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2. Pharmacological assessment of the antineoplastic and immunomodulatory properties of a new spiroindolone derivative (7’,8’-Dimethoxy-1’,3’-dimethyl-1,2,3’,4’-tetrahydrospiro[indole-3,5’-pyrazolo[3,4-c]isoquinolin]-2-one) in chronic myeloid leukemia

Author

de Castro Alves, Carlos Eduardo, Bogza, Serge L., Bohdan, Nathalie, Rozhenko, Alexander B., de Freitas Gomes, Alice, de Oliveira, Regiane Costa, de Azevedo, Renata Galvão, Maciel, Larissa Raquel Silva, Dhyani, Anamika, Grafov, Andriy, and Pontes, Gemilson Soares

Published
2023
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3. The chemical composition and the preservative, antimicrobial, and antioxidant effects of Thymus broussonetii Boiss. essential oil: an in vitro and in silico approach.

Author

Boukhira, Smahane, Amrati, Fatima Ez-Zahra, Chebaibi, Mohamed, Grafov, Andriy, Mothana, Ramzi A., Al-Yousef, Hanan M., Bousta, Dalila, Guo, Yajie, and Baiseitova, Aizhamal

Subjects
THYMES, ANTI-infective agents, ESSENTIAL oils, MOLECULAR docking, GAS chromatography/Mass spectrometry (GC-MS)
Abstract

Introduction: The aim of this study was to evaluate the antioxidant, antimicrobial, and preservative efficacy of Thymus broussonetii Boiss. essential oil (EO) in a topically applied formulation using a challenge test. Methods: The essential oil was extracted from the aerial part of T. broussonetii using hydrodistillation, and the obtained EO was further analyzed by gas chromatography/mass spectrometry (GC/MS). The antioxidant effect of the EO was evaluated using three methods: the inhibition of free radical 2,2-diphenyl-1-picrylhydrazyl (DPPH), βcarotene-linoleic acid, and the ferric reducing antioxidant power (FRAP) methods. The antimicrobial activity and the minimum inhibitory concentration (MIC) of this EO were assayed by the disk-diffusion method and the broth microdilution method, respectively. The preservative efficacy of T. broussonetii EO was assayed at 1% and 2% (v/w) in a topical cream formulation using a challenge test against standard-specific microorganisms recommended by the European Pharmacopoeia. Furthermore, the identified phytochemical compounds were docked for their effect on nicotinamide adenine dinucleotide phosphate oxidase, human casein kinase 1 alpha 1 (CSNK1A1), glycogen synthase kinase 3, Staphylococcus aureus nucleoside diphosphate kinase, Escherichia coli beta-ketoacyl-[acyl-carrier protein] synthase, Pseudomonas aeruginosa LasR ligand-binding domain, and sterol 14-alpha demethylase (CYP51) from Candida albicans. The ADME/toxicity was predicted by analyzing the absorption, distribution, metabolism, and excretion parameters. Results and discussion: chemical composition of the EO revealed the presence of thymol (63.09%), p-cymene (11%), and γ-terpinene (8.99%) as the major components. The antioxidant assays revealed that the essential oil exhibited strong antioxidant activity, as indicated by the minimum inhibitory concentration IC50 (IC50 = 210 ± 0.3 μg/mL for the DPPH assay, IC50 = 145 ± 0.1 μg/mL for the β-carotene assay, and IC50 = 84 ± 0.21 μg/mL for the FRAP assay) when compared to quercetin and butylated hydroxytoluene (BHT) as controls. The investigated essential oil exhibited important antimicrobial activity against all the tested microorganisms, and the MICs of the EO against bacteria and fungi were 0.02%-1%. Moreover, the EO of T. broussonetii evaluated at 2% (v/w) in a cream formulation succeeded in satisfying the A criteria for preservation efficacy against S. aureus, E. coli, and Aspergillus brasiliensis but exhibited less efficacy against P. aeruginosa (1.78 log reduction in the number of CFU/g after 7 days of evaluation) and C. albicans (1.09 log reduction in the number of CFU/g after 14 days of evaluation) when compared to the synthetic preservative phenoxyethanol 1% (v/w). In silico results showed that the antimicrobial activity of T. broussonetii EO is mostly attributed to thymol, terpinen-4-ol, and aromadendrene, while the antioxidant activity is attributed to thymol. These results indicate that the EO of T. broussonetii possesses important antimicrobial and antioxidant properties and can, therefore, be used as a natural preservative ingredient in the cosmetic industry. [ABSTRACT FROM AUTHOR]

