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1.
Rev. biol. trop ; 70(1)dic. 2022.
Article in English | LILACS-Express | LILACS, SaludCR | ID: biblio-1387704

ABSTRACT

Abstract Introduction: Pathogenic protozoans, like Entamoeba histolytica and Trichomonas vaginalis, represent a major health problem in tropical countries; and polymeric nanoparticles could be used to apply plant extracts against those parasites. Objective: To test Curcuma longa ethanolic extract and Berberis vulgaris methanolic extracts, and their main constituents, against two species of protozoans. Methods: We tested the extracts, as well as their main constituents, curcumin (Cur) and berberine (Ber), both non-encapsulated and encapsulated in polymeric nanoparticles (NPs), in vitro. We also determined nanoparticle characteristics by photon correlation spectroscopy and scanning electron microscopy, and hemolytic capacity by hemolysis in healthy erythrocytes. Results: C. longa consisted mainly of tannins, phenols, and flavonoids; and B. vulgaris in alkaloids. Encapsulated particles were more effective (P < 0.001); however, curcumin and berberine nanoparticles were the most effective treatments. CurNPs had IC50 values (µg/mL) of 9.48 and 4.25, against E. histolytica and T. vaginalis, respectively, and BerNPs 0.24 and 0.71. The particle size and encapsulation percentage for CurNPs and BerNPs were 66.5 and 73.4 nm, and 83.59 and 76.48 %, respectively. The NPs were spherical and significantly reduced hemolysis when compared to non-encapsulated extracts. Conclusions: NPs represent a useful and novel bioactive compound delivery system for therapy in diseases caused by protozoans.


Resumen Introducción: Los protozoos patógenos, como Entamoeba histolytica y Trichomonas vaginalis, representan un importante problema de salud en los países tropicales; y se podrían usar nanopartículas poliméricas para aplicar extractos de plantas contra esos parásitos. Objetivo: Probar los extractos etanólicos de Curcuma longa y Berberis vulgaris, y sus principales constituyentes, contra dos especies de protozoos. Métodos: Probamos los extractos, así como sus principales constituyentes, curcumina (Cur) y berberina (Ber), tanto no encapsulados como encapsulados en nanopartículas poliméricas (NPs), in vitro. También determinamos las características de las nanopartículas por espectroscopía de correlación de fotones y microscopía electrónica de barrido, y la capacidad hemolítica por hemólisis en eritrocitos sanos. Resultados: C. longa tenía principalmente: taninos, fenoles y flavonoides; y B. vulgaris, alcaloides. Las partículas encapsuladas fueron más efectivas (P < 0.001); sin embargo, las nanopartículas de curcumina y berberina fueron los tratamientos más efectivos. CurNPs tenía valores IC50 (µg/mL) de 9.48 y 4.25, contra E. histolytica y T. vaginalis, respectivamente, y BerNPs 0.24 y 0.71. El tamaño de partícula y el porcentaje de encapsulación para CurNPs y BerNPs fueron: 66.5 y 73.4 nm, y 83.59 y 76.48 %, respectivamente. Los NP son esféricos y redujeron significativamente la hemólisis en comparación con los extractos no encapsulados. Conclusiones: Las NP representan un sistema de administración de compuestos bioactivos útil y novedoso para la terapia enfermedades causadas por protozoos.


Subject(s)
Trichomonas vaginalis , Berberis vulgaris , Curcuma , Entamoeba histolytica
2.
Braz. dent. j ; 33(3): 55-66, July-Sept. 2022. tab, graf
Article in English | LILACS-Express | LILACS, BBO | ID: biblio-1384030

ABSTRACT

Abstract The objective of this study was to evaluate the effect of natural bleaching products on the color, whiteness, and superficial properties of dental enamel. Seventy fragments of bovine teeth were obtained (6mm x 6mm x 2mm). Initial surface roughness (Surfcorder SE1700, Kosakalab), microhardness (HMV-2, Shimadzu), color (EasyShade, VITA), and surface gloss (Micro-Gloss 45º BYK, Gardner) readings were done. Samples were separated into five groups (n=14) according to the treatments used: CT-conventional toothpaste (negative control); CH-charcoal; TU-turmeric; BP-banana peel, and CP16%-16% carbamide peroxide gel (positive control, 4 h/day for 14 days), and then brushed for 560 cycles (T1) and 1200 cycles (T2), equivalent to 14 and 30 days of brushing. New measurements were performed after T1 and T2. The whiteness index for dentistry change (∆WID) and Weight loss (Wl) were calculated. CP16% demonstrated the highest (p<.05) color change (ΔE00) and ∆WID (2-way ANOVA, Bonferroni, p<.05). Surface gloss alterations were lower for TU, CP16%, and BP. CT and CH increased surface roughness (p<.05). CP16% decreased enamel microhardness. CH presented medium abrasiveness, and CT and TU, low abrasiveness. The popular bleaching products were not efficient for tooth whitening. Furthermore, brushing with charcoal increased the enamel surface roughness, and CP16% decreased enamel microhardness over time


