Two pimaranes -pimara-8(14),15-dien-19-oic acid (1: ) and -8(14),15-pimaradien-3-ol (2: ), isolated from , and six semi-synthetic derivatives methyl ester of the -pimara-8(14),15-dien-19-oic acid (3: ), -pimara-8(14),15-dien-19-ol (4: ), acetate of -pimara-8(14),15-dien-19-ol (5: ), -pimara-8(14),15-dien-19-ol succinic acid (6: ), acetate of -8(14),15-pimaradien-3-ol (7: ), -8(14),15-pimaradien-3-ol succinic acid (8: ) were evaluated for their cytotoxic activities to childhood leukemia cell lines and leishmanicidal activity against the parasite Among these compounds, 1: to 6: presented moderate cytotoxic activity, with compound 4: being the most active (GI of 2.6 µM for the HL60 line) and the derivatives 7: and 8: being inactive. Against the parasite , the most promising derivative was the acetate of -pimara-8(14),15-dien-19-ol (5: ), with EC of 20.
View Article and Find Full Text PDF(-)-Epigallocatechin-3-gallate (EGCG), the major active polyphenol extracted from green tea, has been shown to induce apoptosis and inhibit cell proliferation, cell invasion, angiogenesis and metastasis. Herein, we evaluated the in vivo effects of EGCG in acute myeloid leukaemia (AML) using an acute promyelocytic leukaemia (APL) experimental model (PML/RARα). Haematological analysis revealed that EGCG treatment reversed leucocytosis, anaemia and thrombocytopenia, and prolonged survival of PML/RARα mice.
View Article and Find Full Text PDFIncreased intra-abdominal pressure resulting from pneumoperitoneum can cause renal physiological changes, such as oliguria and anuria, in mammals. Although videolaparoscopic operations are common, the occurrence of renal lesions due to these procedures has not been precisely documented in the literature. The aim of this study was to evaluate the impact of pneumoperitoneum on renal blood flow using renal scintigraphy in a rabbit model.
View Article and Find Full Text PDFANKHD1 is highly expressed in human acute leukemia cells and potentially regulates multiple cellular functions through its ankyrin-repeat domains. In order to identify interaction partners of the ANKHD1 protein and its role in leukemia cells, we performed a yeast two-hybrid system screen and identified SIVA, a cellular protein known to be involved in proapoptotic signaling pathways. The interaction between ANKHD1 and SIVA was confirmed by co-imunoprecipitation assays.
View Article and Find Full Text PDFA novel class of benzo[d][1,3]dioxol-5-ylmethyl alkyl/aryl amide and ester analogues of capsaicin were designed, synthesized, and evaluated for their cytotoxic activity against human and murine cancer cell lines (B16F10, SK-MEL-28, NCI-H1299, NCI-H460, SK-BR-3, and MDA-MB-231) and human lung fibroblasts (MRC-5). Three compounds (5f, 6c, and 6e) selectively inhibited the growth of aggressive cancer cells in the micromolar (µM) range. Furthermore, an exploratory data analysis pointed at the topological and electronic molecular properties as responsible for the discrimination process regarding the set of investigated compounds.
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