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O presente trabalho realizou uma prospecção tecnológica a partir de patentes para identificação de derivados das plantas medicinais para o tratamento da tuberculose. O uso de patentes como fonte de informação pode otimizar o desenvolvimento de novos medicamentos para o tratamento da tuberculose. A identificação de novas tecnologias foi realizada pelo portal Orbit Intelligence, utilizando a sentença “(+tuberculos+)/TI/AB AND (A61K OR A61P)/IPC AND PRD >= 2015” como estratégia de pesquisa. Foram identificadas 16 famílias de patentes apresentando derivados de plantas medicinais com evidência de eficácia in vitro contra cepas resistentes de Mycobacterium tuberculosis. A proteção patentária dos produtos naturais identificados está restrita aos países dos detentores dos novos produtos: China, República da Coreia e Rússia. A maior parte dos derivados de plantas medicinais identificados são substâncias isoladas, principalmente flavonoides e terpenos, extraídos de diferentes espécies de plantas, caracterizando-se, dessa forma como, fitofármacos.

Euterpe oleracea (açaí) fruit has approximately 15% pulp, which is partly edible and commercialized, and 85% seeds. Although açaí seeds are rich in catechins—polyphenolic compounds with antioxidant, anti-inflammatory, and antitumor effects—almost 935,000 tons/year of seeds are discarded as industrial waste. This work evaluated the antitumor properties of E. oleracea in vitro and in vivo in a solid Ehrlich tumor in mice. The seed extract presented 86.26 ± 0.189 mg of catechin/g of extract. The palm and pulp extracts did not exhibit in vitro antitumor activity, while the fruit and seed extracts showed cytotoxic effects on the LNCaP prostate cancer cell line, inducing mitochondrial and nuclear alterations. Oral treatments were performed daily at 100, 200, and 400 mg/kg of E. oleracea seed extract. The tumor development and histology were evaluated, along with immunological and toxicological parameters. Treatment at 400 mg/kg reduced the tumor size, nuclear pleomorphism, and mitosis figures, increasing tumor necrosis. Treated groups showed cellularity of lymphoid organs comparable to the untreated group, suggesting less infiltration in the lymph node and spleen and preservation of the bone marrow. The highest doses reduced IL-6 and induced IFN-γ, suggesting antitumor and immunomodulatory effects. Thus, açaí seeds can be an important source of compounds with antitumor and immunoprotective properties.

BackgroundThe bioactive metabolites production contributes to the resistance of fungi towards adverse environmental conditions. Some metabolites often have interesting health-promoting activities. This study addressed the anti-tumoural properties of Penicillium purpurogenum isolated from a polluted lagoon in Northeastern Brazil.MethodsThe extract obtained from the polished environment strain P. purpurogenum was fermented, filtered, concentrated and lyophilized, giving rise to the Ethyl Acetate Extracellular Extract (EAE). The metabolites of the extracellular extract of P. purpurogenum were studied using direct infusion mass spectrometry. The solid Ehrlic tumor model was used to evaluate the extract antitumor activity. Female Swiss mice were divided in groups (n=10/group) as follow: Negative control (CTL-) treated with phosphate buffered solution; Positive Control (CTL+) treated with cyclophosphamide (25mg/mL); Extracts treatment at doses 4, 20 and 100mg/Kg; Animals without tumor or treatment (Sham); and animals without tumor treated with intermediate dose (EAE20). All treatments were performed intraperitoneally, daily during 15 days. After, the animals were eutanized and the tumor, lymphoid organs and serum were used for immunological, histological and biochemical parameters evaluation.ResultsThe extract was rich in meroterpenoids. All doses of the extract significantly reduced tumor size compared to CLT- and were associated with 100% survival. Histologically, the 20 and 100mg/kg doses reduced tumour-associated inflammation and tumour necrosis. The extract also reduced cellular infiltration of lymphoid organs and circulating TNF-α levels when compared with CLT-. The extract did not induce weight loss and renal or hepatic toxic changes.ConclusionsThese results indicate that P. purpurogenum from a polluted marine environment produce hybrid natural products of the terpenoid pathway that exhibits immunomodulatory and antitumor properties in vivo. Thus, fungal fermentation is a biotechnological approach for the production of antitumour agents.

Leishmaniasis is a complex of diseases caused by protozoa of the genus Leishmania and affects millions of people around the world. Several species of plants are used by traditional communities for the treatment of this disease, among which is Carapa guianensis Aubl. (Meliaceae), popularly known as andiroba. The objective of the present work was to conduct a chemical study of C. guianensis seed oil and its limonoid-rich fractions, with the aim of identifying its secondary metabolites, particularly the limonoids, in addition to investigating its anti-Leishmania potential. The chemical analyses of the C. guianensis seed oil and fractions were obtained by electrospray ionization mass spectrometry (ESI-MS). The cytotoxic activity was tested against peritoneal macrophages, and antileishmanial activity was evaluated against promastigotes and intracellular amastigotes of Leishmania amazonensis. All the C. guianensis seed oil samples analyzed exhibited the same pattern of fatty acids, while the limonoids 7-deacetoxy-7-hydroxygedunin, deacetyldihydrogedunin, deoxygedunin, andirobin, gedunin, 11β-hydroxygedunin, 17-glycolyldeoxygedunin, 6α-acetoxygedunin, and 6α,11β-diacetoxygedunin were identified in the limonoid-rich fractions of the oil. The C. guianensis seed oil did not exhibit antileishmanial activity, and cytotoxicity was higher than 1000 μg/mL. Three limonoid-rich oil fractions demonstrated activity against promastigotes (IC50 of 10.53±0.050, 25.3±0.057, and 56.9±0.043μg/mL) and intracellular amastigotes (IC50 of 27.31±0.091, 78.42±0.086, and 352.2±0.145 μg/mL) of L. amazonensis, as well as cytotoxicity against peritoneal macrophages (CC50 of 78.55±1.406, 139.0±1.523, and 607.7±1.217 μg/mL). The anti-Leishmania activity of the limonoid-rich fractions of C. guianensis can be attributed to the limonoids 11β-hydroxygedunin and 6α,11β-diacetoxygedunin detected in the chemical analysis.