Resumo O objetivo deste estudo foi avaliar o efeito de produtos clareadores naturais na cor, efeito clareador e propriedades superficiais do esmalte dentário. Setenta fragmentos de dente bovino foram obtidos (6mm x 6mm x 2mm). Foram realizadas leituras iniciais de rugosidade de superfície (Surfcorder SE1700, Kosakalab), microdureza (HMV-2, Shimadzu), cor (EasyShade, VITA) e brilho (Micro-Gloss 45º BYK, Gardner). As amostras foram separadas em cinco grupos (n=14), de acordo com os tratamentos utilizados: DC - dentifrício convencional (controle negativo); CA - carvão ativado; CM - cúrcuma; CB - casca de banana e PC16% - gel de peróxido de carbamida a 16% (controle positivo, 4h/dia por 14 dias), foram então escovadas por 560 ciclos (T1) e 1200 ciclos (T2), equivalente a 14 e 30 dias de escovação. Novas leituras foram realizadas após T1 e T2. A alteração do whiteness index for dentistry (∆WID) e perda de massa (Pm) foram calculadas. PC16% demonstrou a maior (p<0,05) alteração de cor (ΔE00) e ∆WID (2-way ANOVA, Bonferroni, p<0,05). A alteração de brilho foi menor para CM, PC16% e CB. DC e CA aumentaram a rugosidade de superfície (p<0,05). PC16% diminuiu a microdureza do esmalte. CA apresentou abrasividade média, e DC e CM, baixa abrasividade. Os produtos clareadores populares não foram eficientes para clareamento dental. Ademais, a escovação com carvão ativado aumentou a rugosidade de superfície do esmalte dentário, e com maior tempo PC16% diminuiu a microdureza do esmalte.

3.
Mem. Inst. Oswaldo Cruz ; 117: e220396, 2022. tab, graf
Article in English | LILACS-Express | LILACS | ID: biblio-1365148

ABSTRACT

Over the past years, natural products have been explored in order to find biological active substances to treat various diseases. Regarding their potential action against parasites such as trypanosomatids, specially Trypanosoma cruzi and Leishmania spp., much advance has been achieved. Extracts and purified molecules of several species from genera Piper, Tanacetum, Porophyllum, and Copaifera have been widely investigated by our research group and exhibited interesting antitrypanosomal and antileishmanial activities. These natural compounds affected different structures in parasites, and we believe that the mitochondrion is a strategic target to induce parasite death. Considering that these trypanosomatids have a unique mitochondrion, this cellular target has been extensively studied aiming to find more selective drugs, since the current treatment of these neglected tropical diseases has some challenges such as high toxicity and prolonged treatment time. Here, we summarise some results obtained with natural products from our research group and we further highlighted some strategies that must be considered to finally develop an effective chemotherapeutic agent against these parasites.

4.
Chinese Journal of Biotechnology ; (12): 478-505, 2022.
Article in Chinese | WPRIM | ID: wpr-927723

ABSTRACT

Yarrowia lipolytica, as an important oleaginous yeast, has been widely used in metabolic engineering. Y. lipolytica is considered as an ideal host for the production of natural products such as terpenes, polyketides and flavonoids, due to its ability to utilize a variety of hydrophobic substrates, high stress tolerance to acid and salt, high flux of tricarboxylic acid cycle and the ability in providing abundant the common precursor acetyl-CoA. Recently, more and more tools for genetic editing, gene expression and regulation has been developed in Y. lipolytica, which facilitate the metabolic engineering of Y. lipolytica for bio-manufacturing. In this review, we summarized the recent progresses in developing gene expression and natural product synthesis in Y. lipolytica, and also discussed the challenges and possible solutions in heterologous synthesis of natural products in this yeast.


Subject(s)
Biological Products/metabolism , Gene Editing , Metabolic Engineering , Polyketides/metabolism , Yarrowia/metabolism
5.
Biota Neotrop. (Online, Ed. ingl.) ; 22(spe): e20221345, 2022. graf
Article in English | LILACS-Express | LILACS | ID: biblio-1394011

ABSTRACT

Abstract The present review aims the discussion of the impact of the bioprospection initiative developed by the projects associated to BIOprospecTA, a subprogram of the program BIOTA, supported by FAPESP. This review brings a summary of the main results produced by the projects investigating natural products (NPs) from non-plants organisms, as examples of the success of this initiative, focusing on the progresses achieved by the projects related to NPs from macroalgae, marine invertebrates, arthropods and associated microorganisms. Macroalgae are one of the most studied groups in Brazil with the isolation of many bioactive compounds including lipids, carotenoids, phycocolloids, lectins, mycosporine-like amino acids and halogenated compounds. Marine invertebrates and associated microorganisms have been more systematically studied in the last thirty years, revealing unique compounds, with potent biological activities. The venoms of Hymenopteran insects were also extensively studied, resulting in the identification of hundreds of peptides, which were used to create a chemical library that contributed for the identification of leader models for the development of antifungal, antiparasitic, and anticancer compounds. The built knowledge of Hymenopteran venoms permitted the development of an equine hyperimmune serum anti honeybee venom. Amongst the microorganisms associated with insects the bioprospecting strategy was to understand the molecular basis of intra- and interspecies interactions (Chemical Ecology), translating this knowledge to possible biotechnological applications. The results discussed here reinforce the importance of BIOprospecTA program on the development of research with highly innovative potential in Brazil.


