RESUMO
A series of alpha-asarone isomers was synthesized and investigated for their hypolipidemic and antiplatelet activity. Considering the hypolipidemic activity in rats at a dose of 80 mg/kg/day, some isomers were more potent than clofibrate at 150 mg/kg. Compound 3 was one of the most active agents elevating the HDL cholesterol level by 56% and lowering the LDL cholesterol level by 46.8% in rats after 7 days of administration. The activities of the platelet aggregation test in vitro were significant but lower than those of the reference substances (indomethacine and acetylsalicylic acid). In the pulmonary thromboembolic in vivo test in mice, two compounds (alpha-asarone (6) and compound 4) produced significant antithrombotic effects at 100 mg/kg, namely 44% and 52% protection against lung microembolia, respectively. alpha-Asarone derivatives form a new group of potential hypolipidemic and/or antithrombotic agents. The compounds 3, 4, and 6 may serve as lead substances whose structural modifications may result in original drugs.
Assuntos
Anisóis/síntese química , Fibrinolíticos/síntese química , Hipolipemiantes/síntese química , Derivados de Alilbenzenos , Animais , Anisóis/química , Anisóis/farmacologia , Fibrinolíticos/química , Fibrinolíticos/farmacologia , Humanos , Hipolipemiantes/química , Hipolipemiantes/farmacologia , Técnicas In Vitro , Pulmão/irrigação sanguínea , Masculino , Camundongos , Agregação Plaquetária/efeitos dos fármacos , Ratos , Ratos Wistar , Estereoisomerismo , Relação Estrutura-Atividade , Tromboembolia/prevenção & controleRESUMO
A silver-halide infrared optical fiber is used in a double-beam spectrometer, demonstrating the ability to guide small infrared signals efficiently. We show that a fractional transmission change of less than 1% is easily measured. Use of the fiber may obviate the necessity for the unfriendly optics currently used in spectrometry systems to probe remote sample zones. As a specific example, we were able to guide with high efficiency an infrared signal to and from a sample that was mounted in a cryostat. Using this setup, we measured the photoinduced absorption due to the e1 ? e2 intersubband transition in a GaAs-GaAlAs multiple quantum-well structure.
RESUMO
Four new dipeptides containing epsilon-aminocaproic acid were synthesized. Antibrinolytic, antiacaseinolytic activity and influence on activation of plasminogen by streptokinase were tested.
Assuntos
Aminocaproatos/síntese química , Aminocaproatos/farmacologia , Dipeptídeos/síntese química , Fibrinólise/efeitos dos fármacos , Dipeptídeos/farmacologiaRESUMO
Three new dipeptides of E-aminocaproic acid were synthesized and their antifibrinolytic activity was examined. H-EACA-L-Trp-OH possess stronger antifibrinolytic activity than H-EACA-L-Tyr-OH and H-EACA-L-Leu-OH. Antifibrinolytic activity of H-EACA-L-Gly-OH was smallest.
Assuntos
Aminocaproatos/química , Antifibrinolíticos/síntese química , Dipeptídeos/biossínteseRESUMO
Sixty hospitalized elderly cardiac patients were tested using the Geriatric Functional Rating Scale (GFRS) and were followed four months postdischarge. Significant relationships were found between GFRS scores and readmission status. These data substantiate the potential usefulness of GFRS as a predictive instrument to identify those high-risk hospitalized elderly cardiac patients who need social-health services in the posthospital recovery period.