Published
2024
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4. A Second Wind for Inorganic APIs: Leishmanicidal and Antileukemic Activity of Hydrated Bismuth Oxide Nanoparticles.

Author

Grafov, Andriy, da Silva Chagas, Ana Flávia, de Freitas Gomes, Alice, Ouedrhiri, Wessal, Cerruti, Pierfrancesco, Del Barone, Maria Cristina, de Souza Mota, Breno, de Castro Alves, Carlos Eduardo, Brasil, Anny Maíza Vargas, Pereira, Antonia Maria Ramos Franco, and Soares Pontes, Gemilson

Subjects
*CUTANEOUS leishmaniasis, *PERITONEAL macrophages, *CYTOTOXINS, *MYELOID leukemia, *BISMUTH trioxide, *LEISHMANIA
Abstract

American cutaneous leishmaniasis is a disease caused by protozoa of the genus Leishmania. Currently, meglumine antimoniate is the first-choice treatment for the disease. The limited efficacy and high toxicity of the drug results in the necessity to search for new active principles. Nanotechnology is gaining importance in the field, since it can provide better efficacy and lower toxicity of the drugs. The present study aimed to synthesize, characterize, and evaluate the in vitro leishmanicidal and antileukemic activity of bismuth nanoparticles (BiNPs). Promastigotes and amastigotes of L. (V.) guyanensis and L. (L.) amazonensis were exposed to BiNPs. The efficacy of the nanoparticles was determined by measurement of the parasite viability and the percentage of infected cells, while the cytotoxicity was characterized by the colorimetry. BiNPs did not induce cytotoxicity in murine peritoneal macrophages and showed better efficacy in inhibiting promastigotes (IC50 < 0.46 nM) and amastigotes of L. (L.) amazonensis. This is the first report on the leishmanicidal activity of Bi-based materials against L. (V.) guayanensis. BiNPs demonstrated significant cytotoxic activity against K562 and HL60 cells at all evaluated concentrations. While the nanoparticles also showed some cytotoxicity towards non-cancerous Vero cells, the effect was much lower compared to that on cancer cells. Treatment with BiNPs also had a significant effect on inhibiting and reducing colony formation in HL60 cells. These results indicate that bismuth nanoparticles have the potential for an inhibitory effect on the clonal expansion of cancer cells. [ABSTRACT FROM AUTHOR]

Published
2024
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7. Corrigendum to Pharmacological effects of Lavandula officinalis Chaix and its polyphenols: Focus on their in vivo estrogenic and anti-inflammatory properties South African Journal of Botany Volume 146, May 2022, Pages 354-364

Author

Slighoua, Meryem, primary, Mahdi, Ismail, additional, Amrati, Fatima ez-zahra, additional, Boucetta, Nabil, additional, Di Cristo, Francesca, additional, Boukhira, Smahane, additional, el Hamsas, Amal El youbi, additional, Tattou, Mohamed Ibn, additional, Grafov, Andriy, additional, Bari, Amina, additional, and Bousta, Dalila, additional

Published
2023
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10. Antileukemic, Antioxidant, Anti-Inflammatory and Healing Activities Induced by a Polyphenol-Enriched Fraction Extracted from Leaves of Myrtus communis L.

