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.

Inactive Publication Date: 2020-04-10
BIONOOX SA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Pentavalent antimony-containing agents have a high incidence of side effects
However, this class of compounds has non-negligible toxicity to host organisms, which hinders their therapeutic applications

Method used

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  • Compositions for use for treating cutaneous leishmaniasis
  • Compositions for use for treating cutaneous leishmaniasis
  • Compositions for use for treating cutaneous leishmaniasis

Examples

Experimental program
Comparison scheme
Effect test

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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PUM

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Abstract

The invention relates to the use of a composition comprising dihydroquercetin, alpha-tocopherol, and optionally bisabolol and / or a compound of formula (I) for use in the treatment of leishmaniasis, especially cutaneous leishmaniasis. The invention further relates to the use of such a composition for treating inflammation induced by leishmaniasis, especially cutaneous leishmaniasis. The invention also relates to a method for treating leishmaniasis, especially cutaneous leishmaniasis, and / or the associated inflammation by administering an effective amount of a composition comprising dihydroquercetin, bisabolol, alpha-tocopherol and optionally bisabolol and / or a compound of formula (I) to a subject in need thereof.

Description

technical field [0001] The present invention is in the field of treatment of leishmaniasis, in particular cutaneous leishmaniasis. [0002] In particular, the present invention relates to a composition comprising dihydroquercetin and alpha-tocopherol for the treatment of leishmaniasis, in particular for the topical treatment of cutaneous leishmaniasis. The composition of the invention may also comprise bisabolol and / or a compound of formula (I), such as ethyl 3-(2-chloroacetamido)benzoate or ethyl 4-(2-chloroacetamido)benzoate . [0003] The present invention also relates to a method of treating a subject in need thereof infected with a leishmaniasis parasite, said method comprising administering to said subject a composition comprising dihydroquercetin and alpha-tocopherol . Background technique [0004] Leishmaniasis is a parasitic disease transmitted by the bite of an infected sandfly. Leishmaniasis is endemic in 88 countries in Africa, Asia, Europe, and North and Sou...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/351A61K31/045A61P33/02A61K31/355A61K31/245
CPCA61K31/045A61K31/245A61K31/355A61P33/02Y02A50/30A61K31/351A61K2300/00
Inventor E·斯塔尔科曼
Owner BIONOOX SA
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