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1.
Acta Pharmaceutica Sinica ; (12): 1372-1382, 2023.
Article in Chinese | WPRIM | ID: wpr-978678

ABSTRACT

italic>O-methyltransferases (OMTs) are one of the key tailoring enzymes in the biosynthesis of many natural products, O-methylation can not only reduce the reactivity of natural products, but also alter their solubility, stability and biological activities. Based on the transcriptome data of Ardisia japonica, a full-length cDNA sequence of candidate OMT (termed as AjOMT1) was cloned by reverse transcription-polymerase chain reaction (RT-PCR) and expressed in Escherichia coli (E. coli) for the first time. In vitro enzyme catalytic activity assay showed that the recombinant AjOMT1 could effectively catalyze quercetin to form O-methylated products. Most importantly, AjOMT1 showed unprecedented substrate promiscuity towards structurally various compounds including flavonoids, stilbenes, coumarins, alkaloids and phenylpropanoids, especially preferring to the compounds with adjacent phenolic hydroxyl groups, and showed regio-selectivity. These results suggested that AjOMT1 could be used as the tool enzyme to conduct O-methylation of different types of compounds to produce diverse active methylated products, and provide a new method for drug discovery, even universal part for synthetic biology of natural products.

2.
Salud bienestar colect ; 4(1): 84-94, ene.-abr. 2020.
Article in Spanish | LILACS | ID: biblio-1179993

ABSTRACT

INTRODUCCIÓN: la promiscuidad activa indica una condición sexual psicológica y comportamiento mental de la persona que vive plenamente en misma sin ningún tipo de ataduras. Por el otro lado la pasiva indica una condición sexual psicológica de cualquier persona cuyos actos no siempre son acordes a su sexualidad voluntaria. OBJETIVOS: determinar las causas y consecuencias de la promiscuidad en los adolescentes del Colegio San Antonio de la ciudad de Milagro, Periodo 2018-2019, analizar la influencia de los medios de comunicación sobre las relaciones sexuales a temprana edad. METODOLOGÍA: en este trabajo se utiliza una técnica bibliográfica-documental y de corte transversal descriptivo, se utilizó plataformas virtuales como Scielo y obteniendo datos de los últimos años, también se tomó una muestra de 100 estudiantes entre las edades de los 18 a 19 años del colegio San Antonio de la Ciudad de Milagro, aplicando una encuesta de 10 ítems en donde se utilizó para la recolección de información. RESULTADOS: el 51% de los encuestados declaró que eran sexualmente activos y el 34% manifestó que han tenido de 2-5 parejas, mientras que el 15% dijo que han tenido entre 6-9 parejas hasta la actualidad. CONCLUSIÓN: este estudio pudo indicar que es importante que los adolescentes lleven una vida sexual con responsabilidad y que los medios de comunicación son una influencia de que los adolescentes comiencen sus relaciones sexuales a temprana edad y que conozcan los tipos de métodos anticonceptivos para cuidarse.


INTRODUCTION: active promiscuity indicates a psychological sexual condition and mental behavior of the person who lives fully in promiscuity without any bindings. On the other hand, the passive indicates a psychological sexual condition of any person whose actions are not always in line with their voluntary sexuality. OBJECTIVES: to determine the causes and consequences of promiscuity in adolescents of the San Antonio College of the city of Milagro Period 2018-2019, analyze the influence of the media on sexual relations at an early age. METHODOLOGY: in this work a bibliographic-documentary and descriptive cross-sectional technique is used, virtual platforms such as Scielo were used and obtaining data from recent years, a sample of 100 students was also taken between the ages of the 18 to 19 years of the San Antonio School of the City of Miracle, applying a survey of 10 items where it was used for the collection of information. RESULTS: 51% of respondents said they were sexually active and 34% said they have had 2-5 couples while 15% said they have had 6-9 partners to date. CONCLUSION: this study may indicate that it is important for adolescents to lead a sexual life responsibly and that the media is an influence on adolescents starting their sex at an early age and knowing the types contraceptive methods to take care of the way.


Subject(s)
Humans , Male , Female , Adolescent , Sexual Behavior/psychology , Sexuality/physiology , Sexuality/psychology , Epidemiology, Descriptive , Cross-Sectional Studies , Ecuador
3.
Chinese Herbal Medicines ; (4): 440-445, 2020.
Article in Chinese | WPRIM | ID: wpr-841996

ABSTRACT

Objective: In order to obtain new glycosyltransferases with highly efficient catalysis, the glycosyltransferases from Carthamus tinctorius which contains diverse types of glycosides were mined. Methods: A new glycosyltransferase gene (UGT88B2) with full length was obtained by PCR and further transformed into Escherichia coli for heterologous expression. The catalytic activity of recombinant UGT88B2 was determined by HPLC-MSn. The structures of representative catalytic products were elucidated by MS and NMR. Results: UGT88B2 exhibited catalytic promiscuity and various patterns in glycosylation of flavonoids with high efficiency. Conclusion: A new glycosyltransferase named UGT88B2 was successfully mined and can be employed as enzymatic tools in glycosylation of flavonoids.

4.
Acta Pharmaceutica Sinica ; (12): 2012-2025, 2018.
Article in Chinese | WPRIM | ID: wpr-780084

ABSTRACT

Currently, single-target drugs are often difficult to achieve the desired results in the treatment of multifactorial diseases such as tumors, cardiovascular and endocrine diseases, and may also cause toxicity. Multi-target drugs can improve the efficacy, reduce side effect and drug resistance by regulating multiple links of the disease, showing good prospects for the application. The main aim of this article is to review the strategies of designing multi-target directed ligands (MTDLs) (including conjugated-pharmacophore, fused-pharmacophore and merged-pharmacophore) and the research progress in recent years. The existing problems and challenges of multi-target drugs are also discussed, to provide new ideas for the study of multi-target drugs.

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