Author

Mechchate, Hamza, primary, de Castro Alves, Carlos Eduardo, additional, Es-safi, Imane, additional, Amaghnouje, Amal, additional, Jawhari, Fatima Zahra, additional, Costa de Oliveira, Regiane, additional, de Freitas Gomes, Alice, additional, Conte, Raffaele, additional, Soares Pontes, Gemilson, additional, Bousta, Dalila, additional, and Grafov, Andriy, additional

Published
2022
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12. Chemical Composition, Antioxidant Potentials, and Calcium Oxalate Anticrystallization Activity of Polyphenol and Saponin Fractions from Argania spinosa L. Press Cake

Author

El oumari, Fatima Ezzahra, primary, Mammate, Naima, additional, Imtara, Hamada, additional, Lahrichi, Anissa, additional, Elhabbani, Radouane, additional, El mouhri, Ghita, additional, Alqahtani, Ali S., additional, Noman, Omar M., additional, Ibrahim, Mansour N., additional, Grafov, Andriy, additional, Bousta, Dalila, additional, and Sqalli Houssaini, Tarik, additional

Published
2022
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13. Chemical Composition and Anti-Urolithiatic Activity of Extracts from Argania spinosa (L.) Skeels Press-Cake and Acacia senegal (L.) Willd

Author

El oumari, Fatima Ezzahra, primary, Bousta, Dalila, additional, Imtara, Hamada, additional, Lahrichi, Anissa, additional, Elhabbani, Radouane, additional, El mouhri, Ghita, additional, Al kamaly, Omkulthom, additional, Saleh, Asmaa, additional, Parvez, Mohammad Khalid, additional, Grafov, Andriy, additional, and Sqalli Houssaini, Tarik, additional

Published
2022
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15. Corrigendum to “Assessment of in vivo estrogenic and anti-inflammatory activities of the hydro-ethanolic extract and polyphenolic fraction of parsley (Petroselinum sativum Hoffm.)” [J. Ethnopharmacol. 265 (2021) 113290]

Author

Slighoua, Meryem, primary, Mahdi, Ismail, additional, ez-zahra Amrati, Fatima, additional, Di Cristo, Francesca, additional, Amaghnouje, Amal, additional, Grafov, Andriy, additional, Boucetta, Nabil, additional, Bari, Amina, additional, and Bousta, Dalila, additional

Published
2022
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16. Pharmacological effects of Lavandula officinalis Chaix and its polyphenols: Focus on their in vivo estrogenic and anti-inflammatory properties

Author

Slighoua, Meryem, primary, Mahdi, Ismail, additional, ez-zahra Amrati, Fatima, additional, Boucetta, Nabil, additional, Cristo, Francesca Di, additional, Boukhira, Smahane, additional, El youbi el Hamsas, Amal, additional, Tattou, Mohamed Ibn, additional, Grafov, Andriy, additional, Bari, Amina, additional, and Bousta, Dalila, additional

Published
2022
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17. Modeling interactions between trypanothione and antimony‐oxide clusters.

Author

Rabaâ, Hassan, Grafov, Andriy, and Sundholm, Dage

Subjects
*DENSITY functional theory, *CARBOXYL group, *LEISHMANIASIS, *HYDROXYL group, *HYDROGEN bonding
Abstract

Interactions of antimony‐oxide clusters with trypanothione have been modeled to understand their inhibitory activity against leishmaniasis. Trypanothione is essential for the survival of leishmania parasites because it is responsible for maintaining their cellular thiol‐disulfide redox regulation. Density functional theory calculations show that SbV oxide clusters form hydrogen bonds from the hydroxyl groups to the amine and carboxyl groups of the trypanothione. The reaction between trypanothione and the SbV oxide cluster does not break the SS bond of trypanothione, whereas a reaction between trypanothione and an antimony‐oxide cluster containing one SbIII atom may lead to dissociation of the SS bond of the trypanothione suggesting that antimony‐oxide clusters with at least one SbIII atom can destroy trypanothione that is vital for the parasite metabolism. [ABSTRACT FROM AUTHOR]

Published
2023
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20. Optimized Antibacterial Effects in a Designed Mixture of Essential Oils of Myrtus communis, Artemisia herba-alba and Thymus serpyllum for Wide Range of Applications