Resumo A presente revisão discute o impacto das iniciativas de bioprospecção desenvolvidas pelos projetos associados ao BIOprospecTA, subprograma do programa BIOTA, apoiado pela FAPESP. Esta revisão traz um resumo dos principais resultados produzidos pelos projetos de investigação de produtos naturais (PNs) de organismos não vegetais, como exemplos do sucesso desta iniciativa, com foco nos avanços alcançados pelos projetos relacionados a PNs de macroalgas, invertebrados marinhos, artrópodes e microrganismos associados. As macroalgas são um dos grupos mais estudados no Brasil com o isolamento de muitas substâncias bioativas, incluindo lipídios, carotenóides, ficocolóides, lectinas, aminoácidos do tipo micosporina e substâncias halogenadas. Invertebrados marinhos e microrganismos associados têm sido estudados de forma mais sistemática nos últimos trinta anos, revelando substâncias únicas, com potentes atividades biológicas. Os venenos de insetos himenópteros também foram amplamente estudados, resultando na identificação de centenas de peptídeos, que foram utilizados para criar uma biblioteca química que contribuiu para a identificação de modelos para o desenvolvimento de substâncias antifúngicas, antiparasitárias e anticancerígenas. O conhecimento construído dos venenos de himenópteros permitiu o desenvolvimento de um soro equino anti-peçonha de abelha. Dentre os microrganismos associados a insetos, a estratégia de bioprospecção foi compreender as bases moleculares das interações intra e interespécies (Ecologia Química), traduzindo esse conhecimento para possíveis aplicações biotecnológicas. Os resultados aqui discutidos reforçam a importância do programa BIOprospecTA no desenvolvimento de pesquisas com alto potencial inovador no Brasil.

6.
Biota Neotrop. (Online, Ed. ingl.) ; 22(spe): e20221356, 2022. graf
Article in English | LILACS-Express | LILACS | ID: biblio-1394012

ABSTRACT

Abstract In Brazil, research with natural products had a strong impulse when FAPESP supported the creation of the Laboratory of Chemistry of Natural Products of the Institute of Chemistry of USP (1966). In 1999, FAPESP launched the Research Program in the Characterization, Conservation, Restoration and Sustainable Use of Biodiversity (BIOTA-FAPESP), which intensified the sustainable exploitation of biodiversity, and which evolved to form the Biota Network for Bioprospection and Bioassays (BIOprospecTA), which integrates groups from all over the country, optimizing the use of the skills already installed for the bioprospecting of microorganisms, plants, invertebrates, vertebrates and marine organisms. Of the 104 projects related to plant sciences, 35 carried out bioprospection of Brazilian flora, belonging to the areas of Chemistry, Botany, Genetics, Plant Physiology, Plant Morphology, Plant (Chemo)taxonomy, Ecosystem Ecology, Plant Genetics. Physical Sciences, Forest Resources, Forestry Engineering, Agronomy, leading to thousands of publications, engagement of hundreds of students and a deeper understanding of natural products in different biological models through macromolecules analysis aided by computational and spectrometric strategies, in addition to pharmacological evaluations. The development of omics approaches led to a more comprehensive view of the chemical profile of an organism, and enabled integrated and concomitant studies of several samples, and faster annotation of known molecules, through the use of hyphenated and chemometric techniques, and molecular networking. This also helped to overcome the lack of information on the safety and efficacy of herbal preparations, in projects dealing with the standardization of herbal products, according to international standards. The BIOTA-FAPESP program has also focused on environmental aspects, in accordance with the principles of Green Chemistry and has had positive effects on international collaboration, on the number and impact of scientific publications and on partnership with companies, a crucial step to add value and expand the production chain of bioproducts. Also, the compilation, systematization and sharing of data were contemplated with the creation of the NUBBEDB database, of free access, and that integrates with international databases (ACD/labs, American Chemical Society - ACS), helping researchers and companies in the development from different areas of science, technology, strengthening the bioeconomy and subsidizing public policies.


Resumo No Brasil, as pesquisas com produtos naturais tiveram um forte impulso quando a FAPESP apoiou a criação do Laboratório de Química de Produtos Naturais do Instituto de Química da USP (1966). Em 1999, a FAPESP lançou o Programa de Pesquisa em Caracterização, Conservação, Restauração e Uso Sustentável da Biodiversidade (BIOTA-FAPESP), que intensificou a exploração sustentável da biodiversidade, e que evoluiu para formar a Rede Biota de Bioprospecção e Bioensaios (BIOprospecTA), que integra grupos de todo o país, otimizando o aproveitamento das competências já instaladas para a bioprospecção de microrganismos, plantas, invertebrados, vertebrados e organismos marinhos. Dos 104 projetos relacionados às ciências vegetais, 35 realizaram a bioprospecção da flora brasileira, em diversas áreas como Química, Botânica, Fisiologia e Morfologia Vegetal, (Quimio)taxonomia Vegetal, Ecologia de Ecossistemas, Genética Vegetal, Recursos Florestais, Engenharia Florestal, dentre outros, levando a milhares de publicações, ao engajamento de centenas de estudantes e ao entendimento mais profundo dos produtos naturais em diferentes modelos biológicos por meio da análise de micromoléculas auxiliada por estratégias computacionais e espectrométricas, além de avaliações farmacológicas. O desenvolvimento de abordagens ômicas ampliou a visão sobre perfil químico dos organismos, possibilitou o estudo integrado e concomitante de várias amostras, e a anotação mais rápida de moléculas conhecidas, por meio do uso de técnicas hifenadas, quimiométricas e redes moleculares. Isso também contribuiu para superar a falta de informação sobre a segurança e eficácia dos fitopreparados, em projetos que tratam da padronização de produtos fitoterápicos, de acordo com normas internacionais. O programa BIOTA-FAPESP também tem focado em aspectos ambientais, de acordo com os princípios da Química Verde e teve reflexos positivos na colaboração internacional, no número e no impacto das publicações científicas e na parceria com empresas, etapa crucial para agregar valor e expandir a cadeia produtiva de bioprodutos. Ainda, a compilação, sistematização e compartilhamento de dados foram contemplados com a criação da base de dados NUBBEDB, de livre acesso, e que se integra com bases internacionais (ACD/labs, American Chemical Society - ACS), auxiliando pesquisadores e empresas no desenvolvimento de diferentes áreas da ciência, tecnologia, fortalecendo a bioeconomia e subsidiando políticas públicas.

