For the immunoassay of ginseng sapogenins, the ligands with which panaxadiol and panaxatriol could be determined together and separately were synthesized. For the total assay of panaxadiol and panaxatriol, panaxatriol-6-hemisuccinate was synthesized. For the separate assay, panaxadiol-3-hemisuccinate and panaxatriol-3-hemisuccinate were also synthesized.

The investigation aimed to study the effects of methanol fraction of licorice (FM 100) and glycyrrhizin on prostaglandin synthetase activity, in relation to their analgesic effects. Effects of FM 100 and glycyrrhizin on the activity of prostaglandin synthetase extracted from bull seminal vesicles were examined by the modified method of Takeguchi et al. The analgesic effect of FM 100 was tested in mice by the acetic acid writhing method. FM 100 was administered orally to mice. BSV prostaglandin synthetase activity was inhibited significantly by FM 100 in a dose-dependent manner, whereas the activity was slightly inhibited by glycyrrhizin. Statistically significant analgesic effects were also observed with FM 100. The results suggest that analgesic effect of licorice may be due to the inhibition of prostaglandin synthesis.

In order to investigate the pharmacological activities of the combined preparation of crude drugs, Chunghyulgangki-Tang was studied. Chunghyulgangki-Tang has been widely used to cerebral apoploxy, hypertension and arteriosclerosis, etc. In this study, water extract of Chunghyulgangki-Tang was conducted in attempt to investigate for analgesic, sedative, antipyretic, isolated ileum and heart, blood vessels and blood pressure action in mice, frogs, rats, guinea-pigs and rabbits. The following results were obtained; Analgesic action by the acetic acid stimulating method in mice was recognized. Sedative activities by the wheel cage method and rotor rod method in mice were shown. Prolonged action against the hypnotic duration induced by thiopental-Na was significantly noted in mice. The effect of antipyretic in endotoxin febrile rats was significantly recognized. Spontaneous motility of the isolated ilem of mice was suppressed and contractions of the isolated ileum of mice and guinea-pigs induced by acetylcholine chloride, barium chloride and histamine were remarkably inhibited. Acceleration of isolated heart motility was shown in frogs. Vaso-dilating and hypotensive actions were recognized in rabbits. According to the above results, effects based on the oriental medicinal references were approximate to the actural experimental results.

The determination of berberine in Berberis koreana was examined by the high performance liquid chromatography using ${\mu}-Bondapak$ $C_{18}$ column and $CH_3CN/phosphate$ buffer (pH 5.2) (60/40) as a mobile phase. The seasonal variations of berberine contents in Berberis koreana were as follows; 1) In roots, the average berberine content was 0.94% with the highest level of 1.32% in October. 2) In stems, their average berberine content was about 0.1% and in March, April, October and November, the contents were relatively high. 3) In leaves, however, the content was as low as 0.005%. According to the experimental results obtained, we found that Berberis koreana roots can serve as the useful natural plant resources for the berberine and October is the optimal season for the collection.

Antimicrobial activities of aucubin, an iridoid glycoside, were investigated. Gram-positive bacterium, S. aureus appeared to be more sensitive to aucubin's aglucone, aucubigenin than Gram-negative, E. coli did. Antimicrobial activities produced by aucubigenin may result in part from the inhibition of RNA and protein biosyntheses in bacterial cells. The conversion of aucubin iridoid glycoside into aucubigenin, an aglucone, appears to be a prerequisite step to exhibit the antimicrobial activities.

Based on a tracer study, starch phosphorylase was implicated as an agent in the starch synthesis in sweet potato roots. The enzyme was purified from the tissue as a cluster of isozymes with an average mw of 205K (fresh roots) or 159K (roots stored for 3 mon.). On SDS polyacrylamide gel electrophoresis, one large subunit of 98K mw and several small ones of 47${\sim}57K mw were observed. From the mw data and the results of peptide mapping and immunoelectrophoretic blotting using mono- and polyclonal antibodies, it was deduced that a large part of the large subunit was cleaved at the middle part of the peptide chain to give rise to the small subunits, and on storage, the enzyme molecules were further modified by proteolysis. During the course of phosphorylase purification, a proteinaceous inhibitor of the enzyme was isolated. It had a mw of 250K and was composed of 5 identical subunits of 51K mw. In the direction of starch synthesis, the inhibitor showed a noncompetitive kinetics with a Ki of $1.3{\times}10^{-6}\;M$. By immunohistochemical methods, both the enzyme and the inhibitor were located on the cell wall and amyloplast. Crossreacting materials of the inhibitor were present in spinach leaf, potato tuber and rice grain. These findings indicate the wide occurrence of the inhibitor and also imply its possible participation in regulating starch phosphorylase activity in vivo.

