ABSTRACT
Abstract Breast cancer is one of the leading types of cancer worldwide, and the search for new treatment options are crucial. Nonsteroidal anti-inflammatory drugs (NSAIDs) -specially ibuprofen and diclofenac-, have shown antitumoral effect against several types of cancer. The synthesis of organometallic compounds has shown significant improvements in pharmacological properties and efficacy of organic molecules. Two zinc II ternary complexes containing the NSAIDs diclofenac and ibuprofen and nicotinamide neutral linker (Nic) were obtained by the two-step solvent metalligand complexation method. The compounds Zn2(Diclof)4(Nic)2 (complex 1) and Zn2(Ibup)4(Nic)2 (complex 2) were tested in breast cancer cell lines (4T1, MCF-7 and MDA-MB-231) to evaluate their cytotoxicity, comparing to ibuprofen and diclofenac as controls. We found that both complex 1 and 2 exerted more than 60% reduction in 4T1 viability at 250µM, and complex 2 decreased cell viability at 250 µM and 137.5 µM in MCF-7 (34.35% and 26.42% reduction, respectively) and in MDA-MB-231 (57.2% and 22.88% reduction, respectively), all compared to controls. Complex 1 was selective only in MCF-7, and complex 2 was selective in both MCF-7 and MDA-MB-231. In summary, our data showed that the cytotoxic effect of complex 1 and 2 is increased comparing to their original NSAID in different breast cancer cell lines, highlighting their potential anti-tumoral activity.
ABSTRACT
ABSTRACT Piper aduncum found naturally in the Amazon and southeastern Brazil, is known for its secondary metabolites that have activity on insects. Anticarsia gemmatalis and Spodoptera frugiperda are among the major insect pests associated with agricultural production. This research evaluated the biological activity of hexane, ethyl acetate, and ethanol extracts of P. aduncum leaves on mortality and duration of larval and pupal periods, as well as weight, width, and length of A. gemmatalis and S. frugiperda pupae. The mortality of A. gemmatalis larvae in trials with P. aduncum extracts were 93.3% (hexane) and 90% (ethyl acetate), estimating LC50 of 6.35 and 5.79 mg/mL, respectively. Mortality in S. frugiperda submitted to the hexane extract ranged from 3.33% to 96.66% (LC50 of 8.22 mg/mL). The ethanol extract induced low mortality (3.33% to 23.33%). The P. aduncum extracts did not affect the development of S. frugiperda pupae. In A. gemmatalis differences in weight and length occurred. The chemical characterization was by GC-MS, which revealed that the major constituent in the hexane extract of P. aduncum was apiol (90.7%). P. aduncum extracts are important and promising components to manage A. gemmatalis and S. frugiperda, which cause extensive production losses.
Subject(s)
Animals , Plant Extracts/pharmacology , Spodoptera/drug effects , Piper/chemistry , Insecticides/pharmacology , Lepidoptera/drug effects , Insecticides/isolation & purificationABSTRACT
Objective: To investigate the antidiabetic effect of Rourea cuspidata hydroalcoholic stem extract in normal and streptozotocin-induced diabetic rats. Methods: In order to evaluate the chemical composition, different extracts from stem in ascending solvent order of polarity were prepared. The extracts were analyzed by high resolution mass spectrometry and 7 compounds were identified, including hyperin, an important and already reported active compound in the literature. Hyperin was also quantified by HPLC-UV in all the extracts. The hydroalcoholic stem extract (Ss5), which showed the highest concentration of hyperin, was administered to STZ-induced diabetes rats to evaluate the potential hypoglycemic activity. Total cholesterol, HDL, triglycerides, ALT and AST were also evaluated. In the present study, the effects of oral administration of hydroalcoholic stem extract (200 mg/kg b. wt.) for 28 days on the level of serum glucose, total cholesterol, HDL, triglycerides, aspartate amino transferase (AST) and alanine amino transferase (ALT) in normal and streptozotocin-induced diabetic rats were evaluated. Histopathological changes in diabetic rats' pancreas were also studied. Results: The extract exposition demonstrated hypoglycemic effect like the drug control glibenclamide. The extract was able to increase the HDL levels. Histopathological study on diabetic rats' pancreas after extract treatment showed morphological alterations in STZ-induced diabetes rats, which were apparently restored after extract treatment. Conclusions: This work demonstrates the potential use of R. cuspidata as hypoglycemic agent in the treatment of diabetes.
ABSTRACT
Propolis has been used worldwide for years in folk medicine and currently marketed by the pharmaceutical industry. In Brazil, propolis was classified into 13 groups based on their organoleptics and physicochemical characteristics. The 13th type named red prop-olis has been an important source of investigation since late 90s. Their property comes from the countless compounds, including terpenes, pterocarpans, prenylated benzophe-nones and especially the flavonoids. This last compound class has been indicated as the responsible for its potent pharmacological actions, highlighting the antimicrobial, anti-inflammatory, antioxidant, healing and antiproliferative activities. The red propolis can also be found in other countries, especially Cuba, which has similar features as the Brazilian. Therefore, with the compilation of 80 papers, this review aims to provide a key reference for researchers interested in natural products and discovery of new active compounds, such as from propolis.
ABSTRACT
The genus Mikania ranks high in the list of best-selling natural products in the world. Its main distribution is in South America, but some species are found in Asia, North America and Africa. It is used for treating fever, rheumatism, colds and respiratory diseases, as well as snake bites and scorpion stings, due to its broad spectrum of action. There are approximately 430 species of this genus and only 12% have been studied, highlighting their chemical and pharmacological diversity. The main chemical groups are: coumarins and derivatives, sesquiterpenes, sesquiterpenes lactones, diterpenes, phytosterols/terpenoids and flavonoids. This review aims to supply useful references for scientists interested in natural products and the search for new compounds, from over the 300 already described for the genus.