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1.
J Food Sci ; 89(2): 1114-1126, 2024 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-38161280

RESUMEN

Papaya postharvest management using low-temperature storage is discouraged as it is a tropical fruit. Extensive research is going on to preserve papaya quality at ambient storage using edible coatings and its composites. The present investigation examined the effects of an eco-safe composite edible coating consisting of hydrocolloid carboxymethyl cellulose (CMC) (1%), guar gum (1.5%), xanthan gum (0.3%), and Gum Arabic (10%) combined with papaya leaf extract (PLE) (1:1 ratio by volume) applied as dip treatment on "Red Lady" papaya fruit at ambient storage condition. Among all the attempted treatments, "PLE incorporated with CMC (1%)" was found to be the best, as the treated fruit exhibited the highest levels of biochemicals, whereas the lowest levels of physiological and enzymatic activity, which positively affected the shelf life. The "CMC + PLE" treatment enhanced the fruit gloss score by 70.1%, phenolics by 6.1%, ascorbic acid by 22.3%, total carotenoid content by 7.4%, and fruit predilection score by 22.0% over the control fruit. However, it lowered (controlling) the physiological loss in weight by 51.0%, decay incidence by 66.6%, and polygalacturonase and pectin methylesterase activity by 24.92% and 35.29%, respectively, over control. Moreover, this treatment exhibited the highest fruit purchase predilection score and prolonged the storage life for >3 days on the physiological loss standard basis (≤10%). This study indicates that "CMC (1%) with PLE (1:1)" composite coating application on papaya under ambient conditions might be an effective, environmentally friendly, and health-friendly way to retain the quality and extend the storage life.


Asunto(s)
Carica , Películas Comestibles , Humanos , Conservación de Alimentos , Frutas/química , Extractos Vegetales/análisis
2.
Chem Biodivers ; 20(11): e202300971, 2023 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-37882429

RESUMEN

Mycobacterium tuberculosis (Mtb) has numerous cell wall and non-cell wall mediated receptors for drug action, of which cell wall mediated targets were found to be more promising because of their pivotal role in bacterial protection and survival. Herein, we reported the design and synthesis of a series of pyrazole-linked triazoles based on the reported structural features of promising drug candidates that target DprE1 receptors through a Structure-based drug design (SBDD) approach (6a-6j and 7a-7j). The synthesized compounds were evaluated for their in-vitro antitubercular activity against virulent strains of Mtb H37Rv. In-silico studies revealed that most compounds exhibit binding interactions with crucial amino acids like Lys418, Tyr314, Tyr60, and Asp386 at DprE1. Furthermore, the protein-ligand (7j) shows appreciable stability compared to innate protein in a 100 ns molecular dynamic simulation study. In-vitro MAB assay revealed that 14 compounds exhibit significant antitubercular activity with minimum inhibitory concentration (MIC) of the 3.15-4.87 µM of the 20 compounds tested. An in-vitro cytotoxicity study on normal cell lines (MCF10) revealed safe compounds (IC50 values:341.85 to 726.08 µM). Hence, the present study opens the development of new pyrazole-linked triazoles as probable DprE1 inhibitors.


Asunto(s)
Antituberculosos , Mycobacterium tuberculosis , Simulación de Dinámica Molecular , Simulación del Acoplamiento Molecular , Triazoles/química , Diseño de Fármacos , Pirazoles/farmacología , Relación Estructura-Actividad , Pruebas de Sensibilidad Microbiana
3.
Int J Risk Saf Med ; 33(1): 23-26, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-33967060

RESUMEN

BACKGROUND: Pheniramine abuse is reported not only in patients with psychiatric disorders but also in the general population. CASE REPORT: We report a case of pheniramine dependence in a patient with obsessive-compulsive disorder. The patient took about 250 mg orally daily and injected about 90 mg every week from the last six months. It reduced his anxiety, was cheaper than his other psychiatric medications, and free of stigma. He had lethargy, headache, uneasiness, anxiety, and poor sleep as withdrawal symptoms. RESULTS: This case highlights the vulnerability of those with psychiatric disorders towards pheniramine abuse. Hence, this report advocates the strict evaluation of over-the-counter drugs for patients with pre-existing psychiatric disorders.


Asunto(s)
Trastorno Obsesivo Compulsivo , Síndrome de Abstinencia a Sustancias , Ansiedad , Trastornos de Ansiedad/inducido químicamente , Trastornos de Ansiedad/diagnóstico , Humanos , Trastorno Obsesivo Compulsivo/diagnóstico , Trastorno Obsesivo Compulsivo/tratamiento farmacológico , Trastorno Obsesivo Compulsivo/epidemiología , Feniramina/efectos adversos
4.
Eur J Med Chem ; 222: 113574, 2021 Oct 15.
Artículo en Inglés | MEDLINE | ID: mdl-34126459

RESUMEN

Lysophosphatidic acid (LPA) activates six LPA receptors (LPAR1-6) and regulates various cellular activities such as cell proliferation, cytoprotection, and wound healing. Many studies elucidated the pathological outcomes of LPA are due to the alteration in signaling pathways, which include migration and invasion of cancer cells, fibrosis, atherosclerosis, and inflammation. Current pathophysiological research on LPA and its receptors provides a means that LPA receptors are new therapeutic targets for disorders associated with LPA. Various chemical modulators are developed and are under investigation to treat a wide range of pathological complications. This review summarizes the physiological and pathological roles of LPA signaling, development of various LPA modulators, their structural features, patents, and their clinical outcomes.


Asunto(s)
Lisofosfolípidos/farmacología , Receptores del Ácido Lisofosfatídico/agonistas , Receptores del Ácido Lisofosfatídico/antagonistas & inhibidores , Relación Dosis-Respuesta a Droga , Humanos , Lisofosfolípidos/química , Lisofosfolípidos/metabolismo , Estructura Molecular , Receptores del Ácido Lisofosfatídico/metabolismo , Transducción de Señal/efectos de los fármacos , Relación Estructura-Actividad
5.
Eur J Med Chem ; 221: 113527, 2021 Oct 05.
Artículo en Inglés | MEDLINE | ID: mdl-34020338

RESUMEN

Dengue virus belongs to the class of RNA viruses and subclass of enveloped single-stranded positive-sense RNA virus. It causes dengue fever (DF), dengue hemorrhagic fever (DHF), or dengue shock syndrome (DSS), where DHF and DSS are life-threatening. Even though dengue is an age-old disease, it is still a mystery and continues to be a global threat. Numerous attempts have been carried out in the past few decades to eradicate the virus through vaccine and antiviral drugs, but still battle continues. In this review, the possible drug targets for discovery and development of potential antiviral drugs against structural proteins of dengue virus, the current development status of the antiviral drugs against dengue around the world, and challenges that need to be addressed to overcome the shortcomings in the process of drug discovery have been discussed.


Asunto(s)
Antivirales/farmacología , Virus del Dengue/efectos de los fármacos , Dengue/tratamiento farmacológico , Desarrollo de Medicamentos , Proteínas Estructurales Virales/antagonistas & inhibidores , Antivirales/síntesis química , Antivirales/química , Dengue/metabolismo , Dengue/virología , Virus del Dengue/química , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Proteínas Estructurales Virales/metabolismo
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