This review describes the dynamics in macromolecular structures and assemblies. First, it is shown that kinetic studies of the hydrogen exchange reactions of proteins and nucleic acids can provide useful information on the structure and fluctuation of such biological macromolecules. Next, a new method is proposed to approach the elementary process of protein assembly. Finally, it is demonstrated that lateral diffusion of lipid haptens and membrane bound antibody has an important role for antigen-antibody reaction on a cell surface.

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Several amino acids and ammonia were allowed to react with L-ascorbic acid or D-glucose in 0.1 M phosphate buffer (pH 7.0) at 37°C for 2 months. The reaction mixtures were submitted to mutagenic assay and structural analysis. The browning products from L-tryptophan (0.25M) and L-ascorbic acid (1M) showed a DNA-damaging potency to B. subtilis. They also gave a mutagenic activity to S. typhimurium TA 100 but not TA 98. By extracting the reaction products with benzene and ethyl acetate, followed by purifying them through silica-gel column and thin layer chromatographies (Kiesel-gel 60), 6 β-carbolyl and 4 furyl derivatives were identified. Among them, 1-(2-furyl)-9H-pyrido-[3, 4-b] indole exhibited a mutagenic activity to S. typhimurium TA 100 with or without S-9 mixture and 1-(2-furyl)-9H-pyrido [3, 4-b] indole-3-carboxylic acid showed the activity to S. typhimurium TA 100 only in the absence of S-9 mixture.

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From North Carolina Helenium autumnale L. (Compositae, Japanese name : dangogiku), new sesquiterpene lactones, 3-O-tigloylcarolenalin (4), 11, 13-dehydrocarolenalin (5), carolenalin-4-O-β-D-glucoside (7), 3-O-tigloylcarolenalone (10), 3-O-angeloylcarolenalone (11), carolenalol (12), 4-O-tigloyl-11, 13-dihydroautumnolide (14), 6-O-angeloylplenolin (15) and 11, 13-dihydroarnifolin (19) were isolated along with some known components, carolenalin (1), carolenin (3) and carolenalone (9), and their structures were proposed on the basis of spectral and chemical evidence.

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10, 11-Dihydro-10-oxo-5H-dibenzo [a, d] cycloheptenylacetic acids (2a-c) and 11-oxo analogs (2d-f) were prepared from the corresponding diphenylmethanediacetic acids by cyclization. 2-(10, 11-Dihydro-11-oxo-5H-dibenzo [a, d] cyclohepten-2-yl) propionic acid was also prepared from its acetic acid derivative (2e) in four steps. Their antiinflammatory and ulcerogenic effects were examined. Some of them showed potent antiinflammatory activity in carrageenin rat paw edema and weaker effect than indomethacin in causing gastrointestinal lesions.

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We have previously communicated the hemostatic activity in the crude drugs employed for hemostatics. This communication is one of the studies on isolation of an active substance, a hemostatic component in Sanchi Gingseng Radix. An active principle which was designated as "dencichine" was isolated by suitable combination of counter current distribution, gelfiltration (Sephadex LH-20) and ionexchange chromatography (CM-Sephadex C-25) from H₂O-extract. Dencichine was identified as β-N-oxalo-L-α, β-diaminopropionic acid (neurotoxin).

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α-(or β-) Naphthol, and p-substituted phenols (or thiophenol) were condensed to 4-chloro-3-nitrobenzotrifluoride or 5-bromo-2-chloronitrobenzene to form their nitro compounds (1-6). Nitro compounds 1-6 were reduced with stannous chloride and hydrochloric acid to the corresponding amino compounds (7-12). Amino compounds (7-12 and 13-16, 23-28, 39-41) were condensed with 5-chloro- and 3, 5-dichloro salicylic acid using phosphorus trichloride in xylene to form their salicylanilide (17-22, 29-38a, 38b, 42-46). Aniline derivatives (47-49) were condensed with salicylaldehyde to form their Schiff bases (50-55). Salicylanilides (17, 20, 29, 31, 34) were acetylated with acetic anhydride and pyridine to form acetylated compounds (56-60). Antimicrobial tests of the synthesized compounds showed that salicylanilides had a strong antimicrobial activity against some gram-positive bacteria.

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Neuropharmacological actions of the water extract of Perillae Herba, and perillaldehyde which is one of the main components of the essential oil of this crude drug, were examined. In ddY strain mice, a dose of 4g/kg, p.o. of the water extract and 100mg/kg, p.o. of perillaldehyde exerted a significant prolongation of sleeping time induced by the administration of hexobarbital Na but did not show any effects on the body temperature and the rotating rod performance. On the laryngeal reflex in cats, the water extract and perillaldehyde exerted a clear inhibitory effect, and such inhibitory effects were also observed on the excitable membranes by using an isolated snail's neuron and frog's sciatic nerve fibers. With the continuous administration of the water extract or perillaldehyde, only the water extract showed a depressive effect on the spontaneous locomoter activity in Fischer strain rats. These results suggest that the water extract of Perillae Herba and perillaldehyde have a depressive action on the central nervous system.

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Anti-inflammatory, analgesic and anti-pyretic activities of tolmetin sodium were studied in comparison with aspirin, ibuprofen and indomethacin. Analgesic ED₅₀ value of tolmetin sodium against AgNO₃-induced arthritic pain in rats was 27.2mg/kg, p.o. and the potency was about 20 times, twice and 3 times that of aspirin, ibuprofen and mefenamic acid, respectively, and about 1/3 and 1/13 times that of diclofenac sodium and indomethacin, respectively. Tolmetin sodium showed a significant therapeutic effect on traumatic hind paw edema in rats at a dose of 20mg/kg, p.o. or more, and the potency was 4 times or more that of aspirin, about the same as ibuprofen and about 1/10 times that of indomethacin. The anti-pyretic ED₅₀ value of tolmetic sodium in adjuvantinduced febrile rats was 15.8mg/kg, p.o., and the potency was about 2.5 times that of aspirin and about 1/13 and 1/40 times that of ibuprofen and indomethacin, respectively. Tolmetin sodium showed an anti-pyretic effect on lipopolysaccharide-induced fever in rabbits at a dose of 40 mg/kg, p.o. or more, and the potency was about 3 times that of aspirin, about the same as ibuprofen and about 1/10 times that of indomethacin. These results confirm the previous results that tolmetin sodium has possessed a relatively potent inhibitory activity on inflammatory pain and acute inflammation.

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From Hedyotis corymbosa LAM., which has been recently used in chinese medicine as a useful drug against some tumors, were isolated six iridoids, asperuloside, scandoside methyl ester, asperulosidic acid, geniposidic acid, scandoside and deacetylasperulosidic acid.

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The essential oil of Rumex japonicus HOUTT. collected in Kashiwara-shi was examined. The oil yield of the aerial part was 0.002% and that of the underground part was 0.004%. The essential oils were separated into individual component by the combination of a chemical method and preparative gas or elution chromatography. Sixty-one compounds in the oils were characterized. The characteristic component was diacetin.

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