Objectives Malva sylvestris L., known as common mallow, is native to Europe, North Africa and Asia. In the Mediterranean region, this species has a long history of use as food, and due to its therapeutic relevance, some parts of this plant have been employed in traditional and ethnoveterinary medicines. The leaves in particular have been reported to have potent anti-inflammatory, antioxidant, anti-complementary, anticancer and skin tissue integrity activity. Additionally, an anti-ulcerogenic effect was recently proven, demonstrating that the aqueous extract was more effective than cimetidine, a potent medicine used to treat gastric ulcers. Due to its wide use and medicinal importance, many studies have been conducted; however, the information in the literature is very extensive and disseminated, making it difficult to use. Key findings A complete review involving the ethnobotanical and scientific aspects of M. sylvestris has been made. The research has provided evidence that M. sylvestris has potential use as a medicinal plant and has highlighted a need for more studies involving clinical and toxicological aspects of its use. Summary This review can contribute to the field with its historical context, and by describing the progress made, new ideas for researchers can arise.
RESUMO:No Brasil as espécies de Mikania glomerata Spreng. e M. laevigata Sch. Bip. ex Baker, Asteraceae, popularmente conhecidas como guaco, são amplamente utilizadas com evidências pré-clínicas para o tratamento de doenças onde estejam envolvidas suas ações broncodilatadoras, antialérgicas, antiasmáticas, anti-inflamatórias, antiulcerogênicas e relaxantes da musculatura lisa. Em virtude das propriedades terapêuticas atribuídas as essas espécies, ambas foram oficializadas na farmacopéia brasileira, e por serem bastante semelhantes, dificilmente são diferenciadas. Com o objetivo de contribuir com novas pesquisas, a presente revisão descreve, de forma sistematizada, sobre os aspectos farmacológicos, toxicológicos, químicos, agronômicos, morfoanatômicos, genéticos e o uso nos programas de fitoterapia do Brasil destas espécies. As principais diferenças e semelhanças entre as duas espécies são evidenciadas através da comparação das informações baseadas na literatura específica.Unitermos: Asteraceae, Mikania glomerata, Mikania laevigata, guaco, plantas medicinais.ABSTRACT: "Mikania glomerata Spreng. e M. laevigata Sch. Bip. ex Baker, Asteraceae: agronomic, genetic, anatomical, chemical, pharmacological, toxicological studies and its use in herbal therapy programs in Brazil." In Brazil the species of Mikania glomerata Spreng. and M. laevigata Sch. Bip. ex Baker, Asteraceae popularly known as guaco, are widely used with preclinical evidence for the treatment of diseases whose actions involve bronchodilators, antiallergic, anti-asthmatic, anti-inflammatory, antiulcerogenic and smooth muscles relaxant. Due to the therapeutic properties attributed to these species, both were included in the official Brazilian Pharmacopoeia, and because of their similarity, they are hardly differentiated. In order to contribute to the new research, this review describes their several aspects: pharmacology, toxicology, chemical, agricultural, anatomical, genetics and the use in herbal medicine programs in Brazil, in a systematic way. The main differences and similarities between the two species are evidenced by comparing the information based on literature.
Invasive aspergillosis is an opportunistic infection that is mainly caused by Aspergillus fumigatus, which is known to produce several secondary metabolites, including gliotoxin, the most abundant metabolite produced during hyphal growth. The diagnosis of invasive aspergillosis is often made late in the infection because of the lack of reliable and feasible diagnostic techniques; therefore, early detection is critical to begin treatment and avoid more serious complications. The present work reports the development and validation of an HPLC-MS/MS method for the detection of gliotoxin in the serum of patients with suspected aspergillosis. Chromatographic separation was achieved using an XBridge C18 column (150×2.1 mm id; 5 mm particle size) maintained at 25°C with the corresponding guard column (XBridge C18, 10×2.1 mm id, 5 mm particle size). The mobile phase was composed of a gradient of water and acetonitrile/water (95∶5 v/v), both containing 1 mM ammonium formate with a flow rate of 0.45 mL min−1. Data from the validation studies demonstrate that this new method is highly sensitive, selective, linear, precise, accurate and free from matrix interference. The developed method was successfully applied to samples from patients suspected of having aspergillosis. Therefore, the developed method has considerable potential as a diagnostic technique for aspergillosis.
For decades guaco species have been empirically used for the treatment of respiratory diseases. However, studies have shown that the toxic and therapeutic effects of the main guaco metabolites are dose-dependent, and none clinical study was done to evaluate the behavior of these substances in humans. In this work, a pilot study measuring the kinetic profile of the main guaco metabolites was performed leading to the knowledge of an alternative route of coumarin metabolism in humans. Initial screenings demonstrated that the administration of 60 mL of guaco syrup (single dose) did not provide sufficient levels of coumarin (COU), 7-hydroxycoumarin (7-HCOU), o-coumaric acid (OCA) and kaurenoic acid (KAU). The pharmacokinetic parameters were calculated by orally administering 60 mL of guaco syrup spiked with 1500 mg of COU. The kinetic study demonstrated that the plasmatic levels of 7-HCOU (considered the main metabolite of COU) were 10 times lower than the levels of COU, and the kinetic profile of 7-HCOU suggests sequential metabolism in the liver with low access of 7-HCOU to the systemic circulation. The study also demonstrated that OCA is one of the main bioavailable metabolites of COU. Therefore, the hydrolysis of the lactone ring forming a carboxylated compound is one of the possible routes of COU metabolism in humans. The half-lives of COU, 7-HCOU and OCA were approximately 4.0, 1.0 and 3.0 h, respectively and there was evidence that the recommended dosage of guaco syrup did not provide sufficient levels of COU, 7-HCOU or OCA to obtain a bronchodilation effect. Clinical studies are necessary to prove the efficacy and safety of products based on guaco.
Coumarin (1,2-benzopyrone) is a natural compound whose metabolism in humans was established in the 1970s. However, a new metabolite was recently identified in human plasma, indicating that the metabolism of coumarin has not been completely elucidated. To complement the knowledge of its metabolism, a rapid and sensitive method using UPLC-QTOF-MS was developed. A total of 12 metabolites was identified using MetaboLynxTM software, including eight metabolites not previously reported in human urine. The identified biotransformation included hydroxylation, glucuronidation, sulfation, methylation, and conjugation with N-acetylcysteine. The present work demonstrates that the metabolism study of coumarin was incomplete, possibly due to limitations of old techniques. The identification of eight inedited metabolites of such a simple molecule suggests that the information regarding the metabolism of other drugs may also be incomplete, and therefore, new investigations are necessary.
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