In Vitro Anti-Toxoplasma Activity of Extracts Obtained from Tabebuia rosea and Tabebuia chrysantha: The Role of ß-Amyrin.

Toxoplasmosis is a parasitic disease caused by the protozoan Toxoplasma gondii that is highly prevalent worldwide. Although the infection is asymptomatic in immunocompetent individuals, it severely affects immunocompromised individuals, causing conditions such as encephalitis, myocarditis, or pneumonitis. The limited therapeutic efficacy of drugs currently used to treat toxoplasmosis has prompted the search for new therapeutic alternatives. The aim of this study was to determine the anti-Toxoplasma activity of extracts obtained from two species of the genus Tabebuia. Twenty-six extracts, 12 obtained from Tabebuia chrysantha and 14 from Tabebuia rosea, were evaluated by a colorimetric technique using the RH strain of T. gondii that expresses ß-galactosidase. Additionally, the activity of the promising extracts and their active compounds was evaluated by flow cytometry. ß-amyrin was isolated from the chloroform extract obtained from the leaves of T. rosea and displayed important anti-Toxoplasma activity. The results show that natural products are an important source of new molecules with considerable biological and/or pharmacological activity.

Scale-Up of the Fermentation Process for the Production and Purification of Serratiopeptidase Using Silkworm Pupae as a Substrate.

Serratiopeptidase, a bacterial metalloprotease known for its pain-relieving and anti-inflammatory properties, can be produced through fermentation with S. marcescens. This study aimed to identify key factors related to nutrient composition and physicochemical conditions for production in Erlenmeyer flasks and to scale up the mixture to a bioreactor to obtain the maximum proteolytic activity. A Plackett-Burman design was used to determine whether the presence of silkworm pupae (at 1.5%) was a significant parameter for serratiopeptidase production. Along with the variables pH, temperature, and time, they were optimized using a Taguchi experimental design, resulting in values of 7, 25 °C, and 36 h, respectively. Scaling up with a kLa of 25.45 ± 3.12 h-1 showed the highest serratiopeptidase production at 24 h. A factorial design was used for ultrafiltration, resulting in an LMH (liters per square meter per hour) of 960 L/m2h, a TMP (transmembrane pressure) of 15 psi, and a concentration factor of five, with a specific activity of 24,325.81 ± 1515.69 U/mg. Afterward, the retentate was purified using strong anion exchange chromatography and ultrafiltration, yielding a 19.94 ± 3.07% recovery and a purification factor of 1.59 ± 0.31. In conclusion, waste from the sericulture industry can be used for serratiopeptidase production.

Antiproliferative activity of thiazole and oxazole derivatives: A systematic review of in vitro and in vivo studies.

Thiazole and oxazole are compounds with a heterocyclic nucleus that have attracted the attention of medicinal chemistry due to the great variety of biological activities that they enable. In recent years, their study has increased, finding a wide range of biological activities, including antifungal, antiparasitic, anti-inflammatory, and anticancer activities. This systematic review provides evidence from the literature on the antiproliferative and antitumor activities of thiazole and oxazole and their derivatives from 2014 to April 2020. Three bibliographical databases were consulted (PubMed, Web of Science, and Scopus), and a total of 32 studies were included in this paper based on our eligibility criteria. The analysis of the activity-structure relationship allows us to conclude that most of the promising compounds identified contained thiazole nuclei or derivatives.

Activation of the Keap1-Nrf2 pathway by specioside and the n-butanol extract from the inner bark of Tabebuia rosea (Bertol) DC.

Background: A large number of chemical compounds exert their antioxidant effects by activation of key transcriptional regulatory mechanisms, such as the transcription factor Nrf2. The aim of this study was to evaluate the activation of the Keap1-Nrf2 pathway by both the n-butanol extract obtained from the inner bark of Tabebuia rosea (Bertol) DC and specioside isolated from this extract. Methods: The antioxidant activity of the extract and specioside isolated from the inner bark of T. rosea were evaluated using the oxygen radical absorbance capacity (ORAC) and the 2,2-diphenyl-1-picrylhydrazyl radical scavenging activity (DPPH) techniques, whereas their effects on the viability of HepG2 cells was determined using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method. The effects of the compound and the extract on activating the Keap1-Nrf2 pathway were evaluated using a Nrf2 Transcription Factor Assay kit. Induction of the Nrf2-mediated antioxidant response genes HMOX-1 and NQO1 was evaluated by real-time PCR. The protective effects against H 2O 2-induced oxidative stress in HepG2 cells was determined as the percent protection using the MTT method. Results: Both the n-butanol extract and specioside exhibited activity at low concentrations without affecting cellular viability, since the cell viability was greater than 80% after 24 hours of exposure at each tested concentration. In addition, Nrf2 dissociated from Keap1 after treatment with the n-butanol extract at a concentration of 0.25 µg/mL after 4 hours of exposure. An increase in the Nrf2 level in the cytoplasm after 4 hours of exposure to 2 µM specioside was observed. Nrf2 levels stabilized in the nucleus 12 hours after stimulation with both specioside and the extract. After 6 hours of stimulation, both the extract and specioside induced the expression of HMOX-1 and NQO1. Conclusion: The n-butanol extract from the inner bark of T. rosea and specioside produced protective effects against H 2O 2-induced oxidative stress in HepG2 cells.

Purification and characterization of a metalloprotease produced by the C8 isolate of Serratia marcescens using silkworm pupae or casein as a protein source.