Author

Ouedrhiri, Wessal, Mechchate, Hamza, Moja, Sandrine, Baudino, Sylvie, Saleh, Asmaa, Al Kamaly, Omkulthom M., Grafov, Andriy, Greche, Hassane, Department of Chemistry, Doctoral Programme in Drug Research, Doctoral Programme in Chemistry and Molecular Sciences, and Doctoral Programme in Materials Research and Nanosciences

Subjects
mixture design, combination, Chemical technology, BIOLOGICAL-ACTIVITIES, PIPERITA L, 116 Chemical sciences, AROMATIC PLANTS, TP1-1185, METHANOL EXTRACTS, CHEMICAL-COMPOSITION, essential oil, microdilution, antibacterial, VARIABILITY, ANTIOXIDANT, optimal mixture, ANTIBIOTICS, L. ESSENTIAL OILS, ANTIMICROBIAL ACTIVITY
Abstract

Nowadays, the combination of molecules influences their biological effects, and interesting outcomes can be obtained from different component interactions. Using a mixture design method, this research seeks to simulate the efficacy of essential oil combinations against various bacteria and forecast the ideal combination. The chemical compositions of Myrtus communis, Artemisia herba-alba and Thymus serpyllum essential oils were analyzed using CG/MS. Then, the combined antibacterial effects were evaluated by testing mixture design formulations using the microdilution bioassay. The main compounds detected for M. communis essential oil were myrtenyl acetate (33.67%), linalool (19.77%) and 1,8-cineole (10.65%). A. herba-alba had piperitone as a chemotype, representing 85%. By contrast, the T. serpyllum oil contained thymol (17.29%), γ-terpinene (18.31%) and p-cymene (36.15%). The antibacterial effect of the essential oils studied, and the optimum mixtures obtained were target strain-dependent. T. serpyllum alone ensured the optimal inhibition against S. aureus and E. coli, while a ternary mixture consisting of 17.1%, 39.6% and 43.1% of M. communis, A. herba-alba and T. serpyllum respectively, was associated with optimal inhibitory activity against B. subtilis. The outcome of this research supports the idea of the boosting effect of essential oil combinations toward better activities, giving better understanding of the usefulness of mixture designs for food, cosmetics, and pharmaceutical applications.

Published
2022

23. New 2,3-Benzodiazepine Derivative: Synthesis, Activity on Central Nervous System, and Toxicity Study in Mice

Author

Amaghnouje, Amal, Bohza, Serhii, Bohdan, Nathalie, Es-Safi, Imane, Kyrylchuk, Andrii, Achour, Sanae, El Fatemi, Hinde, Bousta, Dalila, Grafov, Andriy, Department of Chemistry, Doctoral Programme in Chemistry and Molecular Sciences, and Doctoral Programme in Materials Research and Nanosciences

Subjects
OPEN-FIELD TEST, BIOCHEMICAL PARAMETERS, AMPA RECEPTORS, MEMORY, 116 Chemical sciences, RECOGNITION, mouse behavioral model, toxicity, central nervous system, Article, RS1-441, MODEL, Pharmacy and materia medica, 317 Pharmacy, Medicine, ANXIETY, DRUG, benzodiazepines, BEHAVIOR
Abstract

We report the design and synthesis of a new diazepine derivative, 4-(4-methoxyphenyl)-2,3,4,5-tetrahydro-2,3-benzodiazepin-1-one (VBZ102), and the evaluation of its anxiolytic-like profile, memory impairment effect, and toxicity in Swiss mice. VBZ102 was evaluated for central nervous system effects in an open field, light-dark box, and novel object recognition tests under oral administration for acute and sub-acute treatment. We tested the VBZ102 toxicity in mice through a determination of LD50 values and examination of the biochemical and histopathological parameters. The VBZ102 induced an anxiolytic effect at different doses both in the light-dark box and open field tests. Unlike other benzodiazepines (e.g., bromazepam), a sedative effect was noted only after administration of the VBZ102 at 10.0 mg/kg.