7.
Braz. j. med. biol. res ; 55: e12076, 2022. graf
Article in English | LILACS-Express | LILACS | ID: biblio-1394123

ABSTRACT

Glioblastoma is the most prevalent and malignant brain tumor identified in adults. Surgical resection followed by radiotherapy and chemotherapy, mainly with temozolomide (TMZ), is the chosen treatment for this type of tumor. However, the average survival of patients is around 15 months. Novel approaches to glioblastoma treatment are greatly needed. Here, we aimed to investigate the anti-glioblastoma effect of the combination of matteucinol (Mat) (dihydroxyflavanone derived from Miconia chamissois Naudin) with the chemotherapeutic TMZ in vitro using tumor (U-251MG) and normal astrocyte (NHA) cell lines and in vivo using the chick embryo chorioallantoic membrane (CAM) assay. The combination was cytotoxic and selective for tumor cells (28 μg/mL Mat and 9.71 μg/mL TMZ). Additionally, the combination did not alter cell adhesion but caused morphological changes characteristic of apoptosis in vitro. Notably, the combination was also able to reduce tumor growth in the chick embryo model (CAM assay). The docking results showed that Mat was the best ligand to the cell death membrane receptor TNFR1 and to TNFR1/TMZ complex, suggesting that these two molecules may be working together increasing their potential. In conclusion, Mat-TMZ can be a good candidate for pharmacokinetic studies in view of clinical use for the treatment of glioblastoma.

8.
Rio de Janeiro; s.n; 2022. 172 f p. tab.
Thesis in Portuguese | LILACS | ID: biblio-1378703

ABSTRACT

A presente pesquisa tem por objeto as percepções de estudantes de medicina de uma instituição de ensino superior (IES) privada do interior do Estado do RJ em torno de substâncias ditas de uso para performance. Neste trabalho, elas são entendidas como substâncias, prescritas ou não, utilizadas para o propósito de melhorar alguma função cognitiva ou de humor. Investigamos como as ideias, valores, formação profissional em curso e condições materiais de acesso a medicamentos e outras substâncias colaboram na formação de práticas de uso de medicamentos (prescritos ou não), suplementos e/ou vitaminas por estudantes de medicina. A metodologia de pesquisa utilizada contou com dois procedimentos: 1) a aplicação de um questionário online para mapear os consumos terapêuticos de performance pelos estudantes; 2) entrevistas semiestruturadas em profundidade com estudantes que se voluntariaram a falar sobre suas experiências de uso. Como resultados encontrados, destacam-se práticas de uso de substâncias acionadas pelos estudantes de acordo com suas necessidades acadêmicas ou de vida


This research assumes aims to analyze the perceptions of medical students from a private higher education institution, located in the interior of the State of Rio de Janeiro (RJ), regarding substances used for performance. In this study, they are understood as substances, prescribed or not, used for the purpose of improving some cognitive function or mood. We investigated how ideas, values, ongoing professional training, and material conditions of access to medicines and other substances collaborate in the formation of practices for the use of medicines (prescribed or not), supplements and/or vitamins by medical students. The research methodology adopted was composed of two procedures: 1) the application of an online questionnaire to map the therapeutic consumption of performance by the students; 2) semi-structured interviews with students, who voluntarily talked about their experiences of use. Among the results found, there are practices of substance use triggered by students according to their academic or life needs.


Subject(s)
Humans , Students, Medical , Biological Products , Drug Utilization , Performance-Enhancing Substances
9.
Article in English | WPRIM | ID: wpr-928954

