A novel series of 2-O-alkylascorbic acids (5a-u) was synthesized, and their scavenging activities against active oxygen species as well as their suppressive effects on the arrhythmias in rat heart ischemia-reperfusion models were evaluated. Some 2-O-alkylascorbic acids (5e-1) exhibited potent inhibiting activities against lipid peroxidation in rat brain homogenates and in alleviating effects in the ischemia-reperfusion models. Studies on the structure-activity relationship demonstrated that a free 3-enolic hydroxyl group and the longer alkyl chains substituted on the 2-hydroxyl group of ascorbic acid were beneficial for the biological and pharmacological activities. 2-O-Octadecylascorbic acid (5k, CV-3611), one of the most potent and promising compounds, markedly inhibited lipid peroxidation (IC50 = 4.3 X 10(-6) M) and alleviated myocardial lesions induced by ischemia-reperfusion at an oral dose of 1 mg/kg in rats.

SynopsisPlasma polymerizations in five silicon compounds having chemical formula of (CH3),Si-X--Si(CH,),, X = none, CH2, NH, 0, and S atoms, were investigated by elemental analysis, infrared spectroscopy, and ESCA. The chemical composition of polymers plasma-polymerized was influenced by the X groups in (CH,),Si--X--Si(CH,),.Polymers, when X was S atoms, possessed no sulfur; and X was CH2 groups polymers rich in carbon and hydrogen atoms were formed. Details in chemical composition were discussed by IR and ESCA. Such differences in chemical composition reflected on gas permeability of the plasma films.

The sino-atrial node area was perfused selectively through the right atrial artery in 76 dogs. The relationship between changes in the blood pressure in this artery and sinus node rhythmicity was studied in 56 hearts in which the major blood supply to the sinus node artery came from the right atrial artery. A reciprocal relation was observed between changes of blood pressure in the sinus node artery and the sinus rate. Some characteristics were: (1) The negative chronotropic effect induced by raising the blood pressure was linearly related to the Degrees of pressure change and more prominent than the positive chronotropic effect induced by reducing the pressure. (2) This relationship was most prominent in a limited range between 20 and 100 mm Hg. (3) Dichloroisoproterenol, atropine, hexamethonium, reserpine and vagotomy did not modify these responses. It is concluded that this localized mechanosensitivity of the sinus node to changes in arterial pressure may be responsible for the regulation of the heart rate in the lower range of blood pressure and that complete regulation of the heart rate is achieved physiologically in combination with the reflexes through the carotid and aortic nerves.

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