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1.
Angew Chem Int Ed Engl ; 63(14): e202315668, 2024 Apr 02.
Artículo en Inglés | MEDLINE | ID: mdl-38346927

RESUMEN

Artificial molecular muscles are highly attractive in the field of molecular machinery due to their unique properties of contraction and stretching motion. However, the synthesis of molecular muscles poses formidable challenges as it is hindered by undesirable yields and poor selectivity. Herein, we present a procedure for the dynamic assembly of foldaxane-based [c2]daisy chains, wherein the hermaphroditic sequences consisting of aromatic helices and peptide rods are interlocked through inter-strand hydrogen-bonding interactions. The binding complementarity facilitates a selective and efficient assembly of [c2]daisy chain structures, inhibiting the creation of by-products. Introducing multiple recognition sites confers the system with contraction and stretching motion actuated by chemical stimuli. The rate of this muscle-like motion is calculated to be 0.8 s-1, which is 107 times faster than that of complex dissociation.

2.
J Pharm Biomed Anal ; 242: 116001, 2024 May 15.
Artículo en Inglés | MEDLINE | ID: mdl-38354536

RESUMEN

Saikosaponin D (SsD), a natural triterpenoid saponin compound, exhibits notable potential in suppressing tumor growth and inhibiting metastasis, particularly in breast cancer. However, its underlying mechanism of action for SsD remains unclear. In this study, a combination strategy to reveal the metabolism modulation of SsD on breast cancer was performed by integration of histopathological assessments and untargeted metabolomics analysis. Pathological evaluation of the efficacy of SsD from a visual and intuitive perspective. Accordingly, a non-targeted metabolomics study was used to investigate the pharmacological efficacy using a set of serum samples from mice before and after (0-30 days) modulated with SsD based on ultra-high performance liquid chromatography tandem orbitrap mass spectrometry to discover metabolite biomarkers for finding the key metabolic mechanism in a molecular perspective. As a result, 20 metabolites were selected as potential biomarkers for SsD efficacy evaluation with high sensitivity and specificity. These metabolites changes were involved in sphingolipid metabolism, glycerophospholipid metabolism, phenylalanine and tryptophan metabolism, and phenylalanine, tyrosine and tryptophan biosynthesis pathways, suggesting that SsD exerted anti-breast cancer effects through the regulation of the underlying metabolism. In conclusion, we developed a new analysis strategy that effectively discovers tumor-progressing related metabolite biomarkers in serum for pharmacological efficacy evaluation.


Asunto(s)
Antineoplásicos , Neoplasias , Ácido Oleanólico/análogos & derivados , Saponinas , Ratones , Animales , Triptófano , Metabolómica/métodos , Saponinas/farmacología , Biomarcadores , Cromatografía Líquida de Alta Presión/métodos , Fenilalanina
3.
Zhongguo Zhong Xi Yi Jie He Za Zhi ; 25(12): 1109-11, 2005 Dec.
Artículo en Chino | MEDLINE | ID: mdl-16398433

RESUMEN

OBJECTIVE: To study the pharmacodynamics of qiangyi jiangtang capsules (QJC) to offer the scientific foundation for clinical treatment to model rats of diabetes millitus induced by high lipid forage and streptozotocin. METHODS: The model rats of diabetes mellitus were induced by intraperitoneal injection of 0.6% streptozotocin (30 mg/kg body weight) given to Wistar rats after feeding with high lipid forage for a month and followed by fasting for 18 hours. Rats with level of blood glucose over 10.0 mmol/L 5 days after modelling was regarded as the successful model. Besides, a group of blank control was set up with rats fed with general forage and injected with equal volume of citric acid buffer solution. The successfully modelled rats were randomly divided into the model group, the positive control group and the high (2.0 g/kg), middle (1.2 g/kg) and low (0.4 g/kg) dose QJC treated groups. Meanwhile, the same volume of normal saline was given to rats in the blank control group and the model group, while Matfarmin (0.5 g/kg) was given to the rats in the positive control group. The levels of blood glucose (BG), serum fructose amine (SFA), hemoglobin A1c (HbA1c) were measured after one month of medication, and the amount of water drinking and food intake were measured at the second and the fourth week of the treatment. RESULTS: The levels of BG, SFA, HbA1c, the amount of water drinking and food intake in the 3 QJC treated groups were obviously lower than those in the model group (P < 0.05 or P < 0.01). CONCLUSION: QJC could remarkably lower the levels of BG, HbA1c, SFA and the amount of food intake and water-drinking of DM model rats, it is a Chinese herbal preparation worthy of further development and research.


Asunto(s)
Diabetes Mellitus Experimental/tratamiento farmacológico , Medicamentos Herbarios Chinos/uso terapéutico , Hipoglucemiantes/uso terapéutico , Fitoterapia , Animales , Cápsulas , Femenino , Masculino , Ratas , Ratas Wistar
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