ABSTRACT

OBJECTIVE@#To explore potential natural products against severe acute respiratory syndrome coronavirus (SARS-CoV-2) via the study of structural and non-structural proteins of human coronaviruses.@*METHODS@#In this study, we performed an in-silico survey of 25 potential natural compounds acting against SARS-CoV-2. Molecular docking studies were carried out using compounds against 3-chymotrypsin-like protease (3CLPRO), papain-like protease (PLPRO), RNA-dependent RNA polymerase (RdRp), non-structural protein (nsp), human angiotensin converting enzyme 2 receptor (hACE2R), spike glycoprotein (S protein), abelson murine leukemia viral oncogene homolog 1 (ABL1), calcineurin-nuclear factor of activated T-cells (NFAT) and transmembrane protease serine 2.@*RESULTS@#Among the screened compounds, amentoflavone showed the best binding affinity with the 3CLPRO, RdRp, nsp13, nsp15, hACE2R. ABL1 and calcineurin-NFAT; berbamine with hACE2R and ABL1; cepharanthine with nsp10, nsp14, nsp16, S protein and ABL1; glucogallin with nsp15; and papyriflavonol A with PLPRO protein. Other good interacting compounds were juglanin, betulinic acid, betulonic acid, broussooflavan A, tomentin A, B and E, 7-methoxycryptopleurine, aloe emodin, quercetin, tanshinone I, tylophorine and furruginol, which also showed excellent binding affinity towards a number of target proteins. Most of these compounds showed better binding affinities towards the target proteins than the standard drugs used in this study.@*CONCLUSION@#Natural products or their derivatives may be one of the potential targets to fight against SARS-CoV-2.


Subject(s)
Animals , Antiviral Agents/therapeutic use , Biological Products/pharmacology , COVID-19/drug therapy , Humans , Mice , Molecular Docking Simulation , SARS-CoV-2
10.
Acta Pharmaceutica Sinica B ; (6): 1163-1185, 2022.
Article in English | WPRIM | ID: wpr-929376

ABSTRACT

Cancer immunotherapy has become a new generation of anti-tumor treatment, but its indications still focus on several types of tumors that are sensitive to the immune system. Therefore, effective strategies that can expand its indications and enhance its efficiency become the key element for the further development of cancer immunotherapy. Natural products are reported to have this effect on cancer immunotherapy, including cancer vaccines, immune-check points inhibitors, and adoptive immune-cells therapy. And the mechanism of that is mainly attributed to the remodeling of the tumor-immunosuppressive microenvironment, which is the key factor that assists tumor to avoid the recognition and attack from immune system and cancer immunotherapy. Therefore, this review summarizes and concludes the natural products that reportedly improve cancer immunotherapy and investigates the mechanism. And we found that saponins, polysaccharides, and flavonoids are mainly three categories of natural products, which reflected significant effects combined with cancer immunotherapy through reversing the tumor-immunosuppressive microenvironment. Besides, this review also collected the studies about nano-technology used to improve the disadvantages of natural products. All of these studies showed the great potential of natural products in cancer immunotherapy.

11.
Article in English | WPRIM | ID: wpr-929245

ABSTRACT

Four new sesquiterpene quinone meroterpenoids, dysideanones F-G (1-2) and dysiherbols D-E (3-4), were isolated from the marine sponge Dysidea avara collected from the South China Sea. The new structures were elucidated by extensive analysis of spectroscopic data including HR-MS and 1D and 2D NMR spectra, and their absolute configurations were assigned by single-crystal X-ray diffraction and ECD calculations. Anti-inflammatory evaluation showed that dysiherbols D-E (3-4) exhibited moderate inhibitory activity on TNF-α-induced NF-κB activation in human HEK-293T cells with IC50 values of 10.2 and 8.6 μmol·L-1, respectively.


Subject(s)
Animals , Dysidea/chemistry , Porifera , Quinones/pharmacology , Sesquiterpenes/pharmacology , Skeleton
12.
Article in English | WPRIM | ID: wpr-929232

ABSTRACT

Natural products (NPs), especially those from traditional herbal medicines, can evidently modulate human gene expression at multiple levels, leading to a wide diversity of bioactivities. Although numerous bio-functions of NPs for human body have been found, there is little understanding about how NPs achieve it, as less attention was drawn to the definite mechnism by which NPs regulate gene expression. Furthermore, based on the rapidly advancing knowledge of mechanisms for gene regulation in recent years, newly-understood mechanisms, such as post-transcriptional regulation, are found to be involved in NP-elicited bio-effects, providing a new perspective on understanding the role of NPs in gene expression. Therefore, in the current review, we summarize the function of NPs in gene expression from the perspectives of transcriptional, post-transcriptional, and post-translational regulation, which will reinforce the understanding of NP-induced effects in gene expression and facilitate the exploration of more NPs with potential therapeutic effects.


Subject(s)
Biological Products/pharmacology , Gene Expression , Gene Expression Regulation , Humans
13.
Acta Pharmaceutica Sinica B ; (6): 3113-3123, 2022.
Article in English | WPRIM | ID: wpr-939962

ABSTRACT

P-glycoprotein (P-gp) highly expressed in cancer cells can lead to multidrug resistance (MDR) and the combination of anti-cancer drugs with P-gp inhibitor has been a promising strategy to reverse MDR in cancer treatment. In this study, we established a label-free and detergent-free system combining surface plasmon resonance (SPR) biosensor with styrene maleic acid (SMA) polymer membrane proteins (MPs) stabilization technology to screen potential P-gp inhibitors. First, P-gp was extracted from MCF-7/ADR cells using SMA polymer to form SMA liposomes (SMALPs). Following that, SMALPs were immobilized on an SPR biosensor chip to establish a P-gp inhibitor screening system, and the affinity between P-gp and small molecule ligand was determined. The methodological investigation proved that the screening system had good specificity and stability. Nine P-gp ligands were screened out from 50 natural products, and their affinity constants with P-gp were also determined. The in vitro cell verification experiments demonstrated that tetrandrine, fangchinoline, praeruptorin B, neobaicalein, and icariin could significantly increase the sensitivity of MCF-7/ADR cells to Adriamycin (Adr). Moreover, tetrandrine, praeruptorin B, and neobaicalein could reverse MDR in MCF-7/ADR cells by inhibiting the function of P-gp. This is the first time that SMALPs-based stabilization strategy was applied to SPR analysis system. SMA polymer can retain P-gp in the environment of natural lipid bilayer and thus maintain the correct conformation and physiological functions of P-gp. The developed system can quickly and accurately screen small molecule ligands of complex MPs and obtain affinity between complex MPs and small molecule ligands without protein purification.