Published
2021
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31. Caralluma europaea (Guss.) N.E.Br.: Anti-Inflammatory, Antifungal, and Antibacterial Activities against Nosocomial Antibiotic-Resistant Microbes of Chemically Characterized Fractions

Author

Amrati, Fatima Ez-Zahra, primary, Bourhia, Mohammed, additional, Saghrouchni, Hamza, additional, Slighoua, Meryem, additional, Grafov, Andriy, additional, Ullah, Riaz, additional, Ezzeldin, Essam, additional, Mostafa, Gamal A., additional, Bari, Ahmed, additional, Ibenmoussa, Samir, additional, and Bousta, Dalila, additional

Published
2021
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32. Protective Effect of Chemically Characterized Polyphenol-Rich Fraction from Apteranthes europaea (Guss.) Murb. subsp. maroccana (Hook.f.) Plowes on Carbon Tetrachloride-Induced Liver Injury in Mice

Author

Amrati, Fatima Ez-Zahra, primary, Bourhia, Mohammed, additional, Slighoua, Meryem, additional, Boukhira, Smahane, additional, Ullah, Riaz, additional, Ezzeldin, Essam, additional, Mostafa, Gamal A. E., additional, Grafov, Andriy, additional, and Bousta, Dalila, additional

Published
2021
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33. Anxiolytic, Antidepressant-Like Proprieties and Impact on the Memory of the Hydro-Ethanolic Extract of Origanum majorana L. on Mice

Author

Amaghnouje, Amal, primary, Mechchate, Hamza, additional, Es-safi, Imane, additional, Alotaibi, Amal A., additional, Noman, Omar M., additional, Nasr, Fahd A., additional, Al-zharani, Mohammed, additional, Cerruti, Pierfrancesco, additional, Calarco, Anna, additional, EL Fatemi, Hinde, additional, Grafov, Andriy, additional, and Bousta, Dalila, additional

Published
2020
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34. Anacyclus pyrethrum (L): Chemical Composition, Analgesic, Anti-Inflammatory, and Wound Healing Properties

Author

Jawhari, Fatima Zahra, primary, El Moussaoui, Abdelfattah, additional, Bourhia, Mohammed, additional, Imtara, Hamada, additional, Mechchate, Hamza, additional, Es-Safi, Imane, additional, Ullah, Riaz, additional, Ezzeldin, Essam, additional, Mostafa, Gamal A., additional, Grafov, Andriy, additional, Ibenmoussa, Samir, additional, Bousta, Dalila, additional, and Bari, Amina, additional

Published
2020
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35. In-Vivo Antidiabetic Activity and In-Silico Mode of Action of LC/MS-MS Identified Flavonoids in Oleaster Leaves

Author

Mechchate, Hamza, primary, Es-Safi, Imane, additional, Bourhia, Mohammed, additional, Kyrylchuk, Andrii, additional, El Moussaoui, Abdelfattah, additional, Conte, Raffaele, additional, Ullah, Riaz, additional, Ezzeldin, Essam, additional, Mostafa, Gamal A., additional, Grafov, Andriy, additional, Bekkari, Hicham, additional, and Bousta, Dalila, additional

Published
2020
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36. Alkaloids of Abuta panurensis Eichler: In silico and in vitro study of acetylcholinesterase inhibition, cytotoxic and immunomodulatory activities

Author

da Silva Mesquita, Rochelly, primary, Kyrylchuk, Andrii, additional, Costa de Oliveira, Regiane, additional, Costa Sá, Ingrity Suelen, additional, Coutinho Borges Camargo, Gabriel, additional, Soares Pontes, Gemilson, additional, Moura Araújo da Silva, Felipe, additional, Saraiva Nunomura, Rita de Cássia, additional, and Grafov, Andriy, additional

Published
2020
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42. Evaluation of the in vitro antileishmania activity of Tanacetum vulgare (Asteraceae)

Author

Jensen, Bruno Bezerra, Comandolli-Wyrepkowski, Claudia Dantas, Barros, Angela Maria Comapa, Soares, Fabiane Veloso, Grafovac, Iryna, Grafov, Andriy, and Franco, Antonia Maria Ramos

