of lantanilic (8) and camaric (9) acids (79%/21%) was the most potent one (half maximal inhibitory concentration (IC50) = 12.02 ± 0.36 μM). This study indicates that this cultivar of L. camara has high potential for the development of phytomedicines or as a source of natural products, which might represent lead compounds for the design of new drugs against leishmaniasis.

Antiparasitic efficacy of Gracillin and Zingibernsis newsaponin from Costus speciosus (Koen ex. Retz) Sm. against Ichthyophthirius multifiliis

Parasitology ◽  
2014 ◽  
Vol 142 (3) ◽  
pp. 473-479 ◽  
Author(s):  
WEI ZHENG ◽  
CHUN-MEI YAN ◽  
YA-BIN ZHANG ◽  
ZE-HONG LI ◽  
ZHONGQIANG LI ◽  
...  
Keyword(s):  
New Drugs ◽  
Ichthyophthirius Multifiliis ◽  
Active Components ◽  
Antiparasitic Activity ◽  
Lead Compounds ◽  
Costus Speciosus ◽  
Bioassay Guided Fractionation ◽  
Median Effective Concentration

SUMMARYThe present study aims to evaluate the antiparasitic activity of active components from Costus speciosus against Ichthyophthirius multifiliis. Bioassay-guided fractionation was employed to identify active compounds from C. speciosus yielding 2 bioactive compounds: Gracillin and Zingibernsis newsaponin. In-vitro assays revealed that Gracillin and Zingibernsis newsaponin could be 100% effective against I. multifiliis at concentrations of 0·8 and 4·5 mg L−1, with median effective concentration (EC50) values of 0·53 and 3·2 mg L−1, respectively. All protomonts and encysted tomonts were killed when the concentrations of Gracillin and Zingibernsis newsaponin were 1·0 and 5·0 mg L−1. In-vivo experiments demonstrated that fish treated with Gracillin and Zingibernsis newsaponin at concentrations of 1·0 and 5·0 mg L−1 carried significantly fewer parasites than the control (P<0·05). Mortality of fish did not occur in the treatment group (Zingibernsis newsaponin at 5·0 mg L−1) during the trial, although 100% of untreated fish died. Acute toxicities (LD50) of Gracillin and Zingibernsis newsaponin for grass carp were 1·64 and 20·7 mg L−1, respectively. These results provided evidence that the 2 compounds can be selected as lead compounds for the development of new drugs against I. multifiliis.

scholarly journals Bengamides display potent activity against drug-resistant Mycobacterium tuberculosis

2019 ◽  
Vol 9 (1) ◽  
Author(s):  
Diana H. Quan ◽  
Gayathri Nagalingam ◽  
Ian Luck ◽  
Nicholas Proschogo ◽  
Vijaykumar Pillalamarri ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
New Drugs ◽  
Bioactive Molecules ◽  
Aminopeptidase Activity ◽  
Drug Resistant ◽  
Lead Compounds ◽  
New Class ◽  
Tb Treatment ◽  
Bioassay Guided Fractionation

Abstract Mycobacterium tuberculosis infects over 10 million people annually and kills more people each year than any other human pathogen. The current tuberculosis (TB) vaccine is only partially effective in preventing infection, while current TB treatment is problematic in terms of length, complexity and patient compliance. There is an urgent need for new drugs to combat the burden of TB disease and the natural environment has re-emerged as a rich source of bioactive molecules for development of lead compounds. In this study, one species of marine sponge from the Tedania genus was found to yield samples with exceptionally potent activity against M. tuberculosis. Bioassay-guided fractionation identified bengamide B as the active component, which displayed activity in the nanomolar range against both drug-sensitive and drug-resistant M. tuberculosis. The active compound inhibited in vitro activity of M. tuberculosis MetAP1c protein, suggesting the potent inhibitory action may be due to interference with methionine aminopeptidase activity. Tedania-derived bengamide B was non-toxic against human cell lines, synergised with rifampicin for in vitro inhibition of bacterial growth and reduced intracellular replication of M. tuberculosis. Thus, bengamides isolated from Tedania sp. show significant potential as a new class of compounds for the treatment of drug-resistant M. tuberculosis.

scholarly journals Leismanicidal Activity of Propolis Collected in the Semiarid Region of Brazil