Serratiopeptidase, a metalloprotease produced by Serratia marcescens, is produced through a fermentation process using carbohydrates and proteins as carbon and nitrogen sources. However, some byproducts of the silk industry could be an alternative source for serratiopeptidase production. Therefore, the present work is focused on the purification and characterization of a serratiopeptidase produced from the C8 isolate of Serratia marcescens and obtained from a Colombian silkworm hybrid using casein or silkworm pupae. The protease was purified using ultrafiltration, anion-exchange, and size-exclusion chromatography. The purified enzyme showed a molecular weight of ~50 kDa with a purity above 96%, an isoelectric point of ~4.6, optimum pH and temperature of 6 and 50 °C, and stability at 4 °C for one month. The kinetic constants using azocasein as substrate were 0.63 mM (Km), 2,016 µM/min (Vmax), 41.41 s-1 (Kcat), and 6.56 × 107 M-1 s-1 (Kcat/Km). Inhibition by 5 mM EDTA or 1,10-phenanthroline was recovered by adding Zn2+ at the same concentration. Mass spectrometry analysis indicated 94% homology with the sequence of serratiopeptidase produced by the E-15 strain. We purified and characterized a serratiopeptidase produced by the C8 isolate of S. marcescens in a culture medium based on a renewable source from the silk industry.

Anti-inflammatory activity of triazine derivatives: A systematic review.

Triazines are heterocyclic compounds with a variety of biological activities that have been increasingly studied in recent years due to their versatile structure (three isoforms) and the different derivatives that can be synthesized from them to ensure functional motifs. This systematic review provides the evidence in the literature of the in vitro and in vivo anti-inflammatory activity of triazine derivatives from 2008 to June 2018. Four bibliographical databases were consulted (PubMed, Web of Science, EMBASE and Scopus), and a total of 48 studies were included in this paper based on our eligibility criteria. Although 35.17% of evaluated triazines were demonstrated to be promising anti-inflammatory agents, further studies need to be conducted to explore their pharmacological profiles in the medical research of drug discovery to control the risk factors and pathophysiology of several chronic inflammation-based diseases.

Anti-infectious activity in plants of the genus Tabebuia / Actividad anti-infecciosa en plantas del género Tabebuia / Atividade anti-infecciosa em plantas do género Tabebuia

Infectious diseases are a worldwide public health problem. There is growing research in the field of new plant-based drugs for treating such diseases. Our objective was to perform a systematic literature review to evaluate the anti-infectious activity (antibacterial, antifungal, antiviral and antiparasitic) attributed to plants of the Tabebuia (Bignoniaceae) genus. We conducted a search for the period of 2000-2013 in ScienceDirect, Scopus, PubMed, Embase, Napralert and SciELO databases using the following MeSH terms: Tabebuia, biological activity, bioactive compounds, chemical compounds, diseases, traditional medicine, tropical infections, infections and treatment. We found ethnobotanical and experimental (in vitro) evidence supporting the use of Tabebuia species for treating infectious diseases. In addition, the compounds responsible for their antimicrobial activity have been isolated, and their structures have been elucidated, emphasizing among them naphthoquinones such as lapachol. Natural products isolated from Tabebuia plants may be an alternative for developing new anti-infectious agents.

Dada la importancia de las enfermedades infecciosas como problema de salud pública a nivel mundial y la búsqueda de nuevos medicamentos basados en plantas para tratar dichas enfermedades; se realizó una revisión sistemática de literatura con el fin de evaluar la actividad anti-infecciosa (antibacteriana, antifúngica, antiviral y antiparasitaria) reportada en plantas pertenecientes al género Tabebuia (Bignoniaceae). Las bases de datos fueron: ScienceDirect, Scopus, Pubmed, Embase y Napralert, SciELO, durante 2000 - 2013. Se utilizaron términos en MeSH como: Tabebuia, biological activity, bioactive compounds, chemical compounds, diseases, traditional medicine, tropical infections, infections and treatment. Existe evidencia tanto etnobotánica como experimental (in vitro) que soporta el uso de especies del género Tabebuia en el tratamiento de enfermedades infecciosas. Adicionalmente, se encontró reportado y se esclareció estructuralmente los compuestos responsables de la actividad antimicrobiana, donde se destacan naftoquinonas como el lapachol. Se concluye a partir de la revisión que los productos naturales aislados de las plantas del género Tabebuia podrían considerarse alternativas para el desarrollo de nuevos agentes anti-infecciosos.

Dada a importância das doenças infecciosas como problema de saúde pública a nível mundial e a procura crescente de novos medicamentos baseados em plantas para tratar tais doenças, realiza se uma pesquisa sistematizada da literatura com o fim de avaliar a atividade anti-infecciosa (antibacteriana, antifúngica, antiviral y antiparasitária) reportada em plantas pertenecientes ao género Tabebuia (Bignoniaceae). Foi realizada uma pesquisa nas bases de dados ScienceDirect, Scopus, Pubmed, Embase y Napralert, assim como em SciELO, durante o período 2000 - 2013, empregando os términos MeSH: Tabebuia, biological activity, bioactive compounds, chemical compounds, diseases, traditional medicine, tropical infections, infections and treatment. Existe evidencia tanto etnobotánica como experimental (in vitro) que suporta o uso das espécies do género Tabebuia no tratamento das doenças infecciosas e adicionalmente, há sido isolado e identificado estruturalmente os compostos responsáveis da sua atividade antimicrobiana, donde se destacam as naftoquinonas como o lapachol. Os produtos naturais isolados de plantas do género Tabebuia poderiam considerar se como uma alternativa para o desarrolho de novos agentes anti-infecciosos.