14.
Rev. cuba. estomatol ; 58(3): e3639, 2021. tab, graf
Article in English | LILACS, CUMED | ID: biblio-1347435

ABSTRACT

Introduction: Studies suggested that phytochemical products are considered potential solutions to smear layer removal due to their biological safety in cleaning root canal systems, lower toxicity, lower irritant effect and antimicrobial effect. Objective: The aim of the present study was to perform a systematic review to evaluate smear layer removal of root canal systems by different natural product solutions. Methods: systematic review. Search of the literature was performed on Pubmed, Scopus, Cochrane, Web of Science, Scielo and Google Scholar according the PRISMA protocol. Studies were included if they performed the experiments of smear layer removal on extracted permanent human teeth. Articles published in any language without restriction of year of publication were included in this review. The risk of bias assessment in the included studies was evaluated using the Joanna Briggs Institute Critical Appraisal Checklist for Quasi-Experimental Studies. The search strategy resulted in the retrieval of 6221 publications. After the eligibility criteria application, 8 articles were selected for analysis. Results: It was observed that some natural products solutions showed effects on smear layer removal, especially on coronal third. The phytochemical products such as Salvadora persica, chamomile alcohol extract and grape seed extract demonstrated good potential of smear layer removal, however, its effectiveness and clinical applicability are still unclear. Conclusions: Although the limitations of this study, it is possible to highlight those phytochemical products such as Salvadora persica, chamomile alcohol extract and grape seed extract that demonstrated good potential on SL removal(AU)


Introducción: Los productos fitoquímicos se consideran soluciones potenciales para la eliminación del barro dentinario debido a su seguridad biológica en la limpieza del sistema de conductos radiculares, menor toxicidad, menor efecto irritante y efecto antimicrobiano. Objetivo: Evaluar la eliminación del barro dentinario de los sistemas de conductos radiculares mediante diferentes soluciones de productos naturales. Métodos: La búsqueda de la literatura se realizó en Pubmed, Scopus, Cochrane, Web of Science, SciELO y Google Scholar, según el protocolo PRISMA. Los estudios se incluyeron si realizaron los experimentos de eliminación del barro dentinario en dientes humanos permanentes extraídos. En esta revisión se incluyeron artículos publicados en cualquier idioma, sin restricción de año de publicación. La evaluación del riesgo de sesgo en los estudios incluidos se evaluó mediante la lista de verificación de evaluación crítica del Instituto Joanna Briggs para estudios cuasiexperimentales. La estrategia de búsqueda resultó en la recuperación de 6221 publicaciones. Después de la aplicación de los criterios de elegibilidad, se seleccionaron 8 artículos para su análisis. Resultados: Se observó que algunas soluciones de productos naturales mostraron efectos sobre la eliminación del barro dentinario, especialmente en el tercio coronal. Los productos fitoquímicos como salvadora pérsica, extracto de alcohol de manzanilla y extracto de semilla de uva demostraron un buen potencial de eliminación del barro dentinario; sin embargo, su efectividad y aplicabilidad clínica aún no están claras. Conclusiones: A pesar de las limitaciones de este estudio, es posible destacar aquellos productos fitoquímicos como salvadora pérsica, extracto de alcohol de manzanilla y extracto de semilla de uva demostraron buen potencial de eliminación del barro dentinario(AU)


Subject(s)
Humans , Root Canal Irrigants/adverse effects , Biological Products/therapeutic use , Smear Layer , Phytochemicals/therapeutic use , Review Literature as Topic , Databases, Bibliographic , Grape Seed Extract/administration & dosage
15.
Rev. cuba. med. trop ; 73(1): e573, tab, graf
Article in Spanish | LILACS, CUMED | ID: biblio-1280324

ABSTRACT

. Introducción: El dengue es la enfermedad viral transmitida por mosquitos de más rápida propagación en el mundo. A pesar de la alta incidencia de la enfermedad no existe tratamiento antiviral efectivo ni vacuna aprobada para su uso contra esta infección. La planta Ageratina havanensis ha sido ampliamente utilizada por nuestra cultura popular y en otros países debido a sus diversas propiedades biológicas. Objetivo: Evaluar la actividad antiviral de cuatro extractos provenientes de Ageratina havanensis y dos flavonoides aislados de dicha planta frente al virus dengue 2. Métodos: La pesquisa primaria de actividad antiviral de cada extracto y flavonoide se realizó mediante el ensayo de detección de la productividad vírica, y se evaluó la acción virucida de los extractos etanólico de tallo y butanólico de hoja. Resultados: Todos los extractos inhibieron la replicación viral al evidenciarse disminución del número de placas de lisis, sin embargo, no se evidenció disminución del título infectivo viral en el ensayo virucida. El tratamiento con la sakuranetina mostró valores de inhibición de la productividad viral entre 61-91 por ciento, y para la 7-metoxiaromadendrina se registraron valores de reducción viral entre 64-86 por ciento. Conclusiones: Los extractos y flavonoides aislados de Ageratina havanensis mostraron acción antiviral. Los extractos etanólico de tallo y butanólico de hojas no poseen acción virucida sobre la cepa viral empleada. El presente trabajo constituye el primer informe respecto a la evaluación de extractos y compuestos aislados de A. havanensis frente al virus dengue(AU)