2021 ◽  
Vol 12 ◽  
Author(s):  
Giani Maria Cavalcante ◽  
Celso Amorim Camara ◽  
Eva Monica Sarmento Da Silva ◽  
Mariana Silva Santos ◽  
Anderson Brandão Leite ◽  
...  
Keyword(s):  
Cytotoxic Effect ◽  
Ethanolic Extract ◽  
Ultra Performance Liquid Chromatography ◽  
Semiarid Region ◽  
Array Detector ◽  
Significant Activity ◽  
Exact Mass ◽  
Leishmanicidal Activity ◽  
Etoh Extract

Objective: The aim of the current study is to investigate the chemical composition, cytotoxic effect, and leishmanicidal activity of propolis collected in the semi-arid region of Bahia, Brazil.Methods: EtOH extract, hexane, EtOAc and MeOH fractions from propolis were analyzed by ultra-performance liquid chromatography coupled with diode array detector and quadrupole time-of-flight mass spectrometry. The identification was based on the exact mass, general fragmentation behaviors and UV absorption of the flavonoids. The in vitro cytotoxic effect and leishmanicidal activity of ethanolic extract, hexane, ethyl acetate, and methanolic fractions of propolis were evaluated.Results: Five triterpenes and twenty-four flavonoids were identified. The propolis did not present toxicity to the host cell up to the maximum concentration tested. In addition, all tested samples showed statistically significant activity against promastigotes of Leishmania chagasi and Leishmania amazonensis. Regarding the activity against amastigote forms of L. amazonensis, the hexane fraction, presented statistically significant activity with IC50 of 1.3 ± 0.1 μg/ml.Conclusion: The results support the idea that propolis can be used for future antileishmania studies.

scholarly journals In vitro Antiprotozoal Activity of Extracts of five Turkish Lamiaceae Species

2011 ◽  
Vol 6 (11) ◽  
pp. 1934578X1100601 ◽  
Author(s):  
Hasan Kirmizibekmez ◽  
Irem Atay ◽  
Marcel Kaiser ◽  
Erdem Yesilada ◽  
Deniz Tasdemir
Keyword(s):  
Trypanosoma Brucei ◽  
Leishmania Donovani ◽  
Hexane Extract ◽  
Significant Activity ◽  
Trypanosoma Brucei Rhodesiense ◽  
L6 Cells ◽  
Methanolic Extracts ◽  
Aerial Parts ◽  
Organic Extracts

The in vitro antiprotozoal activities of crude methanolic extracts from the aerial parts of five Lamiaceae plants ( Salvia tomentosa, S. sclarea, S. dichroantha, Nepeta nuda subsp. nuda and Marrubium astracanicum subsp. macrodon) were evaluated against four parasitic protozoa, i.e. Trypanosoma brucei rhodesiense, T. cruzi, Leishmania donovani and Plasmodium falciparum. The cytotoxic potentials of the extracts on L6 cells were also evaluated. Melarsoprol, benznidazole, miltefosine, chloroquine and podophyllotoxin were used as reference drugs. All crude MeOH extracts showed antiprotozoal potential against at least three parasites, so they were dispersed in water and partitioned against n-hexane and chloroform to yield three subextracts that were screened in the same test systems. The n-hexane extract of N. nuda was the most active against T. brucei rhodesiense while the CHCl3 extracts of S. tomentosa and S. dichroantha showed significant activity against L. donovani. All organic extracts displayed in vitro antimalarial and moderate trypanocidal activities against T. cruzi with the n-hexane extract of S. sclarea being the most active against the latter. The extracts displayed low or no cytotoxicity towards mammalian L6 cells.

scholarly journals Trypanocidal Essential Oils: A Review

Molecules ◽  
2020 ◽  
Vol 25 (19) ◽  
pp. 4568 ◽  
Author(s):  
Mayara Castro de Morais ◽  
Jucieudo Virgulino de Souza ◽  
Carlos da Silva Maia Bezerra Filho ◽  
Silvio Santana Dolabella ◽  
Damião Pergentino de Sousa
Keyword(s):  
Experimental Data ◽  
Natural Products ◽  
Essential Oils ◽  
Therapeutic Potential ◽  
Chemical Constituents ◽  
Mechanisms Of Action ◽  
New Drugs ◽  
Important Group

