Abstract:Background: Leishmaniasis is a complex protozoa disease caused by Leishmania genus (Trypanosomatidae family). Currently, there have been renewed interests worldwide in plants as pharmaceutical agents. In this study, the in vivo efficacy of Solanum spp. is assessed in an L. amazonensis BALB/c mice model for experimental cutaneous leishmaniasis. Methods: Animals were infected with 5 × 106 metacyclic promastigotes and 30-day post-infection, a treatment with 30 mg/kg of Solanum extracts or Glucantime® (GTM) was ap… Show more
“…While several reports have demonstrated the leishmanial efficacy of Glucantime ® in vivo, herein we did not observe reductions in parasite load in our in vivo murine model of L. amazonensis. However, our data does corroborate previous reports detailing the ineffectiveness of Glucantime ® in reducing parasite load in L. amazonensis-infected BALB/c mice inoculated in the ear or footpad (Cos et al, 2018;Cavalcanti de Queiroz et al, 2019;Valentim Silva et al, 2020). Furthermore, it is important to highlight the divergent results in the scientific literature regarding important issues, such as dosage, quantity of inoculated Leishmania (10 5 -10 7 ), and the model of cutaneous leishmaniasis employed (ear pinna, hind footpad or tail base), all of which may influence disease severity and outcome, as well as pharmacologic response (Loeuillet et al, 2016;Paladi et al, 2017;Coelho et al, 2016;Kauffmann et al, 2018).…”
Leishmaniasis is a widespread group of neglected vector-borne tropical diseases that possess serious therapeutic limitations. Propolis has been extensively used in traditional medical applications due to its range of biological effects, including activity against infectious agents. Here we evaluated the leishmanicidal and immunomodulatory properties of Brazilian green propolis extract (EPP-AF®) and a gel formulation incorporating EPP-AF®, in both in vitro and in vivo models of Leishmania amazonensis infection. Propolis extract, obtained from a standardized blend following hydroalcoholic extraction, showed the characteristic fingerprint of Brazilian green propolis as confirmed by HPLC/DAD. A carbopol 940 gel formulation was obtained containing propolis glycolic extract at 3.6% w/w. The release profile, assessed using the Franz diffusion cell protocol, demonstrated a gradual and prolonged release of p-coumaric acid and artepillin C from the carbomer gel matrix. Quantification of p-coumaric acid and artepillin C in the gel formulation over time revealed that p-coumaric acid followed the Higuchi model, dependent on the disintegration of the pharmaceutical preparation, while artepillin C followed a zero-order profile with sustained release. In vitro analysis revealed the ability of EPP-AF® to reduce the infection index of infected macrophages (p < 0.05), while also modulating the production of inflammatory biomarkers. Decreases in nitric oxide and prostaglandin E2 levels were observed (p < 0.01), suggesting low iNOS and COX-2 activity. Furthermore, EPP-AF® treatment was found to induce heme oxygenase-1 antioxidant enzyme expression in both uninfected and L. amazonensis-infected cells, as well as inhibit IL-1β production in infected cells (p < 0.01). ERK-1/2 phosphorylation was positively correlated with TNF-α production (p < 0.05), yet no impact on parasite load was detected. In vivo analysis indicated the effectiveness of topical treatment with EPP-AF® gel alone (p < 0.05 and p < 0.01), or in combination with pentavalent antimony (p < 0.05 and p < 0.001), in the reduction of lesion size in the ears of L. amazonensis-infected BALB/c mice after seven or 3 weeks of treatment, respectively. Taken together, the present results reinforce the leishmanicidal and immunomodulatory effects of Brazilian green propolis, and demonstrate promising potential for the EPP-AF® propolis gel formulation as a candidate for adjuvant therapy in the treatment of Cutaneous Leishmaniasis.
“…While several reports have demonstrated the leishmanial efficacy of Glucantime ® in vivo, herein we did not observe reductions in parasite load in our in vivo murine model of L. amazonensis. However, our data does corroborate previous reports detailing the ineffectiveness of Glucantime ® in reducing parasite load in L. amazonensis-infected BALB/c mice inoculated in the ear or footpad (Cos et al, 2018;Cavalcanti de Queiroz et al, 2019;Valentim Silva et al, 2020). Furthermore, it is important to highlight the divergent results in the scientific literature regarding important issues, such as dosage, quantity of inoculated Leishmania (10 5 -10 7 ), and the model of cutaneous leishmaniasis employed (ear pinna, hind footpad or tail base), all of which may influence disease severity and outcome, as well as pharmacologic response (Loeuillet et al, 2016;Paladi et al, 2017;Coelho et al, 2016;Kauffmann et al, 2018).…”
Leishmaniasis is a widespread group of neglected vector-borne tropical diseases that possess serious therapeutic limitations. Propolis has been extensively used in traditional medical applications due to its range of biological effects, including activity against infectious agents. Here we evaluated the leishmanicidal and immunomodulatory properties of Brazilian green propolis extract (EPP-AF®) and a gel formulation incorporating EPP-AF®, in both in vitro and in vivo models of Leishmania amazonensis infection. Propolis extract, obtained from a standardized blend following hydroalcoholic extraction, showed the characteristic fingerprint of Brazilian green propolis as confirmed by HPLC/DAD. A carbopol 940 gel formulation was obtained containing propolis glycolic extract at 3.6% w/w. The release profile, assessed using the Franz diffusion cell protocol, demonstrated a gradual and prolonged release of p-coumaric acid and artepillin C from the carbomer gel matrix. Quantification of p-coumaric acid and artepillin C in the gel formulation over time revealed that p-coumaric acid followed the Higuchi model, dependent on the disintegration of the pharmaceutical preparation, while artepillin C followed a zero-order profile with sustained release. In vitro analysis revealed the ability of EPP-AF® to reduce the infection index of infected macrophages (p < 0.05), while also modulating the production of inflammatory biomarkers. Decreases in nitric oxide and prostaglandin E2 levels were observed (p < 0.01), suggesting low iNOS and COX-2 activity. Furthermore, EPP-AF® treatment was found to induce heme oxygenase-1 antioxidant enzyme expression in both uninfected and L. amazonensis-infected cells, as well as inhibit IL-1β production in infected cells (p < 0.01). ERK-1/2 phosphorylation was positively correlated with TNF-α production (p < 0.05), yet no impact on parasite load was detected. In vivo analysis indicated the effectiveness of topical treatment with EPP-AF® gel alone (p < 0.05 and p < 0.01), or in combination with pentavalent antimony (p < 0.05 and p < 0.001), in the reduction of lesion size in the ears of L. amazonensis-infected BALB/c mice after seven or 3 weeks of treatment, respectively. Taken together, the present results reinforce the leishmanicidal and immunomodulatory effects of Brazilian green propolis, and demonstrate promising potential for the EPP-AF® propolis gel formulation as a candidate for adjuvant therapy in the treatment of Cutaneous Leishmaniasis.