This article aims to evaluate the total phenolics and antioxidant activity of the prepared extract of the fungus Penicillium purpurogenum, obtained from a polluted marine environment of Sao Luis-MA. The research was carried out at Laguna da Jansen located in the Municipality of Sao Luis, Maranhao, Brazil. Four sediment collections were performed from May to September 2017, in the morning period. The samples were obtained from a depth of up to 73.5 cm with the aid of a metal dredger. The identification of the fungus followed methodologies of isolation and subsequent preparation of the extracts with evaluation of total phenolics by the Folin-Ciocalteu method and antioxidant activity by the DPPH radical sequestration method. Identification confirmed the presence of Penicillium purpurogenum . The extracts of P. purpurogenum varied in the quantification of total phenolics of 791.00 mg EAT g -1 for FR1 extract and 650.82 mg EAT g -1 for FR2. In antioxidant activity, wecould verify that the EC 50 found in the FR1 extract was 22.59 μg mL -1 and FR2 39.80 μg mL -1 . Concluding that the EXTRACT FR2 showed strong antioxidant activity while FR1 was very strong by the DPPH radical method.

As folhas de Arrabidaea chica sao empregadas popularmente no tratamento de colica intestinal, diarreia, anemia, inflamacao uterina e de feridas cutâneas como cicatrizante. Tradicionalmente sao usadas tambem na producao de materia corante devido a presenca de 3-desoxiantocianidinas, constituintes quimicos caracteristicos da especie. A. chica e descrita no presente trabalho em termos de botânica, farmacognosia, farmacologia etoxicologia com vistas ao desenvolvimento de um fitoterapico. Arrabidaea chica (Humb. & Bonpl.) B. Verlot (Bignoniaceae)The leaves of Arrabidaea chica are popularly used in the treatment of intestinal pain, diarrhea, anemia, uterine inflammation and for the healing of skin wounds. Traditionally they are also used to produce a red pigment derived from the 3-deoxyanthocyanidines, characteristic of the species. A. chica is here described in terms of its botany, pharmacognosy, pharmacology and toxicology, with a view to developing a phytherapeutic medicine.

Nowadays consumption of herbal medicines has been increasing worldwide.This uncontrolled use can present a serious risk to the health of the population because medicinal plants and herbal medicines represent complex mixtures of substances that can often interact with others and have an adverse effect. This work intends to emphasize the importance of the pharmacovigilance of medicinal plants and herbal medicines in Brazil, in order to decrease the threat that the adverse effects and drug interactions have on the population and to contribute to the rational and correct decision making by health professionals working in this area. Pharmacovigilance of medicinal plants and herbal medicines in Brazil is still in its infancy. This fact can be explained by deficiency in the training of health professionals, the belief in innocuous natural medicinal plants and herbal medicines and self-medication.

The absence of an effective vaccine and the debilitating chemotherapy for Leishmaniasis demonstrate the need for developing alternative treatments. Several studies conducted with Morinda citrifolia have shown various biological activities, including antileishmanial activity, however its mechanisms of action are unknown. This study aimed to analyze the in vivo activity of M. citrifolia fruit juice (Noni) against Leishmania (Leishmania) amazonensis in C57BL/6 mice. M. citrifolia fruit juice from the Brazilian Amazon has shown the same constitution of other juices produced around the world and liquid chromatography–mass spectrometry analysis identified five compounds: deacetylasperulosidic acid, asperulosidic acid, rutin, nonioside B and nonioside C. Daily intragastric treatment with Noni was carried out after 55 days of L. (L.) amazonensis infection in C57BL/6 mice. Parasitic loads, cytokine and extracellular protein matrix expressions of the lesion site were analyzed by qPCR. Histopathology of the lesion site, lymph nodes and liver were performed to evaluate the inflammatory processes. Cytokines and biochemical parameters of toxicity from sera were also evaluated. The Noni treatment at 500 mg.kg-1.day-1 for 60 days decreased the lesion size and parasitic load in the footpad infected with L. (L.) amazonensis. The site of infection also showed decreased inflammatory infiltrates and decreased cytokine expressions for IL-12, TNF-α, TGF-β and IL-10. On the other hand, Noni treatment enhanced the extracellular matrix protein expressions of collagen IV, fibronectin and laminin in the infected footpad as well collagen I and II, fibronectin and laminin in the mock-infected footpads. No toxicity was observed at the end of treatment. These data show the efficacy of Noni treatment., Author Summary Leishmaniasis is a complex of diseases caused by parasites of the Leishmania genus, which affects thousands of people around the world. The parasite lives within the cells and the disease manifests itself in different ways, one of them is wound-like lesions on the skin that do not heal. The treatment, with a medicament discovered in 1912, causes several side effects, its intramuscular administration is painful and it is given daily over a long period of time. These characteristics show the need for new alternatives for leishmaniasis treatment justifying works like this. The Morinda citrifolia is a plant native to the Polynesian islands and has a fruit commonly known as Noni. Noni has been analyzed for various targets such as anticancer, anti-inflammatory and antimicrobial effects; however, the antileishmanial has not yet been fully evaluated. This work proves that Noni treatment can promote a fast clinical cure in mice with leishmaniasis by decreasing parasite number, acting on the immune system and repairing skin components.