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1.
Bioorg Med Chem Lett ; 107: 129795, 2024 Jul 15.
Artículo en Inglés | MEDLINE | ID: mdl-38750906

RESUMEN

Chalcones are chemical scaffolds found in natural products, particularly in plants, and are considered for structural diversity in medicinal chemistry for drug development. Herein, we designed and synthesised novel acetamide derivatives of chalcone, characterizing them using 1H NMR, 13C NMR, HRMS, and IR spectroscopic methods. These derivatives were then screened against human cancer cells for cytotoxicity using the SRB assay. Among the tested derivatives, 7g, with a pyrrolidine group, exhibited better cell growth inhibition activity against triple-negative breast cancer (TNBC) cells. Further assays, including SRB, colony formation, and fluorescent dye-based microscopic analysis, confirmed that 7g significantly inhibited MDA-MB-231 cell proliferation. Furthermore, 7g promoted apoptosis by upregulating cellular reactive oxygen species (ROS) levels and disrupting mitochondrial membrane potential (MMP). Elevated expression of pro-apoptotic proteins (Bax and caspase-3) and a higher Bax/Bcl-2 ratio with downregulation of anti-apoptotic (Bcl-2) protein levels were observed in TNBC cells. The above results suggest that 7g can promote cellular death through apoptotic mechanisms in TNBC cells.


Asunto(s)
Acetamidas , Antineoplásicos , Apoptosis , Proliferación Celular , Diseño de Fármacos , Ensayos de Selección de Medicamentos Antitumorales , Neoplasias de la Mama Triple Negativas , Humanos , Neoplasias de la Mama Triple Negativas/tratamiento farmacológico , Neoplasias de la Mama Triple Negativas/patología , Neoplasias de la Mama Triple Negativas/metabolismo , Antineoplásicos/farmacología , Antineoplásicos/síntesis química , Antineoplásicos/química , Relación Estructura-Actividad , Proliferación Celular/efectos de los fármacos , Acetamidas/farmacología , Acetamidas/síntesis química , Acetamidas/química , Apoptosis/efectos de los fármacos , Estructura Molecular , Línea Celular Tumoral , Chalconas/farmacología , Chalconas/química , Chalconas/síntesis química , Relación Dosis-Respuesta a Droga , Chalcona/farmacología , Chalcona/química , Chalcona/síntesis química , Especies Reactivas de Oxígeno/metabolismo , Potencial de la Membrana Mitocondrial/efectos de los fármacos
2.
Org Biomol Chem ; 21(39): 7928-7934, 2023 Oct 11.
Artículo en Inglés | MEDLINE | ID: mdl-37766675

RESUMEN

A stereo- and regio-selective addition of arenes to alkynes via C-H bond functionalization has been developed using palladium nanoparticles supported on graphite oxide (Pd@GO) as the reusable catalyst. The prepared catalyst was characterized by various spectroscopic techniques such as FT-IR, TEM, SEM, EDX, P-XRD, and XPS analysis. The thermal stability of the catalyst was established by TGA. The C-H functionalized products were obtained in good to excellent yields (69-92%) at room temperature. The methodology further extended to the synthesis of biologically and pharmaceutically important coumarin molecules from phenols and alkynes. Good to excellent yields of the coumarins (74-92%) were obtained. After the reaction, the catalyst was separated by centrifugation followed by filtration. The recovered catalyst was washed and reused up to five cycles. The advantages of this method are the simple procedure of the catalyst preparation, high catalytic efficiency, high selectivity, good functional group tolerance, low catalyst loading, and gram-scale synthesis.

3.
Heliyon ; 10(11): e32333, 2024 Jun 15.
Artículo en Inglés | MEDLINE | ID: mdl-38947433

RESUMEN

In recent decades, biosynthesis of metal and (or) metal oxide nanoparticles using microbes is accepted as one of the most sustainable, cost-effective, robust, and green processes as it does not encompass the usage of largely hazardous chemicals. Accordingly, numerous simple, inexpensive, and environmentally friendly approaches for the biosynthesis of silver nanoparticles (AgNPs) were reported using microbes avoiding conventional (chemical) methods. This comprehensive review detailed an advance made in recent years in the microbes-mediated biosynthesis of AgNPs and evaluation of their antimicrobial activities covering the literature from 2015-till date. It also aimed at elaborating the possible effect of the different phytochemicals, their concentrations, extraction temperature, extraction solvent, pH, reaction time, reaction temperature, and concentration of precursor on the shape, size, and stability of the synthesized AgNPs. In addition, while trying to understand the antimicrobial activities against targeted pathogenic microbes the probable mechanism of the interaction of produced AgNPs with the cell wall of targeted microbes that led to the cell's reputed and death have also been detailed. Lastly, this review detailed the shape and size-dependent antimicrobial activities of the microbes-mediated AgNPs and their enhanced antimicrobial activities by synergetic interaction with known commercially available antibiotic drugs.

4.
Naunyn Schmiedebergs Arch Pharmacol ; 396(4): 633-647, 2023 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-36585999

RESUMEN

The rhizomes of ginger have been in use in many forms of traditional and alternative medicines. Besides being employed as condiment and flavoring agent, it is used in the treatment of nausea, osteoarthritis, muscle pain, menstrual pain, chronic indigestion, Alzheimer's disease, and cancer. Ginger rhizome contains volatile oils, phenolic compounds and resins, and characterization studies showed that [6]-gingerol, [6]-shogaol, and [6]-paradol are reported to be the pharmacologically active components. Gingerol is a major chemical constituent found as volatile oil in the rhizomes of ginger. It has several medicinal benefits and used for the treatment of rheumatoid arthritis, nausea, cancer, and diabetes. Many studies have been carried out in various parts of the world to isolate and standardize gingerol for their use as a complementary medicine. The present review summarizes wide range of research studies on gingerol and its pharmacological roles in various metabolic diseases.


Asunto(s)
Catecoles , Zingiber officinale , Catecoles/farmacología , Catecoles/uso terapéutico , Alcoholes Grasos/farmacología , Alcoholes Grasos/uso terapéutico , Alcoholes Grasos/química , Extractos Vegetales/química , Zingiber officinale/química , Zingiber officinale/metabolismo
5.
J Toxicol ; 2014: 690758, 2014.
Artículo en Inglés | MEDLINE | ID: mdl-25525430

RESUMEN

Cymbopogon citratus (DC.) Stapf commonly known as lemon grass is used extensively as green tea and even as herbal tea ingredient across the world. Plants have the ability to uptake metals as nutrient from the soil and its environment which are so essential for their physiological and biochemical growth. Concentrations of these twelve trace elements, namely, Mg, Ca, Cr, Mn, Fe, Ni, Cu, Zn, Mo, As, Cd, and Pb, are analysed by graphite furnace-atomic absorption spectroscopy (GF-AAS) and are compared with the permissible limits of FAO/WHO, ICMR, and NIH, USA, which are found to be within permissible limits. Toxic metals like As, Cd, and Pb, analysed are within the tolerable daily diet limit and at low concentration.

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