Introduction: Dengue is the fastest spreading mosquito-borne viral disease worldwide. Despite its high incidence, no effective antiviral treatment or vaccine has been approved for use against this infection. The plant Ageratina havanensis has been widely used in our folk culture and in other countries due to its various biological properties. Objective: Evaluate the antiviral activity of four extracts from Ageratina havanensis and two flavonoids isolated from that plant against the dengue 2 virus. Methods: Primary screening of the antiviral activity of each extract and flavonoid was conducted by viral productivity detection assay, and an evaluation was carried out of the virucidal action of the stem ethanolic extract and the leaf butanolic extract. Results: All the extracts inhibited viral replication by a reduction in the number of lysis plates. However, no evidence was found of a reduced viral infective titer in the virucidal assay. Treatment with sakuranetin achieved viral productivity inhibition values of 61 percent-91 percent, whereas 7-methoxyaromadendrin obtained viral reduction values of 64 percent-86 percent Conclusions: The extracts and flavonoids isolated from Ageratina havanensis displayed antiviral activity. The stem ethanolic extract and the leaf butanolic extract do not have a virucidal action against the viral strain used. The paper is the first report about the effect of extracts and compounds isolated from A. havanensis against the dengue virus(AU)


Subject(s)
Humans , Microscopy, Electron, Scanning Transmission , Ageratina , Dengue , Dengue Virus
16.
Saude e pesqui. (Impr.) ; 14(1): 113-123, jan-mar 2021.
Article in Portuguese | LILACS-Express | LILACS | ID: biblio-1254255

ABSTRACT

O objetivo deste estudo foi avaliar os efeitos do timol e carvacrol contra Aspergillus flavus e a produção de aflatoxinas. Foram determinadas a concentração inibitória mínima (CIM), o espectro fungitóxico e a atividade inibidora de micotoxinas pelo timol e carvacrol. Os resultados mostraram que timol e carvacrol exibiram ação fungicida de acordo com a CIM de 2500 e 30 µg mL-1, respectivamente. Tanto o timol quanto o carvacrol inibiram significativamente o crescimento de A. flavus (p<0,05) a partir de 600 e 15 µg mL-1, respectivamente. A biomassa fúngica, estimada pela determinação da concentração de ergosterol, foi significativamente reduzida (p <0,05) em 2500 µg mL-1 de timol e 250 µg mL-1 de carvacrol. O timol e o carvacrol exibiram efeitos antiaflatoxigênicos em 600 e 125 µg mL-1, respectivamente. O timol e o carvacrol exibiram atividade antifúngica, mas não exibiram alta atividade antiaflatoxigênica. Carvacrol e timol podem ser considerados como potentes compostos naturais antifúngicos contra A. flavus.


The aim of this study was to evaluate the effects of thymol and carvacrol upon production of aflatoxins by Aspergillus flavus and upon its growth. Minimal inhibitory concentration (MIC), fungitoxic spectrum and mycotoxin inhibition were assessed. Results showed thymol and carvacrol exhibited fungicidal action, as determined by MIC values of 2500 and 30 µg mL-1, respectively. Both thymol and carvacrol significantly inhibited growth of A. flavus (p<0.05) at concentrations of 600 and 15 µg mL-1, respectively. Fungal biomass, as estimated by determination of ergosterol concentration, was significantly reduced (p<0.05) at thymol concentrations of 2500 µg mL-1 and at carvacrol concentrations of 250 µg mL-1. Thymol and carvacrol exhibited antiaflatoxigenic effects at concentrations of 600 and 125 µg mL-1, respectively. While both thymol and carvacrol showed possessing antifungal activities, neither were highly antiaflatoxigenic. Carvacrol and thymol might be considered for use as potential antifungal natural compounds against A. flavus.

17.
Biota Neotrop. (Online, Ed. ingl.) ; 21(2): e20201069, 2021. tab, graf
Article in English | LILACS-Express | LILACS | ID: biblio-1180714

ABSTRACT

Abstract: This is a systematic review of scientific articles reporting the biodiversity of endophytic fungi isolated from endemic Cerrado plants in Brazil and exposes the potential applications of these microorganisms in the production of known and new metabolites. The "Portal de Periódicos" (CAPES), Science Direct, PubMed, Scielo, and Biblioteca Virtual em Saúde (BVS) databases were used. A total of 418 articles were found using the following sets of keywords: Endophytic, fungi, and Cerrado; endophytic, fungi, rupestrian, and grass lands; endophytic, fungi, Brazilian, and savanna; among these, 14 articles were selected. The articles were grouped into studies on the biodiversity of Cerrado endophytic fungi, chemical studies, and other subjects. All the articles were found to be related to the diversity present in the Cerrado of the southeastern and midwestern regions, they show high fungal biodiversity with Diaporthe genus predominant in almost all plants studied. In all the studies on the chemical diversity of endophytic fungi, new compounds or new natural products were found associated with a range of bioactivity, especially antifungal. It shows the great potential of endophytes in the production of new and bioactive secondary metabolites, as well as the unexplored chemical diversity of endophytes isolated from endemic plant species. The review shows that rare studies performed in regions where the Cerrado biome are predominant, including the central, north, and northeast regions, representing an important niche that is still unexplored.