Subjects
lcsh:GE1-350, lcsh:QH540-549.5, food and beverages, lcsh:Ecology, lcsh:Environmental sciences
Abstract

Leishmaniasis is considered a neglected disease. In recent years studies have shown that several plants have activity against these pathogens, serving as the basis for the formulation of herbal medicines or as a target for obtaining active principles against the disease. This study aimed to evaluate the in vitro antileishmania biological activity of the hexanic and methanolic extracts of the flowers and leaves of Tanacetum vulgare against Leishmania amazonensis and L. guyanensis. The flowers and leaves of the plant material were extracted from the hexane and methanolic solvents. The antileishmania activity of T. vulgare extracts was evaluated according to the inhibition of growth and mortality of L. amazonensis and L. guyanensis promastigotes at periods of 24, 48 and 72 h after incubation at 25 oC in the presence of extracts with concentrations of 31.25 to 500 μg.mL-1. The results showed that the extract metanolic of the flower showed activity against L. amazonensis (IC50 = 31.5 μg.mL-1) and L. guyanensis (IC50 < 100 μg.mL-1) in 72 h of incubation. Therefore, it is verified that the methanolic extract of the T. vulgare flower performed better in relation to antileishmania activity, allowing the possibility of future studies to determine its therapeutic efficacy. A Leishmaniose é considerada uma doença negligenciada. Nos últimos anos estudos tem demonstrado que várias plantas possuem atividade contra esses patógenos, servindo de base para a formulação de fitoterápicos ou como alvo para a obtenção de princípios ativos contra a doença. O presente trabalho teve como objetivo avaliar a atividade biológica in vitro antileishmania dos extratos hexânicos e metanólicos das flores e folhas de Tanacetum vulgare em Leishmania amazonensis e Leishmania guyanensis. Foi realizada a extração das flores e folhas do material vegetal a partir dos solventes hexânico e metanólico. As atividades antileishmania dos extratos de T. vulgare foram avaliadas de acordo com a inibição do crescimento e a mortalidade de promastigotas de L. amazonensis e L. guyanensis, nos períodos de 24, 48 e 72 h após incubação a 25 oC na presença dos extratos com concentrações de 500 a 31,25 µg/mL. Os resultados mostraram que o extrato Metanólico da flor apresentou atividade contra L. amazonensis (IC50 de 31,5 µg/mL) e L. guyanensis (IC50 igual à

Published
2017

43. Marketing and legal status of phytomedicines and food supplements in Morocco.

Author

Es-Safi, Imane, Mechchate, Hamza, Amaghnouje, Amal, El Moussaoui, Abdelfattah, Cerruti, Pierfrancesco, Avella, Maurizio, Grafov, Andriy, and Bousta, Dalila

Subjects
DIETARY supplement laws, LEGAL liability, PHYTOCHEMICALS, MARKETING, QUESTIONNAIRES, DESCRIPTIVE statistics, ANXIETY
Abstract

The Phytomedicine (PM) and Food supplements (FS) Market is considerably growing in Morocco a review of state is necessarily to structure and improve it. Information was collected directly from the pharmacist through a questionnaire-based survey who was conducted in 284 pharmacies in the region of Fez-Meknes in Morocco. Data were analyzed and classified using relative frequency of citations (RFC). More than 98% of the pharmacies commercialized the PM and FS, 80% of the pharmacists deny the existence of a real area dedicated to them, the majority (94%) of them prefer phytomedicine rather than classic drugs. This study reported about 64 products as the most used by the population of the region of Fez-Meknes among them 48 FS (75%) and 16 PM (25%) and the most marketed products are used for Transit Disorders (28.34%), then Anxiety (22.17%) and ENT Disease (20.18%). Despite the fact that Morocco is a country where people use medicinal plants daily, the commercialization of the PM and FS is still unstructured. Due to legal problem the PM Sold in the market are mainly exported. To assure development and also valorization of this sector the regulation of this market is highly required. [ABSTRACT FROM AUTHOR]