Ginseng saponins(GS), protopanaxadiol saponins(PD) and protopanaxatriol saponins (PT) were tested for the inhibition of the development of morphine tolerance and dependence antagonism of morphine analgesia and the loss of morphine tolerance and dependence in mice The results were as follows: 1. Inhibition of the development of morphine tolerance and dependence. 2. Antagonism of morphine analgesia. 3. Increase in the loss of morphine tolerance and dependence. Antagonism of morphine by ginseng saponins and its reversal by L-DOPA and 5-HTP suggest some possibility that catecholamines and serotonin levels might be associated with the results.

The preventive effect of Sosiho-Tang extract administered concurrently with methionine on hepatotoxicity induced by carbon tetrachoride (20% $CCl_4$ in olive oil, 5 ml/kg) in rats was studied. S-GOT values were decreased significantly by the concurrent administration of Sosiho-Tang extract 100 mg/kg with methionine 100 mg/kg and also Sosiho-Tang 200 mg/kg with methionine 100 mg/kg. S-GPT values were decreased remarkably by the concurrent administration of Sosiho-Tang extract 200 mg/kg with methionine 100 mg/kg. In histological observations, the pattern of the contrast group indicated the marked necrosis of the parenchymatous cells around the centrilobular area and the fatty changes of the hepatic cells around the midzonal area, but the concurrent administration of Sosiho-Tang extract 200 mg/kg and methionine 100 mg/kg revealed better improvements than their respective single administration in all pathological aspects.

We have isolated two new metabolites of territrem, designated as territrem $A'\;(TRA';\;C_{28}H_{30}O_{10})$ and $B'\;(TRB';\; C_{29}H_{34}O_{10})$ from chloroform extract of rice culture of Aspergillus terreus 23-1, using the same isolation procedure as that for territrem A, B and C(TRA, TRB, TRC). The present isolation procedure gave about 5 mg of TRA' and 10 mg of TRB' from 4 kg of rice culture per batch. Analysis of the high resolution mass spectrum showed that the molecular composition of TRA' and TRB' are $C_{28}H_{30}O_{10}$ and $C_{29}H_{34}O_{10}$ respectively, Some results of physicochemical properties were presented in this paper. Single crystal X-ray diffractometry of TRB' showed that the three dimensional structure of TRB' has not changed significantly from that of $TRB\;(C_{29}H_{34}O_9)$, except for the insertion of one oxygen atom into TRB to make additional pyran in the E-ring. It is also suggested that the aromatic moiety of TRA' is similar to that of $TRA\;(C_{28}H_{30}O_9)$ and the rest non-aromatic portions resemble to those of TRB'. The tremorgenic activity, lethality and inhibitory effect on acetylcholine esterase of TRA' and TRB' are greatly reduced comparing to that of TRA and TRB.

The smear method developed by Velaskar and Chitre was modified to allow the screening of plant extracts and/or fractions for platelet anti-aggregating activity. The modified smear method was also found suitable for massive screening of pure compounds. Sample fractions prepared from various plant extracts were examined for their effects against ADP, arachidonic acid (AA) or collagen induced platelet aggregations. Several solvent fractions of plant extracts including water fraction prepared from the methanol extract of Acanthopanax sp. was inhibitory against rat platelet aggregations. The activity guided treatments and fractionations of the water fraction from A. senticosus Max yielded two anti-platelet aggregatory substances, 3, 4-dihydroxybenzoic acid (I) and its artefact ethyl 3, 4-dihydroxybenzoate(II). The inhibitory activities of I and II against rat platelet aggregation were compared with that of aspirin, a known inhibitor of platelet aggregation. Discussions also included the results of the investigations on the structural activity relationships among the various dihydroxybenzoic acid derivatives against platelet aggregations induced by either one of ADP, AA or collagen.

