Compositions for use for treating cutaneous leishmaniasis
A leishmaniasis and composition technology, applied in the field of cutaneous leishmaniasis, can solve the problems of high incidence of side effects of pentavalent antimony-containing agents, hindering therapeutic application, host biological toxicity, etc.
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Embodiment 1
[0277] Embodiment 1: the composition of the present invention application
[0278] The composition comprising DHQ (dihydroquercetin), bisabolol, optionally alpha-tocopherol and a cosmetically and pharmaceutically acceptable carrier (oil-in-water emulsion) is given in Table 1 below.
[0279] Table 1
[0280]
[0281] The oil-in-water emulsion used as carrier in the composition of Table 1 had the following composition:
[0282] water;
[0283] sweet almond oil;
[0284] Caprylic / capric triglycerides;
[0285] Olus oil;
[0286] avocado oil;
[0287] ethanol;
[0288] cetearyl alcohol;
[0289] Dioctyl ether;
[0290] glycerin;
[0291] Propylene glycol;
[0292] Sorbitol;
[0293] Glyceryl Stearate;
[0294] Glyceryl Citrate Stearate;
[0295] Polyglyceryl-3 Methyl Glucose Distearate;
[0296] xanthan gum;
[0297] Sodium dehydroacetate;
[0298] sodium benzoate;
[0299] phenoxyethanol; and
[0300] citric acid.
Embodiment 2
[0301] Embodiment 2: Anti-Leishmania activity in vitro
[0302] The anti-Leishmania activities of dihydroquercetin, ethyl 3-(2-chloroacetamido)benzoate and bisabolol were evaluated.
[0303] Compounds were evaluated for direct microbicidal action against Leishmania parasites in infected macrophages and neutrophils.
[0304] Bone marrow-derived macrophages (BMDM) were cultured for 7 days, collected, and infected with Leishmania major mCherry for 2 hours. Non-phagocytosed parasites were then washed away and dihydroquercetin, ethyl 3-(2-chloroacetamido)benzoate or bisabolol were added at different concentrations and incubated at different time points.
[0305] - Evaluation of parasiticidal efficacy by flow cytometry and microscopy.
[0306] - NO production was assessed by Griess reaction of the supernatant.
[0307] Neutrophils were isolated by magnetic activated cell sorting (MACS) and infected with Leishmania major mCherry at a multiplicity of infection (MOI) of 1:10.
[...
Embodiment 3
[0313] Example 3: In Vitro Toxicity Evaluation of Individual Components
[0314] with dihydroquercetin (5, 15 and 25 μM), ethyl 3-(2-chloroacetamido)benzoate (1, 2 and 4 μM) and bisabolol (0.05%, 0.1% and 0.5% w / v) Incubate for 24 hours, stain with DAPI, and assess neutrophil viability by flow cytometry.
[0315] Dihydroquercetin and bisabolol showed no cytotoxicity.
[0316] However, ethyl 3-(2-chloroacetamido)benzoate resulted in decreased neutrophil viability at the concentrations evaluated.
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