The chemical constituents of medicinal plants which have been used in Ayurvedic and Tibetan system of medicines in Nepal were examined. From 21 species consisting of 13 genera of the plants, 121 new compounds, whose structures are shown in Charts (1 to 13), were isolated mainly in our laboratory. Some of the compounds and their related ones showed several biological activities.
Docosahexaenoic acid (DHA) is an n-3 unsaturated fatty acid derived from fish oils. The precise mechanisms of DHA actions are still obscure. Especially, the antihypertensive effect of DHA has not yet been elucidated. Stroke-prone spontaneously hypertensive rats (SHRSP) provide the best available model for essential hypertension and stroke. The present study was undertaken to elucidate the effects of long term administration of DHA on blood pressure and stroke-related behavior in SHRSP. The blood pressure of DHA-treated SHRSP was lowered significantly as compared with that of non-treated SHRSP. DHA produced an ameliorative effect on the decreased passive avoidance response in SHRSP. DHA also improved the behavioral changes in spontaneous motor activity of SHRSP. DHA-treated SHRSP produced a significant decrease in the levels of total cholesterol, low density lipoprotein, triglycerides, lipid peroxide, serum creatinine and blood urea nitrogen as compared with those in non-treated SHRSP. These findings indicate that the DHA-induced antihypertensive action may be associated with the amelioration of both serum lipid alteration and renal dysfunction in non-treated SHRSP. Moreover, DHA-treated SHRSP maintain the normal levels of acetylcholine and choline concentrations in the hippocampus and cerebral cortex. These findings demonstrated that DHA produced an ameliorative effect on cholinergic nerve dysfunction in SHRSP. The improved cholinergic nerve function induced by DHA might have an inhibitory effect on stroke-related behavior in SHRSP. The present study suggests that long term administration of DHA may suppress the development of hypertension and stroke-related behavioral changes in SHRSP.
Recently, hypervalent Iodine (III) reagents have been used extensively in organic synthesis. In particular, phenyliodine (III) diacetate (PIDA) and phenyliodine (III) bis (trifluoroacetate)(PIFA) have received a great deal of attention due to low toxicity, ready availability, easy handling, and reactivities similar to that of heavy metal reagents or anodic oxidation. In contrast to the widely explored phenolic oxidation using PIDA or PIFA, reactions of phenol ethers with hypervalent iodine reagents have been limited and have yielded mostly iodonium salts. We found unexpectedly that the reaction of p-substituted phenol ethers with PIFA in the presence of some nucleophiles in polar and poorly nucleophilic solvents such as 2, 2, 2-trifluoroethanol and 1, 1, 1, 3, 3, 3-hexafluoro-2-propanol caused a novel and straightforward nucleophilic substitution reaction on the aromatic ring via a cation radical intermediate [ArH+·]. Successful application of PIFA-induced umpolung of electron-rich aromatic ring reactivity allowed intramolecular cyclization reactions of phenol ethers leading to novel and efficient preparations of synthetically useful products such as biaryl compounds, quinone-imines, and sulfur-containing heterocycles. Using these methods, the first total synthesis of potent cytotoxic marine alkaloid, makaluvamine F was also achieved.
This review summarizes our studies on the development of the syntheses of mesomeric betaines by thermolysis of N-allylides and N-vinylimino ylides involving back-donated 1, 6-cyclization. Furthermore interesting syntheses of heteropolycycles, indolizinoquinolizines via one step reaction are also reviewd.
The purpose of this study is to construct an educational program for patients with chronic hepatic diseases to avoid self-regulation of medication. We have statistically analyzed the influencing factors of self-regulation from the following 3 viewpoints. First, in the investigation of the number of and the kind of prescribed medicines, it was found that the number of prescribed medicines increased sharply at the stage of Liver Cirrhosis b. Secondly, in the survey of patients' awareness of medication, it was found that self-regulation was influenced by lack of understanding the effects of medicines and the necessity of medication, and by lack of understanding the clinical conditions. Especially, at the stage of Liver Cirrhosis b, self-regulation was strongly influenced by lack of understanding the clinical conditions. Lastly, in the evaluation of patients' characteristics by pharmacists, self-regulation was also strongly influenced by the level of understanding the necessity of medication, understanding the clinical conditions, a patient-doctor relationship, and anxiety about side-effects of medicines. Therefore we have constructed an educational program for patients from the viewpoint of medication. The information consists of two articles; one is the action mechanism of the medicine connected with the clinical conditions to help the patients understand the necessity of medication; the other is how to check the effect and adverse reaction of the medication by themselves to decrease the anxiety about side-effects. Consequently, the medication management and the consultation for inpatients with chronic hepatic diseases were standardized by incorporating the education with the information described above.
Orally-disintegrating tablets of clonidine hydrochloride, an α2-adrenergic agonist, were prepared by the method of drying an aqueous suspension. The suspension was prepared using powdered lactose, and the composition ratio was 2 : 1 (powdered lactose : 0.048% clonidine hydrochloride solution). The suspension was dried under 4±1°C(72±15% R.H.). We obtained tablets containing clonidine hydrochloride (40μg/tablet). Physical properties of the tablets were as follows : hardness was 4.0 kgf, and disintegration time was 41.7 s (in vitro). In the clinical use, 8 patients, aged 1-2 year and weighing 9-11 kg, received approximately 4μg/kg body weight as clonidine hydrochloride. The tablet was administered 90 min before entering the operating room. All patients were willing to accept the tablet. The quality of separation from parents, sedation and a mask acceptance were excellent on all patients. These results suggest that the orally-disintegrating tablet of clonidine hydrochloride was useful in a clinical situation for the preanesthetic medication of pediatric patients aged 1-2 year.