Bioassay-directed isolation has yielded some cytotoxic substances against L1210 cell from the Korean traditional medicine. These include 5,2'-dihydroxy-6,7,8,6'-teramethoxyflavone $(IV,\;scutellaria\;root,\;ED_{50}\;=\;1.7\;{mu}g/ml)$, 7-geranyloxycoumarin $(XXXII,\;poncirus\;fruit,\;10.2\;{mu}g/ml) $and panaxydol $(I,\;white\;ginseng,\;0.03\;{mu}g/ml)$. IV, XXXII and their derivatives were synthesized in the purpose of in vivo tests and for observation of structure-activity relations. Among the flavone derivatives, 5,2',6'-trihydroxy-6,7,8-trimethoxy flavone (XVIII), 5-hydroxy-6,7,8-trimethoxy-6'-benzyloxyflavone (XVII) and 5,8-dihydroxy-6,7-dimethoxyflavone (X) showed the cytotoxicity which has no correlation to the flavone structures. Of the coumarins synthesized, 7,8-dihydroxycoumarin (XXVI), 6-7-dihydroxycoumarin (XXIX) and 6-hydroxy-5,7-dimethoxycoumarin (XXXI) showed considerable activities. Acetylated XXXI has moderate activity $(ED_{50}=17.2\;{mu}g/ml)$. Monobydroxycoumarins or their methyl and allyl ether were inactive. IV inhibits the growth of the solid form of S-180 by 70% at 40 mg/kg and shows T/C of 166% on the ascitic S-180 at 40 mg/kg. It strongly inhibits the activity of the membrane bounded ATPase from L1210 cell. The most cytotoxic fraction of the antitumor materials studied is the one from the trichosanthes root showing $ED_{50}=0. 0003\;{mu}g/ml$ against L1210 cell. This fraction, obtained from ethyl acetate extract, showed T/C of 130 and 135%, on ICR mice bearing S-180 and $BDF_1$ mice bearing L1210 at 10 mg/kg and 7.5 mg/kg, respectively.

It was our working hypothesis that introduction of 11-keto groups to 12-oleanene/ursene series of triterpenoids should endow them with corticoid-like activities, since pharmacological actions of glycyrrhetinic acid (GA) are known to be caused by inhibition on $corticoid-{\delta}^4-reductase$. 11-Keto-triterpenoids derived artificially in these studies, such as 11, 19-diketo-18, 19-secoursolic acid methyl ester(I), $11-keto-{\beta}-boswellic$ acid derivatives (IIa-IIc), 11-Keto-presenegenin dimethyl ester (III), II-keto-oleanolic acid derivatives (IVa-IVd) and 11-keto-hederagenin (V) possess the fundamental functions of ${\alpha},\;{\beta}-unsaturated$ ketone on C-11 and hydroxyl group on C-3, as like GA (VI). Additionally, they involve the carboxyl groups on rings A (II, III), D (I, III, IV, V) and E (VI), and the hydroxyl groups on rings A (III, V) and C (III). All the compounds competitively inhibited $corticoid-5{\beta}-reductase$, and the highest inhibitory potency appeared in I. All of them except $3,\;11-diketo-{\beta}-boswellic$ acid methyl ester (IIc) were more effective about five times to twice than GA. On carrageenin-induced edema test, compounds I and IVa-IVd showed anti-inflammatory activities, but III enhanced rather edema. Structure-activity relations were found in the aspects of hydrophilicity of ring A and hydrophobicity of rings C/D. The more they were hydrophilic in ring A and hydrophobic in rings C/D, the more they inhibited the enzyme. And the more they were hydrophobic in rings C/D, the more they exhibited antiiflammatory activities. However, the increased hydrophilicity in ring A resulted in increasing edema, probably due to a nonspecific inhibition on $aldosterone-5{\beta}-reductase$.

The preliminary antifertility test of Dictamnus albus(Rutaceae) showed that a methanol extract of root bark decreased fertility in rats when administered orally on days $1{\sim}10$ postcoitum. Hexane, chloroform, butanol and aqueous fractions from the methanol extract, were tested to produce the result that only the hexane fraction exhibited positive activity. The hexane fraction was subfractionated into acidic, alkaloidal and neutral subtractions and tested. Neutral subtraction showed positive activity. From the neutral subtraction, fraxinellone was isolated as an active principle. The timed-dosing experiments revealed that antifertility activity of fraxinellone appeared to be exerted after tubal exit of the ova to prevent implantations.