Resumo: Esta é uma revisão sistemática de artigos científicos que relatam a biodiversidade de fungos endofíticos isolados de plantas endêmicas do Cerrado no Brasil, e expõe as possíveis aplicações desses microrganismos na produção de metabólitos novos e conhecidos. Foram utilizadas as bases de dados "Portal de Periódicos" (CAPES), Science Direct, PubMed, Scielo e Biblioteca Virtual em Saúde (BVS). Foram encontrados 418 artigos, usando os seguintes conjuntos de palavras-chave: Endophytic, fungi, and Cerrado; endophytic, fungi, rupestrian, and grasslands; endophytic, fungi, Brazilian, and savanna. Destes, 14 artigos foram selecionados. Os artigos foram agrupados em estudos sobre a biodiversidade de fungos endofíticos do Cerrado, estudos químicos e outros estudos. Todos os artigos foram relacionados à diversidade presente no Cerrado das regiões sudeste e centro-oeste, estes apresentam alta biodiversidade fúngica, com o gênero Diaporthe predominando em quase todas as plantas estudadas. Em todos os estudos sobre a diversidade química de fungos endofíticos, novos compostos ou novos produtos naturais foram identificados, associados a uma série de bioatividades, especialmente antifúngica. Isso mostra o grande potencial dos endófitos na produção de metabólitos secundários novos e bioativos, bem como a diversidade química inexplorada de endófitos isolados de espécies de plantas endêmicas. Esta revisão mostra que raros estudos foram realizados em regiões onde o bioma Cerrado é predominante, incluindo as regiões central, norte e nordeste, que representam um nicho importante ainda inexplorado.

18.
Acta Pharmaceutica Sinica B ; (6): 1446-1468, 2021.
Article in English | WPRIM | ID: wpr-888814

ABSTRACT

The 90-kiloDalton (kD) heat shock protein (Hsp90) is a ubiquitous, ATP-dependent molecular chaperone whose primary function is to ensure the proper folding of several hundred client protein substrates. Because many of these clients are overexpressed or become mutated during cancer progression, Hsp90 inhibition has been pursued as a potential strategy for cancer as one can target multiple oncoproteins and signaling pathways simultaneously. The first discovered Hsp90 inhibitors, geldanamycin and radicicol, function by competitively binding to Hsp90's N-terminal binding site and inhibiting its ATPase activity. However, most of these N-terminal inhibitors exhibited detrimental activities during clinical evaluation due to induction of the pro-survival heat shock response as well as poor selectivity amongst the four isoforms. Consequently, alternative approaches to Hsp90 inhibition have been pursued and include C-terminal inhibition, isoform-selective inhibition, and the disruption of Hsp90 protein-protein interactions. Since the Hsp90 protein folding cycle requires the assembly of Hsp90 into a large heteroprotein complex, along with various co-chaperones and immunophilins, the development of small molecules that prevent assembly of the complex offers an alternative method of Hsp90 inhibition.

19.
Article in English | WPRIM | ID: wpr-888793

ABSTRACT

Natural products are one of the important sources for the discovery of new drugs. Betulinic acid (BA), a pentacyclic triterpenoid widely distributed in the plant kingdom, exhibits powerful biological effects, including antitumor activity against various types of cancer cells. A considerable number of BA derivatives have been designed and prepared to remove their disadvantages, such as poor water solubility and low bioavailability. This review summarizes the current studies of the structural diversity of antitumor BA derivatives within the last five years, which provides prospects for further research on the structural modification of betulinic acid.

20.
Article in English | WPRIM | ID: wpr-888786

ABSTRACT

Candida is an intractable life-threatening pathogen. Candida infection is extremely difficult to eradicate, and thus is the major cause of morbidity and mortality in immunocompromised individuals. Morevover, the rapid spread of drug-resistant fungi has led to significant decreases in the therapeutic effects of clinical drugs. New anti-Candida agents are urgently needed to solve the complicated medical problem. Natural products with intricate structures have attracted great attention of researchers who make every endeavor to discover leading compounds for antifungal agents. Their novel mechanisms and diverse modes of action expand the variety of fungistatic agents and reduce the emergence of drug resistance. In recent decades, considerable effort has been devoted to finding unique antifungal agents from nature and revealing their unusual mechanisms, which results in important progress on the development of new antifungals, such as the novel cell wall inhibitors YW3548 and SCY-078 which are being tested in clinical trials. This review will present a brief summary on the landscape of anti-Candida natural products within the last decade. We will also discuss in-depth the research progress on diverse natural fungistatic agents along with their novel mechanisms.


Subject(s)
Antifungal Agents/pharmacology , Biological Products/pharmacology , Candida/drug effects , Candidiasis/drug therapy , Humans , Microbial Sensitivity Tests
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