According to the traditional usage of the plant for antiinflammation and analgesia, Leucas aspera was tested for its prostaglandin (PG) inhibitory and antioxidant activities. The extract showed both activities, i.e., inhibition at 3 x 10(-4) g/ml against PGE(1)- and PGE(2)-induced contractions in guinea pig ileum and a 1, 1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging effect. The separation guided by the activities in these dual assay methods provided eight lignans and four flavonoids, LA-1- -12, among which LA-1- -7 and LA-10- -12 were identified as nectandrin B, meso-dihydroguaiaretic acid, macelignan, acacetin, apigenin 7-O-[6"-O-(p-coumaroyl)-beta-D-glucoside], chrysoeriol, apigenin, erythro-2-(4-allyl-2, 6-dimethoxyphenoxy)-1-(4-hydroxy-3-methoxyphenyl)propan-1-ol, myristargenol B, and machilin C, respectively. LA-8 was determined to be (-)-chicanine, the new antipode of the (+) compound, by spectroscopic methods including CD and ORD. Chiral-HPLC analysis of LA-9 showed that it was a mixture of two enantiomers, (7R, 8R)- and (7S, 8S)-licarin A. All of these components were first isolated from L. aspera. PG inhibition was observed in LA-1, LA-2, and LA-5, and antioxidant activity in LA-1- -3 and LA-8- -12.

Diffractaic acid and usnic acid were identified as the analgesic and antipyretic components of a lichen, Usnea diffracta. Both compounds showed an analgesic effect by the acetic acid-induced writhing and tail-pressure methods in mice. Regarding the effect on normal body temperature and LPS-induced hyperthermia in mice, diffractaic acid showed a significant effect only on the former and usnic acid only on the latter.

In view of their scientific understanding and potential usage, we have continuously investigated traditional medicines to clarify the active components and their pharmacological properties.1-4) Saposhnikovia root (Saposhnikovia divaricata SCHISCHKIN, syn. Ledebouriella seseloides WOLFF; Umbelliferae) is an important Chinese and Japanese traditional medicine, called Fang-feng and Bofu, respectively. 5,6) The herb is listed as a high-grade drug in the old Chinese Materia Medica, Shen Nung Pen Tsao Ching, and is applied for headaches, vertigo, generalized aching and arthralgia due to "wind, cold and dampness" in the traditional medical system.7) It has been used in many prescriptions, including those for the treatment of analgesic symptoms.Pharmacological experiments using the extract reported its suppression of adjuvant arthritis, inhibitory effects on the CNS and peptic ulcers, and fegrifugal analgesic, anti-convulsant and anti-inflammatory activities, etc.8-11) Chemical study on this herb had been done, and many components such as chromones, coumarins and polyacetylenes were isolated. [12][13][14] However, it has not been clearly identified which components contribute to the pharmacological efficacy, such as analgesia, of this traditional medicine. In Japan, Glehnia root, named Hama-Bofu (Glehnia littoralis FR. SCHMIDT ex MIQUEL; Umbelliferae), is used for the same purpose as Bofu (Saposhnikovia root), and in prescriptions the two medicines are often confused. With respect to Glehnia root, we recently identified the active components which are responsible for the analgesia and/or a prolongation effect on pentobarbitalinduced hypnosis caused by the inhibition of liver-metabolizing enzymes.2) Some of the active components in Glehnia root, such as furanocoumarins and polyacetylenes, are the same as the constituents in Bofu. By applying activity-oriented separation to the extract of Saposhnikovia root, the analgesic components of this herbal medicine can be clarified in this paper, and the activity-mechanisms of the components are also discussed. Results and DiscussionThe methanol extract of Saposhnikovia root showed an analgesic effect at a dose of 2 g/kg in mice by the acetic acidinduced writhing method. The extract also caused a prolongation effect on pentobarbital-induced hypnosis in mice at a dose of 3 g/kg. The separation of the extract was mainly carried out by following the writhing inhibition in mice with oral administration of samples as an isolation guide (Chart 1). Partition using ethyl acetate, n-butanol and water concentrated the activity to the ethyl acetate fraction, which was further separated by Sephadex LH-20 chromatography. The obtained analgesic fraction, fr. 1-C, also showed the prolongation effect on pentobarbital-induced sleeping time in mice. The following silica gel chromatography, however, gave two active fractions, fr. 2-A and fr. 2-B. The latter fraction showed only analgesia at a dose of 150 mg/kg and no prolongation effect at a dose of 200 mg/kg, while the former exhibited both effects...

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1 Anisatin, a toxic, insecticidally active component of Sikimi plant, is known to act on the GABA system. In order to elucidate the mechanism of anisatin interaction with the GABA system, wholecell and single-channel patch clamp experiments were performed with rat dorsal root ganglion neurons in primary culture. 2 Repeated co-applications of GABA and anisatin suppressed GABA-induced whole-cell currents with an EC 50 of 1.10 mM. No recovery of currents was observed after washout with anisatin-free solution.3 However, pre-application of anisatin through the bath had no eect on GABA-induced currents. The decay phase of currents was accelerated by anisatin. These results indicate that anisatin suppression of GABA-induced currents requires opening of the channels and is use-dependent. 4 Anisatin suppression of GABA-induced currents was not voltage dependent. 5 Picrotoxinin attenuated anisatin suppression of GABA-induced currents. [ 3 H]-EBOB binding to rat brain membranes was competitively inhibited by anisatin. These data indicated that anisatin bound to the picrotoxinin site. 6 At the single-channel level, anisatin did not alter the open time but prolonged the closed time. The burst duration was reduced and channel openings per burst were decreased indicating that anisatin decreased the probability of openings.

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A screening study focusing on immunomodulatory activity of the EtOAc extract of an Ascomycete, Chaetomium seminudum, has afforded a known epipolythiodioxopiperazine, chetomin (1), together with three new chetomin-related metabolites named chetoseminudins A (2), B (3), and C (4). Among these four metabolites, 1 and 2 have been deduced as the immunosuppressive features of this fungus.

Fractionation guided by immunomodulatory activity of the EtOAc extract of the Ascomycete Eupenicillium crustaceum has afforded two new naturally occurring products, 4'-oxomacrophorin D (1) and 4'-oxomacrophorin A (2), as the immunosuppressive components of this fungus [1: 3-hydroxy-3-methylglutaryl (HMG) conjugate of 2]. The structures including the absolute configurations of 1 and 2 have been determined on the basis of chemical correlation of 1 with macrophorin D (3). The absolute configuration of the HMG moiety in 3 has been revised from 3R to 3S.