ABSTRACT
ABSTRACT The geopropolis produced by the stingless bee Melipona subnitida (popularly called "jandaíra" in Brazil) is a mixture of resin, wax, and mud. This study analyzed the antifungal activity of the geopropolis extract from Candida spp., developed a gel formulation with this extract and analyzed the delivery of bioactives (kinetics release) in the formulation and their chemical profile by UHPLC-PDA-qTOF-MS/MS. Three different gels were prepared using the geopropolis extract, carbomer, propylene glycol, and water. Formulations with different amounts of propylene glycol were investigated. Physical, visual, pH, viscosity, adhesion, spreadability, leakage, and in vitro release tests were performed in the proposed formulations. Antifungal tests with the geopropolis ethanolic extract were carried out against six Candida species. The chemical profile of the geopropolis extract and compounds released from the formulations were analyzed after the release test. The formulations had a pH between 4.6 and 4.8 and viscosity between 535,600 and 920,400 cPs. The geopropolis extract presented excellent antifungal activity against the tested yeasts. The results of the release test in semipermeable cellulose membrane showed that all formulations containing 5%, 10% and 40% propylene glycol presented release of geopropolis extract. For adhesion and leakage tests, the gel formulation with 5% propylene glycol was more effective. Both geopropolis ethanolic extract and the liquid obtained in the release test showed the presence of flavonoids (flavonol/flavone, flavanone, and chalcones). Gel formulations with geopropolis extract that are rich in flavonoids are promising as an adjuvant treatment of vaginal candidiasis.
ABSTRACT
Abstract A bioassay-guided fractionation of two samples of Brazilian red propolis (from Igarassu, PE, Brazil, hereinafter propolis 1 and 2) was conducted in order to determine the components responsible for its antimicrobial activity, especially against Candida spp. Samples of both the crude powdered resin and the crude ethanolic extract of propolis from both locations inhibited the growth of all 12 tested Candida strains, with a minimum inhibitory concentration of 256 µg/mL. The hexane, acetate and methanol fractions of propolis 1 also inhibited all strains with minimum inhibitory concentration values ranging from 128 to 512 µg/mL for the six bacteria tested and from 32 to 1024 µg/mL for the yeasts. Similarly, hexane and acetate fractions of propolis sample 2 inhibited all microorganisms tested, with minimum inhibitory concentration values of 512 µg/mL for bacteria and 32 µg/mL for yeasts. The extracts were analyzed by HPLC and their phenolic profile allowed us to identify and quantitate one phenolic acid and seven flavonoids in the crude ethanolic extract. Formononetin and pinocembrin were the major constituents amongst the identified compounds. Formononetin was detected in all extracts and fractions tested, except for the methanolic fraction of sample 2. The isolated isoflavone formononetin inhibited the growth of all the microorganisms tested, with a minimum inhibitory concentration of 200 µg/mL for the six bacteria strains tested and 25 µg/mL for the six yeasts. Formononetin also exhibited fungicidal activity against five of the six yeasts tested. Taken together our results demonstrate that the isoflavone formononetin is implicated in the reported antimicrobial activity of red propolis.
Subject(s)
Anti-Infective Agents/pharmacology , Candida/drug effects , Isoflavones/isolation & purification , Isoflavones/pharmacology , Propolis/chemistry , Anti-Infective Agents/isolation & purification , Brazil , Bacteria/drug effects , Chemical Fractionation , Chromatography, High Pressure Liquid , Microbial Sensitivity TestsABSTRACT
Teratogenicity and developmental abnormalities in the offspring of female rats that ingested ethanol extract of Neem plants during pregnancy and lactation period were assessed. Twenty-four female Wistar rats were randomly distributed in control group and in three experimental groups and treated during the 4th, 5th, and 6th day of pregnancy. After birth, the lactating females received, by gavage, 65, 135 and 200 mg kg-1 of Neem ethanol extract, during 15 days. Results show, there was no significant difference in body mass index of neonatal rats in the 4 groups evaluated, whereas mean rate of offspring survival was 79.4%. Hair growth, incisor teeth eruption, ear detachment, eyelid opening, and spontaneous ambulation were similar for all groups. Likewise, physical development and development of motor activity, ambulation, and postural reflexes were similar for all groups. The administration of Neem ethanol extract did not cause any reproductive or systemic toxicity in animals. Results show that, Neem ethanol extract safe at doses 65, 135 and 200 mg kg-1 in pregnant or lactating rats.
Teratogenicidade e anormalidades no desenvolvimento de proles de ratas que ingeriram o extrato etanólico de folhas de nim durante a gestação e lactação foram avaliadas. Vinte e quatro ratas Wistar foram distribuídas aleatoriamente em um grupo controle e três grupos experimentais tratados no quarto, quinto e sexto dias de gestação. Após o nascimento, as fêmeas lactantes receberam através de gavagem, o extrato etanólico de nim nas doses de 65, 135 e 200 mg kg-1 durante 15 dias. Nenhuma diferença significativa foi observada em relação ao índice de massa corpórea das fêmeas em lactação nos grupos em todos os momentos e a taxa média de sobrevivência dos filhotes foi de 79,4%. O tempo de crescimento piloso, erupção dos dentes incisivos, descolamento de orelha, abertura palpebral e deambulação espontânea foram semelhantes em todos os grupos. O desenvolvimento físico e da atividade motora, deambulação e reflexos posturais foram semelhantes em todos os grupos. A administração não resultou em toxicidade reprodutiva ou sistêmica. Os resultados mostraram que o extrato etanólico do nim é seguro para uso nas doses de 65, 135 e 200mg kg-1 em ratas prenhes ou em lactação.
Subject(s)
Rats , Azadirachta , Plants, Medicinal , Reproduction , TeratogensABSTRACT
Phytochemical investigation of the aerial parts of S. paludosum afforded 3,4,7,8-tetramethyl gossypetinr, 3,7- dimethyl kaempferol, 3-methyl kaempferol, 3-methyl apigenin, and 3-methyl quercetin ethers, besides N-p-transcoumaroyltiramine, and protocatecuid acid. The structures were established from spectral data of the natural substances and the permethyl and acetyl derivatives of tetramethyl gossypetin.