Trypanosomiases are diseases caused by parasitic protozoan trypanosomes of the genus Trypanosoma. In humans, this includes Chagas disease and African trypanosomiasis. There are few therapeutic options, and there is low efficacy to clinical treatment. Therefore, the search for new drugs for the trypanosomiasis is urgent. This review describes studies of the trypanocidal properties of essential oils, an important group of natural products widely found in several tropical countries. Seventy-seven plants were selected from literature for the trypanocidal activity of their essential oils. The main chemical constituents and mechanisms of action are also discussed. In vitro and in vivo experimental data show the therapeutic potential of these natural products for the treatment of infections caused by species of Trypanosoma.

scholarly journals Synthesis and in vitro leishmanicidal activity of novel [1,2,3]triazolo[1,5-a]pyridine salts

RSC Advances ◽  
2017 ◽  
Vol 7 (26) ◽  
pp. 15715-15726 ◽  
Author(s):  
Álvaro Martín-Montes ◽  
Rafael Ballesteros-Garrido ◽  
Rubén Martín-Escolano ◽  
Clotilde Marín ◽  
Ramón Guitiérrez-Sánchez ◽  
...  
Keyword(s):  
New Drugs ◽  
Leishmanicidal Activity

Leishmaniasis remains a significant worldwide problem; it is of great interest to develop new drugs to fight this disease.

scholarly journals Functionalization of the Chalcone Scaffold for the Discovery of Novel Lead Compounds Targeting Fungal Infections

Molecules ◽  
2019 ◽  
Vol 24 (2) ◽  
pp. 372 ◽  
Author(s):  
Francesca Bonvicini ◽  
Giovanna Gentilomi ◽  
Francesca Bressan ◽  
Silvia Gobbi ◽  
Angela Rampa ◽  
...  
Keyword(s):  
Biofilm Formation ◽  
Antifungal Agents ◽  
Fungal Infections ◽  
Infection Process ◽  
New Drugs ◽  
Added Value ◽  
Yeast Growth ◽  
Candida Spp ◽  
Lead Compounds

The occurrence of invasive fungal infections represents a substantial threat to human health that is particularly serious in immunocompromised patients. The limited number of antifungal agents, devoid of unwanted toxic effects, has resulted in an increased demand for new drugs. Herein, the chalcone framework was functionalized to develop new antifungal agents able to interfere with cell growth and with the infection process. Thus, a small library of chalcone-based analogues was evaluated in vitro against C. albicans ATCC 10231 and a number of compounds strongly inhibited yeast growth at non-cytotoxic concentrations. Among these, 5 and 7 interfered with the expression of two key virulence factors in C. albicans pathogenesis, namely, hyphae and biofilm formation, while 28 emerged as a potent and broad spectrum antifungal agent, enabling the inhibition of the tested Candida spp. and non-Candida species. Indeed, these compounds combine two modes of action by selectively interfering with growth and, as an added value, weakening microbial virulence. Overall, these compounds could be regarded as promising antifungal candidates worthy of deeper investigation. They also provide a chemical platform through which to perform an optimization process, addressed at improving potency and correcting liabilities.

scholarly journals Identification of Multi-Target Anti-AD Chemical Constituents From Traditional Chinese Medicine Formulae by Integrating Virtual Screening and In Vitro Validation

2021 ◽  
Vol 12 ◽  
Author(s):  
Baoyue Zhang ◽  
Jun Zhao ◽  
Zhe Wang ◽  
Pengfei Guo ◽  
Ailin Liu ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Chinese Medicine ◽  
Traditional Chinese Medicine ◽  
Virtual Screening ◽  
Cell Model ◽  
Chemical Constituents ◽  
New Drugs ◽  
Molecular Docking Study ◽  
Biological Validation

Alzheimer’s disease (AD) is a neurodegenerative disease that seriously threatens the health of the elderly. At present, no drugs have been proven to cure or delay the progression of the disease. Due to the multifactorial aetiology of this disease, the multi-target-directed ligand (MTDL) approach provides an innovative and promising idea in search for new drugs against AD. In order to find potential multi-target anti-AD drugs from traditional Chinese medicine (TCM) formulae, a compound database derived from anti-AD Chinese herbal formulae was constructed and predicted by the anti-AD multi-target drug prediction platform established in our laboratory. By analyzing the results of virtual screening, 226 chemical constituents with 3 or more potential AD-related targets were collected, from which 16 compounds that were predicted to combat AD through various mechanisms were chosen for biological validation. Several cell models were established to validate the anti-AD effects of these compounds, including KCl, Aβ, okadaic acid (OA), SNP and H2O2 induced SH-SY5Y cell model and LPS induced BV2 microglia model. The experimental results showed that 12 compounds including Nonivamide, Bavachromene and 3,4-Dimethoxycinnamic acid could protect model cells from AD-related damages and showed potential anti-AD activity. Furthermore, the potential targets of Nonivamide were investigated by molecular docking study and analysis with CDOCKER revealed the possible binding mode of Nonivamide with its predicted targets. In summary, 12 potential multi-target anti-AD compounds have been found from anti-AD TCM formulae by comprehensive application of computational prediction, molecular docking method and biological validation, which laid a theoretical and experimental foundation for in-depth study, also providing important information and new research ideas for the discovery of anti-AD compounds from traditional Chinese medicine.

