Melipona mondury produces a geopropolis with antioxidant, antibacterial and antiproliferative activities.

Geopropolis is a special type of propolis produced by stingless bees. Several pharmacological properties have been described for different types of geopropolis, but there have been no previous studies of the geopropolis from Melipona mondury. In this study, we investigated the antioxidant, antibacterial, and antiproliferative activities of M. mondury geopropolis, and determined its chemical profile. The antioxidant activity was determined using in vitro ABTS·+, ·DPPH, and ß-carotene/linoleic acid co-oxidation methods. The antibacterial activity was determined using a microdilution method with Pseudomonas aeruginosa, Staphylococcus aureus, and methicillin-resistant S. aureus. The antiproliferative effect was determined in tumor cell lines using the Alamar Blue assay. The chemical profile was obtained using UHPLC-MS and UHPLC-MS/MS. The butanolic fraction had the highest concentration of phenolic compounds and more potent antioxidant properties in all assays. This fraction also had bacteriostatic and bactericidal effects against all bacterial strains at low concentrations, especially S. aureus. The hexane fraction had the highest antiproliferative potential, with IC50 values ranging from 24.2 to 46.6 µg/mL in HL-60 (human promyelocytic leukemia cell) and K562 (human chronic myelocytic leukemia cell), respectively. Preliminary chemical analysis indicates the presence of terpenes and gallic acid in the geopropolis. Our results indicate the therapeutic potential of geopropolis from M. mondury against inflammatory, oxidative, infectious, and neoplastic diseases.

Chemical composition and antimicrobial activity of essential oils of Ocimum canum Sims. and Ocimum selloi Benth.

This work describes the chemical composition and antimicrobial activity of the volatile oils of Ocimum canum and Ocimum selloi, both occurring in Jequié/BA, northeastern Brazil. The plants were collected in the winter/2005 and summer/2006, the oils extracted by steam distillation and further analyzed by GC-MS. A total of 30 and 31 compounds was identified from the oils of O. selloi and O. canum, respectively. It was observed that the oil content of O. canum showed variation during the seasons, while the oils of O. selloi did not. Methylchavicol and linalool were the main chemical components found in the aerial parts and leaves of O. canum. This finding permitted to characterize this specimen as a new chemotype of O. canum. Regarding the aerial parts of O. selloi, eugenol, 1,8-cineole, transcaryophyllene and linalool were identified as their major components. All extracted oils from the aerial parts showed biological activity against gram-positive cocci ­ Staphylococcus aureus ATCC 25923 ­ but only the O. canum one showed activity against gram-negative bacilli ­ Escherichia coli ATCC 25922.

Chemical constituents, antioxidant, anti-inflammatory and, antinociceptive activities of Trichilia ramalhoi.

Trichilia ramalhoi Rizz. is a species from Meliaceae family and its chemical composition and biological activities are still unknown. This work describes the chemical composition and biological activities of the organic extracts of this plant. Therefore, methanolic extract of stem barks and leaves were prepared and submitted to chromatographic procedures. Besides, T. ramalhoi extracts biological evaluation showed antioxidant, antinociceptive and, anti-inflammatory activities. Usual chromatographic procedures of the active extracts permitted to isolate methyl 5-O-caffeoylquinate, apocynin C, cinchonains Ia and Ib, besides ß-sitosterol, stigmasterol and lupeol. The identification of the isolates was based on 13C and 1H NMR (1 D and 2 D) spectroscopic data and mass spectrometry. Although the flavalignans cinchonains Ia and Ib were previously isolated from T. catigua, this is the first occurrence of apocynin C in the Meliaceae family.

Synthesis and insecticidal activity of new 3-benzylfuran-2-yl N,N,N',N'-tetraethyldiamidophosphate derivatives.

BACKGROUND: A series of 3-benzylfuran-2-yl N,N,N',N'-tetraethyldiamidophosphate derivatives were synthesized as potential new agents to control insects. Their structures were confirmed on the basis of IR, NMR and MS analyses. RESULTS: Ten 3-benzylfuran-2-ylN,N,N',N'-tetraethyl derivatives were prepared from the compound furan-2-yl N' (N,N,N',N'-tetraethyldiamidophosphate). The contact toxicity of all derivatives, at a dose of 10 microg mg(-1) insect, was evaluated against four insect species, Ascia monuste orseis Latr. (Lepidoptera: Pyralidae), Diaphania hyalinata (L.) (Lepidoptera: Pyralidae), Sitophilus zeamais Mots. (Coleoptera: Bruchidae) and Solenopsis saevissima (Smith) (Hymenoptera: Formicidae). The mortality range observed for some derivatives, such as 3-(3-methylbenzyl)furan-2-yl N,N,N',N'-tetraethyldiamidophosphate (82.5% mortality against D. hyalinata; 100% mortality against S. saevissima), was comparable with that of the commercial insecticide chlorpyrifos-methyl. The biological activity of the derivatives depended on the substitution pattern of the benzylic ring. Furan-2-yl N,N,N',N'-tetraethyldiamidophosphate, furan-2-yl N,N-diethylamidochlorophosphate and difuran-2-yl N,N-diethylamidophosphate were also evaluated, displaying, in some cases, activity comparable with that of chlorpyrifos-methyl (90%, 100% and 97.5% respectively against A. monuste orseis). Considerable activity was observed for some furan-2(5H)-ones evaluated. CONCLUSION: Ten 3-benzylfuran-2-yl N,N,N',N'-tetraethyldiamidophosphate derivatives were synthesized and fully characterized from a chemical point of view. The results obtained from the biological assays indicate that this class of compounds can be utilized for the design of new substances endowed with insecticidal activity.

