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Abstract: The cytotoxic activity against some tumor cell lines of 16 commonly used species of Asarum was evaluated in this study. All of these plants were widely used in Asian countries as traditional medicines or folk medicines. Their inhibitory activities against four tumor cell lines (HL-60, BGC-823, KB and Bel-7402) were compared. It was observed that 10 of the tested extracts (eight ethanol extracts and two water extracts) among 32 extracts of these plants showed cytotoxic activity. Those 95% ethanol extractions from A. caudigerellum, A. forbesii, A. inflatum and A. maximum exhibited the highest cytotoxic activity, and 95% ethanol extracts or water extracts of A. sieboldii var. seoulense, A. himalaicum, A. splendens and A. crispulatum showed selective activity against one or two cells among the tested tumor cells. This is the first report of Asarum plants possessing cytotoxic activity against tumor cell lines. [Copyright &y& Elsevier]

Five new phenanthrene derivatives: 9-ethoxy-7-methoxy-aristololactam IV (1) , norcepharadione A N - β - d -glucopyranoside (2) , aristololactamoside I (3) , aristololactamoside II (4) and aristothiolactoside (5) together with eleven known phenanthrene derivatives ( 6 – 16 ) were isolated from the ethanol extract of the roots and rhizomes of Asarum heterotropoides var. mandshuricum . The aristololactams with substitution of ethoxy at C-9 position ( 1 , 9 , and 10 ) and the sulfur-containing phenanthrene derivative ( 5 ) were reported in the genus Asarum for the first time. Furthermore, six phenanthrene glucoside derivatives ( 2 – 5 , 13 and 14 ) were also found in this genus for the first time and compounds 7 and 9 – 15 were isolated from the genus Asarum for the first time. Six of them ( 1 , 2 , 9 , 10 , 13 and 14 ) were submitted to cytotoxicity test against human renal proximal tubular epithelial cell lines (HK-2) using MTT and LDH assays. Compounds 1 and 10 showed significant cytotoxic activity against HK-2 cell lines with IC 50 values of 18.18 and 20.44 μmol/L in MTT assay and 84.36 and 35.06 μmol/L in LDH assay, respectively. Compound 9 showed moderate cytotoxicity in MTT assay with IC 50 values of 95.60 μmol/L, but no cytotoxicity in LDH assay. Compounds 2 , 13 and 14 showed cytotoxic effect in neither MTT assay nor LDH assay. Considering the other nephrotoxic phenanthrene derivatives ( 6 , 8 , 12 , 15 and 16 ) previously tested, the results implied the potency of renal toxicity of this herb used as a medicine. [ABSTRACT FROM AUTHOR]

Abstract: Eubacterium limosum ZL-II is an anaerobic bacterium with demethylated activity, which was isolated from human intestinal bacteria in our previous work. In this study, the flavonolignan constituents of Silybi Fructus were biotransformed by E. limosum 1 [1] Eubacterium limosum. ZL-II, producing four new transformation products — demethylisosilybin B (T1), demethylisosilybin A (T2), demethylsilybin B (T3) and demethylsilybin A (T4), among which T1 and T2 were new compounds. Their chemical structures were identified by ESI-TOF/MS, 1H NMR, 13C NMR, HMBC and CD spectroscopic data. The bioassay results showed that the transformation products T1–T4 exhibited significant inhibitory activities on Alzheimer's amyloid-? 42 (A?42 2 [2] Amyloid-?. ) aggregation with IC50 values at 7.49?M–10.46?M, which were comparable with that of the positive control (epigallocatechin gallate, EGCG 3 , [3] Epigallocatechin gallate. at 9.01?M) and much lower than those of their parent compounds (at not less than 145.10?M). The method of biotransformation by E. limosum ZL-II explored a way to develop the new and active lead compounds in Alzheimer's disease from Silybi Fructus. However, the transformation products T1–T4 exhibited decreased inhibitory activities against human tumor cell lines comparing with their parent compounds. [Copyright &y& Elsevier]