Published
2021
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44. Topical treatment of experimental cutaneous leishmaniasis in golden hamster (Mesocricetus auratus) with formulations containing pentamidine

Author

COMANDOLLI-WYREPKOWSKI, Claudia Dantas, GRAFOVA, Iryna, NAIFF, Maricleide de Farias, AVELLA, Maurizio, GENTILE, Gennaro, GRAFOV, Andriy, and FRANCO, Antonia Maria Ramos

Subjects
Leishmania, tratamento experimental, modelo animal, topical formulations, formulações tópicas, animal model, experimental treatment, isetionato de pentamidina, pentamidine isethionate
Abstract

Current treatment of cutaneous leishmaniasis (CL) relies mainly on pentavalent antimonials salts and second-line drugs include pentamidine and amphotericin B, but these therapies have side effects and require parenteral administration. The aim of this work was to evaluate the topical formulations containing pentamidine isethionate (PI) in the experimental treatment of cutaneous leishmaniasis (CL). Golden hamsters (Mesocricetus auratus) were infected in the nose with Leishmania (Leishmania) amazonensis. Six treatment groups received different topical treatments of anhydrous or hydrating emulsions, for a maximum of 10 days, with an application of 50 mg day-1. After treatment tissue samples of lesions were evaluated by histology, transmission electron microscopy and biopsy cultivation. Compared with untreated group, topical treatment with hydrating emulsion with 10% PI and usnic acid (ACE5AU) showed significantly decrease in volume lesion (P= 0.028) on 20th day after the end of the treatment with reduction of 27.37%. Topical treatment with anhydrous emulsion with 10% PI and usnic acid (ACPU) reduces parasite burden in Golden hamsters. This study demonstrated the potential of topical treatment to reduce the number of parasites that could be combined with others drugs and to have a faster and more effective treatment of cutaneous leishmaniasis. RESUMO O tratamento atual para Leishmaniose Tegumentar Americana é realizado com antimoniais pentavalentes como tratamento padrão, e as drogas de segunda escolha incluem pentamidina e anfotericina B, mas essas terapias apresentam efeitos colaterais e requerem administração parenteral. O objetivo deste trabalho foi avaliar formulações tópicas contendo isetionato de pentamidina comercial (IP) no tratamento da leishmaniose cutânea experimental (LC). Hamsters dourados foram infectados no focinho com Leishmania (Leishmania) amazonensis. Grupos de seis animais receberam tratamento tópico com cremes anidro ou emulsões hidratantes, num máximo de 10 dias, com aplicação de 50 mg dia-1. Amostras de tecido de lesões tratadas foram avaliadas por histologia, microscopia eletrônica de transmissão (MET) e cultivo de biópsia. Comparado ao grupo sem tratamento, o tratamento tópico com emulsão hidratante com 10% de IP e ácido úsnico (ACE5AU) mostrou diminuição significativa (P=0,028) nas medidas de lesões, 20 dias após o final do tratamento e 27,37% de redução. O tratamento tópico com emulsão anidra com 10% de IP e ácido úsnico (ACPU) mostrou redução da carga parasitária em Golden hamsters. Este estudo demonstrou a possibilidade de utilizar o tratamento tópico para reduzir o número de parasitas e que este poderia ser associado a outras drogas para tratamento mais rápido e eficaz da leishmaniose cutânea.

Published
2017

45. Antileishmanial activity of extracts from Libidibia ferrea: development of in vitro and in vivo tests

Author

COMANDOLLI-WYREPKOWSKI, Claudia Dantas, primary, JENSEN, Bruno Bezerra, additional, GRAFOVA, Iryna, additional, SANTOS, Pierre Alexandre dos, additional, BARROS, Angela Maria Comapa, additional, SOARES, Fabiane Veloso, additional, BARCELLOS, José Fernando Marques, additional, SILVA, Aline Fagundes da, additional, GRAFOV, Andriy, additional, and FRANCO, Antonia Maria Ramos, additional

Published
2017
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