RESUMEN
In this study, four in situ hydro(solvo)thermal metal-ligand reactions, including oxidation (H2L1), C-C coupling (H4L2), nitration (H2L3), and condensation (HL4-6), based on bis[3-(pyridin-2-yl)-1H-1,2,4-triazol-5-yl]methane (H2L0), in the presence of DyIII ions, were carried out. The in situ metal-ligand reaction gave six new ligands existing in eight novel DyIII coordination complexes, which were characterized by crystal structure, mass spectrometry, and magnetism.
RESUMEN
We present the synthesis, structural characterization, and magnetic properties of two high-nuclearity cobalt clusters formulated as [Co13(µ3-OH)3(µ3-Cl)(dpbt)5(ptd)Cl10][Co(H2O)2Cl2]·(CH3)2CHOH (1) and [Co24(µ3-OH)6(µ3-Cl)2(dpbt)10(ptd)2Cl16]·2CH3CH2OH (2), respectively (H2dpbt = 5,5'-bis(pyridin-2-yl)-3,3'-bis(1,2,4-triazole) and H2ptd = 3-(pyridin-2-yl)-1,2,4-triazine-5,6-diol). Compound 1 is composed of an inner [Co4(µ3-OH)3(µ3-Cl)] cubane and an outer [Co9(dpbt)5(ptd)Cl10] defective adamantane. Compound 2 reveals a giant {Co24} cluster possessing a dual-[Co12] skeleton from 1. The hierarchical assembly from 1 to 2 has been established and tracked through high-resolution electrospray ionization (HRESI-MS) analyses from the solvothermal reaction mother solution. Magnetic studies of 1 and 2 revealed the highly correlated spins, a glasslike magnetic phase transition at ca. 8 K, and slow relaxation behavior of SMM nature in the lower-temperature region (below 4 K).
RESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: The plant Bauhinia brachycarpa Benth (BBB) has been traditionally used for treating muscle aches such as bone pain, and neuralgia for a long time, on account of its sedative and antinociceptive activities in Yunnan province of China. However, there was no experimental evidence to confirm its traditional medicinal use. AIM OF THE STUDY: The antinociceptive effect and possible mechanism of ethanolic extract of BBB on neuropathic pain was evaluated through a model of partial sciatic nerve ligation in mice. MATERIALS AND METHODS: A commonly employed animal model induced by partial sciatic nerve ligation (PSNL) in mice was established in the aim of studying neuropathic pain. Ethanolic extract of BBB (1000, 500, 250 mg/kg) and pregabalin (60 mg/kg) were intragastric administrated daily for 7 days post-PSNL. Mechanical and thermal hyperalgesia were assessed throughout the experimental period. After the experiment, the levels of tumor necrosis factor-α (TNF-α) and interleukin-10 (IL-10) in serum were determined by ELISA. The mRNA expressions of ionized calcium binding adaptor molecule 1 (Iba-1), CD16, CD206, arginine-1 (Arg-1), interleukin-1ß (IL-1ß), and inducible nitric oxide synthase (iNOS) in the spinal cord were detected by qPCR. The protein levels of Iba-1, CD16, CD206, and p38 phosphorylation in the spinal cord were detected by immunohistochemistry and western blotting. The phytochemical analysis of BBB was performed through the colorimetric test. RESULTS: Neuropathic pain induced by PSNL was significantly alleviated by BBB treatment, which decreased pro-inflammatory cytokines such as TNF-α, IL-1ß and iNOS, increased anti-inflammatory cytokine such as IL-10 and Arg-1, and attenuated p38 phosphorylation. BBB also reduced the number of Iba-1 and CD16 positive cells, but it enhanced the number of CD206 positive cells. n-Butanol portion that was partitioned from the ethanolic extract had the highest content of total flavonoids among all the portions, and the antinociceptive effect of n-butanol portion is better than that of other portions. CONCLUSIONS: Our findings indicate that the antinociceptive effect of BBB is mediated by inhibiting the inflammatory response and regulating the differentiation of microglia. The antinociceptive effect of BBB was related to the content of total flavonoids.
Asunto(s)
Bauhinia , Neuralgia , 1-Butanol , Analgésicos/farmacología , Analgésicos/uso terapéutico , Animales , China , Citocinas/metabolismo , Flavonoides/uso terapéutico , Hiperalgesia/tratamiento farmacológico , Interleucina-10 , Ratones , Neuralgia/tratamiento farmacológico , Neuralgia/metabolismo , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Nervio Ciático/metabolismo , Factor de Necrosis Tumoral alfa/metabolismoRESUMEN
In the title compound, C(6)H(6)Cl(2)N(2)O(2)S, the O atoms of the sulfonamide group lie on one side of the benzene ring and the amino group lies on the opposite side. An inter-molecular N-Hâ¯Cl inter-action occurs. In the crystal, adjacent mol-ecules are linked by N-Hâ¯O hydrogen bonds, forming a three-dimensional structure with supporting π-π stacking inter-actions [centroid-centroid distance = 3.7903â (12)â Å]. A short Clâ¯Cl contact [3.3177â (10)â Å] also occurs.
RESUMEN
Three novel single crystals of the metal-based complexes Cu-1, Cu-2, and Co-1 were obtained and characterized. Compared with Cu-2 and Co-1, Cu-1 showed remarkable activities of anti-cervical cancer, anti-cisplatin-resistant non-small cell lung cancer and anti-angiogenesis by downregulating the expressions of important proteins in the VEGF/VEGFR2 signaling pathway to inhibit angiogenesis and cancer cell proliferation, induce apoptosis, and suppress migration and metastasis. Moreover, Cu-1 dramatically inhibited the expression of the anti-apoptotic protein Bcl-2 and up-regulated the expressions of the proapoptotic proteins caspase-9 and Bax to induce the apoptosis of tumor cells, simultaneously decreasing the density of endothelial cells to inhibit tumor angiogenesis in cisplatin-resistant tumors.
Asunto(s)
Antineoplásicos/uso terapéutico , Caspasa 9/metabolismo , Factor A de Crecimiento Endotelial Vascular/metabolismo , Receptor 2 de Factores de Crecimiento Endotelial Vascular/metabolismo , Proteína X Asociada a bcl-2/metabolismo , Células A549/efectos de los fármacos , Animales , Apoptosis , Western Blotting , Línea Celular Tumoral , Movimiento Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Embrión de Pollo , Cristalografía por Rayos X , Femenino , Células HeLa , Células Endoteliales de la Vena Umbilical Humana , Humanos , Inmunohistoquímica , Ratones Desnudos , Neovascularización Fisiológica/efectos de los fármacos , Ensayos Antitumor por Modelo de Xenoinjerto , Proteína X Asociada a bcl-2/genéticaRESUMEN
The toxic effects of artesunate and dihydroartemisinin on the growth metabolism of Tetrahymena thermophila BF5 were studied by microcalorimetry. The results showed that: (1) low concentrations of artesunate (Asunto(s)
Artemisininas/farmacología
, Tetrahymena thermophila/efectos de los fármacos
, Animales
, Artesunato
, Calorimetría
, Tetrahymena thermophila/crecimiento & desarrollo