Abstract: One alkyl glycoside, saussurostelloside A (1), two phenolic glycosides, saussurostellosides B1 (2) and B2 (3), and 27 known compounds, including eleven flavonoids, seven phenolics, six lignans, one neolignan, one phenethyl glucoside and one fatty acid, were isolated from an ethanol extract of Saussurea stella (Asteraceae). Their structures were elucidated by NMR, MS, UV, and IR spectroscopic analysis. Of the known compounds, (+)-medioresinol-di-O-β-d-glucoside (7), picraquassioside C (10), and diosmetin-3′-O-β-d-glucoside (27) were isolated from the Asteraceae family for the first time, while (+)-pinoresinol-di-O-β-d-glucoside (6), di-O-methylcrenatin (11), protocatechuic acid (14), 1,5-di-O-caffeoylquinic acid (17), formononetin (28), and phenethyl glucoside (29) were isolated from the Saussurea genus for the first time. The anti-inflammatory activities of three new compounds (1–3), five lignans ((−)-arctiin (4), (+)-pinoresinol-4-O-β-d-glucoside (5), (+)-pinoresinol-di-O-β-d-glucoside (6), (+)-medioresinol-di-O-β-d-glucoside (7) and (+)-syringaresinol-4-O-β-d-glucoside (8)), one neolignan (picraquassioside C (10)), and one phenolic glycoside (di-O-methylcrenatin (11)) were evaluated by testing their inhibition of the release of β-glucuronidase from PAF-stimulated neutrophils. Only compound 5 showed moderate inhibition of the release of β-glucuronidase, with an inhibition ratio of 39.1%. [Copyright &y& Elsevier]

Constituents of the fruit of Sinopodophyllum hexandrum (Royle) Ying (Sinopodophylli Fructus) were investigated. A new flavonoid, 8,2′-diprenylquercetin 3-methyl ether along with 9 known compounds were isolated and identified. Among them, the new compound 8,2′-diprenylquercetin 3-methyl ether exhibited cytotoxic activities against MDA-231 and T47D breast cancer cell lines, quercetin, kaempferol and rutin were isolated from Sinopodophylli Fructus for the first time. [Copyright &y& Elsevier]

Three new flavonoids, ephedroside A (1), ephedroside B (2), ephedroside C (3), together with fifty-four known compounds 4 – 57 were isolated from the EtOH extract of the herbaceous stems of Ephedra sinica. The structures of these compounds were elucidated by spectroscopic techniques, as well as by comparison with literature data. Thirty-eight of these compounds were isolated from the genus Ephedra for the first time. The antimicrobial activities of eight compounds were tested by measuring the minimum inhibitory concentrations (MIC) against bacteria (both Gram positive and Gram negative) and fungi, and were found to be in the range of 0.105–0.926 mM. Among them, compound 2 showed the best antimicrobial activity against Pseudomonas aeruginosa with MIC value of 0.105 mM. [Display omitted] [ABSTRACT FROM AUTHOR]

8,2′-Diprenylquercetin 3-methyl ether, a natural product with prominent anti-breast cancer activity, is the main active constituent of Sinopodophylli Fructus. A high-performance liquid chromatography with a diode array detector coupled with electrospray ionization ion trap time-of-flight multistage mass spectrometry (HPLC-DAD-ESI-IT-TOF-MSn) method was established and applied to profile and identify the metabolites of 8,2′-diprenylquercetin 3-methyl ether as well as study their distribution in rat organs for the first time. A total of 100 new metabolites were tentatively identified in rats. The metabolic reactions of 8,2′-diprenylquercetin 3-methyl ether in rats in vivo were hydroxylation, methylation, glucuronidation, dehydrogenation, sulfation, polymerization and cysteine conjugation as well as the specific reactions of leucine/isoleucine, proline, and vitamin C conjugation. The detected metabolites included 77 in faeces, 50 in urine, 11 in plasma, 50 in the small intestine, 32 in the stomach, 23 in the liver, 9 in the lungs, 9 in the spleen, 8 in the heart, and 6 in the kidneys. The results indicated that the small intestine, stomach, and liver were the major organs for the distribution of 8,2′-diprenylquercetin 3-methyl ether metabolites. Furthermore, 27 metabolites showed various bioactivities predicted by the analysis of " PharmMapper ", among which 9 metabolites showed anti-cancer activity. These results are very useful for understanding the metabolism and pharmacological actions as well as the effective forms and toxic actions of 8,2′-diprenylquercetin 3-methyl ether in vivo ; moreover, they will lay the foundation for further studies on the metabolism of prenylflavonoid compounds. Unlabelled Image [ABSTRACT FROM AUTHOR]