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1.
Bioorg Med Chem Lett ; 43: 128083, 2021 07 01.
Artículo en Inglés | MEDLINE | ID: mdl-33964448

RESUMEN

A series of 2-amino-5-arylmethyl- or 5-heteroarylmethyl-1,3-thiazole derivatives were synthesized and evaluated for BK channel-opening activities in cell-based fluorescence assay and electrophysiological recording. The assay results indicated that the activities of the investigated compounds were influenced by the physicochemical properties of the substituent at benzene ring.


Asunto(s)
Canales de Potasio de Gran Conductancia Activados por el Calcio/metabolismo , Tiazoles/farmacología , Relación Dosis-Respuesta a Droga , Humanos , Estructura Molecular , Relación Estructura-Actividad , Tiazoles/síntesis química , Tiazoles/química
2.
BMC Biotechnol ; 19(1): 80, 2019 11 21.
Artículo en Inglés | MEDLINE | ID: mdl-31752805

RESUMEN

BACKGROUND: Cord Blood (CB) has been considered a promising source of natural killer (NK) cells for cellular immunotherapy. However, it is difficult to expand the large numbers of highly pure NK cells from CB without cell sorting and feeder cells/multiple cytokines. In this study, we try to develop a simple, safe and economical method for ex vivo expansion and purification of NK cells from CB without cell sorting and feeder cells/multiple cytokines. RESULTS: The large numbers (mean: 1.59 × 1010) of highly pure (≥90%) NK cells from CB could be obtained through interleukin-2, group A streptococcus and zoledronate stimulation of mononuclear cells using the 21-day culture approach. When compared to resting NK cells, expanded NK cells were a higher expression of activating receptors CD16, NKG2D, NKp30, NKp44, NKp46 and activating markers CD62L and CD69, while the inhibitory receptors, CD158a and CD158b remained largely unchanged. In addition, these cells showed a higher concentration of IFN-γ, TNF-α and GM-CSF secretion and cytotoxicity to K562 cells and acute myeloid leukemia targets than resting NK cells. CONCLUSION: We develop a simple, safe and economical method to obtain high yield, purity, and functionality NK cells from CB without cell sorting and feeder cells/multiple cytokines.


Asunto(s)
Sangre Fetal/citología , Inmunoterapia/métodos , Células Asesinas Naturales/citología , Citometría de Flujo , Humanos , Interleucina-2/metabolismo , Células K562 , Leucocitos Mononucleares/efectos de los fármacos , Ácido Zoledrónico/farmacología
3.
Eur J Ageing ; 16(3): 273-282, 2019 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-31543722

RESUMEN

This study was to investigate the effects of Tai Chi (TC) and whole-body vibration (WBV) exercise in sarcopenic men in advanced old age. Ninety sarcopenic men (mean age 88.6 years; age range 85-101 years) were divided into three groups: TC group, WBV group, and control (CON) group. Patients in the two treatment groups received 8 weeks of training in either TC or WBV, while the control group received reminders not to change their level of physical exercise or lifestyle. Patients in all groups also received health information related to sarcopenia. Muscle mass, muscle strength, and physical performance [balance, gait speed, timed-up-and-go test (TUGT), and five-times-sit-to-stand test (FTSST)] were analyzed and compared among the three groups. Finally, seventy-nine subjects completed the study (TC n = 24; WBV n = 28; and CON 27). Muscle strength was significantly increased in the TC and WBV groups compared to the control group (P < 0.01). Following 8 weeks of exercise, improvements were observed in all physical performance tests for the TC and WBV groups (P < 0.05). The improvement in balance was greater in the TC group than the WBV group. Time × Group effects revealed significant improvements in muscle strength in the lower extremities (P < 0.05) and physical performance (P < 0.01) in both the TC and WBV groups. Changes in muscle mass, as measured by dual-energy X-ray absorptiometry, did not significantly differ between groups. These findings indicate that TC and WBV are effective treatments for improving muscle strength and physical performance in sarcopenic men in advanced old age.

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