RESUMO
Four new sesquiterpenoids, conyterpenols A - D (1-4), along with nineteen known analogues (5-23) were isolated from the aerial parts of Conyza japonica. The structures of 1-4 were determined through spectroscopic analysis, while their absolute configurations were determined by comparison of calculated and experimental electronic circular dichroism (ECD) spectra. Conyterpenol D (4) was a new type of sesquiterpenoid with a seven-membered lactone ring. Compounds 1-23 were evaluated for their inhibitory activity against LPS-induced nitric oxide production in RAW264.7 macrophages and cytotoxicity against human hepatoma cell line (HepG2) and human breast adenocarcinoma cell line (MCF-7). Compounds 3, 4, and 12 displayed moderate inhibition against NO production with IC50 values in the range of 26.4-33.6 µM. And all compounds showed no obvious cytotoxicity against these two cancer cell lines at 100 µM.
Assuntos
Conyza/química , Óxido Nítrico/metabolismo , Componentes Aéreos da Planta/química , Sesquiterpenos/química , Sesquiterpenos/farmacologia , Animais , Inflamação/induzido quimicamente , Inflamação/tratamento farmacológico , Lipopolissacarídeos/toxicidade , Camundongos , Modelos Moleculares , Estrutura Molecular , Células RAW 264.7RESUMO
OBJECTIVE: To investigate the effects of Tanshinone IIA (Tan IIA) on procoagulant activity (PCA) of human ECV304 cells induced by acute promyelocytic leukemia cell line NB4 cells. METHODS: ECV304 monolayers were respectively incubated for different hours at 37 degrees C in the conditioned media (CM) of NB4 cells treated with 0.5 microg/mL Tan IIA(Tan IIA-NB4-CM), 0.3 microg/mL all-trans retinoidic acid (ATRA)(ATRA-NB4-CM), DMSO(DMSO-NB4-CM) or the RPMI1640 medium. ECV304 lysates were tested for PCA using the one-stage clotting assay as well as for tissue factor activity (TF: Act) using the chromogenic substrate assay; ECV304 cell monolayers were incubated for different hours at 37 degrees C in a medium system including 0.5 microg/mL Tan IIA and Tan IIA-NB4-CM, and the ECV304 cell lysates were tested for PCA in the same way as above. Also they were controlled by 0.3 microg/mL ATRA, DMSO or RPMI1640 medium. RESULTS: (1) The conditioned mediums from 0. 5 microg/mL Tan IIA that treated NB4 cells for 24, 72 and 120 hours respectively could elevate PCA of ECV cells, and this capability developed with the time of reaction. ATRA did the same as Tan IIA (P > 0.05). (2) 0.5 microg/mL Tan IIA down-regulated the PCA of ECV304 cells induced by Tan IIA-NB4-CM, and the inhibitory effects increased with time, reaching the highest at 120 hours. (3) Tan IIA120 h-NB4-CM up-regulated TF:Act of ECV304 cells, and the effect increased with time. (4) 0. 5 microg/mL Tan IIA down-regulated PCA and TF: Act of ECV304 cells induced by Tan IIA-NB4-CM, and the inhibitory effect increased with time; simultaneously, the test was controlled with 0.3 microg/mL ATRA, the effects on PCA and TF: Act were not significantly different (P > 0.05). CONCLUSION: Tan IIA-NB4-CM can increase the levels of PCA and TF: Act of ECV304 cells through some unidentified factor; however, Tan IIA can obviously decrease the PCA and TF: Act levels of ECV304 cells induced by Tan IIA-NB4-CM.
Assuntos
Meios de Cultivo Condicionados/farmacologia , Células Endoteliais/efeitos dos fármacos , Fenantrenos/farmacologia , Tromboplastina/metabolismo , Abietanos , Anticoagulantes/farmacologia , Diferenciação Celular/efeitos dos fármacos , Linhagem Celular , Linhagem Celular Tumoral , Medicamentos de Ervas Chinesas/farmacologia , Células Endoteliais/citologia , Células Endoteliais/metabolismo , Humanos , Leucemia Promielocítica Aguda/metabolismo , Leucemia Promielocítica Aguda/patologia , Tretinoína/farmacologia , Veias Umbilicais/citologiaRESUMO
OBJECTIVE: To investigate the possible risk factors of congenital malformations in cities of Guangxi. METHODS: A case-control study was carried out on 281 cases of congenital malformations and 730 controls. Analysis of simple factor and multiple factors unconditional logistic regression were done. RESULTS: The analysis of simple factor and multiple factors showed that main risk factors of congenital malformations as multiple pregnancies (OR = 2.6), pregnancy complications (OR = 3.2), exposure to chemical substances before or during pregnancy (OR = 3.0), taking sedatives (OR = 10.2), hormone drug (OR = 9.4) or Chinese herbal medicines (OR = 2.5) during the early stage of pregnancy, mothers' blood type as AB (OR = 3.5) or A (OR = 2.2), mothers' emotion being nervous and melancholy (OR = 2.6), mothers' occupation being workers (OR = 3.8) or peasants (OR = 3.0), fathers' exposure to noise (OR = 5.7) or suffering from chronic diseases (OR = 2.8). CONCLUSIONS: Some risk factors were identified as having important effect on perinatal congenital malformations, including taking sedatives, hormone drug or Chinese herbal medicines during the early stage of pregnancy, mothers' emotion being nervous and melancholy, multiple pregnancies, pregnancy complications, exposure to chemical substances before or during pregnancies, mothers' blood type as AB or A, mothers' occupation being workers or peasants, fathers' exposure to noise or suffering from chronic diseases.