Lipopolysaccharide (LPS) is an endotoxin which induces septic shock syndrome and stimulates the production of inflammatory mediators such as NO, tumor necrosis factor-a (TNF-a), interleukins, prostanoids and leukotrienes. [1][2][3] These mediators frequently result from excessive stimulation of the host immune system through complex signal transductions and lead to hypotension and multiorgan dysfunction with a high mortality rate. 4,5) In patients with sepsis, TNF-a plays a major role in the associated systemic toxicity.6) Loss of hepatic function is one of the hallmarks of the development of multiple-organ failure associated with severe sepsis. 7,8) There have been reports that the synthetic compounds IRFI 042, 9) tyrphostin AG 126, 10) and SR 27388 11) show significant protection against lethality due to septic shock, and lysophosphatidylcholine (LPC) can effectively prevent and treat sepsis and microbial infections. 12) Recently, protective compounds against sepsis have been reported from medicinal plants. 13,14) The protective activity against sepsis-induced lethality of the methanol extracts of about 100 Korean medicinal plants was determined based on the sepsis model induced by lipopolysaccharide/D-galactosamine, from which Saururus chinensis (Saururaceae) was chosen as one of the active plants. Saururus chinensis (Saururaceae) is a perennial herbaceous plant with potential therapeutic utility in treatment of various diseases such as edema, jaundice, gonorrhea, anti-pyretic, diuretic, and anti-inflammatory agents in Korean folk medicine.15) Previous chemical studies of the genus Saururus have shown the presence of more than 20 lignans, [16][17][18][19] some of which exhibited neuroleptic, 20) hepatoprotective, 21) and antifeedant activities. 22) A triene, 12,13-dehydrogeranylgeraniol, was recently demonstrated to inhibit intracellular reactive oxygen species (ROS)-catalyzed oxidation within HL-60 cells.23) Different types of compounds have also been isolated from Saururus species including aristolactams, flavonoids, anthraquinones, and fruanoditerpenes. [24][25][26][27] In this paper, the isolation and activity of twelve known lignans as anti-septic shock agents from the roots of this plant are described. MATERIALS AND METHODS General ProceduresMelting points were measured by Fisher-Johns melting point apparatus and are uncorrected. Optical rotations were measured using a JASCO DIP-1000 (Tokyo, Japan) automatic digital polarimeter. The NMR spectra were recorded on a Bruker 250 MHz (DMX 250, Germany) spectrometer using Bruker's standard pulse program. Samples were dissolved in CDCl 3 -d 1 or CD 3 OD, and chemical-shifts were reported in ppm downfield from TMS. The FABMS spectrum was measured by VG TRIO 2A mass spectrometer. Stationary phases for column chromatography (Silica gel 60, 70-230 and 230-400 mesh and Lichroprep RP-18 gel, 40-63 mm, Merck) and TLC plates (Silica-gel 60 F 254 and RP-18 F 254, 0.25 mm, Merck) were purchased from Merck KGaA (Darmstadt, Germany). Spots were detected under UV radiation ...

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Thirteen lignans, erythro-austrobailignan-6 (1), meso-dihydroguaiaretic acid (2), sauchinone (3), 1'-epi-sauchinone (4), saucerneol D (5), manassantin B (6), manassantin A (7), nectandrin B (8), machilin D (9), saucerneol F (10), saucerneol G (11), saucerneol H (12) and saucerneol I (13), were isolated from the ethyl acetate extract of the roots of Saururus chinensis. Among these compounds, 5 showed potent inhibitory activities against DNA topoisomerase I and II, and 5, 6, 7 and 10 showed mild cytotoxicities against HT-29 (IC(50) values; 13, 12, 11, and 10 microM, respectively) and HepG2 cell lines (IC(50) values; 16, 11, 12, and 11 microM, respectively).

Twenty five compounds including ten triterpenes (1-3, 5-11), six flavonoids (12-15, 24, 25), five lignans (17, 18, 21-23), two butenyl clohexnone glycosides (19-20), one fructofuranoside (16) and one fatty acid (4) were isolated from the roots of Ulmus davidiana var. japonica. The structures of those compounds were identified by comparing their physicochemical and spectral data with those of published in literatures. All the compounds were evaluated for DNA topoisomerase inhibitory activities and cytotoxicities. Among the purified compounds, 4 and 19 showed more potent inhibitory acitivities (IC(50): 39 and 19 μM, respectively) than camptothecin, as the positive control (IC(50): 46 μM) against topoisomerase I. Compounds, 4, 10, 12, 19, 24 and 25 showed strong inhibitory activities toward DNA topoisomerase II (IC(50): 0.1, 0.52, 0.47, 0.42, 0.17 μM and 17 nM, respectively), which were more potent than that of etoposide as positive control (IC(50): 20 μM). In A549 cell line, 5 and 6 showed cytotoxicities (IC(50): 4 μM and 3 μM, respectively, with IC(50) of camptothecin as positive control: 10.3 μM). In the HepG2 cell line, 3, 5 and 7 showed cytotoxicity (IC(50): 4, 3 and 4 μM, respectively, with IC(50) of camptothecin: 0.3 μM). Compounds 6, 12 and 23 showed cytotoxicities in the HT-29 cell line (IC(50): 19, 19 and 15 μM, respectively, with IC(50) of camptothecin: 2 μM).

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