In the research of penems, a versatile intermediate 2-thioxopenam was synthesized, from which many penem derivatives were obtained. The structure-activity relationship analysis of the synthesized penens showed that cyclic amine side chain was most effective one as a substituent of 2-thiopenems. Several carbapenems with the same side chain as penems at 2-position were synthesized, one of the compounds was RS-533. Some effective methods for carbapenem synthesis were also discussed.
To study the utilization of soft X-ray microradiogram for the evaluation of crude drugs, seven different grades of Cinnamomi veri Cortex were examined. As the result, through the surface image, broad-linear bands due to calcium oxalate crystals in the phloem rays were observed definitely in the lower grade ones, and scarcely in the higher grade. Moreover, comparing with the microradiogram of the stem bark of Cinnamomum verum, higher grade ones corresponded to the bark from slender parts and lower grades to thicker parts. By use of this method jointly with optical microscopic observation was found to be more useful for the histological study of crude drugs. In addition, this method might be superior to the observation of the internal structures of large sized crude drugs without any damages, and gives various interesting informations by treating the drugs beforehand with chemical reagents such as hydrochloric acid.
It was found that the subcutaneous treatment with 0.6 mg/kg of methotrexate (MTX) twice a week for 7 weeks in rat led to the increases in blood viscosity-adjusted hematocrit and serum lipidperoxide level and a decrease in the expansibility of erythrocyte during the course of hypotonic hemolysis. The effect of sho-saiko-to, one of the useful kampo prescriptions used in traditional Chinese system of medicine, on biological responses in MTX-treated rats was examined mainly from the biorheological view points. The combined use of sho-saiko-to and MTX inhibited the blood flow properties affected by MTX treatment. It was also found that the administration of sho-saiko-to inhibited the decrease of body weight and the increase of liver lipidperoxide induced by MTX treatment. The MTX-induced increase of liver lipidperoxide level was also restored by the administration of mecobalamin which showed no effect on the blood viscosity and body weight affected by MTX treatment.
The essential oils of seven species of Japanese wild-ginger belonging to Heterotropa genus of Aristolochiaceae were investigated. H. stellata contains borneol, elemicin and safrole as main components. H. aspera contains borneol as the sole major constituent together with various kinds of minor components. Though the botanical character of H. geaster is much similar to that of H. aspera, the former contains trans-asarone and elemicin and these two species are different each other. H. nankaiensis and H. yoshikawae are much similar to H. nipponica on the patterns of their chemical constituents and also on the outernal appearances of their plants. H. trigyna affords an oil containing only safrole as well as two other species of the same group. H. dilatata contains methyleugenol as a main component.
The essential oils of six species of wild-ginger collected in Ryukyu Islands and Taiwan were investigated. Heterotropa yakusimensis contains mainly trans-asarone as the constituent of its essential oil. H. gusk possesses many of minor constituents together with a major component, β-pinene. H. hatsushimae also contains a number of minor sesquiterpenoids along with a large quantity of trans-asarone. H. dissita includes trans-asarone, elemicin and euasarone as major components. H. gelasia contains safrole and elemicin as major components along with many of minor sesquiterpenoids. Geotaenium epigynum collected in Taiwan contains many sesquiterpenoids as minor constituents together with a small amount of elemicin.
The essential oils of about fifty species of wild-gingers in Japan and in neighboring countries have been investigated, and the essential oils are divided into three types as shown in Table I. Namely, the first type is a primitive type characterized by containing many kinds of minor mono- or sesquiterpenoids ; the second one is an intermediate type containing several phenylpropanoids as major components ; the third one is an advanced type characterized by containing propanoids as a major component together with trace amounts of other constituents. A character of each essential oil is related to the taxonomical position of each original plant among groups to which they belong. Therefore, the data of each essential oil afford some significant informations in order to deduce the mutual phylogenical relationship. However, the systematic tree of wild-gingers (Asarum, wide sensed) has not been figured out such ambiguous problems as the existence of many ancestral kinds growing in China, Taiwan and Ryukyu.
Poly (vinyl alcohol) (PVA) gels, which may be used for the base of drug release, were prepared by a given cycle of freezing and thawing. Polymerization degree and concentration of PVA, a given cycle and temperature of freezing and thawing were discussed to obtain enough physical strength of the gel. The physical strength of the gel was evaluated in terms of penetration degree of penetrometer. Furthermore, the gel was cross-linked by glutaraldehyde for the control of the drug release. Polymerization degree and concentration of PVA to obtain enough strength of the gel were over 1000 and 6%, respectively. The physical strength of the gel was increased with increasing the cycle times, then becoming horizontal after fourth time of cycle. The optimum temperature of freezing and thawing were -30 and 20°C, respectively. The drug release of indomethacin from the gel was in agreement with a matrix model. Zero order drug release from the gel was established by cross-linking with glutaraldehyde.
A particulate matter content in prepared ultraclean water was determined. The particle size distributions in ultraclean water was described by a straight-line equation as well as parenteral solutions. A multi-point standard of ultraclean water and ultraclean solvent was proposed. New cleanliness factors, based on the particle-size distribution of this standard, for assessing the particulate matter content in a large-volume parenteral solution were developed and tested. Cleanliness factors were compared with another parameter and there were rank-order correlation among these parameter for cleanliness of parenteral solution, especially highly between the cleanliness factor and commulative number of particles at a diameter of 2.0 μm. Cleanliness control of parenteral solution by using these cleanliness factors is proposed as a worth-while quality control.
Three new secoiridoid glycosides, named isoligustroside, isooleuropein and neooleuropein, were isolated from the leaves of Syringa vulgaris LINN., and the structures were elucidated on the basis of carbon-13 nuclear magnetic resonance spectra and other physicochemical evidence.