Larvicidal activities and chemical composition of essential oils from Piper klotzschianum (Kunth) C. DC. (Piperaceae).

BACKGROUND: Volatile oils from fresh roots, stems, leaves and seeds of Piper klotzschianum (Piperaceae) were obtained by hydrodistillation and analysed by GC-FID and GC-MS. In total, 25 components, representing more than 95% of the examined oils, were identified. The essential oils were evaluated against Artemia salina Leach nauplii and fourth-instar Aedes aegypti larvae. RESULTS: The major chemical constituents that were identified from various parts of this plant were 1-butyl-3,4-methylenedioxybenzene and 2,4,5-trimethoxy-1-propenylbenzene in the root, 1-butyl-3,4-methylenedioxybenzene in the stems and leaves and 1-butyl-3,4-methylenedioxybenzene, limonene and α-phellandrene in the seeds. The biological activities of these essential oils generally exhibited high toxicity against A. salina, with LC50 values that ranged from 7.06 to 15.43 µg mL(-1), and significant larvicidal activity against fourth-instar A. aegypti larvae was observed in the essential oils from the seeds (LC50 of 13.27 µg mL(-1)) and roots (LC50 of 10.0 µg mL(-1)) of the plant. CONCLUSION: The present study indicates that both essential oil of P. klotzsdhianum and the isolate 1-butyl-3,4-methylenedioxybenzene are potential resources for A. aegypti larva control. This is the first report of the biological activities of the oil and isolated compound.

Melipona mondury produces a geopropolis with antioxidant, antibacterial and antiproliferative activities

ABSTRACT Geopropolis is a special type of propolis produced by stingless bees. Several pharmacological properties have been described for different types of geopropolis, but there have been no previous studies of the geopropolis from Melipona mondury. In this study, we investigated the antioxidant, antibacterial, and antiproliferative activities of M. mondury geopropolis, and determined its chemical profile. The antioxidant activity was determined using in vitro ABTS·+, ·DPPH, and β-carotene/linoleic acid co-oxidation methods. The antibacterial activity was determined using a microdilution method with Pseudomonas aeruginosa, Staphylococcus aureus, and methicillin-resistant S. aureus. The antiproliferative effect was determined in tumor cell lines using the Alamar Blue assay. The chemical profile was obtained using UHPLC-MS and UHPLC-MS/MS. The butanolic fraction had the highest concentration of phenolic compounds and more potent antioxidant properties in all assays. This fraction also had bacteriostatic and bactericidal effects against all bacterial strains at low concentrations, especially S. aureus. The hexane fraction had the highest antiproliferative potential, with IC50 values ranging from 24.2 to 46.6 µg/mL in HL-60 (human promyelocytic leukemia cell) and K562 (human chronic myelocytic leukemia cell), respectively. Preliminary chemical analysis indicates the presence of terpenes and gallic acid in the geopropolis. Our results indicate the therapeutic potential of geopropolis from M. mondury against inflammatory, oxidative, infectious, and neoplastic diseases.

Chemical composition and antimicrobial activity of essential oils of Ocimum canum Sims. and Ocimum selloi Benth.

This work describes the chemical composition and antimicrobial activity of the volatile oils of Ocimum canum and Ocimum selloi, both occurring in Jequié/BA, northeastern Brazil. The plants were collected in the winter/2005 andsummer/2006, the oils extracted by steam distillation and further analyzed by GC-MS. A total of 30 and 31 compounds was identified from the oils of O. selloi and O. canum, respectively. It was observed that the oil content of O. canum showed variation during the seasons, while the oils of O. selloi did not. Methylchavicol and linalool were the main chemical components found in the aerial parts and leaves of O. canum. This finding permitted to characterize this specimen as a new chemotype of O. canum. Regarding the aerial parts of O. selloi, eugenol, 1,8-cineole, transcaryophyllene and linalool were identified as their major components. All extracted oils from the aerial parts showed biological activity against gram-positive cocci - Staphylococcus aureus ATCC 25923 - but only the O. canum one showed activity against gram-negative bacilli - Escherichia coli ATCC 25922.

Este trabalho descreve a composição química e a atividade antimicrobiana dos óleos voláteis de Ocimum canum e Ocimum selloi, que ocorrem em Jequié/BA, nordeste do Brasil. As plantas foram colhidas no inverno de 2005 e verão de 2006 e os óleos extraídos por destilação a vapor foram posteriormente analisados por GC-MS. Um total de 30 e 31 compostos foi identificado a partir dos óleos de O. selloi e O. canum, respectivamente. Foi observado que o teor de óleo de O. canum apresentou variação durante as estações do ano, enquanto o óleo de O. selloi não. Metilchavicol e linalol foram os principais componentes químicos encontrados na parte aérea e folhas de O. canum. Esta descoberta permitiu caracterizar este espécime como um novo quimiotipo de O. canum. Com relação às partes aéreas de O. selloi, eugenol, 1,8-cineol, trans-cariofileno e linalol foram identificadas como os seus principais componentes. Todos os óleos extraídos das partes aéreas apresentaram atividade biológica contra cocos gram-positivo - Staphylococcus aureus ATCC 25923 - mas apenas aquele de O. canum apresentou atividade contra bacilo gram-negativo - Escherichia coli ATCC 25922.