“…Some positive results were obtained with IL-Sb V in a hamster CL model (100 % lesion reduction and no parasites in organs) (Travi, et al, 1993;Yépez, et al,1999); however, no complete cure of CL-infected mice has been documented. Per example, treatment of mice infected with L. (L.) amazonensis, with IL-Sb V 28 mg/kg/day × 5, every 4-5 days resulted in partial parasite burden reduction with no increase in footpad thickness, but not in cure (Cos et al, 2018;Fournet et al, 1996). Differences in numbers of Sb V -IL sessions, dose, site of infection, parasite species, and followup time could explain the different results obtained in this study.…”
Introduction: Intralesional-pentavalent antimonials (IL-SbV) are recommended for simple cutaneous leishmaniasis (CL). Few treatment sessions (1-5) and drug volumes (1-5 ml each), relative to lesion size (LS), are recommended. There is not a validated IL-SbV protocol using doses calculated as mg/kg body weight and administered over a large number of IL-sessions, with small injection volumes. Objective: The study aim was to determine the efficacy of different concentrations of IL-SbV administered in 29 daily sessions of 100 μL each, on CL infected mice. Methods: Leishmania (Viannia) panamensis and L. (V.) braziliensis-infected mice (N = 6) were treated with 150, 50, and 16.6 mgSbV/kg/day x 29 days. Percentage of lesion area reduction, aesthetic and final (no lesions, no parasites) efficacy and effective dose (ED)50 were determined. In vitro-SbV activity against parasites was evaluated for both species. Results: The ED50 values were 72.2 and 66.3 (at the end of treatment), 54.3 and 37.7 (15-days pt.), and 145.3 and 148.6 (60-days pt.) for each species, respectively. Differences were observed between Leishmania species at 15-days pt., but not later. At 60-day pt., IL-SbV-150 mg showed final cure rates of 66.6 % for L. (V.) panamensis and 33.3 % for L. (V.) braziliensis-infected mice. After 15 days pt., lesion reactivation was observed in some “aesthetically cured” mice. Glucantime was not active in in vitro assays. Conclusions: The IL-SbV use with a dose calculated as mg/kg body weight and administered over a large number of IL-sessions, with small injection volumes each day could be effective against L. (V.) panamensis and L. (V.) braziliensis-CL infection. An appropriate SbV-dose (higher than 150 mg/kg/day x less than 29 days) must be evaluated.
“…On a comparative evaluation with synthetic antibiotics, the antibacterial activity of methanol extracts of A. lebbeck and S. seaforthianum was comparable with the synthetic antimicrobial agent's erythromycin and fluconazole. The review of literature revealed that the extracts of A. lebbeck and S. seaforthianum showed antimicrobial, antioxidant, antidiabetic, antimalarial, antiarthritic, and anti-allergic properties [17][18][19][20][21][22][23][24][25][26][27]. Ali et al [17] from Bangladesh evaluated the antimicrobial and antioxidant activity of petroleum ether, ethyl acetate and methanol extracts of A. lebbeck against B. subtilis, S. aureus, V. mimicus, S. typhi, S. dysenteriae, C. arrizae, and A. niger.…”
Objective: The continuous emergence of multidrug resistance bacteria and yeast, and the negative impact of synthetic preservatives have led to an increased interest in the use of plant extracts as alternative antimicrobial agents. In the present investigation, the antimicrobial activity of successive solvent extracts of Albizia lebbeck and Solanum seaforthianum has been evaluated against human pathogenic bacteria and yeast.
Methods: The disc diffusion method was employed for determination of the zone of inhibitions (ZOIs) and twofold broth dilution technique was employed for determination of minimal inhibitory concentrations, and minimal bactericidal/fungicidal concentrations.
Results: Among the successive solvent extracts tested, methanol extracts of both A. lebbeck and S. seaforthianum showed highest antibacterial activity with ZOIs ranged between 10.0 and 20.4 mm at 1 mg/disc followed by ethanol (ZOIs 8.1–17.6 mm). The petroleum ether, toluene, and chloroform extracts showed the least activity. The highest activity was observed against Streptococcus faecalis, whereas the least activity was observed against Pseudomonas aeruginosa.
Conclusion: The broad-spectrum antimicrobial activity of methanol extract of A. lebbeck and S. seaforthianum could be explored as antimicrobial agents for the management of pathogenic bacteria and yeast.
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