scholarly journals Impact of the Interaction of R207910 with Rifampin on the Treatment of Tuberculosis Studied in the Mouse Model

2008 ◽  
Vol 52 (10) ◽  
pp. 3568-3572 ◽  
Author(s):  
Nacer Lounis ◽  
Tom Gevers ◽  
Joke Van Den Berg ◽  
Koen Andries
Keyword(s):  
Mouse Model ◽  
Kinetic Studies ◽  
Bactericidal Effect ◽  
New Drugs ◽  
Significant Activity ◽  
Bacterial Clearance ◽  
Background Regimen ◽  
The Difference ◽  
The Impact

ABSTRACT New drugs are needed to shorten the duration of tuberculosis treatment. R207910, a diarylquinoline, is very active against Mycobacterium tuberculosis both in vitro and in mice. In healthy volunteers, the coadministration of R207910 and rifampin induced the increased metabolism of R207910, resulting in a 50% reduction in the level of R207910 exposure. We assessed the impact of reducing the dose of R207910 on its efficacy when R207910 was combined with a background regimen of isoniazid, rifampin, and pyrazinamide. Addition of 25 mg/kg of body weight or 12.5 mg/kg R207910 to the background regimen resulted in faster bacterial clearance and culture negativity. The difference in efficacy between the two doses was not statistically significant. The minimal bactericidal dose of R207910 when it was tested as part of the combination was identical to that when it was tested as monotherapy. Because of the drug-drug interaction in humans, the activity of R207910 in humans could be less than that expected from studies with mice. Our data from the mouse model demonstrate that R207910 has significant activity, even when its exposure is reduced by 50% and when it is added to a strong background regimen of isoniazid, rifampin, and pyrazinamide. In killing kinetic studies, the bactericidal effect of R207910 in mice was modest during the first week of treatment, but it increased in the following 3 weeks, while the bactericidal activity of isoniazid was limited to the first week of treatment.

scholarly journals Design, Synthesis and Antifungal Activity of Novel Benzoylcarbamates Bearing a Pyridine Moiety

2018 ◽  
Vol 8 (12) ◽  
pp. 2577
Author(s):  
Fu-Xian Wan ◽  
Jian-Hua Wang ◽  
Yan-Hua Shi ◽  
Li-Zhi Niu ◽  
Lin Jiang
Keyword(s):  
Antifungal Activity ◽  
High Efficiency ◽  
Plant Diseases ◽  
Moderate Activity ◽  
Significant Activity ◽  
Environmental Friendliness ◽  
Design Synthesis ◽  
Lead Compounds ◽  
Pyridine Moiety

Many natural and synthetic pyridine derivatives have good biological activity, and are widely used in the fields of pesticides and medicines. On the other hand, carbamate fungicides possess some unique properties, such as high efficiency, strong selectivity, low toxicity, and environmental friendliness, and are often used to control many plant diseases. Therefore, discovering novel pyridine-based carbamates is of great significance. In this paper, we chose the excellent fungicides tolprocarb and picarbutrazox as lead compounds, integrating benzoyl, carbamate, and pyridinyl moieties into a molecule. Thus, we designed and synthesized a series of substituted benzoyl carbamates containing a pyridine ring, and evaluated the in vitro antifungal activity. The target compounds exhibited moderate to strong bioactivity against Botrytis cinerea, among which the compounds 4d, 4f, 4g, and 4h exhibited significant activity with EC50 values (the concentration resulting in a 50% inhibition) of 6.45–6.98 μg/mL, and their activities were near or superior to that of chlorothalonil. Additionally, 4h exhibited moderate activity against Sclerotinia sclerotiorumwith an EC50 value of 10.85 μg/mL.

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